Effects of oral contraceptive steroids on acetaminophen metabolism and elimination

Mack C. Mitchell, Teruki Hanew, Christopher G. Meredith, Steven Schenker

Research output: Contribution to journalArticle

56 Citations (Scopus)

Abstract

Plasma acetaminophen elimination was examined in women taking low-dose estrogen oral contraceptive (OC) steroids and in age-matched control women. Fractional rates of elimination and fractional clearances were calculated for each of the metabolic pathways, including oxidation, sulfation, and glucuronidation. The cysteine adduct and mercapturic acid derivative of acetaminophen were used as an index of oxidative biotransformation, a potentially toxic route of metabolism for acetaminophen. Plasma acetaminophen clearance rose from 287 ± 13 ml/min to 470 ± 51 mllmin in women taking OC steroids, whereas elimination t 1 2 decreased from 2.40 ± 0.14 hr to 1.67 ± 0.16 hr. The fractional clearance and rate of elimination of acetaminophen by glucuronidation increased in women taking OC steroids, whereas the clearance and elimination by sulfation did not differ significantly from values in control subjects. Fractional clearance of the cysteine adduct also increased significantly, but clearance of acetaminophen mercapturic acid did not change. These data suggest that the increased clearance of acetaminophen from plasma in women taking OC steroids results from increased glucuronidation of the drug, although the mechanism is not known.

Original languageEnglish (US)
Pages (from-to)48-53
Number of pages6
JournalClinical Pharmacology and Therapeutics
Volume34
Issue number1
StatePublished - Jul 1983

Fingerprint

Acetaminophen
Oral Contraceptives
Steroids
Cysteine
Poisons
Biotransformation
Metabolic Networks and Pathways
Estrogens
Pharmaceutical Preparations
acetaminophen-mercapturic acid conjugate

ASJC Scopus subject areas

  • Pharmacology

Cite this

Effects of oral contraceptive steroids on acetaminophen metabolism and elimination. / Mitchell, Mack C.; Hanew, Teruki; Meredith, Christopher G.; Schenker, Steven.

In: Clinical Pharmacology and Therapeutics, Vol. 34, No. 1, 07.1983, p. 48-53.

Research output: Contribution to journalArticle

Mitchell, Mack C. ; Hanew, Teruki ; Meredith, Christopher G. ; Schenker, Steven. / Effects of oral contraceptive steroids on acetaminophen metabolism and elimination. In: Clinical Pharmacology and Therapeutics. 1983 ; Vol. 34, No. 1. pp. 48-53.
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