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Sample records for peripheral analgesic effect

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

    A. B de Oliveira

    1991-01-01

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

  2. Peripheral analgesic effects of ketamine in acute inflammatory pain

    Pedersen, J L; Galle, T S; Kehlet, H

    1998-01-01

    BACKGROUND. This study examined the analgesic effect of local ketamine infiltration, compared with placebo and systemic ketamine, in a human model of inflammatory pain. METHODS: Inflammatory pain was induced by a burn (at 47 degrees C for 7 min; wound size, 2.5 x 5 cm) on the calf in 15 volunteer...

  3. Involvement of peripheral TRPV1 channels in the analgesic effects of thalidomide.

    Song, Tieying; Wang, Liwen; Gu, Kunfeng; Yang, Yunliang; Yang, Lijun; Ma, Pengyu; Ma, Xiaojing; Zhao, Jianhui; Yan, Ruyv; Guan, Jiao; Wang, Chunping; Qi, Yan; Ya, Jian

    2015-01-01

    Thalidomide was introduced to the market in 1957 as a sedative and antiemetic agent, and returned to the market for the treatment of myelodysplastic syndrome and multiple myeloma. There are reports and studies of thalidomide as an analgesic or analgesic adjuvant in clinic. However, the underlying mechanism is quite elusive. Many studies suggest that the analgesic effect of thalidomide may be due to its immunomodulatory and anti-inflammatory properties as it suppresses the production of tumor necrosis factor α (TNF-α) selectively. However, it is not clear whether any other mechanisms are implicated in the pain relief. In this study, we demonstrated that the peripheral vanilloid receptor 1 (TRPV1) channel was also involved in the analgesic effect of thalidomide in different cell and animal models. During the activation by its agonist capsaicin, the cation inward influx through TRPV1 channels and the whole-cell current significantly decreased after TRPV1-overexpressed HEK293 cells or dorsal root ganglion (DRG) neurons were pre-treated with thalidomide for 20 minutes. And such attenuation in the TRPV1 activity was in a dose-dependent manner of thalidomide. In an acetic acid writhing test, pre-treatment of thalidomide decreased the writhing number in the wild type mice, while it did not happen in TRPV1 knockout mice, suggesting that the TRPV1 channel was involved in the pain relief by thalidomide. Taken together, the study showed that TRPV1 channels were involved in the analgesic effects of thalidomide. Such alteration in the action of TRPV1 channels by thalidomide may help understand how thalidomide takes analgesic effect in the body in addition to its selective inhibition of TNF-α production.

  4. Topical and peripheral ketamine as an analgesic.

    Sawynok, Jana

    2014-07-01

    Ketamine, in subanesthetic doses, produces systemic analgesia in chronic pain settings, an action largely attributed to block of N-methyl-D-aspartate receptors in the spinal cord and inhibition of central sensitization processes. N-methyl-D-aspartate receptors also are located peripherally on sensory afferent nerve endings, and this provided the initial impetus for exploring peripheral applications of ketamine. Ketamine also produces several other pharmacological actions (block of ion channels and receptors, modulation of transporters, anti-inflammatory effects), and while these may require higher concentrations, after topical (e.g., as gels, creams) and peripheral application (e.g., localized injections), local tissue concentrations are higher than those after systemic administration and can engage lower affinity mechanisms. Peripheral administration of ketamine by localized injection produced some alterations in sensory thresholds in experimental trials in volunteers and in complex regional pain syndrome subjects in experimental settings, but many variables were unaltered. There are several case reports of analgesia after topical application of ketamine given alone in neuropathic pain, but controlled trials have not confirmed such effects. A combination of topical ketamine with several other agents produced pain relief in case, and case series, reports with response rates of 40% to 75% in retrospective analyses. In controlled trials of neuropathic pain with topical ketamine combinations, there were improvements in some outcomes, but optimal dosing and drug combinations were not clear. Given orally (as a gargle, throat swab, localized peritonsillar injections), ketamine produced significant oral/throat analgesia in controlled trials in postoperative settings. Topical analgesics are likely more effective in particular conditions (patient factors, disease factors), and future trials of topical ketamine should include a consideration of factors that could predispose

  5. Analgesic effects of melatonin

    Wilhelmsen, Michael; Amirian, Ilda; Reiter, Russel J

    2011-01-01

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

  6. Analgesic effects of melatonin

    Wilhelmsen, Michael; Amirian, Ilda; Reiter, Russel J

    2011-01-01

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

  7. Analgesic effects of calcitonin.

    Lyritis, G P; Trovas, G

    2002-05-01

    The analgesic activity of salmon calcitonin (subcutaneous or intranasal) has been demonstrated in several prospective clinical trials, in patients suffering different painful skeletal conditions, including recent nontraumatic osteoporotic vertebral fractures. The mechanism of the analgesic effect of calcitonin is not clear. It is possible that specific binding sites for salmon calcitonin exist in the brain. Another explanation is that changes in descending serotonergic modification on the sensory transmission mediated by C afferents contribute to the analgesic effects of calcitonin on pain in osteoporotic patients. From the clinical point of use, the analgesic effect of calcitonin is beneficial throughout the whole period of medical treatment of osteoporotic patients. Salmon calcitonin in a daily dose of 100 IU subcutaneously or 200 IU intranasally reduces dramatically the back pain (p salmon calcitonin effectively controls severe pain in osteoporotic patients with a recent vertebral fracture, allowing them earlier mobility in combination with a reduction of the urinary hydroxyproline excretion, and a limitation of the considerable bone loss that may occur during prolonged bed rest, make this therapeutic scheme attractive.

  8. Baclofen as an analgesic in chronic peripheral nerve disease.

    Terrence, C F; Fromm, G H; Tenicela, R

    1985-01-01

    Baclofen has shown analgesic properties in a number of animal studies but has failed as a conventional analgesic in the human postoperative dental pain model. In order to test baclofen's analgesic properties in more chronic pain conditions, we selected postherpetic neuralgia and diabetic neuropathy pain as possible trial diseases for baclofen analgesia. 15 patients with postherpetic neuralgia and 10 with diabetic neuropathy pain were treated with baclofen. In the spinal postherpetic neuralgia group and diabetic neuropathy group, there was little evidence of analgesic effect. 6 of 7 patients with facial postherpetic neuralgia had a good response to baclofen during the 3-week trial. Baclofen does not appear to be a conventional analgesic.

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

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

    2014-08-01

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

  10. Suprofen: the pharmacology and clinical efficacy of a new non-narcotic peripheral analgesic.

    Tolman, E L; Rosenthale, M E; Capetola, R J; McGuire, J L

    1984-08-01

    Suprofen is a potent, peripherally-acting, non-narcotic analgesic agent. The mechanism of action of the compound involves inhibition of prostaglandin biosynthesis and, perhaps, direct antagonism of the peripheral, pain inducing actions of prostaglandins, bradykinin and other pain mediators. Suprofen at a dose of 200 mg appears to be equal or greater in efficacy as an analgesic modality than those of ibuprofen, propoxyphene, naproxen and diflunisal or a combination of 650 mg aspirin plus 60 mg codeine. Its clinical utility has been amply demonstrated in the treatment of a number of types of pain including general and orthopedic surgery, episiotomy, post-partum pain, dysmenorrhea, dental pain and musculoskeletal disorders. Suprofen represents a new class of orally effective nonnarcotic analgesics with potential for effective clinical use in the treatment of pain.

  11. Study on Analgesic Effect of Traditional Chinese Medicine

    YU Shan; XU Ling; WEI Pin-kang; QIN Zhi-feng; LI Jun; PENG Hai-dong

    2008-01-01

    Chinese medicine has been used in treating pain for a long time.Much progress has been made in studies on the mechanism of the analgesic effect of Chinese medicine in animal experiments.It is found that the analgesic action may be related to the following actions:(1)Reducing the secretion of peripheral algogenic substances and inducing the secretion of pain-sensitive substances;(2)Alleviating the accumulation of local algogenic substances;(3)Increasing the release of endogenous analgesic substances;(4)Regulating c-fos gene and increasing the secretion of such substances in the central newous system,etc.In this paper,the experimental methods and analgesic effect of Chinese medicines are reviewed.

  12. Investigation of the Central and Peripheral Analgesic and Anti-inflammatory Activity of Kutajarishta, an Indian Ayurvedic formulation

    Ashraful Kabir

    2012-11-01

    Full Text Available Kutajarishta (KTJ is an Ayurvedic formulation approved by the “National formulary of Ayurvedic Medicine 2011”, of Bangladesh. It is widely available in the Bangladeshi market as an effective preparation to treat lumbago, sciatia and arthritic pain of joints. Our present studies make an attempt toward identifying probable anti-nociceptive and anti-inflammatory mechanisms of KTJ. KTJ, at three doses, (10mL/kg, 20mL/kg, and 40mL/kg showed no involvement of the CNS in anti-nociceptive activity of KTJ. Carrageenan induced paw edema and acetic acid writhing tests both gave significant results (P ≤ 0.05, indicating possible peripheral analgesic and anti-inflammatory action. Formalin induced paw-licking test showed that KTJ had significant effect in suppressing inflammatory pain (P≤0.05 but not neurogenic pain. Hence our study shows anti-inflammatory and peripheral analgesic action for KTJ.

  13. Renal and related cardiovascular effects of conventional and COX-2-specific NSAIDs and non-NSAID analgesics.

    Whelton, A

    2000-03-01

    On a daily basis it appears that as many as one in five adults in the United States may consume an analgesic compound either on a prescription basis or by over-the-counter (OTC) purchase. This high profile of intermittent or repetitive analgesic use appears to be relatively similar throughout the developed world. Although analgesics generally have a good renal safety profile, the nonsteroidal anti-inflammatory drug (NSAID) analgesics may produce mild renal side effects, such as the generation of peripheral edema in up to 5% of the general population. Other more serious renal and related cardiovascular side effects tend to be more apparent in lesser numbers of clinically "at risk" NSAID analgesic users. In contrast, non-NSAID analgesics, such as paracetamol or tramadol, have essentially no renal or related cardiovascular side effects when used at recommended dosing schedules. This review characterizes the renal syndromes associated with the use of NSAID analgesics, identifies the risks inherent in the use of these compounds in treated patients with hypertension and congestive heart failure, summarizes the early comparable data available for the new COX-2-specific inhibitors, and profiles the scant acute and long-term clinical concerns attendant with the use of non-NSAID nonnarcotic analgesics. It is important that healthcare providers and practitioners are aware of the relative renal risks of different analgesics and that they use this knowledge to counsel the analgesic-consuming population appropriately.

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

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

    2013-01-01

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

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

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

    2013-06-01

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

  16. Analgesic effects of dexamethasone in burn injury

    Werner, Mads U; Lassen, Birgit Vibeke; Kehlet, Henrik

    2002-01-01

    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....... 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...

  17. Preliminary evaluation of the analgesic and anti-inflammatory effects of Tacca integrifolia in rodents

    Thatree Autsavakitipong

    2015-01-01

    Full Text Available Summary. This is a preliminary investigation of the ethyl acetate extract of the leaf of Tacca integrifolia (TIE for the analgesic activity using writhing response in mice, tail flick test in rats and for anti-inflammatory activity using ethyl phenyl propiolate (EPP-induced ear edema, carrageenan- and arachidonic acid-induced hind paw edema, as well as cotton pellet-induced granuloma formation in rats. The results showed that TIE (200 mg/kg, PO significantly inhibited pain caused by acetic acid injection (65.9% but did not exhibit effect in tail flick test in rats. These findings suggest that analgesic mechanism of TIE may act via peripherally pathway. The study of anti-inflammatory effect showed that TIE significantly inhibited ear edema induced by EPP. TIE (200 mg/kg, PO inhibited paw edema induced by carrageenan (55.5% and arachidonic acid (48.6% but had no effect on cotton-induced granuloma formation in rats. In conclusion, the ethyl acetate extract of leaf of T. integrifolia possessed anti-inflammatory activity in acute inflammation and analgesic activity.Industrial relevant. Plants of the genus Tacca have been reported to possess many activities such as analgesic, anti-inflammatory and, antipyretic activities. Many species have been used to treat high blood pressure, burn, gastric ulcer, and hepatitis. The scientific studies supporting the traditional uses of Tacca integrifolia for some of the alleged activities are still lacking. The screening test for analgesic and anti-inflammatory effect of the ethyl acetate extract of the leaf of Tacca integrifolia provides scientific data to confirm the potentials of T. integrifolia as an analgesic and anti-inflammatory medicinal plant. In addition, the outcomes may be useful to develop a new analgesic and anti-inflammatory drug in the future. Key words. Tacca integrifolia; Taccaceae; ethyl acetate extract; analgesic activity; anti-inflammatory activity

  18. Local analgesic effect of tramadol is not mediated by opioid receptors in early postoperative pain in rats

    Angela Maria Sousa

    2015-06-01

    Full Text Available BACKGROUND AND OBJECTIVES: Tramadol is known as a central acting analgesic drug, used for the treatment of moderate to severe pain. Local analgesic effect has been demonstrated, in part due to local anesthetic-like effect, but other mechanisms remain unclear. The role of peripheral opioid receptors in the local analgesic effect is not known. In this study, we examined role of peripheral opioid receptors in the local analgesic effect of tramadol in the plantar incision model. METHODS: Young male Wistar rats were divided into seven groups: control, intraplantar tramadol, intravenous tramadol, intravenous naloxone-intraplantar tramadol, intraplantar naloxone-intraplantar tramadol, intravenous naloxone-intravenous tramadol, and intravenous naloxone. After receiving the assigned drugs (tramadol 5 mg, naloxone 200 µg or 0.9% NaCl, rats were submitted to plantar incision, and withdrawal thresholds after mechanical stimuli with von Frey filaments were assessed at baseline, 10, 15, 30, 45 and 60 min after incision. RESULTS: Plantar incision led to marked mechanical hyperalgesia during the whole period of observation in the control group, no mechanical hyperalgesia were observed in intraplantar tramadol group, intraplantar naloxone-intraplantar tramadol group and intravenous naloxone-intraplantar tramadol. In the intravenous tramadol group a late increase in withdrawal thresholds (after 45 min was observed, the intravenous naloxone-intravenous tramadol group and intravenous naloxone remained hyperalgesic during the whole period. CONCLUSIONS: Tramadol presented an early local analgesic effect decreasing mechanical hyperalgesia induced by plantar incision. This analgesic effect was not mediated by peripheral opioid receptors.

  19. Catastrophizing delays the analgesic effect of distraction.

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

    2010-05-01

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

  20. Are peripheral opioid antagonists the solution to opioid side effects?

    Bates, John J

    2012-02-03

    Opioid medication is the mainstay of therapy for severe acute and chronic pain. Unfortunately, the side effects of these medications can affect patient comfort and safety, thus limiting their proven therapeutic potential. Whereas the main analgesic effects of opioids are centrally mediated, many of the common side effects are mediated via peripheral receptors. Novel peripheral opioid antagonists have been recently introduced that can block the peripheral actions of opioids without affecting centrally mediated analgesia. We review the clinical and experimental evidence of their efficacy in ameliorating opioid side effects and consider what further information might be useful in defining their role. IMPLICATIONS: The major analgesic effects of opioid medication are mediated within the brain and spinal cord. Many of the side effects of opioids are caused by activation of receptors outside these areas. Recently developed peripherally restricted opioid antagonists have the ability to block many opioid side effects without affecting analgesia.

  1. The analgesic and anticonvulsant effects of piperine in mice.

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

    2013-12-01

    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 (Ppepper, may be contributing factor in the medicinal uses of black pepper in pain and epilepsy.

  2. Investigation of centrally and peripherally acting analgesic and anti inflammatory activity of biological immune response modulator (an Amazonian plant extract) in animal models of pain and inflammation

    Mital Ravalji; Edwin Cevallos-Arellano; Suresh Balakrishnan

    2015-01-01

    Background: Biological immune response modulator (BIRM) - An aqueous extract of dried roots of the species Dulcamara (family Solanaceae) grown in Ecuador, considered as a natural remedy for various disease is promoted as a natural herbal medicine. Our aim of the study was to assess the central and peripheral analgesic and anti-inflammatory property of BIRM and to study its mechanism of action. Methods: Peripheral analgesic and anti-inflammatory activity was evaluated using acetic acid indu...

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

    Mina Kamkar Asl

    2013-04-01

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

  4. The analgesic effects of exogenous melatonin in humans.

    Andersen, Lars Peter Holst

    2016-10-01

    The hormone, melatonin is produced with circadian rhythm by the pineal gland in humans. The melatonin rhythm provides an endogenous synchronizer, modulating e.g. blood pressure, body temperature, cortisol rhythm, sleep-awake-cycle, immune function and anti-oxidative defence. Interestingly, a number of experimental animal studies demonstrate significant dose-dependent anti-nociceptive effects of exogenous melatonin. Similarly, recent experimental- and clinical studies in humans indicate significant analgesic effects. In study I, we systematically reviewed all randomized studies investigating clinical effects of perioperative melatonin. Meta-analyses demonstrated significant analgesic and anxiolytic effects of melatonin in surgical patients, equating reductions of 20 mm and 19 mm, respectively on a VAS, compared with placebo. Profound heterogeneity between the included studies was, however, present. In study II, we aimed to investigate the analgesic, anti-hyperalgesic and anti-inflammatory effects of exogenous melatonin in a validated human inflammatory pain model, the human burn model. The study was performed as a randomized, double blind placebo-controlled crossover study. Primary outcomes were pain during the burn injury and areas of secondary hyperalgesia. No significant effects of exogenous melatonin were observed with respect to primary or secondary outcomes, compared to placebo. Study III and IV estimated the pharmacokinetic variables of exogenous melatonin. Oral melatonin demonstrated a tmax value of 41 minutes. Bioavailability of oral melatonin was only 3%. Elimination t1/2 were approximately 45 minutes following both oral and intravenous administration, respectively. High-dose intravenous melatonin was not associated with increased sedation, in terms of simple reaction times, compared to placebo. Similarly, no other adverse effects were reported. In Study V, we aimed to re-analyse data obtained from a randomized analgesic drug trial by a selection of

  5. The Analgesic Effect of Pineapple Fruit Juice on Mice

    Ainul Atiqah binti Hilmi

    2014-08-01

    Full Text Available Background: Pain is a feeling stimulated by the nervous system which can be suppressed by giving an analgesic agent. Some studies revealed that pineapples have an analgesic effect. This study aim was to determine analgesic effect of pineapple on mice. Methods: In this experimental study, the effect was examined by using a writhing method on the 28 male mice. Subjects were divided into 4 groups with 7 mice each. The control group received aquades and other groups received pineapple fruit juice with 20%, 40% and 80% concentration with the dosage of 10 mL/kg/body weight. After 30 minutes, 3% acetic acid was injected intraperitoneally to induce pain. Writhing responseswere observed every 5 minutes for 30 minutes. Results: The result for mean of total writhing reaction was 2.39±0.40, 1.92±0.40, 1.50±2.13, 1.66±0.11 respectively for group 1 to 4. These data indicated a significant decrease of total writhing response in mice with 20%, 40% and 80% concentration compared to control group (p=0.023;p=0.000 and p=0.000 respectively. Most optimal concentration was40% with the protective percentage equal to 71.8%. Conclusion: Pineapple fruit juice concentrations (20%, 40%, and 80%has an analgesic effect with the most optimal concentration of 40%.

  6. KETAMINE HAS NO PRE-EMPTIVE ANALGESIC EFFECT

    M E Darabi

    2008-12-01

    Full Text Available Previous studies have suggested that ketamine, an N-methyl-D-aspartate (NMDA receptor antagonist, provides a pre-emptive analgesic effect and pre-emptive analgesia improves postoperative pain management. The aim of this study was to determine the effict of pre-incisional vs. post-incisional intravenous low dose of racemic ketamine in postoperative pain in children undergoing inguinal hernia repair. Seventy-five children aged 1-6 years who were scheduled for inguinal herniorrhaphy were included in a prospective, double-blind randomized controlled trial. Patients were randomly allocated to three groups (pre-incisional, post-incisional and control. Patients in pre-incisional group received an intravenous bolus of racemic ketamine (0.25 mg/kg before surgical incision and patients in post-incisional group received the same dose of racemic ketamine after surgical incision. Children of control group received intravenous boluses of normal saline. In post anesthesia care unit and pediatric surgical ward, the degree of pain and sedation, additional analgesic requirements and side effects were evaluated. There were no differences between groups with respect to demographic and hemodynamic parameters. Pain and sedation scores were not statistically different between groups during 24 h study. In addition, there was no significant difference among groups in number of supplementary analgesic requirements and postoperative nausea and vomiting in the first 24 h. No other side effects were reported during the study period. We found that low dose racemic ketamine administered prior to surgical incision has no pre-emptive effect on post-operative pain and supplementary analgesic requirement during the first 24 h after herniorrhaphy in pediatric patients. "n 

  7. Analgesic and Anti-inflammatory Effects of Ginger Oil

    JIA Yong-liang; XIE Qiang-min; ZHAO Jun-ming; ZHANG Lin-hui; SUN Bao-shan; BAO Meng-jing; LI Fen-fen; SHEN Jian; SHEN Hui-jun; ZHAO Yu-qing

    2011-01-01

    Objective Ginger (Zingiber officinale) is widely used as a spice in cooking and as a medicinal herb in traditional herbal medicine. The present study was to investigate the analgesic and anti-inflammatory activities of ginger oil in experimental animal models. Methods The analgesic effect of the oils was evaluated by the "acetic acid" and "hot-plate" test models of pain in mice. The anti-inflammatory effect of the oil was investigated in rats, using rat paw edema induced by carrageenan, adjuvant arthritis, and vascular permeability induced by bradykinin, arachidonic acid, and histamine. Indomethacin (1 mg/kg), Aspirin (0.5 g/kg) and Dexamethasone (2.5 mg/kg) were used respectively as reference drugs for comparison. Results The ginger oil (0.25-1.0 g/kg) produced significant analgesic effect against chemically- and thermally-induced nociceptive pain stimuli in mice (P < 0.05, 0.01). And the ginger oil (0.25-1.0 g/kg) also significantly inhibited carrageenan-induced paw edema, adjuvant arthritis, and inflammatory mediators-induced vascular permeability in rats (P < 0.05, 0.001). Conclusion These findings confirm that the ginger oil can be used to treat pain and chronic inflammation such as rheumatic arthritis.

  8. Impairment of aspirin antiplatelet effects by non-opioid analgesic medication

    Amin; Polzin; Thomas; Hohlfeld; Malte; Kelm; Tobias; Zeus

    2015-01-01

    Aspirin is the mainstay in prophylaxis of cardiovascular diseases. Impaired aspirin antiplatelet effects are associated with enhanced incidence of cardiovascular events. Comedication with non-opioid analgesic drugs has been described to interfere with aspirin,resulting in impaired aspirin antiplatelet effects. Additionally,nonopioid analgesic medication has been shown to enhance the risk of cardiovascular events and death. Pain is very frequent and many patients rely on analgesic drugs to control pain. Therefore effective analgesic options without increased risk of cardiovascular events are desirable. This review focuses on commonly used nonopioid analgesics,interactions with aspirin medication and impact on cardiovascular risk.

  9. [Has ketamine preemptive analgesic effect in patients undergoing abdominal hysterectomy?].

    Karaman, Semra; Kocabaş, Seden; Zincircioğlu, Ciler; Firat, Vicdan

    2006-07-01

    The aim of this study was to determine if preemptive use of the NMDA receptor antogonist ketamine decreases postoperative pain in patients undergoing abdominal hystrectomy. A total of 60 patients admitted for total abdominal hysterectomy were included in this study after the approval of the ethic committee, and the patients were randomly classified into three groups. After standart general anaesthesia, before or after incision patients received bolus saline or ketamine. Group S received only saline while Group Kpre received ketamine 0.4 mg/kg before incision and saline after incision, and Group Kpost received saline before incision and 0.4 mg/kg ketamine after incision. Postoperatif analgesia was maintained with i.v. PCA morphine. Pain scores were assessed with Vizüal Analog Scale (VAS), Verbal Rating Scale (VRS) at 1., 2, 3., 4., 8., 12. ve 24. hours postoperatively. First analgesic requirement time, morphine consumption and side effects were recorded. There were no significant differences between groups with respect to VAS / VRS scores, the time for first analgesic dose, and morphine consumption ( p>0.05). Patients in Group S had significantly lower sedation scores than either of the ketamine treated groups ( pketamin had no preemptive analgesic effect in patients undergoing abdominal hysterectomy, but further investigation is needed for different operation types and dose regimens.

  10. Non-analgesic effects of opioids

    Højsted, Jette; Kurita, Geana Paula; Kendall, Sally;

    2012-01-01

    Opioids constitute the basis for pharmacological treatment of moderate to severe pain in cancer pain and non-cancer pain patients. Their action is mediated by the activation of opioid receptors, which integrates the pain modulation system with other effects in the central nervous system including...... cognition resulting in complex interactions between pain, opioids and cognition. The literature on this complexity is sparse and information regarding the cognitive effects of opioids in chronic pain patients is substantially lacking. Two previous systematic reviews on cancer pain and non-cancer pain...... patients only using controlled studies were updated. Fourteen controlled studies on the cognitive effects of opioids in chronic non-cancer pain patients and eleven controlled studies in cancer pain patients were included and analyzed. Opioid treatment involved slightly opposite outcomes in the two patient...

  11. [Analgesic placebo effect: contribution of the neurosciences].

    Berna, C; Cojan, Y; Vuilleumier, P; Desmeules, J

    2011-06-29

    Over the past twenty years, neuroscience has changed our understanding of placebo analgesia. Often perceived by researchers as a response bias adding noise to the assessment of efficacy, in the patients' view, it is associated with charlatanism. The origin of the word, qualifying a patient's response to "please" the doctor, did not help its rightful appreciation. However, today the placebo analgesia is considered as a psychobiological phenomenon. Thanks to pharmacological manipulations and the development of functional brain imaging, the neural circuitry involved in this effect as well as the role of endorphins and dopamine have been identified. This article describes our current knowledge about this fascinating phenomenon: a psychological modulation can lead to a biological effect.

  12. Effective analgesic modalities for ambulatory patients.

    Redmond, Martin; Florence, Barry; Glass, Peter S A

    2003-06-01

    The introduction of government-mandated standards for pain management has focused our attention on postoperative pain. With the recent JACHO standards' for ambulatory surgery, it is imperative that all health care workers who care for these patients are familiar with appropriate pain management. Developments in our understanding of the pathophysiology of acute pain have further enhanced our ability to improve pain management for postoperative ambulatory patients. This has led to the concept of preventive analgesia (inhibition of physiological and pathological secondary inflammatory pain). Extensive work has shown that this is best achieved using a multimodel approach usually consisting of an NSAID, opioid, and local anesthetic. NMDA antagonists (ketamine, dextromethorphan) and alpha-2 agnoists (clonodine) show potential supplements to further enhance pain management, especially if given preemptively. Nonpharmacological intervention such as cold therapy or acupuncture may also be considered. The armanentarium for effective pain management has improved substantially over the past few years. The challenge is for health care workers to implement these therapies to obtain optimum pain management in ambulatory surgical patients.

  13. Coffee drinking enhances the analgesic effect of cigarette smoking

    Nastase, Anca; Ioan, Silvia; Braga, Radu I

    2007-01-01

    Nicotine (from cigarette smoke) and caffeine (from coffee) have analgesic effects in humans and experimental animals. We investigated the combined effects of coffee drinking and cigarette smoking on pain experience in a group of moderate nicotine-dependent, coffee drinking, young smokers. Pain...... threshold and pain tolerance were measured during cold pressor test following the habitual nocturnal deprivation of smoking and coffee drinking. Smoking increased pain threshold and pain tolerance in both men and women. Coffee drinking, at a dose that had no independent effect, doubled the increase in pain...

  14. Role of central arginine vasopressin receptors in the analgesic effect of CDP-choline on acute and neuropathic pain.

    Bagdas, Deniz; Yucel-Ozboluk, Hasret; Orhan, Fulya; Kanat, Ozkan; Isbil-Buyukcoskun, Naciye; Gurun, Mine S

    2013-12-04

    Recent studies have demonstrated that arginine vasopressin (AVP) plays a crucial role in pain modulation. In addition, our previous studies have proven that centrally administered cytidine-5'-diphosphate-choline (CDP-choline; citicoline) elicits an analgesic effect in different pain models in rats. Given that CDP-choline enhances central and peripheral vasopressin levels, the present study was designed to investigate the role of central AVP receptors in the analgesic effect of CDP-choline in acute and chronic constriction injury-induced neuropathic pain models. For this purpose, rats were pretreated intracerebroventricularly with the AVP V1 or AVP V2 receptor antagonist 15 min before intracerebroventricular injection of CDP-choline or saline, and pain threshold was determined using the Randall-Selitto test. AVP V1 and AVP V2 receptor antagonist blocked the CDP-choline-induced analgesic effect either in acute or neuropathic models of pain in rats. These results suggest, for the first time, that central AVP receptors are involved in the CDP-choline-elicited analgesic effect.

  15. ANALGESIC AND ANTI-INFLAMMATORY EFFECT OF AN AQUEOUS EXTRACT OF DENDROCNIDE SINUATA (BLUME CHEW

    Binita Angom

    2015-12-01

    Full Text Available The study was aimed to evaluate the analgesic and anti-inflammatory effect of aqueous root extracts of Dendrocnide sinuata (Blume Chew (AEDS in Swiss albino mice and wistar rats. The animals were orally administered AEDS at doses 30 and 100 mgkg-1 (p.o. For analgesic study, acetic acid-induced Writhing test, Eddy’s hot plate and Tail Flick model was performed in mice. For antiinflammatory study, carrageen-induced paw edema study was performed in rats. In acetic acid induced model, effect of AEDS was comparable with the standard meloxicam 10 mgkg-1 (i.p. In the hot plate model, the maximum effect was observed at 30 min at a dose of 100 mgkg-1 (p.o which was comparable with the standard Pentazocine 10 mgkg-1 (p.o, whereas in the tail flick model no significant changes were observed. In the carrageenan-induced paw edema model, administration of AEDS showed significant (P < 0.05 dose dependent inhibition of edema formation. AEDS was effective in both narcotic and non-narcotic models of analgesia. It also showed a significant dose-dependent increase in antiedematogenic activity which revealed good peripheral anti-inflammatory properties of the extract.

  16. Analgesic effects of various extracts of the root of Abutilon indicum linn

    Naveen Goyal

    2009-01-01

    Full Text Available Purpose : Abutilon indicum (Linn. sweet (Malvaceae commonly called ′Country Mallow′ is a perennial plant up to 3 m in height. It is abundantly found as a weed in the sub-Himalayan tract and in the hotter parts of India. The plant is traditionally used for treatment of several diseases like bronchitis, body ache, toothache, jaundice, diabetes, fever, piles, leprosy, ulcers, cystitis, gonorrhea, diarrhea, and so on. Abutilon indicum Linn. is reported to have hepatoprotective, hypoglycemic, antimicrobial, male contraceptive, and antidiarrheal activities. The present study was done to evaluate the analgesic potential of various extracts of the root of Abutilon indicum Linn. Materials and Methods : The powdered root (900 g was subjected to successive solvent extraction, with solvents in increasing order of polarity, namely, petroleum ether (60 - 80΀C, methanol, and ethanol, using the soxhlet apparatus for 72 hours. The marc was extracted by cold maceration for 72 hours, to obtain a water-soluble extract. The peripheral analgesic activity was studied using acetic acid-induced writhing method in Swiss albino mice (20 - 30 g, while the central analgesic activity was evaluated by the tail flick method and the tail immersion method. Results : Results indicated that all the tested extracts, except the methanol extract, exhibited significant analgesic activity in both animals′ models. Petroleum ether extract showed higher analgesic activity. The activity may be related to the central mechanism or may be due to the peripheral analgesic mechanisms. Conclusion : The present study authenticates the traditional use.

  17. Analgesic activity and pharmacological characterization of N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl] propenamide, a new opioid agonist acting peripherally.

    Goicoechea, Carlos; Sánchez, Eva; Cano, Carolina; Jagerovic, Nadine; Martín, Maria Isabel

    2008-10-24

    We previously reported the synthesis of three new opioid agonists as well as their in vitro and in vivo activity [Girón, R., Abalo, R., Goicoechea, C., Martín, M.I., Callado, L.F., Cano, C., Goya, P., Jagerovic, N. 2002. Synthesis and opioid activity of new fentanyl analogs. Life Sci. 71, 1023-1034]. One of them, N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl)] propenamide (IQMF-4), showed an interesting antinociceptive activity. Intraperitoneally (i.p.) administered, it was as effective as fentanyl or morphine, being less potent than fentanyl but more so than morphine. The aim of the present work was to evaluate its antinociceptive effect by different routes of administration, using the hot plate test, and to investigate possible side effects, such as tolerance and withdrawal, in vitro, using the myenteric plexus-longitudinal muscle strip preparation from guinea pig ileum, and in vivo, using the hot plate test. IQMF-4 was more potent than morphine when administered per os (p.o.), but less potent when administered intracerebroventricularly (i.c.v.). By both routes, fentanyl is more potent that IQMF-4. When IQMF-4 was administered i.p., naloxone methiodide, a peripherally acting antagonist, was able to completely block its antinociceptive effect, whereas, after i.c.v. administration, the blockade was only partial. An interesting feature of the new compound is that it induces tolerance in vitro but not in vivo. Moreover, though in vitro withdrawal was not different from fentanyl or morphine, in vivo withdrawal symptoms were significantly less frequent in mice treated with IQMF-4 than in those treated with morphine or fentanyl. Although more assays are required, these results show that IQMF-4 appears to be a potent analgesic compound with an interesting peripheral component, and reduced ability to induce dependence.

  18. Combination of pharmacotherapy and lidocaine analgesic block of the peripheral trigeminal branches for trigeminal neuralgia: a pilot study

    Fabrizio Di Stani

    2015-08-01

    Full Text Available Classical trigeminal neuralgia (CTN is treated predominantly by pharmacotherapy but side effects and unsuccessful occurs. The current study was carried out to evaluate the therapeutic effect of combination of pharmacotherapy and lidocaine block. Thirteen patients with CTN managed with pharmacotherapy were recruited and assigned either to no additional treatment (Group I or to additional analgesic block (Group II. The primary endpoint was the reduction in the frequency of pain episodes in a month assessed at 30 and 90 days. Comparisons of measurements of pain, general health and depression scales were secondary endpoints. The results from the follow-up visits at 30 and 90 days showed the Group II to have larger reduction in the frequency of pain and exhibited a bigger improvement in the scores of the pain, general health and depression scales. The results from this preliminary study suggest a clinical benefit of the combination of pharmacotherapy and lidocaine block.

  19. Combination of pharmacotherapy and lidocaine analgesic block of the peripheral trigeminal branches for trigeminal neuralgia: a pilot study.

    Di Stani, Fabrizio; Ojango, Christine; Dugoni, Demo; Di Lorenzo, Luigi; Masala, Salvatore; Delfini, Roberto; Bruti, Gianluca; Simonetti, Giovanni; Piovesan, Elcio Juliato; Ruggeri, Andrea Gennaro

    2015-08-01

    Classical trigeminal neuralgia (CTN) is treated predominantly by pharmacotherapy but side effects and unsuccessful occurs. The current study was carried out to evaluate the therapeutic effect of combination of pharmacotherapy and lidocaine block. Thirteen patients with CTN managed with pharmacotherapy were recruited and assigned either to no additional treatment (Group I) or to additional analgesic block (Group II). The primary endpoint was the reduction in the frequency of pain episodes in a month assessed at 30 and 90 days. Comparisons of measurements of pain, general health and depression scales were secondary endpoints. The results from the follow-up visits at 30 and 90 days showed the Group II to have larger reduction in the frequency of pain and exhibited a bigger improvement in the scores of the pain, general health and depression scales. The results from this preliminary study suggest a clinical benefit of the combination of pharmacotherapy and lidocaine block.

  20. Analgesic use - prevalence, biomonitoring and endocrine and reproductive effects

    Kristensen, David Møbjerg; Mazaud-Guittot, Sverine; Gaudriault, Pierre

    2016-01-01

    Paracetamol and NSAIDs, in particular acetylsalicylic acid (aspirin) and ibuprofen, are among the most used and environmentally released pharmaceutical drugs. The differences in international trends in the sale and consumption of mild analgesics reflect differences in marketing, governmental...... policies, habits, accessibility, disease patterns and the age distribution of each population. Biomonitoring indicates ubiquitous and high human exposure to paracetamol and to salicylic acid, which is the main metabolite of acetylsalicylic acid. Furthermore, evidence suggests that analgesics can have...

  1. 信息动态%Anti-inflammatory and analgesic effects of granule to pelvic inflammation

    2011-01-01

    Objective To study anti-inflammatory and analgesic effects of granucle to pelvic inflammation. Methods The anti-inflammatory effects were studied by dimethylbenzene-induced swelling oar in mouse, carrageenin induced paw edema and tampon-induced proliferation in rats. The analgesic effects were studied by acetic acid-induced writhing and optothermal-induced pain in mice. Results Granule to pelvic inflammation significantly reduced swelling oar in mouse, paw edema and proliferation in rats;prolonged latency of writhing test, reduced the writhing number and improved optothermal-induced analgesia percentage. Conclusion Granule to pelvic inflammation has anti-inflammatory and analgesic effects.

  2. Pure analgesics in a rheumatological outpatient clinic

    M.A. Cimmino

    2011-09-01

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

  3. The analgesic effect of orexin-A in a murine model of chemotherapy-induced neuropathic pain.

    Toyama, Satoshi; Shimoyama, Naohito; Shimoyama, Megumi

    2017-02-01

    Orexins are neuropeptides that are localized to neurons in the lateral and dorsal hypothalamus but its receptors are distributed to many different regions of the central nervous system. Orexins are implicated in a variety of physiological functions including sleep regulation, energy homeostats, and stress reactions. Furthermore, orexins administered exogenously have been shown to have analgesic effects in animal models. A type of intractable pain in patients is pain due to chemotherapy-induced peripheral neuropathy (CIPN). Several chemotherapeutic agents used for the treatment of malignant diseases induce dose-limiting neuropathic pain that compromises patients' quality of life. Here, we examined the analgesic effect of orexin-A in a murine model of CIPN, and compared it with the effect of duloxetine, the only drug recommended for the treatment of CIPN pain in patients. CIPN was induced in male BALB/c mice by repeated intraperitoneal injection of oxaliplatin, a platinum chemotherapeutic agent used for the treatment of advanced colorectal cancer. Neuropathic mechanical allodynia was assessed by the von Frey test, and the effect on acute thermal pain was assessed by the tail flick test. Intracerebroventricularly administered orexin-A dose-dependently attenuated oxaliplatin-induced mechanical allodynia and increased tail flick latencies. Oxaliplatin-induced mechanical allodynia was completely reversed by orexin-A at a low dose that did not increase tail flick latency. Duloxetine only partially reversed mechanical allodynia and had no effect on tail flick latency. The analgesic effect of orexin-A on oxaliplatin-induced mechanical allodynia was completely antagonized by prior intraperitoneal injection of SB-408124 (orexin type-1 receptor antagonist), but not by prior intraperitoneal injection of TCS-OX2-29 (orexin type-2 receptor antagonist). Our findings suggest that orexin-A is more potent than duloxetine in relieving pain CIPN pain and its analgesic effect is

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

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

    2011-09-01

    Some endogenous hormones (epinephrine and cortisol) can change an individual's pain threshold. Propranolol is a non-selective β adrenergic receptor blocker which antagonises the anti-inflammatory effect of non-steroidal anti-inflammatory drugs via the β1 and β2 adrenergic receptors. The roles of epinephrine and cortisol were investigated in the analgesic activity of metyrosine in rats with reduced epinephrine levels induced by metyrosine. Pain threshold measurement was performed using an analgesimeter with different doses and the single or combined usage of metyrosine, prednisolone, metyrapone and propranolol in rats. Epinephrine and corticosterone levels were measured by high-performance liquid chromatography in metyrosineadministered rats. Metyrosine reduces the epinephrine levels without affecting the corticosterone levels, thereby creating an analgesic effect. It was determined that prednisolone did not have an analgesic effect in rats with normal epinephrine levels, but its analgesic activity increased with a parallel decrease in the epinephrine levels. Similarly, the combined use of prednisolone and metyrosine provided a stronger analgesic effect than that rendered by metyrosine alone. The strongest analgesic effect, however, was observed in the group of rats with the lowest epinephrine level in whom the metyrosine + prednisolone combination was administered. The findings of this study may be useful in severe pain cases in which the available analgesics are unable to relieve the individual's pain.

  5. Analgesic Effects of Various Extracts of Root of Abutilon indicum linn.

    Sumitra Singh

    2009-12-01

    Full Text Available

    Abutilon indicum (Linn. sweet (Malvaceae commonly called “Country Mallow” is a perennial plant up to 3m in
    height. It is abundantly found as weed in sub-Himalayan tract and in hotter parts of India. The plant is traditionally
    used for treatment of several diseases like bronchitis, body ache, toothache, jaundice, diabetes, fever, piles,
    leprosy, ulcers, cystitis, gonorrhea, diarrhoea etc. Abutilon indicum Linn. is reported to have hepatoprotective,
    hypoglycemic, antimicrobial, male contraceptive and antidiarrhoeal activities. The present study was done to
    evaluate the analgesic potential of various extracts of root of Abutilon indicum Linn. The powdered root (900 g
    was subjected to successive solvent extraction with solvents in increasing order of polarity viz. petroleum ether
    (60-80 C°, methanol and ethanol by soxhlet apparatus for 72 hrs. The marc was extracted by cold maceration for
    72 hrs. to obtain water soluble extract. Peripheral analgesic activity was studied using acetic acid induced writhing
    method in Swiss albino mice (20-30 g while central analgesic activity was evaluated by tail flick method and
    tail immersion method. Results indicated that all the tested extracts except methanol extract exhibited significant
    analgesic activity in both animals’ models. Petroleum ether extract showed higher analgesic activity. The activity
    may be related with central mechanism or due to peripheral analgesic mechanisms. Thus the present study authenticates
    the traditional use.

  6. Analgesic activity of Heliopsis longipes and its effect on the nervous system.

    Cilia-López, V G; Juárez-Flores, B I; Aguirre-Rivera, J R; Reyes-Agüero, J A

    2010-02-01

    Heliopsis longipes S.F. Blake (Asteraceae: Heliantheae) (chilcuague) is used in Mexican traditional medicine against parasites and to alleviate tooth and muscle pains. Its biocide effect has already been experimentally demonstrated; however, its analgesic action and its action on the nervous system (NS) have not been investigated yet. The objectives of this study were to evaluate the analgesic action of affinin and the H. longipes root ethanol extract, as well as their effects on the NS using an animal model. The ethanol extract was obtained by maceration, and affinin was purified from it through chromatographic techniques. Chemical and thermal analgesia were used to assess their analgesic proprieties. Irwin's test was used to evaluate their stimulating or depressing effects. The ethanol extract and affinin displayed analgesic action similar to ketorolac and stimulating effect comparable to caffeine on the nervous system of adult mice.

  7. Effect of intravenous esmolol on analgesic requirements in laparoscopic cholecystectomy

    Dhir, Ritima; Singh, Mirley Rupinder; Kaul, Tej Kishan; Tewari, Anurag; Oberoi, Ripul

    2015-01-01

    Background and Aims: Perioperative beta blockers are also being advocated for modulation of acute pain and reduction of intraoperative anesthetic requirements. This study evaluated the effect of perioperative use of esmolol, an ultra short acting beta blocker, on anesthesia and modulation of post operative pain in patients of laproscopic cholecystectomy. Material and Methods: Sixty adult ASA I & II grade patients of either sex, scheduled for laparoscopic cholecystectomy under general anesthesia, were enrolled in the study. The patients were randomly allocated to one of the two groups E or C according to computer generated numbers. Group E- Patients who received loading dose of injection esmolol 0.5 mg/kg in 30 ml isotonic saline, before induction of anesthesia, followed by an IV infusion of esmolol 0.05 μg/kg/min till the completion of surgery and Group C- Patients who received 30 ml of isotonic saline as loading dose and continuous infusion of isotonic saline at the same rate as the esmolol group till the completion of surgery. Results: The baseline MAP at 0 minute was almost similar in both the groups. At 8th minute (time of intubation), MAP increased significantly in group C as compared to group E and remained higher than group E till the end of procedure. Intraoperatively, 16.67% of patients in group C showed somatic signs as compared to none in group E. The difference was statistically significant. 73.33% of patients in group C required additional doses of Inj. Fentanyl as compared to 6.67% in group E. Conclusions: We conclude that intravenous esmolol influences the analgesic requirements both intraoperatively as well as postoperatively by modulation of the sympathetic component of the pain i.e. heart rate and blood pressure. PMID:26330719

  8. Effect of intravenous esmolol on analgesic requirements in laparoscopic cholecystectomy

    Ritima Dhir

    2015-01-01

    Full Text Available Background and Aims: Perioperative beta blockers are also being advocated for modulation of acute pain and reduction of intraoperative anesthetic requirements. This study evaluated the effect of perioperative use of esmolol, an ultra short acting beta blocker, on anesthesia and modulation of post operative pain in patients of laproscopic cholecystectomy. Material and Methods: Sixty adult ASA I & II grade patients of either sex, scheduled for laparoscopic cholecystectomy under general anesthesia, were enrolled in the study. The patients were randomly allocated to one of the two groups E or C according to computer generated numbers. Group E- Patients who received loading dose of injection esmolol 0.5 mg/kg in 30 ml isotonic saline, before induction of anesthesia, followed by an IV infusion of esmolol 0.05 μg/kg/min till the completion of surgery and Group C- Patients who received 30 ml of isotonic saline as loading dose and continuous infusion of isotonic saline at the same rate as the esmolol group till the completion of surgery. Results: The baseline MAP at 0 minute was almost similar in both the groups. At 8th minute (time of intubation, MAP increased significantly in group C as compared to group E and remained higher than group E till the end of procedure. Intraoperatively, 16.67% of patients in group C showed somatic signs as compared to none in group E. The difference was statistically significant. 73.33% of patients in group C required additional doses of Inj.Fentanyl as compared to 6.67% in group E. Conclusions: We conclude that intravenous esmolol influences the analgesic requirements both intraoperatively as well as postoperatively by modulation of the sympathetic component of the pain i.e. heart rate and blood pressure.

  9. Evaluation of 2 celecoxib derivatives: analgesic effect and selectivity to cyclooxygenase-2/1

    Zhi-hong LU; Xiao-yun XIONG; Bang-le ZHANG; Guo-cheng LIN; Yu-xiang SHI; Zhen-guo LIU; Jing-ru MENG; Yu-mei ZHOU; Qi-bing MEI

    2005-01-01

    analgesic effects and the ability to selectively inhibit COX-2. Substitution with a naphthyl group may have more effect on the peripheral pain pathway, whereas substitution with an isopropyl group may have more effect on the central pain pathway. This phenomenon occurs partly because substitution with an isopropyl group is more beneficial for COX-2 selectivity than is substitution with a naphthyl group.

  10. Differential Effectiveness of Clinically-Relevant Analgesics in a Rat Model of Chemotherapy-Induced Mucositis.

    Alexandra L Whittaker

    Full Text Available Chemotherapy-induced intestinal mucositis is characterized by pain and a pro-inflammatory tissue response. Rat models are frequently used in mucositis disease investigations yet little is known about the presence of pain in these animals, the ability of analgesics to ameliorate the condition, or the effect that analgesic administration may have on study outcomes. This study investigated different classes of analgesics with the aim of determining their analgesic effects and impact on research outcomes of interest in a rat model of mucositis. Female DA rats were allocated to 8 groups to include saline and chemotherapy controls (n = 8. Analgesics included opioid derivatives (buprenorphine; 0.05mg/kg and tramadol 12.5mg/kg and NSAID (carprofen; 15mg/kg in combination with either saline or 5-Fluorouracil (5-FU; 150mg/kg. Research outcome measures included daily clinical parameters, pain score and gut histology. Myeloperoxidase assay was performed to determine gut inflammation. At the dosages employed, all agents had an analgesic effect based on behavioural pain scores. Jejunal myeloperoxidase activity was significantly reduced by buprenorphine and tramadol in comparison to 5-FU control animals (53%, p = 0.0004 and 58%, p = 0.0001. Carprofen had no ameliorating effect on myeloperoxidase levels. None of the agents reduced the histological damage caused by 5-FU administration although tramadol tended to increase villus length even when administered to healthy animals. These data provide evidence that carprofen offers potential as an analgesic in this animal model due to its pain-relieving efficacy and minimal effect on measured parameters. This study also supports further investigation into the mechanism and utility of opioid agents in the treatment of chemotherapy-induced mucositis.

  11. [A comparative study of the effectiveness of the analgesic effect of electropuncture stimulation and nonnarcotic analgesics in therapy patients in an emergency dental care office].

    Moroz, B T; Kalinin, V I; Emel'ianova, M V; Rozin, I Ia; Trebich, I Ia

    1990-01-01

    Analysis of patients' subjective sensations, of rheography and electro-odontometry data has lead the authors to a conclusion that the analgesic effect of rengasil was higher than that of ibuprofen and that rengasil combination with electropuncture was still more effective. The analgesic effect was the most marked in alveolitis and periodontitis, less so in inflammations of the pulp, and no effect could be achieved in acute purulent pulpitis. The authors suppose that pain syndrome alleviation after electropuncture stimulation and after administration of anti-inflammatory drugs is explained mainly by changed hemodynamics at the site of inflammation, this resulting in reduction of the edema and in diminished effects of biochemical substances released in the course of inflammation.

  12. Effects of analgesics and antidepressants on TREK-2 and TRESK currents

    Park, Hyun; Kim, Eun-Jin; Han, Jaehee; Han, Jongwoo

    2016-01-01

    TWIK-related K+ channel-2 (TREK-2) and TWIK-related spinal cord K+ (TRESK) channel are members of two-pore domain K+ channel family. They are well expressed and help to set the resting membrane potential in sensory neurons. Modulation of TREK-2 and TRESK channels are involved in the pathogenesis of pain, and specifi c activators of TREK-2 and TRESK may be benefi cial for the treatment of pain symptoms. However, the effect of commonly used analgesics on TREK-2 and TRESK channels are not known. Here, we investigated the effect of analgesics on TREK-2 and TRESK channels. The effects of analgesics were examined in HEK cells transfected with TREK-2 or TRESK. Amitriptyline, citalopram, escitalopram, and fluoxetine significantly inhibited TREK-2 and TRESK currents in HEK cells (pnabumetone, and bupropion inhibited TRESK, but had no effect on TREK-2. These results show that all analgesics tested in this study inhibit TRESK activity. Further study is needed to identify the mechanisms by which the analgesics modulate TREK-2 and TRESK differently. PMID:27382354

  13. Analgesic effect of gabapentin in a rat model for chronic constrictive injury

    MA Lu-lu; LIU Wei; HUANG Yu-guang; YANG Nan; ZUO Ping-ping

    2011-01-01

    Background Gabapentin has been widely and successfully used in the clinic for many neuropathic pain syndromes since last decade,however its analgesic mechanisms are still elusive.Our study was to investigate whether Ca2+/calmodulin-dependent protein kinase II (CaMKII) contributes to the analgesic effect of gabapentin on a chronic constriction injury (CCI) model.Methods Gabapentin (2%,100 mg/kg) or saline (0.5 mil100 g) was injected intraperitoneally 15 minutes prior to surgery and then every 12 hours from postoperative day 0-4 to all rats in control,sham and CCI groups.The analgesic effect of gabapentin was assessed by measuring mechanical allodynia and thermal hyperalgesia of rats.Expression and activation of CaMKII were quantified by reverse-transcriptional polymerase chain reaction and Western blotting.Results The analgesic effect of gabapentin on mechanical allodynia and thermal hyperalgesia was significant in the CCI model,with maximal reduction reached on postoperative day 8.Gabapentin decreased the expression of the total CaMKII and phosphorylated CaMKII in CCI rats.Conclusion The analgesic effect of gabapentin on CCI rats may be related to the decreased expression and phosphorylation of CaMKII in the spinal cord.

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

    Tijanić Miloš

    2012-01-01

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

  15. Analgesic activity of piracetam: effect on cytokine production and oxidative stress.

    Navarro, Suelen A; Serafim, Karla G G; Mizokami, Sandra S; Hohmann, Miriam S N; Casagrande, Rubia; Verri, Waldiceu A

    2013-04-01

    Piracetam is a prototype of nootropic drugs used to improve cognitive impairment. However, recent studies suggest that piracetam can have analgesic and anti-inflammatory effects. Inflammatory pain is the result of a process that depends on neutrophil migration, cytokines and prostanoids release and oxidative stress. We analyze whether piracetam has anti-nociceptive effects and its mechanisms. Per oral pretreatment with piracetam reduced in a dose-dependent manner the overt pain-like behavior induced by acetic acid, phenyl-p-benzoquinone, formalin and complete Freund's adjuvant. Piracetam also diminished carrageenin-induced mechanical and thermal hyperalgesia, myeloperoxidase activity, and TNF-α-induced mechanical hyperalgesia. Piracetam presented analgesic effects as post-treatment and local paw treatment. The analgesic mechanisms of piracetam were related to inhibition of carrageenin- and TNF-α-induced production of IL-1β as well as prevention of carrageenin-induced decrease of reduced glutathione, ferric reducing ability and free radical scavenging ability in the paw. These results demonstrate that piracetam presents analgesic activity upon a variety of inflammatory stimuli by a mechanism dependent on inhibition of cytokine production and oxidative stress. Considering its safety and clinical use for cognitive function, it is possible that piracetam represents a novel perspective of analgesic.

  16. Analgesic effects of lappaconitine in leukemia bone pain in a mouse model

    Xiao-Cui Zhu

    2015-05-01

    Full Text Available Bone pain is a common and severe symptom in cancer patients. The present study employed a mouse model of leukemia bone pain by injection K562 cells into tibia of mouse to evaluate the analgesic effects of lappacontine. Our results showed that the lappaconitine treatment at day 15, 17 and 19 could effectively reduce the spontaneous pain scoring values, restore reduced degree in the inclined-plate test induced by injection of K562 cells, as well as restore paw mechanical withdrawal threshold and paw withdrawal thermal latency induced by injection of K562 cells to the normal levels. Additionally, the molecular mechanisms of lappaconitine’s analgesic effects may be related to affect the expression levels of endogenous opioid system genes (POMC, PENK and MOR, as well as apoptosis-related genes (Xiap, Smac, Bim, NF-κB and p53. Our present results indicated that lappaconitine may become a new analgesic agent for leukemia bone pain management.

  17. Study of Analgesic and Anti-inflammatory Effects of Lappaconitine Gelata

    WANG Ying-zi; XIAO YONG-qing; ZHANG Chao; SUN Xiu-mei

    2009-01-01

    Objective:To explore the analgesic and anti-inflammatory effects of lappaconitine gelata (LA). Methods:The writhing response induced by acetic acid, the pain response induced by formaldehyde and hot plate method in the mouse, and the paw edema induced by egg albumen in the rat and the ear edema induced by xylene in the mouse were used for investigation on the analgesic and anti-inflammatory effects of LA.Results: The writhing response induced by acetic acid, the pain response induced by formaldehyde and hot plate methods was significantly inhibited by LA. In addition, the paw edema induced by egg albumen in the rat and the ear edema induced by xylene in the mouse were all significantly suppressed by LA. Conclusion:LA has the analgesic and anti-inflammatory effects.

  18. Enhanced analgesic effects of tramadol and common trace element coadministration in mice.

    Alexa, Teodora; Marza, Aurelia; Voloseniuc, Tudor; Tamba, Bogdan

    2015-10-01

    Chronic pain is managed mostly by the daily administration of analgesics. Tramadol is one of the most commonly used drugs, marketed in combination with coanalgesics for enhanced effect. Trace elements are frequent ingredients in dietary supplements and may enhance tramadol's analgesic effect either through synergic mechanisms or through analgesic effects of their own. Swiss Weber male mice were divided into nine groups and were treated with a combination of the trace elements Mg, Mn, and Zn in three different doses and a fixed dose of tramadol. Two groups served as positive (tramadol alone) and negative (saline) controls. Nociceptive assessment by tail-flick (TF) and hot-plate (HP) tests was performed at baseline and at 15, 30, 45, and 60 min after intraperitoneal administration. Response latencies were recorded and compared with the aid of ANOVA testing. All three trace elements enhanced tramadol's analgesic effect, as assessed by TF and HP test latencies. Coadministration of these trace elements led to an increase of approximately 30% in the average pain inhibition compared with the tramadol-alone group. The most effective doses were 0.6 mg/kg b.w. for Zn, 75 mg/kg b.w. for Mg, and 7.2 mg/kg b.w. for Mn. Associating trace elements such as Zn, Mg, and Mn with the standard administration of tramadol increases the drug's analgesic effect, most likely a consequence of their synergic action. These findings impact current analgesic treatment because the addition of these trace elements may reduce the tramadol dose required to obtain analgesia.

  19. Analgesic and anti-inflammatory activity of root bark of Grewia asiatica Linn. in rodents

    Udaybhan Singh Paviaya

    2013-01-01

    Conclusions: The present study indicates that root bark of G. asiatica exhibits peripheral and central analgesic effect and anti-inflammatory activity, which may be attributed to the various phytochemicals present in root bark of G. asiatica.

  20. Translational pain research: Evaluating analgesic effect in experimental visceral pain models

    Anne Estrup Olesen; Trine Andresen; Lona Louring Christrup; Richard N Upton

    2009-01-01

    Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mechanisms behind the pain and the mode of action of analgesic substances. This can be achieved through standardized experimental human pain models. Experimental pain models in healthy volunteers are advantageous forevaluation of analgesic action, as this is often difficult to assess in the clinic because of confounding factors such as sedation, nausea and general malaise. These pain models facilitate minimizing the gap between knowledge gained in animal and human clinical studies. Combining experimental pain studies and pharmacokinetic studies can improve understanding of the pharmacokineticpharmacodynamic relationship of analgesics and, thus, provide valuable insight into optimal clinical treatment of visceral pain. To improve treatment of visceral pain, it is important to study the underlying mechanisms of pain and the action of analgesics used for its treatment. An experimental pain model activates different modalities and can be used to investigate the mechanism of action of different analgesics in detail. In combination with pharmacokinetic studies and objective assessment such as electroencephalography, new information re- garding a given drug substance and its effects can be obtained. Results from experimental human visceral pain research can bridge the gap in knowledge between animal studies and clinical condition in patients suffering from visceral pain, and thus constitute the missing link in translational pain research.

  1. Comparison of analgesic effects of intra-articular tenoxicam and morphine in anterior cruciate ligament reconstruction.

    Guler, Gulen; Karaoglu, Sinan; Velibasoglu, Hediye; Ramazanogullari, Nesrin; Boyaci, Adem

    2002-07-01

    This study compared the analgesic effect of intra-articular injection of tenoxicam with that of morphine on postoperative pain after anterior cruciate ligament (ACL) reconstruction. Forty-two patients undergoing arthroscopically ACL reconstructions using hamstring tendons underwent the same anesthetic protocol. The patients were randomized to receive 25 ml normal saline, 20 mg tenoxicam in 25 ml normal saline, or 2 mg morphine in 25 ml normal saline. Postoperative pain was assessed using a visual analogue scale and measuring analgesic requirements. We found both that both intra-articular tenoxicam and intra-articular morphine provided better analgesia than that in the control group. Although pain scores were similar between tenoxicam and morphine groups 30 min postoperative, the analgesic requirements in with tenoxicam were significantly lower than those with morphine group 3-6 h postoperatively.

  2. Analgesic effects of fatty acid amide hydrolase inhibition in a rat model of neuropathic pain.

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

    2006-12-20

    Cannabinoid-based medicines have therapeutic potential for the treatment of pain. Augmentation of levels of endocannabinoids with inhibitors of fatty acid amide hydrolase (FAAH) is analgesic in models of acute and inflammatory pain states. The aim of this study was to determine whether local inhibition of FAAH alters nociceptive responses of spinal neurons in the spinal nerve ligation model of neuropathic pain. Electrophysiological studies were performed 14-18 d after spinal nerve ligation or sham surgery, and the effects of the FAAH inhibitor cyclohexylcarbamic acid 3-carbamoyl biphenyl-3-yl ester (URB597) on mechanically evoked responses of spinal neurons and levels of endocannabinoids were determined. Intraplantar URB597 (25 microg in 50 microl) significantly (p < 0.01) attenuated mechanically evoked responses of spinal neurons in sham-operated rats. Effects of URB597 were blocked by the cannabinoid 1 receptor (CB1) antagonist AM251 [N-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide] (30 microg in 50 microl) and the opioid receptor antagonist naloxone. URB597 treatment increased levels of anandamide, 2-arachidonyl glycerol, and oleoyl ethanolamide in the ipsilateral hindpaw of sham-operated rats. Intraplantar URB597 (25 microg in 50 microl) did not, however, alter mechanically evoked responses of spinal neurons in spinal nerve ligated (SNL) rats or hindpaw levels of endocannabinoids. Intraplantar injection of a higher dose of URB597 (100 microg in 50 microl) significantly (p < 0.05) attenuated evoked responses of spinal neurons in SNL rats but did not alter hindpaw levels of endocannabinoids. Spinal administration of URB597 attenuated evoked responses of spinal neurons and elevated levels of endocannabinoids in sham-operated and SNL rats. These data suggest that peripheral FAAH activity may be altered or that alternative pathways of metabolism have greater importance in SNL rats.

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

    Saikat Chowdhury

    2014-01-01

    Conclusion: The observed effects were comparable with the standard drug-treated group thus demonstrating effective central analgesic and acute anti-inflammatory potentials of the P. capensis leaves aqueous extract and the observations substantiate its folklore use as an analgesic and anti-inflammatory.

  4. 内吗啡肽-1的镇痛作用%Analgesic effect of endomorphin-1

    李正红; 单立冬; 蒋星红; 郭试瑜; 俞光

    2001-01-01

    AIM: To study the analgesic effect of endomorphin-1 ( EM-1 ). METHODS: The experiment was performed in rats and mice to study the analgesic effect of intraperi toneal (ip) injection of EM-1 with tail stimulation vocalization test, writhing test, adjuvant arthritis, and neuropathic pain model and to compare it with the anal gesic effects produced by intracerebroventricular (icv) and intrathecal ( it ) administrations. RESULTS: 1 ) EM-1 raised the pain threshold dose-dependently in tail stimulation-vocalization test in rats and inhibited the writhing responses induced by ip acetic acid in mice. EM-1 also decreased the hyperalgesia in both adjuvant arthritis and neuropathic pain model. 2) The analgesic effect induced by central (icv and it) administration of EM-1 was faster and more powerful than that induced by peripheral (ip) administration. 3) The analgesic effect of EM-1 was reversed by naloxone (opioid receptor an tagonist), as well as by cyprodime (μ-opioid receptor se lective antagonist). Repeated administrations of EM-1 in duced tolerance. CONCLUSION: EM-1 had a definite analgesic effect and the analgesic effect of EM-1 was me diated by central μ-opioid receptor.%目的:研究内吗啡肽-1(EM-1)的镇痛作用.方法: 采用电刺激鼠尾-嘶叫法、扭体法、佐剂性关节炎以及 神经源性疼痛等多种疼痛模型,观察腹腔注射EM-1 的镇痛作用,并和脊髓蛛网膜下腔注射和侧脑室注 射EM-1的镇痛作用进行比较.结果:1)EM-1能剂 量依赖地提高大鼠电刺激鼠尾-嘶叫法的痛阈;能抑 制醋酸引起的小鼠扭体反应;在佐剂性关节炎所致 的炎症性痛觉过敏及坐骨神经部分结扎所引起的神 经源性痛觉过敏中,EM-1也有镇痛作用. 2)中枢 给EM-1的镇痛作用比外周给药出现得较快,而且 较强.3)阿片受体拮抗剂纳洛酮能翻转EM-1的镇 痛作用;μ-阿片受体选择性拮抗剂cyprodime也能翻 转EM-1的镇痛作用;反复给予EM-1

  5. Pharmacokinetics and analgesic effects of intravenous propacetamol vs rectal paracetamol in children after major craniofacial surgery

    Prins, Sandra A.; Van Dijk, Monique; Van Leeuwen, Pim; Searle, Susan; Anderson, Brian J.; Tibboel, Dick; Mathot, Ron A. A.

