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Basics in Anesthesia > Local anesthetics > Flashcards

Local anesthetics Flashcards

1
Q

introduced cocaine as the first local anesthetic in 1884, for use in ophthalmology.

A

koller

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2
Q

negative resting membrane potential

A

-70 - -90

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3
Q

essential for anesthetic activity

A

lipophilic aromatic ring

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4
Q

-CO-

A

ester

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5
Q

-NHC-

A

amide

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6
Q

membrane potential

A

20 mV or 35 mV

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7
Q

Where do local anesthetics bind to

A

Alpha subunit

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8
Q

Guarded receptor theory

A

-LA preferentially binds to both open or inactivated states
-Not to closed state

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9
Q

The IONIZED fraction binds to the receptor on the cell inside or outside of the cell?

A

inside of the cell

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10
Q

Name the Esters

A

Procaine
Chloroprocaine
Tetracocaine
Cocacine
Benzocaine

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11
Q

Name the Amides

A

Lidocaine
Mepiviapine
Prilocaine
Bupivicaine
Ropivacaine
Articaine

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12
Q

Nerve fiber sensitivity & DIFFERENTIAL BLOCKADE

A

B fibers > C fibers > small A > large A

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13
Q

prophylactic measure to prevent bradycardia and hypotension with locals

A

Phenylephrine gtt

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14
Q

a fibers

A

Alpha
Beta
Gamme
Delta

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15
Q

A fiber with the largest diameter and fastest conduction and most heavily myelinated

A

alpha

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16
Q

requires highest concentration of LA to be blocked

A

Alpha A Fibers

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17
Q

fiber responsible for motor and proprioception

A

alpha A fiber

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18
Q

a fiber that motor function, touch, pressure

A

Beta A fiber

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19
Q

conduction velocity second to alpha a

A

beta a

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20
Q

A fiber responsible for reflexes and innervate muscle spindles

A

Gamma

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21
Q

a fiber responsible for reflexes

A

gamma

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22
Q

a fiber that has a small diameter and slower conduction (30m/s)

A

a delta

Lamina I and V

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23
Q

responsible for pain and temperative

A

a delta

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24
Q

Fibers constitute the preganglionic autonomic nerves

A

B fibers

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25
Q

Similar diameter to A-delta, slow and less myelinated

A

B fibers

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26
Q

smallest fibers of all

A

c fibers

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27
Q

conducts pain and temperature

A

c fibers

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28
Q

only fibers unmyelinated and smallest of all fibers (<2m/second)

A

C fibers

Lamine 1 and 2

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29
Q

1/100,000 =

A

10mcg/ml

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30
Q

2% lido =

A

20mg/ml

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31
Q

Acidosis in the environment into which the LA is injected ….

A

increases the ionized fraction of drug

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32
Q

Absorption of drugs

(If teddy interrupts ice cream, everyone be super still)

A

Intravenous
Tracheal
Interpleural
Intercostal
Caudal
Epidural
Brachial plexus
sciatric-femoral
Subcutaneous

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33
Q

systemic toxicity is inversely proportional to

A

rate of hydrolysis

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34
Q

Vasodilation increases drug absorption and may cause ____.

A

toxicity

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35
Q

Most LA except ____ produce relaxation of vascular smooth muscle

A

cocaine

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36
Q

where is cocaine (an ester) metabolized?

A

plasma and LIVER cholinesterases

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37
Q

MAX DOSE OF COCAINE

A

5 mL of 4% solution
or
200 mg should be used

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38
Q

4%

A

4g/100ml
4000mg/100ml
40mg/ml cocaine
200mg = 5mL

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39
Q

DOA of LA is dependent on

A

protein binding
lipid solubility

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40
Q

DOA is directly proportional to

A

protien binding

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41
Q

Weak bases bind primarily to

A

alpha one acid glycoprotein

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42
Q

The onset of action depends on

A

State of ionization #1
Lipid solubility
Chemical structure

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43
Q

potency =

A

lipid solublity

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44
Q

high lipid solubility =

A

toxicity

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45
Q

DOA is directly proportional to

A

protein binding

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46
Q

Pseudochilinesterase deficiency=

A

Choose amide anesthetic

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47
Q

The rate of hydrolysis varies:
Alphabetical

A

Chloroprocaine = most rapid
Procaine = intermediate
Tetracaine = slowest

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48
Q

sunscreen allergy

A

avoid esters
especially procaine

Paraaminobenzoic acid may be an antigen responsible for allergic reactions

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49
Q

how does spinal anesthesia work in metabolism ?

