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Analgesic Activity (analgesic + activity)

Distribution by Scientific Domains

Medical Sciences	75%
Chemistry	24%

Selected Abstracts

Anti-Inflammatory and Analgesic Activities of the Aqueous Extract of Acacia karroo Stem Bark in Experimental Animals

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 5 2008
Adeolu A. Adedapo
The extract at 100 and 200 mg/kg reduced significantly the formation of oedema induced by carrageenan and histamine. In the acetic acid-induced writhing model, the extract showed a good analgesic effect characterized by a significant reduction in the number of writhes with two doses (100 and 200 mg/kg) used when compared to the untreated control group. In the tail immersion test, the extract at the doses used (100 and 200 mg/kg) increased reaction time to pain after 30 min. of oral administration of the extract. Indomethacin at 10 mg/kg served as reference drug in all these tests. The results gave a scientific basis to the traditional uses of Acacia karroo mainly for wound poultices, eye treatments and cold remedies. [source]

Synthesis, Antiinflammatory and Analgesic Activity of 4-Aminoantipyrin Derivatives.

CHEMINFORM, Issue 16 2003
A. E. Rubtsov
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Synthesis, Antiinflammatory and Analgesic Activity of Amino Acids Acylated with Ibuprofen.

CHEMINFORM, Issue 41 2002
L. V. Anikina
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

ChemInform Abstract: Synthesis of Some Triazolyl-Antipyrine Derivatives and Investigation of Analgesic Activity.

CHEMINFORM, Issue 11 2002
Guelhan Turan-Zitouni
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

ChemInform Abstract: Synthesis, Antiinflammatory and Analgesic Activity of Several Arylamides of N-Substituted Anthranilic Acids.

CHEMINFORM, Issue 34 2001
A. B. Shakirova
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Analgesic and hepatotoxic effects of Ononis spinosa L.

PHYTOTHERAPY RESEARCH, Issue 6 2006
Betül Sever Yõlmaz
Abstract The present study investigated the analgesic and hepatoprotective activities of a water extract of Ononis spinosa L. (OS) in mice. Analgesic activity was based on the pain thresholds measured with the tail-flick test before administration at 30, 90 and 150 min. The results were analysed with one-way variance analysis. The extract of Ononis spinosa showed analgesic activity equivalent to aspirin at 30 and 90 min and even higher than aspirin with the 50 mg/kg dose. At a dose of 100 mg/kg OS showed an analgesic effect equivalent to aspirin at all time points. The hepatoprotective influence of OS on carbon tetrachloride (CCl4)-induced acute liver toxicity was also studied. The extract had no significant effect on the increased levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT) and bilirubin in CCl4 treated animals (p > 0.05). Thus, the results reveal that the extract of OS had no hepatoprotective effect on CCl4 -induced acute liver toxicity. Copyright © 2006 John Wiley & Sons, Ltd. [source]

The therapeutic potential of NO-NSAIDs

FUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 1 2003
John L. Wallace
Abstract NSAIDs, including those that are selective for cyclooxygenase-2, are among the most widely used drugs. However, these drugs produce significant side effects in the gastrointestinal and cardiorenal systems, which greatly limit their utility. In recent years, a new type of anti-inflammatory agent has been developed that appears to offer significant advantages over conventional and Cox-2-selective NSAIDs. No-NSAIDs are derivatives of conventional NSAIDs, which are able to release nitric oxide over prolonged periods of time. The combination of balanced inhibition of the two main isoforms of COX with controlled release of nitric oxide yields a series of drugs that exert anti-inflammatory and analgesic activities in a wide range of settings, and have markedly reduced gastrointestinal and cardiorenal toxicity. Recent clinical trials of NO-NSAIDs have provided a ,proof of concept' that is completely consistent with pre-clinical characterization of these compounds. [source]

Anti-inflammatory and analgesic activities of the ethanolic extracts from Zanthoxylum riedelianum (Rutaceae) leaves and stem bark

