Comparative Pharmacology
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus NESACAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus NESACAINE.
ARESTOCAINE HYDROCHLORIDE vs NESACAINE
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.
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.
2-5 mg/kg intramuscularly every 60-90 minutes, not to exceed 500 mg total dose in a 12-hour period.
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 approximately 1.5–2 hours in adults with normal hepatic and renal function; prolonged in hepatic impairment or congestive heart failure.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
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.
Renal: 90-95% as unchanged drug and metabolites (predominantly 4-hydroxypropycaine); biliary/fecal: <5%
Category C
Category C
Local Anesthetic
Local Anesthetic