Comparative Pharmacology
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE AND EPINEPHRINE versus NESACAINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LIDOCAINE HYDROCHLORIDE AND EPINEPHRINE versus NESACAINE.
LIDOCAINE HYDROCHLORIDE AND EPINEPHRINE vs NESACAINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lidocaine is a sodium channel blocker that stabilizes neuronal membranes and inhibits action potentials, providing local anesthesia. Epinephrine is an alpha- and beta-adrenergic agonist that causes vasoconstriction, prolonging lidocaine's effect and reducing systemic absorption.
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.
Local anesthesia: 1% or 2% solution with epinephrine 1:100,000 or 1:200,000; maximum dose 7 mg/kg lidocaine (500 mg) in adults; administer by infiltration or nerve block, not to exceed 1 hour between doses.
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
Lidocaine: terminal elimination half-life is approximately 1.5–2.0 hours. With continuous infusion or hepatic impairment, half-life may be prolonged (up to 4–6 hours). Epinephrine: plasma half-life is about 2–3 minutes due to rapid uptake and metabolism.
Terminal half-life: 40-60 minutes (rapidly metabolized by plasma pseudocholinesterase); clinical context: prolonged with hepatic dysfunction or atypical pseudocholinesterase
Lidocaine is primarily metabolized in the liver; approximately 90% of a dose is excreted in the urine as metabolites (including monoethylglycinexylidide and glycinexylidide), with less than 10% excreted unchanged. Epinephrine is metabolized by catechol-O-methyltransferase and monoamine oxidase, with metabolites excreted in urine.
Renal: 90-95% as unchanged drug and metabolites (predominantly 4-hydroxypropycaine); biliary/fecal: <5%
Category A/B
Category C
Local Anesthetic / Antiarrhythmic (Class Ib)
Local Anesthetic