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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GLYCORT (GLYCORT).
| Breastfeeding | Excreted in breast milk; M/P ratio 0.2-0.4. Use with caution; monitor infant for growth and adrenal suppression. Alternative therapies preferred. |
| 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 |
■ FDA Black Box Warning
None.
| Serious Effects |
["Systemic fungal infections","Administration of live or live attenuated vaccines","Hypersensitivity to any component"]
| 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. |
Loading safety data…
| 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. |