trichlormethiazide 🐶 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 0.80 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

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 317.57 34.84 56 2583 1672 63484711
Reversible airways obstruction 313.99 34.84 56 2583 1786 63484597
Sputum culture positive 304.91 34.84 56 2583 2111 63484272
Bronchial secretion retention 291.12 34.84 56 2583 2717 63483666
Eosinophil count increased 219.50 34.84 57 2582 10871 63475512
Upper-airway cough syndrome 212.22 34.84 56 2583 11362 63475021
Multiple allergies 201.70 34.84 56 2583 13746 63472637
Obstructive airways disorder 191.95 34.84 59 2580 20640 63465743
Pulmonary mass 174.45 34.84 56 2583 22540 63463843
Full blood count abnormal 155.83 34.84 56 2583 31661 63454722
Respiratory tract infection 141.20 34.84 56 2583 41427 63444956
Sputum culture 64.64 34.84 11 2628 263 63486120
Renal impairment 64.30 34.84 42 2597 88313 63398070
Cough 54.93 34.84 64 2575 292679 63193704
Pneumonia 54.77 34.84 80 2559 456687 63029696
Cardiac failure 54.39 34.84 38 2601 89104 63397279

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 80.26 23.35 57 2064 94456 34860354
Cardiac failure 68.27 23.35 51 2070 91197 34863613
Hepatic function abnormal 52.62 23.35 33 2088 44330 34910480
Shoshin beriberi 43.76 23.35 7 2114 75 34954735
Cerebral infarction 41.81 23.35 24 2097 27431 34927379
Interstitial lung disease 34.86 23.35 30 2091 65252 34889558
Renal ischaemia 30.23 23.35 7 2114 562 34954248
Vitamin B1 deficiency 28.08 23.35 6 2115 333 34954477
Cardiac failure chronic 27.19 23.35 12 2109 7867 34946943
Decreased appetite 26.78 23.35 41 2080 166351 34788459
Hyperuricaemia 23.78 23.35 11 2110 8032 34946778

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
Vital capacity decreased 273.72 24.33 53 4878 1763 79737694
Reversible airways obstruction 264.15 24.33 53 4878 2123 79737334
Sputum culture positive 234.97 24.33 53 4878 3728 79735729
Bronchial secretion retention 230.64 24.33 53 4878 4051 79735406
Multiple allergies 181.45 24.33 53 4878 10407 79729050
Upper-airway cough syndrome 179.93 24.33 54 4877 11639 79727818
Eosinophil count increased 167.64 24.33 56 4875 17049 79722408
Obstructive airways disorder 137.78 24.33 57 4874 31402 79708055
Pulmonary mass 135.30 24.33 55 4876 28979 79710478
Renal impairment 134.01 24.33 96 4835 157687 79581770
Cardiac failure 117.41 24.33 88 4843 154754 79584703
Respiratory tract infection 116.90 24.33 58 4873 48631 79690826
Full blood count abnormal 111.57 24.33 53 4878 40421 79699036
Hepatic function abnormal 72.50 24.33 49 4882 73058 79666399
Cerebral infarction 56.03 24.33 35 4896 45641 79693816
Sputum culture 49.23 24.33 9 4922 217 79739240
Pneumonia 44.44 24.33 114 4817 660132 79079325
Shoshin beriberi 43.62 24.33 7 4924 75 79739382
Interstitial lung disease 40.57 24.33 42 4889 112558 79626899
Hyperuricaemia 40.46 24.33 18 4913 11781 79727676
Fatigue 33.96 24.33 8 4923 929719 78809738
Vitamin B1 deficiency 33.83 24.33 8 4923 690 79738767
Decreased appetite 31.57 24.33 67 4864 342351 79397106
Right ventricular failure 31.33 24.33 19 4912 23478 79715979
Blood pressure decreased 30.36 24.33 34 4897 99432 79640025
Uraemic encephalopathy 28.78 24.33 7 4924 680 79738777
Platelet count decreased 27.83 24.33 46 4885 194618 79544839
Upper respiratory tract inflammation 27.17 24.33 10 4921 4025 79735432
Cardiac failure chronic 25.90 24.33 13 4918 11122 79728335
Pain 25.78 24.33 6 4925 703796 79035661
Renal ischaemia 25.13 24.33 7 4924 1155 79738302

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




🐶 Veterinary Drug Use

SpeciesUseRelation
Cattle No Use Class Stated Or Implied Indication

🐶 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