英文药名: Zortress(Everolimus Tablets) 中文药名: 依维莫司片 生产厂家: Novartis 【药品介绍】 Zortress (everolimus，依维莫司)用于预防有轻中度免疫风险的成人肾移植患者产生排异现象。Zortress与低剂量的钙调素抑制剂联合使用，如环孢菌素、巴利昔单抗或皮质激素类药物。依维莫司已以商品名Certican在在美国之外的70多个国家获得批准。 支持此项批准的3期试验显示，Zortress预防器官排异与保护肾功能，同时与使用麦考酚酸相比降低了60%的环孢菌素使用量，显示使用Zortress可在保持同样效果下降低使用钙调素抑制剂产生的副作用。 ZORTRESS(依维莫司片) 诺华制药公司 最初美国批准：2010 适应症 •Zortress是mTOR抑制剂，免疫抑制剂在低中度免疫风险接受肾脏移植的成年患者的器官排斥反应的预防。 basiliximab和同时减少剂量环孢素和皮质类固醇联合使用。 使用限制 •使用高免疫风险的患者是不成立的。 •避免使用标准剂量的环孢素，为了减少肾毒性的危险预防肾等器官的使用是不成立的。 •安全和儿童患者的疗效（<18岁）尚未建立   剂量和用法 •开始口服剂量为0.75毫克，每天两次。调整维持剂量依维莫司谷浓度达到3-8 ng / mL的目标范围内。 管理尽快移植后。 建议常规依维莫司和环孢素A治疗药物浓度监测。 •持续管理或与食物，同时作为环孢素。 •中度肝功能不全：每日剂量减少一半和监测血药浓度.   剂型和优势 zortress是0.25毫克，0.5毫克和0.75毫克片剂。 禁忌 •依维莫司，西罗莫司，或药物产品的组件与已知过敏的患者。   注意事项： •血管性水肿：伴ACE抑制剂的风险增加;监察的症状，及时治疗。 •伤口愈合/液体积聚：延迟伤口愈合的风险增加。监测症状，及时治疗，以最大限度地减少并发症。 高脂血症：血清胆固醇和甘油三酯升高是常见的。监测建议;考虑介入，包括抗脂质治疗。 蛋白尿：与谷浓度较高的风险增加;监测尿蛋白。 •多瘤病毒感染激活潜伏的病毒感染的风险; BK病毒相关性肾病已被观察到;考虑减少免疫抑制。 与CYP3A4的强抑制剂和诱导剂的相互作用：同时使用依维莫司谷浓度密切监察。 非感染性肺炎：临床症状或影像学改变的监视器;致命的案件时有发生。管理剂量减少或停止，直到症状消失;考虑使用皮质类固醇。 •公会/ TTP / HUS的：与环孢素合用可能增加风险。血液学变化或临床症状的监测。 移植后新发糖尿病：血糖升高，可能会发生在剂量相关的方式。监测血糖。 •男性不育症：Azospermia或者少精症，可能会出现。 •免疫接种活疫苗，应避免。   不良反应 最常见（发生率≥20％）的不良事件有：血管神经性水肿，便秘，高血压，恶心，贫血，尿路感染，和高脂血症。   药物相互作用 CYP3A4抑制剂和诱导剂：强中度抑制剂（如环孢素，酮康唑，红霉素，维拉帕米）和诱导剂（如利福平）可能会影响everolimus的浓度。血药浓度监测的建议;考虑依维莫司的剂量调整。   在特殊人群中使用 •妊娠：根据动物数据，可能会对胎儿造成伤害。 哺乳母亲：停止药物或护理考虑药物对母亲的重要性。 更新日期：04/2012 Zortress (Everolimus) Zortress (everolimus) is a risky medication that aside from its enormous benefit, may also come up many disadvantages. It lowers the capacity of your immune system. Although everybody hopes for a strong and powerful immune system, sometimes a low sensitivity is a must. This is needed when the patient goes through an organ transplant and the organism rejects it. The rejections occur when the immune system considers the new organ to be an intruder and tries to protect itself. Zortress (everolimus) isn’t recommended for any transplant, but only for the kidney transplant. It is a side medication that has to be used in a tight collaboration with other postoperative drugs. Administration The initial Zortress (everolimus) dosage is of 0.75mg. The patient needs two such doses a day, one in the morning and another one in the afternoon. There should be about 12 hours between the doses. The treatment is applied on a daily basis. The dosage may be adjusted according to more factors. It first depends on the response of the organism and side effects. If the organism takes it well and the immune system still rejects the kidney, the dosage must be increased. New adjustments should only be made after 5 days. This is the optimal time for the first results to show up. The patients must swallow the Zortress (everolimus) pills whole. A full glass of water is also recommended, to ensure that the pill is completely swallowed. Avoid chewing the tablet before swallowing it. If you have problems swallowing it, get more water or let your doctor know. The tablets are available on the market in three different dosages – 0.25mg, 0.5mg and 0.75mg. Contraindications Zortress (everolimus) is contraindicated in the patients suffering from any type of allergies to its ingredients. The analysis performed prior to the kidney transplant usually include analysis for the postoperative treatments as well. This treatment also implies a strict diet. For instance, fruits like grapefruits should be avoided. The chemical components of grapefruit inhibit the effect of the medication, resulting in an ineffective treatment. Lactates are also to be ignored during the treatment. The patients with mild renal and hepatic dysfunctions don’t have any restrictions, unless the diseases they suffer from are severe. Side effects The Zortress (everolimus) treatment implies a good care of the patient. Since the immune system is low, the organism is open to a lot of viruses and bacteria. The most common adverse reactions imply various diseases caused by such invaders.