Trade Names:Androderm- Transdermal system 2.5 mg per 24 h- Transdermal system 5 mg per 24 h
Trade Names:Testopel- Implant pellets 75 mgTestosterone Cypionate
Trade Names:Depo-Testosterone- Injection 100 mg/mL- Injection 200 mg/mLTestosterone Enanthate
Trade Names:Delatestryl- Injection 200 mg/mLTestosterone Gel
Trade Names:AndroGel- Gel 1%
Trade Names:Testim- Gel 1%Testosterone Buccal System
Trade Names:Striant- Mucoadhesive 30 mg
Promotes growth and development of male reproductive organs, maintains secondary sex characteristics, increases protein anabolism, and decreases protein catabolism.
Testosterone transdermal T max is 2 to 4 h. Slowly released following buccal application, reaching the C max within 10 to 12 h.
After transdermal administration, steady-state testosterone levels occur in 3 to 4 wk; 98% is bound to proteins.
Transdermal testosterone is metabolized in the liver.
Transdermal testosterone t ½ is 10 to 100 min. Approximately 90% is excreted in urine, and approximately 6% is excreted in feces.
Replacement therapy in primary hypogonadism and hypogonadotropic hypogonadism (testosterone enanthate [ Delatestryl ], testosterone pellets [ Testopel ], testosterone gel [ AndroGel , Testim ], testosterone transdermal system [ Androderm ], testosterone buccal system [ Striant ], testosterone cypionate [ Depo-Testosterone ]). Stimulation of puberty (testosterone enanthate [ Delatestryl ], testosterone pellets [ Testopel ]).Women
Ablation of ovaries in metastatic breast cancer (testosterone enanthate [ Delatestryl ]).
Hypersensitivity to product; serious cardiac, hepatic, or renal disease; men with carcinoma of breast or prostate; women who are or may become pregnant; testosterone gel and buccal system are contraindicated in women.
IM 50 to 400 mg every 2 to 4 wk (testosterone enanthate, testosterone cypionate). Subcutaneous 150 to 450 mg every 3 to 6 mo (testosterone pellets). Transdermal 5 mg applied daily ( Androderm ). Topical Start by applying testosterone 5 g gel (containing testosterone 50 mg and delivering 5 mg systemically) to clean, dry skin of shoulders and/or upper arms or abdomen. Based on measurements of serum testosterone levels and clinical response 14 days after initiation of therapy, dose may be increased from 5 to 10 g ( Testim ) or from 5 to 7.5 g ( AndroGel ) and from 7.5 to 10 g ( AndroGel ). Buccal 30 mg applied to the gum region twice daily, morning and evening (about 12 h apart). Place in a comfortable position just above one of the incisor teeth.Breast CancerAdults
IM 200 to 400 mg every 2 to 4 wk (testosterone enanthate).Delayed PubertyAdolescents
IM 50 to 200 mg every 2 to 4 wk for limited duration (testosterone enanthate). Subcutaneous 150 to 450 mg every 4 to 6 mo (testosterone pellets).
Store AndroGel and Testim at 59° to 86°F. Store transdermal systems in protective pouch at controlled room temperature (59° to 86°F). Protect systems from excessive heat or pressure, which can cause bursting of the drug reservoir. Store blister packs ( Striant ) at controlled room temperature (68° to 77°F). Protect from heat and moisture. Do not remove buccal system from blister pack until ready to apply. Store vials and prefilled syringes at controlled room temperature (68° to 77°F). Protect from light. Store pellets in a cool place.
May potentiate anticoagulant effects.Corticosteroids
Use with caution because of increased risk of edema.Insulin, oral hypoglycemics
May decrease glucose levels and antidiabetic drug requirements.Propranolol
Coadministration of an injectable testosterone may increase propranolol Cl, resulting in decreased plasma levels.
Testosterone may suppress expression.Thyroid function tests
Testosterone may cause decreased levels of thyroid hormones.
Hot flashes (postmarketing).Topical gel
Anxiety, depression, generalized paresthesia, headache, increased or decreased libido; amnesia, anxiety, dizziness, hostility, insomnia, malaise, sleep apnea (postmarketing).Buccal
Headache (3%).Topical gel
Headache (4%); asthenia, decreased libido, emotional lability, nervousness (3%); depression (1%).
