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Sample records for peripheral analgesic effect

  1. Quaternary ammonium salt derivatives of allylphenols with peripheral analgesic effect

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    A. B de Oliveira

    1991-01-01

    Full Text Available Ammonium salt derivatives of natural allylphenols were synthesized with the purpose of obtaining potential peripheral analgesics. These drugs, by virtue of their physicochemical properties, would not be able to cross the blood brain barrier. Their inability to enter into the central nervous system (CNS should prevent several adverse effects observed with classical opiate analgesics (Ferreira et al., 1984. Eugenol (1 O-methyleugenol (5 and safrole (9 were submitted to nitration, reduction and permethylation, leading to the ammonium salts 4, 8 and 12. Another strategy applied to eugenol (1, consisting in its conversion to a glycidic ether (13, opening the epoxide ring with secondary amines and methylation, led to the ammonium salts 16 and 17. All these ammonium salts showed significant peripheral analgesic action, in modified version of the Randall-Sellito test (Ferreira et al. 1978, at non-lethal doses. The ammonium salt 8 showed an activity comparable to that of methylnalorphinium, the prototype of an ideal peripheral analgesic (Ferreira et al., 1984.

  2. Quaternary ammonium salt derivatives of allylphenols with peripheral analgesic effect

    Scientific Electronic Library Online (English)

    A. B de, Oliveira; T. H. A., Silva; S. H., Ferreira; B. B., Lorenzetti.

    Full Text Available SciELO Brazil | Language: English Abstract in english Ammonium salt derivatives of natural allylphenols were synthesized with the purpose of obtaining potential peripheral analgesics. These drugs, by virtue of their physicochemical properties, would not be able to cross the blood brain barrier. Their inability to enter into the central nervous system ( [...] CNS) should prevent several adverse effects observed with classical opiate analgesics (Ferreira et al., 1984). Eugenol (1) O-methyleugenol (5) and safrole (9) were submitted to nitration, reduction and permethylation, leading to the ammonium salts 4, 8 and 12. Another strategy applied to eugenol (1), consisting in its conversion to a glycidic ether (13), opening the epoxide ring with secondary amines and methylation, led to the ammonium salts 16 and 17. All these ammonium salts showed significant peripheral analgesic action, in modified version of the Randall-Sellito test (Ferreira et al. 1978), at non-lethal doses. The ammonium salt 8 showed an activity comparable to that of methylnalorphinium, the prototype of an ideal peripheral analgesic (Ferreira et al., 1984).

  3. Peripheral analgesic effects of ketamine in acute inflammatory pain.

    DEFF Research Database (Denmark)

    Pedersen, J L; Galle, T S

    1998-01-01

    BACKGROUND. This study examined the analgesic effect of local ketamine infiltration, compared with placebo and systemic ketamine, in a human model of inflammatory pain. METHODS: Inflammatory pain was induced by a burn (at 47 degrees C for 7 min; wound size, 2.5 x 5 cm) on the calf in 15 volunteers on 3 separate days with 7-day intervals. They received either (1) subcutaneous infiltration with ketamine in the burn area (local treatment) and contralateral placebo injections, or (2) subcutaneous ketamine contralateral to the burn (systemic treatment) and placebo in the burn area, or (3) placebo on both sides. The study was double-blinded and the order of the treatments was randomized. Hyperalgesia to mechanical and heat stimuli was examined by von Frey hairs and contact thermodes (3.75 and 12.5 cm2), and pain was rated using a visual analog scale (0-100). RESULTS: The burns produced significant hyperalgesia. Local ketamine infiltration reduced pain during the burn injury compared with systemic treatment and placebo (P < 0.01). Heat pain thresholds were increased by local ketamine treatment compared with placebo immediately after injection (P < 0.03), and so were the mechanical pain thresholds (P = 0.02). Secondary hyperalgesia and suprathreshold pain responses to heat and mechanical stimuli were not significantly affected by local ketamine. No difference between local ketamine and placebo could be detected 1 h and 2 h after the burn. CONCLUSIONS: Ketamine infiltration had brief local analgesic effects, but several measures of pain and hyperalgesia were unaffected. Therefore, a clinically relevant effect of peripheral ketamine in acute pain seems unlikely.

  4. Effectiveness of the association between carbamazepine and peripheral analgesic block with ropivacaine for the treatment of trigeminal neuralgia

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    Laurinda Lemos

    2010-10-01

    Full Text Available Laurinda Lemos1,2, Ramalho Fontes3, Sara Flores2, Pedro Oliveira4, Armando Almeida11Life and Health Sciences Research Institute (ICVS, School of Health Sciences, Campus de Gualtar, University of Minho, Braga, Portugal; 2Hospital Center of Alto Ave, Unit of Fafe, Fafe, Portugal; 3Department of Neurology, Hospital São Marcos, Braga, Portugal; 4Products and Systems Engineering, Campus de Azurém, University of Minho, Guimarães, PortugalAbstract: Treatment of trigeminal neuralgia (TN is achieved by using adjuvant analgesics like antiepileptics, with carbamazepine (CBZ being the first-line approach for TN patients, although side effects may be present. Other approaches using gabapentin, namely when associated with peripheral analgesic block of TN trigger points with the local anesthetic ropivacaine (ROP, resulted in decreased pain and daily drug intake (reduced side effects. This study evaluates if the association between CBZ and the peripheral block with ROP reinforces the clinical value of CBZ. In this parallel, double-blinded study, idiopathic TN patients were randomized to receive during 4 weeks either CBZ (CBZ; n = 21 or CBZ associated with the peripheral analgesic block using ROP (CBZ + ROP; n = 24. The primary outcome measures were the following: i pain intensity, evaluated by the numerical rating scale; ii number of pain crises; and iii number needed to treat. Evaluation points were at the beginning (day 1 and end (day 29 of treatment and after a follow-up of 5 months (month 6. Both protocols resulted in a decrease of pain intensity and number of pain crises, but only the association CBZ + ROP showed i a significant stronger reduction in pain intensity at month 6 and ii a significant decrease in the daily dose of CBZ given to patients (both at day 29 and month 6. In contrast, the daily dose in CBZ-only patients remained constant or even increased. The number needed to treat for the association CBZ + ROP over the CBZ protocol reduced from 5 at the end of the 4-week treatment to 3 after the 5-month follow-up. Data reinforce the use of CBZ as a primary tool to control pain in TN patients, as the association CBZ + ROP i improves the clinical qualities of CBZ, ii strongly reduces the daily dose of CBZ, and iii reduces the potential side effects attributed to high doses of CBZ.Keywords: trigeminal neuralgia, carbamazepine, ropivacaine, therapeutical association, pain intensity, daily dose

  5. Analgesic effect of piracetam on peripheral neuropathic pain induced by chronic constriction injury of sciatic nerve in rats.

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    Mehta, Ashish K; Bhati, Yogendra; Tripathi, Chakra D; Sharma, Krishna K

    2014-08-01

    Despite immense advances in the treatment strategies, management of neuropathic pain remains unsatisfactory. Piracetam is a prototype of nootropic drugs, used to improve cognitive impairment. The present study was designed to investigate the effect of piracetam on peripheral neuropathic pain in rats. Neuropathic pain was induced by the chronic constriction injury of the sciatic nerve. Following this, piracetam was intraperitoneally administered for 2 weeks in doses of 50, 100 and 200 mg/kg, and pain was assessed by employing the behavioural tests for thermal hyperalgesia (hot plate and tail flick tests) and cold allodynia (acetone test). After the induction of neuropathic pain, significant development of thermal hyperalgesia and cold allodynia was observed. The administration of piracetam (50 mg/kg) did not have any significant effect on all the behavioural tests. Further, piracetam (100 mg/kg) also had no effect on the hot plate and tail flick tests; however it significantly decreased the paw withdrawal duration in the acetone test. Piracetam in a dose of 200 mg/kg significantly modulated neuropathic pain as observed from the increased hot plate and tail flick latencies, and decreased paw withdrawal duration (in acetone test). Therefore, the present study suggests the potential use of piracetam in the treatment of neuropathic pain, which merits further clinical investigation. PMID:24831122

  6. The analgesic effect of dipyrone in peripheral tissue involves two different mechanisms: neuronal K(ATP) channel opening and CB(1) receptor activation.

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    dos Santos, Gilson Gonçalves; Dias, Elayne Vieira; Teixeira, Juliana Maia; Athie, Maria Carolina Pedro; Bonet, Ivan José Magayewski; Tambeli, Cláudia Herrera; Parada, Carlos Amilcar

    2014-10-15

    Dipyrone (metamizole) is an analgesic pro-drug used to control moderate pain. It is metabolized in two major bioactive metabolites: 4-methylaminoantipyrine (4-MAA) and 4-aminoantipyrine (4-AA). The aim of this study was to investigate the participation of peripheral CB1 and CB2 cannabinoid receptors activation in the anti-hyperalgesic effect of dipyrone, 4-MAA or 4-AA. PGE2 (100ng/50µL/paw) was locally administered in the hindpaw of male Wistar rats, and the mechanical nociceptive threshold was quantified by electronic von Frey test, before and 3h after its injection. Dipyrone, 4-MAA or 4-AA was administered 30min before the von Frey test. The selective CB1 receptor antagonist AM251, CB2 receptor antagonist AM630, cGMP inhibitor ODQ or KATP channel blocker glibenclamide were administered 30min before dipyrone, 4-MAA or 4-AA. The antisense-ODN against CB1 receptor expression was intrathecally administered once a day during four consecutive days. PGE2-induced mechanical hyperalgesia was inhibited by dipyrone, 4-MAA, and 4-AA in a dose-response manner. AM251 or ODN anti-sense against neuronal CB1 receptor, but not AM630, reversed the anti-hyperalgesic effect mediated by 4-AA, but not by dipyrone or 4-MAA. On the other hand, the anti-hyperalgesic effect of dipyrone or 4-MAA was reversed by glibenclamide or ODQ. These results suggest that the activation of neuronal CB1, but not CB2 receptor, in peripheral tissue is involved in the anti-hyperalgesic effect of 4-aminoantipyrine. In addition, 4-methylaminoantipyrine mediates the anti-hyperalgesic effect by cGMP activation and KATP opening. PMID:25058903

  7. The analgesic action of topical diclofenac may be mediated through peripheral NMDA receptor antagonism

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    Dong, Xu-Dong; Svensson, Peter

    2009-01-01

    The analgesic mechanism underlying the efficacy of topical diclofenac in the treatment of musculoskeletal pain is incompletely understood. The present study investigated whether intramuscular injection of diclofenac (0.1mg/ml, approximately 340microM) could attenuate jaw-closer muscle nociceptor discharge and mechanical sensitization induced by activation of peripheral 5-hydroxytryptamine (serotonin) or excitatory amino acid receptors in anesthetized Sprague-Dawley rats. Diclofenac inhibited nociceptor discharge evoked by NMDA, but had no effect on nociceptor discharge evoked by 5-hydroxytryptamine or AMPA. Subsequent experiments revealed that diclofenac-mediated inhibition of NMDA-evoked nociceptor discharge was competitive. Intramuscular injection of 5-hydroxytryptamine, NMDA and AMPA also decreased nociceptor mechanical threshold, however, only the mechanical sensitization produced by NMDA was reversed by diclofenac. Co-administration of the proinflammatory prostaglandin PGE(2) did not alter the ability ofdiclofenac to significantly attenuate NMDA-evoked nociceptor discharge or NMDA-induced mechanical sensitization. Intramuscular injection of either diclofenac or the competitive NMDA receptor antagonist DL-2-amino-5-phosphonovalerate (50mM) alone could elevate nociceptor mechanical threshold for a 30min period post-injection. The present study indicates that in vivo, diclofenac can exert a selective, competitive inhibition of peripheral NMDA receptors at muscle concentrations achievable after topical administration of diclofenac containing preparations. This property may contribute to the analgesic effect of topical diclofenac when used for muscle pain.

  8. Botulinum toxin type A induces direct analgesic effects in chronic neuropathic pain.

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    Ranoux, Danie?le; Attal, Nadine; Morain, Franc?oise; Bouhassira, Didier

    2008-01-01

    OBJECTIVE: Botulinum toxin type A (BTX-A) has been reported to have analgesic effects independent of its action on muscle tone, possibly by acting on neurogenic inflammation. Such a mechanism may be involved in peripheral neuropathic pain. METHODS: A possible direct analgesic effect of BTX-A pain processing was investigated in 29 patients with focal painful neuropathies and mechanical allodynia using a randomized, double-blind, placebo-controlled design. Patients received a one-time intraderm...

  9. Antinociceptive peripheral effect of Achillea millefolium L. and Artemisia vulgaris L.: both plants known popularly by brand names of analgesic drugs.

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    Pires, Júlia Movilla; Mendes, Fúlvio R; Negri, Giuseppina; Duarte-Almeida, Joaquim M; Carlini, Elisaldo A

    2009-02-01

    The hydroalcohol extracts of Achillea millefolium L. (AM) and Artemisia vulgaris L. (AV), both belonging to the Asteraceae family, were evaluated by the hot plate, writhing, formalin and intestinal transit tests in an attempt to confirm their folk use as analgesic, antiinflammatory and antispasmodic agents. AM 500 and 1000 mg/kg significantly inhibited abdominal contortions by 65% and 23%, respectively, whereas AV 500 and 1000 mg/kg inhibited them by 48% and 59%, respectively. None of the extracts produced differences in the intestinal transit in mice, nor in the response time in the hot plate or in the immediate or late responses in the formalin test. In HPLC/DAD analyses 'fingerprint', monitored at 360 and 270 nm, both hydroalcohol extracts showed the same flavonoid glycoside as a principal constituent, which was identified as rutin. A high content of caffeic acid derivatives were also found in both extracts. The main differences were observed at 240 nm: AM had a higher content of rutin, while in AV the hydroxybenzoic acid derivative was the major component. PMID:18844327

  10. Analgesic effects of dexamethasone in burn injury.

    DEFF Research Database (Denmark)

    Werner, Mads U; Lassen, Birgit Vibeke

    2002-01-01

    BACKGROUND AND OBJECTIVES: Glucocorticoids are well-known adjuvant analgesics in certain chronic pain states. There is, however, a paucity of data on their analgesic efficacy in acute pain. Therefore, the aim of the study was to examine the analgesic effects of dexamethasone in a validated burn model of acute inflammatory pain in humans. METHODS: Twenty-two volunteers were investigated in a double-blind, randomized, placebo-controlled cross-over study. Intravenous dexamethasone 8 mg or placebo was administered on 2 separate study days. Two hours after drug administration, a first-degree burn injury was produced on the medial aspect of the nondominant calf (12.5 cm2, 47 degrees C for 7 minutes). Quantitative sensory testing included pain ratings to thermal and mechanical stimuli (visual analog scale [VAS]), assessments of thermal and mechanical detection thresholds, and areas of allodynia and secondary hyperalgesia. RESULTS: The burn injury induced significant increases in erythema (P .6). There were no significant differences between treatments in regard to skin erythema (P >.8), thermal or mechanical thresholds (P >.2), thermal or mechanical pain response (P >.2), or mechanical secondary hyperalgesia (P >.2). Dexamethasone had no analgesic effects in normal skin. CONCLUSIONS: The study indicates that systemic administration of dexamethasone 2 hours before a burn injury does not reduce the inflammatory-mediated changes in quantitative sensory thresholds, pain perception, or skin erythema in humans.

  11. Catastrophizing delays the analgesic effect of distraction

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    Campbell, Claudia M.; Witmer, Kenny; Simango, Mpepera; Carteret, Alene; Loggia, Marco L.; Campbell, James N.; Haythornthwaite, Jennifer A.; Edwards, Robert R.

    2010-01-01

    Behavioral analgesic techniques such as distraction reduce pain in both clinical and experimental settings. Individuals differ in the magnitude of distraction-induced analgesia, and additional study is needed to identify the factors that influence the pain relieving effects of distraction. Catastrophizing, a set of negative emotional and cognitive processes, is widely recognized to be associated with increased reports of pain. We sought to evaluate the relationship between catastrophizing and...

  12. Opioid Receptors: Toward Separation of Analgesic from Undesirable Effects

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    Law, P. Y.; Reggio, Patricia H.; Loh, H. H.

    2013-01-01

    The use of opioid analgesics for pain has always been hampered by their many side effects; in particular, the addictive liability associated with chronic use. Recently, attempts to develop analgesic agents with reduced side effects have targeted either the putative opioid receptor splice variants or the receptor heterooligomers. This review discusses the potential for receptor splice variant- and the hetero-oligomer-based discovery of new opioid analgesics. We also examine an alternative appr...

  13. Opioid receptors: toward separation of analgesic from undesirable effects.

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    Law, Ping-Yee; Reggio, Patricia H; Loh, Horace H

    2013-06-01

    The use of opioid analgesics for pain has always been hampered by their many side effects; in particular, the addictive liability associated with chronic use. Recently, attempts to develop analgesic agents with reduced side effects have targeted either the putative opioid receptor splice variants or the receptor hetero-oligomers. This review discusses the potential for receptor splice variant- and the hetero-oligomer-based discovery of new opioid analgesics. We also examine an alternative approach of using receptor mutants for pain management. Finally, we discuss the role of the biased agonism observed and the recently reported opioid receptor crystal structures in guiding the future development of opioid analgesics. PMID:23598157

  14. Catastrophizing delays the analgesic effect of distraction.

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    Campbell, Claudia M; Witmer, Kenny; Simango, Mpepera; Carteret, Alene; Loggia, Marco L; Campbell, James N; Haythornthwaite, Jennifer A; Edwards, Robert R

    2010-05-01

    Behavioral analgesic techniques such as distraction reduce pain in both clinical and experimental settings. Individuals differ in the magnitude of distraction-induced analgesia, and additional study is needed to identify the factors that influence the pain relieving effects of distraction. Catastrophizing, a set of negative emotional and cognitive processes, is widely recognized to be associated with increased reports of pain. We sought to evaluate the relationship between catastrophizing and distraction analgesia. Healthy participants completed three sessions in a randomized order. In one session (Pain Alone), pain was induced by topical application of a 10% capsaicin cream and simultaneous administration of a tonic heat stimulus. In another session (Pain+Distraction), identical capsaicin+heat application procedures were followed, but subjects played video games that required a high level of attention. During both sessions, verbal ratings of pain were obtained and participants rated their degree of catastrophizing. During the other session (Distraction Alone) subjects played the video games in the absence of any pain stimulus. Pain was rated significantly lower during the distraction session compared to the "Pain Alone" session. In addition, high catastrophizers rated pain significantly higher regardless of whether the subjects were distracted. Catastrophizing did not influence the overall degree of distraction analgesia; however, early in the session high catastrophizers had little distraction analgesia, though later in the session low and high catastrophizers rated pain similarly. These results suggest that both distraction and catastrophizing have substantial effects on experimental pain in normal subjects and these variables interact as a function of time. PMID:20188470

  15. Analgesic effect of Irvingia gabonensis stem bark extract.

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    Okolo, C O; Johnson, P B; Abdurahman, E M; Abdu-Aguye, I; Hussaini, I M

    1995-02-01

    Irvingia gabonensis is used medicinally in most parts of tropical Africa for the treatment of a number of ailments. In West Africa the Mende tribe of Sierra Leone uses the stem bark to relieve pain. In order to establish a pharmacological rationale for the traditional use of this plant as a remedy for pain, the water and ethanol extracts of the powdered stem bark were screened for analgesic activity and compared with standard analgesic drugs. The water extract and morphine protected the mice from heat-induced pain. In contrast, the ethanol extract and metamizole sodium showed very low level of analgesic activity in this test. However, using tail pressure as a source of pain, the water and ethanol extracts, metamizole sodium and morphine offered protection to the mice against pain stimuli. Morphine and the water extract were more potent as analgesic agents in heat than non-heat pain test. The analgesic effects of the water extract and morphine were blocked by a non-selective opioid receptor antagonist, naloxone in both tests, whereas the analgesic effects of the ethanol extract and metamizole sodium were not antagonized by the same dose of the opioid antagonist. The data presented in this study suggest that the active principle(s) in the water extract has analgesic profile similar to that of the narcotic analgesic and the ethanol extract might contain compound(s) that behave like non-narcotic analgesic agent. These findings provide for the first time the pharmacological basis for the folkloric use of Irvingia gabonensis in the relief of pain. PMID:7776661

  16. [Analgesic and sedative effects of the Chinese drug rhizoma Paridis].

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    Wang, Q; Xu, G; Jiang, Y

    1990-02-01

    The analgesic and sedative actions of Chinese drug Rhizoma Paridis are reported. All of the 6 experimented species and varieties in common use are obviously effective. Among them Paris polyphylla var. chinensis, P. polyphylla var. yunnanensis are stronger in analgesic action. Sedative action of P. fargesii, P. polyphylla var. chinensis, P. thibetica is also strong. In addition, pariphyllin A and gracillin were also used in the experiment. PMID:2390171

  17. Analgesic effect of the aqueous and ethanolic extracts of clove

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    Mina Kamkar Asl

    2013-04-01

    Full Text Available Objective: The beneficial effects of clove on toothache have been well documented. We have also previously shown the analgesic effects of clove essential oil. The present work was done to investigate the analgesic effects of the aqueous extract of clove using hot plate test. The possible role of opioid receptors in the analgesic effects of clove was also investigated using naloxone. Materials and Methods: Ninety male mice were divided into nine groups: (1 Saline, (2-4 Aaqueous (Aq 50, Aq 100, and Aq 200 groups which were treated with 50, 100, and 200 mg/kg of aqueous extract of clove, respectively, (5-7 Ethanolic (Eth 50, Eth 100, and Eth 200 groups which were treated with 50, 100, and 200 mg/kg of ethanolic extract of clove, respectively, and (8-9 Aq 100- Naloxone and Aq 200- Naloxone which were pretreated with 4 mg/kg of naloxone before injection of 100 or 200 mg/kg of the aqueous extract. The hot plate test was performed as a base record 10 min before injection of drugs and consequently repeated every 10 minutes after the injection. Results: The maximal percent effect (MPE in the animal groups treated with 50, 100, and 200 mg/kg of aqueous extract was significantly higher than the control group. Pretreatment with naloxone reduced the analgesic effects of both 100 and 200 mg/kg of the aqueous extract. Administration of all three doses of the ethanloic extract also non-significantly increased the MPE. Conclusion: The results of the present study showed that aqueous extract of clove has analgesic effect in mice demonstrated by hot plate test which is reversible by naloxone. The role of opioid system in the analgesic effect of clove might be suggested. However, more investigations are needed to elucidate the exact mechanism(s.

  18. Alterations in endocannabinoid tone following chemotherapy-induced peripheral neuropathy: Effects of endocannabinoid deactivation inhibitors targeting fatty-acid amide hydrolase and monoacylglycerol lipase in comparison to reference analgesics following cisplatin treatment

    OpenAIRE

    Guindon, Jose?e; Lai, Yvonne; Takacs, Sara M.; Bradshaw, Heather B.; Hohmann, Andrea G.

    2012-01-01

    Cisplatin, a platinum-derived chemotherapeutic agent, produces mechanical and cold allodynia reminiscent of chemotherapy-induced neuropathy in humans. The endocannabinoid system represents a novel target for analgesic drug development. The endocannabinoid consists of endocannabinoids (e.g. anandamide (AEA) and 2-arachidonoylglycerol (2-AG)), cannabinoid receptors (e.g. CB1 and CB2) and the enzymes controlling endocannabinoid synthesis and degradation. AEA is hydrolyzed by fatty-acid amide hyd...

  19. Analgesic properties of a peripherally acting and GalR2 receptor-preferring galanin analog in inflammatory, neuropathic, and acute pain models.

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    Metcalf, Cameron S; Klein, Brian D; McDougle, Daniel R; Zhang, Liuyin; Smith, Misty D; Bulaj, Grzegorz; White, H Steve

    2015-01-01

    There are ongoing efforts to develop pain therapeutics with novel mechanisms of action that avoid common side effects associated with other analgesics. The anticonvulsant neuropeptide galanin is a potent regulator of neuronal excitability and has a well established role in pain modulation, making it a potential target for novel therapies. Our previous efforts focused on improving blood-brain-barrier penetration and enhancing the metabolic stability of galanin analogs to protect against seizures. More recently, we designed peripherally acting galanin analogs that reduce pain-related behaviors by acting in the periphery and exhibit preferential binding toward galanin receptor (GalR)2 over GalR1. In this study, we report preclinical studies of a monodisperse oligoethylene glycol-containing galanin analog, NAX 409-9 (previously reported as GalR2-dPEG24), in rodent analgesic and safety models. Results obtained with NAX 409-9 in these tests were compared with the representative analgesics gabapentin, ibuprofen, acetylsalicylic acid, acetaminophen, and morphine. In mice that received intraplantar carrageenan, NAX 409-9 increased paw withdrawal latency with an ED50 of 6.6 mg/kg i.p. NAX 409-9 also increased the paw withdrawal threshold to mechanical stimulation following partial sciatic nerve ligation in rats (2 mg/kg). Conversely, NAX 409-9 had no effect in the tail flick or hot plate assays (up to 24 mg/kg). Importantly, NAX 409-9 did not negatively affect gastrointestinal motility (4-20 mg/kg), respiratory rate (40-80 mg/kg), or bleed time (20 mg/kg). These studies illustrate that this nonbrain-penetrating galanin analog reduces pain behaviors in several models and does not produce some of the dose-limiting toxicities associated with other analgesics. PMID:25347995

  20. Analgesic, anti-inflammatory and venotonic effects of Cissus quadrangularis Linn.

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    Panthong, Ampai; Supraditaporn, Wanicha; Kanjanapothi, Duangta; Taesotikul, Tawat; Reutrakul, Vichai

    2007-03-21

    Cissus quadrangularis, a medicinal plant indigenous to Asia and Africa, is used for many ailments, especially for the treatment of hemorrhoid. The effects associated with hemorrhoid, i.e. analgesic and anti-inflammatory activities as well as the venotonic effect of the methanol extract of C. quadrangularis (CQ) were assessed in comparison with reference drugs. In the analgesic test, CQ provoked a significant reduction of the number of writhes in acetic acid-induced writhing response in mice. CQ also significantly reduced the licking time in both phases of the formalin test. The results suggest peripheral and central analgesic activity of CQ. In acute phase of inflammation CQ elicited the inhibitory effect on the edema formation of the rats' ear induced by ethyl phenylpropiolate as well as on the formation of the paw edema in rats induced by both carrageenin and arachidonic acid. It is likely that CQ is a dual inhibitor of arachidonic acid metabolism. In addition, CQ exerted venotonic effect on isolated human umbilical vein similarly to the mixture of bioflavonoids, i.e. 90% diosmin and 10% hesperidin. The results obtained confirmed the traditional use of C. quadrangularis for the treatment of pain and inflammation associated with hemorrhoid as well as reducing the size of hemorrhoids. PMID:17095173

  1. Analgesic and Anti-Arthritic Effect of Enicostemma littorale Blume

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    Mohamed M. Shabi

    2014-11-01

    Full Text Available Enicostemma littorale (Blume, the folk medicine is used for rheumatic pain and it was selected for scientific validation. The 85% methanolic extract obtained from the whole plant of Enicostemma littorale has been assessed for analgesic and anti-inflammatory activity. The analgesic activity has been evaluated by hot plate and tail immersion method and the anti-inflammatory and antioxidant activities are evaluated by Complete Freund’s adjuvant induced arthritic model. The results of the evaluation of analgesic activity in hot plate and tail immersion method revealed that the extract exhibits significant activity at 150 mg/kg body weight and the effect is found to increase dose dependently. In Freund’s adjuvant induced arthritis, Enicostemma littorale is found to decrease the paw volume (15.81%. Significant protection is also observed by elevating antioxidant enzymes. In conclusion, the 85% methanolic extract of Enicostemma littorale possesses significant analgesic and anti-inflammatory activities in Freund’s adjuvant induced arthritic model in rats.

  2. Dexmedetomidine produced analgesic effect via inhibition of HCN currents.

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    Yang, Ying-cong; Meng, Qing-tao; Pan, Xia; Xia, Zhong-yuan; Chen, Xiang-dong

    2014-10-01

    The purpose of this study was to investigate the mechanism by which systemic dexmedetomidine exerts analgesic effect and examine effect of dexmedetomidine on hyperpolarization-activated cyclic nucleotide-gated (HCN) channels currents. The experiments were performed on C57BL/6 J and HCN1 knockout mice. The analgesic effects of intraperitoneal dexmedetomidine (10-40 ?g/kg) were measured by a tail-flick test. Whole-cell clamp recordings were used to examine the properties of cloned HCN subunit currents expressed in HEK 293 cells under control condition and dexmedetomidine administration (0.1-10 ?M). Injection of dexmedetomidine caused a clear time and dose-related increase in the tail-flick latency of both wild type and knockout mice. Compared with the wild type group, the MPE (maximum possible effect) of tail-flick latency induced by 30 ?g/kg and 40 ?g/kg dexmedetomidine in knockout mice was significantly lower. The ?2-adrenergic receptor antagonist yohimbine (5 ?g/kg) reduced the MPE of dexmedetomidine (30 ?g/kg) both in wild type and knockout mice. Dexmedetomidine(0.1-10 ?M) inhibited HCN1 and HCN2 channel currents in HEK 293 cells, caused a decrease of maximal currents, an increase of inhibition rate of hyperpolarization-activated currents (Ih), and a negative shift in V1/2. We conclude that dexmedetomidine produces a dose-dependently analgesic effect, and the effect is likely due to the inhibition of HCN currents. PMID:24998873

  3. Analgesic and anti-arthritic effect of Corallocarpus epigaeus

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    Subashini Uthrapathy

    2011-12-01

    Full Text Available Rheumatoid arthritis is a chronic inflammatory joint disease associated with the development of oxidative stress and inflammation. The safety and efficacy profile of 85% methanolic extract of Corallocarpus epigaeus (CE was evaluated in the present study. In safety profile LD50 value was determined by carrying out an acute toxicity study. In efficacy profile, the analgesic activity was evaluated by both hot plate and tail immersion tests. The anti-inflammatory activity was assessed by carrageenan-induced paw edema and anti-arthritic effect by complete Freund's adjuvant induced arthritis. Phytochemical screening of different CE extracts and quantitative analysis of both raw herb and 85% methanolic extract have been also carried out. The methanolic extract displayed analgesic activity by increasing the response time in both hot plate and tail immersion method. Extract exhibited 23,19% of anti-inflammatory activity and 33,59% of anti-arthritic effect in complete Freund's adjuvant induced paw edema. The CE extract increased the antioxidant level, along with a decrease of the oxidative stress developed by complete Freund's adjuvant induced arthritis. In conclusion, CE is a rich source of phytochemicals with analgesic, anti-inflammatory and antioxidant activities.

  4. Analgesic effects of gabapentine in tonsillectomy

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    Waleed Abdelmageed, Salah Abdelrazik

    2010-01-01

    Objectives: To evaluate the preemptive effects of gabapentin on postoperative pain relief and its effect on meperidine consumption in patients undergoing tonsillectomy. Methods: This study took place in King Abdulaziz Naval Base Hospital in the year 2009. Sixty patients ASA I and II were randomly assigned in a prospective randomized double- blind placebo-control clinical trial. Gabapentine 1200 mg or placebo was given orally two hours before induction of anesthesia to patients undergoing tons...

  5. Analgesic effects of receptin, a chemically modified cobratoxin from Thailand cobra venom.

    Science.gov (United States)

    Zhang, Hui-Ling; Han, Rong; Chen, Zhi-Xing; Gu, Zhen-Lun; Reid, Paul F; Raymond, Laurence N; Qin, Zheng-Hong

    2006-09-01

    Objective To investigate the analgesia induced by receptin (REC), a chemically modified cobratoxin (CTX, a long-chain postsynaptic alpha -neurotoxin from Thailand cobra venom), and the effects of atropine and naloxone on antinociceptive activity of REC in rodent pain models. Methods REC was administered intraperitoneally (5 mg/kg, 7.07 mg/kg, or 10 mg/kg, i.p.) or intra-cerebral venticularly (62.5 mu g/kg, i.c.v.). The antinociceptive action was determined using the hot-plate test, the acetic acid writhing test and tail flick assay in mice and rats. The involvement of cholinergic and the opioid peptidergic systems in REC-induced analgesia were examined by pretreatment of animals with atropine (Atr; 0.5 mg/kg, i.m. or 10 mg/kg, i.p.) or naloxone (Nal; 3 mg/kg, i.p.). The effect of REC on motor activity was tested using the Animex test in mice. Results REC (5 mg/kg, 7.07 mg/kg or 10 mg/kg, i.p.) exhibited a dose-dependent analgesic action in mice as determined with hot-plate test and acetic acid writhing test. The significant analgesia of REC was seen 2 h to 3 h after its administration. In the rat-tail flick assay, the administration of REC at 62.5 mu g/kg (1/160 of systemic dose; i.c.v.) produced marked analgesic effects. Atropine at 0.5 mg/kg (i.m.), 10 mg/kg (i.p.) or naloxone at 3 mg/kg (i.p.) failed to block the analgesic effects of REC. REC at the highest effective dose of 10 mg/kg did not change the spontaneous mobility of mice. Conclusion These results demonstrate that REC has analgesic effect. This activity appears to be mediated through the peripheral nervous system though central nervous system may contribute to REC' s analgesic effects. The central cholinergic system and opioid peptidergic system appear not to be involved in the antinociceptive action of REC. PMID:17690726

  6. ACUTE CENTRAL AND PERIPHERAL ANALGESIC ACTIVITY OF ETHANOLIC EXTRACT OF THE LEAVES OF CLERODENDRUM VISCOSUM (EECV IN RODENT MODELS

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    Chandra Shekar

    2012-09-01

    Full Text Available Pain, inflammation and pyrexia are the most common disturbing symptom a person experiences in life. Numerous drugs are available in the market for relieving these symptoms and which are sold over the counter. However they have high tendency of having adverse drug reaction from a trivial nausea and vomiting to gastric irritation leading to peptic ulcer, perforation and even death. The aim of the study was to investigate the acute peripheral activity of Ethanolic Extract of the leaves of Clerodendrum viscosum (EECV by acetic acid induced writhing reflex test in mice and acute central analgesic activity by tail immersion method in rats. Dried powdered leaves of Clerodendrum viscosum were subjected to solvent extraction by using 90 % ethanol. Based on acute oral toxicity study according to Organization for Economic Cooperation and Development (OECD guidelines No. 423, three doses of the test drug was selected (100, 200 & 400mg/kg for mice  and (75, 150 & 300 mg/kg for rats, and were subjected to acute analgesic activity. The Ethanolic Extract of the leaves of Clerodendrum viscosum (EECV showed significant (p

  7. Evaluation of the analgesic and anxiolytic effects of Dracocephalum polychaetum

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    Mojtaba Khodami

    2011-10-01

    Full Text Available Introduction: Dracocephalum polychaetum bornum is exclusively found in a limited geographical area in the Kerman province; It is used by the local people for treatment of abdominal pain, meteorism and musculoskeletal pain. No study has been performed on the effects of D. polychaetum bornum, so the aim of this work was to assess the role of the extract and essential oil of this plant on pain and anxiety assessed by formalin test and elevated plus-maze (EPM, respectively, in male rats. Methods: Analgesic effects: One hundred twelve NMRI male rats were divided into 14 groups. Aqueous extract and essential oil were administered to 8 groups at doses of 25, 50, 100 and 200 mg/kg i.p., while 2 groups were treated with normal saline, and the last 4 groups (sham positive received ASA (300 mg/kg and morphine (2.5 mg/kg. Anxiolytic effect: Forty-two NMRI male rats were divided into 7 groups. Four groups were injected intraperitoneally with 25, 50, 100 and 200 mg/kg of the extract of the plant and 2 groups were injected with normal saline (control group and 1 mg/kg diazepam (positive sham. Anxiolytic effect was evaluated by EPM. Results: The results showed that the extract but not the essential oil at the dose of 200 mg/kg had a significant analgesic effect 25, 30 and 35 minutes after administration. The findings on the anxiolytic effect revealed that there was no significant difference between groups treated with different doses. Conclusion: This study showed that D. polychaetum bornum had analgesic effects.

  8. SEDATIVE AND ANALGESIC EFFECTS OF DETOMIDINE HYDROCHLORIDE IN GOATS

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    A N Tunio, A. B. Kalhoro And I. H. Kathio

    2003-01-01

    The sedative and analgesic effects of three dose rates of detomidine (40, 50 and 60µg/kg body weight) were studied in six goats. Moderate to deep sedation occurred after administration of 40µg/kg of detomidine as compared to deep sedation produced by 50 and 60µg/kg of detomidine. The degree, onset and duration of sedation and onset and duration of maximum sedation were all dose dependent. Skin analgesia and recumbency were produced in all animals with higher doses (50 and 60µg/kg) and in ...

  9. Comparing Early Postoperative Period Analgesic Effect of Dexketoprofene Trometamol and Lornoxicam in Mediastinoscopy Cases

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    Gonul Sagiroglu

    2011-04-01

    Full Text Available Objective: In this study, we aimed comparing early postoperative period analgesic effectiveness and the effects on opioid consumption of intravenous dexketoprofen and lornoxicam that are given preemptively. Materials and Methods: Forty patients, planned elective mediastinoscopy, were included in this prospective randomized study. These patients were classified in two groups, group D for dexketoprofene trometamol and group L for lornoxicam, randomly. 20 minutes before the operation 50 mg dexketoprofene trometamol and 8 mg lornoxicam were injected intravenously for group D and group L respectively. In postoperative intensive care unit, pain scores, mean arterial pressures, heart rates and peripheric O2 saturations of patients were recorded at 0, 10, 20, 60, 90 and 120th minutes. Results: When we evaluate the VAS score of the groups, there was a significant decrease in group D in all measured timesstatistically compairing to group L (p0.05. Conclusion: Since intravenous dexketoprofen, applied preemptively, has more potent analgesic effect and causing less opioid consumption in early postoperative period, is better than intravenous lornoxicam.

  10. Effects of metabolites of the analgesic agent dipyrone (metamizol) on rostral ventromedial medulla cell activity in mice.

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    Maione, Sabatino; Radanova, Lilyana; De Gregorio, Danilo; Luongo, Livio; De Petrocellis, Luciano; Di Marzo, Vincenzo; Imming, Peter

    2015-02-01

    The molecular mechanism of action of dipyrone, a widely used antipyretic and non-opioid analgesic drug, is still not fully understood. Actions upon peripheral inflamed tissues as well as the central nervous system, especially upon the PAG-RVM axis, have been suggested. Dipyrone is a prodrug and its activity is due to its immediate conversion to its active metabolites. We tested the effect of two recently discovered metabolites of dipyrone, the arachidonoyl amides of 4-methylaminoantipyrine and 4-aminoantipyrine, on the neurons of the rostral ventromedial medulla (RVM), which are part of the descending pathway of antinociception. These compounds reduced the activity of ON-cells and increased the activity of OFF-cells. Both CB1 and TRPV1 blockade reversed these effects, suggesting that the endocannabinoid/endovanilloid system takes part in the analgesic effects of dipyrone. PMID:25557763

  11. Analgesic effects of ?-phenylethylamine and various methylated derivatives in mice.

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    Mosnaim, Aron D; Hudzik, Thomas; Wolf, Marion E

    2014-09-01

    Administration of ?-phenylethylamine (PEA), the simplest endogenous neuroamine, and various methylated PEA derivatives including ?-methyl PEA (amphetamine, AMP) elicits analgesia in mice. Five or 20 min after intraperitoneal PEA injection of as little as 6 mg/kg resulted in an increased latency response time (from 2.4 ± 0.4 to 8.5 ± 2.3 or 7.0 ± 3.0 s, respectively) to the thermal stimulus (hot-plate test), which reached statistical significance at the 15 mg/kg (20 min; 13.1 ± 0.4 s) or 25 mg/kg dose (5 min; 15.3 ± 4.1 s). This PEA effect, was dose-dependent (albeit non-linear: 6, 12, 15, 25, 50 and 100 mg/kg), reached the cut-off time of 45 s at the upper PEA dose (5 min), and it was consistently enhanced by pretreatment with the monoamine oxidase inhibitor pargyline (P). Methylated PEA derivatives (15 and 100 mg/kg dose) produced various degrees of analgesia (in decreasing order p-Me PEA > PEA > N,N-diMe PEA > N-Me PEA) which, likewise to PEA itself, were consistently increased by P and declined over time (mice tested 5, 20 and 60 min after amine injection); small but statistically significant o- and ?-Me PEA antinociceptive effects (5 min) were observed only at the higher dose (in the presence of P for ?-Me PEA). A small analgesic effect was observed after the administration of AMP (5 or 10 mg/kg) which failed, even after P, to reach statistically significance. Independent of the amine and concentration tested, individual compound's antinociceptive properties were reliably increased by P (exception of AMP), decreased by reserpine (R) or haloperidol (H), and remained essentially unchanged after naloxone (N) administration suggesting the involvement of catecholamines, but not opioid peptides, in their observed analgesic effects. Injection of P + N produced results similar to those seen after P alone. Under the experimental conditions described neither P, R, H or N had any effects by themselves. These findings suggest additional understanding of the mechanism of action responsible for the analgesic effects of these amines would be of interest, leading further to controlled studies on their alleged usefulness as weight reducing agents and sport performance enhancers. PMID:24965531

  12. The Effect of Saliva Officinalis Hydroalcoholic Extract on Analgesic Effect of Morphine in Rat

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    A Arzi

    2011-11-01

    Full Text Available Background and Objective: There are some reports in Iranian traditional medicine concerning the anti-inflammatory effect of Saliva Officinalis (SO. In the present study with the aim of decreasing analgesic dose of morphine, analgesic effect of different doses of SO hydroalcoholic extract alone and associated with morphine were evaluated by tail flick in rats. Subjects and Methods: Analgesic effects of SO hydroalcholic extract at doses of 200, 400, 600, 800 and 1000 mg/kg, i.p. were investigated. Then the influence of these doses associated with analgesic dose of morphine (2.5 mg/kg was evaluated. Rats were placed into restrainer and then transferred into the tail flick apparatus with the intensity 55 Cº and cut off time= 10 sec. In order to verify the role of opioid receptors on analgesic effect of SO extract, naloxone (1mg/kg, i.p. was administered to one group of rats 15 min before receiving 800 mg/kg extract. Then, the data were analyzed by two-way ANOVA followed by LSD post hoc test and significant difference between groups was accepted with P<0.05. Results: The Data have shown that, the SO extract relieved pain in tail-flick test dose dependently and the most effective dose was 800 mg/kg. The maximum analgesic effect of the extract combined with morphine was observed at time point 45 min. Naloxane, opioid receptor antagonist could reduce analgesic effect of the extract. Conclusion: On the basis the results obtained in this study, it could be suggested that the SO extract potentiates morphine anti-nociceptive effect and this means that the opioid system may be involved in the analgesic effect of this plant extract. Sci Med J 2011;10(5:505-13

  13. Analgesic effect of Persian Gulf Conus textile venom

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    Nasim Tabaraki

    2014-10-01

    Results: SDS-PAGE indicated 12 bands ranged between 6 and 180 KDa. Finally, ten ng of Conus crude venom showed the best analgesic activity in formalin test. No death observed up to 100 mg/kg. Analgesic activity of crude venom was more significant (P

  14. SEDATIVE AND ANALGESIC EFFECTS OF DETOMIDINE HYDROCHLORIDE IN GOATS

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    A. N. Tunio., A. B. Kalhoro and I.H. Kathio1

    2003-07-01

    Full Text Available The sedative and analgesic effects of three dose rates of detomidine (40, 50 and 60µg/kg body weight were studied in six goats. Moderate to deep sedation occurred after administration of 40µg/kg of detomidine as compared to deep sedation produced by 50 and 60µg/kg of detomidine. The degree, onset and duration of sedation and onset and duration of maximum sedation were all dose dependent. Skin analgesia and recumbency were produced in all animals with higher doses (50 and 60µg/kg and in three animals with lower dose (40µg/kg. Duration of recumbency was 22.66 ± 1.45, 35.16 ± 1.68 and 55.66 ± 1.64 minutes after administration of 40, 50 and 60µg/kg of detomidine, respectively.

  15. Pure analgesics in a rheumatological outpatient clinic

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    M.A. Cimmino

    2011-09-01

    Full Text Available Objective: Pure analgesics are only rarely used by Italian clinicians and this holds true also for rheumatologists. This work is concerned with an evaluation of the use of analgesics in a rheumatological outpatient clinic during the period 1989-1999. Methods: The records of 1705 patients consecutively seen at the clinic were downloaded on a specifically built website. Results: 4469 visits were considered. In 260 of them (5.8%, analgesics were prescribed to 234 (13.7% patients. The number of patients with a prescription of analgesics steadily increased during the years 1989-1999. The diagnoses in patients assuming analgesics were: osteoarthritis (47.1%, inflammatory arthritis (24.2%, soft tissue rheumatisms (13.7%, nonspecific arthralgia/myalgia (7.5%, and connective tissue diseases (2.6%. Peripheral analgesics were used in 188 (82.5% patients and central analgesics were used in the remaining 40 patients (17.5%. Analgesic drugs were used mainly in degenerative joint conditions. The indications for analgesics in the 55 patients with inflammatory arthrits were: (a partial or total remission of arthritis; for this reason non-steroidal anti-inflammatory drugs were no longer required in 18 patients; (b to increase the analgesic effect of NSAIDs in 23 patients; (c contraindications to NSAIDs in 14 patients (renal failure in 2 patients, gastritis in 10, allergy and bleeding in the remaining two. Conclusions: About 14% of our outpatients were treated with analgesics with an increasing trend in the examined period. The main indications for analgesics are degenerative conditions but they can be used also in selected patients with arthritis.

  16. The analgesic effect of betamethasone administered to outpatients before conscious sedation in gynecologic and obstetric surgery.

    Science.gov (United States)

    Pace, Maria Caterina; Palagiano, Antonio; Passavanti, Maria Beatrice; Iannotti, Mario; Sansone, Pasquale; Maistro, Massimo; Pace, Leonardo; Bulletti, Carlo; Aurilio, Caterina

    2008-04-01

    Conscious sedation, used with or without peripheral or central blocks, is an elective anesthetic technique used for many outpatient procedures. The aim of this study was to evaluate the effects of a single pre-anesthetic dose of betamethasone (4 mg) on intraoperative and postoperative pain in 380 women, 18 to 75 years old, undergoing gynecologic and obstetric surgery (diagnostic curettage, operative and diagnostic hysteroscopy, conization, minilaparoscopy, cone biopsy, endometrial ablation, assisted reproduction techniques, and induced and therapeutic abortion) in a outpatient service. In this randomized, double-blind, placebo-controlled study, the patients were divided into two equal groups according to a computer-generated randomized list. One group received 4 mg of betamethasone i.v. as a premedication (group B), whereas the placebo group (group P) received only saline. All patients underwent the same sedation, associated with a peripheral block. Pain was evaluated using a 5-point verbal rating scale during surgery, after 2 h, and on discharge. In group B, intraoperative and postoperative pain was significantly less frequent than in group P (P < 0.001). Consequently, fewer women belonging to group B requested additional analgesic drugs during and after surgery (P < 0.01). Patients in group B also experienced a greater degree of satisfaction (P < 0.01). Briefly, a single dose of betamethasone seemed to reduce the incidence and severity of perioperative pain after gynecologic outpatient surgery. PMID:18443343

  17. Effects of epinephrine and cortisol on the analgesic activity of metyrosine in rats.

    Science.gov (United States)

    Albayrak, Yavuz; Saglam, Mustafa Bahadir; Yildirim, Kadir; Karatay, Saliha; Polat, Beyzagul; Uslu, Turan; Suleyman, Halis; Akcay, Fatih

    2011-09-01

    Some endogenous hormones (epinephrine and cortisol) can change an individual's pain threshold. Propranolol is a non-selective ? adrenergic receptor blocker which antagonises the anti-inflammatory effect of non-steroidal anti-inflammatory drugs via the ?1 and ?2 adrenergic receptors. The roles of epinephrine and cortisol were investigated in the analgesic activity of metyrosine in rats with reduced epinephrine levels induced by metyrosine. Pain threshold measurement was performed using an analgesimeter with different doses and the single or combined usage of metyrosine, prednisolone, metyrapone and propranolol in rats. Epinephrine and corticosterone levels were measured by high-performance liquid chromatography in metyrosineadministered rats. Metyrosine reduces the epinephrine levels without affecting the corticosterone levels, thereby creating an analgesic effect. It was determined that prednisolone did not have an analgesic effect in rats with normal epinephrine levels, but its analgesic activity increased with a parallel decrease in the epinephrine levels. Similarly, the combined use of prednisolone and metyrosine provided a stronger analgesic effect than that rendered by metyrosine alone. The strongest analgesic effect, however, was observed in the group of rats with the lowest epinephrine level in whom the metyrosine + prednisolone combination was administered. The findings of this study may be useful in severe pain cases in which the available analgesics are unable to relieve the individual's pain. PMID:21975814

  18. Evaluation of anti-inflammatory, analgesic, and antipyretic effects of ethanolic extract of Pedalium murex Linn. fruits.

    Science.gov (United States)

    Patel, Mahendra K; Mandavia, Divyesh R; Patel, Tejas K; Barvaliya, Manish J; Tripathi, C B

    2013-01-01

    This study investigated the possible anti-inflammatory, analgesic, and antipyretic effects of ethanolic extract of Pedalium murex Linn. fruits in selected experimental animal models. Anti-inflammatory activity of Pedalium murex Linn., with doses of 200 mg/kg and 400 mg/kg, p.o., was evaluated by Lambda-carrageenan induced paw oedema in Wistar albino rats; analgesic activity with doses of 280 mg/kg and 560 mg/kg, p.o., was evaluated by hot plate method and acetic acid induced writhing method in Swiss albino mice; and antipyretic activity with doses of 110 mg/kg and 220 mg/kg, p.o., was evaluated in New Zealand white rabbits by injecting gram -ve lipopolysaccharide obtained from E. coli. Results were analysed by one way ANOVA followed by Dunnet's multiple comparison test. Pedalium murex Linn. showed significant anti-inflammatory activity from 15 min to 180 min as compared to vehicle treated animals. It was comparable to diclofenac sodium at 180 min. The extract did not prolong the reaction time on hot plate method but significantly reduced the number of writhing after acetic acid administration. Also the extract did not show any antipyretic activity on lipopolysaccharide induced pyrexia. It is therefore concluded that the ethanolic extract of Pedalium murex Linn. fruits has an anti-inflammatory and peripheral analgesic effects. PMID:24146508

  19. Effects of preemptive intravenous lornoxicam on the analgesic efficacy of epidural morphine and expression of chemokines in women undergoing hysterectomy

    OpenAIRE

    Tang, Qi-feng; Qian, Yan-ning; Qiu, Yu-hua; Yang, Jian-jun; Wang, Zhong-yun

    2009-01-01

    Background: It is believed that preemptive IV lornoxicam treatment can reduce the consumption of other analgesics, improve analgesic efficacy, and ameliorate immune function during patient-controlled IV analgesia. However, the effects of preemptive IV lornoxicam treatment on the analgesic efficacy of patient-controlled epidural analgesia (PCEA) with morphine and on chemokine expression remain unknown.

  20. Evaluation of analgesic effectiveness of infrared radiation and interference currents in degenerative diseases

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    Kawa Malgorzata

    2014-12-01

    Full Text Available Background: The aim of this research is to evaluate analgesic effectiveness of infrared radiation and interference currents in degenerative diseases of joints. On the grounds of current practical and theoretical experience, the following hypothesis was formed: Application of interference currents and infrared radiation constitutes effective analgesic therapy in degenerative diseases, and in the case of the applied treatment, its effectiveness is long-term.

  1. The Study of Analgesic Effect of Hydroalcoholilc Extract of vitis vinifsraseedon Rat by Formalin TEST

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    Ardeshir Arzi

    2013-01-01

    Full Text Available Background and Objective: Due to the increased role of medicinal plants in therapy, the aim of this research was to study and compare the analgesic effect of hydroalcoholic extract of the seeds of Vitis vinifera with morphine and aspirin as a common analgesic.Subjects and Methods: In this study, the hydroalcoholic extract of Vitis vinifera seed was prepared by maceration method. This study was done on male Wistar rat species. The animals were divided into 7 groups (n= 9: Negative control group received a single dose of (5mg/kg of serum physiology, two positive control groups (one group 2.5mg/kg of morphine and another 300mg/kg of aspirin, 4 treatment groups (100,200,400and 800 mg/kg of hydroalcoholic extract of the seeds of Vitis vinifera via intraperitoneally. In this study the analgesic effect was investigated by using formalin test.Results: The results indicated that the analgesic effect of 400mg/kg of extract on the phase 1 of pain was more than the aspirin and less than the morphine. Its chronic analgesic effect on phase 2 of pain was less than morphine but there weren't any significant differences with those of the aspirin.Conclusion: The results indicated that the hydroalcoholic extract of Vitis vinefera seed contains analgesic effect in both acute and chronic phases of pain. This can probably be due to the influence of the antioxidants of this extract.

  2. [Effect of analgesics on the castration of male piglets].

    Science.gov (United States)

    Zöls, Susanne; Ritzmann, Mathias; Heinritzi, Karl

    2006-01-01

    According to the current German animal welfare law, male piglets may be surgical castrated without anaesthesia up to four weeks of life. This surgical procedure is painful during and also after the operation, for newborn animals as well as for adults. This study was aimed to investigate the impact of preoperative application of analgesics (Meloxicam) on the postoperative castration - pain of four to six days old male piglets. In this investigation all animals were randomly distributed in three groups:the first one was only immobilized but had no surgery, the second one was castrated without analgesics, and the third group was castrated after application of Meloxicam. Blood samples were taken immediately before immobilization, castration or application of the analgesic as well as one, four and 28 hours afterwards to determine Cortisol-concentration in the blood serum and, via this stress-marker, to indirectly evaluate the postoperative und possible intraoperative castration-pain. As a result all piglets castrated without preoperative application of Meloxicam showed significantly increased Cortisol-concentration one and four hours after castration. In contrast, piglets castrated with analgesics resulted in no significant increase during the entire experiment. PMID:16729464

  3. ANALGESIC AND ANTIINFLAMMATORY EFFECTS OF TOTAL EXTRACT, FLAVONOID FRACTION AND VOLATILE OIL OF SALVIA HYDRANGEA

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    V.A HAJ HASHEMI

    2000-12-01

    Full Text Available Background. Gol-e-arvaneh with the scientific name of salvia hydrangea (Labiatea belongs to Salvia genus. In traditional medicine it has been used as analgesic, relieving headache, cold remedy, antipyretic and diuretic. Since until now this plant has not been investigated pharacologically. This study was aimed to find any anti-inflammatory or analgesic activity of the plant. Methods. At first, total extract, flavonoid fraction and volatile oil was prepared. Analgesic effect was assessed using light tail flick and acetic acid writhing test. Male wistar rats (180-220g and mice (25±2g were used in these tests. Carrageen in test was used for assessing anti-inflammatory activity. Results. Total extract and flavonoid fraction could not produce analgesic effect in light tail flick test, while morphine as a standard drug 15 and 30 min. after administration produced 35% and 90% of MPE respectively. In writhing test, total extract and flavonoid fraction had considerable analgesic effect which was comparable to that of indomethacin. Results of Carageenin test showed that both total extract and flavonoid fraction had marked anti-inflammatory activity and volatile oil had only a slight effect. Discussion. Since potent drugs (such as opioids show positive response to light tail flick test, it seems that the plant lacks such compounds. Considerable analgesic activity of total extract and flavonoid fraction in writhing test and also their anti-inflammatory activity indicate that this plant is probably useful for relieving pains, particularly with inflammatory origin.

  4. Anti-Inflammatory and Analgesic Effects of Aqueous Extract of Stem Bark of Ceiba pentandra Gaertn

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    Romaric De Garde Elion Itou

    2014-11-01

    Full Text Available Anti-inflammatory and analgesic effects of the aqueous extract of the stem bark of Ceiba pentandra Gaertn (Bombacaceae were recorded in rat and mice. Inflammation was induced by carrageenan and cotton pellet. The pain was studied using analgesymeter, Koster and hot plate Methods. Aqueous extract (400 and 800 mg/kg of Ceiba pentandra presents a significant anti-inflammatory and analgesic activity. Flavono?ds present in the extract seem to be responsible for the activity.

  5. Heel lance in newborn during breastfeeding: an evaluation of analgesic effect of this procedure

    OpenAIRE

    Tozzini Danila; Rossi Maura; Ziliotto Anna; Trada Michela; Angilella Giuseppina; Alloni Viviana; Perino Antonella; Candriella Manuela; Uga Elena; Tripaldi Clelia; Vaglio Michela; Grossi Luigina; Allen Michaela; Provera Sandro

    2008-01-01

    Abstract Objectives The reduction of pain due to routine invasive procedures (capillary heel stick blood sampling for neonatal metabolic screening) in the newborn is an important objective for the so-called "Hospital with no pain". Practices such as skin to skin contact, or breastfeeding, in healthy newborn, may represent an alternative to the use of analgesic drugs. The aim of our work is to evaluate the analgesic effect of breastfeeding during heel puncture in full term healthy newborn. Met...

  6. Influence of bile acid derivates on morphine analgesic effect in mice

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    Vasovi? Velibor

    2014-01-01

    Full Text Available Background/Aim. It is known that bile acids improve the absorption, bioavailability and pharmacodynamic characteristics of some drugs. Morphine analgesia is produced by activation of opioid receptors within the central nervous system (CNS at both spinal and supraspinal levels. Since a morphine molecule contains 3 polar groups and therefore hard to transfer through the blood-brain barrier, the aim of the study was to examine the potential influence of bile acids derivates, namely sodium salt of monoketocholic acid (MKH-Na and methyl ester of monoketocholic acid (MKH-Me, on analgesic effect of morphine. Methods. White male mice of NMRI-Haan strain, with body weight of 20-24 g, were used in this study. The analgesic effect of morphine (administered by subcutaneous and intramuscular route in a dose of 2 mg/kg, with and without pretreatment with MKH-Na (4 mg/kg and MKH-Me (4 mg/kg was estimated by the hot plate method. Results. Administration of MKH-Me prior to subcutaneous administration of morphine increased the morphine analgesic effect but the increase was not statistically significant. At the same time administration of MKH-Na did not affect morphine analgesic effect. The analgesic effect of morphine increased when administered intramuscularly 20 min after MKH-Me administration. When compared with the group of animals treated only with morphine, a statistically significant increase in analgesic effect was detected 10, 30, 40 and 50 min after morphine administration (p < 0.05. Pretreatment with MKH-Na did not affect morphine analgesic effect. Conclusion. According to the results of this study it can be presumed that after intramuscular morphine administration methyl ester of monoketocholic acid increases morphine transport into the central nervous system and consequently the analgesic effect, as well. Further research on bile acids-morphine interaction both in vitro and in vivo is necessary to completely elucidate the mechanism of this interaction and increase in the morphine analgesic effect. [Projekat Ministarstva nauke Republike Srbije, br. 41012: Interactions of xenobiotics and the impact on biomedical system i br. 172050: Development and application of advanced chromatographic and spectroscopic techniques in analysing xenobiotics and the mechanisms of their decomposition in biotic and abiotic samples

  7. Spinal and supraspinal analgesic effects of Nimodipine : The role of Hypothalamo-Pituitary-Adrenal(HPA axis .

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    mojtaba dolatshahi-somesofla

    2007-12-01

    Full Text Available Nimodipine, an L-type calcium channel blocker, can induce analgesia. However, it is not clear that this analgesic effect is at the level of spinal or supraspinal pain pathway. In addition, it has been reported that the analgesic effect of nifedipine, another L-type calcium channel blocker is related to the HPA axis, but there is no report indicating the role of this axis in the analgesic effect of nimodipine. Methods: Analgesia was measured by tail-flick (TF test involving spinal reflexes and by hot-plate (HP requiring an intact central nervous system. Assays were done before and 15, 30, 60 and 120 min after drug administration in the intact, sham operated and adrenalectomized rats. To identify the interaction between nimodipine and HPA axis, plasma corticosterone level was measured using the radioimmunoassay. Results: Nimodipine significantly decreased the plasma corticosterone level, and showed significant antinociception in both tests. Adrenalectomy potentiated the analgesic effect of nimodipine which was reversed by corticosterone replacement. Furthermore, nimodipine analgesic effect in ADX rats was more potent in HP test (compared to TF test. Nimodipine, at mentioned doses, did not alter animal’s movement indices in activity monitoring test. Conclusion: Nimodipine involves both spinal and supraspinal sites to control thermal pain transmission in presence of adrenal gland. It seems that there is a mutual interaction between nimodipine and HPA axis, especially at supraspinal levels.

  8. Inhibition of antiplatelet effects of aspirin by nonopioid analgesics.

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    Hohlfeld, T; Schrör, K

    2015-02-01

    In patients undergoing coronary bypass grafting, we noticed that low-dose aspirin failed to inhibit platelet aggregation, potentially elevating the risk of thrombotic bypass occlusion. This "high on-treatment platelet reactivity" was reproducible in vitro and could be transferred with patient plasma or urine to aspirin-sensitive donor platelets, suggesting a drug/drug interaction. Loss of aspirin efficacy was associated with analgesia by dipyrone (metamizol) and initiated further study of the interaction between aspirin and other nonopioid analgesics. PMID:25670517

  9. Assessment of ropivacaine postoperative analgesic effect after periapical maxillary incisors surgery

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    Tijani? Miloš

    2012-01-01

    Full Text Available Background/Aim. Ropivacaine is a relatively new longacting local anesthetic. The aim of this study was to compare the postoperative analgesic effect of topical anesthetics ropivacaine 0.75% and lidocaine 2% with adrenaline in the postoperative treatment of periapical lesions in the maxilla. Methods. The study was conducted on 60 subjects, divided into two groups. The study-group received 0.75% ropivacaine without a vasoconstrictor, while the control group was treated with 2% lidocaine with adrenaline (1 : 80.000. Block anesthesia for n. infraorbitalis was used and local anesthetics were applied also on the palatine side for the end branches of n. nasopalatinus. The following parameters were observed: time elapsed from the application of an anesthetic until the first occurrence of pain after the surgery and first intake of an analgesic, the intensity of initial pain, pain intensity 6 h after the application of anesthetics and the total number of analgesics taken within 24 h after the completion of surgery. Results. The pain appeared statistically significantly earlier in the patients who had been given lidocaine with adrenaline (p < 0.001, while statistically significantly higher mean values of initial postoperative pain (p < 0.05 and pain intensity 6 h after the intervention (p < 0.01 were also registered in the same group of patients. In the period of 24 h upon the intervention, the study-group patients were taking less analgesics as compared to the control-group subjects (46.6% vs 73.3%, who were given analgesics earlier, although no statistically significant differences were observed related to the number of analgesic doses taken. Conclusion. The results of our study indicate a better postoperative analgesic effect of ropivacaine as compared to lidocaine with adrenaline.

  10. Effects of Papaver rhoeas Extract on the Tolerance Development to Analgesic Effects of Morphine in Mice

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    Jamal Shams

    2008-01-01

    Full Text Available Previous studies have shown that the extract of Papaver rhoeas reduces morphine dependence, locomotor activity and reward. In present study, the effects of hydro-alcohol extract of Papaver Rhoeas on the tolerance to analgesic effects of morphine in mice have been investigated using tail flick method. Subcutaneous (s.c. administration of morphine (1, 2, 5 and 10 mg/kg induced analgesia. However, intrapretoneal administration of the hydro-alcohol extract of Papaver rhoeas (25, 50 and 100 mg/kg had not an effects on analgesia. Reduction of analgesic in mice pretreated with morphine (50 mg/kg, twice daily; for 3 days, alone, indicated that tolerance has been developed. Hydro-alcohol extract of Papaver rhoeas (25, 50 and 100 mg/kg, i.p. administration, 30 min before each of three daily doses of morphine, attenuated the morphine tolerance dose-independently,indicating that administration of the extract reduces morphine tolerance in mice.

  11. A comparison of analgesic effect of intra-articular levobupivacaine with bupivacaine following knee arthroscopy

    International Nuclear Information System (INIS)

    To compare the postoperative analgesic effects of intra-articular levobupivacaine with bupivacaine following knee arthroscopy. Forty patients, aged between 20-60 years and undergoing elective knee arthroscopy were enrolled into the study protocol that was carried out in Tepecik Education and Research Hospital, Izmir, Turkey between January and June 2007. General anesthesia protocol was the same in all patients. At the end of surgery, the patients were randomly assigned into 2 groups (n=20 in each group). Group L received 20 ml 0.5% levobupivacaine and Group B received 20 ml 0.5% bupivacaine intra-articularly. We evaluated the level of postoperative pain (by visual analoque scale at 1, 2, 4, 6, 12, and 24 hours after surgery), first analgesic requirement time (period measured from the end of the surgery until further analgesia was demanded), and total analgesic consumption during 24 hours. There were no significant difference in the postoperative pain scores of the patients between groups. The first analgesic requirement times were not statistically different. Twelve patients in Group L (60%) and 9 patients in Group B (45%) needed no additional analgesic during the 24 hours (p>0.05). No complications and side effects were found related to the intra-articular treatment. The results of the study show that intra-articular 20 ml 0.5% levobupivacaine provides effective analgesia comparable to that provided by 20 ml 0.5% bupivacaine. (author) (author)

  12. Seasonal Effects on HPLC-DAD-UV and UPLC-ESI-MS Fingerprints and Analgesic Activities of Vernonia Condensata Baker Extracts

    Scientific Electronic Library Online (English)

    Sabrina, Afonso; Aldair C. de, Matos; Vitor A., Marengo; Estefânia G., Moreira; Daniely X., Soares; Héctor Henrique F., Koolen; Ieda S., Scarminio.

    2015-02-01

    Full Text Available Vernonia condensata Baker leaves have different uses in Brazilian folk medicine, including as analgesic and anti-inflammatory agents. The purpose of this study was to evaluate the seasonal effects on their high performance liquid chromatography with a diode array detector (HPLC-DAD-UV) and ultra-per [...] formance liquid chromatography coupled to a mass spectrometer with an electrospray interface (UPLC-ESI-MS) fingerprints, as well as their analgesic activities in mice. There were significant seasonal effects on the relative abundances of the metabolites of the V. condensate leaves as well as on their activities. Analgesic activities in the writhing test were observed with the polar fraction of the leaf extracts collected in autumn, winter and summer (400 mg kg-1); and with the intermediate fraction of leaves collected in autumn (25 and 400 mg kg-1) and in the summer (100 mg kg-1). In conclusion, the results confirm peripherally-mediated anti-inflammatory and analgesic activities for V. condensata leaves and suggest that these are influenced by the harvesting season. N-oxides alkaloids as well as vernonioside play important roles in determining this activity.

  13. Analgesic effects of melatonin : a review of current evidence from experimental and clinical studies

    DEFF Research Database (Denmark)

    Wilhelmsen, Michael; Amirian, Ilda

    2011-01-01

    Melatonin is an endogenous indoleamine, produced mainly by the pineal gland. Melatonin has been proven to have chronobiotic, antioxidant, antihypertensive, anxiolytic and sedative properties. There are also experimental and clinical data supporting an analgesic role of melatonin. In experimental studies, melatonin shows potent analgesic effects in a dose-dependent manner. In clinical studies, melatonin has been shown to have analgesic benefits in patients with chronic pain (fibromyalgia, irritable bowel syndrome, migraine). The physiologic mechanism underlying the analgesic actions of melatonin has not been clarified. The effects may be linked to G(i) -coupled melatonin receptors, to G(i) -coupled opioid µ-receptors or GABA-B receptors with unknown downstream changes with a consequential reduction in anxiety and pain. Also, the repeated administration of melatonin improves sleep and thereby may reduce anxiety, which leads to lower levels of pain. In this paper, we review the current evidence regarding the analgesic properties of melatonin in animals and humans with chronic pain.

  14. Analgesic Effects of Toad Cake and Toad-cake-containing Herbal Drugs

    Science.gov (United States)

    Inoue, Eiji; Shimizu, Yasuharu; Masui, Ryo; Usui, Tomomi; Sudoh, Keiichi

    2014-01-01

    Objectives: This study was conducted to clarify the analgesic effect of toad cake and toad-cake-containing herbal drugs. Methods: We counted the writhing response of mice after the intraperitoneal administration of acetic acid as a nociceptive pain model and the withdrawal response after the plantar surface stimulation of the hind paw induced by partial sciatic nerve ligation of the mice as a neuropathic pain model to investigate the analgesic effect of toad cake and toad-cake-containing herbal drugs. A co-treatment study with serotonin biosynthesis inhibitory drug 4-chloro- DL-phenylalanine methyl ester hydrochloride (PCPA), the catecholamine biosynthesis inhibitory drug ?-methyl- DL-tyrosine methyl ester hydrochloride (AMPT) or the opioid receptor antagonist naloxone hydrochloride was also conducted. Results: Analgesic effects in a mouse model of nociceptive pain and neuropathic pain were shown by oral administration of toad cake and toad-cake-containing herbal drugs. The effects of toad cake and toad-cake-containing herbal drugs disappeared upon co-treatment with PCPA, but not with AMPT or naloxone in the nociceptive pain model; the analgesic effect of toad-cake-containing herbal drugs also disappeared upon co-treatment with PCPA in the neuropathic pain model. Conclusion: Toad cake and toad-cake-containing herbal drugs have potential for the treatments of nociceptive pain and of neuropathic pain, such as post-herpetic neuralgia, trigeminal neuralgia, diabetic neuralgia, and postoperative or posttraumatic pain, by activation of the central serotonin nervous system.

  15. Analgesic Effects of Toad Cake and Toad-cake-containing Herbal Drugs

    Directory of Open Access Journals (Sweden)

    Inoue Eiji

    2014-03-01

    Full Text Available Objectives: This study was conducted to clarify the analgesic effect of toad cake and toad-cake-containing herbal drugs. Methods: We counted the writhing response of mice after the intraperitoneal administration of acetic acid as a nociceptive pain model and the withdrawal response after the plantar surface stimulation of the hind paw induced by partial sciatic nerve ligation of the mice as a neuropathic pain model to investigate the analgesic effect of toad cake and toad-cake-containing herbal drugs. A co-treatment study with serotonin biosynthesis inhibitory drug 4-chloro-DL-phenylalanine methyl ester hydrochloride (PCPA, the catecholamine biosynthesis inhibitory drug ?-methyl-DL-tyrosine methyl ester hydrochloride (AMPT or the opioid receptor antagonist naloxone hydrochloride was also conducted. Results: Analgesic effects in a mouse model of nociceptive pain and neuropathic pain were shown by oral administration of toad cake and toad-cake-containing herbal drugs. The effects of toad cake and toad-cake-containing herbal drugs disappeared upon co-treatment with PCPA, but not with AMPT or naloxone in the nociceptive pain model; the analgesic effect of toad-cake-containing herbal drugs also disappeared upon co-treatment with PCPA in the neuropathic pain model. Conclusion: Toad cake and toad-cake-containing herbal drugs have potential for the treatments of nociceptive pain and of neuropathic pain, such as post-herpetic neuralgia, trigeminal neuralgia, diabetic neuralgia, and postoperative or posttraumatic pain, by activation of the central serotonin nervous system.

  16. Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain

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    ALVES NILZA D.

    1999-01-01

    Full Text Available Since anticonvulsants have been used for treating neuralgias, an interest has arisen to experimentally test vigabatrin for its gabaergic mechanism of action. For this, 41 Wistar rats were used, and in 25 of them a constrictive sciatic neuropathy was induced (Bennet & Xie model. For testing pain symptoms, spontaneous (scratching and evoked behaviors to noxious (46o C and non-noxious (40o C thermal stimuli were quantified. Moreover, a comparative pharmacological study of vigabatrin with other analgesic anticonvulsant drugs was also performed. The results showed a possible dose-dependent analgesic effect of vigabatrin (gamma-vinyl-GABA on experimental neuropathic pain, as shown by the significant (p<0.05 decreasing effect of vigabatrin on scratching and by its significant (p<0.05 increasing effect on the latency of the right hindpaw withdrawal of the animals to noxious thermal stimulus. This was corroborated by similar findings with analgesic anticonvulsants (carbamazepine, phenytoin and valproic acid. This possible and not yet described analgesic effect of vigabatrin seems not to be opioid mediated.

  17. Preemptive Analgesic Effect of Ketamine in Children with Lower Abdominal Surgery

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    Serbülent Gökhan Beyaz

    2011-06-01

    Full Text Available Objective: Preemptive analgesic effect of low dose ketamine has been supported by clinical studies in adults. The aim of this study was to evaluate the analgesic effect of ketamine applied at different times in children who underwent lower abdominal surgery.Material and Methods: A total of 90 children having ASAI-II physical status between 3 and 12 was randomly divided into three groups as pre, int and post groups. Ketamine were given to these groups in the following manner respectively; 1mg/kg intravenous ketamine before incision (pre-incisional; the same dose ketamine 10 minutes following the first incision (intraoperative; and ketamine at the end of the surgical operation (postoperative. The pain of patients was assessed by postoperative pain scale (CHIPPS in children and infants; the sedation status of children was assessed by Ramsey’s sedation scale. The first analgesic requirement time was recorded.Results: No significant difference was found in demographic characteristics of the three groups (p>0.05. Lower CHIPPS scores were found in Group Post throughout all measurement periods (p<0.05. Group Post was found to have significantly higher sedation levels compared with the other two groups (p=0.003. Conclusion: No analgesic effect was obtained using by pre-incisional and intraoperative i.v.1mg/kg ketamine, during lower abdominal surgery in children. Further studies with different drugs are needed to clarify this topic.

  18. Loss of expectation-related mechanisms in Alzheimer's disease makes analgesic therapies less effective

    OpenAIRE

    Benedetti, Fabrizio; Rainero, Innocenzo; Tarenzi, Luisella

    2006-01-01

    Expectation/placebo-related mechanisms and specific effects of therapies show additive effects, such that a therapy is less effective if the placebo component is absent. So far, the placebo component has been disrupted experimentally by using covert administrations of treatments. Here, we show for the first time that disruption of expectation/placebo-related analgesic mechanisms may occur in a clinical condition, Alzheimer's disease (AD). In order to assess the placebo component of a therapy,...

  19. Pharmacokinetic-Pharmacodynamic modeling of the analgesic effect of bupredermTM, in mice

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    Sun-Ok Kim

    2010-08-01

    Full Text Available Purpose: BupredermTM?Buprenorphine transdermal delivery system (BTDS was developed for the treatment of post-operative and chronic pains. This study examined the relationship between the plasma concentration of buprenorphine and its analgesic effect (tail flick test in order to assess the usefulness of pharmacokinetic-pharmacodynamic (PK-PD modeling in describing this relationship. Methods: After patch application, plasma concentrations of bu- prenorphine in mice were measured for 72 hours with a validated LC/MS/MS system, and the analgesic effects were assessed by tail flick test for the period of 24 hours. A modified two- compartment open model was used to explain the PK properties of BTDS, and the PD model was characterized by slow receptor binding. Results: The peak buprenorphine level in plasma was achieved at 1-24 h and the effective therapeutic drug concentration was maintained for 72 hours. BupredermTM induced prolongation of tail-flick latency in a dose and time dependent manner. Maximum analgesic effect was attained at 3-6 h and was maintained for 24 h after patch application. Counter-clockwise hysteresis between the plasma concentration and the analgesic efficacy of BTDS was observed after BupredermTM application, indicating there was a delay between plasma concentrations and the effect observed. From the developed PK-PD model, Kd values (0.69-0.82 nM that were derived from the pharmacodynamic parameters (Kon and Koff are similar to the reported values (Kd = 0.76 ± 0.14 nM. Good agreement between the predicted and observed values was noted for the rate of change in analgesic effect data (R2 = 0.822, 0.852 and 0.774 for 0.24, 0.8 and 2.4 mg/patch, respectively. Conclusions: The established PK- PD model successfully described the relationship between plasma concentration of buprenorphine and its analgesic efficacy measured by the tail flick test. Our model might be useful in estimation and prediction of onset, magnitude and time course of concentration and pharmacological effects of BTDS and will be useful to simulate PK-PD profiles with clinical regimens.

  20. Flexibilide Obtained from Cultured Soft Coral Has Anti-Neuroinflammatory and Analgesic Effects through the Upregulation of Spinal Transforming Growth Factor-?1 in Neuropathic Rats

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    Nan-Fu Chen

    2014-06-01

    Full Text Available Chronic neuroinflammation plays an important role in the development and maintenance of neuropathic pain. The compound flexibilide, which can be obtained from cultured soft coral, possesses anti-inflammatory and analgesic effects in the rat carrageenan peripheral inflammation model. In the present study, we investigated the antinociceptive properties of flexibilide in the rat chronic constriction injury (CCI model of neuropathic pain. First, we found that a single intrathecal (i.t. administration of flexibilide significantly attenuated CCI-induced thermal hyperalgesia at 14 days after surgery. Second, i.t. administration of 10-?g flexibilide twice daily was able to prevent the development of thermal hyperalgesia and weight-bearing deficits in CCI rats. Third, i.t. flexibilide significantly inhibited CCI-induced activation of microglia and astrocytes, as well as the upregulated proinflammatory enzyme, inducible nitric oxide synthase, in the ipsilateral spinal dorsal horn. Furthermore, flexibilide attenuated the CCI-induced downregulation of spinal transforming growth factor-?1 (TGF-?1 at 14 days after surgery. Finally, i.t. SB431542, a selective inhibitor of TGF-? type I receptor, blocked the analgesic effects of flexibilide in CCI rats. Our results suggest that flexibilide may serve as a therapeutic agent for neuropathic pain. In addition, spinal TGF-?1 may be involved in the anti-neuroinflammatory and analgesic effects of flexibilide.

