Racecadotril

Racecadotril, also known as acetorphan, is an antidiarrheal medication used to treat acute diarrhea. It is a peripheral enkephalinase inhibitor that reduces the secretion of water and electrolytes into the intestine, thereby decreasing the volume of diarrhea.

Mechanism of Action

Racecadotril acts by inhibiting the enzyme enkephalinase, which is responsible for the breakdown of enkephalins. Enkephalins are endogenous peptides that modulate the secretion of water and electrolytes in the gastrointestinal tract. By preventing their degradation, racecadotril enhances the activity of enkephalins, leading to reduced intestinal secretion and decreased diarrhea.

Racecadotril chemical structure

Pharmacokinetics

After oral administration, racecadotril is rapidly absorbed and converted into its active metabolite, thiorphan. The onset of action is typically within 30 minutes, and the duration of effect lasts for several hours. Racecadotril is primarily metabolized in the liver and excreted in the urine.

Clinical Use

Racecadotril is indicated for the symptomatic treatment of acute diarrhea in adults and children. It is often used in conjunction with oral rehydration therapy to ensure adequate hydration. Unlike some other antidiarrheal agents, racecadotril does not affect intestinal motility, making it a preferred choice in certain clinical scenarios.

Side Effects

Common side effects of racecadotril include headache, rash, and nausea. It is generally well-tolerated, but hypersensitivity reactions can occur in some individuals. It is important to monitor for signs of allergic reactions, especially in patients with a history of allergies.

Contraindications

Racecadotril should not be used in patients with known hypersensitivity to the drug or any of its components. It is also contraindicated in patients with chronic diarrhea, such as that caused by inflammatory bowel disease.

Racecadotril Metabolites

Racecadotril metabolites

The primary active metabolite of racecadotril is thiorphan, which is responsible for its therapeutic effects. Thiorphan acts by inhibiting enkephalinase, thereby prolonging the action of enkephalins in the gut.

Related Pages

• Antidiarrheal
• Enkephalinase
• Oral rehydration therapy