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Pharmacology > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

1st LA

A

cocaine

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2
Q

1st synthetic ester

A

procaine (1905)

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3
Q

hallmark LA (amide)

A

lidocaine (1943)

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4
Q

Progressive shutdown in order

A

autonomic, somatic sensory, somatic motor

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5
Q

temporary conduction blockade along peripheral/central nerve pathways

A

local anesthetics

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6
Q

Local MOA

A

block (saltatory) transmission of nerve impulses on axon and dendrites, inhibit passage of Na+ ions through selective Na+ channels in nerve membrane

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7
Q

Does MOA involve synapse, NMJ, or schwann cell?

A

NO

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8
Q

Peripheral nerve wrapped in

A

epineurium

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9
Q

Wraps several axon bundles

A

perineurium

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10
Q

Wraps axon, has own conducting membrane (axolemma)

A

endoneurium

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11
Q

What do schwann cells do

A

wrap one or more axons, insulate axolemma from e’ment

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12
Q

Does entire dose of LA get delivered?

A

No, only 2% reach.. has to penetrate 4-5 layers

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13
Q

Unidirectional, jumping from nodes of Ranvier, full strength yes or no response

A

saltatory conduction

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14
Q

factors of Cm

A

pH, temp, calcium conc, nerve type, stimulus frequency

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15
Q

Motor fibers Cm compared to sensory

A

M is 2X the Cm of sensory

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16
Q

Peripheral nerves made of

A

(myelin) A and B fibers and (unmyelin) C fibers

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17
Q

How many nodes must be exposed for effective blockade

A

3

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18
Q

Most heavily myelinated, largest, fastest

A

Alpha A fibers

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19
Q

Alpha A fibers provide ____ and ____ function

A

motor and proprioception

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20
Q

Less myelinated preganglionic autonomic nerves

A

B fibers

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21
Q

postganglionic sympathetic and afferent sensory

A

c fibers

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22
Q

Pain and temp sensation, slowest, tourniquet pain

A

c fibers

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23
Q

Receptor theory (MOA)

A

LAs bind with receptors on INTRACELLULAR side of Na+ channel to prevent depolarization or repolarization (maintain inactive)

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24
Q

Na+ Channel blockade…

A

Resting potential not affected
Tonic suppression (local binds while gate is at rest)
Phasic suppression (local binds while gate is open)
Channel stabilizes… an occupied ch will not open

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25
Q

LAs contain 3 structures:

A

Unsaturated benzene ring
Intermediate chain (amide or ester)
Quaternary? amine

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26
Q

Which part of LA structure is lipophilc? hydrophilic?

A

benzene ring, quat amine

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27
Q

N on end is what?

N in chain is what?

A

Amine

Amide

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28
Q

pKa + log (ionized/nonionized) =

A

= pH

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29
Q

pKA think…..

A

rate of onset

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30
Q

Locals are weak (acid/bases)

A

bases

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31
Q

Ionized is ? soluble

A

water soluble

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32
Q

Benzene ring responsible for

A

anesthetic activity

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33
Q

Site of metabolism

A

ester or amine (hydrocarbon chain)

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34
Q

The amine end shifts in and out of ionization establishing…

A

water solubility or membrane permeability

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35
Q

Increased substitutions to either end of molecule will (increase/decrease?) hydrophobicity

A

increase

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36
Q

Is the pure base form water soluble? will it precipitate?

A

poorly or non-water soluble, it will precipitate

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37
Q

LAs are shipped as ____, the base ionizes in an acidic carrier and stays water soluble

A

salts

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38
Q

When/what causes LA to shift to basic form, resulting in lipophilicity?

A

Injection into tissue

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39
Q

?philic LAs have slow onset

A

Hydrophilic and highly hydrophobic… moderately hydrophobic have faster onset

40
Q

?phobic = long activity

A

hydrophobic

41
Q

What ties directly to potency?

A

lipid solubility

42
Q

Onset of action/diffusion depends on:

A

chemical structure, lipid solubility, state of ionization (most important)

43
Q

Higher pKa to get to pH 7.4.. drug becomes more/less? ionized

A

more ionized

44
Q

Lower pKa have (slower/faster) onset

A

rapid

45
Q

Ropiv/Bupiv ? onset

A

slower

46
Q

Duration of action is r/t?

