Changing trends in anti-coagulant therapies. Are heparins and oral anti-coagulants challenged?

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dc.authorscopusid7102367063
dc.authorscopusid7004673302
dc.authorscopusid24467275600
dc.authorscopusid7004457653
dc.authorscopusid24400279600
dc.authorscopusid55429479900
dc.authorscopusid24172964200
dc.contributor.authorFareed J.
dc.contributor.authorIqbal O.
dc.contributor.authorCunanan J.
dc.contributor.authorDemir M.
dc.contributor.authorWahi R.
dc.contributor.authorClarke M.
dc.contributor.authorAdiguzel C.
dc.date.accessioned2024-06-12T10:28:08Z
dc.date.available2024-06-12T10:28:08Z
dc.date.issued2008
dc.description.abstractThe conventional management of thrombotic and cardiovascular disorders is based on the use of heparin, oral anti-coagulants and aspirin. Despite progress in the sciences, these drugs still remain a challenge and mystery. The development of low molecular weight heparins (LMWHS) and the synthesis of heparinomimetics represent a refined use of heparin. Additional drugs will continue to develop. However, none of these drugs will ever match the polypharmacology of heparin. Aspirin still remains the leading drug in the management of thrombotic and cardiovascular disorders. The newer antiplatelet drugs such as adenosine diphosphate receptor inhibitors, GPIIb/IIIa inhibitors and other specific inhibitors have limited effects and have been tested in patients who have already been treated with aspirin. Warfarin provides a convenient and affordable approach in the long-term outpatient management of thrombotic disorders. The optimized use of these drugs still remains the approach of choice to manage thrombotic disorders. The new anticoagulant targets, such as tissue factor, individual clotting factors, recombinant forms of serpins (antithrombin, heparin co-factor II and tissue factor pathway inhibitors), recombinant activated protein C, thrombomodulin and site specific serine proteases inhibitors complexes have also been developed. There is a major thrust on the development of orally bioavailable anti-Xa and IIa agents, which are slated to replace oral anticoagulants. Both the anti-factor Xa and anti-IIa agents have been developed for oral use and have provided impressive clinical results. However, safety concerns related to liver enzyme elevations and thrombosis rebound have been reported with their use. For these reasons, the US Food and Drug Administration did not approve the orally active antithrombin agent Ximelagatran for several indications. The synthetic pentasaccharide (Fondaparinux) has undergone clinical development. Unexpectedly, Fondaparinux also produced major bleeding problems at minimal dosages. Fondaparinux represents only one of the multiple pharmacologic effects of heparins. Thus, its therapeutic index will be proportionately narrower. The newer antiplatelet drugs have added a new dimension in the management of thrombotic disorders. The favorable clinical outcomes with aspirin and clopidogrel have validated COX-I and P2Y12 receptors as targets for new drug development. Prasugrel, a novel thienopyridine, Cangrelor and AZD 6140 represent newer P2Y12 antagonists. Cangrelor and AZD 6140 are direct inhibitors, whereas Prasugrel requires metabolic activation. While clinically effective, recent results have prompted a closure of a clinical trial with Prasugrel due to bleeding. The newer anticoagulant and antiplatelet drugs are attractive, however, none of these are expected to replace the conventional drugs in polytherapeutic approaches. Heparins, warfarin and aspirin will continue to play a major role in the management of thrombotic and cardiovascular disorders for years to come.en_US
dc.identifier.endpage192en_US
dc.identifier.issn0392-9590
dc.identifier.issue3en_US
dc.identifier.pmid18506123en_US
dc.identifier.scopus2-s2.0-47249130462en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage176en_US
dc.identifier.urihttps://hdl.handle.net/20.500.14551/17093
dc.identifier.volume27en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.relation.ispartofInternational Angiologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAntithrombosis; Aspirin; Heparin; Warfarinen_US
dc.subjectAcetylsalicylic Acid; Adenosine Diphosphate Receptor Inhibitor; Anticoagulant Agent; Antithrombocytic Agent; Bemiparin; Blood Clotting Factor; Blood Clotting Factor 10a Inhibitor; Blood Clotting Inhibitor; Cangrelor; Clopidogrel; Cyclooxygenase 1; Drotrecogin; Fibrinogen Receptor Antagonist; Fondaparinux; Heparin; Heparin Cofactor Ii; Idraparinux; Low Molecular Weight Heparin; Prasugrel; Prothrombin A Inhibitor; Purinergic P2y12 Receptor; Receptor Blocking Agent; Serine Proteinase Inhibitor; Thrombomodulin; Thromboplastin; Ticagrelor; Tissue Factor Pathway Inhibitor; Unindexed Drug; Warfarin; Ximelagatran; Acetylsalicylic Acid; Anticoagulant Agent; Blood Clotting Factor 10a; Factor Iia; Generic Drug; Heparin; Low Molecular Weight Heparin; New Drug; Prothrombin; Thrombin; Warfarin; Anticoagulant Therapy; Bleeding; Cardiovascular Disease; Clinical Trial; Drug Approval; Drug Indication; Drug Safety; Drug Structure; Drug Synthesis; Drug Targeting; Drug Use; Food And Drug Administration; Granulocytopenia; Heparin Induced Thrombocytopenia; Human; Idiopathic Thrombocytopenic Purpura; Outcome Assessment; Outpatient Care; Review; Side Effect; Therapy; Thrombocytopenia; Thrombosis; United States; Unspecified Side Effect; Blood; Blood Clotting; Drug Antagonism; Drug Effect; Oral Drug Administration; Thrombosis; Transluminal Coronary Angioplasty; Treatment Outcome; Administration, Oral; Angioplasty, Transluminal, Percutaneous Coronary; Anticoagulants; Aspirin; Blood Coagulation; Drugs, Generic; Drugs, Investigational; Factor Xa; Heparin; Heparin, Low-Molecular-Weight; Humans; Platelet Aggregation Inhibitors; Prothrombin; Thrombin; Thrombosis; Treatment Outcome; Warfarinen_US
dc.titleChanging trends in anti-coagulant therapies. Are heparins and oral anti-coagulants challenged?en_US
dc.typeReview Articleen_US

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