Local Anesthetics Flashcards

1
Q

Ester linkage - shorter duration of action

A

Procaine

  • metabolized in plasma
  • hydrolyzed by butyrylcholinesterase
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2
Q

Amide linkage

A

Lidocaine

  • metabolized in liver; excreted unchanged
  • hydrolyzed by CYP450 (hepatic disease - toxicity)
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3
Q

More potent/longer duration of action/Lipophilic –> less potent/shorter duration of action/less Lipophilic

A

Tetracaine > Bupicaine > Ropivacaine > Lidocaine > Procaine > Mepivacaine

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4
Q

What can cause gangrene in tissues supplied by end areas?

A

Epinephrine - Vasoconstrictor

in muscle: activates b2 Rc = dilation but increase potential for toxicity

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5
Q

CNS adverse effects

A
  • low conc = sleepy, lightheaded, visual/auditory disturbances
  • high conc = nystagmus, muscle twitching, convulsion
    (Give premedication - benzodiazepines to increase seizure threshold and decrease chances for CNS toxicity)
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6
Q

Heart adverse effects

A
  1. Bupivacaine - MOST cardiotoxic –> long duration
  2. Lidocaine - Class 1b antiarrthymic –> inc electrical stimulation threshold of ventricle, spont depol of ventricles during diastole
  3. Cocaine - Vasoconstriction, hypertension, cardiac arrhythmia
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7
Q

Which is the only local anesthetic that doesn’t block Na channels?

A

Cocaine

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8
Q

Ester linkage or amide linkage more prone to allergic rxns?

A

Ester linkage

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9
Q

Benzocaine

A
  • poor water solubility

- TOPICAL agent (hemorrhoids, lubricant)

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10
Q

Bupivacaine

A
  • long duration

- sensory block > motor block

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11
Q

Cocaine

A
  • block nerve impulses

- TOPICAL anesthetic of upper resp tract

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12
Q

Dibucaine

A

TOPICAL CREAM only

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13
Q

Lidocaine

A
  • amide (given if sensitive to ester)
  • faster, intense, long lasting, extensive anesthesia
  • antiarrythmial
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14
Q

Procaine

A
  • low potency/slow onset/short duration
  • ONLY USED for infiltration anesthesia
  • metabolized by para-aminobenzoic acid –> inhibits action of sulfonamide antibiotics
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15
Q

Ester linkage - shorter duration of action

A

Procaine

  • metabolized in plasma
  • hydrolyzed by butyrylcholinesterase
How well did you know this?
1
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3
4
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16
Q

Amide linkage

A

Lidocaine

  • metabolized in liver; excreted unchanged
  • hydrolyzed by CYP450 (hepatic disease - toxicity)
17
Q

More potent/longer duration of action/Lipophilic –> less potent/shorter duration of action/less Lipophilic

A

Tetracaine > Bupicaine > Ropivacaine > Lidocaine > Procaine > Mepivacaine

18
Q

What can cause gangrene in tissues supplied by end areas?

A

Epinephrine - Vasoconstrictor

in muscle: activates b2 Rc = dilation but increase potential for toxicity

19
Q

CNS adverse effects

A
  • low conc = sleepy, lightheaded, visual/auditory disturbances
  • high conc = nystagmus, muscle twitching, convulsion
    (Give premedication - benzodiazepines to increase seizure threshold and decrease chances for CNS toxicity)
20
Q

Heart adverse effects

A
  1. Bupivacaine - MOST cardiotoxic –> long duration
  2. Lidocaine - Class 1b antiarrthymic –> inc electrical stimulation threshold of ventricle, spont depol of ventricles during diastole
  3. Cocaine - Vasoconstriction, hypertension, cardiac arrhythmia
21
Q

Which is the only local anesthetic that doesn’t block Na channels?

A

Cocaine

22
Q

Ester linkage or amide linkage more prone to allergic rxns?

A

Ester linkage

23
Q

Benzocaine

A
  • poor water solubility

- TOPICAL agent (hemorrhoids, lubricant)

24
Q

Bupivacaine

A
  • long duration

- sensory block > motor block

25
Q

Cocaine

A
  • block nerve impulses

- TOPICAL anesthetic of upper resp tract

26
Q

Dibucaine

A

TOPICAL CREAM only

27
Q

Lidocaine

A
  • amide (given if sensitive to ester)
  • faster, intense, long lasting, extensive anesthesia
  • antiarrythmial
28
Q

Procaine

A
  • low potency/slow onset/short duration
  • ONLY USED for infiltration anesthesia
  • metabolized by para-aminobenzoic acid –> inhibits action of sulfonamide antibiotics