Pharm

Raltegravir

search

Raltegravir, Isentress, RAL

  • See Also
  1. Anti-Retroviral Therapy
  2. Cabotegravir
  • Indications
  1. HIV Infection (as part of combination therapy)
  • Mechanism
  1. See Integrase Strand Transfer Inhibitor
  • Medications
  1. Raltegravir tablets: 400 mg
  2. Raltegravir HD tablets: 600 mg (use 2 for 1200 mg daily dose)
  3. Raltegravir single use powder packets for suspension: 100 mg/5 ml (when reconstituted)
  4. Raltegravir chewable tablets (with Phenylalanine): 25 and 100 mg
  • Dosing
  • Adult (or child weight>=25 kg)
  1. Twice daily dosing (InSTI experienced, or virus not suppressed)
    1. Raltegravir 400 mg orally twice daily
  2. Once daily dosing (InSTI naive AND suppressed Viral RNA copies)
    1. Raltegravir HD 1200 mg orally once daily
  • Dosing
  • Child (weight <25 kg)
  1. FDA approved for newborns (including weight guidelines down to 2 kg)
  2. See other dosing references for pediatric dosing
  • Adverse Effects
  1. Rhabdomyolysis (or mopathy)
  2. Hypersensitivity Reactions and severe rashses (e.g. Stevens Johnson Syndrome)
  • Safety
  1. Avoid in Lactation
  2. Pregnancy
    1. Among the preferred InSTI's in pregnancy
    2. Pregnancy registry exists
  • Drug Interactions
  1. Rifampin
    1. increase dose to 800 mg orally twice daily
  2. Medications that interfere with absorption (take Dolutegravir 2 hours before or 6 hours after these agents)
    1. Aluminum Hydroxide and Magnesium Hydroxide Antacid
    2. Calcium Carbonate
  3. Medications contraindicated with Dolutegravir HD (daily dosing formulation)
    1. Entravirine
    2. Rifampin
    3. Tipranavir/r
  • Pharmacokinetics
  1. Excretion via Glucuronidation
  2. Avoid before Hemodialysis
  • Resources
  1. Raltegravir (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3