USMLE

Integrase Inhibitors

1,276 views
Antivirals
  1. Oseltamivir, Zanamivir
  2. Acyclovir (Famciclovir, Valacyclovir)
  3. Ganciclovir
  4. Foscarnet
  5. Cidofovir
  6. NRTIs
  7. NNRTIs
  8. Integrase Inhibitors
  9. Protease Inhibitors
  10. Entry Inhibitors (Enfuvirtide, Maraviroc)
  11. NS5A Inhibitors
  12. NS5B Inhibitors
  13. NS3/4A Inhibitors

Summary

Integrase inhibitors are drugs that end in the suffix “-tegravir”, including Raltegravir and Dolutegravir. As the name integrase inhibitor suggests, these drugs inhibit the enzyme integrase found in HIV, blocking the integration or insertion of newly-synthesized viral DNA into the host cell. Integrase inhibitors are active against both subtypes of HIV, and are commonly administered as a component of the HAART combination regimen, or Highly Active Antiretroviral Therapy. However, one potential side effect of integrase inhibitors is muscle damage that often presents as myositis.

Key Points

  • Integrase Inhibitors
    • Drug Names (-tegravir ending)
      • Raltegravir
      • Dolutegravir
      • Bictegravir
      • Elvitegravir
    • Mechanism
      • Inhibit retroviral integrase
        • Blocks integration of HIV viral DNA (made by reverse transcriptase) into host cell chromosome
        • Prevents viral usage of host machinery for replication
    • Indications
      • HIV
        • Active against both HIV-1 and HIV-2
        • Component of highly-active antiretroviral therapy (HAART)
          • Usually 3 drugs: 2 NRTIs and integrase or protease inhibitor
    • Adverse Effects
      • Myositis (myopathy)
        • Increase creatine kinase levels