Proxymetacaine

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

Proxymetacaine
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
    CompTox Dashboard (EPA)
    ECHA InfoCard100.007.169
    Chemical and physical data
    FormulaC16H26N2O3
    Molar mass294.389 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Clinical pharmacology

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

    Mechanism of action

    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

    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

    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

    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

    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.CS1 maint: extra text: authors list (link)
    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.
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