胆碱受体激动药英文ppt课件

,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,*,Cholinoceptor-activating drug,Cholinoceptor-activating,1,Cholinoceptor-activating drug,Acetylcholine receptor stimulants,Cholinesterase inhibitors,Mimic acetylocholine,Cholinoceptor-activating drug,2,胆碱受体激动药英文ppt课件,3,Acetylcholine receptor stimulants,Classified by their spectrum of action depending on the receptor type,Activate muscarinic receptor,Activate nicotinic receptor,Acetylcholine receptor stimula,4,Muscarinic receptor stimulants,Choline esters:acetylcholine,methacholine,carbachol,bethanechol,Alkaloid:pilocarpine,arecoline,Muscarinic receptor stimulants,5,Acetylcholine,Cardiovascular system:,Vessel:dilation via EDRF,Negative chronotropic effect,Negative dromotropic effect,Negative inotropic effect,AcetylcholineCardiovascular sy,6,Acetylcholine,Gastrointestinal 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,AcetylcholineGastrointestinal,7,Acetylcholine,A large dose of Ach after administration of atropine can activate nicotinic receptor,N,1:,ganglion,N,2:,neuromuscular junction,AcetylcholineA large dose of A,8,Activate N,N,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,Activate NN receptorAll gangli,9,Activate Nm receptor,Neuromuscular end plate,Skeletal muscle Contraction,Activate Nm receptorNeuromuscu,10,methacholine,Selectively activate muscarinic receptor,Stronger effects on cardiovascular system,Clinical uses:sjogrens syndrome,Asthma,ulcer,anoxemia,methacholineSelectively activa,11,others,Carbachol:pharmacodynamics is similar to Ach,uses for glaucoma,Bethanechol:more selective to M receptor,othersCarbachol:pharmacodynam,12,Alkaloid,Including pilocarpine,arecoline,muscarine,oxotremorine,Alkaloid,13,pilocarpine,Pharmacodynamics:,Eye:miosis,ocular pressure reduction,accommodation,Glands:secretion,pilocarpinePharmacodynamics:,14,（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,受体,（动眼神经的胆碱能神经支配）毛果芸香碱激动 瞳孔括约肌,15,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,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,16,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,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,17,Clinical uses,Glaucoma,Iritis,Clinical usesGlaucoma,18,Muscarine,Direct acting muscarinic receptor:toxic reaction,Muscarine Direct acting musc,19,nicotine,Contributes to increased risk of vascular disease and sudden coronary death,Contributes to high incidence of ulcer recurrence with peptic ulcer,nicotineContributes to increas,20,Anticholinesterase agents,Anticholinesterase agents,21,Acetylcholinesterase,Ach,=,AchE,Ach-AchE,choline+AcAchE,Acetate+Ache,The entire process takes place in 150ms,Acetylcholinesterase,22,AchE,Nerve terminal,synaptic,cleft,effectors,Most chlinergic synapses are richly supplied with AchE,the half-life of Ach is very short,AchENerve terminal,synaptic c,23,Anticholinesterase agents,Binds to AchE complex,The covalent bond is resistance to the second process,and this step is prolonged,Anticholinesterase agentsBinds,24,classification,Hydration process is prolonged for 30 minutes to 6 hours,Hydration process is prolonged for hundreds of hours,classificationHydration proces,25,Anticholinesterase agents,Pharmacodynamics:,Eye:miosis,ocular pressure reduction,accommodation,Gastrointerase systems:contract,increase secretion,Anticholinesterase agentsPharm,26,Anticholinesterase agents,Neuromuscular junction:,Therapeutic concentration:prolong and intensify the actions of Ach;activate skeletal muscle directly,Higher concentration:fibrillation of muscle fibers,Anticholinesterase agentsNeuro,27,Anticholinesterase agents,Respiratory,urinary tract:contract,Cardiovascular system:increase activation in ganglia and at acetylcholine receptors on neruoeffector cells(HR ,BP ),Anticholinesterase agents,28,Anticholinesterase agents,Glands:secret,CNS,Low concentration:activation of EEG,subjective alerting response,High concentration:coma,respiratory arrest,Anticholinesterase agentsGland,29,Clinical uses,Myasthenia gravis,Ileus,Glaucoma,Detoxifcation,Alzheimiers disease,cholinergic crisis,Clinical usesMyasthenia gravis,30,Neostigmine,Inhibit AchE and thereby increase the concentration of endogenous Ach,Act at neuromuscular junction and smooth muscle Selectively,Myasthenia gravis,Ileus,NeostigmineInhibit AchE and th,31,Pyridostigmine,Pharmacodynamics is similar to Neostigmine,Take effect slowly,Myasthenia g