local anesthetics Flashcards

1
Q

a fundamental use of of local anesthetics is

A

blockade of nerve fxn (both centrally and peripherally)

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2
Q

application may be for blockade of ____ _____ _____ for ___________ or blockade of ________ ________ for a specific limb analgesia, or central blockade for a truncal blockade

A

cardiace nerve fxn
dysrhythmia
peripheral nerves

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3
Q

local anesthetics derive their effect from

A

interrupting the sodium channel action potential in the nerve

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4
Q

depolarization of a receptor channel can be through ________ or ________ __________

A

voltage or ligand gating

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5
Q

with voltage gating, an _________ arrives at the channel causing it to open and a NT or substance such as _________ enters the cell for effect

A

impulse
sodium

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6
Q

a ligand gate opens when a ______ (___) in the environment of operation ______ __ __ _________ and causes it to open.

A

ligand (NT)
binds to the channel

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7
Q

ACh in the NMJ is an example of:

A

ligand gating

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8
Q

local anesthetics operated with _________ gating on the ________ channels

A

voltage gating
sodium channels

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9
Q

LAs operate in _____ dependent fashion with a larger amount of LA blocking a respectively larger number of channels

A

dose-dependent

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10
Q

as greater blockade occurs, so is the prominence of the blockade through interruption in depolarization _______ __________

A

impulse propagation

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11
Q

the inability of an impulse to propogate or carry a signal results in the

A

inability of that nerve to carry the signal to its destination

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12
Q

since different nerve fibers have different signal functions, blocking some nerves will result in lack of _______ fxn past the point of blockade and other fibers will not transmit _______ signals pas the blockade

A

sensory
motor

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13
Q

there is a functional threshold for LAs, that is, until a minimum dose is met, there will be ___________

A

no effect

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14
Q

nerve fibers are blocked in order of their _______ and _________ variables

A

size and myelination

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15
Q

LA effect is __________ and __________ dependent

A

concentration and volume

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16
Q

transmission through tissue in a concentration gradient sufficient to penetrate the nerve sheath is _________ to gaining effect

A

essential

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17
Q

esters

A

cocaine
benzocaine
procaine
chloroprocaine
tetracaine

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18
Q

amides

A

lidocaine
mepivacaine
bupivacaine
prilocaine
ropivacaine

(2 i’s in amide)

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19
Q

2 primary divisions of LAs are created by their chemical structure:

A

lipophilic (lipid soluble) is an aromatic benzene ring
hydrophilic (water soluble) is a tertiary amine

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20
Q

joining these 2 elements: lipophilic (aromatic benzene ring) and hydrophilic (tertiary amine) is a

A

hydrocarbon chain

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21
Q

the link between the ________ ________ and the __________ is the key to classifying the types of LAs

A

lipophilic ring and the hydrocarbon

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22
Q

ESTERS bind the lipid side to the chain with _____

A

CO

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23
Q

AMIDES bind the lipid side to the chain with ______.

A

NHC

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24
Q

ESTERS are metabolized by

A

pseudolchilinesterases

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25
Q

AMIDES are metabolized by

A

the liver

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26
Q

pts with pseudocholinesterase deficiencies will have ______ _________ and risk _________

A

slower metabolism and risk toxicity

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27
Q

recall that AChE drugs are found in the ________ for metabolism of ACh

A

NMJ

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28
Q

The presence of enzymes that break down ester LAs are found in the _______ and are referred to as _________ __________

A

plasma
plasma cholinesterases - bc they are found outside the the NMJ they can also be called pseudocholinesterases

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29
Q

___________ metabolism is generally slower than _________ metabolism

A

amide
esterase

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30
Q

the true metabolism of the drugs becomes pertinent after it is ______________________ from the site of injection

A

taken up into circulation

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31
Q

once this “uptake” occurs, _______ _________ for esters and _________ dysfunction for amides metabolize the LA

A

plasma cholinesterase
liver

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32
Q

a _______ uptake into circulation can _______ the chance of toxicity by preventing a large, less metabolizable bolus from effecting the CNS and CV system.

