Integrase Inhibitors

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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