Delving into the Latest Updates on Trichlormethiazide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Trichlormethiazide (JP17/USP/INN), Achletin

+ [10]

Target

NCC

Action

inhibitors

Mechanism

NCC inhibitors(Thiazide-sensitive sodium-chloride cotransporter inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Heart FailureHypertension

Inactive Indication

Edema

Originator Organization

Merck & Co., Inc.

Active Organization

Shionogi & Co., Ltd.

Inactive Organization

Schering Corp.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (09 Mar 1960),

EdemaHypertension

Regulation-

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Structure/Sequence

Molecular FormulaC8H8Cl3N3O4S2

InChIKeyLMJSLTNSBFUCMU-UHFFFAOYSA-N

CAS Registry133-67-5

Influence of Multidrug resistance protein 4 (MRP4) on serum uric acid levels and uric acid clearance after multiple administration of trichlormethiazide in Japanese healthy volunteers: open-label study - Influence of MRP4 on serum uric acid levels and uric acid clearance after multiple administration of trichlormethiazide

Start Date02 Jul 2013

Sponsor / Collaborator-

JPRN-JMA-IIA00183

/ CompletedNot ApplicableIIT

Clinical study about the hypotensive effect and the inhibitory effect on the elevatin of uric acid level irbesartan and trichlormethiazide in the essential hypertension patients

Start Date01 Jan 2013

Sponsor / Collaborator-

JPRN-UMIN000007013

/ CompletedNot ApplicableIIT

Effect of single dose administration of trichlormethiazide on the serum level and clearance of uric acid: open-label controlled dose-escalating trial with healthy Japanese male volunteers - Effect of single dose administration of trichlormethiazide on the serum level and clearance of uric acid

Start Date01 Jan 2012

Sponsor / Collaborator-

100 Clinical Results associated with Trichlormethiazide

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100 Translational Medicine associated with Trichlormethiazide

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100 Patents (Medical) associated with Trichlormethiazide

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716

Literatures (Medical) associated with Trichlormethiazide

01 Apr 2025·Hypertension Research

Home blood pressure-lowering effect of esaxerenone vs trichlormethiazide for uncontrolled hypertension: a prespecified subanalysis of the EXCITE-HT randomized controlled study by age subgroup

Article

Author: Katsuya, Tomohiro ; Nagashima, Hirotaka ; Tanabe, Ayumi ; Hashimoto, Masami ; Shimosawa, Tatsuo ; Itabashi, Naoki ; Miyamoto, Takahide ; Taguchi, Takashi ; Ishida, Hidenori ; Ebe, Yusuke ; Uchiyama, Kazuaki ; Hatta, Tsuguru ; on behalf of the EXCITE-HT investigators ; Fukui, Toshiki ; Kato, Mitsutoshi ; Kario, Kazuomi ; Ohishi, Mitsuru ; Ohbayashi, Hiroyuki ; Nakamura, Noriko ; Hirano, Kunio

AbstractThis predefined subanalysis of the multicenter, randomized, open-label, parallel-group EXCITE-HT study aimed to determine whether the comparative efficacy and safety of esaxerenone and trichlormethiazide differs with age. Patients were divided into two age subgroups (<65 and ≥65 years). The non-inferiority of esaxerenone to trichlormethiazide was assessed based on the upper limit of the two-sided 95% confidence interval (CI) for the difference in systolic/diastolic blood pressure (SBP/DBP) changes. Esaxerenone was considered non-inferior if this value was <3.9/ < 2.1 mmHg; if it was <0 mmHg, esaxerenone was considered superior in its BP-lowering effect. The results showed that the least squares mean changes in morning home SBP/DBP from baseline to the end of treatment (primary endpoint) were −9.5/−5.7 with esaxerenone and −8.2/−4.9 mmHg with trichloromethiazide (between-group difference: −1.3 [95% CI, −3.3, 0.8]/−0.8 [ − 2.1, 0.5] mmHg) in the subgroup aged <65 years. These changes were −14.6/−7.2 and −11.5/−6.7 (−3.0 [−4.9, −1.2]/−0.5 [−1.5, 0.5] mmHg) in the subgroup aged ≥65 years. The incidences of serum potassium level ≥5.5 mEq/L were 2.2% and 1.9% in the esaxerenone-treated subgroups aged <65 and ≥65 years, respectively. In conclusion, esaxerenone achieved the pre-defined non-inferiority margin to trichlormethiazide in its BP-lowering effect regardless of age. In patients aged <65 years, esaxerenone achieved the non-inferiority margin to trichlormethiazide in lowering both SBP and DBP. In patients aged ≥65 years, esaxerenone was superior to trichlormethiazide in lowering SBP and achieved the non-inferiority margin to trichlormethiazide in lowering DBP. The impact of esaxerenone on serum potassium levels did not show a specific age-related effect.

