PREDNISOLONE TEBUTATE
Clinical safety rating: avoid
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
Corticosteroid that binds to glucocorticoid receptors, leading to modulation of gene expression and suppression of inflammatory mediators (e.g., prostaglandins, leukotrienes) and immune cell activity.
| Metabolism | Primarily hepatic via CYP3A4 to inactive metabolites. |
| Excretion | Renal: primarily as metabolites, <20% unchanged; small fecal/biliary contribution. |
| Half-life | Terminal half-life: 2-4 hours (plasma); clinical effects persist longer (18-36 hours) due to prolonged receptor occupancy and transcriptional effects. |
| Protein binding | 70-90% bound primarily to corticosteroid-binding globulin (CBG) and albumin. |
| Volume of Distribution | 0.6-1.0 L/kg reflecting extensive distribution into tissues. |
| Bioavailability | Oral: 70-100%; intra-articular: 100% locally, with minimal systemic absorption (systemic bioavailability <10%). |
| Onset of Action | Intra-articular: 24-48 hours; oral: 2-6 hours; intravenous: immediate to 2 hours. |
| Duration of Action | Intra-articular: 1-4 weeks depending on joint and dose; oral: 12-36 hours; intravenous: 24-48 hours. |
20-60 mg intramuscularly or intra-articularly once daily as a single dose or divided every 6-12 hours; dose varies by indication and severity.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for renal impairment; use with caution in severe renal impairment due to potential fluid retention. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: reduce dose by 50% or use alternative. |
| Pediatric use | 0.5-2 mg/kg/day intramuscularly or intra-articularly as a single dose or divided every 6-12 hours; not to exceed 80 mg/day. |
| Geriatric use | Initiate at lower end of dosing range (10-20 mg/day) due to increased risk of osteoporosis, glucose intolerance, and immunosuppression; monitor closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
| FDA category | Positive |
| Breastfeeding | Prednisolone enters breast milk; M/P ratio approximately 0.15–0.25. Doses ≤20 mg daily considered safe; temporary avoidance of breastfeeding for 4 hours after high doses recommended. Monitor infant for adrenal suppression if mother on prolonged high doses. |
| Teratogenic Risk |
■ FDA Black Box Warning
None.
| Common Effects | immunosuppression |
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to prednisolone or any component","Administration of live or live-attenuated vaccines"]
| Precautions | ["May cause immunosuppression and increase infection risk.","Long-term use may lead to adrenal suppression, osteoporosis, and growth retardation in children.","Monitor for hyperglycemia, hypertension, and electrolyte disturbances.","Avoid abrupt withdrawal after prolonged therapy."] |
Loading safety data…
| First trimester: Increased risk of orofacial clefts (odds ratio 1.5–3.0) based on epidemiological studies. Second/third trimester: Risk of fetal adrenal suppression, low birth weight, and preterm delivery with prolonged use. High doses may cause fetal growth restriction. No specific data for prednisolone tebutate; profile extrapolated from prednisolone. |
| Fetal Monitoring | Monitor maternal blood glucose, blood pressure, and signs of infection. Fetal surveillance with serial growth ultrasounds if prolonged therapy. Assess newborn for adrenal insufficiency, hypoglycemia, and respiratory status. |
| Fertility Effects | No direct negative effects on fertility reported. Adrenal suppression from high-dose therapy may disrupt ovulation; effects reversible upon dose reduction or discontinuation. |