Hirudin and Derivatives as Anticoagulant Agents

• References

• 1 Markwardt F. Untersuchungen über Hirudin. Naturwissenschaften. 1955; 42: 537-38
• 2 Markwardt F. Untersuchungen über den Mechanismus der blutgerinnungshemmenden Wirkung des Hirudins. Naunyn Schmiedebergs Arch. Pharmacol. 1956; 229: 389-99
• 3 Markwardt F. Die Isolierung und chemische Charakterisierung des Hirudins. Hoppe-Seylers Z. Physiol. Chem. 1957; 308: 147-56
• 4 Markwardt F, Walsmann P. Die Reaktion zwischen Hirudin und Thrombin. Hoppe-Seylers Z. Physiol. Chem. 1958; 312: 85-98
• 5 Markwardt F, Walsmann P. Reindarstellung und Analyse des Thrombininhibitors Hirudin. Hoppe Seylers Z. Physiol. Chem. 1967; 348: 1381-86
• 6 Bagdy D, Barabas E, Graf L, Peterson TE, Magnusson S. Hirudin. Methods Enzymol. 1976; 45: 669-78
• 7 Dodt J, Seemüller U, Maschler R, Fritz H. The complete covalent structure of hirudin. Localization of the disulfide bonds. Biol. Chem. Hoppe Seyler. 1985; 366: 379-85
• 8 Baskova IP, Cherkesova DU, Mosolov VV. Hirudin from leech heads and whole leeches and 'pseudo'-hirudin from leech bodies. Thrombos. Res. 1983; 30: 459-67
• 9 Dodt J, Machleidt W, Seemüller U, Maschler R, Fritz H. Isolation and charcterization of hirudin isoinhibitors and sequence analysis of hirudin PA. Biol. Chem. Hoppe Seyler. 1986; 367: 803-11
• 10 Scharf M, Engels J, Tripier D. Primary structure of new iso-hirudins. FEBS Lett. 1989; 255: 105-10
• 11 Môrki WE, Grossenbacher H, Grütter MG, Liersch MH, Meyhack B, Heim J. Recombinant hirudin: Genetic engineering and structure analysis. Semin. Thromb. Hemost. 1991; 17: 88-93
• 12 Markwardt F. Versuche zur pharmakologischen Charakterisierung des Hirudins. Naunyn Schmiedebergs Arch Pharmacol. 1958; 234: 516-29
• 13 Markwardt F. Hirudin as an inhibitor of thrombin. Methods Enzymol. 1970; 19: 924-32
• 14 Rydel TJ, Ravichandran KG, Tulinski A, Bode W, Huber R, Roitsch C, Fenton II JW. The structure of a complex of recombinant hirudin and human α-thrombin. Science. 1990; 249: 277-80
• 15 Stürzebecher J, Walsmann P. Structure-activity relationships of recombinant hirudins. Semin. Thromb. Hemost. 1991; 17: 94-98
• 16 Maraganore JM, Bourdon P, Jablonski J, Ramachandran KL, Fenton II JW. Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin. Biochemistry. 1990; 29: 7095-7101
• 17 Walsmann P. Über den Einsatz des spezifischen Thrombin-Inhibitors Hirudin für diagnostische und biochemische Untersuchungen. Pharmazie. 1988; 43: 737-44
• 18 Stocker K. Laboratory use of hirudin. Semin. Thromb. Hemost. 1991; 17: 113-21
• 19 Stone SR, Hofsteenge J. Kinetics of the inhibition of thrombin by hirudin. Biochemistry. 1986; 25: 4622-28
• 20 Markwardt F. Die antagonistische Wirkung des Hirudins gegen Thrombin in vivo. Naturwissenschaften. 1956; 43: 11
• 21 Walsmann P, Markwardt F. Biochemische und pharmakologische Aspekte des Thrombininhibitors Hirudin. Pharmazie. 1981; 36: 653-60
• 22 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: 226-29
• 23 Markwardt F. Pharmacology of hirudin: one hundred years after the first report of the anticoagulant agent. Biomed. Biochim. Acta. 1985; 44: 1007-13
• 24 Markwardt F. Hirudin, der blutgerinnungshemmende Wirkstoff des medizinischen Blutegels. Blut. 1958; 4: 161-70
• 25 Markwardt F. Biochemistry and pharmacology of hirudin. in: Pirkle H, Markland jr. FS. (eds) Hemostasis and animal venoms.. Dekker, New York, Basel: 1988. pp 255-69
