etizolam

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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
BA (Bioavailability)	93 %

Property	Description	Value
kinase-safety-class	ACVR2B,AXL,BRAF,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK4,PIK3CG,PRKDC	12
kinase-selectivity-class	GRK2	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

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	239.71	22.55	172	5375	287674	90335226
Hepatic function abnormal	132.47	22.55	62	5485	46226	90576674
Altered state of consciousness	131.43	22.55	55	5492	31477	90591423
Drug abuse	98.94	22.55	62	5485	82285	90540615
Overdose	92.96	22.55	77	5470	157632	90465268
Intentional overdose	89.15	22.55	61	5486	93773	90529127
Renal impairment	65.26	22.55	53	5494	105368	90517532
Spinal compression fracture	64.97	22.55	27	5520	15151	90607749
Distributive shock	57.97	22.55	17	5530	3407	90619493
Cardiac failure	53.36	22.55	48	5499	109448	90513452
Platelet count decreased	53.30	22.55	53	5494	136916	90485984
Suicide attempt	51.11	22.55	40	5507	75359	90547541
Neutrophil count decreased	50.78	22.55	39	5508	71493	90551407
Vasoconstriction	42.25	22.55	10	5537	875	90622025
Anaemia	41.50	22.55	76	5471	352726	90270174
Fatigue	41.42	22.55	10	5537	1154013	89468887
Interstitial lung disease	40.21	22.55	35	5512	76370	90546530
Pemphigoid	38.43	22.55	16	5531	9010	90613890
Haemorrhage subcutaneous	36.89	22.55	12	5535	3384	90619516
Disseminated intravascular coagulation	35.74	22.55	20	5527	21518	90601382
Drug ineffective	34.80	22.55	21	5526	1384277	89238623
Cerebral infarction	34.36	22.55	21	5526	26575	90596325
Hypokalaemia	29.20	22.55	38	5509	131078	90491822
Delusion	28.98	22.55	15	5532	13825	90609075
Needle track marks	28.79	22.55	4	5543	14	90622886
Counterfeit product administered	28.44	22.55	5	5542	97	90622803
Pneumonia aspiration	28.33	22.55	22	5525	40918	90581982
Decorticate posture	27.92	22.55	6	5541	339	90622561
Blood pressure decreased	27.30	22.55	28	5519	74867	90548033
Urinary retention	25.51	22.55	20	5527	37724	90585176
Pain	25.14	22.55	15	5532	996326	89626574
Osteonecrosis of jaw	24.88	22.55	20	5527	39083	90583817
Shock	23.32	22.55	17	5530	28761	90594139
Colitis microscopic	23.09	22.55	12	5535	11147	90611753
Pyelonephritis	22.95	22.55	15	5532	21301	90601599
Vasoplegia syndrome	22.89	22.55	8	5539	2806	90620094

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	1092.53	24.32	516	4184	228620	42388015
Drug abuse	263.85	24.32	156	4544	104615	42512020
Respiratory depression	233.17	24.32	85	4615	18783	42597852
Pulmonary oedema	132.76	24.32	79	4621	53193	42563442
Overdose	88.49	24.32	81	4619	105183	42511452
Alcohol interaction	78.11	24.32	22	4678	2113	42614522
Pulmonary congestion	66.05	24.32	33	4667	15697	42600938
Drug interaction	63.79	24.32	109	4591	266890	42349745
Electrocardiogram J wave	57.78	24.32	9	4691	40	42616595
Antemortem blood drug level abnormal	54.07	24.32	9	4691	65	42616570
Hepatic function abnormal	53.94	24.32	45	4655	51522	42565113
Brain oedema	53.48	24.32	29	4671	16298	42600337
Counterfeit product administered	47.36	24.32	10	4690	284	42616351
Interstitial lung disease	46.55	24.32	50	4650	78412	42538223
Accidental poisoning	41.32	24.32	12	4688	1284	42615351
Postmortem blood drug level abnormal	39.28	24.32	9	4691	375	42616260
Pneumonia aspiration	29.82	24.32	32	4668	50046	42566589
Drug level above therapeutic	29.62	24.32	14	4686	5892	42610743
Depressed level of consciousness	27.42	24.32	30	4670	47940	42568695

