Module 5 Flashcards

1
Q

local anesthetics are manufactured in ____ use cartridges

A

single

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2
Q

how many mL does each carpule contain

A

1.8 mL

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3
Q

2 % solution is how many mg per carpule

A

36

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4
Q

3 % solution is how many mg per carpule

A

54

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5
Q

4 % solution is how many mg per carpule

A

72

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6
Q

0.5 % solution is how many mg per carpule

A

9 mg

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7
Q

what are the different percentages of solution that local anesthetics are produced as

A

0.5, 2, 3, & 4

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8
Q

what are the carpule contents of local anesthetic agents

A
  • local anesthetic drug
  • sodium hydroxide
  • sodium chloride
  • vasoconstrictor
  • vasoconstrictor preservative
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9
Q

what is often used as the vasoconstrictor in local anesthetic agents

A

EPI or levonordefrin

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10
Q

what is often used as the vasoconstrictor preservative

A

sodium bisulfite

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11
Q

what effect does the sodium bisulfite have

A

decreases solution pH making it more acidic and DELAYING ONSET

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12
Q

what is a negative aspect of sodium bisulfite in local anesthetic agents

A

increases likelihood of allergic reactions to occur

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13
Q

prior to 1984 local anesthetic solutions without EPI added ___ as a preservative

A

methylparaben

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14
Q

what are the 2 groups of local anesthetics

A
  • esters
  • amides
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15
Q

which group of local anesthetics has an increased risk of allergic reactions

A

esters

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16
Q

which group of local anesthetics is metabolized in the blood via pseudocholinesterase

A

esters

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17
Q

which group of local anesthetics is metabolized in the liver

A

amides

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18
Q

which group of local anesthetics is the only one used in dentistry in the US

A

amides

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19
Q

amides have low __ with esters

A

cross-hypersensitivity

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20
Q

T/F if you are allergic to one ester then you are most likely allergic to all esters

A

true

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21
Q

what are the three components of the chemical structure of local anesthetics

A
  • lipophilic aromatic ring
  • intermediate linkage
  • hydrophilic terminal amine
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22
Q

what determines the potency of the local anesthetic and can penetrate the membrane but not bind to the receptors unless it picks up a H+ ion

A

lipophilic aromatic ring

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23
Q

what determines if the local anesthetic is an ester or an amide

A

the intermediate linkage

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24
Q

what dissociates becoming a tertiary amine and enters the nerve to gain a H+ ion and the binds to the receptor site activating the drug

A

hydrophillic terminal amine

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25
Q

what is the term used to describe the physiological effects of the drug on the body

A

pharmacodynamics

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26
Q

local anesthetic molecules in the cartiridge include

A
  • cations = RNH+ = active form that CANNOT cross membrane
  • anions = RN = inactive lipid soluble form CAN cross membrane
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27
Q

all local anesthetics are ___ solutions before injection

A

acidic - more cations than anions

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28
Q

T/F all local anesthetics are vasoconstrictors

A

false - vasodilators

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29
Q

a LOW pKa of a local anesthetic causes what to occur

A

RAPID onset - fast diffusion across the membrane

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30
Q

a HIGH pKa of a local anesthetic causes what to occur

A

SLOW onset - slow diffusion across the membrane

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31
Q

what predicts the proportion of acid : base molecules

A

pKa

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32
Q

A local anesthetic with a low pKa will result in:

a - higher concentration of base molecules, resulting in a fast diffusion across the membrane, resulting in rapid onset
b - higher concentration of acid molecules, resulting in a fast diffusion across the membrane, resulting in rapid onset
c - higher concentration of base molecules, resulting in a slow diffusion across the membrane, resulting in slower onset

A

a - higher concentration of base molecules, resulting in a fast diffusion across the membrane, resulting in rapid onset

33
Q

infected tissues are acidic or basic?

A

acidic (pH of 5-6)

34
Q

when local anesthetic (acidic) is injected into an infected tissue (acidic) what occurs

A

INADEQUATE ANESTHESIA - low concentrations of molecules can cross the membrane

35
Q

RNH+ molecules cannot dissociate H+ ions in acidic tissues so what occurs

A

active form CANNOT enter the cell membrane so INADEQUATE ANESTHESIA

36
Q

local anesthetics must penetrate ___ mm of myelinated nerve length to block a nerve impulse

A

8-10 mm (3-4 nodes of Ranvier)

37
Q

what is required for large nerves

A

increased volume of local anesthetics

38
Q

what is the impact of high concentrations

A

increased diffusion across the membrane leading to RAPID ONSET

39
Q

what is the impact of a low pKa

A

increased RN molecules and base leading to RAPID ONSET

40
Q

what is the impact of high lipid solubility

A

increased POTENCY and decreased dose needed because it enhances the diffusion of the drug through the nerve

