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Pharmacokinetics of triethylamine and triethylamine-N-oxide in man

Åkesson, Bengt, Vinge, Ellen, Skerfving, Staffan·1989·Toxicology and Applied Pharmacology
DOI 10.1016/0041-008x(89)90300-1
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Abstract

The pharmacokinetics of the industrially important compound triethylamine (TEA) and its metabolite triethylamine-N-oxide (TEAO) were studied in four volunteers after oral and intravenous administration. TEA was efficiently absorbed from the gastrointestinal (GI) tract, rapidly distributed, and in part metabolized into TEAO. There was no significant first pass metabolism. TEAO was also well absorbed from the GI tract. Within the GI tract, TEAO was reduced into TEA (19%) and dealkylated into diethylamine (DEA; 10%). The apparent volumes of distribution during the elimination phase were 192 liters for TEA and 103 liters for TEAO. Gastric intubation showed that there was a close association between levels of TEA in plasma and gastric juice, the latter levels being 30 times higher. The TEA and TEAO in plasma had half-lives of about 3 and 4 hr, respectively. Exhalation of TEA was minimal. More than 90% of the dose was recovered in the urine as TEA and TEAO. The urinary clearances of TEA and TEAO indicated that in addition to glomerular filtration, tubular secretion takes place. For TEAO at high levels, the secretion appears to be saturable. The present data, in combination with those of earlier studies, indicate that the sum of TEA and TEAO in urine may be used for biological monitoring of exposure to TEA.

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Crossref · 10.1016/0041-008x(89)90300-1

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16 of 16 references verified0 citation errors · 0 not checkable

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  • The high renal clearance rate of TMAO indicates that in addition to glomerular filtration, at least 50% of its renal excretion possibly occurs through tubular secretion.

    “The high renal clearance rate of TMAO indicates that in addition to glomerular filtration, at least 50% of its renal excretion possibly occurs through tubular secretion.”

    From Trimethylamine N-oxide: the good, the bad and the unknown. (2016) · cites this paper as [25]

  • In normal subjects, urinary clearance of TMAO was 219 ± 78 mL/min compared to urinary urea and creatinine clearances 55 ± 14 and 119 ± 21 mL/min, respectively.

    “In normal subjects, the urinary clearance of TMAO was 219 ± 78 mL/min compared to the urinary urea and creatinine clearances 55 ± 14 and 119 ± 21 mL/min, respectively.”

    From Trimethylamine N-oxide: the good, the bad and the unknown. (2016) · cites this paper as [25]

  • TMAO has a small volume of distribution-about one half that of urea-but a higher renal clearance compared to urea and creatinine.

    “Studies on pharmacokinetics [25] and renal clearance of TMAO [26] in healthy human subjects suggest that TMAO has a small volume of distribution—about one half that of urea—but a higher renal clearance compared to urea and creatinine.”

    From Trimethylamine N-oxide: the good, the bad and the unknown. (2016) · cites this paper as [25]

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Authors
Åkesson, B., Vinge, E., & Skerfving, S.
Affiliations
  • Lund University (SE)
  • Skåne University Hospital (SE)
Corresponding author
Åkesson, Bengt
Venue
Toxicology and Applied Pharmacology
Publisher
Elsevier BV
Published
1989-09
Volume
100
Issue
3
Pages
529-538
ISSN
0041-008X (ISSN-L)
DOI
10.1016/0041-008x(89)90300-1
OpenAlex
W2112477369
Cited by
37
References
16
Citations by year
2026: 2 · 2025: 4 · 2024: 1 · 2023: 2 · 2020: 1 · 2019: 1 · 2016: 1 · 2015: 3 · 2012: 4
FWCI
1.54
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Toxicology and Applied Pharmacology (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
  • Life Sciences › Agricultural and Biological Sciences › Plant Science › Pesticide Exposure and Toxicity
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Carcinogens and Genotoxicity Assessment
Keywords
triethylamine, pharmacokinetics, first-pass metabolism, gastrointestinal absorption, volume of distribution, half-life, urinary excretion, renal tubular secretion, diethylamine, gastric juice, biomonitoring, occupational exposure
MeSH terms
Administration, Oral, Biotransformation, Ethylamines, Humans, Infusions, Intravenous, Intestinal Absorption, Male, Middle Aged

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