Loperamide
Regulatory sources consulted
- AEMPS-CIMA-FT-86472
- CredibleMeds.org
- General Clinical Pharmacology Knowledge
- AEMPS CIMA · nº registro 86472 ↗
- RxNorm rxcui 6468 ↗
Approved indications
- Symptomatic treatment of acute non-specific diarrhea in adults and children from 12 years of age.
Contraindications
Absolute
- Hypersensitivity to the active substance. Children under 2 years of age. Acute dysentery (blood in stools and high fever). Acute ulcerative colitis. Pseudomembranous colitis associated with antibiotics. Bacterial enterocolitis.
- When inhibition of peristalsis is to be avoided.
Clinical warnings
- Boxed warning · Cases of serious cardiac events, including QT interval prolongation, Torsades de Pointes, cardiac arrest, and death, have been reported with the use of higher than recommended doses. Do not exceed the maximum daily dose. — FDA
Drug interactions
- HighItraconazoleJ02AC02
Mechanism: Potent inhibitor of CYP3A4 and P-glycoprotein (P-gp), increasing loperamide plasma concentrations 3- to 4-fold and the risk of cardiac and CNS adverse effects.
Recommendation: Avoid concomitant use. If unavoidable, monitor the patient closely for signs of cardiac and CNS adverse effects.
AEMPS CIMA label
- HighQuinidineC01BA01
Mechanism: Potent P-glycoprotein (P-gp) inhibitor. Increases loperamide concentrations and may cause respiratory depression by increasing its CNS penetration.
Recommendation: Concomitant use is contraindicated by some manufacturers due to the risk of respiratory depression.
AEMPS CIMA label
Adverse events
Common (≥1%)
constipation · nausea · flatulence · headache · dizziness
Rare but serious
paralytic ileus · toxic megacolon · QT prolongation · Torsades de Pointes · anaphylactic reactions · acute pancreatitis
Pregnancy and lactation
Pregnancy: Not recommended, especially in the first trimester. Lactation: Small amounts are excreted in breast milk; use is not recommended.