Comparative Pharmacology
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE versus NESACAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE versus NESACAINE.
LIDOCAINE HYDROCHLORIDE vs NESACAINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lidocaine hydrochloride is a sodium channel blocker that inhibits voltage-gated sodium channels in neuronal and cardiac cell membranes, stabilizing the membrane and preventing depolarization, thereby blocking nerve impulses and exerting local anesthetic and antiarrhythmic effects.
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.
IV: 1-1.5 mg/kg bolus, then 1-4 mg/min continuous infusion. Max: 3 mg/kg (300 mg) loading dose. For ventricular arrhythmias.
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 elimination half-life is 1.5–2 hours in adults. In patients with heart failure, hepatic cirrhosis, or those on CYP-inhibitors, half-life may be prolonged to ≥3 hours; in neonates, up to 3–6 hours.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
Primarily hepatic metabolism (90% CYP3A4, also CYP1A2) to inactive metabolites (monoethylglycinexylidide, glycinexylidide); <10% excreted unchanged in urine. Renal elimination accounts for the majority of metabolite clearance.
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