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European Heart Journal 1989 10(Supplement F):147-152; doi:10.1093/eurheartj/10.suppl_F.147
Copyright © 1989 by the European Society of Cardiology.
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© 1989 The European Society of Cardiology

Coronary vasodilation with dihydropyridines—A pharmacokinetic study

S. Jost, W. Rafflenbeul, B. Mogwitz, U. Nellessen, C. Bossaller, P. Zwicky, H. Hecker, P. Lippolt and P. R. Lichtlen

Hannover Medical School Hannover, F.R.G.

Address for reprints: Dr Stefan Jost, Medizinische Hochschule Hannover, Abteilung Kardiologie, Postfach 61 01 80, D-3000 Hannover 61, F.R.G.

In 26 patients with coronary artery disease, the mean diameters of angiographically ‘normal’ epicardial coronary arteries were assessed with the aid of a computer-assisted contour detection system (CAAS) before and up to 15 min after onset of a 4-min intravenous-infusion of 2mg nifedipine (13 patients, group I) or 1 mg nisoldipine (13 patients, group II). Maximal coronary dilation amounted to 20±9% (4th min) in group I and to 18±9% (15th min) in group II. In addition, in group II changes of the minimal diameters of 9 coronary obstructions were measured; the maximum increase averaged 28±15% (7th min). In order to compare the pharmacokinetic properties of these compounds the dilation of the ‘normal’ coronary segments was correlated with the respective drug plasma levels; maximal plasma concentrations averaged 62±21 ng ml–1 (7th min) in group I and 17±7 ng ml–1 (4th min) in group II respectively. A positive, linear correlation between coronary dilation and plasma levels was only found with nifedipine (P<0·05); with nisoldipine, however, coronary dilation developed in form of a hysteresis curve, when plotted against plasma levels, probably due to the high receptor affinity of this substance.

The prolonged efficacy of nisoldipine could be favourable in oral long-term treatment of patients with coronary artery disease.

Key Words: Nisoldipine • nifedipine • coronary vasomotor tone • pharmacokinetics • dihydropyridines


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