非布司他的最新说明书

[Common name]:

[Product name]: uloric

[All names]: febuxostat, febuxostat, feburic, febuxostat, uloric, zurig

[Indications]:

For the treatment of chronic hyperuricemia (gout). 

[Usage and Dosage]:

Febuxostat was started at 10 mg/day for 2 weeks, then increased to 20 mg/day for 4 weeks, then to 40 mg/day. Starting with a low dose and gradually increasing the dose can prevent acute gout attacks caused by initial changes in blood uric acid levels. Treat with febuxostat 40 mg/day for 6 months, and check the uric acid level regularly. Generally, it takes 6 months to clean up excess blood uric acid in the body.

After 6 months of treatment:

(1) If the serum uric acid level remains between 240 umol/l and 360 umol/l, maintain febuxostat 40 mg/day treatment.

(2) If the blood uric acid level is higher than 360 umol/l, increase the dose of fexostatin by 60 mg/day, up to a maximum of 80 mg/day, and monitor blood uric acid, liver and kidney function regularly.

(3) If the blood uric acid level is lower than 240 umol/l, the dose of febuxostat can be reduced to 20 mg/day and the treatment can be maintained for 6 months.

  [Adverse reactions]:

serious side effects

1. Liver function damage (unknown frequency), because the increase in AST (GOT) and ALT (GPT) is accompanied by liver function damage, patients should have regular examinations and discontinue medication if they are found to be unwell.

2. Allergy (unknown frequency), systemic rash, skin rash, etc. Patients should be checked regularly and discontinue medication if any discomfort is found. 

Other side effects

1. (Unknown frequency): Decreased platelet count, anemia;

2. (Less than 1%): Decreased number of white blood cells;

3. (less than 1%): TSH increase;

4. (Unknown frequency) Headache, abnormal taste;

5. (Less than 1%) Numbness in hands and feet, dizziness;

6. Rapid heartbeat;

7. (Less than 1%) Abnormal electrocardiogram;

8. (Less than 1%) Diarrhea, abdominal discomfort, nausea, and abdominal pain;

9. (1%-5%) Abnormal liver function test values [increased ALT (GPT), increased GOT (AST), increased γ-GTP, etc.);

10. (Unknown frequency) Urticaria;

[Taboo]:

1. Patients with past allergies to the essential ingredients;

2. Patients taking thiol-containing drugs or azathioprine tablets at the same time. 

[Notes]:

Due to the rapid decrease in serum uric acid concentration in the early stage of taking this product, the uric acid deposited in the tissue can be mobilized, so symptoms similar to gout attacks may occur. In this case, nonsteroidal anti-inflammatory drugs or colchicine can be used for preventive administration. In addition, during the treatment of this product, some patients need to be monitored for symptoms related to myocardial infarction and liver damage. 

[Mechanism of action]:

Febuxostat is rapidly and extensively absorbed by >80% after oral administration, with a tmax of approximately 1.0 to 1.8 hours. Febuxostat does not accumulate in the body after multiple oral administrations of a single daily dose. The effect of multiple doses of Febuxostat 80 mg on reducing serum uric acid concentration is not affected by food, so the clinical use of Febuxostat does not require consideration of 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. Febuxostat is approximately 99.2% plasma protein bound (mainly to albumin). Four hours after oral administration of febuxostat, unchanged drug in plasma accounted for 84%-96% of the total radioactivity. The plasma half-life of febuxostat is 5 to 8 hours. Taking the drug once a day will reach steady-state plasma concentration within 1 week. Febuxostat is mainly eliminated from the blood by being metabolized by the liver to glucuronide conjugates, and a smaller amount is oxidatively metabolized by CYP450 in the liver. Glucuronide-conjugated febuxostat is excreted in the urine, and less than 4% of febuxostat is excreted unchanged in the urine after oral administration.

  [Efficacy and Safety]:

A multicenter, double-blind, randomized phase II clinical study evaluated the safety and efficacy of febuxostat in gout. A total of 136 male and 17 female gout patients were randomly assigned to receive placebo or this product (40, 80 or 120 mg/d). After 4 weeks, the test found that the serum uric acid concentration of patients in each dose group of this product was significantly lower than before treatment, with an average reduction of 37% in each group from low to high dosage. , 44% and 59%, while patients in the placebo group only decreased by 2%; the vast majority of patients persisted in completing the trial. The incidence of adverse reactions in the febuxostat and placebo groups was similar, and most of these adverse reactions were mild and self-limiting. Common ones include diarrhea, pain, back pain, headache and joint pain.

【Storage】：

Store in a cool place.