【中文品名】依非韦伦 【药效类别】抗病毒药 【通用药名】EFAVIRENZ 【别　　名】Sustiva 【化学名称】 2H-3,1-Benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (S)- 【CA登记号】[154598-52-4] 【结 构 式】 【分 子 式】C14H9ClF3NO2 【分 子 量】315.68 【收录药典】 【开发单位】BRISTOL MYERS SQUIBB 分类名称 一级分类：抗生素 二级分类：抗病毒药 三级分类：    药品英文名 Efavirene   药品别名 依法韦恩茨、Stocrin   药物剂型 胶囊：50mg，100mg，200mg，600mg。   药理作用 依法韦伦是一种半合成二脱氧核苷酸类似物，可抑制HIV-1反转录酶，但对HIV-2病毒无活性。本品通过与HIV-1反转录酶上的特定位点可逆性结合，终止RNA和DNA依赖性DNA聚合酶的活性，阻止病毒的复制。依法韦伦对人免疫缺陷病毒(HIV)有抑制活性。体外试验表明，本品对未分型的实验室病毒株和临床分离的病毒株复制的90%抑制浓度(IC90)为1.7～25.0μmol，与齐多夫定、去羟肌苷、茚地那韦联合应用对HIV-1反转录有协同抑制作用。   药动学 口服吸收良好。健康志愿者单剂量100～600mg顿服，血浆药物浓度达峰时间为5h，血浆峰浓度为0.51～2.87μg/ml。与高脂肪食物同服可增加吸收，在剂量不超过1600mg时，血浆峰浓度与药-时曲线下面积等参数随剂量而改变。HIV感染者每天服用剂量200mg、400mg或600mg后，血浆达峰时间为3～5h，6～10天内达稳态浓度，峰浓度为4.05μg/ml。在体内可通过血-脑脊液屏障，并微量进入脑脊液或乳汁中，浓度为血浆浓度的0.26%～1.19%，血浆蛋白结合率为99.5%～99.75%。在肝经细胞色素P450系统代谢，CYP3A4和CYP2B6是主要的同工酶，长期服用可诱导自身代谢，使药物蓄积程度下降22%～42%，半衰期缩短。本品血浆消除半衰期在单剂量时为52～76h，多剂量时为40～55h。约14%～34%的药物以代谢物形式由尿液中排出，16%～61%以原形药物由粪便中排出。   适应证 用于与其他核苷类和非核苷类反转录酶抑制剂或蛋白酶抑制剂联用治疗HIV感染。   禁忌证 1.对本品过敏者禁用。 2.妊娠及哺乳妇女禁用。   注意事项 1.慎用： (1)肝肾功能严重不全、老年人、乙型及丙型肝炎患者慎用； (2)患有精神疾病或滥用药物史者慎用。 2.如肝酶升高超过正常值的5倍，可考虑停药。 3.本品服用后约有52%的患者出现神经系统的精神症状，通常在服用后1～2天内开始，就寝前服用可增加耐受性，但与乙醇同时饮用可增加不良反应，当患者出现上述不良反应时应避免驾驶车辆和操作机械。 4.如出现皮疹伴随发热、脱皮或起疱，应及时停药或加服肾上腺皮质激素和抗组胺药物。 5.与高脂肪食物同服，可使本品的生物利用度相应增加50%，治疗期间应避免食用高脂肪食物。与其他对肝损伤的药物同用可加重病情，尚需严密观察。 6.本品不易经过透析排除，一旦过量宜及时服用药用炭。   不良反应 常见眩晕、嗜睡、失眠、疲劳、多梦、思维异常、注意力分散、记忆力减退、焦虑、幻觉、欣快、皮疹、斑丘疹。偶见口干、耳鸣、复视、嗅觉异常、恶心、呕吐、面色潮红、心悸、心动过速、关节疼痛、血栓性静脉炎、哮喘、脱发、肝炎、肝酶(AST、ALT)和胆固醇增高。   用法用量 口服：用于HIV感染，每次600mg，每天1次。3岁以下儿童每次200～400mg，3岁以上儿童每次600mg，每天1次。对初始治疗出现不良反应但又需维持治疗者可于睡前服用。   药物相应作用 本品不能与阿司咪唑、西沙必利、咪唑达仑、三唑仑、麦角胺联合应用。与苯巴比妥、苯妥英钠、克拉霉素、利福平等诱导剂合用，可增加本品的消除，体外研究显示，本品抑制肝脏细胞色素P450系统CYP2C9、CYP2C19、CYP3A4、CYP2B6等同工酶，长期服用可诱导自身代谢，并使经上述酶代谢的药物血浆浓度发生改变，须调整药物剂量。与蛋白酶抑制剂沙奎那韦、茚地那韦、利托那韦有相互作用。   专家点评 本品为一种Ⅰ型人类免疫缺陷病毒(HIV-1)的非核苷类反转录酶抑制剂。适用于免疫缺陷感染的成人、青少年和儿童的抗病毒联合治疗。国外报道，本品与齐多夫定、拉米夫定联合治疗，与后者加蛋白酶抑制剂茚地那韦联合应用比较，在临床疗效和耐受性方面均优于茚地那韦。另一项为期48周的临床研究证实，应用本品后血浆病毒数量可降至可检测水平以下者的比例，本品组为98%，茚地那韦组为86%。在一般情况下，本品单独应用易出现耐药性，通常与齐多夫定等核苷类反转录酶抑制剂联合治疗，推荐使用三种不同的反转录酶抑制剂联合治疗，可减低耐药病毒毒株突变体的形成，提高HIV感染者的存活率 Buy Sustiva (Efavirenz) Online Uses: Human immunodeficiency virus type 1 (HIV-1) infection Side Effects: Changes in the shape or location of body fat, insomnia, unusual dreams, muscles and joints pain, headache, tired feeling, dizziness, spinning sensation, blurred vision, cough, nausea, vomiting, diarrhea, constipation, stomach pains, etc. Active Ingredients: Efavirenz Category: Antiretroviral drugs (HIV/AIDS) Dosages: 50mg，100mg，200mg，600mg Sustiva Description This medicine is a non-nucleoside reverse transcriptase inhibitor used to manage human immunodeficiency virus infection (HIV). This