    2008-01-01

    Background: The pharmacokinetics and analgesic effects of intravenous and rectal paracetamol were compared in nonventilated infants after craniofacial surgery in a double-blind placebo controlled study. Methods: During surgery all infants (6 months-2 years) received a rectal loading dose of 40 mg.kg

  6. Repeated injections of orexin-A developed behavioral tolerance to its analgesic effects in rats

    Elmira Ghasemi

    2015-12-01

    Full Text Available Objective(s:Reduction of pharmacological effectiveness or tolerance appears following repeated administration of many analgesic drugs. We investigated tolerance to anti-nociceptive effects of orexin-A, an endogenous potent analgesic peptide using the hot-plate test.Materials and Methods:Orexin-A was microinjected ICV (intracerebroventricular with an interval of 12 hr for 7 continuous days and its anti-nociceptive responses were measured on days 1, 4 and 7 using the hot-plate test following the first day of administration. Orexin-A was used at a dose of 100 pmol to induce analgesic effects. Results:ICV administration of orexin-A produced an effective anti-nociception on the first day of experiment as measured by hot-plate 5, 15, and 30 min after the injection, in comparison with both baselines (hot-plate test one day before the beginning of orexin-A administration and control, saline-administrated group. However, repeated administration of orexin-A on the following days revealed a significant reduction in this analgesic effect during day 4 to day 7. However, to rule out any associative tolerance resulting from learning related to experimental procedures and/or environmental cues, a single injection of orexin-A was administrated to animals of control group (which were receiving saline during 7 days of experiments and the analgesic effect was observed. Conclusion:These results, for the first time, indicated the appearance of tolerance to anti-nociceptive effects of orexin-A, following repeated administrations of this agent.

  7. Analgesic Effect of Indian Gooseberry (Emblica officinalis Fruit Extracts on Postoperative and Neuropathic Pain in Rats

    Dong Wook Lim

    2016-11-01

    Full Text Available Indian gooseberry (Emblica officinalis fruit, also known as “Amla” is one of the oldest edible fruits known in India. It has also traditionally been used to treat inflammation, and as an analgesic to treat wounds. However, experimental evidence for the analgesic effects of E. officinalis has been lacking. The present study investigated whether E. officinalis extracts exhibit analgesic effects in the plantar incision (PI and spared nerve injury (SNI pain-model rats. We evaluated the mechanical withdrawal threshold (MWT using von Frey filaments, and pain-related behavior was determined after surgery based on ultrasonic vocalization (USV. The group treated with E. officinalis extracts at 300 mg/kg had significantly increased MWT values at 6 h and 24 h after the PI, and had a significantly reduced number of 22–27-kHz USVs at 6 h and 24 h after PI. Moreover, after 15 days of continuous treatment with E. officinalis extracts, the treated group showed significantly alleviated SNI-induced hypersensitivity and reduced pro-inflammatory cytokine levels. Thus, E. officinalis extracts have potential analgesic effects in both postoperative and neuropathic pain models in vivo.

  8. Analgesic Effect of Indian Gooseberry (Emblica officinalis Fruit) Extracts on Postoperative and Neuropathic Pain in Rats

    Lim, Dong Wook; Kim, Jae Goo; Kim, Yun Tai

    2016-01-01

    Indian gooseberry (Emblica officinalis fruit), also known as “Amla” is one of the oldest edible fruits known in India. It has also traditionally been used to treat inflammation, and as an analgesic to treat wounds. However, experimental evidence for the analgesic effects of E. officinalis has been lacking. The present study investigated whether E. officinalis extracts exhibit analgesic effects in the plantar incision (PI) and spared nerve injury (SNI) pain-model rats. We evaluated the mechanical withdrawal threshold (MWT) using von Frey filaments, and pain-related behavior was determined after surgery based on ultrasonic vocalization (USV). The group treated with E. officinalis extracts at 300 mg/kg had significantly increased MWT values at 6 h and 24 h after the PI, and had a significantly reduced number of 22–27-kHz USVs at 6 h and 24 h after PI. Moreover, after 15 days of continuous treatment with E. officinalis extracts, the treated group showed significantly alleviated SNI-induced hypersensitivity and reduced pro-inflammatory cytokine levels. Thus, E. officinalis extracts have potential analgesic effects in both postoperative and neuropathic pain models in vivo. PMID:27898027

  9. Ibuprofen as a pre-emptive analgesic is as effective as rofecoxib for mandibular third molar surgery

    Morse, Zac; Tump, Anna; Kevelham, Ester

    2006-01-01

    The objective of this study was to compare the pre-emptive analgesic effect of rofecoxib, a cyclooxygenase (COX)-2 inhibitor, with a more traditional and commonly used analgesic, ibuprofen, for mandibular third molar surgery, utilizing a prospective, randomized, double-blind, placebo-controlled clin

  10. Analgesic Effects of Oligonol, Acupuncture and Quantum Light Therapy on Chronic Nonbacterial Prostatitis

    Akdere, Hakan; Oztekin, Ilhan; Arda, Ersan; Aktoz, Tevfik; Turan, Fatma Nesrin; Burgazli, Kamil Mehmet

    2015-01-01

    Background: Chronic Nonbacterial Prostatitis (CNBP) is a condition that frequently causes long-term pain and a significant decrease in the quality of life. Objectives: The present study aimed to examine the analgesic effects of oligonol, acupuncture, quantum light therapy and their combinations on estrogen-induced CNBP in rats. Materials and Methods: This experimental study was conducted in Edirne, Turkey, using a simple randomized allocation. A total of 90 adult male Wistar rats were randomized into 9 groups of 10 rats each: Group I, control; Group II, CNBP, Group III, oligonol only, Group IV, acupuncture only; Group V, quantum only; Group VI, oligonol + quantum; Group VII, acupuncture + oligonol; Group VIII, quantum + acupuncture; Group IX, acupuncture + quantum + oligonol. Oligonol treatment was given at a dose of 60 mg/day for 6 weeks. Conceptual vessels (CV) 3 and 4, and bilaterally urinary bladder (Bl) 32 and 34 points were targeted with 1-hour acupuncture stimulation. The quantum light therapy was applied in 5-minute sessions for 6 weeks (3-times/a week). For pain measurements, mechanical pressure was applied to a point 2 cm distal to the root of the tail to elicit pain and consequent parameters (peak force, latency time of response and total length of measurement) were assessed. Results: Analgesic effects were observed with all treatment regimens; however, the most prominent median analgesic effect was shown in the quantum light therapy in combination with acupuncture for estrogen-induced CNBP (PF1 = 663.9, PF2 = 403.4) (P = 0.012). Furthermore, we observed that monotherapy with quantum light showed a better analgesic efficacy as compared to oligonol and acupuncture monotherapies (PF1 = 1044.6, PF2 = 661.2) (P = 0.018, P = 0.008, P = 0.018; respectively). Conclusions: All treatment modalities showed a significant analgesic effect on CNBP in rats, being most prominent with the quantum light therapy. PMID:26023344

  11. The Analgesic and Antineuroinflammatory Effect of Baicalein in Cancer-Induced Bone Pain

    2015-01-01

    Cancer-induced bone pain (CIBP) is a severe type of chronic pain. It is imperative to explore safe and effective analgesic drugs for CIBP treatment. Baicalein (BE), isolated from the traditional Chinese herbal medicine Scutellaria baicalensis Georgi (or Huang Qin), has been demonstrated to have anti-inflammatory and neuroprotective effects. In this study, we examined the effect of BE on CIBP and the mechanism of this effect. Intrathecal and oral administration of BE at different doses could a...

  12. Analgesic combinations

    Raffa, Robert B.; Pergolizzi, Joseph V.; Tallarida, Ronald J.

    2010-01-01

    When the pathophysiology of a medical condition is multi-modal, i.e., related to multiple physiological causes or mediated by multiple pathways, the optimal strategy can be to use a drug or a combination of drugs that contribute multiple mechanisms to the therapeutic endpoint. In such situations, a rational multi-modal approach can also result in the fewest adverse effects. We discuss the quantitative analysis of multi-modal action using the treatment of pain as a practical example and give examples of its application to some widely used analgesic drugs. PMID:20338825

  13. Local analgesic effect of tramadol is mediated by opioid receptors in late postoperative pain after plantar incision in rats

    de Oliveira Junior, José Oswaldo; de Freitas, Milena Fernandes; Bullara de Andrade, Carolina; Chacur, Marucia; Ashmawi, Hazem Adel

    2016-01-01

    Tramadol is a drug used to treat moderate to severe pain. It is known to present a peripheral effect, but the local mechanisms underlying its actions remain unclear. The role of peripheral opioid receptors in postoperative pain is not well understood. In the present study, we examined the peripheral opioid receptors to determine the local effect of tramadol in a plantar incision pain model. Rats were subjected to plantar incision and divided into four groups on postoperative day (POD) 1: SF_SF, 0.9% NaCl injected into the right hindpaw; SF_TraI, 0.9% NaCl and tramadol injected into the right hindpaw; SF_TraC, 0.9% NaCl and tramadol injected into the contralateral hindpaw; and Nal_Tra, naloxone and tramadol injected into the ipsilateral hindpaw. To determine the animals’ nociceptive threshold, mechanical hyperalgesia was measured before incision, on POD1 before treatment and at 15, 30, 45, and 60 minutes after the incision. The same procedure was repeated on the POD2. The expression levels of μ-opioid receptor (MOR) and δ-opioid receptor (DOR) were obtained through immunoblotting assays in the lumbar dorsal root ganglia (L3–L6) in naïve rats and 1, 2, 3, and 7 days after the incision. Our results showed that the plantar incision was able to cause an increase in mechanical hyperalgesia and that tramadol reversed this hyperalgesia on POD1 and POD2. Tramadol injections in the contralateral paw did not affect the animals’ nociceptive threshold. Naloxone was able to antagonize the tramadol effect partially on POD1 and completely on POD2. The DOR expression increased on POD2, POD3, and POD7, whereas the MOR expression did not change. Together, our results show that tramadol promoted a local analgesic effect in the postoperative pain model that was antagonized by naloxone in POD2, alongside the increase of DOR expression. PMID:27799813

  14. Post-operative analgesic effects of paracetamol, NSAIDs, glucocorticoids, gabapentinoids and their combinations

    Dahl, J B; Nielsen, R V; Wetterslev, J

    2014-01-01

    , and no well-documented 'gold standards' exist. The aim of the present topical, narrative review is to provide an update of the evidence for post-operative analgesic efficacy with the most commonly used, systemic non-opioid drugs, paracetamol, non-steroidal anti-inflammatory drugs (NSAIDs)/COX-2 antagonists......, glucocorticoids, gabapentinoids, and combinations of these. The review is based on data from previous systematic reviews with meta-analyses, investigating effects of non-opioid analgesics on pain, opioid-requirements, and opioid-related adverse effects. Paracetamol, NSAIDs, COX-2 antagonists, and gabapentin....... Trials of pregabalin > 300 mg/day indicated a morphine-sparing effect of 13.4 (4, 22.8) mg morphine/24 h. Notably, though, the available evidence for additive or synergistic effects of most combination regimens was sparse or lacking. Paracetamol, NSAIDs, selective COX-2 antagonists, and gabapentin all...

  15. [Nootropic and analgesic effects of Semax following different routes of administration].

    Manchenko, D M; Glazova, N Iu; Levitskaia, N G; Andreeva, L A; Kamenskiĭ, A A; Miasoedov, N F

    2010-10-01

    Heptapeptide Semax (MEHFPGP) is the fragment of ACTH(4-10) analogue with prolonged neurotropic activity. The aim of the present work was to study the Semax effects on learning capability and pain sensitivity in white rats following intraperitoneal and intranasal administration in different doses. Semax nootropic effects were studied in the test of acquisition of passive avoidance task. Pain sensitivity was estimated in Randall-Selitto paw-withdrawal test. It was shown that Semax exerts nootropic and analgesic activities following intraperitoneal administration. Analysis of dependence of these effects on dose resulted in different dose-response curves. Following intranasal administration, Semax was more potent in learning improvement compared to intraperitoneal administration. The peptide failed to affect the animal pain sensitivity following intranasal administration as opposed to intraperitoneal administration. The data obtained suggest different mechanisms and brain structures involved in realization of the nootropic and analgesic effects of Semax.

  16. Evaluation of analgesic effect of local administration of morphine after iliac crest bone graft harvesting: A double blind study

    Devinder Singh

    2013-01-01

    Full Text Available Background and Objective: Pain is a complex process influenced by both physiological and psychological factors. In spite of an armamentarium of analgesic drugs and techniques available to combat post-operative pain, appropriate selection, and effective management for relief of post-operative pain still poses unique challenges. The discovery of peripheral opioid receptors has led to growing interest in the use of locally applied opioids (intra-articular, intra-pleural, intra-peritoneal, and perineural for managing acute pain. As bone graft harvesting is associated with significant post-operative pain and there is a paucity of literature on the use of peripheral opioids at the iliac crest bone harvesting site, the present study was planned to evaluate the analgesic efficacy of local administration of morphine after iliac crest bone graft harvesting. Materials and Methods: A total of 60 patients, 20-50 years of age scheduled to undergo elective surgery for delayed and non-union fracture both bone leg with bone grafting under general anaesthesia (GA were randomly assigned to one of the four groups of 15 patients each: group 1: 2.5 ml normal saline (NS +2.5 ml NS infiltrated into the harvest site at 2 sites + 1 ml NS intramuscularly (i/m; Group 2: 2.5 ml NS + 2.5 ml NS infiltrated into the harvest site at 2 sites + 5 mg morphine in 1 ml i/m.; Group 3: 2.5 mg (2.5 ml morphine + 2.5 mg (2.5 ml morphine infiltrated into the harvest site at 2 sites + 1 ml NS i/m; Group 4: 0.5 mg naloxone (2.5 ml +5 mg (2.5 ml morphine infiltrated into the harvest site at 2 sites + 1 ml NS i/m. Pain from the bone graft site and operative site was assessed for 24 h post-operatively. Results: The patients who had received morphine infiltration (Group 3 had significantly less pain scores at the graft site at 4, 6, and 10 post-operative hours. They also had significantly less morphine consumption and overall better pain relief as compared to the other groups. Conclusions

  17. Peripherally applied opioids for postoperative pain

    Nielsen, B N; Henneberg, S W; Schmiegelow, K;

    2015-01-01

    BACKGROUND: Opioids applied peripherally at the site of surgery may produce postoperative analgesia with few side effects. We performed this systematic review to evaluate the analgesic effect of peripherally applied opioids for acute postoperative pain. METHODS: We searched PubMed (1966 to June...... 2013), Embase (1980 to June 2013), and the Cochrane Central Register of Controlled Trials (The Cochrane Library 2013, Issue 6). Randomized controlled trials investigating the postoperative analgesic effect of peripherally applied opioids vs. systemic opioids or placebo, measured by pain intensity...... difference -5 mm, 95% CI: -7 to -3) for peripherally applied opioids vs. placebo and statistically significant increased time to first analgesic (mean difference 153 min, 95% CI: 41-265). When preoperative inflammation was reported (five studies), peripherally applied opioids significantly improved...

  18. Anti-inflammatory, analgesic and antipyretic effects of Lepidagathis anobrya Nees (Acanthaceae).

    Richard, Sawadogo Wamtinga; Marius, Lompo; Noya, Somé; Innocent Pierre, Guissou; Germaine, Nacoulma-Ouedraogo Odile

    2011-01-01

    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 and 100 mgkg(-1) for carrageenan test and doses of 0.5 mg/ear for croton oil test induced a significant reduction (p Lepidagathis anobrya and give the scientific basis for its traditional use. Further studies are needed to clarify the mechanism of action and the components responsible for these pharmacological effects.

  19. Comparable effects of exercise and analgesics for pain secondary to knee osteoarthritis

    Henriksen, Marius; Hansen, Julie B; Klokker, Louise;

    2016-01-01

    AIM: Evidence of comparative effectiveness of different treatment approaches is important for clinical decision-making, yet absent for most recommended treatments of knee osteoarthritis pain. The objective of this study was to estimate the comparative effectiveness of exercise versus orally...... pharmacology, two exercise). From these, 54 trials were eligible (20 pharmacology, 34 exercise), with 9806 participants (5627 pharmacology, 4179 exercise). The pooled effect size of pharmacological pain interventions was 0.41 (95% CI: 0.23-0.59) and for exercise 0.46 standardized mean difference (95% CI: 0...... administered analgesics for pain in patients with knee osteoarthritis. METHODS: The Cochrane Database of systematic reviews was searched for meta-analyses of randomized controlled studies comparing exercise or analgesics with a control group (placebo or usual care) and with pain as an outcome. Individual study...

  20. The Analgesic and Antineuroinflammatory Effect of Baicalein in Cancer-Induced Bone Pain

    Shan Hu

    2015-01-01

    Full Text Available Cancer-induced bone pain (CIBP is a severe type of chronic pain. It is imperative to explore safe and effective analgesic drugs for CIBP treatment. Baicalein (BE, isolated from the traditional Chinese herbal medicine Scutellaria baicalensis Georgi (or Huang Qin, has been demonstrated to have anti-inflammatory and neuroprotective effects. In this study, we examined the effect of BE on CIBP and the mechanism of this effect. Intrathecal and oral administration of BE at different doses could alleviate the mechanical allodynia in CIBP rats. Intrathecal 100 μg BE could inhibit the production of IL-6 and TNF-α in the spinal cord of CIBP rats. Moreover, intrathecal 100 μg BE could effectively inhibit the activation of p-p38 and p-JNK MAPK signals in CIBP rats. The analgesic effect of BE may be associated with the inhibition of the expression of the inflammatory cytokines IL-6 and TNF-α and through the activation of p-p38 and p-JNK MAPK signals in the spinal cord. These findings suggest that BE is a promising novel analgesic agent for CIBP.

  1. The Analgesic and Antineuroinflammatory Effect of Baicalein in Cancer-Induced Bone Pain.

    Hu, Shan; Chen, Yu; Wang, Zhi-Fu; Mao-Ying, Qi-Liang; Mi, Wen-Li; Jiang, Jian-Wei; Wu, Gen-Cheng; Wang, Yan-Qing

    2015-01-01

    Cancer-induced bone pain (CIBP) is a severe type of chronic pain. It is imperative to explore safe and effective analgesic drugs for CIBP treatment. Baicalein (BE), isolated from the traditional Chinese herbal medicine Scutellaria baicalensis Georgi (or Huang Qin), has been demonstrated to have anti-inflammatory and neuroprotective effects. In this study, we examined the effect of BE on CIBP and the mechanism of this effect. Intrathecal and oral administration of BE at different doses could alleviate the mechanical allodynia in CIBP rats. Intrathecal 100 μg BE could inhibit the production of IL-6 and TNF-α in the spinal cord of CIBP rats. Moreover, intrathecal 100 μg BE could effectively inhibit the activation of p-p38 and p-JNK MAPK signals in CIBP rats. The analgesic effect of BE may be associated with the inhibition of the expression of the inflammatory cytokines IL-6 and TNF-α and through the activation of p-p38 and p-JNK MAPK signals in the spinal cord. These findings suggest that BE is a promising novel analgesic agent for CIBP.

  2. The analgesic effect of different antidepressants combined with aspirin on thermally induced pain in Albino mice

    Abdalla S. Elhwuegi

    2012-04-01

    Full Text Available Background:Combination analgesics provide more effective pain relief for a broader spectrum of pain. This research examines the possible potentiation of the analgesic effect of different classes of antidepressants when combined with aspirin in thermal model of pain using Albino mice.Methods:Different groups of six animals each were injected intraperitoneally by different doses of aspirin (50, 100, or 200 mg/kg, imipramine (2.5, 7.5, 15 or 30 mg/kg, fluoxetine (1.25, 2.5, 5 or 7.5 mg/kg, mirtazapine (1.25, 2.5, or 5 mg/kg and a combination of a fixed dose of aspirin (100 mg/kg with the different doses of the three antidepressants. One hour later the analgesic effect of these treatments were evaluated against thermally induced pain. All data were subjected to statistical analysis using unpaired Student's t-test.Results:Aspirin had no analgesic effect in thermally induced pain. The three selected antidepressants produced dose dependent analgesia. The addition of a fixed dose of aspirin to imipramine significantly increased the reaction time (RT of the lowest dose (by 23% and the highest dose (by 20%. The addition of the fixed dose of aspirin to fluoxetine significantly increased RT by 13% of the dose 2.5 mg/Kg. Finally, the addition of the fixed dose of aspirin significantly potentiated the antinociceptive effect of the different doses of mirtazapine (RT was increased by 24, 54 and 38% respectively.Conclusion:Combination of aspirin with an antidepressant might produce better analgesia, increasing the efficacy of pain management and reduces side effects by using smaller doses of each drug.

  3. Does Acupuncture Needling Induce Analgesic Effects Comparable to Diffuse Noxious Inhibitory Controls?

    Juerg Schliessbach

    2012-01-01

    Full Text Available Diffuse noxious inhibitory control (DNIC is described as one possible mechanism of acupuncture analgesia. This study investigated the analgesic effect of acupuncture without stimulation compared to nonpenetrating sham acupuncture (NPSA and cold-pressor-induced DNIC. Forty-five subjects received each of the three interventions in a randomized order. The analgesic effect was measured using pressure algometry at the second toe before and after each of the interventions. Pressure pain detection threshold (PPDT rose from 299 kPa (SD 112 kPa to 364 kPa (SD 144, 353 kPa (SD 135, and 467 kPa (SD 168 after acupuncture, NPSA, and DNIC test, respectively. There was no statistically significant difference between acupuncture and NPSA at any time, but a significantly higher increase of PPDT in the DNIC test compared to acupuncture and NPSA. PPDT decreased after the DNIC test, whereas it remained stable after acupuncture and NPSA. Acupuncture needling at low pain stimulus intensity showed a small analgesic effect which did not significantly differ from placebo response and was significantly less than a DNIC-like effect of a painful noninvasive stimulus.

  4. Correlation of ADRB1 rs1801253 Polymorphism with Analgesic Effect of Fentanyl After Cancer Surgeries.

    Wei, Wei; Tian, Yanli; Zhao, Chunlei; Sui, Zhifu; Liu, Chang; Wang, Congmin; Yang, Rongya

    2015-01-01

    BACKGROUND Our study aimed to explore the association between β1-adrenoceptor (ADRB1) rs1801253 polymorphism and analgesic effect of fentanyl after cancer surgeries in Chinese Han populations. MATERIAL AND METHODS Postoperative fentanyl consumption of 120 patients for analgesia was recorded. Genotype distributions were detected by allele specific amplification-polymerase chain reaction (ASA-PCR) method. Postoperative pain was measured by visual analogue scale (VAS) method. Differences in postoperative VAS score and postoperative fentanyl consumption for analgesia in different genotype groups were compared by analysis of variance (ANOVA). Preoperative cold pressor-induced pain test was also performed to test the analgesic effect of fentanyl. RESULTS Frequencies of Gly/Gly, Gly/Arg, Arg/Arg genotypes were 45.0%, 38.3%, and 16.7%, respectively, and passed the Hardy-Weinberg Equilibrium (HWE) test. The mean arterial pressure (MAP) and the heart rate (HR) had no significant differences at different times. After surgery, the VAS score and fentanyl consumption in Arg/Arg group were significantly higher than in other groups at the postoperative 2nd hour, but the differences were not obvious at the 4th hour, 24th hour, and the 48th hour. The results suggest that the Arg/Arg homozygote increased susceptibility to postoperative pain. The preoperative cold pressor-induced pain test suggested that individuals with Arg/Arg genotype showed worse analgesic effect of fentanyl compared to other genotypes. CONCLUSIONS In Chinese Han populations, ADRB1 rs1801253 polymorphism might be associated with the analgesic effect of fentanyl after cancer surgery.

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

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

    2010-01-01

    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: Anesthetic 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 ...

  6. Analgesic effect of extracorporeal shock wave therapy versus ultrasound therapy in chronic tennis elbow

    2015-01-01

    [Purpose] This study compared the analgesic effects of extracorporeal shock wave therapy with those of ultrasound therapy in patients with chronic tennis elbow. [Subjects] Fifty patients with tennis elbow were randomized to receive extracorporeal shock wave therapy or ultrasound therapy. [Methods] The extracorporeal shock wave therapy group received 5 treatments once per week. Meanwhile, the ultrasound group received 10 treatments 3 times per week. Pain was assessed using the visual analogue ...

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

    You Haitao

    2011-11-01

    Full Text Available 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 compounds on transient expressed human T-type calcium channels were examined in tsA-201 cells using standard whole-cell voltage clamp techniques, and their analgesic effects in response to various administration routes (intrathecally, intraplantarly, intraperitoneally assessed in the formalin model. A series of compounds were synthesized and evaluated for channel and receptor activity. Compound NMP-7 acted as non-selective CB1/CB2 agonist while NMP4 was found to be a CB1 partial agonist and CB2 inverse agonist. Furthermore, NMP-144 behaved as a selective CB2 inverse agonist. All of these three compounds completely inhibited peak Cav3.2 currents with IC50 values in the low micromolar range. All compounds mediated analgesic effects in the formalin model, but depending on the route of administration, could differentially affect phase 1 and phase 2 of the formalin response. Conclusions Our results reveal that a set of novel cannabinioid receptor ligands potently inhibit T-type calcium channels and show analgesic effects in vivo. Our findings suggest possible novel means of mediating pain relief through mixed T-type/cannabinoid receptor ligands.

  8. The cumulative analgesic effect of repeated electroacupuncture involves synaptic remodeling in the hippocampal CA3 region

    Qiuling Xu; Tao Liu; Shuping Chen; Yonghui Gao; Junying Wang; Lina Qiao; Junling Liu

    2012-01-01

    In the present study, we examined the analgesic effect of repeated electroacupuncture at bilateral Zusanli (ST36) and Yanglingquan (GB34) once a day for 14 consecutive days in a rat model of chronic sciatic nerve constriction injury-induced neuropathic pain. In addition, concomitant changes in calcium/calmodulin-dependent protein kinase II expression and synaptic ultrastructure of neurons in the hippocampal CA3 region were examined. The thermal pain threshold (paw withdrawal latency) was increased significantly in both groups at 2 weeks after electroacupuncture intervention compared with 2 days of electroacupuncture. In ovariectomized rats with chronic constriction injury, the analgesic effect was significantly reduced. Electroacupuncture for 2 weeks significantly diminished the injury-induced increase in synaptic cleft width and thinning of the postsynaptic density, and it significantly suppressed the down-regulation of intracellular calcium/ calmodulin-dependent protein kinase II expression in the hippocampal CA3 region. Repeated electroacupuncture intervention had a cumulative analgesic effect on injury-induced neuropathic pain reactions, and it led to synaptic remodeling of hippocampal neurons and upregulated calcium/calmodulin-dependent protein kinase II expression in the hippocampal CA3 region.

  9. Analgesic effect of fendosal, ibuprofen and aspirin in postoperative oral surgery pain.

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

    1984-01-01

    The analgesic efficacy of a single 200-mg dose of fendosal, a nonnarcotic, nonsteroidal antiinflammatory analgesic, was compared, in a double-blind study, with aspirin 650 mg, ibuprofen 400 mg and placebo in outpatients who had moderate or severe pain after the surgical removal of impacted third molars. Using a self-rating record, patients rated their pain and its relief hourly for up to 12 hours after medicating. Each active medication was significantly superior to placebo. The peak analgesic effect of fendosal 200 mg was similar to that of the aspirin 650-mg standard. Although fendosal's onset of action was slow (3 hours), its effect persisted for 8 hours, substantially longer than that of aspirin. Ibuprofen 400 mg was statistically significantly superior to aspirin 650 mg and fendosal 200 mg for most measures of peak and total analgesia, and its effect persisted for 8 hours. The results of this study raise some questions concerning the comparability of data from studies that employ different criteria for remedication and/or different criteria for the inclusion of data in the analyses of efficacy.

  10. [Devil's claw extract as an example of the effectiveness of herbal analgesics].

    Chrubasik, S

    2004-07-01

    Preparations from devil's claw differ in their content of active ingredients as assessed by the quantity of harpagoside present. The harpagoside content in the daily dose of Doloteffin (extraction solvent water) is double that of preparations extracted with 60% ethanol. Only preparations with proven effectiveness for painful lower back or arthrotic pain are an attractive alternative to synthetic analgesics, and are of substantial benefit in the treatment of chronic pain. From an evidence based view, extract with at least 50 mg harpagoside in the daily dose should be recommended for the treatment of pain. Treatment with devil's claw extract is associated with a lower risk of adverse events than treatment with synthetic analgesics, and may contribute in the majority of patients to the relief of pain.

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

    Tozzini Danila

    2008-11-01

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

  12. [Analgesic nephropathy].

    Pintér, I; Nagy, J

    1998-11-22

    Analgesic nephropathy is a slowly progressive disease caused by the chronic abuse of analgesic mixtures containing two analgesic components combined with potentially addictive substances (coffeine and/or codeine). Pathologically, the nephropathy is characterized by renal papillary necrosis with calcification and chronic interstitial nephritis sometimes in association with transitional-cell carcinoma of the uroepithelium. In the early stage, the clinical characteristics are polyuria, sterile pyuria, sometimes renal colic and haematuria. With further progression of the disease, there are the nonspecific symptoms of advanced renal failure. The incidence of classic analgesic nephropathy among Hungarian patients on chronic renal replacement therapy has proven. There is an urgent need for the estimation of analgesic nephropathy among patients with chronic renal disease and among patients with chronic pain presumably regularly taking analgesics in Hungary. As long as analgesic mixtures containing phenacetin or paracetamol and/or nonsteroidal antiinflammatory drugs and addictive substances are available "over-the-counter", analgesic nephropathy will continue to be a problem also in our country.

  13. Investigation of centrally and peripherally acting analgesic and anti inflammatory activity of biological immune response modulator (an Amazonian plant extract in animal models of pain and inflammation

    Mital Ravalji

    2015-04-01

    Conclusion: Our study results show that BIRM has the potential anti-inflammatory property and is able to exert its anti-nociceptive effect through both central and peripheral mechanisms. [Int J Basic Clin Pharmacol 2015; 4(2.000: 342-348

  14. Effects of lidocaine and esmolol infusions on hemodynamic changes, analgesic requirement, and recovery in laparoscopic cholecystectomy operations

    Serpil Dagdelen Dogan; Faik Emre Ustun; Elif Bengi Sener; Ersin Koksal; Yasemin Burcu Ustun; Cengiz Kaya; Fatih Ozkan

    2016-01-01

    ABSTRACT OBJECTIVE: We compared the effects of lidocaine and esmolol infusions on intraoperative hemodynamic changes, intraoperative and postoperative analgesic requirements, and recovery in laparoscopic cholecystectomy surgery. METHODS: The first group (n = 30) received IV lidocaine infusions at a rate of 1.5 mg/kg/min and the second group (n = 30) received IV esmolol infusions at a rate of 1 mg/kg/min. Hemodynamic changes, intraoperative and postoperative analgesic requirements, and rec...

  15. Spider peptide Phα1β induces analgesic effect in a model of cancer pain.

    Rigo, Flavia Karine; Trevisan, Gabriela; Rosa, Fernanda; Dalmolin, Gerusa D; Otuki, Michel Fleith; Cueto, Ana Paula; de Castro Junior, Célio José; Romano-Silva, Marco Aurelio; Cordeiro, Marta do N; Richardson, Michael; Ferreira, Juliano; Gomez, Marcus V

    2013-09-01

    The marine snail peptide ziconotide (ω-conotoxin MVIIA) is used as an analgesic in cancer patients refractory to opioids, but may induce severe adverse effects. Animal venoms represent a rich source of novel drugs, so we investigated the analgesic effects and the side-effects of spider peptide Phα1β in a model of cancer pain in mice with or without tolerance to morphine analgesia. Cancer pain was induced by the inoculation of melanoma B16-F10 cells into the hind paw of C57BL/6 mice. After 14 days, painful hypersensitivity was detected and Phα1β or ω-conotoxin MVIIA (10-100 pmol/site) was intrathecally injected to evaluate the development of antinociception and side-effects in control and morphine-tolerant mice. The treatment with Phα1β or ω-conotoxin MVIIA fully reversed cancer-related painful hypersensitivity, with long-lasting results, at effective doses 50% of 48 (32-72) or 33 (21-53) pmol/site, respectively. Phα1β produced only mild adverse effects, whereas ω-conotoxin MVIIA induced dose-related side-effects in mice at analgesic doses (estimated toxic dose 50% of 30 pmol/site). In addition, we observed that Phα1β was capable of controlling cancer-related pain even in mice tolerant to morphine antinociception (100% of inhibition) and was able to partially restore morphine analgesia in such animals (56 ± 5% of inhibition). In this study, Phα1β was as efficacious as ω-conotoxin MVIIA in inducing analgesia in a model of cancer pain without producing severe adverse effects or losing efficacy in opioid-tolerant mice, indicating that Phα1β has a good profile for the treatment of cancer pain in patients.

  16. Intravenous flurbiprofen axetil can increase analgesic effect in refractory cancer pain

    Hao Jiqing

    2009-03-01

    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.

  17. Intravenous flurbiprofen axetil can increase analgesic effect in refractory cancer pain

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

    2009-01-01

    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. PMID:19267934

  18. The Role of Spinal Dopaminergic Transmission in the Analgesic Effect of Nefopam on Rat Inflammatory Pain

    Kim, Do Yun; Chae, Joo Wung; Lim, Chang Hun; Heo, Bong Ha; Park, Keun Suk; Lee, Hyung Gon; Choi, Jeong Il; Yoon, Myung Ha

    2016-01-01

    Background Nefopam has been known as an inhibitor of the reuptake of monoamines, and the noradrenergic and/or serotonergic system has been focused on as a mechanism of its analgesic action. Here we investigated the role of the spinal dopaminergic neurotransmission in the antinociceptive effect of nefopam administered intravenously or intrathecally. Methods The effects of intravenously and intrathecally administered nefopam were examined using the rat formalin test. Then we performed a microdialysis study to confirm the change of extracellular dopamine concentration in the spinal dorsal horn by nefopam. To determine whether the changes of dopamine level are associated with the nefopam analgesia, its mechanism was investigated pharmacologically via pretreatment with sulpiride, a dopaminergic D2 receptor antagonist. Results When nefopam was administered intravenously the flinching responses in phase I of the formalin test were decreased, but not those in phase II of the formalin test were decreased. Intrathecally injected nefopam reduced the flinching responses in both phases of the formalin test in a dose dependent manner. Microdialysis study revealed a significant increase of the level of dopamine in the spinal cord by intrathecally administered nefopam (about 3.8 fold the baseline value) but not by that administered intravenously. The analgesic effects of intrathecally injected nefopam were not affected by pretreatment with sulpiride, and neither were those of the intravenous nefopam. Conclusions Both the intravenously and intrathecally administered nefopam effectively relieved inflammatory pain in rats. Nefopam may act as an inhibitor of dopamine reuptake when delivered into the spinal cord. However, the analgesic mechanism of nefopam may not involve the dopaminergic transmission at the spinal level. PMID:27413481

  19. Analgesic and antiinflammatory activities of an extract from Parkia biglobosa used in traditional medicine in the Ivory Coast.

    Kouadio, F; Kanko, C; Juge, M; Grimaud, N; Jean, A; N'Guessan, Y T; Petit, J Y

    2000-12-01

    In the Ivory coast, Parkia biglobosa (Mimosaceae) is used in traditional medicine as an analgesic drug, especially against dental pain. Of the three extracts obtained from the plant bark, the hexane fraction was studied to determine its analgesic and/or antiinflammatory activities. The results show that this extract possesses a marked analgesic activity when evaluated with the abdominal writhing test in mice, but, like paracetamol, was ineffective with the hot-plate method, a feature suggesting a peripheral mechanism of action. This activity was accompanied by an antiinflammatory effect, somewhat weaker than the analgesic one.

  20. Analgesic effect of coconut shell (Cocos nucifera L liquid smoke on mice

    Meircurius Dwi C.S

    2012-09-01

    Full Text Available Background: Drugs can be used to eliminate pain by inhibiting the activity of conversing arachidonic acid into prostaglandin. The chemical compositions of coconut shell are cellulose, pentosan, lignin, solvent extraction, uronat anhydrous, nitrogen, and water. One active ingredient in coconut shell is phenyl propanoid (consisting in lignin structure and guaicol. Phenyl propanoid and guaicol are phenolic compounds that can be used as antioxidant, antiseptic, anti-inflammatory, anesthetic and analgesic. Liquid smoke of coconut shell (Cocos nucifera L contains phenolic compound is believed able to bind a component conversing arachidonic acid into prostaglandin. Purpose: The study was aimed to examine the analgesic effect of liquid smoke of coconut shell (Cocos nucifera L. Methods: The study was a laboratory experimental research, conducted on 2-3 months old male mice (Mus musculus with 20-30 grams of weight. There were control group and treatment groups each of which had seven mice. Control group was orally given 0.01 ml/weight (ml/gr of distilled water, after 30 minutes 0.01 ml/weight (ml/gr of acetic acid 0.6% was delivered via intraperitoneal injection. The treatment groups were given liquid smoke of coconut shell (Cocos nucifera L with the concentrations of 25%, 50%, and 100% respectively. The analgesic effect was then determined by decreasing of writhing reflex on mice recorded every 5 minutes for 30 minutes. Results: There were significant differences of writhing reflexes in the treatment groups given liquid smoke of coconut shell with the concentrations of 25%, 50%, and 100%. The higher concentration of liquid smoke the higher its analgesic effect. Conclusion: Liquid smoke of coconut shell (Cocos nucifera L has analgesic effect.Latar belakang: Salah satu mekanisme obat yang digunakan untuk menghilangkan rasa nyeri adalah menghambat aktivitas konversi asam arakhidonat menjadi prostaglandin. Komposisi kimia tempurung kelapa terdiri dari

  1. Paroxetine engenders analgesic effects through inhibition of p38 phosphorylation in a rat migraine model

    Chuanming Wang; Wei Bi; Yanran Liang; Xiuna Jing; Songhua Xiao; Yannan Fang; Qiaoyun Shi; Enxiang Tao

    2012-01-01

    In this study, a model of migraine was established by electrical stimulation of the superior sagittal sinus in rats. These rats were then treated orally with paroxetine at doses of 2.5, 5, or 10 mg/kg per day for 14 days. Following treatment, mechanical withdrawal thresholds were significantly higher, extracellular concentrations of 5-hydroxytryptamine in the periaqueductal grey matter and nucleus reticularis gigantocellularis were higher, and the expression of phosphorylated p38 in the trigeminal nucleus caudalis was lower. Our experimental findings suggest that paroxetine has analgesic effects in a rat migraine model, which are mediated by inhibition of p38 phosphorylation.

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

    Yamamoto, Tatsuo; Miyazaki, Rika; Yamada, Toshihiko

    2009-09-01

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

  3. Renal function in a rat model of analgesic nephropathy: effect of chloroquine.

    Ahmed, Mohamed H; Ashton, Nick; Balment, Richard J

    2003-04-01

    The antimalaria drug chloroquine is often taken against a background of analgesic nephropathy caused by nonsteroidal anti-inflammatory drugs such as paracetamol (acetaminophen). Chloroquine has marked effects on the normal kidney and stimulates an increase in plasma vasopressin via nitric oxide. The aim of this study was to determine the renal action of chloroquine in a model of analgesic nephropathy. Sprague-Dawley rats (n = 6-8/group) were treated with paracetamol (500 mg kg(-1) day(-1)) for 30 days in drinking water to induce analgesic nephropathy; control rats received normal tap water. Under intraval anesthesia (100 mg kg(-1)) rats were infused with 2.5% dextrose for 3 h to equilibrate and after a control hour they received either vehicle, chloroquine (0.04 mg h(-1)), N(omega)-nitro-L-arginine methyl ester (L-NAME, nitric-oxide synthase inhibitor, 60 micro g kg(-1) h(-1)) or combined chloroquine and L-NAME over the next hour. Plasma was collected from a parallel group of animals for vasopressin radioimmunoassay. Long-term paracetamol treatment resulted in a decrease in glomerular filtration rate (p < 0.05), sodium excretion (p < 0.001), and urine osmolality (p < 0.001), but no change in urine flow rate compared with untreated animals. Chloroquine administration in paracetamol treated rats induced a significant reduction (p < 0.05) in urine flow rate and a significant increase in plasma vasopressin (p < 0.001). These effects were blocked by coadministration of L-NAME and thus seem to be mediated by a pathway involving nitric oxide. However, these responses contrast with the chloroquine-induced diuresis previously observed in untreated rats, possibly reflecting paracetamol inhibition of renal prostaglandin synthesis and consequent moderation of vasopressin's action.

  4. COMPARISON OF ANALGESIC EFFECT OF INTRA-ARTICULAR BUPRENORPHINE AND MORPHINE FOLLOWING ARTHROSCOPIC SURGERY OF KNEE

    Shashidhar Gowdra Sugandarajappa

    2016-07-01

    Full Text Available BACKGROUND AND AIMS Pain after orthopaedic surgery depends on the site and extent of surgery and the preoperative use of analgesics by the patient. Arthroscopic procedures are routinely performed on outpatient basis and have spared patients large incisions and decreased morbidity compared with open incisions, but has not eliminated pain. At present several techniques are available to treat pain following arthroscopic surgeries; these include the use of opioids, local anaesthetics, NSAIDs, corticosteroids, clonidine and cryotherapy. Here, we compared the analgesic effect of intra-articular administration of morphine, buprenorphine and placebo following arthroscopic surgery of knee. METHODS A prospective, randomised, placebo-controlled double-blind comparative study conducted in 60 patients of either sex who underwent arthroscopic surgery of knee; between the age group of 18 and 65 years and of ASA class I and II physical status were included in the study. Patients were randomly assigned equally to one of the 3 groups of 20 each by a sealed envelope method. The groups were Group A - Patients receiving IA Buprenorphine 100 mcg in 20 mL normal saline. Group B - Patients receiving IA Morphine 3 mg in 20 mL normal saline. Group C - Patients receiving IA 20 mL normal saline as placebo. Parameters monitored were degree of analgesia along with haemodynamic parameters and side effects. Data were analysed using student’s t-test for continuous variables and Chi-Square test. RESULTS We found that 100 mcg buprenorphine when injected intra-articularly produced good and comparable postoperative pain control and reduced supplementary analgesic requirement when compared to other groups. CONCLUSION In summary, this study demonstrated that for eight hours postoperatively 100 mcg buprenorphine provided superior postoperative analgesia to that of 3 mg morphine

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

    Schulteis Gery

    2008-05-01

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

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

    Mohammad M. Hassan

    2013-04-01

    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

  7. The Analgesic Effect of the Mitochondria-Targeted Antioxidant SkQ1 in Pancreatic Inflammation

    Maximilian Weniger

    2016-01-01

    Full Text Available Background. Chronic pancreatitis is one of the main risk factors for pancreatic cancer. In acute and chronic pancreatitis, oxidative stress is thought to play a key role. In this respect, the recently described mitochondria-targeted antioxidant SkQ1 effectively scavenges reactive oxygen species at nanomolar concentrations. Therefore, we aimed to characterize the influence of SkQ1 on tissue injury and pain in acute and chronic pancreatitis. Methods. Both acute and chronic pancreatitis were induced in C57BL/6 mice by intraperitoneal cerulein injections and treatment with SkQ1 was carried out by peroral applications. Hyperalgesia was assessed by behavioral observation and measurement of abdominal mechanical sensitivity. Blood serum and pancreatic tissue were harvested for analysis of lipase and histology. Results. SkQ1 did not influence pain, serological, or histological parameters of tissue injury in acute pancreatitis. In chronic pancreatitis, a highly significant reduction of pain-related behavior (p<0.0001 was evident, but histological grading revealed increased tissue injury in SkQ1-treated animals (p=0.03. Conclusion. After SkQ1 treatment, tissue injury is not ameliorated in acute pancreatitis and increased in chronic pancreatitis. However, we show an analgesic effect in chronic pancreatitis. Further studies will need to elucidate the risks and benefits of mitochondria-targeted antioxidants as an analgesic.

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

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

    2014-05-01

    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) 3.3004μg/ml. Insecticidal activity was positive against Callosbruchus analis, the percent mortality was 40%.

  9. Analgesic effect of transcranial direct current stimulation on central post-stroke pain.

    Bae, Sea-Hyun; Kim, Gi-Do; Kim, Kyung-Yoon

    2014-01-01

    Pain that occurs after a stroke lowers the quality of life. Such post-stroke pain is caused in part by the brain lesion itself, called central post-stroke pain. We investigated the analgesic effects of transcranial direct current stimulation (tDCS) in stroke patients through quantitative sensory testing. Fourteen participants with central post-stroke pain (7 female and 7 male subjects) were recruited and were allocated to either tDCS (n = 7) or sham-tDCS (n = 7) group. Their ages ranged from 45 to 55 years. tDCS was administered for 20 min at a 2-mA current intensity, with anodal stimulations were performed at primary motor cortex. The sham-tDCS group was stimulated 30-second current carrying time. Both group interventions were given for 3 days per week, for a period of 3 weeks. Subjective pain was measured using the visual analogue scale (VAS) of 0 to 10. Sensations of cold and warmth, and pain from cold and heat were quantified to examine analgesic effects. The sham-tDCS group showed no statistically significant differences in time. In contrast, tDCS group showed decreased VAS scores and skin temperature (p pain from cold increased (p pain from heat decreased (p central post-stroke pain.

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

    Dong Wook Lim

    2014-01-01

    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.

  11. Enhanced analgesic effect of morphine-nimodipine combination after intraspinal administration as compared to systemic administration in mice

    Dilip Verma; Subrata Basu Ray; Ishan Patro; Shashi Wadhwa

    2005-09-01

    Calcium plays an important role in the pathophysiology of pain. A number of studies have investigated the effect of L-type calcium channel blockers on the analgesic response of morphine. However, the results are conflicting. In the present study, the antinociceptive effect of morphine (2.5 g) and nimodipine (1 g) co-administered intraspinally in mice was observed using the tail flick test. It was compared to the analgesic effect of these drugs (morphine – 250 g subcutaneously; nimodipine – 100 g intraperitoneally) after systemic administration. Nimodipine is highly lipophilic and readily crosses the blood brain barrier. Addition of nimodipine to morphine potentiated the analgesic response of the latter when administered through the intraspinal route but not when administered through systemic route. It may be due to direct inhibitory effect of morphine and nimodipine on neurons of superficial laminae of the spinal cord after binding to -opioid receptors and L-type calcium channels respectively.

  12. Investigation of Peripheral Effects of Citrus Limon Essential Oil on Somatic Pain in Male Wistar Rats: Role of Histaminergic System

    Ali Mojtahedin

    2016-12-01

    Full Text Available Background & Objective: One of the plants used in traditional medicine is lemon which has analgesic effect. However, little research has been performed on the analgesic effect of lemon and mechanisms of action with an emphasis on neurotransmitters systems. Therefore, the present study set to investigate the peripheral effects of lemon essential oil on somatic pain using formalin test with an emphasis on histaminergic system in male Wistar rats. Materiala & Methods: Sixty male rats weighing approximately 200-250g and aged 14-16 wk were divided into 10 groups: sham (Salin + Formalin 1% intraplantar, three treatment groups with lemon essential oil (EO (12.5, 25 and 50 mg/kg, three treatment groups with Chlorpheniramine (5, 10 and 20 mg/kg, 1 treatment group with Histamine (10 mg/kg, 1 pretreatment group with Chlorpheniramine (20 mg/kg + EO (50mg/kg, and 1 pretreatment group with Histamine (10 mg/kg + EO (50 mg/kg. Formalin test was used to assess somatic pain. Data analysis was performed using one-way ANOVA. Results:  Intraperitoneal injection of lemon essential oil reduced the pain response induced by formalin in both phases (P<0.05. Pretreatment with chlorpheniramine and lemon essential oil enhanced the analgesic response in both phases (P<0.05. Conclusion: Lemon essential oil had analgesic effects, probably caused by the histaminergic system.

  13. Role of serotonin in pathogenesis of analgesic induced headache

    Srikiatkhachorn, A.

    1999-12-16

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

  14. Side effects can enhance treatment response through expectancy effects: an experimental analgesic randomized controlled trial.

    Berna, Chantal; Kirsch, Irving; Zion, Sean R; Lee, Yvonne C; Jensen, Karin B; Sadler, Pamela; Kaptchuk, Ted J; Edwards, Robert R

    2017-02-04

    In randomized controlled trials, medication side effects may lead to beliefs that one is receiving the active intervention and enhance active treatment responses, thereby increasing drug-placebo differences. We tested these hypotheses with an experimental double-blind randomized controlled trial of a nonsteroidal anti-inflammatory drug with and without the addition of atropine to induce side effects. One hundred healthy volunteers were told they would be randomized to either combined analgesics that might produce dry mouth or inert placebos. In reality, they were randomized double blind, double-dummy to 1 of the 4 conditions: (1) 100 mg diclofenac + 1.2 mg atropine, (2) placebo + 1.2 mg atropine, (3) 100 mg diclofenac + placebo, or (4) placebo + placebo, and tested with heat-induced pain. Groups did not differ significantly in demographics, temperature producing moderate pain, state anxiety, or depression. Analgesia was observed in all groups; there was a significant interaction between diclofenac and atropine, without main effects. Diclofenac alone was not better than double-placebo. The addition of atropine increased pain relief more than 3-fold among participants given diclofenac (d = 0.77), but did not enhance the response to placebo (d = 0.09). A chain of mediation analysis demonstrated that the addition of atropine increased dry mouth symptoms, which increased beliefs that one had received the active medication, which, in turn, increased analgesia. In addition to this indirect effect of atropine on analgesia (via dry mouth and beliefs), analyses suggest that among those who received diclofenac, atropine directly increased analgesia. This possible synergistic effect between diclofenac and atropine might warrant future research.

  15. PHARMACOLOGICAL SCREENING OF ISOLATED COMPOUND FROM MADHUKA LONGIFOLIA SEEDS GIVES SIGNIFICANT ANALGESIC EFFECT

    Chirantan S. Chakma

    2011-08-01

    Full Text Available The study was carried out to assess the analgesic effect of aqueous and ethanolic extracts of isolated compound from M.longifolia seeds in rats and mice model. All three animal groups were administered the aq. and alc.ext of M.longifolia at a dose of 4 mg to 64 mg/kg body weight. The standard drug diclofenac 5 mg/kg b.w is used in three screening method. The paw licking time, tail withdrawal time and chemical writhings in mice both aq. and alc. extracts of M.longifolia prevents significant dose dependent anti-nociceptive effect. Diclofenac 5 mg/kg failed to alter significantly the antinociceptive effect of 16 to 32 mg of both extracts or the effect on chemical assay.

  16. Superior analgesic effect of an active distraction versus pleasant unfamiliar sounds and music

    Garza Villarreal, Eduardo A.; Brattico, Elvira; Vase, Lene

    2012-01-01

    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......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...

  17. Effect of gender on pain perception and analgesic consumption in laparoscopic cholecystectomy: An observational study

    Aziza M Hussain

    2013-01-01

    Full Text Available Background: Evidence regarding gender affecting the response to pain and its treatment is inconsistent in literature. The objective of this prospective, observational study was to determine the effect of gender on pain perception and postoperative analgesic consumption in patients undergoing laparoscopic cholecystectomy. Materials and Methods: We recruited 60 male and 60 female patients undergoing elective laparoscopic cholecystectomy. Patients were observed for additional intraoperative and postoperative analgesia. Numerical rating scale was documented at 10 min interval for 1 h in post-anesthesia recovery room and at 4, 8, and 12 h postoperatively. Boluses of tramadol given as rescue analgesia were also noted. There were no dropouts. Results: The mean pain scores were significantly higher in female patients at 20 and 30 min following surgery. Mean dose of tramadol consumption was significantly higher in female patients for the first postoperative hour (P = 0.002, but not in the later period. Conclusion: Female patients exhibited greater intensity of pain and required higher doses of analgesics compared to males in in the immediate postoperative period in order to achieve a similar degree of analgesia.

  18. Peripheral nerve extract effects on mesenchymal cells.

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

    1996-01-01

    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 regulation of growth, we developed an in vitro assay to assess the effect of fractions of peripheral nerve on myoblast and chondroblast growth and differentiation in a mammalian (rat) system. Whole rat sciatic nerve extract was fractionated by ammonium sulfate precipitation and by affinity chromatography. Concavalin A chromatography resolved whole nerve extract into a glycoprotein and a non-glycoprotein fraction. Serial ammonium sulfate precipitation yielded three pellet fractions designated as 35%, 70%, and 100% pellets; corresponding to ammonium sulfate concentrations of 0 to 35%, 35 to 70%, and 70 to 100% saturation, respectively. Dialyzed solutions of these pellets as well as the fractions from Concavalin A chromatography were assayed for biological activity in micromass cultures of rat limb bud mesenchyme, which allowed assessment of both myoblast and chondroblast stimulation. Stimulation of protein synthesis and myoblast proliferation (as measured by MF20 staining) occurred with both 70% and 100% ammonium sulfate fractions. Stimulation of chondroblasts (as measured by the number of alcian blue staining nodules) occurred with the 35% and 100% fractions. The glycoprotein fraction from the affinity chromatography stimulated protein synthesis and myoblast proliferation and inhibited chondroblast development. Stimulation of chondroblasts was seen with the non-glycoprotein fraction. No effect on protein synthesis, myoblast proliferation or chondroblast proliferation was found in

  19. Evaluation of Analgesic Effect of Caudal Epidural Tramadol, Tramadol-Lidocaine, and Lidocaine in Water Buffalo Calves (Bubalus bubalis)

    Ayman Atiba; Alaa Ghazy; Naglaa Gomaa; Tarek Kamal; Mustafa Shukry

    2015-01-01

    Aim of this study was to compare the analgesic effect of tramadol and a combination of tramadol-lidocaine with that produced by lidocaine administration in the epidural space in buffalo calves. In a prospective randomized crossover study, ten male buffalo calves were used to compare the epidural analgesic effect of tramadol (1 mg/kg) and tramadol-lidocaine combination (0.5 mg/kg and 0.11 mg/kg, resp.) with that produced by 2% lidocaine (0.22 mg/kg). Loss of sensation was examined by pin-prick...

  20. Analgesic effects of adding lidocaine to morphine pumps after orthopedic surgeries

    Mahmoud Reza Alebouyeh

    2014-01-01

    Full Text Available Background: Opiate is used in patient-controlled intravenous analgesia pumps (PCIA for controlling pain in post-surgical patients. Other drugs are remarkably added to opioid pumps to enhance quality, lengthen analgesia, and reduce side effects. Lidocaine, a local anesthetic which inhibits sodium channels, has anesthetic and analgesic effects when injected locally or intravenously. The objective of this study is to evaluate the analgesic effects of adding lidocaine 1% to different doses of morphine via IV pump to patient-controlled analgesia (PCA after orthopedic surgeries. Materials and Methods: In a randomized clinical trial, 60 patients who had undergone orthopedic surgery of lower extremities were divided into three equal groups to control postoperative pain. Intravenous pump with 5 ml/h flow rate was used as the analgesic method. The solution consisted of lidocaine 1% plus 20 mg morphine for the first group, lidocaine 1% plus 10 mg morphine for the second group, and only 20 mg morphine for the third group (control group. Patients were checked every 12 h, and Visual Analog Scale (VAS, extra opioid doses, nausea/vomiting, and sedation scale were examined. Results: Pain score was lower in the first group compared to the other two groups. Mean VAS was 2.15 ± 0.2, 2.75 ± 0.2, and 2 ± 0.25 on the first day and 1.88 ± 0.1, 2.74 ± 0.3, and 2.40 ± 0.3 on the second day, respectively, in the three groups and the difference was statistically significant (P < 0.01 and <0.05, respectively. Also, 10% of patients in the first group needed extra opioid doses, while this figure was 30% in the second group and 25% in the third group (P < 0.01. Nausea/vomiting and sedation scores were not statistically different among the three groups. Conclusion: Compared to lidocaine 1% plus 10 mg morphine or 20 mg morphine alone in PCIA, adding lidocaine 1% to 20 mg morphine decreases the pain score and opioid dose after orthopedic surgeries without having side

  1. Low-dose spinal neostigmine further enhances the analgesic effect of spinal bupivacaine combined with epidural dexamethasone, following orthopedic surgery

    Gabriela Rocha Lauretti

    2014-01-01

    Full Text Available Background: Opioids are considered mainstream for combined spinal-epidural anesthesia, but frequently limited by adverse effects. The aim of this study was to examine whether low-dose spinal neostigmine, epidural dexamethasone or their combination enhances analgesia from spinal bupivacaine without adverse effects. Materials and Methods : A total of 60 patients undergoing orthopedic surgery were randomized to one of four groups and evaluated for 24-h after surgery for analgesia (time to first rescue analgesic and rescue analgesic consumption. Patients received 15 mg bupivacaine plus the test drug intrathecally (saline or 1 microgram (μg neostigmine. The epidural test drug was either saline or 10 mg dexamethasone. The Control group (CG received spinal and epidural saline. The Neostigmine group (NG, spinal neostigmine and epidural saline; the Dexamethasone group (DG, spinal saline and epidural dexamethasone; and the Neostigmine-dexamethasone group (NDG, spinal neostigmine and epidural dexamethasone. Results: The CG (282 ± 163 min and NG (524 ± 142 min were similar in their times to first rescue analgesic and analgesic consumption. The time to first rescue analgesic was longer for the DG (966 ± 397 min compared with CG and NG (P < 0.0002, and the DG had less ketoprofen consumption and lower overall visual analogue scale-pain sores compared with CG and NG (P < 0.0005. Addition of 1 mg-neostigmine (NDG resulted in longer time to rescue analgesic (1205 ± 303 min; P < 0.02 and lower ketoprofen consumption (P < 0.05 compared to DG. Sporadic cases of vesical catheterization and emesis were observed, however adverse effects were similar among groups. Conclusion: Spinal 1 microgram (μg neostigmine further enhanced analgesia from spinal bupivacaine combined with epidural dexamethasone, without increasing the incidence of adverse effects.

  2. MECHANISM OF ANALGESIC EFFECTS OF PROPOFOL ON INCISIONAL PAIN: A RAT MODEL STUDY

    HUANG Zhi-hua; SONG Xiao-xing; HU Jiong; YU Bu-wei

    2009-01-01

    Objective To clarify the role of propofol in controlling incisional pain and its potential effects on the spinal opioid receptor expression.Methods A postoperative model of nociception was established in male Sprague-Dawley rats weighing 200-250 g. A total of 96 rats were randomly divided into 8 groups. All drugs were administered intravenously either 5min pre-operation or 5min post-operation. The analgesic effects of systemic propofol were demonstrated by the measurement of a cumulative pain score (CPS). After that, the lumbar enlargement of the spinal cord was removed to evaluate the mRNA level of the μ-opioid receptor (MOR) and δ-opioid receptor (DOR) by RT-PCR.Results CPS and DOR mRNA expressions significantly increased after the operation. Both propofol post-treatment and propofol pre-treatment groups showed significant suppression of the increased CPS and the expression of DOR mRNA evoked by pain stimulation. Interestingly, propofol pre-treatment had a more pronounced effect in decreasing CPS and the expression of DOR mRNA. Furthermore, these observations were dose-dependent. MOR mRNA expression significantly increased after operation in all animals and propofol treatment had no impact on it.Conclusion Based on these findings, we suggest that propofol can serve as a valuable adjunct in acute postoperative pain management. Systemic propofol induces an analgesic effect on acute incisional pain in a dose-dependant manner, and this effect is mediated in the spinal cord and may be associated with the spinal DOR.

  3. INTRATHECAL MIDAZOLAM PROLONGS THE ANALGESIC EFFECTS OF SPINAL BLOCKADE WITH LIDOCAINE FOR PERINEAL OPERATION

    B. Jahangiri R. Jahangiri

    2006-09-01

    Full Text Available Intrathecal administration of midazolam has been reported to have antinociceptive action, and to be an effective analgesic agent. In this prospective double-blind study we aimed to evaluate the postoperative effects of intrathecal midazolam with lidocaine following perineal operation. Forty patients were randomly allocated to two groups: 20 patients in the control group received 2 ml of 5% heavy lidocaine plus 0.4 ml of 0.9% saline intrathecally; 20 patients in the midazolam group received 2 ml of 5% heavy lidocaine plus 0.4 ml of 0.5% midazolam. Duration of analgesia was significantly greater in the midazolam group (7  1 hours compared to the control group (1.5  0.5 hours.

  4. Ice freezes pain? A review of the clinical effectiveness of analgesic cold therapy.

    Ernst, E; Fialka, V

    1994-01-01

    Among the physical treatments to reduce pain, ice has had its place for many years. Experience tells us that ice has a strong short-term analgesic effect in many painful conditions, particularly those related to the musculoskeletal system. Serial applications may also be helpful. The scientific evidence from clinical trials is, however, fragmentary. This applies both for acute and serial cold-induced analgesia. The mechanisms by which cryotherapy might elevate pain threshold include an antinociceptive effect on the gate control system, a decrease in nerve conduction, reduction in muscle spasms, and prevention of edema after injury. It is concluded that ice may be useful for a variety of musculoskeletal pains, yet the evidence for its efficacy should be established more convincingly.

  5. LABORATORY MODELS FOR SCREENING ANALGESICS

    Parle Milind

    2013-01-01

    Full Text Available Pain is a complex unpleasant phenomenon composed of sensory experiences that include time, space, intensity, emotion, cognition and motivation. Analgesics are the agents, which selectively relieve pain by acting in the CNS or by peripheral pain mechanisms without significantly altering consciousness. Analgesics may be narcotic or non-narcotic. The study of pain in animals raises ethical, philosophical and technical problems. Philosophically, there is a problem that pain cannot be monitored directly in animals but can only be measured by examining their responses to nociceptive stimuli. The observed reactions are almost always motor responses ranging from spinal reflexes to complex behavior. The animal models employed for screening of analgesic agents, include Pain-state models based on the use of thermal stimuli, mechanical stimuli, electrical stimuli and chemical stimuli. The neuronal basis of most of the above laboratory models is poorly understood, however their application is profitable in predicting analgesic activity of newly discovered substances.

  6. A CLINICAL COMPARATIVE STUDY OF ANALGESIC EFFECT OF TRAMADOL AND PENTAZOCINE IN POST - OPERATIVE PATIENTS FOLLOWING UPPER ABDOMINAL SURGERY

    Jamuna

    2015-06-01

    Full Text Available The post - operative pain can be treated by various approaches. Aim of this randomised prospective study was to compare two drugs (Tramadol and Pentazocine . 100 adult patients of both sexes of ASA status 1 & 2 posted for elective upper abdominal surgery were randomly assigned into two groups of 50 each, where Group 1 received Tramadol intravenously and Group 2 received Pentazocine intravenously as post - opera tive pain management. The efficacy of the analgesic effect of intravenous Tramadol & Pentazocine was compared during post - operative pain management. It was observed that Tramadol has got more potent analgesic action compared to equianalgesic dose of Pentaz ocine.

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

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

    2014-11-01

    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.

  8. UP1306, a botanical composition with analgesic and anti-inflammatory effect

    Mesfin Yimam

    2016-01-01

    Pain is the most common clinical manifestations of arthritisCarrageenan.induced rat paw edema and abdominal constriction (writhingfs assays in mouse are among the widely used models to evaluate the anti.inflammatory and analgesic effects of nutraceuticalsCyclooxygenase and lipoxygenase (LO inhibition assays were carried out to determine the IC50 of Acacia and Morus extractsEfficacy of UP1306, a composition containing a blend of two standardized extracts from the heartwood of Acacia catechu and root bark of Morus alba, was evaluated in the above modelsUP1306 demonstrated its enhanced significance by improving the major cardinal signs of arthritis in vivo and inflammation markers in vitroUP1306 could potentially be considered as a dietary supplement product for the management of arthritis.

  9. The effects of a new opioid analgesic, meptazinol, on the respiration of the conscious rat.

    Cowlrick, I S; Shepperson, N B

    1985-05-01

    In the conscious rat arterial PCO2 was measured as an index of respiratory status. The opioid analgesic meptazinol (7.5 - 30 mg kg-1) evoked small but significant increases in arterial PCO2 which were attenuated by naloxone. Meptazinol significantly reduced the increase in arterial PCO2 evoked by morphine. The respiratory depression induced by meptazinol, but not that induced by morphine, was enhanced by pretreatment with atropine. The (+)-enantiomer, but not the (-)-enantiomer of meptazinol increased arterial PCO2. In contrast, only the (-)-enantiomer reduced the respiratory depressant effect of morphine. It is proposed that the degree of respiratory depression induced by meptazinol is limited by its opioid antagonist and cholinomimetic properties.

  10. Analgesic effect of extracorporeal shock wave therapy versus ultrasound therapy in chronic tennis elbow.

    Lizis, Paweł

    2015-08-01

    [Purpose] This study compared the analgesic effects of extracorporeal shock wave therapy with those of ultrasound therapy in patients with chronic tennis elbow. [Subjects] Fifty patients with tennis elbow were randomized to receive extracorporeal shock wave therapy or ultrasound therapy. [Methods] The extracorporeal shock wave therapy group received 5 treatments once per week. Meanwhile, the ultrasound group received 10 treatments 3 times per week. Pain was assessed using the visual analogue scale during grip strength evaluation, palpation of the lateral epicondyle, Thomsen test, and chair test. Resting pain was also recorded. The scores were recorded and compared within and between groups pre-treatment, immediately post-treatment, and 3 months post-treatment. [Results] Intra- and intergroup comparisons immediately and 3 months post-treatment showed extracorporeal shock wave therapy decreased pain to a significantly greater extent than ultrasound therapy. [Conclusion] Extracorporeal shock wave therapy can significantly reduce pain in patients with chronic tennis elbow.

