Comparative Pharmacology
Head-to-head clinical analysis: CHIROCAINE versus LIDOCAINE HYDROCHLORIDE AND EPINEPHRINE.
Head-to-head clinical analysis: CHIROCAINE versus LIDOCAINE HYDROCHLORIDE AND EPINEPHRINE.
CHIROCAINE vs LIDOCAINE HYDROCHLORIDE AND 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 stabilizes neuronal membranes and inhibits action potentials, providing local anesthesia. Epinephrine is an alpha- and beta-adrenergic agonist that causes vasoconstriction, prolonging lidocaine's effect and reducing systemic absorption.
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% or 2% solution with epinephrine 1:100,000 or 1:200,000; maximum dose 7 mg/kg lidocaine (500 mg) in adults; administer by infiltration or nerve block, not to exceed 1 hour between doses.
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.
Lidocaine: terminal elimination half-life is approximately 1.5–2.0 hours. With continuous infusion or hepatic impairment, half-life may be prolonged (up to 4–6 hours). Epinephrine: plasma half-life is about 2–3 minutes due to rapid uptake and metabolism.
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%).
Lidocaine is primarily metabolized in the liver; approximately 90% of a dose is excreted in the urine as metabolites (including monoethylglycinexylidide and glycinexylidide), with less than 10% excreted unchanged. Epinephrine is metabolized by catechol-O-methyltransferase and monoamine oxidase, with metabolites excreted in urine.
Category C
Category A/B
Local Anesthetic
Local Anesthetic / Antiarrhythmic (Class Ib)