medicine is not a cure for HIV. It must be used in combination with other proven anti-HIV medicines. If this medicine is taken alone to treat HIV infection, it may stop working. Contact your doctor for more information Sustiva Directions Follow the directions for using this medicine provided by your doctor. This medicine comes with a patient leaflet. Read it carefully. Ask your doctor, nurse, or pharmacist if you have any questions about taking this medicine. TAKE THIS MEDICINE ON AN EMPTY STOMACH at least 1 hour before or 2 hours after eating. Taking this medicine with food, especially with a high fat meal, may lead to increased blood levels of this medicine. This may increase your risk for side effects. Take this medicine with a full glass of water. Take this medicine at the same time every day, preferably at bedtime unless otherwise directed by your doctor. STORE THIS MEDICINE at room temperature between 59 to 86 degrees F (15 to 30 degrees C) in a tightly-closed container, away from heat and light. For best results take this medicine regularly. CONTINUE TO USE THIS MEDICINE even if you feel well. Do not miss any doses. IF YOU MISS A DOSE OF THIS MEDICINE, take it as soon as you remember. If it is within 2 hours of your next dose, skip the missed dose and go back to your regular dosing schedule. It is important not to miss doses of this medicine. DO NOT TAKE 2 doses at once. Sustiva Cautions DO NOT EXCEED THE RECOMMENDED DOSE without checking with your doctor. Exceeding the recommended dose of this medicine may not provide additional benefits and may increase the risks of side effects. KEEP ALL DOCTOR AND LABORATORY APPOINTMENTS while you are using this medicine. This medicine may interfere with certain laboratory tests (such as cannabinoids/marijuana false positive result). DO NOT STOP USING THIS MEDICINE without first checking with your doctor. DO NOT DRIVE, OPERATE MACHINERY, OR DO ANYTHING ELSE THAT COULD BE DANGEROUS until you know how you react to this medicine. Using this medicine alone, with other medicines, or with alcohol may lessen your ability to drive or to perform other potentially dangerous tasks. LIMIT YOUR ALCOHOL CONSUMPTION while you are taking this medicine. This medicine will add to the effects of alcohol and other depressants. Ask your pharmacist if you have questions about which medicines are depressants. THIS MEDICINE WILL NOT PREVENT YOU FROM SPREADING HIV. If you have questions concerning how to prevent the spreading of HIV, ask your doctor, nurse, or pharmacist. THIS MEDICINE WILL NOT PROTECT you from getting sexually transmitted diseases (STDs). Always use a condom during sexual