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At least 91 records · Page 5Linked to original sources
PubMed1986

High-affinity binding of ethacrynic acid is mediated by the two most important drug binding sites of human serum albumin.

The binding of ethacrynic acid to human serum albumin was investigated by means of circular dichroism and equilibrium dialysis measurements, using native human serum albumin and albumin derivatives with chemical modifications impairing specifically drug binding to the indole and benzodiazepine binding site or the azapropazone-warfarin binding area, respectively. The data presented indicate that the high-affinity binding of ethacrynic acid to human serum albumin is mediated by these two important drug binding sites. Accordingly, even at relatively low concentrations ethacrynic acid displaces other drugs from both binding sites.

Apazone↗
PubMed1980

Expectation and patient preference -- does it matter?

Admission to clinical trials is often based on the assumption of homogeneity of the population. A group of 60 patients, all with pain in the neck or shoulder of at least 3 months duration, were studied. Expectation was graded before treatments were started by sharing out 100 points between freedom from side effects, pain relief, depression relief, improved mobility, improved sleep and speed of action. A double-blind crossover study of two established anti-inflammatory analgesics and placebo was carried out. Using analogue scales, patients were asked to grade their response. Side effects were recorded, and preference was established at the end of the study.Although all the patients were in sufficient pain to require medical attention, some rated relief of depression, improvement in sleep or lack of side effects as more important than pain relief. Differences between drug and placebo were most clearly demonstrated in those patients whose main concern was improved mobility. In our view it is important to select patients who are in need of a dominant property of a drug for a trial of this property and this may have ramifications across the medical spectrum.

Apazone↗
PubMed1983

Early reports on drug interactions.

Letters in correspondence columns or brief reports in medical journals are an essential part of an early warning system, and they are invaluable in alerting clinicians and clinical pharmacists to associations between drugs and their reactions. A survey of the literature during the first half of 1982 has identified a number of these early reports; some are purely anecdotal, others may be coincidental, but all serve to warn the practitioner of potential hazard. Brief information on the following reports of drug-drug interactions is given in this article with the intention of giving these reports wider publicity and, possibly, encouraging further observation and research to establish or disprove their validity in a larger and wider range of patients or volunteer subjects. The following interactions are reviewed: amiodarone-quinidine, lidocaine-prenylamine, erythromycin-carbamazepine, azapropazone-phenytoin, chlordiazepoxide-levodopa, gentamicin-furosemide, ethanol-aspirin, acetaminophen-coumarin anticoagulant, and cimetidine-lidocaine.

Acetaminophen↗
PubMed1975

A comparative trial of azapropazone and ketoprofen in the treatment of acute backache.

A double-blind trial of azapropazone (300 mg. 4-times daily) and ketoprofen (50 mg. 4-times daily) was carried out in 50 patients with acute backache sufficiently severe to necessitate hospital admission. Of 39 patients who completed the full 3-weeks' study period, 18 preferred azapropazone therapy, 10 preferred ketoprofen, and 11 showed either preference for the intermediate placebo period or no preference at all. Ten patients suffered from sufficiently severe side-effects with ketoprofen to necessitate their withdrawal from the trial. There were no similar episodes of withdrawal occurring during the azapropazone period.

Acute Disease↗
PubMed1976

The pharmacology and pharmacokinetics of azapropazone - a review.

The pharmacology and pharmacokinetic properties of azapropazone, a new anti-inflammatory analgesic, are reviewed. Anti-inflammatory activity was assessed by standard in vivo and in vitro methods. The drug was shown to have definite activity with a potency approximately half that of phenylbutazone. Azapropazone was absorbed from the gastro-intestinal tract in animals and man, although wide inter-species variation in pharmacokinetic properties was noted. In man, the biological half life was approximately 20 hours. Azapropazone is not extensively metabolised and most metabolites have been identified and assayed.

Animals↗
PubMed1976

Toxicological studies on azapropazone.

The toxicity of azapropazone, a non-steroidal anti-inflammatory analgesic compound was studied in mice, rats, hamsters, guinea pigs, rabbits, cats, mongrel and beagle dogs, domestic pigs, rhesus monkeys, cynomolgus monkeys and baboons in experiments which ranged from acute, single-dose studies up to treatment periods of 1 year. The beagle dog was found to be especially sensitive to gastro-intestinal ulceration from azapropazone and this contrasted with the marked lack of gastro-intestinal hazard to other animals and particularly to the 3 primate species studied. The animal experiments did not indicate any potential risk to other body systems, and comparisons with other anti-inflammatory compounds, where these were made, suggest that azapropazone is at least as safe as other commonly-used agents. Azapropazone was not found to have teratogenic, carcinogenic or antimitotic activity and was shown not to produce local tissue damage.

Animals↗
PubMed1976

The determination of azapropazone in blood plasma.

Three methods for the determination of azapropazone were studied for the analysis of blood plasma samples taken after oral administration of azapropazone. A gas chromatographic method was compared with two simple spectrophotometric assay methods and the effect of metabolites of the drug on each method is described. It is concluded that metabolites are unlikely to cause significant interference with the two simple methods and that either is suitable for determination of plasma levels of the drug. Some problems associated with a gas chromatographic method are described and the comparative results of the examination of plasma samples using these methods are given.

Adult↗
PubMed1976

Clinical assessment of azapropazone in rheumatoid arthritis.

Azapropazone was investigated in a 2-week double-blind clinical out-patient trial against placebo in 23 patients with definite rheumatoid arthritis. The drug was given at a dose of 1200 mg. per day before food. At this dose level the drug was shown to have an antirheumatic effect in terms of pain relief, articular tenderness and duration of morning stiffness.

Administration, Oral↗
PubMed1976

An assessment of the therapeutic potential of azapropazone in rheumatoid arthritis.

A trial to compare the therapeutic potential of 1200 mg. azapropazone daily with 3.9 g. aspirin daily was carried out in 108 out-patients with rheumatoid arthritis over a 14-day period. Analysis of results from the 85 patients with completed assessment data (49 on azapropazone; 36 on aspirin) showed that azapropazone was better than aspirin from the point of view of pain relief, number of days patients were withdrawn prematurely from the trial, and patient satisfaction with treatment. The differences, however, were not statistically significant. The authors compare the results obtained in this trial with those obtained previously from trials with 13 other antirheumatic drugs using the same method.

Administration, Oral↗
PubMed1976

A comparative study of azapropazone and ibuprofen in the treatment of osteoarthrosis of the knee.

A double-blind crossover study in 41 patients with knee joint osteoarthrosis was carried out to compare the efficacy of 1200 mg. azapropazone per day with 1600 mg. ibuprofen per day. After an initial week on placebo, patients received one or other of the active medications for 2 weeks, then a 1-week placebo wash-out period before being crossed over to the alternative drug for a further 2 weeks. Objective assessments were made of knee joint movement, and of knee joint and thigh circumference. Patients made daily assessments of pain and a final overall assessment of preference for one or other treatment period. The results showed that azapropazone produced a significant improvement (p less than 0.05) in knee joint mobility over placebo, both active drugs were more effective than placebo (p less than 0.05) in providing pain relief, but that there was no significant difference between the two in these parameters. There was a highly significant patient preference, however, for azapropazone (p less than 0.01) compared to ibuprofen treatment periods. The most commonly reported side-effect with both drugs was dyspepsia, but in no case was it sufficiently severe to necessitate stopping treatment.

Adult↗