Pharmacology of recombinant hirudin

Seminars in Thrombosis and Hemostasis

Volumn 28, Issue 5, 2002, Pages 415-423

  Nowak, Götz ^a  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

Author keywords

ECT; Pharmacokinetics; Pharmacology; r hirudin

Indexed keywords

ANTICOAGULANT AGENT; DESULFATOHIRUDIN; ECARIN; HEPARIN; LEPIRUDIN; RECOMBINANT HIRUDIN; THROMBIN INHIBITOR;

ANTICOAGULANT THERAPY; BLEEDING; BLOOD CLOTTING TIME; CARDIOPULMONARY BYPASS; CLINICAL PRACTICE; DEEP VEIN THROMBOSIS; DRUG INDICATION; DRUG METABOLISM; DRUG MONITORING; HEMODIALYSIS; HUMAN; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; REVIEW; THROMBOCYTOPENIA; THROMBOEMBOLISM; THROMBOSIS PREVENTION;

AMINO ACID SEQUENCE; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FIBRINOLYTIC AGENTS; GENETIC ENGINEERING; HIRUDIN THERAPY; HIRUDINS; HUMANS; LEECHES; MOLECULAR SEQUENCE DATA; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; RECOMBINANT PROTEINS; THROMBOSIS; TIME FACTORS;

EID: 0036800881     PISSN: 00946176     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-2002-35293     Document Type: Review

References (56)

