Biochemical effectiveness of allopurinol and allopurinol-probenecid in previously benzbromarone-treated gout patients

Rational pharmacotherapy (RPT) in goutology: Define the serum uric acid target & treat-to-target patient cohort and review on urate lowering therapy (ULT) applying synthetic drugs

“…Many studies so far go into head-to-head comparison of production inhibitor A versus another production inhibitor B solely aiming at a biochemical target, never measuring excretion, the possible target of uricosurics [1,2]. Why not go for the rational principle to combine two different modes of action and go for a more potent strategy: for example add a production inhibitor to an excretion stimulator [3][4][5]. I here wish to elaborate on questions that are rational in individual patient care but were hardly posed over the last decades in studies.…”

Identification of Epoxide-Derived Metabolite(s) of Benzbromarone

“…Both BBR and 6-hydroxy BBR (a metabolite of BBR) have been reported to show potent human uric acid transporter 1 inhibition property (Wempe et al, 2011), which has made BBR a quite useful antigout agent for approximately 30 years in many countries. More recently, however, clinical cases of acute liver damage, including some fatalities related to BBR (Wagayama et al, 2000;Arai et al, 2002;Reinders et al, 2007), have drawn our attention to the metabolism profiles of BBR.…”

Successful Treatment of Refractory Gout Using Combined Therapy Consisting of Febuxostat and Allopurinol in a Patient with Chronic Renal Failure

“…Some studies have demonstrated the efficacy of combining an XOI and uricosuric agent (11,12), while others advocate the administration of high-dose febuxostat (up to 240 mg) and argue against the concurrent use of multiple XOIs due to concerns that the drugs would simply compete for the same active enzyme site (10). Despite such uncertainties, these two XOIs showed an additive effect, achieving the target range for the uric acid level in our patient.…”