PREDNISOLONE ACETATE
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.
Glucocorticoid receptor agonist; modulates gene expression to inhibit pro-inflammatory cytokines, phospholipase A2, and NF-κB; suppresses immune response and inflammation.
| Metabolism | Hepatic; primarily via CYP3A4 to inactive metabolites; also undergoes reduction and conjugation. |
| Excretion | Renal (fraction excreted unchanged: <1%); primarily hepatic metabolism to inactive glucuronide and sulfate conjugates eliminated renally and fecally. After oral administration, 12-15% of dose recovered in bile/feces as metabolites. |
| Half-life | Terminal elimination half-life: 2-4 hours (plasma); biological (tissue) half-life: 18-36 hours due to prolonged glucocorticoid receptor-mediated effects. Half-life prolonged in hepatic disease. |
| Protein binding | 70-90% bound primarily to corticosteroid-binding globulin (CBG, transcorrin) and albumin; binding saturable at high doses. |
| Volume of Distribution | 0.2-0.6 L/kg (total body water); distributes extensively into tissues; crosses placenta and blood-brain barrier. |
| Bioavailability | Oral: 70-90% (peak plasma at 1-2 h); Ophthalmic: minimal systemic absorption (~0.1% with typical dosing); Intra-articular: complete local retention with minor systemic absorption. |
| Onset of Action | Oral: 1-2 hours; IV: rapid (minutes); Intra-articular/Soft tissue injection: 24-48 hours (anti-inflammatory); Ophthalmic suspension: 2-4 hours (ocular effect). |
| Duration of Action | Oral/IV: 30-36 hours (HPA axis suppression); Intra-articular: 1-2 weeks; Ophthalmic: 4-8 hours. Duration prolonged with higher doses and repeated administration. |
| Molecular Weight | 402.48 |
5-60 mg orally once daily or divided every 12-24 hours; dose depends on condition and severity. For acute exacerbations, 200-400 mg intramuscularly once.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >30 mL/min. For GFR 10-30 mL/min, use with caution and monitor for fluid retention; no specific dose reduction recommended. For GFR <10 mL/min, avoid use or use with extreme caution due to potential for fluid overload. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Use with caution; reduce initial dose by 20-40%. Child-Pugh Class C: Avoid use or reduce dose by 50% and monitor closely. |
| Pediatric use | 0.14-2 mg/kg/day orally divided every 6-12 hours, or 0.5-7.5 mg/kg intramuscularly every 12-24 hours for acute conditions. Maximum single dose: 80 mg. |
| Geriatric use | Initiate at the lower end of the dosing range (e.g., 5-10 mg orally daily) due to increased risk of osteoporosis, glucose intolerance, and fluid retention. Monitor blood pressure, blood glucose, and electrolytes regularly. |
| 1st trimester | Use only if clearly needed; associated with palatal cleft risk (low absolute risk). |
| 2nd trimester | May cause fetal adrenal suppression; monitor growth. |
| 3rd trimester | May cause neonatal adrenal suppression; avoid prolonged high doses. |
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 | Crosses placenta; 30-40% maternal serum level in fetal circulation. |
| Breastfeeding | Low levels in breast milk; unlikely to cause adverse effects in infant at moderate doses. Monitor infant for adrenal suppression if high maternal doses. |
■ FDA Black Box Warning
None.
| Common Effects | immunosuppression |
| Serious Effects |
Systemic fungal infectionsHypersensitivity to prednisolone or componentsAdministration of live or live-attenuated vaccines with immunosuppressive doses
| Precautions | Immunosuppression and increased infection risk, Adrenal suppression with prolonged use or abrupt withdrawal, Osteoporosis with chronic use, Cataracts and glaucoma with ophthalmic use, Growth suppression in children, Exacerbation of fungal infections; contraindicated in systemic fungal infections, Live vaccine administration during therapy may cause disseminated infection |
| Food/Dietary | No significant food interactions. Avoid alcohol if taking oral corticosteroids concurrently, but for ophthalmic use, systemic absorption is minimal. |
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| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Prednisolone acetate crosses the placenta. First trimester: Increased risk of orofacial clefts (odds ratio ~3.3) with exposure before 10 weeks; risk of preterm birth and low birth weight. Second/third trimester: Fetal adrenal suppression, growth restriction; possible association with premature rupture of membranes. Chronic use: Risk of neonatal adrenal insufficiency. |
| Fetal Monitoring | Monitor maternal blood pressure, blood glucose (especially in gestational diabetes), fetal growth via ultrasound, and neonatal adrenal function if used near term. Assess for signs of infection due to immunosuppression. |
| Fertility Effects | No direct evidence of impaired fertility in humans. Animal studies show no significant effect on reproductive function. May delay conception if used for autoimmune conditions, but not directly harmful to fertility. |
| Clinical Pearls | Prednisolone acetate is a corticosteroid suspension for ophthalmic use. Shake vigorously before each use to ensure uniform suspension. Do not use while wearing contact lenses. Monitor intraocular pressure (IOP) if used for >10 days. Use with caution in patients with glaucoma, cataracts, or corneal thinning. Discontinue if corneal fungal infection suspected. |
| Patient Advice | Shake the bottle well before each use. · Remove contact lenses before instillation; wait 15 minutes before reinserting. · Do not touch the dropper tip to any surface to avoid contamination. · Use exactly as prescribed; do not stop abruptly. · Report any vision changes, eye pain, or signs of infection (redness, discharge). · Avoid driving or operating machinery if vision is blurred after use. |