Dosing & Uses
Dosage Forms & Strengths
injectable solution (cypionate): Schedule III
- 100mg/mL (Depo-Testosterone)
- 200mg/mL (Depo-Testosterone)
injectable solution (enanthate): Schedule III
- 200mg/mL (Delatestryl)
injectable solution (undecanoate): Schedule III
- 250mg/mL (Aveed)
pellet implant: Schedule III
- 75mg (Testopel)
- 12.5mg, 25mg, 37.5mg, 50mg (generic)
Hypogonadism
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
Testosterone cypionate: 50-400 mg IM every 2-4 weeks
Testosterone enanthate: 50-400 mg IM every 2-4 weeks
Testosterone undecanoate (restricted availability): 750 mg IM initial dose, repeat after 4 weeks, and then q10wk thereafter
Pellet: 150-450 mg SC every 3-6 months; 150 mg of pellet approximately equivalent to 25 mg of testosterone propionate weekly
Delayed Puberty in Males
50-200 mg IM every 2-4 weeks for 4-6 months
Alternative: 150-450 mg SC every 3-6 months
Inoperable Mammary Cancer in Women
200-400 mg enanthate IM every 2-4 weeks
Androgen Deficiency in HIV+ Patients (Orphan)
Physiologic testosterone replacement in androgen-deficient HIV+ patients with associated weight loss
Orphan sponsor
- Watson Laboratories, Research Park, 417 Wakara Way, Salt Lake City, UT 8410
Delayed Growth (Orphan)
Treatment of constitutional delay in growth and puberty in adolescent boys aged 14-17 years (testosterone undecanoate)
Orphan sponsor
- SOV Therapeutics, Inc, 101 Guymon Court, Morrisville, NC 27560
Dosage Forms & Strengths
injectable solution (cypionate): Schedule III
- 100mg/mL (Depo-Testosterone)
- 200mg/mL (Depo-Testosterone)
injectable solution (enanthate): Schedule III
- 200mg/mL (Delatestryl)
injectable solution (undecanoate): Schedule III
- 250mg/mL (Aveed)
pellet implant: Schedule III
- 75mg (Testopel)
- 12.5mg, 25mg, 37.5mg, 50mg (generic)
Hypogonadism
<12 years
- Safety and efficacy not established
≥12 years
- Testosterone cypionate: 50-400 mg IM every 2-4 weeks
- Testosterone enanthate: 50-400 mg IM every 2-4 weeks
- Testosterone undecanoate (restricted availability): 750 mg IM initial dose, repeat after 4 weeks, and then q10wk thereafter
- Pellet: 150-450 mg SC every 3-6 months; 150 mg of pellet approximately equivalent to 25 mg of testosterone propionate weekly
Delayed Puberty in Males
<12 years
- Safety and efficacy not established
≥12 years
- 50-200 mg IM every 2-4 weeks for 4-6 months
- Alternate dosing schedule: 150-450 mg SC every 3-6 months
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
Frequency Not Defined
Acne
Abnormal dreams
Aggressive behavior
Alopecia
Anaphylaxis
Anger
Amnesia
Anxiety
Bladder irritability
Breast soreness
Deep venous thrombosis
Excessive frequency and duration of erection
Fatigue
Growth acceleration
Gynecomastia
Headache
Hirsutism
Hot flashes
Hypersensitivity
Hypercholesterolemia
Hypertension
Insomnia
Liver function alterations
Male pattern baldness
Menstrual irregularities
Priapism
Pruritus
Rash
Seborrhea
Suppression of factors II, V, VII, X
Vasodilation
Virilization
Water retention
Postmarketing Reports
Vascular Disorders: Venous thromboembolism
Warnings
Black Box Warnings
Serious pulmonary oil microembolism reactions, involving urge to cough, dyspnea, throat tightening, chest pain, dizziness, and syncope (POME) reactions and episodes of anaphylaxis reported during or immediately after administration of testosterone undecanoate injection; may occur after first dose
Observe patients for 30 minutes in healthcare setting to provide immediate medical treatment in event of serious POME reactions or anyphylaxis
Because of risks of serious POME reactions and anaphylaxis, testosterone undecanoate is available through restricted program under a risk evaluation and mitigation strategy (REMS) called the Aveed REMS Program
Contraindications
Hypersensitivity to product or formulation components
Cancer of breast or known or suspected carcinoma of prostate in men
Severe cardiac, hepatic, or renal disease
Women: Pregnancy or prospect of pregnancy
Cautions
Do not use testosterone cypionate interchangeably with testosterone propionate
Breast cancer patients: Risk of hypercalcemia; discontinue if this condition develops
Long term use (>10 years) of parenteral testosterone for male hypogonadism may increase the risk of breast cancer
Observe women for signs of virilization during treatment for metastatic breast cancer; if such signs are noted, discontinue to prevent irreversible virilization
Caution in history of myocardial infarction (MI) or coronary artery disease (CAD); some postmarketing studies have shown an increased risk of myocardial infarction and stroke associated with use of testosterone replacement therapy
