tess-TOSS-te-rone en-AN-thate

Therapeutic Classification: hormones

Pharmacologic Classification: androgens

• Hypogonadism in men witb low serum testosterone concentrations.
• Delayed puberty in men.
• Androgen-responsive breast cancer in postmenopausal women (palliative).

Unlabeled Use:

• Masculinizing hormone therapy for transgender men (female-to-male)

• 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:
  • Initiation of male puberty.
• Suppression of tumor growth in some forms of breast cancer.

Absorption: Well absorbed following IM and subcut administration; absorbed slowly.

Distribution: Crosses the placenta.

Protein Binding: 98%.

Metabolism/Excretion: Metabolized by the liver; 90% eliminated in urine as metabolites.

Half-life: IM — 10–100 min; subcut — Unknown.

(androgenic effects†)

†Response is highly variable among individuals; may take mo.

Contraindicated in:

• Hypersensitivity
• Men with breast or prostate cancer
• OB: Pregnancy (may cause fetal virilization)
• Lactation: Lactation.

Use Cautiously in:

• Hypercalcemia
• Coronary artery disease
• Hypertension
• Benign prostatic hyperplasia
• Obesity or chronic lung disease (↑ risk of sleep apnea)
• Polycythemia
• Prepubertal males
• Geri: ↑risk of prostatic hyperplasia/carcinoma in older adults.

CV: MI, STROKE, VENOUS THROMBOEMBOLISM, edema, ↑ blood pressure.

Derm: male pattern baldness.

EENT: deepening of voice.

Endo: hypercholesterolemia.
women-: hirsutism.
men-: gynecomastia.

F and E: hypercalcemia, hyperkalemia, hyperphosphatemia.

GI: HEPATOTOXICITY, nausea, vomiting.

GU: women-: change in libido, clitoral enlargement, menstrual irregularities.
men-: erectile dysfunction, priapism, ↓ sperm count, prostatic enlargement.

Hemat: ↑hematocrit.

Local: pain at injection site.

Neuro: SUICIDAL THOUGHTS/BEHAVIOR, depression.

Resp: sleep apnea.

Drug-Drug:

• May ↑ action of warfarin, oral hypoglycemic agents, andinsulin.
• Concurrent use with corticosteroids may ↑ risk of edema formation.

Male Hypogonadism (replacement therapy)

• IM (Adults): 50–400 mg every 2–4 wk.
• SC (Adults): 75 mg once weekly.

Delayed Male Puberty

• IM (Children): 50–200 mg every 2–4 wk for up to 6 mo.

Palliative Management of Breast Cancer (in postmenopausal women)

• IM (Adults): 200–400 mg every 2–4 wk.

Masculinizing Hormone Therapy for Transgender Men (Female-to-Male) (off-label)

• IM (Adults): 100–200 mg every 2 wk or 50–100 mg once weekly.
• SC (Adults): 50–100 mg once weekly.

(Generic available)

• Solution for intramuscular injection (in oil): 200 mg/mL;
• Solution for subcutaneous injection (autoinjector): 50 mg/0.5 mL; 75 mg/0.5 mL; 100 mg/0.5 mL;

• Monitor intake and output ratios, weigh patient twice weekly, and assess patient for edema. Report significant changes indicative of fluid retention.
• Assess BP before and 6 wks after starting therapy. May cause increased BP.
• 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.
• Men: 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). Bone age determinations should be measured 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.
• Women: Assess for virilism (deepening of voice, unusual hair growth, clitoral enlargement, acne, menstrual irregularities).
  • In women with metastatic breast cancer, monitor for symptoms of hypercalcemia (nausea, vomiting, constipation, lethargy, loss of muscle tone, thirst, polyuria).

