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

Stem definition	Drug id	CAS RN
diazepam derivatives	1945	146-22-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nitrazadon nitrazepam neozepam nitrodiazepam	A benzodiazepine derivative used as an anticonvulsant and hypnotic. Molecular weight: 281.27 Formula: C15H11N3O3 CLOGP: 2.32 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 87.28 ALOGS: -3.97 ROTB: 2

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nitrazadon
nitrazepam
neozepam
nitrodiazepam

A benzodiazepine derivative used as an anticonvulsant and hypnotic.

Molecular weight: 281.27
Formula: C15H11N3O3
CLOGP: 2.32
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 87.28
ALOGS: -3.97
ROTB: 2

Drug dosage:

Dose	Unit	Route
5	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.03 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.02 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	78 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.86 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	26 hours	Lombardo F, Berellini G, Obach RS

Approvals:

None

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
Enthesopathy	414.25	29.65	118	9607	8496	63470801
Tongue disorder	364.65	29.65	112	9613	10468	63468829
Tenosynovitis	363.51	29.65	119	9606	13676	63465621
Blood parathyroid hormone decreased	355.98	29.65	108	9617	9683	63469614
Panniculitis	339.94	29.65	108	9617	11277	63468020
Skin necrosis	322.32	29.65	109	9616	13841	63465456
Granuloma skin	315	29.65	95	9630	8342	63470955
Rheumatoid nodule	300.26	29.65	109	9616	17046	63462251
Red blood cell sedimentation rate	300.03	29.65	81	9644	4773	63474524
Tendonitis	289.63	29.65	110	9615	19505	63459792
Ulcer	259.17	29.65	110	9615	25997	63453300
Drug eruption	255.65	29.65	112	9613	28582	63450715
Hypercalcaemia	247.31	29.65	109	9616	28213	63451084
Basal cell carcinoma	242.06	29.65	107	9618	27884	63451413
Skin ulcer	206.73	29.65	110	9615	42935	63436362
C-reactive protein abnormal	205.19	29.65	112	9613	45984	63433313
Alanine aminotransferase abnormal	177.93	29.65	53	9672	4451	63474846
Rash pruritic	170.62	29.65	109	9616	59690	63419607
Red blood cell sedimentation rate increased	168.87	29.65	97	9628	43885	63435412
Fear of injection	153.74	29.65	53	9672	7111	63472186
Aspartate aminotransferase increased	151.54	29.65	119	9606	90158	63389139
Inflammation	139.25	29.65	109	9616	82164	63397133
Drug tolerance decreased	138.86	29.65	63	9662	17410	63461887
Alanine aminotransferase increased	137.01	29.65	119	9606	103651	63375646
Psoriatic arthropathy	133.18	29.65	111	9614	91409	63387888
Loss of personal independence in daily activities	131.32	29.65	113	9612	97177	63382120
C-reactive protein increased	109.88	29.65	101	9624	94606	63384691
Drug tolerance	95.43	29.65	37	9688	6912	63472385
Granuloma	94.76	29.65	35	9690	5726	63473571
Rheumatoid lung	84.61	29.65	29	9696	3819	63475478
Joint injury	82.01	29.65	53	9672	29519	63449778
Erythema	79.31	29.65	115	9610	175636	63303661
Chest discomfort	77.94	29.65	90	9635	109879	63369418
Musculoskeletal disorder	77.75	29.65	45	9680	20599	63458698
Blood pressure systolic increased	72.01	29.65	59	9666	47338	63431959
Synovitis	68.39	29.65	111	9614	186807	63292490
Therapy non-responder	58.65	29.65	65	9660	75836	63403461
Osteomyelitis	51.73	29.65	38	9687	25982	63453315
Therapeutic response decreased	51.55	29.65	55	9670	61470	63417827
Overdose	49.95	29.65	74	9651	115004	63364293
Suicide attempt	48.49	29.65	53	9672	60865	63418432
Gastric disorder	47.50	29.65	42	9683	37327	63441970
Rheumatoid arthritis	45.66	29.65	112	9613	253707	63225590
Therapeutic product effect incomplete	45.32	29.65	74	9651	124982	63354315
Angioplasty	44.81	29.65	14	9711	1378	63477919
Infusion related reaction	41.69	29.65	106	9619	245415	63233882
Peripheral swelling	40.26	29.65	110	9615	265832	63213465
Retinal vein occlusion	38.88	29.65	14	9711	2129	63477168
Drug hypersensitivity	37.92	29.65	119	9606	310568	63168729
Blood creatinine increased	37.40	29.65	56	9669	87788	63391509
Product use issue	37.21	29.65	95	9630	220425	63258872
Intellectual disability	35.28	29.65	11	9714	1075	63478222
Peripheral vascular disorder	33.44	29.65	17	9708	6018	63473279
Limb injury	33.10	29.65	29	9696	25448	63453849
Musculoskeletal stiffness	32.66	29.65	81	9644	184537	63294760
Drug intolerance	31.22	29.65	111	9614	308550	63170747
Contraindicated product administered	30.91	29.65	88	9637	217560	63261737
Choking	30.60	29.65	19	9706	9860	63469437

