Yes

Androgen

Androgen replacement therapy in the treatment of delayed male puberty; postpartum breast pain and engorgement; inoperable breast cancer; male hypogonadism

C-III

X

Severe renal or cardiac disease, benign prostatic hypertrophy with obstruction, undiagnosed genital bleeding, males with carcinoma of the breast or prostate; hypersensitivity to testosterone or any component; pregnancy

Perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation. May accelerate bone maturation without producing compensating gain in linear growth. Has both androgenic and anabolic activity, the anabolic action may enhance hypoglycemia. Prolonged use has been associated with serious hepatic effects (hepatitis, hepatic neoplasms, cholestatic hepatitis, jaundice). May potentiate sleep apnea in some male patients (obesity or chronic lung disease) or exacerbate heart failure due to fluid retention.

>10%:

Dermatologic: Acne

Endocrine & metabolic: Menstrual problems (amenorrhea), virilism, breast soreness

Genitourinary: Epididymitis, priapism, bladder irritability

1% to 10%:

Cardiovascular: Flushing, edema

Central nervous system: Excitation, aggressive behavior, sleeplessness, anxiety, mental depression, headache

Dermatologic: Hirsutism (increase in pubic hair growth)

Gastrointestinal: Nausea, vomiting, GI irritation

Genitourinary: Prostatic hypertrophy, prostatic carcinoma, impotence, testicular atrophy

Hepatic: Hepatic dysfunction

<1%: Cholestatic hepatitis, gynecomastia, hepatic necrosis, hypercalcemia, hypersensitivity reactions, hypoglycemia, leukopenia, polycythemia, suppression of clotting factors

CYP3A3/4 and 3A5-7 enzyme substrate

Principal endogenous androgen responsible for promoting the growth and development of the male sex organs and maintaining secondary sex characteristics in androgen-deficient males

Duration of effect: Based upon the route of administration and which testosterone ester is used; the cypionate and enanthate esters have the longest duration, up to 2-4 weeks after I.M. administration

Distribution: Crosses the placenta; appears in breast milk

Protein binding: 98% (to transcortin and albumin)

Metabolism: In the liver

Half-life: 10-100 minutes

Elimination: In urine (90%) and feces via bile (6%)

Children: I.M.:

Male hypogonadism:

Initiation of pubertal growth: 40-50 mg/m²/dose (cypionate or enanthate ester) monthly until the growth rate falls to prepubertal levels

Terminal growth phase: 100 mg/m²/dose (cypionate or enanthate ester) monthly until growth ceases

Maintenance virilizing dose: 100 mg/m²/dose (cypionate or enanthate ester) twice monthly

Delayed puberty: 40-50 mg/m²/dose monthly (cypionate or enanthate ester) for 6 months

Adults: Inoperable breast cancer: I.M.: 200-400 mg every 2-4 weeks

Male: Short-acting formulations: Testosterone Aqueous/Testosterone Propionate (in oil): I.M.:

Androgen replacement therapy: 10-50 mg 2-3 times/week

Male hypogonadism: 40-50 mg/m²/dose monthly until the growth rate falls to prepubertal levels (~5 cm/year); during terminal growth phase: 100 mg/m²/dose monthly until growth ceases; maintenance virilizing dose: 100 mg/m²/dose twice monthly or 50-400 mg/dose every 2-4 weeks

Male: Long-acting formulations: Testosterone enanthate (in oil)/testosterone cypionate (in oil): I.M.:

Male hypogonadism: 50-400 mg every 2-4 weeks

Male with delayed puberty: 50-200 mg every 2-4 weeks for a limited duration

Male greater than or equal to 18 years: Transdermal: Primary hypogonadism or hypogonadotropic hypogonadism:

Testoderm®: Apply 6 mg patch daily to scrotum (if scrotum is inadequate, use a 4 mg daily system)

Testoderm-TSS®: Apply 5 mg patch daily to clean, dry area of skin on the arm, back or upper buttocks. Do not apply Testoderm-TSS® to the scrotum

