Background: Proton pump inhibitors (PPIs) are a group of gastric acid suppressing
drugs, they work by irreversibly blocking the H+/K+ ATPase. The structure of PPIs is similar.
They all have a similar core with a sulphur atom chiral center combined with different substituent
groups. In relation to the sulphur atom chiral center, the pharmacodynamics, pharmacokinetics
are diverse between the racemates and their stereoisomers. But there are no reviews outlining the
stereoselective pharmacodynamics and pharmacokinetics in PPIs. This review aims to compare
the differences between the stereoisomers of PPIs in their pharmacodynamics and pharmacokinetics
parameters. And exploring the development directions of PPIs at present.
Methods: We undertook a search of PubMed databases for PPI research literature including
reviews, clinical studies, letters and books, in recent 20 years. The citied papers were high quality,
which were carefully screened by authors using standard tools. The data of the pharmacodynamics
and pharmacokinetics parameters were selected from the retrieved papers, then making
generalization and summary.
Results: Ninety-three papers were included in the review, mainly from East Asia, America and Europe. All these papers
involved the reviews of PPIs, the pharmacodynamics studies of PPIs and the pharmacokinetics studies of PPIs.
Finally, omeprazole, lansoprazole, pantoprazole, rebeprazole and pantoprazole with their enantiomers were discussed
in this paper.
Conclusion: The findings of this review confirm the differences of pharmacodynamics and pharmacokinetics in the
racemates and the stereoisomer of PPIs. Providing longer duration, faster time of onset and better nocturnal gastric acid
secretion control are the development directions of new generation PPIs. But, due to debate on the necessity and superiority
of these new drugs, more validation studies are needed.