PREDNISONE
Clinical safety rating: avoid
Positive evidence of fetus risks but benefits may outweigh risks in some cases
Agonist at glucocorticoid receptors, leading to altered gene transcription that results in anti-inflammatory and immunosuppressive effects, including suppression of cytokines, prostaglandins, and leukotrienes.
| Metabolism | Hepatic, primarily via CYP3A4-mediated 6β-hydroxylation; also reduced by 20-ketosteroid reductases. Prednisone is a prodrug converted to active metabolite prednisolone. |
| Excretion | Renal: <10% as unchanged drug; hepatic metabolism to inactive glucuronide and sulfate conjugates; fecal: ~20-30% via biliary elimination. |
| Half-life | Terminal half-life: 2-3 hours (plasma); clinical effects persist for 12-36 hours due to intracellular actions and active metabolite prednisolone (half-life 3-4 hours). |
| Protein binding | Prednisone: 70-90% bound to albumin and corticosteroid-binding globulin (CBG); prednisolone: 60-70% bound. |
| Volume of Distribution | Vd: 0.5-1.0 L/kg; distributes widely, crosses placenta and enters breast milk; apparent Vd larger with hyperthyroidism. |
| Bioavailability | Oral: 70-80% (active prednisolone after hepatic conversion); IM: ~100%. |
| Onset of Action | Oral: 1-4 hours; IV: rapid (within 1 hour); IM: 1-2 hours. |
| Duration of Action | Oral/IV: 12-36 hours (duration of HPA suppression and anti-inflammatory effects); clinical duration longer than plasma half-life. |
| Molecular Weight | 358.43 |
5-60 mg orally once daily or divided twice daily; for acute indications, initial dose 5-60 mg/day; for chronic conditions, lowest effective dose; route: oral, intravenous, intramuscular.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for renal impairment; consider alternative corticosteroid in severe renal disease if fluid retention is a concern. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: use with caution; dose reduction may be considered due to decreased clearance; monitor for adverse effects. |
| Pediatric use | 0.1-2 mg/kg/day orally divided 1-4 times daily; maximum 60 mg/day; use lowest effective dose; for acute asthma, 1-2 mg/kg/day for 3-5 days. |
| Geriatric use | Start at lower end of dosing range (5-7.5 mg/day) due to increased risk of osteoporosis, hyperglycemia, and infections; monitor glucose and bone density; taper slowly to avoid adrenal suppression. |
| 1st trimester | Use only if clearly needed; risk of cleft palate if used in first trimester. |
| 2nd trimester | May cause adrenal suppression in fetus; monitor for intrauterine growth restriction. |
| 3rd trimester | Risk of neonatal adrenal suppression; avoid prolonged use near term. |
Clinical note
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
| Placental transfer | Prednisone crosses the placenta (inactive prednisone is converted to active prednisolone); transfer is moderate. |
| Breastfeeding | Prednisone is excreted in breast milk in low doses; avoid high doses (>40 mg/day) or monitor infant for adrenal suppression. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Common Effects | immunosuppression |
| Serious Effects |
Systemic fungal infectionHypersensitivity to prednisone or any component
| Precautions | Adrenal suppression and HPA axis suppression with prolonged therapy, Increased risk of infections, Exacerbation of systemic fungal infections, Masking of signs of infection, Osteoporosis with long-term use, Gastrointestinal perforation (especially in patients with certain GI disorders), Kaposi sarcoma reported, Cardiovascular effects (hypertension, fluid retention), Behavioral disturbances (euphoria, depression, psychosis), Posterior subcapsular cataracts and glaucoma, Thromboembolism risk, Vaccine response may be diminished; live vaccines contraindicated |
| Food/Dietary | Avoid grapefruit juice as it may increase prednisone levels. Limit high-sodium foods to prevent fluid retention. Increase calcium and vitamin D intake to counteract bone loss. Avoid alcohol due to added GI irritation risk. |
Loading safety data…
| L2 (Safer) |
| Teratogenic Risk | First trimester: Increased risk of cleft lip/palate (odds ratio 1.3-3.4). Second/third trimester: Fetal growth restriction, adrenal suppression, preterm delivery. Chronic use: Dose-dependent fetal hypothalamic-pituitary-adrenal axis suppression. |
| Fetal Monitoring | Maternal: Blood pressure, blood glucose, weight, signs of infection. Fetal: Ultrasound for growth restriction every 4-6 weeks if chronic use. Neonatal: Assess for adrenal suppression (lethargy, hypoglycemia) if maternal dose >10 mg/day for >2 weeks before delivery. |
| Fertility Effects | No direct effect on fertility. May improve fertility in women with autoimmune disorders by controlling underlying disease. Higher doses may cause menstrual irregularities. |
| Clinical Pearls | Prednisone is a prodrug converted to prednisolone; use prednisolone in severe hepatic impairment. Taper dose after prolonged use (≥3 weeks) to avoid adrenal crisis. Morning dosing mimics cortisol rhythm and reduces insomnia. Monitor for hyperglycemia, osteoporosis, avascular necrosis, and immunosuppression. Do not give live vaccines during therapy. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not stop abruptly; follow a tapering schedule from your doctor. · Notify your doctor if you experience fever, unusual bleeding, or weight gain. · Avoid live vaccines (e.g., MMR, nasal flu) while on prednisone. · Carry a steroid alert card or wear a medical ID bracelet. |