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Uses

Male Hypogonadism

Management of congenital or acquired primary hypogonadism such as that resulting from orchidectomy or from testicular failure caused by cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, Klinefelter's syndrome, chemotherapy, or toxic damage from alcohol or heavy metals.

Management of congenital or acquired hypogonadotropic hypogonadism such as that resulting from idiopathic gonadotropin or gonadotropin-releasing hormone (luteinizing hormone-releasing hormone) deficiency or from pituitary-hypothalamic injury caused by tumors, trauma, or radiation. Should be used in the treatment of hypogonadotropic hypogonadism only in patients uninterested in or unable to achieve fertility.

Considered the androgen of choice for the treatment of androgen deficiency (e.g., hypogonadism) and AIDS wasting in HIV-infected men.

May be used to stimulate puberty when the diagnosis is well established in carefully selected males with delayed puberty (designated an orphan drug by FDA for this use).

Some experts (e.g., American College of Rheumatology) recommend that men who develop low serum testosterone concentrations (<300 ng/mL) while receiving long-term corticosteroid therapy receive testosterone replacement therapy in an attempt to treat hypogonadism and possibly reduce the risk of corticosteroid-induced osteoporosis†.

Clinical evidence to date regarding testosterone therapy in aging men suggests some beneficial effects (e.g., on body composition, strength, bone density, frailty, cognitive function, mood, sexual function, quality of life), but risks relating to benign prostatic hyperplasia and prostate cancer need to be quantified. The Institute of Medicine states that the nature and extent of therapeutic benefits in older men require additional study.

Not indicated for the treatment of erectile dysfunction† in men with normal testosterone concentrations.

Breast Cancer

Palliative treatment of androgen-responsive, advanced, inoperable, metastatic (skeletal) breast cancer in women who are 1–5 years postmenopausal and in premenopausal women who have benefited from oophorectomy.

Poorly tolerated (see Virilization under Cautions); other hormonal agents (e.g., tamoxifen, anastrozole, letrozole, exemestane) currently are preferred for this use.

Misuse and Abuse

Has been misused and abused by athletes, bodybuilders, weight lifters, and others to enhance athletic performance or physique†.

Medical and sports experts (e.g., International Olympic Committee) consider such use to be inappropriate and unacceptable because of known adverse effects and potential long-term sequelae and because such use by athletes is contrary to the rules and ethical principles of athletic competition.

Dosage and Administration

General

Male Hypogonadism

• Individualize dosage according to the condition being treated; the severity of symptoms; the patient’s age, gender, and history of prior androgenic therapy; and the specific testosterone preparation being used.
• Monitor every 3–4 months during the first year of testosterone replacement and periodically thereafter (e.g., every 4–6 months) for response and tolerance.

Delayed Puberty

• Prior to initiation of therapy, fully discuss the potential risk of therapy with the patient and his parents.
• Take into consideration the chronological and skeletal ages of the patient, both in determining the initial dosage and in adjusting the dosage.
• Perform radiographic examination of the hand and wrist at 6-month intervals to determine the rate of bone maturation and to assess the effect of therapy on the epiphyseal centers. (See Pediatric Use under Cautions.)

Breast Cancer

• Administer only under supervision of a qualified clinician experienced in the treatment of breast cancer.
• May occasionally appear to accelerate progression of the disease; monitor patients closely.
• Discontinue the drug if hypercalcemia occurs, since this may indicate progression of metastases to the bone.

Administration

Administer testosterone topically or intrabuccally.

Administer testosterone cypionate and testosterone enanthate by deep IM injection; not for IV administration.

IM Administration

Administer by deep IM injection into the upper outer quadrant of the gluteus maximus.

Topical Administration

Gel

AndroGel^®: Apply gel topically once daily, preferably in the morning, to clean, dry, intact skin on the shoulders and upper arms and/or abdomen. Do not apply to the genitals.

AndroGel^® unit-dose packet: Upon opening the unit-dose packet, squeeze the entire contents into the palm of the hand and immediately apply to the application site. Alternatively, squeeze a portion of the contents into the palm of the hand and immediately apply to application site; repeat procedure until entire contents of the packet has been applied.

AndroGel^® metered-dose pump: Collect gel in the palm of the hand by pressing the pump firmly and fully; apply to application site. This can be done one pump actuation at a time or after completion of all pump actuations needed for the daily dose. Alternatively, apply the gel directly to application site (direct application prevents loss of gel during transfer to hand). Prime pump by depressing 3 times before using the pump for the first dose; discard gel so that household members or pets are not exposed to the gel (i.e., rinse down sink).

Testim^®: Apply gel topically once daily, preferably in the morning, to clean, dry, intact skin on the shoulders and/or upper arms Do not apply to abdomen or genitals. Upon opening the unit-dose tube, squeeze the entire contents into the palm of the hand and immediately apply to the application site.

Wash hands with soap and water after application of the gel.

After the gel has dried, cover the site with clothing (e.g., a shirt) in order to prevent transfer to another individual.

Manufacturer of AndroGel^® recommends waiting ≥5–6 hours and the manufacturer of Testim^® recommends waiting ≥2 hours after application before showering or swimming. However, showering or swimming after the elapse of just 1 hour should have a minimal effect on the amount of testosterone gel absorbed if done very infrequently.

Transdermal System

Apply the transdermal system to clean, dry area of skin on the back, abdomen, upper arm, or thigh by firmly pressing the system with the adhesive side touching the skin. Do not apply to the scrotum or to oily, damaged, or irritated areas of the skin.

