药物说明书drins-雷替曲塞-正大

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噻奈普汀钠片使用说明书

噻奈普汀钠片使用说明书请仔细阅读说明书并在医师指导下使用噻奈普汀钠片使用说明书【药品名称】通用名称：噻奈普汀钠片商品名称：达体朗英文名称：TATINOL (Tianeptine Sodium Tablets)【成份】噻奈普汀钠【性状】白色包衣片。

【适应症】抑郁发作（即典型性）。

【规格】12.5mg【用法用量】推荐剂量是每日三次：一次一片（含噻奈普汀钠12.5mg），于三餐（早、中、晚）前口服。

对于慢性酒精中毒病人，无论是否存在肝硬化，均无必要改变剂量。

对于超过70岁的病人，和存在肾功能不全的病人，剂量应限制在每日二片，或遵医嘱。

【不良反应】罕见，一般并不严重：·上腹疼痛，腹痛，口干，厌食，恶心，呕吐，便秘，胀气；·失眠，嗜睡，恶梦，虚弱；·心动过速，期外收缩，心前区疼痛；·眩晕，头痛，晕厥，震颤，颜面潮红；——呼吸不畅，喉部堵塞感；——肌痛，背痛等。

【禁忌】·对本品或本品中任何成分过敏者；·未满15岁的儿童；·与MAOI（单胺氧化酶抑制剂）类药物合用；·在开始噻奈普汀治疗前，必须停用MAOI类药物二周。

而本来服用噻奈普汀改为MAOI类药物治疗的病人，只需停服噻奈普汀24小时。

【注意事项】·带有遗传性自杀倾向的抑郁症病人服用本药时必须密切监护，特别是在治疗伊始。

·如需进行全身麻醉，应告知麻醉师病人正在服用本药，并在手术前24或48小时停药。

·需进行急诊手术时，可不必有停药期，需进行术前监测。

·与所有治疗精神疾病药物相同，如中断治疗，需逐渐减少剂量，时间为7至14天以上。

·对驾车或操纵机器能力的影响·部分病人会出现警觉力下降。

因此，司机或机器操纵者需注意服用本药时易出现嗜睡的危险。

【孕妇及哺乳期妇女用药】妊娠期在动物，研究发现本药对生殖功能无不良影响，仅有极少量的药物通过胎盘，未见胎儿体内蓄积作用。

雷替曲塞

雷替曲塞雷替曲塞，Raltitrexed英文化学名：S)-2-[(1-{5-[Methyl-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylm ethyl)-amino]-thiophen-2-yl}-methanoyl)-amino]-pentanedioic acid 中文化学名：N-[5-[N-甲基-N-(2-甲基-4-氧代-3,4-二氢喹唑啉-6-基甲基)氨基]-2-噻吩甲酰基]-L-谷氨酸分子式： C21H22N4O6S分子量：458.49质量标准：企标成分：雷替曲塞、甘露醇、氢氧化钠和磷酸氢二钠。

性状：白色或类白色疏松块状物或粉末规格2mg/支【药物名称】雷替曲塞粉针 Raltitrexed Injection【分子式成分】N-[5-[N-甲基-N-(2-甲基-4-氧代-3，4-二氢喹唑啉-6-基甲基)氨基]-2-噻吩甲酰基]-L-谷氨酸【制剂规格】本品为白色冻干粉末，每瓶含雷替曲塞2 mg。

【药理毒理】药理学研究表明，雷替曲塞为新一代水溶性胸苷酸合酶抑制剂，该药通过细胞膜外还原型叶酸盐载体系统将本品主动摄入细胞内，而后迅速代谢为多谷氨酸类化合物抑制胸苷酸合酶的活性，并能在细胞内潴留，长时间发挥作用。

它对结肠直肠癌细胞系的抑制作用强于5-氟尿嘧啶，雷替曲塞的IC50长期给药为1.3～3.9 nmol/L，短期给药为80 nmol/L，而5-氟尿嘧啶与甲酰四氢叶酸合用长期给药IC50为330～5800 nmol/L，短期给药为150000 nmol/L。

体外研究观察到雷替曲塞与5-氟尿嘧啶联合用药有协同作用，这种作用依赖于给药方案和剂量。

对176例晚期结肠直肠癌患者进行的II期临床试验，给予雷替曲塞3 mg/㎡，每3周1次，有25.6%产生综合疗效，从治疗到病情进展平均时间为4.2周，存活期平均为11.2月。

1300多例晚期结肠直肠癌患者的3项III期临床研究结果表明，雷替曲塞治疗组（每3周1次，每次3 mg/㎡）与5-氟尿嘧啶加甲酰四氢叶酸治疗组（5-氟尿嘧啶425mg/㎡加甲酰四氢叶酸20 mg/㎡或5-氟尿嘧啶400 mg/㎡加甲酰四氢叶酸200 mg/㎡，每天1次，连续5天，每4～5周重复1次），所产生的客观有效率相似，分别为14.3%～19.3%和15.2%～18.1%，中位缓解时间分别为3.1～4.8和3.6～5.3个月，中位生存期分别为9.7～10.9和10.2～12.7个月。

药物说明书drins-伊利替康-恒瑞

【儿童用药】
儿童使用安全有效性还未确定。
【老年用药】
由于老年患者各项生理功能的减退机率很大，尤其是肝功能的减退，因此老年患者使用本品时剂量选择应慎重。
【药物相互作用】
目前尚无药物相互作用方面的报道，但伊立替康与神经肌肉阻滞剂之间的相互作用不可忽视，具有抗胆碱酯酶活性的药物可延长琥珀胆碱的神经肌肉阻滞作用，非去极化神经肌肉阻滞剂可能被拮抗。
注射用盐酸伊立替康
说明书来源: 江苏恒瑞医药股份有限公司
【药品名称】
通用名称：注射用盐酸伊立替康英文名称：IrinotecanHydrochlorideforInjection 商品名称：艾力
【成份】
本品主要成份是盐酸伊立替康。其辅料为乳酸和甘露醇。
【性状】
本品为淡黄色或黄色的疏松块状物或粉末。
【孕妇及哺乳期妇女用药】
由于本品在兔和大鼠实验中发现有胚胎毒性，胎儿毒性及致畸性。因此，妊娠期间不能使用本品。育龄妇女在接受本品治疗期间应避免怀孕，且如一旦怀孕应立即通知医生。目前尚无法证实伊立替康是否会从人类乳汁分泌，但因为可能对哺乳婴儿造成的不良反应，在使用本品治疗期间应停止母乳喂养。(见禁忌)。
【毒理研究】
遗传毒性：伊立替康和SN-38在Ames试验中均未显示出致突变性。伊立替康在CHO细胞染色体畸变试验和小鼠微核试验中显示了致断裂作用。生殖毒性：在啮齿动物多次给药试验中，可见雄性动物生殖器官萎缩。雌性大鼠静脉注射14C-伊立替康，其放射性可透过胎盘屏障，大鼠和家兔试验中，可见本品对胚胎和胎儿的毒性反应。大鼠静脉注射放射性标记的伊立替康后5分钟内，可在其乳汁中检测到放射性，给药4小时后乳汁中药物浓度可达到血药浓度的65倍；雌性大鼠在围产期静脉注射本品可引起仔鼠学习能力和雌鼠仔鼠体重的下降。目前尚无足够的和严格控制的孕妇临床研究资料，若患者在孕期使用本品或在使用本品期间怀孕，应被告之对胎儿的潜在危害。有生育可能的妇女在本品给药期间应避免怀孕；母亲在接受本品治疗期间应停止哺乳。致癌性：尚未进行伊立替康长期给药的致癌性研究，但进行了大鼠连续三周、每周一次静脉注射伊立替康2mg/kg和25mg/kg，然后恢复91周的试验 (大鼠静脉注射伊立替康25mg/kg后，其Cmax和AUC分别约相当于人每周给药125mg/m2后的7倍和1.3倍)，结果显示，子宫喇叭口处子宫内膜间质息肉和子宫内膜间质肉瘤发生率的增加有明显的剂量依赖性。

