药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(20116218431118.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文卢非酰胺处方资料(仅供参考)
抗癫痫药卢非酰胺(rufinamide) 介绍 瑞士诺华公司开发的卢非酰胺(rufinamide,商品名为 Banzel)于2008年11月获得FDA批准在美国上市,用于癫痫Lennox-Gastaut综合征(LGS)的辅助治疗。卢非酰胺的中文化学名称: 1-(2, 6-二氟苯甲基)-1H-1, 2, 3-三唑-4-甲酰胺;英文化学名称: 1-[(2, 6-difluoroPHenyl)methyl]-1H-1, 2, 3-triazole-4-carboxamide。分子式: C10H8F2N4O;相对分子质量: 238.2; CAS登记号: 106308-44-5。
文献报道卢非酰胺的合成路线是以2, 6-二氟苯甲酸为起始原料,经酯化得到2 , 6-二氟苯甲酸乙酯, 该中间体经NaBH4还原及SOCl2卤化得取代2, 6-二氟 rufinamide(Banzel) 氯苄,再与叠氮化钠反应得2, 6-二氟苄基叠氮酸酯,该叠氮酸酯与丙炔酸乙酯环合得1-(2, 6-二氟苯甲基)-1H-1, 2, 3-三唑-4-甲酸乙酯,最后经胺解得到卢非酰胺。
卢非酰胺是一种三唑类的衍生物,其化学结构与目前已经上市的抗癫痫药物不同,它是通过调节大脑钠离子通道活性而发挥作用,当浓度大于10μmol·L-1时它对单胺类、肾上腺素、组胺、乙酰胆碱、AMPA-kainate、甘氨酸、NMDA或GABA神经递质-受体系统无明显影响。药理学研究表明,卢非酰胺能有效地拮抗数种电刺激以及化学癫痫发作模型中动物的强直相及阵挛相癫痫的发作,抑制啮齿类动物最大电休克性强直2阵挛发作的口服 ED50值为5~17 mg·kg-1,但对戊四唑诱导的发作疗效较差。临床研究表明,癫痫患者对卢非酰胺辅助治疗(由 400 mg增加至800、1 200、1 600 mg·d-1,每周口服1次) 的耐受性良好,癫痫发作次数减少,而且对治疗耐受的局部或泛发性癫痫患者仍产生作用,它对局部癫痫发作和泛发性强直2阵挛癫痫发作的治疗也有辅助作用,可联合给药或单独给药。卢非酰胺的主要不良反应为轻微神经系统症状,表现为疲惫、困倦、嗜睡及震颤。该药对卡马西平、苯妥英或丙戊酸盐的药物代谢动力学没有影响,因此,在与其他抗癫痫药合用时不必调整卢非酰胺的剂量。
卢非酰胺的化合物专利有WO 9802423、CN 1225087、 EP 199262。同时,卢非酰胺也是欧盟批准的首个专门治疗LGS的药物。除癫痫外,卢非酰胺还正在进行针对焦虑症、双向情感障碍和神经研究。
据WHO统计,目前全球共有癫痫患者约5 000万人, 每年还出现200 万新的癫痫患者。我国癫痫患病率为 7‰,与WHO报告的发展中国家712‰的发病率接近。目前全球抗癫痫药市场总值为80亿美元,近几年来,世界抗癫痫药物市场份额平均年增长率为10% ,因此卢非酰胺作为抗癫痫药在我国有着巨大的市场前景。
IMPORTANT SAFETY INFORMATION There are risks associated with the use of BANZEL that you should know about. We encourage you to talk to your healthcare provider about these risks.
Patients with a history of Familial Short QT syndrome should not be treated with BANZEL. Talk to your healthcare provider if you are unsure if this affects you or your loved one. BANZEL has been shown to reduce the QT interval. Caution should be used when administering BANZEL with other drugs that shorten the QT interval. All medications to treat seizures, including BANZEL, may cause suicidal thoughts or actions in a very small number of people, about 1 in 500. Call your healthcare provider right away if you or your loved one experiences new or worsening symptoms of depression, unusual changes in mood or behavior, thoughts or actions about suicide or self-harm, aggression, agitation, anger, anxiety, or irritability. Use of BANZEL has been associated with side effects such as sleepiness or feeling tired, difficulty with coordination, dizziness, and problems with walking or movement. –Alcohol, in combination with BANZEL, may increase or worsen these side effects. Call your healthcare provider if you or your loved one experiences a rash. This can be a sign of a more serious condition, such as multi-organ hypersensitivity reaction. You or your loved one should take BANZEL only as prescribed. Do not stop taking BANZEL without first talking to your healthcare provider. Stopping BANZEL suddenly can cause serious problems. Tell your healthcare provider about all the medications you or your loved one takes, including prescription and non-prescription medications, vitamins, and herbal supplements. Using BANZEL with certain medications can affect each other, causing side effects. In studies, the most commonly observed (≥10%) side effects with BANZEL vs placebo (sugar pill with no medicine in it), respectively, were headache (25% vs 20%), dizziness (17% vs 10%), feeling tired (15% vs 9%), sleepiness (13% vs 9%), and nausea (11% vs 7%).
Please read the full Prescribing Information and discuss it with your doctor or healthcare professional.
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