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 58.54 13.31 87 13702 95552 63379681
Myocardial infarction 47.53 13.31 81 13708 99812 63375421
Oedema peripheral 42.47 13.31 113 13676 189398 63285835
Off label use 42.01 13.31 51 13738 674411 62800822
Pneumonia aspiration 39.63 13.31 43 13746 34497 63440736
Blood potassium decreased 34.38 13.31 44 13745 41982 63433251
Coronary artery disease 33.18 13.31 38 13751 32339 63442894
Crystal nephropathy 33.11 13.31 11 13778 925 63474308
Focal segmental glomerulosclerosis 31.86 13.31 12 13777 1456 63473777
Cerebrovascular accident 31.16 13.31 71 13718 107953 63367280
Drug intolerance 29.68 13.31 15 13774 308646 63166587
Product use issue 29.50 13.31 6 13783 220514 63254719
Coma 27.75 13.31 50 13739 64314 63410919
Systemic lupus erythematosus 27.29 13.31 6 13783 208912 63266321
Diabetic neuropathy 25.91 13.31 14 13775 3950 63471283
Wound 25.09 13.31 3 13786 163260 63311973
Underdose 24.45 13.31 30 13759 27426 63447807
Exposure during pregnancy 23.55 13.31 3 13786 155544 63319689
Transient ischaemic attack 22.58 13.31 34 13755 37719 63437514
Product complaint 22.24 13.31 20 13769 12789 63462444
Glossodynia 21.68 13.31 6 13783 178870 63296363
Pulmonary embolism 21.62 13.31 65 13724 116619 63358614
Hyponatraemia 21.37 13.31 63 13726 111837 63363396
Blood pressure increased 20.95 13.31 80 13709 161982 63313251
Deep vein thrombosis 20.83 13.31 52 13737 83748 63391485
Depression 20.67 13.31 91 13698 196401 63278832
Feeling abnormal 20.64 13.31 75 13714 148317 63326916
Cardiac failure congestive 20.55 13.31 55 13734 92378 63382855
Hypokalaemia 20.35 13.31 59 13730 103745 63371488
Infusion related reaction 19.35 13.31 15 13774 245506 63229727
Mitral valve incompetence 18.41 13.31 22 13767 19572 63455661
Intentional product use issue 18.12 13.31 3 13786 127889 63347344
Transient acantholytic dermatosis 17.88 13.31 4 13785 74 63475159
Drug ineffective 17.68 13.31 144 13645 1044621 62430612
Dizziness 17.58 13.31 156 13633 429769 63045464
Lacunar infarction 17.13 13.31 10 13779 3270 63471963
Fear 16.99 13.31 19 13770 15747 63459486
Blood triglycerides increased 16.92 13.31 17 13772 12471 63462762
Hyperlipidaemia 16.81 13.31 21 13768 19550 63455683
Asthenia 16.62 13.31 141 13648 383463 63091770
Vitamin B6 deficiency 16.40 13.31 4 13785 109 63475124
Angina unstable 16.27 13.31 13 13776 7082 63468151
Emotional distress 16.27 13.31 27 13762 32522 63442711
Blood sodium decreased 16.18 13.31 23 13766 24229 63451004
Lung neoplasm 16.01 13.31 12 13777 5954 63469279
Renal failure 15.97 13.31 59 13730 117593 63357640
Anxiety 15.96 13.31 91 13698 217450 63257783
Dehydration 15.80 13.31 77 13712 173277 63301956
Arthropathy 15.36 13.31 17 13772 234775 63240458
Product use in unapproved indication 15.34 13.31 10 13779 179070 63296163
Discomfort 14.82 13.31 9 13780 167365 63307868
Spinal stenosis 14.42 13.31 17 13772 14908 63460325
Ventricular hypertrophy 14.16 13.31 9 13780 3427 63471806
Alopecia 14.03 13.31 33 13756 337503 63137730
Myalgia 14.01 13.31 66 13723 146463 63328770
Therapeutic product effect decreased 13.76 13.31 13 13776 193174 63282059
Joint swelling 13.64 13.31 32 13757 327634 63147599
Tubulointerstitial nephritis 13.46 13.31 19 13770 19884 63455349
Hypersomnia 13.36 13.31 18 13771 18037 63457196

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 34.35 17.47 37 4605 48268 34904021
Myocardial infarction 31.40 17.47 57 4585 121028 34831261
Lymphopenia 31.18 17.47 22 4620 16313 34935976
Activated partial thromboplastin time prolonged 24.64 17.47 15 4627 8680 34943609
Dizziness 21.74 17.47 71 4571 218450 34733839
Bundle branch block left 21.40 17.47 12 4630 5967 34946322
Emotional distress 19.33 17.47 16 4626 15010 34937279
Injury 18.61 17.47 18 4624 20669 34931620

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
Gastrooesophageal reflux disease 73.18 13.65 90 13653 104156 79626489
Myocardial infarction 71.64 13.65 120 13623 184009 79546636
Coronary artery disease 67.35 13.65 69 13674 65405 79665240
Cerebrovascular accident 41.28 13.65 86 13657 155206 79575439
Off label use 41.19 13.65 58 13685 907157 78823488
Emotional distress 37.29 13.65 40 13703 39929 79690716
Crystal nephropathy 30.85 13.65 11 13732 1444 79729201
Injury 29.41 13.65 50 13693 77446 79653199
Underdose 28.87 13.65 32 13711 33119 79697526
Blood potassium decreased 27.64 13.65 37 13706 46475 79684170
Deep vein thrombosis 27.60 13.65 63 13680 120856 79609789
Transient ischaemic attack 26.95 13.65 39 13704 52656 79677989
Depression 26.59 13.65 90 13653 216700 79513945
Hyponatraemia 26.53 13.65 79 13664 177769 79552876
Pneumonia aspiration 26.46 13.65 44 13699 66923 79663722
Pulmonary embolism 26.32 13.65 77 13666 171577 79559068
Fear 25.98 13.65 25 13718 21961 79708684
Hyperlipidaemia 25.91 13.65 27 13716 26066 79704579
Focal segmental glomerulosclerosis 25.09 13.65 12 13731 3309 79727336
Cardiac failure congestive 24.90 13.65 67 13676 142335 79588310
Coma 24.72 13.65 54 13689 100595 79630050
Oedema peripheral 24.42 13.65 97 13646 252191 79478454
Product complaint 23.43 13.65 19 13724 13330 79717315
Diabetic neuropathy 23.06 13.65 14 13729 6202 79724443
Pyrexia 22.97 13.65 52 13691 678657 79051988
Dizziness 22.83 13.65 162 13581 526279 79204366
Mitral valve incompetence 22.21 13.65 26 13717 28539 79702106
Anxiety 22.03 13.65 93 13650 248419 79482226
Ventricular hypertrophy 21.65 13.65 14 13729 6924 79723721
Renal failure 20.03 13.65 78 13665 200890 79529755
Myocardial ischaemia 19.46 13.65 23 13720 25496 79705149
Product use issue 19.42 13.65 6 13737 209816 79520829
Carpal tunnel syndrome 19.02 13.65 20 13723 19508 79711137
Chest pain 17.98 13.65 96 13647 282208 79448437
Feeling abnormal 17.69 13.65 64 13679 159135 79571510
Renal injury 17.68 13.65 18 13725 16909 79713736
Asthenia 17.47 13.65 149 13594 511540 79219105
Intentional product use issue 16.73 13.65 3 13740 152109 79578536
Blood sodium decreased 16.12 13.65 24 13719 33231 79697414
Febrile neutropenia 16.03 13.65 10 13733 230989 79499656
Transient acantholytic dermatosis 15.89 13.65 4 13739 158 79730487
Bundle branch block left 15.34 13.65 14 13729 11499 79719146
Arteriosclerosis 14.86 13.65 17 13726 18210 79712435
Hiatus hernia 14.55 13.65 19 13724 23293 79707352
Angina unstable 14.47 13.65 16 13727 16511 79714134
Enterocele 14.45 13.65 3 13740 49 79730596
Blood pressure increased 14.22 13.65 73 13670 211287 79519358
Renal cyst 14.19 13.65 15 13728 14717 79715928
Drug intolerance 13.90 13.65 15 13728 264104 79466541
Hypertension 13.82 13.65 101 13642 330891 79399754

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
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




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
Solute carrier family 12 member 1 Transporter WOMBAT-PK
Cytochrome P450 2D6 Enzyme IC50 5 DRUG MATRIX
Caspase-1 Enzyme IC50 5.44 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 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