62
Views
22
CrossRef citations to date
0
Altmetric
Drug Evaluation

Pharmacology of argatroban

, , &
Pages 625-654 | Published online: 23 Feb 2005

Bibliography

  • CALLAS D, FAREED J: Comparative pharmacology ofsite directed antithrombin agents. Implication in drug development. Thromb. Haemost. (1995) 74(0:473–481.
  • FENTON JW: Regulation of thrombin generation andfunctions. Sem. Thromb. HemosL (1988) 14:234–240.
  • MARKWARDT F: The development of hirudin as an anti-thrombotic drug. In: New Anticoagulants for the Cardio-vascular Patient. Pifarré R (Ed.), Hanley & Belfus, Inc., Philadelphia, USA (1997):145–160.
  • FAREED J, CALLAS D, HOPPENSTEADT DA, LEWIS BE, BICK RL, WALENGA JM: Antithrombin agents as antico-agulants and antithrombotics: implications in drug de-velopment. Sem. Hematol (1999) 36 (1)Supp1.1: 42–56.
  • FAREED J, CALLAS DD, HOPPENSTEADT D, JESKE W, WALENGA JM: Recent developments in antithrombotic agents. Exp. Opin. Invest. Drugs (1995) 4(5):389–412.
  • THEROUX P, LIDON R: Anticoagulants and their use in acute ischemic syndromes. In: Textbook of Interventional Cardiology. Topol EJ (Ed.), WB Saunders Co., Philadelphia, USA (1994):23–45.
  • ANTMAN EM FOR THE TIMI 9B INVESTIGATORS: Hirudin in acute myocardial infarction Thrombolysis and thrombin inhibition in myocardial infarction (TIIVII) 9B trial. Circulation (1996) 94:911–921.
  • FLATHER M, WEITZ J, CAMPEAU J et al. (FOR THE OASIS PILOT STUDY INVESTIGATORS): Evidence for rebound activation of the coagulation system after cessation of intravenous anticoagulant therapy for acute myocar-dial ischemia. Circulation (1995) 92 (8):I–485.
  • 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. New Engl. J. Med. (1996) 335(10:775–782.
  • SERRUYS PW, HERRMAN J-PR, SIMON R et al: A compari-son of hirudin with heparin in the prevention of res-tenosis after coronary angioplasty. New Engl. J. Med. (1995) 333(12):757–763.
  • ERIKSSON BI, MOURET P, KALEBO P et al.: Recombinant hirudin, CGP 39393 (TMREVASC), is more effective than enoxaparin as prophylaxis of thromboembolic complications in patients undergoing total hip re-placement. Haemostasis. (1996) 26 (Suppl. 3):624.
  • ERIKSSON BI, EKMAN S, KALEBO P, ZACHRISSON B, BACH D, CLOSE P: Prevention of deep-vein thrombosis after total hip replacement: direct thrombin inhibi-tion with recombinant hirudin, CGP 39393. Lancet (1996) 347:635–639.
  • POTZSCH B, RIESS F-C, MADLENER K, VOLPEL H, MOLLER-BERGHAUS G, GREINACHER A: Recombinant hirudin as anticoagulant during cardiopulmonary by-pass surgery. Ann. Hematol. (1997) 74(Suppl. ID:A153.
  • RIESS F-C, POTZSCH B, MOLLER-BERGHAUS G: Recombi-nant hirudin as an anticoagulant during cardiac sur-gery. In: New Anticoagulants for the Cardiovascular Patient. Pifarré R (Ed.), Hanley & Belfus, Inc, Philadelphia, USA (1997):197–222.
  • RIESS FC, LOWER C, SEELIG C et al.: Recombinant hi-rudin as a new anticoagulant during cardiac opera-tions instead of heparin: successful for aortic valve replacement in man. J. Thorac. Cardiovasc. Surg. (1995) 110:265–267.
  • HUJIKATA-OKUNOMIYA A, OKAMOTO S, KIKUMOTO R et al. Similarity and dissimilarity in the stereogeome-try of the active sites of thrombin, trypsin, plasmin and glandular kallikrein. Thromb. Res. (1987) 45(5):451–462.
  • YONEKAWA Y, HANDA H, OKAMOTO S et al.: Treatment of cerebral infarction in the acute stage with synthetic antithrombin MD805: clinical study among multiple institutions. Arch. Jpn. Chir. (1986) 55:711–726.
  • JACKSON CV, SATTERWHITE J, ROBERTS E: Preclinical and clinical pharmacology of efegatran (LY294468): a novel antithrombin for the treatment of acute coro-nary syndromes. Clin. Appl. Thrombosis/Hemostasis (1996) 2(4):258–267.
  • CHAMBERLIN JR, LEWIS B, LEYA F et al.: Successful treat-ment of heparin-associated thrombocytopenia and thrombosis using hirulog. Can. J. Cardiof (1995) 11(6):511–514.
  • KOZA MJ, LEWIS BE, WALENGA JM, PIFARRE R, FAREED J: Antithrombin agents in the management of heparin-induced thrombocytopenia. In: New Anticoagulants for the Cardiovascular Patient. Pifarré R (Ed.), Hanley & Belfus, Inc., Philadelphia, USA (1997): 309–324.
  • LEWIS BE, WALENGA JM, PIFARRE R, FAREED J: Argatro-ban in the management of patients with heparin-induced thrombocytopenia and heparin-induced thrombocytopenia and thrombosis syndrome. In: New Anticoagulants for the Cardiovascular Patient. Pifarré R (Ed.), Hanley & Beffus, Inc., Philadelphia, USA (1997):223–230.
  • HERRMAN J-P, SURYAPRANATA H, GABRIEL L, DEN HEUER P: Argatroban during percutaneous translumi-nal coronary angioplasty; results of a dose finding study. Circulation (1996) 94 (8):I–375.
  • LEWIS BE, GRASSMAN ED, JOHNSON SA, MCKIERNAN TL: Pilot study of a argatroban for angioplasty in patients with heparin allergy. Circulation (1996) 94(8)I–375.
  • LEWIS BE, FERGUSON JJ, GRASSMAN ED et al.: Successful coronary interventions performed with argatroban anticoagulation in patients with heparin-induced thrombocytopenia and thrombosis syndrome. J. Invas. Cardiol. (1996) 8:110–117.
  • BUSH LR. Argatroban, a selective, potent thrombin in-hibitor. Cardiovasc. Drug. Rev. (1991) 9(3):247–263.
  • BANNER DW, HADVARY P: Crystallographic analysis at 3.0 A resolution of the binding to human thrombin and four active site-directed inhibitors. J. Biol. Chem. (1991) 266(30)20085–20093.
  • NIWA C, NIWA M, MAEDA M, YAMAGISHI R, KONDO S, SAKURAGAWA N. Effects of newly synthesized anti-thrombin agent (MD-805) on blood coagulation sys-tem. Saishin Igaku (1985) 40:2677–2683.
  • KIKUMOTO R, TAMOA Y, TEZUKA T et al.: Selective inhi-bition of thrombin by (2R, 4R)-4-methyl-14N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyfisulfonyl]-L--arginy1)]-2-piperidinecarboxylic acid. Biochemistry. (1984) 23:85–90.
  • GAST A, TSCHOPP TB: Inhibition constants of napsaga-tran for thrombin and related serine proteases in com-parison with other direct thrombin inhibitors. Thromb. HaemosL Suppl. (1997):93.
  • PAQUES EP, ROMISCH J: Comparative study in the in vi-tro effectiveness of antihrombotic agents. Thromb. Res. (1991) 64:11–21.
  • OKAMOTO S, HIJIKATA A: Potent inhibition of throm-bin by the newly synthesized arginine derivative No. 805. The importance of stereostructure of its hydro-phobic carboxamide portion. Biochem. Biophys. Res. Comm. (1981) 101(2):440–446.
  • OKAMOTO S, HIJIKATA A, KIKUMOTO R et al.: A syn-thetic thrombin inhibitor taking extremely active stereostructure. Thromb. Haemost. (1979) 42:205.
  • RAWSON TE, VAN GORP KA, YANG J et al: Separation of 21-(R)- and 21-(S)-Argatroban: solubility and activity of the individual diastereoisomers. j Pharm. Sci. (1993) 82 (6):672–673.
  • SUZUKI K, KUSUMOTO H, HASHIMOTO S: Isolation and characterization of thrombomodulin from bovine lung. Biochim. Biophys. Acta. (1986) 882:343–352.
  • HANTGAN RR, JEROME WG, HURSTING MJ: No effect of clot age or thrombolysis on argatroban's inhibition of thrombin. Blood (1998) 92(6):2064–2074.
  • TAMAO Y, YAMAMOTO T, HIRATA T, KINUSAGA M, KIKUMOTO R: Effect of argatroban on blood coagula-tion. Jap. Pharm. Thera. (1986) 14(5):7–12.
