Local Anesthetics (Exam #1) Flashcards

1
Q

In what two ways do Esters differ from Amides?

A

ESTERS have…

  • Shorter DOA
  • MORE systemic toxicity
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2
Q

How are local anesthetics transported across cell membranes?

A
  • Non-ionized form to cross

- Ionized form to bind intracellularly

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3
Q

What type of base are most local anesthetics, and at physiological pH, what form dominates?

How would this change their activity if the extracellular pH is more acidic? More basic?

A

LAs = weak bases
- At pH of 7.4, ionized form dominates

  • If more ACIDIC environment = ionized dominates, so LESS activity because can’t cross membrane
  • If more BASIC environment = non-ionized dominates, so MORE activity because more crosses and then becomes ionized → can bind
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4
Q

What is the exception to the pKa/pH rule for local anesthetics, and what does this mean for its use?

A

Benzocaine has pKa of 3.5 and NON-ionized dominates

- Topical use only because unable to bind within cell

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5
Q

What is the MOA for all local anesthetics?

A

Block Na channels

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6
Q

What type of axon are blocks more effective in? How do elevated Ca vs. elevated K affect the block?

A

Block MORE effective in rapidly firing axons (NOT resting)

  • High Ca = block diminished (channels in resting state)
  • High K = block enhanced (channels in open/firing state)
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7
Q

How is duration of action determined for local anesthetics?

A

DOA = time at site of action

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8
Q

Which local anesthetic is SHORT duration of action? Which is INTERMEDIATE? Which three are LONG?

A
  • Short: Procaine
  • Intermediate: Lidocaine
  • Long: TBR (Tetracaine, Bupivicaine, Ropivicaine)
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9
Q

How are amides metabolized? How are esters metabolized?

A
  • Amides = CYP450s (liver)

- Esters = butyrylchlolinesterases

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10
Q

What is a differential block, and what are two examples of different blocks? What is the order of sensitivity from most to least sensitive?

A

Differential block: different degrees of sensory and motor blocks
- Bupivacaine = sensory before motor (epidural)
- Etidocaine = motor before sensory (inverse diff. block)
Sympathetic > Sensory > Touch > Motor

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11
Q

What characteristic of fibers makes them MORE sensitive? Which two characteristics make them LESS sensitive?

A
  • More sensitive: smaller diameter

- Less sensitive: myelinated, faster conduction velocity

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12
Q

What AE differs between esters and amides?

A

Esters are MORE likely to cause hypersensitivity

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13
Q

What local anesthetic has an AE of increased CV toxicity?

A

Bupivacaine (amide)

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14
Q

What local anesthetic has an AE of methemoglobinemia, and how might this present?

A

Prilocaine (amide)

- Chocolate colored skin

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15
Q

Is Procaine an ester or amide? What is its DOA, and what is its primary use?

A

ESTER
- SHORTEST duration of action

Used for diagnostic blocks

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16
Q

Is Tetracaine an ester or amide? What is its DOA, and what does this mean for its use?

What is its primary use?

A

ESTER
- LONG duration of action = more potent and more AEs

Used for ophthalmology

17
Q

Is Benzocaine an ester or amide? What is its primary use, and why is this important?

A

ESTER

Used topically ONLY bc exception to pH rule

18
Q

Is Cocaine an ester or amide? What is its MOA, and in what two ways might it be used?

A

ESTER
- Increase DA → block Na channels

Can be used as topical anesthesia or for dental procedures to reduce bleeding

19
Q

Is Lidocaine an ester or amide? What is its DOA, and what are its two primary uses? What is it NOT used for?

A

AMIDE
- INTERMEDIATE duration of action

GO-TO: used for infiltration blocks and epidural anesthesia
- NOT spinal blocks

20
Q

Is Prilocaine an ester or amide?

21
Q

What is an important note about Prilocaine compared to other amides?

A

Prilocaine has the highest rate of clearance of all amides = SAFER

22
Q

Is Bupivacaine an ester or amide? What is its DOA? What is its primary use, and why is this?

A

AMIDE
- LONG duration of action

Used for epidural blocks in labor/childbirth because more potent SENSORY block than motor

23
Q

What is the primary AE associated with Bupivacaine? What similar drug can be used as an alternative, and why?

A

Cardiac toxicity

- Ropivacaine is the enantiomer of Bupivacaine and is LESS lipid soluble/cleared more rapidly than Bupivacaine

24
Q

What two reasons might Ropivacaine be used?

A
  • Vasoconstriction effects (most other LAs are vasodilating)

- Less cardiac toxicity than Bupivacaine

25
What drug is associated with an inverse differential block, and what does this mean?
Etidocaine | - Motor nerves acted on before sensory nerves
26
Which drug is both an amide AND an ester, and what is its primary use?
Articaine | - Used in dental medicine (allows for multiple injections throughout procedure if needed)
27
What drug can be used to evaluate for butyrylchlinesterase mutations?
Dibucaine
28
Is Dibucaine an ester or amide? What is its primary use?
AMIDE | - Dibucaine Number Test = butyrylchlinesterase mutations
29
What is the MOA of Diazepam, and what does this mean? What type of a muscle relaxant is it?
Acts on GABA A rec. → inhibits Cl channels | - Centrally-acting
30
What is the MOA of Baclofen, and what does this mean? What type of a muscle relaxant is it?
Acts on GABA B rec. → inhibits Ca influx via Gi proteins | - Centrally-acting
31
What is the MOA of Tizanidine? What type of a muscle relaxant is it?
a2 receptor agonist | - Centrally-acting
32
What is the MOA of Dantrolene, and what does this mean? What type of a muscle relaxant is it?
Inhibits Ca release → interferes with excitation-contraction coupling (actin/myosin) - Direct-acting
33
What is the MOA of Botulinum Toxin? What type of a muscle relaxant is it?
Inhibits ACh release | - Direct-acting
34
What PK property regulates AEs/toxicity?
Half life