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Eptifibatide的固相合成及分离纯化 被引量:3
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作者 熊瑛 王宇 陈亮 《厦门大学学报(自然科学版)》 CAS CSCD 北大核心 2007年第1期100-103,共4页
Eptifibatide是一种血小板糖蛋白GPⅡb/Ⅲa受体拮抗剂,临床研究结果显示其医用上的产业前景良好.采用Rink-Am-Resin树脂作为固相载体,Fmoc为保护策略固相合成了Eptifibatide.以DMF为反应溶剂,Piperidine-DMF脱去Fmoc保护基团,以TBTU/HOB... Eptifibatide是一种血小板糖蛋白GPⅡb/Ⅲa受体拮抗剂,临床研究结果显示其医用上的产业前景良好.采用Rink-Am-Resin树脂作为固相载体,Fmoc为保护策略固相合成了Eptifibatide.以DMF为反应溶剂,Piperidine-DMF脱去Fmoc保护基团,以TBTU/HOBt/DIEA作为肽键缩合试剂进行接肽反应,用TFA/EDT/TIS/H2O定量地从树脂上切除,制备型高效液相色谱分离纯化粗肽.同时对产品进行色谱分析和质谱鉴定.实验结果表明Fmoc合成策略中各步的缩合率均在95%以上,多数在99%以上.粗肽纯度为86.8%,产率为55%.分离纯化后的产物纯度达到98.5%,MOLDI-TOF质谱测得的m/z与理论值相符.为化学合成Eptifibatide及其分离纯化提供了一条切实可行的路线. 展开更多
关键词 eptifibatide 固相合成 Fmoc法
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Comparison of efficacy and safety of native eptifibatide vs. tirofiban in patients with acute coronary syndrome undergoing percutaneous coronary intervention 被引量:1
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作者 Jianjin Tang Liansheng Wang Hui Wang Mingwei Wang Kejiang Cao Zhijian Yang 《Journal of Nanjing Medical University》 2008年第4期238-242,共5页
To compare clinical outcomes and safety of eptifibatide or tirofiban in patients with acute coronary syndrome(ACS) undergoing percutaneous coronary intervention(PCI). Methods:Thirty-six patients with ACS(unstabl... To compare clinical outcomes and safety of eptifibatide or tirofiban in patients with acute coronary syndrome(ACS) undergoing percutaneous coronary intervention(PCI). Methods:Thirty-six patients with ACS(unstable angina/non-ST-segment elevation myocardial infarction, UA/NSTEMI) who underwent PCI were randomly divided into two groups to receive eptifibatide or tirofiban treatment. Eptifibatide or tirofiban was predominantly initiated in the catheter laboratory before the intervention. In-hospital and 30-day MACE outcomes; bleeding as well as platelet counting were investigated in those two groups. Results:No in-hospital and 30-day MACE event occurred in the two groups. The number of ischemia leads after treatment reduced compared to that before PCI in the two groups. There was improvement in the number of ischemia leads for 24 h after administration in the tirofiban group than those in eptifibatide group(4.21 ± 2.46 vs. 3.89 ± 3.31, P =0.03). The two groups showed no incidence of massive bleeding. Minor bleeding rates were 16.7% and 22.2% in the two groups respectively. Conclusion:Eptifibatide as an adjunct to PCI may further decrease the incidence of ischemia event in patients with ACS and improve the safety, but its long-term efficacy and side effects need further observation. 展开更多
关键词 acute coronary syndrome percutaneous coronary intervention glycoprotein(GP Ⅱb/Ⅲ a) antagonist eptifibatide tirofiban
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抗血小板药 Eptifibatide 被引量:1
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作者 叶金朝 《国外医药(合成药.生化药.制剂分册)》 1999年第4期218-219,共2页
关键词 抗血小板药 eptifibatide 药理 适应证
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Eptifibatide Induced Severe Thrombocytopenia in an Asymptomatic Patient
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作者 M. Adnan Raufi Ayesha S. Baig +2 位作者 Rama Siddiqui Nouman Akbar Shakaib Jaffery 《Journal of Pharmacy and Pharmacology》 2017年第7期447-450,共4页
GP (glycoprotein) lib/Ilia inhibitors are routinely used in patients with acute coronary syndromes. There have been reported platelet counts of below 20 × 10^9/L within hours of administering the drug. We prese... GP (glycoprotein) lib/Ilia inhibitors are routinely used in patients with acute coronary syndromes. There have been reported platelet counts of below 20 × 10^9/L within hours of administering the drug. We present a case of a 44 years old man with inferior wall myocardial infarction and third-degree heart block who was admitted for cardiac catheterization. The patient successfully underwent percutaneous intervention to right coronary artery and eptifibatide was given per protocol. 6 h post-eptifibatide initiation, platelets dropped from 288 × 10^9/L to 24× 10^9/L. Eptifibatide was stopped and a CBC (complete blood count) was repeated after 2 hours. The platelets had further dropped to undetectable levels showing 0× 10^9/L. The patient remained completely asymptomatic. Pseudo-thrombocytopenia was ruled out on peripheral smear. Platelet transfusion was considered, however, platelets started to rise few hours after stopping of Eptifibatide. Twelve hours later, platelet count reached 4 × 10^9/L. It continued to show a positive trend and reached up to a level of 293× 10^9/L after 5 days. Patient was discharged in a stable condition. Due to this rare but significant phenomenon, patients on these drugs should have their platelet count closely monitored. It is also very rare not to have any symptoms after such critically low platelet levels. 展开更多
关键词 Platelet count asymptomatic thrombocytopenia eptifibatide.
