1、胆碱受体阻断药的分类胆碱受体阻断药的分类 M cholinoceptor blocking drugsM cholinoceptor blocking drugs N N1 1 Cholinoceptor Blocking Drugs Cholinoceptor Blocking Drugs(ganglionic blocking drugs(ganglionic blocking drugs）N N2 2 Cholinoceptor Blocking Drugs Cholinoceptor Blocking Drugs(Skeletal muscle relaxants)(Skeletal
2、muscle relaxants)第一节第一节 M M-Cholinoceptor Blocking Cholinoceptor Blocking DrugsDrugs 阿托品阿托品(Atropine)(Atropine)A belladonna alkaloid,has a high A belladonna alkaloid,has a high affinity for M receptors,where it binds affinity for M receptors,where it binds competitively,preventing acetylcholine comp
3、etitively,preventing acetylcholine from binding to that site.from binding to that site.竞争性拮抗竞争性拮抗AchAch对对M M受体的激动作用，大剂量阻受体的激动作用，大剂量阻断断N N受体。受体。Pharmacological effects Pharmacological effects 1 1、解除平滑肌痉挛：松驰多种内脏平滑肌、解除平滑肌痉挛：松驰多种内脏平滑肌 特点特点:(1)(1)对过度活动或痉挛的平滑肌松驰作用较对过度活动或痉挛的平滑肌松驰作用较显著。显著。(2)(2)胃肠胃肠 膀胱膀胱 胆囊
4、胆囊,胆管胆管,输尿管输尿管,支气管支气管,子宫子宫 2.2.抑制腺体分泌抑制腺体分泌 唾液腺唾液腺(口干口干),),汗腺汗腺(皮肤干燥皮肤干燥)呼吸道呼吸道腺体腺体 胃腺。大剂量也抑制胃的分泌机能胃腺。大剂量也抑制胃的分泌机能 Salivary gland(dry mouth),sweat Salivary gland(dry mouth),sweat gland(dryness of the skin)bronchial gland(dryness of the skin)bronchial secretory gland secretory gland(discharge decreas
5、ed)(discharge decreased)stomach gland(Large dosage may stomach gland(Large dosage may inhibit the secretory function of the inhibit the secretory function of the stomach)stomach)3.Eye:it blocks all cholinergic 3.Eye:it blocks all cholinergic activity on the eye,resulting in activity on the eye,resul
6、ting in dilation of pupil,dilation of pupil,unresponsiveness to light and unresponsiveness to light and inability to focus for near vision.inability to focus for near vision.In patients with glaucoma,In patients with glaucoma,intraocular pressure may rise intraocular pressure may rise dangerously.da
7、ngerously.(1)(1)散瞳散瞳(mydriasis)(mydriasis)：?(2)(2)眼内压升高：眼内压升高：?(3)(3)调节麻痹调节麻痹(cycloplegia)(cycloplegia)：?睫状肌松弛，拉紧悬韧带，使晶状体睫状肌松弛，拉紧悬韧带，使晶状体变扁平，屈光度降低，以致视近物模变扁平，屈光度降低，以致视近物模糊，视远物清楚。糊，视远物清楚。4.Cardiovascular system:4.Cardiovascular system:Atropine produces Atropine produces divergentdivergent effects on t
8、he cardiovascular effects on the cardiovascular system,depending on the dose.system,depending on the dose.（1 1）At low dose(0.4At low dose(0.4-0.6mg),it 0.6mg),it results in the blockade of results in the blockade of 突触前突触前膜膜(presynaptic membrane)的的M1M1受体，受体，thus thus permitting increased Ach release
