triamterene Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
2728 396-01-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • triamterene
  • diurene
  • pterofen
  • pterophene
  • triamteren
  • triamteril
  • triteren
A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.
  • Molecular weight: 253.27
  • Formula: C12H11N7
  • CLOGP: 1.61
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 129.62
  • ALOGS: -2.42
  • ROTB: 1

Drug dosage:

DoseUnitRoute
0.10 g O

Approvals:

DateAgencyCompanyOrphan
Aug. 10, 1964 FDA CONCORDIA PHARMS INC

FDA Adverse Event Reporting System

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
Drug hypersensitivity 300.75 38.85 97 660 68303 4569932
Completed suicide 247.65 38.85 75 682 42370 4595865
Hyponatraemia 188.83 38.85 54 703 24676 4613559
Acute kidney injury 99.71 38.85 44 713 70387 4567848
Dizziness 87.97 38.85 45 712 99826 4538409
Hypokalaemia 82.83 38.85 27 730 18733 4619502
Lymphopenia 79.79 38.85 20 737 5427 4632808
Hyperkalaemia 74.80 38.85 24 733 15813 4622422
Focal segmental glomerulosclerosis 74.11 38.85 13 744 620 4637615
Nausea 71.17 38.85 48 709 177285 4460950
Drug ineffective 69.07 38.85 48 709 186013 4452222
Hypotension 63.89 38.85 32 725 67368 4570867
Rash 62.52 38.85 37 720 108351 4529884
Activated partial thromboplastin time prolonged 60.15 38.85 14 743 2775 4635460
Crystal nephropathy 59.69 38.85 9 748 163 4638072
Dyspnoea 58.90 38.85 39 718 138946 4499289
Tubulointerstitial nephritis 58.40 38.85 16 741 6103 4632132
Asthenia 51.12 38.85 30 727 86133 4552102
Product complaint 50.38 38.85 15 742 7679 4630556
Renal failure 49.25 38.85 23 734 41346 4596889
Somnolence 45.03 38.85 22 735 43638 4594597
Diarrhoea 44.67 38.85 34 723 150151 4488084
Sjogren's syndrome 41.68 38.85 9 748 1268 4636967
Oedema 40.80 38.85 16 741 18735 4619500
Photosensitivity reaction 39.08 38.85 11 746 4615 4633620

Pharmacologic Action:

SourceCodeDescription
ATC C03DB02 CARDIOVASCULAR SYSTEM
DIURETICS
POTASSIUM-SPARING AGENTS
Other potassium-sparing agents
FDA PE N0000008859 Decreased Renal K+ Excretion
FDA PE N0000175359 Increased Diuresis
FDA EPC N0000175418 Potassium-sparing Diuretic
CHEBI has role CHEBI:35498 diuretic
MeSH PA D004232 Diuretics
MeSH PA D062686 Epithelial Sodium Channel Blockers
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D045283 Natriuretic Agents
MeSH PA D026941 Sodium Channel Blockers

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Edema indication 267038008
Peripheral Edema due to Chronic Heart Failure indication
Pulmonary Edema due to Chronic Heart Failure indication
Hypokalemia off-label use 43339004
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Diabetes mellitus type 2 contraindication 44054006 DOID:9352
Diabetes mellitus type 1 contraindication 46635009 DOID:9744
Acidosis contraindication 51387008
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Megaloblastic anemia due to folate deficiency contraindication 85649008 DOID:14026
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Kidney stone contraindication 95570007
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Azotemia contraindication 445009001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.22 Basic
pKa2 5.5 Basic
pKa3 2.21 Basic
pKa4 0.54 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
Amiloride-sensitive sodium channel, ENaC Ion channel BLOCKER IC50 5.30 IUPHAR CHEMBL
Cytochrome P450 2D6 Enzyme IC50 5 DRUG MATRIX
Caspase-1 Enzyme IC50 5.44 DRUG MATRIX
Cathepsin G Enzyme IC50 5.13 DRUG MATRIX
Solute carrier family 12 member 1 Transporter WOMBAT-PK
Pteridine reductase 1 Enzyme Ki 5.47 CHEMBL

External reference:

IDSource
4017902 VUID
N0000146253 NUI
C0040869 UMLSCUI
D00386 KEGG_DRUG
12512008 SNOMEDCT_US
4017902 VANDF
80875 MMSL
10763 RXNORM
387053007 SNOMEDCT_US
5617 MMSL
d00396 MMSL
002315 NDDF
CHEBI:9671 CHEBI
CHEMBL585 ChEMBL_ID
DB00384 DRUGBANK_ID
WS821Z52LQ UNII
1266 INN_ID
5546 PUBCHEM_CID
D014223 MESH_DESCRIPTOR_UI
4329 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DYAZIDE HUMAN PRESCRIPTION DRUG LABEL 2 0007-3650 CAPSULE 37.50 mg ORAL NDA 12 sections
MAXZIDE HUMAN PRESCRIPTION DRUG LABEL 2 0378-0460 TABLET 75 mg ORAL NDA 11 sections
MAXZIDE-25 HUMAN PRESCRIPTION DRUG LABEL 2 0378-0464 TABLET 37.50 mg ORAL NDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1352 TABLET 37.50 mg ORAL NDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1355 TABLET 75 mg ORAL NDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-2537 CAPSULE 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0527-1632 CAPSULE 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0348 TABLET 75 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0424 TABLET 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0615-1333 CAPSULE 37.50 mg ORAL ANDA 11 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0615-3583 TABLET 37.50 mg ORAL ANDA 12 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-1008 TABLET 75 mg ORAL ANDA 12 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-1123 TABLET 37.50 mg ORAL ANDA 12 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-2074 CAPSULE 37.50 mg ORAL ANDA 12 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-2715 CAPSULE 50 mg ORAL ANDA 12 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-5067 TABLET 75 mg ORAL ANDA 11 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-5068 TABLET 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10135-581 CAPSULE 37.50 mg ORAL ANDA 13 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-049 TABLET 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-076 TABLET 37.50 mg ORAL NDA 11 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-080 TABLET 75 mg ORAL ANDA 12 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-536 TABLET 37.50 mg ORAL ANDA 12 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-537 TABLET 75 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 16590-338 TABLET 37.50 mg ORAL ANDA 11 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-496 TABLET 37.50 mg ORAL ANDA 12 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-497 TABLET 75 mg ORAL ANDA 12 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-839 CAPSULE 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33261-365 TABLET 75 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33261-952 TABLET 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 42291-841 CAPSULE 37.50 mg ORAL ANDA 11 sections