Abstract
This report summarizes the results of some of the studies that have evaluated the
pharmacokinetic, pharmacodynamic, anticoagulant, and antithrombotic properties of
Sulodexide, which consists of a mixture of electrophoretically fast moving heparin
(80% of the mass) and dermatan sulfate (the balance), with an average product (Mr)
<8000. The low molecular weight (Mr) of the constituents of Sulodexide would predict
that the product has the high bioavailability associated with low-Mr heparin and low-Mr
dermatan sulfate. Given orally, subcutaneously, or by intravenous injection, Sulodexide
exhibits antithrombotic and profibrinolytic properties in several animal models of
venous and arterial thrombosis and has relatively high affinity for endothelial (and
possibly other) cells. Additionally, in a large multicenter clinical trial involving
3986 patients who had recovered from acute myocardial infarction, oral Sulodexide
was associated with a 32% reduction in death and a significant reduction of left ventricular
thrombus formation. Compared with heparin, low-Mr heparin, and unfractionated and
low-Mr dermatan sulfates, the doses of Sulodexide required for antithrombotic efficacy
suggest that the combination of heparin and dermatan sulfate in Sulodexide provides
a more effective antithrombotic mechanism than heparin/low-Mr heparins (which catalyze
the antiprotease actions of antithrombin III) or dermatan sulfate/low-Mr dermatan
sulfate (which catalyze thrombin inhibition by heparin cofactor II).
Keywords:
Sulodexide - heparin - dermatan sulfates - profibrinolytic
