Drug intelligence / Profile preview

Marcain

Development stage
Approved
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Infiltration, Epidural, Intrathecal, Perineural, Intraarticular, Caudal
01

Overview

Marcain is a long-acting local anesthetic of the amide type used for local infiltration, peripheral nerve blocks, and neuraxial blocks (epidural and spinal anesthesia). It works by reversibly binding to the intracellular portion of voltage-gated sodium channels in nerve fibers. This binding stabilizes the neuronal membrane and prevents the influx of sodium ions required for the initiation and conduction of nerve impulses, effectively producing a reversible block of sensory and motor function. Developed historically by Astra (now AstraZeneca), it is characterized by its high potency and significantly longer duration of action compared to shorter-acting anesthetics like lidocaine, making it a mainstay for postoperative pain management and surgical anesthesia.

Brand names
MarcainMarcaineMarcain HeavyMarcaine SpinalMarcaine Heavy Spinal
Other names
bupivacaine hydrochloridebupivacainebupivacaine HCl
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)NaV (Voltage-gated sodium channels)

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