Testosterone has been subject to abuse, typically at doses higher than recommended for approved indication and in combination with other anabolic androgenic steroids; anabolic androgenic steroid abuse can lead to serious cardiovascular and psychiatric adverse reactions; if testosterone abuse suspected, check serum testosterone concentrations to ensure they are within therapeutic range; consider possibility of testosterone and anabolic androgenic steroid abuse in suspected patients who present with serious cardiovascular or psychiatric adverse events
Prolonged use of high-dose androgens associated with peliosis hepatitis and hepatic neoplasms (including hepatic cancer)
Risk of cholestatic hepatitis with jaundice; discontinue if this condition develops
Geriatric patients: Increased risk of benign prostatic hyperplasia (BPH) and prostate cancer; monitor patients with BPH for worsening of signs and symptoms of BPH
Risk of gynecomastia
May alter serum lipid profile (use caution in history of MI or coronary artery disease)
May increase sensitivity to oral anticoagulants and decreases blood glucose; adjust dosages accordingly
May cause hypercalcemia in patients with prolonged immobilization or cancer
Use with caution in patients with diseases that may be exacerbated by fluid retention, including cardiac, hepatic, or renal dysfunction; testosterone may cause fluid retention; treatment of androgen deficiency syndromes is not recommended for men with uncontrolled or poorly controlled heart failure
May accelerate bone maturation and premature closure of epiphyses in children; in prebubertal children perform radiographic examination
Large doses may suppress spermatogenesis
May potentiate sleep apnea in some patients
Risk of priapism, excessive sexual stimulation, or acute urethral obstruction in patients with BPH
Increased hematocrit (polycythemia), reflective of increased red blood cell mass, may require discontinuation; increases risk for thromboemolism; monitor serum testosterone, prostate specific antigen (PSA), liver function, lipid concentrations, hematocrit and hemoglobin periodically
Skin burns reported at application site in patients wearing an aluminized transdermal system during a magnetic resonance imaging scan (MRI); because transdermal testosterone patch contains aluminum, it is recommended to remove system before undergoing MRI
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
Cardiovascular risks
- Evaluate patients for cardiovascular risk factors prior to initiating therapy and monitor closely for cardiovascular events during therapy; it may be prudent to avoid testosterone therapy in men who have experienced a cardiovascular event
- January 31, 2014: FDA is investigating risk of stroke, MI, and death in men taking prescription testosterone drugs; investigation was prompted by findings from 2 studies suggesting increased risk of MI in men who take testosterone
- In one study, analysis of 55,593 men with history of MI showed that men >65 years had 2-fold increase in MI risk within 90 days of filling initial prescription for testosterone drug; among younger men (<65 years) with history of heart disease, MI risk was increased 2- to 3-fold
- This study confirmed results of earlier, much smaller study, which found that older men, many with underlying heart disease, had 30% increased chance of death, MI, and stroke after receiving testosterone therapy
Edema
- Risk of edema; edema with or without congestive heart failure, may be a complication in patients with pre-existing cardiac, renal, or hepatic disease
- Diuretic treatment may be necessary in addition to discontinuance of drug
- If drug therapy is restarted, use lower dosage
Healthy males with delayed puberty
- Monitor bone maturation by assessing bone age of wrist and hand every 6 months
- May accelerate bone maturation, compromising final adult height
Pregnancy & Lactation
Pregnancy category: X
Lactation: Drug is excreted into breast milk; avoid using
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Endogenous androgen; promotes growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males
Absorption
Bioavailability: IM, slowly absorbed
Duration: 2-4 wk (IM)
Peak plasma time: 24 hr (IM)
Distribution
Protein bound: 98%
Vd: 75-122 L/kg
Metabolism
Metabolized in liver to glucuronic and sulfuric acid conjugates
Metabolites: Testosterone glucuronic conjugate (activity unknown), testosterone sulfuric acid conjugate (activity unknown), testosterone-19-d3
Elimination
Half-life: 10-100 min
Renal clearance: 2 L/min
Excretion: Urine (90%), feces (6%)
Administration
IM Administration
Prior to initiating therapy, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least 2 separate days and that these serum testosterone concentrations are below the normal range
The aluminum metal ring or crimp seal around the gray rubber stopper from the vial, should not be removed prior to the administration of the injection
For IM use, should be administered deep in gluteal muscle
Dosages >400 mg/month not recommended
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Patient Handout
Formulary
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