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
what is the term used to describe the physiological effects of the drug on the body
pharmacodynamics
26
local anesthetic molecules in the cartiridge include
- cations = RNH+ = active form that CANNOT cross membrane - anions = RN = inactive lipid soluble form CAN cross membrane
27
all local anesthetics are ___ solutions before injection
acidic - more cations than anions
28
T/F all local anesthetics are vasoconstrictors
false - vasodilators
29
a LOW pKa of a local anesthetic causes what to occur
RAPID onset - fast diffusion across the membrane
30
a HIGH pKa of a local anesthetic causes what to occur
SLOW onset - slow diffusion across the membrane
31
what predicts the proportion of acid : base molecules
pKa
32
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 - higher concentration of base molecules, resulting in a fast diffusion across the membrane, resulting in rapid onset
33
infected tissues are acidic or basic?
acidic (pH of 5-6)
34
when local anesthetic (acidic) is injected into an infected tissue (acidic) what occurs
INADEQUATE ANESTHESIA - low concentrations of molecules can cross the membrane
35
RNH+ molecules cannot dissociate H+ ions in acidic tissues so what occurs
active form CANNOT enter the cell membrane so INADEQUATE ANESTHESIA
36
local anesthetics must penetrate ___ mm of myelinated nerve length to block a nerve impulse
8-10 mm (3-4 nodes of Ranvier)
37
what is required for large nerves
increased volume of local anesthetics
38
what is the impact of high concentrations
increased diffusion across the membrane leading to RAPID ONSET
39
what is the impact of a low pKa
increased RN molecules and base leading to RAPID ONSET
40
what is the impact of high lipid solubility
increased POTENCY and decreased dose needed because it enhances the diffusion of the drug through the nerve
41
what is the impact of high protein binding capacity
increased DURATION - binds more strongly to the receptor, prolonging the anesthetic presence at the site of action
42
what is the impact of increased vasodilation
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
what is the term used to describe the action of the drug within the body
pharmacokinetics
44
what is included in pharmacokinetics
- onset of action - induction - recovery from block - reinjection - duration / potency - distribution - absorption - biotransformation - excretion - systemic effects
45
what is a secondary factor of the onset of action
site - a small diameter nerve = rapid onset
46
what is the period from local anesthetic deposit to blocked impulse conduction
onset of action
47
what is the diffusion of molecules across a membrane
induction of local anesthetics
48
what is the primary factor of induction of local anesthetics
initial concentration
49
what do anesthetics lose concentration from
- tissue fluid - capillaries - lymphatics - anatomic barriers
50
what is the reversal of local anesthetic action
recovery from local anesthetic block
51
what is the primary factor of recovery from local anesthetic block
degree of binding (slower process than induction)
52
if nerve fibers are only partially recovered a ___ volume is effective with rapid onset
small
53
if nerve fibers are fully recovered what occurs
tachyphylaxis / tolerance / ineffective block
54
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
c - both are correct
55
what is the duration of local anesthetic related to
potency
56
what are the three factors of duration/potency of local anesthetic
- protein binding - vascularity of injection site - vasoconstrictor
57
how does protein binding impact duration and potency
the stronger the binding the longer the duration and the higher the potency
58
how does vascularity of the injection site impact duration and potency
the higher the vascularity the shorter the duration and the lower the potency
59
how does the vasoconstrictor of the local anesthetic impact duration and potency
vasoconstriction decreases the blood flow increasing the duration and potency of the local anesthetic
60
how are local anesthetics distributed
highly vascular organs have higher concentrations brain, heart, lungs, liver, kidneys
61
what is directly related to the amount of local anesthetic accumulated in the tissues
toxicity
62
high rates of absorption lead to to high__
risk of systemic toxicity
63
what are the 5 components of local anesthetic absorption
- total dose administered - local anesthetic concentration - route of administration - vascularity of administration site - presence of vasoconstrictor
64
how does increased dose impact absorption
increases absorption all molecules diffuse out of Na+ channels into bloodstream
65
how does increased local anesthetic concentration impact absorption
increases absorption
66
how does a topical route of administration impact absorption
increases absorption
67
how does intravascular injection impact absorption
increases absorption
68
how does increased presence of vasoconstrictor impact absorption
decreases absorption
69
ALL local anesthetics are __
vasodilators
70
an increased half life increases __
risk of systemic toxicity because drug lingers in tissues for longer
71
what are examples of ester local anesthetics
- benzocaine - tetracaine - procaine TOPICAL ONLY
72
what are examples of amide local anesthetics
- lidocaine - mepivacaine - bupivacaine - prilocaine - articaine INJECTABLES & TOPICALS
73
which amide local anesthetics are metabolized only in the liver
- lidocaine - mepivacaine - bupivacaine
74
where is prilocaine metabolized
liver & lungs --> shorter half life
75
where is articaine metabolized
plasma & liver --> shortest half life
76
what is the primary excretory organ for all local anesthetics
kidneys
77
higher blood levels leads to __
increased toxicity
78
toxicity and adverse reactions are directly related to:
- 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