The anticoagulant effect of heparinoid Org 10172 during haemodialysis: an objective assessment.
The heparinoid of natural origin Org 10172 has anti-factor Xa activity but minimal anti-thrombin activity, and little effect upon broad spectrum assays such as the KCCT in vitro. Its anticoagulant effects have been compared to those of commercial heparin in 7 patients undergoing haemodialysis for chronic renal failure. Commercial heparin was administered in a dose (5,000 iu bolus + 1,500 iu/hour continuous iv infusion) previously shown to inhibit fibrin formation during haemodialysis. This produced mean anti-factor Xa levels in plasma between 0.7-1.0 iu/ml and largely suppressed fibrin formation for 5 h dialysis measured as mean FPA levels in plasma. Administration of Org 10172 as a bolus of 1,350 anti-factor Xa u or 2,000-2,400 anti-factor Xa u produced plasma anti-factor Xa levels of less than 0.5 u/ml and allowed fibrin clot and FPA generation during dialysis. Org 10172 administered as a bolus dose of 4,000-4,800 anti-factor Xa u produced mean anti-factor Xa levels of greater than 0.5 u/ml, allowed dialysis of 6 patients for 5 h and appreciably suppressed FPA generation during dialysis, with little effect on the KCCT. It is concluded that the anti-factor Xa activity of Org 10172 may reflect its ability to inhibit fibrin during dialysis and that single bolus injection of Org 10172 may be a useful alternative method of achieving anticoagulation.
D000925:Anticoagulants / Q000494:pharmacology; D002809:Chondroitin Sulfates; D003871:Dermatan Sulfate; D005069:Evaluation Studies as Topic; D005170:Factor X / Q000037:antagonists & inhibitors; D015951:Factor Xa; D005344:Fibrinopeptide A / Q000032:analysis; D006025:Glycosaminoglycans / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D006493:Heparin / Q000627:therapeutic use; D006497:Heparan Sulfate; D006801:Humans; D007275:Injections, Intravenous; D007676:Kidney Failure, Chronic / Q000188:drug therapy; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D006435:Renal Dialysis
D000925:Anticoagulants; D002809:Chondroitin Sulfates; D003871:Dermatan Sulfate; D005170:Factor X; D015951:Factor Xa; D005344:Fibrinopeptide A; D006025:Glycosaminoglycans; D006493:Heparin; D006497:Heparan Sulfate; C035838:danaparoid