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
  • (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)

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
  • Arteolol
  • Arteoptic
  • Calte
  • Cartéabak
  • Carteol
  • Cartéol
  • Cartrol
  • Elebloc
  • Endak
  • Glauteolol
  • Mikelan
  • Ocupress
  • Poenglaucol
  • Teoptic
  • Singlauc

References
  1. 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.
  2. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.

Further reading
  • El-Kamel A, Al-Dosari H, Al-Jenoobi F (2006). "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride". Drug Delivery. 13 (1): 55–59. doi:10.1080/10717540500309073. PMID 16401594. S2CID 30222292.
  • 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 Francais d'Ophtalmologie. 26 (2): 131–136. PMID 12660585.
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