Pavlatos A M, Fultz O, Monberg M J, Vootkur A
Northside Family Medicine, Chicago, Illinois 60659-4120, USA.
Clin Ther. 2001 Jun;23(6):789-801; discussion 771. doi: 10.1016/s0149-2918(01)80070-9.
Oxymetholone (17beta-hydroxy-2-[hydroxymethylene]-17-methyl-5alpha-androstan-3-one) is a 17alpha-alkylated anabolic-androgenic steroid and a synthetic derivative of testosterone. It has been approved by the US Food and Drug Administration for the treatment of anemias caused by deficient red cell production.
This review summarizes the pharmacokinetics, current and future clinical applications, and adverse effects of oxymetholone. Relevant studies were identified using a search of MEDLINE through March 2001, supplemented by conference abstracts and presentations.
Because of its anabolic properties, oxymetholone has been studied for the treatment of HIV-associated wasting, antithrombin III deficiency, pediatric growth impairment, and damaged myocardium, with varying degrees of success. Hepatotoxicity is a major adverse effect associated with the use of oxymetholone, with cholestatic jaundice the most important hepatic side effect. Less common hepatic side effects associated with the use of anabolic-androgenic steroids include peliosis hepatis and formation of hepatic tumors. All anabolic-androgenic steroids can cause androgenic side effects, including acne, hirsutism, hair loss, clitoral/phallic enlargement, vocal changes, erectile tissue stimulation, gynecomastia, amenorrhea, and changes in libido and sexual potency.
As is the case with many anabolic-androgenic steroids, few pharmacokinetic and tolerability studies were performed before oxymetholone's approval in the 1960s. It has proved, however, to be an appropriate treatment choice for selected patients with anemia, if carefully monitored.
羟甲烯龙（17β - 羟基 - 2 - [羟基亚甲基] - 17 - 甲基 - 5α - 雄甾烷 - 3 - 酮）是一种17α - 烷基化的合成代谢雄激素类固醇，为睾酮的合成衍生物。它已被美国食品药品监督管理局批准用于治疗因红细胞生成不足引起的贫血。
本综述总结了羟甲烯龙的药代动力学、当前及未来的临床应用以及不良反应。通过检索截至2001年3月的MEDLINE数据库，并辅以会议摘要和报告来确定相关研究。
由于其合成代谢特性，羟甲烯龙已被研究用于治疗与艾滋病相关的消瘦、抗凝血酶III缺乏、儿童生长发育障碍及心肌损伤，取得了不同程度的成功。肝毒性是与使用羟甲烯龙相关的主要不良反应，胆汁淤积性黄疸是最重要的肝脏副作用。与使用合成代谢雄激素类固醇相关的较不常见的肝脏副作用包括肝紫癜和肝肿瘤形成。所有合成代谢雄激素类固醇均可引起雄激素样副作用，包括痤疮、多毛症、脱发、阴蒂/阴茎增大、声音改变、勃起组织刺激、男性乳房发育、闭经以及性欲和性功能改变。
与许多合成代谢雄激素类固醇一样，羟甲烯龙在20世纪60年代获批之前几乎没有进行药代动力学和耐受性研究。然而，如果仔细监测，它已被证明是某些贫血患者的合适治疗选择。