To avoid burn-like blisters, do not apply systems over bony prominences or on a part of the body that may be subject to prolonged pressure during sleep or sitting (e.g., the deltoid region of the upper arm, the greater trochanter of the femur, the ischial tuberosity).

Apply once daily at night (e.g., 10 p.m.). Leave transdermal system in place for 24 hours; after 24 hours, remove system and apply a new system. Apply system immediately after removal from its protective pouch and removal of the protective liner.

To minimize and/or prevent potential skin irritation, apply each transdermal system at a different site, with ≥1 week between applications to a particular site.

Mild skin irritation may be ameliorated with topical hydrocortisone 0.5 or 1% cream after system removal; alternatively, apply a small amount of triamcinolone acetonide 0.1% cream to the skin under the drug reservoir (do not use ointment formulations because they may reduce testosterone absorption).

Transdermal system does not need to be removed during sexual intercourse or while showering or bathing.

Intrabuccal Administration

Press the extended-release buccal (transmucosal) tablet against the gum above the upper left or right incisor twice daily (morning and evening) about 12 hours apart. These tablets will adhere to the gum and do not dissolve completely; do not chew or swallow. Dislodge and remove the tablet after 12 hours. Alternate application sites above the left and right upper incisors.

Consult manufacturer’s patient information for instructions on proper intrabuccal administration and removal of the tablet.

If the tablet fails to properly adhere to the gum or falls off within the first 8 hours, replace the old tablet with a new one. The new tablet may remain in place until the time of the next regularly scheduled dose (i.e., 12 hours after the original buccal tablet was administered). If the buccal tablet falls off after 8 hours but before 12 hours, replace the original tablet with one that can serve as the second dose for that day.

Dosage

Available as testosterone; dosage expressed in terms of testosterone. Also available as testosterone enanthante or testosterone cypionate; dosage expressed in terms of the salts.

AndroGel^® unit-dose packets contain 2.5 or 5 g of gel (25 or 50 mg of testosterone). Each depression of the metered-dose pump delivers 1.25 g of gel (12.5 mg of testosterone) after priming.

Testim^® unit-dose tubes contain 5 g of gel (50 mg of testosterone).

Pediatric Patients

Male Hypogonadism

Delayed Puberty

IM

Dosage regimens vary. Some clinicians recommend that lower dosages be used initially, followed by gradual increases in dosage as puberty progresses; subsequently, the dosage may be decreased to maintenance levels. Other clinicians state that higher dosages are required initially to induce pubertal changes and lower dosages can then be used for maintenance therapy after puberty.

Usual dosage of testosterone enanthate: 50–200 mg every 2–4 weeks for a limited period of time (e.g., 4–6 months).

Adults

Male Hypogonadism

IM

Usual dosage: 50–400 mg of testosterone cypionate or testosterone enanthate every 2–4 weeks.

Some clinicians recommend testosterone cypionate or testosterone enanthate dosage of 50–100 mg every 7–10 days or 100–150 mg every 2 weeks. While dosage of 300 mg every 3 weeks also may be considered for convenience, such dosing is associated with wider testosterone fluctuations and generally is inadequate to ensure a consistent clinical response. Serum total testosterone concentrations generally should exceed 250–300 ng/dL just before the next dose.

Adult males with prepubertal onset of hypogonadism who are going through puberty for the first time with testosterone replacement: Initially, 50 mg every 3–4 weeks; increase dosage gradually in subsequent months as tolerated up to full replacement within 1 year.

Attainment of full virilization may require up to 3–4 years of IM testosterone replacement.

Topical (Gel)

AndroGel^® and Testim^®: Apply 50 mg of testosterone (5 g of 1% gel) once daily, preferably in the morning; this dose delivers about 5 mg of testosterone systemically. Adjust dosage according to serum testosterone concentrations obtained approximately 14 days after initiating daily application of the gel.

AndroGel^®: If serum testosterone concentrations are below the normal range or the clinical response is inadequate, the dosage can be increased initially to 75 mg of testosterone (7.5 g of 1% gel) and, if necessary, subsequently to 100 mg of testosterone (10 g of 1% gel).

Testim^®: If serum testosterone concentrations are below the normal range or the clinical response is inadequate, the dosage can be increased to 100 mg of testosterone (10 g of 1% gel).

Topical (Transdermal System)

Usual initial dosage is 1 system delivering 5 mg/24 hours or 2 systems delivering 2.5 mg/24 hours applied to the skin nightly.

Adjust dosage according to morning serum testosterone concentrations. Depending on requirements, increase dosage to 7.5 mg once daily (administered nightly as 1 system delivering 5 mg/24 hours plus 1 system delivering 2.5 mg/24 hours or as 3 systems delivering 2.5 mg/24 hours) or decrease dosage to 2.5 mg once daily (administered nightly as 1 system delivering 2.5 mg/24 hours).

Intrabuccal

30 mg (1 extended-release transmucosal tablet) twice daily (morning and evening) about 12 hours apart. Serum testosterone concentration may be determined just prior to the morning dose at 4–12 weeks after initiation of intrabuccal therapy; if total serum testosterone concentration is excessive, discontinue intrabuccal therapy and consider alternative treatments.

Breast Cancer

IM

200–400 mg of testosterone cypionate or testosterone enanthate every 2–4 weeks.