Racecadotril, also known as acetorphan, stands as a pivotal advancement in antidiarrheal medication. Unlike conventional treatments that often work by reducing intestinal motility, Racecadotril offers a distinctive antisecretory mechanism, providing effective relief from acute diarrhea in both adults and children. This unique action profile makes it a highly regarded pharmaceutical active ingredient.
The primary mechanism of action for Racecadotril involves its rapid conversion into its active metabolite, thiorphan. Thiorphan functions as a selective inhibitor of enkephalinase, an enzyme present in the intestinal epithelium. By inhibiting this enzyme, Racecadotril prevents the breakdown of endogenous enkephalins, which are naturally occurring peptides that act on delta-opioid receptors. The increased availability of enkephalins then leads to reduced hypersecretion of water and electrolytes into the intestine, thereby alleviating diarrheal symptoms without causing the constipation or abdominal discomfort often associated with opioid-based antidiarrheals. This makes Racecadotril a well-tolerated and highly effective alternative.
Clinically, Racecadotril is widely recommended as an adjunct to oral rehydration therapy for managing acute watery diarrhea. Its efficacy has been well-documented, showing significant reduction in stool output and duration of diarrhea. For pediatric patients, especially infants over three months and children, Racecadotril is particularly beneficial due to its favorable safety profile and minimal impact on intestinal transit time, which helps prevent dehydration effectively. Its application extends across various regions, including Europe, South America, and parts of Asia, underscoring its global significance in healthcare.
From a pharmacokinetic perspective, Racecadotril is quickly absorbed after oral administration, reaching peak plasma levels within an hour. It is rapidly metabolized to thiorphan, which is extensively bound to plasma proteins (approximately 90%). The inhibitory effect on enkephalinase begins within 30 minutes, peaking around two hours and lasting for up to eight hours, providing sustained therapeutic action. The drug and its inactive metabolites are predominantly excreted via the kidneys, ensuring efficient clearance from the body. Notably, Racecadotril does not cross the blood-brain barrier at therapeutic doses, which contributes to its low incidence of central nervous system side effects.
While generally well-tolerated, common side effects are typically mild, such as headache or skin rashes, occurring in a small percentage of patients. Contraindications include known hypersensitivity to the substance, diarrhea associated with fever or bloody stools, and antibiotic-associated diarrhea. Caution is also advised when co-administering with ACE inhibitors due to a theoretical increase in angioedema risk, though pharmacokinetic interactions with major liver enzymes are minimal, indicating a low potential for drug-drug interactions.
As a leading Racecadotril manufacturer and Racecadotril supplier, NINGBO INNO PHARMCHEM CO.,LTD. is committed to delivering high-quality Active Pharmaceutical Ingredients (APIs) that meet stringent international standards. We understand the critical importance of reliable sourcing for pharmaceutical production. For companies looking to buy Racecadotril or purchase Racecadotril for their formulations, we offer competitive Racecadotril price options and robust supply chain solutions. Our expertise ensures a consistent supply of this essential API, supporting the global demand for effective and safe antidiarrheal treatments.
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