Bendamustine D4__DataSheet_MedChemExpress
苯达莫司汀说明书
通用名：盐酸苯达莫司汀（发音为 ben-da-MUS-teen）商品名：Treanda®；Bendeka®（生产商：Teva）；Belrapzo®（生产商：Eagle Pharmaceuticals）注：2016 年，Teva 用 Bendeka® 替代了 Treanda®，理由如下：•Bendeka® 的输液时间比 Treanda® 短（10 分钟对 30-60 分钟）。
•Bendeka® 与部分输液设备中包含的某些化学物质相容，而 Treanda® 则不相容。
Bendeka® 与 Treanda® 均含有盐酸苯达莫司汀，并且适应症相同。
Treanda® 仍然可通过 Teva 的子公司 Cephalon, Inc. 获得。
药物类型：苯达莫司汀是一种抗癌化疗药物，被归类为烷化剂。
苯达莫司汀的适用症是什么？苯达莫司汀经美国食品药物管理局 (FDA) 批准用于治疗慢性淋巴细胞性白血病 (CLL)，还可用于在利妥昔单抗 (Rituxan®) 或含有利妥昔单抗方案治疗过程中，或者治疗 6 个月内，病情仍然进展的惰性（生长缓慢） B 细胞非霍奇金淋巴瘤患者。
华氏巨球蛋白血症 (WM) 是一种惰性 B 细胞非霍奇金淋巴瘤。
苯达莫司汀联合单克隆抗体利妥昔单抗是美国国家综合癌症网 (NCCN®) WM 专家和第十届华氏巨球蛋白血症国际研讨会(IWWM-10) 与会成员首选的四种治疗方案之一。
NCCN® 是由美国 31 个领先癌症中心组成的联盟。
虽然苯达莫司汀/利妥昔单抗联合方案是首选，但对于不能注射利妥昔单抗的患者建议单独使用苯达莫司汀。
对于利妥昔单抗不耐受的患者，苯达莫司汀联合利妥昔单抗和单独使用苯达莫司汀是 WM 初治（也称为一线或初期治疗）以及经治的首选方案。
Bentham Science出版社电子期刊列表
Bentham Science出版社电子期刊列表1. Anti Cancer Agents in Medicinal Chemistry（ISSN：1871-5206）《医药化学中抗癌药剂》涵盖与药物化学及开发抗癌药物合理药物设计有关的最新和最重要的进展。
每期包括一系列由本领域权威撰写的深入全面的前沿性综述，涉及与抗癌药物的药物化学有关的各个当今课题。
2. Anti Infective Agents in Medicinal Chemistry（ISSN：1568-0126）涵盖与药物化学及开发新抗感染药物的合理药物设计有关的最新和最重要的进展，涉及与抗感染药物化学有关的各个当前课题。
3. Anti Inflammatory & Anti allergy Agents in Medicinal Chemistry（ISSN：1871-5230）《医药化学中的抗炎与抗过敏药剂》介绍抗炎和抗过敏药物研制方面的最新进展。
4. Cardiovascular & Hematological Disorders- Drug Targets（ISSN：1871-529X）《心血管和血液系统疾病－药物靶体》涵盖与心血管和血液系统疾病有关的最新分子靶体，如疾病特异性蛋白、受体、酶和基因等的最新和最重要的进展。
5. Cardiovascular and Hematological Agents in Medicinal Chemistry（ISSN：1871-5257）《医药化学中的心血管和血液药剂》涵盖与药物化学及开发治疗心血管和血液系统疾病新药合理药物设计有关的最新和最重要的进展。
6. Central Nervous System Agents in Medicinal Chemistry（ISSN：1871-5249）《医药化学中的中枢神经系统药剂》介绍中枢神经系统药剂研究方面的最新进展，发表医药化学领域中枢神经系统最新研究课题的评论。
bendamustine 苯达莫司汀
-------------------------WARNINGS AND PRECAUTIONS--------------------- Myelosuppression: May warrant treatment delay or dose reduction. Monitor closely and restart treatment based on ANC and platelet count recovery. Complications of myelosuppression may lead to death. (5.1) Infections: Monitor for fever and other signs of infection and treat promptly. (5.2) Infusion Reactions and Anaphylaxis: Severe anaphylactic reactions have occurred. Monitor clinically and discontinue drug for severe reactions. Ask patients about reactions after the first cycle. Consider pre-treatment for cycles subsequent to milder reactions. (5.3) Tumor Lysis Syndrome: May lead to acute renal failure and death. Take precautions in patients at high risk. (5.4) Skin Reactions: Discontinue for severe skin reactions. Cases of SJS and TEN, some fatal, have been reported when TREANDA was administered concomitantly with allopurinol and other medications known to cause these syndromes. (5.5) Other Malignancies: Pre-malignant and malignant diseases have been reported. (5.6) Extravasation: Take precautions to avoid extravasation, including monitoring intravenous infusion site during and after administration. (5.7) Use in Pregnancy: Fetal harm can occur when administered to a pregnant woman. Women should be advised to avoid becoming pregnant when receiving TREANDA. (5.8, 8.1) --------------------------------ADVERSE REACTIONS----------------------------Most common non-hematologic adverse reactions for CLL (frequency 15%) are pyrexia, nausea, and vomiting. (6.1) Most common non-hematologic adverse reactions for NHL (frequency 15%) are nausea, fatigue, vomiting, diarrhea, pyrexia, constipation, anorexia, cough, headache, weight decreased, dyspnea, rash, and stomatitis. (6.2) Most common hematologic abnormalities for both indications (frequency ≥15%) are lymphopenia, anemia, leukopenia, thrombocytopenia, and neutropenia. (6.1, 6.2) To report SUSPECTED ADVERSE REACTIONS, contact Cephalon, Inc., at 1-800-896-5855 or FDA at 1-800-FDA-1088 or /medwatch. --------------------------------DRUG INTERACTIONS---------------------------- Concomitant CYP1A2 inducers or inhibitors have the potential to affect the exposure of bendamustine. (7) ---------------------------USE IN SPECIFIC POPULATIONS------------------- Renal impairment: Do not use if CrCL is <40 mL/min. Use with caution in lesser degrees of renal impairment. (8.6) Hepatic impairment: Do not use in moderate or severe hepatic impairment. Use with caution in mild hepatic impairment. (8.7) See 17 for PATIENT COUNSELING INFORMATION
治疗精神分裂症与重度抑郁症辅助用药——依匹哌唑(Brexpiprazole)
治疗精神分裂症与重度抑郁症辅助用药——依匹哌唑(Brexpiprazole)陈本川【摘要】美国食品药品管理局(FDA)于2015年7月10日批准丹麦灵北制药与日本大冢制药株式会社联合研制的brexpiprazole(暂译名依匹哌唑)片剂上市,商品名为Rexulti@.用于治疗成人精神分裂症与重度抑郁症的辅助治疗.该文对依匹哌唑非临床药理毒理学、临床药理毒理学、临床研究、适应证、剂量与用法、用药注意事项、不良反应及知识产权状态和国内外研究进展等进行介绍.【期刊名称】《医药导报》【年(卷),期】2016(035)001【总页数】4页(P后插1-后插4)【关键词】依匹哌唑;精神分裂症;抑郁症,重度【作者】陈本川【作者单位】湖北丽益科技有限公司,武汉430205【正文语种】中文【中图分类】R971.41;R969Brexpiprazole暂译名依匹哌唑，中文异名布瑞哌唑、依匹唑哌、依匹唑派等，中文化学名7-(4-(4-(苯并[b]噻吩)-4-基-哌嗪-1-基)丁氧基)-1H-喹啉-2-酮，代号为OPC-34712，由丹麦灵北制药(Lundbeck)和日本大冢制药株式会社共同研发。
美国食品药品管理局(FDA)于2015年7月10日批准依匹哌唑上市[1-4]，用于治疗成人精神分裂症(schizophrenia)与重度抑郁症(major depressive disorder，MDD)的辅助治疗。
商品名为Rexulti®。
成人精神分裂症是慢性致残性脑神经变性疾病，涉及感知、思维、情感和行为等多方面的障碍及精神活动的不协调。
MDD也是常见的脑精神障碍性疾病，以显著而持久的心境低落为主要临床特征，严重者可导致持续的悲伤、挫折感或愤怒，并有自杀念头和行为，多数病例有反复发作倾向。
1.1 致畸、致突变作用1.1.1 致畸对美国癌症研究所(Institute of Cancer Research，ICR)培育的小鼠和Sprague Dawley(SD)大鼠的生命周期进行致癌实验，分别给予雄性和雌性小鼠依匹哌唑0.75，2.0和 5.0 mg·kg-1·d-1，为期2年，该剂量相当于按体表面积[mg·(m2)-1]计算为人用口服最大推荐量(maximum recommended human dose，MRHD)4 mg·d-1 的0.9～6.1倍；分别给予雄性和雌性大鼠依匹哌唑1.0，3.0和10.0 mg·kg-1·d-1和3.0，10.0，和30.0 mg·kg-1·d-1，相当于按体表面积计算为MRHD 4 mg·d-1的2.4～24.0倍和7.32～73.00倍。
盐酸苯达莫司汀的合成优化
盐酸苯达莫司汀的合成优化关键词：盐酸苯达莫司汀合成优化盐酸苯达莫司汀（bendamustine hydrochloride，如图化合物iii）是一种双功能基烷化剂，具有抗肿瘤和杀细胞作用。
19世纪60年代初期由ozegowski和其同事在德国耶拿的微生物试验协会研制。
美国fda于2008年3月21日批准cephalon公司的盐酸苯达莫司汀（bendamustine hydrochloride，treanda）用于慢性淋巴细胞性白血病（cll）。
盐酸苯达莫司汀的化学名为4-[5-（双（2-氯乙基）氨基-1-甲基-2-苯并咪唑]丁酸盐酸盐，可用于治疗多种恶性肿瘤，具有良好的市场前景，有开发的潜力。
目前，有关其合成方法主要如下：通过2,4-二硝基氯苯与甲胺反应，得到化合物1；化合物1经硝基还原得到化合物2；化合物2经戊二酸酐处理得到化合物3,；化合物3经硫酸乙醇处理，得到化合物4；化合物4经再次硝基还原得到化合物5；化合物5经环氧乙烷反应，得到化合物6；化合物6在氯化亚砜的作用下氯代后用浓盐酸处理，得到化合物7，即盐酸苯达莫司汀。
本方法是合成盐酸苯达莫司汀的主要方法。
但是，在合成过程中，我们发现该合成路线有如下几个缺点：1）起始原料2,4-二硝基氯苯是剧毒化学品，按照我国的法律法规，不容易得到（或则需要较大的代价才可以得到）；2）在化合物2的制备过程中，需用到具有难闻气味的硫化物，给反应处理带来的难度，增加了工作人员的劳动保护成本；3）在最后一步的氯代过程中，我们发现有大量的氯化氢气体产生，对工作人员和反应设备的要求都比较高。
因此我们计划对此工艺进行了部分改进。
通过对工艺的分析并参考文献，我们计划直接采购中间体化合物4，即5-硝基-1-甲基-2-苯并咪唑丁酸乙酯为原料，经催化氢化、酰化、还原、成盐四步完成产品的合成。
其主要路线如下：一、仪器与试剂1h nmr核磁共振仪brucker 400mhz；elementar vario micro元素分析仪；安捷伦质谱仪；yrt-3熔点仪（温度计未校正）。
维莫非尼片说明书
核准日期：2017年3月10日修改日期：2017年5月26日2017年11月29日2018年7月24日2020年2月13日2021年2月26日2022年1月17日2022年2月22日维莫非尼片说明书请仔细阅读说明书并在医师指导下使用【药品名称】通用名：维莫非尼片商品名：佐博伏®,英文商品名Zelboraf®英文名：Vemurafenib film-coated tablets汉语拼音：Weimofeini Pian【成份】本品主要活性成分为维莫非尼，以维莫非尼和琥珀酸醋酸羟丙甲纤维素固体分散体存在。
化学名称：丙烷-1-磺酸{3-[5-(4-氯苯基)-1H- 吡咯并[2,3-b]吡啶-3-羰基]-2,4-二氟代苯基}- 酰胺。
化学结构式：分子式：C23H18ClF2N3O3S分子量：489.93【性状】两面凸起、粉白色至橙白色的薄膜衣片。
【适应症】佐博伏®适用于治疗经CFDA批准的检测方法确定的BRAF V600突变阳性的不可切除或转移性黑色素瘤。
【规格】240 mg【用法用量】患者必须经由CFDA批准的检测方法确定的证明肿瘤为BRAF V600突变阳性，才可使用佐博伏®治疗。
佐博伏®不能用于BRAF野生型黑色素瘤患者。
首剂药物应在上午服用，第二剂应在此后约12小时，即晚上服用。
每次服药均可随餐或空腹服用。
用一杯水送服药物，服药时整片吞下佐博伏®片剂。
不应咀嚼或碾碎佐博伏®片剂。
标准剂量佐博伏®的推荐剂量为960 mg（四片240 mg片剂），每日两次。
治疗持续时间建议佐博伏®治疗应持续至疾病进展或发生不可接受的毒性反应（参见表1和表2）。
漏服如果漏服一剂计划的药物，可在下一剂服药4小时以前补服漏服的药物，以维持每日两次的给药方案。
不应同时服用两剂药物。
呕吐如果佐博伏®服药后发生呕吐，患者不应追加剂量，而应按常规剂量继续治疗。
维格列汀
结语
结语
综上所述，维格列汀具有降低空腹及餐后血糖水平、餐后胰高血糖素分泌及提高B细胞功能的作用，为2型糖 尿病患者的治疗提供了新选择。该药与其他药物联合使用的安全性和有效性，禁忌证、不良反应等还有待于更多 的临床研究观察。
谢谢观看
药动学
药动学
健康人体的药动学研究表明，本品口服给药后迅速吸收，吸收率为85%，蛋白结合率为4%～17%，Tmax为1～ 2 h。当给药剂量在25～200mg时，血药浓度与给药剂量呈线性关系，t1/2为1．5～4．5 h。按25～200 mg单剂 量给药时，在30～60 min内，血浆中DPP-IV的抑制率能达到90%以上，但抑制的持续时间与剂量有关，当剂量为 50和100 mg时，DPP-IV的12 h抑制率分别为70%和90%，而100 mg组DPP-I V的24 h抑制率为40%。本品主要 (55%)通过水解氰基进行代谢，此外，22%的药物以原形药通过肾排泄，极少部分药物通过细胞色素P450酶代谢， 但本品既不是该酶的抑制剂，也不是诱导剂。多剂量给药时未出现药物蓄积现象，肝肾功能不全患者亦无需调整 剂量，且药动学结果也不受食性质
合成方法
基本性质
中文名称：维达列汀 中文别名：(-)-(2S)-1-[[(3-羟基三环[3.3.1.1[3,7]]硅烷-1-基)氨基]乙酰基]吡咯烷-2-甲腈；维他列 汀；(-)-(2S)-1-[[(3-羟基三环[3.3.1.1[3,7]]癸烷-1-基)氨基]乙酰基]吡咯烷-2-甲腈；维格列汀;维达利汀； 维达列汀VILDAGLIPTIN(研发中)；维他列汀S型； 英文名称：Vildagliptin 英文别名：Vildagliptin (NVP-LAF 237)；Galvus；Laf 237 ；Unii-I6B4B2U96p ；(-)-(2S)-1[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile； (-)(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile；2Pyrrolidinecarbonitrile,1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-(2S)-；； CAS号：-16-5 分子式：C17H25N3O2 维格列汀结构式： 分子量：303.