• Prior to therapy, measure serum testosterone in the morning on at least two separate days. Normal range (300–1050 ng/dL). Monitor serum testosterone concentrations 4–12 wk after starting therapy. Discontinue therapy is concentrations are consistently outside of normal range.
  • Subcut: Measure total testosterone trough concentrations (measured 7 days after most recent dose) following 6 wks of therapy, following 6 wks after dose adjustment, and periodically during therapy. Trough concentration of 350–650 ng/dL is in normal range. If total testosterone trough concentration (Ctrough) is 650 ng/dL, ↓ dose by 25 mg. If total testosterone Ctrough is <350 ng/dL, ↑ dose by 25 mg. Maintain same dose if total testosterone Ctrough is 350 ng/dL and <650 ng/dL.
  • 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 serum and urine calcium levels and serum alkaline phosphatase concentrations in women with metastatic breast cancer.
  • 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 rotating the vial between the palms of hands will redissolve crystals. Use of a wet syringe or needle may cause solution to become cloudy but will not affect its potency.
• SC: Inject only into abdominal region. Solution is clear and colorless to pale yellow; do not administer solutions that are cloudy, discolored or contain particulate matter.

• 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 patient to report the following signs and symptoms promptly: in male patients, priapism (sustained and often painful erections), difficulty urinating, or gynecomastia; in female patients, virilism (which may be reversible if medication is stopped as soon as changes are noticed), or hypercalcemia (nausea, vomiting, constipation, and weakness); in male or female patients, edema (unexpected weight gain, swelling of feet), hepatitis (yellowing of skin or eyes and abdominal pain), or unusual bleeding or bruising.
  • Advise patients with diabetes to monitor blood closely for alterations in blood glucose concentrations.
  • Radiologic bone age determinations should be evaluated every 6 mo in prepubertal children to determine rate of bone maturation and effects on epiphyseal centers.
  • Rep: May be teratogenic. Instruct females of reproductive potential to notify health care professional immediately if pregnancy is planned or suspected or if breastfeeding. May irreversibly impair fertility.
  • Emphasize the importance of regular follow-up physical exams, lab tests, and x-ray exams to monitor progress.

• 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.
• Decrease in the size and spread of breast malignancy in postmenopausal women. In antineoplastic therapy, response may require 3 mo of therapy; if signs of disease progression appear, therapy should be discontinued.

Delatestryl, Xyosted

Schedule III (C-III)

• Sexual dysfunction (Indications, Side Effects).

NDC Code^*

• 0143- West-Ward Pharmaceuticals Corp
  • 0143-9750- TESTOSTERONE ENANTHATE
    • 0143-9750-01- 5 mL in 1 VIAL, MULTI-DOSE (0143-9750-01)

• 0591- Actavis Pharma, Inc.
  • 0591-3221- Testosterone Enanthate
    • 0591-3221-26- 1 VIAL, MULTI-DOSE in 1 CARTON (0591-3221-26) > 5 mL in 1 VIAL, MULTI-DOSE

• 54436- Antares Pharma, Inc.
  • 54436-200- XYOSTED
    • 54436-200-01- 1 SYRINGE in 1 CARTON (54436-200-01) >.5 mL in 1 SYRINGE (54436-200-03)

• 54436- Antares Pharma, Inc.
  • 54436-200- XYOSTED
    • 54436-200-04- 4 SYRINGE in 1 CARTON (54436-200-04) >.5 mL in 1 SYRINGE (54436-200-02)

• 54436- Antares Pharma, Inc.
  • 54436-250- XYOSTED
    • 54436-250-01- 1 SYRINGE in 1 CARTON (54436-250-01) >.5 mL in 1 SYRINGE (54436-250-03)

• 54436- Antares Pharma, Inc.
  • 54436-250- XYOSTED
    • 54436-250-04- 4 SYRINGE in 1 CARTON (54436-250-04) >.5 mL in 1 SYRINGE (54436-250-02)

• 54436- Antares Pharma, Inc.
  • 54436-275- XYOSTED
    • 54436-275-01- 1 SYRINGE in 1 CARTON (54436-275-01) >.5 mL in 1 SYRINGE (54436-275-03)

• 54436- Antares Pharma, Inc.
  • 54436-275- XYOSTED
    • 54436-275-04- 4 SYRINGE in 1 CARTON (54436-275-04) >.5 mL in 1 SYRINGE (54436-275-02)