Differences in nifedipine concentration-effect relationship between capsule and slow release tablet administration.

摘要: The relationships between nifedipine plasma concentrations and its hypotensive positive chronotropic effects were studied in healthy volunteers who received either a 10 mg capsule (CAP) or 20 slow release tablet (SRT). Plasma rose more rapidly after CAP than SRT, Cmax being 131 +/- 39 40 7 ng/ml tmax 0.5 0.07 1.8 0.4 h, respectively. Both formulations produced reduction diastolic blood pressure which exhibited significant linear correlation (p 0.45). Since the measured decrease is outcome of nifedipine-induced vasodilation homeostatic responses, results are interpreted as follows. Fast input induced brisk change physiological conditions hence triggered an important response, visualized heart rate increase, partially offset effect. With there was gradual producing lesser activation compensatory mechanisms therefore effect less antagonized with CAP. Nifedipine SRT does not only exhibit pharmacokinetic advantages, but also favorable pharmacodynamic profile