A

slow
decrease

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33
Q

an exception on route of metabolism is the ester local __________ which is metabolized by the liver

A

cocaine

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34
Q

______ are more likely to cause allergic reactions than _______

A

esters
amides

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35
Q

the ester metabolite ______________ (____) is the offending agent

A

p-aminobenzoic acid (PABA)

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36
Q

because __________ such as __________ are used with amide drug packaging, they too may have an allergic response

A

preservatives
methylparaben

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37
Q

true allergic patients may benefit from using a _________ _______ ________ LA

A

preservative free amide LA

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38
Q

_________, which is not as readily available anymore is the more common culprit for allergic responses of the amides

A

prilocaine

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39
Q

___________ is the active LA in “hurricane spray” and is more likely to cause this response than other amides

A

benzocaine

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40
Q

methemoglobinemia correlates with these 2 LAs

A

prilocaine and benzocaine

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41
Q

the formation of methemoglobin is abnormal ______ given the normal amount of this form of ______ is trace

A

Hgb
Hgb

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42
Q

when these LAs are given, especially in high doses, the normal Hgb is susceptible to

A

change to MetHgb

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43
Q

A left shift to the oxygen hemoglobin dissociation curve results and the inability of this Hgb to

A

carry oxygen

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44
Q

__________ is often used for topical anesthesia during GI procedures, TEE exams, and oral procedures

A

benzocaine (hurricane spray)

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45
Q

treatment for HetHgb

A

methylene blue given at 1-2 mg/kg IV

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46
Q

Since LAs have both non-ionized (lipophilic) and ionized (hydrophilic) components, it is valuable to know the respective ____ of each drug

A

pKa

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47
Q

the pKa is the ______ at which half of the drug is non-ionzed and other half is ionized

A

pH

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48
Q

if a pH solution is _____ than the pKa of the drug, then the LA becomes ______ ionized and is less able to enter the nerve and have its effect

A

lower
more

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49
Q

clinically, patients with infections have _____ effect of the drug when injected

A

less

if pH is lower than the pKa of the drug, then the LA becomes MORE ionized and less able to effective

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50
Q

if an ankle block is needed for a toe debridement, and the foot is infected, the pH will be lower and thus the drug becomes more __________ and ____ _________ bc _______ drug enters the nerve

A

ionized
less effective
less

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51
Q

making the onset _______ and ______ dense

A

slower and less dense

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52
Q

the addition of _______ ________ to LAs has been demonstrated to increase speed of onset by keeping more drug in the non-ionized state

A

sodium bicarbonate

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53
Q

one additional benefit of adding bicarbonate is the reduced ____ __ ______

A

pain on injection

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54
Q

This MOA for reduced pain with bicarb is not certain but perhaps related to decreased sensitivity of _____ _______ to ______________ drug

A

nerve fibers to non-ionized

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55
Q

when a drug has a high pKa, it becomes more _________________________

A

difficult to enter the nerve for action

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56
Q

(drug with high pKa difficult to enter the nerve for action)
this is exaggerated when the patient pH is _________ and when ________/__________ make the _______ lower

A

lower
additives/preservatives
lower

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57
Q

bc the alkalization of LA increases the _______ soluble nature, it is able to enter the cells more easily (instead of reaching the nerve)

A

lipid

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58
Q

the more ______ soluble the LA, the more potent and longer duration of action.

A

lipid

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59
Q

most LAs have a non-ionized component that is _______ soluble and an ionized portion that is _______ soluble

A

lipid
water

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60
Q

when the non-ionized portion enters the nerve, it then equilibrates its non-ionized and ionized portion and the ionized portion is able to bind to the ______ _______

A

sodium receptor

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61
Q

thus to speed onset, making the lipophilic portion more ________ by the addition of __________, you assist the speed of onset

A

prominent
bicarbonate

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62
Q

3 factors determine the longevity of action in the LAs

A
  1. dose to start
  2. tissue distribution and lipid solubility
  3. drug metabolism
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63
Q

the larger the _____, the _________ duration of action

A

dose
longer

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64
Q

lipid soluble drugs have _________ duration of action than less soluble drugs

A

longer

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65
Q

increased ______ ______ is inversely related and _______ _______ solubility is directly related to duration of action

A

blood flow (means less on site time)
lipid solubility (means increased time on site)

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66
Q

systemic absorption (uptake from tissue to plasma level) is affected by:

A

site of injection
dose
specific drug properties
vessel rich sites generally absorb more quickly than vessel poor
larger dose increase the concentration gradient of the LA
properties (lipid solubility/pKa) can increase absorption vs uptake

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67
Q

one way to consider the functional duration of action is to think of what keeps the drug from being _____ ______ from the site.

