P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans

• DOI: 10.5414/cpp38161
• Publication Date: 2011-03-25T08:41:07Z
• Authors: U.I. Schwarz; T. Gramatté; J. Krappweis; R. Oertel; W. Kirch
• Keywords: Crossover study

Increased bioavailability of the P-glycoprotein (Pgp) substrates digoxin and cyclosporin due to erythromycin has been observed in vivo. The aim present study was investigate effect orally administered on oral beta-blocker talinolol. Talinolol is a suitable model compound for Pgp drug-drug interaction studies its Pgp-related active intestinal secretion lack any significant metabolism.In randomized crossover study, pharmacokinetics talinolol (50 mg) after concomitant single dose (2 g) or placebo were investigated 9 healthy men. Concentrations measured serum urine by HPLC.The area under curve concentrations from 0 24 h (AUC(0-24)) maximum (Cmax) significantly increased administration compared placebo. t(max) values reduced. renal clearance (CLR) unchanged co-administration there small but statistically decrease elimination half-life (t1/2). Serum correlate with results derived concentration measurement. One subject suffered moderate diarrhea excluded analysis.We suggest that increase caused net absorption inhibition erythromycin.