期刊文献+
共找到416篇文章
< 1 2 21 >
每页显示 20 50 100
Dabigatran etixilate and traumatic brain injury: Evolving anticoagulants require evolving care plans 被引量:3
1
作者 Sam Pakraftar Daniela Atencio +3 位作者 John English Alain Corcos Eric M Altschuler Kurt Stahlfeld 《World Journal of Clinical Cases》 SCIE 2014年第8期362-366,共5页
AIM: To investigate the outcomes of trauma patients with traumatic brain injury(TBI) on Dabigatran Etexilate(DE). METHODS: Following IRB approval, all patients taking DE who were admitted to our level 1 trauma service... AIM: To investigate the outcomes of trauma patients with traumatic brain injury(TBI) on Dabigatran Etexilate(DE). METHODS: Following IRB approval, all patients taking DE who were admitted to our level 1 trauma service were enrolled in the study. Injury complexity, length of stay(LOS), intensive care length of stay, operative intervention, therapeutic interventions and outcomes were analyzed retrospectively. RESULTS: Twenty-eight of 4310 admissions were taking DE. Eleven patients were excluded on concurrent antiplatelet therapy. Average age was 77.14 years(64-94 years), and average LOS was 4.7 d(1-35 d). Thirty-two percent were admitted with intracranial hemorrhage. Eighteen percent received factor Ⅶ, and 22% received dialysis in attempts to correct coagulopathy. Mortality was 21%.CONCLUSION: The low incidence, absence of reversal agents, and lack of practice guidelines makes managing patients with TBI taking DE frustrating and provider specific. Local practice guidelines may be helpful in managing such patients. 展开更多
关键词 dabigatran Brain injury ANTICOAGULATION dabigatran REVERSAL
下载PDF
Association between body mass index and the risk of bleeding in elderly patients with non-valvular atrial fibrillation taking dabigatran:a cohort study 被引量:2
2
作者 Ming-Hui LI Li-Hua HU +7 位作者 Yu-Rong XIONG Yu YU Wei ZHOU Tao WANG Ling-Juan ZHU Xi LIU Hui-Hui BAO Xiao-Shu CHENG 《Journal of Geriatric Cardiology》 SCIE CAS CSCD 2020年第4期193-201,共9页
Background Uncertainty remains regarding the association between body mass index(BMI)and the risk of bleeding in patients with non-valvular atrial fibrillation(NVAF).We aimed to investigate the association between BMI... Background Uncertainty remains regarding the association between body mass index(BMI)and the risk of bleeding in patients with non-valvular atrial fibrillation(NVAF).We aimed to investigate the association between BMI and the risk of bleeding in elderly NVAF patients taking dabigatran.Methods A total of 509 elderly NVAF patients,who were being treated at twelve centers in China from February 2015 to December 2017 and taking dabigatran,were analyzed.The exposure and outcome variables were BMI at baseline and bleeding events within the subsequent six months,respectively.Cox proportional hazards regression analysis was used to evaluate the association between BMI and the risk of bleeding.Moreover,the Cox proportional hazards regression with cubic spline functions and smooth curve fitting was conducted.Results During the six-month follow-up,50 participants experienced bleeding.Every 1 kg/m^2 increase in BMI was associated with a 12%increased risk of bleeding(P=0.021).Compared to those with BMI values in Tertile 1(<22.5 kg/m^2),the adjusted hazard ratio(HR)of bleeding for participants in Tertile 2(22.5–25.3 kg/m^2)and Tertile 3(>25.3 kg/m^2)were 2.71(95%CI:1.02–7.17)and 3.5(95%CI:1.21–8.70),respectively.The Ptrend-value was significant in all models.The adjusted smooth curve showed a linear association between BMI and bleeding.None of the stratified variables showed significant effect modification on the association between BMI and bleeding(Pinteraction>0.05).Conclusions BMI was significantly and positively associated with the risk of bleeding in elderly NVAF patients treated with dabigatran. 展开更多
