Pharmacodynamic and pharmacological effects of MPC-1304, a new calcium channel blocker, in healthy subjects. Results of single oral administration.:Results of Single Oral Administration

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The pharmacodynamic and pharmacological effects of MPC-1304, a new calcium channel blocking agent were studied in 6 healthy adult volunteers. Each subject received a single oral dose (1.25, 2.5, 5, 10, 20 mg) at two-week intervals. Pharmacokinetics of MPC-1304 was assessed by measuring plasma and urine concentrations of MPC-1304 itself and its metabolites. The plasma concentration of MPC-1304-keto-H2, the active metabolite, was approximately 10-20 times that of MPC-1304 itself. The maximum plasma concentration (Cmax) of MPC-1304 and MPC-1304-keto-H2 were dosedependent and their time to peak level (tmax) was 3.8-4. 8 hr and 4.8-6.0 hr and the elimination half-lives (t1/2) were 1.0-1.1 hr, 2.7-3.4 hr, respectively. MPC-1304 and five metabolites were found in urine after single administration. The percent excretion ratio of MPC-1304 and its metabolites in 24-hr urine was 6: 1-7.9%, independent of doses. Following a single administration of 5-20 mg of MPC-1304, blood pressure was lowered during 2-24 hr and heart rate was transiently increased. Subjective symptoms (e. g. headache and dull-headedness) were observed after 10 mg and 20 mg dosing. There were no remarkable abnormalities in laboratory findings during the study. These results suggested the MPC-1304 would be a safe calcium channel blocker with hypotensive effect.
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