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Pharmacologic class: Hormone
Therapeutic class: Androgenic and anabolic steroid, antineoplastic
Controlled substance schedule III
Pregnancy risk category X
FDA Box Warning
Virilization has occurred in children secondarily exposed to testosterone gel.
Children should avoid contact with unwashed or unclothed application sites in men using testosterone gel.
Health care providers should advise patients to strictly adhere to recommended instructions for use.
Responsible for normal growth and development of male sex organs and maintenance and maturation of secondary sex characteristics. Also decreases estrogen activity, which aids treatment of some breast cancers.
Buccal system: 30 mg
Gel: 1% (25 mg, 50 mg), 1.62% (metered-dose pump delivers 20.25 mg/actuation), 2% (10 mg/one metered-dose pump actuation)
Injection (aqueous suspension): 100 mg/ml
Pellets (subcutaneous implant): 75 mg
Solution (topical): 30 mg/metered-dose pump actuation
Transdermal system: 2 mg/day, 4 mg/day
Injection: 100 mg/ml, 200 mg/ml
Injection (in oil): 200 mg/ml
Indications and dosages
➣ Male hypogonadism
Adult males: 10 to 25 mg (testosterone) I.M. two to three times weekly or 50 to 400 mg (enanthate) I.M. q 2 to 4 weeks for 3 to 4 years. Or 150 to 450 mg (pellet) implanted subcutaneously q 3 to 6 months. Or, 4 mg (transdermal system) daily, adjusted to 2 mg or 6 mg based on serum testosterone level. Or, 60 mg (one 30-mg actuation of Axiron topical solution applied to each axilla) daily at same time each morning, adjusted to 30 mg (one pump actuation) or increased from 60 to 90 mg (three pump actuations) or from 90 to 120 mg (four pump actuations) based on serum testosterone concentration from single blood draw 2 to 8 hours after applying solution and at least 14 days after starting treatment or following dosage adjustment. Or, 40 mg (four actuations of Fortesta topical gel) applied to clean, intact skin of thighs once daily in morning, adjusted to 10 mg (one pump actuation) or up to 70 mg (seven pump actuations) based on total serum testosterone level 2 hours after applying gel at approximately 14 days after starting treatment or following dosage adjustment. Or, 50 mg testosterone gel (AndroGel 1%) daily applied topically, adjusted up to 75 mg daily within 14 days, with subsequent dosages up to 100 mg daily. Or, 30 mg (buccal system) to gum region b.i.d. Or, 50 to 400 mg I.M. (cypionate) q 2 to 4 weeks.
➣ Delayed puberty
Adult males: 50 to 200 mg I.M. (enanthate only) q 2 to 4 weeks for limited duration (4 to 6 months); or 150 to 450 mg subcutaneously (pellets) q 3 to 6 months
➣ Inoperable breast cancer in women 1 to 5 years after menopause
Adults: 200 to 400 mg I.M. (enanthate) q 2 to 4 weeks
• Hypersensitivity to drug, its components, or tartrazine
• Males with breast cancer or suspected prostate cancer
• Females (buccal or transdermal systems or gel)
• Pregnancy or breastfeeding
Use cautiously in:
• diabetes mellitus; edema associated with serious cardiac, hepatic, or renal disease; sleep apnea; hypercalcemia
• children younger than age 18 (safety and efficacy not established).
• Evaluate elderly patients and patients at increased risk for prostate cancer for presence of prostate cancer before starting testosterone replacement therapy.
• Inspect aqueous solution for injection. If crystals are visible, warm bottle and shake contents to dissolve crystals.
• Rotate I.M. injection sites within upper outer quadrant of gluteus maximus. Inject deeply into muscle.
• Apply gel once daily to clean, dry, intact skin on shoulder, upper arm, or abdomen.
• Place buccal system just above incisor tooth. Have patient hold it in place for 30 seconds to ensure adhesion. Rotate to other side of mouth with each application.
