CORTONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORTONE (CORTONE).
Cortisone is a corticosteroid that binds to glucocorticoid receptors, leading to decreased inflammation through inhibition of phospholipase A2, reduced cytokine production, and suppression of immune cell migration.
| Metabolism | Cortisone is metabolized in the liver primarily by 11β-hydroxysteroid dehydrogenase type 1 to active cortisol; further metabolism via CYP3A4 and other reductases. |
| Excretion | Renal: ~90% as metabolites (glucuronides and sulfates), ~5% unchanged; biliary/fecal: ~5%. |
| Half-life | Terminal half-life: 8-12 hours (cortisone) but cortisone is a prodrug; active metabolite cortisol has half-life 1.5-2 hours. Clinical context: duration of action 8-12 hours due to prolonged receptor occupancy. |
| Protein binding | ~90% bound to corticosteroid-binding globulin (CBG) and albumin. |
| Volume of Distribution | 0.3-0.5 L/kg; distributes into total body water. |
| Bioavailability | Oral: ~25% due to extensive first-pass metabolism; IM: 100%. |
| Onset of Action | Oral: 1-2 hours; IM: 2-4 hours. |
| Duration of Action | Duration: 8-12 hours following oral or IM administration; clinical effect may persist for 24 hours with supraphysiologic doses. |
| Molecular Weight | 360.44 |
Oral: 25-300 mg daily in 1-4 divided doses; typical initial dose 150-300 mg daily. IM/IV: 100-500 mg every 6-12 hours.
| Dosage form | TABLET |
| Renal impairment | GFR 10-50 mL/min: use 75% of normal dose. GFR <10 mL/min: use 50% of normal dose. |
| Liver impairment | Child-Pugh Class A: no adjustment. Class B: reduce dose by 25%. Class C: reduce dose by 50%. |
| Pediatric use | Oral: 0.1-2.8 mg/kg/day in 3-4 divided doses; IM/IV: 0.5-4.0 mg/kg/day every 6-12 hours. |
| Geriatric use | Initiate at lower end of dosing range; monitor for fluid retention, hyperglycemia, and osteoporosis; use lowest effective dose. |
| 1st trimester | Corticosteroids cross the placenta; increased risk of oral clefts at doses >10 mg/day; use only if clearly needed. |
| 2nd trimester | May cause fetal growth restriction; monitor fetal growth; use lowest effective dose. |
| 3rd trimester | May cause neonatal adrenal suppression; avoid chronic high doses; use short courses if necessary. |
Clinical note
Comprehensive clinical and safety monograph for CORTONE (CORTONE).
| Placental transfer | Prednisolone crosses the placenta but is partially inactivated by placental 11β-HSD2; fetal levels are about 10% of maternal levels. |
| Breastfeeding | Prednisolone is excreted into breast milk in low concentrations; doses up to 40 mg/day are considered compatible with breastfeeding; monitor infant for adrenal suppression. |
■ FDA Black Box Warning
No FDA black box warning for CORTONE.
| Serious Effects |
Systemic fungal infectionHypersensitivity to prednisolone or any componentIntrathecal administration (contraindicated)
| Precautions | Immunosuppression and increased infection risk, Adrenal suppression with prolonged use, Osteoporosis with long-term therapy, Hyperglycemia and diabetes exacerbation, Cushing's syndrome with high doses |
| Food/Dietary | Avoid grapefruit and grapefruit juice (can increase cortisone levels). Limit high-sodium foods to reduce fluid retention. May require increased potassium intake (bananas, oranges) if hypokalemic. Avoid alcohol as it may increase risk of GI ulcers. |
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| Lactation Rating |
| L2 |
| Teratogenic Risk | CORTONE (cortisone) is a corticosteroid. In the first trimester, systemic use may be associated with a small increased risk of cleft palate (odds ratio ~1.3-1.5). In the second and third trimesters, chronic high doses may cause fetal adrenal suppression, intrauterine growth restriction, and premature birth. Risk is dose-dependent and duration-dependent. |
| Fetal Monitoring | Maternal: blood pressure, blood glucose, serum electrolytes, signs of infection, adrenal suppression. Fetal: ultrasound for growth assessment every 4-6 weeks if used chronically in second/third trimesters; neonatal assessment for adrenal insufficiency if used near term. |
| Fertility Effects | Corticosteroids may disrupt normal menstrual cycles and reduce fertility by inhibiting gonadotropin release. However, at low doses or as replacement therapy, fertility is generally unaffected. Withdrawal may restore normal function. |
| Clinical Pearls |
| Cortone (cortisone acetate) is a glucocorticoid with significant mineralocorticoid activity; monitor for sodium retention, hypokalemia, and hypertension. Taper withdrawal to avoid adrenal crisis. Use lowest effective dose. Not for acute stress unless supplemental doses given. Contraindicated in systemic fungal infections. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not stop suddenly; follow your doctor's tapering plan. · Report signs of infection (fever, sore throat) or unusual weight gain/swelling. · Avoid live vaccines while on this medication. · Carry a medical alert card indicating steroid use. · Monitor blood sugar if diabetic; may increase blood glucose. · Avoid grapefruit juice as it can increase drug levels. |