本维莫德乳膏2024课件
[1] 本维莫德乳膏说明书 [2] Cai L, Chen G, Lu Q, et al. Chin Med J (Engl). 2020 Nov 9;133(24):2905-2909. [3] Koo J, et al. J Am Acad Dermatol. 1999 Jul;41(1):51-9 [4]本维莫德乳膏BIA模型
5.公平性
本维莫德乳膏基本信息介绍
通用名：本维莫德乳膏[1] 注册规格：10g：0.1g(1%)；20g：0.2g(1%)；30g：0.3g(1%) 中国大陆首次上市时间：2019年5月29日 目前大陆地区同通用名药品的上市情况：无，独家产品 全球首个上市国家/地区及上市时间：中国，2019年5月29日 是否为OTC药品：非OTC药品 美国相同有效成分产品上市时间：2022年5月 参照药品建议：卡泊三醇软膏 与参照药品相比的优势：①治疗银屑病12周疗效优于卡泊三醇
外用药 是银屑 病的基 础治疗
中国银屑病诊疗指南提到[10]，外用药物适用于绝 大多数患者，并且是首选治疗。寻常型银屑病 中：轻度的斑块状银屑病以外用药物治疗为主， 大多能有效控制病情；中重度的斑块状银屑病使 用系统治疗均可联合外用药物提高疗效
《中国 银屑病 诊疗指 南》 四大治 疗目标
控制及稳定病情，减缓疾病发展进程， 抑制皮损加重及瘙痒等
二肽基肽酶4(DPP 4或DPP IV)
二肽基肽酶4（人重组）-QWBIO产品货号：ENZ-375产品名称：二肽基肽酶4（人重组蛋白），Dipeptidyl-Peptidase 4 Human Recombinant，DPP4 Human产品规格：2ug、10ug和1mg别名：CD26，ADABP，ADCP2，DPPIV，TP103，DPP4，Dipeptidyl peptidase 4（二肽基肽酶4），Dipeptidyl peptidase IV（二肽基肽酶4），DPP IV，T-cell activation antigen CD26（T细胞活化抗原CD26），Adenosine deaminase complexing protein 2（腺苷脱氨酶络合蛋白2），CD26 antigen（CD26抗原）。
产品简介：启维益成提供的二肽基肽酶4（DPP4），也叫腺苷脱氨酶络合蛋白2或T细胞活化抗原CD26，是一种在绝大多数类型细胞表面表达的丝氨酸羧肽酶复合酶。
二肽基肽酶4是一种内膜糖蛋白，具有丝氨酸羧肽酶功能，能从多肽的N末端水解X-脯氨酸二肽。
二肽基肽酶4在T细胞活化方面起着重要作用。
DPP4与细胞内信号转导、细胞凋亡和肿瘤生物学密切相关。
生长因子、趋化因子和神经肽等至少63种底物可以特异性结合二肽基肽酶4。
此外，DPP4在通过分解糖降血糖素如葡萄糖依赖性促胰岛素多肽（GIP）和胰高血糖素样肽-1（GLP-1）在糖代谢中起着重要的作用。
产品性质：启维益成提供的二肽基肽酶4人重组蛋白通过“High-5”细胞系生产，是一个包含746个氨基酸（39-766），分子量为86.4kDa的单一性糖基化多肽。
二肽基肽酶4的C末端融和组氨酸标签，并通过常规色谱技术纯化。
产品来源：High-5细胞系物理性质：过滤除菌的无色溶液产品配制：DPP4悬浮于20mM Tris盐酸缓冲液（pH=8），100mM氯化钠，1mM EDTA和10%甘油中。
产品稳定性：如果整瓶试剂将会在2-4周内用完，请4°C保存；-20°C可冻存较长时间；如果要长时间保存，推荐添加保护蛋白（0.1%HAS或BSA）。
多巴丝肼片日本药品说明书英文
多巴丝肼片日本药品说明书英文Doripenem Tablets: Japanese Medication Guide (English Version)Introduction:Doripenem is a commonly used medication in Japan for the treatment of various bacterial infections. This medication guide aims to provide users with comprehensive information about Doripenem tablets, including usage, dosage, precautions, side effects, and other important details. Please read this guide carefully before using Doripenem and consult your healthcare professional if you have any questions or concerns.Product Overview:- Name: Doripenem Tablets- Active Ingredient: Doripenem- Strength: 250 mg, 500 mg- Dosage Form: Tablets- Manufacturer: [Name of Manufacturer]- Approved by: [Name of Regulatory Authority]Usage:Doripenem is indicated for the treatment of the following infections caused by susceptible bacteria:- Community-acquired pneumonia- Hospital-acquired pneumonia- Complicated urinary tract infections, including pyelonephritis- Complicated intra-abdominal infections- Septicemia (bloodstream infections)- Febrile neutropenia (fever due to low white blood cell count)Dosage and Administration:- The recommended dosage for adults is [Dosage]. Please follow the instructions provided by your healthcare professional.- Doripenem tablets should be taken [Instructions on how to take the tablets, e.g., with or without food, with water].- The duration of treatment may vary depending on the type and severity of the infection. Please consult your healthcare professional for the recommended duration.Precautions:- Before using Doripenem, inform your healthcare professional about any allergies, medical conditions, or medications you are currently taking.- It is important to complete the full course of Doripenem treatment as prescribed by your healthcare professional, even if you start feeling better.- Do not share Doripenem tablets with others or use leftover medication for future infections.- Driving or operating machinery while under the influence of Doripenem may impair your abilities. Use caution until you know how Doripenem affects you.Side Effects:Doripenem may cause side effects in some individuals. Common side effects include:- Nausea- Diarrhea- Headache- Rash- Injection site reactions (if administered intravenously)If you experience severe or persistent side effects, contact your healthcare professional immediately. They will assess the risks and benefits of continuing Doripenem treatment.Storage:- Store Doripenem tablets at room temperature (between [temperature range]) in a dry place.- Keep the medication out of reach of children and pets.- Do not use Doripenem tablets beyond the expiration date mentioned on the packaging.Additional Information:- Doripenem may interact with certain medications. Inform your healthcare professional about all the medications you are taking to avoid potential drug interactions.- In case of an overdose, seek medical attention immediately or contact your local poison control center.- If you miss a dose of Doripenem, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and continue with your regular dosing schedule.Conclusion:This medication guide provides essential information about Doripenem tablets, their proper usage, dosage, precautions, and potential side effects. It is crucial to consult with your healthcare professional and follow their instructions for the safe and effective use of Doripenem. If you have any additional questions or concerns, seek medical advice for further assistance.。
四正柏生物科技基因定点突变试剂盒说明书
基因定点突变试剂盒保存条件及效期：−20℃保存，有效期一年。
产品描述：定点突变是一种广泛应用的分析蛋白和DNA 的非常有力的工具。
普通的定点突变试剂盒通常是基于反向PCR 技术，采用高保真耐热DNA 聚合酶和互补的突变引物向目的基因引入单个碱基或多个邻近碱基的突变、缺失、或插入。
当遇到多个位点突变的需求时，利用单点突变试剂盒只能对目标位点逐一引入突变，耗时费力。
Mut Multi Site-directed Mutagenesis(MSDM)Kit 针对每一个目标突变只采用一条突变引物，利用Mut MSDMEnzyme 的耐热DNA 聚合酶活性合成与模板互补的带有引物突变的DNA 链，然后通过其耐热的连接酶活性修复突变DNA 链之间的切刻(nicks)，使其连接成为一条与模板互补的突变单链DNA 。
经过多个PCR 循环反应后，带有多个特定突变的DNA 链成倍增长。
PCR 反应结束后，采用DpnI 限制性内切酶消化含有甲基化的双链质粒模板，而带有突变的环形单链质粒则通过转化而在大肠杆菌体内复制，最终得到带有不同突变组合的质粒DNA 。
本试剂盒适用于≤6kb 质粒的多点突变，根据质粒性质不同，最多可引入5个位点的突变、插入或删除(通常以1~3个位点突变为主)。
该方法操作简单快捷，突变阳性率高。
产品组分:产品编号规格MSM5303-1010rxnMut MSDM Enzyme12μl 10x MutMSDM Buffer 100μl MutdNTPs25μl Dpn I (10U/ l)12μl ddH 2O1ml版本号:2016-02-19产品说明书图1.Mut 多点基因定点突变试剂盒原理和操作流程示意图使用方法：1.模板准备：(1)请使用6kb以下的质粒作为模板；如果模板质粒过大，可将所需突变的序列亚克隆到较小的载体中，完成突变后再克隆到目的载体中。
(2)对于非甲基化的质粒(例如从大肠杆菌JM110或SCS110菌株中提取的质粒)，可通过转化dam＋的大肠杆菌菌株(如DH5α、TOP10、JM109、XL1-Blue等)，再抽提获得甲基化的质粒作为PCR反应模板。
卫材在日本市场推出其首款抗肿瘤药盐酸苯达莫司汀注射剂
卫材在日本市场推出其首款抗肿瘤药盐酸苯达莫司汀注射剂佚名
【期刊名称】《世界临床药物》
【年(卷),期】2011(32)3
【摘要】卫材公司已在日本推出其抗肿瘤药盐酸苯达莫司汀（bendamustine，Treakisym）注射剂，该药被批准用于治疗低度悲性B细胞性非霍奇金淋巴瘤。
【总页数】1页(P191-191)
【关键词】抗肿瘤药;日本市场;注射剂;B细胞性非霍奇金淋巴瘤;盐酸;苯
【正文语种】中文
【中图分类】R979.1
【相关文献】
1.高效液相色谱荧光检测法测定人血浆中苯达莫司汀及γ-羟基化苯达莫司汀浓度[J], 吴蔚;刘智;程航;刘姗姗;余鹏;程泽能
2.抗肿瘤药苯达莫司汀 [J], 黄世杰
3.新型抗肿瘤药物——苯达莫司汀 [J], 王晓坤
4.Polatuzumab Vedotin联合苯达莫司汀及利妥昔单抗(pola-BR)对比苯达莫司汀联合利妥昔单抗(BR)治疗复发/难治性DLBCL的疗效分析 [J], 应志涛
5.盐酸苯达莫司汀的热稳定性与晶型对比研究 [J], 杜超;刘相男;唐云;李伟
因版权原因，仅展示原文概要，查看原文内容请购买。
贝冬西丁成分
贝冬西丁成分贝冬西丁（Bedaquiline）是一种新型抗结核药物，于2012年被FDA 批准上市。
该药物仅用于治疗多药耐药结核病（MDR-TB），即对常规的抗结核药物产生耐药性的结核菌感染。
一、化学成分贝冬西丁的化学名为N-[4-({(1R,2S)-2-[(6-{3-[(5-cyclopropyl-2-pyridyl)methoxy]phenyl}pyridin-4-yl)methyl]-1-cyclohexen-1-yl}carbonyl)piperazin-1-yl]benzamide，其分子式为C32H31N3O2，分子量为499.62。
二、药理作用贝冬西丁是一种ATP合酶抑制剂，可抑制结核菌细胞内能量代谢的关键酶ATP合酶。
该药物可选择性地抑制革兰氏阳性细菌中的ATP合酶F_0F_1和细胞膜ATPase，从而阻断其能量代谢通路。
三、适应症贝冬西丁仅适用于治疗多药耐药结核病（MDR-TB），即对常规的抗结核药物产生耐药性的结核菌感染。
四、用法用量1. 贝冬西丁的剂量为每天400毫克，分为两次口服，每次200毫克。
2. 该药物应在与其他抗结核药物联合使用的情况下使用，治疗期限一般为24周。
3. 贝冬西丁应在餐后服用，并应与脂肪含量较高的食物一起服用，以提高其吸收率和生物利用度。
五、不良反应1. 最常见的不良反应是恶心和呕吐，发生率约为11%至15%。
2. 另外，贝冬西丁还可能引起头晕、疲劳、关节疼痛、胸痛等不适症状。
3. 在极少数情况下，该药物可能会引起心律失常和肝功能异常等严重不良反应。
六、禁忌症1. 对贝冬西丁或其任何成分过敏者禁止使用该药物。
2. 由于贝冬西丁可能会引起心律失常，在患有心脏问题或正在接受心脏治疗的患者中应慎用。
3. 妊娠和哺乳期妇女应避免使用该药物。
七、注意事项1. 患有肝、肾功能不全或其他严重疾病的患者应在医生的指导下使用该药物。
2. 贝冬西丁可能会与其他药物相互作用，因此在使用该药物之前，应告知医生正在使用的所有药物，包括处方药、非处方药和保健品等。
哌拉西林钠他唑巴坦在重症脓毒症治疗中的临床效果研究
DOI：10.19368/ki.2096-1782.2024.05.064哌拉西林钠他唑巴坦在重症脓毒症治疗中的临床效果研究安宇，张莉，陈卫星青岛市黄岛区中医医院重症医学科，山东青岛266500[摘要]目的研究哌拉西林钠他唑巴坦在重症脓毒症治疗中的临床效果。
