The Use and Method of Action of Intravenous Lidocaine and Its Metabolite in Headache Disorders.

BACKGROUND: Lidocaine, an amide anesthetic, has been used in the treatment of a wide variety of pain disorders for over 75 years. In addition to pain control, lidocaine is an anti-arrhythmic agent and has anti-inflammatory properties. Lidocaine's unique properties, including nonlinear pharmacokinetics, have limited its modern-day use.

OBJECTIVE: The purpose of this review is to offer a better understanding of the properties of this unique treatment, which we hope will allow more practitioners to offer this to their patients.

METHODS: An analysis of the history, pharmacokinetics, and relevant uses of lidocaine in headache medicine based on a synthesis of the medical literature and clinical experience.

RESULTS: Lidocaine is an amide anesthetic that inhibits voltage gated sodium channels, and lidocaine metabolism occurs exclusively in the liver. One lidocaine metabolite has its own unique properties and may be an active form of the drug.

CONCLUSION: Open label and retrospective studies have investigated the use of lidocaine in many headache disorders, primarily via injection or infusion. Further research into the active metabolite of lidocaine may allow for its use as a novel nonopiate treatment of chronic pain.