英文药名: Ethyol (Amifostine Crystalline Vial)

中文药名: 氨磷汀（阿米福汀注射剂）
药品简介
氨磷汀(amifostine)是1996年FDA批准在美国上市的第二个细胞保护剂(抗辐射药)。商品名为Ethyol,Ethiofos.
通常用多剂量顺铂对晚期卵巢癌或非小细胞肺癌化疗和用环磷酰胺对晚期卵巢癌化疗时，易出现累积肾毒性。本品可预防和减少这种累积肾毒性。
药理作用
药效学
本品是硫代磷酸盐的前体药物。它的细胞保护作用是由于正常组织中pH较高、碱基磷酸酯酶活性较强，可将氨磷汀迅速完全地去磷酸化而成游离硫羟基(thiol-)的、有药理活性的代谢物(代号WR-1065)，因而保护非肿瘤组织免于化疗和放射疗法的毒性作用，降低环磷酰胺和顺铂对晚期卵巢癌化疗时引起的、与中性白血球减少症有关的感染发生率。正常组织的血液供应较好，提取的氨磷汀多于癌变组织，因而正常组织细胞内活性代谢物WR-1065的浓度较高，可起到区分保护的作用。
药动学
本品的胃肠吸收很差，故不宜口服。在10s内静脉推注本品150mg.m-2后癌症患者的血清药物峰浓度为100～900μmol.L-1，注射后1～4min活性代谢物WR-1065的峰浓度为7～22μmol.L-1。若给癌症患者以740mg.m-2剂量15min静脉输注本品，则5min内可达到血浆浓度100μmol.L-1，输注结束时可达到100～200μmol.L-1。输注后30min时血浆浓度可下降至10μmol.L-1，45min时为2μmol.L-1左右。
本品自血浆中清除迅速，静脉推注或输注后6min内血浆药物水平可下降90%。分布半衰期不到1min，消除半衰期约9min，仅少量原型药物及代谢物自尿中排出。稳态时的平均分布容积为6L。
有限的资料表明，以910mg.m-2静脉输注本品后2.5h时，病人骨髓中WR-1065的水平较低，提示为了对抗半衰期较长的细胞毒性药物(如环磷酰胺)，需多剂量给予氨磷汀才能起到细胞保护作用。
动物实验结果表明，本品在骨髓、胃肠粘膜、皮肤、肝脏及唾液中的浓度较高，而在肌肉中水平较低，脑组织中几乎没有。
适应症
本品可预防顺铂引起的肾毒性和外周神经病，预防环磷酰胺引起的粒细胞白血病和放射疗法引起的骨髓抑制。与顺铂合用可增加顺铂的抗肿瘤效果。用于晚期卵巢癌及转移黑素瘤的放射疗法。亦可用于头颈部癌症、食道癌、肺癌及头部以上的放射疗法。颈动脉病或高钙血症的患者静脉给予本品易发生低血压，建议用较低剂量。
用法用量
建议本品的初始剂量为910mg.m-2，化疗前30min开始静脉输注，输注时间为15min。若收缩压显著低于正常低限则应停止输注。若停药5min内血压恢复正常且患者无任何症状，可继续输注，以使患者获得全部剂量。若患者不能耐受足量氨磷汀，则下一疗程的剂量应减为740mg.m2。本品的最大耐受剂量是每周4d按340mg.m2给予，连续5周。
本品为单剂量包装，每支500mg，应冷藏。
不良反应
本品最重要的不良反应是一过性低血压，在临床研究中约占62%。有低血压的或正处在脱水状态的患者，不得使用本品。正在服用抗高血压药物且24h内不能中断治疗的患者也不能使用本品。给予氨磷汀输注前，应给患者适当水化，静脉补充一些液体。输液氨磷汀的过程中患者应卧床，每隔5min测一次血压。若收缩压明显下降，应立即停药。
恶心或呕吐常发生于氨磷汀输液后，接受顺铂-环磷酰胺化疗第1天并给予本品的患者中有19%出现严重的反应，而未接受本品的患者反应发生率为10%。建议在给予本品之前给予抗呕吐治疗，如地塞米松20mg静注、或5-羟色胺受体阻断剂昂丹司琼和格拉司琼。抗呕吐剂也可与本品合用。
本品可降低血清钙水平，但引致临床上明显的低钙血症发生率低于1%。对有低钙血症危险性的患者(如肾病综合征)应监测血钙水平，必要时补充钙剂。
其它不良反应还有面色潮红、寒战、眩晕、嗜睡、呃逆和打喷嚏。皮疹变态反应发生率低于1%。
禁忌
属孕期用药C级(美国FDA颁布的妊娠期间使用药物危险性等级的分类之一，即动物实验证明对胎儿有不良反应——致畸或致死，尚未在孕妇中进行对照研究)，因可能危及胎儿而在怀孕期间禁用。哺乳期妇女若使用氨磷汀应停止授乳。本品对儿童和老年人的疗效和安全性尚未知。对氨磷汀、氨硫羟化合物、甘露醇等高敏的不良反应禁用。
不良反应有如下情况时慎用：脑血管病或心血管病、低钙血症的不良反应；有脱水或低血压的不良反应；孕妇和哺乳期妇女；正在服用抗高血压药物且24h内不能停药者。

Amifostine Solution for injection
What is this medicine?
AMIFOSTINE (am i FOS teen) is a protective medicine. It is used to prevent or lessen the kidney damage that can be caused by cisplatin chemotherapy. It is also used to prevent some side effects caused by radiation therapy to the head or neck.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•dehydrated
•heart disease
•history of stroke or TIAs
•irregular heartbeat
•low blood pressure
•low levels of calcium in the blood
•taking medicine for high blood pressure
•an unusual or allergic reaction to amifostine, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
This medicine is for infusion into a vein. It is given by a health care professional in a hospital or clinic setting.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•medicines for blood pressure
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Your condition will be monitored carefully while you are receiving this medicine. Visit your doctor as directed.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•chest pain or tightness
•fast, irregular heartbeat
•feeling faint or lightheaded, falls
•fever, chills
•low blood pressure
•nausea, vomiting
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•seizures
•trouble passing urine or change in the amount of urine
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•flushing
•hiccups
•sneezing
•tired
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
This drug is given in a hospital or clinic and will not be stored at home.
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产地国家: 美国
原产地英文商品名:
ETHYOL 50mg/ml Powder for Infusion Solution 3 Vials
原产地英文药品名:
AMIFOSTINE
中文参考商品译名:
氨磷汀 50毫克/毫升/瓶 3瓶/盒
中文参考药品译名:
阿米福汀
生产厂家中文参考译名:
Pinnacle Biologics BV,
生产厂家英文名:
Pinnacle Biologics BV,