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Cholinergic Drugs
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Cholinergic receptors:
Muscarinic
1, 2, 3
Niocotinic
(Nn and Nm)
Murscarinic receptors
1 GIT
2 heart
3 Smooth muscle in the eyes and lungs
Cholinergic Agonists: Direct Acting
Acetylchonine
Carbechol
Pilocarpine
Betanechol
Drug of choice for Glaucoma
Pilocarpine
- they decrease the
intra-ocular
pressure (
constricting
= draining of fluids)
Betanechol
Px
suffering from
urinary
retention
Indirect acting agonists ( target / inhibit enzymes Ache) :
Reversible
Edrophonium
Physostigmine
Neostigmine
Pyridostigmine
Edrophonium
is used to diagnosed
Myasthenia Gravis
Tensilon's
test
Antidote for
Reversible
Agonist toxicity is
Atropine
Alzheimers
Tacrine
Galantamine
Donepezil
Rivastigmine
Irreversible
(prolonged effect)
Military
Sarin
Tabun
soman
Irreversible :
Insecticides
Parathion
malathion
Irreversible : caused
DUMBELLS
EFFECTS
IRREVERSIBLE DRUG CAUSE MIOSIS
ecothiophate
Cholinergic Antagonist :
Antimuscarinic
Agents: Non selective
Atropine = caused
blurred
vision
Cyclopentolate
Tropicamide
Scopolamine =
motion
sickness
Atropine caused
ALICE
in Wonderland effect
From Atropa
Belladona
Cholinergic Antagonists : Non selective promote urinary retention
Tolterodine
Fesoterodin
Darifenacin
Solifenacin
Oxybutinin
Trospium
Cholinergic Antagonists : Non selective
Asthma
and COPD
Ipatropium
Tiotropium
Ganglionic Blockers
Nicotine
=
increase
in HR and BP but still leads to CNS
depression
Neuromuscular Blockers : Nondepolarizing
Cisatracurium
Pancuronium
Rocuronium
Vecuronium
Atracuronium
Cisatracurium
Pancuronium
90
minutes
Rocuronium
Vecuronium
Atracuronium
40
minutes
Neuromuscular Blocker
:
Depolarizing
Succinylcholine
Phase 1
:
Binds to the
nicotinic
receptors that leads to entrance of
sodium
and release of
calcium
leading to muscle
contraction.
Phase
2
Resistant to
Ache prolonged
binding and leading to
desensitization
of the receptors