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Bisoprolol

ZEBETA

What it isHighly beta-1 selective blocker; heart failure with reduced EF and hypertension.

Why this oneOne of only three beta blockers with heart-failure mortality data, and the most cardioselective of them.

What limits itBradycardia, and it must be titrated slowly in heart failure. Never stop abruptly.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Hypertensionadult5 mg QD (2.5 mg QD may be appropriate in some, e.g. bronchospastic disease)5-10 mg QD (individualized)20 mg QD

Renal CrCl <40 mL/min: initial 2.5 mg QD, cautious titration; not dialyzable — no replacement dose needed on dialysis

Hepatic Hepatitis or cirrhosis: initial 2.5 mg QD, cautious titration

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No adequate human studies; fetotoxic/maternotoxic in animals at high multiples of MRHD; use only if benefit justifies fetal risk

Lactation Not known if excreted in human milk (<2% of dose in rat milk); caution in nursing women

NO BOXED WARNINGS

Principal riskBradycardia

Cost, est. cash$5–$150/month

Generic entry2000

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityBradycardia, hypotension and bronchospasm; overdose may cause conduction block or cardiogenic shock.

Mechanism of action: Bisoprolol ballicule

Bisoprolol ballicule: receptor binding, kinetics and half-life diagram

Open Bisoprolol in the interactive console ↗

Memory aids: mascots and interaction avatars

Bisoprolol ZEBETA mascot mnemonic cartoon
“Bison Zebra beta (blocks)”
LOL hat → beta blocker
Bisoprolol CYP3A4 substrate avatar
CYP3A4 substrate

Open Bisoprolol in the interactive console ↗