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Svetha Chunduri Jon E. Folstad Tushar J. Vachharajani 《Hemodialysis international. International Symposium on Home Hemodialysis》2017,21(4):453-471
The delicate balance of risk vs. benefit of using antiplatelet and antithrombotic agents in the general population is well established. The decision to use these agents in the end stage renal disease (ESRD) population remains complex and difficult. The concomitant association of a prothombotic state with high risk of bleeding in the ESRD population requires individualization and careful clinical judgment before implementing such therapy. There remains a paucity of clinical trials and lack of substantial evidence in literature for safe and effective use of antithrombotic drugs in patients with advanced chronic kidney disease. The current review summarizes the pros and cons of using antiplatelet and antithrombotic agents in primary and secondary prevention of cardiovascular events, evaluate the risks with routine use of anticoagulation for cerebrovascular stroke prevention with nonvalvular atrial fibrillation and role of newer oral anticoagulants as alternate agents in the dialysis population. 相似文献
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Bernice Wright Marcus J. Tindall Julie A. Lovegrove Jonathan M. Gibbins 《Journal of food science》2013,78(12):N1921-N1928
Epidemiological and clinical trials reveal compelling evidence for the ability of dietary flavonoids to lower cardiovascular disease risk. The mechanisms of action of these polyphenolic compounds are diverse, and of particular interest is their ability to function as protein and lipid kinase inhibitors. We have previously described structure–activity studies that reinforce the possibility for using flavonoid structures as templates for drug design. In the present study, we aim to begin constructing rational screening strategies for exploiting these compounds as templates for the design of clinically relevant, antiplatelet agents. We used the platelet as a model system to dissect the structural influence of flavonoids, stilbenes, anthocyanidins, and phenolic acids on inhibition of cell signaling and function. Functional groups identified as relevant for potent inhibition of platelet function included at least 2 benzene rings, a hydroxylated B ring, a planar C ring, a C ring ketone group, and a C‐2 positioned B ring. Hydroxylation of the B ring with either a catechol group or a single C‐4′ hydroxyl may be required for efficient inhibition of collagen‐stimulated tyrosine phosphorylated proteins of 125 to 130 kDa, but may not be necessary for that of phosphotyrosine proteins at approximately 29 kDa. The removal of the C ring C‐3 hydroxyl together with a hydroxylated B ring (apigenin) may confer selectivity for 37 to 38 kDa phosphotyrosine proteins. We conclude that this study may form the basis for construction of maps of flavonoid inhibitory activity on kinase targets that may allow a multitargeted therapeutic approach with analogue counterparts and parent compounds. 相似文献
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Hla Nu Swe Boonchoo Sritularak Ponlapat Rojnuckarin Rataya Luechapudiporn 《International journal of molecular sciences》2021,22(13)
Lusianthridin is a phenanthrene derivative isolated from Dendrobium venustum. Some phenanthrene compounds have antiplatelet aggregation activities via undefined pathways. This study aims to determine the inhibitory effects and potential mechanisms of lusianthridin on platelet aggregation. The results indicated that lusianthridin inhibited arachidonic acid, collagen, and adenosine diphosphate (ADP)-stimulated platelet aggregation (IC50 of 0.02 ± 0.001 mM, 0.14 ± 0.018 mM, and 0.22 ± 0.046 mM, respectively). Lusianthridin also increased the delaying time of arachidonic acid-stimulated and the lag time of collagen-stimulated and showed a more selective effect on the secondary wave of ADP-stimulated aggregations. Molecular docking studies revealed that lusianthridin bound to the entrance site of the cyclooxygenase-1 (COX-1) enzyme and probably the active region of the cyclooxygenase-2 (COX-2) enzyme. In addition, lusianthridin showed inhibitory effects on both COX-1 and COX-2 enzymatic activities (IC50 value of 10.81 ± 1.12 µM and 0.17 ± 1.62 µM, respectively). Furthermore, lusianthridin significantly inhibited ADP-induced suppression of cAMP formation in platelets at 0.4 mM concentration (p < 0.05). These findings suggested that possible mechanisms of lusianthridin on the antiplatelet effects might act via arachidonic acid-thromboxane and adenylate cyclase pathways. 相似文献
