WorldWideScience
1

Quaternary ammonium salt derivatives of allylphenols with peripheral analgesic effect  

Scientific Electronic Library Online (English)

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).

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

2

Quaternary ammonium salt derivatives of allylphenols with peripheral analgesic effect  

Directory of Open Access Journals (Sweden)

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.

A. B de Oliveira

1991-01-01

3

Peripheral analgesic effects of ketamine in acute inflammatory pain.  

DEFF Research Database (Denmark)

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.

Pedersen, J L; Galle, T S

1998-01-01

4

The supraspinally mediated analgesic effects of zonisamide in mice after peripheral nerve injury are independent of the descending monoaminergic system.  

Science.gov (United States)

We have previously demonstrated that the antiepileptic drug zonisamide supraspinally generates analgesic effects on thermal and mechanical hypersensitivity in mice after peripheral nerve injury. To further establish the neurochemical basis for the supraspinally mediated analgesic action of zonisamide, we measured spinal noradrenaline (NA), 3-methoxy-4-hydroxyphenyleneglycol (MHPG), serotonin (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), and dopamine (DA) contents using HPLC with electrochemical detection in a murine neuropathic pain model that was prepared by partial ligation of the sciatic nerve (Seltzer model). Intraperitoneally or intracerebroventricularly administered zonisamide (50 mg/kg, i.p. and 30 mug, i.c.v., respectively), which almost completely reduced mechanical hypersensitivity, did not elicit any changes in spinal NA, MHPG, 5-HT, 5-HIAA, and DA contents. Moreover, the effectiveness of i.p. or i.c.v. administered zonisamide at reducing thermal and mechanical hypersensitivity was not influenced by intrathecally administered yohimbine (3 mug), an alpha(2)-adrenergic receptor antagonist. Thus, it appears that the supraspinally mediated analgesic effects of zonisamide are independent of the descending monoaminergic pain inhibitory system. PMID:17666864

Tanabe, Mitsuo; Takeuchi, Yuichi; Ono, Hideki

2007-08-01

5

Myrcene mimics the peripheral analgesic activity of lemongrass tea.  

Science.gov (United States)

Oral administration of an infusion of lemongrass (Cymbopogon citratus) fresh leaves to rats produced a dose-dependent analgesia for the hyperalgesia induced by subplantar injections of either carrageenin or prostaglandin E2, but did not affect that induced by dibutyryl cyclic AMP. These results indicate a peripheral site of action which was confirmed with the essential oil obtained by steam distillation of the leaves. Silica gel column fractionation of the essential oil allowed the identification of myrcene as the major analgesic component in the oil. Identification of the components was made by thin-layer chromatography and checked by mass spectrometry. The peripheral analgesic effect of myrcene was confirmed by testing a standard commercial preparation on the hyperalgesia induced by prostaglandin in the rat paw test and upon the contortions induced by intraperitoneal injections of iloprost in mice. In contrast to the central analgesic effect of morphine, myrcene did not cause tolerance on repeated injection in rats. This analgesic activity supports the use of lemongrass tea as a "sedative" in folk medicine. Terpenes such as myrcene may constitute a lead for the development of new peripheral analgesics with a profile of action different from that of the aspirin-like drugs. PMID:1753786

Lorenzetti, B B; Souza, G E; Sarti, S J; Santos Filho, D; Ferreira, S H

1991-08-01

6

Capsaicin 8 % as a cutaneous patch (Qutenza™): analgesic effect on patients with peripheral neuropathic pain.  

Science.gov (United States)

Evaluation of the analgesic effect after a single application of the capsaicin 8 % cutaneous patch (Qutenza™) in 37 patients suffering from painful, distal symmetric polyneuropathy (PNP) for an average of 5 years. Patients ranged from 40 to 78 years of age and 22 subjects were HIV-positive. Patients were observed 4 weeks prior to 12 weeks post administration. An evaluation of the therapeutic effect of capsaicin 8 % as a dermal patch in terms of pain reduction, change of sleeping behavior and social activities was performed and statistical analysis of data was conducted using non-parametric methods. Patients were selected according to clinical criteria. Numerical rating scale (NRS 0-10) was used to inquire pain intensity and a pain score was calculated using the painDETECT(©) questionnaire Freynhagen R (Curr Med Res Opin 22:1911-1920, [2006]). A significant reduction of pain was achieved for up to 12 weeks, with a maximum after 2-4 weeks post administration. After patient education and before application of capsaicin patch, a significant reduction of three levels on the NRS was observed. Symptoms of painful PNP decreased over the period of investigation and 8 patients reported a reduction of systemic pain medication. In patients with an HIV infection, a significant extension of sleep was achieved for 2, 4 and 8 weeks after application. Thus, the application of the capsaicin 8 % patch resulted in a significant relief of neuropathic pain, a prolongation of sleep, a reduction of oral pain medication and a resumption of social activities. PMID:25421590

Raber, Julia Marie; Reichelt, Doris; Grüneberg-Oelker, Ute; Philipp, Konstanze; Stubbe-Dräger, Bianca; Husstedt, Ingo-W

2014-11-25

7

The analgesic effect of decursinol.  

Science.gov (United States)

Although decursinol, which is one of the coumarins purified from the dried roots of Angelica gigas Nakai, was previously demonstrated to have antinociceptive effects on various mouse pain models such as tail-flick, hot-plate, formalin, writhing, and several cytokine-induced pain tests, the possible involvement of its analgesic effects and non-steroidal anti-inflammatory drugs (NSAIDs) has not been clearly elucidated yet. In this study, we characterized the possible interaction between decursinol and aspirin or acetaminophen in the writhing test. The antinociceptive effects of decursinol were observed at an orally-administered dose of 50 mg/kg but not at 25 or 10 mg/kg. In addition, the analgesic effects of aspirin (ASA) and acetaminophen (APAP) were shown at an orally-administered dose of 200 mg/kg but not at 50 or 100 mg/kg. We examined the effects of decursinol on the ASA or APAP at sub-analgesic doses. Although the co-administration of decursinol and ASA did not show any differences at doses of 10 or 25 mg/kg and 50 or 100 mg/kg, respectively, synergistic effects between decursinol and APAP were observed in the group of decursinol (25 mg/kg) and APAP (100 mg/kg) co-administration. These results indicated that the analgesic effect of decursinol might be involved in supraspinal cyclooxygenase regulation that might be overlapped with APAP-induced analgesic mechanisms rather than systemic or peripheral prostaglandin modulation. PMID:19557373

Seo, Young-Jun; Kwon, Min-Soo; Park, Soo-Hyun; Sim, Yun-Beom; Choi, Seung-Min; Huh, Gyung-He; Lee, Jin-Koo; Suh, Hong-Won

2009-06-01

8

Effects of peripherally and centrally acting analgesics on somato-sensory evoked potentials.  

OpenAIRE

1. The effects of aspirin 1000 mg, paracetamol 1000 mg, codeine 60 mg on somatosensory evoked potentials (SEPs) were measured in a four-way cross-over study. 2. SEPs were elicited by electrical stimulation of the skin overlying the digital nerve at intensities close to pain threshold. 3. Amplitudes and latencies of both early and late SEPs were recorded, as well as first sensory threshold and subjective pain threshold. 4. None of the study medications affected the amplitude or latency of the ...

Moore, U. J.; Marsh, V. R.; Ashton, C. H.; Seymour, R. A.

1995-01-01

9

Analgesic effects of antihistaminics.  

Science.gov (United States)

The literature provides considerable evidence indicating that several, but not all antihistaminics, are indeed analgesic agents and some are analgesic adjuvants as well. Those for which effectiveness is reported includes diphenhydramine, hydroxyzine, orphenadrine, pyrilamine, phenyltoloxamine, promethazine, methdilazine, and tripelennamine. The proposed mechanisms of analgesic action of antihistaminics are reviewed and discussed. The literature suggests that more than one mechanism of action exists for them. There is considerable evidence suggesting that histaminergic and serotoninergic central pathways are involved in nociception and that antihistaminic drugs can modulate their responses (1). The evidence for a role for norepinephrine and dopamine and the effects of antihistaminics on them are less well established. Still other pathways have been proposed. A greater understanding of pain mechanisms will aid in elucidating the role of antihistaminics in analgesia. PMID:2578597

Rumore, M M; Schlichting, D A

1985-02-01

10

Long-lasting oral analgesic effects of N-protected aminophosphinic dual ENKephalinase inhibitors (DENKIs) in peripherally controlled pain  

Science.gov (United States)

The peripheral endogenous opioid system is critically involved in neuropathic and inflammatory pain generation as suggested by the modulation of opioid receptors expression and enkephalins (ENKs) release observed in these painful conditions. Accordingly, an innovative approach in the treatment of these nocifensive events is to increase and maintain high local concentrations of extracellular pain-evoked ENKs, by preventing their physiological enzymatic inactivation by two Zn metallopeptidases, the neutral endopeptidase (NEP, neprilysin, EC 3.4.24.11) and the neutral aminopeptidase (APN, EC 3.4.11.2). With this aim, new orally active dual ENKephalinase inhibitors (DENKIs) were designed as soluble prodrugs by introducing a N-terminal cleavable carbamate in the previously described aminophosphinic inhibitors. This induces long-lasting antinociceptive responses after oral administration, in various rodent models of inflammatory and neuropathic pain. These responses are mediated through stimulation of peripheral opioid receptors by DENKIs-protected ENKs as demonstrated by naloxone methiodide reversion. In all tested models, the most efficient prodrug 2a (PL265) was active, at least during 150–180 min, after single oral administration of 25–50 mg/kg in mice and of 100–200 mg/kg in rats. In models of neuropathic pain, both hyperalgesia and allodynia were markedly reduced. Interestingly, combination of inactive doses of 2a (PL265) and of the anti-epileptic drug gabapentin had synergistic effect on neuropathic pain. Pharmacokinetic studies of 2a (PL265) in rats show that the active drug is the only generated metabolite produced. These encouraging results have made 2a (PL265) a suitable candidate for clinical development.

Bonnard, Elisabeth; Poras, Hervé; Nadal, Xavier; Maldonado, Rafael; Fournié-Zaluski, Marie-Claude; Roques, Bernard P

2015-01-01

11

Evaluation of the analgesic efficacy and psychoactive effects of AZD1940, a novel peripherally acting cannabinoid agonist, in human capsaicin-induced pain and hyperalgesia.  

Science.gov (United States)

The aim of the present study was to investigate the effects of AZD1940, a novel peripherally acting cannabinoid CB(1) /CB(2) receptor agonist, on capsaicin-induced pain and hyperalgesia, as well as on biomarkers of cannabinoid central nervous system (CNS) effects. The present study was a randomized, double-blind, placebo-controlled, four-sequence, two-period, cross-over study in 44 male healthy volunteers aged 20-45 years. The effects of two single oral doses of AZD1940 (400 and 800 ?g) were compared with placebo. Pain intensity after intradermal capsaicin injections in the forearm was assessed on a continuous visual analogue scale (VAS; 0-100 mm). Primary and secondary hyperalgesia induced by application of capsaicin cream on the calf were assessed by measuring heat pain thresholds and the area of mechanical allodynia, respectively. The CNS effects were assessed at baseline and up to 24 h after dosing using a visual analogue mood scales (VAMS) for feeling 'stimulated', 'high', 'anxious', 'sedated' or 'down'. AZD1940 did not significantly attenuate ongoing pain or primary or secondary hyperalgesia compared with placebo. Mild CNS effects for AZD1940were observed on the VAMS for 'high' and 'sedated'. Dose-dependent mild-to-moderate CNS-related and gastrointestinal adverse events were reported following treatment with AZD1940. No evidence of analgesic efficacy was found for a peripherally acting CB(1)/CB(2) receptor agonist in the human capsaicin pain model. The emergence of mild dose-dependent CNS effects suggests that the dose range predicted from preclinical data had been attained. PMID:23324098

Kalliomäki, Jarkko; Annas, Peter; Huizar, Karin; Clarke, Cyril; Zettergren, Annika; Karlsten, Rolf; Segerdahl, Märta

2013-03-01

12

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

Science.gov (United States)

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

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

13

The selective neuronal nitric oxide synthase inhibitor 7-nitroindazole has acute analgesic but not cumulative effects in a rat model of peripheral neuropathy  

Directory of Open Access Journals (Sweden)

Full Text Available Liliane J Dableh, James L HenryDepartment of Psychiatry and Behavioural Neurosciences, McMaster University, Hamilton, Ontario, CanadaAbstract: Chronic neuropathic pain that may arise from various nerve injuries or insults remains notoriously difficult to manage. The neuronal isoform of the enzyme nitric oxide synthase (nNOS has been shown to be involved in the spinal transmission of nociception in animal models of chronic pain. The aim of this study is to evaluate the effect of single dose and repeated administration of a selective nNOS inhibitor. Rats were unilaterally implanted with a 2-mm polyethylene cuff around the sciatic nerve. Paw withdrawal thresholds were measured using von Frey filament stimulation. Rats were given 10, 20, or 30 mg/kg of 7-nitroindazole (7-NI, or vehicle, on days 2, 5, and 7 after model induction, respectively. Paw withdrawal thresholds were measured before and at 30 and 60 min after injection. 7-NI significantly increased paw withdrawal thresholds at 60 min at the 20 and 30 mg/kg dosages. In the second part of this study, rats were given 20 mg/kg 7-NI daily for five days starting immediately after cuff implantation (days 0 to 4, and the cuff was removed on day 4. Withdrawal thresholds were measured intermittently over a 24-day observation period. No differences in withdrawal thresholds were observed between drug and vehicle-treated rats. Therefore, early and repeated administration of 7-NI did not affect the development or progression of the model. In conclusion, inhibition of nNOS had an analgesic but not a pre-emptive effect in this model of peripheral neuropathic pain.Keywords: neuronal nitric oxide synthase, nitric oxide, 7-nitroindazole, neuropathic pain, peripheral nerve injury, nociception 

Henry JL

2011-03-01

14

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

DEFF Research Database (Denmark)

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.

Dong, Xu-Dong; Svensson, Peter

2009-01-01

15

Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats.  

Science.gov (United States)

The peptide neurotransmitter N-acetylaspartylglutamate (NAAG) selectively activates group II metabotropic glutamate receptors (mGluRs). Systemic administration of inhibitors of the enzymes that inactivate NAAG results in decreased pain responses in rat models of inflammatory and neuropathic pain. These effects are blocked by a group II mGluR antagonist. This research tested the hypothesis that some analgesic effects of NAAG peptidase inhibition are mediated by NAAG acting on sensory neurite mGluRs at the site of inflammation. Group II mGluR agonists, SLx-3095-1, NAAG and APDC, or NAAG peptidase inhibitors, ZJ-43 and 2-PMPA, injected into the rat footpad reduced pain responses in carrageenan or formalin models. The analgesic effects of SLx-3095-1, APDC, ZJ-43, 2-PMPA and NAAG were blocked by co-injection of LY341495, a selective group II mGluR antagonist. Injection of group II mGluR agonists, NAAG or the peptidase inhibitors into the contralateral rat footpad had no effect on pain perception in the injected paw. At 10-100 microm ZJ-43 and 2-PMPA demonstrated no consistent agonist activity at mGluR2 or mGluR3. Consistent with the conclusion that peripherally administered NAAG peptidase inhibitors increase the activation of mGluR3 by NAAG that is released from peripheral sensory neurites, we found that the tissue average concentration of NAAG in the unstimulated rat hind paw was about 6 microm. These data extend our understanding of the role of this peptide in sensory neurons and reveal the potential for treatment of inflammatory pain via local application of NAAG peptidase inhibitors at doses that may have little or no central nervous system effects. PMID:17241276

Yamamoto, Tatsuo; Saito, Osamu; Aoe, Tomohiko; Bartolozzi, Alessandra; Sarva, Jayaprakash; Zhou, Jia; Kozikowski, Alan; Wroblewska, Barbara; Bzdega, Tomasz; Neale, Joseph H

2007-01-01

16

EVALUATION OF CENTRAL AND PERIPHERAL ANALGESIC ACTIVITY OF WHOLE PLANT GOMPHRENA GLOBOSA (L (FAMILY: AMARANTHACEAE  

Directory of Open Access Journals (Sweden)

Full Text Available Gmophrena globosa (L including in Amaranthaceae family is an important medicinal plant in our country, especially in hilly tribal people for their folk medicinal practices. The object of my study was to investigate the central and peripheral analgesic activity of the investigated plant based on the use of Gmophrena globosa extract for the wound healing to the tribal people in our country. After collection of whole plant it was first of all washed and then sun dried and made powder by grinding machine. The powder was extracted by methanol. Around 5gm of concentrated methanolic plant extract was partitioned by modified Kupchan partitioning protocol into n-hexane soluble fraction, carbon tetrachloride soluble fraction, chloroform soluble fraction and aqueous soluble fraction. All the fractions were subjected to the investigation of central and peripheral analgesic activity. Among all the fractions crude methanolic extract, n-hexane soluble fraction and aqueous soluble fraction at a dose of 400mg/kg had shown significant analgesic activity. They produced an inhibition of writhing 74.6%, 71.4% and 74.5% respectively in comparable with positive control diclofenac. On the other hand central analgesic activity of the test samples were compared with Morphine. The crude methanolic extract and n-hexane soluble fraction have significant central analgesic activity at 400mg/kg dose. The central analgesic activity is highest after 30minutes. As the time progress the analgesic activity decreases. After 60minutes there is almost no central analgesic activity in the plant extracts.

Hamiduzzaman Md.

2013-06-01

17

Analgesic effects of dexamethasone in burn injury.  

DEFF Research Database (Denmark)

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.

Werner, Mads U; Lassen, Birgit Vibeke

2002-01-01

18

EVALUATION OF CENTRAL AND PERIPHERAL ANALGESIC ACTIVITY OF WHOLE PLANT GOMPHRENA GLOBOSA (L) (FAMILY: AMARANTHACEAE)  

OpenAIRE

Gmophrena globosa (L) including in Amaranthaceae family is an important medicinal plant in our country, especially in hilly tribal people for their folk medicinal practices. The object of my study was to investigate the central and peripheral analgesic activity of the investigated plant based on the use of Gmophrena globosa extract for the wound healing to the tribal people in our country. After collection of whole plant it was first of all washed and then sun dried and made powder by grindin...

Hamiduzzaman Md.

2013-01-01

19

Catastrophizing delays the analgesic effect of distraction  

OpenAIRE

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...

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

2010-01-01

20

Analgesic effect of the aqueous and ethanolic extracts of clove  

OpenAIRE

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...

Mina Kamkar Asl; Ashraf Nazariborun; Mahmoud Hosseini

2013-01-01

21

Effects of melatonin on peripheral nerve regeneration.  

Science.gov (United States)

In the available literature, there are thousands of studies on peripheral nerve regeneration using many nerves of several animals at different ages with various types of lesions and different methods of evaluation at certain time of follow-up. Despite many experimental data and clinical observations, there is still no ideal treatment method enhancing peripheral nerve regeneration. In clinical practice, various types of surgical nerve repair techniques do not frequently result in complete recovery due to neuroma formation, lipid peroxidative damage, ischemia and other factors. Recently, a number of neuroscientists demonstrated that pineal neurohormone melatonin (MLT) has an effect on the morphologic features of the nerve tissue, suggesting its neuroprotective, free radical scavenging, antioxidative, and analgesic effects in degenerative diseases of peripheral nerves. At present, it is widely accepted that MLT has a useful effect on axon length and sprouting after traumatic events to peripheral nerves. Our studies using various experimental injury models clearly suggest positive effects of MLT on the number of axons, thickness of myelin sheath by inhibition of collagen accumulation and neuroma formation following traumatic events to peripheral nerves, myelination of developing peripheral nerve after intrauterine ethanol exposure. Nevertheless, further experimental and randomized controlled clinical studies are vital to identify the clinical use of MLT hormone. This is an overview of recent patents and current literature in terms of the effects of MLT on peripheral nerve regeneration based on a critical analysis of electrophysiological, biochemical and light and electron microscopic findings, in addition to functional observations. PMID:22074585

Turgut, Mehmet; Kaplan, Süleyman

2011-05-01

22

Analgesic, antipyretic, anti-inflammatory and toxic effects of andrographolide derivatives in experimental animals.  

Science.gov (United States)

Andrographolide (1) and 14-deoxy-11,12-didehydroandrographolide (2) are active constituents of Andrographis paniculata (Burm. f.), family Acanthaceae. A. paniculata extracts are reported to have antiviral, antipyretic, immunostimulant and anticancer activities. In this study, 1 and its 14-acetyl- (4) and 3,19-isopropylidenyl- (3) derivatives, as well as 2 and its 3,19-dipalmitoyl-derivative (5), were intraperitoneally tested for their analgesic, antipyretic, anti-inflammatory and acute toxicity effects in animal models. Analgesic effects were tested in mice using hot plate and writhing tests to distinguish the central and peripheral effects, respectively. The results showed that, at 4 mg/kg, all tested substances have significant analgesic effects, and the highest potency was seen with 3, 4 and 5. Increasing the dose of 3 and 5 to 8 mg/kg did not increase the analgesic effect. In the writhing test, 3 and 5, but not 1, showed significant results. In a baker's yeast-induced fever model, 3 and 5 significantly reduced rats' rectal temperature (p < 0.05). In a carrageenan-induced inflammation model, 1, 3 and 5 significantly reduced rats' paw volume. Doses of 3 and 5 up to 100 mg/kg did not show any serious toxic effects. From this study, 3 and 5 are the most interesting derivatives, showing much greater potency than their parent compounds. These could be further developed as analgesic, antipyretic and anti-inflammatory agents, without any serious toxicity. PMID:19784573

Suebsasana, Supawadee; Pongnaratorn, Panicha; Sattayasai, Jintana; Arkaravichien, Tarinee; Tiamkao, Siriporn; Aromdee, Chantana

2009-09-01

23

Catastrophizing delays the analgesic effect of distraction.  

Science.gov (United States)

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

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

2010-05-01

24

Analgesic effect of Irvingia gabonensis stem bark extract.  

Science.gov (United States)

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

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

1995-02-01

25

Analgesic and neuropharmacological effects of Xanthium indicum leaves  

OpenAIRE

The present study investigated analgesic and some neuropharmacological effects of hydromethanolic extract of the leaves of Xanthium indicum Koenig in mice models. The analgesic activity was evaluated using hot plate ant tail immersion methods, and acetic acid-induced writhing test. The neuropharmacological effects were determined using hole-cross, open field, and thiopental-induced sleeping time tests. The extract, at the doses of 100, 200 and 400 mg/kg, produced a dose dependent and signific...

Akter, Raushanara; Hasan, Raquibul; Hossain, Mokarram; Jamila, Mariam; Mazumder, Mohammed Ehsanul H.; Rana, Sohel; Rahman, Shafiqur

2010-01-01

26

Analgesic and antiinflammatory effects of some 2-mercaptobenzoxazole derivatives.  

Science.gov (United States)

Analgesic and antiinflammatory effects of benzoxazole derivatives have been investigated in mice. In the acetic acid induced writhing test, the analgesic effect of two compounds were found to be stronger than that of diclofenac sodium. In the formaldehyde induced paw swelling edema test, two compounds were found to be more active than diclofenac sodium, another two were as potent as the control drug. PMID:8900870

Safak, C; Simsek, R; Erol, K; Vural, K

1996-03-01

27

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

Science.gov (United States)

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

Wang, Q; Xu, G; Jiang, Y

1990-02-01

28

The effectiveness of analgesics in traumatic injuries of the extremities.  

Science.gov (United States)

In this study, the effectiveness of different analgesics was investigated in patients who presented to the emergency room with traumatic injuries or fractures of the extremities. We observed 100 patients (42 male, 58 female) who presented to the Konya State Hospital emergency service with isolated traumatic injuries of the extremities. We used different analgesics intravenously or intramuscularly in those patients with a high or moderate level of pain according to a visual analog pain scale. Patient pain levels were assessed 15, 30, and 45 minutes after administration of the analgesics. Metamizole sodium 1 g IV was used in 36 patients and diclofenac sodium 75 mg IM was given to 40 patients; tramadol hydrochloride 100 mg IV was administered to 24 patients. Pain became less severe after 15 minutes in 92% of patients who received tramadol IV; pain became less severe after 30 minutes in 72% of those who received metamizole IV. In contrast, pain became less severe after 45 minutes in 65% of patients who received diclofenac IM. Tramadol was the most effective analgesic and was also more effective earlier than the other analgesics tested. PMID:16418155

Cander, Basar; Girisgin, Sadik; Koylu, Ramazan; Gul, Mehmet; Koçak, Sedat

2005-01-01

29

Analgesic effect of the aqueous and ethanolic extracts of clove  

Directory of Open Access Journals (Sweden)

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.

Mina Kamkar Asl

2013-03-01

30

[Analgesic effects of lornoxicam in formalin-induced inflammation].  

Science.gov (United States)

Peroral administration of lornoxicam, a new representative of the class of oxicams, in a total dose of 2-16 mg/kg produced a dose-dependent analgesic effect in rats with formalin-induced tail inflammation, as confirmed by the tail-flick and hot-plate tests. The maximum analgesic effect of lornoxicam during the formalin-induced edema development was observed upon a three-fold drug administration by the scheme 1/2, 1/4, 1/4 of the total dose (8-16 mg/kg, p.o.) with a 3 h interval prior to formalin injection into the rat tail base. Validity of using the tail-flick and hot-plate methods for evaluation of the analgesic effect of NSAID is discussed. PMID:11544800

Marusov, I V; Marusova, I B; Pchelintsev, M V

2001-01-01

31

Analgesic effect of clove essential oil in mice  

OpenAIRE

Objective: Results obtained from literature reviews and human studies have shown the analgesic effects of clove plant in toothache. The present work was undertaken in order to investigate the possible analgesic effect of clove oil in mice.Materials and Methods: Fifty mice were divided into 5 groups: 1) Saline; 2) Essential oil (Ess) 2%, 3) Ess 5%, 4) Ess10% and 5) Ess 20%. The hot plate test (55±0.2 °C; Cut-off 60 sec) was performed as a base record 15 min before injection of drugs (Saline ...

Mahmoud Hosseini; Mina Kamkar Asl; Hassan Rakhshandeh

2011-01-01

32

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

Science.gov (United States)

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

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

2015-01-01

33

The analgesic and anticonvulsant effects of piperine in mice.  

Science.gov (United States)

Piperine, is the major active principal of black pepper. In traditional medicine, black pepper has been used as an analgesic, anti-inflammatory agent and in the treatment of epilepsy. This study was conducted to evaluate the in vivo analgesic and anticonvulsant effects of piperine in mice. The analgesic and anticonvulsant effects of piperine were studied in mice using acetic acid-induced writhing, tail flick assay, pentylenetetrazole (PTZ)- and picrotoxin (PIC)-induced seizures models. The intraperitoneal (i.p.) administration of piperine (30, 50 and 70 mg/kg) significantly inhibited (Ppiperine (30 and 50 mg/kg, i.p.) and morphine (5 mg/kg, i.p.) caused a significant increase (Ppiperine and morphine in the tail flick assay. Piperine (30, 50 and 70 mg/kg, i.p.) and standard drugs, valproic acid (200 mg/kg, i.p.), carbamazepine (30 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.) significantly (Ppiperine exhibits analgesic and anticonvulsant effects possibly mediated via opioid and GABA-ergic pathways respectively. Moreover, piperine being the main constituent of black pepper, may be contributing factor in the medicinal uses of black pepper in pain and epilepsy. PMID:24388894

Bukhari, I A; Pivac, N; Alhumayyd, M S; Mahesar, A L; Gilani, A H

2013-12-01

34

Synthesis and analgesic effects of novel ?2-tryptophan hexapeptide analogs.  

Science.gov (United States)

Aiming to develop more potent analgesic substances a new series of hexapeptides containing ?(2)-tryptophan analogues was synthesized. The Trp in position 4 and 5, respectively in Ac-Arg-Phe-Met-Trp-Met-Lys-NH2 (opioid receptor antagonist) and Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH2 (highly potent and selective NOP-receptor agonist) was substituted by the (S)-2-(1-methyl-1H-indol-3-yl)propionic residue or the (S)-2-(5-methoxy-1H-indol-3-yl)propionic residue. The analgesic effect of the four newly synthesized compounds has been evaluated in male Wistar rats by PP- and HP tests and compared to the native templates. Further estimation of the mechanisms of action of each compound was achieved using specific antagonists-naloxone for opioid and JTC801 for the NOP receptor. Replacement of Trp with ?(2)-tryptophan analogues in 4th position (Ac-Arg-Phe-Met-Trp-Met-Lys-NH2) led to increased and longer lasting analgesic effect. The results obtained permit us to assume that both opioid and NOP receptors take part in the newly synthesized compounds analgesic effects. PMID:23851698

Bocheva, Adriana; Nocheva, Hristina; Pavlov, Nikola; Todorov, Petar; Calmès, Monique; Martinez, Jean; Naydenova, Emilia

2013-10-01

35

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

Science.gov (United States)

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

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

2007-03-21

36

Putative physiological mechanisms underlying tDCS analgesic effects.  

Science.gov (United States)

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 analgesic effects in experimental settings, as well as in post-operative acute pain and chronic pain syndromes. The promising evidence of tDCS-induced analgesic effects raises the challenging and complex question of potential physiologic mechanisms that underlie/mediate the accomplished pain relief. Here we present hypotheses on how the specific montages and targets for stimulation may affect the pain processing network. PMID:24133434

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

2013-01-01

37

Mood-elevating effects of opioid analgesics in patients with bipolar disorder.  

Science.gov (United States)

Opioids can have mood-elevating effects in healthy subjects and have been used successfully to treat refractory depressed patients. A few case reports indicate that opioid analgesics can induce mania. The authors investigated the mood reaction of opioid analgesics in patients with bipolar disorder. Nine (27%) of 33 patients who took opioid analgesics for medical reasons experienced a significant hypomanic/manic reaction, and two other patients reported an antidepressant effect. None of the comparison subjects reported a significant mood reaction from opioid analgesics. These results indicate that opioid analgesics can have an important mood-altering effect on patients with known bipolar disorder. PMID:18070849

Schaffer, Charles B; Nordahl, Thomas E; Schaffer, Linda C; Howe, Jeanne

2007-01-01

38

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

Directory of Open Access Journals (Sweden)

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

Chandra Shekar

2012-09-01

39

Abuse and paradoxical effects of analgesic drug mixtures  

OpenAIRE

1 In patients with chronic pain, two types of analgesic drug dependence occur, that is, dependence of the barbiturate-type and of the morphine-type. Eighty cases of analgesic drug dependence of the barbiturate-type were examined. All these patients were dependent on drug combinations, not a single patient being on one analgesic alone.

Wo?rz, Roland

1980-01-01

40

Evaluation of analgesic effect of Datura fastuosa leaves and seed extracts.  

Science.gov (United States)

The aqueous extracts of Datura fastuosa leaves and seeds were evaluated for the analgesic effect on acetic acid-induced writhing and hot plate reaction in mice. According to the results, D. fastuosa leaves and seeds extracts at oral doses of 400 and 800 mg/kg are effective as analgesic. The analgesic activity of leaf extract is reduced by naloxone but not that of seed extract. PMID:12837368

Abena, A A; Miguel, L M; Mouanga, A; Hondi Assah, Th; Diatewa, M

2003-07-01

41

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

Science.gov (United States)

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.

Sagiroglu, Gonul

2011-01-01

42

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

Directory of Open Access Journals (Sweden)

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.

Gonul Sagiroglu

2011-04-01

43

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

Science.gov (United States)

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

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

2015-02-01

44

Down-regulation of NR2B receptors partially contributes to analgesic effects of Gentiopicroside in persistent inflammatory pain.  

Science.gov (United States)

Gentiopicroside is one of the secoiridoid compound isolated from Gentiana lutea. It exhibits analgesic activities in the mice. The anterior cingulate cortex (ACC) is a forebrain structure known for its roles in pain transmission and modulation. Painful stimuli potentiate the prefrontal synaptic transmission and induce glutamate NMDA NR2B receptor expression in the ACC. But little is known about Gentiopicroside on the persistent inflammatory pain and chronic pain-induced synaptic transmission changes in the ACC. The present study was undertaken to investigate its analgesic activities and central synaptic modulation to the peripheral painful inflammation. Gentiopicroside produced significant analgesic effects against persistent inflammatory pain stimuli in mice. Systemic administration of Gentiopicroside significantly reversed NR2B over-expression during the chronic phases of persistent inflammation caused by hind-paw administration of complete Freunds adjuvant (CFA) in mice. Whole-cell patch clamp recordings revealed that Gentiopicroside significantly reduced NR2B receptors mediated postsynaptic currents in the ACC. Our findings provide strong evidence that analgesic effects of Gentiopicroside involve down-regulation of NR2B receptors in the ACC to persistent inflammatory pain. PMID:18410946

Chen, Lei; Liu, Jin-cheng; Zhang, Xiao-nan; Guo, Yan-yan; Xu, Zhao-hui; Cao, Wei; Sun, Xiao-li; Sun, Wen-ji; Zhao, Ming-Gao

2008-06-01

45

Analgesic effect of Lepidium sativum Linn. (Chandrashura) in experimental animals.  

Science.gov (United States)

Lepidium sativum Linn, which is known as "Aselio" locally, is frequently used by the villagers for the treatment of Sandhivata (osteoarthritis), with good therapeutic relief. Here, we have to observe the analgesic activity of the seed of Lepidium sativum Linn in albino rats and Swiss albino mice with different parameters. The analgesic study was performed with acetic acid-induced writhing response in mice, formaldehyde-induced paw licking response in rats and tail flick response in mice. Experiments were carried out in two groups - therapeutic dose group and double dose group - with comparison with the control group. In the acetic acid-induced writhing syndrome, latency of onset was highly significantly increased in the therapeutic dose group and significant increase was found in the double dose group. In the formaldehyde-induced paw licking response, the test drug produced significant inhibition of neurogenic pain in the double dose group and significant inhibition of inflammatory pain in the therapeutic dose group. In the tail flick response, the test drug produced a mild to moderate effect in the therapeutic dose group and also in the double dose group. PMID:22131742

Raval, Nita D; Ravishankar, B

2010-07-01

46

Comparative analgesic effect of Ligusticum chuanxiong pieces and its products in mice.  

Science.gov (United States)

The present study was undertaken with the objective of finding out the comparative analgesic effect of Ligusticum chuanxiong (LC) pieces decoction, LC formula granule decoction, liquored LC pieces decoction and liquored LC formula granule decoction. The analgesic effects were analyzed using the hot plate and acetic-induced writhing test in mice, and antidysmenorrheic effect was observed with primary dysmenorrhea model. The results showed that four kinds of LC decoction had definite effect in delaying incubation period and decreasing the writhing frequency within 30 min. They also effectively relieved dysmenorrhea. Moreover, liquored LC had better analgesic effect than crude LC in four decoctions. PMID:20668580

Gao, Demin; Xu, Lingchuan

2010-04-01

47

Comparative analgesic effect of Ligusticum chuanxiong pieces and its products in mice  

Directory of Open Access Journals (Sweden)

Full Text Available The present study was undertaken with the objective of finding out the comparative analgesic effect of Ligusticum chuanxiong (LC pieces decoction, LC formula granule decoction, liquored LC pieces decoction and liquored LC formula granule decoction. The analgesic effects were analyzed using the hot plate and acetic-induced writhing test in mice, and antidysmenorrheic effect was observed with primary dysmenorrhea model. The results showed that four kinds of LC decoction had definite effect in delaying incubation period and decreasing the writhing frequency within 30 min. They also effectively relieved dysmenorrhea. Moreover, liquored LC had better analgesic effect than crude LC in four decoctions.

GAO Demin

2010-04-01

48

Pure analgesics in a rheumatological outpatient clinic  

Directory of Open Access Journals (Sweden)

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.

M.A. Cimmino

2011-09-01

49

Analgesic effect of Lepidium sativum Linn. (Chandrashura) in experimental animals  

OpenAIRE

Lepidium sativum Linn, which is known as “Aselio” locally, is frequently used by the villagers for the treatment of Sandhivata (osteoarthritis), with good therapeutic relief. Here, we have to observe the analgesic activity of the seed of Lepidium sativum Linn in albino rats and Swiss albino mice with different parameters. The analgesic study was performed with acetic acid-induced writhing response in mice, formaldehyde-induced paw licking response in rats and tail flick response in mice. ...

Raval, Nita D.; Ravishankar, B.

2010-01-01

50

Anticonvulsant and Analgesic Effects of Harpephyllum caffrum Bernh. ex C.F. Krauss [Anacardiaceae] Stem-Bark Aqueous Extract in Mice  

Directory of Open Access Journals (Sweden)

Full Text Available This study was undertaken to evaluate the anticonvulsant and analgesic effects of Harpephyllum caffrum stem-bark aqueous extract (HCE in mice. The anticonvulsant effect of the plant’s stem-bark extract (HCE, 50-800 mg kg-1 intraperitoneally was examined against pentylenetetrazole (PTZ- and picrotoxin (PCT- induced seizures, while the analgesic effect of the extract (HCE, 50-800 mg kg-1 I. p. was evaluated by hot-plate and acetic acid analgesic test methods. H. caffrum stem-bark extract (HCE, 100-800 mg kg-1 I. p. dose-dependently and significantly delayed (p<0.05-0.001 the onset of the seizures and profoundly antagonized, PTZ- and PCT-induced seizures. Moreover, HCE (50-800 mg kg-1 I. p. produced dose-dependent, significant analgesic effects (p<0.05-0.001 against thermally and chemically-induced nociceptive pain in mice. The findings of the present study appear to suggest that H. caffrum stem-bark aqueous extract produces its anticonvulsant effect by enhancing GABAergic neurotransmission and/or action in the brain. The results also seem to suggest that H. caffrum stem-bark extract possesses centrally- and peripherally-mediated analgesic properties. Although the precise mechanisms of the anticonvulsant and analgesic actions of HCE could not be established, the findings of this laboratory animal study indicate that H. caffrum stem-bark aqueous extract possesses anticonvulsant and analgesic properties. These findings lend pharmacological credence to the suggested folkloric, ethnomedical uses of the plant as a natural supplementary remedy in the management or control of childhood convulsions and epilepsy, as well as in the treatment or management of painful conditions in some rural communities of South Africa.

John A.O. Ojewole

2007-01-01

51

Comparative analgesic effect of Ligusticum chuanxiong pieces and its products in mice  

OpenAIRE

The present study was undertaken with the objective of finding out the comparative analgesic effect of Ligusticum chuanxiong (LC) pieces decoction, LC formula granule decoction, liquored LC pieces decoction and liquored LC formula granule decoction. The analgesic effects were analyzed using the hot plate and acetic-induced writhing test in mice, and antidysmenorrheic effect was observed with primary dysmenorrhea model. The results showed that four kinds of LC decoction had definite effect in ...

Gao, Demin; Xu, Lingchuan

2010-01-01

52

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

OpenAIRE

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.

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

2009-01-01

53

The effect of whole body irradiation on the action of strong analgesics of mice  

International Nuclear Information System (INIS)

The effect of whole body irradiation of male mice with single doses of 3 and 7 Gy (60Co source) on analgesic action of three morphine-like drugs was studied. Over the first 6 days after irradiation, the analgesic effect of alfentanil and fentanyl was significantly less pronounced in irradiated animals than in control ones. During the subsequent period of 24 days till the end of experiment, the analgesic effect in irradiated animals gradually increased reaching and exceeding the control values. On the contrary, the analgesic effect of butorphanole was less pronounced in irradiated animals than in control ones, although the difference was not significantly. The difference between butorphanole and other two drugs are probably due to chemical structure and the metabolic fate in the body. (author) 8 refs.; 2 figs

54

Analgesic activity of 5-HT3 receptor antagonists.  

Science.gov (United States)

The effects of 5-HT3 receptor antagonists tropisetron and condensed derivative of benzimidazole (laboratory code 64B) on nociceptive threshold were examined on models with activation of peripheral and central nociceptive mechanisms. The examined substances demonstrated pronounced analgesic effects in peripheral pain. PMID:16027871

Spasov, A A; Chernikov, M V; Kiabiya, S T

2005-04-01

55

Anti-Inflammatory, Analgesic and Antipyretic Effects of Lepidagathis Anobrya Nees (Acanthaceae)  

OpenAIRE

This study investigated the general acute, anti-inflammatory, analgesic and antipyretic effects of methanol extract of Lepidagathis anobrya Nees (Acanthaceae). Carrageenan-induced rat paw edema and croton oil-induced ear edema in rats were used for the evaluation of general acute anti-inflammatory effects. Acetic acid-induced writhing response and yeast-induced hyperpyrexia in mice were used to evaluate the analgesic and antipyretic activities respectively. The extract at doses of 10, 25, 50 ...

Richard, Sawadogo Wamtinga; Marius, Lompo; Noya, Some?; Innocent Pierre, Guissou; Germaine, Nacoulma-ouedraogo Odile

2011-01-01

56

EVALUATION OF ANTI-INFLAMMATORY ACTIVITY AND ANALGESIC EFFECT OF ALOE VERA LEAF EXTRACT IN RATS  

OpenAIRE

Clinical evaluation of analgesic and anti-inflammatory drugs envisages the development of side effects that makes efficacy of a drug arguable. Alternatively, indigenous drug with fewer side effects is the major thrust area of research in the management of pain and inflammation. In the present study aqueous extract of whole leaf of Aloe vera at various concentrations was investigated for its anti-inflammatory and analgesic activities in albino wistar rats. Carrageenan and formaldehyde-induced ...

Aruna Devaraj; Thirunethiran Karpagam

2011-01-01

57

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

Directory of Open Access Journals (Sweden)

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.

Ardeshir Arzi

2013-01-01

58

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

Directory of Open Access Journals (Sweden)

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.

Romaric De Garde Elion Itou

2014-11-01

59

[The postoperative analgesic effects of magnesium infusion on brachial plexus block].  

Science.gov (United States)

Magnesium sulphate infusion decreases analgesic requirements after general anesthesia. Aim of this study was to assess the effects of postoperative magnesium infusion for 24 hours on duration of the block, sedation and postoperative analgesic consumption after brachial plexus block. After obtaining approval from local ethic committee, 70 ASA class I and II patients were included to the randomised double blind study. Brachial plexus block was performed using axillary approach with lignocaine 1.25% adrenaline 1/200 000 40 ml. Groups received 5 mg/kg bolus and 500 mg/h magnesium sulphate infusion or saline controls at the same volume during 24 hour. Analgesia and sedation were assessed while determining time to first pain and rescue analgesic, time to regain motor capability, visual analogue scale and sedation scores for every 4 hour during postoperative 24 h. period. While time to first pain and rescue analgesic was increased, total analgesic consumption was reduced significantly on magnesium infusion group (Meperidine: C: 36.3 +/- 42.6 mg, Mg: 11.7 +/- 12.2 mg, p: 0.001). Visual analogue scales were also observed to be lower in all periods. Time to motor block resolution, and sedation scores were similar. Magnesium sulphate infusion is thought as a safe and suitable adjunct for reducing analgesic consumption and possible complications without interfering daily activity in patients undergoing brachial plexus block. PMID:18095196

Anbarci, Ozlem; Apan, Alparslan; Sahin, Saziye

2007-07-01

60

Influence of bile acid derivates on morphine analgesic effect in mice  

Directory of Open Access Journals (Sweden)

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

Vasovi? Velibor

2014-01-01

61

Analgesic effect of intra-articular ketorolac in knee arthroscopy: comparison of morphine and bupivacaine.  

Science.gov (United States)

This prospective study assessed the postoperative analgesic effect of intra-articular ketorolac, morphine, and bupivacaine during arthroscopic outpatient partial meniscectomy. Group 1 patients (n=20) received postoperative injection of 60 mg intra-articular ketorolac, group 2 patients (n=20) 10 cc intra-articular bupivacaine 0.25%, group 3 patients (n=20) 1 mg intra-articular morphine diluted in 10 cc saline, and group 4 patients (n=20, controls) only 10 cc saline. We evaluated the postoperative analgesic effect (period measured from the end of the surgery until further analgesia was demanded), the level of postoperative pain (by visual analog scale 1, 2, 3, 12, and 24 h after surgery), and the need for additional pain medication (during the first 24 h after surgery). The best analgesic effect was in patients treated with intra-articular ketorolac, and this was statistically significant in: postoperative analgesic effect and the need for additional pain medication immediately after surgery, and after 24 h. No complications were found related to the intra-articular treatment. We conclude that 60 mg intra-articular ketorolac provides better analgesic effect than 10 cc intra-articular bupivacaine 0.25% or 1 mg intra-articular morphine. PMID:15197428

Calmet, J; Esteve, C; Boada, S; Giné, J

2004-11-01

62

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

Directory of Open Access Journals (Sweden)

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.

Jamal Shams

2008-01-01

63

Inhibition of antiplatelet effects of aspirin by nonopioid analgesics.  

Science.gov (United States)

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

Hohlfeld, T; Schrör, K

2015-02-01

64

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

Directory of Open Access Journals (Sweden)

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 analgesic effects in experimental settings, as well as in post-operative acute pain and chronic pain syndromes. The promising evidence of tDCS-induced analgesic effects raises the challenging and complex question of potential physiologic mechanisms that underlie/mediate the accomplished pain relief. Here we present hypotheses on how the specific montages and targets for stimulation may affect the pain processing network.

HelenaKnotkova

2013-09-01

65

Analgesic, anti-inflammatory, and antipyretic effects of Ixora coccinea.  

Science.gov (United States)

Abstract Background: The present study was carried out to explore the potential of the ethanol extract of Ixora coccinea L. (IC) leaves as analgesic, anti-inflammatory and antipyretic agents using the hot-plate, acetic acid-induced writhing, carrageenan-induced paw edema and brewer's yeast-induced pyrexia tests in rodents. Methods: The extract was prepared by soaking the dried powdered leaves of IC in ethanol for 2 days. The filtrate thus obtained by filtration and evaporation was considered as a stock solution and was used in all experimental models. Results: Oral administration of IC (250 and 500 mg/kg) significantly (pIxora coccinea (250 and 500 mg/kg) produced 56.14% and 63.16% inhibition (p<0.05) in acetic acid-induced writhing. It also (250 and 500 mg/kg) produced significant (p<0.05) inhibition of paw edema pronounced at 6 h after carrageenan injection. Intraperitoneal administration of IC (250 and 500 mg/kg) lowered the body temperature in brewer's yeast-induced hyperthermia. Conclusions: Based on the findings, it may be concluded that the IC leaves possessed analgesic, anti-inflammatory, and antipyretic activities. Phytochemical constituents of IC leaves such as flavonoids, tannins, and triterpenes in ethanol extract could be correlated with its observed biological activities. PMID:24468614

Ali Adnan, Md Syed; Al-Amin, Md Mamun; Nasir Uddin, Mir Muhammad; Shohel, M; Bhattacharjee, Rajib; Hannan, J M A; Das, Biplab Kumar

2014-01-27

66

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

DEFF Research Database (Denmark)

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.

Wilhelmsen, Michael; Amirian, Ilda

2011-01-01

67

Influence of serotonin on the analgesic effect of granisetron on temporomandibular joint arthritis  

Directory of Open Access Journals (Sweden)

Full Text Available THE influence of circulating serotonin (5-HT on the effects of intra-articular administration of granisetron on temporomandibular joint (TMJ pain was investigated in 11 patients with chronic polyarthritides. An analgesic effect superior to placebo has been shown previously.

Sigvard Kopp

1992-01-01

68

Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain  

Directory of Open Access Journals (Sweden)

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.

ALVES NILZA D.

1999-01-01

69

EVALUATION OF ANTI-INFLAMMATORY ACTIVITY AND ANALGESIC EFFECT OF ALOE VERA LEAF EXTRACT IN RATS  

Directory of Open Access Journals (Sweden)

Full Text Available Clinical evaluation of analgesic and anti-inflammatory drugs envisages the development of side effects that makes efficacy of a drug arguable. Alternatively, indigenous drug with fewer side effects is the major thrust area of research in the management of pain and inflammation. In the present study aqueous extract of whole leaf of Aloe vera at various concentrations was investigated for its anti-inflammatory and analgesic activities in albino wistar rats. Carrageenan and formaldehyde-induced rat paw oedema was used to evaluate the anti-inflammatory activity and tail flick, hot plate and acetic acid tests were used to assess the analgesic activity of A. vera leaf aqueous extracts. Whole leaf aqueous extracts at various concentrations (100, 200, 400, and 600 mg/kg of bw significantly reduced formation of oedema induced by carrageenan and formaldehyde and granuloma formation in a dose dependent manner. Further, acetic acid-induced writhing model exhibited significant analgesic effect characterized by reduction in writhes. Whole leaf aqueous extract showed dose-dependent increase in tolerance to thermal stimulus comparable to indomethacin. No mortality was observed during the acute toxicity test at a dosage of 600mg/kg. Thus whole leaf aqueous extract of Aloe vera can be exploited as non toxic drug for the treatment and clinical management of inflammation and pain.

Aruna Devaraj

2011-03-01

70

Adjuvant analgesics.  

Science.gov (United States)

Chronic pain, whether arising from viscera, bone, or any other tissue or structure, is, more often than commonly thought, the result of a mixture of pain mechanisms, and therefore there is no simple formula available to manage chronic complex pain states. Box 1 summarizes a pharmacological algorithm for difficult-to-treat chronic pain, which merely introduces the medication aspect of the treatment. In effect, any comprehensive algorithm should call for an interdisciplinary approach that would include rehabilitation, as well as psychosocial, and when indicated, interventional techniques. Box 1 Analgesic algorithm for difficult-to-treat pain syndromes. Pharmacological Interventions. Moderate to severe pain/functional impairment; pain with a score of >4 on the brief pain inventory. 1. Gabapentinoid (gabapentin, pregabalin)+/-Opioid/opioid rotation or 2. Antidepressant (TCA, duloxetine, venlafaxine)+/-Opioid/opioid rotation or 3. Gabapentinoid+antidepressant+Opioid/opioid rotation; in addition, may consider trials of one or more of the following adjuvants when clinically appropriate: Topical therapies for cutaneous allodynia/hyperalgesia. Anti-inflammatory drugs (corticosteroids for acute inflammatory neuropathic pain)IV bisphosphonates for cancer bone pain or CRPS/RSDNon-gabapentinoid AEDs such as carbamazepine or oxcarbazepine or lamotrigine+/-baclofen for intermittent lancinating pain due to cranial neuralgiasNMDA antagonists Mexiletine On a compassionate basis, according to the patient's clinical condition and pain mechanism, the physician may want to consider an empirical trial of one or more of the emergent topical, oral or parenteral/intrathecal therapies as discussed in the text. If SMP, consider topical clonidine and sympatholytic interventions; if clinically feasible, trials of topical therapies, eg, lidocaine 5% patch, may be considered for a variety of pain states and features.The major rationale for introducing adjuvants is to better balance efficacy and adverse effects. The following scenarios should prompt the use of adjuvants in clinical practice: The toxic limit of a primary analgesic has been reached. The therapeutic benefit of a primary analgesic has plateaued, eg, treatment has reached its true efficacy limit or pharmachodynamic tolerance has developed. The primary analgesic is contraindicated, eg, substance abuse, aberrant behavior, organ failure, allergy, and so forth. Subjective and qualitative symptoms demand broader coverage. Patients often convey that different medications will impart distinct analgesic benefits. Presence of disabling nonpainful complaints and need to manage symptoms such as insomnia, depression, anxiety, and fatigue that all cause worsening of the patient's quality of life and function. Physicians have also been drawn to the adjuvants secondary to new realities of clinical practice. Moreover, aversion to addiction and diversion remains a potent force that shapes prescribing profiles. PMID:17164107

Knotkova, Helena; Pappagallo, Marco

2007-01-01

71

Analgesic activity of the ethanolic extract of Shorea robusta resin in experimental animals  

Science.gov (United States)

Aim: Shorea robusta (Sal), an important traditional Indian medicinal plant used in various ailments and rituals and the indigenous use of the resin of this plant as a medicament for treatment of various inflammatory conditions is well documented in literature. In the present study, ethanolic extract of S. robusta resin (SRE) was evaluated for its analgesic activity by making use of different central and peripheral pain models. Materials and Methods: The analgesic activity of SRE was assessed by employing different pain models such as, i) hot plate and tail flick tests for central analgesia, ii) acetic acid- induced writhing (peripheral analgesic model), iii) formalin-induced hind paw licking (both central and peripheral model), iv) carrageenan-induced hyperalgesia (peripheral analgesic model) and v) post-surgical pain (peripheral analgesic model). Results: The extract produced significant central and peripheral analgesic effects, as is evident from increase in reaction time in hot plate and tail flick tests, inhibition in writhing counts in acetic acid-induced writhing test, inhibition of licking time in formalin-induced hind paw licking, increased pain threshold in paw withdrawal latency in carrageenan-induced hyperalgesia and increased paw withdrawal threshold in post-surgical pain. Conclusion: The results of the present study demonstrate marked antinociceptive effects of SRE. PMID:23087512

Wani, Tariq Ahmad; Kumar, Dhirendra; Prasad, Raju; Verma, Pawan Kumar; Sardar, Kaustuk K.; Tandan, Surendra Kumar; Kumar, Dinesh

2012-01-01

72

Analgesic and anti-inflammatory effect of aqueous extract of the stem bark of Allanblackia gabonensis (Guttiferae).  

Science.gov (United States)

Allanblackia gabonensis (Guttiferae) is a plant used in the African traditional medicine as remedies against pain, rheumatism, inflammations. In the present work, the analgesic effect of aqueous extract has been evaluated using acetic acid, formalin, hot-plate test, tail immersion and paw-pressure test. The anti-inflammatory effect of this extract was also investigated on carrageenan, histamine or serotonin induced by paw oedema. Aqueous extract of stem bark of A. gabonensis administrated p.o. showed significant activity against paw oedema induced by carrageenan, with a maximum percentage of inhibition reaching the 74.01% at the preventive test at a dose of 200 mg/kg. A. gabonensis exhibited a significant reduction of paw oedema induced by both histamine and serotonin with a maximal inhibition of 56.94% (200 mg/kg) and 40.83% (100 mg/kg), respectively. It showed significant protective effects against chemical stimuli (acetic acid and formalin) in the mouse. Administered orally at the doses of 100-400 mg/kg, exhibited protective effect of at least 69.78% on the pain induced by acetic acid and also reduced first (67.18% at 200 mg/kg) and second (83.87% at 400 mg/kg) phase of pain-induced par formalin. It also produced a significant increase of the threshold of sensitivity to pressure and hot plate-induced pain in the rats. These results suggest a peripheral and central analgesic activities as well as an anti-inflammatory effect of the stem bark of A. gabonensis. PMID:22071660

Ymele, Edwige V; Dongmo, A Bertrand; Dimo, Théophile

2013-02-01

73

Analgesic effect of intra-articular magnesium sulphate compared with bupivacaine after knee arthroscopic menisectomy  

Directory of Open Access Journals (Sweden)

Full Text Available This work aimed to evaluate the analgesic efficacy of intra-articular injection of magnesium sulphate (4% compared with equivalent volume of bupivacaine (0.5% after outpatient knee arthroscopic meniscectomy. Forty patients were randomly assigned to two groups. Group M (n = 20 received intra-articular magnesium sulphate 4%, group B (n = 20 received bupivacaine (0.5%. Analgesic effect was evaluated by analgesic duration, and by measuring pain intensity at 1, 2, 4, 6, 12, 24 h both at rest and on knee movement to 90°. The primary outcome variable was pain intensity on the VAS at 1, 2, 4, 6, 12, 24 h post arthroscopy at rest and on movement (flexion of knee to 90°, although the magnesium group had lower time weighted averages (TWAs at rest and on movement, these TWAs were not statistically significant. The median duration of postoperative analgesia was significantly longer in the patients treated with magnesium sulphate (528 min than in the bupivacaine group (317 min (p < 0.0001, with less number of patients needing supplementary analgesia in magnesium group (8/20 than those of the bupivacaine group (16/20 (p < 0.022. Also analgesic consumption was significantly lower in the magnesium sulphate group (p < 0.002. We concluded that the use of magnesium sulphate is rational and effective in reducing pain, and is more physiological and shortens convalescence after outpatient arthroscopic meniscectomy, however our hypotheses that analgesic efficacy of intra-articular isotonic magnesium sulphate would be superior to intra-articular local anaesthetic cannot be supported with this study.

Yasser A. Radwan

2013-07-01

74

Antiinflammatory and analgesic effects of Psidium guajava Linn. (Myrtaceae) leaf aqueous extract in rats and mice.  

Science.gov (United States)

In many parts of Africa, the leaf, stem-bark, and roots of Psidium guajava Linn. (Family: Myrtaceae) are used traditionally for the management, control, and/or treatment of an array of human disorders. In an effort to scientifically appraise some of the ethnomedical properties of P. guajava leaf, and probe its efficacy and safety, the present study was undertaken to examine the antiinflammatory and analgesic properties of the plant's leaf aqueous extract in some experimental animal paradigms. The antiinflammatory property of the aqueous leaf extract was investigated in rats, using fresh egg albumin-induced pedal (paw) edema, while the analgesic effect of the plant extract was evaluated by the "hot-plate" and "acetic acid" test models of pain in mice. Diclofenac (100 mg/kg, i.p.) and morphine (10 mg/kg, i.p.) were used respectively as standard, reference antiinflammatory and analgesic agents for comparison. P. guajava leaf aqueous extract (PGE, 50-800 mg/kg, i.p.) produced dose-dependent and significant (p plant extract (PGE, 50-800 mg/kg, i.p.) also produced dose-dependent and significant (p plant are speculated to account for the observed antiinflammatory and analgesic effects of the plant's leaf extract. In summary, the findings of this experimental animal study indicate that the leaf aqueous extract of P. guajava possesses analgesic and antiinflammatory properties, and thus lend pharmacological credence to the suggested ethnomedical, folkloric uses of the plant in the management and/or control of painful, arthritic and other inflammatory conditions in some rural communities of Africa. PMID:17003849

Ojewole, J A O

2006-09-01

75

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

Directory of Open Access Journals (Sweden)

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.

Nan-Fu Chen

2014-06-01

76

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

OpenAIRE

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

Chandra Shekar

2012-01-01

77

Analgesic effect of highly reversible ?-conotoxin FVIA on N type Ca2+ channels  

Directory of Open Access Journals (Sweden)

Full Text Available Abstract Background N-type Ca2+ channels (Cav2.2 play an important role in the transmission of pain signals to the central nervous system. ?-Conotoxin (CTx-MVIIA, also called ziconotide (Prialt®, effectively alleviates pain, without causing addiction, by blocking the pores of these channels. Unfortunately, CTx-MVIIA has a narrow therapeutic window and produces serious side effects due to the poor reversibility of its binding to the channel. It would thus be desirable to identify new analgesic blockers with binding characteristics that lead to fewer adverse side effects. Results Here we identify a new CTx, FVIA, from the Korean Conus Fulmen and describe its effects on pain responses and blood pressure. The inhibitory effect of CTx-FVIA on N-type Ca2+ channel currents was dose-dependent and similar to that of CTx-MVIIA. However, the two conopeptides exhibited markedly different degrees of reversibility after block. CTx-FVIA effectively and dose-dependently reduced nociceptive behavior in the formalin test and in neuropathic pain models, and reduced mechanical and thermal allodynia in the tail nerve injury rat model. CTx-FVIA (10 ng also showed significant analgesic effects on writhing in mouse neurotransmitter- and cytokine-induced pain models, though it had no effect on acute thermal pain and interferon-? induced pain. Interestingly, although both CTx-FVIA and CTx-MVIIA depressed arterial blood pressure immediately after administration, pressure recovered faster and to a greater degree after CTx-FVIA administration. Conclusions The analgesic potency of CTx-FVIA and its greater reversibility could represent advantages over CTx-MVIIA for the treatment of refractory pain and contribute to the design of an analgesic with high potency and low side effects.

Kim Hyun Jeong

2010-12-01

78

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

Science.gov (United States)

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

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

79

Intravenous flurbiprofen axetil can increase analgesic effect in refractory cancer pain  

OpenAIRE

Abstract Background The aim of this study was to investigate the analgesic effects of intravenous flurbiprofen axetil for the refractory pain in cancer patients. Methods 2109 patients were screened from the department of medical oncology, the first affiliated hospital of Anhui medical university in China between October of 2007 and October of 2008. Thirty-seven cases of cancer patients who had bad effect from anaesthetic drugs were received administration of int...

Hao Jiqing; Pan Yueyin; Gu Kangsheng; Sun Guoping; Chen Zhendong; Wu Hongyang; Du Yingying; Ning Jie

2009-01-01

80

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

OpenAIRE

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...

Gonul Sagiroglu

2011-01-01

81

Influence of serotonin on the analgesic effect of granisetron on temporomandibular joint arthritis  

OpenAIRE

The influence of circulating serotonin (5-HT) on the effects of intra-articular administration of granisetron on temporomandibular joint (TMJ) pain was investigated in 11 patients with chronic polyarthritides. An analgesic effect superior to placebo has been shown previously. The change in TMJ movement pain intensity was negatively correlated to circulating 5-HT; that is, the higher the 5-HT before injection, the greater the reduction of pain intensity. The resting pain intensity reduction wa...

Sigvard Kopp; Riina Kallikorm; Edvitar Leibur; Per Alstergren; Ülle Voog

2004-01-01

82

Pharmacologically active components of viticis fructus (Vitex rotundifolia). II. The components having analgesic effects.  

Science.gov (United States)

The extract of Viticis Fructus appeared to have an analgesic effect, and was subjected to activity-guided separation using acetic acid-induced writhing in mice. The active fraction gave new compounds, vitexfolin A (1A), B and C, 10-O-vanilloylaucubin (3), dihydrodehydrodiconiferylalcohol-beta-D- (2'-O-p-hydroxybenzoyl)glucoside (4), and vanilloyl-beta-D-(2'O-p-hydroxybenzoyl)glucoside, together with agnuside (2) and erythro- and threoguaiacylglycerols. Compounds 1A and 2-4 showed significant writhing inhibition following oral administration at doses of 15, 50, 25, and 50 mg/kg, respectively. The effect on pressure pain threshold was tested using compounds 1A and 2 at a dose of 50 mg/kg, and only the former produced the analgesia. The analgesic effect of some related iridoid glucosides is also discussed. PMID:9579042

Okuyama, E; Fujimori, S; Yamazaki, M; Deyama, T

1998-04-01

83

5. Anti inflammatory and analgesic effect of methanolic extract of Anogeissus acuminata leaf  

Directory of Open Access Journals (Sweden)

Full Text Available In the present study, the anti-inflammatory and analgesic effect of the methanol extract of Anogeissus acuminata leaf was investigated. The methanolic extracts of Anogeissus acuminata leaf were ingested orally (p.o. in the form of suspension in 0.5% Tween 80 in two different doses, 200 and 400 mg/kg body weight. The anti-inflammatory effect of Anogeissus acuminata was tested in: carrageenin-induced paw oedema in wistar albino rats and formalin-induced paw oedema in Swiss albino mice and compared with the standard, indomethacin (5 mg/kg body weight. The analgesic effect was evaluated in Swiss albino mice by Eddy’s hot plate method and compared with the standard, aspirin (25 mg/kg body weight. The results showed that Anogeissus acuminata has significant reduction (p?0.01 in inflammation i.e. 66.67 % (200 mg/kg body weight and 77.78% (400 mg/kg body weight as compared to the standard drug, indomethacin, which was 88.89%. In assessing analgesic effects, there is a significant (p<0.01 reduction in the paw licking and paw jumping response for Anogeissus acuminata (400 mg/kg and aspirin (25 mg/kg when compared to control. These results indicate that the extracts could possess analgesic and anti-inflammatory properties. All these effects and the changes in the behavioural activities could be suggested as contributory effects to the use of Anogeissus acuminata leaf in the management of inflammation and painful conditions.

K. Hemamalini

2010-08-01

84

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

Science.gov (United States)

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

2013-12-01

85

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

OpenAIRE

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-blindly 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...

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

2013-01-01

86

Evaluation of analgesic effects of intrathecal clonidine along with bupivacaine in cesarean section  

OpenAIRE

Aims and Context: The objective of the present study was to evaluate the analgesic and adverse effects of intrathecal clonidine with hyperbaric bupivacaine in spinal anesthesia. Settings and Design : Randomized single blind trial. Methods: 210 ASA I-II pregnant females undergoing emergency cesarean section were randomized in a single-blind fashion to one of the three groups. In group I (n=70) patients received 12.5 mg of 0.5% hyperbaric bupivacaine intrathecally. I...

Kothari Nikhil; Bogra Jaishri; Chaudhary Ajay

2011-01-01

87

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

OpenAIRE

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...

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

2014-01-01

88

Functional characterization and analgesic effects of mixed cannabinoid receptor/T-type channel ligands  

OpenAIRE

Abstract Background Both T-type calcium channels and cannabinoid receptors modulate signalling in the primary afferent pain pathway. Here, we investigate the analgesics activities of a series of novel cannabinoid receptor ligands with T-type calcium channel blocking activity. Results Novel compounds were characterized in radioligand binding assays and in vitro functional assays at human and rat CB1 and CB2 receptors. The inhibitory effects of these comp...

You Haitao; Gadotti Vinicius M; Petrov Ravil R; Zamponi Gerald W; Diaz Philippe

2011-01-01

89

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

OpenAIRE

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...

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

2000-01-01

90

Analgesic effects of intra-articular fentanyl, pethidine and dexamethasone after knee arthroscopic surgery  

OpenAIRE

BACKGROUND: Many different methods have been used in an effort to provide adequate analgesia after knee arthroscopic surgery. In this study analgesic effect of intra-articular fentanyl, pethidine and dexamethasone was compared. METHODS: In a double blind randomized study 48 male patients undergoing knee arthroscopic meniscectomy were allocated to groups receiving intra-articular fentanyl 50 µg or pethidine 20 mg or dexamethasone 8 mg at the end of arthroscopy during general aesthesia. P...

Saryazd, H.; Kashefi, P.; Heydari, M.; Kiani, A.

2006-01-01

91

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

OpenAIRE

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...

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

2009-01-01

92

Anaesthetic, analgesic and cardiorespiratory effects of three intramuscular anaesthetic protocols in cats  

OpenAIRE

Objectives To compare the anaesthetic, analgesic and cardiorespiratory effects of intramuscular medetomidine and ketamine administered alone or combined with morphine or tramadol for orchiectomy in cats. Study design Randomised, blinded, prospective clinical study. Animals Thirty client owned healthy cats. Materials and methods Cats received a combination of medetomidine (60 ?g kg-1) and ketamine (10 mg kg-1) alone (MedK) or combined with morphine (0.2 mg kg-1) (MedKM) or tramadol (...

Zeiler, Gareth Edward

2014-01-01

93

Pharmacodynamic effects of oral oxymorphone: abuse liability, analgesic profile and direct physiologic effects in humans.  

Science.gov (United States)

Oxymorphone is a semisynthetic ?-opioid agonist, marketed as a prescription analgesic purported to be twice as potent as oxycodone for pain relief. Oral formulations of oxymorphone were reintroduced in the United States in 2006 and reports of abuse ensued; however, there are limited data available on its pharmacodynamic effects. The current study aimed to examine the direct physiologic effects, relative abuse liability, analgesic profile and overall pharmacodynamic potency of oxymorphone in comparison with identical doses of oxycodone. Healthy, non-dependent opioid abusers (n?=?9) were enrolled in this within-subject, double-blind, placebo-controlled, 3-week inpatient study. Seven experimental sessions (6.5 hours) were conducted, during which an oral dose of immediate-release formulations of oxymorphone (10, 20 and 40?mg), oxycodone (10, 20 and 40?mg) or placebo was administered. An array of physiologic, abuse liability and experimental pain measures was collected. At identical doses, oxymorphone produced approximately twofold less potent effects on miosis, compared with oxycodone. Oxymorphone also produced lesser magnitude effects on measures of respiratory depression, two experimental pain models and observer-rated agonist effects. However, 40?mg of oxymorphone was similar to 40?mg of oxycodone on several abuse-related subjective ratings. Formal relative potency analyses were largely invalid because of the substantially greater effects of oxycodone. Overall, oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone. These data suggest that the published clinical equianalgesic estimates may not be consistent with the observed direct physiologic effects of opioids, results of experimental pain models or abuse liability measures, as assessed in the human laboratory. PMID:25130052

Babalonis, Shanna; Lofwall, Michelle R; Nuzzo, Paul A; Walsh, Sharon L

2014-07-31

94

Experimental study on anti-inflammatory and analgesic effects of Yitieling Paste  

Directory of Open Access Journals (Sweden)

Full Text Available Objective: To observe the anti-inflammatory and analgesic effects of Yitieling Paste (YTLP. Methods: YTLP and aspirin (as a control drug were introduced to treat the edematous ears of mice induced by xylene and swollen toes of mice induced by carrageenin, and to relieve the pain in mice induced by heat and acetic acid. The swelling degree, pain threshold and body distortions were measured. Results: The repression rates of the ear edema in groups of YTLP of high and low dosages and the aspirin group were 67.92%, 52.52% and 58.28%, respectively. The repression rate of the toe swelling in YTLP high dosage group was higher than that of the aspirin group, which was higher than that of the YTLP low dosage group. The results of analgesic effect of the three YTLP-treated groups showed that with the increase of dosage, the pain thresholds were higher and higher, and the body distortions were lower and lower. The pain thresholds of high and medium dosage YTLP groups were near to the aspirin group. Conclusion: YTLP possesses a strong anti-inflammatory and analgesic effect.

XU Li-Jun

2005-07-01

95

Analgesic effect of simultaneous exposure to infrared laser radiation and ?T magnetic field in rats  

Science.gov (United States)

The aim of the experiment was to estimate the effect of repeated simultaneous exposures to infrared laser radiation and ?T variable magnetic field used in magnetostimulation on pain perception in rats, as well as the involvement of endogenous opioid system in the mechanism of this effect. In experimental group clean-shaven scull of male Wistar rats placed individually in a specially designed plastic chamber were simultaneously exposed to infrared laser radiation (wavelength - 855 nm, mean power - 4,1 mW, energy density - 30 J/cm2) and variable magnetic field of saw-like shape of impulse, at a frequency of basic impulse 180-195 Hz and mean induction value of 120 ?T generated by magneto-laser applicator of device for magnetostimulation Viofor JPS (Med & Life, Poland) 12 minutes daily for 2 periods of 5 consecutive days, with 2 days-lasting break between them, while control animals were sham-exposed. The pain perception was determined by means of "hot plate" test on the basis of calculated analgesic index. As a result of repeated exposures a significant increase in analgesic index persisting also till 14 th day after the end of a cycle of exposures was observed. This analgesic effect was inhibited by prior i.p. injection of opioid antagonist - Naloxone.

Cieslar, Grzegorz; Mrowiec, Janina; Kasperczyk, Slawomir; Sieron-Stoltny, Karolina; Sieron, Aleksander

2008-03-01

96

Analgesic and anti-inflammatory effects of ethanol extracted leaves of selected medicinal plants in animal model  

OpenAIRE

Aim: The research was carried out to investigate the analgesic and anti-inflammatory effects of ethanol extract of Desmodium pauciflorum, Mangifera indica and Andrographis paniculata leaves. Materials and Methods: In order to assess the analgesic and anti-inflammatory effects acetic acid induced writhing response model and carrageenan induced paw edema model were used in Swiss albino mice and Wistar albino rats, respectively. In both cases, leaves extract were administered (2gm/kg body weight...

Hassan, Mohammad M.; Khan, Shahneaz A.; Shaikat, Amir H.; Md. Emran Hossain; Md. Ahasanul Hoque; Md Hasmat Ullah; Saiful Islam,

2013-01-01

97

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

Directory of Open Access Journals (Sweden)

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.

Tozzini Danila

2008-11-01

98

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

Directory of Open Access Journals (Sweden)

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 studied, 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.

Guadalupe García P

2011-10-01

99

Analgesic effects of intra-articular fentanyl, pethidine and dexamethasone after knee arthroscopic surgery  

Directory of Open Access Journals (Sweden)

Full Text Available BACKGROUND: Many different methods have been used in an effort to provide adequate analgesia after knee arthroscopic surgery. In this study analgesic effect of intra-articular fentanyl, pethidine and dexamethasone was compared. METHODS: In a double blind randomized study 48 male patients undergoing knee arthroscopic meniscectomy were allocated to groups receiving intra-articular fentanyl 50 µg or pethidine 20 mg or dexamethasone 8 mg at the end of arthroscopy during general aesthesia. Postoperative pain scores using visual analogue scale were measured and also analgesic requirements and the time of ability to walk were recorded. RESULTS: Pain scores at one, two, six and 24 h after intra-articular injection were not significantly different for fentanyl and pethidine but were higher significantly for dexamethasone at all four mentioned times. The mean average time of ability to walk was significantly longer for dexamethasone. The analgesic requirements during the first 24 h after intraarticular injection were significantly greater only for dexamethasone too. CONCLUSION: Better postoperative analgesia, less pain score and shorter time to walk were achieved by fentanyl and pethidine in comparison to dexamethasone but the results were not significantly different between fentanyl group and pethidine. KEYWORDS: Arthroscopy, opioid, pain.

H Saryazd

2006-07-01

100

The effect of fluorine substitution on the physicochemical properties and the analgesic activity of paracetamol.  

Science.gov (United States)

The physicochemical properties and analgesic action of six fluorinated analogues of 4-hydroxyacetanilide (paracetamol) have been investigated. Fluorine substitution adjacent to the hydroxyl group increased lipophilicity and oxidation potential whilst substitution adjacent to the amide had little effect on lipophilicity but led to a greater increase in oxidation potential. Lack of coplanarity and conjugation of the amide group and aromatic ring was also apparent with the analogues that had fluorine in the 2 and 6 positions. Introduction of fluorine into the amide group of paracetamol increased the lipophilicity 4-fold and also increased the oxidation potential of paracetamol. ED50 values for analgesic activity in the phenylquinone-induced abdominal constriction test on male Swiss White mice showed that ring substitution by fluorine reduced activity, especially at the 2,6-positions. Introduction of fluorine into the amide group enhanced activity significantly. Correlation of the analgesic activity with the physicochemical properties indicated that conjugation (and planarity) of the amide group with the aromatic ring is essential for activity and that ease of oxidation may also be an important factor. PMID:7901373

Barnard, S; Storr, R C; O'Neill, P M; Park, B K

1993-08-01

101

Putative physiological mechanisms underlying tDCS analgesic effects  

OpenAIRE

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...

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

2013-01-01

102

Intravenous flurbiprofen axetil can increase analgesic effect in refractory cancer pain  

Directory of Open Access Journals (Sweden)

Full Text Available Abstract Background The aim of this study was to investigate the analgesic effects of intravenous flurbiprofen axetil for the refractory pain in cancer patients. Methods 2109 patients were screened from the department of medical oncology, the first affiliated hospital of Anhui medical university in China between October of 2007 and October of 2008. Thirty-seven cases of cancer patients who had bad effect from anaesthetic drugs were received administration of intravenous flurbiprofen axetil with dose of 50 mg/5 ml/day. The pain score was evaluated for pre- and post- treatment by Pain Faces Scale criteria, and the side effects were also observed. Results Intravenous flurbiprofen axetil increased the analgesic effects. The total effective rate was 92%. The side effects, such as abdominal pain, alimentary tract bleeding which were found in using NSAIDs or constipation, nausea, vomit, sleepiness which were found in using opioid drugs did not be found. Conclusion Intravenous flurbiprofen axetil could provide better analgesia effects and few side effects to patients with refractory cancer pain. It could also increase analgesia effects when combining with anesthetic drugs in treatment of moderate or severe pain, especially breakthrough pain, and suit to patients who can not take oral drugs for the reason of constipation and psychosomatic symptoms.

Hao Jiqing

2009-03-01

103

The effect of acupuncture duration on analgesia and peripheral sensory thresholds  

Directory of Open Access Journals (Sweden)

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.

Schulteis Gery

2008-05-01

104

"Comparison of the analgesic profile and side effects of tramadol vs pethidine, following urologoical surgery "  

Directory of Open Access Journals (Sweden)

Full Text Available The optimization of pain management following surgery with minimal side effects, is one the major goals of surgical and medical teams. In this randomized double blind study, sixty ASA (American Society of Anesthesiologist class I or II patients, undergoing urological surgery, were assessed to receive either pethidine or tramadol using a standard method for general anesthesia. Pain intensity was assessed by verbal rating, through a 4-step scaling system. Results of this investigation have revealed that the mean total drug administered in tramadol group were 244.53 + 56.95 mg and in pethidine group 176.78+42.99 mg respectively. There were no significant differences in analgesic effect, observed in either group during early hours following surgery, but after 8,12 and 16 hours significant differences were observed. Analgesic properties of tramadol were almost comparable with pethidine nevertheless; pethidine was superior in some extent. No significant differences in patient’s PaO2 were found, but PaCO2 at 1 and 4 hours after surgery had a greater retention in pethidine group. (P<0.001. There was a significant reduction in respiratory rate in pethidine group at 4,8,12 and 16 hours following surgery, compared with tramadol group (P<0.001. Incidence of dizziness was greater in patients who received pethidine (P<0.001, and sweating was higher in tramadol group (P<0.01. Also there was a greater need for metoclopramide to overcome nausea in tramadol group (P<0.05. Results of this study may suggest that tramadol could be considered as a safe and effective analgesic, following urological surgery as compared with pethidine

Mojtaba Mojtahedzadeh

2004-08-01

105

Analgesic and anti-ulcerogenic effects of a polar extract from leaves of Vernonia condensata.  

Science.gov (United States)

An aqueous crude extract and a polar fraction derived from this extract were prepared from leaves of Vernonia condensata Baker and assessed in standard rodent models of algesia and ulcerogenesis. Oral pretreatment with the lyophilized crude extract (200 mg/kg) significantly reduced mouse writhing counts caused by the i.p. injection of increasing concentrations (0.6-1.2%) of acetic acid (0.1 ml/10 g). In doses ranging from 50 to 400 mg/kg, the crude extract inhibited dose-dependently mouse writhing induced by acetic acid (0.6%) (ED50 = 241 mg/kg) and also markedly increased the sleeping time induced by thiopental. The polar fraction, prepared by washing out the crude extract with chloroform, did not alter sleeping time but kept the analgesic activity (ED50 = 154 mg/kg), indicating that these effects are indeed dissociated. In contrast, the tail flick response in the immersion test was not modified by the crude extract or the polar fraction. The relative potency with which polar fraction and non-steroidal anti-inflammatory drugs inhibited mouse writhing caused by acetic acid in mice was indomethacin > dypirone > polar fraction > aspirin. Furthermore, the combined polar fraction/aspirin or polar fraction/indomethacin treatments presented a marked synergistic effect, in contrast to what was observed when submaximal doses of indomethacin and aspirin were coadministered, suggesting that polar fraction and aspirin like drugs may have complementary analgesic actions. Finally, despite being able to potentiate the analgesic effect of indomethacin in mouse writhing caused by acetic acid, the pretreatment with the polar fraction (200 mg/kg, oral) significantly prevented indomethacin-induced ulcers in rats.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:8134411

Frutuoso, V S; Gurjão, M R; Cordeiro, R S; Martins, M A

1994-02-01

106

Effects of Laser Irradiation on Peripheral Nerve  

Science.gov (United States)

A literature review was undertaken to determine the electrophysiological effects of Laser Irradiation (LI) on peripheral mammalian nerves, as a means of elucidating the potential mechanisms underlying pain relief associated with laser therapy. Relevant computerized databases and reference lists were searched, and experts consulted for further articles. A total of 38 studies, comprising 82 separate experiments were identified. In human studies, all types of LI (red and infrared, pulsed and cw) slowed nerve conduction velocity, and reduced compound action potential of irradiated nerves. In animal studies, infrared LI suppressed conduction velocity, as well as noxious stimulation evoked potential. This review thus indicates the potential of laser irradiation to inhibit activity in peripheral nerves, and highlights one potential mechanism of action for laser-mediated pain relief.

Baxter, G. D.; Chow, R.; Armati, P.; Bjordal, J. M.; Laakso, L.

2009-06-01

107

Anticonvulsant and Analgesic Effects of Harpephyllum caffrum Bernh. ex C.F. Krauss [Anacardiaceae] Stem-Bark Aqueous Extract in Mice  

OpenAIRE

This study was undertaken to evaluate the anticonvulsant and analgesic effects of Harpephyllum caffrum stem-bark aqueous extract (HCE) in mice. The anticonvulsant effect of the plant’s stem-bark extract (HCE, 50-800 mg kg-1 intraperitoneally) was examined against pentylenetetrazole (PTZ)- and picrotoxin (PCT)- induced seizures, while the analgesic effect of the extract (HCE, 50-800 mg kg-1 I. p.) was evaluated by hot-plate and acetic acid analgesic test methods....

Ojewole, John A. O.; Amabeoku, George J.

2007-01-01

108

THE EFFECT OF TRANSDERMAL NITROGLYCERINE ON ANALGESIC EFFECT OF INTRATHECAL SUFENTANIL IN LOWER EXTREMITY SURGERY  

Directory of Open Access Journals (Sweden)

Full Text Available Introduction: Sufentanil is a potent but short-acting analgesic that used intrathecally to manage postoperative pain. The goal of study is determining the effect of transdermal nitroglycerine on duration of analgesic effect of spinal sufentanil in lower extremity surgery .
Methods and Material: In a clinical trial study with convenience sampling ASA (I, ASA(IIpatients in 18 -65 old -age condidated for lower extremity surgery in Isfahan st. AlZAHRA medical center in 2001-2002 were randomized to one of four groups. (each group contains ten patients Patients received 15 mg bupivacaine 0.5% plus 2ml of the test drug intrathecally (saline or 10 mic.gram sufentanil. 30 min after the spinal puncture, a transdermal patch of either 5mg nitroglycerinor placebo was applied. The control group (A received spinal saline and transdermal placebo. The sufentanil group (B received spinal sufentanil and transdermal placebo. The nitroglycerine group (C received spinal saline and transdermal nitroglycerine patch. Finally, the sufentanil-nitroglycerine group (D received spinal sufentanil and transdermal nitroglycerine. Pain was evaluated using a 10 - cm visual analog scale. Results were analyzed by ANOVA and chi-square tests.
Results:
1- The four groups showed no differences regarding ASA, gender, age, weight and height .(P>0.05
2- Mean and standard deviation of painless time in (B group (268.5 ±59.7 min and (D group (297.7±43.8 min was longer compared with (A group (246.3±4.1 min . (P<0.05
3- There is no differences regarding mean and standard deviation of painless time between:
a (C group (218.5 ± 52.9 min and (A group (246.3 ± 44.1. (P>0.05
b (D group (297.7 ± 43.8 min and (B group (268.5 ± 59.7min. (P>0.05
c (C group (218.5 ± 52.9 min and (B group (268.5 ± 59.7 min. (P>0.05
4- Mean and standard deviation of painless time in (D group (297.7 + 43.8 min was longer compard with (Cgroup (218.5 ± 52.9in. (P<0.05
5-Mean and standard deviation of the pain VAS score was similar among (A group (7.5±1 , (B group (8 ±0.8, (C group (7.2 ± 0.78 and (D group (8 ±0.66. (P>0.05
6- Mean and standard deviation of changes mean blood pressure 5,10,20,30,40,50,60 min after the spinal injection were also the same in all groups. (P>0.05
In this study, respiratory arrest and decrease of consciousness (complicatications of intrathecal opiate was not seen.
Conclusion: In the same previus study in Brazil show that transdermal nitroglycerine significantly prolonged the analgsic effect of spinal sufentani (10
This study was performed in minor operation. (Arthroscopy (10 That did not cause sever tissue trauma and postoperative pain.(2 (10 Our study showed that: Transdermal nitroglycerine has no effect on prolongation of analgesic effect of intrathecal sufentanil. Our study performed in patients with osseous fracture that can cause sever tissue trauma and postoperative pain. (probably reason for this difference Also, our study showed that: Transdermal nitroglycerine alone (5mg/day did not result in postoperative analgesia itself.

P KASHEF

2003-12-01

109

A study on anti-inflammatory and analgesic effects of alkaloids of Toddalia asiatica  

Directory of Open Access Journals (Sweden)

Full Text Available Objective: To study the pharmacological activities and toxicity of the crude alkaloids of Toddalia asiatica and to provide pharmacological data for the further development of this herbal medicine. Methods: We observed the anti-inflammatory effects of the crude alkaloids of Toddalia asiatica, using xylol and agra to induce the turgidness and sodium carboxymethyl cellulose (CMC-Na to induce leucocyte strolling in the rats. The analgesic effects were observed by body-distortion methods. The effects of alkaloids of Toddalia asiatica on hepatic function were observed by testing the contents of alanine aminotransferase (ALT and aspartate aminotransferase (AST in serum and calculating the liver index. The LD50 and 95% creditability were calculated with developed Karber Method. Results: The administration of alkaloids of Toddalia asiatica had the function of inhibiting the auricle swelling caused by xylol and joint swelling caused by agar and leucocyte migration caused by CMC-Na, decreasing the body-distortion of the rats. After two-week administration, the contents of ALT and AST showed that there was no obvious difference between administered group and control group. The LD50 of the crude alkaloids of Toddalia asiatica was 1.622 g/kg and the 95% creditability was 1.29-2.03 g/kg. Conclusion: Toddalia asiatica has anti-inflammatory and analgesic effects, and there is no injury to the liver after long-term administration in rats

HAO Xiao-Yan

2004-11-01

110

Role of serotonin in pathogenesis of analgesic induced headache  

Energy Technology Data Exchange (ETDEWEB)

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)

Srikiatkhachorn, A.

1999-12-16

111

Analgesic and anti-inflammatory effects of ethanol extracted leaves of selected medicinal plants in animal model  

Directory of Open Access Journals (Sweden)

Full Text Available Aim: The research was carried out to investigate the analgesic and anti-inflammatory effects of ethanol extract of Desmodium pauciflorum, Mangifera indica and Andrographis paniculata leaves. Materials and Methods: In order to assess the analgesic and anti-inflammatory effects acetic acid induced writhing response model and carrageenan induced paw edema model were used in Swiss albino mice and Wistar albino rats, respectively. In both cases, leaves extract were administered (2gm/kg body weight and the obtained effects were compared with commercially available analgesic and anti-inflammatory drug Dclofenac sodium (40mg/kg body weight. Distilled water (2ml/kg body weight was used as a control for the study. Results: In analgesic bioassay, oral administration of the ethanol extract of leaves were significantly (p<0.01 reduced the writhing response. The efficacy of leaves extract were almost 35% in Desmodium pauciflorum, 56% in Mangifera indica and 34% in Andrographis paniculata which is found comparable to the effect of standard analgesic drug diclofenac sodium (76%. Leaves extract reduced paw edema in variable percentages but they did not show any significant difference among the leaves. Conclusion: We recommend further research on these plant leaves for possible isolation and characterization of the various active chemical substances which has the toxic and medicinal values. [Vet World 2013; 6(2.000: 68-71

Mohammad M. Hassan

2013-04-01

112

Comparison of Postoperative Analgesic Effect of Tramadol With Lidocaine When Used as Subcutaneous Local Anesthetic  

Directory of Open Access Journals (Sweden)

Full Text Available We conducted a double blind, controlled trial comparing postoperative analgesic effect of tramadol with lidocaine when used as subcutaneous local anesthetic. Seventy ASA physical status 1 or 2 patients aged 20-50 years, who were scheduled for elective surgery under general anesthesia with flank incision, were randomly assigned to receive either 2 mg kg-1 tramadol or 1 mg kg-1 lidocaine at the end of operation. Postoperative pain was evaluated with a Verbal Analogue Scale (VAS. First VAS and patient’s satisfaction with operation were recorded at recovery room, second record was in the ward (12 h later and third on the next day of surgery (24 h later. Local reactions, nausea and vomiting in recovery and the ward and time to first request for analgesic after operation were also recorded. Satisfaction with operation in recovery room was better in tramadol group (p = 0.016. The VAS score did not differ significantly between the two groups in recovery (p = 0.119, 12 h (p = 0.316 and 24 h after the operation (p = 0.108. Time to first analgesic requirement in tramadol group was longer (4.3±0.3 h than lidocaine group (2.1±0.9 h (p = 0.012. Ten patients in tramadol and 2 in lidocaine group had nausea in recovery room (p = 0.01. Eight and three patients had nausea in the ward, respectively (p = 0.101. There was not significant difference in vomiting between two groups in the recovery and the ward (p = 0.106 and p = 0.112, respectively. No local reactions were recorded in either group. This study showed that subcutaneous administration of tramadol provided local anesthesia equal to lidocaine with longer pain-free period after operation.

Sussan Soltanimohammadi

2007-01-01

113

Analgesic effects of naringenin in rats with spinal nerve ligation-induced neuropathic pain.  

Science.gov (United States)

Naringenin, a flavonoid abundant in citrus fruits, such as grapefruits, has been reported to possess anti-inflammatory properties. The present study aimed to investigate the analgesic potential of naringenin in L5 spinal nerve ligation (SNL)-induced peripheral neuropathic pain and the underlying mechanisms associated with neuroinflammation. Different doses of naringenin or saline were administered intrathecally once daily for 11 consecutive days, from 3 days prior to surgery to 7 days after surgery. Pain development was assessed 1 day prior to and 7-14 days after surgery in terms of mechanical withdrawal threshold and thermal withdrawal latency. Astrocytic and microglial activation and production of inflammatory mediators were determined on day 14 after surgery. The results demonstrated that naringenin dose-dependently attenuated the mechanical allodynia and thermal hyperalgesia induced by SNL. Furthermore, naringenin significantly inhibited SNL-induced activation of glial cells (astrocytes and microglia). Morover, the upregulated expression of inflammatory mediators in neuropathic pain was significantly inhibited by naringenin. Our findings suggested that repeated administration of naringenin may alleviate neuropathic pain, possibly through inhibiting neuroinflammation. PMID:24944810

Hu, Chuan Yin; Zhao, Yun-Tao

2014-07-01

114

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

Science.gov (United States)

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

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

2014-01-01

115

Anti-dermatitis, anxiolytic and analgesic effects of Rhazya stricta from Balochistan.  

Science.gov (United States)

Current study was carried out on Rhazya stricta. Plant material was collected from Jhalmagsi Dist. Balochistan, Pakistan. Methanolic extract of Rhazya stricta was tested for anti-dermatitis, analgesic, anxiolytic effects, insecticidal activity and Brine shrimp Bioassay. Crude extract showed significant anti-dermatitis activity, as the results of intensity score showed mild Excoriation or erosion, moderate Edema or populations and absence of Erythema or hemorrhage, Scratching time was decreased to 1.45 and histological observations of mice treated with crude extract showed mild changes and few inflammatory cells in several microscopic fields. The results of analgesic activity were significant and the percentage inhibition of writhes were 73.54% and 69.38% at 300mg/kg and 500mg/kg respectively. The overall response of crude extract in anxiolytic activities were depressive and crude extract showed sedative effects. In Brine shrimp (Artemsia salina) lethality bioassay crude extract showed dose depended significant activity, and showed positive lethality with LD(50) 3.3004?g/ml. Insecticidal activity was positive against Callosbruchus analis, the percent mortality was 40%. PMID:24811805

Ahmad, Mansoor; Muhammed, Shafi; Mehjabeen; Jahan, Noor; Jan, Syed Umer; Qureshi, Zia-Ul-Rehaman

2014-05-01

116

Use of simple tests to determine the residual effects of the analgesic component of balanced anaesthesia.  

Science.gov (United States)

In order to evaluate simple means of determining the rate of recovery after general anaesthesia, the usefulness of the critical flicker fusion threshold test, the Maddox wing apparatus and the visual analogue scale were compared. The postanaesthetic recovery score was used as a reference. Two patient groups (n = 15 in each) received, in a randomized double-blind study, a similar balanced anaesthesia for Caesarean section, except that the analgesic component was either fentanyl 2.5 micrograms kg-1 i.v. or buprenorphine 7.5 micrograms kg-1 i.v. Maddox wing apparatus and visual analogue scale were sensitive enough to differentiate between the postanaesthetic residual effects of the two opioids, but critical flicker fusion threshold and, especially, postanaesthetic recovery score were insensitive in this respect. There was no difference between the two patient groups in mean arterial pressure and heart rate. Our results show that the residual effects of different kinds of opioids as an analgesic component of balanced anaesthesia can be differentiated using simple means like Maddox wing apparatus and visual analogue scales. PMID:3651280

Manner, T; Kanto, J; Salonen, M

1987-08-01

117

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

Science.gov (United States)

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

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

2014-01-01

118

Analgesic Effect of Harpagophytum procumbens on Postoperative and Neuropathic Pain in Rats  

Directory of Open Access Journals (Sweden)

Full Text Available Harpagophytum procumbens, also known as Devil’s Claw, has historically been used to treat a wide range of conditions, including pain and arthritis. The study was designed to investigate whether H. procumbens extracts exhibit analgesic effects in plantar incision and spared nerve injury (SNI rats. The whole procedure was performed on male SD rats. To evaluate pain-related behavior, we performed the mechanical withdrawal threshold (MWT test measured by von Frey filaments. Pain-related behavior was also determined through analysis of ultrasonic vocalization (USVs. The results of experiments showed MWT values of the group that was treated with 300 mg/kg H. procumbens extract increased significantly; on the contrary, the number of 22–27 kHz USVs of the treated group was reduced at 6 h and 24 h after plantar incision operation. After 21 days of continuous treatment with H. procumbens extracts at 300 mg/kg, the treated group showed significantly alleviated SNI-induced hypersensitivity responses by MWT, compared with the control group. These results suggest that H. procumbens extracts have potential analgesic effects in the case of acute postoperative pain and chronic neuropathic pain in rats.

Dong Wook Lim

2014-01-01

119

Analgesic activity of Nyctanthes arbor-tristis leaves in rodents  

Directory of Open Access Journals (Sweden)

Results: The leaf extract of Nyctanthes arbor-tristis produced significant analgesic activity in a dose dependent manner (both peripheral and central at doses 200 mg/kg and 400 mg/kg. But when compared to the standard drugs (aspirin for peripheral analgesia and pethidine for central analgesia the efficacy of the test drug was found to be inferior even at highest dose (400 mg/kg. The onset of action of the test drug was found to be between 30 minutes to one hour and duration of action was up to three hours in central analgesia and significant peripheral analgesia was seen even after four hours of administration of NALE at 400 mg/kg dose. Conclusion: This study demonstrates the potential analgesic effect of Nyctanthes arbor-tristis leaf which supports the claim of traditional medicine practitioners. [J Intercult Ethnopharmacol 2013; 2(2.000: 105-112

Chaitali Pattanayak

2013-04-01

120

Locally mediated analgesic effect of bradykinin type 2 receptor antagonist HOE 140 during acute inflammatory pain in rats.  

Science.gov (United States)

Opioids like morphine form the mainstay of treatment for moderate to severe burn pain. However, lack of dedicated burn care service and potentially serious side effects of opioids often compromise effective treatment. Newer drugs as well as newer routes of administration of analgesic drugs are long-felt needs in the management of burn pain. Bradykinin is a potent inflammatory mediator present at sites of tissue damage. The present study investigated the analgesic effect of bradykinin type 2 receptor antagonist HOE 140 after direct intrawound administration in rats. Also, whether the analgesic effect was locally mediated was further evaluated. Tissue damage was produced by a surgical incision involving skin, fascia, and muscle. It has been reported that there are minor differences in inflammatory mediators underlying incision-related and burn injury-related pain. HOE 140 (1, 3, or 10 ?g/10 ?l physiological saline) was administered into the wound by a sterile micropipette. After an interval of 30 seconds, the wound was closed. HOE 140-induced analgesic effect was compared to other experimental groups of rats which did not receive any drug or those which were treated with either saline (vehicle) or water. Postincisional pain was determined by monitoring behavior, allodynia, and thermal hyperalgesia. Analgesic effect was also determined after drug administration in contralateral paw. HOE 140 (1, 3, 10 ?g) significantly relieved mechanical allodynia and guarding in comparison with vehicle-treated group. The analgesic effect of HOE 140 was locally mediated. Healing of the wound was normal. In conclusion, the results suggest that bradykinin type 2 receptor antagonists such as HOE 140 could be useful in the treatment of acute inflammatory pain. PMID:24451303

George, Jaiben; Pulickal, Sachin Jose; Singh, Anurag; Gautam, Mayank; Prasoon, Pranav; Kumar, Rahul; Ray, Subrata Basu

2014-01-01

121

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

Science.gov (United States)

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

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

2002-04-01

122

Topical analgesics in neuropathic pain.  

Science.gov (United States)

Neuropathic pain can be difficult to treat clinically, as current therapies involve partial effectiveness and significant adverse effects. Following the development of preclinical models for neuropathic pain, significant advances have been made in understanding the neurobiology of neuropathic pain. This includes an appreciation of the molecular entities involved in initiation of pain, the role of particular afferents (small and large diameter, injured and uninjured), and the contribution of inflammation. Currently, topical formulations of capsaicin (cream) and lidocaine (patch) are available for treating neuropathic pain in humans. Preclinical studies provide evidence that peripheral applications of opioids, alpha-adrenergic agents, and antidepressants also may be beneficial in neuropathic pain, and some clinical reports provide support for topical applications of such agents. An appreciation of the ability of drug application, to sites remote from the site of injury, to alleviate aspects of neuropathic pain will provide a significant impetus for the further development of novel topical analgesics for this condition. PMID:16178758

Sawynok, Jana

2005-01-01

123

Evaluation of analgesic effect of tapentadol, a central novel analgesic versus tramadol, a widely used opioid analgesic in treatment of low back pain: a randomized controlled trial  

Directory of Open Access Journals (Sweden)

Full Text Available Background: The objective of the study was to compare efficacy and tolerability (safety of tapentadol with tramadol in the treatment of low back pain. Methods: The study was a prospective, randomized, single blinded, total 102 patients are recruited for study in which 44 patients are prescribed (50mgtwice daily tapentadol and 58 patients prescribed (50mg twice daily tramadol for 4 weeks. Follow-up was done on days 7, 14, 28 and 4 week after stoppage of treatment. Assessment of improvement were performed by Indian Health Assessment Questionnaire Disability Index (Indian HAQDI, Visual Analogue Scale (VAS, Numerical Rating Scale (NRS and measurement of Pain Relief Rate (PRR. Adverse events were recorded. Results: Scores in Indian HAQDI, VAS and NRS improved significantly in both groups in the last visit but more so with tapentadol. PRR was reasonably higher with tapentadol [27(n=4461.36%] patients experiencing significant to complete pain relief at the end of the study, compared to tramadol [25(n=58 43.10%]. Adverse effects was less in tapentadol group [15(n=4434.09%] versus 33(n=5856.89%], p<0.05]. Conclusion: Tapentadol has better sustained efficacy and tolerability than tramadol in low back pain. [Int J Basic Clin Pharmacol 2013; 2(4.000: 392-396

Zaki Anwar Zaman

2013-08-01

124

Analgesic effect of acetaminophen, phenyltoloxamine and their combination in postoperative oral surgery pain.  

Science.gov (United States)

In this factorial study, 148 outpatients with pain after oral surgery were randomly assigned, on a double-blind basis, a single oral dose of acetaminophen 650 mg, phenyltoloxamine 60 mg, a combination of acetaminophen 650 mg with phenyltoloxamine 60 mg, or placebo. Using a self-rating record, subjects rated their pain and its relief hourly for 6 hours after medication. Measures of total and peak analgesia were derived from these subjective reports. The acetaminophen effect was significant for every measure of total and peak analgesia. The phenyltoloxamine effect was not significant for any measure of analgesia. Although efficacy was lower for the acetaminophen-phenyltoloxamine combination than for acetaminophen alone, for every variable, the contrast for interaction was not statistically significant. The results of this study differ from those of previous studies in patients with headache and musculoskeletal pain. All adverse effects were transitory and consistent with the known pharmacologic profiles of the study medications or the backup analgesic. PMID:6483639

Forbes, J A; Barkaszi, B A; Ragland, R N; Hankle, J J

1984-01-01

125

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

Directory of Open Access Journals (Sweden)

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.

Tsuda Yuko

2010-12-01

126

Comparison of Postoperative Analgesic Effect of Dexamethasone and Fentanyl Added to Lidocaine through Axillary Block in Forearm Fracture.  

Science.gov (United States)

Aim. Regional analgesia has been introduced as better analgesic technique compared to using systemic analgesic agents, and it may decrease the adverse effects of them and increase the degree of satisfaction. Several additives have been suggested to enhance analgesic effect of local anesthetic agents such as opioids and steroids. We designed this randomized double-blind controlled study to compare the analgesic efficacy of the dexamethasone and fentanyl added to lidocaine using axillary block in patients undergoing operation of forearm fracture. Materials and Methods. Seventy-eight patients 20-60 years old were recruited in a prospective, double-blinded, randomized way. Axillary block was performed in the three groups by using 40?mL lidocaine and 2?mL distilled water (L group), 40?mL lidocaine and 2?mL dexamethasone (LD group), and 40?mL lidocaine and 2?mL fentanyl (LF group). The onset time of sensory and motor block, duration of sensory and motor block, the total analgesic dose administered during 6 hours after the surgery, and hemodynamic variables were recorded. Results. The duration of sensory and motor block was significantly longer in LD group compared to other groups (P < 0.001). Similarly, the total analgesic consumption in LD group was smaller compared to other groups (P < 0.001). Comparison of hemodynamic consequences of axillary block and surgery failed to reveal any statistically significant differences between all groups. Conclusion. Addition of dexamethasone to lidocaine significantly prolonged the duration of analgesia compared with fentanyl/lidocaine mixture or lidocaine alone using axillary block in patients undergoing forearm fracture surgery. This trial is registered with IRCT2012120711687N1. PMID:24490067

Yaghoobi, Siamak; Seddighi, Mahyar; Yazdi, Zohreh; Ghafouri, Razieh; Khezri, Marzieh Beigom

2013-01-01

127

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

Scientific Electronic Library Online (English)

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

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

2013-06-01

128

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

Directory of Open Access Journals (Sweden)

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.

Frendin J

2002-12-01

129

Effect of sedative-hypnotics, anesthetics and analgesics on sleep architecture in obstructive sleep apnea.  

Science.gov (United States)

The perioperative care of obstructive sleep apnea (OSA) patients is currently receiving much attention due to an increased risk for complications. It is established that postoperative changes in sleep architecture occur and this may have pathophysiological implications for OSA patients. Upper airway muscle activity decreases during rapid eye movement sleep (REMS). Severe OSA patients exhibit exaggerated chemoreceptor-driven ventilation during non-rapid eye movement sleep (NREMS), which leads to central and obstructive apnea. This article critically reviewed the literature relevant to preoperative screening for OSA, prevalence of OSA in surgical populations and changes in postoperative sleep architecture relevant to OSA patients. In particular, we addressed three questions in regard to the effects of sedative-hypnotics, anesthetics and analgesics on sleep architecture, the underlying mechanisms and the relevance to OSA. Indeed, these classes of drugs alter sleep architecture, which likely significantly contributes to abnormal postoperative sleep architecture, exacerbation of OSA and postoperative complications. PMID:25318836

McEntire, Dan M; Kirkpatrick, Daniel R; Kerfeld, Mitchell J; Hambsch, Zakary J; Reisbig, Mark D; Agrawal, Devendra K; Youngblood, Charles F

2014-11-01

130

Analgesic effects of low-dose intravenous orphenadrine in the state of capsaicin hyperalgesia. A randomised, placebo-controlled, double-blind cross-over study using laser somatosensory evoked potentials obtained from capsaicin-irritated skin in healthy volunteers.  

Science.gov (United States)

The present investigation aimed to elucidate the analgesic efficacy of 30 mg of intravenous orphenadrine citrate (CAS 4682-36-4) in a human pain model. Eighteen healthy female and male subjects were enrolled and received single infusions of 30 mg orphenadrine citrate and matching placebo in two periods which were separated by a 1 week washout period. The study was designed as a randomised, double-blind, placebo-controlled, two-period, cross-over trial. The intended neurogenic inflammation and hyperalgesia were induced by topical, occlusive application of 1% capsaicin solution (INCI: Capsicum frutescens, containing capsaicinoides from Capsicum annuum annuum, CAS 84603-55-4) for 30 min on defined skin areas of the back. The pain response to CO2 laser pulses applied to the capsaicin pre-treated skin was measured by event related Vertex-EEG recordings. This technique allowed studying the influence of orphenadrine citrate on the (central) P2-component and the (peripheral) Ni-component of the pain response (LSEP). Both, orphenadrine citrate and placebo were given as intravenous infusions over 60 min. Orphenadrine citrate exerted a significant reduction in central and peripheral components of the pain response when compared to placebo. The effect on the central component was highly significant and more pronounced than the peripheral effect of the drug. The analgesic effect developed fast, was already present during infusion, was ongoing, and exceeded the observational period of 4 h after start of infusion. In summary, orphenadrine citrate was able to exert an analgesic/anti-hyperalgesic effect in a low-dose paradigm (30 mg dose) which was predominantly due to central/spinal mechanisms in this capsaicin model with laser somatosensory evoked potentials. PMID:15553107

Schaffler, Klaus; Reitmeir, Peter

2004-01-01

131

Analgesic and Anti-inflammatory Effects of Rosa damascena Hydroalcoholic Extract and its Essential Oil in Animal Models  

Science.gov (United States)

Extracts obtained from the petals of Rosa damascena (Rosaceae) are used in Iranian folk medicine as remedies for the treatment of some inflammatory diseases. In this study the hydroalcoholic extract and essential oil of the plant were investigated for its possible anti-inflammatory and analgesic activities. The extract was administered at the doses (p.o.) of 250, 500 and 1000 mg/kg and the doses of essential oil were 100, 200 and 400 ?L/kg. The acetic acid-induced writhing response, formalin-induced paw licking time in the early and late phases and light tail flick test were used in mice to assess analgesic activity. For evaluation of anti-inflammatory effect carrageenan-induced paw edema served as a valid animal model in rats. The extract significantly attenuated the writhing responses induced by an intraperitoneal injection of acetic acid and also showed potent analgesic effect in both phases of formalin test but not in light tail flick test. In addition, the higher dose of the extract significantly (P < 0.05) reduced carrageenan-induced paw edema. Essential oil of the plant at all administered doses failed to show any analgesic or anti-inflammatory effect in above mentioned tests. These results provide support for the use of hydroalcoholic extract of Rosa damascena in relieving inflammatory pain, and insight into the development of new agents for treating inflammatory diseases. PMID:24363723

Hajhashemi, Valiollah; Ghannadi, Alireza; Hajiloo, Mohammad

2010-01-01

132

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

DEFF Research Database (Denmark)

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.

Gravesen, Carina; Olesen, SØren S

2012-01-01

133

Bystander effect in ?-irradiated peripheral blood  

International Nuclear Information System (INIS)

Complete text of publication follows. Objective: Radiation-induced bystander effects (ByEff) are still being actively researched since there are more questions than answers related to this phenomenon. There are two main approaches in studying bystander effects: transferring medium from irradiated cells to unirradiated cells and the second is by irradiation of a single cell by a microbeam. The aim of the present study is to investigate and characterize the 'bystander' effect after ?-irradiation of peripheral blood from healthy donors at molecular level. Methods: Three groups of samples: 1) ?-irradiated peripheral blood, 2) non-irradiated blood incubated with plasma from irradiated blood, and 3) additionally irradiated aliquots of the second group, were studied. The Comet Assay and UDS were performed for DNA-damage and repair analysis and lipid peroxidation assay for ROS production. Alamar Blue Microplate assay for cell viability evaluation in the presence of signal transduction pathways inhibitors, mitochondrial membrane potential (MMP) after rhodamine 123 accumulation, and Ca-flux measurements with Fluo 3/Fura Red were performed additionally. In these experiments immortalized human keratinocytes (HaCaT) were used as a reporter cell line. Results: It was established that ByEffs contribute to radiation injury in the case of ?-irradiated whole blood. Significantly higher levels of DNA damage corresponding to decreases in DNA repair capacity were recorded. At a certainir capacity were recorded. At a certain radiation dose DSB levels were higher than SSB levels in the second and third sample groups. Involvement of ByEffs was detected only for the JNK signal transduction pathway. In all cases there was a decrease in MMP and a slight but not significant increase in Fluo3/FuraRed ratio in individual cells treated with irradiated plasma. Conclusion: Incubation with plasma from irradiated blood transforms sub-lethal damage in unirradiated cells into lethal damage and exerts a suppressive effect on DNA repair capacity to additional irradiation. Bystander signals produced by irradiated cells can induce an adaptive response in irradiated cells to a subsequent exposure to bystander signals. Probably, there is involvement of the MAPK signal transduction pathway in the radio-adaptive effects. ROS did not appear to be involved in bystander effects in low dose pre-treated reporter cells but rather take part in sensitizing the bystander cells to additional irradiation. The large individual differences and heterogeneity of bystander responses makes them difficult to be modulated for medical uses at present.

