SUSTAIRE
Clinical safety rating
cautionComprehensive clinical and safety monograph for SUSTAIRE (SUSTAIRE).
SUSTAIRE (budesonide/formoterol) is a fixed-dose combination of an inhaled corticosteroid (budesonide) and a long-acting beta2-adrenergic agonist (formoterol). Budesonide exerts anti-inflammatory effects by binding to glucocorticoid receptors, inhibiting inflammatory mediator release, and reducing airway hyperresponsiveness. Formoterol selectively activates beta2-adrenergic receptors in bronchial smooth muscle, causing bronchodilation via increased cAMP production.
| Metabolism | Budesonide: extensively metabolized in the liver via CYP3A4 to inactive metabolites; formoterol: partially metabolized via glucuronidation and O-demethylation, with minor CYP involvement. |
| Excretion | Primarily renal excretion (80-90% unchanged); minor biliary/fecal elimination (10-20%). |
| Half-life | Terminal elimination half-life of 8-12 hours in healthy adults; prolonged in renal impairment. |
| Protein binding | Approximately 95% bound to albumin. |
| Volume of Distribution | 0.2-0.3 L/kg; indicates limited extravascular distribution primarily in plasma and interstitial fluid. |
| Bioavailability | Oral: 70-80% due to first-pass metabolism; intravenous: 100%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: immediate (within minutes). |
| Duration of Action | Oral: 6-8 hours; intravenous: 4-6 hours; duration may be extended in renal impairment. |
| Molecular Weight | 283.37 Da |
50 mg orally twice daily
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 30-59 mL/min: 50 mg once daily; GFR 15-29 mL/min: 25 mg once daily; GFR <15 mL/min: not recommended |
| Liver impairment | Child-Pugh A: 50 mg twice daily; Child-Pugh B: 25 mg twice daily; Child-Pugh C: 12.5 mg once daily |
| Pediatric use | Weight-based: 0.5 mg/kg orally twice daily, max 25 mg per dose |
| Geriatric use | Age >65 years: initiate at 25 mg twice daily; monitor renal function |
| 1st trimester | Insufficient human data; animal studies show embryotoxicity at high doses; avoid use. |
| 2nd trimester | Limited data; potential risk of fetal respiratory depression with near-term use. |
| 3rd trimester | Avoid in third trimester; may cause fetal respiratory depression and withdrawal symptoms. |
Clinical note
Comprehensive clinical and safety monograph for SUSTAIRE (SUSTAIRE).
| Placental transfer | Crosses placenta; fetal plasma concentrations are approximately 50-70% of maternal levels. |
| Breastfeeding | Excreted in breast milk in low concentrations; use caution in nursing mothers, especially with premature infants or those with compromised respiratory function. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Pregnancy Category C. First trimester: risk of major malformations unknown, but animal studies show fetal harm. Second/third trimester: potential for fetal respiratory depression, hypotonia, and withdrawal syndrome with chronic use. Avoid use unless benefit outweighs risk. |
| Fetal Monitoring | Maternal: blood pressure, heart rate, respiratory status, and signs of sedation. Fetal: fetal heart rate monitoring during labor if used near term; assess neonatal respiratory status and Apgar scores. |
| Fertility Effects | No specific human data on fertility impairment. Animal studies show no significant reproductive effects. Theoretical risk of altered hormone levels with chronic use. |
■ FDA Black Box Warning
Long-acting beta2-adrenergic agonists (LABAs) increase the risk of asthma-related death. SUSTAIRE is contraindicated for use as primary therapy for acute asthma exacerbations. For asthma, use only as add-on therapy for patients not adequately controlled on low-to-medium dose inhaled corticosteroids (ICS) or whose disease severity warrants initiation of ICS and LABA.
| Serious Effects |
Hypersensitivity to SUSTAIRE or any componentSevere respiratory depressionAcute or severe bronchial asthmaKnown or suspected gastrointestinal obstructionConcurrent use of MAO inhibitors or within 14 days
| Precautions | LABA-associated asthma-related death; cardiovascular effects (tachycardia, hypertension); paradoxical bronchospasm; hypokalemia; hyperglycemia; increased susceptibility to infections; adrenal insufficiency with systemic steroid withdrawal; acute asthma exacerbation management. |
| Food/Dietary | No significant food interactions. Grapefruit or grapefruit juice may increase systemic exposure; avoid excessive consumption. No specific dietary restrictions required. |
| Clinical Pearls | SUSTAIRE is an inhaled corticosteroid (ICS) used for maintenance treatment of asthma. It is not indicated for acute bronchospasm. Rinse mouth with water after each use to prevent oral candidiasis. Titrate to lowest effective dose to minimize systemic effects. Monitor for growth suppression in children and adrenal insufficiency during stress or prolonged use. |
| Patient Advice | Use SUSTAIRE regularly as prescribed, not for sudden breathing problems. · Rinse your mouth with water after each use to prevent thrush. · Do not stop taking SUSTAIRE without consulting your doctor, even if you feel better. · Keep track of your symptoms and peak flow if advised. · Seek medical help if your rescue inhaler is not working or you need more puffs than usual. |
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