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D2 Summer > Pain and Anxiety Week 2 > Flashcards

Pain and Anxiety Week 2 Flashcards

1
Q

New FDA law requires LA carpule labeling to say?

A

1.7 mL

(each carpule contains 1.8 mL but law requires labeling to say 1.7 mL if manufacturer cannot guarantee all carps contain exactly 1.8 mL)

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2
Q

Which LA is no longer available in the US?

A

2% Lidocaine Plain

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3
Q

LAs are manufactured in _________ ________ cartridges/carpules

A

single use

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4
Q

What are the 4 possible % solutions LAs can be produced as?

A

0.5%
2%
3%
4%

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5
Q

What 5 things can be included in LA carpules?

A

LA drug
Sodium hydroxide (buffering agent)
Sodium chloride (buffering agent)
Vasoconstrictor (epi or levonordefrin)
Vasoconstrictor preservative (sodium bisulfite)

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6
Q

Name 2 buffering agents that can be in the carpule

A

sodium hydroxide and sodium chloride

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7
Q

The vasoconstrictor present in the carpule

A

epi or levonordefrin

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8
Q

This vasoconstrictor preservative helps decrease the solution pH (more acidic) to delay the onset of the LA

A

Sodium bisulfite

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9
Q

If a pt reported that they had an allergic rxn to a LA before 1984, then what were they probably allergic to?

A

Parabens

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10
Q

Prior to 1984, LA solutions without epi added _________________ as a preservative, which increased ________ _______, so it is no longer added to LAs

A

methylparaben; allergic rxns

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11
Q

What are the 2 ways LAs cause reversible local anesthesia?

A

preventing generation and conduction of impulses

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12
Q

LAs provide a ________ _______ between source of impulse and brain (impulse never reaches the brain)

A

chemical block

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13
Q

LAs are known as “___________ ___________ drugs,” meaning they decrease the rate of depolarization

A

membrane-stabilizing

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14
Q

What do LAs inhibit the influx of during depolarization?

A

Na+

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15
Q

LAs bind to Na+ channels inside/outside the cell

A

LAs bind to Na+ channels INSIDE the cell

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16
Q

What do LAs provide to allow easier binding to Na+ channels that are firing (NOT resting)?

A

State-dependent blockade

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17
Q

Small diameter nerves are……

A

More sensitive to LAs

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18
Q

Large diameter nerves require…..

A

More volume of LAs

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19
Q

Name the 5 actions of LAs

A
  1. Diffuse through neuron cell membrane
  2. Bind Na+ channels (inside cell membrane)
  3. Prevent Na+ channels from opening
  4. Prevents conduction of nerve impulse
  5. Prevents neuron from reaching firing potential
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20
Q

2 major routes of LA delivery

A
  1. Topical (applied on mucosa, higher concentration needed to penetrate mucosa, higher toxicity)
  2. Submucosal injection (more effective, less concentrations needed)
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21
Q

2 groups of LAs

A

Esters
Amides

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22
Q

Esters are metabolized in the ______ via _____________ while amides are metabolized in the _________

A

blood (plasma); psuedocholinesterase; liver

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23
Q

ALL injectables LAs are…

A

Amides

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24
Q

Topical LAs can be…

A

Esters or amides

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25
Q

Which group of LA has the most allergic reactions?

A

Esters

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26
Q

Amides have a low _______________ with esters

A

cross-hypersensitivity

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27
Q

Describe the chemical structure of LAs

A

1) lipophilic aromatic ring
2) intermediate linkage
3) hydrophilic terminal amine

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28
Q

Characteristics of the lipophilic aromatic ring of LA

A

Base = inactive form
Determines potency
Penetrates membrane, but CANNOT bind receptors unless it picks up H+

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29
Q

What does the intermediate linkage of LA determine?

A

If the LA is ester or amide

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30
Q

Characteristics of the hydrophilic terminal amine of LA

A

Dissociates becoming tertiary amine -> enters nerve -> gains H+ -> ionized -> binds to receptor sites -> ACTIVE form

CANNOT enter neurons until it loses H+, must pick it up again inside

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31
Q

Once the LA has gained a ________ ion, it’s now in it’s ___________ form

A

H+; active

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32
Q

Cation form of LA

A

Active
Only binds to sites within nerve

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33
Q

Anionic form of LA

A

Inactive
Does NOT bind to receptor sites

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34
Q

Physiological effects of drug on the body

A

Pharmacodynamics

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35
Q

L.A. molecules in the cartridge include anions and cations. How do they differ with their onset?

