Generic Name and Formulations:
Lesinurad 200mg; tabs.
Indications for ZURAMPIC:
In combination with a xanthine oxidase inhibitor, to treat hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone.
Limitations Of use:
Not for treatment of asymptomatic hyperuricemia. Not for use as monotherapy.
Take in the AM with food and water. 200mg once daily with a xanthine oxidase inhibitor (including allopurinol or febuxostat). Max 200mg daily. Patients on daily allopurinol dose <300mg (or <200mg with eCLCr <60mL/min): not recommended.
<18yrs: not established.
Severe renal impairment (eCLCr <30mL/min), ESRD, kidney transplant recipients, or dialysis patients. Tumor lysis syndrome or Lesch-Nyhan syndrome.
Risk of acute renal failure, more common when used without a xanthine oxidase inhibitor.
Risk of acute renal failure when used without a xanthine oxidase inhibitor. Assess renal function prior to initiation and periodically thereafter. Renal impairment (eCLCr <45mL/min): do not initiate. If eCLCr <60mL/min or with serum creatinine (SCr) elevations 1.5–2X pre-treatment value: monitor more frequently; if SCr >2X pre-treatment value: interrupt treatment. Discontinue therapy if eCLCr is persistently <45mL/min. Maintain adequate hydration (2 liters of liquid per day). Give gout flare prophylaxis. Severe hepatic impairment: not recommended. Females should use additional non-hormonal methods of contraception. Pregnancy. Nursing mothers.
Caution with concomitant moderate CYP2C9 inhibitors (eg, fluconazole, amiodarone) and in CYP2C9 poor metabolizers. Antagonized by moderate CYP2C9 inducers (eg, rifampin, carbamazepine), aspirin >325mg/day (in combination with allopurinol). Antagonizes CYP3A substrates (eg, sildenafil, amlodipine). May affect sensitive CYP3A substrates (eg, HMG-CoA reductase inhibitors); monitor. Concomitant epoxide hydrolase inhibitors (eg, valproic acid): not recommended. May reduce efficacy of hormonal contraceptives.
Headache, influenza, blood creatinine increase, GERD; gout flares, renal events, cardiovascular events.
Tabs—5, 30, 90