loperamide + red grapefruit juice

Loperamide + red grapefruit juice refers to a specific drug-food interaction combination evaluated in a Phase 1 clinical trial by Johnson & Johnson Consumer and Personal Products Worldwide. Loperamide is a synthetic oral antidiarrheal and a small molecule mu-opioid receptor agonist that works by slowing intestinal motility. Red grapefruit juice contains compounds that inhibit the intestinal enzyme Cytochrome P450 3A4 (CYP3A4), which is a primary metabolic pathway for loperamide. The interaction study demonstrated that co-administration of red grapefruit juice increases the systemic exposure (AUC) of loperamide by approximately 1.7-fold. Loperamide is also a substrate for the P-glycoprotein efflux transporter, and the study aimed to characterize the pharmacokinetic impact of these interactions in healthy volunteers.

Brand names

Imodium

Other names

loperamide hydrochlorideloperamide HCl