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

Stem definition	Drug id	CAS RN
diazepam derivatives	1102	40054-69-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: Y 7131 etizolam depas AHR-3219 Y-7131	Molecular weight: 342.85 Formula: C17H15ClN4S CLOGP: 3.02 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 43.07 ALOGS: -3.91 ROTB: 2

Molecule

Description

Molfile Inchi Smiles

Synonyms:

Y 7131
etizolam
depas
AHR-3219
Y-7131

Molecular weight: 342.85
Formula: C17H15ClN4S
CLOGP: 3.02
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 43.07
ALOGS: -3.91
ROTB: 2

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.30 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1984	YEAR INTRODUCED

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
Toxicity to various agents	115.97	23.12	115	4570	247135	63237202
Hepatic function abnormal	89.52	23.12	47	4638	37095	63447242
Altered state of consciousness	78.61	23.12	38	4647	25192	63459145
Drug abuse	76.43	23.12	54	4631	72464	63411873
Intentional overdose	70.79	23.12	52	4633	74100	63410237
Distributive shock	65.01	23.12	16	4669	1367	63482970
Spinal compression fracture	61.69	23.12	27	4658	14256	63470081
Neutrophil count decreased	50.32	23.12	38	4647	56368	63427969
Cardiac failure	48.27	23.12	45	4640	89097	63395240
Suicide attempt	47.73	23.12	38	4647	60880	63423457

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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
Toxicity to various agents	627.25	21.86	342	3553	200020	34753016
Respiratory depression	244.90	21.86	85	3810	16160	34936876
Drug abuse	223.67	21.86	138	3757	98958	34854078
Pulmonary oedema	140.50	21.86	79	3816	47450	34905586
Pulmonary congestion	69.93	21.86	33	3862	13732	34939304
Alcohol interaction	66.95	21.86	21	3874	2892	34950144
Drug interaction	66.65	21.86	102	3793	225844	34727192
Brain oedema	57.77	21.86	29	3866	13792	34939244
Counterfeit product administered	52.43	21.86	10	3885	165	34952871
Interstitial lung disease	42.64	21.86	44	3851	65238	34887798

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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
Toxicity to various agents	605.66	19.71	442	8425	421098	79314423
Drug abuse	269.50	19.71	187	8680	162504	79573017
Respiratory depression	210.71	19.71	88	8779	27542	79707979
Hepatic function abnormal	113.65	19.71	81	8786	73026	79662495
Pulmonary oedema	95.86	19.71	79	8788	88175	79647346
Altered state of consciousness	80.90	19.71	54	8813	43768	79691753
Alcohol interaction	79.11	19.71	27	8840	4847	79730674
Interstitial lung disease	68.43	19.71	73	8794	112527	79622994
Intentional overdose	64.93	19.71	69	8798	105891	79629630
Spinal compression fracture	60.54	19.71	32	8835	16926	79718595

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05BA19	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents

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

Disease	Relation	SNOMED_ID	DOID
Anxiety	indication	48694002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.64	Basic
pKa2	4.89	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	Type	Activity value (-log[M])	Bioact source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	EC50	8.10	WOMBAT-PK
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN			WOMBAT-PK
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN			WOMBAT-PK
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN			WOMBAT-PK

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External reference:

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ID	Source
008161	NDDF
1163197005	SNOMEDCT_US
1173020002	SNOMEDCT_US
3307	PUBCHEM_CID
4563	INN_ID
A76XI0HL37	UNII
C0059862	UMLSCUI
C044610	MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:31583	CHEBI
CHEMBL1289779	ChEMBL_ID

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Pharmaceutical products:

None