  1. Anti-inflammatory, analgesic and anti-oedematous effects of Lafoensia pacari extract and ellagic acid.

    Science.gov (United States)

    Rogerio, Alexandre P; Fontanari, Caroline; Melo, Mirian C C; Ambrosio, Sérgio R; de Souza, Glória E P; Pereira, Paulo S; França, Suzelei C; da Costa, Fernando B; Albuquerque, Deijanira A; Faccioli, Lúcia H

    2006-09-01

    Lafoensia pacari St. Hil. (Lythraceae) is used in traditional medicine to treat inflammation. Previously, we demonstrated the anti-inflammatory effect that the ethanolic extract of L. pacari has in Toxocara canis infection (a model of systemic eosinophilia). In this study, we tested the anti-inflammatory activity of the same L. pacari extract in mice injected intraperitoneally with beta-glucan present in fraction 1 (F1) of the Histoplasma capsulatum cell wall (a model of acute eosinophilic inflammation). We also determined the anti-oedematous, analgesic and anti-pyretic effects of L. pacari extract in carrageenan-induced paw oedema, acetic acid writhing and LPS-induced fever, respectively. L. pacari extract significantly inhibited leucocyte recruitment into the peritoneal cavity induced by beta-glucan. In addition, the L. pacari extract presented significant analgesic, anti-oedematous and anti-pyretic effects. Bioassay-guided fractionation of the L. pacari extract in the F1 model led us to identify ellagic acid. As did the extract, ellagic acid presented anti-inflammatory, anti-oedematous and analgesic effects. However, ellagic acid had no anti-pyretic effect, suggesting that other compounds present in the plant stem are responsible for this effect. Nevertheless, our results demonstrate potential therapeutic effects of L. pacari extract and ellagic acid, providing new prospects for the development of drugs to treat pain, oedema and inflammation. PMID:16945186

  2. Comparing Early Postoperative Period Analgesic Effect of Dexketoprofene Trometamol and Lornoxicam in Mediastinoscopy Cases

    OpenAIRE

    Gonul Sagiroglu

    2011-01-01

    Objective: In this study, we aimed comparing early postoperative period analgesic effectiveness and the effects on opioid consumption of intravenous dexketoprofen and lornoxicam that are given preemptively. Materials and Methods: Forty patients, planned elective mediastinoscopy, were included in this prospective randomized study. These patients were classified in two groups, group D for dexketoprofene trometamol and group L for lornoxicam, randomly. 20 minutes before the operation 50 mg dexke...

  3. Comparison of the analgesic effects of diflunisal and paracetamol in the treatment of postoperative dental pain.

    Science.gov (United States)

    Selçuk, E; Gomel, M; Bellibas, S E; Köse, T; Tu?lular, I

    1996-01-01

    The search for new effective analgesics without unwanted effects on the coagulation mechanism and a longer duration of activity has been intensified. One such development is diflunisal and the aim of this study was to compare the analgesic effect of diflunisal with that of paracetamol. A combined single dose (500-mg tablets), double-blind, randomized, controlled design in out-patients (n = 104) with moderate or severe pain caused by the surgical removal of impacted mandibular third molars was used in this study. Pain intensity and relief were assessed postoperatively for 8h using category-rating scales. The results showed a statistically significant difference in favour of diflunisal in each and every parameter used in determining the efficacy of the treatment. PMID:9063757

  4. Analgesic Effect of the Methanol Extract of Erica Arborea (L. in Mice Using Formalin Test

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    S Çobanoglu

    2008-09-01

    Full Text Available Background and the purpose of the study: Erica arborea L. (Ericaceae has been used in Turkey folk medicine as a diuretic, urinary antiseptic and laxative. However, its other pharmacological effects have not been yet elucidated clearly. The aim of this study was to investigate analgesic effects of its methanolic (MeOH extract in mice using formalin test, as a model of tonic inflammatory pain. Methods: The MeOH extract of aerial parts and its fractions (20, 40, 60, 80 and 100% MeOH in water were prepared by maceration and solid phase extraction method respectively. Effects of the MeOH extract (10, 20 and 30 mg/kg, i.p. and different fractions (5 mg/kg, i.p. were compared with analgesic effects of the morphine (10 mg/kg, i.p. and indomethacine (5 mg/kg, i.p. as standard analgesic drugs. Results and major conclusion: Results showed that the MeOH extract of E. arborea (10 mg/kg, i.p. similar to the morphine (10 mg/kg, i.p. and indomethacen (5 mg/kg, i.p. decreased formalin-induced paw licking time,. Among the prepared-fractions of the MeOH extract, only fraction of 20% (5 mg/kg, i.p. caused significant decrease in paw licking behavior. Moreover, the MeOH extract (10 mg/kg, i.p. did not produce any motor deficit effects in rotarod test. From the results it may be concluded that the MeOH extract and faction of 20% of E. arborea have a good analgesic effects in formalin test.

  5. [IEM-1460 and spermine potentiate analgesic effect of fentanyl and dipyrone in rats].

    Science.gov (United States)

    2013-12-01

    Intramuscular (i. m.) administration in the minimum effective dose (MED) of central analgesics of fentanyl and dipyrone, polyamine agonist spermine and also IEM-1460 (IEM-1460 is AMPA receptors antagonist and agonist of the NMDA polyamine receptor site) causes the maximal analgesic effect in the tail flick test in rats. The combined i.m. administration of dipyrone with IEM-1460 and spermine in threshold, noneffective alone doses according 1/5 part from their MED leads to decrease of MED dipyrone in the combination with IEM-1460 in 120 times, and MED dipyrone in combination with spermine--in 10 times. The combined i.m. administration of fentanyl with IEM-1460 and spermine in above mentioned threshold doses leads to decrease of MED fentanyl in the combination with IEM-1460 in 150 times, and MED fentanyl in the combination with spermine--in 15 times. PMID:25508397

  6. Analgesic effectiveness of prophylactic therapy and continued therapy with naproxen sodium post simple extraction.

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    Angel Steven Asmat-Abanto

    2015-02-01

    Full Text Available ABSTRACT Objective: To compare the effectiveness of prophylactic therapy and continued therapy with naproxen sodium post simple extraction. Material and methods: Prospective randomized, parallel, single-blind clinical assay, was developed in the Clínica Estomatológica of Universidad Alas Peruanas Filial Trujillo (Peru. Patients who required a simple extraction by dental caries, were randomized into three groups: 30 received naproxen sodium 550 mg preoperatively and then every 12 hours, 30 received naproxen sodium 550 mg postoperatively and then every 12 hours, and 30, ibuprofen (control group 400 mg postoperatively and then every 8 hours, according to the established criteria. The procedure was standardized and the analgesic efficacy assessed by visual analog scale, and the presence of adverse drug reactions. Data were analyzed by IBM SPSS Statistics 22, using ANOVA and Duncan test, considering a significance level of 5%. Result: continued therapy with naproxen sodium showed higher analgesic effectiveness at 1, 8 and 24 hours (p

  7. A comparison of analgesic effect of intra-articular levobupivacaine with bupivacaine following knee arthroscopy.

    OpenAIRE

    Yucel Karaman; Cemil Kayali; Hasan Ozturk; Ahmet Kaya; Canan Bor

    2009-01-01

    OBJECTIVES To compare the postoperative analgesic effects of intra-articular levobupivacaine with bupivacaine following knee arthroscopy. METHODS Forty patients, aged between 20-60 years and undergoing elective knee arthroscopy were enrolled into the study protocol that was carried out in Tepecik Education and Research Hospital, Izmir, Turkey between January and June 2007. General anesthesia protocol was the same in all patients. At the end of surgery, the patients were randomly assi...

  8. Compare the Analgesic Effectiveness of Diclofenac and Paracetamol in Patients with Renal Colic

    OpenAIRE

    Murat Ayan

    2013-01-01

       Aim: This retrospective study was aimed to compare the analgesic effectiveness of paracetamol and diclofenac sodium by using visual analog acale (VAS) in patients applying to emergency room with renal colic. Material and Method: Group I (n=40) patients diagnosed with renal colic and treated with diclofenac sodium (75 mg intramuscular) and Group II (n=40) patients diagnosed with renal colic and treated with paracetamol (1 g intravenous) were included in this study. In both groups,...

  9. Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

    OpenAIRE

    Al-suwayeh, Saleh A.; Taha, Ehab I.; Al-qahtani, Fahad M.; Ahmed, Mahrous O.; Badran, Mohamed M.

    2014-01-01

    The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release usi...

  10. Analgesic effect of topical sodium diclofenac 0.1% drops during retinal laser photocoagulation

    OpenAIRE

    Weinberger, D.; Ron, Y.; Lichter, H.; Rosenblat, I.; Axer-siegel, R.; Yassur, Y.

    2000-01-01

    AIMS—To evaluate the analgesic effect of topical sodium diclofenac 0.1% during retinal laser photocoagulation.?METHODS—87 patients, 45 with proliferative diabetic retinopathy treated with two sessions of panretinal photocoagulation (group A), and 42 patients with non-proliferative diabetic retinopathy who underwent grid treatment of the posterior pole (19 bilaterally) (group B). Sodium diclofenac 0.1% or sodium chloride 0.9% drops were topically applied 30-135 minutes before laser tr...

  11. Analgesic effect of leaf extract from Ageratina glabrata in the hot plate test

    Scientific Electronic Library Online (English)

    Guadalupe, García P; Edgar, García S; Isabel, Martínez G; Thomas R. F., Scior; José L, Salvador; Mauro M, Martínez P; Rosa E. del, Río.

    2011-10-01

    Full Text Available Ageratina glabrata (Kunth) R.M. King & H. Rob., Asteraceae (syn. Eupatorium glabratum Kunth) is widely distributed throughout Mexico and popularly known as "chamizo blanco" and "hierba del golpe" for its traditional use as external analgesic remedy. Though glabrata species has been chemically studie [...] d, there are no experimentally asserted reports about possible analgesic effects which can be inferred from its genus Ageratina. To fill the gap, we evaluated A. glabrata extracts in an animal model of nociception exploiting thermal stimuli. NMR and mass analyses identified a new thymol derivative, 10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate (1), which was computationally converted into a ring-closed structure to explain interaction with the COX-2 enzyme in a ligand-receptor docking study. The resulting docked pose is in line with reported crystal complexes of COX-2 with chromene ligands. Based on the present results of dichloromethane extracts from its dried leaves, it is safe to utter that the plant possesses analgesic effects in animal tests which are mediated through inhibition of COX-2 enzyme.

  12. Heel lance in newborn during breastfeeding: an evaluation of analgesic effect of this procedure

    Directory of Open Access Journals (Sweden)

    Tozzini Danila

    2008-11-01

    Full Text Available Abstract Objectives The reduction of pain due to routine invasive procedures (capillary heel stick blood sampling for neonatal metabolic screening in the newborn is an important objective for the so-called "Hospital with no pain". Practices such as skin to skin contact, or breastfeeding, in healthy newborn, may represent an alternative to the use of analgesic drugs. The aim of our work is to evaluate the analgesic effect of breastfeeding during heel puncture in full term healthy newborn. Methods We studied 200 healthy full term newborns (100 cases and 100 controls, proposing the puncture to mothers during breastfeeding, and explaining to them all the advantages of this practice. Pain assessment was evaluated by DAN scale (Douleur Aigue Nouveau ne scale. Results The difference in score of pain according to the DAN scale was significant in the two groups of patients (p = 0.000; the medium score was 5.15 for controls and 2.65 for cases (newborns sampled during breastfeeding. Conclusion Our results confirmed the evidence of analgesic effect of breastfeeding during heel puncture. This procedure could easily be adopted routinely in maternity wards.

  13. Analgesic and anti-inflammatory effects of aqueous extract of leaves of Pentatropis capensis Linn. f. (Bullock)

    Science.gov (United States)

    Chowdhury, Saikat; Nishteswar, K.; Nariya, Mukesh Kumar

    2014-01-01

    Background: Herbal analgesic and anti-inflammatory remedies are preferred much because of lesser side effects and also a lower tendency for habit formation. Pentatropis capensis is such an analgesic and anti-inflammatory drug which is popular among folklore remedies for various injuries and inflammatory problems. It is called by the name of K?kan?sik? in Ayurvedic works. This study was designed to investigate the analgesic, and anti-inflammatory effects of aqueous extract of P. capensis leaves (AEPC) in rats. Materials and Methods: AEPC was assessed for Analgesic effect through radiant heat tail-flick model and anti-inflammatory effect through carrageenan-induced paw edema model on Wistar strain of albino rats. Results: Pentatropis capensis leaves aqueous extract showed significant (P edema after 3 h of carrageenan induction when compared to the control group. Conclusion: The observed effects were comparable with the standard drug-treated group thus demonstrating effective central analgesic and acute anti-inflammatory potentials of the P. capensis leaves aqueous extract and the observations substantiate its folklore use as an analgesic and anti-inflammatory.

  14. [Analgesic effect of sodium meclofenamate on several painful symptoms].

    Science.gov (United States)

    Castellari, A

    1993-09-01

    Three groups of 20 patients, who suffered of acute pain (dental or low back or menorrhalgia) have been randomized and treated, obtained their informed consent, with meclofenamic acid 100 mg or ketoprofene 50 mg by oral route. The study has been completed double blind to assess the powerful antalgic effect between the two drugs, the results underline that the two NSAID have a very good effect on pain of various nature. The patients have obtained a complete relief not always, but it appears very quickly also by oral route. Statistical analysis has revealed that meclofenamic acid effects are swifter than for ketoprofene, but the latter seems to have a longer action. PMID:8278067

  15. The use and effect of analgesics in patients who regularly drink alcohol.

    Science.gov (United States)

    Dart, R C

    2001-12-01

    Analgesic consumption poses special risks for regular users of alcohol. Among the numerous adverse health effects are acetaminophen toxicity and gastrointestinal (GI) bleeding associated with nonsteroidal anti-inflammatory drug (NSAID) use. An alcohol-acetaminophen hypothesis contends that alcohol enhances acetaminophen toxicity. Because 22% of adults use acetaminophen each week and 5% to 10% of the population is alcoholic, the healthcare implications of serious adverse interactions are considerable. However, such interactions are rare when NSAID doses remain in the therapeutic range. Although clinical studies fail to support anecdotal case reports of liver damage associated with consumption of therapeutic doses of acetaminophen by alcohol users, such reports are probably inaccurate because of the uncritical acceptance of patient history by the clinician and a lack of well-designed prospective trials. Over-the-counter (OTC) NSAIDs, such as aspirin, naproxen, and ketoprofen, are other analgesic options, but each carries the risk of GI bleeding. Unanswered questions about the newer "second-generation" NSAIDs, such as celecoxib and rofecoxib, make them less desirable than acetaminophen and OTC NSAIDs. Because the risk of GI bleeding or ulceration may be higher in alcoholic patients, the optimal strategy in prescribing pain relievers to those who consume alcohol is to use 1 drug at a time and to clearly communicate its generic name. Acetaminophen is the safest OTC analgesic and is recommended as first-line treatment for osteoarthritis. OTC NSAID users should be carefully advised as to recommended dose, and all patients should be reminded to stay within the dosing limits regardless which OTC analgesic is used. PMID:11776482

  16. Effect of some analgesics on paraoxonase-1 purified from human serum.

    Science.gov (United States)

    Ekinci, Deniz; Beydemir, Sükrü

    2009-08-01

    The in vitro effects of the analgesic drugs, lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine, on the activity of purified human serum paraoxonase (hPON1) (EC 3.1.8.1.) were evaluated. hPON1 was purified from human serum with a final specific activity of 3840 U mg(-1) and a purity of 25.3 % using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sepharose 4B-L-tyrozine-1-napthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis indicated a single protein band corresponding to hPON1. The six analgesics dose-dependently decreased in vitro hPON1 activity, with IC(50) values for lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine of 0.136, 0.195, 0.340, 1.639, 6.23 and 9.638 mM, respectively. K(i) constants were 0.009, 0.097, 0.306, 0.805, 13.010 and 11.116 mM, respectively. Analgesics showed different inhibition mechanisms: lornoxicam, diclofenac sodium and lincomycine were uncompetitive, indomethacin and tenoxicam were competitive, ketoprofen was noncompetitive. According to the results, inhibition potency was lornoxicam>indomethacin>tenoxicam> diclofenac sodium>ketoprofen> lincomycine. PMID:19548782

  17. Putative physiological mechanisms underlying tDCS analgesic effects

    OpenAIRE

    Knotkova, Helena; Nitsche, Michael A.; Cruciani, Ricardo A.

    2013-01-01

    Transcranial direct current stimulation (tDCS) is a non-invasive neuromodulation technique that induces changes in excitability, and activation of brain neurons and neuronal circuits. It has been observed that beyond regional effects under the electrodes, tDCS also alters activity of remote interconnected cortical and subcortical areas. This makes the tDCS stimulation technique potentially promising for modulation of pain syndromes. Indeed, utilizing specific montages, tDCS resulted in analge...

  18. Central cardiovascular effects of narcotic analgesics and enkephalins in rats.

    OpenAIRE

    Bellet, M.; Elghozi, J. L.; Meyer, P.; Pernollet, M. G.; Schmitt, H.

    1980-01-01

    1. The cardiovascular effects of morphine, fentanyl, [D-Ala2]-met-enkephalinamide were analyzed after intracisternal injection in anaesthetized rats. PaO2 was measured as an index of respiratory function. 2. At low doses in spontaneously breathing rats, morphine, fentanyl and [D-Ala2]-met-enkephalinamide induced a pressor response with slight tachycardia and no significant change in PaO2. 3. The pressor response appeared to be due to activation of opiate receptors and mediated through the sym...

  19. Gabapentin Increases Analgesic Effect of Chronic Use of Morphine while Decreases Withdrawal Signs

    Directory of Open Access Journals (Sweden)

    Manzumeh-Shamsi Meimandi

    2005-01-01

    Full Text Available This study was performed to evaluate the role of gabapentin co-administration in morphine antinociception and withdrawal effect. Four groups of male rats were examined for latency time using tail flick test; control, morphine (M, gabapentin (GB and gabapentin-morphine (GB-M treated groups. Rats received morphine (10 mg kg < SUP>-1 < /SUP>, s.c. or gabapentin (75 mg kg < SUP>-1 < /SUP>, i.p. or both of them twice a day for 9 days. Control rats received normal saline as schedule time. Latency time was recorded 3 times (5 min of interval before drug injection and in 60, 65 and 70 min after drug injection in days 1, 3, 5, 7 and 9 by tail flick test. Percentage of Maximal Possible Effect (%MPE as antinociceptive effect was calculated for all groups. On 9th day, rats were challenged for withdrawal signs by administration of naloxone (2 mg kg < SUP>-1 < /SUP>, i.p.. Analysis of variance showed no significant difference of %MPE in control and GB groups while in M and GB-M groups the %MPE was changed significantly during the days of study. Gabapentin had no analgesic effect while morphine and gabapentin-morphine had significant analgesic effect compared to control. %MPE of GB-M treated rats was significantly higher than M in days 5, 7 and 9. Also this study showed that pre-treatment with gabapentin reduced most of the opioid withdrawal signs including jumping, weight loss and fore paw tremor. The mechanism(s by which gabapentin enhances the analgesic effect of chronic use of morphine and attenuate opioid withdrawal signs remain to be establish.

  20. Analgesic Effect of the Methanol Extract of Erica Arborea (L.) in Mice Using Formalin Test

    OpenAIRE

    C?obanoglu, S.; Omidbakhsh, R.; Nazemiyeh, H.; Mohajjel Nayebi, A.

    2008-01-01

    Background and the purpose of the study: Erica arborea L. (Ericaceae) has been used in Turkey folk medicine as a diuretic, urinary antiseptic and laxative. However, its other pharmacological effects have not been yet elucidated clearly. The aim of this study was to investigate analgesic effects of its methanolic (MeOH) extract in mice using formalin test, as a model of tonic inflammatory pain. Methods: The MeOH extract of aerial parts and its fractions (20, 40, 60, 80 and 100% MeOH in water) ...

  1. Loss of expectation-related mechanisms in Alzheimer's disease makes analgesic therapies less effective.

    Science.gov (United States)

    Benedetti, Fabrizio; Arduino, Claudia; Costa, Sara; Vighetti, Sergio; Tarenzi, Luisella; Rainero, Innocenzo; Asteggiano, Giovanni

    2006-03-01

    Expectation/placebo-related mechanisms and specific effects of therapies show additive effects, such that a therapy is less effective if the placebo component is absent. So far, the placebo component has been disrupted experimentally by using covert administrations of treatments. Here, we show for the first time that disruption of expectation/placebo-related analgesic mechanisms may occur in a clinical condition, Alzheimer's disease (AD). In order to assess the placebo component of a therapy, we used the recently developed open-hidden paradigm. A local anesthetic was applied, either overtly or covertly, to the skin of AD patients to reduce burning pain after venipuncture. The placebo (psychological) component is represented by the difference between the analgesic effect after open (expected) and after hidden (unexpected) application. We correlated the placebo component with both cognitive status and functional connectivity among different brain regions. We found that AD patients with reduced Frontal Assessment Battery scores showed reduced placebo component of the analgesic treatment. We also found that the disruption of the placebo component occurred when reduced connectivity of the prefrontal lobes with the rest of the brain was present. Remarkably, the loss of these placebo-related mechanisms reduced treatment efficacy, such that a dose increase was necessary to produce adequate analgesia. These findings highlight the active role of cognition and prefrontal lobes in the therapeutic outcome and underscore the need of considering a possible revision of the therapeutic approach in Alzheimer patients in order to compensate for the loss of the endogenous expectation and placebo mechanisms. PMID:16473462

  2. Electroencephalography and analgesics.

    Science.gov (United States)

    Malver, Lasse Paludan; Brokjaer, Anne; Staahl, Camilla; Graversen, Carina; Andresen, Trine; Drewes, Asbjørn Mohr

    2014-01-01

    To assess centrally mediated analgesic mechanisms in clinical trials with pain patients, objective standardized methods such as electroencephalography (EEG) has many advantages. The aim of this review is to provide the reader with an overview of present findings in analgesics assessed with spontaneous EEG and evoked brain potentials (EPs) in humans. Furthermore, EEG methodologies will be discussed with respect to translation from animals to humans and future perspectives in predicting analgesic efficacy. We searched PubMed with MeSH terms 'analgesics', 'electroencephalography' and 'evoked potentials' for relevant articles. Combined with a search in their reference lists 15 articles on spontaneous EEG and 55 papers on EPs were identified. Overall, opioids produced increased activity in the delta band in the spontaneous EEG, but increases in higher frequency bands were also seen. The EP amplitudes decreased in the majority of studies. Anticonvulsants used as analgesics showed inconsistent results. The N-methyl-D-aspartate receptor antagonist ketamine showed an increase in the theta band in spontaneous EEG and decreases in EP amplitudes. Tricyclic antidepressants increased the activity in the delta, theta and beta bands in the spontaneous EEG while EPs were inconsistently affected. Weak analgesics were mainly investigated with EPs and a decrease in amplitudes was generally observed. This review reveals that both spontaneous EEG and EPs are widely used as biomarkers for analgesic drug effects. Methodological differences are common and a more uniform approach will further enhance the value of such biomarkers for drug development and prediction of treatment response in individual patients. PMID:23593934

  3. Intracerebroventricular administration of 26RFa produces an analgesic effect in the rat formalin test.

    Science.gov (United States)

    Yamamoto, Tatsuo; Miyazaki, Rika; Yamada, Toshihiko

    2009-09-01

    GPR103 is one of the orphan G protein-coupled receptors. Recently, an endogenous ligand for GPR103, 26RFa, was identified. Many 26RFa binding sites have been observed in various nuclei of the brain involved in the processing of pain such as the parafascicular thalamic nucleus, the locus coeruleus, the dorsal raphe nucleus, and the parabrachial nucleus. In the present study, the effects of intracerebroventricular injection of 26RFa were tested in the rat. Intracerebroventricular injection of 26RFa significantly decreased the number of both phase 1 and phase 2 agitation behaviors induced by paw formalin injection. This analgesic effect of 26RFa on the phase 1 response, but not phase 2 response, was antagonized by BIBP3226, a mixed antagonist of neuropeptide Y Y1 and neuropeptide FF receptors. Intracerebroventricular injection of 26RFa has no effect in the 52.5 degrees C hot plate test. Intracerebroventricular injection of 26RFa had no effect on the expression of Fos-like immunoreactivity induced by paw formalin injection in the superficial layers of the spinal dorsal horn. These data suggest that (1) 26RFa modulates nociceptive transmission at the supraspinal site during a formalin test, (2) the mechanism 26RFa uses to produce an analgesic effect on the phase 1 response is different from that on the phase 2 response, and (3) intracerebroventricularly injected 26RFa dose not directly inhibit the nociceptive input to the spinal cord. PMID:19520126

  4. Analgesic and systemic effects of xylazine, lidocaine and their combination after subarachnoid administration in goats

    OpenAIRE

    Derossi, R.; Beretta, M. P.; Junqueira, A. L.

    2012-01-01

    The objective of the study was to determine the analgesic and systemic effects of subarachnoid administration of xylazine hydrochloride (XY), lidocaine hydrochloride (LI) and their combination (XYLI) in goats. Six healthy goats were used in a prospective randomised study. Three treatments were administered to each goat, with 1-week intervals between each treatment. Treatments consisted of 0.1 mg/kg xylazine, 2.5 mg/kg lidocaine and a combination of xylazine 0.05 (mg/kg) and lidocaine (1.25 mg...

  5. The effect of acupuncture duration on analgesia and peripheral sensory thresholds

    Directory of Open Access Journals (Sweden)

    Schulteis Gery

    2008-05-01

    Full Text Available Abstract Background Acupuncture provides a means of peripheral stimulation for pain relief. However, the detailed neuronal mechanisms by which acupuncture relieves pain are still poorly understood and information regarding optimal treatment settings is still inadequate. Previous studies with a short burst of unilateral electroacupuncture (EA in the Tendinomuscular Meridians (TMM treatment model for pain demonstrated a transient dermatomally correlated bilateral analgesic effect with corresponding peripheral modality-specific sensory threshold alterations. However, the impact of EA duration on the analgesic effect in this particular treatment model is unknown. To obtain mechanistically and clinically important information regarding EA analgesia, this current prospective cross-over study assesses the effects of EA duration on analgesia and thermal sensory thresholds in the TMM treatment model. Methods Baseline peripheral sensory thresholds were measured at pre-marked testing sites along the medial aspects (liver and spleen meridians of bilateral lower extremities. A 5-second hot pain stimulation was delivered to the testing sites and the corresponding pain Visual Analog Scale (VAS scores were recorded. Three different EA (5Hz stimulation durations (5, 15 and 30 minutes were randomly tested at least one week apart. At the last 10 seconds of each EA session, 5 seconds of subject specific HP stimulation was delivered to the testing sites. The corresponding pain and EA VAS scores of de qi sensation (tingling during and after the EA were recorded. The measurements were repeated immediately, 30 and 60 minutes after the EA stimulation. A four-factor repeat measures ANOVA was used to assess the effect of stimulation duration, time, location (thigh vs. calf and side (ipsilateral vs. contralateral of EA on sensory thresholds and HP VAS scores. Results A significant (P Conclusion Longer durations of EA stimulation provide a more sustainable analgesic benefit to hot noxious stimulation than a shorter duration of stimulation. The increase of cold threshold with sustained warm threshold temperature elevation as observed in the longer durations of EA suggests that as the duration of EA lengthened, there is a gradual shifting from an initial predominantly spinally mediated analgesic effect to a supraspinally mediated modulatory mechanism of thermal pain. The 15-minute stimulation appeared to be the optimal setting for treating acute pain in the lower extremities.

  6. Synergism between analgesics.

    DEFF Research Database (Denmark)

    Kehlet, H

    1995-01-01

    The concept and value of 'multimodal' or 'balanced' analgesia in the treatment of postoperative pain is reviewed. Based upon the relatively few multimodal studies compared to unimodal studies, it is concluded that a combination of analgesics will improve pain relief including movement-associated pain. Since analgesic combination therapy is rational, further studies are needed to evaluate the optimal combination for each surgical procedure, as well as to assess the risk of side effects and need for surveillance in large-scale studies.

  7. Role of serotonin in pathogenesis of analgesic induced headache

    Energy Technology Data Exchange (ETDEWEB)

    Srikiatkhachorn, A.

    1999-12-16

    Analgesic abuse has recently been recognized as a cause of deterioration in primary headache patients. Although the pathogenesis of this headache transformation is still obscure, and alteration of central pain control system is one possible mechanism. A number of recent studies indicated that simple analgesics exert their effect by modulating the endogenous pain control system rather than the effect at the peripheral tissue, as previously suggested. Serotonin (5-hydroxytryptamine ; 5-HT) has long been known to play a pivotal role in the pain modulatory system in the brainstem. In the present study, we investigated the changes in 5-HT system in platelets and brain tissue. A significant decrease in platelet 5-HT concentration (221.8{+-}30.7, 445.3{+-}37.4 and 467.2{+-}38.5 ng/10{sup 9} platelets, for patients with analgesic-induced headache and migraine patients, respectively, p<0.02) were evident in patients with analgesic induced headache. Chronic paracetamol administration induced a decrease in 5-HT{sub 2} serotonin receptor in cortical and brain stem tissue in experimental animals (B{sub max}=0.93{+-}0.04 and 1.79{+-}0.61 pmol/mg protein for paracetamol treated rat and controls, respectively, p<0.05). Our preliminary results suggested that chronic administration of analgesics interferes with central and peripheral 5-HT system and therefore possibly alters the 5-HT dependent antinociceptive system. (author)

  8. Anti-inflammatory and analgesic effects of ketoprofen in palm oil esters nanoemulsion.

    Science.gov (United States)

    Sakeena, M H F; Yam, M F; Elrashid, S M; Munavvar, A S; Azmin, M N

    2010-01-01

    Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen. PMID:21099145

  9. Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

    Science.gov (United States)

    Al-Suwayeh, Saleh A.; Taha, Ehab I.; Al-Qahtani, Fahad M.; Ahmed, Mahrous O.; Badran, Mohamed M.

    2014-01-01

    The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also, in vitro skin permeation of LOR was conducted. The effect of hydroxypropyl ?-cyclodextrin (HP ?-CD), beta-cyclodextrin (?-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31??g/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HP ?-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HP ?-CD and may be promising in enhancing permeation. PMID:25045724

  10. Evaluation of skin permeation and analgesic activity effects of carbopol lornoxicam topical gels containing penetration enhancer.

    Science.gov (United States)

    Al-Suwayeh, Saleh A; Taha, Ehab I; Al-Qahtani, Fahad M; Ahmed, Mahrous O; Badran, Mohamed M

    2014-01-01

    The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also, in vitro skin permeation of LOR was conducted. The effect of hydroxypropyl ?-cyclodextrin (HP ?-CD), beta-cyclodextrin (?-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 ?g/cm(2)/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HP ?-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HP ?-CD and may be promising in enhancing permeation. PMID:25045724

  11. Anticonvulsant, Analgesic and Hypothermic Effects of Aridanin Isolated from Tetrapleura tetrapetra Fruit in Mice

    Directory of Open Access Journals (Sweden)

    A.O. Aderibigbe

    2007-01-01

    Full Text Available Aridanin (an N-acetylglycoside of oleanolic acid isolated from Tetrapleura tetraptera fruit was investigated for anticonvulsant, analgesic and hypothermic activities in mice. Aridanin at doses of 15 and 30 mg kg-1 by intraperitoneal administration was shown to protect animals in pentylenetetrazole (PTZ-induced seizure but not in strychnine and picrotoxin induced convulsions. The same dose of aridanin equally decreased rectal temperature and acetic acid-induced writhes in mice. The hypothermic action of aridanin was reversed by pretreatment with cyproheptadine (0.1 mg kg-1, atropine (2 mg kg-1, naltrexone (0.25 mg kg-1, but not with haloperidol (0.1 mg kg-1. The effect on acetic acid-induced writhes was completely blocked by naltrexone, but not by atropine, cyproheptadine and haloperidol. The results suggest that aridanin could be acting as a Central Nervous System (CNS depressant and that its anticonvulsant property is mediated through the membrane stabilizing property and not through GABA and glycine neurotransmitters respectively. Analgesic and hypothermic actions were mediated through opioids and cholinergic, 5-HT receptors, respectively.

  12. The anti-inflammatory and analgesic effects of a crude extract of Petiveria alliacea L. (Phytolaccaceae).

    Science.gov (United States)

    Lopes-Martins, R A B; Pegoraro, D H; Woisky, R; Penna, S C; Sertié, J A A

    2002-04-01

    Petiveria alliacea L (Phytolaccaceae) is a perennial bush plant that grows widely in Brazil. The roots and leaves of P. alliacea have been used in folk medicine for their antispasmodic, sedative, diuretic and antihelminthic actions. We recently described the anti-inflammatory properties of P. alliacea administered topically and orally in different animal models. In the present study, we investigated the anti-inflammatory activity of a crude lyophilized extract of P. alliacea roots administered to rats with pleurisy. The oral administration of P. alliacea root extract did not significantly reduce the total number of leukocytes at the doses tested. By contrast, the highest dose of extract tested (43.9 mg/kg body wt.) significantly reduced the number of migrating neutrophils, mononuclear cells and eosinophils; the dose of 31.4 mg/kg body wt. also reduced mononuclear cell migration. The P. alliacea root extract also showed a significant analgesic effect in the experimental model used. The results of this study provide a basis for the use of P. alliacea extracts in popular folk medicine, but further studies are necessary to elucidate the mechanism of its anti-inflammatory and analgesic actions. PMID:12046866

  13. The analgesic effect of dexketoprofen when added to lidocaine for intravenous regional anaesthesia: a prospective, randomized, placebo-controlled study.

    Science.gov (United States)

    Yurtlu, S; Hanci, V; Kargi, E; Erdo?an, G; Köksal, B G; Gül, ?; Okyay, R D; Ayo?lu, H; Turan, I Ö

    2011-01-01

    This prospective, randomized, placebo-controlled study evaluated the effects of dexketoprofen as an adjunct to lidocaine in intravenous regional anaesthesia (IVRA) or as a supplemental intravenous (i.v.) analgesic. Patients scheduled for elective hand or forearm soft-tissue surgery were randomly divided into three groups. All 45 patients received 0.5% lidocaine as IVRA. Dexketoprofen was given either i.v. or added into the IVRA solution and the control group received an equal volume of saline both i.v. and as part of the IVRA. The times of sensory and motor block onset, recovery time and postoperative analgesic consumption were recorded. Compared with controls, the addition of dexketoprofen to the IVRA solution resulted in more rapid onset of sensory and motor block, longer recovery time, decreased intra- and postoperative pain scores and decreased paracetamol use. It is concluded that coadministration of dexketoprofen with lidocaine in IVRA improves anaesthetic block and decreases postoperative analgesic requirements. PMID:22117995

  14. Evaluation of Anti-Inflammatory, Analgesic, and Antipyretic Effects of Ethanolic Extract of Pedalium Murex Linn. Fruits

    OpenAIRE

    Patel, Mahendra K.; Mandavia, Divyesh R.; Patel, Tejas K.; Barvaliya, Manish J.; Tripathi, C. B.

    2013-01-01

    This study investigated the possible anti-inflammatory, analgesic, and antipyretic effects of ethanolic extract of Pedalium murex Linn. fruits in selected experimental animal models. Anti-inflammatory activity of Pedalium murex Linn., with doses of 200 mg/kg and 400 mg/kg, p.o., was evaluated by Lambda-carrageenan induced paw oedema in Wistar albino rats; analgesic activity with doses of 280 mg/kg and 560 mg/kg, p.o., was evaluated by hot plate method and acetic acid induced writhing method i...

  15. Noninterventional study of transdermal fentanyl (fentavera) matrix patches in chronic pain patients: analgesic and quality of life effects.

    Science.gov (United States)

    Heim, Manuel

    2015-01-01

    Fentanyl is considered to be an effective, transdermal treatment of chronic, cancer, and noncancer pain. This noninterventional, clinical practice-based study, on 426 patients attending 42 practices, assessed a proprietary, Aloe vera-containing, transdermal fentanyl matrix patch (Fentavera), for its analgesic effects, patients' quality of life (QoL) effects, tolerability, and adhesiveness. Study outcomes were mean changes from baseline of patient (11-point scales) and physician (5-point scales) ratings. After 1 and 2 months treatment, there were significant (P walking, general activity, sleep quality, and QoL. For each parameter, the patient response rate was >30% at 2 months (response = 2-point decrease on 11-point rating scale). In a large majority of patients, the physicians rated the matrix patch as good or very good for analgesic effect, systemic and local tolerance, and adhesiveness. There were 30 adverse events in 4.2% of patients and analgesic comedications were reduced during treatment compared to before treatment. It is concluded, from this population-based data, that the proprietary, transdermal fentanyl matrix patch is effective and safe for chronic pain management in clinical practice, with significant positive analgesic and QoL effects, while being well tolerated and exhibiting good or very good adhesiveness. PMID:25861472

  16. Peripheral muscarinic receptors mediate the anti-inflammatory effects of auricular acupuncture

    Directory of Open Access Journals (Sweden)

    Chung Wai

    2011-01-01

    Full Text Available Abstract Background The cholinergic and opioid systems play important roles in modulating inflammation. This study tests whether auricular acupuncture (AA produces anti-inflammatory effects via opioid and peripheral cholinergic receptors in a rat model. Methods Rats were anesthetized with chloral hydrate and inflammation was induced by intraplantar injection of carrageenan. Electroacupuncture was performed at auricular points bilaterally. The severity of inflammation was assessed using changes in paw volume and thermal and mechanical pain thresholds of the rats during recovery from anesthesia. Results Electroacupuncture at selected auricular acupoints significantly reduced paw edema and mechanical hyperalgesia, with no significant effect on thermal hyperalgesia. The anti-edematous and analgesic effects of AA were abolished by blockade of peripheral cholinergic muscarinic receptors with methyl atropine. Blockade of local muscarinic receptors at the inflamed site with a small dose of atropine also antagonized the anti-edematous effect of AA. By contrast, systemic opioid receptor blockade with naloxone did not antagonize the anti-inflammatory effects of AA. Conclusion This study discovers a role of peripheral muscarinic receptors in mediating the anti-inflammatory effects of AA. The cholinergic muscarinic mechanism appears to be more important than the opioid mechanism in the anti-inflammatory action of AA.

  17. [Co-analgesics--today and tomorrow--a receptor-based overview of therapeutical options].

    Science.gov (United States)

    Wörner, Jakobea; Rukwied, Roman; Konrad, Christoph

    2009-11-01

    The sensation of pain arises through stimulation of peripheral nociceptors and is transmitted centrally involving several receptors and ion channels. In addition many endogenous physiologic pain-modulating mechanisms exist. Besides of classical analgesics, numerous other drugs showed analgesic properties based on diverse modes of actions along the pain pathway. These co-analgesics, administered in combination with classical drugs, are able to reduce painful states of different origin. We describe the peripheral action sites of co-analgesics, such as cannabinoids, capsaicin, bisphosphonates, steroids and somatostatin. We also summarise the effect of peripherally and centrally acting ion-channel blockers, e.g. local anaesthetics, carbamazepine and tolperisone working on sodium channels and gabapentin and pregabalin working on calcium channels. Finally, central analgesic mechanisms are discussed, for instance the inhibition of NMDA-receptors by ketamine or magnesium, the stimulation of alpha2-receptors by clonidine, tizanidine or antidepressants, the activation of GABA-receptors through baclofen and other analgesic mechanisms of i.e. ondansetron and neostigmine. PMID:19918705

  18. The unsolved case of “bone-impairing analgesics”: the endocrine effects of opioids on bone metabolism

    Directory of Open Access Journals (Sweden)

    Coluzzi F

    2015-03-01

    Full Text Available Flaminia Coluzzi,1,2 Joseph Pergolizzi,3,4 Robert B Raffa,5 Consalvo Mattia1,2 1Department of Medical and Surgical Sciences and Biotechnologies, Unit of Anesthesiology, Intensive Care Medicine and Pain Therapy, Faculty of Pharmacy and Medicine – Polo Pontino, Sapienza University of Rome, Latina, Italy; 2SIAARTI Study Group on Acute and Chronic Pain, Rome, Italy; 3Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, 4Naples Anesthesia and Pain Associates, Naples, FL, 5Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, PA, USA Abstract: The current literature describes the possible risks for bone fracture in chronic analgesics users. There are three main hypotheses that could explain the increased risk of fracture associated with central analgesics, such as opioids: 1 the increased risk of falls caused by central nervous system effects, including sedation and dizziness; 2 reduced bone mass density caused by the direct opioid effect on osteoblasts; and 3 chronic opioid-induced hypogonadism. The impact of opioids varies by sex and among the type of opioid used (less, for example, for tapentadol and buprenorphine. Opioid-associated androgen deficiency is correlated with an increased risk of osteoporosis; thus, despite that standards have not been established for monitoring and treating opioid-induced hypogonadism or hypoadrenalism, all patients chronically taking opioids (particularly at doses ?100 mg morphine daily should be monitored for the early detection of hormonal impairment and low bone mass density. Keywords: opioids side effects, bone metabolism, fractures, OPIAD, endocrine system, chronic pain

  19. Does transcutaneous electrical nerve stimulation (TENS have a clinically relevant analgesic effect on different pain conditions? A literature review

    Directory of Open Access Journals (Sweden)

    Asami Naka

    2013-07-01

    Full Text Available Transcutaneous electric nerve stimulation (TENS is a standard therapy used in different painful conditions such as low back pain, diabetic polyneuropathy or arthrosis. However, literature reviews focusing on the effects and the clinical implication of this method in various painful conditions are yet scarce. The purpose of this literature research was to determine, whether TENS provides an analgesic effect on common painful conditions in clinical practice. Literature research was performed using three data bases (Pubmed, Embase, Cochrane Database, focusing on papers published in the space of time from 2007 to 2012. Papers were evaluated from two reviewers independently concerning the clinical outcome, taking account for the level of external evidence according to the German Cochrane levels of evidence (Ia – IV. 133 papers of varying methodological quality dealing with different painful conditions were selected in total. A clinically relevant analgesic effect was described in 90 painful conditions (67%. In 30 painful states (22%, the outcome was inconclusive due to the study design. No significant analgesic effect of TENS was observed in 15 painful conditions (11%. The vast majority of the papers were classified as Cochrane evidence level Ib (n = 64; 48%, followed by level Ia (n = 23; 17%, level III (n = 18; 14%, level IV (n = 15; 11%, level IIb (n = 10; 8% and level IIa (n = 3; 2%. Most of the studies revealed an analgesic effect in various painful conditions, confirming the usefulness of TENS in clinical practice.

  20. [Comparison of the analgesic effect of nicomorphine in two different solutions (author's transl)].

    Science.gov (United States)

    Vadon, P; Rehak, P

    1979-04-30

    The analgesic effect of nicomorphine in two different solutions was tested in 120 patients after cholecystectomy. The patients were divided into three groups: group I was given nicomorphine diluted with water, group II nicomorphine diluted with propylenglykol, group III propylenglykol alone. The degree of pain sensation was determined by interrogation. Pulse, respiratory rate, blood pressure as well as capillary pO2 and pCO2 were measured 10 and 30 minutes after medication. No difference in pain relief could be established in the two groups receiving nicomorphine. Respiratory depression with a significant decrease of respiratory rate together with an increase of pCO2 was observed in the two nicomorphine groups. In the placebo group there was no significant change in the tested parameters. A small decrease of pO2 was observed in all patients after laparotomy. PMID:452619

  1. Analgesic Effect of Meloxicam in Canine Acute Dermatitis – a Pilot Study

    Directory of Open Access Journals (Sweden)

    Frendin J

    2002-12-01

    Full Text Available A double-blind trial was performed on 12 client-owned dogs suffering from acute and painful dermatitis. Clinically these cases represented pyotraumatic dermatitis and pyotraumatic folliculitis. Six dogs were injected with meloxicam and 6 were given placebo. Signs of pain were recorded on a visual analogue scale before administering the drug. This was repeated over the following 2–3 days. All dogs were treated with cephalexin orally. Six dogs given meloxicam and cephalexin showed an average decrease of pain on day 2 of 28.3%, whereas the 6 dogs given placebo and cephalexin showed an average decrease of pain on day 2 of 8.3%. When compared in the Wilcoxon two-sample test, using change in percent and absolute change, the 2 groups yielded p = 0.026 and p = 0.064 respectively. These findings indicate that meloxicam has an analgesic effect on acute dermatitis in dogs.

  2. Comparative analysis of preemptive analgesic effect of dexamethasone and diclofenac following third molar surgery

    Scientific Electronic Library Online (English)

    José Leonardo, Simone; Waldyr Antonio, Jorge; Anna Carolina Ratto Tempestini, Horliana; Talita Girio, Canaval; Isabel Peixoto, Tortamano.

    2013-06-01

    Full Text Available SciELO Brazil | Language: English Abstract in english The objective of the study was to compare the analgesic effectiveness of dexamethasone and diclofenac sodium administered preemptively after surgical removal of third molars. Forty-four ASA (American Society of Anesthesiologists) I patients (19 men, 35 women; 16–28 years old) randomly and double-bli [...] ndly received diclofenac sodium (50?mg) or dexamethasone (8?mg) or placebo 1?h before surgery. Intensity of pain, measured with a visual analog scale (VAS), was the variable studied at different postoperative times (1?h, 2?h, 3?h, 6?h, 8?h, 12?h, 48?h, 4?d and 7?d). The total amount of rescue medication (TARM) ingested (paracetamol) was another variable of the study. The Kruskal-Wallis statistical test was used. A p value of

  3. PK20, a new opioid-neurotensin hybrid peptide that exhibits central and peripheral antinociceptive effects

    Directory of Open Access Journals (Sweden)

    Tsuda Yuko

    2010-12-01

    Full Text Available Abstract Background The clinical treatment of various types of pain relies upon the use of opioid analgesics. However most of them produce, in addition to the analgesic effect, several side effects such as the development of dependence and addiction as well as sedation, dysphoria, and constipation. One solution to these problems are chimeric compounds in which the opioid pharmacophore is hybridized with another type of compound to incease antinociceptive effects. Neurotensin-induced antinociception is not mediated through the opioid system. Therefore, hybridizing neurotensin with opioid elements may result in a potent synergistic antinociceptor. Results Using the known structure-activity relationships of neurotensin we have synthesized a new chimeric opioid-neurotensin compound PK20 which is characterized by a very strong antinociceptive potency. The observation that the opioid antagonist naltrexone did not completely reverse the antinociceptive effect, indicates the partial involvement of the nonopioid component in PK20 in the produced analgesia. Conclusions The opioid-neurotensin hybrid analogue PK20, in which opioid and neurotensin pharmacophores overlap partially, expresses high antinociceptive tail-flick effects after central as well as peripheral applications.

  4. The analgesic effect of pregabalin in chronic pain patients is reflected by changes in pharmaco-EEG spectral indices

    DEFF Research Database (Denmark)

    Gravesen, Carina; Olesen, SØren S

    2012-01-01

    What this paper adds What is already known about this subject • Pregabalin is an anticonvulsive agent prescribed as a secondary analgesic for patients when standard pain treatment is insufficient. • The analgesic effect resides to the central nervous system. • The central analgesic effect can be evaluated by electroencephalographic. What this study adds • The analgesic effect of pregabalin is reflected as a slowing of brain oscillations. • The slowing of brain oscillations for each individual patient is correlated to subjective pain scores. • The developed methodology may be used as a mechanistic approach to monitor the analgesic effect of pregabalin in pharmacological studies. SUMMARY: Aim: To identify electroencephalographic (EEG) biomarkers for the analgesic effect of pregabalin in patients with chronic visceral pain. Methods: This was a double-blind, placebo-controlled study in thirty-one patients suffering from visceral pain due to chronic pancreatitis. Patients received increasing doses of pregabalin (75mg-300mg twice a day) or matching placebo during 3 weeks of treatment. Pain scores were documented in a diary based on the visual analogue scale. In addition, brief pain inventory-short form (BPI) and quality of life questionnaires were collected prior to and after the study period. Multi-channel resting EEG was recorded before treatment onset and at the end of the study. Changes in EEG spectral indices were extracted, and individual changes were classified by a support vector machine (SVM) to discriminate the pregabalin and placebo responses. Changes in individual spectral indices and pain scores were correlated. Results: Pregabalin increased normalized intensity in low spectral indices, most prominent in the theta band (3.5-7.5Hz), difference of -3.18, 95%CI -3.57, -2.80; P = 0.03. No changes in spectral indices were seen for placebo. The maximum difference between pregabalin and placebo treated patients were seen in the parietal region, with a classification accuracy of 85.7% (P = 0.009). Individual changes in EEG indices were correlated to changes in pain diary (P = 0.04) and BPI pain composite scores (P = 0.02). Conclusions: Changes in spectral indices caused by slowing of brain oscillations were identified as a biomarker for the central analgesic effect of pregabalin. The developed methodology may provide perspectives to assess individual responses to treatment in personalized medicine.

  5. Anti-inflammatory, analgesic, and immunostimulatory effects of Luehea divaricata Mart. & Zucc. (Malvaceae) bark

    Scientific Electronic Library Online (English)

    Roseane Leandra da, Rosa; Geisson Marcos, Nardi; Adriana Graziele de Farias, Januário; Renata, Boçois; Katiane Paula, Bagatini; Sandro José Ribeiro, Bonatto; Andrea de Oliveira, Pinto; João Ronaldo Notargiacomo, Ferreira; Luisa Nathália Bolda, Mariano; Rivaldo, Niero; Fabíola, Iagher.

    2014-09-01

    Full Text Available Luehea divaricata (Malvaceae) é utilizada para o tratamento de várias condições patológicas, entretanto, há poucos relatos sobre sua bioatividade. O objetivo deste estudo foi avaliar o efeito anti-inflamatório e analgésico, bem como a atividade de macrófagos em camundongos tratados com extrato brut [...] o hidroalcoólico (CLD) da planta. Cromatografia em camada delgada revelou a presença de epicatequina, estigmasterol, lupeol e ?,?-amirina no material. Para avaliar a atividade anti-inflamatória e analgésica, animais foram submetidos a teste de edema de pata induzido por carragenana, teste de contorções, da formalina e da capsaicina. A atividade imunomodulatória foi avaliada pela capacidade de adesão e de fagocitose dos macrófagos, volume lisossômico e produção de espécies reativas de oxigênio (ROS), após tratamento diário com CLD por 15 dias. CLD promoveu redução do edema de pata (36,8% e 50,2%; 100 e 300 mg/kg, respectivamente; p Abstract in english Luehea divaricata (Malvaceae) is a plant widely used for treatment of various inflammatory and infectious conditions; however few reports discuss its biological properties. The aim of this study was to evaluate the anti-inflammatory and analgesic effects as well as the macrophage activity in mice t [...] reated with the hydroalcoholic crude extract of L. divaricata (CLD). Thin layer chromatography revealed presence of epicathequin, stigmasterol, lupeol and ?,?-amyrin in the extract. To evaluate the anti-inflammatory and analgesic activities, animals were subjected to paw edema induced by carrageenan test, writhing, formalin and capsaicin tests. Immunomodulatory activity was evaluated by adhesion and phagocytic capacity, lysosomal volume, and reactive oxygen species (ROS) production by peritoneal macrophages, after daily treatment with CLD for 15 days. CLD promoted reduction in paw edema (36.8% and 50.2%; p

  6. Cholecystokinin receptors mediate tolerance to the analgesic effect of TENS in arthritic rats ?

    OpenAIRE

    Desantana, Josimari M.; Da Silva, Luis Felipe S.; Sluka, Kathleen A.

    2009-01-01

    Transcutaneous electrical nerve stimulation (TENS) is a treatment for pain that involves placement of electrical stimulation through the skin for pain relief. Previous work from our laboratory shows that repeated application of TENS produces analgesic tolerance by the fourth day and a concomitant cross-tolerance at spinal opioid receptors. Prior pharmacological studies show that blockade of cholecystokinin (CCK) receptors systemically and spinally prevents the development of analgesic toleran...

  7. Paroxetine Augments while Naloxone Abolishes the Analgesic Effect of Paracetamol in Acute Nociceptive Pain in Mice

    Directory of Open Access Journals (Sweden)

    Mohammad Raafat Abdalla

    2013-07-01

    Full Text Available The mechanism(s of analgesic action of paracetamol (acetaminophen; N-acetyl-p-aminophenol remains controversial. Previous studies on rats suggested that the antinociceptive action of paracetamol might involve the central descending inhibitory pain pathways recruiting both a serotoninergic and an opioidergic system. This study explores this issue in mice using paroxetine, the most potent selective serotonin re-uptake inhibitor, and the nonselective opioid pure antagonist naloxone. Animals were divided into two main groups for two separate experiments, each subdivided into 3 subgroups. In both experiments; the first group served as control, the second group received paracetamol (200 mg/kg, i.p. In one experiment, the third group received paroxetine (20 mg/kg p.o for 7 days before paracetamol. In the other experiment, animals of the third group were pretreated with naloxone (5 mg/kg, i.p 30 min before paracetamol. The antinociceptive effect of paracetamol was tested using the hot plate test. Paracetamol displayed a significant antinociceptive activity that was augmented by pretreatment with paroxetine as was shown by maintenance of its effect beyond that shown by paracetamol alone. On the other hand, pretreatment with naloxone abolished paracetamol’s antinociceptive activity in the hot-plate test. These results extended the previous observation in rats that the antinociceptive effect of paracetamol involved activation of a central descending pain inhibitory pathway with serotonin and opioidergic peptides being potential mediators recruited.

  8. Pharmacology of kratom: an emerging botanical agent with stimulant, analgesic and opioid-like effects.

    Science.gov (United States)

    Prozialeck, Walter C; Jivan, Jateen K; Andurkar, Shridhar V

    2012-12-01

    Kratom (Mitragyna speciosa) is a plant indigenous to Thailand and Southeast Asia. Kratom leaves produce complex stimulant and opioid-like analgesic effects. In Asia, kratom has been used to stave off fatigue and to manage pain, diarrhea, cough, and opioid withdrawal. Recently, kratom has become widely available in the United States and Europe by means of smoke shops and the Internet. Analyses of the medical literature and select Internet sites indicate that individuals in the United States are increasingly using kratom for the self-management of pain and opioid withdrawal. Kratom contains pharmacologically active constituents, most notably mitragynine and 7-hydroxymitragynine. Kratom is illegal in many countries. Although it is still legal in the United States, the US Drug Enforcement Administration has placed kratom on its "Drugs and Chemicals of Concern" list. Physicians should be aware of the availability, user habits, and health effects of kratom. Further research on the therapeutic uses, toxic effects, and abuse potential of kratom and its constituent compounds are needed. PMID:23212430

  9. Analgesic and uterine relaxant effects of isoliquiritigenin, a flavone from Glycyrrhiza glabra.

    Science.gov (United States)

    Shi, Yulu; Wu, Debin; Sun, Zhen; Yang, Jing; Chai, Hongyan; Tang, Li; Guo, Yue

    2012-09-01

    Shaoyao-gancao-tang, a Chinese medicinal formula consisting of peony and licorice has been used for the treatment of dysmenorrhea for thousands of years. The purpose of the present study was to demonstrate the analgesic and uterine relaxant effects of isoliquiritigenin (ISL), a flavonoid isolated from the roots of Glycyrrhiza glabra (a type of licorice). In vitro, isoliquiritigenin caused concentration-dependent inhibition of spontaneous contraction of isolated rat uterus and the contraction induced by various types of stimulants, such as acetylcholine (Ach, 10 mM), KCl (40 mM) and oxytocin (1 mU/mL). The uterine contractile response to cumulative concentrations of CaCl? was blocked by 0.1 and 1 mM of isoliquiritigenin. The isoliquiritigenin-induced relaxation was partly inhibited by the nitric oxide synthase (NOS) inhibitor Nv-nitro-L-arginine methylester (L-NAME, 100 mM) and the COX-1/COX-2 inhibitor indomethacin (10mM). In vivo, isoliquiritigenin could cause a significant reduction in the acetic acid-induced writhing response and hot-plate test at the high dose. These results indicate that isoliquiritigenin, a flavonoid isolated from the roots of Glycyrrhiza glabra, not only has a spasmolytic effect on uterine contraction, which is in relation to Ca²? channels, NOS and COX, but also an effective activity in reducing pain. PMID:22389128

  10. Does transcutaneous electrical nerve stimulation (TENS) have a clinically relevant analgesic effect on different pain conditions? A literature review

    OpenAIRE

    Asami Naka; Mohammed Keilani; Stefan Loefler; Richard Crevenna

    2013-01-01

    Transcutaneous electric nerve stimulation (TENS) is a standard therapy used in different painful conditions such as low back pain, diabetic polyneuropathy or arthrosis. However, literature reviews focusing on the effects and the clinical implication of this method in various painful conditions are yet scarce. The purpose of this literature research was to determine, whether TENS provides an analgesic effect on common painful conditions in clinical practice. Literature research was performed u...

  11. Relationship between serotonin transporter occupancies and analgesic effects of AS1069562, the (+)-isomer of indeloxazine, and duloxetine in reserpine-induced myalgia rats.

    Science.gov (United States)

    Murai, N; Fushiki, H; Honda, S; Murakami, Y; Iwashita, A; Irie, M; Tamura, S; Nagakura, Y; Aoki, T

    2015-03-19

    Serotonin (5-HT) and norepinephrine (NE) have been implicated in the mediation of endogenous analgesic mechanisms via the descending inhibitory pain pathway in the brain, and dysfunction in both the 5-HT and NE systems has been suggested as an etiology of fibromyalgia (FM). Given that 5-HT reuptake inhibition in the brain appears to be associated with pain reduction, this mechanism might exert an analgesic effect also on pain associated with FM. In this case, it would be of interest to investigate the correlation of 5-HT transporter (SERT) occupancy with in vivo analgesic effect on pain associated with FM. Here, we investigated the relationship between SERT occupancies and the analgesic effects of AS1069562, the (+)-isomer of indeloxazine, and duloxetine, which are both 5-HT and NE reuptake inhibitors (SNRIs), on muscular pain in reserpine-induced myalgia (RIM) rats, an animal model of FM-like chronic pain. We also investigated the SERT occupancy level necessary for AS1069562 and duloxetine to exert analgesic effects on muscular pain. AS1069562 and duloxetine attenuated muscular hyperalgesia in RIM rats, representing the first findings to be reported regarding the analgesic effect of AS1069562 on pain associated with FM. SERT occupancy levels of AS1069562 and duloxetine increased in both dose- and plasma and brain concentration-dependent manners. SERT occupancy levels of AS1069562 and duloxetine were significantly correlated with efficacy on muscular pain thresholds in RIM rats. This finding concerning the precise correlation of SERT occupancy with in vivo analgesic effect on pain associated with FM is reported here for the first time. SERT occupancy level above 70% was necessary for AS1069562 and duloxetine to exert significant analgesic effects on muscular pain. These results suggest that SERT occupancy level is useful in determining appropriate analgesic doses of AS1069562 and duloxetine for treating pain symptoms in FM patients. PMID:25595980

  12. A placebo-controlled, double-blind, crossover trial on analgesic effect of nitrous oxide-oxygen inhalation

    DEFF Research Database (Denmark)

    GrØnbæk, Anni Birgitte; Svensson, Peter

    2014-01-01

    BACKGROUND: The sedative effect of nitrous oxide-oxygen (N2 O/O2 ) inhalation is relatively well established. Less in known about its analgesic effect. AIM: To determine the analgesic effect of N2 O/O2 inhalation on pulp sensitivity and jaw muscle pressure pain threshold in children. DESIGN: A placebo-controlled, double-blind, crossover trial with random allocation to two sequences: atmospheric air at the first session and N2 O/O2 at the second; or N2 O/O2 at the first session and atmospheric air at the second. Measurements included reaction time, pulp pain sensitivity, jaw muscle pressure pain thresholds and a VAS score of overall discomfort from the pain tests. RESULTS: Fifty-six children (12-15 years) completed the study. N2 O/O2 inhalation increased reaction time (P 

  13. Suppressive effect of electromagnetic field on analgesic activity of tramadol in rats.

    Science.gov (United States)

    Bodera, P; Stankiewicz, W; Antkowiak, B; Paluch, M; Kieliszek, J; Sobiech, J; Zdanowski, R; Wojdas, A; Siwicki, A K; Skopi?ska-Rózewska, E

    2012-01-01

    The electromagnetic fields (EMFs) have been shown to alter animal and human behavior, such as directional orientation, learning, pain perception (nociception or analgesia) and anxiety-related behaviors. The aim of this study was to evaluate the influence of electromagnetic fields of high-frequency microwaves on pain perception and anti-nociceptive activity of tramadol (TRAM) - analgetic effective in the treatment of moderate to severe acute and chronic pain states. Electromagnetic fields exposures of a)1500 MHz frequency and b) modulated, 1800 MHz (which is identical to that generated by mobile phones) were applied. Paw withdrawal latency (PWL) to thermal stimulus was measured in vehicle or tramadol (TRAM) treated animals before and after 30, 60 and 90 minutes from injections. The differences in the level of pain (PWL) between control group and rats exposed to EMF alone in three measurements, were not observed. Tramadol alone significantly increased PWLs to thermal stimulus in comparison to vehicle results at 30 (p < 0.001) and 60 minutes (p < 0.05) after drug injection. EMF exposure of both frequencies transiently suppressed analgesic effect of tramadol, significantly reducing paw withdrawal latency in animals treated with this drug at 30 minutes from the drug injection. PMID:22708363

  14. Effects of some analgesic anaesthetic drugs on human erythrocyte glutathione reductase: an in vitro study.

    Science.gov (United States)

    Senturk, Murat; Irfan Kufrevioglu, O; Ciftci, Mehmet

    2009-04-01

    Inhibitory effects of some analgesic and anaesthetic drugs on human erythrocyte glutathione reductase were investigated. For this purpose, human erythrocyte glutathione reductase was initially purified 2139-fold in a yield of 29% by using 2', 5'-ADP Sepharose 4B affinity gel and Sephadex G-200 gel filtration chromatography. SDS polyacrylamide gel electrophoresis confirmed the purity of the enzyme by sharing a single band. A constant temperature (+4 degrees C) was maintained during the purification process. Diclofenac sodium, ketoprofen, lornoxicam, tenoxicam, etomidate, morphine and propofol exhibited inhibitory effects on the enzyme in vitro using the Beutler assay method. K(i) constants and IC(50) values for drugs were determined from Lineweaver-Burk graphs and plotting activity % versus [I] graphs, respectively. The IC(50) values of diclofenac sodium, ketoprofen, lornoxicam, propofol, tenoxicam, etomidate and morphine were 7.265, 6.278, 0.3, 0.242, 0.082, 0.0523 and 0.0128 mM and the K(i) constants were 23.97 +/- 2.1, 22.14 +/- 7.6, 0.42 +/- 0.18, 0.418 +/- 0.056, 0.13 +/- 0.025, 0.0725 +/- 0.0029 and 0.0165 +/- 0.0013 mM, respectively. While diclofenac sodium, ketoprofen, lornoxicam, tenoxicam etomidate and morphine showed competitive inhibition, propofol displayed noncompetitive inhibition. PMID:18608753

  15. Enhancement of Analgesic Effect by Combination of Non-Noxious Stimulation and Noxious Stimulation in Humans.

    Science.gov (United States)

    Fujii-Abe, Keiko; Umino, Masahiro; Fukayama, Haruhisa; Kawahara, Hiroshi

    2014-12-10

    The aim of the this study was to investigate the combined effects of heterosegmental non-noxious and noxious stimulation on electrically induced tooth pain. The late component of somatosensory-evoked potentials (SEP), induced by electrical tooth stimulation and pain intensity, were examined under electrical stimulation to forearms. Noxious, non-noxious, and combined non-noxious and noxious electrical stimulation were applied to median nerves on the forearms. Four experimental sessions (ie, control session, combined non-noxious and noxious stimulation session, non-noxious stimulation session, and noxious stimulation session were performed for each subject at each 10-minute interval for 30 minutes. The amplitudes of the SEP and VAS scores in the combined stimulation session decreased significantly compared with those in the control session and the reduction rates were 51.1% (13.4 ?V) and 41.0% (23.5 mm), respectively. These results show that the combined stimulation has a more potent analgesic effect than that of either the non-noxious or the noxious stimulation. It is suggested that a potent analgesia was produced by an activated central mechanism, including endogenous opioid and descending pain inhibitory systems due to combined non-noxious and noxious stimulation. PMID:25490991

  16. Postoperative analgesic effects of dexketoprofen, buprenorphine and tramadol in dogs undergoing ovariohysterectomy.

    Science.gov (United States)

    Morgaz, J; Navarrete, R; Muñoz-Rascón, P; Domínguez, J M; Fernández-Sarmiento, J A; Gómez-Villamandos, R J; Granados, M M

    2013-08-01

    The objective of this study was to compare the postoperative analgesic effects of dexketoprofen, tramadol, and buprenorphine in dogs undergoing ovariohysterectomy. Seventy-five adult female dogs were randomly assigned to receive an intravenous injection (IV) of 1mg/kg of dexketoprofen (D), 0.02 mg/kg of buprenorphine (B) or 2mg/kg of tramadol (T). Pain assessment was performed during 48 h after ovariohysterectomy using a dynamic interactive visual analogue scale (DIVAS) and Glasgow composite measure pain scale (CMPS-SF). Rescue analgesia was required in 43%, 21%, and 5% of dogs in the B, T, and D groups, respectively, with significant differences between B and D (p=0.010) groups. The DIVAS and CMPS-SF values of the B group were significantly higher than those of the T and D groups. The most common undesirable effect was dysphoria in dexketoprofen group. Tramadol and dexketoprofen provide superior postoperative analgesia compared with buprenorphine in dogs undergoing ovariohysterectomy. PMID:23562407

  17. Efecto del zumo de Morinda citrifolia L. (noni en modelos de analgesia Effect of Morinda citrifolia L. (noni in analgesic models

    Directory of Open Access Journals (Sweden)

    Nora Sánchez Rodríguez

    2012-09-01

    Full Text Available Introducción: Morinda citrifolia L. (noni ha despertado gran interés y expectativa dentro de la población cubana debido a las propiedades medicinales que se le atribuyen. Investigaciones realizadas evidencian las propiedades analgésicas de algunas de sus partes. Objetivos: evaluar el efecto del zumo de noni en diferentes modelos de analgesia. Métodos: se utilizaron dosis (450, 900 y 1 800 mg/kg del zumo de noni, a partir de contenido en peso seco; se administró por vía intraperitoneal a ratones OF1 en el modelo de irritación peritoneal por ácido acético 0,6 % y se cuantificó el número de contorsiones o estiramientos. Además, se utilizó el modelo del plato caliente y el de la retirada de la cola. Resultados: el zumo de noni fue efectivo de manera dependiente de la dosis en reducir el número de contorsiones inducidas por el ácido acético. En los modelos del plato caliente y de retirada de la cola, solo la dosis más alta prolongó de manera estadísticamente significativa el tiempo de reacción. Conclusiones: los resultados sugieren que el efecto analgésico de noni es fundamentalmente de mecanismo periférico.Introduction: Morinda citrifolia L. (noni has aroused great interest and expectations in the Cuban population due to attributed medicinal properties. Several research works have suggested the analgesic effect of several parts of the plant. Objectives: to evaluate the effect of Noni juice in different analgesic models. Methods: there were used 450, 900, and 1 800 mg/kg doses of the juice, based on the dry content weight. They were administered intraperitonealy to adult male mice OF1 in the peritoneal irritation model induced by acetic acid at 0.6 % concentration, and the number of contorsions or stretchings was quantified. Additionally, the hot plate and the tail immersed in hot water models were applied. Results: the noni juice was effective in reducing the number of contortions induced by the acetic acid in a dose-dependent manner. Just the highest dose of the juice increased significantly the time of reaction in the hot plate and in the tail immersion test. Conclusions: these results suggest that the analgesic effect of Noni juice is basically peripheral.

  18. Efecto del zumo de Morinda citrifolia L. (noni) en modelos de analgesia / Effect of Morinda citrifolia L. (noni) in analgesic models

    Scientific Electronic Library Online (English)

    Nora, Sánchez Rodríguez; Margarita, Bu Wong; Héctor, Pérez-Saad; Gloria, Lara Fernández; Isidoro, Scull.

    2012-09-01

    Full Text Available SciELO Cuba | Language: Spanish Abstract in spanish Introducción: Morinda citrifolia L. (noni) ha despertado gran interés y expectativa dentro de la población cubana debido a las propiedades medicinales que se le atribuyen. Investigaciones realizadas evidencian las propiedades analgésicas de algunas de sus partes. Objetivos: evaluar el efecto del zum [...] o de noni en diferentes modelos de analgesia. Métodos: se utilizaron dosis (450, 900 y 1 800 mg/kg) del zumo de noni, a partir de contenido en peso seco; se administró por vía intraperitoneal a ratones OF1 en el modelo de irritación peritoneal por ácido acético 0,6 % y se cuantificó el número de contorsiones o estiramientos. Además, se utilizó el modelo del plato caliente y el de la retirada de la cola. Resultados: el zumo de noni fue efectivo de manera dependiente de la dosis en reducir el número de contorsiones inducidas por el ácido acético. En los modelos del plato caliente y de retirada de la cola, solo la dosis más alta prolongó de manera estadísticamente significativa el tiempo de reacción. Conclusiones: los resultados sugieren que el efecto analgésico de noni es fundamentalmente de mecanismo periférico. Abstract in english Introduction: Morinda citrifolia L. (noni) has aroused great interest and expectations in the Cuban population due to attributed medicinal properties. Several research works have suggested the analgesic effect of several parts of the plant. Objectives: to evaluate the effect of Noni juice in differe [...] nt analgesic models. Methods: there were used 450, 900, and 1 800 mg/kg doses of the juice, based on the dry content weight. They were administered intraperitonealy to adult male mice OF1 in the peritoneal irritation model induced by acetic acid at 0.6 % concentration, and the number of contorsions or stretchings was quantified. Additionally, the hot plate and the tail immersed in hot water models were applied. Results: the noni juice was effective in reducing the number of contortions induced by the acetic acid in a dose-dependent manner. Just the highest dose of the juice increased significantly the time of reaction in the hot plate and in the tail immersion test. Conclusions: these results suggest that the analgesic effect of Noni juice is basically peripheral.

  19. Involvement of serotonin 2A receptors in the analgesic effect of tramadol in mono-arthritic rats.

    Science.gov (United States)

    Xie, Hong; Dong, Zhi-Qiang; Ma, Fei; Bauer, William R; Wang, Xin; Wu, Gen-Cheng

    2008-05-19

    The analgesic effects of tramadol are considered to be mediated by both the opioid system and the serotonergic system. This study investigated the involvement of a subtype of serotonin receptors, 5-hydroxytryptamine (5-HT)2A receptor, in the analgesic effect of tramadol. The intraperitoneal (i.p.) injection of tramadol reduced the paw withdrawal latency (PWL) to radiant heat testing in mono-arthritic rats. The antagonistic effect of i.p. ketanserin (a 5-HT2A receptor antagonist) on tramadol analgesia was observed. The expression of the 5-HT2A receptor mRNA in the nucleus of raphe magnus (NRM), ventrolateral periaqueductal gray (vlPAG) and spinal dorsal horn of mono-arthritic rats after a ten-day treatment with tramadol was measured with in situ hybridization. Either single injections or 10 days of tramadol treatment dose-dependently elevated PWL of arthritic rats while ketanserin could partially antagonize the tramadol analgesic effect. Expression of the 5-HT2A receptor mRNA in NRM, ipsilateral vlPAG, and the ipsilateral spinal dorsal horn of arthritic rats was significantly increased after tramadol treatment. These results suggest that 5-HT2A receptors are involved in the analgesic effect of tramadol. This study provides evidence for involvement of 5-HT2A receptors in the tramadol analgesia of inflammatory pain. The increase in this receptor mRNA in the chronic study may contribute to the sustaining effect of tramadol long-term treatments in clinical practice. PMID:18417104

  20. Peripheral and central effects of circulating catecholamines.

    Science.gov (United States)

    Tank, A William; Lee Wong, Dona

    2015-01-01

    Physical challenges, emotional arousal, increased physical activity, or changes in the environment can evoke stress, requiring altered activity of visceral organs, glands, and smooth muscles. These alterations are necessary for the organism to function appropriately under these abnormal conditions and to restore homeostasis. These changes in activity comprise the "fight-or-flight" response and must occur rapidly or the organism may not survive. The rapid responses are mediated primarily via the catecholamines, epinephrine, and norepinephrine, secreted from the adrenal medulla. The catecholamine neurohormones interact with adrenergic receptors present on cell membranes of all visceral organs and smooth muscles, leading to activation of signaling pathways and consequent alterations in organ function and smooth muscle tone. During the "fight-or-flight response," the rise in circulating epinephrine and norepinephrine from the adrenal medulla and norepinephrine secreted from sympathetic nerve terminals cause increased blood pressure and cardiac output, relaxation of bronchial, intestinal and many other smooth muscles, mydriasis, and metabolic changes that increase levels of blood glucose and free fatty acids. Circulating catecholamines can also alter memory via effects on afferent sensory nerves impacting central nervous system function. While these rapid responses may be necessary for survival, sustained elevation of circulating catecholamines for prolonged periods of time can also produce pathological conditions, such as cardiac hypertrophy and heart failure, hypertension, and posttraumatic stress disorder. In this review, we discuss the present knowledge of the effects of circulating catecholamines on peripheral organs and tissues, as well as on memory in the brain. PMID:25589262

  1. [Acemetacin in the treatment of painful arthroses. Results of an open short-term study on the starting point of the analgesic effect and its duration].

    Science.gov (United States)

    Siegmeth, W; Bröll, H; Schragl, F

    1984-11-30

    Acemetacin was tested in an open clinical study with regard to occurrence and duration of its analgesic effect to 20 patients suffering from arthrosis of the hip and knee joint. The treatment lasted 3 days. The therapeutic effect was judged by the influence of pain on rest and movement. With Acemetacin the majority of the patients reported a quick onset and long duration of the analgesic effect. The tolerance of Acemetacin was very good. PMID:6531936

  2. Analgesic Effect of Odontopaste and a Compound Intracanal Medicament Between Root Canal Therapy Appointments

    Science.gov (United States)

    Eftekhar, Behrooz; Moghimipour, Eskandar; Pourakbar Jahandideh, Pejman; Jalali, Sahar; Mahmoudian, Mahsa

    2013-01-01

    Background Pain experience makes a serious anxiety for both patient and clinician before and after root canal treatment. Pain is a complex psychophysiologic phenomenon. Objectives The aim of this randomized control trial study was to evaluate the analgesic effect of Odontopaste® and a corticosteroid containing compound medicament between root canal therapy appointments. Materials and Methods One hundred and twenty lower first and second mandibular molars with spontaneous pain and sensitivity to percussion were selected and divided into three groups (40 patients per each group). After root canal preparation, patients were entered one of these groups randomly. Root canals in group 1 were dressed with Odontopaste, in group 2 with a compound intracanal medicament, and in group 3 with placebo. Patients determined their pain rate and percussion sensitivity on Heft-parker VAS diagram, before the first appointment and 24 hours and 7 days after that. Results Spontaneous pain and Percussion sensitivity score averages of 24 hours after the first appointment in group 1 and group 2 were less than group 3, which indicates statistically significant difference between these groups. There was no statistically significant difference between these groups after 7 days neither on spontaneous pain nor percussion sensitivity. Conclusions Odontopaste® and compound intracanal medicaments resulted in statistically significant reduction in postoperative pain and percussion sensitivity after 24 hours, but there was no statistically significant difference after 7 days with placebo. PMID:24624209

  3. Analgesic effects of maxillary and inferior alveolar nerve blocks in cats undergoing dental extractions.

    Science.gov (United States)

    Aguiar, Joana; Chebroux, Alexandre; Martinez-Taboada, Fernando; Leece, Elizabeth A

    2015-02-01

    The aim of this study was to evaluate the analgesic effects of maxillary and/or inferior alveolar nerve blocks with lidocaine and bupivacaine in cats undergoing dental extractions. Twenty-nine cats were enrolled. Using an adapted composite pain scale, cats were pain scored before the dental procedure and 30 mins, and 1, 2 and 4 h after isoflurane disconnection. Cats were sedated with buprenorphine (20 µg/kg), medetomidine (10 µg/kg) and acepromazine (20 µg/kg) intramuscularly. Anaesthesia was induced using alfaxalone (1-2 mg/kg) intravenously and maintained with isoflurane in oxygen. Each cat was randomly assigned to receive maxillary and/or inferior alveolar nerve blocks or no nerve blocks prior to dental extractions. Each nerve block was performed using lidocaine (0.25 mg/kg) and bupivacaine (0.25 mg/kg). Heart rate, systolic arterial blood pressure, respiratory rate, end tidal carbon dioxide and isoflurane vaporiser settings were recorded 5 mins before and after the dental extractions, and the difference calculated. Group mean differences (mean ± SD) for heart rate (-9.7 ± 10.6 vs 7.6 ± 9.5 beats/min [nerve block vs control group, respectively], P heart rate and blood pressure while allowing for a reduction in isoflurane. Cats receiving nerve blocks had lower postoperative pain scores than the group without nerve blocks. PMID:24820999

  4. Characterization of novel cannabinoid based T-type calcium channel blockers with analgesic effects.

    Science.gov (United States)

    Bladen, Chris; McDaniel, Steven W; Gadotti, Vinicius M; Petrov, Ravil R; Berger, N Daniel; Diaz, Philippe; Zamponi, Gerald W

    2015-02-18

    Low-voltage-activated (T-type) calcium channels are important regulators of the transmission of nociceptive information in the primary afferent pathway and finding ligands that modulate these channels is a key focus of the drug discovery field. Recently, we characterized a set of novel compounds with mixed cannabinoid receptor/T-type channel blocking activity and examined their analgesic effects in animal models of pain. Here, we have built on these previous findings and synthesized a new series of small organic compounds. We then screened them using whole-cell voltage clamp techniques to identify the most potent T-type calcium channel inhibitors. The two most potent blockers (compounds 9 and 10) were then characterized using radioligand binding assays to determine their affinity for CB1 and CB2 receptors. The structure-activity relationship and optimization studies have led to the discovery of a new T-type calcium channel blocker, compound 9. Compound 9 was efficacious in mediating analgesia in mouse models of acute inflammatory pain and in reducing tactile allodynia in the partial nerve ligation model. This compound was shown to be ineffective in Cav3.2 T-type calcium channel null mice at therapeutically relevant concentrations, and it caused no significant motor deficits in open field tests. Taken together, our data reveal a novel class of compounds whose physiological and therapeutic actions are mediated through block of Cav3.2 calcium channels. PMID:25314588

  5. Altered Frequency Distribution in the Electroencephalogram is Correlated to the Analgesic Effect of Remifentanil.

    Science.gov (United States)

    Graversen, Carina; Malver, Lasse P; Kurita, Geana P; Staahl, Camilla; Christrup, Lona L; Sjøgren, Per; Drewes, Asbjørn M

    2015-05-01

    Opioids alter resting state brain oscillations by multiple and complex factors, which are still to be elucidated. To increase our knowledge, multi-channel electroencephalography (EEG) was subjected to multivariate pattern analysis (MVPA), to identify the most descriptive frequency bands and scalp locations altered by remifentanil in healthy volunteers. Sixty-two channels of resting EEG followed by independent measures of pain scores to heat and bone pain were recorded in 21 healthy males before and during remifentanil infusion in a placebo-controlled, double-blind crossover study. EEG frequency distributions were extracted by a continuous wavelet transform and normalized into delta, theta, alpha, beta and gamma bands. Alterations relative to pre-treatment responses were calculated for all channels and used as input to the MVPA. Compared to placebo, remifentanil increased the delta band and decreased the theta and alpha band oscillations as a mean over all channels (all p ? 0.007). The most discriminative channels in these frequency bands were F1 in delta (83.33%, p = 0.0023) and theta bands (95.24%, p brain activity during remifentanil treatment. As the EEG alterations were correlated to the analgesic effect, the approach may prove to be a novel methodology for monitoring individual efficacy to opioids. PMID:25250670

  6. Superior Analgesic Effect of an Active Distraction versus Pleasant Unfamiliar Sounds and Music: The Influence of Emotion and Cognitive Style

    OpenAIRE

    Garza Villarreal, Eduardo A.; Brattico, Elvira; Vase, Lene; Østergaard, Leif; Vuust, Peter

    2012-01-01

    Listening to music has been found to reduce acute and chronic pain. The underlying mechanisms are poorly understood; however, emotion and cognitive mechanisms have been suggested to influence the analgesic effect of music. In this study we investigated the influence of familiarity, emotional and cognitive features, and cognitive style on music-induced analgesia. Forty-eight healthy participants were divided into three groups (empathizers, systemizers and balanced) and received acute pain indu...

