Athlete Selective Androgen Receptor Modulators Abuse: A Systematic Review

Nikhil Vasireddi, Henrik A. Hahamyan, Heath P. Gould, Andrew J.M. Gregory, Elizabeth B. Gausden, Christopher C. Dodson, James E. Voos, Jacob G. Calcei
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Abstract

Background:Selective androgen receptor modulators (SARMs) are small-molecule compounds that exert agonist and antagonist effects on androgen receptors in a tissue-specific fashion. Because of their performance-enhancing implications, SARMs are increasingly abused by athletes. To date, SARMs have no Food and Drug Administration approved use, and recent case reports associate the use of SARMs with deleterious effects such as drug-induced liver injury, myocarditis, and tendon rupture.Purpose:(1) To provide a comprehensive synthesis of the literature pertaining to SARMs from a sports medicine perspective and (2) to provide a better understanding of the clinical effects, treatment protocols, prevalence, and potential contamination associated with athlete-consumed SARMs.Study Design:Systematic review; Level of evidence, 4.Methods:A systematic review of the English-language literature from PubMed, Cochrane, and Embase databases was performed according to the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines. Articles relevant to SARM clinical outcomes, elimination profiles, contamination, safety profiles, prevalence, and doping control were included.Results:A total of 72 articles from 2003 to 2022 were identified for inclusion. The prevalence of SARM use among athletes is estimated to be 1% to 3%. SARM preclinical and clinical studies reported significant increases in lean body mass and side effects—including bone remodeling, testosterone suppression, and kidney, liver, and prostate enlargement. Thirteen case reports described 15 cases of SARM abuse. All described patients were men, with a median age of 32 years (range, 19-52 years), more than half were identified as athletes (8/15), and all ingested SARMs orally for a mean course of 8 weeks. Five patients described in the case reports explicitly denied “illicit drug use,” implying patients may believe their use to be legal. Athletes most commonly purchased SARMs online, and most of these compounds have been shown to be contaminated with other substances, contributing to adverse effects. Athletes reported consuming SARMs at much higher doses than clinically studied, which may increase the risk of the reported side effects, such as liver injury, impaired insulin sensitivity, cardiovascular events, and tendon damage.Conclusion:The results of this systematic review serve to educate sports medicine clinicians and researchers on how to better identify, diagnose, and treat athlete SARM abuse. SARM use is associated with increased muscle mass, hepatotoxicity, cardiotoxicity, tendon damage, and androgenic side effects throughout the body—including prostate enlargement and serum testosterone suppression. Identifying and treating SARM abuse requires taking a thorough substance and supplement use history with open communication, providing literature-supported patient education, negotiating SARM discontinuation, and performing multidisciplinary treatment of adverse events. Athlete SARM abuse is increasingly widespread and unsafe, and public health oversight bodies should advocate for regulation of these gray-market compounds.
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运动员选择性雄激素受体调节剂的滥用:系统回顾
背景:选择性雄激素受体调节剂(SARMs)是一种小分子化合物,能以组织特异性的方式对雄激素受体发挥激动剂和拮抗剂作用。由于具有提高成绩的作用,sarm越来越多地被运动员滥用。到目前为止,SARMs还没有得到美国食品和药物管理局的批准使用,最近的病例报告将SARMs的使用与药物性肝损伤、心肌炎和肌腱断裂等有害影响联系起来。目的:(1)从运动医学的角度全面综合有关SARMs的文献;(2)更好地了解运动员服用SARMs的临床效果、治疗方案、流行程度和潜在污染。研究设计:系统评价;证据等级,4级。方法:根据PRISMA(系统评价和荟萃分析首选报告项目)指南,对PubMed、Cochrane和Embase数据库的英语文献进行系统评价。纳入了与SARM临床结果、消除概况、污染、安全性概况、患病率和兴奋剂控制相关的文章。结果:2003 - 2022年共纳入72篇文献。运动员中SARM的使用率估计为1%至3%。SARM临床前和临床研究报告了瘦体重的显著增加和副作用,包括骨重塑、睾酮抑制、肾、肝和前列腺肿大。13例病例报告描述了15例SARM滥用。所有描述的患者均为男性,中位年龄为32岁(范围19-52岁),超过一半的患者为运动员(8/15),所有患者口服SARMs平均疗程为8周。病例报告中描述的五名患者明确否认“非法使用药物”,这意味着患者可能认为他们的使用是合法的。运动员最常在网上购买sarm,这些化合物中的大多数已被证明与其他物质污染,导致不利影响。运动员报告服用SARMs的剂量比临床研究高得多,这可能会增加报道的副作用的风险,如肝损伤、胰岛素敏感性受损、心血管事件和肌腱损伤。结论:本系统综述的结果有助于教育运动医学临床医生和研究人员如何更好地识别、诊断和治疗运动员SARM滥用。SARM的使用与肌肉量增加、肝毒性、心脏毒性、肌腱损伤和全身雄激素副作用(包括前列腺增大和血清睾酮抑制)有关。识别和治疗SARM滥用需要全面的物质和补充使用历史,开放的沟通,提供文献支持的患者教育,协商SARM停药,并对不良事件进行多学科治疗。运动员滥用SARM越来越普遍和不安全,公共卫生监督机构应倡导对这些灰色市场化合物进行监管。
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