Drug reference

benzbromarone

Uricosuric agent, URAT-1 inhibitor · Antihyperuricemic

Uricosuric agent, URAT-1 inhibitorAntihyperuricemic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

FDA category + note

Mechanism

Benzbromarone is a potent uricosuric agent that acts as a reversible inhibitor of the urate-anion exchanger, URAT-1, in the proximal tubule. This mechanism increases uric acid excretion.

Indications

Patients who are allergic to or refractory to other drugs used for the treatment of gout

Dosing

Adult: As the micronized powder, it is effective in a single daily dose ranging from 25 to 100 mg.

Pharmacokinetics

Onset

Absorbed readily after oral ingestion; peak plasma levels are achieved in about 4 h.

Metabolism

Metabolism involves predominantly CYP2C9, with contributions by CYP3A4 and CYP1A1. Potent inhibition of CYP2C9.

Excretion

Metabolized to monobrominated and dehalogenated derivatives (both have uricosuric activity) and is excreted primarily in the bile.

Contraindications

Not approved for use in the U.S. or the European Union

Side effects

Serious

Hepatotoxicity (reported, limiting availability)
Fulminant hepatitis (may be caused by formation of hepatotoxic metabolites and inhibition of mitochondrial function)