Noninvasive assessment of the haemodynamic effects of nicardipine in normotensive subjects.

Abstract

1 Calcium antagonists reduce myocardial contractility in vitro. Nicardipine is a dihydropyridine derivative with enhanced selectivity for vascular smooth muscle. 2 We have studied the pharmacokinetics and the haemodynamic effects that occur in man following bolus intravenous administration of nicardipine. 3 Ten normotensive male subjects received either nicardipine or placebo i.v., allocated in a randomised double-blind manner, over 60 s 4 Plasma nicardipine concentration, blood pressure, heart rate, and systolic time intervals were measured before dosing and at frequent intervals between I and 360 min post dosing. 5 At 160 jug kg-', adequate plasma levels of nicardipine were obtained to permit analysis of individual pharmacokinetic variables, and significant and consistent haemodynamic effects were seen. 6 After injection ofnicardipine, systolic BP and the QS2 (measure of total electromechanical systole) and QT intervals were not altered. 7 The changes in BP and heart rate were consistent with arteriolar vasodilatation. 8 The changes in PEP and LVET suggest an increase in cardiac contractility, which is unlikely to be a direct effect of nicardipine on the myocardium but rather a result of afterload reduction. 9 The close correlation of nicardipine plasma level with haemodynamic effect should permit accurate dose titration. 10 The net increase in contractility should allow nicardipine to be administered safely with fi-adrenoceptor blocking drugs.Keywords blood pressure calcium antagonist heart rate nicardipine systolic time intervals concentration effect modelling

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