Delving into the Latest Updates on Pilsicainide Hydrochloride Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Alisrythm, Pilsicainide, Pilsicainide Hydrochloride

+ [13]

Target

Sodium channels

Action

blockers

Mechanism

Sodium channels blockers

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Arrhythmias, Cardiac

Inactive Indication-

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Daiichi Sankyo Korea Co., Ltd.

Daiichi Sankyo Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (29 Mar 1991),

Arrhythmias, Cardiac

Regulation-

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Structure/Sequence

Molecular FormulaC17H24N2O

InChIKeyBCQTVJKBTWGHCX-UHFFFAOYSA-N

CAS Registry88069-67-4

View All Structures (2)

The multicenter study of rhythm-control drugs in patients with paroxysmal atrial fibrillation: Comparison of the efficacy of flecainide or pilsicainide in patients with symptomatic paroxysmal atrial fibrillation - The multicenter study of rhythm-control drugs in patients with paroxysmal atrial fibrillation

Start Date01 Aug 2011

Sponsor / Collaborator-

100 Clinical Results associated with Pilsicainide Hydrochloride Hydrate

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100 Translational Medicine associated with Pilsicainide Hydrochloride Hydrate

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100 Patents (Medical) associated with Pilsicainide Hydrochloride Hydrate

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377

Literatures (Medical) associated with Pilsicainide Hydrochloride Hydrate

21 Feb 2025·Biological and Pharmaceutical Bulletin

<i>α</i><sub>1</sub>-Adrenoceptor Blockade by Class I Antiarrhythmic Drugs in Guinea Pig Thoracic Aorta as Revealed by Mechanical and Fluorescence Displacement Analysis

Article

Author: Tanaka, Hikaru ; Igarashi, Hiro ; Namekata, Iyuki ; Shirai, Kuniaki ; Kawazoe, Ayaka ; Tsukada, Kohei ; Seki, Maika ; Hamaguchi, Shogo ; Miyahara, Marina

The effects of thirteen Vaughn Williams class I antiarrhythmic drugs on the α₁-adrenergic receptor-mediated contraction were examined in thoracic aorta tissue preparations isolated from the guinea pig. Cibenzoline, quinidine, aprindine, and ranolazine, as well as prazosin, inhibited the phenylephrine-induced contraction with pA₂ values of 5.64, 5.59, 5.61, 5.08, and 8.50, respectively, but not prostaglandin F_2α-induced. These drugs reduced the staining of the smooth muscle layer by fluorescent prazosin. Propafenone inhibited the phenylephrine-induced contraction with an apparent pA₂ value of 5.31 and reduced the staining by fluorescent prazosin, but also inhibited the prostaglandin F_2α-induced contraction. Other class I antiarrhythmic drugs, disopyramide, pirmenol, procainamide, lidocaine, mexiletine, flecainide, pilsicainide, and GS-458967, affected neither the contraction by phenylephrine nor the fluorescent staining by prazosin. These results indicate that among the class I antiarrhythmic drugs, cibenzoline, aprindine, and propafenone, as well as quinidine and ranolazine, have α₁-adrenoceptor-blocking activity at therapeutically relevant concentrations.

01 Feb 2025·Chemosphere

A biomarkers study of human skin fibroblasts exposition to glyphosate-based herbicide using an untargeted and targeted metabolomics approach

Article

Author: Cardeal, Zenilda L ; Gomes, Dawidson A ; Batista, Josimar M ; Menezes, Helvécio C ; Rodrigues, Michele A ; Armijos, María J G

Metabolomics is a valuable tool to assess glyphosate exposure and its potential impact on human health. However, few studies have used metabolomics to evaluate human exposure to glyphosate or glyphosate-based herbicides (GBHs). In this study, an untargeted and targeted metabolomics approach was applied to human skin fibroblasts exposed to the GBH Roundup (GLYP-R). Cytotoxicity, cell death, and oxidative stress assays were performed to evaluate potential damage caused by GLYP-R in fibroblasts. The herbicide showed a cytotoxic effect at concentrations above 100.0 mg L^-1, with IC₅₀ = 164.2 ± 8.7 mg L^-1, inducing significant reactive oxygen species (ROS) production and necrosis. A GC×GC/Q-TOFMS method using derivatization with propyl chloroformate/propanol was developed for untargeted analysis, allowing the identification of 400 metabolites of different classes in the samples. The most significant compounds in the discrimination and classification of the samples were fatty acids and amino acids (AA). Based on the relevance of AA in untargeted analysis, a targeted analysis of 21 AA was performed using the same validated GC×GC method. Metabolomic analyses allowed the construction of two biomarker models with performance evaluated by receiver operating characteristic (ROC) curves: an untargeted model formed by four metabolites (methylcysteine, N-acetyl-l-methionine, methyl stearate, and linoleic acid) and a targeted model formed by three AA (l-glutamic acid, l-cysteine, and γ-aminobutyric acid). This study is the first to report the use of metabolomics to evaluate human skin cells exposed to GLYP-R, contributing to the toxicological research on glyphosate.

01 Oct 2024·Heart Rhythm

Risk stratification for the occurrence of ventricular fibrillation in patients with early repolarization syndrome

Article

Author: Nishii, Nobuhiro ; Kawada, Satoshi ; Ueoka, Akira ; Mizuno, Tomofumi ; Yuasa, Shinsuke ; Nakagawa, Koji ; Masuda, Takuro ; Asada, Saori ; Morita, Hiroshi ; Miyamoto, Masakazu

BACKGROUNDSeveral signs of malignant early repolarizations have been proposed in patients with early repolarization syndrome (ERS). However, reports have challenged the efficacy of these signs in predicting future ventricular fibrillation (VF) in patients with ERS.OBJECTIVEThis study aimed to assess the predictive value of various electrocardiogram (ECG) markers for future VF events in patients with ERS.METHODSWe retrospectively evaluated the clinical characteristics of 44 patients with ERS to identify risk factors for VF during follow-up.RESULTSAfter the initial event, 16 patients experienced VF (VF group), whereas 28 did not (non-VF group). The VF group had a longer QRS interval, more fragmented QRS (fQRS), and a higher T/R voltage ratio than the non-VF group. Wide J waves were more prevalent in the VF group; however, other J-wave markers did not differ between the groups. Positive late potentials recorded on signal-averaged ECGs were more frequent in the VF group. Whereas none of the patients showed spontaneous Brugada syndrome on ECG, the VF group frequently exhibited pilsicainide-induced ST-segment elevation. These ECG markers were significantly associated with the occurrence of VF during follow-up. Patients with multiple ECG factors, including QRS abnormalities (wide QRS or fQRS), wide J waves, and a high T/R ratio, had a worse prognosis than patients without multiple factors, effectively stratifying patient risk.CONCLUSIONThe occurrence of VF in patients with ERS may be associated with conduction abnormalities such as QRS widening, fQRS, high T/R ratio, positive late potentials, and pilsicainide test results. Therefore, ECG factors could be useful in identifying high-risk patients.

100 Deals associated with Pilsicainide Hydrochloride Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01554	Pilsicainide Hydrochloride Hydrate	C01BC	DB12712

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Arrhythmias, Cardiac	Japan	Daiichi Sankyo Co., Ltd.	29 Mar 1991

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASN2019	Not Applicable	Drug intoxication creatinine	-	Pilsicainide Hydrochloride (Hemodialysis)	(auswirqrve) = qphdjfjwty mbwobrfdqn (pdmxgekkan )	Negative	05 Nov 2019