非布司他 说明书

Instructions

[drug name]

Generic name: Febuxostat

English name: Febuxostat

[Main Ingredients] The active ingredient of this product is febuxostat.

[Ingredients] Chemical name: 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid; molecular weight: C16H16N2O3S

[Character] This product is white or off-white tablets.

[Indications/Function Indications] It is suitable for the long-term treatment of hyperuricemia in patients with gout. Not recommended for use in asymptomatic hyperuricemia.

[Usage and Dosage] The recommended oral dose of febuxostat is 40 mg or 80 mg once a day. The recommended starting dose of febuxostat is 40 mg once a day. If the blood uric acid level is still not less than 6 mg/dl (approximately 360 μmol/L) after 2 weeks, the recommended dose is increased to 80 mg once a day. There is no need to consider the effects of food and antacids when administering. Special groups: Patients with hepatic insufficiency: Patients with mild or moderate hepatic insufficiency (Child-Pugh Class A.B) do not need to adjust the dose. The efficacy and safety of febuxostat in patients with severe hepatic insufficiency (Child-Pugh Class C) have not yet been studied. Therefore, febuxostat should be used with caution in these patients. Renal insufficiency: Patients with mild or moderate renal insufficiency (Clcr30-89ml/min) do not need to adjust the dose. The recommended starting dose of febuxostat is 40mg once a day. If the blood uric acid level is still not less than 6mg/dl after 2 weeks, the recommended dose is increased to 80mg once a day. There is no sufficient research data in patients with severe renal insufficiency (Clu<30ml/min), so these patients should use febuxostat with caution. Uric Acid Levels Two weeks after starting febuxostat treatment, it is possible to assess whether the serum uric acid level has reached the target value (less than 6 mg/dl). Gout attack In the early stage of taking this product, gout attack may occur. This is because the change in blood uric acid level causes the urate deposited in the tissue to be mobilized. To prevent gout attacks during the initial stages of taking febuxostat, it is recommended to take NSAIDs or colchicine at the same time. The benefits of preventive treatment can last up to 6 months. If gout attacks during treatment with febuxostat, there is no need to interrupt the medication. Gout should be treated accordingly based on the patient's individual circumstances.

[Contraindications] This product is contraindicated in patients receiving azathioprine and mercaptopurine treatment.

[Precautions] Gout attacks: In the early stages of taking febuxostat, the frequency of gout attacks often increases. This is because blood uric acid concentration decreases, leading to mobilization of urate deposited in tissues. To prevent gout attacks during the initial stages of treatment, it is recommended to take nonsteroidal anti-inflammatory drugs or colchicine at the same time. If gout attacks during febuxostat treatment, there is no need to discontinue febuxostat treatment. Gout should be treated accordingly according to the patient's specific situation. Cardiovascular events In randomized controlled trials, patients treated with febuxostat had a higher rate of cardiovascular thrombotic events (including cardiovascular death, nonfatal myocardial infarction, and nonfatal stroke) than those treated with allopurinol, with febuxostat at 0.74/100 patient-years (95%CI: 0.36-1.37) and allopurinol at 0.60/100 patient-years (95% Cl:0.16-1.53). A causal relationship between febuxostat and cardiovascular thrombotic events has not been established. Pay attention to monitor the symptoms and signs of myocardial infarction and stroke when taking the drug.

[Pediatric Use] The safety and effectiveness of this product in children under 18 years of age have not yet been determined.

[Dose for Elderly Patients] No dose adjustment is required for elderly patients using this product. Compared with other age groups, there are no clinically significant differences in safety and effectiveness, but it cannot be ruled out that some elderly patients are more sensitive to this product. The Cmax and AUC24 of febuxostat in elderly patients (≥65 years old) after multiple-dose oral administration are similar to those in younger patients (18-40 years old).

[Drugs for Pregnant and Lactating Women] 1. Febuxostat is not teratogenic when administered orally to rats and rabbits during the organogenesis period at a dose of 48 mg/kg (respectively 40 and 50 times the human dose of 80 mg/day based on body surface area). During the organogenesis and lactation periods, oral administration of this product to pregnant rats at a dose of 48 mg/kg (40 times the human dose of 80 mg/day) was found to increase neonatal mortality and reduce neonatal weight gain. 2. Febuxostat is secreted into rat milk. It is unknown whether febuxostat is excreted in human breast milk. Because many drugs are excreted in human milk, caution should be exercised when administering this product to breastfeeding women.

[Drug Interactions] Febuxostat is a xanthine oxidase (XO) inhibitor. Although the interaction of this product with drugs metabolized by XO (such as chophylline, mercaptopurine, azathioprine) has not been studied, the inhibitory effect of this product on XO will increase the concentration of these drugs in the plasma and cause toxicity. Patients who are taking azathioprine, mercaptopurine or chophylline are prohibited from using this product.

[Drug Overdose] This product was administered to healthy subjects at a dose of 300 mg per day for 7 days without dose-limiting toxicity. No cases of overdose have been reported. Patients with overdose should receive symptomatic and supportive care.

[Pharmacology and Toxicology] Febuxostat is a xanthine oxidase inhibitor that achieves its therapeutic effect by reducing serum uric acid.

[Pharmacokinetics] In healthy subjects, Cmax and AUC increased in a dose-dependent manner after single or multiple doses of febuxostat 10 mg to 120 mg. No cumulative effect was observed when therapeutic doses were administered every 24 hours. The apparent average terminal elimination half-life (t1/2) of febuxostat is approximately 5 to 8 hours.

【Storage】Should be protected from light and sealed.