右雷佐生（dextrorazoxane，Zinecard，得拉唑沙）由美国Chiron公司开发，1992年首先在意大利上市，后在美国、加拿大等国上市，剂型为静脉注射剂，规格为 250mg、500mg/瓶。用于预防蒽环类抗生素引起的心脏毒性。该药与阿霉素给药剂量比为10:1，即给100mg的阿霉素则需给本品1000mg。
大量的临床试验表明，右雷佐生（dexrazoxane，DEX）能有效地预防蒽环类药物诱发的心脏毒性，且不影响化疗药物的抗肿瘤活性。
目前，DEX主要用于晚期乳腺癌患者。DEX在细胞内水解成螯合剂，然后与铁离子结合，干扰Fe3+-蒽环类药螯合物的形成，进而降低含氧自由基的产生。此外，DEX也抑制了这类螯合物对心脂质的过氧化，因而对心脏具有独特的保护作用。

分类名称
一级分类：抗肿瘤药物 二级分类：放疗化疗解毒剂 三级分类： 
 
药品英文名
Dexrazoaxne

药品别名
右亚丙胺、右雷佐生 Adria、Euro-cetus、Cardioxane、ICRF-187、BTG  Zinecard

药物剂型
注射剂(粉)：250mg 500mg。

药理作用
右雷佐生的作用机制尚未完全阐明，但它被认为参与了自由基螯合，而自由基被认为是阿霉素等蒽环类药物引起心脏毒性的主要原因。实验研究表明，本品在体外可选择性地阻断ADM、MTZ等引起的心脏毒性，在体内、体外它对ADM、MTZ的抗肿瘤活性均无影响，同时可减轻有异丙肾上腺素引起的心脏损伤。

药动学
根据对患者进行的固定剂量的ADM(60mg/m2)和逐渐增加剂量的ICRF-187的研究，其结果表明ADM的平均半衰期为39.5h，总的体内清除率为每分钟598ml/m2，不随ICRF-187的剂量变化而变化；血浆中ICRF-187的分布相和清除相半衰期分别为0.46h和4.16h，总的体内清除率为每分钟111ml/m2。不改变ADM的分布、代谢或排泄。

适应证
可用作接受阿霉素等蒽环类药物化疗的患者的心脏保护剂。

禁忌证
对本品过敏者禁用。

注意事项
用药期间宜定期复查血象，必要时应停药或给予升白治疗.

不良反应
主要为骨髓抑制，当本品与ADM的用药比例为12.5∶1或15∶1合用时，可出现明显的白细胞减少。

用法用量
静脉注射：在使用ADM前30min，在15min内将本品输注完毕，其剂量为ADM的20倍，即ADM∶ICRF-187＝1mg∶20mg。
 
药物相应作用
尚不明确。

专家点评
本品自身无抗癌活性，它的应用主要用来减少抗癌药的副作用，它可阻断ADM和MTZ的心脏毒性，与这两药配伍使用可增加安全性。

 
Medication name
Generic name: Dexrazoxane-Injection
Pronunciation: (DEX-ra-ZOX-ane)
Brand name(s): Zinecard
Uses
Dexrazoxane is used to reduce the risk and severity of heart damage caused by doxorubicin treatment and similar cancer chemotherapy medications. Heart damage limits the length of time you can be treated with doxorubicin. Dexrazoxane allows you to continue doxorubicin treatment for longer. When used for this purpose, dexrazoxane treatment is usually started after you have received several doses of doxorubicin. It is usually not given with the first doses of doxorubicin since doing so may reduce the effectiveness of doxorubicin.
Other uses
This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.Dexrazoxane is also available in another brand that is used to reduce serious tissue injury if doxorubicin or a related chemotherapy drug has leaked out of the vein into the surrounding tissue.
How to use
This medication is usually given by injection into a vein by a health care professional.When this medication is used to reduce the risk and severity of heart damage, the doxorubicin dose is usually given within 30 minutes after the start of the dexrazoxane infusion.If skin contact should occur, wash the area with plenty of soap and water. If irritation occurs, contact your doctor right away.Heart damage may occur at any time with doxorubicin treatment, even years after the end of your doxorubicin treatment. Tell your doctor right away if you have symptoms of heart damage such as sudden nighttime shortness of breath, difficulty breathing while lying down, or shortness of breath when active.
Precautions
Before using dexrazoxane, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. However, because this drug may have undesirable effects on a nursing infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
Drug interactions
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.One product that may interact with this drug is: natalizumab.
Side effects
Pain at the injection site may occur. If this effect persists or worsens, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: signs of infection (such as fever, persistent sore throat), easy bruising/bleeding.Very rarely, people with cancer who have been treated with this medication have developed other cancers (such as leukemia, lymphoma). Consult your doctor for more details.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Missed dose
For the best possible benefit, it is important to receive each scheduled dose of this medication as directed. If you miss a dose, contact your doctor or pharmacist immediately to establish a new dosing schedule.
Overdose
If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.
Notes
Keep all medical appointments while using this medication. Laboratory and/or medical tests (such as complete blood counts, heart function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.
Storage
Not applicable. This medication is given in a clinic and will not be stored at home.
Photos by medication strength
Click the "Photos" link to see sample photographs for a specific medication strength.
Common strengths
Zinecard 250 mg IV Solution
Zinecard 500 mg IV Solution
Important note
HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

Information last revised March 2012. Copyright(c) 2012 First Databank, Inc.

