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• W2113005281 abstract "This study examined in vitro interaction between domperidone and erythromycin. Both are prescribed for refractory gastroparesis. Domperidone is metabolized via human cytochrome P4503A4. Erythromycin is a CYP3A4 inhibitor.Incubations evaluated domperidone metabolite formation in human liver microsomes and recombinant CYP3A4. Concentration- and time-dependent inhibition of 500 μM domperidone was studied with 2.5–200 μM erythromycin over 10–40 min.Domperidone metabolite (5-hydroxy domperidone, M3) formation was inhibited by erythromycin in a concentration- and time-dependent manner. The KI estimate was 18.4 μM in human liver microsomes and 4.1 μM in CYP3A4. Using a model incorporating CYP3A4 hepatic and gut inhibition, in vitro estimates from human liver microsomes and CYP3A4 were used to predict in vivo AUCi/AUC ratios of 2.54 and 4.95, respectively.Significant inhibition of domperidone metabolism by erythromycin occurs. This predicts greater domperidone drug exposure when used with erythromycin. This important drug–drug interaction will be evaluated in future human studies." @default.
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• W2113005281 date "2009-07-03" @default.
• W2113005281 modified "2023-09-24" @default.
• W2113005281 title "Metabolic interactions between prokinetic agents domperidone and erythromycin: an<i>in vitro</i>analysis" @default.
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• W2113005281 doi "https://doi.org/10.1080/00498250903096121" @default.
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