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	1169.34	19.55	660	9808	479895	110098936
Drug abuse	334.00	19.55	208	10260	177203	110401628
Respiratory depression	215.24	19.55	89	10379	31912	110546919
Hepatic function abnormal	165.92	19.55	104	10364	89191	110489640
Overdose	144.78	19.55	142	10326	233652	110345179
Altered state of consciousness	124.64	19.55	74	10394	57552	110521279
Pulmonary oedema	102.13	19.55	81	10387	100578	110478253
Alcohol interaction	95.11	19.55	28	10440	3666	110575165
Intentional overdose	92.37	19.55	86	10382	132415	110446416
Interstitial lung disease	81.26	19.55	82	10386	139252	110439579
Spinal compression fracture	62.95	19.55	32	10436	18360	110560471
Fatigue	62.32	19.55	19	10449	1215939	109362892
Drug interaction	61.74	19.55	142	10326	500041	110078790
Pneumonia aspiration	57.10	19.55	53	10415	81180	110497651
Suicide attempt	56.90	19.55	59	10409	103335	110475496
Accidental poisoning	56.00	19.55	17	10451	2470	110576361
Cardiac failure	55.36	19.55	78	10390	187548	110391283
Antemortem blood drug level abnormal	54.85	19.55	9	10459	70	110578761
Electrocardiogram J wave	53.00	19.55	9	10459	88	110578743
Pulmonary congestion	52.31	19.55	34	10434	30932	110547899
Renal impairment	52.16	19.55	76	10392	188369	110390462
Drug ineffective	50.70	19.55	42	10426	1520498	109058333
Counterfeit product administered	49.47	19.55	10	10458	267	110578564
Platelet count decreased	48.57	19.55	82	10386	230361	110348470
Neutrophil count decreased	44.45	19.55	56	10412	120885	110457946
Cerebral infarction	42.71	19.55	37	10431	51801	110527030
Brain oedema	42.63	19.55	30	10438	31068	110547763
Distributive shock	41.63	19.55	17	10451	5887	110572944
Pain	36.13	19.55	23	10445	954932	109623899
Postmortem blood drug level abnormal	36.07	19.55	9	10459	631	110578200
Vasoconstriction	35.67	19.55	10	10458	1100	110577731
Depressed level of consciousness	35.07	19.55	48	10420	112230	110466601
Delusion	32.75	19.55	23	10445	23732	110555099
Loss of consciousness	32.60	19.55	63	10405	196243	110382588
Drug hypersensitivity	32.07	19.55	3	10465	454087	110124744
Arthralgia	30.55	19.55	18	10450	779614	109799217
Blood creatine phosphokinase increased	30.34	19.55	36	10432	73041	110505790
White blood cell count decreased	30.31	19.55	67	10401	229323	110349508
Pemphigoid	29.33	19.55	20	10448	19687	110559144
Haemorrhage subcutaneous	29.27	19.55	13	10455	5526	110573305
Disseminated intravascular coagulation	29.12	19.55	27	10441	41259	110537572
Rhabdomyolysis	28.25	19.55	45	10423	120356	110458475
Hypersensitivity	27.67	19.55	3	10465	403995	110174836
Urinary retention	26.76	19.55	33	10435	69650	110509181
Decreased appetite	25.75	19.55	101	10367	475745	110103086
Heat illness	24.83	19.55	7	10461	785	110578046
Left ventricular enlargement	24.18	19.55	7	10461	864	110577967
Restlessness	23.82	19.55	28	10440	56231	110522600
Erythema multiforme	23.59	19.55	18	10450	21079	110557752
Anaemia	23.32	19.55	108	10360	546978	110031853
Swelling	23.06	19.55	3	10465	351038	110227793
Drug dependence	23.04	19.55	26	10442	49994	110528837
Enterocolitis	23.04	19.55	17	10451	18932	110559899
Blood pressure decreased	22.96	19.55	40	10428	115051	110463780
Pyelonephritis	22.79	19.55	19	10449	25231	110553600
Drug level above therapeutic	22.76	19.55	14	10454	11574	110567257
Sinus arrest	22.56	19.55	10	10458	4232	110574599
Malignant neoplasm progression	21.94	19.55	50	10418	174517	110404314
Product dose omission issue	20.54	19.55	3	10465	321779	110257052
Blood lactate dehydrogenase increased	20.34	19.55	23	10445	44311	110534520
Cardiogenic shock	20.18	19.55	26	10442	57312	110521519
White blood cell count increased	19.76	19.55	34	10434	96808	110482023
Delirium	19.61	19.55	41	10427	134984	110443847

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etizolam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

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
CHEBI has role	CHEBI:35474	anxiolytic drug

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

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

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.64	Basic
pKa2	4.89	Basic