部份中文米非司酮处方资料（仅供参考）
【商品名】Korlym
【英文名】mifepristone
【中文名】米非司酮
【制造商】CorceptTherapeutics
药品简介
批准日期：2012年2月17日 公司：CorceptTherapeutics
KORLYM(米非司酮[mifepristone])300毫克片剂 仅供口服使用
美国初步批准2000
警告:
终止妊娠查看完整的盒装警告的完整处方信息。
米非司酮具有强大的antiprogestational作用, 并将导致终止妊娠。因此, 怀孕必须在KORLYM治疗开始前被排除在外, 或者如果治疗在生殖潜能的雌性中被中断超过14天。
最近的重大变化
剂量和管理：05/2017
警告和预防措施：05/2017
适应症和用法
KORLYM(米非司酮) 是一种皮质醇受体阻滞剂, 用于控制成人内源性库欣综合征 (2型糖尿病或葡萄糖不耐受) 患者的高血糖, 并有失败的手术或不是手术的候选者.
使用的重要限制:
不用于治疗2型糖尿病与内源性库欣综合征无关。
剂量和管理
每日口服一餐。
建议的起始剂量为每天300毫克。
根据临床反应和耐受性, 剂量可增加300毫克, 最多为1200年毫克, 每天一次。不要超过20毫克/千克每天。
肾脏损害: 每日不超过600毫克。
轻度至中度肝损害: 每日不超过600毫克。不要在严重的肝脏损伤中使用。
伴随管理以强的 CYP3A 抑制剂: 每日不超过600毫克。
剂型和强度
片剂: 300毫克
禁忌
怀孕
辛伐他汀、洛伐他汀、CYP3A 基底狭窄治疗范围的应用
同时使用长期皮质类固醇
有不明原因阴道出血病史的妇女
子宫内膜增生的妇女与异型或子宫内膜癌
警告和预防措施
肾上腺功能不全: 患者应密切监测肾上腺功能不全的体征和症状。
低钾血症: 在治疗前应纠正低钾血症。
阴道出血和子宫内膜改变: 妇女可能会经历子宫内膜增厚或意外阴道出血。如果病人也有出血紊乱或抗凝治疗, 请慎用。
qt间期延长: 避免使用qt间隔延长药物, 或钾通道变异患者导致长QT间隔。
使用强CYP3A抑制剂: 伴随使用可以增加米非司酮血浆水平。仅在必要时使用, 并限制米非司酮剂量为600毫克。
不良反应
库欣综合征最常见的不良反应(≥ 20%): 恶心, 疲劳, 头痛, 血钾减少, 关节痛, 呕吐, 周围水肿, 高血压, 头晕, 食欲减退, 子宫内膜肥大.
药物相互作用
CYP3A 代谢的药物: 在使用KORLYM时用最低剂量 CYP3A 代谢的药物。
CYP3A 抑制剂: KORLYM使用强CYP3A抑制剂时应慎用。将米非司酮剂量限制为每天600毫克, 使用强 CYP3A 抑制剂。
CYP3A 诱导剂: 不要使用KORLYM与CYP3A诱导剂。
CYP2C8/2C9 代谢的药物: 使用最低剂量的CYP2C8/2C9基质时, 使用与KORLYM。
CYP2B6 代谢的药物: 使用 KORLYM 应慎用盐酸和依法韦仑。
荷尔蒙避孕药: 不要用KORLYM。
在特定人群中使用
哺乳母亲: 停止服药或停止护理。
如何提供/存储和处理
KORLYM 是作为一个淡黄色到黄色, 涂膜, 椭圆形的片剂 debossed 与 "Corcept" 一侧和 "300"。每个片剂含有300毫克米非司酮。KORLYM 片可在28片 (NDC 76346-073-01) 瓶和280片 (NDC 76346-073-02) 瓶中使用。
贮存在控制室温下, 25 °c (77 °F);允许15到30° C (59-86 °F) 的短途旅行。[见 USP 控制室温]
修订: 5/2017
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=542f3fae-8bc8-4f00-9228-e4b66c9ad6a9

Korlym (mifepristone) 300mg Tablets

KORLYM

Indication(s):

To control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing’s syndrome who have type 2 diabetes or glucose intolerance and have failed surgery or are not candidates for surgery.

