L8 - drugs affecting neuromuscular transmission Flashcards
how is acetylcholine synthesised
choline + acetylcoenzyme A by action of the enzyme choline acetyl transferase
what drug blocks the uptake of choline into the nerve terminal
hemicholinum
what drug blocks the uptake of acetylcholine into synaptic vesicles
vesamicol / AH5183
what are the two types of acetylcholine receptor
nicotinic and muscarinic
drugs that prevent the destruction of ACh
edrophonium (short duration), neostigmine (nedium duration), irreversible organophosphates e.g novichok (long duration)
what is a motor unit
the motor nerve + the nerve fibres it enervates
how large is the neuromuscular gap
around 60nm
what neurotransmitters and reactors are active at neuromuscular junction
acetylcholine and nicotinic receptors
structure of the nicotinic Ash receptor
⍺⍺β𝛄σ subunits around a non-selective cation channel, permeable to Na+ and K+
when does the nicotinic Ash receptor channel open
when 2 molecules of Ash bind to the protein complex, on to each ⍺ subunit. opening of the channel leads to depolarisation of the end-plate region of the muscle membrane.
what does botulinum toxin do
destroys key proteins involved in exocytosis
clinical used to treat blepharospasm, spasticity associated with MS or cerebral palsy, cluster headache and in cosmetics
clinical uses of reversible, competitive antagonists at neuromuscular junctions
used as muscle relaxants during surgery. effects last for 15-40 minutes.
name a depolarising muscle relaxant
suxamethodium. same effect as acetylcholine but can’t be broken down