Week 6 Review of Local Anesthetics Flashcards

1
Q

T/F: Local anesthetics can produce a reversible conduction blockade of impulses along the central and peripheral nerve pathways.

A

True

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2
Q

When and what was the 1st local anesthetic?

A
  • Cocaine

- 1884

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3
Q

When and what was the 1st synthetic local ester?

A
  • Procaine

- 1905

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4
Q

When and what was the 1st local amide?

A

-lidocaince

1943

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5
Q

What separates the lipophilic and hydrophilic portion of the chemical structure?

A

-hydrocarbon

which makes it a amide or ester

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6
Q

What part of the chemical structure makes the drug lipophilic active?

A

-Benzene Ring

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7
Q

What is the chemical chain for a ester?

A

-CO

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8
Q

What is the chemical chain for a amide?

A

-NHC

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9
Q

T/F: The quaternary amine is hydrophilic.

A

TRUE

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10
Q

What is the pH extracellular (usually)?

A

7.4

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11
Q

What is the pH intracellular (usually)?

A

7.0

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12
Q

What type of enantiomers does racemic use?

A

-s enantiomers and r enantiomers

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13
Q

T/F: A pure isomers uses both enantiomers s and r.

A

FALSE

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14
Q

What two drugs are pure isomers and what enantiomer do they use?

A
  • Ropivacaine
  • Levobupivacaine
  • Enantiomers s
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15
Q

What is the benefit of a S enantiomer?

A
  • Less nuero toxic

- Less cardio toxic

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16
Q

What is the mechanism of action for a local anesthetic?

A

-INHIBITS Na IONS PASSAGE THROUGH ION-SELECTIVE Na CHANNELS

  • Slows rate of depolarization
  • Threshold potential not reached
  • No action potential propogated
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17
Q

What does a local anesthetic NOT alter?

A
  • Resting membrane potential

- Threshold potential

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18
Q

What does the alpha Na+ channel subunit do?

A

Allows ion conduction and binds local

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19
Q

T/F: Local anesthetic bind to receptors in inactivated or open states.

A

True

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20
Q

What occurs if local is not permeable to the Na+?

A

The threshold and action potential cannot be obtained.

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21
Q

Is local anesthetic a strong or weak bond?

A

Weak

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22
Q

The local anesthetic binds both to the internal and external Na+ channel: which is the to be more important?

A

Internal channel

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23
Q

How does frequency dependent blockade work for local anesthetics?

A
  • Access only obtained when receptor is in activated open state
  • Nerves with more activity means faster blockade
  • More frequent firing means more opportunity for access
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24
Q

What is minimum concentration?