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2007
Leonardo Mandalho Lima
We have evaluated the anti-inflammatory and analgesic properties of the leaves (LCE) and stem bark (BCE) crude extracts of Zanthoxylum riedelianum (Rutaceae). Different fractions of the stem bark extract (hexane, BCEH; dichloromethane, BCED; ethyl acetate, BCEE; and lyophilized aqueous residual, BCEW) were also investigated. We studied the effects of the extracts and fractions using the rat paw oedema test induced by carrageenan, dextran, histamine or nystatin; the mouse abdominal constriction test; the mouse hot-plate test (only for LCE and BCE); and the mouse formalin test. Both extracts and all BCE fractions displayed anti-inflammatory activity in the carrageenan-induced oedema model, but not for dextran, histamine or nystatin. Considering the analgesic models, both extracts showed antinociceptive activity, but BCE was more active than LCE in models of central pain. All BCE fractions showed significant inhibition in the abdominal constriction test and in both phases of the formalin test. When BCED was submitted to phytochemical procedures it led to the isolation of six lignans (sesamin, methylpluviatolide, dimethylmatairesinol, piperitol-4,-O-,,,-dimethylallyl ether, kaerophyllin and hinokinin), and a triterpene (lupeol). Inhibition of cyclooxygenase and its metabolites may have been involved in the mechanism of action of this plant, considering previous studies reporting the anti-inflammatory and analgesic activity for the identified lignans, as well as anti-inflammatory activity for lupeol. [source]

Pharmacological studies on siculine syrup.

PHYTOTHERAPY RESEARCH, Issue 2 2009
II: effects on smooth, cardiovascular muscle preparations, skeletal
Abstract Earlier pharmacological screening showed that siculine syrup (a traditional herbal remedy purported to be useful in the prevention and treatment of sickle cell pain , crises, due to sickle cell anaemia , SCA) had antisickling and analgesic activities as well as antimicrobial and diuretic effects. SCA is an important haemoglobinopathy in Africa and many other communities/countries worldwide, with relatively high morbidity and mortality. The present study was to determine the effects of the extract on various isolated muscle preparations , smooth, skeletal and cardiovascular. Siculine (4,20 µg/mL), like acetylcholine (40,400 µg/mL), contracted the isolated rat uterus concentration dependently. Similar effects were observed with the guinea-pig ileum and rabbit jejunum (2,20 µg/mL). In contrast to these effects, the direct (muscle) and indirect (nerve) stimulations of rat phrenic nerve,diaphragm were relaxed by siculine (4 and 8 µg/mL) and d -tubocurarine (0.8 µg/mL). Siculine also concentration-dependently decreased both the rate and force of contraction of guinea-pig atria and rabbit heart and also resulted in a fall in cat blood pressure in a manner similar to those of acetylcholine. The possible therapeutic and/or toxicological consequences of these effects including the hypotensive activity is noteworthy since siculine syrup is used by the local population for the prevention and treatment of sickle cell pain crises. Copyright © 2008 John Wiley & Sons, Ltd. [source]

Antipyretic and analgesic activities of Caesalpinia bonducella seed kernel extract

PHYTOTHERAPY RESEARCH, Issue 5 2005
P. Archana
Abstract Ethanolic extract (70%) of Caesalpinia bonducella seed kernel has been subjected for its antipyretic and antinociceptive activities in adult albino rats or mice of either sex at 30, 100 and 300 mg/kg orally. The extract demonstrated marked antipyretic activity against Brewer's yeast-induced pyrexia in rats. The extract had significant central analgesic activity in hot plate and tail flick methods. It also exhibited marked peripheral analgesic effect in both acetic acid-induced writhing test in mice and Randall-Selitto assay in rats. It also significantly inhibited the formalin-induced hind paw licking in mice. In conclusion, the present study suggests that the ethanolic extract of Caesalpinia bonducella seed kernel possesses potent antipyretic and antinociceptive activities and thus, validates its use in the treatment of pain and pyretic disorders. Copyright © 2005 John Wiley & Sons, Ltd. [source]

