Sulfation

A conjugation reaction that involves adding a sulphate group to a suitable functional group on a drug or a phase I metabolite. Reactions are catalysed by sulfotransferase enzymes found mainly in liver. Different sulfotransferases recognise different classes of substrates; alcohols, phenols, arylamines and steroids. At lower drug concentrations (such as during the early stages of a repeated dosing regimen), sulfation tends to predominate over glucuronidation.

Sulphates formed in the liver are usually transported out of the hepatocyte by ATP-binding cassette (ABC) transporters, either into the bile or into the bloodstream prior to renal elimination.

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An ABC of PK/PD Copyright © 2023 by Dr. Andrew Holt is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License, except where otherwise noted.

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