134

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

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: English Abstract in portuguese 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

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

135

Tapentadol hydrochloride: A novel analgesic  

Science.gov (United States)

Tapentadol is a novel, centrally acting analgesic with dual mechanism of action, combining mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule. It has an improved side effect profile when compared to opioids and nonsteroidal anti-inflammatory drugs. The dual mechanism of action makes Tapentadol a useful analgesic to treat acute, chronic, and neuropathic pain. PMID:24015138

Singh, Dewan Roshan; Nag, Kusha; Shetti, Akshaya N.; Krishnaveni, N.

2013-01-01

136

Tapentadol hydrochloride: A novel analgesic.  

Science.gov (United States)

Tapentadol is a novel, centrally acting analgesic with dual mechanism of action, combining mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule. It has an improved side effect profile when compared to opioids and nonsteroidal anti-inflammatory drugs. The dual mechanism of action makes Tapentadol a useful analgesic to treat acute, chronic, and neuropathic pain. PMID:24015138

Singh, Dewan Roshan; Nag, Kusha; Shetti, Akshaya N; Krishnaveni, N

2013-07-01

137

Analgesic, anti-inflammatory and hypoglycaemic effects of Securidaca longepedunculata (Fresen.) [Polygalaceae] root-bark aqueous extract.  

Science.gov (United States)

The present study was undertaken to investigate the analgesic, anti-inflammatory and hypoglycaemic properties of Securidaca longepedunculata (Fresen.) root-bark aqueous extract (SLE) in mice and rats. The analgesic effect of SLE was evaluated by 'hot-plate' and 'acetic acid' analgesic test methods in mice; while its anti-inflammatory and hypoglycaemic effects were examined in rats, using fresh egg albumin-induced pedal oedema, and streptozotocin (STZ)-induced diabetes mellitus models. Morphine (MPN, 10 mg/kg), diclofenac (DIC, 100 mg/kg) and chlorpropamide (250 mg/kg) were used as reference drugs for comparison. SLE (50-800 mg/kg i. p.) produced dose-dependent, significant (p < 0.05-0.001) analgesic effects against thermally- and chemically-induced nociceptive pain in mice. The plant's extract (SLE, 50-800 mg/kg p. o.) also dose-dependently and significantly inhibited (p < 0.05-0.001) fresh egg albumin-induced acute inflammation, and caused significant hypoglycaemia (p < 0.05-0.001) in normal (normoglycaemic) and STZ-treated diabetic (hyperglycaemic) rats. The results of this experimental animal study indicate that S. longepedunculata root-bark aqueous extract (SLE) possesses analgesic, anti-inflammatory and hypoglycaemic properties. These findings lend pharmacological credence to the anecdotal, folkloric and ethnomedical uses of S. longepedunculata root-bark in the treatment, management and/or control of painful, arthritic, inflammatory conditions, as well as in the management and/or control of type 2 diabetes mellitus in some rural communities of South Africa. PMID:18046514

Ojewole, J A O

2008-08-01

138

The application of a penile block before circumcision: effects on the postoperative FLACC score and analgesic requirement  

Directory of Open Access Journals (Sweden)

Full Text Available Objective: We aimed to evaluate the effect of the application of a penile block before circumcision on the postoperative Face, Legs, Activity, Cry, and Consolability (FLACC score and the analgesic requirement.Material and methods: In this study, 240 patients were included, age range 1 to 9 years, between April 2012 and August 2012. A penile block was performed in 125 of the 240 patients (Group 1 and was not performed in 115 of the 240 patients (Group 2. Both groups were compared in terms of age, operation times, FLACC score and analgesic requirement.Results: The mean age of the patients was 4.8±2.1 years in Group 1 and 5.3±3.1 years in group 2 (p=0.126. The mean operation time was 14.9±5.1 min in Group 1 and 15.2±6.2 min in Group 2 (p=0.242. The mean FLACC score of the patients was 3.1±1.9 (0-6 in group 1 and 6.4±3.3 (3-10 in group 2 (p<0.05. There was a postoperative analgesic requirement in 20 patients (16% of Group 1 and 75 patients (65% of Group 2. Early complications were not observed in any patients.Conclusion: We detected a significantly lower postoperative analgesic requirement and a mean FLACC score in patients with the application of a penile block before circumcision.

Sacit Nuri Görgel

2013-03-01

139

Participation of ATP-sensitive K+ channels in the peripheral antinociceptive effect of fentanyl in rats  

Directory of Open Access Journals (Sweden)

Full Text Available We examined the effect of several K+ channel blockers such as glibenclamide, tolbutamide, charybdotoxin (ChTX, apamin, tetraethylammonium chloride (TEA, 4-aminopyridine (4-AP, and cesium on the ability of fentanyl, a clinically used selective µ-opioid receptor agonist, to promote peripheral antinociception. Antinociception was measured by the paw pressure test in male Wistar rats weighing 180-250 g (N = 5 animals per group. Carrageenan (250 µg/paw decreased the threshold of responsiveness to noxious pressure (delta = 188.1 ± 5.3 g. This mechanical hyperalgesia was reduced by fentanyl (0.5, 1.5 and 3 µg/paw in a peripherally mediated and dose-dependent fashion (17.3, 45.3 and 62.6%, respectively. The selective blockers of ATP-sensitive K+ channels glibenclamide (40, 80 and 160 µg/paw and tolbutamide (80, 160 and 240 µg/paw dose dependently antagonized the antinociception induced by fentanyl (1.5 µg/paw. In contrast, the effect of fentanyl was unaffected by the large conductance Ca2+-activated K+ channel blocker ChTX (2 µg/paw, the small conductance Ca2+-activated K+ channel blocker apamin (10 µg/paw, or the non-specific K+ channel blocker TEA (150 µg/paw, 4-AP (50 µg/paw, and cesium (250 µg/paw. These results extend previously reported data on the peripheral analgesic effect of morphine and fentanyl, suggesting for the first time that the peripheral µ-opioid receptor-mediated antinociceptive effect of fentanyl depends on activation of ATP-sensitive, but not other, K+ channels.

A.R.A. Rodrigues

2005-01-01

140

Analgesic effect of low-power infrared laser radiation in rats  

Science.gov (United States)

The aim of the study was to confirm the analgesic effect of low-power laser radiation with a tail-immersion test and check if nitric oxide is involved in laser radiation-induced analgesia in rats. The experiment was performed on male Wistar rats. On the day of experiment the scull of rats was exposed to IR laser radiation for 10 min and antinociceptive effect was determined by means of tail immersion test. The experiments were also performed on 1-NAME and methylene blue pretreated rates, in which both chemicals were administered into right lateral brain ventricle. The results were compared to the ones obtained in the control group in which sham irradiation was made. It was observed that 10 min. exposure to low-power IR laser radiation induced only transient distinct antinociceptive effect in rats. This effect was prevented by ICV. injection of 1-NAME, an inhibitor of nitric oxide synthase and methylene blue, an inhibitor of soluble guanylate cyclase. It seems that nitric oxide is involved in mechanism of low-power laser radiation- induced analgesia.

Mrowiec, Janina; Sieron, Aleksander; Plech, Andrzej; Cieslar, Grzegorz; Biniszkiewicz, Tomasz; Brus, Ryszard

1997-12-01

141

Peripheral nerve extract effects on mesenchymal cells.  

OpenAIRE

Several common congenital limb disorders are characterized by normal tissue differentiation but abnormal somatic growth. These include: idiopathic clubfoot, idiopathic leg length discrepancy, hemi-atrophy and hemi-hypertrophy. Both clinical and research studies have suggested that peripheral nerves may be important in regulating somatic growth of limb tissues. To investigate the hypothesis that peripheral nerves convey trophic substances to mesenchymal tissues that are involved in the regulat...

Dietz, F. R.; Mukhopadhyay, B.; Becker, G.; Daniels, K.; Solursh, M.

1996-01-01

142

Tolerance develops to the antiallodynic effects of the peripherally acting opioid loperamide hydrochloride in nerve-injured rats.  

Science.gov (United States)

Peripherally acting opioids are potentially attractive drugs for the clinical management of certain chronic pain states due to the lack of centrally mediated adverse effects. However, it remains unclear whether tolerance develops to peripheral opioid analgesic effects under neuropathic pain conditions. We subjected rats to L5 spinal nerve ligation (SNL) and examined the analgesic effects of repetitive systemic and local administration of loperamide hydrochloride, a peripherally acting opioid agonist. We found that the inhibition of mechanical hypersensitivity, an important manifestation of neuropathic pain, by systemic loperamide (1.5mg/kg subcutaneously) decreased after repetitive drug treatment (tolerance-inducing dose: 0.75 to 6.0mg/kg subcutaneously). Similarly, repeated intraplantar injection of loperamide (150 ?g/50 ?L intraplantarly) and D-Ala(2)-MePhe(4)-Glyol(5) enkephalin (300 ?g/50 ?L), a highly selective mu-opioid receptor (MOR) agonist, also resulted in decreased inhibition of mechanical hypersensitivity. Pretreatment with naltrexone hydrochloride (5mg/kg intraperitoneally) and MK-801 (0.2mg/kg intraperitoneally) attenuated systemic loperamide tolerance. Western blot analysis showed that repetitive systemic administration of morphine (3mg/kg subcutaneously), but not loperamide (3mg/kg subcutaneously) or saline, significantly increased MOR phosphorylation in the spinal cord of SNL rats. In cultured rat dorsal root ganglion neurons, loperamide dose-dependently inhibited KCl-induced increases in [Ca(2+)]i. However, this drug effect significantly decreased in cells pretreated with loperamide (3 ?M, 72 hours). Intriguingly, in loperamide-tolerant cells, the delta-opioid receptor antagonist naltrindole restored loperamide's inhibition of KCl-elicited [Ca(2+)]i increase. Our findings indicate that animals with neuropathic pain may develop acute tolerance to the antiallodynic effects of peripherally acting opioids after repetitive systemic and local drug administration. PMID:23880055

He, Shao-Qiu; Yang, Fei; Perez, Federico M; Xu, Qian; Shechter, Ronen; Cheong, Yong-Kwan; Carteret, Alene F; Dong, Xinzhong; Sweitzer, Sarah M; Raja, Srinivasa N; Guan, Yun

2013-11-01

143

Analgesic activity of Justicia beddomei leaf extract  

OpenAIRE

The analgesic activity of ethanolic extract of Justicia beddome leaves (Family: Acanthaceae) was evaluated in albino rats using Eddy's hot plate method. The extract at 50 and 100 mg/ kg, (i.p), showed significant analgesic activity at 90 minutes of administration. The analgesic effect of the extract was comparable to that of morphine sulphate.

Srinivasa, U.; Rao, J. Venkateshwara; Krupanidhi, A. M.; Shanmukhappa, S.

2007-01-01

144

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

Science.gov (United States)

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

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

2012-12-01

145

Analgesic and anti-hyperalgesic effects of epidural morphine in an equine LPS-induced acute synovitis model  

OpenAIRE

Epidural morphine is widely used in veterinary medicine, but there is no information about the antihyperalgesic and anti-inflammatory effects in acute inflammatory joint disease in horses. The analgesic, anti-hyperalgesic and anti-inflammatory effects of epidural morphine (100 mg/animal or 0.17 ± 0.02 mg/ kg) were therefore investigated in horses with acute synovitis. In a cross-over study, synovitis was induced in the talocrural joint by intra-articular lipopolysaccharide (LPS)....

Loon, J. P. A. M.; Menke, E. S.; L Ami, J. J.; Jonckheer-sheehy, V. S. M.; Back, W.; Weeren, P. R.

2012-01-01

146

The analgesic effect of electroacupuncture on acute thermal pain perception-a central neural correlate study with fMRI  

OpenAIRE

Abstract Background Electrical acupuncture (EA) has been utilized in acute pain management. However, the neuronal mechanisms that lead to the analgesic effect are still not well defined. The current study assessed the intensity [optimal EA (OI-EA) vs. minimal EA (MI-EA)] effect of non-noxious EA on supraspinal regions related to noxious heat pain (HP) stimulation utilizing an EA treatment protocol for acute pain and functional magnetic resonance imaging (fMRI) with correlatio...

Leung Albert; Duann Jeng-Ren; Torossian Artour; Shukla Shivshil

2011-01-01

147

Percutaneous neuromodulation therapy: does the location of electrical stimulation effect the acute analgesic response?  

Science.gov (United States)

We studied the effect of the location of electrical stimulation on the acute analgesic response to percutaneous neuromodulation therapy in patients with nonradiating neck pain. Sixty-eight patients received three different nonpharmacologic modalities, namely "needles only" (neck), local (neck) dermatomal stimulation, and remote (lower back) dermatomal stimulation in a random sequence over the course of an 11-wk study period. All treatments were given for 30 min, 3 times per week for 3 wk, with 1 wk "off" between each modality. The assessment tools included the health status survey short form (SF-36) questionnaire, as well as 10-cm visual analog scales for assessing pain, physical activity, and quality of sleep. The pain visual analog scale was repeated 5-10 min after each treatment session. The daily oral nonopioid analgesic requirements were recorded in the patient diary during the entire study period. At the end of each 3-wk treatment block, the SF-36 questionnaire was repeated. Compared with needles only and remote dermatomal stimulation, local dermatomal stimulation produced a significantly greater decrease in pain (38%+/-17% vs 9%+/- 16% and 13%+/-18%), increase in physical activity (41%+/-21% vs 11% +/-17% and 16%+/-15%), and improvement in the quality of sleep (34% +/-18% vs 7%+/-17% and 10%+/-18%) compared with baseline values (Premote dermatomal stimulation, respectively. The posttreatment SF-36 test results revealed that all three modalities produced improvements compared with the prestudy scores for both the physical component summary and mental component summary. However, the magnitude of the changes in the physical component summary and mental component summary with local dermatomal stimulation was significantly greater (+7.9 and +3.6, respectively) than needle only (+3.4 and +1.7, respectively) or remote dermatomal stimulation (+3.7 and +1.9, respectively). No side effects were reported at the needle insertion sites. We conclude that electrical stimulation at the specific dermatomal levels corresponding to the local pathology produces greater short-term improvements in pain control, physical activity, and quality of sleep in patients with chronic neck pain. PMID:11004055

White, P F; Craig, W F; Vakharia, A S; Ghoname, E; Ahmed, H E; Hamza, M A

2000-10-01

148

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)

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.

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

2012-09-01

149

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

DEFF Research Database (Denmark)

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 

GrØnbæk, Anni Birgitte; Svensson, Peter

2014-01-01

150

Analgesic, Anxiolytic and Anaesthetic Effects of Melatonin: New Potential Uses in Pediatrics  

Science.gov (United States)

Exogenous melatonin is used in a number of situations, first and foremost in the treatment of sleep disorders and jet leg. However, the hypnotic, antinociceptive, and anticonvulsant properties of melatonin endow this neurohormone with the profile of a drug that modulates effects of anesthetic agents, supporting its potential use at different stages during anesthetic procedures, in both adults and children. In light of these properties, melatonin has been administered to children undergoing diagnostic procedures requiring sedation or general anesthesia, such as magnetic resonance imaging, auditory brainstem response tests and electroencephalogram. Controversial data support the use of melatonin as anxiolytic and antinociceptive agents in pediatric patients undergoing surgery. The aim of this review was to evaluate available evidence relating to efficacy and safety of melatonin as an analgesic and as a sedative agent in children. Melatonin and its analogs may have a role in antinociceptive therapies and as an alternative to midazolam in premedication of adults and children, although its effectiveness is still controversial and available data are clearly incomplete. PMID:25569095

Marseglia, Lucia; D’Angelo, Gabriella; Manti, Sara; Aversa, Salvatore; Arrigo, Teresa; Reiter, Russel J.; Gitto, Eloisa

2015-01-01

151

Effect of analgesics and their derivatives on antibiotic resistance of environmental microbes.  

Science.gov (United States)

This research is a preliminary study conducted to determine the effects of aspirin (acetyl-salicylic acid) and salicylic acid (analgesics and their derivatives) on the antibiotic resistance of ammonia oxidizing bacterium (AOB) (a non-pathogenic environmental microbe) cultured from the Texas Tech University-Water Recovery System that treats a space related wastewater for NASA. The effect of salicylic acid was investigated by obtaining the minimal inhibition concentration (MIC) of antibiotics (amoxicillin, ciprofloxacin, and nalidixic acid) in the presence of aspirin and salicylic acid. The possibility of transfer of resistance genes between unrelated species was investigated by analyzing the similarity of the AcrA protein (a multi-drug efflux protein) in Nitrosomonas europaea, Escherichia coli and Salmonella enterica. The protein alignment analysis was done using ExPASy, a proteomics tool. The results of this preliminary study indicated that the antibiotic resistance of AOBs increased in the presence of aspirin and salicylic acid and similarities in the AcrA protein of different species indicated the likelihood of possible resistance transfer between the species. This paper high lights the importance of research and further investigation on antibiotic resistance and resistance transfer, highlighting the number of parameters that should be considered while assessing antibiotic resistance in environmental samples. PMID:19448319

Dhanapal, L P; Morse, A N

2009-01-01

152

Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations.  

Science.gov (United States)

The aim of this study was to evaluate the potential application of microemulsions as a transdermal drug delivery for naproxen (Np). The pseudo-ternary phase diagrams were developed for microemulsions composed of isopropyl myristate, Span 80, Labrafil M, Labrasol, and Cremophor EL, ethanol and isopropyl alcohol and 0.5N sodium hydroxide. The final concentration of Np in microemulsion systems was 10% (w/w). The microemulsions were characterised by conductivity, droplet size, viscosity and pH. Moreover, in vitro permeability studies were performed using diffusion cells from rat skin. The permeation rates of Np from microemulsions (M1(Np) and M2(Np)) were higher than the commercial (C) gel formulation. The paw oedema test was performed in rats to evaluate the anti-inflammatory activity of Np. The volume increase in paw oedema after 6hr was 0.71±0.46% with M2(Np), whereas M1(Np) and C exhibited 6.48±2.71% and 14.97±3.15% increases in oedema, respectively. Additionally, a significant analgesic effect was detected in the hot plate and tail-flick tests for all test microemulsion and C formulations when compared with the control. Histopathological examination of the treated skin was performed to investigate changes in skin morphology. In conclusion, the microemulsion formulations, especially the M2(Np) formulation, may be used as an effective alternative for the transdermal delivery of Np. PMID:21723930

Ustünda? Okur, Neslihan; Apayd?n, Sebnem; Karabay Yava?o?lu, N Ülkü; Yava?o?lu, Altu?; Karasulu, H Ye?im

2011-09-15

153

Analgesic, Anxiolytic and Anaesthetic Effects of Melatonin: New Potential Uses in Pediatrics  

Directory of Open Access Journals (Sweden)

Full Text Available Exogenous melatonin is used in a number of situations, first and foremost in the treatment of sleep disorders and jet leg. However, the hypnotic, antinociceptive, and anticonvulsant properties of melatonin endow this neurohormone with the profile of a drug that modulates effects of anesthetic agents, supporting its potential use at different stages during anesthetic procedures, in both adults and children. In light of these properties, melatonin has been administered to children undergoing diagnostic procedures requiring sedation or general anesthesia, such as magnetic resonance imaging, auditory brainstem response tests and electroencephalogram. Controversial data support the use of melatonin as anxiolytic and antinociceptive agents in pediatric patients undergoing surgery. The aim of this review was to evaluate available evidence relating to efficacy and safety of melatonin as an analgesic and as a sedative agent in children. Melatonin and its analogs may have a role in antinociceptive therapies and as an alternative to midazolam in premedication of adults and children, although its effectiveness is still controversial and available data are clearly incomplete.

Lucia Marseglia

2015-01-01

154

Peripheral and central effects of circulating catecholamines.  

Science.gov (United States)

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. © 2015 American Physiological Society. Compr Physiol 5: 1-15, 2015. PMID:25589262

Tank, A William; Lee Wong, Dona

2015-01-01

155

Visceral analgesic effect of 5-HT4 receptor agonist in rats involves the rostroventral medulla (RVM)  

Science.gov (United States)

The 5-HT4 receptor agonist tegaserod (TEG) has been reported to modulate visceral pain. However, the underlying mechanism remains unknown. The objective of the present study was to examine the analgesic mechanism and site of action of TEG. In male rats, visceral pain was assessed by measuring visceromotor response (VMR) to colorectal distension (CRD). Inflammation was induced by intracolonic injection of tri-nitrobenzene sulfonic acid (TNBS). The effect of TEG on the VMR was tested by injecting intraperitoneal (i.p.), intrathecal (i.t.), intracerebroventricular (i.c.v) or in the rostroventral medulla (RVM). The effect of the drug was also tested on responses of CRD-sensitive pelvic nerve afferents (PNA) and lumbo-sacral (LS) spinal neurons. Systemic injection of TEG attenuated VMR in naive and TNBS-treated rats. Similarly, supraspinal, but not spinal, injection of TEG attenuated the VMR. While GR113808, (selective 5-HT4 antagonist) blocked the effect, naloxone (NLX) an opioid receptor antagonist reversed the effect of TEG. Although i.t. NLX did not block the inhibitory effect of TEG in VMR study, i.t. injection of ?2-adrenergic receptor antagonist yohimbine blocked the effect of TEG when given systemically. While TEG had no effect on the responses of CRD-sensitive PNA, it inhibited the responses of CRD-sensitive LS neurons in spinal intact condition. This inhibition was blocked by GR113808, NLX and ?-funaltrexamine (?-FNA) when injected into the RVM. Results indicate that TEG produces analgesia via activation of supraspinal 5-HT4 receptors which triggers the release of opioids at supraspinal site, which activates descending noradrenergic pathways to the spinal cord to produce analgesia. PMID:24334068

Sengupta, Jyoti N.; Mickle, Aaron; Kannampalli, Pradeep; Spruell, Russell; McRorie, John; Shaker, Reza; Miranda, Adrian

2015-01-01

156

[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)

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

Siegmeth, W; Bröll, H; Schragl, F

1984-11-30

157

ANALGESIC AND ANTI INFLAMMATORY EFFECT OF LEECH THERAPY (JALAUKAVCHARAN IN THE PATIENTS OF OSTEOARTHRITIS (SANDHIGATA VATA  

Directory of Open Access Journals (Sweden)

Full Text Available Osteoarthritis (degenerative joint disease is the most common joint disorder. It mostly affects cartilage. The top layer of cartilage breaks down and wears away. Osteoarthritis is of two types, primary (idiopathic and secondary. In idiopathic osteoarthritis, the most common form of the disease, no predisposing factor is apparent. Secondary OA is pathologically indistinguishable from idiopathic OA but is attributable to an underlying cause. The NSAID’S are main drug of choice in modern medicine which have lots of side effect therefore are not safe for long term therapy. Raktamokshan viz bloodletting is one of the ancient and important parasurgical procedure described in Ayurveda for treatment of various diseases. Of them, Jalaukavacharana or Leech Therapy has gained greater attention globally, because of its medicinal values. The saliva of leech contains numerous biologically active substances, which has anti-inflammatory, analgesic as well as anesthetic property. Keeping this view in mind we have started leech therapy in the patients of osteoarthritis and found encouraging results.

Singh Akhilesh Kumar

2012-02-01

158

Characterization of Novel Cannabinoid Based T-Type Calcium Channel Blockers with Analgesic Effects.  

Science.gov (United States)

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

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

2014-11-01

159

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

Science.gov (United States)

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 Cats receiving nerve blocks had lower postoperative pain scores than the group without nerve blocks. PMID:24820999

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

2015-02-01

160

Assessment of the Analgesic Effects of Extrapleural Infusion of Ropivacaine in Neonates with Esophageal Atresia (EA) Repair  

OpenAIRE

Insufficient control of post-thoracotomy pain can produce breathing dysfunction and long term staying in neonatal intensive care unit (NICU). It can increase the incidence of pulmonary complications such as atelectasis, pneumonia and respiratory failure. The aim of this study was to determine the analgesic effect of continuous extrapleural nerve block, using ropivacaine, in neonates younger than 7 days old with esophageal atersia (EA) and the incidence of atelectasis and duration of hospitali...

Rouzrokh, Mohsen; Mirkheshti, Alireza; Mirshemirani, Alireza; Sadeghi, Afsaneh; Tavassoli, Azita; Khaleghnejad Tabari, Ahmad

2010-01-01

161

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

OpenAIRE

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...

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

2008-01-01

162

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

Directory of Open Access Journals (Sweden)

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.

Yu Liu

2014-08-01

163

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)

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

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

164

Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties.  

Science.gov (United States)

In the present study, an efficient synthesis of some Mannich base of 5-methyl-2-[(2-oxo-2H-chromen-3-yl)carbonyl]-2,4-dihydro-3H-pyrazol-3-one (4a-j) have been described by using conventional and non-conventional (microwave) techniques. Microwave assisted reactions showed that require shorter reaction time and good yield. The newly synthesized compounds were screened for their anti-inflammatory, analgesic activity, antioxidant, and antibacterial effects were compared with standard drug. Among the compounds studied, compound (4f) showing nearly equipotent anti-inflammatory and analgesic activity than the standard drug (indomethacin), along with minimum ulcerogenic index. Compounds (4b and 4i) showing 1.06 times more active than ciprofloxacin against tested Gram-negative bacteria. PMID:24835630

Sivakumar, Kullampalayam Krishnasamy; Rajasekaran, Aiyalu; Senthilkumar, Palaniappan; Wattamwar, Prasad P

2014-07-01

165

Analgesic and Anti-Inflammatory Effects of Ethanolic Root Extract of Hippocratea africana  

Directory of Open Access Journals (Sweden)

Full Text Available The ethanolic root extract of Hippocratea africana (200-600 mg kg-1 was evaluated for analgesic, anti-inflammatory and antipyretic properties. The extract dose dependently inhibited acetic acid-induced writhing, formalin-induced paw licking and thermally -induced pain in mice. The extract also inhibited fresh egg albumin, carrageenin and xylene-induced inflammation in mice. These inhibitions were statistically significant (p<0.05 when compared to control. The roots extracts was also found to reduce pyrexia in rats. The analgesic, anti-inflammatory and antipyretic activities of the extract may be related to its active constituents such as tannins, saponins, steroid and flavonoids.

Jude E. Okokon

2008-01-01

166

Analgesic and Anti-inflammatory Effects of Rosa damascena Hydroalcoholic Extract and its Essential Oil in Animal Models.  

Science.gov (United States)

Extracts obtained from the petals of Rosa damascena (Rosaceae) are used in Iranian folk medicine as remedies for the treatment of some inflammatory diseases. In this study the hydroalcoholic extract and essential oil of the plant were investigated for its possible anti-inflammatory and analgesic activities. The extract was administered at the doses (p.o.) of 250, 500 and 1000 mg/kg and the doses of essential oil were 100, 200 and 400 ?L/kg. The acetic acid-induced writhing response, formalin-induced paw licking time in the early and late phases and light tail flick test were used in mice to assess analgesic activity. For evaluation of anti-inflammatory effect carrageenan-induced paw edema served as a valid animal model in rats. The extract significantly attenuated the writhing responses induced by an intraperitoneal injection of acetic acid and also showed potent analgesic effect in both phases of formalin test but not in light tail flick test. In addition, the higher dose of the extract significantly (P Rosa damascena in relieving inflammatory pain, and insight into the development of new agents for treating inflammatory diseases. PMID:24363723

Hajhashemi, Valiollah; Ghannadi, Alireza; Hajiloo, Mohammad

2010-01-01

167

STUDIES OF ANTI INFLAMMATORY, ANTIPYRETIC AND ANALGESIC EFFECTS OF AQUEOUS EXTRACT OF TRADITIONAL HERBAL DRUG ON RODENTS  

Directory of Open Access Journals (Sweden)

Full Text Available Aqueous extract of combination of stems of Tinospora cordifolia, fruits of Emblica officinalis and rhizomes of Cyperus rotundus has been used as traditional herbal drug in Indian medicine system for treatment of fever, body ache, joint pain and inflammation. The collected botanicals were subject to physiochemical, pharmacognostical & phytochemical screening before animal experiments. After acute toxicity studies, anti-inflammatory effect was assessed using carrageen induced paw oedema test and antipyretic effect using yeast induced pyrexia method. Tail immersion, hot plate and writhings test were used for determining the analgesic properties. Phytochemical analysis revealed the presence of polyphenolic flavonoids, tannin and saponins. Significant anti-inflammatory, antipyretic and analgesic properties were noticed in dose dependant manner after aqueous extract administration especially at 600 mg/kg dose. These test drug activities were sustained and comparable to the standard drugs while exhibiting no acute toxicity. Aqueous extract of test drug possesses significantly high anti-inflammatory, antipyretic and analgesic properties without any acute toxicity possibly due to presence of flavonoids.

Gupta Mradu

2013-03-01

168

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

Directory of Open Access Journals (Sweden)

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.

Murat Ayan

2013-01-01

169

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

Directory of Open Access Journals (Sweden)

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.

H.P. Aithal

2012-07-01

170

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

Directory of Open Access Journals (Sweden)

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.

R. DeRossi

2012-06-01

171

Preoperative education and use of analgesic before onset of pain routinely for post-thoracotomy pain control can reduce pain effect and total amount of analgesics administered postoperatively.  

Science.gov (United States)

The purpose of this study was to investigate the efficiency of preoperative pain management education and the role of analgesics administration before the onset of pain postoperatively. The study was a prospective, randomized, and single-blind clinical trial, which was conducted January 1, 2008 through October 1, 2008 in the Thoracic Surgery Unit of Akdeniz University Hospital. A total of 70 patients who underwent thoracotomy (35 in the control group and 35 in the study group) were included in the study. Of the patients, 70% (n = 49) were male and 30% (n = 21) were female. Mean age was 51 ± 10 years (range = 25-65). The same analgesia method was used for all patients; the same surgical team performed each operation. Methods, including preemptive analgesia and placement of pleural or thoracic catheter for using analgesics, that were likely to affect pain level, were not used. The same analgesia medication was used for both patient groups. But the study group, additionally, was educated on how to deal with pain preoperatively and on the pharmacological methods to be used after surgery. An intramuscular diclofenac Na 75 mg was administered to the study group regardless of whether or not they reported pain in the first two postoperative hours. The control group did not receive preoperative education, and analgesics were not administered to them unless they reported pain in the postoperative period. The routine analgesics protocol was as follows: diclofenac Na 75 mg (once a day) intramuscular administered upon the complaint of pain following extubation in the postoperative period and 20 mg mepederin intravenously (maximum dose, 100 mg/day), in addition, when the patient expressed pain. Pain severity was assessed during the second, fourth, eighth, 16th, 24th, and 48th hours, and marked using the Verbal Category Scale and the Behavioral Pain Assessment Scale. Additionally, the total dose of daily analgesics was calculated. The demographic characteristics showed a homogeneous distribution in both patient groups. The rate of pain, which was defined as sharp, stabbing, and exhausting, was higher in the control group than in the study group, and the difference between the two groups was statistically significant (p onset of pain, reduced the amount of analgesics used in the first postoperative 48 hours. PMID:23485658

Kol, Emine; Alpar, Sule Ecevit; Erdo?an, Abdullah

2014-03-01

172

A novel method for detecting the analgesic effect of drugs by quantifying body movement after noxious stimulation in neonatal rat.  

Science.gov (United States)

We developed a method for quantifying nociceptive struggling in neonatal rats induced by bolus, subcutaneous injection of capsaicin (3-3000 ng). The response was quantified by using an audio speaker and electrical instruments such as an amplifier, a rectifier, and a monostable multivibrator. Using this method, we were able to quantify the nociceptive response which appeared immediately after injection of capsaicin. The response peaked at 0-1 min, and then decayed during next 1-3 min. Furthermore, this method also detected that the magnitude of the response increased dose-dependently up to the maximum dose of 3000 ng. In an experiment testing the suitability of this method for screening analgesics, it was shown that morphine (0.03-0.3 mg/kg, s.c.) inhibited the response dose-dependently with an ID50 value of 0.089 mg/kg and that the analgesic effect of morphine (1 mg/kg, s.c.) was reversed by naloxone (0.03-0.1 mg/kg, s.c.). Thus it can be concluded that this method is useful to quantify the capsaicin-induced nociceptive response and is suitable for screening analgesics. PMID:9920532

Kubota, K; Takahashi, T; Yanagisawa, M; Fujibayashi, K; Saito, K

1998-07-01

173

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

DEFF Research Database (Denmark)

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 cross-over 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. This article is protected by copyright. All rights reserved.

Graversen, Carina; Malver, Lasse P

2014-01-01

174

Induction of anesthesia in coronary artery bypass graft surgery: the hemodynamic and analgesic effects of ketamine  

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: English Abstract in english OBJECTIVE: The aim of this prospective, randomized study was to evaluate the hemodynamic and analgesic effects of ketamine by comparing it with propofol starting at the induction of anesthesia until the end of sternotomy in patients undergoing coronary artery bypass grafting surgery. INTRODUCTION: A [...] nesthetic induction and maintenance may induce myocardial ischemia in patients with coronary artery disease. A primary goal in the anesthesia of patients undergoing coronary artery bypass grafting surgery is both the attenuation of sympathetic responses to noxious stimuli and the prevention of hypotension. METHODS: Thirty patients undergoing coronary artery bypass grafting surgery were randomized to receive either ketamine 2 mg.kg-1 (Group K) or propofol 0.5 mg.kg-1 (Group P) during induction of anesthesia. Patients also received standardized doses of midazolam, fentanyl, and rocuronium in the induction sequence. The duration of anesthesia from induction to skin incision and sternotomy, as well as the supplemental doses of fentanyl and sevoflurane, were recorded. Heart rate, mean arterial pressure, central venous pressure, pulmonary arterial pressure, pulmonary capillary wedge pressure, cardiac index, systemic and pulmonary vascular resistance indices, stroke work index, and left and right ventricular stroke work indices were obtained before induction of anesthesia; one minute after induction; one, three, five, and ten minutes after intubation; one minute after skin incision; and at one minute after sternotomy. RESULTS: There were significant changes in the measured and calculated hemodynamic variables when compared to their values before induction. One minute after induction, mean arterial pressure and the systemic vascular resistance index decreased significantly in group P (p

Elif, Basagan-Mogo; Suna, Goren; Gulsen, Korfali; Gurkan, Turker; Fatma Nur, Kaya.

175

Anti-hyperalgesic effects of calcitonin on neuropathic pain interacting with its peripheral receptors  

Directory of Open Access Journals (Sweden)

Full Text Available Abstract Background The polypeptide hormone calcitonin is clinically well known for its ability to relieve neuropathic pain such as spinal canal stenosis, diabetic neuropathy and complex regional pain syndrome. Mechanisms for its analgesic effect, however, remain unclear. Here we investigated the mechanism of anti-hyperalgesic action of calcitonin in a neuropathic pain model in rats. Results Subcutaneous injection of elcatonin, a synthetic derivative of eel calcitonin, relieved hyperalgesia induced by chronic constriction injury (CCI. Real-time reverse transcriptase-polymerase chain reaction analysis revealed that the CCI provoked the upregulation of tetrodotoxin (TTX-sensitive Nav.1.3 mRNA and downregulation of TTX-resistant Nav1.8 and Nav1.9 mRNA on the ipsilateral dorsal root ganglion (DRG, which would consequently increase the excitability of peripheral nerves. These changes were reversed by elcatonin. In addition, the gene expression of the calcitonin receptor and binding site of 125I-calcitonin was increased at the constricted peripheral nerve tissue but not at the DRG. The anti-hyperalgesic effect and normalization of sodium channel mRNA by elcatonin was parallel to the change of the calcitonin receptor expression. Elcatonin, however, did not affect the sensitivity of nociception or gene expression of sodium channel, while it suppressed calcitonin receptor mRNA under normal conditions. Conclusions These results suggest that the anti-hyperalgesic action of calcitonin on CCI rats could be attributable to the normalization of the sodium channel expression, which might be exerted by an unknown signal produced at the peripheral nerve tissue but not by DRG neurons through the activation of the calcitonin receptor. Calcitonin signals were silent in the normal condition and nerve injury may be one of triggers for conversion of a silent to an active signal.

Ito Akitoshi

2012-06-01

176

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

177

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

OpenAIRE

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...

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

2004-01-01

178

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

Directory of Open Access Journals (Sweden)

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.

M. Mohajer

2006-01-01

179

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

Directory of Open Access Journals (Sweden)

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.

