Comparative Pharmacology
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus HEAVY SOLUTION NUPERCAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus HEAVY SOLUTION NUPERCAINE.
ARESTOCAINE HYDROCHLORIDE vs HEAVY SOLUTION NUPERCAINE
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.
Heavy solution nupercaine (dibucaine) is a potent, long-acting amide local anesthetic that stabilizes neuronal membranes by blocking voltage-gated sodium channels, thereby inhibiting the propagation of action potentials and preventing nerve impulse conduction.
2-5 mg/kg intramuscularly every 60-90 minutes, not to exceed 500 mg total dose in a 12-hour period.
Spinal anesthesia: 0.5-1 mL of 0.5% heavy solution (2.5-5 mg) injected intrathecally; dose depends on level of anesthesia required.
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 is 2.5-4 hours (mean 3.5 h) in adults. In neonates, half-life is prolonged (up to 8-12 h) due to immature hepatic function.
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 hepatic metabolism to inactive metabolites; renal excretion of unchanged drug accounts for approximately 1-5%. Biliary excretion is minimal (<5%). Total fecal elimination is negligible (<1%).
Category C
Category C
Local Anesthetic
Local Anesthetic