Bisoprolol Fumarate

INDICATIONS & USAGE Bisoprolol fumarate is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.

CLINICAL PHARMACOLOGY Bisoprolol fumarate is a beta 1 -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 2 -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%.

Clinical clearance of Bisoprolol Fumarate (beta-Adrenergic Blocker) relies on phase i/ii hepatic conjugation of bisoprolol fumarate coupled with glomerular and tubular renal excretion with a Approximately 3–15 hours terminal plasma half-life for Bisoprolol Fumarate half-life; patients absorbing at Estimated 75%–87% oral systemic absorption for Bisoprolol Fumarate bioavailability typically observe target onset around peak plasma concentration (tmax) reached 1–4 hours post-dose for bisoprolol fumarate.

FDA clinical labeling for Bisoprolol Fumarate restricts administration in contraindications bisoprolol fumarate is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree av block, and marked sinus bradycardia.; documented intolerance or hypersensitivity reaction involving bisoprolol fumarate (beta-adrenergic blocker) across 10 mg/1 Tablet, Film Coated, 10 mg/1 Tablet, 5 mg/1 Tablet, 2.5 mg/1 Tablet, Film Coated, 5 mg/1 Tablet, Film Coated, with self-reported patient tracking dominated by dizziness (7.6% of reports), headache (7.2% of reports), fatigue (6.3% of reports).