HALDRONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HALDRONE (HALDRONE).
Glucocorticoid receptor agonist; suppresses inflammation and immune responses by inhibiting phospholipase A2, reducing prostaglandin and leukotriene synthesis, and modulating gene transcription.
| Metabolism | Hepatic; primarily via CYP3A4. |
| Excretion | Renal: 20-30% as unchanged drug; biliary/fecal: 70-80% as metabolites and unchanged drug. |
| Half-life | Terminal elimination half-life: 2.6-3.8 hours. Clinical context: Short half-life requires multiple daily dosing; no significant accumulation with regular dosing. |
| Protein binding | 85-90%, primarily to albumin and corticosteroid-binding globulin. |
| Volume of Distribution | Vd: 1.4-1.6 L/kg. Clinical meaning: Indicates extensive tissue distribution, with high penetration into tissues including brain. |
| Bioavailability | Oral: 60-70% due to first-pass metabolism; IM: 100%. |
| Onset of Action | Oral: 1-2 hours; Intramuscular: 30-60 minutes; Intravenous: within minutes. |
| Duration of Action | Oral: 6-12 hours depending on dose; IM: 12-24 hours; IV: 4-6 hours. Duration is prolonged with higher doses or in hepatic impairment. |
Oral: Initial dose 50-100 mg twice daily; maintenance 25-50 mg twice daily. Maximum 200 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: Reduce dose by 25%. GFR 15-29 mL/min: Reduce dose by 50%. GFR <15 mL/min: Avoid use. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Avoid use. |
| Pediatric use | Safety and efficacy not established; use not recommended. |
| Geriatric use | Start at lower end of dosing range; monitor renal function and electrolyte levels. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HALDRONE (HALDRONE).
| Breastfeeding | Enters breast milk. M/P ratio unknown. Low doses (<20 mg/day prednisone equivalent) are compatible with breastfeeding; high doses may suppress infant adrenal function. Avoid if maternal dose >40 mg/day. |
| Teratogenic Risk | FDA Pregnancy Category D. Corticosteroids cross the placenta. First trimester: increased risk of cleft palate (odds ratio 3-5). Second/third trimester: fetal adrenal suppression, intrauterine growth restriction, premature rupture of membranes. Chronic exposure may cause neonatal adrenal insufficiency. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to Haldrone or any of its components","Administration of live or live attenuated vaccines in immunocompromised patients","Idiopathic thrombocytopenic purpura (for intramuscular use)"]
| Precautions | ["Immunosuppression: Increased risk of infections; may mask signs of infection.","Hypothalamic-pituitary-adrenal (HPA) axis suppression with prolonged use; taper upon discontinuation.","Exacerbation of systemic fungal infections; avoid in active infections without appropriate therapy.","May cause gastrointestinal perforation in patients with diverticulitis, fresh intestinal anastomoses, or peptic ulcer disease.","May exacerbate diabetes mellitus, hypertension, osteoporosis, and glaucoma.","Use caution in patients with congestive heart failure, thromboembolic disorders, and seizure disorders.","May cause growth suppression in children; monitor growth in pediatric patients."] |
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| Fetal Monitoring |
| Monitor maternal blood pressure, blood glucose, and signs of infection. Serial ultrasound for fetal growth and amniotic fluid volume. Assess fetal adrenal function if prolonged therapy near term. |
| Fertility Effects | May impair fertility by disrupting hypothalamic-pituitary-adrenal axis and menstrual cyclicity. Reversible upon dose reduction or discontinuation. No evidence of permanent infertility. |