PHARMACOKINETICS AND PHARMACODYNAMICS OF A NEW CALCIUM CHANNEL BLOCKER MPC-1304 IN HYPERTENSIVE SUBJECTS

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Abstract
The pharmacokinetic and pharmacodynamic properties of a new calcium channel blocker MPC-1304 (MPC) were examined following a single 10 mg oral dose of MPC in six hypertensive subjects. Blood samples for measurement of MPC and its active metabolite (MPC-Keto-H2) were obtained, and blood pressure was measured just before and at 1, 2, 4, 6, 8, 12 and 24 h after administration. Plasma concentrations of MPC-Keto-H2 were significantly higher than those of MPC at every observation point. The value of maximum plasma concentration of MPC-Keto-H2 was 10 times greater than that of MPC. The antihypertensive effect of MPC was observed at 4 h after administration and persisted up to 8 h. A plot of plasma concentrations of MPC versus reductions in blood pressure showed an anticlockwise hysteresis loop. These results suggest that the active metabolite MPC-Keto-H2 contributes in part to the antihypertensive action of MPC, the delayed distribution of MPC into the effector site, or both.

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