  7. Individual Difference Variables and the Effects of Progressive Muscle Relaxation and Analgesic Imagery Interventions on Cancer Pain

    OpenAIRE

    Kwekkeboom, Kristine L.; Wanta, Britt; Bumpus, Molly

    2008-01-01

    Clinicians in acute care settings are often called upon to manage cancer pain unrelieved by medications. Cognitive-behavioral strategies, such as relaxation and imagery, are recommended for cancer pain management; however, there appear to be individual differences in their effects. This pilot study examined variation in pain outcomes achieved with progressive muscle relaxation (PMR) and analgesic imagery interventions among hospitalized patients with cancer pain, and assessed the influence of...

  8. Validación preclínica de actividad analgésica periférica y central de la decocción de hojas frescas de Persea americana Mill. (aguacate) y Musa x paradisiaca L. (plátano) / Preclinical validation of the peripheral and central analgesic activity of decoction of fresh leaves of Persea americana Mill. (avocado) and Musa x paradisiaca L. (banana)

    Scientific Electronic Library Online (English)

    Ana Ibis, García Hernández; Marisol, López Barreiro; Zulema, Morejón Rodríguez; Elisa, Boucourt Rodríguez; María del Carmen, Victoria Amador; Ioanna, Martínez Hormaza; Lérida Lázara, Acosta de la Luz; Abel, Doménigo González; Gisselle, Brito Alvarez; Francisco J, Morón Rodríguez.

    2014-09-01

    Full Text Available Introducción: Persea americana Mill. (aguacate) y Musa x paradisiaca L. (plátano), son dos plantas medicinales que entre sus usos tradicionales reportados, se cita, el efecto beneficioso de la decocción de las hojas frescas de aguacate para la infección urinaria, tos, bronquitis y las de plátano par [...] a la gripe, tos e inflamación. Documentado por las encuestas TRAMIL. No se encontró información preclínica suficiente en las bases de datos: SciELO, CUMED, LIS CUBA y MEDLINE para validar sus usos. Objetivos: evaluar la actividad analgésica periférica y central preclínicas de la decocción al 30 % de hojas frescas de Persea americana Mill. (aguacate) y Musa x paradisiaca L. (plátano). Métodos: se colectaron las hojas frescas de P. americana y M. paradisiaca y se realizaron las decocciones al 30 %. Se evaluó la actividad analgésica periférica mediante el modelo de contorsiones inducidas por ácido acético(writhing test), y la actividad analgésica central fue evaluada aplicando el modelo de retirada de la cola por inmersión en agua 55 ºC (tail flick) en ratones, con dosis de 1, 5, y 10 gramos de material vegetal/kg de peso corporal. Resultados: las decocciones de hojas frescas de P. americana y M. paradisiaca a las dosis estudiadas, inhibieron de forma significativa la respuesta dolorosa inducida por ácido acético con p=6,909e-08 y p=2,842e-03respectivamente. En la evaluación del tail flick, la decocción de hojas frescas de P. americana, tuvo una respuesta significativa no dosis dependiente a (5g/kg), con una p=7,018e-03; las otras dosis estudiadas y la decocción de M. paradisiaca no tuvieron respuesta significativa. Conclusiones: los resultados obtenidos permiten realizar la validación preclínica de la actividad analgésica periférica de la decocción de hojas frescas P. americana (aguacate) y M. paradisiaca (plátano), así como de la actividad analgésica central de P. americana, lo que avala su uso tradicional. Abstract in english Introduction: Persea americana Mill. (avocado) and Musa x paradisiaca L. (banana) are medicinal plants with traditional uses in folk medicine. Reports refer to the beneficial effects of a decoction of fresh leaves of avocado in the treatment of urinary infection, coughing and bronchitis. Decoction o [...] f banana fresh leaves is used to treat the flu, coughing and inflammation. This has been documented by TRAMIL surveys. The preclinical information found in the databases SciELO, CUMED, LIS CUBA and MEDLINE was not sufficient to validate the uses listed above. Objectives: evaluate the preclinical peripheral and central analgesic activity of a 30 % decoction of fresh leaves of Persea americana Mill. (avocado) and Musa x paradisiaca L. (banana). Methods: fresh leaves of P. americana and M. paradisiaca were collected and 30 % decoctions were prepared. Peripheral analgesic activity was evaluated with the acetic acid induced writhing model (writhing test), whereas central analgesic activity was assessed with the tail flick model in mice by immersion in 55 ºC water. The doses used were 1, 5 and 10 grams of plant material / kg of body weight. Results: decoctions of fresh leaves of P. americana and M. paradisiaca at the study doses significantly inhibited the painful response induced by acetic acid with p=6.909e-08 and p=2.842e-03, respectively. In the tail flick evaluation the decoction of fresh leaves of P. americana had a significant non-dose dependent response at 5g/kg with p=7.018e-03. A significant response was not obtained from the other doses studied or from the M. paradisiaca decoction. Conclusions: results permit the preclinical validation of the peripheral analgesic activity of the decoction of fresh leaves of P. americana (avocado) and M. paradisiaca (banana), as well as the central analgesic activity of P. americana, validating the traditional use of both plants.

  9. Synthesis and Analgesic Effects of ?-TRTX-Hhn1b on Models of Inflammatory and Neuropathic Pain

    Directory of Open Access Journals (Sweden)

    Yu Liu

    2014-08-01

    Full Text Available ?-TRTX-Hhn1b (HNTX-IV is a 35-amino acid peptide isolated from the venom of the spider, Ornithoctonus hainana. It inhibits voltage-gated sodium channel Nav1.7, which has been considered as a therapeutic target for pain. The goal of the present study is to elucidate the analgesic effects of synthetic ?-TRTX-Hhn1b on animal models of pain. The peptide was first synthesized and then successfully refolded/oxidized. The synthetic peptide had the same inhibitory effect on human Nav1.7 current transiently expressed in HEK 293 cells as the native toxin. Furthermore, the analgesic potentials of the synthetic peptide were examined on models of inflammatory pain and neuropathic pain. ?-TRTX-Hhn1b produced an efficient reversal of acute nociceptive pain in the abdominal constriction model, and significantly reduced the pain scores over the 40-min period in the formalin model. The efficiency of ?-TRTX-Hhn1b on both models was equivalent to that of morphine. In the spinal nerve model, the reversal effect of ?-TRTX-Hhn1b on allodynia was longer and higher than mexiletine. These results demonstrated that ?-TRTX-Hhn1b efficiently alleviated acute inflammatory pain and chronic neuropathic pain in animals and provided an attractive template for further clinical analgesic drug design.

  10. The analgesic and anti-inflammatory effects of Litsea japonica fruit are mediated via suppression of NF-?B and JNK/p38 MAPK activation.

    Science.gov (United States)

    Koo, Hyun Jung; Yoon, Weon-Jong; Sohn, Eun-Hwa; Ham, Young-Min; Jang, Seon-A; Kwon, Jung-Eun; Jeong, Yong Joon; Kwak, Jong Hwan; Sohn, Eunsoo; Park, Soo-Young; Jang, Ki-Hyo; Namkoong, Seung; Han, Hyo-Sang; Jung, Yong-Hwan; Kang, Se Chan

    2014-09-01

    Fruits of the Litsea family of trees and shrubs contain biologically active compounds, some of which have been used as natural nutrients and flavoring agents in food. In this study, we identified novel anti-nociceptive effects of the 30% ethanol extract, the CH(2)Cl(2) fraction and the associated active components (Hamabiwalactone A and B) from Litsea japonica fruit by using in vivo peripheral and central nervous pain models. In addition, we compared the anti-inflammatory effects of several fractions from L. japonica fruit extracts using lipopolysaccharide (LPS)-stimulated Raw264.7 cells. The CH(2)Cl(2) fraction of L. japonica fruit (LJM) had an optimal combination of anti-inflammatory effects and low cytotoxicity. Dose response studies were performed to determine the inhibitory effects of LJM on the pro-inflammatory enzymes, COX-2/PGE(2) and NO/iNOS, and pro-inflammatory cytokines, IL-1?, IL-6, and TNF-?. Molecular profiling revealed that LJM exerts anti-inflammatory effects through inhibition of NF-?B and JNK/p38 MAPK signaling in LPS-induced macrophages. This study suggests that CH2Cl2 fraction of L. japonica fruit and its bioactive components are potential candidates as anti-inflammatory and analgesic agents (painkillers) for the treatment of inflammatory diseases. PMID:24968348

  11. [Analgesic activity of different nonvolatile extracts of Nepeta atlantica Ball and Nepeta Tuberosa L. ssp. reticulata (Desf.) Maire].

    Science.gov (United States)

    Bouidida, El Houcine; Alaoui, Katim; Cherrah, Yahia; Chammache, Malika; Il Idrissi, Abdelkader

    2008-01-01

    Different extracts of Nepeta atlantica Ball and Nepeta tuberosa L. ssp. reticulata (Desf.) Maire contain mainly secondary metabolites with iridoïd lactonic and glucosidic type, also with triterpine lupan type.The aerial part of each species is crushed, then extracted in methanol by cold maceration, called global extracts. The global extracts will be extracted through various solvents: initially by hexane, then by dichloromethane, after that by ethyl acetate and at the end by buthanol. Each one of the obtained extracts will be used for the following trials: i) Tail flick trial on the rat for central morphine-like analgesic activity; ii) Koster trial on the mouse for peripheral analgesic activity. The evaluation of the central and peripheral analgesic activities for the pre-cited extracts was realized after optimal doses determination of the global extracts activities for both species.The peripheral analgesic activity test on the mouse showed that, for 60 mg/kg intra peritoneum (IP), the hexanic, dichloromethanic, ethyl acetate and butanic extracts have a protection power against abdominal cramp respectively around 89.78%, 81.73%, 70.9% et 69.05% for Nepeta atlantica Ball, and around 89.16%, 82.98%, 71.52% et 70.27% for Nepeta tuberosa L. ssp. reticulata.Central morphine-like analgesic activity on the rat showed that, for both spices under 60 mg/kg IP, the central analgesic activity effect is significantly for two extracts only: dichloromethane and ethyl acetate. PMID:18937913

  12. Effect of oral clonidine premedication on perioperative haemodynamic response and post-operative analgesic requirement for patients undergoing laparoscopic cholecystectomy

    Directory of Open Access Journals (Sweden)

    Singh Shivinder

    2011-01-01

    Full Text Available Clonidine has anti-hypertensive properties and augments the effects of anaesthesia, hence we considered it to be an ideal agent to contain the stress response to pneumoperitoneum. We studied the clinical efficacy of oral clonidine premedication in patients undergoing laparoscopic cholecystectomies. Fifty patients scheduled for elective laparoscopic cholecystectomy under general anaesthesia were randomly allocated to receive premedication with either oral clonidine 150 ?g (Group I, n = 25 or placebo (Group II, n = 25 90 minutes prior to induction. The patients were managed with a standard general anaesthetic. The two groups were compared with respect to haemodynamic parameters, isoflurane concentration, pain and sedation scores, time to request of analgesic and cumulative analgesic requirements. Oral clonidine was found to be significantly better in terms of maintaining stable haemodynamics, having an isoflurane sparing effect and having a prolonged time interval to the first request of analgesia postoperatively compared to the control group. Administration of oral clonidine 150 ?g as a pre-medicant in patients undergoing laparoscopic cholecystectomy results in improved perioperative haemodynamic stability and a reduction in the intra-operative anaesthetic and post-operative analgesic requirements.

  13. Analgesic and systemic effects of xylazine, lidocaine and their combination after subarachnoid administration in goats

    Directory of Open Access Journals (Sweden)

    R. DeRossi

    2012-06-01

    Full Text Available The objective of the study was to determine the analgesic and systemic effects of subarachnoid administration of xylazine hydrochloride (XY, lidocaine hydrochloride (LI and their combination (XYLI in goats. Six healthy goats were used in a prospective randomised study. Three treatments were administered to each goat, with 1-week intervals between each treatment. Treatments consisted of 0.1 mg/kg xylazine, 2.5 mg/kg lidocaine and a combination of xylazine 0.05 (mg/kg and lidocaine (1.25 mg/kg. Analgesia, ataxic, sedative, cardiovascular and respiratory effects, and rectal temperature were evaluated before (baseline and at 5, 10, 15, and 30 min after subarachnoid injection, and then at 30-min intervals until loss of analgesia occurred. Lidocaine induced analgesia in 3.1 + 1min (mean + SD, which lasted for 66 + 31 min. Heart and respiratory rates and blood pressure remained unchanged after lidocaine-induced analgesia. Xylazine induced analgesia in 9.5 + 2.6 min and xylazine-lidocaine in 3.2 + 1.2 min. Xylazine-lidocaine-induced analgesia lasted longer (178.3 + 37 min than that induced by xylazine (88.3 + 15 min. The XYLI treatment induced prolonged motor blocking (115 min, more than the XY (80 min and LI (90 min treatments. Both xylazine and xylazine-lidocaine caused significant decreases in the heart and respiratory rates, but not in blood pressure. The combination of xylazine (0.05 mg/kg and lidocaine (1.25 mg/kg can be administered subarachnoidally (between last lumbar vertebra and 1st sacral vertebra to produce prolonged (>2.5 h analgesia of the tail, perineum, hind limbs, flanks and caudodorsal rib areas in goats. Despite the prolonged analgesia, using this combination is desirable for relieving postoperative pain, but it may be a disadvantage due to a motor block when dealing with goats.

  14. Compare the Analgesic Effectiveness of Diclofenac and Paracetamol in Patients with Renal Colic

    Directory of Open Access Journals (Sweden)

    Murat Ayan

    2013-01-01

    Full Text Available    Aim: This retrospective study was aimed to compare the analgesic effectiveness of paracetamol and diclofenac sodium by using visual analog acale (VAS in patients applying to emergency room with renal colic. Material and Method: Group I (n=40 patients diagnosed with renal colic and treated with diclofenac sodium (75 mg intramuscular and Group II (n=40 patients diagnosed with renal colic and treated with paracetamol (1 g intravenous were included in this study. In both groups, patients were between 19-64 years old. In all groups, the intensity of the pain was ranked between 0 (no pain and 10 (intolerable by using VAS. VAS score of the groups were compared. Result: Before the treatment VAS values of at Group I; 7.95 ± 1.48 while Group II; 7.92 ± 1.76. Respectively in the 10th and 30th minutes VAS value of patient Group I; 5.35±2.19/ 3.73±1.93 and Group II; 4.28±1.9/2.33±1.77. Before the treatment VAS value of paracetamol group was not different from the diclofenac sodium group. However, after the treatment, in the 10th and 30th minutes, VAS values of the paracetamol group scores were lower than diclofenac group (P=0.022 ve 0.002. Discussion: According to our study’s finding, paracetamol gives good results in the renal colic pain treatment. Moreover, paracetamol which lower side effects than non-steroidal antiinflammatory drug (NSAIDs may be a good alternative in the treatment of renal colic.

  15. Analgesic and cardiopulmonary effects of intrathecally administered romifidine or romifidine and ketamine in goats (Capra hircus

    Directory of Open Access Journals (Sweden)

    H.P. Aithal

    2012-07-01

    Full Text Available The study was conducted to evaluate the effects of romifidine alone (50 µg/kg and a combination of romifidine (50 µg/kg and ketamine (2.5 mg/kg after intrathecal administration in goats. Ten adult goats of either sex weighing between 15 and 20 kg were randomly placed in 2 groups (groups I and II. The agents were administered at the lumbosacral subarachnoid space. Clinico-physiological parameters such as analgesia, motor incoordination, sedation, salivation, heart rate, respiratory rate, arterial pressure, central venous pressure and rectal temperature were studied. Other haematobiochemical parameters monitored were packed cell volume, haemoglobin, plasma proteins, glucose, urea and creatinine. The onset of analgesia was faster in group II (35.5 ±6.25 s compared to that of group I (5.2 ±0.54 min. Analgesia of the tail, perineum, hind limbs, flank and thorax was mild to moderate in group I, but complete analgesia of tail, perineum and hind limbs was recorded in group II. Motor incoordination was mild in group I and severe in group II. Significant reduction in heart rate (more pronounced in group I and respiratory rate (more pronounced in group II, and a significant increase in central venous pressure were recorded in both groups. Mean arterial pressure was reduced in both groups, but more markedly in group I. Sedation, electro-cardiogram, rectal temperature and haemato-biochemical parameters did not show significant differences between the 2 groups. The results of this study indicated a possible synergistic analgesic interaction between intrathecally administered romifidine and ketamine, without causing any marked systemic effects in goats.

  16. Involvement of ATP-sensitive K(+) channels in the peripheral antinociceptive effect induced by the alpha(2)-adrenoceptor agonist xylazine.

    Science.gov (United States)

    Romero, Thiago Roberto Lima; Duarte, Igor Dimitri Gama

    2009-12-01

    Xylazine is an alpha(2)-adrenergic agonist extensively used in veterinary medicine and animal experimentation for producing antinociception, sedation, and muscle relaxation. The nitric oxide (NO) / cGMP / ATP-sensitive K(+) (K(ATP)) channel pathway has been proposed as the action mechanism of peripheral antinociception of several groups of drugs, including opioids and nonsteroidal analgesics. Considering the lack of knowledge regarding the mechanisms involved in xylazine effects, the present study investigated the contribution of K(+) channels on peripheral antinociception induced by xylazine using the rat paw pressure test, in which hyperalgesia was induced by intraplantar injection of prostaglandin E(2). Xylazine administered into the right hind paw elicited a local antinociceptive effect, since only much higher doses produced a systemic effect in the contralateral paw. The peripheral antinociceptive effect induced by xylazine was antagonized by glibenclamide, a specific blocker of K(ATP) channels. In another experiment, tetraethylammonium, a voltage-dependent K(+)-channel blocker, and paxilline and dequalinium, which are selective blockers for the large- and small-conductance Ca(2+)-activated K(+) channels, respectively, were ineffective at blocking xylazine antinociception. These results provide evidence that the peripheral antinociceptive effect of xylazine probably results from K(ATP)-channel activation, while the voltage-dependent K(+) channels, small- and large-conductance Ca(2+)-activated K(+) channels, appear not to be involved in this mechanism. PMID:20019444

  17. Altered Frequency Distribution in the Electroencephalogram is Correlated to the Analgesic Effect of Remifentanil

    DEFF Research Database (Denmark)

    Graversen, Carina; Malver, Lasse P

    2014-01-01

    Opioids alter resting state brain oscillations by multiple and complex factors, which are still to be elucidated. To increase our knowledge, multi-channel electroencephalography (EEG) was subjected to multivariate pattern analysis (MVPA), to identify the most descriptive frequency bands and scalp locations altered by remifentanil in healthy volunteers. Sixty-two channels of resting EEG followed by independent measures of pain scores to heat and bone pain were recorded in 21 healthy males before and during remifentanil infusion in a placebo-controlled, double-blind crossover study. EEG frequency distributions were extracted by a continuous wavelet transform and normalized into delta, theta, alpha, beta and gamma bands. Alterations relative to pre-treatment responses were calculated for all channels and used as input to the MVPA. Compared to placebo, remifentanil increased the delta band and decreased the theta and alpha band oscillations as a mean over all channels (all p ? 0.007). The most discriminative channels in these frequency bands were F1 in delta (83.33%, p = 0.0023) and theta bands (95.24%, p < 0.0001), and C6 in the alpha band (80.95%, p = 0.0054). These alterations were correlated to individual changes in heat pain in the delta (p = 0.045), theta (p = 0.038) and alpha (p = 0.039) bands and to bone pain in the alpha band (p = 0.0092). Hence, MVPA of multi-channel EEG was able to identify frequency bands and corresponding channels most sensitive to altered brain activity during remifentanil treatment. As the EEG alterations were correlated to the analgesic effect, the approach may prove to be a novel methodology for monitoring individual efficacy to opioids.

  18. Interdose interval effects on the development of contextual tolerance to nicotine's analgesic effects in rats (Rattus norvegicus).

    Science.gov (United States)

    Cepeda-Benito, Antonio; Reynoso, Jose T; Davis, Kristina W; Susabda, Agnes; Mendez, Ian A; Harraid, James H

    2006-05-01

    Learning models of associative and nonassociative drug tolerance predict that the development of contextual tolerance to drug effects is disrupted when the drug is delivered at short interdose intervals (IDIs). The authors examined the impact of 1 long IDI and 2 short IDIs in the development of contextual nicotine tolerance. Associative tolerance was investigated by giving rats (Rattus norvegicus) 10 subcutaneous injections of nicotine at either long (72-hr) IDIs or short (6-hr and 4.5-hr) IDIs. The delivery of nicotine was either explicitly paired or explicitly unpaired with a distinctive context. A 3rd group of rats was exposed to the experimental procedures but received only saline. Associative tolerance to nicotine's analgesic effects was defined as a shift to the right of the dose-response curve (DRC) of rats in the explicitly paired condition with respect to the DRC of rats in the explicitly unpaired condition. Analgesia was assessed with the tail-flick and hot-plate devices. In the tail-flick assessment, associative tolerance was evident in the 72-hr and the 6-hr IDI conditions only. In the hot-plate assessment, associative tolerance was present in the 72-hr IDI condition only. The findings suggest that contextual tolerance to nicotine's analgesic effects are positively related to IDI length and are more readily demonstrated with the tail-flick method than with the hot-plate method. Overall, the results supported the thesis that nicotine tolerances that develop to different IDIs are qualitatively different and may be mediated by different psychological and physiological mechanisms. PMID:16756422

  19. Elucidation of possible mechanism of analgesic action of Valeriana wallichii DC chemotype (patchouli alcohol) in experimental animal models.

    Science.gov (United States)

    Sah, Sangeeta Pilkhwal; Mathela, Chandra S; Chopra, Kanwaljit

    2010-03-01

    Valeriana wallichii (Family Valerianaceae), popularly named as Indian valerian, exists as three chemotypes. Aim of the study was to evaluate the effect of V. wallichii chemotype (patchouli alcohol) extract (DCME) and essential oil (VPAEO) on experimental models of nociception and to elucidate its possible mechanism of action. Analgesic effect was evaluated using acetic acid induced writhing and tail flick model. DCME and VPAEO (40 and 80 mg/kg, p.o.) significantly inhibited the number of writhings as compared to vehicle treated group. None of the doses of DCME and VPAEO exhibited any effect in tail flick model suggesting only peripheral analgesic activity. When studied for mechanism of action in acetic acid induced writhing, subeffective dose of essential oil significantly potentiated the effect of aspirin while no potentiation was seen in case of extract. These data suggest that essential oil VPAEO exerted peripheral analgesic via inhibition of prostaglandin synthesis. PMID:21046983

  20. The analgesic effect of Magnesium Sulfate in postoperative pain of inguinal hernia repair

    Directory of Open Access Journals (Sweden)

    Mehraein A

    2007-08-01

    Full Text Available Background: Magnesium Sulfate (MgSO4 has been used as a pharmacologic agent in different situations for many years in the treatment of tachyarrhythmias, myocardial ischemia, preeclampsia, and tocolysis among others. The analgesic effect of MgSO4 for postoperative pain has been used since the 1990s. Postoperative pain is one of the most common complications in the perioperative period and can result in serious consequences in different organs if left untreated. Inguinal herniorrhaphy is among the most common surgeries and is almost always accompanied by severe pain. The object of this study is to determine the effect of a pre-induction infusion of MgSO4 on the reduction of postsurgical pain after herniorrhaphy. Methods: This double-blind, randomized clinical trial included 105 ASA class I and class II herniorrhaphy patients at Shariati Hospital in years 2004 and 2005. For statistical analysis, the ?2 and T tests were used. The patients were divided into three groups based on block randomization. Patients in the following groups received: Group A, 200 ml of normal saline infusion (placebo; Group B, 25 mg/kg MgSO4 in 200 ml of normal saline; Group C, 50 mg/kg MgSO4 in 200 ml of normal saline. All groups were infused twenty minutes before induction of anesthesia using identical methods and dosage in all three groups. Heart rate and mean arterial pressure (MAP at pre- and postintubation and so at skin incision time were charted. Visual analog scale (VAS pain score, nausea, vomiting and the amount of morphine used before recovery room discharge and in six, twelve and twenty-four hours after recovery discharge was recorded. Results: The average age for the different groups was as follows: Group A: 33.6, Group B: 37.37, Group C: 32.74. Nausea and vomiting between the case and control groups were not statistically different (60% vs. 71.4%, p=0.0499, nor was the amount of Morphine used. On recovery room discharge, the VAS scores were 8.1, 7.2, and 5.5 for the first, second and third groups, respectively (P<0.001. However, no statistical significance was found for the VAS scores six hours after recovery room discharge. Conclusion: The results in this study show that pre-induction with MgSO4 has no remarkable effect on decreasing postoperative pain or morphine use for inguinal herniorrhaphy.

  1. Evaluation of the Anti-inflammatory, Analgesic, and Anti-pyretic Effects of Origanum majorana Ethanolic Extract in Experimental Animals

    International Nuclear Information System (INIS)

    In the present investigation, various biological studies (toxicological, pharmacological, biochemical and histopathological) were carried out on Origanum majorana ethanolic extract. The acute toxicity study revealed that 0. majorana ethanolic extract is quietly safe. Both doses (0.25 and 0.5 g/kg b.wt.) of 0. majorana ethanolic extract showed a significant anti-inflammatory (acute and systemic), analgesic, and anti-pyretic effect. Moreover, histopathological findings of stomach and intestine of irradiated rats revealed that both doses of tested extract possess a gastrointestinal protective effect against radiation induced gastritis and enteritis

  2. Antiinflammatory and Analgesic Effects of Phlomis lanceolata Boiss. and Hohen. Extracts and Examination of their Components

    Directory of Open Access Journals (Sweden)

    M. Mohajer

    2006-01-01

    Full Text Available The purpose of this investigation was to study the anti-inflammatory and analgesic properties of total extract and four fractions (ether, ethyl acetate, n-butanol and water from Phlomis lanceolata (Lamiaceae in mice. The plant material was extracted with methanol. In order to estimate the polarity of the active compounds, the total extract was dissolved in water and the water soluble portion was successively partitioned between ether, ethyl acetate and n-buthanol. The total extract and four fractions were analyzed by Thin Layer Chromatography (TLC by use of specific reagents. Dose of 100 mg kg 1 of each extracts were used in carrageenan-induced paw edema, formalin and writhing nociception tests in mice. All compounds reduced paw edema in comparison to the control group at 1, 3, 5 and 7 h post carrageenan injection. The total, ether and aqueous extracts were similar to indomethacin while the ethyl acetate extract was weaker than indomethacin in reduction of paw edema. All extracts induced antinociception in both phases of formalin test. The total and ether extracts were as potent as indomethacin in both phases of formalin test. The ethyl acetate extract was weaker than indomethacin in the second phase of formalin-test while the n-butanol and aqueous extracts showed more antinociception than indomethacin in the second phase of formalin test. All extracts as well as indomethacin induced antinociception in writhing test in comparison to control. The total and aqueous extracts induced the same antinociception as indomethacin while ether, ethyl acetate and n-butanol showed weaker antinociception than indomethacin. Positive results for iridoids and phenolic compounds were indicated by phytochemical analysis of total extract. Phenolic compounds were found in four fractions whereas only n-butanol and aqueous fractions showed positive results for iridoid glycosides. The higher antinociceptive effects of n-butanol and aqueous extracts in the inflammatory phase of formalin test among different extracts tested, might back to the presence of iridoid glycosides, phenolic glycosides or other glycosides. These data suggest that different extracts of P. lanceolata produce different antinociceptive activities that could be due to the effect of one or a combination of the bioactive components in each extract.

  3. Intra- and post-operative analgesic effects of carprofen in medetomidine premedicated dogs undergoing ovariectomy

    Directory of Open Access Journals (Sweden)

    Seliškar Alenka

    2005-01-01

    Full Text Available Intra- and post-operative analgesic effects of pre-operative administration of carprofen were investigated in 16 medetomidine-premedicated dogs undergoing elective ovariectomy. Dogs were randomly allocated into carprofen (n=8; 4 mg/kg, intramuscularly or placebo group (n = 8. After medetomidine (1000 [xg/m2, intramuscularly premedication, they were induced with propofol (1 mg/kg, intravenously and maintained with isoflurane (FE'ISO 1.0 % in 100% oxygen. During anaesthesia, the analgesia was assessed in terms of changes in heart rate, respiratory rate and arterial blood pressure as a response to the surgery. Assessments of post-operative sedation (simple numerical rating scale and pain (multifactorial pain scale were made at 15 minutes, 30 minutes, 1,2,3, 4, 5, and 6 hours after the surgery. In addition, pulse rate, respiratory rate and body temperature were measured at the same time. During anaesthesia, lower heart rate, respiratory rate and mean arterial blood pressure and higher tidal volume of respiration were observed in the carprofen group. Post-operative pain score was relatively low in both groups of dogs, however it was higher, but not significantly, in the placebo group. There was no difference between the groups in terms of respiratory and pulse rate after surgery. The post-operative sedation score was higher in the placebo group only in the early post-operative period most probably due to misinterpretation of pain behaviour. Carprofen together with other anaesthetic drugs provided sufficient intra-operative analgesia only until major painful surgical stimulus occurred, after which analgesia had to be supplemented with a subanaesthetic dose of ketamine. Comparing to that analgesia was insufficient in the placebo group throughout the procedure. The post-operative pain scoring system was probably not sensitive enough to detect the differences between the groups; however, the effects of other drugs that extended in the post-operative period may be responsible for a low post­operative pain score in both groups of dogs.

  4. Analgesic Effects of Fatty Acid Amide Hydrolase Inhibition in a Rat Model of Neuropathic Pain

    OpenAIRE

    Jhaveri, Maulik; Richardson, Denise; Kendall, David; Barrett, David; Chapman, Victoria

    2006-01-01

    Cannabinoid-based medicines have therapeutic potential for the treatment of pain. Augmentation of levels of endocannabinoids with inhibitors of fatty acid amide hydrolase (FAAH) is analgesic in models of acute and inflammatory pain states. The aim of this study was to determine whether local inhibition of FAAH alters nociceptive responses of spinal neurons in the spinal nerve ligation model of neuropathic pain. Electrophysiological studies were performed 14-18 days after spinal nerve ligation...

  5. Dexibuprofen (S+-isomer ibuprofen) reduces gastric damage and improves analgesic and antiinflammatory effects in rodents.

    OpenAIRE

    Isaia, Giovanni Carlo; Zara, Gian Paolo

    2003-01-01

    We determined the analgesic and antiinflammatory actions and the related acute mucosal gastric damage from the active S(+)-isomer ibuprofen (dexibuprofen), in comparison with those of the standard racemic formulation of ibuprofen in rodents. The antinociception was evaluated by hot-plate and tail-flick methods after IV and oral (PO) administration in mice and after PO administration in rats. S(+)-Ibuprofen was at least twice more potent than the ibuprofen racemic formulation. The antiinflamma...

  6. Peripheral analgesic blockade of hypernociception: Activation of arginine/NO/cGMP/protein kinase G/ATP-sensitive K+ channel pathway

    OpenAIRE

    Sachs, Daniela; Cunha, Fernando Q.; Ferreira, Se?rgio H.

    2004-01-01

    The final step in the direct restoration of the nociceptor threshold by peripheral administration of morphine and dipyrone was recently suggested to result from the opening of ATP-sensitive K+ channels (\\documentclass[12pt]{minimal} \\usepackage{amsmath} \\usepackage{wasysym} \\usepackage{amsfonts} \\usepackage{amssymb} \\usepackage{amsbsy} \\usepackage{mathrsfs} \\setlength{\\oddsidemargin}{-69pt} \\begin{document} \\begin{equation*}{\\mathrm{K}}_{{\\mathrm{ATP}}}^{+}\\end{e...

  7. Anti-Arthritic and Analgesic Effect of NDI10218, a Standardized Extract of Terminalia chebula, on Arthritis and Pain Model

    OpenAIRE

    Seo, Jong Bae; Jeong, Jae-yeon; Park, Jae Young; Jun, Eun Mi; Lee, Sang-ik; Choe, Sung Sik; Park, Do-yang; Choi, Eun-wook; Seen, Dong-seung; Lim, Jong-soon; Lee, Tae Gyu

    2012-01-01

    The fruit of Terminalia chebula Retzius has been used as a panacea in India and Southeast Asia but its biological activities have not been fully elucidated. Here we report anti-arthritic and analgesic effect of NDI10218, a standardized ethanol extract of Terminalia chebula, on collagen-induced arthritis and acetic acid-induced writhing model, respectively. Arthritis was induced in DBA/1J mice by immunizing bovine type II collagen and mice were treated with NDI10218 daily for 5 weeks after the...

  8. Analgesic Treatment in Patients With Acute Extremity Trauma and Effect of Training

    Directory of Open Access Journals (Sweden)

    Funda KARBEK AKARCA

    2012-01-01

    Full Text Available Objectives: Studies indicate that emergency physicians (EP under-evaluate and undertreat the pain experienced by their patients. The objective of this study was to investigate how EPs treat pain in adult patients with limb trauma and to determine if their behavior could be affected by training in the short-term. Methods: All consecutive adult patients admitted to the university-based emergency department (ED within two months were enrolled in the study. The patients were asked to rate their level of pain on the NRS in triage. NRS scores were noted again after 30 minutes and 60 minutes, and on discharge. Patient prescriptions were also tracked to identify any analgesics. After completion of the pre-education phase, four hours of training on pain evaluation and treatment were undertaken under the leadership of experienced staff faculty. The aforementioned outcomes were gathered again in a 30-day period after training and we compared the pre and post training periods. Results: A hundred and forty-three patients (81 female were enrolled in the pre-education phase, and 130 patients (58 female were eligible for the post-education phase. The mean NRS scores of the females noted on admission were significantly higher than those of the males (7.4±2.3 vs. 6.7±2.5, respectively; p=0.020. Patients included in the first phase received analgesia less frequently (42.7% vs. 70.0%, respectively; p<0.001. The mean period of time between admission and initial analgesic administration was shorter in the second phase (41.3 vs. 19.3 minutes, respectively; p<0.001. The ratio of patients receiving analgesia within thirty minutes was greater after training. All patients in the second phase received analgesia within 60 minutes. The residents prescribed analgesics more frequently after training. Conclusions: A four-hour training program resulted in apparent changes in the residents’ management of pain in patients with extremity trauma. In addition to a more timely administration, the rates of analgesic treatment increased.

  9. Analgesic and anti-inflammatory effectiveness of sitagliptin and vildagliptin in mice.

    Science.gov (United States)

    Újhelyi, Judit; Újhelyi, Zoltán; Szalai, Andrea; László, János F; Cayasso, Mayella; Vecsernyés, Miklós; Pórszász, Róbert

    2014-11-01

    To validate the potential anti-inflammatory and analgesic role of sita- and vildagliptin, five different experimental models were used in mice: i) mustard oil-induced ear edema, ii) neutrophil accumulation, iii) mechanical and iv) thermal touch sensitivity in complete Freund's adjuvant-induced arthritis and v) capsaicin-induced plasma extravasation in the urinary bladder. For the complete examination period in i) the dose of 10mg sitagliptin as well as 1-10mg vildagliptin was found to significantly decrease ear edema as compared to positive control (ptreatment of Type 2 diabetic patients. PMID:25229125

  10. Efecto analgésico del extracto acuoso liofilizado de Ocimum tenuiflorum L. / Analgesic effect of the freeze-dried aqueous extract of Ocimum tenuiflorum L.

    Scientific Electronic Library Online (English)

    Pedro, Barzaga Fernández; Yanier, Núñez Figueredo; Sarah, Agüero Fernández; Ismael, Chávez Hernández; María Lidia, González Sanabria; Yadira, Iser Valdés; Maylin, Olivera Carpio.

    2005-04-01

    Full Text Available Drogas con capacidad de inhibir la síntesis o acción de mediadores como los eicosanoides, histamina, bradicinina, entre otras, impiden la acción sensibilizadora de éstos sobre las terminaciones nerviosas nociceptivas. Teniendo en cuenta la actividad antiinflamatoria demostrada del extracto acuoso li [...] ofilizado de Ocimum tenuiflorum L., fue objetivo de este trabajo evaluar sus propiedades analgésicas en modelos animales. Dosis de O. tenuiflorum de 250, 500 y 1 000 mg/kg fueron evaluadas en modelos de inducción del dolor por vías química y térmica. Como resultado de este estudio se obtuvo que el extracto acuoso liofilizado de O tenuiflorum mostró efecto analgésico en los modelos del plato caliente a la dosis de 1 000 mg/kg; en el de contorsiones por ácido acético en ratones y foco calorífico en ratas a las dosis de 250, 500 y 1 000 mg/kg. Estos resultados indicaron que el extracto acuoso liofilizado de O. tenuiflorum ejerce un efecto antinociceptivo, preferentemente sobre la vía periférica. Abstract in english Drugs with the capacity of inhibiting the synthesis or action of mediators such as eikosanoids, histamine, bradycine, and others, hinder the sensitizing action of them on the nociceptive nervous terminationes. Taking into account the shown antiinflammatory activity of the freeze-dried aqueous extrac [...] t of Ocimum tenuiflorum L., it was the objective of this paper to evaluate the analgesic properties of it in animal models. Doses of O. tenuiflorum of 250, 500 and 1 000 mg/kg were evaluated in pain-induction models by chemical and thermic ways. As a result of this study it was observed that the freeze-dried aqueous extract of O. tenuiflorum. had an analgesic effect in the hot dish model at a dose of 1 000 mg/kg, and in that of contortions by acetic acid in mice and calorific focus in rats at doses of 250, 500 and 1 000 mg/kg. These results indicated that the freeze-dried aqueous extract of O. tenuiflorum has an antinociceptive effect, mainly on the peripheral pathway.

  11. Efecto analgésico del extracto acuoso liofilizado de Ocimum tenuiflorum L. Analgesic effect of the freeze-dried aqueous extract of Ocimum tenuiflorum L.

    Directory of Open Access Journals (Sweden)

    Pedro Barzaga Fernández

    2005-04-01

    Full Text Available Drogas con capacidad de inhibir la síntesis o acción de mediadores como los eicosanoides, histamina, bradicinina, entre otras, impiden la acción sensibilizadora de éstos sobre las terminaciones nerviosas nociceptivas. Teniendo en cuenta la actividad antiinflamatoria demostrada del extracto acuoso liofilizado de Ocimum tenuiflorum L., fue objetivo de este trabajo evaluar sus propiedades analgésicas en modelos animales. Dosis de O. tenuiflorum de 250, 500 y 1 000 mg/kg fueron evaluadas en modelos de inducción del dolor por vías química y térmica. Como resultado de este estudio se obtuvo que el extracto acuoso liofilizado de O tenuiflorum mostró efecto analgésico en los modelos del plato caliente a la dosis de 1 000 mg/kg; en el de contorsiones por ácido acético en ratones y foco calorífico en ratas a las dosis de 250, 500 y 1 000 mg/kg. Estos resultados indicaron que el extracto acuoso liofilizado de O. tenuiflorum ejerce un efecto antinociceptivo, preferentemente sobre la vía periférica.Drugs with the capacity of inhibiting the synthesis or action of mediators such as eikosanoids, histamine, bradycine, and others, hinder the sensitizing action of them on the nociceptive nervous terminationes. Taking into account the shown antiinflammatory activity of the freeze-dried aqueous extract of Ocimum tenuiflorum L., it was the objective of this paper to evaluate the analgesic properties of it in animal models. Doses of O. tenuiflorum of 250, 500 and 1 000 mg/kg were evaluated in pain-induction models by chemical and thermic ways. As a result of this study it was observed that the freeze-dried aqueous extract of O. tenuiflorum. had an analgesic effect in the hot dish model at a dose of 1 000 mg/kg, and in that of contortions by acetic acid in mice and calorific focus in rats at doses of 250, 500 and 1 000 mg/kg. These results indicated that the freeze-dried aqueous extract of O. tenuiflorum has an antinociceptive effect, mainly on the peripheral pathway.

  12. Analgesic effects of botulinum neurotoxin type A in a model of allyl isothiocyanate- and capsaicin-induced pain in mice.

    Science.gov (United States)

    Luvisetto, Siro; Vacca, Valentina; Cianchetti, Carlo

    2015-02-01

    We evaluate analgesic effects of BoNT/A in relation to the two main transient receptor potentials (TRP), the vanilloid 1 (TRPV1) and the ankyrin 1 (TRPA1), having a role in migraine pain. BoNT/A (15 pg/mouse) was injected in the inner side of the medial part of hindlimb thigh of mice, where the superficial branch of femoral artery is located. We chosen this vascular structure because it is similar to other vascular structures, such as the temporal superficial artery, whose perivascular nociceptive fibres probably contributes to migraine pain. After an interval, ranging from 7 to 30 days, capsaicin (agonist of TRPV1) or allyl isothiocyanate (AITC; agonist of TRPA1) were injected in the same region previously treated with BoNT/A and nocifensive response to chemicals-induced pain was recorded. In absence of BoNT/A, capsaicin and AITC induced extensive nocifensive response, with a markedly different temporal profile: capsaicin induced maximal pain during the first 5 min, while AITC induced maximal pain at 15-30 min after injection. Pretreatment with BoNT/A markedly reduced both the capsaicin- and AITC-induced pain for at least 21 days. These data suggest a long lasting analgesic effect of BoNT/A exerted via prevention of responsiveness of TRPV1 and TRPA1 toward their respective agonists. PMID:25529549

  13. Comparing the analgesic effect of heat patch containing iron chip and ibuprofen for primary dysmenorrhea: a randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Navvabi Rigi Shahindokht

    2012-08-01

    Full Text Available Abstract Background Primary dysmenorrhea is a common and sometimes disabling condition. In recent years, some studies aimed to improve the treatment of dysmenorrhea, and therefore, introduced several therapeutic measures. This study was designed to compare the analgesic effect of iron chip containing heat wrap with ibuprofen for the treatment of primary dysmenorrhea. Methods In this randomized (IRCT201107187038N2 controlled trial, 147 students (18–30?years old with the diagnosis of primary dysmenorrhea were enrolled considering the CONSORT guideline. Screening for primary dysmenorrhea was done by a two-question screening tool. The participants were randomly assigned into one of the intervention groups (heat Patch and ibuprofen. Data regarding the severity and emotional impact of the pain were recorded by a shortened version of McGill Pain Questionnaire (SF-MPQ. Student's?t test was used for statistical analysis. Results The maximum and minimum pain severities were observed at 2 and 24?hours in both groups. The severity of sensual pain at 8, 12, and 24?hours was non-significantly less in the heat Patch group. There was also no significant difference between the groups regarding the emotional impact of pain at the first 2, 4, 8, 12 and 12?hours of menstruation. Conclusions Heat patch containing Iron chip has comparable analgesic effects to ibuprofen and can possibly be used for primary dysmenorrhea. Trial registration IRCT201107187038N2

  14. Comparing the analgesic effects of periaqueductal gray matter injection of orexin A and morphine on formalin- induced nociceptive behaviors.

    Directory of Open Access Journals (Sweden)

    Hassan azhdari Zarmehri

    2008-11-01

    Full Text Available Introduction: Orexin-A and B (Hypocretin 1 and 2 are neuropeptides that are mostly expressed in the posterior and lateral hypothalamus (LH. Intracisternal (ICV and intratechal (IT injections of orexin-A (hypocretin-1 have been shown to elicit analgesic responses in formalin test. However, the locations of central sites that may mediate these effects have not been clearly elucidated. Orexin-containing fibers are projected to periaqueductal gray matter (PAG, which is involved in pain modulation. Methods: Behavioral study was done on male Sprague Dawley rats (200-300 g in formalin induced nociceptive behaviour. Results: Intra-PAG microinjection of orexin-A produced a dose-dependent inhibition of formalin-evoked behaviour in interphase and phase 2, but not in phase 1, indicating an antinociceptive role of exogenous orexin-A in the PAG. Analgesic effect of orexin-A was less than and specific to inter- and late phase of formalin test, when compared with that of morphine (5 ?g/0.5?l after intra-PAG administration. Conclusion: The obtained results suggest that orexin-A plays an anti-nociceptive role in PAG, on the interphase and late phase of formalin test in rats. So it is possible that orexin-A might be involved in the mechanisms of inter- and last phases of formalin induced behaviours.

  15. Phytochemical profile and analgesic evaluation of Vitex cymosa leaf extracts

    Scientific Electronic Library Online (English)

    Suzana Guimarães, Leitão; Tereza Cristina dos, Santos; Franco, Delle Monache; Maria Eline, Matheus; Patrícia Dias, Fernandes; Bruno Guimarães, Marinho.

    2011-10-01

    Full Text Available Vitex cymosa Bertero ex Spreng., Lamiaceae, is found in Central and Amazon regions of Brazil, where it is popularly used as antirheumatic. Extracts from the leaves of V. cymosa were tested in analgesia models such as abdominal contortions induced by acetic acid and formalin to test peripheral analge [...] sia; as well as the tail flick and hot plate models, to test spinal and supraspinal analgesia. A significant reduction was observed in the number of contortions with all extracts and in all doses. In the formalin model, a reduction in the second phase (inflammatory) was observed with all extracts, whereas only the n-butanol extract was able to act in the first, neurogenic, phase. In the tail flick model, all extracts increased latency time. Naloxone treatment reverted analgesic effect of all extracts with the exception of the dichloromethane one. All extracts developed peripheral and central analgesic activity. In the hot plate model no antinociceptive effect was observed for all tested extracts. All these results taken together suggest that V. cymosa leaf extracts were able to promote peripheral and central antinociceptive activity mediated by the opioid system.Twenty three substances were isolated and identified in the extracts and include flavonoids (C-glucosyl flavones, flavones and flavonols), triterpene acids from ursane and oleanane types, iridoids (free and glucosides), as well as simple phenols.

  16. Pharmacokinetic-pharmacodynamic modelling of the analgesic and antihyperalgesic effects of morphine after intravenous infusion in human volunteers

    DEFF Research Database (Denmark)

    Ravn, Pernille; Foster, David J R

    2014-01-01

    Using a modelling approach, this study aimed to (i) examine whether the pharmacodynamics of the analgesic and antihyperalgesic effects of morphine differ; (ii) investigate the influence of demographic, pain sensitivity and genetic (OPRM1) variables on between-subject variability of morphine pharmacokinetics and pharmacodynamics in human experimental pain models. The study was a randomized, double-blind, 5-arm, cross-over, placebo-controlled study. The psychophysical cutaneous pain tests, electrical pain tolerance (EPTo) and secondary hyperalgesia areas (2HA) were studied in 28 healthy individuals (15 males). The subjects were chosen based on a previous trial where 100 subjects rated (VAS) their pain during a heat injury (47°C, 7 min., 12.5 cm(2) ). The 33% lowest- and highest pain-sensitive subjects were offered participation in the present study. A two-compartment linear model with allometric scaling for weight provided the best description of the plasma concentration-time profile of morphine. Changes in theEPTo and 2HA responses with time during the placebo treatment were best described by a linear model and a quadratic model, respectively. The model discrimination process showed clear evidence for adding between-occasion variability (BOV) on baseline and the placebo slope for EPTo and 2HA, respectively. The sensitivity covariate was significant on baseline EPTo values and genetics as a covariate on the placebo slope for 2HA. The analgesic and antihyperalgesic effects of morphine were pharmacologically distinct as the models had different effect site equilibration half-lives and different covariate effects. Morphine had negligible effect on 2HA, but significant effect on EPTo.

  17. Pharmacokinetic-Pharmacodynamic Modelling of the Analgesic and Anti-hyperalgesic Effects of Morphine after Intravenous Infusion in Human Volunteers

    DEFF Research Database (Denmark)

    Ravn, Pernille; Foster, David J R

    2014-01-01

    Using a modelling approach, this study aimed to (i) examine whether the pharmacodynamics of the analgesic and anti-hyperalgesic effects of morphine differ; (ii) investigate the influence of demographic, pain sensitivity and genetic (OPRM1) variables on between-subject variability of morphine pharmacokinetics and pharmacodynamics in human experimental pain models. The study was a randomized, double-blind, 5-arm, cross-over, placebo-controlled study. The psychophysical cutaneous pain tests, electrical pain tolerance (EPTo) and secondary hyperalgesia areas (2HA) were studied in 28 healthy subjects (15 males). The subjects were chosen based on a previous trial where 100 subjects rated (VAS) their pain during a heat injury (47°C, 7 min., 12.5 cm(2) ). The 33% lowest- and highest pain sensitive subjects were offered participation in the present study. A two-compartment linear model with allometric scaling for weight provided the best description of the plasma concentration-time profile of morphine. Changes in the EPTo and 2HA responses with time during the placebo treatment were best described by a linear model and a quadratic model, respectively. The model discrimination process showed clear evidence for adding between occasion variability (BOV) on baseline and the placebo slope for EPTo and 2HA, respectively. The sensitivity covariate was significant on baseline EPTo values, and genetics as a covariate on the placebo slope for 2HA. The analgesic and anti-hyperalgesic effects of morphine were pharmacologically distinct as the models had different effect site equilibration half-lives and different covariate effects. Morphine had negligible effect on 2HA, but significant effect on EPTo. This article is protected by copyright. All rights reserved.

  18. Imidazoline receptor mediated natriuresis: central and/or peripheral effect?

    Science.gov (United States)

    Smyth, D D; Penner, S B

    1998-10-15

    The ability of imidazoline agonists, such as moxonidine and rilmenidine, to lower blood pressure has been attributed to a central effect resulting in a decrease in peripheral sympathetic nerve activity. A similar decrease in sympathetic nerve activity to the kidney has been proposed to explain the increase in sodium excretion. The observed increase in sodium excretion following an intrarenal infusion of moxonidine or rilmenidine suggested the existence of a direct renal action. We therefore tested the hypothesis that direct renal infusions were acting at a central rather than a peripheral site. Thus, interventions which would decrease the natriuretic effects of central administered moxonidine would also block the effects of intrarenal administered moxonidine. Studies were performed in anesthetized Sprague-Dawley rats (280-320 g) which had undergone unilateral nephrectomy 7 to 10 days prior to the experiment. The interventions utilized resulted in minimal effects on blood pressure and creatinine clearance. Intracerebroventricular (icv) or intrarenal (ir) administration of moxonidine produced a significant increase in urine flow rate and sodium excretion. Intravenous (iv) prazosin was used to block the ability of the sympathetic nerves to alter sodium excretion secondary to alpha1-adrenoceptor stimulation. Prazosin prevented the natriuresis following icv moxonidine but only partially antagonized the effects of ir moxonidine. To determine if central imidazoline receptors mediated the effects of moxonidine, animals were pretreated with icv idazoxan. Following icv idazoxan, the effects of icv moxonidine were blocked, whereas the response to intrarenal moxonidine was only partially blocked. Peripheral (iv) administration of idazoxan blocked the actions of intrarenal moxonidine but left the response to icv moxonidine intact. Finally, chemical sympathectomy with reserpine did not alter the response to intrarenal moxonidine suggesting that this effect was independent of the sympathetic nervous system. In conclusion, these studies indicate the ability of central and peripheral moxonidine to increase urine flow rate through sodium excretion at two unique sites of action, one central and the other one peripheral, most conceivably within the kidney. PMID:9851564

  19. In adjuvant-induced arthritic rats, acupuncture analgesic effects are histamine dependent: potential reasons for acupoint preference in clinical practice.

    Science.gov (United States)

    Huang, Meng; Zhang, Di; Sa, Zhe-Yan; Xie, Ying-Yuan; Gu, Chen-Li; Ding, Guang-Hong

    2012-01-01

    This study investigated whether immediate acupuncture effects in the acupoint are histamine dependent. Both histamine injection and manual acupuncture stimulation increased the pain threshold (PT) after treatment compared with the model group (P clemastine, an H1 receptor antagonist and an antipruritic, the increase in the animals' pain threshold after acupuncture was suppressed compared with the Acu group (P < 0.01); however, there was no interference with the acupuncture-induced degranulation of mast cells. Pretreatment with disodium cromolyn did not suppress the increase in PT induced by the histamine injection at Zusanli (ST-36). We conclude that in adjuvant-induced arthritic rats, acupuncture analgesic effects are histamine dependent, and this histamine dependence determines the acupoint preference of acupoints away from the target site in acupuncture practice. PMID:23990844

  20. Analgesic effects of JCM-16021 on neonatal maternal separation-induced visceral pain in rats

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    Zhao-Xiang Bian, Man Zhang, Quan-Bin Han, Hong-Xi Xu, Joseph JY Sung

    2010-02-01

    Full Text Available AIM: To investigate the pharmacological effect of JCM-16021, a Chinese herbal formula, and its underlying mechanisms.METHODS: JCM-16021 is composed of seven herbal plant materials. All raw materials of the formula were examined according to the quality control criteria listed in the Chinese Pharmacopeia (2005. In a neonatal maternal separation (NMS model, male Sprague-Dawley rats were submitted to daily maternal separation from postnatal day 2 to day 14, or no specific handling (NH. Starting from postnatal day 60, rats were administered JCM-16021 (2, 4, 8 g/kg per day orally twice a day for 28 d. Pain threshold pressure and electromyographic activities of external oblique muscles in response to colorectal distention recorded with a Power Lab System (AD Instruments International, were tested as pain indices. Changes in serotonin (5-HT and 5-hydroxyindoleacetic acid (5-HIAA concentrations in the colon of rats were analyzed; the enterochromaffin cell numbers and serotonin transporter in the colon of rats were also evaluated with an immunohistochemistry method.RESULTS: NMS treatment significantly reduced pain threshold pressure (37.4 ± 1.4 mmHg, as compared to that of NH rats (57.7 ± 1.9 mmHg, P < 0.05. After JCM-16021 treatment, the pain threshold pressure significantly increased when compared to that before treatment (34.2 ± 0.9 mmHg vs 52.8 ± 2.3 mmHg in the high dose group, 40.2 ± 1.6 mmHg vs 46.5 ± 1.3 mmHg in the middle dose group, and 39.3 ± 0.7 mmHg vs 46.5 ± 1.6 mmHg in the low dose group, P < 0.05. Also JCM-16021 significantly and dose-dependently decreased electromyographic activity to the graded colorectal distension (CRD, (the mean ?AUC values were: 0.17 ± 0.03, 0.53 ± 0.15, 1.06 ± 0.18, 1.22 ± 0.24 in the high dose group; 0.23 ± 0.04, 0.68 ± 0.17, 1.27 ± 0.26, 1.8 ± 0.3 in the middle dose group; and 0.29 ± 0.06, 0.8 ± 0.16, 1.53 ± 0.24, 2.1 ± 0.21 in the low dose group for the pressures 20, 40, 60, 80 mmHg, as compared to the NMS vehicle group. The mean ?AUC values were: 0.57 ± 0.12, 1.33 ± 0.18, 2.57 ± 0.37, 3.08 ± 0.37 for the pressures 20, 40, 60, 80 mmHg (P < 0.05. JCM-16021 treatment significantly reduced the 5-HT concentrations (from high, middle and low dosage groups: 60.25 ± 5.98 ng/100 mg, 60.32 ± 4.22 ng/100 mg, 73.31 ± 7.65 ng/100 mg, as compared to the NMS vehicle groups (93.11 ± 9.85 ng/100 mg, P < 0.05; and increased the 5-HIAA concentrations (after treatment, from high, middle and low dosage groups: 54.24 ± 3.27 ng/100 mg, 50.34 ± 1.26 ng/100 mg, 51.37 ± 2.13 ng/100 mg when compared to that in the NMS vehicle group (51.75 ± 1.98 ng/100 mg, P < 0.05; but did not change the enterochromaffin cell numbers in the colon of rats. In addition, NMS rats had higher SERT expression (n = 10 than NH rats (n = 8, P < 0.05. JCM-16021 treatment significantly decreased SERT expression when compared to the NMS group (P < 0.01-0.001.CONCLUSION: JCM-16021 can attenuate visceral hypersensitivity, and this analgesic effect may be mediated through the serotonin signaling pathway in the colon of rats.

  1. Evaluation of efficacy of sedative and analgesic effects of single IV dose of dexmedetomidine in post-operative patients

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    Manasa CR

    2013-09-01

    Full Text Available Background: In the post-operative period, it has always been an important consideration for clinicians, to keep the patient comfortable, calm and pain free. So there is a constant need for an ideal sedative for postoperative patients. Alpha 2 adrenoreceptor agonists such as dexmedetomidine could provide an answer to this problem because they have several relevant physiological properties like sedation, anxiolysis, analgesia and arousability. Hence, the current study was undertaken to evaluate the efficacy of dexmedetomidine in post-operative patients in order to avoid polypharmacy.Materials and Methods: Thirty patients who were operated under general anesthesia electively were randomly selected . All patients received 1 ?g/kg bodyweight of dexmedetomidine intravenously with normal saline making up to 10 ml over 20 minutes. If the verbal numerical scale (VNS of pain was mild (i.e. 1 to 3 one hour after extubation. The patients were assessed for degree and duration of sedation, hemodynamic changes, episodes of side effects, requirement of analgesics at every 5 min for first 30 min, every 10 min for next 1hr, every 15 min for next 1 h, and eve-ry 30 min for next 1h, every 1 h for 3h and 6th hourly till 24h. The need for rescue analgesic was noted.Results: The mean duration of sedation was 129.6 ± 41.02 min, degree of sedation was -1 at 30 min, duration of analgesia 241.5 min, and mean degree of analgesia was 0 at 30 min, mean degree of sedation was -1. Mean time of administration of rescue analgesia was 170 min. Mean heart rate was 67.8 ± 5.24/min and mean arterial pressure was 78.0 ± 8.97mm of Hg, mean respiratory rate was 15.8 ± 2.33 breaths/min, mean partial pressure of oxygen SpO2 was 99.5 ± 0.56%. No patient had any episode of shivering, vomiting, hypotension and respiratory depression.Conclusion: Single IV dose of dexmedetomidine could provide adequate sedative, analgesic and anxiolytic effects with no accompanying respiratory depression, thereby minimizing polypharmacy.

  2. Differential proteomics analysis of the analgesic effect of electroacupuncture intervention in the hippocampus following neuropathic pain in rats

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    Gao Yong-Hui

    2012-12-01

    Full Text Available Abstract Background Evidence is building steadily on the effectiveness of acupuncture therapy in pain relief and repeated acupuncture-induced pain relief is accompanied by improvement of hippocampal neural synaptic plasticity. To further test the cellular and molecular changes underlying analgesic effect of acupuncture, the global change of acupuncture associated protein profiles in the hippocampus under neuropathic pain condition was profiled. Methods The chronic constrictive injury (CCI model was established by ligature of the unilateral sciatic nerve in adult Wistar rats. Rats were randomized into normal control (NC group, CCI group, and CCI with electroacupuncture (EA stimulation group. EA was applied to bilateral Zusanli (ST36 and Yanglingquan (GB34 in the EA group. Differentially expressed proteins in the hippocampus in the three groups were identified by two-dimensional gel electrophoresis and matrix-assisted laser desorption/ionization time of flight mass spectrometry. The functional clustering of the identified proteins was analyzed by Mascot software. Results After CCI, the thermal pain threshold of the affected hind footpad was decreased and was reversed gradually by 12 sessions of acupuncture treatment. Following EA, there were 19 hippocampal proteins identified with significant changes in expression (>2-fold, which are involved in metabolic, physiological, and cellular processes. The top three canonical pathways identified were “cysteine metabolism”, “valine, leucine, and isoleucine degradation” and “mitogen-activated protein kinase (MAPK signaling”. Conclusions These data suggest that the analgesic effect of EA is mediated by regulation of hippocampal proteins related to amino acid metabolism and activation of the MAPK signaling pathway.

  3. Supra-spinal FAAH is required for the analgesic action of paracetamol in an inflammatory context.

    Science.gov (United States)

    Dalmann, Romain; Daulhac, Laurence; Antri, Myriam; Eschalier, Alain; Mallet, Christophe

    2015-04-01

    Paracetamol (acetaminophen) is the most commonly used analgesic in the world. Recently, a new view of its action has emerged: that paracetamol would be a pro-drug that should be metabolized by the FAAH enzyme into AM404, its active metabolite. However, this hypothesis has been demonstrated only in naive animals, a far cry from the clinical pathologic context of paracetamol use. Moreover, FAAH is a ubiquitous enzyme expressed both in the central nervous system and in the periphery. Thus, we explored: (i) the involvement of FAAH in the analgesic action of paracetamol in a mouse model of inflammatory pain; and (ii) the contributions of central versus peripheral FAAH in this action. The analgesic effect of paracetamol was evaluated in thermal hyperalgesia, mechanical allodynia and hyperalgesia induced by an intra-plantar injection of carrageenan (3%) in FAAH knock-out mice or their littermates. Moreover, the contribution of the central and peripheral enzymes was explored by comparing the effect of a global FAAH inhibitor (URB597) to that of a peripherally restricted FAAH inhibitor (URB937) on paracetamol action. Here, we show that in a model of inflammatory pain submitted to different stimuli, the analgesic action of paracetamol was abolished when FAAH was genetically or pharmacologically inhibited. Whereas a global FAAH inhibitor, URB597 (0.3 mg/kg), reduced the anti-hyperalgesic action of paracetamol, a brain-impermeant FAAH inhibitor, URB937 (0.3 mg/kg), had no influence. However, administered intracerebroventricularly, URB937 (5 ?g/mouse) reduced the action of paracetamol. These results demonstrate that the supra-spinally-located FAAH enzyme is necessary for the analgesic action of paracetamol. PMID:25448494

  4. Effects of the extracts from Mitragyna speciosa Korth. leaves on analgesic and behavioral activities in experimental animals

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    Kitja Sawangjaroen

    2007-03-01

    Full Text Available The leaves of Mitragyna speciosa Korth. (M. speciosa were extracted with methanol to give methanol extract. The methanol extract was made in acid and then in alkaline and extracted with chloroform to give alkaloid extract. The effects of the methanol and alkaloid extracts on analgesic activities in hot plate test in mice and tail flick test in rats and behavioral activities in locomotor activity and pentobarbital-induced sleep in mice, were examined. In acute toxicity test, the LD50 values of oral administration of the methanol and alkaloid extracts of M. speciosa leaves in mice were 4.90 g/kg and 173.20 mg/kg, respectively. Oral administration (50, 100 and 200 mg/kg of the methanol extract of M. speciosa leaves significantly prolonged the latency of nociceptive response on hot plate test in mice. The alkaloid extract of M. speciosa also increased the pain response latency at the dose of 20 mg/kg but less potent than those of the methanol extract (100 mg/kg in mice (comparing 5-10 mg/kg alkaloid extract with corresponding to approximately 200 mg/kg of methanol extract. The antinociceptive action of either methanol extract (100 mg/kg, p.o. or alkaloid extract (20 mg/kg, p.o. of M. speciosa leaves was blocked by naloxone (2 mg/kg, i.p. in mice. Neither the methanol extract nor the alkaloid extract significantly prolonged latency of nociceptive response on tail flick test in rats. Both of the extracts had no significant change on spontaneous motor activity or pentobarbital-induced sleep in mice, respectively. These results suggest that the methanol and alkaloid extracts of M. speciosa leaves possess the analgesic activity which partly acted at opioid receptors in the supraspinal opioid system.

  5. Analgesic and antisympathetic effects of clonidine in burn patients, a randomized, double-blind, placebo-controlled clinical trial

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    Ostadalipour Abbas

    2007-01-01

    Full Text Available Objectives: Unlike most other Analgesic drugs, ?2 adrenoceptor agonists are capable of producing analgesia. The aim of this study was to evaluate the Analgesic and antisympathetic effects of clonidine, an ?2 adrenoceptor agonist in burn patients. Materials and Methods: This randomized, double-blind, placebo-controlled clinical trial performed on one hundred burn patients in Zarea Hospital, Mazandaran, Iran from august 2004 to July 2005. All patients divided in two groups. Case group (n=50 received oral clonidine, 3.3?g/kg TDS and controls (n=50 received placebo. Heart rate and systolic blood pressure and pain severity Visual analogue score (VAS, were recorded after clonidine administration. Statistical analysis was done by means of Mann Witney U test. Results: 50 patients (mean age 28.96±10 years in case group, and 50 patients (mean age 27.60±11.4 years in control group were studied. VAS pain scores and heart rate in the clonidine group were significantly lower than the control group (P< 0.0001, P< 0.02.there were no significant difference in systolic blood pressure between the two groups on the first and second day but on third day the systolic blood pressure in clonidine group, was lower than controls significantly (P=0.002. Conclusion: This study demonstrates that the use of oral clonidine affects the hemodynamic response to pain in burn patients. Our study demonstrated that clonidine can produce good analgesia and decreased in sympathetic over activity in burn patients, and also reduce opioid dose requirements.

  6. Effect of Erythropoietin on Peripheral Nerve Regeneration

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    Mustafa OZKAN

    2010-03-01

    Full Text Available The aim of this study was to identify the effect of erythropoietin (EPO on a sciatic nerve injury model. The effect of single or repeated doses was also determined. Twenty-one Wistar rats were anesthetised and the sciatic nerve was transected 1 cm above the trifurcation and the nerve was repaired with four epineural 10/0 nylon sutures placed at 90 degrees intervals under microscope magnification.The rats were divided into 4 groups as follows: the sham,the saline, the single dose EPO and the multiple dose EPO. The skin was incised and closed and no treatment was given in sham group. In the saline group, 1 mL saline was given intraperitoneally; in the single EPO group, 5000 U/kg EPO was given intraperitoneally immediately after the procedure. In the multiple EPO group, 5000 U/kg EPO was given after the procedure and the same dose was repeated after the 1st, 2nd, 3rd and 4th weeks. Functional recovery was evaluated by static sciatic functional index(SSI.Single EPO group had greater myofibril size, axon number, diameter, and ratio M than the saline group. The multiple EPO treatment was not found to be more effective than single EPO treatment. However, no significant difference was found between the single EPO, multiple EPO, and saline groups based on the 3rd and 4th postoperative month SSI scores. Thus, EPO treatment increased axonal regeneration in our study. However, repeated dose therapy was not found to be more effective than single dose therapy. The optimum dose and duration should be researched in further studies.

  7. Immunohistochemical analysis of opioid receptors in peripheral tissues.

    Science.gov (United States)

    Schmidt, Yvonne; Machelska, Halina

    2015-01-01

    Immunohistochemical staining is widely used to identify opioid receptors in specific cell types or anatomical structures throughout the nervous system. Opioid receptors are not restricted to the central nervous system, but are also present in peripheral sensory neurons, where their activation exerts analgesic effects without inducing centrally mediated side effects. Here, we describe immunohistochemical analysis of opioid receptors in the peripheral sensory neuron cell bodies, along the axons and their peripheral endings in the hind paw skin, as well as in the spinal cord, under naïve and sciatic nerve damage conditions in mice. Moreover, we consider the current debate on the specificity of antibodies. PMID:25293323

  8. Superior analgesic effect of an active distraction versus pleasant unfamiliar sounds and music: The influence of emotion and cognitive style

    DEFF Research Database (Denmark)

    Garza Villarreal, Eduardo A.; Brattico, Elvira

    2012-01-01

    Previous studies have shown a superior analgesic effect of favorite music over other passive or active distractive tasks. However, it is unclear what mediates this effect. In this study we investigated to which extent distraction, emotional valence and cognitive styles may explain part of the relationship. Forty-eight healthy volunteers received heat stimuli during an active mental arithmetic task (PASAT), and passive listening to music (Mozart), environmental sounds (rain and water), and control (noise). The participants scored the conditions according to affective scales and filled out questionnaires concerning cognitive styles (Baron – Cohen and self-report). Active distraction with PASAT led to significantly less pain intensity and unpleasantness as compared to music and sound. In turn, both music and sound relieved pain significantly more than noise. When music and sound had the same level of valence they relieved pain to a similar degree. The emotional ratings of the conditions were correlated with the amount of pain relief and cognitive styles seemed to influence the analgesia effect. These findings suggest that the pain relieving effect previously seen in relation to music may be at least partly mediated by distraction, emotional factors and cognitive styles rather than by the music itself.

  9. Effects of the central analgesic tramadol and its main metabolite, O-desmethyltramadol, on rat locus coeruleus neurones.

    OpenAIRE

    Sevcik, J.; Nieber, K.; Driessen, B.; Illes, P.

    1993-01-01

    1. Tramadol is a centrally acting analgesic with low opioid receptor affinity and, therefore, presumably additional mechanisms of analgesic action. Tramadol and its main metabolite O-desmethyltramadol were tested on rat central noradrenergic neurones of the nucleus locus coeruleus (LC), which are involved in the modulation of nociceptive afferent stimuli. 2. In pontine slices of the rat brain the spontaneous discharge of action potentials of LC cells was recorded extracellularly. (-)-Tramadol...

  10. Analgesic effects of intra-articular botulinum toxin Type B in a murine model of chronic degenerative knee arthritis pain

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    Stephanie Anderson

    2010-09-01

    Full Text Available Stephanie Anderson1,2, Hollis Krug1,2, Christopher Dorman1, Pari McGarraugh1, Sandra Frizelle1, Maren Mahowald1,21Rheumatology Section, Veteran’s Affairs Medical Center, Minneapolis, Minnesota; 2Division of Rheumatology and Autoimmune Diseases, University of Minnesota Medical School, Minneapolis, Minnesota, USAObjective: To evaluate the analgesic effectiveness of intra-articular botulinum toxin Type B (BoNT/B in a murine model of chronic degenerative arthritis pain.Methods and materials: Chronic arthritis was produced in adult C57Bl6 mice by intra-articular injection of Type IV collagenase into the left knee. Following induction of arthritis, the treatment group received intra-articular BoNT/B. Arthritic control groups were treated with intra-articular normal saline or sham injections. Pain behavior testing was performed prior to arthritis, after induction of arthritis, and following treatments. Pain behavior measures included analysis of gait impairment (spontaneous pain behavior and joint tenderness evaluation (evoked pain response. Strength was measured as ability to grasp and cling.Results: Visual gait analysis showed significant impairment of gait in arthritic mice that improved 43% after intra-articular BoNT/B, demonstrating a substantial articular analgesic effect. Joint tenderness, measured with evoked pain response scores, increased with arthritis induction and decreased 49.5% after intra-articular BoNT/B treatment. No improvement in visual gait scores or decrease in evoked pain response scores were found in the control groups receiving intra-articular normal saline or sham injections. Intra-articular BoNT/B was safe, and no systemic effects or limb weakness was noted.Conclusions: This study is the first report of intra-articular BoNT/B for analgesia in a murine model of arthritis pain. The results of this study validate prior work using intra-articular neurotoxins in murine models. Our findings show chronic degenerative arthritis pain can be quantitated in a murine model by measuring gait impairment using visual gait analysis scores (spontaneous pain behavior and joint tenderness scores (evoked pain responses. Reduction of joint pain seen in this study is consistent with our hypothesis of inhibition of release of pain mediators by intra-articular BoNT/B, supporting further investigation of this novel approach to treatment of arthritis pain with intra-articular neurotoxins.Keywords: intra-articular BoNT/B, osteoarthritis

  11. Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II.

    Science.gov (United States)

    Gökçe, Ba?ak; Gençer, Nahit; Arslan, Oktay; Turko?lu, Sumeyye Aydogan; Alper, Meltem; Köçkar, Feray

    2012-02-01

    The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was compared to recombinant hCA I and hCA II expressed in Ecoli. IC(50) values of the drugs that caused inhibition were determined by means of activity percentage diagrams. The IC(50) concentrations of dexketoprofen trometamol and dexamethasone sodium phosphate on hCA I were 683 ?M and 4250 ?M and for hCA II 950 ?M and 6200 ?M respectively. Conversely, the enzyme activity was increased by diflofenac sodium. In addition, thiocolchicoside has not any affect on hCA I and hCA II. The effect of these drugs on erythrocyte hCA I and hCA II were consistent with the inhibition of recombinant enzymes. PMID:21534860

  12. Superior analgesic effect of an active distraction versus pleasant unfamiliar sounds and music: the influence of emotion and cognitive style.

    Science.gov (United States)

    Villarreal, Eduardo A Garza; Brattico, Elvira; Vase, Lene; Østergaard, Leif; Vuust, Peter

    2012-01-01

    Listening to music has been found to reduce acute and chronic pain. The underlying mechanisms are poorly understood; however, emotion and cognitive mechanisms have been suggested to influence the analgesic effect of music. In this study we investigated the influence of familiarity, emotional and cognitive features, and cognitive style on music-induced analgesia. Forty-eight healthy participants were divided into three groups (empathizers, systemizers and balanced) and received acute pain induced by heat while listening to different sounds. Participants listened to unfamiliar Mozart music rated with high valence and low arousal, unfamiliar environmental sounds with similar valence and arousal as the music, an active distraction task (mental arithmetic) and a control, and rated the pain. Data showed that the active distraction led to significantly less pain than did the music or sounds. Both unfamiliar music and sounds reduced pain significantly when compared to the control condition; however, music was no more effective than sound to reduce pain. Furthermore, we found correlations between pain and emotion ratings. Finally, systemizers reported less pain during the mental arithmetic compared with the other two groups. These findings suggest that familiarity may be key in the influence of the cognitive and emotional mechanisms of music-induced analgesia, and that cognitive styles may influence pain perception. PMID:22242169

  13. Analgesic properties of dexketoprofen trometamol.

    Science.gov (United States)

    Walczak, Jean-Sébastien

    2011-09-01

    SUMMARY Dexketoprofen trometamol is the dextrorotary enantiomer of the NSAID ketoprofen formulated as a tromethamine salt. The purpose of administering 50% of the racemic mixture is to keep the same analgesic and anti-inflammatory effect while reducing the adverse events due to both enantiomers. This article describes the pharmacological properties and evaluates the analgesic effects of dexketoprofen trometamol reported in acute and chronic pain conditions. The main conclusions are that dexketoprofen trometamol appears as effective as the double dose of the racemic drug. However, the reduction of adverse effects still has to be demonstrated. In addition, the formulation as tromethamine salt appears beneficial regarding fast onset of analgesia in acute pain conditions. PMID:24645708

  14. The effects of 2 ?g and 4 ?g doses of dexmedetomidine in combination with intrathecal hyperbaric bupivacaine on spinal anesthesia and its postoperative analgesic characteristics

    Science.gov (United States)

    Yekta?, Abdulkadir; Belli, Enver

    2014-01-01

    OBJECTIVE: To compare the postoperative analgesic characteristics and side effects of two different doses of intrathecal dexmedetomidine in combination with hyperbaric bupivacaine, and to evaluate the effects of these combinations on spinal anesthesia. METHODS: After obtaining approval from the local ethics committee, 60 male patients who were undergoing inguinal surgery and were classified as American Society of Anesthesiologists physical status class I were included in the study. The present study was conducted in 2003 in a military hospital with a capacity of 100 beds. The patients were randomly assigned to three groups of 20 patients: group 1, 0.5 mL saline added to 3 mL (15 mg) hyperbaric bupivacaine; and groups 2 and 3, 2 ?g dexme-detomidine and 4 ?g dexmedetomidine added to 3 mL (15 mg) hyperbaric bupivacaine, respectively. Medications were administered by intrathecal injection in a total volume of 3.5 mL. The postoperative analgesic characteristics, effects on spinal anesthesia and side effects were recorded. RESULTS: Demographic characteristics were similar among the groups. The mean (± SD) time to onset of pain was 220.75±112.7 min in group 1, 371.5±223.5 min in group 2 and 1042.50±366.78 min in group 3. Time to first pain sensation in group 3 was significantly longer than that in groups 1 and 2 (P<0.001). CONCLUSION: Two different doses of dexmedetomidine, an ?2-adrenoceptor agonist with analgesic effects, resulted in an increased duration of analgesia and efficacy, decreased postoperative analgesic use and was associated with no notable adverse effects. PMID:24527467

  15. Anti-Inflammatory and Analgesic Activities of a Novel Biflavonoid from Shells of Camellia oleifera

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    Yong Ye

    2012-09-01

    Full Text Available Shells are by-products of oil production from Camellia oleifera which have not been harnessed effectively. The purpose of this research is to isolate flavonoid from shells of Camellia oleifera and evaluate its anti-inflammatory and analgesic effects. The flavonoid was identified as bimolecular kaempferol structure by UV, MS, 1H NMR and 13C NMR spectra, which is a new biflavonoid and first found in Camellia oleifera. It showed dose-dependent anti-inflammatory activity by carrageenin-induced paw oedema in rats and croton oil induced ear inflammation in mice, and analgesic activity by hot plate test and acetic acid induced writhing. The mechanism of anti-inflammation of biflavonoid is related to both bradykinin and prostaglandins synthesis inhibition. The biflavonoid showed both central and peripheral analgesic effects different from aspirin, inhibition of the synthesis or action of prostaglandins may contribute to analgesic effect of biflavonoid. The biflavonoid significantly decreased malonaldehyde (MDA and increased superoxidase dismutase (SOD and Glutathione peroxidase (GSH-Px activity in serum (p < 0.01, revealed strong free radical scavenging activity in vivo. It indicates the biflavonoid can control inflammation and pain by eliminating free radical so as to inhibit the mediators and decrease the prostaglandins. The biflavonoid can be used as a prospective medicine for inflammation and pain.

  16. Antipyretic and analgesic effects of zaltoprofen for the treatment of acute upper respiratory tract infection: verification of a noninferiority hypothesis using loxoprofen sodium.