A

More anions: low pKa, more base, fast diffusion, rapid onset

More cations: high pKa, less base, slow diffusion, slow onset

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36
Q

All LAs are __________ solutions before injection, meaning there are more __________ than ________ in the cartridge

A

acidic; cations; anions

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37
Q

Higher pKa means what?

A

Less base
Slower onset of action

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38
Q

Lower pKa means what?

A

More base
Rapid onset of action

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39
Q

Infected tissues are __________

A

acidic

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40
Q

What happens when you inject LA into infected, acidic tissue?

A

Less molecules cross the membrane = INADEQUATE ANESTHESIA

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41
Q

What happens to the H+ in infected, acidic tissue?

A

RNH+ molecules cannot dissociate H+, so the active form CANNOT enter the cell membrane

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42
Q

What does RNH+ refer to?

A

Cation (acid) = ACTIVE form that CANNOT cross membrane

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43
Q

What does RN refer to?

A

Anion (base) = INACTIVE, lipid soluble form that CAN cross the membrane

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44
Q

L.A. must penetrate _______mm of myelinated nerve length (3-4 nodes of Ranvier) to block a nerve impulse

A

8-10mm

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45
Q

↑___________ of L.A. is required for large nerves (inferior alveolar n.)

A

volume

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46
Q

Increased concentration of LA means…

A

Increased diffusion through membrane
Rapid onset

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47
Q

Low pKa of LA means…

A

Increased RN molecules (anions)
Increased base
Rapid onset

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48
Q

High lipid solubility of LA means…

A

Increased potency
Decreased dose needed (enhances diffusion of drug through nerve)

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49
Q

Increased protein binding of molecules in LA means…

A

Increased duration

(binds more strongly to receptor, prolonging anesthetic presence at site of action)

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50
Q

Increased vasodilation of LA means…

A

Decreased potency + Decreased duration
Must increase dose!

(vasodilation = increased blood flow = increased removal of LA molecules from site)

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51
Q

Describe the onset if there is a high concentration of the LA and it has a low pKa

A

Rapid onset

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52
Q

What happens to the dosage if the lipid solubility decreases?

A

Increase the dose

(to enhance diffusion of drug through the nerve)

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53
Q

What happens to the duration of the LA if there is increased protein binding?

A

Increased duration

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54
Q

T/F: LAs are vasodilators

A

True

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55
Q

Period from LA deposit to blocked impulse conduction

A

Onset of action

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56
Q

What is the primary factor for determining the onset of action of a LA?

A

pKa!!

low pKa = rapid onset
high pKa = slow onset

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57
Q

What does pKa determine the amount of?

A

Ionized molecules in solution

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58
Q

What is the secondary factor for determining the onset of action of a LA?

A

Site!!

small diameter nerves = rapid onset

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59
Q

Diffusion of molecules across membrane

A

Induction of LAs

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60
Q

What is the primary factor for determining the induction of a LA?

A

Initial concentration of LA

inc conc = inc diffusion = rapid onset
dec conc = dec diffusion = slow onset

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61
Q

Name some areas in the body where the anesthetic loses concentration from

A

Tissue fluid
Capillaries
Lymphatics
Anatomic barriers (bone)

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62
Q

Reversal of LA action

A

Recovery from LA block

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63
Q

What is the primary factor for determining the duration of action and speed of nerve recovery?

A

Degree of protein binding

(different for each LA, depends on chemicals)

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64
Q

T/F: Recovery is a slower process than induction

A

True

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65
Q

If you try to reinject LA and the nerve fibers are only partially recovered (pt still numb), what volume of LA is effective and what is the speed of onset of action?

A

Small volume is effective
Rapid onset of action

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66
Q

If you try to reinject LA and the nerve fibers are fully recovered (no numbness), what can occur?

A

Tachyphylaxis = tolerance to LA = LA is ineffective!

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67
Q

Potency

A

Duration of LA

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68
Q

What are the 3 factors that affect the duration/potency of LA?

A

Protein binding
Vascularity of injection site
Vasoconstrictor in LA

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69
Q

Stronger protein binding means _________ duration and __________ potency

A

increased; increased

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70
Q

Increased vascularity of injection site means ___________ duration and ___________ potency

A

decreased; decreased

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71
Q

Presence of a vasoconstrictor in the LA means ___________ blood flow, ___________ duration, and ___________ potency

A

decreased; increased; increased

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72
Q

After absorption, where are LAs distributed?

A

Throughout body

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73
Q

Which organs have higher concentrations of LA?

A

Highly vascular organs

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74
Q

Name 5 examples of highly vascular organs that will have higher concentrations of LA

A

Brain
Heart
Lungs
Liver
Kidneys

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75
Q

What is toxicity directly related to?

A

Amount of LA accumulated in tissues

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76
Q

Increased absorption means there is an __________ risk of systemic ___________

A

increased; toxicity

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77
Q

Increased dose means there is ____________ absorption. All molecules diffused out of _______ channels into ____________

A

increased; Na+; bloodstream

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78
Q

Increased concentration means there is ____________ absorption

A

increased

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79
Q

Which route of administration will allow for increased absorption?

A

Topical

80
Q

An intravascular injection will cause __________ absorption

A

increased

81
Q

Increased vasoconstrictor in the LA will cause ____________ absorption

A

decreased

82
Q

T/F: The presence of a vasoconstrictor increases absorption.

A

FALSE

it decreases bc you’re constricting the blood vessel so less flows into bloodstream

83
Q

All LAs are _______________

A

vasodilators!

84
Q

Biotransformation refers to the ____________ of a drug

A

metabolism

85
Q

How is biotransformation measured?

A

In half-life (time for 50% of drug to be removed)

86
Q

Increased half life means ___________ risk for systemic toxicity

A

increased

(the drug is lingering around in tissue for much longer)

87
Q

Name 3 ester LAs

A
  1. Procaine
  2. Tetracaine
  3. Benzocaine
88
Q

What is the route of administration for ester LAs?

A

Topical

89
Q

What is the route of administration for amide LAs?

A

Injectable and topical

90
Q

Which amide LAs are metabolized in the liver only, and therefore have an increased toxicity in liver disease?

A

Lidocaine
Mepivacaine
Bupivacaine

91
Q

Which amide LA is metabolized in the liver AND lungs?

A

Prilocaine

92
Q

Which amide LA is metabolized in plasma (90%) and liver (10%)?

A

Articaine

93
Q

Which amide LA has the SHORTEST half life?

A

Articaine

94
Q

What is the primary excretory organ for all LAs?

A

Kidneys

95
Q

Where are a small amount of ester LAs excreted?

A

Unchanged in urine

96
Q

Where are a greater % of amide LAs excreted?

A

Unchanged in urine

(small amount, even tho more than esters)

97
Q

Why is there an increased risk of systemic toxicity of LAs in patients with severe renal disease?

A

Due to build up of drug when not cleared by kidneys

98
Q

Although small amounts of both esters and amides L.A.s are excreted unchanged in urine, which is excreted in a greater percent this way?

A

Amides

99
Q

At what point can LAs affect the CNS and CV system?

A

After they are absorbed into blood (before metabolized)

(↑blood levels = ↑toxicity)

100
Q

Toxicity and adverse reactions of LAs are directly related to what? (9)

A

1) Nature of specific L.A. (vasodilation)
2) Concentration of drug
3) Route of administration
4) Dose administered
5) Rate of injection
6) Vascularity of site
7) Age of patient
8) Weight of patient
9) Health of patient

101
Q

Order of selection of LAs (5)

A

1) duration of pain control needed
2) need for post op pain control
3) patient’s health assessment and current meds
4) allergic to the LA or sodium bisulfite
5) need for hemostasis

102
Q

What is the highest concentration of epinephrine?

A

1:50,000

103
Q

What is the lowest concentration of epinephrine?

A

1:200,000

104
Q

If a pt is allergic to wine, dried fruit, or dried potatoes, then we assume they have a ___________ allergy

A

bisulfite

105
Q

T/F: Most LAs are short-acting.

A

FALSE!

Most are intermediate-acting (60 mins of pulpal anesthesia)

106
Q

Which LA is most commonly used in dentistry for nerve blocks?

A

Lidocaine

107
Q

Which LA is good for hemostasis if 1:50,000 epi?

A

Lidocaine

108
Q

Which LA is NOT available in US without epi?

A

Lidocaine

109
Q

What is the duration of Lidocaine?

A

60 mins

110
Q

Lidocaine brand name?

A

Xylocaine

111
Q

Which LA is an effective topical and is the only amide topical?

A

Lidocaine

112
Q

What is the onset of action of Lidocaine?

A

2-3 mins

113
Q

Where is Lidocaine metabolized? What is the 1/2 life?

A

Liver (half life = 1.6 hrs)

114
Q

What is the pregnancy category for Lidocaine?

A

pregnancy = category B; lactation safe

115
Q

Which LA is a good choice if vasoconstrictor is contraindicated?

