trichlormethiazide ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diuretics, chlorothiazide derivatives 2733 133-67-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • triclormetiazide
  • trichlormethiazide
  • hydrotrichlorothiazide
  • trichlormetazid
  • trichlormethiazid
  • trichloromethiazide
A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830)
  • Molecular weight: 380.64
  • Formula: C8H8Cl3N3O4S2
  • CLOGP: 0.88
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 118.36
  • ALOGS: -2.96
  • ROTB: 2

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4 mg O
4 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.18 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
March 9, 1960 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
Vital capacity decreased 151.94 33.14 27 1881 929 50602287
Reversible airways obstruction 150.19 33.14 27 1881 993 50602223
Sputum culture positive 141.39 33.14 27 1881 1387 50601829
Bronchial secretion retention 139.56 33.14 27 1881 1486 50601730
Eosinophil count increased 96.63 33.14 28 1880 8802 50594414
Multiple allergies 93.34 33.14 27 1881 8436 50594780
Upper-airway cough syndrome 93.06 33.14 27 1881 8523 50594693
Obstructive airways disorder 88.68 33.14 30 1878 15622 50587594
Pulmonary mass 72.30 33.14 27 1881 18678 50584538
Full blood count abnormal 66.45 33.14 27 1881 23361 50579855
Renal impairment 63.57 33.14 38 1870 75623 50527593
Cardiac failure 60.81 33.14 37 1871 76003 50527213
Respiratory tract infection 58.29 33.14 27 1881 31990 50571226

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
Renal impairment 80.57 25.24 53 1664 81280 29491530
Cardiac failure 58.12 25.24 43 1674 79244 29493566
Hepatic function abnormal 55.08 25.24 32 1685 39227 29533583
Shoshin beriberi 44.60 25.24 7 1710 69 29572741
Cerebral infarction 39.65 25.24 22 1695 24653 29548157
Renal ischaemia 30.94 25.24 7 1710 530 29572280
Interstitial lung disease 30.77 25.24 26 1691 57692 29515118
Vitamin B1 deficiency 29.87 25.24 6 1711 257 29572553

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
Renal impairment 131.41 24.33 88 3755 134929 64359960
Vital capacity decreased 124.39 24.33 25 3818 1047 64493842
Reversible airways obstruction 122.90 24.33 25 3818 1113 64493776
Cardiac failure 111.58 24.33 79 3764 132294 64362595
Bronchial secretion retention 103.04 24.33 25 3818 2502 64492387
Sputum culture positive 98.56 24.33 25 3818 3001 64491888
Multiple allergies 82.40 24.33 25 3818 5789 64489100
Hepatic function abnormal 72.39 24.33 46 3797 64267 64430622
Upper-airway cough syndrome 72.30 24.33 25 3818 8745 64486144
Eosinophil count increased 71.09 24.33 28 3815 14084 64480805
Obstructive airways disorder 60.76 24.33 29 3814 23156 64471733
Cerebral infarction 55.44 24.33 33 3810 41011 64453878
Pulmonary mass 53.83 24.33 27 3816 23989 64470900
Respiratory tract infection 45.18 24.33 28 3815 37379 64457510
Shoshin beriberi 44.41 24.33 7 3836 69 64494820
Full blood count abnormal 43.00 24.33 25 3818 29732 64465157
Hyperuricaemia 40.29 24.33 17 3826 10174 64484715
Interstitial lung disease 39.24 24.33 38 3805 97694 64397195
Fatigue 31.18 24.33 4 3839 748726 63746163
Platelet count decreased 29.89 24.33 43 3800 167668 64327221
Decreased appetite 28.52 24.33 56 3787 281233 64213656
Right ventricular failure 28.29 24.33 17 3826 21454 64473435
Renal ischaemia 25.88 24.33 7 3836 1076 64493813
Vitamin B1 deficiency 24.98 24.33 6 3837 574 64494315
Upper respiratory tract inflammation 24.42 24.33 9 3834 3773 64491116

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03AA06 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides, plain
ATC C03AB06 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides and potassium in combination
ATC C03EA02 CARDIOVASCULAR SYSTEM
DIURETICS
DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION
Low-ceiling diuretics and potassium-sparing agents
CHEBI has role CHEBI:35498 diuretics
CHEBI has role CHEBI:35674 antihypertensive drugs
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004232 Diuretics
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D045283 Natriuretic Agents
MeSH PA D049993 Sodium Chloride Symporter Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Suicidal thoughts contraindication 6471006
Peptic ulcer contraindication 13200003 DOID:750
Chronic disease of respiratory system contraindication 17097001
Electroconvulsive therapy contraindication 23835007
Depressive disorder contraindication 35489007
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Ulcerative colitis contraindication 64766004 DOID:8577
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:557
Calculus in biliary tract contraindication 266474003




๐Ÿถ Veterinary Drug Use

SpeciesUseRelation
Cattle No Use Class Stated Or Implied Indication

๐Ÿถ Veterinary products

ProductApplicantIngredients
Naquasone Bolus Intervet Inc. 2

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.05 acidic
pKa2 10.3 acidic
pKa3 1.29 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
Solute carrier family 12 member 3 Transporter INHIBITOR A2 7 WOMBAT-PK CHEMBL
Carbonic anhydrase 1 Enzyme Ki 6.46 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 6.35 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.06 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 6.51 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 6.12 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 6.87 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 8.10 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 5.61 CHEMBL
Carbonic anhydrase 14 Enzyme Ki 5.46 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 7.04 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 6.19 CHEMBL

External reference:

IDSource
4018612 VUID
N0000146925 NUI
D00658 KEGG_DRUG
4018612 VANDF
C0040899 UMLSCUI
CHEBI:9683 CHEBI
CHEMBL1054 ChEMBL_ID
DB01021 DRUGBANK_ID
D014237 MESH_DESCRIPTOR_UI
5560 PUBCHEM_CID
7314 IUPHAR_LIGAND_ID
1012 INN_ID
Q58C92TUN0 UNII
10772 RXNORM
3169 MMSL
5619 MMSL
d00646 MMSL
002300 NDDF
11473005 SNOMEDCT_US
409112007 SNOMEDCT_US

Pharmaceutical products:

None