Proton Pump Inhibitors Inhibit Metformin Uptake by Organic Cation Transporters (OCTs)
2011
Proton Pump Inhibitors and Metformin Interaction
publication
Evidence: moderate
Author Information
Author(s): Nies Anne T., Hofmann Ute, Resch Claudia, Schaeffeler Elke, Rius Maria, Schwab Matthias
Primary Institution: Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Hypothesis
Proton pump inhibitors (PPIs) inhibit the uptake of metformin by organic cation transporters (OCTs).
Conclusion
PPIs are potent inhibitors of OCT-mediated metformin transport in vitro.
Supporting Evidence
- PPIs significantly inhibited metformin uptake by OCT1, OCT2, and OCT3 in a concentration-dependent manner.
- IC50 values for PPIs ranged from 3 to 36 µM.
- None of the tested PPIs were identified as substrates for OCTs.
Takeaway
This study found that certain stomach medications can stop a diabetes drug from working properly in the body.
Methodology
The study used in silico modeling and in vitro experiments with stably transfected cell lines expressing human OCTs.
Limitations
The clinical relevance of the findings needs further investigation.
Digital Object Identifier (DOI)
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