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metaproterenol

β2-selective adrenergic receptor agonist · Bronchodilator

β2-selective adrenergic receptor agonistBronchodilator
CDSCO approved
EXCRETION
not curated
INTERACTIONS
7 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 9
  • IsocarboxazidSevereTextbookG&G 14e · p264
  • MoclobemideSevereTextbookG&G 14e · p264
  • PhenelzineSevereTextbookG&G 14e · p264
  • ProcarbazineSevereTextbookG&G 14e · p264

Mechanism

Metaproterenol is a resorcinol bronchodilator with hydroxyl groups at positions 3 and 5 of the phenyl ring, making it resistant to methylation by COMT. It is considered β2 selective, causing relaxation of bronchial smooth muscle.

Indications

long-term treatment of obstructive airway diseasesasthmaacute bronchospasmBronchodilation (as last resort)

Pharmacokinetics

Onset
within minutes of inhalation; slower orally
Bioavailability
substantial fraction (40%) absorbed in active form after oral administration
Protein binding
effects persist for several hours (inhalation), 3 to 4 hours (oral)
Excretion
primarily as glucuronic acid conjugates

Side effects

Common
cardiac stimulation

Drug interactions

Isocarboxazid
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Moclobemide
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Phenelzine
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Procarbazine
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Rasagiline
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Selegiline
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Tranylcypromine
Severe
Textbook

Increased risk of adverse cardiovascular effects.

At least 2 weeks should elapse between the use of MAO inhibitors and administration of β2 agonists or other sympathomimetics.

Source: G&G 14e · p264

Corticosteroids
Moderate
Textbook

Enhanced beneficial effects in asthma therapy for both drugs.

Source: G&G 14e · p887

Digoxin
Moderate
Textbook

Hypokalemia, which could predispose to cardiac arrhythmias, especially in patients with cardiac disease.

Use with caution.

Source: G&G 14e · p264

Related guidelines

Other β2-selective adrenergic receptor agonist drugs

Ask House about metaproterenol

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team