Carteolol

Carteolol
Clinical data
Trade names	Ocupress
AHFS/Drugs.com	Professional Drug Facts
MedlinePlus	a601078
License data	US DailyMed: Carteolol;
Routes of; administration	Eye drops
ATC code	C07AA15 (WHO) S01ED05 (WHO);
Legal status
Legal status	US: ℞-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	85%
Metabolism	Liver, active with 8-hydrocarteolol
Elimination half-life	6–8 hours
Excretion	Kidney (50-70%)
Identifiers
	IUPAC name (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 ;
ChemSpider	2485 ;
UNII	8NF31401XG;
KEGG	D07624 ;
ChEBI	CHEBI:3437 ;
ChEMBL	ChEMBL839 ;
CompTox Dashboard (EPA)	DTXSID3022746 ;
Chemical and physical data
Formula	C16H24N2O3
Molar mass	292.379 g·mol−1
3D model (JSmol)	Interactive image;
Chirality	Racemic 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) ; Key:LWAFSWPYPHEXKX-UHFFFAOYSA-N ;
	(verify)

Carteolol is a non-selective beta blocker used to treat glaucoma.

It has been found to act as a serotonin 5-HT_1A and 5-HT_1B 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

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

References

^ Langlois M, Brémont B, Rousselle D, Gaudy F (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". Eur. J. Pharmacol. 244 (1): 77–87. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.
^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 9783527607495.

External links

El-Kamel A, Al-Dosari H, Al-Jenoobi F (2006). "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride". Drug Deliv. 13 (1): 55–9. doi:10.1080/10717540500309073. PMID 16401594. S2CID 30222292.
Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A (2005). "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro". Cornea. 24 (2): 213–20. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891. S2CID 20523541.
Trinquand C, Romanet J, Nordmann J, Allaire C (2003). "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". J Fr Ophtalmol. 26 (2): 131–6. PMID 12660585.

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[pmid8093601-1] Langlois M, Brémont B, Rousselle D, Gaudy F (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". Eur. J. Pharmacol. 244 (1): 77–87. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.

[2] Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 9783527607495.

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