DEXONE 1.5
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEXONE 1.5 (DEXONE 1.5).
Dexamethasone is a long-acting glucocorticoid receptor agonist that suppresses inflammation and immune responses by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis, and modulating gene expression.
| Metabolism | Primarily hepatic via CYP3A4; also metabolized by other CYP450 enzymes. |
| Excretion | Renal (primarily as metabolites, ~60%), biliary/fecal (~30%), with <5% excreted unchanged. |
| Half-life | Terminal half-life approximately 3-4 hours (dexamethasone), with clinical effects persisting 36-54 hours due to glucocorticoid receptor-mediated actions. |
| Protein binding | Approximately 77% bound, primarily to albumin and corticosteroid-binding globulin (CBG). |
| Volume of Distribution | 0.7-1.0 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 80-90%; Intramuscular: 100% (relative to IV). |
| Onset of Action | Intravenous: 15-30 minutes; Oral: 1-2 hours; Intramuscular: 30-60 minutes. |
| Duration of Action | Duration of anti-inflammatory effect: 24-48 hours after a single dose, with adrenal suppression lasting up to 72 hours. |
1.5 mg orally once daily
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR >30 mL/min; for GFR 10-30 mL/min, use 0.75 mg once daily; for GFR <10 mL/min, use 0.5 mg once daily |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 0.75 mg once daily; Child-Pugh C: 0.5 mg once daily |
| Pediatric use | 0.02-0.05 mg/kg orally once daily; maximum 1.5 mg/day |
| Geriatric use | Start at 0.75 mg orally once daily; titrate based on response and tolerance |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DEXONE 1.5 (DEXONE 1.5).
| Breastfeeding | Dexamethasone is excreted in human breast milk; M/P ratio is approximately 0.4–0.7. Doses up to 20 mg/day are considered compatible with breastfeeding, but monitor infant for adrenal suppression if maternal therapy is prolonged or high-dose. |
| Teratogenic Risk | DEXONE 1.5 (dexamethasone 1.5 mg) is a corticosteroid. First trimester: Increased risk of oral clefts (odds ratio ~3.4). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, and oligohydramnios with prolonged use. Corticosteroids are generally avoided unless maternal benefit outweighs fetal risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to dexamethasone or any component","Administration of live or live-attenuated vaccines during immunosuppressive therapy (relative)"]
| Precautions | ["Immunosuppression and increased susceptibility to infections","Hypothalamic-pituitary-adrenal (HPA) axis suppression with prolonged use","Adrenal insufficiency upon withdrawal","Gastrointestinal perforation (especially in inflammatory bowel disease)","Osteoporosis with long-term use","Cushing's syndrome with high doses","Exacerbation of systemic fungal infections","Live or live-attenuated vaccines contraindicated during immunosuppressive doses","Use caution in patients with hypertension, congestive heart failure, or ocular herpes simplex"] |
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| Fetal Monitoring | Monitor maternal blood glucose (corticosteroid-induced hyperglycemia), blood pressure, weight, and edema. Fetal monitoring: serial ultrasound for growth restriction and amniotic fluid volume; consider fetal adrenal suppression if prolonged therapy. |
| Fertility Effects | Dexamethasone may interfere with hypothalamic-pituitary-adrenal axis, potentially causing menstrual irregularities or transient anovulation. In males, no direct effect on spermatogenesis reported at therapeutic doses. |