scholarly journals Pharmacodynamic evaluation of Dezocine injection from Yangtze River Pharmaceutical Group

2021 ◽  
Vol 245 ◽  
pp. 03077
Author(s):  
Rong-Rong Ye ◽  
Yu-Jun Wang ◽  
Xu Xu ◽  
Yan Lu ◽  
Jing-Gen Liu
Keyword(s):  
Molecular Formula ◽  
Analgesic Effects ◽  
Animal Pain ◽  
Pharmaceutical Group ◽  
First Choice ◽  
Pain Models ◽  
First Pass ◽  
Fast Absorption ◽  
Perioperative Pain Management ◽  
Routes Of Drug Administration

Intramuscular injection and intravenous injection are important routes of drug administration, which not only have a fast absorption rate, but also avoid the first pass effect of the drug. In 2009, Yangtze Pharmaceutical Group redeveloped Dezocine(13-Amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecen-3-ol), molecular formula: C16H23NO, in the form of njection. Quickly, Dezocine injection becomes the first choice for perioperative pain management in China and accounts for 45 % of the analgesic market. This study mainly used animal pain models to study the analgesic effects of Dezocine injection. The results indicated that Dezocine produced potent analgesic effect in the hot plate and writhing tests.

scholarly journals In VitroandIn VivoCharacterization of the New Analgesic Combination Beta-Caryophyllene and Docosahexaenoic Acid

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Paolo Fiorenzani ◽  
Stefania Lamponi ◽  
Agnese Magnani ◽  
Ilaria Ceccarelli ◽  
Anna Maria Aloisi
Keyword(s):  
Docosahexaenoic Acid ◽  
Gonadal Hormones ◽  
Male Rats ◽  
Dependent Manner ◽  
Recurrent Pain ◽  
Analgesic Effects ◽  
Animal Pain ◽  
Pain Models

Beta-caryophyllene (BCP) and docosahexaenoic acid (DHA) are components of several plants with documented anti-inflammatory and analgesic effects in animal pain models. In the present study,in vitroandin vivotests were carried out to evaluate their effects, alone or in combination, during long-lasting administration in a model of persistent pain. IR spectra of the two compounds were obtained to determine their chemical stability and thenin vitrotoxicity was evaluated in fibroblasts and astrocytes. In thein vivotests, the analgesic effects of BCP and BCP+DHA were determined in male rats subjected to a model of persistent recurrent pain (three repetitions of the formalin test once a week) to mimic recurrent pain. Both substances were administeredper osin almond oil for 2 weeks. Gonadal hormones were determined at the end of the tests to evaluate treatment-induced effects on their levels. BCP changed fibroblast and astrocyte survival in a dose-dependent manner and the effect was counteracted by DHA coadministration. In thein vivotests, pain responses were significantly decreased in the BCP and BCP+DHA groups with respect to OIL after 1 and 2 weeks of treatment. Estradiol and testosterone levels were increased only in the BCP group. In conclusion, BCP alone or at lower concentration in combination with DHA was efficacious in modulating pain, showing a clear analgesic activity.

Mesenchymal Stem Cells and their Exosomes: Promising Therapeutics for Chronic Pain

2019 ◽  
Vol 14 (8) ◽  
pp. 644-653 ◽  
Author(s):  
Jinxuan Ren ◽  
Na Liu ◽  
Na Sun ◽  
Kehan Zhang ◽  
Lina Yu
Keyword(s):  
Stem Cells ◽  
Chronic Pain ◽  
Mesenchymal Stem Cells ◽  
Stem Cell ◽  
Side Effects ◽  
Human Life ◽  
Analgesic Effects ◽  
Pain Models ◽  
Inflammatory Drugs ◽  
Anxiety Depression

