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Chapter 7 Cholinoceptor- Blocking Drugs () -N - Cholinoceptor blockers Zhang bin Institute of Pharmacology School of Medicine Shandong University

Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ ) -N - Cholinoceptor blockers

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Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ ) -N - Cholinoceptor blockers. Zhang bin Institute of Pharmacology School of Medicine Shandong University. Nicotinic cholinoceptor- blocking drugs. N N -R antagonists (ganglionic blocking drugs) N M -R antagonists - PowerPoint PPT Presentation

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Page 1: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Chapter 7 Cholinoceptor-Blocking Drugs

(Ⅱ ) -N -Cholinoceptor blockers Zhang bin

Institute of Pharmacology

School of Medicine

Shandong University

Page 2: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Nicotinic cholinoceptor- blocking drugs

NN-R antagonists

(ganglionic blocking drugs)

NM-R antagonists

(neuromuscular blocking drugs )(Skeletal muscle relaxants)

Page 3: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Section1 NN-R antagonists

(ganglionic blocking drugs)

Mecamylamine(美卡拉明,美加明 )

Trimethaphan(樟磺咪酚,曲美芬)

Page 4: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

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

Page 5: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Section2 NM-R antagonists ( Skeletal muscle relaxants )(neuromuscular blocking drugs )

Depolarizing skeletal muscle relaxants

—— succinylcholine Nondepolarizing skeletal muscle

relaxants

—— D-tubocurarine

Page 6: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Depolarizing skeletal muscle relaxants

Page 7: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Mechanism: Two-phase blockPhase 1: durable depolarizing blockPhase 2: NM receptor desensitization

Page 8: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

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

Page 9: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

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 )

Page 10: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

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

Page 11: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

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,骨骼肌对钙呈高反应性,引起剧烈的肌肉收缩、代谢提高 )

丹曲林钠 ( 肌松剂 ): 其主要作用部位是骨骼肌的肌浆网,通过抑制肌浆网释放钙离子而减弱肌肉收缩。

Page 12: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Nondepolarizing muscular relaxants(competitive neuromuscular blockers)

Page 13: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Mechanisms:

NM-R competitive

antagonist

Page 14: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Characteristics of Action (1) no fasciculation (2) Antagonized by AChEI (3) slow onset and long duration (4) NN blockade at therapeutic dose

Page 15: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

d-tubocurarine(筒箭毒碱 )

[[Actions] muscle relaxant block ganglionic release histamine

[Uses]

assistant agents of anesthetics

Page 16: Chapter 7 Cholinoceptor-Blocking Drugs ( Ⅱ )  -N - Cholinoceptor blockers

Other drugsbenzylisoquinolines (苄基异喹啉类 ) Atracurium (阿曲库铵 ) Doxacurium (多库铵 ) Mivacurium (米库铵 )ammoniosteroids(类固醇胺类) Pancuronium (泮库铵 ) Pipecuronium (哌库铵 ) Rocuronium (罗库铵 ) Vecuronium (维库铵 )