A

needs to go into blood stream

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50
Q

how is lido broken down

A

oxidative dealkylation in the liver followed by hydrolysis to metabolite

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51
Q

prilocaine metabolite

A

converts hemoglobin to methemoglobin

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52
Q

treatment for methemoglobinemia

A

methylene blue
1-2 mg/kg

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53
Q

Cyanosis with decreased oxygen-carrying capacity

A

methoglobinemia
left shift

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54
Q

lidocaine metabolite protects against

A

protects against cardiac dysrhytmias

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55
Q

Drugs that cause methoglobinemia

A

prilocaine (EMLA)
BENZOcaine (Cetacaine, hurricane)

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56
Q

20% benzocaine spray delivers

A

200 - 300 mg for awakes, endo, TEE, bronchs

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57
Q

treatment for methemoglobinemia

A

Methylene blue
1 to 2 mg/kg IV over 3 to 10 minutes

** can repeat **

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58
Q

metHB levels >70%

A

transfusion
dialysis

59
Q

Modulates the local from burning and speeds onset

A

Sodium bicarbonate

60
Q

MOA of adding bicarb

A

increases pH of LA resulting in more drug in the nonionized state-readily able to diffuse across membranes

61
Q

epi 1:200,000

A

5 mcg/ml

1g in 200,000ml
1000 mg /200,000 ml
1mg / 200 ml
1000 mcg / 200 ml
5 mcg/ml

62
Q

avoid epi in area of

A

terminal circulation –>
fingers, toes, nears, nose

Hx of
CAD
HTN
arrythmia
uteroplacental insufficiecy

63
Q

A2 agonists + LA

A

100mcg clonidine prolongs LA by 100m

Dex prolongs

64
Q

prolongs DOA of LA

A

epinephrine
dexamethosone
dextran

clonidine?
dexmede?

65
Q

provides supplemental anesthesia

A

clonidine
epinephrine
opiods (neuralaxial)

66
Q

shortens onset time

A

bicarb

67
Q

improves diffusion through tissues

A

hyaluronidase

68
Q

Increases pH so more local anesthetics exist in nonionized state

A

sodium bicrab

69
Q

1:200,000 =

A
70
Q

are associated with a greater incidence of allergic reactions than the use of amides

A

Ester local anesthetics

71
Q

What phase on the cardiac action potential is impacted by locals?

A

phase 0

(Na channel blockers)

72
Q

Iv injection may result in hypotension, cardiac dysrhythmias, and AV block

A

bupivacaine

73
Q

lipid dosing

A

An initial bolus of 1.5 mL/kg 20% lipid emulsion

0.25 mL/kg per minute of infusion -10 minutes after circulatory stability is attained

74
Q

emla

A

5% lidocaine–prilocaine cream

75
Q

1 to 2 g of EMLA cream are applied per

A

a 10 cm2area of skin

76
Q

calculate epi 1:100,000

A

1 gram/100,000mL
1,000mg/100,000mL
1mg/100 mL

0.01mg/mL
10mcg/ml

77
Q
A
78
Q

2% Lidocaine

A

% means parts per hundred
2 grams per cent (100)
2000mg/100 mL
20mg/ mL

79
Q

How many mL of 2% Lidocaine can I give to an 80kg pt?”

A

2% Lido = 20mg/mL
Max dose Lido plain = 5mg/kg
5mg/kg x 80kg = 400mg max for this pt.
400mg divided by 20mg/kg = 20mL Lido 2%

80
Q

max dose bupivicainee

A

2.5 mg/kg
175 mg

81
Q

max dose bupivicaine with epi

A

3 mg/kg
200 mg

82
Q

max dose lidocaine

A

4.5-5 mg/kg
300 mg

83
Q

max dose lidocaine with epi

A

7 mg/kg
500 mg

84
Q

Where are esters metabolized

A

plasma and tissue cholinesterases

85
Q
A
86
Q

if you have an allergy to one ester..

A

you have an allergy to them all

87
Q

esters DOA

A

sshort acting

88
Q

Where are amides metabolized

A

liver

89
Q

Is there a cross-allergy between amides or between amides and esters

A

no

90
Q

are more lipophilic and protein-bound

A

amides

91
Q

resting state of Na channel

A

channel closed

92
Q

active state

A

channel open

93
Q

inactive state

A

channel closed

94
Q

depolarization

A

cell is less negative (more positive)
Na entering cell

95
Q

channel during RMP

A

closed

96
Q

channel during depolarization

A

Open - Na rushes in

97
Q

Inactivation gate

A

Open- but gate blocks Na from entering

98
Q

inactivation gate opens

A

cell repolarizes

99
Q

LA molecular structure

A

aromatic Lipophilic ring + hydrocarbon amine chain + hydrophilic

100
Q

MOA of LA

A

Produce reversible conduction blockade of impulses along central and peripheral nerve pathways

101
Q

Do locals alter RMP or threshold?

A

no

102
Q

Rested-closed and inactivated-closed states.

