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Local Anesthetics Flashcards

1
Q

What was the first LA?

A

Cocaine 1884

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2
Q

First ester LA?

A

Procaine 1905

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3
Q

First amide LA?

A

Lidocaine 1843

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4
Q

Describe the chemical structure of LAs?

A

Lipophilic and hydrophilic portion separated by hyrdrocarbon

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5
Q

Benzene ring is made of the lipophilic or hydrophilic portion?

A

Lipophilic portion

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6
Q

The hydrophilic portion of the LA is also called ______?

A

Quaternary amine

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7
Q

What are the only two pure isomer LA?

A

Ropivacaine and Levobupivacaine

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8
Q

Are ropivacaine and levobupivacaine left or right pure isomers?

A

Pure Left isomers

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9
Q

What is the benefit of an S-entantiomer LA?

A

Less neuro and cardio toxic

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10
Q

What is the mechanism of action of LA?

A

Inhibit Na+ ions passage through ion selective Na+ channels

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11
Q

What are the effects of LA on rate of depolarization, threshold potential, resting membrane potential and action potential?

A
  1. Slows rate of depolarization
  2. Stops an action potential
  3. Does not alter resting membrane potential or threshold potential
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12
Q

Does the LA bind to the internal or external part of the Na+ channel?

A

Internal

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13
Q

Why do nerves with more activity have a faster blockade?

A

Access to receptor is only possible during activated open state.
More frequent firing= more opportunity for access

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14
Q

What is Cm?

A

Minimum concentration to produce conduction blockade

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15
Q

Name one factor than increases Cm?

A

Larger diameter nerve

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16
Q

Name two factors that decrease Cm?

A
  1. Higher frequency

2. Higher pH

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17
Q

How many Nodes of Ranvier must be blocked?

A

2, preferably 3

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18
Q

T/F: Cm for sensory is about twice motor?

A

False; Cm for motor is about twice sensory

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19
Q

Order of nerve blockade for spinal or epidural anesthesia?

A
  1. B fibers
  2. C and A Delta
  3. A Gamma
  4. A Beta
  5. A Alpha
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20
Q

Which fibers are preganglionic sympathetic efferent?

A

B Fibers (Efferent=exiting the brain)

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21
Q

What are examples of C and A Delta Fibers?

A

C: Pain, temp, touch afferent (Afferent=arriving to the brain)
A Delta: Post ganglionic sympathetic neurons

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22
Q

Mneumonic for Order of blockade:

A

ATP-TP-MVP

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23
Q

ATP-TP-MVP

A
  1. Autonomc
  2. Temperature
  3. Pain
  4. Touch
  5. Pressure
  6. Motor
  7. Vibration
  8. Proprioception
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24
Q

According to Nagelhout, what is the order of nerve blockade?

A
  1. Autonomic
  2. Superficial pain, touch, temp
  3. Motor function
  4. Proprioception
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25
All LA are weak bases except which one?
Benzocaine Weak acid pKa= 3.5
26
What form must LA be in to cross lipid bilayer?
un-ionized
27
T/F: As you decrease pH, you become more and more unionized?
False; As you decrease pH, you become more and more ionized
28
What does adding HCO3 do to LA?
Higher pH is closer to pKa=more un-ionized=faster onset by 3-5mins=lessens sting of local infiltration
29
What LA quality is related to potency?
Lipid solubility
30
What LA quality is related to onset?
State of ionization
31
What LA quality is related to duration of action?
Protein binding
32
How are amides metabolized and cleared?
Hepatic metabolism. | Minimal renal excretion of unchanged drug
33
What is the fastest acting amide LA?
Prilocaine
34
Name two intermediate acting amide LAs?
1. Lidocaine | 2. Mepivicaine
35
Name three slow acting amide LAs?
1. Etidocaine 2. Bupivacaine 3. Ropivacaine
36
Name a rapid, intermediate and slow acting ester LAs?
Rapid=Chlroprocaine Intermediate=Procaine Slow=Tetracaine
37
Where are esters metabolized?
Rapid hydrolysis by cholinesterases in the plasma
38
Which ester LA is the one exception to hydrolysis?
Cocaine
39
Which type of LA has PABA as a metabolite?
Esters
40
Which common local injection site contains little to no cholinesterase enzyme?
CSF- must wait until drug goes into systemic circulation for hydrolysis
41
What 5 situations inhibit plasma cholinesterase?
1. Primary deficiency 2. Liver disease 3. Increased BUN 4. Parturients 5. Chemotherapy patients
42
Which vasoconstrictor has been found to be superior as an additive to LA?
Epinephrine
43
Which 2 LAs have no vasodilator activity?
Cocaine (significant vasoconstriction) and Ropivacine (parenteral vasoconstrictive)
44
Dose for clonidine additive to neuraxial anesthesia?
Epidural 150mcg or 2mcg/kg | Spinal 45mcg
45
When mixing different LAs, is there an additive or synergistic effect?
Additive
46
What are S&S of a real LA allergic reaction?
1. Rash 2. Urticaria 3. Laryngeal edema 4. HoTN 5. Bronchospasm
47
Max dose of plain bupivacaine vs with epi?
Plain: 175mg or 2.5mg/kg Epi: 225mg or 3mg/kg
48
Max dose plain lidocaine vs with epi?
Plain: 300mg or 4.5mg/kg Epi: 500mg or 7mg/kg
49
Max dose plain ropivacaine vs with epi?
Both: 200mg or 2.5mg/kg
50
What is the progression of CNS effects from LA toxicity called?
Hadzic's Progression
51
List Hadzic's Progression:
1. Vertigo 2. Tinnitus 3. Ominous feelings 4. Circumoral numbness 5. Garrulousness 6. Tremors 7. Myoclonic jerks 8. Convulsions 9. Coma 10. CV Collapse
52
Above what plasma concentration dose lidocaine begin Hadzic's progression?
>5mcg/ml
53
What is responsible for the speed of systemic levels of LA?
Blood flow of tissues
54
Mneumonic for fastest to slowest bloow flow of tissues in relation to LA distribution
In Time I Can Please Everyone But Suzi and Sally
55
In Time I Can Please Everyone But Suzi and Sally
``` IV Tracheal Intercostal Caudal Paracervical Epidural Brachial Plexus Subarachnoid Subcutaneous ```
56
What is typically S&S of TNS?
Moderate to severe pain in lower back, buttocks, and posterior thighs
57
What is administration type/area carries highest risk of TNS?
Intrathecal lidocaine
58
What two things are a contraindication for neuraxial anesthesia as they are indicative of risk for Cauda Equina Syndrome
Sacral dimple or hairy nevus
59
What is more likely to happen at moderate LA toxicity levels, CNS or CV symptoms?
CNS. CV toxicity requires 3 times blood concentration than seizure threshold
60
Which particular LA might you see CV symptoms prior to CNS?
Bupivacaine
61
What is dose for Lipid Emulsion therapy?
1.5ml/kg Lean body weight over 1 min followed by 0.25ml/kg/min gtt
62
What is treatment for methemoglobinemia?
Methylene blue 1-2mg/kg over 5 mins
63
Which LAs are high risk for methemoglobinemia?
1. Prilocaine 2. Benzocaine 3. Cetacaine 4. Lidocaine

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