A

protein binding and lipid solubility

47
Q

Tetra, bupiv, etido length of action

A

long acting

48
Q

Lido, mepiv, prilo length of action

A

medium

49
Q

Pro and chloropro length of action

A

short

50
Q

All LAs (except cocaine and ropiv) produce ____ of smooth vascular muscle

A

relaxation

51
Q

(Increase/decrease) absortpion preferred

A

decreased

52
Q

Absorption occurs most rapidly with

A

intercostal blocks, caudal-lumbar epidurals, brachial plexus, sciatic-femoral, subQ blocks

53
Q

What determines peak plasma conc?

A

Total dose (not volume or conc)

54
Q

1% solution is ?mg/?mL

A

10mg/mL

55
Q

Ester metabolism

A

ester hydrolysis via esterases in plasma/red cells

bloodstream, dont have to go to liver

56
Q

amides metabolism

A

liver (P450)

57
Q

most important differene between esters and amides

A

site of metabolism

58
Q

Allergenic byproduct from esters

A

PABA

59
Q

Do amides break down to PABA?

A

no but contain methylparaben (close relative) look for MPF (free) labels

60
Q

Which class do drugs have i’s in names

A

amides

61
Q

Toxicities of mixing LAs

A

ADDITIVE, not independent

62
Q

Adding bicarb….

A

to speed onset (carbonation), bu reduced pH?

63
Q

Topical use LAs…drugs?

A

apply to mucous membranes, ENT GU cataracts, tetracaine, lidocaine, cocaine

64
Q

EMLA cream

A

2.5% lido with 2.5% prilocaine

65
Q

Topical most rapidly absorbed

A

tetracaine… then cocaine and lidocaine

66
Q

cocaine blocks uptake of

A

epi and NE

67
Q

Examples of major nerve blocks

A

brachial plexus, interscalene (require higher conc)

68
Q

Examples of minor nerve blocks

A

ulnar, medial (single nerve)

69
Q

Ankle block is an example of what

A

infiltration block

70
Q

Epidural intermediate-acting drugs ? hours

A

1-2 hours

71
Q

Epidural long-acting drugs ? hours

A

3-5 hours

72
Q

Epidural drugs…

A

2-chloroprocaine, lidocaine, mepivacaine, bupivicaine, ropivicaine, levobupivi

73
Q

Indwelling catheter with…

A

epidural

74
Q

Effective dosing pattern with epidural

A

small frequent

75
Q

Common spinal drugs

A

bupivi, tetracaine (basically same numbers), lidocaine

76
Q

varacity…

A

specific gravity

77
Q

reactions rarely allergic.. usually..?

A

toxicity

78
Q

1 suspect fo CNS toxicity

A

lidocaine

79
Q

1 suspect for cardiac toxicity

A

bupivicaine

80
Q

Prevention of toxicity- pretreat with

A

benzos.. supplemental 02, 5cc and aspirate

81
Q

if toxicity occurs… ?ventilation

A

hyperventilate

82
Q

2 causes of systemic toxicity

A

Intravascular injection, too high local dose

83
Q

resp/metabolic acidosis (increase/decrease) CNS toxicity

A

increase

84
Q

sequence of CNS toxicity

A

metallic taste, lightheaded, tinitus, visual, slurring, muscle twitch, irrational, pass out, seizure, coma, apnea

85
Q

cardiac toxicity occurs after

A

CNS toxicity

86
Q

Lidocaine cardiac tox pattern

A

hypotension, bradycardia, hypoxia

87
Q

too much bupivi, what occurs immediately?

A

resusc resistant left vent dysrhythmias

88
Q

Locals bind when channels are (open/closed)?

A

open (systole)

89
Q

Locals release during which part of cardiac cycle

A

diastole

90
Q

CV toxicity

A

prolong conduction time, increase PR/QRS, CHB, SB, arrest

91
Q

Treatment of CV toxicity

A

intralipid 20%

92
Q

only LA that produced prolonged sensory/motor defecits in spinal/epidural

A

chloroprocaine

93
Q

LA that can produce methemoglobin… and what are S&S

A

prilocaine.. DO NOT USE IN OB

brownish-gray cyanosis, tachypnea, met acid

94
Q

severe methemoglobinemia

A

tissue hypoxia, HA, irritability, LOC

95
Q

have phospholipid bilayers that act as barrier, slow release and prolong duration, decrease toxicity

A

liposomal preparatiosn

96
Q

Time release, used for infiltration of surgical site, pain control up to 72 hours

A

exparel

97
Q

Examples of liposomal LAs

A

lidocaine, tetracaine, bupivi

Pharmacology (3 decks)

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