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Indinavir

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Indinavir, Crixivan

  • See Also
  1. Anti-Retroviral Therapy
  2. Protease Inhibitor
  • Indications
  1. HIV Infection (as part of combination therapy)
    1. Has been replaced by newer Protease Inhibitors with fewer adverse effects
    2. Among the first Protease Inhibitors for HIV (FDA approved in 1996)
  • Mechanism
  1. See Protease Inhibitor
  • Efficacy
  1. When originally studied in the 1990s, Indinavir was very effective in combination with Zidovudine (AZT)
  2. Newer Protease Inhibitors are combined with boosters (e.g. Ritonavir, Cobicistat) and are used with other Antiretrovirals
  • Medications
  1. Capsules: 100, 200, 400 mg
  • Dosing
  1. Adults (as part of combination therapy with other Antiretrovirals)
    1. Indinavir 800 mg orally three times daily
    2. Indications to reduce dose to 600 mg orally three times daily
      1. Delavirdine
      2. Itraconazole or Ketoconazole
      3. Hepatic insufficiency
  2. Take on empty Stomach
    1. One hour before or 2 hours after a meal
    2. Concurrent food reduces concentration up to 80%
  3. Drink at least 1.5 Liters (50 oz) liquid per day
    1. Drink 150 ml water per hour for 3 hours after dose
    2. Avoids Nephrolithiasis and Interstitial Nephritis
  • Adverse Effects
  1. See Protease Inhibitor for adverse effects attributed to the class
  2. Well tolerated
  3. Indirect Bilirubin (elevation in 10% of patients)
  4. Nephrolithiasis in 2-3% of patients
  5. Hyperglycemia
  6. Renal Insufficiency
  7. Alopecia
  8. Dry Skin
  9. Xerostomia
  10. Paronychia
  11. Gallstones
  • Drug Interactions
  1. See Protease Inhibitor
  2. Drug Interactions are common with Protease Inhibitors
    1. Protease Inhibitors cause the most Drug Interactions of all Antiretrovirals
    2. Use formal Drug Interaction applications when prescribing
  3. St. John's Wort
    1. May reduce Indinavir concentrations by 80%
    2. Piscitelli (2000) Lancet 355:547-8 [PubMed]
  4. Rifabutin
    1. Decrease Rifabutin dose to 50% AND
    2. Increase Indinavir 1000 mg orally three times daily
  5. Medications contraindicated with Indinavir (a strong CYP3A4 Inhibitor)
    1. Alfuzosin
    2. Amiodarone
    3. Ergot alkaloids (e.g. Ergonovine, Ergotamine)
    4. Pimozide
    5. High dose Sildenafil (Revatio)
    6. Sedative Hypnotics (oral Midazolam, Triazolam, Alprazolam)
  • Safety
  1. Avoid in Lactation (as with other Protease Inhibitors)
  2. Pregnancy Category C
    1. Risk of perinatal Hyperbilirubinemia
  • Resources
  1. Indinavir (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=702727cb-3eff-425b-9573-031332849430
  • References
  1. (1998) Med Lett Drugs Ther 40(1041):115 [PubMed]
  2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]