A

taken away

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68
Q

lipophilic properties promote _____

A

absorption

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69
Q

epinephrine decreases ______ ______ for uptake

A

blood flow

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70
Q

high protein binding increases _______ to the tissue

A

adherence

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71
Q

injection of LA into tissue (not IV) results in it eventually moving into __________ (this is _____)

A

moving into circulation
this is uptake

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72
Q

the uptake of LA represents the duration of _________ utility

A

clinical

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73
Q

lungs remove a large portion of LA, especially _________

A

lidocaine

74
Q

protein binding results in drug being __________, versus free drug in the ________

A

sequestered
plasma

75
Q

metabolism occurs by the two primary methods of:

A

pseudocholinesterase activity
the liver

76
Q

_______ ________ then occurs following metabolism

A

renal excretion

77
Q

we think of clinical duration of action as how long will this drug stay in the tissue around the nerve before it gets _________ and taken away for _________

A

absorbed
metabolism

78
Q

sites of absorption (rates of uptake from fastest to slowest)

A

tracheal > intercostal > caudal > epidural > brachial plexus > femoral/sciatic

TICEBS

79
Q

drug uptake into circulation initiates metabolism of the drug more quickly in _______ than ______________ sites, thus the clinical effect at the _______ is shorter bc its taken up into circulation from that site

A

tracheal
brachial plexus
trachea

80
Q

rate of uptake is important when considering _______ doses

A

toxic

81
Q

several ______ are found to potentiate the effect of LAs.

A

drugs

82
Q

__________ decreases uptake and therefore prolongs effect

A

epinepherine

83
Q

___________ by ____________ decreases blood flow to the area and decreases circulatory uptake (and thus metabolism) of the LA

A

vasoconstriction by epinephrine

84
Q

the use of epi is found to increase duration of ________, ________, and __________ in absorption into tissue in some blocks through vasoconstrictive nature.

A

action, potency and reduction in absorption

85
Q

___________ & ___________ as well, increase the potency and duration of the blocks by delaying repolarization

A

clonidine and dexmedetomidine

86
Q

interestingly, _________, like ___________, has alpha 2 agonist properties

A

epinephrine
clonidine

87
Q

_________ can potentiate LA and have been found to increase intensity and speed of onset for blocks by way of their own mechanism of blockade of _______ transmission

A

opioids
pain

88
Q

regarding metabolism of pseudocholinesterase, the LA, ___________, disables this enzyme

A

dibucaine

89
Q

exposing a patients pseudocholinesterase to dibucaine should __________ the action of the enzyme. Normal is ________ _________

A

inhibit
80% inhibited

90
Q

dibucaine is NOT used ___________, but to test for the presence of ___________ __________

A

anesthetically
abnormal pseudocholinesterase

91
Q

for abnormal pseudocholinesterase, dibucaine only inhibits _______%

A

20%

92
Q

20% inhibition by dibucaine implies that abnormal pseudocholinesterase wont break down drugs at the normal speed, thus _______ LAs and drugs metabolized by this process (remi, esmolol, SCh) will have significant ________ in duration of action over their nominally short duration of action.

