Cholinergic drugs act at cholinergic receptors in the autonomic nervous system and central nervous system. They include acetylcholine and cholinomimetics that act as agonists at muscarinic and nicotinic receptors. Anticholinesterases inhibit the enzyme acetylcholinesterase and increase the level and duration of action of acetylcholine. They are used to treat myasthenia gravis and Alzheimer's disease. Organophosphate poisoning causes inhibition of acetylcholinesterase and cholinergic excess that is treated with atropine and pralidoxime. Pilocarpine is used as a miotic in glaucoma by stimulating muscarinic receptors in the eye
cholingeric and Anticholinesterase drug in detail .this ppt contains introduction ,mechanism of action ,pharmacological action ,uses and adverse effect of the drug
cholingeric and Anticholinesterase drug in detail .this ppt contains introduction ,mechanism of action ,pharmacological action ,uses and adverse effect of the drug
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The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
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7. Heart
↓HR ↓ AV conduction
↓ atrial contractility
Cholinergic effects
M2receptor
Blood Vessels – M3 – Vasodilatation
BUT
Very few vessels supplied – skin of face & neck
8. Muscarinic
action
EYE
M3-
• contraction of circular fibers : Miosis
• Contraction of cilliary muscles
-- spasm of accommodation
(cyclospasm )
Vision fixed for near subjects
• Improving patency of trabeculae
- outflow of aqueous humor increases
IOP - decrease Use in GLAUCOMA
- Pilocarpine
9. • The iris is composed of two types of muscle fibres, the
circular and the radial. The stimulation of
parasympathetic cholinergic nerve supplying circular
fibbers results into contraction of pupil called miosis.
The stimulation of sympathetic adrenergic nerve
supplying the radial fibres results into dilatation of
pupil called mydriasis. Thus the iris regulates the size of
pupil.
• The ciliary muscle is innervated by parasympathetic
cholinergic nerves. Its contraction reduce the focal
length of lens causing accommodation for near vision.
10. Muscarinic action
GIT – peristalsis ↑ - defecation
Use –
Post operative paralytic ileus
Urinary tract
sphincter relax
detrusor contract
voiding of bladder
urination
Bronchoconstriction – c/i in Asthma , COPD
Use – Post Op urinary retention
12. Cholinergic Agonists
ACh -- rapid degradation by ChEs – not used
Methacholine - - Muscarinic action > Nicotinic action
Carbachol - - resistant to ChEs M + N action
Bethanachol - resistant to ChE - Muscarinic action -
git + bladder
- used in Rx of POp urinary retention
Pilocarpine - alkaloid - marked secretary effect
IOP ↓ ---- Used in Glaucoma
14. Anionic site Esteratic site
Normal ACh
hydrolysis by ChE
very fast reaction
within milliseconds
ACh + ChE
↓
complex
↓
Choline + Acetylated E
↓ H2O
Choline + Acetic acid + E
15.
16. Anionic site Esteratic site
REVERSIBLE
Inhibitors
Combines with BOTH sites
carbamylated enzyme
Hydrolysis --- SLOW
ACh action prolonged
Structure similar to ACh
Effect 3- 4 hrs
17. Reversible – antiChEs
Carbamates
Physostigmine – natural alkaloid
Neostigmine Pyridostigmine
Rivastigmine
Donepazil
Galantamine
Alzheimer's disease
E drophonium – E xception
binds ONLY to anionic site – rapid renal elimination
action for 10 mins
18. Anionic site Esteratic site
IRREVERSIBLE
Inhibitors
Combines with
esteratic site
Phosphorylated enzyme
But Hydrolysis --- very very
SLOW
ACh action prolonged
Effects depend upon
regeneration of
new enzymes
19. Anionic site Esteratic site
IRREVERSIBLE
Inhibitors
Combines with
esteratic site
Phosphorylated enzyme
But Hydrolysis --- very very
SLOW
ACh action prolonged
Effects depend upon
regeneration of
new enzymes
20. Dyflos , Parathion , Malathion - insecticide
Tabun , Soman – gas
IRREVERSIBLE Anti ChEs
Carbamate - Propoxur
21. Anionic site Esteratic site
IRREVERSIBLE
Inhibitors
Phosphorylated enzyme
Hydrolysis
--- total resistance
Loss of alkyl group
AGING
process
22. Uses
Myasthenia Gravis
Autoimmune disorder
Antibody against Nm receptor - ↓ no of receptors
Weakness , Easy fatigability
Neostigmine / Pyridostigmine
ACh level ↑ + direct action on muscle end plate
But One Problem
Overtreatment with Anti ChEs
Causes persistent depolarization – WEAKNESS –
= cholinergic crisis
23.
24. Myasthenia Gravis
Crisis = acute worsening of symptoms
Myasthenic Crisis
= Worsening of disease
Cholinergic crisis
= overdose of Anti ChE
Edrophonium – IV 2 mg
Shortest acting Anti ChE
Improvement Worsening
25. Diagnosis
Ameliorative test:
• Edrophonium 2 mg is injected i.v. as a test
dose
• Nothing untoward happens, the remaining 8
mg is injected after 30–60 sec.
