EFFECTIVENESS PROGNOSTICATION OF A COMBINED ANALGESIC FORMULATION DEPENDING ON QUANTITATIVE COMPOSITION OF ITS COMPONENTS

2016 ◽  
pp. 44-48
Author(s):  
N. G. Vengerovich ◽  
M. A. Yudin ◽  
A. S. Nikiforov ◽  
G. S. Sagalov ◽  
M. S. Vakhviyainen ◽  
...  
Keyword(s):  
Drug Interaction ◽  
Opioid Receptor ◽  
Analgesic Activity ◽  
Analgesic Effect ◽  
Receptor Agonist ◽  
Quantitative Composition ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Opioid Receptor Agonist ◽  
Combined Administration

In experiments on rats, analgesic activity of fentanyl opioid receptor agonist and central 2-adrenomimetic dexmedetomidine as well as the character of their interaction at a combined administration were studied. Meaneffective anesthetic doses of the drugs in heat radiant tail flick test were 54.5 and 22.5 μg/kg correspondingly. Using izobolographic analysis, it was shown that for a combination with equal parts or with a greater part of fentanyl, the type of drug interaction can be characterized as potentiation. A model of prognostication of probability values of the analgesic effect development in relation to doses of combination components was elaborated and experimentally tested.

scholarly journals Evaluation of Antinociceptive Effects of Chitosan-Coated Liposomes Entrapping the Selective Kappa Opioid Receptor Agonist U50,488 in Mice

Medicina ◽  
2021 ◽  
Vol 57 (2) ◽  
pp. 138
Author(s):  
Liliana Mititelu Tartau ◽  
Maria Bogdan ◽  
Beatrice Rozalina Buca ◽  
Ana Maria Pauna ◽  
Cosmin Gabriel Tartau ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Kappa Opioid Receptor ◽  
Tail Flick ◽  
Opioid Agonist ◽  
Kappa Opioid ◽  
Tail Flick Test ◽  
Writhing Test ◽  
Opioid Receptor Agonist ◽  
Antinociceptive Effects

Background and Objectives: The selective kappa opioid receptor agonist U50,488 was reported to have analgesic, cough suppressant, diuretic and other beneficial properties. The aim of our study was to analyze the effects of some original chitosan-coated liposomes entrapping U50,488 in somatic and visceral nociceptive sensitivity in mice. Materials and Methods: The influence on the somatic pain was assessed using a tail flick test by counting the tail reactivity to thermal noxious stimulation. The nociceptive visceral estimation was performed using the writhing test in order to evaluate the behavioral manifestations occurring as a reaction to the chemical noxious peritoneal irritation with 0.6% acetic acid (10 mL/kbw). The animals were treated orally, at the same time, with a single dose of: distilled water 0.1 mL/10 gbw; 50 mg/kbw U50,488; 50 mg/kbw U50,488 entrapped in chitosan-coated liposomes, according to the group they were randomly assigned. Results: The use of chitosan-coated liposomesas carriers for U50,488 induced antinociceptive effects that began to manifest after 2 h, andwere prolonged but with a lower intensity than those caused by the free selective kappa opioid in both tests. Conclusion: In this experimental model, the oral administration of nanovesicles containing the selective kappa opioid agonist U50,488 determined a prolonged analgesic outcome in the tail flick test, as well as in the writhing test.

scholarly journals ASSESSMENT OF ANALGESIC ACTIVITY OF NELUMBO NUCIFERA FRUIT ETHANOL EXTRACT

2019 ◽  
pp. 1-5
Author(s):  
MUHAMMAD ALI RAJPUT ◽  
TABASSUM ZEHRA ◽  
FIZZAH ALI ◽  
GUNESH KUMAR
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Research Work ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Herbal Remedies ◽  
Tail Flick ◽  
Traditional Use ◽  
Tail Flick Test ◽  
Pathway Inhibition

