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Serum concentrations and effects of (±)‐nicardipine compared with nifedipine in a population of healthy subjects
Author(s) -
Porchet Hervé C,
Dayer Pierre
Publication year - 1990
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1990.130
Subject(s) - nicardipine , nifedipine , dihydropyridine , blood pressure , medicine , antagonist , pharmacology , crossover study , heart rate , chemistry , anesthesia , endocrinology , calcium , placebo , receptor , alternative medicine , pathology
The dihydropyridine calcium antagonist (±)‐nicardipine shares some of the pharmacologic properties of the dihydropyridine prototype nifedipine. To compare them, serum concentrations and cardiovascular effects of 10 mg nifedipine and 20 mg (±)‐nicardipine were evaluated at 1, 2, and 3 hours after oral intake in a randomized, crossover, single‐blind study involving 79 healthy volunteers. (±)‐Nicardipine serum concentrations were much lower than those of nifedipine, indicating a greater hepatic first‐pass metabolism of (±)‐nicardipine. There was a significant correlation between serum concentrations of both drugs. The frequency distributions of nifedipine and (±)‐nicardipine AUC(0–3), heart rate increase, and mean arterial pressure decrease showed no bimodality. This does not confirm the proposed polymorphism of nifedipine oxidation. Concentration‐effect plots indicate that (±)‐nicardipine is more potent than nifedipine but shows comparable efficacy in blood pressure reduction. Clinical Pharmacology and Therapeutics (1990) 48 155–160; doi: 10.1038/clpt.1990.130