课件：神经系统药理—魏尔清抗帕金森病药.ppt

Part 10 Drugs Treating Parkinson Disease and Alzheimer Disease,Levodopa and related drugs Cholinoceptor antagonists Drugs treating dementia,Drugs for treatment of Parkinson disease (PD) Levodopa and related drugs Cholinoceptor antagonists,Parkinson disease and therapeutic drugs,Rigidity: one of the common symptoms of PD,Tremor: one of the common symptoms of PD,Pyramidal and extrapyramidal pathways,Striatum,黑质-纹状体通路,中脑-皮层通路,结节-漏斗通路,Substantia nigro -striatum dopaminergic pathway is involved in PD pathogenesis,Parkinson disease Dopaminergic neuron degeneration in substantia nigro and striatum,Normal,Dopamine,Acetylcholine,Abnormal balance of DA/ACh neuronal functions in extrapyramidal system of Parkinson disease,Levodopa,Muscarinic antagonists,Normal,Parkinson disease,(-),(-),injured,relatively potentiated,PD: GABA ,HD: GABA ,(+),(-),(-),(+),(-) ,(-) ,(-) ,Levodopa and related drugs,Levodopa, L-dopa 左旋多巴,Drugs for treatment of Parkinson disease,Levodopa,Dopamine,Levodopa 1. ADME Penetrating into the brain, transformed to DA or NE (less) Distributed in peripheral tissue (most) 2. Effects and uses Parkinson disease: decreases the rigidity, tremors, and other symptoms 3. Adverse effects (1) CNS: abnormal involuntary; hallucinations; etc. (2) GI: nausea, vomiting, etc. (3) CVS: hypotension, arrhythmia, etc.,Drugs for treatment of Parkinson disease,Inhibitors of aromatic L-amino acid decarboxylase Carbidopa 卡比多巴 can not cross BBB, but can inhibit peripheral dopamine synthesis. increases availability of levodopa to the CNS and decreases peripheral effects,Drugs for treatment of Parkinson disease,Levodopa alone,Levodopa + Carbidopa,Other drugs 1. DA receptor agonists Bromocriptine 溴隐亭 Pergolide 培高利特 Pramiperole 普拉克索 Ropinirole 罗平尼咯,Drugs for treatment of Parkinson disease,2. MAO inhibitors decreasing DA metabolism in the CNS Selegiline 司来吉兰 Rasagiline 雷沙吉兰 3. COMT inhibitors decreasing DA metabolism in the CNS Nitecapone 硝替卡朋 4. Amantadine 金刚烷胺 increasing DA release,Drugs for treatment of Parkinson disease,Muscarinic antagonists Trihexyphenidyl （苯海索，artane, 安坦） Decreasing CNS cholinergic functions Adjuvant of Parkison disease treatment,Drugs for treatment of Parkinson disease,Drugs for treatment of dementia (Alzheimer and related diseases) Anticholinesterase drugs Cholinoceptor agonists Neurotrophic factor-like drugs,Anticholinesterase drugs Tarcrine 他克林 Huperzine 石杉碱甲（哈伯因） Galantamine 加兰他敏 Cholinoceptor agonists Xanomeline 占诺美林 Milameline 米拉美林 Neurotrophic factor-like drugs AIT 082 Propentofylline 丙戊茶碱,Drugs for treatment of dementia,Pathological characteristics of AD,Atrophy of the brain,Senile plaques Neurofibrillary tangles,Senile plaques and neurofibrillary tangles,Regions related to neuronal injury,Importance of ACh system,淀粉样多肽（A）形成,淀粉样多肽细胞外蓄积,tau蛋白细胞内蓄积,神经元功能损伤，神经变性,痴呆发生,炎症反应，氧自由基产生 钙平衡失调，细胞功能紊乱,遗传异常，环境影响,后面内容直接删除就行 资料可以编辑修改使用 资料可以编辑修改使用 资料仅供参