Procaine

Procaine is an ester-type local anesthetic used for infiltration and nerve block anesthesia by blocking nerve impulse conduction.

Structure of Procaine

  • Procaine is a classic amino benzoic acid derivative with an ethyl ester group, enhancing its solubility and anesthetic duration.
  • Chemical Formula: C₁₀H₂₁N₃O₂
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Structure of Procaine

Mode of Action

  • Voltage-Gated Sodium Channel Inhibition: Blocks sodium influx, preventing nerve impulse conduction.
  • Membrane Stabilization: Decreases nerve excitability by altering membrane permeability.
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Uses

  • Local Anesthesia: Used in dental procedures, minor surgeries, and cosmetic applications.
  • Topical Preparations: Applied to mucous membranes and skin for temporary numbing.
  • Infiltration Anesthesia: Injected around tissues to block nerve signals in a specific area.

Structure-Activity Relationship (SAR)

  • Ester Group: Facilitates rapid onset and short duration of action due to quick hydrolysis.
  • Diethylamino Group: Enhances lipophilicity, improving membrane penetration and anesthetic efficacy.
  • Benzene Ring Substitution: Modifications can influence potency and duration of anesthesia.
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Synthesis of Procaine

Synthesis of Procaine

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