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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	40	37517-30-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: IL-17803A acebutolol HCl acebutolol acebutolol hydrochloride (RS)-Acebutolol (+/-)-Acebutolol dl-Acebutolol	A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action. Molecular weight: 336.43 Formula: C18H28N2O4 CLOGP: 1.71 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 87.66 ALOGS: -3.29 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

IL-17803A
acebutolol HCl
acebutolol
acebutolol hydrochloride
(RS)-Acebutolol
(+/-)-Acebutolol
dl-Acebutolol

A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.

Molecular weight: 336.43
Formula: C18H28N2O4
CLOGP: 1.71
LIPINSKI: 0
HAC: 6
HDO: 3
TPSA: 87.66
ALOGS: -3.29
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.40	g	O
0.40	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	46.09 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	37 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	10 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.74 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1984	FDA	PROMIUS PHARMA

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
Orthostatic hypotension	1355.03	38.05	397	8350	35763	63444512
Sedation complication	1332.67	38.05	321	8426	13501	63466774
Creatinine renal clearance decreased	1284.91	38.05	322	8425	15986	63464289
Cognitive disorder	1277.73	38.05	420	8327	55395	63424880
Sedation	1253.69	38.05	380	8367	38429	63441846
Blood calcium decreased	1130.53	38.05	322	8425	26129	63454146
Balance disorder	1006.93	38.05	392	8355	84030	63396245
Depressed level of consciousness	893.67	38.05	331	8416	61747	63418528
Mobility decreased	716.68	38.05	343	8404	120816	63359459
Hypotension	692.31	38.05	441	8306	272163	63208112
Constipation	659.43	38.05	399	8348	224544	63255731
Fall	573.40	38.05	453	8294	391881	63088394
Toxicity to various agents	548.33	38.05	368	8379	246882	63233393
Multiple drug therapy	176.07	38.05	49	8698	3597	63476678
Pain	152.91	38.05	322	8425	740306	62739969
Endometriosis	93.43	38.05	33	8714	5287	63474988
Drug specific antibody	92.74	38.05	27	8720	2328	63477947
Diabetes mellitus inadequate control	74.48	38.05	38	8709	15088	63465187
Blood pressure inadequately controlled	58.51	38.05	23	8724	4955	63475320
Fatigue	58.19	38.05	25	8722	888003	62592272
Hypocoagulable state	57.25	38.05	16	8731	1191	63479084
Headache	51.76	38.05	12	8735	633229	62847046
Exercise tolerance decreased	49.55	38.05	21	8726	5476	63474799
Cardiogenic shock	44.93	38.05	29	8718	17903	63462372
Oesophageal food impaction	42.40	38.05	9	8738	208	63480067
Nausea	41.90	38.05	34	8713	854437	62625838
Oesophageal achalasia	40.14	38.05	10	8737	476	63479799
Diarrhoea	38.22	38.05	26	8721	715340	62764935

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
Pancreatic carcinoma metastatic	71.12	23.45	19	1976	2921	34952015
Linear IgA disease	41.65	23.45	11	1984	1615	34953321
Interstitial lung disease	38.59	23.45	31	1964	65251	34889685
Pancreatitis acute	34.69	23.45	21	1974	28120	34926816
Ischaemic stroke	34.41	23.45	18	1977	18232	34936704
Pulmonary fibrosis	34.27	23.45	18	1977	18378	34936558
Sudden death	31.56	23.45	16	1979	15185	34939751
Cerebral haematoma	30.35	23.45	11	1984	4604	34950332
Bradycardia	25.18	23.45	26	1969	75392	34879544
Subdural haematoma	24.54	23.45	15	1980	20406	34934530
Eosinophilia	23.46	23.45	16	1979	26206	34928730

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
Sedation complication	1358.15	27.40	333	10456	15336	79718263
Creatinine renal clearance decreased	1284.58	27.40	331	10458	18671	79714928
Cognitive disorder	1221.22	27.40	428	10361	69498	79664101
Orthostatic hypotension	1212.24	27.40	403	10386	55761	79677838
Sedation	1166.35	27.40	384	10405	51511	79682088
Blood calcium decreased	1128.76	27.40	334	10455	31485	79702114
Balance disorder	976.20	27.40	399	10390	98458	79635141
Depressed level of consciousness	799.03	27.40	344	10445	96308	79637291
Mobility decreased	743.30	27.40	351	10438	121824	79611775
Constipation	606.84	27.40	410	10379	282640	79450959
Hypotension	589.48	27.40	480	10309	439837	79293762
Fall	530.53	27.40	472	10317	487157	79246442
Toxicity to various agents	400.71	27.40	379	10410	421161	79312438
Pain	190.78	27.40	340	10449	703462	79030137
Multiple drug therapy	167.02	27.40	48	10741	4030	79729569
Endometriosis	101.87	27.40	32	10757	3636	79729963
Drug specific antibody	85.98	27.40	26	10763	2602	79730997
Diabetes mellitus inadequate control	60.86	27.40	39	10750	24225	79709374
Pancreatic carcinoma metastatic	54.00	27.40	20	10769	3733	79729866
Blood pressure inadequately controlled	50.81	27.40	22	10767	6155	79727444
Hypocoagulable state	48.36	27.40	16	10773	2143	79731456
Fatigue	46.40	27.40	35	10754	929692	78803907
Pneumonia	44.37	27.40	17	10772	660229	79073370
Bradycardia	43.57	27.40	71	10718	135486	79598113
Cerebral haematoma	42.52	27.40	21	10768	7921	79725678
Headache	40.45	27.40	19	10770	653753	79079846
Oesophageal food impaction	37.20	27.40	9	10780	386	79733213
Exercise tolerance decreased	37.06	27.40	20	10769	9051	79724548
Oesophageal achalasia	35.45	27.40	10	10779	784	79732815
Morbid thoughts	35.35	27.40	10	10779	792	79732807
Nausea	35.19	27.40	47	10742	957149	78776450
Cor pulmonale acute	32.14	27.40	9	10780	687	79732912
Diarrhoea	30.57	27.40	45	10744	880444	78853155
Death	29.93	27.40	20	10769	566494	79167105

