本態性高血圧症に対するNilvadipine (FK235) の降圧効果と薬物動

抄録

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.
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.
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..