11.抗帕金森药物——山东大学药理学英文课件.ppt

DA-R agonists Lisuride（利修来得）：stronger than Bromocriptine Pergolide(培高利特)：stronger than Lisuride Ropinirole（罗匹尼罗）和pramipexole（普拉克索） 1.only agonist on D2 receptor ， no effect on D1 2.on-off response is few Apomorphine（阿扑吗啡） Drugs enhancing DA release Amantadine(金刚烷胺) 1.↑release DA from dopaminergic terminals. 2.↓reuptake of DA. 3. dopamine receptor agonism Clinical Uses Parkinson’s disease, less effective than levodopa, and more effective than anticholinergic agents. Onset rapidly; synergised by L-dopa. II.Central Anticholinergic Drugs Actions Blocking the M-R ,↓cholinergic neurons in the nigrostriatal. Trihexyphenidyl(苯海索) Benzatropine(苯扎托品) Improve the tremor and rigidity of PD, little effect on bradykinesia. Drug Therapy in  Alzheimer’s Disease Alzheimer’s disease（AD） 3/4 Vascular dementia（VD） 1/4 Dr.Alois Alzheimer, a German doctor, diagnosed Alzheimer’s disease in 1906 Incidence 65y 5.0% 75y 19% 85y 47% 95y 90% Course of disease: 3~20y International Symposium for Alzheimer’s Disease 2000 “If the effective methods for AD treatment is not found, the AD patients will be 22 000 000 in 2025; 45 000 000 in 2050 in whole world.” Clinical Features Dementia, cognition dysufficiency, memory damage Pathological Features Brain atrophy (脑萎缩) Senile plaque (SP, 老年斑) Neurofibrillary tangles (NFT, 神经元纤维缠结) Selective death of neuron. Pathological Features 1.Neuron toxication of amyloidβ-protein(Aβ) 。 Aβ cholinergic function AchE Aβ Pathological Features 2.Neurotransmittor activity Ach and Glu Cholinergic neurons regress Therapy for AD 1.Potentiate cholinergic function :AChEI、M-R agonists 2.Potentiator of neuronal nutrition factor and neuron cell growth factor 3. brain metabolism activator