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Shivansh Pande Clinical Pharmacist Apollo Hospitals, Jubilee Hills, Hyderabad

Anticholinesterases are drugs that inhibit the enzyme acetylcholinesterase, preventing the breakdown of acetylcholine at nerve endings. They are classified as reversible or irreversible, and include carbamates, organophosphates, and acridines. Anticholinesterases have pharmacological actions similar to direct cholinoreceptor stimulants, causing both muscarinic and nicotinic effects throughout the body. Their uses include treatment of glaucoma, myasthenia gravis, postoperative ileus, as an antidote for cobra bite and belladonna poisoning, and for Alzheimer's disease. Overdose of anticholinesterase pesticides can cause severe symptoms requiring supportive care and ant

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140 views12 pages

Shivansh Pande Clinical Pharmacist Apollo Hospitals, Jubilee Hills, Hyderabad

Anticholinesterases are drugs that inhibit the enzyme acetylcholinesterase, preventing the breakdown of acetylcholine at nerve endings. They are classified as reversible or irreversible, and include carbamates, organophosphates, and acridines. Anticholinesterases have pharmacological actions similar to direct cholinoreceptor stimulants, causing both muscarinic and nicotinic effects throughout the body. Their uses include treatment of glaucoma, myasthenia gravis, postoperative ileus, as an antidote for cobra bite and belladonna poisoning, and for Alzheimer's disease. Overdose of anticholinesterase pesticides can cause severe symptoms requiring supportive care and ant

Uploaded by

shivanshpande
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPTX, PDF, TXT or read online on Scribd
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Shivansh Pande Clinical Pharmacist Apollo Hospitals, Jubilee Hills, Hyderabad

4/13/2012 1

What are Anticholinesterases?


Anticholinesterases or cholinesterase inhibitors (anti

AChEs) effectively inhibit the enzyme acetylcholinesterase so that it is unable to hydrolyze Ach, and thus preserve Ach at nerve ending.
Their action is indirect.

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Classification
Reversible a) Carbamates
Physostigmine
Neostigmine Pyridostigmine Edrophonium Rivastigmine

Irreversible a) Organophosphates
Dyflos (DFP)
Echothiophate Parathioni Malathioni Tabun# Sarin# Soman#

b) Acridine
Tacrine

b) Carbamates
Carbaryli Propoxuri

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Anti AChEs are chemically esters of


Carbamic Acid

Phosphoric Acid

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Pharmacological Actions
Action similar to that of direct cholinoreceptor

stimulants.
Lipid Soluble (physostigmine, Organophos.) : muscarinic, CNS effect. Lipid insoluble (neostigmine, Q A compounds) : nicotinic, skeletal muscle

effect.

Ganglia: CVS:

Stimulant action > muscarinic receptors High dose > transmission blockade Muscarinic > HR, BP Nicotinic > HR, BP Result: Unpredictable

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Skeletal Muscles:
Nerve impulseAch accumulatesstimulates neighbouring

receptorsrepetitive firingtwitching and fasciculations. High DosePersistant depolarisationweakness and paralysis

Other effects: Similar to direct acting drugs

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Pharmacokinetics
Lipid Soluble (physostigmine, organophos): Rapidly

absorbed from GIT, skin lungs etc.

Lipid Insoluble (neostigmine etc.): Poorly absorbed

orally or through cornea.

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Uses/Indications
As Miotic
In glaucoma Counteract the effects of mydriatics in refraction testing. Prevent adhesions between iris and lens.

Myasthenia Gravis (Neostigmine)


Autoimmune disorder Antibodies to nicotinic receptors at muscle

end plate damage at NMJ weakness and fatigue Treatment balanced with atropine Overtreatment with AChE weakness, persistant depolarisation cholinergic weakness

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Post-operative paralytic ileus/ urinary obstruction Postoperative decurarization:


Reverses muscular paralysis due to competitive neuromuscular blocker.

Cobra Bite: (Neostigmine+Atropine) Belladonna poisoning: Physostigmine Other drug overdosages: (Physostigmine)
Tricyclic antidepressants, phenothiazines, antihistaminics, etc.

Alzheimers Disease: (cerebroselective antiChE: Tacrine,

rivastigmine, donepezil)
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Anticholinesterase Poisoning
Agricultural and household insceticides.
Accidental or suicidal poisoning is common.

Symptoms
Irritation of eye, lacrymation, salivation, sweatiing, tracheo-

bronchial secretions, miosis, blurring of vision, breathlessness, colic, involuntary defecation, urination. BP, HR, cardiac arrhythmias, vascular collapse Fasciculations, weakness, respiratory paralysis. Excitement, ataxia, convulsions, coma, death (respiratory failure)

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Treatment Wash skin and mucous membranes with water, gastric lavage if necessary. Maintain airway, positive lung pressure, assisted respiration. Maintain BP, hydration, convulsions. Use Specific antidotes:

Atropine: Counteracts muscarinic symptoms Higher doses counteracts central effects Does not reverse muscular paralysis (nicotinic action) Cholinesterase reactivators: (pralidoxime) Reactivates blocked cholinesterase sites
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4/13/2012

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