VENTOLIN HFA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VENTOLIN HFA (VENTOLIN HFA).
Beta2-adrenergic receptor agonist; stimulates adenylate cyclase, increasing cAMP, leading to relaxation of bronchial smooth muscle.
| Metabolism | Primarily metabolized by sulfotransferase (SULT1A3) to an inactive sulfate conjugate; minor metabolism by COMT and MAO. |
| Excretion | Renal (60-70% as unchanged drug and metabolites, primarily as sulfate conjugate; biliary/fecal: minor, <10%). |
| Half-life | 3-4 hours for systemically absorbed albuterol; terminal half-life is approximately 3.8 hours. No accumulation with repeated dosing. |
| Protein binding | ~10% (primarily to albumin). |
| Volume of Distribution | 1.9-2.5 L/kg (indicating extensive extravascular distribution). |
| Bioavailability | Inhalation: 20-30% (systemic absorption via lungs and swallowed fraction). Oral: ~50% (but not used orally due to systemic effects). |
| Onset of Action | Inhalation: 5-15 minutes (rapid bronchodilation). |
| Duration of Action | 4-6 hours (dose-dependent; shorter in some patients with severe bronchospasm). |
90 mcg (2 inhalations) by oral inhalation every 4 to 6 hours as needed for bronchospasm. For prevention of exercise-induced bronchospasm, 2 inhalations 15 to 30 minutes before exercise.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dose adjustment required for renal impairment. The primary route of elimination is hepatic metabolism. |
| Liver impairment | No specific dose adjustment guidelines for hepatic impairment. Use with caution in severe hepatic disease as albuterol clearance may be reduced. |
| Pediatric use | Children 4 years and older: 90 mcg (2 inhalations) by oral inhalation every 4 to 6 hours as needed. For exercise-induced bronchospasm, 2 inhalations 15 to 30 minutes before exercise. Children 2 to 4 years: Safety and efficacy not established for this age group. |
| Geriatric use | No specific dose adjustment recommended for elderly patients. Monitor for excessive tachypnea, tachycardia, or other side effects, as elderly patients may have increased sensitivity to beta-2 agonists. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VENTOLIN HFA (VENTOLIN HFA).
| Breastfeeding | Albuterol is excreted into human breast milk in small amounts (estimated infant dose less than 1% of maternal weight-adjusted dose). M/P ratio is unknown. Use with caution in breastfeeding women; no adverse effects on nursing infants have been reported, but theoretical risk of beta-adrenergic stimulation exists. |
| Teratogenic Risk | Albuterol (VENTOLIN HFA) is FDA Pregnancy Category C. In animal studies, albuterol administered subcutaneously caused fetal abnormalities (cleft palate, limb defects) at high doses (0.25-2.5 mg/kg). However, among pregnant women, inhaled albuterol has not been shown to increase the risk of major congenital malformations. Hypoglycemia and/or tachycardia may occur in the neonate after maternal use of beta-2 agonists, particularly with high doses or prolonged use near term. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to albuterol or any component of the formulation"]
| Precautions | ["Paradoxical bronchospasm may occur","Cardiovascular effects: increased heart rate, hypertension, arrhythmias","Hypokalemia may occur","Monitor for signs of hypersensitivity reactions"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and signs of pulmonary edema in patients with preeclampsia or cardiovascular disease. Fetal monitoring (non-stress test or biophysical profile) may be considered if used for preterm labor or in cases of maternal tachycardia or hypoxia. |
| Fertility Effects | No adverse effects on fertility have been reported in human studies. In animal studies, albuterol did not impair fertility at doses up to 50 times the maximum human inhalation dose. |