Bioactivity studies on ,-sitosterol and its glucoside

PHYTOTHERAPY RESEARCH, Issue 5 2002
Irene M. Villaseñor
Abstract ,-Sitosterol and ,-sitosteryl-,- D -glucoside were isolated as analgesic constituents from the leaves of Mentha cordifolia Opiz. The acetic acid-induced writhing test showed that ,-sitosterol and ,-sitosteryl-,- D -glucoside decreased the number of squirms induced by acetic acid by 70.0% and 73.0%, respectively, at a dose of 100,mg /,kg mouse. Statistical analysis using the Kruskall Wallis one-way analysis of variance by ranks showed that these isolates approximate the analgesic activity of mefenamic acid at a 0.001 level of significance. The hot plate method confirmed their analgesic activities, as ,-sitosterol and ,-sitosteryl-,- D -glucoside exhibited a 300% and 157% increase in pain tolerance, respectively, while mefenamic acid, a known analgesic, showed a 171% increase. Neither isolate exhibited antiinflammatory activity using the carrageenan-induced mouse paw oedema assay. ,-Sitosterol also exhibited anthelminthic and antimutagenic activities. In vitro tests using live Ascaris suum as test animals showed that the behaviour of worms treated with ,-sitosterol approximated that of the positive controls, Combantrin and Antiox. An in vivo micronucleus test showed that ,-sitosterol inhibited the mutagenicity of tetracycline by 65.3% at a dose of 0.5,mg /kg mouse. At the same dose, it did not exhibit chromosome-breaking activity. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Analgesic and antiinflammatory properties of Sideritis lotsyi var. Mascaensis

PHYTOTHERAPY RESEARCH, Issue 3 2002
Margarita Hernández-Pérez
Abstract The antiinflammatory, analgesic and antimicrobial activities of crude ethanol extracts of Sideritis lotsyi var. mascaensis (Lamiaceae), and chloroform and aqueous fractions were evaluated in mice using paw and ear oedema induced by carrageenan and 12-o-tetradecanoyl-phorbol-acetate (TPA), respectively, as inflammation models, the writhing test induced by acetic acid for evaluating analgesic activity and the disk-diffusion method for testing antimicrobial actions. The results obtained demonstrated significant topical antiinflammatory and analgesic activities for the ethanol extract and chloroform fraction, but no relevant antimicrobial activity against the microorganisms tested. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Studies on Synthesis and Pharmacological Activities of 1,2,4-Triazolo[3,4- b]1,3,4-thiadiazoles and their Dihydro Analogues

ARCHIV DER PHARMAZIE, Issue 4 2009
Vinod Mathew
Abstract 4-Amino-5-substituted aryl-3-mercapto-1,2,4-triazoles are versatile synthons for constructing various biologically active heterocycles. Starting from 4-amino-5-substituted aryl-3-mercapto-1,2,4-triazole 3a,c, a series of new 3,5-disubstituted-1,2,4-triazolo-[3,4- b]1,3,4-thiadiazoles and their 5,6-dihydrotriazolothiadiazoles were prepared. The structures of all the newly synthesized compounds have been confirmed by elemental analysis, IR, 1H-NMR, 13C-NMR, and mass spectra. The antimicrobial effects of the synthesized compounds were investigated using the paper disc method. Anti-inflammatory and analgesic activities of the synthesized compounds were assessed by carrageenan-induced rat paw oedema method and by Eddy's hot plate method, respectively. Some of the compounds exhibited promising antimicrobial activities as well as moderate to good anti-inflammatory activity and analgesic activity. [source]

Synthesis, analgesic, anti-inflammatory and ulcerogenic index activities of novel 2-methylthio-3-substituted-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-ones

