Felodipine (Plendil@/Flodil@/Modip@, Astra) is a highly vascular selective calcium antagonist of the dihydropyridine type. At present, some 300 clinical studies involving more than 8,000 patients have been carried out with felodipine, the majority with hypertension but a substantial number also with other indications, such as angina pectoris and heart failure.In the early clinical studies, felodipine was given as conventional tablets twice daily. However, since 1986, most studies with felodipine have been performed using the extended-release formulation of the drug, which provides smoother plasma concentrations and 24-h blood pressure control with a once-daily dosage (11,37,38). This is the only formulation currently on the market.In controlled clinical trials, felodipine extended release once daily was found to be an effective antihypertensive treatment and reduced the blood pressure to S 9 0 mm Hg, 24 h after the dose, in 50430% of patients (13,22,41,65,82,106). Treatment with felodipine was reported to be more effective than with nifedipine, enalapril, chlorthalidone, or hydrochlorothiazide, but similarly effective to amlodipine, diltiazem, metoprolol, or aten-0101, at the doses studied (22,41,45,65,67,72,82,106,111). The aim of this article is to provide an overview of the experience with felodipine with regard to tolerability profile, effect on quality of life, safety in patients with diseases commonly occurring together with hypertension, effect on hormonal, metabolic, and laboratory variables, and interactions with food and drugs.
PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIESFelodipine is a highly vascular selective dihydropyridine calcium antagonist. It has been shown to be over 100 times more potent in vascular than in cardiac muscle with a selectivity ratio nearly 10 times higher than that for the dihydropyridines nifedipine and amlodipine (73,87). In clinical studies, felodipine has been found to produce significant
