Module 5 Flashcards

1
Q

Each carpule of anesthetic contains how many ml

A

1.8

(New FDA law requires it to labeled as 1.7 ml if can’t guarantee all carpules contain exactly 1.8ml)

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2
Q

LA are produced as
2% = how many mg/carpule ?
3%
4%
0.5%

A

2000mg/100ml = 20 mg/ml * 1.8 ml/carpule = 36 mg/carpule

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3
Q

What does a carpule include
1. LA drug
2. Sodium hydroxide = buffering agent
3. Sodium ________ = buffering agent
4. Vasoconstrictor = EPI or __________
5. Vasoconstrictor preservative = __________ _____________ (increase in allergic rxns) - decrease solution pH = more acidic = delayed onset

A
  1. Chloride
  2. Levonordefrin
  3. Sodium Bisulfite
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4
Q

What does a carpule include
1. ___________
2. Sodium __________ = buffering agent
3. Sodium ________ = buffering agent
4. ___________ = EPI or __________
5. Vasoconstrictor preservative = __________ _____________ (increase in allergic rxns) - decrease solution pH = more acidic = delayed onset

A
  1. LA Drug
  2. Hydroxide
  3. Chloride
  4. Vasoconstrictor; Levonordefrin
  5. Sodium Bisulfite
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5
Q

What does a carpule include
1. LA drug
2. Sodium hydroxide = ?
3. Sodium Chloride = ?
4. Vasoconstrictor = EPI or Levonordefrin
5. Vasoconstrictor preservative = Sodium Bisulfite (increase in allergic rxns) - _______ solution pH = more ______ = ________ onset

A
  1. and 3. Buffering agent
  2. Decrease; acidic; delayed
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6
Q

If a patient reports allergic rxn to LA before 1984 consider an allergy to _______ .

A

Parabens

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7
Q

Before 1984 what was added to LA solutions without EPI?

A

Methylparaben added as a preservatives

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8
Q

LA cause reversible local anesthesia by preventing what?

A

generation and conduction of impulses

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9
Q

What does it mean when it says LA provide a chemical block between source of impulse and brain.

A

It means impulse never reaches the brain.

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10
Q

LAs are _______ stabilizing drugs. This means they ____________ (increase/decrease) the rate of depolarization.

A

membrane; decrease

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11
Q

LAs inhibit influx of ____ ion during depolarization.

A

Na+ (they bind to Na channels inside the cell preventing Na from moving inside the cell)

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12
Q

LAs provide what type of blockade?

A

state-dependent blockade

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13
Q

What is a state dependent blockade?

A

LA bind easier to Na+ channels that are firing, NOT resting

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14
Q

What diameter nerve fibers are more sensitive to LAs?

A

Small

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15
Q

What diameter of nerve fiber require more volume of anesthetics?

A

Large

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16
Q

Action of LAs
1. Diffusion through cell membrane
2. Bind to ____ channels inside the membrane
3. Prevents ____ channels from opening
4. Prevent the conduction of a ______ ________ (as long as LA is bound)
5. Prevents neurons from reaching ________ ____________
6. the membrane remains __________

A
  1. Na+
  2. Na+
  3. nerve impulse
  4. firing potential
  5. polarized
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17
Q

What are the two major routes of LA delivery?

A
  1. Topical (more concentration is needed so there is an increase in toxicity)
  2. Submucosal Injection (less concentration needed)
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18
Q

What are the two groups of LAs

A
  1. Esters (ex. novocaine)
  2. Amides
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19
Q

What group of LA is associated with higher allergic rxns?

A

Ester LA

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20
Q

If allergic to one ester probably allergic to all ester (T/F)

A

True

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21
Q

What are esters are metabolized in blood (plasma) by?

A

pseudocholinesterases

Note: very small amounts metabolized in the liver

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22
Q

What group of LA is injectable dental LAs in the US?

A

amides

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23
Q

What organ are amide LAs metabolized by?

A

liver

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24
Q

Amides have a ______ (low/high) cross-hypersensitivity with Esters.

A

low

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25
Q

What is the base/inactive form of LA?

A

Lipophilic aromatic ring

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26
Q

What determines the potency of LAs?

A

Lipophilic aromatic ring

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27
Q

The lipophilic aromatic ring penetrates the membrane and binds to the receptors. (T/F)

A

False: The lipophilic aromatic ring penetrates the membrane BUT can NOT bind to the receptors unless picks up a H+ ion.

NOTE: must be in base form to penetrate the nerve

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28
Q

What does the intermediate linkage determine?

A

If the LA is a ester or amide

29
Q

What is the hydrophilic terminal amine responsible for?

A

Dissociates becoming a tertiary amine then enters the nerve. It gains a H+ ion (ionized) binds to receptor sites = active form.

Note: It can’t enter the ion unless it lose H+ ion and then pick it back up inside the cell.

30
Q

What does the hydrophilic terminal amine become when it dissociates?

A

tertiary amine

31
Q

Base molecules is unstabilized _______ _________ then penetrate the nerve then pick up the H ion creating an ionized ______ _______ which then binds to receptors sites WITHIN the nerve.