关键词 ATRIAL FIBRILLATION BLEEDING BODY mass index dabigatran
下载PDF
Dabigatran,rivaroxaban,and apixaban are superior to warfarin in Asian patients with non-valvular atrial fibrillation:An updated metaanalysis 被引量:3
3
作者 Wei-Jia Li Paraschos Archontakis-Barakakis +7 位作者 Leonidas Palaiodimos Dimitrios Kalaitzoglou Lazaros Tzelves Apostolos Manolopoulos Yu-Chiang Wang Stefanos Giannopoulos Robert Faillace Damianos G Kokkinidis 《World Journal of Cardiology》 2021年第4期82-94,共13页
BACKGROUND Most of the randomized clinical trials that led to the wide use of non-vitamin K antagonist oral anticoagulants for stroke prevention in patients with atrial fibrillation(AF)originated from western countrie... BACKGROUND Most of the randomized clinical trials that led to the wide use of non-vitamin K antagonist oral anticoagulants for stroke prevention in patients with atrial fibrillation(AF)originated from western countries.AIM To systematically review and quantitatively synthesize the real-world data regarding the efficacy and safety of dabigatran,rivaroxaban,and apixaban compared to warfarin for stroke prevention in Asian patients with non-valvular AF.METHODS Medline,Cochrane,and ClinicalTrial.gov databases were reviewed.A randomeffect model meta-analysis was used and I-square was utilized to assess the heterogeneity.The primary outcome was ischemic stroke.The secondary outcomes were all-cause mortality,major bleeding,intracranial hemorrhage,and gastrointestinal bleeding.RESULTS Twelve studies from East Asia or Southeast Asia and 441450 patients were included.Dabigatran,rivaroxaban,and apixaban were associated with a significant reduction in the incidence of ischemic stroke[hazard ratio(HR)=0.78,95%confidence interval(CI):0.65-0.94;HR=0.79,95%CI:0.74-0.85,HR=0.70,95%CI:0.62-0.78;respectively],all-cause mortality(HR=0.68,95%CI:0.56-0.83;HR=0.66,95%CI:0.52-0.84;HR=0.66,95%CI:0.49-0.90;respectively),and major bleeding(HR=0.61,95%CI:0.54-0.69;HR=0.70,95%CI:0.54-0.90;HR=0.58,95%CI:0.43-0.78;respectively)compared to warfarin.CONCLUSION Dabigatran,rivaroxaban,and apixaban appear to be superior to warfarin in both efficacy and safety in Asians with non-valvular AF. 展开更多
关键词 Novel oral anticoagulant Direct oral anticoagulant Atrial fibrillation Asian population dabigatran RIVAROXABAN APIXABAN WARFARIN
下载PDF
Dabigatran in cardiovascular disease management:A comprehensive review 被引量:1
4
作者 Ayesha Javed Muhammad Ajmal Aaron Wolfson 《World Journal of Cardiology》 2021年第12期710-719,共10页
