Structural characterization of the optical isomers esomeprazole and omeprazole using the JADER and FAERS databases.

Abstract

BACKGROUND:

It is unclear whether the s (-) form of esomeprazole (EPZ) has an improved safety profile when compared with its racemic form omeprazole (OPZ). We assessed the potential complications of these optical isomers when combined with cilostazol, clopidogrel, and prasugrel, which are frequently used concomitant medications.

METHODS:

Using two adverse event spontaneous reporting databases, Japanese Adverse Drug Event Report (JADER) and FDA Adverse Event Reporting System (FAERS), adverse event names for hemorrhage, venous/arterial embolization, and thrombus were obtained from the Medical Dictionary for Regulatory Activities. Reported odds ratios were calculated using a 2 × 2 contingency table, and a signal was considered present if the lower limit of the 95% confidence interval was >1.

RESULTS:

In combination with cilostazol, a hemorrhagic signal for OPZ in JADER and arterial emboli and thrombus signals for EPZ were detected in both databases. In combination with clopidogrel, OPZ showed arterial emboli and thrombus signals in JADER and venous/arterial emboli and thrombus signals in FAERS, while EPZ displayed arterial emboli and thrombus signals in FAERS. In contrast, when in combination with prasugrel, there were no adverse event signals in either database.

CONCLUSION:

This study has confirmed using big data, that EPZ, the optical isomer and racemic form of omeprazole, has the beneficial characteristics of being less sensitive to CYP, as was intended by its design.

• Authors: Mami Neishi, Hirofumi Hamano, Takahiro Niimura, Masaya Denda, Kenta Yagi, Koji Miyata, Tsung-Jen Lin, Tsukasa Higashionna, Mitsuhiro Goda, Yoshito Zamami, Keisuke Ishizawa, Hideki Nawa
• Journal: Toxicology and applied pharmacology (Toxicol Appl Pharmacol) Vol. 475 Pg. 116632 (09 15 2023) ISSN: 1096-0333 [Electronic] United States
• PMID: 37482254 (Publication Type: Journal Article)
• Copyright: Copyright © 2023 Elsevier Inc. All rights reserved.

Chemical References

• Esomeprazole
• Omeprazole
• Clopidogrel
• Prasugrel Hydrochloride
• Cilostazol

Topics

• Humans
• United States
• Esomeprazole (adverse effects)
• Omeprazole (adverse effects)
• Clopidogrel
• Prasugrel Hydrochloride
• Cilostazol
• Adverse Drug Reaction Reporting Systems
• Hemorrhage
• Drug-Related Side Effects and Adverse Reactions
• Databases, Factual