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Pharm II Final > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

What is the prototype ester local anesthetic?

A

Procaine

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2
Q

What local anesthetic has the shortest onset?

A

Cholorprocaine

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3
Q

What are the benefits to using Epinephrine in conjunction with a local anesthetic?

A

Can give more local anesthetic, epi slows absorptionProlongs LA due to vasoconstrictionEpi can detect if we are injecting LA in a vessel

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4
Q

What is the prototype amide local anesthetic?

A

Lidocaine

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5
Q

How do amide local anesthetics undergo metabolism?

A

Hepatic metabolism

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6
Q

What factors affect duration of action of a local anesthetic?

A

Protein binding and available blood supply to area

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7
Q

How do ester local anesthetics undergo metabolism?

A

Non-specific plasma esterases

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8
Q

What is the potency ratio of Procaine?

A

1

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9
Q

What is the potency ratio of Choloroprocaine?

A

4

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10
Q

What is the potency ratio of Tetracaine?

A

16

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11
Q

What is the potency ratio of Lidocaine?

A

1

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12
Q

What is the potency ratio of Ropivacaine?

A

4

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13
Q

What is the potency ratio of Bupivacaine?

A

4

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14
Q

What is the max dose of Procaine without Epi?

A

7mg/kg

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15
Q

What is the max dose of Tetracaine without Epi?

A

1-2mg/kg

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16
Q

What is the max dose of Choloroprocaine without Epi?

A

11mg/kg

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17
Q

What is the max dose of Lidocaine without Epi?

A

5mg/kg

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18
Q

What is the max dose of Bupivacaine without Epi?

A

2-3mg/kg

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19
Q

What is the max dose of Ropivacaine without Epi?

A

3mg/kg

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20
Q

What is the max dose of Lidocaine with Epi?

A

7mg/kg

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21
Q

What is the max dose of Tetracaine with Epi?

A

3mg/kg

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22
Q

What is the max dose of Choloroprocaine with Epi?

A

14mg/kg

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23
Q

What is the max dose of Bupivacaine with Epi?

A

3mg/kg

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24
Q

What is the max dose of Ropivacaine with Epi?

A

3mg/kg

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25
Q

What is the duration of action of Procaine?

A

45-60mins

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26
Q

What is the duration of action of Tetracaine?

A

60-180mins

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27
Q

What is the duration of action of Choloroprocaine?

A

35-40mins

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28
Q

What is the duration of action of Lidocaine?

A

60-120mins

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29
Q

What is the duration of action of Bupivacaine?

A

240-480mins

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30
Q

What is the duration of action of Ropivacaine?

A

240-480mins

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31
Q

What is the mechanism of action for local anesthetics?

A

Local anesthetics bind to voltage gated Na channels and block depolarizing Na current through these channels, they prevent or relieve pin by interrupting nerve conduction

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32
Q

How do local anesthetics prevent the generation of a nerve impulse?

A

They bind to the alpha subunit of the Na channel and prevent the influx of Na into the cell

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33
Q

What neurons are more easily blocked, those that are active or inactive?

A

Active, more sodium channels are in the ready position

34
Q

How does bicarbonate effect the onset of local anesthetics?

A

Bicarb decreases the onset of local anesthetics

35
Q

What does greater lipid solubility in a local anesthetic indicate?

A

Greater lipid solubility increases both the potency and duration of their action

36
Q

What is the therapeutic index of lipid soluble LA compared to others that aren’t as lipid soluble?

A

Greater lipid solubility also increases toxicity, decreasing the therapeutic index

37
Q

What size nerve fibers are more susceptible to local anesthetics?

A

Smaller nerve fibers are more susceptible to LA than large fibers

38
Q

What type of nerve fibers are more susceptible to Local anesthetics?

A

Myelinated fibers are more easily blocked than non-myelinated, the local anesthetics pools near the axonal membrane

39
Q

What is the first sensation to disappear with local anesthetics?

40
Q

What is the last modality lost with the use of local anesthetics?

A

Motor function

41
Q

What other modalities are lost with spinal anesthesia?

A

Sensation of cold, warmth, touch, deep pressure

42
Q

What is a good way to check if a block is setting up?

A

Check the affected area for temperature sensation, if they can’t feel temperature, in theory they shouldn’t be able to feel pain

43
Q

What factors determine the plasma concentration of local anesthetics?

A

Dose administered
Rate of absorption
Site injectedMetabolism/Elimination of drug
Amount bound to protein

44
Q

How can you tell if the LA is an Ester or an Amine just by looking at the name?

