Carteolol

Chemical compound
  • US DailyMed: Carteolol
Routes of
administrationEye dropsATC code
  • C07AA15 (WHO) S01ED05 (WHO)
Legal statusLegal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic dataBioavailability85%MetabolismLiver, active with 8-hydrocarteololElimination half-life6–8 hoursExcretionKidney (50–70%)Identifiers
  • (RS)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one
CAS Number
  • 51781-06-7
PubChem CID
  • 2583
IUPHAR/BPS
  • 7142
DrugBank
  • DB00521 checkY
ChemSpider
  • 2485 checkY
UNII
  • 8NF31401XG
KEGG
  • D07624 checkY
ChEBI
  • CHEBI:3437 checkY
ChEMBL
  • ChEMBL839 checkY
CompTox Dashboard (EPA)
  • DTXSID3022746 Edit this at Wikidata
Chemical and physical dataFormulaC16H24N2O3Molar mass292.379 g·mol−13D model (JSmol)
  • Interactive image
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 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. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.
  2. ^ a b c d 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.

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 Français d'Ophtalmologie. 26 (2): 131–136. PMID 12660585.
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Drugs used for glaucoma preparations and miosis (S01E)
SympathomimeticsParasympathomimetics
muscarinic
muscarinic/nicotinic
acetylcholinesterase inhibitors
Carbonic anhydrase inhibitors/
(sulfonamides)Beta blocking agentsProstaglandin analogues (F)Other agents
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α1
Agonists
Antagonists
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β
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  • See also: Receptor/signaling modulators
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5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
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5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins


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