部份中文盐酸利匹韦林处方资料（仅供参考）
商品名：EDURANT Tablets
英文名：Rilpivirine Hydrochloride
中文名：盐酸利匹韦林片
生产商：杨森制药
药品简介
Edurant(Rilpivirine)是一种非核苷类逆转录酶抑制剂,适合与其他抗逆转录病毒药联用。,用于初治成人的人类免疫缺陷病毒-1(HIV-1)感染。 
エジュラント錠25mg
效果分类名称
抗病毒化疗药物[非核苷逆转录酶抑制剂(NNRTI)]
批准日期：2012年5月
商標名
EDURANT Tablets
一般名
リルピビリン塩酸塩（JAN）、Rilpivirine Hydrochloride（JAN）
化学名
4-{［4-（{4-［（1E）-2-Cyanoethenyl］-2,6-dimethylphenyl}amino）pyrimidin-2-yl］amino}benzonitrile monohydrochloride
分子式
C22H18N6・HCl
分子量
402.88
化学構造式
性状
白色粉末
溶解度
甲醇 5.8Mg/ml
乙醇 0.67mg/mL
水 0.01Mg/ml
熔点
约 250°c (分解)
分布系数
日志 P = 4.86(1-octanol/PH 7.0磷酸盐缓冲液)
批准条件
1. 在使用本制剂时, 只需解释正在为患者收集有关该制剂的进一步疗效和安全性的数据, 并获得知情同意, 并请医生。
2. 如果您目前正在海外进行或计划临床试验, 请在完成后及时提交测试和分析结果。
3. 在重新审议期结束之前, 原则上, 在日本所有病例的生产和销售调查之后, 提供关于药物实际使用情况的信息(患者背景、收集并定期报告有效性和安全性 (包括与其他药物结合使用的有效性和安全性) 和药物相互作用数据, 并在重新审议申请时将调查结果作为附件提交。
药用药理学
1. 作用机制
利皮林有一个二烯丙基吡啶骨架, 是 NNRTI 作用于 HIV-1。 利皮宾林抑制非竞争性 HIV-1 逆转录酶 (RT), 不抑制人 DNA 聚合酶α、β和γ。
2. 抗病毒作用
野生型(WT) Hiv-1 实验室菌株iiib的利必林有效浓度为50%, 急性感染T细胞系(EC50)的中值为 0.73 nmol(0.73 Ng/ml)。
Lilpibinin对HIV-1临床分离株 M 组的影响为0.07 ~ 1.01nmol/L(0.07 ~ 0.07 Ng/ml), o组(1.01 ~ 3.10ng/)为2.88~8.45nmol 我展示了mL的EC50值)。
Lilpibinine, Nrtim/ntrti (Abbacavir、Didaninsin、Emtriccitabine、Samilbudine 和tenofovir)、蛋白酶抑制剂(amiravir, ataza nabil、Darnabil、Indinavir, Ropinavir, Nerfinavir, Riliavir、Saunavir和Tipranavir)、NNRTI (Efavenz、Etravirin 和 Nevirapine)、融合抑制剂 (enfuvirtid) 和 CCR5 抑制剂(Malabiroku) 与。NRBZINE和Didovudine是一种整合酶抑制剂, 具有添加或协同作用。
3. 耐药
采用不同衍生和亚型的WT或NNRTI抗HIV-1菌株进行体外抗性采集试验, 出现了抗利比林菌株。 在这种耐药菌株中出现的最高频率的氨基酸突变是L100I、K101E、K101E、E138K、V179F、y181c、h211y、f227c 和 m230i。
生物截止值(BCO)FC值超过[EC50值之比)是表型抗性(EC50值的EC50值表示为各种分离株)] 株呈显示, 并具有 Lilpibilin 电阻。
在第三阶段的分离分析中, 观察到62例病毒性衰竭患者的耐药突变, 其中72例是代理管理组。氨基酸突变表明NNRTI抵抗主要是V90I, L100I, K101E, E138K, V179I, Y181C, Y181C, h221y和f227c。在96周观察到的48周突变也被观察到。V90I和V189I在基线期间观察到的情况并不影响本研究的效果。 E138K 氨基酸突变在利皮林给药期间的频率最高, 许多都伴随着M184I的氨基酸突变。
根据体外和体内的研究结果, K101E, K101E, E138A, E138A, E138A, E138A, E138A, V179L, Y181C, Y181C, Y181C, Y181C, K101E, 基线时间 F227C 是 F227C 和 F227C 中氨基酸突变的菌株, 被认为有可能影响利必林的抗病毒作用。
4. 交叉阻力
Lilpibilin对67株菌株中的64株(96%)表现出抗病毒作用, 这些菌株引入了一个NNRTI 与耐药相关的氨基酸突变, 如K103N和 Y181C 到 RT。一个单一的氨基酸突变, 导致对利皮宾素的易感性下降是K101P, Y181I和Y181I。K103N氨基酸突变, 虽然没有降低对利必林的敏感性在一个单一的, 在K103N和L100I的双重突变中, 对利必林的敏感性降低了7倍。
在4786株 HIV-1重组临床分离株中, 62%的菌株对利皮宾林和奈韦拉平的抗性表现出耐药性 (FC 值 BCO)。
在介入时间的第三期检查中进行兼并分析, 降低了31例病毒性衰竭62例RPV+BR组表型耐药试验对该药物的敏感性。在这28例埃特拉韦林中, 27例埃法维伦茨, 14例对奈韦拉平有耐药性。在48周时观察到的交叉耐受也在96周观察到。
96周的第三阶段检测在兼并分析中, 在病毒失效实例中, RPV+BR组显示对该制剂有耐药性, 基线HIV RNA量大于主题>100, 000 copiesl基线hiv rna量为100, 在研究对象中, 有一定数量的研究对象表现出表型交叉抗性较小。 在显示对这种制剂的耐药性的病毒性失败示例中, 5例 HIV rna 含量的基线为100, 000 copies ml, 3例Efavilenz, 4例 Etravirin, 1例显示对奈韦拉平的耐药性。HIV RNA 含量基线 > 100, 000 例, 27例, 埃法维伦兹, 28 例 Ewatvirin, 15例对奈韦拉平有耐药性。
适应症
HIV-1感染症
用法与用量
