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Anesthesia Pharmacology > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

Chloroprocaine (Nesacaine)

Chemical Classification
&
MOA

A

Ester
Short acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

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2
Q

Chloroprocaine (Nesacaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak base
pKa
8.7
Lipid Solubility
Low
Protein Binding
Low

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3
Q

Chloroprocaine (Nesacaine)

Dosing

A

Max Infiltration Dose:
600 mg

6 mg/kg w/o EPI
14 mg/kg w/ EPI

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4
Q

Chloroprocaine (Nesacaine)

Onset
Duration

A

Onset
Rapid

Duration
30-45 min

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5
Q

Chloroprocaine (Nesacaine)

Metabolism
&
Elimination

A

Plasma:
Hydrolysis by plasma cholinesterase enzymes

Metabolite:
Para aminobenzoic acid (PABA)
Allergy Concern

Renal Excretion

Fastest metabolism rate by 3.5x

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6
Q

Chloroprocaine (Nesacaine)

Side Effects
&
Considerations

A

Prolonged effects d/t ↓ hydrolysis occur in hepatic disease & ↑BUN

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

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7
Q

Procaine (Novocaine)

Chemical Classification
&
MOA

A

Ester
Short acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

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8
Q

Procaine (Novocaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
8.9
Lipid Solubility
0.6
Protein Binding
6%

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9
Q

Procaine (Novocaine)

Dosing

A

Max Infiltration Dose:
500 mg

7 mg/kg w/o EPI
8.5 mg/kg w/ EPI

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10
Q

Procaine (Novocaine)

Onset
Duration

A

Onset
Slow

Duration
45-60 min

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11
Q

Procaine (Novocaine)

Metabolism
&
Elimination

A

Plasma:
Hydrolysis by plasma cholinesterase enzymes

**Metabolite: **
Para aminobenzoic acid (PABA)
Allergy Concern

Renal Excretion

Metabolism Rate - Intermediate

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12
Q

Procaine (Novocaine)

Side Effects
&
Considerations

A

Prolonged effects d/t
↓ hydrolysis occurs in hepatic disease & ↑BUN

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

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13
Q

Tetracaine (Dicaine)

Chemical Classification
&
MOA

A

Ester
Long acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

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14
Q

Tetracaine (Dicaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
8.5
Lipid Solubility
80
Protein Binding
76%

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15
Q

Tetracaine (Dicaine)

Dosing

A

Local Total Max Dose:
100 mg (topical)

3 mg/kg w/o EPI
3 mg/kg w/ EPI

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16
Q

Tetracaine (Dicaine)

Onset
Duration

A

Onset
Slow

Duration
60-180 min

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17
Q

Tetracaine (Dicaine)

Metabolism
&
Elimination

A

Plasma:
Hydrolysis by plasma cholinesterase enzymes

Metabolite:
Para aminobenzoic acid (PABA)
Allergy Concern

Renal Excretion

Metabolism Rate - Slowest

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18
Q

Tetracaine (Dicaine)

Side Effects
&
Considerations

A

No vasodilatory activity

Prolonged effects d/t
↓ hydrolysis occurs in hepatic disease & ↑BUN

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

Liposome; used to upload ↑ amount of LA into molecule & have consistent release of
LA in

Other formulation:
Tetracaine Gel 4%

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19
Q

Lidocaine (Xylocaine)

Chemical Classification
&
MOA

A

Amide - Intermediate Acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

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20
Q

Lidocaine (Xylocaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
7.9
Lipid Solubility
2.9
Protein Binding
70%

pKa closest to physiologic pH = faster OOA

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21
Q

Lidocaine (Xylocaine)

Dosing

A

Max Infiltration Dose:
300 mg;
500 mg w/ EPI

5 mg/kg w/o EPI
7 mg/kg w/ EPI

Max Spinal Dose:
100 mg

22
Q

Lidocaine (Xylocaine)

Onset
Duration

A

Onset
Rapid

Duration
60-120 min

23
Q

Lidocaine (Xylocaine)

Metabolism
&
Elimination

A

Hepatic:
Oxidative dealkylation by microsomal enzymes

Metabolites:
Xylidide
Monoethylglycine-xylidide

Lungs:
1st Pass

Renal Excretion:
5%

Metabolism Rate - Intermediate

24
Q

Lidocaine (Xylocaine)

Side Effects
&
Considerations

A

Vasodilatory activity = ↑potency & DOA

Metabolite monoethylglycine-xylidide accounts for 75% of antidysrhythmic effects

Highest risk for TNS when given intrathecally

Prolonged clearance in hepatic disease

Can cross
placental barrier

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

Prolonged clearance w/ PIH

Liposome; used to upload ↑ amount of LA into molecule & have consistent release of
LA in tissues

25
Q

Lidocaine (Xylocaine)

