Pharmacology of Lidocaine


This article provides in-depth pharmacology of Lidocaine, a crucial local anesthetic and class Ib antiarrhythmic agent. It delves into detailed pharmacology, elucidating the mechanism of action, factors affecting anesthetic efficacy, and extensive clinical applications. Highlighted are various anesthetic techniques empowered by Lidocaine and recent advancements that expand its therapeutic scope. Through reputable references, this guide aims to furnish a comprehensive understanding of Lidocaine’s pharmacological profile, accentuating its indispensable role in anesthetic practice.



Lidocaine is classified as a local anesthetic of the amino amide type and is also categorized as a class Ib antiarrhythmic agent according to the Vaughan-Williams classification​1​.

Mechanism of Action

Lidocaine primarily exerts its anesthetic effect by inhibiting the sodium ion channels in the neuronal cell membrane. By blocking these channels, lidocaine prevents the transient increase in permeability of excitable membranes to sodium ions which is necessary for the generation and conduction of impulses. As a result, it suppresses the conduction of nerve impulses, leading to a loss of sensation in the localized area where it is applied. Additionally, it has antiarrhythmic effects due to its ability to stabilize the cardiac membrane by blocking sodium channels in the heart​2​.

Lidocaine MOA

Factors Affecting Local Anesthetic Action

  • Tissue pH: The efficacy of lidocaine can be affected by the pH of the tissue, with lower pH (acidic conditions) reducing its effectiveness.
  • Tissue Perfusion: Better perfused tissues may exhibit quicker onset and longer duration of anesthetic action.
  • Lipid Solubility: Higher lipid solubility enhances the potency and duration of action.
  • Protein Binding: Extent of protein binding can affect the duration of action.
  • Individual Variability: Individual responsiveness to lidocaine can vary based on genetic, age, and health factors.

Clinical Uses

  • Local Anesthesia: Used for surface anesthesia, infiltration anesthesia, intravenous regional analgesia, nerve blocks, and dental anesthesia​3​.
  • Cardiac Arrhythmias: Employed intravenously for treating ventricular arrhythmias.
  • Analgesia: Provides pain relief during post-operative and other painful conditions.
  • Adjunct to General Anesthesia: Lidocaine infusions can reduce the minimum alveolar concentration of volatile anesthetics by up to 40%, providing pain relief in the peri-operative phase​4​.
  • Anti-inflammatory Effects: Recent findings have indicated potential anti-inflammatory effects, particularly against SARS-CoV-2 triggered immune pathways.

Contraindications, Adverse Effects, and Drug Interactions

Contraindications include known hypersensitivity and severe heart block without a functioning pacemaker. Adverse effects can range from local irritation to systemic toxicity, and drug interactions may occur with liver enzyme-affecting substances and cardiac medications.

Special Populations

Caution is advised in pregnant and breastfeeding women, and individuals with liver or kidney disease due to potential for altered metabolism and excretion.

Recent Developments

There have been explorations into lidocaine’s potential for managing malignant visceral pain, its anti-inflammatory properties, and intravenous administration for improving pulmonary function under specific severe conditions.

Formulations and Administration

Various formulations are available depending on the application, including topical creams, gels, patches, injectable solutions, and lozenges, with the route of administration and dosage tailored to the condition being treated and patient-specific factors.

Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always seek the advice of a healthcare provider with any questions regarding a medical condition.

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