当前位置：药品说明书与价格首页 >> 皮肤性病 >> 艾滋病 >> 药品推荐 >> Reyataz(atazanavir sulfate Capsules)

Reyataz(atazanavir sulfate Capsules)

2013-03-17 02:31:06 作者：新特药房来源：互联网浏览次数：252 文字大小：【大】【中】【小】

简介： 首个每日一次给药抗艾滋病（HIV/AIDS）药物近日，百时美施贵宝公司正式对外宣布，FDA已经批准了公司抗HIV/AIDS新药Reyataz（atazanavirsulfate）的上市申请。这也是FDA有史以来批准的首个每日一次给药 ...

关键字：硫酸阿扎那韦胶囊 atazanavir sulfate 商品名Reyataz 锐艾妥 HIV蛋白酶抑制剂治疗HIV-1感染

Reyataz（atazanavirsulfate）-为首个每日一次给药抗艾滋病（HIV/AIDS）药物
近日，百时美施贵宝公司正式对外宣布，FDA已经批准了公司抗HIV/AIDS新药Reyataz（atazanavirsulfate）的上市申请。这也是FDA有史以来批准的首个每日一次给药的蛋白酶抑制剂。
FDA对有2400例ＨＩV感染者参加的15项临床试验的结果进行了评审。结果表明：含Reyataz的治疗方案在显示和标准治疗方案相近的病毒学抑制效果的同时，可以使血脂指标中的ＬＤＬ-胆固醇、总胆固醇和甘油三酯分别降低６％、２％和２％，并且抗药性也优于标准方案。
和其他蛋白酶抑制剂一样，Reyataz也是通过阻断受HIV感染的细胞中的蛋白酶，破坏其病毒复制过程而发生作用。但Reyataz提高了病毒的敏感性，每日一次给药就能够维持病毒抑制。此药在美国市场正式推出。
REYATAZ（阿扎那韦硫酸盐[atazanavir sulfate]）胶囊供口服使用
初始美国批准：2003
作用机制
阿扎那韦是一种抗病毒药物[见临床药理学]。
适应症和用法
REYATAZ是一种蛋白酶抑制剂，用于与其它抗逆转录病毒药物联合用于治疗HIV-1感染。
剂量和给药
•治疗天真的患者：REYATAZ 300mg与利托那韦100mg每天一次与食物或REYATAZ 400mg每天一次与食物。当与替诺福韦联合给药时，推荐剂量为REYATAZ 300mg，利托那韦100mg。
•治疗经验的患者：REYATAZ 300mg，利托那韦100mg，每日一次，含食物。
•儿童患者（6岁至18岁以下）：剂量基于体重不超过成人剂量。
•怀孕：REYATAZ 300毫克与利托那韦100毫克每天一次与食品，与一些伴随药物的剂量修改。
•伴随治疗：可能需要进行剂量调整。
•肾功能损害：可能需要进行剂量调整。
•肝脏损害：可能需要进行剂量调整。
剂量形式和强度
•胶囊：150mg，200mg，300mg。
禁忌症
REYATAZ禁忌在之前对该产品的任何组分显示超敏反应（例如，史蒂文斯 - 约翰逊综合征，多形性红斑或有毒皮肤疹）的患者中。
●当作为REVATIO时，与阿夫唑嗪，三唑仑，口服施用咪达唑仑，麦角衍生物，利福平，伊立替康，洛伐他汀，辛伐他汀，茚地那韦，西沙必利，匹莫齐特，圣约翰草和西地那非共同施用。
警告和注意事项
心脏传导异常：一些患者可能发生PR间期延长。在预先存在的传导系统疾病患者中谨慎使用，或者与可能延长PR间期的其他药物一起使用。
•皮疹：如果出现严重皮疹，则停止。
•高胆红素血症：大多数患者的间接胆红素无症状增加，停药后可逆转。不要减少剂量。如果发生伴随的转氨酶升高，则替代病因。
•肝毒性：REYATAZ在肝功能损害患者中应谨慎使用。患有乙型或丙型肝炎感染的患者具有转氨酶或肝代偿失调增加的风险。在治疗前和治疗期间监测肝实验室检查。
•已报告肾结石和胆石病。考虑暂时中断或停止。
•接受REYATAZ的患者可能发生糖尿病/高血糖，免疫重建综合征和体脂重新分配/积累的新发病或加重。
•血友病：可能发生自发性出血，可能需要额外的因子VIII。
不良反应
最常见的不良反应（≥2％）是恶心，黄疸/巩膜黄斑，皮疹，头痛，腹痛，呕吐，失眠，周围神经系统症状，头晕，肌痛，腹泻，抑郁症和发烧。
药物相互作用
REYATAZ的联合给药可以改变其他药物的浓度，其他药物可能改变阿扎那韦的浓度。在治疗之前和期间必须考虑潜在的药物 - 药物相互作用。
在特定人群中使用
•怀孕：仅在潜在利益证明潜在风险时使用。
•由于产后HIV传播的潜力，应指示哺乳母亲不要母乳喂养。
•乙型或丙型肝炎共感染：监测肝酶。
•肾功能损害：不要用于经过血液透析管理的终末期肾病的有经验的治疗患者。
•肝脏损害：REYATAZ应慎用于轻度至中度肝损伤患者。不要在严重肝损伤的患者中使用REYATAZ。不推荐.
-------------------------------------------
注：以下产品美国包装，不同各和不同价格，采购以咨询为准
-------------------------------------------
REYATAZ CAP 300MG 30 ATAZANAVIR SULFATE     00003-3622-12
REYATAZ CAP 150MG 60 ATAZANAVIR SULFATE     00003-3624-12
REYATAZ CAP 200MG 60 ATAZANAVIR SULFATE     00003-3631-12
REYATAZ PWD O/S 50MG 1.5GX30 ATAZANAVIR SULFATE   00003-3638-10

