Metformin is not just an antihyperglycaemic drug but also has protective effects on the vascular endothelium

Research output: Contribution to journalReview article

27 Citations (Scopus)

Abstract

Metformin, a synthetic dimethyl biguanide, has been in clinical use for over 55 years, and today is considered the first-choice drug for the treatment of type 2 diabetes used by an estimated 125 million people worldwide. Metformin is orally effective, not metabolized, excreted unchanged by the kidney, relatively free of side effects and well tolerated by the majority of patients. Of importance is that the United Kingdom Prospective Diabetes Study 20-year study of type 2 diabetics, completed in 1998, compared patients treated with insulin, sulfonylureas and metformin and concluded that metformin provided vascular protective actions. Cardiovascular disease is the primary basis for the high morbidity and mortality that is associated with diabetes and that metformin proved to be protective resulted in a dramatic increase in its use. The vascular protective actions of metformin are thought to be secondary to the antihyperglycaemic effects of metformin that are mediated via activation of AMP kinase and subsequent inhibition of hepatic gluconeogenesis, fatty acid oxidation as well as an insulin sensitizing action in striated muscle and adipose tissue. As reflected by a number of clinical studies, patients treated with metformin also have improvement in endothelial function as measured by the use of plethysmography and measurement of flow-mediated vasodilatation. These data as well as data from animal studies are supportive that metformin has a direct protective action on the vascular endothelium. In this review article, we discuss the pharmacology of metformin and critique the literature as to its cellular sites and mechanism(s) of action.

Original languageEnglish
Pages (from-to)138-151
Number of pages14
JournalActa Physiologica
Volume219
Issue number1
DOIs
Publication statusPublished - 1 Jan 2017

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Metformin
Vascular Endothelium
Hypoglycemic Agents
Pharmaceutical Preparations
Blood Vessels
Insulin
Biguanides
Adenylate Kinase
Plethysmography
Striated Muscle
Gluconeogenesis
Vasodilation
Type 2 Diabetes Mellitus
Adipose Tissue
Cardiovascular Diseases
Fatty Acids
Prospective Studies
Pharmacology
Morbidity
Kidney

Keywords

  • AMPK
  • cancer
  • diabetes
  • EDV
  • metformin
  • SIRT1

ASJC Scopus subject areas

  • Physiology

Cite this

Metformin is not just an antihyperglycaemic drug but also has protective effects on the vascular endothelium. / Triggle, Christopher; Ding, Hong.

In: Acta Physiologica, Vol. 219, No. 1, 01.01.2017, p. 138-151.

Research output: Contribution to journalReview article

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