Premium
Safety and pharmacokinetics of the low molecular weight heparinoid Org 10172 administered to healthy elderly volunteers.
Author(s) -
Stiekema JC,
Wijnand HP,
Dinther TG,
Moelker HC,
Dawes J.,
Vinchenzo A.,
Toeberich H.
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb05333.x
Subject(s) - heparinoid , chemistry , pharmacokinetics , bioavailability , low molecular weight heparin , pharmacology , thrombin , antithrombin , heparin , medicine , biochemistry , platelet
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).