阿米福汀Ethyol(Amifostine Crystalline Vial)

药店国别： 产地国家：美国 处方药：是 所属类别： 50毫克/毫升/瓶 3瓶/盒 包装规格： 50毫克/毫升/瓶 3瓶/盒 计价单位：盒 生产厂家中文参考译名： 生产厂家英文名：Pinnacle Biologics BV 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 曾用名：

简介

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24 h内不能停药者。 阿米福汀英文版说明书 Generic Name: Amifostine (A-mi-FOS-teen)Brand Name: Ethyol---------------------------------------------------------------Ethyol is used for:Reducing kidney damage due to cisplatin chemotherapy in patients with ovarian cancer. It is also used to reduce moderate to severe dry mouth associated with radiation treatment after surgery for head and neck cancer. It may also be used for other conditions as determined by your doctor.Ethyol is a cytoprotective agent. It works by removing certain substances that cause damage to the kidneys. It also reduces some harmful effects of radiation on healthy tissues.---------------------------------------------------------------Do NOT use Ethyol if:you are allergic to any ingredient in Ethyol or to similar medicinesyou have low blood pressure or you are dehydratedContact your doctor or health care provider right away if any of these apply to you.---------------------------------------------------------------Before using Ethyol:Some medical conditions may interact with Ethyol. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:if you are pregnant, planning to become pregnant, or are breast-feedingif you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplementif you have allergies to medicines, foods, or other substancesif you have a history of blood vessel problems, heart problems (eg, congestive heart failure, irregular heartbeat), stroke or transient ischemic attacks ("mini-strokes"), low blood calcium levels, or kidney problems (eg, nephrotic syndrome)if you are taking medicine to treat high blood pressure or you are receiving chemotherapy for other types of cancerSome MEDICINES MAY INTERACT with Ethyol. However, no specific interactions with Ethyol are known at this time.Ask your health care provider if Ethyol may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.---------------------------------------------------------------How to use Ethyol:Use Ethyol as directed by your doctor. Check the label on the medicine for exact dosing instructions.Ethyol is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Ethyol at home, a health care provider will teach you how to use it. Be sure you understand how to use Ethyol. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.Patients who take blood pressure medicines may need to avoid taking them within 24 hours before or after using Ethyol. If you take medicine for high blood pressure, ask your doctor how to take it along with Ethyol.Do not use Ethyol if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.If you miss a dose of Ethyol, contact your doctor right away.Ask your health care provider any questions you may have about how to use Ethyol.---------------------------------------------------------------Important safety information:Ethyol may cause dizziness or drowsiness. These effects may be worse if you take it with alcohol or certain medicines. Use Ethyol with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.Ethyol may cause low blood pressure. If you experience dizziness, shortness of breath, difficulty breathing, seizures, fainting, or decreased urination, contact your doctor immediately. Patients who take blood pressure medicines may need to avoid taking them within 24 hours before or after using Ethyol. If you take medicine for high blood pressure, ask your doctor how to take it along with Ethyol.Severe and sometimes fatal skin reactions have occurred with Ethyol. This reaction may develop even weeks after you start treatment. The risk may be greater in patients who use Ethyol to reduce dry mouth caused by radiation treatment. If you experience severe rash (eg, redness, scaling, swelling, peeling, or blistering of the skin), fever, mouth sores, or red and irritated eyes, contact your doctor right away.If you experience nausea or vomiting, talk to your doctor about how to avoid becoming dehydrated. Your doctor may prescribe medicine to help decrease nausea and vomiting that may occur while you are using Ethyol.Lab tests, including kidney function, blood calcium and electrolyte levels, and blood pressure, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.Use Ethyol with extreme caution in CHILDREN; safety and effectiveness have not been confirmed.PREGNANCY and BREAST-FEEDING: It is not known if Ethyol can cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Ethyol while you are pregnant. It is not known if Ethyol is found in breast milk. Do not breast-feed while taking Ethyol.---------------------------------------------------------------Possible side effects of Ethyol:All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:Drowsiness; feeling of coldness; flushing/feeling of warmth; hiccups; nausea; sneezing; vomiting.Seek medical attention right away if any of these SEVERE side effects occur:Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); chest pain; chills or shaking; decreased urination; dizziness; fainting; fast, slow, or irregular heartbeat; fever; muscle twitching/cramping; numbness of an arm or leg; red, swollen, blistered, or peeling skin; seizures; severe or persistent nausea or vomiting; severe stomach pain; shortness of breath; sores on the lips, mouth, or tongue; sudden, severe headache; unusual fatigue or tiredness; vision changes.This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.---------------------------------------------------------------If OVERDOSE is suspected:Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include seizures; severe or persistent dizziness; shortness of breath.Proper storage of Ethyol:Ethyol is usually handled and stored by a health care provider. If you are using Ethyol at home, store Ethyol as directed by your pharmacist or health care provider.---------------------------------------------------------------General information:If you have any questions about Ethyol, please talk with your doctor, pharmacist, or other health care provider.Ethyol is to be used only by the patient for whom it is prescribed. Do not share it with other people.If your symptoms do not improve or if they become worse, check with your doctor.This information is a summary only. It does not contain all information about Ethyol. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.