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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	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 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	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 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	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:

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
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

🐶 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
Caspase-1	Enzyme	P29466	CASP1_HUMAN		IC50	5.44	DRUG MATRIX
Solute carrier family 12 member 1	Transporter	Q13621	S12A1_HUMAN				WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5	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	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