注射用雷替曲塞产品介绍

。
雷替曲塞药理

做为新一代水溶性胸苷酸合酶(TS)抑制剂，该药通过细胞膜外还原型叶酸盐载体系统将本品主动摄入细胞内，而后迅速代谢为多谷氨酸类化合物抑制胸苷酸合酶活性，并能在细胞内潴留，长时间发挥作用。它对结肠直肠癌细胞系抑制作用强于5-氟尿嘧啶.
雷替曲塞药理

雷替曲塞IC50(50%抑制浓度)长期给药为 1.3～3.9nmol/L，短期给药为80nmol/L，而 5-氟尿嘧啶与甲酰四氢叶酸合用长期给药 IC50为330～5800nmol/L，短期给药为 150000nmol/L。
注射用雷替曲塞产品介绍
南京正大天晴广州办事处

通用名：注射用雷替曲塞英文名：Raltitrexed Injection(Tumudex)
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被列入《国家级化学医药新产品开发指南》
〖功用主治〗:
用于晚期结直肠肠癌患者。
雷替曲塞药理
高选择性的胸腺嘧啶合成酶(TS)抑制剂其代谢物为多聚谷氨酸类化合物，比母药发挥更强的酶抑制作用
结论

综上所述：雷替曲赛作为近几十年来第一个新的一线细胞毒治疗药，可成为5-FU为主的化疗方案的较好替代药。他的问世可为医生和患者提供更多选择。为患者带来方便，治疗效益显著。
注意事项

注意事项：本能只做单独给药，避免与其它药物混合使用。本品用0.9%生理盐水或 5%葡萄糖水溶液稀释后应避光保存，在24 小时内使用。轻度和中毒肝损伤患者使用时无需调整本品剂量，但本品部分经粪便排泄，严重肝损伤患者使用时应注意。孕妇及哺辱期妇女禁用本品。

雷替曲塞储存条件

雷替曲塞储存条件《雷替曲塞储存条件》前段时间，我在医院里碰到件挺有意思的事儿。

有个年轻的小护士，叫晓丽，正对着新药雷替曲塞发愁呢。

她看到我，就像看到救星一样，拉着我说：“你说这雷替曲塞到底该咋储存呀？说明书好像挺复杂的呢。

”我看着她那皱着眉头的小模样，觉得又好气又好笑，就对她说：“这储存条件可不能马虎，要是没存好，这药可就没法好好发挥作用咯。

”于是，这雷替曲塞的储存条件就成了我们今天要好好聊聊的话题。

雷替曲塞呀，是个很特殊的药物。

首先呢，它得在遮光的条件下储存。

这就好比人要睡觉得拉上窗帘避光一样，雷替曲塞也怕光。

如果把它放在光照很强的地方，就像是把人整天放在大太阳下暴晒一样，药物很可能就会发生变质。

再来说温度。

雷替曲塞需要在2 - 8℃的环境中保存。

这个温度区间可是很严格的。

我给晓丽打个比方说：“你想啊，这就像有些人对温度特别挑剔，不能太冷也不能太热。

这药呢，要是放在温度太高的地方，比如说夏天暴晒后的汽车里呀，那可能就像冰淇凌一样融化了，只不过它不是化成水，而是化学结构发生变化，有效性就大打折扣。

如果温度太低呢，也可能会对它里面的有效成分造成损害，就像人在极寒的地方可能会冻伤一样。

”湿度对于雷替曲塞的储存也很关键。

它需要在比较干燥的环境下保存。

要是环境太潮湿了，那药物就像吸水性强的海绵一样，很容易受潮，进而发霉或者分解，这样的药使用起来可就很危险了。

还有啊，这药一定要放在小孩够不到的地方。

我跟晓丽笑着说：“你看那些调皮的小毛孩，什么都好奇，要是不小心拿到药吃了，那可不得了。

”我给晓丽的建议就是，医院药房一定要配备专门的冰箱，能精确控制温度在2 - 8℃，而且要有遮光措施，比如那种不透光的小盒子。

湿度控制方面可以放置一些干燥剂来辅助。

而在家庭里，如果有需要冷藏的雷替曲塞，也要确保放在合适温度的冰箱里，而且要时刻检查冰箱是不是正常工作哦。

总之呢，雷替曲塞的储存条件是个非常重要的事儿，需要我们严格按照要求来操作。

丹曲洛林说明书

丹曲洛林说明书丹曲林, 名称o 通用名称, 丹曲林o 常用名称, 丹曲洛林钠, 硝苯呋海因o 英语名称, Danlene, Dantamacrin, Dantrolen, Dantrolene Sodium Cpsules, Dantrolone Sodium Cpsuleso 商品名称, Dantrium, 药理基础o 药物类别, 麻醉科药物, 特异性药物, 麻醉辅助药, 骨骼肌松弛类药物, 肝毒性药物, 应用o 适应征, 恶性高热, 遗传痉挛性截瘫, 神经阻滞剂恶性综合征, 上运动神经原病症o 禁忌征, 绝对禁忌, 肝硬变, 毒副作用o 副作用, 胸水:嗜酸细胞增高/阳性o 诱发/加剧病症for the national strategy of developing the West, Yibin city as "Yangtze towns" and Southern towns, have become areas of Sichuan, Yunnan and Guizhou provinces central city location advantages, will take Chengdu, Chengdu, Chongqing, Chongqing's, 丹曲林作用/毒副作用, 胸腔积液, 剂量剂型用法o 剂型, 胶囊药物说明, 通用名称:丹曲林英文名:Dantrolene其他中文名:丹曲洛林、胆罗啉、旦著能其他英文名:Danlene、Dantrium[药理]本品系骨骼肌松弛药。

机制不明，可能干扰钙从肌浆网的释放。

药动学本药口服从胃肠道吸收不完全。

口服后达血峰浓度时间为 4,6h，半减期约是9h。

血中本药与血浆蛋白结合。

本药在肝脏中羟基化，其乙酰氨基代谢物有松弛骨骼肌的作用。

约 25,代谢物和小量原形物从尿中排出。

约 45,,50,出现在胆汁中。

[适应症]用于改善锥体损害造成的痉挛症状、不同原因造成的痉挛性偏瘫和截肢，如多发性硬化、脑血管病、脊髓损伤和脊髓炎后遗症等，还可用于儿童脑性瘫痪、横纹肌溶解症和肌红蛋白尿，一氧化碳造成的高热、肌强直和血清中肌酸磷酸激酶增高、麻醉药的不良反应、恶性高热、中暑高热。

