Racecadotril

Racecadotril is an Enkephalinase inhibitor belonging to an Antidiarrheal agent.

Racecadotril is an anti-secretory enkephalinase inhibitor useful in the treatment of diarrhea.

Racecadotril is rapidly absorbed. Delayed time to peak activity by 1-1.5 hours with food. Racecadotril has plasma protein binding 90%, mainly to albumin (thiorphan). Racecadotril rapidly hydrolyzed to thiorphan glycine (active metabolite), which is further metabolized to inactive metabolites. Racecadotril is mainly excreted via urine (81.4%); feces (approx. 8%); as active and inactive metabolites. The elimination half-life: Approx 3 hours (Racecadotril).

Racecadotril shows side effects like Tonsilitis, Skin rash, swelling of the face and lips, Headache, and Difficulty to breath.

Racecadotril is available in the form of Oral Capsules, powder for suspension, powder for solution, and granules for suspension.

Racecadotril is available in India, the US, Canada, France, Germany, Italy, Russia, and Australia.

Racecadotril belongs to the Antidiarrheal agent and acts as an Enkephalinase inhibitor.

Racecadotril is a prodrug of thiorphan, which is an inhibitor of enkephalinase, a cell membrane peptidase enzyme that aids in the hydrolysis of exogenous peptides and the breakdown of endogenous peptides (e.g. enkephalins). Inhibition of enkephalinase enzymatic degradation prolongs peptide action at enkephalinergic synapses in the small intestine and decreases hypersecretion without affecting basal secretion.

The Onset of action of Racecadotril is about 1-2 hours.

The Tmax of Racecadotril is 6-8 hours.

Racecadotril is an antidiarrheal that works by decreasing intestinal secretion. The treatment should be continued until the frequency of stools reached two. The treatment should be discontinued if any symptoms of skin reactions appear.

Racecadotril is approved for use in the following clinical indications

• Acute diarrhea

Racecadotril is an anti-secretory enkephalinase inhibitor useful in the treatment of diarrhea.

• Acute diarrhea

Adult: Initially, 100 mg to be taken regardless of the time of the day, then 100 mg three times a day, preferably before main meals. Continue treatment until 2 normal stools are recorded. Max duration of treatment: 7 days. Dosage recommendations may vary among countries and individual products.

Child: In combination with oral rehydration: As granules/powder for oral use: Recommended dose: 1.5 mg/kg three times a day. Max: Approx 6 mg/kg daily. Usual doses: Infants (>3 months) <9 kg: 10 mg; 9-<13 kg: 20 mg; Children 13-27 kg: 30 mg; >27 kg: 60 mg. All doses are to be taken three times a day. Continue treatment until 2 normal stools are recorded. Max duration of treatment: 7 days. Dosage recommendations may vary among countries and individual products.

Racecadotril is available in various strengths as 100mg, 10mg, 15mg, and 30mg.

Racecadotril is available in the form of Oral Capsules, powder for suspension, powder for solution, and granules for suspension.

• Dosage Adjustment in Kidney Patient

Racecadotril is not recommended in patients with kidney impairment.

• Dosage Adjustment in Hepatic impairment Patient

Racecadotril is not recommended in patients with liver impairment.

Racecadotril is contraindicated in patients with

• Diarrhea associated with fever and/or bloody or purulent stools; antibiotic-associated diarrhea.
• Patients who have experienced angioedema with ACE inhibitors.

• Severe diarrhea

Racecadotril is not effective in severe diarrhea patients and in antibiotic-associated diarrhea patients.

• Pediatric use

Racecadotril is not recommended in children less than 3 months.

• Impaired kidney function

Racecadotril is not recommended in patients with kidney impairment.

• Impaired liver function

Racecadotril is not recommended in patients with liver impairment.

• Severe vomiting

The availability of Racecadotril is decreased in patients with severe vomiting, therefore not used in patients with severe vomiting.

• Skin reactions

Racecadotril is known to cause mild to moderate skin reactions. The treatment should be discontinued if any symptoms of skin rash appear.

Common

● Hypersensitivity or angioedema, Headache, Tonsillitis (particularly in infants or children), Rash, erythema nodosum, erythema multiforme, urticaria, papular rash, prurigo, pruritus, severe skin reactions.

• ACE inhibitors

May increase the risk of angioedema with ACE inhibitors (e.g., captopril, enalapril).

The common side effects of Racecadotril include the following

Common side effects

● Tonsilitis, Skin rash, swelling of face and lips, Headache, Difficulty to breath.

Pharmacodynamic

Information is not available.

Pharmacokinetics

• Absorption

Racecadotril is rapidly absorbed. Delayed time to peak activity by 1-1.5 hours with food.

• Distribution

Racecadotril has plasma protein binding 90%, mainly to albumin (thiorphan).

• Metabolism and Excretion

Racecadotril rapidly hydrolyzed to thiorphan glycine (active metabolite), which is further metabolized to inactive metabolites. Racecadotril is mainly excreted via urine (81.4%); feces (approx. 8%); as active and inactive metabolites. The elimination half-life: Approx 3 hours (Racecadotril).

• https://www.mims.com/india/drug/info/racecadotril?type=full&mtype=generic
• https://www.practo.com/medicine-info/racecadotril-240-api
• https://www.medindia.net/doctors/drug_information/racecadotril.htm#howtake