Pharmacological profile of reviparin-sodium.
Clivarin (reviparin-sodium) is a homogeneous low molecular weight heparin (LMWH) as determined by the data obtained in molecular profiling studies. The limited biochemical studies carried out indicate that this LMWH has a specific potency of 124 anti-XA IU/mg and a weaker aPTT activity of approximately 30 U/mg. Assay-dependent neutralization of the in vitro effects of reviparin-sodium were noted. Protamine preparations at equigravimetric concentrations effectively neutralized the aPTT and TT effects; however, Heptest and anti-Xa effects were only partially neutralized. In contrast, heparin's effects were completely neutralized by this agent. PF 4 only partially neutralized the effects of reviparin-sodium. Assay-dependent variations were noted in this study. In comparison with heparin, the haemorrhagic effects of reviparin-sodium were much weaker. Reviparin-sodium produced a dose-dependent antithrombotic action in both the intravenous and subcutaneous studies. This agent also showed sustained activity and better bioavailability characteristics than heparin. Reviparin-sodium exhibited a distinct biochemical and pharmacological profile that may be useful in the optimization of LMWH.
Hoppensteadt
D
D
Loyola University Medical Center, Hemostasis & Thrombosis, Research Laboratories, Maywood, IL 60153.
Jeske
W
W
Fareed
J
J
D000818:Animals; D001682:Biological Availability; D001777:Blood Coagulation / Q000187:drug effects; D002240:Carbohydrate Sequence; D065427:Factor Xa Inhibitors; D006470:Hemorrhage / Q000139:chemically induced; D006495:Heparin, Low-Molecular-Weight / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008969:Molecular Sequence Data; D011516:Prothrombin / Q000037:antagonists & inhibitors; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000188:drug therapy
D065427:Factor Xa Inhibitors; D006495:Heparin, Low-Molecular-Weight; C094240:reviparin; D011516:Prothrombin; C025337:Factor IIa