Carteolol

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

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)

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]

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. 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). 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.

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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