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Pharm III Exam 1 > Local Anesthetics And Muslce Relaxants (Lauren 🌭) > Flashcards

Local Anesthetics And Muslce Relaxants (Lauren 🌭) Flashcards

1
Q

What is infiltration anesthesia?

A

Injection of the local anesthetic into the tissue

Advantage: anesthesia without disrupting normal body function (for the most part)

Disadvantage: requires large amounts of drug

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2
Q

Local anesthetics can be esters or amides. Which type has a shorter duration of action?

A

Esters

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3
Q

Which type of local anesthetic has more systemic toxicity: esters or amides?

A

Esters

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4
Q

Local anesthetics are weak (acids/bases)

A

Bases

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5
Q

At physiological pH, local anesthetics are mostly (ionized/non-ionized)

A

Ionized

But the closer to physiological pH, the more LA can be non-ionized so that it can cross the membrane

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6
Q

Where do local anesthetics need to bind to nerve cells to have an effect?

A

Inner membrane, plugging up the Na+ channels

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7
Q

Local anesthetics need to be in the (ionized/non-ionized) form to cross the cell membrane and get inside the nerve cells

A

Non-ionized

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8
Q

How do local anesthetics inhibit action potentials and neuron firing?

A

They plug up Na+ channels from the inside, which prevents

membrane depolarization and therefore, action potentials

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9
Q

When local anesthetics plug up the Na+ channels from the inside, they are in the (ionized/non-ionized form)

A

Ionized

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10
Q

The closer the pKa of an anesthetic is to 7.4, the higher the concentration of it will be in the (ionized/non-ionized) form

A

Non-ionized

Which means it can cross the cell membrane faster and kick in faster

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11
Q

Which will have a faster onset of action: Lidocaine (pKa 7.8) or bupivacaine (pKa 8.1)

A

Lidocaine

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12
Q

What is the exception to the rule regarding being in the ionized vs non-ionized form based on the pH

A

Benzocaine (pKa 3.5), it is ALWAYS in the non-ionized form

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13
Q

How come benzocaine can only be applied topically?

A

Because it is ALWAYS in the non-ionized form no matter what.

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14
Q

Inflammation/infection will (increase/decrease) membrane transport

A

Decrease

Inflammation= acidic=need more drug

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15
Q

What effect will adding bicarbonate to the local anesthetic have?

A

It will make the pH more basic and more of the anesthetic will be in the non-ionized form, so more of it can get across the cell membrane

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16
Q

What is the mechanism of action of local anesthetics?

A

Blocks voltage gated Na+ channels= no action potentials, no firing of neurons

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17
Q

What effect will elevated extracellular calcium have on local anesthetic effect?

A

Hyperpolarizes the membrane, causes more Na+ channels to be in the resting state, and the block is diminished

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18
Q

What effect will elevated extracellular K+ have on the effect of local anesthetic?

A

It depolarizes the membrane, so more of the channels will be in the inactivated state, and the block is enhanced

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19
Q

Local anesthetics have a high affinity for channels in what states?

A

Activated (open) and inactivated states

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20
Q

Local anesthetics have a LOW affinity for sodium channels in what state?

A

Resting (closed) state

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21
Q

Increased lipid solubility will (increase/decrease) the duration of action of a local anesthetic

A

Increase

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22
Q

Procaine has a ________ duration of action

A

Short

Shortest of all of them. It is the standard that all of the others are relative to

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23
Q

Cocaine, Mepivacaine, and Lidocaine have a _________ duration of action

A

Medium

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24
Q

Tetracaine, Bupivacaine, and Ropivacaine have a _______ duration of action

A

Long

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25
Q

The duration of action for a local anesthetic is dependent on (half life/time at site)

A

time at site

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26
Q

The systemic toxicities of local anesthetics are dependent on (half life/time at site)

A

Half life

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27
Q

True or false:

The duration of action of a local anesthetic is dependent on its half life

A

FALSE

Time at site

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28
Q

What factors will affect how much a local anesthetic will be systemically absorbed?

A

Dosage

Site of injection (vascular area vs fat)

Drug-tissue binding

Chemical properties of drug

Local blood flow

Vasoconstricing agents (epinephrine)

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29
Q

Why do we add epinephrine to many local anesthetics?

A

Its a vasoconstrictor, which:

Decreases diffusion of drug

Prolongs duration of action

Decreases systemic absorption

Decreases risk of systemic toxicity

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30
Q

Most local anesthetics are vaso (constrictors/dilators)

A

Vasodilators

Except for Ropivacaine

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31
Q

How are LA’s that are amides metabolized?

A

In the liver by CYP450’s

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32
Q

Which type of LA would be bad for someone with a shitty liver:
Amide or Ester

A

Amide

Metabolized in liver

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33
Q

How are LA’s that are esters metabolized?

A

Rapidly metabolized by butyrylcholinesterases in the plasma

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34
Q

What can affect how quickly someone metabolizes an ester local anesthetic?

