Integrase Strand Transfer Inhibitor

Aka: Integrase Strand Transfer Inhibitor, Integrase Inhibitor, InSTI

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II. Indications

  1. HIV Infection
    1. Anti-retroviral naive or experienced patients as part of combination therapy

III. Mechanism

  1. Anti-retroviral agent
  2. Integrase Strand Transfer Inhibitor
    1. Prevents viral DNA from integrating into host DNA
    2. Blocks the integrase enzyme

IV. Medications: Single Agents

  1. Bictegravir
    1. Only available as combination agent
    2. Biktarvy contains Bictegravir (an InSTI) and 2 nRTI agents, Emtricitabine (FTC), Tenofovir (TAF)
  2. Cabotegravir (Vocabria)
    1. See Cabotegravir
    2. Cabenuva (Cabotegravir and Rilpivirine) IM Monthly Injection is used for HIV Infection Treatment
    3. Cabotegravir (Apretude) IM Monthly Injection is indicated in HIV Pre-exposure Prophylaxis or PReP
  3. Dolutegravir (Tivacay)
    1. See Dolutegravir
    2. Dolutegravir and Lamivudine (Dovato)
    3. Dolutegravir 50 mg AND Rilpivirine 25 mg (Juluca)
  4. Raltegravir (Isentress)

V. Safety

  1. Lactation
    1. Unknown safety in Lactation
  2. Pregnancy
    1. Dolutegravir (Tivacay)
      1. Unsafe in pregnancy
      2. Associated with Neural Tube Defects
      3. May be a class effect (unclear if this applies to other Integrase Inhibitors)

VI. Efficacy

  1. Drug resistance is common

VII. Adverse Effects: General

  1. Weight gain
  2. Hyperglycemia
  3. Hyperlipidemia
  4. Weight gain (2 to 7 kg, more in women)

VIII. Adverse Effects: Raltegravir

  1. Diarrhea
  2. Nausea
  3. Headache
  4. Serum Creatinine phosphokinase (CPK) increases
  5. Mild Serum Creatinine increase without affecting Renal Function (Dolutegravir)
  6. Myopathy
  7. Rhabdomyolysis
  8. Insomnia
  9. Liver Function Test abnormalities (Cabotegravir)

IX. Drug Interactions

  1. Typically fewer Drug Interactions than other Anti-Retroviral Agents
  2. Phenytoin
  3. Rifampin
  4. St John's Wort
  5. Avoid taking at the same time as Calcium, Magnesium, aluminum and iron containing agents

X. References

  1. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  2. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]

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