8/17/2019 Choli No Mime
1/32
CHOLINOMIMETI
CS
8/17/2019 Choli No Mime
2/32
8/17/2019 Choli No Mime
3/32
Parasympatheic
system
Neurotransmitter
Acetylcholine
Receptors
Muscarinic
Nicotinic
8/17/2019 Choli No Mime
4/32
Acetylcholine
8/17/2019 Choli No Mime
5/32
Receptors
Muscarinic
Nicotinic
8/17/2019 Choli No Mime
6/32
8/17/2019 Choli No Mime
7/32
Cholinomimetics are
that mimic action ofacetylcholine (Ach) atrecetors
!irectly Indirectly
8/17/2019 Choli No Mime
8/32
8/17/2019 Choli No Mime
9/32
CLASSIFICATION
DIRECTYLY ACTINC!OLINOMIMETICS
Choline
esters
AcetylcholineMethacholine
CarbacholBethanechol
Cholinom
tical"aloi#
MainlyMuscariAgonis
MainlyNicotinAgonis
8/17/2019 Choli No Mime
10/32
CLASSIFICATION
Mainly MuscarinicA$onists
•Natural Al"aloi#s•Muscarine•"ilocarine
•Arecholine
•Synthetic Al"aloi#•O#otremorine•Aceclidine
•Cer$imiline
8/17/2019 Choli No Mime
11/32
CLASSIFICATION
•Mainly Nicotinic A$o
•Natural Al%aloids•Nicotine
•Lo&eline
•Synthetic Al%aloids•!imethylhenylierazPP)
8/17/2019 Choli No Mime
12/32
P ! A
R M A C O % I
N T
I C S
Cholineesters
• 'uarternary amine• esistant to hydro
esterase
Choline
al%aloids •
Tertiary amines
8/17/2019 Choli No Mime
13/32
8/17/2019 Choli No Mime
14/32
MSCAINIC
ACTIONS
8/17/2019 Choli No Mime
15/32
EYEM* recetors
uillary constrictor mu
ciliary muscle
lacrimal gland
8/17/2019 Choli No Mime
16/32
Ciliary &o#yM'
PupillaryconstrictorM'
M'
8/17/2019 Choli No Mime
17/32
M'
8/17/2019 Choli No Mime
18/32
8/17/2019 Choli No Mime
19/32
8/17/2019 Choli No Mime
20/32
L(NS
+ronchoconstriction
tracheo&ronchial secretions
8/17/2019 Choli No Mime
21/32
ASTROINTESTINAL TRA
M* recetor
amlitude of contra
rela# shincter
secretions
8/17/2019 Choli No Mime
22/32
(RINARY TRACT M* recetors
contraction of detrusor
rela#ation of shincter
8/17/2019 Choli No Mime
23/32
!EARTM, (heart)- M* (&lood $essels) heart rate
conduction through A. node
force of contraction
$asodilation
SA no#eA) no#eAtria *+entricles
8/17/2019 Choli No Mime
24/32
CNS
+rain is rich in M / SC in N recetors
Acti$ation of M0 111 slo2 e#citation of neuron
•Imortant role in cogniti$e function secially
"re1senile dementia of Al3heimer tye 1111lossneurons4
8/17/2019 Choli No Mime
25/32
NICOTINIC
ACTIONS
8/17/2019 Choli No Mime
26/32
Autonomic ganglia - Adremedulla
N4M 45unction Central Ner$ous System
8/17/2019 Choli No Mime
27/32
T!ERAPE(TICAPPLICATIONS(MSCAINIC)
Ohthalmology ("ilocarine) Miotic agent 6laucoma
7erostomia ("ilocarine
S8orgen9s syndrome ("ilocarine)
Increase gastrointestinal motility(+ethanechol)
rinary retention(+ethanechol)
!iagnosis of &ronchial air2ay rea(Methacholine)
8/17/2019 Choli No Mime
28/32
T!ERAPE(TICAPPLICATIONS
(NICOTINIC)
!irect1acting nicotinic agonis
no theraeutic alications esmo%ing cessation
.arenicline is a ne2er nicotinagonist 2ith artial agonist
roerties4 It aears to reducra$ing in ersons addicted tnicotine
Cramps and diarrhea(rination (!etrusor contraction and S
8/17/2019 Choli No Mime
29/32
AD)ERSEEFFECT
S
(rination (!etrusor contraction and Srela#ation) Urinary frequency
Muscle (S%eletal) e#citationTwitchings and fasciculations
,ronchosasm Shortness of breathe (Dyspnea)!eart &radycardia and reduced contraconducti$ity Bradycardia
Autonomic ganglia stimulation)ascular dilation (hyotenstion)Hypotension
Eye miosis and accomodation sasm Blurred ision
Secretions increase (lacrimation- s2ea6I secretions) increased sweating and saliation
Stimulation follo2ed &y deression in
8/17/2019 Choli No Mime
30/32
M(S!ROOMPOISONIN
• Signs of muscarinic e#cess1
sali$ation- s2eating- nausea-
$omiting-diarrhea-$isual
distur&ances- headache- a&d4
urinary urgency- &radycardia-
&ronchosasm- hyotension- s
• Atroine (01,mg I:M e$ery *;m
8/17/2019 Choli No Mime
31/32
AC(TENICOTINETO-ICITY
A4 CNS stimulation- causecon$ulsions- coma and
resiratory arrest4
+4 S%eletal muscle deolari3aand resiratory aralysis4
C4 Hyertension and cardiacarrhythmia
8/17/2019 Choli No Mime
32/32
CONTAIN!ICATIONS
• +ronchial asthma
• ecent myocardial infarction
• Coronary insu