INFLUENCE OF ERYTHROMYCIN ON THE PHARMACOKINETICS OF XIMELAGATRAN MAY INVOLVE INHIBITION OF P-GLYCOPROTEIN-MEDIATED EXCRETION

• Published in: Drug metabolism and disposition Vol. 34; no. 5; pp. 775 - 782
• Main Authors: ERIKSSON, Ulf G, DORANI, Hassan, KARLSSON, Johan, FRITSCH, Holger, HOFFMANN, Kurt-Jürgen, OLSSON, Lis, SARICH, Troy C, WALL, Ulrika, SCHÜTZER, Kajs-Marie
• Format: Journal Article
• Language: English
• Published: Bethesda, MD American Society for Pharmacology and Experimental Therapeutics 01.05.2006
• Subjects: Adult; Animals; Anti-Bacterial Agents - adverse effects; Anti-Bacterial Agents - pharmacology; Antimalarials - pharmacology; ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors; ATP-Binding Cassette, Sub-Family B, Member 1 - physiology; Azetidines - adverse effects; Azetidines - pharmacokinetics; Benzylamines - adverse effects; Benzylamines - pharmacokinetics; Bile - metabolism; Biological and medical sciences; Biological Transport, Active; Caco-2 Cells; Calcium Channel Blockers - pharmacology; Cell Line; Dogs; Dose-Response Relationship, Drug; Drug Interactions; Erythromycin - adverse effects; Erythromycin - pharmacology; Female; Humans; In Vitro Techniques; Male; Medical sciences; Partial Thromboplastin Time; Pharmacology. Drug treatments; Quinidine - pharmacology; Rats; Rats, Sprague-Dawley; Verapamil - pharmacology; Excretion; Serine endopeptidases; Hemostatic; Enzyme; P Glycoprotein; Enzyme inhibitor; Thrombin; Erythromycin; Prodrug; Ximelagatran; Antithrombin; Macrolide; Peptidases; Antibiotic; Antithrombotic agent; Hydrolases; Inhibition; Antibacterial agent; Pharmacokinetics

A pharmacokinetic interaction between erythromycin and ximelagatran, an oral direct thrombin inhibitor, was demonstrated in this study in healthy volunteers. To investigate possible interaction mechanisms, the effects of erythromycin on active transport mediated by P-glycoprotein (P-gp) in vitro in...