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Cholinergic Drugs
Dr Azmat Khan
Lecturer:
The University of Lahore
(Islamabad Campus)
Email:opt.azmat@gmail.com
1
Ach Synthesis: 2
Nervous system 3
Types of Cholinergic Receptors 4
Muscarinic Receptors 5
Nicotinic Receptors 6
Muscarinic Agonist
 Direct acting agonist ……. Directly act on Ach receptor
Three action ---------
1) Miosis , ( sphincter pupillae )
2) Accommodation and ( ciliary muscle )
3) Increase aqueous outflow.( longitudinal fibers of CM .. Tension on scleral
spur ….. Opening of TM .
Examples. Acetycholine
Carbachol
Pilocarpine etc
7
Acetycholine.
Acetylcholine : does not penetrate corneal epi…well ,
> rapidly degraded by acetylcholinesterase ,
>not used topically ,
>1% use in ant seg surgery Intracameral.
Note: Produce prompt and marked miosis .
8
Carbachol.
 0.01% carbachol is 100 times more effective and long lasting than Ach.
 Maximal miosis within 5 min .
 Last for 24 hr.
 An effective hypotensive drug.
9
Pilocarpine.
 0.12% used diagnostically to confirm Adie tonic pupil.
 Denervated iris exhibit , hypersensitivity and response well .
 Normal iris doe not response .
 0.25% , 0.5% upto 6% ( 4 times daily in case of POAG) and also in pt with
PACG.
 NOTE: 4% is contraindicated in acute attack of angle closure glaucoma ,,,
closing the angle.
10
SIDE EFFECT.
 MIOISIS & induce Accommodation ….. Scotopic vision, central lens opacity
, myopia , RD
 Cataractogenis …
 Miotic iris cyst .
 Other systemic adverse effect … salivation , diarrhea , urinay urgency ,
vomiting , bronchial spasm, bradycardia & diaphoresis.
11
 Miotic agent and accommodative esotropia ??
12
Muscarinic Drugs.
 Indirect acting agonist:
 Cholinesterase inhibitor . ( forming an enzyme-inhibitor complex )
 Longer duration of actions as compared to direct acting agonist .
 Twice daily treatment is sufficient.
 Reversible inhibitor ( physostigmine , neostigmine and edrophonium)
 Irrersible inhibitor ( echothiophate , diisopropyl phosphorofluoridate )
13
Con…
 The action of phosphorylating cholinesterase inhibitors can be reversed on
an acute basis by treatment with oxime containing compound like
pralidoxime .
14
Con..
 Note: pt receiving long term , irreversible cholinterase inhibitor therapy
such as echothiopate may experience toxic reaction from systemic
absorption by local anesthetic containing ester group (procaine)that are
normally inactivated by plasma cholinesterase.
 Same for succinylcholine during induction of GA …. Respiratory paralysis .
 Not combine with direct acting cholinergic agonist .
 Were use in past for treatment of lice infestation of eyelashes .
 No longer available for ophthalmic use in US.
15
Muscarinic Antagonists
 Paralysis of iris sphincter …. Unopposed action of dilator muscle, causing
pupillary dilation & same for relaxation of Accommodation.
 Uses:
 Examination of peripheral lens, CB & Retina.
 Cycloplegic refraction and Iritis
 Reduce blood-aqueous permeability , hence use in ocular inflammatory
disease.
 Examples: Atropine
Cyclopentolate ,Tropicamide
Scopolamine & Homatropine.
16
 Relive pain in case of iridocylitis.
 Treat ciliary block glaucoma.
 Note: use of these drug to dilate the pupil of pt with POAG may elevate
IOP.
17
Adverse effect:
 Local irritation with swelling.
 Conjuctival hyperemia.
 Photophobia and blurring of vision.
 Systemic effect:
especially in children are, flushing , fever, tachycardia , constipation ,
urinary retention.
Note: in mild cases only discontinuation of the drug while in severe cases IV
physostigmine.
18
Nicotinic Drugs.
 Indirect acting agonist: Edrophonium
 Use in the diagnosis fo MG.
 Nicotinic Antagonist: (neuromuscular blocking agent)
 To facilitate intubation in GA.
 Two types of anatognists,
 1) nondepolarizing agent ( gallamine & pancuronium )
 2) depolarizing agent. ( succinylcholine & decamethonium)
19
Nicotinic antagonist.
 Note: in singly innervated muscle fibers , depolarization and contraction
followed by prolonged unresponsiveness and flaccidity, while in case of
multiply innervated fiber ( one-fifth of EOM) such contractions of EOM
exert force on the globe.
 Avoid such drug in GA in operation on lacerated eyes.
