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Spring 2020 - Pharmacology 1 > Neuromuscular Blockers - Quiz 7 > Flashcards

Neuromuscular Blockers - Quiz 7 Flashcards

1
Q

How does Acetylcholine bind to the Nicotinic Receptor?

A

The positively charged Nitrogen binds to both alpha subunits of the nicotinic receptor, allowing Sodium to enter.

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2
Q

Which enzyme is responsible for the synthesis of Acetylcholine?

A

Choline Acetyltransferase

Choline + Acetyl CoA –> Acetylcholine

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3
Q

Which Autonomic System does Acetylcholine Activate?

A

Both

Primarily Rest & Digest, but also Kick starts the Sympathethic Nervous System

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4
Q

What deactivates Acetylcholine?

A

Acetylcholinesterase break down ACh into choline & acetate

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5
Q

Why are Neuromuscular Blockades used?

A

Cause paralysis to reduce complications d/t movement & help with intubation

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6
Q

What percentage of Suppression of Single Twitch Response is adequate for Surgery?

A

90%

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7
Q

What is the difference b/t Depolarizing & Non-Depolarizing Agents?

A

Depolarizing: constantly stimulates muscle fiber and cant respond to ACh

Non-Depolarizing: Competetively blocks ACh from receptor

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8
Q

What is ED95

A

NMB dose with non volatile anesthetic needed for 95% supression of single twitch during

ED95 is much less when used w/ gas

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9
Q

How much NMB is needed for Tracheal Intubation in terms of ED95?

A

2x ED95

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10
Q

What is the Order of Effect of NMBs?

A

Small quick moving muscles first (Eyes, Fingers)

then

Abdomen (Diaphragm) last

Reverses in reverse order d/t blood flow

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11
Q

What is the effect of NMBs at the Laryngeal Muscles vs Peripheral Muscles?

A

More Rapid & Less Intense @ Laryngeal Muscles

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12
Q

What are indicators of Laryngeal Relaxation when using NMBs?

A

Orbicularis Oculi - good indicator

Adductor Pollicis - poor indicator

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13
Q

What do the Non-Depolarizing NMBs break down into?

A

Benzylisoquinolinium - Histamine Release

Aminosteroid

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14
Q

What does the Quarternary Ammonium part of the NMB do?

A

Makes NMB highly ionized & water soluble - stays in blood

Does not cross into CNS or Placenta

Cant Give Orally

Binds to Alpha Subunits

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15
Q

What does it mean for NMBs to be non selective?

A

They will effects at both Autonomic Nicotinic & Cardiac Muscarinic receptors

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16
Q

Which Non-Depolarizing NMBs are Benzylisoquinoliniums?

A

NMBs that end with -curium

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17
Q

Which Non-Depolarizing NMBs are Aminosteroids?

A

NMBs that end with -curonium

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18
Q

Which Non-Depolarizing NMBs are Long Acting?

A

Pancuronium

Pipercuronium

Doxacurium

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19
Q

Which Non-Depolarizing NMBs are Intermediate Acting?

A

Vecuronium

Rocuronium

Atracurium

Cisatracurium

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20
Q

Which Non-Depolarizing NMBs are Short Acting?

A

Mivacurium

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21
Q

What is the only Depolarizing NMB used?

A

Succinylcholine

Intense Rapid Paralysis

Onset: 30-60 seconds

Duration: 3-5 minutes

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22
Q

What is the Mechansim of Action of Succinylcholine?

A

Binds to one or both alpha subunits @ Nicotinic receptor

Mimics ACh

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23
Q

What is the Mechansim of Action of Succinylcholine?

A
  • Binds to one or both alpha subunits @ Nicotinic receptor
  • Mimics ACh, but longer duration d/t slower hyrdrolysis
  • Hyperpolarizes Receptor & no more ACh can activate the receptor
  • Big Na+ influx causes Efflux of K+
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24
Q

What happens in Phase I of Block w/ Succinylcholine?

A
  • Depolarizing receptor stimulation
  • ↓Contraction to single twich
  • ↓Ampltidude of continuous stimulation
  • TOF > 0.7
  • Muscle twitches @ onset
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25
Q

What happens in Phase II of Block w/ Succinylcholine?

