部份中文奥贝胆酸处方资料（仅供参考）
英文名：obeticholic acid
商品名：Ocaliva film-coated tablets
中文名：奥贝胆酸薄膜片
生产商：Intercept Pharma
药品简介
2016年12月，肝病新药Ocaliva（obeticholic acid）获欧盟批准，用于慢性肝病原发性胆汁性胆管炎（PBC）患者常规治疗药物.这也欧盟国内的患者20年来获得了一种新的治疗方案。
Ocaliva（obeticholic acid，OCA）是Intercept开发的一款创新药物法尼酯X受体（FXR）激动剂，这是一种人类胆汁酸模拟物，目前正开发用于多种慢性肝脏疾病的治疗，包括原发性胆汁性胆管炎（PBC）、非酒精性脂肪性肝炎（NASH）、原发性硬化性胆管炎（PSC）、胆道闭锁。
作用机理
奥贝胆酸是对法呢素X受体（FXR）的选择性强效激动剂，该受体是在肝脏和肠中高水平表达的核受体。FXR被认为是胆汁酸，炎症，纤维化和代谢途径的关键调节剂。FXR激活通过抑制胆固醇从头合成以及增加胆汁酸从肝细胞中的转运，降低了胆汁酸的细胞内肝细胞浓度。这些机制限制了循环胆汁酸池的总体大小，同时促进了胆汁淤积，从而减少了肝对胆汁酸的暴露。
适应症
OCALIVA适用于成人对UDCA的反应不佳或与熊去氧胆酸（UDCA）联合治疗原发性胆源性胆管炎（也称为原发性胆汁性肝硬化），或用于不能耐受UDCA的成人的单一疗法。
用法与用量
在开始用奥贝胆酸治疗之前，必须了解患者的肝状态。
表1显示了PBC患者群体的起始剂量和剂量滴定。
PBC患者人群的剂量方案
分期/分类     非肝硬化或Child-Pugh A级          Child-Pugh B级或C级或失代偿性肝硬化
起始剂量          每天一次5毫克                          每周一次5毫克
剂量滴定   对于在治疗6个月后仍未充分降低碱性磷  对于在治疗3个月后ALP和/或总胆红素未达到
           酸酶（ALP）和/或总胆红素且耐受奥贝   充分降低且耐受奥贝胆酸的患者，每周两次
           胆酸的患者，每天一次滴定至10mg      （间隔至少3天）滴定至5mg，随后每周两次滴
                                                定至10mg（至少间隔3天），具体取决于响应和耐受性
最大剂量  每天一次10毫克     每周两次10毫克（间隔至少3天）
接受奥贝胆酸的患者无需调整伴随UDCA的剂量。
严重瘙痒的管理和剂量调整
管理策略包括添加胆汁酸结合树脂或抗组胺药。
对于因瘙痒而严重无法忍受的患者，应考虑以下一项或多项：
对于非肝硬化或Child-Pugh A级患者：
•将奥贝胆酸的剂量减少至：
每隔一天5 mg，对于每天不耐受5mg的患者
每天一次5毫克，对于不耐受每天10毫克的患者
•暂时中断奥贝胆酸剂量长达2周，然后以降低的剂量重新开始。
•继续每天耐受一次将剂量增加至10mg，以达到最佳反应。
对于Child-Pugh B级或C级或失代偿性肝硬化患者：
•将奥贝胆酸的剂量减少至：
每周一次5毫克，对于不耐受每周两次5毫克的患者
每周一次10毫克，对于不耐受每周两次10毫克的患者
•暂时中断奥贝胆酸剂量长达2周，然后酌情以降低的剂量重新开始。
•继续每周两次增加剂量至10mg，以达到最佳反应。
对于继续经历持续性，无法忍受的瘙痒的患者，请考虑停止使用奥贝胆酸治疗。
特殊人群
肝功能不全患者
推荐剂量见表1。。
老年人（≥65岁）
老年患者的数据有限。老年患者无需调整剂量。
肾功能不全的患者
轻度和中度肾功能不全患者的数据有限，重度肾功能不全患者没有数据。肾功能不全患者无需调整剂量。
小儿
小儿乙肝胆酸在原发性胆源性胆管炎（PBC）的治疗中没有相关用途。
给药方法
薄膜片应随食物或不经食物一起口服。
对于服用胆汁酸结合树脂的患者，应在服用胆汁酸结合树脂的至少4-6小时之前或之后的4-6小时或以尽可能大的间隔服用奥贝胆酸。
禁忌症
-对活性物质或列出的任何赋形剂过敏。
-完全胆道梗阻。
保质期
3年
特殊的储存注意事项
该药品不需要任何特殊的存储条件。
容器的性质和内容
高密度聚乙烯（HDPE）瓶带有防止儿童进入的聚丙烯盖和铝箔感应密封。
包装尺寸：30或100片薄膜包衣片。
完整说明资料附件：
https://www.medicines.org.uk/emc/product/7630/smpc
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包装规格[采购以咨询为准]
OCALIVA 5mg film-coated tablets, 30  EU/1/16/1139/001
OCALIVA 5mg film-coated tablets, 100 EU/1/16/1139/003
OCALIVA 10mg film-coated tablets, 30 EU/1/16/1139/002
OCALIVA 10mg film-coated tablets, 100 EU/1/16/1139/004
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OCALIVA (obeticholic acid)
Important Safety Information
Who should not take OCALIVA® (obeticholic acid)?