  11. Analgesic effect of perioperative escitalopram in high pain catastrophizing patients after total knee arthroplasty

    Lunn, Troels H; Frokjaer, Vibe G; Hansen, Torben Bæk

    2015-01-01

    has not previously been investigated. The authors hypothesized that perioperative escitalopram would reduce pain after TKA in high pain catastrophizing patients. METHODS: A total of 120 pain catastrophizing patients (selected using the pain catastrophizing scale as preoperative screening tool......) scheduled for TKA were randomized in a double-blind manner to either 10 mg escitalopram or placebo daily from preanesthesia to postoperative day 6 in addition to a standardized analgesic regime. The primary outcome was pain upon ambulation 24 h after surgery. Secondary outcomes were overall pain during well......-defined mobilizations and at rest from 2 to 48 h and from days 2 to 6, morphine equivalents, anxiety, depression, and side effects. RESULTS: Pain upon ambulation (mean [95% CI]) 24 h after surgery in the escitalopram versus placebo group was 58 (53 to 64) versus 64 (58 to 69), the mean difference being -5 (-13 to 3), P...

  12. Non-analgesic effects of opioids: opioid-induced respiratory depression.

    Boom, Merel; Niesters, Marieke; Sarton, Elise; Aarts, Leon; Smith, Terry W; Dahan, Albert

    2012-01-01

    Opioids induce respiratory depression via activation of μ-opioid receptors at specific sites in the central nervous system including the pre-Bötzinger complex, a respiratory rhythm generating area in the pons. Full opioid agonists like morphine and fentanyl affect breathing with onset and offset profiles that are primarily determined by opioid transfer to the receptor site, while the effects of partial opioid agonists such as buprenorphine are governed by transfer to the receptor site together with receptor kinetics, in particular dissociation kinetics. Opioid-induced respiratory depression is potentially fatal but may be reversed by the opioid receptor antagonist naloxone, an agent with a short elimination half-life (30 min). The rate-limiting factor in naloxone-reversal of opioid effect is the receptor kinetics of the opioid agonists that requires reversal. Agents with slow dissociation kinetics (buprenorphine) require a continuous naloxone infusion while agents with rapid kinetics (fentanyl) will show complete reversal upon a single naloxone dose. Since naloxone is non-selective and will reverse analgesia as well, efforts are focused on the development of compounds that reverse opioid-induced respiratory depression without affecting analgesic efficacy. Such agents include ampakines and serotonin agonists which are aimed at selectively enhancing central respiratory drive. A novel approach is aimed at the reduction of respiratory depression from opioid-activation of (micro-)glia cells in the pons and brainstem using micro-glia cell stabilizers. Since this approach simultaneously enhances opioid analgesic efficacy it seems an attractive alternative to the classical reversal strategies with naloxone.

  13. Analgesic Effect of Intra-Articular Injection of Temperature-Responsive Hydrogel Containing Bupivacaine on Osteoarthritic Pain in Rats

    Taemin Kim

    2015-01-01

    Full Text Available The present study examined the analgesic effects of slow-releasing bupivacaine from hydrogel on chronic arthritic pain in rats. Osteoarthritis (OA was induced by monosodium iodoacetate (MIA injection into the right knee joint. Hydrogel (HG: 20, 30, and 50 μL and temperature-sensitive hydrogel containing bupivacaine (T-gel: 20, 30, and 50 μL were injected intra-articularly 14 days after MIA injection. Behavioral tests were conducted. The rats showed a significant decrease in weight load and paw withdrawal threshold (PWT. Intra-articular 0.5% bupivacaine (10 and 20 μL significantly reversed MIA-induced decreased PWT, with no effect on weight load. In normal rats, hydrogel did not produce significant changes in PWT but at 30 and 50 μL slightly decreased weight bearing; T-gel did not cause any changes in both the weight load and PWT. In OA rats, T-gel at 20 μL had a significant analgesic effect for 2 days, even though T-gel at 50 μL further reduced the weight load, demonstrating that intra-articular T-gel (20 μL has long-lasting analgesic effects in OA rats. Thus, T-gel designed to deliver analgesics into the joint cavity could be an effective therapeutic tool in the clinical setting.

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

    Asami Naka

    2013-07-01

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

  15. Effects of histamine on spontaneous neuropathic pain induced by peripheral axotomy

    Jie Yu; Guo-Dong Lou; Jia-Xing Yue; Ying-Ying Tang; Wei-Wei Hou; Wen-Ting Shou; Hiroshi Ohtsu

    2013-01-01

    The present study was designed to investigate the effects of histamine on spontaneous neuropathic pain (NP) induced by peripheral axotomy.Rats and mice were subjected to complete transection of the left sciatic and saphenous nerves to induce spontaneous NP (the neuroma model).Rats were then treated with drugs once daily for 30 days (histidine and Ioratadine,i.p.) or 21 days (histamine,i.c.v.).Autotomy behavior was scored daily until day 50 post-operation (PO).On days 14 to 21 PO,some rats in the control group were subjected to single-fiber recording.Autotomy behavior was also monitored daily in histidine decarboxylase (the key enzyme for histamine synthesis) knockout (HDC~) and wild-type mice for 42 days.We found that both histidine (500 mg/kg) (a precursor of histamine that increases histamine levels in the tissues) and histamine (50 μg/5 μL) significantly suppressed autotomy behavior in rats.HDC-/-mice lacking endogenous histamine showed higher levels of autotomy than the wild-type.In addition,the analgesic effect of histidine was not antagonized by Ioratadine (a peripherally-acting H1 receptor antagonist),while Ioratadine alone significantly suppressed autotomy.Electrophysiological recording showed that ectopic spontaneous discharges from the neuroma were blocked by systemic diphenhydramine (an H1 receptor antagonist).Our results suggest that histamine plays an important role in spontaneous NP.It is likely that histamine in the central nervous system is analgesic,while in the periphery,via H1 receptors,it is algesic.This study justifies the avoidance of a histamine-rich diet and the use of peripherally-acting H1 receptor antagonists as well as agents that improve histamine action in the central nervous system in patients with spontaneous NP.

  16. Pharmacogenetics of new analgesics.

    Lötsch, Jörn; Geisslinger, Gerd

    2011-06-01

    Patient phenotypes in pharmacological pain treatment varies between individuals, which could be partly assigned to their genotypes regarding the targets of classical analgesics (OPRM1, PTGS2) or associated signalling pathways (KCNJ6). Translational and genetic research have identified new targets, for which new analgesics are being developed. This addresses voltage-gated sodium, calcium and potassium channels, for which SCN9A, CACNA1B, KCNQ2 and KCNQ3, respectively, are primary gene candidates because they code for the subunits of the respective channels targeted by analgesics currently in clinical development. Mutations in voltage gated transient receptor potential (TRPV) channels are known from genetic pain research and may modulate the effects of analgesics under development targeting TRPV1 or TRPV3. To this add ligand-gated ion channels including nicotinic acetylcholine receptors, ionotropic glutamate-gated receptors and ATP-gated purinergic P2X receptors with most important subunits coded by CHRNA4, GRIN2B and P2RX7. Among G protein coupled receptors, δ-opioid receptors (coded by OPRD1), cannabinoid receptors (CNR1 and CNR2), metabotropic glutamate receptors (mGluR5 coded by GRM5), bradykinin B(1) (BDKRB1) and 5-HT(1A) (HTR1A) receptors are targeted by new analgesic substances. Finally, nerve growth factor (NGFB), its tyrosine kinase receptor (NTRK1) and the fatty acid amide hydrolase (FAAH) have become targets of interest. For most of these genes, functional variants have been associated with neuro-psychiatric disorders and not yet with analgesia. However, research on the genetic modulation of pain has already identified variants in these genes, relative to pain, which may facilitate the pharmacogenetic assessments of new analgesics. The increased number of candidate pharmacogenetic modulators of analgesic actions may open opportunities for the broader clinical implementation of genotyping information.

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

    Tsuda Yuko

    2010-12-01

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

  18. Pharmacokinetic-Pharmacodynamic Modelling of the Analgesic and Antihyperalgesic Effects of Morphine after Intravenous Infusion in Human Volunteers

    Ravn, Pernille; Foster, David J. R.; Kreilgaard, Mads

    2014-01-01

    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...

  19. Investigation on the anti- inflammatory and analgesic effects of Olea europaea L. metanolic extract on male NMRI mouse

    Elaheh Tekye

    2012-04-01

    Full Text Available Background: Different mediators are involved in pain and edema induction during different stages of inflammation. Then, treatment of them encounters some difficulties. Medicinal plants are an important source of substances which are claimed to induce anti-inflammatory effects. This study was aimed to investigate anti-inflammatory and analgesic effects of Olea europaea L.methanolic extract on male NMRI mouse. Methods: Methanolic extraction was done for leaf of Olea europaea L. and different doses (200, 300 and 400 mg/kg were intraperitoneally (i.p. adminstered to male NMRI mice. Analgesic and anti-inflammatory effects of extract was measured during both phases of Formalin test, Acetic acid induced visceral pain and xylene inflammation tests. A standard analgesic and anti-inflammatory drug such as indomethacin, dexamethasone and morphine were administered in positive control groups where appropriates. Results: Results indicated significant dose-dependent analgesic and anti-inflammatory effects of methanolic extract of Olea europaea L. leaf on pain which induced by formalin (both phase and acetic acid, and inflammation caused by xylene. Conclusion: Our findings Showed that administration of methanolic extract of Olea europaea L.leaf can suppress pain and inflammation dose dependently which, may mediate via different components of extract. However, more investigations need to be done.

  20. A comparison Comparison between analgesic effects of aqueous ethanolic extract of mentha longifolia and morphine in male rats

    Ezatollah Paknia

    2013-08-01

    Full Text Available Background and Aim: Long-term consumption of many drugs followed by reduction of their effectiveness has necessitated performing research on new analgesics .Thus, the present study was conducted to evaluate the analgesic effects of mentha longifolia and morphine in mice using writhing and hot plate tests. Materials and Methods: In this experimental study, 70 male rats were divided into 7 equal groups. The groups included the control, three experimental groups receiving 400, 800, or 1600 mg/kg of mentha extract and three experimental groups which received 2, 4, or 8 mg/kg of morphine .In order to measure pain, the two acceptable tests, writhing and hot plate tests, were applied. Pain scores were measured at 0, 15, 30, 45 or 60 min after administration of algogenic stimulus. Results: It was found that in hot plate test, only the dose of 1600mg/kg of Mentha extract after 60 minutes was significantly able to exert an analgesic effect (P<0.05. In wrighting test, mentha extract at different doses significantly reduced the number and time of wrightes in the rats, comparable to morphine (P<0.05. Conclusion: It seems that all doses of mentha extract in wrighting test have analgesic effects which indicate chronic pain inhibition of mentha hydroalcholic extract.

  1. Analgesic Potential of Opuntia dillenii and Its Compounds Opuntiol and Opuntioside Against Pain Models in Mice

    Faheema Siddiqui

    2016-05-01

    Full Text Available Opuntia dillenii (Nagphana traditionally used against inflammation and also possess analgesic effect. Thus in the present study analgesic properties of O. dillenii cladode methanol extract, its fractions obtained via vacuum liquid chromatography along with isolated α-pyrones, opuntiol and its glucoside, opuntioside were analyzed. The acetic acid-induced writhes were reduced by O. dillenii test agents with opuntioside being most effective (IC 50 26 ± 0.9 mg/kg and equipotent to diclofenac and β-sitosterol. Consistently, it also elicited most potent effect (IC 50: 28 ± 1.1 and 24 ± 1.2 mg/kg during early and late phases of formalin-induced paw licking, producing effect similar to diclofenac and indomethacin. It was also most effective in hot plate test. Naloxone (opioid antagonist reversed the analgesic effects of extract and fractions but failed to antagonize the opuntiol and opuntioside analgesic effects. In conclusion, edible O. dillenii extract, its fractions, opuntiol and opuntioside reduced peripheral and centrally mediated pain via opioid dependent and independent systems. Among them opuntioside emerged as most effective analgesic possibly due to the presence of glucose moiety at position 7 of its α-pyrone ring. This is the first report of opuntiol and opuntioside analgesic effect which may serve as lead compounds in designing of new analgesics.

  2. Analgesic, antiinflammatory and hypoglycaemic effects of ethanol extract of Zingiber officinale (Roscoe) rhizomes (Zingiberaceae) in mice and rats.

    Ojewole, John A O

    2006-09-01

    The present study was undertaken to investigate the analgesic, antiinflammatory and hypoglycaemic effects of Zingiber officinale dried rhizomes ethanol extract (ZOE) in mice and rats. The analgesic effect of ZOE was evaluated by 'hot-plate' and 'acetic acid' analgesic test methods in mice; while the antiinflammatory and hypoglycaemic effects of the plant extract were investigated 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. ZOE (50-800 mg/kg i.p.) produced dose-dependent, significant (p diabetic rats. The findings of this experimental animal study indicate that Zingiber officinale rhizomes ethanol extract possesses analgesic, antiinflammatory and hypoglycaemic properties; and thus lend pharmacological support to folkloric, ethnomedical uses of ginger in the treatment and/or management of painful, arthritic inflammatory conditions, as well as in the management and/or control of type 2 diabetes mellitus in some rural Africa communities.

  3. EXPERIMENTAL ESTIMATION OF THE ANALGESIC EFFECT AT COMBINED INFLUENCE OF THE ELECTROSTIMULATION AND THE PERCUSSIVE-FRICTIONAL MASSAGE AND IMPULSE CURRENTS REGISTRATION

    M. G. Kiselev

    2012-01-01

    Full Text Available The experimental complex of percussive-frictional massager with electrostimulation function and softand hardware of original design gives a possibility to use various mechanical and electrical parameters of massage and electrostimulation and it can be used like the alternative instead of the accepted medicine analgesics. Analgesic effect decreases pain sensation of the patient up to 50 %.

  4. Evaluation of the analgesic effects of ammoxetine, a novel potent serotonin and norepinephrine reuptake inhibitor

    Zhang, Ting-Ting; Xue, Rui; Zhu, Lei; Li, Juan; Fan, Qiong-yin; Zhong, Bo-hua; Li, Yun-Feng; Ye, Cai-ying; Zhang, You-zhi

    2016-01-01

    Aim: The selective serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors (SNRIs) are commonly used for the treatment of neuropathic pain and fibromyalgia. Ammoxetine ((±)-3-(benzo[d] [1,3]dioxol-4-yloxy)-N-methyl-3-(thiophen-2-yl)propan-1-amine) has been identified as a novel potent SNRI. In this study, we evaluated the acute analgesic properties of ammoxetine in different animal models of pain, and examined the involvement of monoamines in its analgesic actions. Methods: The analgesic...

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

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

    2012-09-01

    Shaoyao-gancao-tang, a Chinese medicinal formula consisting of peony and licorice has been used for the treatment of dysmenorrhea for thousands of years. The purpose of the present study was to demonstrate the analgesic and uterine relaxant effects of isoliquiritigenin (ISL), a flavonoid isolated from the roots of Glycyrrhiza glabra (a type of licorice). In vitro, isoliquiritigenin caused concentration-dependent inhibition of spontaneous contraction of isolated rat uterus and the contraction induced by various types of stimulants, such as acetylcholine (Ach, 10 mM), KCl (40 mM) and oxytocin (1 mU/mL). The uterine contractile response to cumulative concentrations of CaCl₂ was blocked by 0.1 and 1 mM of isoliquiritigenin. The isoliquiritigenin-induced relaxation was partly inhibited by the nitric oxide synthase (NOS) inhibitor Nv-nitro-L-arginine methylester (L-NAME, 100 mM) and the COX-1/COX-2 inhibitor indomethacin (10mM). In vivo, isoliquiritigenin could cause a significant reduction in the acetic acid-induced writhing response and hot-plate test at the high dose. These results indicate that isoliquiritigenin, a flavonoid isolated from the roots of Glycyrrhiza glabra, not only has a spasmolytic effect on uterine contraction, which is in relation to Ca²⁺ channels, NOS and COX, but also an effective activity in reducing pain.

  6. Antioxidant, analgesic and anti-inflammatory effects of lavender essential oil

    GABRIELA L. DA SILVA

    2015-08-01

    Full Text Available Several studies have investigated the antinociceptive, immunomodulatory and anti-inflammatory properties of compounds found in the lavender essential oil (LEO, however to date, there is still lack of substantial data. The objective of this study was to assess the antioxidant, anti-inflammatory and antinociceptive effects of lavender essential oil. The 1,1-diphenyl-2-picrylhydrazyl radical decolorization assay was used for antioxidant activity evaluation. The anti-inflammatory activity was tested using two models of acute inflammation: carrageenan-induced pleurisy and croton oil-induced ear edema. The antinociceptive activity was tested using the pain model induced by formalin. LEO has antioxidant activity, which is dose-dependent response. The inflammatory response evoked by carrageenan and by croton oil was reduced through the pre-treatment of animals with LEO. In the pleurisy model, the drug used as positive control, dexamethasone, was more efficacious. However, in the ear swelling, the antiedematogenic effect of the oil was similar to that observed for dexamethasone. In the formalin test, LEO consistently inhibited spontaneous nociception and presented a similar effect to that of tramadol. The results of this study reveal (in vivo the analgesic and anti-inflammatory activities of LEO and demonstrates its important therapeutic potential.

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

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

    2012-12-01

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

  8. Peripheral nerve extract effects on mesenchymal cells.

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

    1996-01-01

    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...

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

    Dhanapal, L P; Morse, A N

    2009-01-01

    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.

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

    Lucia Marseglia

    2015-01-01

    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.

  11. The effects of two analgesic regimes on behavior after abdominal surgery in Steller sea lions.

    Walker, Kristen A; Horning, Markus; Mellish, Jo-Ann E; Weary, Daniel M

    2011-10-01

    This study examined the effects of two non-steroidal anti-inflammatory drug (NSAID) treatment protocols on the behavioral responses of juvenile Steller sea lions after abdominal surgery. Sea lions were randomly assigned to one of two treatments designed to control post-operative pain. The flunixin group (n=6) received flunixin meglumine (1mg/kg) administered as a single intramuscular (IM) injection before extubation from surgery. The carprofen group (n=5) received carprofen (4.4 mg/kg) as an IM injection before extubation, then orally at 24, 48 and 72 h after surgery. Seven behaviors related to post-operative pain were monitored by observers, blinded to treatment, for a total of 10 days (3 days pre-, day of surgery, and 6 days post-surgery). All seven behaviors changed after surgery regardless of NSAID treatment, two of which returned to baseline within 6 days of surgery. Only one behavior was mildly affected by analgesic treatment: sea lions in the carprofen group tended to spend less time lying down in Days 1-3 following surgery (i.e., the days which they received oral carprofen). These results suggested that neither treatment, at the dose administered, was effective in controlling pain in the days following this surgery.

  12. Structure-based discovery of opioid analgesics with reduced side effects.

    Manglik, Aashish; Lin, Henry; Aryal, Dipendra K; McCorvy, John D; Dengler, Daniela; Corder, Gregory; Levit, Anat; Kling, Ralf C; Bernat, Viachaslau; Hübner, Harald; Huang, Xi-Ping; Sassano, Maria F; Giguère, Patrick M; Löber, Stefan; Da Duan; Scherrer, Grégory; Kobilka, Brian K; Gmeiner, Peter; Roth, Bryan L; Shoichet, Brian K

    2016-09-08

    Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side effects of morphine and related opioids-which include fatal respiratory depression-are thought to be mediated by μ-opioid-receptor (μOR) signalling through the β-arrestin pathway or by actions at other receptors. Conversely, G-protein μOR signalling is thought to confer analgesia. Here we computationally dock over 3 million molecules against the μOR structure and identify new scaffolds unrelated to known opioids. Structure-based optimization yields PZM21-a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and is devoid of both respiratory depression and morphine-like reinforcing activity in mice at equi-analgesic doses. PZM21 thus serves as both a probe to disentangle μOR signalling and a therapeutic lead that is devoid of many of the side effects of current opioids.

  13. Analgesic Effects and the Mechanisms of Anti-Inflammation of Hispolon in Mice

    Heng-Yuan Chang

    2011-01-01

    Full Text Available Hispolon, an active ingredient in the fungi Phellinus linteus was evaluated with analgesic and anti-inflammatory effects. Treatment of male ICR mice with hispolon (10 and 20 mg/kg significantly inhibited the numbers of acetic acid-induced writhing response. Also, our result showed that hispolon (20 mg/kg significantly inhibited the formalin-induced pain in the later phase (P<.01. In the anti-inflammatory test, hispolon (20 mg/kg decreased the paw edema at the fourth and fifth hour after λ-carrageenin (Carr administration, and increased the activities of superoxide dismutase (SOD, glutathione peroxidase (GPx and glutathione reductase (GRx in the liver tissue. We also demonstrated that hispolon significantly attenuated the malondialdehyde (MDA level in the edema paw at the fifth hour after Carr injection. Hispolon (10 and 20 mg/kg decreased the nitric oxide (NO levels on both the edema paw and serum level at the fifth hour after Carr injection. Also, hispolon (10 and 20 mg/kg diminished the serum TNF-α at the fifth hour after Carr injection. The anti-inflammatory mechanisms of hispolon might be related to the decrease in the level of MDA in the edema paw by increasing the activities of SOD, GPx and GRx in the liver. It probably exerts anti-inflammatory effects through the suppression of TNF-α and NO.

  14. The analgesic effect of preoperative pregabalin in radical cystectomy for cancer bladder patients

    Ayman A. Ghoneim; Mohammed M. Hegazy

    2013-01-01

    Objective: After the pregabalin has been approved for the treatment of neuropathic pain, preliminary clinical studies suggested a possible role in the perioperative period. To our knowledge, It has never been studied the perioperative analgesic effect of pregabalin in patients with cancer bladder. In this study, we hypothesized that cancer bladder patients undergoing radical cystectomy and received oral pregabalin 75 mg twice daily for ten days preoperatively would get their postoperative pain reduced. Methods: Sixty patients scheduled for elective radical cystectomy were randomly assigned to one of 2 groups (control group or pregabalin group). Patients in the pregabalin group received 75 mg pregabalin twice daily for ten days before surgery. Standard anesthesia protocol was applied to all patients. Pain intensity, opioid consumption, level of sedation and other side effects were regularly assessed for 48 h postoperative. Results: Mean time for the first request of analgesia was statistically longer in pregabalin group. Meanwhile, mean morphine consumption, VAS scores at rest (in the first 32 h postoperatively), VAS scores during movement (in the first 20 h postoperatively) were statistically significant lower in the pregabalin group than those in the control group. Patients in the pregabalin group were statistically more sedated in the first four hours postoperative than the control group. Conclusion: Preoperative pregabalin 75 mg twice daily for ten days resulted in 60% reduction in 24 h postoperative morphine requirements in patients undergoing radical cystectomy.

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

    José Leonardo Simone

    2013-06-01

    Full Text Available 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 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 < .05 was adopted to reject the null hypothesis. The dexamethasone group showed lower pain intensity (p < .05 than the diclofenac sodium and placebo groups (p < .05. No difference in TARM was observed among the groups (p < .05. Preemptively administered, dexamethasone was effective in controlling postoperative pain.

  16. Analgesic activity of Justicia beddomei leaf extract.

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

    2007-10-01

    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.

  17. Analgesic activity of Justicia beddomei leaf extract

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

    2007-01-01

    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.

  18. Analgesic Effect of Gabapentin on Post-Operative Pain After Arthroscopic Anterior Cruciate Ligament Reconstruction

    Mario I. Ortiz

    2014-03-01

    Full Text Available To the Editor Mardani-Kivi et al presented results about a triple blinded randomized controlled trial with gabapentin in patients that underwent anterior cruciate ligament (ACL reconstruction (1. In their manuscript, the introduction section is very illustrative about the subject. With respect to methodology, it is well known that the physical diagnosis of ACL injury is particularly difficult in several patients, and partial ACL tears are also difficult to diagnose on physical examination. In this particular case, how did the authors obtain the diagnosis of ACL in the patients? Likewise, ACL reconstruction can be delayed several weeks or months until the swelling has decreased and there is an appropriate range of motion. For this reason, I want to ask: was the cause of the ACL injury homogeneous in all patients?; was the time delay of the surgery the same for everyone; and was the type of damage the same for all participants? Meperidine is an opioid with analgesic effects. The American Pain Society and the Institute for Safe Medication Practice (ISMP do not recommend meperidine use as pain relieving medication or they recommend it only in very special cases and with many precautions during its administration (2, 3. What was the rationale of the authors choosing meperidine as analgesic drug? In this same sense, authors did not indicate in their manuscript whether meperidine was administered by oral, intramuscular or intravenous pathways or patient-controlled analgesia. The time schedule of meperidine administration was not indicate in the manuscript; was meperidine administered q4h or q6h? How many doses were received by patients? I think it was a mistake to publish the demographic data of all patients (n=114. You had to eliminate the patients deleted in the presentation of the demographic characteristics of the patients (n=108, that is more correct. Table 2 and 3 were poorly prepared. Table 2 has missing data about the results at 24 hours in the

  19. The analgesic effect of electrostimulation (WoundEL®) in the treatment of leg ulcers.

    Leloup, Pauline; Toussaint, Pascal; Lembelembe, Jean-Paul; Célérier, Philippe; Maillard, Hervé

    2015-12-01

    This study aims to demonstrate the analgesic efficacy of electrostimulation (ES), a recognised treatment for leg ulcers. Patients treated by ES for leg ulcers between 2011 and 2013 were included in the study. The pain score obtained with the numerical rating scale (NRS) was reported before the start of the ES (D0), after 3 days (D3) and 1 week following treatment initialisation. The analgesic treatments (AT) were reported at each assessment. Seventy-three patients were included (mean age 75·19 years): 31 venous leg ulcers, 21 mixed venous leg ulcers, 2 arterial ulcers, 17 hypertensive ischaemic ulcers, 1 Hydrea(®)-induced ulcer and an amputation stump ulcer. The NRS at D0 was on average 5·3 (median = 6) while it was 2·2 at D7 (median = 2), that is P < 0·001. The results were also significant between D0 and D3 (P < 0·001). A decrease in the number of AT used was observed between D0 (2·0 AT per patient on average) and D7 (1·7 AT on average) (P < 0·001). We also observed a decrease in the consumption of grade 3 analgesics on D0 and D7 (P = 0·03). This study demonstrates the rapid analgesic efficacy of ES in leg ulcers, with a clear impact on the NRS score and especially on the decrease in analgesic consumption.

  20. Non-analgesic effects of opioids: opioids and the endocrine system.

    Elliott, Jennifer A; Opper, Susan E; Agarwal, Sonali; Fibuch, Eugene E

    2012-01-01

    Opioids are among the oldest known and most widely used analgesics. The application of opioids has expanded over the last few decades, especially in the treatment of chronic non-malignant pain. This upsurge in opioid use has been accompanied by the increasingly recognized occurrence of opioid-associated endocrinopathy. This may arise after exposure to enteral, parenteral, or neuraxial opioids. Opioid-associated endocrinopathy consists primarily of hypothalamic-pituitary-gonadal axis or hypothalamic-pituitary-adrenal axis dysfunction and may manifest with symptoms of hypogonadism, adrenal dysfunction, and other hormonal disturbances. Additionally, opioid related endocrine dysfunction may be coupled with such disorders as osteoporosis and mood disturbances including depression. Undesirable changes in pain sensitivity such as opioid-induced hyperalgesia, and reduced potency of opioid analgesia may also be potential consequences of chronic opioid consumption. Few studies to date have been able to establish what degree of opioid exposure, in terms of dose or duration of therapy, may predispose patients to opioid-associated endocrinopathy. This article will review the currently available literature concerning opioid-associated endocrinopathy and will provide recommendations for the evaluation, monitoring, and management of opioid-associated endocrinopathy and its other accompanying undesired effects.

  1. Analgesic effects of intramuscular administration of meloxicam in Hispaniolan parrots (Amazona ventralis) with experimentally induced arthritis.

    Cole, Gretchen A; Paul-Murphy, Joanne; Krugner-Higby, Lisa; Klauer, Julia M; Medlin, Scott E; Keuler, Nicholas S; Sladky, Kurt K

    2009-12-01

    OBJECTIVE-To evaluate the analgesic efficacy of meloxicam in parrots with experimentally induced arthritis, with extent of weight bearing and rotational perch walking used as outcome measures. ANIMALS-15 adult Hispaniolan parrots (Amazona ventralis). PROCEDURES-Arthritis was experimentally induced via intra-articular injection of microcrystalline sodium urate suspension (MSU) into 1 intertarsal joint. Parrots were treated in a crossover design. Five treatments were compared as follows: meloxicam (4 dosages) at 0.05, 0.1, 0.5, and 1.0 mg/kg (IM, q 12 h, 3 times) and 0.03 mL of saline (0.9% NaCl) solution (IM, q 12 h, 3 times). The first treatment was given 6 hours following MSU administration. Lameness was assessed by use of a biomechanical perch to record weight-bearing load and a rotational perch to determine dexterity. Feces were collected to assay for occult blood. RESULTS-Parrots treated with meloxicam at 1.0 mg/kg had significantly better return to normal (baseline) weight bearing on the arthritic pelvic limb, compared with control parrots or parrots treated with meloxicam at 0.05, 0.1, and 0.5 mg/kg. All fecal samples collected from parrots following induction of arthritis and treatment with meloxicam had negative results for occult blood. CONCLUSIONS AND CLINICAL RELEVANCE-Meloxicam administered at 1.0 mg/kg, IM, every 12 hours effectively relieved arthritic pain in parrots.

  2. Innovative Opioid Peptides and Biased Agonism: Novel Avenues for More Effective and Safer Analgesics to Treat Chronic Pain.

    Bedini, Andrea; Spampinato, Santi Mario

    2017-02-15

    Chronic pain is a clinically relevant and yet unsolved conditions that is poorly treated with the currently available drugs, thus highlighting the urgent need of innovative analgesics. Although opiates are not very effective in the treatment of inflammatory and neuropathic pain, developing novel opioid receptor peptide agonists, as well as modulating the opioid receptor-mediated responses in a ligand-specific fashion, may represent an innovative and promising strategy to identify more efficacious and safer antalgic drugs. In this review, novel analogues of endomorphin 1 (a mu opioid receptor selective agonist able to induce analgesia in different animal models of pain - including neuropathic pain) and dermorphin (one of the most potent opioid peptide existing in nature) will be discussed as they are emerging as a promising starting point to develop novel opioid agonists: endomorphin 1 analogues, in fact, may determine antinociception in different models of neuropathic pain with reduced side effects as compared to classic opiates as morphine; dermorphin analogues may elicit analgesia in animal models of both inflammatory and neuropathic pain and with less severe adverse effects. Furthermore, such opioid peptides may allow to explore unprecedented modalities of ligand-receptor interactions, helping to characterize biased agonism at opioid receptors: exploiting functional selectivity at opioid receptor may lead to identify innovative analgesic with improved pharmacological responses and optimized side effects. Thus, innovative opioid peptides, as those outlined in this review, are promising candidates to develop more effective opioid analgesics to be employed as medications for chronic pain states, as inflammatory or neuropathic pain.

  3. Translational pain research: evaluating analgesic effect in experimental visceral pain models

    Olesen, Anne Estrup; Andresen, Trine; Christrup, Lona Louring;

    2009-01-01

    Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mechanisms behind the pain and the mode of action of analgesic substances. This can...... treatment of visceral pain. To improve treatment of visceral pain, it is important to study the underlying mechanisms of pain and the action of analgesics used for its treatment. An experimental pain model activates different modalities and can be used to investigate the mechanism of action of different...... be achieved through standardized experimental human pain models. Experimental pain models in healthy volunteers are advantageous for evaluation of analgesic action, as this is often difficult to assess in the clinic because of confounding factors such as sedation, nausea and general malaise. These pain models...

  4. Comparison of the Effects of Laparoscopic and Open Repair Techniques on Postoperative Pain and Analgesic Consumption in Pediatric Unilateral Inguinal Hernia

    Ferda Yılmaz İnal

    2014-06-01

    Full Text Available Aim: Although laparoscopic inguinal hernia (IH repair in adults is widely accepted, its advantages in pediatric age group are questionable. We aimed to compare the effects of open inguinal hernia repair and laparoscopic inguinal hernia repair on length of anaesthesia, postoperative pain and analgesic consumption in boys who underwent unilateral inguinal hernia repair. Methods: Forty patients aged between 7 and 14 years who underwent open and laparoscopic inguinal hernia repair were included in this study. The patients were randomly divided into two groups: unilateral open inguinal hernia repair group (OR n=20 and unilateral laparoscopic inguinal hernia repair group (LR n=20. All patients underwent general anesthesia. The duration of anaesthesia and the duration of surgery were recorded. The Patient Controlled Analgesia (PCA device was set at a 0.01 mg/kg bolus dose, 10 minutes lockout interval and 4 hour limit of 4 mg morphine. The patients, who received morphine PCA for 24 hours postoperatively, were monitored with continuous oximetry. The Visual Analogue Scale (VAS was used to measure pain (0 cm: no pain, 10 cm: worst possible pain. We recorded the side effects of morphine, such as respiratory depression, nausea, vomiting, urinary retention, pruritus. SpO2 level and Ramsay Sedation Scale (RSS, Numerical Rating Scale (NRS, and Visual Analogue Scale (VAS scores at intervals 1, 2, 4, 12, 24 hours as well as amount of analgesics consumed and number of requests within 24 hours postoperatively were recorded. Time to first walking was recorded. Results: In group OR, the mean duration of anaesthesia and surgery were 39.85 minutes and 28.85 minutes, respectively. In group LR, the mean duration of anaesthesia and surgery were 26.11 and 20.53 minutes, respectively. VAS scores and time to first walking were similar in both groups. There was no significant difference in amount of analgesics consumed and number of request between the two groups. In group OR

  5. Local analgesic efficacy of tramadol following intraplantar injection.

    Mert, Tufan; Gunes, Yasemin; Gunay, Ismail

    2007-03-08

    Several studies have suggested that systemic tramadol, an opioid, can represent a valuable treatment in severe pain conditions because of their effects on central pain pathways. However, there are not enough studies supporting that tramadol is efficacious when administered locally. Therefore, we studied the potential local analgesic effects of tramadol in peripheral nociception. In addition, we tested the antinociceptive effects of tramadol-CaCl(2) or naloxone combinations after subcutaneous intraplantar injection in a validated rat model of acute thermal nociception. Local analgesic effects of tramadol were compared with those of lidocaine. The effects of tramadol on thermal paw withdrawal latencies were monitored using the plantar test. The antinociceptive potency of tramadol is higher and long-lasting than that of lidocaine. Naloxone was unable to inhibit the increased antinociceptive response produced by tramadol. Ca(2+) modified the effect of tramadol. When Ca(2+) dose was increased in the solution, thermal antinociceptive potency of tramadol, but not lidocaine was prolonged. Thermal nociceptive responses were not affected in the non-injected paws, indicating a lack of systemic effects with doses of tramadol and lidocaine that elicited local analgesia. These results suggest that intraplantar tramadol administration can produce local analgesic effect with a different action mechanism than that of lidocaine. In addition, extracellular Ca(2+) may play an important role in the local analgesic action of tramadol.

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

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

    2008-01-01

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

  7. Analgesic effectiveness of the association of transcutaneous electrical nerve stimulation and cryotherapy for chronic low back pain

    Abreu,Eliziete Almeida de; Santos, Jean Douglas Moura dos; Ventura,Patrícia Lima

    2011-01-01

    BACKGROUND AND OBJECTIVES: Transcutaneous electrical nerve stimulation (TENS) and cryotherapy are physical therapy resources individually used, since there is the possibility of interaction between TENS and cryotherapy if they are associated. This study aimed at evaluating the analgesic effectiveness of the association or not of TENS and cryotherapy to relieve chronic low back pain. METHOD: Clinical trial involving six chronic low back pain patients distributed in three groups: cryotherapy, T...

  8. Synthesis and Analgesic Effects of μ-TRTX-Hhn1b on Models of Inflammatory and Neuropathic Pain

    Yu Liu

    2014-08-01

    Full Text Available μ-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 μ-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. μ-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 μ-TRTX-Hhn1b on both models was equivalent to that of morphine. In the spinal nerve model, the reversal effect of μ-TRTX-Hhn1b on allodynia was longer and higher than mexiletine. These results demonstrated that μ-TRTX-Hhn1b efficiently alleviated acute inflammatory pain and chronic neuropathic pain in animals and provided an attractive template for further clinical analgesic drug design.

  9. Evaluation of the Analgesic and Clinical Effects Associated with the Subarachnoid Administration of Propofol in Sheep

    Mousa Daradka

    2014-06-01

    Full Text Available The objective of this study was to evaluate the toxic, analgesic and clinical effects associated with intrathecal administration of propofol in sheep. Five, healthy adult non-pregnant Awassi sheep were used in the study. Propofol (2.85 mg/kg; n = 4 or normal saline (control, n = 1 was administered into the subarachnoid space at the lumbosacral intervertebral junction. Animals were assessed clinically for toxic signs, analgesia, sedation and ataxia. The heart rate, respiratory rate, rectal temperature, arterial blood pH, HCO3-, PaO2 and PaCO2 were recorded before (time = 0 and then at 5, 15, 30, 60, 90 and 120 min after injection of propofol. Tissues from the spinal cord and meninges were evaluated histologically for evidence of local toxic effects due to intrathecal injection of propofol. Following the administration of propofol, sheep showed signs of sedation and were ataxic within 15 min. The sheep developed sufficient surgical analgesia of the caudal abdominal wall, vagina, perinea, pelvic limbs and udder 15 to 30 min following injection of the drug and lasted for over 90 min. Sheep in the treatment group had significantly higher heart rates, PaCO2 and HCO3- values and decreased blood pH. Values of PaO2 increased significantly initially and then decreased while the respiratory rate and rectal temperatures decreased but not significantly. Histological examination of the meninges and spinal cord showed no significant changes. Results of this study showed that a single injection of propofol into the subarachnoid space can result in sufficient surgical analgesia of the caudal abdominal wall, vagina, perinea, pelvic limbs and udder with moderate sedative effect and acceptable clinical and acid-base alterations in sheep.

  10. Effect of oral clonidine premedication on perioperative haemodynamic response and postoperative analgesic requirement for patients undergoing laparoscopic cholecystectomy.

    Singh, Shivinder; Arora, Kapil

    2011-01-01

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

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

    Shivinder Singh

    2011-01-01

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

  12. 评《硫酸软骨素》%Study on Analgesic Effect of Headache Zhijing Extract

    袁勤生

    2012-01-01

    Objective To observe the analgesic effect and mechanism of headache zhijing extract. Methods The evaluation was performed by acetic acid writhing test in mice, nitroglycerin-induced migraine test in rats and dextran-induced blood stasis test in rabbits. Results After 7 days with the administration of headache zhijing extract (0.36-1.44g/kg), the animals could significantly prolong the pain threshold, reduce the number of writhing within 15min after administration, and increase analgesic efficacy. Compared with the control group, the number of scratching heads, scratching cheek, climbing the cage were significantly reduced in headache zhijing extract (0.5-1.0g/kg) group, and the appearance of scratching heads and scratching cheek was significantly later and the disappearance was significantly earlier in a dose-dependent manner. Headache zhijing extract (0.448g/kg) could significantly reduce the low and high shearing stress of blood viscosity, and as well as the low and high shearing stress of blood reduced viscosity and plasma viscosity in rabbits. Conclusion Headache zhijing extract has strong analgesic effect on writhing mice induced by acetic acid and migraine rats induced by nitroglycerin, and it can significantly improve the hemorheology in blood stasis model of rabbit.

  13. Effects of four analgesic treatments on the behavioural and cortisol responses of 3-week-old lambs to tail docking.

    Graham, M J; Kent, J E; Molony, V

    1997-01-01

    The behavioural and cortisol responses of groups of seven or eight lambs were used to determine which of three methods of tail docking (rubber ring, Burdizzo and rubber ring combined, or heated docking iron) produced the least signs of pain in the first 3 h after use and which of four analgesic treatments (1.0 ml bupivacaine subcutaneously, 0.5 ml bupivacaine epidurally, a topical cold analgesic spray or diclofenac 1.5 mg kg-1) was most effective in reducing these signs. Amputation with a heated docking iron produced levels of behaviour and cortisol responses which did not differ markedly from those of handled controls. The rubber ring method produced the greatest increase in all parameters (total active behaviour 110 +/- 91 counts; 51 +/- 23 min spent in abnormal postures; peak cortisol 93 +/- 51 nmol l-1). Subcutaneous bupivacaine, administered immediately prior to application of the ring, appeared to be the analgesic treatment most effective at reducing these responses (23 +/- 15 counts; 24 +/- 22 min.; 44 +/- 20 nmol l-1).

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

    H.P. Aithal

    2001-07-01

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

  15. Evaluation on the analgesic and anti-inflammatory effect of flurbiprofen axetil Injection%氟比洛芬酯注射液的镇痛抗炎作用评价

    李亮; 许笑彬; 赵海涛; 李军; 刘永勤

    2011-01-01

    [目的]研究氟比洛芬酯注射液的镇痛抗炎作用.[方法]通过小鼠醋酸扭体和大鼠福尔马林炎性痛模型评价氟比洛芬酯注射液的镇痛抗炎作用.[结果]在小鼠醋酸扭体模型上,与空白组相比,尾静脉给予20、40和80mg/kg的氟比洛芬酯注射液(Flurbiprofen Axetil Injection,Flu-A)均能够显著抑制小鼠扭体次数,具有较好的镇痛作用;在大鼠福尔马林炎性痛模型上,Flu-A(40和80mg/kg,i.v.)能够显著降低大鼠的缩足次数和右足足肿胀程度,表现出较好的镇痛抗炎作用.此外,Flu-A在80mg/kg剂量下的镇痛强度与阿司匹林相当.[结论]氟比洛芬酯注射液具有一定的镇痛抗炎作用.%[Objective] To estimate the analgesic and anti-inflammatory effects of Flurbipmfen Axetil Injection (Flu-A). [Methods]Acetic acid-induced mouse writhing model and formalin induced rat paw edema models were used to study the analgesic and anti-inflammatory effects of Flu-A. [ Results ] The results of the acetic acid-induced writhing behaviour in mice showed that Flu-A at 20, 40 and 80 mg/kg could significantly reduce the writhing numbem as compared with control group, and indicated that Flu-A had analgesic activity. The results of the formalin test showed that Flu-A at 40 and 80 mg/kg could significantly reduce the flinch numbers and volume of fight pawas compared with control group and showed peripheral analgesic and anti-inflammatory activity. The analgesic effect of Flu-A at 80 rg/kg were comparable with aspirin. [ Conclusion ] Flu-A have certain analgesic and anti-inflammatory activity.

  16. The cannabinoid CB₂ receptor-selective phytocannabinoid beta-caryophyllene exerts analgesic effects in mouse models of inflammatory and neuropathic pain.

    Klauke, A-L; Racz, I; Pradier, B; Markert, A; Zimmer, A M; Gertsch, J; Zimmer, A

    2014-04-01

    The widespread plant volatile beta-caryophyllene (BCP) was recently identified as a natural selective agonist of the peripherally expressed cannabinoid receptor 2 (CB₂). It is found in relatively high concentrations in many spices and food plants. A number of studies have shown that CB₂ is critically involved in the modulation of inflammatory and neuropathic pain responses. In this study, we have investigated the analgesic effects of BCP in animal models of inflammatory and neuropathic pain. We demonstrate that orally administered BCP reduced inflammatory (late phase) pain responses in the formalin test in a CB₂ receptor-dependent manner, while it had no effect on acute (early phase) responses. In a neuropathic pain model the chronic oral administration of BCP attenuated thermal hyperalgesia and mechanical allodynia, and reduced spinal neuroinflammation. Importantly, we found no signs of tolerance to the anti-hyperalgesic effects of BCP after prolonged treatment. Oral BCP was more effective than the subcutaneously injected synthetic CB₂ agonist JWH-133. Thus, the natural plant product BCP may be highly effective in the treatment of long lasting, debilitating pain states. Our results have important implications for the role of dietary factors in the development and modulation of chronic pain conditions.

  17. The effects of analgesic prescription and patient adherence on pain in a Dutch outpatient cancer population

    Enting, Roeline; Oldenmenger, Wendy H.; Van Gool, Arthur R.; van der Rijt, Carin C. D.; Smitt, Peter A. E. Sillevis

    2007-01-01

    Insufficient awareness of cancer Pain, including breakthrough pain, inadequate analgesic prescriptions, and nonadherence contribute to inadequate cancer pain management. There are insufficient data about the contribution of each of these factors. In a cross-sectional survey among 915 adult cancer ou

  18. Beneficial effect of n-3 polyunsaturated fatty acids on inflammation and analgesic use in psoriatic arthritis

    Kristensen, Salome; Schmidt, E B; Schlemmer, A

    2017-01-01

    , double-blind, placebo-controlled study. The participants received a supplement of 3 g n-3 PUFA/day or 3 g olive oil/day (control) for 24 weeks. Outcome measures for disease activity, use of analgesics, and leukotriene formation from activated granulocytes were assessed at baseline and at study end...

  19. Comparison of Analgesic Effects of Novafen and Ibuprofen after Periodontal Surgeries

    Amirreza Babaloo

    2017-01-01

    Full Text Available Introduction: Management of pain after dental procedures is one of the most important issues for dentists. Non-steroidal antiinflammatory agents, such as ibuprofen, are one of the most commonly used medications to relieve pain. Recently a new medication, Novafen, has been introduced into the Iranian pharmaceutical market, which is a combination of ibuprofen, acetaminophen and caffeine. Considering the importance of management of pain after periodontal surgeries and a paucity of studies in this respect, the present study was undertaken to compare the analgesic efficacy of Novafen and ibuprofen in alleviating pain after periodontal surgeries. Materials and methods: In the present controlled randomized clinical trial, 30 systemically healthy subjects with moderate to severe generalized chronic periodontitis, who were candidates for flap surgeries were evaluated in two groups with 30 areas in each group (two areas in each patient. After the periodontal surgical procedures, the subjects in group 1 received Novafen capsules (containing 325 mg of acetaminophen, 200 mg of ibuprofen and 40 mg of caffeine and the subjects in group 2 received ibuprofen (400 mg. The medications were selected from one pharmaceutical company and the patients only used the medications they received. The severity of pain was determined and compared at 3-minute, 1-hour and 3-hour intervals using VAS and 1, 2 and 3 days postoperatively using VRS. Results: Severity of pain at 30-minute interval in the Novafen group was significantly less than that in the ibuprofen group, with no significant differences at 1- and 3-hour intervals. However, VRS revealed significantly less pain 1, 2 and 3 days postoperatively in the Novafen group compared to the ibuprofen group. Conclusion: Based on the results of the present study, it can be concluded than Novafen can be more effective after periodontal surgeries in alleviating pain. However, its pain control capacity was similar to that of

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

    Elif Basagan-Mogo

    2010-01-01

    Full Text Available 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: Anesthetic 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<0.01. CONCLUSION: There were no differences between groups in the consumption of sevoflurane or in the use of additional fentanyl. The combination of ketamine, midazolam, and

  1. Effects of lidocaine and esmolol infusions on hemodynamic changes, analgesic requirement, and recovery in laparoscopic cholecystectomy operations

    Serpil Dagdelen Dogan

    2016-04-01

    Full Text Available ABSTRACT OBJECTIVE: We compared the effects of lidocaine and esmolol infusions on intraoperative hemodynamic changes, intraoperative and postoperative analgesic requirements, and recovery in laparoscopic cholecystectomy surgery. METHODS: The first group (n = 30 received IV lidocaine infusions at a rate of 1.5 mg/kg/min and the second group (n = 30 received IV esmolol infusions at a rate of 1 mg/kg/min. Hemodynamic changes, intraoperative and postoperative analgesic requirements, and recovery characteristics were evaluated. RESULTS: In the lidocaine group, systolic arterial blood pressures values were lower after the induction of anesthesia and at 20 min following surgical incision (p < 0.05. Awakening time was shorter in the esmolol group (p < 0.001; Ramsay Sedation Scale scores at 10 min after extubation were lower in the esmolol group (p < 0.05. The modified Aldrete scores at all measurement time points during the recovery period were relatively lower in the lidocaine group (p < 0.05. The time to attain a modified Aldrete score of ≥9 points was prolonged in the lidocaine group (p < 0.01. Postoperative resting and dynamic VAS scores were higher in the lidocaine group at 10 and 20 min after extubation (p < 0.05, p < 0.01, respectively. Analgesic supplements were less frequently required in the lidocaine group (p < 0.01. CONCLUSION: In laparoscopic cholecystectomies, lidocaine infusion had superiorities over esmolol infusions regarding the suppression of responses to tracheal extubation and postoperative need for additional analgesic agents in the long run, while esmolol was more advantageous with respect to rapid recovery from anesthesia, attenuation of early postoperative pain, and modified Aldrete recovery (MAR scores and time to reach MAR score of 9 points.

  2. Phytochemical constituents,analgesic and anti-inflammatory effects of methanol extract of Triumfetta rhomboidea leaves in animal models

    Uche FI; Okunna BU

    2009-01-01

    Objective:To investigate the analgesic and anti-inflammatory effects of the methanolic extract of the leaves of Triumfetta rhomboidea on mice and rats respectively.And to screen the phytochemical constituent of the ex-tract.Methods:The analgesic effect was determined by acetic acid-induced writhing test in mice.While the anti-inflammatory activity was determined by egg albumin-induced oedema of the rat paw.Phytochemical screening was done by standard procedures.Results:Triumfetta rhomboidea leaf extract (50 -400 mg/kg) caused a statistically significant inhibition on the egg albumin-induced eodema or inflammation in Wister albino rats with P <0.001 (ANOVA).This effect was higher than the observed effect with Piroxicam (0.5 mg/kg) which was used as a standard.The effect was also dose-dependent.Furthermore,Triumfetta rhomboidea ex-tract caused a statistically significant reduction in the number of acetic acid-induced writhing in mice,with P<0.001 (ANOVA).These effects were also does-dependent and greater than the analgesic effects by parac-etamol which was used as a reference drug.Phytochemical screening revealed the presence of flavonoids,ster-oids,triterpenoids alkaloids,tannins and saponins in Truimfetta rhomboidea leaf extract.Conclusion:Trium-fetta rhomboidea can be recommended for acute inflammatory disorders and diseases associated with pains.This also supports its traditional use as an anti-snake bite and anti-cancer or anti-tumor agent.Further study is on the way to find out the mechanism of its action and also to isolate,identify and characterize the active principle responsible for these effects in this plant.

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

    Mehraein A

    2007-08-01

    Full Text Available Background: Magnesium Sulfate (MgSO4 has been used as a pharmacologic agent in different situations for many years in the treatment of tachyarrhythmias, myocardial ischemia, preeclampsia, and tocolysis among others. The analgesic effect of MgSO4 for postoperative pain has been used since the 1990s. Postoperative pain is one of the most common complications in the perioperative period and can result in serious consequences in different organs if left untreated. Inguinal herniorrhaphy is among the most common surgeries and is almost always accompanied by severe pain. The object of this study is to determine the effect of a pre-induction infusion of MgSO4 on the reduction of postsurgical pain after herniorrhaphy. Methods: This double-blind, randomized clinical trial included 105 ASA class I and class II herniorrhaphy patients at Shariati Hospital in years 2004 and 2005. For statistical analysis, the 2 and T tests were used. The patients were divided into three groups based on block randomization. Patients in the following groups received: Group A, 200 ml of normal saline infusion (placebo; Group B, 25 mg/kg MgSO4 in 200 ml of normal saline; Group C, 50 mg/kg MgSO4 in 200 ml of normal saline. All groups were infused twenty minutes before induction of anesthesia using identical methods and dosage in all three groups. Heart rate and mean arterial pressure (MAP at pre- and postintubation and so at skin incision time were charted. Visual analog scale (VAS pain score, nausea, vomiting and the amount of morphine used before recovery room discharge and in six, twelve and twenty-four hours after recovery discharge was recorded. Results: The average age for the different groups was as follows: Group A: 33.6, Group B: 37.37, Group C: 32.74. Nausea and vomiting between the case and control groups were not statistically different (60% vs. 71.4%, p=0.0499, nor was the amount of Morphine used. On recovery room discharge, the VAS scores were 8.1, 7.2, and 5

  4. Analgesic effect of raloxifene on back and knee pain in postmenopausal women with osteoporosis and/or osteoarthritis.

    Fujita, Takuo; Fujii, Yoshio; Munezane, Hiromi; Ohue, Mutsumi; Takagi, Yasuyuki

    2010-07-01

    To assess the effect of raloxifene on bone and joint pain, 24 postmenopausal women with back or knee pain or both were randomly divided into two groups, based on the chronological sequence of consultation, to be treated with 60 mg raloxifene and 1 microg alfacalcidol (RA)/day (group RA) or 1 microg alfacalcidol alone (A)/day (group A), respectively, for 6 months. Pain following knee loading (KL) by standing up from a chair and bending the knee by squatting, knee and spine loading (KSL) by walking horizontally and ascending and descending stairs, and spine loading (SL) by lying down supine on a bed and leaving the bed to stand was evaluated by electroalgometry (EAM), based on measurement of the fall of skin impedance, and a visual rating scale (VRS), recording subjective pain on a scale of 0-100 between no pain and unbearable pain. The two groups showed no significant difference as to age, indices of mineral metabolism, back and knee pain, and bone status. RA gave a significantly greater analgesic effect than A by both EAM (P = 0.0158) and VRS (P = 0.0268) on overall comparison of the mean response to all modalities of exercise loading. Paired comparison between pretreatment and posttreatment indicated a significant effect of RA by both EAM (P = 0.0045) and VRS (P = 0.0017), but not that of A. The analgesic effect was more clearly noted on combined knee-spine loading (KSL) and spine loading (SL) than simple knee loading (KL). Monthly comparison of the analgesic effect indicated a significantly better analgesic effect in the fifth month by VRS. RA effect greater than A was more evident by EAM than VRS and during months 3-6 than during 1-2 months, suggesting a slowly progressive effect of RA. Pain evaluation by EAM and VRS mostly gave parallel results, except for a few occasions such as knee loading and spine loading by sitting up and leaving a bed, when EAM detected a positive effect but VRS failed to do so. RA appeared to be more effective on bone and joint pain

  5. Study on the Analgesic Effect and Mechanism of Zhitong Capsule (止痛胶囊)in Adjuvant Arthritis Rats

    LIU Yan-qing; CHEN Gao-yang; GUO Shi-yu; JIU Guang-zheng

    2005-01-01

    Objective:To observe the analgesic effect of Zhitong Capsule (止痛胶囊, ZTC) and study its mechanism in adjuvant arthritis (AA) rats. Methods: Forty-eight male Sprague-Dawley rats were randomly divided into six groups with 8 rats in each group. On the first day, except to those in the normal group that were treated with normal saline, the same amount of Freund's complete adjuvant (FCA) was given through intradermal injection into the right hind paw to all the rats in the other groups. From the 17th day of the modeling on, the rats in groups of ZTC were administered daily through gastrogavage with a dose of 1000, 500,250 mg/kg respectively, while equal volume of normal saline was given to those in the normal group and model group, and an equal volume of aspirin (ASA) solution was given to rats in the ASA group through gastrogavage for 10 days, once per day, and on the 27th day, the analgesic effect of ZTC was measured with heat withdraw method. The activities and contents of superoxide dismutase (SOD) and lipid peroxides (LPO) in serum were observed by spectrophotometry, and the level of beta-endorphin (β-EP) in hypothalamus were determined by the assay of immunohistochemistry. Results: ZTC showed significant effects on enhancing the pain threshold and at the same time it increased the activities of SOD and reduced the contents of LPO in serum. ZTC could also increase the level of β-EP in hypothalamus. Conclusion: ZTC has analgesic effect and its mechanism is probably related with its effect in inhibiting the level of oxygen free radicals in serum and increasing the level of β-EP of hypothalamus in rats.

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

    Ito Akitoshi

    2012-06-01

    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.

  7. The influence of women's attachment style on the chronobiology of labour pain, analgesic consumption and pharmacological effect.

    Costa-Martins, José Manuel; Pereira, Marco; Martins, Henriqueta; Moura-Ramos, Mariana; Coelho, Rui; Tavares, Jorge

    2014-07-01

    Circadian variation in biological rhythms has been identified as affecting both labour pain and the pharmacological properties of analgesics. In the context of pain, there is also a growing body of evidence suggesting the importance of adult attachment. The purpose of this study was to examine whether labour pain, analgesic consumption and pharmacological effect are significantly affected by the time of day and to analyse whether this circadian variation is influenced by women's attachment style. This prospective observational study included a sample of 81 pregnant women receiving patient-controlled epidural analgesia (PCEA). Attachment was assessed with the Adult Attachment Scale - Revised. The perceived intensity of labour pain in the early stage of labour (3 cm of cervical dilatation and before the administration of PCEA) was measured using a visual analogue scale (VAS). Pain was also indirectly assessed by measuring the consumption of anaesthetics. The latency period and the duration of effect were recorded for a chronopharmacology characterisation. Pain, as assessed with the VAS, was significantly higher in the night-time group than in the daytime group. An insecure attachment style was significantly associated with greater labour pain at 3 cm of cervical dilatation (p < 0.001) and before the beginning of analgesia (p < 0.001) as well as with higher analgesic consumption and lower pharmacological efficacy (p < 0.05). The time of day was significantly associated with the pharmacological effect: the latency period was longer at night, and the duration of the pharmacological effect was longer during the daytime. The interaction between time of day and attachment style was not significant for any of the study variables. Our results provide evidence of the importance of circadian variation in studying labour pain and the pharmacological effect of labour analgesia involving epidural blockage with a PCEA regimen. Moreover, although there was no

  8. Effect of cholic acid and its keto derivatives on the analgesic action of lidocaine and associated biochemical parameters in rats.

    Posa, Mihalj; Kevresan, Slavko; Mikov, Momir; Cirin-Novta, Vera; Kuhajda, Ksenija

    2007-01-01

    This study examined the effect of the structure and concentration of cholic acid and its keto derivatives on the local analgesic action of lidocaine in rats, measured by an analgesimetric method. The increase in bile acid concentrations in the administered lidocaine solution increased the duration of local anesthesia. It was found that the introduction of keto groups into the cholic acid molecule yielded derivatives with lower promotory action, i.e. decreased the duration of local anesthesia. The biochemical parameters investigated indicated that the keto derivatives of cholic acid exhibited no toxicity compared to that of cholic acid itself.

  9. Analgesic and anti-inflammatory effects of the methanol stem bark extract of Prosopis africana.

    Ayanwuyi, Lydia O; Yaro, Abdullahi H; Abodunde, Olajumoke M

    2010-03-01

    Prosopis africana (Guill. & Perr.) Taub. (Mimosoideae) is a shrub used for menstrual and general body pain in Nupe land in north central Nigeria. In this study, the methanol extract of the stem bark of Prosopis africana (at doses of 62.5, 125, and 250 mg/kg) was evaluated for analgesic and anti-inflammatory activities using acetic acid-induced writhing assay and carrageenan-induced inflammation in rats. The extract significantly (P 5000 mg/kg in rats. This study supports the folkloric claim of the use of Prosopis africana in the management of pain.

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

    Navvabi Rigi Shahindokht

    2012-08-01

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

  11. Analgesic effects of meloxicam, morphine sulfate, flunixin meglumine, and xylazine hydrochloride in African-clawed frogs (Xenopus laevis).

    Coble, Dondrae J; Taylor, Douglas K; Mook, Deborah M

    2011-05-01

    We evaluated analgesic use and analgesiometry in aquatic African-clawed frogs (Xenopus laevis). We used the acetic acid test (AAT) to assess the analgesic potential of systemic xylazine hydrochloride, meloxicam, flunixin meglumine, and morphine sulfate after injection into the dorsal lymph sac. Flunixin meglumine provided better analgesia than did the other drugs, most evident at 5 and 9 h after administration. Because the AAT was associated with the development of dermal lesions, we discontinued use of this assay and chose the Hargreaves test as an alternative method of measuring nociception in Xenopus. This assay is commonly performed in rodents, but its efficacy in an aquatic species such as Xenopus was unknown prior to this study. We found that the Hargreaves test was an effective measure of nociception in Xenopus, and we used it to evaluate the effectiveness of the nonopiod agents xylazine hydrochloride, meloxicam, and flunixin meglumine both in the absence of surgery and after surgical oocyte harvest. Similar to findings from the AAT, flunixin meglumine provided better analgesia in the Hargreaves test than did the other agents when analyzed in the absence of surgical intervention. Results were equivocal after oocyte harvest. Although surgical oocyte harvest is a common procedure in Xenopus, and currently there are no published recommendations for analgesia after this invasive surgery. Future studies are needed to clarify the efficacy of nonsteroidal antiinflammatory drugs for that purpose.

  12. Effects of Preoperative Use of Oral Dextromethorphan on Postoperative Need for Analgesics in Patients With Knee Arthroscopy

    Entezary, Saeid Reza; Farshadpour, Saeedeh; Alebouyeh, Mahmood Reza; Imani, Farnad; Emami Meybodi, Mohammad Kazem; Yaribeygi, Habibollah

    2013-01-01

    Background Studies have shown that N-methyl-D-aspartate receptor (NMIDA) plays an essential role in postoperative pain. It seems that use of NMDA receptor antagonists such as Dextromethorphan intensifies the analgesic effects of opioids. Objectives In this study, we evaluated the effect of preoperative administration of Dextromethorphan on postoperative pain reduction. Patients and Methods This double blind randomized clinical trial was conducted on arthroscopic surgery candidates. Participants were randomly allocated to interventions and assigned to two groups of Dextromethorphan and placebo. In Dextromethorphan group, the patients received 1 mg/kg Dextromethorphan orally the night before the operation. Pain severity based on the visual analog scale (VAS) up to 16 hours postoperation, use of opioids, and the first request for analgesics were recorded postoperatively. Results A total of 112 patients in the Dextromethorphan (n = 54) and placebo groups (n = 58) were evaluated. No significant difference was detected between the two groups for age, sex or ASA. The mean amount of opioid consumption was significantly lower in patients who received Dextromethorphan (10.7 ± 5.6 mg) compared to the placebo group (13.1 ± 5.6 mg), (P = 0.03). The mean time until the first opioid request in patients who received Dextromethorphan was longer than that in the placebo group (P = 0.01). Conclusions The study results demonstrated that preemptive use of Dextromethorphan reduced postoperative pain and opioid consumption. PMID:24660143

  13. Redoubling the ring size of an endomorphin-2 analog transforms a centrally acting mu-opioid receptor agonist into a pure peripheral analgesic.

    Piekielna, Justyna; De Marco, Rossella; Gentilucci, Luca; Cerlesi, Maria Camilla; Calo', Girolamo; Tömböly, Csaba; Artali, Roberto; Janecka, Anna

    2016-05-01

    The study reports the synthesis and biological evaluation of two opioid analogs, a monomer and a dimer, obtained as products of the solid-phase, side-chain to side-chain cyclization of the pentapeptide Tyr-d-Lys-Phe-Phe-AspNH2 . The binding affinities to the mu, delta, and kappa opioid receptors, as well as results obtained in a calcium mobilization functional assay are reported. Tyr-[d-Lys-Phe-Phe-Asp]2 -NH2 1 was a potent and selective full agonist of mu with sub-nanomolar affinity, while the dimer (Tyr-[d-Lys-Phe-Phe-Asp]2 -NH2 )2 2 showed a significant mixed mu/kappa affinity, acting as an agonist at the mu. Molecular docking computations were utilized to explain the ability of the dimeric cyclopeptide 2 to interact with the receptor. Interestingly, in spite of the increased ring size, the higher flexibility allowed 2 to fold and fit into the mu receptor binding pocket. Both cyclopeptides were shown to elicit strong antinociceptive activity after intraventricular injection but only cyclomonomer 1 was able to cross the blood-brain barrier. However, the cyclodimer 2 displayed a potent peripheral antinociceptive activity in a mouse model of visceral inflammatory pain. © 2016 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 106: 309-317, 2016.

