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本药为美国FDA于2009年2月13日刚刚批准的新药，根据美国FDA批准的剂量和用量，Uloric只有每片40毫克与每片80毫克的两个剂型；建议用量为起始40毫克剂量，一天一片；服用两星期后，如果sUA指标达不到<6mg/dL，建议服用80毫克剂量，一天一片。（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. ）
2009年美国初次批准：
一般描述
ULORIC (非布索坦)是一种黄嘌呤氧化酶抑制剂。ULORIC中的活性组分是2-[3-cyano4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-羧酸盐，分子量316.38。经验式为C16H16N2O3S。
化学结构是：
非布索坦是一种不吸潮，白色结晶粉易溶于二甲基甲酰胺，溶于二甲基亚砜；微溶于乙醇；略微溶于甲醇和乙腈和实际上不溶于水。熔点范围205°C至208°C。
为口服使用ULORIC片剂含活性组分，非布索坦，和可得到两种剂量规格，40 mg和80 mg。无活性组分包括乳糖一水合物, 微晶纤维素, 羟基丙基纤维素, 交联羧甲基纤维素钠, 二氧化硅和硬脂酸镁。 ULORIC片剂用Opadry II, 绿包被。
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。(1)
不推荐ULORIC对无症状高尿酸血症的治疗。(1)
剂量和给药方法
1）ULORIC被推荐40 mg或80 mg每天1次。推荐的ULORIC起始剂量是40 mg每天1次。对用40 mg后2周未达到血清尿酸(sUA)低于6 mg/dL患者，建议用ULORIC 80 mg。(2.1)
2） ULORIC可以不管食物或使用抗酸药给药。(2.1)
3）当给予ULORIC至有轻至中度肾或肝损伤患者无需调整剂量。(2.2)
剂量和规格
片：40 mg，80 mg。(3)
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。(4)
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.(2.4, 5.1)
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。 (5.2)
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。(5.3)
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。(6.1)
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。(7)
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。(8.6, 8.7)
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 。(8.8)
Important Safety and Other Information
ULORIC is a prescription medicine used to lower blood uric acid levels in adults with gout.
Individual results may vary.
Do not take ULORIC if you are taking Azathioprine(Imuran®,Azasan®),Mercaptopurine (Purinethol), or Theophylline (Theo-24®, Elixophyllin®, Theochron, Theolair®, Uniphyl).
For some people, gout may flare up when starting certain gout medicines, including ULORIC. If you have a flare while taking ULORIC, do not stop taking your medicine.
Your healthcare provider may give you other medicines to help prevent your gout flares.
Heart Problems. A small number of heart attacks, strokes and heart-related deaths were seen in clinical studies.
It is not certain that ULORIC caused these events.
Your healthcare professional may do blood tests to check your liver function while you are taking ULORIC.
The most common side effects are liver problems, nausea, gout flares, joint pain, and rash.
Uloric - What You Need to Know
Uloric, generic name febuxostat, has been approved by the FDA for the chronic management of hyperuricemia in gout.
Uloric is the first new treatment option for gout in over 40 years.
Uloric Recommended for FDA ApprovalThe FDA arthritis advisory committee has recommended the approval of Uloric for the treatment of gout.
Uloric, the name that has been given to generic Febuxostat, was recommended by a 12-0 vote (one member of the committee abstained).
Febuxostat: More Effective Than Standard Drug
Febuxostat, a new treatment for gout, is at least twice as effective at lowering uric acid levels than allopurinol.
Study results about febuxostat came from the largest and longest trial of gout drugs ever conducted.
Mismanagement of Gouty Arthritis Not Uncommon Although gouty arthritis is not considered a difficult disease to diagnose and gout treatments are very effective in most cases, errors in the management of gout are common.
Gout - 10 Things You Should Know
Gout is an intensely painful type of arthritis.
There are 10 important facts you should know about gout.
Fast Facts About GoutGout is one of the most painful types of arthritis.
Gout is caused by uric acid crystals deposited in the body's tissues which lead to recurrent attacks of joint inflammation.
Gout Screening Quiz
Gout is one of the most painful types of arthritis. Do you have symptoms which are
associated with gout? Do you have a lifestyle which increases the risk factors associated with gout?
Take our Gout Screening Quiz.
Gout Risk Factor QuizA risk factor increases your chances of developing gout but it is not certain that you will develop the disease.
