Carteolol

Carteolol is a non-selective beta blocker used to treat glaucoma.

Carteolol
Clinical data
Trade namesOcupress
AHFS/Drugs.comMicromedex Detailed Consumer Information
MedlinePlusa601078
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration
    Eye drops
    ATC code
    Legal status
    Legal status
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Bioavailability85%
    MetabolismHepatic, active with 8-hydrocarteolol
    Elimination half-life6–8 hours
    ExcretionRenal (50-70%)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC16H24N2O3
    Molar mass292.373 g/mol g·mol−1
    3D model (JSmol)
    ChiralityRacemic mixture
      (verify)

    It has been found to act as a serotonin 5-HT1A and 5-HT1B receptor antagonist in addition to being a beta blocker.[1]

    It was patented in 1972 and approved for medical use in 1980.[2]

    Brand names

    Brand names include Cartrol, Ocupress, Teoptic, Arteolol, Arteoptic, Calte, Cartéabak, Carteol, Cartéol, Cartrol, Elebloc, Endak, Glauteolol, Mikelan, Poenglaucol, and Singlauc.

    References

    1. Langlois M, Brémont B, Rousselle D, Gaudy F (1993). "Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors". Eur. J. Pharmacol. 244 (1): 77–87. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.
    2. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 9783527607495.
    • El-Kamel A, Al-Dosari H, Al-Jenoobi F (2006). "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride". Drug Deliv. 13 (1): 55–9. doi:10.1080/10717540500309073. PMID 16401594.
    • Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A (2005). "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro". Cornea. 24 (2): 213–20. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891.
    • Trinquand C, Romanet J, Nordmann J, Allaire C (2003). "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". J Fr Ophtalmol. 26 (2): 131–6. PMID 12660585.



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