• 26 Markwardt F. The comeback of hirudin - an old-established anticoagulant agent. Folia Haematol. 1988; 115: 10-23
• 27 Markwardt F. Development of hirudin as an antithrombotic agent. Semin. Thromb. Hemost. 1989; 15: 269-82
• 28 Markwardt F. Past, present and future of hirudin. Haemostasis. 1991; 21 (suppl 1) 11-26
• 29 Hoet B, Close P, Vermylen J, Verstraete M. Hirudo medicinalis and hirudin. In: Recent Advances in Blood Coagulation.. Poller L. (ed) Vol 3, Publ. Churchill Livingstone: 1990. pp 223-44
• 30 Walsmann P, Kaiser B. Biochemical and pharmacological properties of recombinant hirudin. Drugs of Today. 1989; 25: 473-85
• 31 Walenga JM, Pifarre R, Fareed J. Recombinant hirudin as antithrombotic agent. Drugs of the Future. 1990; 15: 267-80
• 32 Fareed J, Walenga JM, Hoppensteadt D, Pifarre R. Development perspectives for recombinant hirudin as an antithrombotic agent. Biol. Clin. Hematol. 1989; 11: 143-52
• 33 Kawabata SL, Morita T, Kaida S, Igarashi H, Iwanaga S. Difference in enzymatic properties between staphylothrombin and free α-thrombin. Ann. N.Y. Acad. Sci. 1980; 485: 27-40
• 34 Markwardt F. Der Hirudintoleranztest. Klin. Wschr. 1959; 37: 1142-43
• 35 Schmutzler R, Markwardt F. Der Hirudintest, eine Mikromethode zur Kontrolle des Prothrombinspiegels bei der Antikoagulantientherapie. Klin. Wschr. 1962; 40: 796-98
• 36 Markwardt F. Die Bestimmung des Thrombins durch Titration mit Hirudin. Arch. Pharmaz. 1957; 290: 280-84
• 37 Markwardt F. Hirudin - Biochemisch-pharmakologische Wirkung und Anwendung zur gerinnungsphysiologischen Diagnostik. in: Marx R, Thies HA. (eds) Kontrolle von Antithrombotika,. Basel, Editiones Roche: 1980. pp. 105-15
• 38 Griessbach U, Stürzebecher J, Markwardt F. Assay of hirudin in plasma using a chromogenic thrombin substrate. Thromb. Res. 1985; 37: 347-50
• 39 Markwardt F, Stürzebecher J, Walsmann P. The hirudin standard. Thromb. Res. 1990; 59: 395-400
• 40 Lindhout T, Blezer R, Hemker HC. The anticoagulant mechanism of action of recombinant hirudin (CGP 39393) in plasma. Thromb. Haemost. 1990; 64: 464-68
• 41 Hoffmann A, Markwardt F. Inhibition of the thrombin-platelet reaction by hirudin. Hemostasis. 1984; 14: 164-69
• 42 Hofsteenge J, Taguchi H, Stone SR. Effect of thrombomodulin on the kinetics of the interaction of thrombin and inhibitors. Biochem. J. 1986; 237: 243-51
• 43 Hauptmann J, Brüggener E, Markwardt F. Effect of heparin, hirudin and a synthetic thrombin inhibitor on antithrombin III in thrombin-induced disseminated intravascular coagulation in rats. Hemostasis. 1987; 17: 321-28
• 44 Markwardt F, Hoffmann A, Stürzebecher J. Influence of thrombin inhibitors on the thrombin-induced activation of human blood platelets. Hemostasis. 1983; 13: 227-33
• 45 Glusa E, Markwardt F. Platelet functions in recombinant hirudin-anticoagulated blood. Hemostasis. 1990; 20: 112-18
• 46 Glusa E. Hirudin and platelets. Semin Thromb. Hemost. 1991; 17: 122-25
• 47 Basic-Micic M, Krupinski K, Breddin HK. r-hirudin effects on various platelet functions. Angio. Arch. 1989; 18: 1
• 48 Markwardt F, Stürzebecher J, Glusa E. Antithrombin effects of native and recombinant hirudins. Biomed. Biochim. Acta. 1990; 49: 399-404
• 49 Glusa E, Markwardt F. Adrenaline-induced reactions of human platelets in hirudin plasma. Hemostasis. 1980; 9: 188-92
