Safety and pharmacokinetics of the low molecular weight heparinoid Org 10172 administered to healthy elderly volunteers.
1. In a cross-over study a new low molecular weight heparinoid Org 10172 was administered to 12 elderly male and female volunteers. It was well tolerated and no adverse effects occurred. 2. The absolute bioavailability of Org 10172 as measured by plasma anti-Xa activity, glycosaminoglycuronans with no affinity to antithrombin III (NoA-GAG) and thrombin generation inhibiting activity approached 100% in both sexes. 3. The half-life of elimination of its anti-Xa activity (19.2 +/- 6.1 h) was similar to that found previously in young volunteers. Org 10172 was further characterised by a rapid disappearance from the circulation of its anti-thrombin activity (t1/2 1.8 +/- 0.6 h) and of the NoA-GAG (t1/2 3.5 +/- 2.1 h). 4. Its thrombin generation inhibiting activity was of intermediate duration (t1/2 elimination 6.2 +/- 4.0 h).
Stiekema
J C
JC
Scientific Development Group, Organon International B.V., Oss, The Netherlands.
Wijnand
H P
HP
Van Dinther
T G
TG
Moelker
H C
HC
Dawes
J
J
Vinchenzo
A
A
Toeberich
H
H
D000279:Administration, Cutaneous; D000368:Aged; D001682:Biological Availability; D001777:Blood Coagulation / Q000187:drug effects; D002809:Chondroitin Sulfates; D002986:Clinical Trials as Topic; D003871:Dermatan Sulfate; D005260:Female; D006025:Glycosaminoglycans / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D006207:Half-Life; D006496:Heparinoids / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D006497:Heparan Sulfate; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008875:Middle Aged; D011897:Random Allocation; D012016:Reference Values
D002809:Chondroitin Sulfates; D003871:Dermatan Sulfate; D006025:Glycosaminoglycans; D006496:Heparinoids; D006497:Heparan Sulfate; C035838:danaparoid