伊立替康联合雷替曲塞二线化疗方案治疗晚期结直肠癌的疗效

伊立替康联合雷替曲塞二线化疗方案治疗晚期结直肠癌的疗效钱滨滨【摘要】目的分析伊立替康联合雷替曲塞二线化疗方案治疗晚期结直肠癌的临床疗效.方法选取2014年4月—2017年8月于我院采用一线FOLFOX化疗方案治疗失败且拒绝靶向药物治疗的晚期结直肠癌患者71例作为研究对象.所有患者均采用伊立替康联合雷替曲塞二线化疗方案进行治疗,对其临床疗效、用药安全性进行研究分析.结果所有患者均顺利完成化疗,治疗效果为CR、PR、SD、PD的患者分别有3例、13例、35例、20例,DCR为71.83％,ORR为22.54％;对患者随访1年,有3例患者失访,40例患者病死,28例患者存活,存活率为41.18％;化疗过程中,患者出现的主要不良反应包括肝功能异常、食欲下降、疲倦、腹泻、呕吐、恶心等消化系统反应、贫血、中性粒细胞减少等骨髓抑制反应,只偶尔见到3～4级毒副作用,主要为1～2级.结论伊立替康联合雷替曲塞二线化疗方案治疗晚期结直肠癌的临床疗效显著,患者能够耐受药物毒副作用.【期刊名称】《中国继续医学教育》【年(卷),期】2018(010)036【总页数】2页(P90-91)【关键词】伊立替康;雷替曲塞;二线化疗;晚期结直肠癌;临床疗效;药物毒副作用【作者】钱滨滨【作者单位】江苏省南通市通州区人民医院肿瘤科,江苏南通 226300【正文语种】中文【中图分类】R735结直肠癌属于全球第三大恶性肿瘤，死亡率高。

手术是临床治疗该疾病的一种重要方式，但术后有一半左右的患者会出现远处转移或者复发现象[1]。

且研究显示，30%左右的结直肠癌患者入院诊断时，其病情已处于中晚期，需通过化疗来延长生存时间[2-3]。

临床上通常会采用含氟尿嘧啶类药物的一线化疗方案对患者进行治疗，有条件的患者还会在化疗基础上联合采用靶向药物进行治疗[4]。

但随着病程进展，多数患者需要行二线化疗，伊立替康与雷替曲塞属于常见的二线化疗药物，本研究对采用一线FOLFOX化疗方案治疗失败的晚期结直肠癌患者联合应用伊立替康与雷替曲塞治疗，获得了理想的临床疗效，报道如下。

曲妥珠单抗 (Herceptin)使用说明书

曲妥珠单抗 (Herceptin)使用说明书曲妥珠单抗 (Herceptin) 使用说明书I. 药品信息曲妥珠单抗，商品名称为Herceptin，是一种单克隆抗体药物，用于治疗HER2阳性乳腺癌和HER2阳性转移性胃癌。

