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Contents

   



(Top)
  


1 Pharmacology  


1.1  Pharmacodynamics  




1.2  Pharmacokinetics  






2 Society and culture  


2.1  Brand names  






3 References  




4 Further reading  













Carteolol






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From Wikipedia, the free encyclopedia
  

Carteolol
Clinical data
Trade namesOcupress
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa601078
License data
Routes of
administration		Eye drops
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
    • Pharmacokinetic data
    Bioavailability85%
    MetabolismLiver, active with 8-hydrocarteolol
    Elimination half-life6–8 hours
    ExcretionKidney (50–70%)
    Identifiers

    • (RS)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one

    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC16H24N2O3
    Molar mass292.379 g·mol−1
    3D model (JSmol)
    ChiralityRacemic mixture

    • O=C2Nc1cccc(OCC(O)CNC(C)(C)C)c1CC2

    • InChI=1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20) checkY

    • Key:LWAFSWPYPHEXKX-UHFFFAOYSA-N checkY

      (verify)

    Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.[citation needed]

    Carteolol was patented in 1972 and approved for medical use in 1980.[1]

    Pharmacology[edit]

    Pharmacodynamics[edit]

    Carteolol is a beta blocker, or an antagonist of the β-adrenergic receptors.[2] It is selective for the β1-adrenergic receptor and has intrinsic sympathomimetic activity.[2] Carteolol has also been found to act as a serotonin 5-HT1A and 5-HT1B receptor antagonist in addition to being a beta blocker.[3]

    Pharmacokinetics[edit]

    Carteolol is classified as a beta blocker with low lipophilicity and hence lower potential for crossing the blood–brain barrier.[2] This in turn may result in fewer effects in the central nervous system as well as a lower risk of neuropsychiatric side effects.[2]

    Society and culture[edit]

    Brand names[edit]

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

    References[edit]

    1. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.
  • ^ a b c d Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM (February 2021). "Neuropsychiatric Consequences of Lipophilic Beta-Blockers". Medicina (Kaunas). 57 (2): 155. doi:10.3390/medicina57020155. PMC 7914867. PMID 33572109.
  • ^ Langlois M, Brémont B, Rousselle D, Gaudy F (January 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". European Journal of Pharmacology. 244 (1): 77–87. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.

    • Further reading[edit]

  • Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A (March 2005). "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro". Cornea. 24 (2): 213–220. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891. S2CID 20523541.
  • Trinquand C, Romanet JP, Nordmann JP, Allaire C (February 2003). "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". Journal Français d'Ophtalmologie. 26 (2): 131–136. PMID 12660585.

    • Retrieved from "https://en.wikipedia.org/w/index.php?title=Carteolol&oldid=1225477848"
    Categories: 
    ●2-Quinolones
     ●5-HT1A antagonists
     ●5-HT1B antagonists
     ●Beta blockers
     ●N-tert-butyl-phenoxypropanolamines
     ●Ophthalmology drugs
     ●Peripherally selective drugs
     Hidden categories: 
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     ●Short description matches Wikidata
     ●Drugs with non-standard legal status
     ●All articles with unsourced statements
     ●Articles with unsourced statements from September 2023
      


    ●This page was last edited on 24 May 2024, at 17:42 (UTC).
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