Effect of single oral doses of benzbromarone on serum and urinary uric acid

Abstract

The effects of various single oral doses of micronized benzbromarone on serum and urinary uric acid and urinary oxypurines were studied in 5 healthy volunteers and in 5 patients with gout. There was an effective, unequivocal, and dose-related reduction in serum uric acid levels in both groups. The simultaneous increased excretion of urinary uric acid but not of oxypurines suggests the mechanism of effect is uricosuria. The prolonged duration of action up to 48 hours after dosing is advantageous as the drug need be taken only once a day. The data presented favor a protracted trial of benrbromarone in patients with gout and hyperuricemia.

Uricosuric effect of different doses of irtemazole in normouricaemic subjects

“…A prolonged effect of a single dose of 80 mg benzbromarone for up to 48 h has been described [7,8]. Following 1.5 g probenecid, plasma uric acid begins to decline after 0.5 to 3 h [9,10] and effect lasts for 16 to 24 h [11].…”

Management of Hyperuricemia and Gout

“…Allopurinol extends the half-life of Benemid and potentiates its uricosuric effect, whereas Benemid increases the clearance of oxypurinol diminishing the inhibition of xanthine oxidase [ 608,655 ] . These mechanisms would suggest that the usual doses of allopurinol should be increased, whereas standard doses of Benemid should be decreased.…”

“…Like other uricosuric drugs, benzbromarone is ineffective at low glomerular fi ltration rates (<25 ml/min) [ 607 ] . Like other uricosuric drugs, the most common side effects are the precipitation of an acute episode of gouty arthritis or the formation of uric acid calculi [ 606,608 ] . Utilizing colchicine prophylaxis, using low doses of benzbromarone at the outset of therapy, encouraging high fl uid intake, and alkalinizing the urine can easily avoid these complications.…”

Management of gout

“…BNZ shows adequate oral bioavailability, has a long half-life, and its uricosuric action reaches its peak at 12 h, extending to 24 h (112)(113)(114). BNZ may be effective at a 50-200 mg daily dose.…”