PREDNISOLONE SODIUM PHOSPHATE
Clinical safety rating: avoid
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
Agonist of glucocorticoid receptors, leading to anti-inflammatory and immunosuppressive effects via inhibition of phospholipase A2, reduction of pro-inflammatory cytokines, and suppression of immune cell activity.
| Metabolism | Hepatic, primarily via CYP3A4, including reduction to inactive metabolites (e.g., prednisolone metabolized to prednisone interconversion). |
| Excretion | Renal excretion of inactive metabolites (primarily prednisolone) accounts for >80% of elimination; less than 10% excreted unchanged. Biliary/fecal excretion is negligible (<5%). |
| Half-life | Terminal elimination half-life is 2.1–3.5 hours in adults (mean 2.6 h). Clinical context: Short half-life supports twice-daily dosing for most conditions; prolonged in hepatic impairment (up to 8 h). |
| Protein binding | 70–90% bound primarily to corticosteroid-binding globulin (CBG; transcoritin) and albumin. Binding is concentration-dependent and saturable at high doses. |
| Volume of Distribution | 0.4–1.0 L/kg. Clinical meaning: Moderate distribution suggests extensive extravascular tissue uptake; increased in inflammatory states and decreased in obesity. |
| Bioavailability | Oral: 70–90% (immediate-release tablets). Ophthalmic: <0.1% systemic absorption due to extensive first-pass metabolism. Rectal: 20–30%. |
| Onset of Action | Oral: 1–2 hours. Intravenous: rapid (within minutes). Ophthalmic: 30–60 minutes. Rectal: 30–60 minutes. |
| Duration of Action | Oral/IV: 18–36 hours (single dose). Clinical notes: Duration exceeds half-life due to slow receptor dissociation. Longer duration with repeated dosing due to tissue accumulation. |
Initial dose: 5-60 mg orally or intravenously once daily or divided every 12-24 hours; range 5-60 mg/day. For acute conditions, 40-60 mg once daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No specific dose adjustment recommended; monitor fluid/electrolytes in severe impairment. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B/C: reduce dose by 50% or use alternative due to decreased clearance. |
| Pediatric use | 0.5-2 mg/kg/day orally or intravenously divided every 6-12 hours; maximum 60-80 mg/day. |
| Geriatric use | Start at lower end of dosing range (e.g., 5-15 mg/day); monitor for hyperglycemia, osteoporosis, immunosuppression. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
| FDA category | Positive |
| Breastfeeding | Limited transfer into breast milk; M/P ratio not established. Excreted in low amounts (estimated infant dose <0.1% of maternal weight-adjusted dose). AAP compatible with breastfeeding; avoid high doses (e.g., >40 mg/day) or use after a dose-to-nursing interval of 4 hours. |
| Teratogenic Risk |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | immunosuppression |
| Serious Effects |
["Systemic fungal infections","Known hypersensitivity to prednisolone or any component","Live or live-attenuated vaccine administration in patients on immunosuppressive doses"]
| Precautions | ["Increased risk of infections due to immunosuppression","Adrenal suppression with prolonged use","Corticosteroid-induced osteoporosis","Gastrointestinal perforation risk in patients with certain conditions (e.g., diverticulitis, peptic ulcer)","Exacerbation of diabetes mellitus","Psychiatric disturbances (e.g., euphoria, depression)","Kaposi's sarcoma reported with corticosteroid use"] |
Loading safety data…
| First trimester: Increased risk of cleft lip/palate (odds ratio ~3.4) with systemic exposure. Second/third trimester: Risk of intrauterine growth restriction, preterm birth, and adrenal suppression in neonate. Potential for maternal glucose intolerance and preeclampsia. |
| Fetal Monitoring | Monitor maternal blood glucose (gestational diabetes), blood pressure (preeclampsia), and fetal growth via ultrasound every 4-6 weeks in second/third trimester. Assess neonatal adrenal function if chronic maternal use. |
| Fertility Effects | May cause inhibition of ovulation or menstrual irregularities due to hypothalamic-pituitary-adrenal axis suppression. Reversible upon dose reduction or discontinuation. No evidence of permanent impairment. |