DRUG DEVELOPMENT RESEARCH, Issue 3 2007
V. Alagarsamy
Abstract A variety of novel 2-methylthio-3-substituted amino-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-ones were synthesized by reacting 3-amino-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one with different aldehydes and ketones. The starting material 3-amino-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one was synthesized from 2-amino-3-carbethoxy-4,5-dimethyl thiophene. The compounds were investigated for their analgesic activity in albino mice, and for their anti-inflammatory and ulcerogenic index activities in Wistar rats. The compound 2-(1-ethylpropylideneamino)-2-methylthio-5,6-dimethyl thieno [2,3- d] pyrimidin-4(3H)-one (AS2) showed the most potent analgesic activity of the series. It also showed more potent anti-inflammatory activity when compared to the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic potential when compared to aspirin. Drug Dev Res 68:134,142, 2007. © 2007 Wiley-Liss, Inc. [source]

The role of methadone in cancer pain treatment , a review

INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, Issue 7 2009
W. Leppert
Summary Background:, Methadone is an opioid analgesic of step 3 of the World Health Organization (WHO) analgesic ladder. Aim and Methods:, To outline pharmacodynamics, pharmacokinetics, drug interactions, equianalgesic dose ratio with other opioids, dosing rules, adverse effects and methadone clinical studies in patients with cancer pain. A review of relevant literature on methadone use in cancer pain was conducted. Results:, Methadone is used in opioid rotation and administered to patients with cancer pain not responsive to morphine or other strong opioids when intractable opioid adverse effects appear. Methadone is considered as the first strong opioid analgesic and in patients with renal impairment. Methadone possesses different pharmacodynamics and pharmacokinetics in comparison to other opioids. The advantages of methadone include multimode analgesic activity, high oral and rectal bioavailability, long lasting analgesia, lack of active metabolites, excretion mainly with faeces, low cost and a weak immunosuppressive effect. The disadvantages include long and changeable plasma half-life, high bound to serum proteins, metabolism through P450 system, numerous drug interactions, lack of clear equianalgesic dose ratio to other opioids, QT interval prolongation, local reactions when administered subcutaneously. Conclusions:, Methadone is an important opioid analgesic at step 3 of the WHO analgesic ladder. Future controlled studies may focus on establishment of methadone equianalgesic dose ratio with other opioids and its role as the first strong opioid in comparative studies with analgesia, adverse effects and quality of life taken into consideration. [source]

Anti-inflammatory and analgesic activities of the ethanolic extracts from Zanthoxylum riedelianum (Rutaceae) leaves and stem bark

Free radical scavengers, anti-inflammatory and analgesic activity of Acaena magellanica

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2002
Gabriela Egly Feresin
Extracts of the whole plant Acaena magellanica (Rosaceae) were assessed for anti-inflammatory, antipyretic and analgesic activity in animal models. At 600 mg kg,1, the global ethanolic extract (GEE), dichloromethane (DCM) and defatted methanol (MeOH) fractions showed a mild anti-inflammatory effect in the carrageenan-induced guinea-pig paw oedema. The GEE, DCM and defatted MeOH fractions significantly reduced inflammation by 43.2, 40.5 and 42.1%, respectively. The GEE did not showed any significant antipyretic activity in doses up to 600 mg kg,1. A 20% w/v infusion administered orally at 16 mL kg,1 presented analgesic effect in the acetic acid-induced abdominal constriction test in mice. The GEE and MeOH extract of A. magellanica showed free radical scavenging activity in the diphenylpicrylhydrazyl decolouration assay. Assay-guided isolation led to quercetin, Q-3- O -,-D-glucoside, Q-3- O -,-D-galactoside, ellagic acid and catechin as the free radical scavengers. The saponins tormentic acid 28- O -,-D-galactopyranoside and 28- O -,-D-glucopyranoside were isolated from the polar extract. The structures were determined by spectroscopic methods. [source]

