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抗帕金森病药课件(2)

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抗帕金森病药课件 抗帕金森病药 抗帕金森病药PPT 抗帕金森病药物PPT 抗帕金森病药物
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With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 第十七章 治疗中枢神经系统 退行性疾病药 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 中枢神经系统退行性疾病 帕金森病、阿尔茨海默病、 亨廷顿病、肌萎缩侧索硬化 症等. 共同病理:脑或(和)脊 髓神经元退行性变、脱失. With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 典型的症状为: 静止震颤 肌肉强直 运动障碍 共济失调 第一节 抗帕金森病药 帕金森病(PD)震颤麻痹 是锥体外系功能紊乱引起的一种 慢性中枢神经系统退行性疾病。 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 总称为帕金森综合征(Parkinsonism) 分型:根据病因分为 原发性:即帕金森病; 继发性:动脉硬化、脑炎后遗症、 化学药物中毒引起, 均出现类似原发性帕金森病的症状 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society PD是因纹状体内DA减少或缺 乏所致.原发因素是黑质内多 巴胺能神经元退行性病变。 帕金森病的病因 ---多巴胺学说 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 黑质多巴胺能神经元发出上行纤维到达纹状 体,其功能在于抑制纹状体内Ach递质系统 的功能。 黑质-纹状体多巴胺能神经通路 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 发病机制发病机制 黑质多巴胺神经元变性, 多巴胺能神经功能减弱,而胆碱 能神经功能亢进。产生帕金森病 的肌张力增高症状。 药物治疗 拟多巴胺类药:左旋多巴 抗胆碱药:苯海索 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 一.拟多巴胺类药 药物包括: 多巴胺前体药(左旋多巴) 左旋多巴的增效药(卡比多巴等) 多巴胺受体激动药(溴隐亭) 促多巴胺释放药(金刚烷胺) With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 药物包括: 多巴胺前体药(左旋多巴) 左旋多巴的增效药(卡比多巴等) 多巴胺受体激动药(溴隐亭) 促多巴胺释放药(金刚烷胺) With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 左旋多巴(levodopa,L-dopa) ㈠ 多巴胺前体药 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 口服在小肠迅速吸收 【体内过程】 绝大部分被肠粘膜等外周组 织的L-芳香氨基酸脱羧酶脱 羧成为DA,引起不良反应. 进人脑内仅1%左右转变为多巴胺 合用外周脱羧酶抑制剂卡比多巴 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society【药理作用及临床应用】 治疗帕金森病 对大多数帕金森病患者具有 显著疗效,(1)轻症及年轻患者疗 效好;(2) 肌肉僵直和运动困难的患者 疗效较好; • 注意: 对吩噻嗪类等抗精神病药所引 起的帕金森综合征无效。因吩噻嗪类 药物阻断中枢多巴胺受体,使多巴胺 无法发挥作用 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society (1) 胃肠道反应: 厌食、恶心、 呕吐. 与外周脱羧酶抑制剂同服,反应 明显减少. D2受体阻断药多潘立酮可治疗. 【不良反应】 1.早期反应 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 轻度体位性低血压,心动过速 或心律失常. 外周形成的DA:(1)作用于交 感神经末梢,反馈性抑制NE释 放(2)作用于血管壁的DA受体 。 (2)心血管反应 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 服用大量L-DOPA后,多巴胺受 体过度兴奋,出现手足、躯体和 舌的不自主运动 . 2.长期反应 (1)运动过多症 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 服药3-5年后4080%病人出现, 重则出现“开-关反应”。“开 ”时活动正常或接近正常,“关 ”时出现严重PD症状. (2)症状波动: 出现“开-关现 象” With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society (3) 精神障碍 失眠、焦虑、恶梦、狂躁、 幻觉、妄想、抑郁等。 