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Cholinergic Agents PP

Cholinergic agents act on the parasympathetic nervous system by stimulating cholinergic receptors. They can be direct-acting agonists that bind to muscarinic and nicotinic receptors, or indirect-acting agents that inhibit the enzyme acetylcholinesterase and increase the availability of acetylcholine. Cholinergic agents are used to treat glaucoma, urinary retention, myasthenia gravis, Alzheimer's disease, and to reverse neuromuscular blocking agents or anticholinergic poisoning. Anticholinergic drugs block muscarinic receptors in the parasympathetic nervous system and are used to treat irritable bowel syndrome, asthma, Parkinson's disease, and for their effects on the

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194 views13 pages

Cholinergic Agents PP

Cholinergic agents act on the parasympathetic nervous system by stimulating cholinergic receptors. They can be direct-acting agonists that bind to muscarinic and nicotinic receptors, or indirect-acting agents that inhibit the enzyme acetylcholinesterase and increase the availability of acetylcholine. Cholinergic agents are used to treat glaucoma, urinary retention, myasthenia gravis, Alzheimer's disease, and to reverse neuromuscular blocking agents or anticholinergic poisoning. Anticholinergic drugs block muscarinic receptors in the parasympathetic nervous system and are used to treat irritable bowel syndrome, asthma, Parkinson's disease, and for their effects on the

Uploaded by

محمد علي حميد
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

Cholinergic agents

Cholinergic agents
• Drugs that stimulate the parasympathetic
nervous system (PSNS).
• Also known as cholinergic agonists or
parasympathomimetics.
• Acetylcholine is neurotransmitter.
• Cholinergic agents produce effects similar
to acetylcholine.
Cholinergic Receptors:
Muscarinic receptors (M1, M2, M3, M4,
M5).
Nicotinic receptors.
Mechanism of Action
• Direct-acting (agonist): Bind to cholinergic
receptors, causing stimulation like bethanecol and
pilocarpine.

• Indirect-acting: Inhibit the enzyme “cholinesterase”


• Result: more ACh is available at the receptors
• Reversible: Bind to cholinesterase for a period of
minutes to hours like physostigmine, neostigmine,
• Irreversible: Bind to cholinesterase and form a
permanent covalent bond like parathion, malathion,
sarin
• The body must make new cholinesterase
Clinical indication:
1- Reduce intraocular pressure, Useful for glaucoma and
intraocular surgery (pilocarpine).
2- Urinary retention and inadequate emptying of the
bladder when organic obstruction is
absent(bethanechol).
3- Used for diagnosis and treatment of myasthenia
gravis (Neostigmine, Edrophonium).
4- Used in the treatment of mild to moderate
Alzheimer’s disease.
5- Used to reverse neuromuscular blocking agents.
6- Used to reverse anticholinergic poisoning (antidote)
Anticholinergic drugs
• Muscarinic Receptor Antagonist,
Parasympatholytics, Cholinolytics , Atropine-like
Drugs.
• Drugs that block or inhibit the actions of
acetylcholine (ACh) in the parasympathetic
nervous system.
• Atropine, the prototype drug of this class.
• Block ACh at the muscarinic receptors in the
PSNS.
• Most anticholinergic drugs interact with
the muscarinic receptors in the brain,
secretory glands, heart, and smooth
muscle.
• Affects the heart, resp. tract, GI tract,
bladder, eye, & exocrine glands.
Clinical indications:
•Helpful in treating irritable colon or
colitis.(Mebeverine).
• Useful in gastritis and ulcerative colitis as they slow
motility.
•CNS disorders: Scopolamine and hyoscine are
effectively used in the treatment of nausea, vomiting
and motion sickness.
• In organophosphorus poisoning.(Atropine).
•On CVS: Atropine is used for counteracting
bradycardia and partial heart block.
• As mydriatic agent for examinations and
surgery.(Atropine).
• Used in the treatment of (COPD) and asthma.
(Ipratropium bromide).
• Parkinson’s Disease.
Adverse effects:
• dry mouth
• blurred vision
• tachycardia
• urinary retention
• constipation.
• Effects on the CNS include restlessness,
confusion, hallucinations, and delirium,
which may progress to depression

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