A

minimum concentration to produce conduction blockade

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25
What factors influence minimum concentration?
INCREASES -Nerve diameter DECREASES - Higher frequency - Higher pH
26
About how much more blockade is required for a motor blockade then a sensory blockade?
2 times as much
27
How many nodes of Ranvier must a local anesthetic block to obtain local anesthetic?
2 to 3
28
Which nerve fibers are preganglionic sympathetic efferent?
B fiber
29
Which nerve fibers are responsible for pain, temperature, and touch?
- C fibers | - A fibers
30
List the blockade order in which sensation will be last first?
ATP - TP - MVP A - utonomic T - Temperature P - Pain T - touch P - Pressure M - otor V - ibration P - Proprioception
31
A differential blockade will NOT B fibers, C fiber, and small medium A fibers.
FALSE
32
What nerve fiber will most likely not be blocked?
Large A Fibers
33
What will a differential blockade achieve?
- sympathectomy - Loss of sensation for pain and temp - May still have proprioception and moter.
34
What is the pH on a weak base local anesthetic?
7.6 to 8.9
35
Which form (ionized/unionized) crosses the lipid bylayer?
-unionized
36
What local will have a faster onsent?
-locals with pH nearest physiologic pH
37
Adding bicarb to a local will cause what to happen with the onset?
Faster onset by 3 to 5 minutes
38
T/F: The lower the pH of a local anesthetic the less it will sting.
FALSE
39
List the area of the body where 1st, 2nd, and 3rd distribution occur.
1st - Lungs 2nd - Heart, brain, kidney (high perfused tissue) 3rd - Muscle and fat (Low distrubution)
40
Which class of local is more widely distributed?
-AMIDES
41
Why do we worry about which vasopressor can cause fetal acidosis>
-Once the unionized local crosses the placental it become ionized do to the baby's lower pH and can not transport.
42
What does lipid solubility mean?
The more lipid soluble means easier to cross lipid bylayer (POTENCY)
43
Amides are metabolized where mainly.
- mainly in the hepatic system | - Minimal renal exretion
44
Name to local amides from fastest to slow onset?
- prilocaine (FASTEST) - Lidocaine and mepivicaine (Intermediate) Etidocaine, Bupicaine, Popivacan (SLOW)
45
Where are ester metabolized and how?
- Plasma | - Cholinesterases found in the plasma through rapid hydrolysis
46
What one esters is not metabolized by cholinesterases?
Cocaine
47
What metabolite do ester make that are the main concern?
-Paraaminobenzoi acid (PABA)
48
What common local infection site contains little to no cholinesterase enzyme?
CSF
49
What factors will inhibit plasma cholinesterase?
- Deficiency - Liver disease - Increase BUN - Parturients - Chemotherapy
50
Which vasoconstrictor not an ester or amine can be added to a local?
- Epinephrine - phenylephrine - norepinephrine
51
Calculate the the mcg/mL if Epinephrine were labeled 1:200000.
5 mcg/cc
52
By how much can a vasoconstrictor prolong an effect?
1/3 time longer
53
Which two local anesthetic contain no vasodilator activity?
- Cocaine | - Ropiviaine
54
How much can clonidine prolong the effects of an epidural or a spinal?
Epidural from 1.8 hour to 5.3 hours Spinal from 170 minutes to 215
55
What does epi do to lidocaines pH when mixed?
Causes the pH to go down to 4.5
56
T/F: Mixing locals together has a synergistic effect.
FALSE (Additive)
57
Which local may cause more of an allergic reaction
Esters.
58
If a local is injected intravascularly what are the symptoms?
- Hypotension - syncope - tachycardia
59
List Hadzic's Progression from least to greatest.
- vertigo - Tinnitus - Ominous feelings - Circumoral numbeness - Garrulousness - Tremors - myoclonic jerks - Convulsions - Coma - Cardiovascular collaspe
60
List the systemic levels related to blood flow of tissue from fastest to slowest for a local?
- IV - Tracheal - Intercostal - Caudal - Paracervical - Epidural - Brachial Plexus - Subarachnoid - Subcutaneous Acronym: In Time I can Please Everyone But Suzi and Sally.
61
List important information about Transient Neurologic Symptoms (TNS)?
-Moderate to severe pain Lower back, buttocks, and posterior thighs -Unknown etiology -Highest risk after intrathecal lidocaine
62
List important information about Cauda Equina Syndrome?
-Diffuse injury across lumbosacral plexus Various degrees of sensory anesthesia Bowel and bladder sphincter dysfunction Paraplegia -Related to Lidocaine
63
List important information about Anterior Spinal Artery Syndrome?
-Lower extremity paresis and variable sensory defecit.
64
What must the Bupivacaine levels be to see cardiotoxicity?
- 8 to 10 mcg/mL
65
How would you treat local anesthetic toxicity?
- Airway management - Seizure suppression - Management of arrhythmias - Lipid emulsion (20%)
66
What drugs would be avoided for local toxicity especially if you had arrythmias.
- vasopressin - calcium channel blocker - Betablockers - local anesthetic
67
Methemoglobinemia is related to local, but how would it be treated?
-methylene blue 1 to 2 mg/kg over 5 minutes
68
What is the correct dosage for a lipid emulsion (20%) therapy?
- 1.5 mL/kg (LEAN BODY MASS) | - 0.25 ml/kg
69
How long after would you continue to treat for a local cardiogenic toxicity?
10 minutes