方法选取2021年1月—2023年10月青岛市黄岛区中医医院重症医学科收治的62例重症脓毒症患者作为研究对象。
采用随机数表法分为两组，每组31例。
对比组使用头孢噻肟钠治疗，研究组使用哌拉西林钠他唑巴坦治疗。
对比两组的症状积分、炎性因子含量、免疫球蛋白水平、治疗有效性、不良反应情况。
结果治疗后，研究组的症状积分、炎性因子含量均低于对比组；免疫球蛋白水平高于对比组，差异有统计学意义（P均<0.05）。
研究组的治疗有效性高于对比组，不良反应发生率低于对比组，差异有统计学意义（P均<0.05）。
结论哌拉西林钠他唑巴坦为重症脓毒症患者进行治疗的效果较高，能够缓解患者心慌等症状，降低机体炎症反应，且不良反应情况较少。
[关键词]哌拉西林钠他唑巴坦；重症脓毒症；治疗有效性[中图分类号]R4 [文献标识码]A [文章编号]2096-1782（2024）03(a)-0064-04Study on the Clinical Effectiveness of Piperacillin Sodium Tazobactam in the Treatment of Severe SepsisAN Yu, ZHANG Li, CHEN WeixingDepartment of Critical Care Medicine, Huangdao District Hospital of Traditional Chinese Medicine, Qingdao, Shan⁃dong Province, 266500 China[Abstract] Objective To study the clinical effect of piperacillin sodium tazobactam in the treatment of severe sepsis.Methods A total of 62 patients with severe sepsis admitted to the Department of Critical Care Medicine of Huangdao District Hospital of Traditional Chinese Medicine from January 2021 to October 2023 were selected as the study ob⁃jects, and were divided into two groups according to randomized numerical table method, with 31 cases in each group. Cefotaxime sodium was used in the comparison group and piperacillin sodium tazobactam was used in the study group. The symptom scores, inflammatory factor levels, immunoglobulin levels, therapeutic effectiveness, and adverse effects were compared between the two groups. Results After treatment, the symptom score, level of inflammatory factors of the study group were lower than those of the comparison group, the immunoglobulin level of the study group was higher than that of the comparison group, and the differences were statistically significant (all P<0.05). The therapeu⁃tic effectiveness of the study group was higher than that of the comparison group, the incidence rate of adverse reac⁃tions in the study group was lower than that in the comparison group, and the differences were statistically significant (both P<0.05). Conclusion Piperacillin sodium tazobactam is selected for the treatment of patients with severe sepsis has a high effect, can alleviate the symptoms such as panic in patients, reduce the inflammatory response of the body, and the adverse reaction situation is less.[Key words] Piperacillin sodium tazobactam; Severe sepsis; Therapeutic efficacy[作者简介] 安宇（1988-），女，硕士，主治医师，研究方向为中西医结合重症医学。
欧洲术后镇痛指南
PostoperativePain Management –Good Clinical PracticeGeneral recommendationsand principles forsuccessful pain managementProduced in consultation with theEuropean Society of Regional Anaesthesiaand Pain TherapyPostoperativePain Management –Good Clinical PracticeGeneral recommendationsand principles forsuccessful pain managementProduced in consultation with theEuropean Society of Regional Anaesthesiaand Pain TherapyContents ContentsContents11. Introduction and objectives1 Although the choice of drugs shown here is indicative, adjustments will be required to take account ofindividual patient variation and are the responsibility of the prescribing physician.Effective postoperative pain management has a humanitarian role, but there are additional medical and economic benefits for rapid recovery and discharge from hospital. A number of factors contribute to effective postoperative pain management including a structured acute pain management team, patient education, regular staff training, use of balanced analgesia, regular pain assessment using specificassessment tools and adjustment of strategies to meet the needs of special patient groups, such as children and the elderly.Recent advances in pain control provide greater potential for effective postoperative management. This document reflects the opinions of a panel of European anaesthesiologists. Its aims are to raise awareness of recent advances in pain control and to provide advice on how toachieve effective postoperative analgesia. The recommendations and advice are general principles of pain management and do not provide detailed advice for specific surgical procedures.1Effective pain management is now an integral part of modern surgical practice. Postoperative pain management not only minimises patient suffering but also can reduce morbidity and facilitate rapid recovery and early discharge from hospital (see section 8, page 33), which can reduce hospital costs.23Pain is a personal, subjective experience that involves sensory,emotional and behavioural factors associated with actual or potentialtissue injury. What patients tell us about their pain can be very revealing,and an understanding of how the nervous system responds and adaptsto pain in the short and long term is essential if we are to make sense ofpatients’ experiences. The wide area of discomfort surrounding awound, or even a wound that has healed long ago, such as anamputation stump, is a natural consequence of the plasticity of thenervous system. An understanding of the physiological basis of pain ishelpful to the sufferer, and the professionals who have to provideappropriate treatment.According to the International Association for the Study of Pain (IASP),pain is defined as"An unpleasant sensory and emotional experience associated withactual or potential tissue damage, or described in terms of suchdamage."(IASP 1979)There is individual variation in response to pain, which is influenced bygenetic makeup, cultural background, age and gender. Certain patientpopulations are at risk of inadequate pain control and require specialattention. These include:G Paediatric patientsG Geriatric patientsG Patients with difficulty in communicating (due to critical illness,cognitive impairment or language barriers)Postoperative pain can be divided into acute pain and chronic pain:G Acute pain is experienced immediately after surgery (up to 7 days)G Pain which lasts more than 3 months after the injury is considered tobe chronic pain3. Physiology of pain 2. Goals of pain treatmentAcute and chronic pain can arise from cutaneous, deep somatic orvisceral structures. Surgery is typically followed by acute pain and correct identification of the type of pain enables selection of appropriate effective treatment. The type of pain may be somatic (arising from skin, muscle, bone), visceral (arising from organs within the chest and abdomen), or neuropathic (caused by damage or dysfunction in the nervous system). Patients often experience more than one type of pain.3.a. Positive role of painAcute pain plays a useful "positive" physiological role by:G Providing a warning of tissue damageG Inducing immobilisation to allow appropriate healing3.b. Negative effects of painShort term negative effects of acute pain include:G Emotional and physical suffering for the patientG Sleep disturbance(with negative impact on mood and mobilisation)G Cardiovascular side effects(such as hypertension and tachycardia)G Increased oxygen consumption(with negative impact in the case of coronary artery disease)G Impaired bowel movement(while opioids induce constipation or nausea, untreated pain mayalso be an important cause of impaired bowel movement or PONV*)G Negative effects on respiratory function(leading to atelectasis, retention of secretions and pneumonia)G Delays mobilisation and promotes thromboembolism(postoperative pain on mobilisation is one of the major causes fordelayed mobilisation)Long term negative effects of acute pain:G Severe acute pain is a risk factor for the development