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[Anti-inflammatory, analgesic and antipyretic properties of nonachlazine].

Nonachlazin diminishes aseptic inflammation provoked by subplantar administration of carrageenin to rats. Nonachlazin increases the sensitivity pain threshold of the rat paw affected by carrageenin-induced inflammation, decreases the reaction of mice to intraperitoneal injection of phenylchinoin, and the ability of the rabbit central nervous system for impulse summation. Nonachlazin prevents carrageenin-induced temperature rise in rats.

Animals↗

[Correlation of the antiexudative, analgesic and antipyretic components in the action of nonsteroid anti-inflammatory preparations].

Experimental carragenin paw edema in rats, crams in rats induced by acetic acid, and yeast fever in rats were used to study antiexudative, analgetic and antipyretic action of 9 present-day non-steroidal anti-inflammatory drugs (acetylsalicylic acid, amidopyrin, analgin, phenylbutazone, mephenamic acid, voltaren, ibuprofen, indomethacin, naproxen). The correlation of individual types of anti-inflammatory activity was characterized in each drug. Of the drugs studied, the most pronounced anti-inflammatory action was exhibited by voltaren; indomethacin and naproxen were found to be less active. It was shown that the methods for the appraisal of the drugs activity make it possible to study not only their anti-inflammatory activity but also the effect on the inflammation mediators.

Animals↗

[Synthesis of pyrazole derivatives and pyrazolo[4,3-d]pyrimidines. I].

Three series of pyrazole derivatives (III a-g), (IV a-g) and (V a-g) were synthesized and tested for analgesic, antipyretic and antiinflammatory activity. Many of tested compounds showed interesting analgesic and antipyretic activity, whereas no compounds exhibited any antiinflammatory activity.

Animals↗

Pharmacokinetics and pharmacodynamics in the design of controlled-release beads with acetaminophen as model drug.

Relationships between pharmacodynamics (drug concentration and effect) and pharmacokinetics were used to develop an oral, controlled-release-bead dosage form. Reported pharmacodynamic data were used with pharmacokinetic curves to identify effective therapeutic drug concentrations for optimum therapy for a drug with a "deep tissue" effective compartment. The commonly used, over-the-counter, non-narcotic, analgesic-antipyretic acetaminophen (APAP) was used as the model drug. Data reported in the literature were used to compare analgesic and antipyretic efficacy. Computer simulations were performed with MAXSIM (version 3.01) to suggest a zero-order drug release useful for a 12-h, oral, sustained-dosage form for antipyretic therapy in children, on the basis of current pediatric dosing of APAP. Coated APAP beads with the desired release rate were then developed with fluid-bed coating technology.

Acetaminophen↗

Analgesic abuse in the elderly. Renal sequelae and management.

Nephropathy caused by the use of 'classical' analgesics [paracetamol (acetaminophen), salicylates and pyrazolone derivatives] and renal impairment associated with nonsteroidal anti-inflammatory drugs (NSAIDs) are important health problems in the elderly. Classical analgesic nephropathy is a chronic renal disease characterised by renal papillary necrosis and chronic interstitial nephritis. The nephropathy is caused by the excessive consumption of analgesic mixtures containing at least 2 antipyretic analgesics combined with caffeine and/or codeine. The use of NSAIDs is associated with a wide range of tubular, interstitial, glomerular and vascular renal lesions. Despite the well-characterised acute biological effects of NSAIDs on the kidney, there is only limited evidence that they are associated with an increased risk of chronic renal failure. Classical analgesic toxicity can be effectively prevented by limiting the availability of over-the-counter analgesic mixtures containing 2 analgesic compounds in combination with potentially addictive substances (e.g. caffeine and/or codeine). In the elderly in particular, the prolonged, regular use of NSAIDs should be discouraged. Patients starting NSAID therapy should be monitored regularly and drug interactions should be avoided.

Aged↗

Endosprin, an antipyretic, antiinflammatory and analgesic preparation of lysine salicylate: reassessment of its chemical composition and effects in experimental animals in comparison with aspirin.

Endosprin, an antiinflammatory-antipyretic-analgesic salicylate drug marketed in Brazil since 1970, has been shown by NMR-1H spectral analysis to contain salicylic acid and not, as formerly believed, acetylsalicylic acid (aspirin). Its analgesic and antiinflammatory activity in mice and rats was similar to that of aspirin but its antipyretic activity against bacterial pyrogen fever in rabbits was significantly lower than that of aspirin. This result stands in contrast to the large body of clinical evidence indicating a rather high degree of effectiveness of Endosprin in lowering fever of various origin in children.

Animals↗

Influence of various substances on prostaglandin biosynthesis by guinea-pig chopped lung.

Guinea-pig chopped lung tissue was used to investigate the inhibitory effect of various steroidal and non-steroidal anti-inflammatory agents, antipyretics, analgesics, local anaesthetics and psychotropic drugs on mechanically induced release of prostaglandin-like material. Low concentrations of non-steroidal anti-inflammatory agents inhibited synthesis, but other antipyretics and analgesics, and the local anaesthetics had little effect. Thymoleptics, neuroleptics and monoamine oxidase inhibitors except phenelzine exhibited weak activity. It is concluded that the method is a useful pharmacological model to study prostaglandin biosynthesis. The weak effects of the psychotropic drugs suggest that they do not exert their clinical effect by inhibiting PG biosynthesis.

Analgesics↗

[Paracetamol. Present status of knowledge in 1989].

Today paracetamol (acetaminophen), the oldest known synthetic analgesic-antipyretic drug, is one of the most frequently used around the world. The present general review presents the essential knowledge about this drug which has accumulated during the last decade, 1978 from to 1988. It includes recent data concerning toxicity, pharmacokinetics, mechanisms of analgesic and antipyretic action, and therapeutic efficacy. Readers interested in the original papers are referred to 264 bibliographical references.

Acetaminophen↗

Acetylsalicylic acid and acetaminophen.

Aspirin is the most extensively prescribed analgesic, antipyretic, and anti-inflammatory agent. It is effective against the mild-to-moderate pain of inflammation. The best single dose of aspirin is that which is adequate to relieve pain; the proper dosage interval is that which sustains relief without causing toxicity. It would be unfortunate to withhold aspirin from a patient who desperately requires the relief provided by this most useful analgesic because there have been some adverse effects when it is used improperly. Acetaminophen is a suitable substitute for aspirin for its analgesic or antipyretic uses in patients in whom aspirin is contraindicated (e.g., prepartum patients, children with febrile conditions, patients with asthma, peptic ulcer, gouty arthritis, hyperuricemia, hemophilia or other bleeding disorders, and those taking anticoagulants). However, the general substitution of acetaminophen for aspirin as an analgesic is not recommended.

Acetaminophen↗