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1、Cholinoceptor-activating drug,Cholinoceptor-activating drug,Acetylcholine receptor stimulants Cholinesterase inhibitors Mimic acetylocholine,Acetylcholine receptor stimulants,Classified by their spectrum of action depending on the receptor type Activate muscarinic receptor Activate nicotinic recepto
2、r,Muscarinic receptor stimulants,Choline esters: acetylcholine, methacholine, carbachol, bethanechol Alkaloid: pilocarpine, arecoline,Acetylcholine,Cardiovascular system: Vessel: dilation via EDRF Negative chronotropic effect Negative dromotropic effect Negative inotropic effect,Acetylcholine,Gastro
3、intestinal tract: increase motility, stimulate secretion Urinary bladder: detrusor contraction, trigone and sphincter relaxation Glands: stimulate secretion Eye: contract sphincter muscle of iris, contract ciliary muscle for near vision,Acetylcholine,A large dose of Ach after administration of atrop
4、ine can activate nicotinic receptor N1: ganglion N2: neuromuscular junction,Activate NN receptor,All ganglion are activated Sympathetic effects: increase in blood pressure Parasympathetic effects: glands secret, contract smooth muscle excite adrenal gland medulla Overdose: excitement inhibition,Acti
5、vate Nm receptor,Neuromuscular end plate Skeletal muscle Contraction,methacholine,Selectively activate muscarinic receptor Stronger effects on cardiovascular system Clinical uses: sjogrens syndrome Asthma, ulcer, anoxemia,others,Carbachol: pharmacodynamics is similar to Ach, uses for glaucoma Bethan
6、echol: more selective to M receptor,Alkaloid,Including pilocarpine, arecoline, muscarine, oxotremorine,pilocarpine,Pharmacodynamics: Eye: miosis, ocular pressure reduction, accommodation Glands: secretion,（动眼神经的胆碱能神经支配）,毛果芸香碱激动,瞳孔括约肌 缩瞳,阿托品阻断,瞳孔开大肌 扩瞳,（去甲状腺素能神经支配）,虹膜(包括瞳孔括约肌和瞳孔开大肌 ),毛果芸香碱的缩瞳作用,受体,M受
7、体,狭窄时眼内压增高，闭角型青光眼（急，慢型充血性青光眼）,变性或硬化时眼内压增高 开角性青光眼（慢性单纯性青光眼）,睫状体上皮 细胞分泌,血管渗出,房水 瞳孔,前房,前房角间隙,小梁网,巩膜静脉窦,血流,毛果芸香碱的降低眼内压作用,间隙扩大,房水入循环,毛果芸香碱收缩瞳孔括约肌,缩瞳虹膜拉紧,虹膜根部变薄,毛果芸香碱,收缩睫状肌 扩张小血管,阿托品扩瞳，虹膜退向四周，前房角 间隙变窄，房水回流受阻，眼内压升高,降低眼内压,正常时晶体较扁平,受睫状肌控制,环状肌,辐射状肌,(瞳孔括约肌),动眼神经兴奋或毛果芸香碱,动眼神经胆碱能神经,阿托品,向瞳孔中心收缩悬韧带，睫状小带放松,睫状肌松弛而退向
8、外缘，悬韧带拉紧,(瞳孔开大肌),去甲肾上腺素能 神经支配 对眼调节无重要意义,只视近物(调节痉挛),只视远物(调节麻痹),晶状体变扁屈光度降低,晶状体变凸屈光度增加,毛果芸香碱的调节痉挛作用,外界,睫状肌起点,悬韧带,Clinical uses,Glaucoma Iritis,Muscarine,Direct acting muscarinic receptor: toxic reaction,nicotine,Contributes to increased risk of vascular disease and sudden coronary death Contributes to
9、high incidence of ulcer recurrence with peptic ulcer,Anticholinesterase agents,Acetylcholinesterase,Ach=AchE Ach- AchE choline+AcAchE Acetate+Ache The entire process takes place in 150ms,AchE,Nerve terminal, synaptic cleft, effectors Most chlinergic synapses are richly supplied with AchE, the half-l
10、ife of Ach is very short,Anticholinesterase agents,Binds to AchE complex The covalent bond is resistance to the second process, and this step is prolonged,classification,Hydration process is prolonged for 30 minutes to 6 hours Hydration process is prolonged for hundreds of hours,Anticholinesterase a
11、gents,Pharmacodynamics: Eye: miosis, ocular pressure reduction, accommodation Gastrointerase systems: contract, increase secretion,Anticholinesterase agents,Neuromuscular junction: Therapeutic concentration: prolong and intensify the actions of Ach; activate skeletal muscle directly Higher concentra
12、tion: fibrillation of muscle fibers,Anticholinesterase agents,Respiratory, urinary tract: contract Cardiovascular system: increase activation in ganglia and at acetylcholine receptors on neruoeffector cells( HR ,BP ),Anticholinesterase agents,Glands: secret CNS Low concentration: activation of EEG,
13、subjective alerting response High concentration: coma, respiratory arrest,Clinical uses,Myasthenia gravis Ileus, Glaucoma Detoxifcation Alzheimiers disease cholinergic crisis,Neostigmine,Inhibit AchE and thereby increase the concentration of endogenous Ach Act at neuromuscular junction and smooth mu
14、scle Selectively Myasthenia gravis Ileus,Pyridostigmine,Pharmacodynamics is similar to Neostigmine Take effect slowly Myasthenia gravis Ileus,physostigmine,Eye CNS: toxic reaction glaucoma,Edrophonium chloride: Use for diagnosis Ambenonium chloride: Galanthamine Demecarium bromide,Organophosphates,Binds to AchE complex The covalent bond is stable and hydrolyzes in water at a very slow rate Aging: more stable and more difficult to split,Toxic symptom,Activate M receptor Activate N receptor CNS,Diagnosis Prevention Detoxifcation Atropine PAM,