  14. 镇痛治疗对糖尿病足或糖尿病末梢神经损害患者心理影响%Study of the influence on psychology of analgesic therapy in patients with diabetic foot or diabetic peripheral nerve damage

    许艳; 周宁

    2016-01-01

    目的:探讨镇痛治疗对糖尿病足或糖尿病末梢神经损害患者心理状态的影响。方法选择本院2014年1月至2015年1月收治的糖尿病末梢神经损害或糖尿病足患者66例为研究对象,给予降糖治疗及针对糖尿病足或糖尿病末梢神经损害的必要外科处理及神经营养治疗,在此基础上加用镇痛治疗。比较患者治疗前后疼痛数字评价量表(NRS)、Zung 抑郁自评量表(SDS)和焦虑自评量表(SAS)评分以及生活质量评分。结果镇痛治疗后患者 NRS、SDS、SAS 评分均较治疗前显著降低(P <0.01或 P <0.05);治疗后患者8个维度生活质量评分及总评分较治疗前均显著增加(P <0.05或 P <0.01)。结论在有效降糖、必要外科处理的基础上合理使用镇痛治疗能够更好地减轻糖尿病足或糖尿病末梢神经损害患者疼痛症状,改善心理状态,提高其生活质量,值得推广。%Objective To discuss the clinical effects of analgesic therapy in patients with diabetic foot or diabetic peripheral nerve damage. Method 66 patients with diabetic foot or diabetic peripheral nerve damage were treated with analgesic therapy based on hypoglycemic therapy, surgical treatment and nerve nutrition therapy, then pain numerical rating scale (NRS), SDS, SAS, and quality of life (QOL) scores were compared before and after treatment. Result NRS, SDS, and SAS scores were significantly reduced after treatment (P < 0.05 or P < 0.05). After treatment, the scores of QOL in 8 dimensions and total score were significantly higher than before treatment (P < 0.05 or P < 0.05). Conclusion Analgesic therapy based on effective hypoglycemic therapy, surgical treatment and nerve nutrition therapy for diabetic foot or peripheral nerve injury can much better reduce the patient's pain symptoms, improve the psychological state of patients, improve the quality of life, it is worthy of promotion.

  15. Comparison of speed of anti-inflammatory and analgesic effect appearance of nimesulid and diclofenac sodium tablets in gout arthritis: a randomized study

    F. M. Kudaeva

    2008-01-01

    Full Text Available To assess speed of anti-inflammatory and analgesic effect appearance of nimesulid and diclofenac sodium tablets in gout arthritis. 90 male pts with gout were included in an open clinical study. They were randomly assigned into three groups (30 pts in each. Group 1 pts received nimesulid tablets (Nise 100 mg twice a day, group 2 pts — tablets of an other nimesulid preparation and group 3 pts — diclofenac sodium 75 mg twice a day. Duration of treatment was 7 days. Nise significantly earlier provided anti-inflammatory and analgesic effect, gout arthritis, nimesulid, period till effect appearance, tolerability.

  16. Analgesic Effects of Preincision Ketamine on Postspinal Caesarean Delivery in Uganda’s Tertiary Hospital: A Randomized Clinical Trial

    Richard Mwase

    2017-01-01

    Full Text Available Background. Good postoperative analgesic management improves maternal satisfaction and care of the neonate. Postoperative pain management is a challenge in Mulago Hospital, yet ketamine is accessible and has proven benefit. We determined ketamine’s postoperative analgesic effects. Materials and Methods. We did an RCT among consenting parturients that were randomized to receive either intravenous ketamine (0.25 mg/kg or placebo after spinal anesthetic. Pain was assessed every 30 mins up to 24 hours postoperatively using the numerical rating scale. The first complaint of pain requiring treatment was noted as “time to first breakthrough pain.” Results. We screened 100 patients and recruited 88 that were randomized into two arms of 44 patients that received either ketamine or placebo. Ketamine group had 30-minute longer time to first breakthrough pain and lower 24-hour pain scores. Postoperative diclofenac consumption was lesser in the ketamine group compared to placebo and Kaplan-Meier graphs showed a higher probability of experiencing breakthrough pain earlier in the placebo group. Conclusion. Preincision intravenous ketamine (0.25 mg/kg offered 30-minute prolongation to postoperative analgesia requirement with reduced 24-hour pain scores. We recommend larger studies to explore this benefit. This trial is registered with Pan African Clinical Trial Registry number PACTR201404000807178.

  17. Effects of the analgesic acetaminophen (Paracetamol) and its para-aminophenol metabolite on viability of mouse-cultured cortical neurons.

    Schultz, Stephen; DeSilva, Mauris; Gu, Ting Ting; Qiang, Mei; Whang, Kyumin

    2012-02-01

    Acetaminophen has been used as an analgesic for more than a hundred years, but its mechanism of action has remained elusive. Recently, it has been shown that acetaminophen produces analgesia by the activation of the brain endocannabinoid receptor CB1 through its para-aminophenol (p-aminophenol) metabolite. The objective of this study was to determine whether p-aminophenol could be toxic for in vitro developing mouse cortical neurons as a first step in establishing a link between acetaminophen use and neuronal apoptosis. We exposed developing mouse cortical neurons to various concentrations of drugs for 24 hr in vitro. Acetaminophen itself was not toxic to developing mouse cortical neurons at therapeutic concentrations of 10-250 μg/ml. However, concentrations of p-aminophenol from 1 to 100 μg/ml produced significant (p < 0.05) loss of mouse cortical neuron viability at 24 hr compared to the controls. The naturally occurring endocannabinoid anandamide also caused similar 24-hr loss of cell viability in developing mouse cortical neurons at concentrations from 1 to 100 μg/ml, which indicates the mechanism of cell death could be through the cannabinoid receptors. The results of our experiments have shown a detrimental effect of the acetaminophen metabolite p-aminophenol on in vitro developing cortical neuron viability which could act through CB1 receptors of the endocannabinoid system. These results could be especially important in recommending an analgesic for children or individuals with traumatic brain injury who have developing cortical neurons.

  18. Peripheral alpha 2-adrenoceptor-mediated sympathoinhibitory effects of mivazerol.

    Richer, C; Gobert, J; Noyer, M; Wülfert, E; Giudicelli, J F

    1996-01-01

    Mivazerol is a new compound that could potentially reduce perioperative cardiovascular morbidity and mortality in patients with or at risk of coronary disease and submitted to surgery. This action of mivazerol depends on a well documented centrally mediated reduction in sympathetic nerve activity, but a direct peripheral decrease in sympathetic neurotransmitter release induced by activation of prejunctional alpha 2-adrenoceptors located on sympathetic nerve endings could also contribute. To investigate this issue, the effects of mivazerol on the pressor, systemic and regional hemodynamic (pulsed Doppler technique) as well as on the cardiac responses to electrical stimulation of the spinal cord (SCS) were measured in pithed rats in the absence and in the presence of mivazerol. Mivazerol exerted strong sympathoinhibitory effects: SCS-induced increases in blood pressure, total peripheral resistance and heart rate were dose-dependently reduced by mivazerol, but among the regional vascular beds investigated, only the hindlimb vasoconstrictor responses were significantly drug-affected. All these sympathoinhibitory effects of mivazerol were abolished by prior yohimbine administration. Simultaneously, mivazerol did not induce any postjunctional adrenoceptor blockade as it did not affect noradrenaline cardiac and hemodynamic effects. On the contrary, through postjunctional alpha 2-adrenoceptor stimulation, mivazerol, in this pithed preparation, dose-dependently increased blood pressure, total peripheral and hindlimb vascular resistances, but heart rate was not affected. We conclude that, in the pithed rat, mivazerol exerts strong peripheral sympathoinhibitory effects. The mechanism involved is prejunctional alpha 2-adrenoceptor activation as i) mivazerol does not display any postsynaptic alpha-adrenoceptor blocking effect--it even behaves as as postsynaptic alpha 2-adrenoceptor agonist--and ii) yohimbine abolishes mivazerol's sympathoinhibitory effects. Thus, direct

  19. Ghrelin Exerts Analgesic Effects through Modulation of IL-10 and TGF-β Levels in a Rat Model of Inflammatory Pain

    Azizzadeh, Faranak; Mahmoodi, Javad; Sadigh-Eteghad, Saeed; Farajdokht, Fereshteh; Mohaddes, Gisou

    2017-01-01

    Background: Ghrelin is a peptide with attenuating effect on inflammatory pain. Both anti- and pro-inflammatory mediators have a role in the nociception and development of pain and hyperalgesia. IL-10 and TGF-β are anti-inflammatory cytokines and inhibit the expression of pro-inflammatory cytokines related to peripheral and central inflammatory pain. In this study, the effects of i.p. injection of ghrelin on the early and the late phases of pain, as well as serum levels of IL-10 and TGF-β, as anti-inflammatory cytokines, were investigated in formalin-induced pain in male rats. Methods: Adult male Wistar rats (n=48) were randomly divided into six groups: control, formalin+saline, ghrelin (40, 80, and 160 μg/kg), and morphine. Ghrelin was administered i.p. 30 min before inducing pain by formalin. Pain induced by intraplantar (i.pl.) injection of 50 µl formalin 5%, and pain behavior was studied for 60 min. Serum IL-10 and TGF-β levels were assessed by ELISA method. Results: The findings of the present study showed that ghrelin with high doses (80 and 160 μg/kg) significantly reduced pain intensity in both the early and the late phases of pain. The serum levels of cytokines, IL-10, and TGF-β1 showed a significant elevation with ghrelin at the dose of 160 μg/kg. Conclusion: Ghrelin is effective in reducing the intensity of both the early and the late phases of inflammatory pain. It seems that ghrelin exerts its analgesic effects in part by increasing the serum levels of anti-inflammatory cytokines. PMID:27703278

  20. Antinociceptive effects of topical mepivacaine in a rat model of HIV-associated peripheral neuropathic pain

    Sagen J

    2016-06-01

    Full Text Available Jacqueline Sagen, Daniel A Castellanos,† Aldric T Hama The Miami Project to Cure Paralysis, University of Miami Miller School of Medicine, Miami, FL, USA †Daniel A Castellanos passed away on April 14, 2010 Background: A consequence of HIV infection is sensory neuropathy, a debilitating condition that degrades the quality of life of HIV patients. Furthermore, life-extending antiretroviral treatment may exacerbate HIV sensory neuropathy. Analgesics that relieve other neuropathic pains show little or no efficacy in ameliorating HIV sensory neuropathy. Thus, there is a need for analgesics for people with this particular pain. While lidocaine is used in the management of painful peripheral neuropathies, another local anesthetic mepivacaine, with a potentially improved bioavailability, could be utilized for the management of HIV neuropathic pain.Methods: The efficacy of topical anesthetics was evaluated in a preclinical rodent model of painful peripheral neuropathy induced by epineural administration of the HIV envelope protein gp120 delivered using saturated oxidized cellulose implanted around the sciatic nerve. Beginning at 2 weeks following gp120 administration, the effects of local anesthetics topically applied via gauze pads were tested on heat and mechanical hyperalgesia in the hind paw. Rats were tested using several concentrations of mepivacaine or lidocaine during the following 2 weeks.Results: By 2 weeks following epineural gp120 implantation, the ipsilateral hind paw developed significant hypersensitivity to noxious pressure and heat hyperalgesia. A short-lasting, concentration-dependent amelioration of pressure and heat hyperalgesia was observed following topical application of mepivacaine to the ipsilateral plantar hind paw. By contrast, topical lidocaine ameliorated heat hyperalgesia in a concentration-dependent manner but not pressure hyperalgesia. Equipotent concentrations of mepivacaine and lidocaine applied topically to the

  1. Absence of analgesic effect of intravenous melatonin administration during daytime after laparoscopic cholecystectomy

    Andersen, Lars Peter Holst; Kücükakin, Bülent; Werner, Mads U

    2014-01-01

    STUDY OBJECTIVE: To investigate whether melatonin administered intraoperatively reduced pain following laparoscopic cholecystectomy. DESIGN: Randomized, placebo-controlled, double-blinded study. SETTING: Two surgical departments in Copenhagen. PATIENTS: 44 women between 18 and 70 years of age, who...... mg of intravenous (IV) melatonin or placebo were administered at the time of surgical incision. MEASUREMENTS: Pain was assessed by a set of questionnaires documenting "pain at rest" using a visual analog scale (VAS). The use of rescue medication was recorded. Sleep quality and general well-being were...... between the two groups in the postoperative period. The use of postoperative rescue medication did not differ between the groups. CONCLUSIONS: The use of 10mg of IV melatonin administered during laparoscopic cholecystectomy did not affect postoperative pain or use of analgesic medication....

  2. Effect of the analgesic butorphanol on activity behaviour in turkeys (Meleagris gallopavo).

    Buchwalder, T; Huber-Eicher, B

    2005-12-01

    During fattening, the bodyweight of modern broad-breasted turkeys increases considerably within a very short space of time. In particular, the breast muscles increase disproportionately. This leads to a disadvantageous distribution in weight, and as a consequence, to a disturbed leg position and skeletal deformations like antitrochanteric degeneration, tibial dyschondroplasia, bending, twisting and rotation of the tibia, osteochondrosis, osteomyelitis, rickets, and epiphyseolysis of the femoral head increases. This cases of degenerative joint disease cause severe pain in humans and there are indications that this is also true for turkeys. The purpose of this study was to determine if behaviour indicative of such pain in turkeys of the B.U.T. Big 6 breeding line could be attenuated by administering a quick-acting analgesic, butorphanol. Twelve pairs of turkeys were tested at the ages of 7 and 12 weeks. One bird in each pair received an analgesic opioid injection, while the other one received a control injection of physiologically balanced saline solution. The time the birds spent putting weight on their legs, i.e., 'walking' and 'standing' and the distance covered by the birds were recorded during the 30 min periods before and after the application of the drug. At week seven the treated birds spent significantly more time putting weight on their legs than control birds. At week 12, the same tendency was observed. No significant differences were found in the distances covered by the animals. It is concluded that fattening turkeys reduce the time they are putting weight on their legs because these behaviours may be associated with pain.

  3. Protective effect of Jiaweibugan decoction against diabetic peripheral neuropathy

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

    2013-01-01

    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.

  4. Analgesic nephropathy: is it caused by multi-analgesic abuse or single substance use?

    Elseviers, M M; De Broe, M E

    1999-01-01

    Analgesic nephropathy is a slowly progressive renal disease, characterised by renal papillary necrosis. Recently, diagnostic criteria for this disease have been defined based on renal computed tomography scanning performed without contrast. The observation of a decreased renal mass of both kidneys, combined with either bumpy contours or papillary calcifications, has been found to have high diagnostic specificity and sensitivity. However, the question remains as to what kind of analgesics can cause analgesic nephropathy. In the majority of early reports about this condition, phenacetin was singled out as the nephrotoxic culprit. However, during the last decade the nephrotoxic potential of nonphenacetin-containing preparations has become apparent. It is clear that people who abuse analgesics prefer combination analgesics containing 2 analgesics combined with caffeine and/or codeine. In contrast, abuse of products containing only aspirin (acetylsalicylic acid) or paracetamol (acetaminophen) is seldom described and associated renal disease is only occasionally reported. Experimental evidence of the nephrotoxicity of analgesic preparations is not well established. The results of studies involving analgesic administration in animals remain contradictory. Clinical evidence linking high consumption of analgesic preparations with analgesic nephropathy is overwhelming. Most patients who admit to over-consuming analgesics have taken preparation containing more than one compound. In recent years, it has become more apparent that preparations not containing phenacetin also have the potential to cause nephrotoxicity manifesting as identical renal lesions. Further epidemiological evidence of the nephrotoxic potential of analgesic combinations has come from case-control studies published during the last decade and from 2 prospective cohort studies. Effective prevention of analgesic nephropathy consists of the prohibition of over-the-counter sales of preparation containing at least

  5. Preemptive analgesic effects of flurbiprofen axetil in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach

    WANG Yan; ZHANG Hong-bin; XIA Bin; WANG Gong-ming; ZHANG Meng-yuan

    2012-01-01

    Background Systemic non-steroidal anti-inflammatory drugs have been evaluated for their possible preemptive analgesic effects.The efficacy of flurbiprofen axetil for preemptive analgesia in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach needs further investigation.The aim of this study was to research the preemptive analgesic effects of flurbiprofen axetil in thoracic surgery,and the influence of preoperative administration on postoperative respiratory function.Methods This randomized,double-blind,controlled trial enrolled 60 patients undergoing radical resection of esophageal carcinoma via the left thoracic approach.Anesthesia management was standardized.Each patient was randomly assigned to receive either 100 mg flurbiprofen axetil intravenously 15 minutes before incision (PA group) or intravenous normal saline as a control (C group).Postoperative analgesia was with sufentanil delivered by patient-controlled analgesia pump.Postoperative sufentanil consumption,visual analog scale pain scores,plasma levels of interleukin-8,and oxygenation index were measured.Results Compared with the preoperative baseline,postoperative patients in the PA group had no obvious increase in pain scores (P >0.05),but patients in the C group had significantly increased pain scores (P<0.05).Pain scores in the C group were significantly higher at 24 hours postoperatively than preoperatively.Intergroup comparisons showed lower visual analog scale scores at 2-24 hours postoperatively in the PA group than the C group (P <0.05).Sufentanil consumption and plasma interleukin-8 levels at 2 and 12 hours postoperatively were significantly lower in the PA group than the C group (P <0.05).The oxygenation index at 2 and 12 hours postoperatively was significantly higher in the PA group than the C group (P<0.05).Conclusions Intravenous flurbiprofen axetil appears to have a preemptive analgesic effect in patients undergoing radical resection of

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

    Gao Yong-Hui

    2012-12-01

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

  7. Acute Metabolic Changes Associated With Analgesic Drugs

    Hansen, Tine Maria; Olesen, Anne Estrup; Simonsen, Carsten Wiberg;

    2016-01-01

    BACKGROUND AND PURPOSE: Magnetic resonance spectroscopy (MRS) is used to measure brain metabolites. Limited data exist on the analgesic-induced spectroscopy response. This was an explorative study with the aims to investigate the central effects of two analgesic drugs, an opioid and a selective...

  8. Non-analgesic effects of opioids: cardiovascular effects of opioids and their receptor systems.

    Headrick, John P; Pepe, Salvatore; Peart, Jason N

    2012-01-01

    Opioid peptides and their G protein-coupled receptors (GPCRs) are important regulators within the cardiovascular system, implicated in modulation of electrophysiological function, heart rate, myocardial inotropy, vascular function, and cellular stress resistance. The opioid system is also involved in cardiovascular development, adaptation to injury and effects of advanced age. The significant roles of opioids are emphasized by the observation that the heart produces prodynorphin and proenkephalin, which are enzymatically processed from small to large active polypeptides. Indeed, depending on species, cardiac preproenkephalin mRNA levels are comparable to or higher than those found in the central nervous system. This review highlights and discusses current knowledge and recent findings regarding physiological and pathophysiological modulation of the heart and vessels by the opioid receptor system.

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

    Priyank Sethi

    2014-01-01

    Full Text Available 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.

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

    Özlem Özorak

    2010-09-01

    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.

  11. Analgesic Effects of Bee Venom Derived Phospholipase A2 in a Mouse Model of Oxaliplatin-Induced Neuropathic Pain

    Dongxing Li

    2015-06-01

    Full Text Available A single infusion of oxaliplatin, which is widely used to treat metastatic colorectal cancer, induces specific sensory neurotoxicity signs that are triggered or aggravated when exposed to cold or mechanical stimuli. Bee Venom (BV has been traditionally used in Korea to treat various pain symptoms. Our recent study demonstrated that BV alleviates oxaliplatin-induced cold allodynia in rats, via noradrenergic and serotonergic analgesic pathways. In this study, we have further investigated whether BV derived phospholipase A2 (bvPLA2 attenuates oxaliplatin-induced cold and mechanical allodynia in mice and its mechanism. The behavioral signs of cold and mechanical allodynia were evaluated by acetone and a von Frey hair test on the hind paw, respectively. The significant allodynia signs were observed from one day after an oxaliplatin injection (6 mg/kg, i.p.. Daily administration of bvPLA2 (0.2 mg/kg, i.p. for five consecutive days markedly attenuated cold and mechanical allodynia, which was more potent than the effect of BV (1 mg/kg, i.p.. The depletion of noradrenaline by an injection of N-(2-chloroethyl-N-ethyl-2-bromobenzylamine hydrochloride (DSP4, 50 mg/kg, i.p. blocked the analgesic effect of bvPLA2, whereas the depletion of serotonin by injecting DL-p-chlorophenylalanine (PCPA, 150 mg/kg, i.p. for three successive days did not. Furthermore, idazoxan (α2-adrenegic receptor antagonist, 1 mg/kg, i.p. completely blocked bvPLA2-induced anti-allodynic action, whereas prazosin (α1-adrenegic antagonist, 10 mg/kg, i.p. did not. These results suggest that bvPLA2 treatment strongly alleviates oxaliplatin-induced acute cold and mechanical allodynia in mice through the activation of the noradrenergic system, via α2-adrenegic receptors, but not via the serotonergic system.

  12. Analgesic Effects of Bee Venom Derived Phospholipase A2 in a Mouse Model of Oxaliplatin-Induced Neuropathic Pain

    Li, Dongxing; Lee, Younju; Kim, Woojin; Lee, Kyungjin; Bae, Hyunsu; Kim, Sun Kwang

    2015-01-01

    A single infusion of oxaliplatin, which is widely used to treat metastatic colorectal cancer, induces specific sensory neurotoxicity signs that are triggered or aggravated when exposed to cold or mechanical stimuli. Bee Venom (BV) has been traditionally used in Korea to treat various pain symptoms. Our recent study demonstrated that BV alleviates oxaliplatin-induced cold allodynia in rats, via noradrenergic and serotonergic analgesic pathways. In this study, we have further investigated whether BV derived phospholipase A2 (bvPLA2) attenuates oxaliplatin-induced cold and mechanical allodynia in mice and its mechanism. The behavioral signs of cold and mechanical allodynia were evaluated by acetone and a von Frey hair test on the hind paw, respectively. The significant allodynia signs were observed from one day after an oxaliplatin injection (6 mg/kg, i.p.). Daily administration of bvPLA2 (0.2 mg/kg, i.p.) for five consecutive days markedly attenuated cold and mechanical allodynia, which was more potent than the effect of BV (1 mg/kg, i.p.). The depletion of noradrenaline by an injection of N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine hydrochloride (DSP4, 50 mg/kg, i.p.) blocked the analgesic effect of bvPLA2, whereas the depletion of serotonin by injecting DL-p-chlorophenylalanine (PCPA, 150 mg/kg, i.p.) for three successive days did not. Furthermore, idazoxan (α2-adrenegic receptor antagonist, 1 mg/kg, i.p.) completely blocked bvPLA2-induced anti-allodynic action, whereas prazosin (α1-adrenegic antagonist, 10 mg/kg, i.p.) did not. These results suggest that bvPLA2 treatment strongly alleviates oxaliplatin-induced acute cold and mechanical allodynia in mice through the activation of the noradrenergic system, via α2-adrenegic receptors, but not via the serotonergic system. PMID:26131771

  13. Analgesic effect of high intensity focused ultrasound in patients with advanced pancreatic cancer

    Xinjin Tan; Jian Chen; Li Ren; Ruilu Lin; Zailian Chen

    2013-01-01

    Objective:The aim of this study was to evaluate the analgesic ef ect of high intensity focused ultrasound (HIFU) in patients with advanced pancreatic cancer. Methods:A total of 106 patients with advanced pancreatic cancer accompanied by abdominal pain were treated by HIFU. Pain intensities and quantities of morphine consumption before and after treatment were observed and compared. Results:The average pain intensities before treatment, and at d3, d7 after treatment were 5.80 ± 2.14, 2.73 ± 2.68, 2.45 ± 2.43 respectively (P<0.01). Fifty-nine cases (55.7%) got to extremely ef ective, and 29 cases (27.4%) ef ective. Total ef icient rate was 83.0%. The average quantities of morphine consumption before and after treatment in the patients with grade III pain were 114.9 ± 132.5 mg, 16.8 ± 39.7 mg each person everyday respectively (P<0.01). Conclusion:HIFU can relieve pain suf ered by patients with pancreatic cancer ef ectively. It is a new adjuvant treatment for pancreatic cancer pain.

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

    Víctor Molina D.

    2014-09-01

    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.

  15. Analgesic effect of extracts of Alpinia galanga rhizome in mice%大高良姜根茎提取物对小鼠的镇痛作用

    Sahana Devadasa Acharya; Sheetal Dinkar Ullal; Shivaraj Padiyar; Yalla Durga Rao; Kousthubha Upadhyaya; Durga Pillai; Vishnu Raj

    2011-01-01

    , mice in the five groups with six in each received three different doses of ethanolic extracts of dried rhizome of AG suspended in 2% gum acacia orally, morphine subcutaneously and 2% gum acacia orally, respectively. Reaction time was observed after administration of vehicle or drugs. For the hot-plate test after naloxone pretreatment, mice in the five groups received naloxone subcutaneously 30 min prior to the administration of vehicle or drugs and reaction time was observed as explained above. In the writhing test, writhes were induced by injecting acetic acid intraperitoneally in another 30 mice which were randomly allocated to five groups of six in each and received three different doses of ethanolic extracts of dried rhizome of AG suspended in 2% gum acacia, aspirin suspended in 2% gum acacia and 2% gum acacia orally, respectively. The mice were observed individually for a period of 15 min and the number of writhes was recorded for each animal.Results: AG treatment significantly increased the latency period in the hot-plate test at all three doses at 30, 60, 90 and 120 min time intervals compared with control group (P<0.05 or P<0.01). Naloxone pretreatment significantly reduced the latency period in hot-plate test for both AG and morphine groups as compared with corresponding groups that did not receive naloxone pretreatment (P<0. 05 or P<0. 01). AG at all doses significantly reduced the number of writhes compared with control group (P<0.01).Conclusion: The study confirmed the analgesic effect of AG rhizome and hence justified its use in ethnomedicine for the treatment of pain due to various causes. The probable mechanism of its analgesic action may be central as well as peripheral.

  16. Qigong Effects on Heart Rate Variability and Peripheral Vasomotor Responses.

    Chang, Mei-Ying

    2015-11-01

    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.

  17. Activation of κ Opioid Receptors in Cutaneous Nerve Endings by Conorphin-1, a Novel Subtype-Selective Conopeptide, Does Not Mediate Peripheral Analgesia.

    Deuis, Jennifer R; Whately, Ella; Brust, Andreas; Inserra, Marco C; Asvadi, Naghmeh H; Lewis, Richard J; Alewood, Paul F; Cabot, Peter J; Vetter, Irina

    2015-10-21

    Selective activation of peripheral κ opioid receptors (KORs) may overcome the dose-limiting adverse effects of conventional opioid analgesics. We recently developed a vicinal disulfide-stabilized class of peptides with subnanomolar potency at the KOR. The aim of this study was to assess the analgesic effects of one of these peptides, named conorphin-1, in comparison with the prototypical KOR-selective small molecule agonist U-50488, in several rodent pain models. Surprisingly, neither conorphin-1 nor U-50488 were analgesic when delivered peripherally by intraplantar injection at local concentrations expected to fully activate the KOR at cutaneous nerve endings. While U-50488 was analgesic when delivered at high local concentrations, this effect could not be reversed by coadministration with the selective KOR antagonist ML190 or the nonselective opioid antagonist naloxone. Instead, U-50488 likely mediated its peripheral analgesic effect through nonselective inhibition of voltage-gated sodium channels, including peripheral sensory neuron isoforms NaV1.8 and NaV1.7. Our study suggests that targeting the KOR in peripheral sensory nerve endings innervating the skin is not an alternative analgesic approach.

  18. Gabapentin, an Analgesic Used Against Cancer-Associated Neuropathic Pain: Effects on Prostate Cancer Progression in an In Vivo Rat Model.

    Bugan, Ilknur; Karagoz, Zeynep; Altun, Seyhan; Djamgoz, Mustafa B A

    2016-03-01

    A major problem associated with clinical management of cancer is controlling the accompanying pain, and various analgesics are in common use for this purpose. Recent evidence suggests that some of the targets of analgesics, such as ion channels and receptors, may also be involved in the cancer process, thereby raising the possibility that such use of some analgesics may impact upon cancer itself. The main aim of this study was to determine whether gabapentin, a common adjuvant analgesic in current use against cancer-associated neuropathic pain, would affect tumour development and progression in vivo. The Dunning rat model of prostate cancer was used. Strongly metastatic Mat-LyLu cells were implanted subcutaneously into syngeneic Copenhagen rats which were then treated every other day with 4.6-16.8 μg/kg gabapentin by gavage. Primary tumourigenesis was monitored daily. Lung metastases were counted and measured after killing the rats 21 days later. Gabapentin had no effect on primary tumourigenesis but produced dose-dependent effects on lung metastasis. Whilst 4.6 μg/kg had no effect, 9.1 μg/kg gabapentin decreased the number of lung metastases significantly by 64%. In contrast, 16.8 μg/kg gabapentin promoted metastasis significantly by 112% and showed a strong tendency to shorten mean survival time. It is concluded that gabapentin prescribed to cancer patients against pain could impact upon the cancer process itself.

  19. Effects of ocular transverse chromatic aberration on peripheral word identification.

    Yang, Shun-Nan; Tai, Yu-chi; Laukkanen, Hannu; Sheedy, James E

    2011-11-01

    Transverse chromatic aberration (TCA) smears the retinal image of peripheral stimuli. We previously found that TCA significantly reduces the ability to recognize letters presented in the near fovea by degrading image quality and exacerbating crowding effect from adjacent letters. The present study examined whether TCA has a significant effect on near foveal and peripheral word identification, and whether within-word orthographic facilitation interacts with TCA effect to affect word identification. Subjects were briefly presented a 6- to 7-letter word of high or low frequency in each trial. Target words were generated with weak or strong horizontal color fringe to attenuate the TCA in the right periphery and exacerbate it in the left. The center of the target word was 1°, 2°, 4°, and 6° to the left or right of a fixation point. Subject's eye position was monitored with an eye-tracker to ensure proper fixation before target presentation. They were required to report the identity of the target word as soon and accurately as possible. Results show significant effect of color fringe on the latency and accuracy of word recognition, indicating existing TCA effect. Observed TCA effect was more salient in the right periphery, and was affected by word frequency more there. Individuals' subjective preference of color-fringed text was correlated to the TCA effect in the near periphery. Our results suggest that TCA significantly affects peripheral word identification, especially when it is located in the right periphery. Contextual facilitation such as word frequency interacts with TCA to influence the accuracy and latency of word recognition.

  20. Antinociceptive effects of analgesic-antitumor peptide (AGAP), a neurotoxin from the scorpion Buthus martensii Karsch, on formalin-induced inflammatory pain through a mitogen-activated protein kinases-dependent mechanism in mice.

    Mao, Qinghong; Ruan, Jiaping; Cai, Xueting; Lu, Wuguang; Ye, Juan; Yang, Jie; Yang, Yang; Sun, Xiaoyan; Cao, Junli; Cao, Peng

    2013-01-01

    In the present study, we investigated the anti-nociceptive effect and the underlying mechanism of the analgesic-antitumor peptide (AGAP), a neurotoxin from the scorpion Buthus martensii Karsch. AGAP in doses of 0.2, 1 and 5 µg was injected intraplantarly (i.pl.) before formalin injection 10 min at the same site. The suppression by intraplantar injection of AGAP on formalin-induced spontaneous nociceptive behaviors was investigated. The results show that AGAP could dose-dependently inhibit formalin-induced two-phase spontaneous flinching response. To investigate the mechanism of action of treatment with AGAP in inflammatory pain, the expressions of peripheral and spinal phosphorylated mitogen-activated protein kinases (phospho-MAPKs) including p-p38, p-ERK and p-JNK were examined. We found that formalin increased the expressions of peripheral and spinal MAPKs, which were prevented by pre-intraplantar injection of AGAP in inflammation pain model in mice. AGAP could also decrease the expression of spinal Fos induced by formalin. Furthermore, combinations the lower doses of the inhibitors of MAPKs (U0126, SP600125, or SB203580 0.1 µg) with the lower dose of AGAP (0.2 µg), the results suggested that AGAP could potentiate the effects of the inhibitors of MAPKs on the inflammatory pain. The present results indicate that pre-intraplantar injection of AGAP prevents the inflammatory pain induced by formalin through a MAPKs-mediated mechanism in mice.

  1. Antinociceptive effects of analgesic-antitumor peptide (AGAP, a neurotoxin from the scorpion Buthus martensii Karsch, on formalin-induced inflammatory pain through a mitogen-activated protein kinases-dependent mechanism in mice.

    Qinghong Mao

    Full Text Available In the present study, we investigated the anti-nociceptive effect and the underlying mechanism of the analgesic-antitumor peptide (AGAP, a neurotoxin from the scorpion Buthus martensii Karsch. AGAP in doses of 0.2, 1 and 5 µg was injected intraplantarly (i.pl. before formalin injection 10 min at the same site. The suppression by intraplantar injection of AGAP on formalin-induced spontaneous nociceptive behaviors was investigated. The results show that AGAP could dose-dependently inhibit formalin-induced two-phase spontaneous flinching response. To investigate the mechanism of action of treatment with AGAP in inflammatory pain, the expressions of peripheral and spinal phosphorylated mitogen-activated protein kinases (phospho-MAPKs including p-p38, p-ERK and p-JNK were examined. We found that formalin increased the expressions of peripheral and spinal MAPKs, which were prevented by pre-intraplantar injection of AGAP in inflammation pain model in mice. AGAP could also decrease the expression of spinal Fos induced by formalin. Furthermore, combinations the lower doses of the inhibitors of MAPKs (U0126, SP600125, or SB203580 0.1 µg with the lower dose of AGAP (0.2 µg, the results suggested that AGAP could potentiate the effects of the inhibitors of MAPKs on the inflammatory pain. The present results indicate that pre-intraplantar injection of AGAP prevents the inflammatory pain induced by formalin through a MAPKs-mediated mechanism in mice.

  2. Effectiveness of combined alprostadil and pancreatic kininogenas in treating gerontal diabetic peripheral neuropathy

    张玉

    2013-01-01

    Objective To observe the clinical effectiveness of alprostadil combined with pancreatic kininogenas in the treatment of gerontal diabetic peripheral neuropathy.Methods Totally 90 gerontal patients with diabetic peripheral neuropathy were randomly divided into three

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

    Stephanie Anderson

    2010-09-01

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

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

    Md Shamsuddin Sultan Khan

    2013-04-01

    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.

  5. Analgesic effect of parecoxib and flurbiprofen axetil for patients undergoing laparoscopic cholecystectomy and their influences on platelet aggregation

    JI Fu-hai; JIN Xin; YANG Jian-ping; ZAN Li-li

    2010-01-01

    It is known that opioids produce postoperative analgesia,while it can also cause, especially in large doses, side effects like nausea, vomiting, constipation, syncope, skin itching, urinary retention and even respiratory inhibition.These factors have all greatly limited its clinical use for treating postoperative pain. Meanwhile, non-steroidal anti-inflammatory drags (NSAIDs) play an increasingly important role in postoperative analgesia. Some studies suggest that NSAIDS may be neural protective in cerebral ischemic conditions.1 Flurbiprofen axetil, which utilizes a lipid microsphere drag delivery system, may promote accumulation of flurbiprofen granular at inflammatory lesion sites and absorption by inflammatory cells,2 both factors which help to effectively target therapy. Parecoxib is the first selective cyclooxygenase-2 (COX-2) inhibitor available for intravenous injection, which is beneficial to patients susceptible to NSAIDs3 and those prone to gastrointestinal disturbances like perforation, ulcers, and bleeding.4 This investigation assesses the analgesic effect of parecoxib and flurbiprofen axetil for patients undergoing laparoscopic cholecystectomy and their influence on platelet aggregation in order to offer some guidance for clinic practice.

  6. Intrathecal clonidine for postoperative analgesia in elderly patients: the influence of baricity on hemodynamic and analgesic effects.

    Baker, Amir; Klimscha, Walter; Eisenach, James C; Li, Xin-Hui; Wildling, Eckart; Menth-Chiari, Wolfgang A; Chiari, Astrid I

    2004-07-01

    Intrathecal (IT) clonidine is an effective analgesic, but it also produces hemodynamic depression and sedation which are likely to be related to IT clonidine's cephalad spread within the cerebrospinal fluid. We hypothesized that IT clonidine's side effects could be reduced without compromising the duration and quality of analgesia by injecting clonidine IT in a hyperbaric solution and elevating the patient's trunk. We prospectively randomized 30 elderly patients to receive IT 150 microg of either isobaric (ISO) or hyperbaric (HYPER) clonidine for postoperative analgesia after surgical repair of traumatic hip fracture. Hemodynamics, IV fluid administration, visual analog pain scores, sedation scores, and clonidine cerebrospinal fluid levels were recorded at fixed intervals. Patients in the ISO group required significantly more crystalloid fluid administration (median, 2500 mL; range, 1500-3000 mL) than those in the HYPER group (median, 1500; range, 500-3000 mL) to maintain adequate arterial blood pressure (P ISO than in the HYPER group (P ISO (median, 400 min; range, 115-400 min) than in the HYPER (median, 265 min; range, 205-400 min) group (P < 0.05). Sedation scores did not differ between groups. We conclude that increasing the baricity of IT clonidine solution in the conditions of our experiment reduces hemodynamic side effects but also analgesia from IT administered clonidine.

  7. Comparative Study on the Analgesic Effects of Different Moxibustion Methods with Tai-yi Moxa Stick in Treating Primary Dysmenorrhea

    Wu Jiu-long; Wang Yu-fan; Zhang Jian-bin; Wang Ling-ling; Chen Hong-yu; Tang Yi-chun; Ma Xiao-yu; Huan Jia-hui; Chen Ruo-yang; Mo Hui; Xu Xiu-zhu; Shen Xiao-jing

    2014-01-01

    Objective: To compare the therapeutic effects of two different moxibustion methods both with tai-yi moxa stick in treating primary dysmenorrhea. Methods: Forty-three patients were randomized into two groups by the random number table according to their treatment orders. The causalgic group was intervened by causalgic stimulation with tai-yi moxa stick while the tepid group was treated by mild thermal stimulation with tai-yi moxa stick. Shiqizhui (EX-B 8) was selected for both groups. Visual analogue scale (VAS) was used for observation before and during the treatment by every 10 min to compare the clinical efficacies between the two groups. Results: Before treatment, there was no statistically significant difference in pain intensity between the two groups (P>0.05). After treatment, both groups achieved significant improvements in pain intensity (P0.05), but the difference was enlarged comparing with that before treatment. The pain relief during the first 10 min of treatment was slower in the causalgic group than that in the tepid group. However, during the later 20 min, the pain relief in the calsalgia group gradually outpaced that in the tepid group. Conclusion: The two moxibustion methods with tai-yi moxa stick both have a good instant analgesic effect in treating primary dysmenorrhea. For patients with primary dysmenorrhea, if 30 min is regarded as the treatment time, mild stimulation was suggested to be used for the first 10 min, and causalgic stimulation for the later 20 min to achieve a better curative effect.

  8. Effect of PACAP in Central and Peripheral Nerve Injuries

    Andras Buki

    2012-07-01

    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.

  9. Effect of PACAP in Central and Peripheral Nerve Injuries

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

    2012-01-01

    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. PMID:22942712

  10. The analgesic effect of rolipram is associated with the inhibition of the activation of the spinal astrocytic JNK/CCL2 pathway in bone cancer pain

    Guo, Chi-Hua; Bai, Lu; Wu, Huang-Hui; Yang, Jing; Cai, Guo-Hong; Wang, Xin; Wu, Sheng-Xi; Ma, Wei

    2016-01-01

    Bone cancer pain (BCP) is one of the most difficult and intractable tasks for pain management, which is associated with spinal 'neuron-astrocytic' activation. The activation of the c-Jun N-terminal kinase (JNK)/chemokine (C-C motif) ligand (CCL2) signaling pathway has been reported to be critical for neuropathic pain. Rolipram (ROL), a selective phosphodiesterase 4 inhibitor, possesses potent anti-inflammatory and anti-nociceptive activities. The present study aimed to investigate whether the intrathecal administration of ROL has an analgesic effect on BCP in rats, and to assess whether the inhibition of spinal JNK/CCL2 pathway and astrocytic activation are involved in the analgesic effects of ROL. The analgesic effects of ROL were evaluated using the Von Frey and Hargreaves tests. Immunofluorescence staining was used to determine the number of c-Fos immunoreactive neurons, and the expression of spinal astrocytes and microglial activation on day 14 after tumor cell inoculation. Enzyme-linked immunosorbent assay (ELISA) was used to detect the expression of pro-inflammatory cytokines [interleukin (IL)-1β, IL-6 and tumor necrosis factor (TNF)-α] and chemokines (CCL2), and western blot analysis was then used to examine the spinal phosphodiesterase 4 (PDE4), ionized calcium binding adapter molecule-1 (IBA-1) and JNK levels on day 14 after tumor cell inoculation. The results revealed that ROL exerted a short-term analgesic effect in a dose-dependent manner, and consecutive daily injections of ROL exerted continuous analgesic effects. In addition, spinal 'neuron-astrocytic' activation was suppressed and was associated with the downregulation of spinal IL-1β, IL-6 and TNF-α expression, and the inhibition of PDE4B and JNK levels in the spine was also observed. In addition, the level of CCL2 was decreased in the rats with BCP. The JNK inhibitor, SP600125, decreased CCL2 expression and attenuated pain behavior. Following co-treatment with ROL and SP600125, no significant

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

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

    2012-01-01

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

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

    Eduardo A Garza Villarreal

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

  13. Analgesic effect of propofol combined with fentanyl or dezocine on polypectomy under colonoscope as well as the neurohumoral changes

    Dong-Wu Xie

    2016-01-01

    Objective:To analyze the analgesic effect of propofol combined with fentanyl or dezocine on polypectomy under colonoscope as well as the neurohumoral changes.Methods:A total of 116 patients who received polypectomy under colonoscope in our hospital between February 2013 and February 2016 were selected as the research subjects and randomly divided into observation group and control group, and after polypectomy under colonoscope, control group received fentanyl analgesia and observation group received dezocine analgesia. The levels of indole neurotransmitters, pain-related indexes, inflammatory factors and stress hormones in serum were compared between two groups of patients 6 h after operation.Results:Six hours after operation, 5-HTP, 5-HIAA, 5-HT, SP, PGE2, NGF, NPY, IL-1β, IL-6, IL-8, TNF-α, PCT, HSP70, Cor, DA, ALD, NE and ACTH content in serum of observation group were significantly lower than those of control group.Conclusions:Propofol combined with dezocine can more effectively inhibit the postoperative pain in patients with polypectomy under colonoscope, and also stabilize neurohumoral balance.

  14. Intravenous administration of lidocaine directly acts on spinal dorsal horn and produces analgesic effect: An in vivo patch-clamp analysis

    Miyuki Kurabe; Hidemasa Furue; Tatsuro Kohno

    2016-01-01

    Intravenous lidocaine administration produces an analgesic effect in various pain states, such as neuropathic and acute pain, although the underlying mechanisms remains unclear. Here, we hypothesized that intravenous lidocaine acts on spinal cord neurons and induces analgesia in acute pain. We therefore examined the action of intravenous lidocaine in the spinal cord using the in vivo patch-clamp technique. We first investigated the effects of intravenous lidocaine using behavioural measures i...

  15. Effect of Large Dose Methylcobalamin on Diabetic Peripheral Neuropathy

    2005-01-01

    The effects of large dose methylcobalamin injection on diabetic peripheral neuropathy in patients were observed to observe the subjective symptom of diabetic perpheral neuropathy (DPN) patients and detect the motor nerve conduction velocity (MCV) and sense nerve conduction velocity (SCV). Fifteen patients were received large dose methylcobalamin injection for two weeks as treatment group, another eleven patients were received muscular injection VitB1 100mg/ d, VitB12 500ug/ d for two weeks as control group. After 2 weeks treatment the subjective symptoms and signs were significantly improved with a total effective rate of 82.9% in the treatment group however the effective rate only has 52.0% in the control group. The result has obvious difference in statistics nerve MCV in median common peroneal nerve, SCV in median and superficial peroneal nerve were improved significantly in the treatment group and no such changes were observed in the control group. So, large dose methylcobalamin is an effective and safe agent for treatment of diabetic peripheral neuropathy.

  16. Peripheral Biomarkers of Parkinson's Disease Progression and Pioglitazone Effects.

    Simon, David K; Simuni, Tanya; Elm, Jordan; Clark-Matott, Joanne; Graebner, Allison K; Baker, Liana; Dunlop, Susan R; Emborg, Marina; Kamp, Cornelia; Morgan, John C; Ross, G Webster; Sharma, Saloni; Ravina, Bernard

    2015-01-01

    Pioglitazone, an oral hypoglycemic agent, recently failed to show promise as a disease-modifying agent in a 44-week phase 2 placebo-controlled study in 210 Parkinson's disease (PD) subjects. We analyzed peripheral biomarkers, including leukocyte PGC-1α and target gene expression, plasma interleukin 6 (IL-6) as a marker of inflammation, and urine 8-hydroxydeoxyguanosine (8OHdG) as a marker of oxidative DNA damage. Baseline or changes from baseline in biomarker levels were not associated with the rate of progression of PD. Pioglitazone did not significantly alter biomarker levels. Other agents that more effectively target these mechanisms remain of potential interest as disease modifying therapies in PD.

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

    Reza Heidari

    2010-04-01

    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.

  18. Flurbiprofen axetil reduces postoperative sufentanil consumption and enhances postoperative analgesic effects in patients with colorectal cancer surgery.

    Lin, Xue; Zhang, Ruiqin; Xing, Jingchun; Gao, Xiaocui; Chang, Pan; Li, Wenzhi

    2014-01-01

    To investigate the effects of different strategies of flurbiprofen axetil (FA) administration on postoperative pain and sufentanil (SF) consumption after open colorectal cancer (CRC) surgery. Forty patients undergoing elective CRC resection were divided into two groups (n = 20 each). Patients in the F50+50 group received 50 mg of intravenous FA 30 min before skin incision and six hours after the first dose; patients in the F100 group received 100 mg of intravenous FA 30 min before skin incision. Perioperative plasma FA (CFA) and SF concentrations (CSF) were determined. Analgesic and sedative efficacy were evaluated using the visual analogue scale (VAS), Bruggman Comfort Scale (BCS), and Ramsay sedation scale. The time to the first PCIA trigger, the number of patients that pressed the PCIA trigger within 24 h after surgery, and the cumulative doses of SF consumption within 6 and 24 h after surgery were recorded. At postoperative 6 and 24 h, CFA was significantly higher, CSF was significantly lower, and the number of patients that pressed the PCIA trigger and the consumption of SF were significantly lower in the F50+50 group compared with the F100 group. At postoperative 4 h, VAS and BCS were significantly lower in the F50+50 group compared with the F100 group (P < 0.05). An administration strategy that maintains a relatively high plasma FA concentration at 6-24 h post-operatively may reduce postoperative inflammatory pain and SF-requirement in patients undergoing CRC resection.

  19. The analgesic effect on neuropathic pain of retrogradely transported botulinum neurotoxin A involves Schwann cells and astrocytes.

    Sara Marinelli

    Full Text Available In recent years a growing debate is about whether botulinum neurotoxins are retrogradely transported from the site of injection. Immunodetection of cleaved SNAP-25 (cl-SNAP-25, the protein of the SNARE complex targeted by botulinum neurotoxin serotype A (BoNT/A, could represent an excellent approach to investigate the mechanism of action on the nociceptive pathways at peripheral and/or central level. After peripheral administration of BoNT/A, we analyzed the expression of cl-SNAP-25, from the hindpaw's nerve endings to the spinal cord, together with the behavioral effects on neuropathic pain. We used the chronic constriction injury of the sciatic nerve in CD1 mice as animal model of neuropathic pain. We evaluated immunostaining of cl-SNAP-25 in the peripheral nerve endings, along the sciatic nerve, in dorsal root ganglia and in spinal dorsal horns after intraplantar injection of saline or BoNT/A, alone or colocalized with either glial fibrillar acidic protein, GFAP, or complement receptor 3/cluster of differentiation 11b, CD11b, or neuronal nuclei, NeuN, depending on the area investigated. Immunofluorescence analysis shows the presence of the cl-SNAP-25 in all tissues examined, from the peripheral endings to the spinal cord, suggesting a retrograde transport of BoNT/A. Moreover, we performed in vitro experiments to ascertain if BoNT/A was able to interact with the proliferative state of Schwann cells (SC. We found that BoNT/A modulates the proliferation of SC and inhibits the acetylcholine release from SC, evidencing a new biological effect of the toxin and further supporting the retrograde transport of the toxin along the nerve and its ability to influence regenerative processes. The present results strongly sustain a combinatorial action at peripheral and central neural levels and encourage the use of BoNT/A for the pathological pain conditions difficult to treat in clinical practice and dramatically impairing patients' quality of life.

  20. The Analgesic Effect on Neuropathic Pain of Retrogradely Transported botulinum Neurotoxin A Involves Schwann Cells and Astrocytes

    Ricordy, Ruggero; Uggenti, Carolina; Tata, Ada Maria; Luvisetto, Siro; Pavone, Flaminia

    2012-01-01

    In recent years a growing debate is about whether botulinum neurotoxins are retrogradely transported from the site of injection. Immunodetection of cleaved SNAP-25 (cl-SNAP-25), the protein of the SNARE complex targeted by botulinum neurotoxin serotype A (BoNT/A), could represent an excellent approach to investigate the mechanism of action on the nociceptive pathways at peripheral and/or central level. After peripheral administration of BoNT/A, we analyzed the expression of cl-SNAP-25, from the hindpaw’s nerve endings to the spinal cord, together with the behavioral effects on neuropathic pain. We used the chronic constriction injury of the sciatic nerve in CD1 mice as animal model of neuropathic pain. We evaluated immunostaining of cl-SNAP-25 in the peripheral nerve endings, along the sciatic nerve, in dorsal root ganglia and in spinal dorsal horns after intraplantar injection of saline or BoNT/A, alone or colocalized with either glial fibrillar acidic protein, GFAP, or complement receptor 3/cluster of differentiation 11b, CD11b, or neuronal nuclei, NeuN, depending on the area investigated. Immunofluorescence analysis shows the presence of the cl-SNAP-25 in all tissues examined, from the peripheral endings to the spinal cord, suggesting a retrograde transport of BoNT/A. Moreover, we performed in vitro experiments to ascertain if BoNT/A was able to interact with the proliferative state of Schwann cells (SC). We found that BoNT/A modulates the proliferation of SC and inhibits the acetylcholine release from SC, evidencing a new biological effect of the toxin and further supporting the retrograde transport of the toxin along the nerve and its ability to influence regenerative processes. The present results strongly sustain a combinatorial action at peripheral and central neural levels and encourage the use of BoNT/A for the pathological pain conditions difficult to treat in clinical practice and dramatically impairing patients’ quality of life. PMID:23110146

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

    Yong Ye

    2012-09-01

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

  2. Intravenous administration of lidocaine directly acts on spinal dorsal horn and produces analgesic effect: An in vivo patch-clamp analysis.

    Kurabe, Miyuki; Furue, Hidemasa; Kohno, Tatsuro

    2016-05-18

    Intravenous lidocaine administration produces an analgesic effect in various pain states, such as neuropathic and acute pain, although the underlying mechanisms remains unclear. Here, we hypothesized that intravenous lidocaine acts on spinal cord neurons and induces analgesia in acute pain. We therefore examined the action of intravenous lidocaine in the spinal cord using the in vivo patch-clamp technique. We first investigated the effects of intravenous lidocaine using behavioural measures in rats. We then performed in vivo patch-clamp recording from spinal substantia gelatinosa (SG) neurons. Intravenous lidocaine had a dose-dependent analgesic effect on the withdrawal response to noxious mechanical stimuli. In the electrophysiological experiments, intravenous lidocaine inhibited the excitatory postsynaptic currents (EPSCs) evoked by noxious pinch stimuli. Intravenous lidocaine also decreased the frequency, but did not change the amplitude, of both spontaneous and miniature EPSCs. However, it did not affect inhibitory postsynaptic currents. Furthermore, intravenous lidocaine induced outward currents in SG neurons. Intravenous lidocaine inhibits glutamate release from presynaptic terminals in spinal SG neurons. Concomitantly, it hyperpolarizes postsynaptic neurons by shifting the membrane potential. This decrease in the excitability of spinal dorsal horn neurons may be a possible mechanism for the analgesic action of intravenous lidocaine in acute pain.

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

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

    2011-12-06

    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.

  4. Topical Anti-Inflammatory and Analgesic Effects of Multiple Applications of S(+)-Flurbiprofen Plaster (SFPP) in a Rat Adjuvant-Induced Arthritis Model.

    Sugimoto, Masanori; Toda, Yoshihisa; Hori, Miyuki; Mitani, Akiko; Ichihara, Takahiro; Sekine, Shingo; Kaku, Shinsuke; Otsuka, Noboru; Matsumoto, Hideo

    2016-06-01

    Preclinical Research The aim of this study was to evaluate the efficacy of multiple applications of S(+)-flurbiprofen plaster (SFPP), a novel Nonsteroidal anti-inflammatory drug (NSAID) patch, for the alleviation of inflammatory pain and edema in rat adjuvant-induced arthritis (AIA) model as compared to other NSAID patches. The AIA model was induced by the injection of Mycobacterium butyricum and rats were treated with a patch (1.0 cm × 0.88 cm) containing each NSAID (SFP, ketoprofen, loxoprofen, diclofenac, felbinac, flurbiprofen, or indomethacin) applied to the paw for 6 h per day for 5 days. The pain threshold was evaluated using a flexion test of the ankle joint, and the inflamed paw edema was evaluated using a plethysmometer. cyclooxygenase (COX)-1 and COX-2 inhibition was evaluated using human recombinant proteins. Multiple applications of SFPP exerted a significant analgesic effect from the first day of application as compared to the other NSAID patches. In terms of paw edema, SFPP decreased edema from the second day after application, Multiple applications of SFPP were superior to those of other NSAID patches, in terms of the analgesic effect with multiple applications. These results suggest that SFPP may be a beneficial patch for providing analgesic and anti-inflammatory effects clinically. Drug Dev Res 77 : 206-211, 2016. © 2016 The Authors Drug Development Research Published by Wiley Periodicals, Inc.

  5. Nonnarcotic analgesics and hypertension.

    Gaziano, J Michael

    2006-05-01

    In 2004, individuals in the United States spent >$2.5 billion on over-the-counter (OTC) nonsteroidal anti-inflammatory drugs (NSAIDs) and filled >100 million NSAID prescriptions. The most commonly used OTC analgesics include aspirin, acetaminophen, and nonaspirin NSAIDs. Nonnarcotic analgesics are generally considered safe when used as directed but do have the potential to increase blood pressure in patients with hypertension treated with antihypertensives. This is important because hypertension alone has been correlated with an increased risk of cardiovascular disease or stroke. Small increases in blood pressure in patients with hypertension also have been shown to increase cardiovascular morbidity and mortality. Therefore, when nonnarcotic analgesics are taken by patients with hypertension, there may be important implications. This review explores the potential connection among analgesic agents, blood pressure, and hypertension, and discusses possible mechanisms by which analgesics might cause increases in blood pressure. This is followed by a summary of data on the relation between analgesics and blood pressure from both observational and randomized trials.

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

    Amir Farshchi

    2010-05-01

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

  7. Analgesic effects of an ethanol extract of the fruits of Xylopia aethiopica (Dunal A. Rich (Annonaceae and the major constituent, xylopic acid in murine models

    Eric Woode

    2012-01-01

    Full Text Available Background: Fruit extracts of Xylopia aethiopica are used traditionally in the management of pain disorders including rheumatism, headache, colic pain, and neuralgia. Little pharmacological data exists in scientific literature of the effect of the fruit extract and its major diterpene, xylopic acid, on pain. The present study evaluated the analgesic properties of the ethanol extract of X. aethiopica (XAE and xylopic acid (XA, in murine models. Materials and Methods: XAE and XA were assessed in chemical (acetic acid-induced abdominal writhing and formalin tests, thermal (Tail-flick and Hargreaves thermal hyperalgesia tests, and mechanical (Randall-Selitto paw pressure test pain models. Results: XAE and XA exhibited significant analgesic activity in all the pain models used. XAE (30-300 mg kg -1 , p.o. and XA (10-100 mg kg -1 , p.o. inhibited acetic acid-induced visceral nociception, formalin- induced paw pain (both neurogenic and inflammatory, thermal pain as well as carrageenan-induced mechanical and thermal hyperalgesia in animals. Morphine (1-10 mg kg -1 , i.p. and diclofenac (1-10 mg kg -1 , i.p., used as controls, exhibited similar anti-nociceptive activities. XAE and XA did not induce tolerance to their respective anti-nociceptive effects in the formalin test after chronic administration. Morphine tolerance did not also cross-generalize to the analgesic effects of XAE or XA. Conclusions: These findings establish the analgesic properties of the ethanol fruit extract of X. aethiopica and its major diterpene, xylopic acid.

  8. Case report: analgesic nephropathy: a soda and a powder.

    Appel, R G; Bleyer, A J; McCabe, J C

    1995-10-01

    Analgesic nephropathy has long been considered a potentially preventable cause of renal disease. Early reports were described in patients who consumed analgesics containing phenacetin. In recent data, the removal of phenacetin from analgesic preparations resulted in a reduction in analgesic-induced end stage renal disease in Europe and Australia. However, a reduction in the incidence of analgesic nephropathy has not occurred uniformly, suggesting that phenacetin is not the sole cause. Current data raise concerns regarding adverse renal effects of acetaminophen and nonsteroidal antiinflammatory drugs. Aspirin taken alone may be of least concern. The diagnosis of analgesic nephropathy is suggested in subjects with chronic renal failure, a history of daily consumption of analgesic preparations, small bumpy kidneys, and renal papillary necrosis or chronic interstitial nephritis. However, the spectrum of disease may be changing, because these agents also may increase the risk of cardiovascular disease and chronic renal disease due to nephrosclerosis, glomerulonephritis, and diabetes mellitus. Potential pathogenetic mechanisms in analgesic nephropathy include direct cellular injury induced by analgesics, prostaglandin inhibition with reduction or redistribution of renal blood flow, and interesting new concepts regarding the role of caffeine in increasing oxygen demand and reducing oxygen supply in the medulla. The primary goal of therapy is discontinuation of analgesic consumption. Because of the association between analgesic intake and uroepithelial tumors, surveillance of patients for neoplasm is suggested.

  9. Prescription trajectories and effect of total hip arthroplasty on the use of analgesics, hypnotics, antidepressants, and anxiolytics: results from a population of total hip arthroplasty patients.

    Blågestad, Tone; Nordhus, Inger H; Grønli, Janne; Engesæter, Lars B; Ruths, Sabine; Ranhoff, Anette H; Bjorvatn, Bjørn; Pallesen, Ståle

    2016-03-01

    Total hip arthroplasty (THA) has been shown to reduce pain and improve function. In addition, it is suggested that THA improves sleep and alleviates symptoms of anxiety and depression. Patients with chronic pain are frequent users of analgesic and psychotropic drugs and thereby risk adverse drug events. The impact of THA on such drug use has not been thoroughly investigated. Based on merged data from the Norwegian Prescription Database and the Norwegian Arthroplasty Register, this study sought to investigate redeemed medications in a complete population (N = 39,688) undergoing THA in 2005 to 2011. User rates and redeemed drug volume of analgesics (nonsteroid anti-inflammatory drugs (NSAIDs), opioids, and nonopioids) and psychotropics (hypnotics, anxiolytics, and antidepressants) were calculated for 4 quarters before and 4 quarters after surgery. We analysed preoperative prescription trends (Q1 vs Q4), postoperative prescription (Q4 vs Q5), and long-term effect of surgery (Q4 vs Q8). Before surgery, use of all drug groups increased from Q1 to Q4. Use of opioids, nonopioids, and hypnotics dramatically increased from Q4 to Q5. Long-term (Q4 vs Q8) surgery reduced prescriptions of analgesics, hypnotics, and anxiolytics, but not antidepressants. Overall, the present results extend the positive effects of THA to include reduced reliance on medication to alleviate symptoms.

  10. Purification, characterization and functional expression of a new peptide with an analgesic effect from Chinese scorpion Buthus martensii Karsch (BmK AGP-SYPU1).

    Wang, Yu; Wang, Li; Cui, Yong; Song, Yong-Bo; Liu, Yan-Feng; Zhang, Rong; Wu, Chun-Fu; Zhang, Jing-Hai

    2011-07-01

    In this study, a new peptide named BmK AGP-SYPU1 with an analgesic effect was purified from the venom of Chinese scorpion Buthus martensi Karsch (BmK) through a four-step chromatographic process. The mouse twisting test was used to identify the target peptides in every separation step. The purified BmK AGP-SYPU1 was further qualified by RP-HPLC and HPCE. The molecular mass determined by the MALDI-4800-TOF/TOF MS for BmK AGP-SYPU1 was 7544 Da. Its primary structure of the N-terminal was obtained using Edman degradation. The gene sequence of BmK AGP-SYPU1 was cloned from the cDNA pool and genomic of scorpion glands, respectively, and then expressed in Escherichia coli. The sequence determination showed that BmK AGP-SYPU1 was composed of 66 amino acid residues with a new primary structure. The metal chelating affinity column and cation exchange chromatography were used to purify the recombinant BmK AGP-SYPU1. Consequently, the native and recombinant BmK AGP-SYPU1 showed similar analgesic effects on mice as assayed using a mouse twisting model. These results suggested that BmK AGP-SYPU1 is a new analgesic component found in the Chinese scorpion Buthus martensi Karsch.

  11. Analgesic and antihyperalgesic effects of dipyrone, meloxicam or a dipyrone-meloxicam combination in bitches undergoing ovariohysterectomy.

    Zanuzzo, Felipe S; Teixeira-Neto, Francisco J; Teixeira, Lívia R; Diniz, Miriely S; Souza, Vivian L; Thomazini, Camila M; Steagall, Paulo V M

    2015-07-01

    The analgesic and antihyperalgesic effects of dipyrone, meloxicam or a dipyrone-meloxicam combination were compared in dogs undergoing elective ovariohysterectomy. In a double-blinded, prospective, randomised design, 40 bitches premedicated with intramuscular pethidine (4 mg/kg) and anaesthetised with isoflurane received one of four intravenous treatments (n = 10 per group) before ovariohysterectomy: control (physiological saline), meloxicam (0.2 mg/kg), dipyrone (25 mg/kg) or dipyrone-meloxicam (25 mg/kg and 0.2 mg/kg, respectively). Glasgow composite measure pain scale (GCMPS) and mechanical nociceptive thresholds (MNT) were assessed before anaesthesia and at 1, 2, 3, 4, 6, 8, 12 and 24 h postoperatively. Rescue analgesia (0.5 mg/kg morphine) was administered intramuscularly if the GCMPS was ≥3. The GCMPS and MNT did not differ among groups. The frequency of rescue analgesia was significantly (P meloxicam (70%) or dipyrone-meloxicam (40%). There was a significant reduction in the total number of rescue treatments in the dypyrone (n = 5) and dipyrone-meloxicam (n = 5) groups when compared with the control (n = 17) and meloxicam (n = 19) groups. Meloxicam and dipyrone-meloxicam significantly reduced the percentage of animals exhibiting severe pain during MNT measurements (30% and 0%, respectively) compared with the control group (50%). Dipyrone produced superior analgesia (reduced morphine consumption), while meloxicam produced better antihyperalgesia (fewer episodes of severe pain) in contrast to controls. When used in tandem, the beneficial effects were combined.

  12. Therapeutic Effect Observations on Individualized Treatment of Peripheral Facial Palsy

    何希俊; 谭吉林; 王本国; 郭瑞兰; 韩丑萍

    2006-01-01

    目的:观察采用个体化方案治疗周围性面瘫的疗效.方法:治疗组121例患者根据其病情特点采用个体化方案进行针刺治疗,与118例常规针灸治疗者进行对照研究,比较其疗程与疗效的差异.结果:治疗组愈显率为90.9%,对照组愈显率为69.5%,差异有显著性(P<0.01);两组各疗程愈显率比较,差异有显著性(P<0.01).结论:采用个体化方案治疗周围性面瘫效果明显优于常规针刺方法,且疗程短.%To investigate the curative effect of individualized treatment on peripheral facial paralysis. Methods:A treatment group of 121 patients was treated with acupuncture under an individualized plan based on the condition of disease. For a control study,118 patients were treated with conventional acupuncture. The courses of treatment and the curative effects were compared. Results:The cure and marked efficacy rate was 90.9% in the treatment group and 69.5% in the control group. There was a significant difference (P<0.01).There was also a significant difference in the cure and marked efficacy rate in each courses of treatment between the two groups (P<0.01). Conclusion:Individualized acupuncture treatment is better in the effect and shorter in the courses than conventional acupuncture treatment for peripheral facial paralysis.

  13. Analgesic effect of topical oral capsaicin gel in burning mouth syndrome

    Jørgensen, Mette Rose; Pedersen, Anne Marie Lynge

    2017-01-01

    OBJECTIVE: To investigate the effectiveness of repeated topical application of oral capsaicin gel in two different concentrations for relief of burning/stinging sensations in patients with burning mouth syndrome (BMS). MATERIAL AND METHODS: This randomized double-blind cross-over study included 2...

