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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	1054	81147-92-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: esmolol brevibloc esmolol hydrochloride esmolol HCl	a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages Molecular weight: 295.38 Formula: C16H25NO4 CLOGP: 1.72 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 67.79 ALOGS: -3.31 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

esmolol
brevibloc
esmolol hydrochloride
esmolol HCl

a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages

Molecular weight: 295.38
Formula: C16H25NO4
CLOGP: 1.72
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 67.79
ALOGS: -3.31
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2.50	g	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	290 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.68 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.59 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.15 hours	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 31, 1986	FDA	BAXTER HLTHCARE

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
Drug ineffective	84.87	69.19	72	523	1044693	62443734

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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
Drug ineffective	78.62	42.83	75	817	456676	34499363
Bradycardia	57.56	42.83	31	861	75387	34880652
Cardiac arrest	53.13	42.83	32	860	96127	34859912
Pulseless electrical activity	46.94	42.83	14	878	7197	34948842
Hypotension	46.59	42.83	41	851	221608	34734431

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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
Drug ineffective	129.43	42.88	125	1331	1080788	78662144
Cardiac arrest	83.96	42.88	47	1409	172049	79570883
Bradycardia	63.25	42.88	36	1420	135521	79607411
Neuromuscular block prolonged	52.82	42.88	10	1446	1020	79741912
Pulseless electrical activity	50.35	42.88	16	1440	14144	79728788
Hypotension	50.04	42.88	50	1406	440267	79302665

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AB09	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
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
MeSH PA	D058671	Adrenergic beta-1 Receptor Antagonists
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D018377	Neurotransmitter Agents

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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
Supraventricular tachycardia	indication	6456007
Atrial fibrillation	indication	49436004	DOID:0060224
Perioperative hypertension	indication	434711000124103
Perioperative Tachycardia	indication
Malignant essential hypertension	off-label use	78975002	DOID:10823
Dissection of aorta	off-label use	308546005
Acute coronary syndrome	off-label use	394659003
Hypertensive urgency	off-label use	443482000
Prevention of Hypertension in Pheochromocytoma	off-label use
Bronchospasm	contraindication	4386001

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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	6.90	IUPHAR	IUPHAR
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		Kd	5.20	CHEMBL
Beta-1 adrenergic receptor	GPCR		B0FL73_CAVPO		Kd	7	CHEMBL

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External reference:

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ID	Source
001861	NDDF
004745	NDDF
151448	RXNORM
35318005	SNOMEDCT_US
372847006	SNOMEDCT_US
3762	MMSL
4019349	VANDF
4019746	VUID
4019746	VANDF
4681	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9825	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9825	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9825	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-055	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-055	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-055	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-075	INJECTION	20 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-075	INJECTION	20 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-075	INJECTION	20 mg	INTRAVENOUS	NDA	25 sections
Brevibloc	HUMAN PRESCRIPTION DRUG LABEL	1	10019-115	INJECTION	10 mg	INTRAVENOUS	NDA	25 sections

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