Therapeutic application of achEIs Indirect acting cholinergic agonists Treatment of myasthenia gravis(重症肌无力), atony(弛缓 ) in the gastrointestinal tract and glaucoma(青光眼) Investigational therapy for alzheimer's disease Agricultural insecticides and nerve gas warfare agents
Therapeutic Application of AChEIs • Treatment of myasthenia gravis (重症肌无力), atony （弛缓 ） in the gastrointestinal tract and glaucoma （青光眼）. • Investigational therapy for Alzheimer’s disease • Agricultural insecticides and nerve gas warfare agents. • Indirect acting cholinergic agonists
Reversible aches Classical acheIs CH CH3NH O O、N(cH3)z 0、N(cH3)2 H3 CH3 N(CH3)3 Br Physostigmine Neostigmine bromide Pyridostigmine bromide 毒扁豆碱 溴新斯的明 溴吡斯的明 Nonclassical AchEIs CH3o CH H2 CH3o HCI CH3 Tacrine 他克林 Donepezil (Aricept) Rivastigmine(Exelon) 多奈嘛齐 巴拉汀
Reversible AChEIs N NH2 Tacrine 他克林 O CH2 CH3O CH3O N CH2 HCl Donepezil (Aricept) 多奈哌齐 O N N H3C CH3 CH3 O CH3 CH3 Rivastigmine (Exelon) 卡巴拉汀 • Classical AChEIs • Nonclassical AChEIs
Neostigmine bromide(溴新斯的明) 3O、N(CH3)2 N(CH3)3 Br 3-L[[(Dimethylamino carbonylJoxyI-N,N,N trimethylbenzenaminium bromide
Neostigmine Bromide （溴新斯的明） 3-[[[(Dimethylamino)carbonyl]oxy]-N,N,Ntrimethylbenzenaminium bromide
Actions and uses Chemically more stable than physostigmine(毒扁 豆碱) Longer duration of action Administered orally orⅳ The most frequent use of neostigmine is to prevent atony(张力迟缓) of the intestinal, skeleta,and bladder musculature. Also used as urinary stimulant
Actions and Uses • Chemically more stable than physostigmine （毒扁 豆碱） • Longer duration of action • Administered orally or iv • The most frequent use of neostigmine is to prevent atony (张力迟缓) of the intestinal, skeletal, and bladder musculature. Also used as urinary stimulant
Tacrine(他克林) Potent centrally acting achE inhibitor FDA approved for the treatment of NH 2 Alzheimer's disease (To increase ACh levels in the brain Side Effects: Hepatotoxicity Abdominal cramping(腹部绞痛)
Tacrine（他克林） •Potent centrally acting AChE inhibitor • FDA approved for the treatment of Alzheimer’s Disease (To increase ACh levels in the brain) • Side Effects: Hepatotoxicity; Abdominal cramping （腹部绞痛）