Antiplatelet medications and their indications in preventing and treating coronary thrombosis

Graaff, Eric Van De; Steinhubl, Steven R.

doi:10.3109/07853890008998836

Cited by 19 publications

(39 citation statements)

References 67 publications

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“…Aspirin reduces the risk of myocardial infarction 1,2 and has been shown to improve graft patency rates after coronary artery bypass grafting (CABG). 3,4 Paradoxically, the very mechanisms that confer protection against myocardial infarction and graft closure may also contribute to increased bleeding complications after cardiac surgery.…”

Section: Discussionmentioning

confidence: 99%

Aspirin and Postoperative Bleeding After Coronary Artery Bypass Grafting

Ferraris

Ferraris²,

Joseph³

et al. 2002

Annals of Surgery

102

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ObjectiveTo evaluate the relationship between aspirin ingestion and postoperative bleeding complications, and to test the hypothesis that there is a subset of patients who are aspirin hyperresponders with a proclivity toward platelet dysfunction. Summary Background DataDespite numerous retrospective and prospective analyses, it is still controversial as to whether aspirin ingestion before coronary artery bypass grafting (CABG) is associated with significant postoperative bleeding. MethodsBetween January 1995 and December 1999, the records of 2,606 consecutive patients undergoing CABG were reviewed to identify patients with a history of aspirin ingestion up until the time of surgery. Aspirin ingestion was correlated with postoperative blood transfusion using multivariate analysis. In a subset of preoperative aspirin users (n ϭ 40), bleeding times were measured before and after aspirin use. Flow cytometry was performed in another cohort of patients with known heart disease (n ϭ 30) to determine the effect of aspirin on platelet surface receptors. ResultsDuring the 5-year study period, 63% of the CABG patients were identified as aspirin users. Among these, 23.1% required blood transfusions compared with 19% for the nonusers. Non-red blood cell transfusions were more common in aspirin users, as was reexploration for bleeding. Stratification of these results according to the frequency of aspirin use showed that aspirin is an independent multivariate predictor of postoperative blood transfusion only in high-risk patients. In the prospective studies, aspirin treatment resulted in a significant increase in the template bleeding time, an increase in platelet PAR-1 thrombin receptor activity, and a decrease in the binding of platelets to monocytes. ConclusionsThe findings support the hypothesis that aspirin is associated with a greater likelihood of postoperative bleeding. A platelet function testing algorithm that combines preoperative risk factor assessment, template bleeding times, and flow cytometry may allow the identification of aspirin hyperresponders who are at increased risk for bleeding.

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Section: Discussionmentioning

confidence: 99%

Aspirin and Postoperative Bleeding After Coronary Artery Bypass Grafting

Ferraris

Ferraris²,

Joseph³

et al. 2002

Annals of Surgery

102

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“…1) Anti-thrombotic therapy agents, mainly aiming at treating thrombin platelet and thrombosis, are divided into 1) anti-platelet drugs, to prevent the coronary and cerebrovascular thrombosis from forming, such as aspirin and ticlopidine 2) ; 2) drugs against thrombin, 3,4) known as anticoagulants, including heparin and warfarin; 3) thrombolytic drugs such as fibrinolytic drugs. 5) Currently the most widely clinically applicable anti-platelet drugs are cyclooxygenase inhibitor, ADP receptor antagonists, phosphodiesterase inhibitor and GPIIb/IIIa receptor antagonist.…”

Section: 4-benzoxazine-3(4h)-ones As Potent Inhibitors Of Plateletmentioning

confidence: 99%

1,4-Benzoxazine-3(4<i>H</i>)-ones as Potent Inhibitors of Platelet Aggregation: Design, Synthesis and Structure–Activity Relations

Liu

Tan

Xiao

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of novel potentially platelet aggregation-inhibiting 1,4-benzoxazine-3(4H)-one derivatives was designed and synthesized through Smiles rearrangement, reduction and acetylation reactions. The antiaggregatory activities of the target molecules on arterial blood samples from rabbits, expressed by IC 50 values (μM), were then evaluated in vitro against ADP induced platelet aggregation. The favorable IC 50 values of compound 8c (IC 50 8.99 µM) and 8d (IC 50 8.94 µM) indicated that these two compounds were the most potent molecules among all the synthesized compounds. A detailed molecular docking study to explore the interaction of compounds 8c and 8d with GP IIb/IIIa receptor showed that they these two compounds were docked into the active site of GPIIb/IIIa receptor. These results suggest that the 1,4-benzoxazine-3(4H)-one derivatives are promising lead compounds to develop new platelet aggregation inhibitors.

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“…Among these agonists, AA is one of the most powerful agonists for platelet activation 6,7 . Currently, essential antiplatelet drugs used for the prophylaxis and treatment of thromboembolic diseases are aspirin, ridogrel, ticlopidine, clopidogrel, dipyridamole, cilostazol, tirofiban and sibrafiban [8][9][10][11][12] . Nevertheless, these orally administered antiplatelet drugs have certain disadvantages, such as gastric erosion, agranulocytosis, neutropenia, thrombocytopenia, aplastic anemia and thrombotic thrombocytopenic purpura along with inefficient therapy [13][14][15][16] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of some dibenzofuran-piperazine derivatives

Yurttaş

Mohsen

Özkan

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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In the present paper, a novel series of dibenzofuran-piperazine derivatives were synthesized via the treatment of N-(2-methoxy-3-dibenzofuranyl)-2-chloroacetamide with substituted piperazine derivatives. The chemical structures of the compounds were elucidated by 1 H NMR, 13C NMR, mass spectral data; elemental analysis and HPLC analysis. Each derivative was evaluated for antiplatelet activity and anticholinesterase activity. Compound 2 m with 2-furoyl moiety exhibited high percentage inhibition as much as standard drug aspirin on arachidonic acid (AA)-induced platelet aggregation. None of the compounds presented significant inhibitor effect on collagen-induced platelet aggregation. Furthermore, the anticholinesterase activity of the compounds was determined and they did not show promising inhibitor activity compared with standard drug donepezil.

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Antiplatelet medications and their indications in preventing and treating coronary thrombosis

Cited by 19 publications

References 67 publications

Aspirin and Postoperative Bleeding After Coronary Artery Bypass Grafting

Aspirin and Postoperative Bleeding After Coronary Artery Bypass Grafting

1,4-Benzoxazine-3(4<i>H</i>)-ones as Potent Inhibitors of Platelet Aggregation: Design, Synthesis and Structure–Activity Relations

Synthesis and biological evaluation of some dibenzofuran-piperazine derivatives

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