PROAIR HFA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROAIR HFA (PROAIR HFA).
Selective beta-2 adrenergic receptor agonist; relaxes bronchial smooth muscle by increasing intracellular cyclic AMP.
| Metabolism | Primarily metabolized by catechol-O-methyltransferase (COMT) and to a lesser extent by sulfation; not metabolized by CYP450 enzymes. |
| Excretion | Renal: approximately 72% as unchanged drug and metabolites; fecal: approximately 10%; biliary: minimal. |
| Half-life | Terminal elimination half-life: 3.8 to 5 hours; clinically, this supports a dosing interval of every 4-6 hours as needed for symptom relief. |
| Protein binding | Approximately 94% bound to human serum albumin. |
| Volume of Distribution | Vd: 1.9 to 2.7 L/kg; this large Vd indicates extensive distribution into tissues, including lung tissue. |
| Bioavailability | Inhalation: approximately 10-20% of the administered dose reaches the lungs; the remainder is swallowed and undergoes first-pass metabolism resulting in negligible oral bioavailability. |
| Onset of Action | Inhalation: 5 to 15 minutes. |
| Duration of Action | Inhalation: 3 to 6 hours; clinical note: duration may be shorter in patients with more severe airways obstruction. |
Two inhalations (90 mcg each) via oral inhalation every 4-6 hours as needed; for prevention of exercise-induced bronchospasm, two inhalations 15-30 minutes before exercise.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Children 4-11 years: Two inhalations (90 mcg each) via oral inhalation every 4-6 hours as needed; for exercise-induced bronchospasm, two inhalations 15-30 minutes before exercise. Children <4 years: Safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to potential for decreased renal function and increased sensitivity to beta-agonists. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROAIR HFA (PROAIR HFA).
| Breastfeeding | Albuterol is excreted into human breast milk in small amounts (M/P ratio not established). No reported adverse effects in nursing infants. Use with caution in lactating women; benefit of breastfeeding should outweigh potential risk to infant. Monitor infant for signs of beta-adrenergic stimulation (tachycardia, irritability). |
| Teratogenic Risk | FDA Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, albuterol sulfate caused fetal malformations (cleft palate, limb defects) at doses 0.4-1.2 times the maximum human daily inhalation dose. Risk cannot be ruled out; use only if potential benefit justifies potential risk. For trimester-specific risks: first trimester: potential for orofacial clefts and limb defects; second/third trimesters: risk of maternal tachycardia and hypoglycemia in neonate; labor inhibition near term; possible neonatal transient hypoglycemia. |
■ FDA Black Box Warning
Not applicable; no black box warning.
| Serious Effects |
["Hypersensitivity to albuterol or any component of the formulation"]
| Precautions | ["Paradoxical bronchospasm may occur","Cardiovascular effects: increased heart rate, blood pressure, or ECG changes","Immediate hypersensitivity reactions","Potentially severe hypokalemia","May exacerbate diabetes and ketoacidosis"] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and serum potassium (risk of hypokalemia). In pregnancy, assess fetal heart rate patterns and uterine activity. Monitor for signs of preterm labor suppression. Assess maternal respiratory status and peak expiratory flow. In neonates, monitor for transient hypoglycemia, tachycardia, and jitteriness if used near delivery. |
| Fertility Effects | No human data on fertility. In animal studies, albuterol caused decreased fertility in rats at doses 50 times the maximum human daily inhalation dose. Effect on human fertility is unknown. |