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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	60 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.49 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	88 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	10.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.70 hours	Lombardo F, Berellini G, Obach RS
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
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

Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1988	FDA

FDA Adverse Event Reporting System (Female)

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

FDA Adverse Event Reporting System (Male)

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

FDA Adverse Event Reporting System (Geriatric)

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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
FDA MoA	N0000000161	Adrenergic beta-Antagonists
FDA EPC	N0000175556	beta-Adrenergic Blocker
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
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D013565	Sympatholytics

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

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
Pulmonary emphysema	contraindication	87433001
Cardiogenic shock	contraindication	89138009
Myasthenia gravis	contraindication	91637004	DOID:437
Second degree atrioventricular block	contraindication	195042002
Decompensated cardiac failure	contraindication	195111005
Asthma	contraindication	195967001	DOID:2841
Pregnancy, function	contraindication	289908002
Severe chronic obstructive pulmonary disease	contraindication	313299006

🐶 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:

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

External reference:

ID	Source
4019351	VUID
N0000147523	NUI
D00599	KEGG_DRUG
51781-21-6	SECONDARY_CAS_RN
142132	RXNORM
C0007299	UMLSCUI
CHEBI:3437	CHEBI
CHEMBL839	ChEMBL_ID
DB00521	DRUGBANK_ID
CHEMBL1201002	ChEMBL_ID
D002354	MESH_DESCRIPTOR_UI
2583	PUBCHEM_CID
7142	IUPHAR_LIGAND_ID
3990	INN_ID
8NF31401XG	UNII
31453	MMSL
4361	MMSL
4362	MMSL
d00708	MMSL
108544005	SNOMEDCT_US
386866004	SNOMEDCT_US
386867008	SNOMEDCT_US
4019351	VANDF
4020617	VANDF
001863	NDDF
004747	NDDF

Pharmaceutical products:

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