Advantages and limitations of the new anticoagulants

Abstract

During recent years, three new anticoagulants (dabigatran, rivaroxaban and apixaban) have been introduced to the market, probably with one more anticoagulant (edoxaban) in the next 2 years. This review is not intended to compare the efficacy and risks of these new agents, but rather to detail the advantages and limitations. The pharmacokinetic characteristics of these drugs have few drug and food interactions, predictable dose responses, and rapid onset and offset, thus resulting in simplified management of the patient requiring anticoagulant therapy. No routine laboratory monitoring is required. A somewhat unexpected, but exciting observation involving the new anticoagulants, is the uniform reduction in intracranial bleeding by one-half compared with warfarin. The potential limitations of the new anticoagulants include uncertainty regarding assessment of drug levels, safe drug levels for major surgery, management of major bleeding, renal dependence, multiple dose regimens, adherence in the absence of frequent monitoring and unknown, rare side effects that were not captured in the trials. This review should clarify some of these concerns.

Effect of the FXa inhibitors Rivaroxaban and Apixaban on platelet activation in patients with atrial fibrillation

“…Rivaroxaban and Apixaban are direct inhibitors of free and clot-or prothrombinase bound FXa and, thereby, prevent generation of relevant amounts of thrombin upon haemostatic activation [4]. Thrombin is not only a key protein in fibrin clot formation, but also the most potent activator of platelet aggregation known in vivo [2,3].…”

“…Developed by rational drug design Apixaban and Rivaroxaban inhibit high affine and selective the catalytic center of free-, clotbound and prothrombinase-bound FXa, the rate-limiting step in fibrin clot formation. By interacting with a specific component of the coagulation process they bear a predictable pharmakokinetic and pharmakodynamic, a rapid onset and offset of action, a short half-life-time, no food interactions, only few drug interactions and no need for routine laboratory monitoring [4]. As they have demonstrated Abstract Rivaroxaban and Apixaban, increasingly used for stroke prevention in non-valvular atrial fibrillation (AF), might impact platelet reactivity directly or indirectly.…”

Effect of Patient Characteristics, Knowledge and Satisfaction with Warfarin Therapy on Willingness to Switch to a New Oral Anticoagulant

“…difference in the individual maintenance dose requirement (0.5-20 mg daily) to achieve exactly the same effect [1]. In addition to these disadvantages, warfarin carries the risk of intracranial hemorrhage which occurs in 0.4% of patients per year and has a mortality of approximately 50% [5][6][7].…”

“…While it has proven efficacy in treating and preventing thrombotic conditions (stroke and venous thromboembolism [VTE]), warfarin is also associated with several disadvantages such as frequent lab monitoring, multiple drug interactions, narrow therapeutic index and interpersonal variability in metabolism and target effect due to genetic polymorphisms [1][2][3][4][5][6][7]. These factors correlate to a 40-fold This article is available from: http://www.hsprj.com/archive.php…”

Direct Oral Anticoagulant Drugs in Dental Clinical Practice

“…The traditional oral anticoagulant drugs like vitamin K antagonists (VKA-especially warfarin), commonly used in the management of thrombosis, have got many drawbacks (1,2).…”