A

ester
increases

93
Q

the ________ the dibucaine number, the more normal the enzyme and likelihood that it breaks down at a normal rate

A

higher

94
Q

__________ is often noted in the CNS due to crossing the BBB

A

toxicity

95
Q

toxicity is due to the _________ of the inhibitory neurons

A

depression

96
Q

__________ & _________ are the hallmarks of toxicity

A

seizures and hyperexcitation

97
Q

_______________, ____________, & ______________ is followed by excitation and seizures

A

ringing in the ears, circumoral numbness, and tongue numbness

98
Q

subsequent excitatory blockade results in excitatory block with ____________ & _________ collapse

A

respiratory and cardiac collapse

99
Q

acute and significant uptake may result in __________ arrest

A

respiratory

100
Q

the ____________ features are secondary (though timing may be varied) due to blockade of the excitatory neurons resulting in ________ _________ and ________

A

cardiotoxicity
cardiac dysrhythmia and arrest

101
Q

CV effects may include decreased __________ and __________ through the same inhibitory mechanism of action on sodium channels

A

contractility and conductivity

102
Q

at higher concentrations, smooth muscle relaxation occurs which may be helpful in the _________, but causes systemic __________.

A

lungs
systemic hypotension

103
Q

cardiac toxicity, likely related to high _____ ______ is more associated with longer acting drugs, particularly ___________

A

protein binding
bupivicaine

104
Q

in most cases, occurrence of toxicity is _____

A

rapid

most often less than 1 minute and majority less than 5 minutes from time of injection

105
Q

rapid toxicity is often due to direct injection of the LA ____________ rather than into ___________

A

intravascularly rather than tissue

106
Q

efforts to avoid intravascular injection include:

A

frequent needle aspiration
avoidance of excessive dosing
use of ultrasound
test-dosing for epidurals
incremental dosing

107
Q

maximum bupivicaine dose

A

2.5 mg/kg = 2.5 mg/ml

108
Q

2.5 mg/kg max dose for bupivicaine (or 2.5 mg/ml) means that the patient’s weight in kg is the ________ ________

A

maximum volume, or half the volume if 0.5% is used

109
Q

_______ ________ ________ is a form of toxicity in the intrathecal space which can be caused by LA in prolonged exposure as well as mechanical processes such as infection, compression, hematoma, or structural changes

A

cauda equina syndrome

110
Q

this process tends to be ________ lasting, if not _________

A

longer lasting, if not permanent

111
Q

loss of _______, ________, or _______ and ________ fxn are consistent along with intractable pain inconsistent with __________ or absence of noxious ___________

A

sensory, motor, or bowel and bladder
stimulus, stimulus

112
Q

_______ _________ _________ are resolvable syndromes that have similar features

A

transient neurologic symptoms

113
Q

________, _________, lower extremity ________ and ________ deficits are the hallmarks of these two processes (CES/TNS)

A

bowel, bladder, lower extremity motor and sensory deficits

114
Q

________ _________, particularly with _________ have been associated with TNS

A

subarachnoid catheters
lidocaine

115
Q

___ ___________ for SAB has fallen out of favor even for single injection blocks

A

5% lidocaine

116
Q

often indistinguishable, the _______ resolves within a few weeks whereas the _______ does not

A

TNS
CES

117
Q

several factors influence increase the risk for systemic toxicity. _______ ________ into circulation is a risk for any LA. This achieves potentially toxic level in the shortest amount of time

A

unintended uptake

118
Q

_______ _________ is reportedly reduced by the use of ultrasound for constant visualization of the needle tip

A

vascular injection

119
Q

fast uptake from highly perfused areas can result in toxicity when ______ _______ of LA are near the ______

A

large quantities
near the site

120
Q

toxicity parallels _______

A

potency

121
Q

drugs that are very lipophilic are _____ _____, with the most prominent drug being _______

A

more toxic
bupivacaine

122
Q

_______ toxicity generally precedes _________ and is related to level of drug

A

CNS
cardiotoxicity

123
Q

since the increase in level can change quickly during (unintended) IV injection, _____ ______ _ ______ can occur in short succession

A

both types of toxicity

124
Q

keep in mind that toxicity is not a “ _______ _____”, it is a ______ that enters circulation and the brain ________ than it can be cleared

A

“large dose”
dose
faster

125
Q

large doses CAN be used for protracted effect but within the confines of the ______ _______ ________

A

peripheral nerve space (outside the vasculature)

126
Q

prevention by use of ________, _________ dosing, use of _______ for blockade, _____ dosing, and knowledge of toxic levels are key

