Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “ANALGESICS”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 919 records · Page 51Linked to original sources
PubMed2003

Amide derivatives of [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids as potential analgesic and anti-inflammatory compounds.

In this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We have tested the analgesic and anti-inflammatory activities of the synthesized compounds in vivo by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. Compounds 3a, 3d, 3e, 3j and 3k potent analgesic and anti-inflammatory activities without gastric lesions in the tested animals. Therefore, conversion of the carboxylate moiety into certain amide derivatives generated potent analgesic and anti-inflammatory compounds while eliminating the gastrointestinal side effects. Cyclooxygenase (COX)-selectivity of the active compounds was also investigated by using in vitro human whole blood assay. Compounds 3a, 3e, 3h and 3k selective inhibition of COX-2 to some extent although the inhibitory activity was not very potent.

Acetates↗
PubMed2006

Synthesis of some novel azo derivatives of 3,5-dimethyl-1-(2-hydroxyethyl)pyrazole as potent analgesic agents.

A series of 1-(2-hydroxyethyl)-3,5-dimethylpyrazolylazo derivatives, incorporating thiosemicarbazide 2a-c, 1,3,4-thiadiazole 3a-c, and 1,2,4-triazole-3-thione 4a-c were synthesized. The structure of these novel synthesized compounds 2a-c, 3a-c, and 4a-c was confirmed by spectral analysis. All these compounds were screened for their analgesic activity. Hot-plate and tail-immersion tests were used for the determination of the analgesic activity. Morphine, an analgesic through both spinal and supraspinal pathways, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg i.p. Among the compounds, 2-(butylamino)-5-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-1,3,4-thiadiazole 3a and 4-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-4-(2-phenethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 4c showed analgesic effects in both tests. Especially 4c exerted strong analgesia starting at 30 min after injection.

Analgesics↗
PubMed2003

Anti-inflammatory drugs, analgesics and the risk of perforated colonic diverticular disease.

BACKGROUND: Acute perforated colonic diverticular disease has a mortality rate of up to 30 per cent, but little is known about its aetiology. The aim of this study was to test the hypothesis that three classes of drugs, namely non-steroidal anti-inflammatory drugs (NSAIDs), opioid analgesics and corticosteroids, are risk factors for perforated diverticular disease. METHODS: All patients with confirmed perforated colonic diverticular disease were identified over a 5-year period in two hospitals in Norfolk, UK. Two control groups were selected and matched for age, sex and hospital of admission. Data on medication use were obtained from hospital records. Odds ratios for each drug were calculated using conditional logistic regression. RESULTS: Opioid analgesics, NSAIDs and corticosteroids were all positively associated with perforated colonic diverticular disease. The odds ratio for opioid analgesics was 1.8 (95 per cent confidence interval (c.i.) 1.1 to 3.0) in the analysis with ophthalmology controls and 3.1 (95 per cent c.i. 1.8 to 5.5) in that with dermatology controls. Respective odds ratios for NSAIDs were 4.0 (95 per cent c.i. 2.1 to 7.6) and 3.7 (95 per cent c.i. 2.0 to 6.8), and those for corticosteroids were 5.7 (95 per cent c.i. 2.2 to 14.4) and 7.8 (95 per cent c.i. 2.6 to 23.3). CONCLUSION: Opioid analgesics, NSAIDs and corticosteroids are all positively associated with perforated colonic diverticular disease. The consistency of these associations, together with plausible biological mechanisms, suggests that these drugs may have a causative role in this condition.

Adrenal Cortex Hormones↗
PubMed1995

Analgesics and cancers of the renal pelvis and ureter.

