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:

Bryant Ranch Prepack

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:

BISOPROLOL FUMARATE is supplied as 5 mg tablets. The 5 mg tablet is pink colored, biconvex, round, film coated tablet debossed with UL on one side and scored on the other side with 5 debossed on either side of the score. NDC 63629-5173-1: 30 TABLET in a BOTTLE NDC 63629-5173-2: 100 TABLET in a BOTTLE NDC 63629-5173-3: 90 TABLET in a BOTTLE NDC 63629-5173-4: 28 TABLET in a BOTTLE NDC 63629-5173-5: 120 TABLET in a BOTTLE Store at 20° to 25°C (68° to 77°F). [see USP Controlled Room Temperature]. Protect from moisture. Dispense in tight, light-resistant containers. Repackaged/Relabeled by: Bryant Ranch Prepack, Inc. Burbank, CA 91504

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET
BRYANT RANCH PREPACK
----------
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
1
18
31
4 2
4
4
4
1
2
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 approx