triamterene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2728	396-01-0

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.10	g	O

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Aug. 10, 1964	FDA	CONCORDIA PHARMS INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Gastrooesophageal reflux disease	53.88	13.09	82	13433	83175	56195377
Myocardial infarction	45.92	13.09	81	13434	92789	56185763
Oedema peripheral	44.60	13.09	115	13400	171139	56107413
Off label use	37.73	13.09	47	13468	556133	55722419
Rheumatoid arthritis	35.82	13.09	24	13491	382580	55895972
Blood potassium decreased	33.79	13.09	44	13471	38628	56239924
Crystal nephropathy	33.12	13.09	11	13504	835	56277717
Pneumonia aspiration	31.68	13.09	39	13476	32372	56246180
Coronary artery disease	31.63	13.09	38	13477	30758	56247794
Focal segmental glomerulosclerosis	30.71	13.09	12	13503	1454	56277098
Cerebrovascular accident	30.42	13.09	71	13444	99199	56179353
Drug intolerance	27.00	13.09	15	13500	264803	56013749
Product use issue	26.68	13.09	6	13509	186035	56092517
Systemic lupus erythematosus	25.44	13.09	6	13509	180072	56098480
Diabetic neuropathy	25.33	13.09	14	13501	3734	56274818
Wound	23.14	13.09	3	13512	138801	56139751
Exposure during pregnancy	22.60	13.09	3	13512	136339	56142213
Coma	22.03	13.09	46	13469	59609	56218943
Product complaint	21.99	13.09	20	13495	11740	56266812
Glossodynia	21.69	13.09	5	13510	152453	56126099
Transient ischaemic attack	21.60	13.09	33	13482	33544	56245008
Product use in unapproved indication	21.31	13.09	4	13511	140818	56137734
Pulmonary embolism	21.04	13.09	65	13450	107059	56171493
Deep vein thrombosis	20.32	13.09	52	13463	76925	56201627
Cardiac failure congestive	19.87	13.09	56	13459	87664	56190888
Depression	19.29	13.09	90	13425	180027	56098525
Feeling abnormal	19.17	13.09	73	13442	133529	56145023
Underdose	19.16	13.09	26	13489	23731	56254821
Hyponatraemia	19.16	13.09	61	13454	102078	56176474
Blood pressure increased	18.95	13.09	77	13438	145099	56133453
Mitral valve incompetence	17.99	13.09	22	13493	18131	56260421
Transient acantholytic dermatosis	17.79	13.09	4	13511	68	56278484
Drug ineffective	17.66	13.09	139	13376	918850	55359702
Dizziness	17.59	13.09	152	13363	375988	55902564
Hypokalaemia	17.35	13.09	56	13459	94381	56184171
Asthenia	17.31	13.09	141	13374	342832	55935720
Infusion related reaction	17.10	13.09	15	13500	208916	56069636
Vitamin B6 deficiency	17.04	13.09	4	13511	83	56278469
Anxiety	16.79	13.09	91	13424	193081	56085471
Lacunar infarction	16.59	13.09	10	13505	3135	56275417
Blood triglycerides increased	16.45	13.09	17	13498	11660	56266892
Hyperlipidaemia	16.43	13.09	21	13494	18088	56260464
Fear	16.31	13.09	19	13496	14889	56263663
Emotional distress	16.05	13.09	27	13488	29736	56248816
Blood sodium decreased	15.87	13.09	23	13492	22311	56256241
Lung neoplasm	15.83	13.09	12	13503	5475	56273077
Alopecia	15.78	13.09	29	13486	293429	55985123
Angina unstable	15.57	13.09	13	13502	6808	56271744
Dehydration	15.30	13.09	77	13438	158748	56119804
Intentional product use issue	14.73	13.09	3	13512	99730	56178822
Renal failure	14.73	13.09	59	13456	110441	56168111
Tubulointerstitial nephritis	14.61	13.09	19	13496	16646	56261906
Injury	14.33	13.09	39	13476	59812	56218740
Spinal stenosis	13.91	13.09	17	13498	13997	56264555
Ventricular hypertrophy	13.82	13.09	9	13506	3229	56275323
Arthropathy	13.44	13.09	17	13498	200258	56078294
Myalgia	13.42	13.09	65	13450	131960	56146592
Hypersomnia	13.35	13.09	18	13497	16323	56262229
Carpal tunnel syndrome	13.35	13.09	19	13496	18125	56260427
Osteoarthritis	13.31	13.09	46	13469	80250	56198302

