|
当前位置：新特药品资料下载首页 >> 新特药品PDF说明书 >> ZURAMPIC(lesinurad 200mg/tablets)
ZURAMPIC(lesinurad 200mg/tablets)
痛风是一种在机体中积蓄太多尿酸所致的疼痛形式的关节炎，和通常表现首先为发红，疼痛，和大脚趾肿。尿酸在血中通过物质在机体所有组织都找到的被称为嘌呤分解而产生。尿酸通常在血中溶解然后经过肾和在尿至机体外。尿酸可在血中积蓄，一种情况被称为高尿酸血症。这发生当机体增加制造尿酸量，肾脏不能摆脱足够尿酸，或人们吃太多高嘌呤食物。大多数有高尿酸血症人们不发生痛风，但如尿酸在机体中形成结晶，可能发生痛风。 FDA的药品评价和研究中心中肺，过敏反应，和风湿病产品部主任Badrul Chowdhury，M.D.，Ph.D说：“卫生保健提供者和其有严重哮喘患者当疾病用他们当前哮喘治疗不能很好控制时现有另外治疗选择考虑。” 批准日期：2016年3月23日；公司：Teva Pharmaceutical Industries Ltd. ZURAMPIC(lesinurad)片，为口服使用 一般描述 ZURAMPIC(lesinurad)是一种URAT1抑制剂。Lesinurad有以下化学名：2-((5-bromo-4-(4cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)醋酸。分子式为C17H14BrN3O2S和分子量为404.28。结构式为： 可得到ZURAMPIC为为口服给药蓝色膜包衣片含200 mg lesinurad和以下无活性成分：一水乳糖，微晶纤维素，羟丙甲纤维素2910，交联聚乙烯吡咯烷酮，和硬脂酸镁。ZURAMPIC片s 涂盖有欧巴代蓝。 作用机制 Lesinurad通过抑制涉及在肾脏中尿酸再吸收转运蛋白的功能减低血清尿酸水平。Lesinurad 抑制两个负责对尿酸再吸收根尖[apical]转运蛋白的功能，尿酸转运蛋白1(URAT1)和有机阴离子转运蛋白4(OAT4)，有IC50值分别为7.3和3.7 μM。URAT1 是负责从肾小管腔被过滤的尿酸的再吸收的多数。OAT4是一个利尿剂-诱导高尿酸血症关联尿酸转运蛋白。Lesinurad与位于近端曲小管细胞的基底侧膜上尿酸再吸收转运蛋白SLC2A9(Glut9)无相互作用。 适应证和用途 ZURAMPIC是一种URAT1抑制剂适用与一种黄嘌呤氧化酶抑制剂联用为与痛风关联高尿酸血症的治疗在患者单独用一种黄嘌呤氧化酶抑制剂未实现目标血清尿酸水平。 使用限制： ⑴ 建议对无症状高尿酸血症的治疗不用ZURAMPIC。 ⑵ ZURAMPIC不应用作单药治疗。 剂量和给药方法 ⑴ ZURAMPIC被推荐在200 mg每天1次与一种黄嘌呤氧化酶抑制剂联用，包括别嘌呤醇[allopurinol]或非布索坦[febuxostat]。ZURAMPIC的最大每天剂量是200 mg。 ⑵ 未能服用ZURAMPIC与一种黄嘌呤氧化酶抑制剂可能增加肾不良反应风险。 ⑶ ZURAMPIC片应在早晨与食物和水服用。 ⑷应指导患者处于被很好水化。 ⑸ 开始ZURAMPIC前评估肾功能。如eCLcr是低于45mL/min不要开始ZURAMPIC。 ⑹如eCLcr持续地下降低于45mL/min终止ZURAMPIC。 剂型和规格 片：200 mg。 禁忌证 严重肾受损，肾病终末期，肾移植受体，或用透析患者。 警告和注意事项 ⑴ 肾事件： ZURAMPIC开始后曽发生肾功能相关不良反应，在400 mg剂量观察到较高发生率，用单药治疗发生率最高。用ZURAMPIC治疗开始和期间监视肾功能，尤其是有eCLcr 低于60 mL/min患者，和评价急性尿酸肾病的体征和症状. ⑵ 心血管事件：用ZURAMPIC观察到重大不良心血管事件；尚未确定因果相互关系。 不良反应 在12-个月对照临床试验中最常见不良反应(发生大于或等于2%用Zurampic治疗与一种黄嘌呤氧化酶抑制剂联用患者和比用单独黄嘌呤氧化酶抑制剂更频)是头痛，流感，血肌酐增加，和胃食管反流病， 药物相互作用 ⑴ 中度细胞色素P450 2C9(CYP2C9)抑制剂：谨慎使用。 ⑵ 敏感CYP3A底物：监视对CYP3A底物的疗效。 特殊人群中使用 ⑴ 肾受损：对有eCLcr低于45 mL/min患者建议不使用。 ⑵ 肝受损：建议对有严重肝受损患者不使用。 ZURAMPIC® (lesinurad) 200mg tablets Lesinurad 200mg tablets were approved as ZURAMPIC® by the U.S. Food and Drug Administration (FDA) in December 2015 for use in combination with a xanthine oxidase inhibitor (XOI) for the treatment of hyperuricemia associated with uncontrolled gout. The licensing agreement includes exclusive U.S. rights to the fixed-dose combination of lesinurad and allopurinol. AstraZeneca plans to submit, on Ironwood’s behalf, the fixed-dose combination program for FDA regulatory review in the second half of 2016. The agreement also includes certain rights to potentially access RDEA3170 in gout indications in the U.S. Gout is a serious, progressive and debilitating form of inflammatory arthritis. As many as two million patients in the U.S. on urate-lowering therapy have inadequately controlled hyperuricemia associated with gout, as XOI treatment alone is not sufficient to achieve their serum uric acid (sUA) treatment goals. ZURAMPIC is not recommended