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MUSCULO-SKELETAL SYSTEM › ANTIGOUT PREPARATIONS › ANTIGOUT PREPARATIONS › Preparations increasing uric acid excretion
lesinurad
M04AB05
Adult Dosing
- 200 mg once daily, taken in the morning with food and water
- Must be co-administered with a xanthine oxidase inhibitor (allopurinol or febuxostat)
- Maximum recommended dose is 200 mg daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of hyperuricemia associated with gout in combination with a xanthine oxidase inhibitor when target serum uric acid levels are not reached with the xanthine oxidase inhibitor alone
Mechanism of Action
- Selective uric acid reabsorption inhibitor (SURI)
- Inhibits urate transporters anion transporter 1 (URAT1) and organic anion transporter 4 (OAT4)
- Decreases uric acid reabsorption, increases uric acid excretion, and lowers serum uric acid levels
Contraindications
- CrCl less than 30 mL/min
- End-stage renal disease
- Dialysis
- Kidney transplant recipients
- Tumor lysis syndrome or Lesch-Nyhan syndrome
- Hypersensitivity to lesinurad
Adverse Reactions
- Acute renal failure
- Increased serum creatinine
- Influenza
- Gastroesophageal reflux disease (GERD)
- Headache
Drug Interactions
- Moderate to strong CYP2C9 inhibitors (e.g., fluconazole, amiodarone) may increase exposure
- May decrease systemic exposure of sensitive CYP3A substrates (e.g., oral contraceptives); additional non-hormonal contraception recommended
- Aspirin doses greater than 325 mg/day may decrease the efficacy of lesinurad
Curated Content: Needs Vetting Before Put to Clinical Use