拟胆碱药CholinergicDrugs.HNNCH3CH3HOOCH3CH3CH3NNOHNCOH3C-+OCH3ONCH3H3CH3CBrNCH3,+ICHOHCH3NN-毛果芸香碱碱性异构化水解性稳定性毒扁豆碱碱性水解性溴新斯的明碱性水解性鉴别反应碘解磷定稳定性水解性鉴别反应抗胆碱药AnticholinergicDrugs胆碱受体拮抗剂•作用阻断乙酰胆碱与胆碱受体的相互作用•治疗胆碱能神经系统过度兴奋造成的病理状态抗胆碱药分类•按照药物的作用部位及对胆碱受体亚型的选择性M胆碱受体拮抗剂(节后抗胆碱药/平滑肌解痉药)神经节阻断剂(N1)神经肌肉阻断剂(N2)(骨骼肌松驰药)M胆碱受体拮抗剂(节后抗胆碱药/平滑肌解痉药)•可逆性阻断节后胆碱能神经支配的效应器上的M受体∮抑制腺体分泌(唾液腺、汗腺、胃液)∮散大瞳孔∮加速心律∮松弛支气管和胃肠道平滑肌等•治疗∮消化性溃疡∮散瞳∮内脏绞痛等(平滑肌痉挛)神经节阻断剂•在交感和副交感神经节选择性拮抗N1胆碱受体∮稳定突触后膜,阻断神经冲动在神经节中的传递∮降低血压•治疗重症高血压(见“心血管系统药物”)神经肌肉阻断剂(骨骼肌松驰药)•与骨骼肌运动终板膜上的N2受体结合∮阻断神经冲动在神经肌肉接头处的传递∮骨骼肌松弛作用•临床用于麻醉辅助药节后抗胆碱药颠茄生物碱类(托烷类生物碱)阿托品山莨菪碱东莨菪碱樟柳碱合成类专属行较强后马托品溴甲基阿托品叔胺类解痉药贝那替秦阿地芬宁(解痉素)胃安季铵类解痉药服止宁奥芬溴铵溴本辛普鲁本辛(溴丙胺太林)87654321NCH3OCCHCH2OHO(8-13)HONCH3O(ONCH3O(ONCH3OCCHCH2OHO(8-15)432CH3OCCHCH2OHO(8-13)HONCH3OCCHCH2OHO(8-14)OHCONCH3OCCH2OHO(8-16)CH3OCCHCH2OHO(8-15)87654321NCH3OCCHCH2OHO(8-13)HONCH3OONCH3O(ONCH3OCCHCH2OHO(8-15)3OCCHCH2OHO(8-13)HONCH3OCCHCH2OHO(8-14)OHCONCH3OCCH2OHO(8-16)OCCHCH2OHO(8-15)阿托品山莨菪碱东莨菪碱樟柳碱莨菪醇莨菪酸增加分子的亲脂性,使中枢作用增强增加分子的亲水性,使中枢作用减弱(8-17)OHOCHCOCH3N+OCH2OHCHCOCH3NCH3Br-.(8-18)(8-19)(8-20)C2H5C2H5CCOOCH2CH2NRHOHR(8-21)CH2SO412CH3CH3CH3CH2CHNCONH2后马托品溴甲基阿托品贝那替秦阿地芬宁(解痉素)胃安(8-19)(8-20)C2H5C2H5CCOOCH2CH2NRHOHR扩瞳时间短,副作用少,不抑制腺体分泌对中枢作用较弱,胃肠道作用强解痉作用明显,抑制胃液分泌较弱(8-22)(8-23)R-+BrOHC2H5C2H5OCH2CH2NOCCCH3RC2H5(8-24)(8-25)CH(CH3)2RRCH3-+BrHCOCH2CH2NOOR服止宁奥芬溴铵溴本辛普鲁本辛(溴丙胺太林...