Pharmacodynamics of Parenteral and Oral Anticoagulants

Fremont, Rudolph E.

doi:10.1177/000331976401500308

Cited by 5 publications

(3 citation statements)

References 28 publications

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“…It cannot be used in acute presentations of a condition that requires immediate anticoagulation therapy as it has a long onset of action, between three and ten days [44]. In addition, as warfarin inhibits the anticoagulation proteins C and S first due to their short half-life, bridge therapy is necessary with heparin or low molecular weight heparins to maintain an antithrombotic state until warfarin achieves its full effect [54]. Warfarin is also a teratogen, and so cannot be used in pregnancy [55].…”

Section: Limitations To Warfarin Therapymentioning

confidence: 99%

“…It directly inactivates thrombin and factor Xa [54,61]. Low molecular weight heparin (LMWH) fragments that contain a specific pentasaccharide sequence can also exert their inhibitory effects and serve a role as an anticoagulant.…”

Section: Limitations To Heparin Therapymentioning

confidence: 99%

“…By binding to thrombin and inhibiting its action, heparin works immediately upon administration. As a result, heparin can be used when warfarin treatment is being started as a bridge therapy to provide anticoagulation until warfarin is able to decrease the formation of various members of the clotting cascade and achieve its anticoagulation effect [54,61].…”

Section: Limitations To Heparin Therapymentioning

confidence: 99%

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Recent Developments in Antithrombotic Therapy: Will Sodium Warfarin Be a Drug of the Past?

Desai¹,

Massad²,

DiDomenico³

et al. 2006

PRC

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Warfarin and heparin have formed the mainstay in the prophylaxis of deep vein thrombosis (DVT), stroke prevention in atrial fibrillation, and treatment of thromboembolic disease (TED). However, these choices are hampered by difficult administration, interactions with other medications, side effect profile, and limited indications for treatment. Anti-factor Xa (anti-Xa) inhibitors have already entered the drug market with the drug Fondaparinux being the first anti-Xa inhibitor to be approved for use in the U.S. by the Food and Drug Administration (FDA), and other drugs such as idraparinux being currently in development. A new class of medications, known as direct thrombin inhibitors (DTI), includes the parental agents lepirudin, argatroban and bivalirudin which have been approved by the FDA and the oral agents ximelagatran, melagatran and dabigatran. The latter three drugs which are oral DTIs may soon replace warfarin and heparin as the preferred medications for DVT prophylaxis and for reducing the relative risk of stroke. These drugs do not rely on blocking serine proteases nor do they require a co-factor (antithrombin III) like unfractionated heparin (UFH) or low molecular weight heparin (LMWH). DTIs are rapid in onset, easy to administer, do not interact with other medications or foods, have limited side effects, and can be administered in a fixed dose. The DTI ximelagatran has already been approved in several European and Asian countries, and over a dozen randomized clinical trials have been conducted demonstrating its performance to be on par with warfarin. However, approval by the FDA in the U.S. remains pending in view of reported incidences of elevations in hepatic enzymes that are currently under evaluation. This review examines the role of DTIs in the prevention and treatment of TED and the recent patents reported in the literature.

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Section: Limitations To Warfarin Therapymentioning

confidence: 99%

Section: Limitations To Heparin Therapymentioning

confidence: 99%

Section: Limitations To Heparin Therapymentioning

confidence: 99%

See 1 more Smart Citation

Recent Developments in Antithrombotic Therapy: Will Sodium Warfarin Be a Drug of the Past?

Desai¹,

Massad²,

DiDomenico³

et al. 2006

PRC

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Chemistry and Pharmacology of Heparin

Ehrlich

Stivala

1973

Journal of Pharmaceutical Sciences

121

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Long term thromboresistance of heparinized surfaces

Ehrlich¹

1975

Polymer Engineering & Sci

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It has long been known that interaction of blood with artificial surfaces results in thrombogenic effects. With the increased use of prosthetic cardiovascular appliances, it is becoming more evident that surfaces which are thromboresistant are of utmost importance. A review is presented of the recent research on binding of heparin by ionic, covalent and thermal means, to different polymer surfaces, with the results of in vitro and in vivo tests. Additionally, a survey of theories on the role of heparin surfaces in thromboresistance is given.

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Pharmacodynamics of Parenteral and Oral Anticoagulants

Cited by 5 publications

References 28 publications

Recent Developments in Antithrombotic Therapy: Will Sodium Warfarin Be a Drug of the Past?

Recent Developments in Antithrombotic Therapy: Will Sodium Warfarin Be a Drug of the Past?

Chemistry and Pharmacology of Heparin

Long term thromboresistance of heparinized surfaces

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