[New anticoagulants for secondary haemostasis--anti IIa inhibitors].
In contrast to heparins and oral anticoagulants, anti IIa inhibitors (thrombin inhibitors) are able to directly inhibit the protease activity of thrombin and can thereby precisely control the blood coagulation process. Direct thrombin inhibitors are either biosimilars (r-hirudin) or synthetically produced substances (bivalirudin, argatroban, dabigatran). In 1997 r-hirudin was introduced into clinical practice, however due to its narrow therapeutic range and the necessity of drug monitoring it has not gained widespread clinical use by now. Since 2004 and 2005 the synthetic thrombin inhibitors bivalirudin and argatroban, respectively, are available. With dabigatran the first oral synthetic thrombin inhibitor followed in 2008. These four drugs can inhibit even clot bound thrombin and show low plasma protein binding. They differ in respect to route and duration of application as well as elimination from the body, thereby offering a precise inhibition of blood coagulation adjusted to the individual case and without danger of HIT II. These advantages shall be used and advanced by the development of further direct thrombin inhibitors.
Nowak
G
G
Universitätsklinikum Jena, AG "Pharmakologische Hämostaseologie", Drackendorfer Str. 1, 07747 Jena. AGPHH@med.uni-jena.de
D000368:Aged; D000925:Anticoagulants / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001711:Biotransformation; D003374:Coumarins / Q000493:pharmacokinetics / Q000627:therapeutic use; D005260:Female; D006487:Hemostasis / Q000187:drug effects* / Q000235:genetics; D006493:Heparin / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D019934:International Normalized Ratio; D008297:Male; D008875:Middle Aged; D010597:Pharmacogenetics; D051437:Renal Insufficiency / Q000139:chemically induced; D014812:Vitamin K / Q000037:antagonists & inhibitors*; D014859:Warfarin / Q000493:pharmacokinetics / Q000627:therapeutic use
D000925:Anticoagulants; D003374:Coumarins; D014812:Vitamin K; D014859:Warfarin; D006493:Heparin