Comparative Pharmacology
Head-to-head clinical analysis: CHIROCAINE versus LIDOCAINE HYDROCHLORIDE W EPINEPHRINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CHIROCAINE versus LIDOCAINE HYDROCHLORIDE W EPINEPHRINE.
CHIROCAINE vs LIDOCAINE HYDROCHLORIDE W/ EPINEPHRINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Chirocaine (levobupivacaine) is a long-acting local anesthetic of the amide type. It blocks sodium channels, inhibiting nerve impulse initiation and conduction, thereby producing local anesthesia.
Lidocaine is a sodium channel blocker that inhibits voltage-gated sodium channels, preventing depolarization and conduction of nerve impulses. Epinephrine is an alpha- and beta-adrenergic agonist that causes vasoconstriction, reducing systemic absorption of lidocaine and prolonging local anesthetic effect.
0.5% to 0.75% solution; epidural: 10-20 mL of 0.5% solution (50-100 mg) as initial dose; for surgical anesthesia, 15-20 mL of 0.75% solution (112.5-150 mg); repeat doses of 0.25% to 0.5% solution at 40-60 minute intervals as needed. Maximum single dose: 225 mg.
Local anesthesia: 1-5 mL of 1% or 2% solution with epinephrine 1:100,000 or 1:200,000; maximum dose 7 mg/kg lidocaine (500 mg without epinephrine, 7 mg/kg with epinephrine) per procedure. Intravenous: 1-1.5 mg/kg bolus for ventricular arrhythmias, followed by continuous infusion 1-4 mg/min.
None Documented
None Documented
Terminal elimination half-life is 0.5–1.5 hours (adults) and 1–2 hours (neonates). Clinically, this short half-life limits accumulation with repeated doses.
Terminal half-life 1.5-2 hours (single dose), prolonged to 2-3 hours with continuous infusion; in heart failure or hepatic cirrhosis, half-life may exceed 5 hours.
Renal excretion accounts for approximately 95% of the dose, with most being eliminated as metabolites (mainly p-aminobenzoic acid and other conjugates) and less than 5% as unchanged drug. Biliary/fecal excretion is minimal (<5%).
Renal: unchanged drug <10%, major metabolites (MEGX and GX) ~70% renal; biliary: <10% fecal; total clearance ~10-20 mL/min/kg. Renal impairment prolongs elimination of metabolites.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)