What is lesinurad, and how does it work (mechanism of action)?

Lesinurad is an oral medication that reduces uric acid levels in people who have too much uric acid in their blood (hyperuricemia) and have symptoms of gout. It is the first approved drug in a new class of drugs called selective uric acid reabsorption inhibitors (SURI).

Uric acid is formed from the breakdown of certain chemicals (purines) in the body. Hyperuricemia occurs when the body produces more uric acid than it can eliminate. The uric acid forms crystals in joints (gouty arthritis) and tissues, causing inflammation and pain. Elevated blood uric acid levels also can cause kidney disease and kidney stones.

Lesinurad reduces uric acid levels by blocking the function of proteins in the kidney involved in reabsorbing uric acid from urine back into the blood stream. Reducing reabsorption of uric acid reduces the levels of uric acid in the body. Lesinurad is used in combination with another class of drugs called xanthine oxidase inhibitors. The FDA approved lesinurad in December, 2015.

What brand names are available for lesinurad?

Zurampic

Is lesinurad available as a generic drug?

No

Do I need a prescription for lesinurad?

Yes

What are the uses for lesinurad?

Lesinurad is used in combination with a xanthine oxidase inhibitor for the treatment of  high blood uric acid levels (hyperuricemia) associated with gout in patients who do not reach target serum uric acid levels with a xanthine oxidase inhibitor alone. Lesinurad should not be used for the treatment of high uric acid levels without symptoms of gout and it should not be used by itself (monotherapy).

What are the side effects of lesinurad?

Common side effects of lesinurad include:

Possible serious side effects of lesinurad include:

What is the dosage for lesinurad?

Lesinurad is taken by mouth and should be combined with axanthine oxidase inhibitor such as allopurinol (Zyloprim) or febuxostat (Uloric). The recommended daily dose and maximum dose is 200 mg once daily by mouth, in the morning with food and water. Lesinurad should be taken at the same time as the morning dose of the xanthine oxidase inhibitor. If the xanthine oxidase inhibitor is stopped, lesinurad should also be stopped. Lesinurad is not recommended for patients taking daily doses of allopurinol less than 300 mg or less than 200 mg in patients with estimated creatinine clearance (a measure of kidney function) less than 60 mL/min.

QUESTION

The term arthritis refers to stiffness in the joints. See Answer

Which drugs or supplements interact with lesinurad?

Lesinurad blood levels are increased by drugs such as amiodarone (Cordarone) and fluconazole (Diflucan) that reduce its breakdown in the liver. Lesinurad blood levels are decreased by drugs, such as rifampin and carbamazepine, that increase its breakdown in the liver. Lesinurad may reduce blood levels of sildenafil (Viagra), amlodipine (Norvasc), and other drugs that are broken down by CYP3A4 liver enzymes. Aspirin doses higher than 325 mg per day may decrease the effect of lesinurad and allopurinol treatment.

Lesinurad may reduce the effect of hormonal contraceptives. Women should use additional methods of contraception when taking lesinurad.

Is lesinurad safe to take if I'm pregnant or breastfeeding?

There are no adequate trials of lesinurad use in pregnant women. Therefore, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if lesinurad is excreted into human milk.

What else should I know about lesinurad?

What preparations of lesinurad are available?

Tablets: 200 mg

How should I keep lesinurad stored?

Lesinurad tablets should be stored at room temperature, 15 C to 30 C (59 to 86 F)

Summary

Lesinurad (Zurampic) is a drug that lowers uric acid levels in the blood, which helps alleviate the symptoms of gouty arthritis. It is used in combination with a xanthine oxidase inhibitor and should not be used by itself. Doing so may cause kidney failure.

Treatment & Diagnosis

Prevention & Wellness

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Medically Reviewed on 9/4/2019
References
FDA Prescribing Information.