药品名称 英文药名: Azathioprine Tablets 中文药名: 依木兰 硫唑嘌呤 氮杂硫代嘌呤;咪唑巯嘌呤;依木兰;义美仁;硫唑嘌呤  别名：氮杂硫代嘌呤;咪唑巯嘌呤;依木兰;义美仁;硫唑嘌呤 外文名：Azathioprine,Imuran, AZP 生产厂家 (品牌)生产厂家: Glaxo Smith Kline 葛兰素史克 药理作用 本药是6-硫基嘌呤的咪唑衍生物，为具有免疫抑制作用的抗代谢剂。可产生烷基化作用阻断SH组群，抑制核酸的生物合成，防止细胞的增生，并可引起DNA的损害。动物实验证实，本药可使胸腺、脾内DNA、RNA减少，影响DNA、RNA，以及蛋白质的合成，主要抑制T-淋巴细胞而影响免疫，所以可抑制迟发过敏反应，器官移植的排斥反应。本药的疗效需于治疗数周或数月后才出现。在上消化道内吸收较佳。血浆中的硫唑嘌呤及6-硫基嘌呤水平与本药的疗效及毒性无相互关系。 毒理研究 本药可致染色体异常，动物实验表明可致不同程度的胎儿异常，并具有明显的致畸性，不能排除本药对人体的致癌性。 适应症 本药与其它药物联合应用于器官移植病人的抗排斥反应，例如肾移植、心脏移植及肝移植，亦减少肾移植受者对皮质激素的需求。本药也可单独使用于严重的风湿性关节炎，系统性红斑狼疮，皮肌炎/多发性肌炎，自体免疫性慢性活动性肝炎，寻常天疱疮，结节性多动脉炎，自体免疫性溶血性贫血，慢性顽固自发性血小板减少性紫癜。 用法用量 *注射剂只有在无法口服时才由静脉给药，且当口服疗法可以耐受时即应停用。 器官移植 第1日给予5 mg/kg体重，口服或静注。维持剂量要根据临床需要和血液系统的耐受性而调整，通常为1-4 mg/kg体重/日。维持治疗应无限期地进行。因为如果治疗中断，就有排斥的危险。 其它疾病 开始剂量为1-3 mg/kg体重/日。应根据临床反应和血液学指标所示耐受程度而定。治疗效果明显时，应减少维持量至可保持此治疗效果的最低水平。如3个月内病人情况无改善，应考虑停用。所需维持量从1 mg/kg体重/日至3 mg/kg体重/日不等，取决于临床治疗需要和病人个体反应，包括血液学指标所示的耐受程度。 兼有肝和/或肾功能不全者，剂量酌减。老年人用药的副作用发生率较其他病人高，应采用推荐剂量范围的低限值。 *本药片剂不应被切开。 任何疑问，请遵医嘱！ 不良反应 过敏反应：如全身不适、头晕、恶心、呕吐、腹泻、发热、寒战、肌痛、关节痛、肝功能异常和低血压。应立即停药和给予支持疗法，可使大部分病例恢复。 造血功能：可能产生剂量相关性、可逆性骨髓抑制，常见白细胞减少症，偶见贫血及血小板减少性紫癜。 感染：使用本药和肾上腺皮质激素的器官移植受者对病毒、真菌和细菌感染的易感性增加。 胃肠道反应：偶有恶心，餐后服药可缓解。罕见胰腺炎。 肺部反应：罕见可逆性肺炎。 禁忌症 对本药及6-疏基嘌呤过敏者禁用。 注意事项 在治疗的首8周内，至少每周检查1次全血象，包括血小板。如使用大剂量或病人有肝和/或肾功能不全时，血象检查的次数应该更多。此后每月或最少每3个月重复进行全血象的检查。 对肾和/或肝功能不全者，应使用推荐剂量的低限值及小心地监察血液学及肝肾功能。若出现肝或血液学毒性时，更应再减剂量。用药期间不要进行活疫苗的免疫接种。 孕妇及哺乳期妇女用药 临床上证明本药对胎儿有不良影响，只有对孕妇的益处大于对胎儿产生的危险时，才可考虑使用。本药可分泌入乳汁，故哺乳妇女慎用。 药物相互作用 别嘌呤醇可抑制巯基嘌呤（后者是硫唑嘌呤的活性代谢物）代谢成无活性产物，结果使巯基嘌呤的毒性增加，当二者必须同时服用时，硫唑嘌呤的剂量应该大大地减低，硫唑嘌呤可降低6-巯嘌呤的灭活率，6-巯嘌呤的灭活通过下列方式：酶的S-甲基化，与酶无关的氧化，或是被黄嘌呤氧化酶转变成硫尿酸盐等。硫唑嘌呤能与巯基化合物如谷胱甘肽起反应，在组织中缓缓释出6-巯嘌呤而起到前体药物的作用。 药物过量 症状 无法解释的感染、喉部溃疡、紫癜和出血，通常是用药9-14天达到最大的骨髓抑制而引起。一次性用药过量后，可出现恶心、呕吐及腹泻，接着是轻微的白血球减少和肝功能异常。 治疗 目前尚无特效解毒药，进行胃灌洗后，可予对症支持治疗及密切监察血象。   Azasan is an immunosuppressant, which is a medicament whose purpose is to weaken the immune system. It also goes by the brand name Imuran and is available in tablet form, as an injection, or intravenously. Azasan is given to patients anticipating an organ transplant or who have already been given a new organ, to help prevent rejection by the immune system. It is also given to reduce the signs and symptoms of rheumatoid arthritis, which is a disorder where the immune system attacks the joints and causes severe pain. In some cases, Azasan is used to treat colitis ulcerosa, a chronic condition that causes pain and diarrhea in the intestines. Other inflammatory conditions can be treated by Azasan and include systemic lupus erythematosus, inflammatory myositisis, inflammatory bowel illness, and vasculitis. It usually takes six to eight weeks for your condition to improve, though it sometimes takes up to twelve weeks. Azasan has several different side effects. Most importantly, it can cause a decrease in the number of blood cells in your bone marrow. Call your doctor immediately if you have any unusual bleeding or bruising, fatigue, headache, confusion or dizziness, increased heart rate, weakness, difficulty breathing, sore throat, fever, chills, or any signs of infection. It can also increase your risk of developing some cancers, such as skin cancer and lymphoma. Let your doctor know if you have ever taken any cancer medicaments or if you find suspicious lumps or masses on your body. In addition to the rare but serious side effects above, Azasan's common side effects include an upset stomach, emesis or diarrhea, muscle soreness, blurred vision, mouth sores, coughing, lack of energy or appetite, flu-like symptoms, rash, or yellowing of the skin or eyes. Contact your doctor if these symptoms are severe or do not go away. During the course of your treatment with Azasan, you should be receiving regular blood tests to ensure that these side effects are not inhibiting your treatment. Some people are not able to take Azasan, or may require a lower dose or special monitoring. Studies regarding the effects of Azasan offer contradicting conclusions with respects to the safety of this medicament for pregnant women. Early studies indicated that Azasan would not cause any deformities or problems for a developing fetus, and very little risk for pregnant women or their babies. However, recent studies suggest that fetal harm can result from taking Azasan. No conclusions have been reached as to how much harm or what doses put a fetus in danger. Due to the uncertainty surrounding this subject, exercise extreme caution if you are pregnant and considering treatment with Azasan. Do not breastfeed while taking this medicament since it is considered a cytotoxic medicament and can be harmful to nursing babies.