Description
Felodipine is a vasodilatory calcium antagonist with a high degree of vascular selectivity.
It is currently indicated for use only in hypertension, either as monotherapy or in
conjunction with diuretics or beta blockers.
Chemical Properties
White or Light Yellow Crystalline Powder
Originator
Astra (Sweden)
Uses
Zanarnivir influenza prophylaxis and therapy
Uses
vasodilator, Ca channel blocker
Uses
Felodipine is used as a dihydropyridine calcium channel blocker. It displays high vascular selectivity; lowers arterial blood pressure without altering cardiac contractility. Antihypertensive.
Definition
ChEBI: The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth m
scle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.
Manufacturing Process
Preparation of 2,3-dichlorobenzylideneacetylacetic acid-methylester.
2,3-Dichlorobenzaldehyde is reacted with methyl acetoacetate in a suitable
solvent in the presence of a catalytic amount of acetic acid and piperidine.
Water is azeotropically separated off during the reaction. The reaction mixture
is extracted in order to remove the catalysts. The solvent is evaporated and
methanol is added. The product is crystallized by cooling the solution, isolated
by filtration and finally washed with methanol.
brand name
Plendil (AstraZeneca).
Therapeutic Function
Antihypertensive
General Description
Felodipine, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethylmethyl ester (Plendil), is a second-generation dihydropyridinechannel blocker of the nifedipine type. It is more selectivefor vascular smooth muscle than for myocardial tissueand serves as an effective vasodilator.
Biological Activity
L-type Ca 2+ channel blocker that is selective over N-, R-, P/Q- and T-type channels. Displays high vascular selectivity; lowers arterial blood pressure without altering cardiac contractility. Antihypertensive.
Clinical Use
Felodipine is used inthe treatment of angina and mild-to-moderate essential hypertension.Felodipine, like most of the dihydropyridines,exhibits a high degree of protein binding and has a half-liferanging from 10 to 18 hours.
References
1) Todd and Faulds, (1992)?Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders; Drugs?44?251
2) Furukawa?et al. (1999)?Selectivities of Dihydropyridine Derivatives in Blocking Ca2+ Channel Subtypes Expressed in Xenopus Oocytes; J. Pharmacol. Exp. Ther.?291?464
