Intranasal tetracaine and oxymetazoline: a newly approved drug formulation that provides maxillary dental anesthesia without needles

Abstract

Background: An intranasal formulation of 3% tetracaine and 0.05% oxymetazoline (Kovanaze) received FDA approval on 29 June 2016. This formulation appears to provide sufficient local anesthesia to perform routine dental restorative (filling) procedures in maxillary teeth from second premolar forward.

Objectives: The aim of this paper is to provide an overview of the efficacy, pharmacokinetics and tolerability of 3% tetracaine plus 0.05% oxymetazoline when administered intranasally.

Methods: The literature was reviewed employing the search terms intranasal delivery, tetracaine, oxymetazoline and dental local anesthesia employing the search engines PubMed Plus, Scopus and the Web of Science. The search was limited to double-blind, randomized, placebo or sham-controlled trials except for phase 1 and phase 2 pharmacokinetic and safety data.

Results: A total of five relevant publications appeared in the peer reviewed literature. Three per cent tetracaine plus 0.05% oxymetazoline produced a success rate of between 83% and 90% in providing sufficient local anesthesia to perform dental restorative procedures in maxillary premolars, canines, and incisors. The vasoconstrictive action of the oxymetazoline component was determined to be necessary for anesthetic success. The tetracaine component has a very short half-life and is undetectable in many subjects. Oxymetazoline has a half-life of approximately 2 hours. The most common side effects of this formulation are nasal runniness, stuffiness, and stinging. Cardiovascular parameters remained relatively stable although there was a pressor response in two individuals out of 186 subjects exposed to the drug; one with a history of Hashimoto’s thyrotoxicosis (a relative contraindication to the use of oxymetazoline) and one in a normal volunteer. These hypertensive events are most likely due to the oxymetazoline component, the active ingredient in over-the-counter nasal decongestants.

Conclusions: Intranasal 3% tetracaine plus 0.05% oxymetazoline provides sufficient dental anesthesia to complete restorative dentistry procedures in maxillary premolar, canine and incisor teeth. Future phase 4 clinical trials will evaluate whether this drug provides the necessary anesthetic profundity to perform more complex dental procedures.

Keywords:

• Intranasal drug delivery
• local anesthesia
• oxymetazoline
• tetracaine

Notes

Transparency

Declaration of funding

This review was not funded.

Declaration of financial/other relationships

E.V.H. has disclosed that, representing the Trustees of the University of Pennsylvania, he received grant monies for the phase 1 and phase 3 studies he helped design and carried out from St Renatus, the makers of Kovanaze. P.A.M. has disclosed that he has received consulting monies from St Renatus for helping design the phase 1–3 protocols and interpreting data related to them. M.S. has disclosed that she has no significant relationships with or financial interests in any commercial companies related to this study or article.

CMRO peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Notes

1 Kovanaze is a registered trade name of St Renatus LLC, Fort Collins, CO.

2 Accuspray is a registered trademark of Becton Dickinson, Franklin Lakes, NJ.

3 Flumist is a registered trade name of MedImmune (a subsidiary of AstraZeneca), Gaithersburg MD.