Comparative Pharmacology
Head-to-head clinical analysis: CHLOROPROCAINE HYDROCHLORIDE versus NESACAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CHLOROPROCAINE HYDROCHLORIDE versus NESACAINE.
CHLOROPROCAINE HYDROCHLORIDE vs NESACAINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Blocks voltage-gated sodium channels in nerve cell membranes, inhibiting conduction of nerve impulses. Exhibits rapid onset and short duration due to hydrolysis by plasma pseudocholinesterase.
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.
10-30 mL of 1% solution infiltrated locally; epidural: 15-25 mL of 2% or 3% solution, repeated as needed, not to exceed 800 mg total dose.
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 of chloroprocaine is approximately 0.1-0.2 hours (6-12 minutes) in adults with normal pseudocholinesterase activity. This extremely short half-life accounts for its rapid clearance and short duration of action.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
Primarily renal excretion of metabolites; unchanged drug undergoes rapid hydrolysis by plasma pseudocholinesterase, producing 2-chloro-4-aminobenzoic acid and diethylaminoethanol. Less than 2% excreted unchanged in urine. Biliary/fecal elimination is negligible.
Renal: 90-95% as unchanged drug and metabolites (predominantly 4-hydroxypropycaine); biliary/fecal: <5%
Category C
Category C
Local Anesthetic
Local Anesthetic