Swegle John M, Kelly Michael W
College of Pharmacy, The University of Iowa, Mercy Family Medicine Residency Program, Mason City, IA 50401-2859, USA.
Ann Pharmacother. 2004 May;38(5):874-81. doi: 10.1345/aph.1D462. Epub 2004 Mar 16.
To review the pharmacology, pharmacokinetics, efficacy, and safety of tibolone in the treatment of menopausal symptoms and the prevention of osteoporosis.
Information was obtained from a MEDLINE search (1966-July 2003) and from Organon International. The bibliographies of reviewed literature were searched for additional studies.
Studies and review articles evaluating tibolone were evaluated. Since tibolone has been available for many years in Europe and has an extensive literature base, this review emphasizes information from studies published after 1995.
Tibolone possesses estrogenic activity and is effective for treating the symptoms and osteoporosis associated with menopause. While the impact of tibolone on the risk of breast cancer or cardiovascular and thromboembolic events is not well defined, its unique pharmacologic profile may provide a safer alternative to traditional hormone replacement therapy. Although widely used for many years in other countries, tibolone has not been approved for use in the US.
Results of recent trials have led to questions regarding the safety of established hormone replacement therapies in peri- and postmenopausal women. Tibolone appears to be an attractive alternative to these traditional regimens. Additional studies will determine whether the promise of increased safety with tibolone will be realized.
综述替勃龙在治疗更年期症状及预防骨质疏松症方面的药理作用、药代动力学、疗效和安全性。
从MEDLINE检索数据库（1966年至2003年7月）及欧加农国际公司获取信息。查阅已发表文献的参考文献以寻找更多研究。
对评估替勃龙的研究及综述文章进行评价。由于替勃龙在欧洲已上市多年且有大量文献基础，本综述重点关注1995年后发表的研究中的信息。
替勃龙具有雌激素活性，对治疗与更年期相关的症状及骨质疏松症有效。虽然替勃龙对乳腺癌风险或心血管及血栓栓塞事件的影响尚不明确，但其独特的药理特性可能为传统激素替代疗法提供更安全的选择。尽管替勃龙在其他国家已广泛使用多年，但在美国尚未获批使用。
近期试验结果引发了对围绝经期和绝经后妇女既定激素替代疗法安全性的质疑。替勃龙似乎是这些传统治疗方案的一个有吸引力的替代选择。更多研究将确定替勃龙提高安全性的前景是否能够实现。
