ANDROID-F
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANDROID-F (ANDROID-F).
Fingolimod is a sphingosine 1-phosphate receptor modulator that sequesters lymphocytes in lymph nodes, reducing central nervous system immune cell infiltration.
| Metabolism | Metabolized primarily by CYP4F2, with minor contributions from CYP2D6, CYP2E1, CYP3A4, and CYP1A2. Undergoes biotransformation to an inactive metabolite. |
| Excretion | Primarily renal (90% as glucuronide and sulfate conjugates, 10% unchanged); small amount biliary/fecal. |
| Half-life | 2.5-3.5 hours (terminal half-life); oral administration may require multiple daily doses for stable levels. |
| Protein binding | 97-99% bound to sex hormone-binding globulin (SHBG) and albumin. |
| Volume of Distribution | 0.5-0.8 L/kg; reflects distribution into muscle, liver, and reproductive tissues. |
| Bioavailability | Oral: 3-6% (extensive first-pass metabolism); IM: 100%. |
| Onset of Action | Intramuscular: 24-48 hours; Oral: 2-3 days (max effect by 1-2 weeks). |
| Duration of Action | IM: 2-4 weeks (depot formulation); Oral: 2-4 days (drug levels return to baseline). |
| Molecular Weight | 288.43 |
Adults: 1 tablet (methyltestosterone 2.5 mg, ethinyl estradiol 0.025 mg) orally once daily, with food.
| Dosage form | TABLET |
| Renal impairment | GFR 10-50 mL/min: reduce dose by 50%. GFR <10 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: reduce dose by 50%. Child-Pugh B: avoid use. Child-Pugh C: contraindicated. |
| Pediatric use | Not recommended for use in children due to risk of premature epiphyseal closure and virilization. |
| Geriatric use | Use with caution; consider lower starting dose due to increased risk of fluid retention, hypertension, and prostatic hypertrophy in males. |
| 1st trimester | Contraindicated due to teratogenicity (virilization of female fetus). |
| 2nd trimester | Contraindicated; virilization of female fetus. |
| 3rd trimester | Contraindicated; virilization of female fetus. |
Clinical note
Comprehensive clinical and safety monograph for ANDROID-F (ANDROID-F).
| Placental transfer | Crosses placenta; androgens can cause virilization of female fetus. |
| Breastfeeding | Excreted into breast milk; may cause virilization in female infants. Not recommended during breastfeeding. |
| Lactation Rating | L5 (Contraindicated) |
■ FDA Black Box Warning
Risk of bradyarrhythmia and atrioventricular block, requiring first-dose monitoring for 6 hours. Fatal infections, including opportunistic infections, have occurred. Macular edema has been reported.
| Serious Effects |
PregnancyKnown or suspected carcinoma of the breast or prostateHypersensitivity to testosterone or any component
| Precautions | May cause bradycardia and AV block; monitor heart rate after first dose. Increased risk of infections, including herpes viruses and cryptococcal meningitis. Macular edema, especially in patients with diabetes or uveitis. Posterior reversible encephalopathy syndrome (PRES). Respiratory effects, including decreased FEV1 and DLCO. Hepatic injury; monitor liver enzymes. |
| Food/Dietary | No significant food interactions reported. Avoid excessive alcohol consumption due to hepatotoxic effects. |
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| Teratogenic Risk | ANDROID-F contains methyltestosterone, a synthetic androgen. Androgens are teratogenic in humans. In first trimester: masculinization of female fetus, including clitoromegaly, labial fusion, and urogenital sinus abnormalities. Second and third trimesters: continued virilization of female fetus; no increased risk of malformations in male fetuses. Contraindicated in pregnancy. |
| Fetal Monitoring | Monitor pregnant patients: serial ultrasound to assess fetal anatomy and growth (particularly genital development if female). After birth: evaluate female infants for signs of virilization. Maternal monitoring: liver function tests, lipid profile, hemoglobin/hematocrit for polycythemia; clinical assessment for fluid retention, hypertension, and hirsutism. |
| Fertility Effects | Methyltestosterone can suppress endogenous testosterone production via negative feedback on hypothalamic-pituitary-gonadal axis, leading to oligospermia or azoospermia in males. In females, high doses may cause anovulation and menstrual irregularities. Effects on fertility are typically reversible upon discontinuation but may persist with prolonged use. |
| Clinical Pearls | Android-F is a brand of methyltestosterone, an androgen used primarily for male hypogonadism. Monitor liver function due to potential hepatotoxicity. Avoid in males with breast or prostate cancer. Use with caution in older patients due to increased risk of prostatic hypertrophy. May suppress clotting factors II, V, VII, and X. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency. · Report any signs of liver problems (yellowing eyes/skin, dark urine, persistent nausea) immediately. · Women should report hoarseness, acne, or menstrual changes. · Men should report frequent or persistent erections, or breast swelling/tenderness. · May cause decreased sperm count in men; discuss family planning. · Avoid concurrent use with other medications without consulting doctor. |