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効能
胃酸分泌抑制薬, 消化性潰瘍薬, プロトンポンプ阻害薬
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説明
Esomeprazole, formulated as a magnesium salt, reached the market as a treatment for
acid-related diseases such as gastro-esophageal reflux (GERD) disease including peptic
ulcer disease and reflux esophagitis. Esomeprazole (formerly perprazole) is the active (S)-
enantiomer of omeprazole (1988) and the first proton pump inhibitor developed as an
optical isomer. It can be obtained by several routes such as asymmetric oxidation of the
pro-chiral pyridylmethyl benzimidazole sulfide, separation from the racemic sulfoxide by
chiral chromatography or separation of a diastereomeric mixture obtained from the racemic
compound and a chiral acid, followed by hydrolysis. Biochemical studies have shown that
esomeprazole irreversibly inhibits the gastric H+/K+-adenosine triphosphatase (ATPase),
an enzyme system involved at the secretory surface of the stomach’s parietal cells
responsible for the secretion of gastric acid. Compared with racemic omeprazole in healthy
subjects, esomeprazole has higher bioavailability, is absorbed more rapidly and exhibits a
more uniform and predictable dose-response with higher plasma levels, leading to less
inter-individual variability between slow and rapid metabolizers. In extensive clinical trials
in patients suffering from GERD symptoms, esomeprazole provided superior acid control
and significantly reduced the healing time compared to omeprazole.
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使用
(-)-Omeprazole can be used to treat migraine.
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使用
Esomeprazole is used to treat certain stomach and esophagus problems (such as acid reflux, ulcers). It works by decreasing the amount of acid your stomach makes. It relieves symptoms such as heartburn, difficulty swallowing, and persistent cough.
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定義
ChEBI: A 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole that has S configuration at the sulfur atom. An inhibitor of gastric acid secretion, it is used (generally as its sodium or magnesium
alt) for the treatment of gastro-oesophageal reflux disease, dyspepsia, peptic ulcer disease, and Zollinger-Ellison syndrome.
