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Lesinurad

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Lesinurad, Zurampic, Duzallo

  • See Also
  1. Uricosuric
  2. Gouty Arthritis
  3. Probenecid
  • Indications
  1. Gouty Arthritis (chronic, refractory)
    1. Must be used in combination with Xanthine Oxidase Inhibitor (Allopurinol or Febuxostat)
  • Contraindications
  1. Renal Impairment (GFR <30-45 mL/min) including end-stage renal disease and those on Hemodialysis
  2. Renal Transplant
  3. Tumor Lysis Syndrome
  4. Lesch-Nyhan syndrome
  5. Severe hepatic Impairment
  • Mechanism
  1. Selective Uricosuric (increases renal Uric Acid excretion)
  2. Blocks Uric Acid renal reabsorption via blockade of 2 apical transporters
    1. Uric Acid Transporter 1 Inhibitor (URAT1 Inhibitor)
    2. Organic Anion Transporter 4 Inhibitor (OAT-4 Inhibitor)
  • Medications
  1. Lesinurad (Zurampic): 200 mg tabs
  2. Allopurinol with Lesinurad (Duzallo)
    1. As of 2017, costs $12/day (compared with $3/day for Allopurinol and probenacid)
    2. (2017) Presc Lett 24(11): 64
  • Dosing
  1. Adults: 200 mg orally each morning
  • Adverse Effects
  1. Acute Renal Failure (black box warning)
    1. Monitor Renal Function at baseline and periodically during treatment
    2. Do NOT use as Uric Acid monotherapy
    3. Must be taken with Xanthine Oxidase Inhibitor (Allopurinol or Febuxostat)
      1. Allopurinol dose must be at least 300 mg/day (at least 200 if CrCl <60 ml/min)
  2. Cardiovascular events
  • Safety
  1. Unknown safety in Lactation
  2. Unknown safety in pregnancy
  • Drug Interactions
  1. Oral Contraceptives
    1. Lesinurad may reduce Oral Contraceptive efficacy
    2. Use non-Hormonal Contraception
  2. CYP2C9 Inhibitors (e.g. Fluconazole, Amiodarone) and CYP2C9 poor metabolizers
    1. May increase Lesinurad levels
  • Resources
  1. Lesinurad (FDA package insert)
    1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207988lbl.pdf