triamterene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.201 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.360 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 15.849 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.559 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 46.320 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 56.580 % High 1
herg hERG pIC50 4.522 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.560 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.133 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 39.890 % High 1
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,JAK1,JAK3,MAP3K1,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PDK2,PIK3CA,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 46
kinase-selectivity-class AXL,MAP2K3,MAP3K21,MAPK7,PIK3CD,PIK3CG 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.428 High 1
mh-clint Mouse hepatocyte intrinsic clearance 4.699 High 1
mppb Mouse plasma protein binding (% unbound) 46.040 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 5.623 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 56.520 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.339 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 88.680 % High 1
rppb Rat plasma protein binding (% unbound) 51.320 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 106.660 uM High 1

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
Pneumonia aspiration 65.98 14.46 46 9805 40894 90577702
Gastrooesophageal reflux disease 49.95 14.46 75 9776 166262 90452334
Coma 43.04 14.46 46 9805 72586 90546010
Crystal nephropathy 38.37 14.46 11 9840 1140 90617456
Myocardial infarction 37.98 14.46 52 9799 105920 90512676
Focal segmental glomerulosclerosis 37.27 14.46 12 9839 1839 90616757
Blood potassium decreased 37.05 14.46 35 9816 47692 90570904
Hyponatraemia 34.21 14.46 56 9795 133482 90485114
Underdose 31.62 14.46 34 9817 53983 90564613
Somnolence 29.36 14.46 68 9783 209016 90409580
Diabetic neuropathy 26.71 14.46 12 9839 4562 90614034
Feeling abnormal 26.40 14.46 57 9794 167178 90451418
Treatment failure 22.89 14.46 3 9848 303925 90314671
Oedema peripheral 21.27 14.46 69 9782 257846 90360750
Pulmonary embolism 21.11 14.46 45 9806 130775 90487821
Glossodynia 20.30 14.46 5 9846 321774 90296822
Infusion related reaction 20.26 14.46 10 9841 416770 90201826
Drug intolerance 19.92 14.46 12 9839 447579 90171017
Cardiac failure congestive 19.57 14.46 37 9814 98657 90519939
Lung neoplasm 19.55 14.46 11 9840 6724 90611872
Ileus paralytic 19.51 14.46 10 9841 5075 90613521
Transient acantholytic dermatosis 19.45 14.46 4 9847 101 90618495
Coronary artery disease 19.39 14.46 21 9830 33602 90584994
Blood pressure increased 19.27 14.46 56 9795 197161 90421435
Product use issue 19.18 14.46 6 9845 329913 90288683
Tubulointerstitial nephritis 18.55 14.46 18 9833 25325 90593271
Wound 18.55 14.46 5 9846 302975 90315621
Deep vein thrombosis 17.74 14.46 34 9817 91586 90527010
Photosensitivity reaction 17.66 14.46 15 9836 17792 90600804
Vitamin B6 deficiency 16.69 14.46 4 9847 206 90618390
Fear 16.48 14.46 14 9837 16608 90601988
Dry skin 16.22 14.46 32 9819 88041 90530555
Cerebrovascular accident 16.05 14.46 39 9812 123494 90495102
Dehydration 16.00 14.46 52 9799 194395 90424201
Off label use 15.84 14.46 64 9787 1102188 89516408
Renal failure 15.59 14.46 40 9811 130967 90487629
Myalgia 15.47 14.46 48 9803 175077 90443519
Hypersomnia 15.22 14.46 15 9836 21516 90597080
Completed suicide 14.95 14.46 42 9809 145016 90473580
Hypokalaemia 14.54 14.46 39 9812 131077 90487519
Therapeutic product effect decreased 14.51 14.46 6 9845 277565 90341031
Exposure during pregnancy 14.47 14.46 4 9847 238406 90380190

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
Lymphopenia 39.07 19.26 23 3277 21540 42596495
Dizziness 22.10 19.26 55 3245 249199 42368836
Activated partial thromboplastin time prolonged 21.29 19.26 14 3286 15889 42602146

