| 简介：
部份中文非达霉素处方资料（仅供参考）
商品名：Dafclir Tablets
英文名：Fidaxomicin
中文名：非达霉素
生产商：安斯泰来制药
药品简介
2018年7月2日，安斯泰来（Astellas）宣布，抗生素新产品Dafclir（fidaxomicin，非达霉素，ダフクリア錠200mg）已获日本批准，用于治疗感染性肠炎（包括假膜性结肠炎[PMC]）（敏感菌株：非达霉素敏感的艰难梭状芽胞杆菌[CD]）。
Dafclir是一种口服、大环内酯类抗生素，具有一种新的作用机制和一个选择性抗菌谱，该药主要是通过抑制细菌的RNA聚合酶而产生迅速的抗难治梭状芽孢杆菌感染（CDI）作用。
ダフクリア錠200mg
药用类别名称
二苯二甲酸梭菌感染性疾病治疗剂
批准日期：2018年8月
商標名
Dafclir Tablets 200mg
一般名
フィダキソマイシン（Fidaxomicin）
略号
FDX
化学名
（3E,5E,8S,9E,11S,12R,13E,15E,18S）-3-（{[6-Deoxy-4-O-（3,5-dichloro-2-ethyl-4,6-dihydroxybenzoyl）-2-O-methyl-β-D-mannopyranosyl]oxy}methyl）-12-{[6-deoxy-5-C-methyl-4-O-（2-methylpropanoyl）-β-D-lyxo-hexopyranosyl]oxy}-11-ethyl-8-hydroxy-18-[（1R）-1-hydroxyethyl]-9,13,15-trimethyloxacyclooctadeca-3,5,9,13,15-pentaen-2-one
構造式
分子式
C52H74Cl2O18
分子量
1058.04
融点
177〜180℃
分配係数
3.7
性状：
植物霉素是一种白色粉末。四氢呋喃, 易溶于二甲基亚硫酸和甲醇, 微溶于丙酮、乙酸乙酯、乙醇(99.5), 几乎不溶于二氯甲烷和乙腈, 几乎不溶于异丙醇, 很难溶于布列顿-罗宾逊缓冲液 (Hh8), 几乎不溶于布列顿-罗宾逊缓冲液 (Hh)。
批准条件
制定药品风险管理计划并加以实施。
药用药理学
1. 抗菌活性
植物霉素在某些革兰氏阳性细菌中表现出抗菌活性, 包括扩散梭菌, 它对大多数革兰氏阴性菌不具有抗菌活性。
2. 作用机制
通过抑制细菌RNA聚合酶, 显示出抗菌活性。
适应症
〈适应细菌物〉
该制剂中的低苯二甲菌
〈适应症〉
传染性肠炎 (包括假冒结肠炎)
用法与用量
通常, 成人每天口服两次200毫克。
临床结果
1. 国内临床结果
为了考虑该制剂对20岁以上的肠炎患者的疗效和安全性(210例靶例数[每组105例]), 进行了随机双盲并发组比较试验。主要评价项目, 设置了扩散梭菌对肠炎的愈合保留率, 结果如下。代理组与万古霉素组(95%置信区间) 之间的组差为1.2(-11.3 ~ 13.7)%, 因为95%置信区间的下限低于预先设定的非自卑幅度(-10%), 该制剂对万古霉素的非劣势未得到证实。
2. 海外临床结果
海外三期试验(北美试验)
为了检测该制剂治疗16岁以上二菲生性梭菌肠炎患者的疗效和安全性, 进行了随机双盲并发组比较试验。主要评价项目, 临床试验药物管理局结束日期(±2天) 或设定停药时的愈合率, 在PP人群中, 制剂组和万古霉素组的治愈率为 92.2(247-268例) 和锐减9.6%(251/280例), 代理组与万古霉素组(95%置信区间) 之间的组差为2.5(-2.4~7.3%), 因为95%置信区间的下限超过了预先设定的非自卑幅度(-10%), 验证了万古霉素集团代理组的非劣势。
海外三期测试 (欧美)
为了检测该制剂治疗16岁以上二菲生性梭菌肠炎患者的疗效和安全性, 进行了随机双盲并发组比较试验。主要评价项目, 临床试验药物管理局结束日期(± 2天) 或设定停药时的愈合率, 在PP人群中, 制剂组和万古霉素组的治愈率为91.7(199"217 例) 和91.7(2-234例), 代理组与万古霉素组(95%置信区间) 之间的组差为1.1(-4.2 ~ 6.4), 因为95% 置信区间的下限超过了预先设定的非自卑幅度(-10%), 验证了该制剂对万古霉素的非劣势。
包装
片剂
200mg:20片(10片x2)
制造供应商
安斯泰来制药公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整资料附件：
http://www.info.pmda.go.jp/go/pack/6119001F1025_1_02/
Dafclir Tablets 200mg（Fidaxomicin ダフクリア錠）
Brand name:Dafclir Tablets 200mg
Active ingredient:Fidaxomicin
Dosage form:pale yellow red tablet, major axis: approx. 13.1 mm, minor axis:
approx. 7.0 mm, thickness : approx. 5.1 mm
Print on wrapping:(Face) ダフクリア 200 mg, house-mark,(Back) ダフクリア 200 mg, 感染性腸炎治療剤, house-mark
Effects of this medicine
This medicine suppresses RNA polymerase necessary for bacterial growth and shows antibactrial activities.
It is usually used for the treatment of infectious enterocolitis (including pseudomembranous colitis) by Clostridiumdifficile.
Before using this medicine, be sure to tell your doctor and pharmacist
・If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
・If you are pregnant or breastfeeding.
・If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal
effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
・Your dosing schedule prescribed by your doctor is(( to be written by a healthcare professional))
・In general, for adults, take 1 tablet (200 mg of the active ingredient) at a time, twice a day. Strictly follow theinstructions.
・If you miss a dose, please take immediately when you notice. However, if it is almost time for the next dose, skip themissed dose and continue your regular dosing schedule. Do not take two tablets at once.
・If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
・Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include constipation, nausea, and vomiting. If any of these symptomsoccur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicatedin brackets. If any of these symptoms occur, stop taking this medicine and see your doctorimmediately.
・rash, itching, angioedema, dyspnea [anaphylaxis]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with yourdoctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
・Keep out of the reach of children. Store away from direct sunlight, heat and moisture.
・Discard the remainder. Do not store them
Internal
Published: 08/2018
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approvaldetails may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It isimportant to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response,patients should understand their medication and cooperate with the treatment. |
