Loperamide is a so-called peristaltic inhibitor. It is used for the symptomatic treatment of diarrhoea. It is the most widely sold active ingredient of this type and is also included on the WHO's list of essential medicines.
Loperamide does not require a prescription and is usually taken in the form of a tablet.
Loperamide has structural properties of an opioid and therefore binds to certain opioid receptors in the nerves of the intestine. This reduces the activity of the small intestinal muscles and the intestinal contents take longer to pass through. This gives more time for the intestinal contents to extract water. Loperamide, unlike conventional opioids, has no effect on the central nervous system.
Plasma protein binding is 97% and plasma half-life is 9-14 hours. Loperamide is metabolized mainly in the liver and subsequently excreted almost entirely in the stool.
When taken with quinidine, verapamil or ketoconazole, respiratory depression may occur.
Signs of overdose include dizziness, nausea, fatigue, and constipation.
Common side effects include constipation, nausea, dizziness, headache, and flatulence.
Oral, mouse: LD50 = 105 mg/kg.
| ATC Code | A07DA03 |
| Formula | C29H33ClN2O2 |
| Molar Mass (g·mol−1) | 477,04 |
| Physical State | solid |
| Melting Point (°C) | 222–223 |
| PKS Value | 8,6 |
| CAS Number | 53179-11-6 |
| PUB Number | 3955 |
| Drugbank ID | DB00836 |
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