Heparin and low molecular weight heparin: background and pharmacology.
The various LMWHs available for therapeutic use have multiple mechanisms of action, most of which are similar to the mechanisms of UH. The relative potencies of expression of the mechanisms differ between LMWH and UH and among specific LMWHs. The pharmacokinetics of LMWHs and UH are often measured according to the results of anti-Xa assays, although the correlation between anti-Xa levels and the antithrombotic activities of the drugs is questionable. Animal models of thrombosis give some information regarding the antithrombotic efficacy of different LMWHs when compared with UH and with other LMWHs, but the results are not directly applicable to human thrombosis. Unfortunately, no single measure of antithrombosis has been developed in humans whereby the potencies of LMWHs, UH, and other new anticoagulants can be directly compared. Large clinical outcome studies are expensive and difficult to carry out. Perhaps for this reason, different subcutaneous LMWHs have not been compared with each other in this format. Various LMWHs have demonstrated equivalent efficacy and safety when compared with intravenous UH and high-dose subcutaneous UH, and it is reasonable to assume that there would not be large differences in efficacy and safety among different agents. The superiority of one subcutaneous regimen over another can be confirmed (or refuted) only by the performance of well-planned clinical studies.
Morris
Timothy A
TA
Division of Pulmonary and Critical Care Medicine, University of California, San Diego Medical Center, 200 West Arbor Drive, San Diego, CA 92103-8378, USA. tlmorris@ucsd.edu
D000818:Animals; D000925:Anticoagulants / Q000493:pharmacokinetics / Q000494:pharmacology; D015951:Factor Xa / Q000187:drug effects / Q000378:metabolism; D005343:Fibrinolytic Agents / Q000493:pharmacokinetics / Q000494:pharmacology; D006493:Heparin / Q000493:pharmacokinetics / Q000494:pharmacology; D006495:Heparin, Low-Molecular-Weight / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D013917:Thrombin / Q000187:drug effects / Q000378:metabolism; D020246:Venous Thrombosis / Q000188:drug therapy
D000925:Anticoagulants; D005343:Fibrinolytic Agents; D006495:Heparin, Low-Molecular-Weight; D006493:Heparin; D013917:Thrombin; D015951:Factor Xa