A

Mepivacaine

116
Q

Which LA is NOT used for hemostasis since there is no epi?

A

Mepivacaine

117
Q

Which LA is a WEAK vasodilator? (2)

A

Mepivacaine
Prilocaine

118
Q

What is the duration of Mepivacaine (without epi and with levo)?

A

Duration w/o epi = 20-40 mins
Duration w/ levo = 60 mins

119
Q

What is the onset of action of Mepivacaine?

A

1.5-2 mins

120
Q

Where is Mepivacaine metabolized? What is the 1/2 life?

A

Liver (half life = 1.9 hrs)

121
Q

What is the pregnancy category for Mepivcaine?

A

pregnancy = category C; lactation safe

122
Q

Mepivacaine brand name?

A

Carbocaine

123
Q

Which LA is the LEAST toxic in dentistry?

A

Prilocaine

124
Q

Which LA is the BEST choice for pregnancy + CV pts?

A

Prilocaine

125
Q

Which LA has a risk of methemoglobinemia?

A

Prilocaine

126
Q

What patients should you be worried about for methemoglobinemia risk with Prilocaine?

A

COPD patients

127
Q

Which LA has no anticonvulsant properties? (2)

A

Prilocaine
Articaine

128
Q

Which LA is an effective topical when combined w/ lido?

A

Prilocaine

129
Q

What is the duration of Prilocaine (with and without epi)?

A

Duration w/o epi = 40-60 mins
Duration w/ epi = 60-90 mins

130
Q

What is the onset of action of Prilocaine?

A

2 mins

131
Q

Where is Prilocaine metabolized? What is the 1/2 life?

A

Lungs + small amount in liver (half life = 1.6 hrs)

132
Q

What is the pregnancy category for Prilocaine?

A

pregnancy = category B; lactation unknown safety

133
Q

Prilocaine brand name?

A

Citnest

134
Q

Which LA has a risk for IA nerve injury?

A

Articaine

134
Q

Which LA is highly lipid soluble and has high diffusion thru bone?

A

Articaine

135
Q

What is the pregnancy category for Articaine?

A

pregnancy = category C; lactation unknown safety

136
Q

What is the duration of Articaine (with 1:100,000 epi and 1:200,000 epi?

A

Duration with 1:100,000 epi = 60-75 mins
Duration with 1:200,000 epi = 45-60 mins

137
Q

What is the onset of action of Articaine?

A

1-3 mins

138
Q

Where is Articaine metabolized? What is the 1/2 life?

A

Plasma (90%) + liver (half life = 45 mins)

139
Q

Which LA is NOT an effective topical? (2)

A

Articaine
Bupivacaine

140
Q

Which LA is highly lipid soluble and has high diffusion thru bone?

A

Articaine

141
Q

Which LA is a good choice in CV + liver disease pts?

A

Articaine

142
Q

Articaine brand name?

A

Septocaine

143
Q

Which LA is MOST potent and toxic?

A

Bupivacaine

144
Q

Which LA is the MOST potent vasodilator?

A

Bupivacaine

145
Q

Which LA is good for long treatment?

A

Bupivcaine

146
Q

Which LA has a HIGH toxicity risk?

A

Bupivcaine

147
Q

T/F: You MUST give Bupivacaine with a vasoconstrictor (not available w/o epi)

A

True

148
Q

What is the duration of Bupivacaine?

A

1.5-3 hours

149
Q

What is the onset of action for Bupivacaine?

A

5-10 mins

150
Q

Where is Bupivacaine metabolized? What is the 1/2 life?

A

Liver (half life = 2.7 hrs)

151
Q

What is the pregnancy category for Bupivacaine?

A

pregnancy = category C; lactation unknown safety

152
Q

Bupivacaine brand name?

A

Marcaine

153
Q

The CNS is very sensitive to high levels of LA because they?

A

Readily cross BBB

154
Q

Has this pt suffered from a moderate or high overdose of LAs?

Presents with:
increased HR, RR, BP, and also has muscle twitching with tremors

A

Moderate

155
Q

Has this pt suffered from a moderate or high overdose of LAs?

Presents with:
decreased HR, RR, BP, they’re convulsing and experiencing unconsciousness

A

High!

They are progressing to respiratory arrest due to CNS depression

156
Q

Has this pt suffered from a moderate or high overdose of LAs?

Presents with:
increased HR, RR, BP, headache and feeling lethargic

A

Moderate!

They have initial cardiovascular stimulation

157
Q

Has this pt suffered from a moderate or high overdose of LAs?

Presents with:
decreased HR, RR, BP, slurred speech, disoriented

A

High!

