Clinical Pharmacology

Lidocaine produces faster, more intense, longer lasting, and more extensive anesthesia than does an equal concentration of procaine. Lidocaine is an alternative choice for individuals sensitive to ester-type local anesthetics.

Lidocaine is absorbed rapidly after parenteral administration and from the GI and respiratory tracts. In addition to preparations for injection, an iontophoretic, needle-free drug-delivery system for a solution of lidocaine and epinephrine (iontocaine) is available for dermal procedures and provides anesthesia to a depth of up to 10 mm.

A lidocaine transdermal patch (lidoderm) is used for relief of pain associated with postherpetic neuralgia. The combination of lidocaine (2.59%) and prilocaine (2.5%) in an occlusive dressing (emla anesthetic disc) is used as an anesthetic prior to venipuncture, skin graft harvesting, and infiltration of anesthetics into genitalia.

Lidocaine is dealkylated by hepatic CYPs to metabolites with local anesthetic activity.

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