N受体阻滞剂——山东大学药理学英文课件.ppt

  Chapter 7 Cholinoceptor-Blocking Drugs (Ⅱ) -N -Cholinoceptor blockers  Zhang bin Institute of Pharmacology School of Medicine Shandong University Nicotinic cholinoceptor- blocking drugs NN-R antagonists (ganglionic blocking drugs) NM-R antagonists (neuromuscular blocking drugs ) (Skeletal muscle relaxants) Section1 NN-R antagonists (ganglionic blocking drugs) Mecamylamine(美卡拉明，美加明) Trimethaphan（樟磺咪酚，曲美芬） NN-R antagonists [Characteristics] Co-innervation and dominant theory Blood vessel: vasodilation, peripheral resistance decrease, blood pressure decrease. Glands, eye, GI, bladder: dry mouth, mydriasis, constipation, urinary retention [Clinical use] HBP Section2 NM-R antagonists （Skeletal muscle relaxants） (neuromuscular blocking drugs ) Depolarizing skeletal muscle relaxants —— succinylcholine Nondepolarizing skeletal muscle relaxants —— D-tubocurarine Depolarizing skeletal muscle relaxants Mechanism: Two-phase blockPhase 1: durable depolarizing blockPhase 2: NM receptor desensitization Depolarizing skeletal muscle relaxants [Characteristics of Action] （1）Muscle fasciculation (肌束震颤) （2）Tachyphylaxis (快速耐受性) （3）Can’t be antagonized by AChEI （4）have no ganglionic blocking actions at therapeutic dose (5) rapid onset and short duration succinylcholine (琥珀胆碱,scoline,司可林) (1)Onset rapid(1’), Emax 2’, short duration(5’) (2) Neck and limbs (3)pseudocholinesterase [Uses] 1.assistant agents of anesthetics 2.bronchial cannulation，bronchoscopy oesophagoscop(食道镜) Adverse reactions (1)? asphyxy(窒息): respiratory muscle paralysis: genetic pseudo-ChE low patients anti-AChE agents local anesthetics and aminoglycosides (2) Muscle fasciculation (3) Elevation of extracellular K+ (4) CVS: complex (5) Malignant hyperpyrexia(恶性高热): idiosyncrasy （特异质反应) (6) increase histamine release Malignant hyperpyrexia 在并用琥珀胆碱和强挥发性全麻药（氟烷、异氟烷）时引起的高代谢反应，体温极度升高。是一种常染色体显性遗传。(钙释放通道基因变异