II. 药物治疗适应症曲妥珠单抗适用于以下症状的患者：1. HER2阳性乳腺癌：用于早期HER2阳性乳腺癌术后辅助治疗，以及未接受曲妥珠单抗的晚期或转移性HER2阳性乳腺癌患者的一线治疗和二线治疗。

2. HER2阳性转移性胃癌：与化疗药物联合使用可以作为一线治疗。

III. 药物使用方法1. 注射剂制剂：曲妥珠单抗为无色或淡黄色透明溶液，适用于静脉注射。

按患者体重和疾病状态确定治疗剂量和疗程。

2. 首次治疗：推荐首次治疗方案为：初始剂量为8mg/kg，随后每周维持剂量为6mg/kg，连续治疗至少为18个疗程。

3. 维持治疗：治疗后期，维持剂量为6mg/kg，每三周一次，直至疾病进展或不可耐受。

4. 药物注射后，应监测患者的生命体征和药物不良反应。

IV. 注意事项和禁忌症1. 使用曲妥珠单抗前，应评估患者的心脏功能，并进行相关监测。

2. 孕妇和哺乳期妇女应避免使用曲妥珠单抗。

3. 对曲妥珠单抗或其他成分过敏的患者禁止使用。

4. 使用曲妥珠单抗可能引发心脏毒性反应，如心衰、心律不齐等，需密切监测患者的心脏功能。

V. 不良反应1. 常见不良反应包括：恶心、呕吐、腹泻、疼痛、乏力、头痛、发热等。

2. 严重不良反应：包括肺炎、肺水肿、心衰、过敏反应等。

VI. 药物相互作用1. 药物相互作用可能影响曲妥珠单抗的疗效或增加不良反应的风险。

2. 与其他心脏毒性药物联用应注意风险。

VII. 储存和处理1. 曲妥珠单抗冷藏储存，并在2-8摄氏度下保存。

2. 不要冻结曲妥珠单抗。

3. 未使用的药品应按照规定的处置方法处理。

VIII. 有效期限1. 未拆封的曲妥珠单抗有效期为36个月。

2. 拆封后，避免阳光直射和潮湿环境，根据说明使用。

雷替曲塞用量计算方法

雷替曲塞用量计算方法
雷替曲塞的用量取决于病人的身体状况、年龄、体重、病情和治疗目的等因素。

在使用雷替曲塞前，应该先进行身体检查和相关药物过敏测试，然后在医生的指导下确定用量。

以下是雷替曲塞的用量计算方法参考：
1. 高血压病：一般建议起始剂量为每日50毫克，根据病情可逐渐增加到每日100-200毫克。

2. 心绞痛：一般建议起始剂量为每日50毫克，根据病情可逐渐增加到每日100-200毫克。

3. 心力衰竭：一般开始剂量为每日25毫克，根据病情一周后逐渐增加到每日50毫克，逐步调整至每日200毫克。

4. 冠心病：一般建议起始剂量为每日50毫克，根据病情可逐渐增加到每日100-200毫克。

需要注意的是，以上用量仅供参考，具体用量仍应根据医生的建议和病情确定。

在使用雷替曲塞期间，也要严格遵照医嘱，避免自行调整用量。

注射用雷替曲塞说明书

TomudexSummary of Product Characteristics Updated 04-Dec-2017 | Hospira UK Ltd1. Name of the medicinal product'Tomudex'2. Qualitative and quantitative composition'Tomudex' contains 2 mg raltitrexed in each vial.3. Pharmaceutical formPowder for solution for infusion.4. Clinical particulars4.1 Therapeutic indicationsThe palliative treatment of advanced colorectal cancer where 5-Fluorouracil and folinic acid based regimens are either not tolerated or inappropriate.4.2 Posology and method of administrationFor instructions on reconstitution and dilution of the product before administration, see section 6.6 Instructions for use/handling.Adults: - The dose of 'Tomudex' is calculated on the basis of the body surface area. The recommended dose is 3 mg/m2 given intravenously, as a single short, intravenous infusion in 50 to 250 ml of either 0.9% sodium chloride solution or 5% dextrose (glucose) solution. It is recommended that the infusion is given over a 15 minute period. Other drugs should not be mixed with 'Tomudex' in the same infusion container. In the absence of toxicity, treatment may be repeated every 3 weeks.Dose escalation above 3 mg/m2 is not recommended, since higher doses have been associated with an increased incidence of life-threatening or fatal toxicity.Prior to the initiation of treatment and before each subsequent treatment a full blood count (including a differential count and platelets), liver transaminases, serum bilirubin and serum creatinine measurements should be performed.The total white cell count should be greater than 4,000/mm3, the neutrophil count greater than 2,000/mm3 and the platelet count greater than 100,000/mm3 prior to treatment. In the event of toxicity the next scheduled dose should be withheld until signs of toxic effects regress. In particular, signs of gastrointestinal toxicity (diarrhoea or mucositis) and haematological toxicity (neutropenia or thrombocytopenia) should have completely resolved before subsequent treatment is allowed. Patients who develop signs of gastrointestinal toxicity should have their full blood counts monitored at least weekly for signs of haematological toxicity.Based on the worst grade of gastrointestinal and haematological toxicity observed on the previous treatment and provided that such toxicity has completely resolved, the following dose reductions are recommended for subsequent treatment:● 25% dose reduction: in patients with WHO grade 3 haematological toxicity (neutropenia or thrombocytopenia) or WHOgrade 2 gastrointestinal toxicity (diarrhoea or mucositis).● 50% dose reduction: in patients with WHO grade 4 haematological toxicity (neutropenia or thrombocytopenia) or WHOgrade 3 gastrointestinal toxicity (diarrhoea or mucositis).Once a dose reduction has been made, all subsequent doses should be given at the reduced dose.Treatment should be discontinued in the event of any WHO grade 4 gastrointestinal toxicity (diarrhoea or mucositis) or in the event of a WHO grade 3 gastrointestinal toxicity associated with WHO grade 4 haematological toxicity. Patients with such toxicity should be managed promptly with standard supportive care measures including i.v. hydration and bone marrow support. In addition, preclinical data suggest that consideration should be given to the administration ofleucovorin (folinic acid). From clinical experience with other antifolates, leucovorin may be given at a dose of 25 mg/m2i.v. every 6 hours until the resolution of symptoms. Further use of 'Tomudex' in such patients is not recommended.It is essential that the dose reduction scheme should be adhered to since the potential for life threatening and fatal toxicity increases if the dose is not reduced or treatment not stopped as appropriate.Elderly: - Dosage and administration as for adults. However, 'Tomudex' should be used with caution in elderly patients (see section 4.4 Special warnings and precautions for use).Children: - 'Tomudex' is not recommended for use in children as safety and efficacy have not been established in this group of patients.Renal impairment:- For patients with abnormal serum creatinine, before the first or any subsequent treatment, a creatinine clearance should be performed or calculated.For patients with a normal serum creatinine when the serum creatinine may not correlate well with the creatinine clearance due to factors such as age or weight loss, the same procedure should be followed. If creatinine clearance is≤65 ml/min, the following dose modifications are recommended:Dose modification in the presence of renal impairmentCreatinine Clearance Dose as % of 3.0 mg/m2Dosing Interval> 65 ml/min Full dose3-weekly55 to 65 ml/min75%4-weekly25 to 54 ml/min50%4-weekly< 25 ml/min No therapy Not applicableSee Contraindications for use in patients with severe renal impairmentHepatic Impairment:- No dosage adjustment is recommended for patients with mild to moderate hepatic impairment. However, given that a proportion of the drug is excreted via the faecal route, (see section 5.2 Pharmacokinetic Properties) and that these patients usually form a poor prognosis group, patients with mild to moderate hepatic impairment need to be treated with caution (see section 4.4 Special warnings and special precautions for use).'Tomudex' has not been studied in patients with severe hepatic impairment, clinical jaundice or decompensated liver disease and its use in such patients is not recommended.4.3 Contraindications'Tomudex' should not be used in pregnant women, in women who may become pregnant during treatment or women who are breast feeding. Pregnancy should be excluded before treatment with 'Tomudex' is commenced. (see section 4.6 Pregnancy and lactation).'Tomudex' is contraindicated in patients with severe renal impairment (creatinine clearance < 25ml/min).Administration of leucovorin (folinic acid), folic acid or vitamin preparations containing these agents with 'Tomudex' is contraindicated (see section 4.5 Interaction with other medicinal products and other forms of interaction).4.4 Special warnings and precautions for use'Tomudex' must only given by or under the supervision of a physician who is experienced in cancer chemotherapy, and in the management of chemotherapy-related toxicity. Patients undergoing therapy should be subject to appropriate supervision so that signs of possible toxic effects or adverse reactions (particularly diarrhoea) may be detected and treated promptly (see section 4.2 Posology and method of administration).In common with other cytotoxic agents of this type, caution is necessary in patients with depressed bone marrow function, poor general condition, or prior radiotherapy.Patients whose disease progressed on previous treatment for advanced disease with 5-Fluorouracil based regimens may also be resistant to the effects of 'Tomudex'.Elderly patients are more vulnerable to the toxic effects of 'Tomudex'. Since renal function tends to decline with age and the plasma clearance of raltitrexed is reduced with renal function impairment, there is a potential for accumulation of raltitrexed in elderly patients. Extreme care should be taken to ensure adequate monitoring of adverse reactions especially signs of gastrointestinal toxicity (diarrhoea or mucositis) and myelosuppression (neutropenia, thrombocytopenia, infection) and dose should be reduced and /or delayed as appropriate. A proportion of the 'Tomudex' is excreted via the faecal route, (see section 5.2 Pharmacokinetic properties) therefore, patients with mild to moderate hepatic impairment should be treated with caution.Treatment with 'Tomudex' in patients with severe hepatic impairment is not recommended.It is recommended that pregnancy should be avoided during treatment and for at least 6 months after cessation of treatment if either partner is receiving 'Tomudex' (see also section 4.6 Pregnancy and lactation).There is no clinical experience with extravasation. However, perivascular tolerance studies in animals did not reveal any significant irritant reaction.'Tomudex' is a cytotoxic agent and should be handled according to normal procedures adopted for such agents (see section 6.6 Instructions for use/handling).4.5 Interaction with other medicinal products and other forms of interactionNo specific clinical drug - drug interaction studies have been conducted in man.Leucovorin (folinic acid), folic acid or vitamin preparations containing these agents must not be given immediately prior to or during administration of 'Tomudex', since they may interfere with its action.Clinical trials evaluating the use of Tomudex in combination with other antitumour therapies are currently ongoing.'Tomudex' is 93% protein bound and while it has the potential to interact with similarly highly protein bound drugs, no displacement interaction with warfarin has been observed in vitro. Data suggest that active tubular secretion may contribute to the renal excretion of raltitrexed, indicating a potential interaction with other actively secreted drugs such as non-steroidal antiinflammatory drugs (NSAIDS). However, a review of the clinical trial safety database did not reveal evidence of clinically significant interaction in patients treated with 'Tomudex' who also received concomitant NSAIDS, warfarin and other commonly prescribed drugs.4.6 Pregnancy and lactationPregnancyPregnancy should be avoided if either partner is receiving 'Tomudex'. It is also recommended that conception should be avoided for at least 6 months after cessation of treatment.'Tomudex' should not be used during pregnancy or in women who may become pregnant during treatment (see section 5.3 Preclinical safety data). Pregnancy should be excluded before treatment with 'Tomudex' is started.Breastfeeding'Tomudex' should not be given to women who are breast feeding.FertilityFertility studies in the rat indicate that 'Tomudex' can cause impairment of male fertility. Fertility returned to normal three months after dosing ceased. 