1、 膽堿受體激動(dòng)藥 易逆性膽堿酯酶抑制藥 抗膽堿酯酶藥 難逆性膽堿酯酶抑制藥 擬膽堿藥擬膽堿藥膽堿受體激動(dòng)藥膽堿受體激動(dòng)藥cholinoceptor agonists是指可與膽堿受體結(jié)合并能激動(dòng)該受體，是指可與膽堿受體結(jié)合并能激動(dòng)該受體，產(chǎn)生與遞質(zhì)乙酰膽堿作用類似的藥物。產(chǎn)生與遞質(zhì)乙酰膽堿作用類似的藥物。膽堿酯酶抑制藥膽堿酯酶抑制藥(Anticholinesterase drug)是指經(jīng)過抑制膽堿酯酶的活性，使乙酰膽是指經(jīng)過抑制膽堿酯酶的活性，使乙酰膽堿破壞減少，在突觸間隙大量堆積而激動(dòng)堿破壞減少，在突觸間隙大量堆積而激動(dòng)膽堿受體的藥物。膽堿受體的藥物。膽堿受體激動(dòng)藥分類：膽堿受體激動(dòng)藥分類：M

2、，N受體激動(dòng)藥，如氨甲酰膽受體激動(dòng)藥，如氨甲酰膽堿；堿；M受體激動(dòng)藥，如毛果蕓香堿；受體激動(dòng)藥，如毛果蕓香堿；N受體激動(dòng)藥，如煙堿，作用復(fù)受體激動(dòng)藥，如煙堿，作用復(fù)雜，無臨床運(yùn)用價(jià)值。雜，無臨床運(yùn)用價(jià)值。生生M樣作用。對眼睛和腺體的作用樣作用。對眼睛和腺體的作用明顯，明顯，對心血管的影響小。對心血管的影響小。 1. 1.對眼睛的作用對眼睛的作用 (1)(1)縮瞳縮瞳 興奮瞳孔括約肌細(xì)胞膜上的興奮瞳孔括約肌細(xì)胞膜上的M M受體，受體，使瞳孔括約肌收縮，瞳孔減少。使瞳孔括約肌收縮，瞳孔減少。 (2) (2)降低眼內(nèi)壓只見于眼壓高者降低眼內(nèi)壓只見于眼壓高者 房水產(chǎn)生及回流房水產(chǎn)生及回流 (3) (3

3、)調(diào)理痙攣調(diào)理痙攣 睫狀肌睫狀肌M M受體興奮受體興奮, ,睫狀肌收縮睫狀肌收縮, ,睫狀肌向眼中心部方向睫狀肌向眼中心部方向拉緊拉緊, ,懸韌帶松弛懸韌帶松弛, ,晶狀體變凸晶狀體變凸, ,屈光度增大屈光度增大, ,視近物清視近物清楚楚, ,遠(yuǎn)物模糊稱調(diào)理痙攣。遠(yuǎn)物模糊稱調(diào)理痙攣。 睫狀肌睫狀肌 懸韌帶懸韌帶 晶狀體 2.對腺體作用對腺體作用 皮下注射皮下注射1015mg毛果蕓香堿，可明顯添加汗腺、毛果蕓香堿，可明顯添加汗腺、唾液腺的分泌。唾液腺的分泌。 臨床運(yùn)用臨床運(yùn)用 1.青光眼青光眼 毛果蕓香堿是治療青光眼首選藥物。毛果蕓香堿是治療青光眼首選藥物。 特點(diǎn)：作用快、溫暖、短暫，刺激性小，

4、浸透性特點(diǎn)：作用快、溫暖、短暫，刺激性小，浸透性好。好。 青光眼青光眼閉角型閉角型(angle-closure glauconma 充血性青光眼充血性青光眼)：前房角間隙狹窄：前房角間隙狹窄(近視者近視者) 。開角型開角型(open-closure glauconma 單純性青光眼單純性青光眼)：鞏膜靜脈竇血管：鞏膜靜脈竇血管硬化老年者。硬化老年者。Mushroom Poisoning煙堿煙堿Nicotine ，尼古，尼古丁丁1. The actions of acetylcholine released from autonomic and somatic motor nerves are

5、terminated by enzymatic destruction of AchE. Its actions are mediated through nicotinic and muscarinic cholinergic receptors. These agonists typically are longer-acting congeners of acetylcholine or natural alkaloids. The clinical uses of the muscarinic receptor agonists, primarily in ophthalmology

6、and to enhance gastrointestinal and bladder tone.2. Pilocarpine is the most used drug for the treatment of glaucoma.3. Nicotine cholinoceptor agonists，nicotine stimulates the nicotinic acetylcholine receptor. NR mediates neurotransmission at the neuromuscular junction and peripheral autonomic gangli

7、a; in the central nervous system, it largely controls release of neurotransmitters from presynaptic sites.summary酶藥：酶藥：有機(jī)磷酸酯類有機(jī)磷酸酯類藥藥 Cholinesterase cleans up unused acetylcholine, by breaking it down into its components acetate and choline. Neurons which produce acetylcholine are damaged in, with t

8、he result that levels of acetylcholine fall in the brain. Cholinesterase inhibitors may be useful in Alzheimers disease patients by allowing what acetylcholine there is to survive longer and be more effective.3.陣發(fā)性室上性心動(dòng)過速陣發(fā)性室上性心動(dòng)過速 在壓迫眼球或頸動(dòng)脈竇等興奮迷走在壓迫眼球或頸動(dòng)脈竇等興奮迷走神經(jīng)措施無效時(shí)，可用新斯的明，神經(jīng)措施無效時(shí)，可用新斯的明，經(jīng)過抑制心肌上的

9、膽堿酯酶，間接經(jīng)過抑制心肌上的膽堿酯酶，間接興奮興奮M受體，使心率減慢。受體，使心率減慢。4.用于非去極化型骨骼肌松弛藥用于非去極化型骨骼肌松弛藥如筒箭毒堿和阿托品中毒時(shí)的如筒箭毒堿和阿托品中毒時(shí)的挽救。挽救。 1. Cholinesterase inhibitors are drugs that prevent (or inhibit) cholinesterase from cleaning up unused acetylcholine. neostimine2. Cholinesterase inhibitors may be useful in Alzheimers disease patients by allowing what acetylchol