Local Anesthetics Flashcards

1
Q

What is the most widely used anaesthetic?

A

Lidocaine

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2
Q

What local anaesthetic is cardiotoxic?

A

Bupivacaine

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3
Q

Which local anaesthetic is contraindicated in obstetric anaesthesia?

A

Mepivacaine

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4
Q

Why is Mepivacaine contraindicated in obstetric anesthesia?

A

Due to its increased toxicity to neonates

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5
Q

What is the clinical use of local anaesthetics?

A

Complete loss of sensory modalities

Analgesia

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6
Q

What is the target of local anaesthetics?

A

Inactivated voltage gated sodium channels

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7
Q

What part of the voltage gated sodium channel do local anaesthetics bind to?

A

The IC part

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8
Q

Which drugs bind to the EC part of the activated voltage gated sodium channel?

A

Tetrodotoxin

Saxitotoxin

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9
Q

What are the three states of the voltage gated sodium channel?

A

Resting state
Inactivation state
Activation state

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10
Q

What are the M and H gate doing during resting state?

A

M gate is closed

H gate is open

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11
Q

What are the M and H gate doing during the activation state?

A

Both gates are open

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12
Q

What are the M and H gate doing during the inactivation state?

A

The M gate is open

The H gate is closed

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13
Q

What is the M gate?

A

The activation gate

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14
Q

What is the H gate?

A

The inactivation gate

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15
Q

What are the methods of administration of local anaesthetics?

A
Surface
Infiltration
IV
Peripheral nerve blocks
Spinal
Epidural
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16
Q

What is the order of disappearance of sensations?

A
  1. Pain
  2. Temperature
  3. Touch
  4. Deep pressure
  5. Motor function
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17
Q

What nerve fibres are most sensitive to blockage?

A

Nerve fibres off small diameter and high firing rates

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18
Q

What is the order of sensitivity of the nerve fiber types?

A

Type B and C
A delta
A beta and gamma
A alpha

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19
Q

What are the CNS side effects of local anaesthetics?

A
Headache
Sleepiness
Visual and auditory disturbances 
Restlessness
Nystagmus 
Shivering
Muscular twitching
Seizures 
Depression
Death
Cocaine: feeling of well being, psychostimulant, euphoria
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20
Q

What are the cardiovascular side effects of local anaesthetics?

A

Depression of pacemaker activity, condition, excitability, contractility
Vasodilation - hypotension
Cocaine: vasoconstriction

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21
Q

Why is a side effect of local anaesthetics allergies?

A

Esters viva PABA formation

Sulfonamides are esters of PABA

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22
Q

What are the haematological side effects of local anaesthetic use?

A

Prilocaine can result in methemoglobinemia

23
Q

Can local anaesthetics cross the placenta?

A

Local anaesthetics may cross the placenta

24
Q

What are the (broad) side effects of local anasthetic use?

A
CNS effects
Cardiovascular toxicity 
Allergies
Haematological effects
Local anaesthetics may cross the placenta
25
Q

What is Ropivacaine metabolised by?

A

CYP1A2

26
Q

What enzyme is Lidocaine and Bupoivacaine metabolised by?

A

CYP3A4

27
Q

What are the general categories of LI?

A

Esters and amides

28
Q

Name the ester LA?

A

Procaine
Cocaine
Benzocaine

29
Q

Name the amide LA?

A
Lidocaine
Prilocaine
Bupivacaine
Ropivacaine 
Mepivacaine
Atricaine
30
Q

What are the esters metabolised by?

A

Plasma and tissue esterases

31
Q

What are the amides metabolised by?

A

Liver amidases

32
Q

What is the potency of procaine?

A

1

33
Q

What is the potency of bupivacaine?

A

16

34
Q

What is the potency of Mepivacaine?

A

2

35
Q

What is the potency of Atricaine?

A

10

36
Q

Which LA is the most potent?

A

Bupivacaine

37
Q

Which LA is the least potent?

A

Procaine

38
Q

Which LA have a short duration of action?

A

Procaine

Atricaine

39
Q

Which LA have a medium duration of action?

A

Cocaine
Lidocaine
Prilocaine
Mepivacaine

40
Q

Which LA have a long duration of action?

A

Benzocaine
Bupivacaine
Ropivacaine

41
Q

Which LA have poor tissue penetration?

A

Procaine

42
Q

Which LA have moderate tissue penetration?

A

Prilocaine
Bupivacaine
Ropivacaine

43
Q

Which LA have good tissue penetration?

A

Cocaine
Lidocaine
Mepivacaine
Atricaine

44
Q

What is the clinical indication of procaine?

A

No longer used

45
Q

What is the clinical indication of cocaine?

A

Rarely used. Only as a spray for upper respiratory tract

46
Q

What is the clinical use of Benzocaine?

A

Surface anesthesia

47
Q

What is the clinical use of lidocaine?

A

Local anaesthesia but also IV for treating ventricular dysrhythmias

48
Q

What is the clinical use of prilocaine?

A

Spinal anesthesia

Not used for obstetric analgesia

49
Q

What is the clinical use of Ropivacaine?

A

Spinal anesthesia

Not used for obstetric analgesia

50
Q

What is the clinical use of Mepivacaine?

A

Infiltration and nerve block anesthesia
Mild vasoconstrictor effect
Not used in babies or small children

51
Q

What is the clinical use of Atricaine?

A

Infiltration and nerve block anesthesia
More lipophillic
Used in dentistry

52
Q

What are the cardiovascular side effects of procaine?

A

Bradycardia and vasodilation

53
Q

What are the adverse CNS effects of procaine?

A

Restlessness
Convulsions
Respiratory depression

54
Q

What are the adverse effects of prilocaine?

A

No vasodilator activity

Less risk of systemic toxicity but risk of methemoglobinemia