ANDROID 5
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANDROID 5 (ANDROID 5).
Androgen receptor agonist; stimulates protein synthesis and growth of androgen-sensitive tissues.
| Metabolism | Hepatic via CYP3A4 and CYP2B6; undergoes first-pass metabolism. |
| Excretion | Primarily renal: ~90% as glucuronide and sulfate conjugates, 6% as unchanged drug; ~5% fecal via bile. |
| Half-life | Terminal elimination half-life is 3.5–5.5 hours; clinical effects may persist for several days due to active metabolites. |
| Protein binding | 98% bound to sex hormone-binding globulin (SHBG) and albumin. |
| Volume of Distribution | Vd approximately 1.0 L/kg; indicates extensive tissue distribution, especially to reproductive organs and bone marrow. |
| Bioavailability | Oral: 15–25% due to first-pass metabolism; buccal or transdermal: higher, but not commercially available for this formulation. |
| Onset of Action | Oral: 1–2 hours for androgenic effects; peak plasma concentrations at 2–4 hours. |
| Duration of Action | Oral: androgenic effects last 8–12 hours; clinical impact on erythropoiesis persists for weeks. |
2.5-10 mg orally once daily in the morning for androgen replacement therapy in adult males.
| Dosage form | TABLET |
| Renal impairment | No specific dose adjustment required based on GFR; caution in severe impairment (CrCl <30 mL/min) due to potential fluid retention. |
| Liver impairment | Contraindicated in Child-Pugh class B and C cirrhosis due to hepatotoxicity risk; in class A, use with caution and monitor liver function. |
| Pediatric use | Not recommended for use in children as it may cause premature epiphyseal closure and virilization; limited data. |
| Geriatric use | Increased risk of prostatic hyperplasia and carcinoma; use lowest effective dose with regular prostate monitoring. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANDROID 5 (ANDROID 5).
| Breastfeeding | Excretion into human milk is unknown. Due to potential for androgenic effects in nursing infants, breastfeeding is not recommended. No M/P ratio available. |
| Teratogenic Risk | Pregnancy Category X. ANDROID 5 (oxandrolone) is contraindicated in pregnancy due to teratogenic effects including masculinization of female fetus, clitoral enlargement, and labial fusion. Risk is highest during first trimester but applies throughout gestation. |
| Fetal Monitoring |
■ FDA Black Box Warning
Warning: Prolonged use may cause virilization in women, premature epiphyseal closure, and increased risk of prostatic hypertrophy/carcinoma.
| Serious Effects |
Known or suspected prostate cancer; breast cancer in males; hypersensitivity to androgens; pregnancy and lactation.
| Precautions | Monitor liver function, lipid profile, and prostate-specific antigen; risk of edema in patients with cardiac disease; avoid use in patients with sleep apnea. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase drug levels. Limit salt intake to reduce fluid retention. Alcohol may increase risk of liver toxicity. |
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| Monitor maternal liver function tests, lipid profile, and signs of virilization (e.g., hirsutism, voice deepening). Fetal ultrasound for abnormal genital development if inadvertent exposure occurs. |
| Fertility Effects | May suppress spermatogenesis and reduce fertility in males by inhibiting gonadotropin secretion. In females, can cause menstrual irregularities and anovulation. Effects are reversible upon discontinuation. |
| Clinical Pearls |
| Android 5 (methyltestosterone) is an androgenic anabolic steroid used for hypogonadism and delayed puberty. Monitor liver function due to hepatotoxicity. Use with caution in elderly due to increased risk of prostatic hypertrophy and carcinoma. Can cause fluid retention in patients with cardiac, renal, or hepatic disease. Avoid in patients with breast cancer or known or suspected prostate cancer. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Report any signs of liver problems: yellowing of skin or eyes, dark urine, severe stomach pain. · Women should report any signs of virilization: hoarseness, acne, menstrual changes, growth of facial hair. · Men should report any breast enlargement, changes in urination, or priapism. · Avoid driving or operating machinery if you experience dizziness or drowsiness. · Do not use if you are pregnant or planning to become pregnant. |