Proxymetacaine

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Proxymetacaine
Proxymetacaine structure.svg
Clinical data
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
Topical (eye drops)
ATC code
Pharmacokinetic data
MetabolismPlasma
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard100.007.169 Edit this at Wikidata
Chemical and physical data
FormulaC16H26N2O3
Molar mass294.389 g/mol
3D model (JSmol)
  (verify)

Proxymetacaine (INN) or proparacaine (USAN) is a topical anesthetic drug of the aminoester group.

Clinical pharmacology[edit]

Proxymetacaine is a local anesthetic which on topical application penetrates sensory nerve endings in the corneal tissue.[1]

Mechanism of action[edit]

Proxymetacaine is believed to act as an antagonist on voltage-gated sodium channels to affect the permeability of neuronal membranes; how this inhibits pain sensations and the exact mechanism of action of proxymetacaine are, however, unknown.[2]

Indications and usage[edit]

Proxymetacaine hydrochloride ophthalmic solution (eye drops) is indicated for procedures such as tonometry, gonioscopy, removal of foreign bodies, or other similar procedures requiring topical anesthesia of the cornea and conjunctiva.[3]

Warnings[edit]

Proxymetacaine is for topical ophthalmic use only, and it is specifically not intended for injection. Prolonged use of this or any other topical ocular anesthetic may produce permanent corneal opacification with accompanying visual loss.

How supplied[edit]

Proxymetacaine is available as its hydrochloride salt in ophthalmic solutions at a concentration of 0.5%. Although it is no longer on patent, it is still marketed under the trade names Alcaine, Ak-Taine, and others. Proparacaine 0.5% is marketed as Poencaina by Poen Laboratories.[4]

References[edit]

  1. ^ Draeger, J.; Langenbucher, H.; Bannert, C. (1984). "Efficacy of Topical Anaesthetics". Ophthalmic Research. 16 (3): 135–138. doi:10.1159/000265308. PMID 6472792.
  2. ^ Melmon, editors Alfred Goodman Gilman, Louis S. Goodman, Alfred Gilman ; associate editors Steven E. Mayer, Kenneth L. (1980). The Pharmacological Basis of Therapeutics ; Alfred Goodman Gilman (6 ed.). New York: MacMillan Pub. ISBN 978-0023447204.
  3. ^ Murphy, Paul J.; Ntola, Anna M. (April 2009). "Prolonged corneal anaesthesia by proxymetacaine hydrochloride detected by a thermal cooling stimulus". Contact Lens and Anterior Eye. 32 (2): 84–87. doi:10.1016/j.clae.2008.12.006. PMID 19181566.
  4. ^ "Poen-Caina generic. Price of poen-caina. Uses, Indications and Description". ndrugs. Retrieved 15 March 2018.