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 ACEinhibitors. It has
been shown to be effective and well tolerated in hypertensive
patients who also suffer from angina pectoris, with concomitant ventricular
dysfunction2,3,4. 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.
Felodipine is found to be the best choice for elderly patients with
hypertension, especially isolated systolic hypertension5. These
findings strongly suggest that felodipine is a valuable
antihypertensive vasodilating calcium antagonist.
Felodipine is also highly selective compared with
other calcium antagonists and can prevent or
retard the progress of renal disease6.
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:7
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. Black HR et al. PubMed 2001 Nov;38(5):1118-23
6. Ljung B. Drugs 1985; 29 (Suppl 2): 46-58
7. Physicians' Desk Reference ed. 51, 1997:
514-516.
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 function6.
Proprietary Names
a. Felodipine : AgonR; FenselR; FrodilR; ModipR;
MunobalR; PerfudalR; PlendilR; PrevexR; PreslowR;
RenedilR.
b.
Combination products : LexxelR (felodipine,
enalapril) ; LogimaxR (felodipine, metoprolol) ;
UnimaxR (felodipine, ramipril).
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