Dabigatran,a direct thrombin inhibitor,has robust data for the treatment of deep venous thrombosis and pulmonary embolism,stroke prevention in non-valvular atrial fibrillation,and the prophylaxis of venous thromboembo... Dabigatran,a direct thrombin inhibitor,has robust data for the treatment of deep venous thrombosis and pulmonary embolism,stroke prevention in non-valvular atrial fibrillation,and the prophylaxis of venous thromboembolism(VTE)after knee and hip replacement.Recent studies have evaluated dabigatran to determine its safety and efficacy in such conditions as VTE in malignancy,coronary artery disease,mechanical and bioprosthetic valves,and antiphospholipid syndrome.This article provides a comprehensive review on the role of dabigatran in various cardiovascular diseases. 展开更多
关键词 dabigatran ANTICOAGULATION THROMBUS BLEEDING Atrial fibrillation Deep venous thrombosis Stroke
下载PDF
Dabigatran in the Treatment of Extensive Cerebral Venous Thrombosis:A Case Report 被引量:1
5
作者 Viviane Maria Vedana Luiz Carlos Porcello Marrone +5 位作者 Nathalia Guarienti Missima William Alves Martins Camila Simeoni Luisa Franciscatto Ricardo Bernardi Soder Antonio Carlos Huf Marrone 《World Journal of Neuroscience》 2018年第1期32-37,共6页
Background: Cerebral venous thrombosis (CVT) is a rare type of cerebrovascular disease associated with a 15% rate of death or function dependence. The mainstay of treatment for CVT is systemic anticoagulation, despite... Background: Cerebral venous thrombosis (CVT) is a rare type of cerebrovascular disease associated with a 15% rate of death or function dependence. The mainstay of treatment for CVT is systemic anticoagulation, despite venous hemorrhagic infarction. Vitamin K antagonists have long been the only available option for anticoagulation;however, the past few years have brought the development of many new target-specific drugs, collectively called non-vitamin K antagonist oral anticoagulants (NOACs). Although emerging evidence suggests NOACs have an acceptable safety and tolerability profile in CVT, there are limited data available and no randomized controlled trials have been performed to date. Case Presentation: This describes the case of a patient with CVT occurring during an infection who was successfully treated with a NOAC, dabigatran, after a difficult time on warfarin. Conclusions: A case of extensive and deep CVT was identified. Dabigatran 150 mg treatment twice daily in this patient resulted in no additional damage to the brain. This case study illustrates that the use of NOACs such as dabigatran can be safe and effective in patients with CVT. 展开更多
关键词 Cerebral Venous Thrombosis dabigatran Non-Vitamin K Antagonist Oral Anticoagulant SAFETY
下载PDF
Idarucizumab reverses dabigatran-induced anticoagulation in treatment of gastric bleeding:A case report
6
作者 Yu Jia Shao-Hua Wang +5 位作者 Na-Juan Cui Quan-Xi Liu Wei Wang Xue Li Ya-Mei Gu Yan Zhu 《World Journal of Clinical Cases》 SCIE 2022年第8期2537-2542,共6页
BACKGROUND The drug instructions for dabigatran recommend adjusting the dosage to 110 mg twice daily for patients with bleeding risk,and performing at least one renal function test per year for patients with moderate ... BACKGROUND The drug instructions for dabigatran recommend adjusting the dosage to 110 mg twice daily for patients with bleeding risk,and performing at least one renal function test per year for patients with moderate renal impairment.However,owing to chronic insidiously worsening renal insufficiency,dabigatran can still accumulate abnormally,necessitating therapy with idarucizumab to reverse the anticoagulation due to severe erosive gastritis with widespread