Brands, Medical Use, Clinical Data
Brands / Synonyms
Andriol; Andro; Andro 100; Andro L.A. 200; Androderm; Androgel; Android 10; Android 25; Android 5; Androlin; Andronaq; Andronate 100; Andronate 200; Andropatch; Andropository 200; Andrusol; Andryl 200; Axiron; Beta Testosterone; CDB 111C; Cristerona T; Cristerone T; Dea No. 4000; Delatest; Delatestryl; Depo-Testosterone; Depo-Testosterone Cypionate; Depotest; Dofsol; Everone 200; Fortesta; Geno-Cristaux Gremy; Homosteron; Homosterone; Libigel; Malerone; Malestrone; Malogen in Oil; Malogen, Aquaspension Injection; Mertestate; Metandren; Methyltestosterone; Neo-Hombreol F; Neo-Testis; Neotestis; Oreton; Oreton F; Oreton Methyl; Oreton-F; Orquisteron; Perandren; Percutacrine Androgenique; Primotest; Primoteston; Relibra; Scheinpharm Testone-Cyp; Striant; Sustanon; Sustanone; Sustason 250; Synandrol F; T-Cypionate; TES; Teslen; Testamone 100; Testandrone; Testaqua; Testex; Testiculosterone; Testim; Testobase; Testoderm; Testoderm Tts; Testogel; Testoject-50; Testolin; Testopel Pellets; Testopropon; Testosteroid; Testosteron; Testosterona [Inn-Spanish]; Testosterone; Testosterone and Its Esters; Testosterone Cypionate; Testosterone Enanthate; Testosterone Hydrate; Testosterone Propionate; Testosterone [Ban:Inn]; Testosteronum [Inn-Latin]; Testostosterone; Testoviron; Testoviron Schering; Testoviron T; Testred; Testred Cypionate 200; Testrin-P.A; Testro Aq; Testrone; Testryl; Trans-Testosterone; Virilon; Virilon IM; Virormone; Virosterone
For replacement therapy in males for conditions associated with a deficiency or absence of endogenous testosterone.
Testosterone is a steroid hormone from the androgen group. Testosterone is primarily secreted in the testes of males and the ovaries of females although small amounts are secreted by the adrenal glands. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does.
Mechanism of Action
The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Approximately 10% of the testosterone dose applied on the skin surface is absorbed into systemic circulation
Side effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation.
Biotrnasformation / Drug Metabolism
Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT).
Androgens are contraindicated in men with carcinoma of the breast or known or suspected carcinoma of the
AndroGel® is not indicated for use in women, has not been evaluated in women, and must not be used in
Pregnant women should avoid skin contact with AndroGel® application sites in men. Testosterone may cause fetal
harm. In the event that unwashed or unclothed skin to which AndroGel® has been applied does come in direct
contact with the skin of a pregnant woman, the general area of contact on the woman should be washed with soap and
water as soon as possible. In vitro studies show that residual testosterone is removed from the skin surface
by washing with soap and water.
AndroGel® should not be used in patients with known hypersensitivity to any of its ingredients, including
testosterone USP that is chemically synthesized from soy.
Oxyphenbutazone: Concurrent administration of oxyphenbutazone and androgens may result in elevated
serum levels of oxyphenbutazone.
Insulin: In diabetic patients, the metabolic effects of androgens may decrease blood glucose and,
therefore, insulin requirements.
Propranolol: In a published pharmacokinetic study of an injectable testosterone product,
administration of testosterone cypionate led to an increased clearance of propranolol in the majority of men
Corticosteroids: The concurrent administration of testosterone with ACTH or corticosteroids may
enhance edema formation; thus, these drugs should be administered cautiously, particularly in patients with cardiac
or hepatic disease.
Drug/Laboratory Test Interactions
Androgens may decrease levels of thyroxin-binding globulin, resulting in decreased total T4 serum levels and
increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical
evidence of thyroid dysfunction.