Studies on Factor Affecting Pharmacokinetics of Cilostazol and Pharmacokinetics-Pharmacodynamics Analysis Based Platelet Aggregation.

Cilostazol is being developed for the treatment of intermittent claudication due to peripheral arterial disease (PAD). In this study, we measured the serum cilostazol concentrations and platelet aggregations induced by adenosine diphosphate (ADP) and collagen, and also investigated the pharmacokinetics and pharmacodynamics of cilostazol in inpatients receiving cilostazol therapy. No significant difference was observed in C/D (serum trough concentration/dose) between males and females. A trend toward increasing the serum cilostazol concentration by increasing the dose (mg/kg) was observed (P<0.05). The interindividual variation of the C/D for cilostazol was found to be very large. No significant difference was observed between the C/D for cilostazol and the age, GPT or Ccr. A statistical correlation was observed between the serum cilostazol concentration and the maximum extent of aggregation (%) induced by ADP and collagen (P<0.05).