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Nurs 575 Anesthesia Pharmacology > Local Anesthetics (week 8) > Flashcards

Local Anesthetics (week 8) Flashcards

1
Q

What are the important differences between Amides & Esters?

besides the i

A
  • Metabolism
  • Allergy potential
  • Duration of action

Nagelhout 7th ed, Ch. 25, pg. 123, Table 10.2

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2
Q

Which bond is this?

A

Ester

-CO-

Nagelhout 7th ed, Ch. 25, pg. 122, Fig 10.7

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3
Q

Which bond is this?

A

Amide

-NHC-

Nagelhout 7th ed, Ch. 25, pg. 122, Fig 10.7

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4
Q

Procaine potency and onset?

A
  • 1
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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5
Q

Procaine Duration and Max dose?

A
  • 45-60min
  • 500mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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6
Q

Chloroprocaine potency and onset?

A
  • 4
  • Rapid

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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7
Q

Tetracaine potency and onset?

A
  • 16
  • slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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8
Q

Lidocaine potency and onset?

A
  • 1
  • Rapid

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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9
Q

Prilocaine potency and onset?

A
  • 1
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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10
Q

Chloroprocaine duration and max dose?

A
  • 30-45 min
  • 600 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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11
Q

Tetracaine duration and max dose?

A
  • 1-3 hrs
  • 100mg (topically)

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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12
Q

Lidocaine duration and max dose?

A
  • 1-2hrs
  • 300 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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13
Q

Prilocaine duration and max dose?

A
  • 1-2 hrs
  • 400 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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14
Q

Mepivacaine potency and onset?

A
  • 1
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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15
Q

Bupivacaine potency and onset?

A
  • 4
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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16
Q

Levobupivacaine potency and onset?

A
  • 4
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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17
Q

Ropivacaine potency and onset?

A
  • 4
  • Slow

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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18
Q

Mepivacaine duration and max dose?

A
  • 1.5-3 hrs
  • 300 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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19
Q

Bupivacaine duration and max dose?

A
  • 4-8hrs
  • 175 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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20
Q

Levobupivacaine duration and max dose?

A
  • 4-8 hrs
  • 175 mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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21
Q

Ropivacaine duration and max dose?

A
  • 4-8 hrs
  • 200mg

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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22
Q

Procaine pKa?

A

8.9

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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23
Q

Chloroprocaine pKa?

A

8.7

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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24
Q

Tetracaine pKa?

A

8.5

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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25
Q

Lidocaine pKa?

A

7.9

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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26
Q

Prilocaine pKa?

A

7.9

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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27
Q

Mepivacaine pKa?

A

7.6

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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28
Q

Bupivacaine pKa?

A

8.1

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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29
Q

Levobupivacaine pKa?

A

8.1

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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30
Q

Ropivacaine pKa?

A

8.1

Stoelting’s 5th ed, Ch. 10, pg. 284, Table 10.1

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31
Q

Liposomal LA benefits?

A
  • Prolong Duration of action
  • Decrease Toxicity

Stoelting’s 5th ed, Ch. 10, pg. 283

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32
Q

Which drugs are used in Lipsomal formulations?

A
  • Lidocaine
  • Tetracaine
  • Bupivicaine

Stoelting’s 5th ed, Ch. 10, pg. 283

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33
Q

Mechanism of action of LAs?

A

LAs bind to the internal α-subunits on voltage gated Na+ channels, inhibiting passage of Na+ through ion-specific channels.

Stoelting’s 5th ed, Ch. 10, pg. 297

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34
Q

What effects do LAs have on nerve conduction?

A

Slows depolarization -> Threshold potential not reached -> Action potentials not generated

Stoelting’s 5th ed, Ch. 10, pg. 297

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35
Q

What state(s) must the Na+ voltage gated channel be in in order for LAs to bind?

A

Inactivated-closed

Stoelting’s 5th ed, Ch. 10, pg. 298

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36
Q

What state(s) can the Na+ voltage gated channel be in?

A
  • Inactivated-closed
  • Resting-closed
  • Activated-open

Stoelting’s 5th ed, Ch. 10, pg. 298

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37
Q

Definition of Cm?

A
  • Miniumum effective concentration
  • of LA to produce conduction blockade of nerve impulses

Stoelting’s 5th ed, Ch. 10, pg. 300

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38
Q

What is Cm similar to?