Intravenous
Recon Soln
Dexrazoxane|
Doxorubicin-Induced Cardiomyopathy|
Heart Muscle Disease caused by the Medication Doxorubicin|
Selected from NATIONAL DRUG DATA FILE (NDDF) data included with permission and copyrighted by First DataBank, Inc., 2012. This copyrighted material has been downloaded from a licensed data provider.
The above information is intended to supplement, not substitute for, the expertise and judgment of your health care professional. You should consult your health care professional before taking any drug, changing your diet, or commencing or discontinuing any course of treatment.

右雷佐生临床适用于预防蒽环类药物诱发的心脏毒性。上市剂型为注射剂，规格为250mg和500mg两种，稀释液分别为0.167mol/l乳酸钠25ml，50ml。
右雷佐生（dexrazoxane）是消旋雷佐生（razoxane）的d-异构体，也是螯合剂乙二胺四乙酸（EDTA）的亲脂性衍生物，能迅速透过细胞膜，降低多柔比星等蒽环类抗肿瘤抗生素的心脏毒性，右雷佐生在细胞内水解为TCRE-198，再与细胞内的铁螯合，使三价铁离子与多柔比星等蒽环类抗肿瘤药物的复合物减少，防止自由基的形成而起效的。右雷佐生还能抑制拓朴异构酶II产生的细胞毒性作用，在动物模型中对某些抗肿瘤药物的细胞毒性有增强或拮抗作用。右雷佐生是目前临床上认可的唯一用于预防蒽环类药心脏毒性的药物，目前在欧美国家的临床试验表明，该药有望成为蒽环类抗肿瘤药物的标准配伍用药。尽管目前右雷佐生主要用于预防蒽环类药物诱发的心脏毒性，但该药在调节拓朴异构酶II的活性和细胞铁代谢等方面的潜力，未来在癌症治疗、免疫学、感染性疾病等方面的应用将可能成为重点。      
大量临床试验已证实，对于蒽环类药物引起的心肌损害，右雷佐生能提供有效的预防作用，不仅不影响化疗药物的抗癌活性，而且允许化疗药物给予较高的累积剂量。右雷佐生在许多国家已得到批准，用于降低蒽环类药物引发的心脏毒性。采用超声波心动描记法或左心室射血分数（LVEF）及心肌内膜活检作为心脏毒性的参数。当本品与多柔比星的比率为20:1或10：1时，本品能降低多柔比星引起的心脏毒性。本品组病人心脏事件的危险率比对照组低50%～67%，充血性心衰的危险率比对照组低87.5%～90%。本品组病人能耐受较高累积剂量的多柔比星，多柔比星从300mg/m2之后开始用药时仍有心脏保护作用，发生心脏事件的危险性下降77.80%。与高剂量表柔比星联合治疗时，右雷佐生与表柔比星的剂量比为10：1时具有心脏保护作用。右雷佐生对接受含阿霉素化疗方案治疗的儿童患者亦是有益的。上述数据表明本品是一安全、有效的心脏保护剂。
近年来DOX与PAC联用也是治疗晚期乳腺癌的一个有效方案，客观有效率可达50%～90%。紫杉醇也具有心脏毒性，可导致心动过缓等，已有建议将右雷佐生加入到这一方案中。动物实验显示，紫杉醇不加剧DOX诱发的慢性心肌病变，右雷佐生加入到DOX和紫杉醇联合方案中，对DOX诱发的心脏毒性仍具有预防作用，且不增加非心脏毒性。为了降低蒽环类药与紫杉烷类药联用的心脏毒性，目前提出了多种方案（包括使用右雷佐生），有关右雷佐生在上述联用方案中的实际效果尚需在临床试验中进行评价。
研究表明，接受过蒽环类药物治疗有可能长期存活的癌症者，有发生进行性心脏毒性的危险。早期就开始使用心脏保护剂是否能降低这种危险，有待进一步研究。
详细资料附件1：http://www.drugs.com/pro/zinecard.html
详细资料附件2：http://www.rxlist.com/zinecard-drug.htm