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Galinsky RE, Chałasinska B. Effect of taurolithocholate on in vivo sulfation and glucuronidation of acetaminophen in rats. Pharm Res. 1988;5(1):61-4doi: 10.1023/a:1015871713954.
Galinsky, R. E., & Chałasinska, B. (1988). Effect of taurolithocholate on in vivo sulfation and glucuronidation of acetaminophen in rats. Pharmaceutical research, 5(1), 61-4. https://doi.org/10.1023/a:1015871713954
Galinsky, R E, and Chałasinska, B. "Effect of taurolithocholate on in vivo sulfation and glucuronidation of acetaminophen in rats." Pharmaceutical research vol. 5,1 (1988): 61-4. doi: https://doi.org/10.1023/a:1015871713954
Galinsky RE, Chałasinska B. Effect of taurolithocholate on in vivo sulfation and glucuronidation of acetaminophen in rats. Pharm Res. 1988 Jan;5(1):61-4. doi: 10.1023/a:1015871713954. PMID: 3244612.
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Pharm Res. 1988 Jan;5(1):61-4. doi: 10.1023/a:1015871713954.

Effect of taurolithocholate on in vivo sulfation and glucuronidation of acetaminophen in rats.

Pharmaceutical research

R E Galinsky, B Chałasinska

Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, University of Utah, Salt Lake City 84112.

PMID: 3244612 DOI: 10.1023/a:1015871713954

Abstract

Taurolithocholate produces a prompt, complete, and reversible cessation of bile flow in rats. This is associated with impaired hepatic oxidative drug-metabolizing activity. The purpose of this study was to examine the effects of taurolithocholate-induced cholestasis on in vivo conjugation. The pharmacokinetics of acetaminophen and the two major processes specifically responsible for its elimination, namely, the formations of acetaminophen sulfate and acetaminophen glucuronide, were used to assess hepatic conjugating activity. A 30-mg/kg bolus of acetaminophen was administered intravenously to rats 2 hr (acute cholestasis) or 20 hr (postcholestasis) after intravenous pretreatment with sodium taurolithocholate, 5 mumol/100 g body weight. Acute cholestasis increased the total clearance of acetaminophen 20%, the partial clearance to acetaminophen sulfate 12%, and the partial clearance to acetaminophen glucuronide 85%. Postcholestasis, these parameters had significantly decreased compared to those during acute cholestasis and were comparable to control values. The results show that cholestasis does not impair acetaminophen conjugation in the rat.

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