DEPO-TESTOSTERONE
Clinical safety rating: avoid
Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.
Testosterone binds to androgen receptors, activating gene transcription that promotes development of male secondary sexual characteristics, anabolic effects, and erythropoiesis.
| Metabolism | Testosterone is extensively metabolized in the liver via reduction and conjugation, yielding androsterone, etiocholanolone, and dihydrotestosterone (DHT). The CYP3A4 enzyme is involved in oxidative metabolism. |
| Excretion | Testosterone is primarily excreted in urine as glucuronide and sulfate conjugates (90%) and in feces via bile (10%). |
| Half-life | The terminal elimination half-life of testosterone cypionate after intramuscular injection is approximately 8 days, allowing for dosing every 2-4 weeks. |
| Protein binding | Testosterone is 97-99% bound to sex hormone-binding globulin (SHBG) and albumin. |
| Volume of Distribution | Vd is approximately 0.6-1.0 L/kg, indicating distribution into total body water and tissues. |
| Bioavailability | Intramuscular: 100% (depot injection). Not available orally due to first-pass metabolism. |
| Onset of Action | Intramuscular: 2-3 days for initial clinical effect; maximal effects in 1-2 weeks. |
| Duration of Action | Intramuscular: 2-4 weeks depending on dose; sustained levels allow for biweekly to monthly dosing. |
| Molecular Weight | 244.37 |
50-400 mg IM every 2-4 weeks
| Dosage form | INJECTABLE |
| Renal impairment | No adjustment recommended; monitor fluid balance in severe impairment |
| Liver impairment | Contraindicated in Child-Pugh class C; use with caution in class A/B, reduce dose by 50% |
| Pediatric use | Not recommended for use in children; limited data |
| Geriatric use | Lower initial doses (50-100 mg IM every 4 weeks) due to increased risk of prostatic hypertrophy and cardiovascular events |
| 1st trimester | Contraindicated; androgenic effects may cause virilization of female fetus; risk of teratogenicity. |
| 2nd trimester | Contraindicated; continued risk of virilization and potential adverse effects on fetal development. |
| 3rd trimester | Contraindicated; may cause premature closure of epiphyses in fetus and other androgenic effects. |
Clinical note
Corticosteroids may increase edema risk and anticoagulants may have increased effects Can cause polycythemia and increased risk of cardiovascular events.
| FDA category | Contraindicated |
| Placental transfer | Crosses placenta; testosterone derivatives can cause fetal harm. |
| Breastfeeding |
■ FDA Black Box Warning
Exogenous testosterone may cause virilization in pregnant women and is contraindicated in pregnant or breastfeeding women due to risk of fetal harm. Prolonged use of high doses has been associated with peliosis hepatis, hepatic neoplasms, and hepatocellular carcinoma.
| Common Effects | Acne |
| Serious Effects |
PregnancyKnown or suspected carcinoma of the prostateKnown or suspected carcinoma of the male breastSevere hepatic impairmentHypersensitivity to testosterone or any componentNephrosis or history of nephrotic syndrome
| Precautions | Monitor prostate cancer risk, polycythemia (hematocrit increase), and sleep apnea. Use with caution in patients with cardiovascular disease, hepatic impairment, and fluid retention. Risk of venous thromboembolism and worsening of benign prostatic hyperplasia. |
| Food/Dietary |
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| Excreted in breast milk; potential for serious adverse effects in nursing infants, including virilization and hepatotoxicity. Decision to discontinue nursing or drug should be based on importance of drug to mother. |
| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | Contraindicated in pregnancy. Androgens can cause virilization of female fetus (clitoral hypertrophy, labial fusion, urogenital sinus abnormalities) when administered during first trimester. Second and third trimester exposure may lead to clitoral hypertrophy and other virilizing effects. Risk is dose-dependent and severity increases with gestational age at exposure. |
| Fetal Monitoring | Monitor maternal serum testosterone levels to maintain within physiologic range. Monitor for signs of virilization in mother (hirsutism, acne, voice deepening, clitoromegaly). Ultrasound for fetal growth and anatomy if inadvertent exposure during pregnancy. Liver function tests periodically. |
| Fertility Effects | Exogenous testosterone suppresses endogenous gonadotropin release, potentially impairing spermatogenesis in males. Reversible upon discontinuation. In females, may disrupt menstrual cycle and ovulatory function, leading to infertility. Contraceptive advice recommended for women of childbearing potential. |
| No significant food interactions. Avoid excessive grapefruit juice as it may affect CYP3A4 metabolism of testosterone. |
| Clinical Pearls | Depo-Testosterone (testosterone cypionate) is an IM injection typically given every 1-4 weeks. Monitor serum testosterone levels mid-injection interval. Contraindicated in men with breast or prostate cancer. Caution in polycythemia, sleep apnea, and heart failure. Use with aromatase inhibitor if gynecomastia occurs. |
| Patient Advice | Inject deep into the gluteal muscle, rotating sites. · Report signs of blood clots, difficulty breathing, or priapism. · May cause acne, fluid retention, mood changes, and increased PSA. · Do not use if pregnant, breastfeeding, or suspect prostate cancer. · Regular blood tests required to monitor testosterone levels and blood counts. |