Lidocaine CAS 137-58-6 Lidocaine 99% Apis, Pharma Materials

Lidocaine, known chemically as 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide, is a widely used local anesthetic and antiarrhythmic agent. First synthesized in 1943, it has become a cornerstone in medical practice due to its rapid onset, effectiveness, and versatility.

Pharmacological Properties

1. Mechanism of Action:

   • Local Anesthesia: Blocks voltage-gated sodium channels in neuronal membranes, inhibiting the initiation and conduction of nerve impulses, thereby preventing pain signals.

   • Antiarrhythmic: Stabilizes cardiac cell membranes by inhibiting sodium influx, particularly in ventricular tissues, to treat abnormal heart rhythms.

2. Pharmacokinetics:

   • Absorption: Rapidly absorbed through mucous membranes and skin (topical forms) or via injection.

   • Metabolism: Primarily metabolized in the liver by cytochrome P450 enzymes.

   • Excretion: Eliminated via the kidneys (90% as metabolites, 10% unchanged).

Clinical Applications

1. Local Anesthesia:

   • Surface Anesthesia: Creams, gels, or sprays for minor procedures (e.g., dental work, endoscopy).

   • Infiltration/Regional Anesthesia: Injected to numb specific areas (e.g., suturing, biopsies).

   • Nerve Blocks: Epidural or spinal anesthesia for surgery or labor pain management.

2. Cardiology:

   • Ventricular Arrhythmias: Used intravenously to treat life-threatening arrhythmias (e.g., ventricular tachycardia).

3. Topical Uses:

   • Pain Relief: Patches or gels for post-herpetic neuralgia, burns, or insect bites.

   • Mucosal Procedures: Lubricants for urinary catheterization or intubation.