Antipyretic and analgesic activities of Caesalpinia bonducella seed kernel extract

Black cumin seed essential oil, as a potent analgesic and antiin,ammatory drug

PHYTOTHERAPY RESEARCH, Issue 3 2004
Valiollah Hajhashemi
Abstract The steam-distilled essential oil of Iranian black cumin seed (Nigella sativa L.) was investigated for its composition and analgesic and antiin,ammatory properties. After oil analysis by GC/MS, 20 compounds were identi,ed in the oil, obtained in 0.4% (v/w) yield. Among them, para -cymene (37.3%) and thymoquinone (13.7%) were the major components. Acetic acid-induced writhing, formalin and light tail ,ick tests were used for assessment of analgesic activity. Antiin,ammatory activity was evaluated using carrageenan-induced paw oedema in rats and croton oil-induced ear oedema in mice. Black cumin seed essential oil (BCSEO) was found to produce a signi,cant analgesic effect in acetic acid-induced writhing, formalin and light tail ,ick tests. Naloxone, an opioid antagonist, could not reverse the analgesic effect observed in the formalin test. Although oral administration of BCSEO at doses of 100, 200 and 400 µL/kg did not exert a signi,cant antiin,ammatory effect in the carrageenan test, i.p. injection of the same doses signi,cantly (p < 0.001) inhibited carrageenan-induced paw oedema. BCSEO at doses of 10 and 20 µL/ear could also reduce croton oil-induced oedema. It seems that mechanism(s) other than opioid receptors is (are) involved in the analgesic effect of BCSEO since naloxone could not reverse this effect. Both systemic and local administration of BCSEO showed antiin,ammatory activity. Thymoquinone, as one of the major components of BCSEO, probably has an important role in these pharmacological effects. Copyright © 2004 John Wiley & Sons, Ltd. [source]

Analgesic studies on total alkaloids and alcohol extracts of Eclipta alba (Linn.) Hassk.

PHYTOTHERAPY RESEARCH, Issue 2 2004
Mahesh Sawant
Abstract A variety of analgesics are used for the treatment of acute and chronic pain in different disease states. A narcotic or a non-narcotic analgesic that does not cause respiratory depression and addiction is needed. In Ayurveda a large number of indigenous drugs have been mentioned possessing analgesic properties (e.g. Guggul, Erand, Rasna, Bhringaraj, Methika, Palandu and Prasikayavani). The present experimental research work was undertaken to determine the analgesic activity of the total ethanol extract of Eclipta alba, and also the isolated alkaloids of Eclipta alba in albino mice by using standard experimental models such as the tail clip method, the tail ,ick method and the acetic acid induced writhing response. The results from this study show that both the ethanol extract as well as the total alkaloids produce good analgesic activity in all the different models of analgesia used. The total alkaloidal fraction was the most ef,cacious in all models tested. Copyright © 2004 John Wiley & Sons, Ltd. [source]

Bioactivity studies on ,-sitosterol and its glucoside

Analgesic and antiinflammatory properties of Sideritis lotsyi var. Mascaensis

Analgesic and antipyretic effects of Myrica salicifolia (Myricaceae)

PHYTOTHERAPY RESEARCH, Issue S1 2002
K. Njung'e
Abstract Myrica salicifolia Hoechst (Myricaceae) root extract was found to have analgesic activity in mice. In rats there was antipyretic but no antiinflammatory activity. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Evaluation of tramadol and its main metabolites in horse plasma by high-performance liquid chromatography/fluorescence and liquid chromatography/electrospray ionization tandem mass spectrometry techniques