intercourse. If your health changes, check with your doctor. BEFORE YOU BEGIN TAKING ANY NEW MEDICINE, either prescription or over-the-counter, check with your doctor or pharmacist. FOR WOMEN TAKING BIRTH CONTROL PILLS: this medicine may decrease the effectiveness of your birth control pill. To prevent pregnancy, also use a barrier form of birth control. FOR WOMEN: IF YOU ARE ABLE TO BECOME PREGNANT, talk with your doctor or pharmacist about the use of effective birth control while taking this medicine. THIS MEDICINE HAS BEEN SHOWN TO CAUSE HARM to the human fetus. DO NOT USE THIS MEDICINE if you are pregnant. IF YOU SUSPECT THAT YOU COULD BE PREGNANT, contact your doctor immediately. IT IS UNKNOWN IF THIS MEDICINE IS EXCRETED in breast milk. DO NOT BREAST-FEED while taking this medicine. Sustiva Side Effects SIDE EFFECTS that may occur while taking this medicine include dizziness, trouble sleeping, diarrhea, trouble concentrating, or drowsiness. These side effects tend to go away after a few weeks. If they continue or are bothersome, check with your doctor. CHECK WITH YOUR DOCTOR AS SOON AS POSSIBLE if you experience rash with or without fever; mouth sores; change in personality, behavior, mood, or emotions; yellowing of the skin or eyes; dark urine or pale stools; unusual fatigue; or vision changes. Changes in body fat may occur while you are taking this medicine (e.g., increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of therapy with your doctor, as well as the possible role of exercise to reduce this side effect. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist. 附件： 200952603375516.pdf     --------------------------------------------------------------- 注：以下产品不同规格和不同价格，购买时请以电话咨询为准！ --------------------------------------------------------------- 产地国家：美国 原产地英文药品名： EFAVIRENZ 中文参考药品译名： 依非韦伦 原产地英文商品名： SUSTIVA 100mg/Cap 30Caps/bottle 中文参考商品译名： SUSTIVA 100毫克/胶囊 30胶囊/瓶 生产厂家英文名： Bristol Myers-Squibb 生产厂家中文参考译名： 百时美施贵宝 ------------------------------------------------------------------ 产地国家：美国 原产地英文药品名： EFAVIRENZ 中文参考药品译名： 依非韦伦 原产地英文商品名： SUSTIVA 50mg/Cap 30Caps/bottle 中文参考商品译名： SUSTIVA 50毫克/胶囊 30胶囊/瓶 生产厂家英文名： Bristol Myers-Squibb 生产厂家中文参考译名： 百时美施贵宝 ------------------------------------------------------------------ 产地国家：美国 原产地英文药品名： EFAVIRENZ 中文参考药品译名： 依非韦伦 原产地英文商品名： SUSTIVA 600mg/tab 30tabs/bottle 中文参考商品译名： SUSTIVA 600毫克/片 30片/瓶 生产厂家英文名： Bristol Myers-Squibb 生产厂家中文参考译名： 百时美施贵宝 ------------------------------------------------------------------- 产地国家：美国 原产地英文药品名： EFAVIRENZ 中文参考药品译名： 依非韦伦 原产地英文商品名： SUSTIVA 200mg/Cap 90Caps/bottle 中文参考商品译名： SUSTIVA 200毫克/胶囊 90胶囊/瓶 生产厂家英文名： Bristol Myers-Squibb 生产厂家中文参考译名： 百时美施贵宝