Clinical potential of oral direct thrombin inhibitors in the prevention and treatment of venous thromboembolism
Review published in Drugs (2004)
Abstract
Current antithrombotic therapies are associated with various practical limitations and risks that restrict their utility in the management of venous thromboembolism. The coagulation factor, thrombin, has been the focus of extensive investigation as a pharmacological target in efforts to improve the management of venous thromboembolism. Hirudin, desirudin, bivalirudin and argatroban are direct thrombin inhibitors that have been launched for limited indications as anticoagulants. Their usefulness for long-term prophylaxis is limited by a requirement for parenteral administration, restricted licensing and bleeding/tolerability profile. Ximelagatran--which, after oral administration, is rapidly converted to its active form, melagatran--is the first oral direct thrombin inhibitor and the first new oral anticoagulant to become available in 60 years. Clinical studies have shown that melagatran/ximelagatran, without coagulation monitoring, is effective and well tolerated for the prevention of venous thromboembolism after hip replacement and knee replacement surgery. Ximelagatran is also effective in the acute treatment of venous thromboembolism and long-term secondary prevention of recurrent venous thromboembolism, the prevention of stroke in patients with atrial fibrillation and in the prevention of cardiovascular events after myocardial infarction. Oral direct thrombin inhibitors have a promising role in the management of venous thromboembolism and other associated medical conditions.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Current antithrombotic therapies are associated with various practical limitations and risks that restrict their utility in the management of venous thromboembolism.
Por qué esto importa para la hirudoterapia
Esta revisión examina los inhibidores directos de trombina orales para la prevención y el tratamiento del tromboembolismo venoso, señalando que la hirudina, desirudina, bivalirudina y argatrobán han sido lanzados para indicaciones anticoagulantes limitadas, pero requieren administración parenteral. El resumen se centra en ximelagatrán/melagatrán, reportando efectividad clínica para la profilaxis de TEV tras cirugía ortopédica, el tratamiento agudo de TEV y la prevención de accidentes cerebrovasculares en fibrilación auricular sin monitorización de la coagulación. Para el dominio de ASH, la revisión es relevante en la medida en que la hirudina y sus derivados se presentan como predecesores parenterales cuyas limitaciones prácticas motivaron el desarrollo de alternativas orales. Advertencia: Se trata de una revisión farmacológica centrada en un anticoagulante oral sintético; no aborda la hirudoterapia ni la aplicación de sanguijuelas vivas, y todas las afirmaciones clínicas pertenecen a DTI farmacéuticos.
Citación
Clinical potential of oral direct thrombin inhibitors in the prevention and treatment of venous thromboembolism.
Agnelli G · Drugs, 2004
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026