Guide for use Nevirapine tablet
【药品名 Drug name】
通用名：奈韦拉平片
Generic name: Nevirapine Tablets
英文名：Nevirapine Tablets
English name: Nevirapine Tablets
本品主要成份及其化学名称为：奈韦拉平，其化学名为11-环丙基-5,11-二氢-4-甲基-6氢-二吡啶并[3,2-b:2’,3’-e][1,4]二氮杂 -6-酮
Active ingredient and Chemical name: 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido [3,2-b:2",3"-][1,4] diazepin-6-one.
分子式：C15H14N4O,分子量：266.3
Molecular formula:: C15H14N4O ,Molecular weight: 266.3
【药理作用Pharmacology】
奈韦拉平是人体免疫缺陷病毒(HIV-1)的非核苷类逆转录酶抑制剂(NNRTI)。奈韦拉平与HIV-1的逆转录酶(RT)直接连接并通过使此酶的催化端破裂来阻断RNA依赖和DNA依赖的DNA聚合酶活性。奈韦拉平不与底物或三磷酸核苷产生竞争。
Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Nevirapine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme"s catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphates.
【药代动力学Pharmacokinetics】
吸收及生物利用度： 成人口服奈韦拉平后快速吸收(>90%)。奈韦拉平的吸收范围(AUC)与禁食情况下相似。奈韦拉平的吸收不受饮食、抗酸药或其它碱性药物的影响(如去羟肌苷)。分布： 奈韦拉平在人体内分布广泛。奈韦拉平易通过胎盘且可进入乳汁。在血浆浓度为1-10μg/mL时，奈韦拉平约60%与血浆蛋白结合。奈韦拉平在人体脑脊液(n=6)浓度为其血浆浓度的45%（±5%）。新陈代谢/消除：奈韦拉平通过细胞色素P450代谢、产生葡糖苷酸结合物，之后葡萄糖醛酸化的代谢物由尿中排出， 。肾排泄对奈韦拉平原形产物的消除所起作用很小。
Absorption and Bioavailability: Nevirapine is readily absorbed (>90%) after oral administration in healthy volunteers and in adults with HIV-1 infection. The extent of nevirapine absorption (AUC) was comparable to that observed under fasting conditions. Nevirapine may be administered with or without food, antacid or ddI.
Distribution: Nevirapine is widely distributed in humans. Nevirapine readily crosses the placenta and is found in breast milk. Nevirapine is about 60% bound to plasma proteins in the plasma concentration range of 1-10 µg/mL. Nevirapine concentrations in human cerebrospinal fluid (n=6) were 45% (±5%) of the concentrations in plasma; this ratio is approximately equal to the fraction not bound to plasma protein.
Metabolism/Elimination: cytochrome P450 metabolism, glucuronide conjugation, and urinary excretion of glucuronidated metabolites represent the primary route of nevirapine biotransformation and elimination in humans. Renal excretion plays a minor role in elimination of the parent compound.
【适应症Indication and usage】
本品适用于治疗HIV-1感染，应与其他抗HIV-1药物联合用药。可单独用于预防母婴传播。
Nevirapine is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection. This medicine also is used to help prevent pregnant women who have HIV from passing the virus to their babies during labor and at birth.
【用法用量Dosage and administration】
成人：口服，一次200mg，一日一次，连续14天(这一导入期的应用可以降低皮疹的发生率)；之后改为一日两次，一次200mg，并同时使用至少两种以上的其它抗HIV-1药物。
儿童患者： 2个月至8岁(不含8岁)的儿童患者推荐口服剂量是用药初始14天内一天一次每次4mg/kg；之后改为一天两次，每次7mg/kg。 8岁及8 岁以上的儿童患者推荐剂量为初始14天内，一天一次，每次4mg/kg；之后改为一天两次，每次4mg/kg。 任何患者每天的总用药量不能超过400mg。
应告知患者按照处方剂量每日服用奈韦拉平的必要性。如果漏服药物，患者应该尽快服用下一次药物，但不要加倍服用。
如果患者停用奈韦拉平超过七天，应按照给药的原则重新开始，即200mg药物，每日一次导入，之后每次200mg，每日二次。
Adults: The recommended dose for Nevirapine is one 200 mg tablet daily for the first 14 days (this lead-in period should be used because it has been found to lessen the frequency of rash), followed by one 200 mg tablet twice daily, in combination with antiretroviral agents.
