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Quiz 5 (Local Anesthetics) Flashcards

1
Q

1st Local Anesthetic
1st Synthetic Local (Ester)
1st Amide Local

A

1st Local Anesthetic Cocaine 1884
1st Synthetic Local (Ester) Procaine 1905
1st Amide Local Lidocaine 1943

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2
Q

Chemical Structure of both amide and Ester

A

-Lipophilic and hydrophilic portion separated by hydrocarbon
-Lipophilic portion is the Benzene ring
Necessary for activity

Ester
-CO-
Amide
-NHC-

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3
Q

extracellular vs intracellular pH

A

Extra - 7.4

Intra - 7.0

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4
Q

Enantiomers
s
r

A

Left = sinister

Right = rectus

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5
Q

S enantiomers - What’s the benefit? 2 examples?

A

Found to be less neuro- and cardio-toxic

Ropivacaine and Levobupivacaine

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6
Q

MOA of local anesthetics (main site of action)

A

Inhibit Na+ ions passage through ion-selective Na+ channels:

  • Slows rate of depolarization
  • Threshold potential not reached
  • No action potential propagated
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7
Q

L.A.’s Binds to receptors in ____________________ states

A

inactivated/activated

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8
Q

Nerves with more activity = ______ blockade

A

faster

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9
Q

look at slide 12

A

.

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10
Q

other sites of action for L.A.’s

A

-Voltage-dependent potassium ion channels
(Much lower affinity)

  • Calcium ion currents (L-type)
  • G protein-coupled receptors
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11
Q

Cm for motor about _____ sensory

A

twice

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12
Q

factors that increase and decrease Cm

A

Increases:
-Larger diameter

Decreases:

  • Higher frequency
  • Higher pH
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13
Q

Epidural vs Spinal Cm and dose

A
  • Unchanged Cm

- Direct access to nerves = less amount

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14
Q

Nodes of Ranvier, Must block?

A

at least 2, preferably 3

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15
Q

order of blockade of fibers

A 
B fibers
C and A-delta fibers
A-Gamma fibers
A-Beta fibers
A-Alpha fibers
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16
Q

which fibers travel faster?

A

Myelenated

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17
Q

ATP-TP-MVP acronym

A
  • Autonomic
  • Temperature
  • Pain
  • Touch
  • Pressure
  • Motor
  • Vibration
  • Proprioception
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18
Q

What form to cross lipid bylayer?

A

Un-ionized

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19
Q

Locals with pks nearest physiologic pH?

A

Faster onset

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20
Q

all are typically weak bases, which on is a weak acid and what pH?

A

Benzocaine

  • pKa – 3.5
  • Does not ionize based on pH
  • Also does not block by same mechanism
  • Mechanism is unknown
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21
Q

adding bicarb does what?

A

makes pH closer to physiologic pH, making onset quicker by 3-5 mins

also lessens sting of local infiltration

22
Q

Absorption into systemic circulation

Influenced by:

A
  • Site of injection
  • Dosage
  • Use of Epi
  • Characteristics of drug
23
Q

Distribution :

A 
1st large uptake to lungs
2nd distribution to high perfused tissue 
(heart, brain, kidneys)
3rd distribution to low perfused tissue
(muscle and fat)
Amides are more widely distributed
24
Q

Why is placental transfer important?

A

Ion trapping

25
Why do we worry about which vasopressor can cause fetal acidosis?
- Once un-ionized local crosses placenta and hits low fetal pH more drug is ionized and can’t cross back - Build up of trapped local in fetal circulation leads to toxicity in fetus
26
Lipid Solubility
More lipid soluble means easier to cross lipid by-layer
27
Onset related to :
- State of Ionization – most important | - Lipid Solubility
28
Duration of Action related to:
- Protein Binding - Lipid Solubility (Higher affinity to proteins and lipids = stronger attachment. Drug remains close to the Na+ channels to act longer)
29
Amides metabolism
Mainly hepatic metabolism
30
Amides fastest to slowest
Fastest: -Prilocaine 30 sec – 1 min Intermediate: - Lidocaine - Mepivicaine Slow: - Etidocaine - Bupivacaine - Ropivacaine
31
Esters metabolism
- Rapid hydrolysis - Cholinesterases - Mostly plasma, lesser liver
32
Esters fastest to slowest
Rapid: -Chloroprocaine Intermediate: -Procaine Slow: -Tetracaine
33
One exception to hydrolysis?
Cocaine – significant metabolism in liver
34
which L.A. group has allergy concerns? what is it?
Esters PABA
35
What common local injection site contains little to no cholinesterase enzyme?
CSF | Must wait until drug goes into systemic circulation for hydrolysis
36
Plasma Cholinesterase Inhibited in:
- Chemotherapy patients - Liver disease - Increased BUN - Parturients - Deficiency
37
Epi dosing
1:200,000 or | 5 mcg/ml
38
Epi helps LA by:
- Limits systemic absorption - Maintains drug concentration around nerves - Can prolong Lidocaine by 1/3 - No effect to onset - Helps to decrease toxicity
39
Which 2 local anesthetics have no vasodilator activity?
- Cocaine | - Ropivacaine (only parenteral with vasoconstrictive activity)
40
Clonidine as an LA additive
- Preservative free alpha-2 agonist - Enhances neuraxial anesthesia - Can be used in combo with Opioids (additive)
41
effects of mixing LAs?
additive (not synergistic)
42
how much drug in 40 mL 1%? 80 mL 0.5%?
40mL of 1% or 80mL of 0.5% | Both 400 mg
43
Tx of seizures
100% o2 | Benzos
44
memorize slide 44
.
45
Systemic levels related to blood flow of tissue | Fastest to Slowest
- IV - Tracheal - Intercostal - Caudal - Paracervical - Epidural - Brachial Plexus - Subarachnoid - Subcutaneous In Time I Can Please Everyone But Suzi and Sally
46
indications of spinals issues in caudal block
- Sacral Dimple | - Hairy Nevi
47
Cauda Equina Syndrome
Diffuse injury across lumbosacral plexus - Various degrees of sensory anesthesia - Bowel and bladder sphincter dysfunction - Paraplegia
48
Anterior Spinal Artery Syndrome
Lower extremity paresis and variable sensory deficit
49
look at slide 47
.
50
Lipid Emulsion (20%) Therapy
- 1.5 mL/kg (lean body mass) IV over 1 minute - 0.25 mL/kg/min - Repeat Bolus once or twice for persistant cardiovascular collapse - Double infusion rate to 0.5 mL/kg/min if BP remains low - Continue infusion for at least 10 min after circulatory stability - Upper limit: Approximately 10 mL/kg lipid emulsion over first 30 minutes
51
treatment for methemeglobinemia?
methylene blue
52
look at slide 51
.

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