Seliškar Alenka

2005-01-01

180

Comparison of analgesic effects of nimesulide, paracetamol, and their combination in animal models  

OpenAIRE

Objectives: To compare the analgesic activity of nimesulide and paracetamol alone and their combination in animal models for the degree of analgesia and the time course of action. Materials and Methods: Analgesia was studied in albino rats using formalin test and in albino mice using writhing test and the radiant heat method. For each test, four groups of six animals each were orally fed with a single dose of nimesulide, paracetamol, and combination of nimesulide + parac...

Ahmed Mushtaq; Upadhyaya Prerna; Seth Vikas

2010-01-01

181

Relevancia clínica de las acciones tópicas de los opioides / Clinical relevance of peripheral opioid effects  

Scientific Electronic Library Online (English)

Full Text Available SciELO Colombia | Language: Spanish Abstract in spanish Se trata de una práctica frecuente en algunos centros, es aún poca la evidencia que justifica el uso de formulaciones tópicas a base de un enfoque local en el tratamiento analgésico de condiciones dolorosas consiste en aplicar medicamentos localmente en el sitio de origen del dolor. Esto puede alcan [...] zarse mediante la aplicación tópica de una crema, loción, gel, aerosol o parche para sitios somáticos o mediante la utilización de enjuagues en el caso de lesiones de la mucosa oral. Estos métodos de aplicación permiten una mayor concentración local del fármaco en el sitio de iniciación del dolor y disminuye los niveles sistémicos del fármaco a niveles mínimos o insignificantes, teóricamente disminuyendo el riesgo de efectos adversos sistémicos. El presente artículo pretende revisar información clínica y preclínica relevante para la prescripción de opioides tópicos. (MÉD.UIS. 2014;27:(2)59-65) Abstract in english Although it is a common practice in some centers, there is still little evidence that validates the use of topical analgesic formulations based on opioids for treatment painful skin and mucous conditions. A local focus on the analgesic treatment of painful conditions consists of applying drugs direc [...] tly in the peripheral site of pain origin. This can be achieved through the topical application of a cream, lotion, gel, spray or patch for somatic sites or through the use of mouthwash in the case of lesions of the oral mucosa. These methods allow a greater local concentration of the drug at the painful site and decrease the systemic levels of the medication to minimum or negligible levels, theoretically reducing the risk of systemic adverse effects. This article aims to review relevant clinical and preclinical information on topical opioid prescribing. (MÉD.UIS. 2014;27:(2)59-65)

Gabriel, Carvajal Valdy.

2014-08-01

182

A comparison of the analgesic effects of butorphanol with those of meloxicam after elective ovariohysterectomy in dogs  

OpenAIRE

This study was designed to compare the analgesic effects of butorphanol with those of meloxicam following ovariohysterectomy. Fifteen dogs were premedicated with 0.05 mg/kg body weight (BW) of acepromazine by intramuscular (IM) injection, plus 0.2 mg/kg BW of meloxicam by subcutaneous (SC) injection. Fifteen dogs were premedicated with 0.05 mg/kg BW of Acepromazine, IM, plus 0.2 mg/kg BW of butorphanol, IM. Anesthesia was induced with thiopental, and dogs were maintained on halothane. All pai...

Caulkett, Nigel; Read, Matt; Fowler, David; Waldner, Cheryl

2003-01-01

183

Clinical efficacy of antihistaminics as analgesics.  

Science.gov (United States)

This paper reviews the clinical information on antihistaminic agents as analgesics and as analgesic adjuvants. The evidence indicates a direct analgesic effect of various antihistaminics. In clinical studies, diphenhydramine, hydroxyzine, orphenadrine and pyrilamine have been shown to produce analgesia as simple entities but chlorpheniramine has not and results with phenyltoloxamine have been equivocal when tested alone. Analgesic adjuvant effects of several antihistaminics have been reported. Clinically, orphenadrine and phenyltoloxamine have shown adjuvant effects with acetaminophen and aspirin. The mechanism of action remains speculative. The most recent trends in the classification of histamine receptors and how these receptors may interact with pain modulation are also considered. PMID:2872645

Rumore, M M; Schlichting, D A

1986-04-01

184

Antinociceptive effects of S(+)-ketoprofen and other analgesic drugs in a rat model of pain induced by uric acid.  

Science.gov (United States)

We investigated the antinociceptive properties of dexketoprofen trometamol [S(+)-ketoprofen tromethamine salt; SKP], a new analgesic, antiinflammatory drug, using the pain-induced functional impairment model in the rat (PIFIR), an animal model of arthritic pain. SKP was compared with racemic ketoprofen tromethamine salt (rac-KP), R(-)-ketoprofen tromethamine salt (RKP), ketorolac (KET), and morphine (MOR). We also assessed the effects of flurbiprofen (rac-FB) and its enantiomers (SFB and RFB) in the same model. Groups of six rats received either vehicle or analgesic drug and antinociception was evaluated by evaluating the dose-response curves over time. SKP was an effective antinociceptive drug in this model and was almost equally potent by either oral or intracerebroventricular administration. The oral potency of SKP was similar to that of oral KET and greater than that of oral MOR. No significant differences were observed between racemic ketoprofen and its enantiomers when administered orally. In the rat, significant bioinversion of RKP to SKP occurs when RKP is given orally. After oral administration of RKP, SKP was detectable in 30 min and surpassed the concentration of RKP after 3 h. Nevertheless, when the compounds were given intracerebroventricularly, some stereoselectivity in favor of SKP was observed. Stereoselectivity was observed with flurbiprofen, an analogue of ketoprofen that does not undergo significant metabolic inversion. Whereas SFB was an effective antinociceptive, RFB had no antinociceptive effect at the doses tested when given either orally or intracerebroventricularly. PMID:9882077

López-Muñoz, F J; Ventura, R; Díaz, I; Fernández-Guasti, A; Tost, D; Cabré, F; Mauleón, D

1998-12-01

185

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)

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.

Pedro Barzaga Fernández

2005-04-01

186

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)

Full Text Available SciELO Cuba | Language: Spanish Abstract in spanish 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.

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

187

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

Science.gov (United States)

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 onset of the disease. NDI10218 reduced the arthritis index and blocked the synovial hyperplasia in a dose-dependent manner. The serum levels of pro-inflammatory cytokines TNF-?, IL-6, and IL-1? were significantly reduced in mice treated with NDI10218. Production of the inflammatory IL-17, but not immunosuppressive IL-10, was also inhibited in splenocytes isolated from NDI10218-treated arthritis mice. Administration of NDI10218 markedly decreased the number of T cell subpopulations in the regional lymph nodes of the arthritis mice. Finally, NDI10218 reduced the number of abdominal contractions in acetic acid-induced writhing model, suggesting an analgesic effect of this extract. Taken together, these results suggest that NDI10218 can be a new therapeutic candidate for the treatment of rheuma-toid arthritis. PMID:24116282

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

188

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

Science.gov (United States)

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

Luvisetto, Siro; Vacca, Valentina; Cianchetti, Carlo

2015-02-01

189

Evaluation of analgesic effect of skin-to-skin contact compared to oral glucose in preterm neonates.  

Science.gov (United States)

Nonpharmacological interventions are important alternatives for pain relief during minor procedures in preterm neonates. Skin-to-skin contact or kangaroo mother care is a human and efficient way of caring for low-weight preterm neonates. The aim of the present study was to assess the analgesic effect of kangaroo care compared to oral glucose on the response of healthy preterm neonates to a low-intensity acute painful stimulus. Ninety-five preterm neonates with a postmenstrual age of 28-36 weeks were randomly assigned to three groups in a single-blind manner. In group 1 (isolette, n=33), the neonate was in the prone position in the isolette during heel lancing and did not receive analgesia. In group 2 (kangaroo method, n=31), the neonate was held in skin-to-skin contact for 10 min before and during the heel-lancing procedure. In group 3 (glucose, n=31), the neonate was in the prone position in the isolette and received oral glucose (1 ml, 25%) 2 min before heel lancing. A smaller variation in heart rate (p=0.0001) and oxygen saturation (p=0.0012), a shorter duration of facial activity (brow bulge, eye squeeze and nasolabial furrowing) (p=0.0001), and a lower PIPP (Premature Infant Pain Profile) score (p=0.0001) were observed in group 2. In conclusion, skin-to-skin contact produced an analgesic effect in preterm newborns during heel lancing. PMID:18434021

Freire, Nájala Borges de Sousa; Garcia, João Batista Santos; Lamy, Zeni Carvalho

2008-09-30

190

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)

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.

Hassan azhdari Zarmehri

2008-11-01

191

Phytochemical profile and analgesic evaluation of Vitex cymosa leaf extracts  

Directory of Open Access Journals (Sweden)

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 analgesia; 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.

Suzana Guimarães Leitão

2011-10-01

192

Phytochemical profile and analgesic evaluation of Vitex cymosa leaf extracts  

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: English Abstract in english 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.

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

2011-10-01

193

Protective effect of Jiaweibugan decoction against diabetic peripheral neuropathy.  

Science.gov (United States)

Oxygen free radical damage is regarded as a direct or indirect common pathway associated with diabetic neuropathy and is the main cause of complications in peripheral neuropathies. We speculate that Jiaweibugan decoction has a significant effect in treating diabetic peripheral neuropathy through an anti-oxidative stress pathway. In this study, a diabetic rat model was established by intraperitoneal injection of streptozotocin. Rats were treated with Jiaweibugan decoction via intragastric administration. The levels of malondialdehyde and glutathione, which are indirect indexes of oxidative stress, in serum were determined using a colorimetric method. The expression levels of nuclear factor kappa B p65 mRNA and p38 mitogen-activated protein kinase, which are oxidative stress associated factors, in the dorsal root ganglion of spinal S4-6 segments were evaluated by reverse-transcriptase polymerase chain reaction and immunohistochemistry. Results showed that, Jiaweibugan decoction significantly ameliorated motor nerve conduction velocity in diabetic rats, effectively decreased malondialdehyde levels in serum and the expression of nuclear factor kappa B p65 mRNA and p38 mitogen-activated protein kinase mRNA in the dorsal root ganglion, and increased glutathione levels in serum. Therefore, our experimental findings indicate that Jiaweibugan decoction plays an anti-oxidative stress role in the diabetic peripheral neuropathy process, which has a protective effect on peripheral nerve injury. PMID:25206405

Wang, Yu; Chen, Zeqi; Ye, Renqun; He, Yulei; Li, Yuhong; Qiu, Xinjian

2013-04-25

194

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

DEFF Research Database (Denmark)

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.

Ravn, Pernille; Foster, David J R

2014-01-01

195

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

DEFF Research Database (Denmark)

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.

Ravn, Pernille; Foster, David J R

2014-01-01

196

Effect of Erythropoietin on Peripheral Nerve Regeneration  

OpenAIRE

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 ...

Ozkan, Mustafa; Gokmen, Necati; Yilmaz, Osman; Erbayraktar, Serhat; Bagriyanik, Alper

2010-01-01

197

Behavioural and electrophysiological evidence for an analgesic effect of a non-steroidal anti-inflammatory agent, sodium diclofenac.  

Science.gov (United States)

The effects of various i.v. doses of diclofenac sodium (Voltaren, 1.5, 3, 6 and 9 mg/kg) were evaluated by measuring the vocalization threshold in response to paw pressure in normal and in Freund's adjuvant-induced arthritic rats. An electrophysiological study performed in parallel in arthritic rats considered the effects of 6 mg/kg i.v. diclofenac on ventrobasal thalamic neuronal responses driven by mild stimulation of an inflamed joint. In normal rats, 6 and 9 mg/kg i.v. diclofenac raised vocalization thresholds significantly (maximum vocalization thresholds were respectively 135.67 +/- 3.30% and 157.41 +/- 4.62% of the preinjection control at 30 min, n = 9 in each group), while no effect was observed with 3 mg/kg. In arthritic rats, i.v. doses of 3, 6 and 9 mg/kg diclofenac induced a clear analgesic effect (maximum vocalization thresholds were respectively 172.22 +/- 4.26, 201.78 +/- 4.76, 222.33 +/- 5.10% of the control at 25 min, n = 9 in each group), whereas a dose of 1.5 mg/kg i.v. did not raise the threshold. In arthritic rats, the VB neuronal responses were depressed by about 50% 20 min after an injection of 6 mg/kg i.v. diclofenac. These results clearly establish that diclofenac produces a dose-dependent analgesic effect, which is more potent in arthritic than in normal rats. PMID:3226759

Attal, N; Kayser, V; Eschalier, A; Benoist, J M; Guilbaud, G

1988-12-01

198

The central analgesic and anti-inflammatory activities of the methanolic extract of Carthamus oxycantha.  

Science.gov (United States)

The plant extract and fractions of Carthamus oxycantha (Compositae) were assessed for analgesic and antiinflammatory activities. Acetic acid and formalin-induced nociception, hot plate and carrageenan-induced rat paw oedema tests were employed to evaluate the analgesic and anti-inflammatory potential of the plant extract. The intraperitoneal (i.p.) administration of the methanolic extract (25-30 mg/kg), hexane (10-50 mg/kg, i.p.) and ethylacetate (50 and 100 mg/kg i.p.) fractions produced significant inhibition (P<0.01) of the acetic acid-induced writhing in mice and suppressed formalin-induced licking response of animals in both phases of the test. In the hot plate assay the plant extract (100 mg/kg i.p.) increased pain threshold of mice. Pre-treatment of animals with naloxone (5 mg/kg i.p.) abolished the analgesic effect of the C. oxycantha in formalin and hot plate tests. C. oxycantha (50-200 mg/kg i.p.) produced marked anti-inflammatory effect in carrageenan-induced rat paw edema assay comparable to diclofenac. These findings suggest that C. oxycantha possesses central analgesic and peripheral anti-inflammatory properties, with analgesic effects associated with the opioid system. PMID:23959734

Bukhari, I A

2013-06-01

199

Effects of SOD on the peripheral blood in irradiated dogs  

International Nuclear Information System (INIS)

Dogs were exposed to 0.6 Gy of 60Co-gamma-rays daily and 10 min after exposure, SOD was injected intramuscular to them. Such treatment continued for 5 days and the effect of SOD on the hemogram of peripheral blood was observed in exposed dogs. The results show that there was a certain protective effect for those exposed dogs to which a double equivalent dose of SOD was injected

200

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

Science.gov (United States)

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

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

2012-01-01

201

Effect of Erythropoietin on Peripheral Nerve Regeneration  

Directory of Open Access Journals (Sweden)

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.

Mustafa OZKAN

2010-03-01

202

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

Directory of Open Access Journals (Sweden)

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.

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

2010-02-01

203

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

Directory of Open Access Journals (Sweden)

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.

Manasa CR

2013-09-01

204

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

Directory of Open Access Journals (Sweden)

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.

Gao Yong-Hui

2012-12-01

205

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

Science.gov (United States)

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

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

2015-04-01

206

Comparative Free Radical Scavenging and Analgesic Activity of Ethanolic Leaves and Stem Extracts of Solanum nigrum  

Directory of Open Access Journals (Sweden)

Full Text Available In the present investigation a comparative analysis of the Free radical scavenging potential and analgesic activity of the Ethanolic Leaf (ELS and stem extracts (ESS of Solanum nigrum was performed. The extracts were evaluated for its DPPH and hydroxyl free radicals scavenging effect and inhibitory potential on protein carbonyl formation. Total phenolic and flavonoid content of the extracts were also determined by a colorimetric method. The ethanolic extracts of Solanum nigrum were evaluated for its peripheral analgesic activity by Acetic-acid induced writhing response and central analgesic activity by Tail flicking method and Hot plate method in mice. Both the plant extracts scavenged the free radicals in a dose dependent manner. However the scavenging effect was more pronounced in ELS extract when comparable to ESS extract. Both the extract possessed considerable quantity of phenols and flavonoids. In Tail flicking and Hot plate methods the ELS extract of Solanum nigrum showed higher mean basal latency time when comparable to ESS extract suggesting its central analgesic activity. Similarly in Acetic acid induced writhing response the ELS extract exhibited a significant inhibition of writhing 53.28% when comparable to ESS which exhibited an inhibition of 46.53%. The positive control Diclofenac sodium showed 70.66% of writhing inhibition. The analgesic activity of the plants extracts is probably due to its free radical scavenging activity.

B. Muralikrishna

2013-01-01

207

The Radiation Effect on Peripheral Blood Cell  

International Nuclear Information System (INIS)

To evaluate radiation effect on the hematopoietic system, we analyzed 44 patients who were treated with conventionally fractionated radiation therapy (RT) at Chonbuk National University Hospital. According to the treatment sites, we classified them into three groups: group I as head and neck, group II as thorax, and group III as pelvis. White blood cell, lymphocyte, platelet and hemoglobin were checked before and during RT The results were as follow; 1. White blood cell (WBC) and lymphocyte count were declined from the first week of RT to the third week, and then slightly recovered after the third or fourth week. There was prominent decrease in lymphocyte counts than WBC. 2. Platelet counts were declined until the second week of the RT, showed slight recovery at fourth week in all groups. Hemoglobin values were slightly decreased in the first week and then recovered the level of pretreatment value, gradually. 3. Lymphocyte count were declined significantly on group III(p<0.01), WBC and platelet counts were decreased on group II but statistically not significant

208

Qigong Effects on Heart Rate Variability and Peripheral Vasomotor Responses.  

Science.gov (United States)

Population aging is occurring worldwide, and preventing cardiovascular event in older people is a unique challenge. The aim of this study was to examine the effects of a 12-week qigong (eight-form moving meditation) training program on the heart rate variability and peripheral vasomotor response of middle-aged and elderly people in the community. This was a quasi-experimental study that included the pre-test, post-test, and nonequivalent control group designs. Seventy-seven participants (experimental group = 47; control group = 30) were recruited. The experimental group performed 30 min of eight-form moving meditation 3 times per week for 12 weeks, and the control group continued their normal daily activities. After 12 weeks, the interaction effects indicated that compared with the control group, the experimental group exhibited significantly improved heart rate variability and peripheral vasomotor responses. PMID:24869492

Chang, Mei-Ying

2014-05-27

209

Therapeutic Effect of Progesterone on Experimental Peripheral Nerve Injury  

Directory of Open Access Journals (Sweden)

Full Text Available This study aims to investigate the therapeutic effect of progesterone on experimental peripheral nerve injury. Methods: A total of 20 male Albino rats weighing 250-300 g were anaesthetized and subjected to sciatic nerve injury model. Rats were then seperated into two groups; one group was treated with progesterone and the other with saline for five time up to 21 days after injury. Both groups were evaluated fuctionally for 21 days and then killed. Sciatic nerves were examined histopathologically. There was no statistically significant difference between these two groups for up to 4 days. But evaluations after 4th day revealed a better improvement in progesterone treatment group. Our data indicate that progesterone has a beneficial effect in peripheral nerve injury.

Mehmet Kizilkaya

2006-01-01

210

Comparing analgesic and hemodynamic effects of unilateral spinal levobupivacaine, levobupivacaine-fentanyl and levobupivacaine-morphine combinations for arthroscopic procedures  

Directory of Open Access Journals (Sweden)

Full Text Available Objectives: Aim of the study was to compare the analgesic and hemodynamic effects of levobupivacaine, levobupivacaine-fentanyl, levobupivacaine-morphine for arthroscopic knee surgery under unilateral spinal anesthesia.Methods: A total of 44 ASA I/II patients scheduled for arthroscopy were included in the study. After prehydration patients kept in a lateral position on the nondependent side. Spinal puncture was performed at L3–4/L4–5 intervertebral space. Patients divided into three subgroups: Group L (n=14 received 0.5% levobupivacaine 1 ml+1 ml distilled water; Group LF (n=15, 25 mcg fentanyl (0.5 ml+0.5 ml distilled water; and Group LM (n=15, 0.01 mg morphine (0.5 ml+0.5 ml distilled water. Patients remained in that position for 15 minutes. Blood pressure and heart rate were recorded before and 1st, 3rd, 5th, 10th, 15th, 20th and 30th minutes after the block and every 15 minutes during the operation. Motor blockade and sensorial level, side effects, motor block regression time (MBRT, first urination time and first analgesic need (FAN were recorded.Results: Group LM had the longest MBRT, but difference with other groups did not reach to a significant level (p>0.05. Group LM had significantly longer FAN time compare with other groups (p<0.05. The first urination time was latest in Group LM (p<0.05. Motor blockade was least in Group L (p<0.05 and almost 50% patients had not motor block.Conclusion: All three groups had successful anesthesia. Morphine group added group had significantly longer analgesia without significant urinary retention and motor blockade regression time. We concluded that additional low doses of morphine will be a better choice.

Özlem Özorak

2010-09-01

211

Effect of single dose pretreatment analgesia with three different analgesics on postoperative endodontic pain: A randomized clinical trial  

Science.gov (United States)

Introduction: One of the aims of root canal treatment is to prevent or eliminate pain. Postoperative endodontic pain control continues to be a significant challenge. Aim: To compare and evaluate the effect of single oral dose of 100 mg of tapentadol, 400 mg of etodolac, or 10 mg of ketorolac as a pretreatment analgesic for the prevention and control of postoperative endodontic pain in patients with symptomatic irreversible pulpitis. The incidence of side effects was recorded as secondary outcome. Materials and Methods: Sixty emergency patients with moderate to severe pain, diagnosed with symptomatic irreversible pulpitis were randomly allocated (1:1:1) to any of the three groups; tapentadol, etodolac, or ketorolac. Medications were administered 30 min before beginning of the endodontic treatment. Patients recorded pain intensity on 10 cm visual analog scale (VAS) after treatment, for upto 24 h. Results: At 24 h, mean ±standard deviation (SD) of VAS scores (in cm) for tapentadol, etodolac, and ketorolac were 0.89 ± 0.83, 2.68 ± 2.29, and 0.42 ± 0.69, respectively. Kruskal-Wallis (K-W) test showed significant difference among the three groups (P = 0.001). Mann-Whitney test showed significantly lower VAS scores in tapentadol and ketorolac than etodolac group (P = 0.013 and 0.001, respectively). Conclusions: Single oral dose of 10 mg of ketorolac and 100mg of tapentadol as a pretreatment analgesic significantly reduced postoperative endodontic pain in patients with symptomatic irreversible pulpitis when compared to 400 mg of etodolac. PMID:25506136

Sethi, Priyank; Agarwal, Manish; Chourasia, Hemant Ramesh; Singh, Mahesh Pratap

2014-01-01

212

Effect of modulating macrophage phenotype on peripheral nerve repair  

OpenAIRE

Peripheral nerve repair across long gaps remains clinically challenging despite progress made with autograft transplantation. While scaffolds that present trophic factors and extracellular matrix molecules have been designed, matching the performance of autograft-induced repair has been challenging. In this study, we explored the effect of cytokine mediated ‘biasing’ of macrophage phenotypes on Schwann cell (SC) migration and axonal regeneration in vitro and in vivo. Macrophage phenotype ...

Mokarram, Nassir; Merchant, Alishah; Mukhatyar, Vivek; Patel, Gaurangkumar; Bellamkonda, Ravi V.

2012-01-01

213

Therapeutic Effect of Progesterone on Experimental Peripheral Nerve Injury  

OpenAIRE

This study aims to investigate the therapeutic effect of progesterone on experimental peripheral nerve injury. Methods: A total of 20 male Albino rats weighing 250-300 g were anaesthetized and subjected to sciatic nerve injury model. Rats were then seperated into two groups; one group was treated with progesterone and the other with saline for five time up to 21 days after injury. Both groups were evaluated fuctionally for 21 days and then killed. Sciatic nerves were examined histopathologica...

Mehmet Kizilkaya; Sedat Binler; Kayaoglu, C. R.; Goksin Sengul

2006-01-01

214

Endothelin B receptors exert antipruritic effects via peripheral ?-opioid receptors.  

Science.gov (United States)

Endothelin B receptor agonists exert antipruritic effects on itching induced via endothelin-1 (ET-1) and compound 48/80. Peripheral µ- and ?-opioid receptors (MORs and KORs, respectively) are reported to be involved in the anti-nociceptive properties triggered by ET(B) agonists. Therefore, we investigated the role of peripheral opioid receptors in the scratching response induced by ET-1. ET(A) and ET(B) antagonists and non-selective and selective opioid receptor antagonists were co-injected with ET-1 in the neck of mice and the number of scratching bouts was counted. Pretreatment with systemically administered naloxone significantly reduced the number of scratches, while co-injection of naloxone substantially augmented the effect of ET-1. Co-injection of nor-Binaltorphimine (nor-BNI), a KOR antagonist, significantly increased the number of scratches induced by ET-1. However, CTOP (a MOR antagonist) and naltrindole [a ?-opioid receptor (DOR) antagonist] did not alter the scratching response elicited by ET-1. These results indicate that peripheral KORs mediate the antipruritic effect of endothelin B receptor activation. PMID:23181126

Ji, Wenjin; Liang, Jiexian; Zhang, Zhiwei

2012-09-01

215

Comparison of analgesic effects of nimesulide, paracetamol, and their combination in animal models  

Directory of Open Access Journals (Sweden)

Full Text Available Objectives: To compare the analgesic activity of nimesulide and paracetamol alone and their combination in animal models for the degree of analgesia and the time course of action. Materials and Methods: Analgesia was studied in albino rats using formalin test and in albino mice using writhing test and the radiant heat method. For each test, four groups of six animals each were orally fed with a single dose of nimesulide, paracetamol, and combination of nimesulide + paracetamol and gum acacia as control, respectively. Results: In all the three test models, all three drug treatments showed significant analgesia (P < 0.001 as compared to control, but there was no significant difference in the analgesia produced by either drugs alone or in combination. The radiant heat method demonstrated a quicker onset and longer duration of action with nimesulide, whereas writhing test showed a quicker onset of action with paracetamol. In formalin test, greater degree of analgesia was seen with individual drugs than that of the combination, though this difference was not statistically significant. Conclusions: Nimesulide and paracetamol combination offers no advantage over nimesulide alone or paracetamol alone, either in terms of degree of analgesia or onset of action. Therefore, our study supports the reports claiming irrationality of the fixed dose combination of nimesulide and paracetamol.

Ahmed Mushtaq

2010-01-01

216

Analgesic effect and side effects of celecoxib and meloxicam in canine hip osteoarthritis  

Directory of Open Access Journals (Sweden)

Full Text Available 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 percent 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.

Víctor Molina D.

2014-09-01

217

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

Directory of Open Access Journals (Sweden)

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.

Ostadalipour Abbas

2007-01-01

218

Effect of glial inhibition in attenuation of neuropathic pain and improvement of morphine analgesic effect in a rat model of neuropathy  

Directory of Open Access Journals (Sweden)

Full Text Available Introduction: Pharmacological blockage of glial activity has been proved useful for treatment of neuropathic pain by lowering proinflammatory cytokines. The present study is to confirm the effect of post-injury administration of pentoxifylline on chronic constriction injury (CCI-induced neuropathic pain symptoms_ and improved the efficacy of morphine anti-nociception. Methods: Male Wistar rats (230-270 g underwent surgery for induction of CCI model of neuropathy. In the sham group the nerve was exposed but not ligated. In 5 groups (n=8 morphine (2.5, 5, 7.5, 10, 15 mg/kg s.c. was administered in post-operative days (POD 0, 6 and 14. To evaluate the analgesic effect of different doses of morphine, Von Frey and Hargreaves tests were performed before and 30 minutes after morphine administration. In different groups, pentoxifylline (8, 15, 30 mg/kg i.p. or normal saline (vehicle were administered from POD6 to POD13. Behavioral tests were utilized after last dose of pentoxifylline and also on POD14 again after injection of a single dose of morphine (5 mg/kg, s.c.. Results: The analgesic effect of morphine (5 mg/kg on POD6 and morphine (5, 7.5, 10, 15 mg/kg on POD14 was significantly decreased in comparison to POD0. Pentoxifylline effectively attenuated thermal hyperalgesia (at 15 and 30 mg/kg and mechanical allodynia (at 30 mg/kg on POD13. However, pentoxifylline (15, 30 mg/kg improved the antihyperalgesic effect of morphine (5 mg/kg s.c. on POD14. Conclusion: Analgesic effect of morphine was reduced after nerve injury and it may be due to the activation of glia. Inhibition of glial activity is an effective way to attenuate CCI-induced neuropathic pain and also to improve the antihyperalgesic effect of morphine, without significant effect on its anti-allodynic effect.

samad nazemi

2012-01-01

219

The analgesic effect of electroacupuncture on acute thermal pain perception-a central neural correlate study with fMRI  

Directory of Open Access Journals (Sweden)

Full Text Available Abstract Background Electrical acupuncture (EA has been utilized in acute pain management. However, the neuronal mechanisms that lead to the analgesic effect are still not well defined. The current study assessed the intensity [optimal EA (OI-EA vs. minimal EA (MI-EA] effect of non-noxious EA on supraspinal regions related to noxious heat pain (HP stimulation utilizing an EA treatment protocol for acute pain and functional magnetic resonance imaging (fMRI with correlation in behavioral changes. Subjects underwent five fMRI scanning paradigms: one with heat pain (HP, two with OI-EA and MI-EA, and two with OI-EA and HP, and MI-EA and HP. Results While HP resulted in activations (excitatory effect in supraspinal areas known for pain processing and perception, EA paradigms primarily resulted in deactivations (suppressive effect in most of these corresponding areas. In addition, OI-EA resulted in a more robust supraspinal sedative effect in comparison to MI-EA. As a result, OI-EA is more effective than MI-EA in suppressing the excitatory effect of HP in supraspinal areas related to both pain processing and perception. Conclusion Intensities of EA plays an important role in modulating central pain perception.

Leung Albert

2011-06-01

220

Study of interaction between opioid and ?-2 adrenergic systems in analgesic effect of oxytocin in locus coeruleus nucleus  

Directory of Open Access Journals (Sweden)

Full Text Available Introduction: Oxytocin is a active neuropeptide of central nervous system. In this study the effects of naloxone (opioid receptor antagonist and yohimbine (?-2 adrenergic receptor antagonist on analgesic effect of oxytocin applied into the locus coeruleus (LC nucleus were investigated. Methods: Adult male Wistar rats were used. Animals divided into different groups receiving saline, oxytocin (3 nmol / 2?l, naloxone (3 nmol / 2?l + oxytocin, yohimbine (3 nmol / 2?l + oxytocin, and naloxone + yohimbine + oxytocin. Hot-plate and tail-flick tests were used to evaluate pain threshold. Results: Data showed that the injection of oxytocin into the LC nucleus increases the response time to thermal stimulations in both tail flick and hot plate tests. Injection of naloxone and yohimbine either separately and or in combination inhibite the antinociception effect of oxytocin. Conclusion: It seems that oxytocin induces its inhibitory effect on acute pain via LC nucleus. This effect is probably mediated by the combination of opioid and ?-2 adrenergic systems.

Nasrin haghighi

2006-12-01

221

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

DEFF Research Database (Denmark)

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.

Garza Villarreal, Eduardo A.; Brattico, Elvira

2012-01-01

222

Effect of PACAP in Central and Peripheral Nerve Injuries  

Directory of Open Access Journals (Sweden)

Full Text Available Pituitary adenylate cyclase activating polypeptide (PACAP is a bioactive peptide with diverse effects in the nervous system. In addition to its more classic role as a neuromodulator, PACAP functions as a neurotrophic factor. Several neurotrophic factors have been shown to play an important role in the endogenous response following both cerebral ischemia and traumatic brain injury and to be effective when given exogenously. A number of studies have shown the neuroprotective effect of PACAP in different models of ischemia, neurodegenerative diseases and retinal degeneration. The aim of this review is to summarize the findings on the neuroprotective potential of PACAP in models of different traumatic nerve injuries. Expression of endogenous PACAP and its specific PAC1 receptor is elevated in different parts of the central and peripheral nervous system after traumatic injuries. Some experiments demonstrate the protective effect of exogenous PACAP treatment in different traumatic brain injury models, in facial nerve and optic nerve trauma. The upregulation of endogenous PACAP and its receptors and the protective effect of exogenous PACAP after different central and peripheral nerve injuries show the important function of PACAP in neuronal regeneration indicating that PACAP may also be a promising therapeutic agent in injuries of the nervous system.

Andras Buki

2012-07-01

223

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

OpenAIRE

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...

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

1993-01-01

224

Brain P450 Epoxygenase Activity is Required for the Antinociceptive Effects of Improgan, a Non-Opioid Analgesic  

OpenAIRE

The search for the mechanism of action of improgan (a non-opioid analgesic) led to the recent discovery of CC12, a compound which blocks improgan antinociception. Since CC12 is a cytochrome P450 inhibitor, and brain P450 mechanisms were recently shown to be required in opioid analgesic signaling, pharmacological and transgenic studies were performed in rodents to test the hypothesis that improgan antinociception requires brain P450 epoxygenase activity. Intracerebroventricular (icv) administr...

Hough, L. B.; Nalwalk, J. W.; Yang, J.; Conroy, J. L.; Vanalstine, M. A.; Yang, W.; Gargano, J.; Shan, Z.; Zhang, S. Z.; Wentland, M. P.; Phillips, J. G.; Knapp, B. I.; Bidlack, J. M.; Zuiderveld, O. P.; Leurs, R.

2011-01-01

225

Effects of Melatonin and Vitamin E on Peripheral Neuropathic Pain in Streptozotocin-Induced Diabetic Rats  

Directory of Open Access Journals (Sweden)

Full Text Available Objective(sPrevious studies have indicated that diabetes mellitus might be accompanied by neuropathic pain. Oxidative stress is implicated as a final common pathway in development of diabetic neuropathy. Pharmacological interventions targeted at inhibiting free radical production have shown beneficial effects in diabetic neuropathy. The aim of this study was to investigate and compare the possible analgesic effects of melatonin and vitamin E in diabetic rats.Materials and MethodsThis study was performed on 32 male Wistar rats divided into 4 groups: control, diabetic, melatonin-treated diabetic and vitamin E-treated diabetic. Experimental diabetes was induced by intraperitoneal streptozotocin (50 mg/kg injection. Melatonin (10 mg/kg, i.p. and vitamin E (100 mg/kg, i.p. were injected for 2 weeks after 21st day of diabetes induction. At the end of administration period, pain-related behavior was assessed using 0.5% formalin test according to two spontaneous flinching and licking responses. The levels of lipid peroxidation as well as glutathione-peroxidase and catalase activities were evaluated in lumbosacral dorsal root ganglia.ResultsFormalin-evoked flinching and total time of licking were increased in both acute and chronic phases of pain in diabetic rats as compared to control rats, whereas treatment with melatonin or vitamin E significantly reduced the pain indices. Furthermore, lipid peroxidation levels increased and glutathione-peroxidase and catalase activities decreased in diabetic rats. Both antioxidants reversed the biochemical parameters toward their control values.ConclusionThese results suggest that oxidative stress may contribute to induction of pain in diabetes and further suggest that antioxidants, melatonin and vitamin E, can reduce peripheral neuropathic pain in streptozotocin-induced diabetic rats.

Reza Heidari

2010-04-01

226

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

Directory of Open Access Journals (Sweden)

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

Stephanie Anderson

2010-09-01

227

Analgesic effects mediated by neuronal nicotinic acetylcholine receptor agonists: correlation with desensitization of ?4?2* receptors.  

