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 详细处方信息以本药内容附件PDF文件（2010122822004425.pdf）的“原文Priscribing Information”为准
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部分中文安吖啶处方资料（仅供参考）

安吖啶Amsacrine

[中文别名] 胺苯吖啶，胺苯比啶，安沙克林。

[外 文 名] Acridiylaminon,Amsarcrine,Amsidine,Methancsulfonamide,Amekrin.

[外文缩写] AMSA，M-AMSA，AMS，CI-880，NSC-156303，SN-11841。

[化 学 名] N-[4-(9-吖啶氨基)甲基苯基]甲磺酰胺。

[分 子 式] C21H19N3O3S。

[性 状] 本品为橙红色结晶性粉末，在碱性条件下，乙酸乙酯几乎能定量地吸收水中的该药原形物，关能使药物与蛋白解离或与胆汁中的主要代谢物分离。本品的盐酸盐，水溶性差，另含有甲碘酸盐、乳酸盐和葡萄糖酸盐等。

[药理作用] 本品是一系一合成的吖啶类衍生物中筛选出来的抗肿瘤新药，为Can等于1974年首次合成，具有广谱的抗瘤活性、免疫抑制和抗病毒作用。本品主要是能和细胞DNA5`末端起共价结合或与核内DNA拓扑异构酶Ⅱ的活力，使与蛋白连结的DNA的合成；干扰细胞膜蛋白质构象。在细胞周期中主要作用于G2期及G2/M边界期细胞，对G1期有S期作用较小。

[体内过程] 本品口服吸收较差，通常静脉给药。口服90mg/m2,4~6小时血药浓度达峰值(0.63~1.3μg/ml)，当口服剂量无关。静脉滴注90mg/m2后，体内血浆清除量双相曲线，t1/2α为10~15分钟，t1/2β为8~9小时。本品吸收后，广泛分布于肾、肺心、脾和肝中，均比血中高。在肝脏内浓度最大，主要以代谢物吸收形式存在， 在脑脊液中最低。在血清内浓度为1~100μg/ml时，与蛋白结合占80%~90%。本品主要经肝脏代谢、失活，最终代谢产物为9-氨基吖啶(9-AA)，肝功能不良可影响其代谢；主要从胆汁排泄，胆汁药物浓度与血浆药物浓度的比为400：1，在胆汁中的峰值时间为5小时，部分经肾排泄，肾功能不全对其排泄影响不大。

[临床应用] 本品是继蒽环类、阿糖胞苷后又一种治疗急性粒细胞白血病有交药物，对急性白血端正的缓解率为50%；与大剂量Ara-C、6-TG、VP-16等联合治疗晚期急性粒细胞白血病可提高疗效。对蒽环类和Ara-c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。
    本品对恶性淋巴瘤也有较好疗效，亦可用于乳腺癌。

[用法用量] 静脉滴注：急性白血病，75mg/m2，连用7日；最大耐受量为150mg/m2,连用5日。实体瘤，75~120mg/m2,3~4周1次，总量500~700mg/m2为1周期。

[不良反应]
    (1) 骨髓抑制：为剂量限制毒性，有药后10~14日白细胞达最低点，21~25日恢复泻；亦有血小板及血红蛋白减少等。
    (2) 胃肠道反应：食欲不振、恶心、呕吐、腹泻等。
    (3) 心脏毒性：部分病例人有心悸、胸闷、心力衰竭、室性纤维颤动等，总发生率<5%。
    (4) 肝功能损害：较大剂量可出现血清碱性磷酸酶和胆红素升高，发生率为35%，但多数为可逆性反应。
    (5) 其他反应：粘膜炎、皮疹、感觉异常、头痛、头晕、关节痛、。静脉炎与脱发较常邮；偶见癫痫大发作。

[注意事项]
    (1) 严格掌握剂量，在用药期间应监测病情变化，及时调整剂量。
    (2) 每次使用时以5%葡萄糖150ml以上将药液稀释，静脉点滴1小时，及时更换注射部位。
    (3) 凡能影响微粒体酶的药物如苯巴比妥、西咪替丁等均可影响本品药支学参数。
    (4) 本品与Ara-C、Vp-16合用能增台疗效。

[制剂规格] 注射剂：75mg/1.5ml,附稀释剂。

[贮 藏] 室温，阴凉处保存，勿冻结。

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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 详细处方信息以本药内容附件PDF文件（2010122822004425.pdf）的“原文Priscribing Information”为准
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2010-12-29更新