Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 5 AND DEXTROSE 7 5.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 5 AND DEXTROSE 7 5.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 5% AND DEXTROSE 7.5%
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 stabilizes the neuronal membrane by inhibiting sodium ion influx, thereby blocking the initiation and conduction of nerve impulses. Dextrose provides caloric support.
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.
For IV administration, typical adult dose is 5-7 mg/kg intravenously as a single bolus, followed by 0.5-1 mg/kg every 5-10 minutes as needed, up to a maximum total dose of 200-300 mg. For epidural or caudal anesthesia, 15-20 mL of the 5% solution provides adequate block. For peripheral nerve block, 10-30 mL. Do not exceed 5 mg/kg per dose intravenously or 300 mg per dose by infiltration.
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 healthy adults after intravenous administration. In patients with heart failure or hepatic impairment, half-life may be prolonged to 4-6 hours or more. After epidural administration, half-life may be slightly longer due to ongoing absorption.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of unchanged lidocaine and metabolites; less than 10% excreted unchanged in urine. Hepatic metabolism produces active metabolites (MEGX, GX) which are renally excreted. Biliary/fecal excretion negligible.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)