Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 4 IN DEXTROSE 5.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 4 IN DEXTROSE 5.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 0.4% IN DEXTROSE 5%
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Liposomal bupivacaine is a local anesthetic that blocks sodium channels in nerve cell membranes, inhibiting nerve impulse conduction and providing prolonged analgesia.
Lidocaine is a class IB antiarrhythmic agent that blocks voltage-gated sodium channels, inhibiting phase 0 depolarization and decreasing automaticity in ventricular myocardial cells. It also has local anesthetic properties by blocking nerve impulse conduction.
Local infiltration: up to 266 mg (20 mL) as a single dose; interscalene brachial plexus block: up to 133 mg (10 mL); femoral nerve block: up to 133 mg (10 mL). Maximum dose 266 mg. Administer via slow injection with frequent aspiration.
Intravenous infusion: 1-4 mg/min (0.25-1 mL/min of 0.4% solution) after a loading dose of 1-1.5 mg/kg IV bolus for ventricular arrhythmias. Maximum total dose: 3 mg/kg.
None Documented
None Documented
Terminal elimination half-life is 12-48 hours (mean ~24 hours), reflecting prolonged release from the multivesicular liposome depot.
Terminal elimination half-life is approximately 1.5-2 hours (mean 1.8 h) in healthy adults. In patients with hepatic impairment or heart failure, half-life may be prolonged to >3 hours. In neonates, half-life can be 3-6 hours.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of metabolites (primarily monoethylglycinexylidide and glycinexylidide) accounts for >90% of elimination. Less than 10% excreted unchanged in urine. Biliary/fecal excretion is negligible.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)