METICORTEN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for METICORTEN (METICORTEN).

How it works

Prednisone is a prodrug that is converted to prednisolone, which binds to the glucocorticoid receptor, modulating gene expression and suppressing inflammation, immune response, and adrenal function.

What the body does with it

Metabolism	Prednisone is converted to active prednisolone via 11-beta-hydroxysteroid dehydrogenase; both are metabolized by CYP3A4 and other enzymes.
Excretion	Primarily renal: approximately 80% as inactive metabolites (conjugated and oxidized forms) and <5% as unchanged prednisolone. Biliary/fecal excretion accounts for about 10-15% of the dose.
Half-life	Following oral or IV administration, the terminal elimination half-life of total prednisolone (active form) is 2.1–3.5 hours in adults with normal hepatic function. In hepatic impairment, half-life may be prolonged (up to 6–8 hours), necessitating dose adjustment.
Protein binding	Approximately 90–95% bound to serum proteins, primarily corticosteroid-binding globulin (CBG, transcorrin) and albumin. Binding is saturable; at high doses, the free fraction increases, enhancing tissue penetration.
Volume of Distribution	The apparent volume of distribution (Vd) is 0.6–1.0 L/kg, reflecting extensive distribution into tissues and body water compartments. In obesity, Vd may increase due to higher adipose tissue affinity.
Bioavailability	Oral bioavailability of prednisone (prodrug) is approximately 80%, with extensive first-pass hepatic conversion to prednisolone (active form). Sublingual and rectal routes have lower and more variable bioavailability (50–70%).
Onset of Action	Oral (tablet): Anti-inflammatory and immunosuppressive effects begin within 2–4 hours, with peak clinical response seen within 24–48 hours. IV (if applicable): Onset is more rapid, within 1–2 hours.
Duration of Action	The clinical duration of action for a single dose is 18–36 hours, sustained by the prolonged presence of active metabolites. Prednisolone's biological half-life (duration of ACTH suppression) is 18–36 hours, supporting once-daily dosing in chronic conditions.

Classification & Brands

Dosing & administration

5-60 mg orally once daily, depending on condition; for acute exacerbations, up to 250 mg IV every 4-6 hours.

Dosage form	TABLET
Renal impairment	No adjustment necessary for mild to moderate renal impairment; for severe renal impairment (GFR < 30 mL/min), consider prolonging dosing interval to every 12-24 hours.
Liver impairment	For Child-Pugh class A: no adjustment; class B: reduce dose by 50%; class C: reduce dose by 75% or avoid use.
Pediatric use	0.14-2 mg/kg/day orally in divided doses every 6-12 hours, not to exceed 60 mg/day.
Geriatric use	Initiate at 5-10 mg/day orally, titrate slowly due to increased risk of osteoporosis, glucose intolerance, and immune suppression.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for METICORTEN (METICORTEN).

Breastfeeding	Prednisone enters breast milk in low amounts (M/P ratio ~0.1-0.2). Milk levels peak 1-2 hours after dose. Generally considered compatible; monitor infant for growth and adrenal suppression. No high-dose studies.
Teratogenic Risk	First trimester: Increased risk of oral clefts (odds ratio ~1.5-3.0). Second/third trimester: Fetal adrenal suppression, growth restriction, preterm birth. Chronic use: Risk of neonatal adrenal insufficiency.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

Systemic fungal infections; concurrent live or live-attenuated vaccines (except as replacement therapy in adrenal insufficiency); known hypersensitivity to prednisone or any component.

Clinical Precautions

Precautions

Immunosuppression and increased infection risk; dose-dependent adrenal suppression; osteoporosis with prolonged use; gastrointestinal perforation risk; psychiatric disturbances; masking of infections; Kaposi sarcoma have been reported.

Clinical Tips & Counseling

Drug interactions

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METICORTEN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for METICORTEN (METICORTEN).

How it works

Prednisone is a prodrug that is converted to prednisolone, which binds to the glucocorticoid receptor, modulating gene expression and suppressing inflammation, immune response, and adrenal function.

What the body does with it

Metabolism	Prednisone is converted to active prednisolone via 11-beta-hydroxysteroid dehydrogenase; both are metabolized by CYP3A4 and other enzymes.
Excretion	Primarily renal: approximately 80% as inactive metabolites (conjugated and oxidized forms) and <5% as unchanged prednisolone. Biliary/fecal excretion accounts for about 10-15% of the dose.
Half-life	Following oral or IV administration, the terminal elimination half-life of total prednisolone (active form) is 2.1–3.5 hours in adults with normal hepatic function. In hepatic impairment, half-life may be prolonged (up to 6–8 hours), necessitating dose adjustment.
Protein binding	Approximately 90–95% bound to serum proteins, primarily corticosteroid-binding globulin (CBG, transcorrin) and albumin. Binding is saturable; at high doses, the free fraction increases, enhancing tissue penetration.
Volume of Distribution	The apparent volume of distribution (Vd) is 0.6–1.0 L/kg, reflecting extensive distribution into tissues and body water compartments. In obesity, Vd may increase due to higher adipose tissue affinity.
Bioavailability	Oral bioavailability of prednisone (prodrug) is approximately 80%, with extensive first-pass hepatic conversion to prednisolone (active form). Sublingual and rectal routes have lower and more variable bioavailability (50–70%).
Onset of Action	Oral (tablet): Anti-inflammatory and immunosuppressive effects begin within 2–4 hours, with peak clinical response seen within 24–48 hours. IV (if applicable): Onset is more rapid, within 1–2 hours.
Duration of Action	The clinical duration of action for a single dose is 18–36 hours, sustained by the prolonged presence of active metabolites. Prednisolone's biological half-life (duration of ACTH suppression) is 18–36 hours, supporting once-daily dosing in chronic conditions.

Classification & Brands

Dosing & administration

5-60 mg orally once daily, depending on condition; for acute exacerbations, up to 250 mg IV every 4-6 hours.

Dosage form	TABLET
Renal impairment	No adjustment necessary for mild to moderate renal impairment; for severe renal impairment (GFR < 30 mL/min), consider prolonging dosing interval to every 12-24 hours.
Liver impairment	For Child-Pugh class A: no adjustment; class B: reduce dose by 50%; class C: reduce dose by 75% or avoid use.
Pediatric use	0.14-2 mg/kg/day orally in divided doses every 6-12 hours, not to exceed 60 mg/day.
Geriatric use	Initiate at 5-10 mg/day orally, titrate slowly due to increased risk of osteoporosis, glucose intolerance, and immune suppression.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for METICORTEN (METICORTEN).

Breastfeeding	Prednisone enters breast milk in low amounts (M/P ratio ~0.1-0.2). Milk levels peak 1-2 hours after dose. Generally considered compatible; monitor infant for growth and adrenal suppression. No high-dose studies.
Teratogenic Risk	First trimester: Increased risk of oral clefts (odds ratio ~1.5-3.0). Second/third trimester: Fetal adrenal suppression, growth restriction, preterm birth. Chronic use: Risk of neonatal adrenal insufficiency.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

Systemic fungal infections; concurrent live or live-attenuated vaccines (except as replacement therapy in adrenal insufficiency); known hypersensitivity to prednisone or any component.