Pediatric Patients: The recommended oral dose of Nevirapine for pediatric patients 2 months up to 8 years of age is 4 mg/kg once daily for the first 14 days followed by 7 mg/kg twice daily thereafter. For patients 8 years and older the recommended dose is 4 mg/kg once daily for two weeks followed by 4 mg/kg twice daily thereafter.
The total daily dose should not exceed 400 mg for any patient.
Dosage Adjustment: Patients who interrupt Nevirapine dosing for more than 7 days should restart the recommended dosing, using one 200 mg tablet daily (4 mg/kg/day in pediatric patients) for the first 14 days (lead-in) followed by one 200 mg tablet twice daily (4 or 7 mg/kg twice daily, according to age, for pediatric patients).
【不良反应Adverse reactions】
除皮疹和肝功能异常外，与奈韦拉平治疗有关的最常见的不良反应有恶心、疲劳、发热、头痛、嗜睡、呕吐、腹泻、腹痛和肌痛。详见说明书。
The adverse reactions are clinical hepatitis/hepatic failure and severe rash or accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, diarrhea, nausea etc. The details see instruction.
【禁忌症Contraindications】
对奈韦拉平及片中任一成份过敏者禁用。
Nevirapine is contraindicated in patients with clinically significant hypersensitivity to any of the components contained in the tablet
【注意事项Warnings】
本品治疗后的初始8周是很关键的阶段，对患者情况需进行严密的监测，及时发现潜在的严重和威胁生命的皮肤反应或严重的肝炎/肝衰竭。另外必须严格遵守剂量要求，尤其是在14天导入期时。对于监控检查的频率，有专家指出至少每月一次以上，特别在增加剂量之前及增加后2周。
对由于严重皮疹，皮疹伴全身症状，过敏反应和奈韦拉平引起的肝炎而永久中断奈韦拉平治疗的患者不能重新服用。
在服用奈韦拉平期间，继往出现AST或ALT＞正常值上限5倍，重新服用韦拉平后迅速复发肝功能不正常的患者应禁用。
The first 8 weeks of therapy with Nevirapine are a critical period during which intensive monitoring of patients is required to detect potentially life-threatening hepatic events and skin reactions. The optimal frequency of monitoring during this time period has not been established. Some experts recommend clinical and laboratory monitoring more often than once per month, and in particular, would include monitoring of liver function tests at baseline, prior to dose escalation and at two weeks post dose escalation. After the initial 8-week period, frequent clinical and laboratory monitoring should continue throughout Nevirapine treatment. In addition, the 14-day lead-in period with Nevirapine 200-mg daily dosing has been demonstrated to reduce the frequency of rash.
If clinical hepatitis occurs, Nevirapine should be permanently discontinued and not restarted
after recovery.
【孕妇及哺乳期妇女用药Pregnancy and nursing mothers use】
仅在用药潜在益处大于用药可能造成的胎儿危害时，才考虑孕妇使用本品。 建议HIV感染母亲不要给她们的婴儿哺乳，以免产后传染给婴儿HIV。
Nevirapine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Nevirapine readily crosses the placenta and is found in breast milk, mothers should be instructed not tobreast-feed.
【儿童用药Pediatric use】
儿童的清除率比成人快，且随年龄的增大而清除率降低。副作用与成人类似。
The most frequently reported adverse events related to Nevirapine in pediatric patients were similar to those observed in adults. Nevirapine apparent clearance adjusted for body weight was greater in children compared to adults.
【老年患者用药Geriatric use】
对55岁以上的HIV-1患者，奈韦拉平的药代动力学尚未评估。
Clinical studies of Nevirapine did not include sufficient numbers of patients aged 55 years and over to determine whether they respond differently than younger patients. Greater sensitivity of some older individuals to the effects of Nevirapine cannot be ruled out.
【药物相互作用Drug interactions】
奈韦拉平是肝细胞色素P450代谢酶的诱导剂，可以降低主要由CYP3A、CYP2B代谢的药物的血浆浓度。因此，如果一个患者正在接受由CYP3A或CYP2B代谢的药物的一个稳定剂量的治疗，若开始合用本品，前者剂量需要调整。
Nevirapine induce cytochrome P450 activity and coadministration with other drugs metabolized by P450 CYP3A or CYP2B may result in lower plasma concentrations of those drugs, so need to adjust the dosage of those drugs when combination use drugs.
【规格specification】0.2g/片
【包装packag】60片/瓶 ,60pills/bottle
【有效期term of validity】暂定二年 Two year
