Testosterone therapy in men: Clinical and pharmacological perspectives

Abstract

There is increasing evidence that androgen therapy in men may be effectively applied in several conditions to improve well being and health. Classical indications for androgen therapy in males are represented by primary or secondary hypogonadism, delayed puberty, aplastic anemia and that secondary to chronic renal failure, protein wasting diseases such as trauma, burns, tumors and infectious diseases. Androgen innovating applications in men are represented by aging and visceral obesity associated with the metabolic syndrome. In addition, it is clear that appropriate testosterone treatment can be adequately used in male contraception, provided spermatogenesis is abolished and tolerability is adequate. Due to unphysiological hormone levels achieved by currently available testosterone preparations, new delivery systems have been produced to achieve more physiological and sustained hormone levels and improve tolerability and action at the levels of target tissues. Some of them are now available in several countries and new formulas are under development.

Possible role of leptin in hypoandrogenicity in patients with systemic lupus erythematosus and rheumatoid arthritis

“…Intervention studies with androgens show that correction of relative hypogonadism in men with visceral obesity and other manifestations of the metabolic syndrome decreases the abdominal fat mass and reverses glucose intolerance. 28 In the obese state, the fat tissue hormone leptin was found to have a dominant role for hypoandrogenicity because leptin inhibits gonadal androgen secretion. [29][30][31] Furthermore, a recent study in bovine adrenocortical cells demonstrated leptin induced inhibition of 17a-hydroxylase P450 mRNA expression, 32 which is the key enzyme for androgen production (fig 1).…”

Avaliação dos níveis séricos de testosterona em pacientes com síndrome da apneia obstrutiva do sono

“…Total and free testosterone levels fall in obese males -as body weight and fat increase -because of decreased globulin-bound hormone synthesis and altered activity of the aromatase system in peripheral tissues. [39][40][41] Prior studies have shown that serum levels of testosterone are inversely correlated with the severity of OSAHS (AHIs); such altered levels result from fragmented sleep and decreased oxygenation, which are known inhibitors of testosterone production. 27,33 A cross-sectional study of 225 male subjects undergoing polysomnography showed that the severity of OSAHS correlated significantly with globulin-bound sex hormones, decreased levels of total testosterone, and free testosterone.…”

Evolution of delivery systems for testosterone administration

“…Supraphysiologic levels of total testosterone with low levels of free testosterone, erratic absorption, hepatic toxicity, and high cost have made these agents (methyltestosterone, fluoxymesterone) very unattractive; they have been discontinued in Europe but are still available in the United States [2][3][4]. Because the alkyl groups are not removed before the hormone acts in target cells and excretion and degradation products contain the intact 17-alpha alkyl groups, serum testosterone cannot be monitored to gauge effectiveness of therapy [2][3][4]. Furthermore, oral androgen may have an undesirable effect on serum lipid Hypogonadism, especially in aging men, is being identified and treated more frequently.…”

“…The beneficial effects of ART for hypogonadism include improvements in sexual function (erection and libido), bone density, muscle mass, hematopoiesis, cognition, and cardiovascular function. Potential adverse effects of ART center on benign prostatic hypertrophy and prostate cancer [1][2][3][4].…”

“…Testosterone plays an essential role in normal male development and in the maintenance of many male characteristics, including muscle mass and strength, bone density, and sexual function [1][2][3][4]. Androgen replacement therapy (ART) is indicated for androgen deficiency caused by testicular or pituitary disorders, which may be hereditary or acquired.…”