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Levalbuterol

XOPENEX

What it isR-enantiomer and beta-2 agonist; rescue treatment of acute bronchospasm.

Why this oneRemoving albuterol's S-enantiomer has not produced a consistent clinical advantage over racemic albuterol.

What limits itTremor, tachycardia, and hypokalemia remain possible; higher cost usually makes albuterol the practical default.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Bronchospasm (asthma)Adults & adolescents ≥12 yr0.63 mg TID (q6–8h)0.63 mg TID1.25 mg TID
Bronchospasm (asthma)Children 6–11 yr0.31 mg TID0.31 mg TID0.63 mg TID

Renal Use with caution; risk of toxicity may be greater in renal impairment — monitor renal function.

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No adequate controlled studies; no teratogenicity for levalbuterol in rabbits (racemic albuterol teratogenic in animals at high doses).

Lactation No data on presence in human milk.

NO BOXED WARNINGS

Principal riskNo proven advantage over albuterol at higher cost

Cost, est. cash$30–$500/month

Generic entry2008

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityTremor, tachycardia or anticholinergic effects; excessive beta-agonist exposure can cause hypokalemia and arrhythmia.

Mechanism of action: Levalbuterol ballicule

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

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