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

Stem definition	Drug id	CAS RN
diazepam derivatives	1056	29975-16-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: estazolam tasedan	A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. Molecular weight: 294.74 Formula: C16H11ClN4 CLOGP: 2.29 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 43.07 ALOGS: -3.84 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

estazolam
tasedan

A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.

Molecular weight: 294.74
Formula: C16H11ClN4
CLOGP: 2.29
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 43.07
ALOGS: -3.84
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
3	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	4 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.10 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 26, 1990	FDA	ABBOTT

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
Serotonin syndrome	53.71	22.56	25	2471	28657	63457869
Electrocardiogram QT prolonged	49.02	22.56	30	2466	59500	63427026
Drug interaction	41.62	22.56	48	2448	229083	63257443
Intentional overdose	38.39	22.56	28	2468	74124	63412402
Disseminated intravascular coagulation	36.88	22.56	17	2479	19034	63467492
Bradycardia	36.43	22.56	27	2469	73200	63413326
Ventricular arrhythmia	36.38	22.56	11	2485	3817	63482709
Procedural hypotension	33.19	22.56	8	2488	1182	63485344
Drug dependence	32.83	22.56	17	2479	24466	63462060
Electrocardiogram QRS complex prolonged	31.64	22.56	11	2485	5927	63480599

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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
Delirium	33.61	22.34	22	1511	43969	34911429
Hyperammonaemia	29.73	22.34	11	1522	6356	34949042
Altered state of consciousness	29.38	22.34	16	1517	22877	34932521
Inappropriate antidiuretic hormone secretion	28.51	22.34	13	1520	12740	34942658
Drug interaction	24.62	22.34	39	1494	225907	34729491

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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 interaction	50.73	19.12	83	4070	415100	79325135
Delirium	48.41	19.12	38	4115	84589	79655646
Altered state of consciousness	39.61	19.12	26	4127	43796	79696439
Electrocardiogram QT prolonged	38.04	19.12	34	4119	90352	79649883
Persecutory delusion	34.46	19.12	12	4141	4897	79735338
Intentional overdose	33.44	19.12	34	4119	105926	79634309
Rhabdomyolysis	30.57	19.12	32	4121	103099	79637136
Serotonin syndrome	29.65	19.12	22	4131	45005	79695230
Inappropriate antidiuretic hormone secretion	27.21	19.12	17	4136	26296	79713939
Suicide attempt	26.87	19.12	27	4126	82905	79657330

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05CD04	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:50268	GABA modulators
FDA CS	M0002356	Benzodiazepines
FDA EPC	N0000175694	Benzodiazepine
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants

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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
Severe Insomnia	indication
Alcohol intoxication	contraindication	25702006
Depressive disorder	contraindication	35489007
Substance abuse	contraindication	66214007
Psychotic disorder	contraindication	69322001
Sleep apnea	contraindication	73430006	DOID:0050847
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002

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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	5.82	Basic
pKa2	4.83	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	Bioact source	MoA source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN	POSITIVE ALLOSTERIC MODULATOR	WOMBAT-PK	CHEMBL

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External reference:

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ID	Source
003566	NDDF
10202	MMSL
3261	PUBCHEM_CID
3611	INN_ID
36S3EQV54C	UNII
371364001	SNOMEDCT_US
4019566	VUID
4019566	VANDF
4077	RXNORM
4682	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0744	TABLET	1 mg	ORAL	ANDA	16 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0744	TABLET	1 mg	ORAL	ANDA	16 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0745	TABLET	2 mg	ORAL	ANDA	16 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0745	TABLET	2 mg	ORAL	ANDA	16 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	21695-220	TABLET	2 mg	ORAL	ANDA	29 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	51862-069	TABLET	1 mg	ORAL	ANDA	33 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	51862-070	TABLET	2 mg	ORAL	ANDA	33 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	51862-073	TABLET	1 mg	ORAL	ANDA	33 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	51862-073	TABLET	1 mg	ORAL	ANDA	33 sections
Estazolam	HUMAN PRESCRIPTION DRUG LABEL	1	51862-073	TABLET	1 mg	ORAL	ANDA	33 sections

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