.Pharmacolibrary.Drugs.A_AlimentaryTractAndMetabolism.A07D_Antipropulsives.A07DA03_Loperamide.Loperamide

Information

Loperamide is a synthetic piperidine derivative and an opioid-receptor agonist that acts on the μ-opioid receptors in the large intestine. It is primarily used as an antidiarrheal agent to reduce the frequency of diarrhea. It is approved and widely used over-the-counter for the treatment of both acute and chronic diarrhea.

Pharmacokinetics

Pharmacokinetic parameters in healthy adult volunteers after a single oral dose.

References

1. Cha, YJ, et al., & Cho, JY (2013). Sustained Increase in the Oral Bioavailability of Loperamide after a Single Oral Dose of HM30181, a P-glycoprotein Inhibitor, in Healthy Male Participants. Basic & clinical pharmacology & toxicology 113(6) 419–424. DOI:10.1111/bcpt.12108 PUBMED:https://pubmed.ncbi.nlm.nih.gov/23829508

2. Krishna, G, et al., & McLeod, J (2009). Pharmacokinetics and absorption of posaconazole oral suspension under various gastric conditions in healthy volunteers. Antimicrobial agents and chemotherapy 53(3) 958–966. DOI:10.1128/AAC.01034-08 PUBMED:https://pubmed.ncbi.nlm.nih.gov/19075045

3. Kobayashi, M, et al., & Aungst, BJ (2005). Relationship between loperamide-induced sedative effect and digoxin pharmacokinetics in healthy Japanese subjects. Pharmaceutical research 22(3) 413–418. DOI:10.1007/s11095-004-1879-6 PUBMED:https://pubmed.ncbi.nlm.nih.gov/15835747

Revisions

• 06/2025 initial generated model