'Tomudex' caused embryolethality and foetal abnormalities in pregnant rats.4.7 Effects on ability to drive and use machines'Tomudex' may cause malaise or asthenia following infusion and the ability to drive/use machinery could be impaired whilst such symptoms continue.4.8 Undesirable effectsAs with other cytotoxic drugs, 'Tomudex' may be associated with certain adverse drug reactions. These mainly include reversible effects on the haemopoietic system, liver enzymes and gastrointestinal tract. Table 1 presents the possible adverse drug reactions occurring with 'Tomudex' treatment.In this section undesirable effects are defined as follows: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to ≤1/100); rare (≥1/10,000 to ≤1/1,000); very rare (≤1/10,000), not known (cannot be estimated from the available data).Table 1: Adverse drug reactions in patients treated with Tomudex for advanced colorectal carcinoma divided by System Organ Class and frequencySystem Organ Class Frequency Adverse drug reactionInfections & infestations Common CellulitisSepsisFlu-like syndrome Blood and lymphatic disorders Very Common Leucopenia (neutropenia in particular) a, bAnaemia aCommon Thrombocytopenia a, b Metabolism and Nutrition Disorders Very Common AnorexiaCommon DehydrationNervous system disorders Common HeadacheHypertonia (usually muscular cramps)Taste perversion Eye disorders Common ConjunctivitisGastrointestinal disorders Very Common Nausea cDiarrhoea d,eVomiting c,eConstipationAbdominal PainCommon StomatitisDyspepsiaMouth ulcerationFrequency unknown Gastrointestinal Bleeding f,gHepato-biliary disorder Common HyperbilirubinemiaSkin & subcutaneous tissue disorders Very Common RashCommon AlopeciaPruritusSweatingUncommon DesquamationCommon ArthralgiaMusculoskeletal, Connective tissue & bonedisordersVery Common Asthenia hGeneral disorders and administration siteconditionsFever hMucositisCommon Peripheral oedemaPainMalaiseInvestigations Very Common AST increased iALT increased iCommon Weight lossAlkaline phosphatase increaseda Leucopenia (neutropenia in particular), anaemia and thrombocytopenia, alone or in combination, are usually mild to moderate and occur in the first or second week after treatment and recover by the third week.b Severe (WHO grade 3 and 4) leucopenia (neutropenia in particular) and thrombocytopenia of WHO grade 4 can occur and may be life-threatening or fatal especially if associated with signs of gastrointestinal toxicity.c Nausea and Vomiting are usually mild (WHO grade 1 and 2), occur usually in the first week following the administration of 'Tomudex', and are responsive to antiemetics.d Diarrhoea is usually mild or moderate (WHO grade 1 and 2) and can occur at any time following the administration of 'Tomudex'. However, severe diarrhoea (WHO grade 3 and 4) can occur, and may be associated with concurrent haematological suppression especially leucopenia (neutropenia in particular). Subsequent treatment may need to be discontinued or dose reduced according to the grade of toxicity (see Section 4.2 Posology and method of administration).e Diarrhoea and vomiting may be severe and if untreated may proceed to dehydration, hypovolaemia and renalimpairmentf from spontaneous reportingg Gastrointestinal bleeding may be associated with mucositis and/or thrombocytopenia.h Asthenia and fever were usually mild to moderate following the first week of administration of 'Tomudex' and reversible.Severe asthenia can occur and may be associated with malaise and a flu-like syndrome.i Increases in AST and ALT have usually been asymptomatic and self-limiting when not associated with progression ofthe underlying malignancy.Reporting of suspected adverse reactionsReporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions viaYellow Card SchemeWebsite: /yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store4.9 OverdoseThere is no clinically proven antidote available. In the case of inadvertent or accidental administration of an overdose, preclinical data suggest that consideration should be given to the administration of leucovorin. From clinical experience with other antifolates leucovorin may be given at a dose of 25mg/m2 i.v. every 6 hours. As the time interval between 'Tomudex' administration and leucovorin rescue increases, its effectiveness in counteracting toxicity may diminish.The expected manifestations of overdose are likely to be an exaggerated form of the adverse drug reactions anticipated with the administration of the drug. Patients should, therefore, be carefully monitored for signs of gastrointestinal and haematological toxicity. Symptomatic treatment and standard supportive care measures for the management of this toxicity should be applied.5. Pharmacological properties5.1 Pharmacodynamic propertiesRaltitrexed is a folate analogue belonging to the family of anti-metabolites and has potent inhibitory activity against the enzyme thymidylate synthase (TS). Compared to other antimetabolites such as 5-Fluorouracil or methotrexate, raltitrexed acts as a direct and specific TS inhibitor. TS is a key enzyme in the de novo synthesis of thymidine triphosphate (TTP), a nucleotide required exclusively for deoxyribonucleic acid (DNA) synthesis. Inhibition of TS leads to DNA fragmentation and cell death. Raltitrexed is transported into cells via a reduced folate carrier (RFC) and is then extensively polyglutamated by the enzyme folyl polyglutamate synthetase (FPGS) to polyglutamate forms that are retained in cells and are even more potent inhibitors of TS. Raltitrexed polyglutamation enhances TS inhibitory potency and increases the duration of TS inhibition in cells which may improve antitumour activity. Polyglutamation could also contribute to increased toxicity due to drug retention in normal tissues.In clinical trials, 'Tomudex' at the dose of 3mg/m2 i.v. every 3 weeks has demonstrated clinical antitumour activity with an acceptable toxicity profile in patients with advanced colorectal cancer.Four large clinical trials have been conducted with 'Tomudex' in advanced colorectal cancer. Of the three comparative trials, two showed no statistical difference between 'Tomudex' and the combination of 5-fluorouracil plus folinic acid for survival while one trial showed a statistically significant difference in favour of the combination of 5-fluorouracil plus folinic acid. 'Tomudex' as a single agent was as effective as the combination of 5-fluorouracil and folinic acid in terms of objective response rate in all trials.5.2 Pharmacokinetic propertiesFollowing intravenous administration at 3.0 mg/m2, the concentration-time profile in patients was triphasic: Peak concentrations, found at the end of the infusion, were followed by a rapid initial decline in concentration. This was followed by a slow elimination phase. The key pharmacokinetic parameters are presented below:Summary of mean pharmacokinetic parameters in patients administered 3.0 mg/m2 Raltitrexed byintravenous infusionC m ax (ng/ml)AUC o-∞(ng.h/ml)CL(ml/min)CL r(ml/min)V ss(l)t1/2β(h)t1/2γ(h)656185651.625.1548 1.79198 Key:C m ax: Peak plasma concentration.AUC: Area under plasma concentration-time curve.CL: Clearance.V ss: Volume of distribution at steady state. t ½γ: Terminal half life.CL r: Renal clearancet½β: Half life of the second (β) phase.The maximum concentrations of raltitrexed increased linearly with dose over the clinical dose range tested.During repeated administration at three week intervals, there was no clinically significant plasma accumulation of raltitrexed in patients with normal renal function.Apart from the expected intracellular polyglutamation, raltitrexed was not metabolised and was excreted unchanged, mainly in the urine, 40 - 50%. Raltitrexed was also excreted in the faeces with approximately 15% of the radioactive dose being eliminated over a 10 day period. In the [14C] - raltitrexed trial approximately half of the radiolabel was not recovered during the study period. This suggests that a proportion of the raltitrexed dose is retained within tissues, perhaps as raltitrexed polyglutamates, beyond the end of the measurement period (29 days). Trace levels of radiolabel were detected in red blood cells on Day 29.Raltitrexed pharmacokinetics are independent of age and gender. Pharmacokinetics have not been evaluated in children.Mild to moderate hepatic impairment led to a small reduction in plasma clearance of less than 25%.Mild to moderate renal impairment (creatinine clearance of 25 to 65 ml/min) led to a significant reduction (approximately 50%) in raltitrexed plasma clearance.5.3 Preclinical safety dataPerivascular tolerance in studies in animals did not reveal any significant irritant reaction.Acute toxicityThe approximate LD50 values for the mouse and rat are 875-1249 mg/kg and >500 mg/kg respectively. In the mouse, levels of 750 mg/kg and above caused death by general intoxication.Chronic toxicityIn one month continuous and six month intermittent dosing studies in the rat, toxicity was related entirely to the cytotoxic nature of the drug. Principal target organs were the gastrointestinal tract, bone marrow and the testes. In similar studies in the dog, cumulative dose levels similar to that used clinically, elicited only pharmacologically-related changes to proliferating tissue. Target organs in the dog were therefore similar to the rat.Mutagenicity'Tomudex' was not mutagenic in the Ames test or in supplementary tests using E. coli or Chinese hamster ovary cells.'Tomudex' caused increased levels of chromosome damage in an in vitro assay of human lymphocytes. This effect was ameliorated by the addition of thymidine, thus confirming it to be due to the anti-metabolic nature of the drug. An in vivo micronucleus study in the rat indicated that at cytotoxic dose levels, 'Tomudex' is capable of causing chromosome damage in the bone marrow.Reproductive toxicologyFertility studies in the rat indicate that 'Tomudex' can cause impairment of male fertility. Fertility returned to normal three months after dosing ceased. 'Tomudex' caused embryolethality and foetal abnormalities in pregnant rats.CarcinogenicityThe carcinogenic potential of 'Tomudex' has not been evaluated.6. Pharmaceutical particulars6.1 List of excipientsMannitol Ph Eur, USPDibasic sodium phosphate (heptahydrate USP or dodecahydrate Ph Eur)Sodium hydroxide Ph Eur, USNF6.2 IncompatibilitiesThere is no information on incompatibilities at present and therefore 'Tomudex' should not be mixed with any other drug.6.3 Shelf lifeThe expiry life of 'Tomudex' is 36 months when stored below 25°C, protected from light.Once reconstituted, 'Tomudex' is chemically stable for 24 hours at 25°C exposed to ambient light. For storagerecommendation, see Instructions for Use/Handling.6.4 Special precautions for storageAddressHorizon, Honey Lane, Hurley, Maidenhead, SL6 6RJ, UK WWWMedical Information Direct LineUnopened vial - Do not store above 25°C. Keep container in the outer carton.Reconstituted vial - Refrigerate at 2-8°C.6.5 Nature and contents of container'Tomudex' is packed in 5ml clear neutral type I glass vials, with a bromobutyl rubber closure and an aluminium crimp seal with a plastic flip-off cover.The vials are packed in individual cartons to protect the product from light.6.6 Special precautions for disposal and other handlingEach vial, containing 2mg of raltitrexed, should be reconstituted with 4ml of sterile water for injections to produce a 0.5 mg/ml solution.The appropriate dose of solution is diluted in 50 - 250 ml of either 0.9% sodium chloride or 5% glucose (dextrose) injection and administered by a short intravenous infusion over a period of 15 minutes.There is no preservative or bacteriostatic agent present in 'Tomudex' or the materials specified for reconstitution or dilution. 'Tomudex' must therefore be reconstituted and diluted under aseptic conditions and it is recommended that solutions of 'Tomudex' should be used as soon as possible. Reconstituted 'Tomudex' solution may be stored refrigerated(2 - 8°C) for up to 24 hours.In accordance with established guidelines, when diluted in 0.9% sodium chloride or 5% glucose (dextrose) solution, it is recommended that administration of the admixed solution should commence as soon as possible after admixing. The admixed solution must be completely used or discarded within 24 hours of reconstitution of 'Tomudex' intravenous injection.Reconstituted and diluted solutions do not need to be protected from light.Do not store partially used vials or admixed solutions for future patient use.Any unused injection or reconstituted solution should be discarded in a suitable manner for cytotoxics.'Tomudex' should be reconstituted for injection by trained personnel in a designated area for the reconstitution of cytotoxic agents. Cytotoxic preparations such as 'Tomudex' should not be handled by pregnant women.Reconstitution should normally be carried out in a partial containment facility with extraction e.g. a laminar air flow cabinet, and work surfaces should be covered with disposable plastic-backed absorbent paper.Appropriate protective clothing, including normal surgical disposable gloves and goggles, should be worn. In case of contact with skin, immediately wash thoroughly with water. For splashes in the eyes irrigate with clean water, holding the eyelids apart, for at least 10 minutes. Seek medical attention.Any spillages should be cleared up using standard procedures.Waste material should be disposed of by incineration in a manner consistent with the handling of cytotoxic agents.7. Marketing authorisation holderHospira UK LimitedHorizon, Honey Lane, HurleyMaidenhead,SL6 6RJUnited Kingdom8. Marketing authorisation number(s)PL 04515/02259. Date of first authorisation/renewal of the authorisation25th June 200010. Date of revision of the text11/2017Ref: gxTM 3_1Company Contact DetailsHospira UK Ltd+44 (0)1304 616161 Fax+44 (0)800 098 8653Medical Information Fax+44 (0)1304 656221。

