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Updated: Jan 11 2022

Reverse Transcriptase Inhibitors

  • Snapshot
    • A 31-year-old woman is in the labor and delivery unit undergoing about to undergo a cesarean section at 38-weeks gestation. She is HIV-positive and was found to have an HIV RNA viral load of 1200 copies/mL. She has been nonadherent to her medications. She is started on intravenous zidovudine 3 hours prior to the surgery in order to decrease the risk of HIV transmission to the newborn.
  • Introduction
    • Mechanism of action
      • nucleoside reverse transcriptase inhibitors (NRTIs)
        • NRTIs are phosphorylated inside the infected cell, inhibiting the viral reverse transcriptase and impairing viral replication
          • terminates chain elongation
            • the NRTIs lacks a 3‚Ä≤ OH group
          • note that these are highly active against HIV-1 and HIV-2
          • tenofovir is a nucleotide reverse transcriptase inhibitor, the others are nucleosides
      • non-nucleoside reverse transcriptase inhibitors (NNRTIs)
        • a similar mechanism of action as NRTIs; however, it binds to the viral reverse transcriptase at a different site
          • note these are highly active against HIV-1 but not HIV-2
          • NNRTIs do not require phosphorylation
    • Mechanism of resistance
      • resistance mutations (there are multiple)
    • Clinical use
      • a component of antiretroviral therapy for treating HIV
    • Adverse reactions
      • NRTIs
        • mitochondrial toxicity
          • can result in peripheral neuropathy, pancreatitis, lipoatrophy, and/or hepatic steatosis
        • lactic acidosis
        • bone marrow suppressing
      • NNRTIs
        • there are no specific class-related adverse events
          • neurologic and psychiatric side effects (efavirenz and rilpivirine)
      • NRTIs (Reverse Transcriptase Inhibitors)
      • Abacavir (ABC)
      • Contraindicated in patients with HLA-B*5701
        • associated with increased risk of hypersensitivity¬†
      • Didanosine (ddl)
      • Associated with pancreatitis
      • Emtricitabine (FTC)
      • -
      • Lamivudine (3TC)
      • -
      • Stavudine (d4T)
      • -
      • Tenofovir (TDF)
      • -
      • Zidovudine (ZDV)
      • Associated with anemia
      • Can be used for
        • post-exposure prophylaxis
        • intrapartum prophylaxis
      • NNRTIs (Reverse Transcriptase Inhibitors)
      • Delavirdine
      • Contraindicated in pregnancy
      • Efavirenz
      • Associated with vivid dreams and central nervous system symptoms
      • Contraindicated in pregnancy
      • Nevirapine
      • -
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