Medicinal chemistry of Benzocaine

Introduction :   Benzocaine belongs to the group of Anesthetics particularly Local Anesthetics as Ester Derivatives. Description Being i...

Introduction: 
Benzocaine belongs to the group of Anesthetics particularly Local Anesthetics as Ester Derivatives.

Description
Being insoluble it is generally used as an ointment to get rid of the pain caused due to wounds, ulcers and mucous surfaces. Its anaesthetic action is usually displayed for the period it remains in contact with the skin or mucosal surface. Hence, it forms an important ingredient in various types of creams, ointments, powders, lozenges and aerosol sprays so as to relieve the pain of naked surfaces and severely inflamed mucous membranes

Category

• Antipruritics
• Anesthetics
• Local Anesthetics
• Anesthetics, Local

Analysis

ethyl 4-aminobenzoate
Chemical Formula: C9H11NO2
Exact Mass: 165.08
Molecular Weight: 165.19
m/z: 165.08 (100.0%), 166.08 (10.2%)
Elemental Analysis: C, 65.44; H, 6.71; N, 8.48; O, 19.37

Pharmacology of Benzocaine

Indication	For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea, urinary tract, vagina. It is also used to suppress gag reflex.
Pharmacodynamics	Benzocaine is a local anesthetic commonly used as a topical pain reliever. It is the active ingredient in many over-the-counter analgesic ointments. It is also indicated for general use as a lubricant and topical anesthetic on intratracheal catheters and pharyngeal and nasal airways to obtund the pharyngeal and tracheal reflexes; on nasogastric and endoscopic tubes; urinary catheters; laryngoscopes; proctoscopes; sigmoidoscopes and vaginal specula.
Mechanism of action	Benzocaine binds to sodium channels and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions. Depolarization of the neuronal membrane is inhibited thereby blocking the initiation and conduction of nerve impulses.

Structure and Synthesis of Benzocaine