stomach mucosal bleeding.CASE SUMMARY A 76-year-old woman with a history of atrial fibrillation who took dabigatran 110 mg twice daily as directed to lessen the chance of stroke,was transported to the hospital with hematemesis and melena.Laboratory findings revealed severe lifethreatening,blood-loss-induced anemia with a hemoglobin(Hb)level of 41.0 g/L and marked coagulation abnormalities with thrombin time(TT)>180 s,most likely caused by dabigatran-induced metabolic disorder.Aggressive acid suppressive,hemostatic,and blood transfusion therapy resulted in the misconception that the bleeding was controlled,with subsequent rebleeding.Idarucizumab was administered in a timely manner to counteract dabigatran’s anticoagulant impact,and 12 h later,TT was determined to be 17.4 s,which was within the normal range.Finally,the patient had no active bleeding signs and laboratory findings showed an Hb level of 104 g/L and TT of 17.7 s.CONCLUSION Renal function,coagulation function,and dabigatran concentration should be regularly monitored in older patients.Proton pump inhibitor and dabigatran coadministration is still controversial in preventing upper gastrointestinal tract bleeding. 展开更多
关键词 Idarucizumab dabigatran Gastric bleeding Atrial fibrillation Case report
下载PDF
Major bleeding events in octagenarians associated with drug interactions between dabigatran and P-gp inhibitors
7
作者 Marjorie Bernier Sarah-Line Lancrerot +5 位作者 Fanny Rocher Elise K Van-Obberghen Pierre Olivier Thibaud Lavrut Nadège Parassol-Girard Milou-Daniel Drici 《Journal of Geriatric Cardiology》 SCIE CAS CSCD 2019年第11期806-811,共6页
Background The direct oral anticoagulant dabigatran does not require any routine therapeutic drug monitoring.Yet,concerns about possible drug interactions susceptible to increase its inherent bleeding risk,especially ... Background The direct oral anticoagulant dabigatran does not require any routine therapeutic drug monitoring.Yet,concerns about possible drug interactions susceptible to increase its inherent bleeding risk,especially in very elderly patients,have been raised recently.The aim of our study was to evaluate to what extent the co-prescription of P-gp inhibitors with dabigatran may increase its plasma levels and lead to bleeding complications,in usual conditions of care of the very elderly.Methods Fifty-eight patients over 85 years old with non valvular atrial fibrillation receiving dabigatran were included in a prospective cohort.Prescriptions were screened for the presence of P-gp inhibitors(Group A)or not(Group B).Results Patients from Group A had increased dabigatran mean plasma concentrations as compared with patients from Group B(A vs.B:182.2±147.3 vs.93.7±64.9 ng/m L).One third of the patients from Group A had dabigatran concentrations that were deemed"out of range"versus none in Group B(P=0.05).This was associated with more frequent bleeding complications in Group A(A:30.4%,B:8.6%,P=0.04).Conclusion In our cohort of very elderly patients,at least,the co-prescription of dabigatran with P-gp inhibitors in usual conditions of care resulted in higher dabigatran plasma concentrations and more frequent bleeding occurrences. 展开更多
关键词 dabigatran Drug interaction HEMORRHAGE P-gp inhibitors The elderly
下载PDF
