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SUMMER PHARM > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

What 3 kinds of blocks do LA’s providE?

A

autonomic, somatic sensory, somatic motor

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2
Q

_______ nerve roots contain the cell bodies of the Afferent neurons. These are _________ neurons.

A

Dorsal

Sensory

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3
Q

________ nerve roots contain the cell bodies of Efferent neurons. These are _______ neurons.

A

Ventral

Motor

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4
Q

A ___________ cell wraps itself around a myelinated nerve fiber

A

Schwann Cell

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5
Q

Extracellularly is a high concentration of _____ and low concentration of _________.

A

Na

K

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6
Q

The velocity an impulse travels is ___________ to the diameter of the fiber

A

proportional

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7
Q

LA’s will keep ion channel in the ________ state

A

inactive

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8
Q

_____ is the more permeable ion

A

K

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9
Q

Are A fibers myelinated or unmyelinated? What is their size? How fast are they?

A

Myelinated
1-22microns
fastest of all of the fibers

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10
Q

Which is faster? Aalpha or A delta

A

A alpha

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11
Q

What is the size of B fibers?

A

1-3 micrometers

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12
Q

What is the size of C fibers? are they myelinated or unmyelinated?

A

.1 - 2.5 micrometers

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13
Q

Which is the slowest fiber?

A

C

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14
Q

Which fibers are PREganglionic auntonomic

A

B

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15
Q

Which fibers deal with pain, temperature, and touch

A

A delta

and C with dull pain

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16
Q

Which fibers are POSTganglionic autonomic

A

C

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17
Q

CLINICALLY, Which type of blockade will you see first? Last?

A

autonomic

motor

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18
Q

The sequence of onset and recovery from a LA block in a mixed peripheral nerve relies heavily on ______________________________

A

Where is it located

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19
Q

What # is RMP?

A

-70mv

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20
Q

___________ is he difference in the concentration of + and - ions when the cell is at rest

A

RMP

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21
Q

Intracellular space has a relative ________ charge compared to the extracellular space. This is bc ______ ion is impermeable to the resting cell membrane

A

negative

Na

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22
Q

The membrane is more permeable to ______

A

K

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23
Q

It is the movement of _____ that establishes and maintains RMP

A

K

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24
Q

An AP occurs when what 4 physiologic stimuli is received b the nerve receptor?

A

mechanical, thermal, chemical, pressure

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25
Q

As an AP is propagated, the stimulus causes _____ channels on the membrane to open.

A

Na

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26
Q

During an AP, influx of _____ causes membrane potential to increase to ____-____ mv

A

Na

20-40mV

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27
Q

Local Anesthetics change ______________________________

A

The ability to reach threshold

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28
Q

LA’s bind the Na Channel ________ subunit when it is in the _______________ state

A

Alpha

Inactivated Closed State

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29
Q

LAs access nerve cell Na channels during the _____________ state

A

activated open

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30
Q

A _________ nerve is less sensitive to block.

A

resting (versus a repetitively stimulated nerve)

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31
Q

LAs have a _______________ head made, a ______________ chain, and a _____________ tail.

A

lipophilic
intermediate
hydrophilic

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32
Q

NH represents a ____________ and COO- represents a ______________

A

amide

ester

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33
Q

Is lidocaine an amide or an ester?

A

amide (2 I’s)

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34
Q

How are Esters metabolized/broken down?

A

Hydrolyzed by non-specific esterase in the pasha and tissues

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35
Q

How are Amides metabolized/broken down?

A

in the liver

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36
Q

Highly lipid soluble anesthetics are more or less potent than water soluble anesthetics

A

MORE SOLUBLE

37
Q

An increase in the length in the chain, tail, or head increases _________________

A

Potency and toxicity

38
Q

Are bupivacaine and mepivacaine pure S enantiomers or racemic?

A

RACEMIC

39
Q

Exparel is an extended release _________ injection. Max dose is ________mg

A

Liposome

266 (20ml)

40
Q

Cm refers to the ____________________ of LAs

A

minimum blocking concentration

41
Q

An impulse can make it through ___ blocked nerves but not ____… this becomes an issue with ___ fibers

A

2 not 3

A

42
Q

The distance between nodes in a myelinated nerve fiber contributes to: _______________

A

Differential Nerve Blockade

43
Q

A differential Nerve Block is a __________ block with incomplete __________ block

A

sensory

motor

44
Q

The Pain conducting fibers are:

A

A Delta and C fibers

45
Q

____________ was the first LA shown to produce a beneficial differential block

A

bupivacaine

46
Q

What is the order from highest to lowest of absorption by type of block?

