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.
Zusammenfassung
Comparative pharmacology of site directed antithrombin agents. Implication in drug development.
Warum dies für die Hirudotherapie relevant ist
This review compares the pharmacology of newer antithrombin agents, noting that—beyond direct thrombin inhibition—many produce additional effects such as fibrinolytic compromise (via actions on t-PA, plasmin, urokinase, and protein C) and hemodynamic/hemostatic deficits, and that ongoing clinical-trial designs remain largely empirical. The abstract discusses heparin and synthetic peptide inhibitors but does not mention leeches, hirudin, or hirudotherapy at any point. Consequently, the article's relevance to applied leech therapy is at best indirect and conceptual, offering only general background on antithrombin pharmacology rather than any direct leech-related evidence.
Zitation
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