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lidocaine

D04AB01

Forms & Strengths

Topical ointment: 2.5%, 5%
Topical patch: 1.8%, 5%
Topical solution: 2%, 4%
Topical gel: 2%
Topical spray: 10%

Adult Dosing

Topical ointment (2.5%-5%): Apply a thin layer to intact skin to relieve pain/itching; maximum 4.5 mg/kg per dose, not to exceed 300 mg per dose.
Topical patch (5%): Apply up to 3 patches to painful areas for up to 12 hours within a 24-hour period.
Topical spray (10%): Apply 1 to 5 metered doses to mucous membranes prior to minor procedures.

Pediatric Dosing

Topical formulations: Use smallest effective dose to minimize risk of systemic toxicity; do not exceed 2 to 3 mg/kg per dose in children.
Safety and efficacy of topical patches have not been established in pediatric patients under 18 years of age.

Indications

Localized relief of pain associated with post-herpetic neuralgia
Anesthesia of mucous membranes during minor diagnostic and endoscopic procedures
Temporary relief of pain and itching associated with minor skin irritations, abrasions, and insect bites

Mechanism of Action

Stabilizes neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses
Blocks voltage-gated sodium channels in neuronal axons, resulting in local local anesthetic and analgesic effects

Contraindications

Known history of hypersensitivity to local anesthetics of the amide type
Application to broken, denuded, or inflamed skin surfaces where systemic absorption is significantly increased

Adverse Reactions

Local: Erythema, edema, contact dermatitis, pruritus, and burning at the application site
Systemic (rare with topical use): Central nervous system excitation or depression, dizziness, drowsiness, paresthesia, hypotension, and bradycardia

Drug Interactions

Class I antiarrhythmic drugs (e.g., tocainide, mexiletine): Additive toxic effects can occur when used concomitantly with systemic lidocaine absorption
CYP3A4 inhibitors (e.g., erythromycin, ketoconazole): May decrease the hepatic clearance of absorbed lidocaine, increasing systemic exposure

Curated Content: Needs Vetting Before Put to Clinical Use