Biomaterial Database

Felodipine clinical pharmacokinetics. 1991

P H Dunselman, and B Edgar

Department of Cardiology, Ignatius Hospital, Breda, The Netherlands.

Absorption of felodipine is rapid and complete. A pronounced first-pass metabolism results in a bioavailability of 15%, irrespective of the oral formulation used. The peak plasma concentrations and area under the plasma concentration-time curve are linearly related to the dose. The variability in plasma concentrations is wide, and individualization of the dosage is recommended. Plasma felodipine concentrations are increased in the elderly, and in patients with congestive heart failure or liver cirrhosis; in these patients felodipine should be started at a low dosage. Food intake has no clinically significant effect on felodipine absorption. Serum digoxin concentrations are increased by felodipine in plain tablet form, but not when it is administered as extended release tablets. Activators, inducers and inhibitors of the cytochrome P450 system affect the plasma concentrations of felodipine. No displacement reactions with high affinity protein binding drugs have been observed. There is a significant correlation between plasma concentration and haemodynamic effect. The mean elimination half-life of 24h together with the extended release formulation of felodipine favours once-daily dosage in patients with hypertension.

UI	MeSH Term	Description	Entries
D007408	Intestinal Absorption	Uptake of substances through the lining of the INTESTINES.	Absorption, Intestinal
D012016	Reference Values	The range or frequency distribution of a measurement in a population (of organisms, organs or things) that has not been selected for the presence of disease or abnormality.	Normal Range,Normal Values,Reference Ranges,Normal Ranges,Normal Value,Range, Normal,Range, Reference,Ranges, Normal,Ranges, Reference,Reference Range,Reference Value,Value, Normal,Value, Reference,Values, Normal,Values, Reference
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004347	Drug Interactions	The action of a drug that may affect the activity, metabolism, or toxicity of another drug.	Drug Interaction,Interaction, Drug,Interactions, Drug
D005243	Feces	Excrement from the INTESTINES, containing unabsorbed solids, waste products, secretions, and BACTERIA of the DIGESTIVE SYSTEM.
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001682	Biological Availability	The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.	Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D015394	Molecular Structure	The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.	Structure, Molecular,Molecular Structures,Structures, Molecular
D015736	Felodipine	A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.	Agon,Felo Biochemie,Felo-Puren,Felobeta,Felocor,Felodipin 1A Pharma,Felodipin AL,Felodipin AZU,Felodipin AbZ,Felodipin Dura,Felodipin Heumann,Felodipin Stada,Felodipin Von Ct,Felodipin-Ratiopharm,Felodur,Felogamma,Fensel,Flodil,H 154-82,Modip,Munobal,Perfudal,Plendil,Renedil,Felo Puren,Felodipin Ratiopharm,H 154 82,H 15482,Heumann, Felodipin,Von Ct, Felodipin