reyataz (atazanavir sulfate)capsule, gelatin coated
[Bristol-Myers Squibb Company]
IMPORTANT SAFETY INFORMATION:
•REYATAZ® (atazanavir), along with other antiretroviral medications, can help you treat HIV-1
•When taken as part of combination therapy, REYATAZ can help reduce your viral load to undetectable*
•REYATAZ may also help raise the number of T cells in your body that help fight off other infections
*Having an undetectable viral load means that your viral load is below what a lab test can detect. The value depends on the test being used. In REYATAZ clinical trials, undetectable was defined as a viral load of fewer than 400 copies/mL or 50 copies/mL depending on the trial.
Ask your HCP what the viral load cut-off for undetectable is for the test used for you.
REYATAZ does not cure HIV infection or AIDS (Acquired Immunodeficiency Syndrome). You must keep taking HIV medicines to control HIV infection and decrease HIV-related illnesses.
IMPORTANT SAFETY INFORMATIONDo not take REYATAZ if you are:
Allergic to REYATAZ or to any of its ingredients
Taking certain medicines with REYATAZ that may affect how REYATAZ works. REYATAZ may cause serious, life-threatening side effects or death if taken with the following medicines: alfuzosin (Uroxatral®), cisapride (Propulsid®), ergot medicines (refer to patient information for complete list of these medicines), indinavir (Crixivan®), irinotecan (Camptosar®), lurasidone (Latuda®) if REYATAZ is used with ritonavir (Norvir®), lovastatin (Advicor®, Altoprev®, Mevacor®), midazolam (Versed®) when taken by mouth for sedation, nevirapine (Viramune®, Viramune XR®), pimozide (Orap®), rifampin (Rifadin®, Rifamate®, Rifater®, Rimactane®), sildenafil (Revatio®) when used for pulmonary arterial hypertension, simvastatin (Simcor®, Vytorin®, Zocor®), St. John’s wort (Hypericum perforatum), triazolam (Halcion®)
Before taking REYATAZ, tell your healthcare provider if you:
Have heart problems
Have liver problems including hepatitis B or C infection
Have phenylketonuria (PKU). REYATAZ oral powder contains phenylalanine as part of the artificial sweetener aspartame and can be harmful to people with PKU.
Are receiving dialysis treatment
Have diabetes
Have hemophilia
Have any other medical conditions
Are pregnant or plan to become pregnant. Talk to your healthcare provider about taking REYATAZ during your pregnancy or if you are planning to become pregnant while you are taking REYATAZ.
Hormonal forms of birth control, such as injections, vaginal rings or implants, contraceptive patch, and some birth control pills, may not work when you are taking REYATAZ
After your baby is born, tell your healthcare provider if your baby’s skin or the white part of the eyes turns yellow
Are breastfeeding or plan to breastfeed. Do not breastfeed if you are taking REYATAZ. REYATAZ can pass into your breast milk.
Tell your healthcare provider about all the medicines you take, including prescription and over-the counter medicines, vitamins and herbal supplements. Some medicines interact with REYATAZ. Keep a list of medicines to show your healthcare provider and pharmacist. Do not start taking a new medicine without telling your healthcare provider.
REYATAZ can cause serious side effects. Call your healthcare provider right away if you have any of the following:
A change in the way your heart beats. You may feel dizzy or lightheaded. These could be symptoms of a heart problem.
