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- Open Access
Effects of omeprazole and AlOH/MgOH on riociguat absorption
- Corina Becker†1Email author,
- Reiner Frey1,
- Sigrun Unger2,
- Ulrike Artmeier-Brandt1,
- Gerrit Weimann1 and
- Wolfgang Mueck1
© Becker et al; licensee BioMed Central Ltd. 2013
- Published: 29 August 2013
Riociguat, a soluble guanylate cyclase stimulator, is currently under investigation for the treatment of pulmonary hypertension. The present studies investigated the influence of omeprazole and AlOH/MgOH on riociguat absorption and bioavailability.
The pharmacokinetics of oral, single-dose, immediate-release riociguat 2.5 mg were characterized in two open-label, randomized, crossover studies in healthy males. In the first study, subjects pretreated for 4 days with once-daily omeprazole 40 mg received co-treatment with omeprazole + riociguat or riociguat alone (no pretreatment) on Day 5 (n=12). In the second study, subjects received co-treatment with 10 mL AlOH/MgOH + riociguat or riociguat alone (n=12). Pharmacokinetic characteristics were analyzed assuming log-normally distributed data. Safety and tolerability were also assessed.
Riociguat pharmacokinetic parameters (geometric means and coefficients of variation)
Riociguat 2.5 mg (n=12)
Riociguat 2.5 mg + omeprazole (n=12)
Riociguat 2.5 mg (n=12)
Riociguat 2.5 mg + AlOH/MgOH (n=12)
Treatment with riociguat, with or without omeprazole or AlOH/MgOH, was well tolerated, with a good safety profile. The results confirm the lower bioavailability of riociguat in neutral versus acidic medium as expected from in vitro data. For co-medication of antacids like AlOH/MgOH, staggered intake between riociguat and antacid is practically possible and may be advisable. A general dose adaptation for patients with co-medication acting on gastric acidity, beyond the dose titration concept for riociguat, is not recommended.
The studies were funded by Bayer HealthCare Pharmaceuticals, Wuppertal, Germany. Medical writing assistance was provided by Adelphi Communications Ltd, Bollington, UK and funded by Bayer HealthCare Pharmaceuticals.
This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.