Comparative pharmacology of site directed antithrombin agents. Implication in drug development
Research article published in Thrombosis and haemostasis (1995)
Abstract
Beside the direct inhibition of thrombin and its regulatory functions, many of the newer antithrombin agents produce several additional effects, unrelated to their anticoagulant actions. Synthetic peptide inhibitors are capable of producing fibrinolytic compromise by virtue of their actions on fibrinolytic enzymes such as t-PA, plasmin, urokinase and protein Ca. In addition, the low molecular weight arginine-containing peptides are also known to produce hemodynamic and hemostatic deficits. The designs of the ongoing clinical trials are largely empirical because of the non-availability of valid pharmacologic and toxicologic data on thrombin inhibitors. In contrast to heparin, none of the thrombin inhibitors produce endogenous release of tissue factor pathway inhibitor (TFPI) in the experimental and clinical settings. These observations suggest that beside the direct inhibition of thrombin, these agents also produce multiple additional effects that can significantly contribute to their pharmacologic and toxicologic profile.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Comparative pharmacology of site directed antithrombin agents. Implication in drug development.
Por qué esto importa para la hirudoterapia
Esta revisión compara la farmacología de los agentes antitrombina más recientes, señalando que—más allá de la inhibición directa de la trombina—muchos producen efectos adicionales como compromiso fibrinolítico (mediante acciones sobre t-PA, plasmina, uroquinasa y proteína C) y déficits hemodinámicos/hemostáticos, y que los diseños de ensayos clínicos en curso siguen siendo en gran medida empíricos. El resumen discute la heparina y los inhibidores peptídicos sintéticos, pero no menciona sanguijuelas, hirudina ni hirudoterapia en ningún momento. En consecuencia, la relevancia del artículo para la terapia aplicada con sanguijuelas es en el mejor de los casos indirecta y conceptual, ofreciendo solo antecedentes generales sobre la farmacología de la antitrombina en lugar de evidencia directa relacionada con la sanguijuela.
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026