of chronicpain1G There is a risk of behavioural changes in children for a prolongedperiod (up to 1 year) after surgical painThere are two major mechanisms in the physiology of pain:G Nociceptive (sensory):Inflammatory pain due to chemical,mechanical and thermal stimuli at the nociceptors (nerves thatrespond to painful stimuli).G Neuropathic:Pain due to neural damage in peripheral nervesor within the central nervous system.During normal physiology, pain sensations are elicited by activity in unmyelinated (C-) and thinly myelinated (Ad-) primary afferent neurons that synapse with neurons is the dorsal horn of the spinal cord. Sensory information is then relayed to the thalamus and brainstem.Repetitive activation of C- nociceptive receptors produces alterations in central as well as peripheral nervous systems.3.c. The mechanism of peripheral pain sensitisationNormally, C- fibres (slow-conducting fibres that transmit dull aching pain) are silent in the absence of stimulation, but following acute tissue injury in the presence of ongoing pathophysiology, these nociceptors become sensitised and release a complex mix of pain and inflammatory mediators leading to pain sensations (Figure 1, page 6).1Several investigations into chronic pain have concluded that 20% to 50% of all patients with chronic pain syndromes started with acute pain following trauma or surgery, but the role of effective pain treatment in preventing this risk is not clear.* PONV = Postoperative Nausea and Vomiting.Figure 1.Mechanism of peripheral sensitisation3.d. The mechanism of central sensitisationThe responses in the CNS are primarily physiological. Centralsensitisation is a physiological process and, only if there is continual firing of C-nociceptors over time, will these processes leads to more chronic pain syndromes.Sustained or repetitive C-nociceptor activity produces alterations in the response of the central nervous system to inputs from the periphery.When identical noxious stimuli are repeatedly applied to the skin at a certain rate, there is a progressive build-up in the response of spinalcord dorsal horn neurons (known as ‘wind up’). This allows the size of the dorsal horn neuron’s receptive field to grow (Figure 2). This process,called central sensitisation, occurs with any tissue damage. As with sensitisation of primary afferent nociceptors, this sensitisation of central pain transmission is a normal physiological response of the undamaged nervous system.Figure 2.Pain mediatorsGUnexpected intense pain, particularly if associated with altered vital signs, (hypotension, tachycardia, or fever), is immediately evaluated. New diagnoses, such as wound dehiscence, infection, or deep venous thrombosis, should be considered.GImmediate pain relief without asking for a pain rating is given to patients in obvious pain who are not sufficiently focused to use a pain rating scale.GFamily members are involved when appropriate.4.a. Specific tools for pain assessmentSpecific pain assessment scales are used to quantify pain. The use of one scale within a hospital ensures that everyone in the team "speaks the same language"regarding the intensity of pain. The patient's own report is the most useful tool. The intensity of pain should therefore be assessed as far as possible by the patient as long as he/she is able tocommunicate and express what pain feels like. Always listen to and believe what the patient says.A number of different patient self-assessment scales are available (Figure 3, page 12):A. Facial expressions: a pictogram of six faces with differentexpressions from smiling or happy through to tearful. This scale is suitable for patients where communication is a problem, such as children, elderly patients, confused patients or patients who do not speak the local language.B. Verbal rating scale (VRS): the patient is asked to rate their pain on a five-point scale as "none, mild, moderate, severe or very severe".Assessment of pain is a vital element in effective postoperative pain management. The principles of successful pain assessment are shown in Table 1.44. Assessment of pain4G The treatment strategy to be continued is discussed by the physician responsible for the patient in conjunction with the ward nurses.GThe physician and nurses pay attention to the effects and side effects of the pain treatment.C. Numerical rating scale (NRS): This consists of a simple 0 to 5 or 0 to 10 scale which correlates to no pain at zero and worst possible pain at 5 (or 10). The patient is asked to rate his/her pain intensity as a number.D. Visual analogue scale (VAS): This consists of an ungraduated,straight 100 mm line marked at one end with the term " no pain" and at the other end "the worst possible pain". The patient makes a cross on the line at the point that best approximates to their pain intensity.The VRS and NRS are the most frequently used assessment tools in the clinical setting while the VAS scale is primarily used as a research tool.4.b. Selection of suitable assessment tool (Figure 3, page 12):When selecting a pain assessment tool ensure that:GIt is appropriate for the patient's developmental, physical, emotional, and cognitive statusGIt meets the needs of both the patient and the pain management team4.c. DocumentationDocument pain regularly, take appropriate action and monitor efficacy and side effects of treatment. Record the information in a well-defined place in the patient record, such as the vital sign sheet or a purpose-designed acute pain chart.GThe nurse responsible for the patient reports the intensity of pain and treats the pain within the defined rules of the local guidelines. GThe physician responsible for the patient may need to modify theintervention if evaluation shows that the patient still has significant pain.44Faces painassessmentscale(Fig A) Patientable to communicatewell ?VRS painassessmentscale(Fig B)NRSassessmentscale(Fig C)VASassessmentscale(Fig D) NoYesChoice of assessment tool12Fig A. Alternatecoding Fig B.Fig C. Fig D.G Select a pain assessment tool, and teach the patient to use it.Determine the level of pain above which adjustment of analgesia or other interventions will be considered.G Provide the patient with education and information about pain control.GEmphasise the importance of a factual report of pain, avoiding stoicism or exaggeration.The "Patient Information Project" is a useful source of information for patients who require information about anaesthesia and postoperative pain management. This is a joint project between the Royal College of Anaesthetists and the Association of Anaesthetists of Great Britain and Ireland, together with patient representative groups. The website is:Patients are unlikely to be aware of postoperative pain treatment techniques and as the success of pain relief is influenced by theirknowledge and beliefs, it is helpful to give patients (and parents in case of children) detailed information about postoperative pain and pain treatment. Adequate information gives the patient realistic expectations of the care that can be provided (pain relief, not a "pain free status"). This information can include:G The importance of treating postoperative pain G Available methods of pain treatment G Pain assessment routinesG Goals (optimum pain scoring) (see section 2, page 2)GThe patient's participation in the treatment of painInformation for the patient can be given in different