In vivo neutralization of unfractionated heparin and low-molecular-weight heparin by a novel salicylamide derivative

Clinical and Applied Thrombosis/Hemostasis

Volumn 16, Issue 4, 2010, Pages 377-386

  Kuziej, Jacqueline ^a   Litinas, Evangelos ^a   Hoppensteadt, Debra A ^a   Liu, Dahui ^b   Walenga, Jeanine M ^a   Fareed, Jawed ^a   Jeske, Walter ^a  

^a LOYOLA UNIVERSITY MEDICAL CENTER   (United States)

^b PolyMedix Inc   (United States)

Author keywords

low molecular weight heparins (LMWHs); PMX 60056; protamine sulfate; unfractionated heparin (UFH)

Indexed keywords

BLOOD CLOTTING FACTOR 10A; ENOXAPARIN; HEPARIN; PMX 60056; PROTAMINE SULFATE; PROTHROMBIN A; SALICYLAMIDE; TETRA [ 5 LYSYL AMINO O METHYLSALICYLAMIDE]; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; ARTICLE; BLEEDING; CONTROLLED STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; IN VIVO STUDY; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; RAT; THROMBOSIS;

ANIMALS; ANTICOAGULANTS; DISEASE MODELS, ANIMAL; HEMORRHAGE; HEPARIN; HEPARIN ANTAGONISTS; HEPARIN, LOW-MOLECULAR-WEIGHT; HUMANS; MALE; PROTAMINES; RATS; RATS, SPRAGUE-DAWLEY; THROMBOSIS;

EID: 77954906432     PISSN: 10760296     EISSN: None     Source Type: Journal    
DOI: 10.1177/1076029610366439     Document Type: Article

References (30)

