carteolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	520	51781-06-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carteolol dl-Carteolol carteolol hydrochloride carteolol HCl	A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. Molecular weight: 292.38 Formula: C16H24N2O3 CLOGP: 1.29 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 70.59 ALOGS: -2.84 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carteolol
dl-Carteolol
carteolol hydrochloride
carteolol HCl

A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent.

Molecular weight: 292.38
Formula: C16H24N2O3
CLOGP: 1.29
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 70.59
ALOGS: -2.84
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	88 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	60 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	4.70 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	4.05 L/kg	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	10.13 mL/min/kg	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
CL (Clearance)	10.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.49 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1988	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intraocular pressure increased	67.85	34.07	14	417	6064	63482527

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatitis fulminant	46.93	39.77	10	277	4180	34952464

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intraocular pressure increased	67.32	30.38	16	755	9189	79734428
Choluria	30.77	30.38	5	766	401	79743216
Bradycardia	30.65	30.38	18	753	135539	79608078

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AA15	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective
ATC	S01ED05	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents
ATC	S01ED55	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:39456	antiglaucoma agent
CHEBI has role	CHEBI:66991	sympatholytic drug
FDA EPC	N0000175556	beta-Adrenergic Blocker
FDA MoA	N0000000161	Adrenergic beta-Antagonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Ocular hypertension	indication	4210003	DOID:9282
Hypertensive disorder	indication	38341003	DOID:10763
Open-angle glaucoma	indication	84494001	DOID:1067
Angina pectoris	off-label use	194828000
Complete atrioventricular block	contraindication	27885002
Anaphylaxis	contraindication	39579001
Sinus bradycardia	contraindication	49710005
Chronic bronchitis	contraindication	63480004	DOID:6132
Diabetes mellitus	contraindication	73211009	DOID:9351
Heart failure	contraindication	84114007	DOID:6000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.31	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	9.30		WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Ki	9.20		WOMBAT-PK	CHEMBL

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External reference:

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ID	Source
001863	NDDF
004747	NDDF
108544005	SNOMEDCT_US
142132	RXNORM
2583	PUBCHEM_CID
31453	MMSL
386866004	SNOMEDCT_US
386867008	SNOMEDCT_US
3990	INN_ID
4019351	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Carteolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	61314-238	SOLUTION	10 mg	OPHTHALMIC	ANDA	19 sections

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