Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE IN PLASTIC CONTAINER.
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE IN PLASTIC CONTAINER.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 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.
Blocks voltage-gated sodium channels, inhibiting action potential propagation in neurons and cardiac myocytes.
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.
1-1.5 mg/kg IV bolus, then 0.5-0.75 mg/kg IV bolus every 5-10 min to a max of 3 mg/kg total loading dose; maintenance infusion 1-4 mg/min IV. For epidural: 5-10 mL of 1-2% solution.
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: 1.5–2 hours (single dose); prolonged to 2–3 hours with repeated dosing or in heart failure, liver disease, or elderly. Context: Effective for 1–2 hours after IV bolus, requiring infusion for sustained effect.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of unchanged drug and metabolites: ~90% as metabolites (e.g., monoethylglycinexylidide, glycinexylidide), <10% unchanged. Biliary/fecal: minimal (<1%).
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)