To evaluate renal pelvis and ureter (RPU) cancer risk in relation to lifetime use of analgesics, a population-based case-control study was carried out in 3 areas of the United States. Among 502 cases and 496 controls diagnosed and interviewed during 1983-1986, no significant increases in risk were found for any of the non-prescription and prescription analgesics evaluated or among regular users of phenacetin, acetaminophen or aspirin. Neither cumulative lifetime ingestion nor duration of regular use of these 3 drugs, whether alone or in combination, was associated with significantly increased risk of RPU cancer, although a slight excess was observed among long-term users of acetaminophen. Risk was not increased among persons reporting highest cumulative dose and/or longest duration of phenacetin use. Although our study of RPU cancer is the largest to date, it was nonetheless limited by the small number of regular analgesic users and the relatively low response rates. Because of the relatively recent onset of widespread use of acetaminophen, its pharmacologic similarity to phenacetin, a known urothelial carcinogen, and the elevation in risk seen in long-term users, further surveillance of this analgesic is warranted.

Acetaminophen↗
PubMed1986

Oral ciramadol: a new analgesic for postoperative pain.

Ciramadol, a new synthetic narcotic agonist-antagonist analgesic, was compared in 30 and 60 mg doses with pentazocine 50 mg, aspirin 650 mg, and placebo in the treatment of 153 patients with postoperative pain. All drugs were administered between six and 72 hours after surgery. Analgesic efficacy was assessed for six hours after study drug administration using verbal pain intensity, analog pain intensity, and verbal pain relief scales. Significantly (P less than .05) higher analgesic efficacy scores were seen with ciramadol 30 mg than with pentazocine 50 mg and placebo at most of the evaluation points. Doses of ciramadol 30 mg were significantly (P less than .05) more effective than aspirin 650 mg at several time periods, and ciramadol 60 mg was better than pentazocine and placebo at several evaluation times. The 30-mg dose of ciramadol was generally more effective than the 60-mg dose. The mean six-hour cumulative sum of pain intensity difference scores, total pain relief scores, and sum of pain analog intensity difference scores showed that the best analgesic response occurred in the ciramadol 30 mg group, followed by the ciramadol 60 mg, aspirin 650 mg, pentazocine 50 mg, and placebo groups. Side effects were rare and mild. There were no medically important changes in vital signs in any treatment group.

Adolescent↗
PubMed1987

Comparison of the analgesic efficacy and safety oral ciramadol, codeine, and placebo in patients with chronic cancer pain.

Ciramadol is a new opioid agonist-antagonist analgesic with low potential for dependency. Forty-three patients with moderate to severe chronic pain from primary or metastatic malignancy of the bone or major organs were enrolled in a randomized double-blind study that compared orally administered ciramadol (30 mg or 90 mg) to codeine (60 mg) and placebo. A single-dose, four-way crossover design, with a randomized Latin-square treatment sequence, was used. Data for 40 patients who received the above four study medications were included in the final statistical analysis of efficacy. Analgesic efficacy was measured at 0, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, and 6.0 hours, using standard visual and verbal pain relief and pain intensity scales. All active therapies provided greater pain relief than placebo (P less than .05). Ciramadol 30 mg and codeine 60 mg demonstrated equal analgesic activity, whereas ciramadol 90 mg was superior to both therapies. The predominant adverse experiences associated with ciramadol were nausea and drowsiness, which were apparently not dose related. Ciramadol appears to be an effective analgesic at the doses tested, with tolerable gastrointestinal central nervous system side effects at both the 30-and 90-mg dose levels.

Adult↗
PubMed1985

Analgesic potencies of morphine 3- and 6-sulfates after intracerebroventricular administration in mice: relationship to structural characteristics defined by mass spectrometry and nuclear magnetic resonance.

Morphine 3-sulfate, which carries a polar, acidic group at the 3-position much like morphine, does not differ greatly in analgesic potency from morphine following intracerebroventricular administration. This differs from the non-ionizable 3-methyl and 3-ethyl ethers, which are less potent analgesics than morphine. Morphine 6-sulfate, which differs from morphine by having an ionizable group at carbon-6 at physiological pH, is a more potent analgesic than morphine following intracerebroventricular administration. Variations in analgesic potency following modifications at the hydroxyl groups appear only to reflect alterations in point charges rather than structural alterations.