CNS: headache, depression, emotional lability, nervousness, anxiety, asthenia, memory loss, dizziness, vertigo, cerebrovascular accident
CV: edema, peripheral edema, deepvein phlebitis, heart failure
GU: hematuria, urinary tract infection, impaired urination, scrotal cellulitis, benign prostatic hyperplasia, scrotal papilloma (with transdermal use), prostatitis, libido changes, breast pain or tenderness, gynecomastia, virilization in females, excessive hormonal effects in males
Hematologic: polycythemia, leukopenia, suppressed clotting factors
Hepatic: hepatic adenoma (with long-term enanthate use)
Metabolic: hyperphosphatemia, hypernatremia, hypercalcemia, hypoglycemia, hyperkalemia
Respiratory: sleep apnea
Skin: acne; rash, itching, burning, discomfort, irritation, burn-like blister, erythema (with transdermal use); pain, local edema, and induration at injection site (with I.M. or subcutaneous use)
Other: accidental injury, flulike symptoms, hypersensitivity reaction
Drug-drug. Corticosteroids: increased risk of edema
Hepatotoxic drugs: increased risk of hepatotoxicity
Insulin, oral hypoglycemics: decreased blood glucose level
Oral anticoagulants: increased anticoagulant effect
Oxyphenbutazone: increased oxyphenbutazone blood level
Propranolol: increased propranolol clearance
Drug-diagnostic tests. Bilirubin, liver function tests: abnormal results
Calcium, cholesterol, hematocrit, hemoglobin, phosphate, prostate-specific antigen (with topical use), sodium: increased levels
Clotting factors, creatine excretion, glucose, serum creatinine, thyroxine, thyroxine-binding globulin: decreased levels
Urine creatine and creatinine: decreased excretion
Urine 17-ketosteroids: increased excretion
Drug-herbs. Chaparral, comfrey, germander, jin bu huan, kava, pennyroyal: increased risk of hepatotoxicity
• Monitor electrolyte levels, liver function tests, blood and urine calcium levels, lipid panels, CBC with white cell differential, and semen studies.
• Assess diabetic patient carefully for hypoglycemia.
• Closely monitor neurologic status. Stay alert for sleep apnea.
• Assess for early signs of excessive hormonal effects in females (virilization). If these occur, drug withdrawal may be indicated.
Instruct patient to immediately report signs and symptoms of liver problems, including nausea, vomiting, yellowing of skin or eyes, and ankle swelling.
• Teach prepubertal male about signs and symptoms of excessive hormonal effects, such as acne, priapism, increased body and facial hair, and penile enlargement.
• Teach postpubertal male about signs and symptoms of excessive adverse hormonal effects, such as erectile dysfunction, gynecomastia, epididymitis, testicular atrophy, and infertility.
Tell female patient to immediately report signs of masculinization, such as excessive body or facial hair, deepening of voice, clitoral enlargement, and menstrual irregularities.
• Advise female of childbearing age to use barrier contraceptives. Caution her not to breastfeed.
• Tell patient which transdermal patches can be applied to scrotum. Instruct him to apply patch daily to clean, dry skin after removing protective liner to expose drug-containing film. To prevent irritation, instruct him to apply each patch to a different site, waiting at least 1 week before reusing same site.
• Advise patient to apply topical gel once daily to clean, dry skin on shoulder, upper arm, or abdomen. Tell him that after opening packet, he should squeeze entire contents into palm and apply immediately. Instruct him to wait until gel dries before getting dressed.
• Teach patient to place buccal system in comfortable position just above incisor tooth and hold it in place for about 30 seconds to ensure adhesion. Tell him to use opposite side of mouth with each application. Caution him not to dislodge buccal system, especially when eating, drinking, brushing teeth, or using mouthwash. If system doesn't properly adhere or falls out during 12hour dosing interval, tell him to discard it and apply new system. If it falls out within 4 hours of next dose, tell him to apply new system and keep it in place until next regularly scheduled dose.
• Instruct patient to apply topical solution to clean, dry, intact skin of axilla area only and to allow application site to dry completely before dressing. Advise patient to wash axilla with soap and water to remove any testosterone residue if direct skin-to-skin contact with another person is anticipated.
• Tell patient drug shouldn't be used to enhance athletic performance or physique.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.
testosterone enanthate(tess-toss-te-rone en-an-thate) ,
- Growth and maturation of the prostate, seminal vesicles, penis, scrotum,
- Development of male hair distribution,
- Vocal cord thickening,
- Alterations in body musculature and fat distribution.
- Initiation of male puberty.
Time/action profile (androgenic effects†)
Adverse Reactions/Side Effects
Ear, Eye, Nose, Throat
- deepening of voice (most frequent)
- edema (most frequent)
- cholestatic jaundice
- drug-induced hepatitis
- liver function test elevation
- change in libido (most frequent)
- clitoral enlargement (most frequent)
- menstrual irregularities men-:
- erectile dysfunction (most frequent)
- priapism (most frequent)
- prostatic enlargement
- hypercholesterolemia women-:
- hirsutism (most frequent) men-:
- gynecomastia (most frequent)
- oligospermia (most frequent)
Fluid and Electrolyte
- male pattern baldness
- pain at injection site
Drug-Drug interactionMay ↑ action of warfarin, oral hypoglycemic agents, andinsulin.Concurrent use with corticosteroids may ↑ risk of edema formation.
Route/DosageMale Hypogonadism (replacement therapy)
Availability (generic available)
- Monitor intake and output ratios, weigh patient twice weekly, and assess patient for edema. Report significant changes indicative of fluid retention.
- Men: Monitor for precocious puberty in boys (acne, darkening of skin, development of male secondary sex characteristics—increase in penis size, frequent erections, growth of body hair). Bone age determinations should be measured every 6 mo to determine rate of bone maturation and effects on epiphyseal closure.
