BISOPROLOL FUMARATE tablet

Country: Ամերիկայի Միացյալ Նահանգներ

language: անգլերեն

source: NLM (National Library of Medicine)

active_ingredient:

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

MAH:

Proficient Rx LP

INN:

BISOPROLOL FUMARATE

composition:

BISOPROLOL FUMARATE 5 mg

administration_route:

ORAL

prescription_type:

PRESCRIPTION DRUG

therapeutic_indication:

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.

leaflet_short:

BISOPROLOL FUMARATE is supplied as 5 mg and 10 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. Bottles of 30: NDC 63187-871-30 Bottles of 60: NDC 63187-871-60 Bottles of 90: NDC 63187-871-90 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 Unichem's toll free # 1-866-562-4616.

authorization_status:

Abbreviated New Drug Application

SPC

BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET
PROFICIENT RX LP
----------
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 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%.
1
18
31
4 2
4
4
4
1
2
Binding to serum proteins is approximatel