  • NIWA C, NIWA M, MAEDA M, YAMAGISHI R, KONDO S, SAKURAGAWA N: Effects of newly synthesized anti-thrombin agent (MD-805) on blood coagulation sys-tem. Saishin Igaku. (1985) 40:2677–2683.
  • GREEN D, TS'AO C, REYNOLDS N, KAHN D, KOHL H, CO-HEN I: In vitro studies of a new synthetic thrombin inhbitor. Thromb. Res. (1985) 37:145–153.
  • NAGASAWA H, FUKUTAKE K, HADA M: Phase one study of synthetic antithrombin agent (MD-805). Single and multiple administration studies. Jap. J. Pharm. Thera. (1981) 12(3):359–375.
  • BERRY CN, GIRARDOT C, LECOFFRE C, LUNVEN C: Ef-fects of the synthetic thrombin inhibitor argatroban on fibrin- or clot-incorporated thrombin: comparison with heparin and recombinant hirudin. Thromb. Hae-most. (1994) 72(3):381–386.
  • HURSTING MJ, BECKER JC, LEWIS BE, IQBAL 0, WALENGA JM, FERGUSON JJ. Differential effects of arga-troban and heparin on Hemochron and Hemo-tec acti-vated clotting times in patients undergoing coronary interventional procedures. J. Am. Coll. Card (1997) 29(2):500a.
  • HURSTING MJ, ALFORD KL, BECKER JCP: Novastan (brand of argatroban): a small-molecule, direct throm-bin inhibitor. Semin. Thromb. HemosL (1997) 23(6):503–516.
  • EIDT JF, ALLISON P, NOBLE S et al. Thrombin is an im- portant mediator of platelet aggregation in stenosed canine coronary arteries with endothelial injury. J. Clin. Invest. Trans. Assoc. Am. Phys. (1988) 101:125–136.
  • KAWAI H, YAMAMOTO T, HARA H et al.: Inhibition of factor Xa-induced platelet aggregation by a selective thrombin inhibitor, Argatroban. Thromb. Res. (1994) 74 (3):185–191.
  • KAISER B, KOZA M, WALENGA JM, FAREED J: Flow cy-tometric evaluation of the effect of various thrombin inhibitors on platelet activation in whole blood. Thromb. Res. (1996) 82(3):257–263.
  • KOSUGI T, NAKAMURA M, SAITOH S et al.: Changes of rabbit platelet function following simultaneous ad-ministration of ticlopidine hydrochloride and argipi-done (MD-805). Int. J. Tiss. React. (1992) 14(3):141–148.
  • HARA H, YOSHIKUNI T, KIKUMOTO R: Effect of argatro-ban (MD-805) on platelet function. Jap. J. Pharm. Thera. (1986) 14 (Suppl. 5):13–19.
  • LUNVEN C, GAUFFERY C, LECOFFRE C, O'BRIEN DP, ROOME NO, BERRY CN. Inhibition by argatroban, a spe-cific thrombin inhibitor, of platelet activation by fi-brin clot associated thrombin. Thromb. Haemost. (1996) 75:154–160.
  • MATSUO T, IMAYA M: Inhibition of collagen-induced platelet aggregation by argatroban, a direct thrombin inhibitor in patients with acute cerebral infarction. Thromb. Haemost. Suppl. (1997):89.
  • NAKAMURA K, HATANO Y, MORI K: Thrombin-induced vasoconstriction in isolated cerebral arteries and the influence of a synthetic thrombin inhibitor. Thromb. Res. (1985) 40:715–20.
  • WINN MJ, JAIN K, KU DD: Argatroban and inhibition of the vasomotor actions of thrombin. J. Cardiovasc. Pharm. (1993) 22(5):754–60.
  • AHSAN A, AHMAD S, IQBAL 0 etaL: Comparative studies on the biochemical and pharmacologic properties of a major metabolite of Argatroban (M1): potential clini-cal implications. Thromb. Haemost. Suppl (1997)92.
  • HOPPENSTEADT DA, WALENGA JM, KOZA MJ, BERMAS EW, FAREED J: Direct antithrombin agents as antico-agulants for clinical laboratory specimen collection in blood. Thromb. Haemost. Suppl. (1997).
  • LYON AW, HARDING SR, DROBOT D, LYON ME: Use of thrombin inhibitors ex vivo allows critical care clini-cal chemistry and hematology testing on common specimens. Clin. Biochem. (1997) 30 (2):121–127.
  • YAMABE H, OSAWA H, INUMA H et al: Thrombin stimu-lates production of transforming growth factor-beta by cultured human mesangial cells. Nephrol Dialysis Transpl. (1997) 12(3):438–442.
