Felodipine is a member of the dihydropyridine class of calcium antagonist. Like Amlodipine, Felodipine is the second generation CCBs. It is very effective in the treatment of hypertension and has few side effects¹.  

Felodipine may be easily used alone or concomitantly with other antihypertensive agents such as beta-blocker, diuretics, or ACE-inhibitors. It has been shown to be effective and well tolerated in hypertensive patients who also suffer from angina pectoris, with concomitant ventricular dysfunction^2,3,4. Felodipine is also highly selective compared with other calcium antagonists and can prevent or retard the progress of renal disease^5,6. Accordingly, the demand for Felodipine is expected to increase significantly in the near future.

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.  Felodipine: Agon^®; Fensel^®; Frodil^®; Modip^®; Munobal^®; Perfudal^®; Plendil^®; Prevex^®; Preslow^®; Renedil^®.

b.  Combination products: Lexxel^® (felodipine, enalapril); Logimax^® (felodipine, metoprolol); Unimax^® (felodipine, ramipril).

• Technical package and impurity profiles are available upon request.

•  Sales to countries without patent issues only.

•  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 Cardiovascular Care. Basel, February 13-15, 1991; 12.

7. B Ljung and M. Nordlander Department of Pharmacology and Biochemistry, Hassle Cardiovascular Research Laboratories, Molndal

8. Physicians’ Desk Reference ed. 51, 1997: 514-516.

产  品

用  途

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