Objective: Utilization of herbal remedies rich in flavonoids and vitamins have increased significantly these days to treat various disorders, thus existing research work encircled to appraise the analgesic effect of Nelumbo nucifera fruit (NNF) for evaluating its traditional use pharmacologically in disorders which are associated with pain and inflammation. Methods: Central analgesic activity in mice was assessed by tail flick test and the latency time i.e. the removal of tail from the stimulus was recorded. Similarly acetic acid induced writhing test was also conducted for the assessment of peripheral analgesic effect in mice and number of writhes was counted along with percent inhibition of writhes. Results: In tail flick test the peek anti-nociceptive effect at all doses of fruit was observed at 90 min. However, the percentage of tail elongation time was highest at a dose of 200 mg/kg i.e. 82% at 90 min. Number of writhes was highly significantly reduced at all doses of NNF but maximum effects were observed at dose 200 mg/kg as compared to control, indicating 48.41 % inhibition of writhes. Conclusion: NNF have exhibited strong analgesic effect in both animal models, which may be connected with the synergistic actions of flavonoids, saponins and tannins on arachidonic acid pathway inhibition. Hence NNF seems to have a great potential in disorders associated with pain but more experimental trials in this field are required to confirm these findings.

scholarly journals Effect of adjuvant drugs on the analgesic activity of opioid morphine analgesics and compound RU-1205

2021 ◽  
Vol 7 (3) ◽  
pp. 41-47
Author(s):  
Alexander A. Spasov ◽  
Olesya Iu. Grechko ◽  
Natalya V. Eliseeva ◽  
Yuliya V. Lifanova ◽  
Angelina N. Aleksandrenkova
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Opioid Analgesics ◽  
Benzodiazepine Receptor ◽  
Tail Flick ◽  
Opioid Agonist ◽  
Tail Flick Test ◽  
Kappa Agonist ◽  
Kappa Opioid Agonist ◽  
Probable Interaction

Introduction: Adjuvant medications can be used to increase the analgesic effect of opioid analgesics, reduce the manifestation of side effects, and also for premedication. This paper provides information on the effect of clonidine, haloperidol, metocloparmide, diazepam, midazolam on opioid analgesics: - morphine and the selective kappa-opioid agonist compound RU-1205. Materials and methods: A probable interaction between RU-1205, morphine and adjuvant drugs in pain behaviors was carried out on the model of somatogenic pain. 95 male mice received either RU-1205 (5 mg/kg, i.p.) and morphine (1 mg/kg, i.p.) separately or in combination with haloperidol (0.45 mg/kg, i.p.); midazolam (0.3 mg/kg, i.p.); diazepam (1 mg/kg, i.p.); metoclopramide (5 mg/kg, i.p.), and clonidine (1 mg/kg, i.p.). The analgesic effect was assessed by tail flick test. Registration of the latent period of the reaction was carried out 30, 60 and 90 minutes after the adjuvant drug administration. Results: When studying the interaction with morphine, it was found that clonidine, haloperidol and metoclopramide enhanced the effects; diazepam offset them, and midazolam had no affect on the analgesic properties. In the course of the studies, RU-1205 showed an increase in analgesic activity when combined with clonidine, a slight increase with midazolam, and a decrease when co-administered with diazepam. Haloperidol had no influence on the effect of RU-1205, while metoclopramide both potentiated and reduced the analgesic effect. Discussion: Pharmacodynamic and pharmacokinetic interactions of RU-1205 with an α2AR agonist, benzodiazepine receptor agonists, D2P antagonist, and σ-receptor blocker were established. Conclusion: The presented data make it possible to more accurately formulate ideas about the localization and action mechanism of the kappa-agonist of opioid receptors, the compound RU-1205.

scholarly journals ASSESSMENT OF ANALGESIC ACTIVITY OF NELUMBO NUCIFERA FRUIT ETHANOL EXTRACT

2019 ◽  
pp. 1-5
Author(s):  
MUHAMMAD ALI RAJPUT ◽  
TABASSUM ZEHRA ◽  
FIZZAH ALI ◽  
GUNESH KUMAR
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Research Work ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Herbal Remedies ◽  
Tail Flick ◽  
Traditional Use ◽  
Tail Flick Test ◽  
Pathway Inhibition