RAPID COMMUNICATIONS IN MASS SPECTROMETRY, Issue 2 2009
Marinella De Leo
Tramadol is a centrally acting analgesic drug that has been used clinically for the last two decades to treat pain in humans. The clinical response of tramadol is strictly correlated to its metabolism, because of the different analgesic activity of its metabolites. O -Desmethyltramadol (M1), its major active metabolite, is 200 times more potent at the µ -receptor than the parent drug. In recent years tramadol has been widely introduced in veterinary medicine but its use has been questioned in some species. The aim of the present study was to develop a new sensible method to detect the whole metabolic profile of the drug in horses, through plasma analyses by high-performance liquid chromatography (HPLC) coupled with fluorimetric (FL) and photodiode array electrospray ionization mass spectrometric (PDA-ESI-MS) detection, after its sustained release by oral administration (5,mg/kg). In HPLC/FL experiments the comparison of the horse plasma chromatogram profile with that of a standard mixture suggested the identification of the major peaks as tramadol and its metabolites M1 and N,O -desmethyltramadol (M5). LC/PDA-ESI-MS/MS analysis confirmed the results obtained by HPLC/FL and also provided the identification of two more metabolites, N -desmethyltramadol (M2), and N,N -didesmethyltramadol (M3). Another metabolite, M6, was also detected and identified. The present findings demonstrate the usefulness and the advantage of LC/ESI-MS/MS techniques in a search for tramadol metabolites in horse plasma samples. Copyright © 2008 John Wiley & Sons, Ltd. [source]

Studies on Synthesis and Pharmacological Activities of 1,2,4-Triazolo[3,4- b]1,3,4-thiadiazoles and their Dihydro Analogues

Neuroexcitatory Effects Of Morphine And Hydromorphone: Evidence Implicating The 3-Glucuronide Metabolites

CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 7 2000
Mt Smith
SUMMARY 1. Morphine is recommended by the World Health Organization as the drug of choice for the management of moderate to severe cancer pain. 2. Education of health professionals in the past decade has resulted in a large increase in the prescribing of opioids, such as morphine, and in the magnitude of the doses administered, resulting in an improvement in the quality of pain relief available for many cancer patients. 3. However, the reported incidence of neuroexcitatory side effects (allodynia, myoclonus, seizures) in patients administered large doses of systemic morphine or its structural analogue, hydromorphone (HMOR), has also increased. 4. Clinically, increasing the magnitude of the morphine or HMOR dose administered to patients already exhibiting neuroexcitatory opioid related side effects, results in an exacerbation rather than an attenuation of the excitatory behaviours. 5. In contrast, cessation of the opioid or rotation to a structurally dissimilar opioid (e.g. from morphine/HMOR to methadone or fentanyl), usually results in a restoration of analgesia and resolution of the neuroexcitatory opioid side effects over a period of hours to days. 6. To explain the clinical success of ,opioid rotation', it is essential to understand the in vivo metabolic fate of morphine and HMOR. 7. Following systemic administration, morphine and HMOR are metabolized primarily to the corresponding 3-glucuronide metabolites, morphine-3-glucuronide (M3G) and hydromorphone-3-glucuronide (H3G), which are not only devoid of analgesic activity but evoke a range of dose-dependent excitatory behaviours, including allodynia, myoclonus and seizures, following intracerebroventricular (i.c.v.) administration to rats. 8. Several studies have shown that, following chronic oral or subcutaneous morphine administration to patients with cancer pain, the cerebrospinal fluid (CSF) concentrations of M3G exceed those of morphine and morphine-6-glucuronide (analgesically active morphine metabolite) by approximately two- and five-fold, respectively. 9. These findings suggest that when the M3G concentration (or H3G by analogy) in the CSF exceeds the neuroexcitatory threshold, excitatory behaviours will be evoked in patients. 10. Thus, rotation of the opioid from morphine/HMOR to a structurally dissimilar opioid, such as methadone or fentanyl, will allow clearance of M3G/H3G from the patient central nervous system over hours to days, thereby producing a time-dependent resolution of the neuroexcitatory behaviours while maintaining analgesia with methadone or fentanyl. [source]