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

Stem definition	Drug id	CAS RN
diuretics, chlorothiazide derivatives	2733	133-67-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: triclormetiazide trichlormethiazide hydrotrichlorothiazide trichlormetazid trichlormethiazid trichloromethiazide	A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830) Molecular weight: 380.64 Formula: C8H8Cl3N3O4S2 CLOGP: 0.88 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 118.36 ALOGS: -2.96 ROTB: 2 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

triclormetiazide
trichlormethiazide
hydrotrichlorothiazide
trichlormetazid
trichlormethiazid
trichloromethiazide

A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830)

Molecular weight: 380.64
Formula: C8H8Cl3N3O4S2
CLOGP: 0.88
LIPINSKI: 0
HAC: 7
HDO: 3
TPSA: 118.36
ALOGS: -2.96
ROTB: 2

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
4	mg	O
4	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.80 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.18 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
March 9, 1960	FDA

FDA Adverse Event Reporting System (Female)

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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
Vital capacity decreased	317.57	34.84	56	2583	1672	63484711
Reversible airways obstruction	313.99	34.84	56	2583	1786	63484597
Sputum culture positive	304.91	34.84	56	2583	2111	63484272
Bronchial secretion retention	291.12	34.84	56	2583	2717	63483666
Eosinophil count increased	219.50	34.84	57	2582	10871	63475512
Upper-airway cough syndrome	212.22	34.84	56	2583	11362	63475021
Multiple allergies	201.70	34.84	56	2583	13746	63472637
Obstructive airways disorder	191.95	34.84	59	2580	20640	63465743
Pulmonary mass	174.45	34.84	56	2583	22540	63463843
Full blood count abnormal	155.83	34.84	56	2583	31661	63454722

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FDA Adverse Event Reporting System (Male)

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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
Renal impairment	80.26	23.35	57	2064	94456	34860354
Cardiac failure	68.27	23.35	51	2070	91197	34863613
Hepatic function abnormal	52.62	23.35	33	2088	44330	34910480
Shoshin beriberi	43.76	23.35	7	2114	75	34954735
Cerebral infarction	41.81	23.35	24	2097	27431	34927379
Interstitial lung disease	34.86	23.35	30	2091	65252	34889558
Renal ischaemia	30.23	23.35	7	2114	562	34954248
Vitamin B1 deficiency	28.08	23.35	6	2115	333	34954477
Cardiac failure chronic	27.19	23.35	12	2109	7867	34946943
Decreased appetite	26.78	23.35	41	2080	166351	34788459

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FDA Adverse Event Reporting System (Geriatric)

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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
Vital capacity decreased	273.72	24.33	53	4878	1763	79737694
Reversible airways obstruction	264.15	24.33	53	4878	2123	79737334
Sputum culture positive	234.97	24.33	53	4878	3728	79735729
Bronchial secretion retention	230.64	24.33	53	4878	4051	79735406
Multiple allergies	181.45	24.33	53	4878	10407	79729050
Upper-airway cough syndrome	179.93	24.33	54	4877	11639	79727818
Eosinophil count increased	167.64	24.33	56	4875	17049	79722408
Obstructive airways disorder	137.78	24.33	57	4874	31402	79708055
Pulmonary mass	135.30	24.33	55	4876	28979	79710478
Renal impairment	134.01	24.33	96	4835	157687	79581770

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C03AA06	CARDIOVASCULAR SYSTEM DIURETICS LOW-CEILING DIURETICS, THIAZIDES Thiazides, plain
ATC	C03AB06	CARDIOVASCULAR SYSTEM DIURETICS LOW-CEILING DIURETICS, THIAZIDES Thiazides and potassium in combination
ATC	C03EA02	CARDIOVASCULAR SYSTEM DIURETICS DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION Low-ceiling diuretics and potassium-sparing agents
CHEBI has role	CHEBI:35498	diuretics
CHEBI has role	CHEBI:35674	antihypertensive drugs
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004232	Diuretics
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D045283	Natriuretic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Suicidal thoughts	contraindication	6471006
Peptic ulcer	contraindication	13200003	DOID:750
Chronic disease of respiratory system	contraindication	17097001
Electroconvulsive therapy	contraindication	23835007
Depressive disorder	contraindication	35489007
Conduction disorder of the heart	contraindication	44808001
Chronic heart failure	contraindication	48447003
Ulcerative colitis	contraindication	64766004	DOID:8577
Epilepsy	contraindication	84757009	DOID:1826

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🐶 Veterinary Drug Use

Species	Use	Relation
Cattle	No Use Class Stated Or Implied	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Naquasone Bolus	Intervet Inc.	2

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.05	acidic
pKa2	10.3	acidic
pKa3	1.29	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Solute carrier family 12 member 3	Transporter	P55017	S12A3_HUMAN	INHIBITOR	A2	7	WOMBAT-PK	CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	6.46	CHEMBL
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN		Ki	6.35	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	7.06	CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	6.51	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	6.12	CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	6.87	CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	8.10	CHEMBL
Carbonic anhydrase 6	Enzyme	P23280	CAH6_HUMAN		Ki	5.61	CHEMBL
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		Ki	5.46	CHEMBL

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External reference:

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ID	Source
002300	NDDF
1012	INN_ID
10772	RXNORM
11473005	SNOMEDCT_US
3169	MMSL
4018612	VUID
4018612	VANDF
409112007	SNOMEDCT_US
5560	PUBCHEM_CID
5619	MMSL

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Pharmaceutical products:

None