Science.gov (United States)

Nicotinic ?4?2* agonists are known to be effective in a variety of preclinical pain models, but the underlying mechanisms of analgesic action are not well-understood. In the present study, we characterized activation and desensitization properties for a set of seventeen novel ?4?2*-selective agonists that display druggable physical and pharmacokinetic attributes, and correlated the in vitro pharmacology results to efficacies observed in a mouse formalin model of analgesia. ABT-894 and Sazetidine-A, two compounds known to be effective in the formalin assay, were included for comparison. The set of compounds displayed a range of activities at human (?4?2)(2)?2 (HS-?4?2), (?4?2)(2)?5 (?4?2?5) and (?4?2)(2)?4 (LS-?4?2) receptors. We report the novel finding that desensitization of ?4?2* receptors may drive part of the antinociceptive outcome. Our molecular modeling approaches revealed that when receptor desensitization rather than activation activitiesat ?4?2* receptors are considered, there is a better correlation between analgesia scores and combined in vitro properties. Our results suggest that although all three ?4?2 subtypes assessed are involved, it is desensitization of ?4?2?5 receptors that plays a more prominent role in the antinociceptive action of nicotinic compounds. For modulation of Phase I responses, correlations are significantly improved from an r(2) value of 0.53 to 0.67 and 0.66 when HS- and LS-?4?2 DC(50) values are considered, respectively. More profoundly, considering the DC(50) at ?4?2?5 takes the r(2) from 0.53 to 0.70. For Phase II analgesia scores, adding HS- or LS-?4?2 desensitization potencies did not improve the correlations significantly. Considering the ?4?2?5 DC(50) value significantly increased the r(2) from 0.70 to 0.79 for Phase II, and strongly suggested a more prominent role for ?4?2?5 nAChRs in the modulation of pain in the formalin assay. The present studies demonstrate that compounds which are more potent at desensitization of ?4?2* receptors display better analgesia scores in the formalin test. Consideration of desensitization propertiesat ?4?2* receptors, especially at ?4?2?5, in multiple linear regression analyses significantly improves correlations with efficacies of analgesia. Thus, ?4?2* nicotinic acetylcholine receptor desensitization may contribute to efficacy in the mediation of pain, and represent a mechanism for analgesic effects mediated by nicotinic agonists. PMID:23036283

Zhang, Jiahui; Xiao, Yun-De; Jordan, Kristen G; Hammond, Phil S; Van Dyke, Katherine M; Mazurov, Anatoly A; Speake, Jason D; Lippiello, Patrick M; James, John W; Letchworth, Sharon R; Bencherif, Merouane; Hauser, Terry A

2012-12-18

228

The analgesic effect of nefopam combined with low dose remifentanil in patients undergoing middle ear surgery under desflurane anesthesia: a randomized controlled trial  

Science.gov (United States)

Background We investigated the effects of the combined administration of nefopam, a N-methyl-D-aspartate receptor antagonist and low dose remifentanil, on early postoperative pain and analgesic requirement. Methods Fifty patients scheduled to undergo mastoidectomy and tympanoplasty were randomized to be given either nefopam 40 mg mixed with normal saline 100 ml (Group N) or an equal amount of normal saline (Group C) before anesthesia induction. Anesthesia was maintained with 5-6 vol% desflurane and remifentanil 0.05-0.15 µg/kg/min during the surgery. Postoperative pain was controlled by titration of ketorolac in the postanesthesia care unit (PACU) and ward. We evaluated the intraoperative remifentanil dose, recovery profiles, ketorolac demand in the PACU and ward, numeric rating scale (NRS) for pain at time intervals of every 10 min for 1 h in the PACU, 6, 12, 18 and 24 h in a ward, as well as the time to first analgesic requirement in the PACU and ward. Results Ketorolac demand and NRS in the PACU were significantly lower in Group N than Group C (P = 0.002, P = 0.005, respectively). The time to first analgesic requirement in the PACU in Group N were significantly longer than Group C (P = 0.046). There were no significant differences in intraoperative remifentanil dose, ketorolac demand, NRS, and the time to first analgesic requirement in the ward between the groups. Conclusions Nefopam administration combined with low dose remifentanil infusion reduces pain and analgesic consumption during the immediate postoperative period in patients undergoing middle ear surgery under desflurane anesthesia.

Yoo, Jung Young; Kim, Heezoo; Kong, Myoung-Hoon; Lee, IL-Ok; Kim, Nan Sook

2015-01-01

229

The study of Analgesic, Antidiarrhoeal and Anti-oxidant Effect of Ethanolic Extracts of Ecbolium linnaenum in Albino Mice  

Directory of Open Access Journals (Sweden)

Full Text Available The Ecbolium linnaenum(leaves is used as a folk medicine in Bangladesh for pain, diarrhea and infectious diseases. Phytochemical evaluation of the ethanolic extracts of Ecboliumlinnaenumleaves demonstratesthese pharmacologic effect for the presence of alkaloids, tannins, gums,flavonoids and absence of carbohydrates, steroids, saponins. In this present study an attempt was made to determine the analgesic, antidiarrhoel, antioxidantand antimicrobial effectin Swiss Albino mice. Ethanolic extracts of250 and 500 mg/kg showed significant inhibition of writhing reflex 36.20% (P< 0.01 and 54.48% (P< 0.001, respectively while the standard drug diclofenac-Na was 75.52% (P< 0.001 at a dose of 25 mg/kg body weight.In the castor oil-induced diarrhoealmice, the ethanolic extracts of 250 mg/kg & 500 mg/kg, raised the latent period and reduced the number of stools comparing with standard drug Loperamide. 0.02% DPPH solution of ethanol on TLC plate showed the presence of anti-oxidant components in the Ecboliumlinnaenum.From the % inhibition of ascorbic acid and Ecboliumlinnaenum we observe that it has anti-oxidation effect. The IC50 (inhibitory conc. 50% for ascorbic acid is approximately 1 µg/ml and for the sample it is more than 500 µg/ml. The ethanolic extract of Ecboliumlinnaenum was tested for antimicrobial activity against a number of both gram positive and gram-negative bacteria but it does not show any anti-microbial effect.

Md Kamrul Hasan Chowdhury

2013-03-01

230

Ketorolac tromethamine improves the analgesic effect of hyoscine butylbromide in patients with intense cramping pain from gastrointestinal or genitourinary origin.  

Science.gov (United States)

The symptomatic treatment of pain associated with spasm of gastrointestinal or genitourinary origin can include the use of spasmolytic agents and/or non-steroidal anti-inflammatory drugs. However, the evidence of a superior effectiveness of combination in comparison with individual drugs is scarce and controversial. A double-blind, randomised, clinical trial study was designed to characterize the analgesic effect and safety of ketorolac and hyoscine butylbromide against hyoscine butylbromide alone in patients with ambulatory acute cramping pain of gastrointestinal and genitourinary origin. 160 patients with a pain level ?4 in a 1-10?cm visual analogue scale were allocated to receive a fixed dose of ketorolac/hyoscine butylbromide (10?mg/20?mg) or hyoscine butylbromide (20?mg) alone at 6?h intervals, during a 48?h period. Both treatments were similarly effective when compared as a whole or when groups were classified by pain origin. Conversely, when treatments were grouped by pain intensity, ketorolac/hyoscine butylbromide combination showed a significant better pain relief profile than hyoscine butylbromide alone in pain intensity ?7, but not hyoscine butylbromide mixture could be a better option than hyoscine butylbromide alone in the treatment of some acute intense cramping painful conditions. PMID:23093479

del Valle-Laisequilla, C F; Flores-Murrieta, F J; Granados-Soto, V; Rocha-González, H I; Reyes-García, G

2012-12-01

231

Effects of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood  

DEFF Research Database (Denmark)

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.

SØrensen, S F; Dirksen, Asger

1979-01-01

232

Indirect genotoxic effect of gamma rays in human peripheral lymphocytes  

International Nuclear Information System (INIS)

The aim of this study was to investigate the indirect genotoxic effect of various doses of gamma rays in human peripheral lymphocytes. For this aim, chromosome mediums were irradiated with various doses (2000, 4000, 8000, 16000 rad) of gamma rays. In this study, we were found that SCE (Sister Chromatid Exchange) was increased by gamma rays doses-dependently. In addition to these, percentages of abnormal cells with chromosomal abnormalities and CA (Chromosome Aberration)/Cell were increased by all doses of gamma rays compared to control. Besides, gamma rays decreased the MI dose-dependently. RI was not also reduced at all concentrations. (author)

233

First evidence of the analgesic activity of govaniadine, an alkaloid isolated from Corydalis govaniana Wall.  

Science.gov (United States)

In this work, govaniadine, an alkaloid isolated from Corydalis govaniana Wall. was evaluated for its analgesic activity by writhing and hot-plate tests. Govaniadine did not display any toxic effects in mice up to 20 mg/kg during 24 h assessment study. The acetic acid-induced writhing was significantly reduced by pretreatment with govaniadine in a dose-dependent manner (1.25-5.0 mg/kg, intraperitoneally (i.p.)). Furthermore, molecular docking study has shown that this alkaloid binds the COX-2 enzyme. In the hot-plate test, govaniadine at dose of 2.5 and 5 mg/kg, i.p. displayed analgesic effect at all time points (30, 60, 90 and 120 min). The analgesic effect of govaniadine was significantly antagonised by naloxone administration. Our results demonstrate for the first time that the peripheral and central analgesic effects of govaniadine could be in part related to the involvement of COX-2 activity and by its interaction with the opioid system. PMID:25154594

Muhammad, Naveed; Lal Shrestha, Ram; Adhikari, Achyut; Wadood, Abdul; Khan, Haroon; Khan, Amir Zada; Maione, Francesco; Mascolo, Nicola; De Feo, Vincenzo

2015-03-01

234

Evaluation of the anti-inflammatory and analgesic activities of Liu-Shen-Wan and its individual fractions.  

Science.gov (United States)

Liu-Shen-Wan (LSW), a famous traditional Chinese medicine for treatment of upper respiratory tract inflammation, was evaluated for its anti-inflammatory and analgesic activities. Acetic acid-elevated vascular permeability, carboxymethylcellulose sodium (CMC-Na)-induced leukocyte migration and ear edema induced by picryl chloride were used to test anti-inflammatory activity. Moreover, acetic acid-induced writhing and hot-plate tests were used to determine analgesic effect. It was observed that LSW exerted significant anti-inflammatory and analgesic activities in these models at doses of 30 and 90mg/kg crude drug in vivo. In addition, LSW potently inhibited proliferation of human peripheral blood mononuclear cell (PBMC) stimulated by streptococcal pyrogenic exotoxin at doses of 0.5-5microg/ml in vitro. LSW was then partitioned with chloroform, methanol, water and mineral fraction. Several fractions inhibited inflammation and pain in varying degrees. Among them, chloroform fraction was the most active in hot-plate and writhing tests, and exerted the remarkable inhibitory effect on human PBMC proliferation. Methanol and water fractions had more suppressive activities in vascular permeability, leukocyte migration and PC-DTH tests. These results suggest that LSW has significantly anti-inflammatory and analgesic activities. The chloroform fraction is a key fraction of LSW to the overall anti-inflammatory and analgesic effects, while methanol and water fractions also partly contribute to anti-inflammatory activities of LSW. PMID:17368990

Ma, Hong-Yue; Kou, Jun-Ping; Wang, Jing-Rong; Yu, Bo-Yang

2007-05-30

235

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

OpenAIRE

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...

Homa Manaheji

2011-01-01

236

Semi-mechanistic modeling of the interaction between the central and peripheral effects in the antinociceptive response to lumiracoxib in rats.  

Science.gov (United States)

The model-based approach was undertaken to characterize the interaction between the peripheral and central antinociceptive effects exerted by lumiracoxib. The effects of intraplantar and intrathecal administrations and of fixed ratio combinations of lumiracoxib simultaneously administered by these two routes were evaluated using the formalin test in rats. Pain-related behavior data, quantified as the number of flinches of the injected paw, were analyzed using a population approach with NONMEM 7. The pain response during the first phase of the formalin test, which was insensitive to lumiracoxib, was modeled using a monoexponential decay. The second phase, which was sensitive to lumiracoxib, was described incorporating synthesis and degradation processes of pain mediators that were recruited locally after tissue injury. Upregulation at the local level and in the central nervous system (CNS) was set to be proportional to the predicted levels of pain mediators in the local (injured) compartment. Results suggest a greater role of upregulated COX-2(Local) in generating the pain response compared to COX-2(CNS). Drug effects were described as inhibition of upregulated COX-2. The model adequately described the time course of nociception after formalin injection in the absence or presence of lumiracoxib administered locally and/or spinally. Data suggest that the overall response is the additive outcome of drug effects at the peripheral and central compartments, with predominance of peripheral mechanisms. Application of modeling opens new perspectives for understanding the overall mechanism of action of analgesic drugs. PMID:22968496

Vélez de Mendizábal, Nieves; Vásquez-Bahena, Dalia; Jiménez-Andrade, Juan M; Ortiz, Mario I; Castañeda-Hernández, Gilberto; Trocóniz, Iñaki F

2012-12-01

237

Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects.  

Science.gov (United States)

Pain remains a pervasive problem throughout medicine, transcending all specialty boundaries. Despite the extraordinary insights into pain and its mechanisms over the past few decades, few advances have been made with analgesics. Most pain remains treated by opiates, which have significant side effects that limit their utility. We now describe a potent opiate analgesic lacking the traditional side effects associated with classical opiates, including respiratory depression, significant constipation, physical dependence, and, perhaps most important, reinforcing behavior, demonstrating that it is possible to dissociate side effects from analgesia. Evidence indicates that this agent acts through a truncated, six-transmembrane variant of the G protein-coupled mu opioid receptor MOR-1. Although truncated splice variants have been reported for a number of G protein-coupled receptors, their functional relevance has been unclear. Our evidence now suggests that truncated variants can be physiologically important through heterodimerization, even when inactive alone, and can comprise new therapeutic targets, as illustrated by our unique opioid analgesics with a vastly improved pharmacological profile. PMID:22106286

Majumdar, Susruta; Grinnell, Steven; Le Rouzic, Valerie; Burgman, Maxim; Polikar, Lisa; Ansonoff, Michael; Pintar, John; Pan, Ying-Xian; Pasternak, Gavril W

2011-12-01

238

Effects of estrogen peripheral metabolism in rheumatoid arthritis  

Directory of Open Access Journals (Sweden)

Full Text Available It is well known that the immune reactivity is modulated by gender. In fact, women show a more effective immune response as well as a more frequent development of autoimmune diseases. In particular, 17b-estradiol (E2 in patients with systemic inflammatory diseases leads to an higher production of IgG and IgM in peripheral blood mononucleated cells (PBMC and the secretion of metalloproteinases and IL-6 by synovial fibroblasts. The effect of E2 seems to be partially related to its concentration. In fact, at the physiological concentration, E2 seems to exert a pro-inflammatory effect, while at pharmacological concentrations shows anti-inflammatory effects. Steroid hormones can be converted in downstream hormones along defined pathways. The conversion of dehydroepiandrosterone (DHEA in peripheral macrophages leads to the androgen production. Subsequently the enzyme aromatase converts androgens in estrogens, and its activity is increased by some inflammatory cytokines such as IL-1b, IL-6 and TNF-a. In the synovial fluids of rheumatoid arthritis (RA patients the levels of estrogens result significantly increased compared with controls, showing the consequence of this unbalanced steroid metabolism. Furthermore, the metabolism of estrogens leads to some downstream hydroxylated metabolites, that are not waste products, but still active molecules in the inflammatory response. In fact, it has been found that synovial fluids of RA patients present a different ratio of 16-hydroxylated estrogen metabolites/ 2-hydroxylated metabolites, confirming that also the unbalanced metabolism of estrogens and not only the estrogen concentration seems to be related to the development and worsening of rheumatoid arthritis.

M. Cutolo

2011-09-01

239

Analgesic Activity of Psidium guajava root extracts  

OpenAIRE

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 chlor...

Girish Kumar Gupta, Manisha Bhatia

2013-01-01

240

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)

241

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)

242

Effects of microwave radiation on peripheral lymphocyte subpopulations in rats  

Directory of Open Access Journals (Sweden)

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.

Jin-ling YIN

2011-10-01

243

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

Directory of Open Access Journals (Sweden)

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.

Apurba Mukherjee, Meghali Chaliha and Swarnamoni Das

2009-12-01

244

ANALGESIC AND ANTI-INFLAMMATORY POTENTIAL OF THE PLANT ERVATAMIA CORONARIA (STAPF.  

Directory of Open Access Journals (Sweden)

Full Text Available ABSTRACT: The present study was conducted to evaluate the analgesic and anti-inflammatory potential of the flowers of Ervatamia coronaria. The analgesic activity of the extract was assessed by the acetic acid induced writhing test. Aspirin was used as a standard drug. The anti-inflammatory activity was evaluated by carrageenan induced rat hind paw edema method. The initial paw volume was measured plethysmographically immediately before subplanter injection. The relative increase in the paw volume was measured in control, standard and treated groups, 4h after carrageenan injection. The results of acetic acid writhing test in mice showed a significant decrease in number of wriths in ethanolic extracts of flowers of E. coronaria, suggesting peripheral analgesic effect. In carrageenan induced rat hind paw method; it was found that ethanolic extract of the flowers of E. coronaria, at a dose of 400 mg/kg body weight significantly reduced the oedema volume, which was comparable to standard drug diclofenac sodium. The flowers of the plant exhibited significant analgesic and anti-inflammatory activity, thereby justifying their use in traditional system of medicine.

Himanshu Joshi*, Arun B Joshi, D. Satyanarayana, M.P. Gururaja and C.S Shastry

2013-04-01

245

T-type calcium channel inhibition underlies the analgesic effects of the endogenous lipoamino acids.  

Science.gov (United States)

Lipoamino acids are anandamide-related endogenous molecules that induce analgesia via unresolved mechanisms. Here, we provide evidence that the T-type/Cav3 calcium channels are important pharmacological targets underlying their physiological effects. Various lipoamino acids, including N-arachidonoyl glycine (NAGly), reversibly inhibited Cav3.1, Cav3.2, and Cav3.3 currents, with potent effects on Cav3.2 [EC(50) approximately 200 nm for N-arachidonoyl 3-OH-gamma-aminobutyric acid (NAGABA-OH)]. This inhibition involved a large shift in the Cav3.2 steady-state inactivation and persisted during fatty acid amide hydrolase (FAAH) inhibition as well as in cell-free outside-out patch. In contrast, lipoamino acids had weak effects on high-voltage-activated (HVA) Cav1.2 and Cav2.2 calcium currents, on Nav1.7 and Nav1.8 sodium currents, and on anandamide-sensitive TRPV1 and TASK1 currents. Accordingly, lipoamino acids strongly inhibited native Cav3.2 currents in sensory neurons with small effects on sodium and HVA calcium currents. In addition, we demonstrate here that lipoamino acids NAGly and NAGABA-OH produced a strong thermal analgesia and that these effects (but not those of morphine) were abolished in Cav3.2 knock-out mice. Collectively, our data revealed lipoamino acids as a family of endogenous T-type channel inhibitors, suggesting that these ligands can modulate multiple cell functions via this newly evidenced regulation. PMID:19846698

Barbara, Guillaume; Alloui, Abdelkrim; Nargeot, Joël; Lory, Philippe; Eschalier, Alain; Bourinet, Emmanuel; Chemin, Jean

2009-10-21

246

Feed-forward inhibition: a novel cellular mechanism for the analgesic effect of substance P  

OpenAIRE

Abstract Substance P (SP) is a neuropeptide well known for its contribution to pain transmission in the spinal cord, however, less is known about the possible modulatory effects of SP. A new study by Gu and colleagues, published in Molecular Pain (2005, 1:20), describes its potential role in feed-forward inhibition in lamina V of the dorsal horn of the spinal cord. This inhibition seems to function through a direct excitation of GABAergic interneurons by substance P release...

Yoshimura Megumu; Ko Shanelle W; Xu Hui; Wu Long-Jun; Zhuo Min

2005-01-01

247

Experimental designs and brain mapping approaches for studying the placebo analgesic effect  

OpenAIRE

The placebo effect has intrigued scientists since it was proposed. The debate has now centered on how it works. Significant progress has been made and most of our knowledge about the neurobiological mechanisms comes from the field of pain and analgesia. The appropriateness of the experimental/clinical paradigms is crucial when we want to investigate the mechanisms of the placebo phenomenon. Recently, functional imaging techniques, such as positron emission tomography, magnetic resonance imagi...

Benedetti, Fabrizio

2008-01-01

248

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

OpenAIRE

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...

HelenaKnotkova; MichaelA.Nitsche; RicardoACruciani

2013-01-01

249

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

International Nuclear Information System (INIS)

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 [3H]-etorphine, [3H]-dihydromorphine and [3H]-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

250

NATURAL AND PARTIALLY SYNTETIC ANALGESICS  

Directory of Open Access Journals (Sweden)

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.

Stevan Glogovac

2005-12-01

251

Clinical effects of preemptive analgesia using three different analgesics in strabismus surgery  

Directory of Open Access Journals (Sweden)

Full Text Available AIM:To compare the effects of preemptive analgesia of parecoxib, butorphanol, and pethidine used in and after strabismus surgery, and explore an effective and safe method of analgesia for strabismus surgery. METHODS: This was a prospective, randomized, double-blind, placebo-controlled study.After the ethic committee approval and written conformed consent were obtained, 80 ASA ? patients aged 18-50 years undergoing strabismus surgery under local anesthesia were randomly allocated to 4 groups(n=20 each: group P received intramuscular parecoxib(40mg, group B received intramuscular butorphanol(1mg, group D received intramuscular pethidine(50mg, and group N received intramuscular normal saline(2mL. All patients received the drug at 30 minutes before surgery. Basal heart rate(HRand meananerial pressure(HAPwere recorded on the day before surgery. The intensity of pain was measured using(numeric rating scalesNRS(0-10, 0=no pain, 10=worst painand recorded during operation time(T1. Meanwhile, culocardiacreflex(OCR, nausea and vomiting, and sweating were also recorded. NRS, nausea and vomiting were recorded at 2 hours(T2, 4 hours(T3, 8 hours(T4after operation. RESULTS: The NRS scores at T1 were significantly lower in groups P, B, and D than in group N. OCR, nausea and vomiting, and sweating at T1 were not significantly different among the 4 groups. The nausea and vomiting were significantly higher in group D than in groups P, B, and N. The NRS scores at T2 were not significantly different among the 4 groups. The NRS scores in groups D and N at T3 were significantly higher than those at T2. And the NRS scores at T3 were significantly higher in group D and N than groups P and B. The nausea and vomiting were significantly higher in group D than in groups P, B, and N. The NRS, nausea and vomiting were not significantly different among the 4 groups. The NRS scores in groups P and B were not significantly different at T2, T3, and T4. CONCLUSION:Preemptive analgesia with 40mg of parecoxib for strabismus surgery under local anesthesia is effective intraoperatively and postoperatively, and can reduce the postoperative nausea and vomiting.

Chun - Jian Li

2013-05-01

252

Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis  

Directory of Open Access Journals (Sweden)

Full Text Available Abstract Background Pain and impaired mobility because of osteoarthritis (OA is common in dogs and humans. Efficacy studies of analgesic drug treatment of dogs with naturally occurring OA may be challenging, as a caregiver placebo effect is typically evident. However, little is known about effect sizes of common outcome-measures in canine clinical trials evaluating treatment of OA pain. Forty-nine client-owned dogs with hip OA were enrolled in a randomized, double-blinded placebo-controlled prospective trial. After a 1 week baseline period, dogs were randomly assigned to a treatment (ABT-116 – transient receptor potential vanilloid 1 (TRPV1 antagonist, Carprofen – non-steroidal anti-inflammatory drug (NSAID, Tramadol - synthetic opiate, or Placebo for 2 weeks. Outcome-measures included physical examination parameters, owner questionnaire, activity monitoring, gait analysis, and use of rescue medication. Results Acute hyperthermia developed after ABT-116 treatment (P P ? 0.01 and tramadol (P ? 0.001 led to improved mobility assessed by owner questionnaire. Nighttime activity was increased after ABT-116 treatment (P = 0.01. Kinetic gait analysis did not reveal significant treatment effects. Use of rescue treatment decreased with treatment in the ABT-116 and Carprofen groups (P R ? ±0.40, P ? 0.005. Placebo treatment effects were evident with all variables studied. Conclusion Treatment of hip OA in client-owned dogs is associated with a placebo effect for all variables that are commonly used for efficacy studies of analgesic drugs. This likely reflects caregiver bias or the phenomenon of regression to the mean. In the present study, outcome measures with significant effects also varied between groups, highlighting the value of using multiple outcome measures, as well as an a priori analysis of effect size associated with each measure. Effect size data from the present study could be used to inform design of future trials studying analgesic treatment of canine OA. Our results suggest that analgesic treatment with ABT-116 is not as effective as carprofen or tramadol for treatment of hip arthritis pain in client-owned dogs.

Malek Sarah

2012-10-01

253

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

Directory of Open Access Journals (Sweden)

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.

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

2004-04-01

254

Evaluation of the analgesic effect of salmon calcitonin in metastatic bone pain  

Directory of Open Access Journals (Sweden)

Full Text Available Aim: To evaluate the efficacy of calcitonin in controlling metastatic bone pain. Materials and methods: Patients with bone metastases, with a numerical pain score greater than 4 wererandomized to receive calcitonin 200 IU subcutaneously 6 hourly for 48 hours (n= 10 or normal saline placebo (n = 10 . The parameters measured were the 11-point numerical pain score, ECOG functional capacity score, morphine consumption in 24 hours, duration of pain in 24 hours and subjective assessment of efficacy of treatment by a blinded investigator. Results: There was a statistically significant decrease in pain score at 48 hours (2 vs 6 and 7 days (3 vs 6 in the calcitonin arm as compared to the control arm. The reduction in duration of pain (3 vs 13 and improvement in ECOG (1.5 vs 2.5 score were also statistically significant. Adverse effects were nausea in 5 patients and vomiting in 3 patients on the day of calcitonin administration. This was controlled with antiemetics. There was no significant change in serum calcium level in either group.

Mishra Seema

2003-01-01

255

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

Directory of Open Access Journals (Sweden)

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.

Y.J. Mousa

2012-01-01

256

The analgesic and antiplasmodial activities and toxicology of Vernonia amygdalina.  

Science.gov (United States)

Vernonia amygdalina possesses several bioactive compounds and is used in traditional medicines of southwestern Uganda, along with other regions. Its analgesic potential has not been investigated thus far. The present study examines the antinociceptive potential of the aqueous leaf extract (50-200 mg/kg) using three models of nociception (acetic acid-induced writhing, formalin test, and tail-flick test), antiplasmodial activity, and toxicology of the extract. The results show the extract significantly inhibits acetic acid-induced writhing and the formalin test in mice but did not give a potent effect in the tail-flick test, suggesting that the extract may have peripheral and central analgesic properties. The extract also exhibited significant antiplasmodial activity in mice against Plasmodium berghei with 73% inhibition in the group that received a dose of 200 mg/kg i.p. daily for 4 days. Toxicology results show no clinical signs of toxicity or adverse toxicological effects in the treated groups, except for a significant decrease in red blood cell count and a dose-dependent increase in serum bilirubin. These changes were within control values based on historical reference ranges at doses of 500-2,000 mg/kg/day for 14 consecutive days as compared to the control. This study supports the traditional use of V. amygdalina as an alternative therapy for malaria and the symptomatic relief of pain usually associated with malaria. PMID:18800909

Njan, Anoka A; Adzu, Bulus; Agaba, Amon G; Byarugaba, Dominic; Díaz-Llera, Silvia; Bangsberg, David R

2008-09-01

257

The effects of peripheral wall conduction in pool boiling  

International Nuclear Information System (INIS)

Given uniform heat generation within a heater placed in an asymmetrical fluid boundary condition, as in the case of a horizontally placed cylindrical heater in pool boiling, heat flows by conduction within the wall of the heater and creates a non-uniform wall surface temperature distribution. The authors conclude that it is known that when all other flow conditions are equal, the overall heat transfer rate is strongly affected by the heating boundary conditions. This is because the local heat transfer is a function of the local thermal conditions affected by the physical dimensions and thermal properties of the heater. Therefore, a study on the boiling heat transfer from a heater placed in an asymmetric heating condition must recognize the effect of the peripheral wall conduction on the overall heat transfer rate. To compare the experimental results obtained by different investigators, all parameters governing the heat transfer process should be set equal. Seldom included is the effect of the variation of the surface temperature, which is dependent on the Biot Number, and the specific heat generation rate of the heater. A few studies on boiling heat transfer indirectly recognize this variation of the surface temperature on the surface heat transfer coefficient

258

Testing and Comparison of Non-Opioid Analgesics in Amphibians  

OpenAIRE

Because of the lack of information about effective analgesics in non-mammalian vertebrates, the potency of various non-opioid agents were tested in a model of analgesia by using Northern grass frogs (Rana pipiens). This alternative model has been used widely for investigating opioid analgesic action. Potential non-opioid analgesics tested included antipsychotic, benzodiazepine, barbiturate, antihistamine, non-steroidal anti-inflammatory (NSAID), and partial opioid agents. Northern grass frogs...

Stevens, Craig W.; Maciver, Donald N.; Newman, Leslie C.

2001-01-01

259

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

OpenAIRE

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...

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

1998-01-01

260

Antidepressants as analgesics: a review of randomized controlled trials.  

OpenAIRE

This review provides an overview of 59 randomized placebo-controlled trials that examined the analgesic effect of antidepressants. To summarize, there is significant evidence that the tricyclic group of antidepressants is analgesic and that trazodone is not; the data regarding selective serotonin reuptake inhibitors are conflicting. To date, there are no randomized controlled trials examining the potential analgesic action of nefazodone or venlafaxine, but on the basis of initial clinical rep...

Lynch, M. E.

2001-01-01

261

United Kingdom legislation on pack sizes of analgesics: background, rationale, and effects on suicide and deliberate self-harm.  

OpenAIRE

Following increasing concern in the UK about the mortality and morbidity associated with self-poisoning with analgesics, especially paracetamol (Tylenol, acetaminophen), legislation was introduced in 1998 to modify packs sold over-the-counter. The most important change was a reduction in the maximum size of packs. In this paper the background to the legislation, the rationale behind it, and its early impact are reviewed. The changes have had significant positive initial benefits on the mortal...

Hawton, K.

2002-01-01

262

Perspective of nurses on effective factors on their decisions to administer PRN analgesics to children after surgery  

OpenAIRE

Post-surgery pain is usually controlled by PRN drugs administered by nurses. According to the decision-making theories, this clinical decision-making depends on three factors: nurse-related factors; child-related factors; and hospital-related factors. This study deals with the first and second factors mentioned. This descriptive-analytic study aims at determining the perspective of nurses on factors which affect their decisions to administer the analgesic PRN to children after surgery in seve...

Karimi; Parsa-yekta, R.; Mehran, Z.; Nik-farid, A.; L.

2002-01-01

263

Peripheral oedema as a side-effect of fluticasone  

OpenAIRE

A 14-year-old girl had experienced gross peripheral oedema for nearly 2 years. She was under review by several paediatric specialists for a variety of problems. Her local paediatric team were unable to find the cause of her oedema, despite extensive investigations. Eventually, her mother discovered the cause was inhaled fluticasone, prescribed at normal dosage for asthma. As far as the authors are aware, this is the first reported case of peripheral oedema associated with the use of fluticaso...

Myers, Alice; Godden, Charles

2010-01-01

264

The analgesic effect of the GABA-agonist THIP in patients with chronic pain of malignant origin. A phase-1-2 study.  

OpenAIRE

Fourteen patients with chronic pain of malignant origin were treated with escalating doses of THIP intramuscularly 5-30 mg in an open phase 1 study. Analgesic activity was demonstrated in 60% of the patients at the level of 20 mg THIP and a dose response relation was present. Side effects, sedation, dizziness, euphoria, nausea, and blurred vision were present in up to 80% of the patients and were dose limiting. The maximum serum concentration was reached within 1 h after dosing in 87% of all ...

Kjaer, M.; Nielsen, H.

1983-01-01

265

Effects of Passive Physical Exercise on Peripheral Vision in Muscular Dystrophic Children.  

Science.gov (United States)

The effects of passive exercise of the extremities on peripheral vision of muscular dystrophic children aged 9 to 13 years was investigated. Compared to control subjects, those who experienced six minutes of passive exercise evidenced increased peripheral vision. Curriculum revisions for muscular dystrophic children indicate the importance of…

Eickelberg, Warren; And Others

1983-01-01

266

Evaluation of analgesic activity of Emblica officinalis in albino rats  

Directory of Open Access Journals (Sweden)

Results: Emblica officinalis extract did not produced statistically significant (p>0.05 analgesia when compared with the control group in hot plate latency, but produced a statistically significant reduction in 6% NaCl induced abdominal writhing (pEmblica officinalis exhibit analgesic activity involving peripheral mechanisms. [Int J Basic Clin Pharmacol 2014; 3(2.000: 365-368

Bhomik Goel

2014-04-01

267

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)

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

Muthanna F Abdulkarim

2010-11-01

268

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)

[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

Bae, Young-Hyeon; Lee, Suk Min

2014-12-01

269

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

Science.gov (United States)

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

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

2012-10-01

270

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)

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.

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

2011-09-01

271

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

Directory of Open Access Journals (Sweden)

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

Meregalli C

2012-06-01

272

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

Science.gov (United States)

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 ?g/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 ?M, 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. PMID:22792002

Meregalli, Cristina; Ceresa, Cecilia; Canta, Annalisa; Carozzi, Valentina Alda; Chiorazzi, Alessia; Sala, Barbara; Oggioni, Norberto; Lanza, Marco; Letari, Ornella; Ferrari, Flora; Avezza, Federica; Marmiroli, Paola; Caselli, Gianfranco; Cavaletti, Guido

2012-01-01

273

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

Directory of Open Access Journals (Sweden)

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.

Kim Min-jung

2013-09-01

274

Analgesic Activity of Psidium guajava root extracts  

Directory of Open Access Journals (Sweden)

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.

Girish Kumar Gupta1, Manisha Bhatia, Randhir Singh

2013-03-01

275

Paracetamol and analgesic nephropathy: Are you kidneying me?  

Directory of Open Access Journals (Sweden)

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

Waddington F

2014-12-01

276

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

Science.gov (United States)

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

Hesselink, Jan M Keppel

2013-01-01

277

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

Directory of Open Access Journals (Sweden)

Full Text Available Jan M Keppel Hesselink Department of Pharmacology, University of Witten/Herdecke, Witten, Germany Abstract: 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. Keywords: palmitoylethanolamide, sociology, science, paradigm, peroxisome proliferator-activated receptor-alpha, nutraceutical

Keppel Hesselink JM

2013-08-01

278

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)

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.

O.J. Olorunfemi

2012-04-01

279

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

Science.gov (United States)

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

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

1998-01-01

280

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)

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

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

1999-12-01

281

Observation of the curative effect of decompression of peripheral nerve for greater occipital neuralgia  

OpenAIRE

Objective To investigate the efficacy of decompression of peripheral nerve for greater occipital neuralgia. Methods A total of 62 patients with greater occipital neuralgia were given greater occipital nerve decompression under local anesthesia, and were followed up 6-12 months later. Results There were 54 cases cured, 5 cases effective, 2 cases ineffective, and 1 case lost during the follow-up period. Conclusion The decompression of peripheral nerve is a safe and effective method for g...

Liu, Qing-jun; Han, Yan-qing; Zhu, Jun

2013-01-01

282

Observation of the curative effect of decompression of peripheral nerve for greater occipital neuralgia  

Directory of Open Access Journals (Sweden)

Full Text Available Objective To investigate the efficacy of decompression of peripheral nerve for greater occipital neuralgia. Methods A total of 62 patients with greater occipital neuralgia were given greater occipital nerve decompression under local anesthesia, and were followed up 6-12 months later. Results There were 54 cases cured, 5 cases effective, 2 cases ineffective, and 1 case lost during the follow-up period. Conclusion The decompression of peripheral nerve is a safe and effective method for greater occipital neuralgia.

LIU Qing-jun

2013-10-01

283

Effect of indomethacin on peripheral blood count of gamma-irradiated laboratory rats  

International Nuclear Information System (INIS)

The effect was studied of single or repeat injection administration of indomethacin on the peripheral blood count of gamma-irradiated rats with single whole-body doses (5.5 and 6.0 Gy). It was found that the post-irradiation administration of indomethacin stimulated the recovery of the peripheral granulocyte count. The stimulating effects of indomethacin on the granulocyte level in peripheral blood were also apparent in non-irradiated rats. The unfavourable effect of higher doses of indomethacin became apparent in a decreased red blood cell count in peripheral blood, possibly caused by the ulcerogenic influence of this non-steroid antiinflammatory drug on mucous membrane of the gastrointestinal tract with subsequent bleeding. (author). 2 figs., 15 refs

284

The effect of glycomimetic functionalized collagen on peripheral nerve repair  

OpenAIRE

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...

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

2012-01-01

285

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)

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.

Homa Manaheji

2011-02-01

286

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

Directory of Open Access Journals (Sweden)

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.

Wang Wen

2011-01-01

287

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)

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

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

2013-08-19

288

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)

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.

Fábio José Reis

2006-12-01

289

Involvement of Moesin in the Development of Morphine Analgesic Tolerance through P-glycoprotein at the Blood-Brain Barrier.  

