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Brain Anatomy > PHAR232 - Neuromuscular blockers > Flashcards

PHAR232 - Neuromuscular blockers Flashcards

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1
Q

Are neuromuscular blockers depolarising or non-depolarising? (located at neuromuscular junction)

A

Both - working on nAChRs

NO TONE
WET NOODLE

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2
Q

What are non-depolarising blockers?

A

nicotinic antagonists

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3
Q

What are depolarising blockers?

A

Nicotinic agonists

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4
Q

What was the first non-depolarising neuromuscular blocker?

A

Curare

‘kur-rah-ree

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5
Q

What is the active compound for morphine and codeine?

A

Alkaloids

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6
Q

What is the suffix associated with curarine or tubocurarine?

A

Things ending in curonium or curium

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7
Q

Non-depolarising NM blockers - KNOW THIS

A
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8
Q

Can non-depolarising neuromuscular blockers be overcome?

A

Yes - as they are agonist or competitive antagonists

e.g. acetylcholinesterase INHIBITOR to encourage ACh release to outcompete NM blocker

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9
Q

AChE inhibitor information

A

KNOW HOW AChE WORKS (antidote)

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10
Q

Tries to not let it get systemic for PSNS for side effects etc

A

PNS
- Tears
- Brochodilation
- Uncontrolable bladder
- Salivation etc

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11
Q

Is 4-aminopyridine an AChE inhibitor ?

A

No
It OUTCOMPETES NM blocker to ACTIVATE nAChRs on muscle cells

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12
Q

Is 4-aminopyridine a longer or shorter-acting?

A

Longer

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13
Q

Does 4-aminopyridine cross the BBB?

A

Yes

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14
Q

What do non-depolarising NM blockers tubocurarine, mivacurium, atracurium all have in common?

A

Induce histamine release

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15
Q

What can a significant histamine release induce?

A

Drop in BP
Cause bronchospasms

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16
Q

REVIEW AND UPDATE =- PRINT OUT ALL OF THE DIAGRAMS IN THE TEXT BOOK

A
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17
Q

are depolarising NM blockers agonists or antagonists?

A

They are nAChR agonists = they depolarise

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18
Q

What is the only clinically relevant compound for depolarising NM blockers for humans?

A

Suxamethonium (succinylcholine)

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19
Q

How long does suxamethonium aka succinylcholine have after depolarisation for desensitization?

A

30 sec desensitation

20
Q

How does a depolarising NM blocker work e.g. suxamethonium for phase 1?

A

Continuous nicotinic ACh receptor depolarisation is overstimulated
- Prevents repolarisation
- Short acting paralysis (phase 1)

21
Q

How does a depolarising NM blocker work e.g. suxamethonium for phase 2?

A

phase 2

  • Repeated exposure = increased accumulation of metabolite SUCCINYLMONOCHOLINE
  • Succinylmonocholine = antagonist curare action
    = PHASE II blocker

CONTINUES as an antagonist and blocks NM nAChRs

22
Q

Is phase II of depolarising NM blockers and non-DNM blockers the same actions?

A

yes - know the steps they are the same

23
Q
A
24
Q
A
25
Q

What do all neuromuscular blockers paralyse?

A

Skeletal muscle

26
Q

Are respiratory muscles under skeletal muscles?

A

Yes

27
Q

Do all neuromuscular blockers cause respiratory paralysis?

A

Yes

28
Q

What is the main target for muscle relaxants?

A

GABA

29
Q

What does baclofen target as a muscle relaxant?

A

A GABA-B agonist

30
Q

Learn GABA-B receptor signalling = for baclofen

A

MECHANISM OF ACTION FOR BACLOFEN

31
Q

PKA is _________ dependent

A

cAMP dependent

32
Q

What happens if you inhibit AdCy?

A
  • decrease cAMP
  • Decrease PKA
  • Decrease VG-Ca2+ channels
  • Decrease synaptic vesicle mobilisation
  • Decrease NT release
33
Q

Baclofen post-synaptic mechanism of action

A
34
Q

Baclofen antispasmotic effect is mainly exerted through _________

A

Spinal cord

35
Q

What does the activation of GABA-B receptors do post-synaptically?

A
  • Activate inward K+ channels
  • Increase efflux of K+
  • Hyperpolarise post-synaptic motor neurons
36
Q

Benzodiazepam therapeutic interventions

A
37
Q

Benzodiazepines are ________________ modulators

A

positive allosteric modulator

38
Q

What is a positive allosteric modulator?

A

Its easier to GABA to activate its own receptor

39
Q

mehcniams of action of benzodiazepines (BDZ)

A
40
Q

MECHANISM OF ACTION FOR DANTROLENE

A
41
Q

Dantrolene is a _____________ and _____________ antagonist

A

Ryanodine receptor 1 (RyR1)
Ryanodine receptor 3 (RyR3)

42
Q

What does dentrolene primarily act on?

A

Skeletal muscle receptors RyR1

43
Q

Are RyR3 receptors found in the brain?

A

Yes

44
Q

What is a ryanodine receptor channel pathway?

A

Ryanodine receptors are part of a channl to promote Ca2+ efflux from the SR in the cytoplasm

45
Q
A

Brain Anatomy (59 decks)

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