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Toward More GI-Friendly Anti-Inflammatory Medications
John L Wallace1,2,3, Gilberto de Nucci4, Oksana Sulaieva5
1Department of Physiology & Pharmacology, University of Calgary, Calgary, AB, Canada. altapharm@hotmail.com.
Current Treatment Options in Gastroenterology
|August 26, 2015
Summary
Hydrogen sulfide (H2S)-releasing nonsteroidal anti-inflammatory drugs (NSAIDs) offer a novel solution to gastrointestinal (GI) damage. These H2S-NSAIDs demonstrate potent anti-inflammatory effects with significantly reduced GI toxicity.
Area of Science:
- Gastroenterology
- Pharmacology
- Drug Development
Background:
- Nonsteroidal anti-inflammatory drugs (NSAIDs) cause significant gastrointestinal (GI) adverse effects, including small intestinal injury, despite existing acid secretion inhibitors.
- Current treatments like proton pump inhibitors (PPIs) and histamine H2-receptor antagonists (H2RAs) may worsen NSAID-induced small intestinal damage.
- NSAID-induced GI damage remains a considerable clinical concern and economic burden.
Purpose of the Study:
- To explore a new therapeutic strategy for mitigating NSAID-induced GI damage.
- To evaluate the potential of endogenous, cytoprotective molecules as adjuncts to NSAIDs.
- To assess the efficacy and safety of hydrogen sulfide (H2S)-releasing NSAIDs.
Main Methods:
- Synthesis and laboratory testing of H2S-releasing NSAIDs.
- Preclinical and clinical evaluation of H2S-NSAIDs in animal models and human subjects.
- Assessment of anti-inflammatory activity and GI tolerability.
Main Results:
- H2S-releasing NSAIDs exhibit enhanced anti-inflammatory activity compared to parent NSAIDs.
- H2S-NSAIDs cause negligible damage to the GI tract.
- This approach offers a promising alternative for managing pain and inflammation with improved GI safety.
Conclusions:
- Hydrogen sulfide (H2S) acts as a potent endogenous cytoprotective agent in the GI tract.
- H2S-releasing NSAIDs represent a novel therapeutic class with significant potential for reducing NSAID-induced GI injury.
- This innovative strategy addresses a critical unmet need in managing chronic inflammatory conditions.
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