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pharm II > Chapter 10 LA > Flashcards

Chapter 10 LA Flashcards

1
Q

amides

A
  • lidocaine
  • prilocaine
  • ropivicaine
  • bupivicaine
  • articaine
  • mepivacaine
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1
Q

esters

A
  • cocaine
  • procaine
  • chloroprocaine
  • tetracaine
  • benzocaine
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2
Q

miscellaneous LA

A
  • EMLA cream
  • hyaluronidase (wydase, virtase, others) –> sometimes added to LA to help spread
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3
Q

intermediate chain is an

A

ester or amide linkage

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4
Q

T/F benzene ring is lipophilic

A

True

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4
Q

T/F Quaternary amide is hydrophilic

A

True

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5
Q

LA have 3 things always

A
  • lipid soluble side
  • water-soluble side
  • amide/ester linkage
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6
Q

amide’s have a __ in chain

A

nitrogen

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7
Q

ester’s have a __ in chain

A

oxygen

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8
Q

how are esters broken down?

A

catalyzed by plasma and tissue cholinesterase via hydrolysis; occurs throughout the body

IS RAPID

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9
Q

esters have a __ allergy potential

A

higher

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10
Q

if patients exhibit an allergy to any ester drug, all other esters should be

A

avoided

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11
Q

what is the longest acting ester?

A

tetracaine

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12
Q

amides are metabolized in the

A

liver by CYP1A2 and CYP3A4

and thus a significant blood level may develop witha rapid absorption

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13
Q

T/F allergy to amides are extremely common

A

false

extremely rare

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14
Q

amides are longer acting because they are more

A

lipophilic and protein-bound and require transport to the liver for metabolism

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14
Q

absorption =

A

offset

absorption of LA offsets its action, its done working

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15
Q

there is no __ __ among amide class or between the ester and amide agents

A

cross allergy

just allergic to that amide NOT all the amides

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16
Q

Type A beta fiber:
function, myelination/diameter, anesthetic block onset

A
  • touch, pressure
  • heavy 5-12 µm
  • intermediate
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16
Q

Type A gamma fiber:
function, myelination/diameter, anesthetic block onset

A
  • muscle tone
  • heavy 3-6 µm
  • intermediate
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17
Q

Type alpha A fiber:
function, myelination/diameter, anesthetic block onset

A
  • proprioception, motor
  • heavy, 12-20 µm
  • last
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18
Q

Type A delta fiber:
function, myelination/diameter, anesthetic block onset

A
  • pain, cold temperature, touch
  • heavy 1-5 µm
  • intermediate
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19
Q

Type B fiber:
function, myelination/diameter, anesthetic block onset

A
  • preganglionic autonomic vasomotor
  • light, < 3
  • early
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20
Q

Type C dorsal root fiber:
function, myelination/diameter, anesthetic block onset

A
  • pain, warm and cold temperature, touch
  • none, 0.4-0.12
    early
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20
Q

Type C sympathetic fiber:
function, myelination/diameter, anesthetic block onset

A
  • postganglionic vasomotor
  • none, 0.3-1.3
  • early
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21
Q

which LA are chiral drugs because the molecules possess an asymmetric carbon atom

A

mepivacaine, bupivacaine, ropivacaine

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22
Q

which amide LA’s have a long DOA

A

bupivicaine
ropivicaine

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23
Q

which amide LA’s have a medium DOA

A

lidocaine
mepivacaine
prilocaine

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24
Q

which ester LA has a medium DOA

A

cocaine

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25
Q

which ester LA has a short DOA

A

procaine

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26
Q

which ester LA has a topical only DOA

A

benzocaine

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27
Q

which ester LA has a long DOA

A

tetracaine

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28
Q

LA cause temporary loss of __ __ without loss of consciousness by blocking conduction along __ nerve fibers

A

pain sensation; sensory

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29
Q

some selectivity for pain afferents is acheived partly by using the agent close to

A

target neurons

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30
Q

LA are either strong acids or weak bases?

