Coronary vasodilation with dihydropyridines--a pharmacokinetic study.
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.
Jost
S
S
Hannover Medical School, F.R.G.
Rafflenbeul
W
W
Mogwitz
B
B
Nellessen
U
U
Bossaller
C
C
Zwicky
P
P
Hecker
H
H
Lippolt
P
P
Lichtlen
P R
PR
D000328:Adult; D017023:Coronary Angiography; D003327:Coronary Disease / Q000000981:diagnostic imaging / Q000188:drug therapy* / Q000503:physiopathology; D003331:Coronary Vessels / Q000187:drug effects*; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D009543:Nifedipine / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D015737:Nisoldipine / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D014664:Vasodilation / Q000187:drug effects*
D015737:Nisoldipine; D009543:Nifedipine