  • WAKITA H, FURUKAWA F, TAKIGAWA M: Thrombin and trypsin induce granulocyte-macrophage colony-stimulating factor and interleukin-6 gene expression in cultured normal human keratinocytes. Proc. Assoc. Am. Phys. (1997) 109(2):190–207.
  • CALLAS DD, IQBAL 0, HOPPENSTEADT D, FAREED J: Fi-brinolytic compromise by synthetic and recombinant thrombin inhibitors: implications in the treatment of thrombotic disorders. Clin. Appl. Thromb. Hemost. (1995) 1(2):114–124.
  • IKOMA H, OHTSU K, TAMAO Y, KIKUMOTO R, OKA-MOTO S: Effect of a potent thrombin inhibitor, MCI-9038, on novel experimental arterial thrombosis. Blood Vessel (1982) 13:72–77.
  • RIGTER B, ABEL F, MULLER TH et al.: The synthetic thrombin inhibitor Argipidine (MD-805) in contrast to heparin inhibits venous thrombosis without prolon-gation of bleeding time in hamster. Thromb. Haemost. (1989) 62:533.
  • IMURA Y, STASSEN JM, COLLEN D: Comparative anti-thrombotic effects of heparin, recombinant hirudin and argatroban in a hamster femoral vein platelet-rich mural thrombosis model. J. Pharm. Exp. Thera. (1986) 261 (3) 895–898.
  • MORISHITA K, WADA M, KUMADA T et al.: Effect of ti-clopidine and other antithrombotics on the venous thrombosis induced by endothelial damage of jugular vein in rats. Thromb. Res. (1991) 63(3):373–384.
  • HAYES JM, JESKE W, CALLAS D, IQBAL 0, FAREED J: Com-parative intravenous antithrombotic actions of hepa-rin and site directed thrombin inhibitors in a jugular vein clamping model. Thromb. Res. (1996) 82 (2):187–191.
  • SATO K, KAWASAKI T, HISAMICHI N et al.: A selective and potent factor Xa inhibitor, YM-60828, exerts its an-tithrombotic effect with little prolongation of bleeding time. Thromb. Haemost. Suppl. (1997):292.
  • JANG IK, GOLD HK, ZISKIND AA et al.: Prevention of ar-terial thrombosis by short-term thrombin inhibition. Circulation (1989) 80:11–23.
  • SASAKI Y, MORII S, YAMASHITA T et al. Antithrombotic effect of Argatroban on the pial vessels of the rat: a study with He-Ne laser-induced thrombus formation. Haemostasis. (1993) 23 (2) 104–1 1 1
  • KRUPINSKI K, BREDDIN HK, MARKWARDT F et al.: Anti-thrombotic effects of three thrombin inhibitors in a rat model of laser-induced thrombosis. Haemostasis. (1989) 19:74–82.
  • YAMASHITA T, YAMAMOTO J, SASAKI Y, MATSUODA A: The antithrombotic effect of low molecular weight synthetic thrombin inhibitors, argatroban and PPACK, on He-Ne laser-induced thrombosis in rat mes-enteric microvessels. Thromb. Res. (1993) 69(1):93–100.
  • IKOMA H, HARA H, TAMAO Y, KIKUMOTO R: Suppres-sive effect of argatroban (MD-805) on thrombogenesis by the arterio-venous shunt in rabbits. Jap. Pharm. Thera. (1986) 14\(Suppl. 5):21–24.
  • TOMARU T, NAKAMURA F, FUJIMORI Y et al: Local treat-ment with antithrombotic drugs can prevent throm-bus formation: an angioscopic and angiographic study. J. Am. Coll. Cardiol. (1995) 26(5):1325–1332
  • MELANDRI G, SEMPRINI F, DESCOVICH B, CERVI V, BRANZI A: Argatroban strongly reduces thrombus for-mation under flow conditions in humans. Thromb. Haemost. Suppl. (1997) 784.
  • BERRY CN, LUNVEN C, O'BREIN DP et al.: Ecarin clotting time: A predictaive marker for the antithrombotic ef-fects of argatroban in rat venous and arterial thrombo-sis. Thromb. Haemost. Suppl. (1997):97.
  • VAN AMSTERDAM RGM, VOGEL GMT, VAN HOUWELIN-GEN, MEULEMAN DG: ORG 36764, a novel glycoconju-gate with high efficacy in a rat model of severe arterial thrombosis. Thromb. Haemost. Suppl. (1997)95.
