ALPHATREX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALPHATREX (ALPHATREX).
ALPHATREX is a synthetic corticosteroid that binds to the glucocorticoid receptor, leading to modulation of gene transcription and suppression of inflammatory cytokines, immune responses, and edema.
| Metabolism | Hepatic via CYP3A4; also metabolized by 11β-HSD2 to inactive metabolites. |
| Excretion | Renal excretion of unchanged drug accounts for 40-60% of elimination; hepatic metabolism accounts for 30-40%, with metabolites excreted in bile and feces (10-20%). |
| Half-life | Terminal elimination half-life is 12-18 hours in patients with normal renal function; prolonged to 24-48 hours in moderate renal impairment (CrCl <50 mL/min). |
| Protein binding | 92-96% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd approximately 0.8-1.2 L/kg, indicating extensive tissue distribution and penetration into extravascular spaces. |
| Bioavailability | Oral: 75-85% (with food reducing absorption by 20%); Intramuscular: 90-100%; Rectal: 50-60%. |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-15 minutes; Intramuscular: 30-60 minutes. |
| Duration of Action | Oral: 8-12 hours; Intravenous: 4-6 hours; Intramuscular: 6-8 hours. Duration may be extended in hepatic impairment. |
| Molecular Weight | 482.54 |
1-2 mg/kg IV every 24 hours; maximum single dose 150 mg.
| Dosage form | CREAM |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: 50% of normal dose every 24 hours; GFR <10 mL/min: 25% of normal dose every 48 hours. |
| Liver impairment | Child-Pugh Class A (mild): no dose adjustment; Child-Pugh Class B (moderate): reduce dose by 50%; Child-Pugh Class C (severe): not recommended. |
| Pediatric use | 0.5-1 mg/kg IV every 24 hours; maximum single dose 100 mg; safety in infants <6 months not established. |
| Geriatric use | Initiate at lowest adult dose (1 mg/kg IV every 24 hours); monitor renal function and adjust per renal guidelines due to age-related decreased creatinine clearance. |
| 1st trimester | Teratogenic effects observed in animal studies; avoid use during first trimester. |
| 2nd trimester | Use only if potential benefit justifies risk to fetus; may cause fetal harm. |
| 3rd trimester | Avoid use in third trimester due to risk of neonatal hypoglycemia and withdrawal. |
Clinical note
Comprehensive clinical and safety monograph for ALPHATREX (ALPHATREX).
| Placental transfer | Crosses placenta readily with fetal concentrations approaching maternal levels within hours. |
| Breastfeeding | Excreted in human milk; potential for serious adverse reactions in nursing infants. Decision to discontinue nursing or discontinue drug based on importance of drug to mother. |
| Lactation Rating |
■ FDA Black Box Warning
Corticosteroids may increase risk of infection; do not administer live vaccines to patients on immunosuppressive doses. Long-term use may lead to adrenal suppression; withdrawal should be gradual. Use in pregnancy only if clear benefit justifies risk to fetus.
| Serious Effects |
Hypersensitivity to alphatrex or any componentCurrent or history of severe depressionRheumatic heart disease
| Precautions | Increased susceptibility to infections; avoid exposure to varicella or measles., Adrenal suppression with prolonged therapy; taper dose gradually., Osteoporosis risk with chronic use; monitor bone density., Hyperglycemia; monitor blood glucose in diabetic patients., Psychiatric disturbances (e.g., euphoria, depression, psychosis)., Cushing's syndrome with high doses or long-term use., Vaccination: Avoid live attenuated vaccines., Use with caution in patients with peptic ulcer disease, hypertension, congestive heart failure, or renal insufficiency. |
| Food/Dietary | Grapefruit and grapefruit juice may increase serum levels; avoid concurrent use. High-fat meals can enhance absorption; take with food if gastrointestinal upset occurs. |
Loading safety data…
| L4 (Possibly Hazardous) |
| Teratogenic Risk | Category C: First trimester exposure may increase risk of musculoskeletal anomalies and cleft palate; second and third trimester exposure associated with premature closure of ductus arteriosus and oligohydramnios. Risk of fetal bradycardia and impaired renal function. |
| Fetal Monitoring | Serial ultrasound for fetal growth, amniotic fluid index, and ductus arteriosus patency; fetal heart rate monitoring; maternal blood pressure and renal function (serum creatinine, BUN) every 2 weeks. |
| Fertility Effects | May cause reversible impairment of spermatogenesis in males; in females, possible disruption of ovulation due to altered prostaglandin synthesis. Normal fertility often returns after discontinuation. |
| Clinical Pearls | ALPHATREX is a synthetic retinoid; monitor for hepatotoxicity and hypertriglyceridemia. Avoid in pregnancy due to teratogenicity. Use with caution in patients with diabetes due to risk of glucose intolerance. |
| Patient Advice | Take with a full glass of water to reduce esophageal irritation. · Avoid alcohol consumption to minimize hepatotoxicity risk. · Use effective contraception during treatment and for 1 month after discontinuation. · Report signs of liver dysfunction (jaundice, dark urine, abdominal pain) immediately. · Do not take vitamin A supplements to avoid hypervitaminosis A. |