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:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	4 %	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
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Dec. 26, 1990	FDA	ABBOTT

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
Serotonin syndrome	54.58	24.29	25	2203	24688	50578208
Electrocardiogram QT prolonged	47.14	24.29	29	2199	51857	50551039
Intentional overdose	39.85	24.29	28	2200	62476	50540420
Disseminated intravascular coagulation	36.77	24.29	17	2211	17118	50585778
Drug interaction	35.94	24.29	44	2184	199577	50403319
Ventricular arrhythmia	32.46	24.29	10	2218	3299	50599597
Electrocardiogram QRS complex prolonged	31.56	24.29	11	2217	5333	50597563
Bradycardia	30.19	24.29	24	2204	64402	50538494
Suicide attempt	28.01	24.29	21	2207	51711	50551185
Rhabdomyolysis	26.06	24.29	18	2210	39009	50563887
Poverty of speech	24.36	24.29	5	2223	316	50602580

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
Hyperammonaemia	30.79	23.02	11	1310	5652	29567554
Inappropriate antidiuretic hormone secretion	30.21	23.02	13	1308	10919	29562287
Altered state of consciousness	28.36	23.02	15	1306	19874	29553332
Delirium	28.08	23.02	19	1302	39378	29533828

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
Delirium	45.68	20.75	35	3619	69159	64425919
Drug interaction	40.56	20.75	73	3581	362010	64133068
Electrocardiogram QT prolonged	37.36	20.75	33	3621	79415	64415663
Altered state of consciousness	36.15	20.75	24	3630	37878	64457200
Intentional overdose	35.74	20.75	34	3620	89910	64405168
Persecutory delusion	31.53	20.75	11	3643	4147	64490931
Serotonin syndrome	30.68	20.75	22	3632	39260	64455818
Rhabdomyolysis	29.65	20.75	31	3623	91695	64403383
Inappropriate antidiuretic hormone secretion	28.50	20.75	17	3637	22272	64472806
Suicide attempt	26.61	20.75	26	3628	70981	64424097
Disseminated intravascular coagulation	24.99	20.75	18	3636	32330	64462748
Hepatic function abnormal	23.07	20.75	23	3631	64290	64430788
Electrocardiogram QRS complex prolonged	23.03	20.75	11	3643	9233	64485845
Hyperammonaemia	22.31	20.75	11	3643	9893	64485185
Ventricular arrhythmia	22.13	20.75	10	3644	7405	64487673
Neuroleptic malignant syndrome	21.84	20.75	15	3639	24981	64470097

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CD04	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives
FDA CS	M0002356	Benzodiazepines
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:50268	GABA modulators
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents
FDA EPC	N0000175694	Benzodiazepine

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

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
Severe chronic obstructive pulmonary disease	contraindication	313299006
Breastfeeding (mother)	contraindication	413712001

🐶 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:

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

External reference:

ID	Source
4019566	VUID
N0000147666	NUI
D00311	KEGG_DRUG
4019566	VANDF
C0014892	UMLSCUI
CHEBI:4858	CHEBI
CHEMBL285674	ChEMBL_ID
DB01215	DRUGBANK_ID
D004949	MESH_DESCRIPTOR_UI
3261	PUBCHEM_CID
7550	IUPHAR_LIGAND_ID
3611	INN_ID
36S3EQV54C	UNII
4077	RXNORM
10202	MMSL
4682	MMSL
d00915	MMSL
003566	NDDF
371364001	SNOMEDCT_US
96235001	SNOMEDCT_US

Pharmaceutical products:

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	0591-0745	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	51862-074	TABLET	2 mg	ORAL	ANDA	33 sections
Estazolam	Human Prescription Drug Label	1	70954-480	TABLET	1 mg	ORAL	ANDA	27 sections
Estazolam	Human Prescription Drug Label	1	70954-481	TABLET	2 mg	ORAL	ANDA	27 sections