STERANE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STERANE (STERANE).
Sterane (prednisolone) is a glucocorticoid that binds to the glucocorticoid receptor, leading to modulation of gene expression and suppression of inflammation by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis, and decreasing cytokine production.
| Metabolism | Primarily hepatic via CYP3A4; prednisolone is the active metabolite of prednisone. |
| Excretion | Renal (approximately 70% as unchanged drug and glucuronide conjugate), biliary/fecal (approximately 30%) |
| Half-life | Terminal elimination half-life is approximately 2.5 hours (range 2-3 hours) in adults with normal renal function; clinically, this supports twice-daily dosing |
| Protein binding | Approximately 95% bound, primarily to albumin and corticosteroid-binding globulin |
| Volume of Distribution | 0.5-1.0 L/kg; reflects moderate tissue penetration and distribution into extracellular fluid |
| Bioavailability | Oral: approximately 80% (range 70-90%) |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours; clinical note: duration may be prolonged in hepatic impairment |
| Molecular Weight | 360.44 |
100 mg orally every 12 hours
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >30 mL/min. For GFR 10-30 mL/min: 100 mg every 24 hours. For GFR <10 mL/min: 100 mg every 48 hours. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: 50% of normal dose. Child-Pugh Class C: avoid use. |
| Pediatric use | 1.5 mg/kg orally every 12 hours, maximum 100 mg per dose. |
| Geriatric use | Start at 50 mg every 12 hours, titrate based on renal function and tolerability. |
| 1st trimester | Prednisone crosses placenta; associated with cleft palate in animal studies, but risk in humans is low. Use only if clearly needed. |
| 2nd trimester | May be used for maternal benefit; monitor fetal growth. Potential for adrenal suppression in neonate if used near term. |
| 3rd trimester | Risk of neonatal adrenal suppression if used in high doses near delivery. Use lowest effective dose. |
Clinical note
Comprehensive clinical and safety monograph for STERANE (STERANE).
| Placental transfer | Prednisone crosses the placenta; approximately 10-20% of maternal concentration reaches fetal circulation. Inactive prednisone is converted to active prednisolone in the fetus. |
| Breastfeeding | Prednisone is excreted into breast milk in small amounts. Maternal doses up to 20 mg/day are generally considered compatible with breastfeeding. Higher doses may require waiting 4 hours after dose to nurse. |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionsHypersensitivity to prednisone or any componentAdministration of live or live-attenuated vaccines in patients receiving immunosuppressive doses
| Precautions | Immunosuppression and increased risk of infections, Adrenal suppression with prolonged use, Osteoporosis with long-term therapy, Gastrointestinal perforation risk (especially in patients with GI disease), Exacerbation of systemic fungal infections, Kaposi's sarcoma has been reported, Neuropsychiatric reactions (e.g., euphoria, psychosis), Corticosteroid-induced myopathy, Growth suppression in children, Ocular effects (e.g., glaucoma, cataracts) |
| Food/Dietary | Grapefruit and grapefruit juice inhibit CYP3A4, increasing prednisolone levels; avoid concurrent use. High-sodium foods may exacerbate fluid retention and hypertension; advise low-sodium diet. Alcohol may increase risk of gastrointestinal ulcers; limit or avoid. Calcium and vitamin D supplementation recommended to counteract bone loss. |
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| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | First trimester: Cleft palate risk increased (odds ratio 3.35); second and third trimester: Intrauterine growth restriction, adrenal suppression, premature birth. Overall FDA category C (animal teratogenicity, human data limited). |
| Fetal Monitoring | Monitor maternal blood glucose, blood pressure, weight gain; fetal growth ultrasound every 4-6 weeks in 2nd/3rd trimester; assess for neonatal adrenal insufficiency at birth. |
| Fertility Effects | May impair ovulation (dose-dependent) with prolonged use; reversible upon discontinuation. No evidence of permanent infertility. |
| Clinical Pearls | Sterane (prednisolone) is a potent corticosteroid; use the lowest effective dose for the shortest duration to minimize adverse effects. Taper dose upon discontinuation after prolonged therapy (>2 weeks) to avoid adrenal crisis. Monitor for hyperglycemia, especially in diabetic patients; consider insulin adjustment. Avoid live vaccines during therapy. For acute exacerbations, a short course can be life-saving. Be cautious in patients with osteoporosis, hypertension, or peptic ulcer disease. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not stop abruptly; follow a tapering schedule as prescribed. · Report any signs of infection (fever, sore throat) or unusual bruising/bleeding. · Avoid live vaccines (e.g., MMR, nasal flu) while on this medication. · Monitor blood sugar if diabetic; report increased thirst or urination. · Carry a medical alert card indicating corticosteroid use. · Avoid grapefruit and grapefruit juice as they may increase drug levels. · Limit salt intake and maintain adequate calcium/vitamin D to prevent bone loss. |