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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	1865	42200-33-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nadolol corgard anabet solgol	A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor. Molecular weight: 309.41 Formula: C17H27NO4 CLOGP: 0.38 LIPINSKI: 0 HAC: 5 HDO: 4 TPSA: 81.95 ALOGS: -2.14 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nadolol
corgard
anabet
solgol

A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.

Molecular weight: 309.41
Formula: C17H27NO4
CLOGP: 0.38
LIPINSKI: 0
HAC: 5
HDO: 4
TPSA: 81.95
ALOGS: -2.14
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.16	g	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	9.20 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	73 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	34.58 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	2.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	2.25 mg/mL	Bocci G, Oprea TI, Benet LZ
Vd (Volume of distribution)	1.90 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.14 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 10, 1979	FDA	KING PHARMS

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
Macular degeneration	932.65	15.07	293	11672	24083	63452974
Chronic sinusitis	195.54	15.07	78	11887	12765	63464292
Paraesthesia oral	159.03	15.07	76	11889	19180	63457877
Procedural pain	150.84	15.07	76	11889	21493	63455564
Neovascularisation	148.48	15.07	36	11929	1109	63475948
Drug ineffective	135.46	15.07	466	11499	1044299	62432758
Dyspepsia	128.52	15.07	125	11840	102071	63374986
Weight decreased	115.15	15.07	195	11770	276603	63200454
Vaginal flatulence	102.78	15.07	34	11931	3259	63473798
Paradoxical drug reaction	102.67	15.07	36	11929	4116	63472941

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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
Hepatic encephalopathy	94.72	17.10	45	5010	14640	34937236
Varices oesophageal	67.53	17.10	24	5031	3731	34948145
Ascites	47.35	17.10	45	5010	46526	34905350
Hepatic cirrhosis	47.08	17.10	30	5025	17284	34934592
Hepatic failure	46.27	17.10	39	5016	34492	34917384
Oesophageal varices haemorrhage	41.44	17.10	16	5039	3130	34948746
Hypoglycaemia	37.87	17.10	43	5012	54597	34897279
Lactic acidosis	34.19	17.10	33	5022	34739	34917137
Bradycardia	32.70	17.10	47	5008	75371	34876505
Portal hypertensive gastropathy	32.48	17.10	9	5046	618	34951258

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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
Macular degeneration	193.03	14.39	74	14515	11222	79718577
Chronic sinusitis	186.25	14.39	75	14514	12951	79716848
Paraesthesia oral	150.70	14.39	74	14515	20397	79709402
Neovascularisation	146.54	14.39	36	14553	1209	79728590
Procedural pain	142.29	14.39	74	14515	23010	79706789
Dyspepsia	123.22	14.39	124	14465	108563	79621236
Vaginal flatulence	107.73	14.39	33	14556	2542	79727257
Weight decreased	93.88	14.39	203	14386	354995	79374804
Varices oesophageal	90.84	14.39	36	14553	5955	79723844
Paradoxical drug reaction	84.52	14.39	36	14553	7149	79722650

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AA12	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective
ATC	C07BA12	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, non-selective, and thiazides
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:66991	sympatholytic drug
FDA EPC	N0000175556	beta-Adrenergic Blocker
FDA MoA	N0000000161	Adrenergic beta-Antagonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic 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
Hypertensive disorder	indication	38341003	DOID:10763
Angina pectoris	indication	194828000
Thyrotoxicosis	off-label use	90739004	DOID:7997
Mitral valve prolapse	off-label use	409712001
Essential tremor	off-label use	609558009	DOID:4990
Prevention of Congenital Long QT Syndrome associated Ventricular Arrhythmia	off-label use
Myocardial Reinfarction Prevention	off-label use
Prevention of Bleeding Esophageal Varices	off-label use
Migraine Prevention	off-label use
Anuria	contraindication	2472002	DOID:2983

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.57	acidic
pKa2	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])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	6.90	IUPHAR	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Ki	8.60	IUPHAR	CHEMBL
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN	ANTAGONIST	Ki	6.30	IUPHAR

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External reference:

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ID	Source
001854	NDDF
151549	RXNORM
2018	MMSL
220045-89-6	SECONDARY_CAS_RN
31	MMSL
387482003	SNOMEDCT_US
3875	INN_ID
39147	PUBCHEM_CID
4017603	VUID
4017603	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Corgard	HUMAN PRESCRIPTION DRUG LABEL	1	27505-100	TABLET	20 mg	ORAL	NDA	20 sections
Corgard	HUMAN PRESCRIPTION DRUG LABEL	1	27505-101	TABLET	40 mg	ORAL	NDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0028	TABLET	20 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0028	TABLET	20 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1132	TABLET	80 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1132	TABLET	80 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1171	TABLET	40 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1171	TABLET	40 mg	ORAL	ANDA	20 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-8004	TABLET	20 mg	ORAL	ANDA	21 sections
Nadolol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-8004	TABLET	20 mg	ORAL	ANDA	21 sections

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