Androderm®: Apply 2 systems nightly to clean, dry area on the back, abdomen, upper arms or thighs for 24 hours for a total of 5 mg/day

AndroGel®: Males >18 years of age: 5 g (to deliver 50 mg of testosterone) applied once daily (preferably in the morning) to clean, dry, intact skin of the shoulder and upper arms and/or abdomen. Upon opening the packet(s), the entire contents should be squeezed into the palm of the hand and immediately applied to the application site(s). Application sites should be allowed to dry for a few minutes prior to dressing. Hands should be washed with soap and water after application. Do not apply AndroGel® to the genitals

Dosing adjustment/comments in hepatic disease: Reduce dose

Periodic liver function tests, radiologic examination of wrist and hand every 6 months (when using in prepubertal children)

Testosterone, urine: Male: 100-1500 ng/24 hours; Female: 100-500 ng/24 hours

May cause a decrease in creatinine and creatine excretion and an increase in the excretion of 17-ketosteroids, thyroid function tests

May cause anxiety, insomnia, aggressive behavior, or depression

May rarely cause neutropenia; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Diabetics should monitor serum glucose closely and notify prescriber of changes; this medication may alter hypoglycemic requirements. You may experience acne, growth of body hair, loss of libido, impotence, or menstrual irregularity (usually reversible); nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report changes in menstrual pattern; enlarged or painful breasts; deepening of voice or unusual growth of body hair; persistent penile erection; fluid retention (swelling of ankles, feet, or hands, difficulty breathing or sudden weight gain); unresolved changes in CNS (nervousness, chills, insomnia, depression, aggressiveness); altered urinary patterns; change in color of urine or stool; yellowing of eyes or skin; unusual bruising or bleeding; or other persistent adverse reactions.

Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Male: Do not cause a female to become pregnant. Male/female: Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Warm injection to room temperature and shaking vial will help redissolve crystals that have formed after storage; administer by deep I.M. injection into the upper outer quadrant of the gluteus maximus. Transdermal system should be applied on clean, dry, scrotal skin. Dry-shave scrotal hair for optimal skin contact. Do not use chemical depilatories.

Injection:

Aqueous suspension: 25 mg/mL (10 mL, 30 mL); 50 mg/mL (10 mL, 30 mL); 100 mg/mL (10 mL, 30 mL)

In oil, as cypionate: 100 mg/mL (1 mL, 10 mL); 200 mg/mL (1 mL, 10 mL)

In oil, as enanthate: 100 mg/mL (1 mL, 5 mL, 10 mL); 200 mg/mL (1 mL, 5 mL, 10 mL)

In oil, as propionate: 100 mg/mL (10 mL, 30 mL)

Pellet: 75 mg (1 pellet per vial)

Transdermal system:

Androderm®: 2.5 mg/day; 5 mg/day

Testoderm®: 4 mg/day; 6 mg/day

Testoderm-TTS®: 5 mg/day

Transdermal gel: AndroGel®: 1%: 50 mg (5 g gel); 75 mg (7.5 g gel)

Borhan-Manesh F and Farnum JB, "Methyltestosterone-Induced Cholestasis. The Importance of Disproportionately Low Serum Alkaline Phosphatase Level," Arch Intern Med, 1989, 149(9):2127-9.

Cunningham GR, Cordero E, and Thornby JI, "Testosterone Replacement With Transdermal Therapeutic Systems. Physiological Serum Testosterone and Elevated Dihydrotestosterone Levels," JAMA, 1989, 261(17):2525-30.

Daigle RD, "Anabolic Steroids," J Psychoactive Drugs, 1990, 22(1):77-80.

Moller BB and Ekelund B, "Toxicity of Cyclosporine During Treatment With Androgens," N Engl J Med, 1985, 313(22):1416.

Ruch W and Jenny P, "Priapism Following Testosterone Administration for Delayed Male Puberty," Am J Med, 1989, 86(2):256.