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
Tenosynovitis	299.95	24.37	82	5966	4488	34946395
Enthesopathy	299.19	24.37	82	5966	4531	34946352
Tongue disorder	260.56	24.37	76	5972	5263	34945620
C-reactive protein abnormal	227.88	24.37	77	5971	8633	34942250
Synovitis	209.38	24.37	82	5966	13984	34936899
Alanine aminotransferase abnormal	186.46	24.37	57	5991	4631	34946252
Tendonitis	185.95	24.37	67	5981	9073	34941810
Psoriatic arthropathy	133.01	24.37	66	5982	19732	34931151
Loss of personal independence in daily activities	123.89	24.37	75	5973	33104	34917779
Treatment failure	114.24	24.37	81	5967	46616	34904267
Red blood cell sedimentation rate	100.11	24.37	26	6022	1162	34949721
Aspartate aminotransferase increased	99.55	24.37	87	5961	67696	34883187
Granuloma skin	98.20	24.37	26	6022	1253	34949630
Drug hypersensitivity	94.20	24.37	91	5957	80438	34870445
Blood parathyroid hormone decreased	89.84	24.37	25	6023	1455	34949428
Panniculitis	86.78	24.37	26	6022	1968	34948915
Drug intolerance	82.52	24.37	74	5974	59496	34891387
Alanine aminotransferase increased	77.42	24.37	82	5966	80733	34870150
Rheumatoid nodule	76.79	24.37	26	6022	2921	34947962
Erythema	76.19	24.37	85	5963	88695	34862188
Skin necrosis	59.45	24.37	26	6022	5827	34945056
Contraindicated product administered	56.50	24.37	39	6009	21442	34929441
Ulcer	49.26	24.37	26	6022	8809	34942074
Suicide attempt	45.25	24.37	44	6004	39072	34911811
Intentional overdose	44.77	24.37	46	6002	43628	34907255
Drug eruption	42.85	24.37	32	6016	19866	34931017
C-reactive protein increased	41.61	24.37	49	5999	54049	34896834
Multiple-drug resistance	39.75	24.37	19	6029	5220	34945663
Therapy non-responder	39.70	24.37	41	6007	39105	34911778
Neuroleptic malignant syndrome	38.97	24.37	29	6019	17905	34932978
Headache	38.76	24.37	98	5950	200537	34750346
Cor pulmonale acute	38.14	24.37	9	6039	269	34950614
Mobility decreased	36.94	24.37	35	6013	30093	34920790
Altered state of consciousness	36.81	24.37	31	6017	22862	34928021
Hypercalcaemia	35.84	24.37	26	6022	15442	34935441
Hypersensitivity	35.36	24.37	48	6000	60987	34889896
Toxicity to various agents	34.73	24.37	94	5954	200268	34750615
Skin ulcer	31.49	24.37	28	6020	22188	34928695
Dyspnoea	31.46	24.37	13	6035	376769	34574114
Rheumatoid lung	31.34	24.37	10	6038	932	34949951
Procedural failure	31.00	24.37	6	6042	67	34950816
Basal cell carcinoma	30.33	24.37	26	6022	19632	34931251
Dystonia	26.89	24.37	19	6029	10826	34940057
Fear of injection	26.45	24.37	10	6038	1542	34949341
Renal tubular acidosis	25.83	24.37	11	6037	2308	34948575
Inflammation	25.77	24.37	28	6020	28267	34922616