A

tertiary amines; quaternary amine

32
Q

LA molecules in the cartridge include:

A

A. Cation (acid)
B. Anion (base)

33
Q

Active form of a drug that cant cross the membrane.

A

Cation

34
Q

Lipid soluble form of the drug that crosses membrane (inactive).

A

Anion (base form)

35
Q

All LA are _____ (acidic/basic) solutions before injection.

A

acidic

(which means more cations than anions in the solution)

36
Q

Are LAs vasodilators or vasoconstrictors?

A

vasodilators

37
Q

Decrease in pka = ?
Increase in pka = ?

A

Decrease in pka = increase in anions = increase base = rapid onset
Increase in pka = increase in cations = decrease in base = slow onset

38
Q

A increase in PKA means a ______ onset.

A

slow

39
Q

The pka of a molecule represent the ___ at which ____% of the molecule exist in the lipid-soluble ____ form and _______% in the water-soluble ______ form. It is the proportion of cation to base molecules when manufactured.

A

The pka of a molecule represent the pH at which 50% of the molecule exist in the lipid-soluble tertiary form and 50% in the water-soluble quaternary form.

40
Q

Effect of Infection on LAs (infected tissues have a pH of 5-6.0)

A

LAs are acidic and when injected into acidic tissues there is a decrease of molecules crossing the membrane = inadequate anesthesia

41
Q

How many mm must LA penetrate through of myelinated nerve length (3-4 nodes of ranvier) to block a nerve impulse?

A

8-10 mm

42
Q

Increase in concentration = (increase/decrease) in diffusion through membrane = (slow/rapid) onset

A

increase; rapid

43
Q

Increase in lipid solubility = (increase/decrease) potency = (increase/decrease) dose needed

A

increase; decrease

44
Q

Increase vasodilation of LA = (increase/decrease) potency + (increase/decrease) duration = (increase/decrease) in dose need

A

decrease potency; decrease duration; increase dose needed

Note: this is because increase in vasodilation increases blood flow and increase removal of LA molecules from site

45
Q

Period of LA deposit to blocked impulse conduction. Which category of pharmacokinetics does this fall under?

A

Onset of action

46
Q

What is the primary and secondary factor under the category of action?

A
  1. PKA of LA is the primary factor (Low pka = rapid onset)
  2. Site is the secondary factor (small diameter nerves = rapid onset)
47
Q

Diffusion of molecules across the membrane. Which category of pharmacokinetics does this fall under?

A

Induction of LAs

48
Q

What is the primary factor for induction of LAs?

A

Initial concentration (increase in [ ] = increase in diffusion = rapid onset)

49
Q

What causes anesthetic to lose [ ]?

A

Tissue fluid
Capillaries
Lymphatic
Anatomic barriers

50
Q

What is the primary factor in recovery from a LA block?

A

Degree of binding to the receptor site

51
Q

Which is slower induction or recovery from a LA block?

A

recovery from LA block

52
Q

Reinjection of LA in the case of partially recovered vs fully recovered?

A

partially - small volume is effective with rapid onset
fully recovered - tachyphylaxis occurs = tolerance to LA and LA is ineffective

53
Q

What are the 3 factors of duration of LA = potency?

A
  1. Protein binding
  2. Vascularity (increase in vascularity = decrease in potency and duration)
  3. Vasoconstrictors (decrease in blood flow = increase in potency and duration)
54
Q

Distribution: After absorption LAs are distributed throughout the body. (T/F)

A

True

55
Q

Distribution: Highly vascualr organs have rgeat concentrations (such as brain, heart, lungs, liver, and kidneys) (T/F)

A

True

56
Q

Toxicity is (indirectly/directly) related to the amount of LA in accumulated tissues

A

Directly

57
Q

How does this affect absorption?
Increase in dose =
Increase in [ ] =
Topical =
Intravascular injection =
Presence of vasoconstrictor =

A

ALL increase absorption except presence of vasocontrictor

58
Q

A increase in half life = (increase/decrease) risk for systemic toxicity

A

increase because greater amount in tissues for longer

59
Q

Ester LAs include topicals (there are 3)

A
  1. Benzocaine
  2. Tetracaine
  3. Procaine

bradley takes percocet

60
Q

Amide LAs include injectable and topicals (there are 5)

A
  1. Lidocaine
  2. Mepivacaine
  3. Bupivacaine
  4. Prilocaine
  5. Articaine

Leave me by pizza, alright.

61
Q

What three amides are metabolized in the liver only?

A
  1. Lidocaine
  2. Mepivacaine
  3. Bupivacaine
62
Q

What is prilocaine metabolized in?

A

Liver and lungs (shorter half life due to lung metabolism)

63
Q

What LA is 90% metabolized in the plasma and 10% in the liver?

A

Articaine

64
Q

What amide LA has the shortest half life?

A

Articaine

65
Q

What is the primary excretory organ for all LAs?

A

Kidneys

Greater percentage of amides are excreted unchanged in the urine than esters even though it’s still a small small amount.

66
Q

Children and elderly have (increase/decrease) rate of metabolism.

A

decrease

67
Q

If the weight is lower you would give a ______ dose.

A

lower

68
Q
A
69
Q

When do systemic effects of LA happen?

A

After absorbed into the blood BUT before metabolized (affect CNS and CV)