• 50 Shuman MA. Thrombin-cellular interaction. Ann. N.Y. Acad. Sci. 1986; 485: 228-39
• 51 Markwardt F jr, Franke T, Glusa E, Nilius B. Pharmacological modification of mechanical and electrical responses of frog heart to thrombin. Naunyn-Schmiedebergs Arch. Pharmac. 1990; 341: 341-46
• 52 Van Obberghen-Schilling E, Perez-Rodriguez R, Pouyssegur J. Hirudin, a probe to analyze the growth promoting activity of thrombin in fibroblasts; reevaluation of the temporal action of competence factors. Biochem. Biophys. Res. Commun. 1982; 105: 79-86
• 53 Glusa E, Markwardt F. Studies on thrombin-induced endothelium-dependent vascular effects. Biomed Biochim Acta. 1988; 47: 623-30
• 54 Walenga JM, Hoppensteadt D, Koza M, Pifarre R, Fareed J. Comparative studies on various assays for the laboratory evaluation of r-hirudin. Semin. Thromb. Hemost. 1991; 17: 103-12
• 55 Stürzebecher J. Methods for determination of hirudin. Semin. Thromb. Hemost. 1991; 17: 99-102
• 56 Spannagl M, Bichler J, Lill L, Schramm W, Fritz H. A fast chromogenic assay for determination of hirudin in plasma (abstract). Thromb. Hemost. 1989; 62: 32
• 57 Richter M, Walsmann P, Cyranka U, Markwardt F. 125-1 Markierung von Hirudin. Pharmazie. 1986; 41: 52
• 58 Bichler J, Fichtl B, Siebeck M, Fritz H. Pharmacokinetics and pharmacodynamics of hirudin in man after single subcutaneous and intravenous bolus administration. Arzneim.-Forsch. 1988; 38: 704-10
• 59 Spinner S, Stöffler G, Fink E. Quantitative enzyme-linked immunosorbent assay (ELISA) for hirudin. J. Immunol. Methods. 1986; 87: 79-93
• 60 Schlaeppi JM, Vekemans S, Rink H, Chang JY. Preparation of monoclonal antibodies to hirudin and hirudin peptides. Eur. J. Biochem. 1990; 188: 463-70
• 61 Spinner S, Scheffauer F, Maschler R, Stöffler G. A hirudin catching ELISA for quantitating the anticoagulant in biological fluids. Thrombos. Res. 1980; 51: 617-25
• 62 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: 226-29
• 63 Markwardt F, Nowak G, Stürzebecher U, Walsmann P. Studies on the pharmacokinetics of hirudin. Biomed. Biochim. Acta. 1987; 46: 237-44
• 64 Nowak G. Pharmacokinetics of hirudin. Semin. Thromb. Hemost. 1991; 17: 145-49
• 65 Nowak G, Markwardt F, Fink E. Pharmacokinetic studies with recombinant hirudin in dogs. Folia Haematol. 1988; 115: 70-74
• 66 Markwardt F, Huan XQ, Walenga JM, Münch M, Hoppensteadt D. Pharmacokinetics of recombinant hirudin in primates (abstract). Fed. Proc. 1988; 1: 48
• 67 Markwardt F, Fink E, Kaiser B, Klöcking H-P, Nowak G, Richter M, Stürzebecher J. Pharmacological survey of recombinant hirudin. Pharmazie. 1988; 43: 202-07
• 68 Richter M, Cyranka U, Nowak G, Walsmann P. Pharmacokinetics of 125 I-hirudin in rats and dogs. Folia Haematol. 1988; 115: 64-69
• 69 Henschen A, Markwardt F, Walsmann P. Identification by HPLC analysis of the unaltered forms of hirudin and desulfated hirudin after kidney passage (abstract).. Thromb. Res. 1987; 7 (suppl) 37
• 70 Henschen A, Markwardt F, Walsmann P. Evidence for the identity of hirudin isolated after kidney passage with the starting material. Folia Haematol. 1988; 115: 59-63
• 71 Richter M, Walsmann P, Markwardt F. Plasma level of dextran-r-hirudin. Pharmazie. 1989; 44: 73-74
• 72 Markwardt F, Richter M, Walsmann P, Riesener G, Paintz M. Preparation of dextran-bound recombinant hirudin and its pharmacokinetic behaviour. Biomed. Biochim. Acta. 1990; 49: 1103-08
