Pharmacokinetics of Lidocaine and Its Metabolites Following Vaginal Administration of Lidocaine Gel to Healthy Female Subjects.
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.
Juniper Pharmaceuticals, Inc (formerly Columbia Laboratories), Boston, MA, USA.
Bridget
B
Martell
BioMedical Computer Research Institute, Philadelphia, PA, USA.
Harvey
H
Kushner
Juniper Pharmaceuticals, Inc (formerly Columbia Laboratories), Boston, MA, USA.
Elaine
E
Richardson
ABC Laboratories, Columbia, MO, USA.
Amy
A
Mize
Independent Pharmacokinetics Consultant, Philadelphia, PA, USA.
Philip
P
Mayer
D000282:Administration, Intravaginal; D000328:Adult; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D008012:Lidocaine / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
D000779:Anesthetics, Local; D008012:Lidocaine; C001306:glycinexylidide; C001173:monoethylglycinexylidide
absorption; anesthetic; lidocaine; pharmacokinetics; vaginal