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Is Metformin a Perfect Drug? Updates in Pharmacokinetics and Pharmacodynamics

[ Vol. 23 , Issue. 17 ]

Author(s):

Magdalena Markowicz-Piasecka*, Kristiina M. Huttunen, Lukasz Mateusiak, Elzbieta Mikiciuk-Olasik and Joanna Sikora   Pages 2532 - 2550 ( 19 )

Abstract:


Metformin, a synthetic biguanide, is currently one of the most frequently recommended medications for type 2 diabetes treatment around the world. This review presents the latest discoveries in the pharmacokinetics of metformin, especially the role of transporters (e.g. Organic Cation Transporters OCTs, Multidrug and Toxin Extrusion transporters MATE) in oral absorption, distribution, elimination and biochemical effects of metformin in humans. We also review the associations between genetic variations of metformin transporters, their pharmacokinetics and drug efficacy or drug responses.

In the second part of this paper, we highlight the current knowledge on novel metformin actions including favourable effects on lipid profile (e.g. decreasing plasma triglycerides (TG) and low density lipoprotein (LDL) cholesterol levels) and the cardiovascular system (e.g. decline in systolic and diastolic blood pressure, and vasoprotective effects). Furthermore, we provide an up-to-date overview of multidirectional activities of metformin, including the effects on coagulation and fibrinolysis, polycystic ovary syndrome, as well as the anti-ageing and antiinflammatory properties. Over the past two decades, metformin’s antineoplastic properties have been drawing increasing attention of scientists; herein, we outline the state-of-the-art discoveries concerning metformin use in the field of oncology. Finally, we review the newly synthesized derivatives and pro-drugs of metformin and other biguanides.

Keywords:

Biguanides, metformin, pharmacokinetics, glycaemia, coagulation, pro-drugs.

Affiliation:

Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyńskiego 1, 90-151 Lodz, School Of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Yliopistonranta 1C, POB 1627, 70211 Kuopio, Students Research Group, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyńskiego 1, 90-151 Lodz, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyńskiego 1, 90-151 Lodz, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul Muszyńskiego 1, 90-151 Lodz



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