Progressing to cardiac arrest and cardiac depression

158
Q

2 vasoconstrictors used in US

A

Epinephrine
Levonordefrin

159
Q

4 functions of vasoconstrictors

A

1) constrict blood vessels @ site
2) increase duration of LA (6x longer)
3) provides hemostasis at injection site
4) decrease absorption rate of LA (and risk of toxicity)

160
Q

Which vasoconstrictor affects alpha and beta receptors equally?

A

Epi

161
Q

T/F: Levonordefrin affects the alpha receptors more.

A

True! 75% is alpha and 25% is beta

162
Q

MRD for epi (healthy pt and CV disease)

A

Healthy MRD = 0.2 mg
CV disease = 0.04 mg

163
Q

MRD for levonordefrin (healthy pt and CV disease)

A

Healthy MRD = 1.0 mg
CV disease = 0.2 mg

164
Q

An overdose usually occurs via which route?

A

Intravascular injection

165
Q

How fast due overdose symptoms appear? How long does it take for the body to clear the drug?

A

Symptoms appear within 60 seconds
Body clears within 5-10 mins

166
Q

Symptoms of an overdose (6)

A

1) dysrhytmias
2) increased HR + BP
3) headache
4) hyperventilation
5) tremors
6) anxiety

167
Q

What does an overdose lead to in patients with CV disease?

A

Cardiac arrest

168
Q

Absolute contraindication for LA

A

Allergy

169
Q

Relative contraindications of LA (6)

A

1) H2 receptor blocker
2) Beta blocker
3) CNS depressants
4) Pregnancy
5) Significant liver disease
6) Renal dysfunction

170
Q

H2 receptor blockers decrease liver metabolism. What do you do when a pt is taking a H2 receptor blocker?

A

Decrease dosage of lidocaine

171
Q

Beta blockers decrease amide metabolism. What do you do when a pt is taking a beta blocker?

A

Decrease dosage of all amides

172
Q

CNS depressants can decrease metabolism. What do you do when a pt is taking a CNS depressant?

A

Decrease dosage of all amides

173
Q

What do you do if your pt is pregnant?

A

Use prilocaine or lidocaine

174
Q

Significant liver disease decreases amide metabolism. What do you do if your pt has significant liver disease?

A

Use articaine and/or decrease dosage of all amides

175
Q

Renal dysfunction decreases excretion. What do you do if your pt has renal dysfunction?

A

Use LAs with caution

176
Q

Absolute contraindications for vasocontrictors (5)

A

MI/coronary bypass surgery within 3-6 months
Uncontrolled hypertension, angina, arrythmias, hyperthyroidism
Sulfite allergy
Glaucoma
Cocaine/methamphetamine use

(basically anything heart related)

177
Q

Relative contraindications of vasoconstrictors (4)

A

CVD pts
Tricyclic antidepressants
Nonselective beta blockers
Digitalis

178
Q

What is cardiac protocol?

A

0.04 mg epi
0.2 mg levo

179
Q

What do you do if your pt has CV disease?

A

Cardiac protocol

180
Q

What do you do if your pt is taking tricyclic anti-depressants?

A

No levo
0.04 mg epi

181
Q

What do you do if your pt is taking a nonselective beta blocker?

A

Cardiac protocol

182
Q

What do you do if your pt is taking digitalis?

A

Consult physician

183
Q

MRD stands for

A

Max recommended dose

184
Q

What is MRD adjusted to accommodate?

A

Pts medical status

185
Q

We use the lowest effective dose for…

A

Elderly
Children
Medically compromised

186
Q

MRD is based on…

A

Maximum dose per appointment
Body weight

187
Q

MRD is calculated as…

A

mg/lb or mg/kg

188
Q

MRD and AMD of Lidocaine

A

MRD: 3.2 mg/lb
AMD: 500 mg

189
Q

MRD and AMD of Mepivacaine

A

MRD: 3.0 mg/lb
AMD: 400 mg

190
Q

MRD and AMD of Prilocaine

A

MRD: 4.0 mg/lb
AMD: 600 mg

191
Q

MRD and AMD of Articaine

A

MRD: 3.2 mg/lb
AMD: none

192
Q

MRD and AMD of Bupivacaine

A

MRD: none
AMD: 90 mg

193
Q

How many mg of epi per carpule?

A

0.018 mg

194
Q

In healthy pts, the ______________ is the limiting drug, but in cardiac pts the _______________ is the limiting drug

A

LA; vasoconstrictor

D2 Summer (37 decks)

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