Pronunciation:

(tes TOS ter one)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Injection: Androgen replacement therapy in the treatment of delayed male puberty; male hypogonadism (primary or hypogonadotropic); inoperable female breast cancer (enanthate only)

Pellet: Androgen replacement therapy in the treatment of delayed male puberty; male hypogonadism (primary or hypogonadotropic)

Buccal, topical: Male hypogonadism (primary or hypogonadotropic)

Restrictions:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

Cardiovascular: Flushing, edema, hypertension, vasodilation

Central nervous system: Aggressive behavior, amnesia, anxiety, dizziness, emotional lability, excitation, headache, mental depression, nervousness, sleeplessness

Dermatologic: Acne, allergic contact dermatitis (transdermal 4%), alopecia, burn-like blisters (transdermal 12%), dry skin, erythema (transdermal 7%), hirsutism (increase in pubic hair growth), pruritus

Endocrine & metabolic: Breast soreness, gynecomastia, hypercalcemia, hypoglycemia, menstrual problems (amenorrhea), virilism

Gastrointestinal: GI irritation, nausea, vomiting

Following buccal administration: Bitter taste, gum edema, gum or mouth irritation, gum tenderness, taste perversion

Genitourinary: Bladder irritability, epididymitis, impotence, priapism, prostatic carcinoma, prostatic hyperplasia, testicular atrophy, urination impaired

Hepatic: Cholestatic hepatitis, hepatic dysfunction, hepatic necrosis

Hematologic: Leukopenia, polycythemia, suppression of clotting factors

Neuromuscular & skeletal: Paresthesias, weakness

Miscellaneous: Diaphoresis, hypersensitivity reactions

Drug Interactions:

Increased toxicity: Effects of oral anticoagulants may be enhanced

Ethanol/Nutrition/Herb Interactions:

Stability:

Androderm®: Store at room temperature; do not store outside of pouch. Excessive heat may cause system to burst.

Androgel®, Delatestryl®, Striant™, Testim™: Store at room temperature.

Depo® Testosterone: Store at room temperature; protect from light.

Testopel®: Store in a cool location.

Mechanism of Action:

Pharmacodynamics/Kinetics:

Duration (route and ester dependent): I.M.: Cypionate and enanthate esters have longest duration, 2-4 weeks

Absorption: Transdermal gel: ~10% of dose

Distribution: Crosses placenta; enters breast milk

Protein binding: 98% bound to sex hormone-binding globulin (40%) and albumin

Metabolism: Hepatic; forms metabolites

Half-life elimination: 10-100 minutes

Excretion: Urine (90%); feces (6%)

Dosage:

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

Adolescents and Adults: Pellet (for subcutaneous implantation): Delayed male puberty, male hypogonadism: 150-450 mg every 3-6 months

Adults:

I.M.:

Female: Inoperable breast cancer: Testosterone enanthate: 200-400 mg every 2-4 weeks

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

Hypogonadism: 50-400 mg every 2-4 weeks

Delayed puberty: 50-200 mg every 2-4 weeks for a limited duration

Transdermal: Primary male hypogonadism or hypogonadotropic hypogonadism:

Androderm®: Initial: Apply 5 mg/day once nightly to clean, dry area on the back, abdomen, upper arms, or thighs (do not apply to scrotum); dosing range: 2.5-7.5 mg/day; in nonvirilized patients, dose may be initiated at 2.5 mg/day

AndroGel®, Testim™: 5 g (to deliver 50 mg of testosterone with 5 mg systemically absorbed) applied once daily (preferably in the morning) to clean, dry, intact skin of the shoulder and upper arms. AndroGel® may also be applied to the abdomen. Dosage may be increased to a maximum of 10 g (100 mg). Do not apply testosterone gel to the genitals.

Oral (buccal): Hypogonadism or hypogonadotropic hypogonadism: 30 mg twice daily (every 12 hours) applied to the gum region above the incisor tooth

Dosing adjustment/comments in hepatic disease: Reduce dose

Administration:

I.M.: Warm to room temperature; 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.

Oral: Striant™: One mucoadhesive for buccal application (buccal system) should be applied to a comfortable area above the incisor tooth. Apply flat side of system to gum. Rotate to alternate sides of mouth with each application. Hold buccal system firmly in place for 30 seconds to ensure adhesion. The buccal system should adhere to gum for 12 hours. If the buccal system falls out, replace with a new system. If the system falls out within 4 hours of next dose, the new buccal system should remain in place until the time of the following scheduled dose. System will soften and mold to shape of gum as it absorbs moisture from mouth. Do not chew or swallow the buccal system. The buccal system will not dissolve; gently remove by sliding downwards from gum; avoid scratching gum.

Transdermal (Androderm®): Apply patch to clean, dry area of skin on the arm, back, or upper buttocks. Following patch removal, mild skin irritation may be treated with OTC hydrocortisone cream. A small amount of triamcinolone acetonide 0.1% cream may be applied under the system to decrease irritation; do not use ointment. Patch should be applied nightly. Rotate administration sites, allowing 7 days between applying to the same site.

Gel: AndroGel®, Testim™: Apply (preferably in the morning) to clean, dry, intact skin of the shoulder and upper arms (AndroGel® may also be applied to the 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). Alternatively, a portion may be squeezed onto palm of hand and applied, repeating the process until entire packet has been applied. 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 testosterone gel to the genitals.

Monitoring Parameters:

Androderm®: Morning serum testosterone levels following application the previous evening

Gel: Morning serum testosterone levels 14 days after start of therapy

Reference Range:

Test Interactions:

Dietary Considerations:

Patient Education:

Transdermal:

Androderm®: Apply patch to clean, dry area of skin on the arm, back, or upper buttocks.

AndroGel®, Testim™: Apply gel (preferably in the morning) to clean, dry, intact skin of the shoulder and upper arms (AndroGel® may also be applied to the 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). Alternatively, a portion may be squeezed onto palm of hand and applied, repeating the process until entire packet has been applied. 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 testosterone gel to the genitals.

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 contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Gel, topical:

AndroGel®:

25 mg/2.5 g (30s); 50 mg/5 g (30s) [1% unit-dose packet]

1.25 g/dose (75 g) [1% metered-dose pump; provides 60 doses]

Testim™: 50 mg/5 g (30s) [1% unit-dose tube]

Injection, in oil, as cypionate (Depo® Testosterone): 100 mg/mL (10 mL); 200 mg/mL (1 mL, 10 mL) [contains benzyl alcohol, benzyl benzoate, and cottonseed oil]

Injection, in oil, as enanthate (Delatestryl®): 200 mg/mL (1 mL [prefilled syringe; contains sesame oil]; 5 mL [multidose vial; contains sesame oil])

Mucoadhesive, for buccal application [buccal system] (Striant™): 30 mg

Pellet, for subcutaneous implantation (Testopel®): 75 mg (1 pellet/vial)

Transdermal system (Androderm®): 2.5 mg/day (60s); 5 mg/day (30s)

International Brand Names: