Effects of Ischaemic Heart Disease, Crohn’s Disease and Antimicrobial Therapy on the Pharmacokinetics of Sulphinpyrazone
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The renewed interest in sulphinpyrazone in recent years has arisen from its potential to inhibit platelet aggregation. In vivo much of the activity is probably due to the thioether or sulphide metabolite which has a greater potency and a longer half-life than the parent compound. The sulphide metabolite is formed exclusively by the gut microflora in man. The pharmacokinetics of sulphinpyrazone (200mg orally) have been studied, with particular attention to the formation of the sulphide metabolite, in groups of patients who might be expected to show abnormal formation of this active metabolite due to altered delivery of the drug to the lower gut or altered gut flora. Five patients studied 1 month after a myocardial infarction did not differ markedly from young, normal volunteers with respect to either sulphinpyrazone or its metabolite. Crohn’s disease in the quiescent phase did not significantly alter the pharmacokinetics or metabolism of the drug, but 1 patient who had undergone a hemicolectomy formed negligible concentrations of the active metabolite. Antimicrobial therapy produced highly variable results with almost complete suppression of sulphide formation in some subjects but no apparent effect in others.
KeywordsNormal Volunteer Amoxycillin Sulphasalazine Lincomycin Sulfinpyrazone
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- Anturan Reinfarction Italian Study Group. Sulphinpyrazone in post-myocardial infarction. Lancet 1: 237–242, 1982Google Scholar
- Crooks J, Stevenson IH (Eds). Drugs and the elderly: perspectives in geriatric clinical pharmacology, Macmillan Press Ltd, 1979Google Scholar
- Drasar BS, Hill MJ. Human intestinal flora, Academic Press, New York, 1984Google Scholar
- Kucers A, Bennett N (Eds). The use of antibiotics, William Heinemann Medical Books Ltd, London, 1979Google Scholar
- O’Malley K (Ed.). Clinical pharmacology and drug treatment in the elderly, Churchill Livingstone, Edinburgh, 1984Google Scholar
- Parsons RL, David JA. Gastrointestinal disease and drug absorption. In Prescott & Nimmo (Eds) Drug absorption. Proceedings of the Edinburgh International Conference, pp. 262–277, ADIS Press, Sydney, 1981Google Scholar
- Prescott LF. Clinically important drug interactions. In Avery (Ed.) Drug treatment, 2nd ed., pp. 236–262, ADIS Press, Sydney; Churchill Livingstone, London, 1980Google Scholar
- Westwick J, Webb H, Lewis GP. The effect of sulphinpyrazone, aspirin and their metabolites on prostacyclin production by rabbit aortic rings. Thrombosis and Haemostasis 42: 99, 1979Google Scholar