PRELONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRELONE (PRELONE).
Prednisolone is a corticosteroid that binds to the glucocorticoid receptor, leading to inhibition of phospholipase A2, decreased production of prostaglandins and leukotrienes, and suppression of cytokine release.
| Metabolism | Primarily hepatic via CYP3A4, with minor involvement of other CYP enzymes. |
| Excretion | Prednisolone is primarily metabolized in the liver; renal excretion accounts for <1% unchanged. Metabolites are excreted renally (~60-70%) and in bile/feces (~20-30%). |
| Half-life | The terminal elimination half-life is 2-4 hours in adults; prolonged in hepatic impairment (up to 8-12 hours). |
| Protein binding | 70-90% bound to corticosteroid-binding globulin and albumin. |
| Volume of Distribution | Vd: 0.4-0.6 L/kg; indicates distribution into total body water. |
| Bioavailability | Oral bioavailability: 70-90%. |
| Onset of Action | Oral: 1-2 hours (peak plasma concentration); IV: rapid (minutes). |
| Duration of Action | Duration of effect is 18-36 hours based on hypothalamic-pituitary-adrenal axis suppression. |
| Molecular Weight | 360.44 |
| Action Class | Glucocorticoids |
| Brand Substitutes | Predace 4 Tablet, Coelone 4mg Tablet, Pilsone 4mg Tablet, Premisol 4mg Tablet, Cortilog 4mg Tablet, Prelid 16mg Tablet, Predace 16 Tablet, Mepresso T 16mg Tablet, Medrol 16mg Tablet, Rednisol 16mg Tablet |
Initial adult dose: 40-60 mg orally once daily; maintenance: 5-60 mg orally once daily; dose individualized based on disease severity and response.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment; however, monitor fluid and electrolyte balance due to mineralocorticoid effects. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: consider 50% dose reduction. Child-Pugh Class C: avoid use or reduce dose by 75% due to altered metabolism. |
| Pediatric use | 0.1-2 mg/kg/day orally in divided doses every 6-12 hours; maximum 60 mg/day; dose tapered to lowest effective dose. |
| Geriatric use | Start at lower end of dosing range (e.g., 5-20 mg/day) and titrate slowly; monitor for hyperglycemia, osteoporosis, and fluid retention. |
| 1st trimester | Prednisolone is associated with a slightly increased risk of cleft palate (about 1-2 per 1000 births) when used in the first trimester. Caution is advised, but the benefit may outweigh risk for maternal conditions like asthma or autoimmune disease. |
| 2nd trimester | Use may increase risk of preterm delivery and intrauterine growth restriction. Monitor fetal growth and amniotic fluid. Generally considered acceptable if maternal benefit outweighs fetal risk. |
| 3rd trimester | Higher doses near term may cause neonatal adrenal suppression and immunosuppression. Use lowest effective dose. Monitor neonatal for adrenal insufficiency after birth. |
Clinical note
Comprehensive clinical and safety monograph for PRELONE (PRELONE).
| Placental transfer | Prednisolone crosses the placenta but is extensively metabolized to inactive prednisone. Only about 10% of maternal dose reaches fetus. Fetal exposure is lower than with other corticosteroids. |
| Breastfeeding |
■ FDA Black Box Warning
None
| Serious Effects |
Systemic fungal infectionsHypersensitivity to prednisolone or any component
| Precautions | Adrenal suppression with prolonged therapy, Increased susceptibility to infections, Osteoporosis with long-term use, Avascular necrosis of femoral head, Gastrointestinal perforation, especially in diverticulitis or colitis, Psychiatric disturbances, Exacerbation of hypertension and heart failure, Cataracts and glaucoma with prolonged use, Kaposi sarcoma has been reported |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they can increase prednisolone levels. Limit salt and fluid intake if edema or hypertension occurs. Take with food to minimize gastrointestinal irritation. |
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| Prednisolone enters breast milk in low concentrations (estimated infant dose <10% of maternal weight-adjusted dose). No adverse effects reported in infants. Use lowest effective dose; avoid high-dose therapy (e.g., >40 mg/day) or consider timing breastfeeding 4 hours after dose. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | First trimester: Corticosteroids are associated with a small increased risk of orofacial clefts (odds ratio ~1.3-3.0). Second/third trimester: Prolonged therapy may increase risk of preterm delivery, intrauterine growth restriction, and maternal hyperglycemia. Fetal adrenal suppression possible with high doses near term. |
| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, and signs of infection. Serial fetal growth ultrasound if prolonged therapy. Assess for adrenal insufficiency in newborns after in utero exposure to high doses. |
| Fertility Effects | No established adverse effects on fertility. Corticosteroids may be used to treat autoimmune conditions that otherwise impair fertility. |
| Clinical Pearls | PRELONE (prednisolone) is a corticosteroid with high anti-inflammatory potency. Use for short-term exacerbations; taper to avoid adrenal insufficiency. Monitor for hyperglycemia, hypertension, and osteoporosis with prolonged use. Avoid live vaccines during therapy. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not stop suddenly; follow the tapering schedule prescribed by your doctor. · Report signs of infection (fever, sore throat) or unusual weight gain/swelling. · Wear a medical alert bracelet indicating corticosteroid use. · Avoid live vaccines (e.g., MMR, flu mist) while on this medication. |