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:

Mylan Pharmaceuticals Inc.

INN (International Name):

BISOPROLOL FUMARATE

Composition:

BISOPROLOL FUMARATE 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Bisoprolol fumarate tablets are indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents. Bisoprolol fumarate tablets are 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 are supplied as 5 mg or 10 mg tablets. The 5 mg tablet is a purple, film-coated, round, tablet debossed with 523 above the score on one side of the tablet and M on the other side. It is available as follows: NDC 0378-0523-93 bottles of 30 tablets NDC 0378-0523-77 bottles of 90 tablets NDC 0378-0523-01 bottles of 100 tablets The 10 mg tablet is a white, film-coated, round, unscored tablet debossed with 524 on one side of the tablet and M on the other side. It is available as follows: NDC 0378-0524-93 bottles of 30 tablets NDC 0378-0524-77 bottles of 90 tablets NDC 0378-0524-25 bottles of 250 tablets 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 using a child-resistant closure. Mylan Pharmaceuticals Inc. Morgantown, WV 26505 U.S.A. Revised: 1/2018 BISO:R8

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET, FILM COATED
MYLAN PHARMACEUTICALS INC.
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DESCRIPTION
Bisoprolol fumarate, USP is a synthetic, beta -selective
(cardio-selective) 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.
Each tablet for oral administration contains either 5 mg or 10 mg of
bisoprolol fumarate. In addition,
each tablet contains the following inactive ingredients: anhydrous
lactose, colloidal silicon dioxide,
croscarmellose sodium, hypromellose, magnesium stearate,
microcrystalline cellulose, polydextrose,
polyethylene glycol, sodium lauryl sulfate and titanium dioxide. Each
5 mg tablet also contains FD&C
Blue No. 2 Aluminum Lake and FD&C Red No. 40 Aluminum Lake.
_Meets USP Dissolution Test 2._
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 f