scholarly journals Analgesic activity of allopurinol and febuxostat in experimental animals

Author(s):  
Yajnesh P. Sahu ◽  
Sachchidanand Pandey ◽  
Sabita Mohapatra

Background: Currently, two classes of analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are used to manage pain in different clinical situations. Chronic uses of these drugs have various adverse effects like gastric ulceration/bleeding, analgesic nephropathy and respiratory depression, physical dependence, addiction, respectively. Xanthine oxidase inhibitors, used for chronic gout, might have a role in alleviation of pain, as per literature survey. Hence, the present study was carried out to evaluate the potential analgesic activity of allopurinol and febuxostat in different experimental models.Methods: The analgesic activity of allopurinol and febuxostat was assessed by employing two different experimental pain models-tail flick latency model in rats for central analgesia and acetic acid induced writhing model in mice for peripheral analgesia and was compared with tramadol and aspirin.Results: Allopurinol and febuxostat produced significant central and peripheral analgesic effects as is evident from increase in reaction time in tail flick test and inhibition in number of writhes in acetic acid induced writhing test.Conclusions: The results of the present study demonstrate marked analgesic effect of allopurinol and febuxostat.

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4172
Author(s):  
Sarinee Leksiri ◽  
Hasriadi Hasriadi ◽  
Peththa Wadu Dasuni Wasana ◽  
Opa Vajragupta ◽  
Pornchai Rojsitthisak ◽  
...  

Analgesic drugs in a combination-form can achieve greater efficacy with lesser side effects compared to either drug alone. The combination of drugs acting at different targets or mechanisms of action has been recognized as an alternative approach for achieving optimal analgesia. In this study, the analgesic effects of pregabalin (30, 60, 100, 200 mg/kg), curcumin (15, 30, 60, 100, 120 mg/kg), and 1:1 fixed-dose ratio of the pregabalin-curcumin combination were assessed using two acute nociceptive pain models, the acetic acid-induced writhing and tail-flick tests in mice. The pregabalin-curcumin combination produced a dose-dependent decrease in mean of writhes and an increase in the percentage of antinociception by the acetic acid-induced writhing test. In the tail-flick test, the combination also showed an improvement in antinociception indicated by the tail-flick latency, % antinociception, and area under the curve (AUC). Isobolographic analysis of interactions demonstrated a significant synergistic interaction effect between pregabalin and curcumin in both acute nociceptive pain models with the experimental ED50 below the predicted additive line and the combination index < 1. These findings demonstrate that the combination of pregabalin and curcumin exhibits a synergistic interaction in mouse models of acute nociceptive pain.


2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Zahra Rabiei ◽  
Zahra Lorigooini ◽  
Fatemeh Firuzi ◽  
Mohammad Rahimi-Madiseh

Background: The use of natural compounds in relieving pain has been commonplace since ancient times and their use is currently increasing. Objectives: Given that analgesic and anti-inflammatory effects of Kombucha have not been studied, this study was designed to examine these effects in vitro. Methods: In this experimental study, rats were divided into four groups. The control group received normal saline i.p in the same amount of the drug. The other groups received Kombucha tea i.p at 250, 500, and 1000 mg/kg. Tail-flick and acetic acid tests were used to evaluate the analgesic effects of Kombucha tea and the xylene-induced ear inflammation test to evaluate the anti-inflammatory effects of Kombucha tea. Results: Kombucha tea at three doses 250, 500, and 1000 mg/kg significantly reduced the number of writhings in the acetic acid test. Kombucha tea at 1000 mg/kg significantly increased pain tolerance in the tail-flick test. Kombucha tea at 250 and 500 mg/kg could significantly reduce inflammation in the rat’s ear. Conclusions: The results of this study indicate that Kombucha has analgesic effects in rats and can be considered in future treatments.


