Loperamide

pharmacological · nervous · digestive · Oral

Loperamide. Peripheral µ-opioid agonist — slows gut motility via enteric neurons; P-glycoprotein efflux at the BBB keeps CNS exposure minimal at therapeutic doses.…

Peripheral µ-opioid agonist — slows gut motility via enteric neurons; P-glycoprotein efflux at the BBB keeps CNS exposure minimal at therapeutic doses. Abused at megadoses for euphoria — cardiotoxicity (QT, torsades) emerged as the predominant overdose harm.

Sources: PMID:10087042, PMID:15496339, PMID:438356