A

aspiration, incremental dosing, use of US for blockade, test dosing, and knowledge of toxic levels are key

127
Q

Initial toxic response is often _________

A

seizures/ CNS toxicity

128
Q

___________ are the most common therapy though ________ can be effectively used.

A

benzos
propofol

129
Q

caution with propofol d/t _______ ______ effect

A

myocardial depressant

130
Q

decreased ________ ________ and peripheral ____________ are effects of the propofol by itself and may be more prominent in the presence of LA toxicity

A

myocardial contractility and peripheral vasodilation

131
Q

_______ may stop external muscle activity, but they don’t affect cerebral excitation

A

paralytics

132
Q

_______ toxicity is more difficult to address with traditional resuscitation

A

Cardiac

133
Q

ACLS is used in standard workflow but some recommendations include using smaller doses of _________

A

epinephrine - 100 mcg rather than 1000 mcg

134
Q

______ ______ is the most complicated but best method to sustain the patient until drug is metabolized

A

cardiac bypass

135
Q

the newest mechanism of therapy is use of _____ ______ ______

A

20% lipid solution

136
Q

use of lipids absorbs the LA which ________ the removal of the LA from the _______ receptors and has resulted in many anecdotal resuscitations

A

accelerates
cardiac

137
Q

the _______ is inversely related to the seizure threshold

A

PaCO2

138
Q

if person is hypoventilating, the _______ will increase and consequently _________ threshold

A

CO2
lower

139
Q

additional factors include ________, ________, and _________ which can worsen LAST

A

acidosis, hypoxia, hyperkalemia

140
Q

an intuitive response for suspected or known LAST is control of the ______ with ______ and _______ to prevent these issues

A

control of the airway with oxygenation and ventilation

141
Q

prilocaine

A

unique metabolite, o-toluidine. pre-cursor for MetHgb

142
Q

benzocaine can also cause __________

A

MetHgb

143
Q

benzocaine is a __________ amine (most LAs are ______ amines)

A

secondary
tertiary

144
Q

benzocaine is permanently _________ and stays ______ soluble and crosses into the _______ and attaches to the _____ channel directly

A

non-ionized
lipid
cell
Na

(this may account for its rapid onset and is most commonly used in the aersolized form for topical use in airway analgesia)

145
Q

5% lidocaine (concentrated form) can be, and historically was used for ______

A

SAB

146
Q

lidocaine has fallen out of favor for spinals due to reports of _______, specifically _________ when catheters were used to continuously infuse the medication

A

neurotoxicity, specifically CES

147
Q

_______ from single injections of 5% lidocaine have been reported with spontaneous resolution of symptoms

A

TNS

148
Q

_________ has a particular propensity to cause cardiac effects more than other LAs

A

bupivacaine

149
Q

in addition to prominent cardiac toxicity, the prolonged duration makes bupivacaine more concerning bc it doesnt “____ ____”. pay attention to ____ ______

A

wear off
max dose

150
Q

ropivacaine behaves similarly to ___________ with respect to _____/______/_______ however it has less cardiotoxic effects and generally has less pronounced ______ _____ potency

A

bupivacaine
onset/time/duration
motor block

151
Q

Eutectic mixture of LA

A

EMLA cream

152
Q

eutectic means

A

lower melting point

153
Q

_____ & _______ are the combo used for topical EMLA, and must be applied an _______ in advance

A

lidocaine and prilocaine
hour

154
Q

liposomal bupivicaine (exparel) is a ______ ______ LA

A

sustained release

155
Q

designated for infiltration, exparel is found to have prolonged duration of action, presumably from _______ ______

A

delayed uptake

156
Q

exparel is also being used with _______ ________ _______ for increased duration of action

A

peripheral nerve blocks

(24-48 hours reportedly)

157
Q

_________ has become the preferred method of providing long acting pain relief for orthopedic sx (a single injections perform as well/better than pain catheter that must be removed/monitored)

A

exparel

158
Q

several drugs when added to LAs improve their fxns

A

steroids
alpha2 agonists
opioids
bicarbonate

159
Q

steroids - particularly ________ has been shown to increase duration of action of blocks. studies have compare _________ and _________ injections and found similar effects on the block when either route is used

A

decadron
IV and perineural

160
Q

alpha2 agonist - _________, address pain directly but also ______ ______ _______ ________ conduction in the ___ and ___ fibers thus prolonging and improving blockade. the synergistic effect of the two mechanisms of action make it a popular _________.

