STANOZIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STANOZIDE (STANOZIDE).
Androgen receptor agonist; increases protein synthesis and muscle mass by binding to androgen receptors, leading to enhanced nitrogen retention and erythropoiesis.
| Metabolism | Hepatic via reduction and conjugation; primarily excreted in urine. |
| Excretion | Primarily hepatic metabolism (approximately 80%) with biliary excretion of metabolites; renal excretion of unchanged drug is minimal (<5%). Fecal elimination accounts for <15%. |
| Half-life | Terminal elimination half-life is 24-30 hours, supporting once-daily dosing. Clinical context: Steady-state achieved after approximately 5-7 days. |
| Protein binding | Approximately 94-97% bound primarily to albumin and sex hormone-binding globulin (SHBG). |
| Volume of Distribution | Approximately 0.5-0.7 L/kg, indicating moderate distribution into tissues, including muscle and liver. |
| Bioavailability | Oral: 60-70% due to first-pass metabolism. Intramuscular: 90-95% if available; not currently marketed. |
| Onset of Action | Oral: 2-4 hours after a single dose. Intramuscular: 30-60 minutes if available. Intravenous: Not applicable as no IV formulation exists. |
| Duration of Action | Oral: 24-36 hours. Clinical note: Therapeutic effects on nitrogen retention and erythropoiesis persist beyond plasma levels due to active metabolite activity. |
100 mg orally twice daily or 200 mg orally once daily; immediate-release formulation.
| Dosage form | TABLET |
| Renal impairment | GFR >=50 mL/min: no adjustment; GFR 30-49 mL/min: 50% of standard dose; GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50% of standard dose; Child-Pugh C: contraindicated. |
| Pediatric use | Weight <20 kg: 2.5 mg/kg/day divided into 2 doses; 20-40 kg: 5 mg/kg/day divided into 2 doses; >40 kg: 10 mg/kg/day divided into 2 doses. Maximum single dose 200 mg. |
| Geriatric use | Initiate at 50% of standard dose (50 mg twice daily) with gradual titration based on tolerability and renal function. Maximum dose 200 mg daily. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for STANOZIDE (STANOZIDE).
| Breastfeeding | Stanozolol is excreted in breast milk; M/P ratio not established. Use is contraindicated due to potential androgenic effects in the nursing infant, including virilization and growth disturbances. |
| Teratogenic Risk | Stanozolol is contraindicated in pregnancy. First trimester: High risk of virilization of female fetus, including clitoromegaly, labial fusion, and urogenital sinus abnormalities. Second and third trimesters: Continued risk of virilization, growth retardation, and potential for premature closure of epiphyseal plates. |
■ FDA Black Box Warning
Peliosis hepatis, hepatic neoplasms, and hepatocellular carcinoma; contraindicated in pregnancy (virilization of female fetus).
| Serious Effects |
Pregnancy, breastfeeding, known or suspected prostate cancer, male breast cancer, severe hepatic dysfunction, hypercalcemia.
| Precautions | Hepatotoxicity, hypercalcemia, hyperlipidemia, prostatic hypertrophy, glucose intolerance, fluid retention, and increased risk of cardiovascular events. |
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| Fetal Monitoring |
| Monitor maternal liver function tests, lipid profile, glucose levels. In fetus, ultrasound for growth parameters and signs of virilization. Avoid use during pregnancy; if accidental exposure occurs, monitor fetal development closely. |
| Fertility Effects | Stanozolol may impair fertility in both males and females. In males: oligospermia, azoospermia, decreased libido. In females: menstrual irregularities, anovulation, and potential for irreversible virilization. Use should be avoided in individuals planning pregnancy. |