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药品详细

Esomeprazole (埃索美拉唑 )

化学结构式图
中文名
埃索美拉唑
英文名
Esomeprazole
分子式
Not Available
化学名
6-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methane]sulfinyl}-1H-1,3-benzodiazole
分子量
Average: 345.416
Monoisotopic: 345.114712179
CAS号
161796-78-7
ATC分类
A02B 未知;A02B 未知
药物类型
small molecule
阶段
商品名
Axagon;Esopral;Lucen;Nexiam;Nexium;Nexium IV;
同义名
esomeprazole;Esomeprazole Sodium;Esomperazole;
基本介绍

A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H()-K()-ATPase (H()-K()-exchanging ATPase) in the proton pump of gastric parietal cells. [PubChem]

生产厂家
  • Astrazeneca lp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Lind T, Rydberg L, Kyleback A, Jonsson A, Andersson T, Hasselgren G, Holmberg J, Rohss K: Esomeprazole provides improved acid control vs. omeprazole In patients with symptoms of gastro-oesophageal reflux disease. Aliment Pharmacol Ther. 2000 Jul;14(7):861-7. Pubmed
剂型
Form Route Strength
Capsule, delayed release Oral 20 mg
Capsule, delayed release Oral 40 mg
Granule, for suspension Oral 10 mg per packet
Granule, for suspension Oral 20 mg per packet
Granule, for suspension Oral 40 mg per packet
Injection Intravenous 20 mg
Injection Intravenous 40 mg
规格
Unit description Cost Unit
Nexium i.v. 20 mg vial 33.91 USD vial
Nexium i.v. 40 mg vial 33.91 USD vial
NexIUM 20 mg Delayed Release Capsule 6.76 USD capsule
NexIUM 40 mg Delayed Release Capsule 6.76 USD capsule
Nexium 10 mg packet 6.5 USD each
Nexium 20 mg capsule 6.5 USD capsule
Nexium 20 mg packet 6.5 USD each
Nexium 40 mg capsule 6.5 USD capsule
Nexium 40 mg packet 6.5 USD each
化合物类型
Type small molecule
Classes
  • Phenols and Derivatives
  • Benzimidazoles
  • Ethers
  • Anisoles
Substructures
  • Phenols and Derivatives
  • Benzimidazoles
  • Pyridines and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Imines
  • Cyanamides
  • Phenyl Esters
  • Sulfoxides
适应症
gastric acid RELATED DISORDERS 中和胃酸;
药理
Indication For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.
Pharmacodynamics Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
Mechanism of action Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Absorption 90%
Volume of distribution
  • 16 L [healthy volunteers]
Protein binding 97%
Metabolism

Mainly hepatic. Esomeprazole is completely metabolized by the cytochrome P450 system via CYP2C19 and CYP3A4. Metabolism produces inactive hydroxy and desmethyl metabolites, which have no effect on gastric acid secretion. Less than 1% of the parent drug is excreted in urine.

Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 2C19 5-hydroxyesomeprazole 5-hydroxylation
Route of elimination Approximately 80% of the administered dose of esomeprazole is excreted as metabolites in urine and the remaining 20% is excreted in feces.
Half life 1-1.5 hours
Clearance Not Available
Toxicity Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00225 Esomeprazole Pathway SMP00225
理化性质
Properties
State solid
Melting point 155 oC
Experimental Properties
Property Value Source
water solubility Very slightly soluble in water PhysProp
logP 0.6 PhysProp
Predicted Properties
Property Value Source
water solubility 3.59e-01 g/l ALOGPS
logP 1.66 ALOGPS
logP 2.43 ChemAxon Molconvert
logS -2.98 ALOGPS
pKa 18.29 ChemAxon Molconvert
hydrogen acceptor count 5 ChemAxon Molconvert
hydrogen donor count 1 ChemAxon Molconvert
polar surface area 77.10 ChemAxon Molconvert
rotatable bond count 5 ChemAxon Molconvert
refractivity 93.66 ChemAxon Molconvert
polarizability 37.45 ChemAxon Molconvert
药物相互作用
Drug Interaction
Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
Enoxacin Esomeprazole may decrease the absorption of enoxacin.
Indinavir Omeprazole decreases the absorption of indinavir
Itraconazole The proton pump inhibitor, esomeprazole, may decrease the absorption of itraconazole.
Ketoconazole The proton pump inhibitor, esomeprazole, may decrease the absorption of ketoconazole.
Tipranavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Esomeprazole. Consider alternate therapy or increase the dose of Esomeprazole based on the therapeutic response.
食物相互作用
  • Take without regard to meals.

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