Background To detect interaction between nebivolol (N), a unique cardioselective β‐blocker shown to possess vascular endothelial nitric oxide releasing capabilities, and spironolactone by comparing pharmacokinetic (PK) parameters for spironolactone (S) and metabolites, canrenone (C) and 7α‐thiomethyl spirolactone (TMS), in healthy subjects. This potassium‐sparing diuretic (S) is used with β‐blockers to treat CHF. Previously, S showed no effect on the PK of N. Methods Thirty‐six healthy subjects were enrolled, without regard to CYP2D6 genotype, in this open‐label, randomized, one period study. Subjects received once‐daily oral S (25 mg) on Days 1–10 and oral S (25 mg) plus N (10 mg) once‐daily on Days 11–20. Blood samples were collected on Days 10 and 20 and prior to dosing on Days 8, 9, 18, and 19. Plasma concentrations of S, C and TMS were measured by LC/MS. Pharmacokinetic parameter estimates for S, C and TMS were compared by statistical analyses using 90% confidence intervals (CIs). Results All treatments were well tolerated. (see Table) Conclusion Co‐administration of N (10 mg) with S (25 mg) results in no clinically significant changes in the PK profile of S, C or TMS. Clinical Pharmacology & Therapeutics (2005) 77, P46–P46; doi: Cmax AUCT Analyte Ratio 90% CI Ratio 90% CI S1.060.95–1.190.950.90–1.02C1.041.00–1.091.051.03–1.08TMS1.191.10–1.291.141.07–1.20
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.