神经系统药理2胆碱能神经系统
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• Measurement of the refractive errors(验光): children • Acute iritis or iridocyclitis: mydriatics/miotics （ to
prevent synechia/adhesion）
(2) Antispasmodic agent
• GI, biliary or renal colic, enuresis(遗尿)
(3) Inhibiting exocrine gland secretion
• Preanesthetic medication
(4) Bradyarrhythmia
• sinus or nodal bradycardia, A-V block
• N cholinoceptor antagonists
NN cholinoceptor antagonists: mecamylamine美加明 (Ganglionic Blocking drugs, rarely used )
NM cholinoceptor antagonists: succinylcholine琥珀胆碱 (Neuromuscular Blocking drugs )
• ห้องสมุดไป่ตู้ow: xerostomia (dry mouth); anhidrosis (dry skin), tachycardiad • Moderate: above plus mydriasis (扩瞳), cycloplegia(睫状肌麻痹);
difficulty on speaking, swallowing & urinating; and hot, red, dry skin • High: above plus ataxia(共济失调), hallucinations(幻觉) & delirium(谵妄);
bronchial tract • insensitive: uterus
(3) Inhibition of exocrine gland secretion
• salivary, sweat glands • tear, respiratory tract glands • relatively ineffective: GI tract
Regulation of K+ Channels
↓ Heart rate ↓
Moderate to high therapeutic doses : Block Post-synaptic M2 receptor → HR↑
Atropine
2. Clinical uses
(1) Ophthalmology
iris
zonule Anterior chamber Ciliary muscle (contraction)
调节麻痹
• paralysis of accommodation
•mydriasis
far sight
atropine
miosis
spasm of accommodation
near sight
• sedation, memory loss, psychosis (high dose)
Lower therapeutic doses: Block Pre-synaptic M1 receptor → ACh release↑→ activate Post-synaptic M2 receptor → HR↓
• Botulinum Toxin肉毒毒素 (blocks ACh release)
Muscarinic Antagonists
(Antimuscarinic drugs)
Tertiary amines叔胺类
Quaternary amines季胺类
阿托品 东莨菪碱 异丙托溴铵
甲硝阿托品 噻托溴铵
Atropine
(5) Antidote for organophosphate poisoning
Atropine
3. Adverse effects
(1) Side effects dry mouth, blurred vision, “sandy eyes”
(2) toxicity Lethal dose: 80~130 mg (adult), 10 mg (child)
神经系统药理2胆碱能神经系统
Muscurinic receptor antagonists
Drug classification of cholinergic antagonists
• M cholinoceptor antagonists
Atropine阿托品 (Antimuscarinic drugs)
pilocarpine
Atropine
1. Pharmacological effects
(2) Antispasmodic action on smooth muscle
• sensitive: GI, urinary bladder (spasmodic state) • relatively insensitive: bile duct, urinary tract,
• Moderate to high therapeutic doses / high vagal tone: HR↑ (tachycardia); A-V conduction ↑
• Larger doses: cutaneous vasodilatation
(5) CNS stimulation
light
1. Pharmacological effects
(1) Eye •intraocular pressure
Ciliary muscle (relaxation)
Canal of Schlemm zonule
posterior chamber Anterior chamber lens
Atropine
1. Pharmacological effects
(4) Cardiovascular System: dose dependent
• Lower therapeutic doses: HR↓(bradycardia); Blood vessels and blood pressure: no effect
prevent synechia/adhesion）
(2) Antispasmodic agent
• GI, biliary or renal colic, enuresis(遗尿)
(3) Inhibiting exocrine gland secretion
• Preanesthetic medication
(4) Bradyarrhythmia
• sinus or nodal bradycardia, A-V block
• N cholinoceptor antagonists
NN cholinoceptor antagonists: mecamylamine美加明 (Ganglionic Blocking drugs, rarely used )
NM cholinoceptor antagonists: succinylcholine琥珀胆碱 (Neuromuscular Blocking drugs )
• ห้องสมุดไป่ตู้ow: xerostomia (dry mouth); anhidrosis (dry skin), tachycardiad • Moderate: above plus mydriasis (扩瞳), cycloplegia(睫状肌麻痹);
difficulty on speaking, swallowing & urinating; and hot, red, dry skin • High: above plus ataxia(共济失调), hallucinations(幻觉) & delirium(谵妄);
bronchial tract • insensitive: uterus
(3) Inhibition of exocrine gland secretion
• salivary, sweat glands • tear, respiratory tract glands • relatively ineffective: GI tract
Regulation of K+ Channels
↓ Heart rate ↓
Moderate to high therapeutic doses : Block Post-synaptic M2 receptor → HR↑
Atropine
2. Clinical uses
(1) Ophthalmology
iris
zonule Anterior chamber Ciliary muscle (contraction)
调节麻痹
• paralysis of accommodation
•mydriasis
far sight
atropine
miosis
spasm of accommodation
near sight
• sedation, memory loss, psychosis (high dose)
Lower therapeutic doses: Block Pre-synaptic M1 receptor → ACh release↑→ activate Post-synaptic M2 receptor → HR↓
• Botulinum Toxin肉毒毒素 (blocks ACh release)
Muscarinic Antagonists
(Antimuscarinic drugs)
Tertiary amines叔胺类
Quaternary amines季胺类
阿托品 东莨菪碱 异丙托溴铵
甲硝阿托品 噻托溴铵
Atropine
(5) Antidote for organophosphate poisoning
Atropine
3. Adverse effects
(1) Side effects dry mouth, blurred vision, “sandy eyes”
(2) toxicity Lethal dose: 80~130 mg (adult), 10 mg (child)
神经系统药理2胆碱能神经系统
Muscurinic receptor antagonists
Drug classification of cholinergic antagonists
• M cholinoceptor antagonists
Atropine阿托品 (Antimuscarinic drugs)
pilocarpine
Atropine
1. Pharmacological effects
(2) Antispasmodic action on smooth muscle
• sensitive: GI, urinary bladder (spasmodic state) • relatively insensitive: bile duct, urinary tract,
• Moderate to high therapeutic doses / high vagal tone: HR↑ (tachycardia); A-V conduction ↑
• Larger doses: cutaneous vasodilatation
(5) CNS stimulation
light
1. Pharmacological effects
(1) Eye •intraocular pressure
Ciliary muscle (relaxation)
Canal of Schlemm zonule
posterior chamber Anterior chamber lens
Atropine
1. Pharmacological effects
(4) Cardiovascular System: dose dependent
• Lower therapeutic doses: HR↓(bradycardia); Blood vessels and blood pressure: no effect