Note: Metaproterenol tablets and syrup have been discontinued in the United States for >1 year.
Asthma/Bronchospasm: Note: Oral bronchodilators are not recommended for routine use in the management of acute asthma or long-term daily maintenance treatment due to a slower onset of action and higher risk of side effects compared to inhaled short-acting beta agonists (GINA 2022; NAEPP 2007).
Oral: 20 mg 3 or 4 times daily.
There are no dosage adjustments provided in the manufacturer's labeling.
There are no dosage adjustments provided in the manufacturer's labeling.
(For additional information see "Metaproterenol (orciprenaline) (United States: Not available): Pediatric drug information")
Note: Metaproterenol tablets and syrup have been discontinued in the United States for >1 year.
Asthma/bronchospasm: Note: Although FDA approved, oral bronchodilators are not recommended for routine use in the management of acute asthma or long-term daily maintenance treatment due to a slower onset of action and higher risk of adverse effects compared to inhaled short-acting beta agonists (GINA 2022; NAEPP 2007).
Children ≤5 years: Oral: 1.3 to 2.6 mg/kg/day divided every 6 to 8 hours; maximum dose: 10 mg/dose (Nelson 1996).
Children 6 to 9 years or weighing <27 kg: Oral: 10 mg 3 to 4 times daily.
Children >9 years and Adolescents or weighing ≥27 kg: Oral: 20 mg 3 to 4 times daily.
There are no dosage adjustments provided in the manufacturer's labeling.
There are no dosage adjustments provided in the manufacturer's labeling.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral, as sulfate:
Generic: 10 mg [DSC], 20 mg [DSC]
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Syrup, Oral, as sulfate:
Generic: 10 mg/5 mL (250 mL)
Metaproterenol tablets and syrup have been discontinued in the United States for >1 year.
Administer without regards to food. May administer with food if GI upset occurs.
Oral: Administer without regards to food. May administer with food if GI upset occurs.
Asthma/Bronchospasm: Bronchial asthma and for reversible bronchospasm which may occur in association with bronchitis and emphysema.
Note: Clinical practice guidelines do not recommend oral short-acting beta agonists or nonselective beta agonists, including oral metaproterenol, for routine management and treatment of asthma due to their potential for excessive cardiac stimulation, especially in high doses and slower onset of action (GINA 2022; NAEPP 2007).
Metaproterenol may be confused with metipranolol, metoprolol
Alupent may be confused with Atrovent
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Cardiovascular: Tachycardia (6% to 17%)
Central nervous system: Nervousness (5% to 20%)
Neuromuscular & skeletal: Tremor (2% to 17%)
1% to 10%:
Cardiovascular: Palpitations (4%)
Central nervous system: Headache (1% to 7%), dizziness (2%), insomnia (2%), fatigue (1%)
Gastrointestinal: Nausea (1% to 4%), diarrhea (1%)
Respiratory: Exacerbation of asthma (2%)
<1%, postmarketing, and/or case reports: Blurred vision, change in appetite, chest pain, chills, clonus, cough, diaphoresis, drowsiness, dry throat, edema, facial edema, fever, flu-like symptoms, hypertension, muscle spasm, pain, pruritus, sensory disturbance, swelling of fingers, syncope, unpleasant taste, urticaria, vomiting, weakness, xerostomia
Hypersensitivity to metaproterenol or any component of the formulation; preexisting cardiac arrhythmias associated with tachycardia.
Canadian labeling: Additional contraindications (not in the US labeling): Hypersensitivity to other sympathomimetic amines; hypertrophic cardiomyopathy; concurrent use with beta-adrenergic blocking agents (eg, propranolol); tocolytic use in patients at risk of premature labor or threatened abortion.
Documentation of allergenic cross-reactivity for sympathomimetics is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity can not be ruled out with certainty.
Concerns related to adverse effects:
• Hypersensitivity reactions: Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) have been reported.
Disease-related concerns:
• Asthma: Appropriate use: Metaproterenol (a less selective beta2-agonist) is not recommended in the management of asthma due to potential for excessive cardiac stimulation (NAEPP, 2007). Oral systemic agents (eg, tablets, syrup) should be avoided due to increased risk of adverse effects (eg, excessive cardiac stimulation).
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (arrhythmia or hypertension or HF); beta-agonists may cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation. Beta2-agonists may also increase risk of arrhythmias.
• Chronic obstructive lung disease (COPD): Appropriate use: Inhaled bronchodilators are preferred therapy for COPD exacerbations; oral systemic agents (eg, tablets, syrup) should be avoided due to increased risk of adverse effects (eg, excessive cardiac stimulation).
• Diabetes: Use with caution in patients with diabetes mellitus; beta2-agonists may increase serum glucose.
• Glaucoma: Use with caution in patients with glaucoma; beta2-agonists may elevate intraocular pressure.
• Hyperthyroidism: Use with caution in hyperthyroidism; beta2-agonists may stimulate thyroid activity.
• Hypokalemia: Use with caution in patients with hypokalemia; beta2-agonists may decrease serum potassium.
• Seizures: Use with caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation.
Dosage form specific issues:
• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Atomoxetine: May enhance the tachycardic effect of Beta2-Agonists. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Atosiban: Beta2-Agonists may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Risk C: Monitor therapy
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Beta2-Agonists. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Risk C: Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Risk X: Avoid combination
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Risk D: Consider therapy modification
Loop Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Loop Diuretics. Risk C: Monitor therapy
Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Risk X: Avoid combination
Methacholine: Beta2-Agonists (Short-Acting) may diminish the therapeutic effect of Methacholine. Management: Hold short-acting beta2 agonists for 6 hours before methacholine use. Risk D: Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Theophylline Derivatives: Beta2-Agonists may enhance the adverse/toxic effect of Theophylline Derivatives. Specifically, sympathomimetic effects may be increased. Theophylline Derivatives may enhance the hypokalemic effect of Beta2-Agonists. Risk C: Monitor therapy
Thiazide and Thiazide-Like Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Beta agonists, including metaproterenol, may interfere with uterine contractility if administered during labor; maternal and fetal tachycardia have been observed (Baillie 1970; Tyack 1971).
Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal mortality, preeclampsia, preterm birth, low birth weight infants, cesarean delivery, and the development of gestational diabetes). Poorly controlled asthma or asthma exacerbations may have a greater fetal/maternal risk than what is associated with appropriately used asthma medications. Maternal treatment improves pregnancy outcomes by reducing the risk of some adverse events (eg, preterm birth and gestational diabetes). Maternal asthma symptoms should be monitored monthly during pregnancy. Agents other than metaproterenol are recommended to treat asthma during pregnancy (ERS/TSANZ [Middleton 2020]; GINA 2021).
It is not known if metaproterenol is present in breast milk.
Heart rate, and blood pressure; FEV1, peak flow, and/or other pulmonary function tests; CNS stimulation; serum glucose, serum potassium (in selected patients)
Stimulates beta2-receptors which increases the conversion of adenosine triphosphate (ATP) to 3’-5’-cyclic adenosine monophosphate (cAMP), resulting in bronchial smooth muscle relaxation
Onset of action: Bronchodilation: Oral: ~30 minutes
Peak effect: Oral: ~1 hour
Duration: ~2 to 6 hours, regardless of route administered
Absorption: Oral: Well absorbed
Metabolism: Extensive first-pass in the liver (~40% of oral dose is available)
Excretion: Mainly as glucuronic acid conjugates
Syrup (Metaproterenol Sulfate Oral)
10 mg/5 mL (per mL): $0.07
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
