Drug intelligence / Profile preview

lidocaine + epinephrine + levobupivacaine

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Infiltration, Perineural, Epidural, Intrathecal, Subcutaneous, Dental
01

Overview

This is a combination of three agents used for local or regional anesthesia: - **Lidocaine** is an amide-type local anesthetic that blocks sodium channels in neuronal membranes, inhibiting nerve impulse conduction and providing rapid-onset anesthesia. - **Epinephrine** (adrenaline) is a vasoconstrictor that prolongs the duration of local anesthetics by reducing systemic absorption and limiting bleeding at the injection site. - **Levobupivacaine** is the S-enantiomer of bupivacaine, also an amide-type local anesthetic with a longer duration of action than lidocaine. It acts by blocking sodium channels in nerve cells. The rationale for combining these drugs is to achieve both rapid onset (from lidocaine), prolonged duration (from levobupivacaine), and reduced bleeding/prolonged effect (from epinephrine). This mixture may be used in various surgical procedures requiring infiltration or nerve block anesthesia. However, evidence suggests that mixing short-acting and long-acting local anesthetics does not always provide additive benefits; pharmacokinetic interactions may reduce efficacy or alter onset/duration compared to single agents[3][5][8][10]. The safety profile must be considered due to potential toxicity from each component.

Other names
lidocaine with epinephrine and levobupivacainelidocaine/epinephrine/levobupivacaine combination
02

Targets

ADRA1A (α1A)ADRB2 (β2)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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