Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 4 IN DEXTROSE 5 IN PLASTIC CONTAINER.
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 4 IN DEXTROSE 5 IN PLASTIC CONTAINER.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 0.4% IN DEXTROSE 5% IN PLASTIC CONTAINER
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 sodium channel blocker that inhibits depolarization of cardiac myocytes and nerve axons by binding to voltage-gated sodium channels and stabilizing the neuronal membrane, thereby preventing the propagation of action potentials.
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 (20-50 mcg/kg/min) for cardiac arrhythmias. Bolus: 1-1.5 mg/kg IV, then infusion.
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 approximately 1.5-2 hours after bolus, prolonged to 2-4 hours in heart failure or hepatic impairment; continuous infusion may show context-sensitive half-life.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of unchanged drug and metabolites; <10% unchanged in urine, >90% as metabolites (primarily monoethylglycinexylidide and glycinexylidide). Biliary/fecal elimination minimal (<1%).
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)