Antithrombotic activity, bleeding effect and pharmacodynamics of a succinyl derivative of dermatan sulphate in rabbits

Saivin, Sylvie; Caranobe, C; Petitou, Maurice; Sié, P.; Lormeau, J C; Level, Michel; Crepon, B.; Houin, Georges; Boneu, B

doi:10.1111/j.1365-2141.1992.tb04565.x

Cited by 1 publication

(2 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Indeed,o ral rivaroxaban 3.0mgkg -1 ,nadroparinand fondaparinux were similarly effectivea tr educing thrombin growth in the treatment model. Thenadroparindose waschosen in ordertoobtain therapeutic levels observedinpatients receiving nadroparin for the treatment of venous thrombosis (18)(19)(20).T he fondaparinux dose (42 µg kg -1 )had an equivalent antithrombotic effect to nadroparininthis experimental thrombosis model. It should be noted that fondaparinux 7.5 mg has beenapprovedfor treatment in patients with symptomatic DVTo ra cutep ulmonarye mbolism( 5, 25).…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Prevention and treatment of experimental thrombosis in rabbits with rivaroxaban (BAY 597939) – an oral, direct factor Xa inhibitor

Biemond¹,

Perzborn²,

Friederich³

et al. 2007

Thromb Haemost

View full text Add to dashboard Cite

Current anticoagulant therapies for the prevention and treatment of thromboembolic disorders have many drawbacks: vitamin K antagonists interact with food and drugs and require frequent laboratory monitoring, and heparins require parenteral administration. Oral rivaroxaban (BAY 597939) is a new, highly selective and potent direct factor-Xa (FXa) inhibitor with a predictable pharmacodynamic and pharmacokinetic profile and could therefore be an attractive antithrombotic drug. It was the objective of this study to investigate the antithrombotic efficacy of oral rivaroxaban in two rabbit models of experimental venous thrombosis. In the venous stasis (prevention) model, animals were randomized to receive oral rivaroxaban 0.3, 1.0, 3.0 or 10.0 mg/kg or vehicle control. Thrombosis was induced by jugular vein stasis and injection of thromboplastin into the ear vein. In the venous thrombosis (treatment) model, intravenous (1.0 and 3.0 mg/kg) and oral (3.0 mg/kg) rivaroxaban was compared with intravenous nadroparin (40 U bolus and 20 U/h), fondaparinux (42 microg/kg) and vehicle control. Thrombus growth was assessed by measuring the accretion of radiolabelled fibrinogen into preformed clots in the jugular veins. Bleeding was assessed using an ear bleeding model. In the prevention model, rivaroxaban reduced thrombus formation dose-dependently (calculated ED(50) 1.3 mg/kg). In the treatment model, oral rivaroxaban (3.0 mg/kg) reduced thrombus growth to a similar extent to intravenous rivaroxaban (1.0 mg/kg), nadroparin and fondaparinux. Oral rivaroxaban did not prolong bleeding time. In conclusion, the orally available selective, direct FXa inhibitor rivaroxaban is effective in the prevention and treatment of venous thrombosis in two well-established models of experimental thrombosis.

show abstract

Section: Discussionmentioning

confidence: 99%

“…The antithromboticactivity of rivaroxaban wasdeterminedina venous stasis thrombosis model (prevention model) usingmethodsdescribed previously,with some modifications (16)(17)(18). The animals were anesthetized by intramuscular (i.m.)…”

Section: Prevention Model:venous Stasis Modelmentioning

confidence: 99%