ANADROL-50
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANADROL-50 (ANADROL-50).
Anabolic steroid; binds to androgen receptors, increasing protein synthesis and promoting nitrogen retention, leading to muscle growth and erythropoietin production.
| Metabolism | Hepatic, primarily via reduction and glucuronidation; undergoes enterohepatic circulation. |
| Excretion | Primarily renal: 90% as glucuronide and sulfate conjugates; 6% fecal; <3% unchanged. |
| Half-life | Terminal elimination half-life: 4-6 hours for parent drug; active metabolite 17α-methyl-5α-androstan-3α,17β-diol has half-life ~12-18 hours. Requires multiple daily dosing. |
| Protein binding | ~75-80% bound to albumin and sex hormone-binding globulin (SHBG). |
| Volume of Distribution | ~20-30 L/kg; extensive tissue distribution, especially skeletal muscle and liver. |
| Bioavailability | Oral: ~40-60% (extensive first-pass metabolism); IM: 100%. |
| Onset of Action | Oral: 2-3 hours; intramuscular (sustained release formulations): 24-48 hours. |
| Duration of Action | Oral: 6-8 hours; IM: up to 2 weeks. Clinical androgenic effects persist longer. |
Adults: 50-200 mg orally once daily for 2-6 weeks, then 2-4 weeks off. Not for continuous use.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with nephrosis or significant renal impairment. No specific GFR-based dose adjustments established. |
| Liver impairment | Contraindicated in severe hepatic disease (Child-Pugh class C). Use with caution in mild to moderate impairment; reduce dose or discontinue if abnormalities develop. No specific dose recommendations for Child-Pugh A or B. |
| Pediatric use | Weight-based dosing: 1-2 mg/kg orally once daily for 2-6 weeks. Maximum 50 mg/day. Use only in severe growth failure or anemia. Monitor bone age and growth velocity. |
| Geriatric use | Use lowest effective dose due to increased risk of prostatic hypertrophy, hepatotoxicity, and fluid retention. Start at 50 mg orally once daily; titrate based on response and tolerability. Monitor prostate-specific antigen (PSA) and liver function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANADROL-50 (ANADROL-50).
| Breastfeeding | Excretion into breast milk unknown; potential for serious adverse effects in nursing infants (virilization, growth disturbances). M/P ratio not established. Contraindicated during breastfeeding. |
| Teratogenic Risk | First trimester: High risk of fetal masculinization in female fetuses (clitoral enlargement, labial fusion). Second and third trimesters: Continued risk of virilization, potential for premature closure of epiphyseal growth plates, and other androgenic effects. Use contraindicated throughout pregnancy. |
■ FDA Black Box Warning
Anabolic steroids may cause severe hepatic toxicity, including hepatic neoplasms, peliosis hepatis, and cholestatic hepatitis. Prolonged use may increase risk of liver tumors and fatal liver disease.
| Serious Effects |
Carcinoma of the breast or prostate, hypercalcemia, nephrotic syndrome, known or suspected pregnancy, hypersensitivity to any component, severe hepatic impairment.
| Precautions | Hepatotoxicity, peliosis hepatis, hepatic neoplasms, altered serum lipids (decreased HDL, increased LDL), erythrocytosis, hypercalcemia, glucose intolerance, premature epiphyseal closure in children, pseudotumor cerebri, increased risk of prostatic hypertrophy and carcinoma, and edema due to salt and water retention. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase drug levels and toxicity. Limit high-fat meals to reduce potential gastrointestinal upset. Ensure adequate protein intake for optimal response. Avoid alcohol completely due to hepatotoxicity. |
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| Fetal Monitoring |
| Monitor maternal liver function (transaminases, bilirubin), lipid profile, blood glucose (risk of hyperglycemia), and signs of virilization. For fetus: ultrasound for growth restriction, skeletal development, and genital abnormalities if inadvertent exposure. |
| Fertility Effects | In males: May suppress spermatogenesis via negative feedback on gonadotropins, causing oligospermia or azoospermia; effects may be reversible. In females: May inhibit ovulation and disrupt menstrual cycle; potential for androgenic effects on reproductive organs. |
| Clinical Pearls | Anadrol-50 (oxymetholone) is a potent anabolic steroid with significant hepatotoxicity; monitor liver function tests (LFTs) closely, especially AST, ALT, and bilirubin. Due to its strong androgenic effects, it can cause virilization in women and premature epiphyseal closure in children. Use is contraindicated in prostate or breast cancer in males. Watch for severe fluid retention and hypertension; consider diuretics if needed. Dose adjustments may be necessary with hepatic impairment. Discontinue if jaundice or hepatitis occurs. |
| Patient Advice | Take exactly as prescribed; do not increase dose or duration without consulting your doctor. · Avoid alcohol and acetaminophen to reduce liver stress. · Report signs of liver problems: yellowing skin/eyes, dark urine, abdominal pain, nausea/vomiting. · Women: notify doctor if voice deepens, facial hair grows, or menstrual changes occur. · Men: report breast tenderness, swelling, or difficulty urinating. · Monitor blood pressure regularly; fluid retention is common. · Use effective contraception during treatment and for 3 months after stopping due to hormonal effects. |