Local Anesthetics (week 8) Flashcards

(99 cards)

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
Lidocaine pKa?
7.9 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
26
Prilocaine pKa?
7.9 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
27
Mepivacaine pKa?
7.6 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
28
Bupivacaine pKa?
8.1 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
29
Levobupivacaine pKa?
8.1 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
30
Ropivacaine pKa?
8.1 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 284, Table 10.1
31
Liposomal LA benefits?
* Prolong Duration of action * Decrease Toxicity ## Footnote Stoelting's 5th ed, Ch. 10, pg. 283
32
Which drugs are used in Lipsomal formulations?
* Lidocaine * Tetracaine * Bupivicaine ## Footnote Stoelting's 5th ed, Ch. 10, pg. 283
33
Mechanism of action of LAs?
LAs bind to the internal α-subunits on voltage gated Na+ channels, inhibiting passage of Na+ through ion-specific channels. ## Footnote Stoelting's 5th ed, Ch. 10, pg. 297
34
What effects do LAs have on nerve conduction?
Slows depolarization -> Threshold potential not reached -> Action potentials not generated ## Footnote Stoelting's 5th ed, Ch. 10, pg. 297
35
What state(s) must the Na+ voltage gated channel be in in order for LAs to bind?
Inactivated-closed ## Footnote Stoelting's 5th ed, Ch. 10, pg. 298
36
What state(s) can the Na+ voltage gated channel be in?
* Inactivated-closed * Resting-closed * Activated-open ## Footnote Stoelting's 5th ed, Ch. 10, pg. 298
37
Definition of Cm?
* Miniumum effective concentration * of LA to produce conduction blockade of nerve impulses ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
38
What is Cm similar to?
MAC for inhaled anesthetics ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
39
How does Cm of Motor fibers compare to sensory fibers?
Cm of Motor fibers approx. twice that of sensory fibers ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
40
True/False: Motor & Sensory blockade always accompany ea. other
Negative, Ghost Rider * sensory anesthesia may NOT always be accompanied by skeletal muscle paralysis ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
41
Using a LA with the same Cm, is more or less volume required for spinal or epidural anesthesia? Why?
More volume for Epidural * LAs are provided VIP access to them unprotected nerves in subarachnoid space ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
42
What changes in response to LAs occurs during Pregnancy? Why?
* Increased sensitivity * More rapid onset Protein-binding characteristics change -> more unbound, pharmacologically active drug ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
43
Is there concern for the fetus during pregnancy with the use of LAs?
Yes, may be significant placental transfer of LA from Mother -> fetus ## Footnote Stoelting's 5th ed, Ch. 10, pg. 301
44
When might placental transfer be of concern?
* Prolonged labor * Acidosis in the fetus causing ion trapping ## Footnote Stoelting's 5th ed, Ch. 10, pg. 301
45
Which has a more rapid onset, Lidocaine or Bupivicaine? Why?
LAs with pKa closer to physiological pH (7.4) have more rapid onset Lidocaine pKa = 7.9 Bupivicaine pKa = 8.1 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
46
Are LAs acids or bases?
Weak bases pKa 7.6 ~ 8.1 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
47
What intrinsic property of LAs influence potency and duration of action? Why?
* Vasodilatory activity * vasodilation results in faster/greater systemic absorption -> metabolized ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
48
Between Lidocaine & Mepivacaine, which has a shorter duration of action? Why?
**Lidocaine** * Mepivacaine does not have vasoactive effects (specifically vasodilatory) ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
49
Absorption of LA is influenced by what 4 things?
* Site of injection * Dosage * Use of Epi * Pharmacological characteristics of the drug ## Footnote Stoelting's 5th ed, Ch. 10, pg. 300
50
Are LA water or Lipid soluble?
Lipid soluble ## Footnote Stoelting's 5th ed, Ch. 10, pg. 288
51
What percent of LAs are renally excreted? Any exceptions?
* 5% unchanged in urine * Cocaine is 10-12% renally excreted unchanged ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
52
What part of LAs (amides or esters) can be renally excreted? Any examples?
* Water-soluble metabolites are readily excreted in urine * PABA (paraaminobenzoic acid) from metabolism of esters ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
53
Where are Amide LAs metabolized?