A

MAC for inhaled anesthetics

Stoelting’s 5th ed, Ch. 10, pg. 300

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39
Q

How does Cm of Motor fibers compare to sensory fibers?

A

Cm of Motor fibers approx. twice that of sensory fibers

Stoelting’s 5th ed, Ch. 10, pg. 300

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40
Q

True/False: Motor & Sensory blockade always accompany ea. other

A

Negative, Ghost Rider
* sensory anesthesia may NOT always be accompanied by skeletal muscle paralysis

Stoelting’s 5th ed, Ch. 10, pg. 300

41
Q

Using a LA with the same Cm, is more or less volume required for spinal or epidural anesthesia? Why?

A

More volume for Epidural
* LAs are provided VIP access to them unprotected nerves in subarachnoid space

Stoelting’s 5th ed, Ch. 10, pg. 300

42
Q

What changes in response to LAs occurs during Pregnancy? Why?

A
  • Increased sensitivity
  • More rapid onset

Protein-binding characteristics change -> more unbound, pharmacologically active drug

Stoelting’s 5th ed, Ch. 10, pg. 300

43
Q

Is there concern for the fetus during pregnancy with the use of LAs?

A

Yes, may be significant placental transfer of LA from Mother -> fetus

Stoelting’s 5th ed, Ch. 10, pg. 301

44
Q

When might placental transfer be of concern?

A
  • Prolonged labor
  • Acidosis in the fetus causing ion trapping

Stoelting’s 5th ed, Ch. 10, pg. 301

45
Q

Which has a more rapid onset, Lidocaine or Bupivicaine? Why?

A

LAs with pKa closer to physiological pH (7.4) have more rapid onset
Lidocaine pKa = 7.9
Bupivicaine pKa = 8.1

Stoelting’s 5th ed, Ch. 10, pg. 300

46
Q

Are LAs acids or bases?

A

Weak bases
pKa 7.6 ~ 8.1

Stoelting’s 5th ed, Ch. 10, pg. 300

47
Q

What intrinsic property of LAs influence potency and duration of action? Why?

A
  • Vasodilatory activity
  • vasodilation results in faster/greater systemic absorption -> metabolized

Stoelting’s 5th ed, Ch. 10, pg. 300

48
Q

Between Lidocaine & Mepivacaine, which has a shorter duration of action? Why?

A

Lidocaine
* Mepivacaine does not have vasoactive effects (specifically vasodilatory)

Stoelting’s 5th ed, Ch. 10, pg. 300

49
Q

Absorption of LA is influenced by what 4 things?

A
  • Site of injection
  • Dosage
  • Use of Epi
  • Pharmacological characteristics of the drug

Stoelting’s 5th ed, Ch. 10, pg. 300

50
Q

Are LA water or Lipid soluble?

A

Lipid soluble

Stoelting’s 5th ed, Ch. 10, pg. 288

51
Q

What percent of LAs are renally excreted? Any exceptions?

A
  • 5% unchanged in urine
  • Cocaine is 10-12% renally excreted unchanged

Stoelting’s 5th ed, Ch. 10, pg. 289

52
Q

What part of LAs (amides or esters) can be renally excreted? Any examples?

A
  • Water-soluble metabolites are readily excreted in urine
  • PABA (paraaminobenzoic acid) from metabolism of esters

Stoelting’s 5th ed, Ch. 10, pg. 289

53
Q

Where are Amide LAs metabolized?

A

Microsomal enzymes in the liver

Stoelting’s 5th ed, Ch. 10, pg. 289

54
Q

List the Amides in the order of rate metabolized

A
  • Rapid - Prilocaine
  • Intermediate - Lido/Mepivacaine
  • Slow - Bupivacine/Ropivacaine

Stoelting’s 5th ed, Ch. 10, pg. 289

55
Q

Is systemic toxicity more likely with Amides or Esters? Why?

A

Amides

  • Esters are rapidly metabolized by plasma esterases

Stoelting’s 5th ed, Ch. 10, pg. 289

56
Q

Are cumulative effects more likely with Amides or Esters?

A

Amides

Stoelting’s 5th ed, Ch. 10, pg. 289

57
Q

How are esters metabolized?

A

Hydrolysis by Cholinesterase in the plasma

Stoelting’s 5th ed, Ch. 10, pg. 290

58
Q

In what order are the Esters metabolized?

A
  1. Rapid - Chloroprocaine
  2. Intermediate - Procaine
  3. Slow - Tetracaine

Stoelting’s 5th ed, Ch. 10, pg. 290

59
Q

What metabolite(s) of Ester LAs are antigenic?

