Comparative Pharmacology
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus CHLOROPROCAINE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus CHLOROPROCAINE HYDROCHLORIDE.
ARESTOCAINE HYDROCHLORIDE vs CHLOROPROCAINE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Arestocaine hydrochloride is a local anesthetic of the amide type. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthesia.
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.
2-5 mg/kg intramuscularly every 60-90 minutes, not to exceed 500 mg total dose in a 12-hour period.
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.
None Documented
None Documented
Terminal elimination half-life is approximately 1.5–2 hours in adults with normal hepatic and renal function; prolonged in hepatic impairment or congestive heart failure.
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.
Renal excretion of unchanged drug and metabolites; approximately 90% excreted in urine as parent compound and metabolites (60% as unchanged drug, 30% as metabolites), with less than 10% fecal elimination.
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.
Category C
Category C
Local Anesthetic
Local Anesthetic