  14. Experimental studies on antipyretic, analgesic and antibacterial effects of GK 001, a poly-prescription of traditional chinese medicine

    JIANG Su-yun; ZhANG Ting-ting; DING Hong-yu

    2008-01-01

    Objective To study the anti-inflammatory effect of a poly-prescription of traditional Chinese medicine GK001. Methods 1. Inhibitory effect on pain in mice: The pain was induced by i. p. 0.2 ml of 0.6 % HAc per mouse 1 h post dosing GK001. The writhing numbers of mice were recorded in 10 minutes and the inhibitory rate of pain was calculated compared with the control group. 2. Antipyretie effect In single dose experiment 15 healthy rabbits weighing 1.7-2.8 kg with body temperature(BT) measured in the experiment day meeting to the requirements were selected for the experiment and divided into 5 groups(3 in each group), which were dosed orally with GK001 and 1 h later followed by i. p. injection of 40 EU bacterial endotoxin standard·kg-1. Then, the BT of rabbits was measured every 30 min during 1-3 h after administration. The difference between the highest BT post-dose and the average BT pre-dose was calculated. In multi-dose experiment rabbits were selected and grouped as well as received i. p. endotoxin in the same way as above, but were administered with GK001 for consecutive 5 day. 3. Bacteriostatie effect. The antibacterial activities of GK001 on Bacillus Pumilus, Bacillus Subtilis and Micrococcus Luteus were measured in vitro at concentrations of 0.125-1.0 g·mL-1. Results 1. The GK001 showed a significant and dose-dependent painsuppressant effect, with inhibitory rate being 45.2 %, 31.2 % and 20.8 % at high, medium and low dose, respectively (P< 0.05). 2. Both single and multiple administration of GK001 had no effect on rabbit pyrogen response caused by endotoxin. 3. GK001 had bacteriostatic effects on the aforementioned 3 bacteria significantly and in dose-dependent fashion. Conclusions GK001 has analgesic and in vitro antibacterial but no antipyretie effects.

  15. CLINICAL OBSERVATION ON THE ANALGESIC EFFECT OF ACUPUNCTURE OF HEGU-POINT GVRING HYSTEROTOKOTOMY

    史素云; 陈勇; 陈文玲; 郭淑英

    2000-01-01

    Due to multiple factors as supernutrition of pregnant women, etc., the hysterotokotomy rate is increasing day by day. In most cases, local anesthesia is adopted, the parturient often complain of pain loudly and even groan incessantly. For relieving parturient's pain and ensuring the smooth conduction of hysterotokotomy, the author applied acupuncture combined with local anesthetics in 100 cases of hysterotokotomy from March of 1998 to March of 1999 and achieved a good therapeutic effect. Here is the summary.

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

    A. Shafiee

    2006-01-01

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

  17. Tianeptine prevents respiratory depression without affecting analgesic effect of opiates in conscious rats.

    Cavalla, David; Chianelli, Fabio; Korsak, Alla; Hosford, Patrick S; Gourine, Alexander V; Marina, Nephtali

    2015-08-15

    Respiratory depression remains an important clinical problem that limits the use of opiate analgesia. Activation of AMPA glutamate receptors has been shown to reverse fentanyl-induced respiratory changes. Here, we explored whether tianeptine, a drug known for its ability to phosphorylate AMPA receptors, can be used to prevent opiate-induced respiratory depression. A model of respiratory depression in conscious rats was produced by administration of morphine (10mg/kg, i.p.). Rats were pre-treated with test compounds or control solutions 5min prior to administration of morphine. Respiratory activity was measured using whole-body plethysmography. In conscious animals, tianeptine (2 and 10mg/kg, ip) and DP-201 (2-(4-((3-chloro-6-methyl-5,5-dioxido-6,11-dihydrodibenzo[c,f][1,2] thiazepin-11-yl)amino)butoxy)acetic acid; tianeptine analogue; 2mg/kg, ip) triggered significant (~30%) increases in baseline respiratory activity and prevented morphine-induced respiratory depression. These effects were similar to those produced by an ampakine CX-546 (15mg/kg, ip). The antinociceptive effect of morphine (hot plate test) was unaffected by tianeptine pre-treatment. In conclusion, the results of the experiments conducted in conscious rats demonstrate that systemic administration of tianeptine increases respiratory output and prevents morphine-induced respiratory depression without interfering with the antinociceptive effect of opiates.

  18. Analgesic Effect of the Newly Developed S(+)-Flurbiprofen Plaster on Inflammatory Pain in a Rat Adjuvant-Induced Arthritis Model.

    Sugimoto, Masanori; Toda, Yoshihisa; Hori, Miyuki; Mitani, Akiko; Ichihara, Takahiro; Sekine, Shingo; Hirose, Takuya; Endo, Hiromi; Futaki, Nobuko; Kaku, Shinsuke; Otsuka, Noboru; Matsumoto, Hideo

    2016-02-01

    Preclinical Research This article describes the properties of a novel topical NSAID (Nonsteroidal anti-inflammatory drug) patch, SFPP (S(+)-flurbiprofen plaster), containing the potent cyclooxygenase (COX) inhibitor, S(+)-flurbiprofen (SFP). The present studies were conducted to confirm human COX inhibition and absorption of SFP and to evaluate the analgesic efficacy of SFPP in a rat adjuvant-induced arthritis (AIA) model. COX inhibition by SFP, ketoprofen and loxoprofen was evaluated using human recombinant COX proteins. Absorption of SFPP, ketoprofen and loxoprofen from patches through rat skin was assessed 24 h after application. The AIA model was induced by injecting Mycobacterium tuberculosis followed 20 days later by the evaluation of the prostaglandin PGE2 content of the inflamed paw and the pain threshold. SFP exhibited more potent inhibitory activity against COX-1 (IC50  = 8.97 nM) and COX-2 (IC50  = 2.94 nM) than the other NSAIDs evaluated. Absorption of SFP was 92.9%, greater than that of ketoprofen and loxoprofen from their respective patches. Application of SFPP decreased PGE2 content from 15 min to 6 h and reduced paw hyperalgesia compared with the control, ketoprofen and loxoprofen patches. SFPP showed analgesic efficacy, and was superior to the ketoprofen and loxoprofen patches, which could be through the potent COX inhibitory activity of SFP and greater skin absorption. The results suggested SFPP can be expected to exert analgesic effect clinically.

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

    Joseph; JY; Sung

    2010-01-01

    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 SpragueDawley 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...

  20. Analgesic effect of ultrasound-guided transversus abdominis plane block after total abdominal hysterectomy

    Røjskjaer, Jesper O; Gade, Erik; Kiel, Louise B

    2015-01-01

    University Hospital. PATIENTS: Forty-six women scheduled for total abdominal hysterectomy. INTERVENTION: Women received either ropivacaine 0.75%, 20 mL (n = 24) or 0.9% saline, 20 mL (n = 24) in the transversus abdominis plane on each side. MAIN OUTCOME MEASURES: Primary outcome was the 24-h postoperative...... an ultrasound-guided transversus abdominis plane block in women undergoing total abdominal hysterectomy. As part of a multimodal regimen the transversus abdominis plane block showed some effect on pain scores at rest only in the early postoperative period....

  1. Effects of Neutron Skin Thickness in Peripheral Nuclear Reactions

    FANG De-Qing; MA Yu-Gang; CAI Xiang-Zhou; TIAN Wen-Dong; WANG Hong-Wei

    2011-01-01

    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.%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.Determining the size and shape of a nucleus is one of the most important subjects since the discovery of atomic nuclei.The rms radii of the neutron (rn) and proton (rp) density distributions are among the most prominent observables for this purpose.Studies for stable nuclei have shown that the nuclear radii are proportional to A1/3,with A being the nuclear mass number.Meanwhile,the density distributions of neutrons and protons in stable nuclei are very similar.

  2. Characterising the Analgesic Effect of Different Targets for Deep Brain Stimulation in Trigeminal Anaesthesia Dolorosa

    Sims-Williams, Hugh P.; Javed, Shazia; Pickering, Anthony E.; Patel, Nikunj K.

    2016-01-01

    Background Several deep brain stimulation (DBS) targets have been explored for the alleviation of trigeminal anaesthesia dolorosa. We aimed to characterise the analgesia produced from the periaqueductal grey (PAG) and centromedian-parafascicular (CmPf) nucleus using a within-subject design. Method We report a case series of 3 subjects implanted with PAG and CmPf DBS systems for the treatment of anaesthesia dolorosa. At follow-up, testing of onset and offset times, magnitude, and thermal and mechanical sensitivity was performed. Results The mean pain score of the cohort was acutely reduced by 56% (p effective at different stimulation frequencies and were not antagonistic in effect. Conclusion The mechanisms by which stimulation at these two targets produces analgesia are likely to be different. Certain pain qualities may respond more favourably to specific targets. Knowledge of onset and offset times for the targets can guide optimisation of stimulation settings. The use of more than one stimulation target may be beneficial and should be considered in anaesthesia dolorosa patients. PMID:27322524

  3. Analgesic effect of extracorporeal shock-wave therapy on chronic tennis elbow.

    Rompe, J D; Hope, C; Küllmer, K; Heine, J; Bürger, R

    1996-03-01

    We report a controlled, prospective study to investigate the effect of treatment by low-energy extracorporeal shock waves on pain in tennis elbow. We assigned at random 100 patients who had had symptoms for more than 12 months to two groups to receive low-energy shock-wave therapy. Group I received a total of 3000 impulses of 0.08 mJ/mm2 and group II, the control group, 30 impulses. The patients were reviewed after 3, 6 and 24 weeks. There was significant alleviation of pain and improvement of function after treatment in group I in which there was a good or excellent outcome in 48% and an acceptable result in 42% at the final review, compared with 6% and 24%, respectively, in group II.

  4. The analgesic effect of wound infiltration with local anaesthetics after breast surgery

    Byager, N; Hansen, Mads; Mathiesen, Ole;

    2014-01-01

    BACKGROUND: Wound infiltration with local anaesthetics is commonly used during breast surgery in an attempt to reduce post-operative pain and opioid consumption. The aim of this review was to evaluate the effect of wound infiltration with local anaesthetics compared with a control group on post-operative...... pain after breast surgery. METHODS: A systematic review was performed by searching PubMed, Google Scholar, the Cochrane database and Embase for randomised, blinded, controlled trials of wound infiltration with local anaesthetics for post-operative pain relief in female adults undergoing breast surgery...... partial or segmental mastectomy, and three trials breast reduction, excision of benign lump and unspecified breast surgery, respectively. Six trials demonstrated a small and short-lasting, but statistically significant reduction of post-operative pain scores, and four trials observed a statistically...

  5. Research Progress in Analgesic Effects of Curcumin%姜黄素镇痛作用研究进展

    张力(综述); 侯娜; 向勇(审校)

    2015-01-01

    姜黄素是从姜科植物姜黄的根茎中提取的一种橙黄色多酚类物质,具有抗肿瘤、抗病毒、抗风湿、抗氧化、抗炎症反应的药理特性,可以改善癌症、炎症、糖尿病、心血管疾病及神经系统疾病等多种疾病症状。姜黄素对多种疼痛均具有良好的效果,如外周神经损伤所致的神经病理性疼痛、糖尿病周围神经痛、手术后疼痛和炎症性疼痛等。%Curcumin is an orange-yellow polyphenol natural product isolated from the rhizome of the plant Curcuma longa.Curcumin was reported to have anticancer,antiviral,antiarthritic,antioxidant,and anti-inflammatory pharmacological properties,and curcumin has been linked with suppression of various cancers, inflammation,diabetes,diseases of the cardiovascular and neurological systems.Recent studies also showed that curcumin has antinociceptive effects on several painful diseases,such as peripheral nerve injury-induced neuropathic pain,diabetic peripheral neuralgia,postoperative pain,and inflammatory pain.

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

    Gönül Sağıroğlu

    2011-11-01

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

  7. Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.

    Trotter, B Wesley; Nanda, Kausik K; Burgey, Christopher S; Potteiger, Craig M; Deng, James Z; Green, Ahren I; Hartnett, John C; Kett, Nathan R; Wu, Zhicai; Henze, Darrell A; Della Penna, Kimberly; Desai, Reshma; Leitl, Michael D; Lemaire, Wei; White, Rebecca B; Yeh, Suzie; Urban, Mark O; Kane, Stefanie A; Hartman, George D; Bilodeau, Mark T

    2011-04-15

    A new series of imidazopyridine CB2 agonists is described. Structural optimization improved CB2/CB1 selectivity in this series and conferred physical properties that facilitated high in vivo exposure, both centrally and peripherally. Administration of a highly selective CB2 agonist in a rat model of analgesia was ineffective despite substantial CNS exposure, while administration of a moderately selective CB2/CB1 agonist exhibited significant analgesic effects.

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

    Jin-ling YIN

    2011-10-01

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

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

    Mishra Seema

    2003-01-01

    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.

  10. Analgesic Effect of Dexamethasone after Arthroscopic Knee Surgery: A Randomized Controlled Trial

    Jairo Moyano

    2016-01-01

    Full Text Available Background. Dexamethasone is sometimes used as a coanalgesic because of its anti-inflammatory properties. Objective. To evaluate opioid use, postoperative pain intensity, and side effects after a single dose of dexamethasone in patients undergoing arthroscopic knee surgery. Methods. In this randomized controlled study patients were randomized to receive either 10 mg of intravenous dexamethasone (DM group or 0.9% normal saline (NS group during the intraoperative period. Primary outcomes were pain intensity and total morphine and codeine use after surgery. Results. Seventy-eight patients were included in the study. The DM group showed statistically significant higher pain intensity at the fourth postoperative hour (DM: 3.96/10, standard deviation [SD] 0.54; NS: 2.46/10, SD 0.45; p=0.036. No statistically significant difference in total opioid use (morphine plus codeine was identified with 15.9 (SD 1.97 codeine tablets used in DM group and 20 (SD 2.14 in NS group (p=0.25. Discussion. Pain intensity tended to decrease in both groups suggesting morphine as the main source of analgesia. Conclusions. Intravenous dexamethasone during the intraoperative period has no clinical impact on postoperative pain intensity during the first 48 h after arthroscopic knee surgery. This trial is registered with R000020892.

  11. Evaluation of the analgesic effect of subcutaneous methadone after cesarean section

    Mitra Jabalameli

    2014-01-01

    Full Text Available Background: Inadequate pain control has a significant role in maternal and neonatal health in early post-partum period which interferes with breastfeeding and has a negative influence on child normal growth. The aim of this study is evaluation of subcutaneous methadone effectiveness on post-operative pain control. Materials and Methods: Double blind randomized prospective clinical trial involving 60 term pregnancy patients through 2008 to 2009 Undergo cesarean. Inclusion criteria: Prime gravid candidate of elective cesarean and spinal anesthesia class 1 or 2. Known case of drug allergy and methadone interaction, addiction, uncontrolled medical disease excluded. Case group injected 10 mg of subcutaneous methadone in the site of incision before final suture. Morphine was a pain reliever in follow up examination. Data include mean of pain, nausea and vomiting, MAP, etc., collected and analyzed by independent-T test and Man Whitney test. Results: Although mean usage of morphine between groups was not significant statistically but the mean pain severity (P value < 0.05 and mean satisfactory (P value = 0.02 was statistically significant between groups. Other parameters were not statistically significant. Conclusion: We suggest subcutaneous methadone as a safe pain reliever in post cesarean section patients.

  12. Analgesic effect of polygonum bistorta L. water extract%拳参水提取物的镇痛作用

    曾昭毅; 汪敏; 叶和杨; 周俐; 周青; 曾靖

    2006-01-01

    物,热板法测定给药后15,30,60min的痛觉反应.④拳参水提取物对电刺激致痛的实验:小鼠40只,随机数字表法分为4组,10只/组,分别腹腔注射0.02 mL/g生理盐水,0.10,0.15 mg/g拳参水提取物,1g/L吗啡,于给药后20,35,50,70 min重复电刺激,电刺激法测定痛觉反应.主要观察指标:①小鼠扭体反应次数.②热板法致小鼠痛觉反应的时间.③电刺激法致小鼠镇痛率.结果:共选取健康成年昆明种小鼠150只用于4个独立实验,全部进入结果分析.①小鼠扭体反应次数:拳参水提取物0.10,0.15mg/g组及氨基比林组小鼠给药后15min扭体反应次数均少于生理盐水组[(15.1±11.1),(8.0±6.5),(6.3±3.2),(54.1±20.2)次,t=3.532~3.681,<0.01].②热板法致小鼠痛觉反应的时间:拳参水提取物0.10,0.15 mg/g组和吗啡组小鼠给药后15,30,60 min痛觉反应的时间均长于生理盐水组(t=2.676~3.683,P<0.05~0.01).③纳洛酮+拳参水提取物组小鼠给药后各时间点痛觉反应的时间均长于生理盐水组(t=2.676~3.563,P<0.05~0.01),但纳洛酮+吗啡组与生理盐水组相接近(P>0.05).④电刺激法致小鼠镇痛率:拳参水提取物0.10,0.15 mg/g组及吗啡组给药后20,35,50,70 min镇痛率均高于生理盐水组(t=3.455~3.634,<0.01).结论:①拳参水提取物具有明显的镇痛作用,其镇痛强度与氨基比林、吗啡相当.②阿片受体拮抗剂纳洛酮可拮抗吗啡的镇痛作用,但不能拮抗拳参水提取物的镇痛作用,这表明拳参水提取物的镇痛作用并非通过激动阿片受体而发挥.%BACKGROUND: Bistort rhizome is also named as caoheche, which is characterized by clearing heat, relieving convulsion, regulating damp and reducing swelling. Additionally, its water extract is characterized by antiarrhythmia and central inhibition; however, analgesia should be studied further.OBJECTIVE: To observe analgesic effect of polygonum bistorta L. Water extract, and compare with morphine and amidazofen

  13. EFFECT OF PREOPERATIVE PREGABALIN ON POSTOPERATIVE ANALGESIC REQUIREMENT AFTER SKIN GRAFTING

    Mamta

    2014-05-01

    effects.

  14. Analgesic Effect of Coptis chinensis rhizomes (Coptidis Rhizoma) Extract on Rat Model of Irritable Bowel Syndrome

    Tjong, Yungwui; Ip, Siupo; Lao, Lixing; Fong, Harry H. S.; Sung, Joseph J. Y.; Berman, Brian; Che, Chuntao

    2011-01-01

    Aim of study Coptis chinensis rhizomes (Coptidis Rhizoma, CR), also known as “Huang Lian”, is a common component of traditional Chinese herbal formulae used for the relief of abdominal pain and diarrhea. Yet, the action mechanism of CR extract in the treatment of irritable bowel syndrome is unknown. Thus, the aim of our present study is to investigate the effect of CR extract on neonatal maternal separation (NMS)-induced visceral hyperalgesia in rats and its underlying action mechanisms. Materials and methods Male Sprague-Dawley rats were subjected to 3-hr daily maternal separation from postnatal day 2 to day 21 to form the NMS group. The control group consists of unseparated normal (N) rats. From day 60, rats were administrated CR (0.3, 0.8 and 1.3 g/Kg) or Vehicle (Veh; 0.5% carboxymethylcellulose solution) orally for 7 days for the test and control groups, respectively. Results Electromyogram (EMG) signals in response to colonic distension were measured with the NMS rats showing lower pain threshold and increased EMG activity than those of the unseparated (N) rats. CR dose-dependently increased pain threshold response and attenuated EMG activity in the NMS rats. An enzymatic immunoassay study showed that CR treatment significantly reduced the serotonin (5HT) concentration from the distal colon of NMS rats compared to the Veh (control) group. Real-time quantitative PCR and Western-blotting studies showed that CR treatment substantially reduced NMS induced cholecystokinin (CCK) expression compared with the Veh group. Conclusions These results suggest that CR extract robustly reduces visceral pain that may be mediated via the mechanism of decreasing 5HT release and CCK expression in the distal colon of rats. PMID:21511022

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

    Apurba Mukherjee

    2009-06-01

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

  16. Peripheral administration of lactate produces antidepressant-like effects

    Carrard, A

    2016-10-18

    In addition to its role as metabolic substrate that can sustain neuronal function and viability, emerging evidence supports a role for l-lactate as an intercellular signaling molecule involved in synaptic plasticity. Clinical and basic research studies have shown that major depression and chronic stress are associated with alterations in structural and functional plasticity. These findings led us to investigate the role of l-lactate as a potential novel antidepressant. Here we show that peripheral administration of l-lactate produces antidepressant-like effects in different animal models of depression that respond to acute and chronic antidepressant treatment. The antidepressant-like effects of l-lactate are associated with increases in hippocampal lactate levels and with changes in the expression of target genes involved in serotonin receptor trafficking, astrocyte functions, neurogenesis, nitric oxide synthesis and cAMP signaling. Further elucidation of the mechanisms underlying the antidepressant effects of l-lactate may help to identify novel therapeutic targets for the treatment of depression.

  17. The Effectiveness of Intravenous Dexmedetomidine on Perioperative Hemodynamics, Analgesic Requirement, and Side Effects Profile in Patients Undergoing Laparoscopic Surgery Under General Anesthesia

    Panchgar, Vinayak; Shetti, Akshaya N.; Sunitha, H. B.; Dhulkhed, Vithal K.; Nadkarni, A. V.

    2017-01-01

    Background: There is an upward surge in the use of laparoscopic surgeries due to various advantages when compared to open surgeries. Major advantages are, due to small incisions which are cosmetically acceptable and most of them are now daycare procedures. Problem of economic burden and hospital bed occupancy has been overcome with laparoscopic surgeries. All these advantages are not free from disadvantages, as hemodynamic changes such as hypertension; tachycardia and other surgical-related complications are commonly observed intraoperatively. Dexmedetomidine is one of the α2 agonist drugs which acts at both supraspinal and spinal level and modulate the transmission of nociceptive signals in the central nervous system. The basic effect of dexmedetomidine on the cardiovascular system is to decrease the heart rate and systemic vascular resistance with additional feature of opioid sparing effect. This drug has become an ideal adjuvant during general anesthesia, especially when stress is expected. Hence, the drug was studied in laparoscopic surgeries. Aims and Objectives: (a) To study the effect of dexmedetomidine on hemodynamic parameters during perioperative period in patients undergoing laparoscopic surgery. (b) To study the postoperative sedation score and analgesic requirement. (c) To study the side effect profile of dexmedetomidine. Settings and Design: Randomized double blind controlled trial. Subjects and Methods: After obtaining the Institutional Ethical Clearance, the study was conducted. Forty patients of American Society of Anesthesiologists Class I and II were enrolled in this randomized study. The patients were randomly divided into two groups; group normal saline (NS) and group dexmedetomidine. Patient received either NS or dexmedetomidine in group NS and group dexmedetomidine, respectively, depending upon the allocation. The infusion rate was adjusted according to; loading dose (1 μg/kg) over 10 min and maintenance dose (0.5 μg/kg/h) and

  18. Intrathecal Analgesic Drug Delivery is Effective for Analgesia in a Patient with Post-Poliomyelitis Syndrome: A Case Report

    van Tilburg, Cornelis W.J.

    2016-01-01

    Patient: Female, 45 Final Diagnosis: Post-poliomyelitis syndrome Symptoms: Chronic pain Medication: Fentanyl • Oxycodone • Gabapentin • Naproxen • Paracetamol Clinical Procedure: Intrathecal analgesic drug delivery Specialty: Anesthesiology Objective: Unusual setting of medical care Background: Post-poliomyelitis syndrome (PPS) is a progressive neuromuscular syndrome, with chronic pain being one of the most prevalent symptoms. We present a case report on intrathecal analgesic drug delivery to diminish chronic, refractory pain in a patient with PPS. Case Report: In a wheelchair-bound 45-year-old female patient (Caucasian, body mass index [BMI] 20.5) with severe chronic, refractory pain, a Synchromed® II pump (Medtronic, Minneapolis, Minnesota, USA) was implanted after multi-disciplinary consultation and a successful trial period. After 8 months, relocation of the pump due to regional pressure problems with surrounding erythema had to occur. A second pump relocation due to pressure problems and skin erosion was needed 18 months after the first relocation, moving from the abdominal wall to the sheath of the rectus abdominis muscle, resulting in resolution of the problems. Conclusions: In patients with PPS, intrathecal analgesic drug delivery can be an option to treat chronic, refractory pain. Multidisciplinary consultation is necessary to deal with the wide variety of problems in these patients. Skin problems at the site of the pump reservoir can be challenging and time-consuming and, ultimately, can necessitate relocation (or removal) of the device. PMID:27980323

  19. 羌活挥发油的GC-MS分析及其抗炎镇痛的药理作用初探%Analysis of Volatile Oil of Notopterygium Incisum by GC-MS and Its Effects of Anti-inflammatory and Analgesic

    陈智煌; 廖华军; 刘晨; 邱颂平

    2015-01-01

    目的: GC-MS分析羌活挥发油主要成分,并观察其抗炎、镇痛的药理作用。方法通过 GC-MS联用分析羌活挥发油的主要成分;通过二甲苯小鼠耳部肿胀实验观察抗炎作用;通过醋酸扭体法和小鼠热板法观察其镇痛效果。结果鉴定出羌活挥发油17种化合物;羌活挥发油的高、中、低剂量均可显著抑制二甲苯所致小鼠耳肿胀,具有良好的抗炎作用;羌活挥发油高剂量组可显著减少醋酸所致的小鼠扭体次数,镇痛率可达47.15%;但羌活挥发油对热板所致小鼠疼痛无明显抑制作用。结论羌活挥发油的主要成分为(1R)-(+)-α-蒎烯,松油醇,且总挥发油具有明显的抗炎作用和镇痛作用。%OBJECTIVE To analyze main ingredient of volatile oil of Notopterygium incisum by GC-MS and ob-serve pharmacological effects of anti-inflammatory and analgesic.METHODS GC-MS was employed.The analgesic effect was observed with the response of writhes and hot plate test.The anti-inflammatory effect was observed by mice inflammation models caused by xylene and mice models with reinforce permeability of abdominal cavity capillary caused by acetic acid.RESULTS Seventeen volatile constituents were determined.Volatile of Notopterygium inci-sum could obviously inhibit the xylene induced ear swelling.High dose of volatile had significant analgesic effect on writhing responses induced by acetic acid,47.15%rate of analgesic,but had no effect on analgesic response in the hot plate test.CONCLUSION Main ingredient of volatile oil of Notopterygium incisum are (1R)-(+)-α-pinene, terpineol.The volatile oil have definite effects on anti-inflammation and peripheral analgesia.

  20. Peripheral metabolic effects of endocannabinoids and cannabinoid receptor blockade.

    Engeli, Stefan

    2008-01-01

    The endocannabinoid system consists of endogenous arachidonic acid derivates that activate cannabinoid receptors. The two most prominent endocannabinoids are anandamide and 2-arachidonoyl glycerol. In obesity, increased concentrations of circulating and tissue endocannabinoid levels have been described, suggesting increased activity of the endocannabinoid system. Increased availability of endocannabinoids in obesity may over-stimulate cannabinoid receptors. Blockade of cannabinoid type 1 (CB1) receptors was the only successful clinical development of an anti-obesity drug during the last decade. Whereas blockade of CB1 receptors acutely reduces food intake, the long-term effects on metabolic regulation are more likely mediated by peripheral actions in liver, skeletal muscle, adipose tissue, and the pancreas. Lipogenic effects of CB1 receptor signalling in liver and adipose tissue may contribute to regional adipose tissue expansion and insulin resistance in the fatty liver. The association of circulating 2-arachidonoyl glycerol levels with decreased insulin sensitivity strongly suggests further exploration of the role of endocannabinoid signalling for insulin sensitivity in skeletal muscle, liver, and adipose tissue. A few studies have suggested a specific role for the regulation of adiponectin secretion from adipocytes by endocannabinoids, but that has to be confirmed by more experiments. Also, the potential role of CB1 receptor blockade for the stimulation of energy expenditure needs to be studied in the future. Despite the current discussion of safety issues of cannabinoid receptor blockade, these findings open a new and exciting perspective on endocannabinoids as regulators of body weight and metabolism.

  1. Analgesic and anti-inflammatory effect of Anwei Pills%安胃丸抗炎镇痛作用的实验研究

    任守忠; 李鑫; 郭建生; 何书华; 师振宇

    2012-01-01

    Objective To study the analgesic and anti-inflammatory effect of Anwci Pills. Methods The analgesic effects of Anwci Pills were observed by acetic acid writhing assay and hot plate methods in mice. The anti-inflammatory effect was observed by c-valuating xylcnc-induccd car swelling in mice (acute inflammation) and cotton-induced granuloma in rats (chronic inflammation). Results Anwci Pills at various doses significantly reduced the number of writhing caused by acetic acid in mice. Anwci Pills at middle doses significantly prolonged the latency of writhing in mice. Anwci Pills at high doses improved the pain threshold in mice; Anwci Pills at various doses significantly inhibited car swelling caused by xylcne in mice and cotton-induced proliferation of granulation tissue in rats. Conclusion Anwci Pills has an anti-inflammatory and analgesic effect.%目的 研究安胃丸的镇痛、抗炎作用.方法 采用扭体法和热板法,观察安胃丸的镇痛作用;采用二甲苯致小鼠耳廓肿胀模型和大鼠棉球肉芽肿模型,观察该药的抗炎作用.结果 安胃丸各剂量组小鼠扭体次数显著减少;其中安胃丸中剂量可显著延长小鼠扭体潜伏期.安胃丸高剂量可提高热刺激小鼠的痛阈值.安胃丸各组二甲苯引起的小鼠耳肿胀度及大鼠棉球所致肉芽组织的质量显著降低.结论 安胃丸具有良好的抗炎、镇痛作用.

  2. Effect of pre-operative rectal diclofenac suppository on post-operative analgesic requirement in cleft palate repair: A randomised clinical trial

    E S Adarsh

    2012-01-01

    Full Text Available Background: Opioid analgesics used for analgesia are associated with sedation, respiratory depression and post-operative nausea and vomiting. Non-steroidal anti-inflammatory drugs such as diclofenac are a safe and effective alternative with opioid-sparing effect. Objective: To evaluate the effectiveness of pre-operative rectal diclofenac suppository (1 mg/kg in cleft palate repair for post-operative analgesia and reduction in post-operative opioid requirements. Study Design: A randomized clinical trial. Methods: After obtaining approval from the institutional ethical committee, 60 children were allocated by a computer-generated randomisation into two groups of 30 each; group D (Diclofenac group and group C (Conventional group. Children in group D and group C were similar in all aspects except for the fact that group D children received 1 mg/kg diclofenac suppository after induction. Pain was evaluated using modification of the objective pain scale by Hannallah and colleagues for 6 h post-operatively by an anaesthesiology resident or nursing staff who was blinded to the group. If the pain score was more than 3, rescue analgesic I.V. fentanyl 0.5 μgm/kg was administered. The pain scores at different intervals, number of doses and quantity of rescue analgesic required were noted. Results: We observed that pre-operative rectal diclofenac provided effective analgesia in the immediate post-operative period, as evidenced by reduced pain scores and reduced opioid requirement (P=0.00002. There was no evidence of any increased perioperative bleeding in the diclofenac group. Conclusion: Pre-operative rectal diclofenac reduces opioid consumption and provides good post-operative analgesia.

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

    Y.J. Mousa

    2012-01-01

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

  4. Effects of peripheral-type benzodiazepine receptor ligands on Ehrlich tumor cell proliferation.

    Sakai, Mônica; Fonseca, Evelise Souza Monteiro; Oloris, Silvia Catarina Salgado; Matsuzaki, Patrícia; Otake, Andréia Hanada; Leite, Kátia Ramos Moura; Massoco, Cristina Oliveira; Dagli, Maria Lúcia Zaidan; Palermo-Neto, João

    2006-11-21

    Peripheral-type benzodiazepine receptors have been found throughout the body, and particularly, in high numbers, in neoplastic tissues such as the ovary, liver, colon, breast, prostate and brain cancer. Peripheral-type benzodiazepine receptor expression has been associated with tumor malignity, and its subcellular localization is important to define its function in tumor cells. We investigated the presence of peripheral-type benzodiazepine receptors in Ehrlich tumor cells, and the in vitro effects of peripheral-type benzodiazepine receptors ligands on tumor cell proliferation. Our results demonstrate the presence of peripheral-type benzodiazepine receptor in the nucleus of Ehrlich tumor cells (85.53+/-12.60%). They also show that diazepam and Ro5-4864 (peripheral-type benzodiazepine receptor agonists) but not clonazepam (a molecule with low affinity for the peripheral-type benzodiazepine receptor) decreased the percentage of tumor cells in G0-G1 phases and increased that of cells in S-G2-M phases. The effects of those agonists were prevented by PK11195 (a peripheral-type benzodiazepine receptor antagonist) that did not produce effects by itself. Altogether, these data suggest that the presence of peripheral-type benzodiazepine receptor within the nucleus of Ehrlich tumor cells is associated with tumor malignity and proliferation capacity.

  5. Evidence for Inhibitory Effects of Flupirtine, a Centrally Acting Analgesic, on Delayed Rectifier K+ Currents in Motor Neuron-Like Cells

    Sheng-Nan Wu; Ming-Chun Hsu; Yu-Kai Liao; Fang-Tzu Wu; Yuh-Jyh Jong; Yi-Ching Lo

    2012-01-01

    Flupirtine (Flu), a triaminopyridine derivative, is a centrally acting, non-opiate analgesic agent. In this study, effects of Flu on K+ currents were explored in two types of motor neuron-like cells. Cell exposure to Flu decreased the amplitude of delayed rectifier K+ current (I K(DR)) with a concomitant raise in current inactivation in NSC-34 neuronal cells. The dissociation constant for Flu-mediated increase of I K(DR) inactivation rate was about 9.8  μ M. Neither linopirdine (10  μ M), NMD...

  6. Effects of treatment of peripheral pain generators in fibromyalgia patients.

    Affaitati, Giannapia; Costantini, Raffaele; Fabrizio, Alessandra; Lapenna, Domenico; Tafuri, Emmanuele; Giamberardino, Maria Adele

    2011-01-01

    Fibromyalgia syndrome (FS) frequently co-occurs with regional pain disorders. This study evaluated how these disorders contribute to FS, by assessing effects of local active vs placebo treatment of muscle/joint pain sources on FS symptoms. Female patients with (1) FS+myofascial pain syndromes from trigger points (n=68), or (2) FS+joint pain (n=56) underwent evaluation of myofascial/joint symptoms [number/intensity of pain episodes, pressure pain thresholds at trigger/joint site, paracetamol consumption] and FS symptoms [pain intensity, pressure pain thresholds at tender points, pressure and electrical pain thresholds in skin, subcutis and muscle in a non-painful site]. Patients of both protocols were randomly assigned to two groups [34 each for (1); 28 each for (2)] to receive active or placebo local TrP or joint treatment [injection/hydroelectrophoresis] on days 1 and 4. Evaluations were repeated on days 4 and 8. After therapy, in active--but not placebo-treated-- groups: number and intensity of myofascial/joint episodes and paracetamol consumption decreased and pressure thresholds at trigger/joint increased (ppain intensity decreased and all thresholds increased progressively in tender points and the non-painful site (ppain was still lower than basis in patients not undergoing further therapy and had decreased in those undergoing active therapy from day 8 (ppains impact significantly on FS, probably through increased central sensitization by the peripheral input; their systematic identification and treatment are recommended in fibromyalgia.

  7. Pharmacological Treatment Of Diabetic Peripheral Neuropathy

    2015-01-01

    Pain modulation is a key treatment goal for diabetic peripheral neuropathy patients. Guidelines have recommended antidepressant, anticonvulsant, analgesic, and topical medications—both approved and off-label—to reduce pain in this population.

  8. Experimental study on analgesic anti-inflammatory effects of golden cream%金黄膏镇痛抗炎作用的实验研究

    李国春; 黄新武

    2013-01-01

    Objective: To study the anti-inflammatory analgesic efficacy of hospital preparation golden cream. Methods: Using hot-plate and writhing method to carry out analgesic test, using xylene-induced ear edema and carrageenan-induced rat paw edema methods for anti-inflammatory test. Results: Golden cream can improve the mice to thermal stimulation pain threshold; suppress pain caused by acetic acid in mice;golden cream also markedly inhibited by the xylene-induced mouse ear edema and carrageenan-induced rat paw edema. Conclusion:Golden cream has a significant analgesic effect and anti-inflammatory effects.%目的:对医院制剂金黄膏进行镇痛抗炎的药效学研究。方法:采用热板法和扭体法进行镇痛试验;采用二甲苯所致小鼠耳廓肿胀及角叉菜胶致大鼠足跖肿方法进行抗炎试验。结果:金黄膏能提高小鼠对热刺激的疼痛阈值,抑制醋酸所致的小鼠疼痛;金黄膏也能明显抑制由二甲苯所致的小鼠耳廓肿胀和角叉菜胶所致的大鼠足跖肿胀。结论:金黄膏具有明显的镇痛作用及抗炎作用。

  9. The Isolated Effect of Adductor Canal Block on Quadriceps Femoris Muscle Strength After Total Knee Arthroplasty

    Sørensen, Johan Kløvgaard; Jæger, Pia; Dahl, Jørgen Berg;

    2016-01-01

    BACKGROUND: Using peripheral nerve block after total knee arthroplasty (TKA), without impeding mobility, is challenging. We hypothesized that the analgesic effect of adductor canal block (ACB) could increase the maximum voluntary isometric contraction (MVIC) of the quadriceps femoris muscle after...

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

    Meregalli C

    2012-06-01

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

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

    Keppel Hesselink JM

    2013-08-01

    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

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

    Hesselink, Jan M Keppel

    2013-01-01

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

  13. Analgesic Potential of Essential Oils

    José Ferreira Sarmento-Neto

    2015-12-01

    Full Text Available Pain is an unpleasant sensation associated with a wide range of injuries and diseases, and affects approximately 20% of adults in the world. The discovery of new and more effective drugs that can relieve pain is an important research goal in both the pharmaceutical industry and academia. This review describes studies involving antinociceptive activity of essential oils from 31 plant species. Botanical aspects of aromatic plants, mechanisms of action in pain models and chemical composition profiles of the essential oils are discussed. The data obtained in these studies demonstrate the analgesic potential of this group of natural products for therapeutic purposes.

  14. Analgesic Effect of the Newly Developed S(+)‐Flurbiprofen Plaster on Inflammatory Pain in a Rat Adjuvant‐Induced Arthritis Model

    Toda, Yoshihisa; Hori, Miyuki; Mitani, Akiko; Ichihara, Takahiro; Sekine, Shingo; Hirose, Takuya; Endo, Hiromi; Futaki, Nobuko; Kaku, Shinsuke; Otsuka, Noboru; Matsumoto, Hideo

    2016-01-01

    ABSTRACT Preclinical Research This article describes the properties of a novel topical NSAID (Nonsteroidal anti‐inflammatory drug) patch, SFPP (S(+)‐flurbiprofen plaster), containing the potent cyclooxygenase (COX) inhibitor, S(+)‐flurbiprofen (SFP). The present studies were conducted to confirm human COX inhibition and absorption of SFP and to evaluate the analgesic efficacy of SFPP in a rat adjuvant‐induced arthritis (AIA) model. COX inhibition by SFP, ketoprofen and loxoprofen was evaluated using human recombinant COX proteins. Absorption of SFPP, ketoprofen and loxoprofen from patches through rat skin was assessed 24 h after application. The AIA model was induced by injecting Mycobacterium tuberculosis followed 20 days later by the evaluation of the prostaglandin PGE2 content of the inflamed paw and the pain threshold. SFP exhibited more potent inhibitory activity against COX‐1 (IC50 = 8.97 nM) and COX‐2 (IC50 = 2.94 nM) than the other NSAIDs evaluated. Absorption of SFP was 92.9%, greater than that of ketoprofen and loxoprofen from their respective patches. Application of SFPP decreased PGE2 content from 15 min to 6 h and reduced paw hyperalgesia compared with the control, ketoprofen and loxoprofen patches. SFPP showed analgesic efficacy, and was superior to the ketoprofen and loxoprofen patches, which could be through the potent COX inhibitory activity of SFP and greater skin absorption. The results suggested SFPP can be expected to exert analgesic effect clinically. Drug Dev Res 76 : 20–28, 2016. © 2016 Wiley Periodicals, Inc. PMID:26763139

  15. Effects of limited peripheral vision on shuttle sprint performance of soccer players

    Lemmink, KAPM; Dijkstra, B; Visscher, C

    2005-01-01

    This study examined the effect of limited peripheral vision oil the shuttle sprint performance of soccer players. Participants were 14 male soccer players of a student soccer club (M age = 22.1 yr., SD = 1.3 yr.). They performed a repeated shuttle sprint with full and limited peripheral vision. Mean

  16. Selective 5-HT7 receptor agonists LP 44 and LP 211 elicit an analgesic effect on formalin-induced orofacial pain in mice

    Kadriye DEMİRKAYA

    Full Text Available ABSTRACT The most recently identified serotonin (5-HT receptor is the 5-HT7 receptor. The antinociceptive effects of a 5-HT7 receptor agonist have been shown in neuropathic and inflammatory animal models of pain. A recent study demonstrated the functional expression of 5-HT7 receptors in the substantia gelatinosa (SG of the trigeminal subnucleus caudalis, which receives and processes orofacial nociceptive inputs. Objective To investigate the antinociceptive effects of pharmacological activation of 5-HT7 receptors on orofacial pain in mice. Material and Methods Nociception was evaluated by using an orofacial formalin test in male Balb-C mice. Selective 5-HT7 receptor agonists, LP 44 and LP 211 (1, 5, and 10 mg/kg, were given intraperitoneally 30 min prior to a formalin injection. A bolus of 10 µl of 4% subcutaneous formalin was injected into the upper lip of mice and facial grooming behaviors were monitored. The behavioral responses consisted of two distinct periods, the early phase corresponding to acute pain (Phase I: 0–12 min and the late phase (Phase II: 12–30 min. Results LP 44 and LP 211 (1, 5, and 10 mg/kg produced an analgesic effect with reductions in face rubbing time in both Phase I and Phase II of the formalin test. Conclusion Our results suggest that 5-HT7 receptor agonists may be promising analgesic drugs in the treatment of orofacial pain.

  17. Regulation of Neurotrophin-3 and Interleukin-1β and Inhibition of Spinal Glial Activation Contribute to the Analgesic Effect of Electroacupuncture in Chronic Neuropathic Pain States of Rats

    Wenzhan Tu

    2015-01-01

    Full Text Available Growing evidence indicates that neurotrophin-3, interleukin-1β, and spinal glia are involved in neuropathic pain derived from dorsal root ganglia to spinal cord. Electroacupuncture is widely accepted to treat chronic pain, but the precise mechanism underlying the analgesic effect of EA has not been fully demonstrated. In this study, the mechanical withdrawal threshold and thermal withdrawal latency were recorded. We used immunofluorescence and western blots methods to investigate the effect of EA on the expression of NT-3 and IL-1β in DRG and spinal cord of CCI rats; we also examined the expression of spinal GFAP and OX-42 in spinal cord. In present study, the MWT and TWL of CCI group rats were lower than those in the Sham CCI group rats, but EA treatment increased the pain thresholds. Furtherly, we found that EA upregulates the expression of NT-3 in DRG and spinal cord of CCI rats, while EA downregulates the expression of IL-1β. Additionally, immunofluorescence exhibited that CCI-induced activation of microglia and astrocytes was inhibited significantly by EA treatment. These results demonstrated that the analgesic effect of EA may be achieved through promoting the neural protection of NT-3 as well as the inhibition of IL-1β production and spinal glial activity.

  18. Selective 5-HT7 receptor agonists LP 44 and LP 211 elicit an analgesic effect on formalin-induced orofacial pain in mice

    DEMİRKAYA, Kadriye; AKGÜN, Özlem Martı; ŞENEL, Buğra; ÖNCEL TORUN, Zeynep; SEYREK, Melik; LACİVİTA, Enza; LEOPOLDO, Marcello; DOĞRUL, Ahmet

    2016-01-01

    ABSTRACT The most recently identified serotonin (5-HT) receptor is the 5-HT7 receptor. The antinociceptive effects of a 5-HT7 receptor agonist have been shown in neuropathic and inflammatory animal models of pain. A recent study demonstrated the functional expression of 5-HT7 receptors in the substantia gelatinosa (SG) of the trigeminal subnucleus caudalis, which receives and processes orofacial nociceptive inputs. Objective To investigate the antinociceptive effects of pharmacological activation of 5-HT7 receptors on orofacial pain in mice. Material and Methods Nociception was evaluated by using an orofacial formalin test in male Balb-C mice. Selective 5-HT7 receptor agonists, LP 44 and LP 211 (1, 5, and 10 mg/kg), were given intraperitoneally 30 min prior to a formalin injection. A bolus of 10 µl of 4% subcutaneous formalin was injected into the upper lip of mice and facial grooming behaviors were monitored. The behavioral responses consisted of two distinct periods, the early phase corresponding to acute pain (Phase I: 0–12 min) and the late phase (Phase II: 12–30 min). Results LP 44 and LP 211 (1, 5, and 10 mg/kg) produced an analgesic effect with reductions in face rubbing time in both Phase I and Phase II of the formalin test. Conclusion Our results suggest that 5-HT7 receptor agonists may be promising analgesic drugs in the treatment of orofacial pain. PMID:27383702

  19. The pharmacology of topical analgesics.

    Barkin, Robert L

    2013-07-01

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

  20. Anti-analgesic effect of the mu/delta opioid receptor heteromer revealed by ligand-biased antagonism.

    Laura Milan-Lobo

    Full Text Available Delta (DOR and mu opioid receptors (MOR can complex as heteromers, conferring functional properties in agonist binding, signaling and trafficking that can differ markedly from their homomeric counterparts. Because of these differences, DOR/MOR heteromers may be a novel therapeutic target in the treatment of pain. However, there are currently no ligands selective for DOR/MOR heteromers, and, consequently, their role in nociception remains unknown. In this study, we used a pharmacological opioid cocktail that selectively activates and stabilizes the DOR/MOR heteromer at the cell surface by blocking its endocytosis to assess its role in antinociception. We found that mice treated chronically with this drug cocktail showed a significant right shift in the ED50 for opioid-mediated analgesia, while mice treated with a drug that promotes degradation of the heteromer did not. Furthermore, promoting degradation of the DOR/MOR heteromer after the right shift in the ED50 had occurred, or blocking signal transduction from the stabilized DOR/MOR heteromer, shifted the ED50 for analgesia back to the left. Taken together, these data suggest an anti-analgesic role for the DOR/MOR heteromer in pain. In conclusion, antagonists selective for DOR/MOR heteromer could provide an avenue for alleviating reduced analgesic response during chronic pain treatment.

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

    Waddington F

    2014-12-01

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

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

    Kim Min-jung

    2013-09-01

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

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

    O.J. Olorunfemi

    2012-04-01

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

  4. Transection of peripheral nerves, bridging strategies and effect evaluation

    IJkema-Paassen, J; Jansen, K; Gramsbergen, A; Meek, MF

    2004-01-01

    Disruption of peripheral nerves due to trauma is a frequently Occurring clinical problem. Gaps in the nerve are bridged by guiding the regenerating nerves along autologous grafts or artificial guides. This review gives an overview oil the different methods of nerve repair techniques. Conventional su

  5. Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonianEunicella singularis

    Monia Deghrigue; Carmen Festa; Lotfi Ghribi; Maria Valeria DAuria; Simona De Marino; Hichem Ben Jannet; Abderrahman Bouraoui

    2015-01-01

    Objective:To explore anti-inflammatory activities of organic extract and its semi-purified fractions (ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis.Methods:The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature.Results: The fraction F-EtOH showed an important anti-inflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols.Conclusions: These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

  6. Analgesic effect and mechanism of the three TCM-herbal drug-combination Tou Feng Yu pill on treatment of migraine.

    Li, Jia-chuan; Shen, Xiao-fei; Meng, Xian-li; Zhang, Yi; Lai, Xian-rong

    2011-06-15

    It is well known that pain is one of the most important characteristics of migraine. Therefore, it is important and interesting to investigate the analgesic effect and mechanism of drugs which are used to treat migraine. Tou Feng Yu pill (TFY) is a traditional Chinese herbal medicine, consisting of the three Chinese herbal drugs Radix Angelicae dahuricae (Baizhi), Rhizome Ligustici (Chuanxiong) and Folium Camelliae sinensis (green tea) for the treatment of migraine. In this study, we found that TFY could significantly reduce the writhing times induced by acetic acid and licking foot response induced by formalin, and extend the writhing latent period. But the analgesic effect was not observed at hot-plate test. Meanwhile, experimental migrainous model induced by nitroglycerin was used to investigate the therapeutic effect of TFY. Compared with the control group, the levels of plasma calcitonin gene related to peptide (CGRP), serum nitric oxide (NO) and contents of brain dopamine (DA) in TFY administration groups were significantly decreased, and the levels of plasma endothelin (ET) and contents of brain 5-hydroxytryptamine (5-HT) and norepinephrine (NE) were remarkably increased, also the ratio of ET/NO was clearly corrected. Furthermore, the improving effect of behavior abnormality was observed in TFY administration rats. Meanwhile, isolated vascular ring test indicated that TFY had an significant effect on vasomotion, and antagonize vasospasm; moreover TFY also could increase cerebral blood flow (CBF) and reduce cerebrovascular resistance index (RI) in normal rabbits, which verified the effect of TFY on vasomotion and abnormal hemorheology. All the results indicate that TFY has an effective therapeutical action on migraine, which may be related to three aspects as following: firstly, adjusting the level of neurotransmitters, neuropeptides and vasoactive substances, relieving neurogenic inflammation; secondly, improving vasomotion, increase cerebral blood flow

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

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

    1998-01-01

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

  8. Survey of Current Experimental Studies of Effects of Traditional Chinese Medicine on Peripheral Nerve Regeneration

    WU Qun-li; LIANG Xiao-chun

    2006-01-01

    The repairing and regeneration of peripheral nerves is a very complex biological and cytological process, its mechanism is unclear so far, and thus results in the lack of specific and effectual therapy and medicament. Chinese herbs and their effective components have their own inimitable predominance in promoting peripheral nerve regeneration, such as their multi-factorial, multi-target and multi-functional action, abundant source, inexpensive, etc. In this paper, the experimental studies reported in recent 5 years concerning the effects of Chinese herbs or their active components on peripheral nerve repairing and regeneration are reviewed in respects of the integral level, cellular level, molecular level and gene level.

  9. Acid solution is a suitable medium for introducing QX-314 into nociceptors through TRPV1 channels to produce sensory-specific analgesic effects.

    He Liu

    Full Text Available BACKGROUND: Previous studies have demonstrated that QX-314, an intracellular sodium channel blocker, can enter into nociceptors through capsaicin-activated TRPV1 or permeation of the membrane by chemical enhancers to produce a sensory-selective blockade. However, the obvious side effects of these combinations limit the application of QX-314. A new strategy for targeting delivery of QX-314 into nociceptors needs further investigation. The aim of this study is to test whether acidic QX-314, when dissolves in acidic solution directly, can enter into nociceptors through acid-activated TRPV1 and block sodium channels from the intracellular side to produce a sensory-specific analgesic effect. METHODOLOGY/PRINCIPAL FINDINGS: Acidic solution or noradrenaline was injected intraplantarly to induce acute pain behavior in mice. A chronic constrictive injury model was performed to induce chronic neuropathic pain. A sciatic nerve blockade model was used to evaluate the sensory-specific analgesic effects of acidic QX-314. Thermal and mechanical hyperalgesia were measured by using radiant heat and electronic von Frey filaments test. Spinal Fos protein expression was determined by immunohistochemistry. The expression of p-ERK was detected by western blot assay. Whole cell clamp recording was performed to measure action potentials and total sodium current in rats DRG neurons. We found that pH 5.0 PBS solution induced behavioral hyperalgesia accompanied with the increased expression of spinal Fos protein and p-ERK. Pretreatment with pH 5.0 QX-314, and not pH 7.4 QX-314, alleviated pain behavior, inhibited the increased spinal Fos protein and p-ERK expression induced by pH 5.0 PBS or norepinephrine, blocked sodium currents and abolished the production of action potentials evoked by current injection. The above effects were prevented by TRPV1 channel inhibitor SB366791, but not by ASIC channel inhibitor amiloride. Furthermore, acidic QX-314 employed adjacent to the

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

    Wang Wen

    2011-01-01

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

  11. 酒大黄的镇痛抗炎作用%Analgesic and Anti-inflammatory Effect of Prepared Rhei Radix et Rhizoma with Wine

    王梅; 陈俊荣; 宋翠荣; 王国明; 赵超

    2013-01-01

    目的:观察酒大黄的镇痛抗炎作用.方法:采用小鼠热板法和小鼠扭体法观察酒大黄(2,1,0.5 g·kg-1·d-1,ig连续7d)的镇痛作用,采用小鼠耳肿胀法和小鼠棉球肉芽肿法观察酒大黄(2,1,0.5 g·kg-1ig,连续7d)的抗炎作用.结果:酒大黄能提高热板法疼痛模型小鼠痛阈,抑制醋酸致小鼠扭体反应,并能抑制二甲苯致小鼠耳肿胀和皮下植入棉球所致的小鼠肉芽肿生成(均P<0.05).结论:酒大黄有良好的镇痛抗炎作用.%Objective:To investigate the analgesic and anti-inflammatory effect of prepared Rhei Radix et Rhizoma with wine. Method:The analgesic effects of prepared Rhei Radix et Rhizoma with wine were observed by hot-plate in mice and acetic acid writhing assay (2, 1, 0. 5 g ·kg-1, ig, for 7 d). The anti-inflammatory effect were observed by evaluating xylene-induced ear edema in mice and cotton ball-induced granuloma in mice (2, 1 , 0. 5 g ·kg-1, ig, for 7 d). Result:Prepared Rhei Radix et Rhizoma with wine could prolong the latent time of reaction on hot-plate in mice, and reduce the wristle reaction times in mice. It could inhibit the ear edema caused by xylene in mice and the granuloma hyperplasia caused by cotton ball (all P < 0. 05 ). Conclusion:Prepared Rhei Radix et Rhizoma with wine has anti-inflammatory and analgesic effect.

  12. Evaluation of analgesic effect of two different doses of fentanyl in combination with bupivacaine for surgical site infiltration in cases of modified radical mastoidectomy: A double blind randomized study

    Bhandari, Geeta; Shahi, Kedar Singh; Parmar, Nitish Kumar; Asad, Mohammad; Joshi, Hemchandra Kumar; Bhakuni, Rajni

    2013-01-01

    Background: Limited evidence supports the efficacy of peripheral route fentanyl and local anesthetic combination for postoperative analgesia. Our study was therefore designed to demonstrate the analgesic efficacy of two different doses of fentanyl in combination with bupivacaine for surgical site infiltration in patients undergoing modified radical mastoidectomy (MRM). Materials and Methods: 60 patients undergoing MRM under general anesthesia were randomly allocated into two groups, first group receiving 0.5% bupivacaine at a dose of 2 mg/kg body weight with 50 μg fentanyl and second group receiving bupivacaine 0.5% at a dose of 2 mg/kg body weight with 100 μg fentanyl as infiltration of operative field in and around the incision site, after the incision and just before completion of surgery. In postoperative period pain, nausea-vomiting and sedation was recorded at 0 hr, 2, 4, 6, 12 and 24 hrs. Results: Both the combinations of bupivacaine and fentanyl (Group I and Group II) were effective for postoperative analgesia. In both the groups the Visual Analogue Scale (VAS) score was less than 3 at each time interval. None of the patients required rescue analgesia. The comparison of VAS scores at different intervals showed that group II had lower VAS scores at all time points. Conclusions: Fentanyl and bupivacaine combinations in doses of 50 and 100 μg along with 0.5% bupivacaine at a fixed dose of 2 mg/kg body weight are effective in the management of postoperative pain. Patients who received 100 μg fentanyl (Group II) had lower VAS scores as compared to the patients who received 50 μg fentanyl (Group I) with similar side effects. PMID:25885841

  13. A Method for Functional Quantification of the Reflex Effect of Human Peripheral Nerve Stimulation

    Zehr, E. P.; Komiyama, Tomoyushi; Stein, R B

    2000-01-01

    E.P. Zehr, KOMIYAMA, T. and R.B. Stein. A Method for Functional Quantification of the Reflex Effect of Human Peripheral Nerve Stimulation. Adv. Exerc. Sports Physiol., Vol.6, No.1 pp25-32, 2000. We have developed simple method that accounts for the overrall function of reflex effects occurring in the surface electrimyogran (EMG) after human nerve stimulation. This method involves the subtraction of pre-stimulus EMG levels from EMG modulation curves obtained after human peripheral nerve stimul...

  14. Verapamil enhanced the analgesic effect of ketamine in mice%维拉帕米增强氯胺酮对小鼠的镇痛作用

    武玉清; 周成华; 张永

    2011-01-01

    目的:观察钙通道拮抗剂维拉帕米对静脉麻醉药氯胺酮镇痛效应的影响.方法:取40只小鼠,雌雄各半,随机分为4组:生理盐水对照组(NS)、氯胺酮处理组(K)、维拉帕米处理组(V)、维拉帕米和氯胺酮联合用药组(V+K),通过醋酸致小鼠扭体法观察小鼠给药后扭体潜伏期和次数的变化.另取40只小鼠,雌雄各半,随机分为上述4组,利用甩尾实验分别观察给药后小鼠对热水和冰水痛阙值的改变.结果:维拉帕米单独用药对小鼠扭体潜伏期和次数、热水和冰水痛阈值均无显著影响;氯胺酮能够延长醋酸致小鼠扭体的潜伏期,并且减少醋酸致小鼠扭体的次数,升高小鼠对热水和冰水甩尾痛阈值;而维拉帕米能够进一步增强氯胺酮延长小鼠扭体潜伏期,减少扭体次数和升高小鼠甩尾痛阈值的效应.结论:维拉帕米能够显著增强氯胺酮对小鼠的镇痛效应.%AIM; To observe the analgesic effects of ketamine combind with verapamil in mice. METHODS: 40 mice were randomly divided into 4 groups: normal saline group (NS), ketamine group (K), verapamil group (V) and verapamil combind with ketamine group (V + K). The method of stretching induced by acetic acid was adopted. In another experiment, 40 mice were randomly divided into 4 groups above. The pain thresholds of mice to hot and ice water were observed through tail-flick experiment.RESULTS: Ketamine prolonged stretching latent time and reduced the stretching times. In addition, ketamine increased tail-flick pain threshold to hot or ice water. These analgesic effects of ketamine were markedly enhanced by verapamil. CONCLUSION: Verapamil can significantly enhance the analgesic effect of ketamine in mouse.

  15. Sedative and Analgesic Effects of Propofol-Fentanyl Versus Propofol-Ketamine During Endoscopic Retrograde Cholangiopancreatography: A Double-Blind Randomized Clinical Trial

    Bahrami Gorji, Fakhroddin; Amri, Parviz; Shokri, Javad; Alereza, Hakimeh; Bijani, Ali

    2016-01-01

    Background Endoscopic retrograde cholangiopancreatography (ERCP) is a painful procedure that requires analgesia and sedation. Objectives In this study, we compared the analgesic and sedative effects of propofol-ketamine versus propofol-fentanyl in patients undergoing ERCP. Methods In this clinical trial, 72 patients, aged 30 - 70 years old, who were candidates for ERCP were randomly divided into two groups. Before the start of ERCP, both groups received midazolam 0.5 - 1 mg. The intervention group (PK) received ketamine 0.5 mg/kg, and the control group (PF) received fentanyl 50 - 100 micrograms. All patients received propofol 0.5 mg/kg in a loading dose followed by 75 mcg/kg/minute in an infusion. The patients, the anesthesiologist, and the endoscopist were unaware of the medication regimen. Sedation and analgesia quality (based on a VAS), blood pressure, respiratory rate, heart rate, arterial oxygen saturation, recovery time (based on Aldrete scores), and endoscopist and patient satisfation were recorded. Results The sedative effects were equal in the two groups (P > 0.05), but the analgesic effects were higher in the PF group than in the PK group (P 0.05). Endoscopist satisfaction, patient satisfaction, and recovery time showed no significant differences between the two groups (P > 0.05). Conclusions The results showed that the sedative effect of propofol-ketamine was equal to the propofol-fentanyl combination during ERCP. To prevent respiratory and hemodynamic complications during ERCP, the propofol-ketamine combination should be used in patients with underlying disease. PMID:27853681

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

    Ali Pourmotabbed

    2010-06-01

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

  17. 小茴香挥发油的抗炎镇痛作用%Anti-inflammatory and Analgesic Effects of Volatile Oil Extracted from Foeniculum vulgare Mill. Seeds

    滕光寿; 刘曼玲; 毛峰峰; 韩燕; 杨鹏; 石磊; 畅敏

    2011-01-01

    Objective: To study the efects of anti-inflammatory and analgesic of volatile oil extracted from Foeniculum vulgare Mill.Seeds and offer pharmacological and experimental basis for its safe and effective use in clinic.Methods: The pharmacodynamic effects were obsersed in three experimental models of inflammation and pain: (l)mouse auricular edema induced by xylen; (2) Feet tumefaction caused by albumen in rats; (3)writhing induced by acetic acid in mice.Results: Volatile oil from Foeniculum vulgare Mill.Seeds could distinctively inhibit the inflammatory edema caused by various inflammatory agents and reduce the times of writhe induced by acetic acid in mice.Conclusion: Volatile oil from Foeniculum vulgare Mill.Seeds has analgesic effect and could inhibit inflammation in animals.%目的:研究小茴香挥发油的抗炎、镇痛作用,为指导临床合理用药提供科学依据.方法:应用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足肿胀2种动物模型进行抗炎药效学实验;采用醋酸致小鼠扭体反应进行镇痛实验.结果:小茴香挥发油能显著抑制上述各种动物模型的炎症反应及醋酸引起的小鼠扭体反应.结论:小茴香挥发油具有抗炎和镇痛作用.

  18. Analgesic and antihyperalgesic effects of melatonin in a human inflammatory pain model: a randomized, double-blind, placebo-controlled, three-arm crossover study.

    Andersen, Lars P H; Gögenur, Ismail; Fenger, Andreas Q; Petersen, Marian C; Rosenberg, Jacob; Werner, Mads U

    2015-11-01

    Antinociceptive effects of melatonin have been documented in a wide range of experimental animal models. The aim of this study was to investigate the analgesic, antihyperalgesic, and anti-inflammatory properties of melatonin using a validated burn injury (BI) model in healthy male volunteers. The design was a randomized, double-blind, placebo-controlled, three-arm crossover study. Each volunteer participated in 3 identical study sessions with intravenous administration of placebo, melatonin 10 mg, or melatonin 100 mg. Sixty minutes after bolus injection of study medication, a BI was induced by a computerized contact thermode (47.0°C, 420 seconds, 5.0 × 2.5 cm). Pain ratings during the BI and quantitative sensory testing at baseline and at 1, 2, 4, and 6 hours after the BI were performed. Quantitative sensory testing included assessments of secondary hyperalgesia areas, mechanical and thermal thresholds in the BI area, and pressure algometry. Furthermore, markers of inflammation, skin-reflectance spectrophotometry, and high-resolution ultrasonography were applied to measure skin erythema and dermal thickness in the BI area. Pain during the BI and secondary hyperalgesia areas were defined as primary outcomes. Twenty-nine volunteers were randomized and completed the study. While the BI induced large secondary hyperalgesia areas and significantly increased the markers of inflammation, no significant effects of melatonin were observed with respect to primary or secondary outcomes, compared with placebo. The administration of melatonin was not associated with any adverse effects. Melatonin did not demonstrate any analgesic, antihyperalgesic, or anti-inflammatory properties in the BI model.

  19. Full inhibition of spinal FAAH leads to TRPV1-mediated analgesic effects in neuropathic rats and possible lipoxygenase-mediated remodeling of anandamide metabolism.

    Starowicz, Katarzyna; Makuch, Wioletta; Korostynski, Michal; Malek, Natalia; Slezak, Michal; Zychowska, Magdalena; Petrosino, Stefania; De Petrocellis, Luciano; Cristino, Luigia; Przewlocka, Barbara; Di Marzo, Vincenzo

    2013-01-01

    Neuropathic pain elevates spinal anandamide (AEA) levels in a way further increased when URB597, an inhibitor of AEA hydrolysis by fatty acid amide hydrolase (FAAH), is injected intrathecally. Spinal AEA reduces neuropathic pain by acting at both cannabinoid CB1 receptors and transient receptor potential vanilloid-1 (TRPV1) channels. Yet, intrathecal URB597 is only partially effective at counteracting neuropathic pain. We investigated the effect of high doses of intrathecal URB597 on allodynia and hyperalgesia in rats with chronic constriction injury (CCI) of the sciatic nerve. Among those tested, the 200 µg/rat dose of URB597 was the only one that elevated the levels of the FAAH non-endocannabinoid and anti-inflammatory substrates, oleoylethanolamide (OEA) and palmitoylethanolamide (PEA), and of the endocannabinoid FAAH substrate, 2-arachidonoylglycerol, and fully inhibited thermal and tactile nociception, although in a manner blocked almost uniquely by TRPV1 antagonism. Surprisingly, this dose of URB597 decreased spinal AEA levels. RT-qPCR and western blot analyses demonstrated altered spinal expression of lipoxygenases (LOX), and baicalein, an inhibitor of 12/15-LOX, significantly reduced URB597 analgesic effects, suggesting the occurrence of alternative pathways of AEA metabolism. Using immunofluorescence techniques, FAAH, 15-LOX and TRPV1 were found to co-localize in dorsal spinal horn neurons of CCI rats. Finally, 15-hydroxy-AEA, a 15-LOX derivative of AEA, potently and efficaciously activated the rat recombinant TRPV1 channel. We suggest that intrathecally injected URB597 at full analgesic efficacy unmasks a secondary route of AEA metabolism via 15-LOX with possible formation of 15-hydroxy-AEA, which, together with OEA and PEA, may contribute at producing TRPV1-mediated analgesia in CCI rats.

  20. Full inhibition of spinal FAAH leads to TRPV1-mediated analgesic effects in neuropathic rats and possible lipoxygenase-mediated remodeling of anandamide metabolism.

    Katarzyna Starowicz

    Full Text Available Neuropathic pain elevates spinal anandamide (AEA levels in a way further increased when URB597, an inhibitor of AEA hydrolysis by fatty acid amide hydrolase (FAAH, is injected intrathecally. Spinal AEA reduces neuropathic pain by acting at both cannabinoid CB1 receptors and transient receptor potential vanilloid-1 (TRPV1 channels. Yet, intrathecal URB597 is only partially effective at counteracting neuropathic pain. We investigated the effect of high doses of intrathecal URB597 on allodynia and hyperalgesia in rats with chronic constriction injury (CCI of the sciatic nerve. Among those tested, the 200 µg/rat dose of URB597 was the only one that elevated the levels of the FAAH non-endocannabinoid and anti-inflammatory substrates, oleoylethanolamide (OEA and palmitoylethanolamide (PEA, and of the endocannabinoid FAAH substrate, 2-arachidonoylglycerol, and fully inhibited thermal and tactile nociception, although in a manner blocked almost uniquely by TRPV1 antagonism. Surprisingly, this dose of URB597 decreased spinal AEA levels. RT-qPCR and western blot analyses demonstrated altered spinal expression of lipoxygenases (LOX, and baicalein, an inhibitor of 12/15-LOX, significantly reduced URB597 analgesic effects, suggesting the occurrence of alternative pathways of AEA metabolism. Using immunofluorescence techniques, FAAH, 15-LOX and TRPV1 were found to co-localize in dorsal spinal horn neurons of CCI rats. Finally, 15-hydroxy-AEA, a 15-LOX derivative of AEA, potently and efficaciously activated the rat recombinant TRPV1 channel. We suggest that intrathecally injected URB597 at full analgesic efficacy unmasks a secondary route of AEA metabolism via 15-LOX with possible formation of 15-hydroxy-AEA, which, together with OEA and PEA, may contribute at producing TRPV1-mediated analgesia in CCI rats.

  1. Full Inhibition of Spinal FAAH Leads to TRPV1-Mediated Analgesic Effects in Neuropathic Rats and Possible Lipoxygenase-Mediated Remodeling of Anandamide Metabolism

    Starowicz, Katarzyna; Makuch, Wioletta; Korostynski, Michal; Malek, Natalia; Slezak, Michal; Zychowska, Magdalena; Petrosino, Stefania; De Petrocellis, Luciano; Cristino, Luigia; Przewlocka, Barbara; Di Marzo, Vincenzo

    2013-01-01

    Neuropathic pain elevates spinal anandamide (AEA) levels in a way further increased when URB597, an inhibitor of AEA hydrolysis by fatty acid amide hydrolase (FAAH), is injected intrathecally. Spinal AEA reduces neuropathic pain by acting at both cannabinoid CB1 receptors and transient receptor potential vanilloid-1 (TRPV1) channels. Yet, intrathecal URB597 is only partially effective at counteracting neuropathic pain. We investigated the effect of high doses of intrathecal URB597 on allodynia and hyperalgesia in rats with chronic constriction injury (CCI) of the sciatic nerve. Among those tested, the 200 µg/rat dose of URB597 was the only one that elevated the levels of the FAAH non-endocannabinoid and anti-inflammatory substrates, oleoylethanolamide (OEA) and palmitoylethanolamide (PEA), and of the endocannabinoid FAAH substrate, 2-arachidonoylglycerol, and fully inhibited thermal and tactile nociception, although in a manner blocked almost uniquely by TRPV1 antagonism. Surprisingly, this dose of URB597 decreased spinal AEA levels. RT-qPCR and western blot analyses demonstrated altered spinal expression of lipoxygenases (LOX), and baicalein, an inhibitor of 12/15-LOX, significantly reduced URB597 analgesic effects, suggesting the occurrence of alternative pathways of AEA metabolism. Using immunofluorescence techniques, FAAH, 15-LOX and TRPV1 were found to co-localize in dorsal spinal horn neurons of CCI rats. Finally, 15-hydroxy-AEA, a 15-LOX derivative of AEA, potently and efficaciously activated the rat recombinant TRPV1 channel. We suggest that intrathecally injected URB597 at full analgesic efficacy unmasks a secondary route of AEA metabolism via 15-LOX with possible formation of 15-hydroxy-AEA, which, together with OEA and PEA, may contribute at producing TRPV1-mediated analgesia in CCI rats. PMID:23573230

  2. Comparing the analgesic effect of caudal and ilioinguinal iliohypogastric nerve blockade using bupivacaine-clonidine in inguinal surgeries in children 2-7 years old

    Mahin Seyedhejazi

    2014-01-01

    Full Text Available Background: We compared the analgesic effects of caudal and ilioinguinal-iliohypogastric nerve block using bupivacaine-clonidine performed in children undergoing inguinal hernia repair. The ilioinguinal-iliohypogastric nerve block provides excellent pain relief for operations on the inguinal region, including emergency procedures (e.g. strangulated inguinal hernia with intestinal obstruction. It should be preferred to caudal block for these procedures. Materials and Methods: After local ethics committee approval and written parental consent, 67 ASA class I - II patients aged between 2-7 years old scheduled for elective inguinal hernia repair were allocated randomly into two groups after general anesthesia with same drugs in both groups. Group C received caudal block with 1 ml/kg bupivacaine 0.25% combined with 1 μg/kg clonidine, and group I received ilioinguinal- iliohypogastric nerve block with 0.3 ml /kg bupivacaine 0.25% combined with 1 μg/kg clonidine. Blood pressure and heart rate were documented every 5 minutes. Post-operative analgesia, analgesic use and side-effects were assessed during first 24 hours. Results: In group C, 7 / 34 and in group I, 12/33 patients required post-operative analgesia (P = 0.174. Five patients (15.5% in group I and one patient (2.94% in group C had severe pain after operation. Systolic and diastolic blood pressure decreased during operation, but the differences between two groups were not significant (P = 0.176, P = 0.111. Heart rate changes between two groups were insignificant (P = 0.182. Conclusion: It seems that in children, caudal epidural block and ilioinguinal - iliohypogastric nerve block using bupivacaine-clonidine have comparable effects on analgesia, severity of pain and hemodynamic changes during and after surgery on inguinal region.

  3. 眼镜蛇长链神经毒素镇痛效应及可能机制%Analgesic effect of cobratoxin and its possible mechanism

    彭建明; 苏兰娣; 罗雪; 叶记林; 于有江

    2015-01-01

    Objective To investigate the analgesic effect of cobratoxin (CBT) and its possible mechanisms. Methods The pain-evoked discharge from the spinal dorsal horn neurons in rats with chronic pain was recorded by the somatic extracellular record method. The 6 experimental rat groups were injected by the normal saline (5μL),CBT(20,40,80 ng/kg),atropine(2 mg/kg) and atropine(2 mg/kg)+CBT(40 ng/kg) respectively. The influence of different concentrations of CBT on the pain-evoked discharge from the spinal dorsal horn neurons was observed. At the same time ,whether cholinergic receptor antagonist atropine overturning its analgesic effect was observed too. Results The different concentrations of CBT could obviously inhibit the pain-evoked discharge from the spinal dorsal horn neuron in rats with chronic pain ,the discharge frequency had statistically significant difference between the different concentration and the normal saline group (P<0.05),moreover the effect could be blocked by atropine , the difference of the discharge frequency at 20,30,40,50,60 min had statistical difference between the atropine+CBT group and the CBT 40 ng/kg group(P<0.05). Conclusion CBT possesses a significant analgesic effect,this effect has certain dose dependence and the cholinergic receptor system participates in this analgesic process.%目的:探究眼镜蛇长链神经毒素(CBT)的镇痛作用及可能机制。方法采用在体细胞外记录方法记录慢性炎症痛模型大鼠脊髓背角神经元的痛诱发放电,分别对六组实验大鼠注射生理盐水(5μL)、CBT(20、40、80 ng/kg)、阿托品(2 mg/kg)、阿托品(2 mg/kg)+CBT(40 ng/kg),观察不同含量CBT对脊髓背角神经元痛诱发放电的影响,同时观察胆碱能受体拮抗剂阿托品能否翻转其镇痛效应。结果不同含量CBT均可以显著抑制慢性炎症痛大鼠脊髓背角神经元的痛诱发放电,各含量CBT组放电频率与生理盐水组比较,差

  4. EXPERIMENTAL EVALUATION FOR ANALGESIC ACTIVITY OF MAMSYADI KWATHA

    Shreevathsa

    2011-04-01

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

  5. Central and peripheral testosterone effects in men with heart failure: An approach for cardiovascular research

    ?eljko; Bu?i?; Viktor; ?uli?

    2015-01-01

    Heart failure(HF) is a syndrome recognized as a health problem worldwide. Despite advances in treatment, patients with HF still have increased morbidity and mortality. Testosterone is one of the most researched hormones in the course of HF. Growing interest regarding the effect of testosterone, on a variety of body systems, has increased the knowledge about its mechanisms of action. The terms central and peripheral effects are used to distinguish the effects of testosterone on cardiac and extracardiac structures. Central effects include influences on cardiomyocytes and electrophysiology. Peripheral effects include influences on blood vessels, baroreceptor reactivity, skeletal muscles and erythropoesis. Current knowledge about peripheral effects of testosterone may explain much about beneficiary effects in the pathophysiology of HF syndrome. However, central, i.e., cardiac effects of testosterone are to be further explored.

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

    Naumenko L.Yu.

    2010-01-01

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

  7. The effect of instruction in analgesic use compared with neuromuscular exercise on knee-joint load in patients with knee osteoarthritis

    Holsgaard-Larsen, Anders; Clausen, Brian; Søndergaard, Jens

    2017-01-01

    OBJECTIVE: To investigate the effect of a NEuro-Muscular EXercise (NEMEX) therapy program compared with instructions in optimized analgesics and anti-inflammatory drug use (PHARMA), on measures of knee-joint load in people with mild to moderate knee osteoarthritis. We hypothesized that knee joint...... loading during walking would be reduced by NEMEX and potentially increased by PHARMA. DESIGN: Single-blind, RCT comparing NEMEX therapy twice a week with PHARMA. Participants with mild-to-moderate medial tibiofemoral knee osteoarthritis were randomly allocated (1:1) to one of two 8-week treatments....... Primary outcome was change in knee load during walking (Knee Index, a composite score from all three planes based on 3D movement analysis) after 8 weeks of intervention. Secondary outcomes were frontal plane peak knee adduction moment (KAM), Knee Injury and Osteoarthritis Outcome Scores (KOOS...

  8. Analgesic and anti-Inflammatory effect of UP3005, a botanical composition Containing two standardized extracts of Uncaria gambir and Morus alba

    Mesfin Yimam

    2015-01-01

    Full Text Available Background: Osteoarthritis (OA is a chronic debilitating degenerative joint disease characterized by cartilage degradation and synovial inflammation exhibited by clinical symptoms such as joint swelling, synovitis, and inflammatory pain. Present day pain relief therapeutics heavily relies on the use of prescription and over the counter nonsteroidal anti-inflammatory drugs as the first line of defense where their long-term usage causes detrimental gastrointestinal and cardiovascular-related side-effects. As a result, the need for evidence based safer and efficacious alternatives from natural sources to overcome the most prominent and disabling symptoms of arthritis is a necessity. Materials and Methods: Describe the anti-inflammatory and analgesic effect of UP3005, a composition that contains a standardized blend of two extracts from the leaf of Uncaria gambir and the root bark of Morus alba in carrageenan-induced rat paw edema, abdominal constriction (writhing′s and ear swelling assays in mouse with oral dose ranges of 100-400 mg/kg. Results: In vivo, statistically significant improvement in pain resistance, and suppression of paw edema and ear thickness in animals treated with UP3005 were observed compared with vehicle-treated diseased rats and mice. Ibuprofen was used a reference compound in all the studies. In vitro, enzymatic inhibition activities of UP3005 were determined with IC50 values of 12.4 μg/ml, 39.8 μg/ml and 13.6 μg/ml in cyclooxygenase-2 (COX-1, COX-2 and lipoxygenase (5-LOX enzyme activity assay, respectively. Conclusions: These data suggest that UP3005, analgesic and anti-inflammatory agent of botanical origin with balanced dual COX-LOX inhibition activity, could potentially be used for symptom management of OA.

  9. Analgesic effect of Facebook: Priming with online social networking may boost felt relatedness that buffers against physical pain.

    Ho, Liang-Chu; Wu, Wen-Hsiung; Chiou, Wen-Bin

    2016-10-01

    Social networking sites (SNSs) are extremely popular for providing users with a convenient platform for acquiring social connections and thereby feeling relatedness. Plenty of literature has shown that mental representations of social support can reduce the perception of physical pain. The current study tested whether thinking about SNS would interfere with users' perceptions of experimentally induced pain. Ninety-six undergraduate Facebook users were recruited to participate in a priming-based experiment. They were randomly assigned to one of the three study conditions (SNS prime, neutral prime, or no prime) via rating the aesthetics of logos. The results showed that participants exposed to SNS primes reported less pain of immersion in hot water than did both control groups (neutral- and no-prime). Felt relatedness mediated the link between SNS primes and diminished pain perceptions. This research provides the first demonstration that thinking about SNS can lower experienced physical pain among Facebook users. Online social networking may serve as an analgesic buffer against pain experience than previously thought. The SNS-enabled analgesia has far reaching implications for pain relief applications and the enhancement of well-being in human-interaction techniques.

  10. Intraoperative nitrous oxide as a preventive analgesic.

    Stiglitz, D K; Amaratunge, L N; Konstantatos, A H; Lindholm, D E

    2010-09-01

    Preventive analgesia is defined as the persistence of the analgesic effects of a drug beyond the clinical activity of the drug. The N-methyl D-aspartate receptor plays a critical role in the sensitisation of pain pathways induced by injury. Nitrous oxide inhibits excitatory N-methyl D-aspartate sensitive glutamate receptors. The objective of our study was to test the efficacy of nitrous oxide as a preventive analgesic. We conducted a retrospective analysis of data from a subset of patients (n = 100) randomly selected from a previous major multicentre randomised controlled trial on nitrous oxide (ENIGMA trial). Data analysed included postoperative analgesic requirements, pain scores and duration of patient-controlled analgesia during the first 72 postoperative hours. There was no significant difference in postoperative oral morphine equivalent usage (nitrous group 248 mg, no nitrous group 289 mg, mean difference -43 mg, 95% confidence interval 141 to 54 mg). However, patients who received nitrous oxide had a shorter duration of patient-controlled analgesia use (nitrous group 35 hours, no nitrous group 51 hours, mean difference -16 hours, 95% confidence interval -29 to -2 hours, P = 0.022). There was no difference in pain scores between the groups. The shorter patient-controlled analgesia duration in the nitrous oxide group suggests that intraoperative nitrous oxide may have a preventive analgesic effect.

  11. Peripheral morphine analgesia in dental surgery.

    Likar, R; Sittl, R; Gragger, K; Pipam, W; Blatnig, H; Breschan, C; Schalk, H V; Stein, C; Schäfer, M

    1998-05-01

    The recent identification of opioid receptors on peripheral nerve endings of primary afferent neurons and the expression of their mRNA in dorsal root ganglia support earlier experimental data about peripheral analgesic effects of locally applied opioids. These effects are most prominent under localized inflammatory conditions. The clinical use of such peripheral analgesic effects of opioids was soon investigated in numerous controlled clinical trials. The majority of these have tested the local, intraarticular administration of morphine in knee surgery and have demonstrated potent and long-lasting postoperative analgesia. As the direct application of morphine into the pain-generating site of injury and inflammation appears most promising, we examined direct morphine infiltration of the surgical site in a unique clinical model of inflammatory tooth pain. Forty-four patients undergoing dental surgery entered into this prospective, randomized, double-blind study. Before surgery they received, together with a standard local anesthetic solution (articaine plus epinephrine) a submucous injection of either 1 mg of morphine (group A) or saline (group B). Postoperative pain intensity was assessed using the visual analog scale (VAS) and numeric rating scale (NRS) at 2, 4, 6, 8, 10, 12, 16, 20 and 24 h after surgery. In addition, patients recorded the occurrence of side effects and the supplemental consumption of diclofenac tablets. Results of 27 patients were analyzed (group A: n=14, group B: n=13). Pain scores which were moderate to severe preoperatively were reduced to a similar extent in both groups up to 8 h postoperatively. Thereafter, pain scores in group A were significantly lower than those in group B for up to 24 h, demonstrating the analgesic efficacy of additional morphine. The time to first analgesic intake and the total amount of supplemental diclofenac were less in group A than in group B. No serious side effects were reported. Our results show that 1 mg of

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

    Torrades Sandra

    2011-01-01

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

  13. Reply to "Analgesic Effect of Gabapentin on Post-Operative Pain After Arthroscopic Anterior Cruciate Ligament Reconstruction"

    Mohsen Mardani-Kivi

    2014-03-01

    Full Text Available In Reply Dr. Ortiz and Dr. Romero-Quezada evaluated our study precisely and authors are grateful for their great survey on our article. There were some questions and concerns that we are going to answer. We wish it could help others to come up with better ideas and conclusions. 1. ACL tear may occur in two scenarios and we believe that there is not a third one: 1st- the ACL injury functionally disables the patient and becomes symptomatic; in this scenario the patient would suffer from giving way and the “Lachman test” is definitely positive (3+ or 4+ (1. Intra-operatively (post anesthesia “Pivot shift test” is almost positive in all cases. 2nd- ACL injury does not conflict with the patient’s routine and social activity and giving way are usually negative and Lachman test can be negative, 1+ and in the most severe condition 2+ positive. Partial ACL tear may be reported in MRI, however authors believe these cases do not benefit from a surgical intervention, and conservative treatment should be performed. 2. Although most of our patients were suffered from sports trauma, mechanisms of ACL tears were not the same in all patients. The duration between traumas to surgeries in all patients enrolled in this study were at least 6 weeks which were included the proceeding from acute trauma phase to performing physical therapy and accomplishing full range of motion pre-operatively. Since the present study was not about surgical technique and pre or post rehab protocols and programs, authors avoided such additional issues. 3. About Pethidine issue, this drug is the main protocol one in our hospital to provide analgesics for post-operative pain, so authors routinely decided to utilize the pethidine as analgesics such as recent relative article (2. We used the pethidine intravenously and by patient’s demand; if a patients requested for pain killers, we provided him/her with 0.5 mg-per-Kg pethidine which was injected intravenously. The time and

  14. Non-analgesic effects of opioids: opioid-induced nausea and vomiting: mechanisms and strategies for their limitation.

    Coluzzi, Flaminia; Rocco, Alessandra; Mandatori, Ilenia; Mattia, Consalvo

    2012-01-01

    Nausea and vomiting are common gastrointestinal symptoms following opioid administration, for either chronic or acute pain management. As a consequence, patients' dissatisfaction has a negative impact on treatment efficacy. A number of mechanisms have been identified, involving both central and peripheral sites. This article will review the pathophysiology of opioid-induced nausea and vomiting and the various pharmacological treatments currently available for its management. Preventive strategies and therapeutic approaches are evaluated in the perioperative setting and in chronic pain. Newer drugs include second generation serotonin receptor antagonists (palonosetron) and neurokinin-1 (NK-1) antagonists (aprepitant).

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

    Khaled Taha

    2003-09-01

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

  16. Endocannabinoids and pain: spinal and peripheral analgesia in inflammation and neuropathy.

    Rice, A S C; Farquhar-Smith, W P; Nagy, I

    2002-01-01

    Analgesia is an important physiological function of the endocannabinoid system and one of significant clinical relevance. This review discusses the analgesic effects of endocannabinoids at spinal and peripheral levels, firstly by describing the physiological framework for analgesia and secondly by reviewing the evidence for analgesic effects of endocannabinoids obtained using animal models of clinical pain conditions. In the spinal cord, CB(1) receptors have been demonstrated in laminae of the dorsal horn intimately concerned with the processing of nociceptive information and the modulation thereof. Similarly, CB(1) receptors have been demonstrated on the cell bodies of primary afferent neurones; however, the exact phenotype of cells which express this receptor requires further elucidation. Local administration, peptide release and electrophysiological studies support the concept of spinally mediated endocannabinoid-induced analgesia. Whilst a proportion of the peripheral analgesic effect of endocannabinoids can be attributed to a neuronal mechanism acting through CB(1) receptors expressed by primary afferent neurones, the antiinflammatory actions of endocannabinoids, mediated through CB(2) receptors, also appears to contribute to local analgesic effects. Possible mechanisms of this CB(2)-mediated effect include the attenuation of NGF-induced mast cell degranulation and of neutrophil accumulation, both of which are processes known to contribute to the generation of inflammatory hyperalgesia. The analgesic effects of cannabinoids have been demonstrated in models of somatic and visceral inflammatory pain and of neuropathic pain, the latter being an important area of therapeutic need. Analgesia is one of the principal therapeutic targets of cannabinoids. This review will discuss the analgesic effects of endocannabinoids in relation to two areas of therapeutic need, persistent inflammation and neuropathic pain. The more general aspects of the role of cannabinoids

  17. Antipyretic,Analgesic and Anti-inflammatory Effects of Huangyu Cataplasm%黄萸巴布剂的解热、镇痛、抗炎作用

    石强

    2011-01-01

    Objective; To study the antipyretic, antinociceptive and anti-inflammatory effects of Huangyu cataplasm ( HYC). Method: The antipyretic effects of HYC were observed on febrile animals induced by three kinds of pyrogens including dry yeast,typhoid paratyphoik A,B vaccines,and milk,correspondingly. The analgesic effect was determined by writhing and hot plate tests in mice. Anti-inflammatory action was investigated on the model of paw edema caused by egg white and the pathological model with increasing vascular permeability induced by acetic acid in mice. Result;HYC had good antipyretic effects for experimental fever rabbits induced by dry yeast, typhoid paratyphoik A, B vaccines, and milk heating method. HYC could significantly inhibit the pain responses caused by hot plate and writhing responses induced by acetic acid. HYC could significantly decrease the degree of paw edema caused by egg white in mice and notably inhibit the degree of the increase in permeability of the capillaries. Conclusion; HYC shows considerable antipyretic,analgesic and anti-inflammatory effects%目的:观察黄萸巴布剂的解热、镇痛、抗炎作用.方法:分别采用干酵母、牛奶和伤寒、副伤寒甲、乙三联菌苗致热法观察黄萸巴布剂对3种致热原所致动物发热的影响;采用扭体法和热板法观察黄萸巴布剂的镇痛作用;采用蛋清致大鼠足跖肿胀法和醋酸致小鼠腹腔毛细血管通透性增高法观察黄萸巴布剂的抗炎作用.结果:黄萸巴布剂可显著抑制干酵母、牛奶、伤寒、副伤寒甲、乙三联菌苗所致发热反应;对醋酸和热板诱发的小鼠疼痛有明显的抑制作用;可减轻蛋清所致大鼠足跖肿胀度;降低醋酸引起的小鼠腹腔毛细血管通透性增高.结论:黄萸巴布剂具有明显的解热、镇痛和抗炎作用.

  18. The effect of stress on core and peripheral body temperature in humans

    Vinkers, Christiaan H.; Penning, Renske; Hellhammer, Juliane; Verster, Joris C.; Klaessens, John H. G. M.; Olivier, Berend; Kalkman, Cor J.

    2013-01-01

    Even though there are indications that stress influences body temperature in humans, no study has systematically investigated the effects of stress on core and peripheral body temperature. The present study therefore aimed to investigate the effects of acute psychosocial stress on body temperature u

  19. Analgesic Effects of Inhalation of Nitric Oxide (Entonox and Parenteral Morphine Sulfate in Patients with Renal Colic; A Randomized Clinical Trial

    Hamid Kariman

    2015-04-01

    Full Text Available Objective: To compare the analgesiceffects of Nitrous oxide and morphine sulfate in patients with acute renal colic due to urolithiasis. Methods: This was randomized clinical trial being performed in Imam Hossein hospital affiliated with Shahid Beheshti University of Medical Sciences during a 1-year period from May2013 to May2014. A total of number of 100 patients, with an age range of 20-50 years, who presented with renal colic secondary to urolithiasis confirmed by ultrasonography were randomly assigned to receive morphine sulfate injection (0.1 mg/kg with 100 mg diclofenac suppository (n=50 or Entonox exhalation (50% nitric oxide and 50% oxygenfor 30-minutes with 100 mg diclofenac suppository (n=50. Quantitative measurement was of pain was performed according to a visual analogue scale (VAS, before, 3, 5, 10 and 30-minute after the intervention. The pain severity and side effects were measured between two study groups. Results: The baseline characteristics of the patients in two study groups were comparable. The frequencies of pain persistence (at least 50% at 3-, 5-, 10- and 30-minute intervals in morphine sulfategroup were 96%, 80%, 50% and 8%, respectively; these frequencies in Entonex were 82%, 42%, 12% and 2%, respectively (p<0.001. Cox regression modeling showed that use of Entonox was the only effective agent in the success of treatment, compared to the use of morphine, i.e. use of Entonox increased the success of treatment up to 2.1 folds compared to the use of morphine (HR=2.1; 95% CI: 1.2-3.6; p=0.006. Conclusion: The results of the present study demonstrate that inhalation of Entonox is an effective and safe analgesic regimen for acute renal colic. It acts more rapidly and is more potent in relieving renal colic when compared to morphine sulfate.Entonox can be regarded as an appropriate alternative to analgesics like opioids in this ground. Clinical Trial Registry: The current study is registered with Iranian Registry for Clinical

  20. Comparative analysis of analgesic and anti-inflammatory activity of bark and leaves of Acacia ferruginea DC.

    Samriti Faujdar

    2016-03-01

    Full Text Available The aim of the present study was to investigate and compare the analgesic and anti-inflammatory activities of hydroalcoholic extracts of bark and leaves of Acacia ferruginea DC. Hydroalcoholic extracts of bark and leaves were evaluated for analgesic activity using hot plate method and acetic acid-induced writhing test, whereas the anti-inflammatory activity was evaluated by carrageenan-induced paw oedema method. Hydroalcoholic extract of the bark at the dose of 50 mg/kg (6.10 ± 0.30 and leaves at a dose of 100 mg/kg (5.72 ± 0.39 after 45 min exhibited significant (P < 0.001 analgesic activity in hot plate test, which was comparable to Tramadol (6.11 ± 0.31 at a dose of 10 mg/kg. However, in acetic acid-induced writhing test, hydroalcoholic extract of both bark (90% and leaves (90.91% showed maximum protection from acetic acid at the dose of 100 mg/kg as compared to standard drug (50.91% at a dose of 5 mg/kg. In the evaluation of anti-inflammatory activity, hydroalcoholic extract of leaves at a dose of 400 mg/kg had significantly (74.68% inhibited the inflammation as comparable to indomethacin (82.8% after 3 h of induction of carrageenan. It is concluded that hydroalcoholic extracts of bark and leaves have central analgesic and peripheral analgesic effects, respectively. Both hydroalcoholic extracts of the bark and leaves significantly reduced the paw oedema at a dose of 400 mg/kg and exhibited anti-inflammatory activity.

  1. Analgesic effect of Cestrum nocturnum L. extract on mice%夜来香提取物对小鼠的镇痛作用

    黄龙岗; 张乡城; 肖海; 叶和杨; 曾靖

    2006-01-01

    BACKGROUND: It has been considered that Cestrum nocturnum L. (CNL) has the effects of antiarrhythmia, local anesthesia and central inhibition.OBJECTIVE: To investigate the analgesic effect of CNL extract on mice,so as to find new drugs for clinical treatment of pain.DESIGN: A randomized control observation.SETTING: Center of Modern Education and Department of Pharmacology,Gannan Medical College.MATERIALS: The experiments were carried out in the laboratory of scientific research center, Gannan Medical College between March and April in 2005. ① A total of 150 healthy adult Kunming mice were used in four independent experiments. ② Drugs: CNL extract was provided by the Department of Phytochemistry, Shenyang Pharmaceutical University (batch number: 2002080901), morphine hydrochloride injection by Shenyang No.1Pharmaceutical Factory (batch number: 000305), and naloxone hydrochloride injection by Yanqiao (Hunan) Pharmaceutical Co. Ltd., (batch number:20021109).METHODS: ① Effects of CNL extract on writhing times induced by acetic acid: Forty female mice were randomly divided into four groups with 10 mice in each, and they were treated with intraperitoneal injections of 0.02 mL/g saline, 0.10 and 0.20 mg/g CNL extract and 0.10 mg/g aminophenazone respectively. The intraperineal injection of 6 g/L glacial acetic acid was given after 15 minutes. The writhing times of mice within 15 minutes were observed and recorded in each group. ② Effects of CNL extract on the pain induced by hot pla in mice: Forty female mice were randomly divided into four groups with 10 mice in each, and they were treated with intraperineal injections of 0.02 mL/g saline, 0. 10 and 0.20 mg/g CNL extract and 0.10 mg/g morphine respectively. The pain responses were detected at 15, 30 and 60 minutes after administration. ③ The antagonistic effect of naloxone on morphine and CNL extract to the pain induced by hot plate in mice: Thirty female mice were randomly divided into three groups ith 10 mice

  2. Study on the analgesic effect of oxysophocarpine and its mechanism%氧化槐果碱的镇痛作用及其机制研究

    刘红艳; 姚婉霞; 李玉香; 贺晓亮; 蒋袁絮; 余建强

    2011-01-01

    目的 研究氧化槐果碱(OSC)的镇痛作用及其作用机制.方法 采用小鼠热板法、温浴法、醋酸扭体法和甲醛致痛法,观察OSC的镇痛作用,并分析其镇痛作用与Ca2+的关系.结果 80、40 mg·kg-1 OSC可显著延长小鼠的热板反应舔足潜伏期(P<0.05,P<0.01);80、40、10 mg·k-1 OSC均可延长温浴致小鼠的缩尾潜伏期(P<0.05,P<0.01);80、40、10 mg·k-1OSC呈剂量依赖性抑制醋酸导致的小鼠扭体反应(P<0.05,P<0.01),并呈剂量依赖性抑制小鼠甲醛致痛的累计舔足时间(P<0.05,P<0.01);OSC延长小鼠热板反应舔后足潜伏期的作用可被CaCl2拮抗,而被维拉帕米增强.结论 OSC具有镇痛作用,其镇痛作用机制可能与Ca2+有关.%OBJECTIVE To observe the analgesic effect and its mechanism of oxysophocarpine(OSC). METHODS Adopting the hot plate test, the warm water tail - flick lest,the writhing test and the formalin test to observe the analgesic effect of OSC and analyze its association with calcium ions. RESULTS OSC of 80,40 mg. kg- 1 , could prolong the foot - licking latencies of mice in the hot plate test(P <0.05,P <0.01 );OSC of 80,40,10 mg·kg-1 ,could prolong the tail -curling latencies of mice in the warm water tail- flick test ( P < 0.05,P < 0.01 ); OSC of 80,40,10 mg. kg- 1, could significant dose - dependently inhibit the writhing reflex induced by acetic acid in mice( P <0.05 ,P < 0.01 ) ;OSC of 80,40,10 mg. kg - 1 remarkably and dose -dependently inhibited the two -phases pain in the formalin test(P <0.05,P <0.01 ) ;the antinociception of OSC could be antagonized by CaCl2 and enhanced by Verapamil. CONCLUSION Oxysophocarpine has analgesic effects, the mechanism may be related to calcium ions.

  3. Effect of visual stimulus using central and peripheral visual field on postural control of normal subjects.

    Park, Du-Jin

    2016-06-01

    [Purpose] This study investigated the effects of visual stimulus using central and peripheral vision fields on postural control. [Subjects and Methods] The subjects consisted of 40 young adult volunteers (15 males, 25 females) who had been informed of the study purpose and procedure. The subjects were randomly divided into four groups of differing visual stimulus. Each group was given visual intervention in a standing position for 3 minutes. Postural control was evaluated before and after visual intervention. [Results] The results of the functional reach test and body sway test showed significant differences among the four groups. [Conclusion] The two-way peripheral vision-field group showed significantly more body sway after visual intervention than the other three groups. This finding may suggest two-way peripheral vision field is a more effective visual stimulus for training postural control and balance.

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

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

    1985-01-01

    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.

  5. Analgesic effectiveness and tolerability of oral oxycodone/naloxone and pregabalin in patients with lung cancer and neuropathic pain: an observational analysis

    De Santis, Stefano; Borghesi, Cristina; Ricciardi, Serena; Giovannoni, Daniele; Fulvi, Alberto; Migliorino, Maria Rita; Marcassa, Claudio

    2016-01-01

    Introduction Cancer-related pain has a severe negative impact on quality of life. Combination analgesic therapy with oxycodone and pregabalin is effective for treating neuropathic cancer pain. We investigated the efficacy and tolerability of a dose-escalation combination therapy with prolonged-release oxycodone/naloxone (OXN-PR) and pregabalin in patients with non-small-cell lung cancer and severe neuropathic pain. Methods This was a 4-week, open-label, observational study. Patients were treated with OXN-PR and pregabalin. Average pain intensity ([API] measured on a 0–10 numerical rating scale) and neuropathic pain (Douleur Neuropathique 4) were assessed at study entry and at follow-up visits. The primary endpoint was response to treatment, defined as a reduction of API at T28 ≥30% from baseline. Secondary endpoints included other efficacy measures, as well as patient satisfaction and quality of life (Brief Pain Inventory Short Form), Hospital Anxiety and Depression Scale, and Symptom Distress Scale; bowel function was also assessed. Results A total of 56 patients were enrolled. API at baseline was 8.0±0.9, and decreased after 4 weeks by 48% (4.2±1.9; P<0.0001 vs baseline); 46 (82.1%) patients responded to treatment. Significant improvements were also reported in number/severity of breakthrough cancer pain episodes (P=0.001), Brief Pain Inventory Short Form (P=0.0002), Symptom Distress Scale (P<0.0001), Hospital Anxiety and Depression Scale depression (P=0.0006) and anxiety (P<0.0001) subscales, and bowel function (P=0.0003). At study end, 37 (66.0%) patients were satisfied/very satisfied with the new analgesic treatment. Combination therapy had a good safety profile. Conclusion OXN-PR and pregabalin were safe and highly effective in a real-world setting of severe neuropathic cancer pain, with a high rate of satisfaction, without interference on bowel function. PMID:27445495

  6. Assessment of the effectiveness and safety of Ethosuximide in the Treatment of non-Diabetic Peripheral Neuropathic Pain: EDONOT—protocol of a randomised, parallel, controlled, double-blinded and multicentre clinical trial

    Kerckhove, Nicolas; Mallet, Christophe; Pereira, Bruno; Chenaf, Chouki; Duale, Christian; Dubray, Claude; Eschalier, Alain

    2016-01-01

    Introduction Currently available analgesics are ineffective in 30–50% of patients suffering from neuropathic pain and often induce deleterious side effects. T-type calcium channel blockers (mibefradil, ethosuximide, NNC 55-0396) are of great interest for the development of new symptomatic treatments of neuropathic pain, due to their various effects on pain perception. Interestingly, ethosuximide, which has already been approved for treating epilepsy, is available on the European market for clinical use. Despite numerous preclinical data demonstrating an antinociceptive effect of ethosuximide in various animal models of neuropathic pain, no clinical studies have been published to date on the analgesic efficacy of ethosuximide in patients with neuropathic pain. Methods and analysis The Ethosuximide in the Treatment of non-Diabetic Peripheral Neuropathic Pain (EDONOT) trial is a randomised, parallel, controlled, double-blinded, multicentre clinical study. It is the first clinical trial to evaluate the efficacy and safety of ethosuximide in the treatment of non-diabetic peripheral neuropathic pain. Adult patients exhibiting peripheral neuropathic pain (Numeric Rating Scale (NRS) ≥4 and Douleur Neuropathique 4 (DN4)≥4) for at least 3 months and under stable analgesic treatment for at least 1 month will be included. Patients (n=220) will be randomly assigned to receive either ethosuximide or control treatment for 6 weeks following a 1 week run-in period. The primary end point is the intensity of neuropathic pain, assessed by NRS (0–10) before and after 6 weeks of treatment. The secondary end points are safety (adverse events are collected during the study: daily by the patient on the logbook and during planned phone calls by investigators), the intensity and features of neuropathic pain (assessed by Brief Pain Inventory (BPI) and Neuropathic Pain Symptom Inventory (NPSI) questionnaires) and health-related quality of life (assessed by Medical Outcome

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

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

    2012-01-01

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

  8. Effects of myopic spectacle correction and radial refractive gradient spectacles on peripheral refraction.

    Tabernero, Juan; Vazquez, Daniel; Seidemann, Anne; Uttenweiler, Dietmar; Schaeffel, Frank

    2009-08-01

    The recent observation that central refractive development might be controlled by the refractive errors in the periphery, also in primates, revived the interest in the peripheral optics of the eye. We optimized an eccentric photorefractor to measure the peripheral refractive error in the vertical pupil meridian over the horizontal visual field (from -45 degrees to 45 degrees ), with and without myopic spectacle correction. Furthermore, a newly designed radial refractive gradient lens (RRG lens) that induces increasing myopia in all radial directions from the center was tested. We found that for the geometry of our measurement setup conventional spectacles induced significant relative hyperopia in the periphery, although its magnitude varied greatly among different spectacle designs and subjects. In contrast, the newly designed RRG lens induced relative peripheral myopia. These results are of interest to analyze the effect that different optical corrections might have on the emmetropization process.

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

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

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

  10. A Study of Scientific Reasoning in a Peripheral Context: The Discovery of the Raman Effect

    Dasgupta, Deepanwita

    2015-01-01

    This paper is an attempt to reconstruct how C.V. Raman, a peripheral scientist in the early 20th century colonial India, managed to develop a research programme in physical optics from his remote colonial location. His attempts at self-training and self-education eventually led him to the discovery of the Raman Effect and to the Nobel Prize in…

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

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

    1999-05-01

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

  12. Analgesic and sedative effects of perioperative gabapentin in total knee arthroplasty A randomized, double-blind, placebo-controlled, dose-finding study

    Lunn, Troels Haxholdt; Husted, Henrik; Laursen, Mogens Berg

    2015-01-01

    Gabapentin has shown acute postoperative analgesic effects, but the optimal dose and procedure-specific benefits vs harm have not been clarified. In this randomized, double-blind, placebo-controlled dose-finding study, 300 opioid-naive patients scheduled for total knee arthroplasty were randomized......, and the secondary outcome was sedation 6 hours after surgery. Other outcomes were overall pain during well-defined mobilizations and at rest and sedation during the first 48 hours and from days 2-6, morphine use, anxiety, depression, sleep quality, and nausea, vomiting, dizziness, concentration difficulty, headache...... was as follows: 3.2 [0-10] vs 2.6 [0-9] vs 2.3 [0-9], the mean difference A vs C being 0.9 [0.2-1.7], P = 0.046. No between-group differences were observed in overall pain or morphine use the first 48 hours and from days 2-6. Sleep quality was better during the first 2 nights in group A and B vs C. Dizziness...

  13. Flurbiprofen Axetil Enhances Analgesic Effects of Sufentanil and Attenuates Postoperative Emergence Agitation and Systemic Proinflammation in Patients Undergoing Tangential Excision Surgery

    Wujun Geng

    2015-01-01

    Full Text Available Objective. Our present study tested whether flurbiprofen axetil could reduce perioperative sufentanil consumption and provide postoperative analgesia with decrease in emergency agitation and systemic proinflammatory cytokines release. Methods. Ninety patients undergoing tangential excision surgery were randomly assigned to three groups: (1 preoperative dose of 100 mg flurbiprofen axetil and a postoperative dose of 2 μg/kg sufentanil and 10 mL placebo by patient-controlled analgesia (PCA pump, (2 preoperative dose of 100 mg flurbiprofen axetil and a postoperative dose of 2 μg/kg sufentanil and 100 mg flurbiprofen axetil by PCA pump, and (3 10 mL placebo and a postoperative dose of 2 μg/kg sufentanil and 10 mL placebo by PCA pump. Results. Preoperative administration of flurbiprofen axetil decreased postoperative tramadol consumption and the visual analog scale at 4, 6, 12, and 24 h after surgery, which were further decreased by postoperative administration of flurbiprofen axetil. Furthermore, flurbiprofen axetil attenuated emergency agitation score and Ramsay score at 0, 5, and 10 min after extubation and reduced the TNF-α and interleukin- (IL- 6 levels at 24 and 48 h after the operation. Conclusion. Flurbiprofen axetil enhances analgesic effects of sufentanil and attenuates emergence agitation and systemic proinflammation in patients undergoing tangential excision surgery.

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

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

    1990-01-01

    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...

  15. A novel and cost-effective way to follow-up adequacy of pain relief, adverse effects, and compliance with analgesics in a palliative care clinic

    Radhika Kannan

    2013-01-01

    Full Text Available Introduction: A way to assess compliance with analgesics in an outpatient palliative care clinic is essential since often the patient is too ill or weak to come to hospital for weekly follow-ups. A pilot study was conducted using Short Messaging Service via mobile phone as a follow-up tool. Context: A predominantly outpatient palliative care clinic of a 300 bedded multidisciplinary hospital. Materials and Methods: Sixty patients attending the palliative care clinic were enrolled in the study. Analgesic drugs, co-analgesics, and adjuvants were prescribed on an outpatient basis. If possible, patients were admitted for 1 or 2 days. A simple scoring system was devised and taught to the patients and their attenders. A short message service had to be sent to the author′s mobile number. The period was fixed at 2 weeks by which the patients and attenders were familiar with the drugs and pain relief as well. Drowsiness was a worrisome complaint. The mobile number of the patient was called and attender instructed to skip one or two doses of morphine and reassurance given. If required, attender was asked to bring patient to the hospital or come to the hospital for a different prescription as the situation warranted. Results: Out of 60 patients, 22 were admitted initially for dose titration and all others were outpatients. Three patients were lost to follow-up and one patient died after 7 days. 93% of patients responded promptly. Random survey was done in 10 patients to confirm their SMS response and the results were analyzed. Conclusion: Mobile phones are available with all strata of people. It is easy to train patients to send an SMS.This technology can be used to follow- up palliative care patients and help them comply with their treatment regimen.

  16. 清脑镇痛液镇痛作用的实验研究%Empirical study on analgesic effect of Qingnao Zhentong Liquid

    武刚毅; 刘峙; 李小纪; 李德爱

    2011-01-01

    Objective: To observe Qingnao Zhentong Liquid (QZL) through the mouth for 5 straight days, after filling in mice stomach give the analgesic action generated. Methods: 120 SPF Kunming nice were randomly divided into the product high, medium and low dose group, positive and negative control group, each group 12 only, male and female half and half, the method of tenderness (n=60), acetic acid body torsion (n=60) according to improve rate of pain threshold, time of body torsion and body torsion times as the index. QZL was given according to 25 g liquid crude/kg or 12.5 g crude/kg weight through the mouth for 5 straight days to mice, the analgesic effect of Qingnao Zhentong Liquid was researched on mechanical stimuli and chemical stimulation the analgesic action which caused pain. Results: The product high dose group and positive control group could obviously improve the improve rate of pain threshold and compared with negative control group respectively, there were significant difference in them (P<0.01), the improve rate of pain threshold in the product of low, medium dose group which compared with negative control group respectively, there was no significant difference. There were no significant differences on the first time of body torsion of the product of high, medium and low dose group and positive control group which compared respectively with negative control group. The body torsion times in the product of high, medium dose group were diminished, which were compared with negative control group and there were significant differences in them (P<0.01). There were no significant differences on body torsion times of the product of low dose group compared with negative control group. Conclusion: QZL can observably increase the improve rat of pain threshold, and reduce the times of body torsion, so it has analgesic effect.%目的:观察清脑镇痛液连续5 d经口灌胃给予小鼠后,所产生的镇痛作用.方法:试验选用SPF级昆明种小鼠120只,随

  17. Peripheral and Central Effects of Melatonin on Blood Pressure Regulation

    Olga Pechanova

    2014-10-01

    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.

  18. COMPARATIVE EVALUATION OF POSTOPERATIVE ANALGESIC EFFECTS OF WOUND INFILTRATION WITH TRAMADOL, LEVOBUPIVACAINE AND COMBINATION OF THE TWO IN CHILDREN UNDERGOING INGUINAL HERNIA AND UNDESCENDED TESTIS SURGERY

    Aftab Ahmad

    2016-04-01

    Full Text Available BACKGROUND Wound infiltration with local anaesthetics may improve postoperative analgesia and has become increasingly common. It has the ability to reduce the need for opioids, additional complications, duration of hospital stay and its provision of effective postoperative analgesia. Tramadol infiltration of wound has been shown to have effects similar to those of local anaesthetics. AIMS AND OBJECTIVES To investigate the effects of wound infiltration with levobupivacaine and tramadol on postoperative analgesia in children undergoing elective unilateral inguinal hernia and undescended testis surgery. METHODS Ninety children (Age Group 1 to 7 years who were scheduled to undergo elective unilateral inguinal hernia and undescended testis surgery were included in the study. Patients were allocated to 3 groups of 30 each: Group A received wound infiltration with 2 mg/kg Tramadol in 0.2 mL/kg saline, Group B received wound infiltration with 0.2 mL/kg of 0.25% Levobupivacaine and Group C received wound infiltration with 2 mg/kg Tramadol plus 0.25% Levobupivacaine (total volume of solution as 0.2 mL/kg. Pain score was assessed using FACES pain scale at 1, 4, 8, 12 and 24 hours postoperatively. Patients with pain score of ≥4 were treated with paracetamol suppository (20 mg/kg body weight as rescue analgesia. Respiratory rate and pulse rate were also recorded at 1, 4, 8, 12 and 24 hours postoperatively. The frequency of side effects and rescue analgesic used were also recorded during the 24-hour postoperative period. RESULTS Average pain scores, respiratory rate and pulse rate were lowest in Group C compared to Group A and Group B at 1, 4, 8, 12 and 24 hours postoperatively (P value of 0.05. CONCLUSION Infiltration of the wound site with combined Levobupivacaine and Tramadol provides significantly better analgesia compared with Levobupivacaine or Tramadol alone.

  19. A benefit-risk assessment of caffeine as an analgesic adjuvant.

    Zhang, W Y

    2001-01-01

    Caffeine has been an additive in analgesics for many years. However, the analgesic adjuvant effects of caffeine have not been seriously investigated since a pooled analysis conducted in 1984 showed that caffeine reduces the amount of paracetamol (acetaminophen) necessary for the same effect by approximately 40%. In vitro and in vivo pharmacological research has provided some evidence that caffeine can have anti-nociceptive actions through blockade of adenosine receptors, inhibition of cyclo-oxygenase-2 enzyme synthesis, or by changes in emotion state. Nevertheless, these actions are only considered in some cases. It is suggested that the actual doses of analgesics and caffeine used can influence the analgesic adjuvant effects of caffeine, and doses that are either too low or too high lead to no analgesic enhancement. Clinical trials suggest that caffeine in doses of more than 65 mg may be useful for enhancement of analgesia. However, except for in headache pain, the benefits are equivocal. While adding caffeine to analgesics increases the number of patients who become free from headache [rate ratio = 1.36, 95% confidence interval (CI) 1.17 to 1.58], it also leads to more patients with nervousness and dizziness (relative risk = 1.60, 95% CI 1.26 to 2.03). It is suggested that long-term use or overuse of analgesic medications is associated with rebound headache. However, there is no robust evidence that headache after use or withdrawal of caffeine-containing analgesics is more frequent than after other analgesics. Case-control studies have shown that caffeine-containing analgesics are associated with analgesic nephropathy (odds ratio = 4.9, 95% CI 2.3 to 10.3). However, no specific contribution of caffeine to analgesic nephropathy can be identified from these studies. Whether caffeine produces nephrotoxicity on its own, or increases nephrotoxicity due to analgesics, is yet to be established.

  20. Effect of scorpion venom analgesic active peptide extracted from Buthus martensii Karsch on evoked potential in the thalamic posterior nucleus group in rats

    Qiuhong Lin; Xinxin Li

    2008-01-01

    BACKGROUND: Buthus martensii Karsch is a rare medicinal animal, and dried integral Buthus martensii Karsch is an important drug in traditional Chinese medicine. OBJECTIVE: To investigate the effects of scorpion venom analgesic active peptide (SAP) extracted from Buthus martensii Karsch on evoked unit discharge of the common peroneal nerve in the posterior nucleus group of the thalamus using a stereotaxic electrophysiological extracellular microelectrode recording. DESIGN, TIME AND SETTING: One-way designed study, performed in the Physiological Laboratory of Shenyang Medical College on September 15, 2006. MATERIALS: Fifty 3-4 months old Wistar rats (25 males and 25 females) were used. SAP was provided by Shenyang Pharmaceutical University. Morphine solution was made by the First Drug Manufactory, Northeastern Drug Manufacture Group (batch number: H20013351). Naloxone solution was made by Hunan Pharmaceutical Co., Ltd. (batch number: H43021669). Type ATAC-350 medical data processing equipment was made by the Photoelectricity Company, Japan.MAIN OUTCOME MEASURES: Evoked discharge in the posterior nucleus group of the thalamus and effects of SAP alone and SAP in combination with saline, morphine, or naloxone on discharges in the posterior nucleus group of the thalamus as measured by TQ-19 medical data processing equipment.RESULTS: SAP group: At 1-3 minutes after SAP injection, evoked discharges in the posterior nucleus group of the thalamus were inhibited, and the inhibitory time lasted for (45.0?.7) minutes. Saline group: Evoked discharges in the posterior nucleus group of the thalamus did not change after saline injection. Morphine group: At 1-3 minutes after morphine injection, evoked discharges in the posterior nucleus group of the thalamus were inhibited, and the inhibitory time lasted for (35.0?.8) minutes. Naloxone group: SAP had no effects on evoked potentials in the posterior nucleus group of the thalamus.

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

    Toroudi Hamidreza

    2009-01-01

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

  2. Phytochemical Screening and Evaluation of Analgesic Activity of Oroxylum indicum.

    Das, B K; Al-Amin, M M; Russel, S M; Kabir, S; Bhattacherjee, R; Hannan, J M A

    2014-01-01

    We aimed to study phytochemical screening and analgesic activity of ethanol extract of Oroxylum indicum. The dried powder of the barks of the plant was extracted with 95% ethanol and was subjected to various phytochemical tests to ascertain the principle constituents contained in the extract. The result revealed the presence of alkaloids, flavonoids, tannins, glycosides in the ethanol extract of Oroxylum indicum. The extract was screened for analgesic activity by using hot plate, acetic acid-induced writhing and formalin test. The ethanol extract of the plant at two different doses (250 and 500 mg/kg) showed significant (P<0.05) analgesic effect in all test methods (hot plate, acetic acid-induced writhing and formalin). The analgesic activity was compared with a standard drug (ketorolac at 10 mg/kg). Based on the present findings and previous literature review it can be concluded that flavonoids and tannins might be responsible for the analgesic activity. We suggest that ethanol extract of Oroxylum indicum might have potential chemical constituents that could be used in the future for the development of novel analgesic agent.

  3. Relative Biological Effectiveness and Peripheral Damage of Antiproton Annihilation

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

    2002-01-01

    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 (...

  4. Effect of intravenous dexmedetomidine on haemodynamic responses to laryngoscopy, tracheal intubation and anaesthetic and analgesic requirements: a randomized double-blind clinical efficacy study

    Madhusudan M

    2016-10-01

    Full Text Available Background: Dexmedetomidine is an alpha 2-adrenergic receptor agonist that provides sedation, anxiolysis, hypnosis, analgesia, and sympatholysis. The present study is aimed to assess the efficacy of dexmedetomidine in attenuating sympathoadrenal response to laryngoscopy and tracheal intubation and to analyse its effect on intraoperative anaesthetic and analgesic requirements. Methods: Sixty patients were randomized to receive either dexmedetomidine 1µg/kg (Group D or 10 mL of 0.9% saline (Group S over 10 minutes before induction of anaesthesia and after standard induction procedure the same study drug infusions were continued. Blood pressure, heart rate (HR and Ramsay sedation score (RSS were monitored at fixed time interval after study drug infusion and anaesthesia induction. Results: After study drug administration the changes in HR and blood pressure was statistically significant between the groups (p = <0.001 at all-time intervals during study period. There was 50% reduction in thiopentone requirements in Group D in comparison to Group S (p<0.001. The intraoperative additional dose of morphine requirement was less in Group D in comparison to Group S to maintain the steady haemodynamics (p<0.001. Statistically significant difference was noticed in Group D regarding RSS at 5 min and 10 min after study drug infusion (p=0.025 and p=0.001 respectively and again at 30 min after extubation (p= 0.002 when compared with Group S. Conclusions: Our observations suggest that dexmedetomidine was effective in attenuating the heart rate and blood pressure rise during laryngoscopy and intubation, and decrease the thiopentone and morphine requirements intraoperatively.

  5. Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain

    Jennifer R. Deuis

    2016-03-01

    Full Text Available Loss-of-function mutations of NaV1.7 lead to congenital insensitivity to pain, a rare condition resulting in individuals who are otherwise normal except for the inability to sense pain, making pharmacological inhibition of NaV1.7 a promising therapeutic strategy for the treatment of pain. We characterized a novel mouse model of NaV1.7-mediated pain based on intraplantar injection of the scorpion toxin OD1, which is suitable for rapid in vivo profiling of NaV1.7 inhibitors. Intraplantar injection of OD1 caused spontaneous pain behaviors, which were reversed by co-injection with NaV1.7 inhibitors and significantly reduced in NaV1.7−/− mice. To validate the use of the model for profiling NaV1.7 inhibitors, we determined the NaV selectivity and tested the efficacy of the reported NaV1.7 inhibitors GpTx-1, PF-04856264 and CNV1014802 (raxatrigine. GpTx-1 selectively inhibited NaV1.7 and was effective when co-administered with OD1, but lacked efficacy when delivered systemically. PF-04856264 state-dependently and selectively inhibited NaV1.7 and significantly reduced OD1-induced spontaneous pain when delivered locally and systemically. CNV1014802 state-dependently, but non-selectively, inhibited NaV channels and was only effective in the OD1 model when delivered systemically. Our novel model of NaV1.7-mediated pain based on intraplantar injection of OD1 is thus suitable for the rapid in vivo characterization of the analgesic efficacy of NaV1.7 inhibitors.

  6. Effects of selenium on electrophysiological changes associated with diabetic peripheral neuropathy

    Murat Ayaz; Hülagu Kaptan

    2011-01-01

    Our previous study has demonstrated that sodium selenite prevents oxidative stress, suggesting that selenium can improve diabetic peripheral neuropathy. Results from this study demonstrated that diabetes mellitus resulted in significant increased time to peak, as well as rheobase and chronaxie values, In addition, maximum depolarization, area under compound action potential, kinetics, and conduction velocities of fast and stow nerve fiber groups were decreased. Sodium selenite exhibited positive effects on alterations of diabetes mellitus-induced conduction velocity distribution. This neuroprotective effect was primarily observed in the area under compound action potential and compound action potential kinetic waveforms, as well as rheobase and chronaxie. Results from this study showed that selenium supplementation blocked the diabetes mellitus-induced shift of actively contributing nerve fibers, and restored levels towards age-matched control group values. Chronic selenate supplementation for experimental diabetic peripheral neuropathy exhibited protective effects in measured electrophysiological parameters.

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

    Khomiak O.V.

    2012-01-01

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

  8. Composition of The Essential Oil From Danggui-zhiqiao Herb-Pair and Its Analgesic Activity and Effect on Hemorheology in Rats With Blood Stasis Syndrome

    Wang, Yuanqing; Yan, Jianye; Li, Shunxiang; Wang, Wei; Cai, Xiong; Huang, Dan; Gong, Limin; Li, Xin

    2016-01-01

    Background: Angelica sinensis and Aurantii fructu used in a pair, named Danggui-Zhiqiao herb-pair (DZHP), which was rich in essential oil and has been adopted to promote blood circulation, dispel blood stasis, and relieve pain in traditional Chinese medicine (TCM) Objective: To analyze the composition and pharmacological effects of essential oil from DZHP Materials and Methods: The composition of the essential oil from DZHP was analyzed by gas chromatography/mass spectrometry (GC/MS). Its analgesic activity was evaluated by acetic acid-induced writhing test and hot plate test. The hemorheology test was carried out to evaluate the effect on hemorheology in rats with blood stasis syndrome Results: Twenty-eight components were identified and the main components were α-pinene (3.07%), β-pinene (2.0%), β-myrcene (3.71%), D-limonene (49.28%), γ-terpinen (9.53%), α-terpinolene (1.80%), α-terpineol (2.02%), β-bisabolene (1.13%), butylidenephthalide (1.43%), and Z-ligustilide (16.08%). The pharmacology test showed that the essential oil significantly inhibited the number of writhes induced by acetic acid with inhibition rate of 44.64% and significantly increased hot-plate latency compared with control group from 30 to 90 min after oral administration of drugs in mice. It could significantly decrease plasma viscosity, whole blood relative index at high and low shear rate, whole blood reduced viscosity at high and low shear rate, and erythrocyte rigidity index in hemorheology test Conclusion: The composition of the essential oil of DZHP was determined successfully and it had analgesic and promoting blood circulation activities. SUMMARY Angelica sinensis and Aurantii fructu used in a pair, named Danggui-Zhiqiao herb-pair (DZHP), which was rich in Essential oil and has been adopted to promote blood circulation, dispel blood stasis and relieve pain in traditional Chinese medicine (TCM).Twenty-eight components were identified and the main components were α-pinene (3

  9. Clinical and pathological aspects of analgesic nephropathy

    Nanra, R. S.

    1980-01-01

    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.

  10. Clinical Observation on Therapeutic Effect of Acupuncture and Moxibustion Treatment for Melanoderm's Peripheral Facial Paralysis at Remission Stage

    MA Deng-shang; YANG Ling

    2007-01-01

    The traditional acupuncture and moxibustion therapies were adopted to treat 32cases of melanoderm's peripheral facial paralysis at remission stage, the effective rate was 93.8%, indicating that acupuncture and moxibustion therapies are effective for different races.

  11. Effect of glial cell line-derived neurotrophic factor on peripheral nerve regeneration in adult rat

    CHEN Zhe-yu; LI Jian-hong; ZHENG Xing-dong; LU Chang-lin; HE Cheng

    2001-01-01

    Objective: To study the effect of glial cell line-derived neurotrophic (GDNF) on adult peripheral nerve regeneration. Methods: Transectioned sciatic nerve in adult rats was sutured into silicone channel. GDNF or SAL solution was injected into the silicone channels during operation. Four weeks later, the effect of GDNF on axonal regeneration was evaluated by degenerative neurofiber staining and HRP retrograde tracing. Results: Compared with SAL group, the percentage of degenerative neurofiber areas decreased from 17.3% to 1.9% ( P<0.01 ) and the ratio of labeled spinal somas number was significantly increased from 43.5% to 68.3% ( P<0.01 ) in GDNF group. Conclusion: The results suggest that exogenous GDNF can obviously enhance adult peripheral nerve regeneration.

  12. Analgesic Effects and Safety of Desmopressin, Tramadol and Indomethacin in Patients with Acute Renal Colic; A Randomized Clinical Trial

    Mehdi Shirazi

    2015-04-01

    Full Text Available Objective: To compare the efficacy of desmopressin (DDAVP, tramadol and indomethacin on pain intensity of patients with acute renal colic caused by urolithiasis. Methods: This prospective, randomized clinical trial was conducted between July 2005 and July 2006 including 120 patients (70 men and 50 women, mean age 38.2±5.8 years referring to emergency room of Shahid Faghihi hospital with renal colic caused by urolithiasis without any previous treatment. The patients were randomly assigned to three groups: group A received tramadol 50mg intramuscularly (n=40, group B received desmopressin 40 µg intranasally (n=40 and group C received indomethacin 100mg rectally (n=40. The pain was assessed both on admission and 30 minutes after the intervention. The pain intensity and the side effects were compared between two study groups. Results: There was no significant difference between two study groups regarding the baseline characteristics. The intensity of pain of presentation was almost similar in all groups. In group A, 30 patients (75%, in group B, 15 patients (37.5% and in group C, 19 patients (47.5% had complete pain relief. The pain intensity decreased significantly after the intervention within all three groups ( p<0.001. Conclusion: According to the results of the current study, rectal indomethacin, intramuscular tramadol and intranasal desmopressin are effective and safe routs of controlling pain in acute renal colic secondary to urolithiasis. Tramadol was the most effective agent in controlling the pain. Clinical Trial Registry: The current study is registered with Iranian Registry for Clinical Trials (www.irct.ir; IRCT2015030919470N18

  13. Health-related quality of life and its predictive role for analgesic effect in patients with painful polyneuropathy

    Otto, Marit; Bach, Flemming W; Jensen, Troels S;

    2007-01-01

    with a diagnosis of painful polyneuropathy were included in the analysis. Data were obtained from three randomised, placebo-controlled cross-over studies testing the effect of different drugs on polyneuropathic pain (St. John's wort, venlafaxine/imipramine and valproic acid). Patients completed a HRQL...... questionnaire (SF-36) after a drug-free baseline period and at the end of each treatment period. At baseline, all eight SF-36 scores were lower than in the normal population. No significant differences were found between SF-36 scales during placebo and treatment with valproic acid and St. John's wort. Those two...

  14. Analgesic and Sensory Effects of the Pecs Local Anesthetic Block in Patients with Persistent Pain after Breast Cancer Surgery

    Wijayasinghe, Nelun; Andersen, Kenneth Geving; Kehlet, Henrik

    2016-01-01

    BACKGROUND: Persistent pain after breast cancer surgery (PPBCS) develops in 15% to 25% of patients, sometimes years after surgery. Approximately 50% of PPBCS patients have neuropathic pain in the breast, which may be due to dysfunction of the pectoral nerves. The Pecs local anesthetic block...... proposes to block these nerves and has provided pain relief for patients undergoing breast cancer surgery, but has yet to be evaluated in patients with PPBCS. METHODS: The aim of this pilot study was to examine the effects of the Pecs block on summed pain intensity (SPI) and sensory function (through...

  15. Analgesic effect of salmon calcitonin in osteoporotic vertebral fractures: a double-blind placebo-controlled clinical study.

    Lyritis, G P; Tsakalakos, N; Magiasis, B; Karachalios, T; Yiatzides, A; Tsekoura, M

    1991-12-01

    Back pain due to vertebral collapse is the main symptom of postmenopausal osteoporosis. The clinical picture in these crush fractures varies, depending on the type and the location of fracture, but in general, a new vertebral crush fracture gives rise to severe pain that immobilizes the patient and necessitates bedrest. In this double-blind controlled clinical trial, 56 patients who had recently (within the last 3 days) suffered an osteoporotic vertebral fracture were hospitalized for a period of 14 days. Salmon calcitonin (100 IU) or placebo injections were given daily. Pain was rated daily on a 10-point scale by the same observers. Blood and urinary parameters were also evaluated. The results showed a significant (P less than 0.001) difference in pain intensity between the calcitonin group and the placebo group. This beneficial effect was generally apparent from the second day of treatment onward, and over the following 2 weeks, the patients were able to sit and stand, and gradually started to walk again. A significant decrease in urinary hydroxyproline and urinary calcium was also noted in the calcitonin group. It is concluded that calcitonin exerts a beneficial effect on back pain following a vertebral crush fracture.

  16. The Analgesic and Anxiolytic Effect of Souvenaid, a Novel Nutraceutical, Is Mediated by Alox15 Activity in the Prefrontal Cortex.

