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Cited by 391Diabetes Treatment and ManagementDiabetes Management and ResearchMetabolism, Diabetes, and Cancer

Metformin: A Review of its Pharmacological Properties and Therapeutic Use in Non-Insulin-Dependent Diabetes Mellitus

Dunn, Christopher J., Peters, David H.·1995·Drugs
DOI 10.2165/00003495-199549050-00007
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Abstract

The biguanide metformin (dimethylbiguanide) is an oral antihyperglycaemic agent used in the management of non-insulin-dependent diabetes mellitus (NIDDM). It reduces blood glucose levels, predominantly by improving hepatic and peripheral tissue sensitivity to insulin without affecting the secretion of this hormone. Metformin also appears to have potentially beneficial effects on serum lipid levels and fibrinolytic activity, although the long term clinical implications of these effects are unclear. Metformin possesses similar antihyperglycaemic efficacy to sulphonylureas in obese and nonobese patients with NIDDM. Additionally, interim data from the large multicentre United Kingdom Prospective Diabetes Study (UKPDS) indicated similar antihyperglycaemic efficacy for metformin and insulin in newly diagnosed patients with NIDDM. Unlike the sulphonylureas and insulin, however, metformin treatment is not associated with increased bodyweight. Addition of metformin to existing antidiabetic therapy confers enhanced antihyperglycaemic efficacy. This may be of particular use in improving glycaemic control in patients with NIDDM not adequately controlled with sulphonylurea monotherapy, and may serve to reduce or eliminate the need for daily insulin injections in patients with NIDDM who require this therapy. The acute, reversible gastrointestinal adverse effects seen with metformin may be minimised by administration with or after food, and by using lower dosages, increased slowly where necessary. Lactic acidosis due to metformin is rare, and the risk of this complication may be minimised by observance of prescribing precautions and contraindications intended to avoid accumulation of the drug or lactate in the body. Unlike the sulphonylureas, metformin does not cause hypoglycaemia. Thus, metformin is an effective antihyperglycaemic agent which appears to improve aberrant plasma lipid and fibrinolytic profiles associated with NIDDM. Possible long term clinical benefits of this drug with regard to cardiovascular mortality and morbidity are not yet established but are being assessed in a major ongoing study. Since metformin does not promote weight gain or hypoglycaemia it should be considered first-line pharmacotherapy in obese patients with NIDDM inadequately controlled by nonpharmacological measures. Metformin appears similarly effective for the pharmacological management of NIDDM in nonobese patients.

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Crossref · 10.2165/00003495-199549050-00007

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  • Thiazolidinediones have concerning side effects including edema, congestive heart failure, and in the case of rosiglitazone, myocardial infarction, which led to a black box warning from the FDA.

    “However, they have concerning side effects including edema, congestive heart failure (CHF), and in the case of rosiglitazone, myocardial infarction (MI) [69], which led to a black box warning from the Food and Drug Administration (FDA) [70].”

    From Metformin in Amnestic Mild Cognitive Impairment: Results of a Pilot Randomized Placebo Controlled Clinical Trial (2016) · cites this paper as [70]

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Authors
Dunn, C. J., & Peters, D. H.
ORCID
Venue
Drugs
Publisher
Springer Science and Business Media LLC
Published
1995-05
Volume
49
Issue
5
Pages
721-749
ISSN
0012-6667 (ISSN-L)
DOI
10.2165/00003495-199549050-00007
OpenAlex
W2071723829
Cited by
391
References
123
Citations by year
2026: 8 · 2025: 5 · 2024: 7 · 2023: 9 · 2022: 12 · 2021: 8 · 2020: 14 · 2019: 7 · 2018: 11 · 2017: 7 · 2016: 18 · 2015: 9 · 2014: 13 · 2013: 10 · 2012: 24
FWCI
9.48
Type
journal article
Language
en
Open access
closed
Locations
  • Drugs (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Keywords
metformin, biguanides, type 2 diabetes, insulin sensitivity, insulin resistance, sulfonylureas, insulin, lactic acidosis, gastrointestinal adverse effects, hypoglycemia, serum lipids, fibrinolysis, UKPDS, obesity, first-line pharmacotherapy, glycemic control
MeSH terms
Clinical Trials as Topic, Diabetes Mellitus, Type 2, Humans, Hypoglycemic Agents, Metformin

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