testosterone

TOP 100

tes-tos-te-rone

Trade Name(s): (Androderm, AndroGel Pump, Aveed, Depo-Testosterone, Fortesta, Jatenzo, Kyzatrex, Natesto, Testim, Tlando, Testopel, Vogelxo, Xyosted)

■BLACK BOX ALERT■ Testosterone undecanoate and testosterone enanthate may cause an increase of blood pressure (B/P) that can increase the risk of lifethreatening cardiovascular events, including CVA, MI, and cardiovascular death. Virilization in children and women may occur following secondary exposure to testosterone topical gel and solution. Aveed: Serious pulmonary oil microembolism reaction involving chest pain, dizziness, urge to cough, dyspnea, throat tightening, syncope; life-threatening hypersensitivity reactions, including anaphylaxis, reported during or immediately after administration.

Do not confuse testosterone with testolactone.

• PHARMACOTHERAPEUTIC:Androgen. CLINICAL:Sex hormone.

Hypogonadism: Treatment of testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter syndrome, chemotherapy, or toxic damage from alcohol or heavy metals; gonadotropin or luteinizing hormone–releasing hormone deficiency; or pituitary-hypothalamic injury from tumors, trauma, or radiation. Delayed puberty: To stimulate puberty in carefully selected males with delayed puberty. OFF-LABEL: Hormone therapy (transgender female to male).

Contraindications: Hypersensitivity to testosterone. Breastfeeding, pregnant or who may become pregnant, prostate (known or suspected) or breast cancer in males. Depo-Testosterone (additional): Severe cardiac/hepatic/renal disease. Cautions: Renal/hepatic/cardiac dysfunction, pts with history of MI or CAD; conditions influenced by edema (e.g., seizure disorder, migraines).

Principal endogenous androgen promoting growth, development of male sex organs, maintains secondary sex characteristics in androgen-deficient males. Therapeutic Effect: Relieves androgen deficiency.

Widely distributed. Metabolized in liver. Protein binding: 98%. Primarily excreted in urine. Unknown if removed by hemodialysis. Half-life: 10–100 min.

Pregnancy/Lactation: Contraindicated in pregnant women, women who may become pregnant, or during lactation. Children: Safety and efficacy not established; use with caution. Elderly: May increase risk of hyperplasia, stimulate growth of occult prostate carcinoma.

DRUG: May increase hepatotoxic effect of cycloSPORINE. May increase the anticoagulant effect of warfarin. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase Hgb, Hct, LDL, serum alkaline phosphatase, bilirubin, calcium, potassium, sodium, AST. May decrease HDL.

Capsule: (Jatenzo): 158 mg, 198 mg, 237 mg. (Kyzatrex): 100 mg, 150 mg, 200 mg. (Tlando): 112.5 mg. Gel, Topical: (AndroGel): 1.62%: packets containing 20.25 mg, 40.5% mg; pump 20.25 mg/actuation. (Testim): 50 mg of testosterone in a unit-dose tube. (Vogelxo): 50-mg packet or tube, 12.5 mg/actuation metered dose pump. (Fortesta): Metered-dose pump: 10 mg/actuation. Injection: (Cypionate [Depo-Testosterone]): 100 mg/mL, 200 mg/mL. (Enanthate [Delatestryl]): 200 mg/mL. (Aveed [Undecanoate]): 750 mg/3 mL. Nasal Gel: (Natesto): 5.5 mg/actuation. Pellet for SQ Implantation: (Testopel): 75 mg. Solution, Topical: 30 mg/activation. Transdermal System Patch: (Androderm): 2 mg/day or 4 mg/day. Solution, Auto-injector: (Xyosted): 50 mg/0.5 mL, 75 mg/0.5 mL, 100 mg/0.5 mL.

IM

• Give deep in gluteal muscle.
• Do not give IV.

PO

• Give with morning and evening meals.
• Administer capsule whole; do not break, cut, or crush. Capsule cannot be chewed.

Transdermal

(Androderm):

• Apply to clean, dry area on skin on back, abdomen, upper arms, thighs.
• Do not use tape to secure. Avoid bathing, swimming for at least 3 hrs after each application.
• Do not apply to bony prominences (e.g., shoulder) or oily, damaged, irritated skin. Do not apply to scrotum.
• Rotate application site with 7-day interval to same site.

Transdermal Gel

(AndroGel, Testim, Vogelxo):

• Apply (morning preferred) to clean, dry, intact skin of shoulder, upper arms. (Foresta): Apply to skin of front and inner thighs.
• Upon opening packet(s), squeeze entire contents into palm of hand, immediately apply to application site.
• Allow to dry.
• Do not apply to genitals.
• Avoid swimming, showering, or washing the administration site for a minimum of 2 hrs after application.

Topical Solution

(Axiron):

• Apply using applicator to axilla at same time each morning.
• Avoid washing site for 2 hrs after application.

Nasal Gel

(Natesto)

• Prime pump on first use by pumping 10 times into a sink. Follow steps according to manufacturer guidelines.

