testosterone Pharmacologic classification: androgen
Depo-Testosterone, Virilon IM
Delatestryl, Everone 200
Therapeutic classification: androgen replacement, antineoplastic
Pregnancy risk category X
Controlled substance schedule III
Available by prescription only
Injection (aqueous suspension): 25 mg/ml, 50 mg/ml, 100 mg/ml
Pellets for S.C. implantation: 75 mg
testosterone cypionate (in oil)
Injection: 100 mg/ml, 200 mg/ml
testosterone enanthate (in oil)
Injection: 100 mg/ml, 200 mg/ml
testosterone propionate (in oil)
Injection: 100 mg/ml
Indications and dosages
Male hypogonadism. testosterone or testosterone propionate. Adults: 10 to 25 mg I.M. two or three times weekly.
testosterone cypionate or enanthate
Adults: 50 to 400 mg I.M. q 2 to 4 weeks.
Delayed puberty in males. testosterone or testosterone propionate. Boys: 25 to 50 mg I.M. two or three times weekly for up to 4 to 6 months.
testosterone cypionate or enanthate Boys: 50 to 200 mg I.M. q 2 to 4 weeks for up to 6 months.
Postpartum breast pain and engorgement. testosterone or testosterone propionate. Women: 25 to 50 mg I.M. daily for 3 to 4 days.
Inoperable breast cancer. testosterone propionate. Women: 50 to 100 mg I.M. three times weekly.
testosterone cypionate or enanthate Adults: 200 to 400 mg I.M. q 2 to 4 weeks.
testosterone Adults: 100 mg I.M. three times weekly.
Postpubertal cryptorchidism. testosterone or testosterone propionate. Men: 10 to 25 mg I.M. two or three times weekly.
Growth stimulation in Turner’s syndrome. testosterone propionate. Adults: 40 to 50 mg/m2 I.M. once monthly for 6 months.
Androgenic action: Testosterone is the endogenous androgen that stimulates receptors in androgen-responsive organs and tissues to promote growth
and development of male sexual organs and secondary sexual characteristics.
Antineoplastic action: Testosterone exerts inhibitory, antiestrogenic effects on hormone-responsive breast tumors and metastases.
Absorption: Testosterone and its esters must be administered parenterally because they’re inactivated rapidly by the liver when given
orally. The onset of action of cypionate and enanthate esters of testosterone is somewhat slower than that of testosterone
Distribution: 98% to 99% plasma protein-bound, primarily to the testosterone-estradiol binding globulin.
Metabolism: Metabolized to several 17-ketosteroids by two main pathways in the liver. A large portion of these metabolites then form
glucuronide and sulfate conjugates. Plasma half-life of testosterone ranges from 10 to 100 minutes. The cypionate and enanthate
esters of testosterone have longer durations of action than testosterone. Cypionate half-life is about 8 days.
Excretion: Very little unchanged testosterone appears in urine or feces. About 90% of metabolized testosterone is excreted in urine
in the form of sulfate and glucuronide conjugates.
Contraindications and precautions
Contraindicated in men with breast or prostate cancer; in patients with hypercalcemia or cardiac, hepatic, or renal decompensation;
in pregnant women; and in breast-feeding women. Also contraindicated in patients hypersensitive to the drug and sensitive
or allergic to mercury compounds (histerone).
Use cautiously in elderly patients and in women of childbearing age.
Drug-drug. Hepatotoxic drugs: Increases risk of hepatotoxicity. Monitor patient closely.
Insulin, oral antidiabetics: Decreases serum glucose levels; alters glucose levels in diabetic patients. Monitor patient closely. Dosage may need adjustment.
Oral anticoagulants: Prolongs PT and INR. Monitor patient closely.
Oxyphenbutazone: May increase serum oxyphenbutazone levels. Monitor patient closely.
CNS: headache, anxiety, depression, paresthesia, sleep apnea syndrome.
Hematologic: polycythemia, suppression of clotting factors.
Hepatic: reversible jaundice, cholestatic hepatitis.
Metabolic: hypercalcemia, hypernatremia, hyperkalemia, hyperphosphatemia.
Skin: pain and induration at injection site, local edema, hypersensitivity reactions.
Other: hypoestrogenic effects in women (flushing; diaphoresis; vaginitis, including itching, drying, and burning; vaginal bleeding;
menstrual irregularities), androgenic effects in women (acne, edema, oily skin, weight gain, hirsutism, hoarseness, clitoral enlargement, deepening voice, decreased or increased libido), excessive hormonal effects in men (prepubertal-premature
epiphyseal closure, acne, priapism, growth of body and facial hair, phallic enlargement; postpubertal-testicular atrophy, oligospermia, decreased ejaculatory volume, impotence, gynecomastia,
Effects on lab test results
May increase sodium, potassium, phosphate, cholesterol, liver enzyme, calcium, and creatinine levels. May decrease thyroxine-binding
globulin and total T4 levels.
May increase PT and INR, resin uptake of T3 and T4, and RBC count. May increase or decrease glucose tolerance test results.
Overdose and treatment
When used to treat male hypogonadism, start therapy with full therapeutic doses and taper according to patient tolerance and
response. Administering long-acting esters (enanthate or cypionate) at intervals greater than every 2 to 3 weeks may cause
hormone levels to fall below those found in normal adults.
Testosterone enanthate has been used for postmenopausal osteoporosis and to stimulate erythropoiesis.
ALERT Carefully observe women for signs of excessive virilization. If possible, stop therapy at first sign of virilization because
some adverse effects, such as deepening of voice and clitoral enlargement, are irreversible.
ALERT Patients with metastatic breast cancer should have regular determinations of serum calcium levels to avoid serious hypercalcemia.
Drug isn’t indicated for use during pregnancy.
It isn’t known whether drug appears in breast milk. An alternative to breast-feeding is recommended because of potential for
severe adverse effects of androgens on the infant.
Use with extreme caution in children to avoid precocious puberty and premature closure of the epiphyses. Obtain X-ray examinations
every 6 months to assess skeletal maturation.
Observe elderly men for prostatic hyperplasia. Development of symptomatic prostatic hyperplasia or prostatic carcinoma mandates
discontinuation of the drug.
Explain to women that virilization may occur, and advise them to report androgenic effects immediately. Stopping drug prevents
further androgenic changes but probably won’t reverse those already present.
Tell women to report menstrual irregularities; drug may be discontinued pending determination of the cause.
Inform men to report too frequent or persistent penile erections.
Advise patient to report persistent GI distress, diarrhea, or the onset of jaundice.
Reactions may be common, uncommon, life-threatening, or
COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use