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Testosterone is obtained for therapeutic purposes by extraction from animal testes or by synthesis from cholesterol in a laboratory. It is used to treat male hypogonadism and delayed male puberty as well as to relieve symptoms in some forms of metastatic breast cancer in females, and is used as the base for various esters (e.g., cypionate, enanthate, propionate). Women normally secrete a certain amount of male hormones; however, if the hormone balance is disturbed and there is overproduction of male hormones in a woman, masculinization may develop.
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/tes·tos·te·rone/ (tes-tos´tĕ-rōn″) the principal androgenic hormone, produced by the interstitial (Leydig) cells of the testes in response to stimulation by the luteinizing hormone of the anterior pituitary gland; it is thought to be responsible for regulation of gonadotropic secretion, spermatogenesis, and wolffian duct differentiation. It is also responsible for other male characteristics after its conversion to dihydrotestosterone. In addition, testosterone possesses protein anabolic properties. It is used as replacement therapy for androgen deficiency in males, in the treatment of delayed male puberty or hypogonadism, and in the palliation of certain breast cancers in females; used as the base or various esters (e.g., cypionate, enanthate, propionate).
testosteroneEndocrinology The principal and most potent of the C-19 androgenic steroids, produced from its precursor hormone, progesterone, by the Leydig cells of testis, and, in far lesser amounts, in the ovary and adrenal cortex, and drives the development and maintenance of ♂ sex characteristics Activity Nitrogen retention, buildup of protein, induction and maintenance of 2º ♂ characteristics–eg, facial hair; testosterone secretion is in turn regulated by LH, which is produced by the anterior pituitary Indications Treatment of sexual dysfunction, weight loss, depression Ref range ♂–total, 300–1000 ng/dL; free, 5.1–41.0 ng/dL; ♀–total, 20-90 ng/dL; free, 0.1–2.3 ng/dL ↑ in ♂ sexual precocity, hyperplasia of adrenal cortex, adrenogenital syndrome, polycystic ovary syndrome ↓ in Alcoholism, anterior pituitary gland hypofunction, estrogen therapy, Klinefelter syndrome–aka 1º hypogonadism, testicular hypoactivity. See Sublingual testosterone. Cf Progesterone.
testosteroneThe principal male sex hormone (androgen) produced in the INTERSTITIAL cells of the TESTIS and, to a lesser extent in the OVARY. Testosterone is ANABOLIC and stimulates bone and muscle growth and the growth of the sexual characteristics. It is also used as a drug to treat delayed puberty or some cases of infertility or to help to treat breast cancer in post-menopausal women. It may be given by mouth, depot injection or skin patch. The drug is on the WHO official list. Brand names are Andropatch, Restandol, Sustanon, Testogel and Virormone.
testosteronea steroid ANDROGEN produced by the LEYDIG CELLS between the SEMINIFEROUS TUBULES of the TESTIS. It causes the development and maintenance of accessory sex organs, the genitalia and the SECONDARY SEXUAL CHARACTERS.
anabolic steroidsusually refers to a group of synthetic drugs based on the male sex hormone testosterone secreted by the testes, and having similar anabolic and other androgenic actions to this and other androgens from the adrenal cortex in both sexes. These drugs are misused in sports, especially where enhanced power and strength are beneficial such as weight lifting and cycling. Used in conjunction with a training programme, they lead to an increase in muscle size and power. They may also lessen fatigue and improve tissue repair. Use in children can lead to premature fusion of the epiphyses, stunting skeletal growth. Side effects are common and potentially serious. They include psychological changes (notably aggression), liver damage, cardiovascular (raised blood pressure) and endocrine effects (masculinization in females, testicular atrophy and reduced sperm count in males.) See also adrenal glands, hormones; Table 1.
|Site of production||Name of hormone||Main targets||Involved in regulating:||Secretion controlled by:|
|Hypothalamus||Releasing and inhibiting hormones||Anterior pituitary (via local blood vessels)||Secretion of anterior pituitary hormones||Other brain regions; feedback re regulated hormones and their actions|
|Neurohormones released from posterior pituitary:|
|Oxytocin||Uterus, breasts||Labour and lactation||Afferent information from target organs|
|Antidiuretic hormone (ADH, vasopressin)||Kidneys||Water loss: ECF volume and osmolality||Hypothalamic osmoreceptors|
|Anterior pituitary||(Human) growth hormone (H)GH||Most cells||Growth and metabolism||Hypothalamic releasing and inhibiting hormones via local blood vessels|
|Thyroid-stimulating (TSH)||Thyroid gland||Thyroid secretions|
|Gonadotrophins||Ovary or testis||Germ cell maturation and hormone secretions|
|Adrenocorticotrophic (ACTH)||Adrenal cortex||Cortisol secretion|
|Pineal body||Melatonin||Widespread, including brain, thymus, etc.||Hypothalamus; varying light input from retina|
|Parathyroids||Parathormone||Bone, kidneys, gut||ECF [Ca2+]|
|Medulla||Heart, smooth muscle, glands||Cardiovascular and metabolic adjustments to activity and stress||Sympathetic nervous system|
|Atrial wall||Atrial natriuretic hormone||Kidneys||Blood volume; increases sodium (therefore also water) loss in urine||Stretch of atrial wall by venous pressure|
|Gonads: Testis||Androgens (mainly testosterone)||Genitalia and other tissues||Reproductive function and sex characteristics||Anterior pituitary gonadotrophins|
|Ovary||Uterus, breasts and other tissues||Menstrual cycle, pregnancy, lactation|
|Pancreas||Blood levels, storage and cellular uptake of nutrients, notably glucose, but also proteins and fats||Blood levels of nutrients; autonomic nervous system; other gastrointesinal hormones|
|Stomach||Gastrin||Gastric acid-secreting cells||Gastrointestinal functions: motility, digestive juices and other secretions||Local chemical and mechanical factors in the alimentary tract|
|Small intestine||Several GI functions including bile flow, pancreatic enzyme and exocrine secretions||Ingestion of food, distension of GI tract|