Carteolol

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

Carteolol
Clinical data
Trade namesOcupress
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa601078
License data
Routes of
administration		Eye drops
ATC code
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability85%
MetabolismLiver, active with 8-hydrocarteolol
Elimination half-life6–8 hours
ExcretionKidney (50-70%)
Identifiers
IUPAC name
  • (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
SMILES
  • O=C2Nc1cccc(OCC(O)CNC(C)(C)C)c1CC2
InChI
  • 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) Y
  • Key:LWAFSWPYPHEXKX-UHFFFAOYSA-N Y
  (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. S2CID 30222292.
  • 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. S2CID 20523541.
  • 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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