第5章拟胆碱药.ppt
2023-11-61 胆碱受体激动药胆碱受体激动药 难难 拟胆碱药拟胆碱药2023-11-62胆碱受体激动药胆碱受体激动药（cholinoceptor agonists）是指可与胆碱受体结合并能激动该受体，产生是指可与胆碱受体结合并能激动该受体，产生与递质乙酰胆碱作用相似的药物。与递质乙酰胆碱作用相似的药物。胆碱酯酶抑制药胆碱酯酶抑制药(Anticholinesterase drug)是指通过抑制胆碱酯酶的活性，使乙酰胆碱破是指通过抑制胆碱酯酶的活性，使乙酰胆碱破坏减少，在突触间隙大量堆积而激动胆碱受体坏减少，在突触间隙大量堆积而激动胆碱受体的药物。的药物。2023-11-63胆碱受体激动药分类胆碱受体激动药分类：lM，N受体激动药受体激动药，如氨甲酰，如氨甲酰胆碱；胆碱；lM受体激动药受体激动药，如毛果芸香碱；，如毛果芸香碱；lN受体激动药受体激动药，如烟碱，作用，如烟碱，作用复杂，无临床应用价值。复杂，无临床应用价值。2023-11-64Muscarine cholinoceptor agonists毛果芸香碱毛果芸香碱(pilocarpine,匹鲁卡品匹鲁卡品)是从毛果芸香属植物中提取的生物碱是从毛果芸香属植物中提取的生物碱 药理作用药理作用 作用机制和特点：作用机制和特点：激动激动M受体受体，产生，产生M样作用。对样作用。对眼睛眼睛和和腺体腺体的作用明显，的作用明显，对心血管的影响小。对心血管的影响小。2023-11-65 1.1.对眼睛的作用对眼睛的作用 (1)(1)缩瞳缩瞳 兴奋瞳孔括约肌细胞膜上的兴奋瞳孔括约肌细胞膜上的M M受体，受体，使瞳孔括约肌收缩，瞳孔缩小。使瞳孔括约肌收缩，瞳孔缩小。2023-11-66 (2)(2)降低眼内压降低眼内压（只见于眼压高者）（只见于眼压高者）房水产生及回流房水产生及回流2023-11-672023-11-682023-11-692023-11-610 (3)(3)调节痉挛调节痉挛 睫状肌睫状肌M M受体兴奋受体兴奋,睫状肌收缩睫状肌收缩,睫状肌向眼中心部方向睫状肌向眼中心部方向拉紧拉紧,悬韧带松弛悬韧带松弛,晶状体变凸晶状体变凸,屈光度增大屈光度增大,视近物清视近物清楚楚,远物模糊称调节痉挛。远物模糊称调节痉挛。睫状肌睫状肌 悬韧带悬韧带 晶状体2023-11-6112023-11-612 2.对腺体作用对腺体作用 皮下注射皮下注射1015mg毛果芸香碱，可明显增加汗腺、毛果芸香碱，可明显增加汗腺、唾液腺的分泌。唾液腺的分泌。临床应用临床应用 1.青光眼青光眼 毛果芸香碱是治疗青光眼首选药物。毛果芸香碱是治疗青光眼首选药物。特点：作用快、温和、短暂，刺激性小，渗透性特点：作用快、温和、短暂，刺激性小，渗透性好。好。2023-11-613青光眼青光眼闭角型闭角型(angle-closure glauconma 充血性青光眼充血性青光眼)：前房角间隙狭窄：前房角间隙狭窄(近视者近视者)。开角型开角型(open-closure glauconma 单纯性青光眼单纯性青光眼)：巩膜静脉窦血管：巩膜静脉窦血管硬化（老年者）。硬化（老年者）。2023-11-6142023-11-6152023-11-616Mushroom Poisoning2023-11-617烟碱（烟碱（Nicotine，尼古，尼古丁）丁）2023-11-6181.The actions of acetylcholine released from autonomic and somatic motor nerves are 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 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 ganglia;in the central nervous system,it largely controls release of neurotransmitters from presynaptic sites.summary2023-11-6192023-11-620 Cholinesterase cleans up unused acetylcholine,by breaking it down into its components acetate and choline.Neurons which produce acetylcholine are damaged in,with the 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.2023-11-6212023-11-6222023-11-6232023-11-6242023-11-6252023-11-6262023-11-6273.阵发性室上性心动过速阵发性室上性心动过速 在压迫眼球或颈动脉窦等兴奋在压迫眼球或颈动脉窦等兴奋迷走神经迷走神经措施无措施无效时，可用新斯的明，通过抑制心肌上的胆碱效时，可用新斯的明，通过抑制心肌上的胆碱酯酶，间接兴奋酯酶，间接兴奋M受体，使心率减慢。受体，使心率减慢。4.4.用于非去极化型骨骼肌松弛药（如筒箭毒碱）用于非去极化型骨骼肌松弛药（如筒箭毒碱）和阿托品中毒时的解救。和阿托品中毒时的解救。2023-11-6282023-11-6292023-11-6302023-11-6312023-11-6322023-11-6332023-11-6341.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 acetylcholine there is to survive longer and be more effective.summary2023-11-635u毛果芸香碱和毒扁豆碱治疗青光眼的异同点u试述毛果芸香碱的药理作用和临床应用u试述新斯的明的药理作用和临床应用
