Coronary vasodilation with dihydropyridines--a pharmacokinetic study

• Published in: European heart journal Vol. 10 Suppl F; p. 147
• Main Authors: Jost, S, Rafflenbeul, W, Mogwitz, B, Nellessen, U, Bossaller, C, Zwicky, P, Hecker, H, Lippolt, P, Lichtlen, P R
• Format: Journal Article
• Language: English
• Published: England 01.11.1989
• Subjects: Adult; Coronary Angiography; Coronary Disease - diagnostic imaging; Coronary Disease - drug therapy; Coronary Disease - physiopathology; Coronary Vessels - drug effects; Female; Hemodynamics - drug effects; Humans; Male; Middle Aged; Nifedipine - blood; Nifedipine - pharmacokinetics; Nifedipine - therapeutic use; Nisoldipine - blood; Nisoldipine - pharmacokinetics; Nisoldipine - therapeutic use; Vasodilation - drug effects
• ISSN: 0195-668X
• DOI: 10.1093/eurheartj/10.suppl_F.147

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 2 mg 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 less than 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.