Local Anesthetics Flashcards by Trenton Mobley

Chloroprocaine (Nesacaine)

Chemical Classification
&
MOA

Ester
Short acting

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

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Chloroprocaine (Nesacaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

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

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Chloroprocaine (Nesacaine)

Dosing

Max Infiltration Dose:
600 mg

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

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Chloroprocaine (Nesacaine)

Onset
Duration

Onset
Rapid

Duration
30-45 min

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Chloroprocaine (Nesacaine)

Metabolism
&
Elimination

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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Chloroprocaine (Nesacaine)

Side Effects
&
Considerations

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

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

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Procaine (Novocaine)

Chemical Classification
&
MOA

Ester
Short acting

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

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Procaine (Novocaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

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

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Procaine (Novocaine)

Dosing

Max Infiltration Dose:
500 mg

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

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Procaine (Novocaine)

Onset
Duration

Onset
Slow

Duration
45-60 min

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Procaine (Novocaine)

Metabolism
&
Elimination

Plasma:
Hydrolysis by plasma cholinesterase enzymes

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

Renal Excretion

Metabolism Rate - Intermediate

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Procaine (Novocaine)

Side Effects
&
Considerations

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

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

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Tetracaine (Dicaine)

Chemical Classification
&
MOA

Ester
Long acting

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

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Tetracaine (Dicaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

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

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Tetracaine (Dicaine)

Dosing

Local Total Max Dose:
100 mg (topical)

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

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Tetracaine (Dicaine)

Onset
Duration

Onset
Slow

Duration
60-180 min

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Tetracaine (Dicaine)

Metabolism
&
Elimination

Plasma:
Hydrolysis by plasma cholinesterase enzymes

Metabolite:
Para aminobenzoic acid (PABA)
Allergy Concern

Renal Excretion

Metabolism Rate - Slowest

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Tetracaine (Dicaine)

Side Effects
&
Considerations

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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Lidocaine (Xylocaine)

Chemical Classification
&
MOA

Amide - Intermediate Acting

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

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Lidocaine (Xylocaine)

Acid/Base
pKa
Lipid Solubility
Protein Binding

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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Lidocaine (Xylocaine)

Dosing

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

Lidocaine (Xylocaine)

Onset
Duration

Onset
Rapid

Duration
60-120 min

Lidocaine (Xylocaine)

Metabolism
&
Elimination

Hepatic:
Oxidative dealkylation by microsomal enzymes

Metabolites:
Xylidide
Monoethylglycine-xylidide

Lungs:
1st Pass

Renal Excretion:
5%

Metabolism Rate - Intermediate

Lidocaine (Xylocaine)

Side Effects
&
Considerations

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

**Lidocaine (Xylocaine)** Other Indications

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

**Prilocaine** Chemical Classification & MOA

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

**Prilocaine** Acid/Base pKa Lipid Solubility Protein Binding

**Acid/Base** Weak Base **pKa** 7.9 **Lipid Solubility** 0.9 **Protein Binding** 55% | pKa closest to physiologic pH = faster OOA

**Prilocaine** Dosing

Max Infiltration Dose: 400 mg 6 mg/kg w/o EPI 8.5 mg/kg w/ EPI

**Prilocaine** Onset Duration

**Onset** Slow **Duration** 60-120 min

**Prilocaine** Metabolism & Elimination

**Hepatic:** Microsomal enzymes **Metabolite:** Ortholuidine **Lungs:** 1st Pass **Renal Excretion:** 5% | Metabolism Rate - Most Rapid

**Prilocaine** Side Effects & Considerations

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

**Prilocaine** Other Indications

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

**Mepivacaine (Carbocaine)** Chemical Classification & MOA

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

**Mepivacaine (Carbocaine)** Acid/Base pKa Lipid Solubility Protein Binding

**Acid/Base** Weak Base **pKa** 7.6 **Lipid Solubility** 1 **Protein Binding** 77% | pKa closest to physiologic pH = faster OOA

**Mepivacaine (Carbocaine)** Dosing

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

**Mepivacaine (Carbocaine)** Onset Duration

**Onset** Slow **Duration** 90-180 min

**Mepivacaine (Carbocaine)** Metabolism & Elimination

**Hepatic:** Microsomal enzymes **Renal Excretion:** 5% | Metabolism Rate - Intermediate

**Mepivacaine (Carbocaine)** Side Effects & Considerations

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

**Bupivacaine (Marcaine)** Chemical Classification & MOA

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

**Bupivacaine (Marcaine)** Acid/Base pKa Lipid Solubility Protein Binding

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

**Bupivacaine (Marcaine)** Dosing

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

**Bupivacaine (Marcaine)** Onset Duration

**Onset** Slow **Duration** 240-480 min

**Bupivacaine (Marcaine)** Metabolism & Elimination

**Hepatic:** Aromatic hydroxylation, N-dealkylation, amide hydrolysis & conjugation by microsomal enzymes **Lungs:** 1st Pass Dose-dependent **Renal Excretion:** 5% | Metabolism Rate - Slowest

**Bupivacaine (Marcaine)** Side Effects & Considerations

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

**Bupivacaine (Marcaine)** Other Indications

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

**Ropivacaine (Naropin)** Chemical Classification & MOA

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

**Ropivacaine (Naropin)** Acid/Base pKa Lipid Solubility Protein Binding

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

**Ropivacaine (Naropin)** Dosing

Max Infiltration Dose: 200 mg 3 mg/kg w/o EPI 4 mg/kg w/ EPI

**Ropivacaine (Naropin)** Onset Duration

**Onset** Slow **Duration** 240-280 min

**Ropivacaine (Naropin)** Metabolism & Elimination

**Hepatic:** CYP450 enzymes **Renal Excretion:** 5%