Lack of Methemoglobin Elevations After Topical Applications of Benzocaine Alone or Benzocaine Plus Tetracaine to the Oral Mucosa

Clin Ther. 2017 Oct;39(10):2103-2108. doi: 10.1016/j.clinthera.2017.08.017. Epub 2017 Sep 22.

Abstract

Purpose: This study evaluated changes in methemoglobin and oxygen saturation concentrations after the administration of recommended doses of 14% benzocaine alone or 14% benzocaine combined with 2% tetracaine.

Methods: American Society of Anesthesiology class 1 and 2 subjects (n = 40) were enrolled in this modified crossover study. Subjects were administered 0.2 mL of 14% benzocaine alone, 0.2 mL of 14% benzocaine plus 2% tetracaine, or 0.4 mL of 14% benzocaine plus 0.2% benzocaine to their cheek mucosa. Venous blood (5 mL) was drawn from the antecubital fossa before and 60 minutes after drug application for methemoglobin analyses. Oxygen saturation was also recorded via pulse oximetry at baseline and every 10 minutes through 60 minutes after drug application.

Findings: Methemoglobin and oxygen saturation levels did not change from baseline after the administration of benzocaine alone or when combined with tetracaine.

Implications: Recommended doses of benzocaine or benzocaine combined with tetracaine when applied to the cheek mucosa do not induce even clinically insignificant elevations in methemoglobin levels. Metered dosing, such as that used in this study, can help avoid this overdose phenomena with these drugs. ClinicalTrials.gov identifier: NCT02908620.

Keywords: benzocaine; methemoglobinemia; tetracaine; topical anesthetics.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Topical
  • Adult
  • Anesthetics, Local / administration & dosage
  • Anesthetics, Local / pharmacology*
  • Benzocaine / administration & dosage
  • Benzocaine / pharmacology*
  • Cross-Over Studies
  • Double-Blind Method
  • Female
  • Humans
  • Male
  • Methemoglobin / analysis*
  • Mouth Mucosa
  • Single-Blind Method
  • Tetracaine / administration & dosage
  • Tetracaine / pharmacology*

Substances

  • Anesthetics, Local
  • Tetracaine
  • Methemoglobin
  • Benzocaine

Associated data

  • ClinicalTrials.gov/NCT02908620