Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE PRESERVATIVE FREE.
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE PRESERVATIVE FREE.
EXPAREL vs LIDOCAINE HYDROCHLORIDE PRESERVATIVE FREE
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 local anesthetic that stabilizes the neuronal membrane by inhibiting sodium ion channels, thereby blocking the initiation and conduction of nerve impulses. It also exhibits cardiac effects as a class IB antiarrhythmic agent by modulating sodium channels in myocardial cells.
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.
1-4 mg/kg via intravenous bolus, not to exceed 300 mg; may be followed by continuous infusion of 1-4 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.
1.5–2 hours (terminal) in healthy adults; prolonged in hepatic impairment (up to 5–7 hours), heart failure (up to 10 hours), or with continuous infusion (>24 h) due to accumulation. Context: requires monitoring in hepatic or cardiac dysfunction to avoid toxicity.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal: ~90% as metabolites (primarily monoethylglycinexylidide [MEGX] and glycinexylidide [GX]), <10% unchanged. Fecal: <1%.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)