Other Indications

A

Eutectic Mixture of LA (EMLA)
Lidocaine 2.5% + Prilocaine 2.5% = 5% LA

Dose: 1-2 g/10 cm2 area
Readiness: 45 min OOA
Duration: 2 hrs

26
Q

Prilocaine

Chemical Classification
&
MOA

A

Amide - Intermediate

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

27
Q

Prilocaine

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
7.9
Lipid Solubility
0.9
Protein Binding
55%

pKa closest to physiologic pH = faster OOA

28
Q

Prilocaine

Dosing

A

Max Infiltration Dose:
400 mg

6 mg/kg w/o EPI
8.5 mg/kg w/ EPI

29
Q

Prilocaine

Onset
Duration

A

Onset
Slow

Duration
60-120 min

30
Q

Prilocaine

Metabolism
&
Elimination

A

Hepatic:
Microsomal enzymes

Metabolite:
Ortholuidine

Lungs:
1st Pass

Renal Excretion:
5%

Metabolism Rate - Most Rapid

31
Q

Prilocaine

Side Effects
&
Considerations

A

Less vasodilatory activity

Methemoglobinemia @ dose >600 mg d/t ortholuidine metabolite oxidizing Hgb

Can cross placental barrier

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

Tx for methemoglobin;
Methylene Blue:
IV: 1-2 mg/kg
over 5 min
Max: 7-8 mg/kg
OOA: 30-60 min

32
Q

Prilocaine

Other Indications

A

Eutectic Mixture of LA (EMLA)
Lidocaine 2.5% + Prilocaine 2.5% = 5% LA

Dose: 1-2 g/10 cm2 area
Readiness: 45 min OOA
Duration: 2 hrs

33
Q

Mepivacaine (Carbocaine)

Chemical Classification
&
MOA

A

Amide - Intermediate Acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

34
Q

Mepivacaine (Carbocaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
7.6
Lipid Solubility
1
Protein Binding
77%

pKa closest to physiologic pH = faster OOA

35
Q

Mepivacaine (Carbocaine)

Dosing

A

Max Infiltration Dose:
300 mg;
500 mg w/ EPI

5 mg/kg w/o EPI
7 mg/kg w/ EPI

Max Spinal Dose:
100 mg

36
Q

Mepivacaine (Carbocaine)

Onset
Duration

A

Onset
Slow

Duration
90-180 min

37
Q

Mepivacaine (Carbocaine)

Metabolism
&
Elimination

A

Hepatic:
Microsomal enzymes

Renal Excretion:
5%

Metabolism Rate - Intermediate

38
Q

Mepivacaine (Carbocaine)

Side Effects
&
Considerations

A

Dysrhythmias; SB & SA

Subsequent dose (2nd)
↑ risk of dysrhythmias

↑ HR & SBP; ANS response

Lacks vasodilatory activity

Highest risk for TNS when given intrathecally

Can cross placental barrier
Prolonged eliminationin fetus

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

39
Q

Bupivacaine (Marcaine)

Chemical Classification
&
MOA

A

Amide - Long Acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

40
Q

Bupivacaine (Marcaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
8.1
Lipid Solubility
28
Protein Binding
95% to α-1-acid glycoprotein

41
Q

Bupivacaine (Marcaine)

Dosing

A

Max Infiltration Dose:
175 mg
225 mg w/ EPI

2.5 mg/kg w/o EPI
2.5 mg/kg w/ EPI

Max Spinal Dose:
20 mg

42
Q

Bupivacaine (Marcaine)

Onset
Duration

A

Onset
Slow

Duration
240-480 min

43
Q

Bupivacaine (Marcaine)

Metabolism
&
Elimination

A

Hepatic:
Aromatic hydroxylation, N-dealkylation, amide hydrolysis & conjugation by microsomal enzymes

Lungs:
1st Pass
Dose-dependent

Renal Excretion:
5%

Metabolism Rate - Slowest

44
Q

Bupivacaine (Marcaine)

Side Effects
&
Considerations

A

Vasodilatory activity

↑ affinity for cardiac toxicity in neuraxial anesthesia

Least risk for TNS when given intrathecally

Continuous or intermittent epidural infusions can cause hepatic toxicity

Can cross placental barrier

↑ sensitivity d/t
↓ PChE levels;
↓protein levels

Liposome; used to upload ↑ amount of LA into molecule & have consistent release of
LA in tissues

FDA released Bupivacaine ER (Exparel); up to 90 hrs

45
Q

Bupivacaine (Marcaine)

Other Indications

A

Combination of Chloroprocaine & Bupivacaine has rapid onset w/
8.4% NaHCO3 (1 ml ONLY) in 30 ml of LA

46
Q

Ropivacaine (Naropin)

Chemical Classification
&
MOA

A

Amide - Long Acting

Intracellular Voltage-Gated Na+ Channel Blocker; Blocks initiation & conduction of
nerve impulses

47
Q

Ropivacaine (Naropin)

Acid/Base
pKa
Lipid Solubility
Protein Binding

A

Acid/Base
Weak Base
pKa
8.1
Lipid Solubility
~2.9-28
Protein Binding
94% to α-1-acid glycoprotein

48
Q

Ropivacaine (Naropin)

Dosing

A

Max Infiltration Dose:
200 mg

3 mg/kg w/o EPI
4 mg/kg w/ EPI

49
Q

Ropivacaine (Naropin)

Onset
Duration

A

Onset
Slow

Duration
240-280 min

50
Q

Ropivacaine (Naropin)

Metabolism
&
Elimination

A

Hepatic:
CYP450 enzymes

Renal Excretion:
5%

Anesthesia Pharmacology (16 decks)

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