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. |
| 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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRELONE (PRELONE).
| Breastfeeding | Prednisolone (active metabolite) is excreted into breast milk in low concentrations. M/P ratio approximately 0.22. Doses up to 40 mg daily are considered compatible with breastfeeding; avoid nursing within 4 hours of dose to minimize infant exposure. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
["Systemic fungal infections","Known hypersensitivity to prednisolone or its components","Administration of live or live attenuated vaccines in immunosuppressive doses"]
| 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"] |
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| 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. |