Oxybuprocaine Hydrochloride

(BANM, rINNM)
Oxybuprocaine Hydrochloride Chemical formula
Synonyms: (BANM, rINNM) Benoxinate Hydrochloride; Hidrocloruro de oxibuprocaína; Oksibuprokaiinihydrokloridi; Oksibuprokain Hidroklorür; Oksibuprokaino hidrochloridas; Oxibuprokain-hidroklorid; Oxibuprokainhydroklorid; Oxybuprocaïne, chlorhydrate d’; Oxybuprocaini hydrochloridum; Oxybuprokain hydrochlorid. 2-Diethylaminoethyl 4-amino-3-butoxybenzoate hydrochloride.
Cyrillic synonym: Оксибупрокаина Гидрохлорид.

💊 Chemical information

Chemical formula: C17H28N2O3,HCl = 344.9.
CAS — 99-43-4 (oxybuprocaine); 5987-82-6 (oxybuprocaine hydrochloride).
ATC — D04AB03; S01HA02.
ATC Vet — QD04AB03; QS01HA02.

Pharmacopoeias.

In Eur., Jpn, and US.

Ph. Eur. 6.2

(Oxybuprocaine Hydrochloride). A white or almost white, crystalline powder or colourless crystals. It exhibits polymorphism. Very soluble in water; freely soluble in alcohol. A 10% solution in water has a pH of 4.5 to 6.0. Protect from light.

USP 31

(Benoxinate Hydrochloride). White or slightly offwhite, crystals or crystalline powder, odourless or with a slight characteristic odour. Soluble 1 in 0.8 of water, 1 in 2.6 of alcohol, and 1 in 2.5 of chloroform; insoluble in ether. A 1% solution in water has a pH of 5.0 to 6.0.

💊 Adverse Effects, Treatment, and Precautions

Effects on the eyes.

Fibrinous iritis and moderate corneal swelling occurred in 2 patients after the use of a 0.4% or 1% solution of oxybuprocaine hydrochloride for topical anaesthesia of the eye for minor surgery.1 The effects may have been due to inadvertent entry of the drug into the anterior chamber of the eye.
1. Haddad R. Fibrinous iritis due to oxybuprocaine. Br J Ophthalmol 1989; 73: 76–7.

💊 Interactions

For interactions associated with local anaesthetics.

💊 Uses and Administration

It is used for surface anaesthesia and is reported to be less irritant than tetracaine when applied to the conjunctiva in therapeutic concentrations. Oxybuprocaine is used as the hydrochloride in a 0.4% solution in short ophthalmological procedures. One drop instilled into the conjunctival sac anaesthetises the surface of the eye sufficiently to allow tonometry after 60 seconds and a further drop after 90 seconds provides adequate anaesthesia for the fitting of contact lenses. Three drops at 90-second intervals produces sufficient anaesthesia after 5 minutes for removal of a foreign body from the corneal epithelium, or for incision of a Meibomian cyst through the conjunctiva. The sensitivity of the cornea is normal again after about 1 hour. A 1% solution of oxybuprocaine hydrochloride is used for surface anaesthesia of the ear, nose, and throat.

💊 Preparations

BP 2008: Oxybuprocaine Eye Drops; USP 31: Benoxinate Hydrochloride Ophthalmic Solution; Fluorescein Sodium and Benoxinate Hydrochloride Ophthalmic Solution.

Proprietary Preparations

Arg.: Oftalmocaina†; Austria: Benoxinat; Novain; Belg.: Unicaine; Braz.: Oxinest; Cz.: Benoxi; Novesin; Fin.: Oftan Obucain; Fr.: Cebesine; Novesine†; Ger.: Benoxinat SE†; Conjuncain-EDO; Novesine; Oxbarukain†; Hong Kong: Benoxinate†; Novesin†; Hung.: Humacain; India: Bendzon; Israel: Localin; Ital.: Novesina; Malaysia: Novesin†; Philipp.: Oxyben; Port.: Anestocil; Rus.: Inokain (Инокаин); S.Afr.: Novesin; Singapore: Novesin†; Spain: Prescaina; Switz.: Cebesin; Novesin; Thai.: Novesin; Turk.: Benoxinate; Novesin. Multi-ingredient: Austral.: Fluress; Austria: Flurekain; Cz.: Thilorbin†; Fin.: Oftan Flurekain; Fr.: Collu-Blache†; Ger.: Thilorbin; Mex.: Mentalgina; NZ: Fluress†; Port.: Fluotest; Mebocaina; Spain: Anestesi Doble; Fluotest; Swed.: Fluress; Switz.: Collu-Blache; Mebucaine; UAE: B-Cool; USA: FluOxinate†; Fluorox; Flurate; Fluress; Flurox.
Published November 22, 2018.