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Chemical Name Felodipine is a dihydropyridine
derivative and optically active described as (±)ethyl
methyl
4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-
pyridinedicarboxylate. Its empirical formula is C18H19Cl2NO4
with structural formula shown as:8
Pharmacology Felodipine is a calcium channel blocker which is thought to prevent the flow of calcium in the walls of smooth muscle cells which line small arteries. The effect of felodipine on blood pressure is principally a consequence of a dose-related decrease of peripheral vascular resistance in man, with a modest reflex increase in heart rate. With the exception of a mild diuretic effects seen in several animal species and man the effects of Felodipine are accounted for by its effects on peripheral vascular resistance.
Felodipine is a highest selective calcium
antagonist, which dilates the arteriolar resistance
vessels without significantly depressing cardiac
function5. It is a potent antihypertensive
agent and causes baroreflex readjustment as well as
regression of cardiac and vascular hypertrophy. In
addition, it exerts a diuretic/ natriuretic effect due
to a direct tubular action7. In elderly
hypertensive patients, felodipine not only can lower
blood pressure, but also be well tolerated. It does not
cause cardic orthostatic hypotension or impair cardiac
performance. These findings strongly suggest that
felodipine is a valuable antihypertensive vasodilating
calcium antagonist.
Proprietary Names a.Fensel®; Frodil®; Modip®; Munobal®; Perfudal®; Plendil®; Prevex®; Preslow®; Renedil®. b. Combination products: Lexxel® (felodipine, enalapril); Logimax® (felodipine, metoprolol); Unimax® (felodipine, ramipril). ²
Technical
package and impurity profiles are available upon
request. ² Sales to countries without patent issues only. ² Patent application is in process.
References 1.
Collets P. et al. Drugs 1985, 29 (s2) 124-130. 2.
Culling W. et al. Br. Heart J. 1984, 52: 431-434. 3.
Hedner T. et al. Br. J. Clin. Pharmacol. 1987,
24: 145-149. 4.
Hosie J et al. J Drug Dev 1992; 5 (3): 129-36 5.
Ljung B. Drugs 1985; 29 (Suppl 2): 46-58 6.
Nordlander M Et Al. Second International Symposium,
Calcium Antagonsists In 7.
B Ljung and M. Nordlander Department of Pharmacology and
Biochemistry, 8.
Physicians’ Desk Reference ed. 51, 1997: 514-516. |
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