Wilson J D, Griffin J E
Metabolism. 1980 Dec;29(12):1278-95. doi: 10.1016/0026-0495(80)90159-6.
Because testosterone is rapidly metabolized by the liver, it is necessary either to administer androgens by injection in the form of testosterone esters that are absorbed slowly into the circulation or to administer by mouth derivatives that are slowly metabolized by the liver. The later derivatives, however, have deleterious side effects that limit their usefulness. Long-acting parenteral androgen esters are the treatment of choice in the replacement therapy of male hypogonadism. Because these esters must be hydrolyzed to the free hormone prior to exerting their cellular actions the effectiveness of therapy can be monitored by following plasma testosterone levels. All known effects of the endogenous hormone can be duplicated except for the induction and maintenance of normal spermatogenesis. Androgens have been tried in a variety of clinical situations other than male hypogonadism in the hopes that the nonvirilizing actions would outweigh any detectable side effects. The only disorders in which a salutary effect has been documented are hereditary angioneurotic edema and some patients with anemia due to failure off the bone marrow.
由于睾酮会被肝脏迅速代谢,因此有必要通过注射睾酮酯的形式来给予雄激素,睾酮酯会缓慢吸收进入循环系统,或者口服肝脏代谢缓慢的衍生物。然而,后一种衍生物具有有害的副作用,限制了它们的用途。长效肠胃外雄激素酯是男性性腺功能减退替代治疗的首选。由于这些酯在发挥细胞作用之前必须水解为游离激素,因此可以通过监测血浆睾酮水平来监测治疗效果。除了诱导和维持正常精子发生外,内源性激素的所有已知作用都可以复制。除了男性性腺功能减退外,雄激素还被用于多种临床情况,希望其非男性化作用能超过任何可检测到的副作用。唯一有文献记载有益效果的疾病是遗传性血管性水肿和一些因骨髓功能衰竭导致贫血的患者。