Classes
DEA Class; Rx
Common Brand Names; Androderm, AndroGel, Testim, Axiron, Fortesta, Vogelxo
- Androgens
Description
Primary androgen in humans synthesized by testes, ovaries, and adrenal cortex; available in a variety of dosage forms
Primarily used in males with primary hypogonadism or with hypogonadism due to medical conditions; may be used for a limited duration for constitutional delay of puberty; used off-label in men with sexual dysfunction due to low testosterone associated with aging
Not recommended for low testosterone status alone due to aging due to potential risk for cardiovascular events and stroke
Indications
Primary hypogonadism (congenital or acquired): Testicular failure due to conditions such as cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter Syndrome, chemotherapy, or toxic damage from alcohol or heavy metals; these men usually have low serum testosterone concentrations and gonadotropins (FSH, LH) above normal range
Hypogonadotropic hypogonadism (congenital or acquired): Gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency or pituitary-hypothalamic injury from tumors, trauma, or radiation; these men have low testosterone serum concentrations but have gonadotropins in the normal or low range
Contraindications
Males with breast or prostate cancer
Hypersensitivity
Breast feeding women
Pregnancy
Adverse Effects
- Pruritus at application site (37%)
- Skin reactions at application site (16.1%)
- Blisters under skin (12%)
- Erythema at application site (7%)
- Vesicles at application site (6%)
- Allergic contact dermatitis (4%)
- Burning at application site (3%)
- Induration at application site (3%)
- Abnormal dreams
- Acne
- Anaphylaxis
- Bladder irritability
- Breast soreness
- Cholestatic jaundice
- Deep vein thrombosis
- Dry skin
- Fatigue
- Gynecomastia
- Headache
- Insomnia
- Menstrual irregularities
- Priapism
- Suppression of factors II, V, VII
- Virilization
Warnings
Use with caution in patients with chronic lung disease, obesity, advanced age, or preexisting cardiac, renal, or hepatic disease
Employ caution with prolonged use of high doses, which may be associated with hepatic effects
May increase risk of prostate cancer
Risk of gynecomastia when used for male hypogonadism
May change serum lipid profile; use with caution in patients who have history of mycoardial infarction (MI) or coronary artery disease (CAD)
Large doses may suppress spermatogenesis
May increase hematocrit, which requires dose adjustment or discontinuation; monitor serum testosterone, prostate specific antigen (PSA), liver function, lipid concentrations, hematocrit and hemoglobin periodically
May cause hypercalcemia in patients with prolonged immolibization or cancer
Anabolic activity of androgens may enhance hypoglycemia
Children: Risks of inappropriate genital enlargement, premature pubic hair, advanced bone age, increased libido, and aggressive behavior
Fortesta: Exogenous administration of androgens may lead to azoospermia; sleep apnea may occur in those with risk factors; preparation is flammable until dry
Discontinue if urethral obstruction develops in patients with benign prostatic hyperplasia (BPH); monitor patients with BPH for worsening of signs and symptoms of BPH
Edema with or without congestive heart failure, may be a complication in patients with pre-existing cardiac, renal, or hepatic disease; use with caution
May worsen sleep apnea in some male patients
Evaluate patients for cardiovascular risk factors prior to initiating therapy and monitor closely during therapy
Use caution in patients with diseases that may be exacerbated by fluid retention, including cardiac, hepatic, or renal dysfunction; not recommended for men with poorly controlled heart failure
Monitor women for virilization when treating for metastatic breast cancer
Geriatric patients may be at greater risk for prostatic hyperplasia, prostate cancer, fluid retention, and increase in transaminase levels
Increased hematocrit (polycythemia), reflective of increased red blood cell mass, may require discontinuation; increases risk for thromboemolism
Venous thromboembolism, including DVT and PE reported in patients using testosterone products; these observations have included patients with and without polycythemia; evaluate signs or symptoms consistent with DVT or PE; if venous thromboembolic event suspected, discontinue treatment with testosterone and initiate appropriate workup and management
Pregnancy and Lactation
Contraindicated in pregnant women; drug is teratogenic and may cause fetal harm when administered to a pregnant woman based on data from animal studies and its mechanism of action; exposure of female fetus to androgens may result in varying degrees of virilization
Drug is not indicated for use in women
Maximum Dosage
Dependent on indication for therapy, as well as route of administration and specific product chosen for use.
Dependent on indication for therapy, as well as route of administration and specific product chosen for use.
Dependent on indication for therapy, as well as route of administration and specific product chosen for use.
Dependent on indication for therapy, as well as route of administration and specific product chosen for use.
Safety and efficacy have not been established.
How supplied
Testosterone Topical
patch, transdermal: Schedule III
- 2mg/24hr
- 4mg/24hr
gel, transdermal: Schedule III
- 1% (12.5mg/actuation) (Androgel)
- 1.62% (20.25mg/actuation) (Androgel)
- 10mg/actuation (1 pump actuation dispenses 0.5 g of gel) (Fortesta)
- 12.5mg/actuation (Vogelxo)
- 20.25mg/1.25g
- 25mg/2.5g
- 40.5mg/2.5g
- 50mg/5g (Testim)
- 50mg/unit dose pack (Vogelxo)
ointment, topical: Schedule III
- 2%
solution, topical: Schedule III
- 30mg/actuation (90mL) (Axiron)
cream, transdermal: Schedule III
- 2%
