Bioequivalence of ximelagatran, an oral direct thrombin inhibitor, as whole or crushed tablets or dissolved formulation

References

• Leys D. Atherothrombosis: a major health burden. Cerebrovasc Dis 2001;11:1–4
   Web of Science ®Google Scholar
• Fareed J, Hoppensteadt DA, Iqbal O, Bick RL. Current perspectives in antithrombotic therapy. Haemostaseologie 2001;21:82–96
   Google Scholar
• Nordström M, Lindblad B, Bergqvist D, et al. A prospective study of the incidence of deep-vein thrombosis within a defined urban population. J Intern Med 1992;232:155–60
   Google Scholar
• Anderson FA Jr, Wheeler HB, Goldberg RJ, et al. A population-based perspective of the hospital incidence and case-fatality rates of deep vein thrombosis and pulmonary embolism. The Worcester DVT Study. Arch Intern Med 1991;151:933–8
   PubMed Web of Science ®Google Scholar
• Tegos TJ, Kalodiki E, Daskalopoulou SS, et al. Stroke: epidemiology, clinical picture, and risk factors – Part I of III. Angiology 2000;51:793–808
   PubMed Web of Science ®Google Scholar
• Williams GR, Jiang JG, Matchar DB, et al. Incidence and occurrence of total (first-ever and recurrent) stroke. Stroke 1999;30:2523–8
   PubMed Web of Science ®Google Scholar
• Tavazzi L. Clinical epidemiology of acute myocardial infarction. Am Heart J 1999(2 Pt 2);138:S48–54
   Google Scholar
• Stollberger C, Finsterer J, Langer T, et al. Problems, interventions and complications in long-term oral anticoagulant therapy. J Thromb Thrombolysis 2003;14:65–72
   Web of Science ®Google Scholar
• Gautier S, Bachelet H, Bordet R, Caron J. The cost of adverse drug reactions. Expert Opin Pharmacother 2003;3:319–26
   Google Scholar
• Rodrigues HL, Brandao ES, Lima BS. Update of the management of venous thromboembolism. Rev Port Cardiol 2002;21:183–99
   PubMedGoogle Scholar
• Punthakee X, Doobay J, Anand SS. Oral-anticoagulant-related intracerebral hemorrhage. Thromb Res 2003;108:31–6
   Google Scholar
• Martin MT, Codina C, Tuser M, Carne X, Nogue S, Ribas J. Drug related hospital admissions. Med Clin (Barc) 2002;118:205–10
   PubMed Web of Science ®Google Scholar
• Bordet R, Gautier S, Le Louet H, Dupuis B, Caron J. Analysis of the direct cost of adverse drug reactions in hospitalised patients. Eur J Clin Pharmacol 2001;56:935–41
   Google Scholar
• Eriksson UG, Bredberg U, Hoffmann K-J, et al. Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans. Drug Metab Dispos 2003;31:294–305
   Google Scholar
• Eriksson UG, Bredburg U, Gislén K, et al. Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young, healthy male subjects. Eur J Clin Pharmacol 2003;59:35–43
   Google Scholar
• Sarich TC, Eriksson UG, Mattsson C, et al. Inhibition of thrombin generation by the oral direct thrombin inhibitor ximelagatran in shed blood from healthy male subjects. Thromb Haemost 2002;87:300–5
   PubMed Web of Science ®Google Scholar
• Gustafsson D, Antonsson T, Bylund R, et al. Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb Haemost 1998;79:110–8
   PubMed Web of Science ®Google Scholar
• Gustafsson D, Nyström J, Carlsson S, et al. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. Thromb Res 2001;101:171–81
   PubMed Web of Science ®Google Scholar
• Elg M, Gustafsson D, Deinum J. The importance of enzyme inhibition kinetics for the effect of thrombin inhibitors in a rat model of arterial thrombosis. Thromb Haemost 1997;78:1286–92
   Google Scholar
• Elg M, Gustafsson D, Carlsson S. Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat. Thromb Res 1999;94:187–97
   Google Scholar
• Mehta JL, Chen L, Nichols WW, Mattsson C, Gustafsson D, Saldeen TG. Melagatran, an oral active-site inhibitor of thrombin, prevents or delays formation of electrically induced occlusive thrombus in the canine coronary artery. J Cardiovasc Pharmacol 1998;31:345–51
   PubMed Web of Science ®Google Scholar
• Eriksson BI, 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 1997;78:1404–7
   Google Scholar
• Mattsson C, Björkman J-A, Ulvinge J-C. Melagatran, hirudin and heparin as adjuncts to tissue-type plasminogen activator in a canine model of coronary artery thrombolysis. Fibrinol Proteolysis 1997;11:121–8
   Google Scholar
• Sarich TC, Eriksson UG, Mattsson C, et al. Inhibition of thrombin generation by the oral direct thrombin inhibitor ximelagatran in shed blood from healthy male subjects. Thromb Haemost 2002;87:300–5
