ALPHADROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALPHADROL (ALPHADROL).
Selective glucocorticoid receptor agonist with high potency, binding to the glucocorticoid receptor and modulating gene transcription, leading to anti-inflammatory and immunosuppressive effects.
| Metabolism | Hepatic via CYP3A4; undergoes extensive first-pass metabolism. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugates (20-25%); biliary/fecal excretion accounts for 5-10%. |
| Half-life | Terminal elimination half-life of 12-15 hours in healthy adults; prolonged in renal impairment (up to 30 hours) requiring dose adjustment. |
| Protein binding | Highly protein bound (92-95%), primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg; indicates extensive distribution into total body water with some tissue binding. |
| Bioavailability | Oral: 70-80% due to first-pass metabolism; intramuscular: 90-100%. |
| Onset of Action | Oral: 1-2 hours; intravenous: within 5-10 minutes; intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 6-8 hours; intravenous: 4-6 hours; intramuscular: 6-8 hours; duration may be extended in hepatic impairment. |
0.5 mg intravenously every 4 hours as needed; maximum 2 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: administer 50% of dose; GFR <10 mL/min: avoid use due to risk of accumulation. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: contraindicated. |
| Pediatric use | 0.01 mg/kg intravenously every 4-6 hours; maximum 0.2 mg/kg/day. |
| Geriatric use | Initiate with 0.25 mg intravenously every 6 hours; titrate cautiously due to increased sensitivity and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ALPHADROL (ALPHADROL).
| Breastfeeding | Excreted into breast milk; M/P ratio not reported. Potential for infant adrenal suppression and growth retardation. Breastfeeding not recommended during therapy and for at least 3 months after last dose. |
| Teratogenic Risk | ALPHADROL is contraindicated in pregnancy. First trimester exposure associated with increased risk of cleft palate, cardiac defects, and neural tube defects. Second and third trimester exposure can cause fetal growth restriction, oligohydramnios, and adrenal suppression. Risk category X. |
■ FDA Black Box Warning
None
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to the drug or any component","Administration of live or live attenuated vaccines"]
| Precautions | ["Increased risk of infections due to immunosuppression","Adrenal suppression with prolonged use","Osteoporosis with long-term use","Exacerbation of diabetes mellitus","Psychiatric disturbances"] |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase drug levels. Take with food to reduce gastrointestinal irritation. Limit sodium intake to reduce fluid retention; consider potassium-rich foods. |
| Clinical Pearls |
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| Fetal Monitoring |
| Monitor fetal growth by ultrasound every 4 weeks; assess amniotic fluid volume; fetal echocardiography at 20-24 weeks if first trimester exposure. Maternal monitoring: blood pressure, glucose, electrolytes, and signs of infection. Adrenal function testing in neonates if used near term. |
| Fertility Effects | May impair fertility in both males and females; reversible upon discontinuation. Oligospermia in males; ovulatory dysfunction in females. |
| Monitor blood glucose closely in diabetic patients; may cause hyperglycemia. Administer with food to reduce GI upset. Taper dose over 1-2 weeks after prolonged use to avoid adrenal insufficiency. Avoid live vaccines during therapy. |
| Patient Advice | Take with food or milk to prevent stomach upset. · Do not stop taking this medication suddenly without consulting your doctor. · Report any signs of infection (fever, sore throat) or unusual bleeding/bruising. · Avoid alcohol while on this medication. · Inform all healthcare providers that you are taking Alphadrol. |