Drug intelligence / Profile preview

lidocaine

Development stage
Approved
Lead developer
Astra
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Intradermal, Topical, Transdermal, Oromucosal, Intrathecal, Ophthalmic, Rectal, Inhalation, Intranasal
01

Overview

Lidocaine is a local anesthetic of the amide type and a class Ib antiarrhythmic agent. It is widely used to provide local or regional anesthesia by nerve blockade at various sites in the body and for the treatment of ventricular arrhythmias. Lidocaine works primarily by blocking voltage-gated sodium channels (especially Sodium channel protein type 1 subunit alpha) on neuronal cell membranes, thereby inhibiting the initiation and conduction of nerve impulses. This action results in reversible loss of sensation in targeted tissues. In cardiac tissue, lidocaine raises the depolarization threshold by blocking sodium channels during their open and inactive states, reducing abnormal automaticity and suppressing arrhythmias[1][5][6][8]. Additionally, lidocaine exhibits anti-inflammatory effects through inhibition of pro-inflammatory cytokine release[6]. It was first introduced for clinical use in the late 1940s.

Brand names
XylocaineLignocaineLidoderm
Other names
lidocaine hydrochloridelignocaine hydrochloride
02

Targets

SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)SCN5A (Sodium channel protein type 5 subunit alpha)

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