Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 8 IN DEXTROSE 5 IN PLASTIC CONTAINER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE HYDROCHLORIDE 0 8 IN DEXTROSE 5 IN PLASTIC CONTAINER.
EXPAREL vs LIDOCAINE HYDROCHLORIDE 0.8% IN DEXTROSE 5% 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.
Lidocaine is an amide-type local anesthetic that acts by blocking voltage-gated sodium channels in neuronal cell membranes, thereby inhibiting the initiation and conduction of nerve impulses. This stabilizes the neuronal membrane and produces a reversible loss of sensation.
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.
Intravenous administration: 1-1.5 mg/kg bolus, followed by 1-4 mg/min continuous infusion for ventricular arrhythmias. Max dose: 3 mg/kg bolus, 4 mg/min infusion.
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 1.5–2.0 hours after a single IV dose. In patients with heart failure or hepatic impairment, it may be prolonged to >3 hours. After continuous infusion, the half-life may increase due to accumulation.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Lidocaine is primarily metabolized in the liver by CYP1A2 and CYP3A4 to active metabolites (MEGX, GX). Less than 10% is excreted unchanged in urine. Renal excretion accounts for about 20% of total clearance as metabolites and parent drug; fecal elimination is minimal (<5%).
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)