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Argatroban

Pharmakologische Eigenschaften und anästhesiologische Aspekte

Argatroban

Pharmacological properties and anaesthesiological aspects

  • Klinische Pharmakologie
  • Published:
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Zusammenfassung

Argatroban ist ein direkter, selektiver und reversibler „Active-site-Thrombininhibitor“. Die Substanz leitet sich chemisch vom L-Arginin ab und hemmt sowohl freies als auch bereits fibringebundenes Thrombin. Argatroban hat eine vorteilhafte Pharmakokinetik mit einer β-Eliminationshalbwertszeit von 40–50 min, wird hepatisch metabolisiert, überwiegend biliär eliminiert und kumuliert nicht bei Patienten mit Niereninsuffizienz. In Japan und in den USA ist die Substanz seit mehreren Jahren im klinischen Gebrauch und wurde erfolgreich als Antikoagulans zur koronaren Angioplastie sowie zur extrakorporalen Zirkulation bei herzchirurgischen Eingriffen und bei Nierenersatzverfahren angewendet. Insbesondere bei Patienten mit heparininduzierter Thrombozytopenie (HIT-Typ II), die eine suffiziente und gut steuerbare Antikoagulation benötigen, stellt Argatroban eine attraktive therapeutische Alternative zu den bisher verwendeten Antikoagulanzien, wie Lepirudin oder Heparinoiden, dar. Die Überwachung der Antikoagulation kann mit der aktivierten partiellen Thromboplastinzeit (aPTT) erfolgen. Argatroban ist in Deutschland seit Juni 2005 zur Antikoagulation bei Patienten mit HIT-Typ II zugelassen und somit für das Fachgebiet Anästhesiologie von zunehmender Bedeutung. Die vorliegende Übersicht beschreibt die Pharmakologie von Argatroban, bisherige klinische Erfahrungen sowie mögliche Indikationsgebiete in Anästhesie und Intensivmedizin.

Abstract

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 (β-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.

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Authors and Affiliations

  1. Klinik für Anaesthesiologie, Intensivmedizin und Schmerztherapie, Universitätsklinikum des Saarlandes, Homburg (Saar)

    S. Kleinschmidt & C. Bauer

  2. Abteilung für Klinische Hämostaseologie und Transfusionsmedizin, Universitätsklinikum des Saarlandes, Homburg (Saar)

    B. Stephan & G. Pindur

  3. Klinik für Anaesthesiologie, Intensivmedizin und Schmerztherapie, Universitätsklinikum des Saarlandes, 66421, Homburg/Saar

    S. Kleinschmidt

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  1. S. Kleinschmidt
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  2. B. Stephan
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  3. G. Pindur
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  4. C. Bauer
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Correspondence to S. Kleinschmidt.

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Kleinschmidt, S., Stephan, B., Pindur, G. et al. Argatroban. Anaesthesist 55, 443–450 (2006). https://doi.org/10.1007/s00101-005-0962-7

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  • DOI: https://doi.org/10.1007/s00101-005-0962-7

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