BISOPROLOL FUMARATE tablet, coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Eon Labs, Inc.

INN (International Name):

BISOPROLOL FUMARATE

Composition:

BISOPROLOL FUMARATE 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Bisoprolol fumarate tablets, USP are 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:

Bisoprolol Fumarate Tablets, USP, for oral administration, are available as 5 mg Pink, round, biconvex, film-coated, debossed “E ” over “771” and bisected on the other side and supplied as: NDC 0185-0771-30 bottles of 30 NDC 0185-0771-01 bottles of 100 10 mg White, round, biconvex, film-coated, debossed “E ” over “774” and plain on the other side and supplied as: NDC 0185-0774-30 bottles of 30 NDC 0185-0774-01 bottles of 100 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure, as required. KEEP TIGHTLY CLOSED. To report SUSPECTED ADVERSE REACTIONS, contact Sandoz Inc. at 1-800-525-8747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Manufactured by Sandoz Inc. Princeton, NJ 08540 46192536 Rev. September 2016 MF0771REV09/16

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET, COATED
EON LABS, INC.
----------
BISOPROLOL FUMARATE TABLETS, USP
RX ONLY
DESCRIPTION
Bisoprolol fumarate tablets, USP (bisoprolol fumarate) is a synthetic,
beta -selective (cardioselective)
adrenoceptor blocking agent. The chemical name for bisoprolol
fumarate, USP 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 766.96. 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 mg and 10 mg
tablets for oral administration.
The tablets contain the following inactive ingredients: colloidal
silicon dioxide, corn starch, dibasic
calcium phosphate anhydrous, hypromellose, magnesium stearate,
microcrystalline cellulose,
polyethylene glycol, polysorbate and titanium dioxide. In addition,
the 5 mg tablets contain FD&C
yellow No. 6 aluminum lake and FD&C red No. 40 aluminum lake.
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
(greater than or equal to 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