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:

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Property	Value	Reference
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
t_half (Half-life)	3.50 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	10 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.74 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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

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
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

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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
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

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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
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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
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
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
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

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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	9.19	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		Ki	6.40	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5	CHEMBL

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External reference:

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ID	Source
001858	NDDF
004742	NDDF
142130	RXNORM
1978	PUBCHEM_CID
3295	INN_ID
34381-68-5	SECONDARY_CAS_RN
3597005	SNOMEDCT_US
372815001	SNOMEDCT_US
4018063	VUID
4018063	VANDF

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Pharmaceutical products:

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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

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