Analgesics↗
PubMedDate not supplied

Risk factors for adverse events in analgesic drug users: results from the PAIN study.

BACKGROUND: The relative influence of various risk factors for adverse events (AE) in analgesics users have never been precisely quantified. Advantage was taken of data generated in the paracetamol, aspirin and ibuprofen new tolerability (PAIN) study, a large randomized double-blinded trial of paracetamol, aspirin or ibuprofen for common pain in general practice to attempt this. OBJECTIVE: Identify and quantify factors associated with the occurrence of AE in users of analgesic drugs. METHOD: Multivariate logistic regression analysis of potential risk factors for all AE, clinically significant AE (SAE) and clinically significant gastro-intestinal AE (GI SAE). RESULTS: Of the 8677 patients included in the study, 8633 contributed data. The main risk factors for SAE were indication: compared to those treated for musculoskeletal pain, patients treated for menstrual pain had an odds ratio (95% Confidence Interval) of 0.4 (0.2-0.7), sore throat 0.6 (0.5-0.8), cold and flu 0.7 (0.6-0.8), headache 0.8 (0.7-1.0); concomitant use of medication contra-indicated in the drugs' labeling (OR: 2.2; 1.6-2.9); increasing number of other concomitant medications: 1: OR 1.5 (1.3-1.8); 2-3: OR 1.9 (1.6-2.3); more than 3: OR (2.7; 2.1-3.5); treatment with aspirin: OR 1.4; (1.2-1.6) but not ibuprofen: OR 0.9; (0.8-1.1) compared to paracetamol; history of previous GI disorder OR 1.4 (1.0-1.8); female gender: OR 1.3 (1.1-1.4). Age was not significantly associated with AE in the multivariate analysis. Risk factors for all AE and GI SAE were mostly the same as for significant AE, but there were fewer GI SAE with ibuprofen than with paracetamol (OR 0.8; 0.6-0.9). CONCLUSION: Apart from the analgesic used and its indication, the main risk factors identified for AE in users of first-line analgesics for common pain were the number and nature of concomitant medication.

Acetaminophen↗
PubMed2004

Analgesic, antiinflammatory and antidiabetic properties of Harpagophytum procumbens DC (Pedaliaceae) secondary root aqueous extract.

South Africa is blessed with a rich floral biodiversity of medicinally useful plants. One such plant is Harpagophytum procumbens DC (Family: Pedaliaceae). H. procumbens is widely used in South African traditional medicine for the treatment, management and/or control of a variety of human ailments. In the present study, the analgesic effect of H. procumbens secondary root aqueous extract was evaluated in mice, using the 'hot-plate' and 'acetic acid' test methods; while the antiinflammatory and antidiabetic effects of the plant's secondary root extract were investigated in rats. Fresh egg albumin-induced pedal oedema and streptozotocin (STZ)-induced diabetes mellitus were used as experimental test models of inflammation and diabetes Diclofenac (DIC, 100 mg/kg i.p.) was used as a reference analgesic and antiinflammatory agent for comparison. Chlorpropamide (250 mg/kg p.o.) was used as a reference hypoglycaemic agent for comparison. H. procumbens root aqueous extract (HPE, 50-800 mg/kg i.p.) produced significant (p < 0.05-0.001) analgesic effects against thermally and chemically induced nociceptive pain stimuli in mice. H. procumbens root extract (HPE, 50-800 mg/kg i.p.) also produced dose-related, significant reductions (p < 0.05-0.001) of the fresh egg albumin-induced acute inflammation of the rat hind paw oedema. Furthermore, the plant extract (HPE, 50-800 mg/kg i.p.) produced dose-dependent, significant reductions (p < 0.05-0.001) in the blood glucose concentrations of both fasted normal and fasted diabetic rats. The results of this experimental animal study indicate that H. procumbens root aqueous extract possesses analgesic, antiinflammatory and hypoglycaemic properties, and lend pharmacological support to the suggested folklore uses of Harpagophytum procumbens root in the management and/or control of painful, arthritic and other inflammatory conditions, as well as for adult-onset, type-2 diabetes mellitus in some communities of South Africa.

