APIs

OXYBUPROCAINE HYDROCHLORIDE

Oxybuprocaine also known as benoxinate is a synthetic local anesthetic, which is used in ophthalmology and otolaryngology. The synthesis as free base was first described in 1950 by Dr. Wander¹. In 1976 it was commercially available in Switzerland as Novesine². It is also sold as mixture product with Fluorescein sodium and Cetylpyridinium chloride.

USES

As 0.4% ophthalmic solution Oxybuprocaine is used topically in the eye for short ocular diagnostic and minor surgical procedures.  Sensation of pain is locally and reversibly reduced, with the possibility of temperature and pressure sensitivity also affected. Anesthetic activity of Oxybuprocaine is ten times that of cocaine and twice that of tetracaine.

In otolaryngology it is used to numb the mucous membranes of the nostrils and pharynx for diagnostic purposes and small operations.³

MECHANISM OF ACTION

Oxybuprocaine hydrochloride is a highly permeable and rapidly absorbed anesthetic. It binds to sodium channels and reversibly stabilizes the neuronal membrane that decreases its permeability to sodium ions.⁴

References

¹ Patent CH308379A, 1950.

² https://www.yumpu.com/en/document/read/3618449/wirkstoff-i-vl-an-originator-originator-erste-patente-go-thekurers

³ Jasek W, ed. (2007). Austria-Codex (in German) (2007/2008 ed.).

⁴ Int J Clin Pract. 2022, doi: 10.1155/2022/5734387