Kuhn Cynthia M
Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA.
Recent Prog Horm Res. 2002;57:411-34. doi: 10.1210/rp.57.1.411.
The term "anabolic steroids" refers to testosterone derivatives that are used either clinically or by athletes for their anabolic properties. However, scientists have questioned the anabolic effects of testosterone and its derivatives in normal men for decades. Most scientists concluded that anabolic steroids do not increase muscle size or strength in people with normal gonadal function and have discounted positive results as unduly influenced by positive expectations of athletes, inferior experimental design, or poor data analysis. There has been a tremendous disconnect between the conviction of athletes that these drugs are effective and the conviction of scientists that they aren't. In part, this disconnect results from the completely different dose regimens used by scientists to document the correction of deficiency states and by athletes striving to optimize athletic performance. Recently, careful scientific study of suprapharmacologic doses in clinical settings - including aging, human immunodeficiency virus, and other disease states - supports the efficacy of these regimens. However, the mechanism by which these doses act remains unclear. "Anabolism" is defined as any state in which nitrogen is differentially retained in lean body mass, either through stimulation of protein synthesis and/or decreased breakdown of protein anywhere in the body. Testosterone, the main gonadal steroid in males, has marked anabolic effects in addition to its effects on reproduction that are easily observed in developing boys and when hypogonadal men receive testosterone as replacement therapy. However, its efficacy in normal men, as during its use in athletes or in clinical situations in which men are eugonadal, has been debated. A growing literature suggests that use of suprapharmacologic doses can, indeed, be anabolic in certain situations; however, the clear identification of these situations and the mechanism by which anabolic effects occur are unclear. Furthermore, the pharmacology of "anabolism" is in its infancy: no drugs currently available are "purely" anabolic but all possess androgenic properties as well. The present review briefly recapitulates the historic literature about the androgenic/anabolic steroids and describes literature supporting the anabolic activity of these drugs in normal people, focusing on the use of suprapharmacologic doses by athletes and clinicians to achieve anabolic effects in normal humans. We will present the emerging literature that is beginning to explore more specific mechanisms that might mediate the effects of suprapharmacologic regimens. The terms anabolic/androgenic steroids will be used throughout to reflect the combined actions of all drugs that are currently available.
“合成代谢类固醇”一词指的是睾酮衍生物,临床上或运动员会因其合成代谢特性而使用。然而,几十年来科学家们一直质疑睾酮及其衍生物对正常男性的合成代谢作用。大多数科学家得出结论,合成代谢类固醇不会增加性腺功能正常者的肌肉大小或力量,并认为积极结果是受到运动员的积极预期、较差的实验设计或数据分析不当的过度影响。运动员坚信这些药物有效,而科学家坚信它们无效,二者之间存在巨大脱节。部分原因在于,科学家用于记录缺乏状态纠正情况的剂量方案与运动员为优化运动表现而使用的剂量方案完全不同。最近,在临床环境中对超药理剂量进行的仔细科学研究——包括衰老、人类免疫缺陷病毒及其他疾病状态——支持了这些方案的有效性。然而,这些剂量发挥作用的机制仍不清楚。“合成代谢”被定义为通过刺激蛋白质合成和/或减少体内任何部位蛋白质分解,使氮在瘦体重中差异保留的任何状态。睾酮是男性主要的性腺类固醇,除了对生殖的影响外,在发育中的男孩以及性腺功能减退的男性接受睾酮替代治疗时,很容易观察到其具有显著的合成代谢作用。然而,其在正常男性中的功效,比如在运动员使用期间或男性性腺功能正常的临床情况下,一直存在争议。越来越多的文献表明,在某些情况下使用超药理剂量确实可以促进合成代谢;然而,这些情况的明确界定以及合成代谢作用发生的机制尚不清楚。此外,“合成代谢”的药理学尚处于起步阶段:目前没有任何可用药物是“纯粹”的合成代谢药物,它们都还具有雄激素特性。本综述简要回顾了关于雄激素/合成代谢类固醇的历史文献,并描述了支持这些药物在正常人中具有合成代谢活性的文献,重点关注运动员和临床医生使用超药理剂量在正常人中实现合成代谢作用的情况。我们将展示新兴文献,这些文献开始探索可能介导超药理方案作用的更具体机制。 throughout 将始终使用合成代谢/雄激素类固醇这一术语来反映目前所有可用药物的综合作用。