A

Paraaminobenzoic acid (PABA)

Stoelting’s 5th ed, Ch. 10, pg. 290

60
Q

How frequent are allergic reactions to LAs?

A

Rare

<1% of adverse reactions are due to allergy

Stoelting’s 5th ed, Ch. 10, pg. 292

61
Q

In solutions without preservatives, which are more allergenic, Esters or Amides?

A

Esters

Stoelting’s 5th ed, Ch. 10, pg. 292

62
Q

You give mepivicaine due to a patient having a paraben allergy, but after injection, they start to have signs of a systemic allergic reaction. How could this have occurred?

A

The amide solution may have a methyparaben or chemically similar substance to PABA.

Stoelting’s 5th ed, Ch. 10, pg. 292

63
Q

Which direction of allergic cross-sensitivity occurs between LAs?

A

Cross-sensitivity between Esters, but not Amides

Stoelting’s 5th ed, Ch. 10, pg. 292

64
Q

What is LAST?

A

Local anesthetic systemic toxicity

Stoelting’s 5th ed, Ch. 10, pg. 293

65
Q

How does LAST occur, broadly?

A

Excess plasma concentration of a drug?

Stoelting’s 5th ed, Ch. 10, pg. 293

66
Q

Most common reason for LAST occurance?

A

Direct IV injection of LA during PNB or Epidural anesthesia

Stoelting’s 5th ed, Ch. 10, pg. 293

67
Q

Will Dr. C ever release our Exam 2 grades?

A

IDK MAN WTF

written 3/7/24

68
Q

What occurs at a plasma concentration of 1-5 mcg/mL of Lidocaine?

A

Analgesia

Stoelting’s 5th ed, Ch. 10, pg. 293, Table. 10.2

69
Q

What occurs at a plasma concentration of 5-10 mcg/mL of Lidocaine?

A
  • Circumoral numbness
  • Tinnitus
  • Skeletal muscle twitching
  • HoTN
  • Myocardial depression

Stoelting’s 5th ed, Ch. 10, pg. 293, Table. 10.2

70
Q

What occurs at a plasma concentration of 10-15 mcg/mL of Lidocaine?

A
  • Seizures
  • Unconsciousness

Stoelting’s 5th ed, Ch. 10, pg. 293, Table. 10.2

71
Q

What occurs at a plasma concentration of 15-25 mcg/mL of Lidocaine?

A
  • Apnea
  • Coma

Stoelting’s 5th ed, Ch. 10, pg. 293, Table. 10.2

72
Q

What occurs at a plasma concentration of >25 mcg/mL of Lidocaine?

A

CV depression

…. prolly ded

Stoelting’s 5th ed, Ch. 10, pg. 293, Table. 10.2

73
Q

Treatment for LAST seizures?

A
  • Benzos
  • Ventilation (reduce hypoxia/metabolic acidosis)
  • NMB reduce hypoxia/acidosis

Stoelting’s 5th ed, Ch. 10, pg. 296

74
Q

Definitive treatment for LAST? Dosing?

A

Intralipids (lipid emulsion)
* 1.5mL/kg bolus
* 0.25mL/kg/min infusion for 10 min

Stoelting’s 5th ed, Ch. 10, pg. 296

75
Q

During cardiac collapse due to LAST, which drugs should be avoided?

A
  • Vasopressin
  • CCB
  • BBs
  • Use Epi at a lower dose (10-100mcg)

Stoelting’s 5th ed, Ch. 10, pg. 296

76
Q

What is methemoglobinemia?

A

Oxidation of the (Ferrous ion) Fe2+ to (Ferric ion) 3+ in Hgb, losing it’s transport ability of O2 & CO2

Stoelting’s 5th ed, Ch. 10, pg. 298

77
Q

What LAs are associated with methemoglobinemia?

A

Typically topical LAs
* Prilocaine
* Benzocaine
* Lidocaine

Stoelting’s 5th ed, Ch. 10, pg. 296

78
Q

How do you reverse Methemoglobinemia? Dose?

A

Methylene Blue
* 1-2 mg/kg IV over 5 min
* 7-8mg/kg MAX

Stoelting’s 5th ed, Ch. 10, pg. 298

79
Q

What are the 6 classifications of Regional Anesthesia?

A
  1. Topical/Surface
  2. Local infiltration
  3. PNB
  4. IV regional (Bier)
  5. Epidural
  6. Spinal (SAB)

Stoelting’s 5th ed, Ch. 10, pg. 298

80
Q

Where should epi-containing LA NOT be injected into?

A

Tissues supplied by end arteries
* Finguhs
* Toes
* Ears
* Shnozz (nose)

Stoelting’s 5th ed, Ch. 10, pg. 301

81
Q

Duration of a PNB is dependent on what 4 things?

A
  • Dose of LA
  • Lipid solubility
  • Protein-binding
  • Use of a vasoconstrictor

Stoelting’s 5th ed, Ch. 10, pg. 301

82
Q

What is more safe to increase Duration of action, including epi or more LA?

A

Inclusion of epi

Stoelting’s 5th ed, Ch. 10, pg. 301

83
Q

You should already know this, but what LA is most frequently given with IV Bier Block

Dude has it bolded so I gotta

A

50mL of Lidocaine 0.5%

but also Prilocaine

Stoelting’s 5th ed, Ch. 10, pg. 302

84
Q

How does LA work during an epidural?

A

LA diffuses across dural cuff to act on nerve roots

Stoelting’s 5th ed, Ch. 10, pg. 303

85
Q

How long does the diffusion take with an epidural injection of LA?

A

15 - 30 min delay

Stoelting’s 5th ed, Ch. 10, pg. 303

86
Q

Principal site of action of LA during a spinal injection?

A

Preganglionic fibers as they leave spinal cord in the anterior rami

Stoelting’s 5th ed, Ch. 10, pg. 304

87
Q

Most important for spinal anesthesia? Concentration, Volume, or Total Dose

A

Total dose

Stoelting’s 5th ed, Ch. 10, pg. 304

88
Q

Which LAs are most commonly selected for Spinal anesthesia?

A
  • Bupivacaine
  • Ropivacaine
  • Mepivacaine
  • Chloroprocaine

According to his slide, Stoeltings says Tetra, Lido, Bup, Levobup, & Rop

Stoelting’s 5th ed, Ch. 10, pg. 304

89
Q

Giving NaHCO3 during an epidural will do what?

A
  • Shorten onset (by 3-5 minutes)
  • Enhance depth of sensory/motor block
  • Increase spread of epidural block

Nagelhut 7th ed., Ch. 10, pg. 125

90
Q

What is the purpose of the addition of 1:200,00- Epi to LA solution?

A
  • Decrease systemic absorption of LA -> decrease risk for LAST
  • Maintains drug concentration @ site of injection -> prolonged duration

Nagelhut 7th ed., Ch. 10, pg. 124

91
Q

Describe the Tumescent technique for Liposuction

A

Subcutaneous injection of 5 or more liters of 0.05-0.10% Lido & 1:100,000 epi

Stoelting’s 5th ed, Ch. 10, pg. 307

92
Q

Tumescent technique is associated with what plasma levels over what period of time?

A
  • 1.5mcg/mL peak at 12-14 hours
  • Gradually decline over the next 6-14 hours

Stoelting’s 5th ed, Ch. 10, pg. 307

93
Q

Compared to the recommended max dosage of Lidocaine with epi (7mg/kg) what doses occur with Tumescent technique?

A

Mega-dose Lidocaine
35-55 mg/kg

Stoelting’s 5th ed, Ch. 10, pg. 307

94
Q

Why is Dibucaine used to measure pseduocholinesterase activity?

A

It inhibits normal pseudocholinesterase 70%
but inhibits atypical only 20%

Stoelting’s 5th ed, Ch. 10, pg. 290

95
Q

What is the dibucaine test used for

A

Measurement of pseudocholinesterase suppression -> dibucaine numbuh

Stoelting’s 5th ed, Ch. 10, pg. 290

96
Q

Which LAs cause vasoconstriction?

A
  • Cocaine
  • Ropivacaine

Nagelbutt says Lido but Dr. C says no.

Nagelbutt 7th. Ch. 10, pg. 124

97
Q

Which LAs are affected the most by epinephrine co-administration?

A
  • Procaine
  • Mepivacaine
  • Lidocaine
98
Q

Which LAs are affected the least by epinephrine co-administration?

A
  • Ropivacaine
  • Prilocaine
  • Etidocaine
99
Q

Maximum dose of Cocaine?

A

200mg or 5mL of 4% Cocaine

Nagelbutt pg. 135

Nurs 575 Anesthesia Pharmacology (14 decks)

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