• Reversal of weakness and shortlasting
improvement in the strength
26. • Provocative test:
• Demonstration of anti-NR antibodies in
plasma or muscle biopsy specimen
27. Other drugs
• Corticosteroids
• Immunosuppressant action
• Inhibit production of NR-antibodies and may
increase synthesis of NRs
• Dose:30-60mg/day
• Other immunosuppressant: cyclosporin,
azathiopyrine
• Thymetomy
• Plasmapheresis
30. increase the tone of Cilliary muscle + iris sphincter
Pores of the canal of Schlemm open
↓
Facilitate Aqueous Humor drainage – through Trabecular pathway
↓
IOP decrease in OPEN ANGLE GLAUCOMA
PILOCARPINE
– is preferred 2nd / 3rd choice drugs
Use
Glaucoma
31. Other uses
• Post operative paralytic ileus:Neostigmine
• Post operative urinary retention
Neostigmine to be used
• Post operative decurarization
Neostigmine
• Cobra bite - curare like effect --
– Neostigmine +Atropine prevent respiratory paralysis
• Atropine overdose -- Physostigmine
32. Other uses
Other drug overdosages
• Tricyclic antidepressants, phenothiazines
• Additional anticholinergic property
33. Organophosphrus poisoning
• Easily available
• Extensively used as agricultural and household
insecticides
• Accidental as well as suicidal and homicidal
poisoning is common.
• Local muscarinic manifestations at the site of
exposure (skin, eye, g.i.t.) occur immediately
34. S alivation
L acrimation
U rination
D efecation
G I upset
E mesis
Miosis
blurred vision
Bradycardia
fall in BP
muscle weakness
paralysis
Tremor
Convulsion
Coma .. death
ORGANOPHOSPHATE poisoning
SLUDGE
35. General measures
Termination of further exposure to the
poison—
• fresh air,
• Wash the skin and mucous membranes with
soap and water,
• Gastric lavage according to need
Maintain patent airway, positive pressure
respiration
37. Specific antidote
Atropine
• Highly effective in counteracting the
muscarinic symptom
• Higher doses are required to antagonize the
central effects
• Does not reverse peripheral muscular
paralysis
Atropine 2 mg i.v. repeated every 10 min till dryness of
mouth or other signs of atropinization appear
39. Anionic site Esteratic site
ChE
OXIMES
PRALIDOXIME = cholinesterase REACTIVATOR
NOT effective for Carbamate poisonings
IMP for skeletal mucle symptoms
40. Physostigmine Neostigmine
Source Natural alkaloid Synthetic
Chemistry Tertiary amine derivative Quaternary ammonium
compound
Oral absorption Good Poor
CNS actions Present Absent
Applied to eye Penetrates cornea Poor penetration
Direct action on NM
cholinoceptors
Absent Present
Important use Miotic Myasthenia gravis
41. MCQ
• Cholinomimetics are not used in
• (a) Glaucoma
• (b) Myasthenia gravis
• (c) Post operative atony
• (d) Partial heart block
42. • A patient presents to emergency with
pinpoint pupil, salivation, lacrimation,
tremors and red tears. Plasmacholinesterase
level was 30% of normal. Most probable
Diagnosis is:
• (a) Organophospahte poisoning
• (b) Dhatura poisoning
• (c) Opioid poisoning
• (d) Pontine hemorrhage
43. • Which of the following cranical nerve does
not contain parasympathetic motor (GVE)
fibers?
• (a) III
• (b) VI
• (c) IX
• (d) X
44. • Major neurotransmitter released at end
organ effectors of the sympathic division of
the autonomic nervous system is:
• (a) Adrenaline
• (b) Noradrenaline
• (c) Dopamine
• (d) Acetylcholine
45. • Mechanism of action of pralidoxime is:
• (a) Stimulation of ACh receptors
• (b) Inhibition of breakdown of ACh
• (c) Blockade of ACh receptors
• (d) Reactivation of AChE enzyme
46. • Dr Sunil used edrophonium for differentiating
myasthenic crisis from cholinergic crisis. He
preferred it over other anticholinesterase
agents because of its:
• (a) Shorter duration of action
• (b) Longer duration of action
• (c) Direct action on muscle end plate
• (d) Selective inhibition of true cholinesterase
47. • All of the following effects are seen with
cholinergic muscarinic receptor stimulation
except:
• (a) Sweating
• (b) Rise in blood pressure
• (c) Bradycardia
• (d) Urination
48. • A patient Raj Kishore was given pilocarpine.
All of the following can be the features seen
in him except:
• (a) Sweating
• (b) Salivation
• (c) Miosis
• (d) Cycloplegia
49. • Which of the following provides the best
explanation for neostigmine being preferred
over physostigmine for treating myasthenia
gravis?
• (a) It is better absorbed orally
• (b) It has longer duration of action
• (c) It has additional direct agonistic action on
nicotinic receptors at the muscle end plate
• (d) It penetrates blood brain barrier
50. • Which of the following properties make
pyridostigmine different from neostigmine?
• (a) It is more potent
• (b) It is longer acting
• (c) It produces less muscarinic side effects
• (d) It does not have any direct action on NM
receptors
Edrophonium – shortest
Test Help in differentiating Cholinergic Crisis or Myasthenic Crisis
Inject → if improvement - - Myasthenic Crisis
↓
if worsening - - Cholinergic crisis
Edrophonium action – 10 -20 mins
Edrophonium test for differentiating CRISIS in Myasthenia Gravis
Crisis in Myasthenia are of 2 types
Myasthenic Crisis= Worsening of disease
2 . Cholinergic crisis
= overdose of Anti ChE
To differentiate that Edrophonium is given IV = Shortest acting Anti ChE
If improvement occurs --- Myasthenic Crisis
If worsening occurs -- Cholinergic Crisis ( dose of Neostigmine / Pyridostigmine has to be reduced )
S alivation L acrimation U rination D efecation G I upset E mesis
SLUDGE + Miosis
At toxic dose Bradycardia fall in BP muscle weakness paralysis
Tremor Convulsion Coma .. death
Specific antidote - Atropine
In case of OP poisoning
Pralidoxime -- ChE reactivator to restore transmission at Neuromuscular junction
Not used in Carbamate overdose
Atropine is virtually without effect against the peripheral neuromuscular compromise
