Pulmonary first-pass and steady-state metabolism of phenols

Pharm Res. 1996 May;13(5):744-8. doi: 10.1023/a:1016003717666.

Abstract

Purpose: To study (A) the effect of the administration route (i.v. and i.t.) on pre- and post-absorptive metabolism of phenol and 1-naphthol by the lung and (B) pulmonary extraction of phenol at steady-state.

Methods: Phenols were administered intra-arterially, intravenously and intratracheally and the pre- and post-absorptive metabolism assessed by comparing the AUCs in arterial blood. Phenol was infused to steady-state and the pulmonary extraction assessed by measuring jugular vein and carotid artery blood concentrations.

Results: In contrast to previously published data (e.g., Mistry and Houston, Drug Metab.Dispos.l3:740-745 (1985)) we could not detect pulmonary first-pass metabolism of the phenols; reasons for this disparity are discussed. An apparent negative pulmonary extraction of phenol at steady-state was observed, probably as a consequence of extraction by organs which are in series, and not parallel, with the lungs (e.g. liver, kidneys and GIT).

Conclusions: (A) Phenol and 1-naphthol do not undergo pulmonary first-pass metabolism. (B) Traditional methods of assessing organ extraction and clearance at steady-state cannot be utilised when metabolising organs are in series.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Infusions, Intra-Arterial
  • Infusions, Intravenous
  • Lung / metabolism*
  • Male
  • Naphthols / administration & dosage
  • Naphthols / blood
  • Naphthols / pharmacokinetics*
  • Phenol
  • Phenols / administration & dosage
  • Phenols / blood
  • Phenols / pharmacokinetics*
  • Rats
  • Rats, Wistar
  • Spectrometry, Fluorescence
  • Trachea

Substances

  • Naphthols
  • Phenols
  • 1-naphthol
  • Phenol