Acetic Acid↗
PubMed2005

Analgesic and anticonvulsant properties of Tetrapleura tetraptera (Taub) (Fabaceae) fruit aqueous extract in mice.

Previous studies in our laboratories and elsewhere have shown that the fruit of Tetrapleura tetraptera (Taub) (family: Fabaceae) is widely used in African traditional medicine for the management and/or control of an array of human ailments, including schistosomiasis, asthma, epilepsy, hypertension and so on. The present study was designed to investigate the analgesic and anticonvulsant effects of Tetrapleura tetraptera (Taub) fruit aqueous extract (TTE) in mice. Morphine (MPN, 10 mg/kg i.p.), diclofenac (DIC, 100 mg/kg i.p.), phenobarbitone (20 mg/kg i.p.) and diazepam (0.5 mg/kg i.p.) were used, respectively, as reference analgesic and anticonvulsant agents for comparison. T. tetraptera fruit aqueous extract (TTE, 50-800 mg/kg i.p.) produced dose-dependent, significant (p < 0.05-0.001) analgesic effects against thermally and chemically induced pain in mice. Like the standard anticonvulsant agents (phenobarbitone and diazepam) used, T. tetraptera fruit aqueous extract (TTE, 50-800 mg/kg i.p.) significantly (p < 0.05-0.001) delayed the onset of, and antagonized, pentylenetetrazole (PTZ)-induced seizures. Aqueous extract of the fruit (TTE, 50-800 mg/kg i.p.) also profoundly antagonized picrotoxin (PCT)-induced seizures, but only partially and weakly antagonized bicuculline (BCL)-induced seizures. However, the results of this experimental animal study indicate that Tetrapleura tetraptera (Taub) fruit aqueous extract (TTE) possesses analgesic and anticonvulsant properties. These findings lend pharmacological support to the suggested folkloric uses of the plant's fruit in the management and/or control of painful, arthritic inflammatory conditions, as well as for the management and/or control of epilepsy and childhood convulsions in some tropical African countries.

Acetic Acid↗
PubMed2006

Analgesic and hepatotoxic effects of Ononis spinosa L.

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 (CCl(4))-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 CCl(4) treated animals (p > 0.05). Thus, the results reveal that the extract of OS had no hepatoprotective effect on CCl(4)-induced acute liver toxicity.

Alanine Transaminase↗
PubMed2001

Analgesic and toxic effects of neonicotinoid insecticides in mice.

Several nicotinic agonists with the 6-chloro-3-pyridinyl moiety are potent insecticides (e.g., the neonicotinoids imidacloprid and thiacloprid) while others are candidate nonopioid and nonantiinflammatory analgesics (i.e., epibatidine and several heterocyclic analogs). This study examines the hypothesis for the first time that the neonicotinoid insecticides and their imine metabolites and analogs display analgesic (antinociceptive) activity or adverse toxic effects associated with their action on binding to the alpha 4 beta 2 nicotinic acetylcholine receptor (AChR) subtype. Seven 6-chloro-3-pyridinyl compounds were studied, i.e., imidacloprid and thiacloprid, the corresponding imines and an olefin derivative, a nitromethylene analog, and (+/-)-epibatidine. Like (-)-nicotine and carbachol, they all act as full agonists in the (86)rubidium ion efflux experiment with intact mouse fibroblast M10 cells stably expressing the alpha 4 beta 2 nicotinic AChR. Their agonist action is correlated with binding affinity to the alpha 4 beta 2 receptor from M10 cells. Imidacloprid, thiacloprid, and their imine analogs are not antinociceptive agents in mice by abdominal constriction and hot plate analgesic tests. Their agonist actions at the alpha 4 beta 2 receptor correlate instead with their toxicity. Surprisingly, the nitromethylene analog, a weak agonist, is as potent as (-)-nicotine in inducing antinociception, and the effect persists longer than that caused by (-)-nicotine. However, mecamylamine (1 mg/kg) prevents antinociception induced by (-)-nicotine but not by the nitromethylene analog. Interestingly, this nitromethylene neonicotinoid insecticide gives 80-100% mortality within 15 min at 3 mg/kg with mecamylamine pretreatment at 2 mg/kg, doses at which each agent alone gives no lethality. Therefore, analgesic and toxic effects of the nitromethylene analog differ in their mechanism of action from (-)-nicotine and (+/-)-epibatidine.

