国家: 美国
语言: 英文
来源: NLM (National Library of Medicine)
BISOPROLOL FUMARATE (UNII: UR59KN573L) (BISOPROLOL - UNII:Y41JS2NL6U)
Teva Pharmaceuticals USA, Inc.
BISOPROLOL FUMARATE
BISOPROLOL FUMARATE 5 mg
ORAL
PRESCRIPTION DRUG
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.
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 bottles of 30 with CRC. 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 bottles of 30 with CRC. 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. Manufactured In Canada By: TEVA CANADA LIMITED Toronto, Canada M1B 2K9 Manufactured For: TEVA PHARMACEUTICALS USA Sellersville, PA 18960 Rev. I 3/2011
Abbreviated New Drug Application
BISOPROLOL FUMARATE- BISOPROLOL FUMARATE TABLET, FILM COATED TEVA PHARMACEUTICALS USA, INC. ---------- BISOPROLOL FUMARATE TABLETS USP 5270 5271 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 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 occ 阅读完整的文件