Chapter 7 Cholinoceptor-Blocking Drugs Zhang Bin Institute of Pharmacology School of medicine Shandong university
Chapter 7 Cholinoceptor-Blocking Drugs Zhang Bin Institute of Pharmacology School of Medicine, Shandong University
Section 1 Muscarinic cholinoceptor blocking drugs A tropine and atropine-like alkaloids Synthetic atropine substitutes
Section 1 Muscarinic cholinoceptor -blocking drugs Atropine and atropine-like alkaloids Synthetic atropine substitutes
Atropine and atropine-like alkaloids atropine-like alkaloids and their resources 植物 主要生物碱 颠茄( atropa belladonna) 莨菪碱(h hyoscyamine 曼陀罗( datura stramonium)莨菪碱 洋金花( datura sp) 东莨菪碱( scopolamine 莨菪( hyoscyamus niger) 莨菪碱 唐古特莨菪( scopolia tangutica)山莨菪碱( anisodamine)) 樟柳碱( anisodine) 阿托品为消旋莨菪碱
atropine-like alkaloids and their resources 植物 主要生物碱 颠茄(atropa belladonna) 莨菪碱(hyoscyamine ) 曼陀罗(datura stramonium) 莨菪碱 洋金花(datura sp) 东莨菪碱 (scopolamine) 莨菪(hyoscyamus niger) 莨菪碱 唐古特莨菪(scopolia tangutica) 山莨菪碱 (anisodamine) 樟柳碱(anisodine) 阿托品为消旋莨菪碱 Atropine and atropine-like alkaloids
阿托品( atropine) CH2 CH20 酸开园片 N一CH H-0-C0-C 叔胺 H2C-CH CH2 H 200青药GMP 中的数常文号:(6你m2 @黑硫酸阿托品注射液 本品为硫酸阿托品的灭菌水溶液 5支盒 【主要成分】硫酸阿托品 【适应症】有机磷酸酯类中毒、麻酵前给药和拮抗拟胆碱 国药准字31021160 神经兴奋症状 肌内、皮下或静脉注射:一次量,每1kg体 硫酸阿托品眼膏 重,麻酵前给 002~005mg解除有机磷酸酯类中毒,马 0.5-1mg 1% 上海通用药业股份育公司 【停药期】28日,弃奶期7日,蛋期7日 【贮藏】密闭保存 【生产批号 【生产日期】 【有效期】二年 南阳市理邦制药有限公司 地址:南阳市店电话:037163660159传真:63081571邮端:473134
阿托品（atropine） N C H C H 3 H 2 C C H 2 H 2 C C H C H 2 C H O C O C C H 2 O H H 叔胺
Atropine pharmacological actions a block M-R: Competitive and Nonselective block Ny-R: in large dose Organ sensitivity: Gland >eye splanchnic smooth muscle cardiovascular system CNS
pharmacological actions ◼ block M-R: Competitive and Nonselective block NN-R : in large dose Organ sensitivity: Gland ＞eye ＞ splanchnic smooth muscle ＞cardiovascular system ＞CNS Atropine
l. glands: secretion↓ salivary, sweat>lacrimal, respiratory gastric acid pancreatic, intestinal juice 头期刺激 神经中枢 胃期刺激 (扩张、化学) 冒粘膜G细胞 迷走神经 胃泌素 局部反射 肠期剌激 胃泌素 胃腺 十二指肠粘膜G细胞 其他胃肠道激素 及非胆碱能递质
1. glands:secretion↓ salivary, sweat > lacrimal, respiratory > gastric acid > pancreatic, intestinal juice 十二指肠粘膜G细胞 迷 走 神 经 其他胃肠道激素 及非胆碱能递质
g(1) Sweat glands Actions secretion of the sweat glands--dry skin n adu ult. large dose cause T℃↑;In infants children ordinary dose cause atropine fever ■Uses: night sweat
❖ (1) Sweat glands ◼ Actions: ◼ ↓secretion of the sweat glands—dry skin. In adult, large dose cause T℃↑; In infants& children ordinary dose cause “atropine fever” ◼ Uses: night sweat
(2)salivary glands: Actions: salivary secretion markedly a Side reactions: dry mouth, swallowing and talking difficultly a Uses: salivation
❖ (2) salivary glands: ◼ Actions: ↓salivary secretion markedly ◼ Side reactions: dry mouth, swallowing and talking difficultly ◼ Uses: salivation
(3) Respiratory tract glands ■Uses pre-anaesthetic agent to avoid asphyxia(窒息) asthma(ipratropium) (4) Lacriminal glands
(3) Respiratory tract glands ◼ Uses: ◼ pre-anaesthetic agent to avoid asphyxia (窒息) ◼ asthma (ipratropium) (4) Lacriminal glands
(5) gastic glands a Actions. Large dose, gastric acid, pepsin secretion Uses: peptic ulcer(pirenzepine
❖ (5) gastic glands: ◼ Actions: ◼ Large dose, ↓gastric acid, pepsin secretion ◼ Uses: peptic ulcer (pirenzepine)