1. De la Llosa P, Tertrin C, Justisz M. Composition en acides aminés de l'hirudin. Identification du résidu N-terminal. Bulletin de la Societé de Chimie Biologique 1963;45:69-74
2. De la Llosa P, Tertrin C, Justisz M. L'enchainemant C-terminal de l'hirudin. Biochim Biophys Acta 1964;93:40-44
3. Dodt J, Müller HP, Seemüller U, Chang JY. The complete amino acid sequence of hirudin, a thrombin specific inhibitor. FEBS Lett 1984;162:180-183
4. Johnson P, Sze P, Winant R, Payne PW, Lazar JB. Biochemistry and genetic engineering of hirudin. Semin Thromb Hemost 1989;15:302-315
5. Bagdy D, Barabas E, Graf L, Peterson TE, Magnusson S. Hirudin. In: Lorand L, ed. Methods in Enzymology: Proteolytic Enzymes, Vol. 19. New York: Academic Press; 1976:924-932
6. Scharf M, Engels J, Tripier D. Primary structures of new "isohirudins." FEBS Lett 1989;225:105-110
7. Walsmann P, Markwardt F. Biochemische und pharmakologische aspekte des thrombininhibitors hirudin. Pharmazie 1981;26:653-660
8. Rydel TJ, Ravichandran KG, Tulinsky A, et al. The structure of a complex of recombinant hirudin and human α-thrombin. Science 1990;249:277-280
9. Stone S, Hofsteenge J. The kinetics of the inhibition of thrombin by hirudin. Biochemistry 1986;25:4622-4628
10. Nowak G, Markwardt F, Fink E. Pharmacokinetic studies with recombinant hirudin in dogs. Folia Haematol Leipzig 1988;115:70-74
11. Markwardt F, Fink G, Kaiser B, et al. Pharmacological survey of recombinant hirudin. Pharmazie 1988;43:202-207
12. Markwardt F, Hauptmann J, Nowak G, Klessen C, Walsmann P. Pharmacological studies on the antithrombotic action of hirudin in experimental animals. Thromb Haemost 1982;47:226-229
13. Markwardt F, Kaiser B, Nowak G. Studies on antithrombotic effects of recombinant hirudin. Thromb Res 1989;54:377-388
14. Lindhoff-Last E, Willeke A, Mosch G, et al. Hirudin treatment in a breastfeeding woman. Lancet 2000;355:467-468
15. Markwardt F, Nowak G, Stürzebecher J, Vogel G. Clinico-pharmacological studies with recombinant hirudin. Thromb Res 1988;52:393-400
16. Markwardt F, Nowak G, Stürzebecher J, et al. Pharmacokinetics and anticoagulant effect of hirudin in man. Thromb Haemost 1984;52:160-163
17. Nowak G, Bucha E, Göök T, Prasa D, Thieler H. Pharmakokinetik von hirudin bei gestórter nierenfunktion. Hämostaseologie 1991;11:152-157
18. Nowak G, Bucha E, Göök T, Thieler M, Markwardt F. Pharmacology of r-hirudin in renal impairment. Thromb Res 1992;66:707-715
19. Bucha E, Markwardt F, Nowak G. Hirudin in haemodialysis. Thromb Res 1990;60:445-455
20. Nowak G, Bucha E, Brauns I, Czerwinski R. Anticoagulation with r-hirudin in regular haemodialysis with heparin-induced thrombocytopenia (HIT II). Wien Klin Wochenschr 1997;109:354-358
21. Markwardt F, Nowak G, Bucha E. Hirudin as anticoagulant in experimental hemodialysis. Haemostasis 1991;21(Suppl 1):149-155
22. Stringer KA, Lindenfield J. Hirudins: Antithrombin anticoagulants. Ann Pharmacother 1992;26:1535-1540
23. Bucha E, Nowak G, Markwardt F. Prevention of experimental coronary thrombosis by hirudin. Folia Haematol 1988;115:52-58
24. Heras M, Chesebro JH, Webster MWI, et al. Hirudin, heparin or placebo during deep arterial injury in the pig: The in vivo role of thrombin in platelet-mediated thrombosis. Circulation 1990;82:1476-1484
25. Markwardt F. Past, present and future of hirudin. Haemostasis 1991;21(Suppl 1):11-26
26. Pötzsch B, Iversen S, Riess FC, et al. Recombinant hirudin as an anticoagulant in open-heart surgery: A case report. Ann Hematol 1993;68(Suppl 2):A46 (Abst)
27. Pötzsch B, Madlener K, Silage C, et al. Monitoring of r-hirudin anticoagulation during cardiopulmonary bypass - Assessment of the whole blood achorion clotting time. Throb Hammiest 1997;77:920-925
28. Broaden HI, Radziwon P, Eschenfelder V, Müller-Peltzer H, Esslinger HU. PEG-hirudin and acetylsalicylic acid show a strong interaction on bleeding time. Ann Haematol 1996;72:53 (Abst)
29. Meyer BH, Luus HG, Müller FO, Badenhorst PN, Röthig H-J. The pharmacology of recombinant hirudin, a new anti-coagulant. S Afr Med J 1990;78:268-270
30. Weitz JI, Hudoba M, Massel D, Maragonore J, Hirsh J. Clotbound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors. J Clin Invest 1990;86:385-391
31. Antman EM for the TIMI 9B investigators. Hirudin in acute myocardial infarction. Thrombolysis and thrombin inhibition in myocardial infarction (TIMI) 9B trial. Circulation 1996;94:911-921