Male Hypogonadism (Primary or Hypogonadotropic)

IM: ADULTS: (Cypionate or Enanthate): 75–100 mg/wk or 150–200 mg q2wks. (Undecanoate): 750 mg at initiation, 4 wks and q10 wks thereafter. CHILDREN 12 YRS AND OLDER: (Cypionate or Enanthate): Initiation of pubertal growth: 25–75 mg q3–4wks, gradually titrate q6–9mos to 100–150 mg. Duration: 3–4yrs. Maintenance virilizing dose: 200–250 mg q3–4wks. May convert to other testosterone replacement dosages once expected adult height and adequate virilization achieved.

PO: (Jatenzo): 237 mg twice daily in morning and evening. Range: 158–396 mg twice daily. (Kyzatrex): 200 mg in morning and evening. Range: 100–400 mg twice daily. (Tlando): 225 mg twice daily.

SQ: (Pellets): ADULTS, CHILDREN 12 YRS AND OLDER: 150–450 mg q3–6mos.

Topical gel: (Fortesta): 40 mg once daily in morning. Range: 10–70 mg. Maximum: 70 mg. (Vogelxo): 50 mg once daily (one tube or one packet or 4 pump actuations). Range: 50–100 mg/day.

Topical solution: ADULTS, ELDERLY: 60 mg once daily (1 pump activation of 30 mg to each axilla). Range: 30–120 mg.

Transdermal patch: (Androderm): ADULTS, ELDERLY: Start therapy with 4 mg/day patch applied at night. Apply patch to abdomen, back, thighs, upper arms. Dose adjustment based on testosterone levels. Range: 2–6 mg/day.

Transdermal gel: ADULTS, ELDERLY: (AndroGel 1.62%): Initial dose of 40.5 mg applied once daily in the morning to shoulder and upper arms. May increase to 81 mg. Further adjustments based on testosterone levels. (Testim, Vogelxo): ADULTS, ELDERLY: Initial dose of 5 g delivers 50 mg testosterone and is applied once daily to the shoulders, upper arms. May increase to 10 g (100 mg testosterone).

Nasal gel: (Natesto): ADULTS ELDERLY: 11 mg (2 actuations, 1 per each nostril) 3 times/day (6–8 hrs apart).

Delayed Male Puberty

IM: (Enanthate): ADOLESCENTS: 50–200 mg q2–4wks for limited duration (4–6 months).

SQ: (Pellets): ADULTS: 150–450 mg q3–6mos.

Dosage in Renal/Hepatic Impairment

Use caution.

Frequent (37–10%): Increased blood pressure, skin blisters (transdermal), benign prostatic hypertrophy, increased hematocrit. Topical: skin reactions, itching, allergic contact dermatitis. Occasional (10–3%): Oily stools (due to IM injection oily solvent), injection site pain, application site erythema, edema, altered sense of smell, headache, acne, nausea (PO), diarrhea, back pain, nasopharyngitis (intranasal), rhinorrhea (intranasal), nose bleeding (intranasal). Rare (less than 3%): Fatigue, vertigo, insomnia, skin rash, weight gain, gynecomastia, increased appetite.

Peliosis hepatitis (presence of bloodfilled cysts in parenchyma of liver), hepatic neoplasms, hepatocellular carcinoma have been associated with prolonged high-dose therapy. Anaphylactic reactions occur rarely. Venous thromboembolism (e.g., DVT, PE) reported.

BASELINE ASSESSMENT

Obtain CBC, BMP, LFT, lipid panel; weight, B/P. Wrist X-rays may be ordered to determine bone maturation in children. Question history of hepatic/renal impairment, seizure disorder, thromboembolism (CVA, MI, pulmonary embolism).

INTERVENTION/EVALUATION

Weigh daily, report wkly gain of more than 5 lb; evaluate for edema. Monitor B/P. Assess serum electrolytes, cholesterol, Hgb, Hct (periodically for high dosage), LFT, radiologic exam of wrist, hand (when using in prepubertal children). With breast cancer or immobility, check for hypercalcemia (anxiety, bradycardia, facial twitching; muscle cramps, spasm, weakness; seizures). Ensure adequate intake of protein, calories. Assess for virilization. Monitor sleep patterns. Monitor for CVA (aphasia, confusion, paresthesia, hemiparesis, seizures), MI (chest pain, diaphoresis, left arm/jaw pain, increased serum troponin, ST segment elevation), pulmonary embolism (chest pain, dyspnea, hypoxia, tachycardia).

PATIENT/FAMILY TEACHING

Females:

• Do not take any other medication without consulting physician.
• Maintain diet high in protein, calories.
• Weigh daily; report 5 lb/wk gain.
• Report nausea, vomiting, acne, pedal edema.
• Promptly report menstrual irregularities, hoarseness, deepening of voice.
• Males: Report frequent erections, difficulty urinating, gynecomastia.
• Treatment may cause arterial or venous blood clots; report symptoms of heart attack (chest pain, difficulty breathing, jaw pain, nausea, pain that radiates to the left arm, sweating), stroke (blindness, confusion, one-sided weakness, loss of consciousness, trouble speaking, seizures); DVT (swelling, pain, hot feeling in the arms or legs), lung embolism (difficulty breathing, chest pain, rapid heart rate).