A

Mutations in the butyrylcholinesterase enzymes

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35
Q

What is a differential block?

A

The block is not limited to the intended site: pain is blocked, but motor nerves are too.

Can cause paralysis, respiratory impairment, and hypotension

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36
Q

Bupivacaine will hit (sensory/motor) neurons first

A

Sensory

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37
Q

Etidocaine will hit (motor/sensory) neurons first

A

Motor

This is called an inverse differential block. Paralyzed but still feeling pain. FUN!

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38
Q

In general, what is the order that neuron types are affected by LA’s?

A

Sympathetic

Sensory (pain)

Touch

Motor

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39
Q

Which type of nerve fibers are more sensitive to LA’s:

Small diameter or Large diameter

A

Smaller diameter

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40
Q

Which type of nerve fiber is more sensitive to LA’s:

Myelinated or Unmyelinated

A

Unmyelinated

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41
Q

The faster that a nerve fiber conducts, the (more/less) sensitive it is to LAs

A

Less

Slow conducting neurons are more sensitive

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42
Q

LAs will affect myelinated, fast conducting, large diameter neurons last or not at all. Which types of neurons have these properties?

A

Motor neurons

Neurons that detect pressure and temperature

(The ones that don’t usually get affected by LAs)

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43
Q

LAs will affect small, Unmyelinated, slow-conducting nerve fibers the most. Which nerve fiber types have these properties and will be the most sensitive to LAs?

A

Pain

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44
Q

Which local anesthetic has the most cardiac toxicity?

A

Bupivacaine

45
Q

Which type of local anesthetic is most likely to cause hypersensitivity: esters or amides

A

Esters

Allergic reactions RARE with amides

46
Q

Which local anesthetics has a metabolite that may produce methemoglobinemia?

A

Prilocaine

47
Q

Why is lidocaine not recommended for spinal anesthesia?

A

Can cause transient neurological symptoms: pain and dysesthesia (tingling)

48
Q

In general, older anesthetics are (amides/esters) and newer ones are (amides/esters)

A

Older: esters

Newer: amides

49
Q

Ester or amide:

Procaine

A

Ester

50
Q

What is the duration of action of procaine?

A

SHORT

51
Q

What are the two uses for procaine?

A

Infiltration anesthesia (short procedures)

Diagnostic nerve blocks

52
Q

If youre going to get a colonoscopy and the doctor wants to numb up your booty hole for a short period of time, which local anesthetic would be good for this?

A

Procaine

53
Q

Which anesthetic would be good for diagnostic nerve blocks?

A

Procaine

54
Q

Ester or amide:

Tetracaine (Pontocaine)

A

Ester

55
Q

Which anesthetic is 16x more potent and more toxic than procaine?

A

Tetracaine (Pontocaine)

56
Q

Which anesthetic is preferred for ophthalmological use (retrobulbar anesthesia)

A

Tetracaine (Pontocaine)

57
Q

Can Tetracaine (Pontocaine) be used for spinal anesthesia?

A

Yes, when combined with dextrose it becomes heavier than the CSF

58
Q

Ester or amide:

Benzocaine (Americaine)

A

Ester

59
Q

Benzocaine is (very/not at all) lipophilic

A

Very

60
Q

Benzocaine is always in WHAT form

A

Non-ionized (since its pKa is only 3.5)

61
Q

What anesthetic is ONLY used topically for sunburns, minor burns and itching?

A

Benzocaine

62
Q

Ester or amide:

Cocaine

A

Ester

63
Q

Which anesthetic can reduce bleeding and is sometimes used for dental procedures?

A

Cocaine 🦷

64
Q

What is the major MOA of cocaine?

A

Increasing dopamine in the CNS and periphery

The anesthetic effects are secondary

65
Q

What are the adverse effects of cocaine?

A

CNS

Cardiovascular

66
Q

Ester or amide:

Lidocaine

A

Amide

67
Q

Which drug should NOT be used for spinal blocks since it can cause transient neurological symptoms

A

Lidocaine

68
Q

Ester or amide:

Prilocaine

A

Amide

69
Q

Which anesthetic has the highest clearance rate of all the amides, which makes it very safe?

A

Prilocaine

70
Q

What iOS the biggest risk of prilocaine?

A

Methemoglobinemia due to its metabolites

71
Q

Ester or amide:

Bupivacaine

A

Amide

72
Q

Which anesthetic has the highest risk of cardiotoxicity?

A

Bupivacaine 💔

73
Q

For some reason, i decide to get pregnant. When I’m in the delivery room, screaming for an epidural, which local anesthetic will the CRNA inject into my epidural space?

A

Bupivacaine 🤰🏼

74
Q

Bupivacaine is more potent as a (sensory/motor) block

A

Sensory

(Decreases pain, not motor function. Which i thought was the point of all of these, but he made a special mention of this and then said it again in the review, so i guess you should know it)

75
Q

Ester or amide:

Ropivacaine

A

Amide

76
Q

Which LA is the S-enantiomer of Bupivacaine?

