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metaproterenol

 

Classes: Beta2 Agonists

Dosing and uses of Metaproterenol

 

Adult dosage forms and strengths

tablet

  • 10mg
  • 20mg

syrup

  • 10mg/5mL

 

Asthma, Reversible Bronchospasm

20 mg PO three/four times daily

 

Pediatric dosage forms and strengths

tablet

  • 10mg
  • 20mg

syrup

  • 10mg/5mL

 

Asthma

PO

  • <2 years old: 0.4 mg/kg PO q8-12hr
  • 2-6 years old: 1-3.5 mg/kg/day divided q6-8hr PO; not to exceed 10 mg/dose
  • 6-9 years old: 10 mg PO three/four times daily
  • >12 years old: 20 mg PO three times daily

 

Metaproterenol adverse (side) effects

>10%

Tremor (2-17%)

Tachycardia (6-17%)

Nervousness (5-20%)

 

1-10%

Diaphoresis increased (4%)

Headache (4%)

Heartburn (4%)

Palpation (4%)

Pharyngitis (4%)

Dizziness (1-4%)

Insomnia (2%)

Weakness (1%)

Nausea (1-4%)

Exacerbation of asthma (2%)

 

<1%

Chest pain

Hypertension

Weakness

Syncope

Spasms

 

Warnings

Contraindications

Hypersensitivity

Tachycardia secondary to heart condition

 

Cautions

Reports of some patients who developed cramps in muscles of extremities which responded to potassium salts PO

Use caution in recent MI, myocardial insufficiency, HTN, hyperthyroidism, severe cardiovascular disorder, seizure disorders

Increases risk of hypokalemia;; use with caution

Beta2-agonists may increase serum glucose; use caution

Metered-dose inhalers that contain chlorofluorocarbons (CFCs) are currently being phased out in the United States; alternate inhalers without CFCs are available

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Not known if excreted in breast milk, not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Metaproterenol

Mechanism of action

Beta-2 receptor agonist with some beta-1 activity; stimulation of beta2 receptors may result in bronchial smooth muscle relaxation

 

Pharmacokinetics

Onset: 30 min (oral)

Peak effect: 1 hr

Duration: 2-6 hr

Metabolism: Liver

Metabolites: Metaproterenol-O-sulfate

Excretion: Uurine (40%)