Direct thrombin inhibitors
Dabigatran: Will it change clinical practice - Siddharth A. Wartak MD
image by: Niña Faustino Macasang
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The New Anticoagulants
Hirudin, the prototype direct thrombin inhibitor, was derived from leech saliva (seriously). Argatroban and Dabigatran are newer direct thrombin inhibitors. Dabigatran has been approved for DVT prophylaxis after surgery and stroke prevention in patients with atrial fibrillation.
The half-life is 12-17 hours in patients with normal renal function. As it is cleared by both the liver and kidneys, this agent is not recommended in patients with renal failure or impaired hepatic function. Compared to warfarin, dabigatran is touted for its immediate anticoagulation, lack of transient hypercoagulable state, minimal interactions with food and other drugs and lack of any required testing to…
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One Thing Leads to Another – Idarucizumab for Dabigatran
We agree idarucizumab rapidly normalizes abnormal coagulation parameters associated with use, but its suspected clinical effectiveness and safety cannot be confirmed at this time.
A Case Example: Reversing Anticoagulant Dabigatran with Idarucizumab
You recall that there is a new drug out that specifically counters dabigatran. It is composed of monoclonal antibodies that bind to and inactivate the drug. It is made by the same company that makes dabigatran (Boehringer Ingelheim).
A New Anticoagulant for a New Era: Review of Recent Data on Dabigatran Etexilate
Dabigatran etexilate is an orally administered prodrug, which is rapidly absorbed and metabolized to its active form, dabigatran. It selectively targets thrombin in a dose-dependent and reversible manner.
Dabigatran etexilate: a new thrombin inhibitor
Dabigatran etexilate is a low-molecular-weight prodrug that itself exhibits no pharmacological activity. However, after oral administration, dabigatran etexilate is rapidly absorbed and converted to its active moiety, dabigatran, by catalysed hydrolysis in plasma and in the liver. Dabigatran is a potent, competitive and reversible direct inhibitor of the thrombin enzyme, with an oral bioavailability of 6.5%. Dabigatran has a terminal half-life of 14–17 hours, thereby facilitating once-daily dosing.
Dabigatran, A Direct Thrombin Inhibitor (DTI) as the First Line Treatment for Cerebral Venous Thrombosis. An Updated Case Series
This case series suggests DTI are probably effective primary treatment modality for patients with CVST with good safety profile.
Dabigatran: Will it change clinical practice?
Dabigatran etexilate (Pradaxa) is a new oral anticoagulant that has distinct advantages over warfarin (Coumadin) in terms of its ease of administration, efficacy, and safety.
Direct thrombin inhibitors
Heparins and vitamin K antagonists have been the primary agents used for anticoagulation in certain cardiovascular and thromboembolic diseases for over 50 years. However, they can be difficult to administer and are fraught with limitations. In response to the need for new anticoagulants, direct thrombin inhibitors (DTIs) have been developed and investigated for their utility in prophylaxis and treatment of venous thromboembolism (VTE), heparin-induced thrombocytopenia (HIT), acute coronary syndromes (ACS), secondary prevention of coronary events after ACS, and nonvalvular atrial fibrillation. C
Implications of Dabigatran, a Direct Thrombin Inhibitor, for Oral Surgery Practice
Direct thrombin inhibitors, specifically orally administered dabigatran etexilate, are emerging as alternatives to warfarin for anticoagulation in the management of atrial fibrillation and venous thromboembolism. The risk associated with bleeding events while taking dabigatran has been documented in multiple randomized controlled trials, but to date, no studies have focused on the risk of bleeding after dental extraction.
Safety of Dabigatran as an Anticoagulant: A Systematic Review and Meta-Analysis
Dabigatran has a favorable safety profile in terms of major bleeding, intracranial hemorrhage, and life-threatening events, among other safety outcomes. The present study suggested that dabigatran may be a suitable alternative to VKAs as an oral anticoagulant.
The New Anticoagulants
Hirudin, the prototype direct thrombin inhibitor, was derived from leech saliva (seriously). Argatroban and Dabigatran are newer direct thrombin inhibitors. Dabigatran has been approved for DVT prophylaxis after surgery and stroke prevention in patients with atrial fibrillation. The half-life is 12-17 hours in patients with normal renal function. As it is cleared by both the liver and kidneys, this agent is not recommended in patients with renal failure or impaired hepatic function.
Pradaxa (Dabigatran)
PRADAXA is used to: •reduce risk of stroke and blood clots in patients with atrial fibrillation (AFib) not caused by a heart valve problem •treat blood clots in the veins of your legs (deep vein thrombosis, or DVT) or lungs (pulmonary embolism, or PE) and reduce the risk of them occurring again.
Praxbind
PRAXBIND is a specific reversal agent for PRADAXA, with no impact on the effect of other anticoagulant or antithrombotic therapies. PRADAXA can be re-initiated after 24 hours following PRAXBIND administration.
Acova (Argatroban)
Argatroban is a synthetic direct thrombin inhibitor. The chemical name is 1-[(2S)-5-[(aminoimino-methyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-,(2R,4R)- 2-Piperidinecarboxylic acid. Argatroban has 4 asymmetric carbons.
Thrombosis Adviser
Dabigatran is orally administered as the prodrug dabigatran etexilate, which is converted to the active form in plasma and in the liver...
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