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Details

Stereochemistry RACEMIC
Molecular Formula C16H24N2O3
Molecular Weight 292.3734
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CARTEOLOL

SMILES

CC(C)(C)NCC(O)COC1=C2CCC(=O)NC2=CC=C1

InChI

InChIKey=LWAFSWPYPHEXKX-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Molecular Formula C16H24N2O3
Molecular Weight 292.3734
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Carteolol is a nonselective beta-adrenoceptor blocking agent for ophthalmic use. It has been shown to be effective in lowering intraocular pressure and may be used in patients with chronic open-angle glaucoma and intraocular hypertension. It may be used alone or in combination with other intraocular pressure lowering medications. The following adverse reactions have been reported: transient eye irritation, burning, tearing, conjunctival hyperemia and edema. Carteolol may cause bradycardia and decreased blood pressure, headache, arrhythmia, syncope, heart block, cerebral vascular accident, cerebral ischemia, congestive heart failure, palpitation, nausea, depression. Carteolol should be used with caution in patients who are receiving a beta-adrenergic blocking agent orally, because of the potential for additive effects on systemic beta-blockade.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
635.0 nM [EC50]
9.37 null [pKi]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
OCUPRESS
Primary
OCUPRESS

Cmax

ValueDoseCo-administeredAnalytePopulation
3.64 ng/mL
2 % 2 times / day multiple, ocular
CARTEOLOL plasma
Homo sapiens
0.998 ng/mL
1 drop single, ocular
CARTEOLOL plasma
Homo sapiens
1.627 ng/mL
1 drop 1 times / day multiple, ocular
CARTEOLOL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
10.27 ng × h/mL
2 % 2 times / day multiple, ocular
CARTEOLOL plasma
Homo sapiens
12.7 ng × h/mL
1 drop single, ocular
CARTEOLOL plasma
Homo sapiens
18 ng × h/mL
1 drop 1 times / day multiple, ocular
CARTEOLOL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
12.5 h
1 drop single, ocular
CARTEOLOL plasma
Homo sapiens
14.1 h
1 drop 1 times / day multiple, ocular
CARTEOLOL plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
40%
CARTEOLOL plasma
Homo sapiens

Doses

Drug as perpetrator​

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
The usual dose is one drop of 1% solution in the affected eye(s) twice a day.
Route of Administration: Topical
In Vitro Use Guide
Carteolol hydrochloride at 1 mmol/L attenuated the UVB-induced cell damage when added before, during, or after UVB irradiation (P<0.01). Carteolol hydrochloride at 1 mmol/L (P<0.05) significantly inhibited H2O2-induced cell damage and was able to scavenge O2 (EC50 value: 48 mmol/L).
Substance Class Chemical
Record UNII
8NF31401XG
Record Status Validated (UNII)
Record Version