Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 2 IN DEXTROSE 5 IN PLASTIC CONTAINER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 2 IN DEXTROSE 5 IN PLASTIC CONTAINER.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 0.2% 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 stabilizes the neuronal membrane by inhibiting the ionic fluxes required for initiation and conduction of impulses, resulting in local anesthetic and antiarrhythmic effects.
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 (0.2% solution = 2 mg/mL) for antiarrhythmic therapy; loading dose 1-1.5 mg/kg IV bolus, then infusion. Maximum infusion rate 4 mg/min.
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 adults with normal hepatic function; may be prolonged in patients with hepatic impairment (e.g., cirrhosis) or heart failure (up to 10 h), and in neonates (3–6 h).
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of unchanged drug and metabolites accounts for >95% of elimination, with ~10% as unchanged lidocaine and ~90% as metabolites (primarily 4-hydroxy-2,6-xylidine, with minor contribution from monoethylglycinexylidide and glycinexylidide). Biliary/fecal excretion is minimal (<1%).
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)