2021 ◽  
Vol 7 (3) ◽  
pp. 41-47
Author(s):  
Alexander A. Spasov ◽  
Olesya Iu. Grechko ◽  
Natalya V. Eliseeva ◽  
Yuliya V. Lifanova ◽  
Angelina N. Aleksandrenkova

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.


Author(s):  
Sumanlata . ◽  
Akanksha Suman ◽  
Rajeev Kumar Sharma ◽  
Meenakshi Jindal ◽  
Adnan Khan

Background: Pain and pyrexia are the warning signals, primarily protective in nature, that cause discomfort and suffering and may even be unbearable and incapacitating. The modern drugs (like opioids, NSAIDs, corticosteroids) currently used for the management of pain, fever and inflammatory conditions, present with many known adverse effects. Tinospora cordifolia known as Giloe, widely used in folk medicine due to its property to cure a number of diseases. Hence the present study was undertaken to explore the analgesic activity of water-soluble extract of stem of T. cordifolia in albino rats in experimentally induced pain.Methods: Present study was done in the department of pharmacology, albino rats were used to study the analgesic activity of T. cordifolia aqueous extract at the dose of 1.25g/kg,2.5g/kg and 5g/kg p.o. Various methods like Eddy’s hot plate, tail flick test and acetic acid induced writhing were used for the anti- nociceptive study.Results: In Eddy’s hot plate and tail flick test an increase in reaction time was observed with peak effect at 90min. Results were similar to the standard drug Tramadol in acetic acid induced writhing increase in time of onset, decrease in number and duration of writhing was observed.Conclusions: Aqueous extract of T. cordifolia was effective in all the three models of pain suggesting its possible action by central and peripheral mechanisms. Activity of T. cordifolia can be attributed to various phytoconstituents viz. protoberberine alkaloids, terpenoids, glycosides and polysaccharides. It can be developed as potent analgesic agent in future.


2018 ◽  
Vol 17 (1) ◽  
pp. 36-41 ◽  
Author(s):  
Hina Imran ◽  
Atiq Ur Rahman ◽  
Tehmina Sohail ◽  
S Intasar H Taqvi ◽  
Zahra Yaqeen

Background: This study was aimed to find out the central and peripheral analgesic activity of hydro methanolic extract of aerial parts of Onosma bracteatum.Material and methods: The central and peripheral analgesic activity is evaluated by tail flick test and acetic acid induced writhing test at the doses of 50, 100, 250 and 500mg/kg body weight respectively in animal models.Results: The results obtained from Tail flick test revealed that O. bracteatum possesses potent analgesic effects by inducing significant increase in latency period in dose dependent manner at all doses at 1, 2 and 3 hours post feeding respectively. The maximum effect was observed at a dose of 500mg/kg i.e. 258.9% (p<0.05) at 3hrs post feeding. Diclofenac sodium (5mg/kg body weight) run as standard also increased the latency period continuously and highest activity was noted at 3hr i.e. 284.5% (p<0.05). Acetic acid induced writhing test also showed significant activity in a similar manner by O. bracteatum i.e 54% (p<0.05) at 500mg/kg while standard drug Diclofenic sodium (5mg/kg body weight) showed 45.9% (p<0.05) activity.Conclusion: It is concluded that O. bracteatum possesses significant central and peripheral analgesic activity in animal model.Bangladesh Journal of Medical Science Vol.17(1) 2018 p.36-41


2020 ◽  
Vol 19 (2) ◽  
pp. 127-132
Author(s):  
Siddig Ibrahim Abdelwahab ◽  
Shyam Sunder Pancholi ◽  
Syam Mohan ◽  
Muhammad Hadi Sultan ◽  
Pankaj Tripathi ◽  
...  