    Science.gov (United States)

    Azuma, Arata; Kudoh, Shoji; Nakashima, Mitsuyoshi; Nagatake, Tsuyoshi

    2011-01-01

    A multicenter, placebo-controlled, double-dummy, randomized, parallel-group, double-blind study was conducted to verify the hypothesis of noninferiority for single-dose administration of zaltoprofen 160 mg, a nonsteroidal anti-inflammatory drug, compared with loxoprofen sodium 60 mg (loxoprofen), in terms of antipyretic and analgesic effects in patients with acute upper respiratory tract infection. The eligible 330 patients were assigned to one of 3 groups: zaltoprofen 160 mg, loxoprofen 60 mg and placebo. The analysis set consisted of 322 patients. Antipyretic effects were assessed by measuring body temperature, and analgesic effects were evaluated using a visual analog scale (VAS) for 4 h under the control of study staff. A detection kit for influenza virus A and B antigens was used to determine the presence of influenza virus infection. Compared with immediately before administration and with the placebo group, significant decreases in body temperature and summary VAS pain scores were noted in both the zaltoprofen and loxoprofen groups at 4 h after drug administration. Based on the degree of decrease in body temperature and the summary VAS pain scores up to 4 h after administration, noninferiority in terms of antipyretic and analgesic effects of zaltoprofen compared with those of loxoprofen was confirmed after single administration. Similar antipyretic and analgesic effects were also confirmed in influenza virus antigen-positive patients (73 patients). No clinical concerns were identified regarding safety. Zaltoprofen and loxoprofen are confirmed to be safe and useful for patients with acute upper respiratory tract infection, including those with influenza infection. PMID:21430410

  17. Comparison of the Analgesic Effect of Diclofenac Sodium-Eudragit® RS100 Solid Dispersion and Nanoparticles Using Formalin Test in the Rats

    Science.gov (United States)

    Adibkia, Khosro; Mohajjel Nayebi, Alireza; Barzegar-Jalali, Mohammad; Hosseinzadeh, Siavash; Ghanbarzadeh, Saeed; Shiva, Afshin

    2015-01-01

    Purpose: In this study the intensity and duration of analgesic effect of diclofenac Na - Eudragit® RS100 solid dispersion and nanoparticles were evaluated by using formalin test in the rats. Methods: The animals received different formulations of diclofenac Na and subsequently 50 ?l of formalin solution (2.5%) was injected subcutaneously in the right paws after 1 h, 2 h and 3 h. The paw licking behavior was then evaluated in two phases. A dose of 20 mg/kg of pure diclofenac Na powder was determined as effective dose. Results: In the first phase, in term of reduced paw licking time, no significant differences were found in any of the groups compared to the control group. However, in the second phase, the animals which received pure drug powder and the physical mixture of diclofenac Na with Eudragit® RS100 showed significant differences at the first and second hours. In the animals received the nanoparticles and solid dispersion, significant differences were observed in the third hour compared to the control group. Conclusion: The analgesic effect of diclofenac Na could be improved by formulating its nanoparticles and solid dispersion with Eudragit® RS100. However, the nanoparticles revealed significantly higher analgesic effect than solid dispersion.

  18. Analgesic effects of methanolic extracts of the leaf or root of Moringa oleifera on complete Freund’s adjuvant-induced arthritis in rats

    OpenAIRE

    Homa Manaheji

    2011-01-01

    Objective: Moringa oleifera (family Moringaceae) has been widely used in African folk medicine, and researchers have recently revealed its anti-inflammatory effects in human. This study aimed to evaluate the analgesic properties of methanolic extracts of M. oleifera in complete Freund’s adjuvant (CFA)-induced arthritis in rats. Methods: Adult male Wistar rats, weighing 200 to 220 g, were used in this study. Adjuvant arthritis was induced on day 0 by a single subcutaneous injection of CFA. T...

  19. Effects of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood

    DEFF Research Database (Denmark)

    SØrensen, S F; Dirksen, Asger

    1979-01-01

    The in vitro and in vivo effects of therapeutical doses of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood were investigated with the following results: Acetylsalicylic acid caused both in vitro and in vivo a reduction of complement receptor bearing lymphocytes and of lymphocytes identified with fluorescent rabbit antibody to human Ig (polyvalent) and to human IgG. Sheep red blood cell receptor bearing lymphocytes, and lymphocytes identified with antibody to human IgM and IgD were unaffected by acetylsalicylic acid.

  20. Pharmacokinetics and analgesic effect of ropivacaine during continuous epidural infusion for postoperative pain relief.

    DEFF Research Database (Denmark)

    Erichsen, C J; Sjövall, J

    1996-01-01

    BACKGROUND: The pharmacokinetics and clinical efficacy of ropivacaine (2.5 mg/ml) during a 24-h continuous epidural infusion for postoperative pain relief in 20 patients scheduled for abdominal hysterectomy were characterized using an open-label, increasing-dose design. METHODS: Through an epidural catheter inserted at T10-T12, a test dose of 7.5 mg ropivacaine was given 3 min before a bolus dose of 42.5 mg and immediately followed by a 24-h continuous epidural infusion with either 10 or 20 mg/h. Peripheral venous plasma samples were collected up to 48 h after infusion, and urinary excretion was followed up to the end of infusion. Postoperative pain at rest, on coughing, and at mobilization was assessed by means of a visual analog scale 2,4,6,8,12, and 24 h after the end of surgery. Sensory (pinprick) and motor block (modified Bromage scale) were assessed at the same intervals. RESULTS: The total plasma concentrations of ropivacaine increased markedly and consistently during the 24-h epidural infusion, in contrast to stable unbound concentrations. Both total and unbound plasma concentrations at the end of infusion were proportional to the total dose, although only the latter was proportional to the infusion rate. The total and unbound plasma clearance was independent of dose. Total mean clearance decreased on average by 21% (P < 0.001) during the last 12 h of epidural infusion, i.e., from 539 +/- 191 ml/min to 418 +/- 138 ml/min, indicating time-dependent kinetics. The unbound clearance also varied between estimates after 8 h of infusion and the end of treatment, i.e., a 5.3% decrease from 10.4 +/- 5.3 l/min to 9.5 +/- 3.9 l/min (P < 0.05). The unbound fraction of ropivacaine in plasma decreased during treatment, and this was related to the increase in alpha1-acid glycoprotein concentration. Pain was generally well controlled, and median visual analog scale scores during mobilization were less than 30 mm in patients receiving ropivacaine at 20 mg/h. CONCLUSIONS: The pharmacokinetics of ropivacaine were independent of dose, but total clearance decreased with time over 24 h. The consistent increase in total plasma concentration during the postoperative epidural infusion contrasted to much less variation in the unbound plasma concentrations of ropivacaine.

  1. Comparison the Analgesic Effects of Single Dose Administration of Tramadol or Piroxicam on Postoperative Pain after Cesarean Delivery

    Directory of Open Access Journals (Sweden)

    Amir Farshchi

    2010-05-01

    Full Text Available "nA multimodal approach to postcesarean pain management may enhance analgesia and reduce side effects after surgery. We investigated postoperative pain in a double-blinded, randomized, single-dose comparison of the monoaminergic and µ-opioid agonist tramadol, 100 mg (Group T and piroxicam 20 mg (Group P given IM alone- single dose in 150 patients who had elective cesarean delivery. All patients were assessed at 0, 6, 12 and 24 hours post operation for pain degree (by Visual Analogue Score: VAS 1-10, nausea and vomiting. Pain degree was classified as: Painless: 0, Mild: 1-4, Moderate: 5-8, Severe: 9-10. There was no significant difference between the efficacy of tramadol and piroxicam injections (P>0.05. Pain intensity decreased markedly over time in both groups. Mean±SEM pain degrees were as follows: P=7.7±0.5, T=8.2±0.8 after 0 hours; P=5.4±0.6, T=6.1±0.5 after 6 hours; P=3.3±0.4, T=3.4±0.7 after 12 hours; P=1.1±0.4, T=1.3±0.5 after 24 hours of surgery. Side effects were similarly minimal with all treatments. It might be concluded that i.m. injections of 20 mg piroxicam (single dose therapy could relieve postoperative pain after cesarean section as well as tramadol and it could reduce opioid analgesic requirements with less adverse side effects during the first postoperative 24 h.

  2. Gabapentina en dolor raquídeo crónico: Valoración de su eficacia analgésica Gabapentin in chronic rachidian pain: Assessment of its analgesic effectiveness

    Directory of Open Access Journals (Sweden)

    J. Cartagena

    2005-05-01

    Full Text Available Objetivos: Valorar la eficacia analgésica de la gabapentina (GBP en pacientes con dolor raquídeo crónico (DRC, que no han respondido adecuadamente a los tratamientos farmacológicos habitualmente empleados (antiinflamatorios no esteroideos -AINE-, opioides menores o mayores, relajantes musculares, antidepresivos, etc.. Material y métodos: Se han estudiado de modo prospectivo y aleatorio 41 pacientes afectos de DRC (cervical, dorsal y/o lumbar, independientemente de su etiología, con o sin radiculopatía asociada, que no hubieran respondido previamente a los tratamientos farmacológicos habituales. No obstante, durante el estudio, por razones éticas y, en un intento de obtener la mayor eficacia analgésica posible con tales fármacos, se permitió el empleo de los mismos, aunque realizando, previamente, un reajuste de las dosis por parte de un especialista de la Unidad de Dolor. Si tras este ajuste no se obtenía una respuesta adecuada, se iniciaba el tratamiento con gabapentina de manera gradual hasta alcanzar una dosis de 300 mg cada 8 h; dicha dosis se fue incrementando hasta obtener una respuesta terapéutica (con un máximo de 2400 mg.día-1 o la aparición de efectos secundarios intolerables. A partir del inicio del tratamiento con gabapentina se realizó un seguimiento durante tres meses en el que se valoraban características del dolor, localización, irradiación, y se cuantificaba mediante una escala analógica visual -EVA- (100 mm y test de Lattinen. Asimismo, se evaluó la calidad del sueño mediante una EVA modificada. Se recogieron también la dosis utilizadas para el control del dolor así como los efectos secundarios aparecidos y las causas de abandono. Resultados: Desde el primer mes de tratamiento y ya con dosis bajas de gabapentina se observó una mejoría significativa en los valores de la EVA del dolor, test Lattinen y calidad de sueño, incluso en aquellos pacientes en los que no existía radiculopatía asociada o dolor de características neuropáticas claras. Dicha mejora en los parámetros mencionados fue progresiva incluso sin necesidad de seguir aumentando la dosis de gabapentina. La tolerancia fue muy buena no siendo preciso interrumpir en ningún caso el tratamiento por los efectos secundarios, los cuales han sido en general leves y autolimitados. Conclusión: La gabapentina, como coadyuvante de la terapia habitual, es un fármaco eficaz en pacientes con dolor crónico raquídeo, no precisando dosis elevadas y presentando buena tolerancia con una baja incidencia de efectos secundarios.Objectives: To assess the analgesic effectiveness of gabapentin (GBP in patients with chronic rachidian pain (CRP refractory to standard pharmacological therapies (non-steroid anti-inflammatory drugs, NSAIDs, minor and major opiates, muscular relaxants, antidepressants, etc.. Material and methods: Forty one patients with CRP (cervical, dorsal and lumbar pain refractory to prior standard drug therapies were prospectively and randomly studied, regardless their etiology, with or without associated radiculopathy. However, during the study, due to ethical reasons and in order to obtain the greatest analgesic effectiveness as possible with such drugs, their use was allowed, although with a prior dose titration performed by the Pain Unit specialist. If the response was inadequate even after dose titration, treatment with gabapentin was gradually introduced up to a dose of 300 mg each 8 hours; such dose was increased until obtaining a therapeutic response (up to a maximum of 2400 mg.day-1 or causing intolerable side effects. From the beginning of the treatment with gabapentin, a three-month follow-up was conducted in which pain features, location and irradiation were assessed and quantified using a visual analogical scale (VAS (100 mm and the Lattinen's test. Quality of sleep was also determined using a modified VAS. Doses required to relief pain, as well as side effects reported and dropout causes were also recorded. Results: Since the first month of therapy and with low doses of gabapentin, a

  3. Gabapentina en dolor raquídeo crónico: Valoración de su eficacia analgésica / Gabapentin in chronic rachidian pain: Assessment of its analgesic effectiveness

    Scientific Electronic Library Online (English)

    J., Cartagena; J. P., Vicente; E., Borrás; J. A., Castillo; G., Motos.

    2005-05-01

    Full Text Available SciELO Spain | Language: Spanish Abstract in spanish Objetivos: Valorar la eficacia analgésica de la gabapentina (GBP) en pacientes con dolor raquídeo crónico (DRC), que no han respondido adecuadamente a los tratamientos farmacológicos habitualmente empleados (antiinflamatorios no esteroideos -AINE-, opioides menores o mayores, relajantes musculares, [...] antidepresivos, etc.). Material y métodos: Se han estudiado de modo prospectivo y aleatorio 41 pacientes afectos de DRC (cervical, dorsal y/o lumbar), independientemente de su etiología, con o sin radiculopatía asociada, que no hubieran respondido previamente a los tratamientos farmacológicos habituales. No obstante, durante el estudio, por razones éticas y, en un intento de obtener la mayor eficacia analgésica posible con tales fármacos, se permitió el empleo de los mismos, aunque realizando, previamente, un reajuste de las dosis por parte de un especialista de la Unidad de Dolor. Si tras este ajuste no se obtenía una respuesta adecuada, se iniciaba el tratamiento con gabapentina de manera gradual hasta alcanzar una dosis de 300 mg cada 8 h; dicha dosis se fue incrementando hasta obtener una respuesta terapéutica (con un máximo de 2400 mg.día-1) o la aparición de efectos secundarios intolerables. A partir del inicio del tratamiento con gabapentina se realizó un seguimiento durante tres meses en el que se valoraban características del dolor, localización, irradiación, y se cuantificaba mediante una escala analógica visual -EVA- (100 mm) y test de Lattinen. Asimismo, se evaluó la calidad del sueño mediante una EVA modificada. Se recogieron también la dosis utilizadas para el control del dolor así como los efectos secundarios aparecidos y las causas de abandono. Resultados: Desde el primer mes de tratamiento y ya con dosis bajas de gabapentina se observó una mejoría significativa en los valores de la EVA del dolor, test Lattinen y calidad de sueño, incluso en aquellos pacientes en los que no existía radiculopatía asociada o dolor de características neuropáticas claras. Dicha mejora en los parámetros mencionados fue progresiva incluso sin necesidad de seguir aumentando la dosis de gabapentina. La tolerancia fue muy buena no siendo preciso interrumpir en ningún caso el tratamiento por los efectos secundarios, los cuales han sido en general leves y autolimitados. Conclusión: La gabapentina, como coadyuvante de la terapia habitual, es un fármaco eficaz en pacientes con dolor crónico raquídeo, no precisando dosis elevadas y presentando buena tolerancia con una baja incidencia de efectos secundarios. Abstract in english Objectives: To assess the analgesic effectiveness of gabapentin (GBP) in patients with chronic rachidian pain (CRP) refractory to standard pharmacological therapies (non-steroid anti-inflammatory drugs, NSAIDs, minor and major opiates, muscular relaxants, antidepressants, etc.). Material and methods [...] : Forty one patients with CRP (cervical, dorsal and lumbar pain) refractory to prior standard drug therapies were prospectively and randomly studied, regardless their etiology, with or without associated radiculopathy. However, during the study, due to ethical reasons and in order to obtain the greatest analgesic effectiveness as possible with such drugs, their use was allowed, although with a prior dose titration performed by the Pain Unit specialist. If the response was inadequate even after dose titration, treatment with gabapentin was gradually introduced up to a dose of 300 mg each 8 hours; such dose was increased until obtaining a therapeutic response (up to a maximum of 2400 mg.day-1) or causing intolerable side effects. From the beginning of the treatment with gabapentin, a three-month follow-up was conducted in which pain features, location and irradiation were assessed and quantified using a visual analogical scale (VAS) (100 mm) and the Lattinen's test. Quality of sleep was also determined using a modified VAS. Doses required to relief pain, as well as side effects reported and dropout cause

  4. Evaluation of the clinical and analgesic effects of subarachnoid ketamine-lidocaine administration in goats undergoing mastectomy

    Directory of Open Access Journals (Sweden)

    Daradka M

    2014-05-01

    Full Text Available Mousa Daradka, Zuhair Bani IsmailDepartment of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, JordanAbstract: Twenty adult female goats affected with chronic mastitis were subjected to mastectomy or hemimastectomy under subarachnoid regional analgesia using a ketamine-lidocaine combination. Ketamine at 1.5 mg/kg and lidocaine hydrochloride at 1.25 mg/kg were administered intrathecally at the lumbosacral intervertebral space. Goats were then subjected to a 120-minute observation period for systemic or neurotoxic symptoms such as agitation, restlessness, hind limb paralysis, or seizures. In addition, analgesia of the caudal abdominal region and signs of systemic sedation were scored on a scale of 0–3. Heart rate, respiratory rate, and rectal temperature were also recorded prior to (baseline values and at 5, 15, 30, 60, 90, and 120 minutes after administration. Mastectomy or hemimastectomy operation was carried out after full assurance of the analgesic effect on the udder and caudal abdominal region. Time of onset of surgical analgesia (score 3 was achieved at 15 minutes and lasted for 60 minutes. Maximal sedation score was recorded at 15 minutes and lasted for 60 minutes, then decreased thereafter, with the lowest sedation score recorded at 120 minutes. There was a significant (P<0.05 rise in heart rate at some point between 5–90 minutes, while the respiratory rate and rectal temperature did not change significantly from baseline values. Postoperatively, animals did not show any signs of pain or discomfort. Follow-up on the operated goats showed that all wounds were fully healed without any significant complications. In goats, intrathecal administration of ketamine-lidocaine combination resulted in a safe and effective analgesia of the caudal abdominal and udder region sufficient to perform mastectomy or hemimastectomy.Keywords: analgesia, sedation, ruminants, mastectomy

  5. The sedative and analgesic effects of detomidine-butorphanol and detomidine alone in donkeys

    OpenAIRE

    Joubert, K. E.; Briggs, P.; Gerber, D.; Gottschalk, R. G.

    2012-01-01

    Butorphanol and detomidine constitute an effective combination for sedation and analgesia in horses. This trial was undertaken to assess the effectiveness of this combination in donkeys. The detomidine and butorphanol were given intravenously one after the other. A dose of 10 mg/kg of detomidine and 25 mg/kg of butorphanol was used. Sedation is easily extended by additional doses of butorphanol. The average dose of detomidine was 11.24 mg/kg and that of butorphanol was 28.0 mg/kg. Four donkey...

  6. Comparing the painlessness effects of spinal (sufentanil and epidural(bupivacaine plus lidocaine analgesic methods in labour and delivery

    Directory of Open Access Journals (Sweden)

    A. Shafiee

    2006-01-01

    Full Text Available Background and purpose: This study was designed in order to compare the effects of spinal and epidural analgesia on labour and also several maternal and fetal factors in vaginal delivery.Materials and Methods: The study was a randomized clinical trail and participatnts were 120 gravid 1 and gravid 2 women in the active phase of delivery, admitted to the labour room of Fatemieh Hospital in Hamedan in 1381-1382.Sixty patients were randomly divided into two groups of 30, analgesia was induced by single spinal sufentanil injection in one group and, bupivacaine plus lidocaine injection in the other group.Maternal vital signs and pain score were recorded (VAS at 1, 5, 15 and 30 minutes after administration of analgesia and every 30 minutes thereafter. Fetal heart rate every 15 minutes, vaginal examination every hour, urinary output every 4 hours after delivery and the incidence of headache and back pain, one week after delivery were the variables under study.Results: Both groups were matched regarding demographic, gravida and Parity factors. There was no significant difference between groups regarding pain score, (based on VAS,duration of the first and second delivery phase, the incidence of fetal distress, meconium excretion, apgar scores at 1 and 5 minutes after delivery, abnormal laboar, operative or assisted delivery. Average analgesic duration was longer in spinal analgesia than single epidural injection analgesia.Conclusion: Considering the difficulty of the technique, the need for anaestheticianHs supervision and injection repeatition in epidural analgesia, it seems that spinal analgesia is a suitable replacement which is more practical, less expensive, easy to perform and induces a desirable analgesia.

  7. Effectiveness of the association between carbamazepine and peripheral analgesic block with ropivacaine for the treatment of trigeminal neuralgia

    OpenAIRE

    Laurinda Lemos; Ramalho Fontes; Sara Flores; et al.

    2010-01-01

    Laurinda Lemos1,2, Ramalho Fontes3, Sara Flores2, Pedro Oliveira4, Armando Almeida11Life and Health Sciences Research Institute (ICVS), School of Health Sciences, Campus de Gualtar, University of Minho, Braga, Portugal; 2Hospital Center of Alto Ave, Unit of Fafe, Fafe, Portugal; 3Department of Neurology, Hospital São Marcos, Braga, Portugal; 4Products and Systems Engineering, Campus de Azurém, University of Minho, Guimarães, PortugalAbstract: Treatment of trig...

  8. Study of analgesic activity of ethanol extract of Phlogacanthus thyrsiflorus on experimental animal models

    Directory of Open Access Journals (Sweden)

    Apurba Mukherjee, Meghali Chaliha and Swarnamoni Das

    2009-12-01

    Full Text Available The aim of the study was to evaluate the central and peripheral analgesic action of Phlogacanthus thyrsiflorus in experimental animal models. The extract was prepared by percolation method and acute oral toxicity testing was performed as per OECD guidelines. Analgesic activity was assessed by tail flick method (for central action and glacial acetic acid-induced writhing test (for peripheral action. Leaves extract (500 mg/kg, p.o. and aspirin (100 mg/kg showed significant peripheral analgesic activity (p<0.05. Leaves extract (500 mg/kg, p.o. and pethidine (50 mg/kg, i.p. also showed significant central analgesic activity (p<0.05. Naloxone (1 mg/kg, s.c. was used to find the mechanism of central analgesic action. Some partial agonistic activity for the opioid receptors seems to be probable mechanism of action.

  9. PUTATIVE PHYSIOLOGICAL MECHANISMS UNDERLYING ANALGESIC EFFECTS OF TRANSCRANIAL DIRECT CURRENT STIMULATION (TDCS)

    OpenAIRE

    HelenaKnotkova; MichaelA.Nitsche; RicardoACruciani

    2013-01-01

    Transcranial direct current stimulation (tDCS) is a non-invasive neuromodulation technique that induces changes in excitability, and activation of brain neurons and neuronal circuits. It has been observed that beyond regional effects under the electrodes, tDCS also alters activity of remote interconnected cortical and subcortical areas. This makes the tDCS stimulation technique potentially promising for modulation of pain syndromes. Indeed, utilizing specific montages, tDCS resulted in ana...

  10. The sedative and analgesic effects of detomidine-butorphanol and detomidine alone in donkeys

    Directory of Open Access Journals (Sweden)

    K.E. Joubert

    2012-07-01

    Full Text Available Butorphanol and detomidine constitute an effective combination for sedation and analgesia in horses. This trial was undertaken to assess the effectiveness of this combination in donkeys. The detomidine and butorphanol were given intravenously one after the other. A dose of 10 mg/kg of detomidine and 25 mg/kg of butorphanol was used. Sedation is easily extended by additional doses of butorphanol. The average dose of detomidine was 11.24 mg/kg and that of butorphanol was 28.0 mg/kg. Four donkeys in the detomidine group required additional sedation and analgesia. Detomidine alone did not totally eliminate coronary band pain. Heart rates dropped significantly in the first minute after the injection of the combination. One donkey developed an atrioventricular block, while another developed a sino-atrial block. Four donkeys developed a Cheyne-Stokes respiratory pattern. The combination of detomidine and butorphanol is an effective combination for sedation and analgesia of donkeys for standing procedures.

  11. Morphine-6-glucuronide: analgesic effects and receptor binding profile in rats

    Energy Technology Data Exchange (ETDEWEB)

    Abbott, F.V.; Palmour, R.M.

    1988-01-01

    The antinociceptive effects of morphine-6-glucuronide (M6G) were examined in two animal models of pain, the tail immersion test (reflex withdrawal to noxious heat) and the formalin test (behavioral response to minor tissue injury). In the tail immersion test, M6G produced and increase in withdrawal latency that rose rapidly between 0.01 and 0.025 ug ICV or 1 and 2 mg/kg SC. A further increase occurred at doses greater than 0.2 ug ICV or 4 mg/kg SC and was associated with marked catelepsy and cyanosis. Naloxone, 0.1 mg/kg SC, shifted the lower component of the dose-effect relation by a factor of 24. In the formalin test, 0.01 ug M6G ICV produced hyperalgesia, while between 0.05 and 0.2 ug ICV, antinociception increased rapidly without toxicity. The dose effect relations for hyperalgesia and antinociception were shifted to the right by factors of 20- and 3-fold, respectively. By comparison, ICV morphine was 60 (formalin test) to 145-200 (tail immersion test) times less potent than M6G. At sub-nanomolar concentrations, M6G enhanced the binding of (/sup 3/H)-etorphine, (/sup 3/H)-dihydromorphine and (/sup 3/H)-naloxone to rat brain membrane receptors by 20-40%. At higher concentrations, M6G displaced each ligand from binding sites, with K/sub i/ values of about 30 nM, as compared to morphine K/sub i/ values of about 3 nM.

  12. Gabapentin Increases Analgesic Effect of Chronic Use of Morphine while Decreases Withdrawal Signs

    OpenAIRE

    Manzumeh-Shamsi Meimandi; Mina-Mobasher; GholamReza-Sepehri; Ashrafganjooei Narges

    2005-01-01

    This study was performed to evaluate the role of gabapentin co-administration in morphine antinociception and withdrawal effect. Four groups of male rats were examined for latency time using tail flick test; control, morphine (M), gabapentin (GB) and gabapentin-morphine (GB-M) treated groups. Rats received morphine (10 mg kg < SUP>-1 < /SUP>, s.c.) or gabapentin (75 mg kg < SUP>-1 < /SUP>, i.p.) or both of them twice a day for 9 days. Control rats received normal ...

  13. NATURAL AND PARTIALLY SYNTETIC ANALGESICS

    Directory of Open Access Journals (Sweden)

    Stevan Glogovac

    2005-12-01

    Full Text Available Humans have a long hystory of stimulating and mind-altering substances use. Depressive drugs, including morphine and other narcotics, barbiturates and ethanol, are strongly addictive for susceptible individuals. The phenomenon is most striking in the case of opiates. Morphine is an alkaloid of opium. Named after the Roman god of dreams, Morpheus, the compound has potent analgesic properties toward all types of pain. By supstitution of two hydroxylic groups of morphine many natural and semysyntetic derivatives with different pharmacological activity and analgesic action are obtained. Determinations and quantifications of narcotic analgesics in drug addicts are important in forensic medicine and clinical toxicology. With development of highly sensitive chromatography technique (HPLC-GC, GH-MS, more and more substances are determined, including opioid drugs: morphine, codeine, dyhydrocodeine, and heroin and 6-monoacetyl morphine. Hair analysys by HPLC/MS spectroscopy is an effective forensic tool for determining the use of abused drugs. The “fingerprint” for heroin in the mixture with the other substances(1-10 components is determined by 1D-TOCSY NMR.

  14. Comparison of Postoperative Analgesic Effects of Thoracic Epidural Morphine and Fentanyl

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    Gönül Sa??ro?lu

    2011-11-01

    Full Text Available Objective: In our study, we aimed to compare epidural morphine and fentanyl analgesia and the side effects in post-thoracotomy pain management. Material and Methods: Forty patients, planned for elective thoracotomy were included. Bupivacain- morphine was administered through an epidural catheter to the patients in Group-M while bupivacain-fentanyl was given in Group-F. Pain assessment was carried out with the Visual Analogue Scale (VAS and VAS-I and VAS-II were assessed in 0, 4, 16 and 24th hour in the postoperative unit. Adverse effects were recorded after the 24th hour. Statistical analyses were performed by using Two-sample independent-t test, Mann Whitney-U test, Wilcoxon-signed ranks test and Pearson chi-squared tests. Results: Although, the VAS-I and VAS-II scores were lower in Group-M than Group-F, the difference was not significant statistically (p>0.05. When other hours were compared with initial states, beginning from the 4th hour, in both groups there was a statistically significant drop in VAS-I and VAS-II scores at all times (p<0.001. Comparing the complications between the groups, in Group-M nausea-vomiting (p<0.015 and bradycardia (p<0.012 were found significantly more frequently than in Group-F. Conclusion: We concluded that, in pain management after thoracic surgery, either morphine or fentanyl may be chosen in thoracal epidural analgesia but, especially in the early postoperative hours, close follow-up is necessary due to the risk of bradycardia development.

  15. COMPARATIVE EFFECTS OF DETOMIDINE AND XYLAZINE AS SEDATIVE AND ANALGESIC AGENTS IN SMALL RUMINANTS

    Directory of Open Access Journals (Sweden)

    M. A. Khan, M. Ashraf, K. Pervez, H. B. Rashid, A. K. Mahmood and M. Chaudhry1

    2004-04-01

    Full Text Available The study was carried out on 60 healthy rams and male goats presented for castration in the Surgery Clinics, Department of Clinical Medicine and Surgery, University of Veterinary and Animal Sciences, Lahore. The weight of the animals ranged between 25 and 50 kg and ages between 3 and 6 months. The animals were divided into three groups A, B and C, with 20 animals in each group. In group A, castration was performed under detomidine sedation injected at a dose rate of 50 ?g/kg body weight intramuscularly. In group B, xylazine was administered at a dose rate of 200 ?g/kg body weight intramuscularly. In group C, castration was performed without the use of any sedative agent. However, animals of group C were given normal saline (placebo. Before surgical manipulation, physical examination of each animal was conducted to ascertain the normal health status. From the study it was concluded that detomidine and xylazine produced similar sedative effects but the analgesia was considerably better with the former.

  16. Developmental effects of propyphenazone in analgesic and antipyretic combination with caffeine or paracetamol.

    Science.gov (United States)

    Burdan, F

    2004-05-01

    The aim of the study was to determine the influence of an over-the-counter (OTC) mixture of propyphenazone with caffeine or paracetamol on prenatal development. Propyphenazone:caffeine and propyphenazone:paracetamol mixtures were prepared with constant 3:1 and 3:5 ratios, respectively. Three dose levels of each of the mixtures were administered separately in Tween-80 water suspension once a day to pregnant Wistar rats on gestation days 8-14. The low dose was similar to the OTC preparations, 2.1 mg/kg of propyphenazone, 0.7 mg/kg of caffeine or 3.5 mg/kg of paracetamol. The middle dose was 21.0, 7.0 or 35.0 mg/kg, and the highest 210.0, 70.0 or 350.0 mg/kg for propyphenazone, caffeine or paracetamol, respectively. On day 21 of gestation the fetuses were delivered by hysterectomy. Dead or live fetuses, resorptions and the number of implantation sites were counted. Live fetuses were examined for external, visceral and skeletal malformation. Postimplantation mortality was calculated. Dose-dependent effects in the middle and high dose groups on fetal body weight/length and placental weight were found. No increase in external or internal congenital anomalies was found in any of the mixture-exposed groups. Prenatal coadministration of propyphenazone with caffeine or paracetamol caused intrauterine growth retardation but did not increase external or internal congenital anomalies. The risk of midline defects (umbilical hernia and gastroschisis) is discussed. PMID:15222401

  17. Effects of therapeutic irradiation on peripheral blood lymphocytes

    International Nuclear Information System (INIS)

    Effects of therapeutic irradiation on peripheral blood lymphocytes in 11 cases of breast cancer and 10 cases of uterine cancer were examined immediately after, 6 months after and 2 years after irradiation. The absolute granulocyte count immediately after irradiation increased in over a half of all cases though it decreased markedly in a few cases, and the mean values of absolute granulocyte count after irradiation were always above the mean value before irradiation (P > 0.05). In contrast to the changes of granulocyte count, the absolute lymphocyte count in all cases decreased extremely immediately after irradiation (P 0.05) but increased 2 years after irradiation to exceed the value before irradiation (P 0.05) and decreased 2 years after irradiation (P > 0.05). (author)

  18. Effects of Neutron Skin Thickness in Peripheral Nuclear Reactions

    International Nuclear Information System (INIS)

    Effects of neutron skin thickness in peripheral nuclear collisions are investigated using the statistical abrasion ablation (SAA) model. The reaction cross section, neutron (proton) removal cross section, one-neutron (proton) removal cross section as well as their ratios for nuclei with different neutron skin thickness are studied. It is demonstrated that there are good linear correlations between these observables and the neutron skin thickness for neutron-rich nuclei. The ratio between the (one-)neutron and proton removal cross section is found to be the most sensitive observable of neutron skin thickness. Analysis shows that the relative increase of this ratio could be used to determine the neutron skin size in neutron-rich nuclei. (nuclear physics)

  19. The effects of recombinant interleukin 2-activated natural killer cells on autologous peripheral blood hematopoietic progenitors

    OpenAIRE

    1988-01-01

    In the present study, we demonstrate that resting and rIL-2-activated NK cells had no inhibitory effects on peripheral blood-derived hematopoietic progenitor (HP) cells. Peripheral blood HP cells were similar to bone marrow progenitors in phenotype and clonogenic colony formation capabilities. Peripheral blood HP cells could be cocultured in vitro with rIL-2-activated autologous NK cells for 3 d without adverse effects on the HP cells. Acute myelogenous leukemia patients in stable remission w...

  20. The analgesic efficacy of xylazine and dipyrone in hydrogen peroxide-induced oxidative stress in chicks

    Directory of Open Access Journals (Sweden)

    Y.J. Mousa

    2012-01-01

    Full Text Available The effect of oxidative stress–induced by hydrogen peroxide (H2O2 on the analgesic effect of xylazine and dipyrone in 7-14 days old chicks was studied, compared with the control group that given plane tap water. H2O2, 0.5 % in water, induced oxidative stress in chicks by significantly lowering glutathione, rising malondialdehyde in plasma, whole brain during the day 7th, 10th, 14th of chicks old in comparison with the control group. The analgesic median effective doses (ED50 of xylazine and dipyrone in the control group were determined to be 0.79 and 65.3 mg/kg, intramuscularly (i.m., respectively whereas H2O2 treated groups decreased these values to be 0.31 and 37.2 mg/kg, i.m. by 61 and 43%, respectively. Intramuscular injection of xylazine and dipyrone at 0.5, 70 mg/kg respectively causes analgesia from electro-stimulation induced pain in 50, 66.67% respectively in control groups whereas H2O2 treated chicks increases the analgesic efficacy to be 83.33 and 83.33% respectively. Xylazine and dipyrone injection at 1 and 100 mg/kg, i.m. 15 minutes before formaldehyde injection in right planter foot of stressed chicks causes analgesia from pain induced by formaldehyde through significant increases in onset of lifting of formaldehyde injected foot, significantly decreases its lifting numbers, decreases the time elapsed of lifting of formaldehyde injected foot in comparison with the stressed control group that injected with saline in right planter foot. The data of this study indicate that H2O2-induced oxidative stress potentiate the analgesic efficacy of the central and peripheral analgesics of xylazine and dipyrone in chicks.

  1. Effects of microwave radiation on peripheral lymphocyte subpopulations in rats

    Directory of Open Access Journals (Sweden)

    Jin-ling YIN

    2011-10-01

    Full Text Available Objective To investigate the effects and mechanisms of microwave radiation on peripheral lymphocyte subpopulations in Wistar rats.Methods A total of 100 Wistar rats(180-220g were exposed to microwave with different average power densities of 5,10,30 and 60 mW/cm2,and sham exposure of 0mW/cm2 was performed in a control group at the same time.At day 1,7,14 and 28 after microwave irradiation,the changes in peripheral CD3+,CD4+,CD8+ T cells,ratio of CD4+/CD8+ and CD45RA+ B lymphocyte in rats were analyzed by flow cytometry(FCM.Results The CD3+ T cells decreased significantly in 10-30mW/cm2 groups at day 7 and in 5-30 mW/cm2 groups at day 14 after radiation as compared with control group(P < 0.05,and CD4+ T cells decreased significantly in 10mW/cm2 group at day 14 after radiation as compared with control group(P < 0.01.From day 1 to day 14 after radiation,CD8+ T cells showed a reduction in number in all irradiated groups when compared with the control,but statistical significance was only found in the 30mW/cm2 group(P < 0.05.The CD4+/CD8+ ratio increased in 5mW/cm2 group on day 1,while decreased significantly in 5-30mW/cm2 groups on day 14 after radiation as compared with control group(P < 0.05.After microwave exposure,however,CD45RA+ B cells in 30mW/cm2 group at day 1 and in 30-60mW/cm2 groups at day 14 after radiation increased significantly in a dose-dependent manner.Conclusion A definite dosage of microwave radiation,ranging from 5-60mW/cm2,may induce changes in subpopulations of peripheral lymphocytes and cause acute immune function impairment in rats.

  2. Use and abuse of over-the-counter analgesic agents.

    OpenAIRE

    Abbott, F. V.; Fraser, M. I.

    1998-01-01

    Pain and discomfort in everyday life are often treated with over-the-counter (OTC) analgesic medications. These drugs are remarkably safe, but serious side effects can occur. Up to 70% of the population in Western countries uses analgesics regularly, primarily for headaches, other specific pains and febrile illness. It is not known whether the patterns of use are consistent with good pain management practices. OTC analgesics are also widely used to treat dysphoric mood states and sleep distur...

  3. Ketorolac, an injectable nonnarcotic analgesic.

    Science.gov (United States)

    Litvak, K M; McEvoy, G K

    1990-12-01

    Clinical studies of the injectable nonsteroidal anti-inflammatory agent (NSAIA) ketorolac tromethamine are reviewed, and the chemistry, pharmacology, pharmacokinetics, drug interactions, and adverse effects of ketorolac are described. Ketorolac exhibits anti-inflammatory, analgesic, and antipyretic activity. Although the exact mechanisms of action have not been determined, its effects appear to be associated principally with the inhibition of prostaglandin synthesis. After oral, i.m., or i.v. administration, ketorolac and its metabolites are excreted mainly in urine. Ketorolac tromethamine has been used for the symptomatic relief of moderate to severe postoperative pain, including that associated with abdominal, gynecologic, oral, orthopedic, or urologic surgery. Ketorolac has also been used for the relief of acute renal colic, pain associated with trauma, and visceral pain associated with cancer. When administered i.m., ketorolac produced analgesia comparable to that of i.m. doses of meperidine, pentazocine, or morphine. The most common adverse effects associated with short-term administration are nervous system and gastrointestinal effects; these are usually mild and occur in about 39% of patients. Unlike opiate analgesics, ketorolac does not appear to cause tolerance or physical dependence in patients receiving long-term therapy. Ketorolac tromethamine has been administered concomitantly with morphine or meperidine without apparent adverse interaction. For short-term pain management, an initial i.m. ketorolac tromethamine loading dose of 30 or 60 mg is recommended. Ketorolac tromethamine appears to be as effective as morphine or meperidine for short-term management of moderate to severe postoperative pain. It lacks the respiratory depressant effects of opiate analgesics but shares the toxic potentials of other NSAIAs. PMID:2292174

  4. Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream

    Science.gov (United States)

    Abdulkarim, Muthanna F; Abdullah, Ghassan Z; Chitneni, Mallikarjun; Salman, Ibrahim M; Ameer, Omar Z; Yam, Mun F; Mahdi, Elrashid S; Sattar, Munavvar A; Basri, Mahiran; Noor, Azmin M

    2010-01-01

    Introduction During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, anti-pyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery. Methods A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20), respectively was selected as the basic composition for the production of a nanocream with ideal properties. Various nanocreams were prepared using phosphate-buffered saline as the external phase at three different pH values. The abilities of these formulae to deliver piroxicam were assessed in vitro using a Franz diffusion cell fitted with a cellulose acetate membrane and full thickness rat skin. These formulae were also evaluated in vivo by comparing their anti-inflammatory and analgesic activities with those of the currently marketed gel. Results After eight hours, nearly 100% of drug was transferred through the artificial membrane from the prepared formula F3 (phosphate-buffered saline at pH 7.4 as the external phase) and the marketed gel. The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel. Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae. Conclusion The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam. PMID:21116332

  5. Anti-inflammatory, Analgesic and Antiulcer properties of Porphyra vietnamensis

    Science.gov (United States)

    Bhatia, Saurabh; Sharma, Kiran; Sharma, Ajay; Nagpal, Kalpana; Bera, Tanmoy

    2015-01-01

    Objectives: Aim of the present work was to investigate the anti-inflammatory, analgesic and antiulcer effects of red seaweed Porphyra vietnamensis (P. vietnamenis). Materials and Methods: Aqueous (POR) and alcoholic (PE) fractions were successfully isolated from P. vietnamenis. Further biological investigations were performed using a classic test of paw edema induced by carrageenan, writhing induced by acetic acid, hot plate method and naproxen induced gastro-duodenal ulcer. Results: Among the fractions POR showed better activity. POR and PE significantly (p < 0.05) reduced carrageenan induced paw edema in a dose dependent manner. In the writhing test POR significantly (p < 0.05) reduced abdominal writhes than PE. In hot plate method POR showed better analgesic activity than PE. POR showed comparable ulcers reducing potential (p<0.01) to that of omeprazole, and has more ulcer reducing potential then PE. Conclusions: The results of this study demonstrated that P. vietnamenis aqueous fraction possesses biological activity that is close to the standards taken for the treatment of peripheral painful or/and inflammatory and ulcer conditions. PMID:25767759

  6. Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream

    Directory of Open Access Journals (Sweden)

    Muthanna F Abdulkarim

    2010-11-01

    Full Text Available Muthanna F Abdulkarim1*, Ghassan Z Abdullah1*, Mallikarjun Chitneni2, Ibrahim M Salman1, Omar Z Ameer1, Mun F Yam1,3, Elrashid S Mahdi1, Munavvar A Sattar1, Mahiran Basri4, Azmin M Noor11School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia; 2School of Pharmacy and Health Sciences, International Medical University, Kuala Lumpur, Malaysia; 3Faculty of Medicine and Health Sciences, 4Faculty of Science, Universiti Putra Malaysia, Selangor, Malaysia; *The First and Second Authors have Contributed Equally to this WorkIntroduction: During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, antipyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs-based nanocream containing piroxicam for topical delivery.Methods: A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20, respectively was selected as the basic composition for the production of a nanocream with ideal properties. Various nanocreams were prepared using phosphate-buffered saline as the external phase at three different pH values. The abilities of these formulae to deliver piroxicam were assessed in vitro using a Franz diffusion cell fitted with a cellulose acetate membrane and full thickness rat skin. These formulae were also evaluated in vivo by comparing their anti-inflammatory and analgesic activities with those of the currently marketed gel.Results: After eight hours, nearly 100% of drug was transferred through the artificial membrane from the prepared formula F3 (phosphate-buffered saline at pH 7.4 as the external phase and the marketed gel. The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel. Pharmacodynamically, nanocream formula F3 exhibited the highest anti-inflammatory and analgesic effects as compared with the other formulae.Conclusion: The nanocream containing the newly synthesized POEs was successful for transdermal delivery of piroxicam.Keywords: piroxicam, nanocream, analgesic, anti-inflammatory, skin permeation

  7. Analgesic effects of transcutaneous electrical nerve stimulation and interferential current on experimental ischemic pain models: frequencies of 50?hz and 100?hz.

    Science.gov (United States)

    Bae, Young-Hyeon; Lee, Suk Min

    2014-12-01

    [Purpose] This study compared the analgesic effects of transcutaneous electrical nerve stimulation (TENS) and interferential currents (IFC) on induced ischemic pain in healthy volunteers. [Subjects] The subjects were 36 volunteers (18 male, 18 female) without known pathology that could cause pain. Their mean age was 24.5±2.2?years. [Methods] A single-blind and parallel-group method was used. Subjects were randomly allocated to receive each 50?Hz TENS, 50?Hz IFC, 100?Hz TENS, and 100?Hz IFC. This study experimentally induced ischemic pain in otherwise pain-free subjects using a modified version of the submaximal effort tourniquet technique. Subjects completed twelve cycles of the ischemic-induced pain test. The primary outcome measure was the change in self-reported of pain intensity during one of four possible treatments. [Results] There were significant effects for Time, which were attributed to a significant reduction in pain intensity for all groups. There were no significant effects for groups or group-time interaction. The 50?Hz IFC treatment was more comfortable than the other treatments in the present study, and it is likely to be better accepted and tolerated by patients. [Conclusion] We conclude that there were no differences in the analgesic effects of the four treatments under the present experimental conditions. The 50?Hz IFC treatment is more comfortable than the other treatments. PMID:25540504

  8. Analgesic and anti-inflammatory effects in animal models of an ethanolic extract of Taheebo, the inner bark of Tabebuia avellanedae.

    Science.gov (United States)

    Lee, Mu Hong; Choi, Hyun Mi; Hahm, Dae-Hyun; Her, Erk; Yang, Hyung-In; Yoo, Myung Chul; Kim, Kyoung Soo

    2012-10-01

    Taheebo, the purple inner bark of the Bignoniaceae tree Tabebuia avellanedae Lorentz ex Griseb, which is found in tropical rain forests in northeastern Brazil, has been used as a traditional medicine for various diseases for more than 1,500 years. In the current study, various animal models were used to demonstrate the analgesic and anti-inflammatory properties of its ethanolic extract, thereby investigating its potential as a therapeutic treatment for diseases with pain and inflammation. In the hot plate and writhing tests for the in vivo analgesic effect test of Taheebo, a 200 mg/kg dose of the extract induced a significant anti-nociceptive effect and increased the pain threshold by approximately 30% compared with the control. In vascular permeability and tetradecanoylphorbol acetate (TPA)?, arachidonic acid- and carrageenan-induced paw edema tests for anti-inflammatory effects, treatment with 200 mg/kg Taheebo led to significant anti-inflammatory effects and inhibited inflammation by 30-50% compared with the control. At 100 mg/kg, the extract decreased the levels of pain and inflammation in all tested models, but the degree of inhibition was not statistically significant. The results suggest that the ethanolic extract of the inner bark of Tabebuia avellanedae has the potential to be developed as a therapeutic or supportive drug against diseases with accompanying pain and inflammation, including osteoarthritis. PMID:22825254

  9. CR4056, a new analgesic I2 ligand, is highly effective against bortezomib-induced painful neuropathy in rats

    Directory of Open Access Journals (Sweden)

    Meregalli C

    2012-06-01

    Full Text Available Cristina Meregalli,1 Cecilia Ceresa,1 Annalisa Canta,1 Valentina Alda Carozzi,1 Alessia Chiorazzi,1 Barbara Sala,1 Norberto Oggioni,1 Marco Lanza,2 Ornella Letar,i2 Flora Ferrari,2 Federica Avezza,1 Paola Marmiroli,1 GianFranco Caselli,2 Guido Cavaletti11Department of Neuroscience and Biomedical Technologies, University of Milan-Bicocca, 2Pharmacology and Toxicology Department, Rottapharm | Madaus Research Center, Monza, ItalyAbstract: Although bortezomib (BTZ is the frontline treatment for multiple myeloma, its clinical use is limited by the occurrence of painful peripheral neuropathy, whose treatment is still an unmet clinical need. Previous studies have shown chronic BTZ administration (0.20 mg/kg intravenously three times a week for 8 weeks to female Wistar rats induced a peripheral neuropathy similar to that observed in humans. In this animal model of BTZ-induced neurotoxicity, the present authors evaluated the efficacy of CR4056, a novel I2 ligand endowed with a remarkable efficacy in several animal pain models. CR4056 was administered in a wide range of doses (0.6–60 mg/kg by gavage every day for 2–3 weeks in comparison with buprenorphine (Bupre (28.8 µg/kg subcutaneously every day for 2 weeks and gabapentin (Gaba (100 mg/kg by gavage every day for 3 weeks. Chronic administration of BTZ reduced nerve conduction velocity and induced allodynia. CR4056, Bupre, or Gaba did not affect the impaired nerve conduction velocity. Conversely, CR4056 dose-dependently reversed BTZ-induced allodynia (minimum effective dose 0.6 mg/kg. The optimal dose found, 6 mg/kg, provided a constant pain relief throughout the treatment period and without rebound after suspension, being effective when coadministered with BTZ, starting before or after allodynia was established, or when administered alone after BTZ cessation. A certain degree of tolerance was seen after 7 days of administration, but only at the highest doses (20 and 60 mg/kg. Bupre was effective only acutely, since tolerance was evident from the fourth day onwards. Gaba showed a significant activity only at the fourth day of treatment. CR4056, over the range of concentrations of 3–30 µM, was unable to hinder BTZ cytotoxicity on several tumor cell lines, which could indicate that this substance does not directly interfere with BTZ antitumor activity. Therefore, CR4056 could represent a new treatment option for BTZ-induced neuropathic pain.Keywords: imidazoline I2 receptor ligand, antinociception, allodynia, neuropathic pain, bortezomib

  10. Efeito analgésico de antagonistas do receptor da histamina H2 em modelo de dor provocada por formalina em ratos / Analgesic effect of hystamine H2 receptor antagonists in formalin-induced pain model in rats

    Scientific Electronic Library Online (English)

    Deutsch, Fernanda; Hazem Adel, Ashmawi; Cláudia Carneiro de Araújo, Palmeira; Irimar de Paula, Posso.

    2011-09-01

    Full Text Available SciELO Brazil | Language: Portuguese Abstract in portuguese JUSTIFICATIVA E OBJETIVOS: Antagonistas de receptor de histamina apresentam efeitos sobre a dor. Antagonistas de receptor H1 apresentam efeito analgésico local, o papel de antagonistas de receptor H2 sobre a dor no sistema nervoso periférico ainda não está claro. Esse estudo teve como objetivo avali [...] ar os efeitos de diferentes antagonistas H2 sobre a dor induzida pela administração de formalina na pata de ratos. MÉTODO: Foram estudados ratos machos divididos em grupos que receberam formalina na pata e diferentes antagonistas de receptor H2 - ranitidina, cimetidina e loxtidina, injetados na pata em diferentes concentrações (0,05 ?mol, 0,25 ?mol ou 1 ?mol). Foi avaliado o número de elevações da pata pelo período de 45 minutos. RESULTADOS: A loxtidina inibiu o número de elevações da pata nas duas fases do teste a partir das três concentrações utilizadas, a ranitidina diminuiu o número de elevações da pata a partir da concentração de 0,25 ?mol na fase II, a cimetidina não inibiu esse comportamento doloroso. CONCLUSÃO: De acordo com os resultados deste estudo, alguns antagonistas do receptor H2 apresentaram efeito analgésico local fármaco específico e não classe farmacológica específica. Abstract in english BACKGROUND AND OBJECTIVES: Histamine receptor antagonists affect pain perception. H1 receptor antagonists present local analgesic effect, but the role of H2 receptor antagonists on pain in the peripheral nervous system is not clear yet. This study aimed at evaluating the effects of different H2 rece [...] ptor antagonists on pain induced by formalin paw injection in rats. METHOD: Male rats were studied and divided into groups that received formalin and different H2 receptor antagonists - ranitidine, cimetidine and loxtidine, injected in the paw at different concentrations (0.05 mol, 0.25 mol or 1 mol). The number of flinches was evaluated during 45 minutes. RESULTS: Loxtidine inhibited the number of flinches in both phases of the test with the three different concentrations. Ranitidine decreased the number of flinches in phase II as from 0.25 mol. Cimetidine did not affect pain behavior. CONCLUSION: According to the results of this study, some H2 receptor antagonists presented local analgesic effects, which seem to be drug-related and not pharmacological class-specific.

  11. Analgesic Activity of Psidium guajava root extracts

    Directory of Open Access Journals (Sweden)

    Girish Kumar Gupta1, Manisha Bhatia, Randhir Singh

    2013-03-01

    Full Text Available Natural products constitute the major division of pharmacotherapy. Psidium guajava Linn. has received much attention due to a variety of potential beneficial effects. Numerous polyphenolic compounds, triterpenoids and other chemical compounds are present in this plant. So the present study was designed to investigate the analgesic activity of petroleum ether extract and chloroform extract of Psidium guajava in rats. In the present study, analgesic activity of petroleum ether extract and chloroform extract of roots of Psidiium guajava L. was evaluated for the first time. Extracts were prepared by cold maceration process. The analgesicactivity was evaluated by using the tail immersion test andEddy's hot plate method. Different doses (100, 150 and200 mg/kg of petroleum ether extract (PEE and chloroform extract (CE of root of Psidiium guajava L were used for the study. Different doses (100, 150 and 200 mg/kg of PEE of Psidium guajava produced a significant increase in withdrawal time in mice in tail immersion test and effect was found to be dose dependent. Similar results were observed with different doses (100, 150 and 200 mg/kg of CE of Psidium guajava. The Evaluation of analgesic activity in Eddy's hot plate method revealed that PEE and CE has significant analgesic activity. Theincrease in time was found be dose dependent. The resultsobtained from the study indicate that PEE and CE ofPsidium guajava have significant analgesic activity.

  12. Evolution in pharmacologic thinking around the natural analgesic palmitoylethanolamide: from nonspecific resistance to PPAR-? agonist and effective nutraceutical.

    Science.gov (United States)

    Hesselink, Jan M Keppel

    2013-01-01

    The history of development of new concepts in pharmacology is a highly interesting topic. This review discusses scientific insights related to palmitoylethanolamide (PEA) and its progression over a period of six decades, especially in light of the work of the science sociologists, Ludwig Fleck and Thomas Kuhn. The discovery of the cannabis receptors and the nuclear peroxisome proliferator-activated receptors was the beginning of a completely new understanding of many important homeostatic physiologic mechanisms in the human body. These discoveries were necessary for us to understand the analgesic and anti-inflammatory activity of PEA, a body-own fatty amide. PEA is a nutrient known already for more than 50 years. PEA is synthesized and metabolized in animal cells via a number of enzymes and has a multitude of physiologic functions related to metabolic homeostasis. PEA was identified in the 1950s as a therapeutic principle with potent anti-inflammatory properties. Since 1975, its analgesic properties have been noted and explored in a variety of chronic pain states. Since 2008, PEA has been available as a nutraceutical under the brand names Normast® and PeaPure®. A literature search on PEA meanwhile has yielded over 350 papers, all referenced in PubMed, describing the physiologic properties of this endogenous modulator and its pharmacologic and therapeutic profile. This review describes the emergence of concepts related to the pharmacologic profile of PEA, with an emphasis on the search into its mechanism of action and the impact of failing to identify such mechanism in the period 1957-1993, on the acceptance of PEA as an anti-inflammatory and analgesic compound. PMID:23964161

  13. Paracetamol and analgesic nephropathy: Are you kidneying me?

    Directory of Open Access Journals (Sweden)

    Waddington F

    2014-12-01

    Full Text Available Freya Waddington, Mark Naunton, Jackson Thomas Faculty of Health, University of Canberra, Canberra, ACT, Australia Introduction: Analgesic nephropathy is a disease resulting from the frequent use of combinations of analgesic medications over many years, leading to significant impairment of renal function. The observation of a large number of cases of renal failure in patients abusing analgesic mixtures containing phenacetin led to the initial recognition of the nephrotoxicity from the use of analgesics. Phenacetin was subsequently exclusively blamed for this disease. However, the role of a single analgesic as a sole cause of analgesic nephropathy was challenged, and a number of researchers have since attempted to determine the extent of involvement of other analgesics including nonsteroidal anti-inflammatory drugs (NSAIDs, aspirin, and paracetamol. Case presentation: We present the case of an 83-year-old woman with a history of NSAID-induced nephropathy with poor pain control and reluctance to use paracetamol. We attempt to briefly review the evidence of paracetamol being implicated in the development of analgesic-induced nephropathy. Conclusion: There is a lack of concrete data regarding causative analgesics, including paracetamol. Patients should therefore not be withheld paracetamol, an effective and commonly recommended agent, for fear of worsening renal function. Keywords: kidney, paracetamol, nephropathy, phenacetin

  14. The pharmacology of topical analgesics.

    Science.gov (United States)

    Barkin, Robert L

    2013-07-01

    Pain management of patients continues to pose challenges to clinicians. Given the multiple dimensions of pain--whether acute or chronic, mild, moderate, or severe, nociceptive or neuropathic--a multimodal approach may be needed. Fortunately, clinicians have an array of nonpharmacologic and pharmacologic treatment choices; however, each modality must be chosen carefully, because some often used oral agents are associated with safety and tolerability issues that restrict their use in certain patients. In particular, orally administered nonsteroidal antiinflammatory drugs, opioids, antidepressants, and anticonvulsants are known to cause systemic adverse effects in some patients. To address this problem, a number of topical therapies in various therapeutic classes have been developed to reduce systemic exposure and minimize the risks of patients developing adverse events. For example, topical nonsteroidal anti-inflammatory drug formulations produce a site-specific effect (ie, cyclo-oxygenase inhibition) while decreasing the systemic exposure that may lead to undesired effects in patients. Similarly, derivatives of acetylsalicylic acid (ie, salicylates) are used in topical analgesic formulations that do not significantly enter the patient's systemic circulation. Salicylates, along with capsaicin, menthol, and camphor, compose the counterirritant class of topical analgesics, which produce analgesia by activating and then desensitizing epidermal nociceptors. Additionally, patches and creams that contain the local anesthetic lidocaine, alone or co-formulated with other local anesthetics, are also used to manage patients with select acute and chronic pain states. Perhaps the most common topical analgesic modality is the cautious application of cutaneous cold and heat. Such treatments may decrease pain not by reaching the target tissue through systemic distribution, but by acting more directly on the affected tissue. Despite the tolerability benefits associated with avoiding systemic circulation, topically applied analgesics are associated with application-site reactions in patients, such as dryness, erythema, burning, and discoloration. Furthermore, some adverse events that have been observed in patients may be suggestive of some degree of systemic exposure. This article reviews the mechanisms of action, pharmacokinetics, and tolerability of topical treatments for the management of patient pain. PMID:24547599

  15. Evaluation of Anti-Inflammatory, Analgesic and Antipyretic Effects of Azadrichcta indica Leaf Extract on Fever-Induced Albino Rats (Wistar

    Directory of Open Access Journals (Sweden)

    O.J. Olorunfemi

    2012-04-01

    Full Text Available The present study was carried out to investigate the anti-inflammatory, antipyretic and analgesic effect of the crude ethanol extract of Azadirachta indica leaves on experimental rat model at three different dose levels- 100, 200 and 300 mg/kg, respectively. Hot plate test were used to assess analgesic activity, formalin induced inflammation was used for anti-inflammatory study and baker’s yeast was used to induce pyrexia. Acute toxicity test was also performed in rats after administration of the extract orally at high dose level (4 g/kg. In addition, ethanol extract obtained from Azadirachta indica leaves at different doses and different periods of study showed significant effect (p<0.05 compared to control. For analgesic study, the extract at 100 mg/kg showed a slow but time dependent effect, at 200 mg/kg, its effect was noticed in all the periods although still time dependent and at 300 mg/kg, the effect was significant in all the periods and long-lasting at the final minutes (90 min with values expressed in mean±SEM of 14.0±1.41 which was significant (*p<0.05 compared to control and all other groups. The anti-inflammatory study of the ethanolic extract of Azadirachta indica showed a time and dose dependent effect at different periods. It’s effect was noticed in all doses but was most significant (**p<0.05 in group 4 which was given 300 mg/kg of the extract with a value of 40.6±8.80 expressed in mean±SEM compared to control and all other groups. The extract at all dose showed significant effect (*p<0.05 over control. Its effect was time and dose-dependent. However, the extract attenuated the pain, fever and inflammation induced in the rats at 100, 200 and 300 mg/kg, respectively dose levels but its significant protective effect was noticed at higher doses than low doses and at a longer period of time. In acute toxicity study, no mortality was observed at 4 g/kg dose level.

  16. Study of the effects of semiconductor laser irradiation on peripheral nerve injury

    Science.gov (United States)

    Xiong, G. X.; Li, P.

    2012-11-01

    In order to study to what extent diode laser irradiation effects peripheral nerve injury, the experimental research was made on rabbits. Experimental results show that low-energy semiconductor laser can promote axonal regeneration and improve nervous function. It is also found that simultaneous exposure of the injured peripheral nerve and corresponding spinal segments to laser irradiation may achieve the most significant results.

  17. Pain: Identification of novel analgesics from traditional Chinese medicines

    Science.gov (United States)

    Ingram, Susan L.

    2014-01-01

    The search for analgesics with fewer side effects and less abuse potential has had limited success. A new study from Zhang and colleagues identifies an analgesic alkaloid compound from Corydalis yanhusuo, a traditional Chinese medicinal herb that has a surprising mechanism of action. PMID:24502784

  18. [Analgesic and anti-inflammatory activity of saponins of Argania spinoza].

    Science.gov (United States)

    Alaoui, K; Lagorce, J F; Cherrah, Y; Hassar, M; Amarouch, H; Roquebert, J

    1998-01-01

    We studied analgesic and antiinflammatory actions of saponins of Argania spinosa cakes in mice and rats. With oral doses of 50 to 300 mg/kg, we found peripheric analgesic actions equivalent to the acetyl salicylic acid ones. The maximum protection was obtained with 500 mg/kg per os. There is no morphine-like central analgesic effect. Antiinflammatory studies were done in vivo using oedema due to carrageenine or experimental trauma in rats. There was a decrease in the paw swelling at doses of 10 mg/kg per os. At doses of 50 to 100 mg/kg per os, the antiinflammatory effect was similar to the one of indomethacin at doses of 10 to 20 mg/kg per os. In vitro, there was an inhibition of beef synovial fluid degradation by OH. radicals. The inhibition action is evaluated with an IC20 > or = 6 microM. Argania spinosa saponins have also an antiradical action against DPPH (IC25 = 85 mM) and against OH. radicals (IC25 = 0.56 M). Since they do not have any inhibition effect on PGE2 synthesis, their antiinflammatory activity can be explained by their action on leucotriens in the metabolic pathway of arachidonic acid. PMID:9805822

  19. Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain / Possível efeito analgésico da vigabatrina na dor neuropática crônica experimental animal

    Scientific Electronic Library Online (English)

    NILZA D., ALVES; CARLOS M. DE, CASTRO-COSTA; ALBA M. DE, CARVALHO; FRANKLIN J. C., SANTOS; DELANO G., SILVEIRA.

    1999-12-01

    Full Text Available SciELO Brazil | Language: English Abstract in portuguese O uso de anticonvulsivantes no tratamento de neuralgias despertou um interesse em testar novas drogas anticonvulsivantes, e dentre essas a vigabatrina por possuir mecanismo de ação gabaérgico. Para isso, foram usados 41 ratos Wistar e em 25 deles induziu-se neuropatia ciática constritiva (modelo de [...] Bennett & Xie). Para testar sintomas de dor, foram quantificados comportamentos espontâneos (coçar-se) e evocados, por meio de estímulos térmicos nocivos (46oC) e não-nocivos (40oC). Além disso, realizou-se estudo comparativo da vigabatrina com outros anticonvulsivantes analgésicos. Os resultados mostraram um possível efeito analgésico, dose-dependente, de vigabatrina (gama-vinil-GABA) em dor neuropática experimental. Isso foi evidenciado pela diminuição significativa (p Abstract in english Since anticonvulsants have been used for treating neuralgias, an interest has arisen to experimentally test vigabatrin for its gabaergic mechanism of action. For this, 41 Wistar rats were used, and in 25 of them a constrictive sciatic neuropathy was induced (Bennet & Xie model). For testing pain sym [...] ptoms, spontaneous (scratching) and evoked behaviors to noxious (46o C) and non-noxious (40o C) thermal stimuli were quantified. Moreover, a comparative pharmacological study of vigabatrin with other analgesic anticonvulsant drugs was also performed. The results showed a possible dose-dependent analgesic effect of vigabatrin (gamma-vinyl-GABA) on experimental neuropathic pain, as shown by the significant (p

  20. Differential analgesic effects of low-dose epidural morphine and morphine-bupivacaine at rest and during mobilization after major abdominal surgery.

    DEFF Research Database (Denmark)

    Dahl, J B; Rosenberg, J

    1992-01-01

    In a double-blind, randomized study, epidural infusions of low-dose morphine (0.2 mg/h) combined with low-dose bupivacaine (10 mg/h) were compared with epidural infusions of low-dose morphine (0.2 mg/h) alone for postoperative analgesia at rest and during mobilization and cough in 24 patients after elective major abdominal surgery. All patients in addition received systemic piroxicam (20 mg daily). No significant differences were observed between the groups at any assessment of pain at rest (P greater than 0.05), whereas pain in the morphine/bupivacaine group was significantly reduced during mobilization from the supine into the sitting position 12 and 30 h after surgical incision and during cough 8, 12, and 30 h after surgical incision (P less than 0.05). We conclude, that low-dose epidural bupivacaine potentiates postoperative low-dose epidural morphine analgesia during mobilization and cough. Evaluation of postoperative analgesic regimens should include assessment of pain during various activities as different analgesics may have differential effects on pain at rest and during mobilization.

  1. Efficacy of OTC analgesics.

    Science.gov (United States)

    Moore, R A; Derry, C

    2013-01-01

    For many 'over-the-counter' (OTC) analgesics, there is little information available about their relative efficacy. We have examined information available in a series of Cochrane reviews of single doses of analgesic drugs in acute pain and migraine for its relevance for analgesic products commonly available without prescription, at doses generally equivalent to two tablets. Pain following third molar extraction was used as a homogeneous acute pain model; with the outcome of at least 50% maximum pain relief over 6 h. For many OTC drugs, there was no information available. For some OTC drugs, there was at least some information available either for the marketed product itself, or from studies that used the same doses of drug or drugs. For acute pain, data from third molar extraction studies showed that several OTC products were highly efficacious, principally non-steroidal anti-inflammatory drugs (ibuprofen, naproxen, diclofenac) and combination products based on ibuprofen; aspirin and paracetamol-based products were less efficacious. Fixed-dose combinations, especially those with ibuprofen, provided high levels of analgesia. For migraine headache, the outcome used was pain initially moderate or severe becoming no worse than mild pain (no pain, mild pain) at 2 h. Single-dose ibuprofen 400 mg was better than aspirin and paracetamol. PMID:23163544

  2. Analgesic Activity of Abelmoschus manihot Extracts

    Directory of Open Access Journals (Sweden)

    J. Surana Sanjay

    2011-01-01

    Full Text Available The natural products served as important sources of medicines now a day increasing, as they possess the therapeutic activity. Therefore, the present study was carried out to evaluate the analgesic activity of the petroleum ether and methanol extract of Abelmoschus manihot (Malvaceae leaves using hot plate and tail immersion model. The air-dried, powdered leaves (1000 g were extracted over Soxhlet with petroleum ether and methanol. The crude dried petroleum ether (10 g and methanol (25 g extracts was prepared at the doses of 100, 200 and 400 mg kg-1 and evaluated for analgesic activity using the hot plate and tail immersion test. The results obtained indicate that the extracts possessed significant (p-1 dose as compared with the standard drug. This study showed that the petroleum ether and methanol extracts of Abelmoschus manihot leaves possess potential pharmacological active constituents responsible for inhibition of the analgesic effect.

  3. Effects of Dioscoreae Rhizoma (SanYak on Peripheral Neuropathy and its Safety

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    Kim Min-jung

    2013-09-01

    Full Text Available Objectives: This study aimed to evaluate the evidence available in the literature for the safety and efficacy of Dioscoreae Rhizoma (DR for the treatment of peripheral neuropathy. Methods: Literature searches were performed in MEDLINE and three Korean medical databases up to April 2013. All studies evaluating the effects on peripheral neuropathy or the safety of DR monopreparations were considered. Results: Three studies - DR extract per os (po on diabetic neuropathy in mice, DR extract injection on the peripheral sciatic nerve after crush injury in rats and DR extract injection to patients with peripheral facial paralysis proved that DR treatments were effective for the treatment of nerve injuries. Conclusions: In conclusion, we found the DR has a strong positive potential for the treatment of peripheral neuropathy, but studies addressing direct factors related to the nerve still remain insufficient.

  4. Analgesic, Anti-inflammatory and Antihyperlipidemic Activities of Commiphora molmol Extract (Myrrh

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    Mostafa Abbas Shalaby

    2014-04-01

    Full Text Available Aim: To evaluate the analgesic, anti-inflammatory and antihyperlipidemic activities of Commiphora molmol extract (CME and its effect on body weight. Material and Methods: The analgesic effect was assessed using thermal (hot plate test and chemical (writhing test stimuli to induce central and peripheral pain in mice. The anti-inflammatory activity was determined using formalin-induced paw edema in rats. For antihyperlipidemic effect, thirty five rats were randomized into five equal groups (n=7. Group (1 was fed on basal diet (Normal control, while the other 4 groups were fed on high-fat diet for 6 weeks to induce obesity and hyperlipidemia. Thereafter, group (2 was kept obese hyperlipidemic, and groups (3, (4 and (5 were orally given CME in doses of 125, 250 and 500 mg/kg for 6 weeks, respectively. Body weight gains of rats were calculated and blood samples were collected for analysis of blood lipids. Results: CME produced a dose-dependent analgesic effect using both hot plate and writhing tests in mice. The hot plate method appeared to be more sensitive than writhing test. CME exhibited an anti-inflammatory activity as it reduced volume of paw edema induced by formalin in rats. This extract decreased body weight gains; normalized the high levels of blood lipids and decreased atherogenic index (LDL/HDL in obese hyperlipidemic rats. Conclusion: The results of this study denote that Commiphora molmol extract (Myrrh has significant analgesic, anti-inflammatory, and antihyperlipidemic effects and decreases body weight. These results affirm the traditional use of Commiphora molmol for the treatment of pain, inflammations, and hyperlipidemia. [J Intercult Ethnopharmacol 2014; 3(2.000: 56-62

  5. Analgesic effects of methanolic extracts of the leaf or root of Moringa oleifera on complete Freund’s adjuvant-induced arthritis in rats

    Directory of Open Access Journals (Sweden)

    Homa Manaheji

    2011-02-01

    Full Text Available Objective: Moringa oleifera (family Moringaceae has been widely used in African folk medicine, and researchers have recently revealed its anti-inflammatory effects in human. This study aimed to evaluate the analgesic properties of methanolic extracts of M. oleifera in complete Freund’s adjuvant (CFA-induced arthritis in rats. Methods: Adult male Wistar rats, weighing 200 to 220 g, were used in this study. Adjuvant arthritis was induced on day 0 by a single subcutaneous injection of CFA. The prepared extracts from both the root and leaf (200, 300 and 400 mg/kg of M. oleifera were administered intraperitonealy to rats in the treatment groups 0, 3 and 6 d after CFA injection and indomethacin (5 mg/kg was used as a positive control drug. Thermal hyperalgesia and mechanical allodynia were evaluated for the analgesic effect 0, 3 and 6 d after CFA injection. Combined methanolic root and leaf extracts of M. oleifera (200 mg/kg were also tested for the analgesic effect.Results: The potency of the root or leaf extracts of M. oleifera (300 and 400 mg/kg was similar to that of indomethacin, resulted in significant reductions in both thermal hyperalgesia and mechanical allodynia in rats with CFA-induced arthritis compared with the control group after 3 and 6 d, respectively (P<0.01 or P<0.05. Combined root and leaf extracts (200 mg/kg of M. oleifera resulted in a significant reduction in thermal hyperalgesia compared with the control group after 3 and 6 d, respectively (P<0.01. Prophylactic injections of combined root and leaf extracts of M. oleifera (200 mg/kg resulted in a significant reduction in thermal hyperalgesia compared with the control group, the root extracts group, and the leaf extracts group after 3 and 6 d, respectively (P<0.01. Conclusion: The methanolic extracts of the root or leaf of M. oleifera are effective in the reduction of pain induced by CFA in rats. A comparison of single and combination therapies of root and leaf extracts also showed a synergistic effect on pain reduction.

  6. Effects of Reference Analgesics and Psychoactive Drugs on the Noxious Heat Threshold of Mice Measured by an Increasing-Temperature Water Bath.

    Science.gov (United States)

    Boros, Melinda; Benkó, Rita; Bölcskei, Kata; Szolcsányi, János; Barthó, Loránd; Peth?, Gábor

    2013-08-19

    The study aimed at validating an increasing-temperature water bath suitable for determining the noxious heat threshold for use in mice. The noxious heat threshold was determined by immersing the tail of the gently held awake mouse into a water container whose temperature was near-linearly increased at a rate of 24°C/min. until the animal withdrew its tail, that is, heating attained the noxious threshold. The effects of standard analgesic, neuroleptic and anxiolytic drugs were investigated in a parallel way on both the noxious heat threshold and the psychomotor activity assessed by the open field test. Morphine, diclofenac and metamizol (dipyrone) elevated the heat threshold of mice with minimum effective doses of 6, 30 and 1000 mg/kg i.p., respectively. These doses of morphine and diclofenac failed to induce any remarkable effect on psychomotor activity in the open field test while that of metamizol exerted a profound inhibition. The anxiolytic diazepam and the neuroleptic droperidol at doses evoking a mild and moderate, respectively, psychomotor inhibition failed to alter the heat threshold. Combination of a subliminal dose of morphine (regarding both antinociceptive and psychomotor inhibitory action) with diclofenac, metamizol, diazepam or droperidol at doses also subliminal regarding the thermal antinociceptive effect elevated the noxious heat threshold without major additional effects in the open field test. It is concluded that the increasing-temperature water bath is suitable for studying the thermal antinociceptive effects of morphine and diclofenac as well as the morphine-sparing action of diclofenac, metamizol, droperidol and diazepam. Behavioural testing is recommended when testing analgesics. PMID:23957272

  7. Inhibition of spinal astrocytic c-Jun N-terminal kinase (JNK activation correlates with the analgesic effects of ketamine in neuropathic pain

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    Wang Wen

    2011-01-01

    Full Text Available Abstract Background We have previously reported that inhibition of astrocytic activation contributes to the analgesic effects of intrathecal ketamine on spinal nerve ligation (SNL-induced neuropathic pain. However, the underlying mechanisms are still unclear. c-Jun N-terminal kinase (JNK, a member of mitogen-activated protein kinase (MAPK family, has been reported to be critical for spinal astrocytic activation and neuropathic pain development after SNL. Ketamine can decrease lipopolysaccharide (LPS-induced phosphorylated JNK (pJNK expression and could thus exert its anti-inflammatory effect. We hypothesized that inhibition of astrocytic JNK activation might be involved in the suppressive effect of ketamine on SNL-induced spinal astrocytic activation. Methods Immunofluorescence histochemical staining was used to detect SNL-induced spinal pJNK expression and localization. The effects of ketamine on SNL-induced mechanical allodynia were confirmed by behavioral testing. Immunofluorescence histochemistry and Western blot were used to quantify the SNL-induced spinal pJNK expression after ketamine administration. Results The present study showed that SNL induced ipsilateral pJNK up-regulation in astrocytes but not microglia or neurons within the spinal dorsal horn. Intrathecal ketamine relieved SNL-induced mechanical allodynia without interfering with motor performance. Additionally, intrathecal administration of ketamine attenuated SNL-induced spinal astrocytic JNK activation in a dose-dependent manner, but not JNK protein expression. Conclusions The present results suggest that inhibition of JNK activation may be involved in the suppressive effects of ketamine on SNL-induced spinal astrocyte activation. Therefore, inhibition of spinal JNK activation may be involved in the analgesic effects of ketamine on SNL-induced neuropathic pain.

  8. Analgesic, antiinflammatory and hypoglycaemic activities of Sida cordifolia.

    Science.gov (United States)

    Kanth, V R; Diwan, P V

    1999-02-01

    Sida cordifolia extracts of the aerial and root parts showed good analgesic, antiinflammatory and hypoglycaemic activities. The ethyl acetate (EA) extract of root (SCR-E) showed comparable antiinflammatory activity with indomethacin and possessed significantly higher activity when compared with that of the methanol extract of the root part (SCR-M). The ethyl acetate extract of both root and aerial parts of Sida cordifolia (SCR-E and SCA-E) showed very good central and peripheral analgesic activities at a dose of 600 mg/kg. The methanol extract of root (SCR-M) was found to possess significant hypoglycaemic activity. PMID:10189958

  9. Analgesic effect of electroacupuncture on chronic neuropathic pain mediated by P2X3 receptors in rat dorsal root ganglion neurons.

    Science.gov (United States)

    Tu, Wen-zhan; Cheng, Rui-dong; Cheng, Bo; Lu, Jike; Cao, Fen; Lin, Hai-yan; Jiang, Yong-xia; Wang, Jie-zhi; Chen, Hao; Jiang, Song-he

    2012-03-01

    Adenosine 5'-triphosphate disodium (ATP) gated P2X receptors, especially the subtype P2X(3), play a key role in transmission of pain signals in neuropathic pain, ATP has been documented to play a significant role in the progression of pain signals, suggesting that control of these pathways through electroacupuncture (EA) is potentially an effective treatment for chronic neuropathic pain. EA has been accepted to effectively manage chronic pain by applying the stimulating current to acupoints through acupuncture needles. To determine the significance of EA on neuropathic pain mediated by P2X(3) receptors in the dorsal root ganglion (DRG) neurons, mechanical withdrawal threshold (MWT) and thermal withdrawal latency (TWL) were recorded, and the expression of P2X(3) receptors in the DRG neurons was assessed by immunohistochemistry (IHC) and in situ hybridization (ISH). In addition, the currents which were evoked in DRG neurons isolated from rats following chronic constriction injury (CCI) by the P2X(3) receptors agonists i.e. ATP and ?,?-methylen-ATP (?,?-meATP) were examined through the experimental use of whole cell patch clamp recording. The present study demonstrates that EA treatment can increase the MWT and TWL values and decrease the expression of P2X(3) receptors in DRG neurons in CCI rats. Simultaneously, EA treatment attenuates the ATP and ?,?-meATP evoked currents. EA may be expected to induce an apparent induce analgesic effect by decreasing expression and inhibiting P2X(3) receptors in DRG neurons of CCI rats. There is a similar effect on analgesic effect between rats with contralateral EA and those with ipsilateral EA. PMID:22269805

  10. Analgesic and Anti-inflammatory Activity of Teucrium chamaedrys Leaves Aqueous Extract in Male Rats

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    Ali Pourmotabbed

    2010-06-01

    Full Text Available Objective(sCurrent study was undertaken to investigate the analgesic and anti-inflammatory effects of the aqueous extract of Teucrium chamaedrys in mice and rats. Materials and MethodsFor evaluating of analgesic and anti-inflammatory activity, we used the carrageenan- and dextran-induced paw oedema, acetic acid-induced writhing, tail flick and formalin pain tests.ResultsThe extract of T. chamaedrys (50–200 mg/kg and acetylsalicylic acid (100 mg/kg produced a significant (P< 0.01 inhibition of the second phase response in the formalin pain model, while only the high dose (200 mg/kg of the extract showed an analgesic effect in the first phase. The extract also inhibited acetic acid-induced abdominal writhes in a dose-dependent manner. The tail flick latency was dose dependently enhanced by the extract but this was significantly (P< 0.05 lower than that produced by morphine (10 mg/kg. The extract (25–250 mg/kg administered 1 hr before carrageenan-induced paw swelling produced a dose dependent inhibition of the oedema. No effect was observed with the dextran-induced oedema model. Results of the phytochemical screening show the presence of alkaloids, flavonoids and triterpenoids in the extract.ConclusionThe data obtained also suggest that the anti-inflammatory and analgesic effects of the extract may be mediated via both peripheral and central mechanisms. The role of alkaloids, flavonoids and triterpenoids will evaluate in future studies.

