| 【中文别名】正定霉素，柔毛霉素，红比霉素，红保霉素，佐柔比星，红比脘。 【外 文 名】Daunorubicin,Daunomycin,Daunoblastin,Rubidomycin,Rubomycin,Ondena,Cerubidine. 【外文缩写】DNR，DRB，DM，F.I.6339,NSC-82151,13057R.P。 【化 学 名】（1S，3S）-3-乙酰基-1，2，3，6，11-六氢-3，5，12-三羟基-10-甲氧基-6，11-二氧-1-1萘基-3-氨基-2，3，6-三去氧-a-L来苏六吡喃糖甙。 【分 子 式】C27H29NO10。 【性状】本品为橙红色针状结晶，易溶于水，其水溶液相当稳定，在0℃ 能保存3周，其活力不变，不溶于氯仿、丙酮、乙醚、苯。 【药理作用】pp本品为Str.peucetius或Str.coeruleorubidus菌种所产生的抗生素，是从我国河北正定县土壤中得到的放线菌菌株，故亦名正定霉素。本品与ADM都具有一个蒽环平面，可通过它嵌合于DNA碱基对之间并紧密地结合到DNA上，因而使核酸中含有相当高浓度的药物，这种嵌合可导致DNA空间结构的障碍，从而抑制DNA及DNA依赖的RNA合成，对RNA的影响尤为明显，并可选择性作用于嘌呤核苷。本品虽为细胞周期非特异性药物，对增殖细胞各期均有杀伤作用，但对G2作用更为显著。 【体内过程】pp本品口服不吸收，静脉注射后能广泛分布于各组织，在骨髓、肠道、血细胞内分布较多，其次为心、肝、肾，在淋巴腺和骨髓内最高浓度可维持8~24小时，但不能进入脑脊液中。药物通过主动转运进入细胞，细胞对药物主动转运的抑制是造成耐药的主要原因。血中半衰期为30-50小时。药物主要在肝内代谢成羟化的与结合的代谢物，其中在肝内工谢成的阿霉素配基主要从胆汗中排除，通过胆汁外排是其主要消除方式，仅有5%~15%从尿中排泄，给药后3日患者尿呈橘红色。 【临床应用】 （1）主要用于急性粒细胞性白血病，对小儿急性淋巴细胞白血病（VP方案首选）缓解率达60%，与强的松、Ara-C或VCR合同可提高疗效。 （2）与博莱霉素、CTX合同，对成骨肉瘤有效率为61.5%。 （3）对淋巴肉瘤、神经母细胞瘤、骨骼肌瘤、绒癌亦有一定疗效。 【用法用量】pp成人：开始0.5~0.8mg/kg，以生理盐水或5%葡萄糖液250ml稀释后静脉滴注，1小时内滴完，每周2次；亦可1mg/kg，每日1次，连用5日。总量实体瘤为8~10mg/kg。 小儿：1mg/kg，以生理盐水或5%葡萄糖液稀释，连用2~5日，每周期总量不超过1.5mg/kg，每周期间隔至少7-10日，总共不宜超过4个周期，总剂量不超过6mg/kg。 【不良反应】 （1）骨髓抑制：白细胞下降在给药后2~4周达到最低点，发生率为45%~90%；血小板下降，尤以儿童明显。 （2）胃肠道反应：恶心，呕吐，腹痛，腹泻，口腔溃疡和肝功能障碍。 （3）心脏毒性：突发性心动过速，呼吸困难，心脏扩大，急性心力衰竭，肺水肿等，能迅速导致死亡，病检可见多灶性心肌退行性变。心脏毒性发生率为2%~10%。 （4）其他反应：部分患者可出现蛋白尿、皮疹、脱发等；漏出血管外时可致局部坏死。 【禁 忌 证】 （1）心肌损伤、骨髓抑制患者禁用。 （2）孕妇及免疫机能低下者禁用。 （3）肝功能受损者慎用。 【注意事项】 （1）本品在肝脏中氧化还原水解而代谢，有肝肠循环，故首次剂量不宜过大，且应严密注意蓄积。 （2）本吕毒性较大，使用剂量应依血像而定。 （3）一般稀释至2mg/ml后静脉注射或静脉滴注。 （4）静脉注射时勿使药物漏出血管外，以免致局部坏死；静脉滴注时不宜过快，以免引起心律失常。 （5）骨髓抑制明显者，应及时停药，必要时可给予抗生素、输血或其他措施。 （6）对高年龄患者及有心脏病史的病人应注意剂量选择。 （7）为防止脱发，可在用药前10分钟于头皮局部降温30分钟，使局部血流减慢，而减少药物进入毛囊。 （8）本品不宜与酸性、碱性药物配伍，以防失效。 【制剂规格】pp注射剂：10mg/支，20mg/支。价格相对甲氧柔红霉素便宜许多。但副作用较甲氧柔红霉素稍大。
Cerubidine® (Daunorubicin Hydrochloride) for Injection Daunorubicin hcl is used for treating certain types of cancer.Daunorubicin can cause tissue damage if it is injected by a route other than through the vein. Notify your doctor immediately if redness, pain, and swelling occur at or around the injection site. Daunorubicin may cause heart problems, including heart failure, or bone marrow depression, making it hard to fight off infection. Notify your doctor immediately if you develop chest pain, an irregular heartbeat, trouble breathing, swelling of the hands or feet, easy bruising or bleeding, or signs of infection, such as fever, unusual fatigue, or persistent sore throat. Tell your doctor if you have liver or kidney problems before starting treatment with Daunorubicin . You may require smaller doses. Treating certain types of cancer. It may be used in combination with other medicines. It may also be used for other conditions as determined by your doctor. Daunorubicin is a cytotoxic agent. It works by preventing the cancer cell from reproducing, which results in death of the cancer cell. Do NOT use Daunorubicin if: you are allergic to any ingredient in Daunorubicin Contact your doctor or health care provider right away if any of these apply to you. Before using Daunorubicin : Some medical conditions may interact with Daunorubicin . 