Comparative Pharmacology
Head-to-head clinical analysis: LIDODERM versus NESACAINE.
Head-to-head clinical analysis: LIDODERM versus NESACAINE.
LIDODERM vs NESACAINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lidocaine is an amide-type local anesthetic that blocks voltage-gated sodium channels (Nav1.7) in nerve cell membranes, inhibiting depolarization and conduction of nerve impulses, thereby producing both local anesthesia and systemic analgesia.
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.
Apply 1 to 3 patches (5% lidocaine) to intact skin over most painful area for up to 12 hours within a 24-hour period; maximum 3 patches at once.
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 3–5 hours after topical application; after intravenous administration, half-life is 1.5–2 hours. Clinical context: Systemic accumulation possible with prolonged use on inflamed skin.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
Renal excretion of metabolites (primarily 4-hydroxy-2,6-xylidine glucuronide) accounts for >85% of elimination; <3% excreted unchanged; biliary/fecal elimination minimal (<10%).
Renal: 90-95% as unchanged drug and metabolites (predominantly 4-hydroxypropycaine); biliary/fecal: <5%
Category C
Category C
Local Anesthetic
Local Anesthetic