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Prokinetics and fundic relaxants in upper functional GI disorders.
1Center for Gastroenterological Research, KU Leuven, Belgium. Jan.Tack@med.kuleuven.ac.be
Current Opinion in Pharmacology
|October 23, 2008
Summary
Gastrointestinal prokinetic drugs and fundic relaxant agents are explored for motility disorders. Establishing symptomatic benefit remains challenging due to patient variability and outcome measurement issues.
Area of Science:
- Pharmacology
- Gastroenterology
- Drug Discovery
Background:
- Gastrointestinal prokinetics enhance gastric emptying and intestinal transit by stimulating smooth muscle contractions.
- Recent prokinetic agents include antidopaminergic, serotonergic, motilin receptor, and ghrelin receptor agonists.
- Challenges in treating gastroparesis and functional dyspepsia include patient heterogeneity and unclear links between motor function and symptoms.
Purpose of the Study:
- To review recently studied gastrointestinal prokinetic drugs.
- To introduce fundic relaxant drugs as a novel approach for gastric motility disorders.
- To highlight challenges in establishing symptomatic benefit for prokinetic therapies.
Main Methods:
- Literature review of recently studied prokinetic agents.
- Identification of novel fundic relaxant drug classes and examples.
- Analysis of difficulties in clinical trial endpoints for motility disorders.
Main Results:
- Several classes of prokinetic drugs have been investigated, including itopride, tegaserod, mitemcinal, and TZP101.
- Fundic relaxant drugs represent a different therapeutic strategy, with agents like nitrates, serotonin reuptake blockers, 5-HT(1A) receptor agonists (buspirone, R137696), and muscarinic M1/M2 receptor antagonists (acotiamide) under study.
- Consistent symptomatic improvement has been difficult to demonstrate for prokinetic drugs in gastroparesis and functional dyspepsia.
Conclusions:
- Prokinetic drug development faces hurdles related to patient population heterogeneity and outcome assessment.
- Fundic relaxant drugs offer an alternative therapeutic avenue for gastric motility disorders.
- Further research is needed to refine endpoints and demonstrate efficacy for both prokinetic and fundic relaxant agents.
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