CENTRAL NERVOUS SYSTEM

CHOLINERGIC AGENTS

“REST AND DIGEST”

Objectives
• Biosynthesis of Acetylcholine
• Cholinergic Agonists (Basic Structure)
Parasympathomimetic Drugs
• Cholinergic Antagonists (Basic Structure)
Parasympatholytic Drugs
BIOSYNTHESIS OF ACETYLCHOLINE
CHOLINERGIC BASIC STRUCTURE
CENTRAL NERVOUS SYSTEM
PARASYMPATHOMIMETIC
AGENTS

“REST AND DIGEST”

• Direct-Acting
Choline Esters
Cholinergic Alkaloids
• Indirect-Acting
• Short acting anti-cholinesterase
Carbamates
Organophosphates
Alzheimer’s Disease
• Choline Esters
Acetylcholine
Bethanechol
Methacholine
Carbachol

• Cholinergic Alkaloids
Pilocarpine
Arecoline
Lobeline
Muscarine
• Short-acting anticholinesterase
Edrophonium – diagnostic agent for Myasthenia Gravis

Carbamates
Neostigmine – ax. For Tubocurarine poisoning
Physostigmine (aka Eserine) – reversal of severe Atropine poisoning
Pyridostigmine
• Organophosphate
Ecothiophate
Malathion
Parathion

• Alzheimer’s Disease
Rivastigmine
Tacrine
Donepezil
CENTRAL NERVOUS SYSTEM
PARASYMPATHOLYTICS
AGENTS

“REST AND DIGEST”

• Anti-muscarinic
CNS-acting
Mydriatic-Cycloplegic
Bronchodilator
Hyperacidity
GIT & Urinary bladder hyperactivity

Anti-nicotinic
Neuromuscular blockers
Ganglionic blockers
• CNS-acting
Scopolamine
Biperiden
Benztropine
Trihexyphenidyl

• Mydriatic-Cycloplegic
Atropine (aka Hyoscyamine) – DOC for Cholinergic toxicity
Homatropine
Tropicamide
Cyclopentolate
• Bronchodilator
Ipatropium
Oxytropium
Tiotropium

• Hyperacidity
 Pirenzepine
 Telenzepine

• GIT & Urinary bladder hyperacidity

 Dicycloverine
 Glycopyrrolate
 Hyosine-N-butylbromide
• Neuromuscular Blockers
Succinylcholine
Atracurium (Isoquinolines der.)
Pancuronium (Steroidal der.)

• Ganglionic Blockers
Hexamethonium
Mecamylamine
Trimethaphan camsylate

• Regenerator
Pralidoxime – DOC for Organophosphate poisoning
-end-