Intranasal tetracaine and oxymetazoline: a newly approved drug formulation that provides maxillary dental anesthesia without needles. (1st November 2016)

• Record Type: Journal Article
• Authors: Hersh, Elliot V.; Saraghi, Mana; Moore, Paul A.
• Is Part Of: Current medical research and opinion. Volume 32:Number 11(2016:Nov.)
• Page Start: 1919
• Page End: 1925
• Publication Date: 2016-11-01
• Subjects: Intranasal drug delivery -- local anesthesia -- oxymetazoline -- tetracaine; Clinical medicine -- Periodicals; Therapeutics -- Periodicals; 615.5
• DOI: 10.1080/03007995.2016.1238352
• Languages: English
• ISSNs: 0300-7995

Abstract

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.