阿那曲唑的药理作用及临床应用

The Pharmacological Actions and Clinical Use of Anastrozole

阿那曲唑是－种新型高选择性的非甾体类芳香酶抑制剂，临床用于绝经后妇女晚期乳腺癌的治疗。它通过阻断绝经后妇女内源性雌激素的合成，降低体内循环雌激素水平，达到有效阻滞肿瘤生长，甚至导致癌细胞死亡的作用。本品口服后吸收迅速且完全，消除半率期较长（３０－５０ｈ），每日只需口服一次（１ｍｇ）即可产生最大的雌二醇抑制作用，且耐受性较好。本文主要对阿那曲唑的药理作用机理、药代动力学和临床应用进展等进行了介绍。

Anastrozole is a new, highly selective nonsteroidal aromatase inhibitor indicated for the endocrine treatment of postmenopausal women with advanced breast cancer. In postmenopausal women, anastrozole prevent the synthesis of estrogens and significantly reduced plasma estrogen levels, and this has been associated with tumour regression in patients with estrogen-dependent breast cancer. Absorption of anastrozole was rapid and virtually complete after oral administration. The 1 mg per day of anastrozole is highly selective and well tolerated by patients. It has a terminal half life (30-50 h) long enough to provide for once- daily dosing and this dose produces the maximum detectable estradiol suppression. In this paper, we reviewed its mechanism, pharmacokinetics and clinical use.