BISOPROLOL FUMARATE tablet, film coated

País: Estados Unidos

Idioma: inglés

Fuente: NLM (National Library of Medicine)

Ingredientes activos:

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

Disponible desde:

AvPAK

Vía de administración:

ORAL

tipo de receta:

PRESCRIPTION DRUG

indicaciones terapéuticas:

Bisoprolol fumarate tablets are indicated in the management of hypertension. They 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.

Resumen del producto:

Bisoprolol fumarate is supplied as 5 mg and 10 mg tablets. Bisoprolol Fumarate Tablets, USP 5 mg are pink colored, circular, biconvex, film coated tablets, debossed with ‘C and break line’ on one side and ‘86’ on the other side. NDC 50268-127-15 (10 tablets per card, 5 cards per carton) Bisoprolol Fumarate Tablets, USP 10 mg are white, circular, biconvex, film coated tablets, debossed with ‘C’ on one side and ‘87’ on the other side. Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Protect from light and moisture. Dispensed in Unit Dose Packaging. For Institutional Use Only. Manufactured for: AvKARE Pulaski, TN 38478 Mfg. Rev. 10/21 AV 11/21 (P) AvPAK

Estado de Autorización:

Abbreviated New Drug Application

Ficha técnica

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET, FILM COATED
AVPAK
----------
BISOPROLOL FUMARATE TABLETS, USP
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 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 is available as 5 and 10 mg tablets for oral
administration.
Inactive ingredients include microcrystalline cellulose, anhydrous
dibasic calcium
phosphate, crospovidone, colloidal silicon dioxide, magnesium
stearate, hypromellose,
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 important to
1
18
31
4
2
4
4
4
1
2
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
concentrati