Lecture

1. CHOLINERGIC BLOCKERS
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Dr Igor Khalin

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Parasympatholytics
• Eye
 inability to focus for near vision, midriasis, IOP ↑
• Saliva
 xerostomia
• Bronchi
 bronchodilation, secretion ↓
• Heart
 Rate ↑
 GIT
 secretion, peristalsis ↓ sphincter tone ↑
• Bladder
 detrusor ↓ sphincter tone ↑

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Mechanism of action
1. Competitive antagonist
2. Compete with Ach
3. Block the Ach at the
muscarinic receptors
4. As a result Ach is unable to
bind to the receptor site and
cause a cholinergic effect

4. Cholinergic Antagonists
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Antimuscarinic
agents
Neuromuscular
blockers
Atropine
Scopolamine
Ipratropium
Tropicamide
Trihexyphenidyl
Atracurium
Pancuronium
Succinylcholine
Ganglionic
blockers
Nicotine

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Pharmakokinetics
ATROPINE
1. Tertiary nitrogen
2. Good adsorbtion
3. Penetrate BBB
Atropa belladonna

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Main Effects
ATROPINE
• Smooth muscle relaxation
• Antisecretory

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Dose-dependent effects
ATROPINE

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Therapeutic uses
ATROPINE
1. Midriasis
2. Spasmolythic
3. Antisecretory
4. Mushroom poisoning
5. Organophosphates
poisoning
6. Heart block, bradycardia
7. Resuscitation (asystole)

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Adverse effects
ATROPINE

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Contraindications
ATROPINE
1. Narrow-angle glaucoma
2. Pyloric stenosis
3. Prostatic hypertrophy
4. Drivers

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Pharmakokinetics
SCOPOLAMINE
Solanaceae family
1. Tertiary nitrogen
2. Good adsorbtion
3. Penetrate BBB

12. Main Effects & Adverse Effects
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SCOPOLAMINE ATROPINE

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Therapeutic uses
SCOPOLAMINE

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Therapeutic uses
TROPICAMIDE
Eye examination

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Therapeutic uses
IPRATROPIUM
1. Bronchial asthma
2. COPD

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Therapeutic uses
TRIHEXYPHENIDYL
Parkinson’s disease

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Cholinergic Antagonists