Inhibition of Human Platelet Function Induced by Sulphinpyrazone

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Abstract
A single 400 mg dose of sulphinpyrazone (S) administered orally to 5 volunteers inhibited arachidonic acid (AA)-induced platelet aggregation and platelet MDA production ex vivo biphasically. The initial inhibitory phase coincided with the maximum plasma concentration of S but the second phase occurred 24 h after dosing when no plasma S was detectable. At 2 h the concentration of AA inducing half-maximal aggregation was increased 1.95 times and at 24 h by 1.61 times. Dosing 7 volunteers with 200 mg q.d.s. for 7 days and 5 volunteers with 400 mg b.d.s. for 5 days also led to inhibitory activity against AA-induced platelet aggregation and MDA production which declined to zero 48 h after the last dose. Platelet count, fibrinogen, F VIII, β-TG and AT III were not influenced by the longer term treatment but bleeding time was slightly extended in all but one subject.

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