Drug intelligence / Profile preview

lidocaine + prilocaine + tetracaine

Development stage
Unknown
Modality
Small Molecules
Administration
Topical
01

Overview

This is a **topical combination anesthetic** consisting of **lidocaine**, **prilocaine**, and **tetracaine**, used for local dermal anesthesia. All three agents are local anesthetics that act primarily by blocking sodium ion channels in neuronal membranes, thereby inhibiting nerve impulse conduction and producing a reversible loss of sensation in the application area. Lidocaine and prilocaine are amide-type local anesthetics, while tetracaine is an ester-type. The combination is used to increase the efficacy and duration of topical anesthesia, most often prior to procedures such as venipuncture, minor dermatological interventions, or management of pain related to medical devices. In clinical studies, the combined preparation has demonstrated more effective prevention of procedure-induced pain, agitation, and reflexes (such as coughing during tracheal extubation) compared to any component alone[1][4][17]. Lidocaine, prilocaine, and tetracaine act by binding to and inhibiting "Sodium channel protein type 1 subunit alpha" (Nav1.1), and possibly other voltage-gated sodium channels, resulting in reduced neuronal excitability.

Other names
lidocaine 3% + prilocaine 3% + tetracaine 4% creamlidocaine 1.5% + prilocaine 1.5% + tetracaine 4% gel
02

Targets

NaV (Voltage-gated sodium channels)NMDAR (Glutamate receptor ionotropic, NMDA)TRPV1 (Transient receptor potential cation channel subfamily V member 1)Kir (Inward-rectifier potassium channels)TRPA1 (Transient receptor potential cation channel subfamily A member 1)CaV (Voltage-gated calcium channel protein complex)

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