A

Intravenous, Tracheal, intercostal, caudal, pericervical, epidural, brachial plexus, subarachnoid/spinal, subcutaneous

47
Q

Do ionized or non-ionized cross a lipid membrane more readily?

A

non-ionized

48
Q

The non-ionized form is favored when you have an acidic drug in a ____________ environment or a basic drug in a ___________ environment

A

acidic

basic

49
Q

All LA’s are weak ________ with pka values between ____-____

A

bases

7.5-9

50
Q

What is the ideal pka?

A

7.4

51
Q

The __________ form binds and blocks the Na channel

A

ionized

52
Q

The __________ form penetrates the nerve sheath and axon membrane to reach the site of action

A

non ionized

53
Q

_______ is the most important property in determining onset of LAs

A

pKa

54
Q

Which pKa will provide a faster onset in a LA? A pKa of 7.5 or 9?

A

7.5 because the closer the pKa is to physiologic pH, the faster the onset

55
Q

How can we increase the amnt of non-ionized form so that we can speed up the onset?

A

increase the pH (add BICARB)

56
Q

Adding _________ to a block increases the onset, enhances block depth, and increases the spread of the block

A

bicarb!

57
Q

A _________ temperature reduces drug absorption across the nerve membrane

A

decreasing

58
Q

Lipid solubility is directly related to __________ for LAs

A

potency

59
Q

The 3 most potent LAs are:

A

Etidocaine, bupivacaine, tetracaine

60
Q

Potency: ________ as onset: ___________ as duration: _________

A

lipid solubility
pKa
protein binding

61
Q

The most important factor in determining DOA for LAs is: ________________

A

protein binding

62
Q

What 3 purposes does adding epi to a LA serve?

A
  1. inhibit systemic absorption
  2. prolong effects
  3. detect IV injection
63
Q

____________ is a LA similar to lidocaine but without the intrinsic vasodilator effect

A

mepivicaine (so won’t need epi)

64
Q

Which 3 LAs have uptake by the lungs?

A

Bupivicaine, lidocaine, prilocaine

65
Q

How are esters metabolized?

A

hydrolyzed by pseudocholinesterases

66
Q

Which LA’s have a metabolite? whats it’s name?

A

Esters,

PABA - its inactive but allergenic

67
Q

How is cocaine metabolized?

A

by the liver

68
Q

With LA toxicity, muscle twitching in the face means……

A

seizures are imminent

69
Q

____________ increases the risk of LA toxicity and ___________ decreases the risk

A

hyperkalemia

hypokalemia

70
Q

The _____________ system is more resistant to toxic effects of LAs

A

Cardiovascular system

71
Q

_________________ is the most CV toxic and cardiac arrest may occur at lower levels of toxic doses

A

bupivicaine

72
Q

____________ and ____________ decrease hepatic blood flow and therefore decrease clearance of amide LAs

A

propranolol

cimetidine

73
Q

_________ blocks NE and dopamine reuptake

A

cocaine

74
Q

________ is an ester with a short DOA and a slow onset

A

procaine

75
Q

________ is an ester with a very long DOA (6hrs) and slow onset.

A

tetracaine

76
Q

__________ is an ester that is popular with OB anesthesia d/t its ultra rapid serum hydrolysis

A

Chloroprocaine

77
Q

Monoethylglycinexylidide is the active metabolite for _______________

A

lidocaine

78
Q

T/F Lidocaine can be used in all routes of administration

A

F - shouldn’t use with spinal d/t cauda equina syndrome

79
Q

_____________ has the highest unionized fraction @ physiologic pH

A

mepivicaine

80
Q

______________ is a good amide LA to consider when use of a vasoconstrictor is contraindicated

A

mepivicaine

81
Q

Ortho-toluidine is the toxic metabolite of _____________

A

prilocaine

82
Q

Avoid the use of _____________ in OB

A

prilocaine

83
Q

Methemoglobinemia can be an issue mainly with ______________ but also also

A

prilocaine

lidocaine - topical

84
Q

Methemoglobinemia can occur in prilocaine doses >________ and is treated with _____________

A

600mg

methylene blue 1-2mg/kg iv over 5mins

85
Q

_____________ is popular for differential nerve blocks. ________>_________

A

bupivacaine

sensory > motor

86
Q

Bupivacaine is high protein bond to _________________

A

alpha 1 glycoprotein

87
Q

The bad s/e of bupivacaine is ___________

A

very cardio toxic

88
Q

___________ and _________ are S-enantiomers of bupivacaine.

A

ropivacaine and levobupivacaine

89
Q

For epidural blocks, you give _____-_____ml/per segment desired

A

1.25 - 1.6

SUMMER PHARM (5 decks)

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