- Monitor for breast enlargement, persistent erections, and increased urge to urinate in men. Monitor for difficulty urinating in elderly men, because prostate enlargement may occur.
- Women: Assess for virilism (deepening of voice, unusual hair growth, clitoral enlargement, acne, menstrual irregularities).
- In women with metastatic breast cancer, monitor for symptoms of hypercalcemia (nausea, vomiting, constipation, lethargy, loss of muscle tone, thirst, polyuria).
- Lab Test Considerations: Monitor hemoglobin and hematocrit periodically during therapy; may cause polycythemia.
- Monitor hepatic function tests and serum cholesterol levels periodically during therapy. May ↑ serum AST, ALT, and bilirubin, ↑ cholesterol levels, and suppress clotting factors II, V, VII, and X.
- Monitor serum and urine calcium levels and serum alkaline phosphatase concentrations in women with metastatic breast cancer.
- Monitor blood glucose closely in patients with diabetes who are receiving oral hypoglycemic agents or insulin.
- Monitor serum sodium, chloride, potassium, and phosphate concentrations (may be ↑).
Potential Nursing DiagnosesSexual dysfunction (Indications, Side Effects)
- Range-of-motion exercises should be done with all bedridden patients to prevent mobilization of calcium from the bone.
- Intramuscular: Administer IM deep into gluteal muscle. Crystals may form when vials are stored at low temperatures; warming and rotating the vial between the palms of hands will redissolve crystals. Use of a wet syringe or needle may cause solution to become cloudy but will not affect its potency.
- Advise patient to report the following signs and symptoms promptly: in male patients, priapism (sustained and often painful erections), difficulty urinating, or gynecomastia; in female patients, virilism (which may be reversible if medication is stopped as soon as changes are noticed), or hypercalcemia (nausea, vomiting, constipation, and weakness); in male or female patients, edema (unexpected weight gain, swelling of feet), hepatitis (yellowing of skin or eyes and abdominal pain), or unusual bleeding or bruising.
- Explain rationale for prohibiting use of testosterone for increasing athletic performance. Testosterone is neither safe nor effective for this use and has a potential risk of serious side effects.
- Instruct females to notify health care professional immediately if pregnancy is planned or suspected.
- Advise diabetic patients to monitor blood closely for alterations in blood glucose concentrations.
- Emphasize the importance of regular follow-up physical exams, lab tests, and x-ray exams to monitor progress.
- Radiologic bone age determinations should be evaluated every 6 mo in prepubertal children to determine rate of bone maturation and effects on epiphyseal centers.
- Resolution of the signs of androgen deficiency without side effects. Therapy is usually limited to 3–6 mo followed by bone growth or maturation determinations.
- Decrease in the size and spread of breast malignancy in postmenopausal women. In antineoplastic therapy, response may require 3 mo of therapy; if signs of disease progression appear, therapy should be discontinued.
anabolic steroidA drug or hormone-like substance chemically or pharmacologically related to 17-α-alkylated testosterone that promotes muscle growth, which are commonly abused by athletes. Lipid changes by ASs are more marked with oral stanazol (manufactured for horses) than with IV testosterone; it decreases HDL-C (especially HDL2) and increases hepatic TG lipase (HDL) catabolism.
Children, adolescents with delayed puberty, decreased growth, small penis, hypogonadism, testosterone deficiency, osteoporosis management, aplastic anaemia, endometriosis, angioedema, sports performance enhancement (no longer legal), relief and recovery from common injuries, rehabilitation, weight control, anti-insomnia, and regulation of sexuality, aggression and cognition.
Increased protein synthesis and amino acid consumption, androgenesis, catabolism and gluticocototitosis.
Adverse effects (men)
Breast enlargement (gynecomastia), testicular atrophy, sterility, sperm abnormalities, impotence, prostatic hypertrophy, myocardial hypertrophy and fibrosis, myocardial infarction and fatal arrhythmias, peliosis hepatis, cholestasis, hepatic adenomas, testicular atrophy, peripheral oedema, intracerebral thrombosis.
Adverse effects (women)
Clitoral hypertrophy, beard growth, baldness, deepened voice, decreased breast size.
Adverse effects (men and women)
Aggression and antisocial behavior, increased risk of cardiovascular disease, peliosis hepatis, haemorrhage, jaundice, acne, accelerated bone maturation resulting in short stature, liver tumours (hepatic adenomas and CA) which may regress with abstinence; AS abusers are at an increased risk for HIV transmission, given the common practice of sharing of needles when injecting ASs.
ASs are detectable to 1 parts per billion 4 days after last use if the hormone is water-soluble, or 14 days after use in lipid-soluble compounds.
ASs are schedule-III drugs per the Controlled Substances Act.