ways (in combination):G Verbal informationGWritten and/or audiovisual information -Brochures -Wall posters -Video films -Web pagesA preoperative discussion with the patient and relatives can include the following:GDiscuss the patient's previous experiences with pain and preferences for pain assessment and management.GGive the patient information about pain management therapies that are available and the rationale underlying their use.GDevelop with the patient a plan for pain assessment and management.141555. Patient education51716Effective treatment of postoperative pain includes a number of factors,including good nursing, non-pharmacological techniques, such as distraction, and balanced (multimodal) analgesia to provide adequate pain relief with optimal drug combinations used at the lowest effective doses.6.a. Pharmacological methods of pain treatment 1Postoperative pain management should be step-wise and balanced (Figure 4, page 18). The four main groups of analgesic drugs used for postoperative pain management are shown in Table 2 opposite, with examples of drugs listed in each group.6.a.i. Balanced (multimodal) analgesiaBalanced (multimodal) analgesia uses two or more analgesic agents that act by different mechanisms to achieve a superior analgesic effect without increasing adverse events compared with increased doses of single agents. For example, epidural opioids can be administered in combination with epidural local anaesthetics; intravenous opioids can be administered in combination with NSAIDs, which have a dose sparing effect for systemically administered opioids.Balanced analgesia is therefore the method of choice wherever possible,based on paracetamol and NSAIDs for low intensity pain with opioid analgesics and/or local analgesia techniques being used for moderate and high intensity pain as indicated (Figure 4, page 18).66. Treatment optionsTable 2Pharmacological options of pain managementNon-opioid analgesicsParacetamolNSAIDs, including COX-2 inhibitors*Gabapentin, pregabalin 2Weak opioidsCodeine TramadolParacetamol combined with codeine or tramadol Strong opioidsMorphine Diamorphine Pethidine Piritramide Oxycodone Adjuvants**Ketamine Clonidine* At the time of writing, COX-2 inhibitor drugs are subject to scrutiny by international regulatory bodies with regard to adverse outcomes when used for long-term oralprescription or for pain relief in patients with cardiovascular problems such as myocardial infarction, angina pectoris, hypertension. Rofecoxib has been withdrawn fromsales and prescription of valdecoxib has been suspended pending further research into its adverse events profile for cardiovascular morbidity and the occurrence of severemuco-cutaneous side effects. The injectable COX-2 inhibitor, parecoxib remains available for short-term use in treating postoperative pain. All NSAIDs should be used with care in patients with cardiovascular disease.** These adjuvants are not recommended for routine use in acute pain management because of their adverse side effects. Their use should be restricted to specialists in managing pain problems.62Gabapentin and pregabalin are approved for pain management but at the time of writing there is little published data to recommend the use of these drugs for acute pain management.1The example doses given are indicative and do not take account of individual patient variation.196.a.ii. Opioids 1Severeintensity painFor example:ThoracotomyUpper abdominal surgery Aortic surgery Knee replacementModerateintensity painFor example:Hip replacement Hysterectomy Jaw surgeryMildintensity painFor example:Inguinal hernia VaricesLaparoscopy(i) Paracetamol and wound infiltration with local anaesthetic (ii) NSAIDs (unless contraindicated) and(iii) Regional block analgesiaAdd weak opioid or rescue analgesia with small increments of intravenous strong opioid if necessary(i) Paracetamol and wound infiltration withlocal anaesthetic (ii) NSAIDs (unless contraindicated) and (iii) Peripheral nerve block(single shot or continuous infusion) or opioid injection (IV PCA)(i) Paracetamol and woundinfiltration with local anaesthetic (ii) NSAIDs (unlesscontraindicated) and (iii) Epidural local analgesia ormajor peripheral nerve or plexus block or opioid injection (IV PCA)1 The examples given here represent levels of pain commonly experienced and are subject to individual variation and contra-indications may apply.Figure 4Treatment options in relation to magnitude of postoperative pain expected following different types of surgery 1Table 3Morphine and weak opioidsMorphine Administration(i) Intravenous.(ii) Subcutaneous by continuous infusion or intermittent boluses via indwelling cannula.(iii) Intramuscular (not recommended due to incidence of pain. 5-10 mg 3-4 hourly).Dosage:IV PCABolus: 1-2 mg, lockout: 5-15 min (usually 7-8 min),no background infusion.Subcutaneous0.1-0.15 mg/kg 4-6 hourly, adapted in relation to pain score, sedation and respiratory rate.Monitoring Pain score, sedation, respiratory rate, side mentsSide effects such as nausea, vomiting, sedation and apnoea.No other opioid or sedative drug should be administered.18continued overleaf1 The doses and routes of administration of drugs described above are general examples and each patient should beassessed individually before prescribing.2120 6.a.iii. Non-opioids 1Table 5Combination of codeine + paracetamolAdministration Oral.DosageParacetamol 500 mg + codeine 30 mg. 4 x 1 g paracetamol/day.Monitoring Pain score, sedation, side effects.CommentsAnalgesic action is likely to be due to conversion to morphine. A small number of patients derive no benefit due to absence of the converting enzyme.NV = nausea and vomitingTramadol Administration(i) Intravenous: inject slowly (risk of high incidence of NV).(ii) Intramuscular.(iii) Oral administration as soon as possible.Dosage 50-100 mg 6 hourly.Monitoring Pain score, sedation, respiratory rate, side mentsTramadol reduces serotonin and norepinephrine reuptake and is a weak opioid agonist.In analgesic efficiency, 100 mg tramadol is equivalent to 5-15 mg morphine.Sedative drugs can have an additive effect.Table 4ParacetamolAdministration(i) Intravenous: Start 30 min before the end of surgery.(ii) Oral administration as soon as possible.Duration: as long as required.Dosage4 x 1 g paracetamol/day (2 g propacetamol/day).Dose to be reduced (e.g. 3 x 1 g/day) in case of hepatic insufficiency.Monitoring Pain scores.CommentsShould be combined with NSAID and/or opioids or loco-regional analgesia for moderate to severe pain.1 The doses and routes of administration of drugs described above are general examples and each patient should beassessed individually before prescribing.1 The doses and routes of administration of drugs described above are generally examples and each patient should be assessed individually before prescribing.Table 3 (continued)Codeine Administration OralDosage3 mg/kg/day combined with paracetamol.A minimum of 30 mg codeine/tablet is required.Monitoring Pain score, sedation, side effects.CommentsAnalgesic action is likely to be due to conversion to morphine. A small number of patients derive no benefit due to absence of the converting enzyme.6.a.iv. AdjuvantsIn addition to systemic administration of NSAIDs or paracetamol, weak opioids and non-opioid analgesic drugs may be administered "on request" for moderate or severe pain. These include ketamine and clonidine. Clonidine