Pharmacokinetics of Lidocaine and Its Metabolites Following Vaginal Administration of Lidocaine Gel to Healthy Female Subjects

• Published in: Clinical pharmacology in drug development Vol. 6; no. 1; pp. 27 - 35
• Main Authors: Martell, Bridget, Kushner, Harvey, Richardson, Elaine, Mize, Amy, Mayer, Philip
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.01.2017; John Wiley and Sons Inc
• Subjects: absorption; Administration, Intravaginal; Adult; anesthetic; Anesthetics, Local - administration & dosage; Anesthetics, Local - pharmacokinetics; Dose-Response Relationship, Drug; Double-Blind Method; Female; Healthy Volunteers; Humans; lidocaine; Lidocaine - administration & dosage; Lidocaine - analogs & derivatives; Lidocaine - blood; Lidocaine - pharmacokinetics; Metabolites; Original Manuscript; pharmacokinetics; vaginal; Young Adult; pharmacokinetics; anesthetic; absorption; lidocaine; vaginal
• ISSN: 2160-763X; 2160-7648
• DOI: 10.1002/cpdd.286

Lidocaine vaginal bioadhesive gel is being developed as a local anesthetic for use in minimally invasive outpatient gynecological procedures and was investigated in single‐dose and multiple‐dose studies in healthy young adult women. Lidocaine doses of 2.5%, 5%, and 10% (w/w) were administered, and parent drug and metabolites monoethylglycinexylidide and glycinexylidide were measured in plasma. Lidocaine was absorbed through vaginal tissue and into the systemic circulation in a dose‐proportional manner, and there was little systemic accumulation. Plasma concentrations were 10‐ to 20‐fold lower than concentrations obtained after administration of intravenous lidocaine used to treat arrhythmic activity, thus demonstrating a wide safety margin for a vaginal lidocaine product.