Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat

Thrombosis Research

Volumn 94, Issue 3, 1999, Pages 187-197

  Elg, Margareta ^a   Gustafsson, David ^a   Carlsson, Stefan ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

Arterial thrombosis; Bleeding time; Heparin; Inogatran; Melagatran; Rat; Warfarin

Indexed keywords

BLOOD CLOTTING FACTOR 10; BLOOD CLOTTING FACTOR 7; BLOOD CLOTTING FACTOR 9; HEPARIN; INOGATRAN; MELAGATRAN; PROTEIN C; PROTEIN S; PROTHROMBIN; WARFARIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; ARTICLE; BLEEDING TIME; BLOOD CLOTTING; DOSE RESPONSE; DRUG EFFECT; DRUG POTENCY; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; PROTEIN SYNTHESIS INHIBITION; RAT; THROMBOSIS;

EID: 0033135457     PISSN: 00493848     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0049-3848(98)00213-8     Document Type: Article

References (27)

1. Lindahl U., Lidholt K., Spillmann D., Kjellen L. More to "heparin" than anticoagulation. Thromb Res. 75:1994;1-32.
2. Hirsh J., Raschke R., Warkentin T.E., Dalen J.E., Deykin D., Poller L. Heparin. Mechanism of action, pharmacokinetics, dosing considerations, monitoring, efficacy, and safety Chest. 108:1995;258S-275S.
3. Hirsh J., Dalen J.E., Deykin D., Poller L., Bussey H. Oral anticoagulants. Mechanism of action, clinical effectiveness, and optimal therapeutic range. Chest. 108:1995;231S-246S.
4. Hirsh J., Ginsberg J., Marder V. Anticoagulant therapy with coumarin agents. Colman R.W., Hirsh J., Marder V.J., Salzman E.W. Haemostasis and Thrombosis. Basic Principles and Clinical Practice:1994;1567-1583 J.B. Lippincott Company, Philadelphia.
5. Stirling Y. Warfarin-induced changes in procoagulant and anticoagulant proteins. Blood Coagul Fibrinolysis. 6:1995;361-373.
6. Lind S.E., Callas P.W., Golden E.A., Joyner K.A. Jr., Ortel T.L. Plasma levels of factors II, VII and X and their relationship to the international normalised ratio during chronic warfarin therapy. Blood Coagul Fibrinolysis. 8:1997;48-53.
7. Brigden M.L. Oral anticoagulant therapy. Practical aspects of management Postgrad Med. 99:1996;81-94.
8. Bush L.R. Argatroban, a selective, potent thrombin inhibitor. Cardiovasc Drug Rev. 9:1991;247-263.
9. Markwardt F. The development of hirudin as an antithrombotic drug. Thromb Res. 74:1994;1-23.
10. Eriksson B.I., Ekman S., Kälebo P., Zachrisson B., Bach D., Close P. Prevention of deep-vein thrombosis after total hip replacement. Direct thrombin inhibition with recombinant hirudin, CGP 39393 Lancet. 347:1996;635-639.
11. Challapalli R., Lefkovits J., Topol E.J. Clinical trials of recombinant hirudin in acute coronary syndromes. Coron Artery Dis. 7:1996;429-437.
12. Gustafsson D., Elg M., Lenfors S., Börjesson I., Teger-Nilsson A.C. Effects of inogatran, a new low-molecular-weight thrombin inhibitor, in rat models of venous and arterial thrombosis, thrombolysis and bleeding time. Blood Coagul Fibrinolysis. 7:1996;69-79.
13. Gustafsson D., Antonsson T., Bylund R., Eriksson U., Gyzander E., Nilsson I., Elg M., Mattsson C., Deinum J., Pehrsson S., Karlsson O., Nilsson A., Sörensen H. Effects of melagatran, a new low molecular weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb Haemost. 79:1997;110-118.
14. Eriksson H, Eriksson UG, Frison L, Hansson PO, Held P, Holmström M, Hägg A, Jonsson T, Lapidus L, Leijd B, Stockelberg D, Säfwenberg U, Taghavi A, Thorsén M. Pharmacokinetics and pharmacodynamics of melagatran, a novel synthetic low molecular weight thrombin inhibitor, in patients with acute deep vein thrombosis. Thromb Haemost. In Press 1999.
15. Elg M., Gustafsson D., Deinum J. The importance of inhibition kinetics for the effect of thrombin inhibitors in a rat model of arterial thrombosis. Thromb Haemost. 78:1997;1286-1292.
16. Teger-Nilsson A, Bylund R. Preparation of peptide derivates as thrombin inhibitors. Patent Application WO9311152-A1 1991.
17. Antonsson K, Bylund R, Gustafsson D, Nilsson I. New peptide derivatives. Patent Application WO9429336-A 1993.
18. Palareti G., Legnani C. Warfarin withdrawal. Pharmacokinetic-pharmacodynamic considerations. Clin Pharmacokinet. 30:1996;300-313.
19. Schumacher W.A., Steinbacher T.E., Heran C.L., Megill J.R., Durham S.K. Effects of antithrombotic drugs in a rat model of aspirin-insensitive arterial thrombosis. Thromb Haemost. 69:1993;509-514.
20. Eriksson B., Carlsson S., Halvarsson M., Risberg B., Mattsson C. Antithrombotic effect of two low molecular weight thrombin inhibitors and a low molecular weight heparin in a caval vein thrombosis model in the rat. Thromb Haemost. 78:1997;1404-1407.
21. Weitz J.I., Hudoba M., Massel D., Maraganore J., Hirsh J. Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors. J Clin Invest. 86:1990;385-391.
22. Hogg P.J., Jackson C.M. Fibrin monomer protects thrombin from inactivation by heparin-antithrombin III. Implications for heparin efficacy Proc Natl Acad Sci USA. 86:1989;3619-3623.
23. Potzsch B., Hund S., Madlener K., Unkrig C., Muller-Berghaus G. Monitoring of recombinant hirudin. Assessment of a plasma-based ecarin clotting time assay Thromb Res. 86:1997;373-383.
24. Berry C., Lunven C., Girardot C., Lechaire I., Girard D., Charles M.C., Ferrari P., O'Brien D. Ecarin clotting time. A predictive coagulation assay for the antithrombotic activity of argatroban in the rat Thromb Haemost. 79:1998;228-233.
25. Lind S.E. The bleeding time does not predict surgical bleeding. Blood. 77:1991;2547-2552.
26. Dejana E., Callioni A., Quintana A., de Gaetano G. Bleeding time in laboratory animals. II. A comparison of different assay conditions in rats. Thromb Res. 15:1979;191-197.
27. Ansell J.E. Anticoagulation management as a risk factor for adverse events. Ground for improvement J Thromb Thrombolysis. 5:1998;S13-S18.