雷替曲塞治疗晚期恶性肿瘤

雷替曲塞治疗晚期恶性肿瘤-安全有效(基础知识与进展）发表者:刘连科（访问人次:406）由于既往国外研究认为雷替曲塞较5-FU存在较高死亡患者,而且雷替曲塞的疗效并不优于5—FU，在国外未得到足够的重视.国内2010年由南京正大天晴上市（赛维健），研究基于一项设计严格的多中心、随机盲法、阳性药物平行对照，雷替曲塞的适应症为：在患者无法接受联合化疗时，本品可单药用于治疗不适合5—Fu/亚叶酸钙的晚期结直肠癌患者。

目前已在国内广泛应用，逐渐得到大家的认可。

事实上，雷替曲塞不但可单药化疗，而且更多的学者采用雷替曲塞联合其他药物。

越来越多的文献支持，对于中国肿瘤患者，雷替曲塞可能较西方人更安全.1. 雷替曲塞为氟尿嘧啶类药物发生心脏毒性者的最佳替代药物临床上，氟尿嘧啶类药物(5-FU、卡培他滨、替吉奥胶囊等）可引起严重的心脏毒性,既往只能放弃氟尿嘧啶类药物。

2012年欧洲肿瘤内科学会(ESMO）发布ARCTIC试验，对于接受氟尿嘧啶类药物出现心脏毒性的患者，可用雷替曲塞（一种胸甘酸合成酶（TS）的特异性抑制剂）来替代，并且是一个安全的替代药品.文献报道5—FU/卡培他滨引起的心脏毒性发生率为0。

55％～ 19％（平均值: 5。

0％，中位数: 3.85%）,而与雷替曲塞相关的心脏毒性未见报道。

但最近有学者报道有心脏病史或者发生5—FU/卡培他滨引起心脏毒性的患者，再用雷替曲塞，可有4.5%的患者再发生心脏毒性。

2. 不良反应较多，但易处理国内大型III临床研究（临床肿瘤学杂志2012年）：“雷替曲塞或氟尿嘧啶/亚叶酸钙联合奥沙利铂治疗局部晚期或复发转移性结直肠癌的随机对照多中心Ⅲ期临床试验"，试验组1~2 级中性粒细胞减少( 48.2% vs.29.4%, P= 0.005) 和转氨酶升高（ 49.1% vs。

35.3％, P = 0.041) 的发生率明显高于对照组。

对照组呕吐的发生率明显高于试验组( 61.8% vs. 40.2%, P = 0。

雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的疗效

雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的疗效发布时间：2022-06-16T00:40:48.824Z 来源：《中国医学人文》2021年34期作者：任云会[导读] 目的：分析雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的疗效及其改善效果任云会大庆龙南医院黑龙江大庆 163453【摘要】目的：分析雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的疗效及其改善效果。