A

One I = EsterTwo I’s = Amine

45
Q

What are the signs of local anesthetic systemic toxicity?

A 
Drowsiness 
Paresthesia in mouth or tongue (metallic taste)
Ringing in ears
Muscular spasm
Seizure
Coma 
Respiratory Arrest
Cardiac Arrest
46
Q

What local anesthetic is associated with cardiovascular toxicity?

A

Bupivacaine (central cardiac depressant)

47
Q

What is often the first sign of bupivacaine toxicity?

A

Cardiac arrest

48
Q

Where is the primary site of action of local anesthetics in the heart?

A

Myocardium, where they decrease electrical excitability, conduction rate and the force of myocardial contraction

49
Q

How do local anesthetics contribute to hypotension?

A

Most LAs cause arteriolar dilation

50
Q

What protein is most associated with local anesthetics?

A

Alpha1 acid glycoprotein (AAG)

51
Q

Why are pregnant women and newborns more susceptible to local anesthetics?

A

Low circulating AAG, avoid bupivacaine

52
Q

What local anesthetic should never be injected IV?

A

Bupivacaine, cardiac specific will cause arrest

53
Q

Where is cocaine derived?

A

Leave of the coca shrub

54
Q

Why type of local anesthetic is cocaine?

A

Ester of benzoic acid

55
Q

What is the clinical action of cocaine?

A

Blockade of nerve impulse and vasoconstriction secondary to inhibition of local norepi re-uptake

56
Q

Why has Cocaine lost favor in practice?

A

Toxicity and potential for abuse

57
Q

What gives cocaine its euphoric properties?

A

Inhibition of catecholamine uptake, particularly dopamine at CNS synapses

58
Q

What is cocaine currently used in practice for?

A

Topical anesthesia, vasoconstrictor (decrease bleeding) and shrinking of the mucosa

59
Q

What local anesthetic has the most rapid onset and metabolism?

A

Choloroprocaine (about 20min motor block)

60
Q

What type of local anesthetic is Choloroprocaine?

61
Q

Why don’t we typically give more than one anesthetic agent at once?

A

The effects are compounded by one another

62
Q

What type of local anesthetic is tetracaine?

A

Ester and considered more toxic

63
Q

When is tetracaine typically utilized?

A

Spinal anesthesia when a long duration is required and topical preparations such as eye drops

64
Q

What is the most versatile local anesthetic agent?

65
Q

What local anesthetic has a similar profile as lidocaine but has lost favor with the exception of peripheral nerve blocks?

A

Mepivacaine (Carbocaine)

66
Q

What is the most common local anesthetic used for post op pain control?

A

Bupivacaine

67
Q

What type of local anesthetic is Bupivacaine?

68
Q

If a patient gets LAST from bupivacaine what is the best option for survival?

A

Cardiac Bypass

69
Q

What type of local anesthetic is Ropivacaine?

70
Q

How do lower concentrations of Ropivacaine compare to Bupivacaine?

A

Ropivacaine is slightly less potent in producing anesthesia when used in lower concentrations

71
Q

Where are opioid receptors present in the spinal cord?

A

Substantia gelatinosa

72
Q

Why don’t opioids have a significant clinical role in peripheral nerve blockade?

A

There are no peripheral receptors, or the effects are negligible

73
Q

What type of drug is Clonidine?

A

Centrally acting selective alpha 2 agonist

74
Q

What is the benefit to using Clonidine in an epidural or spinal compared to opioids?

A

Does not produce depression of ventilation, pruritus, nausea and vomiting

75
Q

What factors should be considered when selecting a local anesthetic?

A

Length of surgery
Speed of onset LA
Need of post-op pain control
Patient-related factors

76
Q

How does the pKa affect the onset of a local anesthetic?

A

The lower the pKa, the shorter the onset of action (exception chloroprocaine)

77
Q

What factors enhance the toxicity of bupivacaine?

A

Pregnancy
Use of CCB
Acidosis
Hypercarbia

78
Q

What is the most common cause of toxic plasma concentrations of local anesthetic?

A

Administration of LA directly into a vessel

79
Q

How does Lidocaine effect ventilatory response to hypoxia?

A

Depresses the response (remember local anesthetics are still anesthetics)

80
Q

What percentage of Lidocaine is typically used in a bier block?

81
Q

What form of a local anesthetics has the most effect of blocking sodium channels?

A

The charged form

82
Q

What type of local anesthetics are more likely to cross the placenta?

Pharm II Final (12 decks)

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