Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus XYLOCAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus XYLOCAINE.
EXPAREL vs XYLOCAINE
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 binds to and inhibits voltage-gated sodium channels in the neuronal membrane, stabilizing the membrane and preventing the initiation and conduction of nerve impulses, thereby producing local anesthesia.
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.
1-5 mg/kg (max 300 mg) local infiltration; epidural: 1-2% solution, 5-20 mL.
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 to 2 hours in adults, prolonged to 2-3 hours in patients with hepatic impairment, and may exceed 5 hours in neonates or patients with heart failure.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Hepatic metabolism (primarily by CYP1A2 and CYP3A4) to metabolites, mainly monoethylglycinexylidide (MEGX) and glycinexylidide (GX); less than 10% excreted unchanged in urine. Renal excretion of metabolites: MEGX (70-80%) and GX (10-20%). Biliary/fecal elimination is minimal.
Category C
Category C
Local Anesthetic
Local Anesthetic