Pharmacokinetics of single and repeated oral doses of esomeprazole and gastrin elevation in healthy males and females.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
MetadataShow full item record
CitationHelgadóttir 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.
AbstractObjective: 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.
DescriptionTo access publisher's full text version of this article click on the hyperlink below
- The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study.
- Authors: Shin JS, Lee JY, Cho KH, Park HL, Kukulka M, Wu JT, Kim DY, Park SH
- Issue date: 2014 Sep
- Pharmacokinetics of esomeprazole after oral and intravenous administration of single and repeated doses to healthy subjects.
- Authors: Hassan-Alin M, Andersson T, Bredberg E, Röhss K
- Issue date: 2000 Dec
- Randomised trial of the effect of a gastrin/CCK<sub>2</sub> receptor antagonist on esomeprazole-induced hypergastrinaemia: evidence against rebound hyperacidity.
- Authors: Boyce M, van den Berg F, Mitchell T, Darwin K, Warrington S
- Issue date: 2017 Feb
- Phase I, multicenter, randomized, open-label study evaluating the pharmacokinetics and safety profile of repeated once-daily doses of intravenous esomeprazole in children 0 to 17 years of age.
- Authors: Sandström M, Davidson G, Tolia V, Sullivan JE, Långström G, Lundborg P, Brown K
- Issue date: 2012 Aug
- Clinical impact of CYP2C19 polymorphism on the action of proton pump inhibitors: a review of a special problem.
- Authors: Klotz U
- Issue date: 2006 Jul