Acne, hirsutism, male pattern baldness, seborrhea; discolored hair, erythema, rash, paresthesia (postmarketing).Topical gel
Acne (8%); dry skin, pruritus (2%); alopecia (1%).Transdermal
Pruritus at application site (37%); burnî“¸like blister reaction under system (12%); erythema at application site (7%); vesicles at application site (6%); prostate abnormalities (5%); allergic contact dermatitis (4%); burning and induration at application site (3%).
Inhibition or gonadotropin secretion.
Nausea; nausea (postmarketing).Transdermal
GI bleeding (2%).
Amenorrhea and other menstrual irregularities, virilization (women); excessive frequency and duration of penile erection, gynecomastia, oligospermia (men).Topical gel
Enlarged prostate (12%); prostate disorder including benign prostatic hypertrophy and elevated prostatic-specific antigen (PSA) (5%); urinary symptoms including nocturia, urinary hesitancy, urinary incontinence, urinary retention, urinary urgency, weak urinary stream (4%); breast pain, gynecomastia, testis disorder including left varicocele, slight testis sensitivity (3%); prostate carcinoma (1%).
Polycythemia, suppression of clotting factors II, V, VII, and X.Topical gel
Alterations in LFTs, cholestatic jaundice, hepatocellular neoplasms, peliosis hepatitis.
Abnormalities, including elevated AST or ALT, cholesterol, testosterone, serum creatinine, triglycerides, total bilirubin, cholesterol/LDL ratio, glucose, HDL decrease, and hemoglobin or hematocrit (6% to 9%); hyperlipidemia (postmarketing).
Inflammation and pain at injection site.Buccal
Gum or mouth disorder (9%); bitter taste (4%); gum pain, gum tenderness (3%); gum edema, taste perversion (2%).Topical gel
Applicationî“¸site reactions (6%).
Increased serum cholesterol; retention of calcium, chloride, potassium, sodium, water; electrolyte changes (eg, calcium nitrogen, phosphorus, potassium, sodium), increased weight (postmarketing).
Anaphylactic reactions; edema, hirsutism (postmarketing).
Regularly monitor serum calcium concentrations in cancer patients at risk of hypercalcemia. Observe women for signs of virilization (eg, clitoral enlargement, deepening of voice). In patients with delayed puberty, effect on bone maturation should be monitored by assessing bone age of the wrist and hand every 6 mo. In patients receiving high doses, periodically check hemoglobin and hematocrit for polycythemia.
Category X .
Undetermined. Testosterone gel, cypionate, buccal, and transdermal are not indicated for women.
Use drug with great caution; may affect bone maturation.Androderm
Safety and efficacy not established in children younger than 15 yr of age.Testosterone cypionate
Safety and efficacy not established in children younger than 12 yr of age.Testosterone gel and buccal system
Safety and efficacy not established.
Elderly men may be at increased risk of developing prostatic hypertrophy or carcinoma.
Acute intermittent porphyria has been reported. Use drug with caution in patients known to have this condition.
Abuse of these agents to enhance athletic performance has potential risk of serious adverse reactions.
May develop hypercalcemia.
Edema with or without CHF may be a serious complication in patients with preexisting cardiac, hepatic, or renal disease. Use with caution in patients with conditions affected by fluid retention (eg, asthma, cardiac or renal function impairment, epilepsy).
Frequently occurs and may persist. Use drug with caution in patients with preexisting gynecomastia.
Prolonged use of high doses of androgens may result in potentially life-threatening peliosis, cholestatic jaundice, hepatitis, hepatic neoplasms, or hepatocellular carcinoma.
Use with caution in cancer patients at risk of hypercalcemia.
May occur after prolonged use.
Do not interchange products because of their differences in duration of action.
Levels may increase with androgen use; use drug with caution in patients with history of MI or coronary artery disease.
Treatment of hypogonadal men may potentiate sleep apnea, particularly in patients with risk factors (eg, chronic lung diseases, obesity).
May occur in female patients.
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