A

weak bases

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30
Q

all currently used drugs block

A

voltage-dependent Na channels in excitable cells

which decreases the likelihood of an action potential

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31
Q

the target site of the drugs is on the

A

cytoplasmic side of the neuron membrane

so drug molecules must pass through the membrane

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32
Q

LA exist in __ between ionized and nonionized forms

A

equilibirum

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33
Q

lipophilic forms diffuse more __ through the membrane

A

readily

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34
Q

hydrophilic diffuse more readily though

A

cytoplasm

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35
Q

because LA act on excitable cells then can cause toxicity including:

A

fatal cardiovascular effects or seizures

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36
Q

what characteristics of LA increases when epi is added?

A
  • degree of motor blockade
  • degree of sensory blockade
  • duration of blockade
  • area of blockade
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37
Q

does onset time increase or decrease when epi is added to LA?

A

decreases

*except during spinal anesthesia

38
Q

what characteristics of LA increase when the dose is increased (volume or concentration)?

A
  • degree of motor blockade
  • degree of sensory blockade
  • duration of blockade
  • area of blockade
  • peak plasma concentration
39
Q

does onset time increase or decrease when the dose is increased of LA (volume or concentration)?

A

decrease

40
Q

peak plasma concentraiton __ with the addition of epi to LA

A

decreases

41
Q

what is the usual dose of epi when added to a LA?

A

5 µm/mL or 1:200,000

42
Q

epi is usually added to LA to __ the __ of vascular absorption

A

decrease; rate

allowing more anesthetic molecules to reach the nerve membrane and improve the depth and duration of A

42
Q

adding epi can also be used as a __ for inadvertent intravascular injection

A

marker

43
Q

dose mg/kg for procaine 1%

A

14

44
Q

dose mg/kg for tetracaine 1%

A

1

MOST TOXIC LA

44
Q

dose mg/kg for chloroprocaine 3%

A

11 (14)

45
Q

dose mg/kg for cocaine 4%

A

3 (topical) –> 200mg total

46
Q

dose mg/kg for lidocaine 1%

A

4 (7)

47
Q

dose mg/kg for lidocaine 2%

A

4 (7)

48
Q

dose mg/kg for mepivacaine 2%

A

4 (7)

49
Q

dose mg/kg for prilocaine 3%

A

7 (8.5)

50
Q

dose mg/kg for bupivacaine 0.75%

A

2.5 (3.2)

51
Q

dose mg/kg for ropivaciane 0.75%

A

3 (3.5)

52
Q

variation occurs in single injection dose depending on

A

the type of LA and the location of the block

53
Q

in the event of LA overdose, respiratory depression may occur resulting in __ & __

A

hypoxia; acidosis

54
Q

the acidosis may increased the

A

ionized fraction of LA within the cerebral circulation thereby DECREASING its ability to cross the blood/brain barrier

cannot leave the brain to reenter systemic circulation!! very bad!!

55
Q

LA accumulation in the fetal circulation is enhanced by

A

fetal pH is lower than the maternal pH this may result in high fetal levels of LA

56
Q

LA injected into acioditic, infected tissues are __ due to the loss of lipid solubility

A

ineffective

57
Q

LA lipid solubility is diminished in an acidotic environment d/t

A

increased concentration of the ionized (water-soluble) form of the drug

loss of lipid solubility prevents ABSORPTION INTO THE NERVE thereby preventing access to the site of action

58
Q

carbonation of LA __ the onset and intensity of of action of neural blockafe

A

speeds

59
Q

CO2 readily diffuses into the nerve __ the pH within the nerve

A

lowering

60
Q

the lipid-soluble form of the LA after passing through the neuronal membrane will receive

A

protons from the intra-neuronal environment and ionize

60
Q

increasing th eionized fraction within the neuron produces

A

higher concentration of the active form of the anesthetic available at the Na channel (site of action)

61
Q

T/F CO2 makes the outside of the nerve more acidic

A

false

inside of the nerve

62
Q

commercialy available LA are prepared in a slightly

A

acidic formulation

improves stability by increasing the concentration of the ionized form of the drug

