FELODIPINE tablet extended release

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

FELODIPINE (UNII: OL961R6O2C) (FELODIPINE - UNII:OL961R6O2C)

Available from:

American Health Packaging

INN (International Name):

FELODIPINE

Composition:

FELODIPINE 5 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FELODIPINE- FELODIPINE TABLET, EXTENDED RELEASE
AMERICAN HEALTH PACKAGING
----------
FELODIPINE EXTENDED-RELEASE TABLETS, USP
8288321/0815OS
RX ONLY
DESCRIPTION
Felodipine is a calcium antagonist (calcium channel blocker).
Felodipine is a dihydropyridine derivative
that is chemically described as ± ethyl methyl
4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-
pyridinedicarboxylate. Its molecular formula is C
H
Cl
NO
and its structural formula is:
Felodipine, USP is a light yellow to yellow crystalline powder with a
molecular weight of 384.26. It is
insoluble in water and is freely soluble in acetone and in methanol;
very slightly soluble in heptane.
Felodipine is a racemic mixture.
Felodipine extended-release tablets, USP provide extended release of
felodipine. They are available as
tablets containing 2.5 mg, 5 mg or 10 mg of felodipine, USP for oral
administration. Inactive ingredients
are: calcium silicate, castor oil polyethoxylated 40, hydroxypropyl
cellulose, hypromellose, lactose
monohydrate, microcrystalline cellulose, propyl gallate, sodium
stearyl fumarate, titanium dioxide, and
triacetin. In addition, the 2.5 mg tablet strength contains FD&C Blue
2/indigo carmine aluminum lake and
iron oxide yellow and the 5 mg and 10 mg strengths contain iron oxide
red.
_Felodipine extended-release tablets, USP complies with USP
Dissolution Test I and Test II._
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Felodipine is a member of the dihydropyridine class of calcium channel
antagonists (calcium channel
blockers). It reversibly competes with nitrendipine and/or other
calcium channel blockers for
dihydropyridine binding sites, blocks voltage-dependent Ca
currents in vascular smooth muscle and
cultured rabbit atrial cells, and blocks potassium-induced contracture
of the rat portal vein.
_In vitro_ studies show that the effects of felodipine on contractile
processes are selective, with greater
effects on vascular smooth muscle than cardiac muscle. Negative
inotropic effects can be detected _in_
18
19
2
4
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_vitro_, but