L8: drugs affecting neuromuscular junction Flashcards

1
Q

How many processes can drug affect to modify chemical synaptic transmission?

A

5

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2
Q

What processes pre-synaptically can affect the synaptic transmission?

A
  • Synthesis
  • Storage
  • Release
    of the neurotransmitter
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3
Q

What processes post-synaptically can affect the synaptic transmission?

A
  • Receptors
  • Removal mechanism
    for the neurotransmitter
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4
Q

First stage of events in pre-synaptic ‘cholinergic’ transmission

A

Acetylcholine is synthesised from choline + acetylcoenzyme A by action of enzyme Choline Acetyl Transferase (CAT)

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5
Q

Second stage of events in pre-synaptic ‘cholinergic’ transmission

A

Choline is taken into nerve terminal by a transporter protein

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6
Q

Synthesis

What does Hemicholinium block the uptake of?

A

Uptake of choline into nerve terminal

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7
Q

Storage

What does **AH5184 **block the uptake of?

A

Uptake of ACh into synaptic vesicle

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8
Q

Release

What does **Conotoxins **block?

A

Blocks voltage-gated Ca2+ channels

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9
Q

Release

What does Botulinum block?

A

Blocks process of exocytosis

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10
Q

Third stage of events in pre-synaptic ‘cholinergic’ transmission

A

ACh is stored by synaptic vesicles that are released by exocytosis

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11
Q

First stage of post-synaptic events in cholinergic transmission

A

After being released, ACh diffuses across synaptic gap & activates receptors on post-synaptic membrane

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12
Q

Two types of ACh receptors

A

1) Nicotinic Receptors
2) Muscarinic Receptors

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13
Q

What are nicotinic receptors activated by?

A

Nicotine from tobacco plant

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14
Q

What are muscarinic receptors activated by?

A

Muscarine from poisonous Fly Agaric mushroom

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15
Q

What is ACh broken down by during the removal from the synapse?

A

Enzyme acetylcholinesterase (AChE), found in the synaptic gap

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16
Q

Name the enzyme involved in the synthesis of acetylcholine (ACh)

A

Choline Acetyl Transferase (CAT)

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17
Q

Name the enzyme involved in the destruction of ACh

A

Acetylcholinesterase (AChE)

18
Q

What happens to the choline produced following the destruction of ACh?

A

Being recycled, taken back into nerve terminal for synthesis of new ACh

19
Q

What are the FIVE key processes that drugs can interfere with at any chemical synapse

A

1) Synthesis
2) Removal
3) Release
4) Receptors
5) Removal

20
Q

What is the motor unit?

A

Motor nerve + muscle fibre it controls

21
Q

Why is the muscle membrane thrown into folds?

A

Increasing SA

22
Q

What is the specialised area of the muscle membrane called?

A

Muscle “end plate”

23
Q

What is the neurotransmitter released in skeletal neuromuscular junction?

A

Acetylcholine

24
Q

What is the receptor present on the muscle in skeletal neuromuscular junction?

A

Nicotinic acetylcholine receptors

25
Define agonist
Substance that mimics the actions of a neurotransmitter to produce a response when it binds to a specific receptor
26
How many protein subunits form the nicotinic ACh receptor?
5
27
Structure of nicotinic ACh receptor
5 protein subunit surrounding a non-selective cation channel which is permeable to Na+ & K+
28
When does the non-selective cation channel on the nicotinic ACh receptor open?
2 molecules of ACh bind to the protein complex, 1 to each alpha-subunit
29
What does opening of the channel of nicotinic ACh receptor leads?
Leads to depolarisation of the end-plate region of muscle membrane
30
Where is botulinum toxin found?
Uncooked foods
31
32
What is blepharospasm?
Involuntary tight closure of eyelids
33
What does botulin target in blepharospasm?
Inappropriate contraction of the skeletal muscle
34
Does botulinum toxin given locally or systemically?
Locally
35
Role of botulin in presynaptic transmission
Inhibits the release of ACh
36
Define antagonist
Substance that stops the action/effect of another substance
37
What are at the nicotinic ACh receptor to post- synaptically inhibit neuromuscular transmission?
Reversible competitive antagonists
38
Are reversible competitive antagonists GENERAL ANAESTHETICS?
NOOO, used alongside to stop contraction
39
How can effects of muscle relaxants during surgery be reversed?
Acetylcholinesterase inhibitor, neostigmine
40