QbD Approach Method Development for Estimation of Dabigatran Etexilate along with Its Impurities and Identification of Degradants in Capsule Dosage Form
8
作者 Hanimi Reddy Bapatu Ravi Kumar Maram +1 位作者 Woo Hyung Cho Venkat Bhaskar Rao Pasagadugula 《American Journal of Analytical Chemistry》 2016年第6期494-524,共31页
The concept of Quality by Design was demonstrated in the development of a stability-indicating assay and related substances method by HPLC for Dabigatran Etexilate Capsules dosage form. Method design, method evaluatio... The concept of Quality by Design was demonstrated in the development of a stability-indicating assay and related substances method by HPLC for Dabigatran Etexilate Capsules dosage form. Method design, method evaluation, method control and life cycle management were explained by systematic flow chart. Analytical Target Product profile was defined. The method was developed using the Inertsil ODS-3V, 150 mm × 4.6 mm, 5 μm column using the gradient program with ammonium formate buffer as mobile phase A and acetonitrile as mobile phase B. Risk assessment was performed as part of method evaluation. Design of experiment tools was used to optimize the chromatographic conditions. A two-level Full Factorial Design along with Face Centered Central Composite design augmentation was employed and statistical analysis of the experimental data uncovered the significant influential of chromatographic factors. The design space and the contour plot suggest that the current center point parameters can be further modified, resulting in better acceptability of the response parameters. The performance of the optimized method was validated according to current ICH guidelines. Dabigatran Etexilate Capsules was subjected to various stress conditions like oxidative, acid, base, hydrolytic, thermal, humidity, and photolytic degradations and evaluated chromatograms at 220 nm. The degradation products were well separated from each other and main peak, demonstrating the stability-indicating power of the method. One of the major degradant impurities, which are forming in neutral hydrolysis stress condition, is isolated and characterized by using analytical techniques like IR, LC-MS and NMR. Degradation pathway for Dabigatran Etexilate was proposed based on forced degradation data along with reaction mechanism. 展开更多
关键词 Quality by Design Design of Experiment dabigatran Etexilate Degradant Impurities
下载PDF
新型抗凝药Dabigatran或将成为华法林替代品用于治疗静脉血栓栓塞
9
《药学进展》 CAS 2010年第4期189-190,共2页
关键词 dabigatran 华法林 直接凝血酶抑制剂 静脉血栓栓塞
下载PDF
Traumatic fatal cerebral hemorrhage in an old patient with a history of multiple sclerosis under dabigatran: a case report and review of the literature 被引量:4
10
作者 Claudia Stollberger Andreas Ulram Adam Bastovansky Josef Finsterer 《Journal of Geriatric Cardiology》 SCIE CAS CSCD 2015年第1期83-87,共5页
直接抗凝剂药的一劣势是一粒解毒药的缺乏,它可以与创伤的大脑损害在病人变得相关。尽管有周期性的下降,有 atrial 纤维性颤动和中略的一个 77 年的老人收到了 dabigatran。由于 ground-level-fall,他与中线移动受不了 subarachnoid... 直接抗凝剂药的一劣势是一粒解毒药的缺乏,它可以与创伤的大脑损害在病人变得相关。尽管有周期性的下降,有 atrial 纤维性颤动和中略的一个 77 年的老人收到了 dabigatran。由于 ground-level-fall,他与中线移动受不了 subarachnoidal 和 intraparenchymal 出血, subdural hematoma 和大脑浮肿。没有重获知觉,尽管有 osteoclastic 环锯术和 hematoma 撤退,他七天以后仍然保持无知觉、死。最可能,减少了由于增加的年龄,力量贡献了的 dabigatran 清理致命的功课。我们与 unexplained 下降在病人建议抑制抗凝剂治疗。如果抗凝剂治疗被认为必要,有他们为实验室监视和抗凝剂活动的颠倒的潜力的 vitamin-K-antagonists 应该被比较喜欢。 展开更多
