Kinetics and metabolism of sulfinpyrazone
- 1 April 1983
- journal article
- research article
- Published by Springer Nature in Clinical Pharmacology & Therapeutics
- Vol. 33 (4) , 491-497
- https://doi.org/10.1038/clpt.1983.67
Abstract
Normal subjects (3 men and 3 women) took 200 mg sulfinpyrazone in 2 oral preparations, a capsule and a suspension. Plasma and urine levels of sulfinpyrazone and the sulfide, p-hydroxy and sulfone metabolites were measured over 3 days. The plasma sulfinpyrazone/time concentration profiles indicated a postabsorptive biexponential decline with a mean terminal half life (t1/2) of 299 .+-. 107 min. There was intersubject variation in the formation of the metabolites, the greatest being with the sulfide metabolite. Mean t1/2 of the sulfide metabolite was 659 .+-. 192 min. The apparent fraction of sulfinpyrazone absorbed was 0.93 .+-. 0.24 and the free fraction in plasma was 1.26 .+-. 0.04%. Since the sulfide metabolite has a more potent antiplatelet effect and its formation in normal subjects is variable, direct administration of the sulfide may provide a more predictable antithrombotic effect in patients.This publication has 0 references indexed in Scilit: