PREDNISOLONE
Clinical safety rating: avoid
Positive evidence of fetus risks but benefits may outweigh risks in some cases
Prednisolone is a glucocorticoid that binds to the glucocorticoid receptor, leading to modulation of gene expression and suppression of inflammatory cytokines, inhibition of phospholipase A2, and reduction of prostaglandin and leukotriene synthesis.
| Metabolism | Hepatic via CYP3A4; reduced form prednisolone is reversible to prednisone; further metabolized to inactive glucuronide and sulfate conjugates. |
| Excretion | Renal (primarily as glucuronide and sulfate conjugates; <20% as unchanged prednisolone); biliary/fecal (minor, <5%). |
| Half-life | Terminal half-life: 2.1-3.5 hours in adults; prolonged in hepatic impairment (up to 12 hours) or with concurrent estrogen use. |
| Protein binding | 60-80% bound to corticosteroid-binding globulin (CBG) and albumin; concentration-dependent (saturable). |
| Volume of Distribution | 0.5-1.0 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 82% ± 13% (immediate-release); intra-articular: negligible systemic absorption. |
| Onset of Action | Oral: 1-2 hours; IV: rapid (within 1 hour); Intra-articular: 24-48 hours. |
| Duration of Action | Oral/IV: 12-36 hours (dose-dependent); Intra-articular: 7-35 days (depends on preparation). |
| Molecular Weight | 360.44 |
Initial adult dose: 5-60 mg orally, intramuscularly, or intravenously daily, divided into 2-4 doses; maintenance: 2.5-15 mg daily.
| Dosage form | TABLET |
| Renal impairment | No specific GFR-based dose adjustment required; use with caution in renal impairment due to fluid retention. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: reduce dose by 75% or avoid use. |
| Pediatric use | 0.14-2 mg/kg/day orally or intravenously divided into 3-4 doses; maximum 60 mg/day. |
| Geriatric use | Initiate at lowest effective dose; monitor for osteoporosis, hyperglycemia, and fluid retention; consider calcium and vitamin D supplementation. |
| 1st trimester | Associated with cleft palate (1-2% risk) and other malformations; use only if benefits outweigh risks. |
| 2nd trimester | May cause fetal growth restriction and adrenal suppression; use with caution. |
| 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 | Prednisolone crosses the placenta but is extensively metabolized; placental 11β-HSD2 converts prednisolone to inactive prednisone, reducing fetal exposure. Fetal levels are about 10-15% of maternal. |
| Breastfeeding | Prednisolone enters breast milk in low amounts (<2% maternal dose); generally considered compatible with breastfeeding, but high doses may require monitoring of infant for adrenal suppression. |
■ FDA Black Box Warning
No FDA boxed warning exists for prednisolone.
| Common Effects | immunosuppression |
| Serious Effects |
Systemic fungal infections (except when used for fungal meningitis with concomitant antifungal therapy)Known hypersensitivity to prednisolone or any component
| Precautions | Increased risk of infections, adrenal suppression, Cushing's syndrome, osteoporosis, gastrointestinal perforation, avascular necrosis, myopathy, psychiatric disturbances, Kaposi sarcoma, and growth suppression in children. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase prednisolone levels. Limit sodium intake to reduce fluid retention. Increase potassium-rich foods (bananas, oranges) and calcium/vitamin D to counteract bone loss. Alcohol may increase risk of gastrointestinal irritation. |
Loading safety data…
| Lactation Rating | L2 |
| Teratogenic Risk | First trimester: Increased risk of cleft palate (OR 1.3–3.3). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, premature birth. No consistent association with major malformations. |
| Fetal Monitoring | Maternal: Blood pressure, blood glucose, signs of infection. Fetal: Serial growth ultrasounds, nonstress test if prolonged use. |
| Fertility Effects | No direct impairment; may improve fertility in autoimmune or inflammatory conditions by controlling disease. |
| Clinical Pearls | Do not abruptly discontinue after prolonged therapy (>3 weeks) due to risk of adrenal suppression; taper gradually. Monitor for hyperglycemia, especially in diabetics. Use with caution in patients with osteoporosis, peptic ulcer disease, or active infections. Consider Pneumocystis jirovecii prophylaxis when combined with other immunosuppressants. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not stop taking this medication suddenly; follow your doctor's tapering schedule. · Report any signs of infection (fever, sore throat) or unusual weight gain/swelling. · Avoid live vaccines while on this medication. · Carry a medical alert card indicating steroid use. |