01 Feb 2025·Hypertension Research

Home blood pressure-lowering effect of esaxerenone versus trichlormethiazide for uncontrolled hypertension: a predefined subanalysis of the EXCITE-HT randomized controlled trial by basal calcium channel blocker versus angiotensin receptor blocker

Article

Author: Shimosawa, Tatsuo ; Nagashima, Hirotaka ; Tanabe, Ayumi ; Hashimoto, Masami ; Itabashi, Naoki ; Miyamoto, Takahide ; Taguchi, Takashi ; Ishida, Hidenori ; Ebe, Yusuke ; Katsuya, Tomohiro ; Uchiyama, Kazuaki ; Hatta, Tsuguru ; on behalf of the EXCITE-HT investigators ; Kato, Mitsutoshi ; Fukui, Toshiki ; Kario, Kazuomi ; Ohishi, Mitsuru ; Ohbayashi, Hiroyuki ; Nakamura, Noriko ; Hirano, Kunio

AbstractThis prespecified subanalysis of the multicenter, randomized, open-label, parallel-group EXCITE-HT study aimed to examine the non-inferiority of esaxerenone to trichlormethiazide as a second-line antihypertensive agent according to the basal antihypertensive agent used (angiotensin receptor blocker [ARB] or calcium channel blocker [CCB]). The primary endpoint, change in morning home systolic/diastolic blood pressure (SBP/DBP) from baseline to end of treatment was similar between the two groups (intergroup difference in least squares mean change [95% confidence interval]: −1.3 [−3.8, 1.3]/−0.2 [−1.6, 1.3] mmHg for ARB; −2.7 [−4.2, −1.2]/−0.8 [−1.7, 0.1] mmHg for CCB). The respective incidences of serum potassium levels <3.5 mEq/L and ≥5.5 mEq/L in the ARB subgroup were 3.4% and 4.2% for esaxerenone and 7.9% and 0% for trichlormethiazide; in the CCB subgroup, they were 2.8% and 0.6% for esaxerenone and 13.9% and 1.2% for trichlormethiazide, respectively. The incidence of uric acid level ≥7.0 mg/dL was numerically higher in the trichlormethiazide group than the esaxerenone group in both the ARB and CCB subgroups. The non-inferiority of esaxerenone to trichlormethiazide in lowering morning home BP was demonstrated regardless of whether the basal antihypertensive agent was an ARB or CCB. Esaxerenone with a CCB showed superiority to trichlormethiazide in lowering SBP, without any new safety concerns. Serum potassium levels tended to be higher when esaxerenone was combined with an ARB than with a CCB, but this can be mitigated if administered according to the package insert.

01 Jan 2025·Journal of Hypertension

Mechanisms of thiazide-induced hypertension treatment: insights from gene expression and histological analysis in malignant stroke-prone spontaneously hypertensive rats

Article

Author: Khan, Malik W.Z. ; Nawaz, Muhammad Usama ; Fatima, Syeda Mashal ; Khan, Saad ; Ahmad, Bilal

Chloromethiazide (TCM) on malignant stroke-prone spontaneously hypertensive rats (M-SHRSPs), specifically the effects on blood pressure, survival rates, and gene expression.The article shows that high-dose trichloromethiazide (TCM) lowers SBP and increases survival in MSHRSPs, while low-dose TCM has no effect. The benefits are linked to gene changes that reduce oxidative stress.Adding control groups treated with other antihypertensive drugs could provide valuable comparison data and insights into TCM′s mechanisms.Addnl., key data points are overlooked, such as potential adverse effects of TCM and a broader histol. evaluation of organs like the heart and liver, which could reveal more about systemic impacts.Addnl., some studies suggest that while thiazide diuretics may reduce cardiovascular morbidity, they might not significantly impact overall mortality and may also be associated with increased risk of progression of diabetes mellitus.In conclusion, provide valuable insights into the mechanisms of TCM in hypertension, the study′s limitations highlight the necessity for further research.

100 Deals associated with Trichlormethiazide

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External Link

KEGG	Wiki	ATC	Drug Bank
D00658	Trichlormethiazide	C03AA06	DB01021

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Heart Failure	Japan	Shionogi & Co., Ltd.	22 Aug 1960
Hypertension	Japan	Shionogi & Co., Ltd.	22 Aug 1960

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


GUARD study (ESH2012)	Not Applicable	Diabetes Mellitus \| Hypertension	-	Olmesartan + Azelnidipine	(svezeaaagl) = wrtbpllqse zqlxtvdbzm (wpxgkhapwj )	Positive	01 Sep 2012
				Olmesartan + Trichlormethiazide	(svezeaaagl) = vajaelwqqw zqlxtvdbzm (wpxgkhapwj )