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
Enthesopathy	620.59	24.55	181	14923	11427	79717857
Tenosynovitis	572.50	24.55	182	14922	15372	79713912
Tongue disorder	541.19	24.55	170	14934	13805	79715479
Tendonitis	426.98	24.55	163	14941	23667	79705617
Blood parathyroid hormone decreased	374.05	24.55	120	14984	10416	79718868
Panniculitis	359.07	24.55	121	14983	12250	79717034
Alanine aminotransferase abnormal	352.09	24.55	110	14994	8757	79720527
Granuloma skin	340.11	24.55	108	14996	9066	79720218
C-reactive protein abnormal	339.50	24.55	171	14933	48196	79681088
Red blood cell sedimentation rate	333.97	24.55	95	15009	5470	79723814
Rheumatoid nodule	322.10	24.55	122	14982	17316	79711968
Skin necrosis	317.76	24.55	122	14982	17965	79711319
Ulcer	261.46	24.55	123	14981	29849	79699435
Psoriatic arthropathy	243.85	24.55	163	14941	77836	79651448
Drug eruption	236.14	24.55	130	14974	43805	79685479
Hypercalcaemia	229.64	24.55	122	14982	38308	79690976
Basal cell carcinoma	227.15	24.55	120	14984	37255	79692029
Loss of personal independence in daily activities	216.74	24.55	169	14935	102411	79626873
Aspartate aminotransferase increased	207.22	24.55	187	14917	138454	79590830
Skin ulcer	195.74	24.55	124	14980	54026	79675258
Fear of injection	177.66	24.55	63	15041	7411	79721873
Alanine aminotransferase increased	172.92	24.55	182	14922	162388	79566896
Synovitis	169.74	24.55	174	14930	150560	79578724
Rash pruritic	159.92	24.55	122	14982	71507	79657777
Red blood cell sedimentation rate increased	138.64	24.55	94	15010	45848	79683436
Drug tolerance decreased	134.27	24.55	60	15044	12918	79716366
Inflammation	133.18	24.55	123	14981	93630	79635654
Erythema	128.03	24.55	183	14921	223107	79506177
C-reactive protein increased	122.30	24.55	136	14968	128891	79600393
Rheumatoid lung	113.24	24.55	39	15065	4206	79725078
Drug tolerance	112.33	24.55	47	15057	8628	79720656
Granuloma	107.59	24.55	45	15059	8252	79721032
Drug hypersensitivity	97.25	24.55	190	14914	298726	79430558
Therapy non-responder	93.86	24.55	101	15003	92204	79637080
Musculoskeletal disorder	92.46	24.55	55	15049	21393	79707891
Joint injury	91.87	24.55	63	15041	31272	79698012
Drug intolerance	89.69	24.55	171	14933	263948	79465336
Treatment failure	87.90	24.55	133	14971	170353	79558931
Contraindicated product administered	67.54	24.55	113	14991	157425	79571859
Gastric disorder	62.80	24.55	54	15050	37379	79691905
Blood pressure systolic increased	62.35	24.55	70	15034	66916	79662368
Rheumatoid arthritis	58.78	24.55	125	14979	208345	79520939
Osteomyelitis	56.33	24.55	48	15056	32817	79696467
Chest discomfort	51.30	24.55	93	15011	137951	79591333
Therapeutic product effect incomplete	47.11	24.55	91	15013	141554	79587730
Dyspnoea	47.10	24.55	56	15048	856969	78872315
Angioplasty	45.39	24.55	16	15088	1847	79727437
Infusion related reaction	45.27	24.55	120	14984	230117	79499167
Asthenia	43.99	24.55	21	15083	511668	79217616
