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:

Golden State Medical Supply, Inc.

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 are supplied as 5 mg and 10 mg tablets. The 5 mg tablet is pink, round, uncoated tablet debossed "N455" on one side and scored on other side. Bottles of 30 Tablets (Unit-of-Use): NDC 51407-645-30 Bottles of 100 Tablets: NDC 51407-645-01 The 10 mg tablet is white to off-white, round, uncoated tablet debossed "N" on one side and "456" on the other side. Bottles of 30 Tablets (Unit-of-Use): NDC 51407-646-30 Bottles of 100 Tablets: NDC 51407-646-01 Store at 20° to 25°C (68° to 77°F). [see USP Controlled Room Temperature]. Protect from moisture. Dispense in tight, light-resistant containers. Please address medical inquiries to Novitium Pharma’s toll free # 1-855-204-1431. All trademarks are the property of their respective owners. Manufactured by: Novitium Pharma, LLC 70 Lake Drive, East Windsor New Jersey 08520 Issued: 10/2021 LB4290-01 Marketed/Packaged by: GSMS, Inc. Camarillo, CA USA 93012

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET
GOLDEN STATE MEDICAL SUPPLY, INC.
----------
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 766.96. 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 and 10 mg tablets
for oral
administration.
Inactive ingredients include: microcrystalline cellulose,
pregelatinized starch, dicalcium
1
18
31
4
2
4
4
4
phosphate, colloidal silicon dioxide, magnesium stearate, iron oxide
red and ferrosoferric
oxide.
FDA approved dissolution test specifications differ from USP.
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%. Binding to serum proteins is
approximately 30%. Peak
plasma concentrations