Testosterone and derivatives


Thông tin thuốc gốc
Chỉ định và Liều dùng
Buccal
Male hypogonadism
Adult: 30 mg bid.

Intramuscular
Inoperable metastatic breast cancer
Adult: As enanthate: 200-400 mg every 2-4 wk.

Intramuscular
Male hypogonadism
Adult: 50-400 mg every 2-4 wk for the cipionate; 50-400 mg every 2-4 wk for the enantate (or an initial dose of 250 mg every 2-3 wk followed by a maintenance dose every 3-6 wk); up to 50 mg 2-3 times wkly for the propionate.

Oral
Male hypogonadism
Adult: Initially, 120-160 mg daily of the undecylate ester followed by a maintenance dose of 40-120 mg daily.

Subcutaneous
Male hypogonadism
Adult: As SC implant: 100-600 mg. A dose of 600 mg is usually able to maintain plasma testosterone level within physiological range for 4-5 mth.

Transdermal
Male hypogonadism
Adult: As patch delivering 2.5-7.5 mg daily: Apply to the back, abdomen, thighs, upper arms as directed. As scrotal patch containing 10 or 15 mg (supplying 4-6 mg in 24 hr): Use as directed.
Chống chỉ định
Hypercalcaemia or hypercalciuria, males with breast or prostate carcinoma. Pregnancy and lactation.
Thận trọng
Cardiovascular disorders, skeletal metastases, renal or hepatic impairment, epilepsy, migraine, diabetes or other conditions which may be aggravated by fluid retention, eg heart failure. Elderly, prepubertal boys. Monitor signs of virilization (females) and development of priapism or excessive sexual stimulation (males). Periodic haemoglobin, lipid determinations and rectal prostate examination.
Phản ứng phụ
Fluid and electrolyte retention; increased vascularity of the skin; hypercalcaemia, impaired glucose tolerance; increased bone growth and skeletal weight; increase LDL cholesterol; increase haematocrit and fibrinolytic activity; headache, depression and GI bleeding. Males: spermatogenesis suppression, priapism, gynaecomastia, prostatic hyperplasia and accelerate growth of malignant prostate neoplasms. Females: suppression of lactation, ovarian activity and menstruation; virilization, clitoris hypertrophy, increased libido, oily skin, acne, hirsutism, male pattern baldness. Children: Closure of the epiphyses and stop linear growth in early puberty, symptoms of virilisation. Precocious sexual development, increased frequency of erection in boys, and clitoral enlargement in girls. IM: urticaria, inflammation at Inj site, postinjection induration, furunculosis. Transdermal: local irritation. Buccal: Gum irritation, bitter taste, gum pain, tenderness.
Potentially Fatal: Peliosis hepatis, liver toxicity, malignant neoplasm.
Buccal/IM/Nasal/Parenteral/PO/SC/Topical/Transdermal: X
Tương tác
Enhance activities of ciclosporine, antidiabetics, thyroxine, anticoagulants. Long term use of testosterone may cause resistance to effects of neuromuscular blockers. Enhance fluid retention from corticosteroids.
Lab Interference
May decrease protein bound iodine (PBI) and thyroxine-binding globulin concentrations. May cause a decrease in excretion of creatinine and creatine and increase in excretion of 17-ketosteroids.
Tác dụng
Description: Testosterone is the principal endogenous androgen responsible for promoting the growth and development of male sexual organs and maintaining secondary sex characteristics in androgen-deficient males.
Pharmacokinetics:
Absorption: Absorbed from GI tract, skin, and oral mucosa
Distribution: 80% bound to sex-hormone binding globulin. Undergo enterohepatic recirculation. Half-life of testosterone: 10 to 100 min.
Metabolism: Hepatic to active and inactive metabolites.
Excretion: Excreted via urine as metabolites; and faeces as unchanged drug (6%)
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