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 a preferred alternative to motility inhibitors like loperamide. It is a prodrug that is rapidly hydrolyzed to its active metabolite, thiorphan.
Adult: 30mg (one capsule) three times daily, before main meals. Continue for a maximum of 7 days or until the first normal stool.
Note: Capsule should be swallowed whole with a glass of water, preferably before meals. For pediatric sachets, mix the granules with a small amount of water, milk, or soft food (like yogurt) and administer immediately. Oral Rehydration Solution (ORS) must be used concurrently to prevent and treat dehydration.
Racecadotril is a prodrug hydrolyzed to thiorphan, which is a potent and selective inhibitor of membrane-bound enkephalinase (neprilysin) located on the brush border of enterocytes. Inhibition of this enzyme prevents the degradation of endogenous enkephalins (like met-enkephalin). Enkephalins then bind to delta-opioid receptors on enterocytes, activating a pertussis toxin-sensitive G-protein. This leads to a reduction in intracellular cyclic AMP and calcium levels, ultimately inhibiting the hypersecretion of water and electrolytes into the intestinal lumen without affecting normal peristalsis.
Pregnancy: Category B3 (as per some references). Animal studies are insufficient. Use only if clearly needed and potential benefit justifies potential risk to the fetus. Preferably avoid in first trimester.
Driving: May cause dizziness or drowsiness in some individuals. Patients should not drive or operate machinery if they experience these effects.
| ACE Inhibitors (e.g., Ramipril, Enalapril) | Theoretical potential for additive inhibition of enkephalinase/bradykinin degradation, potentially increasing risk of angioedema. Clinical significance is uncertain. | Moderate |
| Antihypertensives | Potential additive hypotensive effect (rare). | Low |
| CNS Depressants (Alcohol, Benzodiazepines, Opioids) | May potentiate drowsiness or dizziness. | Low |
| Diuretics | Increased risk of electrolyte imbalance (hyponatremia, hypokalemia) in the context of diarrhea. | Moderate |
Same composition (Racecadotril (30mg)), different brands: