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

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.03 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 13.15 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 51 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 13 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 63 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.42 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.30 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 10, 1964 FDA CONCORDIA PHARMS INC

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
Gastrooesophageal reflux disease 44.03 12.87 75 13219 76353 50515477
Myocardial infarction 43.14 12.87 81 13213 88946 50502884
Oedema peripheral 41.89 12.87 113 13181 157848 50433982
Off label use 34.03 12.87 45 13249 474381 50117449
Crystal nephropathy 32.55 12.87 11 13283 804 50591026
Blood potassium decreased 32.26 12.87 44 13250 36901 50554929
Focal segmental glomerulosclerosis 30.70 12.87 12 13282 1329 50590501
Coronary artery disease 29.97 12.87 38 13256 29688 50562142
Cerebrovascular accident 28.43 12.87 71 13223 94609 50497221
Drug intolerance 22.46 12.87 15 13279 219089 50372741
Diabetic neuropathy 22.05 12.87 13 13281 3578 50588252
Product use issue 22.04 12.87 6 13288 149469 50442361
Exposure during pregnancy 21.74 12.87 3 13291 121012 50470818
Product complaint 20.89 12.87 20 13274 11446 50580384
Transient ischaemic attack 20.40 12.87 33 13261 32177 50559653
Systemic lupus erythematosus 20.07 12.87 6 13288 140616 50451214
Pneumonia aspiration 19.95 12.87 32 13262 30972 50560858
Transient acantholytic dermatosis 19.14 12.87 4 13290 43 50591787
Depression 19.06 12.87 90 13204 165333 50426497
Deep vein thrombosis 18.95 12.87 52 13242 73252 50518578
Pulmonary embolism 18.68 12.87 64 13230 101640 50490190
Product use in unapproved indication 18.34 12.87 4 13290 115815 50476015
Wound 18.14 12.87 3 13291 105791 50486039
Hyponatraemia 18.10 12.87 61 13233 96078 50495752
Feeling abnormal 17.27 12.87 72 13222 125420 50466410
Blood pressure increased 17.25 12.87 75 13219 133057 50458773
Injury 17.17 12.87 39 13255 48886 50542944
Mitral valve incompetence 17.08 12.87 22 13272 17449 50574381
Vitamin B6 deficiency 17.02 12.87 4 13290 76 50591754
Hypokalaemia 16.71 12.87 56 13238 87936 50503894
Glossodynia 16.37 12.87 5 13289 115564 50476266
Cardiac failure congestive 16.29 12.87 54 13240 84328 50507502
Asthenia 16.28 12.87 141 13153 318901 50272929
Drug ineffective 16.13 12.87 138 13156 819195 49772635
Dizziness 16.10 12.87 150 13144 346219 50245611
Lacunar infarction 15.94 12.87 10 13284 3077 50588753
Anxiety 15.86 12.87 90 13204 177516 50414314
Blood triglycerides increased 15.63 12.87 17 13277 11295 50580535
Hyperlipidaemia 15.52 12.87 21 13273 17469 50574361
Fear 15.30 12.87 19 13275 14530 50577300
Blood sodium decreased 15.24 12.87 23 13271 21124 50570706
Osteoarthritis 15.15 12.87 46 13248 68560 50523270
Lung neoplasm 15.08 12.87 12 13282 5370 50586460
Emotional distress 15.02 12.87 27 13267 28636 50563194
Angina unstable 14.75 12.87 13 13281 6693 50585137
Tubulointerstitial nephritis 14.63 12.87 19 13275 15192 50576638
Dehydration 13.44 12.87 77 13217 152372 50439458
Coma 13.38 12.87 39 13255 56840 50534990
Infusion related reaction 13.25 12.87 15 13279 169542 50422288
Spinal stenosis 13.15 12.87 17 13277 13533 50578297
Ventricular hypertrophy 13.14 12.87 9 13285 3206 50588624
Carpal tunnel syndrome 13.08 12.87 19 13275 16874 50574956
Renal failure 13.00 12.87 59 13235 106574 50485256

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
Coronary artery disease 31.41 17.11 36 4436 44154 29525901
Lymphopenia 29.98 17.11 21 4451 13512 29556543
Myocardial infarction 29.91 17.11 57 4415 110239 29459816
Activated partial thromboplastin time prolonged 24.45 17.11 15 4457 7727 29562328
Dizziness 22.24 17.11 71 4401 189613 29380442
Bundle branch block left 18.67 17.11 11 4461 5266 29564789
Emotional distress 18.61 17.11 16 4456 13879 29556176
Injury 17.89 17.11 18 4454 19028 29551027

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
Myocardial infarction 65.53 13.67 120 13118 165701 64319793
Coronary artery disease 60.22 13.67 68 13170 60365 64425129
Gastrooesophageal reflux disease 57.74 13.67 78 13160 83065 64402429
Cerebrovascular accident 38.14 13.67 86 13152 137497 64347997
Injury 35.07 13.67 50 13188 55942 64429552
Emotional distress 34.95 13.67 40 13198 35998 64449496
Off label use 33.36 13.67 49 13189 632757 63852737
Crystal nephropathy 30.47 13.67 11 13227 1254 64484240
Pulmonary embolism 25.60 13.67 77 13161 146279 64339215
Transient ischaemic attack 25.55 13.67 38 13200 44144 64441350
Depression 25.36 13.67 89 13149 183202 64302292
Hyperlipidaemia 24.85 13.67 27 13211 22949 64462545
Oedema peripheral 24.81 13.67 97 13141 210220 64275274
Focal segmental glomerulosclerosis 24.47 13.67 12 13226 2932 64482562
Fear 24.11 13.67 25 13213 20146 64465348
Deep vein thrombosis 24.01 13.67 61 13177 105121 64380373
Anxiety 22.73 13.67 92 13146 202557 64282937
Dizziness 22.43 13.67 158 13080 430005 64055489
Product complaint 22.36 13.67 19 13219 11935 64473559
Pyrexia 21.69 13.67 52 13186 558592 63926902
Hyponatraemia 21.35 13.67 73 13165 148266 64337228
Blood potassium decreased 20.90 13.67 33 13205 40366 64445128
Mitral valve incompetence 20.90 13.67 26 13212 25512 64459982
Cardiac failure congestive 20.34 13.67 66 13172 130514 64354980
Ventricular hypertrophy 20.22 13.67 14 13224 6502 64478992
Diabetic neuropathy 19.69 13.67 13 13225 5588 64479906
Carpal tunnel syndrome 19.61 13.67 20 13218 15808 64469686
Chest pain 18.20 13.67 96 13142 235884 64249610
Myocardial ischaemia 17.96 13.67 23 13215 23228 64462266
Transient acantholytic dermatosis 17.32 13.67 4 13234 91 64485403
Asthenia 17.18 13.67 148 13090 427896 64057598
Hypertension 17.02 13.67 101 13137 259160 64226334
Renal failure 16.92 13.67 78 13160 181610 64303884
Product use issue 15.28 13.67 6 13232 151709 64333785
Feeling abnormal 15.24 13.67 61 13177 133541 64351953
Blood sodium decreased 15.13 13.67 24 13214 29458 64456036
Febrile neutropenia 15.06 13.67 10 13228 187647 64297847
Renal injury 14.74 13.67 17 13221 15412 64470082
Arteriosclerosis 14.35 13.67 17 13221 15860 64469634
Hiatus hernia 14.26 13.67 19 13219 19938 64465556
Enterocele 14.11 13.67 3 13235 46 64485448

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03DB02 CARDIOVASCULAR SYSTEM
DIURETICS
ALDOSTERONE ANTAGONISTS AND OTHER 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 diuretics
CHEBI has role CHEBI:38633 sodium channel blockers
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 | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Edema indication 267038008
Pulmonary Edema due to Chronic Heart Failure indication
Peripheral 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




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 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
Caspase-1 Enzyme IC50 5.44 DRUG MATRIX
Solute carrier family 12 member 1 Transporter WOMBAT-PK
Cytochrome P450 2D6 Enzyme IC50 5 DRUG MATRIX
Cathepsin G Enzyme IC50 5.13 DRUG MATRIX
Pteridine reductase 1 Enzyme Ki 5.47 CHEMBL

External reference:

IDSource
4017902 VUID
N0000146253 NUI
D00386 KEGG_DRUG
4017902 VANDF
C0040869 UMLSCUI
CHEBI:9671 CHEBI
DX2 PDB_CHEM_ID
CHEMBL585 ChEMBL_ID
DB00384 DRUGBANK_ID
D014223 MESH_DESCRIPTOR_UI
5546 PUBCHEM_CID
4329 IUPHAR_LIGAND_ID
1266 INN_ID
WS821Z52LQ UNII
10763 RXNORM
5617 MMSL
80875 MMSL
d00396 MMSL
002315 NDDF
12512008 SNOMEDCT_US
387053007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MAXZIDE HUMAN PRESCRIPTION DRUG LABEL 2 0378-0460 TABLET 75 mg ORAL NDA 20 sections
MAXZIDE HUMAN PRESCRIPTION DRUG LABEL 2 0378-0460 TABLET 75 mg ORAL NDA 20 sections
MAXZIDE-25 HUMAN PRESCRIPTION DRUG LABEL 2 0378-0464 TABLET 37.50 mg ORAL NDA 20 sections
MAXZIDE-25 HUMAN PRESCRIPTION DRUG LABEL 2 0378-0464 TABLET 37.50 mg ORAL NDA 20 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1352 TABLET 37.50 mg ORAL NDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1352 TABLET 37.50 mg ORAL NDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1355 TABLET 75 mg ORAL NDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-1355 TABLET 75 mg ORAL NDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-2537 CAPSULE 37.50 mg ORAL ANDA 21 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0527-1632 CAPSULE 37.50 mg ORAL ANDA 20 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0348 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0348 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0424 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0591-0424 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0615-1333 CAPSULE 37.50 mg ORAL ANDA 23 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0615-3583 TABLET 37.50 mg ORAL ANDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-2074 CAPSULE 37.50 mg ORAL ANDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0781-2715 CAPSULE 50 mg ORAL ANDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10135-581 CAPSULE 37.50 mg ORAL ANDA 20 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-049 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-076 TABLET 37.50 mg ORAL NDA 22 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-080 TABLET 75 mg ORAL ANDA 23 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-536 TABLET 37.50 mg ORAL ANDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-537 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 16590-338 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-496 TABLET 37.50 mg ORAL ANDA 21 sections
Triamterene hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-497 TABLET 75 mg ORAL ANDA 21 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-839 CAPSULE 37.50 mg ORAL ANDA 23 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33261-365 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33261-952 TABLET 37.50 mg ORAL ANDA 19 sections