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PubMed1975

A new method for the evaluation of analgesic activity using adjuvant-induced arthritis in the rat.

A bioassay was developed for the assessment of analgesic activity by using pain resulting from a reproducible pathological condition. The vocalization displayed by rats with adjuvant-induced polyarthritis was defined as an expression of pain, and a decrease of this response was established as specifically demonstrating analgesic activity. This method was capable of detecting the analgesic activity of morphine-like and narcotic antagonist-type analgesics, as well as the activity of the antipyretic analgesics. The relative potencies of known analgesic agents determined with this technique closely approximated the potencies of these analgesics in man. The instrumentation for recording and measuring the vocal response of arthritic rats is described.

Analgesics↗
PubMed2004

Management of childhood febrile illness prior to clinic attendance in urban Nigeria.

Parents and caregivers often try various treatment modalities for their sick children before bringing them to clinic. Many community-based studies have documented home and self-treatment practices, often with the aid of patent medicine vendors, but less is known about prior treatment behaviour of caregivers who actually reach a government clinic. This study, therefore, aimed at documenting the treatment provided by caregivers prior to their attendance at a public hospital. Beginning in April 1996, a year-long study was conducted among 1,943 sick children and their caregivers who attended the largest government-owned paediatric hospital in Lagos, Nigeria. The major complaints mentioned by the caregivers included fever, cough, and diarrhoea. Most (89%) caregivers had administered some form of medicine to the child prior to the clinic visit, and on average, 2.5 medications had been given. Associations were found between major complaint and type of medicine given: fevers were associated with antimalarial drugs and analgesics (antipyretics), cough was associated with cough syrup and analgesics, while diarrhoea was associated with antidiarrhoeal drugs. Although one-fifth of the children had received an antibiotic, provision of antibiotics was not associated with a particular complaint/illness. Since caregivers appeared to use perceived complaints/illnesses as a treatment guide, this can form the basis of safer and more appropriate recognition of illness and home management. In addition, the information obtained in this study can be used for training clinicians to inquire about home management and, thus, for making more informed decisions about their own treatment and prescribing practices.

Child Care↗
PubMed1989

[Drug therapy of pain].

Pain represents the most frequent complaint for which patients ask for medical help. Successful treatment of acute and chronic pain syndromes largely depends on the knowledge and the therapy of the underlying disease process and on the rational use of analgesics, such as the nonnarcotic analgesic-antipyretics, the anti-inflammatory agents and the opioid analgesics. In addition, so-called 'adjuvant' analgesics of different chemical structures can be used in special clinical conditions to increase the efficacy of the common analgesics. For optimal therapy, the selection and dosing of a specific agent has to be tailored to the individual needs of the patient. For this purpose it is important to follow some general principles of pain management and to consider the relevant pharmacokinetic and pharmacodynamic properties of the various analgesics. This overview summarizes the most important pharmacological properties of the widely used analgetic drugs, with special emphasis on their risk-benefit ratio in various clinical situations.

Analgesics↗
PubMed1981

Aspirin and acetaminophen as constituents of analgesic combinations.

Aspirin and acetaminophen are the mainstays of oral analgesic combinations. One group of combinations is composed of antipyretic-analgesics combined with each other. The superior efficacy of such combinations as compared with an optimal dose of one of the constituents remains to be proved, and there is little evidence that such combinations have less adverse-effect liability than a single agent. On the other hand, there is substantial evidence that combinations of an optimal dose of aspirin or acetaminophen with a narcotic (eg, codeine, hydrocodone, or oxycodone) produce an additive analgesic effect greater than that obtained by doubling the dose of either constituent administered alone. There is also some evidence that the adverse effects produced by such combinations are less than would be produced by an equianalgesic dose of a single constituent.

Acetaminophen↗
PubMed1992

4-substituted 1-methyl-1H-indazoles with analgesic, antiinflammatory and antipyretic activities.

The synthesis of [(1-methyl-1H-indazol-4-yl)oxy]acetic acid 4, 1-methyl-1H-indazole-4-acetic acid 9, 2-(1-methyl-1H-indazol-4-yl)propanoic acid 15 and [[(1,5,6,7-tetrahydro-1-methyl-4H-indazol-4-ylidene)amino]oxy]acet ic acid 16, as well as of amides and esters derived from 4 and 9, starting from 1,5,6,7-tetrahydro-1-methyl-4H-indazol-4-one is described. Some of the above compounds showed weak antiinflammatory, analgesic, antipyretic and hypotensive activities in rats and mice, as well as moderate platelet antiaggregating effects in vitro.

Animals↗
PubMed1982

Studies on an anti-inflammatory agent. III. Pharmacological investigations of a new non-steroidal anti-inflammatory agent: 2-oxo-3-[4-(1-oxo-2-isoindolinyl)-phenyl]-butanamide (GP 650).

The anti-inflammatory, analgesic, antipyretic and ulcerogenic activities and acute toxicity of 2-oxo-3-[4-(1-oxo-2-isoindolinyl)-phenyl]-butanamide (GP 650) were investigated in laboratory animals and compared with those of phenylbutazone, acetylsalicylic acid (ASA), ibuprofen, tiaramide-HCl and tinoridine-HCl. The anti-inflammatory and analgesic activities of GP 650 were found to be almost equivalent to those of phenylbutazone on the basis of various anti-inflammatory and analgesic tests while its antipyretic activity was less marked, and its ulcerogenic action and acute toxicity were much lower than those of the other agents. It is interesting to note that GP 650 possesses marked anti-inflammatory activity similar to acidic anti-inflammatory agents in chronic inflammatory models along with mild antipyretic and ulcerogenic activities found in basic anti-inflammatory agents. Therefore, GP 650 appears to be a promising anti-inflammatory and analgesic agent.

Analgesics↗
PubMed1990

Pharmaco-toxicological effects of acetaminophen in rodents. Battery of tests to screen potential analgesic acetaminophen derivatives.

The pharmacological effects of acute oral administration of acetaminophen have been extensively evaluated in rodents. Using this drug as reference compound we have also standardized several pharmaco-toxociological tests in order to select new analgesic-antipyretic acetaminophen derivatives. According to the results obtained in this work, the following battery of assays is proposed to screen these compounds: a) pharmacological: antipyretic activity against Brewer's yeast-induced pyresis in rats; analgesic activity against chemical-induced writhings in mice and paw pressure test in rats; b) toxicological: oral acute toxicity in mice with and without phenobarbital pretreatment; determination of SGOT and SGPT activities as well as total bilirubin in mice. The usefulness of this procedure in the evaluation of drug effects is also considered.

Acetaminophen↗
PubMed1986

Pharmacological activity of FPP028 (2-phenylpyrazolo-4-ethyl-4,7-dihydro [1,5a]pyrimidin-7-one) a new non-steroid anti-inflammatory agent.

The activity of 2-phenylpyrazolo-4-ethyl-4,7-dihydro [1,5a]pyrimidin-7-one (FPP028), a non-acidic, analgesic, antipyretic, and anti-inflammatory compound, was investigated in a number of pharmacological tests performed in rats. The anti-inflammatory properties of FPP028 were evaluated through the carrageenan induced paw edema and the cotton pellet induced granuloma and compared with the activity of indomethacin, phenylbutazone, and isoxicam; as a result, the activity of FPP028 was shown to be similar to that of the latter compounds. To assess the analgesic properties of FPP028 in comparison with indomethacin and phenylbutazone, the Randall and Sellitto and the mouse-writhing tests were used; in both tests, FPP028 demonstrated a significant analgesic activity. FPP028 was shown to possess antipyretic properties in the test of yeast-induced pyrexia. The gastro-erosive activity of phenylbutazone and FPP028 was studied in restraint-stressed rats; in such test the ulcerogenic activity of phenylbutazone appeared to be dose-related; conversely, FPP028 demonstrated a gastro-protective effect since the number of gastric lesions induced either by stress or phenylbutazone treatment was decreased bu FPP028. Our data show that FPP028 is endowed with most of the pharmacological properties of the classic antiinflammatory drugs. Further studies are however needed to more fully elucidate its mechanism of action because our in-vivo data indicate that FPP028 is not an inhibitor of prostaglandin biosynthesis.

Adrenalectomy↗
PubMed1985

The pharmacology of fever.