Science.gov (United States)

?Altered expression of P-glycoprotein (P-gp), a drug efflux transporter expressed by brain capillary endothelial cells (BCECs), may contribute to the development of opioid analgesic tolerance, as demonstrated by cumulative evidence from research. However, the detailed mechanism by which chronic morphine treatment increases P-gp expression remains unexplained. Ezrin/radixin/moesin (ERM) are scaffold proteins that are known to regulate the plasma membrane localization of some drug transporters such as P-gp in peripheral tissues, although a few reports suggest its role in the central nervous system as well. In this study, we investigated the involvement of ERM in the development of morphine analgesic tolerance through altered P-gp expression in BCECs. Repeated treatment with morphine (10 mg/kg/day, s.c. for 5 days) decreased its analgesic effect in the tail-flick test and increased P-gp protein expression in BCECs, as determined by western blotting. Furthermore, moesin protein expression increased in the same fraction whereas that of ezrin decreased; no change was observed in the radixin expression. Furthermore, immunoprecipitation and immunofluorescence assays revealed interaction between moesin and P-gp molecules, along with co-localization, in BCECs. In conclusion, an increase in moesin expression may contribute to the increased expression of P-gp in BCECs, leading to the development of morphine analgesic tolerance. PMID:25048710

Kobori, Takuro; Fujiwara, Shuhei; Miyagi, Kei; Harada, Shinichi; Nakamoto, Kazuo; Nakagawa, Takayuki; Takahashi, Hideo; Narita, Minoru; Tokuyama, Shogo

2014-07-22

290

A comparative study of analgesic property of whole plant and fruit extracts of Fragaria vesca in experimental animal models  

OpenAIRE

The aim of the study was to compare the analgesic activities of ethanolic extract of fruits and whole plant of Fragaria vesca in experimental animal models. The extracts were prepared by percolation method and oral toxicity testing was performed as per OECD guidelines. Analgesic activity was assessed by tail flickmethod (for central action) and acetic acid-induced writhing test (for peripheral action). Fruit extract, whole plant extract and aspirin showed significant analgesic activity, both ...

Lalit Kanodia; Swarnamoni Das

2009-01-01

291

EXPERIMENTAL EVALUATION FOR ANALGESIC ACTIVITY OF MAMSYADI KWATHA  

Directory of Open Access Journals (Sweden)

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.

Shreevathsa

2011-04-01

292

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

Directory of Open Access Journals (Sweden)

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.

Naumenko L.Yu.

2010-01-01

293

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

Directory of Open Access Journals (Sweden)

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.

Leila Ahmad-Molaei

2011-10-01

294

Twelve cases of analgesic headache  

OpenAIRE

Analgesic headache occurs when drugs given for the treatment of headache aggravate symptoms. The condition is well recognised in adults but has not been described before in children in whom it may be induced by mild analgesics such as paracetamol used alone. Twelve children (nine girls and three boys, aged 6 to 16.5years) with analgesic headache (from three months to 10 years) are reported. Five children were taking paracetamol alone, six were taking paracetamol with code...

Symon, D.

1998-01-01

295

Effect of hydrocortisone on interleukin-6 production in human ,peripheral blood rnononuclear ceils  

OpenAIRE

The effect of hydrocortisone on the production of interleukin-6 (IL-6) in human peripheral blood mononuclear cells was studied. Using our newly developed radioimmunoassay system for IL-6 of which specificity, reproducibility, sensitivity and usefulness have been demonstrated. IL-6 production in peripheral blood mononuclear cells of ten normal subjects revealed that in lipopolysaccharide (LPS, 10?g/ml)-stimulation, the mean ± SD of IL-6 was 2.71 ± 0.85 ng/ml. No detecta...

Hirooka, Y.; Mitsuma, T.; Nogimori, T.; Ishizukis, Y.

1992-01-01

296

Effects of snake venom from Saudi cobras and vipers on hormonal levels in peripheral blood.  

OpenAIRE

OBJECTIVES Knowledge about the effects of snake venoms on endocrine glands in the Kingdom of Saudi Arabia (KSA) is meager. The aim of the present study is to investigate the acute and chronic envenomation from 4 snakes out of 8 species of Saudi Cobras and Vipers on the tissues of endocrine glands and peripheral hormonal levels in male rats. METHODS The peripheral blood levels of 4 hormones mainly testosterone, cortisol, insulin and thyr...

Abdel-galil, Khidir A.; Al-hazimi, Awdah M.

2004-01-01

297

Steroid metabolism and effects in central and peripheral glial cells  

OpenAIRE

Hormonal steroids participate in the control of a large number of functions of the central nervous system (CNS); recent data show that they may also intervene at the level of the peripheral nervous system (PNS). Both the CNS and the PNS metabolize endogenous as well as exogenous steroids; one of the major enzymatic system is represented by the 5alpha-reductase-3alpha-hydroxysteroid complex. This is a versatile system, since every steroid possessing the delta 4-3keto configuration (e.g., testo...

Melcangi, Cosimo; Magnaghi, Valerio; Martini, Luciano

1999-01-01

298

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)

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.

Torrades Sandra

2011-01-01

299

Analgesic and anti-inflammatory studies of cyclopeptide alkaloid fraction of leaves of Ziziyphus nummularia.  

Science.gov (United States)

Ziziyphus nummularia (family: Rhamnaceae) is a thorny small bush, grows in abundance in the grazing lands of the arid areas of Rajasthan, India. It is an important ethnomedicinal plant of the Thar Desert; local inhabitants use every part of the plant as medicine. Kernels are prescribed in pregnancy as soporific, antiemetic and for relieving abdominal pain. The insect gall is powered and given orally with water to cure bone fracture. Crushed root is applied on the paining shoulder of the bullock. The decoction of leaves is used for the treatment of cough and cold; leaves are also regarded as diaphoretic and prescribed in typhoid. Paste of leaves is used for healing of cuts, boils and cutaneous disease. It is widely used in pain and inflammatory conditions. Z. nummularia contains a unique group of alkaloids known as cyclopeptide alkaloids, in continuation of our work carried out on the leaves of Z. nummularia , present study was initiated to explore antiinflammatory and analgesic potential of cyclopeptide alkaloids isolated from the leaves of Z. nummularia (IFZN). Anti-inflammatory activity was tested against rat paw oedema, mouse peritonitis and cotton pellet granuloma. For screening of analgesic activity, acetic acid induced writhing, tail flick and hot plate test were performed. IFZN 30 mg/kg shows the anti-oedematogenic effect against paw oedema induced by carrageenan, dextran, serotonin and histamine; IFZN 20 and 30 mg/kg were found to have highly significant anti-nociceptive effects. Result of pharmacological studies indicated that IFZN is a potent and efficacious analgesic agent. The analgesic activity of IFZN is mediated by the peripheral as well as central pathways. PMID:24235873

Goyal, Manoj; Ghosh, Manik; Nagori, B P; Sasmal, D

2013-10-01

300

[Present status of the use of adjuvant analgesics in Japan].  

Science.gov (United States)

Adjuvant analgesics are drugs that have primary indications other than pain but are analgesic in selected circumstances. Antidepressants, anticonvulsants, local anesthetics, and NMDA receptor antagonists are drugs used in the treatment of neuropathic cancer pain. Assessment of pain is very important in selecting appropriate adjuvant analgesics. The assessment includes visual analog scale for pain intensity, McGill Pain Questionaire for quality of pain, and the location of pain. It is also important to assess the effectiveness of immediate release opioids. Most neuropathic pain is thought to be refractory to opioids. In Japan, effective adjuvant analgesics such as gabapentin and pregabalin are not available. The main adjuvant analgesics are still tricyclic antidepressants such as amytriptylin and amoxapin, and anticonvulsants such as carbamazepin and clonazepam. Another problem is that morphine is the only rescue drug available for the assessment of opioid responsiveness since morphine is the only opioid with an immediately release form among the strong opioids available in Japan which are morphine, oxycodone, and fentanyl. Adjuvant analgesics also have side effects such as constipation and sleepiness, which may augment the side effects of morphine and may impair the QOL of cancer patients with neuropathic pain. There is a need to improve the systems of development and importation of adjuvant analgesics. PMID:17233416

Nakayama, Rika; Takahashi, Hidenori; Shimoyama, Naohito

2007-01-01

301

Tapentadol-ER for the treatment of diabetic peripheral neuropathy.  

Science.gov (United States)

With the prevalence of diabetes mellitus (DM) increasing, pathologic complications such as diabetic peripheral neuropathy (DPN) are also becoming more common. Of those diagnosed with DM, 10% to 20% of patients suffer from painful DPN. Until recently, only pregabalin and duloxetine possessed Food and Drug Administration (FDA) approval for this condition. However, FDA recently approved tapentadol-ER [extended release] (Nucynta ER) for painful DPN. Tapentadol-ER is an opioid analgesic commonly used for the treatment of moderate-to-severe chronic pain that contains a unique dual mechanism acting as both a weak mu-opiod receptor agonist and norepinephine-reuptake inhibitor. It is by way of this unique dual mechanism that allows for effective analgesic effects with increased tolerability. This new FDA approval provides an additional therapeutic option to treat DPN in symptomatic patients. PMID:24129223

Games, Gina; Hutchison, Amber

2013-10-01

302

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

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: English Abstract in portuguese 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.

Marcelo E., Bigal.

2011-06-01

303

Can quantitative sensory testing predict responses to analgesic treatment?  

DEFF Research Database (Denmark)

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.

Grosen, K; Fischer, Iben W. Deleuran

2013-01-01

304

Investigation of central versus peripheral effects of estradiol in ovariectomized mice.  

Science.gov (United States)

It is generally believed that estrogens exert their bone sparing effects directly on the cells within the bone compartment. The aim of the present study was to investigate if central mechanisms might be involved in the bone sparing effect of estrogens. The dose-response of central (i.c.v) 17beta-estradiol (E2) administration was compared with that of peripheral (s.c.) administration in ovariectomized (ovx) mice. The dose-response curves for central and peripheral E2 administration did not differ for any of the studied estrogen-responsive tissues, indicating that these effects were mainly peripheral. In addition, ovx mice were treated with E2 and/or the peripheral estrogen receptor antagonist ICI 182,780. ICI 182,780 attenuated most of the estrogenic response regarding uterus weight, retroperitoneal fat weight, cortical BMC and trabecular bone mineral content (P<0.05). These findings support the notion that the primary target tissue that mediates the effect of E2 on bone is peripheral and not central. PMID:16293778

Andersson, Niklas; Islander, Ulrika; Egecioglu, Emil; Löf, Elin; Swanson, Charlotte; Movérare-Skrtic, Sofia; Sjögren, Klara; Lindberg, Marie K; Carlsten, Hans; Ohlsson, Claes

2005-11-01

305

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)

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.

Khaled Taha

2003-09-01

306

Bovine dehorning: assessing pain and providing analgesic management.  

Science.gov (United States)

Dehorning or disbudding in cattle is performed for a variety of reasons using various methods. Pain associated with this procedure has been mostly evaluated through behavioral, physiologic, and neuroendocrine changes following dehorning. Analgesics, including local nerve blockades, anti-inflammatories, and opioids have demonstrated an effective attenuation of the cortisol response. The administration of sedatives with analgesic properties has been indicated in the attenuation of the acute phase of pain associated with dehorning. Following a literature review, this article recommends a multimodal approach to analgesia for dehorning procedures, including the use of a local anesthetic and anti-inflammatory and, when possible, a sedative-analgesic. PMID:23438402

Stock, Matthew L; Baldridge, Sarah L; Griffin, Dee; Coetzee, Johann F

2013-03-01

307

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

Energy Technology Data Exchange (ETDEWEB)

In order to test the hypothesis that peripheral benzodiazepine binding sites mediate some direct effects of benzodiazepines on striated muscles, the properties of specific /sup 3/H-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 /sup 3/H-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.

Mueller, W.E.; Ickstadt, A. (Mainz Univ. (Germany, F.R.). Pharmakologisches Inst.); Hopf, H.Ch. (Mainz Univ. (Germany, F.R.))

1985-01-01

308

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)

309

Diferentes doses de tramadol em cães: ações analgésicas, sedativas e sobre o sistema cardiorrespiratório / Different doses of tramadol in dogs: analgesic, sedative and cardiopulmonary effects  

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: Portuguese Abstract in portuguese Objetivou-se comparar os efeitos cardiorrespiratório, analgésico e sedativo de diferentes doses de tramadol em cadelas submetidas à ovariosalpingohisterectomia (OSH). Foram avaliadas 24 cadelas SRD, adultas, distribuídas aleatoriamente em três grupos de oito animais, tratados com tramadol pela via i [...] ntravenosa (IV) nas doses de 1, 2 e 4mg kg-1 (T1, T2 e T4, respectivamente). Na medicação pré-anestésica, foi administrada acepromazina (0,05mg kg-1 IV). Vinte minutos após, a anestesia foi induzida com propofol (4mg kg-1 IV), com posterior manutenção anestésica com isofluorano. O tramadol foi administrado 5 minutos antes da incisão cirúrgica em todos os tratamentos. Foram mensurados: frequência cardíaca, frequência respiratória, temperatura retal, pressão arterial sistólica, grau de analgesia, grau de sedação, concentração sérica de cortisol e efeitos adversos. Mínimas alterações cardiorrespiratórias foram observadas, sem diferença entre os tratamentos. O cortisol, o grau de sedação e o grau de analgesia não variaram entre os tratamentos, com exceção da terceira hora pós-cirúrgica, em que menores escores de dor foram observados no T4. Vômito foi observado em 50% dos animais do T4. Conclui-se que as diferentes doses de tramadol induziram efeitos analgésicos semelhantes, com discreto efeito sedativo e mínimas alterações cardiorrespiratórias. Paralelamente, a dose de 4mg kg-1 de tramadol induziu alta incidência de vômito em cadelas submetidas à OSH. Abstract in english The aim of this study was compare the cardiopulmonary, analgesic and sedative effects of different doses of tramadol in bitches undergoing to ovariohysterectomy. Twenty four adult crossbreed bitches were randomly assigned to three treatments of 8 animals and received intravenously (IV) tramadol 1, 2 [...] or 4mg kg-1 (T1, T2 and T4, respectively). Pre-anesthetic medication was acepromazine (0.05mg kg-1 IV). Anesthesia was induced with propofol (4mg kg-1 IV) and maintained with isoflurane delivered in oxygen. Tramadol was administered 5 minutes before surgical incision in all groups. Heart rate, respiratory rate, rectal temperature, systolic blood pressure, degree of analgesia and sedation, serum cortisol concentration and adverse effects were measured. Mild changes were observed in cardiopulmonary variables in all treatments. The pain score was lower in T4 in the 3rd hour after surgery in relation to other treatments. Sedation degree was not different among the treatments. The serum cortisol did not differ among the groups. In conclusion, different doses of tramadol promoted similar analgesic effects, with mild sedative and cardiopulmonary effects. However, high incidence of vomiting was observed with tramadol at 4mg kg-1 in bitches undergoing ovariohysterectomy.

Rodrigo Jesus, Paolozzi; Renata Navarro, Cassu; Fernando Silvério Ferreira da, Cruz; Letícia Rodrigues, Parrilha.

1417-14-01

310

Non-steroidal anti-inflammatory analgesics other than salicylates.  

Science.gov (United States)

The largest group of non-narcotic analgesics are the arylalkanoic acid derivatives, comprising derivatives of arylacetic acid, propionic acid, heteraryl acetic acid and indole acetic acid. Common to all of these drugs is their inhibition of prostaglandin biosynthesis, which contributes to their analgesic and other pharmacological properties as well as to their principal side effect, gastrointestinal irritation. Although these drugs all cause some gastric microbleeding, they do so to a lesser extent than aspirin. The arylalkanoic acid derivatives, as well as the anthranilic acid and oxicam derivatives, are peripherally acting as evidenced by their lack of activity in classical tests of central analgesic activity. After oral administration of these drugs, their peak plasma concentrations are generally attained in 1 to 3 hours; absorption is not generally influenced by food. Volume of distribution is mostly low (less than 0.2 L/kg) and protein binding is high (usually 95 to 99%). Elimination is by glucuronide formation for several of the propionic acid derivatives and generally by biotransformation for derivatives of arylacetic acid, indole and indene acetic acid, and the oxicams. The elimination half-life of the arylalkanoic acid derivatives is in most instances about 2 to 5 hours, although notable exceptions include carprofen (approximately equal to 20 h), fenbufen (10 h), naproxen (12-15 h) and sulindac (16 h for the active metabolite). The elimination half-life of indomethacin varies considerably between and within individuals. Piroxicam has the longest half-life, averaging 45 hours. The pharmacokinetic properties of the anthranilic acid derivatives (fenamates, glafenine) generally resemble those of the arylacetic acids. Few clinically significant drug interactions are associated with concomitant administration of the arylalkanoic acids or piroxicam and other drugs. Since the arylalkanoic acids are highly bound to plasma proteins (mainly albumin) there is a theoretical potential for displacement reactions with drugs that are used at plasma concentrations high enough to exceed the binding capacity of their own primary binding sites. However, such reactions have rarely been reported. Although the concomitant administration of aspirin and several of the propionic acid derivatives results in a significant decrease in the plasma concentration of the latter, the clinical significance of such interactions is uncertain and probably minimal.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:3552584

Brogden, R N

1986-01-01

311

The effects of peripheral vascular disease on gait.  

Science.gov (United States)

This study was designed to determine whether patients with peripheral vascular disease (PVD) have gait abnormalities. A previous study on humans with PVD found no abnormalities whereas significant gait changes were seen with a rat model of PVD. The study population was comprised of 10 controls and 9 subjects with PVD (all male). The PVD group had documented pain in one or both legs while walking. Subjects ranged in age from 55-92 years of age, with a mean age of 69 in the PVD group and 70 in the control group. The GaitMat II system was used to measure both spatial and temporal variables of gait. Subjects walked across the mat, four to six times, at their comfortable walking speed. The PVD group then walked on a treadmill until they experienced moderate claudication pain and felt they had to stop (pain levels between 6 and 8, with maximal pain at level 10). Control group walked on a treadmill for 10 minutes without pain. All subjects repeated the gait tests on the GaitMat H system immediately after treadmill walking. Claudication pain persisted in the PVD group during the second gait test. The PVD group was not different than control group in any of the measured variables on the first test (p values from .35 to .99). Difference scores (post- minus pre-treadmill walking)for PVD group were significantly different than those for control group on 8 of 11 variables (p values <.005). The primary response in PVD subjects was reduced walking speed (1.02+/-0.16 to 0.94+/-0.16 m/s) and reduced step length (0.60+/-0.08 to 0.57+/-0.09 m/s), whereas control subjects increased their speed (1.09+/-0.17 to 1.19+/-0.19 m/s) and step length (0.63+/-0.10 to 0.67+/-0.10 m/s). No asymmetries in gait were measured in either group, either before or after treadmill walking. In conclusion, PVD subjects were not different in gait while rested, but responded to claudication pain by reducing preferred walking speed and step size. PMID:10462161

McCully, K; Leiper, C; Sanders, T; Griffin, E

1999-07-01

312

Dextropropoxyphene withdrawal from a French university hospital: impact on analgesic drug consumption.  

Science.gov (United States)

Dextropropoxyphene is a weak opioid analgesic, widely used as a step 2 analgesic (according to WHO classification) in combination with peripheral analgesics, mainly paracetamol. Recent data have underlined its poor analgesic efficacy (in comparison with paracetamol), risks of serious adverse drug reactions (i.e. hepatic reactions, hallucinations, abuse, withdrawal symptoms, hypoglycaemia), possible lethality after overdose, its risk of accumulation in patients with renal failure or in elderly people and some pharmacokinetic insufficiencies (i.e. different half-lives for dextropropoxyphene and paracetamol). Taking into account these data, the drug committee of the Toulouse University Hospital (France) decided to withdraw dextropropoxyphene from the hospital formulary since 1 June 2005. The aim of our study was to investigate the consequences of this withdrawal by comparing use of analgesic drugs in Toulouse University Hospital before (2004) and after (2006) dextropropoxyphene withdrawal (using defined daily dose for 1000 hospitalization-days as the unit measure). Before withdrawal, dextropropoxyphene (in combination with paracetamol) was the second most used analgesic drug after paracetamol alone. After dextropropoxyphene withdrawal, total consumption of analgesic drugs decreased by 4.6% (2006 vs. 2004). There was a 28% decrease in consumption of step 2 analgesics [with an increase in oral tramadol and a slight decrease in codeine (in combination with paracetamol)]. During the same period, step 1 analgesic consumption increased by 11% (mainly paracetamol) and that of step 3 analgesics slightly decreased (-8%). These results show that dextropropoxyphene withdrawal was not associated with a marked switch in prescriptions towards other analgesic drugs. This paper underlines the interest of a hospital-based drug committee to promote rational drug use. Finally, the present data allow us to discuss putative misuse of dextropropoxyphene. PMID:19298233

Gaubert, Sabine; Vié, Martine; Damase-Michel, Christine; Pathak, Atul; Montastruc, Jean-Louis

2009-04-01

313

Antiinflammatory, Analgesic and Antipyretic Activities of Mimusops elengi Linn  

OpenAIRE

In the present study, 70% ethanol extract of Mimusops elengi Linn. bark was assessed for antiinflammatory, analgesic and antipyretic activities in animals. The antiinflammatory activity of ethanol extract of Mimusops elengi (200 mg/kg, p.o) was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma models. Analgesic effect was evaluated using acetic acid-induced writhing and Eddy’s hot plate models and antipyretic activity was assessed by Brewer’s yeast-induced ...

Purnima, A.; Koti, B. C.; Thippeswamy, A. H. M.; Jaji, M. S.; Swamy, A. H. M. Vishwantha; Kurhe, Y. V.; Sadiq, A. Jaffar

2010-01-01

314

Analgesic activity of diterpene alkaloids from Aconitum baikalensis.  

Science.gov (United States)

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

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

315

Analgesic effect of milnacipran is associated with c-Fos expression in the anterior cingulate cortex in the rat neuropathic pain model.  

Science.gov (United States)

The objective of the present study was to examine whether milnacipran, a serotonin-noradrenaline reuptake inhibitor, has an analgesic effect in rats with neuropathic pain. In addition, the c-Fos expression was investigated in the supraspinal sites of the brain and in the spinal dorsal horn in association with the nociceptive processing in rats with neuropathic pain produced by chronic constriction injury (CCI) in the sciatic nerve. In the CCI-induced neuropathic rats, behavioral testing for determining the change in the withdrawal threshold to mechanical stimulation and immunohistochemical detection of c-Fos were both performed. The anti-allodynic effect derived from milnacipran gradually increased over the observation period, indicating that the delayed-onset analgesia might be elicited by the continuous administration of milnacipran. The increased level of c-Fos expression in the anterior cingulate cortex (ACC) induced by noxious mechanical stimulation was significantly inhibited by the continuous administration of milnacipran, indicating that milnacipran might cause a functional modification in the nociceptive processing in the ACC. PMID:19383518

Takeda, Ryuichiro; Watanabe, Yuko; Ikeda, Tetsuya; Abe, Hiroshi; Ebihara, Kosuke; Matsuo, Hisae; Nonaka, Hiroi; Hashiguchi, Hiroyuki; Nishimori, Toshikazu; Ishida, Yasushi

2009-08-01

316

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)

317

Effect of PACAP in Central and Peripheral Nerve Injuries  

OpenAIRE

Pituitary adenylate cyclase activating polypeptide (PACAP) is a bioactive peptide with diverse effects in the nervous system. In addition to its more classic role as a neuromodulator, PACAP functions as a neurotrophic factor. Several neurotrophic factors have been shown to play an important role in the endogenous response following both cerebral ischemia and traumatic brain injury and to be effective when given exogenously. A number of studies have shown the neuroprotective effect of PACAP in...

Andras Buki; Tamas Doczi; Zalan Szanto; Endre Czeiter; Attila Schwarcz; Povlishock, John T.; Jozsef Pal; Erzsebet Kovesdi; Orsolya Farkas; Dora Reglodi; Andrea Tamas; Peter Bukovics

2012-01-01

318

Peripheral and Central Effects of Melatonin on Blood Pressure Regulation  

OpenAIRE

The pineal hormone, melatonin (N-acetyl-5-methoxytryptamine), shows potent receptor-dependent and -independent actions, which participate in blood pressure regulation. The antihypertensive effect of melatonin was demonstrated in experimental and clinical hypertension. Receptor-dependent effects are mediated predominantly through MT1 and MT2 G-protein coupled receptors. The pleiotropic receptor-independent effects of melatonin with a possible impact on blood pressure involve the reactive oxyge...

Olga Pechanova; Ludovit Paulis; Fedor Simko

2014-01-01

319

Analgesics and sedatives in vascular interventionist radiologic  

International Nuclear Information System (INIS)

Interventionist radiology routinely requires the use of different drugs (analgesics and sedatives) in the course of a procedure. Aside from their therapeutic action, these drugs can produce secondary or undesirable effects, making necessary an in-depth knowledge of them to assure their safe and efficient management. The aim of this work is to provide the vascular interventionist radiologist with additional information on the management of those drugs that contribute to minimizing patient discomfort and pain in interventionist procedures. Author

320

OTC analgesics and drug interactions: clinical implications  

OpenAIRE

The risk of drug interactions with concurrent use of multiple medications is a clinically relevant issue. Many patients are unaware that over-the-counter (OTC) analgesics can cause potentially serious adverse effects when used in combination with other common medications such as anticoagulants, corticosteroids, or antihypertensive agents. Of particular significance is the increased risk of upper abdominal gastrointestinal adverse events in patients who take traditional nonsteroidal anti-infla...

Fendrick, A. Mark; Pan, Deborah E.; Johnson, Grace E.

2008-01-01

321

Effects of food on the central and peripheral haemodynamic response to upright exercise in normal volunteers.  

OpenAIRE

The central and peripheral haemodynamic effects of a modest meal were investigated in healthy volunteers at rest and in response to submaximal exercise. The meal increased heart rate, cardiac output, oxygen consumption, carbon dioxide production, and minute ventilation at rest and during exercise. The effects of food were additive to those induced by the exercise. Food had no effect on limb blood flow and lowered total systemic vascular resistance suggesting that there were no compensatory ch...

Yi, J. J.; Fullwood, L.; Stainer, K.; Cowley, A. J.; Hampton, J. R.

1990-01-01

322

Opioid peptide-derived analgesics  

OpenAIRE

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...

Schiller, Peter W.

2005-01-01

323

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

DEFF Research Database (Denmark)

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.

LillesØ, J; Hammer, N A

2000-01-01

324

Analgesic use in dentistry in a tertiary hospital in western Nepal.  

Science.gov (United States)

The present study had been planned to determine the pattern of drug utilization of analgesics (non-opioid and opioid analgesics) in dental outpatients in a referral hospital in western Nepal. A total of 1820 prescriptions of dental patients attending the dental outpatient at Manipal Teaching Hospital (MTH), Fulbari, Pokhara, Nepal were collected by a random once-weekly survey between March 2001 and February 2002. The analgesic-containing prescriptions (n = 1346) were separated from the total prescriptions collected. This information was compiled, scored and analyzed in consultation with dentists using WHO guidelines. There were more female patients (56%) than male patients (44%) in this study. The dental disorders most frequently reported in our study were diseases of pulp and periapical tissue (36.5%), gingivitis and periodontal diseases (28.5%) and dental caries (16%) etc. In total, 74% prescriptions contained analgesics which are the second-most commonly prescribed drugs after anti-microbials (44.9%) in dental OPD. The total analgesics prescribed were 1358 that account for 36.7% of total drugs prescribed. Only 5 and 37.8% of analgesics were prescribed generically and from the essential drug list of WHO respectively. All the analgesics were administered orally which included 89.7 and 10.3% of non-opioid analgesics and opioid analgesics (propoxyphene and dextropopoxyphene) respectively. The average duration of analgesic use was 3.5 +/- 0.3 days. The most commonly prescribed non-opioid analgesic was ibuprofen (41%) followed by nimesulide (22%). A total of 38.9% analgesics were fixed-dose combinations (FDCs) of two drugs and the most common analgesic combination used was ibuprofen + paracetamol and paracetamol + opioid analgesics. All opioid analgesics were prescribed in combination with paracetamol (10.3%) only. In total, 1.6% analgesics were prescribed concomitantly with gastroprotective agents. All gastroprotective agents (n = 22) were prescribed concomitantly with opioid analgesics only. No gastroprotective was used when NSAIDs were prescribed alone or in combination with paracetamol. Our present study indicate that all the analgesics were prescribed in oral dosage forms but analgesics prescribed in generic name (5%) and from essential drug lists (37.8%) were very less. There was an inclination to prescribe the older non-opioid analgesics. Selection of analgesics was quite rational in our study but some lacunae were observed. A total of 38.9% analgesics were FDCs and most common FDC analgesics were ibuprofen + paracetamol. Avoiding unnecessary FDCs may help in reducing prescribing costs because FDCs usually cost more than single ingredient preparations. It is best to avoid combination therapy with more than one non-opioid analgesic; there is little evidence of extra benefit to the patient and the incidence of side effects generally is additive. Prescribing generic names aids in avoiding confusion and minimizing the costs. In the present study, coprescription of gastroprotective agents with analgesic use was low compared to a previous study but when opioid analgesics were prescribed, concurrent use of gastroprotective agents were irrational as opioid analgesics usually decrease the secretion of hydrochloric acid. It is also surprizing that, no gastroprotective was used when NSAIDs were prescribed alone, irrespective of sex, age, dose or duration or type of NSAID treatment in our study. There is a clear need for the development of prescribing guidelines and educational initiatives to encourage the rational and appropriate use of analgesics in dentistry. PMID:15386729

Sarkar, Chayna; Das, Biswadeep; Baral, P

2004-10-01

325

Synthesis and Analgesic Activity of Novel Hydrazide and Hydrazine Derivatives  

Science.gov (United States)

The uses of non-steroidal anti-inflammatory drugs (NSAIDs) are limited by a variety of side effects. So research on preparing new analgesic agents is important. According to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. The final compounds 10a-10e and 15a-15d were prepared by condensation of corresponding hydrazides 7,8 and 11-14 with different aldehydes 9a-9e. The structures of all synthesized compounds were confirmed by means of FT-IR, 1H-NMR and Mass spectra. All compounds were evaluated for their analgesic activities by abdominal constriction test (writhing test). Most of the synthesized compounds induced significant reduction in the writhing response when compared to control and compound 15 was more potent than mefenamic acid in the writhing test. PMID:24523751

Nassiri Koopaei, Mansur; Assarzadeh, Mohammad Javad; Almasirad, Ali; Ghasemi-Niri, Seyedeh Farnaz; Amini, Mohsen; Kebriaeezadeh, Abbas; Nassiri Koopaei, Nasser; Ghadimi, Maryam; Tabei, Arash

2013-01-01

326

Naloxone can act as an analgesic agent without measurable chronic side effects in mice with a mutant mu-opioid receptor expressed in different sites of pain pathway.  

Science.gov (United States)

Midbrain periaqueductal gray (PAG) and spinal cord dorsal horn are major action sites of opioid analgesics in the pain pathway. Our previous study has shown that opioid antagonists activate MORS196A-CSTA (a mutant of mu-opioid receptor) as full agonists in vitro cell models and naloxone showed antinociceptive effects after the expression of MORS196A-CSTA in the spinal cord in mice. The purpose of this study is to investigate the site-directed antinociceptive effects of naloxone in mice injected with dsAAV-MORS196A-CSTA-EGFP at spinal cord or at periaqueductal gray. MORS196A-CSTA-EGFP was administered to ICR mice using dsAAV as vector. We measured MORS196A-CSTA-EGFP expression by detecting the EGFP visualization with a fluorescence microscope. The antinociceptive effect of naloxone was determined by tail-flick test and hot plate test. Drug rewarding effect was evaluated by the conditioned place preference test. Naloxone (10 mg/kg, s.c.) elicited both supraspinal and spinal antinociceptive responses in mice injected with the virus at PAG while only spinal antinociceptive response was observed in mice injected with virus at dorsal horn region. Chronic naloxone treatment did not induce physical dependence or rewarding effect in mice injected with MORS196A-CSTA-EGFP in spinal cord or PAG. These data suggest that the observed naloxone-induced antinociceptive response is the consequence of the local expression of MORS196A-CSTA at specific sites of pain pathway. Injection of such MOR mutant and the systemic administration of naloxone can be a new strategy in the management of chronic pain without the various side effects associated with the use of morphine. PMID:22407757

Chou, Shu-Husan; Kao, Jen-Hsin; Tao, Pao-Luh; Law, Ping-Yee; Loh, Horace H

2012-08-01

327

The effect of exercise on the peripheral nerve in streptozotocin (STZ)-induced diabetic rats.  

Science.gov (United States)

The exact effectiveness of supportive care activities, such as exercise, in diabetes patients has yet to be elucidated in the diabetic peripheral neuropathy (DPN) field. Therefore, this study was designed to investigate the effect of regular exercise on the peripheral nerves of streptozotocin-induced diabetic rats. The animals were divided as follows into six groups according to exercise combination and glucose control: Normal group, normal group with exercise (EXE), diabetic group (DM), DM group with EXE, DM + glucose control with insulin (INS), and DM + INS + EXE. Animals in the exercise groups were made to walk on a treadmill machine everyday for 30 min at a setting of 8 m/min without inclination. After 8 weeks, sensory parameters were evaluated, and after 16 weeks, biochemicals and peripheral nerves were quantified by immunohistochemistry and compared among experimental groups. The resulting data showed that fasting blood glucose levels and HbA1c levels were not influenced significantly by exercise in normal and DM groups. However, the current perception threshold and the von Frey stimulation test revealed higher thresholds in the DM + INS + EXE group than in the DM + INS group (P nerve fiber density was reduced in a lesser degree in the DM + INS + EXE group than in the DM + INS group (9.8 ± 0.4 vs. 9.1 ± 0.5, P peripheral nerve in the normal or DM groups; however, a beneficial effect from exercise was observed when hyperglycemia was controlled with insulin in the DM group. These findings suggest that exercise has a potential protective effect against DPN based on the preferential effort for glucose control, although exercise alone cannot prevent peripheral nerve damage from hyperglycemia. PMID:25253638

Jin, Heung Yong; Lee, Kyung Ae; Park, Tae Sun

2014-09-25

328

The effect of flankers on three tasks in central, peripheral, and amblyopic vision.  

Science.gov (United States)

Using identical stimuli and methods, we assessed the effects of flankers on three different tasks, orientation discrimination, contrast discrimination, and detection, in central, peripheral, and amblyopic vision. The goal was to understand the factors that limit performance of a task in the presence of flankers in each of these visual systems. The results demonstrate that: (1) For unflanked targets, the losses in peripheral and amblyopic vision (relative to the normal fovea) are ordered, with the loss of unflanked contrast discrimination thresholds considerably smaller than those for either detection or orientation discrimination. (2) For flanked targets, in normal foveal vision and anisometropic amblyopia, the critical distance is more or less proportional to the target size, whereas in peripheral and strabismic amblyopic vision, the critical distance shows much less (or no) dependence on target size. (3) For the normal fovea, and anisometropic amblyopia, when the target is large (>?0.2 deg) the amount of threshold elevation induced by flankers is low, increasing when the target is very small. On the other hand, for the periphery and the amblyopic eyes of most strabismic amblyopes, the elevation is large over the range of sizes tested. (4) In peripheral and strabismic amblyopic vision, remote flankers elevate orientation discrimination and contrast discrimination thresholds but not detection thresholds. Our results show clearly that the effects of flanks depend on both the task and the type of visual system. We conclude that in normal foveal vision and anisometropic amblyopia, the effects of flankers largely reflects a reduction in visibility and may be explained by masking. On the other hand, in peripheral vision and strabismic amblyopia, the effects of flankers on orientation discrimination and to a lesser extent contrast discrimination cannot be explained by simple masking and are due to crowding. PMID:21220540

Levi, Dennis M; Carney, Thom

2011-01-01

329

[Standardised postoperative analgesic system in orthopaedic surgery].  

Science.gov (United States)

In order to treat patients with postoperative acute pain effectively, we have developed a standardised algorithm for analgesia. This process includes three levels and the appropriate supply of medication. The therapy level is defined based on the scale of the operation. Accordingly, the prescription and handling of the pain medication is simplified for the attending physician and nurses. The pain level has to be measured by the nursing staff sing a visual analogue scale (VAS). Thus, the efficiency of the analgesics will be continuously evaluated and controlled. The standardised supply medication can be applied in those cases with pain levels > or = 4 (VAS). It is possible to up- or down-grade the level within the system depending on the actual pain experienced by the patient. With this structured pain therapy algorithm we now have a guideline for the consistent postoperative analgesic treatment of patients. PMID:16821177

Giesa, M; Drees, P; Meurer, A; Jage, J; Eckardt, A

2006-01-01

330

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.)

331

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)

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.