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society (1)VB6是多巴脱羧酶的辅基,可增 强左旋多巴的外周副作用,降低疗 效. (2) 抗精神病药能引起帕金森综合征, 又能阻断中枢多巴胺受体,所以能对 抗左旋多巴的疗效。 【药物相互作用】 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 卡比多巴(carbidopa) α-甲基多巴肼 有两种异构体,其左旋体称卡比多巴 . ㈡ 左旋多巴的增效药 1 氨基酸脱羧酶抑制药 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 可减少左旋多巴在外周组织的 脱羧作用,使较多的左旋多巴到 达黑质—纹状体发挥作用,从而 提高左旋多巴的疗效. 抑制左旋多巴在外周生成多巴胺而 减少了它的外周不良反应 是左旋多巴的重要辅助药 与左旋多巴合用 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 两药合用的优点如下 ①减少左旋多巴的用量75%; ②明显减少左旋多巴的不良反应; 复方制剂心宁美 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society A A:单独应用:单独应用L-dopaL-dopaB B::L-dopaL-dopa与与carbidopacarbidopa合用合用 用法用法: : carbidopacarbidopa与与levodopalevodopa之比之比 1:10 1:10合剂:心宁美(合剂:心宁美(sinemetsinemet)) With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 苄丝肼(benserazide) 与卡比多巴有同样的效应, 它与左旋多巴按1:4制成的复 方制剂称美多巴(madopar),应用 于临床. With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 3 COMT抑制药 降低L-DOPA降解. 硝替卡朋 2 MAO-B抑制药 MAO-B主要分布于黑质-纹状体, 降解DA 司来吉兰 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 选择性抑制中枢神经系统MAO-B, 降低脑内DA降解,DA浓度↑. 与L-DOPA合用,疗效↑, L-DOPA 用量↓,外周副作用↓. 能抑制自由基形成,延迟神经元变 性和PD发展.帕金森病辅助治疗药. 司来吉兰(selegiline) With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society ㈢ 多巴胺受体激动药 溴隐亭(bromocriptine) --- ---D2D2受体激动剂受体激动剂 激动垂体激动垂体D D 2 2 受体受体→→催乳素、生长激素催乳素、生长激素↓↓ 用于治疗泌乳闭经综合征、肢端肥大症用于治疗泌乳闭经综合征、肢端肥大症 增加剂量激动黑质纹状体增加剂量激动黑质纹状体D2D2受体受体→→改善改善 帕金森病症状帕金森病症状. . 帕金森病(用于帕金森病(用于L-L-多巴不能耐受或效果多巴不能耐受或效果 不佳者)不佳者). .不良反应较多,与不良反应较多,与L-DOPAL-DOPA类似类似. . With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society ㈣ 促多巴胺释放药 金刚烷胺(amantadine) 通过多种方式加强DA功能(1)促 进L-DOPA进入脑;(2)增加DA合成 、释放和减少DA重摄取;(3)激动 DA受体. With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 苯海索(trihexyphenidyl) --安坦 作用机理 阻断中枢M胆碱受体,减弱 纹状体中乙酰胆碱的作用。 二. 抗胆碱药 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 临床应用 轻症患者效果好; 不能耐受左旋多巴或禁用左旋多巴的 患者; 治疗抗精神病药引起的帕金森综合 征有效; 与左旋多巴合用,可使50%患者症 状得到进一步改善. With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 第二节 治疗阿尔茨海默病药 老年性痴呆症 原发性痴呆症(阿尔茨海默病,AD) 血管性痴呆症(VD)。血管性痴呆 症是由脑血管病变引起的脑功能衰 退的结果。 With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society 胆碱酯酶抑制药 他克林(tacrine) [作用机制] (1)可逆性抑制ChE (2)激动M和N受体 (3)增加脑组织对糖的利用. 与卵磷脂合用治疗AD, 肝毒性大, 现较少用. 与卵磷脂合用,延缓病程. With the improving quality of life as well as the ever-accelerating pace of life, the quality of people's food needs and rate also changing.In order to meet the needs of society M受体激动药 • 占诺美林 • M1受体激动药
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