AIRSUPRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AIRSUPRA (AIRSUPRA).
AIRSUPRA is a fixed-dose combination of albuterol (a short-acting beta2-agonist) and budesonide (an inhaled corticosteroid). Albuterol relaxes bronchial smooth muscle via beta2-adrenergic receptor activation, increasing cAMP and causing bronchodilation. Budesonide reduces airway inflammation by binding to glucocorticoid receptors, modulating gene transcription to suppress inflammatory mediators.
| Metabolism | Budesonide is extensively metabolized in the liver via CYP3A4 to inactive metabolites. Albuterol is metabolized primarily by sulfotransferase (SULT1A3) to an inactive sulfate conjugate, with minor hepatic metabolism. |
| Excretion | Budesonide: ~60% renal as metabolites, ~40% fecal; formoterol: ~60% renal, ~40% fecal |
| Half-life | Budesonide: 2-3 hours; formoterol: 10-14 hours; clinical context: steady state achieved within days for both |
| Protein binding | Budesonide: 85-90% (albumin); formoterol: ~50% (albumin) |
| Volume of Distribution | Budesonide: 4-5 L/kg (extensive tissue distribution); formoterol: 5-6 L/kg |
| Bioavailability | Inhalation: budesonide ~15%, formoterol ~50% (systemic); oral budesonide: 6-11% |
| Onset of Action | Inhalation: budesonide days to weeks; formoterol 1-3 minutes |
| Duration of Action | Budesonide: 12 hours; formoterol: 12 hours (maintenance), up to 12 hours for bronchodilation |
2 inhalations (albuterol 180 mcg / budesonide 160 mcg) orally inhaled twice daily (morning and evening), maximum 2 inhalations twice daily.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dose adjustment required for renal impairment; drug is primarily hepatically metabolized. |
| Liver impairment | No specific dose adjustment in Child-Pugh A or B; use with caution in severe hepatic impairment (Child-Pugh C) due to potential increased systemic exposure. |
| Pediatric use | Approved for ages 12 years and older: same as adult dosing (2 inhalations twice daily). Not indicated for children <12 years. |
| Geriatric use | No specific dose adjustment; start at lower end of dosing range due to potential for increased systemic exposure and comorbidities; monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AIRSUPRA (AIRSUPRA).
| Breastfeeding | Albuterol: Excreted into breast milk in small amounts; estimated infant dose <0.1% of maternal weight-adjusted dose. No adverse effects reported in infants. Budesonide: Low systemic absorption and rapid first-pass metabolism; inhaled dose leads to negligible milk levels. M/P ratio not established for the combination; for albuterol, M/P ratio ~0.24. Infant exposure is minimal. Benefits of maternal asthma control outweigh theoretical risks. Consider using at lowest effective dose. |
| Teratogenic Risk | AIRSUPRA (albuterol/budesonide) is a combination of a beta-2 agonist and an inhaled corticosteroid. For albuterol: Epidemiological studies suggest no increased risk of major congenital malformations when used during pregnancy; however, high doses may cause maternal tachycardia and hyperglycemia. For budesonide: Extensive data (over 10,000 pregnancies) indicate no increased risk of congenital anomalies with inhaled budesonide; systemic absorption is low. First trimester: No specific teratogenic risk identified from human data. Second and third trimesters: No fetal toxicity expected at therapeutic doses; however, beta-agonists may theoretically cause fetal tachycardia or hypoglycemia if used excessively. Overall, AIRSUPRA is considered low risk when used as indicated for asthma control. |
■ FDA Black Box Warning
No boxed warning is present in the FDA-approved labeling for AIRSUPRA.
| Common Effects | Headache Drowsiness Dizziness Nausea |
| Serious Effects |
["Hypersensitivity to albuterol, budesonide, or any ingredient in AIRSUPRA.","Status asthmaticus as primary therapy (requires rapid-acting bronchodilator).","Severe hypersensitivity to milk proteins (budesonide contains lactose with trace milk proteins)."]
| Precautions | ["Use of long-acting beta2-agonists as monotherapy without inhaled corticosteroid in asthma increases risk of asthma-related death; AIRSUPRA contains budesonide to mitigate this risk.","Monitor for worsening asthma symptoms, paradoxical bronchospasm, and hypersensitivity reactions.","May cause hypercorticism and adrenal suppression at high doses or prolonged use.","Use with caution in patients with cardiovascular disorders, especially coronary insufficiency, arrhythmias, and hypertension, due to albuterol's sympathomimetic effects.","Hypokalemia and hyperglycemia have been reported with beta-agonists.","Systemic corticosteroid withdrawal effects may occur upon switching from systemic corticosteroids to inhaled budesonide.","Patients with active or quiescent tuberculosis, fungal, bacterial, viral, or parasitic infections should be monitored."] |
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| Fetal Monitoring | Monitor maternal respiratory function (peak flow, FEV1) and fetal growth via ultrasound if asthma is severe or poorly controlled. Assess maternal blood glucose and blood pressure in women with comorbidities. Fetal heart rate monitoring may be considered if high doses of albuterol are used near term due to potential for fetal tachycardia. No specific monitoring required for budesonide component. |
| Fertility Effects | No evidence of impaired fertility in humans. In animal studies, high-dose budesonide caused reduced fecundity; however, inhaled doses produce low systemic exposure. Albuterol has no known adverse effects on fertility at therapeutic doses. AIRSUPRA is not expected to significantly impact female or male fertility. |
| Food/Dietary | No specific food interactions reported. Avoid grapefruit products as they may increase systemic exposure to budesonide; however, evidence is limited. Alcohol may worsen asthma symptoms in some patients. |
| Clinical Pearls | AIRSUPRA (albuterol/budesonide) is a pressurized metered-dose inhaler (pMDI) used for as-needed treatment or prevention of bronchoconstriction and reduction of exacerbations in asthma. It combines a short-acting beta-agonist (SABA) with an inhaled corticosteroid (ICS). Instruct patients to prime the inhaler with 4 test sprays before first use or if not used for 14 days. Rinse mouth with water and spit after each use to reduce oral candidiasis and dysphonia. Not for relief of acute bronchospasm in acute severe asthma; use separate SABA rescue inhaler. Do not exceed 12 inhalations in 24 hours. Monitor for adrenal insufficiency during stress or if switching from systemic corticosteroids. Contraindicated in severe hypersensitivity to any ingredient. |
| Patient Advice | Use AIRSUPRA exactly as prescribed; do not use more than 12 inhalations in 24 hours. · Shake the inhaler well for 5 seconds before each spray. · Prime the inhaler with 4 test sprays into the air away from your face before first use or if not used for 14 days. · Rinse your mouth with water and spit after each use to prevent thrush and hoarseness. · Do not use AIRSUPRA for sudden asthma symptoms; use your separate rescue inhaler (albuterol) instead. · If your symptoms worsen or you need more than 6 inhalations of AIRSUPRA in 24 hours, contact your healthcare provider. · Keep track of your asthma symptoms and peak flow readings; report any changes to your doctor. · Store the inhaler at room temperature away from heat and open flames. Do not puncture or incinerate the canister. · Seek emergency medical attention if you have signs of an allergic reaction: rash, hives, swelling, or trouble breathing. |