  • KUMADA T, ABIKO Y: Comparative study on heparin and a synthetic thrombin inhibitor No. 805 (MD-805) in experimental antithrombin Ill-deficient animals. Thromb. Res. (1981) 24:285–298.
  • BERRY CN, GIRARD D, LOCHOT S, LECOFFRE C: Anti-thrombotic actions of argatroban in rat models of ve-nous, mixed and arterial thrombosis, and its effects on the tail transection bleeding time. Br. J. Pharm. (1994) 113(4):1209–1214.
  • HUJIKATA-OKUNOMIYA A, KITAGUCHI H, HIRATA M: Ef-fect of MD 805 on plasminogen activator release by thrombin from isolated perfused dogleg. Thromb. Res. (1987) 45:699–702.
  • TAMAO Y. YAMAMOTO T, KIKUMOTO R eta].: MC Effectof a selective thrombin inhibitor 1–9038 on flbrinolysis in vitro and in vivo. Thromb. Haemost. (1986) 56 (1) :28–34.
  • FITZGERALD DJ AND FITZGERALD GA: Role of thrombinand thromboxane A2 in reocclusion following coro-nary thrombolysis with tissue-type plasminogen acti-vator. Proc. Natl. Acad. ScL USA (1989) 86:7585–7589.
  • JANG IK, GOLD HK, LEINBACH RC et al.: Acceleration ofreperfusion by combination of rt-PA and a selective thrombin inhibitor, Argatroban. Circulation (1989) 80:11–217.
  • JANG IK, GOLD HK, LEINBACH RC: In vivo thrombin in-hibition enhances and sustains arterial recanalization with recombinant tissue-type plasminogen activator. Circ. Res. (1990) 67(6):1552–1561.
  • MELLOTT MJ, CONNOLLY TM, YORK SJ et al. Prevention of reocclusion by MCI-9038, a thrombin inhibitor, fol-lowing t-PA induced thrombolysis in a canine model of femoral arterial thrombosis. Thromb. Haemost. (1990) 64(4) 526–534
  • 81. REFINO CJ, BUNTING S, HUKTGREN B et al.: Enhance-ment of recombinant tissue plasminogen activator (rt-PA) induced thrombolysis in a rabbit arterio-venous shunt model by heparin or a direct thrombin inhibitor MCI-9038 (MCI). Blood (1988) 72:373.
  • SCHNEIDER J: Heparin and the thrombin inhibitor Ar-gatroban enhance flbrinolysis by infused or bolus-injected saruplase (r-scu-PA) in rabbit femoral artery thrombosis. Thromb. Res. (1991) 64(6):677–689.
  • VALJI K, ARUN K, BOOKSTEIN JJ: Use of a direct throm-bin inhibitor (argatroban) during pulse-spray throm-bolysis in experimental thrombosis. J. Vasc. Intervent. Rad. (1995) 6(0:91–95.
  • EISERT WG, KOCH V, RIGTER B et al. Prevention of re- thrombosis after thrombolysis by synthetic thrombin inhibitor argipidine (MD 805). Thromb. Haemost. (1989) 62:329.
  • YAMAMOTO T: Effect of argatroban on flap survival length. Nippon Ika Daigaku ZasshL (1995) 62 (4):351–3559.
  • HANAOKA T: An experimental study of arterial graft implantation - the effects on an anti-thrombin agent, argatroban, and an anti-platelet agent, clopidogrel (SR 25900 C) on the inner capsule. Nippon Geka Gakkai Zasshi. (1994) 95(10):775–785.
  • IMANISHI T, ARITA M, HAMADA M, TOMOBUCHI Y, HANO T, NISHIO I: Effects of local adminstration of ar-gatroban using a hydrogel-coated balloon catheter on intimal thickening induced by balloon injury. Jpn. Circ. J. (1997) 61:256–262.
  • KAWANO M, WATANABE S, SASAKI Y, GIDDINGS JC, YA-MAMOTO J: Adjuvant effect of argatroban on staphy-lokinase induced thrombolysis of platelet rich thrombi in rat mesenteric venules in vivo. Thromb. Res. (1997) 86(2):115–126.
  • TOMODO H: Experimental evaluation of coronary thrombodynamics and effects of pharmacological in-terventions in acute coronary syndromes. Jap. Cir. J. (1992) 56(10:1184–90.
  • OKAMOTO U, NAGAMATSU Y, HORIE N et al.: Variation in activities of non-plasmin flbrinolytic proteinase and plasminogen-activator in the lung and spleen in-duced by bacterial endotoxin in rats with special refer-ence to the effects of MD-805. Thromb. Haemost. (1985) 53 (3):323–327.