  11. Efeito analgésico de longa duração da dipirona sobre a hiperalgesia persistente induzida pela constrição do nervo ciático em ratos: participação do óxido nítrico Long term analgesic effect of dipyrone on the persistent hyperalgesia induced by chronic constriction injury of sciatic nerve in rats: involviment of nitric oxide

    Directory of Open Access Journals (Sweden)

    Fábio José Reis

    2006-12-01

    Full Text Available O efeito analgésico de longa duração da dipirona foi avaliado em um modelo de dor neuropática assim como a participação da via óxido nítrico-GMPc neste mecanismo analgésico. Uma única administração intraplantar de dipirona (80 µg, no 14º dia após a instalação da hiperalgesia neuropática induzida pela constrição do nervo ciático exerceu um efeito analgésico, significativo e de longa duração. A inibição da óxido nítrico sintetase com L-NAME (50 ou 100 µg/pata, ou do óxido nítrico (NO endógeno com hemoglobina (10 ou 30 µg/pata, bloquearam o desenvolvimento do efeito analgésico da dipirona. A L-arginina (500 µg/pata reverteu o efeito do L-NAME. Cloreto de metiltionínio (azul de metileno (500 µg/pata, ODQ (50 µg/pata (bloqueadores da guanilil ciclase ou glibenclamida (100, 200 ou 300 µg/pata (bloqueador de canais de K+ sensíveis ao ATP inibiram o efeito analgésico da dipirona. O nitroprussiato de sódio administrado no 14º dia após a instalação da hiperalgesia neuropática também exerceu efeito analgésico de longa duração, semelhante ao observado com a dipirona. Sugerimos que a ação analgésica periférica e de longa duração da dipirona, neste modelo experimental, ocorra devido a provável dessensibilização dos nociceptores, envolvendo a via óxido nítrico - GMPc e canais de K+ sensíveis ao ATP.The long term analgesic effect of dipyrone was evaluated on a model of neuropathic pain and the role of nitric oxide/GMPc pathway in this antinociceptive mechanism. One intraplantar dipyrone administration (80 mg, at 14th day after the chronic constriction injury of the sciatic nerve, induced a significant and long term analgesic effect. The inhibition of nitric oxide synthase (NOS with L-NAME (50 or 100 mg/paw or scavenging of the endogenous NO with hemoglobin (10 or 30 mg/paw inhibited the development of the dipyrone analgesia. L-arginine (500 mg/paw could reverted the effect of L-NAME. Metylene blue (500 mg/paw or ODQ (50 mg/paw (blockers of guanyl cyclase, or glybenclamide (100, 200 or 300 mg/paw (blocker of ATP-sensitive K+ channels inhibited the development of dipyrone analgesia. The sodium nitroprussiate administered at 14th day after the chronic constriction injury of the sciatic nerve also induced a long term analgesic effect similar to that of dipyrone. Our data may support the suggestion that the peripheral and the long term analgesic action of dipyrone on this model experimental occurs due to a probable nociceptor desensitisation with involviment of activation of the nitric oxide-cGMP pathway, followed by an opening of ATP-sensitive K+ channels.

  12. Effect of prostaglandin E1 analogue administration on peripheral skin temperature at high altitude.

    Science.gov (United States)

    Saito, S; Shimada, H

    1994-06-01

    The effect of prostaglandin E1 analogue on peripheral skin temperature was examined at high altitude, where local cold injuries are common owing to severe environmental conditions. The peripheral skin temperature at rest was significantly lower at higher altitudes. Oral administration of the prostaglandin E1 analogue limaprost reversed this temperature decrease, probably by enhancement of peripheral circulation. The temperature recovery rate after a cold water challenge was also improved after the administration of limaprost. This oral type of prostaglandin E1 analogue is strongly recommended as an effective prophylactic and therapeutic vasodilator for local cold injuries at high altitudes. PMID:8203772

  13. Analgesic effect of morphine microinjected into the nucleus raphe magnus after electrolytic lesion of nucleus cuneiformis in tail-flick and formalin tests in rat

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    Leila Ahmad-Molaei

    2011-10-01

    Full Text Available Introduction: The antinociceptive effect of morphine is, in part, mediated through the activation of a descending pathway. One of the major components of this pathway is the nucleus raphe magnus (NRM. Our previous study demonstrated the involvement of NRM in the analgesic effect of morphine microinjected into the nucleus cuneiformis (NCF in a descending manner. The aim of the current study was to investigate another aspect of the interaction between these two nuclei in both acute and chronic inflammatory pain models. Methods: In order to calculate 50% effective dose (ED50 of morphine, animals received bilateral morphine injections (1, 2.5, 5 and 10 ?g/0.5 ?l saline into the NRM. The obtained ED50 of morphine was applied into the NRM with/without bilateral electrolytic lesion (500 ?A, 30 sec of the NCF. Tail-flick and formalin tests were applied as behavioral analgesic tests in this study. Results: Results interestingly showed that the intra-NRM morphine injection (ED50; 1 ?g/0.5 ?l saline resulted in an increase in tail flick latencies (morphine-induced antinociception at 30-min intervals, while bilateral electrolytic lesions in the NCF could notably decreased the morphine-induced antinociception during 30-90 min after the injection of morphine. Data also showed that bilateral morphine microinjected into the NRM, dose-dependently increases the antinociceptive responses during both early and late phases of formalin test. The antinociceptive effect of morphine microinjected into the NRM was significantly attenuated at the late phase but not early phase following the bilateral destruction of NCF in formalin test. Conclusion: It could be concluded that there is a reciprocal interaction between NRM and NCF during morphine - induced antinociception in both acute and chronic inflammatory pain models in rat.

  14. EXPERIMENTAL EVALUATION FOR ANALGESIC ACTIVITY OF MAMSYADI KWATHA

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    Shreevathsa

    2011-04-01

    Full Text Available Siddha Yoga Sangraha of Yadavji Trikamji Acharya, states about Mamsyadi kwatha, an Ayurvedic formulation which is said to be effective in minor mental disorders. The ingredients of Mamsyadi kwatha are Jatamamsi (Nardistachys jatamansi DC, Ashwagandha (Withania somnifera Linn and Parasika yavani (Hyoscymus niger Linn, in 8:4:1 ratio respectively. The test formulation was subjected to assess its analgesic effect. The model selected for the assessment of analgesic effect was tail flick test, in albino mice. The test formulation possesses analgesic effect, which is mainly due to its component Parasika yavani.

  15. Superior analgesic effect of H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA), a multifunctional opioid peptide, compared to morphine in a rat model of neuropathic pain

    OpenAIRE

    Shimoyama, Megumi; Schiller, Peter W.; Shimoyama, Naohito; Toyama, Satoshi; Szeto, Hazel H.

    2012-01-01

    H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA), is a synthetic tetrapeptide with extraordinary selectivity for the mu-opioid receptor and is an extremely potent analgesic. [Dmt1]DALDA is unusual in the way that the greater part of its analgesic potency appears to be produced by its actions in the spinal cord. Furthermore, [Dmt1]DALDA inhibits norepinephrine re-uptake and is a mitochondria-targeted antioxidant. Such characteristics may make [Dmt1]DALDA particularly effective against neuropathic pain. T...

  16. The effect of glycomimetic functionalized collagen on peripheral nerve repair

    OpenAIRE

    Masand, Shirley N.; Chen, Jian; Perron, Isaac J.; Hammerling, Babette C.; Loers, Gabriele; Schachner, Melitta; Shreiber, David I.

    2012-01-01

    Increasing evidence suggests that the improper synaptic reconnection of regenerating axons is a significant cause of incomplete functional recovery following peripheral nerve injury. In this study, we evaluate the use of collagen hydrogels functionalized with two peptide glycomimetics of naturally occurring carbohydrates—polysialic acid (PSA) and human natural killer cell epitope epitope (HNK-1)—that have been independently shown to encourage nerve regeneration and axonal targeting. Our n...

  17. GABA(B) receptor-mediated selective peripheral analgesia by the non-proteinogenic amino acid, isovaline.

    Science.gov (United States)

    Whitehead, R A; Puil, E; Ries, C R; Schwarz, S K W; Wall, R A; Cooke, J E; Putrenko, I; Sallam, N A; MacLeod, B A

    2012-06-28

    Peripherally restricted analgesics are desirable to avoid central nervous system (CNS) side effects of opioids. Nonsteroidal anti-inflammatory drugs produce peripheral analgesia but have significant toxicity. GABA(B) receptors represent peripheral targets for analgesia but selective GABA(B) agonists like baclofen cross the blood-brain barrier. Recently, we found that the CNS-impermeant amino acid, isovaline, produces analgesia without apparent CNS effects. On observing that isovaline has GABA(B) activity in brain slices, we examined the hypothesis that isovaline produces peripheral analgesia mediated by GABA(B) receptors. We compared the peripheral analgesic and CNS effect profiles of isovaline, baclofen, and GABA (a CNS-impermeant, unselective GABA(B) agonist). All three amino acids attenuated allodynia induced by prostaglandin E2 injection into the mouse hindpaw and tested with von Frey filaments. The antiallodynic actions of isovaline, baclofen, and GABA were blocked by the GABA(B) antagonist, CGP52432, and potentiated by the GABA(B) modulator, CGP7930. We measured Behavioural Hyperactivity Scores and temperature change as indicators of GABAergic action in the CNS. ED(95) doses of isovaline and GABA produced no CNS effects while baclofen produced substantial sedation and hypothermia. In a mouse model of osteoarthritis, isovaline restored performance during forced exercise to baseline values. Immunohistochemical staining of cutaneous layers of the analgesic test site demonstrated co-localization of GABA(B1) and GABA(B2) receptor subunits on fine nerve endings and keratinocytes. Isovaline represents a new class of peripherally restricted analgesics without CNS effects, mediated by cutaneous GABA(B) receptors. PMID:22525135

  18. The paradoxical effects of analgesics and the development of chronic migraine / Migrânea crônica e os efeitos paradoxais dos analgésicos

    Scientific Electronic Library Online (English)

    Marcelo E., Bigal.

    2011-06-01

    Full Text Available Fração não desprezível de pacientes com migrânea episodica evolve para um estágio em que cefaléias acontecem na maior parte dos dias. Dentre os fatores de risco para esse processo de cronificação, o uso excessivo de analgésicos tem importância particular e é o tema desse artigo. A causalidade da ass [...] ociação é discutida, assim como a especificidade da associação. Evidência sugerindo que doses críticas de exposição podem ser inferidas também é revisada, assim como a plausibilidade da associação e mecanismos da mesma. Abstract in english In a subgroup of individuals episodic migraine evolves into a stage where individuals have headaches on more days than not. Among the risk factors for chronification, excessive use of analgesic medications figure prominently and reviewing this topic is the scope of this article. The issue of causali [...] ty is discussed and evidence suggesting that specific medications, at critical doses, are risk factors for chronic migraine (CM) is reviewed. The concept of critical dose of exposure for different classes is presented and biological plausibility and putative mechanisms are reviewed.

  19. An effect of wrapping peripheral nerve anastomosis with pedicled muscle flap on nerve regeneration in experiment

    Directory of Open Access Journals (Sweden)

    Naumenko L.Yu.

    2010-01-01

    Full Text Available Despite intrinsic capacity of peripheral nerves to regenerate, functional outcomes of peripheral nerves injury remain poor. Nerve ischemia, intra-/perineurial fibrosis and neuroma formation contribute a lot to that. Several authors demonstrated beneficial effects of increased vascularization at the site of injury on peripheral nerves regeneration. The use of highly vascularized autologous tissues (greater omentum as a source of peripheral nerves neovascularization shows promising re-sults. We proposed a surgical technique in which injured peripheral nerves anastomosis was wrapped in a pedicled muscular flap and performed morphological assessment of the efficacy of such technique with the aid of immunohistochemistry. 14 rats (which underwent sciatic nerve transection were operated according to proposed technique. Another 14 rats, in which only end-to-end nerve anastomosis (without muscular wrapping was performed served as controls. Morphological changes were evaluated at 3 weeks and 3 months periods. Higher blood vessel and axon counts were observed in experimental groups at both checkpoints. There was also an increase in Schwann cells and macrophages counts, and less collagen content in pe-ripheral nerves of experimental groups. Axons in neuromas of experimental groups showed a higher degree of arrangement. We conclude that proposed surgical technique provides better vascularisation of injured peripheral nerves, which is beneficial for nerve regeneration.

  20. Can quantitative sensory testing predict responses to analgesic treatment?

    DEFF Research Database (Denmark)

    Grosen, K; Fischer, Iben W. Deleuran

    2013-01-01

    The role of quantitative sensory testing (QST) in prediction of analgesic effect in humans is scarcely investigated. This updated review assesses the effectiveness in predicting analgesic effects in healthy volunteers, surgical patients and patients with chronic pain. A systematic review of English written, peer-reviewed articles was conducted using PubMed and Embase (1980-2013). Additional studies were identified by chain searching. Search terms included 'quantitative sensory testing', 'sensory testing' and 'analgesics'. Studies on the relationship between QST and response to analgesic treatment in human adults were included. Appraisal of the methodological quality of the included studies was based on evaluative criteria for prognostic studies. Fourteen studies (including 720 individuals) met the inclusion criteria. Significant correlations were observed between responses to analgesics and several QST parameters including (1) heat pain threshold in experimental human pain, (2) electrical and heat pain thresholds, pressure pain tolerance and suprathreshold heat pain in surgical patients, and (3) electrical and heat pain threshold and conditioned pain modulation in patients with chronic pain. Heterogeneity among studies was observed especially with regard to application of QST and type and use of analgesics. Although promising, the current evidence is not sufficiently robust to recommend the use of any specific QST parameter in predicting analgesic response. Future studies should focus on a range of different experimental pain modalities rather than a single static pain stimulation paradigm.

  1. A Cost-Consequences analysis of the effect of Pregabalin in the treatment of peripheral Neuropathic Pain in routine medical practice in Primary Care settings

    Directory of Open Access Journals (Sweden)

    Torrades Sandra

    2011-01-01

    Full Text Available Abstract Background Neuropathic pain (NeP is a common symptom of a group of a variety of conditions, including diabetic neuropathy, trigeminal neuralgia, or postherpetic neuralgia. Prevalence of NeP has been estimated to range between 5-7.5%, and produces up to 25% of pain clinics consultations. Due to its severity, chronic evolution, and associated co-morbidities, NeP has an important individual and social impact. The objective was to analyze the effect of pregabalin (PGB on pain alleviation and longitudinal health and non-health resources utilization and derived costs in peripheral refractory NeP in routine medical practice in primary care settings (PCS in Spain. Methods Subjects from PCS were older than 18 years, with peripheral NeP (diabetic neuropathy, post-herpetic neuralgia or trigeminal neuralgia, refractory to at least one previous analgesic, and included in a prospective, real world, and 12-week two-visit cost-of-illness study. Measurement of resources utilization included both direct healthcare and indirect expenditures. Pain severity was measured by the Short Form-McGill Pain Questionnaire (SF-MPQ. Results One-thousand-three-hundred-fifty-four PGB-naive patients [58.8% women, 59.5 (12.7 years old] were found eligible for this secondary analysis: 598 (44% switched from previous therapy to PGB given in monotherapy (PGBm, 589 (44% received PGB as add-on therapy (PGB add-on, and 167 (12% patients changed previous treatments to others different than PGB (non-PGB. Reductions of pain severity were higher in both PGBm and PGB add-on groups (54% and 51%, respectively than in non-PGB group (34%, p Conclusion In Spanish primary care settings, PGB given either add-on or in monotherapy in routine medical practice was associated with pain alleviation leading to significant longitudinal reductions in resource use and total costs during the 12-week period of the study compared with non-PGB-therapy of patients with chronic NeP of peripheral origin. The use of non-appropriate analgesic therapies for neuropathic pain in a portion of subjects in non-PGB group could explain partially such findings.

  2. EXPERIMENTAL EVALUATION FOR ANALGESIC ACTIVITY OF MAMSYADI KWATHA

    OpenAIRE

    Shreevathsa,; Ravishankar B; Dwivedi R. R; Rao Ravi S; Krishnamurthy M.S.

    2011-01-01

    Siddha Yoga Sangraha of Yadavji Trikamji Acharya, states about Mamsyadi kwatha, an Ayurvedic formulation which is said to be effective in minor mental disorders. The ingredients of Mamsyadi kwatha are Jatamamsi (Nardistachys jatamansi DC), Ashwagandha (Withania somnifera Linn) and Parasika yavani (Hyoscymus niger Linn), in 8:4:1 ratio respectively. The test formulation was subjected to assess its analgesic effect. The model selected for the assessment of analgesic effect was tail flick test, ...

  3. Effect of Peripheral Communication Pace on Attention Allocation in a Dual-Task Situation

    Science.gov (United States)

    Gueddana, Sofiane; Roussel, Nicolas

    Peripheral displays allow continuous awareness of information while performing other activities. Monitoring such a display while performing a central task has a cognitive cost that depends on its perceptual salience and the distraction it causes, i.e. the amount of attention it attracts away from the user’s primary action. This paper considers the particular case of peripheral displays for interpersonal communication. It reports on an experiment that studied the effect of peripheral communication pace on subjects’ allocation of attention in a dual-task situation: a snapshot-based peripheral monitoring task where participants need to assess the presence of a remote person, and a central text-correcting task against the clock. Our results show that the addition of the peripheral task caused a drop in the success rate of the central task. As the pace of snapshots increased, success rate decreased on the peripheral task while on the central one, success rate remained the same but failures to reply in time occurred more frequently. These results suggest that the increase in pace of snapshots caused participants to change their strategy for the central task and allocate more attention to the peripheral one, not enough to maintain peripheral performance but also not to the point where it would affect central performance. Overall, our work suggests that peripheral communication pace subtly influences attention allocation in dual-task situations. We conclude by discussing how control over information pace could help users of communication systems to adjust their local distraction as well as the attention they draw from remote users.

  4. Analgesic, Sedative and Hemodynamic Effects of Dexmedetomidine Following Major Abdominal Surgeries: A Randomized, Double Blinded Comparative Study with Morphine

    Directory of Open Access Journals (Sweden)

    Khaled Taha

    2003-09-01

    Full Text Available This was a randomized double-blinded study; in which 60 ASAI-II adult patients scheduled for major abdominal surgeries (colostomy, radical cystectomy, major gynecological surgery, and abdominal vascular surgery were received standard general anesthesia. Twenty minutes before the anticipated end of surgery, patients were randomized into two equal groups: dexmedetomidine group (group D and morphine group (group M. Group D received dexmedetomidine IV infusion 4µg/kg/h for 15 minutes (1µg/Kg followed by 0.4µg/kg/h for 3h. Group M received morphine sulfate IV (0.07mg/kg. All patients were given a morphine patient controlled analgesia (PCA pump in the post anesthesia care unit (PACU, delivering IV morphine 2mg with a lockout time of 5 minutes if pain score assessed through visual analog scale (VAS was more than 5 at any given 5-min assessment. During the PACU recovery period, morphine consumption; pain and sedation scores; hemodynamic variables (heart rate, mean arterial blood pressure, oxygen saturation and respiratory rate; and postoperative nausea, retching and vomiting (PONV were recorded every 30 min for 3h (study period by a member of staff blinded to the treatment. The study demonstrated that the use of dexmedetomidine led to significant decrease in the total amount of morphine consumed throughout the entire PACU recovery period (P0.05; significant decrease in mean arterial pressure (P0.05; without any significant changes in oxygen saturation (P<0.05 or respiratory rate (P<0.05. In conclusion, dexmedetomidine exhibited both analgesic and sedative properties. The associated cardiovascular protective pharmacological profile and the lack of respiratory depression made it potentially extremely interesting for postoperative analgesia after major abdominal surgeries.

  5. The protective effects of lafutidine for bortezomib induced peripheral neuropathy

    Directory of Open Access Journals (Sweden)

    Tsukaguchi M

    2013-07-01

    Full Text Available Machiko Tsukaguchi, Masaru Shibano, Ai Matsuura, Satoru MukaiDepartment of Hematology,Sakai City Hospital, Osaka, JapanAbstract: Peripheral neuropathy (PN caused by bortezomib is an important complication of multiple myeloma. Subcutaneous injection of bortezomib reduced PN, but 24% of cases were grade 2 PN and 6% of cases were grade 3 PN. PN higher than grade 2 was not resolved by subcutaneous injection. PN higher than grade 3 has serious dose limiting toxicity and is the cause of discontinuing bortezomib treatment. Lafutidine is an H2-blocker with gastroprotective activity and is thought to function by increasing mucosal blood flow via capsaicin sensitive neurons. The same activity of lafutidine is considered to improve glossodynia and taxane induced PN. We hypothesized that lafutidine prevents or improves PN that is caused by bortezomib. In the current study, bortezomib was administered in the usual manner (intravenous administration of bortezomib 1.3 mg/m2, twice a week for 2 weeks, followed by 1 week without treatment for up to four cycles to compare our data with other studies. Lafutidine was administered orally at a dose of 10 mg twice daily. In our eight evaluated cases, the total occurrence of PN was four out of eight patients (50%. There were only grade 1 PN (4 out of 8 cases, and no cases higher than grade 2. We conclude that (1 the total occurrence of PN was not improved, (2 there was no PN after the first course, (3 there were only grade 1 cases and there were no cases higher than grade 2, and (4 no cases discontinued bortezomib treatment because of PN. This is the first report showing that lafutidine is useful for the amelioration of bortezomib induced PN.Keywords: bortezomib induced peripheral neuropathy, lafutidine, capsaicin sensitive neurons, calcitonin gene-related peptide, transient receptor potential 1, multiple myeloma

  6. The effect of spatial frequency on peripheral collinear facilitation.

    Science.gov (United States)

    Maniglia, Marcello; Pavan, Andrea; Trotter, Yves

    2015-02-01

    The detection of a Gabor patch (target) can be decreased or improved by the presence of co-oriented Gabor patches (flankers) having the same spatial frequency as the target. These phenomena are thought to be mediated by lateral interactions. Depending on the distance between target and flankers, commonly defined as a multiple of the wavelength (?) of the carrier, flankers can increase or decrease a target's detectability. Studies with foveal presentation showed that for target-to-flankers distances 3? contrast thresholds decrease. Earlier studies on collinear facilitation at the near-periphery of the visual field (4° of eccentricity) showed inconsistent facilitation (Shani & Sagi, 2005, Vision Research, 45, 2009-2024) whereas more recent studies showed consistent facilitation for larger separations (7-8?) (Maniglia et al., 2011, PLoS ONE, 6, e25568; Lev & Polat, 2011, Vision Research, 51, 2488-2498). However, all of these studies used medium-to-high spatial frequencies (3-8cpd). In this study we tested lower spatial frequencies (1, 2, and 3cpd) with different target-to-flankers distances. The rationale was that near-peripheral vision is tuned for lower spatial frequencies and this could be reflected in collinear facilitation. Results show consistent collinear facilitation at 8? for all the spatial frequencies tested, but also show collinear facilitation at shorter target-to-flanker distance (6?) for the lowest spatial frequencies tested (1cpd). Additionally, collinear facilitation decreases as spatial frequency increases; opposite to the findings of Polat (2009, Spatial Vision, 22, 179-193) in the fovea, indicating a different spatial frequency tuning between foveal and peripheral lateral interactions. PMID:25557179

  7. Invention of Analgesic and Anti-Inflammatory Activity of Ethanolic Extract of Mimosa Pudica

    Directory of Open Access Journals (Sweden)

    Dr. Chandrashekar D. K.

    2012-07-01

    Full Text Available The ethanolic extract of the leaves of Mimosa pudica at the doses of 200 and 400mg/kg was tested for anti-inflammatory and analgesic activity. The extract produced dose dependent and significant inhibition of carrageenan induced paw oedema.The analgesic activity was found to be more significant on the acetic acid induced writhing model (p<0.001 than the tail flick model (p<0.001. So the extract inhibits predominantly the peripheral mechanism. The presence of flavonoids in the ethanolic extract may be contributory to its analgesic and anti-inflammatory activity.

  8. The adjuvant effect of hypertension upon diabetic peripheral neuropathy in experimental type 2 diabetes.

    Science.gov (United States)

    De Visser, Adriena; Hemming, Amanda; Yang, Christina; Zaver, Shaila; Dhaliwal, Raj; Jawed, Zaid; Toth, Cory

    2014-02-01

    Type 2 diabetes (DM) is the most common cause of peripheral neuropathy in the Western world. A comorbidity, hypertension, has been speculated to contribute to initiation or worsening of diabetic peripheral neuropathy. We studied adult rat models using genetic strains with DM (Zucker Diabetic Fat rats)±hypertension (HTN (ZSF-1 rats)) to investigate the relative contributions of DM and HTN and the potential for additive effects of HTN upon existing DM for the development of peripheral neuropathy. Long duration sensorimotor behavioral and electrophysiological testing was complemented by histological and molecular methods. Only DM led to tactile and thermal hyperalgesia and affected motor nerve electrophysiology. Although DM led to marked loss of sensory amplitudes and to sensory conduction slowing, a mild additive effect from HTN contributed after 6months of DM with worsening of slowing of sensory nerve conduction velocities, but without effect upon sensory amplitudes. At the sensory dominant sural nerve, mild (diabetic peripheral neuropathy at sensory peripheral nerve fibers manifesting with the loss of myelin thickness. PMID:23938761

  9. The peripheral antinociceptive effect induced by morphine is associated with ATP-sensitive K(+) channels.

    Science.gov (United States)

    Rodrigues, A R; Duarte, I D

    2000-01-01

    The effect of several K(+) channel blockers such as glibenclamide, tolbutamide, charybdotoxin (ChTX), apamin, tetraethylammonium (TEA), 4-aminopyridine (4-AP) and cesium on the peripheral antinociceptive effect of morphine was evaluated by the paw pressure test in Wistar rats. The intraplantar administration of a carrageenan suspension (250 microg) resulted in an acute inflammatory response and a decreased threshold to noxious pressure. Morphine administered locally into the paw (25, 50, 100 and 200 microg) elicited a dose-dependent antinociceptive effect which was demonstrated to be mediated by a peripheral site up to the 100 microg dose. The selective blockers of ATP-sensitive K(+) channels glibenclamide (20, 40 and 80 microg paw(-1)) and tolbutamide (40, 80 and 160 microg paw(-1)) antagonized the peripheral antinociception induced by morphine (100 microg paw(-1)). This effect was unaffected by ChTX (0. 5, 1.0 and 2.0 microg paw(-1)), a large conductance Ca(2+)-activated K(+) channel blocker, or by apamin (2.5, 5.0 and 10.0 microg paw(-1)), a selective blocker of a small conductance Ca(2+)-activated K(+) channel. Intraplantar administration of the non-specific K(+) channel blockers TEA (160, 320 and 640 microg), 4-AP (10, 50 and 100 microg) and cesium (125, 250 and 500 microg) also did not modify the peripheral antinociceptive effect of morphine. These results suggest that the peripheral antinociceptive effect of morphine may result from activation of ATP-sensitive K(+) channels, which may cause a hyperpolarization of peripheral terminals of primary afferents, leading to a decrease in action potential generation. In contrast, large conductance Ca(2+)-activated K(+) channels, small conductance Ca(2+)-activated K(+) channels as well as voltage-dependent K(+) channels appear not to be involved in this transduction pathway. British Journal of Pharmacology (2000) 129, 110 - 114 PMID:10694209

  10. Opioid peptide-derived analgesics

    OpenAIRE

    Schiller, Peter W.

    2005-01-01

    Two recent developments of opioid peptide-based analgesics are reviewed. The first part of the review discusses the dermorphin-derived, cationic-aromatic tetrapeptide H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA, where Dmt indicates 2?,6?-dimethyltyrosine), which showed subnanomolar ? receptor binding affinity, extraordinary ? receptor selectivity, and high ? agonist potency in vitro. In vivo, [Dmt1]DALDA looked promising as a spinal analgesic because of its extraordinary antinociceptive effec...

  11. The Analgesic Potential of Cannabinoids

    OpenAIRE

    Elikottil, Jaseena; Gupta, Pankaj; Gupta, Kalpna

    2009-01-01

    Historically and anecdotally cannabinoids have been used as analgesic agents. In recent years, there has been an escalating interest in developing cannabis-derived medications to treat severe pain. This review provides an overview of the history of cannabis use in medicine, cannabinoid signaling pathways, and current data from preclinical as well as clinical studies on using cannabinoids as potential analgesic agents. Clinical and experimental studies show that cannabis-derived compounds act ...

  12. Analgesic activity of diterpene alkaloids from Aconitum baikalensis.

    Science.gov (United States)

    Nesterova, Yu V; Povet'yeva, T N; Suslov, N I; Zyuz'kov, G N; Pushkarskii, S V; Aksinenko, S G; Schultz, E E; Kravtsova, S S; Krapivin, A V

    2014-08-01

    We compared analgesic activities of individual alkaloids extracted from Baikal aconite (Aconitum baikalensis): napelline, hypaconitine, songorine, mesaconitine, 12-epinapelline N-oxide. The detected analgesic activity was comparable to that of sodium metamizole. The mechanisms of analgesia were different in diterpene alkaloids of different structure. The antinociceptive effect of atisine alkaloids (12-epinapelline N-oxide, songorine) was naloxonedependent and realized via opioid receptor modulation. PMID:25110090

  13. Drug Therapy in Dental Practice: Nonopioid and Opioid Analgesics

    OpenAIRE

    Becker, Daniel E.; Phero, James C.

    2005-01-01

    To prevent patient pain, the clinician may chose from opioid and nonopioid analgesics. It is rational for the practitioner to combine drugs from these classes when managing moderate to severe pain. To select combination regimens wisely, it is necessary to understand the significant pharmacological features of each category alone. Careful selection of an effective analgesic regimen based on the type and amount of pain the patient is expected to have can prevent the stress and anxiety associate...

  14. Analgesic and hypnotic activities of Laghupanchamula: A preclinical study

    Science.gov (United States)

    Ghildiyal, Shivani; Gautam, Manish K.; Joshi, Vinod K.; Goel, Raj K.

    2014-01-01

    Background: In Ayurvedic classics, two types of Laghupanchamula -five plant roots (LP) have been mentioned containing four common plants viz. Kantakari, Brihati, Shalaparni, and Prinshniparni and the fifth plant is either Gokshura (LPG) or Eranda (LPE). LP has been documented to have Shothahara (anti-inflammatory), Shulanashka (analgesic), Jvarahara (antipyretic), and Rasayana (rejuvenator) activities. Aim: To evaluate the acute toxicity (in mice), analgesic and hypnotic activity (in rats) of 50% ethanolic extract of LPG (LPGE) and LPE (LPEE). Materials and Methods: LPEG and LPEE were prepared separately by using 50% ethanol following the standard procedures. A graded dose (250, 500 and 1000 mg/kg) response study for both LPEE and LPGE was carried out for analgesic activity against rat tail flick response which indicated 500 mg/kg as the optimal effective analgesic dose. Hence, 500 mg/kg dose of LPEE and LPGE was used for hot plate test and acetic acid induced writhing model in analgesic activity and for evaluation of hypnotic activity. Results: Both the extracts did not produce any acute toxicity in mice at single oral dose of 2.0 g/kg. Both LPGE and LPEE (250, 500, and 1000 mg/kg) showed dose-dependent elevation in pain threshold and peak analgesic effect at 60 min as evidenced by increased latency period in tail-flick method by 25.1-62.4% and 38.2-79.0% respectively. LPGE and LPEE (500 mg/kg) increased reaction time in hot-plate test at peak 60 min analgesic effect by 63.2 and 85.8% and reduction in the number of acetic acid-induced writhes by 55.9 and 65.8% respectively. Both potentiated pentobarbitone-induced hypnosis as indicated by increased duration of sleep in treated rats. Conclusion: The analgesic and hypnotic effects of LP formulations authenticate their uses in Ayurvedic system of Medicine for painful conditions. PMID:25364205

  15. Comparative study of analgesic effect of the infrared low-intensity laser and 33% sodium fluoride paste in the treatment of dentinal hypersensitivity

    International Nuclear Information System (INIS)

    Different desensitizing agents have been used in the treatment of dentinal hypersensitivity, however, some presented treatments are still frustrating. The purpose of this study was to evaluate the analgesic effect of the low-intensity GaAlAs laser (?= 830 nm) in the treatment of dentinal hypersensitivity after mechanical and thermal stimuli, and compared it with the 33% sodium fluoride paste. Thirty two teeth with dentinal hypersensitivity were selected and randomly divided into two groups. For the laser group, each tooth was irradiated by a dose of 6 J/cm2 during two minutes and half on the buccal side. The paste group was treated with a NaF/kaolin/glycerin (33:33:33) paste by burnishing the sensitive surface during four minutes. The sensitivity degree was measured before the beginning of the experiment, 24 h, 48 h, 72 h, 120 h, 15 days and 30 days after the first application. The results indicate that the dentinal hypersensitivity significantly diminished for the paste group after dental explorer. Regarding to air-blast, no significant differences were observed between the groups. Both of them were effective in reducing pain of the dentine hypersensitive after 120 h. (author)

  16. Peripheral benzodiazepine binding sites on striated muscles of the rat: Properties and effect of denervation

    International Nuclear Information System (INIS)

    In order to test the hypothesis that peripheral benzodiazepine binding sites mediate some direct effects of benzodiazepines on striated muscles, the properties of specific 3H-Ro 5-4864 binding to rat biceps and rat diaphragm homogenates were investigated. In both tissues a single population of sites was found with a Ksub(D) value of 3 nmol/l. The density of these sites in both muscles was higher than the density in rat brain, but was considerably lower than in rat kidney. Competition experiments indicate a substrate specificity of specific 3H-Ro 5-4864 binding similar to the properties already demonstrated for the specific binding of this ligand to peripheral benzodiazepine binding sites in many other tissues. The properties of these sites in the rat diaphragm are not changed after motoric denervation by phrenicectomy. It is concluded that peripheral benzodiazepine binding sites are not involved in direct effects of benzodiazepines on striated muscles. (Author)

  17. Effects of hyperbaric oxygen (HBO) treatment on chromosome aberrations in peripheral lymphocytes in rabbits induced by ?-ray irradiation

    International Nuclear Information System (INIS)

    Effect of hyperbaric oxygen (HBO) treatment on chromosome aberrations in peripheral lymphocytes in rabbits induced by 60Co ?-rays irradiation were studied. It was found that there is no effect of HBO itself on chromosomes in peripheral lymphocytes, and definite promotion effect of HBO treatment on recovery of chromosome damage in preipheral lymphocytes in rabbits induced by irradiation

  18. Activation of Central, But Not Peripheral, Estrogen Receptors Is Necessary for Estradiol’s Anorexigenic Effect in Ovariectomized Rats

    OpenAIRE

    Rivera, Heidi M.; Eckel, Lisa A.

    2010-01-01

    Estradiol appears to exert its anorexigenic effect by activating nuclear estrogen receptors (ERs), which are expressed widely in peripheral tissues and in the brain. Here, we used ICI-182,780 (ICI), a pure antiestrogen with limited ability to cross the blood-brain barrier, to assess the relative involvement of peripheral vs. central ERs to estradiol’s anorexigenic effect. Food intake was measured after peripheral (sc) administration of ICI or vehicle in ovariectomized rats treated with acut...

  19. Analgesic therapy of skeletal metastases with radionuclides

    International Nuclear Information System (INIS)

    The radionculide therapy of bone metastases is an unspecific palliative treatment of metastatic skeletal pain especially useful in patients suffering in multiple sites. In these cases the long-term administration of increasing doses of analgesics such as opiate which have important side effects can be reduced. The aim of this therapy is pain relief and improvement of quality of life in patients with advanced cancer. This report is focusing on options, indications and contraindications of the radionuclide therapy of metastases and on used radionuclides such as Strontium-89, Yttrium-90, Rhenium-186 (188) and Samarium-153. In oncology, the analgesic therapy using boneseeking radiopharmaceuticals in combination to drug administration should gain more importance because this therapy can be administered on an outpatient basis. (orig.)

  20. Analgesic and anti-inflammatory activity of Crinum glaucum aqueous extract.

    Science.gov (United States)

    Okpo, S O; Fatokun, F; Adeyemi, O O

    2001-12-01

    The anti-inflammatory and analgesic effects of the aqueous extract of Crinum glaucum were evaluated in mice and rats using the carrageenan- and dextran-induced paw oedema, acetic acid-induced writhing, cold water tail flick and formalin pain tests. The extract (100-400 mg/kg) and acetylsalicylic acid (100 mg/kg) produced a significant (P<0.05) inhibition of the second phase response in the formalin pain model, while only the high dose (400 mg/kg) of the extract showed an antinociceptive effect in the first phase. The extract also showed a dose-dependent inhibition of acetic acid-induced abdominal writhes. The tail flick latency was dose dependently enhanced by the extract but this was significantly (P<0.05) lower than that produced by morphine (2 mg/kg). The extract (125-500 mg/kg) administered 1 h before or after carrageenan-induced paw swelling produced a dose dependent inhibition of the oedema. No effect was observed with the dextran-induced oedema model. The data obtained suggest that the anti-inflammatory and analgesic effects of the extract may be mediated via both peripheral and central mechanisms. PMID:11694366

  1. Prolonged analgesic response of cornea to topical resiniferatoxin, a potent TRPV1 agonist.

    Science.gov (United States)

    Bates, Brian D; Mitchell, Kendall; Keller, Jason M; Chan, Chi-Chao; Swaim, William D; Yaskovich, Ruth; Mannes, Andrew J; Iadarola, Michael J

    2010-06-01

    Analgesics currently available for the treatment of pain following ophthalmic surgery or injury are limited by transient effectiveness and undesirable or adverse side effects. The cornea is primarily innervated by small-diameter C-fiber sensory neurons expressing TRPV1 (transient receptor potential channel, subfamily V, member 1), a sodium/calcium cation channel expressed abundantly by nociceptive neurons and consequently a target for pain control. Resiniferatoxin (RTX), a potent TRPV1 agonist, produces transient analgesia when injected peripherally by inactivating TRPV1-expressing nerve terminals through excessive calcium influx. The aim of the present study was to evaluate topical RTX as a corneal analgesic. In rat cornea, a single application of RTX dose dependently eliminated or reduced the capsaicin eye wipe response for 3-5 days, with normal nociceptive responses returning by 5-7 days. RTX alone produced a brief but intense noxious response, similar to capsaicin, necessitating pretreatment of the cornea with a local anesthetic. Topical lidocaine, applied prior to RTX, blocks acute nociceptive responses to RTX without impairing the subsequent analgesic effect. Importantly, RTX analgesia (a) did not impair epithelial wound healing, (b) left the blink reflex intact and (c) occurred without detectable histological damage to the cornea. Immunohistochemistry showed that loss of CGRP immunoreactivity, a surrogate marker for TRPV1-expressing fibers, extended at least to the corneal-scleral boundary and displayed a progressive return, coincident with the return of capsaicin sensitivity. These data suggest that RTX may be a safe and effective treatment for post-operative or post-injury ophthalmic pain. PMID:20403666

  2. Transdermal therapeutic system of narcotic analgesics using nonporous membrane (I) : Effect of the ethanol permeability on vinylacetate content of EVA membrane

    Energy Technology Data Exchange (ETDEWEB)

    Kwon, H.; Song, H.Y. [Chungnam National University, Taejon (Korea); Khang, G.S. [Chonbuk National University, Chonju (Korea); Lee, H.B. [Korea Research Institute of Chemical Technology, Taejon (Korea)

    1999-05-01

    The fundamental properties of transdermal therapeutic patch as narcotic analgesics agent has been investigated. From the study of drug and ethanol release patterns from the fentanyl base (FB) patches through diffusion cell and hairless mouse skin, it was observed that the FB release patterns were largely affected by the content of vinyl acetate (VA) of ethylene-co-vinyl acetate (EVA) membrane, and volume fraction of ethanolic solution. Additionally, a variety of control membrane as a function of VA content were examined for swelling following equilibration with ethanolic solutions. Generally, ethanol was incorporated into a transdermal therapeutic device to enable the controlled delivery of enhancer and drug to the skin surface. In vitro skin permeation analysis of the control membrane showed that ethanol flux was linearly related to the ethanol volume fraction. This result was shown that drug permeability increased with increasing as the content of VA. But, the FB flux from saturated aqueous ethanol solutions increases until 80% ethanol volume fraction. Over 80% ethanol volume fraction, the FB flux through skin samples is independent of ethanol volume. These results showed that the decrease in skin permeation due to dehydration nis the dominant effect. 26 refs., 8 figs.

  3. Effects of exposure to different types of radiation on behaviors mediated by peripheral or central systems

    Science.gov (United States)

    Rabin, B. M.; Joseph, J. A.; Erat, S.

    1998-01-01

    The effects of exposure to ionizing radiation on behavior may result from effects on peripheral or on central systems. For behavioral endpoints that are mediated by peripheral systems (e.g., radiation-induced conditioned taste aversion or vomiting), the behavioral effects of exposure to heavy particles (56Fe, 600 MeV/n) are qualitatively similar to the effects of exposure to gamma radiation (60Co) and to fission spectrum neutrons. For these endpoints, the only differences between the different types of radiation are in terms of relative behavioral effectiveness. For behavioral endpoints that are mediated by central systems (e.g., amphetamine-induced taste aversion learning), the effects of exposure to 56Fe particles are not seen following exposure to lower LET gamma rays or fission spectrum neutrons. These results indicate that the effects of exposure to heavy particles on behavioral endpoints cannot necessarily be extrapolated from studies using gamma rays, but require the use of heavy particles.

  4. Corticotropin-releasing-hormone lacks analgesic properties: an experimental study in humans, using non-inflammatory pain.

    Science.gov (United States)

    Lautenbacher, S; Roscher, S; Kohl, G; Vedder, H; Krieg, J

    1999-10-01

    The antinociceptive potency of corticotropin-releasing-hormone (CRH) has been established in several animal studies in which both central and peripheral sites of action were considered. However, there have not yet been any experimental trials, besides one attempt using clinical dental pain demonstrating the potential analgesic properties of CRH in humans. For this reason, we studied the effect of CRH on experimental heat pain sensitivity in 18 healthy men, using a double-blind, cross-over and placebo-controlled design. A dose of 100 microg (i.v.) was chosen because of its well-known neuroendocrine effects in humans. The pain parameters assessed were, visual analog scale (VAS) ratings for pain intensity and pain unpleasantness, pain thresholds and scores for discrimination ability. To differentiate between a direct analgesic effect of CRH and indirect effects via evoked hormonal responses in the hypothalamic-pituitary-adrenocortical (HPA) system (beta-endorphin, ACTH, cortisol), CRH was applied with and without a pre-treatment with dexamethasone. In neither of the two conditions was there any systematic change in our pain parameters. This failure to find any evidence suggesting an analgesic action of CRH or of the subsequent hormones of the HPA system was obtained despite the fact that CRH produced clear neuroendocrine responses such as increases in the plasma concentration of beta-endorphin and cortisol. It is unclear whether the lack of analgesic action of CRH is due to its non-existence in humans, due to the use of a pain model which does not assess minute changes in pain sensitivity and does not trigger substantial inflammatory responses, or due to an insufficient dose of CRH. PMID:10506666

  5. Combined Effects of Gamma Radiation and High Dietary Iron on Peripheral Leukocyte Distribution and Function

    Science.gov (United States)

    Crucian, Brian E.; Morgan, Jennifer L. L.; Quiriarte, Heather A.; Sams, Clarence F.; Smith, Scott M.; Zwart, Sara R.

    2012-01-01

    Both radiation and increased iron stores can independently increase oxidative damage, resulting in protein, lipid and DNA oxidation. Oxidative stress increases the risk of many health problems including cancer, cataracts, and heart disease. This study, a subset of a larger interdisciplinary investigation of the combined effect of iron overload on sensitivity to radiation injury, monitored immune parameters in the peripheral blood of rats subjected to gamma radiation, high dietary iron or both. Specific immune measures consisted of: (1) peripheral leukocyte distribution, (2) plasma cytokine levels and (3) cytokine production profiles following whole blood mitogenic stimulation

  6. The effects of peripheral message cues on clinicians' judgments about clients' psychological status.

    Science.gov (United States)

    Brewer, Neil; Barnes, John; Sauer, James

    2011-03-01

    This research examined the influence of peripheral message cues on clinicians' judgment about the psychological status of clients. The elaboration likelihood model (ELM) of social persuasion suggests that peripheral message cues are likely to exert a greater influence on clinicians' judgments when a client's presentation meets some, but not all, diagnostic criteria for a disorder (i.e., when the presentation is ambiguous). Within this theoretical framework, we examined the effects of a peripheral message cue (level of irrelevant detail in the client's presentation) and presentation ambiguity on clinicians' judgments of need for treatment, illness severity, and distress. Consistent with predictions based on the ELM, for both obsessive-compulsive disorder and post-traumatic stress disorder presentations, high levels of irrelevant detail exerted a greater influence on clinicians' judgments of clients' need for treatment when presentation ambiguity was high than when it was low. PMID:21332521

  7. Acid increases inflammatory pain in rats: effect of local peripheral ASICs inhibitors.

    Science.gov (United States)

    Rocha-González, Héctor I; Herrejon-Abreu, Emma B; López-Santillán, Francisco J; García-López, Blanca E; Murbartián, Janet; Granados-Soto, Vinicio

    2009-01-28

    The purpose of this study was to assess the possible antinociceptive effect of the acid sensing ion channels (ASICs) inhibitors amiloride and benzamil after local peripheral administration in three models of inflammatory pain in rats. Reduction of pH, from 7.4 to 5.8 units, significantly increased the flinching/licking behavior induced by either 0.1% serotonin, 0.1% capsaicin or 0.5% formalin. Local peripheral ipsilateral, but not contralateral, injection of amiloride or benzamil significantly reduced nociceptive behaviors (flinching and licking/lifting) induced by serotonin, capsaicin or formalin in acidic conditions (pH 6.2). Interestingly, benzamil produced antinociception at low doses (0.001-0.1 microM/paw) while higher doses (1 microM/paw) did not affect capsaicin- or formalin-induced licking/lifting. Our data suggest that local peripheral inhibition of ASICs play an important role in inflammatory pain. PMID:19109946

  8. Developmental Effects on the Reception of Signs in Peripheral Vision by Deaf Students.

    Science.gov (United States)

    Swisher, M. Virginia

    1990-01-01

    Replication of a study that showed that deaf 15- to 18-year- olds could accurately identify a significant number of isolated signs presented well out in peripheral vision found that 8- to 12-year-olds could also identify such signs, although results showed a significant effect of age on performance. (Author/CB)

  9. The analgesic effect of combined treatment with intranasal S-ketamine and intranasal midazolam compared with morphine patient-controlled analgesia in spinal surgery patients: a pilot study

    Science.gov (United States)

    Riediger, Christine; Haschke, Manuel; Bitter, Christoph; Fabbro, Thomas; Schaeren, Stefan; Urwyler, Albert; Ruppen, Wilhelm

    2015-01-01

    Objectives Ketamine is a well-known analgesic and dose-dependent anesthetic used in emergency and disaster medicine. Recently, a new formulation of S-ketamine, as an intranasal spray, was developed and tested in our institution in healthy volunteers. The authors investigated the effect of intranasal S-ketamine spray combined with midazolam intranasal spray in postoperative spinal surgery patients. Materials and methods In this prospective, computer-randomized, double-blinded noninferiority study in spinal surgery patients, the effects of intranasal S-ketamine and midazolam were compared with standard morphine patient-controlled analgesia (PCA). The primary end point was the numeric rating scale pain score 24 hours after surgery. Results Twenty-two patients finished this study, eleven in each group. There were similar numeric rating scale scores in the morphine PCA and the S-ketamine-PCA groups at 1, 2, 4, 24, 48, and 72 hours after surgery during rest as well as in motion. There were no differences in the satisfaction scores at any time between the groups. The number of bolus demands and deliveries was not significantly different. Discussion In our study, we found that an S-ketamine intranasal spray combined with intra-nasal midazolam was similar in effectiveness, satisfaction, number of demands/deliveries of S-ketamine and morphine, and number/severity of adverse events compared with standard intravenous PCA with morphine. S-ketamine can be regarded as an effective alternative for a traditional intravenous morphine PCA in the postoperative setting. PMID:25709497

  10. Effects of transgene-mediated endomorphin-2 in inflammatory pain

    OpenAIRE

    Hao, Shuanglin; Wolfe, Darren; Glorioso, Joseph C.; Mata, Marina; Fink, David J.

    2008-01-01

    We examined the analgesic properties of endomorphin-2 expressed in DRG neurons transduced with a non-replicating herpes simplex virus (HSV)-based vector containing a synthetic endomorphin-2 gene construct. HSV-mediated endomorphin-2 expression reduced nocisponsive behaviors in response to mechanical and thermal stimuli after injection of complete Freund’s adjuvant (CFA) into the paw, and reduced peripheral inflammation measured by paw swelling after injection of CFA. The analgesic effect of...

  11. Effect of Peripheral Arterial Disease on Serum Ischemia-Modified Albumin Levels in Type 2 Diabetic Patients

    OpenAIRE

    Tugra Gencpinar; Umut Ayo?lu; Koray Aykut; Gokhan Albayrak; Hamid Ya?ar Ellidag; Muzaffer Y?lmaz; Kadir Sa?d?ç; Mustafa Emmiler

    2014-01-01

    Background: The aim of this study is to evaluate the role of IMA and the effect of Type-2 diabetes in peripheral arterial ischemic patient. Methods: In our study, randomized patient groups to be undergone peripheral surgery, consisting of 16 diabetic and 12 non-diabetic patients diagnosed with peripheral arterial disease, have been examined. After standard anesthesia, the surgery was performed by the same surgical team, blood samples were taken before and after cross-clamp, and the levels of ...

  12. Analgesic effect of percutaneously absorbed non-steroidal anti-inflammatory drugs: an experimental study in a rat acute inflammation model

    Directory of Open Access Journals (Sweden)

    Kikuchi Shin-ichi

    2008-01-01

    Full Text Available Abstract Background External medication that is absorbed percutaneously may be used to reduce inflammation and relieve pain from acute injuries such as ankle sprains and bruises. The plaster method of percutaneous absorption for non-steroidal anti-inflammatory drugs (NSAIDs was established in Japan in 1988. However, due to the possibility of a placebo effect, the efficacy of this method remains unclear. This experimental study was conducted to control for the placebo effect and to study the efficacy of the plaster method in relieving pain by using a rat model of inflammation. Methods Male Wistar-Imamichi rats were used. A yeast suspension was injected into the right hind paw to induce inflammation. A sheet (2.0 × 1.75 cm containing the drug was adhered to the inflamed paw. Five treatment groups were used, and each sheet contained a single drug: loxoprofen sodium (loxoprofen-Na (2.5 mg; felbinac (1.75 mg; indomethacin (1.75 mg; ketoprofen (0.75 mg; or base only (control, 0 mg. Mechanical pain threshold, expression of c-Fos in the dorsal horn, and amount of prostaglandin (PG E2 in the inflamed paw were evaluated. Results Pain threshold increased after treatment, and was significantly increased in the loxoprofen-Na group compared with the control group (p 2 were significantly decreased in the loxoprofen-Na and indomethacin groups compared with the control group (p p Conclusion Percutaneously absorbed NSAIDs have an analgesic effect, inhibit expression of c-Fos in the dorsal horn, and reduce PGE2 in inflamed tissue, indicating the efficacy of this method of administration for acute inflammation and localized pain.

  13. Comparison of the analgesic effect of ibuprofen with mesalamine after discectomy surgery in patients with lumbar disc herniation: A double-blind randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Toroudi Hamidreza

    2009-01-01

    Full Text Available Background: Pain management is an important component in the postoperative period following discectomy. Aims: We hypothesized that mesalamine considering its better safety profile, is likely to be a better choice, if it would be as effective as ibuprofen in controlling post-discectomy pain. Settings and Design: A double-blind randomized controlled trial was performed on patients who underwent lumbar discectomy surgery. Materials and Methods: Of the 58 patients who had lumbar discectomy, 27 patients were randomized to oral ibuprofen 500 mg and 31 patients to mesalamine 400 mg, three times a day for nine days following surgery. There was no placebo group. Severity of pain was assessed by using 10- cm visual analogue scale (VAS, once before operation and for nine days after. Statistical Analysis: Mean ± SD pain scores were compared between groups and the statistical difference was estimated by Student?s test using SPSS (Version 13. We also calculated the power of each t-test. Repeated measure ANOVA was performed for measuring the effect of time. Results: The age range of the patients was 35 to 60 years (mean: 42.2 years. Mean ± SD preoperative pain scores for ibuprofen or mesalamine-treated groups were 7.852 ± 2.441 and 7.806 ± 2.892, respectively. At the end of day 9, mean ± SD of pain score was 2.704 ± 2.284 and 2.717 ± 2.273 for ibuprofen and mesalamine-treated groups respectively. Both drugs significantly reduced postoperative pain and there was no statistically significant difference between the two groups.Conclusions: Since both drugs showed almost equal analgesic effect, considering its safety profile mesalamine, seems to be the preferred choice to alleviate post-discectomy surgery pain.

  14. Effect of peripheral morphine in a human model of acute inflammatory pain.

    DEFF Research Database (Denmark)

    LillesØ, J; Hammer, N A

    2000-01-01

    Several studies have demonstrated the presence of opioid inducible receptors on peripheral nerves and peripheral antinociceptive effects of opioids. However, the effects of peripheral opioid administration in man are controversial. Our study used a randomized, double-blind, placebo-controlled, three-way crossover design in a human model of acute inflammatory pain (heat injury). We studied 18 healthy volunteers who each received morphine locally (2 mg), morphine systemically (2 mg), or placebo on three separate study days. The subjects received morphine infiltration subcutaneously (s.c.). 1 h before heat injury (47 degrees C, 7 min) and naloxone infiltration s.c. (0.2 mg) 2.5 h after the heat injury. Hyperalgesia to mechanical and heat stimuli were examined using von Frey hairs and thermodes, and pain was rated using a visual analogue scale. The burns produced significant hyperalgesia, but local morphine infiltration neither reduced pain during the burn, nor primary or secondary hyperalgesia to mechanical and heat stimuli after the burn. In conclusion, peripherally applied morphine had no acute antinociceptive effects in this human model of acute inflammatory pain.

  15. Influência da naloxona e metisergida sobre o efeito analgésico do laser em baixa intensidade em modelo experimental de dor Influencia de la naloxona y la metisergida sobre el efecto analgésico del láser en baja intensidad en modelo experimental de dolor Influence of naloxone and methysergide on the analgesic effects of low-level laser in an experimental pain model

    Directory of Open Access Journals (Sweden)

    André Peres e Serra

    2010-06-01

    Full Text Available JUSTIFICATIVA E OBJETIVOS: A fototerapia com laser (LPT é um método analgésico promissor, embora seu mecanismo de ação não seja totalmente conhecido. O objetivo deste estudo foi avaliar se a ação da LPT é dependente da ativação de receptores opioides ou serotoninérgicos periféricos. MÉTODO: Foram utilizados ratos Wistar machos. A dor produzida foi de caráter inflamatório, através da injeção de carragenina na pata posterior esquerda dos ratos. O laser utilizado foi o Photon Lase III em meio ativo InGaAIP (660 nm, fluência de 2,5 J.cm-2. Analisou-se a hiperalgesia mecânica utilizando filamentos de von Frey. Os animais foram separados em cinco grupos: Carragenina; Laser (LPT; Luz não coerente; LPT + Naloxona e LPT + Metisergida. RESULTADOS: A fototerapia com laser em baixa intensidade mostrou-se um método analgésico eficaz, enquanto o emprego de fonte de luz não coerente não mostrou ter efeito analgésico. O uso de naloxona bloqueou o efeito analgésico do LPT; já o uso de metisergida não afetou a analgesia do LPT. CONCLUSÕES: A LPT nos parâmetros utilizados apresentou efeito analgésico. A analgesia da LPT é mediada por receptores opioides periféricos. A LPT parece não interagir com receptores serotoninérgicos periféricos.JUSTIFICATIVA Y OBJETIVOS: La fototerapia con láser (LPT es un método analgésico promisorio, aunque su mecanismo de acción no se conozca en su totalidad. El objetivo de este estudio fue evaluar si la acción de la LPT es dependiente de la activación de receptores opioides o serotoninérgicos periféricos. MÉTODO: Se usaron ratones Wistar machos. El dolor generado fue de carácter inflamatorio, a través de la inyección de carragenina en la pata posterior izquierda de los ratones. El láser utilizado fue el GaIAsAl (660 nm, fluencia de 2,5 J.cm-2. Se analizó la hiperalgesia mecánica utilizando filamentos de von Frey. Los animales se dividieron en cinco grupos: Carragenina; Láser (LPT; Luz no coherente; LPT + Naloxona y LPT + Metisergida. RESULTADOS: La fototerapia con láser en baja intensidad demostró ser un método analgésico eficaz, mientras que el uso de la fuente de luz no coherente no demostró poseer ningún efecto analgésico. El uso de naloxona bloqueó el efecto analgésico del LPT, mientras que el uso de metisergida no afectó la analgesia del LPT. CONCLUSIONES: La LPT en los parámetros utilizados tuvo un efecto analgésico. La analgesia de la LPT es mediada por receptores opióides periféricos. La LPT parece que no interactúa con los receptores serotoninérgicos periféricos.BACKGROUND AND OBJECTIVES: Although the mechanism of action of laser phototherapy (LPT is not known, it is a promising analgesic method. The aim of this study was to evaluate whether the action of LPT depends on the activation of peripheral opioid or serotonergic receptors. METHOD: Inflammatory pain was induced through the injection of carrageenin in the left posterior paw of male Wistar rats. The InGaAIP visible laser diode (660 nm with fluency of 2.5 J.cm-2 was used. Von Frey filaments were used to analyze mechanical hyperalgesia. Animals were separated into five groups: Carrageenin; Laser (LPT; Non-coherent light; LPT + Naloxone; and LPT + Methysergide. RESULTS: Low-Level Laser phototherapy proved to be an effective analgesic method, while non-coherent light did not show a similar effect. The use of naloxone blocked the analgesic effect of LPT, while methysergide did not affect LPT-induced analgesia. CONCLUSIONS: According to the parameter used in this study, LPT produced analgesia. Analgesia induced by laser phototherapy is mediated by peripheral opioid receptors. Laser phototherapy does not seem to interact with peripheral serotonergic receptors.

  16. Pattern of use of analgesics in a surgical unit

    Directory of Open Access Journals (Sweden)

    Mohammad Abdullah Al Masud

    2009-06-01

    Full Text Available The present study was designed to evaluate the prescribing pattern of analgesics in post-operative patients in a surgical unit. Total number of 180 prescriptions containing analgesics was collected randomly. The only drug in the operation day that was used was pethidine (90.6%. Patients (9.4% did not receive any analgesics in the operation day. Associated analgesics in the operation day were either tramadol (42.2 % or ketorolac (54.4%. Only 3.3% did not receive any such drugs. In first post-operative day most of the patients received single drug tramadol (48.3%, ketorolac (38.9% and pethidine (0.6%. In second, third, forth and fifth post-operative day most patients received tramadol (47.8% (44.4%, (41.4% and (33.2% respectively. In sixth post-operative day most of the patients (81.1% did not receive any analgesics. In this study tramadol was found to be widely used post-operative analgesics with minimal side effects and better adherence to this drug by the patient.

  17. Role of analgesics, sedatives, neuromuscular blockers, and delirium.

    Science.gov (United States)

    Hall, Jesse B; Schweickert, William; Kress, John P

    2009-10-01

    A major focus on critical care medicine concerns the institution of life-support therapies, such as mechanical ventilation, during periods of organ failure to permit a window of opportunity to diagnose and treat underlying disorders so that patients may be returned to their prior functional status upon recovery. With the growing success of these intensive care unit-based therapies and longer-term follow-up of patients, severe weakness involving the peripheral nervous system and muscles has been identified in many recovering patients, often confounding the time course or magnitude of recovery. Mechanical ventilation is often accompanied by pharmacologic treatments including analgesics, sedatives, and neuromuscular blockers. These drugs and the encephalopathies accompanying some forms of critical illness result in a high prevalence of delirium in mechanically ventilated patients. These drug effects likely contribute to an impaired ability to assess the magnitude of intensive care unit-acquired weakness, to additional time spent immobilized and mechanically ventilated, and to additional weakness from the patient's relative immobility and bedridden state. This review surveys recent literature documenting these relationships and identifying approaches to minimize pharmacologic contributions to intensive care unit-acquired weakness. PMID:20046129

  18. Interaction of U-69,593 with. mu. -, delta- and k-opioid binding sites and its analgesic and intestinal effects in rats

    Energy Technology Data Exchange (ETDEWEB)

    La Regina, A.; Petrillo, P.; Sbacchi, M.; Tavani, A.

    1988-01-01

    The k-opioid compound U-69,593 was studied in rats in vitro in binding assays to assess its selectivity at the single types of opioid sites and in vivo to assess its analgesic activity and effect on intestinal propulsion. In vitro the U-69,593 inhibition curve of (/sup 3/H)-(-)-bremazocine binding suppressed at ..mu..- and delta-sites was biphasic and the inhibition constant (K/sub l/) at the high-affinity site (10-18nM) was two orders of magnitude smaller the K/sub l/ at the low-affinity site. The K/sub l/ at ..mu..- and delta-sites were respectively 3.3 and 8.5 ..mu..M. Thus (/sup 3/H)-(-)-bremazocine, suppressed at ..mu..- and delta-sites, may still bind more than one site, which U-69,593 might distinguish. In vivo U-69,593 i.p. prolonged the reaction time of rats on a 55/sup 0/C hot-plate and the dose of naloxone required to antagonize this effect was 40 times the dose that antagonized morphine-induced antinociception, suggesting the involvement of the k-receptor. In the intestinal transit test U-69,593 at doses between 0.5 and 15 mg/kg i.p. only slightly slowed intestinal transit of a charcoal meal in rats with no dose-relation; it partly but significantly antagonized morphine-induced constipation. These results suggest that the k-type of opioid receptor, with which U-69,593 interacts may induce analgesia, but has no appreciable role in the mechanisms of opioid-induced inhibition of intestinal transit in rats.

  19. Intracisternal injection of palmitoylethanolamide inhibits the peripheral nociceptive evoked responses of dorsal horn wide dynamic range neurons.

    Science.gov (United States)

    González-Hernández, Abimael; Martínez-Lorenzana, Guadalupe; Rodríguez-Jiménez, Javier; Rojas-Piloni, Gerardo; Condés-Lara, Miguel

    2015-03-01

    Endogenous palmitoylethanolamide (PEA) has a key role in pain modulation. Central or peripheral PEA can reduce nociceptive behavior, but no study has yet reported a descending inhibitory effect on the neuronal nociceptive activity of A?- and C-fibers. This study shows that intracisternal PEA inhibits the peripheral nociceptive responses of dorsal horn wide dynamic range cells (i.e., inhibition of A?- and C-fibers), an effect blocked by spinal methiothepin. These results suggest that a descending analgesic mechanism mediated by the serotonergic system could be activated by central PEA. PMID:24919882

  20. Free Radical Scavenging and Analgesic Activities of Cucumis sativus L. Fruit Extract

    OpenAIRE

    Kumar, D.; Kumar, S.; Singh, J.; Narender,; Rashmi,; Vashistha, Bd; Singh, N.

    2010-01-01

    The aqueous fruit extract of Cucumis sativus L. was screened for free radical scavenging and analgesic activities. The extract was subjected to in vitro antioxidant studies at 250 and 500 ?g/ml and analgesic study at the doses 250 and 500 mg/kg, respectively. The free radical scavenging was compared with ascorbic acid, BHA (Butylated hydroxyl anisole), whereas, the analgesic effect was compared with Diclofenac sodium (50 mg/kg). The C. sativus fruit extract showed maximum antioxidant and ana...

  1. Effect of regular aerobic exercise with ozone exposure on peripheral leukocyte populations in Wistar male rats

    OpenAIRE

    Afshar Jafari; Mohammad Ali Hosseinpour faizi; Fariba Askarian; Hassan Pourrazi

    2009-01-01

    • BACKGROUND: The immune system in endurance athletes may be at risk for deleterious effects of gasous pollutants such as ambient ozone. Therefore, this study was performed to assess the effect of regular aerobic exercise with ozone exposure on peripheral leukocytes populations in male Wistar rats.
    • METHODS: Twenty eight 8 weeks old rats were selected and randomly divided into four groups of ozone-u...

    • Beneficial effect of fish oil on blood viscosity in peripheral vascular disease.

      OpenAIRE

      Woodcock, B. E.; Smith, E.; Lambert, W. H.; Jones, W. M.; Galloway, J. H.; Greaves, M; Preston, F. E.

      1984-01-01

      Reports suggest that the low incidence of ischaemic heart disease in Greenlandic Eskimos is related to the effect of a diet rich in eicosapentaenoic acid on platelet reactivity and plasma lipid concentrations. A double blind randomised investigation was therefore conducted of the effects on blood viscosity of dietary supplementation with an oil rich in this fatty acid (1.8 g/day, given as fish oil) and an eicosapentaenoic acid poor oil (as corn/olive oil) in patients with peripheral arterial ...

    • Effect of green tea extracts on oxaliplatin-induced peripheral neuropathy in rats

      OpenAIRE

      Lee Jung; Kim Yoon; Jeon Eun; Won Hye; Cho Young-Seok; Ko Yoon

      2012-01-01

      Abstract Background A common side effect of oxaliplatin is peripheral neurotoxicity. Oxidative stress to dorsal root ganglion (DRG) may be one of important pathogenic mechanisms. Green tea contains four polyphenol catechins, which are known to be potent antioxidants. The present work is aimed to determine whether green tea extracts have neuroproective or palliative effects on neurotoxicity symptoms induced by oxaliplatin. Methods We conducted behavioral tests including sensory and thermal thr...

    • Lack of effect of domperidone on gastrin release: evidence for a peripheral activity of the drug.

      OpenAIRE

      Masci, E.; Caldara, R.; Testoni, P. A.; Guslandi, M.; Cambielli, M.; Passaretti, S.; Tittobello, A.

      1984-01-01

      The effect of intravenous administration of domperidone, a dopamine receptor antagonist with peripheral activity, on basal and submaximal pentagastrin-stimulated gastric acid secretion and gastrin release has been evaluated in healthy volunteers. No significant changes were observed in the parameters studied. The lack of effect on gastrin release appears to confirm that domperidone is unable to penetrate the blood brain barrier in appreciable amounts in adults.

    • Effect of analgesics, antidepressants and their combinations on changes of structures' of the central nervous system activity in animals with simulated depression

      Directory of Open Access Journals (Sweden)

      Khomiak O.V.

      2012-01-01

      Full Text Available Experiments were carried out on outbred rabbits of both sexes using neurophysiological methods. We resurched the ability of analgesics, antidepressants and their combinations tochange parameters of electrophysiological brain activity under conditions of normal functioning of the central nervous system and on the background ofsimulated depression. Found that in brain pathology combination analgesics with amitriptyline caused activation of the reticular formation (RF and in-creased excitability of dorsomedial tonsils (DMT in comparison with its action in intact rabbits. Analysis of these data on reserpine showed the change of the sign of excitability in the frontal cortex (FC, RF (from inhibition to activation, and re-duction in the dorsal hippocampus (DH, or leveling DMT increased excitability of brain structures under the influence of this combination. Functional relationships between structures were characterized by increasing activating influence of RFon the FC and inhibiting influence of RFon DMT (increasing analgesic activity and reduce brake control DH on FC (increase antidepressant properties. Notably, the combination of celecoxib with the amitriptyline caused fewer changes in excitability of brain structures and intracentral relationships between them that assotiates with less manifested analgesic activity com-pared with the combination of" meloxicam +amitriptyline."

    • The effect of cold application in combination with standard analgesic administration on pain and anxiety during chest tube removal: a single-blinded, randomized, double-controlled study.

      Science.gov (United States)

      Demir, Yurdanur; Khorshid, Leyla

      2010-09-01

      The aim of this study was to investigate the effect of cold application on pain and anxiety during chest tube removal (CTR) in patients who had undergone cardiac surgery. A single-blinded randomized design was used in this study. Ninety patients aged 18-74 years, hospitalized in the intensive care unit (ICU), who had a chest tube for a duration of at least 24 hours were used for this convenience sample. The application of cold, placebo, or control therapies was randomized into three different groups. Sixty minutes before CTR was scheduled, an ICU nurse administered 10mg/kg paracetamol intravenously to all study subjects. Cold and warm packs covered with gauze dressing were applied to the area surrounding the chest tubes for 20 minutes. Pain intensity, pain quality and situational anxiety for CTR were measured. Variance analysis and the latent growth model were used in the analysis of the data. Patients in the cold group had significantly lower pain intensity than the placebo group. The perception of pain intensity measured by visual analog scores of patients in the cold group showed the least variation. There was no statistically significant difference in McGill Melzack Pain Questionnaire scores or in change of anxiety level between the three groups. The application of cold prolonged the length of time until analgesics were needed after CTR. Results showed that cold application reduced patients' intensity of pain due to CTR but did not affect anxiety levels or the type of pain. Cold application is recommended as a pain-relieving technique during CTR. PMID:20728068

    • The effect of the use of ultrasound in the success of peripheral venous catheterisation.

      Science.gov (United States)

      Ismailo?lu, Elif Günay; Zaybak, Ayten; Akarca, Funda Karbek; K?yan, Selahattin

      2014-08-15

      The aim of this study was to investigate the effect of ultrasound-guided peripheral venous catheterisation in patients where difficulty was experienced in peripheral venous catheterisation. The study was conducted in the emergency department at a university hospital in ?zmir Turkey. After obtaining institutional review board approval and written informed consent, 60 patients with a history or suspicion of difficult cannulation were enrolled with 30 patients in traditional and 30 in ultrasound group. In the ultrasound group, peripheral intravenous catheterisation was performed using a portable ultrasound device with 13.5?MHz ultrasound probe and 20 gauge intravenous catheter. The success rate of peripheral venous catheterisation was 30% in the control group and 70% in the treatment group. The success rate was significantly higher among the treatment group. The mean intensity of felt pain was 6.00?±?1.98 in the control group and 4.77?±?1.74 in the treatment group. The mean intensity of felt pain was significantly lower in the treatment group. The state of chronic disease affected the success rate in patients in the treatment group. PMID:25175514

    • Analgesic Effects of Tramadol, Tramadol–Gabapentin, and Buprenorphine in an Incisional Model of Pain in Rats (Rattus norvegicus)

      OpenAIRE

      Mckeon, Gabriel P.; Pacharinsak, Cholawat; Long, Charles T.; Howard, Antwain M.; Jampachaisri, Katechan; Yeomans, David C.; Felt, Stephen A.

      2011-01-01

      Postoperative pain management in laboratory animals relies heavily on a limited number of drug classes, such as opioids and nonsteroidal antiinflammatory drugs. Here we evaluated the effects of saline, tramadol, tramadol with gabapentin, and buprenorphine (n = 6 per group) in a rat model of incisional pain by examining thermal hyperalgesia and weight-bearing daily for 6 d after surgery. All drugs were administered preemptively and continued for 2 consecutive days after surgery. Rats treated w...

    • Analgesic Effect of Regular Breathing Exercises with the Aim of Distraction during Venipuncture in School-aged Thalassemic Children

      Directory of Open Access Journals (Sweden)

      Mohsenpour M

      2012-09-01

      Full Text Available AbstractBackgroundPain is described as the fifth vital sign, and inadequate pain management is linked to numerous immediate and long-term negative outcomes. Venipuncture is one of the most painful medical procedures in children. Distraction is one of the main effective ways to relieve pain. Reducing patients’ pain sensation maybe feeling is important for all nurses for many reasons. Unnecessary pain can damage the nurse-patient relationship, whereas the knowledge of alternative techniques can improve patient care and satisfaction. Materials and MethodsForty patients (6–12 years suffering from thalassemia and requiring venipuncture were randomized into distraction group (n=20, regular breathing exercise and control group (n=20, without any intervention. The pediatric pain behavioral symptoms and Numeric Pain Rating Scale were used to assess pain caused by venipuncture.ResultsThe mean of pain score based on the numerical scale was 5.60 ± 3.13 in the control group and 1.85±1.42 in breathing exercises and the mean score of behavioral pain symptoms was 3.80±2.80 in the control group and 0.96±0.75 in breathing exercise group. Results showed a significant difference between the mean of pain scores (based on numeric scale and pain behavior scale. (p?0.001Conclusion Distraction demonstrated to be effective in reducing pain. This intervention requires minimum effort and time and may be a cost-effective and convenient nursing intervention that could be used easily in clinical settings.

    • The effect of sarsasapogenine on peripheral lymphocyle ?-adrenoceptors in rabbit hydrocortisone models

      International Nuclear Information System (INIS)

      The effects of sarsasapogenine (SAR), an active principle of Anemorrhenae Rhizome, on peripheral lymphocyte ?-adrenoceptors (?-AR) and serum cortisol contents were studied in rabbit hydrocortisone models produced by repeated injections of therapeutic doses of hydrocortisone. The lymphocyte ?-AR binding sites (SB) were measured with 125I-PIN binding assay and the serum cortisol contents were estimated with radioimmunoassay. Experimental data revealed that hydrocortisone treatment markedly elevated the lymphocyte SB (0.65 ± 0.03 and 1.48 ± 0.13 fmol/106 cells before and after treatment) as well as the serum cortisol (128 ± 21 and 239 ± 45 nmol/1 before and after treatment). Oral administration of SAR for 6 days decreased the lymphocyte ?-AR significantly (1.48 ± 0.13 and 0.76 ± 0.06 fmol/106 cells before and after administration). On the contrary, SAR showed no significant effect on serum cortisol contents. Therefore the down-regulation effect of SAR on peripheral lymphocyte ?-AR, which might reflect one of the clinical effects of Anemorrhenae Rhizome for treating 'Yin Deficiency'syndrome, is unlikely to be mediated through an influence on serum cortisol content. The mechanism of the down-regulation effect of SAR on peripheral lymphocyte ?-AR remains to be studied

    • Sildenafil enhances the peripheral antinociceptive effect of ellagic acid in the rat formalin test

      Science.gov (United States)

      Mansouri, Mohammad Taghi; Naghizadeh, Bahareh; Ghorbanzadeh, Behnam

      2014-01-01

      Objective: Ellagic acid (EA), a major polyphenolic compound of pomegranate juice, produces antinociceptive effects, which are mediated through opioidergic and nitric oxide-cyclic guanosine monophosphate (NO-cGMP) pathways. The present study was conducted to elucidate the peripheral antinociceptive effect of EA alone and in combination with sildenafil in the rat formalin test. Materials and Methods: Pain was produced by intraplantar injection of formalin (2.5%) in rats and nociceptive behavior was measured as the number of flinches every 5 min in 60 min after injection. Results: Local administration of EA and sildenafil dose-dependently increased the nociception threshold in both phases of the test. Moreover, sub-effective doses of sildenafil (25 or 50 mcg/paw, i.p.) significantly and dose-dependently enhanced the antinociception induced by a sub-effective dose of EA (60 mcg/paw, i.pl.) in both phases of the test. The antinociception produced by these drugs alone, or in combination, was due to a peripheral site of action, since the administration in the contralateral paw was ineffective. Conclusion: Our results suggest that EA has local peripheral antinociceptive activity, and enhancement of this effect with sildenafil probably occurs through the inhibition of cGMP metabolism. PMID:25097278

    • Analgesic and anti-arthritic effect of Corallocarpus epigaeus / Efeito analgésico e antiartrítico de Corallocarpus epigaeus / Efecto analgésico y antiartrítico de Corallocarpus epigaeus

      Scientific Electronic Library Online (English)

      Subashini, Uthrapathy; Mohamed M, Shabi; Gayathri, Krishnamoorthy; Dhevi, Ravindhran; Victor G, Rajamanickam; Govindha, Pillay Dubey.

      2011-12-01

      Full Text Available A artrite eumatóide é uma doença inflamatória crônica das articulações que se encontra associada ao desenvolvimento de estresse oxidativo e inflamação. No presente estudo é avaliado o perfil de segurança e de eficácia de um extrato metanólico a 85% de Corallocarpus epigaeus (CE). No perfil de segura [...] nça foi determinado o valor de DL50 levando a cabo um estudo de toxicidade aguda. No perfil de eficácia, a atividade analgésica foi avaliada tanto pelo método de prato quente como por meio do teste de imersão da cauda. Foi avaliada a atividade antiinflamatória por edema de pata induzido por carragenina e o efeito antiartrítico mediante artrite induzida por adjuvante completo de Freund. Também se têm levado a cabo a análise fitoquímica das famílias de compostos presentes em diferentes extratos de CE e a análise quantitativa da erva crua e do extrato metanólico a 85%. O extrato metanólico apresentou atividade analgésica ao aumentar o tempo de resposta tanto no método do prato quente como no teste de imersão da cauda. O extrato exibiu 23,19% de atividade antiinflamatória e 33,59% de efeito antiartrítico em edema de pata induzido por adjuvante completo de Freund. O extrato de CE aumentou o nível antioxidante, ao mesmo tempo que diminuiu o estresse oxidativo desenvolvido pela artrite induzida pelo adjuvante completo de Freund. Em conclusão, CE é uma fonte rica de compostos fitoquímicos com atividades analgésicas, anti-inflamatórias e antioxidantes. Abstract in spanish La artritis reumatoidea es una enfermedad inflamatoria crónica de las articulaciones que se encuentra asociada con el desarrollo de estrés oxidativo e inflamación. En el presente estudio se evalúa el perfil de seguridad y de eficacia de un extracto metanólico al 85% de Corallocarpus epigaeus (CE). E [...] n el perfil de seguridad se determinó el valor de DL50 llevando a cabo un estudio de toxicidad aguda. En el perfil de eficacia, la actividad analgésica se evaluó tanto por el método de plato caliente como por medio de la prueba de inmersión de la cola. Se evaluó la actividad antiinflamatoria por edema de pata inducido por carragenina y el efecto antiartrítico mediante artritis inducida por adyuvante completo de Freund. También se han llevado a cabo el análisis fitoquímico de las familias de compuestos presentes en diferentes extractos de CE y el análisis cuantitativo de la hierba cruda y del extracto metanólico al 85%. El extracto metanólico presentó actividad analgésica al incrementar el tiempo de respuesta tanto en el método del plato caliente como en la prueba de inmersión de la cola. El extracto exhibió 23,19% de actividad antiinflamatoria y 33,59% de efecto antiartrítico en edema de pata inducido por adyuvante completo de Freund. El extracto de CE aumentó el nivel antioxidante al tiempo que disminuyó el estrés oxidativo desarrollado por la artritis inducida por el adyuvante completo de Freund. En conclusión, CE es una fuente rica de compuestos fitoquímicos con actividades analgésicas, antiinflamatorias y antioxidantes. Abstract in english Rheumatoid arthritis is a chronic inflammatory joint disease associated with the development of oxidative stress and inflammation. The safety and efficacy profile of 85% methanolic extract of Corallocarpus epigaeus (CE) was evaluated in the present study. In safety profile LD50 value was determined [...] by carrying out an acute toxicity study. In efficacy profile, the analgesic activity was evaluated by both hot plate and tail immersion tests. The anti-inflammatory activity was assessed by carrageenan-induced paw edema and anti-arthritic effect by complete Freund's adjuvant induced arthritis. Phytochemical screening of different CE extracts and quantitative analysis of both raw herb and 85% methanolic extract have been also carried out. The methanolic extract displayed analgesic activity by increasing the response time in both hot plate and tail immersion method. Extract exhibited 23,19% of anti-inflammatory activity and 33,59% of a

    • Analgesic and Anti-Ulcer Activities of Ethanol and Aqueous Extracts of Root of Bauhinia variegata Linn.

