胆碱受体阻断药.pptxVIP

胆碱受体阻断药 M-R阻断药muscarinic blocking drugs 抗胆碱药anticholinegics副交感神经阻断药 parasympatholytics Muscarinic blocking drugs have no intrinsic activity, and they can produce effects only by blocking the activation of muscarinic receptors by muscarinic agonists or by neuronally released ACh、图5-2传出神经分类模式图§ 1 阿托品和阿托品类生物碱 Atropine ＆ atropine-like alkaloid 存在于颠茄 、曼陀罗、莨菪中颠茄曼陀罗莨菪Atropa belladonna山莨菪碱Anisodamine 阿托品Atropine 东莨菪碱Scopolamine 中枢作用:氧桥?,羟基?东莨菪碱＞阿托品＞山莨菪碱阿托品 Atropine【 Mechanism of action】(作用机理)1、(-)M-R2、 large dose:(-)NN -R 【 Pharmacological actions 】(药理作用) gland (腺体) eye smooth muscle (平滑肌) heart CNS1、 腺体(glands)(-)腺体分泌 (inhibits the secretion of glands) 汗腺( sweat gland ) 、唾液腺(salivary gland ) 泪腺( lachrymal ) 、呼吸道腺体 胃壁细胞 ( gastric parietal cells ) 　Please pare atropinewith pilocarpine2、 眼(eye) atropine(1) 扩瞳(mydriasis)(-) 瞳孔括约肌M-R开大肌功能占优势瞳孔扩大( dilate the pupil )(2) 升高眼压 ( increase intraocular pressure ) Atropine → 扩瞳→虹膜退向四周边缘→根部变厚→前房角间隙↓ →房水回流↓ →眼内压↑。(3) 调节麻痹( paralysis acmodation ) Atropine (-) 睫状肌M-R→睫状肌松驰→悬韧带拉紧→晶状体扁平→视远物清楚,近物模糊。summaryMuscarinic agonist PilocarpineMuscarinic antagonist Atropine Miosis 缩瞳↓intraocular pressure ↓眼内压 Spasm of acmodation 调节痉挛 ↑lacrimal secretion ↑泪腺分泌 Mydriasis 扩瞳 ↑intraocular pressure ↑眼内压 paralysis of acmodation 调节麻痹 ↓ lacrimal secretion ↓泪腺分泌3、 平滑肌(smooth muscle )松弛内脏平滑肌Relaxes visceral smooth muscle、Characteristics ( 特点 )(1) 作用强度与平滑肌的功能状态有关;(2) 作用强度顺序:胃肠道膀胱 输尿管胆管、支气管、子宫。4、 心脏( Heart )(1) 心率 (heart rate, HR )治疗量(therapeutic dose):HR ?大剂量( higher dose):HR↑解除了迷走神经对心脏的抑制。( Block vagal effects on the sinoatrial node directly、 )(2) 房室传导: 促进房室传导5、 血管与血压 ( Vessels＆ blood pressure ) Therapeutic dose ---无明显作用 原因:多数血管缺乏胆碱能神经支配Large dose--- 扩张血管 --- atropine blush(脸红 )The mechanism is unknown、There is little effect on blood pressure、6、 CNS 兴奋 ? 抑制Excitation followed by depression、【Clinical Uses 】解痉药1、 缓解内脏绞痛( releves visceral colic pain )胃肠绞痛( gastric and intestinal colic pain )膀胱刺激症状 ( bladder irritating symptoms ) 胆绞痛 ( gallblad