Medicinal Use of Testosterone and Related Steroids Revisited

Abstract

Testosterone derivatives and related compounds (such as anabolic-androgenic steroids—AAS) are frequently misused by athletes (both professional and amateur) wishing to promote muscle development and strength or to cover AAS misuse. Even though these agents are vastly regarded as abusive material, they have important pharmacological activities that cannot be easily replaced by other drugs and have therapeutic potential in a range of conditions (e.g., wasting syndromes, severe burns, muscle and bone injuries, anemia, hereditary angioedema). Testosterone and related steroids have been in some countries treated as controlled substances, which may affect the availability of these agents for patients who need them for therapeutic reasons in a given country. Although these agents are currently regarded as rather older generation drugs and their use may lead to serious side-effects, they still have medicinal value as androgenic, anabolic, and even anti-androgenic agents. This review summarizes and revisits the medicinal use of compounds based on the structure and biological activity of testosterone, with examples of specific compounds. Additionally, some of the newer androgenic-anabolic compounds are discussed such as selective androgen receptor modulators, the efficacy/adverse-effect profiles of which have not been sufficiently established and which may pose a greater risk than conventional androgenic-anabolic agents.

The Prevalence of Hypogonadism and the Effectiveness of Androgen Administration on Body Composition in HIV-Infected Men: A Meta-Analysis

“…The relevance of hypogonadism in HIV settings has progressively increased in recent years, since it has been suggested as a marker of poor health status and frailty in the general population [6,7] and in HIV subjects [5,8]. Te and each related derivative compound (such as anabolic-androgenic steroids) [9] are used and, in terms of androgen anabolic properties, an involvement of Te reduction in HIV-related changes in body composition has been investigated [10]. Indeed, a variable degree of body composition alterations is described in HIV populations, such as subcutaneous lipoatrophy, increased amounts of visceral adipose tissue and wasting syndrome (WS), defined as an involuntary 10% weight loss in one year or a 5% weight loss in six months [11].…”

“…Therefore, WS remains a relevant medical problem, considering its strict correlation with several metabolic comorbidities, reduced global performance status and impaired survival [12,[14][15][16][17][18]. Since Te and/or Te-derived analogues are steroid molecules that are largely known to promote muscle mass gain [9,19,20], it is not surprising that exogenous androgenic treatment constituted an attractive therapeutic option for preventing WS in HIV populations. Hence, for many years, androgen treatments have been proposed in HIV settings, even in the absence of biochemical hypogonadism, for the contrasting of several disease-associated conditions, such as muscle mass lost, reduced bone mineral density, impaired mood and poor quality of life [21][22][23][24][25][26].…”

Androgens and Parkinson's Disease: A Review of Human Studies and Animal Models

“…Moreover, although testosterone derivatives and related compounds (such as anabolic-androgenic steroids) are frequently misused by athletes, they offer possibilities that could be helpful in PD neurodegeneration condition (reviewed Ref. 103 ). Selective androgen receptor modulators (SARMs) are compounds developed to be tissue-selective androgen receptor ligands.…”

Advances in the Determination of Anabolic-Androgenic Steroids: From Standard Practices to Tailor-Designed Multidisciplinary Approaches

“…Particularly alarming, however, is a tendency to engage in criminal activities [ 13 ], along with the growing number of case reports of fatal medical conditions connected to the misuse of AASs [ 14 , 15 , 16 , 17 , 18 ], potentially resulting in sudden deaths [ 19 , 20 , 21 , 22 ]. It is also worth mentioning that, on the other hand, AASs have therapeutic potential, and cannot be easily replaced by other drugs in a range of conditions such as wasting syndromes, severe burns, muscle and bone injuries, anemia, and hereditary angioedema [ 23 ].…”