Which pharmacologic drug classes are used in antiretroviral therapy for HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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HAART provides effective treatment options for treatment-naive and treatment-experienced patients. Pharmacologic drug classes include:

  • Nucleoside reverse transcriptase inhibitors (NRTIs)

  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

  • Protease inhibitors (PIs)

  • Integrase inhibitors (INSTIs)

  • Fusion inhibitors (FIs)

  • Chemokine receptor antagonists (CCR5 antagonists)

  • Entry inhibitors (CD4-directed post-attachment inhibitors)

Each class targets a different step in the viral life cycle as the virus infects a CD4 T lymphocyte or other target cell. The use of these agents in clinical practice is largely dictated by their ease or complexity of use, side-effect profile, efficacy based on clinical evidence, practice guidelines, and clinician preference.

Resistance, adverse effects, pregnancy, and coinfection with hepatitis B virus, or hepatitis C virus present important challenges to clinicians when selecting and maintaining therapy.

This article reviews the mechanism of action, resistance, pharmacokinetics, and adverse effects of each of these classes, as well as current treatment guidelines for their use in adults and adolescents with HIV infection. Also discussed are the important challenges involved in selecting and maintaining antiretroviral therapy for pregnant women and patients with acute HIV infection, hepatitis B or C coinfection, or Mycobacterium tuberculosis coinfection.

For additional information on HIV disease, see the following Medscape Reference articles HIV Infection and AIDS and Pediatric HIV Infection.

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