1. Hirsh J., Raschke R. Heparin and low-molecular-weight heparin. Chest 2004 ; 126: 1885-2038.
2. Alban S. Molecular weight-dependent influence of heparin on the form of tissue factor pathway inhibitor circulating in plasma. Semin Thromb Hemost. 2001 ; 27 (5). 503-511.
3. Holmer E., Kurachi K., Soderstrom G. The molecular-weight dependence of the rate-enhancing effect of heparin on the inhibition of thrombin, factor Xa, factor IXa, factor XIa, factor XIIa and kallikrein by antithrombin. Biochem J. 1981 ; 193 (2). 395-400.
4. Khorana AA, Sahni A., Altland OD, et al. Heparin inhibition of endothelial cell proliferation and organization is dependent on molecular weight. Arterioscler Thromb Vasc Biol. 2003 ; 23 (11). 2110-2115.
5. Bray B., Lane DA, Freyssinet JM, et al. Effect of saccharide chain length on thrombin inhibition by heparin cofactor II and by antithrombin. Biochem J. 1989 ; 262 (1). 225-232.
6. Jeske WP, Walenga JM, Fareed J. Differentiating between the low-molecular-weight heparins used for venous thromboembolism treatment and prophylaxis. In: Merli G, ed. Thromb Clin. 2008 ; 2 (3). 8-21.
7. Middeldorp S. Heparin: from animal organ extract to designer drug. Thromb Res. 2008 ; 122 (6). 753-762.
8. Antman EM, McCabe CH, Gurfinkel EP, et al. Enoxaparin prevents death and cardiac ischemic events in unstable angina/non-Q-wave myocardial infarction: results of the thrombolysis in myocardial infarction (TIMI) 11B trial. Circulation. 1999 ; 100 (15). 1593-1601.
9. Cohen M., Demers C., Gurfinkel EP, et al. A comparison of low-molecular-weight heparin with unfractionated heparin for unstable coronary artery disease. N Eng J Med. 1997 ; 337 (7). 447-452.
10. Van Ryn-McKenna J., Cai L., Ofosu FA, Hirsh J., Buchanan MR Neutralization of enoxaparin-induced bleeding by protamine sulfate. Thromb Haemost. 1990 ; 63 (2). 271-274.
11. Gouin-Thibault I., Pautas E., Siguret V. Safety profile of different low-molecular weight heparins used at therapeutic dose. Drug Saf. 2005 ; 28 (4). 333-349.
12. Horrow J. Protamine: a review of its toxicity. Anesth Analg. 1985 ; 64 (3). 348-361.
13. Horrow J. Adverse reactions to protamine. Int Anesthesiol Clin. 1985 ; 23 (3). 133-144.
14. Holst J., Lindblad B., Bergqvist D., et al. The effect of protamine sulphate on plasma tissue factor pathway inhibitor released by intravenous and subcutaneous unfractionated and low molecular weight heparin in man. Thromb Res. 1997 ; 86 (4). 343-348.
15. Godal HC A comparison of two heparin-neutralizing agents: protamine and polybrene. Scand J Lab Clin Invest. 1960 ; 12: 446-457.
16. Weiss WA, Gilman J., Catenacci A., Osterberg A. Heparin neutralization with polybrene administered intravenously. JAMA. 1958 ; 166 (6). 603-607.
17. Haller JA, Ransdell HT, Stowens D., Rubel WF Renal toxicity of polybrene in open heart surgery. J Thorac Cardiovasc Surg. 1962 ; 44: 486-493.
18. Ransdell HT, Hailer JA, Stowens D., Barton PB Renal toxicity of polybrene (hexadimethrine bromide). J Surg Res. 1965 ; 5 (pt 5). 195-199.
19. Dehmer GJ, Fisher M., Tate DA, et al. Reversal of heparin anticoagulation by recombinant platelet factor 4 in humans. Circulation. 1995 ; 91 (8). 2188-2194.
20. Levy JH, Cormack JG, Morales A. Heparin neutralization by recombinant platelet factor 4 and protamine. Anesth Analg. 1995 ; 81 (1). 35-37.
21. Amiral J., Bridey F., Dreyfus M., et al. Platelet factor 4 complexed to heparin is the target for antibodies generated in heparin-induced thrombocytopenia. Thromb Haemost. 1992 ; 68 (1). 95-96.
22. Dietrich CP, Silva ME, Michelacci YM Sequential degradation of heparin in Flavobacterium heparinum. J Biol Chem. 1973 ; 248 (18). 6408-6415.
23. Despotis GJ, Summerfield AL, Joist JH, et al. In vitro reversal of heparin effect with heparinase: evaluation with whole blood prothrombin time and activated partial thromboplastin time in cardiac surgical patients. Anesth Analg. 1994 ; 79 (4). 670-674.
24. Stafford-Smith M., Lefrak EA, Qazi AG, et al. Efficacy and Safety of heparinase I versus protamine in patients undergoing coronary artery bypass grafting with and without cardiopulmonary bypass. Anesthesiology. 2005 ; 103 (2). 229-240.
25. Jeske W., Brubaker A., Liu D., et al. In vitro characterization of the neutralization of unfractionated heparin and low molecular weight heparin by novel salicylamide derivatives. Hämostaseologie. 2008 ; 28: P- 11-04.
26. Jeske W., Iqbal O., Fareed J., Kaiser B. A survey of animal models to develop novel antithrombotic agents. In: Sasahara A, Loscalzo J, eds. New Therapeutic Agents in Thrombosis and Thrombolysis. 2 nd Ed. Boston, MA: Marcel Dekker, Inc, 2003 ; 9-32.
27. Dejana E., Villa S., deGaetano G. Bleeding time in rats: a comparison of different experimental conditions. Thromb Haemost. 1982 ; 48 (1). 108-111.
28. Raake W., Elling H. Rat jugular vein hemostasis-a new model for testing antithrombotic agents. Thromb Res. 1989 ; 53 (1). 73-77.
29. Harenberg J., Siegele M., Dempfle CE, et al. Protamine neutralization of the release of tissue factor pathway inhibitor activity by heparins. Thromb Haemost. 1993 ; 70 (6). 942-945.
30. Turpie A. Pharmacology of the low-molecular-weight heparins. Am Heart J. 1998 ; 135 (6 pt 3 Su). S329 - S335.