What factors increase the risk of developing gout?
How to Recognize the Signs and Symptoms of GoutGout symptoms are very painful and are caused by monosodium urate crystals in joints and surrounding tissues. Gout symptoms can occur with more frequency if untreated.
The Gout Quiz - Test Your Knowledge of Gout
How much do you know about gout?
You probably heard of it, but do you know the difference between purines and gout medication probenecid?
Do you know what you need to do to prevent gout attacks? Does your lifestyle put you at risk for gout?
Take the Gout Quiz and test your knowledge.
How To Treat Gout With Diet And MedicationGout is one of the most painful types of arthritis.
Gout attacks can be controlled or prevented by lifestyle changes and the use of
certain medications.
The Gout Guide: Free E-Course Newsletter
We have designed our free newsletter e-course to guide you to better understand gout. Learn more about gout basics, gout history, gout cause, gout diagnosis, gout treatment, gout prevention, gout diet, gout medication, and gout research.
New Gout Drug Gets FDA Panel NodUloric, First New Gout Drug in 40 Years, Recommended for FDA ApprovalBy Daniel J.
DeNoonWebMD Health NewsReviewed by Louise Chang, MDNov. 24, 2008 -- Uloric should be the first new gout drug to be approved in over 40 years, an FDA expert panel recommends.
Currently, allopurinol (trade name, Zyloprim) is the only FDA-approved drug that prevents formation of the uric acid crystals that cause gout.
However, side effects -- including potentially fatal reactions -- limit the amount of allopurinol that can be tolerated. Most gout patients do not receive fully effective doses of allopurinol.
In clinical trials sponsored by Takeda, Uloric's manufacturer, an 80-milligram dose of Uloric worked better than allopurinol; a 40-milligram dose worked at least as well as allopurinol.
Unlike allopurinol, very little Uloric is excreted through the urine, making Uloric safe
for patients with kidney problems. Gout patients with impaired kidney function have to take very low doses of allopurinol, making the drug even less effective for these patients.
In 2005, the FDA refused to approve Uloric because there were slightly more deaths and heart problems in patients taking the drug than in patients taking allopurinol. As people with gout problems already are at higher risk of heart disease, the FDA issued an "approvable" letter, noting that Uloric could be approved if this safety question were addressed.
Takeda then performed a large new phase 3 clinical trial that enrolled more gout patients than the two previous phase 3 trials combined.
The new study found no more deaths and no more heart problems in patients taking Uloric than in patients taking allopurinol.
Based on the safety and efficacy data, the FDA panel recommended by a 12-0 vote that the FDA approve Uloric at both the 40-milligram and 80-milligram doses.
Takeda suggests the higher dose is more effective in subjects with more severe gout.
Takeda has offered to continue studying Uloric after FDA approval. A phase 4 clinical trial would compare Uloric to allopurinol for the reduction of gout flare-ups.
And because drugs with the same mechanism of action as Uloric and allopurinol may affect theophylline bronchodilators, Takeda has agreed to conduct a postmarketing phase 1 study of Uloric's interactions with theophylline.
Gout occurs when blood levels of uric acid rise.
At blood levels above 7 mg/dL -- and above 6 mg/dL in the extremities -- crystals can form that lodge in the joints and other body tissues.
These crystal deposits provoke an immune response that results in extremely painful swelling and in inflammatory arthritis that can permanently destroy the joints.
(For more on the causes, symptoms, and treatment of gout, see WebMD's Gout Pictures Slideshow.)About 1.4% of men and 0.6% of women have gout.
But prevalence rises with age. After age 80, about 9% of men and 6% of women develop gout.
The body converts a chemical called xanthine into uric acid via an enzyme called xanthine oxidase or XO. Allopurinol and Uloric each inhibit XO and prevent the formation of uric acid.
Allopurinol is approved in doses up to 800 milligrams. However, it's rarely dosed above 300 milligrams per day and is often ineffective.
Allopurinol side effects include upset stomach, headache, diarrhea, and rash. Although rare, allopurinol hypersensitivity syndrome can develop. It's fatal 20% to 30% of the time.
The most common side effects seen in patients taking Uloric during clinical trials were upper respiratory tract infections, muscle and connective-tissue symptoms, and diarrhea. The drug was well tolerated, and these side effects did not increase over long-term use.
