Racecadotril

Products

Racecadotril was registered in many countries in 2015 in capsule form (Vaprino). It is currently approved for export only.

Structure and properties

Racecadotril (C21H23NO4S, Mr = 385.5 g/mol) is a prodrug that is biotransformed (hydrolyzed) in the organism to the active metabolite thiorphan. It exists as a white powder that is practically insoluble in water.

Effects

Racecadotril (ATC A07XA04) has antidiarrheal and antisecretory properties in the intestine. The effects are due to inhibition of the enzyme enkephalinase, a peptidase localized in the small intestinal epithelium. Racecadotril protects enkephalins – endogenous opioids – from enzymatic degradation. This reduces hypersecretion. Racecadotril, on the other hand, has no effect on basal secretion. It is not active in the CNS and does not prolong intestinal transit time.

Indications

For symptomatic treatment of acute diarrhea.

Dosage

According to the SmPC. Capsules are usually taken three times daily before main meals.

Contraindications

  • Hypersensitivity
  • Diarrhea with fever and/or bloody or mucous stools (invasive bacteria)
  • Pseudomembranous colitis associated with antibiotics.

For complete precautions, see the drug label.

Interactions

There are no known drug-drug interactions.

Adverse effects

The most common possible adverse effects include headache. Occasionally, skin rashes are observed.