The ability to minimise, if not prevent, large variations in deep body temperature that would otherwise result from some environmental conditions is a homeostatic function of unquestioned benefit that is demonstrated only by the more highly evolved animals. Nevertheless, body temperature is raised above normal values in many pathological conditions. This increase in temperature or fever is an active and co-ordinated response, which indicates the involvement of the CNS. Central injection and lesion studies have shown that the brain, in particular the PO/AH, is the site of action of fever-inducing agents, termed pyrogens. Electrophysiological data show that pyrogens modify the activity of central thermosensitive neurones as if to increase heat gain and decrease heat loss. The common response of fever to pyrogens of diverse origins is attributable to fever being mediated by an endogenous pyrogen released by phagocytic cells in the host. The mechanism by which central neuronal function is disturbed by pyrogens present in the periphery is not known. Tracer studies have yet to demonstrate the passage of a pyrogen across the blood-brain barrier. The possible involvement of several putative neurotransmitters and modulators in fever has been reviewed here, but most compounds have not been studied sufficiently to allow firm conclusions to be drawn. Much of the data is limited to the effects of the putative mediators on normal thermoregulation but, even when the effect is hyperthermia, such observations do not necessarily indicate a role for the endogenous material in fever. Dose-response curves for agonists and the effects of antagonists are often undetermined. This shortfall in data is due to some extent to the nature of fever; a central response in vivo over several hours. Although fever may enhance other host reactions to combat infection and inflammation, neither this benefit nor the undesirability of antipyretic therapy has been demonstrated unequivocally in either homeothermic laboratory animals or humans. Consequently, antipyretic drugs continue to be used clinically to alleviate the fever, malaise and/or pain commonly associated with disease. The drugs in common usage are the nonsteroidal antipyretic analgesics, many of which also have an anti-inflammatory effect. The primary mode of action of these drugs as antipyretics appears at present to be the inhibition of cyclo-oxygenase and a consequent reduction of prostanoid material in pyrogen-sensitive areas of the brain.(ABSTRACT TRUNCATED AT 400 WORDS)

Acetylcholine↗
PubMed1992

Preliminary pharmacologic evaluation of crude whole plant extracts of Elephantopus scaber. Part I: In vivo studies.

Elephantopus scaber has been used in Brazil as a traditional remedy to cause diuresis, antipyresis and to eliminate bladder stones. In the current study, aqueous and hydroalcoholic extracts of whole plants were tested for acute toxicity, analgesic, antipyretic, antiinflammatory, cardiovascular, diuretic and constipating activities. Both extracts (0.3-6 g/kg i.p.) induced writhing, loss of muscle tone, ataxia, prostration and death in mice. No analgesic effects of these extracts were detected using mouse hot-plate and acetic acid-induced writhing tests. Both extracts failed to modify diuresis or carrageenan-induced rat paw edema. In contrast, given intraperitoneally, both reduced brewer's yeast-induced hyperthermia in rats, but when given orally did not affect it. Moreover, the aqueous extract decreased the intestinal transit time in mice while the hydroalcoholic extract increased it. Finally, these extracts, given intravenously, reduced blood pressure and heart rate in rats; these effects could be blocked by atropine but not by co-administration of pyrilamine and cimetidine.

Administration, Oral↗
PubMed2002

Pharmacological evidence favouring the folkloric use of Diospyros mespiliformis Hochst in the relief of pain and fever.

The methanol extract of Diospyros mespiliformis was evaluated for its claimed folkloric usage in the relief of pain and fever. Antipyretic, analgesic and anti-inflammatory effects of the extract were evaluated in rats and mice. Studies were carried out on yeast-induced pyrexia in rats, acetic acid-induced writhing in mice, formalin test and egg albumin-induced anti-inflammatory activity in rats. The extract (50 and 100 mg/kg i.p.) gave a potent antipyretic effect for 100 mg/kg and significant activity (P<0.05) against all the analgesic and anti-inflammatory models used. The LD(50) of the extract was estimated to be 513.80+/-33.92 mg/kg i.p. in mice. These results provide support for the use of the plant in relieving pain and fever.

Animals↗
PubMed1991

Antipyretic activity of tebufelone (NE-11740) in man.

Tebufelone (formerly NE-11740) is a member of the new class of di-tert-butyl-phenol anti-inflammatory agents. It has previously been reported that this new agent has potent analgesic, antipyretic, and anti-inflammatory effects using in vitro, in vivo, and ex vivo experimental models. A randomized, active- and placebo- controlled double-blinded study in 120 healthy males, 20 to 55 years old, was conducted to clinically assess tebufelone's antipyretic activity. Subjects received a single peroral dose of placebo, 650 mg aspirin (ASA), or tebufelone at doses of 25, 50, 100, or 200 mg. Thirty minutes later, E. coli endotoxin (2 ng/kg) was administered intravenously. Oral temperatures were recorded at 15 minute intervals from 30 minutes post dosing to 8 hours post endotoxin administration. Areas under the temperature curves (AUCs), adjusted for baseline, were significantly lower than placebo for ASA and all but the 25 mg tebufelone groups. An AUC dose-response equation estimates 60 mg tebufelone as equivalent to 650 mg ASA, with 50 mg tebufelone not significantly greater than 650 mg ASA. Side effects, attributable to the endotoxin, included mild flu-like symptoms and were worse in the placebo group and the non-efficacious 25 mg tebufelone group. Doses of 100 and 200 mg tebufelone had onset characteristics indistinguishable from 650 mg ASA, whereas 50 mg tebufelone showed significantly slower onset while suppressing temperature for a longer period than ASA. These results provide an important early demonstration of tebufelone's biological activity in man.