   PubMed Web of Science ®Google Scholar
• Sarich TC, Wolzt M, Eriksson UG, et al. Effects of ximelagatran, an oral direct thrombin inhibitor, r-hirudin and enoxaparin on thrombin generation and platelet activation in healthy male subjects. J Am Coll Cardiol 2003;41:557–64
   PubMed Web of Science ®Google Scholar
• Eriksson BI, Arfwidsson A-C, Frison L, et al. A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibition in Orthopaedic surgery. Thromb Haemost 2002;87:231–7
   Google Scholar
• Eriksson BI, Bergqvist D, Kälebo P, et al. Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial. Lancet 2002;360:1441–7
   Google Scholar
• Francis CW, Davidson BL, Berkowitz SD, et al. Ximelagatran versus warfarin for the prevention of venous thromboembolism after total knee arthroplasty: a randomized, double-blind trial. Ann Intern Med 2002;137:648–55
   PubMed Web of Science ®Google Scholar
• Eriksson BI, Agnelli G, Cohen AT, et al. Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement. The METHRO III study. Thromb Haemost 2003;89:288–96
   PubMed Web of Science ®Google Scholar
• Heit JA, Colwell CW, Francis CW, et al. Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement: a phase 2 dose-finding study. Arch Intern Med 2001;161:2215–21
   PubMed Web of Science ®Google Scholar
• Francis CW, Berkowitz SD, Comp PC, Lieberman JR, Ginsberg JS, Paiement G, Peters GR, Roth AW, McElhattan JL, Colwell CW Jr for the EXULT A Study Group. Comparison of the oral direct thrombin inhibitor ximelagatran with warfarin for the prevention of venous thromboembolism following total knee replacement: EXULT A. N Engl J Med 2003;349:1703–12
   Google Scholar
• Eriksson H, Wåhlander K, Gustafsson D, et al. A randomized, controlled, dose-guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I. J Thromb Haemost 2003;1:41–7
   PubMed Web of Science ®Google Scholar
• Schulman S, Wåhlander K, Lundström T, Billing Clason S, Eriksson H, for the THRIVE III Investigators. Secondary prevention of venous thromboembolism with the oral direct thrombin inhibitor ximelagatran. N Engl J Med 2003;349:1713–21
   Google Scholar
• Petersen P, Grind M, Adler J for the SPORTIF II Investigators. Ximelagatran versus warfarin for stroke prevention in patients with nonvalvular atrial fibrillation – SPORTIF II: a dose-guiding, tolerability and safety study. J Am Coll Cardiol 2003;41:1445–51
   Google Scholar
• The Executive Steering Committee on behalf of the SPORTIF III Investigators. Stroke prevention with the oral direct thrombin inhibitor ximelagatran compared with warfarin in patients with non-valvular atrial fibrillation: the SPORTIF III trial. Lancet 2003;362:1691–8
   PubMed Web of Science ®Google Scholar
• Wallentin L, Wilcox R, Weaver WD, et al. Efficacy and safety of long term treatment with the oral direct thrombin inhibitor ximelagatran, in combination with acetylsalicylic acid, in patients with a recent acute myocardial infarction: the ESTEEM trial. Lancet 2003;789–97
   PubMedGoogle Scholar
• Grübel P, Cave DR. Factors affecting solubility and penetration of clarithromycin through gastric mucus. Aliment Pharmacol Ther 1998;6:569–76
   Google Scholar
• Weitz JI, Hirsh J. New anticoagulant drugs, Chest 2001;119;S95–107
   Google Scholar
• Hull RD, Pineo GF. Current concepts of anticoagulation therapy. Clin Chest Med 1995;16:269–80
   PubMed Web of Science ®Google Scholar
• Boucher M, Rodger M, Johnson J A, Tierney M. Shifting from inpatient to outpatient treatment of deep vein thrombosis in a tertiary care centre; a cost minimization analysis. Pharmacotherapy 2003;23:301–9
   PubMed Web of Science ®Google Scholar
• Westergren A, Ohlsson O, Rahm Hallberg I. Eating difficulties, complications and nursing interventions during a period of three months after a stroke. J Adv Nurs 2001;35:416–26
   Google Scholar
• Perry L. Screening swallowing function of patients with acute stroke. Part one: identification, implementation and initial evaluation of a screening tool for use by nurses. J Clin Nurs 2001;10:463–73
   Google Scholar
• Penman JP, Thomson M. A review of the textured diets developed for the management of dysphagia. J Hum Nutr Diet 1998;11:51–60
   Web of Science ®Google Scholar
• McNamara EP, Flood P, Kennedy NP. Home tube feeding: an integrated multidisciplinary approach. J Hum Nutr Diet 2001;14:13–9
   Google Scholar