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Cholinergics agonists Which mimic the action of neurotransmitter…
Cholinergics agonists
Which mimic the action of neurotransmitter acetylcholine
cholinergic receptors
mascarinic receptor
M1-found in gastric glands
M2 cardiac cells
M3-found in smooth muscle, eyes,lungs,digestive tract, exocrine glands(sweat & Salivary)
Nicotinic receptor
NM is located in the neuromuscular junction -responsible fo muscle constriction
N2 or NN located in the autonomic central nervous system Adrenal medulla - involve in transmission of cholonergics
Subtypes of mascarinic receptor
M1 and M3 are preferantially couple to the Gq-pathway
*Gq-when stimulated leads to increase in intracellular levels of calcium
*Increasing intracellular Ca²± content trigger processes such as : construction,secreatilion and nuerotransmission
M2 favor Gi-pathway
Stimulation of Gi can lead to opening of K± which in turn causes :hypoporalisation and reduction heart rate
Direct acting-mimic the effect of acetylcholine by binding to the mascarinic or nicotinic receptor
ACETYLHOLINE -have non-specific cholinergic effect.
When admitted intravenously
Decrease cardiac output,heart rate and blood pressure activities
Increases GI activity
It is available in opthalmological solutions used to produce meiosis during eye surgery
CARBAHOL-has longer duration of action as far as theraptic use
It is used to local to construct pupil during eye surgery
It also decrease intra-ocular pressure.
PILACARPINE
Act on smooth muscle of the eyes to construct the pupil.
Treat the glaucoma attack
BETHANOTHOL
stimulate urinary and gastro instestinal tracts
*Given oral and sabcutanous
Treat: urinary retention, gastrointestinal lack of mascular tone
Indirect acting agonists-increases availability of ach act cholonergic receptors.
ADROPHONIUM
Bind to acetylcholine and acetate receptors and has a very long duration of about 10-20mins
Treatment:
Used to diagnosis of myasthenia gravis -is a nueromascular disease caused by antibodies that blocks acetylcholine receptor which leads to muscle weakness
PHYSOSTIGMINE
stimulation both mascarinic and nicotinic receptor
Has a duration of about 30 2 hours
Historical was used for overdoses of anticholinergic drugs such as Atropine
rervese toic
NEOSTIGMINE
has small pores structure,it does not absorb well in GI tract
Does not enter CNS
It is used in: symptoms of myasthenia gravis
: Stimulation of bladder and GI tract
PYRIDOSTIGMINE- treatment of myasthenia gravis
Irreversible
Are extremely toxic
ECHOTHIOPHATE
acetylcholinesterase inhibitor used to increase the of intra ocular fluid.
Used to treat chronic glaucoma
Adverse effect
Broichorrhea
Miosis/muscle weakness
Urination
Diarrhoea
Bradycardia
Emests
Tacrimation
Salvation/sweating