Hirudin and hirudin fragments

Hirudin is a potent and specific thrombin inhibitor: compared with heparin thrombin inhibition occurs directly and does not require the presence of plasma cofactors. Recombinant hirudin is well tolerated in animals and in healthy volunteers. Its clearance half-life after IV administration range from 1 to 2 hours and its bioavailability after subcutaneous administration reaches 75%. In most of the experimental models the ratio of the haemorrhagic side effect against the antithrombotic efficacy is satisfactory. Hirudin analogs are mono or bivalent according to their recognition site on thrombin. Bivalent derivatives (Hirulogs) have been mostly evaluated: they exhibit pharmacologic properties similar experimental to that of recombinant hirudin and have been successfully used in several thrombosis models and in healthy volunteers. Taking into account these data the most appropriate use for hirudin and hirudin derivatives should be clinical situations where the role of thrombin is important or which are only partially controlled by heparin therapy.

Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.

This review of hirudin and its fragments reports that recombinant hirudin is well tolerated, with a 1-2 hour intravenous half-life and 75% subcutaneous bioavailability; bivalent Hirulog derivatives show similar pharmacology, suggesting use where thrombin matters or heparin control is incomplete.

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