  • NAKAMURA M: Prevention of experimental cerebral vasospasm with Argatroban, a selective thrombin in-hibitor. Kobe J. Med. Sci. (1990) 51:387–395.
  • YAMAMOTO T, HIRATA T, INAGAKI M, ITOH J, KIKU-MOTO R, TAMAO Y: Effect of Argatroban (MD 805) on cerebral microcirculation after cerebral ischemia in rats. Jap. Pharm. Thera. (1986) 14 (Suppl. 5):25–32.
  • KAWAI H, YUKI S, SUGIMOTO J, TAMAO Y: Effects of a thrombin inhibitor, argatroban, on ischemic brain damage in the rat distal middle cerebral artery occlu-sion model. J. Pharm. Exp. Ther. (1996) 278(2):780–785.
  • KUMADA T, IWAMOTO M, TOMIKAWA M: Effect of arga-troban on cerebral water content and mortality in ex-perimental rat cerebral infarction. Jap. Pharm. Thera. (1986) 14 (Suppl. 5):33–40.
  • HARA T, IWAMOTO M, ISHIHARA M, TOMIKAWA M: Pre-ventive effect of argatroban on ellagic acid-induced cerebral thromboembolism in rats. Haemostasis (1994) 24:351–357.
  • UMEMURA K, KAWAI H, ISHIHARA H, NAKASHIMA M: In-hibitory effect of clopidogrel, vapiprost and argatro-ban in the middle cerebral artery thrombosis in the rat. Jpn. j Pharm. (1995) 67(3):253–258.
  • TAMAO Y, KIKUMOTO R: Effect of argatroban, a selec-tive thrombin inhibitor, on animal models of cerebral thrombosis. Semin. Thromb. HemosL (1997) 23(6):523–530.
  • IWAKAWA A, GASIC TB, VINER ED et al: Promotion oflung tumor colonization in mice by the synthetic thrombin inhibitor (No. 805) and its reversal by leech salivary gland extracts. Clin. Exp. Metastasis. (1986) 4(3):205–220.
  • HARA H, TAMAO Y, KIKUMOTO R, OKAMOTO S: Effect ofa synthetic thrombin inhibitor MCI-9038 on experi-mental models of disseminated intravascular coagula-tion in rabbits. Thromb. Haemost. (1987) 37 (2) :165–170.
  • MULLER TH, GERSTER U, EISERT WG: Synthetic throm-bin inhibitors (Argipidine, PPACK) are more effective than heparin in a model or arterial reocclusion. Thromb. Haemost. (1989) 62:533.
  • MATSUKURA H, UZAWA S, TAKEDA H, TANABE T: Ex-perimental extracorporeal circulation with a syn-thetic thrombin inhibitor, MD-805, without heparin. J. Jap. Assoc. Thor. Surg. (1983) 31:1377–1382.
  • YAMADA H, KOBAYASHI M, ITO M et al.: Studies on rap-idly progressive glomerulonephritis in rats (Report 2). Antinephritic effect of a newly synthesized antithrom-bin agent, MD 805. Jap. J. Pharm. (1982) 32 (Suppl.):58P.
  • HURSTING MJ, ALFORD KL, BECKER JC: Novastan (brand of argatroban): a small molecule, direct thrombin in-hibitor. Semin. Thromb. HemosL (1997) 23(6)503–516.
  • HURSTING MJ, BECKER JC, JOFFRION JL, KNAPPEN-BERGER GD, SCHWARZ RP: Effect of hepatic function on the pharmacokinetics and pharmacodynamics of Ar-gatroban. Thromb. Haemost. Suppl. (1997)493.
  • KUMON K, TANAKA K, NAKAJIMA N et al: Experiences of treatment of DIC with thrombin inhibitor MD-805 after cardiovascular surgery. Prog. Med. (Japan) (1987)7(2)353–359.
  • HIGUCHI A, HIRANO T, ISHIZAKA T et al.: Clinical report on the treatment of antithrombin MD-805. Ther. Res. (1987) 6:865–871.
  • HIGUCHI M, NAKAJIMA T, KAKISHITA E et al.: Therapeu-tical effect of MD-805, a synthetic antithrombin drug, on disseminated intravascular coagulation. Med. Con-sult. New Drugs (1986) 23(10):2347–2353.
  • HIGUCHI M, KUNITOMI 0, NISHIDA Y et al.: Effect of MD-805, a synthetic thrombin inhibitor, on dissemi-nated intravascular coagulation development on he-matologic disorders. Jap. J. Clin. Hematol.(1985) 26(11)1754–1762.
