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

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 226.99 33.26 40 2190 1248 56288589
Reversible airways obstruction 224.11 33.26 40 2190 1344 56288493
Sputum culture positive 214.99 33.26 40 2190 1699 56288138
Bronchial secretion retention 212.14 33.26 40 2190 1828 56288009
Eosinophil count increased 151.49 33.26 41 2189 9596 56280241
Upper-airway cough syndrome 147.64 33.26 40 2190 9398 56280439
Multiple allergies 143.43 33.26 40 2190 10456 56279381
Obstructive airways disorder 136.11 33.26 43 2187 17239 56272598
Pulmonary mass 117.10 33.26 40 2190 20430 56269407
Full blood count abnormal 107.06 33.26 40 2190 26422 56263415
Respiratory tract infection 95.04 33.26 40 2190 36031 56253806
Renal impairment 64.57 33.26 40 2190 80673 56209164
Cardiac failure 63.94 33.26 40 2190 82053 56207784
Sputum culture 41.60 33.26 7 2223 164 56289673
Pneumonia 38.10 33.26 62 2168 407036 55882801

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
Cardiac failure 82.72 26.37 56 1871 85897 31609520
Renal impairment 80.11 26.37 55 1872 86294 31609123
Hepatic function abnormal 54.82 26.37 33 1894 41189 31654228
Shoshin beriberi 43.75 26.37 7 1920 75 31695342
Cerebral infarction 40.31 26.37 23 1904 25954 31669463
Interstitial lung disease 32.31 26.37 28 1899 61375 31634042
Renal ischaemia 30.57 26.37 7 1920 534 31694883
Vitamin B1 deficiency 28.49 26.37 6 1921 310 31695107

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 193.42 25.06 38 4324 1371 70922711
Reversible airways obstruction 188.44 25.06 38 4324 1569 70922513
Bronchial secretion retention 164.68 25.06 38 4324 2972 70921110
Sputum culture positive 160.59 25.06 38 4324 3316 70920766
Cardiac failure 140.41 25.06 95 4267 143446 70780636
Renal impairment 133.04 25.06 92 4270 143845 70780237
Multiple allergies 128.98 25.06 38 4324 7722 70916360
Upper-airway cough syndrome 124.67 25.06 39 4323 9692 70914390
Eosinophil count increased 115.08 25.06 41 4321 15181 70908901
Obstructive airways disorder 96.88 25.06 42 4320 26071 70898011
Pulmonary mass 90.50 25.06 40 4322 25993 70898089
Respiratory tract infection 77.52 25.06 42 4320 42356 70881726
Full blood count abnormal 74.57 25.06 38 4324 33840 70890242
Hepatic function abnormal 71.11 25.06 47 4315 67949 70856133
Cerebral infarction 55.58 25.06 34 4328 42975 70881107
Shoshin beriberi 43.66 25.06 7 4355 75 70924007
Interstitial lung disease 39.63 25.06 40 4322 104645 70819437
Hyperuricaemia 38.57 25.06 17 4345 10949 70913133
Right ventricular failure 32.37 25.06 19 4343 22255 70901827
Fatigue 32.12 25.06 6 4356 824313 70099769
Pneumonia 31.54 25.06 94 4268 596138 70327944
Cardiac failure chronic 30.03 25.06 14 4348 10255 70913827
Decreased appetite 29.93 25.06 61 4301 304719 70619363
Uraemic encephalopathy 29.83 25.06 7 4355 587 70923495
Platelet count decreased 28.24 25.06 44 4318 178178 70745904
Sputum culture 27.73 25.06 5 4357 112 70923970
Upper respiratory tract inflammation 27.45 25.06 10 4352 3932 70920150
Renal ischaemia 25.53 25.06 7 4355 1096 70922986

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