32. Canon CP, McCabe CH, Henry TD, et al for the TIMI-5 investigators. Hirudin reduces reocclusion compared to heparin following thrombolysis in acute myocardial infarction. J Am Coll Cardiol 1993;21:136a (Abst)
33. Moia M, Schiele F, Walker M, et al. Treatment of acute deep vein thrombosis (DVT) by subcutaneous r-hirudin (HBW 023): A multicenter study. Thromb Haemost 1995;73:1456 (Abst)
34. Parent F, Bridey F, Dreyfus M, et al. Treatment of severe venous thrombo-embolism with intravenous hirudin (HBW-023). An open pilot study. Thromb Haemost 1993;70:386-388
35. Rupprecht HJ, Terres W, Özbek C, et al. Recombinant hirudin (HBW 023) prevents troponin release after coronary angioplasty in patients with unstable angina. J Am Coll Cardiol 1995;26:1637-1642
36. Hermann JPR, Kutryk MJV, Serruys PW. Clinical trials of direct thrombin inhibitors during invasive procedures. Thromb Haemost 1997;78:367-376
37. The Global Use of Strategies To Open occluded coronary arteries (GUSTO) IIb investigators. A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes. N Engl J Med 1996;335:775-782
38. Walenga JM, Pifarré R. Hirudin as an anticoagulant in cardiopulmonary bypass. In: Pifarré R, ed. New Anticoagulants for the Cardiovascular Patient. Philadelphia, PA: Hanley & Belfus; 1997:175-186
39. Zeymer U, von Essen R, Tebbe U, et al. Frequency of "optimal anticoagulation" for acute myocardial infarction after thrombolysis with front-load recombinant tissue-type plasminogen activator and conjunctive therapy with recombinant hirudin (HBW 023). Am J Cardiol 1995;76:997-1001
40. Zoldhelyi P, Webster MWI, Fuster V, et al. Recombinant hirudin in patients with chronic, stable coronary artery disease. Safety, half-life, and effect on coagulation parameters. Circulation 1993;88:2015-2022
41. Greinacher A. Lepirudin for the treatment of heparin-induced thrombocytopenia: a prospective study. Blood 1998;92:1490 (Abst)
42. Schiele F, Vuillemenot A, Kramarz P, et al. Use of recombinant hirudin as antithrombotic treatment in patients with heparin-induced thrombocytopenia. Am J Hematol 1995;50:20-25
43. Schmidt OH, Lang W. Heparin-induced thrombocytopenia with thromboembolic arterial occlusion treated with recombinant hirudin. N Engl J Med 1997;337:1389
44. Agnelli G, Snaglia F. Recombinant hirudin in the prevention of venous thromboembolism in patients undergoing elective hip surgery. Semin Thromb Hemost 1997;22:143-148
45. Eriksson BI, Ekman S, Kälebo P, et al. Prevention of deep-vein thrombosis after total hip replacement: Direct thrombin inhibition with recombinant hirudin, CGP 39393. Lancet 1996;347:635-639
46. Eriksson B, Kälebo P, Ekman S, et al. Direct thrombin inhibition with Rec-hirudin CGP 39393 as prophylaxis of thromboembolic complications after total hip replacement. Thromb Haemost 1994;72:227-231
47. Buchwald AB, Sandrock D, Unterberg CA, et al. Platelet and fibrin deposition on coronary stents in minipigs: Effects of hirudin versus heparin. J Am Coll Cardiol 1993;21:249-254
48. Haskel EJ, Prager NA, Sobel BE, Abenschein DR. Relative efficacy of antithrombin compared with antiplatelet agents in accelerating coronary thrombolysis and preventing early reocclusion. Circulation 1991;83:1048-1056
49. Bichler J, Gemmerli R, Fritz H. Studies for revealing a possible sensitization to hirudin after repeated intravenous injections in baboons. Thromb Res 1991;61:39-51
50. Eichler P, Friesen HJ, Lubenow N, Jaeger B, Greinacher A. Antihirudin antibodies in patients with heparin-induced thrombocytopenia treated with lepirudin: Incidence, effects on aPTT, and clinical relevance. Blood 2000;96:2373-2378
51. Brüggener E, Walsmann P, Markwardt F. Neutralization of hirudin anticoagulant action by DIP-thrombin. Pharmazie 1989;44:648-649
52. Tripodi A, Chantarangkul V, Arbini AA, Moia M, Manucci PM. Effects of hirudin on activated partial thromboplastin time determined with ten different reagents. Thromb Haemost 1993;70:286-288
53. Spinner S, Stöffler G, Fink E. Quantitative enzyme-linked immunosorbent assay (ELISA) for hirudin. J Immunol Methods 1988;87:79-83
54. Nowak G. Monitoring of the action of antithrombin agents by ecarin clotting time. In: Pifarré R, ed. New Anticoagulants for the Cardiovascular Patient. Philadelphia, PA: Hanley & Belfus; 1997:530-550
55. Nowak G, Bucha E. Quantitative determination of hirudin in blood and body fluids. Semin Thromb Hemost 1996;22:197-202
56. Nowak G, Bucha E, Hoffmann J. Verfahren zur Bestimmung von Hirudin und synthetischen Thrombininhibitoren. DPA 4203980.0 Deutsches Patentamt, 1992