    Shalini, Suku-Maran; Herr, Deron R; Ong, Wei-Yi

    2016-10-01

    Pain and anxiety have a complex relationship and pain is known to share neurobiological pathways and neurotransmitters with anxiety. Top-down modulatory pathways of pain have been shown to originate from cortical and subcortical regions, including the dorsolateral prefrontal cortex. In this study, a novel docosahexaenoic acid (DHA)-containing nutraceutical, Souvenaid, was administered to mice with infraorbital nerve ligation-induced neuropathic pain and behavioral responses recorded. Infraorbital nerve ligation resulted in increased face wash strokes of the face upon von Frey hair stimulation, indicating increased nociception. Part of this response involves general pain sensitization that is dependent on the CNS, since increased nociception was also found in the paws during the hot plate test. Mice receiving oral gavage of Souvenaid, a nutraceutical containing DHA; choline; and other cell membrane components, showed significantly reduced pain sensitization. The mechanism of Souvenaid's activity involves supraspinal antinociception, originating in the prefrontal cortex, since inhibition of the DHA-metabolizing enzyme 15-lipoxygenase (Alox15) in the prefrontal cortex attenuated the antinociceptive effect of Souvenaid. Alox15 inhibition also modulated anxiety behavior associated with pain after infraorbital nerve ligation. The effects of Souvenaid components and Alox15 on reducing central sensitization of pain may be due to strengthening of a known supraspinal antinociceptive pathway from the prefrontal cortex to the periaqueductal gray. Together, results indicate the importance of the prefrontal cortex and DHA/Alox15 in central antinociceptive pathways and suggest that Souvenaid may be a novel therapeutic for neuropathic pain.

  17. Analgesic effect of repetitive transcranial magnetic stimulation (rTMS) in patients with chronic low back pain.

    Ambriz-Tututi, Mónica; Alvarado-Reynoso, Beatriz; Drucker-Colín, René

    2016-08-22

    The objective of the present study was to assess the benefits of 1-week repetitive transcranial magnetic stimulation (rTMS) in patients with chronic low back pain (LBP). The visual analogue scale (VAS), Short Form McGill pain questionnaire (SF-MPQ), and Short Form 36 Health Survey were used to evaluate the effect of this treatment. Eighty-two patients diagnosed with LBP were divided randomly into three groups: rTMS-treated group, sham group, and physical therapy-treated group. We observed a significant reduction in VAS and SF-MPQ scores in the rTMS-treated group, but not in the sham group. Moreover, patients who received rTMS had a lower mean pain score than patients treated with physical therapy. Our study suggests that rTMS produces safe, significant, and long-term relief in patients with LBP without evident side effects. This study shows for the first time that long-term repeated sessions of rTMS decrease pain perception of LBP. Bioelectromagnetics. © 2016 Wiley Periodicals, Inc.

  18. EFEITO ANALGÉSICO DO BUTORFANOL NA DOR SOMÁTICA EM GATOS ANESTESIADOS COM PROPOFOL ANALGESIC EFFECT OF BUTORPHANOL ON SOMATIC PAIN IN CATS ANESTHETIZED WITH PROPOFOL

    Isabela Ciniello Araujo

    2001-02-01

    Full Text Available O propofol é um agente anestésico intravenoso usado para indução e manutenção da anestesia, mas produz analgesia limitada, havendo a necessidade do uso concomitante de analgésicos. Avaliou-se o efeito analgésico do butorfanol na dor somática em gatos anestesiados com doses fracionadas de propofol. Foram utilizados 16 animais, distribuídos aleatoriamente em dois grupos. Os animais do grupo controle foram pré-tratados com 0,2mg/kg de acepromazina por via IM e, após 15 minutos, receberam 6mg/kg de propofol por via IV. Os animais do grupo tratamento foram pré-medicados com uma combinação de acepromazina (0,2mg/kg e butorfanol (0,8mg/kg, administrados na mesma seringa por via IM, e, após 15 minutos, receberam 6mg/kg de propofol por via IV. Em ambos os grupos, a manutenção da anestesia foi feita com administrações de propofol, na dose de 3mg/kg, por via IV, sempre que necessário, durante 60 minutos. A necessidade de readministração de propofol foi verificada pela resposta apresentada ao pinçamento cutâneo, através de uma pinça de Kocher. Avaliaram-se também as freqüências cardíaca e respiratória, pressão arterial média, saturação de oxiemoglobina e temperatura retal. A administração de butorfanol causou apenas redução nas freqüências cardíaca e respiratória e na saturação de oxiemoglobina, em comparação com o grupo controle,sem exercer influência significativa sobre o período hábil, a dose total administrada e o período de recuperação do propofol. Concluiu-se que a adição de butorfanol não produziu analgesia somática em gatos anestesiados com doses fracionadas de propofol.Propofol is an intravenous anesthetic agent used for induction and maintenance of anesthesia but produces limited analgesia, and concomitant use of analgesics is necessary. The analgesic effect of butorphanol in somatic pain in cats anesthetized with intermittent doses of propofol was evaluated. Sixteen animals were randomly

  19. Central and peripheral benzodiazepine receptors in rat brain and platelets: effects of treatment with diazepam and clobazam.

    Larkin, J G; Thompson, G G; Scobie, G; Brodie, M J

    1992-09-01

    Tolerance to the effects of benzodiazepines (BZ) may be mediated by changes in benzodiazepine receptors (BZRs). Peripheral BZRs (in brain and platelets) and central BZRs (in brain) were measured in rats following intraperitoneal administration of diazepam and clobazam each for 4 and 12 days. BZRs were measured by binding assays using [3H] PK 11195 (peripheral) and [3H] flunitrazepam (central) as radioligands. Diazepam, but not clobazam, increased peripheral BZR numbers in platelets (both P < 0.005), but not in brain, after 4 and 12 days' treatment compared with appropriate controls. Neither drug altered central BZR affinities or numbers in rat brain. BZ effects on peripheral BZRs in platelets cannot be extrapolated to predict changes in brain receptors, either peripheral or central.

  20. Effects of Peripheral Neurotensin on Appetite Regulation and Its Role in Gastric Bypass Surgery.

    Ratner, Cecilia; Skov, Louise J; Raida, Zindy; Bächler, Thomas; Bellmann-Sickert, Kathrin; Le Foll, Christelle; Sivertsen, Bjørn; Dalbøge, Louise S; Hartmann, Bolette; Beck-Sickinger, Annette G; Madsen, Andreas N; Jelsing, Jacob; Holst, Jens J; Lutz, Thomas A; Andrews, Zane B; Holst, Birgitte

    2016-09-01

    Neurotensin (NT) is a peptide expressed in the brain and in the gastrointestinal tract. Brain NT inhibits food intake, but the effects of peripheral NT are less investigated. In this study, peripheral NT decreased food intake in both mice and rats, which was abolished by a NT antagonist. Using c-Fos immunohistochemistry, we found that peripheral NT activated brainstem and hypothalamic regions. The anorexigenic effect of NT was preserved in vagotomized mice but lasted shorter than in sham-operated mice. This in combination with a strong increase in c-Fos activation in area postrema after ip administration indicates that NT acts both through the blood circulation and the vagus. To improve the pharmacokinetics of NT, we developed a pegylated NT peptide, which presumably prolonged the half-life, and thus, the effect on feeding was extended compared with native NT. On a molecular level, the pegylated NT peptide increased proopiomelanocortin mRNA in the arcuate nucleus. We also investigated the importance of NT for the decreased food intake after gastric bypass surgery in a rat model of Roux-en-Y gastric bypass (RYGB). NT was increased in plasma and in the gastrointestinal tract in RYGB rats, and pharmacological antagonism of NT increased food intake transiently in RYGB rats. Taken together, our data suggest that NT is a metabolically active hormone, which contributes to the regulation of food intake.

  1. Propylthiouracil and peripheral neuropathy

    Valentina Van Boekel

    1992-06-01

    Full Text Available Peripheral neuropathy is a rare manifestation in hyperthyroidism. We describe the neurological manifestations of a 38 year old female with Graves' disease who developed peripheral neuropathy in the course of her treatment with propylthiouracil. After the drug was tapered off, the neurological signs disappeared. Therefore, we call attention for a possible toxic effect on peripheral nervous system caused by this drug.

  2. Low-intensity Laser (660 NM) has Analgesic Effects on Sternotomy of Patients Who Underwent Coronary Artery Bypass Grafts

    Fernandes, Gilderlene Alves; Araújo Júnior, Raimundo de Barros; Lima, Andréa Conceição Gomes; Gonzaga, Isabel Clarisse Albuquerque; de Oliveira, Rauirys Alencar; Nicolau, Renata Amadei

    2017-01-01

    Background: The aim of this study was to evaluate the efficacy of low-level laser therapy for reducing the acute pain of sternotomy in patients who underwent a coronary artery bypass graft (CABG). Methods: This study was conducted with ninety volunteers who electively submitted to CABG. The volunteers were randomly allocated into three groups of equal size (n = 30): control, placebo, and laser (λ of 660 nm and spatial average energy fluency of 1.06 J/cm2). Pain when coughing was assessed by a visual analog scale (VAS) and McGill Pain Questionnaire, according to sensory, affective, evaluative, and miscellaneous domains. The patients were followed for 1 month after the surgery. Results: The laser group had a greater decrease in pain with analogous results, as indicated by both the VAS and the McGill questionnaire (P ≤ 0.05) on sensory and affective scores, on days 6 and 8 postsurgery compared to the placebo and control groups. Conclusion: Laser seems to be effective promoting pain reduction after coronary-arterial bypass grafting. PMID:28074796

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

    Stathopoulos Efstathios N

    2010-09-01

    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 β-catenin expression.

  4. The CB1 receptor mediates the peripheral effects of ghrelin on AMPK activity but not on growth hormone release.

    Kola, Blerina; Wittman, Gábor; Bodnár, Ibolya; Amin, Faisal; Lim, Chung Thong; Oláh, Márk; Christ-Crain, Mirjam; Lolli, Francesca; van Thuijl, Hinke; Leontiou, Chrysanthia A; Füzesi, Tamás; Dalino, Paolo; Isidori, Andrea M; Harvey-White, Judith; Kunos, George; Nagy, György M; Grossman, Ashley B; Fekete, Csaba; Korbonits, Márta

    2013-12-01

    This study aimed to investigate whether the growth hormone release and metabolic effects of ghrelin on AMPK activity of peripheral tissues are mediated by cannabinoid receptor type 1 (CB1) and the central nervous system. CB1-knockout (KO) and/or wild-type mice were injected peripherally or intracerebroventricularly with ghrelin and CB1 antagonist rimonabant to study tissue AMPK activity and gene expression (transcription factors SREBP1c, transmembrane protein FAS, enzyme PEPCK, and protein HSL). Growth hormone levels were studied both in vivo and in vitro. Peripherally administered ghrelin in liver, heart, and adipose tissue AMPK activity cannot be observed in CB1-KO or CB1 antagonist-treated mice. Intracerebroventricular ghrelin treatment can influence peripheral AMPK activity. This effect is abolished in CB1-KO mice and by intracerebroventricular rimonabant treatment, suggesting that central CB1 receptors also participate in the signaling pathway that mediates the effects of ghrelin on peripheral tissues. Interestingly, in vivo or in vitro growth hormone release is intact in response to ghrelin in CB1-KO animals. Our data suggest that the metabolic effects of ghrelin on AMPK in peripheral tissues are abolished by the lack of functional CB1 receptor via direct peripheral effect and partially through the central nervous system, thus supporting the existence of a possible ghrelin-cannabinoid-CB1-AMPK pathway.

  5. Peripheral and central effects of intracerebroventricular microinjection of Hottentotta gentili (Pallary, 1924) (Scorpiones, Buthidae) venom.

    El Hidan, Moulay Abdelmonaim; Touloun, Oulaid; El Hiba, Omar; Laadraoui, Jawad; Ferehan, Hind; Boumezzough, Ali

    2016-03-01

    Central effects of scorpion venom toxins have been neglected, due both to the common belief that scorpion venoms act by targeting peripheral organs and also to the misunderstanding that these peptides do not cross the brain-blood barrier (BBB). Determining whether scorpion neurotoxicity is restricted to peripheral actions or whether a central mechanism may be partly responsible for systemic manifestations could be crucial in clinical therapy trends. The present study therefore aims to assess histopathological damages in some organs (heart, kidney, liver, and lungs) and the related biochemical impairments, together with a neurobehavioral investigation following an intracerebroventricular (i.c.v) micro-injection of Hottentotta gentili (Scorpiones, Buthidae) venom (0.47 μg/kg). I.c.v. injection of venom produced focal fragmentation of myocardial fibers, while lungs showed rupture of the alveolar structure. Concurrently, there was a significant rise in the serum enzymes levels of ASAT, ALAT, CPK and LDH. Meanwhile, we observed behavioral alterations such as a hypoactivity, and in addition the venom seems to have a marked anxiogenic-like effect. The present investigation has brought new experimental evidence of a peripheral impact of central administration of H. gentili venom, such impact was manifested by physiological and behavioral disturbances, the last of these appearing to reflect profound neuro-modulatory action of H. gentili venom.

  6. Clinical Research on Nourishing Yin and Unblocking Meridians Recipe Combined with Opioid Analgesics in Cancer Pain Management

    ZHANG Ting; MA Sheng-lin; XIE Guang-ru; DENG Qing-hua; TANG Zhong-zhu; PAN Xiao-chan; ZHANG Min; XU Su

    2006-01-01

    Objective: To investigate the analgesic effects of Nourishing yin and Unblocking meridians Receipe (NUR) combined with opioid analgesics in managing cancer pain. Methods: All the patients enrolled were differentiated as of yin deficiency and meridian blocked syndrome type of TCM. Forty-one of them in the treated group were treated with NUR combined with opioid analgesics, while 43 of them in the control group were given opioid analgesics alone with successive 14 days as one treatment course for both groups. Results:The indexes of the treated group were superior to those in the control group as to the degree of pain-relieving, the therapeutic effect of analgesia, the occurrence frequency of cancer pain every day and its duration each time, the analgesic initial time, and the quality of life. Conclusion: NUR combined with opioid analgesics in cancer pain management was more effective than opioid analgesics alone.

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

    Deepraj Paul

    2013-06-01

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

  8. Combination analgesic involvement in the pathogenesis of analgesic nephropathy: the European perspective.

    Elseviers, M M; De Broe, M E

    1996-07-01

    Analgesic nephropathy (AN) is a chronic renal disease characterized by renal papillary necrosis and interstitial nephritis caused by excessive consumption of analgesic mixtures. In a recent study, diagnostic criteria for AN, based on a computed tomography scan investigation without contrast, were presented. The observation of a decreased renal mass of both kidneys combined with either bumpy contours or papillary calcifications was found to have a high diagnostic performance. Although several case control studies and two prospective studies demonstrated the association between analgesic abuse and nephropathy, the nephrotoxicity of the different analgesic products had not been clearly established. Analgesic abuse can be defined as a daily consumption of analgesic mixtures over a several-year period. Abuse of single analgesics is rare; it has been clearly demonstrated that abusers prefer analgesic mixtures. In Belgium, the prevalence of AN was positively related to the sales of analgesic mixtures containing two analgesic components plus caffeine and/or codeine. This relationship could not be observed for analgesics containing only one analgesic component plus caffeine and/or codeine. Moreover, during a European multicenter study, nephrotoxicity of different combinations of analgesic mixtures (all containing caffeine and/or codeine) could be documented in the absence of any previous phenacetin consumption. Epidemiologic observations in Sweden, France, and Belgium regarding incidence of AN, sales figures of analgesics, and legislative measurements concerning analgesic consumption supported the previous observations.

  9. A comparison of the newer COX-2 drugs and older nonnarcotic oral analgesics.

    Sunshine, A

    2000-09-01

    The newer COX-2 drugs are safer analgesics than the older NSAIDs. At the usual dose used in osteoarthritis, they have less analgesic effect than the older NSAIDs. The non-narcotic analgesics such as acetaminophen, salicylate, NSAIDs, and the newer COX-2 drugs seem to have distinctly different mechanisms of action. In limited clinical trials, some of these drugs in combination give additive analgesia. Consideration should be given to using these drugs in combination, after suitable clinical trials, to enhance the efficacy of this category of analgesics.

  10. Structural comparisons of meptazinol with opioid analgesics

    Wei LI; Jing-lai HAO; Yun TANG; Yan CHEN; Zhui-bai QIU

    2005-01-01

    Aim: To investigate the mechanism of action of a potent analgesic, (±)-meptazinol.Methods: The structures of meptazinol enantiomers were compared with opioid pharmacophore and tramadol. Results: Neither enantiomer of meptazinol fitted any patterns among the opioid pharmacophore and tramadol, although they did share some structural and pharmacological similarities. However, the structure superpositions implied that both enantiomers of meptazinol might share some similar analgesic mechanisms with typical opiate analgesics. Conclusion:Meptazinol should have a different mechanism of action to known analgesics,which would be helpful in further investigations of meptazinol in the search for non-addictive analgesics.

  11. Pharmacologic interventions for painful diabetic neuropathy: an umbrella systematic review and comparative effectiveness network meta-analysis (Protocol)

    Griebeler Marcio L; Tsapas Apostolos; Brito Juan P; Wang Zhen; Phung Olivia J; Montori Victor M; Murad M

    2012-01-01

    Abstract Background Neuropathic pain can reduce the quality of life and independence of 30% to 50% of patients with diabetes. The comparative effectiveness of analgesics for patients with diabetic neuropathy remains unclear. The aim of the current work, therefore, was to summarize the evidence about the analgesic effectiveness of the most common oral and topical agents used for the treatment of peripheral diabetic neuropathy. Methods We will use an umbrella approach (systematic review of syst...

  12. Analgesic profile of hydroalcoholic extract obtained from Marrubium vulgare.

    de Souza, M M; de Jesus, R A; Cechinel-Filho, V; Schlemper, V

    1998-04-01

    Marrubium vulgare L. is a medicinal plant used in folk medicine to cure a variety of diseases. Recently we have demonstrated that a hydroalcoholic extract of this plant showed significant, nonspecific antispasmodic effects on isolated smooth muscle. In this report, we have investigated the possible analgesic effects of the same hydroalcoholic extract in different models of pain in mice. The results suggest that this extract exhibits significant analgesic activity, antagonizing chemically-induced acute pain. Such effects may be related to the presence of steroids and terpenes, which were detected by TLC analysis.

  13. Analgesic effect of flurbiprofen axetil for chest trauma%氟比洛芬酯用于胸部创伤镇痛的临床观察

    刘武新

    2012-01-01

    Objective To investigate the analgesic affects and safety of intravenous infusion of flurbiprofen axetil in chest trauma patients. Methods 60 chest trauma patients with multiple rib fractures (three or more ) were randomly divided into groups A and B. The flurbiprofen axetil injection ( kaifen ) 50 mg were given by intravenous infusion in group A. The tramadol injection 100 mg were given by intramuscular injection in group B. VAS scales and the side effects were observed in the two groups during drug onset and duration, before treatment, and 2, 6, 24 hours after treatment. Result The difference in drug onset time and duration between the two groups was statistically significant ( P 0. 05 ). 3. 33% of group A experienced adverse reactions compared with 16. 67% from group B. Conclusion The use of glurbiprofen axetil for chest trauma patients is effective and adverse reactions are less.%目的 观察静脉滴注氟比洛芬酯对胸部创伤患者的镇痛效果及安全性.方法 60例以多发肋骨骨折(3根以上)为主的胸部创伤患者随机分为A、B两组,A组给予氟比洛芬酯注射液(凯纷)50 mg加入生理盐水50 ml静脉滴注,B组给予曲马多注射液100 mg肌肉注射.比较起效时间、维持时间及用药前、用药后2、6、24 h疼痛视觉模拟评分(VAS)值,以及副反应观察.结果 A组药物起效时间及持续时间与B组比较差异有统计学意义(P0.05);两组用药后不良反应:A组不良反应率为3.33%,B组不良反应发生率为16.67%.结论 氟比洛芬酯用于胸部创伤镇痛效果确切,且副作用少.

  14. Screening of cetirizine for analgesic activity in mice

    Priya M

    2013-04-01

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

  15. Analgesic efficacy with rapidly absorbed ibuprofen sodium dihydrate in postsurgical dental pain

    Nørholt, Sven Erik; Hallmer, F; Hartlev, Jens;

    2011-01-01

    To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid).......To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid)....

  16. Expermiental Research on Anti-Inflammatory and Analgesic Effects of Geniposide Cream and Microemulsion%京尼平苷透皮制剂抗炎镇痛作用的研究

    施华平; 张杰; 游伟良; 曹维; 孙敏捷

    2012-01-01

    目的:考察京尼平苷乳膏和京尼平苷微乳的抗炎镇痛作用.方法:乳化法制备京尼平苷乳膏和京尼平苷微乳;热板测痛法和醋酸诱导的扭体法考察制剂的镇痛效果;采用二甲苯致炎和角叉菜胶致脚趾肿胀法考察制剂的抗炎效果,并与市售的抗炎和镇痛的制剂进行了比较.结果:京尼平苷乳膏和京尼平苷微乳具有抗炎镇痛的作用,乳膏剂型的效果更为显著,和市售产品的效果接近或者是更强.结论:将京尼平苷制成透皮制剂具有抗炎和镇痛的作用,其中乳膏的效果更好,为临床应用提供了实验依据.%Objective:To study the analgesic and anti-inflammatory effects of geniposide cream and microemulsion.Methods:The o/w type cream and microemulsion of geniposide were prepared and applied to tests of plate heating, writhing response induced by acetic acid, ear swollen of mice induced by xylene and foot swollen in mice induced by carrageenan, in comparison with the pharmaceutical market products.Result:Compared with the pharmaceutical market products, geniposide cream and microemulsion all showed analgesic effects and anti-inflammatory effects, but the geniposide cream was more effective and had no skin irritation.Conclusion:Geniposide cream and microemulsion have certain analgesic and anti-inflammatory effects, while the cream is better.

  17. Effects of estrogen on CD4+CD25+ regulatory T cell in peripheral blood during pregnancy

    Yuan-Huan Xiong; Zhen Yuan; Li He

    2013-01-01

    Objective:To investigate the effects of estrogen (E2) level on regulatory T cells (Treg) in peripheral blood during pregnancy. Methods:A total of 30 healthy non-pregnant women were selected as control group, 90 pregnant women of early, middle and late pregnancy and 30 postpartum women at 1 month after parturition were selected as experimental groups including early pregnancy group, middle pregnancy group and late pregnancy group;the proportions of CD4+CD25+Treg and CD4+CD25+CD127-Treg among CD4+T cells were detected by flow cytometry;the serum estrogen content in peripheral blood was detected by electrochemical immune luminescence method. Results: E2 level was coincident with the change of Tregs number during pregnancy. The estrogen content in peripheral blood increased gradually from early pregnancy to late pregnancy, then decreased significantly after parturition, and the level at 1 month after parturition down to the level in non-pregnancy group (P>0.05);the level of E2 in pregnancy groups were significantly higher than those in non-pregnancy group (P0.05);the proportions in middle and late pregnancy groups were significantly higher than those in early pregnancy group (P0.05). There was correlation between Tregs number with estrogen level during pregnancy. The proportion of CD4+CD25+ Treg and CD4+CD25+CD127- Treg were positively correlated with estrogen level. Conclusions:High proportion of CD4+CD25+Treg and CD4+CD25+CD127-Treg is closely related to the high level of E2 during pregnancy. It suggested that high level of estrogen may induce an increase of CD4+CD25+Treg in peripheral blood, and then influence the immune function of pregnant women. The results of this experiment might play an important role of estrogen in immune-modulation during pregnancy.

  18. Effect of propranolol on the splanchnic and peripheral renin angiotensin system in cirrhotic patients

    Walkiria Wingester Vilas-Boas; Ant(o)nio Ribeiro-Oliveira Jr; Renata da Cunha Ribeiro; Renata Lúcia Pereira Vieira; Jerusa Almeida; Ana Paula Nadu; Ana Cristina Sim(o)es e Silva; Robson Augusto Souza Santos

    2008-01-01

    AIM: To evaluate the effect of β-blockade on angiotensins in the splanchnic and peripheral circulation of cirrhotic patients and also to compare hemodynamic parameters during liver transplantation according to propranolol pre-treatment or not. METHODS: Patients were allocated into two groups: outpatients with advanced liver disease(LD) and during liver transplantation(LT). Both groups were subdivided according to treatment with propranolol or not. Plasma was collected through peripheral venipuncture to determine plasma renin activity(PRA), Angiotensin(Ang) Ⅰ, Ang Ⅱ, and Ang-(1-7) levels by radioimmunoassay in LD group. During liver transplantation, hemodynamic parameters were determined and blood samples were obtained from the portal vein to measure renin angiotensin system(RAS) components.RESULTS: PRA, Ang Ⅰ, Ang Ⅱ and Ang-(1-7) were significantly lower in the portal vein and periphery in all subgroups treated with propranolol as compared to non-treated. The relationships between Ang-(1-7) and Ang Ⅰ levels and between Ang Ⅱ and Ang Ⅰ were significantly increased in LD group receiving propranolol. The ratio between Ang-(1-7) and Ang Ⅱ remained unchanged in splanchnic and peripheral circulation in patients under 13-blockade, whereas the relationship between Ang Ⅱ and Ang Ⅰ was significantly increased in splanchnic circulation of LT patients treated with propranolol. During liver transplantation, cardiac output and index as well systemic vascular resistance and index were reduced in propranolol-treated subgroup.CONCLUSION: In LD group, propranolol treatment reduced RAS mediators, but did not change the ratio between Ang-(1-7) and Ang Ⅱ in splanchnic and peripheral circulation. Furthermore, the modification of hemodynamic parameters in propranolol treated patients was not associated with changes in the angiotensin ratio.

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

    Chen, Zhe; Treisman, Anne

    2008-08-01

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

  20. Aerosol influence domain of Beijing and peripheral city agglomeration and its climatic effect

    XU Xiangde; SHI Xiaohui; ZHANG Shengjun; DING Guoan; MIAO Qiuju; ZHOU Li

    2006-01-01

    The aerosol distribution in Beijing and peripheral cities agglomeration (BPCA) and its regional climatic effect are investigated on the basis of the statistical analyses of satellite Total Ozone Mapping Spectrometer (TOMS) retrieval aerosol optical depth (AOD) and the meteorological data of sunshine duration, fog days, and low cloud cover, observed at Beijing and its peripheral meteorological stations. The analysis on multi-samples variational correction of the satellite remote sensing Moderate Resolution Imaging Spectroradiometer (MODIS) AOD under the clear sky and stable weather condition in conjunction with surface observations reveal that there was a "triangle-like" distribution pattern of the high values of aerosols in the southern "valley" of the "U-shape"megarelief of Beijing and its peripheral areas. The distribution pattern suggests that the large-scale transfer and diffusion of city agglomeration pollutants might form a relatively persistent characteristic spatial distribution of city agglomeration pollutants much larger than city-scale. Under the background of the particular megarelief effect of Beijing and peripheral areas, the high value area of TOMS AOD, as well as regional correlation distribution between clear sky sunshine duration and TOMS AOD are also similar to the composite image of MODIS AOD variational fields,that is to say, the effect of atmospheric aerosols was very distinctive in Beijing and peripheral areas. The high value area of the negative correlation between clear sky sunshine duration and TOMS AOD approximately accorded with the significant negative value area of the sunshine duration deviations of the 1980s to the 1990s, and the daily variations of the AOD also showed an anti-phase relation with those of clear sky sunshine duration. The above high correlation area of the urban aerosol impact of Beijing-Tianjin region leant towards south peripheral area,with its "center of gravity" in the south of Beijing-Tianjin agglomeration, and

  1. Factors associated with a continuous regular analgesic use - a population-based study of more than 45,000 Danish women and men 18-45 years of age

    Hargreave, Marie; Andersen, Tina Veje; Nielsen, Ann;

    2010-01-01

    Widespread use of and serious adverse effects associated with use of analgesics accentuates the need to consider factors related to analgesic use. The objective of this study was to describe continuous regular analgesics use and examine factors associated with a continuous regular analgesic use....

  2. Antiplasmodial and analgesic activities ofClausena anisata

    Jude E Okokon; Ette O Etebong; John A Udobang; Grace E Essien

    2012-01-01

    Objective:Antiplasmodial and analgesic activities of the leaf extract and fractions ofClausena anisata (C. anisata) were evaluated for antimalarial and analgesic activities.Methods:The crude leaf extract (39 - 117 mg/kg) and fractions (chloroform and acqeous; 78 mg/kg) ofC. anisata were investigated for antiplasmodial activity against chloroquine-sensitivePlasmodium berghei (P. berghei ) infections in mice using suppressive, prophylactic and curative models and analgesic activity against acetic acid, formalin and heat-induced pains. Artesunate,5 mg/kg and pyrimethamine,1.2 mg/kg were used as positive controls. Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice.Results: The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine-sensitive P. berghei in prophylactic, suppressive and curative models in mice. These reductions were statistically significant (P<0.001). They also improved the mean survival time (MST) from17 to21 days relative to control (P<0.01 - 0.001). On chemically and thermally- induced pains, the extract inhibited acetic acid and formalin-induced inflammation as well as hot plate-induced pain in mice. These inhibitions were statistically significant (P<0.001) and in a dose-dependent fashion. Conclusions: The antiplasmodial and analgesic effects of this plant may in part be mediated through its chemical constituents and it can be concluded that the C. anisata possess significant antimalarial and analgesic properties.

  3. The effect of stress on core and peripheral body temperature in humans.

    Vinkers, Christiaan H; Penning, Renske; Hellhammer, Juliane; Verster, Joris C; Klaessens, John H G M; Olivier, Berend; Kalkman, Cor J

    2013-09-01

    Even though there are indications that stress influences body temperature in humans, no study has systematically investigated the effects of stress on core and peripheral body temperature. The present study therefore aimed to investigate the effects of acute psychosocial stress on body temperature using different readout measurements. In two independent studies, male and female participants were exposed to a standardized laboratory stress task (the Trier Social Stress Test, TSST) or a non-stressful control task. Core temperature (intestinal and temporal artery) and peripheral temperature (facial and body skin temperature) were measured. Compared to the control condition, stress exposure decreased intestinal temperature but did not affect temporal artery temperature. Stress exposure resulted in changes in skin temperature that followed a gradient-like pattern, with decreases at distal skin locations such as the fingertip and finger base and unchanged skin temperature at proximal regions such as the infra-clavicular area. Stress-induced effects on facial temperature displayed a sex-specific pattern, with decreased nasal skin temperature in females and increased cheek temperature in males. In conclusion, the amplitude and direction of stress-induced temperature changes depend on the site of temperature measurement in humans. This precludes a direct translation of the preclinical stress-induced hyperthermia paradigm, in which core temperature uniformly rises in response to stress to the human situation. Nevertheless, the effects of stress result in consistent temperature changes. Therefore, the present study supports the inclusion of body temperature as a physiological readout parameter of stress in future studies.

  4. Synthesis of novel trifluoromethyl-substituted spiro-[chromeno[4,3-d]pyrimidine-5,1'-cycloalkanes], and evaluation of their analgesic effects in a mouse pain model.

    Bonacorso, Helio G; Rosa, Wilian C; Oliveira, Sara M; Brusco, Indiara; Brum, Evelyne S; Rodrigues, Melissa B; Frizzo, Clarissa P; Zanatta, Nilo

    2017-04-01

    Herein we report the synthesis of twelve 2,5-substituted 4-(trifluoromethyl)-spirochromeno[4,3-d]pyrimidines (7-10), as well as an evaluation of their analgesic effect in a mouse pain model. The nine new chromeno[4,3-d]pyrimidines (7-9) were synthesized from the cyclocondensation reactions of three 2,2,2-trifluoro-1-(4-methoxyspiro[chromene-2,1'-cycloalkane]-3-yl)ethanones (3) containing 5-, 6- and 7-membered spirocycloalkanes, with some well-known amidine salts (4-6) [NH2CR(NH)]-in which R=Me, Ph, and NH2-at yields of 60-95%. Subsequently, three new 2-(pyrrol-1-yl)-4-(trifluoromethyl)-chromeno[4,3-d]pyrimidines (10) were obtained through a Clauson-Kaas reaction between the respective 2-(amino)-4-(trifluoromethyl)-chromeno[4,3-d]pyrimidines (9) and 2,5-dimethoxy-tetrahydrofuran. The analgesic evaluation showed that these 4-(trifluoromethyl)chromeno[4,3-d]pyrimidines (100mg/kg, p.o.) and Ketoprofen (100mg/kg, p.o.) significantly reduced capsaicin-induced spontaneous nociception. Moreover, the 2-pyrrolyl-spirocyclohexane derivative 10b (100 and 300mg/kg, p.o.) had an anti-allodynic effect comparable to Ketoprofen (100 and 300mg/kg, p.o.) in the arthritic pain model, without causing locomotor alterations in the mice. These results suggest that the compound 10b is a promising molecule for new analgesic drugs in the treatment of pathological pain, such as in arthritis.

  5. Age and gender effects on DNA strand break repair in peripheral blood mononuclear cells

    Garm, Christian; Moreno-Villanueva, Maria; Bürkle, Alexander;

    2013-01-01

    single-strand breaks (SSBs) and double-strand breaks (DSBs) in human peripheral blood mononuclear cells (PBMCs). Of these lesions, DSBs are the least frequent but the most dangerous for cells. We have measured the level of endogenous SSBs, SSB repair capacity, γ-H2AX response, and DSB repair capacity...... in a study population consisting of 216 individuals from a population-based sample of twins aged 40-77 years. Age in this range did not seem to have any effect on the SSB parameters. However, γ-H2AX response and DSB repair capacity decreased with increasing age, although the associations did not reach...

  6. Effect of insulin-induced hypoglycaemia on the peripheral nervous system

    Jensen, Vivi Flou Hjorth; Mølck, A.-M.; Bøgh, I. B.

    2014-01-01

    Insulin-induced hypoglycaemia (IIH) is a common acute side effect in type 1 and type 2 diabetic patients, especially during intensive insulin therapy. The peripheral nervous system (PNS) depends on glucose as its primary energy source during normoglycaemia and, consequently, it may be particularly...... prone to IIH than the central nervous system when hypoglycaemia is not severe (blood glucose level ≤ 2 mm), possibly reflecting a preferential protection of the brain during periods of inadequate glucose availability. With a primary focus on evidence from experimental animal studies investigating...

  7. Effects of peripherally administered urocortin 3 on feeding behavior and gastric emptying in mice

    2011-01-01

    Human and mouse urocortin 3 (Ucn3) were first identified in 2001. Ucn3 binds selectively to corticotropin-releasing factor receptor type 2 (CRF-R2). Previous studies have shown that centrally administered Ucn3 decreases food intake in rats. However, the role of Ucn3 in the regulation of gut motility remains to be determined. In the present study, we investigated the effects of peripherally administered Ucn3 on food intake and gastric emptying in mice. After intraperitoneal (i.p.) administrati...

  8. Effect of peripheral nerve on the neurite growth from retinal explants in culture

    LiuLi; SoKwokfai

    1990-01-01

    The effect of peripheral nerve (PN) on neurite outgrowth from retinal explants of adult hamsters was examined.Cultures of retinal explants,and co-cultures of retinal explants and PN were performed using chick retinal basement memebrane (BM) as substrate.The presence of PN increases the number and length of neurite outgrowth.In addition,a high proportion of neurites situated close to PN tend to grow towards it.Since there was no contact between retinal explants and PN,we suggest that PN might secete diffusible substances to attract the neurites to grow towards it.

  9. Anti-inflammatory and analgesic activities of Melanthera scandens

    Jude E Okokon; Anwanga E Udoh; Samuel G Frank; Louis U Amazu

    2012-01-01

    Objective: To evaluate the anti-inflammatory and analgesic activities of leaf extract of Melanthera scandens (M. scandens). Methods: The crude leaf extract (39-111 mg/kg) of M. scandens was investigated for anti-inflammatory and analgesic activities using various experimental models. The anti-inflammatory activity was investigated using carragenin, egg-albumin induced oedema models, while acetic acid, formalin-induced paw licking and thermal-induced pain models were used to evaluate the antinociceptive property. Results: The extract caused a significant (P<0.05 - 0.001) dose-dependent reduction of inflammation and pains induced by different agents used. Conclusions: The leaf extract possesses anti-inflammatory and analgesic effects which may be mediated through the phytochemical constituents of the plant.

  10. Deep neural network architectures for forecasting analgesic response.

    Nickerson, Paul; Tighe, Patrick; Shickel, Benjamin; Rashidi, Parisa

    2016-08-01

    Response to prescribed analgesic drugs varies between individuals, and choosing the right drug/dose often involves a lengthy, iterative process of trial and error. Furthermore, a significant portion of patients experience adverse events such as post-operative urinary retention (POUR) during inpatient management of acute postoperative pain. To better forecast analgesic responses, we compared conventional machine learning methods with modern neural network architectures to gauge their effectiveness at forecasting temporal patterns of postoperative pain and analgesic use, as well as predicting the risk of POUR. Our results indicate that simpler machine learning approaches might offer superior results; however, all of these techniques may play a promising role for developing smarter post-operative pain management strategies.

  11. 氟比洛芬酯超前镇痛效果的Meta分析%Meta-analysis of flurbiprofen on preemptive analgesic effect

    张旭彤; 黄志莲; 李兴旺; 李军

    2011-01-01

    AIM: Meta analysis of preoperative use of flurbiprofen on postoperative analgesia efficacy and safety. METHODS: 15 articles were sieved into the pump out of according to set a comprehensive search of the database search methods and research into the proposed standard from 267 documents, applications RevMan 5. 0 software into the pump after the literature 4 h, 24 h two time points Meta-analysis of VAS score. RESULTS; 15 articles of the heterogeneity test showed the results of trials was significantly (P<0. 05), select the random effects model analysis. Meta analysis showed that the forest plan-, post- operative 4 h, 24 h of VAS combined effect of the amount of test score were statisti-cally significant in analgesic effect between flurbiprofen group and control group (P<0. 05). The number of patients in the combined adverse effects of the amount of testing was not statistically significant, still could not believe that flurbiprofen group and control group differences in adverse reactions. CONCLUSION: The available clinical data indicate that preoperative use of flurbiprofen can reduce postoperative pain, patients still can not believe that could reduce the incidence of adverse reactions.%目的:评价术前使用氟比洛芬酯对术后镇痛的有效性和安全性.方法:按设定的检索方法全面检索万方、维普数据库,根据研究的纳入标准在267篇文献中筛出15篇有效文献,应用RevMan 5.0软件对文献中术后4h、24 h两个时间点的视觉模拟评分法(Visual Analogue Score,VAS)评分进行Meta分析.结果:15篇文献研究的异质性检验显示试验结果的差异有统计学意义(P<0.05);选择随机效应模型进行分析,Meta 森林图分析结果显示:术后4h、24 h的VAS评分合并效应量的检验均具有统计学意义,认为氟比洛芬酯组较空白对照组的镇痛效果有差异(P<0.05);不良反应例数的合并效应量的检验不具有统计学意义,尚不能认为

  12. Effect of peripheral 5-HT on glucose and lipid metabolism in wether sheep.

    Hitoshi Watanabe

    Full Text Available In mice, peripheral 5-HT induces an increase in the plasma concentrations of glucose, insulin and bile acids, and a decrease in plasma triglyceride, NEFA and cholesterol concentrations. However, given the unique characteristics of the metabolism of ruminants relative to monogastric animals, the physiological role of peripheral 5-HT on glucose and lipid metabolism in sheep remains to be established. Therefore, in this study, we investigated the effect of 5-HT on the circulating concentrations of metabolites and insulin using five 5-HT receptor (5HTR antagonists in sheep. After fasting for 24 h, sheep were intravenously injected with 5-HT, following which-, plasma glucose, insulin, triglyceride and NEFA concentrations were significantly elevated. In contrast, 5-HT did not affect the plasma cholesterol concentration, and it induced a decrease in bile acid concentrations. Increases in plasma glucose and insulin concentrations induced by 5-HT were attenuated by pre-treatment with Methysergide, a 5HTR 1, 2 and 7 antagonist. Additionally, decreased plasma bile acid concentrations induced by 5-HT were blocked by pre-treatment with Ketanserin, a 5HTR 2A antagonist. However, none of the 5HTR antagonists inhibited the increase in plasma triglyceride and NEFA levels induced by 5-HT. On the other hand, mRNA expressions of 5HTR1D and 1E were observed in the liver, pancreas and skeletal muscle. These results suggest that there are a number of differences in the physiological functions of peripheral 5-HT with respect to lipid metabolism between mice and sheep, though its effect on glucose metabolism appears to be similar between these species.

  13. The effect on knee-joint load of instruction in analgesic use compared with neuromuscular exercise in patients with knee osteoarthritis

    Clausen, Brian; Holsgaard-Larsen, Anders; Søndergaard, Jens

    2014-01-01

    BACKGROUND: Knee osteoarthritis (OA) is a mechanically driven disease, and it is suggested that medial tibiofemoral knee-joint load increases with pharmacologic pain relief, indicating that pharmacologic pain relief may be positively associated with disease progression. Treatment modalities......, compared with optimized analgesics and antiinflammatory drug use, on the measures of knee-joint load in people with mild to moderate medial tibiofemoral knee osteoarthritis. METHOD/DESIGN: One hundred men and women with mild to moderate medial knee osteoarthritis will be recruited from general medical...... and physical function in people with mild to moderate knee osteoarthritis. TRIAL REGISTRATION: ClinicalTrials.gov Identifier: NCT01638962 (July 3, 2012)....

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

    Szucs Szilard

    2012-06-01

    Full Text Available Abstract Background Peripheral nerve blocks are effective in treating acute pain, thereby minimizing the requirement for opiate analgesics. Fractured neck of femur (FNF is a common, painful injury. The provision of effective analgesia to this cohort is challenging but an important determinant of their functional outcome. We investigated the analgesic efficacy of continuous femoral nerve block (CFNB in patients with FNF. Methods Following institutional ethical approval and with informed consent, patients awaiting FNF surgery were randomly allocated to receive either standard opiate-based analgesia (Group 1 or a femoral perineural catheter (Group 2. Patients in Group 1 received parenteral morphine as required. Those in Group 2 received a CFNB comprising a bolus of local anaesthetic followed by a continuous infusion of 0.25% bupivacaine. For both Groups, rescue analgesia consisted of intramuscular morphine as required and all patients received paracetamol regularly. Pain was assessed using a visual analogue scale at rest and during passive movement (dynamic pain score at 30 min following first analgesic intervention and six hourly thereafter for 72 hours. Patient satisfaction with the analgesic regimen received was recorded using verbal rating scores (0-10. The primary outcome measured was dynamic pain score from initial analgesic intervention to 72 hours later. Results Of 27 recruited, 24 patients successfully completed the study protocol and underwent per protocol analysis. The intervals from recruitment to the study until surgery were similar in both groups [31.4(17.7 vs 27.5(14.2 h, P = 0.57]. The groups were similar in terms of baseline clinical characteristics. For patients in Group 2, pain scores at rest were less than those reported by patients in Group 1 [9.5(9.4 vs 31(28, P = 0.031]. Dynamic pain scores reported by patients in Group 2 were less at each time point from 30 min up to 54 hours [e.g at 6 h 30.7(23.4 vs 67

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

    Szucs, Szilard

    2012-06-27

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

  16. Over-the-counter analgesic use.

    De Broe, Marc E; Elseviers, Monique M

    2009-10-01

    Chronic analgesic nephropathy, particularly chronic interstitial nephritis and renal papillary necrosis, results from daily use for many years of mixtures containing at least two analgesics and caffeine or dependence-inducing drugs. Computed tomography scan can accurately diagnose this disease even in the absence of reliable information on previous analgesic use. The occasion to moderate regular use of aspirin and nonsteroidal anti-inflammatory drugs is without renal risk when renal function is normal. Paracetamol use is less clear although the risk is not great. The continued use of non-phenacetin-combined analgesics with or without nonsteroidal anti-inflammatory drugs is associated with faster progression toward renal impairment. As long as high-risk analgesic mixtures are available over the counter, analgesic nephropathy will continue to be a problem.

  17. Analgesic effect of intrathecal bumetanide is accompanied by changes in spinal sodium-potassium-chloride co-transporter 1 and potassium-chloride co-transporter 2 expression in a rat model of incisional pain

    Yanbing He; Shiyuan Xu; Junjie Huang; Qingjuan Gong

    2014-01-01

    Accumulating evidence has demonstrated that the sodium-potassium-chloride co-transporter 1 and potassium-chloride co-transporter 2 have a role in the modulation of pain transmission at the spinal level through chloride regulation in the pain pathway and by effecting neuronal excitability and pain sensitization. The present study aimed to investigate the analgesic effect of the speciifc sodium-potassium-chloride co-transporter 1 inhibitor bumetanide, and the change in spinal sodium-potassium-chloride co-transporter 1 and potassium-chloride co-transporter 2 expression in a rat model of incisional pain. Results showed that intrathecal bumetanide could decrease cumulative pain scores, and could increase thermal and mechanical pain thresholds in a rat model of incisional pain. Sodium-potassium-chloride co-transporter 1 expression in-creased in neurons from dorsal root ganglion and the deep laminae of the ipsilateral dorsal horn following incision. By contrast, potassium-chloride co-transporter 2 expression decreased in neurons of the deep laminae from the ipsilateral dorsal horn. These ifndings suggest that spinal sodium-potassium-chloride co-transporter 1 expression was up-regulated and spinal potassi-um-chloride co-transporter 2 expression was down-regulated following incision. Intrathecal bumetanide has analgesic effects on incisional pain through inhibition of sodium-potassi-um-chloride co-transporter 1.

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

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

    2012-11-01

    H-Dmt-D-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA) is a synthetic tetrapeptide with extraordinary selectivity for the mu-opioid receptor and is an extremely potent analgesic. [Dmt(1) ]DALDA is unusual in the way that the greater part of its analgesic potency appears to be produced by its actions in the spinal cord. Furthermore, [Dmt(1) ]DALDA inhibits norepinephrine re-uptake and is a mitochondria-targeted antioxidant. Such characteristics may make [Dmt(1)]DALDA particularly effective against neuropathic pain. The present study was designed to compare the effects of [Dmt(1)]DALDA and morphine on thermal hyperalgesia in an experimental neuropathic pain model. Neuropathic pain was induced in rats by surgical ligation of the L5 spinal nerve, and thermal pain thresholds were assessed by latencies of paw withdrawal to radiant heat. The increase in paw withdrawal latency was greater after the administration of [Dmt(1) ]DALDA than that of morphine in neuropathic rats at doses that were equianalgesic in naïve animals. We conclude that [Dmt(1)]DALDA is more effective than morphine against thermal hyperalgesia in this experimental model of neuropathic pain.

  19. Analgesic effects of balanced acupuncture versus body acupuncture in low-back and leg pain patients with lumbar disc herniation, as assessed by resting-state functional magnetic resonance imaging

    Yongsong Ye; Bo Liu

    2012-01-01

    Balanced acupuncture, a single-acupoint balance therapy, regulates the balance of the cerebral center, and is characterized by exerting quick effects and a short treatment course. A total of 20 low-back and leg pain patients with lumbar disc herniation were treated with balanced acupuncture or body acupuncture. Central mechanisms of varied acupunctures were compared using rest-ing-state functional MRI. Patients from both groups received functional MRI before and after acu-puncture. Functional connectivity in brain regions that were strongly associated with the bilateral amygdala was analyzed utilizing AFNI software. Visual analogue scale scores were greater in the balanced acupuncture group compared with the body acupuncture group. Function of the endoge-nous pain regulation network was enhanced in patients in the balanced acupuncture group, but was not changed in the body acupuncture group. This result indicates that the analgesic effects of body acupuncture do not work through the central nervous system. These data suggest that balanced acupuncture exerts analgesic effects on low-back and leg pain patients with lumbar disc herniation by regulating the function of the endogenous pain regulation network.

  20. The Contemporary Safety and Effectiveness of Lower Extremity Bypass Surgery and Peripheral Endovascular Interventions in the Treatment of Symptomatic Peripheral Arterial Disease

    Rehring, Thomas F.; Rogers, R. Kevin; Shetterly, Susan M.; Wagner, Nicole M.; Gupta, Rajan; Jazaeri, Omid; Hedayati, Nasim; Jones, W. Schuyler; Patel, Manesh R.; Ho, P. Michael; Go, Alan S.; Magid, David J.

    2015-01-01

    Background— Treatment for symptomatic peripheral artery disease includes lower extremity bypass surgery (LEB) and peripheral endovascular interventions (PVIs); however, limited comparative effectiveness data exist between the 2 therapies. We assessed the safety and effectiveness of LEB and PVI in patients with symptomatic claudication and critical limb ischemia. Methods and Results— In a community-based clinical registry at 2 large integrated healthcare delivery systems, we compared 883 patients undergoing PVI and 975 patients undergoing LEB between January 1, 2005 and December 31, 2011. Rates of target lesion revascularization were greater for PVI than for LEB in patients presenting with claudication (12.3±2.7% and 19.0±3.5% at 1 and 3 years versus 5.2±2.4% and 8.3±3.1%, log-rank P<0.001) and critical limb ischemia (19.1±4.8% and 31.6±6.3% at 1 and 3 years versus 10.8±2.5% and 16.0±3.2%, log-rank P<0.001). However, in comparison with PVI, LEB was associated with increased rates of complications up to 30 days following the procedure (37.1% versus 11.9%, P<0.001). There were no differences in amputation rates between the 2 groups. Findings remained consistent in sensitivity analyses by using propensity methods to account for treatment selection. Conclusions— In patients with symptomatic peripheral artery disease, in comparison with LEB, PVI was associated with fewer 30-day procedural complications, higher revascularization rates at 1 and 3 years, and no difference in subsequent amputations. PMID:26362632

  1. Prejunctional and peripheral effects of the cannabinoid CB(1) receptor inverse agonist rimonabant (SR 141716).

    van Diepen, Hester; Schlicker, Eberhard; Michel, Martin C

    2008-10-01

    Rimonabant is an inverse agonist specific for cannabinoid receptors and selective for their cannabinoid-1 (CB(1)) subtype. Although CB(1) receptors are more abundant in the central nervous system, rimonabant has many effects in the periphery, most of which are related to prejunctional modulation of transmitter release from autonomic nerves. However, CB(1) receptors are also expressed in, e.g., adipocytes and endothelial cells. Rimonabant inhibits numerous cardiovascular cannabinoid effects, including the decrease of blood pressure by central and peripheral (cardiac and vascular) sites of action, with the latter often being endothelium dependent. Rimonabant may also antagonize cannabinoid effects in myocardial infarction and in hypotension associated with septic shock or liver cirrhosis. In the gastrointestinal tract, rimonabant counteracts the cannabinoid-induced inhibition of secretion and motility. Although not affecting most cannabinoid effects in the airways, rimonabant counteracts inhibition of smooth-muscle contraction by cannabinoids in urogenital tissues and may interfere with embryo attachment and outgrowth of blastocysts. It inhibits cannabinoid-induced decreases of intraocular pressure. Rimonabant can inhibit proliferation of, maturation of, and energy storage by adipocytes. Among the many cannabinoid effects on hormone secretion, only some are rimonabant sensitive. The effects of rimonabant on the immune system are not fully clear, and it may inhibit or stimulate proliferation in several types of cancer. We conclude that direct effects of rimonabant on adipocytes may contribute to its clinical role in treating obesity. Other peripheral effects, many of which occur prejunctionally, may also contribute to its overall clinical profile and lead to additional indications as well adverse events.

  2. Bottlenecks in the development of topical analgesics: molecule, formulation, dose-finding, and phase III design

    Keppel Hesselink JM

    2017-03-01

    Full Text Available Jan M Keppel Hesselink,1 David J Kopsky,2 Stephen M Stahl3 1Institute Neuropathic Pain, Bosch en Duin, the Netherlands; 2Institute Neuropathic Pain, Amsterdam, the Netherlands; 3University of California San Diego, La Jolla, CA, USA Abstract: Topical analgesics can be defined as topical formulations containing analgesics or co-analgesics. Since 2000, interest in such formulations has been on the rise. There are, however, four critical issues in the research and development phases of topical analgesics: 1 The selection of the active pharmaceutical ingredient. Analgesics and co-analgesics differ greatly in their mechanism of action, and it is required to find the most optimal fit between such mechanisms of action and the pathogenesis of the targeted (neuropathic pain. 2 Issues concerning the optimized formulation. For relevant clinical efficacy, specific characteristics for the selected vehicle (eg, cream base or gel base are required, depending on the physicochemical characteristics of the active pharmaceutical ingredient(s to be delivered. 3 Well-designed phase II dose-finding studies are required, and, unfortunately, such trials are missing. In fact, we will demonstrate that underdosing is one of the major hurdles to detect meaningful and statistically relevant clinical effects of topical analgesics. 4 Selection of clinical end points and innovatively designed phase III trials. End point selection can make or break a trial. For instance, to include numbness together with tingling as a composite end point for neuropathic pain seems stretching the therapeutic impact of an analgesic too far. Given the fast onset of action of topical analgesics (usually within 30 minutes, enrichment designs might enhance the chances for success, as the placebo response might decrease. Topical analgesics may become promising inroads for the treatment of neuropathic pain, once sufficient attention is given to these four key aspects. Keywords: topical, analgesics

  3. Neuroimmune Interaction in the Regulation of Peripheral Opioid-Mediated Analgesia in Inflammation.

    Hua, Susan

    2016-01-01

    Peripheral immune cell-mediated analgesia in inflammation is an important endogenous mechanism of pain control. Opioid receptors localized on peripheral sensory nerve terminals are activated by endogenous opioid peptides released from immune cells to produce significant analgesia. Following transendothelial migration of opioid-containing leukocytes into peripheral sites of inflammation, opioid peptides are released into a harsh milieu associated with an increase in temperature, low pH, and high proteolytic activity. Together, this microenvironment has been suggested to increase the activity of opioid peptide metabolism. Therefore, the proximity of immune cells and nerve fibers may be essential to produce adequate analgesic effects. Close associations between opioid-containing immune cells and peripheral nerve terminals have been observed. However, it is not yet determined whether these immune cells actually form synaptic-like contacts with peripheral sensory terminals and/or whether they secrete opioids in a paracrine manner. This review will provide novel insight into the peripheral mechanisms of immune-derived analgesia in inflammation, in particular, the importance of direct interactions between immune cells and the peripheral nervous system.

  4. Effect of Diet and Exercise on the Peripheral Immune System in Young Balb/c Mice

    Martínez-Carrillo, B. E.; Jarillo-Luna, R. A.; Campos-Rodríguez, R.; Valdés-Ramos, R.; Rivera-Aguilar, V.

    2015-01-01

    Although diet and exercise clearly have an influence on immune function, studies are scarce on the effect caused by exercise and the consumption of a carbohydrate-rich or fat-rich diet on the peripheral immune system. The aim of the present study was to evaluate the effect of exercise and the two aforementioned unbalanced diets on young Balb/c mice, especially in relation to BMI, the level of glucose, and the percentage of lymphocyte subpopulations in peripheral blood. The changes found were then related to the synthesis of leptin and adiponectin as well as the production of oxidative stress. The increase in BMI found with the carbohydrate-rich and fat-rich diets showed correlation with the levels of leptin and adiponectin. An increase in leptin and a decrease in adiponectin directly correlated with an increase in total lymphocytes and CD4+ cells and with a decrease in B cells. The increase in leptin also correlated with an increase in CD8+ cells. Glycemia and oxidative stress increased with the two unbalanced diets, negatively affecting the proliferation of total lymphocytes and the percentage of B cells, apparently by causing alterations in proteins through carbonylation. These alterations caused by an unbalanced diet were not modified by moderate exercise. PMID:26634209

  5. Position displacement effect on the doses in the peripheral head regions

    Kortesniemi, M.; Seppaelae, T.; Bjugg, H. [Helsinki Univ., Department of Physics, Helsinki (Finland); Seren, T.; Kotiluoto, P.; Auterinen, I. [VTT Chemical Technology, Espoo (Finland); Parkkinen, R. [STUK Finnish Radiation and Nuclear Safety Authority, Helsinki (Finland); Savolainen, S. [Helsinki Univ. Hospital, Departments of Radiology, Helsinki (Finland)

    2000-10-01

    Patient positioning is a challenging task in BNCT-treatments due to the use of multiple fields and a static horizontal beam construction. Positioning accuracy of 5 mm is required for acceptable dose delivery within appropriate limits of dose uncertainty (up to 10% of point dose in target volume). The aim of this study was to determine if a patient head position creating a clear gap between the beam port and the head would have a significant effect on the doses to the peripheral regions of the head, e.g. to the eyes. The gamma dose rates were measured in a water filled ellipsoidal phantom with an ionisation chamber (IC). Mn activation wires were used to determine the Mn-55(n, {gamma}) reaction rates. Twelve measurement points were chosen in the phantom and two phantom positions were applied. According to this study the 35 mm position change and the resulting gap has an obvious effect on the peripheral doses in BNCT. The Mn activation reaction rates were on the average 80% higher in the deviation position than in the reference position. Increasing depth from the surface inside the phantom diminished the gamma dose difference between the two positions. Scattering environment changes with position displacement and resulting gap causes differences in neutron fluences and gamma doses. (author)

  6. Effects of pigment epithelium derived factor (PEDF) on malignant peripheral nerve sheath tumours (MPNSTs).

    Demestre, Maria; Terzi, Menderes Yusuf; Mautner, Victor; Vajkoczy, Peter; Kurtz, Andreas; Piña, Ana Luisa

    2013-12-01

    Neurofibromatosis type 1 (NF1) is an inherited genetic disease affecting 1 in 3,500 individuals. A prominent feature of NF1 is the formation of benign tumours of the peripheral nerve sheath (neurofibromas). However, these can become malignant and form highly metastatic malignant peripheral nerve sheath tumours (MPNST), which are usually fatal despite aggressive surgery, chemotherapy, and radiotherapy. Recent studies have shown that pigment epithelium-derived factor (PEDF) can induce differentiation and inhibit angiogenesis in several kinds of tumours. The present study was designed to determine the in vitro and in vivo effects of PEDF on MPNST angiogenesis and tumour growth. PEDF inhibited proliferation and augmented apoptosis in S462 MPNST cells after 48 h of treatment in culture. In xenografts of S462 MPNST cells in athymic nude mice, PEDF suppressed MPNST tumour burden, due mainly to inhibition of angiogenesis. These results demonstrate for the first time inhibitory effects of PEDF on the growth of human MPNST via induction of anti-angiogenesis and apoptosis. Our results suggest that PEDF could be a novel approach for future therapeutic purposes against MPNST.

  7. 加巴喷丁对骨癌痛模型大鼠的镇痛作用及机制研究%Research on the analgesic effect and mechanism of gabapentin on rats model with tibia metastatic cancer pain

    张莹; 王志国; 孙丹丹; 欧阳竞锋; 赵小亮; 王丹巧; 李涛; 崔悦; 牛晓红

    2014-01-01

    目的:研究加巴喷丁对Walker-256乳腺癌细胞构建的大鼠胫骨转移性癌痛模型的镇痛作用及其机制。方法雌性wistar大鼠30只,随机分为假手术组(sham)、模型组(model)和加巴喷丁组(GBP,100 mg/kg),每组10只;分别进行操作对照和胫骨转移性癌痛造模手术。以机械痛缩足域值和影像学观察作为大鼠疼痛行为学的评价指标;分别采用微透析分析仪 ISCUSFflex Microdialysis Analyzer、放射免疫法、流式多因子检测技术,测定脑脊液中谷氨酸(Glutamate,Glu)、脊髓中P物质(Substance P,SP)及肿瘤局部组织中白细胞介素-12/P70(Interleukin-12/p70,IL-12P70)、γ干扰素(Interferon-γ,IFN-γ)及β-神经生长因子(β-nerve growth factor,β-NGF)的含量。结果与假手术组相比,手术组胫骨转移性癌痛模型大鼠机械痛缩足域值明显下降,影像学观察到骨质破坏,脑脊液中Glu、脊髓中SP水平明显升高(P<0.01,P<0.05),肿瘤组织中IL-12P70、IFN-γ水平明显降低而β-NGF水平明显升高(P<0.05)。与模型组相比,加巴喷丁给药后30 min大鼠机械痛缩足阈值开始上升,60~300 min明显升高(均P<0.01)。加巴喷丁显著降低了骨癌痛大鼠脑脊液中Glu、脊髓中SP浓度(P<0.01,P<0.05),提高了大鼠肿瘤组织中IL-12P70和IFN-γ水平,降低了β-NGF浓度(P<0.05)。结论加巴喷丁可减轻骨癌痛大鼠的疼痛行为学指标,其镇痛机制可能与抑制中枢兴奋性氨基酸、痛感调质及周围神经生长因子水平、增强外周的免疫作用有关。%Objective To study the analgesic effect and mechanism of gabapentin on tibia metastatic cancer pain rat model constructed by walker-256 breast cancer cells.Methods 30 Female wistar rats were randomly divided into sham group,model group and GBP group(100 mg/kg),each group had 10 rats.Sham operation were used as operation

  8. Analgesic Activity of Sphaeranthus indicus Linn

    P. Malairajan

    2012-12-01

    Full Text Available The ethanol extracts of the whole plant Sphaeranthus indicus Linn. (ALSI (Compositae was tested for analgesic activity by tail immersion method in rat models. The test extracts were tested at 250 mg and 500 mg/kg body weight. The analgesic activity was assessed by keeping pentazocine 10 mg/kg as standard drug. The parameters studied were tail withdrawal reflex and percentage protection. In tail immersion method ALSI pretreatment caused significant increase in analgesic activity and percentage protection found was 66.6 and 67.4 respectively. The result suggested that ALSI possess significant and dose dependent analgesic activity.

  9. Enhanced analgesic properties and reduced ulcerogenic effect of a mononuclear copper(II) complex with fenoprofen in comparison to the parent drug: promising insights in the treatment of chronic inflammatory diseases.

    Agotegaray, Mariela; Gumilar, Fernanda; Boeris, Mónica; Toso, Ricardo; Minetti, Alejandra

    2014-01-01

    Analgesic and ulcerogenic properties have been studied for the copper(II) coordination complex of the nonsteroidal anti-inflammatory drug Fenoprofen and imidazole [Cu(fen)2(im)2] (Cu: copper(II) ion; fen: fenoprofenate anion from Fenoprofen, im: imidazole). A therapeutic dose of 28 mg/kg was tested for [Cu(fen)2(im)2] and 21 mg/kg was employed for Fenoprofen calcium, administered by oral gavage in female mice to compare the therapeutic properties of the new entity. The acetic acid induced writhing test was employed to study visceral pain. The percentage of inhibition in writhing and stretching was 78.9% and 46.2% for the [Cu(fen)2(im)2] and Fenoprofen calcium, respectively. This result indicates that the complex could be more effective in diminishing visceral pain. The formalin test was evaluated to study the impact of the drugs over nociceptive and inflammatory pain. The complex is a more potent analgesic on inflammatory pain than the parent drug. Ulcerogenic effects were evaluated using a model of gastric lesions induced by hypothermic-restraint stress. Fenoprofen calcium salt caused an ulcer index of about 79 mm(2) while the one caused by [Cu(fen)2(im)2] was 22 mm(2). The complex diminished the development of gastric mucosal ulcers in comparison to the uncomplexed drug. Possible mechanisms of action related to both therapeutic properties have been discussed.

  10. Enhanced Analgesic Properties and Reduced Ulcerogenic Effect of a Mononuclear Copper(II Complex with Fenoprofen in Comparison to the Parent Drug: Promising Insights in the Treatment of Chronic Inflammatory Diseases

    Mariela Agotegaray

    2014-01-01

    Full Text Available Analgesic and ulcerogenic properties have been studied for the copper(II coordination complex of the nonsteroidal anti-inflammatory drug Fenoprofen and imidazole [Cu(fen2(im2] (Cu: copper(II ion; fen: fenoprofenate anion from Fenoprofen, im: imidazole. A therapeutic dose of 28 mg/kg was tested for [Cu(fen2(im2] and 21 mg/kg was employed for Fenoprofen calcium, administered by oral gavage in female mice to compare the therapeutic properties of the new entity. The acetic acid induced writhing test was employed to study visceral pain. The percentage of inhibition in writhing and stretching was 78.9% and 46.2% for the [Cu(fen2(im2] and Fenoprofen calcium, respectively. This result indicates that the complex could be more effective in diminishing visceral pain. The formalin test was evaluated to study the impact of the drugs over nociceptive and inflammatory pain. The complex is a more potent analgesic on inflammatory pain than the parent drug. Ulcerogenic effects were evaluated using a model of gastric lesions induced by hypothermic-restraint stress. Fenoprofen calcium salt caused an ulcer index of about 79 mm2 while the one caused by [Cu(fen2(im2] was 22 mm2. The complex diminished the development of gastric mucosal ulcers in comparison to the uncomplexed drug. Possible mechanisms of action related to both therapeutic properties have been discussed.

