Metaproterenol (Orciprenaline)

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Germany: Alupent; Greece: Alupent; Ireland: Alupent; Malta: Alupent; Poland: Astmopent; UK: Alupent.

North America

Canada: Apo-Orciprenaline; USA: Metaproterenol.

Latin America

Mexico: Alupent.


Japan: Alotec.

Drug combinations


Metaproterenol Sulfate: (C~11~H~17~NO~3~)~2~. H~2~SO~4~. Mw: 520.59. (1) 1,3-Benzenediol, 5-[1-hydroxy-2-(1-methylethyl)amino]ethyl-, (±)-, sulfate (2:1); (2)(±)-3,5-Dihydroxy-α-[(isopropylamino)methyl]benzyl alcohol sulfate (2:1). CAS-5874-97-5 (1964).

Pharmacologic Category

Sympathomimetic (Adrenergic) Agents; β-Adrenergic Agonists; Selective β~2~-Adrenergic Agonists. (ATC-Code: R03AB03).

Mechanism of action

Relaxes bronchial smooth muscle by action on β~2~-receptors with very little effect on heart rate.

Therapeutic use

Bronchodilator in reversible airway obstruction due to asthma or chronic obstructive pulmonary disease.

Pregnancy and lactiation implications

No data on crossing placenta. Reported association with polydactyly in one study. Unknown whether metaproterenol is distributed into milk. Administer oral solution or inhalation aerosol to nursing women only if potential benefits to woman outweigh possible risk to infant.

Unlabeled use


Hypersensitivity to metaproterenol or any component of the formulation. Pre-existing cardiac arrhythmias associated with tachycardia.

Warnings and precautions

Paradoxical bronchospasm might occur (rarely) with use of inhaled bronchodilating agents. Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) reported. Serious adverse events, including fatalities, associated with excessive use of inhaled sympathomimetics. Do not use as component of chronic therapy without an anti-inflammatory agent. Use with caution in cardiovascular disease (arrhythmia or hypertension or heart failure); β-agonists may cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation. β~2~-Agonists may also increase risk of arrhythmias. Use with caution in diabetes mellitus (β~2~-agonists might increase serum glucose), in glaucoma (might elevate intraocular pressure), in hyperthyroidism (might stimulate thyroid activity), in hypokalemia (β~2~-agonists might decrease serum potassium), and in seizure disorders (β-agonists might result in CNS stimulation/excitation). Face masks should be used in children under 4 years of age. Oral use should be avoided (increased incidence of adverse effects). Metaproterenol has more β~1~ activity than β~2~-selective agents such as albuterol (may no longer be β-agonist of first choice).



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