Abstract

Metformin is a most widely used medication all around the world to treat Type 2 diabetes mellitus. It is also found to be effective against various conditions including, Prediabetes, Gestational diabetes mellitus (GDM), Polycystic Ovarian Syndrome (PCOS), Obesity, Cancer, etc. It is a cationic drug and it depends Organic Cation Transporters (OCTs) and Multidrug and Toxin Extruders (MATEs) mostly for its pharmacokinetics movement. The probability of drug interaction increases with the number of concomitant medications. This article focuses the drug interactions of metformin and most of them are linked to the inhibition of OCTs and MATEs leading to increased plasma metformin concentrations and subsequent elevation of risk of Metformin Associated Lactic Acidosis (MALA). By identifying the drugs inhibiting OCTs and MATEs, the healthcare professionals can predict the drug interactions of metformin.

Highlights

  • Metformin is a popular drug and is used by millions worldwide to treat various conditions including Type 2 diabetes mellitus, Prediabetes, Gestational diabetes mellitus (GDM), Polycystic Ovarian Syndrome (PCOS), Obesity, Cancer, etc

  • The oral absorption and hepatic uptake of Metformin are mediated possibly by Organic cation transporters (OCTs) (OCT1 and OCT3) and renal excretion of Metformin is largely mediated by Metformin transporters such as Multidrug and Toxin Extruders (MATEs) Multidrug and toxin extruder 1 (MATE1) and MATE2-k and Organic cation transporter 2 (OCT2).[9]

  • Interactions with acid suppressing agents H2 receptor blockers Cimetidine Cimetidine is a potent inhibitor of Multidrug and toxin extruder 1 (MATE1) of proximal tubular epithelial cells and it is a broad-spectrum inhibitor of transporters including Organic Cation Transporter 2 (OCT 2).[17,18]

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Summary

Drug Interactions of Metformin Involving Drug Transporter Proteins

Naina Mohamed Pakkir Maideen1*, Abdurazak Jumale[1], Rajkapoor Balasubramaniam[2 1] Dubai Health Authority, Dubai, United Arab Emirates. 2 Department of Pharmacology, Faculty of Medicine, Sebha University, Sebha, Libya. Article info Article History: Received: 2 August 2017 Revised: September 2017 Accepted: September 2017 ePublished: 31 December 2017

Introduction
Drug Interactions of Metformin
Conclusion
Dolutegravir and Metformin in Real Life?
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