Skin rash is common with REYATAZ and usually goes away within 2 weeks. Skin rash can sometimes be severe and may develop with other symptoms which can be serious. If you develop a severe rash with any of the following symptoms stop taking REYATAZ and call your healthcare provider right away: general feeling of discomfort or "flu-like" symptoms, fever, muscle or joint aches, red or inflamed eyes, blisters, mouth sores, swelling of your face, painful, warm or red lump under the skin.
Yellowing of your skin or the white part of your eyes is common, and usually not harmful in adults and infants older than 3 months of age, but it could also be a symptom of a serious problem. This may occur due to increases in bilirubin levels in the blood (bilirubin is made by the liver).
Liver problems including hepatitis B or C may get worse when taking REYATAZ. Your healthcare provider will do blood tests before and during treatment with REYATAZ. Liver problem symptoms may include: dark “tea-colored” urine, your skin or the white part of your eyes turning yellow, light colored stools, nausea, itching, or stomach area pain.
Kidney stones have happened in some people taking REYATAZ. Symptoms may include pain in your back or low stomach area, blood in your urine, pain when you urinate.
Gallbladder problems have happened in some people who take REYATAZ. Symptoms may include pain in the right or middle upper stomach area, fever, nausea and vomiting, or your skin or the white part of your eyes turning yellow.
Diabetes and high blood sugar have happened or worsened in some people who take protease inhibitor medicines like REYATAZ. Some people may need to start diabetes medicine or change their diabetes medicine.
Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Tell your healthcare provider if you have any new symptoms after starting REYATAZ.
Changes in body fat can happen in people taking HIV-1 medicines. The exact cause and long-term health effects are not known.
Increased bleeding problems in people with hemophilia have happened when taking protease inhibitors like REYATAZ.
The most common side effects of REYATAZ include: nausea, headache, stomach-area pain, vomiting, trouble sleeping, numbness, tingling, or burning of hands or feet, dizziness, muscle pain, diarrhea, depression, and fever.
You should take REYATAZ capsules and oral powder once daily with food. Swallow the capsules whole; do not open the capsules. REYATAZ oral powder must be mixed with food or liquid and taken with ritonavir. Take REYATAZ exactly as your healthcare provider tells you to.
抗HIV药物锐艾妥的最新说明书为孕妇提供用药指导
2011年2月7日，百时美-施贵宝公司宣布，美国食品药品管理局(FDA)已经批准锐艾妥(Reyataz，阿扎那韦)的最新说明书，其中新增了针对感染人类免疫缺陷病毒(HIV)的孕妇的推荐剂量。
锐艾妥是一种蛋白酶抑制剂，已经在感染HIV 的初治和经治患者中得到了研究，其用法是作为HIV感染联合治疗方案的一部分每日用药1次。
在HIV感染的联合治疗方案中，采用锐艾妥300mg(成人推荐剂量)联合利托那韦100mg进行治疗，可在孕晚期达到最低血药浓度(给药后24h)，这与既往在成人HIV感染者中所观察到的数据相当。在产后期阿扎那韦的浓度可能会增加，因此尽管无需调整剂量，也应该在分娩后2个月内监测患者是否发生不良事件。
孕妇在使用锐艾妥与利托那韦联合治疗方案时不需要进行剂量调整，但在孕中期或孕晚期联用锐艾妥和替诺福韦或一种H2受体拮抗剂(H2RA)的经治孕妇除外。
在那种情况下，推荐实施1剂锐艾妥(400mg)+利托那韦100mg、每日1次的治疗方案。
根据现有数据尚不足以推荐对经治孕妇实施1剂锐艾妥联用替诺福韦和一种H2RA的治疗方案。除妊娠期间的用药指导之外，锐艾妥的完整处方信息中还包括总体用药指南以及针对肾功能、肝功能的具体用药指导和配伍药物间的相互作用。
说明书更新的依据是一项多中心、开放性、前瞻性、单组药代动力学研究，此研究共纳入41名处于12~32孕周的HIV感染孕妇，其CD4细胞计数≥200/mm3。患者的治疗方案为锐艾妥300mg+利托那韦100mg(n=20)或锐艾妥400mg+利托那韦100mg(n=21)，每日1次；对孕中期患者采用锐艾妥300 mg+利托那韦100mg进行治疗。所有患者都接受齐多呋定300mg+拉米呋定150mg、每日2次治疗。
此研究的主要目的是，确定锐艾妥/利托那韦在作为孕妇联合治疗方案的组成部分时，产生足够的药物暴露所需的剂量，并与成人HIV感染者的既往数据进行比较。
该研究的次要目的是评估该药对孕妇及其婴儿的抗病毒疗效和安全性。有39名妇女完成了研究，其中有38名(97%)在分娩时的HIV RNA读数<50拷贝/ml。
在20名接受锐艾妥300mg+利托那韦100mg治疗方案的妇女和21名接受锐艾妥400mg+利托那韦100mg治疗方案的妇女中，分别有6名(30%)和13名(62%)发生了高胆红素血症。研究中未观察到乳酸酸中毒的病例。
阿扎那韦的安全性已经在少数孕妇和产后期妇女中得到了评估。现有的人类试验和动物实验的数据表明，总体而言，与背景发病率相比，使用阿扎那韦不会增加重大出生缺陷的风险。
由于人类研究无法排除产生危害的可能性，故在妊娠期间应该仅在收益超过风险的情况下使用锐艾妥。在使用锐艾妥+核苷类似物联合治疗方案的孕妇中，已有发生乳酸酸中毒综合征(有时为致死性)和症状性高乳酸血症的病例。使用核苷类似物可增加乳酸酸中毒综合征的风险。另外，高胆红素血症在服用锐艾妥的患者(包括孕妇)中较常见。