ANESTHESIOLOGY FAST REVIEW

ANESTHESIOLOGY_FAST_REVIEWKAPAK1-0-25

LOCAL ANESTHETIC

Bilge Tuncer

Ankara Bilkent City Hospital, Department of Anesthesiology and Reanimation, Ankara, Türkiye

Tuncer B. Local Anesthetic. In: Kazancı D, editor. Anesthesiology Fast Review. 1st ed. Ankara: Türkiye Klinikleri; 2025. p.135-147.

ABSTRACT

  • Local anesthetics induce anesthesia and analgesia by obstructing the passage of nociceptive signals along nerve fibers.
  • Local anesthetics target a subunit of voltage-gated sodium channels in the cell membrane and obstruct Na+ inflow, linked to channel activation and membrane depolarization.
  • The efficacy of local anesthetics correlates with octanol and lipid solubility. The onset of action is influenced by lipid solubility and pKa.
  • Local anesthetics consist of a lipid-soluble benzene ring and an amide group, classified into two: aminoamides and aminoesters, depending on the chemical bond. Aminoesters are metabolized by pseudocholinesterases, whereas aminoamides are metabolized by hepatic carboxylesterases and cytochrome P450 enzymes.
  • Potent and lipid-soluble agents last longer.
  • Local anesthetic systemic absorption and blood levels depend on injection location, vascularity, dosage, pharmacokinetics, and vasoactive agent.
  • Local anesthetics seldom cause systemic harm. Central nervous system dosages affect conscious individuals and cause stimulatory effects. Severe cardiovascular toxicity include heart block and potentially fatal arrhythmias. Resuscitation from cardiotoxicity poses considerable challenges; nonetheless, intravenous lipid infusions show effectiveness.
  • Ester-type local anesthetics are more likely to cause allergic responses due to their metabolite, para-aminobenzoic acid, but such reactions are rare.
  • Clinical effectiveness of local anesthetics can be enhanced using adjuvants such as dexamethasone, epinephrine, opioids, and a2-agonists.

Keywords: Local anesthetics; Mechanism of action; Pharmakinetics; Toxicity; Adjuvants

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