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

Stem definitionDrug idCAS RN
histamine-H2-receptor antagonists, cimetidine derivatives 1955 76963-41-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nizatidine
  • naxidine
  • nizaxid
A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
  • Molecular weight: 331.45
  • Formula: C12H21N5O2S2
  • CLOGP: -0.16
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 83.33
  • ALOGS: -3.93
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 21.40 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 61 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.08 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 70 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.65 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.50 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.296 Moderate 0.70
caco2-efflux Caco-2 efflux ratio (BA/AB) 5.888 Moderate 0.70
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.783 10^-6 cm/s Moderate 0.70
dh-clint Dog hepatocyte intrinsic clearance 2.301 uL/min/10^6 cells Moderate 0.70
dppb Dog plasma protein binding (% unbound) 89.160 % Moderate 0.70
fcs-ppb Fetal calf serum protein binding (% unbound) 84.810 % Moderate 0.70
herg hERG pIC50 3.784 pIC50 Moderate 0.70
hh-clint Human hepatocyte intrinsic clearance 1.102 uL/min/10^6 cells Moderate 0.70
hlm-clint Human liver microsomal intrinsic clearance 3.304 uL/min/mg protein Moderate 0.70
hppb Human plasma protein binding (% unbound) 78.010 % Moderate 0.70
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK2,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IGF1R,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 56
kinase-selectivity-class AXL,CDK4,EIF2AK3,EPHB4,GRK2,MAPK7,STK33,TEK 8
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 2.477 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.164 Moderate 0.70
mh-clint Mouse hepatocyte intrinsic clearance 6.339 Moderate 0.70
mppb Mouse plasma protein binding (% unbound) 90.930 Moderate 0.70
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 2.529 Moderate 0.70
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 88.700 % Moderate 0.70
rat-kpuu-brain Rat brain Kpuu 0.030 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.317 uL/min/10^6 cells Moderate 0.70
rh-fuinc Rat hepatocyte fraction unbound in incubation 96.320 % Moderate 0.70
rppb Rat plasma protein binding (% unbound) 87.270 % Moderate 0.70
solubility-dd Solubility at pH 7.4 in DMSO 966.051 uM Moderate 0.70

Approvals:

DateAgencyCompanyOrphan
April 12, 1988 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Chronic kidney disease 36.53 21.33 18 1644 50173 90576612

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tonsillar ulcer 52.32 26.79 8 921 188 42620218
Catheter site cellulitis 31.48 26.79 5 924 151 42620255
Intestinal metaplasia 28.39 26.79 4 925 52 42620354

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tonsillar ulcer 45.28 22.31 8 2405 463 110586423
Platelet count decreased 30.56 22.31 31 2382 230412 110356474
Intestinal metaplasia 26.71 22.31 4 2409 81 110586805
Catheter site cellulitis 24.97 22.31 5 2408 569 110586317
Aortic valve disease mixed 24.69 22.31 4 2409 137 110586749
Hepatic function abnormal 24.02 22.31 18 2395 89277 110497609

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A02BA04 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
H2-receptor antagonists
FDA MoA N0000000151 Histamine H2 Receptor Antagonists
MeSH PA D000897 Anti-Ulcer Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006635 Histamine H2 Antagonists
MeSH PA D018377 Neurotransmitter Agents
FDA EPC N0000175784 Histamine-2 Receptor Antagonist
CHEBI has role CHEBI:37961 H<small><sub>2</sub></small>-receptor antagonist
CHEBI has role CHEBI:38323 cholinergic drug
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:55324 gastrointestinal drug

Related Drugs by ATC class:

A02BA H2-receptor antagonists 6 drugs
cimetidinefamotidinelafutidineniperotidineranitidineroxatidine acetate

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

DiseaseRelationSNOMED_IDDOID
Peptic ulcer indication 13200003 DOID:750
Heartburn indication 16331000
Erosive esophagitis indication 40719004
Duodenal ulcer disease indication 51868009 DOID:1724
Peptic reflux disease indication 57643001
Indigestion indication 162031009
Gastroesophageal reflux disease indication 235595009 DOID:8534
Gastric ulcer indication 397825006 DOID:10808
Maintenance of Healing Duodenal Ulcer indication
Upper gastrointestinal hemorrhage off-label use 37372002
Zollinger-Ellison syndrome off-label use 53132006 DOID:0050782
Multiple endocrine adenomas off-label use 60549007
Systemic mast cell disease off-label use 397016004 DOID:349
Gastric Hypersecretory Conditions off-label use
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Malignant tumor of stomach contraindication 363349007 DOID:10534




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.68 Basic
pKa2 6.01 Basic
pKa3 1.26 Basic
pKa4 0.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H2 receptor GPCR ANTAGONIST Kd 6.92 WOMBAT-PK CHEMBL
Acetylcholinesterase Enzyme IC50 5.25 DRUG MATRIX

External reference:

IDSource
4019342 VUID
N0000147517 NUI
D00440 KEGG_DRUG
4019342 VANDF
C0085154 UMLSCUI
CHEBI:7601 CHEBI
CHEMBL3183075 ChEMBL_ID
DB00585 DRUGBANK_ID
D016567 MESH_DESCRIPTOR_UI
4513 PUBCHEM_CID
7248 IUPHAR_LIGAND_ID
5194 INN_ID
P41PML4GHR UNII
42319 RXNORM
44069 MMSL
5184 MMSL
d00322 MMSL
003418 NDDF
108664005 SNOMEDCT_US
386887009 SNOMEDCT_US
P41PML4GHR INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 0591-3137 CAPSULE 150 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 0591-3138 CAPSULE 300 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 16590-741 CAPSULE 150 mg ORAL ANDA 9 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 21695-043 CAPSULE 300 mg ORAL ANDA 10 sections
nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 21695-375 CAPSULE 150 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 42254-093 CAPSULE 150 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 42806-299 CAPSULE 150 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 42806-300 CAPSULE 300 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 45865-374 CAPSULE 150 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 52959-824 CAPSULE 150 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 55111-310 CAPSULE 150 mg ORAL ANDA 23 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 55111-311 CAPSULE 300 mg ORAL ANDA 23 sections
NIZATIDINE HUMAN PRESCRIPTION DRUG LABEL 1 60846-301 SOLUTION 15 mg ORAL ANDA 11 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68151-0017 CAPSULE 150 mg ORAL ANDA 10 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68258-3006 CAPSULE 300 mg ORAL ANDA 19 sections