Chemistry:Carteolol

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Short description: Chemical compound
Carteolol
Carteolol skeletal.svg
Clinical data
Trade namesOcupress
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa601078
License data
Pregnancy
category
  • US: C (Risk not ruled out)
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
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC16H24N2O3
Molar mass292.379 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  (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

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. ↑ (in en) Analogue-based Drug Discovery. John Wiley & Sons. 2006. p. 460. ISBN 978-3-527-60749-5. https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA460. 
  2. ↑ 2.0 2.1 2.2 2.3 "Neuropsychiatric Consequences of Lipophilic Beta-Blockers". Medicina (Kaunas) 57 (2): 155. February 2021. doi:10.3390/medicina57020155. PMID 33572109. 
  3. ↑ "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. January 1993. doi:10.1016/0922-4106(93)90061-d. PMID 8093601. 

Further reading

  • "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride". Drug Delivery 13 (1): 55–59. 2006. doi:10.1080/10717540500309073. PMID 16401594. 
  • "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro". Cornea 24 (2): 213–220. March 2005. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891. 
  • "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". Journal Francais d'Ophtalmologie 26 (2): 131–136. February 2003. PMID 12660585. 




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