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