Document Detail


Felodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension.
MedLine Citation:
PMID:  3069435     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Felodipine is a dihydropyridine calcium antagonist which selectively relaxes vascular smooth muscle. By acting at peripheral arterioles, it lowers systemic vascular resistance and thereby produces substantial decreases in blood pressure and increases in cardiac output. Felodipine is indicated for the management of hypertension, and in patients with mild to moderate disease felodipine monotherapy markedly lowers blood pressure. It proved as effective as atenolol, and equivalent to hydrochlorothiazide, either with or without amiloride, in terms of antihypertensive activity. Comparative studies also demonstrated that once daily administration with an extended-release formulation provides equivalent antihypertensive efficacy to the same amount of drug administered twice daily as the standard tablets. As a second- or third-line treatment for patients with moderate to severe hypertension refractory to standard drug combinations, felodipine produced considerable reductions in blood pressure when added to beta-blockers and diuretics, either alone or in combination, in studies lasting up to 48 weeks. In comparative studies of multiple-drug treatments felodipine was found to have superior efficacy to hydralazine and prazosin, and was at least as effective as nifedipine, minoxidil and propranolol, when used with diuretics and/or beta-blockers. As an alternative to hydrochlorothiazide, in combination with beta-blockers, felodipine consistently controlled blood pressure in a greater percentage of patients and usually provided greater decreases in blood pressure. The main side effects with felodipine are ankle oedema, headache and flushing. Although the overall incidence of effects is quite high, they are usually mild in nature. Nevertheless, withdrawal due to side effects has been necessary in about 7% of patients overall. Thus, the efficacy of felodipine has been demonstrated in mild, moderate and severe hypertension. At the present time it seems particularly suitable as a second- or third-line treatment in refractory hypertension, but it also can be used as monotherapy for mild to moderate disease.
Authors:
E Saltiel; A G Ellrodt; J P Monk; M S Langley
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Drugs     Volume:  36     ISSN:  0012-6667     ISO Abbreviation:  Drugs     Publication Date:  1988 Oct 
Date Detail:
Created Date:  1989-05-02     Completed Date:  1989-05-02     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  7600076     Medline TA:  Drugs     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  387-428     Citation Subset:  IM    
Affiliation:
Cedars-Sinai Medical Center, Los Angeles, California.
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MeSH Terms
Descriptor/Qualifier:
Felodipine
Humans
Hypertension / drug therapy*
Metabolic Clearance Rate
Nitrendipine / analogs & derivatives*,  pharmacokinetics,  pharmacology,  therapeutic use
Chemical
Reg. No./Substance:
39562-70-4/Nitrendipine; 72509-76-3/Felodipine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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