A

Acts like Non-Depolarizer

ACh can no longer act

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26
Q

How do Plasma Cholinesterase affect Succinylcholine?

A

Break SCh down to weak metabolite

Give Neostigmine to reverse for pts w/ liver disease

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27
Q

How does High Estrogen & Reglan affect Succinylcholine?

A

High Estrogen reduces Cholinesterase levels

Reglan Inhibits Cholinsterase

Build up of Succinylcholine

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28
Q

How does Obesity affect Succinylcholine?

A

Obese pt’s have more Cholinesterase and may reduce effects of SCh

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29
Q

How does Atypical Cholinesterase affect Succinylcholine?

A

May increase Duration of SCh from 10 minutes to 3+ hours

Test w/ Dibucaine

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30
Q

How can side effects of Succinylcholine be reduced?

A

Pretreat with small dose of Non-Depolarizing NMB

Non effective for Hyperkalemia

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31
Q

What kind of Arrythmias might Succinylcholine cause?

A

Bradycardia, Junctional Rhythm, Sinus Arrest d/t muscarinic receptors

Worsens w/ 2nd dose in 5 min

Give Atropine

(May also see increased HR & BP)

32
Q

Who is most at risk for Succinylcholine-induced Hyperkalemia?

A

Boys w/ muscular dystrophy or can’t create muscle movement so nicotinic receptor upregulation happens

Hyperkalemia can last from 96 hrs to 2 years

33
Q

What is a side effect of Succinylcholine r/t muscles?

A

Myalgias in Neck, Back, and Abdomen

34
Q

Where in the body might you see Increased Pressures from Succinylcholine?

A

Intragastric - Aspiration

Intraocular

Intracranial

All Transient and Uncommon

35
Q

What is the Mechanism of Action for Non-Depolarizing NMBs?

A

Competes with ACh for Nicotinic Receptors

↓Single Twitch

TOF < 0.7

Posttetanic Poteniation

Antagonism by Anticholinesterase

36
Q

What are the CV effects of Non-Depolarizing NMBs?

A

Atracurium & Mivacurium - Histamine Release

Pancuronium - Blocks Muscuranic Receptor - ↑HR

Blocks Nicotinic - Possible ↓HR & ↓BP

Mostly CV Stable

37
Q

What is a consideration after using Non-Depolarizing NMBs?

A

Critical Myopathy

Long term paralysis on vent

More common w/ Aminosteroids (especially w/ steroids)

Can last for an unknown time

38
Q

What is the main causes of Allergic reactions in the OR?

A

Neuromuscular Blocker

Higher risk for Females

More Nitrogen in the molecule = higher risk for allergic rxn

39
Q

Which dementia meds inhibit Cholinesterase?

A

Razadyne

Aricept (Donepezil)

Exelon (Rivastigmine)

40
Q

What Drugs Enhance NMBs?

A
  • Anesthetic Gas
  • Local Anesthetics
  • Antiarrythmics - Lidocain, Quinidine
  • Aminoglycosides - Gentamicin
  • Diuretics
  • Mag & Lithium
41
Q

How does Phenytoin effect the use of Vecuronium?

A

Reduce Duration

42
Q

How do Cyclosporines affect NMBs?

A

Prolongs Block

43
Q

How does Hypothermia affect NMBs?

A

Prolongs Duration

For every degree change from 36C, prolongs block by 10-15 min

44
Q

How does Hypokalemia affect Succinylcholine & Non-Depolarizing NMBs?

A

Sux: Resistance

NDNMB: ↑Sensitivity

45
Q

How does Hyperkalemia affect Succinylcholine & Non-Depolarizing NMBs?

A

Sux: ↑Effect

NDNMB: Opposes

46
Q

How do Burn Injuries affect Non-Depolarizing NMBs?

A

Resistance to NDNMBs

47
Q

Would a patient who is already has Hemiplagia need more or less of a NMB dose?

A

More d/t upregulation of receptors

48
Q

How are Infants & Elderly affected by NMBs?

