4.

Articaine: Both amide & ester; choice for liver

Local Anesthesia Comprehensive Reviewer disease.
General Characteristics of Local Anesthetics 5. Prilocaine: Can cause methemoglobinemia.
1. Potent Local Anesthesia: Effective nerve
conduction blockade. Mechanism of Action
2. Reversible: Effects wear off after metabolism. 1. Primary Mode: Decreases depolarization rate
3. Non-irritating: Minimal tissue irritation. by blocking sodium channels.
4. Low Systemic Toxicity: Safe when used within 2. Membrane Expansion Theory: LA integrates
recommended doses. into lipid membrane, blocking sodium influx.
5. Low Allergic Reaction: Rare, especially with 3. Specific Receptor Theory: LA binds to sodium
amides. channel receptors, reducing sodium
6. Rapid Onset: Quick action after injection. permeability.
7. Sufficient Duration: Lasts long enough for
procedures. Pharmacokinetics
8. Adequate Tissue Penetration: Effective Absorption
diffusion into tissues. • Movement of drug from injection site into
9. Stable in Solution: Long shelf life. blood.
10. Sterile or Capable of Sterilization: Safe for • Disadvantage: High absorption reduces local
injection. effect and increases toxicity.
• Vasodilation: All LAs except cocaine cause
Types of Local Anesthetics vasodilation, increasing absorption.
Ester Anesthetics • Vasoconstrictors: Added to reduce absorption
• Examples: Procaine, Benzocaine, Cocaine, and prolong duration.
Tetracaine, Chloroprocaine.
• Metabolism: Plasma by Distribution
pseudocholinesterase. • Therapeutic: Blocks sodium channels in nerve
• Characteristics: membranes.
o High allergy rate (PABA metabolite). • Non-therapeutic: Can cause adverse effects
o Generally used topically (e.g., (e.g., CNS, cardiac toxicity).
Benzocaine). • Factors:
o Cocaine: Only natural anesthetic and o Unionized molecules pass membranes
vasoconstrictor. easily.
o Procaine: Shortest acting overall; first o Ionized molecules bind to receptor
injectable anesthetic. sites.
o Tetracaine: Most toxic; slow Metabolism
metabolism. • Ester: Plasma pseudocholinesterase.
o Benzocaine: Topical use; risk of • Amide: Liver (cytochrome P450).
methemoglobinemia. • Articaine: Metabolized rapidly in plasma; 5-
10% in liver.
Amide Anesthetics
• Examples: Lidocaine, Bupivacaine, Articaine, Excretion
Mepivacaine, Prilocaine, Ropivacaine. • Kidney is the major organ for excretion.
• Metabolism: Liver by cytochrome P450.
• Characteristics: Factors Affecting LA Action
o Commonly used injectable anesthetics. 1. pKa: Lower pKa = faster onset (closer to pH
o Rare allergic reactions. 7.4).
o Lidocaine: Most commonly used; safe 2. Protein Binding: Higher binding = longer
for children. duration.
o Bupivacaine: Longest duration; 3. Lipid Solubility: Higher solubility = higher
cardiotoxic. potency.
o Articaine: Both amide & ester; choice
for liver disease. Duration of Action
o Mepivacaine: Least vasodilation; • Ultra-Short Acting: 2% lidocaine without
medium duration. vasoconstrictor.
o Prilocaine: Can cause • Short Acting: 2% lidocaine with epinephrine;
methemoglobinemia. mepivacaine without vasoconstrictor.
• Medium Acting: Mepivacaine with
Key Local Anesthetics levonordefrin.
1. Lidocaine: Most commonly used; safe for • Long Acting: 0.5% bupivacaine with
children. epinephrine.
2. Bupivacaine: Longest duration; cardiotoxic.
3. Mepivacaine: Least vasodilation; medium
duration.
Toxicology
CNS Effects
• Initial: Anxiety, restlessness, lightheadedness.
• Severe: Seizures, respiratory depression,
coma.

Cardiovascular Effects
• Bradycardia, hypotension, cardiac arrest.

Allergic Reactions
• Ester: PABA metabolite.
• Amide: Rare; cross-sensitivity not reported.

Methemoglobinemia
• Caused by Prilocaine and Benzocaine.

Vasoconstrictors
Purpose
1. Prolongs Numbness: Reduces blood flow,
increasing duration.
2. Reduces Toxicity: Prevents systemic
absorption.
3. Promotes Hemostasis: Counteracts
vasodilation.

Common Types
1. Epinephrine: Most potent; increases HR & BP.
2. Levonordefrin: Less cardiac stimulation; used
with mepivacaine.
3. Phenylephrine: Weak, limited duration.

Dosage Calculations
Formula
• Total mg = Volume (mL) × Concentration
(mg/mL).
Examples
1. 2% Lidocaine:
o 20 mg/mL × 1.8 mL = 36 mg per
cartridge.
o Maximum dose: 7 mg/kg (healthy), 4.4
mg/kg (CVD).
2. 4% Articaine:
o 40 mg/mL × 1.7 mL = 68 mg per
cartridge.

Maximum Dose
• Lidocaine: 490 mg/day for a 70 kg patient.
• Epinephrine: 0.2 mg/day (healthy), 0.04
mg/day (CVD).

Special Mentions
1. Cocaine: First discovered; only natural
vasoconstrictor.
2. Procaine: First synthetic injectable; shortest
acting.
3. Bupivacaine: Longest duration; cardiotoxic.
4. Articaine: Choice for liver disease.
5. Mepivacaine: Least vasodilation.