关键词 脑出血 加群 致死性 创伤性 蛛网膜下腔 抗凝活性 审查 案件
下载PDF
Safety of Dabigatran in Patients with Non-valvular Atrial Fibrillation: A Short-Term Registry
11
作者 Ahmad Al-Meman Nawaf Abdulrahman Almutairi 《Journal of Pharmacy and Pharmacology》 2014年第9期565-569,共5页
关键词 药剂学 药理学 药学 药物分析 药典
下载PDF
Association of ABCB1 gene polymorphisms rs1128503, rs2032582, rs4148738 with anemia in patients receiving dabigatran after total knee arthroplasty
12
作者 Alina Kasimova Dmitry Labutin +1 位作者 Anton Gvozdetsky Svetlana Bozhkova 《Chinese Journal of Traumatology》 CAS CSCD 2024年第1期27-33,共7页
Purpose:Dabigatran is usually prescribed in recommended doses without monitoring of the blood coagulation for the prevention of venous thromboembolism after joint arthroplasty.ABCB1 is a key gene in the metabolism of ... Purpose:Dabigatran is usually prescribed in recommended doses without monitoring of the blood coagulation for the prevention of venous thromboembolism after joint arthroplasty.ABCB1 is a key gene in the metabolism of dabigatran etexilate.Its allele variants are likely to play a pivotal role in the occurrence of hemorrhagic complications.Methods:The prospective study included 127 patients with primary knee osteoarthritis undergoing total knee arthroplasty.Patients with anemia and coagulation disorders,elevated transaminase and creatinine levels as well as already receiving anticoagulant and antiplatelet therapy were excluded from the study.The association of ABCB1 gene polymorphisms rs1128503,rs2032582,rs4148738 with anemia as the outcome of dabigatran therapy was evaluated by single-nucleotide polymorphism analysis with a realtime polymerase chain reaction assay and laboratory blood tests.The beta regression model was used to predict the effect of polymorphisms on the studied laboratory markers.The probability of the type 1 error(p)was less than 0.05 was considered statistically significant.BenjaminiHochberg was used to correct for significance levels in multiple hypothesis tests.All calculations were performed using Rprogramming language v3.6.3.Results:For all polymorphisms there was no association with the level of platelets,protein,creatinine,alanine transaminase,prothrombin,international normalized ratio,activated partial thromboplastin time and fibrinogen.Carriers of rs1128503(TT)had a significant decrease of hematocrit(p=0.001),red blood count and hemoglobin(p=0.015)while receiving dabigatran therapy during the postoperative period compared to the CC,CT.Carriers of rs2032582(TT)had a significant decrease of hematocrit(p=0.001),red blood count and hemoglobin(p=0.006)while receiving dabigatran therapy during the postoperative period compared to the GG,GT phenotypes.These differences were not observed in carriers of rs4148738.Conclusion:It might be necessary to reconsider thromboprophylaxis with dabigatran in carriers of rs1128503(TT)or rs2032582(TT)polymorphisms in favor of other new oral anticoagulants.The longterm implication of these findings would be the reduction of bleeding complications after total joint arthroplasty. 展开更多
关键词 THROMBOPROPHYLAXIS P-GLYCOPROTEIN dabigatran ANEMIA SNPs
原文传递
基于《中国医疗机构药品评价与遴选快速指南(第二版)》的口服抗凝药物临床综合评价
13
作者 田冬冬 曹格溪 +3 位作者 薛朝军 董占军 刘建平 赵志刚 《医药导报》 北大核心 2024年第2期274-282,共9页