Microsomal enzymes in the liver ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
54
List the Amides in the order of rate metabolized
* Rapid - Prilocaine * Intermediate - Lido/Mepivacaine * Slow - Bupivacine/Ropivacaine ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
55
Is systemic toxicity more likely with Amides or Esters? Why?
**Amides** * Esters are rapidly metabolized by plasma esterases ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
56
Are cumulative effects more likely with Amides or Esters?
Amides ## Footnote Stoelting's 5th ed, Ch. 10, pg. 289
57
How are esters metabolized?
Hydrolysis by Cholinesterase in the plasma ## Footnote Stoelting's 5th ed, Ch. 10, pg. 290
58
In what order are the Esters metabolized?
1. Rapid - Chloroprocaine 2. Intermediate - Procaine 3. Slow - Tetracaine ## Footnote Stoelting's 5th ed, Ch. 10, pg. 290
59
What metabolite(s) of Ester LAs are antigenic?
Paraaminobenzoic acid (PABA) ## Footnote Stoelting's 5th ed, Ch. 10, pg. 290
60
How frequent are allergic reactions to LAs?
Rare <1% of adverse reactions are due to allergy ## Footnote Stoelting's 5th ed, Ch. 10, pg. 292
61
In solutions without preservatives, which are more allergenic, Esters or Amides?
Esters ## Footnote Stoelting's 5th ed, Ch. 10, pg. 292
62
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?
The amide solution may have a methyparaben or chemically similar substance to PABA. ## Footnote Stoelting's 5th ed, Ch. 10, pg. 292
63
Which direction of allergic cross-sensitivity occurs between LAs?
Cross-sensitivity between Esters, but not Amides ## Footnote Stoelting's 5th ed, Ch. 10, pg. 292
64
What is **LAST**?
Local anesthetic systemic toxicity ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293
65
How does LAST occur, broadly?
Excess plasma concentration of a drug? ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293
66
Most common reason for LAST occurance?
Direct IV injection of LA during PNB or Epidural anesthesia ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293
67
Will Dr. C ever release our Exam 2 grades?
IDK MAN WTF | written 3/7/24
68
What occurs at a plasma concentration of 1-5 mcg/mL of Lidocaine?
Analgesia ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293, Table. 10.2
69
What occurs at a plasma concentration of 5-10 mcg/mL of Lidocaine?
* Circumoral numbness * Tinnitus * Skeletal muscle twitching * HoTN * Myocardial depression ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293, Table. 10.2
70
What occurs at a plasma concentration of 10-15 mcg/mL of Lidocaine?
* Seizures * Unconsciousness ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293, Table. 10.2
71
What occurs at a plasma concentration of 15-25 mcg/mL of Lidocaine?
* Apnea * Coma ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293, Table. 10.2
72
What occurs at a plasma concentration of >25 mcg/mL of Lidocaine?
CV depression .... prolly ded ## Footnote Stoelting's 5th ed, Ch. 10, pg. 293, Table. 10.2
73
Treatment for LAST seizures?
* Benzos * Ventilation (reduce hypoxia/metabolic acidosis) * NMB reduce hypoxia/acidosis ## Footnote Stoelting's 5th ed, Ch. 10, pg. 296
74
Definitive treatment for LAST? Dosing?
**Intralipids** (lipid emulsion) * 1.5mL/kg bolus * 0.25mL/kg/min infusion for 10 min ## Footnote Stoelting's 5th ed, Ch. 10, pg. 296
75
During cardiac collapse due to LAST, which drugs should be avoided?
* Vasopressin * CCB * BBs * Use Epi at a lower dose (10-100mcg) ## Footnote Stoelting's 5th ed, Ch. 10, pg. 296
76
What is methemoglobinemia?
Oxidation of the (Ferrous ion) Fe2+ to (Ferric ion) 3+ in Hgb, losing it's transport ability of O2 & CO2 ## Footnote Stoelting's 5th ed, Ch. 10, pg. 298
77
What LAs are associated with methemoglobinemia?
Typically topical LAs * Prilocaine * Benzocaine * Lidocaine ## Footnote Stoelting's 5th ed, Ch. 10, pg. 296
78
How do you reverse Methemoglobinemia? Dose?
**Methylene Blue** * 1-2 mg/kg IV over 5 min * 7-8mg/kg MAX ## Footnote Stoelting's 5th ed, Ch. 10, pg. 298
79
What are the 6 classifications of Regional Anesthesia?