A

Ropivacaine

🤚🖐

77
Q

Which has more cardiac toxicity: bupivacaine or its mirror image twin, ropivacine

A

Bupivacaine

78
Q

At clinical doses, what effect does Ropivacaine have on the vasculature?

A

Vaso-constricting!!!

Most others dilate

79
Q

Ester or amide:

Mepivacaine (Carbocaine)

A

Amide

80
Q

Ester or amide:

Etidocaine (Duranest)

A

Amide

81
Q

Which anesthetic has the tendency to cause an inverse differential block, causing motor block before or without a sensory block?

A

Etidocaine (Duranest)

82
Q

Ester or amide:

Articaine (Septocaine)

A

Amide WITH an ester group!!!

=two routes of metabolism

83
Q

Which anesthetic has two routes of metabolism since it is an amide as well as an ester?

A

Articaine (septocaine)

84
Q

Why do we care if articaine (septocaine) has two routes of metabolism?

A

It decreases the half life and thus, potential for systemic toxicity.

Which means when your dentist is drilling away at your teeth and all of a sudden you start feeling pain again, he can inject more of it later in the procedure and not have to worry about systemic toxicity from giving you so much freaking anesthetic, you baby

85
Q

Ester or amide:

Dibucaine (Nupercainal)

A

Amide-type

86
Q

Which anesthetic is used to measure how much butyrylcholinesterase activity someone has, and can identify people with mutations/deficiencies in this enzyme?

A

Dibucaine (Nupercainal)

87
Q

What is the “Dibucaine number test?’

A

Its the test to measure how much butyrylcholinesterase activity you have to see if you can metabolize ester anesthetics

88
Q

Which muscle relaxers (spasmolytics) are centrally-acting?

A

Baclofen (Lioresal)

Cyclobenzaprine (Flexeril)

Diazepam (Valium)

Tizanidine (Zanaflex)

Carisoprodol (Soma)

89
Q

Which muslce relaxers (spasmolytics) are direct acting?

A

Dantrolene

Botox

90
Q

Which receptor is targeted by Diazepam (Valium)?

A

GABA “A” receptor

Causes GABA-mediated inhibition in the spinal cord

91
Q

Which receptor is targeted by Baclofen (Lioresal)

A

GABA “B”

92
Q

What do you need to know about GABA B receptors?

A

They are Ga-i protein coupled and metabotropic

Dont know what this means but he said it in the review

93
Q

What is the MOA of Tizanidine (Zanaflex)?

A

a2 receptor agonist - decreases glutamate

94
Q

What is the MOA of Baclofen (Lioresal)?

A

It is a GABA B agonist, which hyperpolarizes the membranes and inhibits Calcium influx. This decreases transmitter release

95
Q

What are the 2 effects of Tizanidine (Zanaflex)?

A
  1. ) Pre and post-synaptic inhibition of spinal cord activity to decrease muscle spasticity
  2. ) Inhibits pain transmission in dorsal horn
96
Q

What is the MOA of Dantrolene (Dantrium)?

A

Prevents the excitation-contraction coupling of actin and myosin in skeletal muscle fibers

97
Q

What muscle relaxer is used to treat neuroleptic malignant syndrome?

A

Dantrolene (Dantrium)

98
Q

Centrally or Direct acting:

Dantrolene (Dantrium)

A

Direct

99
Q

What is the MOA of Botox?

A

Inhibits ACh release from the nerve at neuromuscular junction

100
Q

How is Botox administered?

A

Injected locally to control muscle spasms

101
Q

The pharmacokinetic property that regulates the duration of action of anesthetics is:

A

Time at site of action

102
Q

Which is a major difference between ester and amide anesthetics:

A. Allergic reactions are common with amides

B. Esters are metabolized by CYP450s and amides are not

C. Esters have less toxicity

D. Amides have different mode of action

E. Esters have a shorter duration of action

A

E. Esters have a shorter duration of action

103
Q

The pharmacokinetic property that regulates the adverse effects and toxicity is:

A

Half life

104
Q

What is an advantage that Ropivacaine has over Bupivacaine ?

A. Absorbed easier

B. Longer duration of action

C. Less potential for adverse effects

D. It is more potent

E. Metabolized in plasma

A

C. Less potential for adverse effects

(It is less lipid soluble and cleared more rapidly, so this leads to lower potential for adverse effects, including less cardiac toxicity than Bupivacaine)

105
Q

Metabolites of prilocaine can cause this condition:

A

Methemoglobinemia

106
Q

What is the prototype amide anesthetic?

A

Lidocaine

107
Q

Which LA’s are Esters?

A

Procaine

Tetracaine

Benzocaine

Cocaine

108
Q

Which LAs are amides?

A

Lidocaine

Prilocaine

Bupivacaine

Mepivacaine

Ropivacaine

Etidocaine

Articaine

Dibucaine

Pharm III Exam 1 (4 decks)

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