Pharmacological properties of hirudin and its derivatives. Potential clinical advantages over heparin
Research article published in Drugs & aging (1996)
Abstract
Hirudin and its derivatives represent the first parenteral anticoagulants introduced since the discovery of heparin in the early 1900s. Hirudin, the naturally occurring anticoagulant of the leech, is a single peptide chain of 65 amino acids with a molecular weight of about 7000. Recombinant technology has developed methods to produce recombinant forms of hirudin (r-hirudin) in sufficient quantities for therapeutic use. Hirudin is a potent thrombin-specific inhibitor that forms equimolar complexes with thrombin. It represents a new anticoagulant agent in a field in which heparin has been the only available drug for many years. In contrast to heparin, hirudin does not require antithrombin III as a cofactor, is not inactivated by antiheparin proteins, has no direct effects on platelets and may also inactivate thrombin bound to clot or the subendothelium. In humans, experience with r-hirudin in preventing or treating venous thromboembolism is very preliminary. However, r-hirudin achieved promising results in patients with unstable angina, or following coronary angioplasty. In patients with acute myocardial infarction, 3 important clinical trials were stopped because of an excess of bleeding complications. At present, the discovery of a r-hirudin regimen that is more efficacious than heparin and at least as safe needs a reappraisal of the drug in further trials.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Hirudin and its derivatives represent the first parenteral anticoagulants introduced since the discovery of heparin in the early 1900s. Hirudin, the naturally occurring anticoagulant of the leech, is a single peptide chain of 65 amino acids with a molecular weight of about 7000.
Por qué esto importa para la hirudoterapia
Este artículo examina las propiedades farmacológicas de la hirudin—identificada como el anticoagulante natural de la sanguijuela—y sus formas recombinantes (r-hirudin), detallando su mecanismo como un inhibidor potente y directo específico de la trombina que, a diferencia de la heparina, no requiere antitrombina III como cofactor, no es inactivado por proteínas antiheparínicas, no tiene efectos directos sobre las plaquetas y puede inactivar la trombina unida al coágulo. Esto es relevante para el ámbito de ASH porque la hirudin es un compuesto natural derivado de la sanguijuela, aunque el resumen la discute únicamente como agente farmacéutico y no aborda la terapia con sanguijuelas, la hirudoterapia ni las secreciones salivales. La experiencia clínica descrita es preliminar: la r-hirudin mostró resultados tempranos prometedores en contextos de angina inestable y post-angioplastia coronaria, mientras que tres ensayos en infarto agudo de miocardio fueron suspendidos debido a un exceso de complicaciones hemorrágicas. El resumen concluye que la identificación de un régimen de r-hirudin que sea tanto más seguro como más eficaz que la heparina requiere ensayos adicionales.
Citación
Pharmacological properties of hirudin and its derivatives. Potential clinical advantages over heparin.
Monreal M, Costa J, Salva P · Drugs & aging, 1996
Contexto clínico relacionado
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Añadido a la biblioteca ASH: March 18, 2026 · Última actualización del sitio: June 18, 2026