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As of November 2016update, testosterone is available in Canada in the form of topical gels (AndroGel, Testim), topical solutions (Axiron), transdermal patches (Androderm), and intranasal gels (Natesto). The pharmacokinetics of testosterone, including its bioavailability, circulating testosterone levels, metabolism, biological half-life, and other parameters, differ by route of administration. These metabolites, along with estradiol, may be involved in a number of the effects of testosterone in the brain, including its antidepressant, anxiolytic, stress-relieving, rewarding, and pro-sexual effects. Estrogens can reduce the effects of testosterone by increasing the hepatic production and in turn circulating levels of sex hormone-binding globulin (SHBG), a carrier protein that binds to and occupies androgens like testosterone and DHT, and thereby reducing free concentrations of these androgens. As only a very small fraction of testosterone is converted into estradiol, this does not affect testosterone levels, but it can prevent estrogenic side effects like gynecomastia that can occur when testosterone is administered at relatively high dosages.
Signs and symptomshave included enlargement of the penis or clitoris, development of pubic hair,increased erections and libido, aggressive behavior, and advanced bone age. The concurrent use of testosterone with corticosteroidsmay result in increased fluid retention and requires careful monitoringparticularly in patients with cardiac, renal or hepatic disease. In diabetic patients, the metaboliceffects of androgens may decrease blood glucose and, therefore, may necessitatea decrease in the dose of anti-diabetic medication. In at leastone reported case, the reporter considered the possibility of secondaryexposure from items such as the testosterone gel user's shirts and/or otherfabrics, such as towels and sheets see WARNINGS AND PRECAUTIONS. Signs and symptoms of these reported cases haveincluded enlargement of the clitoris (with surgical intervention) or of the penis, development of pubic hair, increased erections and libido, aggressivebehavior, and advanced bone age. Cases of secondary exposure to testosterone resulting invirilization of children have been reported in postmarketing surveillance oftestosterone gel products.
These included decreased levels of total cholesterol, triglycerides, and high-density lipoprotein (HDL) cholesterol, and increased levels of low-density lipoprotein (LDL) cholesterol. Testosterone therapy is effective in the short-term for the treatment of hypoactive sexual desire disorder (HSDD) in women. To take advantage of its virilizing effects, testosterone, often shortened to T, is administered to transgender men and other transmasculine individuals as part of masculinizing hormone therapy, titrated to clinical effect with a "target level" of the average male's testosterone level. This treatment is referred to as hormone replacement therapy (HRT), or alternatively, and more specifically, as testosterone replacement therapy (TRT) or androgen replacement therapy (ART). Serious side effects may include liver toxicity, heart disease, and behavioral changes. Common side effects of testosterone include acne, swelling, and breast enlargement in men.
Testosterone gel should be promptly discontinued until thecause of virilization has been identified. Changes in insulin sensitivity or glycemic control mayoccur in patients treated with androgens. Because the reactionsare reported voluntarily from a population of uncertain size, it is not alwayspossible to reliably estimate their frequency or establish a causalrelationship to drug exposure. The patient should avoid swimming or showering or washingthe administration site for a minimum of 2 hours after application seeCLINICAL PHARMACOLOGY. In order to prevent transfer to another person, clothingshould be worn to cover the application sites. Hands should be washed thoroughly with soap and waterafter Vogelxo has been applied. Table 2 has specific dosing guidelines for whenthe metered pump is used.