can be administered orally, intravenously orperineurally in combination with local anaesthetics. However, the side effects could be significant. The most important ones are hypotension and sedation. Ketamine can be administered via oral, intramuscular or intravenous routes. It has also significant side effects.6.a.v. Regional analgesiaContinuous Central Neuraxis Blockade (CCNB)CCNB is one of the most effective forms of postoperative analgesia, but it is also one of the most invasive. However, CCNB remains the first choice for a number of indications, such as abdominal, thoracic, and major orthopaedic surgery, where adequate pain relief cannot be achieved with other analgesia techniques NB can be achieved via two routes:G Continuous epidural analgesia - the recommended first choice GContinuous spinal analgesia - should be limited to selected cases only, as there is less experience with this techniquePostoperative epidural analgesia is usually accomplished with acombination of a long-acting local anaesthetic and an opioid, in dilute concentrations. Long-acting local anaesthetics are preferred because they are associated with less tachyphylaxis. Maintenance techniques in epidural analgesia include:GContinuous Infusion (CI): An easy technique that requires littleintervention. The cumulative dose of local anaesthetic is likely to be higher and side effects are more likely than with the other two techniques.2322Table 6NSAIDs 1Administration(i) Intravenous: administration should start at least 30-60 min before end of surgery.(ii) Oral administration should start as soon as possible.Duration: 3-5 days.Dosage examples(i) Conventional NSAIDs include:ketorolac: 3 x 30-40 mg/day (only IV form)diclofenac: 2 x 75 mg/day ketoprofen: 4 x 50 mg/day (ii) Selective NSAIDs include:meloxicam 15 mg once dailyCOX-2 inhibitors are now licensed for postoperative pain management. They are as efficient as ketorolac but reduce GI side effects. Examples include: parecoxib: 40 mg followed by 1-2 x 40 mg/day (IV form) or celecoxib: 200 mg/day. However, there is some debate due to cardiovascular risks in patients witharteriosclerosis. *See note below Table 2, page 17MonitoringPain scores.Renal function in patients with renal or cardiac disease, elderly patients, or patients with episodes of severe hypotension. Gastrointestinal side effects. Non-selective NSAIDs would be combined with proton inhibitors (i.e. omeprasol) in patients at risk of gastrointestinal side effects.CommentsCan be added to the pre-medication.Can be used in association with paracetamol and/or opioids or local regional analgesia for moderate to severe pain.1 The doses and routes of administration of drugs described above are general examples and each patient should beassessed individually before prescribing.2524Continuous Peripheral Nerve Blockade (CPNB)Continuous peripheral nerve blocks are being increasingly used since they may provide more selective but still excellent postoperative analgesia with reduced need for opioids over an extended period.Peripheral nerve blocks (PNBs) avoid the side effects associated with central neuraxial blockade, such as hypotension and wide motorblockade with reduced mobility and proprioception, and complications such as epidural haematoma, epidural abscess and paraparesis.After major orthopaedic lower limb surgery, clinical studies showperipheral nerve blocks are as effective as epidural and that both are better than IV opioids. Examples of drugs and dosages for use in continuous peripheral analgesia are shown in Table 8.Table 8Examples of local anaesthetics and doses in continuous peripheral nerve analgesiaG Intermittent Top-up: Results in benefits due to frequent patient/staff contact but can produce a high staff workload and patients may have to wait for treatment.GPatient-Controlled Epidural Analgesia (PCEA): This technique produces high patient satisfaction and reduced dose requirements compared with CI. However, sophisticated pumps are required and accurate catheter position is important for optimal efficacy.Examples of drugs and dosages for use in continuous epidural analgesia are shown in Table 7.Table 7Examples of local anaesthetics and opioids and doses in epidural analgesia 1LocalRopivacaineSufentanil 0.5-1 µg/ml anaesthetics/opioids0.2% (2 mg/ml) or orFentanyl 2-4 µg/mlLevobupivacaine or Bupivacaine0.1-0.2% (1-2 mg/ml)Dosage for continuous 6-12 ml/hinfusion (thoracic or lumbar level)Dosage for patient Background: 4-6 ml/h controlled infusion Bolus dose: 2 ml (2-4 ml)(lumbar or thoracic)2Minimum lockout interval 10 min (10-30 min)Recommended maximum hourly dose (bolus + background): 12 ml1 The tip of the catheter should be placed as close as possible to the surgical dermatomes: T6-T10 for majorintra-abdominal surgery, and L2-L4 for lower limb surgery.2 There are many possible variations in local anaesthetic/opioid concentration yielding good results, the examples givenhere should be taken as a guideline; higher concentrations than the ones mentioned here are sometimes required but cannot be recommended as a routine for postoperative pain relief.Site of catheterLocal anaesthetics and dosage*Ropivacaine 0.2%Bupivacaine 0.1-0.125%Levobupivacaine 0.1-0.2%Interscalene5-9 ml/h Infraclavicular 5-9 ml/h Axillary 5-10 ml/h Femoral 7-10 ml/h Popliteal3-7 ml/h*Sometimes, higher concentrations are required in individual patients. As a standard, starting with a low concentration/dose is recommended to avoid sensory loss or motor block.2726Patient Controlled Regional Analgesia (PCRA) can be used to maintain peripheral nerve block. A low basal infusion rate (e.g. 3-5 ml/h)associated with small PCA boluses (e.g. 2.5-5 ml - lockout: 30-60 min) is the preferred technique.Infiltration blocksPain relief may be achieved by infiltration of the wound with localanaesthetic. The technique is easy to perform by the surgeon at the time of surgery. The efficacy and duration of analgesia depend on the length of the wound and the type of local anaesthetic used (Table 9).The advantages and disadvantages of various techniques of regional analgesia are shown in Table 10.Table 9Local anaesthetic infiltrationLocal anaestheticVolumeAdditivesIntraarticular instillation Knee arthroscopy0.75% Ropivacaine 20 ml Morphine 1-2 mg 0.5% Bupivacaine20 ml Morphine 1-2 mgShoulder arthroscopy 0.75% Ropivacaine10-20 mlIntraperitoneal instillation Gynaecological 0.75% Ropivacaine 20 ml Cholecystectomy 0.25% Ropivacaine40-60 mlWound infiltration Inguinal hernia0.25-0.5% Ropivacaine 30-40 ml 0.25-0.5% Levobupi*30-40 ml0.25-0.5% Bupivacaine Up to 30 mlTable 10Advantages of different techniques of regional analgesiaAdvantagesDisadvantagesContinuous Very effective.Motor block and urinary Epiduralretention may develop Analgesia (CEA)Much experience.or persist depending on the concentrations used.Differential block withDrugs used must have motor sparing is possible.low risk of systemic toxicity and produce as little motor Excellent postoperative block as possible.pain control over an extended period.Requires regular clinical monitoring on surgical Useful for rehabilitation wards or ICU.and physiotherapy.There are no universal Reduces the quantity of guidelines for monitoring.opioid analgesics needed.May mask a haematoma or abscess resulting in damage to spinal nerves.continued overleafThyroid surgery0.25-0.5% Ropivacaine 10-20 ml 0.25-0.5% Levobupi*10-20 ml0.25-0.5% Bupivacaine Up to 20 mlPerianal surgery0.25-0.5% Ropivacaine 30-40 ml 0.25-0.5% Levobupi*30-40 ml0.25-0.5% Bupivacaine Up to 30 mlcontinued opposite* Levobupi = Levobupivacaine.* Levobupi = Levobupivacaine.Please consult the manufacturer’s full prescribing information before use.。