目的基于《中国医疗机构药品评价与遴选快速指南(第二版)》,对口服抗凝药物(OACs)进行综合评价,以期为医疗机构药品遴选、临床用药决策提供参考。方法收集评价证据,从临床属性(有效性和安全性)、药学特性、经济性及其他属性4个维度对纳... 目的基于《中国医疗机构药品评价与遴选快速指南(第二版)》,对口服抗凝药物(OACs)进行综合评价,以期为医疗机构药品遴选、临床用药决策提供参考。方法收集评价证据,从临床属性(有效性和安全性)、药学特性、经济性及其他属性4个维度对纳入的药品赋分与评价。结果所有纳入评价的OACs综合评分均在70分以上,华法林综合评分最高。临床属性和药学特性是药品遴选评价的核心属性,当仅评估临床属性和药学特性时,评分最高的药品是艾多沙班。结论OACs是长期抗凝治疗患者的首选药物,不同OACs在临床治疗中有不同的优势。通过《指南(第二版)》对OACs进行遴选评价,可为医疗机构药品遴选与科学、合理、安全用药提供依据。 展开更多
关键词 口服抗凝药物 华法林 达比加群酯 利伐沙班 艾多沙班 阿哌沙班 遴选评价 数字化评分
下载PDF
Individualized anti-thrombotic therapy for acute myocardial infarction complicated with left ventricular thrombus: A case report
14
作者 Yan Song Hua Li +5 位作者 Xia Zhang Lei Wang Hong-Yan Xu Zhi-Chao Lu Xiao-Gang Wang Bo Liu 《World Journal of Clinical Cases》 SCIE 2024年第4期835-841,共7页
BACKGROUND Presently,there is no established standard anti-blood clot therapy for patients facing acute myocardial infarction(AMI)complicated by left ventricular thrombus(LVT).While vitamin K antagonists are the prefe... BACKGROUND Presently,there is no established standard anti-blood clot therapy for patients facing acute myocardial infarction(AMI)complicated by left ventricular thrombus(LVT).While vitamin K antagonists are the preferred choice for oral blood thinning,determining the best course of blood-thinning medication remains challenging.It is unclear if non-vitamin K antagonist oral blood thinners have different effectiveness in treating LVT.This study significantly contributes to the medical community.CASE SUMMARY The blood-thinning treatment of a patient with AMI and LVT was analyzed.Triple blood-thinning therapy included daily enteric-coated aspirin tablets at 0.1 g,daily clopidogrel hydrogen sulfate at 75 mg,and dabigatran etexilate at 110 mg twice daily.After 15 d,the patient’s LVT did not decrease but instead increased.Clinical pharmacists comprehensively analyzed the cases from the perspective of the patient’s disease status and drug interaction.The drug regimen was reformulated for the patient,replacing dabigatran etexilate with warfarin,and was administered for six months.The clinical pharmacist provided the patient with professional and standardized pharmaceutical services.The patient’s condition was discharged after meeting the international normalized ratio value(2-3)criteria.The patient fully complied with the follow-up,and the time in the therapeutic range was 78.57%,with no serious adverse effects during pharmaceutical monitoring.CONCLUSION Warfarin proves to be an effective drug for patients with AMI complicated by LVT,and its blood-thinning course lasts for six months. 展开更多
关键词 Myocardial infarction Left ventricular thrombus dabigatran etexilate WARFARIN Clinical pharmacist Case report
下载PDF
新型口服抗凝药dabigatran etexilate
15
作者 黄赛杰 徐佳骏 《中国新药杂志》 CAS CSCD 北大核心 2009年第17期1587-1589,1596,共4页
Dabigatran etexilate是一种新型口服抗凝药物,通过直接抑制凝血酶起到抗凝作用。该药在预防静脉血栓栓塞症(venous thromboem bolism,VTE)中已完成Ⅲ期临床试验,治疗急性VTE和心房颤动(atrial fibrillation,AF)的预防正在进行Ⅲ期临床... Dabigatran etexilate是一种新型口服抗凝药物,通过直接抑制凝血酶起到抗凝作用。该药在预防静脉血栓栓塞症(venous thromboem bolism,VTE)中已完成Ⅲ期临床试验,治疗急性VTE和心房颤动(atrial fibrillation,AF)的预防正在进行Ⅲ期临床试验。2008年3月,欧盟已批准其在欧盟27个成员国上市。现对其作用机制、药动学、药效学、临床应用及安全性等做一简要介绍。 展开更多
关键词 dabigatranet exilate 药动学 药效学 安全性
原文传递
达比加群酯-d_(3)的合成 被引量:1
16
作者 王昌 梁林辉 +2 位作者 姚永秀 梁大伟 董金华 《化学试剂》 CAS 2024年第1期105-110,共6页
