nizatidine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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) 21.65 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 61 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.08 ┬ÁM/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

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 31.85 20.28 18 1369 40853 46643822

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 50.85 26.42 8 736 199 29951535
Catheter site cellulitis 31.06 26.42 5 739 144 29951590

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
FDA EPC N0000175784 Histamine-2 Receptor Antagonist
MeSH PA D000897 Anti-Ulcer Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006635 Histamine H2 Antagonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:37961 h2-receptor blockers
CHEBI has role CHEBI:38323 cholinergic drugs
CHEBI has role CHEBI:49201 anti-ulcer agents

Drug Use (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

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
CHEMBL653 ChEMBL_ID
CHEMBL3183075 ChEMBL_ID
D016567 MESH_DESCRIPTOR_UI
DB00585 DRUGBANK_ID
7248 IUPHAR_LIGAND_ID
5194 INN_ID
P41PML4GHR UNII
4513 PUBCHEM_CID
42319 RXNORM
44069 MMSL
5184 MMSL
d00322 MMSL
003418 NDDF
108664005 SNOMEDCT_US
386887009 SNOMEDCT_US

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 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 63187-249 CAPSULE 150 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 63629-2769 CAPSULE 300 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 65162-659 SOLUTION 15 mg ORAL ANDA 11 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68071-1633 CAPSULE 150 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68071-5043 CAPSULE 150 mg ORAL ANDA 10 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
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68462-425 CAPSULE 150 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 68462-426 CAPSULE 300 mg ORAL ANDA 21 sections
Nizatidine HUMAN PRESCRIPTION DRUG LABEL 1 71335-0086 CAPSULE 150 mg ORAL ANDA 21 sections