• 73 Markwardt F, Nowak G, Stürzebecher J, Griessbach U, Walsmann P, Vogel G. Pharmacokinetics and anticoagulant effect of hirudin in man. Thromb. Haemost. 1984; 52: 160-63
• 74 Markwardt F, Nowak G, Stürzebecher J, Vogel G. Clinico-pharmacological studies with recombinant hirudin. Thromb. Res. 1988; 52: 393-400
• 75 Markwardt F, Nowak G, Stürzebecher J. Clinical pharmacology of recombinant hirudin. Haemostasis. 1991; 21 (suppl 1) 133-36
• 76 Klöcking H-P, Güttner J, Fink E, Markwardt F. Studies in toxicity of recombinant hirudin. Blut. 1990; 60: 12
• 77 Klöcking H-P. Toxicology of hirudin. Semin. Thromb. Hemost. 1991; 17: 126-29
• 78 Bichler J, Gemmerli R, Fritz H. Studies for revealing a possible sensitization to hirudin after repeated intravenous injection in baboons. Thromb. Res. 1991; 61: 39-51
• 79 Kaiser B. Anticoagulant and antithrombotic actions of recombinant hirudin. Semin. Thromb. Hemost. 1991; 17: 130-36
• 80 Markwardt F, Kaiser B, Nowak G. Studies on antithrombotic effects of recombinant hirudin. Thromb. Res. 1989; 54: 377-88
• 81 Talbot MD, Ambler J, Butler KD, Findley VS, Mitchel KA, Peters RF, Tweed MF, Wallis RB. Recombinant desulphatohirudin (CGP 39393) anticoagulant and antithrombotic properties in vivo. Thromb. Haemost. 1989; 61: 77-80
• 82 Doutremepuich C, Deharo E, Guyot M, Lalanne MC, Walenga J, Fareed J. antithrombotic activity of recombinant hirudin in the rat: A comparative study with heparin. Thromb. Res. 1989; 54: 435-45
• 83 Talbot M. Biology of recombinant hirudin (CGP 39393): A new prospect in the treatment of thrombosis. Semin. Thromb. Hemost. 1989; 15: 293-301
• 84 Kaiser B, Markwardt F. Antithrombotic and haemorrhagic effects of synthetic and naturally occurring thrombin inhibitors.. Thromb. Res. 1986; : 613-20
• 85 Kaiser B, Markwardt F. Antithrombotic and haemorrhagic effects of the naturally occurring thrombin inhibitor hirudin. Folia Haematol. 1988; 115: 41-46
• 86 Fareed J, Walenga JM. Do we need to neutralize hirudin's anticoagulant effects to minimize bleeding?. Fed. Proc. 1989; 3: A 328
• 87 Fareed J, Walenga JM, Hoppensteadt D, Iyer L, Pifarre R. Neutralization of recombinant hirudin: Some practical considerations. Semin. Thromb. Hemost. 1991; 17: 137-44
• 88 Brüggener E, Walsmann P, Markwardt F. Neutralization of hirudin anticoagulant action by DIP-thrombin. Pharmazie. 1989; 44: 648-49
• 89 Walsmann P. Untersuchungen zur Affinitôtschromatographie von Hirudin an trôgerfixiertem Thrombin. Pharmazie. 1981; 36: 860-61
• 90 Walsmann P, Markwardt F. On the isolation of the thrombin inhibitor hirudin. Thromb. Res. 1985; 40: 563-70
• 91 Bucha E, Markwardt F, Nowak G. Hirudin in haemodialysis. Thromb. Res. 1990; 60: 445-55
• 92 Markwardt F, Nowak G, Bucha E. Hirudin as anticoagulant in experimental haemodialysis.. Haemostasis 1991; 21 (suppl 1) 149-55
• 93 Walenga JM, Pifarre R, Hoppensteadt D, Fareed J. Development of recombinant hirudin as a therapeutic anticoagulant and antithrombotic agent: Some objective considerations. Semin. Thromb. Haemost. 1989; 15: 316-33
• 94 Markwardt F. Prospective clinical use of hirudin as an anticoagulant. Biomed. Prog. 1990; 3: 19-23
• 95 Klöcking H-P, Markwardt F. Influence of recombinant hirudin on the thrombogenicity of prothrombin complex concentrates. Pharmazie. 1989; 44: 341-42
