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Bupivacaine

MARCAINE

What it isPeripheral sodium-channel-blocking amide anesthetic; regional and epidural anesthesia.

Why this oneIts duration outlasts lidocaine several-fold, and the liposomal form extends it further.

What limits it⚑ Inadvertent intravascular injection can cause refractory ventricular arrhythmia or arrest; lipid emulsion is the rescue treatment.

FDA-approved for

FDA label

BOXED WARNING Risk of cardiac arrest (difficult resuscitation/death) with the 0.75% concentration in obstetrical epidural anesthesia; 0.75% not recommended for obstetrical anesthesia.
FDA dosingPopulationStartTargetMax
Local or regional anesthesia/analgesia (surgery, oral surgery, diagnostic/therapeutic and obstetrical procedures)AdultsIndividualized by block type and concentration (0.25%, 0.5%, 0.75%)Lowest effective doseIndividualized (see labeling); single dose usually sufficient

Renal Substantially excreted by the kidney; greater risk of adverse reactions in renal impairment

Hepatic Reduced dosing and increased monitoring for systemic toxicity in moderate to severe hepatic impairment (impaired metabolism), especially with repeat doses

Repeated doses may cause significant cumulative increases in plasma levels; allow adequate spacing

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Contraindicated for obstetrical paracervical block; no adequate human data; local anesthetics rapidly cross the placenta and can cause maternal/fetal/neonatal toxicity.

Lactation Undefined

⚠ BOXED WARNING

Cost, est. cash$20–$1,000/procedure

Generic entry1986

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk0 / 4

Legacy pregnancy categoryC

Defining liabilityLocal tissue injury and inadvertent systemic exposure can cause seizures or cardiovascular toxicity.

Mechanism of action: Bupivacaine ballicule

Bupivacaine ballicule: receptor binding, kinetics and half-life diagram

Open Bupivacaine in the interactive console ↗