Do not take OCALIVA if you have been told by a healthcare provider that you have complete biliary obstruction. Report to your healthcare provider immediately if you develop symptoms of complete biliary obstruction.
What are the possible side effects of OCALIVA?
OCALIVA may cause serious side effects, including:
•Liver-Related Adverse Reactions. Liver-related adverse reactions including jaundice (yellow pigmentation of skin and whites of the eyes), worsening ascites (accumulation of fluid in the stomach) and primary biliary cholangitis flare (sudden worsening of PBC symptoms) have been observed in clinical trials, as early as one month after starting treatment with OCALIVA 10 mg once-daily up to 50 mg once-daily (up to 5-times the highest recommended dosage). Your healthcare provider may do blood tests periodically during your treatment with OCALIVA to check how well your liver is working. Report to your healthcare provider immediately if you develop any symptoms of worsening liver disease.
•Severe Pruritus. Cases of severe pruritus have occurred in patients being treated with OCALIVA. Severe pruritus consists of intense or widespread itching, interfering with activities of daily living, or causing severe difficulty in staying asleep, or intolerable discomfort, and typically requiring medical interventions. Your healthcare provider may recommend taking bile acid resins or antihistamines, OCALIVA dosage reduction, and/or temporary interruption of OCALIVA dosing to help manage the symptoms of severe pruritus. Be sure to tell your healthcare provider if pruritus develops or worsens during treatment with OCALIVA.
•Decreases in HDL-C Cholesterol. Decreases in HDL-C (good cholesterol) have been observed in patients taking OCALIVA. Your healthcare provider may check your lipid levels periodically during your treatment with OCALIVA.
The most common side effects of OCALIVA include: pruritus (severe itching of the skin), fatigue (feeling tired all over), stomach pain and discomfort, rash, arthralgia (joint pain), oropharyngeal pain (pain in the middle part of the throat), dizziness, constipation, abnormal thyroid function and eczema (inflammation of the skin).
These are not all the possible side effects associated with OCALIVA. Tell your healthcare provider if you have any side effect that bothers you or does not go away.
What should I tell my healthcare provider before taking OCALIVA?
Before taking OCALIVA, tell your healthcare provider about:
•all of your medical conditions
•all of the medicines you take, including prescription and over-the-counter (OTC) medicines, vitamins and herbal supplements. OCALIVA and other medicines may affect each other, so be sure to tell your healthcare provider if you start a new medicine.
OCALIVA may affect the way other medicines work, and other medicines may affect how OCALIVA works.
Especially tell your healthcare provider if you take:
•Bile Acid Resins, such as cholestyramine, colestipol or colesevelam. Some medicines used to lower blood cholesterol levels, so-called bile acid resins may reduce the effectiveness of OCALIVA. If you take any of these medicines, take OCALIVA at least 4 hours before or 4 hours after taking the bile acid resin, or at as great an interval as possible.
•Warfarin. Your International Normalized Ratio (INR) (which measures how your blood clots) is decreased when warfarin is taken along with OCALIVA. Your physician may need to monitor your INR and/or adjust your dosage of warfarin to keep your INR in a target range while you are taking both warfarin and OCALIVA. Your healthcare provider may need to monitor the co-administration of OCALIVA and warfarin.
•CYP1A2 Substrates with Narrow Therapeutic Index. Obeticholic acid, the active ingredient in OCALIVA, may increase the exposure to certain drugs that are CYP1A2 substrates, such as theophylline and tizanidine. Your healthcare provider may, as needed, monitor CYP1A2 Substrates with Narrow Therapeutic Index when they are taken along with OCALIVA.
Please see the full Prescribing Information for OCALIVA (obeticholic acid) 5mg and 10mg tablets.