ANDROID 25
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANDROID 25 (ANDROID 25).
Android 25 contains methyltestosterone, a synthetic androgen that binds to androgen receptors, promoting protein synthesis and anabolic effects. It also inhibits gonadotropin secretion from the pituitary, reducing endogenous testosterone production.
| Metabolism | Primarily hepatic via reduction and oxidation; metabolites include androsterone and etiocholanolone; excreted in urine. |
| Excretion | Renal: 90% (as glucuronide and sulfate conjugates, 5–10% unchanged); fecal/biliary: 10% |
| Half-life | Terminal elimination half-life: 10–100 minutes (testosterone); clinical context: rapid clearance necessitates frequent dosing or use of esters for sustained effect |
| Protein binding | 97–99% (sex hormone-binding globulin and albumin) |
| Volume of Distribution | 0.3–0.6 L/kg; indicates distribution into lean muscle and sex organs |
| Bioavailability | Oral: <5% (methyltestosterone: ~20–25% due to 17α-alkylation); IM: 100% |
| Onset of Action | Oral: 1–2 hours (methyltestosterone); IM: 24–48 hours (testosterone esters) |
| Duration of Action | Oral: 6–8 hours (methyltestosterone); IM: 2–4 weeks (testosterone cypionate/enanthate) |
Testosterone 25 mg subcutaneously or intramuscularly every 2 to 4 weeks. Alternatively, 125 mg intramuscularly every 10 days.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, consider reducing dose or increasing interval; monitor for fluid retention and hypertension. |
| Liver impairment | Contraindicated in Child-Pugh class B or C cirrhosis. For mild hepatic impairment (Child-Pugh A), start with lower dose (e.g., 12.5 mg every 2 weeks) and titrate based on response and liver function. |
| Pediatric use | Not recommended for use in pediatric patients (safety and efficacy not established). For male adolescents with hypogonadism, individualize: start at 12.5 mg every 2 weeks and adjust based on testosterone levels and growth. |
| Geriatric use | Start with lower initial dose (e.g., 12.5 mg every 2 weeks); monitor prostate-specific antigen (PSA) and hematocrit frequently. Avoid in patients with prostate cancer or untreated sleep apnea. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANDROID 25 (ANDROID 25).
| Breastfeeding | Methyltestosterone is excreted into breast milk; M/P ratio not established. May cause virilization in female infants and premature sexual development in male infants. Androgens can suppress lactation. Use during breastfeeding is contraindicated. |
| Teratogenic Risk | Android 25 (methyltestosterone) is an androgen. First trimester: Virilization of female fetus, including clitoromegaly, labial fusion, urogenital sinus abnormalities if exposure occurs before 12 weeks gestation. Second and third trimesters: Continued risk of female pseudohermaphroditism, and potential for masculinization of female external genitalia. Androgens can cross the placenta and may also cause skeletal abnormalities and growth retardation. Pregnancy category X. |
■ FDA Black Box Warning
WARNING: Androgens are contraindicated in pregnancy due to masculinization of female fetus. Hepatotoxicity, including peliosis hepatis and hepatic neoplasms, has been reported with prolonged use.
| Serious Effects |
Known or suspected prostate cancer; male breast cancer; pregnancy; lactation; hypersensitivity to methyltestosterone; severe hepatic impairment.
| Precautions | Use with caution in patients with hepatic, renal, or cardiovascular disease; may cause gynecomastia, edema, hypercalcemia, and polycythemia; monitor liver function, lipid profile, and hematocrit periodically; may accelerate bone maturation in children; risk of prostate hypertrophy and urethral obstruction. |
| Food/Dietary | Take with food containing fat (e.g., avocado, nuts, olive oil) to enhance absorption. Avoid grapefruit juice as it may increase testosterone levels via CYP3A4 inhibition. Limit alcohol due to potential liver effects. |
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| Fetal Monitoring | Monitor maternal blood pressure, liver function tests, lipid profile, and signs of virilization (e.g., hirsutism, acne, voice deepening). Fetal monitoring: Ultrasound for fetal genital development and growth if inadvertent exposure occurs during pregnancy. |
| Fertility Effects | Methyltestosterone can suppress spermatogenesis in males due to negative feedback on gonadotropin release, potentially causing oligospermia or azoospermia. In females, it may disrupt normal ovulatory cycles and cause menstrual irregularities, impairing fertility. Effects are generally reversible upon discontinuation. |
| Clinical Pearls | Android 25 (testosterone undecanoate) requires absorption via lymphatic system; administer with fat-containing meal. Monitor serum testosterone levels 3-5 hours post-dose. Avoid in patients with breast cancer or known or suspected prostate cancer. Risk of polycythemia; check hematocrit before and during therapy. |
| Patient Advice | Take capsules with meals, especially those containing fat, to improve absorption. · Do not chew or crush capsules; swallow whole. · Report signs of deep vein thrombosis (leg swelling, pain) or pulmonary embolism (sudden dyspnea, chest pain). · Women of reproductive potential should avoid pregnancy; use effective contraception. · Keep out of reach of children; testosterone can cause serious harm if accidentally ingested. · Regular blood tests (testosterone, hematocrit, PSA, lipid profile) are required. |