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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	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 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	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 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	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:

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