英文药名：RILUTEK/RILUZOLE TABLETS（Riluzole） 中文药名：利鲁唑片 生产厂家：赛诺菲公司和大东公司 リルテック錠50 リルゾール錠50mg「AA」 利鲁唑片（RILUTEK/RILUZOLE TABLETS）—是一种治疗肌萎缩侧索硬化(ALS)安全、高效药物 治疗类别名称 肌萎缩侧索硬化用剤 批准日期： 1：赛诺菲 1995年12月 2：大东    2014年2月 商標名 RILUTEK RILUZOLE TABLETS 一般名 リルゾール（Riluzole） 化学名 2-Amino-6-(trifluoromethoxy)benzothiazole 分子式 C8H5F3N2OS 分子量 234.20 構造式 性　状 本产品为晶体细小的黄色粉白色。 产物N，N-二甲基甲酰胺，是在甲醇或乙腈，乙醇（95）或在水中易溶于乙醚，极微溶于非常可溶的。 本产品可溶于0.1mol / L的盐酸试液。 此产品不溶于稀氢氧化钠TS。 熔点 117〜120℃ 药效药理 1. 薬理作用 (1)与ALS病理学相关测试 1)在使用培养的大鼠皮质神经元在体外研究中，利鲁唑已显示抑制神经元细胞死亡，由于暴露于脑脊液ALS患者。 2)如家族性ALS的致病基因中的一个，在超氧化物歧化酶（SOD1）突变也已确定。转基因小鼠过量表达突变人类SOD1基因的利鲁唑延长生存。 (2)神经细胞保护作用 1)在使用培养的大鼠脊髓运动神经元，利鲁唑抑制神经元细胞死亡由谷氨酸和谷氨酸摄取抑制剂在体外研究 2)在使用大鼠海马切片的体外研究，通过利鲁唑NMDA（N-甲基-D-天门冬氨酸）或兴奋性氨基酸受体激动剂的电压门控的Na +通道激动剂的藜芦碱抑制神经元细胞死亡。 2. 作用机序 本剤的作用机制尚未完全阐明，各种体外，在体内，谷氨酸释放的抑制作用，兴奋性氨基酸受体的非竞争性抑制，抑制电压门控Na +通道的一个测试具有同等的效果，可以认为它们是单独或合并来表达神经细胞保护作用。 适应病症 治疗肌萎缩侧索硬化症（ALS） 肌萎缩侧索硬化症的疾病活动进步抑制（ALS） 用法与用量 成人，用于口服给药的每日2次（早，晚餐前），1日剂量为100mg（主剂2片）。 包装规格（利鲁唑片：注：以下产品不同厂家不同使用，使用时请以原处方资料为准） 片剂[赛诺菲（リルテック錠）商品名：RILUTEK]：50mg 28片[14片剂（PTP）×2] 56粒[14片剂（PTP）×4] 生产和销售 赛诺菲公司 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/1190011F1021_1_15/ 片剂[大东（リルゾール錠）商品名：RILUZOLE]：50mg 50毫克「AA」：56片（14片×4） 生产和销售 大东有限公司[销售]武田薬品 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/1190011F1030_1_05/ Riluzole(also known as Rilutek®RILUZOLE, PK-26124, RP-54274) is a neuroprotective and anticonvulsant drug that can be used to treat amyotrophic lateral sclerosis (AlS), enabling patients to survive Extended for 3-5 months under the trade name Rilutek, RILUZOLE. Roxuzole blocks tetrodotoxin-sensitive (TTX-S) and tetrodotoxin-resistant (TTX-R) sodium channels in the dorsal root ganglion neurons of rats, but has a stronger effect on TTX-S sodium channels. Name of drug classification Agent for amyotrophic lateral sclerosis Sales name Riltec tablet 50 common name Riluzole Chemical name 2-Amino-6- (trifluoromethoxy) benzothiazole Molecular formula C8H5F3N2OS Molecular weight 234.20 Property This product is white to slightly yellow crystalline powder. This product is very soluble in N, N-dimethylformamide, methanol or acetonitrile, is easily soluble in ethanol (95) or diethyl ether, and is very insoluble in water. This product dissolves in 0.1 mol / L hydrochloric acid reagent solution. This product is insoluble in dilute sodium hydroxide solution. Melting point 117 ~ 120 ℃ composition Active ingredient (in 1 tablet) Riluzole 50 mg Additive Anhydrous calcium hydrogen phosphate, crystalline cellulose, croscarmellose sodium, light anhydrous silicic acid, magnesium stearate, hypromellose, macrogol, titanium oxide Contraindications Patients with serious liver dysfunction [see 1. Careful Administration, 2. Important Basic Precautions "and" 4. Side Effects "] Patients with a history of hypersensitivity to this drug or the ingredients of this drug Pregnant women or patients who may be pregnant [see 6. Administration to pregnant women, maternity women, lactating women etc.] Indication or effect Treatment of amyotrophic lateral sclerosis (ALS) Suppression of disease progression in amyotrophic lateral sclerosis (ALS) Usually for adults, take 1 tablet once a day, twice daily (before morning and dinner), orally as a riluzole 100 mg daily dose (2 tablets). Careful Administration Patient with a history of liver dysfunction or patient with liver dysfunction [This product is mainly metabolized by the liver, which may deteriorate liver function] Patients with fever and suspected of infection [neutropenia may occur] Patients with impaired renal function [safety is not established] Serious side effects Anaphylactoid symptoms Frequency unknown ※ Anaphylactoid symptoms may occur, so observe thoroughly and if abnormalities such as angioedema, dyspnea, wheezing, sweating etc. are observed, administration should be stopped and appropriate measures should be taken. Neutropenia Less than 0.1% Because there is a report of severe neutropenia, if white blood cell count is measured immediately when fever is observed, administration should be discontinued if neutropenia is observed. Interstitial pneumonia 0.1% As interstitial pneumonia may appear, if respiratory symptoms such as fever, cough, respiratory distress, etc. appear, immediately perform chest x - ray and other appropriate measures. Liver dysfunction 0.3% Liver dysfunction accompanied by marked elevation of AST (GOT), ALT (GPT), γ-GTP, Al-P etc., jaundice may appear, so observe thoroughly and if abnormality is found, Take appropriate measures such as discontinue. Medicinal pharmacology Pharmacological action Examination related to ALS pathology In vitro studies using cultured rat cerebral cortical neurons demonstrated that riluzole inhibits nerve cell death by exposure to cerebrospinal fluid of ALS patients. Mutation of superoxide dismutase (SOD1) has been identified as one of the causative genes of familial ALS. Riluzole extended the survival time of transgenic mice overexpressing mutant human SOD1 gene. Neuroprotective action Riluzole inhibited nerve cell death by glutamate and glutamate uptake inhibitors in in vitro studies using cultured rat spinal motor neurons. Riluzole inhibited nerve cell death by excitatory amino acid receptor agonist NMDA (N-methyl-D-aspartic acid) or voltage-dependent Na + channel agonist Veratridine in an in vitro test using rat brain hippocampal slices. Mechanism of action Although the mechanism of action of this drug is not completely elucidated, in various in vitro and in vivo tests, inhibition of glutamate release, noncompetitive inhibition with excitatory amino acid receptor, inhibition of voltage-dependent Na + channel It is considered that these compounds alone or in combination produce a neuronal cell protective effect.