Pharmacokinetics of Lidocaine and Its Metabolites Following Vaginal Administration of Lidocaine Gel to Healthy Female Subjects. Issue 1 (4th August 2016)

• Record Type: Journal Article
• Authors: Martell, Bridget; Kushner, Harvey; Richardson, Elaine; Mize, Amy; Mayer, Philip
• Is Part Of: Clinical pharmacology in drug development. Volume 6:Issue 1(2017)
• Page Start: 27
• Page End: 35
• Publication Date: 2016-08-04
• Subjects: lidocaine -- vaginal -- pharmacokinetics -- anesthetic -- absorption; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.286
• Languages: English
• ISSNs: 2160-7648

Abstract

Abstract: 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.