Drug intelligence / Profile preview

loperamide + pink grapefruit juice (Johnson & Johnson)

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

This refers to a specific Phase 1 clinical pharmacokinetic drug-interaction study (NCT00806299) conducted by Johnson & Johnson Consumer and Personal Products Worldwide. The study evaluated the effect of pink grapefruit juice on the pharmacokinetics of loperamide (brand name Imodium), a small molecule mu-opioid receptor agonist used to treat diarrhea. Loperamide is primarily metabolized by the intestinal enzyme CYP3A4 during its first-pass metabolism. Pink grapefruit juice contains furanocoumarins that inhibit CYP3A4, and the trial demonstrated that co-administration leads to an approximately 1.7-fold increase in loperamide exposure. The study was an open-label, randomized, single-dose, fixed-sequence crossover trial in healthy volunteers.

Brand names
Imodium
Other names
Loperamide HCl + pink grapefruit juiceLoperamide + pink grapefruit juice-Johnson & Johnson Consumer and Personal Products Worldwide-Diarrhea
02

Targets

ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)MOR (Mu opioid receptor)

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