Chronic pain is a common condition that seriously affects the quality of human life with variable etiology and complicated symptoms; people who suffer from chronic pain may experience anxiety, depression, insomnia, and other harmful emotions. Currently, chronic pain treatments are nonsteroidal anti-inflammatory drugs and opioids; these drugs are demonstrated to be insufficient and cause severe side effects. Therefore, research into new therapeutic strategies for chronic pain is a top priority. In recent years, stem cell transplantation has been demonstrated to be a potent alternative for the treatment of chronic pain. Mesenchymal stem cells (MSCs), a type of pluripotent stem cell, exhibit multi-directional differentiation, promotion of stem cell implantation, and immune regulation; they have also been shown to exert analgesic effects in several chronic pain models. Exosomes produced by MSCs have been demonstrated to relieve painful symptoms with fewer side effects. In this review, we summarize the therapeutic use of MSCs in various chronic pain studies. We also discuss ways to enhance the treatment effect of MSCs. We predict in the future, cell-free therapies for chronic pain will develop from exosomes secreted by MSCs.

scholarly journals Comparison of antinociceptive effect of the antiepileptic drug gabapentin to that of various dosage combinations of gabapentin with lamotrigine and topiramate in mice and rats

2011 ◽  
Vol 02 (02) ◽  
pp. 130-136 ◽  
Author(s):  
Keshab Raj Paudel ◽  
SK Bhattacharya ◽  
GP Rauniar ◽  
BP Das
Keyword(s):  
Pain Perception ◽  
Late Phase ◽  
Antinociceptive Effect ◽  
Experimental Pain ◽  
Mechanical Hyperalgesia ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Pain Models ◽  
Antinociceptive Effects

ABSTRACT Introduction: Newer anticonvulsants have a neuromodulatory effect on pain perception mechanisms in a hyperexcitable and damaged nervous system. Aim: This study was designed to study the analgesic effects of gabapentin alone and in combination with lamotrigine and topiramate in experimental pain models. Materials and Methods: Adult albino mice (n = 490) weighing 20–30 g and rats (n = 130) weighing 100–200 g were injected intraperitoneally with gabapentin, lamotrigine, and topiramate alone and in different dose combinations. The hot-plate method, tail-flick method, capsaicin-induced mechanical hyperalgesia, and formalin assay were used to assess the antinociceptive effects. Results: Of the three antiepileptic drugs, when given separately, gabapentin was more efficacious than either topiramate or lamotrigine in all the pain models. Combination of 25 mg/kg gabapentin with 25 mg/kg topiramate was more efficacious (P <.05) than 50 mg/kg gabapentin alone in the capsaicin-induced mechanical hyperalgesia test. Similarly, 50 mg/kg gabapentin with 50 mg/kg topiramate or 5 mg/kg lamotrigine was more efficacious (P <.05) than 50 or 100 mg/kg gabapentin alone in late-phase formalin-induced behaviors. Conclusions: Combination of gabapentin with either lamotrigine or topiramate produced better results than gabapentin alone in capsaicin-induced mechanical hyperalgesia test and in late-phase formalin-induced behaviors.

scholarly journals Analgesic Interaction Between Morphine with Fentanyl In Experimental Murine Pain

2021 ◽  
Author(s):  
Hugo F Miranda ◽  
Viviana Noriega ◽  
Fernando Sierralta ◽  
Ramon Sotomayor-Zarate ◽  
Juan Carlos Prieto
Keyword(s):  
Phase I ◽  
Dose Response ◽  
Multimodal Treatment ◽  
Binding Capacity ◽  
Tail Flick ◽  
Pharmacological Interaction ◽  
Isobolographic Analysis ◽  
Antinociceptive Action ◽  
Animal Pain ◽  
Pain Models

Abstract Opioids are among the most effective pain relievers available, however multimodal antinociception between opioids, has not been extensively studied in diverse animal pain models.In this study the pharmacological interaction of morphine with fentanyl was evaluated in different murine pain models by means of isobolographic analysis. In control animals, morphine and fentanyl produced a dose-related antinociceptive action in the murine assays and the rank of potency was: formalin hind paw phase I > formalin phase II > tail flick. Coadministration of morphine with fentanyl, in a fixed relation 1:1 of their ED50, produces a dose response in all tests and the isobologram resulted in synergism. Fentanyl was more effective than morphine which could be explained according the suggestion that opioids could be acting through other targets, with different binding capacity thru the regulation or activation of non-opioid receptors. Co-administration of morphine with fentanyl induces synergism in all murine trials, confirming the antinociceptive capacity of both opioids which would constitute a promisory idea to multimodal treatment of pain.

scholarly journals Analgesic Effects of Thiamine in Male Long Evans Rats

2017 ◽  
Vol 12 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Sayema Ainan ◽  
Noorzahan Begum ◽  
Taskina Ali
Keyword(s):  
Experimental Pain ◽  
Immersion Test ◽  
Writhing Test ◽  
Analgesic Effects ◽  
Inhibitory Mechanisms ◽  
Significant Decrement ◽  
Pain Models ◽  
Tail Immersion ◽  
Long Evans ◽  
Post Hoc

Background: The concept of analgesic effects of thiamine along with other B vitamins has been supported since long by various clinical and experimental evidences, though effects of individual thiamine on pain are yet to be clearly demonstrated.Objective: To assess the effects of increasing doses of thiamine supplementation on pain.Methods: Forty-eight (48) male Long Evans rats (200±20 gm) were given thiamine (100, 200, 250, mg/kg/day; experimental) or normal saline (5 ml/kg/day; control) intraperitonealy (i.p) for 7 consecutive days. The analgesic activity was evaluated by three experimental pain models, hot (52±0.50C) water tail immersion test, the interphase (6th-15th minutes) of formalin (50?l, 2.5%, subcutaneous) test and acetic acid (2%, i.p) induced writhing test. Statistical analysis was done by ANOVA followed by Bonferroni post hoc test and p?0.05 was considered as significant.Results: In tail immersion test, %MPE significantly increased after 200 (p?0.05) and 250 (p?0.001) mg/kg of thiamine. In the formalin test, thiamine significantly lowered the jerking frequency (p?0.05, p?0.001, p?0.001, respectively) and duration of flexing and licking (p?0.001, in all doses), compared to control. In addition, in writhing test, significant increment in latency of appearance of 1st writhe (p?0.001, in higher 2 doses) and significant decrement in frequency of writhes (p?0.01, p?0.001, p?0.001, respectively, in all doses) were observed.Conclusion: The results of this study conclude that, repetitive administration of thiamine may cause alleviation of pain through central as well as peripheral inhibitory mechanisms, which is dose dependent as well.Bangladesh Soc Physiol. 2017, June; 12(1): 1-9

scholarly journals Analgesic Effects of Cnidium officinale Extracts on Postoperative, Neuropathic, and Menopausal Pain in Rat Models

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Eun Yeong Lim ◽  
Jae Goo Kim ◽  
Jaekwang Lee ◽  
Changho Lee ◽  
Jaewon Shim ◽  
...  
Keyword(s):  
Ferulic Acid ◽  
Dorsal Root Ganglion Neurons ◽  
Great Efficacy ◽  
Withdrawal Threshold ◽  
Analgesic Effects ◽  
Pain Models ◽  
Cnidium Officinale ◽  
Model Treatment ◽  
Ganglion Neurons

Cnidium officinale, widely cultivated in East Asia, has been reported to exhibit pharmacological efficacy in various disorders. However, little has been reported on its role as a pain killer. In this study, we reveal that the C. officinale extract (COE) has great efficacy as a novel analgesic in various in vivo pain models. Administration of COE attenuated hypersensitivity in all postoperative, neuropathic, and menopausal pain models. Decreased hyperalgesia was confirmed by a mechanical withdrawal threshold assay and ultrasonic vocalization call analysis. In addition, application of COE inhibited the induction of the proinflammatory cytokines and calpain-3 on dorsal root ganglion neurons in a spared nerve injury rat model. Treatment with ferulic acid, which was identified as one of the components of COE by HPLC analysis, alleviated nociceptive behaviors. Our findings suggest that ferulic acid is an active compound from COE, and COE is a potential phytomedical source for pain relief by inhibiting the process of inflammation.