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 58.18 14.45 76 9824 179900 110399499
Pneumonia aspiration 48.06 14.45 47 9853 81186 110498213
Myocardial infarction 45.61 14.45 70 9830 192013 110387386
Coma 36.87 14.45 49 9851 117820 110461579
Hyponatraemia 36.60 14.45 68 9832 217585 110361814
Underdose 36.15 14.45 36 9864 63518 110515881
Crystal nephropathy 35.29 14.45 11 9889 1845 110577554
Completed suicide 34.99 14.45 71 9829 242310 110337089
Coronary artery disease 34.28 14.45 37 9863 71653 110507746
Blood potassium decreased 31.42 14.45 31 9869 54083 110525316
Diabetic neuropathy 30.13 14.45 14 9886 6985 110572414
Focal segmental glomerulosclerosis 30.09 14.45 12 9888 4133 110575266
Somnolence 25.36 14.45 71 9829 297378 110282021
Feeling abnormal 21.53 14.45 49 9851 180662 110398737
Cardiac failure congestive 21.49 14.45 44 9856 150956 110428443
Emotional distress 21.18 14.45 23 9877 44824 110534575
Tubulointerstitial nephritis 20.83 14.45 25 9875 54259 110525140
Ileus paralytic 20.76 14.45 13 9887 11724 110567675
Deep vein thrombosis 20.19 14.45 41 9859 139846 110439553
Pulmonary embolism 19.06 14.45 52 9848 214422 110364977
Fear 18.76 14.45 16 9884 23177 110556222
Off label use 18.25 14.45 71 9829 1500114 109079285
Cerebrovascular accident 18.20 14.45 46 9854 181238 110398161
Renal failure 17.29 14.45 52 9848 226522 110352877
Pyrexia 16.40 14.45 35 9865 898230 109681169
Infusion related reaction 16.07 14.45 7 9893 381155 110198244
Dry skin 16.07 14.45 32 9868 107621 110471778
Dizziness 15.96 14.45 112 9788 698081 109881318
Transient acantholytic dermatosis 15.68 14.45 4 9896 325 110579074
Lichenification 15.16 14.45 5 9895 1004 110578395
Unevaluable event 14.62 14.45 22 9878 59205 110520194

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
MeSH PA D004232 Diuretics
MeSH PA D026941 Sodium Channel Blockers
MeSH PA D045283 Natriuretic Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D062686 Epithelial Sodium Channel Blockers
CHEBI has role CHEBI:35498 diuretic
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:38633 sodium channel blocker
CHEBI has role CHEBI:62868 hepatoprotective agent
CHEBI has role CHEBI:145947 antiatherosclerotic agent

Related Drugs by ATC class:

C03DB Other potassium-sparing agents 1 drug
amiloride

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




🐶 Veterinary Drug Use

None

🐶 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
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 0591-0424 TABLET 37.50 mg ORAL ANDA 19 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 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
Triamterene and Hydrochlorothiazide Human Prescription Drug Label 2 33342-467 CAPSULE 37.50 mg ORAL ANDA 11 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 45865-402 CAPSULE 37.50 mg ORAL ANDA 24 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-1270 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-1834 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-2028 CAPSULE 37.50 mg ORAL ANDA 20 sections
triamterene and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-5801 TABLET 37.50 mg ORAL ANDA 17 sections
triamterene and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-6736 TABLET 75 mg ORAL ANDA 17 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-6944 CAPSULE 37.50 mg ORAL ANDA 22 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-7437 CAPSULE 37.50 mg ORAL ANDA 18 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-7438 CAPSULE 37.50 mg ORAL ANDA 18 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 51407-286 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 51655-217 TABLET 37.50 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 51655-582 TABLET 75 mg ORAL ANDA 19 sections
Triamterene and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 51655-630 TABLET 37.50 mg ORAL ANDA 19 sections