Carteolol

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) 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.

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

Pharmacology

Pharmacodynamics

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

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]

Chemistry

The experimental log P of carteolol is 1.1 and its predicted log P ranges from 0.99 to 2.39.[4][5][6][7] It is a hydrophilic or low-lipophilicity beta blocker.[7][2]

Society and culture

Brand names

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

References

  1. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.
  2. 1 2 3 4 5 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.
  3. ↑ 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.
  4. ↑ "Carteolol". PubChem. Retrieved 10 July 2025.
  5. ↑ "C16H24N2O3". ChemSpider. 10 June 2024. Retrieved 10 July 2025.
  6. ↑ "Carteolol: Uses, Interactions, Mechanism of Action". DrugBank Online. 19 September 2006. Retrieved 10 July 2025.
  7. 1 2 Mannhold R (February 2005). "The impact of lipophilicity in drug research: a case report on beta-blockers". Mini Rev Med Chem. 5 (2): 197–205. doi:10.2174/1389557053402701. PMID 15720289.

Further reading

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