Febuxostat

Abstract

Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing inservices. A comprehensive target drug utilization evaluation (DUE) is also provided each month. With a subscription, the monographs are sent in print and are also available online. Monographs can be customized to meet the needs of a facility. Subscribers to The Formulary Monograph Service also receive access to a pharmacy bulletin board, The Formulary Information Exchange (The F.I.X.). All topics pertinent to clinical and hospital pharmacy are discussed on The F.I.X. Through the cooperation of The Formulary, Hospital Pharmacy publishes selected reviews in this column. For more information about The Formulary Monograph Service or The F.I.X., call The Formulary at 800-322-4349. The August 2009 monograph topics are tolvaptan, besifloxacin ophthalmic suspension 0.6%, tadalafil, bromocriptine mesylate, and acetaminophen intravenous. The DUE is on tolvaptan.

A comparative study of efficacy of febuxostat and allopurinol regimens in patients of hyperuricemia

“…Since these drugs are unable to get metabolised by xanthine oxidase, severe toxicity is experienced. 30 Febuxostat does not inhibit or induce cytochrome P450 enzymes, thus lacking significant drug interactions with other drugs metabolized by these enzymes. 26 Allopurinol increases the plasma concentration of probenecid and enhances its uricosuric effect, while probenecid increases oxypurinol clearance, thus increased dose regimens of allopurinol are needed.…”

“…Less than 6% of the administered dose is excreted in the urine in its unchanged form. Its mean halflife is 4 to 9 h. 30 No clinically significant effect has been found for food or antacids on its absorption. 31…”

Febuxostat: A novel agent for management of Hyperuricemia in gout

“…The pharmacokinetics of febuxostat appears to be linear in the 10 mg to 120 mg once-daily dose range[ 9 ]. It is mainly metabolized to its acylglucuronide metabolite via uridine diphosphate glucuronosyltransferase (UGT) enzymes and to a lesser extent to its active oxidative metabolites 67M-1, 67M-2, and 67M-4 via cytochrome P450 enzymes[ 10 ]. Less than 6% of the administered dose is excreted in the urine as unchanged drug[ 10 ].…”

“…All adverse events were of mild intensity. The overall incidence of adverse events during dosing was higher for subjects in the moderate hepatic impairment (75%) and mild hepatic impairment (63%) groups as compared to subjects in the normal hepatic function group (25%)[ 10 ]. There were no serious adverse events or clinically significant changes from baseline in laboratory values, physical examination, vital signs, or ECG readings during the study period.…”

“…Prophylactic therapy with nonsteroidal anti-inflammatory drug or colchicine is advised to prevent the same. However, discontinuation of febuxostat is not necessary if a gout flare occurs[ 10 ]. Periodic liver function tests are advised for patients receiving febuxostat as transaminase elevations greater than 3 times the upper limit of normal were observed in patients treated with febuxostat in clinical trials[ 10 ].…”