febuxostat是什么药？

(Febuxostat) is a prescription drug suitable for the long-term treatment of hyperuricemia in patients with gout. It is not recommended for use in asymptomatic hyperuricemia.

The starting dose of febuxostat is 40 mg once daily. If the blood uric acid level is still not less than 6 mg/dl (approximately 360 μmol/L) after 2 weeks, it is recommended that the dose be increased to 80 mg once a day. Food and antacid effects do not need to be considered when administering the drug. Patients with mild or moderate hepatic insufficiency (Child-Pugh classes A and B) do not need to adjust the dosage. Patients with severe hepatic insufficiency (Child-Pugh class C) should use febuxostat with caution.

Pediatric Use: The safety and effectiveness of this product in treating patients under 18 years of age have not been established.

Elderly patients: No dosage adjustment is required for elderly patients. According to foreign literature reports, in clinical studies of febuxostat, people aged 65 and over accounted for 16% of the total number of subjects, and people aged 75 and over accounted for 4%. Comparing subjects of different age groups, there is no clinically significant difference in effectiveness and safety, but it cannot be ruled out that some elderly patients are more sensitive to this product. After multiple oral administrations of febuxostat to elderly subjects (65 years and above), Cmax and AUC24 were similar to those of young subjects (18 to 40 years old).

Mechanism of action of febuxostat: >80% of febuxostat can be rapidly and extensively absorbed after oral administration, with a tmax of approximately 1.0 to 1.8 hours. Febuxostat does not accumulate in the body after multiple oral doses of febuxostat administered daily. The effect of febuxostat 80 mg taken multiple times to reduce serum uric acid concentration is not affected by food, so febuxostat can be taken clinically without considering food factors. The steady-state apparent volume of distribution (Vss/F) of febuxostat after oral administration of 10 mg to 300 mg is 29 to 75 L. The plasma protein binding rate of febuxostat is approximately 99.2% (mainly albumin). Four hours after oral administration of febuxostat, the unchanged drug in plasma accounted for 84%-96% of the total radioactivity. The plasma half-life of febuxostat is 5 to 8 hours, and steady-state plasma concentration will be reached within 1 week after taking the drug once a day. febuxostat is mainly eliminated from the blood by being metabolized by the liver into glucuronic acid conjugates, and a smaller amount is oxidized and metabolized by CYP450 in the liver. Glucuronide-conjugated febuxostat is excreted in the urine, and less than 4% is excreted unchanged in the urine after oral administration.