Correlation between inhibitory effect on platelet aggregation and disposition of sulfinpyrazone and its metabolites...

In a crossover study rabbits were given perorally sulfinpyrazone (SO) and the sulfide metabolite (S) every 24 h for 5 days on separate occasions and inhibition of aggregation was measured. The results showed: the dosage regimen is effective if the minimum effective concentration of S is defined to be between 0.5-1.0 microgram ml-1, and the repeated dosing did not cause changes in disposition kinetics except that the terminal half-life of S was reduced after dosing with S. No significant accumulations in trough concentration and inhibition of aggregation were observed. The results obtained in this study could provide some useful information for design of dosage regimen and blood level monitoring for humans.