Quiz 4 Local Anesthetics Flashcards

1
Q

Where do local anesthetics (LA) have a better access to the axon on myelinated nerves?

A

at the Nodes of Ranvier

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2
Q

What channels do LA work on to block signals on a nerve axon?

A

Na+ channels

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3
Q

Local anesthetics are greatly facilitated if the drug is in the ____________ or _________ state

A

Uncharged or non-ionized state

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4
Q

What is a quick way of telling whether the LA is an amide or ester anesthetic?

A

The Amides have 2 “i” in the name, ex. Lidocaine, Ropivacaine….

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5
Q

What correlates well with the LA’s potency?

A

Lipid solubility

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6
Q

What are some factors that affect the minimum blocking concentration of a LA?

A
  • Fiber size
  • fiber type
  • myelination
  • pH of tissues
  • pKa of LA
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7
Q

T/F - a LA with a pKa closer to physiologic pH will have a higher concentration of IONZED form and can readily pass through the nerve cell membrane.

A

False - non-ionized

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8
Q

Why do LA’s with higher lipid solubility have greater potency?

A

they are less likely to be cleared by blood flow

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9
Q

Which Amides have the highest and lowest potency?

A

Highest - Bupivacaine (duration 200+ min)

Lowest - Mepivacaine (duration 45-90 min)

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10
Q

Which Ester has the highest potency?

A

Tetracaine (duration 200+ min)

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11
Q

What are 2 factors that will help determine the sensitivity of the nerve to a LA?

A
  1. Axonal Diameter: Small > Large

2. Myelination: Unmyelinated > myelinated

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12
Q

In spinal nerves, which is most sensitive to local anesthetics: Autonomic, sensory, or motor?

A

Autonomic is most sensitive.

Autonomic > Sensory > Motor

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13
Q

Systemic absorption of LA depends on what?

A
  • blood flow to area being injected
  • vasoconstrictors
  • specific LA agent (high or low lipid solubility)
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14
Q

Which LA is the only one to not produce relaxation of vascular smooth muscle?

A

Cocaine - causes vasoconstriction which makes it great for nosebleeds and ENT procedures

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15
Q

If most LA’s cause relaxation of vascular smooth muscle, what could happen to your anesthetic?

A
  • increased absorption
  • decreased duration of action
  • increased probability of systemic/toxic effects
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16
Q

How are Esters metabolized?

A

By pseuodcholinesterase, water soluble metabolites excreted through urine

17
Q

Which 2 esters are metabolized by PABA and associated with allergic reactions?

A

Procaine and benzocaine

18
Q

How are Amides metabolized?

A

P-450 and metabolism is slower than with Esters but are excreted through urine, also.

**Decrease in liver fxn will reduce metabolism and increase toxicity”

19
Q

What are 2 LA’s that are implicated for causing methemoglobinemia?

A

Prilocaine - amide
Benzocaine spray - ester

++Treat with methylene blue

20
Q

T/F: The slower a local anesthetic is absorbed into the vascular space, the less likely that high blood levels and subsequent CNS or cardiac toxicity will occur.

A

True

21
Q

If you have 1% lidocaine, what is the concentration of that drug? (g/ml)

A

1 gram per 100 ml

22
Q

What environments will cause ion trapping and what will it do to anesthetics?

A
  • Acidosis, injection into acidotic/infected tissues, septic pts
  • causes higher accumulation of drug, which will prolong duration of action
23
Q

Effects of LA on CNS?

Effects of LA on cardiovascular?

A

CNS - convulsions - increased O2 consumption in presence of compromised ventilation
Cardiovascular - depresses automaticity, reduced refractory period, depressed contractility/conduction, vasodilation,

Bradycardia -> heart block -> hypotension -> cardiac arrest

24
Q

How long do you need to leave EMLA cream on to get satisfactory analgesia?

A

1 hr covered in occlusive dressing

25
Q

What sites are good for topical anesthesia?

A

Mucus Membranes: nose, mouth, tracheobronchial tree, esophagus, GU tract

**absorption of LA through Mucus Membranes is significant and can cause systemic toxicity

26
Q

What sites should you NOT use epinephrine in your LA’s?

A

Should NOT be injected around end arteries like:

  • fingers/toes
  • Ears/Nose
  • Genitals
27
Q

What are concentrations of LA used for infiltration?
Lidocaine -
Procaine -
Bupivacaine -

A

Lido - 0.5 - 1%
Pro - 0.5 - 1%
Bupiv - 0.125 - 0.25%

28
Q

What is Transient Neuologic Symptoms (TNS)?

A

dyesthesia, burning pain, and aching in lower extremities/buttocks associated with use of lidocaine in spinal

29
Q

Methemoglobinemia becomes an issue in patient’s with severe ________ or ________ failure.

A

anemia, heart