New options with dabigatran etexilate in anticoagulant therapy

Abstract

Thrombosis, the localized clotting of blood, occurs in both the arterial and venous circulation, and has a major impact on health outcomes. The primary etiology of myocardial infarctions, and approximately 80% of strokes, is acute arterial thrombosis. In combination this represents the most common cause of death in the Western world, while the third leading cause of cardiovascular-associated death is venous thromboembolism. An understanding of the pathogenic changes in the vessel wall and the blood that result in thrombosis is crucial for developing safer and more effective antithrombotic drugs. Dabigatran etexilate belongs to a new class of direct thrombin inhibitors. Following oral administration, dabigatran reaches peak plasma concentrations within 2 hours, shows linear pharmacokinetics, and a limited (but important) amount of direct drug interactions. Given once daily at 150 mg or 220 mg, it has proven to be competitive with enoxaparin in the prevention of venous thromboembolism after major orthopedic surgery, with a comparable safety profile. For stroke prevention in patients suffering from atrial fibrillation, dabigatran administered at a dose of 110 mg twice daily was associated with rates of stroke and systemic embolism that were similar to those associated with warfarin, as well as lower rates of hemorrhage. Dabigatran given at a dose of 150 mg twice daily, as compared with warfarin, was associated with lower rates of stroke and systemic embolism but similar rates of major hemorrhage. Oral bioavailability of dabigatran, together with a rapid onset and offset of action and predictable anticoagulation response, makes this newly available antithrombotic drug an attractive alternative to traditional anticoagulant therapies for numerous thrombosis-related indications.

Screening of direct thrombin inhibitors from Radix Salviae Miltiorrhizae by a peak fractionation approach

“…They have the effects of attenuating plaque progression and promoting stability in advanced atherosclerotic lesions [2]. Nowadays several kinds of direct thrombin inhibitors, such as argatroban and dabigatran etexilate, have been clinically used to prevent and treat cardiovascular diseases [5,6]. However, they may also cause serious side effects like hemorrhage [7].…”

Complications With New Oral Anticoagulants Dabigatran and Rivaroxaban in Cutaneous Surgery

“…Their side-effect profile is more advantageous than that of vitamin K antagonists in that they produce fewer severe lifethreatening hemorrhagic complications. [8][9][10][11] Outcomes of major bleeding events also have been reported to be better with dabigatran than with warfarin, resulting in shorter stays in intensive care and lower mortality. 12,13 Thus, treatment with these new oral anticoagulants is an attractive alternative to treatment with vitamin K antagonists.…”

Dabigatran Does Not Prolong the QT Interval with Supratherapeutic Exposure: a Thorough QT Study in Healthy Subjects

“…However, VKAs have a narrow therapeutic window, numerous drug and food interactions, and require routine monitoring and dose adjustments [1]. Heparins require parenteral administration, which can be difficult when chronic use is required [2, 3]. …”