Adult↗
PubMed1996

Combination analgesic-induced kidney disease: the Australian experience.

Analgesic nephropathy is a unique drug-induced kidney disease characterized pathologically by renal papillary necrosis and chronic interstitial nephritis, and is the result of excessive consumption of combination antipyretic analgesics. The clinical features of the disorder relate mainly to the papillary necrosis, renal colic, and obstructive uropathy and the development of chronic renal failure in a small percentage of patients. There are significant geographic variations in the clinical features that may be related to the differing combinations of analgesics. The pathogenesis of the disease is in part related to the kidneys' ability to concentrate drugs in the papillae. The following sequence of events presents a plausible explanation for the evolution of the disease. If a combination of phenacetin and aspirin is ingested, the following steps occur. Phenacetin is converted in the gut and liver to acetaminophen by first-pass metabolism. Acetaminophen is then taken up by the kidney and excreted. During its excretion, acetaminophen becomes concentrated in the papillae of the kidney during physiologic degrees of antidiuresis, the concentration being up to five times the intracellular concentration of other tissues. Acetaminophen undergoes oxidative metabolism by prostaglandin H synthase to a reactive quinoneimine that is conjugated to glutathione. If acetaminophen is present alone, there is sufficient glutathione generated in the papillae to detoxify the reactive intermediate. If the acetaminophen is ingested with aspirin, the aspirin is converted to salicylate and salicylate becomes highly concentrated in both the cortex and papillae of the kidney. Salicylate is a potent depletor of glutathione. The mechanism is not completely understood; however, the inhibition of the production of NADPH via the pentose shunt is a possible explanation. With the cellular glutathione depleted, the reactive metabolite of acetaminophen then produces lipid peroxides and arylation of tissue proteins, ultimately resulting in necrosis of the papillae.

Analgesics↗
PubMed1986

Activation of inhibition from the periaqueductal grey matter mediates central analgesic effect of metamizol (dipyrone).

The pyrazolone derivative, metamizol (dipyrone), possesses analgesic, antipyretic, anti-inflammatory and spasmolytic properties. It is often classified as peripherally acting. To test the possibility that a central action of the drug contributes to its antinociceptive and analgesic effects, experiments were carried out in which the tail-flick response to radiant heat, flexor reflex activity in the tibialis anterior muscle and activity in ascending spinal axons evoked by stimulation of afferent C fibres in the sural nerve, and activity of neurones in the periaqueductal grey matter and the substantia nigra were assessed in rats. Metamizol administered by intraperitoneal (i.p.; 10, 20 and 40 mg/kg) or intrathecal (i.t.; 50 to 400 micrograms) injection to intact rats dose-dependently prolonged the tail-flick latency. Administration by i.t. injection to spinal rats was without effect. Intravenous (i.v.) injection of metamizol (140 mg/kg) reduced flexor reflex activity in intact animals, while an i.t. injection to spinal rats was ineffective at a low dose (100 micrograms) or enhanced the reflex activity at a higher dose (400 micrograms). Activity in ascending axons responding to afferent C fibre stimulation was mostly depressed by i.t. injection of metamizol (40, 80 and 140 mg/kg) in rats with an intact spinal cord. Ascending activity was increased by i.t. injection of the drug (100 and 200 micrograms) to spinal rats. Metamizol (140 mg/kg) i.v. increased the activity of neurones in the PAG and reduced that of neurones in the substantia nigra. Metamizol administered by microinjection into the PAG prolonged the tail-flick latency (15-100 micrograms) and depressed C fibre-evoked activity in ascending axons (100 micrograms). The results suggest that a central action is involved in the analgesic effect of metamizol and that this central action manifests itself by an activation of inhibition originating in the PAG.

Action Potentials↗
PubMed1981

Research on heterocyclic compounds. X.-Imidazo[1,2-a]pyrazine derivatives: synthesis and antiinflammatory activity.

Since we had previously observed the considerable anti-inflammatory activity of imidazo[1,2-a]pyrazine 2-acetic acid, we prepared a series of imidazo[1,2-a]pyrazine derivatives, bearing some substituents on the pyrazine ring and a carboxylic, acetic or alpha-methylacetic moiety on the imidazole ring. These new compounds were tested for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

Analgesics↗