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2022 Update-Veterinary Drugs & Uses
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L1000
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DrugCentral 2023 ๐
2022 Update-Veterinary Drugs & Uses
Search
Structure ๐
Similarity ๐
Smart API
Redial
About
Download
L1000
FAQ
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All
FDA-approved
EMA-approved
PMDA-approved
Target Card Uniprot Example:
P23975
nitrazepam ๐ถ
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
Drug dosage:
Dose
Unit
Route
5
mg
O
ADMET properties:
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Property
Value
Reference
BA (Bioavailability)
78 %
Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)
26 hours
Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)
2
Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)
1.70 L/kg
Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)
1.02 ยตM/kg/day
Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)
0.86 mL/min/kg
Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)
0.50 %
Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)
0.13 %
Lombardo F, Berellini G, Obach RS
S (Water solubility)
0.03 mg/mL
Benet LZ, Broccatelli F, Oprea TI
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Approvals:
None
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
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
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6
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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
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
Showing 1 to 10 of 46 entries
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1
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3
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5
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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
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
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3
4
5
โฆ
9
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FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
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Source
Code
Description
ATC
N05CD02
NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
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
MeSH PA
D014151
Anti-Anxiety Agents
MeSH PA
D000927
Anticonvulsants
MeSH PA
D002491
Central Nervous System Agents
MeSH PA
D002492
Central Nervous System Depressants
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Drug Use
| Suggest Off label Use Form|
|View source of the data|
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Disease
Relation
SNOMED_ID
DOID
Myoclonic seizure
indication
37356005
Insomnia
indication
193462001
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๐ถ Veterinary Drug Use
None
๐ถ Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
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Dissociation level
Dissociation constant
Type (acidic/basic)
pKa1
11.11
acidic
pKa2
2.85
Basic
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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
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
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External reference:
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ID
Source
003484
NDDF
152070
RXNORM
2121
INN_ID
387449001
SNOMEDCT_US
4506
PUBCHEM_CID
78449007
SNOMEDCT_US
9CLV70W7HS
UNII
C0028126
UMLSCUI
CHEBI:7581
CHEBI
CHEMBL13209
ChEMBL_ID
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Pharmaceutical products:
None
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L1000
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nitrazepam