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Cholinergics and Cholinergic Blockers

Cholinergics and Cholinergic Blockers

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Published by: api-3739910 on Oct 15, 2008
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Cholinergics and Cholinergic Blockers
I.Cholinergics / Parasympathomimetics
mimics effects of acetylcholine, stimulating PSNSA.Effects of Cholinergics at receptor sites:Muscarinic receptorNicotinic recepto
pupil constriction
bronchoconstriction
decrease HR, BP, & conduction
increase GI peristalsis & secretions
increase urinary bladder contraction, relaxurinary sphincters
uterine contraction
increase glandular secretions (sweat, tears,saliva)
erection
muscle contractionB.Inactivation of Acetylcholine
AcetylcholinesteraseC.Classification of Cholinergics/ Parasympathomimetics
I.Direct acting cholinergics
 
Muscarinic agonists
bethanechol*
carbachol
pilocarpine
metoclopramide (Reglan)Indications: Tx of urinary retention, glaucoma, & gastroesophageal refluxMOA: acts on muscarinic receptors to increase urination, constrict pupils & reduceIntraocular pressure, increase GI peristalsisCI : intestinal or urinary tract obstruction
 
 
Nicotinic agonists
NicotineMOA: stimulates nicotinic receptors at autonomic ganglia , neuromuscular junction& CNSOverdose: respiratory paralysis & cardiovascular collapse
SE & adverse reactions of direct acting cholinergics:
hypotension & bradycardia
bronchoconstriction
increase
s
alivation & secretion of gastric acid
Increase
l
acrimation
Increase
u
rination
Increase
d
efecation & abdominal cramps
II.Indirect Acting (Cholinesterase Inhibitors)
A.Reversible cholinesterase inhibitors
 Alzheimer’s disease drugs
donezepil
tacrine
rivastigmine
memantine
GalantamineMOA: blocks AChE and cross blood brain barrier thus improving memory byincreasing Ach in the brain
Myasthenia Gravis Drugs
ambenonium
edrophonium (Tensilon)
neostigmine
physostigmine
pyridostigmine *MOA: blocks AChE, thus increasing Ach at synaptic cleft and cause increase inmuscle strength & tone.
S/E of indirect acting :
Same as direct actingCaution in : bradycardia, asthma, peptic ulcer dse(PUD), hyperthyroidismCI: intestinal & urinary obstruction
 
B.Irreversible cholinesterase inhibitors
organophosphate (malathion & parathion)
nerve gasuses : insecticide , chemical weaponMOA: irreversibly bind with AChE causing excessive accumulation of Ach atreceptor sites
parasympathetic crisis & muscle paralysis
Cholinergic / Parasympathetic Crisis (DUMBBELSS)
D
iarrhea
U
rination
M
iosis
B
ronchospasm
B
radycardia
E
xcitation of skeletal muscles & CNS
L
acrimation
 
S
weating
S
alivation
II. Cholinergic Blockers/ Anticholinergics/ Parasympatholytics
block stimulating effects of Ach, blocking PSNS 
 A.Cholinergic blockers (Antimuscarinics) for GIT 
 
Atropine*
hyoscine bromide (Buscopan)
dicylcomine (Bentyl)
propantheline
glycopyrrolateIndications: antispasmodic in the Tx of peptic ulcer disease (PUD) & irritable bowelSyndrome (IBS)AtropineIndications:1.preop med to decrease salivary & respiratory secretions2. tx PUD by decreasing GI spasms & peristalsis3. tx sinus bradycardia by increasing HR4.antidote for cholinergic drug overdose5.mydriatic agentMOA: blocks Ach by occupying muscarinic receptors causing:
increase HR by blocking vagus stimulation

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