Parasympathetic / Cholinergic Flashcards
Cholinergic transmission steps
Synthesis Storage in vesicles Release Binding to receptor Degradation of acetylcholine Recycling of choline
Carries choline from extracellular to pre-synaptic region
Na-dependent transporter
Process in synthesis
Enzyme
Product
Acetylation
Choline acetyltransferase
Acetylcholine
Inhibits transporter, uptake of acetylcholine
Vesamicol
Inhibits transport of choline to the pre-synaptic region
Hemicholinum
Blocks release of acetylcholine
Decreased neurotransmitter
Decreased muscle contraction
Paralysis
Botulinum toxin
Cholinoceptors
Muscarinic
Nicotinic
M1
E - exocrine glands
A - autonomic glands
C - CNS
M2
HCSP Heart CNS Smooth muscle Peripheral nerve
M3
ESEBC Exocrine glands Smooth muscle Eye Blood vessel CNS
M4
CNS
Enhanced locomotion
M5
CSI
CNS
Salivary glands
Iris
NN
Ganglion - stimulation
CNS - neurotransmisson
NM
Skeletal muscle - contraction
Subtypes of cholinergic agonists
DIRECT
Indirect
DIRECT acting cholinergic agonists
Choline esters
Alkaloids
Choline esters
Acetylcholine
Bethanechol
Carbachol
Methacholine / provocholine
Most potent cholinergic agonist
Cause 10-Min miosis during cataract surgery
Lack of selectivity
Acetylcholine
Strong muscarinic activity
Increase intestinal motility after surgery
Bethanechol
Ester of carbamic acid
Carbachol
For open angle glaucoma that is resistant to pilocarpine
Carbachol
Weak nicotinic activity
Diagnosis of asthma
Methacholine
What should be given after the methacholine test
Rapid-acting bronchodilator
DOC for glaucoma
Can Cross blood brain barrier
Pilocarpine
No therapeutic use
Muscarine
Has muscarinic and nicotinic activity
Potential for Alzheimer’s
Arecholine
Indirect-acting cholinergic agonists /
Cholinesterase inhibitors
Organophosphates
Carbamates
Quaternary amines
DFP Keana
Diisopropylfluorophosphate
Organophosphates
Isofluorophate
Echothiophate
Malathion, parathion
Tabon, sarin, soman
Chronic treatment of open-angle glaucoma
Duration 1 week
Isofluorophate
Open angle glaucoma
3-7 days
Echothiophate
Insecticides / Pesticides
No clinical use
Active metabolites: malaoxon, paraoxon
Malathion, parathion
Phospholine Iodide
Echothiophate