Suicide attempt	43.10	24.55	65	15039	82867	79646417
Overdose	42.46	24.55	102	15002	184104	79545180
Peripheral swelling	40.88	24.55	128	14976	269489	79459795
Salivary hypersecretion	40.27	24.55	28	15076	14196	79715088
Musculoskeletal stiffness	39.36	24.55	96	15008	174912	79554372
Multiple-drug resistance	39.03	24.55	23	15081	8785	79720499
Therapeutic response decreased	38.50	24.55	55	15049	66798	79662486
Pain in extremity	37.95	24.55	11	15093	364527	79364757
Neuroleptic malignant syndrome	36.85	24.55	35	15069	27524	79701760
Altered state of consciousness	36.07	24.55	43	15061	43779	79685505
Limb injury	34.81	24.55	35	15069	29493	79699791
Mobility decreased	34.09	24.55	73	15031	122102	79607182
Choking	32.35	24.55	23	15081	12078	79717206
Product use issue	32.14	24.55	100	15004	209722	79519562
Intentional overdose	30.35	24.55	64	15040	105896	79623388
Retinal vein occlusion	30.06	24.55	14	15090	3309	79725975
Pneumonia aspiration	29.95	24.55	49	15055	66918	79662366
Procedural failure	29.20	24.55	6	15098	84	79729200
Cor pulmonale acute	29.15	24.55	9	15095	687	79728597
Peripheral vascular disorder	28.01	24.55	18	15086	8012	79721272
Arthritis	27.96	24.55	65	15039	114815	79614469
Psychiatric symptom	27.63	24.55	17	15087	7018	79722266
Vomiting	27.35	24.55	53	15051	665775	79063509
Rhabdomyolysis	26.92	24.55	60	15044	103071	79626213
Back pain	26.86	24.55	12	15092	304168	79425116
Anaemia	26.66	24.55	27	15077	444988	79284296
Product dose omission issue	26.63	24.55	7	15097	247530	79481754
Sinusitis	26.53	24.55	3	15101	195498	79533786
Dystonia	26.39	24.55	26	15078	21373	79707911
Headache	26.08	24.55	212	14892	653560	79075724
Pruritus	25.93	24.55	22	15082	394626	79334658
Chest pain	25.14	24.55	11	15093	282293	79446991
Pulmonary fibrosis	24.96	24.55	36	15068	44076	79685208

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CD02	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives
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	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:50268	GABA modulators
CHEBI has role	CHEBI:53784	antispasmodics

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

Disease	Relation	SNOMED_ID	DOID
Myoclonic seizure	indication	37356005
Insomnia	indication	193462001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.11	acidic
pKa2	2.85	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism 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	EC50	8		WOMBAT-PK	KEGG DRUG
GABA-A receptor; anion channel	Ion channel		GBRA1_BOVIN GBRB1_BOVIN GBRA2_BOVIN GBRA3_BOVIN GBRA4_BOVIN GBRG2_BOVIN		IC50	7.42		CHEMBL

External reference:

ID	Source
N0000166923	NUI
D00531	KEGG_DRUG
C0028126	UMLSCUI
CHEBI:7581	CHEBI
CHEMBL13209	ChEMBL_ID
DB01595	DRUGBANK_ID
D009567	MESH_DESCRIPTOR_UI
4506	PUBCHEM_CID
2121	INN_ID
9CLV70W7HS	UNII
152070	RXNORM
003484	NDDF
387449001	SNOMEDCT_US
78449007	SNOMEDCT_US

Pharmaceutical products:

None