inPractice® - Hepatic Metabolism

Authors: Amanda H. Corbett, PharmD, BCPS, FCCP; Colin I. Sheffield, PharmD (More Info)
Section Editor: Eric S. Daar, MD
Editors in Chief: Daniel R. Kuritzkes, MD; Joseph J. Eron, Jr., MD
Last Reviewed: 6/1/18 (What's New)

Most antiretrovirals are metabolized via the liver and are known as substrates for liver enzyme metabolism
- Raltegravir and dolutegravir are primarily metabolized by glucuronidation via the UGT1A1 enzyme^{[FDA Raltegravir; Reese 2013]}
  - Raltegravir is available in 2 doses for treatment-naive patients and patients who are virologically suppressed on an initial 400-mg twice-daily regimen: 400 mg twice daily or 1200 mg once daily^{[FDA Raltegravir]}