CHEARS

What is Racecadotril?

Racecadotril is a lipophilic derivative of thiorphan. It is a prodrug which is rapidly converted to thiorphan. It is the only drug which proved a significant reduction in stool output. Racecadotril (anti-secretory agent) is safe, efficient and can be routinely used in acute watery diarrhea in addition to ORS (Oral Rehydration Salts).

What is Racecadotril used for?

Racecadotril is an Anti-diarrheal drug and it is used for treatment for Acute diarrhea.

What is the other name for racecadotril?

Acetorphan

What category does racecadotril belong to?

Potent Enkephalinase Inhibitor

How does a racecadotril work?

Racecadotril produces intestinal antisecretory activity where the active metabolite of racecadotril is “thiorphan” which inhibits enkephalinase enzymes in the intestinal epithelium thereby protecting the enkephalins from being broken down by these enzymes (i,e, enkephalinase enzymes). This reduces the hypersecretion in the small intestine without influencing basal secretion.

Enkephalins are endogenous opioid peptides. It is secreted by myenteric and sub mucosal neurons in the digestive tract. The enkephalins inhibit the secretion of Cl–and fluids by activating the δ opioid receptors thus reducing the loss of fluids and electrolytes during diarrhea.

Racecadotril decreases the intestinal hypersecretion, without affecting the intestinal motility. Intestinal motility is regulated through µ receptors.

What are the adverse drug reactions of racecadotril?

• Abdominal      distension

• Constipation      (after resolution of diarrhea)

• Itching      / Skin rash (less common)

• Racecadotril      does not enter the central nervous system (CNS)      therefore it does not produce any neurotoxicity. But in children below 2      years of age it can cause depression due to immature blood brain barrier.

• Headache      (common)

• Flatulence

Mention the cautions of racecadotril/ who should not take racecadotril?

• Caution - in patients with disorders of carbohydrate intolerance due to the presence      of saccharose as an excipient.

• It should only be used in children over 3 months of age

• Avoid in children with liver/ kidney problems

• Patients with chronic diarrhoea

• Patients with diarrhoea which is started during or after treatment of antibiotics.

• Caution in adults with hepatic/ renal impairment

• Manufacturer advises to avoid in pregnancy and Breast feeding

• Patients with uncontrolled vomiting- because the drug may not properly absorb and      leads to decrease in its efficacy.

Mention the contraindication of racecadotril?

Patients who are hypersensitivity to racecadotril

What is the pharmacokinetics of racecadotril?

• Administration: oral route

• Absorption: Well absorbed in the intestinal tract

• Metabolism: rapidly converted into its active metabolite called “thiorphan”

• Peak plasma levels: attained in about an hour

• Elimination Half-life: 3 hours.

What is the dose of racecadotril?

Ø ADULT: (Over 18 years)

· 100 mg initially, then 100 mg 3 times daily (preferably before food) → until diarrhoea stops.

· Maximum duration of treatment: 7 days.

Ø CHILD: (3 Months- 18 Years) [1.5 mg/kg  3 times daily]

· Body Weight less than 9 Kg: 10 mg 3 times daily until diarrhoea stops (Maximum duration of treatment: 7 days).

· Body weight 9-13 Kg: 20 mg 3 times daily until diarrhoea stops (Maximum duration of treatment: 7 days).

· Body weight 13-27 Kg: 30 mg 3 times daily until diarrhoea stops (Maximum duration of treatment: 7 days).

· Body weight over 27 Kg: 60 mg 3 times daily until diarrhoea stops (Maximum duration of treatment: 7 days).

Mention the dosage form availability of racecadotril?

• Capsule      (100 mg capsule)

• Granules      (10, 15, 30 mg sachets)

How to use Racecadotril sachets?

Empty the granules in a glass of water/milk then stir it and consume immediately.