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

Mode of Action

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

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.

Synthesis of Procaine

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