Document Detail

Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct factor Xa inhibitor, in healthy subjects.
MedLine Citation:
PMID:  16638738     Owner:  NLM     Status:  MEDLINE    
To investigate the influence of food and administration of an antacid (aluminum-magnesium hydroxide) or ranitidine on the absorption of BAY 59-7939 (rivaroxaban), 4 randomized studies were performed in healthy male subjects. In 2 food interaction studies, subjects received BAY 59-7939, either as two 5-mg tablets (fasted and fed), four 5-mg tablets (fasted), or one 20-mg tablet (fasted and fed). In 2 drug interaction studies, BAY 59-7939 (six 5-mg tablets) was given alone or with ranitidine (150 mg twice daily, preceded by a 3-day pretreatment phase) or antacid (10 mL). Plasma samples were obtained to assess pharmacokinetic and pharmacodynamic parameters of BAY 59-7939. In the presence of food, time to maximum concentration (t(max)) was delayed by 1.25 hours; maximum concentration (C(max)) and area under the curve (AUC) were increased, with reduced interindividual variability at higher doses of BAY 59-7939. Compared with baseline, BAY 59-7939 resulted in a relative increase in maximum prothrombin time (PT) prolongation of 44% (10 mg) and 53% (20 mg) in the fasted state, compared with 53% and 83% after food. Time to maximum PT prolongation was delayed by 0.5 to 1.5 hours after food, with no relevant influence of food type. No significant difference in C(max) and AUC was observed with coadministration of BAY 59-7939 and ranitidine or antacid.
Dagmar Kubitza; Michael Becka; Michael Zuehlsdorf; Wolfgang Mueck
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Publication Detail:
Type:  Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  46     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2006 May 
Date Detail:
Created Date:  2006-04-26     Completed Date:  2006-12-12     Revised Date:  2009-11-02    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  549-58     Citation Subset:  IM    
Institute of Clinical Pharmacology, Bayer HealthCare AG, Wuppertal, Germany.
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MeSH Terms
Aluminum Hydroxide / pharmacology
Antacids / pharmacology*
Cross-Over Studies
Dietary Carbohydrates / pharmacology
Dietary Fats / pharmacology
Drug Combinations
Drug Interactions
Factor Xa / antagonists & inhibitors
Fasting / metabolism
Food-Drug Interactions*
Histamine H2 Antagonists / pharmacology
Intestinal Absorption / drug effects
Magnesium Hydroxide / pharmacology
Morpholines / adverse effects,  blood,  pharmacokinetics*,  pharmacology
Prothrombin Time
Ranitidine / pharmacology*
Thiophenes / adverse effects,  blood,  pharmacokinetics*,  pharmacology
Reg. No./Substance:
0/Antacids; 0/Dietary Carbohydrates; 0/Dietary Fats; 0/Drug Combinations; 0/Histamine H2 Antagonists; 0/Morpholines; 0/Thiophenes; 0/rivaroxaban; 1309-42-8/Magnesium Hydroxide; 21645-51-2/Aluminum Hydroxide; 37317-08-1/aluminum hydroxide, magnesium hydroxide, drug combination; 66357-35-5/Ranitidine; EC Xa

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