Mechanism of action omeprazole

Pro Research Analysisby

Searched over 200M research papers

Analyzed relevant papers

Mechanism of Action of Omeprazole

Introduction to Omeprazole

Omeprazole is a widely used medication for the treatment of gastric acid-related disorders. It belongs to a class of drugs known as proton pump inhibitors (PPIs) and is primarily used to reduce stomach acid production. This article delves into the detailed mechanisms through which omeprazole exerts its therapeutic effects.

Inhibition of H+/K+ ATPase

Proton Pump Inhibition

The primary mechanism of action of omeprazole is the inhibition of the H+/K+ ATPase enzyme, also known as the gastric proton pump, located in the parietal cells of the stomach. Omeprazole is a prodrug that requires activation in an acidic environment. Once activated, it forms a sulfenamide intermediate that covalently binds to the sulfhydryl groups of the H+/K+ ATPase enzyme, leading to irreversible inhibition of the proton pump and a subsequent reduction in gastric acid secretion 4567.

pH-Dependent Activation

Omeprazole's activation is highly pH-dependent. It is activated in the acidic environment of the parietal cell canaliculi, where it inhibits the H+/K+ ATPase enzyme more effectively at lower pH levels. This specificity ensures that omeprazole acts primarily in the stomach, minimizing systemic side effects 358.

Dual Mechanism: Carbonic Anhydrase Inhibition

Inhibition of Carbonic Anhydrase

In addition to inhibiting the H+/K+ ATPase enzyme, omeprazole also inhibits carbonic anhydrase (CA) isozymes, specifically CA I, II, and IV, in the gastric mucosa. This inhibition is both dose- and pH-dependent. The selective inhibition of gastric mucosa CA IV by omeprazole suggests a dual mechanism of action, which may contribute to its enhanced efficacy in reducing gastric acid secretion 29.

Functional Coupling

The inhibition of both H+/K+ ATPase and carbonic anhydrase enzymes suggests a functional coupling between these two mechanisms. This dual inhibition could explain the superior effectiveness of omeprazole compared to other acid-reducing therapies 29.

Cytoprotective Effects

Interaction with Gastric Mucosa

Omeprazole also exhibits cytoprotective effects on the gastric mucosa. Studies have shown that omeprazole can intercalate among dipalmitoylphosphatidylcholine (DPPC) molecules in the gastric mucosa, promoting the formation of domains with untilted phospholipids. This interaction reinforces and protects the gastric mucosa, providing an additional layer of protection against gastric acid .

Conclusion

Omeprazole's mechanism of action is multifaceted, involving the inhibition of the H+/K+ ATPase enzyme and carbonic anhydrase isozymes, as well as cytoprotective effects on the gastric mucosa. This dual mechanism of action and its pH-dependent activation make omeprazole a highly effective treatment for reducing gastric acid secretion and protecting the stomach lining.

Sources and full results

Most relevant research papers on this topic

Interface-Mediated Mechanism of Action-The Root of the Cytoprotective Effect of Immediate-Release Omeprazole.

Local release of omeprazole in the stomach allows it to act as a phospholipid-like drug, strengthening and protecting the gastric mucosa through electrostatic and hydrophobic interactions.

2021·

4citations

·Daniela Lopes-de-Campos et al.

Omeprazole has a dual mechanism of action: it inhibits both H(+)K(+)ATPase and gastric mucosa carbonic anhydrase enzyme in humans (in vitro and in vivo experiments).

Omeprazole has a dual mechanism of action, inhibiting both H(+)K(+)ATPase and gastric mucosa carbonic anhydrase, potentially explaining its greater effectiveness compared to other therapies.

In Vitro Study

1999·

43citations

·I. Puscas et al.

Studies on the mechanism of action of omeprazole.

Omeprazole inhibits pig gastric (H+ + K+)-ATPase activity with an IC50 of 3.9 microM, with its potency depending on the conditions used and pH.

In Vitro Study

1985·

66citations

·D. Keeling et al.

Structure—activity relationships of omeprazole analogues and their mechanism of action

Omeprazole is a highly selective and effective anti-ulcer agent that inhibits gastric acid secretion by specifically inhibiting H+/K+-ATPase, the gastric proton pump.

1987·

45citations

·P. Lindberg et al.

The mechanism of action of omeprazole--a survey of its inhibitory actions in vitro.

Omeprazole inhibits gastric acid secretion by blocking the gastric H+K+ATPase enzyme, with its inhibitory effects being pH-dependent.

In Vitro StudyHighly Cited

1985·

73citations

·B. Wallmark et al.

Mechanism of action of omeprazole.

Omeprazole effectively inhibits gastric acid secretion by transforming into an inhibitory compound within the acid compartment of the parietal cell.

In Vitro StudyHighly Cited

1986·

80citations

·B. Wallmark

Omeprazole, a long-lasting inhibitor of gastric secretion.

Omeprazole effectively reduces gastric acid secretion in dogs, with 44% suppression still present after 24 hours.

RCTAnimal Study

1984·

6citations

·G. Larson et al.

Omeprazole, a specific inhibitor of gastric (H+-K+)-ATPase, is a H+-activated oxidizing agent of sulfhydryl groups.

Omeprazole effectively inhibits gastric (H+-K+)-ATPase by oxidizing its essential sulfhydryl groups, with acidic environments enhancing its potency.

In Vitro StudyHighly Cited

1985·

93citations

·W. Im et al.

A new concept regarding the mechanism of action of omeprazole.

Omeprazole selectively inhibits gastric mucosa CA IV, with a dual mechanism of action involving H+K+ATPase and carbonic anhydrase inhibition, potentially explaining its higher effectiveness compared to other therapies.

In Vitro Study

1999·

7citations

·I. Puscas et al.

Mechanism of Inhibition of H+K+ATPase by Omeprazole

Omeprazole inhibits gastric acid secretion by targeting the H+K+ATPase enzyme, which is distal to second messenger production and likely close to the proton pump site.

1986·

27citations

·B. Wallmark et al.

Try another search

types of cell in animals

is gerd curable

albuterol sulfate inhalation solution como se usa

omeprazole 20mg tab

total iron

open source a.i