1. Topical/Surface 2. Local infiltration 3. PNB 4. IV regional (Bier) 5. Epidural 6. Spinal (SAB) ## Footnote Stoelting's 5th ed, Ch. 10, pg. 298
80
Where should epi-containing LA **NOT** be injected into?
Tissues supplied by end arteries * Finguhs * Toes * Ears * Shnozz (nose) ## Footnote Stoelting's 5th ed, Ch. 10, pg. 301
81
Duration of a PNB is dependent on what 4 things?
* Dose of LA * Lipid solubility * Protein-binding * Use of a vasoconstrictor ## Footnote Stoelting's 5th ed, Ch. 10, pg. 301
82
What is more safe to increase Duration of action, including epi or more LA?
Inclusion of epi ## Footnote Stoelting's 5th ed, Ch. 10, pg. 301
83
You should already know this, but what LA is most frequently given with IV Bier Block | Dude has it bolded so I gotta
50mL of Lidocaine 0.5% but also Prilocaine ## Footnote Stoelting's 5th ed, Ch. 10, pg. 302
84
How does LA work during an epidural?
LA diffuses across dural cuff to act on nerve roots ## Footnote Stoelting's 5th ed, Ch. 10, pg. 303
85
How long does the diffusion take with an epidural injection of LA?
15 - 30 min delay ## Footnote Stoelting's 5th ed, Ch. 10, pg. 303
86
Principal site of action of LA during a spinal injection?
Preganglionic fibers as they leave spinal cord in the anterior rami ## Footnote Stoelting's 5th ed, Ch. 10, pg. 304
87
Most important for spinal anesthesia? Concentration, Volume, or Total Dose
Total dose ## Footnote Stoelting's 5th ed, Ch. 10, pg. 304
88
Which LAs are most commonly selected for Spinal anesthesia?
* Bupivacaine * Ropivacaine * Mepivacaine * Chloroprocaine | According to his slide, Stoeltings says Tetra, Lido, Bup, Levobup, & Rop ## Footnote Stoelting's 5th ed, Ch. 10, pg. 304
89
Giving NaHCO3 during an epidural will do what?
* Shorten onset (by 3-5 minutes) * Enhance depth of sensory/motor block * Increase spread of epidural block ## Footnote Nagelhut 7th ed., Ch. 10, pg. 125
90
What is the purpose of the addition of 1:200,00- Epi to LA solution?
* **Decrease systemic absorption of LA** -> decrease risk for LAST * Maintains drug concentration @ site of injection -> prolonged duration ## Footnote Nagelhut 7th ed., Ch. 10, pg. 124
91
Describe the Tumescent technique for Liposuction
Subcutaneous injection of 5 or more liters of 0.05-0.10% Lido & 1:100,000 epi ## Footnote Stoelting's 5th ed, Ch. 10, pg. 307
92
Tumescent technique is associated with what plasma levels over what period of time?
* 1.5mcg/mL peak at 12-14 hours * Gradually decline over the next 6-14 hours ## Footnote Stoelting's 5th ed, Ch. 10, pg. 307
93
Compared to the recommended max dosage of Lidocaine with epi (7mg/kg) what doses occur with Tumescent technique?
Mega-dose Lidocaine 35-55 mg/kg ## Footnote Stoelting's 5th ed, Ch. 10, pg. 307
94
Why is Dibucaine used to measure pseduocholinesterase activity?
It inhibits normal pseudocholinesterase 70% but inhibits atypical only 20% ## Footnote Stoelting's 5th ed, Ch. 10, pg. 290
95
What is the dibucaine test used for
Measurement of pseudocholinesterase suppression -> dibucaine numbuh ## Footnote Stoelting's 5th ed, Ch. 10, pg. 290
96
Which LAs cause vasoconstriction?
* Cocaine * Ropivacaine | Nagelbutt says Lido but Dr. C says no. ## Footnote Nagelbutt 7th. Ch. 10, pg. 124
97
Which LAs are affected the **most** by epinephrine co-administration?
* Procaine * Mepivacaine * Lidocaine
98
Which LAs are affected the **least** by epinephrine co-administration?
* Ropivacaine * Prilocaine * Etidocaine
99
Maximum dose of Cocaine?
200mg or 5mL of 4% Cocaine ## Footnote Nagelbutt pg. 135