Uloric (Febuxostat Tablets)—近40年来获美国FDA批准的第一个用于治疗高尿酸症的痛风药物
2009年美国初次批准：
作用机制
ULORIC，一种黄嘌呤氧化酶抑制剂，通过降低血清尿酸达到其治疗作用。在治疗浓度不期望ULORIC抑制涉及嘌呤和嘧啶合成和代谢的其它酶。
适应证和用途
ULORIC是一种黄嘌呤氧化酶(XO)抑制剂适用于高尿酸血症痛风患者的慢性处理。
不推荐ULORIC对无症状高尿酸血症的治疗。
剂量和给药方法
1）ULORIC被推荐40mg或80 mg每天1次。推荐的ULORIC起始剂量是40mg每天1次。对用40mg后2周未达到血清尿酸(sUA)低于6mg/dL患者，建议用ULORIC 80mg。
2）ULORIC可以不管食物或使用抗酸药给药。
3）当给予ULORIC至有轻至中度肾或肝损伤患者无需调整剂量。
剂量和规格
片：40mg，80mg。
禁忌证
正在用硫唑嘌呤，巯基嘌呤，或茶碱治疗的患者禁忌ULORIC。
警告和注意事项
1）爆发痛风：开始用抗尿酸血症药物，包括ULORIC期间经常观察到爆发痛风增加。如治疗期间发生爆发痛风，不需要停止ULORIC。预防性治疗(即，开始治疗用非甾体抗炎药物(NSAID)或秋水仙碱)可能有益直至6个月.
2）心血管事件：在临床试验中，用ULORIC治疗患者中比别嘌呤醇观察到更高发生率的心血管栓塞事件。监查MI和中风的征象和症状。
3）肝酶升高：在ULORIC-治疗患者中曾观察到转氨酶升高。定期监查肝功能试验。
不良反应
ULORIC-治疗患者发生率至少1%和大于安慰剂至少0.5%的不良反应是肝功能异常，恶心，关节痛，和皮疹。
为报告怀疑的不良反应，联系Takeda Pharmaceuticals在1.877.825.3327或FDA在1.800.FDA.1088或www.fda.gov/medwatch.
药物相互作用
同时给予ULORIC与XO底物药物，硫唑嘌呤，巯基嘌呤，或茶碱 可能增加这些药物的血浆浓度导致严重毒性。
特殊人群中使用
1）有严重肾损伤患者资料不够充分。.尚未在严重肝损伤患者中进行研究。应谨慎对待这些患者。
2）未曾在继发性高尿酸血症(包括患者正在治疗的Lesch-Nyhan综合征或恶性病，或器官移植接受者)进行研究；所以，建议这些患者不使用ULORIC 。

Uloric (febuxostat tablets)
DESCRIPTION
ULORIC (febuxostat) is a xanthine oxidase inhibitor. The active ingredient in ULORIC is 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid, with a molecular weight of 316.38. The empirical formula is C16H16N2O3S.
Febuxostat is a non-hygroscopic, white crystalline powder that is freely soluble in dimethylformamide; soluble in dimethylsulfoxide; sparingly soluble in ethanol; slightly soluble in methanol and acetonitrile; and practically insoluble in water. The melting range is 205°C to 208°C.
ULORIC tablets for oral use contain the active ingredient, febuxostat, and are available in two dosage strengths, 40 mg and 80 mg. Inactive ingredients include lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, sodium croscarmellose, silicon dioxide and magnesium stearate. ULORIC tablets are coated with Opadry II, green.
CLINICAL PHARMACOLOGY
Mechanism of Action
ULORIC, a xanthine oxidase inhibitor, achieves its therapeutic effect by decreasing serum uric acid. ULORIC is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations
INDICATIONS AND USAGE
ULORIC is a xanthine oxidase (XO) inhibitor indicated for the chronic management of hyperuricemia in patients with gout.
ULORIC is not recommended for the treatment of asymptomatic hyperuricemia.
USE IN SPECIFIC POPULATIONS
There is insufficient data in patients with severe renal impairment. No studies have been conducted in patients with severe hepatic impairment. Caution should be exercised in these patients.