  11. Preemptive analgesic effects of low-dose ketamine on growth-associated protein expression in dorsal root ganglion of chronic constriction injury model rats

    Shuyong Lin; Chen Wang

    2008-01-01

    BACKGROUND: Ketamine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonists and plays an important role in the treatment of pain.OBJECTIVE: To analyze the preemptive analgesic effects of different doses of ketamine on growth-associated protein-43 (GAP-43) expression in dorsal root ganglion in a rat model of chronic sciatic nerve constricted injury, and to study the differences between high-dose and low-dose ketamineDESIGN: Randomized controlled animal study.SETTING: Medical College of Shantou University. MATERIALS: Thirty-five adult male Sprague Dawley rats were provided by the Experimental Animal Center of Guangzhou University of Traditional Chinese Medicine. Ketamine hydrochloride injection was provided by Hengrui Pharmaceutical Co., Ltd., Jiangsu. METHODS: This study was performed at the Immunological Laboratory, Medical College of Shantou University from September to December 2006. Model of chronic sciatic nerve constricted injury: after anesthesia, the right sciatic nerve was exposed and ligated 1-cm distal to the ischiadic tuberosity with a No. 3-0 cat gut suture. Grouping and intervention: 35 rats were randomly divided into 4 groups: normal control group (n = 5), chronic constriction injury (CCI) group (n = 10), low-dose ketamine group (n = 10), and high-dose ketamine group (n = 10). Rats in the normal control group did not undergo any surgery or drug intervention. Rats in the CCI group received intraperitoneal injection of saline (1 mL), and their sciatic nerves were ligated after 10 minutes. Rats in the low-dose ketamine group underwent intraperitoneal injection of ketamine (25 mg/kg) 10 minutes prior to ligation of sciatic nerve; while, rats in the high-dose ketamine group were given intraperitoneal injection of ketamine (50 mg/kg) 10 minutes prior to ligation of sciatic nerve. On the third and the seventh days after surgery, dorsal root ganglion were resected from the sciatic nerve and cut into sections. MAIN OUTCOME MEASURES: GAP-43

  12. Effect of low-frequency pulse percutaneous electric stimulation on peripheral nerve injuries at different sites

    Jinwu Wang; Liye Chen; Qi Li; Weifeng Ni; Min Zhang; Shangchun Guo; Bingfang Zeng

    2006-01-01

    BACKGROUND: The postoperative recovery of nerve function in patients with peripheral nerve injury is always an important problem to solve after treatment. The electric stimulation induced electromagnetic field can nourish nerve, postpone muscular atrophy, and help the postoperative neuromuscular function.OBJECTIVE: To observe the effects of low-frequency pulse percutaneous electric stimulation on the functional recovery of postoperative patients with peripheral nerve injury, and quantitatively evaluate the results of electromyogram (EMG) examination before and after treatment.DESIGN: A retrospective case analysis.SETTING: The Sixth People's Hospital affiliated to Shanghai Jiaotong University.PARTICIPANTS: Nineteen postoperative inpatients with peripheral nerve injury were selected from the Department of Orthopaedics, the Sixth People's Hospital affiliated to Shanghai Jiaotong University from June 2005 to January 2006, including 13 males and 6 females aged 24-62 years with an average of 36 years old.There were 3 cases of brachial plexus nerve injury, 3 of median nerve injury, 7 of radial nerve injury, 3 of ulnar nerve injury and 3 of common peroneal nerve injury, and all the patients received probing nerve fiber restoration. Their main preoperative manifestations were dennervation, pain in limbs, motor and sensory disturbances. All the 19 patients were informed with the therapeutic program and items for evaluation.METHODS : ① Low-frequency pulse percutaneous electric stimulation apparatus: The patients were given electric stimulation with the TERESA cantata instrument (TERESA-0, Shanghai Teresa Health Technology, Co.,Ltd.). The patients were stimulated with symmetric square waves of 1-111 Hz, and the intensity was 1.2-5.0 mA, and it was gradually adjusted according to the recovered conditions of neural regeneration following the principle that the intensity was strong enough and the patients felt no obvious upset. They were treated for 4-24 weeks, 10-30 minutes

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

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

    2015-05-01

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

  14. Effects of Flurbiprofen Axetil on Postoperative Analgesia and Cytokines in Peripheral Blood of Thoracotomy Patients.

    Zhou, Mi; Li, Beiping; Kong, Ming

    2015-06-01

    The objective is to study the effects of flurbiprofen axetil (FA) with fentanyl together in postoperative controlled intravenous analgesia (PCIA) on pain intensity, cytokine levels in peripheral blood and adverse reactions of thoracotomy patients. Fifty thoracotomy patients were divided into a FA and a control group, each with 25 cases. Postoperative analgesia was administered in the two groups using PCIA. The pressing times of analgesia pump, the visual analog scale (VAS) scores during resting and coughing at 2, 6, 24, 48, 72 h after surgery and the incidence of adverse drug reactions were recorded. Levels of IL-1β, IL-6, IL-8, IL-2, and TNF-α in peripheral blood were determined before the administration of FA (T0), and at 24 h (T1), 48 h (T2), 72 h (T3) after surgery. The analgesia pump pressing times in the FA group was less than that of the control group. The VAS scores during resting and coughing at 2, 6, 24, 48, 72 h after surgery, were statistically less than those of control group. The incidence rate of nausea and vomiting was insignificantly different between the two groups. Administration of FA together with PCIA in thoracotomy patients can improve postoperative analgesia.

  15. Peripheral Signals Mediate the Beneficial Effects of Gastric Surgery in Obesity

    Silvia Barja-Fernández

    2015-01-01

    Full Text Available Obesity is nowadays a public health problem both in the industrialized world and developing countries. The different treatments to fight against obesity are not very successful with the exception of gastric surgery. The mechanism behind the achievement of this procedure remains unclear although the modifications in the pattern of gastrointestinal hormones production appear to be responsible for the beneficial effect. The gastrointestinal tract has emerged in the last time as an endocrine organ in charge of response to the different stimulus related to nutritional status by the modulation of more than 30 signals acting at central level to modulate food intake and body weight. The production of some of these gastric derived signals has been proved to be altered in obesity (ghrelin, CCK, and GLP-1. In fact, bariatric surgery modifies the production of both gastrointestinal and adipose tissue peripheral signals beyond the gut microbiota composition. Through this paper the main peripheral signals altered in obesity will be reviewed together with their modifications after bariatric surgery.

  16. Analgesic nephropathy selectively affecting a unilateral non-functioning hypoplastic kidney.

    Granese, J; Brightbill, K; Osborne, P; Cox, C E; Gaber, L W

    2007-08-01

    Analgesic nephropathy results from chronic abuse of non-narcotic analgesics, most frequently with the use of phenacetin and mixed analgesic preparations. Renal papillary necrosis and chronic interstitial nephritis with progressive scarring are characteristic of the histopathology of analgesic nephropathy. Typically, papillary necrosis in these patients is bilateral and affects almost all renal papillae. This report describes a case of severe analgesic nephropathy that discriminantly affected a unilateral non-functioning kidney and spared the contralateral normally developed kidney. The patient herein consumed therapeutic doses of acetaminophen and naproxen daily and for several years. We estimated the cumulative doses of acetaminophen and naproxen used by the patient during that period to be approximately 1.0 and 0.4 kg, respectively. The cumulative dose of acetaminophen is at the threshold of doses that were traditionally associated with an increased risk for end-stage kidney failure. Simultaneous intake of both analgesics could have had a synergetic adverse effect on renal function. This case also demonstrates that preexisting renal insufficiency is prerequisite to the development of analgesic nephropathy. Conversely, kidneys with normal function are resistant to the chronic nephrotoxicity associated with habitual analgesic use.

  17. Amiodarone: Effects on thyroid function and the peripheral metabolism of the thyroid hormones

    Braverman, L.E.; Safran, M.; Bambini, G.; Pinchera, A.; Martino, E.

    1985-11-01

    In addition to the effects of Amiodarone on the peripheral metabolism of the thyroid hormones and on pituitary TSH secretion, a major complication of therapy is the relatively high frequency of iodide-induced thyroid dysfunction. The mean T/sub 4/ and T/sub 3/ concentration following Amiodarone application was measured in euthyroid, hypothyroid and hyperthyroid patients and in control patients with and without cardiac disorders. Furthermore, the serum TSH was determined in euthyroid Amiodarone-treated euthyroid patients. /sup 131/I uptake was studied in patients with Amiodarone-associated thyrotoxicosis. The difficulties of the therapy of Amiodarone-induced hyperthyroidism are outlined. Preliminary studied of the effect of Amiodarone and its analogues on the metabolism of thyroid hormones in the rat indicate that Amiodarone may act as a thyroid hormone agonist in the pituitary. (MG).

  18. 塞隆风湿酒对小鼠镇痛、抗寒的实验研究%Experimental Research Analgesic and resist-cool effects in Mice by Sai long Feng shi Wine

    徐淑玲; 沈华; 王笑红

    2001-01-01

    To investigate Analgesic and resist-cool effects of sai long Feng shi wine in mice. Methods: Analgesic action of sai long Feng shi wine was obserated acetic acid-induced writhing test in mice. Anti-cool test was obserad in mice in -20℃ refrigerator.Results: Sai long feng shi wine can inhibit writing reaction and prolong the surrival time in cooled mice.%目的:观察塞隆风湿酒A、B及大小剂量对小鼠镇痛、抗寒冷作用影响。方法:采用昆明系小鼠灌胃塞隆酒A、B不同剂量,观察各组动物对醋酸致痛后发生扭体反应数及各组动物在-20℃低温条件下存活时间。结果:塞隆风湿酒A、B大小剂量对实验动物具有明显的镇痛及抗寒作用。

  19. Cord blood T cells mediate enhanced antitumor effects compared with adult peripheral blood T cells.

    Hiwarkar, Prashant; Qasim, Waseem; Ricciardelli, Ida; Gilmour, Kimberly; Quezada, Sergio; Saudemont, Aurore; Amrolia, Persis; Veys, Paul

    2015-12-24

    Unrelated cord blood transplantation (CBT) without in vivo T-cell depletion is increasingly used to treat high-risk hematologic malignancies. Following T-replete CBT, naïve CB T cells undergo rapid peripheral expansion with memory-effector differentiation. Emerging data suggest that unrelated CBT, particularly in the context of HLA mismatch and a T-replete graft, may reduce leukemic relapse. To study the role of CB T cells in mediating graft-versus-tumor responses and dissect the underlying immune mechanisms for this, we compared the ability of HLA-mismatched CB and adult peripheral blood (PB) T cells to eliminate Epstein-Barr virus (EBV)-driven human B-cell lymphoma in a xenogeneic NOD/SCID/IL2rg(null) mouse model. CB T cells mediated enhanced tumor rejection compared with equal numbers of PB T cells, leading to improved survival in the CB group (P cells that were autologous vs allogeneic to the lymphoma demonstrated that this antitumor effect was mediated by alloreactive rather than EBV-specific T cells. Analysis of tumor-infiltrating lymphocytes demonstrated that CB T cells mediated this enhanced antitumor effect by rapid infiltration of the tumor with CCR7(+)CD8(+) T cells and prompt induction of cytotoxic CD8(+) and CD4(+) T-helper (Th1) T cells in the tumor microenvironment. In contrast, in the PB group, this antilymphoma effect is impaired because of delayed tumoral infiltration of PB T cells and a relative bias toward suppressive Th2 and T-regulatory cells. Our data suggest that, despite being naturally programmed toward tolerance, reconstituting T cells after unrelated T-replete CBT may provide superior Tc1-Th1 antitumor effects against high-risk hematologic malignancies.

  20. Subchronic peripheral neuregulin-1 increases ventral hippocampal neurogenesis and induces antidepressant-like effects.

    Ian Mahar

    Full Text Available BACKGROUND: Adult hippocampal neurogenesis has been implicated in the mechanism of antidepressant action, and neurotrophic factors can mediate the neurogenic changes underlying these effects. The neurotrophic factor neuregulin-1 (NRG1 is involved in many aspects of brain development, from cell fate determination to neuronal maturation. However, nothing is known about the influence of NRG1 on neurodevelopmental processes occurring in the mature hippocampus. METHODS: Adult male mice were given subcutaneous NRG1 or saline to assess dentate gyrus proliferation and neurogenesis, as well as cell fate determination. Mice also underwent behavioral testing. Expression of ErbB3 and ErbB4 NRG1 receptors in newborn dentate gyrus cells was assessed at various time points between birth and maturity. The phenotype of ErbB-expressing progenitor cells was also characterized with cell type-specific markers. RESULTS: The current study shows that subchronic peripheral NRG1β administration selectively increased cell proliferation (by 71% and neurogenesis (by 50% in the caudal dentate gyrus within the ventral hippocampus. This pro-proliferative effect did not alter neuronal fate, and may have been mediated by ErbB3 receptors, which were expressed by newborn dentate gyrus cells from cell division to maturity and colocalized with SOX2 in the subgranular zone. Furthermore, four weeks after cessation of subchronic treatment, animals displayed robust antidepressant-like behavior in the absence of changes in locomotor activity, whereas acute treatment did not produce antidepressant effects. CONCLUSIONS: These results show that neuregulin-1β has pro-proliferative, neurogenic and antidepressant properties, further highlight the importance of peripheral neurotrophic factors in neurogenesis and mood, and support the role of hippocampal neurogenesis in mediating antidepressant effects.

  1. Riluzole exerts central and peripheral modulating effects in amyotrophic lateral sclerosis.

    Vucic, Steve; Lin, Cindy Shin-Yi; Cheah, Benjamin C; Murray, Jenna; Menon, Parvathi; Krishnan, Arun V; Kiernan, Matthew C

    2013-05-01

    Riluzole, a benzothiazole derivative, has been shown to be effective in prolonging survival in amyotrophic lateral sclerosis. The mechanisms by which riluzole exerts neuroprotective effects in amyotrophic lateral sclerosis remains to be fully elucidated, although inhibition of glutamatergic transmission and modulation of Na+ channel function have been proposed. In an attempt to determine the mechanisms by which riluzole exerts neuroprotective effects, in particular to dissect the relative contributions of inhibition of glutamatergic transmission and Na+ channel modulation, the present study utilized a combination of cortical and peripheral axonal excitability approaches to monitor changes in excitability and function in patients with amyotrophic lateral sclerosis. Cortical assessment was undertaken by utilising the threshold tracking transcranial magnetic stimulation (TMS) technique and combined with peripheral axonal excitability studies in 25 patients with amyotrophic lateral sclerosis. Studies were performed at baseline and repeated when patients were receiving riluzole 100 mg/day. At the time of second testing all patients were tolerating the medication well. Motor evoked potential and compound muscle action potential responses were recorded over the abductor pollicis brevis muscle. At baseline, features of cortical hyperexcitability were evident in patients with amyotrophic lateral sclerosis, indicated by marked reduction in short interval intracortical inhibition (P amyotrophic lateral sclerosis had significant increases in depolarizing threshold electrotonus [amyotrophic lateral sclerosisbaseline TEd (90-100 ms) 49.1 ± 1.8%; controlsTEd (90-100 ms) 45.2 ± 0.6%, P amyotrophic lateral sclerosisbaseline 30.1 ± 2.3%; control subjects 23.4 ± 1.0%, P amyotrophic lateral sclerosisbaseline 30.1 ± 2.3%; amyotrophic lateral sclerosisON riluzole 27.3 ± 2.3%, P amyotrophic lateral sclerosisbaseline 98.7 ± 10.7%; amyotrophic lateral sclerosisON riluzole 67.8 ± 9

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

    Afshar Jafari

    2009-09-01

    Full Text Available

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

  3. 自控硬膜外镇痛在骨科患者术后中的应用效果观察%Clinical effect of patient-controlled epidural analgesics on patients after orthopedic surgery

    刘丽兰

    2012-01-01

    目的 观察自控硬膜外镇痛(patient-controlled epidural analgesics,PCEA)对骨科患者术后镇痛和镇静的效果.方法 选择280例手术后采用PCEA方法的骨科患者,采用视觉模拟评分法(visual analogue scales,VAS)和Ramsay评分法观察并记录患者术后4、8、12、24、48 h疼痛及镇静情况和不良反应发生情况.结果 280例患者疼痛评分为(1.5±0.5)分;镇静程度为(2.5±0.5)分.44例患者发生恶心和呕吐,142例患者出现尿潴留,无1例发生呼吸抑制等严重不良反应.结论 对骨科术后的患者采用PCEA,镇痛和镇静效果满意,术后12 h后无不良反应的发生,值得临床推广应用.%Objective To investigate the clinical effect of patient-controlled epidural analgesics on patients after orthopedic surgery. Methods 280 patients admitted in our department accepted the PCEA after surgery. We observed the clinical effect including side effect of the medication, and gathered the data in hours 4, 8, 12, 24 and 48 after surgeries. Results The average score was (1.5 ± 0.5) according to the visual analogue scales (VAS). 44 of them were affected with nausea and vomiting and 142 with urinary retention. No severe side effect like respiratory depression was observed. Conclusion Patient-controlled epidural analgesics for the patients after orthopedic surgery can achieve satisfactory effect with minor side effects, which is worth spreading clinically.

  4. 吴茱萸不同炮制方法对抗炎镇痛作用的影响研究%Study on Analgesic and Anti - Inflammatory Effects of Different Kinds of Evodia Rutaecarpa (Juss.)Benth.

    杨磊; 黄开颜; 陈兴; 杨晖; 李康; 张志国

    2013-01-01

    目的 观察吴茱萸不同炮制品的抗炎镇痛作用.方法 采用小鼠热板法和扭体法,观察吴茱萸不同炮制品的镇痛作用;采用耳肿法观察吴茱萸不同炮制品的抗炎作用.结果 吴茱萸不同炮制品能明显提高热板和扭体试验小鼠的痛阈值,其中以砂烫盐炙组作用较强;对二甲苯所致的小鼠耳廓肿胀有明显的抑制作用,其中以砂烫组作用较强.结论 吴茱萸不同炮制品均有显著的抗炎、镇痛作用,其中以砂烫组和砂烫盐炙组作用较强.%Objective To study analgesic and anti - inflammatory effects of different processed products of Evodia rutaecarpa (Juss. ) Benth. Methods The analgesic effect was tested by hot plate method and writhing body method in mice. The anti - inflammatory effect was tested by ear swollen method in mice. Results For the pain caused by hot plate method and writhing body method, the different processed products of Evodia rutaecarpa{Juss. ) Benth. have obviously increased threshold of pain in mice. Among these products, the group of stir - baked in sand with processed salty water shows more intensive effect,which has substantially inhibiting effects on mice s ear swelling caused by dimethylbenzene. The stir - baked in sand is more intensive. Conclusion Different processed products of Evodia rutaecarpa (Juss. ) Benth. have marked analgesic and anti - inflammatory effects, of which the stir - baked in sand one and stir - baked in sand wTith processed salty water one are more intensive.

  5. 复方烧伤膏收敛止痛的疗效观察%Analgesic effect and astringency of Compound burn ointment

    2001-01-01

    @@Background:Burns are injuries caused by attaching factors such as high-temperature,strong acids,and bases etc.Areola and blister or vesticles appear at site in mild cases.Charring,serious toxic heat,consumption of yin fluid,fever,dizzy,thirst,constipation,and oliguria appear in severe cases.Compound burn ointment was developed according to modern traditional Chineses medicine principles and pathological changes of burned skin,which consisted of Sanguisorba root 120 g,Earth worm 120 g,Fibraurea stem 120 g,Dandelion herb 150 g,Dried rehmannia root 150 g,Huanglian 120 g,Yuanhu 150 g,Beeswax 120 g,Borneol 30 g,Oliva 2000 g. Objective:To investigate the analgesic and astringency of compound burn ointment. Unit: Affiliated Central Hospital of Shengyang Medical College.

  6. Analgesic Activity of Tramadol and Buprenorphine after Voluntary Ingestion by Rats (Rattus norvegicus).

    Taylor, Bryan F; Ramirez, Harvey E; Battles, August H; Andrutis, Karl A; Neubert, John K

    2016-01-01

    Effective pain management for rats and mice is crucial due to the continuing increase in the use of these species in biomedical research. Here we used a recently validated operant orofacial pain assay to determine dose-response curves for buprenorphine and tramadol when mixed in nut paste and administered to male and female rats. Statistically significant analgesic doses of tramadol in nut paste included doses of 20, 30, and 40 mg/kg for female rats but only 40 mg/kg for male rats. For male rats receiving buprenorphine mixed in nut paste, a significant analgesic response was observed at 0.5 and 0.6 mg/kg. None of the doses tested produced a significant analgesic response in female rats. Our results indicate that at the doses tested, tramadol and buprenorphine produced an analgesic response in male rats. In female rats, tramadol shows a higher analgesic effect than buprenorphine. The analgesic effects observed 60 min after administration of the statistically significant oral doses of both drugs were similar to the analgesic effects of 0.03 mg/kg subcutaneous buprenorphine 30 min after administration. The method of voluntary ingestion could be effective, is easy to use, and would minimize stress to the rats during the immediate postoperative period.

  7. 小剂量曲马多用于膝关节镜术后镇痛效果比较%Analgesic effects of low-dose tramadol after arthroscopic knee surgery

    袁红斌; 李科; 王新华; 刘虎

    2001-01-01

    Objective To investigate analgesic effect of intra-articular low-dose tramadol after arthroscopic knee surgery.Methods 60 patients undergoing arthroscopic knee surgery under lumbar anesthesia were randomly divided into intra-articular injection of tramadol(TJ group),mulscle injection of tramadol(TM)and saline control group.Vision analog scoring was conducted under extension of knee joint 8h and 24h after drugs administration.Follow-up was done to observe unwanted effects 48h after surgery.Results Score of TJ group was significantly lower than those of other groups(P<0.05).No unwanted effects were found.Conclusion Intra-articular tramadol in low-dose could relieve operative pain.

  8. Experimental observation on the analgesic effect of NT on frog rectus abdominis N2 -receptor%中华眼镜蛇神经毒素的活性研究

    高红瑾; 许云禄; 王少明; 陈燕

    2014-01-01

    Objective To study the analgesic effect and the drug-receptor interactions with frog rectus abdominis N2-receptor of the neurotoxin from Naja atra venom( NT). Methods Three model of pain( tail electric stimulation-vocali-zation test ,the hot-plate test ,and writhing responses in mice)were used. The effects of NT on acetylcholine-induced i-solated frog rectus abdoninis were observed. Results NT could dose-dependently raise the pain threshold in hot-plate test in mice and inhibit the writhing reaction induce by acetic acid in mice . The analgesic effect of NT effect at 2 h and peaked at 5 h. NT produced a concentration-dependent parallel shift to the right of dose-response curve of acetylcholine applied exogenously with no change in the maximal asymptotic response. Conclusion NT had a better analgesic effect on the pain due to hot- plate ,acetic acid and electric stimulation. NT was determined as the competitive antagonists of N2 -AChR.%目的:研究中华眼镜蛇神经毒素( NT)的镇痛活性和对离体蛙腹直肌N2-AChR的拮抗作用。方法采用三种模型(电刺激-嘶叫法,热板法,醋酸扭体法)观察NT的镇痛活性,并观察NT对ACh所致蛙离体腹直肌收缩的影响。结果 NT能提高电刺激-嘶叫法,热板法的痛阈,抑制醋酸引起的扭体次数。NT镇痛具有剂量-效应关系,给药后2 h起效,5 h达峰。NT能使ACh引起的蛙腹直肌收缩的量效曲线平行右移。结论 NT对三种致痛模型均有确切的镇痛活性,NT对N2-AChR的拮抗作用为竞争性拮抗。

  9. Dispersion of Soluble Matters in Newton—dipolar Stratified fluid and Effects of Peripheral Layer

    ZhangJiLU; ShoushengDONG; 等

    1998-01-01

    In the paper,the dispersion law and the concentration distributions of soluble matters in ewton-dipolar fluids flowing through a circular tube have been investigated.Main results are:(1) for the dependence of M on λ(or H),the completely opposite trends are obtained in the cases with and without the peripheral layer.(2) effects of δ on M have the minimum values near δ=0.85-0.9,(3) various models such as couple stress,micropolar,dipolar,Newton-newtonican,Newton-couple stress and Newton-micropolar model etc.are all special cases of Newton-dipolar fluid(where Mz=0).When Mz≠0,however,there are evident differences between the Newton-dipolar fluid and the Newton-couple stress fluid,the Newton-micropoloar fluid.

  10. Study on the effects of cefotaxime on intracellular Ca2+ in human peripheral lymphocytes by fluoremetry

    Dan Dan Wang; Hai Yan Wang; Ye Hong Zhou; Chun Gui Zhao; Chuan Dong; Shao Min Shuang

    2007-01-01

    Characteristic of Fura-2-Ca2+ interaction was studied based on the fluorescence technique. The apparent dissociation constants(Kd) of the Fura-2-Ca2+ complex were determined at different temperature. The effect of cefotaxime (CEFA) on intracellular Ca2+concentration ([Ca2+]i) was discussed by using a ratiometric fluorescence dye Fura-2 as a probe. The basal [Ca2+]i in resting human peripheral lymphocytes was 100 ± 7 nmol/L but after treatment with cefotaxime, the changes of [Ca2+]i were observed in different conditions. In the concentration range of 1-30 μmol/L of cefotaxime [Ca2+]i increased, as a result of releasing intracellular Ca2+ stores. Higher concentration of cefotaxime (50-500 μmol/L) stimulated to decrease of [Ca2+]i.

  11. Phytochemical screening and studies of analgesic potential of Moringa oleifera Lam. stem bark extract on experimental animal model

    Shumaia Parvin

    2014-11-01

    Full Text Available The work has been done for the phytochemical investigation and study of analgesic activity of Moringa oleifera Lam. ethanolic stem bark extract using Acetic Acid Induced Writhing method. The effect of extract was tested for qualitative chemical analysis which reveals the presence of alkaloid, glycosides, flavonoids, tannins, saponin, carbohydrate etc. For peripheral analgesic effect acetic acid induced writhing test was used and for this stem bark extract was administered intraperitoneally at doses of 250 mg/kg and 500 mg/kg of body weight to young Swiss-albino mice. Both doses of the extract significantly inhibited writhing response induced by acetic acid in a dose dependent manner which is comparable to the positive control drug Diclofenac Na. These two different doses were found to exhibit 13.22% and 28.94% writhing inhibitory response respectively where the Diclofenac Na inhibited about 42.15% of writhes at a dose of 100mg/kg of body weight. The obtained results provide promising baseline information for the potential use of these crude extract in the treatment of pain.

  12. 九节茶肿痛宁乳膏镇痛抗炎及皮肤刺激和过敏性作用%Studies on the anti-inflammatory and analgesic effects and the safety of Sarcandra Zhongtongning cream

    欧余航; 李杰; 陈强

    2013-01-01

    目的:对九节茶肿痛宁乳膏的镇痛抗炎作用进行了研究,并对其皮肤的刺激性和致敏性进行了初步评价.方法:以醋酸扭体法和二甲苯致耳肿胀实验研究九节茶肿痛宁乳膏的镇痛抗炎作用;通过对家兔皮肤刺激性实验、豚鼠皮肤过敏性实验对乳膏的安全性进行初步研究.结果:九节茶肿痛宁乳膏对二甲苯所致小鼠耳郭炎症和醋酸所致的腹痛有显著的抑制作用;对家兔皮肤无刺激性,对豚鼠也不引起过敏反应.结论:九节茶肿痛宁乳膏具有明显的镇痛抗炎作用,是一种安全性高的外用产品.%OBJECTIVE To study the anti-inflammatory and analgesic effects of Sarcandra Zhongtongning cream and to evaluate preliminarily its irritation and allergic reaction on animal skin.METHODS The anti-inflammatory and analgesic effects of Sarcandra Zhongtongning cream were researched through xylene-induced auricle swelling experiment and acetic acid writhing method in mice.The experiment of irritation on the skin was studied in rabbits and the experiment of allergic reaction was studied on the skin of guinea pig to evaluate the preliminary safety of the creams.RESULTS Sarcandra Zhongtongning creams possessed marked inhibitory effect on auricular inflammation caused by xylene and abdominal pain induced by acetic acid in mice.The results showed that there was no irritation on the skin of rabbits and no allergic reaction on the skin of guinea pigs.CONCLUSION Sarcandra Zhongtongning cream has obvious anti-inflammatory and analgesic effects.It is a kind of external product with high safety.

  13. 河豚毒素与吗啡联合用药对吗啡依赖性与镇痛耐受作用的影响%EFFECTS OF TETRODOTOXIN COMBINED WITH MORPHINE ON MORPHINE'S DEPENDENCE AND ANALGESIC TOLERANCE

    徐开俊; 周娟; 翟清波; 赵继红

    2012-01-01

    Objective: To study the effect of tetrodotoxin ( TTX) combined with morphine on the dependence and analgesic tolerance acting of morphine. Methods-. The mouse model of morphine dependency and hot plate experiment were used in this research to investigate the effects of morphine alone< morphine 2. 5 ml · kg-1) and morphine combined with TTX ( morphine 2. 5 mg · kg + TTX 0. 5 μg· kg-1, morphine 2. 5 mg · kg-1 + TTX 1. 0 μg· kg-1) on the withdrawal symptoms induced by naloxone and the analgesic tolerance of morphine. Results-. Administration of morphine combined with TTX could inhibit the weight loose of mice, significantly inhibit the jumping effect after the withdrawal experiment induced by naloxone and reduce the increase of the response latency in the hot - plate experiment. Conclusion-. Administration of morphine combined with TTX can inhibit the effect of dependence and analgesic tolerance acting of morphine.%目的:研究河豚毒素(tetrodotoxin,TTX)与吗啡联合使用对吗啡依赖性及镇痛耐受作用的影响.方法:采用吗啡依赖性小鼠模型及热板实验,评价单独使用吗啡(2.5 ml·kg-1)以及联合给药(吗啡2.5 mg·kg-1+TTX0.5μg·kg-1、吗啡2.5 mg·kg-1TTX1.0μg·kg-1)对纳洛酮催促戒断症状及镇痛耐受性的影响.结果:联合用药可以抑制吗啡依赖性小鼠戒断后体重的丢失,明显抑制吗啡依赖小鼠纳洛酮催促后的跳跃反应,抑制小鼠热板实验的潜伏期时间的增加.结论:TTX与吗啡联合用药可以抑制吗啡的依赖性与镇痛耐受作用的产生.

  14. 瓜子金提取物及不同部位的抗炎镇痛作用研究%Experimental Study on Analgesic and Anti-inflammatory Effects of the Methanol Extract and its Fractions from Polygalajaponica

    王洪兰; 李祥; 陈建伟

    2011-01-01

    Objective To evaluate the analgesic and anti-inflammatory effects of the methanol extract and its different fractions from Polygala japonica. Methods The methanol extract from Polygala japonica and its fractions (petroleum ether fraction, ethyl acetate fraction, n-butanol fraction and water residure fraction) were obtained by solvent partition of its total extract. Analgesic effect was observed by acetic acid-induced writhing response in mice, and anti-inflammatory effects were investigated on xylene-induced ear swelling in mice, acetic acid-induced peritoneal capillary permeability in mice, carrageenan-induced paw edema in mice. Results The methanol extract including ethyl acetate fraction and n-butanol fraction could inhibit twisting response of mice, and could reduce pedal swelling and aurical swelling obviously. Conclusion In the same dose, the methanol extract shows analgesic effect obviously, while anti-inflammatory activities might be mainly ascribable to ethyl acetate fraction and n-butanol fraction.%目的 探讨瓜子金提取物及其不同部位的抗炎、镇痛活性.方法 采用醋酸扭体法进行镇痛实验,采用二甲苯致小鼠耳肿胀、醋酸致小鼠腹腔通透性增加、角叉菜胶致小鼠足趾肿胀实验进行抗炎实验,对瓜子金的甲醇提取物及其各个萃取部位进行镇痛和抗炎实验.结果 瓜子金甲醇提取物及乙酸乙酯部位和正丁醇部位对醋酸所致小鼠扭体反应有较好的抑制作用,可以显著抑制二甲苯所致的小鼠耳廓肿胀和角叉菜胶所致的小鼠足趾肿胀.结论 在相同剂量下,瓜子金的甲醇提取物显示出较好的镇痛活性,乙酸乙酯部位和正丁醇部位相对具有较好的抗炎活性.

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

    Lee Jung

    2012-08-01

    Full Text Available Abstract Background A common side effect of oxaliplatin is peripheral neurotoxicity. Oxidative stress to dorsal root ganglion (DRG may be one of important pathogenic mechanisms. Green tea contains four polyphenol catechins, which are known to be potent antioxidants. The present work is aimed to determine whether green tea extracts have neuroproective or palliative effects on neurotoxicity symptoms induced by oxaliplatin. Methods We conducted behavioral tests including sensory and thermal thresholds, an electrophysiological study, and TUNEL staining to assess neurotoxicity during the experimental period using animal models. Results A total of 14 adult rats were randomly allocated into two groups. Oxaliplatin (4 mg/kg with or without green tea (300 mg/kg orally once daily was administered intraperitoneally twice per week for 6 weeks. At 4 and 6 weeks after oxaliplatin administration, sensory threshold values were significantly decreased and at 6 weeks after oxaliplatin administration, thermal threshold values were significantly increased in oxaliplatin-treated rats compared with those in rat treated with oxaliplatin and green tea extracts. The electrophysiological assessment, including sensory nerve conduction and H-reflex-related sensory nerve conduction velocity, revealed no significant changes in the two groups. TUNEL staining showed no significant difference in the number of apoptotic-featured cells between the two experimental groups in the DRG or peripheral nerves, but the number of apoptotic-featured cells in DRG was higher than that in sciatic nerves within each group. Conclusions Green tea extracts may be a useful adjuvant to alleviate sensory symptoms after oxaliplatin administration, such as allodynia, but did not prevent morphometric or electrophysiological alterations induced by oxaliplatin.

  16. Antiinflammatory, analgesic and antipyretic activities of Mimusops elengi Linn

    Purnima A

    2010-01-01

    Full Text Available 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 pyrexia in rats. The ethanol extract of Mimusops elengi (200 mg/kg, p.o significantly inhibited the carrageenan-induced paw oedema at 3rd and 4th h and in cotton pellet model it reduced the transudative weight and little extent of granuloma weight. In analgesic models the ethanol extract of Mimusops elengi decreases the acetic acid-induced writhing and it also reduces the rectal temperature in Brewer′s yeast induced pyrexia. However, Mimusops elengi did not increase the latency time in the hot plate test. These results show that ethanol extract of Mimusops elengi has an antiinflammatory, analgesic and antipyretic activity.

  17. 芬太尼联合异丙酚用于人工流产的镇痛效果%Analgesic effect of fentanyl combined with propofol in the abortion

    朱建丽; 叶咏菊; 蓝关翠

    2014-01-01

    目的:评价芬太尼与芬太尼联合异丙酚用于人工流产时的镇痛效果及安全性。方法2010-08-2013-08我院门诊要求人工流产者366例,其中术中用芬太尼镇痛者167例,芬太尼100μg+5%葡萄糖4 mL (1 min ), iv;用芬太尼+异丙酚镇痛者199例,首先给予芬太尼100μg,再给予异丙酚2 mg· kg-1, ivgtt。比较2组患者术中疼痛分级、阴道出血量、术后恶心呕吐及人工流产综合征的发生率等。结果芬太尼+异丙酚组患者术中镇痛效果明显好于单用芬太尼组( P<0.05);2组患者术中出血量,术后恶心呕吐及人工流产综合征发生率差别无统计学意义( P>0.05)。结论与单用芬太尼相比,芬太尼+异丙酚镇痛效果明显,且不增加药物不良反应。%Objective To investigate the analgesic effects of fentanyl combined with propofol compared with fentanyl alone in the abortion.Methods A total of 366 abortion patients were recruited from Aug 2010 to Aug 2013 in the outpatients department of our hospital.One hundred and sixty-seven patients were given fentanyl combined with propofol and the other 199 cases were given fentanyl only.The pain score , vaginal bleeding , the incidence of postoperative nausea vomiting and abortion syndrome were compared between the two groups.Results The analge-sic effect was better in combination group compared with fentanyl group ( P0.05 ).Conclusion Fentanyl combined with propofol can significantly improve the analge-sic effects compared with fentanyl only in the treatment of abortion , and without increase in the risk of nausea vomiting and abortion syndrome.

  18. Analysis of analgesic effect and safety of meloxicam after orthopedic surgery%美洛昔康在骨科术后的镇痛疗效及其安全性分析

    周力文

    2015-01-01

    目的:探讨美洛昔康在骨科术后的镇痛效果,评价其安全性。方法136例骨科手术患者为研究对象, A组(62例)大型手术, B组(42例)中型手术, C组(32例)小型手术,三组术后均予以美洛昔康镇痛,视觉模拟评分(VAS)评价镇痛效果,监测用药前后血常规、肝功能,统计不良反应事件。结果三组用药后VAS评分均明显好于用药前,差异具有统计学意义(P0.05),无严重不良反应。结论美洛昔康在中小型骨科手术中的术后镇痛效果良好,安全性佳,值得临床推广应用。%Objective To investigate analgesic effect of meloxicam after orthopedic surgery, and to evaluate its safety.Methods There were 136 patients under orthopedic surgery as study subjects. Group A (62 cases) received major surgery, group B (42 cases) received medium surgery, and group C (32 cases) received minor surgery. All three groups received meloxicam in postoperative analgesia, and the analgesic effects were evaluated by visual analogue scale (VAS). Monitoring was made on blood routine examination and liver function after treatment, and adverse reactions were summarized.Results All three groups had much better VAS scores after treatment than those before treatment, and their difference had statistical significance (P0.05). No severe adverse reactions were found.Conclusion Meloxicam provides good analgesic effect and safety after medium surgery and minor surgery, and it is worthy of clinical promotion and application.

  19. Study on analgesic and anti -inflammation effects of the compounds isolated from Corm of Crocus Alatavicus with ethanol%白番红花球茎醇提取物的镇痛抗炎作用研究

    高红艳; 杨元华; 刘静; 程媛媛; 韩汝春; 杨晓绒

    2016-01-01

    目的:探讨白番红花球茎醇提取物的镇痛抗炎作用。方法:采用小鼠醋酸扭体法观察白番红花球茎醇提取物的镇痛作用;采用二甲苯致小鼠耳廓肿胀法观察白番红花球茎醇提取物的抗炎作用。结果:白番红花球茎醇提取物高、中、低剂量组能显著减少醋酸所致小鼠的扭体次数,与空白对照组比较,差异均有统计学意义(P <0.05);白番红花球茎醇提取物高剂量组能显著抑制二甲苯所致的小鼠耳廓肿胀度,与空白对照组比较,差异有统计学意义(P <0.05)。结论:白番红花球茎醇提取物有明显的镇痛作用,高剂量有一定的抗炎作用。%Objective To investigate analgesic activities and anti -inflammatory of the compounds isolated from Corm of Crocus Alatavicus with ethanol.Methods Analgesic effects of Corm of Crocus Alatavicus were investigated by acetic acid writhing test in mice;Anti -inflammatory effects were investigated by xylene -induced auricle swelling in mice.Results The results showed that the high, middle and low dosages of Corm of Crocus Alatavicus could markedly reduce the twisting number compared with blank control group, they showed a strong difference (P <0.05);and the high dosages of Corm of Crocus Alatavicus could relieve swollen auricle of mice induced by xylene,the result showed a strong difference compared with blank control group (P <0.05).Conclusion The results showed that Corm of Crocus Alatavicus have remarkable analgesic and high dosages of Corm of Crocus Alatavicus have anti -inflammato-ry effects by different administrations.

  20. 三黄皮炎膏镇痛抗炎作用的实验研究%Experimental Study on Analgesic and Anti-inflammatory Effects of Sanhuang Piyan Cream

    杨延林

    2013-01-01

    目的:观察三黄皮炎膏的镇痛抗炎作用.方法:采用热板试验观察三黄皮炎膏对小鼠痛阈提高百分率的影响,采用二甲苯耳肿胀试验观察三黄皮炎膏对小鼠耳肿胀率的影响.结果:三黄皮炎膏可以显著提高实验小鼠的热痛阈,显著降低实验小鼠的耳肿胀率,与空白组、赋形剂组、阳性药组比较,差异均有统计学意义(P<0.05).结论:三黄皮炎膏具有较好的镇痛抗炎作用.%Objective:To observe the analgesic and anti-inflammatory effects of Sanhuang Piyan Cream.Methods:The hot plate test was used to observe the effects of Sanhuang Piyan Cream to improve the percentage on the pain threshold in mice,the xyleneinduced mouse ear edema test was used to observe the effects of Sanhuang Piyan Cream on the mice ear swelling rate.Results:Sanhuang Piyan Cream could significantly improve the thermal pain threshold in mice,and significantly reduce the mice ear swelling rate,the difference was statistically significant (P < 0.05) compared with the blank group,vehicle group,positive drug group.Conclusion:Sanhuang Piyan Cream has good analgesic and anti-inflammatory effects.

  1. Analgesic Effect of Flurbiprofen Axetil and Transdermal Fentanyl on Refractory Cancer Pain%氟比洛芬酯联合芬太尼透皮贴剂治疗难治性癌痛

    欧武陵; 姚国庆; 高建飞; 章必成

    2012-01-01

    Objective: To evaluate the analgesic effect of flurbiprofen axetil and transdermal fentanyl on refractory cancer pain. Methods: One hundred patients with refractory cancer pain were divided into three groups randomly. Thirty-three patients received only flurbiprofen axetil, 33 patients received only transdermal fentanyl, and the other 34 patients received the combined therapy. The analgesic effects and side effects were observed respectively. Results: The pain control rates of flurbiprofen axetil group, transdermal fentanyl group and the combined therapy group were 72.7%, 69. 7%, and 91. 2%, respectively. No obvious side effects were found in all the three groups. Conclusion: Flurbiprofen axetil combined with transdermal fentanyl is an optimized treatment for refractory cancer pain.%目的:评价氟比洛芬酯联合芬太尼透皮贴剂治疗难治性癌痛的疗效.方法:100例难治性癌痛患者随机分为3组,分别为氟比洛芬酯组(33例)、芬太尼组(33例)和联合用药组(34组),观察止痛效果和毒副反应.结果:氟比洛芬酯、芬太尼组和联合用药组的癌痛缓解率分别为72.7%、69.7%和91.2%,均无明显的毒副反应.结论:氟比洛芬酯联合芬太尼透皮贴剂是治疗难治性癌痛的优选方案.

  2. ANALGESIC ACTIVITY OF AQUEOUS EXTRACT OF CURCUMA AMADA (MANGO - GINGER IN MALE ALBINO WISTAR RATS

    Kumari Bai

    2015-09-01

    Full Text Available BACKGROUND: Mango ginger ( Curcuma amada Roxb. has morphological resemblance with ginger, but imparts mango flavour. According to Ayurveda and Unani medicinal systems , the biological activities include antioxidant, antibacterial, antifungal, anti - inflammatory, antiallergic, CNS depressant and analgesic activity. Hence curcuma amada aqueous extract for analgesic activity was evaluated in pain animal models. Pain is a most common complaint of many medical conditions, and pain control is one of t he most important therapeutic priorities. Curcuma Amada suppresses the inflammatory mediators associated with pain. However there is no scientific data suggestive of its analgesic activity. Hence this study was carried out to evaluate its role in central a nd peripheral models of pain. OBJECTIVE: To Evaluate rhizomes of Curcuma Amada for analgesic activity in male albino wistar rats . MATERIALS AND METHODS: Albino rats, the proven models for analgesic studies. They were obtained from the animal house of DR.B. R. Ambedkar Medical College. Animals were maintained as per CPCSEA guidelines . The aqueous extract of curcuma amada was used.4x2 groups of 6 Rats were used to ensure that results obtained were statistically significant using ANOVA test. Analgesic activity was assessed with the help of following screening methods . Acetic Acid Writhing Method using Acetic Acid . Tail Flick Method using the Analgesiometer . Tail Immersion Method using Hot Water (55 0 C . Hot Plate method using Hot Plate . RESULT S: Aqueous extract of curcuma amada significantly suppressed the 1% acetic acid induced writhing response in rats when compared to control group (Gum acacia. In Tail flick test and Hot plate test Curcuma Amada increases the latency period of pain (reaction time. In Tail im mersion test the test drug significantly (P < 0.001 reduces pain at 30 min when compared to control group at 60 min of oral administration. CONCLUSION : The present findings indicate that

  3. Study the Anti-inflammatory and Analgesic Effects of Piroxicam Microemulsions on Mice%吡罗昔康新制剂微乳的药效学研究

    刘娜; 杨保仲; 王颖莉; 葛曙光

    2013-01-01

    Objective:To prepare piroxicam miroemulsion and study its anti-inflammatory and analgesic effects,observe the continuous medication on skin morphology,and compare with piroxiam gel. Method:The microemulsion was prepared with the system contained of Lauroglycol FCC as oil phase,Labrasol and Cremophor EL as surfactants,Transcutol P as consurfactants,piroxicam,water 1%dichlofenac sodium gel was used as positive control,xylene and carrageenan were used to induce ear edema in mice and pedal swelling in rats respectively in order to study anti-inflammatory effect of Piroxiam microemulsion. The hot-plate test and writhing test was adopted to study the analgesic effect,then compared with Piroxiam gel. Result:Middle dose and high dose Piroxiam miroemulsion was equal or superior to positive control in anti-inflammatory and analgesic effect. Compared with piroxiam gel, it had longer action time and more stable effects. In addition,there was no irritation to the skin. Conclusion:Piroxiam miroemulsion has significant anti-inflammatory and analgesic effects,it is expected to become a new formulation.%  目的:制备吡罗昔康微乳新剂型,对其抗炎、镇痛作用进行初步药效学研究,观察连续用药对皮肤组织形态学的改变,并与凝胶制剂进行比较。方法:采用油相Lauroglycol FCC,表面活性剂Labrasol、Cremophor EL,助表面活性剂Transcutol P、吡罗昔康及水制备吡罗昔康微乳,1%的双氯芬酸钠凝胶剂作为阳性对照药,采用二甲苯诱导小鼠耳廓肿胀,卡拉胶诱发大鼠足跖肿胀,痛阈提高率和醋酸致小鼠扭体实验,对吡罗昔康微乳的抗炎镇痛作用进行初步探讨并与市售的吡罗昔康凝胶进行比较。结果:吡罗昔康微乳具有抗炎镇痛作用,中、低剂量的吡罗昔康微乳与阳性对照组比较均显示相近或更强的抗炎镇痛作用,与吡罗昔康凝胶组比较,作用强、时间长、效果平稳,且对皮肤无刺激性。结论:吡罗昔康

  4. [Analgesic abuse and psychiatric comorbidity in headache patients].

    Radat, F; Irachabal, S; Swendsen, J; Henry, P

    2002-01-01

    Headache patients frequently overuse analgesic medications: 20% of the patients from headache centers is concerned by this problem, which has been estimated to occur in four percent of the community migrainers. Frequent use of various types of headache medication may paradoxically cause an increase in headache attack frequency as well as their chronicisation due to potentially complex mechanisms of sensitization. Patients will enter into a self- perpetuating cycle of daily headaches and use of symptomatic medications which can lead to addiction and to social and occupational impairement. Indeed, many patients will experience pharmacological tolerance and dependence but also by some kind of craving. International Headache Society qualify these patients as abusers referring mostly to the amount of substance ingested. Hence patients are labelled analgesic abusers . However, as many of these analgesic medications contained psychotropic substances (i.e. caffeine, codeine.), these patients may fulfill DSM IV criteria of dependance. Nevertheless, the dependance criteria should be adapted to chronic pain patients. Indeed, if pharmacological dependence and tolerance criteria are easy to apply in such patients, it is not the case for the criteria a great deal of time spent to obtain substances, to use substances or to recover from substances effects . As analgesic medications are legally obtained from medical practitioners, drug seeking behaviours are mostly: obtaining medications from multiple providers, repeating episodes of prescription loss and multiplying requests for early refills. Moreover the detrimental effects of analgesic abuse on psychosocial functioning is likely to be related to pain rather than to medication overuse. Finally the best indicator of addictive behaviors in such patients, is the loss of control over the use of analgesic medication despite the adverse consequences over pain. Comorbidity with addiction to other substances has never been specifically

  5. Effects of Propolis on Peripheral White Cells, Antioxidative Activity and Tumor Growth in Irradiated mice

    Takashi Nakamura; Yuka Itokawa; Kwang-Ho Cho; Jung-Sook Choi; Ikukatsu Suzuki; Toshihoro Miura; Torao Ishida; Yeunhwa Gu

    2006-01-01

    The effect of continuous water-soluble propolis administration on radioactivity-induced reduction of hemocytes, and the antioxidant and antitumor effects were investigated. Following a 1-week adjustment period, water-soluble propolis was administered intraperitoneally to male ICR mice at a dose of 100mg/kg every other day for 2 weeks. Following administration, 2 Gy whole-body irradiation was performed and the counts of leukocytes, lymphocytes, and granulocytes and monocytes in the peripheral blood were determined 1, 3, 7, 15 and 30 days after irradiation. In the second experiment, water-soluble propolis was similarly administered to the mice for 2 weeks after a 1-week adjustment period, and 2 Gy whole-body irradiation was performed. The antioxidant effects in hemocytes were then investigated using 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH), a radical generator. In the third experiment, 1×l06 Sarcoma-180 cells were inoculated into the right thigh of mice, which were divided into four groups: control, water-soluble propolis-treated, 6 Gy irradiated and water-soluble propolis-treated + 6 Gy irradiated groups, and changes in tumor size were measured for 20 days. Results show that administration of water-soluble propolis inhibits the reduction of hemocytes caused by whole-body irradiation, enhances antioxidant effects against radioactivity, and inhibits tumor growth.

  6. Pharmacodynamic Study on Anti-inflammatory and Analgesic Effects of Tibetan Medicine Pleurospermum hookeri var.thomsonii%藏药西藏棱子芹抗炎镇痛药效学研究

    袁明; 李云周; 许苗; 赵协慧

    2012-01-01

    本文采用二甲苯致小鼠耳廓肿胀法、棉球致小鼠肉芽肿法观察藏药西藏棱子芹的抗炎作用,采用热板法、醋酸扭体法观察藏药西藏棱子芹的镇痛作用.结果表明藏药西藏棱子芹能明显抑制二甲苯所致小鼠耳廓肿胀和棉球所致小鼠肉芽肿;能提高小鼠对热板疼痛的阈值,减少小鼠扭体反应的次数,延长醋酸所致小鼠扭体反应的潜伏时间.藏药西藏棱子芹具有显著的抗炎镇痛作用,值得开发研究.%The anti-inflammatory effects of Tibetan Medicine Pleurospermum hookeri var. thomsonii in mice was observed in test of ear swelling caused by xylene and cotton pellet-induced granuloma mouse method. The analgesic effect of P. hookeri var. thomsonii in mice was observed in hot-plate test and acetic acid-induced writhing. The experiments showed that P. hookeri var. thomsonii could apparently inhibit auricle swelling induced by xylene and cotton pellet-induced granuloma, obviously prolong the pain threshold of temperature stimuli, decrease the number of writhe induced by acetic acid, and reduce the latent twisted body reaction times in mice. Tibetan Medicine P. hookeri var. thomsonii has both anti-inflammatory and analgesic effects obviously,and is worthy of research and development.

  7. Effects of peripheral dynamic movements on the lower-limb circulation assessed by thermography: three one-group studies

    Kaerki, Anne; Laehdeniemi, Matti

    2002-03-01

    Peripheral dynamic movements are used as part of postoperative protocols and for preventing vascular complications during bed rest. The effects of peripheral movements have not been studied. The purposes of these studies were to explain the effects of peripheral dynamic movements on lower limb circulation. The aim was also to explain how other factors like sex, age, BMI, medication, smoking, sports activity etc. affect the circulation. Healthy young subjects (N=19), healthy elderly subjects (N=19) and diabetic subjects (N=21) participated in the studies between 1997 and 1999. The study design was the same in each study. Infrared technology and image processing belong to our focus fields of applied research and IR is widely used in our real time industrial applications including also ongoing research of new possibilities. This paper presents the results of our newest application of IR thermography, where it was used to measure the skin temperature over the soleus muscle during and after dynamic ankle movements. The results showed that the skin temperature increased further during the recovery period after movements, and temperature was highest after 3- 5 minutes. Diabetic male subjects were the only subgroup that had immediate decrease during recovery period. The studies showed that smoking had a negative effect on circulation. BMI had also negative correlation (-0,356), showing that subjects with higher BMI had less increase. The results proved that peripheral movements were effective for increasing circulation in the soleus muscle and the effect was still seen after 15 minutes.

  8. Pharmacodynamic analysis of the analgesic effect of capsaicin 8% patch (QutenzaTM in diabetic neuropathic pain patients: detection of distinct response groups

    Martini C

    2012-03-01

    Full Text Available Christian Martini1,*, Ashraf Yassen2,*, Erik Olofsen1, Paul Passier2, Malcom Stoker3, Albert Dahan1 1Department of Anesthesiology, Leiden University Medical Center, Leiden, The Netherlands; 2Global Clinical Pharmacology and Exploratory Development, Astellas Pharma Global Development Europe, Leiderdorp, The Netherlands; 3Global Medical Sciences, Astellas Pharma Global Development Europe, Leiderdorp, The Netherlands*These authors contributed equally to this workAbstract: Treatment of chronic pain is associated with high variability in the response to pharmacological interventions. A mathematical pharmacodynamic model was developed to quantify the magnitude and onset/offset times of effect of a single capsaicin 8% patch application in the treatment of painful diabetic peripheral neuropathy in 91 patients. In addition, a mixture model was applied to objectively match patterns in pain-associated behavior. The model identified four distinct subgroups that responded differently to treatment: 3.3% of patients (subgroup 1 showed worsening of pain; 31% (subgroup 2 showed no change; 32% (subgroup 3 showed a quick reduction in pain that reached a nadir in week 3, followed by a slow return towards baseline (16% ± 6% pain reduction in week 12; 34% (subgroup 4 showed a quick reduction in pain that persisted (70% ± 5% reduction in week 12. The estimate of the response-onset rate constant, obtained for subgroups 1, 3, and 4, was 0.76 ± 0.12 week-1 (median ± SE, indicating that every 0.91 weeks the pain score reduces or increases by 50% relative to the score of the previous week (= t½. The response-offset rate constant could be determined for subgroup 3 only and was 0.09 ± 0.04 week-1 (t½ 7.8 weeks. The analysis allowed separation of a heterogeneous neuropathic pain population into four homogenous subgroups with distinct behaviors in response to treatment with capsaicin. It is argued that this model-based approach may have added value in analyzing

  9. Pathobiology of cancer chemotherapy-induced peripheral neuropathy (CIPN

    Yaqin eHan

    2013-12-01

    Full Text Available Chemotherapy induced peripheral neuropathy (CIPN is a type of neuropathic pain that is a major dose-limiting side-effect of potentially curative cancer chemotherapy treatment regimens that develops in a ‘stocking and glove’ distribution. When pain is severe, a change to less effective chemotherapy agents may be required, or patients may choose to discontinue treatment. Medications used to alleviate CIPN often lack efficacy and/or have unacceptable side-effects. Hence the unmet medical need for novel analgesics for relief of this painful condition has driven establishment of rodent models of CIPN. New insights on the pathobiology of CIPN gained using these models are discussed in this review. These include mitochondrial dysfunction and oxidative stress that are implicated as key mechanisms in the development of CIPN. Associated structural changes in peripheral nerves include neuronopathy, axonopathy and/or myelinopathy, especially intra-epidermal nerve fiber (IENF degeneration. In patients with CIPN, loss of heat sensitivity is a hallmark symptom due to preferential damage to myelinated primary afferent sensory nerve fibers in the presence or absence of demyelination. The pathobiology of CIPN is complex as cancer chemotherapy treatment regimens frequently involve drug combinations. Adding to this complexity, there are also subtle differences in the pathobiological consequences of commonly used cancer chemotherapy drugs, viz platinum compounds, taxanes, vincristine, bortezomib, thalidomide and ixabepilone, on peripheral nerves.

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

    Lassoued Saloua

    2011-08-01

    Full Text Available Abstract Background The aim of this study is to investigate the effect of quercetin in alleviating the cytotoxic effects of Dimethoate in human peripheral blood lymphocytes. Methods Lymphocytes were divided into too groups. The first group, lymphocytes were incubated for 4 h at 37°C with different concentrations (0, 40, 60 and 100 mM of Dimethoate. The second group was preincubated with quercetin for 30 min and followed by Dim incubation for 4 h at 37°C. Results Following in vitro incubation, Dimethoate caused a significant increase in malondialdehyde levels, a significant decrease in thiol levels, as well as a significant increase in superoxide dismutase, and catalase activities in lymphocytes at different concentrations. Quercetin pretreated lymphocytes showed a significant protection against the cytotoxic effects inducted by Dimethoate on the studied parameters. Conclusion In conclusion, antioxidant quercetin could protect against Dimethoate-induced oxidative stress by decreasing lipid peroxidation, protein oxidation and increasing superoxide dismutase and catalase activities in human lymphocytes.

  11. Effect of Surface Pore Structure of Nerve Guide Conduit on Peripheral Nerve Regeneration

    Oh, Se Heang; Kim, Jin Rae; Kwon, Gu Birm; Namgung, Uk; Song, Kyu Sang

    2013-01-01

    Polycaprolactone (PCL)/Pluronic F127 nerve guide conduits (NGCs) with different surface pore structures (nano-porous inner surface vs. micro-porous inner surface) but similar physical and chemical properties were fabricated by rolling the opposite side of asymmetrically porous PCL/F127 membranes. The effect of the pore structure on peripheral nerve regeneration through the NGCs was investigated using a sciatic nerve defect model of rats. The nerve fibers and tissues were shown to have regenerated along the longitudinal direction through the NGC with a nano-porous inner surface (Nanopore NGC), while they grew toward the porous wall of the NGC with a micro-porous inner surface (Micropore NGC) and, thus, their growth was restricted when compared with the Nanopore NGC, as investigated by immunohistochemical evaluations (by fluorescence microscopy with anti-neurofilament staining and Hoechst staining for growth pattern of nerve fibers), histological evaluations (by light microscopy with Meyer's modified trichrome staining and Toluidine blue staining and transmission electron microscopy for the regeneration of axon and myelin sheath), and FluoroGold retrograde tracing (for reconnection between proximal and distal stumps). The effect of nerve growth factor (NGF) immobilized on the pore surfaces of the NGCs on nerve regeneration was not so significant when compared with NGCs not containing immobilized NGF. The NGC system with different surface pore structures but the same chemical/physical properties seems to be a good tool that is used for elucidating the surface pore effect of NGCs on nerve regeneration. PMID:22871377

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

    Silva, Mabile Francine Ferreira

    2011-10-01

    Full Text Available Introduction: The peripheral facial paralysis (PFP results from the reduction or interruption of the axonal transport to the seventh cranial nerve resulting in complete or partial paralysis of the facial movements. The facial deformity and limitation of movements, besides affecting the aesthetics and functionality, can significantly interfere with interpersonal communication. Objective: Investigate the psychological contents and other social effects associated to PFP in adult subjects, performing a comparative analysis in three groups of subjects with PFP: at flaccid, recovery and sequel phases. Method: Quantitative and qualitative research. 16 adult subjects, from both sexes, aging between 43 and 88 years old, with PFP. Procedure: Open interviews with subjects. The material was recorded in audio and video, literally transcribed, systematized through categorical and statistical analysis. Results: The subjects bearing sequels presented higher statistical significance of psychological contents and social effects associated to PFP. Followed, respectively, by those that were on flaccid and recovery phases. The results suggest that the speech-language therapist, besides performing functional and aesthetical rehabilitation with the subject with PFP, needs to be aware of psychological and social aspects that may be involved, in order to evaluate and seek to reduce the degree of psychological distress and promote the social adjustment of these patients. Conclusion: The biopsychosocial approach to patients with PFP revealed a wide and significant range of subjective contents that warrant new studies that may contribute to the effectiveness of the speech-language clinical method to approach this medical condition.

  13. Effect of surface pore structure of nerve guide conduit on peripheral nerve regeneration.

    Oh, Se Heang; Kim, Jin Rae; Kwon, Gu Birm; Namgung, Uk; Song, Kyu Sang; Lee, Jin Ho

    2013-03-01

    Polycaprolactone (PCL)/Pluronic F127 nerve guide conduits (NGCs) with different surface pore structures (nano-porous inner surface vs. micro-porous inner surface) but similar physical and chemical properties were fabricated by rolling the opposite side of asymmetrically porous PCL/F127 membranes. The effect of the pore structure on peripheral nerve regeneration through the NGCs was investigated using a sciatic nerve defect model of rats. The nerve fibers and tissues were shown to have regenerated along the longitudinal direction through the NGC with a nano-porous inner surface (Nanopore NGC), while they grew toward the porous wall of the NGC with a micro-porous inner surface (Micropore NGC) and, thus, their growth was restricted when compared with the Nanopore NGC, as investigated by immunohistochemical evaluations (by fluorescence microscopy with anti-neurofilament staining and Hoechst staining for growth pattern of nerve fibers), histological evaluations (by light microscopy with Meyer's modified trichrome staining and Toluidine blue staining and transmission electron microscopy for the regeneration of axon and myelin sheath), and FluoroGold retrograde tracing (for reconnection between proximal and distal stumps). The effect of nerve growth factor (NGF) immobilized on the pore surfaces of the NGCs on nerve regeneration was not so significant when compared with NGCs not containing immobilized NGF. The NGC system with different surface pore structures but the same chemical/physical properties seems to be a good tool that is used for elucidating the surface pore effect of NGCs on nerve regeneration.

  14. Effects of xenogeneic, allogeneic and isogeneic thymus grafts on lymphocyte populations in peripheral lymphoid organs of the nude rat

    Hougen, H P; Klausen, B; Stenvang, J P

    1987-01-01

    In order to gain information about the effect of xenografted, allografted and isografted thymic tissue on peripheral lymphoid organs of immune-deficient rats, athymic nude LEW rats of ninth backcross-intercross were grafted with fetal calf and neonatal BDIX and LEW thymus. Adrenalectomy was also...

  15. Indirect effects of glucagon-like peptide-1 receptor agonist exendin-4 on the peripheral circadian clocks in mice.

    Ando, Hitoshi; Ushijima, Kentarou; Fujimura, Akio

    2013-01-01

    Circadian clocks in peripheral tissues are powerfully entrained by feeding. The mechanisms underlying this food entrainment remain unclear, although various humoral and neural factors have been reported to affect peripheral clocks. Because glucagon-like peptide-1 (GLP-1), which is rapidly secreted in response to food ingestion, influences multiple humoral and neural signaling pathways, we suggest that GLP-1 plays a role in the food entrainment of peripheral clocks. To test this, we compared the effects of exendin-4, a GLP-1 receptor agonist, on mRNA expression of the clock genes (Clock, Bmal1, Nr1d1, Per1, Per2, and Cry1) with those of refeeding. In addition, we investigated whether exendin-4 could affect the rhythms of the peripheral clocks. In male C57BL/6J mice, although refeeding rapidly (within 2 h) altered mRNA levels of Per1 and Per2 in the liver and that of Per1 in adipose tissue, a single i.p. injection of exendin-4 did not cause such changes. However, unlike the GLP-1 receptor antagonist exendin-(9-39), exendin-4 significantly influenced Per1 mRNA levels in the liver at 12 h after injection. Moreover, pretreatment with exendin-4 affected the rapid-feeding-induced change in Per1 not only in the liver, but also in adipose tissue, without effect on food intake. Furthermore, during light-phase restricted feeding, repeated dosing of exendin-4 at the beginning of the dark phase profoundly influenced both the food intake and daily rhythms of clock gene expression in peripheral tissues. Thus, these results suggest that exendin-4 modulates peripheral clocks via multiple mechanisms different from those of refeeding.

  16. Indirect effects of glucagon-like peptide-1 receptor agonist exendin-4 on the peripheral circadian clocks in mice.

    Hitoshi Ando

    Full Text Available Circadian clocks in peripheral tissues are powerfully entrained by feeding. The mechanisms underlying this food entrainment remain unclear, although various humoral and neural factors have been reported to affect peripheral clocks. Because glucagon-like peptide-1 (GLP-1, which is rapidly secreted in response to food ingestion, influences multiple humoral and neural signaling pathways, we suggest that GLP-1 plays a role in the food entrainment of peripheral clocks. To test this, we compared the effects of exendin-4, a GLP-1 receptor agonist, on mRNA expression of the clock genes (Clock, Bmal1, Nr1d1, Per1, Per2, and Cry1 with those of refeeding. In addition, we investigated whether exendin-4 could affect the rhythms of the peripheral clocks. In male C57BL/6J mice, although refeeding rapidly (within 2 h altered mRNA levels of Per1 and Per2 in the liver and that of Per1 in adipose tissue, a single i.p. injection of exendin-4 did not cause such changes. However, unlike the GLP-1 receptor antagonist exendin-(9-39, exendin-4 significantly influenced Per1 mRNA levels in the liver at 12 h after injection. Moreover, pretreatment with exendin-4 affected the rapid-feeding-induced change in Per1 not only in the liver, but also in adipose tissue, without effect