9、.permitting increased Ach release.心率减慢。心率减慢。（2 2）With higher dose of atropine With higher dose of atropine(at least of 1mg),the cardiac M(at least of 1mg),the cardiac M-receptors on the SAreceptors on the SA（sinoatrial）nodenode窦房结窦房结are blocked,and the cardiac are blocked,and the cardiac rate increa
10、ses moderately.rate increases moderately.迷走神经张力高的青年，心率加快作用迷走神经张力高的青年，心率加快作用显著，对婴幼儿和老年人的心率影响很显著，对婴幼儿和老年人的心率影响很小。小。(3)(3)扩张血管，改善微循环扩张血管，改善微循环：治疗量对血管和：治疗量对血管和血压无明显影响，大剂量解除小血管痉挛，血压无明显影响，大剂量解除小血管痉挛，改善微循环和重要器官的血流供应，减轻组改善微循环和重要器官的血流供应，减轻组织缺氧。织缺氧。The mechanism of dilation of blood The mechanism of dilation
11、of blood vessel is not related to the vessel is not related to the blockage of M receptor.blockage of M receptor.5.CNS5.CNS (1)(1)治疗量（治疗量（0.50.51mg)1mg)：可轻度兴奋：可轻度兴奋延脑和大脑皮层。延脑和大脑皮层。(2)(2)较大剂量（较大剂量（5mg)5mg)：中枢兴奋明显：中枢兴奋明显加强，可由兴奋转入抑制、死亡。加强，可由兴奋转入抑制、死亡。In In high doses,it causes agitation,high doses,it c
12、auses agitation,seizures,hallucinations and coma.seizures,hallucinations and coma.Clinical uses Clinical uses 1.Atropine is used as an 1.Atropine is used as an antispasmodic agent to relax antispasmodic agent to relax the gastrointestinal tract and the gastrointestinal tract and bladder.bladder.解除平滑
13、肌痉挛：胃肠绞痛解除平滑肌痉挛：胃肠绞痛 膀胱刺膀胱刺激症激症 胆绞痛和肾绞痛（胆、肾绞痛胆绞痛和肾绞痛（胆、肾绞痛常与镇痛药哌替啶合用）。常与镇痛药哌替啶合用）。2.2.眼科：眼科：（1 1）虹膜睫状体炎）虹膜睫状体炎:it may be also be:it may be also be used to topically in iritis as a used to topically in iritis as a mydriatic agent,to prevent the mydriatic agent,to prevent the formation of adhesions be
14、tween the iris formation of adhesions between the iris and the cornea.and the cornea.(2)(2)扩瞳扩瞳:检查眼底。检查眼底。(3)(3)验光配镜：使调节麻痹，晶状体固定，验光配镜：使调节麻痹，晶状体固定，准确地测定屈光度。仅儿童验光时用。准确地测定屈光度。仅儿童验光时用。3.This drug is sometimes used 3.This drug is sometimes used as an antisecretory agent to as an antisecretory agent to bl
15、ock secretions in the upper block secretions in the upper and lower respiratory tracts and lower respiratory tracts prior to surgery.prior to surgery.全身麻醉前给药抑制腺体分泌全身麻醉前给药抑制腺体分泌 4.4.缓慢型缓慢型心律失常：心律失常：窦性心动过缓窦性心动过缓(bradycardias)(bradycardias)，I,III,II度房室度房室传导阻滞等。传导阻滞等。心肌梗死引起的窦性或房室结性心动过缓时，心肌梗死引起的窦性或房室结性心动
16、过缓时，大剂量增加心率而加重心肌缺血。大剂量增加心率而加重心肌缺血。5.5.抗休克抗休克:？暴发型流脑、中毒性菌痢、中毒性肺炎暴发型流脑、中毒性菌痢、中毒性肺炎等所致的休克。等所致的休克。伴高热不用。？伴高热不用。？6.Atropine can be used for the 6.Atropine can be used for the treatment of overdose of treatment of overdose of organophosphate and some types organophosphate and some types of mushroom poisoning.of mushroom poisoning.Mechanism?Mechanism?Its ability to enter the CNS is Its ability to enter the CNS is one of particular importance.one of particular importance.Adverse effects Adverse effects