63
Q

addition of Na bicarb to the LA mixture increased the

A

pH of the solution thereby increasing the concentration of the non-ionized form of the drug

64
Q

improving lipid solubility of the LA improves

A

diffusion of the LA through the neuronal membrane leading to a more rapid onset of action

65
Q

Basic solution make the __ of the nerve more __ and easier for LA to __ onset of action

A

outside; basic; increase

66
Q

fetus has a more __ environment than mom

A

acidic

67
Q

one of the most important factors of how fast a LA will work it its

A

pKa

67
Q

the lower the pKa the ___ the onset

A

faster

the greater the portion of nonionized drug available, and the drug needs to be non-ionized to penetrate the nerve

68
Q

the exception is __ the pKa is 8.7

A

chloroprocaine

but its still the fastest LA because we give it a high concentration 3%

68
Q

the more protein bound a LA =

A

the longer the duration of action

69
Q

how does a more protein-bound LA make it last longer?

A

if it binds to stronger proteins, it binds to tissues/nerves and therefore takes longer to be released

70
Q

Why do we add epinephrine to locals?

A

to increase the duration of action and decrease toxicity!

71
Q

unique properties of cocaine

A
  • naturally occurring
  • comes from coca plants
  • sigmund freud introduced it into medicine
72
Q

T/F cocaine is extremely potent

A

True

  • can only be used as a topical NOT injectable (Max dose 200mg)
  • blocks the reuptake of norepinephrine and epinephrine –> sympathomimetic effects
73
Q

LA accumulation in the fetal circulation is enhanced by

A

the fact that the fetal pH is lower than the maternal pH

this may result in high fetal levels of LA

74
Q

lipid solubility correlates with

A

potency

*greater lipid solubility enhances diffusion through neural coverings and cell membranes allowing a lower mg dosage

75
Q

dissociation constant (pKa) correlates with

A

time of onset

*determines the portion of an administered dose that exists in the lipid-soluble, tertiary molecular state at a given pH. Agents having a lower pKa have a greater proportion in the tertiary, diffusible state, and the hastens onset

76
Q

chemical linkage correlates with

A

metabolism

*esters are principally hydrolyzed in plasma by cholinesterases. Amides are primarily biotransformed within the liver

77
Q

protein binding correlates with

A

duration

*affinity for plasma proteins also corresponds to affinity for protein at the receptor site within Na channels, prolonging the presence of anesthetic at the site of action

78
Q

symptoms of the therapeutic level of LAST

A
  • lightheadedness
  • tinnitus
  • circumoral and tongue numbness
79
Q

Stage 2 of LAST

A

visual disturbances and muscular twitching and convulsions

80
Q

stage 3 of LAST

A

coma and unconsciousness

81
Q

bupivacaine binds to

A

certain cardiac proteins

  • binds to the heart preferentially over any other tissue
82
Q

stage 4 of LAST

A

respiratory arrest & CVS depression

83
Q

T/F bupivacaine can be used for IV regional

A

FALSE

binds to the cardiac proteins causing cardiac arrest

84
Q

the spectrum of presenting signs:
CNS: CV: combination

A

45%: 11%: 44%

85
Q

spectrum of CNS signs

A
  • seizure 68%
  • dizziness, drowsiness, tinnitus, perioral, confusion,dysphoria, dysarthria 11%
  • loss of consciousness 7%
  • agitation 11%
86
Q

spectrum of CV signs

A
  • bradycardia/asystole 27%
  • hypotension 18%
  • tachycardia 16%
  • wide complex 12%
  • VT/VF 13%
87
Q

when does LAST usually occur in 50% of cases?

A

in less than 1 minute

88
Q

when does LAST usually occur in 25% of cases?

A

1 to 5 mins

89
Q
A
90
Q
A
91
Q
A
92
Q
A
92
Q
A
93
Q
A

pharm II (2 decks)

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