title: The pharmacology of recombinant hirudin, a new anticoagulant.
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 side-effects. The mean elimination half-life is about 1 hour. Mean total clearance and volume of distribution are approximately 190 ml/min and 14 l, respectively. Hirudin obeys first-order pharmacokinetics.
authors.affiliation: Department of Pharmacology, University of the Orange Free State, Bloemfontein.
authors.forename: B H
authors.initials: BH
authors.lastname: Meyer
authors.forename: H G
authors.initials: HG
authors.lastname: Luus
authors.forename: F O
authors.initials: FO
authors.lastname: Müller
authors.forename: P N
authors.initials: PN
authors.lastname: Badenhorst
authors.forename: H J
authors.initials: HJ
authors.lastname: Röthig
mesh_terms: D004305:Dose-Response Relationship, Drug; D005069:Evaluation Studies as Topic; D006629:Hirudins / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008297:Male; D010314:Partial Thromboplastin Time; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D013918:Thrombin Time
chemical_list: D006629:Hirudins; D011994:Recombinant Proteins