BISOPROLOL FUMARATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

BISOPROLOL FUMARATE (UNII: UR59KN573L) (BISOPROLOL - UNII:Y41JS2NL6U)

Available from:

Carilion Materials Management

INN (International Name):

BISOPROLOL FUMARATE

Composition:

BISOPROLOL FUMARATE 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

BISOPROLOL FUMARATE is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents. BISOPROLOL FUMARATE is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

Product summary:

NDC:68151-4504-0 in a PACKAGE of 1 TABLETS

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET
CARILION MATERIALS MANAGEMENT
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BISOPROLOL FUMARATE TABLETS USP
Rx Only
DESCRIPTION
BISOPROLOL FUMARATE USP is a synthetic, beta -selective
(cardioselective) adrenoceptor
blocking agent. The chemical name for bisoprolol fumarate is
(±)-1-[4-[[2-(1-
Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol
(E)-2-butenedioate (2:1)
(salt). It possesses an asymmetric carbon atom in its structure and is
provided as a racemic mixture. The
S(-) enantiomer is responsible for most of the beta-blocking activity.
Its molecular formula is (C H NO )
•C H O and its structure is:
Bisoprolol fumarate has a molecular weight of 766.97. It is a white
crystalline powder which is
approximately equally hydrophilic and lipophilic, and is readily
soluble in water, methanol, ethanol, and
chloroform.
BISOPROLOL FUMARATE TABLETS USP are available as 5 and 10 mg tablets
for oral
administration.
Inactive ingredients include Colloidal Silicon Dioxide, Corn Starch
(Pregelatinized), Crospovidone,
Dibasic Calcium Phosphate, Hypromellose, Magnesium Stearate,
Microcrystalline Cellulose,
Polyethylene Glycol, Polysorbate 80 and Titanium Dioxide. The 5 mg
tablets also contain Red and
Yellow Iron Oxide.
CLINICAL PHARMACOLOGY
BISOPROLOL FUMARATE is a beta -selective (cardioselective)
adrenoceptor blocking agent without
significant membrane stabilizing activity or intrinsic sympathomimetic
activity in its therapeutic dosage
range. Cardioselectivity is not absolute, however, and at higher doses
(≥ 20 mg) bisoprolol fumarate
also inhibits beta -adrenoceptors, chiefly located in the bronchial
and vascular musculature; to retain
selectivity it is therefore important to use the lowest effective
dose.
PHARMACOKINETICS AND METABOLISM
The absolute bioavailability after a 10 mg oral dose of bisoprolol
fumarate is about 80%. Absorption is
not affected by the presence of food. The first pass metabolism of
bisoprolol fumarate is about 20%.
1183142444
12
Binding to serum proteins is approxi