Racecadotril is a peripherally-acting enkephalinase inhibitor used as an antisecretory agent for the symptomatic treatment of acute diarrhea in adults and children. It acts locally in the intestine without affecting intestinal motility, making it distinct from opioids like loperamide. It is a prodrug that is rapidly hydrolyzed to its active metabolite, thiorphan.
Adult: 100 mg three times daily. Take before main meals (breakfast, lunch, dinner). Continue until diarrhea stops, but not for more than 7 days.
Note: Oral administration. Swallow the tablet whole with a glass of water. Can be taken with or without food, but taking before meals may be preferable. Must be used in conjunction with Oral Rehydration Solution (ORS) to prevent and correct dehydration. Do not crush or chew unless specified (some dispersible forms exist).
Racecadotril is a prodrug of thiorphan, a potent and selective inhibitor of membrane-bound enkephalinase (neprilysin). This enzyme degrades endogenous enkephalins in the gastrointestinal tract. By inhibiting enkephalinase, racecadotril increases the local concentration of enkephalins. Enkephalins then activate delta-opioid receptors on enterocytes, which inhibits adenylate cyclase. This reduces the production of cyclic AMP (cAMP), leading to a decrease in the secretion of water and electrolytes into the intestinal lumen. It normalizes intestinal hypersecretion without affecting gastrointestinal motility or transit time.
Pregnancy: Category B3 (as per some regulatory bodies). Animal studies have shown some fetotoxicity at high doses. No adequate and well-controlled studies in pregnant women. Use only if clearly needed and potential benefit justifies potential risk to the fetus.
Driving: May cause dizziness. Patients should be cautioned about driving or operating machinery if they experience this effect.
| Loperamide, Diphenoxylate/Atropine | Theoretical risk of severe constipation or ileus. No therapeutic synergy. Concurrent use is contraindicated. | Major |
| ACE Inhibitors (e.g., Enalapril, Ramipril) | Both inhibit enzymes in the renin-angiotensin system (neprilysin is involved in bradykinin metabolism). Concurrent use may theoretically increase risk of angioedema, though clinical evidence is limited. Monitor closely. | Moderate |
| Sacubitril/Valsartan | Sacubitril is a neprilysin inhibitor. Concurrent use with racecadotril (also a neprilysin inhibitor) is contraindicated due to significantly increased risk of angioedema. | Major |
| Alcohol | May worsen dehydration and dizziness. Not a direct pharmacokinetic interaction. | Minor |
Same composition (Racecadotril (100mg)), different brands: