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Metformin: An Update
Abstract
Metformin is an insulin-sensitizing agent with potent antihyperglycemic properties. Its efficacy in reducing hyperglycemia in type 2 diabetes mellitus is similar to that of sulfonylureas, thiazolidinediones, and insulin. Metformin-based combination therapy is often superior to therapy with a single hypoglycemic agent. The antihyperglycemic properties of metformin are mainly attributed to suppressed hepatic glucose production, especially hepatic gluconeogenesis, and increased peripheral tissue insulin sensitivity. Although the precise mechanism of hypoglycemic action of metformin remains unclear, it probably interrupts mitochondrial oxidative processes in the liver and corrects abnormalities of intracellular calcium metabolism in insulin-sensitive tissues (liver, skeletal muscle, and adipocytes) and cardiovascular tissue.
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“The principal function of metformin is to reduce hepatic glucose production and to improve peripheral insulin sensitivity, thus ameliorating hyperglycemia (20).”
From Hypoglycemic effects of brassinosteroid in diet-induced obese mice (2012) · cites this paper as [20]
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Metadata
- Authors
- Kirpichnikov, D., McFarlane, S. I., & Sowers, J. R.
- Affiliations
- State University of New York (US)
- Venue
- Annals of Internal Medicine
- Publisher
- American College of Physicians
- Published
- 2002-07-02
- Volume
- 137
- Issue
- 1
- Pages
- 25-33
- ISSN
- 0003-4819 (ISSN-L)
- 1539-3704
- OpenAlex
- W2046503553
- Cited by
- 1,084
- References
- 98
- Citations by year
- 2026: 8 · 2025: 15 · 2024: 31 · 2023: 31 · 2022: 41 · 2021: 33 · 2020: 41 · 2019: 39 · 2018: 63 · 2017: 55 · 2016: 50 · 2015: 68 · 2014: 77 · 2013: 62 · 2012: 54
- FWCI
- 5.11
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Annals of Internal Medicine (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Heart, Lung, and Blood Institute (R01-HL63904-01)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
- Keywords
- metformin, type 2 diabetes, insulin sensitization, antidiabetic drugs, combination therapy, hepatic gluconeogenesis, hepatic glucose production, mitochondrial oxidative phosphorylation, hypoglycemic mechanism
- MeSH terms
- Animals, Cardiovascular Diseases, Diabetes Mellitus, Type 2, Drug Therapy, Combination, Female, Humans, Hyperglycemia, Hypoglycemic Agents, Metformin, Polycystic Ovary Syndrome, Vascular Resistance
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