Pharmacokinetics of single and repeated oral doses of esomeprazole and gastrin elevation in healthy males and females.
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Issue Date
2020-12-17
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Helgadóttir H, Lund SH, Gizurarson S, Waldum H, Björnsson ES. Pharmacokinetics of single and repeated oral doses of esomeprazole and gastrin elevation in healthy males and females. Scand J Gastroenterol. 2020 Dec 17:1-9. doi: 10.1080/00365521.2020.1859610.Abstract
Objective: Gastrin elevation secondary to proton pump inhibitor (PPI) therapy is well documented. Recent studies have demonstrated a sex-related difference where females on PPIs have significantly higher baseline gastrin levels than males. The aim of the study was to analyse the pharmacokinetics of esomeprazole and short-term effect on serum gastrin levels and evaluate potential sex-related difference. Materials and methods: Healthy volunteers received 40 mg of esomeprazole daily for five days. After the 1st and 5th dose blood samples for fasting gastrin and pharmacokinetic analysis were collected at scheduled time-points for eight hours. Esomeprazole was analysed by liquid chromatography and gastrin concentrations were measured using radioimmunoassay. Results: A total of 30 volunteers were enrolled. Females had higher median baseline gastrin (pM) than males 12 (IQR 10-15) vs. 7 (IQR 4-11) (p = .03). In the study cohort, median gastrin levels rose from 10 (IQR 6-14) to 15 (IQR 13-20) (p = .0002). The serum levels for esomeprazole increased by an average of 299.8 ng/mL (p < .001) from day 1 to day 5. Comparison of the esomeprazole pharmacokinetic parameters between males and females revealed no significant sex-related differences. No significant correlation was found between the AUC and the gastrin level on day 5 (p = .15). Conclusions: In healthy volunteers, serum gastrin increased significantly after a four-day PPI-therapy. There was also a significant increase in serum esomeprazole from day 1 to day 5. The increase in gastrin and esomeprazole concentration was not related to sex and no significant sex-related difference was found in terms of pharmacokinetic parameters. European Clinical Trial Database (2015-002230-41). Keywords: Proton pump inhibitors; area under the serum concentration curve; gastrin; pharmacokinetics; pharmacology; sex-related difference.Description
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https://www.tandfonline.com/doi/full/10.1080/00365521.2020.1859610ae974a485f413a2113503eed53cd6c53
10.1080/00365521.2020.1859610
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