CORTISONE ACETATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORTISONE ACETATE (CORTISONE ACETATE).
Corticosteroid with glucocorticoid and mineralocorticoid activity; binds to glucocorticoid receptors, modulating gene expression to suppress inflammation and immune responses.
| Metabolism | Hepatic reduction and conjugation; primarily metabolized by 5α- and 5β-reductases and 3α-hydroxysteroid dehydrogenase. |
| Excretion | Renal (approximately 90% as metabolites, <5% unchanged); biliary/fecal (<5%) |
| Half-life | 30 minutes (plasma half-life of cortisol); biological half-life 8-12 hours (due to intracellular receptor binding and transcriptional effects) |
| Protein binding | 90% bound to corticosteroid-binding globulin (CBG) and albumin |
| Volume of Distribution | 0.3-0.4 L/kg (largely confined to extracellular space; extensive tissue distribution for a corticosteroid) |
| Bioavailability | Oral: 20-30% (due to first-pass metabolism to cortisol); IM: approximately 100% |
| Onset of Action | Oral: 1-2 hours (glucocorticoid effects); IM: 1-2 hours; topical: variable, typically within days |
| Duration of Action | 8-12 hours (single oral or IM dose; clinical effects may persist up to 24-36 hours due to delayed feedback mechanisms) |
25-300 mg per day orally, in divided doses every 6-12 hours, depending on condition severity.
| Dosage form | TABLET |
| Renal impairment | No specific GFR-based adjustment required; caution in severe renal impairment due to fluid retention risk. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B/C: reduce dose by 50% and monitor for glucocorticoid adverse effects. |
| Pediatric use | 0.5-10 mg/kg/day orally in divided doses every 6-8 hours, maximum 300 mg/day. |
| Geriatric use | Start at lowest adult dose (e.g., 25 mg daily) and titrate carefully due to increased risk of osteoporosis, fluid retention, and hyperglycemia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CORTISONE ACETATE (CORTISONE ACETATE).
| Breastfeeding | Cortisone acetate is excreted into breast milk at low concentrations (M/P ratio approximately 0.2-0.5). At maternal doses up to 25 mg daily, infant exposure is minimal (<10% of maternal weight-adjusted dose). Monitor infant for adrenal suppression if mother on high doses. |
| Teratogenic Risk | First trimester: Cleft lip and palate risk increased (odds ratio ~1.3-3.4). Second/third trimester: Fetal adrenal suppression, low birth weight, and potential neurodevelopmental effects. Chronic high dose: Risk of premature rupture of membranes and intrauterine growth restriction. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to any component","Administration of live or attenuated vaccines (relative)","Concurrent use with antidiabetic therapy may require dose adjustment (relative)"]
| Precautions | ["Immunosuppression and increased susceptibility to infections","Adrenal suppression with prolonged use","Osteoporosis and increased fracture risk","Cushing's syndrome with chronic therapy","Exacerbation of diabetes mellitus","Increased intraocular pressure and glaucoma","Gastrointestinal perforation risk","Psychiatric disturbances including euphoria and psychosis"] |
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| Fetal Monitoring | Maternal: Blood pressure, blood glucose, weight, signs of infection. Fetal: Ultrasound for growth and amniotic fluid volume. Neonatal: Assess for adrenal insufficiency after delivery if maternal use in third trimester. |
| Fertility Effects | High doses may inhibit ovulation and cause menstrual irregularities due to suppression of gonadotropins and direct ovarian effects. Reversible upon dose reduction. |