方法：此次研究初始时间为2020年1月，截止时间为2021年6月，抽取此段时间内到院接受治疗的结直肠癌肝转移患者共30例，按照随机抓阄法均分为两组，其中15例接受雷替曲塞联合奥沙利铂治疗，为观察组，余下15例接受单一奥沙利铂治疗，为对照组。

结果：两组患者的临床治疗总有效率分别为观察组100.00%和对照组73.33%，具有统计学意义（P＜0.05）。

结论：雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的临床应用当中，患者的临床疗效得到了显著的提升，值得推广应用。

【关键词】：雷替曲塞；奥沙利铂；结直肠癌结直肠癌作为临床中常见的消化道恶性肿瘤疾病之一，患者在早期阶段的时候并没有明显的临床变化或体征，部分患者是在体检过程中发现，大多数在确诊的时候已经发展为晚期阶段，多数甚至还伴随有远处脏器转移等现象，对患者的整体健康状况造成严重影响[1]。

鉴于此，本文就雷替曲塞联合奥沙利铂治疗结直肠癌肝转移的疗效进行研究，详细报道如下。

1.资料与方法1.1一般资料此次研究初始时间为2020年1月，截止时间为2021年6月，抽取此段时间内到院接受治疗的结直肠癌肝转移患者共30例，按照随机抓阄法均分为两组，其中15例接受雷替曲塞联合奥沙利铂治疗，为观察组，余下15例接受单一奥沙利铂治疗，为对照组。

观察组患者男女10:5，年龄49到79岁，均值（60.13±4.62）岁；对照组患者男女11:4，年龄50到79岁，均值（59.87±4.53）岁。

从一般资料对比分析可观察到，本次研究的两组患者的自身一般病例信息具备较高的相似性（P＞0.05），可进行对比。

雷替曲塞联合内生场热疗治疗晚期结直肠癌的疗效评估

雷替曲塞联合内生场热疗治疗晚期结直肠癌的疗效评估发表时间：2013-09-10T09:53:07.107Z 来源：《医药前沿》2013年第23期供稿作者：朱麟玉朱纪华武建毅姚晓祥黄晓东[导读] 高热还可促使肿瘤细胞分泌的血管内皮细胞生长因子(VEGF)浓度明显下降，诱导肿瘤细胞凋亡，直接杀伤肿瘤细胞朱麟玉朱纪华武建毅姚晓祥黄晓东（上海市普陀区人民医院肿瘤科 200060）【摘要】目的探讨雷替曲塞（Raltitrexed，商品名赛维健）联合内生场热疗治疗晚期结直肠癌的临床疗效。

方法 23例晚期结直肠癌患者，静脉滴注雷替曲塞3mg／m2，第1天给药，之后行腹部内生场热疗（每周二次，每次一小时），21天为一周期。

随访观察客观疗效、中位无疾病进展生存期（MPFS）、不良反应等。

结果 23例患者的客观缓解率为30%，中位无疾病进展生存期（MPFS）7.4个月，一年生存率61%。

结论雷替曲塞联合内生场热疗治疗晚期结直肠癌可获得较好的临床疗效，患者耐受良好，值得进一步研究。

【关键词】结直肠肿瘤内生场热疗化疗雷替曲塞【中图分类号】R730.5 【文献标识码】A 【文章编号】2095-1752（2013）24-0027-02结直肠癌是常见的恶性肿瘤之一。

中国结直肠癌发病率为20.6／10万，并且逐年上升，现已居恶性肿瘤的第3位。

目前的治疗手段是以手术为主，但由于早期难以发现，往往就诊时已是中晚期。

雷替曲塞是喹啉类叶酸盐类似物，可特异性直接抑制胸苷酸合成酶（TS）而产生细胞毒作用，与5-氟尿嘧啶（5-Fu）相比具有更强的抗肿瘤活性和更好的安全性[1]。

该药通过细胞膜外还原型叶酸盐载体系统将本品主动摄取至细胞内，而后迅速代谢为多谷氨酸类化合物抑制胸苷酸合酶活性，并能在细胞内潴留，长时间发挥作用。

本品对结肠直肠细胞系的抑制作用强于5- Fu。

目前已有Ⅲ期临床试验报道[2-3]：雷替曲塞对比5-Fu+CF方案治疗晚期结直肠癌，疗效相当，毒性可以预测并处理，用药方便。

雷珠单抗注射液Ranibizumab-详细说明书与重点

雷珠单抗注射液Ranibizumab 英文名称: Ranibizumab Injections商品名称: 诺适得Lucentis【成分】活性成份：雷珠单抗，化学名称：G1,抗-（人血管内皮生长因子）Fab片段（人-鼠单克隆rhuFabV2γ-1链），二硫键结合人-鼠单克隆rhuFabV2κ-链）分子量：48KD【性状】透明至微乳白色液体。

【处方组成】每1ml 含10mg 雷珠单抗，预装在注射器中。

本品所含辅料为：α,α-海藻糖二水合物；组氨酸；盐酸组氨酸一水合物；聚山梨醇酯20。

【适应症】用于治疗湿性（新生血管性）年龄相关性黄斑变性（AMD）。

【规格】10mg/ml，每瓶装量0.165ml。

【用法用量】本品应在有资质的医院和眼科医生中使用。

医院应具备该疾病诊断和治疗所需的相关仪器设备和条件，眼科医生应具备确诊湿性年龄相关性黄斑变性的能力和丰富的玻璃体内注射经验。

本品经玻璃体内注射给药。

推荐剂量为每次0.5mg（相当于0.05ml的注射量），每月一次给药。

如果不能长期每月注射给药，也可在初始3个月连续每月注射1次给药之后，按每3个月注射给药1次。

与持续每月注射相比，在初始3个月，连续每月注射之后的9个月治疗中，如果按每3个月给药1次，则视力改善将平均减少约5个字母（ETDRS视力或Snellen视力表1行）。

治疗期间应每月监测患者视力变化情况，如果出现显著的视力下降，需进一步接受本品注射治疗。

两次注射之间的间隔时间不得小于一个月。

给药方法：在玻璃体内注射给药前，应对患者的既往病史进行全面的评估，以评估其发生高敏反应的可能性。

（见【警告】与【注意事项】）本品必须在无菌条件下进行玻璃体内注射，其中包括采用外科手术的手部消毒、无菌口罩、无菌手套、无菌手术单和无菌开睑器（或类似器具）。

注射前必须给予患者适当的麻醉剂和眼局部用光谱抗生素。

注射前消毒眼周皮肤、眼睑和眼球表面。

应指导患者在每次注射前后3天自行滴注抗生素滴眼液，每天4次。

塞替派注射液

塞替派注射液
【药品名称】【通用名称】塞替派注射液
【汉语拼音】Sɑitipɑi Zhusheye
【成份】【化学名称】本品主要成份为塞替派，其化学名称为：1,
1′,1″-硫次膦基三氮丙啶。

【化学结构式】
【分子式】C
6H
12
N
3
PS
【分子量】189.22
【注射剂辅料】聚乙二醇400。

【性状】本品为无色或几乎无色的黏稠澄明液体。

【适应症】主要用于乳腺癌、卵巢癌、癌性体腔积液的腔内注射以及膀胱癌的局部灌注等，也可用于胃肠道肿瘤等。

【规格】1ml:10mg
【用法用量】静脉或肌内注射（单一用药）：一次10mg（0.2mg/kg），一日1次，连续5天后改为每周3次，一疗程总量300mg，如血象良好，在第一
疗程结束后1.5～2月后可重复疗程。

