Therapeutic Classification: bronchodilators
Pharmacologic Classification: beta-adrenergic agonists
Absorption: 30% absorbed following oral inhalation (from lung surface); swallowed drug is minimally absorbed.
Distribution: Extensively distributed to tissues.
Metabolism/Excretion: Extensively metabolized by the liver, some by the CYP3A4 isoenzyme; only one metabolite binds to beta2 adrenergic receptors. 57% excreted unchanged in urine, remainder in feces as drug and metabolites (84%).
Half-Life: 45 hr.
Contraindicated in:
- Acutely deteriorating COPD or acute respiratory symptoms;
- Asthma.
Use Cautiously in:
- History of seizures;
- Thyrotoxicosis;
- History of cardiovascular disorders (coronary insufficiency, arrhythmias, hypertension);
- Sensitivity to sympathomimetics (adrenergics);
- Severe hepatic impairment;
- OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; may interfere with uterine contractility during labor;
- Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
- Pedi: Safety and effectiveness not established in children.
Exercise Extreme Caution in:
- Concurrent use with MAO inhibitors, tricyclic antidepressants, or drugs that prolong the QTc interval (↑ risk of adverse cardiovascular reactions).