Oregon Health & Science University, Portland, OR 97239, USA.
Endocr Pract. 2013 Mar-Apr;19(2):313-26. doi: 10.4158/EP12149.RA.
Cushing's syndrome (CS) is a serious endocrine disorder caused by prolonged exposure to high cortisol levels. Initial treatment of this condition is dependent upon the cause, but is generally surgical. For patients whose hypercortisolism is not cured by surgery, medical therapy is often required. Drugs that have typically been used for CS medical therapy act by decreasing cortisol levels. Mifepristone is a glucocorticoid receptor antagonist now available for use in patients with CS. Unlike other agents, mifepristone does not decrease cortisol levels, but directly antagonizes its effects. Our objective is to review the pharmacology and clinical use of this novel agent and to discuss detailed guidance on the management of CS patients treated with mifepristone.
We review the literature regarding mifepristone use in CS and recently published clinical trial data. Detailed information related to clinical assessment of mifepristone use, potential drug interactions, drug initiation and dose titration, and monitoring of drug tolerability are provided.
Clinical trial data have shown that mifepristone improves glycemic control and blood pressure, causes weight loss and a decrease in waist circumference, lessens depression, and improves overall wellbeing. However, adverse effects include adrenal insufficiency, hypokalemia, and endometrial thickening with vaginal bleeding. These findings are supported by the earlier literature case reports.
This article provides a review of the pharmacology and clinical use of mifepristone in Cushing's syndrome, as well as detailed guidance on the management of patients treated with this novel agent.
库欣综合征（CS）是一种由长期暴露于高皮质醇水平引起的严重内分泌紊乱。这种疾病的初始治疗取决于病因，但通常是手术。对于那些手术不能治愈的皮质醇过多的患者，通常需要药物治疗。用于 CS 药物治疗的药物通常通过降低皮质醇水平起作用。米非司酮是一种现已可用于 CS 患者的糖皮质激素受体拮抗剂。与其他药物不同，米非司酮不会降低皮质醇水平，而是直接拮抗其作用。我们的目的是回顾该新型药物的药理学和临床应用，并讨论详细的 CS 患者米非司酮治疗管理指南。
我们回顾了关于 CS 中米非司酮使用的文献和最近发表的临床试验数据。提供了与米非司酮使用的临床评估、潜在药物相互作用、药物起始和剂量滴定以及药物耐受性监测相关的详细信息。
临床试验数据表明，米非司酮可改善血糖控制和血压，减轻体重和腰围，减轻抑郁，改善整体健康状况。然而，不良反应包括肾上腺皮质功能不全、低钾血症和子宫内膜增厚伴阴道出血。这些发现得到了更早的文献病例报告的支持。
本文综述了米非司酮在库欣综合征中的药理学和临床应用，并提供了详细的治疗患者管理指南。
