ORAPRED
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORAPRED (ORAPRED).
Prednisolone is a corticosteroid that binds to the glucocorticoid receptor, leading to modulation of gene expression and suppression of inflammatory cytokines, immune responses, and adrenal function.
| Metabolism | Primarily hepatic via CYP3A4; also undergoes reversible metabolism to inactive metabolites. |
| Excretion | Renal: approximately 60-80% as unchanged drug and conjugated metabolites; biliary/fecal: minor (5-10%) |
| Half-life | 4-5 hours (terminal); prolonged in renal impairment (up to 12+ hours in anuria) and hepatic dysfunction; clinical context: dosing interval adjustment in severe renal failure |
| Protein binding | Approximately 70-90%, primarily to albumin and corticosteroid-binding globulin (CBG) |
| Volume of Distribution | 0.8-1.2 L/kg; indicates extensive tissue distribution, including CNS penetration |
| Bioavailability | Oral: 60-90% (dependent on formulation, food reduces rate but not extent) |
| Onset of Action | Oral: 1-2 hours; IV: immediate (within minutes) for immunosuppression |
| Duration of Action | 12-24 hours; clinical note: dose-dependent, with higher doses extending lympholytic effect to 24-36 hours |
| Action Class | Glucocorticoids |
| Brand Substitutes | Predace 4 Tablet, Coelone 4mg Tablet, Pilsone 4mg Tablet, Premisol 4mg Tablet, Cortilog 4mg Tablet, Rednisol 8 Tablet, Prelid 8mg Tablet, Predace 8mg Tablet, Sterio 8 Tablet, MP 8mg Tablet, Prelid 16mg Tablet, Predace 16 Tablet, Mepresso T 16mg Tablet, Medrol 16mg Tablet, Rednisol 16mg Tablet |
5-60 mg orally once daily or divided as 5-15 mg every 4-12 hours; adjust based on response and condition.
| Dosage form | SOLUTION |
| Renal impairment | No specific dose adjustment required for GFR >30 mL/min; for GFR 10-30 mL/min, reduce dose by 50%; for GFR <10 mL/min, reduce dose by 75%. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use or reduce dose by 75%. |
| Pediatric use | 0.14-2 mg/kg/day orally in 3-4 divided doses; maximum 60 mg/day. |
| Geriatric use | Initiate at lowest effective dose; consider reduced starting dose (e.g., 2.5-5 mg/day) and monitor for increased sensitivity and adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORAPRED (ORAPRED).
| Breastfeeding | Prednisolone enters breast milk with a milk-to-plasma ratio of approximately 0.11-0.25. At maternal doses up to 40 mg daily, infant exposure is typically <2% of maternal weight-adjusted dose, considered compatible with breastfeeding. Monitor infant for signs of adrenal suppression if high maternal doses (>40 mg/day) prolonged. |
| Teratogenic Risk | Orapred (prednisolone sodium phosphate) crosses the placenta and is metabolized to prednisolone. First trimester exposure may increase risk of oral clefts (odds ratio 3-5 per 1000 births). Second/third trimester: risk of fetal adrenal suppression, intrauterine growth restriction, and preterm birth. Chronic high-dose use associated with oligohydramnios and premature rupture of membranes. |
■ FDA Black Box Warning
None
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to prednisolone or any component","Administration of live or live-attenuated vaccines with immunosuppressive doses"]
| Precautions | ["Immunosuppression and increased susceptibility to infections","Adrenal suppression with prolonged use","Osteoporosis risk with long-term therapy","Gastrointestinal perforation risk","Cushing's syndrome with high doses","Psychiatric disturbances","Growth suppression in children","Increased intraocular pressure and glaucoma","Fluid and electrolyte disturbances","Thrombotic events"] |
Loading safety data…
| Fetal Monitoring | Maternal: blood pressure, blood glucose, serum electrolytes, adrenal function (if prolonged use), bone density (chronic use). Fetal: growth ultrasound every 4-6 weeks in second/third trimester; amniotic fluid volume assessment; fetal heart rate monitoring if IUGR or oligohydramnios. Neonatal: monitor for signs of adrenal insufficiency (hypoglycemia, hypotension, failure to thrive) for 48-72 hours after delivery. |
| Fertility Effects | No direct evidence of impaired fertility in humans. High-dose corticosteroids may suppress gonadotropin release leading to menstrual irregularities or anovulation, reversible upon dose reduction or discontinuation. No known effects on spermatogenesis. |