20
21

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Cholinergic drugs uses in Ophthalmology

  • 1. Cholinergic Drugs Dr Azmat Khan Lecturer: The University of Lahore (Islamabad Campus) Email:opt.azmat@gmail.com 1
  • 4. Types of Cholinergic Receptors 4
  • 7. Muscarinic Agonist  Direct acting agonist ……. Directly act on Ach receptor Three action --------- 1) Miosis , ( sphincter pupillae ) 2) Accommodation and ( ciliary muscle ) 3) Increase aqueous outflow.( longitudinal fibers of CM .. Tension on scleral spur ….. Opening of TM . Examples. Acetycholine Carbachol Pilocarpine etc 7
  • 8. Acetycholine. Acetylcholine : does not penetrate corneal epi…well , > rapidly degraded by acetylcholinesterase , >not used topically , >1% use in ant seg surgery Intracameral. Note: Produce prompt and marked miosis . 8
  • 9. Carbachol.  0.01% carbachol is 100 times more effective and long lasting than Ach.  Maximal miosis within 5 min .  Last for 24 hr.  An effective hypotensive drug. 9
  • 10. Pilocarpine.  0.12% used diagnostically to confirm Adie tonic pupil.  Denervated iris exhibit , hypersensitivity and response well .  Normal iris doe not response .  0.25% , 0.5% upto 6% ( 4 times daily in case of POAG) and also in pt with PACG.  NOTE: 4% is contraindicated in acute attack of angle closure glaucoma ,,, closing the angle. 10
  • 11. SIDE EFFECT.  MIOISIS & induce Accommodation ….. Scotopic vision, central lens opacity , myopia , RD  Cataractogenis …  Miotic iris cyst .  Other systemic adverse effect … salivation , diarrhea , urinay urgency , vomiting , bronchial spasm, bradycardia & diaphoresis. 11
  • 12.  Miotic agent and accommodative esotropia ?? 12
  • 13. Muscarinic Drugs.  Indirect acting agonist:  Cholinesterase inhibitor . ( forming an enzyme-inhibitor complex )  Longer duration of actions as compared to direct acting agonist .  Twice daily treatment is sufficient.  Reversible inhibitor ( physostigmine , neostigmine and edrophonium)  Irrersible inhibitor ( echothiophate , diisopropyl phosphorofluoridate ) 13
  • 14. Con…  The action of phosphorylating cholinesterase inhibitors can be reversed on an acute basis by treatment with oxime containing compound like pralidoxime . 14
  • 15. Con..  Note: pt receiving long term , irreversible cholinterase inhibitor therapy such as echothiopate may experience toxic reaction from systemic absorption by local anesthetic containing ester group (procaine)that are normally inactivated by plasma cholinesterase.  Same for succinylcholine during induction of GA …. Respiratory paralysis .  Not combine with direct acting cholinergic agonist .  Were use in past for treatment of lice infestation of eyelashes .  No longer available for ophthalmic use in US. 15
  • 16. Muscarinic Antagonists  Paralysis of iris sphincter …. Unopposed action of dilator muscle, causing pupillary dilation & same for relaxation of Accommodation.  Uses:  Examination of peripheral lens, CB & Retina.  Cycloplegic refraction and Iritis  Reduce blood-aqueous permeability , hence use in ocular inflammatory disease.  Examples: Atropine Cyclopentolate ,Tropicamide Scopolamine & Homatropine. 16
  • 17.  Relive pain in case of iridocylitis.  Treat ciliary block glaucoma.  Note: use of these drug to dilate the pupil of pt with POAG may elevate IOP. 17
  • 18. Adverse effect:  Local irritation with swelling.  Conjuctival hyperemia.  Photophobia and blurring of vision.  Systemic effect: especially in children are, flushing , fever, tachycardia , constipation , urinary retention. Note: in mild cases only discontinuation of the drug while in severe cases IV physostigmine. 18
  • 19. Nicotinic Drugs.  Indirect acting agonist: Edrophonium  Use in the diagnosis fo MG.  Nicotinic Antagonist: (neuromuscular blocking agent)  To facilitate intubation in GA.  Two types of anatognists,  1) nondepolarizing agent ( gallamine & pancuronium )  2) depolarizing agent. ( succinylcholine & decamethonium) 19
  • 20. Nicotinic antagonist.  Note: in singly innervated muscle fibers , depolarization and contraction followed by prolonged unresponsiveness and flaccidity, while in case of multiply innervated fiber ( one-fifth of EOM) such contractions of EOM exert force on the globe.  Avoid such drug in GA in operation on lacerated eyes. 20
  • 21. 21