A

clonidine
inhibit peripheral nerve signal
A and C fibers
additive

161
Q

opioids - have been added to blocks to increase _______. the _____ of the block likely wont change and neither will the total _______ __ ______, but some suggest there is ___________ or ________ effect

A

potency
density
duration of action
potentiation or cumulative

162
Q

opioids are recognized by some providers as an ______ in speed of onset in certain central blocks. others suggest there are more consistencies and fewer ______ ______ in the presence of opioids

A

increase
spotty blocks

163
Q

bicarbonate - the addition of an ____________ agent is deigned to increased _____________ portion of the drug to allow access to the nerve. this process improves both the pain of ___________ and the ___________ of the block

A

alkalyzing
non-ionized
injection
efficacy

164
Q

in addition to selective nerve blockade, LAs have additional application: inhibition of ______ ______, reduction in ______ ______ _______ (for high _____ during intubation), and pain ________ ________ are a few examples

A

ventricular dysrhythmias
reduction in cerebral blood flow (for high ICP during intubation)
pain management therapy

165
Q

specific to anesthesia is the use of lidocaine to blunt ______ _______ by ______ _______ relaxation

A

respiratory stimulation
smooth muscle

166
Q

______, _______, and ________ applications have been described

A

IV, inhaled, and topical

167
Q

for dysrhythmia applications, the disruption of conduction in the cardiac cycle can address _____ _______ sites by blocking ______ _____

A

aberrant ectopic
Na channels

168
Q

however, in the presence of conduction delay or heart block, lidocaine can actually cause _______ ______ ______

A

complete cardiac standstill

169
Q

complete cardiac standstill with lidocaine is exacerbated in the presence of concurrent therapy with _____ _____ and/or ________ _____ ________

A

beta blockers
calcium channel blockers

170
Q

our focus is on the use of LAs to provide __________ nerve blockade and provide __________ nerve blockade

A

peripheral
central

171
Q

how do we pick what drug to use?

A

onset/duration
safety factor

172
Q

goals for regional should include understanding of (5)

A

peripheral nerve anatomy
LAs
US equipment
nerve blockage techniques
practice with tools for block delivery

173
Q

benzocaine technique/concentration/max/duration

A

technique - topical
concentration - 20%
max - NA
duration - NA

174
Q

chloroprocaine - technique/concentration/max/duration

A

technique - epidural, infiltration, peripheral nerve block, spinal
concentration - 1%, 2%, 3%
max - 12mg/kg
duration - short

175
Q

cocaine - technique/concentration/max/duration

A

technique - topical
concentration - 4%, 10%
max - 3 mg/kg
duration - short

176
Q

tetracaine (amethocaine) - technique/concentration/max/duration

A

technique - spinal, topical (eye)
concentration - 0.2%, 0.3%, 0.5%, 1%, 2%
max - 3 mg/kg
duration - long

177
Q

bupivacaine - technique/concentration/max/duration

A

technique - epidural, spinal, infiltration, PNB
concentration - 0.25%, 0.5%, 0.75%
max - 2.5 mg/kg
duration - long

178
Q

lidocaine - technique/concentration/max/duration

A

technique - epidural, spinal, infiltration, PNB, IV regional, topical
concentration - 0.5%, 1%, 1.5%, 2%, 4%, 5%
max - 4.5 mg/kg (7 mg/kg with epi)
duration - medium

179
Q

mepivacaine - technique/concentration/max/duration

A

technique - epidural, infiltration, PNB, spinal
concentration - 1%, 1.5%, 2%, 3%
max - 4.5 mg/kg (7 mg/kg with epi)
duration - medium

180
Q

ropivacaine - technique/concentration/max/duration

A

technique - epidural, spinal, infiltration, PNB
concentration - 0.2%, 0.5%, 0.75%, 1%
max - 3 mg/kg
duration - long