研究抗凝血药物达比加群酯-d_(3)的合成工艺。以4-氯-3-硝基苯甲酸甲酯为起始原料,氘代甲胺盐酸盐为氘代试剂,经氘代甲基化、取代、还原、缩合、环合、水解、亲核等反应得到关键氘化中间体3-{[(2-{[(4-氰基苯基)氨基]甲基}-1-(甲基-d_(... 研究抗凝血药物达比加群酯-d_(3)的合成工艺。以4-氯-3-硝基苯甲酸甲酯为起始原料,氘代甲胺盐酸盐为氘代试剂,经氘代甲基化、取代、还原、缩合、环合、水解、亲核等反应得到关键氘化中间体3-{[(2-{[(4-氰基苯基)氨基]甲基}-1-(甲基-d_(3))苯并咪唑-5-基)氧亚基](吡啶-2-基)氨基}丙酸乙酯,而后再经氨解和亲核反应,成功制备稳定的达比加群酯-d_(3),8步反应总产率为6.4%,目标化合物结构经NMR和MS确认,同位素丰度达99.7%。该合成方法原料简单易得、操作简便、重现性好,可用于达比加群酯-d_(3)的合成。 展开更多
关键词 抗凝血药物 达比加群酯-d_(3) 合成工艺 优化 同位素标记
下载PDF
达比加群抗凝机理的光谱研究
17
作者 龚梦洁 海滢 +2 位作者 吕凯文 顾洪斌 祖莉莉 《光谱学与光谱分析》 SCIE EI CAS CSCD 北大核心 2024年第3期699-706,共8页
达比加群酯(DE)是一种新型口服抗凝药,用于预防非瓣膜性房颤患者的卒中和全身性血管栓塞。达比加群酯本身没有药理活性,其活性成分是在血浆和肝脏中经酯酶催化水解生成的达比加群(DAB)。尽管已经被用于临床治疗,活性成分达比加群的极性... 达比加群酯(DE)是一种新型口服抗凝药,用于预防非瓣膜性房颤患者的卒中和全身性血管栓塞。达比加群酯本身没有药理活性,其活性成分是在血浆和肝脏中经酯酶催化水解生成的达比加群(DAB)。尽管已经被用于临床治疗,活性成分达比加群的极性基团苯甲脒和羧基在其与凝血酶(Thr)结合时的作用机理仍不清晰,并且目前还未找到针对达比加群的特定逆转剂。采用稳态和瞬态荧光光谱、分子对接模拟等方法研究了DAB与凝血酶在模拟生理条件下的相互作用。通过研究极性基团酯化前后DAB与凝血酶作用时的时间分辨荧光光谱,揭示了DAB对凝血酶的荧光猝灭包含动态猝灭和静态猝灭的双重机制,指出DAB苯甲脒基团与凝血酶之间的静电导向效应是DAB与凝血酶快速有效形成复合物的关键动力学因素。运用分子对接模拟方法研究了DAB与凝血酶相互作用时的分子构象,探究DAB极性基团的酯化对两者结合能的影响。通过比较DAB双极性基团酯化后的达比加群酯(DE)、 DAB羧酸基团酯化后的达比加群乙酯(DAE)、以及DAB苯甲醚基团酯化后的达比加群己酯(DAH)与凝血酶相互作用的荧光光谱和分子对接模拟结果,进一步验证了极性基团在DAB与凝血酶结合时的重要作用。获得了DAB和DE与牛血清白蛋白(BSA)在生理pH条件下相互作用的稳态和瞬态荧光光谱的对照结果,提出DAB的极性基团在其与凝血酶的选择性结合中发挥重要作用。研究结果为提高达比加群药物生理活性以及逆转剂的研究提供了理论和实验依据。 展开更多
关键词 达比加群 抗凝机理 荧光光谱 静电导向效应
下载PDF
老年非瓣膜性心房颤动患者临床应用达比加群酯的疗效分析
18
作者 赵思佳 胡瑶瑶 +1 位作者 朱业 刘佳 《实用临床医药杂志》 CAS 2024年第3期29-33,38,共6页
目的 调查老年非瓣膜性房颤患者达比加群酯的临床应用情况。方法 收集扬州大学附属苏北人民医院2021年1月—2022年6月心内科使用达比加群酯的老年非瓣膜性房颤患者的信息,根据相关指南对临床应用、实验室指标、临床结局等情况进行统计... 目的 调查老年非瓣膜性房颤患者达比加群酯的临床应用情况。方法 收集扬州大学附属苏北人民医院2021年1月—2022年6月心内科使用达比加群酯的老年非瓣膜性房颤患者的信息,根据相关指南对临床应用、实验室指标、临床结局等情况进行统计分析。结果 150例患者中,无适应证用药14例,禁忌证12例;给药剂量不足93例,给药剂量过大9例,给药频次不合理13例,与其他抗凝药物转换不合理20例。实验室指标显示,服药1、3、6个月后活化部分凝血酶原时间(APTT)升高,差异有统计学意义(P<0.05)。临床结局显示,缺血性卒中事件发生率为3.33%(4/120),大出血发生率为1.67%(2/120),脑出血事件发生率为0.83%(1/120)。结论 本院达比加群酯的临床应用以给药剂量不足最为常见。药师应注重老年患者达比加群酯的规范应用。 展开更多
关键词 达比加群酯 非瓣膜性心房颤动 老年患者 合理用药 抗凝治疗 不良反应
下载PDF
心房颤动射频消融术后口服利伐沙班、达比加群酯、华法林预防脑卒中的价值
19
作者 孙西振 蒋培培 王高峰 《中国医药导报》 CAS 2024年第8期94-98,共5页
目的 探讨心房颤动射频消融术后口服利伐沙班、达比加群酯、华法林预防脑卒中的价值。方法 选择2020年1月至2022年10月在安徽省阜阳市人民医院接受治疗的120例心房颤动患者,采用随机数字表法将其分为三组,各40例。利伐沙班组(口服利伐沙... 目的 探讨心房颤动射频消融术后口服利伐沙班、达比加群酯、华法林预防脑卒中的价值。方法 选择2020年1月至2022年10月在安徽省阜阳市人民医院接受治疗的120例心房颤动患者,采用随机数字表法将其分为三组,各40例。利伐沙班组(口服利伐沙班,15 mg/次,1次/d)、达比加群酯组(口服达比加群酯,110 mg/次,2次/d)及华法林组[口服华法林,起始剂量2.5 mg/次,1次/d,依据国际标准化比率(INR)目标值2.0~3.0,华法林每次用量可增减0.625 mg],三组均治疗3个月。治疗3个月后比较三组凝血功能、超敏C反应蛋白(hs-CRP)、同型半胱氨酸(Hcy)水平及不良反应发生率,随访6个月比较三组血栓及出血事件发生率。结果 治疗后三组INR、凝血酶原时间(PT)、活化部分凝血活酶时间(APTT)均高于治疗前,且利伐沙班组和达比加群酯组INR、PT、APTT低于华法林组(P<0.05)。治疗后三组hs-CRP、Hcy水平均较治疗前降低,且利伐沙班组和达比加群酯组hs-CRP、Hcy水平低于华法林组(P<0.05);三组血栓和不良反应总发生率比较,差异无统计学意义(P>0.05)。达比加群酯组轻微出血发生率低于华法林组(P<0.05)。结论 利伐沙班、达比加群酯、华法林三种药物均可有效预防心房颤动射频消融术后脑卒中的发生,但利伐沙班与达比加群酯更有利于降低出血风险,改善凝血功能,调节hs-CRP、Hcy水平,临床应用价值更高。 展开更多
关键词 利伐沙班 达比加群酯 华法林 心房颤动 射频消融术 脑卒中
下载PDF
达比加群辅助手术治疗肥厚型心肌病合并心房颤动的应用效果
20
作者 秦丽 张海涛 《华夏医学》 CAS 2024年第1期89-94,共6页
目的观察达比加群辅助手术治疗肥厚型心肌病(HCM)合并心房颤动(AF)的临床效果。方法选取121例HCM合并AF患者,按照随机数字表法分为对照组和观察组。两组均行射频消融术治疗,对照组60例,采用常规抗凝辅助手术治疗,观察组61例,采用达比加... 目的观察达比加群辅助手术治疗肥厚型心肌病(HCM)合并心房颤动(AF)的临床效果。方法选取121例HCM合并AF患者,按照随机数字表法分为对照组和观察组。两组均行射频消融术治疗,对照组60例,采用常规抗凝辅助手术治疗,观察组61例,采用达比加群辅助手术治疗,比较两组治疗前后的血小板活性、凝血功能变化情况,随访期间的心血管不良事件及不良反应发生情况。结果治疗后,观察组的β-TG、颗粒膜蛋白CD62P、CD63均低于对照组,活化部分凝血活酶时间(APTT)、凝血酶原时间(PT)、凝血酶时间(TT)均高于对照组,差异有统计学意义(P<0.05)。随访期间,观察组心血管不良事件发生率、不良反应发生率均低于对照组(P<0.05)。结论达比加群辅助射频消融术治疗能有效抑制HCM合并AF患者的血小板活性并改善凝血功能,对降低心血管不良事件及药物的不良反应均有积极意义。 展开更多
关键词 达比加群 肥厚型心肌病 心房颤动 抗凝治疗
下载PDF
上一页 1 2 21 下一页 到第
使用帮助 返回顶部