Comparative Pharmacology
Head-to-head clinical analysis: LIDOCAINE AND PRILOCAINE versus PROCAINE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LIDOCAINE AND PRILOCAINE versus PROCAINE HYDROCHLORIDE.
LIDOCAINE AND PRILOCAINE vs PROCAINE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lidocaine and prilocaine are amide-type local anesthetics that stabilize neuronal membranes by inhibiting sodium ion channels, thereby blocking the initiation and conduction of nerve impulses.
Blocks voltage-gated sodium channels, inhibiting nerve impulse conduction by stabilizing the neuronal membrane and preventing depolarization.
Apply 2.5 g cream (lidocaine 25 mg/prilocaine 25 mg) to intact skin under occlusive dressing; maximum single application area 400 cm², maximum application time 4 hours. For genital mucous membranes: apply 5-10 g for 5-10 minutes without occlusion. Not recommended for dental use.
Local infiltration: 0.5% solution, up to 200 mg (40 mL) per dose. Nerve block: 0.5% solution, 100-200 mg (20-40 mL) per dose. Intravenous regional anesthesia (Bier block): 0.5% solution, 50-100 mg (10-20 mL) per dose. Maximum total dose: 200 mg without epinephrine, 250 mg with epinephrine 1:200,000.
None Documented
None Documented
Lidocaine: 1.5-2 hours; prilocaine: 1.5-2 hours. In hepatic impairment, half-life may be prolonged up to 2-3 times.
Terminal elimination half-life is approximately 7.7 minutes in adults with normal hepatic function. This short half-life reflects rapid hydrolysis by plasma pseudocholinesterases. In patients with pseudocholinesterase deficiency, half-life may be prolonged to 20-30 minutes.
Renal excretion of metabolites (lidocaine: 70-80% as 4-hydroxy-2,6-xylidine and conjugates; prilocaine: 85-95% as o-toluidine metabolites and conjugates). Less than 10% of parent drugs excreted unchanged.
Primarily renal excretion of metabolites (para-aminobenzoic acid and diethylaminoethanol) and unchanged drug. Approximately 80% of a dose is excreted in urine as para-aminobenzoic acid and conjugates; <2% excreted unchanged. Biliary/fecal elimination is negligible.
Category A/B
Category C
Local Anesthetic / Antiarrhythmic (Class Ib)
Local Anesthetic