Saussurea lappa Clarke (Compositae) is well known as a medicinal plant. Its roots are traditionally used in alleviating pain and swelling. In the current research, we have evaluated the antinociceptive activity of essential oil obtained from the roots of S. lappa. In addition, the development and evaluation of a pharmaceutical-grade cream was also conducted in this study. Extraction of essential oil from the roots of the plant was performed by a steam distillation method using the Clevenger apparatus. The antinociceptive activity was assessed in Sprague Dawley rats using tail flick, hot plate, and analgesic-meter, where diclofenac was used as a standard reference analgesic agent. S. lappa showed analgesic activity in all test systems in a dose- and time-dependent manner. In addition, the formulated cream obtained from the essential oil showed very promising pharmaceutical and pharmacological properties. The analgesic activity of S. lappa may be due to its interaction with opioid receptors and involvement of peripheral analgesia. The ability of S. lappa to show both slow- and fast-onset analgesic effects suggests it could be used as a drug candidate for pain management. The current findings thus warrant further research in the development of this novel analgesic agent.


1999 ◽  
Vol 54 (10) ◽  
pp. 1327-1336 ◽  
Author(s):  
Zafar Saeed Saify ◽  
Khalid Mohammed Khan ◽  
Syed Moazzam Haider ◽  
Syed Tasadaque Ali Shah ◽  
Muhammad Saeed ◽  
...  

Synthesis and analgesic activity of 4-phenylpiperidine derivatives is a topic of high actuality. A s part of a programme towards obtaining new potential analgesics, ten derivatives of 4- acetyl-4-phenylpiperidine and ten derivatives of 4-hydroxy-4-phenylpiperidine were synthesised and characterized through spectroscopic techniques. All derivatives along with the parent compounds were evaluated for analgesic activity in the acetic acid-induced writhing assay and tail-flick test in mice. All derivatives of 4-acetyl-4-phenylpiperidine except one com pound exhibited more or less protection against mice writhing, whereas all the compounds proved to be inactive in the tail-flick test at doses of 50 and 100 mg/kg body weight.


1997 ◽  
Vol 87 (6) ◽  
pp. 1348-1358 ◽  
Author(s):  
Jorn Lotsch ◽  
Gerd Kobal ◽  
Anne Stockmann ◽  
Kay Brune ◽  
Gerd Geisslinger ◽  
...  

Background The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine. Methods In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide. Results Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G. Conclusion After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.


2011 ◽  
Vol 02 (02) ◽  
pp. 130-136 ◽  
Author(s):  
Keshab Raj Paudel ◽  
SK Bhattacharya ◽  
GP Rauniar ◽  
BP Das

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.


2019 ◽  
Vol 65 (3) ◽  
pp. 22-31
Author(s):  
Ighodaro Igbe ◽  
Osaze Edosuyi ◽  
Agbonlahor Okhuarobo ◽  
Adarki Pongri ◽  
Nkechi Maduako ◽  
...  

Summary Introduction: Potato (Solanum tuberosum L.) is an important vegetable crop in Syria. Potato tuber moth Cussonia barteri is a small tree that grows in the sub-Saharan part of Africa. Various parts of the plant are used for the treatment of a variety of ailments in ethno-medicine. Objective: To evaluate the anti-inflammatory and analgesic effect of the methanol leaf extract of Cussonia barteri. Material and methods: The leaves were air-dried, powdered and repeatedly extracted with methanol using a Soxhlet apparatus. The resulting methanol extract (100, 200 and 400 mg/kg) was evaluated for anti-inflammatory activity using carrageenan-induced paw oedema, xylene-induced ear oedema and formalin-induced arthritis tests. Analgesic effect was evaluated using acetic acid-induced mouse writhing, hot plate and tail flick tests. Results: All doses of the extract significantly (p<0.05) reduced carrageenan-induced paw oedema, however the 400 mg/kg dose gave a sustained effect. The extract significantly inhibited xylene induced ear oedema at all doses. There were no significant (p>0.05) reductions in paw swellings due to formalin. In the acetic acid induced writhing test, the extract significantly (p<0.05) decreased writhing at 400 mg/kg only. Reaction times were not significantly different from the control in the hot plate and tail flick tests. Conclusion: This study has shown that the methanol extract possesses acute anti-inflammatory and peripherally mediated analgesic effects.


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