PREDAIR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PREDAIR (PREDAIR).
Prednisone is a prodrug that is converted to prednisolone, which binds to the glucocorticoid receptor, leading to anti-inflammatory and immunosuppressive effects via modulation of gene expression.
| Metabolism | Primarily hepatic, via reduction to inactive metabolites; prednisone is converted to active prednisolone by 11-beta-hydroxysteroid dehydrogenase. |
| Excretion | Renal: 75-90% as unchanged drug; Biliary/Fecal: 10-25% as metabolites and unchanged drug. |
| Half-life | 3-4 hours (terminal) in patients with normal renal function; prolonged to 12-24 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 90-95% bound primarily to albumin. |
| Volume of Distribution | 0.3-0.4 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 60-70% due to first-pass metabolism. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | 4-6 hours for oral; 2-4 hours for intravenous; may persist up to 12 hours in renal impairment. |
10-60 mg orally once daily in the morning, gradually tapered as tolerated. Maintenance dose 5-10 mg orally once daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No adjustment required for renal impairment; use with caution in severe renal failure. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B and C: reduce dose by 50% or use alternative. |
| Pediatric use | 0.14-2 mg/kg/day orally divided twice daily, maximum 60 mg/day. Titrate to lowest effective dose. |
| Geriatric use | Start at lowest effective dose (5-10 mg/day) and titrate slowly due to increased risk of osteoporosis and hyperglycemia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PREDAIR (PREDAIR).
| Breastfeeding | Prednisolone (active metabolite) excreted in breast milk; M/P ratio ~0.5-0.7. Considered compatible with breastfeeding at maternal doses ≤40 mg/day; high doses may necessitate discard milk for 4 hours after dose. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Increased risk of cleft palate (odds ratio 1.5-3.0). Second/third trimester: Fetal adrenal suppression, growth restriction, oligohydramnios with prolonged use. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to prednisone or any component","Systemic fungal infections","Administration of live or live-attenuated vaccines"]
| Precautions | ["Immunosuppression and increased susceptibility to infections","Adrenal insufficiency with withdrawal","Osteoporosis with long-term use","Hyperglycemia and diabetes mellitus","Gastrointestinal perforation","Psychiatric disturbances","Cushing's syndrome with prolonged use"] |
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| Maternal: Blood pressure, blood glucose, bone density (long-term). Fetal: Ultrasound for growth and amniotic fluid volume (oligohydramnios) with prolonged use. |
| Fertility Effects | No significant impairment; may suppress ovulation at high doses due to hormonal disruption; reversible upon dose reduction/discontinuation. |