| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
Sign In to gain access to subscriptions and/or personal tools.
|
|
|
|||||||
Sign In to gain access to subscriptions and/or personal tools. |
|||||||||
DRUG INTERACTIONS |
From Experimental Medicine, AstraZeneca, Wilmington, Delaware, and Mölndal, Sweden.
Ximelagatran—a direct thrombin inhibitor rapidly converted to its active form, melagatran, after oral administration—is being developed for the prevention and treatment of thromboembolic disease. The pharmacokinetics, pharmacodynamics, and tolerability/safety of ximelagatran following a single 36-mg oral dose of ximelagatran ± a single oral dose of alcohol (0.5 and 0.6 g ethanol/kg to women and men, respectively) were assessed in a randomized, open-label, twoway crossover study (n = 26). The 90% confidence intervals (CIs) and least squares mean estimates for the ratio of ximelagatran plus alcohol to ximelagatran alone for melagatran AUC (1.04 [90% CI = 1.00-1.08]) and Cmax (1.08 [90% CI = 1.03-1.14]) fell within the bounds demonstrating no interaction. Alcohol did not alter the melagatran-induced prolongation of the activated partial thromboplastin time or the good tolerability/safety profile of ximelagatran. In conclusion, the pharmacokinetics, pharmacodynamics, and tolerability/safety of oral ximelagatran were not affected by alcohol.
Key Words: Ximelagatran • pharmacokinetics • pharmacodynamics • safety/tolerability • thromboembolic disease • anticoagulants • alcohol
Address for reprints: Troy C. Sarich, PhD, Experimental Medicine, AstraZeneca LP, C4C-123, P.O. Box 15437, 1800 Concord Pike, Wilmington, DE 19850.
This article has been cited by other articles:
|
|
 |
|
  U. G. Eriksson, H. Dorani, J. Karlsson, H. Fritsch, K.-J. Hoffmann, L. Olsson, T. C. Sarich, U. Wall, and K.-M. Schutzer INFLUENCE OF ERYTHROMYCIN ON THE PHARMACOKINETICS OF XIMELAGATRAN MAY INVOLVE INHIBITION OF P-GLYCOPROTEIN-MEDIATED EXCRETION Drug Metab. Dispos., May 1, 2006; 34(5): 775 - 782. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 G. Y.H. Lip Stroke prevention in atrial fibrillation: the case for ximelagatran Eur. Heart J. Suppl., June 1, 2005; 7(suppl_E): E21 - E25. [Full Text] [PDF]
|
|
|
|
|
|
M. O'Donnell, G. Agnelli, and J. I. Weitz Emerging therapies for stroke prevention in atrial fibrillation Eur. Heart J. Suppl., May 1, 2005; 7(suppl_C): C19 - C27. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. Schulman and R. J. Beyth Risk of bleeding with long-term antithrombotic therapy in atrial fibrillation Eur. Heart J. Suppl., May 1, 2005; 7(suppl_C): C34 - C40. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. L. Halperin Ximelagatran: Oral direct thrombin inhibition as anticoagulant therapy in atrial fibrillation J. Am. Coll. Cardiol., January 4, 2005; 45(1): 1 - 9. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 W. E Dager, T. G Vondracek, B. A McIntosh, and E. A Nutescu Ximelagatran: An Oral Direct Thrombin Inhibitor Ann. Pharmacother., November 1, 2004; 38(11): 1881 - 1897. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 T. C. Sarich, K.-M. Schutzer, H. Dorani, U. Wall, I. Kalies, L. Ohlsson, and U. G. Eriksson No Pharmacokinetic or Pharmacodynamic Interaction Between Atorvastatin and the Oral Direct Thrombin Inhibitor Ximelagatran J. Clin. Pharmacol., August 1, 2004; 44(8): 928 - 934. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. C. Sarich, K.-M. Schutzer, M. Wollbratt, U. Wall, E. Kessler, and U. G. Eriksson No Pharmacokinetic or Pharmacodynamic Interaction Between Digoxin and the Oral Direct Thrombin Inhibitor Ximelagatran in Healthy Volunteers J. Clin. Pharmacol., August 1, 2004; 44(8): 935 - 941. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 W. E. Dager Ximelagatran: A New Antithrombotic Option in Atrial Fibrillation Journal of Cardiovascular Pharmacology and Therapeutics, July 1, 2004; 9(3): 151 - 162. [Abstract] [PDF]
|
|
| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
