CORTEF ACETATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORTEF ACETATE (CORTEF ACETATE).
Corticosteroid with anti-inflammatory and immunosuppressant activity; binds to glucocorticoid receptors, modulating gene expression and inhibiting phospholipase A2, thereby reducing prostaglandin and leukotriene synthesis.
| Metabolism | Hepatic; primarily via CYP3A4. |
| Excretion | Primarily renal as inactive metabolites; less than 5% unchanged. Biliary/fecal elimination is minimal (<2%). |
| Half-life | Plasma terminal half-life is approximately 1.5-2 hours. However, biologic half-life (duration of adrenal suppression) is 18-36 hours due to intracellular receptor binding. |
| Protein binding | 90-95% bound to corticosteroid-binding globulin (CBG) and albumin. |
| Volume of Distribution | 0.3-0.6 L/kg; distributes into total body water with higher concentrations in liver and kidney. |
| Bioavailability | Oral: 60-70% (first-pass metabolism reduces absorption); IM: 80-100% (complete absorption from depot site). |
| Onset of Action | Oral: 2-4 hours; Intramuscular: 6-12 hours; Intravenous: immediate (within minutes for hemodynamic effects). |
| Duration of Action | Oral: 1.5-2 days for hypothalamic-pituitary-adrenal axis suppression; IM: 1-5 days depending on dose and formulation; IV: 4-6 hours for physiological effects. |
Adult: 5-60 mg orally every 6-12 hours (hydrocortisone base equivalent), or 10-240 mg IV/IM every 12 hours (as hydrocortisone sodium succinate). Dose depends on severity and condition.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment for GFR; hydrocortisone is primarily hepatically metabolized. However, in ESRD, dose may need reduction due to potential accumulation of inactive metabolites; monitor for side effects. |
| Liver impairment | In severe hepatic impairment (Child-Pugh C), consider dose reduction by 50% or more due to reduced clearance. Moderate impairment (Child-Pugh B) may require 25-50% reduction. Use with caution. |
| Pediatric use | Initial: 1-2 mg/kg orally every 6-8 hours (hydrocortisone base), or IV/IM 1-2 mg/kg every 6-8 hours (as sodium succinate). Maintenance dose varies by condition, typically 0.5-2 mg/kg/day divided q6-12h. |
| Geriatric use | Start at lowest effective dose; elderly may have increased risk of osteoporosis, hyperglycemia, and immunosuppression. Use for shortest duration. No specific dose adjustment but monitor closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CORTEF ACETATE (CORTEF ACETATE).
| Breastfeeding | Hydrocortisone is excreted into breast milk in low amounts. The milk-to-plasma ratio (M/P) is approximately 0.25. At maternal doses up to 80 mg/day, the relative infant dose is estimated <10% of maternal weight-adjusted dose, considered compatible with breastfeeding. However, monitor infant for adrenal suppression if high maternal doses used long-term. Use lowest effective dose. |
| Teratogenic Risk | Corticosteroids including Cortef Acetate (hydrocortisone acetate) are generally considered low risk for major congenital malformations. First trimester exposure: No consistent association with oral clefts or other malformations in human studies, though a small increased risk of cleft lip/palate was noted in some studies with first trimester use. Second/third trimester: May cause fetal growth restriction, adrenal suppression, and preterm delivery if used chronically. High systemic exposure may increase risk of preterm premature rupture of membranes. Overall, FDA Pregnancy Category C (risk cannot be ruled out). |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infections, administration of live or live attenuated vaccines in patients receiving immunosuppressive doses of corticosteroids, hypersensitivity to hydrocortisone or any component of the formulation.
| Precautions | Suppression of hypothalamic-pituitary-adrenal axis, increased susceptibility to infections, corticosteroid-induced osteoporosis, glaucoma, cataracts, exacerbation of systemic fungal infections, risk of Kaposi sarcoma, and live or attenuated vaccine administration contraindicated during immunosuppressive doses. |
| Food/Dietary | Avoid excessive salt intake as corticosteroids can cause sodium retention. Limit caffeine and alcohol. Grapefruit may increase systemic exposure; avoid large amounts. Monitor potassium intake if taking diuretics concurrently. |
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| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, and signs of infection. For fetal growth, serial ultrasound for growth restriction if prolonged therapy. Assess newborn for adrenal insufficiency if maternal use continued until delivery. Monitor fetal heart rate during labor if high doses given parenterally. |
| Fertility Effects | No direct evidence of impaired fertility in humans. High doses may suppress hypothalamic-pituitary-adrenal axis and gonadotropins, potentially disrupting menstrual cycle and ovulation. Reversible upon dose reduction or discontinuation. |
| Clinical Pearls | Cortef Acetate (hydrocortisone acetate) is a corticosteroid for intra-articular, soft tissue, or intralesional injection. Avoid injection into infected areas or unstable joints. Do not administer intravenously. Limit frequency to every 3-4 weeks to avoid joint damage. Monitor for adrenal suppression with prolonged use. |
| Patient Advice | Do not stop taking this medication abruptly; dose must be tapered under medical supervision. · Report any signs of infection (fever, pain, redness) at injection site immediately. · Inform all healthcare providers you are using this medication, including before surgery or vaccinations. · Avoid close contact with individuals who have chickenpox or measles. |