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Title: The NMJ
Description: Pharmacology of the NMJ containing many interesting images, all colour coded. Done by a First year Dental student from the University of Birmingham. (lecturer was medical so perfectly suitable for Medical students). Names of all drugs mentioned and explained because it is easier for me and probably you. The images are great to memorize. Written in mostly bullet point format to make them super easy to understand, I wrote these right after the lecture so things are explained well.
Description: Pharmacology of the NMJ containing many interesting images, all colour coded. Done by a First year Dental student from the University of Birmingham. (lecturer was medical so perfectly suitable for Medical students). Names of all drugs mentioned and explained because it is easier for me and probably you. The images are great to memorize. Written in mostly bullet point format to make them super easy to understand, I wrote these right after the lecture so things are explained well.
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17 – Dr Whitehead
Tuesday 31st October 2017
The Pharmacology of the Neuromuscular Junction
Pharmacology of the NMJ:
Nicotinic ACh present pre-synaptically; influences release
CAT = synthetic enzyme for ACh
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)
Vesicles with special protein on them which takes ACh and loads it into vesicles for
exocytosis
Choline carrier takes choline back up into pre-synaptic element
...
o Choline taken back up; used to make more ACh and then loaded into vesicle
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o Receptors for the neurotransmitter released by its own neuron is detecting itself,
called an auto-receptor
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Mediate negative feedback on release
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Makes synapse more reliable
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10
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Cholinacetyltransferase (CAT) from acetyl CoA & choline (No Drugs target this)
o Carrier transports ACh into vesicle (loads acetylcholine into vesicles (blocked by
Vesamicol – drug with no clinical use)
o Choline transporter – blocked by Hemicholinium – drug used for research but not
clinically
o Exocytosis of vesicle (blocked by toxins) – these drugs are actually toxins, stops
release of neurotransmitter
Botulinum Toxin
Clostridium botulinum (anaerobic bacteria)
o Thrives in anaerobic environments
Source of potentially lethal food poisoning
10-12g toxin – lethal for mouse
2 subunits:
o 1- binds to presynaptic membrane (binds selectively to nerve endings of neurones
which release ACh – something specific on membrane)
o 2- (peptidases) cleaves proteins involved in exocytosis (inside nerve ending)
Kills you by affecting release of ACh by blocking exocytosis/ ACh release
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S
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E
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glands- GIT, smooth muscle contraction, secretion of saliva
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10
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g
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Drugs Acting post-synaptically: Neuromuscular blockers:
More commonly used clinically
Working on post-synaptic receptor; so, at level of nicotinic receptor
Used as Adjunct (add-on) to anaesthesia
o Used when GA used to allow clinician to use lower conc of GA
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E
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tubocurarine
o Depolarising blockers
Agonists
Both produce paralysis
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10
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Structure of D-Tubocurarine has sites which block both sites on
ACh
Title: The NMJ
Description: Pharmacology of the NMJ containing many interesting images, all colour coded. Done by a First year Dental student from the University of Birmingham. (lecturer was medical so perfectly suitable for Medical students). Names of all drugs mentioned and explained because it is easier for me and probably you. The images are great to memorize. Written in mostly bullet point format to make them super easy to understand, I wrote these right after the lecture so things are explained well.
Description: Pharmacology of the NMJ containing many interesting images, all colour coded. Done by a First year Dental student from the University of Birmingham. (lecturer was medical so perfectly suitable for Medical students). Names of all drugs mentioned and explained because it is easier for me and probably you. The images are great to memorize. Written in mostly bullet point format to make them super easy to understand, I wrote these right after the lecture so things are explained well.