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) |
| Molecular Weight | 402.48 |
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 | Corticosteroids including cortisone acetate are associated with increased risk of cleft palate when used in first trimester. Use only if clearly needed. |
| 2nd trimester | May be used for maternal benefit; monitor for intrauterine growth restriction and maternal glucose levels. |
| 3rd trimester | Use with caution; may cause fetal adrenal suppression. Avoid high doses near term to prevent neonatal adrenal crisis. |
Clinical note
Comprehensive clinical and safety monograph for CORTISONE ACETATE (CORTISONE ACETATE).
| Placental transfer | Crosses placenta; about 67% of maternal level is transferred to fetus. Metabolized by placental 11β-HSD2 to inactive cortisone, but active cortisol moiety can still affect fetus. |
| Breastfeeding | Cortisone acetate enters breast milk in low amounts. Short-term use up to 40 mg daily is considered compatible with breastfeeding. High doses may suppress infant adrenal function; monitor infant for growth and development. |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionsHypersensitivity to cortisone acetate or any componentAdministration of live virus vaccines (due to immunosuppression)Idiopathic thrombocytopenic purpura (relative contraindication, but absolute if severe)
| 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 |
| Food/Dietary | Avoid grapefruit juice (may increase corticosteroid levels). Limit sodium intake to reduce fluid retention and hypertension. Increase potassium intake (e.g., bananas, oranges) as corticosteroid can cause hypokalemia. Avoid alcohol as it may increase risk of gastrointestinal bleeding. |
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| Lactation Rating | L2 (Safer) |
| 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. |
| 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. |
| Clinical Pearls | Cortisone acetate is a prodrug requiring hepatic conversion to active hydrocortisone. Monitor for adrenal suppression during prolonged therapy; taper dose gradually. Use lowest effective dose for shortest duration. Antagonizes insulin, may exacerbate diabetes. Avoid live vaccines. Corticosteroids can mask infection symptoms. |
| Patient Advice | Take with food to reduce stomach upset. · Do not stop abruptly; dose must be tapered under medical supervision. · Report any signs of infection (fever, sore throat, cough). · Avoid live vaccines (e.g., MMR, nasal flu vaccine) while on this medication. · Monitor blood sugar regularly if you have diabetes. · Carry a medical alert card stating you are taking a corticosteroid. · Notify any healthcare provider of your corticosteroid use before surgery or emergency treatment. |