【中文品名】安吖啶
【药效类别】抗肿瘤药
【通用药名】AMSACRINE
【别　　名】Amsakrin, AMSA-PD, Amsidine, Amsidyl, NSC-156303, NSC-249992, SN-11841
【化学名称】 Methanesulfonamide, N-[4-(9-acridinylamino)-3-methoxyphenyl]-
【CA登记号】[51264-14-3]
【结 构 式】

【分 子 式】C21H19N3O3S
【分 子 量】393.46
【收录药典】
【开发单位】Auckland Cancer Chemotherapy Labs（无专利保护）
【首次上市】1987年，瑞典
【性　　状】
【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。

药理毒理

安吖啶具有广谱的抗肿瘤活性，作用机理类似蒽环类药物。安吖啶和DNA结合，对腺嘌呤、胸腺嘧啶碱基对的配对有影响。主要抑制DNA合成，对S和G2期细胞抑制作用较明显，对RNA的合成影响较小。
药代动力学

口服吸收较差，通常经静脉给药。在肝脏内代谢，经胆汁排泄。对血脑脊液屏障的渗透性差，脑脊液含量不到血中浓度的20%。
适应症

对急性白血病和恶性淋巴瘤有效。对蒽环类和阿糖胞苷产生耐药的患者无明显交叉耐药性，部分患者仍有效。
用法用量

急性白血病：按体表面积一次75mg/m2，一日1次，静脉注射或滴注，连用7天，最大耐受剂量是150mg/m2。
实体瘤：按体表面积一次75～120mg/m2，3～4周一次。
本药必须在有经验的医生指导和严密观察下应用。一般每日剂量为50～70mg/m2。用药前先将主药1.5ml加入L-乳酸溶液13.5ml中，混匀后溶于5%葡萄糖溶液500ml中（内含主药75mg），静脉滴注，1.5～3小时内滴完，一日1次，连续5～7日为一疗程，或遵医嘱。
不良反应

（1）主要是骨髓抑制，为剂量限制性毒性。当给药量达到90～120mg/m2，即可出现血小板和白细胞减少。
（2）常见胃肠道反应，与剂量有关。常出现低至中度恶心、呕吐。当总剂量达到750mg/m2或更高时，容易发生黏膜炎。
（3）心、肝、神经毒性较轻，个别患者可出现室性心率不齐。较少出现过敏反应和癫痫发作，常伴有脱发。
禁忌

肝功能不良时慎用，或调整剂量。
注意事项

1. 对骨髓抑制及心、肝、神经系统疾病的患者应慎用或适当减少剂量。
2. 为避免静脉炎，应将每次剂量稀释到150ml以上的溶液中，缓慢静滴。
3. 本药遇氯离子易产生沉淀，全部过程中应避免与生理盐水及其他含氯离子的器皿或容器接触。
4. 安吖啶注射液未经稀释前应避免接触塑料制品，包括注射器，最好用玻璃注射器吸药。
5. 未加抗菌剂，故在安瓿开启后应按无菌操作，避免污染，并应在8小时内用完。
6. 安吖啶注射液未稀释前应避免与皮肤或粘膜直接接触，以防止可能发生的组织刺激性。
7. 用药期间应每日查白细胞数及分类，必要时应查骨髓象，以指导用药。
孕妇及哺乳期妇女用药

孕妇及哺乳期妇女应慎用本品。
儿童用药

儿童用药无特殊要求。剂量应按体表面积调整。
老年患者用药

老年患者用药无特殊要求。剂量应适当降低。
规格

1.5ml：75mg。
贮藏

遮光，密闭在阴凉处保存。

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.
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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
处方药:处方药
包装规格: 75毫克/1.5毫升/瓶
销售单价(美元 US$): 280 美元
销售单价(人民币 RMB): 1,848 元
计价单位: 瓶