AMSIDINE INJECTION 75mg/1.5ml/bottle（安吖啶） 【用　　途】 一种细胞生长抑制剂，用于治疗成人成淋巴细胞和成髓细胞白血病。 分类名称 一级分类：抗肿瘤药物 二级分类：其他抗肿瘤药物 三级分类：  药品英文名 Amsacrine 药品别名 安沙吖啶、胺苯吖啶、注射用胺苯吖啶Amsacrine、Amsidine、Amsacrinum、Amsidinevial 药物剂型 胺苯吖啶：注射剂，英国派德公司生产。5%，每支1.5ml含75mg(附稀释剂)。 药理作用 本品是第一个吖啶类抗癌药，其作用机理类似于蒽环类，与腺嘌呤-胸腺嘧啶碱基对有相互作用，通过嵌入和外结合两种方式与DNA结合，从而阻止DNA作为DNA复制和RNA合成的模板，对S和G2期细胞抑制作用明显。尚能干扰细胞膜蛋白质的结构而产生抗肿瘤活性。本品静脉给药后在肝内与谷胱甘肽结合而代谢，主要代谢产物经胆汁排泄，肾功能不全者消除相半衰期延长不太显著，而严重肝功能障碍者，可大大延长其半衰期。 药动学 本品口服后吸收较差，在剂量120mg/m2时吸收最完全，通常每3～4wk静脉给药1次(90～120mg/m2)，可分布于肝、肾、心肌，不易透过血脑屏障进入脑脊液，可通过胎盘屏障进入胎体，并向乳汁移行，在血浆中清除呈双相，血浆分布半衰期为0.20～1.66小时，血浆消除半衰期为3～10h。在肝内与谷胱甘肽结合而代谢，最终代谢物为奎诺亚胺的谷胱甘肽结合体。代谢物80%经胆汁排泄，少量经肾脏排泄，严重肝肾功能不全者消除半衰期稍增加，但严重肝功能障碍的患者，消除半衰期则大为增加。 适应证 用于对成人急性非淋巴性白血病，与高剂量阿糖胞苷合并治疗复发的急性非淋巴细胞性白血病患者，其完全缓解率达70%。亦试用于其他类型急性白血病、淋巴瘤和实体癌，但疗效不佳。 禁忌证 心律失常和心肌病患者应慎用。孕妇慎用。已有骨髓抑制者禁用 注意事项 1.本品骨髓抑制作用很强，须经常查血象，且应在经验丰富的肿瘤专科医生监护下用药。 2.用药期间定期检查肝、心、肾功能，及时调整剂量。 3.本品可引起因肿瘤细胞的急速溶解而继发的高尿酸血症，必须密切监测血中尿酸含量。 4.孕妇应慎用。 5.不能与含有氯离子的溶液如生理盐水、糖盐水等相配伍。 6.有些患者单用安吖啶时会出现感染(发热和粒细胞减少)，有时会危及生命。一次应用0.75g/m2或更大剂量时约有80%患者出现口腔炎。将本品稀释到150ml以上的液体中，可以避免静脉炎的发生。 不良反应 为剂量依赖性毒性，主要为骨髓抑制和黏膜炎。规定剂量范围内约10%病人有胃肠道反应，常见有恶心、呕吐、胃炎、口腔炎、腹泻及直肠周围脓肿等。也有肝脏毒性、中枢神经毒性和心毒性的报道。尚有脱发、皮疹及全身无力等症状。骨髓抑制，常见白细胞和血小板计数减少、贫血，这种毒性在3～4wk内给予剂量90～120mg/m2时即会出现。常见脱发、皮疹、全身无力、静脉炎。偶发肝脏、神经和心脏毒性。 用法用量 静滴：只能用附带的L-乳酸稀释液混合后，再用5%葡萄糖液稀释(不得用其他溶液稀释)。3～4周1次，剂量为90～120mg/m2，1疗程为500～750mg/m2。 药物相应作用 不能与含有氯离子的溶液配伍。本品不会增加阿霉素、多柔比星所致的心脏毒性作用。 专家点评 国内报道，本品对急性白血病和恶性肿瘤均有较好的疗效，尤其联合用药。对急性非淋巴细胞性白血病的完全缓解率为16%～20%。-(中国新药与临床杂志，1991年)对蒽环类和阿糖胞苷已产生耐药性的患者，改用本品仍有缓解作用无交叉耐药性。(Leuk Res，1986年)国外报道，在适当剂量下本品也对淋巴瘤有效，对6例霍奇金淋巴瘤患者治疗，50%有效；对23例非霍奇金淋巴瘤患者中6例有效，有效率26%；对转移细胞膀胱癌患者有效，但不如CAP方案(环磷酰胺、阿霉素、顺铂)。(Cancer Chemotherapy，1986年)   Amsacrine (Amsidine®) Amsacrine is a chemotherapy| drug that is usually given in combination with other chemotherapy drugs to treat types of adult and childhood leukaemia|. What amsacrine looks like Amsacrine is an orange/red coloured fluid. How it is given Amsacrine is given by a drip (infusion) in one of the following ways: through a fine tube (cannula) placed into the vein, usually in the back of the hand through a fine plastic tube inserted under the skin into a vein near the collarbone (central line ) into a fine tube inserted into a vein in the crook of your arm (PICC line ). The infusion usually takes between 60 and 90 minutes.  Chemotherapy is usually given as a course of several sessions (or cycles) of treatment over a few months. The length of your treatment and the number of cycles you have will depend on the type of cancer for which you are being treated. Your nurse or doctor will discuss your treatment plan with you. Possible side effects Each person's reaction to chemotherapy is different. Some people have very few side effects, while others may experience more. The side effects described here won't affect everyone who is given amsacrine, and may be different if you are having more than one chemotherapy drug. We have outlined the most common side effects and also some of the rarer ones, so that you can be aware of them if they occur. However, we haven't included those that are very rare and therefore extremely unlikely to affect you. If you notice any effects that are not listed in this information, please discuss them with your doctor or nurse. Feeling sick (nausea) and being sick (vomiting) This may begin a few hours after the treatment is given and last for up to a day. Your doctor can prescribe very effective anti-sickness (anti-emetic) drugs to prevent or greatly reduce nausea and vomiting| . If the sickness isn't controlled, or if it continues, tell your doctor; they can prescribe other anti-sickness drugs which may be more effective. Some anti-sickness drugs can cause constipation. Let your doctor or nurse know if this is a problem. Lowered resistance to infection Amsacrine can reduce the production of white blood cells by the bone marrow, making you more prone to infection| . This effect can begin seven days after treatment has been given, and your resistance to infection usually reaches its lowest point 11-13 days after chemotherapy. The number of your white blood cells will then increase steadily and usually returns to normal levels before your next course of chemotherapy. Contact your doctor or the hospital straight away if: your temperature goes above 38°C (100.4°F) you suddenly feel unwell (even with a normal temperature). You will have a blood test before having more chemotherapy to make sure that your cells have recovered. Occasionally, it may be necessary to delay your treatment if the number of blood cells (the blood count) is still low. Bruising or bleeding Amsacrine can reduce the production of platelets, which help the blood to clot and stop bleeding. Let your doctor know if you have any unexplained bruising or bleeding, such as nosebleeds, blood spots or rashes on the skin, or bleeding gums. Anaemia (low number of red blood cells) While having treatment with amsacrine you may become anaemic. This may make you feel tired| and breathless| . Let your doctor or nurse know if you develop these symptoms. Discoloured urine  Your urine may become an orange colour. This may last up to 24 hours after you have had amsacrine and is due to the colour of the drug. It's normal and nothing to worry about. Tiredness and feeling weak You may feel very tired| . It's important to allow yourself plenty of time to rest. Less common side effects Diarrhoea This can usually be controlled with medicine, but let your doctor know if it is severe or if it continues. It is important to drink plenty of fluids if you have diarrhoea| . Hair loss If your hair falls out it usually starts 3-4 weeks after the first dose of amsacrine, although it may happen earlier. Your hair might fall out completely or may just get thinner. You may also have thinning and loss of your eyelashes, eyebrows and other body hair. Hair loss| is temporary and your hair will regrow once the treatment ends. Your nurse can give you advice about coping with hair loss. Mouth sores and ulcers Your mouth may become sore| , or you may notice small ulcers during this treatment. Drinking plenty of fluids, and cleaning your teeth regularly and gently with a soft toothbrush, can help to reduce the risk of this happening. Tell your nurse or doctor if you have any of these problems, as they can prescribe special mouthwashes and medicines, which prevent or clear mouth infections. Taste changes You may notice that your food tastes different. Normal taste will usually come back after the treatment finishes. Abdominal pain Let your doctor know if you develop any abdominal (tummy) pain. It can usually be controlled with mild painkillers. Pain and swelling at the injection site If you feel pain, tell the doctor or nurse. They can slow the drip, which should reduce the feeling. Changes to the normal rhythm of the heart If this happens, it's usually temporary and can be reversed with medication. Your heart function is likely to be checked before treatment starts. You will also have regular blood tests to check the chemicals in the blood, as changes in the level of one of these chemicals (potassium) can affect the normal rhythm of the heart. Additional information Injection site  If the area around the injection site becomes red or swollen you should tell the nurse or doctor on the ward. If you are at home, ring the clinic or ward and ask to speak to someone. Risk of blood clots  Cancer can increase your risk of developing a blood clot (thrombosis), and having chemotherapy may increase this risk further. A blood clot may cause symptoms such as pain, redness and swelling in a leg, or breathlessness and chest pain. Blood clots can be very serious, so it's important to tell your doctor straight away if you have any of these symptoms. However, most clots can be treated with drugs that thin the blood. Your doctor or nurse can give you more information. Other medicines  Some medicines, including those you can buy in a shop or a chemist, can be harmful to take when you are having chemotherapy. Let your doctor know about any medicines you are taking, including over-the-counter drugs, complementary therapies and herbal drugs. Fertility Your ability to become pregnant or father a child may be affected by taking this drug. It's important to discuss fertility| with your doctor before starting treatment. Contraception It's not advisable to become pregnant or father a child while taking amsacrine as it may harm the developing foetus. It is important to use effective contraception whilst taking this drug, and for at least a few months afterwards. Again, discuss this with your doctor. ------------------------------------------------------------- 原产地英文商品名: AMSIDINE INJECTION 75mg/1.5ml/bottle 原产地英文药品名: AMSACRINE 中文参考商品译名: AMSIDINE注射剂 75毫克/1.5毫升/瓶 中文参考药品译名: 安吖啶 中文参考化合物名称: N-[4-(9-吖啶氨基)甲基苯基]甲磺酰胺 产地国家: 加拿大 所属类别: 抗癌药物->治疗白血病药物