A

Infants: Reduce Dose, Shorter Onset, Longer Recovery

Elderly: Longer Duration

49
Q

How many Nitrogens does Pancuronium have?

A

Two - Bisquartenary

50
Q

What is the ED95, Onset, and Duration of Pancuronium?

A

ED95: 70 mcg/kg

Onset: 3-5 min

Duration: 60-90 min

51
Q

How is Pancuronium Eliminated from the Body?

A

80% in urine - renal failure reduces to 50%

Half Potent Metabolite

Liver Disease prolongs duration

52
Q

What are the CV effects of Pancuronium?

A

Most CV effects out of all Long Acting NMBs

↑HR, ↑BP, ↑MAP d/t vagal block

Big risk for Dysrhythmias when given with Digoxin

53
Q

How many Nitrogens does Doxacurium have?

A

Two - Bisquaternary

54
Q

What is the ED95, Onset, and Duration of Doxacurium?

A

ED95: 30mcg/kg

Onset: 4-6 min

Duration: 60-90 min

55
Q

What is the difference b/t Doxacurium & Pancuronium?

A

Less CV effects

More Metabolites

56
Q

Why are Intermediate NMBs preferred?

A

Better Clearance

Shorter Duration

Faster Recovery

Predictable

57
Q

What is the Priming Principle for NDNMBs?

A

Give baby dose of NMB to bind spare receptors

Next dose will have rapid effect

58
Q

What is the ED95, Onset, and Duration for Atracurium?

A

ED95: 0.2mg/kg

Onset: 3-5 min

Duration: 20-35 min

59
Q

How is Atracurium Eliminated?

A

80% Protein Bound

Rapid Clearance

60
Q

What is Hoffman Elimination?

A

Relates to Atracurium & Cisatracurium

Does not Rely on Kidneys or Liver

3 Steps: Hoffman –> Hydrolysis –> Hoffman

Laudanosine Metabolite

61
Q

What is Laudanosine and what does it do?

A

Inactive Metabolite of Atracurium & Cisatracurium from Hoffman Elimination

CNS Stimulant

Peripheral Vasodilation

Increase MAC of Gas

62
Q

Whare are the CV effects of Atracurium?

A

Generally Safe

but @ 3x ED95

↑HR & ↓MAP

Histamine Release - use H1/H2 Blocker

63
Q

What are some dosing considerations when giving Atracurium to Infants & Elderly?

A

Infants: Half Dose - More Sensitive & More Rapid Clearance

Elderly: No dose adjustments

64
Q

How does Cisatracurium compare with Atracurium?

A

Pretty much the same

Less CV Effect

No Histamines

Prolong Duration in Obese

65
Q

How many Nitrogen groups does Vecuronium have?

A

One - Monoquaternary

66
Q

How is the elmination of Vecuronium different from Atracurium & Cisatracurium)

A

Relies on Liver & Kidneys

More Lipid Soluble

Half Potent Metabolite then Very Weak 2nd Metabolite

67
Q

What are the CV effects of Vecuronium?

A

No Histamine

More Stable than Cis & Atracurium

68
Q

How man Nitrogen groups does Rocuronium have?

A

One - Monoquaternary

69
Q

What is the ED95, Onset, and Duration for Rocuronium?

A

ED95: 0.3 mg/kg

Onset: 1-2 min

Duration: 20-35 min

70
Q

How does giving 3-4x ED95 dose affect Rocuronium?

A

Speeds up Onset & Increase Duration

71
Q

How is Rocuronium eliminated?

A

Relies on Liver and Kidneys

72
Q

What are the CV effects of Rocuronium?

A

Same as Vecuronium

CV Safe

No Histamines

73
Q

What is the ED95, Onset, and Duration for Mivacurium?

A

ED95: 80 mcg/kg

Onset: 2-3 min

Duration: 12-20 min

74
Q

How is Mivacurium Eliminated?

A

Cholinesterase

Effected by Liver & Kidneys

Rapid Spontaneous Recovery

75
Q

What are the CV effects of Mivacurium?

A

Generally Safe

but at 3x ED95: Histamine Release, ↓MAP & Bronchospasm

Spring 2020 - Pharmacology 1 (11 decks)

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