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单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,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,PD,Control,Produce dopamine,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,
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