传出神经系统药理英文(睢大员)
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Pharmacology
Department of Pharmacology School of Pharmacy Jilin University
SUI Da-yuan 睢大筼
Chapter 5
pharmacology of efferent nervous system
What is efferent nervous system (ENS)? ceptor effector ANS ENS
Norepinephrin (NE)
synthesis releasing
elimination
1
NA
2
NA
Synthesis,releasing and elimination of NA
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
reversible cholinesterase inhibitors
galanthamine tensilon tacrine donepezil
Chapter 7
cholinoceptor antagonists
1. M-cholinoceptor antagonists 2. N1-cholinoceptor antagonists 3. N2-cholinoceptor antagonists
molecular mechanism of biological effect
Ligand gated ion channel receptor， regulate Na+、K+、Ca2+ flux.
G-protein-coupled receptors）
drug action and signai transduction
reversible choliesterase inhibitors
neostigmine
Adverse drug reaction
large dosage
nausea vomiting abdominal pain muscle thrill or paralysis cholinergic crisis
1. Eye
3. M-cholinoceptor agonists pilocarpine 1. eye a. miosis (constrict pupil) b. decrease intraocular pressure c. cyclospasm (spasm of accommodation)
--direct activating N2 receptors --release Ach at the motor nerve endings
2. stimulating GI tract and gallbladder smooth muscle
reversible cholinesterase inhibitors
Chapter 5 pharmacology of ENS
Section 4 action manners and classification of drugs
classification of drugs
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
neostigmine
clinical uses
1. myasthenia gravis
cholinergic crisis
2. postoperative ileus and urinary retention 3. paroxysmal supraventricular tachycardia
4. overdosage of muscle relaxants
ACh
Chapter 5 pharmacology of ENS
Section 3 biological effect and mechanism
biological effect of ENS
see under table
Chapter 5 pharmacology of ENS
Section 3 biological effect and mechanism
Section 1 cholinoceptor agonists
3. M-cholinoceptor agonists
pilocarpine
stimulates M-receptor
3、M-cholinoceptor agonists pilocarpine
Pharmacologic effects
M-cholinoceptor antagonists
atropine
Pharmacologic effects
2. relaxing visceral smooth muscle stomach intestine detrusor of bladder urinary tract bronchial muscle biliary tract uterus
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors reversible cholinesterase inhibitors neostigmine physostigmine non-reversible cholinesterase inhibitors
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
Classification of transmitters （1）cholinergic nerve
（2）noradrenergic nerve (adrenergic nerve)
drugs
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors reversible cholinesterase inhibitors
neostigmine
organophosphates
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors
hydrolysis of ACh Ach
AChE
choline acetic acid
depolarizing drugs succinylcholine nondepolarizing drugs tubocurarine
M-cholinoceptor antagonists
atropine
Pharmacologic effects
1. inhibiting the secretion of gland salivary gland sweat gland bronchial secretary gland stomach gland
CNS
Chapter 5 pharmacology of ENS
Section 1 structure and function Classification of anatomy
（1）Autonomic nervous system
Sympathetic nerve parasympathetic nerve
M-cholinoceptor antagonists
atropine
Pharmacologic effects
receptors
（1）cholinceptors Muscarine receptor (MR): M1 and M2 Nicotine receptor (NR)：N1 and N2 （2）adrenoceptors αreceptor：α1 andα2 βreceptor：β1、β2 andβ3 （3）dopamine receptors: D1 and D2
M-cholinoceptor antagonists
atropine
Pharmacologic effects
3. eye mydriasis
increases intraocular pressure
cycloplegia
circular muscle
M
Radial muscle
transmitters
（2） Acetylcholine (Ach)
releasing synthesis elimination
AChE
ACh
Synthesis,releasing and elimination of ACh
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
reversible cholinesterase inhibitors
neostigmine
contraindications
mechanical intestinal obstruction
urinary obstruction
bronchial asthma
reversible cholinesterase inhibitors physostigmine eye a. miosis b. decrease intraocular pressure c. Cyclospasm
circular muscle
M
radial muscle
3、M-cholinoceptor agonists pilocarpine 1. eye 2. glands
increase secretion of sweat gland and salivary gland
3. smooth muscle
3. M-cholinoceptor agonists pilocarpine clinical uses 1. glaucoma
open-angle glaucoma close-angle glaucoma
2. iritis
cornea
iris canal schlemn ciliary muscle lens suspensory ligaments
reversible inhibit AChE
Ach
M-receptor
N-receptor
reversible cholinesterase inhibitors
neostigmine
Pharmacologic effects
very strong
1. contracting skeletal muscle
Section 1 cholinoceptor agonists
1. M、N-cholinoceptor agonists acetylcholine carbaylcholine 2. N-cholinoceptor agonists nicotine
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Chapter 5 pharmacology of ENS
Section 4 action manners and classification of drugs
action manners
（1）Direct: agonist antagonist （2）Indirect: affect release affect transport and storage
（2）Motor nervous system
synapse
突触间隙 Synaptic cleft
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
transmitters
Transmitters
源自文库
（1）Noradrenaline (NA)
Department of Pharmacology School of Pharmacy Jilin University
SUI Da-yuan 睢大筼
Chapter 5
pharmacology of efferent nervous system
What is efferent nervous system (ENS)? ceptor effector ANS ENS
Norepinephrin (NE)
synthesis releasing
elimination
1
NA
2
NA
Synthesis,releasing and elimination of NA
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
reversible cholinesterase inhibitors
galanthamine tensilon tacrine donepezil
Chapter 7
cholinoceptor antagonists
1. M-cholinoceptor antagonists 2. N1-cholinoceptor antagonists 3. N2-cholinoceptor antagonists
molecular mechanism of biological effect
Ligand gated ion channel receptor， regulate Na+、K+、Ca2+ flux.
