PREDNISONE INTENSOL
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.
Prednisone is a prodrug that is converted to prednisolone, which binds to the glucocorticoid receptor, modulating gene expression to produce anti-inflammatory and immunosuppressive effects by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis, and suppressing cytokine production.
| Metabolism | Prednisone is primarily converted to its active metabolite prednisolone via hepatic 11β-hydroxysteroid dehydrogenase. Prednisolone is further metabolized by hepatic CYP3A4 and other enzymes to inactive metabolites, which are excreted renally. |
| Excretion | Renal: <30% unchanged; major metabolites (prednisolone, 20-dihydroprednisolone) conjugated and excreted in urine. Fecal: <10%. |
| Half-life | 2-4 hours (terminal) for prednisone; prednisolone half-life 2-4 hours. Clinical context: shorter than anti-inflammatory effect due to delayed receptor-mediated action. |
| Protein binding | Prednisolone: 70-90% bound to corticosteroid-binding globulin (CBG) and albumin. Prednisone: ~70% bound. |
| Volume of Distribution | 0.5-1.0 L/kg (prednisolone). Reflects extensive tissue distribution including intracellular receptors. |
| Bioavailability | Oral: 70-90% (rapidly converted to prednisolone). IM: ~80-100%. |
| Onset of Action | Oral: 1-2 hours (peak anti-inflammatory effect). IM: 0.5-1 hour. IV: immediate (when converted to prednisolone). |
| Duration of Action | 18-36 hours (receptor occupancy and genomic effects). Clinical note: single dose suppresses ACTH for 24-48 hours. |
5-60 mg orally once daily or divided twice daily, titrated to response.
| Dosage form | SOLUTION |
| Renal impairment | No specific adjustment required; monitor for fluid retention and hypertension. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: use with caution, monitor for increased toxicity; dose reduction may be needed but no specific guidelines. |
| Pediatric use | 0.1-2 mg/kg/day orally in divided doses (every 6-12 hours) based on severity. |
| Geriatric use | Start at lower end of adult dose (5-10 mg/day); monitor for osteoporosis, hyperglycemia, and 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 | Prednisone enters breast milk; M/P ratio ~0.25. Doses ≤20 mg/day are considered low risk. Infant serum levels are negligible (<0.1% of maternal weight-adjusted dose). Monitor infant for adrenal suppression with high maternal doses. |
| Teratogenic Risk | First trimester: Increased risk of cleft lip/palate (odds ratio 1.3-3.3). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, oligohydramnios, and preterm birth. Chronic use may cause neonatal adrenal insufficiency. |
■ FDA Black Box Warning
None. Prednisone does not have a black box warning.
| Common Effects | immunosuppression |
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to prednisone or any component of the formulation","Administration of live or live-attenuated vaccines (relative)","Idiopathic thrombocytopenic purpura (relative, for intramuscular use)","Active untreated infections (relative)"]
| Precautions | ["Immunosuppression and increased risk of infections","Hypothalamic-pituitary-adrenal (HPA) axis suppression with prolonged use","Corticosteroid withdrawal syndrome upon abrupt discontinuation","Osteoporosis with chronic use","Gastrointestinal perforation (especially in patients with diverticulitis or peptic ulcer)","Steroid-induced myopathy","Increased intraocular pressure and glaucoma","Corticosteroid-induced psychosis and mood disturbances","Fluid and electrolyte disturbances (sodium retention, potassium loss)","Growth suppression in children","Kaposi sarcoma (rare)"] |
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| Fetal Monitoring | Maternal: Blood glucose, blood pressure, weight, electrolyte levels, signs of infection. Fetal: Serial ultrasound for growth restriction and amniotic fluid volume (if prolonged use). Neonatal: Assessment for adrenal insufficiency after delivery if maternal use continued to term. |
| Fertility Effects | Prednisone may inhibit ovulation, but effects are reversible upon discontinuation. No evidence of permanent fertility impairment. |