Analgesics, Non-Narcotic↗
PubMed1984

Control of cancer pain with analgesics acting in the central nervous system.

Systemic administration of opioids is one of the traditional, but by no means optimized therapeutic procedures in cancer pain. Besides the underlying pathophysiology, appropriate treatment has to take into account the psychodynamics and behavior of the patient as well as his life expectancy. In view of this, therapy with centrally acting analgesics can be considered after administration of analgesics with peripheral action first and then of psychoactive agents. Nefopam is a centrally (but not spinally) acting analgesic with a novel activity profile. Its advantages and disadvantages in the treatment of carcinoma pain are outlined. The opiate agonist-antagonist principle has the advantage of a lower dependence and tolerance potential. In addition, the preparations pentazocine, tilidine plus naloxone, and buprenorphine deviate from the morphine derivatives in various constituent effects. Their actions and side effects are outlined. The optimization of control of cancer pain is not possible without taking into account the time dimension. In 50 pain patients with advanced cancer, the following main errors were observed in previous treatment of pain syndromes: (1) too early parenteral administration in the course of the disease; (2) underdosage; (3) application intervals that were too long; and (4) use of analgesics as needed by the patient or on request and not according to a time schedule.

Adult↗
PubMed1996

Increased risk of ischaemic heart disease mortality in elderly men using anxiolytics-hypnotics and analgesics. Results of the 10-year follow-up of the prospective population study "Men born in 1914", Malmo, Sweden.

OBJECTIVES: An increased risk of all-cause and cardiovascular mortality in users of anxiolytic-hypnotic drugs (AHD) has been reported, and use of analgesics may be an additional factor. Therefore, we examined the association of AHD and analgesic use, alone and in combination, with all-cause and ischaemic heart disease (IHD) mortality. METHODS: Multivariate 10-year survival analysis in a population based cohort of 500 men born in 1914. Relative risks (RR) were adjusted by relevant confounders (blood pressure, serum cholesterol, diabetes mellitus, smoking habit, high alcohol consumption, history of previous IHD, cancer, and other diseases). RESULTS: The RR of both all-cause and IHD mortality were significantly increased among those using both AHD and analgesics compared to those who took neither of these drugs: RR = 1.8 for all-cause mortality, and RR = 2.7 for IHD mortality. CONCLUSION: Although the number of cases was small, warranting interpretative caution, the current study suggests that the combined use of AHD (mainly benzodiazepines) and analgesics seems to be associated with an increase in all-cause and IHD mortality in elderly men.

Aged↗
PubMed1975

Comparative analgesic activity of various naturally occurring cannabinoids in mice and rats.

The analgesic effectiveness of delta-9-tetrahydrocannabinol (THC), a crude marihuana extract (CME), cannabinol (CBN), cannabidiol (CBD), morphine SO-4 and aspirin following oral administration was directly compared in mice using the acetic-induced writhing and hot plate tests and the Randall-Selitto paw pressure test in rats. THC and morphine were equipotent in all tests except that morphine was significantly more potent in elevating pain threshold in the uninflamed rat hind paw. In terms of THC content, CME was nearly equipotent in the hot plate and Randall-Selitto tests, but was 3 times more potent in the acetic acid writhing test. On the other hand, CBN, like aspirin, was only effective in reducing writhing frequency in mice (3 times more potent than aspirin) and raising pain threshold of the inflamed hind paw of the rat (equipotent with aspirin). CBD did not display a significantly analgesic effect in any of the test systems used. The results of this investigation seem to suggest that both THC and CME possess narcotic-like analgesic activity similar to morphine, while CBN appears to be a non-narcotic type analgesic like aspirin.

