Comparative Pharmacology
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE W EPINEPHRINE versus NESACAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE W EPINEPHRINE versus NESACAINE.
LIDOCAINE HYDROCHLORIDE W/ EPINEPHRINE vs NESACAINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Nesacaine (chloroprocaine) is an ester-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting the initiation and conduction of nerve impulses.
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.
Injectable local anesthetic: 1% or 2% solution, maximum dose 7 mg/kg (not to exceed 500 mg) with epinephrine, 4.5 mg/kg (not to exceed 300 mg) without epinephrine. Administer by infiltration or nerve block; may repeat at 30-minute intervals.
None Documented
None Documented
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.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
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.
Renal: 90-95% as unchanged drug and metabolites (predominantly 4-hydroxypropycaine); biliary/fecal: <5%
Category A/B
Category C
Local Anesthetic / Antiarrhythmic (Class Ib)
Local Anesthetic