Testosterone and derivatives


Generic Medicine Info
Indications and Dosage
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.
Contraindications
Hypercalcaemia or hypercalciuria, males with breast or prostate carcinoma. Pregnancy and lactation.
Special Precautions
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.
Adverse Reactions
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
Drug Interactions
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.
Action
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%)
Disclaimer: This information is independently developed by MIMS based on Testosterone and derivatives from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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