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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	255	29122-68-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: atenolol (RS)-Atenolol (+/-)-Atenolol betablok	A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect. Molecular weight: 266.34 Formula: C14H22N2O3 CLOGP: -0.11 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 84.58 ALOGS: -2.79 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

atenolol
(RS)-Atenolol
(+/-)-Atenolol
betablok

A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.

Molecular weight: 266.34
Formula: C14H22N2O3
CLOGP: -0.11
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 84.58
ALOGS: -2.79
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
75	mg	O
75	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	94 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	6.10 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	56 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	26.50 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	2.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	12.50 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.95 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.94 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 19, 1981	FDA	ALVOGEN IPCO SARL

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
Bradycardia	650.85	9.69	834	149487	72393	63266308
Pemphigus	403.91	9.69	6	150315	183720	63154981
Systemic lupus erythematosus	340.06	9.69	46	150275	208872	63129829
Hand deformity	317.86	9.69	14	150307	159443	63179258
Maternal exposure during pregnancy	286.21	9.69	83	150238	219979	63118722
Glossodynia	284.95	9.69	42	150279	178834	63159867
Off label use	255.23	9.69	787	149534	673675	62665026
Pericarditis	245.38	9.69	17	150304	131562	63207139
Wound	215.13	9.69	60	150261	163203	63175498
Hypotension	208.44	9.69	1228	149093	271376	63067325

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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
Bradycardia	520.03	10.27	824	95632	74594	34785881
Off label use	322.87	10.27	412	96044	419112	34441363
Myocardial infarction	268.94	10.27	839	95617	120246	34740229
Completed suicide	203.94	10.27	665	95791	97503	34762972
Coronary artery disease	194.62	10.27	419	96037	47886	34812589
Sinus bradycardia	181.88	10.27	201	96255	12762	34847713
Syncope	123.60	10.27	540	95916	90911	34769564
Hypotension	122.03	10.27	1035	95421	220614	34639861
Product use in unapproved indication	119.16	10.27	90	96366	117409	34743066
Cardiac failure congestive	110.46	10.27	489	95967	82781	34777694

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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
Bradycardia	1090.16	9.64	1517	199353	134040	79409478
Off label use	472.97	9.64	988	199882	906227	78637291
Myocardial infarction	429.03	9.64	1224	199646	182905	79360613
Coronary artery disease	328.69	9.64	591	200279	64883	79478635
Cardiac failure congestive	306.02	9.64	920	199950	141482	79402036
Sinus bradycardia	302.19	9.64	345	200525	24902	79518616
Hypotension	299.23	9.64	2015	198855	438302	79105216
Completed suicide	267.77	9.64	1277	199593	244490	79299028
Cerebrovascular accident	242.58	9.64	901	199969	154391	79389127
Pemphigus	222.59	9.64	6	200864	99576	79443942

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AB03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
ATC	C07BB03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, selective, and thiazides
ATC	C07CB03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, selective, and other diuretics
ATC	C07CB53	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, selective, and other diuretics
ATC	C07DB01	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, THIAZIDES AND OTHER DIURETICS Beta blocking agents, selective, thiazides and other diuretics
ATC	C07FB03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents and calcium channel blockers
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:38070	antiarrhythmic agent

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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
Myocardial infarction	indication	22298006	DOID:5844
Hypertensive disorder	indication	38341003	DOID:10763
Angina pectoris	indication	194828000
Chronic heart failure	off-label use	48447003
Atrial fibrillation	off-label use	49436004	DOID:0060224
Thyrotoxicosis	off-label use	90739004	DOID:7997
Mitral valve prolapse	off-label use	409712001
Diastolic heart failure	off-label use	418304008	DOID:9775
Essential tremor	off-label use	609558009	DOID:4990
Pheochromocytoma Adjunct Therapy	off-label use

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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	12.92	acidic
pKa2	9.19	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])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	7.30	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Kd	5.80	WOMBAT-PK
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		IC50	8.75	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		Kd	5.93	CHEMBL
Beta-1 adrenergic receptor	GPCR		B0FL73_CAVPO		Kd	7.62	CHEMBL
Urease	Enzyme		UREA_CANEN		IC50	4.19	CHEMBL

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External reference:

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ID	Source
2TN	PDB_CHEM_ID
001855	NDDF
1202	RXNORM
2249	PUBCHEM_CID
353	MMSL
3801	INN_ID
387506000	SNOMEDCT_US
4018460	VUID
4018460	VANDF
4225	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0752	TABLET	50 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0752	TABLET	50 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0752	TABLET	50 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0753	TABLET	100 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0753	TABLET	100 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0753	TABLET	100 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0787	TABLET	25 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0787	TABLET	25 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0787	TABLET	25 mg	ORAL	ANDA	24 sections
Atenolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0218	TABLET	25 mg	ORAL	ANDA	19 sections

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