苯佐那酯胶囊说明书(英语)
TESSALON ®100 mg Perles200 mg Capsules(benzonatate, USP)DESCRIPTIONTESSALON, a non-narcotic oral antitussive agent, is 2, 5, 8, 11, 14, 17, 20, 23, 26-nonaoxaoctacosan-28-yl p-(butylamino) benzoate; with a molecular weight of 603.7.CH 3(CH 2)2CH 2NHCOOCH 2CH 2(OCH 2CH 2)n OCH 3Each TESSALON Perle contains:Benzonatate, USP 100 mg C 30H 53NO 11 Each TESSALON Capsule contains: Benzonatate, USP 200 mg TESSALON Capsules also contain: D&C Yellow 10, gelatin, glycerin, methylparaben and propylparaben.CLINICAL PHARMACOLOGY TESSALON acts peripherally by anesthetizing the stretch receptors located in the respiratory passages, lungs, and pleura by dampening their activity and thereby reducing the cough reflex at its source. It begins to act within 15 to 20 minutes and its effect lasts for 3 to 8 hours. TESSALON has no inhibitory effect on the respiratory center in recommended dosage.INDICATIONS AND USAGETESSALON is indicated for the symptomatic relief of cough.CONTRAINDICATIONSHypersensitivity to benzonatate or related compounds.WARNINGS Hypersensitivity Severe hypersensitivity reactions (including bronchospasm, laryngospasm and cardiovascular collapse) have been reported which are possibly related to local anesthesia from sucking or chewing the capsule instead of swallowing it. Severe reactions have required intervention with vasopressor agents and supportive measures. Psychiatric Effects Isolated instances of bizarre behavior, including mental confusion and visual hallucinations, have also been reported in patients taking TESSALON in combination with other prescribed drugs.Accidental Ingestion and Death in Children Keep TESSALON out of reach of children. Accidental ingestion of TESSALON resulting in death has been reported in children below age 10. Signs and symptoms of overdose have been reported within 15-20 minutes and death has been reported within one hour of ingestion. If accidental ingestion occurs, seek medical attention immediately (see OVERDOSAGE).PRECAUTIONS Benzonatate is chemically related to anesthetic agents of the para-amino-benzoic acid class (e.g. procaine; tetracaine) and has been associated with adverse CNS effects possibly related to a prior sensitivity to related agents or interaction with concomitant medication.Information for patients:oral mucosa and choking could occur. If numbness or tingling of the tongue, mouth, throat, or face occurs, refrain from oral ingestion of food or liquids until the numbness has resolved. If the symptoms worsen or persist, seek medical attention.Keep TESSALON out of reach of children. Accidental ingestion resulting in death has been reported in children. Signs and symptoms of overdose have been reported within 15-20 minutes and death has been reported within one hour of ingestion. Signs and symptoms may include restlessness, tremors, convulsions, coma and cardiac arrest. If accidental ingestion occurs, seek medical attention immediately.Overdosage resulting in death may occur in adults.Do not exceed a single dose of 200 mg and a total daily dosage of 600 mg. If you miss a dose of TESSALON, skip that dose and take the next dose at the next scheduled time. Do not take 2 doses of TESSALON at one time.Usage in Pregnancy: Pregnancy Category C. Animal reproduction studies have not been conducted with TESSALON. It is also not known whether TESSALON can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. TESSALON should be given to a pregnant woman only if clearly needed.Nursing mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk caution should be exercised when TESSALON is administered to a nursing woman.Carcinogenesis, mutagenesis, impairment of fertility: Carcinogenicity, mutagenicity, and reproduction studies have not been conducted with TESSALON.Pediatric Use: Safety and effectiveness in children below the age of 10 have not been established. Accidental ingestion resulting in death has been reported in children below age 10. Keep out of reach of children.ADVERSE REACTIONSPotential Adverse Reactions to TESSALON may include:Hypersensitivity reactions including bronchospasm, laryngospasm, cardiovascular collapse possibly related to local anesthesia from chewing or sucking the capsule.CNS: sedation; headache; dizziness; mental confusion; visual hallucinations.GI: constipation; nausea; GI upset.Dermatologic: pruritus; skin eruptions.Other: nasal congestion; sensation of burning in the eyes; vague “chilly” sensation; numbness of th e chest; hypersensitivity.Deliberate or accidental overdose has resulted in death, particularly in children.OVERDOSAGEIntentional and unintentional overdose may result in death, particularly in children.The drug is chemically related to tetracaine and other topical anesthetics and shares various aspects of their pharmacology and toxicology. Drugs of this type are generally well absorbed after ingestion.Signs and Symptoms:The signs and symptoms of overdose of benzonatate have been reported within 15-20 minutes. If capsules are chewed or dissolved in the mouth, oropharyngeal anesthesia will develop rapidly, which may cause choking and airway compromise.CNS stimulation may cause restlessness and tremors which may proceed to clonic convulsions followed by profound CNS depression. Convulsions, coma, cerebral edema and cardiac arrest leading to death have been reported within 1 hour of ingestion.Treatment:In case of overdose, seek medical attention immediately. Evacuate gastric contents and administer copious amounts of activated charcoal slurry. Even in the conscious patient, cough and gag reflexes may be so depressed as to necessitate special attention to protection against aspiration of gastric contents and orally administered materials. Convulsions should be treated with a short-acting barbiturate given intravenously and carefully titrated for the smallest effective dosage. Intensive support of respiration and cardiovascular-renal function is an essential feature of the treatment of severe intoxication from overdosage.Do not use CNS stimulants.DOSAGE AND ADMINISTRATIONAdults and Children over 10 years of age: Usual dose is one 100 mg or 200 mg capsule three times a day as needed for cough. If necessary to control cough, up to 600 mg daily in three divided doses may be given. TESSALON should be swallowed whole. TESSALON Capsules and Perles are not to be broken, chewed, dissolved, cut or crushed.HOW SUPPLIEDPerles, 100 mg (yellow);bottles of 100NDC 0069-0122-01 Imprint: T.Perles, 100 mg (yellow);bottles of 500NDC 0069-0122-02 Imprint: TCapsules, 200 mg (yellow);bottles of 100NDC 0069-0124-01 Imprint: 0698.Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature]. Rev. 12/15Mfd byCatalent Pharma SolutionsSt. Petersburg, Florida 33716Pfizer Inc.Madison, New Jersey 07940©2010 Pfizer Inc.。
bendamustine 化学式
bendamustine 化学式
Bendamustine是一种抗肿瘤化合物，其化学式为C16H21Cl2N3O2。
它是一种混合型的DNA损伤剂，可通过破坏DNA双链或单链断裂来杀死癌细胞。
Bendamustine已被广泛用于治疗多种类型的癌症，包括
非霍奇金淋巴瘤、慢性淋巴细胞白血病和多发性骨髓瘤等。
它可以通过静脉注射或口服给药进行使用，并且通常作为化疗方案的一部分使用。
Bendamustine是一种强效的化疗药物，可能会产生一些副作用，如恶心、呕吐、疲劳和骨髓抑制等。
然而，在适当的用药指导下，它可以安全地使用并且对癌症患者的治疗效果非常显著。
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