Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus NOVOCAIN.
Head-to-head clinical analysis: EXPAREL versus NOVOCAIN.
EXPAREL vs NOVOCAIN
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.
Procaine, an ester-type local anesthetic, reversibly binds to the intracellular portion of voltage-gated sodium channels, inhibiting sodium influx and blocking nerve impulse conduction.
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.
Local infiltration: 0.5% solution, up to 20 mL (100 mg) per dose; nerve block: 1-2% solution, 5-10 mL (50-200 mg); maximum single dose: 7 mg/kg or 350 mg (without epinephrine).
None Documented
None Documented
Terminal elimination half-life is 12-48 hours (mean ~24 hours), reflecting prolonged release from the multivesicular liposome depot.
Plasma half-life: approximately 30–60 seconds due to rapid hydrolysis by pseudocholinesterases; clinical effects short-lived.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of para-aminobenzoic acid (PABA) and diethylaminoethanol as major metabolites; <2% excreted unchanged in urine. Biliary/fecal: minimal.
Category C
Category C
Local Anesthetic
Local Anesthetic