Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies.

Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies. Research Abstract Details 

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Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies. Abstract Text:

Sonja Eberl,Bertold Renner,Antje Neubert,Mareike Reisig,Iouri Bachmakov, ,Frank ,Thomas E ,Andreas Ackermann,Harald Dormann,Karl G Gassmann,Eckhart G Hahn,Stefanie Zierhut,Kay Brune,Martin F Fromm,Sonja Eberl,Bertold Renner,Antje Neubert,Mareike Reisig,Iouri Bachmakov,Jörg König,Frank Dörje,Thomas E Mürdter,Andreas Ackermann,Harald Dormann,Karl G Gassmann,Eckhart G Hahn,Stefanie Zierhut,Kay Brune,Martin F Fromm,Sonja Eberl,Bertold Renner,Antje Neubert,Mareike Reisig,Iouri Bachmakov, ,Frank ,Thomas E ,Andreas Ackermann,Harald Dormann,Karl G Gassmann,Eckhart G Hahn,Stefanie Zierhut,Kay Brune,Martin F Fromm,

OBJECTIVES: We determined in vitro the potency of macrolides as P-glycoprotein inhibitors and tested in hospitalised patients whether coadministration of P-glycoprotein inhibitors leads to increased serum concentrations of the P-glycoprotein substrates digoxin and digitoxin. METHODS: In vitro, the effect of macrolides on polarised P-glycoprotein-mediated digoxin transport was investigated in Caco-2 cells. In a pharmacoepidemiological study, we analysed the serum digoxin and digitoxin concentrations with and without coadministration of P-glycoprotein inhibitors in hospitalised patients. RESULTS: All macrolides inhibited P-glycoprotein-mediated digoxin transport, with concentrations producing 50% inhibition (IC(50)) values of 1.8, 4.1, 15.4, 21.8 and 22.7 micromol/L for telithromycin, clarithromycin, roxithromycin, azithromycin and erythromycin, respectively. Coadministration of P-glycoprotein inhibitors was associated with increased serum concentrations of digoxin (1.3 +/- 0.6 vs 0.9 +/- 0.5 ng/mL, p < 0.01). Moreover, patients receiving macrolides had higher serum concentrations of cardiac glycosides (p < 0.05). CONCLUSION: Macrolides are potent inhibitors of P-glycoprotein. Drug interactions between P-glycoprotein inhibitors and substrates are likely to occur during hospitalisation.

Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies. Publishing Authors By Initials

S Eberl,B Renner,A Neubert,M Reisig,I Bachmakov,J ,F ,TE ,A Ackermann,H Dormann,KG Gassmann,EG Hahn,S Zierhut,K Brune,MF Fromm,S Eberl,B Renner,A Neubert,M Reisig,I Bachmakov,J König,F Dörje,TE Mürdter,A Ackermann,H Dormann,KG Gassmann,EG Hahn,S Zierhut,K Brune,MF Fromm,S Eberl,B Renner,A Neubert,M Reisig,I Bachmakov,J ,F ,TE ,A Ackermann,H Dormann,KG Gassmann,EG Hahn,S Zierhut,K Brune,MF Fromm,

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Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Clinical pharmacokinetics

VOLUME: 46

Page Numbers: 1039-49

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ISSN: 0312-5963

DAY: 21

MONTH: 11

YEAR: 2007

Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies. Information

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LANGUAGE: eng

NlmUniqueID: 7606849

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Grant and Affiliation Information for Role of p-glycoprotein inhibition for drug interactions : evidence from in vitro and pharmacoepidemiological studies.

AFFILIATION: Institute of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nuremberg, Erlangen, GermanyDepartment of Pharmacy, University Hospital, Erlangen, Germany.

Country: New Zealand

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MEDLINETA: Clin Pharmacokinet

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