Controlled Substance Schedule: III
Hypogonadism in men with low serum testosterone concentrations.
- Responsible for the normal growth and development of male sex organs.
Maintenance of male secondary sex characteristics:
- Growth and maturation of the prostate, seminal vesicles, penis, scrotum,
- Development of male hair distribution,
- Vocal cord thickening,
- Alterations in body musculature and fat distribution.
Correction of hormone deficiency in male hypogonadism.
Absorption: Well absorbed from IM sites; absorbed slowly.
Distribution: Crosses the placenta.
Protein Binding: 98%.
Metabolism and Excretion: Metabolized by the liver; 90% eliminated in urine as metabolites.
Half-life: 8 days.
TIME/ACTION PROFILE (androgenic effects†)
- OB: Lactation: Pregnancy and lactation
- Male patients with breast or prostate cancer
- Severe liver, renal, or cardiac disease
- Patients with known hypersensitivity to benzyl alcohol.
Use Cautiously in:
- Benign prostatic hyperplasia
- Geriatric patients (↑ risk of prostatic hyperplasia/carcinoma)
- Males <12 yr (safety and effectiveness not established).
Adverse Reactions/Side Effects
EENT: deepening of voice
CV: MI, STROKE, VENOUS THROMBOEMBOLISM, edema
GI: cholestatic jaundice, drug-induced hepatitis, liver function test elevation, nausea, vomiting
GU: change in libido, erectile dysfunction, priapism, prostatic enlargement
Endo: gynecomastia, hirsutism, oligospermia, hypercholesterolemia
F and E: hypercalcemia, hyperkalemia, hyperphosphatemia
Derm: male pattern baldness
Local: pain at injection site
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
IM (Adults): Replacement therapy –50–400 mg every 2–4 wk.
Availability (generic available)
Solution for intramuscular injection (in oil): 100 mg/mL, 200 mg/mL
- Monitor intake and output ratios, weigh patient twice weekly, and assess patient for edema. Report significant changes indicative of fluid retention.
- Assess for abuse using higher doses than prescribed and usually in conjunction with other anabolic androgenic steroids. May result in heart attack, heart failure, stroke, depression, hostility, aggression, liver toxicity, and infertility. Measure serum testosterone if abuse is suspected.
Monitor for precocious puberty in boys (acne, darkening of skin, development of male secondary sex characteristics–increase in penis size, frequent erections, growth of body hair). Measure bone age determinations every 6 mo to determine rate of bone maturation and effects on epiphyseal closure.
- Monitor for breast enlargement, persistent erections, and increased urge to urinate in men. Monitor for difficulty urinating in elderly men, because prostate enlargement may occur.
Lab Test Considerations:
Prior to therapy, confirm diagnosis of hypogonadism by measuring serum testosterone in the morning on at least two separate days and these serum testosterone concentrations are below the normal range (300 to 1050 ng/dL). Monitor serum testosterone concentrations 4–12 wk after starting therapy. Discontinue therapy is concentrations are consistently outside of normal range.
- Monitor hemoglobin and hematocrit periodically during therapy; may cause polycythemia.
- Monitor hepatic function tests and serum cholesterol levels periodically during therapy. May ↑ serum AST, ALT, and bilirubin, ↑ cholesterol levels, and suppress clotting factors II, V, VII, and X.
- Monitor blood glucose closely in patients with diabetes who are receiving oral hypoglycemic agents or insulin.
- Monitor serum sodium, chloride, potassium, and phosphate concentrations (may be ↑).
- Range-of-motion exercises should be done with all bedridden patients to prevent mobilization of calcium from the bone.
- IM Administer IM deep into gluteal muscle. Crystals may form when vials are stored at low temperatures; warming and shaking the vial will redissolve crystals. Use of a wet syringe or needle may cause solution to become cloudy but will not affect its potency.
Advise patient to report the following signs and symptoms promptly: priapism (sustained and often painful erections), difficulty urinating, gynecomastia, edema (unexpected weight gain, swelling of feet), hepatitis (yellowing of skin or eyes and abdominal pain), or unusual bleeding or bruising.
- Instruct patient to use testosterone as directed. Do not use higher than prescribed doses. Explain rationale for prohibiting use of testosterone for increasing athletic performance. Testosterone is neither safe nor effective for this use and has a potential risk of serious side effects.
- Advise diabetic patients to monitor blood closely for alterations in blood glucose concentrations.
- Emphasize the importance of regular follow-up physical exams, lab tests, and x-ray exams to monitor progress.
- Radiologic bone age determinations should be evaluated every 6 mo in prepubertal children to determine rate of bone maturation and effects on epiphyseal centers.
Resolution of the signs of androgen deficiency without side effects. Therapy is usually limited to 3–6 mo followed by bone growth or maturation determinations.
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