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ABSTRACT
Objective
The objective of this study was to assess the influence of enzyme suppression on the values of various pharmacokinetic factors of orally administered metoclopramide.
Method
This study was conducted in two phases and a 4-week duration was adopted for drug washout. This randomized study involved 12 healthy human volunteers who received a single oral dose of metoclopramide 20 mg. After the washout period, volunteers received clarithromycin 500 mg two times per day for consecutive 5 days. On test day (fifth day), a single oral dose of metoclopramide 20 mg was also given to the volunteers, and collection of blood samples was conducted at pre-decided time points. Various pharmacokinetic parameters such as Cmax, Tmax, and AUC0-∞ of metoclopramide were determined by analyzing the blood samples using a validated HPLC-UV method.
Results
Clarithromycin increased the mean values of Cmax, AUC0-∞, and T1/2 of metoclopramide by 46%, 78.6%, and 9.8%, respectively.
Conclusion
Clarithromycin noticeably increased the concentration of plasma metoclopramide. This study’s results provide in vivo confirmation of the CYP3A4 involvement in metoclopramide metabolism, in addition to CYP2D6. Therefore, metoclopramide pharmacokinetics may be clinically affected by clarithromycin and other potent enzyme inhibitors.
Declaration of interest
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Reviewer disclosures
Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.
Author contributions
I Kaukab, SNH Shah, ZJ Kharaba, MA Buabeid, and G Murtaza design this study. I Kaukab and G Murtaza performed the experiments. SNH Shah supervised this work. YA Alfoteih improved the English language quality.