Comparative Pharmacology
Head-to-head clinical analysis: ALPHACAINE versus EXPAREL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ALPHACAINE versus EXPAREL.
ALPHACAINE vs EXPAREL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
ALPHACAINE is a local anesthetic that binds to the intracellular portion of voltage-gated sodium channels, blocking sodium influx and preventing depolarization and conduction of nerve impulses.
Liposomal bupivacaine is a local anesthetic that blocks sodium channels in nerve cell membranes, inhibiting nerve impulse conduction and providing prolonged analgesia.
10-20 mg IM or IV every 4-6 hours as needed; maximum 80 mg/day.
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.
None Documented
None Documented
Terminal elimination half-life: 3.5-5.0 hours (prolonged in hepatic impairment; requires dose adjustment in Child-Pugh B or C).
Terminal elimination half-life is 12-48 hours (mean ~24 hours), reflecting prolonged release from the multivesicular liposome depot.
Renal: ~60-70% unchanged; Hepatic metabolism: ~20-30% via CYP3A4 and CYP2C9; Fecal: <10%.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Category C
Category C
Local Anesthetic
Local Anesthetic