Effect of Montelukast on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Volunteers
| Autor: | Barry J. Gertz, Marleen Depré, Amanda Freeman, Sherry D. Holland, Kathleen Wynants, Paul J. De Schepper, René Verbesselt, Peggy H. Wong, Inge De Lepeleire, Jef Arnout, Anne Van Hecken |
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| Rok vydání: | 1999 |
| Předmět: |
Adult
Cyclopropanes Male medicine.drug_class Acetates Sulfides Pharmacology Double-Blind Method Pharmacokinetics Oral administration Humans Medicine Drug Interactions Pharmacology (medical) Anti-Asthmatic Agents International Normalized Ratio Montelukast Prothrombin time Cross-Over Studies medicine.diagnostic_test business.industry Anticoagulant Warfarin Anticoagulants Drug interaction Crossover study Area Under Curve Prothrombin Time Quinolines Leukotriene Antagonists business medicine.drug |
| Zdroj: | The Journal of Clinical Pharmacology. 39:495-500 |
| ISSN: | 1552-4604 0091-2700 |
| Popis: | Montelukast, a cysteinyl leukotriene receptor antagonist, is being developed for the treatment of asthma and related diseases. This study was designed to evaluate whether montelukast at clinically used dosage levels would interfere with the anticoagulant effect of warfarin. In a two-period, double-blind, randomized crossover study, 12 healthy male subjects received a single oral dose of 30 mg warfarin on the 7th day of a 12-day treatment with montelukast, 10 mg daily by mouth, or a placebo. Montelukast had no significant effect on the area under the plasma concentration-time curves and peak plasma concentrations of either R- or S-warfarin. However, slight but statistically significant decreases in time to peak concentration of both warfarin enantiomers and in elimination half-life of the less potent R-warfarin were observed in the presence of montelukast. These changes were not considered as clinically relevant. Montelukast had no significant effect on the anticoagulant effect of warfarin, as assessed by the international normalized ratio (INR) for prothrombin time (AUC0-144 and INR maximum). The results of this study suggest that a clinically important interaction between these drugs is unlikely to occur in patients requiring concomitant administration of both drugs. |
| Databáze: | OpenAIRE |
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