Trimebutine CAS NO.39133-31-8

Active Pharmaceutical Ingredients 2025-03-03

Catalog ID80017769

CAS NO.39133-31-8

Purity 98%

MDL NumberMFCD00133873

Molecular FormulaC22H29NO5

Molecular Weight387.4694

Melting point: 78~80°C

Aspect Details
Mechanism of Action Trimebutine is a spasmolytic agent that acts directly on smooth muscle to modulate gastrointestinal (GI) motility. It has a dual function: at lower concentrations, it stimulates contractions by inhibiting outward potassium currents, while at higher concentrations, it inhibits contractions by blocking L-type calcium channels. Additionally, it acts as a weak agonist at mu-opioid receptors, providing local anesthetic effects.
Pharmacokinetics – Absorption: Rapidly absorbed after oral administration, with peak plasma concentration reached within 1 hour.<br>- Distribution: Accumulates primarily in the stomach and intestinal walls.<br>- Metabolism: Undergoes extensive hepatic first-pass metabolism, with active metabolites such as N-monodesmethyltrimebutine.<br>- Elimination: Predominantly excreted by the kidneys as metabolites; less than 2.4% of the drug is excreted unchanged in urine.
Indications Used to treat functional gastrointestinal disorders such as irritable bowel syndrome (IBS), gastroesophageal reflux disease (GERD), and functional dyspepsia.
Adverse Effects Generally well-tolerated, but may cause dizziness, somnolence, or gastrointestinal discomfort.
Storage Conditions Store at room temperature, protected from moisture.
Special Considerations – Pregnancy and Lactation: Use with caution; fetal transfer is reported to be low.<br>- Antimicrobial Activity: Preliminary studies suggest trimebutine has in vitro antimicrobial activity against certain bacteria, potentially offering additional therapeutic benefits in post-infectious functional gastrointestinal disorders

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