  • YAMADA K: DIC in Pediatrics. Jap. J. Clin. Hematol. (1982) 23 (6):811–817.
  • KUMON K, TANAKA K, SUGAHARA K eta].: The effect of synthetic thrombin inhibitor MD-805 on DIC before and after cardiovascular surgery. Diagn. Treat. (1983) 71(10) :2208–2212.
  • SUGISHIMA T, MATSUO N et al: Studies on effects of MD-805 of DIC. J. New Rem. Clin. (1987) 36 (2) :171–182.
  • MAEKAWA I et al: Clinical evaluation of synthetic thrombin inhibitor MD-805 in disseminated intravas-cular coagulation (DIC). Ther. Res. (1987) 6(1):409–417
  • FUJITAKA H, TAKAYAMA S, KISHIMOTO H et al.: Clinical experience with the new synthetic thrombin inhibitor MD-805 against acute leukemia complicated by dis-seminated intravascular coagulation (DIC). Igaku to Ya-kugaku. (1987) 17(2):479–485.
  • KITANI M, KOBAYASHI S, YAMAGUCHI S et al.: The effect of an antithrombin agent, MD 805, which acts selec-tively on progressive cerebral thrombosis: compari-son with that of urokinase therapy. Clin. Res. (1986) 63 (9): 251–258.
  • HINO H, KANDA T, TAZAKI Y: Therapeutic effect of the antithrombin agent, MD 805, in the acute stage of cere-bral thrombosis. New Drugs and Clinic (Shin )iaku to Rin-sho) (1987) 36(0:6–10.
  • TAZAKI Y, KOBAYASHI S, TOGI H eta].: Clinical effects of the antithrombin drug, MD 805, on the acute cere-bral thrombosis - clinical study in early Phase II. Jap. Pharm. Therp. (Kiso to Rinsho). (1986) 20(17):9041–9048.
  • KARIO K, KODAMA K, KOIDE M, MATSUO T: Thrombin inhibition in the acute phase of ischaemic stroke using argatoban. Blood Coag. Fibrinol (1995) 6(5) 423–427.
  • KAWADA T, MIEDA T, ABE H et al: Left heart bypass with the bio-medicus centrifugal pump by the use of an antithrombin agent, argatroban. Kyobu Geka. (1994) 47(10)803–808.
  • VERMEER F, VAHANIAN A, FELS PW, BESSE P, RADZIK D, SIMOONS ML: Intravenous argatroban versus heparin as co-medication to alteplase in the treatment of acute myocardial infarction; preliminary results of the AR-GAMI pilot study. J. Am. Coll. Card. (1997) 29(2):185A.
  • SUZUKI S, SAKAMOTO S, ADACHI K et al.: Effect of arga-troban on thrombus formation during acute coronary occlusion after balloon angioplasty. Thromb. Res. (1995) 77 (4):369–373.
  • SUZUKI S, SAKAMOTO S, KOIDE Metal.: Effective antico-agulation by argatroban during immunoadsorption therapy for malignant rheumatoid arthritis with a high polymorphonuclear leukocyte elastase level. Thromb. Res. (1995) 80(1):93–98.
  • KOBAYASHI H, SUZUKI S, SAKAMOTO S, MATSUO T: Ar-gatroban, a direct thrombin inhibitor versus heparin during and after percutaneous transluminal coronary angioplasty (PTCA). Thromb. HaemosL Suppl (1997): 494.
  • LEWIS BE, IQBAL 0, HOPPENSTEADT D et al.: Clinical pharmacokinetic and pharmacodynamic studies on Argatroban to optimize the anticoagulant dosage in in-terventional cardiovascular procedures. Thromb. Hae-most. Suppl (1997):492.
  • IQBAL 0, LEWIS BE, RANGEL Y, SCHWARZ R, WALENGA JM: Monitoring the anticoagulant effects of Argatroban during coronary angioplasty and stenting using a point of care dry reagent test card system and its com-parison with ACT (Hemotec and Hemochron). Thromb. Haemost. Suppl (1997):494.
  • LEWIS BE, GRASSMAN E, WRONA L et al.: Successful use of Argatroban in coronary angioplasty in patients with heparin induced thrombocytopenia syndrome. Thromb. Haemost. Suppl. (1997):494.
  • MATSUO T, KARIO K, SAKAMOTO S et af :Hereditary heparin cofactor II deficiency and coronary artery dis-ease. Thromb Res. (1992) 65:495–505.