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C07AB04	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
ATC	C07BB04	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, selective, and thiazides
FDA MoA	N0000000161	Adrenergic beta-Antagonists
FDA EPC	N0000175556	beta-Adrenergic Blocker
CHEBI has role	CHEBI:35524	sympathomimetic
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D058671	Adrenergic beta-1 Receptor 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	D013566	Sympathomimetics

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

Disease	Relation	SNOMED_ID	DOID
Ventricular premature beats	indication	17338001
Hypertensive disorder	indication	38341003	DOID:10763
Anxiety	off-label use	48694002
Thyrotoxicosis	off-label use	90739004	DOID:7997
Angina pectoris	off-label use	194828000
Mitral valve prolapse	off-label use	409712001
Myocardial Reinfarction Prevention	off-label use
Psoriasis	contraindication	9014002	DOID:8893
Complete atrioventricular block	contraindication	27885002
Depressive disorder	contraindication	35489007
Sick sinus syndrome	contraindication	36083008	DOID:13884
Anaphylaxis	contraindication	39579001
Sinus bradycardia	contraindication	49710005
Diabetes mellitus	contraindication	73211009	DOID:9351
Pulmonary emphysema	contraindication	87433001
Cardiogenic shock	contraindication	89138009
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Partial atrioventricular block	contraindication	195039008
Decompensated cardiac failure	contraindication	195111005
Asthma	contraindication	195967001	DOID:2841
Disease of liver	contraindication	235856003	DOID:409
Raynaud's phenomenon	contraindication	266261006
Pregnancy, function	contraindication	289908002
Pheochromocytoma	contraindication	302835009
Severe chronic obstructive pulmonary disease	contraindication	313299006
Peripheral arterial occlusive disease	contraindication	399957001
Peripheral vascular disease	contraindication	400047006
Acute exacerbation of asthma	contraindication	708038006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.19	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])	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		Ki	6.40	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5	CHEMBL

External reference:

ID	Source
4018063	VUID
N0000179521	NUI
D00597	KEGG_DRUG
34381-68-5	SECONDARY_CAS_RN
142130	RXNORM
C0000946	UMLSCUI
CHEBI:2379	CHEBI
CHEMBL642	ChEMBL_ID
CHEMBL1200813	ChEMBL_ID
DB01193	DRUGBANK_ID
D000070	MESH_DESCRIPTOR_UI
1978	PUBCHEM_CID
7107	IUPHAR_LIGAND_ID
3295	INN_ID
67P356D8GH	UNII
3597005	SNOMEDCT_US
372815001	SNOMEDCT_US
68088000	SNOMEDCT_US
4018063	VANDF
4019592	VANDF
4118	MMSL
64	MMSL
d00128	MMSL
001858	NDDF
004742	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-630	CAPSULE	200 mg	ORAL	ANDA	21 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-631	CAPSULE	400 mg	ORAL	ANDA	21 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-010	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50268-050	CAPSULE	200 mg	ORAL	ANDA	13 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51407-666	CAPSULE	200 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51407-667	CAPSULE	400 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53746-669	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53746-669	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53746-670	CAPSULE	400 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53746-670	CAPSULE	400 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4216	CAPSULE	400 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5520	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62559-255	CAPSULE	200 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62559-255	CAPSULE	200 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62559-256	CAPSULE	400 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62559-256	CAPSULE	400 mg	ORAL	ANDA	23 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	65162-669	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	65162-669	CAPSULE	200 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	65162-670	CAPSULE	400 mg	ORAL	ANDA	14 sections
Acebutolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	65162-670	CAPSULE	400 mg	ORAL	ANDA	14 sections
SECTRAL	HUMAN PRESCRIPTION DRUG LABEL	1	67857-700	CAPSULE	200 mg	ORAL	NDA	26 sections
SECTRAL	HUMAN PRESCRIPTION DRUG LABEL	1	67857-701	CAPSULE	400 mg	ORAL	NDA	26 sections