Pharm

Non-Nucleoside Reverse Transcriptase Inhibitor

search

Non-Nucleoside Reverse Transcriptase Inhibitor, NNRTI, Rilpivirine, Endurant, Delavirdine, Rescriptor

  • Mechanism
  1. Bind directly to reverse transcriptase
  2. Prevents RNA conversion to DNA
  3. Completely different mechanism than nRTI
  • Preparations
  • First Generation
  1. Delavirdine (Rescriptor)
  2. Efavirenz (Sustiva, EFV)
  3. Nevirapine (Viramune, NVP)
  • Preparations
  • Second Generation
  1. Etravirine (Intelence)
    1. Approved in treatment experienced patients
  2. Rilpivirine (Endurant)
    1. FDA approved in 2011 for treatment-naive patients
    2. Available as oral agent and monthly IM Injection (as part of Cabenuva therapy)
  • Adverse Reaction
  1. See specific agents
  2. Hyperlipidemia
  3. Rash is common (especially with Nevirapine)
    1. More common and more severe in women
    2. Reduced Incidence if start dose slowly over 2 weeks
    3. Prophylaxis not recommended (e.g. Corticosteroids)
      1. Antinori (2001) AIDS 15:1579-81 [PubMed]
    4. Switching to a different drug class may be needed
    5. My progress to Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis, Erythema Multiforme
      1. Severe rash is especially more common with Etravirine and especially in women