[Argatroban: pharmacological properties and anaesthesiological aspects].
Argatroban is a direct, selective and reversible active site thrombin inhibitor derived from L-arginine. It is a representative of a new class of antithrombotic drugs which offer inhibition of clot-bound as well as fluid-phase thrombin. Argatroban is characterised by favourable pharmacokinetics (beta-elimination half-time approximately 40-50 min) undergoing hepatic metabolism and mainly biliary excretion. Renal impairment will not result in altered or delayed elimination. For many years, argatroban has been used in Japan and in the United States and is approved by the FDA for anticoagulation in patients with heparin-induced thrombocytopenia (HIT type II). The ease of monitoring with the activated partial thromboplastin time, lack of induction of antibodies and adequate safety in renal failure patients, make this drug a favourable mode therapy in comparison with other anticoagulants such as lepirudin or heparinoids. Since June 2005 argatroban has been approved in Germany for the treatment of patients with HIT type II. The main characteristics of the drug with special considerations for anaesthesiologists and intensive care physicians are presented in this review.
Kleinschmidt
S
S
Klinik für Anaesthesiologie, Intensivmedizin und Schmerztherapie, Universitätsklinikum des Saarlandes, Homburg (Saar), Germany. aiskle@uniklinik-saarland.de
Stephan
B
B
Pindur
G
G
Bauer
C
C
D000758:Anesthesia; D000925:Anticoagulants / Q000009:adverse effects; D000991:Antithrombins / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001120:Arginine / Q000031:analogs & derivatives; D003331:Coronary Vessels / Q000601:surgery; D003422:Critical Care; D005112:Extracorporeal Circulation / Q000009:adverse effects; D006493:Heparin / Q000009:adverse effects; D006801:Humans; D010875:Pipecolic Acids / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D010975:Platelet Aggregation Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D012121:Respiration, Artificial; D013449:Sulfonamides; D013921:Thrombocytopenia / Q000139:chemically induced / Q000188:drug therapy
D000925:Anticoagulants; D000991:Antithrombins; D010875:Pipecolic Acids; D010975:Platelet Aggregation Inhibitors; D013449:Sulfonamides; D006493:Heparin; D001120:Arginine; C031942:argatroban