SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMs) IN THE CONTEXT OF DOPING

Abstract

Selective androgen receptor modulators (SARMs) are substances of increasingly interest in the medical area due to the anabolic effect on muscle and bone tissue. Even if they aren`t yet introduced into therapy, they are in various stages of experimental and clinical research for pathologies involving catabolic states in protein metabolism. These molecules manage to dissociate the anabolic effect from the virilising effect, compared with androgenic hormones, due to the non-steroidal structure that they detain. Having this pharmacological advantage, besides the possibility of being orally administered, these substances are used illegally by athletes and bodybuilders. It is important to note that SARMs are prohibited for performance athletes by World Anti-Doping Agency (WADA), but the concern is that they can be easily obtained from various uncertain sources. Moreover, their pharmacotoxicological profile is not clearly known, so their chronic administration, in high doses, represents a possible risk for the health. RezumatModulatorii selectivi ai receptorilor androgenici (SARM) sunt substanțe de interes crescut în aria medicală datorită efectelor anabolice la nivelul țesutului muscular și osos. Chiar dacă nu sunt introduse încă în terapie, sunt incluse în diverse stadii de cercetare experimentală și clinică pentru tratarea patologiilor cu stări catabolice în metabolismul proteic. Aceste molecule reușesc să disocieze efectul anabolic de cel virilizant, în comparație cu hormonii androgeni, datorită structurii lor nesteroidice. Deținând acest avantaj farmacologic, pe lângă posibilitatea de a fi administrate oral, aceste substanțe se utilizează în scop ilicit de către atleți și culturiști. Este important de menționat faptul că aceste substanțe sunt interzise sportivilor de performanță de către World-Anti Doping Agency (WADA), dar totuși pot fi ușor de procurat din diverse surse nesigure. În plus, profilul lor farmacotoxicologic nu este suficient cunoscut, deci administrarea cronică, în doze mari, reprezintă un posibil risc pentru sănătate.

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“…Although there are a lot of studies on LC-MS or GC-MS (gas chromatography-mass spectrometry), it seems that they should still be optimized to avoid the false positive results due to the structural similarity of active metabolites of SARMs with androgen receptor antagonists such as flutamide (Perrenoud et al 2016). There was a case report regarding an in-competition female athlete urine sample, in which metabolites of S-4 were detected, proving that the athlete used andarine for better physical performance (Miklos et al 2018).…”

A new trend in use of performance enhancing drugs in CrossFit®

“…Jak se ukazuje, SARM dokáží působit velmi podobně a v krátkodobém měřítku jsou srovnatelné s externě dodávaným testosteronem (Basaria et al, 2013). Problémem SARM se stává jejich dobrá dostupnost (pomocí e-shopů), orální podání (není nutná injekční aplikace) a také relativně nízké vedlejší efekty (v porovnání s jinými steroidními látkami) (Miklos, 2018). Jedná se však o černý trh, kde se nelze spoléhat na kvalitu produktu.…”

Selective Androgen Receptor Modulators (SARMs) in the World of Sports

“…Several studies have been conducted on selective androgen receptor modulators and their effect on the human body. However, SARMs' true potential and risks are not fully understood nor studied [4,5,6,7,8,9].…”