A

in equillibrium

103
Q

When a local anesthetic interrupts nerve transmission of autonomic nerves but not sensory nerves or motor nerves

A

differential nerve block

104
Q

Sequence of differential nerve block

A

loss of autonomic function
superficial pain
touch
temperature
motor function
proprioception

105
Q

Local that spares motor function, but provides analgesia

A

Bupivacaine

106
Q

what influences sensitivity to LA

A

diameter
myeiination of nerve fibers

107
Q

Which nerve fibers are numbed first by LA

A

B
> C fibers
> A gamma/delta
> A beta/alpha

108
Q

high pKA but fast onset due to high concentration of 3%

A

CHLOROPROCAINE

109
Q

alternate selection when addition of epinephrine to the local anesthetic solution is contraindicated

A

mepivacaine (lacks vasodilator activity)

110
Q

binding site of bupivacaine

A

α1-acid glycoprotein

111
Q

serious side effect of bupivacaine toxicity

A

Cardiac toxicity

most highly protein bound 90% and highly lipid soluble.

112
Q

chosen over Bupivicaine because it is cleared faster to avoid toxicity

A

ropivacaine

113
Q

has a metabolite

A

ropivacaine
lidocaine
prilocaine
esters

114
Q

LA that cause methaglobinemia

A

prilocaine
benzocaine

115
Q

Atypical plasma cholinesterase’s account for prolonged effects and toxicity of drugs such as

A

succinylcholine and chloroprocaine

116
Q

dibucaine number

A

atypical pseudocholinesterase is facilitated by measurement of the degree of enzyme suppression by dibucaine

117
Q

Anesthesia produced by subarachnoid placement of tetracaine will persist until the drug has been

A

absorbed into the systemic circulation

118
Q

slow onset LA

A

procaine (slow and low potency- novacaine)
tetra
bupiv
ropiv

119
Q

fast onset LA’s

A

chloroprocaine
mepivacaine
lidocaine

120
Q

Results from an inadvertent vascular injection or absorption of large amounts of LA from nerve blocks

A

LAST

121
Q

A toxic level of LA results in decreased

A

Contractility & arrythmias

Blockade of the cardiac ion channels will affect initiation and propagation of the contraction, and repolarization

122
Q

Progression of subjective symtoms

A

CNS before CV effects

123
Q

progression of symptoms

A
  1. Excitation, agitation, tinnitus, circumoral numbness
  2. Blurred vision, metallic taste, muscle twitching
  3. Unconsciousness, seizures, CV and resp. arrest
124
Q

IV injection of bupivicaine causes (3)

A

hypotension
dysrthymias (PVC, wide QRS, VTAC)
AV block

125
Q

Cardiotoxic plasma concentrations of bupivacaine

A

8 to 10 µg/mL

126
Q

what drugs worsen bupivicaine cardiotoxicity

A

Epinephrine and phenylephrine

127
Q

The cardiac toxicity is enhanced by

A

arterial hypoxemia
acidosis
hypercarbia

128
Q

Treatment of Last

A

1 Airway (decrease acidosis)
2 seizure (benzo)
3 CV support
4 epi less than 1mck/kg
5 lipid emulsion!!

129
Q

lipid emulsion therapy dose

A

bolus 20% lipid 1.5ml/kg

0.25-0.6 ml/kg/min 10 min later

max dose 10ml/kg for 20 min

130
Q

EMLA

A

5% lidocaine–prilocaine
2.5% lidocaine and 2.5% prilocaine

131
Q

IV injection of a local anesthetic solution into an extremity isolated from the rest of the systemic circulation by a tourniquet

A

BIER block

132
Q

bier block dose

A

50 mL of a 0.5% solution of lidocaine

133
Q

local

A

lidocaine

134
Q

meds for peripherals

A

lido
Bupivacaine, levobupivacaine ropivacaine

135
Q

epidural meds

A

Lidocaine
Bupivicaine –> levobup, ropiv

136
Q

Addition of DISTILLED WATER lowers the specific gravity of local anesthetic solutions below that of CSF

A

hypobaric

137
Q

addition of GLUCOSE to LA solutions increases the specific gravity of local anesthetic solutions above that of CSF

A

hyperbaric

138
Q

max dose of lido in TLA

A

35-55

139
Q

direct effects of LA on cancer patients

A

interference with tumor promoting pathways, and direct toxic effects on tumors when used for local infiltration.

140
Q

Indirect effects of LA on Ca patients

A

result from a reduction of the perioperative stress response and the preservation of the immune response.

141
Q

Plasma concentration is determined by what?

A

rate of tissue distribution
rate of clearance

142
Q

why is ropivacaine more desirable than bupivacaine in terms of systemic toxicity?

A

ropivacaine has a faster clearance

143
Q

spinal anesthesia MOA–> what does it work on

A

preganglionic fibers leaving the spinal cord in anterior ramus

144
Q

TUMESCENT LA max dose

A

55mg/kg

Basics in Anesthesia (5 decks)

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