Objective: Utilization of herbal remedies rich in flavonoids and vitamins have increased significantly these days to treat various disorders, thus existing research work encircled to appraise the analgesic effect of Nelumbo nucifera fruit (NNF) for evaluating its traditional use pharmacologically in disorders which are associated with pain and inflammation. Methods: Central analgesic activity in mice was assessed by tail flick test and the latency time i.e. the removal of tail from the stimulus was recorded. Similarly acetic acid induced writhing test was also conducted for the assessment of peripheral analgesic effect in mice and number of writhes was counted along with percent inhibition of writhes. Results: In tail flick test the peek anti-nociceptive effect at all doses of fruit was observed at 90 min. However, the percentage of tail elongation time was highest at a dose of 200 mg/kg i.e. 82% at 90 min. Number of writhes was highly significantly reduced at all doses of NNF but maximum effects were observed at dose 200 mg/kg as compared to control, indicating 48.41 % inhibition of writhes. Conclusion: NNF have exhibited strong analgesic effect in both animal models, which may be connected with the synergistic actions of flavonoids, saponins and tannins on arachidonic acid pathway inhibition. Hence NNF seems to have a great potential in disorders associated with pain but more experimental trials in this field are required to confirm these findings.

scholarly journals AN AN STUDY OF ANALGESIC ACTIVITY OF HAFFNER’S TAIL CLIP METHOD ON ALBINO WISTAR RATS OF SOME POLYHERBAL FORMULATION

2019 ◽  
pp. 142-144
Author(s):  
LOKENDRA SINGH
Keyword(s):  
Analgesic Activity ◽  
Side Effect ◽  
Analgesic Effect ◽  
Design Method ◽  
Curcuma Longa ◽  
Albino Rats ◽  
Tail Flick ◽  
Herbal Drugs ◽  
Tail Flick Test ◽  
Tail Clip

Objective: Herbal drugs are more beneficial better than aspirin because this is an herb so no side effect this drug and it is easy to collect or use to as herbal drugs. Words are inadequate to describe the motivation for my work given to my beloved guide. I would like to add special thanks to my guide Gauravbilwal, for their guidance, support, and encouragement. Purpose (Hypothesis): The main purpose of this article pays to attention for herbal drugs because they are naturally old effective drugs. As well as, Ayurveda treatment is very older effective technique. Design/Method: Haffner gave to this technique of determining analgesic are around in 1929. Procedure: This technique according to tail if clipped with any object and tightly or will be compression generation of pain in the tail as well as mice starting to bite that portion of its tail, and could evaluate and recorded the response how much it bites tail quickly or in potential. Using this simple yet important marvel, we may apply the drug to be evaluated and record the response whether it bites tail quickly or in potential. If given drugs have analgesic likely, then rat will not bite its tail so frequently. Mice that do not show any response within 15 s will reject from the experiment. Results: The found in analgesic activity of additional compounds test to significant on tail flick test than acetic acid-induced test and thus it appears that the test compounds inhibit predominantly the peripheral pain mechanism. The results of the study indicate that the extracts of polyherbal plants of analgesic activity by reducing the abdominal constriction significantly and may supposed to have a possible role in inhibition of cyclooxygenase in the prostaglandin pathways (p****<0.0001, ***0.0001, *0.05). Conclusion: The present study showed the significant analgesic effect of both aqueous and alcoholic at 400 mg/kg doses in albino rats, we reported for the 1st time analgesic effect of different plants (Curcuma longa, Colchicaceae, Colocynthis, Withania somnifera, and Achyranthes aspera) in Haffner’s tail clip models. Aspirin has each uncoated effervescent tablet content are acetylsalicylic acid I.P. 325 mg. Finally summarized in this article represent a most effective results of herbal drugs equalized allopathic drugs without any other side effect. Hence, this is very usefully combination of Ayurveda drugs.

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