GLYCORT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GLYCORT (GLYCORT).
Glucocorticoid receptor agonist; modulates gene expression to produce anti-inflammatory and immunosuppressive effects.
| Metabolism | Hepatic via CYP3A4; primarily to inactive metabolites. |
| Excretion | Renal: 70% as unchanged drug; biliary/fecal: 25% (metabolites); 5% other |
| Half-life | 3.5 hours (terminal); prolonged in hepatic impairment (up to 8 hours) and severe renal impairment (up to 6 hours) |
| Protein binding | 90% (primarily albumin and corticosteroid-binding globulin) |
| Volume of Distribution | 0.8 L/kg (high, indicating extensive tissue distribution) |
| Bioavailability | Oral: 60-70% (due to first-pass metabolism); IM: 80-100% |
| Onset of Action | IV: 5-10 minutes; oral: 30-60 minutes; IM: 15-30 minutes |
| Duration of Action | Oral/IV: 6-12 hours (dose-dependent); IM: 12-24 hours |
| Molecular Weight | 360.44 |
Intravenous: 2 mg/kg every 12 hours; Oral: 20 mg twice daily.
| Dosage form | LOTION |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 25%; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: use not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: use not recommended. |
| Pediatric use | Intravenous: 0.5-1 mg/kg every 12 hours; Oral: 1 mg/kg twice daily, maximum 40 mg per day. |
| Geriatric use | Initiate at lowest adult dose; monitor renal function; maximum oral dose 40 mg daily. |
| 1st trimester | Avoid: Corticosteroids are associated with increased risk of oral clefts (odds ratio 3.3) and other malformations. Use only if clearly needed and benefits outweigh risks. |
| 2nd trimester | Use with caution: May cause fetal growth restriction, adrenal suppression, and premature delivery. Monitor fetal growth and consider lowest effective dose. |
| 3rd trimester | Use with caution: Risk of adrenal suppression in neonate (withdrawal symptoms), premature delivery, and low birth weight. Taper dose gradually before delivery if possible. |
Clinical note
Comprehensive clinical and safety monograph for GLYCORT (GLYCORT).
| Placental transfer | Prednisolone crosses the placenta but is inactivated by placental 11β-hydroxysteroid dehydrogenase 2; however, at high maternal doses, significant transfer can occur. Ratio of cord to maternal plasma concentrations is approximately 0.1-0.5. |
| Breastfeeding | Prednisolone is excreted into breast milk in low concentrations (less than 10% of maternal dose) and is unlikely to cause adverse effects in term infants. However, with high doses (>40 mg/day), monitor infant for adrenal suppression, growth, and development. Consider timing breastfeeding 4 hours after dose to reduce infant exposure. |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionKnown hypersensitivity to prednisolone or any componentAdministration of live or live attenuated vaccines (due to immunosuppression)
| Precautions | Immunosuppression and increased risk of infections, Adrenal suppression and withdrawal syndrome, Osteoporosis with long-term use, Growth suppression in children, Cushing's syndrome with high doses, Gastrointestinal perforation risk, Masking of infection signs, Increased intraocular pressure, Psychiatric disturbances |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they inhibit CYP3A4 and can increase colchicine levels, raising toxicity risk. No other significant food interactions. |
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| Lactation Rating | L2 - Safer |
| Teratogenic Risk | First trimester: Increased risk of cleft palate (odds ratio ~3.4). Second/third trimesters: Risk of fetal adrenal suppression, growth restriction, and preterm birth. Dose-dependent; avoid high doses. |
| Fetal Monitoring | Maternal: Blood pressure, blood glucose, and signs of infection. Fetal: Ultrasound for growth restriction every 4 weeks, nonstress test after 28 weeks if prolonged use. |
| Fertility Effects | May cause menstrual irregularities and inhibit ovulation due to hypothalamic-pituitary-adrenal axis suppression. Reversible upon dose reduction or discontinuation. |
| Clinical Pearls |
| For acute gout flares, initiate at 0.6 mg twice daily for 2 days, then 0.6 mg once daily for up to 5 days; avoid use in patients with severe renal impairment (CrCl <30 mL/min) or concomitant strong CYP3A4 inhibitors. Monitor for diarrhea and neutropenia. Colchicine toxicity can occur with therapeutic doses in hepatic or renal impairment. |
| Patient Advice | Take exactly as prescribed; do not exceed recommended dose. · Discontinue immediately and contact healthcare provider if you experience severe diarrhea, vomiting, or muscle weakness. · Avoid grapefruit juice and grapefruit products during treatment. · Do not take with other colchicine-containing products. · Seek emergency care for signs of overdose: bloody diarrhea, burning throat, or seizures. |