DELTASONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).
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.
| 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. |
| Molecular Weight | 358.47 |
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. |
| 1st trimester | Prednisone is associated with increased risk of cleft palate (approximately 3-4-fold) when used in first trimester; benefit-risk assessment required. Use lowest effective dose. |
| 2nd trimester | Risk of fetal adrenal suppression, growth restriction, and premature rupture of membranes with prolonged use. Monitor fetal growth. |
| 3rd trimester | Risk of neonatal adrenal insufficiency if used near term. Taper if possible; monitor neonate for signs of adrenal suppression. |
Clinical note
Comprehensive clinical and safety monograph for DELTASONE (DELTASONE).
| Placental transfer | Placental transfer occurs; prednisone is partially metabolized by placental 11β-HSD2 to inactive prednisolone, but significant fetal exposure still occurs. About 10-20% of maternal dose reaches fetus. |
| Breastfeeding | Prednisone is excreted into breast milk in small amounts. The infant dose is estimated at less than 10% of maternal dose; however, high maternal doses (>40 mg daily) may increase risk. Monitor infant for growth, adrenal suppression, and immunosuppression. Use lowest effective dose and consider timing feeds to minimize exposure. |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionsHypersensitivity to prednisone or any component of the formulationAdministration of live or live-attenuated vaccines in patients receiving immunosuppressive dosesIdiopathic thrombocytopenic purpura (if using other therapies available)
| 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. |
| Food/Dietary | Avoid grapefruit and grapefruit juice due to CYP3A4 inhibition potential. Limit sodium intake to reduce fluid retention. May increase appetite; monitor caloric intake to avoid excessive weight gain. Take with food or milk to minimize gastrointestinal irritation. |
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| Lactation Rating | L3 - Moderately Safe |
| 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 | Maternal: Blood pressure, glucose, and signs of infection. Fetal: Serial growth ultrasound (every 4-6 weeks) for intrauterine growth restriction; fetal adrenal axis assessment if long-term use. |
| Fertility Effects | No direct impairment of fertility. May affect menstrual cycle through suppression of hypothalamic-pituitary-adrenal axis; reversible upon dose reduction or discontinuation. |
| Clinical Pearls | DELTASONE (prednisone) is a prodrug converted to prednisolone; use with caution in hepatic impairment. Monitor for adrenal suppression with abrupt withdrawal. Taper dose after prolonged use. May cause hyperglycemia; monitor blood glucose in diabetic patients. Avoid live vaccines during therapy. |
| Patient Advice | Take exactly as prescribed; do not stop abruptly without consulting your doctor. · Take with food to reduce stomach upset. · Report any signs of infection (fever, sore throat) or unusual bruising/bleeding. · Avoid grapefruit juice as it may increase drug levels. · Do not receive live vaccines during treatment. |