BISOPROLOL FUMARATE tablet, film coated

Ülke: ABD

Dil: İngilizce

Kaynak: NLM (National Library of Medicine)

Aktif bileşen:

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

Mevcut itibaren:

Physicians Total Care, Inc.

INN (International Adı):

BISOPROLOL FUMARATE

Kompozisyon:

BISOPROLOL FUMARATE 5 mg

Uygulama yolu:

ORAL

Reçete türü:

PRESCRIPTION DRUG

Terapötik endikasyonlar:

Bisoprolol is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents. Bisoprolol is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

Ürün özeti:

Bisoprolol fumarate is supplied as 5 mg and 10 mg tablets. The 5 mg tablet is a pink, round, film-coated, convex tablet debossed with “5270” and “93”, bisect on one side and plain on the other side, in The 10 mg tablet is a white, round, film-coated, convex tablet debossed with “5271” and “93”, on one side and plain on the other side, in Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature], protected from moisture. Dispense in tight containers as defined in the USP, with a child-resistant closure, as required.

Yetkilendirme durumu:

Abbreviated New Drug Application

Ürün özellikleri

BISOPROLOL FUMARATE - BISOPROLOL FUMARATE TABLET, FILM COATED
PHYSICIANS TOTAL CARE, INC.
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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 structural formula is:
(C
H NO ) •C H O M.W. 766.98
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 colloidal silicon dioxide, dibasic
calcium phosphate anhydrous, magnesium
stearate, microcrystalline cellulose, pregelatinized corn starch NF,
titanium dioxide, hypromellose,
polyethylene glycol, and polysorbate 80. The 5 mg tablets also contain
FD&C Red # 40 Aluminum Lake
and FD&C Yellow # 6 Aluminum Lake.
CLINICAL PHARMACOLOGY
Bisoprolol 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 occur within 2 to 4 hours
of dosing with 5 to 20 mg, an