成人；口服一次, 每天25毫克一次, 或吃后立即作为利皮宾林。在服用时, 一定要将其与其他抗艾滋病药物一起使用。
包装
片剂
25mg:30 片 (瓶装)
製造和銷售來源
杨森制药
注：以上中文不够完整，使用者以原处方资料为准。
完整说明附件：
http://www.info.pmda.go.jp/go/pack/6250036F1024_1_14/ 
EDURANT Tablets 25mg（エジュラント錠25mg） 
Brand name : EDURANT Tablets 25mg
　Active ingredient: Rilpivirine hydrochloride
　Dosage form: white tablet, diameter 6.4 mm, thickness 3.4 mm
　Print on wrapping: 
Effects of this medicine
This medicine is an antiviral agent that inhibit reverse transcriptase of human immunodeficiency virus type-1 (HIV-1) to slow disease progression.
Usually, used for treatment of HIV-1 infection.
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 (25 mg of rilpivirine) at a time, once daily, definitely with concomitant other anti-HIV agent medication. Take this medicine during a meal or within 30 minutes after a meal because its effect may diminish if taken on an empty stomach. Strictly follow the instructions.
Do not miss any single dose because you lose its effect if you miss a dose. In case you have missed a dose and when you become aware of it, take the missed dose immediately with food if it is within 12 hours after the dose missing, and return to your regular dosing schedule the following day. If you become aware of dose missing after more than 12 hours, then do not take the missed dose and take a dose at your next regular dosing time. You should never take two doses at one time.
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
This medicine is not intended for radical treatment of HIV infection. The disease may progress even though you are taking it; therefore, inform your doctor of all changes in your physical condition.
Be cautious against ill effects of taking this medicine together with other drugs. Report to your doctor all drugs you are now taking. Consult with your doctor about any drug you are intending to newly start.
Avoid taking this medicine with food or beverage containing Saint. John's wort. Because Saint. John's wort (Hypericum perforatum) may decrease the blood concentration of this medicine and reduce the effect of it.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include headache, nausea, insomnia, dizziness, and abnormal dreams. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
No pertinent entries.
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor 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 light, heat and moisture.
Discard the remainder. Do not store them. If you dispose of unused medicines, seek advice of your pharmacist about proper disposal of drugs.
JANSSEN PHARMACEUTICAL K.K. Internal
Published: 6/2012
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.
http://www.kegg.jp/medicus-bin/japic_med?japic_code=00060371