HEXADROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HEXADROL (HEXADROL).
Synthetic glucocorticoid that binds to the glucocorticoid receptor, leading to regulation of gene expression and suppression of inflammatory cytokines, immune response, and adrenal function.
| Metabolism | Primarily hepatic via CYP3A4; metabolites are excreted in urine. |
| Excretion | Primarily renal: ~65-80% as unchanged drug and metabolites via glomerular filtration, with tubular reabsorption; minor biliary/fecal (5-10%). |
| Half-life | Terminal elimination half-life: 36-54 hours; prolonged in hepatic impairment (up to 72 hours) due to reduced clearance. |
| Protein binding | 70-80% bound; primary binding to corticosteroid-binding globulin (CBG) and albumin. |
| Volume of Distribution | 0.8-1.0 L/kg; indicates extensive tissue distribution, including crossing the blood-brain barrier. |
| Bioavailability | Oral: 80-90% (well absorbed); IM: 100% (systemic). |
| Onset of Action | Oral: 1-2 hours; IV: rapid (minutes to 1 hour); IM: 1-2 hours; topical: varies. |
| Duration of Action | Oral: 1-2 days (due to long half-life); IV: 1-2 days; IM: 1-3 weeks (repository forms). |
Adult: 0.75-9 mg/day orally in divided doses every 6-12 hours; IV/IM: initial 0.5-9 mg/day in divided doses every 6-12 hours.
| Dosage form | ELIXIR |
| Renal impairment | No specific GFR-based dose adjustments required; use with caution in severe renal impairment (eGFR <30 mL/min). |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B/C: reduce dose by 50% or use lowest effective dose. |
| Pediatric use | 0.08-0.3 mg/kg/day or 2.5-10 mg/m²/day orally in divided doses every 6-12 hours; IV/IM: 0.08-0.3 mg/kg/day in divided doses every 12-24 hours. |
| Geriatric use | Start at lowest effective dose (e.g., 0.75 mg/day) and titrate slowly; monitor for hyperglycemia, osteoporosis, and infections. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HEXADROL (HEXADROL).
| Breastfeeding | Enters breast milk; M/P ratio ~0.3; low concentrations; considered compatible with breastfeeding but monitor infant for adrenal suppression if high maternal doses. |
| Teratogenic Risk | First trimester: Increased risk of cleft palate (odds ratio 3.6), orofacial clefts; second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, oligohydramnios with prolonged high-dose use. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to dexamethasone or any component","Administration of live virus vaccines in patients on immunosuppressive doses"]
| Precautions | ["Immunosuppression and increased susceptibility to infections","Hypothalamic-pituitary-adrenal axis suppression and adrenal insufficiency with withdrawal","Gastrointestinal perforation (especially in colitis)","Osteoporosis and avascular necrosis","Ocular effects: cataracts, glaucoma","Psychiatric disturbances","Cardiovascular effects: hypertension, fluid retention","Growth suppression in children"] |
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| Maternal: Blood pressure, blood glucose, signs of infection; Fetal: Ultrasound for growth and amniotic fluid index; neonatal: Adrenal function if prolonged exposure. |
| Fertility Effects | May inhibit gonadotropin secretion leading to ovulatory dysfunction; reversible upon discontinuation. |