Carteolol

Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.^{[citation needed]}

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 Y
ChemSpider	2485 Y
UNII	8NF31401XG
KEGG	D07624 Y
ChEBI	CHEBI:3437 Y
ChEMBL	ChEMBL839 Y
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) Y Key:LWAFSWPYPHEXKX-UHFFFAOYSA-N Y
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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-HT_1A and 5-HT_1B 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.