DELTASONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).

How it works

Prednisone is a prodrug that is converted to prednisolone, which binds to the glucocorticoid receptor, leading to altered gene expression and suppression of inflammatory mediators, immune cells, and cytokine production.

What the body does with it

Metabolism	Prednisone is metabolized by the liver to its active metabolite prednisolone. Prednisolone is further metabolized via CYP3A4 and other pathways.
Excretion	Prednisone is a prodrug converted to prednisolone. Prednisolone is metabolized primarily in the liver. Renal excretion of unchanged drug is negligible (<1%). Metabolites are excreted renally (approximately 80% as glucuronides and sulfates) and to a small extent in feces (<5%). Biliary excretion is minimal.
Half-life	The terminal elimination half-life of prednisolone (active form) is 2.1–3.5 hours. In clinical context, this short half-life supports once-daily to twice-daily dosing for anti-inflammatory effects, but adrenal suppression can persist longer due to receptor binding.
Protein binding	Prednisolone is 90–95% bound to plasma proteins, primarily corticosteroid-binding globulin (CBG) and albumin. Binding is saturable; at higher doses, free fraction increases.
Volume of Distribution	Volume of distribution (Vd) for prednisolone is 0.5–1.0 L/kg. This moderate Vd reflects distribution into total body water. Vd increases with obesity and decreases with hypoalbuminemia.
Bioavailability	Oral bioavailability of prednisone is approximately 70–80% due to first-pass metabolism to prednisolone. Rectal bioavailability (enema) is about 50%.
Onset of Action	Oral: Onset of clinical effect is 1–2 hours. Peak plasma levels of prednisolone occur within 1–2 hours. IV: Onset is immediate after administration, with clinical effects seen within 1 hour.
Duration of Action	Duration of anti-inflammatory effect is 12–36 hours after a single oral dose, though hypothalamic-pituitary-adrenal (HPA) axis suppression can last up to 12 days after chronic therapy. Clinical duration is dose-dependent.

Classification & Brands

Dosing & administration

5-60 mg orally once daily or divided twice daily; dose individualized based on condition and response.

Dosage form	TABLET
Renal impairment	No dosage adjustment necessary for acute use; for chronic use, monitor for fluid retention and adjust dose accordingly.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B or C: Use with caution; consider dose reduction of 50% due to decreased clearance.
Pediatric use	0.14-2 mg/kg/day orally divided every 6-12 hours; maximum 60 mg/day; dose adjusted based on response and severity.
Geriatric use	Start at lowest effective dose; monitor for hyperglycemia, osteoporosis, and hypertension; consider shorter-acting glucocorticoids if possible.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).

Breastfeeding	Prednisone enters breast milk with an M/P ratio of approximately 0.8. Doses ≤20 mg/day are generally considered compatible. For higher doses, monitor infant for adrenal suppression. Delay breastfeeding 4 hours after dose.
Teratogenic Risk	First trimester: Increased risk of cleft palate (odds ratio 3.35). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, and preterm delivery. 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; hypersensitivity to prednisone or any component; concurrent live or attenuated virus vaccines; idiopathic thrombocytopenic purpura (use IM formulation contraindicated).

Clinical Precautions

Precautions

Adrenal suppression with prolonged use; increased risk of infections; masking of infection signs; osteoporosis; gastrointestinal perforation; psychiatric disturbances; Kaposi sarcoma; vaccination risks; live vaccines contraindicated; fetal risk (Category C); hypertension; diabetes; growth suppression in children; Cushing's syndrome with chronic use.

Clinical Tips & Counseling

Drug interactions

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DELTASONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).

How it works

What the body does with it

Metabolism	Prednisone is metabolized by the liver to its active metabolite prednisolone. Prednisolone is further metabolized via CYP3A4 and other pathways.
Excretion	Prednisone is a prodrug converted to prednisolone. Prednisolone is metabolized primarily in the liver. Renal excretion of unchanged drug is negligible (<1%). Metabolites are excreted renally (approximately 80% as glucuronides and sulfates) and to a small extent in feces (<5%). Biliary excretion is minimal.
Half-life	The terminal elimination half-life of prednisolone (active form) is 2.1–3.5 hours. In clinical context, this short half-life supports once-daily to twice-daily dosing for anti-inflammatory effects, but adrenal suppression can persist longer due to receptor binding.
Protein binding	Prednisolone is 90–95% bound to plasma proteins, primarily corticosteroid-binding globulin (CBG) and albumin. Binding is saturable; at higher doses, free fraction increases.
Volume of Distribution	Volume of distribution (Vd) for prednisolone is 0.5–1.0 L/kg. This moderate Vd reflects distribution into total body water. Vd increases with obesity and decreases with hypoalbuminemia.
Bioavailability	Oral bioavailability of prednisone is approximately 70–80% due to first-pass metabolism to prednisolone. Rectal bioavailability (enema) is about 50%.
Onset of Action	Oral: Onset of clinical effect is 1–2 hours. Peak plasma levels of prednisolone occur within 1–2 hours. IV: Onset is immediate after administration, with clinical effects seen within 1 hour.
Duration of Action	Duration of anti-inflammatory effect is 12–36 hours after a single oral dose, though hypothalamic-pituitary-adrenal (HPA) axis suppression can last up to 12 days after chronic therapy. Clinical duration is dose-dependent.

Classification & Brands

Dosing & administration

5-60 mg orally once daily or divided twice daily; dose individualized based on condition and response.

Dosage form	TABLET
Renal impairment	No dosage adjustment necessary for acute use; for chronic use, monitor for fluid retention and adjust dose accordingly.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B or C: Use with caution; consider dose reduction of 50% due to decreased clearance.
Pediatric use	0.14-2 mg/kg/day orally divided every 6-12 hours; maximum 60 mg/day; dose adjusted based on response and severity.
Geriatric use	Start at lowest effective dose; monitor for hyperglycemia, osteoporosis, and hypertension; consider shorter-acting glucocorticoids if possible.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).

Breastfeeding	Prednisone enters breast milk with an M/P ratio of approximately 0.8. Doses ≤20 mg/day are generally considered compatible. For higher doses, monitor infant for adrenal suppression. Delay breastfeeding 4 hours after dose.
Teratogenic Risk	First trimester: Increased risk of cleft palate (odds ratio 3.35). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, and preterm delivery. 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; hypersensitivity to prednisone or any component; concurrent live or attenuated virus vaccines; idiopathic thrombocytopenic purpura (use IM formulation contraindicated).