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.

How it works

Glucocorticoid receptor agonist; modulates gene expression to inhibit pro-inflammatory cytokines, phospholipase A2, and NF-κB; suppresses immune response and inflammation.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

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	Prednisolone acetate enters breast milk with M/P ratio ~0.05-0.2. At maternal doses ≤40 mg/day, infant exposure <10% of maternal dose. No reported adverse effects in breastfed infants. Use caution with high doses (>40 mg/day); consider waiting 4 hours after dose to breastfeed.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Common Effects	immunosuppression
Serious Effects

Absolute Contraindications

["Hypersensitivity to prednisolone or any component","Systemic fungal infections","Ocular herpes simplex (topical ophthalmic use relative contraindication)"]

Clinical Precautions

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"]

Clinical Tips & Counseling

Drug interactions

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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.

How it works

Glucocorticoid receptor agonist; modulates gene expression to inhibit pro-inflammatory cytokines, phospholipase A2, and NF-κB; suppresses immune response and inflammation.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

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	Prednisolone acetate enters breast milk with M/P ratio ~0.05-0.2. At maternal doses ≤40 mg/day, infant exposure <10% of maternal dose. No reported adverse effects in breastfed infants. Use caution with high doses (>40 mg/day); consider waiting 4 hours after dose to breastfeed.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Common Effects	immunosuppression
Serious Effects

Absolute Contraindications

["Hypersensitivity to prednisolone or any component","Systemic fungal infections","Ocular herpes simplex (topical ophthalmic use relative contraindication)"]