The pharmacology of recombinant hirudin, a new anticoagulant.
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.
Meyer
B H
BH
Department of Pharmacology, University of the Orange Free State, Bloemfontein.
Luus
H G
HG
Müller
F O
FO
Badenhorst
P N
PN
Röthig
H J
HJ
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
D006629:Hirudins; D011994:Recombinant Proteins