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Acebutolol

SECTRAL

What it isBeta-1 selective blocker with intrinsic sympathomimetic activity; hypertension and ventricular arrhythmia.

Why this oneThe partial agonism means less bradycardia, which suits patients with a low resting rate.

What limits itThat same activity makes it a poor choice after myocardial infarction. Drug-induced lupus.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
HypertensionAdult400 mg QD400–800 mg/day (QD or BID)1200 mg/day (BID)
Ventricular arrhythmiaAdult200 mg BID600–1200 mg/day

Renal Undefined

Hepatic Undefined

Elderly: ~2-fold higher bioavailability; use lower maintenance doses and avoid >800 mg/day.

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskIntrinsic sympathomimetic activity makes it poor post-infarction

Cost, est. cash$10–$300/month

Generic entry1995

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: Acebutolol ballicule

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

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