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Georges Jourdi Marie Lordkipanidz Aurlien Philippe Christilla Bachelot-Loza Pascale Gaussem 《International journal of molecular sciences》2021,22(23)
Over the last decades, antiplatelet agents, mainly aspirin and P2Y12 receptor antagonists, have significantly reduced morbidity and mortality associated with arterial thrombosis. Their pharmacological characteristics, including pharmacokinetic/pharmacodynamics profiles, have been extensively studied, and a significant number of clinical trials assessing their efficacy and safety in various clinical settings have established antithrombotic efficacy. Notwithstanding, antiplatelet agents carry an inherent risk of bleeding. Given that bleeding is associated with adverse cardiovascular outcomes and mortality, there is an unmet clinical need to develop novel antiplatelet therapies that inhibit thrombosis while maintaining hemostasis. In this review, we present the currently available antiplatelet agents, with a particular focus on their targets, pharmacological characteristics, and patterns of use. We will further discuss the novel antiplatelet therapies in the pipeline, with the goal of improved clinical outcomes among patients with atherothrombotic diseases. 相似文献
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Dr. Jennifer X. Qiao Tammy C. Wang Dr. Sheldon Hiebert Carol H. Hu Dr. William A. Schumacher Dr. Steven A. Spronk Charles G. Clark Dr. Ying Han Ji Hua Laura A. Price Hong Shen Dr. Silvi A. Chacko Dr. Gerry Everlof Jeffrey S. Bostwick Thomas E. Steinbacher Yi‐Xin Li Dr. Christine S. Huang Dr. Dietmar A. Seiffert Dr. Robert Rehfuss Dr. Ruth R. Wexler Dr. Patrick Y. S. Lam 《ChemMedChem》2014,9(10):2327-2343
Current antithrombotic discovery efforts target compounds that are highly efficacious in thrombus reduction with less bleeding liability than the standard of care. Preclinical data suggest that P2Y1 antagonists may have lower bleeding liabilities than P2Y12 antagonists while providing similar antithrombotic efficacy. This article describes our continuous SAR efforts in a series of 7‐hydroxyindolinyl diaryl ureas. When dosed orally, 4‐trifluoromethyl‐7‐hydroxy‐3,3‐dimethylindolinyl analogue 4 was highly efficacious in a model of arterial thrombosis in rats with limited bleeding. The chemically labile CF3 group in 4 was then transformed to various groups via a novel one‐step synthesis, yielding a series of potent P2Y1 antagonists. Among them, the 4‐benzothiazole‐substituted indolines had desirable PK properties in rats, specifically, low clearance and small volume of distribution. In addition, compound 40 had high i.v. exposure and modest bioavailability, giving it the best overall profile. 相似文献
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徐玲霞 《水利水运工程学报》2016,14(5)
【摘要】 目的 探讨经皮冠状动脉介入治疗（PCI）术前应用负荷量西洛他唑、阿司匹林、氯吡格雷,继以术后维持量三联抗血小板治疗（TAPT）1周对围手术期心肌梗死（PMI）和随访1个月时主要不良心血管事件发生率的影响。方法 入选2014年6月至2015年5月在天津医科大学第二医院心脏科住院并行PCI治疗的冠心病患者113例。采用随机数字表法进行分组,57例接受阿司匹林（300 mg负荷,继以100 mg Qd,）、氯吡格雷（300 mg负荷,继以75 mg Qd）双联抗血小板治疗（DAPT）,56例在DAPT基础上加用西洛他唑（100 mg负荷,继以50 mg Bid,TAPT组）。本研究进行了两项亚组分析：用药亚组（此次入院前正在应用阿司匹林和（或）氯吡格雷者为用药亚组,n=57）和未用药亚组（此次入院前未应用阿司匹林、氯吡格雷和其他抗血小板药物者为未用药亚组,n=56）。测定PCI术前,术后8 h、24 h的CK-MB、cTnI、hs-CRP水平,确定PMI发生率。结果 PMI总体发生率为39.8%。TAPT组与DAPT组PMI发生率未见统计学差异（32.1%比47.4%,P=0.098）。未应用抗血小板药物患者中,TAPT组较DAPT组PMI发生率明显下降（17.9%比42.9%,P=0.042）。而应用抗血小板药物者,两组PMI发生率未见统计学差异（46.4%比51.7%,P=0.689）。 整体研究人群的多因素Cox回归分析表明,已应用抗血小板药物［风险比（HR）=2.45;95%可信区间（CI） 1.09～5.52;P=0.030］与PMI发生呈显著性正相关,而是否接受TAPT与PMI未见显著性相关。结论 本研究提示,与DAPT相比,加用西洛他唑的TAPT在未应用抗血小板药物的患者中能显著降低PCI相关PMI发生率。而对于已应用抗血小板药物者,TAPT则未显示相似的有益作用。【关键词】 围手术期心肌梗死; 三联抗血小板治疗; 西洛他唑; 冠状动脉介入治疗 相似文献
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目的 比较短期与长期双重抗血小板治疗对冠心病患者的疗效和安全性。方法 计算机检索PubMed、Cochrane Central Register of Controlled Trials、中国生物医学文献数据库、CNKI全文数据库,收集2001年1月至2014年6月公开发表的有关短期双重抗血小板治疗和长期双重抗血小板治疗疗效比较的随机对照试验（RCTs）,手检已获文献的参考文献、会议摘要及相关网站。对文献质量进行严格评价后,对符合要求的RCTs进行资料提取并采用RevMan5.0软件进行Meta分析。结果 共纳入5项RCTs,Meta分析显示：短期和长期双重抗血小板治疗组全因死亡率（OR=0.87,95%CI：0.65～1.17,P=0.36）、心肌梗死发生率（OR=1.04,95%CI：0.73～1.48,P=0.84）、支架内血栓发生率（OR=1.23,95%CI：0.70～2.17,P=0.47）、再血管化发生率（OR=0.94,95%CI：0.71～1.25,P=0.68）、心源性死亡（OR=0.96,95%CI：0.62～1.48,P=0.84）、脑卒中发生率（OR=0.66,95%CI：0.40～1.07,P=0.09）均无统计学意义;短期双重抗血小板治疗组大出血发生率（OR=0.48,95%CI：0.25～0.93,P=0.03）低于长期双重抗血小板治疗组。结论 在冠心病双重抗血小板治疗中,短期和长期双重抗血小板治疗在全因死亡率、心肌梗死发生率、支架内血栓发生率、再血管化发生率、心源性死亡、脑卒中发生率二者相似,短期双重抗血小板治疗有更低的大出血发生率,,初步显示了短期双重抗血小板治疗安全性的优越性。 相似文献