Drug intelligence / Profile preview

bupivacaine + lidocaine + ropivacaine

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Epidural, Infiltration, Peripheral Nerve Block, Intrathecal, Intraarticular
01

Overview

This is a combination of three amide-type local anesthetics—bupivacaine, lidocaine, and ropivacaine—used for local or regional anesthesia. Each component acts by blocking voltage-gated sodium channels in neuronal membranes, thereby inhibiting the initiation and conduction of nerve impulses. Lidocaine provides rapid onset but short duration; bupivacaine has slower onset with longer duration; ropivacaine offers similar properties to bupivacaine but with less cardiotoxicity. The rationale for combining these agents is to potentially achieve both rapid onset (from lidocaine) and prolonged effect (from bupivacaine/ropivacaine), though evidence suggests that mixing them does not necessarily improve clinical outcomes and may increase neurotoxicity risks, especially when lidocaine is combined with ropivacaine[1][3][4][9]. This combination is not a standard commercial product but may be compounded for specific procedural needs.

02

Targets

SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN3A (Sodium channel protein type 3 subunit alpha)

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