Acetates↗
PubMed1978

Effects of medial raphe and raphe magnus lesions on the analgesic activity of morphine and methadone.

The effects of lesions of the raphe nuclei on opiate-induced antinociception and brain serotonin (5-HT) levels were investigated. Lesions of the medial raphe nucleus effectively antagonized the analgesic effects of morphine, but not methadone, and lowered brain 5-HT. The decrement in analgesic activity of morphine was reversed by pretreatment with 5-hydroxytryptophan. Lesions of the raphe magnus, a descending 5-HT system, antagonized the analgesic potency of both morphine and methadone. These experiments indicate a differential effect of 5-HT manipulation on opiate-induced analgesia, suggesting a different mechanism of analgesic action for morphine and methadone.

Analgesics↗
PubMed1980

Narcotic analgesics and stereotyped behaviour in mice.

In this paper we have studied the effects of morphine, codeine, fentanyl, pentazocine, etorphine and fluphenazine (all drugs injected i.p.) on stereotyped behaviour induced by methylphenidate 60 mg/kg i.p., as well as induced by apomorphine 5 mg/kg s.c. in mice. It was found that all used analgesics and fluphenazine dose--dependently inhibited the intensity of methylphenidate--induced gnawing in mice. This effect of analgesics, but not that of fluphenazine was antagonized by naloxone (0.8 mg/kg i.p.) and nalorphine (10 mg/kg i.p.). Climbing behaviour induced by apomorphine was not reduced by narcotic analgesics, but fluphenazine inhibited this effect dose--dependently. These findings give the behavioural support that analgesics applied have antidopaminergic activity in mice.

Analgesics, Opioid↗
PubMed1996

Postoperative analgesic effects of an external cooling system and intra-articular bupivacaine/morphine after arthroscopic cruciate ligament surgery.

The aim of this study was to evaluate the analgesic effect of an external cooling system with or without the combined effect of intra-articularly administered bupivacaine/morphine after arthroscopic anterior cruciate ligament (ACL) reconstruction. Fifty patients with isolated ACL insufficiency operated on under general anaesthesia were randomized to three different postoperative treatment groups. Group I was treated with the cooling system during the first 24 h after surgery and an intra-articular injection of 20 ml of physiological saline given at the completion of surgery; in group II, the cooling system was combined with an intra-articular injection of 20 ml bupivacaine 3.75 mg/ml and 1 mg of morphine at the end of the operation; while group III (placebo group) received an intra-articular injection of 20 ml of physiological saline at the completion of surgery. Pain was assessed using a visual analogue scale (VAS) at 1, 2, 4, 6, 24 and 48 h postoperatively. Supplementary analgesic requirements were registered. In group I 80% (16/20) and in group II 90% (18/20) of the patients were satisfied with the postoperative pain control regimen (NS). This was significantly better than in group III, where 30% (3/10) were satisfied. The pain scores were significantly lower in the two treatment groups compared with the placebo group during the entire postoperative period. The pain score was significantly lower in group II than in group I at 24 and 48 h after surgery. The supplementary analgesic requirements were also lower in the two treatment groups compared with the placebo group. No complications due to the use of the cooling system or the intra-articular injections of bupivacaine/morphine were observed. The external cooling system used in this study provides an effective method of obtaining pain relief after arthroscopic surgery. The combination with an intra-articular injection of morphine and bupivacaine results in a slightly greater analgesic effect than the cooling system alone.

Adolescent↗