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Cited by 348Pharmacogenetics and Drug MetabolismDiabetes Treatment and ManagementMetabolism, Diabetes, and Cancer

Pharmacokinetics of Metformin After Intravenous and Oral Administration to Man

Pentik�inen, P. J., Neuvonen, P. J., Penttil�, Aneri·1979·European Journal of Clinical Pharmacology
DOI 10.1007/bf00562061
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Abstract

The kinetics of 14C-metformin have been studied in five healthy subjects after oral and intravenous administration. The intravenous dose was distributed to a small central compartment of 9.9 +/- 1.61 (X +/- SE), from which its elimination could be described using three-compartment open model. The elimination half-life from plasma was 1.7 +/- 0.1 h. Urinary excretion data revealed a quantitatively minor terminal elimination phase with a half-life of 8.9 +/- 0.7 h. After the intravenous dose, metformin was completely excreted unchanged in urine with a renal clearance of 454 +/- 47 ml/min. Metformin was not bound to plasma proteins. The concentration of metformin in saliva was considerably lower than in plasma and declined more slowly. The bioavailability of metformin tablets averaged 50--60%. The rate of absorption was slower than that of elimination, which resulted in a plasma concentration profile of "flip-flop" type for oral metformin.

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Crossref · 10.1007/bf00562061

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  • When prescribed in the usual oral dosage range of 250 to ~2550 mg/day for T2DM and in the absence of reduced renal function, peak plasma levels of metformin are unlikely to exceed 15-20 μM, with trough levels between 1-5 μM, and a plasma half-life of approximately 3 to 5 hours.

    “When prescribed in the usual oral dosage range of 250 to ~2550 mg/day for the treatment of T2DM and in the absence of reduced renal function, it is unlikely that peak plasma levels of metformin would exceed 15-20 μM, with trough levels of between 1-5 μM, and a plasma half-life of approximately 3 to 5 hours.”

    From A Critical Review of the Evidence That Metformin Is a Putative Anti-Aging Drug That Enhances Healthspan and Extends Lifespan (2021) · cites this paper as [154]

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Authors
Pentik�inen, P. J., Neuvonen, P. J., & Penttil�, A.
Affiliations
University of Helsinki (FI)
ORCID
Neuvonen, P. J.
Venue
European Journal of Clinical Pharmacology
Publisher
Springer Science and Business Media LLC
Published
1979
Volume
16
Issue
3
Pages
195-202
ISSN
  • 0031-6970 (ISSN-L)
  • 1432-1041
DOI
10.1007/bf00562061
OpenAlex
W2091831319
Cited by
348
References
28
Citations by year
2026: 7 · 2025: 9 · 2024: 13 · 2023: 16 · 2022: 16 · 2021: 16 · 2020: 13 · 2019: 18 · 2018: 17 · 2017: 13 · 2016: 12 · 2015: 24 · 2014: 22 · 2013: 8 · 2012: 13
FWCI
1.07
Type
journal article
Language
en
Open access
closed
Licence
www.springer.com/tdm (tdm)
Locations
  • European Journal of Clinical Pharmacology (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Keywords
metformin, pharmacokinetics, oral bioavailability, intravenous administration, urinary excretion, renal clearance, plasma protein binding, flip-flop kinetics, drug absorption, elimination half-life, three-compartment model
MeSH terms
Administration, Oral, Adult, Breath Tests, Feces, Female, Humans, Injections, Intravenous, Kinetics, Male, Metformin, Middle Aged, Protein Binding, Saliva

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