Pharm

Darunavir

search

Darunavir, Darunavir/r, Prezista, Prezcobix

  • See Also
  1. Anti-Retroviral Therapy
  2. Protease Inhibitor
  • Indications
  1. HIV Infection (as part of combination therapy)
  • Contraindications
  1. Age <3 years (toxicity risk)
  2. Sulfonamide Allergy (Exercise caution if used)
  • Mechanism
  1. See Protease Inhibitor
  • Medications
  1. Darunavir (Prezista)
    1. Tablets: 75, 150, 600 and 800 mg (600 mg tablet is generic)
    2. Suspension: 100 mg/ml
    3. Typically combined wiith Ritonavir as separate tablet (Darunavir/r)
      1. All adverse effects and Drug Interactions on this page assume administration with Ritonavir
  2. Combinations (with Cobicistat instead of Ritonavir)
    1. Darunavir with Cobicistat (Prezcobix)
    2. Darunavir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide (Symtuza)
  • Dosing
  • Adult
  1. Therapy naive or experienced without known Darunavir resistance substitutions
    1. Darunavir 800 mg orally daily AND
    2. Ritonavir 100 mg orally daily
  2. Known Darunavir resistance substitutions, pregnancy or child weight >40 kg
    1. Darunavir 600 mg orally twice daily AND
    2. Ritonavir 100 mg orally twice daily
  • Dosing
  • Child (age 3 to 11 years, weight >=10 kg)
  1. Contraindicated in age <3 years
  2. Dosing off-label and per U.S. HIV Treatment guidelines (differs from FDA approved package insert dosing)
    1. Indicated in therapy naive or experienced with or without known Darunavir resistance substitutions
  3. Weight 10 to 11 kg: Darunavir 200 mg and Ritonavir 32 mg, both taken orally twice daily
  4. Weight 11 to 12 kg: Darunavir 220 mg and Ritonavir 32 mg, both taken orally twice daily
  5. Weight 12 to 13 kg: Darunavir 240 mg and Ritonavir 40 mg, both taken orally twice daily
  6. Weight 13 to 14 kg: Darunavir 260 mg and Ritonavir 40 mg, both taken orally twice daily
  7. Weight 14 to 15 kg: Darunavir 280 mg and Ritonavir 48 mg, both taken orally twice daily
  8. Weight 15 to 30 kg: Darunavir 375 mg and Ritonavir 48 mg, both taken orally twice daily
  9. Weight 30 to 40 kg: Darunavir 450 mg and Ritonavir 100 mg, both taken orally twice daily
  10. Weight >40 kg: Darunavir 600 mg and Ritonavir 100 mg, both taken orally twice daily (adult dose)
  • Adverse Effects
  1. See Protease Inhibitor for adverse effects attributed to the class
  2. Rash (10%)
    1. Stevens-Johnson Syndrome risk
    2. May be severe, requiring Darunavir to be discontinued
  3. Hepatotoxicity
    1. Monitor serum transaminases (AST, ALT) at baseline and for at least the first few months of therapy
  • Safety
  1. Avoid in Lactation
  2. Pregnancy
    1. Among preferred Protease Inhibitors in pregnant women who are HIV Treatment naive
  • Drug Interactions
  1. Multiple Drug Interactions
    1. See Protease Inhibitor
    2. As with other Protease Inhibitors, check a formal Drug Interaction application before prescribing
  2. Clarithromycin
    1. Decrease Clarithromycin dose if Creatinine Clearance <60 ml/min
  3. Azole Antifungals (esp. Ketoconazole, Itraconazole)
    1. Limit to low dose (e.g. ketonazole 200 mg)
  4. Voriconazole
    1. Ritonavir decreases Voriconazole levels and efficacy
    2. Avoid concurrent use if possible
  5. Oral Contraceptives
    1. Use backup or alternative Contraception
  6. Drospirenone
    1. Hyperkalemia risk when used in combination
    2. Monitor Serum Potassium if Drospirenone used with Darunavir
  7. Didanosine
    1. Didanosine is buffered with decreased Darunavir oral absorption
    2. Take Didanosine at least 1 hour before or 2 hours after Darunavir/r
  8. Statins (esp. Atorvastatin, Pravastatin or Rosuvastatin)
    1. Limit to lowest effective dose (e.g. Atorvastatin 20 mg/day)
  9. Contraindicated medications in combination with Darunavir
    1. Dronedarone
    2. Elbasavir-grazoprevir (Zepatier)
    3. Everolimus
    4. Glecaprevir-pibrentasvir (Mavyret)
    5. Lopinavir-Ritonavir
    6. Ranolazine
    7. Saquinavir
    8. Ticagrelor
  • Resources
  1. Darunavir (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=814301f9-c990-46a5-b481-2879a521a16f
  2. Darunavir with Cobicistat (Prezcobix, DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9c38fdb6-d0ba-4f16-a0e3-85d9ec334d9f
  3. Darunavir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide (Symtuza, DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=85a17d00-6b7c-41ea-a6b3-5ad924820dab
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]