The effect of pentosan polysulphate (SP54) on the fibrinolytic enzyme system--a human volunteer and experimental animal study.
Pentosan polysulphate causes an increase in plasminogen activator activity in plasma both after oral ingestion and after subcutaneous injection. The effect is greatest after 3 h and has disappeared by 6 h. Repeat doses by mouth over 5 days elicit a similar response. The recorded increase in activity is due largely to the release of tissue-type plasminogen activator (tPA) from the endothelium according to the antigen assay although there could be a small contribution from Factor XII-related "intrinsic" fibrinolysis induced in vitro. SP54 enhances activity ex vivo by a non-specific surface effect, and this phenomenon may contribute the increased levels of activity seen in vitro. Administration of SP54 to animals elicits a similar increase in activator activity, the intramuscular route being slightly more effective. Results with an inferior vena cava thrombosis model in the rat suggest that pentosan polysulphate may induce a thrombolytic effect.
Marsh
N A
NA
Peyser
P M
PM
Creighton
L J
LJ
Mahmoud
M
M
Gaffney
P J
PJ
D000284:Administration, Oral; D000328:Adult; D000818:Animals; D005260:Female; D005342:Fibrinolysis / Q000187:drug effects*; D006801:Humans; D007279:Injections, Subcutaneous; D008297:Male; D010426:Pentosan Sulfuric Polyester / Q000008:administration & dosage / Q000494:pharmacology*; D011134:Polysaccharides / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013927:Thrombosis / Q000188:drug therapy; D010959:Tissue Plasminogen Activator / Q000378:metabolism; D014682:Vena Cava, Inferior
D011134:Polysaccharides; D010426:Pentosan Sulfuric Polyester; D010959:Tissue Plasminogen Activator