胸腹腔或心包腔内注射：一次10～30mg，每周1～2次。

膀胱腔内灌注：每次排空尿液后将导尿管插入膀胱内向腔内注入50～
100mg（溶于50～100ml氯化钠注射液中），每周1～2次，10次为一。

药物说明书drins-曲妥珠单抗-罗氏

【性状】
每瓶含浓缩曲妥珠单抗粉末440mg，为白色至淡黄色冻干粉剂。配制成溶液后为无色或淡黄色澄清或微乳光色溶液，供静脉输注用。溶解后曲妥珠单抗的浓度为21mg/ml。
【适应症】
转移性乳腺癌：本品适用于HER2过度表达的转移性乳腺癌：作为单一药物治疗已接受过1个或多个化疗方案的转移性乳腺癌；与紫杉醇或者多西他赛联合，用于未接受化疗的转移性乳腺癌患者。乳腺癌辅助治疗：本品单药适用于接受了手术、含蒽环类抗生素辅助化疗和放疗（如果适用）后的HER2过度表达乳腺癌的辅助治疗。转移性胃癌：本品联合卡培他滨或5-氟尿嘧啶和顺铂适用于既往未接受过针对转移性疾病治疗的HER2过度表达的转移性胃腺癌或胃食管交界腺癌患者。曲妥珠单抗只能用于HER2过度表达的转移性胃癌患者，HER2过度表达的定义为使用已验证的检测方法得到的IHC3+或IHC2+/FISH+结果。
注射用曲妥珠单抗
说明书来源: 上海罗氏制药有限公司
【药品名称】
通用名称：注射用曲妥珠单抗英文名称：Herceptin(TrastuzumabInjection) 商品名称：赫赛汀
【成份】
活性成分：的人源化单克隆抗体，是由悬养于无菌培养基中的哺乳动物细胞 (中国仓鼠卵巢细胞CHO) 生产的，纯化过程包括特定的病毒灭活和去除步骤，采用的是用亲合色谱法和离子交换法。稀释液为含1.1%苯甲醇的20ml灭菌注射用水 (以下称稀释液) 。赋形剂：L-盐酸组氨酸，L-组氨酸，α,α-双羧海藻糖，聚山梨醇酯20。
【规格】
440mg(20ml)/瓶。
【用法用量】
【不良反应】
以下不良反应会在说明书的其他部分进行更详细的讨论：心肌病[见注意事项] 输注反应[见注意事项] 化疗引起的中性粒细胞减

静脉药物外渗的认识与处理

此类的药物外渗常引起皮肤炎症、脱皮，顺铂、柔红霉素脂质体、多西他赛、多柔比星
但一般不引起组织坏死。
脂质体、米托蒽醌、奥沙利铂、拓扑替康。
刺激性物质可能导致疼痛、静脉炎，可伴卡铂、依托泊苷、伊立替康、替尼泊苷。发或不伴发炎症反应，通常不发展为组织损伤。
外渗后引起的反应较温和，通常为局部皮阿扎胞苷、硼替佐米、氟尿嘧啶、甲氨蝶呤、
类别发泡剂
剥离素刺激性物
质炎性物质中性物质
药物特点
主要药物
具有腐蚀性，外渗可致组织发生不同程度
的损伤，包括疼痛、水肿、红斑、起泡，甚至坏死。非DNA结合型物质发生外渗后可快速代谢、失活并自我修复； DNA 结合型物质，外渗后易残留在组织中导致长期损伤。
非DNA结合型物质（长春碱、长春瑞滨、长春新碱）、 DNA结合型物质（表柔比星、丝裂霉素、阿霉素、柔红霉素）、安吖啶、白消安、卡莫司汀、氮芥、达卡巴嗪、放线菌素、紫杉醇、链脲霉素
美国INS药液渗出的分级
分级 0级 1级
2级
3级
4级
表现
无症状
皮肤发白，水肿范围的最大处直径＜1英寸（2.5cm），伴有或不伴有疼痛。
皮肤发白，水肿范围的最大处直径1-6英寸（2.5-15cm），皮肤发冷，伴有或不伴有疼痛。
皮肤发白，半透明状，水肿范围的最大处直径＞6英寸（15cm），皮肤发冷，轻到中度疼痛，可能有麻木感。
注射方法：推荐5点式注射法，即在渗漏区域边缘平均分5个注射点进行注射，每个注射部位30u（0.2ml），一般15-30min 后肿胀会明显减轻，也可增加剂量或加入利多卡因或普鲁卡因以减轻注射部位的疼痛问题。
② 酚妥拉明：通过舒张血管平滑肌扩张血管，主要用于缩血管药物渗漏引起的组织损害，增加血流供应及促进回流，减轻缺血、缺氧带来的组织损害。5-10mg 酚妥拉明稀释于10ml 氯化钠溶液局部注射，酚妥拉明的应用越早越好，最迟不超过渗漏事件发生后12h 。

注射用雷替曲塞说明书

注射用雷替曲塞说明书说明书来源：南京正大天晴制药有限公司【药品名称】通用名称：注射用雷替曲塞英文名称：RaltitrexedforInjection 商品名称：赛维健【成份】本品活性成份为雷替曲塞辅料：甘露醇、磷酸氢二钠及氢氧化钠。

【性状】本品为白色或类白色疏松块状物或粉末。

【适应症】在患者无法接受联合化疗时，本品可单药用于治疗不适合5-Fu/亚叶酸钙的晚期结直肠癌患者。

【规格】2mg。

【用法用量】成人：推荐剂量为3mg/m2，用50-250ml 0.9%氯化钠注射液或5%葡萄糖注射液溶解稀释后静脉输注，给药时间15分钟，如果未出现毒性，可考虑按上述治疗每3周重复给药1次。

本药应避免与其它药物混合输注。

增加剂量会致使危及生命或致死性毒性反应的发生率升高，所以不推荐剂量大于3mg/m2。

每次用药治疗前需检查全血细胞计数（包括白细胞分类计数和血小板计数）和肝、肾功能。

治疗前应该白细胞计数＞4.0×108/L、中性粒细胞计数＞2.0×109/L和血小板计数＞1.0×1011/L。

出现毒性反应时，下一周期用药需延迟至不良反应消退；尤其是胃肠道毒性（腹泻或粘膜炎）及血液学毒性（中性粒细胞减少或血小板减少）需完全恢复才可进行后续治疗，出现胃肠道毒性者应至少每周检查一次全血细胞计数以监测血液学毒性。

根据前一治疗周期观察到的最严重的胃肠道及血液学毒性等级，如果此类毒性已完全缓解，推荐按前一周期最严重的胃肠道、血液学毒性（以下毒性均按WHO标准分级）进行剂量调整：剂量减少25%：血液学毒性（中性粒细胞减少或者血小板减少）3级或胃肠道毒性2级（腹泻或粘膜炎）；剂量减少50%：血液学毒性（中性粒细胞减少或者血小板减少）4级或胃肠道毒性3级（腹泻或粘膜炎）。

一旦减量，后续治疗的剂量也须按减量后给药。

出现4级胃肠道毒性（腹泻或粘膜炎），或3级胃肠道毒性伴4级血液学毒性时必须中止治疗；同时迅速给予标准支持治疗，包括静脉补水和造血功能支持。