Ritonavir-boosted protease inhibitors in HIV therapy

Ann Med. 2011 Aug;43(5):375-88. doi: 10.3109/07853890.2011.572905. Epub 2011 Apr 18.


The advent of combination antiretroviral therapy has led to significant improvement in the care of HIV-infected patients. Originally designed as a protease inhibitor (PI), ritonavir is currently exclusively used as a pharmacokinetic enhancer of other protease inhibitors, predominantly due to ritonavir's potent inhibition of the cytochrome P450 3A4 isoenzyme. Ritonavir-boosting of PIs decrease pill burden and frequency of dosing. Boosted PIs are recommended for first-line therapy in treatment and play a key role in the management of treatment-experienced patients. Potential problems associated with PIs include metabolic abnormalities (e.g. dyslipidemia), increased cardiovascular risk, and drug interactions.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 CYP3A Inhibitors
  • Drug Interactions
  • Drug Therapy, Combination
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / pharmacology
  • HIV Protease Inhibitors / therapeutic use*
  • Humans
  • Ritonavir / administration & dosage
  • Ritonavir / pharmacology
  • Ritonavir / therapeutic use*


  • Cytochrome P-450 CYP3A Inhibitors
  • Enzyme Inhibitors
  • HIV Protease Inhibitors
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human
  • Ritonavir