非布司他治疗痛风效果如何？

In February 2009, the U.S. Food and Drug Administration approved it for the long-term treatment of patients with gout and hyperuricemia. Febuxostat can reduce uric acid levels in the blood of patients with hyperuricemic gout. Clinical studies have shown that febuxostat is safe and effective. Febuxostat is metabolized by the liver and does not rely on renal excretion. Therefore, there is no need to reduce the dose for patients with moderate to severe hepatic and renal insufficiency. Today we will find out how effective febuxostat is in the treatment of gout?

The advantages of febuxostat compared with allopurinol: 1. No dose adjustment is required for patients with mild to moderate renal insufficiency; 2. There are few drug-drug interactions, which increases efficacy and safety; 3. Patients with hypersensitivity to allopurinol tolerate febuxostat well; 4. The half-life is long and can be taken once a day, improving compliance; 5. It does not affect other enzymes in the metabolism of purine and pyrimidine, with fewer adverse reactions; 6. The tophi dissolution rate is higher.

   Research results show that long-term use of febuxostat can maintain long-term blood uric acid in most patients at ≤6.0 mg/dl. Mild to moderate impairment of renal function has no significant impact on the pharmacodynamics and pharmacokinetics of febuxostat. Therefore, the uric acid-lowering effect of febuxostat is no different from that of patients with normal renal function, and its safety is good. Due to the limitations of allopurinol application, there is an urgent need for the emergence of new urate-lowering drugs. Febuxostat is a non-purine xanthine oxidase inhibitor. Its launch provides a new option for gout patients. It has been approved by the European Union and the United States for the treatment of gout and hyperuricemia. Moreover, febuxostat has a better uric acid-lowering effect than allopurinol without serious adverse reactions, and has been fully used clinically. The currently recommended application method is: the initial dose is 40 mg/d. If the blood uric acid still does not reach ≤6.0 mg/dl after 2 weeks, increase the dose to 80 mg/d. 

  Febuxostat is absorbed in the intestine after oral administration, with a bioavailability of 47%, a blood and plasma protein binding rate of 99.2%, and is mainly metabolized in the liver, with a half-life of 5 to 8 hours. It is metabolized in the liver into inactive substances, 49% is excreted through the kidneys, and 45% is excreted through the feces, which is a dual-channel excretion drug. Therefore, the dosage is small and it is not completely dependent on renal excretion, so patients with gout who have mild to moderate renal insufficiency do not need to adjust the dosage when using it. However, gout patients with abnormal liver function need to use it with caution.