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. |
| Molecular Weight | 392.46 Da |
| 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 | CORTALONE (dexamethasone) is a potent corticosteroid. Use in first trimester is associated with increased risk of orofacial clefts (odds ratio ~1.6-3.3). Should be used only if clearly needed and after counseling. |
| 2nd trimester | Use in second trimester may cause fetal adrenal suppression with prolonged therapy. Dose-dependent risk of intrauterine growth restriction (IUGR) and preterm birth. |
| 3rd trimester | Third trimester use can cause neonatal adrenal insufficiency, hyperglycemia, and electrolyte disturbances. Risk of low birth weight and hypothalamic-pituitary-adrenal axis suppression. |
Clinical note
Comprehensive clinical and safety monograph for CORTALONE (CORTALONE).
| Placental transfer | Dexamethasone readily crosses the placenta with a maternal-to-fetal transfer rate of approximately 75-85%. It is partially inactivated by placental 11β-HSD2, but still significant fetal exposure occurs. |
| Breastfeeding |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionsHypersensitivity to dexamethasone or any componentLive or live-attenuated vaccines (concurrent use)Untreated systemic infectionsIdiopathic thrombocytopenic purpura (if used as intrathecal route)
| 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 |
| Food/Dietary | No clinically significant food interactions have been reported for topical hydrocortisone acetate. However, patients with allergies to dairy or corn products should check with their pharmacist regarding excipients, as formulations may vary. |
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| Dexamethasone is excreted into breast milk in low amounts (estimated infant dose ~3.6-7.6% of maternal weight-adjusted dose). Short-term use is considered compatible with breastfeeding, but advise monitoring for potential adrenal suppression and growth impairment in premature or low-birth-weight infants. High doses or prolonged use should prompt caution. |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls | CORTALONE is a brand name for hydrocortisone acetate, a topical corticosteroid used for its anti-inflammatory and antipruritic effects. It is classified as a low-potency corticosteroid (Group VII). For best results, apply a thin film to affected areas and rub in gently. Avoid prolonged use on the face, intertriginous areas, or under occlusive dressings due to increased risk of systemic absorption and local adverse effects. Do not use on infected lesions unless accompanied by appropriate anti-infective therapy. |
| Patient Advice | Use only as directed; do not apply to large areas or for longer than prescribed. · Avoid contact with eyes, mouth, and open wounds; if contact occurs, rinse thoroughly with water. · Do not bandage or cover the treated area unless advised by your healthcare provider. · Report any signs of skin irritation, infection, or worsening condition to your doctor. · Do not use this medication for conditions other than those for which it was prescribed. |