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-feeding if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement if you have allergies to medicines, foods, or other substances if you have bone marrow depression, heart disease, gout, or liver or kidney problems, or if you have taken Daunorubicin before Some MEDICINES MAY INTERACT with Daunorubicin . Tell your health care provider if you are taking any other medicines, especially any of the following: Certain medicines that act upon the liver (eg, methotrexate) or cyclosporine because the actions and side effects of Daunorubicin may be increased Trastuzumab because the risk of heart problems may be increased Hydantoins (eg, phenytoin) because the effectiveness may be decreased and the risk of seizures may be increased by Daunorubicin How to use Daunorubicin : Use Daunorubicin as directed by your doctor. Check the label on the medicine for exact dosing instructions. Daunorubicin is usually administered as an injection at your doctor's office, hospital, or clinic. If Daunorubicin contains particles or is discolored, or if the vial is cracked or damaged in any way, do not use it. Keep this product, as well as syringes and needles, out of the reach of children and away from pets. Do not reuse needles, syringes, or other materials. Dispose of properly after use. Ask your doctor or pharmacist to explain local regulations for proper disposal. If you miss a dose of Daunorubicin , contact your doctor as soon as possible. Ask your health care provider any questions you may have about how to use Daunorubicin . Important safety information: If nausea, vomiting, or loss of appetite occurs, ask your doctor or pharmacist for ways to lessen these effects. If you get Daunorubicin on your skin, wash thoroughly with soap and water. Daunorubicin may lower your body's ability to fight infection. Prevent infection by avoiding contact with people with colds or other infections. Notify your doctor of any signs of infection, including fever, sore throat, rash, or chills. Daunorubicin may reduce the number of clot-forming cells (platelets) in your blood. To prevent bleeding, avoid situations in which bruising or injury may occur. Report any unusual bleeding, bruising, blood in stools, or dark, tarry stools to your doctor. Daunorubicin causes the urine to turn red. This is harmless and not a cause for concern. Check with your doctor before having vaccinations while you are using Daunorubicin . LAB TESTS, including blood cell counts; heart, liver, and kidney function tests; and uric acid levels, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments. Use Daunorubicin with caution in CHILDREN because they may be more sensitive to its effects, such as heart problems. PREGNANCY and BREAST-FEEDING: Daunorubicin may cause harm to the fetus. If you become pregnant, discuss with your doctor the benefits and risks of using Daunorubicin during pregnancy. It is unknown if Daunorubicin is excreted in breast milk. Do not breast-feed while taking Daunorubicin . Possible side effects of Daunorubicin : 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: Diarrhea; hair loss; loss of appetite; mouth pain; nausea; sore throat; stomach pain; tiredness; weakness. |
