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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. [50]
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 a subject of a patent litigation in the U.S. [66] The invention involved application of two different coatings to a drug in pill form to ensure that the omeprazole did not disintegrate before reaching its intended site of action in stomach. Although the solution by means of two coating was obvious, the patent was found valid ...
[20] [21] [22] In the United States, the Food and Drug Administration (FDA) has advised that over-the-counter PPIs, such as Prilosec OTC, should be used no more than three 14-day treatment courses over one year. [23] [24] Despite their extensive use, the quality of the evidence supporting their use in some of these conditions is variable.
The proton-pump inhibitor Nexium by AstraZeneca is a me-too which was granted its patent by showing that it was effective for heartburn, not that it was better than its precursor, Prilosec. [10] It was shown to preserve revenues of Prilosec, whose U.S. patent expired in 2001.
Depakote (valproic acid/sodium valproate) – an antiepileptic and mood stabilizer used to treat bipolar disorder, neuropathic pain and others; sometimes called an antimanic medication.