The antihypertensive effect and pharmacokinetics of nilvadipine (FK235) in essential hypertension.

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Nilvadipine, a new calcium channel blocking agent, was compared with nicardipine regarding antihypertensive effect and pharmacokinetic profile in essential hypertensiye patients after single administration. Nilvadipine at doses of 6 mg and 4 mg was compared with nicardipine 20 mg using a randomized crossover procedure. Nilvadipine at 6 mg doses was more potent and longer-lasting in antihypertensive effect than nicardipine. On the other hand, nilvadipine at 4 mg doses was comparable to nicardipin although its duration was a little longer. There was a good linear correlation between plasma concentration and antihypertensive effect of nilvadipine. The minimum effective plasma concentration (MEPC) of nilvadipine inducing 7% decrease in mean blood pressure was estimated to be 0.5-0.7 ng/ml. The adverse effects observed by nilvadipine were transient and not clinically significant. However, adverse effects by nilvadipine at doses of 6 mg occurred a bit more frequently than by nicardipine.<BR>The antihypertensive effect and pharmacokinetic profile of nilvadipine were also studied after multiple administration in the hypertensive patients. Nilvadipine was given in the dosage regimen of 4 mg b.i.d. for 6-10 days. The plasma concentration at 12 hours after dosing on the final day of treatment was consistent with MEPC followed by prolonged antihypertensive effect.<BR>These data show that nilvadipine is a potent antihypertensive drug, and suggest anoptimal dosage regimen of nilvadipine in essential hypertension at 4 mg or less, b.i.d..
一般社団法人日本臨床薬理学会の論文

The antihypertensive effect and pharmacokinetics of nilvadipine (FK235) in essential hypertension.

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