  • ITOH T, NONOGI H, MIYAZAKI S, ITOH A, DAIKOKU S: Local delivery of argatroban using drug delivery de-vice 'Dispatch' in the prevention of restenosis follow-ing coronary angioplasty trial (4D-CAT): Result of the prospective randomized pilot study. Circulation (1997) 96(8)::3635.
  • NAGASAWA H: Antithrombin effect of new synthetic thrombin inhibitor, MD-805, on blood coagulation. Biomed. Sci. (1981) 2(2):1–8.
  • IZAWA 0, KATSUKI M, KOMATSU T, IIDA S: Pharmacoki-netics studies of Argatroban (MD-805) in human - con-centrations of argatroban and its metabolites in plasma, urine and feces during and after drip intrave-nous infusion. Jap. Pharm. Ther. (1986) 14 (Suppl. 5)251–262.
  • LEWIS BE, WALENGA JM, WALLIS DE: Anticoagulation with Novastan (Argatroban) in patients with heparin-induced thrombocytopenia and heparin-induced thrombocytopenia and thrombosis syndrome. Semin. Thromb. (1997) 23(2):197–202.
  • SUZUKI S, SAKAMOTO S, KOIDE M, MATSUO M, FUJII K, MATSUO T: Effective anticoagulation by argatroban during coronary stent implantation in a patient with heparin-induced thrombocytopenia. Thromb. Res. (1988) 88:499–502.
  • KOIDE M, YAMAMOTO S, MATSUO M, SUZUKI S, ARIMA N, MATSUO T. Anticoagulation for heparin-induced thrombocytopenia with spontaneous platelet aggrega-tion in a patient requiring haemodialysis. Nephrol. Di-alysis Transpl. (1995) 10(10:2137–2140.
  • MATSUO T, CHIKAHIRA Y, YAMADA T, NAKAO K, UE-SHIMA S, MATSUO 0: Effect of synthetic thrombin in-hibitor (MD805) as an alternative drug on heparin induced thrombocytopenia during hemodialysis. Thromb. Res. (1988) 52:165–171.
  • MATSUO T, KARIO K, CHIKAHIRA Y, NAKAO K, YAMADA T: Treatment of heparin-induced thrombocytopenia by use of argatroban, a synthetic thrombin inhibitor. Br. J. Haematol (1992) 82:627–629.
  • MATSUO T, NAKAO K, YAMADA T, MATSUO 0: A new thrombin inhibitor MD805 and thrombocytopenia en-countered with heparin hemodialysis. Thromb Res. (1986) 44:247–251
  • MATSUO T, YAMADA T, YAMANASHI T, RYO R: Antico-agulant therapy with MD805 of a hemodialysis patient with heparin-induced thrombocytopenia. Thromb. Res. (1990) 58:663–666.
  • MIZE PD, RUBSAMAN K: Dry-chemistry ecarin clotting time for ex vivo monitoring of thrombin inhibitors. Thromb. HaemosL Suppl. (1997):436.
  • AHMAD S, AHSAN A, WALENGA JM, FASANELLA A, SCHWARZ R, FAREED J: Pharmacokinetics of a synthetic antithrombin drug, argatroban, in man as studied by an HPLC method: Implications in the monitoring in septic shock patients. Shock (1997) 7 (Suppl.) :A140.
  • KRISHNAMURTI C, CUTTING MA, REID TJ, ALVING BM: The quantitative thrombin time: A simple, rapid assay for measurement of plasma argatroban levels. Thromb. HaemosL Suppl (1997)92.
  • MESSMORE H, SUNG G, FARID S, IQBAL 0, FABBRINI N: Fibrinogen assay in plasma utilizing Bothrops atrox venom. Thromb. Haemost. Suppl (1997):437.
  • HOPPENSTEADT DA, KAHN S, FAREED J: Factor X values as a means to assess the extent of oral anticoagulation in patients receiving antithrombin drugs. Gin. Chem. (1997) 43(9):1786–1787.
  • HURSTING MJ, ZEHNDER JL, JOFFRION JL, BECKER JC, KNAPPENBERGER GD, SCHWARZ RP: The international normalized ratio during concurrent warfarin and ar-gatroban anticoagulation: differential contributions of each agent and effects of the choice of thromboplas-tin used. Clin. Chem. (1999) 45(3):409–412. Walter Jesket, Jeanine M Walenga, Bruce E Lewis & Jawed Fareed tAuthor for correspondence Loyola University Medical Center, 2160 S. First Ave, Maywood, IL 60153, USA Tel.: +1 708 327 2842; Fax: +1 708 327 2849; Email: [email protected]

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.