• 96 Freund M, Cazenave JP, Courtney M, Degryse E, Roitsch C, Bernat A, Delebassee D, Defreyn G, Maffrand JP. Inhibition by recombinant hirudins of experimental venous thrombosis and disseminated intravascular coagulation induced by tissue-factor in rats. Thromb. Haemost. 1990; 63: 187-92
• 97 Degryse E, Acker M, Defreyn G, Bernat A, Maffrand JP, Roitsch C, Courtney M. Point mutations modifying the thrombin inhibition kinetics and antithrombotic activity in vivo of recombinant hirudin. Protein Eng. 1989; 2: 459-65
• 98 Nowak G, Markwardt F. Hirudin in disseminated intravascular coagulation.. Haemostasis. 1991; 2 (suppl 1) 142-48
• 99 Nowak G, Markwardt F. Influence of hirudin on endotoxin-induced disseminated intravascular coagulation (DIC) in weaned pigs. Exp. Pathol. 1980; 18: 438-43
• 100 Markwardt F, Nowak G, Hoffmann J. Comparative studies on thrombin inhibitors in experimental microthrombosis. Thromb. Haemost. 1983; 49: 235-37
• 101 Siebeck M, Hoffmann H, Weipert J, Spannagl M, Weis M, Bichler J. Hirudin prevents intravascular coagulation in porcine endotoxin shock. In : Chirurgisches Forum '88 f. exp. u. klin.. Forschung Schriefers. et al. (eds) 1988. Springer, Berlin-Heidelberg: pp. 297-300
• 102 Ishikawa A, Hafter R, Seemüller U, Gokel JM, Graeff H. The effect of hirudin on endotoxin induced disseminated intravascular coagulation (DIC). Thromb. Res. 1980; 19: 351-358
• 103 Hauptmann J, Brüggener E. Influence of hirudin on the consumption of antithrombin III in experimental DIC. Folia Haematol. 1988; 115: 83-87
• 104 Chesebro JH, Heras M, Mruk J, Grill D, Fuster V. The critical role of thrombin in arterial thrombosis is demonstrated by hirudin.. Angio. Arch. 1989; 18: 9
• 105 Krupinski K, Breddin H K, Markwardt F, Haarmann W. Antithrombotic effects of three thrombin inhibitors in a rat model of laser-induced thrombosis. Haemostasis. 1989; 19: 74-82
• 106 Heras M, Chesebro JH, Penny WJ, Bailey KR, Badimon L, Fuster V. Effects of thrombin inhibition on the development of acute platelet-thrombus deposition during angioplasty in pigs. Heparin versus recombinant hirudin, a specific thrombin inhibitor. Circulation. 1989; 79: 657-65
• 107 Kaiser B, Simon A, Markwardt F. Antithrombotic effects of recombinant hirudin in experimental angioplasty and intravascular thrombolysis. Thromb. Haemost. 1990; 63: 44-47
• 108 Bucha E, Nowak G, Markwardt F. Prevention of experimental coronary thrombosis by hirudin. Folia Haematol. 1988; 115: 52-58
• 109 Markwardt F. Anticoagulants after thrombolysis;. in Schettler G. (ed) Reperfusion and revascularisation in acute myocardial infarction.. Springer, Berlin.: 1988. pp. 137-43
• 110 Markwardt F. Prevention of coronary thrombosis by hirudin;. in Papp J Gy. (ed) Cardiovascular pharmacology '87 Budapest. ( Akademiai Kiado, Budapest: 1987. ) pp. 449-56
• 111 Walenga JM, Bakhos M, Messmore HL, Fareed J, Pifarre R. The potential use of r-hirudin as an anticoagulant in cardiopulmonary bypass model.. Ann. Thorac. Surg. (in press)
• 112 Vogel G, Markwardt F. Clinical use of hirudin. Folia Haematol. 1988; 115: 113-18
• 113 Vogel G, Markwardt F. Preliminary clinical reports on the antithrombotic action of hirudin (abstract).. Thromb. Res. 1987; 7 (suppl.) 42
• 114 Markwardt F. The comeback of hirudin as an antithrombotic agent. Semin. Thromb. Haemost. 1991; 17: 75-82