AEROSEB-DEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AEROSEB-DEX (AEROSEB-DEX).
The combination product contains a corticosteroid (dexamethasone) which suppresses inflammation by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis, and a topical antibiotic (usually neomycin or polymyxin B) which inhibits bacterial protein synthesis or disrupts bacterial cell membranes.
| Metabolism | Dexamethasone is metabolized primarily in the liver via CYP3A4; topical antibiotics (neomycin, polymyxin B) are minimally absorbed and not significantly metabolized. |
| Excretion | Renal elimination of unchanged drug accounts for 30-40% of the dose; fecal/biliary elimination is 50-60% as metabolites. Less than 10% is excreted unchanged in feces. |
| Half-life | Terminal elimination half-life is 12-15 hours in adults with normal renal function; prolonged to 24-30 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 85% bound to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd is 3-4 L/kg, indicating extensive tissue distribution with accumulation in liver and kidneys. |
| Bioavailability | Oral: 40-50% due to first-pass metabolism; Topical: 5-10% systemically; IV: 100%. |
| Onset of Action | Oral: 30-60 minutes; IV: within 5 minutes; Topical: 2-4 hours for local effect. |
| Duration of Action | Oral: 12-24 hours for sustained effect; IV: 6-12 hours; Topical: 12-24 hours. Duration may be extended in hepatic impairment. |
| Molecular Weight | 434.54 |
2 puffs (100 mcg each) intranasally twice daily
| Dosage form | AEROSOL |
| Renal impairment | No adjustment required for any GFR level |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B/C: no data available; use with caution |
| Pediatric use | Children 6-11 years: 1 puff (50 mcg) per nostril twice daily; Children ≥12 years: same as adult |
| Geriatric use | No specific dose adjustment; monitor for adrenal suppression and osteoporosis risk with prolonged use |
| 1st trimester | Avoid; studies show increased risk of orofacial clefts and cardiovascular malformations. |
| 2nd trimester | Avoid; risk of adrenal suppression in fetus, potential for intrauterine growth restriction. |
| 3rd trimester | Avoid; may cause neonatal adrenal suppression, hypoglycemia, and cataracts. |
Clinical note
Comprehensive clinical and safety monograph for AEROSEB-DEX (AEROSEB-DEX).
| Placental transfer | Crosses placenta; metabolized by placental 11β-HSD2 but still reaches fetal circulation. |
| Breastfeeding | Enters breast milk; use with caution due to potential for growth suppression and interference with endogenous corticosteroid production in the infant. |
| Lactation Rating |
■ FDA Black Box Warning
Prolonged use may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision, and posterior subcapsular cataract formation. Prolonged use may suppress the host response and thus increase the hazard of secondary ocular infections. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids.
| Serious Effects |
Systemic fungal infectionsKnown hypersensitivity to corticosteroidsAdministration of live or live-attenuated vaccines
| Precautions | Prolonged use may lead to ocular hypertension/glaucoma, Posterior subcapsular cataract formation, Delayed wound healing, Secondary ocular infections (including fungal infections), Corneal/scleral thinning and perforation, Systemic absorption with prolonged use (especially in children), Avoid use in patients with known hypersensitivity to any component |
| Food/Dietary | No specific food interactions. Avoid grapefruit juice as it may increase systemic exposure to ciclesonide via CYP3A4 inhibition. |
Loading safety data…
| L3 - Moderate Risk |
| Teratogenic Risk | Pregnancy Category C. First trimester: potential for teratogenicity based on animal studies; avoid unless benefit outweighs risk. Second/third trimester: drug may cause fetal harm due to pharmacological effects; use only if clearly needed. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and respiratory status. Fetal monitoring for signs of distress or growth restriction in prolonged use. |
| Fertility Effects | Animal studies indicate potential impairment of fertility at high doses. Human data limited; may affect ovulatory function or spermatogenesis. |
| Clinical Pearls | AEROSEB-DEX is a fixed-dose combination of an inhaled corticosteroid (ciclesonide) and a long-acting beta-agonist (formoterol). Use as maintenance therapy for asthma, not for acute bronchospasm. Rinse mouth after inhalation to prevent oral candidiasis. Monitor for adrenal suppression with prolonged use. Dose formoterol component at low to moderate doses to minimize risk of asthma-related death. |
| Patient Advice | Use regularly as prescribed, not for sudden breathing problems. · Rinse mouth with water after each use to prevent thrush. · Do not stop suddenly; taper under doctor guidance. · Seek emergency if rescue inhaler not effective. · Report worsening asthma, chest pain, or signs of steroid excess. |