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. |
| Molecular Weight | 358.43 |
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 | Use only if clearly needed; risk of cleft palate (1st trimester exposure), adrenal suppression. Consider maternal benefit vs fetal risk. |
| 2nd trimester | Use caution; may cause adrenal suppression, growth restriction. Monitor fetal growth. |
| 3rd trimester | Use caution; may cause neonatal adrenal suppression, growth restriction. 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.
| FDA category | Positive |
| Placental transfer | Prednisone is metabolized to prednisolone (active form); both cross placenta. Prednisone itself has limited transfer due to 11β-hydroxysteroid dehydrogenase type 2 conversion, but prednisolone crosses effectively. |
■ FDA Black Box Warning
None. Prednisone does not have a black box warning.
| Common Effects | immunosuppression |
| Serious Effects |
Systemic fungal infectionsHypersensitivity to prednisone or any component
| 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) |
| Food/Dietary |
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| Breastfeeding |
| Prednisone is excreted into breast milk in low amounts. Doses up to 50 mg daily not expected to cause adverse effects in term infants. Monitor for growth and development in prolonged use. Consider waiting 4 hours after dose to breastfeed. |
| Lactation Rating | L2 (Safer) |
| 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. |
| 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. |
| Avoid grapefruit and grapefruit juice as they may increase prednisone levels. Limit foods high in sodium (e.g., processed foods) and consider potassium-rich foods (e.g., bananas) if recommended. May require calcium and vitamin D supplementation to prevent bone loss. |
| Clinical Pearls | Prednisone Intensol is a concentrated oral solution (5 mg/mL) used for glucocorticoid therapy. Administer with food to reduce GI irritation. Do not use in patients with systemic fungal infections or known hypersensitivity. Monitor for adrenal suppression during taper. Avoid live vaccines. May cause hyperglycemia; monitor blood glucose in diabetics. |
| Patient Advice | Take exactly as prescribed; do not stop suddenly without doctor's guidance. · Take with food or milk to minimize stomach upset. · Measure dose using the provided dropper; do not use household spoons. · Report any unusual weight gain, swelling, vision changes, or signs of infection (fever, sore throat) immediately. · Avoid close contact with people who have measles or chickenpox; inform doctor if exposed. · Carry a medical alert card or ID indicating you are on steroids. · Do not receive live vaccines while on this medication. · May cause mood swings or insomnia; report severe changes. · Avoid alcohol and NSAIDs (e.g., ibuprofen) without doctor approval to reduce GI risks. |