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Omeprazole is used alone or with other medications to treat gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and possible injury of the esophagus. This widely prescribed drug is also used to treat conditions such as dyspepsia, peptic ulcer disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.

Omeprazole is a proton-pump irreversible inhibitors and it is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic health system.

Omeprazole is a racemate. It contains a tricoordinated sulfur atom and can exist in equal amounts of both the S and R enantiomers. In the acidic conditions of the stomach, both are converted to achiral products, which bind irreversibly to sulfhydryl groups present on the active site of the H+/K+ ATPase, thereby inhibiting the ability of the parietal cells to produce gastric acid.