BISOPROLOL FUMARATE- bisoprolol fumarate tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Teva Pharmaceuticals USA, Inc.

INN (International Name):

BISOPROLOL FUMARATE

Composition:

BISOPROLOL FUMARATE 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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

Product summary:

Bisoprolol fumarate is supplied as 5 mg and 10 mg tablets. The 5 mg tablet is a pink, round, film-coated, convex tablet debossed with “5270” and “93”, bisect on one side and plain on the other side, in bottles of 30 with CRC. The 10 mg tablet is a white, round, film-coated, convex tablet debossed with “5271” and “93”, on one side and plain on the other side, in bottles of 30 with CRC. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature], protected from moisture. Dispense in tight containers as defined in the USP, with a child-resistant closure, as required. Manufactured In Canada By: TEVA CANADA LIMITED Toronto, Canada M1B 2K9 Manufactured For: TEVA PHARMACEUTICALS USA Sellersville, PA 18960 Rev. I 3/2011

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET, FILM COATED
TEVA PHARMACEUTICALS USA, INC.
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BISOPROLOL FUMARATE TABLETS USP
5270
5271
RX ONLY
DESCRIPTION
Bisoprolol fumarate 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 structural formula is:
(C
H NO ) •C H O M.W. 766.98
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 is available as 5 and 10 mg tablets for oral
administration.
Inactive ingredients include colloidal silicon dioxide, dibasic
calcium phosphate anhydrous, magnesium
stearate, microcrystalline cellulose, pregelatinized corn starch NF,
titanium dioxide, hypromellose,
polyethylene glycol, and polysorbate 80. The 5 mg tablets also contain
FD&C Red # 40 Aluminum Lake
and FD&C Yellow # 6 Aluminum Lake.
CLINICAL PHARMACOLOGY
Bisoprolol 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%.
Binding to serum proteins is approximately 30%. Peak plasma
concentrations occ