What are pharmacokinetic interactions that affect hepatic metabolism in antiretroviral therapy?

Updated: Jul 12, 2021
  • Author: Shahab Qureshi, MD, FACP; Chief Editor: Michael Stuart Bronze, MD  more...
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Answer

Answer

Pharmacokinetic interactions that affect hepatic metabolism occur via the following mechanisms:

  • Via the cytochrome P450 enzyme system (most drugs)
  • CYP3A4 is the most common enzyme responsible for drug metabolism
  • Via the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) 1A1 enzyme: Metabolism of INSTIs dolutegravir (DTG) and raltegravir (RAL)
  • The INSTIs bictegravir and dolutegravir have mixed metabolic pathways, including both CYP3A4 and UGT1A1

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