Nitrous Oxide Revisited

2005 ◽  
Vol 103 (4) ◽  
pp. 845-854 ◽  
Author(s):  
Philippe Richebé ◽  
Cyril Rivat ◽  
Cyril Creton ◽  
Jean-Paul Laulin ◽  
Pierre Maurette ◽  
...  
Keyword(s):  
Nitrous Oxide ◽  
Morphine Tolerance ◽  
Acute Tolerance ◽  
Dependent Manner ◽  
Analgesic Effects ◽  
Pain Models ◽  
Opioid Induced Hyperalgesia ◽  
Incisional Pain ◽  
Fentanyl Administration ◽  
Dose Dependent

Background Although opioids are unsurpassed analgesics for surgery, they also induce an N-methyl-D-aspartate-dependent enhancement of postoperative hyperalgesia. Because nitrous oxide (N2O) has anti-N-methyl-D-aspartate properties, the purpose of this study was to evaluate nitrous oxide ability to prevent such an opioid-induced hyperalgesia in rats. Methods First, preventive effects of 50/50% N2O-O2 on the development of delayed hyperalgesia observed after inflammatory pain (hind paw carrageenan injection on D0) were examined for several days. Second, the ability of nitrous oxide (10-40%) to limit opioid-induced hyperalgesia induced by fentanyl was evaluated in nonsuffering rats. Third, antihyperalgesic effects of various nitrous oxide concentrations (20-50%) were assessed in both inflammatory and incisional pain models in fentanyl-treated rats (4 x 100 microg/kg subcutaneously). Finally, the analgesic effect of a single dose of morphine was evaluated 24 h after fentanyl administration and nitrous oxide (D0) to assess its preventive effect on acute morphine tolerance in both nonsuffering and hind paw-incised rats. Results When applied on D0, nitrous oxide reduced delayed hyperalgesia induced by inflammation. Exposure to nitrous oxide on D0 also reduced opioid-induced hyperalgesia in nonsuffering rats in a dose-dependent manner. In fentanyl-treated rats with inflammatory or incisional pain, nitrous oxide strongly limited both magnitude and duration of hyperalgesia. Moreover, nitrous oxide exposure on D0 opposed development of acute tolerance to analgesic effects of morphine administered on D1 in both nonsuffering and incised fentanyl-treated rats. Conclusions Nitrous oxide, an N-methyl-D-aspartate receptor antagonist, prevented the enhancement of pain sensitivity induced by both nociceptive inputs and fentanyl and opposed acute morphine tolerance. Results suggest that perioperative nitrous oxide use reduces exaggerated postoperative pain and morphine consumption.

Analgesic effects of neurotensin agonists in a rat bone cancer pain model

2016 ◽  
Author(s):  
Louis Dore-Savard ◽  
Pascal Tetreault ◽  
Melisange Roux ◽  
Marylie Martel ◽  
Myriam Lemire ◽  
...  
Keyword(s):  
Cancer Pain ◽  
Weight Bearing ◽  
Bone Cancer ◽  
Opioid Analgesics ◽  
Bone Cancer Pain ◽  
Intractable Pain ◽  
Analgesic Effects ◽  
Selective Agonist ◽  
Neurotensin Receptors ◽  
Pain Models

Bone metastases are a source of intractable pain, resistant to conventional opioid and non-opioid analgesics. The neurotensin system represents a potential pathway toward bone cancer pain (BCP) relieve via the inhibition of its receptors NTS1 and NTS2. Capitalizing on our recent results using neurotensin analogs in inflammatory and neuropathic pain models, we here show, for the first time, a potential role for neurotensin receptors agonists in the treatment of BCP. The novel non-selective agonist JMV-2009 (300 μg/kg) reversed mechanical allodynia in our rodent BCP model at both early and late stages of the disease. The NTS2-selective agonist JMV-431 (90 μg/kg), in addition to anti-allodynia, also had an effect on weight bearing deficits. In parallel, we tested proven analgesics from several classes to put the effect of neurotensin analogs in perspective and found that morphine (3 mg/kg), tramadol (15 mg/kg) and amitriptyline (10 mg/kg) had mild effects on BCP while the cannabinoid nabilone (1 mg/kg) significantly reversed both allodynia and weight bearing deficits. Taken together, our results affirm the potential of the modulation of the neurotensin system for the development of new analgesics for the treatment of bone cancer pain.

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