      Directory of Open Access Journals (Sweden)

      Yamini R. Kumar

      2011-01-01

      Full Text Available The present study was aimed at evaluating analgesic and antiulcer activities of the ethanolic (BVE and aqueous (BVA extracts of root of Bauhinia variegata Linn., respectively in animal models. The analgesic activity was evaluated for its central and peripheral pharmacological actions by using Eddys hot plate method and acetic acid-induced writhing, respectively. The anti-ulcer activity was evaluated by using pylorus ligation, ethanol and aspirin induced ulcer models. The study was carried out in two different dose levels of 200 and 400 mg kg-1 body weight orally for both ethanolic and aqueous extracts, respectively. BVE and BVA did not produce any mortality up to 2000 mg kg-1. Dose dependent increase in latency of response in the hot plate method was observed with BVE 400 mg kg-1 and 81% inhibition in acetic acid induced writhings in mice was observed with BVA 400 mg kg-1. BVE and BVA at both the doses showed 99% protection in ethanol induced ulcer model. BVE 400 mg kg-1 showed 99.9% protection in aspirin induced ulcer model. Both BVE and BVA at the dose of 400 mg kg-1 showed 99.8% protection in pylorus ligation ulcer model. Pharmacological screening of the root extracts of Bauhinia variegata Linn. showed significant (p<0.001 dose dependent analgesic activity and significant (p<0.001 anti-ulcer activity when compared with reference standard. Presence of flavonoids might be responsible for these activities. NSAIDs are associated with side effects of gastric ulcers. BVE and BVA are reported to be plant-derived natural remedy having analgesic and anti-ulcer activities.

    • EVALUATION OF HYDROALCOHOLIC EXTRACT OF AERIAL PARTS OF ABUTILON INDICUM FOR ITS ANALGESIC AND SEDATIVE PROPERTY

      Directory of Open Access Journals (Sweden)

      Deepraj Paul

      2013-06-01

      Full Text Available The hydro alcoholic extract of aerial parts of Abutilon Indicum was tried for its efficacy as analgesic and sedative property. Several pain models namely Eddy’s hot plate, acetic acid induced writhing test, tail clip test and hot water immersion test were tried and for sedative property actophotometer test was performed. As the extract has shown very significant (P?0.01 result in Eddy’s hot plate, acetic acid induced writhing test and hot water immersion test hence it is believed that the extract has certain central and peripheral analgesic property which may be mediated either by closing Na+ or/and Ca2+ channels or by facilitating chloride Cl- influx by acting on GABAA receptor. As the extract has significantly reduced loco motor activity hence the mechanism of action of the extract is believed to be mediated by opening of Cl- channel, indicating that the extract may have GABA mimetic or facilitating effect. As following the administration of the extract no straub reaction was observed hence may be in future it will gain more popularity to be used as a substitute for narcotics to treat pain and also as a good sedative.

    • Peripheral neuropathies treatment with Scrambler Therapy

      Directory of Open Access Journals (Sweden)

      V. Iorno

      2007-12-01

      Full Text Available Thirty-one patients with painful peripheral neuropathy were treated with one 45-minute ST5 application daily, for a total of 10 treatments per patient.To evaluate effectiveness of treatment, three variables were measured: pain intensity as measured by visual analogue scale (VAS, presence of allodynia, and analgesic usage.All measurements were made pretreatment (T0, immediately posttreatment cycle (T1, and after 3 months (T2. Mean pre-treatment VAS was 8,2, which diminished to 2,7 at T1, and to 3,0 at T2 (p<0.001. Pretreatment allodynia was present in 77,41% of patients, decreasing to 16,12% at T1. Allodynia was present in 25,8% of patients at T2. Pharmacologic analgesic consumption diminished by 42,86% at T1, and further reduced by 54,74% at three-month follow-up. No adverse side effects were noted.

    • Effects of trapidil after crush injury in peripheral nerve.

      Directory of Open Access Journals (Sweden)

      Kurtoglu,Zeliha

      2005-04-01

      Full Text Available

      In this study, we evaluated the effects of trapidil on crush injury by monitoring nitric oxide, malondialdehyde and transforming growth factor-Beta2 levels and by transmission electron microscopy in the rat sciatic nerve. The sciatic nerve was compressed for 20 sec by using a jewelers forceps. Trapidil treatment groups were administrated a single dose of trapidil (8 mg/kg intraperitoneally just after the injury. The crush and crush + trapidil treatment groups were evaluated on the 2nd, 7th, 15th, 30th and 45th days of the post-crush period. On the 7th and 15th days, damage in thin and thick myelinated axons, endoneural edema and mitochondrial swelling were less severe in the trapidil group histopathologically. These findings supported the idea that trapidil prevented cell damage and edema at the injury site. Day/group interaction with regard to serum nitric oxide, malondialdehyde and transforming growth factor-Beta2 levels did not show significant changes.

    • Efeito analgésico de longa duração da dipirona sobre a hiperalgesia persistente induzida pela constrição do nervo ciático em ratos: participação do óxido nítrico / Long term analgesic effect of dipyrone on the persistent hyperalgesia induced by chronic constriction injury of sciatic nerve in rats: involviment of nitric oxide

      Scientific Electronic Library Online (English)

      Fábio José, Reis; Noeli Pereira, Rocha.

      2006-12-01

      Full Text Available SciELO Brazil | Language: Portuguese Abstract in portuguese O efeito analgésico de longa duração da dipirona foi avaliado em um modelo de dor neuropática assim como a participação da via óxido nítrico-GMPc neste mecanismo analgésico. Uma única administração intraplantar de dipirona (80 µg), no 14º dia após a instalação da hiperalgesia neuropática induzida pe [...] la constrição do nervo ciático exerceu um efeito analgésico, significativo e de longa duração. A inibição da óxido nítrico sintetase com L-NAME (50 ou 100 µg/pata), ou do óxido nítrico (NO) endógeno com hemoglobina (10 ou 30 µg/pata), bloquearam o desenvolvimento do efeito analgésico da dipirona. A L-arginina (500 µg/pata) reverteu o efeito do L-NAME. Cloreto de metiltionínio (azul de metileno) (500 µg/pata), ODQ (50 µg/pata) (bloqueadores da guanilil ciclase) ou glibenclamida (100, 200 ou 300 µg/pata) (bloqueador de canais de K+ sensíveis ao ATP) inibiram o efeito analgésico da dipirona. O nitroprussiato de sódio administrado no 14º dia após a instalação da hiperalgesia neuropática também exerceu efeito analgésico de longa duração, semelhante ao observado com a dipirona. Sugerimos que a ação analgésica periférica e de longa duração da dipirona, neste modelo experimental, ocorra devido a provável dessensibilização dos nociceptores, envolvendo a via óxido nítrico - GMPc e canais de K+ sensíveis ao ATP. Abstract in english The long term analgesic effect of dipyrone was evaluated on a model of neuropathic pain and the role of nitric oxide/GMPc pathway in this antinociceptive mechanism. One intraplantar dipyrone administration (80 mg), at 14th day after the chronic constriction injury of the sciatic nerve, induced a sig [...] nificant and long term analgesic effect. The inhibition of nitric oxide synthase (NOS) with L-NAME (50 or 100 mg/paw) or scavenging of the endogenous NO with hemoglobin (10 or 30 mg/paw) inhibited the development of the dipyrone analgesia. L-arginine (500 mg/paw) could reverted the effect of L-NAME. Metylene blue (500 mg/paw) or ODQ (50 mg/paw) (blockers of guanyl cyclase), or glybenclamide (100, 200 or 300 mg/paw) (blocker of ATP-sensitive K+ channels) inhibited the development of dipyrone analgesia. The sodium nitroprussiate administered at 14th day after the chronic constriction injury of the sciatic nerve also induced a long term analgesic effect similar to that of dipyrone. Our data may support the suggestion that the peripheral and the long term analgesic action of dipyrone on this model experimental occurs due to a probable nociceptor desensitisation with involviment of activation of the nitric oxide-cGMP pathway, followed by an opening of ATP-sensitive K+ channels.

    • Inhibitory effect of mitragynine, an analgesic alkaloid from Thai herbal medicine, on neurogenic contraction of the vas deferens.

      Science.gov (United States)

      Matsumoto, Kenjiro; Yamamoto, Leonardo T; Watanabe, Kazuo; Yano, Shingo; Shan, Jie; Pang, Peter K T; Ponglux, Dhavadee; Takayama, Hiromitsu; Horie, Syunji

      2005-11-26

      The effect of an indole-alkaloid mitragynine isolated from the Thai medicinal herb kratom (Mitragyna speciosa) on neurogenic contraction of smooth muscle was studied in guinea-pig vas deferens. Mitragynine inhibited the contraction of the vas deferens produced by electrical transmural stimulation. On the other hand, mitragynine failed to affect the responses to norepinephrine and ATP. Mitragynine did not reduce KCl-induced contraction in the presence of tetrodotoxin, prazosin and alpha,beta-methylene ATP. Mitragynine inhibited nicotine- or tyramine-induced contraction. By using the patch-clamp technique, mitragynine was found to block T- and L-type Ca2+ channel currents in N1E-115 neuroblastoma cells. In the Ca2+ measurement by a fluorescent dye method, mitragynine reduced KCl-induced Ca2+ influx in neuroblastoma cells. The present results suggest that mitragynine inhibits the vas deferens contraction elicited by nerve stimulation, probably through its blockade of neuronal Ca2+ channels. PMID:16107269

    • Rapid Sensitization of Physiological, Neuronal, and Locomotor Effects of Nicotine: Critical Role of Peripheral Drug Actions

      OpenAIRE

      Lenoir, Magalie; Tang, Jeremy S.; Woods, Amina S.; Kiyatkin, Eugene A.

      2013-01-01

      Repeated exposure to nicotine and other psychostimulant drugs produces persistent increases in their psychomotor and physiological effects (sensitization), a phenomenon related to the drugs' reinforcing properties and abuse potential. Here we examined the role of peripheral actions of nicotine in nicotine-induced sensitization of centrally mediated physiological parameters (brain, muscle, and skin temperatures), cortical and VTA EEG, neck EMG activity, and locomotion in freely moving rats. Re...

    • Psychological contents and social effects associated to peripheral facial paralysis: a speech-language approach

      OpenAIRE

      Silva, Mabile Francine Ferreira; Cunha, Maria Claudia; Lazarini, Paulo Roberto; Fouquet, Marina Lang

      2011-01-01

      Introduction: The peripheral facial paralysis (PFP) results from the reduction or interruption of the axonal transport to the seventh cranial nerve resulting in complete or partial paralysis of the facial movements. The facial deformity and limitation of movements, besides affecting the aesthetics and functionality, can significantly interfere with interpersonal communication. Objective: Investigate the psychological contents and other social effects associated to PFP in adult subjects, perfo...

  1. Effect of lymphokines on ?-adrenoceptor function of human peripheral blood mononuclear cells

    OpenAIRE

    Oosterhout, A. J. M.; Nijkamp, F. P.

    1990-01-01

    Pathological induced changes in ?-adrenoceptor function occur in diseases such as asthma and hypertension. The mechanism(s) of this dysfunction is at present unclear. In the present study, the effect of lymphokines on ?-adrenoceptor agonist induced cAMP production in peripheral blood mononuclear cells (PBMC) is investigated. Pre-incubation of PBMC during 20 h with interleukin-2 (IL-2, 100 u ml-1) and granulocyte/macrophage-colony stimulating factor (GM-CSF, 100 u ml-1) significantly decreas...

  2. Screening of cetirizine for analgesic activity in mice

    Directory of Open Access Journals (Sweden)

    Priya M

    2013-04-01

    Full Text Available Background: Pain is the most common symptom for which patients approach doctors. We have multitude of drugs for pain relief, but they have serious side effects ranging from peptic ulcer (e.g. NSAIDs to renal failure. The other group, opioids have well known side effects ranging from sedation to drug dependence. So a search for a drug for analgesia with high therapeutic effect and fewer side effects will be a boon for the patients. The objective of this study was to find whether cetirizine, a second generation antihistaminic drug, has got any analgesic activity in mice. Methods: Ten adult albino mice weighing 20-30 grams of either sex were randomized to two groups (n=5. Group I: control group (Treated with solvent 0.1 ml/kg, Group II: Test group (Cetirizine 1mg/kg. All drugs were given orally. The analgesic activity was evaluated by using tail flick, tail immersion and tail clip methods. Reaction time of animals to pain sensation before and after Cetirizine administration were noted at 0, 15, 30, 60 and 90 minutes time intervals respectively on Day 1, 3, 5, 7, 10. Results: Mean reaction time was expressed as Mean±SEM, and one way ANOVA was used to assess statistical significance. Cetirizine was found to have statistically significant analgesic effect in mice and time dependent increase in analgesic effect were observed in all three pain models and maximum analgesic activity was observed at 60 minutes (p<0.001 after drug administration. Conclusions: Through this study, Cetirizine, a second generation antihistamine, is found to have significant analgesic activity in mice. This effect has to be studied further elaborately in animals as well as in humans. [Int J Basic Clin Pharmacol 2013; 2(2.000: 187-192

  3. Reduction of the Spatial Stroop Effect by Peripheral Cueing as a Function of the Presence/Absence of Placeholders

    OpenAIRE

    Luo, Chunming; Lupia?n?ez Castillo, Juan; Funes, Mari?a Jesu?s; Fu, Xiaolan

    2013-01-01

    In a paradigm combining spatial Stroop with spatial cueing, the current study investigated the role of the presence vs. absence of placeholders on the reduction of the spatial Stroop effect by peripheral cueing. At a short cue-target interval, the modulation of peripheral cueing over the spatial Stroop effect was observed independently of the presence/absence of placeholders. At the long cue-target interval, however, this modulation over the spatial Stroop effect only occurred in the placehol...

  4. Comparison of analgesic effect of intrathecal morphine alone or in combination with bupivacaine and fentanyl in patients undergoing total gastrectomy: A prospective randomised, double blind clinical trial

    Directory of Open Access Journals (Sweden)

    Slavkovi? Zoran

    2013-01-01

    Full Text Available Background/Aim. Combined spinal-epidural-general anesthesia has several advantages over general anesthesia alone. This study was designed to compare the efficacy of intrathecal (IT morphine alone, or in combination with bupivacaine and fentanyl, as part of a combined spinal-epidural (CSE analgesia, in patients undergoing elective total gastrectomy. Methods. This prospective, randomized double-blind study included 60 patients undergoing total gastrectomy under general anesthesia and CSE. We compared the analgesic effect of lumbar IT morphine 300 ?g (the group M, n = 20 vs morphine 300 ?g + bupivacaine 2 mg (the group MB, n = 20 vs morphine 300 ?g + bupivacaine 2 mg + fentanyl 25 ?g (the group MBF, n = 20 given after thoracic epidural catheter placement (T6-7 but before general anesthesia induction. Pain visual analogue scale (VAS at rest (R, with movement (M and with cough (C, and the number of analgesia requests were assessed for 72 h and after epidural catheter removal. Results. Compared to other groups, the MBF group required significantly fewer additional intra-operative epidural bupivacaine doses (p < 0.001, whereas the M group required significantly more supplemental intraoperative intravenous fentanyl, compared with the MBF (p = 0.022 and MB groups (p = 0.005. Postoperative pain relief was satisfactory in all the groups at all the time. VAS-R and VAS-M did not differ significantly among the groups. Compared to the M group, VAS-C scores 30 min postoperatively were significantly lower in the MBF (p = 0.029 and MB groups (p = 0.002. Duration of analgesia was longer in the MBF and MB groups, but the difference reached no significance. The number of supplemental analgesia requests was similar in all the groups in the first 12 h and during 72 h. Additional analgesia requests after epidural catheter removal were similar in all the groups, and side effects were infrequent. Conclusion. Compared to IT morphine alone, triple IT combination administered as part of CSE provided better intraoperative analgesia, but conferred no benefit with regards to postoperative analgesia.

  5. Analgésicos tópicos Analgésicos tópicos Topical analgesics

    Directory of Open Access Journals (Sweden)

    Murilo Pereira Flores

    2012-04-01

    Full Text Available JUSTIFICATIVA E OBJETIVOS: O tratamento da dor envolve a utilização de analgésicos opioides, analgésicos comuns, anti-inflamatórios não hormonais (AINH's e analgésicos adjuvantes. Tradicionalmente, estes fármacos são administrados por via sistêmica ou no neuroeixo. Entretanto, quando aplicados por estas vias, estão associados a efeitos colaterais importantes, os quais podem inviabilizar o seu uso. A administração tópica de analgésicos é uma alternativa. O objetivo deste trabalho é discutir os analgésicos tópicos, seus mecanismos de ação e eficácia clínica. CONTEÚDO: Trata-se de um trabalho de revisão que aborda a utilização tópica de anestésicos locais, capsaicina, clonidina, antidepressivos tricíclicos, cetamina, opioides e canabinoides, discutindo o seu mecanismo de ação e a sua eficácia. CONCLUSÕES: Os analgésicos tópicos são promissores como estratégia para o tratamento da dor, já que estão associados à menor incidência de efeitos colaterais. O benefício dos anestésicos locais, dos AINH's e da capsaicina está bem estabelecido, entretanto, a eficácia de clonidina, antidepressivos tricíclicos, cetamina, opioides e canabinoides ainda é questionável. Trabalhos demonstram que a abordagem multimodal é uma alternativa, porém estudos são necessários para confirmar esta hipótese.JUSTIFICATIVA Y OBJETIVOS: El tratamiento del dolor involucra la utilización de analgésicos opioides, analgésicos comunes, antiinflamatorios no hormonales (AINH's y analgésicos adyuvantes. Tradicionalmente, esos fármacos son administrados por vía sistémica o en el neuro eje. Sin embargo, cuando se aplican por esas vías, están asociados a los efectos colaterales importantes, los cuales pueden impedir su uso. La administración tópica de analgésicos es una alternativa. El objetivo de este trabajo es discutir los analgésicos tópicos, sus mecanismos de acción y la eficacia clínica. CONTENIDO: Se trata de un trabajo de revisión que aborda la utilización tópica de anestésicos locales, capsaicina, clonidina, antidepresivos tricíclicos, cetamina, opioides y canabinoides, discutiendo su mecanismo de acción y su eficacia. CONCLUSIONES: Los analgésicos tópicos son promisorios como una estrategia para el tratamiento del dolor, ya que están asociados con una menor incidencia de efectos colaterales. El beneficio de los anestésicos locales, de los AINH's y de la capsaicina está muy bien establecido, sin embargo, la eficacia de la clonidina, los antidepresivos tricíclicos, cetamina, opioides y canabinoides, todavía es cuestionable. Algunos trabajos demuestran que el abordaje multimodal es una alternativa, pero más estudios son necesarios para poder confirmar esa hipótesis.BACKGROUND AND OBJECTIVES: Pain treatment involves the usage of common and opioid analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs and adjuvant analgesics. Traditionally, these drugs are administered systemically or into the neuraxis. However, when analgesics are applied through these pathways, they are associated with significant side effects, which can hinder its use. Topical administration of analgesics is an alternative. The objective of this paper is to discuss topical analgesics, the mechanisms of action and clinical efficacy. CONTENT: This is a review paper addressing the usage of the topical local anesthetics: capsaicin, clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids, discussing mechanism of action and effectiveness. CONCLUSIONS: Topical analgesics are promising as a strategy for pain treatment, as they are associated with lower incidence of side effects. The benefit of local anesthetics, NSAID's and capsaicin is well established. However, the efficacy of clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids is still questionable. Studies have shown that the multimodal approach is an alternative, but studies are needed to confirm this hypothesis.

  6. Analgésicos tópicos / Topical analgesics / Analgésicos tópicos

    Scientific Electronic Library Online (English)

    Murilo Pereira, Flores; Anita Perpetua Carvalho Rocha de, Castro; Jedson dos Santos, Nascimento.

    2012-04-01

    Full Text Available SciELO Brazil | Languages: English, Portuguese, Spanish Abstract in portuguese JUSTIFICATIVA E OBJETIVOS: O tratamento da dor envolve a utilização de analgésicos opioides, analgésicos comuns, anti-inflamatórios não hormonais (AINH's) e analgésicos adjuvantes. Tradicionalmente, estes fármacos são administrados por via sistêmica ou no neuroeixo. Entretanto, quando aplicados por [...] estas vias, estão associados a efeitos colaterais importantes, os quais podem inviabilizar o seu uso. A administração tópica de analgésicos é uma alternativa. O objetivo deste trabalho é discutir os analgésicos tópicos, seus mecanismos de ação e eficácia clínica. CONTEÚDO: Trata-se de um trabalho de revisão que aborda a utilização tópica de anestésicos locais, capsaicina, clonidina, antidepressivos tricíclicos, cetamina, opioides e canabinoides, discutindo o seu mecanismo de ação e a sua eficácia. CONCLUSÕES: Os analgésicos tópicos são promissores como estratégia para o tratamento da dor, já que estão associados à menor incidência de efeitos colaterais. O benefício dos anestésicos locais, dos AINH's e da capsaicina está bem estabelecido, entretanto, a eficácia de clonidina, antidepressivos tricíclicos, cetamina, opioides e canabinoides ainda é questionável. Trabalhos demonstram que a abordagem multimodal é uma alternativa, porém estudos são necessários para confirmar esta hipótese. Abstract in spanish JUSTIFICATIVA Y OBJETIVOS: El tratamiento del dolor involucra la utilización de analgésicos opioides, analgésicos comunes, antiinflamatorios no hormonales (AINH's) y analgésicos adyuvantes. Tradicionalmente, esos fármacos son administrados por vía sistémica o en el neuro eje. Sin embargo, cuando se [...] aplican por esas vías, están asociados a los efectos colaterales importantes, los cuales pueden impedir su uso. La administración tópica de analgésicos es una alternativa. El objetivo de este trabajo es discutir los analgésicos tópicos, sus mecanismos de acción y la eficacia clínica. CONTENIDO: Se trata de un trabajo de revisión que aborda la utilización tópica de anestésicos locales, capsaicina, clonidina, antidepresivos tricíclicos, cetamina, opioides y canabinoides, discutiendo su mecanismo de acción y su eficacia. CONCLUSIONES: Los analgésicos tópicos son promisorios como una estrategia para el tratamiento del dolor, ya que están asociados con una menor incidencia de efectos colaterales. El beneficio de los anestésicos locales, de los AINH's y de la capsaicina está muy bien establecido, sin embargo, la eficacia de la clonidina, los antidepresivos tricíclicos, cetamina, opioides y canabinoides, todavía es cuestionable. Algunos trabajos demuestran que el abordaje multimodal es una alternativa, pero más estudios son necesarios para poder confirmar esa hipótesis. Abstract in english BACKGROUND AND OBJECTIVES: Pain treatment involves the usage of common and opioid analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and adjuvant analgesics. Traditionally, these drugs are administered systemically or into the neuraxis. However, when analgesics are applied through these pathw [...] ays, they are associated with significant side effects, which can hinder its use. Topical administration of analgesics is an alternative. The objective of this paper is to discuss topical analgesics, the mechanisms of action and clinical efficacy. CONTENT: This is a review paper addressing the usage of the topical local anesthetics: capsaicin, clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids, discussing mechanism of action and effectiveness. CONCLUSIONS: Topical analgesics are promising as a strategy for pain treatment, as they are associated with lower incidence of side effects. The benefit of local anesthetics, NSAID's and capsaicin is well established. However, the efficacy of clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids is still questionable. Studies have shown that the multimodal approach is an alternative,

  7. Percutaneous Ablation of Peripheral Pseudoaneurysms Using Thrombin: A Simple and Effective Solution

    International Nuclear Information System (INIS)

    Purpose: To assess the effectiveness of tissue adhesive and thrombin solution in the percutaneous ablation of peripheral artery pseudoaneurysms.Methods: Twenty-five pseudoaneurysms were treated over a 33-month period; all had failed ultrasound-guided compression. Tissue adhesive or thrombin solution was injected percutaneously, with needle tip position and changes within the aneurysm confirmed with color Doppler ultrasound. In 19 cases we utilized a protective balloon inflated across the aneurysm neck prior to the injection of tissue adhesive and in six cases used thrombin injection alone. Seven patients were anticoagulated. Patients were followed up after the procedure.Results: All 25 aneurysms were treated successfully; two patients required a return visit and there were no immediate complications or peripheral emboli detected. One patient developed a contralateral pseudoaneurysm.Conclusions: The percutaneous injection of pseudoaneurysms is a safe, a traumatic, and effective treatment for femoral artery pseudoaneurysms in the peripheral circulation. There are significant advantages over ultrasound-guided compression or surgical repair

  8. Evaluation of Anti-inflammatory and Analgesic Activity of the Extract and Fractions of Astragalus hamosus in Animal Models

    OpenAIRE

    Shojaii, Asie; Motaghinejad, Majid; Norouzi, Sima; Motevalian, Manijeh

    2015-01-01

    The objective of this study was to evaluate the anti-inflammatory and analgesic activities of the hydro-alcoholic extract of the pods of Astragalus hamosus (HAAH), a plant used in Iranian traditional medicine, and antinociceptive effects of different fractions in animal models. The anti-inflammatory effect was evaluated by the rat paw edema induced by formalin. Also the analgesic effect was examined by the acetic-acid-induced writhing response and hot plate test. The analgesic effects of chlo...

  9. Box jellyfish (Carybdea alata) in Waikiki: their influx cycle plus the analgesic effect of hot and cold packs on their stings to swimmers at the beach: a randomized, placebo-controlled, clinical trial.

    Science.gov (United States)

    Thomas, C S; Scott, S A; Galanis, D J; Goto, R S

    2001-04-01

    The study measured the analgesic effect of hot and cold packs on box jellyfish (Carybdea alata) stings to Waikiki swimmers at the beach. Analysis of data showed a minimal trend toward pain relief 10 minutes after the application of hot packs, particularly when the initial pain was mild to moderate. Cold packs showed no clinically significant relief of pain, compared to the control. Data tracking shows that most box jellyfish appear in Waikiki waters on the 9th or 10th day after the full moon. PMID:11383098

  10. Effects of competitive and noncompetitive antagonists of the N-methyl-D-aspartate receptor on the analgesic action of delta 1- and delta 2-opioid receptor agonists in mice.

    OpenAIRE

    Bharagava, H. N.; Zhao, G. M.

    1996-01-01

    1. The effects of MK-801, a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor and LY 235959, a competitive antagonists of the NMDA receptor on the analgesic actions of [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2, Glu4] deltorphin II (deltorphin II), the putative delta 1- and delta 2-opioid receptor agonists, respectively, were determined in the male Swiss-Webster mice. 2. Intracerebroventricular administration of DPDPE or deltorphin II produced analgesia. MK-801 administ...

  11. Effects of low-dose continuously fractionated X-ray irradiation on murine peripheral blood lymphocytes

    International Nuclear Information System (INIS)

    For estimating biological risks from low doses continual irradiation, we investigated the effects of exposure to continuously fractionated X-rays on murine immune system. The BALB/c mice were irradiated with 0.07Gy at the first day and 0.08 Gy/d in the following 12 days at a dose rate of 0.2 Gy/min. The peripheral blood lymphocyte cycle and death were determined by flow cytometry at the cumulative doses of 0, 0.07, 0.23, 0.39, 0.55, 0.71, 0.87 and 1.03 Gy respectively. The results showed that the cycle of peripheral blood lymphocyte was arrested in G0/G1 at cumulative doses of 0.07, 0.23, 0.71 and 0.87 Gy, and in G2/M at cumulative doses of 0.39 and 1.03 Gy; the percentage of death of peripheral blood lymphocyte was ascended with dose increasing, and reached the death peak at cumulative doses of 0.71 Gy. The results suggested that low doses continual X-rays total-body irradiated could result in changes of cellular cycle and death, and some damages to immunocytes, which accorded to linear square model. (authors)

  12. Distractor inhibition is more effective at a central than at a peripheral location.

    Science.gov (United States)

    Chen, Zhe; Treisman, Anne

    2008-08-01

    The "distractor eccentricity effect" refers to the finding of reduced interference from an incompatible distractor at a central relative to a peripheral location (Chen, 2008). The present study examines the mechanism that underlies the distractor eccentricity effect, and relates it to the inattentional blindness explored by Mack and Rock (1998), which was also more marked at a foveal than at a parafoveal location. The results suggest that these two visual phenomena may reflect the same underlying mechanism--a gradient of increasing attentional suppression from the periphery to the center. PMID:18717393

  13. Protective effect of quercetin against oxidative stress caused by dimethoate in human peripheral blood lymphocytes

    OpenAIRE

    Lassoued Saloua; Elfekih Abdelfetteh; Abdallah Fatma; Mansour Riadh; Gargouri Bochra; Khaled Hamden

    2011-01-01

    Abstract Background The aim of this study is to investigate the effect of quercetin in alleviating the cytotoxic effects of Dimethoate in human peripheral blood lymphocytes. Methods Lymphocytes were divided into too groups. The first group, lymphocytes were incubated for 4 h at 37°C with different concentrations (0, 40, 60 and 100 mM) of Dimethoate. The second group was preincubated with quercetin for 30 min and followed by Dim incubation for 4 h at 37°C. Results Following in vitro incubati...

  14. Analgesic efficacy of continuous femoral nerve block commenced prior to operative fixation of fractured neck of femur

    LENUS (Irish Health Repository)

    Szucs, Szilard

    2012-06-27

    AbstractBackgroundPeripheral nerve blocks are effective in treating acute pain, thereby minimizing the requirement for opiate analgesics. Fractured neck of femur (FNF) is a common, painful injury. The provision of effective analgesia to this cohort is challenging but an important determinant of their functional outcome. We investigated the analgesic efficacy of continuous femoral nerve block (CFNB) in patients with FNF.MethodsFollowing institutional ethical approval and with informed consent, patients awaiting FNF surgery were randomly allocated to receive either standard opiate-based analgesia (Group 1) or a femoral perineural catheter (Group 2). Patients in Group 1 received parenteral morphine as required. Those in Group 2 received a CFNB comprising a bolus of local anaesthetic followed by a continuous infusion of 0.25% bupivacaine. For both Groups, rescue analgesia consisted of intramuscular morphine as required and all patients received paracetamol regularly. Pain was assessed using a visual analogue scale at rest and during passive movement (dynamic pain score) at 30?min following first analgesic intervention and six hourly thereafter for 72 hours. Patient satisfaction with the analgesic regimen received was recorded using verbal rating scores (0-10). The primary outcome measured was dynamic pain score from initial analgesic intervention to 72 hours later.ResultsOf 27 recruited, 24 patients successfully completed the study protocol and underwent per protocol analysis. The intervals from recruitment to the study until surgery were similar in both groups [31.4(17.7) vs 27.5(14.2) h, P?=?0.57]. The groups were similar in terms of baseline clinical characteristics. For patients in Group 2, pain scores at rest were less than those reported by patients in Group 1 [9.5(9.4) vs 31(28), P?=?0.031]. Dynamic pain scores reported by patients in Group 2 were less at each time point from 30?min up to 54 hours [e.g at 6?h 30.7(23.4) vs 67.0(32.0), P?=?0.004]. Cumulative morphine consumption over 72?h was less in Group 2. Patient satisfaction scores were greater in Group 2 [9.4(1.1) vs 7.6(1.8), P?=?0.014].ConclusionsCFNB provides more effective perioperative analgesia than a standard opiate-based regimen for patients undergoing fixation of FNF. It is associated with lesser opiate use and greater patient satisfaction.

  15. Eficacia y efectos secundarios de 3 técnicas analgesicas en el control del dolor postoperatorio en artroplastia de rodilla Efficacy and side effects of three analgesic techniques for postoperative pain management after total knee arthroplasty

    Directory of Open Access Journals (Sweden)

    M. Illescas

    2007-01-01

    Full Text Available Objetivo: El dolor postoperatorio en artroplastia total de rodilla, aún considerándose uno de los más severos, es un reto por resolver. Con nuestro estudio pretendemos analizar y comparar la eficacia analgésica, incidencia y severidad de efectos secundarios de una pauta epidural, otra consistente en bloqueo femoral y una pauta intravenosa con morfina. Material y métodos: Se trata de un estudio observacional retrospectivo en el que se revisan 359 hojas de seguimiento de pacientes sometidos a artroplastia total de rodilla. Según la pauta analgésica que recibieron en el postoperatorio fueron asignados a tres grupos diferentes: a Grupo Femoral (n=56 a los que se realizó bloqueo femoral continuo con ropivacaina al 0,2 %. En todos los casos se asoció un bloqueo del nervio ciático mediante punción única medio-femoral con ropivacaina al 0,2%. b Grupo epidural (n=135 a los que se coloca catéter epidural lumbar mediante el cuál se administra bupivacaina al 0,07%+ fentanilo 2 µg/ml. c Grupo intravenoso (n=168 a los que se administra morfina intravenosa. En todas las pautas el modo de administración es mediante perfusión continua con PCA. Todos los pacientes recibieron como analgesia complementaria Paracetamol IV 1g/6h. Valoramos el grado de analgesia en reposo, náuseas y vómitos, bloqueo motor, sedación, prurito y necesidad de analgesia de rescate en las primeras 24 horas del postoperatorio. Resultados: No se encontraron diferencias significativas en cuanto a eficacia analgésica entre las 3 pautas analizadas. Igualmente, no encontramos diferencias significativas respecto a sedación ni naúseas y vómitos, siendo el bloqueo motor y el prurito superiores en los casos de bloqueo femoral y epidural respectivamente. Conclusiones: Aunque el perfil de efectos secundarios sea discretamente mayor en cuanto a prurito en el grupo epidural y bloqueo motor en el grupo femoral, no podemos afirmar la superioridad en cuanto a eficacia analgésica de ninguna estrategia con respecto a otra.Purpose: Despite the fact that it is expected and intense, postoperative pain after knee arthroplasty is still an unresolved challenge. In our study we intend to analyse and compare analgesic efficacy, incidence and severity of adverse effects resulting from three different techniques: a Epidural analgesia , bFemoral block, and c intravenous analgesia with mor-phine. Patients and Methods: An observational and retrospective study is presented, re-viewing data obtained from 359 patients who had a total knee arthroplasty: Patients were assigned to three different groups, according to the method of pain relief that was prescribed for each of them: a Femoral group (n=56.A continuous femoral block was performed using ropivacaine 0.2%. Sciatic block was associated on each patient (single injection at middle femoral point with ropivacaine 0.2%. b Epidural group (n=135.This figure includes patients in whom an epidural catheter was inserted and bupivacaine 0.07% plus fentanyl 2 mc./mi was administered through the catheter. c Intravenous group (n=168. Intravenous morphine was administered to this group of patients. Each analgesic plan included continuous perfusión of drugs via PCA devices, and paracetamol (lg iv every 6 hourly was prescribed as complementary analgesia in all the cases. Parameters to evalúate: analgesia obtained at rest, nausea and vomiting, motor blockade, sedation, pruritus and complementary analgesia given in the first 24 hours postoperatively. Results: Significative differences were not appreciated at the moment of evaluation of the analgesic efficieney of the three analgesic plans. Equally, sedation, nausea and vomiting had the same incidence in all groups. Motor blockade and pruritus appeared more frequently in the cases treated with femoral block and epidural catheter respectively. Conclusión: We can not assert that any of the analgesic strategies was superior to the others as to its analgesic effectiveness, although pruritus appeared in the epidural group and motor blockade did in the femoral group, as adve

  16. Eficacia y efectos secundarios de 3 técnicas analgesicas en el control del dolor postoperatorio en artroplastia de rodilla / Efficacy and side effects of three analgesic techniques for postoperative pain management after total knee arthroplasty

    Scientific Electronic Library Online (English)

    M., Illescas; J. R., Ríos; R., Rodríguez de la Torre; I., Mojarroa; J. I., Gallego; M., Gil-Fernández.

    2007-01-01

    Full Text Available Objetivo: El dolor postoperatorio en artroplastia total de rodilla, aún considerándose uno de los más severos, es un reto por resolver. Con nuestro estudio pretendemos analizar y comparar la eficacia analgésica, incidencia y severidad de efectos secundarios de una pauta epidural, otra consistente en [...] bloqueo femoral y una pauta intravenosa con morfina. Material y métodos: Se trata de un estudio observacional retrospectivo en el que se revisan 359 hojas de seguimiento de pacientes sometidos a artroplastia total de rodilla. Según la pauta analgésica que recibieron en el postoperatorio fueron asignados a tres grupos diferentes: a) Grupo Femoral (n=56) a los que se realizó bloqueo femoral continuo con ropivacaina al 0,2 %. En todos los casos se asoció un bloqueo del nervio ciático mediante punción única medio-femoral con ropivacaina al 0,2%. b) Grupo epidural (n=135) a los que se coloca catéter epidural lumbar mediante el cuál se administra bupivacaina al 0,07%+ fentanilo 2 µg/ml. c) Grupo intravenoso (n=168) a los que se administra morfina intravenosa. En todas las pautas el modo de administración es mediante perfusión continua con PCA. Todos los pacientes recibieron como analgesia complementaria Paracetamol IV 1g/6h. Valoramos el grado de analgesia en reposo, náuseas y vómitos, bloqueo motor, sedación, prurito y necesidad de analgesia de rescate en las primeras 24 horas del postoperatorio. Resultados: No se encontraron diferencias significativas en cuanto a eficacia analgésica entre las 3 pautas analizadas. Igualmente, no encontramos diferencias significativas respecto a sedación ni naúseas y vómitos, siendo el bloqueo motor y el prurito superiores en los casos de bloqueo femoral y epidural respectivamente. Conclusiones: Aunque el perfil de efectos secundarios sea discretamente mayor en cuanto a prurito en el grupo epidural y bloqueo motor en el grupo femoral, no podemos afirmar la superioridad en cuanto a eficacia analgésica de ninguna estrategia con respecto a otra. Abstract in english Purpose: Despite the fact that it is expected and intense, postoperative pain after knee arthroplasty is still an unresolved challenge. In our study we intend to analyse and compare analgesic efficacy, incidence and severity of adverse effects resulting from three different techniques: a )Epidural a [...] nalgesia , b)Femoral block, and c) intravenous analgesia with mor-phine. Patients and Methods: An observational and retrospective study is presented, re-viewing data obtained from 359 patients who had a total knee arthroplasty: Patients were assigned to three different groups, according to the method of pain relief that was prescribed for each of them: a) Femoral group (n=56).A continuous femoral block was performed using ropivacaine 0.2%. Sciatic block was associated on each patient (single injection at middle femoral point with ropivacaine 0.2%). b) Epidural group (n=135).This figure includes patients in whom an epidural catheter was inserted and bupivacaine 0.07% plus fentanyl 2 mc./mi was administered through the catheter. c) Intravenous group (n=168). Intravenous morphine was administered to this group of patients. Each analgesic plan included continuous perfusión of drugs via PCA devices, and paracetamol (lg iv every 6 hourly) was prescribed as complementary analgesia in all the cases. Parameters to evalúate: analgesia obtained at rest, nausea and vomiting, motor blockade, sedation, pruritus and complementary analgesia given in the first 24 hours postoperatively. Results: Significative differences were not appreciated at the moment of evaluation of the analgesic efficieney of the three analgesic plans. Equally, sedation, nausea and vomiting had the same incidence in all groups. Motor blockade and pruritus appeared more frequently in the cases treated with femoral block and epidural catheter respectively. Conclusión: We can not assert that any of the analgesic strategies was superior to the others as to its analgesic effectiveness, although pruritus appeared in the epidural group a

  17. Analgesic and anti-inflammatory activity of Caryophyllene oxide from Annona squamosa L. bark.

    Science.gov (United States)

    Chavan, M J; Wakte, P S; Shinde, D B

    2010-02-01

    Caryophyllene oxide was isolated from an unsaponified petroleum ether extract of the bark of Annona squamosa and studied for its analgesic and anti-inflammatory activity. Caryophyllene oxide at the doses of 12.5 and 25mg/kg body wt. and unsaponified petroleum ether extract at a dose of 50mg/kg body wt. showed significant central as well as peripheral analgesic, along with anti-inflammatory, activity. These activities of caryophyllene oxide were comparable with the standard drug used in the respective experiments. PMID:19576741

  18. Clinical efficacy of aconitum-containing traditional Chinese medicine for diabetic peripheral neuropathic pain.

    Science.gov (United States)

    Feng, Ling; Liu, Wen-Ke; Deng, Lan; Tian, Jia-Xing; Tong, Xiao-Lin

    2014-01-01

    Diabetic peripheral neuropathy is a common chronic complication of diabetes. Routine clinical management uses analgesics to relieve pain in combination with drugs for nerve repair. The drugs are often not effective for the severe pain cases, and these western medications also have side effects. We report a more effective treatment of diabetic peripheral neuropathic pain using a high dose of a traditional Chinese medicine, aconitum (including both Radix aconite preparata and Radix aconite kusnezoffii), in combination with Huangqi Guizhi Wuwu Tang (i.e., astragalus, cassia twig, white peony root, and spatholobi). In order to achieve stronger analgesic effects, we increased the clinical dosage of aconitum from 15 to 120 g. The aconitum was boiled for 6-8 hours, and licorice was also used to reduce potential toxicities of aconitum. In the four reported cases, the patients' neuropathic pain was remarkably reduced and the EMG profile was also improved with this treatment regimen. Adverse reactions were not observed during the therapy. Thus, aconitum represents a promising and safe treatment for the well-being of patients and their diabetic peripheral neuropathic pain. Future controlled clinical trials using traditional Chinese medicines containing aconitum in treating the neuropathic pain are warranted. PMID:24467538

  19. In vitro Effects of Beet Root Juice on Stimulated and Unstimulated Peripheral Blood Mononuclear Cells

    Directory of Open Access Journals (Sweden)

    Christiana Winkler

    2005-01-01

    Full Text Available Intake of fruits and vegetables rich in antioxidants is suggested to reduce the incidence of cancer and coronary heart disease in humans. Exceptional antioxidant activity of beet root extracts has been reported. Likewise in animal models, e.g., extracts of red beetroot Beta vulgaris var. rubra revealed significant tumor inhibitory effects. Red beetroot concentrate is universally permitted as a food ingredient. In this study, effects of a commercially available beetroot juice on freshly isolated human peripheral blood mononuclear cells stimulated with the mitogens phytohaemagglutinin and concanavalin A were investigated in vitro. Tryptophan degradation and neopterin formation were monitored in culture supernatants to determine effects of test substances on immunobiochemical pathways which both are induced by the pro-inflammatory cytokine interferon-?. Compared to unstimulated cells, the mitogens induced significant formation of neopterin and degradation of tryptophan which is reflected by increasing concentrations of kynurenine together with diminished tryptophan levels in supernatants. Addition of beetroot extracts significantly suppressed these mitogen-induced changes, e.g. the rate of neopterin production as well as tryptophan degradation was dose-dependently suppressed. Our data show that beetroot extract is able to counteract pro-inflammatory cascades in peripheral blood mononuclear cells. Because inflammation is strongly involved in the development and progression of several clinical conditions including coronary heart disease and cancer, beneficial effect of beetroot extract may relate to this anti-inflammatory capacity.

  20. Effect of peripheral benzodiazepine receptor ligands on lipopolysaccharide-induced tumor necrosis factor activity in thioglycolate-treated mice.

    OpenAIRE

    Matsumoto, T.; Ogata, M.; Koga, K.; Shigematsu, A.

    1994-01-01

    To investigate the effect of peripheral and central benzodiazepine receptor ligands on lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF) activity in mouse macrophages, three types of ligands, 4'-chlorodiazepam (pure peripheral), midazolam (mixed), and clonazepam (pure central), were compared. Midazolam and 4'-chlorodiazepam significantly suppressed LPS (1-microgram/ml)-induced TNF activity in thioglycolate-elicited mouse macrophages. In every concentration examined (0.001 to 100 mi...

  1. Use of simple analgesics in rheumatoid arthritis.

    OpenAIRE

    Gibson, T.; Clark, B.

    1985-01-01

    The usefulness of anti-inflammatory drugs in rheumatoid arthritis (RA) is beyond dispute. The role of simple analgesics is less clear and has been disputed. A survey of 21 rheumatologists indicated that a majority sometimes supplemented anti-inflammatory treatment of RA with simple analgesics. A random sample of 120 RA patients treated by the same doctors revealed that 47% ranked pain relief as the most desirable objective of their treatment and 54% were taking analgesics regularly. Of those ...

  2. COMPARATIVE EFFICACY OF GABAPENTIN A CONVENTIONAL ANTICONVULSANT WITH CONVENTIONAL ANALGESIC TREMADOL IN VISCERAL PAIN MODEL OF RODENTS

    OpenAIRE

    Saurabh Kansal; Priti Sinha

    2014-01-01

    Carabmazepine is an established drug for trigeminal neuralgia while gabapentin has been tried in postoperative pain but its effectiveness in visceral pain and when compared to conventional analgesics needs to be evaluated.The present study was planned to study the analgesic effects of gabapentin in animal pain model of visceral nociception like writhing test and to compare it with conventional analgesic tremadol. This study has been carried out for evaluation of role of gabapentin in visceral...

  3. Effects of a Traditional Japanese Medicine Goshajinkigan, Tokishigyakukagoshuyushokyoto on the Warm and Cold Sense Threshold and Peripheral Blood Flow

    Directory of Open Access Journals (Sweden)

    Rika Tsukada

    2014-03-01

    Full Text Available The purpose of this study was to investigate the effects of a traditional Japanese medicine Goshajinkigan (TJ-107 and Tokishigyakukagoshuyushokyoto (TJ-38 on warm sense threshold, cold sense threshold and the peripheral blood flow. 31 healthy volunteers (control group: 9people, TJ-107 group: 12 people, TJ-38group:10 people were examined. Drugs administered 2.5 g a dose. Analysis was before and after 1 hour dosage. The warm and cold sense threshold in the thenar of the non-handedness site of these subjects was measured using a thermostimulator (Intercross-200, Intercross Co., Tokyo, Japan. The peripheral blood flow in the finger of the non-handedness site of these subjects was measured using a full-field laser perfusion imager (FLPI, Moor Instruments Ltd., England. Control: The vehicle had no significant effect on the warm sense threshold, cold sense threshold and the peripheral blood flow. TJ-107: The warm sense threshold and cold sense threshold were significantly decreased, and the reaction latency of cold sense was significantly shortening. The peripheral blood flow was significantly increased second and third finger at 115.6%, 119.3%, respectively. TJ-38: The cold sense threshold and the reaction latency of cold sense were significantly increased. The peripheral blood flow was significantly increased second and third finger with 114.3%, 112.8%, respectively. These results suggest that TJ-107 and TJ-38 have effects on the changed warm sense threshold, cold sense threshold and increased peripheral blood flow.

  4. Peripheral, but not central effects of cannabidiol derivatives: mediation by CB(1) and unidentified receptors.

    Science.gov (United States)

    Fride, Ester; Ponde, Datta; Breuer, Aviva; Hanus, Lumir

    2005-06-01

    Delta-9 tetrahydrocannabinol (Delta(9)-THC) and (-)-cannabidiol ((-)-CBD) are major constituents of the Cannabis sativa plant with different pharmacological profiles: (Delta(9)-THC activates cannabinoid CB(1) and CB(2) receptors and induces psychoactive and peripheral effects. (-)-CBD possesses no, or very weak affinity for these receptors. We tested a series of (+)- and (-)-CBD derivatives for central and peripheral effects in mice. None of the (-)-CBD derivatives were centrally active, yet most inhibited intestinal motility. Of the five (+)-CBD derivatives, all with CB(1) receptor affinity, only (+)-7-OH-CBD-DMH (DMH=1,1-dimethylheptyl), acted centrally, while all five arrested defecation. The effects of (+)-CBD-DMH and (+)-7-OH-CBD-DMH were inhibited by the CB(1) receptor antagonist SR141716. The CB(2) receptor antagonist SR144528, and the vanilloid TRPV1 receptor antagonist capsazepine, had no influence. Further, the (-)-CBD derivatives (-)-7-COOH-CBD and (-)-7-COOH-CBD-DMH, displayed antiinflammatory activity. We suggest that (+)-CBD analogues have mixed agonist/antagonist activity in the brain. Second, (-)-CBD analogues which are devoid of cannabinoid receptor affinity but which inhibit intestinal motility, suggest the existence of a non-CB(1), non-CB(2) receptor. Therefore, such analogues should be further developed as antidiarrheal and/or antiinflammatory drugs. We propose to study the therapeutic potential of (-)- and (+)-CBD derivatives for complex conditions such as inflammatory bowel disease and cystic fibrosis. PMID:15910887

  5. The effect of Ginkgo extract EGb761 in cisplatin-induced peripheral neuropathy in mice

    International Nuclear Information System (INIS)

    Neuroprotective effect of Ginkgo biloba extract EGb761 in cisplatin (cis-diamminedi-chloroplatinum, or CDDP)-induced peripheral neuropathy was investigated. Swiss albino mice were treated with CDDP, 2 mg/kg ip twice a week for nine times. One group of the animals also received EGb761 in the drinking water at an estimated dosage of 100 mg/kg per day. Two other groups received vehicle (control) or EGb761 only. Development of neuropathy was evaluated with changes in sensory nerve conduction velocity (NCV). Following the treatments, dorsal root ganglia (DRGs) were microscopically examined and some were cultured for 3 days. EGb761 proved effective in preventing the reduction in NCV (P < 0.0001) caused by CDDP. CDDP caused a decrease in the number of migrating cells (P < 0.01) and in the length of outgrowing axons (P < 0.01) while EGb761 treatment prevented the latter. CDDP led to smaller nuclear and somatic sizes in neurons (P < 0.01), while with EGb761 co-administration, both were close to control values. Animals having EGb761 only had similar results with controls. In conclusion, EGb761 was found to be effective in preventing some functional and morphological deteriorations in CDDP-induced peripheral neuropathy

  6. Effect of glare on reaction time for peripheral vision at mesopic adaptation.

    Science.gov (United States)

    Aguirre, Rolando C; Colombo, Elisa M; Barraza, José F

    2011-10-01

    When a bright light is present in the field of view, visibility is dramatically reduced. Many studies have investigated the effect of glare on visibility considering foveal vision. However, the effects on peripheral vision have received little attention. In a previous work [J. Opt. Soc. Am. A 25, 1790 (2008)], we showed that the effect of glare on reaction time (RT) for foveal vision at mesopic adaptation depends on the stimulus spatial frequency. In this work, we extend this study to peripheral vision. We measured the RT of achromatic sinusoidal gratings as a function of contrast for a range of spatial frequency, and eccentricity, and for two glare levels, in addition to the no-glare condition. Data were fitted with Piéron's law, following a linear relationship. We found that glare increases the slope of these lines for all conditions. These slopes seem to depend critically on eccentricity for 4 cycles/degree (c/deg), but not for 1 and 2 c/deg. We explain our results in terms of the contrast sensitivity (gain) of the underlying detection mechanisms. PMID:21979526

  7. Stimulation of peripheral Kappa opioid receptors inhibits inflammatory hyperalgesia via activation of the PI3K?/AKT/nNOS/NO signaling pathway

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    Cunha Thiago M

    2012-02-01

    Full Text Available Abstract Background In addition to their central effects, opioids cause peripheral analgesia. There is evidence showing that peripheral activation of kappa opioid receptors (KORs inhibits inflammatory pain. Moreover, peripheral ?-opioid receptor (MOR activation are able to direct block PGE2-induced ongoing hyperalgesia However, this effect was not tested for KOR selective activation. In the present study, the effect of the peripheral activation of KORs on PGE2-induced ongoing hyperalgesia was investigated. The mechanisms involved were also evaluated. Results Local (paw administration of U50488 (a selective KOR agonist directly blocked, PGE2-induced mechanical hyperalgesia in both rats and mice. This effect was reversed by treating animals with L-NMMA or N-propyl-L-arginine (a selective inhibitor of neuronal nitric oxide synthase, nNOS, suggesting involvement of the nNOS/NO pathway. U50488 peripheral effect was also dependent on stimulation of PI3K?/AKT because inhibitors of these kinases also reduced peripheral antinociception induced by U50488. Furthermore, U50488 lost its peripheral analgesic effect in PI3K? null mice. Observations made in vivo were confirmed after incubation of dorsal root ganglion cultured neurons with U50488 produced an increase in the activation of AKT as evaluated by western blot analyses of its phosphorylated form. Finally, immunofluorescence of DRG neurons revealed that KOR-expressing neurons also express PI3K? (? 43%. Conclusions The present study indicates that activation of peripheral KORs directly blocks inflammatory hyperalgesia through stimulation of the nNOS/NO signaling pathway which is probably stimulated by PI3K?/AKT signaling. This study extends a previously study of our group suggesting that PI3K?/AKT/nNOS/NO is an important analgesic pathway in primary nociceptive neurons.

  8. Effects of peripheral ?, ?, and ?-opioid receptor agonists on the levels of anxiety and motor activity of rats.

    Science.gov (United States)

    Alexeeva, E V; Nazarova, G A; Sudakov, S K

    2012-09-01

    The effects of intragastric administration of ?-, ?, and ?-opioid receptor agonists DAMGO, DADLE, and ICI 204,448, respectively, on the anxiety and motor activity of rats in an elevated plus-maze were studied. Peripheral administration of ICI 204,448 produced an anxiolytic effect, but had no effect on motor activity of rats. DAMGO and DADLE reduced motor activity; DADLE also increased anxiety. The data on the opposite effects of ICI 204,448 and DADLE on anxiety confirmed our previous hypothesis on the interactions between the central and peripheral components of the endogenous opioid system. PMID:23113268

  9. Anti-Inflammatory and Analgesic Effects of Pyeongwisan on LPS-Stimulated Murine Macrophages and Mouse Models of Acetic Acid-Induced Writhing Response and Xylene-Induced Ear Edema

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    You-Chang Oh

    2015-01-01

    Full Text Available Pyeongwisan (PW is an herbal medication used in traditional East Asian medicine to treat anorexia, abdominal distension, borborygmus and diarrhea caused by gastric catarrh, atony and dilatation. However, its effects on inflammation-related diseases are unknown. In this study, we investigated the biological effects of PW on lipopolysaccharide (LPS-mediated inflammation in macrophages and on local inflammation in vivo. We investigated the biological effects of PW on the production of inflammatory mediators, pro-inflammatory cytokines and related products as well as the activation of nuclear factor kappa B (NF-?B and mitogen-activated protein kinases (MAPKs in LPS-stimulated macrophages. Additionally, we evaluated the analgesic effect on the acetic acid-induced writhing response and the inhibitory activity on xylene-induced ear edema in mice. PW showed anti-inflammatory effects by inhibiting the production of nitric oxide (NO, tumor necrosis factor-? (TNF-? and interleukin-6 (IL-6 and interleukin-1? (IL-1?. In addition, PW strongly suppressed inducible nitric oxide synthase (iNOS, a NO synthesis enzyme, induced heme oxygenase-1 (HO-1 expression and inhibited NF-?B activation and MAPK phosphorylation. Also, PW suppressed TNF-?, IL-6 and IL-1? cytokine production in LPS-stimulated peritoneal macrophage cells. Furthermore, PW showed an analgesic effect on the writhing response and an inhibitory effect on mice ear edema. We demonstrated the anti-inflammatory effects and inhibitory mechanism in macrophages as well as inhibitory activity of PW in vivo for the first time. Our results suggest the potential value of PW as an inflammatory therapeutic agent developed from a natural substance.

  10. Anti-inflammatory and analgesic effects of pyeongwisan on LPS-stimulated murine macrophages and mouse models of acetic acid-induced writhing response and xylene-induced ear edema.

    Science.gov (United States)

    Oh, You-Chang; Jeong, Yun Hee; Cho, Won-Kyung; Ha, Jeong-Ho; Gu, Min Jung; Ma, Jin Yeul

    2015-01-01

    Pyeongwisan (PW) is an herbal medication used in traditional East Asian medicine to treat anorexia, abdominal distension, borborygmus and diarrhea caused by gastric catarrh, atony and dilatation. However, its effects on inflammation-related diseases are unknown. In this study, we investigated the biological effects of PW on lipopolysaccharide (LPS)-mediated inflammation in macrophages and on local inflammation in vivo. We investigated the biological effects of PW on the production of inflammatory mediators, pro-inflammatory cytokines and related products as well as the activation of nuclear factor kappa B (NF-?B) and mitogen-activated protein kinases (MAPKs) in LPS-stimulated macrophages. Additionally, we evaluated the analgesic effect on the acetic acid-induced writhing response and the inhibitory activity on xylene-induced ear edema in mice. PW showed anti-inflammatory effects by inhibiting the production of nitric oxide (NO), tumor necrosis factor-? (TNF-?) and interleukin-6 (IL-6) and interleukin-1? (IL-1?). In addition, PW strongly suppressed inducible nitric oxide synthase (iNOS), a NO synthesis enzyme, induced heme oxygenase-1 (HO-1) expression and inhibited NF-?B activation and MAPK phosphorylation. Also, PW suppressed TNF-?, IL-6 and IL-1? cytokine production in LPS-stimulated peritoneal macrophage cells. Furthermore, PW showed an analgesic effect on the writhing response and an inhibitory effect on mice ear edema. We demonstrated the anti-inflammatory effects and inhibitory mechanism in macrophages as well as inhibitory activity of PW in vivo for the first time. Our results suggest the potential value of PW as an inflammatory therapeutic agent developed from a natural substance. PMID:25569097

  11. Morphological content of rat peripheral blood in combined effect of radiation factors

    International Nuclear Information System (INIS)

    Combined effect of two radiation factors: a single x-irradiation and internal irradiation due to chronic intake of 90Sr and 144Ce radionuclides, on blood morphology is studied. In combined effect of radiation factors on morphological blood content 3 periods are distinguished. In the first period the blood changes correspond to an acute radiation injury without severe consequences. The second normalization period was muck shorter than in case of external irradiation alone. In the third period external preirradiation was complicated by aftereffects of long-term 90Sr and 144Ce radionuclide intake. The experiment have shown that combined radiation delayed effects result in deep shifts in morphology of rat peripheral blood

  12. Reduction of the spatial stroop effect by peripheral cueing as a function of the presence/absence of placeholders.

    Science.gov (United States)

    Luo, Chunming; Lupiáñez, Juan; Funes, María Jesús; Fu, Xiaolan

    2013-01-01

    In a paradigm combining spatial Stroop with spatial cueing, the current study investigated the role of the presence vs. absence of placeholders on the reduction of the spatial Stroop effect by peripheral cueing. At a short cue-target interval, the modulation of peripheral cueing over the spatial Stroop effect was observed independently of the presence/absence of placeholders. At the long cue-target interval, however, this modulation over the spatial Stroop effect only occurred in the placeholders-present condition. These findings show that placeholders are modulators but not mediators of the reduction of the spatial Stroop effect by peripheral cueing, which further favor the cue-target integration account. PMID:23894485

  13. Contrasting effects of transcranial direct current stimulation on central and peripheral visual fields.

    Science.gov (United States)

    Costa, Thiago L; Gualtieri, Mirella; Barboni, Mirella T S; Katayama, Rafael K; Boggio, Paulo S; Ventura, Dora F

    2015-05-01

    Recent research suggested that transcranial direct current stimulation (tDCS) can affect visual processing and that it can be useful in visual rehabilitation. Nevertheless, there are still few investigations on the subject. tDCS selectivity and the extent of its outcomes on visual perception are still to be assessed. Here, we investigate whether central and peripheral visual fields are equally affected by tDCS. We also tried to reproduce a previous work that has evaluated tDCS effects on the central visual field only (Kraft et al. 207:283-290, 2010). Fifteen healthy subjects participated in this randomized repeated-measure design study and received 1.5-mA anodal, cathodal and sham stimulation in different sessions, while performing 10-2 and 60-4 protocols in an automated perimeter. Anodal tDCS significantly decreased thresholds, but was limited to the most eccentric regions of the visual field measured (60°). This suggests that tDCS might be used for rehabilitation of peripheral visual field losses. We did not replicate the excitatory tDCS effect in the central visual field as previously reported by another group. Instead, we observed a trend toward an inhibitory (yet not statistically significant) effect of anodal tDCS on the central field. This might be explained by methodological differences. These results highlight that although tDCS is a technique with a low focality in the spatial domain, its effects might be highly focal in a functional domain. When taken together with previous findings, this also suggests that tDCS may have a differential effect on different retinotopic areas in the brain. PMID:25650104

  14. Effect of peripheral administration of peptide ligands of ?-opioid receptors on anxiety level and locomotor activity of rats.

    Science.gov (United States)

    Sudakov, S K; Nazarova, G A; Kolyasnikova, K N; Kolpakov, A A; Bashkatova, V G

    2011-10-01

    We studied the effect of intragastric administration of a peptide ?-opioid receptor agonist DADLE and peptide ?-opioid receptor antagonist ICI 174.864 on anxiety and locomotor activity of rats. Peripheral administration of ICI 174.864 produced an anxiolytic effect, but did not modulate locomotor activity of rats. Agonist DADLE in doses of 50 and 100 ?g/kg increased anxiety, but decreased locomotor activity of rats. Our results indicate that ICI 174.864 and DADLE produce opposite effects on anxiety in rats. These data support our hypothesis on the interaction between the central and peripheral compartments of the endogenous opioid system. PMID:22485201

  15. Effects of manganese exposure on iron metabolism in peripheral blood of exposed population

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    Yun-gang XIONG

    2012-11-01

    Full Text Available Objectives ?To investigate the adverse effect of manganese exposure on the iron metabolism in peripheral blood of professionally exposed workers. Methods ?The manganese in air was collected using personal air sampler, and the time weighted average (TWA concentration of exposure to manganese was then calculated. The subjects were divided into exposure group (n=85 and control group (n=80 based on the exposure doses they received. The concentrations of iron and manganese in the plasma and blood cells of the subjects were determined using flame atomic absorption detector and graphite furnace atomic absorption detector. Serum ferritin, transferrin, transferrin receptor and total iron binding capacity were determined using enzyme linked immunosorbent assay. Results ?The manganese contents in both plasma and blood cells were much higher in exposure group than in control group (P 0.05. It was revealed by linear correlation analysis that no linear correlation existed between the professional exposure time and manganese and iron contents in both plasma and blood cells, serum ferrin, transferrin, transferring receptor and total iron binding capacity (P>0.05. Conclusion ?The long-term exposure to high dose manganese may result in an imbalance of iron metabolism in the peripheral blood in exposed population, manifesting a decrease of plasma iron and serum transferrin receptors, and an increase of serum transferrin.

  16. Combined effects of noise and hand-arm vibration on auditory organ and peripheral circulation

    Science.gov (United States)

    Miyakita, T.; Miura, H.; Futatsuka, M.

    1991-12-01

    This paper first presents an overview of an epidemiological study on noise-induced hearing loss (NIHL) in relation to vibration-induced white finger (VWF). Secondly, the results obtained in a model experiment with a chain-saw under laboratory conditions are discussed from the viewpoints of elucidating the etiological mechanisms of VWF and NIHL. In the epidemiological study, in which 499 chain-saw workers were examined, chain-saw workers with VWF showed a significantly greater hearing loss at high frequencies than those without VWF. Next, an experimental study was designed to determine whether a combination of noise and vibration produced more pronounced changes in temporary shifts of finger skin temperature and temporary threshold shift (TTS) of hearing than those resulting from exposure to either stress alone. The results suggested that noise might play a part in inducing the constriction of the peripheral vessels seen with local exposure to vibration, and that hand-arm vibration may produce an additive effect on the noise-induced TTS. Furthermore, finger skin temperature and finger blood flow were measured simultaneously as indicators of peripheral circulatory movement for five healthy subjects. The relation between the synergistic action of noise and vibration and the participation of the sympathetic nervous system are also discussed.

  17. Effect of regular aerobic exercise with ozone exposure on peripheral leukocyte populations in Wistar male rats

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    Afshar Jafari

    2009-09-01

    Full Text Available

    • BACKGROUND: The immune system in endurance athletes may be at risk for deleterious effects of gasous pollutants such as ambient ozone. Therefore, this study was performed to assess the effect of regular aerobic exercise with ozone exposure on peripheral leukocytes populations in male Wistar rats.
    • METHODS: Twenty eight 8 weeks old rats were selected and randomly divided into four groups of ozone-unexposed anduntrained (control or group 1, n = 6, ozone-exposed and untrained (group 2, n = 6, ozone-unexposed and trained (group 3, n = 8, ozone-exposed and trained (group 4, n = 8. All animals in groups 3 and 4 were regularly running (20 m/min, 30 min/day on a treadmill for 7 weeks (5 day/week. After the last ozone exposure [0.3 ppm, 30 min per sessions], blood samples were obtained from the cardiac puncture and hematological parameters as well as blood lactate were measured using automatic analyzers. Data were expressed as means (± SD and analyzed by ANOVA and Pearson's correlation tests at p < 0.05.
    • RESULTS: All the hematological parameters differences (except RBC and hemoglobin rate were significantly higher in the trained groups (p < 0.001. However, ozone-induced leukocytosis in the trained (but not in the sedentary rats was statistically higher than in the counterpart groups.
    • CONCLUSIONS: Repeated acute ozone exposure has more additive effect on peripheral leukocyte counts in active animals. But, more researches are needed to identify effects of ozone exposure on other components of the immune system in athletes and non-athletes.
    • KEYWORDS: Moderate Aerobic Exercise, Ozone Exposure,  eukocytosis, Wistar Rats.

  18. Peripheral degenerative joint diseases

    Directory of Open Access Journals (Sweden)

    Nilzio Antonio da Silva

    2008-03-01

    Full Text Available Osteoarthritis, a degenerative joint disease, is the most commonrheumatic disorder mainly in a geriatric population. Manifestationsare pain, stiffness and functional loss in the affected joint.According to etiology it is classifi ed as primary (or idiopathicand secondary. Some risk factors for disease development aregenetics, race, age, sex, obesity, occupational activities andarticular biomechanics. Pathogenesis is the same for any cause orlocalization, being catabolic alterations, with synthesis, inhibitionand reparing intent of the cartilage matrix. Metalloproteinases andcytokines (IL-1,IL-6,TNF-? actions promote infl ammatory reactionand cartilage degradation. Pain, the most important symptom,does not correlate with radiologic fi ndings. Peripheral osteoarthritisoccurs predominantly in the knee, hip and hand. Diagnosis is basedon clinical features, laboratorial tests and radiological changes.Rheumatological associations’ guidelines for treatment includenon-pharmacologic (education, physiotherapy, assistive devices,and pharmacologic (analgesics, anti-infl ammatory drugs therapyand surgery. Arthroplasty seems to work better than medicines, butshould be used if other treatments have failed.

  19. Analgesic and anti-inflammatory activity of Argyreia speciosa root

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    Bachhav R

    2009-01-01

    Full Text Available Objective: To study analgesic and anti-inflammatory activities of a methanolic extract (ME of Argyreia speciosa (AS root powder. Materials and Methods: The study was carried out using male albino mice (20-25 gm and male wistar rats (100-150gm. The ME was prepared using soxhlet extraction process. The effect of ME of A. speciosa was investigated for analgesic activity using acetic acid-induced abdominal constriction, tail immersion method and hot plate method. The anti-inflammatory activity of ME of AS roots was studied using carrageenan-induced rat paw edema. Result: The ME of A. speciosa root was used in pain and inflammation models. The analgesic activity of AS at the dose of (30,100, and 300 mg/kg p.o showed significant (P< 0.01 decrease in acetic acid-induced writhing, whereas ME of A. speciosa at the dose of (100, 300 mg/kg p.o showed significant (P< 0.01 increase in latency to tail flick in tail immersion method and elevated mean basal reaction time in hot plate method. The ME of the A. speciosa at doses (30, 100, and 300mg/kg showed significant (P < 0.01 inhibition of carrageenan induced hind paw edema in rats. Conclusion: The ME of A. speciosa showed significant analgesic and anti-inflammatory activity in mice and rat.

  20. Preoperative low-dose ketamine has no preemptive analgesic effect in opioid-naïve patients undergoing colon surgery when nitrous oxide is used - a randomized study [v1; ref status: indexed, http://f1000r.es/4bp

    Directory of Open Access Journals (Sweden)

    Beatriz Nistal-Nuño

    2014-09-01

    Full Text Available Background: The analgesic properties of ketamine are associated with its non-competitive antagonism of the N-methyl-D-aspartate receptor; these receptors exhibit an excitatory function on pain transmission and this binding seems to inhibit or reverse the central sensitization of pain. In the literature, the value of this anesthetic for preemptive analgesia in the control of postoperative pain is uncertain. The objective of this study was to ascertain whether preoperative low-dose ketamine reduces postoperative pain and morphine consumption in adults undergoing colon surgery. Methods: In a double-blind, randomized trial, 48 patients were studied. Patients in the ketamine group received 0.5 mg/kg intravenous ketamine before surgical incision, while the control group received normal saline. The postoperative analgesia was achieved with a continuous infusion of morphine at 0.015 mg?kg?¹?h?¹ with the possibility of 0.02 mg/kg bolus every 10 min. Pain was assessed using the Visual Analog Scale (VAS, morphine consumption, and hemodynamic parameters at 0, 1, 2, 4, 8, 12, 16, and 24 hours postoperatively. We quantified times to rescue analgesic (Paracetamol, adverse effects and patient satisfaction. Results: No significant differences were observed in VAS scores between groups (P>0.05, except at 4 hours postoperatively (P=0.040. There were no differences in cumulative consumption of morphine at any time point (P>0.05. We found no significant differences in incremental postoperative doses of morphine consumption in bolus, except at 12 h (P =0.013 and 24 h (P =0.002. The time to first required rescue analgesia was 70 ± 15.491 min in the ketamine group and 44 ± 19.494 min in the control (P>0.05. There were no differences in hemodynamic parameters or patient satisfaction (P>0.05. Conclusions: Preoperative low-dose-ketamine did not show a preemptive analgesic effect or efficacy as an adjuvant for decreasing opioid requirements for postoperative pain in patients receiving intravenous analgesia with morphine after colon surgery.

  1. Theacrine, a purine alkaloid with anti-inflammatory and analgesic activities.

    Science.gov (United States)

    Wang, Yuanyuan; Yang, Xiaorong; Zheng, Xinqiang; Li, Jing; Ye, Chuangxing; Song, Xiaohong

    2010-09-01

    The anti-inflammatory and analgesic effects of theacrine (1, 3, 7, 9-tetramethyluric acid), a purine alkaloid which is abundantly present in Camellia kucha, were investigated. Xylene-induced ear edema, acetic acid-induced vascular permeability and lambda-carrageenan-induced paw edema were used to investigate anti-inflammatory activity, and acetic acid-induced writhing and hot-plate tests were used to determine analgesic effect. Oral administration of theacrine (8-32 mg/kg) induced dose-related anti-inflammatory and analgesic effects. On the other hand, oral caffeine administration (8-32 mg/kg) did not show an inhibitory effect on the inhibition of inflammatory response or cause analgesia. Additionally, the result of the acute toxicity test showed that the LD(50) of theacrine was 810.6 mg/kg (769.5-858.0mg/kg). The data obtained suggest theacrine possessed analgesic and anti-inflammatory activities. PMID:20227468

  2. Investigation of the effect of telmisartan on experimentally induced peripheral nerve injury in rats.

    Science.gov (United States)

    Yuksel, Tugba Nurcan; Halici, Zekai; Demir, Recep; Cakir, Murteza; Calikoglu, Cagatay; Ozdemir, Gokhan; Unal, Deniz

    2014-08-26

    Aim: The aim of this study was to investigate the effects of telmisartan on nerve healing in a rat peripheral nerve injury model. Material and method: Thirty adult male Wistar albino rats were divided into five groups: healthy, axonotmesis, anastomosis, axonotmesis+10 mg/kg telmisartan and anastomosis+10 mg/kg telmisartan. Walking track analyses were performed 4 weeks after the surgery. The right sciatic nerves of all the animals were exa- mined histopathologically, stereologically and molecularly. Results: Many badly damaged axons were detected in the axonotmesis group, in addition to enlarged spaces between the axons. In the anastomosis group, both ir- regular and degenerated axons at different severities were observed. The sections of the telmisartan group after the axonotmesis were similar to those of the healthy group. The sections of the telmisartan group after the anastomosis were similar to those of the healthy group and the telmisartan group after the axonotmesis. Interleukin-1 beta (IL-1?) gene expression increased in both the axonotmesis and the anastomosis groups when compared with the healthy group. Telmisartan had a significant down-regulatory effect on IL-1? expression. Caspase-3 mRNA expression was significantly increased in the anastomosis group, and the administration of telmisartan in this group significantly decreased this rise in caspase-3 mRNA expression. As a functional outcome, telmisartan also increased the walking distance of the rats after axonotmesis and anastomosis. Conclusion: The histopathological, stereological, functional and molecular data suggest that telmisartan improves nerve regeneration in peripheral nerve injuries by inhibiting inflammatory cytokine IL-1? and apoptotic caspase-3. PMID:25069044

  3. Adamantyl Analogues of Paracetamol as Potent Analgesic Drugs via Inhibition of TRPA1

    Science.gov (United States)

    Fresno, Nieves; Pérez-Fernández, Ruth; Goicoechea, Carlos; Alkorta, Ibon; Fernández-Carvajal, Asia; de la Torre-Martínez, Roberto; Quirce, Susana; Ferrer-Montiel, Antonio; Martín, M. Isabel; Goya, Pilar; Elguero, José

    2014-01-01

    Paracetamol also known as acetaminophen, is a widely used analgesic and antipyretic agent. We report the synthesis and biological evaluation of adamantyl analogues of paracetamol with important analgesic properties. The mechanism of nociception of compound 6a/b, an analog of paracetamol, is not exerted through direct interaction with cannabinoid receptors, nor by inhibiting COX. It behaves as an interesting selective TRPA1 channel antagonist, which may be responsible for its analgesic properties, whereas it has no effect on the TRPM8 nor TRPV1 channels. The possibility of replacing a phenyl ring by an adamantyl ring opens new avenues in other fields of medicinal chemistry. PMID:25438056

  4. Analgesic activity of Nyctanthes arbor-tristis leaves in rodents

    OpenAIRE

    Chaitali Pattanayak; Pratyay Pratim Datta

    2013-01-01

    Aim: Traditional medicine practitioners use leaf extract of Nyctanthes arbor-tristis for symptomatic relief of arthritis. Studies indicate the anti-inflammatory effect of this extract. The objective of the present study was to investigate the analgesic effect of leaves of Nyctanthes arbor-tristis linn in rodents. Methods: The leaf extract was prepared by and #8220;maceration and #8221; with 90% ethanol at room temperature, filtered and the filtrate evaporated to dryness. The extract was ...

  5. Anti-inflammatory and analgesic activity of different fractions of Boswellia serrata

    OpenAIRE

    Sharma, A.; Bhatia, S.; Kharya, M. D.; Gajbhiye, V.; Ganesh, N.; Namdeo, A. G.; Mahadik, K. R.

    2011-01-01

    The study was designed to investigate the anti-inflammatory and analgesic effect of different fractions of Boswellia serrata. The effect of different fractions of Boswellia serrata were studied using carrageenan induced paw edema, acetic acid induced writhing response, formalin induced pain, hot plate and tail flick method for studying anti-inflammatory and analgesic activity, respectively. The different fractions of B. serrata, essential oil (10 ml/kg), gum (100 mg/kg, resin (100 mg...

  6. Acetate free biofiltration. Effects on peripheral blood monocyte activation and cytokine release.

    Science.gov (United States)

    Carozzi, S; Nasini, M G; Caviglia, P M; Schelotto, C; Santoni, O; Atti, M

    1992-01-01

    Acetate free biofiltration (AFB), a new hemodiafiltration (HDF) technique characterized by a buffer free dialysate and postdilution infusion of a sterile HCO3 solution, was recently proposed as an alternative to HDF performed with acetate or bicarbonate dialysate. To evaluate the effects of dialysate buffer on immune cell activation, release of interleukin-1 (IL-1), tumor necrosis factor (TNF), prostaglandin E2 (PGE2), and leukotriene B4 (LTB4) from peripheral blood monocytes was studied in 12 uremic patients before and after HDF with polyacrylonitrile membranes (Filtral 12, Hospal Laboratories, Bologna, Italy) and consecutive dialysis with acetate, bicarbonate, and AFB. Data were correlated with the monocyte cytoplasmic concentration of Ca++, an index of early cell activation. Levels of bacterial endotoxins in the acetate, bicarbonate, buffer free dialysate, and infusate for AFB were also determined. Results showed that release of IL-1, PGE2, and LTB4, was greater after HDF with acetate than with bicarbonate; after bicarbonate dialysis, however, TNF production was significantly higher. On the other hand, after AFB, minimal production of these cytokines was seen and TNF, in particular, was undetectable. There was a direct correlation between release of cytokines in the monocytes and cytoplasmic Ca++ content. In the bicarbonate dialysate, detectable levels of bacterial endotoxins were found, whereas the acetate, buffer free dialysate, and infusate were endotoxin free. It was concluded that acetate dialysis directly activates peripheral blood monocytes to produce IL-1, PGE2, and LTB4, whereas bicarbonate induced TNF activation occurs through endotoxins. In AFB, which uses a buffer free dialysate and sterile bicarbonate infusion, monocyte activation is negligible. PMID:1313318

  7. Peripheral PDLIM5 expression in bipolar disorder and the effect of olanzapine administration

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    Zain Mohd

    2012-10-01

    Full Text Available Abstract Background One of the genes suggested to play an important role in the pathophysiology of bipolar disorder (BPD is PDLIM5, which encodes LIM domain protein. Our main objective was to examine the effect of olanzapine treatment on PDLIM5 mRNA expression in the peripheral blood leukocytes of BPD patients. Methods We measured the expression of PDLIM5 mRNA from 16 patients with BPD Type I after 0, 4, and 8 weeks of treatment with olanzapine using quantitative real-time PCR. The Young Mania Rating Scale was used to evaluate the severity of manic symptoms in BPD patients. We also compared PDLIM5 mRNA expression in treatment-naïve BPD patients with that in healthy control subjects. Results No significant difference was found in PDLIM5 mRNA expression between patients before olanzapine treatment and following 4 and 8 weeks of treatment (p>0.05. Although we observed a significant reduction in the severity of manic symptoms in all BPD patients (pPDLIM5 mRNA (p>0.05. Interestingly, PDLIM5 mRNA expression differed significantly between treatment-naïve BPD patients and healthy control subjects (p=0.002. Conclusion PDLIM5 mRNA expression did not appear to be a reflection of the efficacy of olanzapine in reducing the manic symptoms of BPD. The significant difference in expression of PDLIM5 mRNA in the peripheral blood leukocytes of treatment-naïve BPD patients versus that of healthy control subjects, however, suggests that it may be a good biological marker for BPD.