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Effects of two different glycoprotein platelet Ⅱb/Ⅲa inhibitors and the clinical endpoints in patients with intracranial Pipeline flow diverter implant 被引量:6
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作者 Qiao Deng Shichao Zhang +2 位作者 Mingzhou Li Guozhong Zhang Wenfeng Feng 《Journal of Interventional Medicine》 2020年第4期174-179,共6页
Objective:To compare the antiplatelet effect and major adverse cerebrovascular events of Pipeline for intracranial aneurysms using glycoproteinⅡb/Ⅲa antagonists(GPI)eptifibatide and tirofiban.Methods:Retrospective a... Objective:To compare the antiplatelet effect and major adverse cerebrovascular events of Pipeline for intracranial aneurysms using glycoproteinⅡb/Ⅲa antagonists(GPI)eptifibatide and tirofiban.Methods:Retrospective analysis of relevant data of patients using GPIs combined with oral antiplatelet therapy in Nanfang Hospital of Southern Medical University from December 2017 to December 2019.The study was approved by the ethics Committee of Nanfang Hospital of Southern Medical University.According to the random use of GPIs drugs,they were assigned to the eptifibatide group and tirofiban group.Basic data,platelet inhibition rates at baseline,24 h and 72 h after administration,short-term major adverse cerebrovascular events,and bleeding complications were compared between the two groups.Results:A total of 47 patients were included in this study,including 24 patients in eptifibatide group and 23 patients in tirofiban group.There was no significant difference in average age(53.75 vs.53.91 years)and body mass index(BMI)(24.39 vs.22.73 kg/m2)between eptifibatide group and tirofiban group.There was no significant difference in coagulation factor function(R),fibrinogen function(K),fibrinolysis function(EPL),comprehensive coagulation index(Cl),arachidonic acid pathway inhibition rate(AA%)and adenosine diphosphate inhibition rate(ADP%).However,the baseline level of residual platelet function MA(ADP)in eptifibatide group was significantly higher than that in tirofiban group(50.79 vs.35.29 mm,P=0.0026).There was a statistical difference in the platelet aggregation function MA(65.38 vs.62.54 mm,p=0.0442),the rate of spontaneous hemorrhagic stroke(4.3%vs.0%)and the rate of asymptomatic minor bleeding(26.08%vs.4.1%)in the two groups(P<0.05).Conclusion:Both eptifibatide and tirofiban can effectively inhibit platelets,but the effect of etifeptide is better than that of tirofiban in preventing intracranial microhemorrhage and asymptomatic cerebral infarction. 展开更多
关键词 eptifibatide Tirofiban Cerebral hemorrhage Flow guiding device
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血小板糖蛋白Ⅱb/Ⅲa受体抑制剂在急性冠状动脉综合征中的应用
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作者 徐立宏 徐巧玲 《中国临床保健杂志》 CAS 2006年第3期285-288,共4页
关键词 Ⅱb/Ⅲa受体抑制剂 急性冠状动脉综合征 血小板糖蛋白 GPⅡb/Ⅲa受体 eptifibatide ABCIXIMAB tirofiban 糖蛋白Ⅱb/Ⅲ 血小板膜 纤维蛋白原
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急性缺血性卒中重组组织型纤溶酶原激活物加依替巴肽与单用重组组织型纤溶酶原激活物的比较——倾向得分匹配的事后分析
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作者 李宏建 《国际脑血管病杂志》 2015年第5期400-400,共1页
依替巴肽与重组组织型纤溶酶原激活剂(recombinant tissue type plasminogen activator, rtPA)联合溶栓治疗急性缺血性卒中(acute ischemic stroke, AIS)增强方案试验(Combined Approach to Lysis Utilizing Eptifibatide and rtPA... 依替巴肽与重组组织型纤溶酶原激活剂(recombinant tissue type plasminogen activator, rtPA)联合溶栓治疗急性缺血性卒中(acute ischemic stroke, AIS)增强方案试验(Combined Approach to Lysis Utilizing Eptifibatide and rtPA in AIS-Enhanced Regimen, CLEAR-ER)证实了rtPA加依替巴肽在AIS患者中的安全性,该研究将AIS患者按5∶1比例随机分组接受0.6 mg/kg rtPA加依替巴肽或标准rtPA(0.9 mg/kg )溶栓治疗。卒中介入治疗试验(Interventional Management of Stroke, IMS)-Ⅲ是将AIS患者随机分组接受rtPA加血管内治疗或标准rtPA溶栓治疗。白蛋白治疗急性卒中试验-2(Albumin in Acute Stroke Part 2)则是将患者随机分组接受白蛋白±rtPA或生理盐水±rtPA治疗。美国辛辛那提大学神经科学研究所的Adeoye等进行了一项研究,旨在对CLEAR-ER试验联合治疗组患者的转归与后2项试验中倾向得分匹配且仅接受rtPA溶栓治疗的受试者进行比较。 展开更多
关键词 重组组织型纤溶酶原激活物 急性缺血性卒中 依替巴肽 重组组织型纤溶酶原激活剂 eptifibatide PLASMINOGEN 匹配 activator
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