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High inter-individual variability of vardenafil pharmacokinetics in patients with pulmonary hypertension
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Analytical Pharmaceutical Chemistry.
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2013 (English)In: European Journal of Clinical Pharmacology, ISSN 0031-6970, E-ISSN 1432-1041, Vol. 69, no 2, 197-207 p.Article in journal (Refereed) Published
Abstract [en]

To evaluate the pharmacokinetic parameters of a single oral dose of vardenafil in patients with pulmonary hypertension (PH). Sixteen patients with PH received vardenafil in single oral doses (20, 10 or 5 mg), and repeated blood sampling for up to 9 h was performed. Vardenafil plasma concentration was determined using liquid chromatography tandem mass spectrometry. Pharmacokinetic parameters were calculated using model-independent analysis. The plasma vardenafil concentration increased rapidly and exhibited a median time to maximum plasma concentration (t(max)) of 1 h and a mean elimination half-life (t(1/2)) of 3.4 h. The geometric mean and standard deviation of (1) the peak plasma concentration (C-max) was 21.4 +/- 1.7 mu g/L, (2) the normalized C-max (C-max,C- norm) 79.1 +/- 1.6 g/L, (3) the area under the time-concentration curve (AUC) 71.5 +/- 1.6 mu g center dot h/L and (4) the normalized AUC (AUC(norm)) 261.6 A +/- 1.7 g center dot h/L. Patients co-medicated with bosentan reached t(max) later and had a 90% reduction of C-max, C-max,C- norm, AUC and AUC(norm). The pharmacokinetic profile of vardenafil overall revealed considerable inter-individual variability in patients with PH. Co-medication with bosentan resulted in a pharmacokinetic drug interaction, leading to significantly decreased plasma concentrations of vardenafil. Therapeutic drug monitoring for individual dose optimization may be warranted.

Place, publisher, year, edition, pages
2013. Vol. 69, no 2, 197-207 p.
Keyword [en]
Vardenafil, Population pharmacokinetics, Pulmonary hypertension, Right heart catheterization, Phosphodiesterase type 5 inhibitors
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-195351DOI: 10.1007/s00228-012-1323-5ISI: 000313791600008OAI: oai:DiVA.org:uu-195351DiVA: diva2:607999
Available from: 2013-02-26 Created: 2013-02-25 Last updated: 2013-02-26Bibliographically approved

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Henrohn, DanHedeland, MikaelBondesson, Ulf G.Wikström, Björn G.
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