Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCATON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus LIDOCATON.
EXPAREL vs LIDOCATON
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 the inward sodium current, thereby stabilizing cardiac membranes, decreasing automaticity, and increasing the fibrillation threshold. It also acts as a local anesthetic by reversibly blocking nerve impulse propagation.
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.
Lidocaine: Initial IV bolus 1-1.5 mg/kg, then IV infusion 1-4 mg/min. Adjust for arrhythmia suppression.
None Documented
None Documented
Terminal elimination half-life is 12-48 hours (mean ~24 hours), reflecting prolonged release from the multivesicular liposome depot.
Terminal half-life 1.5–2 hours (adults); prolonged in heart failure (up to 4–6 hours) or hepatic impairment (up to 8 hours).
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal: ~90% as metabolites (major metabolite 4-hydroxyxylidine) and ~10% unchanged. Biliary/fecal: <5%.
Category C
Category C
Local Anesthetic
Local Anesthetic