英文药名: Rilutek(Riluzole Tablets) 中文药名: 力如太 (利鲁唑片) 生产厂家: Aventis 药品介绍 利鲁唑为苯噻唑类化合物,通过抑制脑内神经递质的释放，抑制兴奋性氨基酸的活性及稳定电压依赖性钠通道的失活状态来表现其神经保护作用，可减少兴奋性递质的毒性作用，增加细胞的存活率,对阿尔茨海默病、帕金森病、脑卒中或脑损伤等神经伤害或退行性疾病均有明显疗效。 药品名称 [商品名] Rilutek，力如太, 利鲁唑 [别名] pk-26124, Rp-54274 [类别] 运动神经元疾病治疗药，谷氨酸盐拮抗剂. 药理作用 肌萎缩性侧索硬化症（ALS）或运动神经元疾病是一种渐进的致命性疾病。该病有两种发病形式：肢体发病或延髓发病。两者均表现为上、下运动神经元丧失，导致渐进性和不可逆性的肌肉消瘦和无力。尽管该病发病机理尚未完全弄清，但谷氨酸毒性是神经元损伤的一种可能原因。因此目前已将能调节中枢神经系统中谷氨酸水平的药物作为可行性疗法。 苯并噻唑类药物利鲁唑就是这类抗谷氨酸药物，其神经保护作用机理复杂，涉及几个不同过程。已经知道的是它能抑制谷氨酸在突触前释放并能与受体结合防止谷氨酸的激活。本品也可使神经末梢及细胞体上的电位依赖性钠通道失活，刺激依赖G蛋白的信号传导过程。 在体外，本品能保护所培养的运动神经元免受谷氨酸激活的毒性影响，并防止ALS病人因缺氧或暴露于CSF中的毒性因素而导致的神经元死亡。在脊柱运动神经元变性的小鼠模型中，本品能改善其可动性。 药代动力学 口服给药后，本品能被迅速吸收，给药60-90min内达到血药浓度峰值。约90%的药物被吸收，绝对生物利用度为60%。本品经肝代谢，主要随尿排出，消除半衰期为9-15h。 临床研究 在最初的一项包括155例ALS患者的双盲研究中，本品治疗组病人12个月生存率为74%，而安慰剂组为58%。此外，延髓发病病人的1年生存率，本品与安慰剂组分别为73%和35%，而肢体发病病人的1年生存两者分别为74%和64%。研究还证实，经本品治疗的病人其肌肉减退明显较慢。 在第二项包括959例ALS病人的多中心双盲试验中，又一次证明本品治疗生存率明显较高（57%对50%）。但治疗18个月后肢体发病亚组与延髓发病亚组间或在肌肉测试中未发现有显著差异。 考虑到研究中ALS病人生存结果有较大差异，为对这些结果作进一步评价，还要使用cox模型（补偿已知的预后因素）。该模型证实治疗18个月后治疗组病人死亡危险率降低了35%。 适应症 本品适用于肌萎缩性侧索硬化症的治疗，延长生命或机械换气时间。但不适用于其他形式的运动神经元疾病。 用法用量 成人每日2次，每次1片；儿童不推荐使用。任何疑问, 请遵医嘱! 不良反应 最常见的不良反应是乏力、恶心、头痛、腹痛、呕吐、肝功能指标升高、头晕、心动过速、嗜睡、口周感觉错乱。 注意事项 （1）在专家指导下开始治疗； （2）伴严重肝病的患者，妊娠期及哺乳期妇女禁用，肾功能不全者慎用； （3）轻、中度肝病患者在治疗前及治疗期间要监测血清转氨酶值，若转氨酶水平升高至正常值的5倍时，需中止治疗； （4）提醒病人报告因轻微的中性粒细胞减少所致的发热性疾病。 制剂规格 片剂，50mg。 完整资料附件：http://www.drugs.com/pro/rilutek.html Product Description This page contains drug information on Rilutek. The information provided includes the following: what is Rilutek the possible side effects of Rilutek what happens if you miss a dose of Rilutek what happens if you overdose with Rilutek the most important information about Rilutek how to use Rilutek other drugs that may affect Rilutek what to avoid while using Rilutek Generic Name: riluzole (RILL you zole) Brand Names: Rilutek What is the most important information I should know about rilutek? •  Rarely, rilutek may cause serious blood problems. Notify your doctor immediately if you develop a fever, chills or other signs of infection which may be an early sign of potential blood problems. •  Use caution when driving, operating machinery, or performing other hazardous activities. rilutek may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities. •  Use alcohol with caution while taking rilutek. Alcohol may increase the risk of liver problems caused by rilutek. What is rilutek? •  rilutek affects muscles and nerves in the body. The exact way that it works is unknown. •  rilutek is used to treat amyotrophic lateral sclerosis, also known as ALS and Lou Gehrigs disease. •  rilutek may also be used for purposes other than those listed in this medication guide. What should I discuss with my healthcare provider before taking rilutek? •  Before taking this medication, tell your doctor if you · have liver disease or · have kidney disease. •  You may not be able to take rilutek, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above. •  rilutek is in the FDA pregnancy category C. This means that it is not known whether rilutek will be harmful to an unborn baby. Do not take rilutek without first talking to your doctor if you are pregnant or could become pregnant during treatment. •  It is not known whether rilutek passes into breast milk. Do not take rilutek without first talking to your doctor if you are breast-feeding a baby. How should I take rilutek? •  Take rilutek exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you. •  Take each dose with a full glass of water. •  rilutek should be taken at least an hour before or two hours after a meal. •  rilutek is usually taken twice a day, every twelve hours. It should be taken at the same time each day. •  Your doctor may want you to have blood tests during treatment with rilutek. It is important for your doctor to know how much rilutek is in the blood and how well the liver is working. •  Store rilutek at room temperature away from moisture, heat, and bright light. What happens if I miss a dose? •  If you miss a dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication. What happens if I overdose? •  Seek emergency medical treatment. •  Symptoms of a rilutek overdose have not been reported. What should I avoid while taking rilutek? •  Use caution when driving, operating machinery, or performing other hazardous activities. rilutek may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities. •  Use alcohol cautiously while taking rilutek. Alcohol may increase the risk of liver problems caused by rilutek. What are the possible side effects of rilutek? •  If you experience any of the following serious side effects, contact your doctor immediately or seek emergency medical attention: · an allergic reaction (difficulty breathing closing of the throat swelling of the lips, tongue, or face or hives) · a fever, chills or other signs of infection or · liver problems (yellowing of the skin or eyes, nausea, abdominal pain or discomfort, severe fatigue). •  Other, less serious side effects may be more likely to occur. Continue to take rilutek and talk to your doctor if you experience · weakness · drowsiness · dizziness or · nausea, vomiting, diarrhea, constipation or decreased appetite.  •  Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. What other drugs will affect rilutek? •  Before taking this medication, tell your doctor if you are taking any of the following medicines: · theophylline (Theo-Dur, Slo-Bid, Elixophyllin, Bronkodyl, Aerolate, Slo-Phyllin, Theovent, Theoclear, Uniphyl, Uni-Dur, Respbid,), and many others · allopurinol (Lopurin, Zyloprim) · methyldopa (Aldomet) · sulfasalazine (Azulfidine) · omeprazole (Prilosec) · amitriptyline (Elavil, Endep, others) · caffeine-containing products · fluoroquinolone antibiotics, such as ciprofloxacin (Cipro), ofloxacin (Floxin), lomefloxacin (Maxaquin), or norfloxacin (Norflex) or · rifampin (Rifadin, Rimactane). •  Drugs other than those listed here may also interact with rilutek. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including herbal products.