No studies have been conducted in patients with secondary hyperuricemia (including patients being treated for Lesch-Nyhan syndrome or malignant disease, or in organ transplant recipients); therefore, ULORIC is not recommended for use in these patients. 
CONTRAINDICATIONS
ULORIC is contraindicated in patients being treated with azathioprine or mercaptopurine
WARNINGS AND PRECAUTIONS
Gout Flare: An increase in gout flares is frequently observed during initiation of anti-hyperuricemic agents, including ULORIC. If a gout flare occurs during treatment, ULORIC need not be discontinued. Prophylactic therapy (i.e., non-steroidal anti-inflammatory drug (NSAID) or colchicine upon initiation of treatment) may be beneficial for up to six months.
Cardiovascular Events: A higher rate of cardiovascular thromboembolic events was observed in patients treated with ULORIC than allopurinol in clinical trials. Monitor for signs and symptoms of MI and stroke.
Liver Enzyme Elevation: Transaminase elevations have been observed in ULORIC-treated patients. Monitor liver function tests periodically.
DRUG INTERACTIONS
Concomitant administration of ULORIC with XO substrate drugs, azathioprine or mercaptopurine could increase plasma concentrations of these drugs resulting in severe toxicity
ADVERSE REACTIONS
Adverse reactions occurring in at least 1% of ULORIC-treated patients, and, at least 0.5% greater than placebo, are liver function abnormalities, nausea, arthralgia, and rash.
To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals at 1-877-TAKEDA-7 (1-877-825-3327) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
DOSAGE AND ADMINISTRATION - SUMMARY
ULORIC is recommended at 40 mg or 80 mg once daily. The recommended starting dose of ULORIC is 40 mg once daily. For patients who do not achieve a serum uric acid (sUA) less than 6 mg per dL after 2 weeks with 40 mg, ULORIC 80 mg is recommended.
ULORIC can be administered without regard to food or antacid use.
No dose adjustment is necessary when administering ULORIC to patients with mild to moderate renal or hepatic impairment.
Recommended Dose
For treatment of hyperuricemia in patients with gout, ULORIC is recommended at 40 mg or 80 mg once daily.
The recommended starting dose of ULORIC is 40 mg once daily. For patients who do not achieve a serum uric acid (sUA) less than 6 mg per dL after 2 weeks with 40 mg, ULORIC 80 mg is recommended.
ULORIC can be taken without regard to food or antacid use.
Special Populations
No dose adjustment is necessary when administering ULORIC in patients with mild to moderate renal impairment. The recommended starting dose of ULORIC is 40 mg once daily. For patients who do not achieve a sUA less than 6 mg per dL after 2 weeks with 40 mg, ULORIC 80 mg is recommended.
No dose adjustment is necessary in patients with mild to moderate hepatic impairment.
Uric Acid Level
Testing for the target serum uric acid level of less than 6 mg per dL may be performed as early as 2 weeks after initiating ULORIC therapy.
Gout Flares
Gout flares may occur after initiation of ULORIC due to changing serum uric acid levels resulting in mobilization of urate from tissue deposits. Flare prophylaxis with a non-steroidal anti-inflammatory drug (NSAID) or colchicine is recommended upon initiation of ULORIC. Prophylactic therapy may be beneficial for up to six months.
If a gout flare occurs during ULORIC treatment, ULORIC need not be discontinued. The gout flare should be managed concurrently, as appropriate for the individual patient [see Warnings and Precautions].
HOW SUPPLIED
DOSAGE FORMS AND STRENGTHS
40 mg tablets, light green to green, round shaped, debossed with "TAP" and "40"
80 mg tablets, light green to green, teardrop shaped, debossed with "TAP" and "80"
http://www.drugs.com/pro/uloric.html
http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021856lbl.pdf
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产地国家： 加拿大
原产地英文商品名:
ULORIC tablets 80mg/tablet 30tablets/bottle
原产地英文药品名:
Febuxostat
中文参考商品译名:
ULORIC 80毫克/片 30片/瓶
中文参考药品译名:
非布索坦
曾用名:
非布索坦 菲布力 非布司他
生产厂家中文参考译名:
Takeda
生产厂家英文名:
Takeda