feburic在治疗痛风这方面疗效如何?
Feburic (Febuxostat) is a new drug currently approved for the treatment of gout in my country. It can bind closely to the central active site of XO molybdopterin, so that its oxidized or reduced molybdenum cofactors are always in an isolated state, thereby inhibiting the collection of XO and substrates, reducing the formation of uric acid, and reducing the level of uric acid in the blood to achieve the effect of treating gout.
Unlike allopurinol, the feburic structure is a non-purine analogue and will not interact with other enzymes in the metabolism of purine and pyrimidine (such as purine nucleoside phosphorylase, etc.), nor will it affect the metabolism of pyrimidine and purine. In comparison, it can alleviate some adverse reactions caused by drugs.
A phase III clinical trial compared feburic (80 and 120 mg/d) and allopurinol (300 mg/d) in parallel. A 1-year study of 760 patients showed that compared with the allopurinol group, more patients in the feburic group achieved the main trial efficacy indicator - the sUA concentration was measured below 60 mg/L in the last 3 months (all subjects were gout patients, and the sUA concentration before the trial was above 80 mg/L);
After 52 weeks of treatment, feburic failed to significantly reduce the area of tophi (tophi is an aggregate of urate crystals unique to gout), but the effect was more obvious in the high-dose group early in the trial; in each treatment group, patients with sUA concentrations reaching the target (<60mg/L) were less likely to have gout attacks again, and their tophi area had a more significant reduction.
The "China Guidelines for the Diagnosis and Treatment of Hyperuricemia and Gout (2019)" recommends feburic (febuxostat) as the first-line drug for lowering uric acid in patients with gout. The starting dose is 20 mg/d, which can be increased by 20 mg/d in 2 to 4 weeks, and the maximum dose is 80 mg/d. It should be used with caution in the elderly with cardiovascular and cerebrovascular diseases; feburic is preferred for CKD stages 4 to 5 uric acid-lowering drugs, with a maximum dose of 40 mg/d.
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