Comparative Pharmacology
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE.
Head-to-head clinical analysis: EXPAREL versus LIDOCAINE.
EXPAREL vs LIDOCAINE
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 a sodium channel blocker that inhibits the influx of sodium ions into cardiac Purkinje fibers and myocytes, thereby stabilizing the neuronal membrane and decreasing automaticity. It also exhibits local anesthetic effects by reversibly binding to voltage-gated sodium channels in nerve cell membranes, blocking 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.
For ventricular arrhythmias: IV bolus 1-1.5 mg/kg, then continuous infusion 1-4 mg/min. For local anesthesia: 0.5-2% solution, max 4.5 mg/kg (300 mg) without epinephrine, 7 mg/kg (500 mg) with epinephrine.
None Documented
None Documented
Clinical Note
moderateLidocaine + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Lidocaine is combined with Fluticasone propionate."
Clinical Note
moderateLidocaine + Tenofovir disoproxil
"The metabolism of Tenofovir disoproxil can be decreased when combined with Lidocaine."
Clinical Note
moderateLidocaine + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Lidocaine."
Clinical Note
moderateLidocaine + Erythromycin
Terminal elimination half-life is 12-48 hours (mean ~24 hours), reflecting prolonged release from the multivesicular liposome depot.
Terminal elimination half-life 1.5-2 hours (normal hepatic function). In CHF or hepatic impairment, prolonged to 6-8 hours; in neonates, 3-6 hours. Context: rapid redistribution after IV bolus (alpha half-life ~8 min) accounts for brief clinical effect, while terminal half-life determines accumulation with infusion.
Renal (approximately 96% as metabolites, <10% unchanged). Biliary/fecal excretion is negligible.
Renal excretion of metabolites: 4-hydroxyxylidine (70-80% renal, 10-20% biliary/fecal), unchanged lidocaine <10% renal. Total renal elimination ~90% (as metabolites), biliary/fecal ~10%.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)
"The metabolism of Erythromycin can be decreased when combined with Lidocaine."