G-protein-coupled receptors）
drug action and signai transduction
reversible choliesterase inhibitors
neostigmine
Adverse drug reaction
large dosage
nausea vomiting abdominal pain muscle thrill or paralysis cholinergic crisis
1. Eye
3. M-cholinoceptor agonists pilocarpine 1. eye a. miosis (constrict pupil) b. decrease intraocular pressure c. cyclospasm (spasm of accommodation)
--direct activating N2 receptors --release Ach at the motor nerve endings
2. stimulating GI tract and gallbladder smooth muscle
reversible cholinesterase inhibitors
Chapter 5 pharmacology of ENS
Section 4 action manners and classification of drugs
classification of drugs
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
neostigmine
clinical uses
1. myasthenia gravis
cholinergic crisis
2. postoperative ileus and urinary retention 3. paroxysmal supraventricular tachycardia
4. overdosage of muscle relaxants
ACh
Chapter 5 pharmacology of ENS
Section 3 biological effect and mechanism
biological effect of ENS
see under table
Chapter 5 pharmacology of ENS
Section 3 biological effect and mechanism
Section 1 cholinoceptor agonists
3. M-cholinoceptor agonists
pilocarpine
stimulates M-receptor
3、M-cholinoceptor agonists pilocarpine
Pharmacologic effects
M-cholinoceptor antagonists
atropine
Pharmacologic effects
2. relaxing visceral smooth muscle stomach intestine detrusor of bladder urinary tract bronchial muscle biliary tract uterus
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors reversible cholinesterase inhibitors neostigmine physostigmine non-reversible cholinesterase inhibitors
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
Classification of transmitters （1）cholinergic nerve
（2）noradrenergic nerve (adrenergic nerve)
drugs
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors reversible cholinesterase inhibitors
neostigmine
organophosphates
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Section 2 cholinesterase inhibitors
hydrolysis of ACh Ach
AChE
choline acetic acid
depolarizing drugs succinylcholine nondepolarizing drugs tubocurarine
M-cholinoceptor antagonists
atropine
Pharmacologic effects
1. inhibiting the secretion of gland salivary gland sweat gland bronchial secretary gland stomach gland
CNS
Chapter 5 pharmacology of ENS
Section 1 structure and function Classification of anatomy
（1）Autonomic nervous system
Sympathetic nerve parasympathetic nerve
M-cholinoceptor antagonists
atropine
Pharmacologic effects
receptors
（1）cholinceptors Muscarine receptor (MR): M1 and M2 Nicotine receptor (NR)：N1 and N2 （2）adrenoceptors αreceptor：α1 andα2 βreceptor：β1、β2 andβ3 （3）dopamine receptors: D1 and D2
M-cholinoceptor antagonists
atropine
Pharmacologic effects
3. eye mydriasis
increases intraocular pressure
cycloplegia
circular muscle
M
Radial muscle
transmitters
（2） Acetylcholine (Ach)
releasing synthesis elimination
AChE
ACh
Synthesis,releasing and elimination of ACh
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
reversible cholinesterase inhibitors
neostigmine
contraindications
mechanical intestinal obstruction
urinary obstruction
bronchial asthma
reversible cholinesterase inhibitors physostigmine eye a. miosis b. decrease intraocular pressure c. Cyclospasm
circular muscle
M
radial muscle
3、M-cholinoceptor agonists pilocarpine 1. eye 2. glands
increase secretion of sweat gland and salivary gland
3. smooth muscle
3. M-cholinoceptor agonists pilocarpine clinical uses 1. glaucoma
open-angle glaucoma close-angle glaucoma
2. iritis
cornea
iris canal schlemn ciliary muscle lens suspensory ligaments
reversible inhibit AChE
Ach
M-receptor
N-receptor
reversible cholinesterase inhibitors
neostigmine
Pharmacologic effects
very strong
1. contracting skeletal muscle
Section 1 cholinoceptor agonists
1. M、N-cholinoceptor agonists acetylcholine carbaylcholine 2. N-cholinoceptor agonists nicotine
Chapter 6
cholinoceptor agonists and cholinesterase inhibiting drugs
Chapter 5 pharmacology of ENS
Section 4 action manners and classification of drugs
action manners
（1）Direct: agonist antagonist （2）Indirect: affect release affect transport and storage
（2）Motor nervous system
synapse
突触间隙 Synaptic cleft
Chapter 5 pharmacology of ENS
Section 2 transmitter and receptor
transmitters
Transmitters
源自文库
（1）Noradrenaline (NA)