DELTA-CORTEF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DELTA-CORTEF (DELTA-CORTEF).
Glucocorticoid; binds to glucocorticoid receptors, modulating gene expression to suppress inflammation, immune response, and adrenal function.
| Metabolism | Primarily hepatic via CYP3A4. |
| Excretion | Renal: approximately 80-90% as unchanged drug and metabolites (primarily 20β-dihydrocortisone and other inactive conjugates); biliary/fecal: <10%. |
| Half-life | Terminal elimination half-life: 1.5-2.5 hours (mean ~2 hours) for prednisolone; clinical context: short-acting glucocorticoid, requires multiple daily dosing for sustained anti-inflammatory effect, adrenocortical suppression lasts approximately 1.25-1.5 days after discontinuation. |
| Protein binding | Prednisolone: 65-91% bound to corticosteroid-binding globulin (CBG, transcortin) and albumin; binding is dose-dependent and saturable. |
| Volume of Distribution | Vd: 0.5-1.5 L/kg; reflects extensive tissue distribution and penetration into intracellular compartments. |
| Bioavailability | Oral: 70-90%; IM: 80-100%; intra-articular: locally high, systemic absorption slow and incomplete; rectal: 30-50%. |
| Onset of Action | IV: immediate (minutes); oral: 1-2 hours; IM: 1-2 hours; intra-articular: 2-4 hours. |
| Duration of Action | Duration of anti-inflammatory effect: 12-36 hours; duration of HPA axis suppression: 1.25-1.5 days; clinical note: single dose effect may last up to 36 hours; repeated dosing may prolong effect. |
| Molecular Weight | 360.44 |
Prednisolone (DELTA-CORTEF) typical adult dose: 5-60 mg orally once daily or in divided doses, depending on condition. For acute exacerbations: 20-60 mg orally daily. Route: oral. Frequency: once daily or divided.
| Dosage form | TABLET |
| Renal impairment | No specific GFR-based dose adjustment required. Use with caution in severe renal impairment due to fluid retention risk. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: consider dose reduction by 50% due to reduced clearance. |
| Pediatric use | Children: 0.5-2 mg/kg/day orally in divided doses every 6-12 hours, up to 60 mg/day. For acute asthma: 1-2 mg/kg/day, max 60 mg/day. |
| Geriatric use | Elderly: start at lowest effective dose; monitor for osteoporosis, hyperglycemia, and fluid retention. Consider calcium and vitamin D supplementation. |
| 1st trimester | Prednisolone crosses the placenta; associated with a small increased risk of oral clefts (about 1-2 per 1000) if used in first trimester. Use only if clearly needed. |
| 2nd trimester | May cause fetal adrenal suppression, but generally considered safe for maternal conditions when benefit outweighs risk. |
| 3rd trimester | Chronic use may lead to neonatal adrenal suppression, premature birth, or low birth weight. Monitor for signs of adrenal insufficiency in the neonate. |
Clinical note
Comprehensive clinical and safety monograph for DELTA-CORTEF (DELTA-CORTEF).
| Placental transfer | Prednisolone is oxidized to prednisone by placental 11β-HSD2, but some active drug crosses. The extent is low to moderate, with fetal concentrations about 10-20% of maternal levels. |
| Breastfeeding | Prednisolone is excreted into breast milk in low doses (<0.1% of maternal dose for <80 mg/day). Considered compatible with breastfeeding; monitoring infant for possible adrenal suppression is not routinely necessary. |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infections (except in patients with adrenal insufficiency)Live or live-attenuated vaccines (risk of disseminated infection)
| Precautions | Immunosuppression and increased infection risk, Hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome with prolonged use, Osteoporosis, Gastrointestinal perforation, Psychiatric disturbances, Exacerbation of diabetes mellitus, Hypertension |
| Food/Dietary | Grapefruit and grapefruit juice may increase serum levels; avoid concurrent use. High-sodium foods should be limited to reduce fluid retention and hypertension. Potassium-rich foods (e.g., bananas, oranges) may be recommended to counteract hypokalemia. |
Loading safety data…
| Lactation Rating | L2 - Safe |
| Teratogenic Risk | First trimester: Increased risk of oral clefts (odds ratio ~3.4). Second/third trimester: Fetal adrenal suppression, growth restriction, preterm birth. Risk is dose-dependent and cumulative. |
| Fetal Monitoring | Monitor maternal blood pressure, glucose tolerance, signs of infection. Fetal ultrasound for growth restriction and amniotic fluid volume. Assess for adrenal insufficiency in neonates. |
| Fertility Effects | No direct impairment of fertility. Chronic use may disrupt menstrual cycles or ovulation due to hypothalamic-pituitary-adrenal axis suppression. |
| Clinical Pearls | DELTA-CORTEF (prednisolone) is a corticosteroid with rapid onset; avoid abrupt discontinuation after prolonged use to prevent adrenal crisis. Monitor for hyperglycemia, especially in diabetics. Use lowest effective dose for shortest duration. Not for use in systemic fungal infections. Live vaccines contraindicated during therapy. |
| Patient Advice | Take with food or milk to reduce gastrointestinal irritation. · Do not stop taking suddenly; dose must be tapered under medical supervision. · Report unusual weight gain, swelling, black/tarry stools, or vision changes. · Avoid exposure to infections; inform healthcare provider if exposed to chickenpox or measles. · Carry medical identification indicating corticosteroid use. |