Delatestryl

Delatestryl [del″ah-tes´tril]

trademark for a preparation of testosterone, used for treatment of male hypogonadism and delayed male puberty, and palliation of metastatic breast cancer in women.

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testosterone enanthate Warning - Hazardous drug!

Delatestryl

Pharmacologic class: Hormone

Therapeutic class: Androgenic and anabolic steroid, antineoplastic

Controlled substance schedule III

Pregnancy risk category X

Action

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.

Availability

testosterone

Buccal system: 30 mg

Gel: 1% (25 mg, 50 mg)

Injection (aqueous suspension): 100 mg/ml

Pellets (subcutaneous implant): 75 mg

Transdermal system: 2.5 mg/24 hours, 4 mg/24 hours, 5 mg/24 hours, 6 mg/24 hours

testosterone cypionate

Injection: 100 mg/ml, 200 mg/ml

testosterone enanthate

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 5 mg daily transdermal (nonscrotal) system (Androderm); may increase up to 7.5 mg daily or 5 mg daily (Testoderm TTS), adjusted after 3 to 4 weeks and possibly increased to 10 mg daily. Or 4 to 6 mg daily transdermal scrotal system (Testoderm), adjusted after 3 to 4 weeks. 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

Contraindications

• Hypersensitivity to drug, its components, or tartrazine
• Serious cardiac, hepatic, or renal disease
• Males with breast cancer or suspected prostate cancer
• Females (buccal or transdermal systems or gel)
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• diabetes mellitus, cardiovascular or hepatic disease, sleep apnea, or hypercalcemia.

Administration

• 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.

Route	Onset	Peak	Duration
Buccal	Slow	10-12 hr	Unknown
I.M.	Unknown	10-100 min	Unknown
Subcut.	Unknown	Unknown	3-4 mo
Topical gel	30 min	Unknown	Unknown
Transdermal	Unknown	2-4 hr	Unknown

Adverse reactions

CNS: headache, depression, emotional lability, nervousness, anxiety, asthenia, memory loss, dizziness, vertigo, cerebrovascular accident

CV: edema, peripheral edema, deep-vein phlebitis, heart failure

GI: bleeding

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

Musculoskeletal: myalgia

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

Interactions

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

Patient monitoring

• 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.

Patient teaching

☞ 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 12-hour 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.
• 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.