Pharmacology:

Korlym blocks the glucocorticoid receptor type II (GR-II) to which cortisol normally binds. By blocking this receptor, Korlym inhibits the effects of excess cortisol in Cushing’s syndrome patients.

Clinical Trials:

An uncontrolled, open-label, 24-week, multicenter clinical study was conducted to evaluate the safety and efficacy of Korlym in the treatment of endogenous Cushing’s syndrome. Patients belonged to one of two cohorts: a “diabetes” cohort (29 patients, 26 with type 2 diabetes and 3 with glucose intolerance), and a “hypertension” cohort (21 patients). Efficacy was evaluated separately in the two cohorts. Korlym was started in all patients at a dose of 300mg once a day. The study protocol allowed an increase in dose to 600mg after 2 weeks, and then by additional 300mg increments every 4 weeks to a maximum of 900mg/day for patients <60kg, or 1200mg/day for patients >60kg, based on clinical tolerance and clinical response. Patients in the diabetes cohort underwent standard oral glucose tolerance tests at baseline and periodically during the trial. The primary efficacy analysis for the diabetes cohort was an analysis of responders. A responder was defined as a patient who had a ≥25% reduction from baseline in glucose AUC. Mean HbA1c was 7.4% in the 24 patients with HbA1c values at baseline and Week 24. For these 24 patients mean reduction in HbA1c was 1.1% (95% CI -1.6, -0.7) from baseline to the end of the trial.

There were no changes in mean systolic and diastolic blood pressures at the end of the trial relative to baseline in the modified intent-to-treat group (n=21).

Legal Classification:

Rx

Adults:

Swallow whole. Take with a meal. Initially 300mg once daily; may increase in 300mg increments every 2–4 weeks to max 1200mg once daily; do not exceed 20mg/kg/day. If interrupted, re-start at 300mg and titrate to dose lower than the one that resulted in treatment interruption. Renal or mild to moderate hepatic impairment: max dose 600mg. Severe hepatic impairment: not recommended. Concomitant strong CYP3A inhibitors (see Interactions): max 300mg/day.

Children:

Not recommended.

Contraindication(s):

Pregnancy (Cat.X). Concomitant simvastatin, lovastatin, CYP3A substrates with narrow therapeutic ranges (eg, cyclosporine, ergots, fentanyl, pimozide, quinidine, sirolimus, tacrolimus). Concomitant systemic corticosteroids for serious medical conditions or illnesses (eg, immunosuppression after organ transplantation). History of unexplained vaginal bleeding. Endometrial hyperplasia with atypia or endometrial carcinoma.

Warnings/Precautions:

Pregnancy must be excluded before initiating therapy and if treatment is interrupted for >14 days in females of reproductive potential. Prevent pregnancy during and for 1 month after stopping treatment (use non-hormonal contraceptive). Monitor for adrenal insufficiency; if suspected, discontinue treatment immediately and give glucocorticoids; may resume at a lower dose after resolution. Correct hypokalemia prior to initiating therapy; measure serum potassium 1–2 weeks after starting or increasing dose, then periodically. Women with hemorrhagic disorders or are receiving concurrent anticoagulant therapy. Autoimmune disorders. Heart failure. Coronary vascular disease. Monitor for Pneumocystis jiroveci infection. Nursing mothers: not recommended.

Interaction(s):

Potentiated by strong CYP3A inhibitors (eg, ketoconazole, itraconazole, nefazodone, ritonavir, nelfinavir, indinavir, atazanavir, amprenavir, fosamprenavir, boceprevir, clarithromycin, conivaptan, lopinavir, nefazodone, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, voriconazole). Caution with moderate CYP3A inhibitors (eg, amprenavir, aprepitant, atazanavir, ciprofloxacin, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, imatinib, verapamil). Avoid concomitant CYP3A inducers (eg, rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, St. John’s wort). May potentiate drugs metabolized by CYP2C8/2C9 (eg, fluvastatin, NSAIDs, warfarin, repaglinide); monitor, use smallest effective dose. May potentiate drugs metabolized by CYP2B6 (eg, bupropion, efavirenz). Antagonizes hormonal contraceptives.

Adverse Reaction(s):

Nausea, fatigue, headache, decreased blood potassium, arthralgia, vomiting, peripheral edema, hypertension, dizziness, decreased appetite, endometrial hypertrophy; QT prolongation, hypokalemia, reduced HDL-C, elevated TSH.

How Supplied:

Tabs—28, 280