Autonomic & NMJ Pharmacology Flashcards
What are the nicotinic receptors and where are they?
N1 (ganglia)
N2 (NMJ)
What are the muscarinic receptors and where are they?
M1 (neronal)
M2 (cacrdiac and presynaptic)
M3 (smooth muscle and glands)
What are the alpha receptors?
A1
A2
What are the beta receptors?
B1
B2
B3
What receptors are ionotropic?
Nicotinic
What receptors use G proteins?
All of them apart from nicotinic, which is ionotropic
What receptors do most drugs not distinguish between?
Sub classes of:
muscarinic
alpha
beta
What is the typical process of synaptic transmission?
- Synthesis and packaging of neurotransmitter into synsynaptic terminal
- Na+ action potential invades terminal
- Depolarise and activates voltage gated Ca2+ channels
- Triggers Ca+ dependent exocytosis of vesicles of transmitter
- Transmitter difuses across synaptic cleft and binds to receptor to provide a post synaptic response
- Presynaptic autoreceptors inhibit further transmitter release
- Transmiter is inactivated by uptake into glia or neurones
- Transmitter is metabolised within cells
What are potential sites of action for pharmacology of the NMJ?
Inhibit choline transporter
Block voltage gated Ca2+ channels
Block vesicle fusion
Non polarising nicotinic receptor blocker
Depolarising nicotinic receptor blocker
Prolong the action potential
Block acetylcholinesterase
What are some clinical applications of pharmacolgy at the NMJ?
Non polarising or depolarising blockers used for paralysis during surgery, electroconvulsive therapy or controlling spasms in tetanus
Botulinum toxin used for treating muscle spasms or cosmetic procedures
Anti cholinesterase used for treating myasthenic syndrome, reversing action of non depolarising blocker or countering botulinum poison
Where could pharmacology of the ANS be at?
Ganglionic transmission
Post ganglionic sympathetic transmission
Post ganglionic parasympathetic transmission
What are potential sites of action for ganglionic transmission?
Inhibit choline transporter
Block voltage gated Ca2+ channels
Block vesicle fusion
Block aceylcholine activated channel
Non depolarising nicotinic receptor blockers
Deploarising nicotinic receptor blocker
Activate nicotinic receptors
What are potential clinical applicaitons of pharmacology of ganglionic transmission?
Almost none because the drugs affect both the sympathetic and parasympathetic, and possible th NMJ so there are so many side effects
What are post ganglionic parasympathetic transmission potential sites of action?
Muscarinic receptor antagonist
Muscarinic receptor agonist
What are clinical applicaitons of post ganglionic parasympathetic pharmacology?
Agonist mimics the effects of the parasympathetic system
Antagonist blocks the effects of the parasympathetic system