CORTALONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORTALONE (CORTALONE).
Cortisone is a corticosteroid that binds to glucocorticoid receptors, modulating gene expression to suppress inflammation and immune response, and regulate metabolism.
| Metabolism | Cortisone is metabolized primarily in the liver via 11-beta-hydroxysteroid dehydrogenase to hydrocortisone (cortisol), and further metabolized by hepatic CYP3A4 and other reductases and hydroxylases. |
| Excretion | Primarily renal (60-70% as unchanged drug), with 10-20% biliary/fecal. |
| Half-life | Terminal elimination half-life is 3-5 hours in patients with normal renal function; prolonged to 12-24 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 85-90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating distribution into total body water and tissues. |
| Bioavailability | Oral: 70-80%; Intramuscular: 90-100%. |
| Onset of Action | Oral: 30-60 minutes; Intramuscular: 15-30 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 6-8 hours; IM: 6-12 hours; IV: 4-6 hours. Duration may be extended in renal impairment. |
| Action Class | Glucocorticoids |
| Brand Substitutes | Zefcort 6 Tablet, Sterozit 6mg Tablet, Mahacort DZ 6 Tablet, Ronicort 6mg Tablet, Flacort 6mg Tablet |
10-40 mg orally once daily in the morning; for acute exacerbations, up to 60 mg/day divided into 2-4 doses.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min; for GFR <30 mL/min, reduce dose by 50% and monitor for fluid retention. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use or reduce by 75% with close monitoring. |
| Pediatric use | 0.2-0.7 mg/kg/day orally in 1-2 divided doses; maximum 60 mg/day. |
| Geriatric use | Initiate at lowest effective dose (e.g., 5-10 mg/day); titrate slowly due to increased risk of osteoporosis, hyperglycemia, and immunosuppression. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CORTALONE (CORTALONE).
| Breastfeeding | Hydrocortisone enters breast milk in low concentrations (M/P ratio approx. 0.25). At maternal doses up to 20 mg daily, infant exposure is minimal and considered compatible with breastfeeding. Higher doses may suppress infant adrenal function. |
| Teratogenic Risk | CORTALONE (hydrocortisone) is a corticosteroid. First trimester: Increased risk of cleft palate (odds ratio 1.3-3.4). Second/third trimester: Risk of fetal adrenal suppression, growth restriction, and premature labor. Chronic use may cause neonatal adrenal insufficiency. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Systemic fungal infections","Known hypersensitivity to cortisone or any component of the formulation","Administration of live or live-attenuated vaccines","Idiopathic thrombocytopenic purpura (for intramuscular use)"]
| Precautions | ["Immunosuppression and increased risk of infections","Hypothalamic-pituitary-adrenal (HPA) axis suppression with prolonged use","Osteoporosis and increased fracture risk","Glaucoma and cataracts with long-term use","Fluid and electrolyte disturbances, including hypertension and hypokalemia","Gastrointestinal effects: peptic ulcer, pancreatitis","Growth suppression in children","Cushing's syndrome with chronic use","Wound healing impairment","Psychiatric disturbances: euphoria, insomnia, mood swings, psychosis"] |
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| Fetal Monitoring |
| Monitor maternal blood pressure, blood glucose, and signs of infection. Fetal growth ultrasound every 4-6 weeks if prolonged use. Assess for neonatal adrenal insufficiency after delivery (Cortrosyn stimulation test). |
| Fertility Effects | High doses may suppress hypothalamic-pituitary-adrenal axis and gonadotropin secretion, potentially causing menstrual irregularities and transient infertility. Low doses have minimal impact. |