Grapefruit juice ingestion significantly reduces talinolol bioavailability

• DOI: 10.1016/j.clpt.2004.11.111
• Publication Date: 2005-04-18T18:21:11Z
• Authors: U SCHWARZ; D SEEMANN; R OERTEL; S MIEHLKE; E KUHLISCH; M FROMM; R KIM; D BAILEY; W KIRCH
• Keywords: Grapefruit juice

Objectives Our objectives were to evaluate the effect of single and repeated grapefruit juice ingestion relative water on oral pharmacokinetics nonmetabolized P-glycoprotein-transported drug talinolol in humans assess potential impact P-glycoprotein intestinal uptake transporters. Methods The 50 mg was determined with water, 1 glass (300 mL), after 6 days (900 mL/d) 24 healthy white volunteers. MDR1 messenger ribonucleic acid levels measured duodenal biopsy specimens obtained from 3 individuals before juice. Three commonly occurring polymorphisms gene also assessed. Results A decreased area under serum concentration-time curve (AUC), peak concentration (Cmax), urinary excretion values 56% (P < .001), 57% respectively, those water. Repeated had a similar (44% 65% reduction; P .01). Single or did not affect renal clearance, elimination half-life, time reach Cmax (tmax). affected by genotypes (C1236T, G2677T/A, C3435T) associated altered pharmacokinetics. Conclusion Because both lowered rather than increased AUC, our findings suggest that constituents preferentially inhibited an process P-glycoprotein. Moreover, alter expression. Clinical Pharmacology & Therapeutics (2005) 77, 291–301; doi: 10.1016/j.clpt.2004.11.111