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:

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

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1984	YEAR INTRODUCED

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
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
Platelet count decreased	46.95	23.12	50	4635	116072	63368265
Fatigue	39.01	23.12	9	4676	888019	62596318
Pemphigoid	38.73	23.12	16	4669	7328	63477009
Drug ineffective	37.96	23.12	15	4670	1044750	62439587
Anaemia	37.66	23.12	73	4612	293357	63190980
Haemorrhage subcutaneous	36.22	23.12	12	4673	2971	63481366
Renal impairment	35.61	23.12	38	4647	88317	63396020
Interstitial lung disease	33.00	23.12	31	4654	61877	63422460
Hypokalaemia	32.24	23.12	39	4646	103765	63380572
Overdose	32.16	23.12	41	4644	115037	63369300
Cerebral infarction	30.37	23.12	20	4665	23873	63460464
Needle track marks	28.04	23.12	4	4681	14	63484323
Disseminated intravascular coagulation	26.81	23.12	17	4668	19034	63465303
Counterfeit product administered	25.39	23.12	4	4681	31	63484306
Vasoplegia syndrome	25.38	23.12	8	4677	1691	63482646
Osteonecrosis of jaw	23.49	23.12	20	4665	35103	63449234
Accidental poisoning	23.23	23.12	6	4679	622	63483715

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
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
Hepatic function abnormal	40.55	21.86	36	3859	44327	34908709
Pneumonia aspiration	26.90	21.86	28	3867	41875	34911161
Left ventricular enlargement	24.54	21.86	7	3888	695	34952341
Product counterfeit	23.14	21.86	5	3890	157	34952879
Fatigue	22.03	21.86	7	3888	370646	34582390

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
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
Fatigue	57.96	19.71	16	8851	929711	78805810
Drug interaction	54.32	19.71	133	8734	415050	79320471
Suicide attempt	52.56	19.71	55	8812	82877	79652644
Pulmonary congestion	51.46	19.71	34	8833	27066	79708455
Cardiac failure	51.30	19.71	74	8793	154768	79580753
Counterfeit product administered	48.59	19.71	9	8858	126	79735395
Distributive shock	48.00	19.71	16	8851	2671	79732850
Pneumonia aspiration	45.29	19.71	46	8821	66921	79668600
Brain oedema	43.90	19.71	30	8837	25233	79710288
Neutrophil count decreased	43.62	19.71	53	8814	93906	79641615
Platelet count decreased	42.53	19.71	77	8790	194587	79540934
Drug ineffective	42.42	19.71	35	8832	1080878	78654643
Cerebral infarction	35.77	19.71	34	8833	45642	79689879
Pemphigoid	30.99	19.71	20	8847	15295	79720226
Renal impairment	30.20	19.71	59	8808	157724	79577797
Accidental poisoning	30.13	19.71	10	8857	1647	79733874
Haemorrhage subcutaneous	29.03	19.71	13	8854	4796	79730725
White blood cell count decreased	28.56	19.71	64	8803	188224	79547297
Pain	28.52	19.71	22	8845	703780	79031741
Delusion	28.00	19.71	21	8846	20402	79715119
Arthralgia	25.63	19.71	16	8851	571787	79163734
Restlessness	24.50	19.71	28	8839	46464	79689057
Left ventricular enlargement	24.13	19.71	7	8860	739	79734782
Blood creatine phosphokinase increased	23.95	19.71	33	8834	66057	79669464
Decreased appetite	23.94	19.71	88	8779	342330	79393191
Erythema multiforme	23.87	19.71	18	8849	17633	79717888
Drug hypersensitivity	23.07	19.71	3	8864	298913	79436608
Overdose	22.93	19.71	58	8809	184148	79551373
Malignant neoplasm progression	22.63	19.71	48	8819	135942	79599579
Enterocolitis	22.33	19.71	16	8851	14496	79721025
Anaemia	22.16	19.71	103	8764	444912	79290609
Hypokalaemia	21.87	19.71	49	8818	143991	79591530
Pyelonephritis	21.58	19.71	18	8849	20370	79715151
Upper respiratory tract inflammation	21.49	19.71	10	8857	4025	79731496
Rhabdomyolysis	21.49	19.71	40	8827	103091	79632430
Drug withdrawal maintenance therapy	21.46	19.71	4	8863	58	79735463
Disseminated intravascular coagulation	21.32	19.71	23	8844	35819	79699702
Heat illness	21.30	19.71	6	8861	571	79734950
White blood cell count increased	20.89	19.71	33	8834	74600	79660921
Drug dependence	20.55	19.71	24	8843	40745	79694776
Urinary retention	20.10	19.71	28	8839	56602	79678919

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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:

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

External reference:

ID	Source
D01514	KEGG_DRUG
C0059862	UMLSCUI
CHEBI:31583	CHEBI
CHEMBL1289779	ChEMBL_ID
DB09166	DRUGBANK_ID
C044610	MESH_SUPPLEMENTAL_RECORD_UI
3307	PUBCHEM_CID
4563	INN_ID
A76XI0HL37	UNII
008161	NDDF
1163197005	SNOMEDCT_US
1173020002	SNOMEDCT_US
H4C	PDB_CHEM_ID

Pharmaceutical products:

None