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:
- Headache
- Influenza
- Blood creatinine increased
- gastroesophageal reflux disease
Possible serious side effects of lesinurad include:
- Kidney failure
- Increased blood creatinine levels
- Kidney stones
- Heart attack
- Stroke
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)