Fields of Applications

Central components of the therapeutic actions of pentosan polysulfate sodium are due to its early development antithrombotic and antilipemic effects. which can be viewed as acting in concert with the primary antithrombotic actions ([1]). Finally, hypercholesterolemic patients show evidence of increased platelet activity when compared with normocholesterolemic patients.
Further properties of pentosan polysulfate sodium have been demonstrated in studies demonstrating anti-inflammatory, antiviral, and anticarcinogenic effects, antihistamine activity, and inhibition of elastase. The antithrombotic effects of pentosan polysulfate sodium are based on effects on platelet function, anticoagulant effects, and fibrinolytic effects.

Pentosan polysulfate sodium inhibits the aggregation of blood platelets in response to collagen and ADP. However, it inhibits aggregation as far as thrombin is concerned ([2]-[3]). This effect, less pronounced than that of heparin, makes pentosan polysulfate sodium a candidate for the treatment and prevention of acute coronary syndromes. The effect of pentosan polysulfate sodium on blood coagulation is mainly due to its influence on the clotting factor Xa. This factor and its formation in the endogenous coagulation cascade are inhibited through a mechanism which is independent from AT-III ([4], [5]). This process also involves an interaction with factor VIIIa. Furthermore, pentosan polysulfate sodium is able to inhibit activation of clotting factor V. pentosan polysulfate sodium has only a weak inhibitory action on thrombin. ([6], [4]-[7]). The most important anticoagulant effects of pentosan polysulfate sodium are mediated by AT-III-independent mechanisms.

The lipolytic effect of  pentosan polysulfate sodium is based on the release of lipoproteinlipase. In patients with increased blood lipid levels, the drug acts to decrease total cholesterol, triglycerids and beta-lipoprotein concentrations improving the beta/alpha-lipoprotein relation ([8], [9]).

References

1) Plana, J. and P. Jones, The use of statins in acute coronary syndromes: The mechanisms behind the outcomes. Curr Atheroscler Rep., 2001. 3(5): p. 355-64.
2) Frandoli, G., et al., Action on fibrinolysis and platelet aggregation of a synthetic, heparin-like sulfated polyanion (SP 54) given orally and parenterally, as related to lipidic fractions. Trials on long-term prophylactic treatment under double-blind conditions. Arzneimittel-Forschung, 1972a. 22(4): p. 759-63.
3) Kollár, L., et al., Internal carotid stent implantation with angioscopic control. Acta chirurgica Hungarica, 1997. 36(1-4): p. 168-9.
4) Fischer, A.M., T.W. Barrowcliffe, and D.P. Thomas, A comparison of pentosan polysulphate (SP54) and heparin. I: Mechanism of action on blood coagulation. Thromb Haemost, 1982a. 47(2): p. 104-8.
5) Fischer, A.M., et al., A comparison of pentosan polysulphate and heparin. II: Effects of subcutaneous injection. Thromb Haemost, 1982b. 47(2): p. 109-13.
6) Vinazzer, H., S. Haas, and A. Stemberger, Influence on the clotting mechanism of sodium pentosan polysulfate (SP54) in comparison to commercial beef lung sodium heparin. Thromb Res, 1980. 20(1): p. 57-68.
7) Ghosh, P., The pathobiology of osteoarthritis and the rationale for the use of pentosan polysulfate for its treatment. Semin Arthritis Rheum, 1999. 28(4): p. 211-67.
8) Gaffney, P.J. and N.A. Marsh, The effect of pentosan polysulphate (SP54) on the human fibrinolytic system. Folia Haematol Int Mag Klin Morphol Blutforsch, 1986. 113(1-2): p. 262-71.
9) Barrowcliffe, T.W., et al., Anticoagulant activities of pentosan polysulphate (Hemoclar) due to release of hepatic triglyceride lipase (HTGL). Thromb Haemost, 1986. 56(2): p. 202-6.