  8. Apoptotic effects of tamoxifen on leukocytes from horse peripheral blood and bronchoalveolar lavage fluid.

    Science.gov (United States)

    Sarmiento, J; Perez, B; Morales, N; Henriquez, C; Vidal, L; Folch, H; Galecio, J S; Morán, G

    2013-12-01

    A reduction in inflammatory cell apoptosis is an important concept in the maintenance of inflammation and a potential target for the resolution of inflammation in many inflammatory diseases. Dysregulation of apoptosis has been implicated in a range of diseases, including tumors, neurodegenerative disorders and autoimmunity, and may also be implicated in allergic asthma. In horses, recurrent airway obstruction (RAO) is an asthma-like condition that is characterized increased survival neutrophil bronchial. Tamoxifen is a synthetic, non-steroidal, anti-estrogen agent that is widely used for treating all stages of breast cancer and has been approved for the prevention of breast cancer in high-risk women. The observed efficacy of tamoxifen has been attributed to both growth arrest and the induction of apoptosis. Therefore, the aim of our study was to evaluate the ability of tamoxifen to induce apoptosis in vitro in granulocytic cells from peripheral blood and in mononuclear cells from bronchoalveolar lavage fluid (BALF) in horses. Flow cytometry using commercial AnnexinV-FITC and propidium iodide was used to quantify early and late apoptotic leukocytes, respectively. The results showed a significant increase in early apoptosis in peripheral blood and bronchial granulocytic cells treated with tamoxifen. The rate of early apoptosis of mononuclear cells from blood and BALF when incubated with tamoxifen was significantly lower compared with granulocytic cells. We did not observe a direct effect of tamoxifen on late apoptosis in any of the in vitro assays in the cell types used here. These results indicate that the apoptotic mechanisms under these experimental conditions would affect only blood and BALF granulocytic cells, particularly in early apoptosis. Finally, further in vitro and in vivo studies are needed to better understand apoptotic mechanisms because tamoxifen could be used to treat chronic, inflammatory pathologies associated with granulocytes and allergic diseases, such as asthma or equine RAO. PMID:23846832

  9. Effects of Nanpao, a kampo medicine, on peripheral blood flow and surface skin temperature in aged female rats.

    Science.gov (United States)

    Ichihashi, Masaru; Takatani, Hiromi; Hashimoto, Yoshikatsu; Yano, Kouji; Nishida, Atsuyuki; Kitamura, Kazuyuki

    2009-01-01

    The effects of long-term treatment with Nanpao, a kampo medicine, on cold constitution were evaluated in aged female rats. Five-month-old rats were administered Nanpao orally at doses of 0, 30, or 100 mg/kg/day. The peripheral blood flow and surface skin temperature in the hind paws were measured using a laser Doppler blood flow meter and infrared thermography, respectively. In animals treated with Nanpao, the peripheral blood flow increased dose-dependently compared to that in the control group. Moreover, the surface skin temperature after immersion in ice-cold water was higher in the Nanpao-treated groups than in the control group at all measurement times. These results suggest that Nanpao has the potential to improve cold constitution associated with decreased peripheral blood flow in women. PMID:19151515

  10. Psychological contents and social effects associated to peripheral facial paralysis: a speech-language approach

    Directory of Open Access Journals (Sweden)

    Silva, Mabile Francine Ferreira

    2011-10-01

    Full Text Available Introduction: The peripheral facial paralysis (PFP results from the reduction or interruption of the axonal transport to the seventh cranial nerve resulting in complete or partial paralysis of the facial movements. The facial deformity and limitation of movements, besides affecting the aesthetics and functionality, can significantly interfere with interpersonal communication. Objective: Investigate the psychological contents and other social effects associated to PFP in adult subjects, performing a comparative analysis in three groups of subjects with PFP: at flaccid, recovery and sequel phases. Method: Quantitative and qualitative research. 16 adult subjects, from both sexes, aging between 43 and 88 years old, with PFP. Procedure: Open interviews with subjects. The material was recorded in audio and video, literally transcribed, systematized through categorical and statistical analysis. Results: The subjects bearing sequels presented higher statistical significance of psychological contents and social effects associated to PFP. Followed, respectively, by those that were on flaccid and recovery phases. The results suggest that the speech-language therapist, besides performing functional and aesthetical rehabilitation with the subject with PFP, needs to be aware of psychological and social aspects that may be involved, in order to evaluate and seek to reduce the degree of psychological distress and promote the social adjustment of these patients. Conclusion: The biopsychosocial approach to patients with PFP revealed a wide and significant range of subjective contents that warrant new studies that may contribute to the effectiveness of the speech-language clinical method to approach this medical condition.

  11. Seismic analysis of high arch dams considering contraction-peripheral joints coupled effects

    Science.gov (United States)

    Hariri-Ardebili, Mohammad; Mirzabozorg, Hasan; Kianoush, M.

    2013-09-01

    Dam-reservoir interaction is one of the classic coupled problems in which two various environments with different physical characteristics are in contact with each other on interface boundary. Consideration of such interaction is important in design of new dams as well as on safety evaluation of the existing ones. In the present study, the effect of hydrodynamic pressures at various reservoir operational levels on seismic behavior of an arch dam is investigated. Dez ultra-high arch dam in Iran was selected as case study and all contraction and peripheral joints were simulated using node-to-node contact elements which have the ability of opening/closing and tangential movement. In addition, stage construction effects including joint grouting based on available construction reports were considered. The reservoir was assumed to be compressible and the foundation rock was modeled to account for its flexibility. The TABAS earthquake record was used to excite the finite element model of dam-reservoir-foundation system. It was found that dam-reservoir interaction has significant structural effects on the system and generally, operating the considered arch dam at different water levels can highly affects the distribution of the crack prone area under the maximum credible earthquake.

  12. Hypoxic effect of exogenous insulin on normal and diabetic peripheral nerve.

    Science.gov (United States)

    Kihara, M; Zollman, P J; Smithson, I L; Lagerlund, T D; Low, P A

    1994-06-01

    Insulin administration can cause or worsen experimental and human diabetic neuropathy ("insulin neuritis"). In this study, we tested the hypothesis that insulin administration impairs tissue oxygenation. We infused insulin under nonhypoglycemic conditions and evaluated its effect on endoneurial oxygen tension, nerve blood flow, and the oxyhemoglobin dissociation curve of peripheral nerve in normal and diabetic rats. Intravenous insulin infusion resulted in a dose-dependent reduction in endoneurial oxygen tension in normal nerves (from 26% at 0.04 U/kg insulin to 55% at 32 U/kg). The nerves of rats with streptozotocin-induced diabetes were resistant, but with control of hyperglycemia this susceptibility to the endoneurial hypoxic effect of insulin returned. The reduction in endoneurial oxygen tension regressed with glycosylated hemoglobin (Y = 53.8-2.7X, where Y = %reduction in endoneurial oxygen tension and X = HbA1; r = 0.87; P = < 0.001). Diabetes or insulin administration resulted in only minimal and physiologically insignificant alterations in the oxygen dissociation curve and 2,3-diphosphoglycerate of sciatic nerve. Instead, insulin administration resulted in a reduction in nerve nutritive blood flow and an increase in arteriovenous shunt flow. When the latter was eliminated by the closure of arteriovenous shunts (infusion of 5-hydroxytryptamine), endoneurial oxygen reverted to normal. These findings indicate a deleterious vasoactive effect of insulin and may explain the development of insulin neuritis. PMID:8023930

  13. Effect of Trichostatin A on CD4 surface density in peripheral blood T cells.

    Directory of Open Access Journals (Sweden)

    Anna Koz?owska

    2007-01-01

    Full Text Available Acetylation level of chromatin histones is maintained by histone acetylases (HATs and deacetylases (HDACs and correlates with transcriptional activity of genes. Trichostatin A (TSA is HDAC inhibitor that causes various effects in cells, including immunomodulation. The CD4 antigen is a key coreceptor involved in activation of T helper cells. Using quantitative real-time PCR (RQ-PCR and flow cytometry techniques, we estimated CD4 transcript level and density of CD4 antigen on the surface of TSA-treated stimulated and unstimulated peripheral T cells. We observed a dose dependent decrease in CD4 mRNA level and antigen density on surface of TSA-treated stimulated T cells. However, we did not observe any significant TSA effect on CD4 mRNA and protein expression in unstimulated T cells. Our data suggest that TSA may induce biosynthesis of factors responsible for negative regulation of CD4 antigen expression in stimulated T cells. Our investigation may support previous observation that this drug has immunosuppresive effect on primary T cells and may be useful in treatment of certain autoimmune disorders.

  14. Efeitos cardiovasculares e analgésicos da administração epidural de ropivacaína isolada ou associada à morfina, em felinos / Cardiovascular and analgesic effects of epidural administration of ropivacaine alone or in combination with morphine in cats

    Scientific Electronic Library Online (English)

    Doughlas, Regalin; Marina, Moresco; Vanessa Sasso, Padilha; Ronise, Tocheto; Nilson, Oleskovicz.

    2228-22-01

    Full Text Available SciELO Brazil | Language: Portuguese Abstract in portuguese Visando avaliar os efeitos cardiovasculares e analgésicos de dois protocolos epidurais em felinos submetidos à OSH, 16 gatas mestiças, adultas, que, após indução à anestesia geral, receberam anestesia epidural (L7 - S1) com 0,26mL kg-1 de ropivacaína 0,75%, isolada (GR) ou associada a 0,1mg kg-1 mor [...] fina (GRM). A ETCO2, f, FC, PAS, T°R e relaxamento muscular foram avaliados no momento basal, 30 minutos após epidural, após incisão de pele, ligadura dos pedículos ovarianos e cérvix, final da celiorrafia e cirurgia, sendo administrado fentanil, caso ocorresse aumento de 20% na PAS, FC ou f em relação ao momento basal. Ao final do procedimento, foram avaliados, com auxílio de uma escala multidimensional de dor aguda em felinos, durante 12 horas, e, quando a pontuação fosse ?8, era realizado resgate analgésico com morfina 0,2mg kg-1. Não ocorreram diferenças entre ETCO2, f, T°C e relaxamento muscular. A PAS aumentou em ambos os grupos durante o pinçamento dos pedículos ovarianos e cérvix, quando 100% dos animais do GR e 87,5% do GRM necessitaram fentanil transoperatório. Em 100% dos animais do GR, houve necessidade de morfina pós-operatória às 2 e 4 horas de avaliação, comparados com 50% e 37,5% no GRM. Nos momentos seguintes aos resgates, o somatório de pontos foi semelhante entre grupos. Conclui-se que a administração epidural de ropivacaína associada à morfina em gatas submetidas à ovariosalpingohisterectomia reduz o requerimento analgésico pós-operatório em até 56,2%, durante as primeiras 4 horas, e promove analgesia adequada durante 12 horas, quando comparado à ropivacaína isolada Abstract in english Seeking to evaluate the cardiovascular and analgesic effects of two epidural protocols in cats undergoing OH, 16 female adult mixed-breed cats were induced to general anesthesia, and then epidural was achieved with 0,26mL kg-1 of isolated ropivacaine (GR) (0,75%) or associated with 0,1mg kg-1 morphi [...] ne (GRM). ETCO2, RR, HR, SAP, T° and muscular relaxation were evaluated in baseline, 30 minutes after epidural; after skin incision, ovarian pedicles and uterine cervix ligation; end of laparohraphy; and end of surgery. They received fentanyl if SAP, HR or f, rise in 20% of baseline. At the end of OH, a multidimensional pain scale for cats was used during 12 hours, and rescued with morphine 0,2mg kg-1, when the scale score was ?8 points. There were no differences in ETCO2, RR, T°C and muscular relaxation. SAP increased in both groups during the ovarian pedicle and cervix clamping. In 100% of the animals in GR and 87.5% of the GRM, it was necessary fentanyl during surgery. In 100% of GR animals was required analgesic rescue with morphine at 2 and 4 hours of postoperative evaluation, compared with 50% and 37,5% in GRM, where after the analgesic rescue, in the next hours, the sum of points was similar between groups. It was concluded that epidural administration of morphine and ropivacaine in cats submitted to OH, reduces post operatory analgesic requirements to 56,2% during the first four hours, and promote adequate analgesia for 12 hours in cats submitted to OH, when compared to ropivacaine alone

  15. Non-analgesic effects of opioids : the cognitive effects of opioids in chronic pain of malignant and non-malignant origin. An update

    DEFF Research Database (Denmark)

    HØjsted, Jette; Kurita, Geana Paula

    2012-01-01

    Opioids constitute the basis for pharmacological treatment of moderate to severe pain in cancer pain and non-cancer pain patients. Their action is mediated by the activation of opioid receptors, which integrates the pain modulation system with other effects in the central nervous system including cognition resulting in complex interactions between pain, opioids and cognition. The literature on this complexity is sparse and information regarding the cognitive effects of opioids in chronic pain patients is substantially lacking. Two previous systematic reviews on cancer pain and non-cancer pain patients only using controlled studies were updated. Fourteen controlled studies on the cognitive effects of opioids in chronic non-cancer pain patients and eleven controlled studies in cancer pain patients were included and analyzed. Opioid treatment involved slightly opposite outcomes in the two patient groups: no effects or worsening of cognitive function in cancer pain patients and no effect or improvements in the chronic non-cancer pain patients, however, due to methodological limitations and a huge variety of designs definite conclusions are difficult to draw from the studies. In studies of higher quality of evidence opioid induced deficits in cognitive functioning were associated with dose increase and the use of supplemental doses of opioids in cancer patients. Future perspectives should comprise the conduction of high quality randomized controlled trials (RCTs) involving relevant control groups and validated neuropsychological assessments tools before and after opioid treatment in order to further explore the complex interaction between pain, opioids and cognition.

  16. Human experimental pain models for assessing the therapeutic efficacy of analgesic drugs

    DEFF Research Database (Denmark)

    Olesen, Anne Estrup; Andresen, Trine

    2012-01-01

    Pain models in animals have shown low predictivity for analgesic efficacy in humans, and clinical studies are often very confounded, blurring the evaluation. Human experimental pain models may therefore help to evaluate mechanisms and effect of analgesics and bridge findings from basic studies to the clinic. The present review outlines the concept and limitations of human experimental pain models and addresses analgesic efficacy in healthy volunteers and patients. Experimental models to evoke pain and hyperalgesia are available for most tissues. In healthy volunteers, the effect of acetaminophen is difficult to detect unless neurophysiological methods are used, whereas the effect of nonsteroidal anti-inflammatory drugs could be detected in most models. Anticonvulsants and antidepressants are sensitive in several models, particularly in models inducing hyperalgesia. For opioids, tonic pain with high intensity is attenuated more than short-lasting pain and nonpainful sensations. Fewer studies were performed in patients. In general, the sensitivity to analgesics is better in patients than in healthy volunteers, but the lower number of studies may bias the results. Experimental models have variable reliability, and validity shall be interpreted with caution. Models including deep, tonic pain and hyperalgesia are better to predict the effects of analgesics. Assessment with neurophysiologic methods and imaging is valuable as a supplement to psychophysical methods and can increase sensitivity. The models need to be designed with careful consideration of pharmacological mechanisms and pharmacokinetics of analgesics. Knowledge obtained from this review can help design experimental pain studies for new compounds entering phase I and II clinical trials.

  17. Preclinical Evaluation of the Abuse Potential of the Analgesic Bicifadine

    OpenAIRE

    Nicholson, Katherine L.; Balster, Robert L.; Golembiowska, Krystyna; Kowalska, Magdalena; Tizzano, Joseph P.; Skolnick, Phil; Basile, Anthony S.

    2009-01-01

    The abuse liability of the analgesic bicifadine was investigated in animal models used to predict the abuse potential of psychostimulants in humans. Bicifadine, cocaine, d-amphetamine, bupropion, and desipramine were evaluated for the production of cocaine-like discriminative stimulus effects in rats. Cocaine, d-amphetamine, and bupropion dose-dependently and fully substituted for cocaine. Bicifadine and desipramine produced a maximum mean cocaine-lever selection of 80 and 69%, respectively, ...

  18. Novel analgesic interventions in cancer-induced bone pain

    OpenAIRE

    Currie, Gillian Laura

    2012-01-01

    Cancer-induced bone pain (CIBP), due to bony metastases, is a major clinical problem, significantly reducing quality of life in cancer patients. Current therapies often provide inadequate analgesia or unacceptable side effects. The aim of this thesis was to characterise behaviours of a preclinical model of CIBP and test novel analgesic interventions in this model. A secondary aim was to investigate the involvement of the N-methyl-D-Aspartate (NMDA) receptors and TRP channels ...

  19. Single dose oral analgesics for acute postoperative pain in adults.

    OpenAIRE

    Moore, Ra; Derry, S.; Mcquay, Hj; Wiffen, Pj

    2011-01-01

    BACKGROUND: Thirty-five Cochrane Reviews of randomised trials testing the analgesic efficacy of individual drug interventions in acute postoperative pain have been published. This overview brings together the results of all those reviews and assesses the reliability of available data. OBJECTIVES: To summarise data from all Cochrane Reviews that have assessed the effects of pharmaceutical interventions for acute pain in adults with at least moderate pain following surgery, who have been given ...

  20. ANALGESIC, ANTIPYRETIC AND ANTI-INFLAMMATORY STUDIES ON METHANOLIC EXTRACT OF JASMINUM TRICHOTOMUM LEAVES

    OpenAIRE

    Vijayakumar Mannangatti; Venkata Naresh babu Achuta; Sidharath Panda; Eatakota Usha rani; Pakalapati Prasanthi

    2011-01-01

    The present study was planned to evaluate the analgesic, antipyretic and anti-inflammatory activities of methanolic extract of Jasminum trichotomum leaves in albino rats following oral administration. The results showed that the methanolic extract significantly reduce the acetic acid induce writhing in analgesic model. Its effects on antipyretic activity were also appreciable it significantly reduces fever at higher doses within 2 hrs on yeast induce hyperthermia in rats. Edema induced by car...

  1. Personalized Medicine and Opioid Analgesic Prescribing for Chronic Pain: Opportunities and Challenges

    OpenAIRE

    Bruehl, Stephen; Apkarian, A. Vania; Ballantyne, Jane C.; Berger, Ann; Borsook, David; Chen, Wen G.; Farrar, John T.; Haythornthwaite, Jennifer A.; Horn, Susan D.; Iadarola, Michael J.; Inturrisi, Charles E.; Lao, Lixing; Mackey, Sean; Mao, Jianren; Sawczuk, Andrea

    2013-01-01

    Use of opioid analgesics for pain management has increased dramatically over the past decade, with corresponding increases in negative sequelae including overdose and death. There is currently no well-validated objective means of accurately identifying patients likely to experience good analgesia with low side effects and abuse risk prior to initiating opioid therapy. This paper discusses the concept of data-based personalized prescribing of opioid analgesics as a means to achieve this goal. ...

  2. Comparative analgesic efficacy of buprenorphine or clonidine with bupivacaine in the caesarean section

    OpenAIRE

    Agarwal, Kiran; Agarwal, Navneet; Agrawal, Vijender; Agarwal, Ashok; Sharma, Mahender; Agarwal, Kanupriya

    2010-01-01

    The need for early ambulation for caring of the neonate by mothers makes postoperative pain management after cesarean delivery unique. Favorable results have been observed with buprenorphine, clonidine and bupivacaine as epidural analgesics. This prospective, randomised triple blind control study was carried out among 112 lower segment caesarean segment (LSCS) patients, divided into three groups, to assess the analgesic efficacy and side effects of epidural analgesia, with an intermittent top...

  3. Analgesic and Anti-Inflammatory Activities of the Methanol Extract from Pogostemon cablin

    OpenAIRE

    Yung-jia Chiu; Chia-Yu Liu; Tai-Hung Huang; Ying-Chih Lin; Jung-Chun Liao; Tsung-Chun Lu; Wen-Huang Peng

    2011-01-01

    Pogostemon cablin (PC) is a herbal medicine traditionally applied to treat not only common cold, nausea and diarrhea but also headache and fever. The aim of this study was to investigate the analgesic and anti-inflammatory properties of standardized PC methanol extract (PCMeOH) in vivo. Investigations were performed in mice with two analgesic models. One was acetic acid-induced writhing response and the other formalin-induced paw licking. The anti-inflammatory effect was tested by ?-carragee...

  4. Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics

    OpenAIRE

    Goldberg, Joel S.

    2011-01-01

    Low molecular weight opioid peptide esters (OPE) could become a class of analgesics with different side effect profiles than current opiates. OPE may have sufficient plasma stability to cross the blood brain barrier (BBB), undergo ester hydrolysis and produce analgesia. OPE of dipeptides, tyr-pro and tyr-gly conjugated to ethanol have a structure similar to the anesthestic agent, etomidate. Based upon the analgesic activity of dipeptide opioids, Lipinski’s criteria, and permeability of sele...

  5. Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to NO/cGMP and ATP-sensitive K(+) channels pathway activation in mice.

    Science.gov (United States)

    de Carvalho Veloso, Clarice; Rodrigues, Vanessa Gregório; Ferreira, Renata Cristina Mendes; Duarte, Lucienir Pains; Klein, Andre; Duarte, Igor Dimitri; Romero, Thiago Roberto Lima; de Castro Perez, Andrea

    2015-05-15

    Substances derived from plants play an important role in the development of new analgesic drugs, among them, triterpenoids. The connection between the participation of L-arginine/NO/cGMP pathway and the activation of ATP-sensitive K(+) channels (KATP) has been established on the peripheral antinociception induced by various drugs. The study assessed the involvement of L-arginine/NO/cGMP/KATP pathway in the antinociceptive effect induced by tingenone, from Maytenus imbricata, against the hyperalgesia evoked by prostaglandin E2 (PGE2) in peripheral pathway. The paw pressure test was used, with hyperalgesia induced by intraplantar injection of PGE2 (2?g). Tingenone (200µg/paw) administered into the right hind paw induced a local antinociceptive effect, that was antagonized by l-NOArg, nonselective nitric oxide synthase (NOS) inhibitor and by L-NPA, selective neuronal NOS (nNOS) inhibitor. The L-NIO, selective inhibitor of endothelial (eNOS), and the L-NIL, selective inhibitor of inducible (iNOS), did not alter the peripheral antinociceptive effect of the tingenone. The ODQ, selective soluble guanylyl cyclase inhibitor, prevented the antinociceptive effect of tingenone, and zaprinast, inhibitor of the phosphodiesterase that is cyclic guanosine monophosphate (cGMP) specific, intensified the peripheral antinociceptive effect of the smaller dose of tingenone. Glibenclamide, ATP-sensitive K(+) channels (KATP) blocker, but not tetraethylammonium chloride, voltage-dependent K(+) channel blocker; dequalinium dichloride, blocker of the small conductance Ca(2+)-activated K(+) channel, and paxilline, a potent blocker of high-conductance Ca(2+)-activated K(+) channels, respectively, prevented the peripheral antinociceptive effect of tingenone. The results demonstrate that tingenone induced a peripheral antinociceptive effect by L-arginine/NO/cGMP/KATP pathway activation, with potential for a new analgesic drug. PMID:25748602

  6. A Novel Behavioral Fish Model of Nociception for Testing Analgesics

    Directory of Open Access Journals (Sweden)

    E. Don Stevens

    2011-04-01

    Full Text Available Pain is a major symptom in many medical conditions, and often interferes significantly with a person’s quality of life. Although a priority topic in medical research for many years, there are still few analgesic drugs approved for clinical use. One reason is the lack of appropriate animal models that faithfully represent relevant hallmarks associated with human pain. Here we propose zebrafish (Danio rerio as a novel short-term behavioral model of nociception, and analyse its sensitivity and robustness. Firstly, we injected two different doses of acetic acid as the noxious stimulus. We studied individual locomotor responses of fish to a threshold level of nociception using two recording systems: a video tracking system and an electric biosensor (the MOBS system. We showed that an injection dose of 10% acetic acid resulted in a change in behavior that could be used to study nociception. Secondly, we validated our behavioral model by investigating the effect of the analgesic morphine. In time-course studies, first we looked at the dose-response relationship of morphine and then tested whether the effect of morphine could be modulated by naloxone, an opioid antagonist. Our results suggest that a change in behavioral responses of zebrafish to acetic acid is a reasonable model to test analgesics. The response scales with stimulus intensity, is attenuated by morphine, and the analgesic effect of morphine is blocked with naloxone. The change in behavior of zebrafish associated with the noxious stimulus can be monitored with an electric biosensor that measures changes in water impedance.

  7. Anti-inflammatory, Analgesic and Antiulcer properties of Porphyra vietnamensis

    Directory of Open Access Journals (Sweden)

    Saurabh Bhatia

    2014-12-01

    Full Text Available Objectives: Aim of the present work was to investigate the anti-inflammatory, analgesic and antiulcer effects of red seaweed Porphyra vietnamensis (P. vietnamenis. Materials and Methods: Aqueous (POR and alcoholic (PE fractions were successfully isolated from P. vietnamenis. Further biological investigations were performed using a classic test of paw edema induced by carrageenan, writhing induced by acetic acid, hot plate method and naproxen induced gastro-duodenal ulcer. Results: Among the fractions POR showed better activity.  POR and PE significantly (p < 0.05 reduced carrageenan induced paw edema in a dose dependent manner. In the writhing test POR significantly (p < 0.05 reduced abdominal writhes than PE.  In hot plate method POR showed better analgesic activity than PE. POR showed comparable ulcers reducing potential (p

  8. [Effect of stevia on the picture of peripheral blood under exposure to vibration].

    Science.gov (United States)

    Adamyan, Ts I; Gevorkyan, E S

    2014-01-01

    There were investigated changes in the peripheral blood of rabbits under prolonged exposure to vibration (5, 10, 20, 30 days). In a separate series of experiments, the nature of changes in the peripheral blood was investigated under the combined action of vibration and stevia leaves. Contained in stevia biologically active substances were found to accelerate metabolism in bone marrow stem cells, promote the compensatory ability of the organism, thereby providing the resistance of the body to the vibration factor. PMID:25306709

  9. The impact of stress on tumor growth: peripheral CRF mediates tumor-promoting effects of stress

    OpenAIRE

    Stathopoulos Efstathios N; Ripoll Jorge; Rassouli Olga; Dermitzaki Erini; Androulidaki Ariadne; Mol Berber; Venihaki Maria; Arranz Alicia; Gomariz Rosa P; Margioris Andrew N; Tsatsanis Christos

    2010-01-01

    Abstract Introduction Stress has been shown to be a tumor promoting factor. Both clinical and laboratory studies have shown that chronic stress is associated with tumor growth in several types of cancer. Corticotropin Releasing Factor (CRF) is the major hypothalamic mediator of stress, but is also expressed in peripheral tissues. Earlier studies have shown that peripheral CRF affects breast cancer cell proliferation and motility. The aim of the present study was to assess the significance of ...

  10. Peripheral reactions

    International Nuclear Information System (INIS)

    Peripheral collisions, that is, collisions involving a small amount of overlap of nuclear matter, are discussed including inclusive interactions, the magnitude of the peripheral cross section, fragmentation, a compilation of experiments and available data, limiting fragmentation, factorization, some models, fragment momentum distributions, and future research directions

  11. Cannabinoids and ghrelin have both central and peripheral metabolic and cardiac effects via AMP-activated protein kinase.

    OpenAIRE

    Kola, B.; Hubina, E.; Tucci, Sa; Kirkham, Tc; Garcia, Ea; Mitchell, Se; Williams, Lm; Hawley, Sa; Hardie, Dg; Grossman, Ab; Korbonits, M.

    2005-01-01

    Endocannabinoids and ghrelin are potent appetite stimulators and are known to interact at a hypothalamic level. However, both also have important peripheral actions, including beneficial effects on the ischemic heart and increasing adipose tissue deposition, while ghrelin has direct effects on carbohydrate metabolism. The AMP-activated protein kinase (AMPK) is a heterotrimeric enzyme that functions as a fuel sensor to regulate energy balance at both cellular and whole body levels, and it may ...

  12. Peripheral nerve stimulation for treatment of postherpetic neuralgia: A Case report

    Directory of Open Access Journals (Sweden)

    Scott C. Palmer

    2011-11-01

    Full Text Available Neuromodulation techniques have been successfully used for a varietyof neuropathic pain conditions. Th e aim of this paper is to presenta case of the successful use of a subcutaneously placed peripheralnerve stimulator for treatment of intractable postherpetic neuralgia(PHN. A 57-year old man presented with a two-year history of leftthoracic pain that developed aft er a vesicular rash. Focal neuropathic pain had not responded to treatment with multiple analgesic medications and steroid injections. Th e patient had significant relief following implantation of a peripheral nerve stimulator. Th is case represents a contribution to the small but growing body of evidence indicating that peripheral nerve stimulation may be an effective option for treatment of PHN not responsive to less invasive modalities.

  13. Analgesic and anti-inflammatory activities of Polygonum stagninum.

    Science.gov (United States)

    Mazid, M Abdul; Datta, Bidyut K; Bachar, Sitesh C; Bashar, S A M Khairul; Nahar, Lutfun; Sarker, Satyajit D

    2010-07-01

    The n-hexane, ethyl acetate (EtOAc), and methanol extracts of the aerial parts of Polygonum stagninum Buch.-Ham. ex Meissn. (Polygonaceae), a Bangladeshi medicinal plant, were assessed for analgesic and anti-inflammatory properties in experimental mice and/or rat models. In the acetic-acid-induced writhing test in mice, all extracts displayed a dose dependent analgesic effect. The most potent analgesic activity was observed with the EtOAc extract at the dose of 400 mg/kg body weight, with an inhibition of writhing response of 50.3% compared to 62.2% for the positive control aminopyrine. Among the extracts, n-hexane extract at the doses of 200 and 400 mg/kg body weight showed the highest levels of anti-inflammatory activity after 2 h, with the inhibition of paw edema of 60.1% and 64.1%, respectively, and this effect was much better than that of the conventional anti-inflammatory agent phenylbutazone (maximum inhibition of 38.3% after 4 h). PMID:20645775

  14. Occlusive Peripheral Arterial Disease

    Science.gov (United States)

    ... Disease Peripheral Arterial Disease Aneurysms and Aortic Dissection Venous Disorders Lymphatic Disorders Topics in Peripheral Arterial Disease Overview of Peripheral Arterial Disease Occlusive Peripheral Arterial ...

  15. Effects of defibrotide on physical performance and hemorheologic picture in patients with peripheral arteriopathy.

    Science.gov (United States)

    Marrapodi, E; Leanza, D; Giordano, S; Nazzari, M; Corsi, C

    1994-04-01

    In a random double-blind study versus placebo, 60 ambulatory patients with peripheral occlusive disease of the lower limbs and claudicatio intermittens (Leriche's stage 2), were treated for 60 days with defibrotide (400 mg b.i.d., oral, n = 30) or placebo (n = 30). Patients in the defibrotide group received additional treatment with the same drug at the reduced rate of 400 mg once daily for another 120 days for maintenance (total treatment duration 180 days). All patients were assessed at intake and 60 days for relative and absolute walking distance (RWD and AWD) in a standard treadmill test and for the Winsor Index (WI) at rest and after exercise; patients of the defibrotide treatment group were retested in the same way at 90-180 days. In a subgroup of patients (defibrotide = 11, placebo = 12), blood samples were obtained for the assessment of whole blood and plasma viscosity at intake and after 60 days of treatment. These samples could not be collected properly in the remaining cases, for technical reasons. At day 60, we compared the effects of the two treatments on physical performance: mean (SE) values of RWD were for defibrotide 148 (9.7) and 179 (12.4) m in basal and post-treatment conditions, respectively, and 209 (16.2) and 212 (17.1) m for placebo. Similar changes were observed for AWD: for defibrotide 206 (13.4) and 241 (15.2) m and for placebo 270 (22.9) and 272 (23.1) m. The mean changes were significantly larger with defibrotide: for RWD + 33 (7.1) vs. + 0.3 (3.8) m (p < 0.01) and for AWD + 34 (9.2) and -2 (6.6) m (p < 0.01). The overall gain of walking distance after maintenance therapy with the reduced defibrotide dosage amounted to approximately + 50% over basal (after 180 days). Blood and plasma viscosity improved in patients on defibrotide but the change fell short of statistical significance versus placebo. All findings confirm the potential usefulness of defibrotide in the treatment of peripheral arterial disease, at the same time encouraging further studies of the involved mechanisms of action. PMID:10150182

  16. Selective effects of MAO inhibition on peripheral benzodiazepine receptor binding in the mouse.

    Science.gov (United States)

    Park, C H; Lukacs, L G; Mastropaolo, J; Deutsch, S I

    1997-01-01

    Monoamine Oxidase (MAO) and the peripheral benzodiazepine binding site (PBR) share a close physical proximity to each other in the outer mitochondrial membrane. Furthermore, MAO activity and the density of PBR sites are affected by stress; benzodiazepines may influence stress-induced changes in MAO activity. In view of the close physical association between MAO and the PBR, we examined the effects of chronic administration of selective and nonselective MAO inhibitors to mice on the specific binding of 3H-Ro5-4864 and 3H-PK-11195 to crude membranes prepared from kidney, heart and liver. Chronic MAO inhibition was associated with alterations in PBR binding in all three tissues; however, in heart and liver changes were not detectable with 3H-PK-11195. Perhaps, the ability to discern changes with 3H-Ro5-4864 that are not detectable with 3H-PK-11195 reflects a functional change in the "activity" of the PBR site in heart and liver that is elicited by chronic MAO inhibition and mediated by a change in the "conformation" of the protein that is detected with 3H-Ro5-4864. Importantly, iproniazid, the nonselective MAO inhibitor, caused changes in PBR binding in all three of the tissues. PMID:9409087

  17. Biological radiation dose estimation by chromosomal aberrations analysis in human peripheral blood (dose-effect curve)

    International Nuclear Information System (INIS)

    In order to draw a dose-effect curve, experimentally gamma ray induced chromosomal aberrations in human peripheral lymphocytes from eight healthy people were studied. Samples from 4 males and 4 females were irradiated in tubes with 0.15, 0.25, 0.5, 1, 1.5, 2, 2.5 gray of gamma ray (Co60 at dose rate 0.3 Gy/min). Irradiated and control samples were incubated in 37 centigrade for 48 hours cell cultures. Cell cultures then were stopped and metaphases spread, Giemsa stained to score the induced chromosomal aberrations. Chromosomal aberrations from 67888 metaphases were scored. Curves from the total number of dicentrics, dicentrics + rings and total numbers of breaks in cell for each individual or for all people were drawn. An increase of all chromosomal aberrations types with the elevation of the doses was observed. The yield of chromosome aberrations is related to the dose used. These curves give a quick useful estimation of the accidentally radiation exposure. (author)

  18. Peripheral blood RNA expression profiling in illicit methcathinone users reveals effect on immune system.

    Science.gov (United States)

    Sikk, Katrin; Kõks, Sulev; Soomets, Ursel; Schalkwyk, Leonard C; Fernandes, Cathy; Haldre, Sulev; Aquilonius, Sten-Magnus; Taba, Pille

    2011-01-01

    Methcathinone (ephedrone) is relatively easily accessible for abuse. Its users develop an extrapyramidal syndrome and it is not known if this is caused by methcathinone itself, by side-ingredients (manganese), or both. In the present study we aimed to clarify molecular mechanisms underlying this condition. We used microarrays to analyze whole-genome gene expression patterns of peripheral blood from 20 methcathinone users and 20 matched controls. Gene expression profile data were analyzed by Bayesian modeling and functional annotation. Of 28,869 genes on the microarrays, 326 showed statistically significant differential expression with FDR adjusted p-values below 0.05. Quantitative real-time PCR confirmed differential expression for the most of the genes selected for validation. Functional annotation and network analysis indicated activation of a gene network that included immunological disease, cellular movement, and cardiovascular disease functions (enrichment score 42). As HIV and HCV infections were confounding factors, we performed additional stratification of subjects. A similar functional activation of the "immunological disease" category was evident when we compared subjects according to injection status (past versus current users, balanced for HIV and HCV infection). However, this difference was not large therefore the major effect was related to the HIV status of the subjects. Mn-methcathinone abusers have blood RNA expression patterns that mostly reflect their HIV and HCV infections. PMID:22303338

  19. Effect of polyoxidonium on the phagocytic activity of human peripheral blood leukocytes.

    Science.gov (United States)

    Dambaeva, Svetlana V; Mazurov, Dmitry V; Golubeva, Nina M; D'yakonova, Vera A; Pinegin, Boris V; Khaitov, Rakhim M

    2003-04-01

    The effect of polyoxidonium on the functional activity of human peripheral blood phagocytes was studied in vitro. Polyoxidonium is an N-oxidized polyethylene-piperazine derivative, a water-soluble high-molecular synthetic immunomodulator. It was established that a one-hour incubation of leukocytes with polyoxidonium increases the ability of leukocytes to kill the ingested Staphylococcus aureus in a dose-dependent manner. This increase was observed in leukocytes obtained from healthy individuals and from patients with chronic granulomatous disease. The study of phagocyte spontaneous and stimulated chemiluminescence showed a significant decrease in the quantity of chemiluminescent impulses in the extracellular space in the presence of polyoxidonium both in luminol- and lucigenin-dependent chemiluminescence assays. Polyoxidonium proved to have an antioxidant activity at all doses tested (100, 250, and 500 &mgr;g/ml). Evaluation of the intracellular hydrogen peroxide (H(2)O(2)) level with a fluorescent indicator dichlorofluorescein showed that incubation with polyoxidonium leads to a higher luminescence intensity of dichlorofluorescein, thus indicating an increase in the intracellular H(2)O(2) level. This increase was not as substantial as in the case of stimulation with phorbol myristate acetate. When polyoxidonium was used at a dose of 500 &mgr;g/ml, the difference with the control was significant for neutrophils and monocytes. Polyoxidonium can be used as adjuvant in combined treatment of acute and chronic infections of any etiology, and in the treatment of chronic granulomatous disease and secondary immunodeficiences along with etiotropic drugs. PMID:12717555

  20. A novel SOD1-ALS mutation separates central and peripheral effects of mutant SOD1 toxicity

    Science.gov (United States)

    Joyce, Peter I.; Mcgoldrick, Philip; Saccon, Rachele A.; Weber, William; Fratta, Pietro; West, Steven J.; Zhu, Ning; Carter, Sarah; Phatak, Vinaya; Stewart, Michelle; Simon, Michelle; Kumar, Saumya; Heise, Ines; Bros-Facer, Virginie; Dick, James; Corrochano, Silvia; Stanford, Macdonnell J.; Luong, Tu Vinh; Nolan, Patrick M.; Meyer, Timothy; Brandner, Sebastian; Bennett, David L.H.; Ozdinler, P. Hande; Greensmith, Linda; Fisher, Elizabeth M.C.; Acevedo-Arozena, Abraham

    2015-01-01

    Transgenic mouse models expressing mutant superoxide dismutase 1 (SOD1) have been critical in furthering our understanding of amyotrophic lateral sclerosis (ALS). However, such models generally overexpress the mutant protein, which may give rise to phenotypes not directly relevant to the disorder. Here, we have analysed a novel mouse model that has a point mutation in the endogenous mouse Sod1 gene; this mutation is identical to a pathological change in human familial ALS (fALS) which results in a D83G change in SOD1 protein. Homozgous Sod1D83G/D83G mice develop progressive degeneration of lower (LMN) and upper motor neurons, likely due to the same unknown toxic gain of function as occurs in human fALS cases, but intriguingly LMN cell death appears to stop in early adulthood and the mice do not become paralyzed. The D83 residue coordinates zinc binding, and the D83G mutation results in loss of dismutase activity and SOD1 protein instability. As a result, Sod1D83G/D83G mice also phenocopy the distal axonopathy and hepatocellular carcinoma found in Sod1 null mice (Sod1?/?). These unique mice allow us to further our understanding of ALS by separating the central motor neuron body degeneration and the peripheral effects from a fALS mutation expressed at endogenous levels. PMID:25468678

  1. A novel SOD1-ALS mutation separates central and peripheral effects of mutant SOD1 toxicity.

    Science.gov (United States)

    Joyce, Peter I; Mcgoldrick, Philip; Saccon, Rachele A; Weber, William; Fratta, Pietro; West, Steven J; Zhu, Ning; Carter, Sarah; Phatak, Vinaya; Stewart, Michelle; Simon, Michelle; Kumar, Saumya; Heise, Ines; Bros-Facer, Virginie; Dick, James; Corrochano, Silvia; Stanford, Macdonnell J; Luong, Tu Vinh; Nolan, Patrick M; Meyer, Timothy; Brandner, Sebastian; Bennett, David L H; Ozdinler, P Hande; Greensmith, Linda; Fisher, Elizabeth M C; Acevedo-Arozena, Abraham

    2015-04-01

    Transgenic mouse models expressing mutant superoxide dismutase 1 (SOD1) have been critical in furthering our understanding of amyotrophic lateral sclerosis (ALS). However, such models generally overexpress the mutant protein, which may give rise to phenotypes not directly relevant to the disorder. Here, we have analysed a novel mouse model that has a point mutation in the endogenous mouse Sod1 gene; this mutation is identical to a pathological change in human familial ALS (fALS) which results in a D83G change in SOD1 protein. Homozgous Sod1(D83G/D83G) mice develop progressive degeneration of lower (LMN) and upper motor neurons, likely due to the same unknown toxic gain of function as occurs in human fALS cases, but intriguingly LMN cell death appears to stop in early adulthood and the mice do not become paralyzed. The D83 residue coordinates zinc binding, and the D83G mutation results in loss of dismutase activity and SOD1 protein instability. As a result, Sod1(D83G/D83G) mice also phenocopy the distal axonopathy and hepatocellular carcinoma found in Sod1 null mice (Sod1(-/-)). These unique mice allow us to further our understanding of ALS by separating the central motor neuron body degeneration and the peripheral effects from a fALS mutation expressed at endogenous levels. PMID:25468678

  2. Potential Analgesic & Anti-Pyretic Herbal drugs: A Comparative Review of Marketed Products

    Directory of Open Access Journals (Sweden)

    Mukesh Kumar Singh

    2011-04-01

    Full Text Available

    Analgesic from the family of the non-steroidal anti-inflammatory drugs (NSAIDs have probably been used for more than 2000 years. In the 1900 ASA become an established treatment for pain and migraine. The detection of the main mechanism of the clinical effect of ASAs in John R.Vane’s group in 1972(who received the Nobel Prize for medicine in 1982 for his discovery of prostaglandin synthesis inhibition gave a new and persistent drive to the development of other chemically different NSAID. The currently available analgesic and antipyretic drugs in allopathic system of medicine are not so effective in combating wide variety of complications. The remedial measure may lie in the ayurvedic system of medicine. The various herbal drugs such as Acacia nilotica, Bauhinia racemosa Linn. Cleome viscose, Hippobromus panciflorus etc known for their potential analgesic and antipyretic activity shall be discussed. The various branded herbal formulations like Rumalaya, Charak, Rumartho, Arthrella, and Reosto etc available in the market as analgesic and antipyretic remedies are also discussed along with their clinical merits. It may be concluded that since ayurvedic formulations contain number of ingredients in which one ingredient may act to enhance the action of other ingredient. Also as a result of so many ingredients present in the particular ayurvedic formulation it helps in combating other diseases in addition to analgesic and antipyretic activity.

    Keywords: Analgesic, Ayurvedic system, Herbal drugs, Antipyretic.

  3. Flow cytometric assay for analysis of cytotoxic effects of potential drugs on human peripheral blood leukocytes

    Science.gov (United States)

    Nieschke, Kathleen; Mittag, Anja; Golab, Karolina; Bocsi, Jozsef; Pierzchalski, Arkadiusz; Kamysz, Wojciech; Tarnok, Attila

    2014-03-01

    Toxicity test of new chemicals belongs to the first steps in the drug screening, using different cultured cell lines. However, primary human cells represent the human organism better than cultured tumor derived cell lines. We developed a very gentle toxicity assay for isolation and incubation of human peripheral blood leukocytes (PBL) and tested it using different bioactive oligopeptides (OP). Effects of different PBL isolation methods (red blood cell lysis; Histopaque isolation among others), different incubation tubes (e.g. FACS tubes), anticoagulants and blood sources on PBL viability were tested using propidium iodide-exclusion as viability measure (incubation time: 60 min, 36°C) and flow cytometry. Toxicity concentration and time-depended effects (10-60 min, 36 °C, 0-100 ?g /ml of OP) on human PBL were analyzed. Erythrocyte lysis by hypotonic shock (dH2O) was the fastest PBL isolation method with highest viability (>85%) compared to NH4Cl-Lysis (49%). Density gradient centrifugation led to neutrophil granulocyte cell loss. Heparin anticoagulation resulted in higher viability than EDTA. Conical 1.5 mL and 2 mL micro-reaction tubes (both polypropylene (PP)) had the highest viability (99% and 97%) compared to other tubes, i.e. three types of 5.0 mL round-bottom tubes PP (opaque-60%), PP (blue-62%), Polystyrene (PS-64%). Viability of PBL did not differ between venous and capillary blood. A gentle reproducible preparation and analytical toxicity-assay for human PBL was developed and evaluated. Using our assay toxicity, time-course, dose-dependence and aggregate formation by OP could be clearly differentiated and quantified. This novel assay enables for rapid and cost effective multiparametric toxicological screening and pharmacological testing on primary human PBL and can be adapted to high-throughput-screening.°z

  4. Cytogenetic effects of low-dose radiation with different LET in human peripheral blood lymphocytes.

    Science.gov (United States)

    Nasonova, E A; Shmakova, N L; Komova, O V; Mel'nikova, L A; Fadeeva, T A; Krasavin, E A; Ritter, S

    2006-11-01

    Chromosome damage and the spectrum of aberrations induced by low doses of gamma-irradiation, X-rays and accelerated carbon ions (195 MeV/u, LET 16.6 keV/microm) in peripheral blood lymphocytes of four donors were studied. G0-lymphocytes were exposed to 1-100 cGy, stimulated by PHA, and analyzed for chromosome aberrations at 48 h post-irradiation by the metaphase method. A complex nonlinear dose-effect dependence was observed over the range of 1 to 50 cGy. At 1-7 cGy, the cells showed the highest radiosensitivity per unit dose (hypersensitivity, HRS), which was mainly due to chromatid-type aberration. According to the classical theory of aberration formation, chromatid-type aberrations should not be induced by irradiation of unstimulated lymphocytes. With increasing dose, the frequency of aberrations decreased significantly, and in some cases it even reached the control level. At above 50 cGy the dose-effect curves became linear. In this dose range, the frequency of chromatid aberrations remained at a low constant level, while the chromosome-type aberrations increased linearly with dose. The high yield of chromatid-type aberrations observed in our experiments at low doses confirms the idea that the molecular mechanisms which underlie the HRS phenotype may differ from the classical mechanisms of radiation-induced aberration formation. The data presented, as well as recent literature data on bystander effects and genetic instability expressed as chromatid-type aberrations on a chromosomal level, are discussed with respect to possible common mechanisms underlying all low-dose phenomena. PMID:17031661

  5. Effects of the L/N-type calcium channel antagonist cilnidipine on morning blood pressure control and peripheral edema formation.

    Science.gov (United States)

    Narita, Sumito; Yoshioka, Yasuko; Ide, Atsumi; Kadokami, Toshiaki; Momii, Hidetoshi; Yoshida, Masayoshi; Ando, Shin-ichi

    2011-01-01

    The L/N-type calcium channel blocker cilnidipine has unique effects including sympathetic nerve suppression and the balanced vasodilatation of arteries and veins that may alleviate morning hypertension (MHT) or peripheral edema caused by calcium channel antagonists. We used ambulatory blood pressure monitoring (ABPM) and a unique peripheral edema measurement to evaluate the effect of morning and bedtime cilnidipine in patients with MHT. Forty-three patients with MHT (60 ± 12 years) were randomly assigned to a morning or bedtime cilnidipine (10-20 mg/day). MHT was defined as a mean systolic blood pressure (SBP) ? 135 mm Hg by ABPM within 2 hours after awaking. After 3 months, greater SBP reductions were observed in the bedtime administration group (versus the morning administration group) at 3:30-6:00 AM (-24 ± 20 mm Hg vs. -10 ± 4 mm Hg; P Cilnidipine had a greater effect on MHT, without causing significant leg edema, when administered at bedtime. PMID:21640687

  6. Effects of long-term, low dose rate fission neutron irradiation on the peripheral hematological cells in rats

    International Nuclear Information System (INIS)

    Objective: To evaluate the effects of long-term, low dose rate fission neutron irradiation on the peripheral hematological cells in rats. Methods: 96 rats were randomly divided into the control group and the irradiation group with low dose rate fission neutron (252Cf, 0.35 mGy/h) irradiation 20.5 h every day. 8 rats of each group were killed at 14 d, 28 d, 42d, 56d, 70d after irradiation and 35d after the irradiation, and their peripheral hematological cells were tested respectively. Results: Compared with the control group, peripheral blood WBC was reduced significantly at the dose of 0.3Gy and 0.4Gy (P < 0.05), and was reduced remarkably at dose of 0.5Gy (P<0.01) and 35d after stopping irradiation(P<0.01). At dose of 0.2Gy, Peripheral blood RBC was abnormally higher comparing with the control group (P<0.01), accompanying with higher HCT and HGB, which suggests condensed blood. At the other point, RBC tend to become lower, but only at dose 0.5Gy, and the difference is significant comparing with control group(P <0.05). At dose of 0.3Gy, 0.4Gy and 0.5Gy, HCT were significantly lower comparing with control group. Comparing with control group, MCV was higher at 35d after stopping irradiation, and PLT was significantly lower in dose of 0.2Gy. Conclusion: Long-term irradiation with low dose rate fission neutron could significantly reduce peripheral blood WBC, with less effects on RBC and PLT. The reduced WBC could not recover at 35d after stopping irradiation. (cover at 35d after stopping irradiation. (authors)

  7. Analgesic effect and side effects of celecoxib and meloxicam in canine hip osteoarthritis / Efectos analgésicos y secundarios de celecoxib y meloxicam en osteoartritis de cadera canina

    Scientific Electronic Library Online (English)

    Víctor, Molina D; David, Álzate V; Jhon, Ruíz B; Manuela, Urrea A; Juan, Tobón J.

    2014-09-01

    Full Text Available SciELO Colombia | Language: English Abstract in spanish Objetivos. Evaluar el efecto farmacológico, clínico y toxicológico de celecoxib y meloxicam utilizados como analgésicos durante 30 días en caninos con osteoartritis de cadera. Materiales y métodos. Fueron evaluados 24 pacientes, 75% hembras, con edad de 7.16 ± 2.06 años, y el 25% machos; con edad de [...] 7.83 ± 2.22 años, todos tenían osteoartritis de cadera, se asignaron aleatoriamente a dos grupos; un grupo recibió celecoxib 5 mg/kg oral cada 12 horas durante 1 mes y el segundo grupo recibió 0.2 mg/kg de meloxicam, oral cada 24 horas durante 1 mes. Todos fueron evaluados por grado de analgesia y pruebas renales, hepáticas y de coagulación al día 0, 10 y 30. Se realizó una endoscopía gástrica al día 30. Para el análisis estadístico se utilizó el test HSD Tukey y c², con nivel significancia del 5%. Resultados. Ambos tratamientos redujeron el dolor articular durante los 30 días, según la escala Melbourne (p?0.05). Las variables hemáticas, renales, hepáticas y de coagulación estuvieron dentro de los valores normales sin diferencia. Todos presentaron gastritis crónica por endoscopia a los 30 días. Conclusiones. Ambos fármacos redujeron el dolor, ninguno tuvo efectos sobre la hematología, función renal, hepática y de coagulación a los 30 días; sin embargo, hubo gastritis crónica a los 30 días. Abstract in english Objective. To evaluate the pharmacological, clinical and toxicological effects of celecoxib and meloxicam for analgesia for 30 days in dogs with hip osteoarthritis. Materials and methods. Twenty-four patients were evaluated, 75% were females with an average age of 7.16 ± 2.06 years and twenty five p [...] ercent were males with an average age of 7.83 ± 2.22 years. All patients had hip osteoarthritis and they were randomized into two groups; one group received oral celecoxib 5 mg/kg every 12 hours during one month and the second group received oral meloxicam 0.2 mg/kg every 24 hours during 1 month. The patients were evaluated for analgesia, and hematological, renal, liver, and coagulation tests on days 0, 10th and 30th after treatment initiation, and a gastric endoscopy on day 30. Statistical analysis was performed using a HSD Tukey test and c² with a 5% level of statistical significance. Results. Both drugs reduced articular pain according to the Melbourne scale during the 30 days of treatment (p?0.05). Hematological, renal, hepatic and coagulation tests were normal in both treatment groups. All patients presented chronic gastritis on endoscopy on day 30th. Conclusions. Both drugs decreased pain at day 30th without causing alterations in hematological, renal, hepatic or coagulation tests after 30 days of treatment. However, both drugs induced chronic gastritis.

  8. Analgesia e ação antiinflamatória da Arnica montana 12CH comparativamente ao cetoprofeno em cães Analgesic and anti-inflammatory effects of Arnica montana 12CH in comparison with ketoprofen in dogs

    Directory of Open Access Journals (Sweden)

    Renata Navarro Cassu

    2011-10-01

    Full Text Available Objetivou-se avaliar os efeitos analgésico e antiinflamatório da Arnica montana 12CH comparativamente ao cetoprofeno em cadelas submetidas à ovariossalpingohisterectomia (OSH. Foram avaliadas 16 cadelas, distribuídas aleatoriamente em dois grupos de oito animais cada, tratados por via oral com 1mg kg-1 de cetoprofeno (TC e com cinco glóbulos de Arnica montana 12CH (TA. Decorridos 60 minutos, os animais foram tranquilizados com acepromazina (0,05mg kg-1, IV, seguindo-se indução e manutenção anestésica com propofol (5mg kg-1, IV e isofluorano, respectivamente. Foram mensurados: frequência cardíaca, frequência respiratória, pressão arterial sistólica, concentração final expirada de dióxido de carbono, concentração final expirada de isofluorano, variáveis hemogasométricas, concentração sérica de cortisol, grau de analgesia e de inflamação. Em casos de analgesia insuficiente, foi realizada suplementação com morfina (0,5mg kg-1, IM. A estatística foi realizada com ANOVA e teste de Tukey (PThis study aimed to evaluate the analgesic and anti-inflammatory effects of Arnica montana 12CH comparatively to ketoprofen in dogs undergoing ovariohysterectomy. Sixteen female dogs were randomly distributed in two groups of eight animals and received 1mg kg-1 of ketoprofen (TC and 5 globules of Arnica montana 12CH (TA by oral route. After 60 minutes, the dogs were sedated with acepromazine (0.05mg kg-1, IV, followed by anesthetic induction with propofol (5mg kg-1 IV and maintained with isoflurane. Heart rate, respiratory rate, systolic blood pressure, arterial blood gases, serum cortisol concentration and degree of analgesia and inflammation were measured. Additional morphine (0.5mg kg-1IM was given when the analgesia was insufficient. Statistical analyses were performed by ANOVA and Tukey tests (P<0.05. Cardiopulmonary stability was observed in both treatments during the surgery. The degree of analgesia and inflammation did not differ between groups. Rescue analgesia was administered to two dogs from each group. It was concluded that Arnica montana 12CH provides similar analgesic and anti-inflammatory effects when compared with ketoprofen, suggesting that this treatment is a safe and effective option to dogs undergoing ovariohysterectomy.

  9. Local Peripheral Effects of ?-Caryophyllene through CB2 Receptors in Neuropathic Pain in Mice

    Directory of Open Access Journals (Sweden)

    Hikari Kuwahata

    2012-10-01

    Full Text Available ?-Caryophyllene (BCP is known as a common constitute of the essential oils of numerous food plants and primary component in Cannabis. In this study, we investigated the effect of local intraplantar (i.pl. injection of BCP on mechanical hypersensitivity induced by partial sciatic nerve ligation (PSNL in mice. Relative to sham operation controls, mice with the PSNL displayed a maximum level of hyperresponsiveness to von Frey metallic filament on post-operative day 7. PSNL-induced allodynia was seen in the ipsilateral side of nerve ligation, but not in the contralateral side. The i.pl. injection of BCP into the ipsilateral hindpaw to PSNL attenuated mechanical allodynia in a dose-dependent manner. BCP injection into the contralateral hindpaw did not produce anti-allodynic effects, suggesting a local peripheral anti-allodynic effect of BCP. Anti-allodynic effects induced by i.pl. injection of BCP were prevented by pretreatment with the cannabinoid (CB2 receptor antagonist AM630, but not by the CB1 receptor antagonist AM251. These data suggest that i.pl. injection of BCP could produce anti-allodynia by activating peripheral CB2 receptors, but not CB1 receptors in a mouse model of neuropathic pain. Taken together, these results suggest that peripheral CB2 receptors may contribute to the effectiveness of BCP in the treatment of neuropathic pain disorders.

  10. Intrauterine exposure to mild analgesics is a risk factor for development of male reproductive disorders in human and rat

    DEFF Research Database (Denmark)

    Kristensen, David MØbjerg; Hass, Ulla

    2011-01-01

    BACKGROUND More than half of pregnant women in the Western world report intake of mild analgesics, and some of these drugs have been associated with anti-androgenic effects in animal experiments. Intrauterine exposure to anti-androgens is suspected to contribute to the recent increase in male reproductive problems, and many of the anti-androgenic compounds are like the mild analgesics potent inhibitors of prostaglandin synthesis. Therefore, it appears imperative to further investigate the potential endocrine disrupting properties of mild analgesics. METHODS In a prospective birth cohort study, 2297 Danish and Finnish pregnant women completed a questionnaire and 491 of the Danish mothers participated in a telephone interview, reporting on their use of mild analgesics during pregnancy. The testicular position of newborns was assessed by trained paediatricians. In rats, the impact of mild analgesics on anogenital distance (AGD) after intrauterine exposure was examined together with the effect on ex vivo gestational day 14.5 testes. RESULTS In the Danish birth cohort, the use of mild analgesics was dose-dependently associated with congenital cryptorchidism. In particular, use during the second trimester increased the risk. This risk was further increased after the simultaneous use of different analgesics. The association was not found in the Finnish birth cohort. Intrauterine exposure of rats to paracetamol led to a reduction in the AGD and mild analgesics accordingly reduced testosterone production in ex vivo fetal rat testes. CONCLUSION There was an association between the timing and the duration of mild analgesic use during pregnancy and the risk of cryptorchidism. These findings were supported by anti-androgenic effects in rat models leading to impaired masculinization. Our results suggest that intrauterine exposure to mild analgesics is a risk factor for development of male reproductive disorders.

  11. Effects of traditional Chinese medicine Tenghuanglin on peripheral T and B lymphocyte subsets in microwave irradiated rats

    Directory of Open Access Journals (Sweden)

    Qiong MA

    2014-03-01

    Full Text Available Objective ?To observe the effect of Tenghuanglin (THL on peripheral T and B lymphocyte subsets in microwave irradiated rats, and explore the protective effect of THL on injury to immunity induced by microwave irradiation and its mechanism. Methods ?Eighty healthy male SD rats were randomly divided into 4 groups (n=20: normal control group (CON, radiation group (RAD, radiation + Anduolin (positive control drug treatment group (ADL, and radiation + THL treatment group (THL. Rats in ADL and THL groups received gavage of the individual drug once a day for 7 days, and then exposed to 30mW/cm2 microwave whole body for 15min. Rats in RAD group received same dose of microwave irradiation, and those in CON group received sham irradiation. The animals were sacrificed on 7th and 14th day after irradiation, and the changes in peripheral blood smear was observed, and CD3+, CD4+ and CD8+ T lymphocyte subsets, and CD45RA+ B lymphocyte subset were determined. Results ?Fourteen days after irradiation, peripheral red blood cells in RAD group was obviously lower than those in CON, ADL and THL groups, and there was no statistically significant difference of red cell count between CON, ADL and THL groups. Seven days after irradiation, peripheral CD3+, CD4+ and CD8+ T cells in RAD group were lower in number than those in CON group, and they did not return to normal level up to 14th day. The peripheral CD3+, CD4+ and CD8+ T cells in THL and ADL groups were obviously higher than those in RAD group, and peripheral CD3+, CD4+ T cells were still higher than those in RAD group 14d after irradiation, while the peripheral CD3+, CD4+ and CD8+ T cells in THL and ADL groups were similar both at 7th and 14th day. Seven days after irradiation, the CD4/CD8 ratio was lower in RAD group than that in CON and THL groups (P<0.05, while the ratio in CON, ADL and THL groups was similar. The CD4/CD8 ratio in 4 groups was similar on 14th day after irradiation. Peripheral CD45RA+ B lymphocytes were lower in number in RAD group than in CON group on 7th and 14th days (P<0.05, while they were higher in ADL group on 7th day and in THL group on 7th and 14th days than in RAD group (P<0.05, but they were similar to CON group. Conclusions ?Peripheral T and B lymphocytes reduce in number, and CD4/CD8 ratio lowers early after the microwave irradiation, resulting in immunosuppression and immune imbalance in rats. Traditional Chinese medicine THL could increase the peripheral T and B lymphocyte counts and improve the CD4/CD8 ratio after microwave irradiation in rats. The present study provides a new basis for the research on drugs for preventing and treating micro-wave irradiation injury. DOI: 10.11855/j.issn.0577-7402.2014.03.13

  12. Effects on the peripheral nervous system of workers' exposure to carbon disulfide

    Energy Technology Data Exchange (ETDEWEB)

    Johnson, B.L.; Boyd, J.; Burg, J.R.; Lee, S.T.; Xintaras, C.; Albright, B.E.

    An evaluation of the effects of occupational exposure to carbon disulfide was performed in a sample of 156 male viscos rayon workers. Effects of CS/sub 2/ on the peripheral nervous system (PNS) were evaluated in ulnar and peroneal nerves using measurements of maximum motor nerve conduction velocity (MCV) and distal latency; and sensory conduction velocity (SCV) in the sural nerve. Self-reported symptoms related to PNS disorders were also obtained from each study participant. Industrial hygiene records showed the rayon workers to have had CS/sub 2/ exposures that generally had not exceeded 20 ppm. The overall mean number of years of CS/sub 2/ exposure was 12.1 years (+/- 6.9 S.D.). The workers were divided prior to the study into three groups according to historical mean CS/sub 2/ levels calculated for job titles and area. Personal CS/sub 2/ samples were obtained during the conduct of the study to characterize each job. For these three groups the median CS/sub 2/ levels were measured to be 1.0, 4.1 and 7.6 ppm. The comparison group's median CS/sub 2/ level approximated 0.2 ppm. Results showed CS/sub 2/-exposed workers to have small but statistically significant (p less than .05) reductions in sural SCV and peroneal MCV. Other neurophysiological measures consisting of distal latency, residual latency, and muscle or nerve action potential amplitudes showed no significant differences between study groups. A reduction in the ratio of amplitudes of muscle action potentials obtained from peroneal nerve stimulation was significant (p less than .05). Reductions in the peroneal nerve MCV were found to be related, in a dose response sense, to workers' cumulative exposure to CS/sub 2/. No increase attributable to CS/sub 2/ was found in the prevalence of symptoms related to PNS disorders.

  13. N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation.

    Science.gov (United States)

    Romero, Thiago Roberto Lima; Duarte, Igor Dimitri Gama

    2012-01-01

    Although the antinociceptive effects of N-palmitoyl-ethanolamine (PEA) were first characterized nearly 50 years ago, the identity of the mechanism that mediates these actions has not been elucidated. The present study investigated the contribution of K(+) channels on peripheral antinociception induced by the CB(2) agonist PEA. Nociceptive thresholds to mechanical paw stimulation of Wistar rats treated with intraplantar prostaglandin E(2) to induce hyperalgesia were measured, and other agents were also given by local injection. PEA (5, 10, and 20 µg/paw) elicited a local peripheral antinociceptive effect. This effect was antagonized by glibenclamide, a selective blocker of ATP-sensitive K(+) channels (20, 40, and 80 µg/paw). In addition, neither the voltage-dependent K(+) channel-specific blocker tetraethylammonium (30 µg/paw) nor the small and large conductance blockers of Ca(2+)-activated K(+) channels, dequalinium (50 µg/paw) and paxilline (20 µg/paw), respectively, were able to block the local antinociceptive effect of PEA. These results indicate that the activation of ATP-sensitive K(+) channels could be the mechanism that induces peripheral antinociception by PEA and that voltage-dependent K(+) channels and small and large conductance Ca(2+)-activated K(+) channels do not appear to be involved in this mechanism. PMID:22343363

  14. Effect of Peripheral Arterial Disease on Serum Ischemia-Modified Albumin Levels in Type 2 Diabetic Patients

    Directory of Open Access Journals (Sweden)

    Tugra Gencpinar

    2014-05-01

    Full Text Available Background: The aim of this study is to evaluate the role of IMA and the effect of Type-2 diabetes in peripheral arterial ischemic patient. Methods: In our study, randomized patient groups to be undergone peripheral surgery, consisting of 16 diabetic and 12 non-diabetic patients diagnosed with peripheral arterial disease, have been examined. After standard anesthesia, the surgery was performed by the same surgical team, blood samples were taken before and after cross-clamp, and the levels of ischemia modified albumin (IMA, which is a new ischemic marker, were studied spectrophotometrically. Demographic data were compared with the type-2 diabetes association. Results: In this study, we found that there were no correlation with the ankle brachial index (ABI and risk factors of diabetes between postoperative IMA levels (P: 0.47. Preoperative IMA serum blood levels were significantly higher in patients with peripheral arterial disease (P: 0.70, and positively associated with ABI (diabetic group P: 0.04, non-diabetic group P: 00. Also, no correlation was found with X clamp times, ABI, and IMA blood levels (P: 0.30. In diabetic group, ischemia marker increase was high and there was a positive correlation between HbA1c levels (P: 0.002. Conclusion: Our study suggested that, preoperative serum IMA levels were positively associated with ABI. In diabetic group, the increase in IMA levels was high and there was positive correlation between HbA1c levels. IMA was a benefit marker for monitoring and early diagnosis of the peripheral arterial disease.

  15. Peripheral Dose Heterogeneity Due to the Thread Effect in Total Marrow Irradiation With Helical Tomotherapy

    Energy Technology Data Exchange (ETDEWEB)

    Takahashi, Yutaka [Masonic Cancer Center, University of Minnesota, Minneapolis, Minnesota (United States); Verneris, Michael R. [Division of Hematology, Oncology, and Bone Marrow Transplantation, Department of Pediatrics, University of Minnesota, Minneapolis, Minnesota (United States); Dusenbery, Kathryn E. [Department of Therapeutic Radiology, University of Minnesota, Minneapolis, Minnesota (United States); Wilke, Christopher T. [Department of Radiotherapy, Universitair Ziekenhuis Brussel, Brussels (Belgium); Storme, Guy; Weisdorf, Daniel J. [Department of Medicine, University of Minnesota, Minneapolis, Minnesota (United States); Hui, Susanta K., E-mail: huixx019@umn.edu [Masonic Cancer Center, University of Minnesota, Minneapolis, Minnesota (United States); Department of Therapeutic Radiology, University of Minnesota, Minneapolis, Minnesota (United States)

    2013-11-15

    Purpose: To report potential dose heterogeneity leading to underdosing at different skeletal sites in total marrow irradiation (TMI) with helical tomotherapy due to the thread effect and provide possible solutions to reduce this effect. Methods and Materials: Nine cases were divided into 2 groups based on patient size, defined as maximum left-to-right arm distance (mLRD): small mLRD (?47 cm) and large mLRD (>47 cm). TMI treatment planning was conducted by varying the pitch and modulation factor while a jaw size (5 cm) was kept fixed. Ripple amplitude, defined as the peak-to-trough dose relative to the average dose due to the thread effect, and the dose–volume histogram (DVH) parameters for 9 cases with various mLRD was analyzed in different skeletal regions at off-axis (eg, bones of the arm or femur), at the central axis (eg, vertebrae), and planning target volume (PTV), defined as the entire skeleton plus 1-cm margin. Results: Average ripple amplitude for a pitch of 0.430, known as one of the magic pitches that reduce thread effect, was 9.2% at 20 cm off-axis. No significant differences in DVH parameters of PTV, vertebrae, or femur were observed between small and large mLRD groups for a pitch of ?0.287. Conversely, in the bones of the arm, average differences in the volume receiving 95% and 107% dose (V95 and V107, respectively) between large and small mLRD groups were 4.2% (P=.016) and 16% (P=.016), respectively. Strong correlations were found between mLRD and ripple amplitude (rs=.965), mLRD and V95 (rs=?.742), and mLRD and V107 (rs=.870) of bones of the arm. Conclusions: Thread effect significantly influences DVH parameters in the bones of the arm for large mLRD patients. By implementing a favorable pitch value and adjusting arm position, peripheral dose heterogeneity could be reduced.

  16. Effects of Blood Transportation on Human Peripheral Mononuclear Cell Yield, Phenotype and Function: Implications for Immune Cell Biobanking

    OpenAIRE

    Posevitz-fejfa?r, Anita; Posevitz, Vilmos; Gross, Catharina C.; Bhatia, Urvashi; Kurth, Frank; Schu?tte, Verena; Bar-or, Amit; Meuth, Sven G.; Wiendl, Heinz

    2014-01-01

    Human biospecimen collection, processing and preservation are rapidly emerging subjects providing essential support to clinical as well as basic researchers. Unlike collection of other biospecimens (e.g. DNA and serum), biobanking of viable immune cells, such as peripheral blood mononuclear cells (PBMC) and/or isolated immune cell subsets is still in its infancy. While certain aspects of processing and freezing conditions have been studied in the past years, little is known about the effect o...

  17. Effect on the gonads and peripheral blood of mice at independent and combined treatment with adaptogens before radiation

    International Nuclear Information System (INIS)

    The independent and combined effect of pharmacopeial preparations such as Torphot, Aloe, placenta extract and eleouterococcus have been investigated. The preparations was introduced prophylactically within 28 days, read according to the weight and cellular quality of the testicles on 28th day following 3 Gy Gamma irradiation. A comparative analysis has been made between the data obtained and the ones received earlier on leucocytes dynamics in the peripheral blood

  18. Effect on the gonads and peripheral blood of mice at independent and combined treatment with adaptogens before radiation

    Energy Technology Data Exchange (ETDEWEB)

    Pantev, T.; Topalova, S. (Meditsinska Akademiya, Sofia (Bulgaria). Nauchen Inst. po Rentgenologiya i Radiobiologiya)

    1984-01-01

    The independent and combined effect of pharmacopeial preparations such as Torphot, Aloe, placenta extract and eleouterococcus have been investigated. The preparations was introduced prophylactically within 28 days, read according to the weight and cellular quality of the testicles on 28th day following 3 Gy gamma irradiation. A comparative analysis has been made between the data obtained and the ones received earlier on leucocytes dynamics in the peripheral blood.

  19. Pancratistatin induces apoptosis in clinical leukemia samples with minimal effect on non-cancerous peripheral blood mononuclear cells

    OpenAIRE

    McNulty James; Hamm Caroline; Griffin Carly; Pandey Siyaram

    2010-01-01

    Abstract Background Pancratistatin, a natural compound extracted from Hymenocallis littoralis, can selectively induce apoptosis in several cancer cell lines. In this ex vivo study, we evaluated the effect of pancratistatin on peripheral blood mononuclear cells obtained from 15 leukemia patients prior to clinical intervention of newly diagnosed patients, as well as others of different ages in relapse and at various disease progression states. Results Mononuclear cells from healthy volunteers a...

  20. Therapeutic Effects of Fenofibrate on Diabetic Peripheral Neuropathy by Improving Endothelial and Neural Survival in db/db Mice

    OpenAIRE

    Cho, Ye Rim; Lim, Ji Hee; Kim, Min Young; Kim, Tae Woo; Hong, Bo Young; Kim, Yong-soo; Chang, Yoon Sik; Kim, Hye Won; Park, Cheol Whee

    2014-01-01

    Neural vascular insufficiency plays an important role in diabetic peripheral neuropathy (DPN). Peroxisome proliferative-activated receptor (PPAR)? has an endothelial protective effect related to activation of PPAR? coactivator (PGC)-1? and vascular endothelial growth factor (VEGF), but its role in DPN is unknown. We investigated whether fenofibrate would improve DPN associated with endothelial survival through AMPK-PGC-1?-eNOS pathway. Fenofibrate was given to db/db mice in combination wi...

  1. Effects of peripheral sympathectomy on thermoregulatory vascular control in the rabbit ear.

    Science.gov (United States)

    Smith, T L; Koman, L A; Gordon, E S; Holden, M B; Smith, B P

    1998-01-01

    A rabbit ear model of the human digit was utilized to determine the vascular response to peripheral sympathectomy. Vascular responses were evaluated by subjecting chronically instrumented rabbits to a cold stress before and after sympathectomy surgery. The typical response to cold stress is for ear temperatures and auricular cutaneous perfusion to decrease during the cooling phase of the test and to increase toward baseline levels during the rewarming phase after cold exposure. Following peripheral sympathectomy, ear temperatures were significantly increased during both the cooling and rewarming phase of the cold stress test although overall ear perfusion and skin perfusion were not different from sham-operated rabbits. The responses observed in the rabbit ear following peripheral sympathectomy appear to mimic those noted in patients receiving digital peripheral sympathectomies for the treatment of refractory pain and ulceration. Peripheral sympathectomy may result in clinical improvements in patients because it improves both total digital and nutritional cutaneous blood flow. Peripheral sympathectomy in normal rabbit ears does not result in altered perfusion patterns with cold exposure although ear temperature is significantly higher. This pattern of changes suggests that the distribution of extremity perfusion is altered even though overall extremity perfusion and cutaneous perfusion per se are not significantly different from sham-operated controls. Complete sympathectomy was accompanied by a persistent increase in ear temperature and a dissociation between conductance and microvascular perfusion. Auricular conductance was transiently increased and then decreased to levels below preoperative control values. Microvascular perfusion is decreased immediately following amputation/replantation and thereafter increases. PMID:9674929

  2. Effects of lithium on peripheral neuropathy induced by vincristine in rats.

    Science.gov (United States)

    Alimoradi, Houman; Pourmohammadi, Nasir; Mehr, Shahram Ejtemaei; Hassanzadeh, Gholamreza; Hadian, Mohammad Reza; Sharifzadeh, Mohammad; Bakhtiarian, Azam; Dehpour, Ahmad Reza

    2012-01-01

    Vincristine (VCR) as a frequently used antimitotic agent which is commonly prescribed for wide spectrum of neoplasm, causes mixed sensorimotor neuropathy. Several evidences show lithium could be a neuroprotective agent, therefore to assess whether a pretreatment and at subtherapeutic dose it could prevent the peripheral neuropathy produced by VCR, rats were treated with VCR 0.1mg/kg i.p. for 3 alternative doses and / or lithium chloride (20mg/kg or 40 mg/kg i.p. daily from the first day to the day of sacrifice). Erythrocyte lithium concentration (ELC) and plasma lithium concentration (PLC) were measured at the seventh day of study and the day of scarification. After seventh day of lithium administration, PLC and ELC reached to a steady state at subtheraputic dose and they did not significantly change at normal housing situation. Hot plate, open field test and nerve conduction velocity were used to evaluate the sensory and motor neuropathy. Only VCR treated rats showed behavioral, electrophysiological and histological evidences of a mixed sensorimotor neuropathy by significant increase in hot plate latencies and a marked decrease in total distance moved and conduction velocities in both sensory and motor nerves. Lithium at the dose of 20mg/kg and specially 40mg/kg robustly reduced the rate of mortality, general toxicity and was able to ameliorate mixed sensorimotor neuropathy induced by VCR. These results suggest that lithium at dose of 20mg/kg and 40 mg/kg, potentially by its effects on cell survival pathways such as inhibition of glycogen synthase kinase-3 (GSK3?), can prevent both motor and sensory components of VCR neuropathy. PMID:22837115

  3. Effect of blood storage conditions on DNA repair capacity measurements in peripheral blood mononuclear cells.

    Science.gov (United States)

    Allione, Alessandra; Porcedda, Paola; Russo, Alessia; Ricceri, Fulvio; Simonelli, Valeria; Minoprio, Anna; Guarrera, Simonetta; Pardini, Barbara; Mazzei, Filomena; Dogliotti, Eugenia; Giachino, Claudia; Matullo, Giuseppe

    2013-09-01

    Due to the great number of genes involved in DNA repair and the interactions among the pathways responsible for the repair of different types of DNA damage, there is an increasing need for simple and reliable approaches to phenotypically assess DNA repair capacity (DRC). The use of peripheral blood mononuclear cells (PBMCs) in DRC assays is particularly useful for human monitoring studies. However, in such studies it is not always possible to collect and process samples on the same day as the blood is taken. We performed a genotype-phenotype correlation study on DRC on 225 healthy subjects. Due to the large number of blood samples to be processed, PBMCs were either isolated and cryopreserved on the same day of blood collection (day 1) or on the following day after 24h blood storage at room temperature (day 2-RT). Samples processed in different days showed a significant difference in the DRC evaluated as 8-oxoguanine glycosylase activity (OGG assay) in cell extracts (pstorage conditions on the outcome of ?-ray induced H2AX phosphorylation assay was reported. These results prompted us to further analyze the effects of blood storage conditions by performing a validation study. Three blood samples were simultaneously taken from ten healthy donors, PBMCs were isolated and cryopreserved as follows: immediately after blood collection (day 1); on the following day, after blood storage at RT (day 2-RT); or after blood storage at 4°C (day 2-4°C). DRC was then evaluated using phenotypic assays. The ?-ray induced H2AX phosphorylation assay has been confirmed as the only assay that showed good reproducibility independently of the blood storage conditions. The measurement of OGG assay was most affected by the blood storage conditions. PMID:23727398

  4. EFECTIVIDAD DE ANESTESIA DE PLEXO CERVICAL SUPERFICIAL PREOPERATORIO PARA CONTROL DE DOLOR POSTOPERATORIO EN CIRUGÍA DE TIROIDES / Analgesic effects of bilateral superficial cervical plexus block with Bupivacaine after thyroidectomy

    Scientific Electronic Library Online (English)

    Nicolás, Ávalos J; Carolina, Cabrera Sch; Irini, Semertzakis P; Silvia, Schmied P.