Uloric (Febuxostat)
Uloric (febuxostat) is a medication prescribed for treating the patients diagnosed with gout or kidney stones. Patients with such condition have a remarkably high concentration level of uric acid causing build-up of stones in the urinary canal. The drug tries to prevent the uric acid from being produced in massive amounts.
Usage
The starting dose for taking Uloric (febuxostat) is 40mg and will be the recommended dosage for two weeks. After that time frame, the dosage will be increased to 80mg if the serum uric acid level is below 6 mg/dL. The drug is taken once a day. It can be taken with or without food intake and regardless if you are taking in any antacids. Do not worry if your physician might change the dosage from time to time. It is a required action, according to the needs of your organism. To avoid any confusion, do not hesitate to ask your doctor.
Prior to taking the medication, make sure that you have understood all the prescriptions the physician has given you. Do not take any dose larger or smaller than the desired amount of medicine or even take the drug longer than the required period. It may cause unwanted effects to your body.
Precaution
Uloric (febuxostat) has the capacity to react dangerously with other medications, so make sure to go through each medication you are taking with your health care provider. The medications you need to be extra cautious with are Azathioprine (Azasan) and Mercaptopurine (Purinethol), as the combination may cause toxicity in the body.
Meanwhile, when you happen to forget and miss a dose, take the drug as soon as you remember it. However, if in any case that you remembered about the dose just hours before the next scheduled administration, forget the missed dose and just administer the next. Avoid taking in extra doses because this might pose unwanted effects.
Side Effects
Alert the physician for any occurrence of allergic reactions from Uloric (febuxostat), such as difficulty and shortness of breath, skin inflammation/itchiness/blotchiness, and swelling of the lips, tongue, mouth, and throat. It is important to know how to identify the minor drug effects from the serious ones. Ask for medical intervention when you are experiencing any of the following: pain in the chest area, abrupt body weakness and numbness, yellowing of the ayes and skin. Although dubbed as minor effects, moderate rashes in the skin and nausea should not be ignored at all.
Uloric（febuxostat，非布索坦）-FDA批准40年来首个抗痛风新药
Uloric（febuxostat，非布索坦），是抗痛风药。Uloric（febuxostat，非布索坦）对氧化型和还原型的XOR均有显著的抑制作用，因而其降低尿酸的作用更强大、持久，因此本品可用于治疗痛风的慢性高尿酸血症。
痛风的发生是由于体内产生尿酸过多及肾脏清除能力下降，尿酸体内蓄积，导致尿酸盐结晶在关节及各脏器沉积。因此，痛风的治疗通常采取的手段是：促进尿酸排泄和抑制尿酸生成，并采用适当措施改善相关症状。
体内尿酸的生成与嘌呤代谢有关，在嘌呤代谢的最后步骤中，次黄嘌呤在黄嘌呤氧化还原酶（XOR）的作用下生成黄嘌呤，再进一步生成尿酸，抑制该酶的活性可以有效的减少尿酸的生成。非布索坦为目前世界上最新研制的XOR抑制剂，其通过高度选择性地作用于该氧化酶，减少体内尿酸合成，降低尿酸浓度，从而有效治疗通风疾病。
30年来，别嘌呤醇是临床上唯一一个用于抑制尿酸生成的药物，并作为痛风的黄金治疗药物广泛用于临床，在抗痛风的治疗中取得了不俗的成绩。
日本武田开发的Uloric（febuxostat，非布索坦）是FDA最近40年来批准的唯一一只用于治疗痛风的新药，在2005年FDA曾经拒绝过Uloric（febuxostat，非布索坦），的申请，因为当时的临床数据显示，Uloric有可能会有较高的死亡率和心血管副作用，但在经过新的更大规模的Ⅲ期试验后解决了这个悬疑。
适应症： 痛风
生产公司：日本武田（Takeda）
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产地国家: 武田制药美国公司
原产地英文商品名:
ULORIC
原产地英文药品名:
FEBUXOSTAT
原产地英文化合物名称:
FEBUXOSTAT
中文参考商品译名:
优络瑞克 80毫克/片 30片/瓶
中文参考药品译名:
非布索坦
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产地国家: 武田制药美国公司
原产地英文商品名:
ULORIC
原产地英文药品名:
FEBUXOSTAT
原产地英文化合物名称:
FEBUXOSTAT
中文参考商品译名:
优络瑞克 40毫克/片 30片/瓶
中文参考药品译名:
非布索坦 |