41
Q

what is the impact of high protein binding capacity

A

increased DURATION - binds more strongly to the receptor, prolonging the anesthetic presence at the site of action

42
Q

what is the impact of increased vasodilation

A

decreased POTENCY + decreased DURATION + increased DOSE needed

because vasodilation increases blood flow and increases the rate of removal of local anesthetics from the site of action

43
Q

what is the term used to describe the action of the drug within the body

A

pharmacokinetics

44
Q

what is included in pharmacokinetics

A
  • onset of action
  • induction
  • recovery from block
  • reinjection
  • duration / potency
  • distribution
  • absorption
  • biotransformation
  • excretion
  • systemic effects
45
Q

what is a secondary factor of the onset of action

A

site - a small diameter nerve = rapid onset

46
Q

what is the period from local anesthetic deposit to blocked impulse conduction

A

onset of action

47
Q

what is the diffusion of molecules across a membrane

A

induction of local anesthetics

48
Q

what is the primary factor of induction of local anesthetics

A

initial concentration

49
Q

what do anesthetics lose concentration from

A
  • tissue fluid
  • capillaries
  • lymphatics
  • anatomic barriers
50
Q

what is the reversal of local anesthetic action

A

recovery from local anesthetic block

51
Q

what is the primary factor of recovery from local anesthetic block

A

degree of binding (slower process than induction)

52
Q

if nerve fibers are only partially recovered a ___ volume is effective with rapid onset

A

small

53
Q

if nerve fibers are fully recovered what occurs

A

tachyphylaxis / tolerance / ineffective block

54
Q

the degree of protein binding at the receptor site controls which of the following:

a - the duration of anesthetic action
b - the speed of the nerve recovery from local anesthesia
c - both are correct

A

c - both are correct

55
Q

what is the duration of local anesthetic related to

A

potency

56
Q

what are the three factors of duration/potency of local anesthetic

A
  • protein binding
  • vascularity of injection site
  • vasoconstrictor
57
Q

how does protein binding impact duration and potency

A

the stronger the binding the longer the duration and the higher the potency

58
Q

how does vascularity of the injection site impact duration and potency

A

the higher the vascularity the shorter the duration and the lower the potency

59
Q

how does the vasoconstrictor of the local anesthetic impact duration and potency

A

vasoconstriction decreases the blood flow increasing the duration and potency of the local anesthetic

60
Q

how are local anesthetics distributed

A

highly vascular organs have higher concentrations

brain, heart, lungs, liver, kidneys

61
Q

what is directly related to the amount of local anesthetic accumulated in the tissues

A

toxicity

62
Q

high rates of absorption lead to to high__

A

risk of systemic toxicity

63
Q

what are the 5 components of local anesthetic absorption

A
  • total dose administered
  • local anesthetic concentration
  • route of administration
  • vascularity of administration site
  • presence of vasoconstrictor
64
Q

how does increased dose impact absorption

A

increases absorption

all molecules diffuse out of Na+ channels into bloodstream

65
Q

how does increased local anesthetic concentration impact absorption

A

increases absorption

66
Q

how does a topical route of administration impact absorption

A

increases absorption

67
Q

how does intravascular injection impact absorption

A

increases absorption

68
Q

how does increased presence of vasoconstrictor impact absorption

A

decreases absorption

69
Q

ALL local anesthetics are __

A

vasodilators

70
Q

an increased half life increases __

A

risk of systemic toxicity

because drug lingers in tissues for longer

71
Q

what are examples of ester local anesthetics

A
  • benzocaine
  • tetracaine
  • procaine

TOPICAL ONLY

72
Q

what are examples of amide local anesthetics

A
  • lidocaine
  • mepivacaine
  • bupivacaine
  • prilocaine
  • articaine

INJECTABLES & TOPICALS

73
Q

which amide local anesthetics are metabolized only in the liver

A
  • lidocaine
  • mepivacaine
  • bupivacaine
74
Q

where is prilocaine metabolized

A

liver & lungs –> shorter half life

75
Q

where is articaine metabolized

A

plasma & liver –> shortest half life

76
Q

what is the primary excretory organ for all local anesthetics

A

kidneys

77
Q

higher blood levels leads to __

A

increased toxicity

78
Q

toxicity and adverse reactions are directly related to:

A
  • nature of specific local anesthetic
  • concentration
  • route of administration
  • dose administered
  • rate of injection
  • vascularity of site
  • age of patient (child/elder = low rate of metabolism)
  • weight of patient
  • height of patient