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Coronary artery disease	33.46	17.11	37	4506	46050	31646751
Myocardial infarction	30.94	17.11	57	4486	113397	31579404
Lymphopenia	29.92	17.11	21	4522	14308	31678493
Activated partial thromboplastin time prolonged	24.35	17.11	15	4528	8210	31684591
Dizziness	22.44	17.11	71	4472	199076	31493725
Emotional distress	18.90	17.11	16	4527	14340	31678461
Bundle branch block left	18.76	17.11	11	4532	5507	31687294
Injury	18.19	17.11	18	4525	19691	31673110

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myocardial infarction	69.14	13.18	120	13370	171525	70743429
Gastrooesophageal reflux disease	67.88	13.18	85	13405	90754	70824200
Coronary artery disease	64.14	13.18	69	13421	62667	70852287
Cerebrovascular accident	40.14	13.18	86	13404	143384	70771570
Off label use	37.63	13.18	52	13438	743008	70171946
Emotional distress	36.42	13.18	40	13450	37148	70877806
Injury	32.14	13.18	50	13440	65195	70849759
Crystal nephropathy	31.08	13.18	11	13479	1279	70913675
Transient ischaemic attack	26.63	13.18	38	13452	45906	70869048
Pulmonary embolism	26.23	13.18	77	13413	155790	70759164
Deep vein thrombosis	25.95	13.18	62	13428	110980	70803974
Hyperlipidaemia	25.70	13.18	27	13463	23836	70891118
Depression	25.05	13.18	89	13401	198885	70716069
Fear	25.05	13.18	25	13465	20786	70894168
Hyponatraemia	24.97	13.18	77	13413	160010	70754944
Oedema peripheral	24.54	13.18	97	13393	227994	70686960
Focal segmental glomerulosclerosis	24.38	13.18	12	13478	3192	70911762
Cardiac failure congestive	23.83	13.18	68	13422	135389	70779565
Hypertension	23.56	13.18	115	13375	295918	70619036
Product complaint	23.24	13.18	19	13471	12212	70902742
Anxiety	23.14	13.18	93	13397	220237	70694717
Blood potassium decreased	23	13.18	34	13456	42387	70872567
Underdose	22.73	13.18	28	13462	29355	70885599
Diabetic neuropathy	22.55	13.18	14	13476	5844	70909110
Dizziness	22.43	13.18	158	13332	463983	70450971
Pyrexia	22.12	13.18	52	13438	606900	70308054
Mitral valve incompetence	21.53	13.18	26	13464	26702	70888252
Ventricular hypertrophy	21.06	13.18	14	13476	6570	70908384
Pneumonia aspiration	20.55	13.18	40	13450	62249	70852705
Coma	20.09	13.18	50	13440	91794	70823160
Carpal tunnel syndrome	19.63	13.18	20	13470	17037	70897917
Chest pain	18.84	13.18	96	13394	251164	70663790
Myocardial ischaemia	18.62	13.18	23	13467	24177	70890777
Renal failure	18.42	13.18	78	13412	188992	70725962
Product use issue	17.81	13.18	6	13484	179931	70735023
Asthenia	17.74	13.18	148	13342	457518	70457436
Renal injury	16.96	13.18	18	13472	16076	70898878
Feeling abnormal	16.50	13.18	62	13428	142257	70772697
Transient acantholytic dermatosis	16.16	13.18	4	13486	133	70914821
Blood sodium decreased	15.60	13.18	24	13466	30974	70883980
Febrile neutropenia	15.32	13.18	10	13480	204308	70710646
Rheumatoid arthritis	15.13	13.18	20	13470	291785	70623169
Arteriosclerosis	14.75	13.18	17	13473	16621	70898333
Hiatus hernia	14.54	13.18	19	13471	21115	70893839
Renal cyst	14.19	13.18	15	13475	13330	70901624
Enterocele	14.16	13.18	3	13487	49	70914905
Intentional product use issue	13.77	13.18	3	13487	120139	70794815
Therapeutic product effect incomplete	13.73	13.18	3	13487	119879	70795075
Angina unstable	13.69	13.18	16	13474	15877	70899077
Bundle branch block left	13.46	13.18	13	13477	10386	70904568
Blood pressure increased	13.41	13.18	71	13419	188446	70726508

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Amiloride-sensitive sodium channel, ENaC	Ion channel	P37088 P51168 P51170	SCNNA_HUMAN SCNNB_HUMAN SCNNG_HUMAN	BLOCKER	IC50	5.30	IUPHAR	CHEMBL
Solute carrier family 12 member 1	Transporter	Q13621	S12A1_HUMAN				WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5	DRUG MATRIX
Caspase-1	Enzyme	P29466	CASP1_HUMAN		IC50	5.44	DRUG MATRIX
Cathepsin G	Enzyme	P08311	CATG_HUMAN		IC50	5.13	DRUG MATRIX
Pteridine reductase 1	Enzyme		PTR1_LEIMA		Ki	5.47	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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