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

Stem definitionDrug idCAS RN
diuretics, chlorothiazide derivatives 1392 135-09-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • hydroflumethiazide
  • trifluoromethylhydrothiazide
A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822)
  • Molecular weight: 331.28
  • Formula: C8H8F3N3O4S2
  • CLOGP: -0.21
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 118.36
  • ALOGS: -2.59
  • ROTB: 2

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
25 mg O
25 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.30 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 90 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 10.05 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.70 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 22, 1959 FDA SHIRE LLC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03AA02 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides, plain
ATC C03AB02 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides and potassium in combination
ATC C03AH02 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides, combinations with psycholeptics and/or analgesics
FDA CS M0471776 Thiazides
FDA PE N0000175359 Increased Diuresis
FDA EPC N0000175419 Thiazide Diuretic
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
CHEBI has role CHEBI:35498 diuretics
CHEBI has role CHEBI:35674 antihypertensive drugs

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Edema indication 267038008
Calcium renal calculus off-label use 427649000
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

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.86 acidic
pKa2 10.57 acidic
pKa3 1.75 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 7.37 WOMBAT-PK CHEMBL

External reference:

IDSource
4018143 VUID
N0000146480 NUI
D00654 KEGG_DRUG
4018143 VANDF
C0020273 UMLSCUI
CHEBI:5784 CHEBI
HFZ PDB_CHEM_ID
CHEMBL1763 ChEMBL_ID
DB00774 DRUGBANK_ID
D006857 MESH_DESCRIPTOR_UI
3647 PUBCHEM_CID
7197 IUPHAR_LIGAND_ID
895 INN_ID
501CFL162R UNII
5495 RXNORM
4845 MMSL
d00645 MMSL
002296 NDDF
18914005 SNOMEDCT_US
395946004 SNOMEDCT_US

Pharmaceutical products:

None