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Most of these medications are benzimidazole derivatives, related to omeprazole, but imidazopyridine derivatives such as tenatoprazole have also been developed. [75] Potassium-competitive inhibitors such as revaprazan reversibly block the potassium-binding site of the proton pump, acting more quickly, but are not available in most countries.
A derivative of timoprazole, omeprazole, was discovered in 1979, and was the first of a new class of drug that control acid secretion in the stomach, a proton pump inhibitor (PPI). [11] [12] Addition of 5-methoxy-substitution to the benzimidazole moiety of omeprazole was also made and gave the compound much more stability at neutral pH. [6]
Omeprazole was patented in 1978, and approved for medical use in 1988. [15] [16] It is on the World Health Organization's List of Essential Medicines. [17] It is available as a generic medication. [1] In 2022, it was the ninth most commonly prescribed medication in the United States, with more than 52 million prescriptions.
Chemically speaking, however, Nexium was extremely similar to Prilosec. There was little evidence that it was better than Prilosec or new generic alternatives. In fact, public health experts argued that many people taking acid inhibitors didn’t need medications at all—they needed to change their diets.
Cimetidine was the prototypical histamine H 2 receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W. Black, C. Robin Ganellin, and others to develop a histamine receptor antagonist that would suppress stomach acid secretion.
Esomeprazole's successful predecessor, omeprazole, is a mixture of two mirror-imaged molecules (esomeprazole which is the S-enantiomer, and R-omeprazole); critics said the company was trying to "evergreen" its omeprazole patent by patenting the pure esomeprazole and aggressively marketing to doctors that it is more effective than the mixture.
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