[Change in the diameter of the coronary vessels following sublingual or intravenous nifedipine administration correlated with the plasma level].
The diameter changes of angiographically normal epicardial coronary arteries were studied in 25 patients in correlation to nifedipine plasma levels. In group 1 (15 patients) 20 mg of s.l. nifedipine were administered. Measurements of the coronary lumen size (automated contour detection system, accuracy 0.12 mm) and detection of plasma levels (gas-chromatography) were done before and 10, 20 and 30 min after drug administration. According to the slope of nifedipine plasma levels, patients were divided into group 1 A (n = 4) and 1 B (n = 11). Plasma levels in both groups were: at 10 min, 27.8 +/- 9.8 and 13.5 +/- 4.5 ng/ml resp.; P less than 0.05; at 20 min, 54.0 +/- 11.7 and 21.7 +/- 6.6 ng/ml resp.; P less than 0.001; at 30 min, 79.1 +/- 9.3 and 28 +/- 9.8 ng/ml resp.; P less than 0.001. The corresponding diameter changes in A and B were: 7.3 +/- 5.1%/.-5.6 +/- 9.0% resp.; P less than 0.01; 11.4 +/- 4.1% and -4.5 +/- 11.3% resp.; P less than 0.01; 14.5 +/- 5.9% and 0.5 +/- 13.6% resp.; P less than 0.05. In group 2 (10 patients) 1 mg nifedipine was administered intravenously within 4 min. Measurements were done at 1 min intervals during infusion as well as 7 and 15 min after beginning and compared to a placebo group (n = 10). Peak plasma levels amounted to 16.7 +/- 5.7 ng/ml after 7 min. The maximum coronary dilation was reached after 4 min (verum 5.0 +/- 6.8%; placebo 3.2 +/- 3.6%). Significant differences between both groups were observed after 7 min (verum 4.1 +/- 5.3%; placebo -3.1 +/- 5.8%, P less than 0.05) and 15 min (verum 1.2 +/- 3.2%; placebo -6.2 +/- 8.4%; P less than 0.05).


CONCLUSIONS
based on significantly different plasma levels following sublingual application of 20 mg nifedipine a classification of patients into "early-" and "late-coronary-responders" could be established. After intravenous infusion of 1 mg nifedipine peak plasma levels were much lower than after sublingual application of 20 mg and coronary diameters showed only a mild increase.
D000284:Administration, Oral; D003326:Coronary Circulation / Q000187:drug effects; D003327:Coronary Disease / Q000097:blood / Q000188:drug therapy*; D003331:Coronary Vessels / Q000187:drug effects*; D005260:Female; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008875:Middle Aged; D009543:Nifedipine / Q000008:administration & dosage* / Q000097:blood
D009543:Nifedipine
Koronarweitenänderung nach sublingualer und intravenöser Nifedipinapplikation in Korrelation zu Plasmaspiegeln.