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South African Medical Journal

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The pharmacology of recombinant hirudin, a new anticoagulant

B.H. Meyer, H.G. Luus, F.O. Muller, P.N. Badenhorst, H.J. Rothig

Abstract


A new anticoagulant, recombinant hirudin, was given to healthy volunteers (5 per test dose) in single .intravenous doses of 0,01, 0,02, 0,04, 0,07 and 0,1 mg/kg to study its anticoagulant effects, how it was tolerated and its pharmacokinetics. Hirudin proved to be a potent anticoagulant with important effects on thrombin (increase in thrombin time and partial thromboplastin time). The maximum pharmacodynamic effect was achieved with the 0,07 mg/kg dose, and upwards. All doses of the compound were tolerated without sideeffects. The mean elimination half-life is about 1 hour. Mean total clearance and volume of distribution are approximately 190 ml/min and 14 I, respectively. Hirudin obeys first-order pharmacokinetics.




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