    2014-12-01

    Full Text Available SciELO Chile | Language: Spanish Abstract in spanish Introducción: La cirugía de la glándula tiroides es reconocida como un procedimiento que produce un dolor leve a moderado. El bloqueo bilateral de plexo cervical superficial es una técnica simple, poco invasiva, que pudiera ser beneficioso en estos pacientes como modelo de analgesia preventiva. Obje [...] tivos: Evaluar la calidad de la analgesia del postoperatorio de la cirugía de tiroides, con el uso de bloqueo bilateral del plexo cervical superficial. Material y Métodos: Se estudiaron pacientes ASA I y II propuestos para cirugía de tiroides bajo anestesia general. En todos los pacientes se hizo anestesia general balanceada con Fentanyl, Propofol, Vecuronio e Isoflurano. En forma aleatoria y ciega se asignaron los pacientes en 2 grupos: grupo A, Bupivacaína 0,25% 20 ml y grupo B placebo. Se evaluó características demográficas, dolor postoperatorio, necesidad de analgésicos de rescate, náuseas, vómitos y satisfacción del paciente. Resultados: 35 pacientes, 7 hombres y 28 mujeres. Con edad promedio de 55,3 ± 14,8 ASA I y 27 ASA II. Quince pacientes en grupo A y 20 pacientes grupo B. Comparables en variables demográficas. El uso promedio de morfina fue de 10,4 mg en grupo B y 5,8 mg en grupo A (p Abstract in english Background: Bilateral superficial cervical plexus block is a simple non-invasive technique that can be used as preventive analgesia in the perioperative period of thyroidectomy. Aim: to assess the analgesic effects of the technique during the postoperative period of thyroidectomy. Material and Metho [...] ds: Patients with indication of total thyroidectomy, with a low operative risk according to the American Society of Anesthesiology, were studied. All were operated with general anesthesia using Fentanyl, Propofol, Vecuronium and Isoflurane. Patients were randomly and blindly assigned to superficial cervical plexus block using Bupivacaine 0.25% or to a placebo injection. Postoperative pain, need for analgesics and patient satisfaction were assessed. Results: Thirty five patients aged 55 + 15 years (28 women) were studied. Mean use of morphine in the Bupivacaine and placebo groups was 5.8 and 10.4 mg, respectively (p

  5. Anti-inflammatory, analgesic, and antipyretic activities of virgin coconut oil.

    Science.gov (United States)

    Intahphuak, S; Khonsung, P; Panthong, A

    2010-02-01

    This study investigated some pharmacological properties of virgin coconut oil (VCO), the natural pure oil from coconut [Cocos nucifera Linn (Palmae)] milk, which was prepared without using chemical or high-heat treatment. The anti-inflammatory, analgesic, and antipyretic effects of VCO were assessed. In acute inflammatory models, VCO showed moderate anti-inflammatory effects on ethyl phenylpropiolate-induced ear edema in rats, and carrageenin- and arachidonic acid-induced paw edema. VCO exhibited an inhibitory effect on chronic inflammation by reducing the transudative weight, granuloma formation, and serum alkaline phosphatase activity. VCO also showed a moderate analgesic effect on the acetic acid-induced writhing response as well as an antipyretic effect in yeast-induced hyperthermia. The results obtained suggest anti-inflammatory, analgesic, and antipyretic properties of VCO. PMID:20645831

  6. Evaluation of the Combined Effects of Gamma Radiation and High Dietary Iron on Peripheral Leukocyte Distribution and Function

    Science.gov (United States)

    Crucian, Brian E.; Morgan, Jennifer L. L.; Quiriarte, Heather A.; Sams, Clarence F.; Smith, Scott M.; Zwart, Sara R.

    2011-01-01

    NASA is concerned with the health risks to astronauts, particularly those risks related to radiation exposure. Both radiation and increased iron stores can independently increase oxidative damage, resulting in protein, lipid and DNA oxidation. Oxidative stress increases the risk of many health problems including cancer, cataracts, and heart disease. This study, a subset of a larger interdisciplinary investigation of the combined effect of iron overload on sensitivity to radiation injury, monitored immune parameters in the peripheral blood of rats subjected to gamma radiation, high dietary iron or both. Specific immune measures consisted of (A) peripheral leukocyte distribution; (B) plasma cytokine levels; (C) cytokine production profiles following whole blood stimulation of either T cells or monocytes.

  7. COMPARATIVE EFFICACY OF GABAPENTIN A CONVENTIONAL ANTICONVULSANT WITH CONVENTIONAL ANALGESIC TREMADOL IN VISCERAL PAIN MODEL OF RODENTS

    Directory of Open Access Journals (Sweden)

    Saurabh Kansal

    2014-09-01

    Full Text Available Carabmazepine is an established drug for trigeminal neuralgia while gabapentin has been tried in postoperative pain but its effectiveness in visceral pain and when compared to conventional analgesics needs to be evaluated.The present study was planned to study the analgesic effects of gabapentin in animal pain model of visceral nociception like writhing test and to compare it with conventional analgesic tremadol. This study has been carried out for evaluation of role of gabapentin in visceral nociception in mice . In the writhing test, a significant reduction in number of writhes have been observed in pretreated groups of mice reflects antinociceptive efficacy of gabapentin in acetic acid induced visceral nociception

  8. fMRI investigation of the effect of local and systemic lidocaine on noxious electrical stimulation-induced activation in spinal cord.

    Science.gov (United States)

    Zhao, Fuqiang; Williams, Mangay; Welsh, Denise C; Meng, Xiangjun; Ritter, Amy; Abbadie, Catherine; Cook, Jacquelynn J; Reicin, Alise S; Hargreaves, Richard; Williams, Donald S

    2009-09-01

    Spinal cord fMRI offers an excellent opportunity to quantify nociception using neuronal activation induced by painful stimuli. Measurement of the magnitude of stimulation-induced activation, and its suppression with analgesics can provide objective measures of pain and efficacy of analgesics. This study investigates the feasibility of using spinal cord fMRI in anesthetized rats as a pain assay to test the analgesic effect of locally and systemically administered lidocaine. Blood volume (BV)-weighted fMRI signal acquired after intravenous injection of ultrasmall superparamagnetic iron oxide (USPIO) particles was used as an indirect readout of the neuronal activity. Transcutaneous noxious electrical stimulation was used as the pain model. BV-weighted fMRI signal could be robustly quantified on a run-by-run basis, opening the possibility of measuring pharmacodynamics (PD) of the analgesics with a temporal resolution of approximately 2 min. Local administration of lidocaine was shown to ablate all stimulation-induced fMRI signals by the total blockage of peripheral nerve transmission, while the analgesic effect of systemically administered lidocaine was robustly detected after intravenous infusion of approximately 3mg/kg, which is similar to clinical dosage for human. This study establishes spinal cord fMRI as a viable assay for analgesics. With respect to the mode of action of lidocaine, this study suggests that systemic lidocaine, which is clinically used for the treatment of neuropathic pain, and believed to only block the peripheral nerve transmission of abnormal neural activity (ectopic discharge) originating from the damaged peripheral nerves, also blocks the peripheral nerve transmission of normal neural activity induced by transcutaneous noxious electrical stimulation. PMID:19560271

  9. Time-effect relationship of mitochondrial DNA 4977bp deletion in human peripheral blood cell after X ray irradiation

    International Nuclear Information System (INIS)

    To investigate the time-effect of mitochondrial DNA 4977bp deletion in human peripheral blood cells exposed to X ray, human peripheral whole blood samples were collected from two healthy individuals, and exposed to X rays with dose from 0 to 10 Gy. The genomic DNAs were isolated from the whole-blood samples, and the levels of mtDNA 4977bp deletion and copy number of total mtDNA in the DNA samples were detected by Real-time PCR after irradiation at 2, 12, 24, 48 and 72 h, respectively. The results showed that the copy number of mtDNA 4977bp deletion and total mtDNA, and the rates of mtDNA 4977bp deletion increase with incubation time with dose at 5 Gy after irradiation. Moreover, they increased with dose from 0 to 10 Gy after irradiation at 24 h and 72 h, respectively. The results suggested that the levels of mtDNA 4977bp deletion and the copy number of total mtDNA in human peripheral blood cells exposed to X ray were accumulated with incubation time and dose increase, respectively. (authors)

  10. Effects of granulocyte-colony stimulating factor on chromosome aneuploidy and replication asynchrony in healthy peripheral blood stem cell donors.

    Science.gov (United States)

    Hirsch, Betsy; Oseth, Leann; Cain, Meghan; Trader, Erin; Pulkrabek, Shelley; Lindgren, Bruce; Luo, Xianghua; Clay, Mary; Miller, John; Confer, Dennis; Weisdorf, Daniel; McCullough, Jeffrey

    2011-09-01

    As peripheral blood has surpassed bone marrow as a predominant source of stem cells for transplantation, use of the cytokine granulocyte colony-stimulating factor (G-CSF) to mobilize peripheral blood stem cells (PBSCs) is increasing. Issues regarding potential genotoxic effects of even short-term, low-dose G-CSF treatment for the healthy donors have been raised. To address the question of chromosomal instability, we used FISH to evaluate the peripheral blood lymphocytes of 22 PBSC donors and 22 matched controls at 5 time points over a 12-month period. The specimens obtained were a pre-G-CSF, followed by collections at the time of PBSC harvest (days 5-7) and at 2, 6, and 12 months after donation. Eight additional PBSC donors provided a single sample at 12 months. Nine loci (mapped to chromosomes 7, 8, 9, 17, 21, and 22) were evaluated for aneuploidy, including 3 mapped to chromosome 7 because of the specific relevance of monosomy 7. Replication timing was evaluated for chromosome 15 and 17 loci. No evidence was found of G-CSF-induced chromosomal instability. This work supports the epidemiologic data that have demonstrated no increased risk for hematologic malignancies in G-CSF-primed PBSC donors. PMID:21719598

  11. Laser Doppler flowmetry signals to quantify effects of isoflurane on the peripheral cardiovascular system of healthy rats

    Science.gov (United States)

    Humeau, Anne; Fizanne, Lionel; Roux, Jérôme; Asfar, Pierre; Cales, Paul; Rousseau, David; Chapeau-Blondeau, François

    2007-12-01

    The optical Doppler effect resulting from interactions between laser light photons and red blood cells of the microcirculation is used to characterize the influence of isoflurane, an halogenated volatile anesthetic, on the peripheral cardiovascular system. After having recorded laser Doppler flowmetry blood perfusion signals on isoflurane-induced anesthetized healthy rats, wavelet analyses show a significant decrease of the myogenic and neurogenic activities when isoflurane dose increases from 1.5% to 3%. Moreover, the approximate entropy shows a weak decrease of signal irregularity when dose of isoflurane increases. These findings demonstrate the usefulness of the optical Doppler effect in physiological and pharmacological applications.

  12. Effects of water-borne copper and lead on the peripheral blood in the rosy barb, Barbus (Puntius) conchonius Hamilton

    Energy Technology Data Exchange (ETDEWEB)

    Gill, T.S. (Thomas Jefferson Univ., Philadelphia, PA (United States)); Tewari, H.; Pande, J. (Kumaun Univ., Naini (India))

    1991-04-01

    The Pb-induced abnormalities of hematopoiesis are primarily confined to the erythrocytes the leucocytes and platelets do not appear to be altered during chronic exposure. Pb effects in fishes show responses similar to those in mammals. The absence of erythrocyte {delta}-ALAD inhibition in fish exposed to Cd, Cu, Zn, and Hg indicated that this enzyme is quite specific for Pb. The objective of this work was to examine the effects of chronically sublethal concentrations of Cu and Pb on the peripheral blood parameters in the rosy barb, Barbus (Puntius) conchonius, a widely distributed freshwater bony fish.

  13. Effects of low dose rate fission neutron irradiation on the lymphocyte subpopulations of peripheral blood in rats

    International Nuclear Information System (INIS)

    Objective: To evaluate the effects of long-term, low dose rate fission neutron irradiation on lymphocyte subpopulations in peripheral blood of rats. Methods: Ninety-six rats were randomly divided into control group and irradiated group exposed to low dose rate fission neutron (252Cf,0.35 mGy/h) for 20.5 h every day. At days 14,28,42,56 and 70 d after irradiation and 35 d after stopping irradiation, After 8 rats of each group were killed, WBC and lymphocyte subpopulations of CD4+ CD3+, CD8+ CD3+ and CD45RA+/CD161?+ in peripheral blood were estimated respectively. Results: Compared with the control group, WBC was reduced significantly at dose of 0.3, 0.4 and 0.5 Gy (P+ CD3- was evidently higher compared with control group at doses of 0.1,0.3, 0.4 and 0.5 Gy and 35 d after stopping irradiation (P+ CD3- was obviously higher compared with control group at dose of 0.2 and 0.3 Gy (P+ CD3+ at dose of 0.1 Gy (P+ CD3+ at doses of 0.1 and 0.2 Gy (P+ CD45RA-) was increased ssup> CD45RA-) was increased significantly at doses of 0.2-0.3 Gy, and peripheral blood B cells(CD161?- CD45RA+) was reduced remarkably at doses of 0.1-0.5 Gy and 35 d after stopping irradiation compared with the control group. Conclusions: Long-term irradiation with low dose rate fission neutron could make TCR (T-cell-receptor) mutant, therefore, WBC, B cells in peripheral blood significantly reduced and NK cells increased. These changes may could not recover at 35 d after Stopping irradiation. (authors)

  14. Effect of peripheral vision training on the attack of beginner indoor soccer players: a study during competition

    Directory of Open Access Journals (Sweden)

    Nelson Kautzner Marques Junior

    2009-01-01

    Full Text Available This study was conducted within the context of Human Motor Skill Science, in the area of Biophysical Dimension and following the research line of the Study of Learning Mechanisms and Processes and of Motor Conduct within the epistemological construct of phenomenological explanation. The objective of this study was to investigate peripheral vision training (PVT and its effect on attack runs during indoor soccer, taking into account dominant laterality (brain hemisphere function in both learning speed andoffensive skills. Ten beginner indoor soccer players aged 10.4 ± 2.31 years, from Lar da Criança Padre Franz Neumair, Ititioca, Niterói, Rio de Janeiro, Brazil, participated in the study. The boys were divided into an experimental group (EG, n = 5 and a controlgroup (CG, n = 5 with similar dominant laterality (brain hemisphere function (H (EG: 80% left H and 20% right H, CG: 60% left H and 40% right H. The players underwent nine training sessions, followed by a championship, and then six additional sessions, followed by a second championship. Each championship was filmed for scoutvideo analysis. Two-way ANOVA revealed a significant difference in peripheral vision during offensive runs between CG and EG, with marked acquisition of peripheral vision in EG. The quality of the attack runs was significant (two-way ANOVA. EG was the better team at the beginning of the attack runs and during attack development, whereas CG was better at attack finalization during the first championship. EG showed more competence in attack run finalization during the second championship. No significant difference in the number of goals scored was observed between the two groups (two-wayANOVA, p>0.05. The frequency of participation in the training sessions was significant (t-test for independent samples, p?0.05, with EG attending more sessions. In conclusion, EG acquired peripheral vision, a finding suggesting that PVT improves the attack capacity of indoor soccer players.

  15. Effect of low-dose methylprednisolone on peripheral blood endothelial progenitor cells and its significance in rats after brain injury

    Directory of Open Access Journals (Sweden)

    Bin ZHANG

    2011-05-01

    Full Text Available Objective To explore the effects of low-dose methylprednisolone(MP treatment after traumatic brain injury(TBI in rats on the number of peripheral blood endothelial progenitor cells(EPCs and injury area of the brain.Methods One hundred and fifty-four adult male Wistar rats were involved in the present study,and they were randomly divided into normal control group(n=18,TBI control group(n=38,MP control group(n=30,MP+TBI group(n=30 and TBI+MP group(n=38.The TBI model was reproduced by fluid percussion injury(FPI.MP(5mg/kg was intraperitoneally administered once a day for 4 days.Peripheral venous blood samples were taken on day 1,3,7 and 14,and the counts of EPCs were determined by flow cytometry.The rats were sacrificed on day 1 and 3,brain edema was estimated by dry-wet weight method,and the blood-brain barrier(BBB permeability was determined by Evans-blue extravasation.Results The counts of peripheral blood EPCs were significantly higher in MP control group,MP+TBI group and TBI+MP group on day 1,3 and 7 than that in normal control and TBI control group,and it returned to the level of normal control group on day 14.The BBB permeability was improved and brain edema alleviated in MP+TBI and TBI+MP group on day 3.Conclusion The administration of low-dose MP may increase the count of peripheral blood EPCs in rats,decrease BBB damage,and alleviate brain edema.

  16. The impact of socioeconomic and clinical factors on purchase of prescribed analgesics before and after hysterectomy on benign indication

    DEFF Research Database (Denmark)

    Daugbjerg, Signe Bennedbæk; Brandsborg, Birgitte

    2014-01-01

    Pelvic pain is a primary symptom of women referred for hysterectomy. This study identified risk factors for purchase of prescribed analgesics before and after hysterectomy and examined purchase changes after hysterectomy, specifically focusing on socioeconomic effects.

  17. The analgesic efficacy of xylazine and dipyrone in hydrogen peroxide-induced oxidative stress in chicks

    OpenAIRE

    Mousa, Y. J.; Mohammad, F. K.

    2012-01-01

    The effect of oxidative stress–induced by hydrogen peroxide (H2O2) on the analgesic effect of xylazine and dipyrone in 7-14 days old chicks was studied, compared with the control group that given plane tap water. H2O2, 0.5 % in water, induced oxidative stress in chicks by significantly lowering glutathione, rising malondialdehyde in plasma, whole brain during the day 7th, 10th, 14th of chicks old in comparison with the control group. The analgesic median effective doses (ED50) of xylazine a...

  18. The Effect of Letter-stroke Boldness on Reading Speed in Central and Peripheral Vision

    OpenAIRE

    Bernard, Jean-baptiste; Kumar, Girish; Junge, Jasmine; Chung, Susana T. L.

    2013-01-01

    People with central vision loss often prefer boldface print over normal print for reading. However, little is known about how reading speed is influenced by the letter-stroke boldness of font. In this study, we examined the reliance of reading speed on stroke boldness, and determined whether this reliance differs between the normal central and peripheral vision. Reading speed was measured using the rapid serial visual presentation paradigm, where observers with normal vision read aloud short ...

  19. A Review of the Adverse Effects of Peripheral Alpha-1 Antagonists in Hypertension Therapy

    OpenAIRE

    Bryson Chris L; Psaty Bruce M

    2002-01-01

    Abstract Background Doxazosin and its role as an antihypertensive agent have come under recent scrutiny as a result of the early termination of that treatment arm in ALLHAT. It is unclear why the cardiovascular (CV) event rate in this randomized, controlled trial (RCT), especially heart failure, is higher in those treated with a doxazosin-based regimen than with a chlorthalidone based-regimen. There has been little work in the past to summarize information on peripheral alpha-1 antagonists th...

  20. Effect of blood storage conditions on DNA repair capacity measurements in peripheral blood mononuclear cells.

    OpenAIRE

    Allione, Alessandra; Porcedda, Paola; Russo, Alessia; Ricceri, Fulvio; Simonelli, Valeria; Minoprio, Anna; Guarrera, Simonetta; Pardini, Barbara; Mazzei, Filomena; Dogliotti, Eugenia; Giachino, Claudia; Matullo, Giuseppe

    2013-01-01

    Due to the great number of genes involved in DNA repair and the interactions among the pathways responsible for the repair of different types of DNA damage, there is an increasing need for simple and reliable approaches to phenotypically assess DNA repair capacity (DRC). The use of peripheral blood mononuclear cells (PBMCs) in DRC assays is particularly useful for human monitoring studies. However, in such studies it is not always possible to collect and process samples on the same day as the...

  1. Peripheral Blood RNA Expression Profiling in Illicit Methcathinone Users Reveals Effect on Immune System

    OpenAIRE

    Sikk, Katrin; Ko?ks, Sulev; Soomets, Ursel; Schalkwyk, Leonard C.; Fernandes, Cathy; Haldre, Sulev; Aquilonius, Sten-magnus; Taba, Pille

    2011-01-01

    Methcathinone (ephedrone) is relatively easily accessible for abuse. Its users develop an extrapyramidal syndrome and it is not known if this is caused by methcathinone itself, by side-ingredients (manganese), or both. In the present study we aimed to clarify molecular mechanisms underlying this condition. We used microarrays to analyze whole-genome gene expression patterns of peripheral blood from 20 methcathinone users and 20 matched controls. Gene expression profile data were analyzed by B...

  2. Effect of mixed ?-plus neutron-radiation on permeability to taurine of peripheral blood leukocyte membranes

    International Nuclear Information System (INIS)

    A study was made of permeability to taurine of cellular membranes of peripheral blood leukocytes in vitro under normal conditions and 24 k following mixed ?-plus neutron-irradiation in a dose of 3.5 Gy. It was established that radiation increases the taurine content of cells. The protein content of leukocytes also increases probably due to a better sorption of serum proteins of blood

  3. Effects of Lipid Emulsion and Multivitamins on the Growth of Microorganisms in Peripheral Parenteral Nutrition Solutions

    OpenAIRE

    Kuwahara, Takashi; Kaneda, Shinya; Shimono, Kazuyuki; Inoue, Yoshifumi

    2013-01-01

    Background: Blood stream infections caused by Bacillus cereus or Serratia marcescens in patients receiving peripheral parenteral nutrition (PPN) have occasionally been reported in Japan, but these microorganisms are not major causes of blood stream infections in patients receiving total parenteral nutrition via a central venous catheter. In Japan, commercially available PPN solutions contain amino acids, glucose, and electrolytes, but not contain lipid emulsion (LE) and multivitamins (MV). In...

  4. Evaluation of Anti-inflammatory and Analgesic Activity of the Extract and Fractions of Astragalus hamosus in Animal Models

    Science.gov (United States)

    Shojaii, Asie; Motaghinejad, Majid; Norouzi, Sima; Motevalian, Manijeh

    2015-01-01

    The objective of this study was to evaluate the anti-inflammatory and analgesic activities of the hydro-alcoholic extract of the pods of Astragalus hamosus (HAAH), a plant used in Iranian traditional medicine, and antinociceptive effects of different fractions in animal models. The anti-inflammatory effect was evaluated by the rat paw edema induced by formalin. Also the analgesic effect was examined by the acetic-acid-induced writhing response and hot plate test. The analgesic effects of chloroform, hexane, ethyl acetate and aqueous fractions were evaluated by the hot-plate method. The hydroalcoholic extract of Astragalus hamosus could reduce the edema in a dose-dependent manner (Pextract were more significant and comparable with the effect of sodium salicylate. Also application of different doses of HAAH had significant anti-nociceptive effects on both animal models. The findings showed that HAAH at doses of 700 and 1000 mg/Kg produced analgesic effects comparable to sodium salicylate. The hexane and ethyl acetate (but not the other fractions) showed significant analgesic activity in hot plate test, when compared to morphine. The results of this study demonstrated the anti-inflammatory and analgesic effects of HAAH extract and hexane and ethyl acetate fractions of the extract in animal models and justify traditional use of this plant in the treatment of pain and inflammatory conditions. More studies to clarify the active components are necessary. PMID:25561932

  5. Effect of autologous transplantation of peripheral blood stem cells on dogs with acute radiation sickness

    International Nuclear Information System (INIS)

    In a study of autologous transplantation of peripheral blood stem cells for the treatment of radiation sickness, 16 adult male mongrel dogs were used. All the animals received 1000 rad irradiation from a 60Co source at a dose rate of 9.7 to 11.0 R/min. Five dogs in the control group survived 6.6 days on the average after irradiation. Six dogs in the symptomatic treatment group survived 9.4 days. Another 5 dogs were transfused with monocytoid cells from the peripheral blood of their own, and the number of cells was 29.9x109, in which the CFU-C content was 12.6x105. The therapeutic regimen other than the transplantation of stem cells from the peripheral blood consisted of supportive measures to overcome serious symptoms of gastro-intestinal disorders. Results showed that four of the transfused dogs survived the whole period of observation - a total of 40 days. The recipients developed much more milder systematic symptoms than the control animals. (author)

  6. Research on effects of ionizing radiation of human peripheral blood white cell adhesive molecules

    International Nuclear Information System (INIS)

    Objective: To investigate the links between expression and function of adhesive molecule on the surface of irradiated peripheral blood white cells. Methods: Heparinized human peripheral blood was exposed to ? rays with different dose. At the different post-radiation time adhesive molecule expression on cellular surface was determined by double fluorescence labeling antibodies which were against adhesive molecule and special mark of granulocyte or mononuclear cell respectively with flow cytometry, and cellular adhesive ability to different matrixes mediated by adhesive molecule was estimated by commercializing enzyme-linked immunosorbent assay kit and crystalviolet dying. Results: A decline pattern of CD11b on surface of mononuclear cells and CD29 on surface of granulocyte with irradiation dose increase was found. The changes of adhesive ability of mononuclear cells to substance of ?1-integrin and collagen-I was well related with irradiation dose. Conclusion: Good relationship shown by the changes of adhesive molecule expression and adhesive ability mediated by the molecules on the surface of peripheral blood white cells with radiation dose was primary base of further research on indicting exposure dose by biomarker. (authors)

  7. Peripheral ?-opioid receptor mediated inhibition of calcium signaling and action potential-evoked calcium fluorescent transients in primary afferent CGRP nociceptive terminals.

    Science.gov (United States)

    Baillie, Landon D; Schmidhammer, Helmut; Mulligan, Sean J

    2015-06-01

    While ?-opioid receptor (MOR) agonists remain the most powerful analgesics for the treatment of severe pain, serious adverse side effects that are secondary to their central nervous system actions pose substantial barriers to therapeutic use. Preclinical and clinical evidence suggest that peripheral MORs play an important role in opioid analgesia, particularly under inflammatory conditions. However, the mechanisms of peripheral MOR signaling in primary afferent pain fibres remain to be established. We have recently introduced a novel ex vivo optical imaging approach that, for the first time, allows the study of physiological functioning within individual peripheral nociceptive fibre free nerve endings in mice. In the present study, we found that MOR activation in selectively identified, primary afferent CGRP nociceptive terminals caused inhibition of N-type Ca(2+) channel signaling and suppression of action potential-evoked Ca(2+) fluorescent transients mediated by 'big conductance' Ca(2+)-activated K(+) channels (BKCa). In the live animal, we showed that the peripherally acting MOR agonist HS-731 produced analgesia and that BKCa channels were the major effectors of the peripheral MOR signaling. We have identified two key molecular transducers of MOR activation that mediate significant inhibition of nociceptive signaling in primary afferent terminals. Understanding the mechanisms of peripheral MOR signaling may promote the development of pathway selective ?-opioid drugs that offer improved therapeutic profiles for achieving potent analgesia while avoiding serious adverse central side effects. PMID:25721395

  8. The association between anticholinergic load and cognitive performance, elevated blood pressure and the presence of peripheral anticholinergic side effects.

    Directory of Open Access Journals (Sweden)

    Jeff Hughes

    2009-04-01

    Full Text Available BACKGROUND:To quantify the association between anticholinergic drug use (burden or load and cognitive function (MMSE, bloodpressure and the presence of anticholinergic side effects.METHODS:The medical records of 182 aged care home residents in the Perth metropolitan area, Western Australia werereviewed retrospectively to obtain demographic data, past and current medical problems, history of use of agentswith anticholinergic effects and the following medication-related problems: cognitive impairment (as determined byMini Mental State Examination {MMSE} score, blood pressure elevation and the presence of anticholinergic sideeffects. Anticholinergic load was calculated, and the relationship between the anticholinergic load and the presenceof anticholinergic side effects was assessed using stepwise multiple regression and multiple logistic regressionanalysis.RESULTS:Increasing anticholinergic load was associated with the presence of peripheral anticholinergic side effects includinghypertension (AOR=1.53, dry mouth (AOR=1.38, dry eyes (AOR=1.30, constipation (AOR=1.24 and urinaryhesitancy (AOR=1.21 (all p values ?0.05. The anticholinergic load was not associated with blurred vision (p=0.084and Mini Mental State Examination score decline (p=0.142.CONCLUSIONS:The anticholinergic load was associated with statistically significantly increased risk of peripheral anticholinergicadverse effects in older aged care residents, however not with cognitive decline.

  9. Screening of Bauhinia purpurea Linn. for analgesic and anti-inflammatory activities

    Directory of Open Access Journals (Sweden)

    Shreedhara C

    2009-01-01

    Full Text Available Objectives: Ethanol extract of the stem of Bauhinia purpurea Linn. was subjected to analgesic and anti-inflammatory activities in animal models. Materials and Methods: Albino Wistar rats and mice were the experimental animals respectively. Different CNS depressant paradigms like analgesic activity (determined by Eddy?s hot plate method and acetic acid writhing method and anti-inflammatory activity determined by carrageenan induced paw edema using plethysmometer in albino rats were carried out, following the intra-peritoneal administration of ethanol extract of Bauhinia purpurea Linn. (BP at the dose level of 50mg/kg and 100mg/kg. Results: The analgesic and anti-inflammatory activities of ethanol extracts of BP were significant (P < 0.001. The maximum analgesic effect was observed at 120 min at the dose of 100mg/kg (i.p. and was comparable to that of standard analgin (150mg/kg and the percentage of edema inhibition effect was 46.4% and 77% for 50mg/kg and 100mg/kg (i.p respectively. Anti-inflammatory activity was compared with standard Diclofenac sodium (5mg/kg. Conclusion: Ethanol extract of Bauhinia purpurea has shown significant analgesic and anti-inflammatory activities at the dose of 100 mg/kg and was comparable with corresponding standard drugs. The activity was attributed to the presence of phytoconstituents in the tested extract.

  10. Anti-inflammatory and analgesic activity of different fractions of Boswellia serrata

    Directory of Open Access Journals (Sweden)

    A. Sharma

    2011-04-01

    Full Text Available

    The study was designed to investigate the anti-inflammatory and analgesic effect of different fractions of Boswellia serrata. The effect of different fractions of Boswellia serrata were studied using carrageenan induced paw edema, acetic acid induced writhing response, formalin induced pain, hot plate and tail flick method for studying anti-inflammatory and analgesic activity, respectively. The different fractions of B. serrata, essential oil (10 ml/kg, gum (100 mg/kg, resin (100 mg/kg oleo-resin (100 mg/kg and oleo-gum-resin (100 mg/kg significantly reduces carrageenan induced inflammation in rats and shows analgesic activity, as determined by acetic acid induced writhing response, formalin induced pain, hot plate and tail flick method. The different fractions of B. serrata showed prompt anti-inflammatory and analgesic activity due to the inhibition of 5-lipoxygenase enzyme.

    Keywords: Analgesic; Boswellia serrata; Inflammation; 5- lipoxygenase; Burseraceae.

  11. Conditional gene deletion reveals functional redundancy of GABAB receptors in peripheral nociceptors in vivo

    Directory of Open Access Journals (Sweden)

    Bettler Bernhard

    2009-11-01

    Full Text Available Abstract Background ?-aminobutyric acid (GABA is an important inhibitory neurotransmitter which mainly mediates its effects on neurons via ionotropic (GABAA and metabotropic (GABAB receptors. GABAB receptors are widely expressed in the central and the peripheral nervous system. Although there is evidence for a key function of GABAB receptors in the modulation of pain, the relative contribution of peripherally- versus centrally-expressed GABAB receptors is unclear. Results In order to elucidate the functional relevance of GABAB receptors expressed in peripheral nociceptive neurons in pain modulation we generated and analyzed conditional mouse mutants lacking functional GABAB(1 subunit specifically in nociceptors, preserving expression in the spinal cord and brain (SNS-GABAB(1-/- mice. Lack of the GABAB(1 subunit precludes the assembly of functional GABAB receptor. We analyzed SNS-GABAB(1-/- mice and their control littermates in several models of acute and neuropathic pain. Electrophysiological studies on peripheral afferents revealed higher firing frequencies in SNS-GABAB(1-/- mice compared to corresponding control littermates. However no differences were seen in basal nociceptive sensitivity between these groups. The development of neuropathic and chronic inflammatory pain was similar across the two genotypes. The duration of nocifensive responses evoked by intraplantar formalin injection was prolonged in the SNS-GABAB(1-/- animals as compared to their control littermates. Pharmacological experiments revealed that systemic baclofen-induced inhibition of formalin-induced nociceptive behaviors was not dependent upon GABAB(1 expression in nociceptors. Conclusion This study addressed contribution of GABAB receptors expressed on primary afferent nociceptive fibers to the modulation of pain. We observed that neither the development of acute and chronic pain nor the analgesic effects of a systematically-delivered GABAB agonist was significantly changed upon a specific deletion of GABAB receptors from peripheral nociceptive neurons in vivo. This lets us conclude that GABAB receptors in the peripheral nervous system play a less important role than those in the central nervous system in the regulation of pain.

  12. Changes in the Gene Expression of ?1 and ?2 Integrins Following Development of Tolerance to Analgesic Effect of Morphine in Rats

    Directory of Open Access Journals (Sweden)

    Jamal Ghorbi

    2010-01-01

    Full Text Available Objective: Considering the inhibitory effect of integrin-activity modulator (manganese onthe development of morphine tolerance; in this study we have tried to assess the effectof chronic administration of both morphine and manganese on the expression levels of ?1and ?2 integrins in the dorsal horn of the lumbar spinal cord.Materials and Methods: Morphine tolerance was induced by intrathecal injection of morphine,15 ?g/rat twice a day for five days. In order to study the effect of manganese on tolerancedevelopment; we injected manganese alone or in combination with morphine. Theanalgesic effect of morphine was assessed by using the tail flick test. Semi-quantitativereverse transcription - polymerase chain reaction (RT-PCR was used to assess the expressionlevels of ?1 and ?2 integrins.Results: As assessed on day 6, five days administration of morphine significantly increasedthe expression levels of integrins ?1 and ?2. Combined administration of morphineand manganese, which inhibited morphine tolerance, prevented the effect of morphineon integrins’ expression.Conclusion: Increased expression of integrins may be due to direct effect of chronic morphineor a negative feedback that resulted from the potent inhibitory effect of morphine onintegrins’ activity. It seems that the activating of integrins via manganese in the presenceof morphine can reverse feedback and consequently the effect of chronic administrationof morphine on ?1 and ?2 integrins’ and expression. Our findings suggest a role for intracellularmatrix molecules in the development of morphine tolerance and possibly otherforms of synaptic plasticity.

  13. Full Inhibition of Spinal FAAH Leads to TRPV1-Mediated Analgesic Effects in Neuropathic Rats and Possible Lipoxygenase-Mediated Remodeling of Anandamide Metabolism

    OpenAIRE

    Starowicz, Katarzyna; Makuch, Wioletta; Korostynski, Michal; Malek, Natalia; Slezak, Michal; Zychowska, Magdalena; Petrosino, Stefania; Petrocellis, Luciano; Cristino, Luigia; Przewlocka, Barbara; Di Marzo, Vincenzo

    2013-01-01

    Neuropathic pain elevates spinal anandamide (AEA) levels in a way further increased when URB597, an inhibitor of AEA hydrolysis by fatty acid amide hydrolase (FAAH), is injected intrathecally. Spinal AEA reduces neuropathic pain by acting at both cannabinoid CB1 receptors and transient receptor potential vanilloid-1 (TRPV1) channels. Yet, intrathecal URB597 is only partially effective at counteracting neuropathic pain. We investigated the effect of high doses of intrathecal URB597 on allodyni...

  14. THE IMMUNOMODULATORY EFFECTS OF PROBIOTIC BACTERIA ON PERIPHERAL BLOOD MONONUCLEAR CELLS (PBMCS OF ALLERGIC PATIENTS

    Directory of Open Access Journals (Sweden)

    Somaya M. El Sheikh

    2014-01-01

    Full Text Available Allergic diseases represent major health burden. An allergic reaction is characterized by a disrupted T- helper 1?T-helper 2 balance toward a preferential allergen specifically induced TH2 cytokine profile, causing allergic inflammation Probiotic bacteria have various benificial effects in many pathologic situation. Studies have shown that the bacteria present in the intestinal micro flora play a role in the TH1/TH2 balance and its modulation can promote the control of infectious and immune processes. Testing the effects of probiotic bacteria on TH1/TH2 cytokine production by peripheral blood mononuclear cells of allergic patients and control subjects. This study included 24 patients allergic to date pollen and 16 healthy control subjects. PBMC of both groups were separated and cultured for 72 h with date pollen allergen (home-made in the presence or absence of Lactobacillus rhamnosus ATCC 7469 (Living and dead and C- phycocyanin (extracted from Spirulina platensis. The cell culture supernatants were collected to measure Interlukin 4 and Interferon gamma by quantitative ELISA. Incubation of PBMCs of allergic patients with living Lactobacillus rhamnosus ATCC 7469 showed marked reduction in IL4 production (median IL4 concentarion = 3.9 pg. compared to PBMCs callenged with pollen alone (mediam IL4 conentration = 52.6 pg. When PBMC were incubated with living Lactobacillus rhamnosus in absence of allergen significant increase in and IFN? (median concentration = 42.75 pg. was obtained, compared to PBMC challenged with allergen alone (median = 22.8 pg. When PBMCs incubated with heat killed Lactobacillus rhamnosus either in presence or absence of the offending allergen, marked reduction in IL4 production was obtained (median = 10.6, 3.6 pg respectively compared to PBMC incubated with allergen alone (median = 52.6 pg. When PBMCs incubated with dead Lactobacillus rhamnosus, marked increase in IFN? production was obtained (median = 49 pg when compared to IFN? production by PBMC challenged with allergen (median 22.8 pg. PBMCs challenged with PC in the presence or absence of allergen showed marked decrease of IL4 production (median = 19.8, 17 pg respectively when compared to PBMC incubated with the offending allergen alone (median = 52.6 pg. PBMCs incubated with PC showed significant increase of and IFN? production (median= 319.6 pg when compared to PBMC incubated with the offending allergen alone (median = 22.8 pg. Conclusion: Lactobacillus rhamnosus ATCC 7469 and C-phycocyanin (extracted from Spirulina platensis inversed the TH1: TH2 polarization in allergic patients and could be a promissing line of treatment.

  15. Effects of tizanidine, eperisone and afloqualone on feline dorsal horn neuronal responses to peripheral cutaneous noxious and innocuous stimuli.

    Science.gov (United States)

    Davies, J

    1989-12-01

    The effects of eperisone and afloqualone have been compared with those of tizanidine on excitatory responses of spinal dorsal horn neurones, evoked by noxious and innocuous peripheral stimuli. Tizanidine, administered intravenously or iontophoretically, resulted in a profound, long-lasting and selective depression of the responses to noxious stimuli. In contrast, intravenous injection of eperisone produced either a rapidly reversible depression of responses to both noxious and innocuous stimuli or had no effect on these responses. Iontophoretic administration of eperisone also reduced neuronal responses to both forms of peripheral stimuli and that induced by quisqualate. This depressant action of eperisone was rapidly reversible but was often accompanied by a reduction of the amplitude of the action potentials. Afloqualone had no depressant action on any evoked response when administered iontophoretically. However, intravenous injection of this agent resulted in weak depressant effects on responses to noxious, innocuous or both types of stimuli, of a few of the neurones tested. This effect of afloqualone was not dose-dependent and was mimicked by control injections of the vehicle in which it was suspended. It is suggested that the muscle relaxants, eperisone and afloqualone, in contrast to tizanidine, do not possess any direct spinal antinociceptive activity. PMID:2615916

  16. ANTIHYPERGLYCEMIC AND ANALGESIC ACTIVITIES OF ETHANOLIC EXTRACT OF CASSIA FISTULA (L. STEM BARK

    Directory of Open Access Journals (Sweden)

    M. Ashraf Ali et al.

    2012-01-01

    Full Text Available The present study was designed to evaluate antihyperglycemic and analgesic effects of ethanolic extract of Cassia fistula (CF stem barks in rats and mice, respectively. The analgesic effect of extract was evaluated by acetic acid induced writhing test method while antihyperglycemic effect was investigated by oral glucose tolerance test (OGTT in normal and alloxan induced diabetic rats. Diclofenac (10 mg/kg, i. p. and metformin (150 mg/kg, p. o. were used as reference drugs for comparison. The extract significantly (P<0.05 reduced blood sugar level in alloxan induced diabetic (hyperglycaemic and glucose induced hyperglycemic (normo-hyperglycaemic rats orally at 250 mg/kg and 500 mg/kg body weight respectively. The glucose tolerance results showed significant (p<0.05 improved at the dose 250 mg/kg and 500 mg/kg body weight (b. wt. of ethanolic extract respectively. On the Other hand, the analgesic activity of extract at 200 mg/kg and 400 mg/kg dose level were produced 45% and 62% writhing inhibitory response but diclofenac was observed 82% of that when compared to control group. The plant's extract produced dose-dependent, significant (P<0.05 analgesic effects against chemically induced nociceptive pain in mice. Preliminary phytochemical screening of the plant extract showed the presence of alkaloids, triterpenoids, flavonoids, saponins and tannins etc. were present in the plant which has antihyperglycemic and analgesic properties. However a glucose tolerance hypoglycemic test is comparable to diabetic control group and effect is a dose dependent. The findings of this experimental animal study indicate that Cassia fistula stem-bark ethanolic extract possesses analgesic and antihyperglycemic properties; and thus lend pharmacological credence to the folkloric, ethnomedical uses of the plant in the treatment and/or management of painful, inflammatory conditions, as well as in the management and/or control of type 2 diabetes mellitus.

  17. Evaluation of analgesic activities of tremetone derivatives isolated from the Chilean altiplano medicine Parastrephia lepidophylla.

    Science.gov (United States)

    Benites, Julio; Gutierrez, Eunices; López, Jóse; Rojas, Mauricio; Rojo, Leonel; Costa, Maria do Céu; Vinardell, Maria Pilar; Calderon, Pedro Buc

    2012-05-01

    Parastrephia lepidophylla, family Asteraceae, has ancient use in traditional medicine in the region of Tarapacá, Chile. Bioguided fractionation of extracts of this plant was undertaken in the search for compounds with analgesic and antioxidant activity. Two benzofuran derivatives were isolated as the major components of this plant, identified as tremetone 1 and methoxytremetone 6. Remarkably, neither of these showed antioxidant activity, but tremetone 1 exhibited a morphine-like analgesic property. Reduction of this analgesic effect by naloxone suggests a direct effect on opiate receptors as a possible signaling pathway. However, both the low diffusion across lipid membranes (PAMPA assay) and the lipophilicity (Log P) shown by tremetone 1 make elusive the mechanism explaining its induced analgesia. PMID:22799089

  18. Nalbuphine, a non-controlled opioid analgesic, and its potential use in research mice.

    Science.gov (United States)

    Narver, Heather Lyons

    2015-03-01

    Nalbuphine is an inexpensive, non-controlled, opioid analgesic that has been in clinical use for decades. A kappa opioid receptor agonist and mu opioid receptor antagonist, nalbuphine causes fewer adverse effects than other opioid analgesics. The author reviews the characteristics of nalbuphine, analyzes studies of nalbuphine in mice and explores the potential use of nalbuphine to treat pain in research mice. In analgesiometric studies in mice, nalbuphine ameliorates both somatic and visceral pain. Nalbuphine seems to have a broad range of safe doses for subcutaneous administration in mice. Unlike non-steroidal anti-inflammatory drugs, nalbuphine does not antagonize prostaglandins or impede labor in mice. Although additional study is needed before clinical use can be recommended, evidence presented here suggests that nalbuphine might be an effective analgesic for dystocia (or difficult birth) and other painful conditions in research mice. PMID:25693108

  19. ANALGESIC ACTIVITY OF LEAVES EXTRACTS OF SAMANEA SAMAN MERR., AND PROSOPIS CINERARIA DRUCE.

    Directory of Open Access Journals (Sweden)

    Ahmed Syed Muzammil

    2013-01-01

    Full Text Available Current study was designed to explore the analgesic effects of methanol extracts of the leaves of Samanea saman Merr., and Prosopis cineraria Druce., using tail immersion test. The painful reactions in mice were produced by thermal stimuli through dipping the tail tips of mice into hot water. Methanol extracts of the leaves of Samanea saman Merr., and Prosopis cineraria Druce., were administered intraperitoneally at the dose of 100mg /kg body weight. Pethidine 50mg/Kg intraperitoneally was used as standard analgesic drug. The tail flick latency delay was measured at 0.5, 1.0, 1.5, 2.0, 2.5 and 3.0 hour after the intraperitoneal administration. Both extracts produce analgesic effects when compare with pethidine.

  20. Regulation of opioid receptor signalling: Implications for the development of analgesic tolerance

    Directory of Open Access Journals (Sweden)

    Nagi Karim

    2011-06-01

    Full Text Available Abstract Opiate drugs are the most effective analgesics available but their clinical use is restricted by severe side effects. Some of these undesired actions appear after repeated administration and are related to adaptive changes directed at counteracting the consequences of sustained opioid receptor activation. Here we will discuss adaptations that contribute to the development of tolerance. The focus of the first part of the review is set on molecular mechanisms involved in the regulation of opioid receptor signalling in heterologous expression systems and neurons. In the second part we assess how adaptations that take place in vivo may contribute to analgesic tolerance developed during repeated opioid administration.

  1. Regulation of opioid receptor signalling: implications for the development of analgesic tolerance.

    Science.gov (United States)

    Nagi, Karim; Piñeyro, Graciela

    2011-01-01

    Opiate drugs are the most effective analgesics available but their clinical use is restricted by severe side effects. Some of these undesired actions appear after repeated administration and are related to adaptive changes directed at counteracting the consequences of sustained opioid receptor activation. Here we will discuss adaptations that contribute to the development of tolerance. The focus of the first part of the review is set on molecular mechanisms involved in the regulation of opioid receptor signalling in heterologous expression systems and neurons. In the second part we assess how adaptations that take place in vivo may contribute to analgesic tolerance developed during repeated opioid administration. PMID:21663702

  2. Early effects of low dos 12C6+ ion or X-ray irradiation on human peripheral blood lymphocytes

    OpenAIRE

    Chen, Yingtai; Li, Yumin; Zhang, Hong; Xie, Yi; Chen, Xuezhong; Ren, Jinyu; Zhang, Xiaowei; Zhu, Zijiang; Liu, Hongliang; Zhang, Yawei

    2010-01-01

    The aim of this study was to estimate the acute effects of low dose 12C6+ ions or X-ray radiation on human immune function. The human peripheral blood lymphocytes (HPBL) of seven healthy donors were exposed to 0.05Gy 12C6+ ions or X-ray radiation and cell responses were measured at 24 hours after exposure. The cytotoxic activities of HPBL were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT); the percentages of T and NK cells subsets were detected by flow cyto...

  3. Recombinant human erythropoietin therapy is very effective after an autologous peripheral blood stem cell transplant when started soon after engraftment.

    OpenAIRE

    Baron, Fre?de?ric; Frere, Pascale; Fillet, Georges; Beguin, Yves

    2003-01-01

    PURPOSE: Previous trials of recombinant human erythropoietin (rHuEpo) therapy after autologous hematopoietic stem cell transplantation have administered very high doses of i.v. rHuEpo starting on day 1 and continuing for 1-2 months until erythroid engraftment and have shown no benefit of rHuEpo therapy. We sought to establish a more effective use of rHuEpo in this setting. EXPERIMENTAL DESIGN: In this report, we show in a first cohort of 45 lymphoma or myeloma patients undergoing peripheral b...

  4. The effect of ?-linolenic acid-?-lipoic acid on functional deficits in the peripheral and central nervous system of streptozotocin- diabetic rats

    OpenAIRE

    Gispen, W. H.; Biessels, G. J.; Smale, S.; Duis, S. E.; Kamal, A.

    2001-01-01

    Diabetes mellitus can lead to functional and structural deficits in both the peripheral and central nervous system. The pathogenesis of these deficits is multifactorial, probably involving, among others, microvascular dysfunction and oxidative stress. The present study examined the effects of 12 weeks of treatment with a conjugate of the essential fatty acid gamma-linolenic acid and the anti-oxidant alpha-lipoic acid (GLA?LA) on functional deficits in the peripheral and central nervous syste...

  5. Lentiviral Vector-Mediated Gradients of GDNF in the Injured Peripheral Nerve: Effects on Nerve Coil Formation, Schwann Cell Maturation and Myelination

    OpenAIRE

    Eggers, Ruben; Winter, Fred; Hoyng, Stefan A.; Roet, Kasper C. D.; Ehlert, Erich M.; Malessy, Martijn J. A.; Verhaagen, Joost; Tannemaat, Martijn R.

    2013-01-01

    Although the peripheral nerve is capable of regeneration, only a small minority of patients regain normal function after surgical reconstruction of a major peripheral nerve lesion, resulting in a severe and lasting negative impact on the quality of life. Glial cell-line derived neurotrophic factor (GDNF) has potent survival- and outgrowth-promoting effects on motoneurons, but locally elevated levels of GDNF cause trapping of regenerating axons and the formation of nerve coils. This phenomenon...

  6. Structure-related effects of pyrethroid insecticides on the lateral-line sense organ and on peripheral nerves of the clawed frog, Xenopus laevis

    OpenAIRE

    Vijverberg, H. P. M.; Ruigt, Ges F.; Bercken, J. Den

    1982-01-01

    The effects of seven different pyrethroid insecticides on the lateral-line sense organ and on peripheral nerves of the clawed frog, Xenopus laevis, were investigated by means of electrophysiological methods. The results show that two classes of pyrethroid can be clearly distinguished. (i) Pyrethroids without an ?-cyano group (permethrin, cismethrin, and bioresmethrin). These noncyano pyrethroids induce short trains of nerve impulses in the lateral-line sense organ. In peripheral nerve branch...

  7. Allosteric interactions between ? and ? opioid receptors in peripheral sensory neurons.

    Science.gov (United States)

    Berg, Kelly A; Rowan, Matthew P; Gupta, Achla; Sanchez, Teresa A; Silva, Michelle; Gomes, Ivone; McGuire, Blaine A; Portoghese, Philip S; Hargreaves, Kenneth M; Devi, Lakshmi A; Clarke, William P

    2012-02-01

    The peripheral ? opioid receptor (DOR) is an attractive target for analgesic drug development. There is evidence that DOR can form heteromers with the ?-opioid receptor (KOR). As drug targets, heteromeric receptors offer an additional level of selectivity and, because of allosteric interactions between protomers, functionality. Here we report that selective KOR antagonists differentially altered the potency and/or efficacy of DOR agonists in primary cultures of adult rat peripheral sensory neurons and in a rat behavioral model of thermal allodynia. In vitro, the KOR antagonist nor-binaltorphimine (nor-BNI) enhanced the potency of [D-Pen(2,5)]-enkephalin (DPDPE), decreased the potency of [D-Ala(2),D-Leu(5)]-enkephalin (DADLE), and decreased the potency and efficacy of 4-[(R)-[(2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl](3-methoxyphenyl)methyl]-N,N-diethylbenzamide (SNC80) to inhibit prostaglandin E(2) (PGE(2))-stimulated adenylyl cyclase activity. In vivo, nor-BNI enhanced the effect of DPDPE and decreased the effect of SNC80 to inhibit PGE(2)-stimulated thermal allodynia. In contrast to nor-BNI, the KOR antagonist 5'-guanidinonaltrindole (5'-GNTI) reduced the response of DPDPE both in cultured neurons and in vivo. Evidence for DOR-KOR heteromers in peripheral sensory neurons included coimmunoprecipitation of DOR with KOR, a DOR-KOR heteromer selective antibody augmented the antinociceptive effect of DPDPE in vivo, and the DOR-KOR heteromer agonist 6'-GNTI inhibited adenylyl cyclase activity in vitro as well as PGE(2)-stimulated thermal allodynia in vivo. Taken together, these data suggest that DOR-KOR heteromers exist in rat primary sensory neurons and that KOR antagonists can act as modulators of DOR agonist responses most likely through allosteric interactions between the protomers of the DOR-KOR heteromer. PMID:22072818

  8. Inhibition of anandamide hydrolysis attenuates nociceptor sensitization in a murine model of chemotherapy-induced peripheral neuropathy.

    Science.gov (United States)

    Uhelski, Megan L; Khasabova, Iryna A; Simone, Donald A

    2015-03-01

    Painful neuropathy frequently develops as a consequence of commonly used chemotherapy agents for cancer treatment and is often a dose-limiting side effect. Currently available analgesic treatments are often ineffective on pain induced by neurotoxicity. Although peripheral administration of cannabinoids, endocannabinoids, and inhibitors of endocannabinoid hydrolysis has been effective in reducing hyperalgesia in models of peripheral neuropathy, including chemotherapy-induced peripheral neuropathy (CIPN), few studies have examined cannabinoid effects on responses of nociceptors in vivo. In this study we determined whether inhibition of fatty acid amide hydrolase (FAAH), which slows the breakdown of the endocannabinoid anandamide (AEA), reduced sensitization of nociceptors produced by chemotherapy. Over the course of a week of daily treatments, mice treated with the platinum-based chemotherapy agent cisplatin developed robust mechanical allodynia that coincided with sensitization of cutaneous C-fiber nociceptors as indicated by the development of spontaneous activity and increased responses to mechanical stimulation. Administration of the FAAH inhibitor URB597 into the receptive field of sensitized C-fiber nociceptors decreased spontaneous activity, increased mechanical response thresholds, and decreased evoked responses to mechanical stimuli. Cotreatment with CB1 (AM281) or CB2 (AM630) receptor antagonists showed that the effect of URB597 was mediated primarily by CB1 receptors. These changes following URB597 were associated with an increase in the endocannabinoid anandamide in the skin. Our results suggest that enhanced signaling in the peripheral endocannabinoid system could be utilized to reduce nociceptor sensitization and pain associated with CIPN. PMID:25505113

  9. Peripheral kappa and delta opioid receptors are involved in the antinociceptive effect of crotalphine in a rat model of cancer pain.

    Science.gov (United States)

    Brigatte, Patricia; Konno, Katsuhiro; Gutierrez, Vanessa Pacciari; Sampaio, Sandra Coccuzzo; Zambelli, Vanessa Olzon; Picolo, Gisele; Curi, Rui; Cury, Yara

    2013-08-01

    Cancer pain is an important clinical problem and may not respond satisfactorily to the current analgesic therapy. We have characterized a novel and potent analgesic peptide, crotalphine, from the venom of the South American rattlesnake Crotalus durissus terrificus. In the present work, the antinociceptive effect of crotalphine was evaluated in a rat model of cancer pain induced by intraplantar injection of Walker 256 carcinoma cells. Intraplantar injection of tumor cells caused the development of hyperalgesia and allodynia, detected on day 5 after tumor cell inoculation. Crotalphine (6 ?g/kg), administered p.o., blocked both phenomena. The antinociceptive effect was detected 1 h after treatment and lasted for up to 48 h. Intraplantar injection of nor-binaltorphimine (50 g/paw), a selective antagonist of ?-opioid receptors, antagonized the antinociceptive effect of the peptide, whereas N,N-diallyl-Tyr-Aib-Phe-Leu (ICI 174,864, 10 ?g/paw), a selective antagonist of ?-opioid receptors, partially reversed this effect. On the other hand, D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr amide (CTOP, 20 g/paw), an antagonist of ?-opioid receptors, did not modify crotalphine-induced antinociception. These data indicate that crotalphine induces a potent and long lasting opioid-mediated antinociception in cancer pain. PMID:23628488

  10. Analgesia e ação antiinflamatória da Arnica montana 12CH comparativamente ao cetoprofeno em cães / Analgesic and anti-inflammatory effects of Arnica montana 12CH in comparison with ketoprofen in dogs

    Scientific Electronic Library Online (English)

    Renata Navarro, Cassu; Carlos Meirelles, Collares; Beatriz Porto, Alegre; Rosângela Cristóvão, Ferreira; Helaine, Stevanin; Camila Ângela, Bernardi.

    1784-17-01

    Full Text Available Objetivou-se avaliar os efeitos analgésico e antiinflamatório da Arnica montana 12CH comparativamente ao cetoprofeno em cadelas submetidas à ovariossalpingohisterectomia (OSH). Foram avaliadas 16 cadelas, distribuídas aleatoriamente em dois grupos de oito animais cada, tratados por via oral com 1mg [...] kg-1 de cetoprofeno (TC) e com cinco glóbulos de Arnica montana 12CH (TA). Decorridos 60 minutos, os animais foram tranquilizados com acepromazina (0,05mg kg-1, IV), seguindo-se indução e manutenção anestésica com propofol (5mg kg-1, IV) e isofluorano, respectivamente. Foram mensurados: frequência cardíaca, frequência respiratória, pressão arterial sistólica, concentração final expirada de dióxido de carbono, concentração final expirada de isofluorano, variáveis hemogasométricas, concentração sérica de cortisol, grau de analgesia e de inflamação. Em casos de analgesia insuficiente, foi realizada suplementação com morfina (0,5mg kg-1, IM). A estatística foi realizada com ANOVA e teste de Tukey (P Abstract in english This study aimed to evaluate the analgesic and anti-inflammatory effects of Arnica montana 12CH comparatively to ketoprofen in dogs undergoing ovariohysterectomy. Sixteen female dogs were randomly distributed in two groups of eight animals and received 1mg kg-1 of ketoprofen (TC) and 5 globules of A [...] rnica montana 12CH (TA) by oral route. After 60 minutes, the dogs were sedated with acepromazine (0.05mg kg-1, IV), followed by anesthetic induction with propofol (5mg kg-1 IV) and maintained with isoflurane. Heart rate, respiratory rate, systolic blood pressure, arterial blood gases, serum cortisol concentration and degree of analgesia and inflammation were measured. Additional morphine (0.5mg kg-1IM) was given when the analgesia was insufficient. Statistical analyses were performed by ANOVA and Tukey tests (P

  11. Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery.

    Science.gov (United States)

    Curtright, Andrew; Rosser, Micaela; Goh, Shamii; Keown, Bailey; Wagner, Erinn; Sharifi, Jasmine; Raible, David W; Dhaka, Ajay

    2015-01-01

    Acute and chronic pain conditions are often debilitating, inflicting severe physiological, emotional and economic costs and affect a large percentage of the global population. However, the development of therapeutic analgesic agents based primarily on targeted drug development has been largely ineffective. An alternative approach to analgesic development would be to develop low cost, high throughput, untargeted animal based behavioral screens that model complex nociceptive behaviors in which to screen for analgesic compounds. Here we describe the development of a behavioral based assay in zebrafish larvae that is effective in identifying small molecule compounds with analgesic properties. In a place aversion assay, which likely utilizes supraspinal neuronal circuitry, individually arrayed zebrafish larvae show temperature-dependent aversion to increasing and decreasing temperatures deviating from rearing temperature. Modeling thermal hyperalgesia, the addition of the noxious inflammatory compound and TRPA1 agonist allyl isothiocyanate sensitized heat aversion and reversed cool aversion leading larvae to avoid rearing temperature in favor of otherwise acutely aversive cooler temperatures. We show that small molecules with known analgesic properties are able to inhibit acute and/or sensitized temperature aversion. PMID:25587718

  12. Poisoning deaths involving opioid analgesics - new york state, 2003-2012.

    Science.gov (United States)

    Sharp, Mark J; Melnik, Thomas A

    2015-04-17

    Deaths involving opioid analgesics have increased dramatically in the United States. Approximately 4,000 such deaths were documented in 1999, increasing to 16,235 in 2013, reflecting a nearly quadrupled death rate from 1.4 to 5.1 deaths per 100,000. To investigate this increase in New York state, trends in poisoning deaths involving opioid analgesics from 2003 to 2012 were examined. Data sources used were New York state vital statistics multiple-cause-of-death data, consisting of data from both the New York City (NYC)* and non-NYC reporting jurisdictions, as well as statewide Medicaid enrollment data. Deaths involving opioid analgesics increased both in number and as a percentage of all drug poisoning deaths, and rates were highest among men, whites, persons aged 45-64 years, persons residing outside of NYC, and Medicaid enrollees. The analysis found that, in 2012, 70.7% of deaths involving opioid analgesics also involved at least one other drug, most frequently a benzodiazepine. These results underscore the potential to mitigate the trend of increasing opioid analgesic-related mortality through initiatives such as New York state's Internet System for Tracking Over-Prescribing (I-STOP) law,† which took effect on August 27, 2013. Provisions under I-STOP include the requirements that providers consult the Prescription Monitoring Program (PMP) Registry when writing prescriptions for controlled substances, and that they use electronic prescribing. PMID:25879895

  13. The effects of age and LPS-mediated peripheral inflammation on numbers of central catecholaminergic neurons

    OpenAIRE

    Mouton, P. R.; Kelley-bell, B.; Tweedie, D.; Spangler, E. L.; Perez, E.; Carlson, O. D.; Short, R. G.; Decabo, R.; Chang, J.; Ingram, D. K.; Li, Y.; Greig, N. H.

    2010-01-01

    Parkinson’s disease (PD), an age-related movement disorder, is characterized by severe catecholaminergic neuron loss in the substantia nigra pars compacta-ventral tegmental area (SNPC-VTA) and locus coeruleus (LC). To assess the stability of these central catecholaminergic neurons following an acute episode of severe inflammation, 6 to 22 month-old C57/Bl6 mice received a maximally tolerated dose of LPS followed by euthanasia two hours later to assay peak levels of peripheral and central cy...

  14. Iopaque 300 vs. Omnipaque 300: Comparison of Efficacy and Adverse Effects in Peripheral Angiography

    OpenAIRE

    Hadjibabaie, M.; Alidadi, S.; Firouznia, K.; Ghanaati, H.; Rokni, H.; Saberi, H.; Shabani, M. A.; Sh. Shariyaran; Shakiba, M.; Bakhshandeh, H.; Shadman Yazdi, A. A.; Khoei, A.

    2007-01-01

    Background and Objectives: The contrast medium has to be selected with regard to safety and efficacy. Io-hexol is produced in Iran by the brand name of Iopaque. But even now, there are some concerns about using this brand instead of the traditional and more expensive brand (Omnipaque). This study was designed to compare the safety and radiographic effi-cacy of Iopaque 300 mg I/ml and Omnipaque 300 mg I/ml in peripheral angiography. Materials and Methods: eighty-four patients ran-domly receive...

  15. Investigation of the potentiation of the analgesic effects of fentanyl by ketamine in humans: a double-blinded, randomised, placebo controlled, crossover study of experimental pain[ISRCTN83088383

    Directory of Open Access Journals (Sweden)

    Nadeson Raymond

    2005-04-01

    Full Text Available Abstract Background Despite preclinical evidence suggesting a synergistic interaction between ketamine and opioids promoting analgesia, several clinical trials have not identified dosing regimens capable of eliciting a benefit in the co-administration of ketamine with opioids. Methods Ten healthy volunteers participated in a double blinded, randomised, placebo controlled, crossover laboratory study in order to determine whether a low dose of ketamine potentiated the antinociceptive effect of fentanyl without causing an increase in sedative effects. A battery of tests was used to assess both nociception and sedation including electrical current, pressure, thermal stimuli, psychometric tests, and both subjective and objective scores of sedation. Target controlled infusions of the study drugs were used. Ketamine and fentanyl were administered alone and in combination in a double-blinded randomised crossover design. Saline was used as the control, and propofol was used to validate the tests of sedation. Cardiovascular and respiratory parameters were also assessed. Results The electrical current pain threshold dose response curve of fentanyl combined with ketamine was markedly steeper than the dose response curve of fentanyl alone. While a ketamine serum concentration of 30 ng/ml did not result in a change in electrical pain threshold when administered alone, when it was added to fentanyl, the combination resulted in greater increase in pain threshold than that of fentanyl administered alone. When nociception was assessed using heat and pressure stimuli, ketamine did not potentiate the anti-nociceptive effect of fentanyl. There was no difference between the sedative effect of fentanyl and fentanyl in combination with ketamine as assessed by both subjective and objective measures of sedation. Cardiovascular and respiratory parameters were unaffected by the study drugs at the doses given. Conclusion A serum concentration of ketamine that did not alter indices of sedation potentiated the antinociceptive effect of fentanyl. This potentiation of antinociception occurred without an increase in sedation suggesting that low steady doses of ketamine (30–120 ng/ml might be combined with ? opioid agonists to improve their analgesic effect in a clinical setting. (296 words

  16. Evaluation of anti-hyperalgesic and analgesic effects of two benzodiazepines in human experimental pain: a randomized placebo-controlled study

    OpenAIRE

    Vuilleumier, Pascal; Besson, Marie; Desmeules, Jules Alexandre; Arendt-nielsen, Lars; Curatolo, Michele

    2013-01-01

    Compounds that act on GABA-receptors produce anti-hyperalgesia in animal models, but little is known on their effects in humans. The aim of this study was to explore the potential usefulness of GABA-agonism for the control of pain in humans. Two agonists at the benzodiazepine-binding site of GABAA-receptors (clobazam and clonazepam) were studied using multiple experimental pain tests. Positive results would support further investigation of GABA agonism for the control of clinical pain.

  17. Platelet-rich plasma exerts antinociceptive activity by a peripheral endocannabinoid-related mechanism.

    Science.gov (United States)

    Descalzi, Fiorella; Ulivi, Valentina; Cancedda, Ranieri; Piscitelli, Fabiana; Luongo, Livio; Guida, Francesca; Gatta, Luisa; Maione, Sabatino; Di Marzo, Vincenzo

    2013-10-01

    In regenerative medicine, platelet by-products containing factors physiologically involved in wound healing, have been successfully used in the form of platelet-rich plasma (PRP) for the topical therapy of various clinical conditions since it produces an improvement in tissue repair as well as analgesic effects. Measurement of endocannabinoids and related compounds in PRP revealed the presence of a significant amount of anandamide, 2-arachidonoylglycerol, palmitoylethanolamide, and oleoylethanolamide. Investigation of the activity of PRP on the keratinocyte cell line NCTC2544 in physiological and inflammatory conditions showed that, under inflammatory conditions, PRP induced in a statistically significant manner the production of these compounds by the cells suggesting that PRP might induce the production of these analgesic mediators particularly in the physiologically inflamed wounded tissue. Studies in a mouse model of acute inflammatory pain induced by formalin injection demonstrated a potent antinociceptive effect against both early and late nocifensive responses. This effect was observed following intrapaw injection of (1) total PRP; (2) lipids extracted from PRP; and (3) an endocannabinoid-enriched lipid fraction of PRP. In all conditions, antagonists of endocannabinoid CB1 and CB2 receptors, injected in the paw, abrogated the antinociceptive effects strongly suggesting for this preparation a peripheral mechanism of action. In conclusion, we showed that PRP and PRP lipid extract exert a potent antinociceptive activity linked, at least in part, to their endocannabinoids and related compound content, and to their capability of elevating the levels of these lipid mediators in cells. PMID:23578218

  18. Analgesic effectiveness of the association of transcutaneous electrical nerve stimulation and cryotherapy for chronic low back pain / Eficácia analgésica da associação da eletroestimulação nervosa transcutânea e crioterapia na lombalgia crônica

    Scientific Electronic Library Online (English)

    Eliziete Almeida de, Abreu; Jean Douglas Moura dos, Santos; Patrícia Lima, Ventura.

    2011-03-01

    Full Text Available SciELO Brazil | Language: English Abstract in portuguese JUSTIFICATIVA E OBJETIVOS: A eletroestimulação nervosa transcutânea (TENS) e a crioterapia são recursos fisioterapêuticos aplicados isoladamente, uma vez que existe a possibilidade de interação entre a TENS e a crioterapia caso sejam utilizadas associadas. O objetivo desse estudo foi avaliar a efeti [...] vidade analgésica da associação TENS e crioterapia isoladas e associadas no alívio da lombalgia crônica. MÉTODO: Trata-se de ensaio clínico envolvendo 6 pacientes com dor lombar crônica, divididas em 3 grupos: crioterapia, TENS, e associação crioterapia e TENS. A técnica analgésica foi aplicada pelo tempo de 20 minutos, durante 5 dias, com 1 sessão por dia. Todas as pacientes foram submetidas à cinesioterapia convencional com alongamento de isquiostibiais, quadrado lombar e iliopsoas, com o objetivo de aumentar a aderência ao tratamento. A crioterapia foi feita com bolsa de gelo moído, e a modalidade de TENS foi a burst, com o aparelho Physiotonus TENS/FES 3050, da marca BIOSET, com trens de pulsos de 2 Hz, frequência individual de pulsos de 100 Hz e duração de pulso de 150 µs. A intensidade da dor foi avaliada pela escala analógica visual antes e após a realização de cada sessão. RESULTADOS: Quanto a intensidade da dor, no grupo crioterapia, as medianas dos escores iniciais e finais foram 5,5 e 4, respectivamente, e nos grupos TENS e TENS associado à crioterapia as medianas foram 5 e 3, respectivamente. Quanto ao grau de alívio, 100% referiram alívio bom no grupo TENS, e nos grupos crioterapia e TENS associado à crioterapia 50% referiram alívio bom e 50% alívio muito bom. CONCLUSÃO: Apesar da terapia combinada não ter apresentado nenhuma melhora significativa em relação às modalidades de terapias isoladas, as três modalidades analgésicas utilizadas neste estudo foram eficazes em aliviar a dor lombar crônica das pacientes e nos grupos em que foi utilizado a crioterapia o grau de satisfação das pacientes foi maior do que as do grupo em que foi usada apenas a TENS. Abstract in english BACKGROUND AND OBJECTIVES: Transcutaneous electrical nerve stimulation (TENS) and cryotherapy are physical therapy resources individually used, since there is the possibility of interaction between TENS and cryotherapy if they are associated. This study aimed at evaluating the analgesic effectivenes [...] s of the association or not of TENS and cryotherapy to relieve chronic low back pain. METHOD: Clinical trial involving six chronic low back pain patients distributed in three groups: cryotherapy, TENS, and the association of both techniques. Analgesia was induced for 20 minutes during 5 days, with one session per day. All patients were submitted to conventional kinesiotherapy with ischiotibial, lumbar square and iliopsoas elongation, aiming at increasing adherence to treatment. Cryotherapy was applied with crushed ice bag and TENS was in burst with Physiotonus TENS/FES 3050 equipment of the BIOSET brand, with pulse trains of 2 Hz, individual pulse frequencies of 100 Hz and pulse duration of 150 µs. Pain intensity was evaluated by the visual analog scale before and after each session. RESULTS: With regard to pain intensity in the cryotherapy group, initial and final medians were 5.5 and 4, respectively. For the TENS and TENS associated to cryotherapy groups they were 5 and 3, respectively. With regard to pain relief, 100% have referred good relief in the TENS group; in cryotherapy and TENS associated to cryotherapy groups 50% have referred good relief and 50% very good relief. CONCLUSION: Although the combined therapy has caused no significant improvement as compared to isolated therapies the three analgesic modalities used in this study were effective to relieve chronic low back pain. Satisfaction was higher in the cryotherapy group as compared to the TENS group.

  19. Analgesic nephropathy: an underestimated cause of end-stage renal disease.

    Science.gov (United States)

    Drukker, W; Schwarz, A; Vanherweghem, J L

    1986-07-01

    Addiction and abuse of antipyretic analgesics has been recognized early after the turn of this century. The incidence markedly increased and the syndrome spread over many countries in the first half of the 20th century. The syndrome and its pathology, consisting of renal papillary necrosis and tubulo-interstitial nephritis, was first described in the medical literature in the early 1950's in Switzerland by Spühler and Zollinger, who rightly suspected chronic analgesic (Saridon) intoxication as being the cause in their cases. Clinically the disease is characterized by slowly progressive renal failure with renal colics from passage of necrotic papillae. Death from uremia is common unless dialyzed. The disease has been particularly prevalent in certain areas of Australia, Belgium, Western Germany, in Switzerland and some other countries. The nephrotoxic agents are mixtures of salicylates (aspirin) with phenacetin or acetaminophen. The principal nephrotoxic compound is probably aspirin--the aminophenol derivatives increasing its nephrotoxicity. However, all these components alone may cause--exceptionally--the syndrome. Rarely some newer, nonsteroid analgesics (NSAID's) can also be nephrotoxic. Phenacetin has--in particular in compound mixtures--mood-altering (euphoric) properties, giving rise to craving, addiction and chronic abuse. Addiction has been greatly facilitated by the over-the-counter availability of these cheap analgesic mixtures. Mass addiction--and abuse--may occur in all kinds of communities, in factories or families because of the euphoric effect, taking away fatigue and weariness and increasing productivity. There is a relation between the per capita consumption of antipyretic analgesics and analgesic nephropathy in several countries and in certain districts. The pattern of sales and mass consumption (and the incidence of nephropathy) is substantially promoted by the local presence of production facilities, usually accompanied by vigorous sales and advertising policies. Individual addiction usually occurs in psychoneurotic females often with social and marital problems and mental instability, often with long histories of headaches, backpains, and other, often psychogenic disorders. Analgesic nephropathy is often complicated by anemia, peptic ulcer, premature aging and atherosclerosis and in 8-10% by uro-epithelial carcinoma (the so called analgesic syndrome). The diagnosis depends largely on the history of chronic abuse of analgesics, which is often doggedly denied, hampering the diagnosis.(ABSTRACT TRUNCATED AT 400 WORDS) PMID:3536758

  20. Effects of peripheral inflammation on the blood-spinal cord barrier

    Directory of Open Access Journals (Sweden)

    Xanthos Dimitris N

    2012-06-01

    Full Text Available Abstract Background Changes in the blood-central nervous system barriers occur under pathological conditions including inflammation and contribute to central manifestations of various diseases. After short-lasting peripheral and neurogenic inflammation, the evidence is mixed whether there are consistent blood-spinal cord changes. In the current study, we examine changes in the blood-spinal cord barrier after intraplantar capsaicin and ?-carrageenan using several methods: changes in occludin protein, immunoglobulin G accumulation, and fluorescent dye penetration. We also examine potential sex differences in male and female adult rats. Results After peripheral carrageenan inflammation, but not capsaicin inflammation, immunohistochemistry shows occludin protein in lumbar spinal cord to be significantly altered at 72?hours post-injection. In addition, there is also significant immunoglobulin G detected in lumbar and thoracic spinal cord at this timepoint in both male and female rats. However, acute administration of sodium fluorescein or Evans Blue dyes is not detected in the parenchyma at this timepoint. Conclusions Our results show that carrageenan inflammation induces changes in tight junction protein and immunoglobulin G accumulation, but these may not be indicative of a blood-spinal cord barrier breakdown. These changes appear transiently after peak nociception and may be indicative of reversible pathology that resolves together with inflammation.

  1. Effects of peripheral and axial substitutions on electronic transitions of tin naphthalocyanines.

    Science.gov (United States)

    Jakubikova, Elena; Campbell, Ian H; Martin, Richard L

    2011-08-25

    Tin naphthalocyanine molecules display strong absorption in the infrared region (IR), making them ideal as components of organic photodiodes and solar cells. We use density functional theory and time-dependent density functional theory (TD-DFT) at the B3LYP level to study the influence of axial and peripheral ligands on the absorption wavelength of tin naphthalocyanines. We find that TD-DFT is successful at reproducing the experimental absorption spectra of free base naphthalocyanine and tin naphthalocyanine molecules and can be used as a reliable tool to predict absorption spectra of substituted naphthalocyanines. Functional groups attached axially to tin (-F, -Cl, -Br, -I) and peripherally to the inner ring (-F, -Cl, -Br, -Ph, -OH, -COCH(3), -O(CH(2))(3)CH(3)) of the tin naphthalocyanine molecule tune the excitation wavelength in the near-infrared region between 770 and 940 nm. While substituents to the outer naphthalocyanine ring (-Cl, -Br) affect the intensity of the absorption peaks in the NIR region, they do not influence their absorption wavelength. Asymmetric substitution of naphthalocyanine pendant arms can be employed to decrease intensity of the absorption peaks in the visible region with respect to the intensity of the peaks in the NIR. PMID:21800923

  2. Tratamiento epidural del dolor en la isquemia vascular periférica (I Treatment of epidural pain in peripheral vascular ischemia (I

    Directory of Open Access Journals (Sweden)

    M.J. Orduña González

    2009-03-01

    Full Text Available La isquemia arterial periférica puede ser el resultado de diversas enfermedades que afectan la vascularización de los miembros, generando dolor, discapacidad y deterioro de la calidad de vida del paciente, y en los casos de isquemia crítica produciendo una considerable morbimortalidad y dolor crónico. El objetivo ha sido realizar una revisión histórica de publicaciones científicas acerca de los distintos tipos de isquemia periférica, del dolor derivado, de su tratamiento analgésico por vía epidural y de las peculiaridades que hay que tener en cuenta en dicha patología. Se ha realizado una búsqueda en MEDLINE y se han recopilado los principales datos respecto a la evolución y las principales líneas de investigación científicas publicadas en las áreas de la analgesia epidural y el dolor en el contexto de la isquemia arterial periférica. Desde su introducción terapéutica en la isquemia periférica, la analgesia con perfusión de fármacos epidurales ha constituido un método eficaz analgésico, que en el caso de los anestésicos locales, además, aporta efectos hemorreológicos positivos a través de un bloqueo simpático. La neuroestimulación eléctrica epidural (NEE medular es una modalidad analgésica crónica con indicaciones específicas dentro de la isquemia periférica, con potencial efecto trófico y capacidad de preservación de miembros, incluso en isquemia crítica aterooclusiva. El efecto, tanto analgésico como trófico de las distintas modalidades analgésicas epidurales, varía según sus características técnicas y según los distintos tipos de isquemia periférica. Se deben tener en cuenta las limitaciones y riesgos del tratamiento analgésico epidural en la isquemia de miembros. Se necesitan estudios científicos que evalúen la eficiencia y la efectividad de la NEE en la isquemia periférica de naturaleza no aterooclusiva, así como la investigación de parámetros clínicos vasculares que puedan actuar como predictores de preservación de miembros con isquemia crítica en el período de prueba de la NEE.Peripheral arterial ischemia can result from various diseases that compromise limb vascularization, leading to pain, disability, and reduced quality of life; critical limb ischemia can cause substantial morbidity and mortality and chronic pain. The present article aims to provide a historical review of the scientific literature on the distinct types of peripheral ischemia, pain due to this