ABSTRACT
Andrew Blann has reviewed in Chapter 3 the heparins, coumarin derivatives, and the antiplatelet drug aspirin. These drugs have served patients with arterial or venous thrombosis excellently during the last decades. However, they also have major drawbacks, which may at least in part be overcome by novel classes of anticoagulants or antiplatelet drugs. Attributes of ideal anticoagulants are listed in Table 15.1. This chapter shall mainly focus on the more recently developed anticoagulants which have already been introduced into clinical practice, including fondaparinux, hirudins, ximelagatran, and clopidogrel. It will also provide some perspective on anticoagulants that have entered the clinical drug development process but will deliberately exclude those which are currently in an experimental phase of development. An excellent review of these drugs has been published recently [1], Additionally, this chapter will also briefly touch on the use of glycoprotein (Gp) IIb/IIIa inhibitors and the use of novel fibrinolytic agents. After reviewing the tissue factor inhibitors, we will step down the coagulation ladder to Factor Xa inhibitors, thrombin inhibitors, discuss the use of endogenous
Table 15.1 Attributes of an ideal anticoagulant Orally
admin. Fixed dose
Rapid on/offset
Predi ctable
PK
No routine coagu lation
monitoring
Low food/ drug
interaction
No thrombo cytopenia
Inhibits free and
clotb ound
thrombin LMWH X X X X X
UFH X
Fondaparinux X Xa X X X X
Warfarin X X X X X X X
Ximelagatran X X X X X X X X
a Due to the relatively long half-life, fondaparinux does not have a rapid offset of action.