for the treatment of asymptomatic hyperuricemia and should not be used as monotherapy. About ZURAMPIC® (lesinurad) 200mg tablets FDA-approved ZURAMPIC® (lesinurad) works selectively to complement xanthine oxidase inhibitors (XOIs) in the treatment of hyperuricemia associated with uncontrolled gout. ZURAMPIC is not recommended for the treatment of asymptomatic hyperuricemia and should not be used as monotherapy. XOIs reduce the production of uric acid; ZURAMPIC increases the excretion of uric acid. Together, the combination of ZURAMPIC and an XOI provides a dual mechanism of action that both decreases production and increases excretion of uric acid, thereby lowering serum uric acid (sUA) levels in patients who have not achieved target serum uric acid levels with XOI treatment alone. ZURAMPIC selectively inhibits the function of transporter proteins urate transporter (URAT1) and organic anion transporter 4 (OAT4), involved in uric acid reabsorption in the kidney. The safety and efficacy of ZURAMPIC was established in three Phase III clinical trials that evaluated a once-daily dose of ZURAMPIC in combination with the XOI allopurinol or febuxostat compared to XOI alone. Important Safety Information and Limitations of Use WARNING: RISK OF ACUTE RENAL FAILURE MORE COMMON WHEN USED WITHOUT A XANTHINE OXIDASE INHIBITOR (XOI) •Acute renal failure has occurred with ZURAMPIC and was more common when ZURAMPIC was given alone •ZURAMPIC should be used in combination with an XOI Contraindications: •Severe renal impairment (eCLcr less than 30 mL/min), end-stage renal disease, kidney transplant recipients, or patients on dialysis •Tumor lysis syndrome or Lesch-Nyhan syndrome Warnings and Precautions: •Renal events: Adverse reactions related to renal function have occurred after initiating ZURAMPIC. A higher incidence was observed at the 400-mg dose, with the highest incidence occurring with monotherapy use. Monitor renal function at initiation and during therapy with ZURAMPIC, particularly in patients with eCLcr below 60 mL/min, and evaluate for signs and symptoms of acute uric acid nephropathy. ZURAMPIC should not be initiated in patients with an eCLcr less than 45 mL/min •Cardiovascular events: Major adverse cardiovascular events were observed with ZURAMPIC; a causal relationship has not been established Adverse Reactions: •Most common adverse reactions with ZURAMPIC (in combination with an XOI and more frequently than on an XOI alone) were headache, influenza, blood creatinine increased, and gastroesophageal reflux disease Indication and Limitations of Use for ZURAMPIC ZURAMPIC is a URAT1 inhibitor indicated in combination with an XOI for the treatment of hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with an XOI alone. |
最新下载推荐下载
下载排行
|
中国新特药网-第一时间提供全球医药资讯
注： 本站药品信息仅供医药研发机构作参考-
在线咨询：
- 鲁ICP备05035203号 @