Proxymetacaine Hydrochloride

(BANM, rINNM)
Proxymetacaine Hydrochloride Chemical formula
Synonyms: (BANM, rINNM) Hidrocloruro de proximetacaína; Proksimetakain Hidroklorür; Proparacaine Hydrochloride; Proparakain Hidroklorür; Proxymétacaïne, Chlorhydrate de; Proxymetacaini Hydrochloridum. 2-Diethylaminoethyl 3-amino4-propoxybenzoate hydrochloride.
Cyrillic synonym: Проксиметакаина Гидрохлорид.

💊 Chemical information

Chemical formula: C16H26N2O3,HCl = 330.9.
CAS — 499-67-2 (proxymetacaine); 5875-06-9 ATC — S01HA04.
ATC Vet — QS01HA04.

BP 2008

for use on single unit doses of eye drops containing proxymetacaine hydrochloride where the individual container may be too small to bear all the appropriate labelling information. PROXFLN is a similar code approved for eye drops containing proxymetacaine hydrochloride and fluorescein sodium.

Pharmacopoeias.

In Br. and US.

BP 2008

(Proxymetacaine Hydrochloride). A white or almost white, odourless or almost odourless, crystalline powder. Soluble in water and in chloroform; very soluble in dehydrated alcohol; practically insoluble in ether. A 1% solution in water has a pH of 5.7 to 6.4. Protect from light.

USP 31

(Proparacaine Hydrochloride). A white to off-white, or faintly buff-coloured, odourless, crystalline powder. Soluble in water, in warm alcohol, and in methyl alcohol; insoluble in ether and in benzene.

💊 Adverse Effects, Treatment, and Precautions

A severe immediate-type corneal reaction to proxymetacaine may rarely occur. Allergic contact dermatitis has also been reported.

Effects on the skin.

Exacerbation of Stevens-Johnson syndrome has been reported1 in a woman after ophthalmic anaesthesia with proxymetacaine hydrochloride.
1. Ward B, et al. Dermatologic reaction in Stevens-Johnson syndrome after ophthalmic anesthesia with proparacaine hydrochloride. Am J Ophthalmol 1978; 86: 133–5.

💊 Interactions

For interactions associated with local anaesthetics.

💊 Pharmacokinetics

See under Local Anaesthetics.

💊 Uses and Administration

It is used for surface anaesthesia in ophthalmology in a concentration of 0.5%. Proxymetacaine is of similar potency to tetracaine in equal concentrations and induces anaesthesia within about 20 seconds. The duration of action may be 15 minutes or longer. Instillation of 1 or 2 drops permits tonometry after 30 seconds. For removal of foreign bodies or sutures from the cornea 1 or 2 drops are instilled every 5 to 10 minutes for up to 3 applications, or 1 or 2 drops are instilled 2 to 3 minutes before the procedure. For deeper anaesthesia such as needed for cataract extraction 1 drop is instilled every 5 to 10 minutes to a total of 5 to 7 applications.

Trigeminal neuralgia.

There have been anecdotal reports that proxymetacaine eye drops relieved trigeminal neuralgia refractory to carbamazepine.1,2 However, a controlled study failed to demonstrate any benefit.3
1. Zavon MR, Fichte CM. Trigeminal neuralgia relieved by ophthalmic anesthetic. JAMA 1991; 265: 2807
2. Zavon MR, Fichte CM. Trigeminal neuralgia relieved by optical anesthesia. JAMA 1991; 266: 1649
3. Kondziolka D, et al. The effect of single-application topical ophthalmic anesthesia in patients with trigeminal neuralgia: a randomized double-blind placebo-controlled trial. J Neurosurg 1994; 80: 993–7.

💊 Preparations

BP 2008: Proxymetacaine Eye Drops; USP 31: Fluorescein Sodium and Proparacaine Hydrochloride Ophthalmic Solution; Proparacaine Hydrochloride Ophthalmic Solution.

Proprietary Preparations

Arg.: Anestalcon; Poencaina; Austral.: Alcaine; Ophthetic†; Belg.: Alcaine; Braz.: Anestalcon; Visonest; Canad.: Ak-Taine; Alcaine; Diocaine†; Ophthetic†; Chile: Anestalcon; Ger.: Proparakain-POS; Gr.: Alcaine; Hong Kong: Alcaine; Malaysia: Alcaine; Mex.: Alcaine; Norw.: Alcaine; NZ: Ophthetic; Philipp.: Alcaine; Pol.: Alcaine; Rus.: Alcaine (Алкаин); Singapore: Alcaine; Switz.: Alcaine; Turk.: Alcaine; Opticaine; USA: Ak-Taine; Alcaine; Ocu-Caine; Ophthetic; Parcaine; Venez.: Alcaine; Oftaine†; Poencaina. Multi-ingredient: Canad.: Fluoracaine†; USA: Fluoracaine; Fluorocaine.
Published December 03, 2018.