Trial reportBritish journal of clinical pharmacology2009
Enantioselective disposition of fexofenadine with the P-glycoprotein inhibitor verapamil.
Trial report in British journal of clinical pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 46 citations in OpenAlex.
- Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers.European journal of clinical pharmacology · 2014Trial
- The role of P-glycoprotein in CNS antihistamine effects.Psychopharmacology · 2013Trial
- Enantioselective transplacental transfer of xenobiotics: mechanisms, plasma protein binding, and health implications for fetal development.Archives of toxicology · 2025Review
- Clinical Pharmacokinetics of Fexofenadine: A Systematic Review.Pharmaceutics · 2024Review
- Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability.Therapeutic delivery · 2024Article
- Molecular basis of polyspecific drug and xenobiotic recognition by OCT1 and OCT2.Nature structural & molecular biology · 2023Article
- Effects of Simvastatin on Pharmacokinetics and Anticoagulant Effects of Dabigatran in Healthy Subjects.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Chiral Discrimination of P-glycoprotein in Parturient Women: Effect of Fluoxetine on Maternal-Fetal Fexofenadine Pharmacokinetics.Pharmaceutical research · 2020Article
- Enantioselective Drug Recognition by Drug Transporters.Molecules (Basel, Switzerland) · 2018Review
- Membrane Assays to Characterize Interaction of Drugs with ABCB1.The Journal of membrane biology · 2015Article
- Effects of danshen ethanol extract on the pharmacokinetics of fexofenadine in healthy volunteers.Evidence-based complementary and alternative medicine : eCAM · 2014Article
- Fruit juice inhibition of uptake transport: a new type of food-drug interaction.British journal of clinical pharmacology · 2010Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsThe aim was to compare possible effects of verapamil, as a P-glycoprotein (P-gp) inhibitor, on the pharmacokinetics of each fexofenadine enantiomer, as a P-gp substrate.
methodsThirteen healthy Japanese volunteers (10 male and three female) were enrolled. In a randomized, two-phase, crossover design, verapamil was dosed 80 mg three times daily (with total daily doses of 240 mg) for 6 days, and on day 6, a single 120-mg dose of fexofenadine was administered along with an 80-mg dose of verapamil. Subsequently, fexofenadine was administered alone after a 2-week wash-out period. The plasma concentrations of fexofenadine enantiomers were measured up to 24 h after dosing.
resultsDuring the control phase, the mean AUC(0-infinity) of S(-)- and R(+)-fexofenadine was 700 ng h(-1) ml(-1)[95% confidence interval (CI) 577, 823] and 1202 ng h(-1) ml(-1) (95% CI 1007, 1396), respectively, with a significant difference (P < 0.001). Verapamil had a greater effect on the pharmacokinetic parameters of S(-)-fexofenadine compared with those of the R(+)-enantiomer, and increased AUC(0-infinity) of S(-)-fexofenadine and R(+)-fexofenadine by 3.5-fold (95% CI of differences 1.9, 5.1; P < 0.001) and by 2.2-fold (95% CI of differences 1.7, 3.0; P < 0.001), respectively. The R/S ratio for the AUC(0-infinity) was reduced from 1.76 to 1.32 (P < 0.001) by verapamil treatments.
conclusionThis study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine.
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