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

332

A Review of the Adverse Effects of Peripheral Alpha-1 Antagonists in Hypertension Therapy  

Directory of Open Access Journals (Sweden)

Full Text Available 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 that may be helpful in evaluating the results of this randomized controlled trial. Methods Using Medline and the Cochrane databases, we performed a comprehensive review of the literature on the use of peripheral alpha-1 antagonists as antihypertensive agents, focusing on available information that could explain the excess cardiovascular events observed in the Antihypertensive and Lipid-Lowering Treatment to prevent Heart Attack Trial (ALLHAT. Results Minimal data were available concerning the effects of peripheral alpha-1 antagonists on CV endpoints. A multitude of short-term studies-ranging from small observational studies to short-term moderate-sized RCTs – focused on safety, efficacy, and tolerability, and some studies investigated the physiologic effects of these agents. These previously reported studies reveal associations with weight gain, fluid retention, and neurohormonal changes among various populations of those treated with peripheral alpha-1 antagonists. Conclusion These findings suggest several possible mechanisms by which doxazosin may be inferior to low-dose diuretics as antihypertensive therapy for the prevention of heart failure.

Bryson Chris L

2002-04-01

333

Topical analgesics in the management of acute and chronic pain.  

Science.gov (United States)

Oral analgesics are commonly prescribed for the treatment of acute and chronic pain, but these agents often produce adverse systemic effects, which sometimes are severe. Topical analgesics offer the potential to provide the same analgesic relief provided by oral analgesics but with minimal adverse systemic effects. This article describes the results of a systematic review of the efficacy of topical analgesics in the management of acute and chronic pain conditions. A literature search of MEDLINE/PubMed was conducted using the keywords topical analgesic AND chronic pain OR acute pain OR neuropathic pain and focused only on individual clinical trials published in English-language journals. The search identified 92 articles, of which 65 were eligible for inclusion in the review. The most commonly studied topical analgesics were nonsteroidal anti-inflammatory drugs (n=27), followed by lidocaine (n=9), capsaicin (n=6), amitriptyline (n=5), glyceryl trinitrate (n=3), opioids (n=2), menthol (n=2), pimecrolimus (n=2), and phenytoin (n=2). The most common indications were acute soft tissue injuries (n=18), followed by neuropathic pain (n=17), experimental pain (n=6), osteoarthritis and other chronic joint-related conditions (n=5), skin or leg ulcers (n=5), and chronic knee pain (n=2). Strong evidence was identified for the use of topical diclofenac and topical ibuprofen in the treatment of acute soft tissue injuries or chronic joint-related conditions, such as osteoarthritis. Evidence also supports the use of topical lidocaine in the treatment of postherpetic neuralgia and diabetic neuropathy. Currently, limited evidence is available to support the use of other topical analgesics in acute and chronic pain. PMID:23374622

Argoff, Charles E

2013-02-01

334

Peripheral and Central Effects of Melatonin on Blood Pressure Regulation  

Directory of Open Access Journals (Sweden)

Full Text Available The pineal hormone, melatonin (N-acetyl-5-methoxytryptamine, shows potent receptor-dependent and -independent actions, which participate in blood pressure regulation. The antihypertensive effect of melatonin was demonstrated in experimental and clinical hypertension. Receptor-dependent effects are mediated predominantly through MT1 and MT2 G-protein coupled receptors. The pleiotropic receptor-independent effects of melatonin with a possible impact on blood pressure involve the reactive oxygen species (ROS scavenging nature, activation and over-expression of several antioxidant enzymes or their protection from oxidative damage and the ability to increase the efficiency of the mitochondrial electron transport chain. Besides the interaction with the vascular system, this indolamine may exert part of its antihypertensive action through its interaction with the central nervous system (CNS. The imbalance between the sympathetic and parasympathetic vegetative system is an important pathophysiological disorder and therapeutic target in hypertension. Melatonin is protective in CNS on several different levels: It reduces free radical burden, improves endothelial dysfunction, reduces inflammation and shifts the balance between the sympathetic and parasympathetic system in favor of the parasympathetic system. The increased level of serum melatonin observed in some types of hypertension may be a counter-regulatory adaptive mechanism against the sympathetic overstimulation. Since melatonin acts favorably on different levels of hypertension, including organ protection and with minimal side effects, it could become regularly involved in the struggle against this widespread cardiovascular pathology.

Olga Pechanova

2014-10-01

335

Peripheral and central effects of melatonin on blood pressure regulation.  

Science.gov (United States)

The pineal hormone, melatonin (N-acetyl-5-methoxytryptamine), shows potent receptor-dependent and -independent actions, which participate in blood pressure regulation. The antihypertensive effect of melatonin was demonstrated in experimental and clinical hypertension. Receptor-dependent effects are mediated predominantly through MT1 and MT2 G-protein coupled receptors. The pleiotropic receptor-independent effects of melatonin with a possible impact on blood pressure involve the reactive oxygen species (ROS) scavenging nature, activation and over-expression of several antioxidant enzymes or their protection from oxidative damage and the ability to increase the efficiency of the mitochondrial electron transport chain. Besides the interaction with the vascular system, this indolamine may exert part of its antihypertensive action through its interaction with the central nervous system (CNS). The imbalance between the sympathetic and parasympathetic vegetative system is an important pathophysiological disorder and therapeutic target in hypertension. Melatonin is protective in CNS on several different levels: It reduces free radical burden, improves endothelial dysfunction, reduces inflammation and shifts the balance between the sympathetic and parasympathetic system in favor of the parasympathetic system. The increased level of serum melatonin observed in some types of hypertension may be a counter-regulatory adaptive mechanism against the sympathetic overstimulation. Since melatonin acts favorably on different levels of hypertension, including organ protection and with minimal side effects, it could become regularly involved in the struggle against this widespread cardiovascular pathology. PMID:25299692

Pechanova, Olga; Paulis, Ludovit; Simko, Fedor

2014-01-01

336

Acetyl-L-carnitine: from a biological curiosity to a drug for the peripheral nervous system and beyond.  

Science.gov (United States)

Acetyl-L-carnitine (ALC) is a molecule derived from acetylation of carnitine in the mitochondria. Carnitine acetylation enables the function of CoA and facilitates elimination of oxidative products. Beyond this metabolic activity, ALC provides acetyl groups for acetylcholine synthesis, exerts a cholinergic effect and optimizes the balance of energy processes. Acetylcarnitine supplementation induces neuroprotective, neurotrophic and analgesic effects in the peripheral nervous system. In the recent studies, ALC, by acting as a donor of acetyl groups to NF-kb p65/RelA, enhanced the transcription of the GRM2 gene encoding the mGLU2 receptors, inducing long-term upregulation of the mGluR2, evidencing therefore that its long-term analgesic effects are dependent on epigenetic modifications. Several studies, including double-blind, placebo-controlled, parallel group studies and few open studies showed the effect of ALC in diseases characterized by neuropathies and neuropathic pain: the studies included diabetic neuropathy, HIV and antiretroviral therapy-induced neuropathies, neuropathies due to compression and chemotherapeutic agents. Double-blinded studies involved 1773 patients. Statistical evaluations evidenced reduction of pain, improvements of nerve function and trophism. In conclusion, ALC represents a consistent therapeutic option for peripheral neuropathies, and its complex effects, neurotrophic and analgesic, based on epigenetic mechanism, open new pathways in the study of peripheral nerve disease management. PMID:23965166

Onofrj, Marco; Ciccocioppo, Fausta; Varanese, Sara; di Muzio, Antonio; Calvani, Menotti; Chiechio, Santina; Osio, Maurizio; Thomas, Astrid

2013-08-01

337

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

OpenAIRE

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 ...

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

1984-01-01

338

Peripheral and central adrenoceptor modulation of the behavioural effects of clozapine in the paw test.  

OpenAIRE

1. In rats, the atypical neuroleptic, clozapine, has been found to increase the hindlimb retraction time but not the forelimb retraction time, in the paw test. These parameters have predictive validity for the antipsychotic efficacy and extrapyramidal side-effects of drugs, respectively. The present study analysed to what extent drugs acting on adrenoceptors affect the behavioural effect of clozapine in the paw test. 2. The alpha 1-adrenoceptor agonist, ST 587 but not the peripherally working...

Prinssen, E. P.; Ellenbroek, B. A.; Cools, A. R.

1994-01-01

339

The analgesic effect of electroacupuncture on inflammatory pain in the rat model of collagenase-induced arthritis: mediation by opioidergic receptors.  

Science.gov (United States)

Electroacupuncture (EA) is widely practiced for the treatment of osteoarthritic (OA) pain, but its therapeutic mechanisms have not yet been fully studied, especially in the experimental OA rat model. In order to induce collagenase-induced arthritis (CIA) in rats, male Sprague-Dawley rats were intra-articularly injected with 0.05 ml of 4 mg/ml collagenase solution in the left knee of the hind limb, followed by a booster injection 4 days later. Maximal gross, histopathological features and biomarker activity changes consistent with human OA characteristics were observed four weeks after the first collagenase injection. In the exploratory preliminary study of EA stimulation parameters, low-frequency train pulse EA stimulation (2 Hz, 0.07 mA, 0.3 ms) delivered to the Zusanli (ST36) acupoint exerted an antinociceptive effect with acupoint specificity in a rat model of CIA. The antinociceptive effect of Zusanli EA was blocked by intraperitoneal pretreatment with naloxone (?-opioid receptor antagonist, 2 mg/kg) and naltrindole (?-opioid receptor antagonist, 1 mg/kg), but not with norbinaltophimine (?-opioid receptor antagonist, 20 mg/kg). The synergistic antinociceptive effects of Zusanli EA were achieved with statistical significance by i.p. pretreatment with DAMGO (?-opioid receptor agonist, 1 mg/kg) and with [D-Ala2]-Deltorphin II (?-opioid receptor agonist, 6 mg/kg), but not with (±)-U-50488 (?-opioid receptor agonist, 3 mg/kg). These results suggest that the 2-Hz EA can attenuate the osteoarthritic pain in CIA, and the analgesic effects of EA can be mediated by ?-opioid and ?-opioid, but not by ?-opioid receptors. PMID:22961089

Seo, Byung Kwan; Park, Dong Suk; Baek, Yong Hyeon

2013-05-01

340

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)

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.

André Peres e Serra

2010-06-01

341

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

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: Portuguese Abstract in portuguese 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 u [...] tilizados 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. Abstract in spanish 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 periféri [...] cos. 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. Abstract in english 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 pai [...] n 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.

André Peres e, Serra; Hazem A, Ashmawi.

2010-06-01

342

Comparison of postoperative analgesic effect of intrathecal clonidine and fentanyl added to bupivacaine in patients undergoing cesarean section: a prospective randomized double-blind study.  

Science.gov (United States)

Objectives. To compare the analgesic efficacy of intrathecal clonidine and fentanyl added to bupivacaine after cesarean section. Methods. Ninety patients scheduled for cesarean section under spinal anesthesia were randomly allocated to one of the three following groups to receive bupivacaine 10?mg combined with 75?µg clonidine (group C), bupivacaine 10?mg combined with 0.5?mL fentanyl (group F), and bupivacaine 10?mg combined with 0.5?mL distilled water (group P), intrathecally. The time to first analgesic request, analgesic requirement in the first 24 hours after surgery, sensory and motor blockade onset time, duration of sensory and motor blockade, the incidence of hypotension, ephedrine requirements, bradycardia, and hypoxemia were recorded. Results. The duration of anesthesia in clonidine group (275.10 ± 96.09) was longer compared to the placebo (211.73 ± 74.80) and fentanyl (192.33 ± 30.36) groups. This difference between group C versus F (P = 0.006) and P groups (P < 0.001) was significant. Similarly, the mean time to first analgesic request was also longer in group C (519.44 ± 86.25) than in groups F (277.88 ± 94.25) and P (235.43 ± 22.35?min). This difference between group C versus F (P < 0.001) and P groups (P < 0.001) was significant. Conclusion. Intrathecal clonidine 75?µg with bupivacaine prolonged the time to first analgesic request compared to fentanyl; however, the total analgesic consumption within the first 24?h postoperative was similar in fentanyl and clonidine groups following cesarean section. This trial is registered with ACTRN12611000909921 and ClinicalTrials.gov NCT01425658. PMID:24649361

Khezri, Marzieh Beigom; Rezaei, Meisam; Delkhosh Reihany, Morteza; Haji Seid Javadi, Ezzatalsadat

2014-01-01

343

Three newly approved analgesics: an update.  

Science.gov (United States)

Abstract Since 2008, three new analgesic entities, tapentadol immediate release (Nucynta) diclofenac potassium soft gelatin capsules (Zipsor), and bupivacaine liposome injectable suspension (EXPAREL) were granted US Food and Drug Administration (FDA) approval to treat acute pain. Tapentadol immediate-release is a both a mu-opioid agonist and a norepinephrine reuptake inhibitor, and is indicated for the treatment of moderate to severe pain. Diclofenac potassium soft gelatin capsules are a novel formulation of diclofenac potassium, which is a nonsteroidal anti-inflammatory drug (NSAID), and its putative mechanism of action is through inhibition of cyclooxygenase enzymes. This novel formulation of diclofenac allows for improved absorption at lower doses. Liposomal bupivacaine is a new formulation of bupivacaine intended for single-dose infiltration at the surgical site for postoperative analgesia. Bupivacaine is slowly released from this liposomal vehicle and can provide prolonged analgesia at the surgical site. By utilizing NSAIDs and local anesthetics to decrease the transmission of afferent pain signals, less opioid analgesics are needed to achieve analgesia. Since drug-related adverse events are frequently dose related, lower doses from different drug classes may be employed to reduce the incidence of adverse effects, while producing synergistic analgesia as part of a multimodal analgesic approach to acute pain. PMID:24423420

Saraghi, Mana; Hersh, Elliot V

2013-01-01

344

Pattern of use of analgesics in a surgical unit  

Directory of Open Access Journals (Sweden)

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.

Mohammad Abdullah Al Masud

2009-06-01

345

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

346

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)

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.

Toroudi Hamidreza

2009-01-01

347

Relative Biological Effectiveness and Peripheral Damage of Antiproton Annihilation  

CERN Multimedia

The use of ions to deliver radiation to a body for therapeutic purposes has the potential to be significant improvement over the use of low linear energy transfer (LET) radiation because of the improved energy deposition profile and the enhanced biological effects of ions relative to photons. Proton therapy centers exist and are being used to treat patients. In addition, the initial use of heavy ions such as carbon is promising to the point that new treatment facilities are planned. Just as with protons or heavy ions, antiprotons can be used to deliver radiation to the body in a controlled way; however antiprotons will exhibit additional energy deposition due to annihilation of the antiprotons within the body. The slowing down of antiprotons in matter is similar to that of protons except at the very end of the range beyond the Bragg peak. Gray and Kalogeropoulos estimated the additional energy deposited by heavy nuclear fragments within a few millimeters of the annihilation vertex to be approximately 30 MeV (...

Kavanagh, J N; Kaiser, F; Tegami, S; Schettino, G; Sellner, S; Moller, S; Kovacevic, S; Welsch, C; Hajdukovic, D; Currell, F J; Toelli, H T; Doser, M; Holzscheiter, M; Herrmann, R; Timson, D J; Alsner, J; Landua, R; Knudsen, H; Comor, J; Beyer, G

2002-01-01

348

Selective peripheral fading: evidence for inhibitory sensory effect of attention.  

Science.gov (United States)

A circular array of six discs, three green and three orange in alternate positions, was presented against a uniform grey background. Sixteen observers maintained steady fixation at the centre of the array, and were instructed to direct their attention to three discs of one colour and to ignore the three discs of the other colour. In about 10 s (mean = 11.35 s), some discs started to fade away from awareness. Of those starting to fade, most (mean = 81.3%) were those selected for attention. The faded discs remained out of awareness for up to a few seconds (mean = 1.55 s) during which other discs were clearly visible. The fading increased with eccentricity, a defining characteristic of Troxler fading. However, the selectivity of the fading strongly suggests that voluntary attention can have an inhibitory effect on early sensory processing. Were the fading entirely due to local sensory adaptation, the unattended stimuli would have to be equally adapted and yet somehow remain visible for seconds, which is not plausible. PMID:10664791

Lou, L

1999-01-01

349

Effect of mianserin hydrochloride on peripheral uptake mechanisms for noradrenaline and 5-hydroxytryptamine in man  

Science.gov (United States)

1 Mianserin seems to have little effect on peripheral noradrenaline (NA) re-uptake mechanisms as shown by its lack of effects on the tyramine dose and NA dose/pressor response. 2 Mianserin has no effect on the hypotensive action of bethanidine. 3 Mianserin in vivo has a significant action on platlet transport (Vmax) of 5-hydroxytryptamine (5-HT), which changes toward normal values in depressive patients on the drug. This action is not observed in vitro. 4 It is possible that a metabolite of mianserin is responsible for this effect, and that this may be of therapeutic importance. PMID:341939

Coppen, A.; Ghose, Karabi; Swade, Cynthia; Wood, K.

1978-01-01

350

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

OpenAIRE

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...

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

2010-01-01

351

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

OpenAIRE

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...

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

2013-01-01

352

Protective Effect of Melatonin Against Mitomycin C-Induced Genotoxic Damage in Peripheral Blood of Rats  

OpenAIRE

Mitomycin C (MMC) generates free radicals when metabolized. We investigated the effect of melatonin against MMC-induced genotoxicity in polychromatic erythrocytes and MMC-induced lipid peroxidation in brain and liver homogenates. Rats (N = 36) were classified into 4 groups: control, melatonin, MMC, and MMC + melatonin. Melatonin and MMC doses of 10?mg/kg and 2?mg/kg, respectively, were injected intraperitoneally. Peripheral blood samples were collected at 0, 24, 48, 72, and 96 h...

Ortega-guti Amp Rrez, S.; Amp Pez-vicente, M. L.; Lostal Amp, F.; Fuentes-broto, L.; E. Martínez-Ballarín; J. J. García

2009-01-01

353

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)

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."

Khomiak O.V.

2012-01-01

354

Acetaminophen: a central analgesic drug that involves a spinal tropisetron-sensitive, non-5-HT(3) receptor-mediated effect.  

Science.gov (United States)

The reversal of the antinociceptive effect of systemically administered acetaminophen (paracetamol) by intrathecal administration of the potent 5-HT(3) receptor antagonist tropisetron has been reported in rats subjected to the paw pressure test, suggesting that acetaminophen action is mediated through spinal 5-HT(3) receptors. However, more recent data, showing differences between the pharmacological profiles of various 5-HT(3) receptor antagonists, led us to reconsider the involvement of spinal 5-HT(3) receptors. To address this question, two different approaches were used: 1) electrophysiological recordings to assess whether acetaminophen directly modulates 5-HT(3) receptor activity and 2) pharmacological investigations with various 5-HT(3) receptor antagonists and spinal 5-HT(3) receptors antisense oligodeoxynucleotides (AODNs) to determine how those treatments might affect the antinociceptive action of acetaminophen. Electrophysiological studies demonstrated that acetaminophen had no direct agonist or antagonist effects on 5-HT(3A) receptors. Unlike tropisetron, other 5-HT(3) receptor antagonists, such as ondansetron and granisetron, injected intrathecally were unable to reverse the antinociceptive effect of acetaminophen. Moreover, pretreatment with AODNs did not reverse the acetaminophen-induced antinociceptive effect, although it suppressed the antinociceptive effect of m-chlorophenylbiguanide, a specific agonist of 5-HT(3) receptors, and significantly reduced (30%) the expression of these receptors in the dorsal horn of the spinal cord. These results suggest that acetaminophen-induced antinociceptive action involves a spinal tropisetron-sensitive receptor that is not the 5-HT(3) receptor and that remains to be identified. PMID:15322266

Libert, F; Bonnefont, J; Bourinet, E; Doucet, E; Alloui, A; Hamon, M; Nargeot, J; Eschalier, A

2004-09-01

355

[Effect of narcotic analgesics on the cortical control process of impulse transmission in the afferent pathways of the sciatic nerve].  

Science.gov (United States)

The effect produced by narcotic analgetics with their intravenous administration on the process of cortical control over the transmission of impulses along specific routes of the sciatic nerve was studied. The conditioning stimulation of the cortex was effected by using a monopolar electrode through single electric impulses. The interval between conditioning and test (on sciatic nerve) impulses was of 80-120 ms. Morphine (1-2 mg/kg), promedol (trimeperidin) (1-2 mg/kg) and phentanyl (100 gamma/kg) potentiated the inhibition of evoked potentials in the nucleus gracilis and in VPL, observed upon stimulation of the cortex of optic lobuses. The intensification of inhibitory corticifugal mechanisms occurring under the effect of narcotic analgetics takes place both on the level of the medulla oblongata and of the thalamic one. PMID:6310

Churiukanov, V V; Bilibin, D P

1976-01-01

356

The thalidomide analgesic effect is associated with differential TNF-? receptor expression in the dorsal horn of the spinal cord as studied in a rat model of neuropathic pain.  

Science.gov (United States)

The proinflammatory cytokine tumor necrosis factor-? (TNF-?) is well recognized as a key player in nociceptive signaling. Yet, therapeutic capitalization of this knowledge requires a better understanding of how TNF receptors (TNFR) contribute to pain. To address this question, we studied TNFR expression in the chronic sciatic nerve constriction (CCI) model of neuropathic pain. CCI and sham operated rats received two subcutaneous injections (one immediately after surgery, the other on postoperative day 5) containing either saline, GABA-reuptake inhibitor (NO-711), insulin-like growth factor-1 (IGF-1), ZVAD or thalidomide. Mechanical (using von Frey filaments) and thermal hypersensitivity (Hargreaves test) were assessed preoperatively and weekly during the first four postoperative weeks. Spinal cord dorsal horn samples were collected from animals that were sacrificed at 2 weeks and 4 weeks after surgery, and analyzed for TNFR1 and TNFR2 mRNA levels by qPCR and protein levels by Western blot. Compared to saline, all applied drug treatments resulted in a faster recovery from mechanical and thermal hypersensitivity, yet in a potency order of thalidomide>ZVAD=IGF-1>NO-711. CCI resulted in increased TNFR1 and TNFR2 mRNA and protein levels in the ipsilateral dorsal horn. Thalidomide was the only treatment that attenuated these increases. Finally, animals that showed a poor behavioral recovery were characterized by a significantly higher TNFR1/TNFR2 mRNA ratio. These data show that differential expression of TNFR in the dorsal horn is associated with recovery from pain in this model and suggest that the analgesic effects of thalidomide may act via this mechanism. PMID:22425187

Andrade, Pablo; Visser-Vandewalle, Veerle; Del Rosario, John S; Daemen, Marc A; Buurman, Wim A; Steinbusch, Harry W; Hoogland, Govert

2012-04-23

357

The impact of stress on tumor growth: peripheral CRF mediates tumor-promoting effects of stress  

Directory of Open Access Journals (Sweden)

Full Text Available 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 peripheral CRF on tumor growth as a mediator of the response to stress in vivo. Methods For this purpose we used the 4T1 breast cancer cell line in cell culture and in vivo. Cells were treated with CRF in culture and gene specific arrays were performed to identify genes directly affected by CRF and involved in breast cancer cell growth. To assess the impact of peripheral CRF as a stress mediator in tumor growth, Balb/c mice were orthotopically injected with 4T1 cells in the mammary fat pad to induce breast tumors. Mice were subjected to repetitive immobilization stress as a model of chronic stress. To inhibit the action of CRF, the CRF antagonist antalarmin was injected intraperitoneally. Breast tissue samples were histologically analyzed and assessed for neoangiogenesis. Results Array analysis revealed among other genes that CRF induced the expression of SMAD2 and ?-catenin, genes involved in breast cancer cell proliferation and cytoskeletal changes associated with metastasis. Cell transfection and luciferase assays confirmed the role of CRF in WNT- ?-catenin signaling. CRF induced 4T1 cell proliferation and augmented the TGF-? action on proliferation confirming its impact on TGF?/SMAD2 signaling. In addition, CRF promoted actin reorganization and cell migration, suggesting a direct tumor-promoting action. Chronic stress augmented tumor growth in 4T1 breast tumor bearing mice and peripheral administration of the CRF antagonist antalarmin suppressed this effect. Moreover, antalarmin suppressed neoangiogenesis in 4T1 tumors in vivo. Conclusion This is the first report demonstrating that peripheral CRF, at least in part, mediates the tumor-promoting effects of stress and implicates CRF in SMAD2 and ?-catenin expression.

Stathopoulos Efstathios N

2010-09-01

358

Clinical and pathological aspects of analgesic nephropathy  

OpenAIRE

1 Analgesic nephropathy is part of the analgesic syndrome which has gastrointestinal, haematological, cardiovascular, psychological and psychiatric, and pregnancy and gonadal manifestations; premature ageing may also be a feature.

Nanra, R. S.

1980-01-01

359

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)

Full Text Available SciELO Argentina | Language: English Abstract in portuguese 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 ex

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

2011-12-01

360

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

Directory of Open Access Journals (Sweden)

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.

Deepraj Paul

2013-06-01

361

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

OpenAIRE

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...

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

2011-01-01

362

Sex differences in the analgesic effects of ICI 182,780 and Flutamide on ureteral calculosis in rats.  

Science.gov (United States)

To better define the involvement of gonadal hormones in the sex differences observed in experimental visceral pain, we administered antagonists of estrogen receptors (ICI 182,780 [ICI]) or androgen receptors (Flutamide [FLU]) to adult male and female rats suffering from artificial ureteral calculosis. Subjects were divided into groups and treated with one of the substances (ICI, FLU) or sweet almond oil (OIL, vehicle) for 5 days, starting 2 days before surgery. On day 3, animals underwent surgery, with half receiving an artificial calculosis (Stone) and half only a sham procedure. The animals' behavior (number and duration of ureteral crises) and blood hormone levels (estradiol and testosterone) were determined in all groups. In OIL-treated rats the number and duration of crises were higher in females than in males. The administration of ICI or FLU resulted in hormonal effects in males and behavioral effects in females. In males ICI treatment increased estradiol plasma levels and FLU increased testosterone plasma levels; in females ICI and FLU treatments both decreased the number and duration of the ureteral crises. These results, confirming previous findings of higher sensitivity of females than males to urinary tract pain, showed the modulatory effects of estrogen and androgen antagonists on the behavioral responses induced by pain but only in females. PMID:20920504

Affaitati, Giannapia; Ceccarelli, Ilaria; Fiorenzani, Paolo; Rossi, Cosmo; Pace, Maria Caterina; Passavanti, Maria Beatrice; Aurilio, Caterina; Sorda, Giuseppina; Danielli, Barbara; Giamberardino, Maria Adele; Aloisi, Anna Maria

2011-01-01

363

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

Directory of Open Access Journals (Sweden)

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.

Mohsenpour M

2012-09-01

364

A comparative study of analgesic property of whole plant and fruit extracts of Fragaria vesca in experimental animal models  

Directory of Open Access Journals (Sweden)

Full Text Available The aim of the study was to compare the analgesic activities of ethanolic extract of fruits and whole plant of Fragaria vesca in experimental animal models. The extracts were prepared by percolation method and oral toxicity testing was performed as per OECD guidelines. Analgesic activity was assessed by tail flickmethod (for central action and acetic acid-induced writhing test (for peripheral action. Fruit extract, whole plant extract and aspirin showed significant analgesic activity, both central and peripheral, as compared to control (p< 0.01. Although fruit extract at dose of 500 mg/kg showed better activity than 250 mg/kg (p<0.05. Analgesic activities of fruit extract 250 mg/kg and whole plantextract 500 mg/kg were almost equivalent while aspirin was most potent among all with significantly greater activities as compared to all the extracts (p<0.05.

Lalit Kanodia

2009-06-01

365

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)

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.

Fábio José, Reis; Noeli Pereira, Rocha.

2006-12-01

366

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

Science.gov (United States)

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

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

2005-11-26

367

Functional plasticity of the N/OFQ-NOP receptor system determines analgesic properties of NOP receptor agonists.  

Science.gov (United States)

Despite high sequence similarity between NOP (nociceptin/orphanin FQ opioid peptide) and opioid receptors, marked differences in endogenous ligand selectivity, signal transduction, phosphorylation, desensitization, internalization and trafficking have been identified; underscoring the evolutionary difference between NOP and opioid receptors. Activation of NOP receptors affects nociceptive transmission in a site-specific manner, with antinociceptive effects prevailing after peripheral and spinal activation, and pronociceptive effects after supraspinal activation in rodents. The net effect of systemically administered NOP receptor agonists on nociception is proposed to depend on the relative contribution of peripheral, spinal and supraspinal activation, and this may depend on experimental conditions. Functional expression and regulation of NOP receptors at peripheral and central sites of the nociceptive pathway exhibits a high degree of plasticity under conditions of neuropathic and inflammatory pain. In rodents, systemically administered NOP receptor agonists exerted antihypersensitive effects in models of neuropathic and inflammatory pain. However, they were largely ineffective in acute pain while concomitantly evoking severe motor side effects. In contrast, systemic administration of NOP receptor agonists to non-human primates (NHPs) exerted potent and efficacious antinociception in the absence of motor and sedative side effects. The reason for this species difference with respect to antinociceptive efficacy and tolerability is not clear. Moreover, co-activation of NOP and ?-opioid peptide (MOP) receptors synergistically produced antinociception in NHPs. Hence, both selective NOP receptor as well as NOP/MOP receptor agonists may hold potential for clinical use as analgesics effective in conditions of acute and chronic pain. PMID:24762001

Schröder, W; Lambert, D G; Ko, M C; Koch, T

2014-08-01

368

Anti-Inflammatory and Analgesic Activities of Ethanol Extract of Aerial Parts of Justicia gendarussa Burm.  

OpenAIRE

The aim of the present study was to evaluate the anti-inflammatory and analgesic activities of the ethanol extract of aerial parts of Justicia gendarussa (EJG) in animal models. The anti-inflammatory activity of the extract was evaluated by using carrageenan-induced rat paw edema and cotton pellet granuloma method. The analgesic activity of the extract was evaluated for its central and peripheral pharmacological actions by using Eddy’s hot plate method and acetic acid-induced writhin...

Jothimanivannan, C.; Subramanian, N.; Kumar, R. S.

2010-01-01

369

Comparative clinical study of light analgesic effect on temporomandibular disorder (TMD) using red and infrared led therapy.  

Science.gov (United States)

Low-level laser therapy (LLLT) has been widely applied in pain relief in several clinical situations, including temporomandibular disorders (TMD). However, the effects of LED therapy on TMD has not been investigated. This study aims to evaluate the effects of red and infrared LEDs on: (1) tissue temperature in ex vivo and (2) pain relief and mandibular range of motion in patients with TMD. Thirty patients between 18 and 40 years old were included and randomly assigned to three groups. The two experimental groups were: the red LED (630?±?10 nm) group and the infrared LED (850?±?10 nm) group. The irradiation parameters were 150 mW, 300 mW/cm(2), 18 J/cm(2), and 9 J/point. The positive control group received an infrared laser (780 nm) with 70 mW, 1.7 W/cm(2), 105 J/cm(2), and 4.2 J/point. LED and laser therapies were applied bilaterally to the face for 60 s/point. Five points were irradiated: three points around the temporomandibular joint (TMJ), one point for the temporalis, and one near the masseter. Eight sessions of phototherapy were performed, twice a week for 4 weeks. Pain induced by palpating the masseter muscle and mandibular range of motion (maximum oral aperture) were measured at baseline, immediately after treatment, 7 days after treatment, and 30 days after treatment. There was an increase in tissue temperature during both the red and the infrared LED irradiation in ex vivo. There was a significant reduction of pain and increase of the maximum oral aperture for all groups (p???0.05). There was no significant difference in pain scores and maximum oral aperture between groups at baseline or any periods after treatment (p???0.05). The current study showed that red and infrared LED therapy can be useful in improving outcomes related to pain relief and orofacial function for TMD patients. We conclude that LED devices constitute an attractive alternative for LLLT. PMID:24197518

Panhoca, Vitor Hugo; de Fatima Zanirato Lizarelli, Rosane; Nunez, Silvia Cristina; Pizzo, Renata Campi de Andrade; Grecco, Clovis; Paolillo, Fernanda Rossi; Bagnato, Vanderlei Salvador

2015-02-01

370

[Effect of dicarbamin on postradiation leukocyte composition dynamics in peripheral blood of mice].  

Science.gov (United States)

Effects of dicarbamin on the post-irradiation dynamics of leukocyte composition in the peripheral blood of mice have been studied upon oral administration of the drug in a single dose of 0.5, 5.0, 15.0, and 50.0 mg/kg. It is established that the drug doses of 5.0, 15.0, and 50.0 mg/kg produce statistically significant radioprotective effects. The leukocyte fall decreases due to segmented neutrophils and lymphocytes. In addition, the drug accelerates the process of restoration of the leukocyte cell numbers on the initial level. PMID:20184283

Moiseeva, I Ia; Zinov'ev, A I; Mozerova, I V; Filimonov, S A

2010-01-01

371

An evaluation of the analgesic effects of meloxicam in addition to epidural morphine/mepivacaine in dogs undergoing cranial cruciate ligament repair  

OpenAIRE

The analgesic efficacy of an epidural morphine/mepivacaine combination alone versus epidural morphine/mepivacaine in combination with meloxicam administered prior to the onset of anesthesia was assessed in 20 dogs undergoing cranial cruciate ligament repair. Numerical and visual analog pain scores were performed prior to anesthesia and at 6, 8, 12, 16, and 24 hours after epidural administration by a trained observer, blinded to treatment. An analgesiometer was used to determine the amount of ...

Fowler, David; Isakow, Kevin; Caulkett, Nigel; Waldner, Cheryl

2003-01-01

372

Analgésicos tópicos Analgésicos tópicos Topical analgesics  

Directory of Open Access Journals (Sweden)

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 ? 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.

Murilo Pereira Flores

2012-04-01

373

Analgésicos tópicos / Topical analgesics / Analgésicos tópicos  

Scientific Electronic Library Online (English)

Full Text Available SciELO Brazil | Language: Portuguese 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, but studies are nee

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

2012-04-01

374

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

OpenAIRE

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...

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

2015-01-01

375

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

Directory of Open Access Journals (Sweden)

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.

Christiana Winkler

2005-01-01

376

Clinical Evaluation of Analgesic Activity of Guduchi (Tinospora Cordifolia) Using Animal Model  

OpenAIRE

Introduction: Pain is a very well-known signal of ill health and analgesics are the drugs that are used to relieve pain. The main problem with these drugs remains that of side effects. Safer alternatives are natural herbs. Guduchi (Tinospora cordifolia) is one such plant with analgesic potential but few studies are there.

Goel, Bhomik; Pathak, Nishant; Nim, Dwividendra Kumar; Singh, Sanjay Kumar; Dixit, Rakesh Kumar; Chaurasia, Rakesh

2014-01-01

377

A simple effective interaction for peripheral heavy-ion collisions at intermediate energies  

International Nuclear Information System (INIS)

A very simple phenomenological nucleon-nucleon effective interaction is derived by folding-model analyses of 36 sets of heavy-ion elastic-scattering data at energies E/A between 10 and 100 MeV. It is represented by a single Yukawa term with a complex strength that varies slowly with energy. It is appropriate for peripheral collisions at intermediate energies. It is proposed for use in consistent analyses of elastic- and inelastic-scattering measurements. The possible role of spin-orbit coupling in heavy-ion elastic scattering at the higher energies is discussed. ((orig.))

378

Glutamate and capsaicin effects on trigeminal nociception I: Activation and peripheral sensitization of deep craniofacial nociceptive afferents  

OpenAIRE

We have examined the effect of the peripheral application of glutamate and capsaicin to deep craniofacial tissues in influencing the activation and peripheral sensitization of deep craniofacial nociceptive afferents. The activity of single trigeminal nociceptive afferents with receptive fields in deep craniofacial tissues were recorded extracellularly in 55 halothane-anesthetized rats. The mechanical activation threshold (MAT) of each afferent was assessed before and after injection of 0.5M g...

Lam, David K.; Sessle, Barry J.; Hu, James W.

2009-01-01

379

The effect of the acute combined action of radiation and some pesticides on the peripheral blood of rats  

International Nuclear Information System (INIS)

The effects of the combined action of external gamma radiation and certain pesticides on peripheral blood were studied in rats. The pesticides introduced into the stomach were the organophosphoric compound Dipterex, the organochlorine compound Lindane or tetramethyl-thiuram disulphide. In the peripheral blood, the quantity of haemoglobin, red blood corpuscles and white blood corpuscles, and the leucocyte formula were defined and qualitative changes in the white blood cells revealed according to the frequency with which atypical cells were encountered. (UK)

380

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

OpenAIRE

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...

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

1994-01-01