Comparative Pharmacology
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus POSIMIR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARESTOCAINE HYDROCHLORIDE versus POSIMIR.
ARESTOCAINE HYDROCHLORIDE vs POSIMIR
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.
Bupivacaine, the active ingredient in POSIMIR, is an amide-type local anesthetic that blocks voltage-gated sodium channels in nerve cell membranes, inhibiting the generation and conduction of nerve impulses. POSIMIR is a bupivacaine extended-release liposomal formulation designed for sustained release at the surgical site.
2-5 mg/kg intramuscularly every 60-90 minutes, not to exceed 500 mg total dose in a 12-hour period.
Posimir (bupivacaine) is administered as a single intra-articular injection into the subacromial space following arthroscopic shoulder surgery. The recommended adult dose is 5 mL (66 mg) of the 1.32% solution.
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 approximately 27 hours (range 16-38 hours), supporting once-daily dosing in clinical use.
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 via CYP3A4 and CYP1A2 to inactive metabolites; <5% excreted unchanged in urine. Biliary/fecal excretion accounts for >90% of total clearance.
Category C
Category C
Local Anesthetic
Local Anesthetic