Plasma concentration-effect relationships of intravenous and extended-release oral felodipine in hypertensive patients

Journal of Cardiovascular Pharmacology
E BlychertD Elmfeldt

Abstract

Felodipine, a dihydropyridine calcium antagonist, was given double-blind in a crossover design comparing once-daily doses of 20 mg felodipine extended-release (ER) tablets with placebo in 12 hypertensive patients. A 2-h intravenous infusion was given after a placebo washout. After oral felodipine, blood pressure (BP) was significantly lower than after placebo, both after the first dose and after 2 weeks of treatment. Supine BP 24 h after the first dose of placebo and felodipine was 159/97 and 153/92 mm Hg (p less than 0.01/0.05), respectively. Corresponding BPs at 2 weeks were 158/99 and 144/89 mm Hg (p less than 0.01/0.01). Approximately 75% of the maximal and 60% of the trough effect at steady state were obtained already after the first dose. The plasma concentration (CpF) vs. time curve after felodipine ER was relatively flat. After oral felodipine, a linear correlation was found between BP reduction and logarithmic CpF. After intravenous administration, CpF correlated well with a hyperbolic function. These data indicate that there is an almost linear relation between BP reduction and log CpF in the range from 2-20 nmol/L, and that little additional effect is to be expected above approximately 20 nmol/L. No hysteresis was fo...Continue Reading

Citations

Jan 1, 1997·Cardiovascular Drugs and Therapy·H Scholz
Jan 1, 1991·British Journal of Clinical Pharmacology·E BlychertT Hedner
Oct 31, 2002·CMAJ : Canadian Medical Association Journal = Journal De L'Association Medicale Canadienne·J David Spence
Jan 15, 1992·The American Journal of Cardiology·Y S HwangE C Wong
Nov 19, 2005·Scandinavian Journal of Gastroenterology·Juhani SandIsto Nordback
Nov 1, 1991·DICP : the Annals of Pharmacotherapy·K C Yedinak, L M Lopez
Sep 2, 1998·British Journal of Clinical Pharmacology·D G BaileyJ D Spence

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