Delving into the Latest Updates on Barnidipine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Barnidipine, Barnidipine hydrochloride (JAN), Cyress

+ [15]

Target

Cav2.1

Action

inhibitors

Mechanism

Cav2.1 inhibitors(calcium voltage-gated channel subunit alpha1 A inhibitors)

Therapeutic Areas

Cardiovascular DiseasesUrogenital Diseases

Active Indication

Essential HypertensionHypertension, RenovascularParenchymal renal hypertension+ [1]

Inactive Indication-

Originator Organization

Japan Established Medicine Corp

Active Organization

LTL Pharma Co., Ltd.

Daiichi Sankyo Co., Ltd.Japan Established Medicine Corp

+ [2]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (01 Jan 1992),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC27H30ClN3O6

InChIKeyXEMPUKIZUCIZEY-YSCHMLPRSA-N

CAS Registry104757-53-1

View All Structures (2)

BackgroundChronic inflammation is a well-recognized contributor to hypertension pathogenesis. However, the role of targeting inflammation in hypertension treatment, particularly through modulation of inflammatory markers like interleukin-6 (IL-6), remains less understood. We investigated the effects of antihypertensive medications with and without IL-6-lowering properties on long-term blood pressure (BP) control in a multi-ethnic cohort in the Netherlands.MethodsParticipants from HELIUS cohort receiving hypertension treatment were followed over six years. BP control at follow-up was determined using WHO criteria. Due to unavailability of IL-6 data, a literature review was conducted to classify antihypertensives based on their IL-6-lowering properties - a proxy approach. Logistic regression models were used to assess associations between the IL-6-lowering potential of antihypertensives and BP control, both within and between antihypertensive classes. Effect modification by ethnicity was explored.ResultsA total of 1510 participants were included (mean age 57 years, 62 % women). Within the calcium channel blocker (CCB) class, medications with IL-6-lowering properties (amlodipine and barnidipine) were associated with superior BP control (aOR 1.41, 95 % confidence interval 1.05-1.90) compared to other CCBs (lercanidipine, nifedipine, verapamil, clevidipine, diltiazem). No significant associations were observed within angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs), between different antihypertensive drug classes, nor across ethnic groups.ConclusionAmlodipine and barnidipine were associated with better BP control compared to other CCBs. Our findings provide an important starting point for understanding the role of IL-6 in hypertension management. Further studies are warranted to confirm these observations by directly measuring IL-6 levels and investigating underlying mechanisms.

01 Jan 2025·Clinical Rheumatology

Barnidipine as a potential alternative treatment for Raynaud's phenomenon secondary to systemic sclerosis: a retrospective pilot study

Article

Author: Luca, Idolazzi ; Bertelle, Davide ; Di Donato, Stefano ; Mastropaolo, Francesca ; Viapiana, Ombretta ; Bixio, Riccardo ; Rossini, Maurizio ; Morciano, Andrea ; Bertoldo, Eugenia ; Adami, Giovanni ; Appoloni, Matteo

OBJECTIVESTo assess short-term barnidipine efficacy and tolerability on Systemic Sclerosis (SSc)-Raynaud's phenomenon (RP).METHODSWe retrospectively evaluated patients with SSc starting barnidipine 10 mg/day. Raynaud's Condition Score (RCS) and mean blood pressure (MBP) were assessed at baseline and 6-month follow-up. Discontinuation rates and adverse events (AEs) were compared with retrospectively evaluated patients who started MR-nifedipine 20 mg/day at our centre.RESULTSSixty-four patients (29 barnidipine, 35 MR-nifedipine) were evaluated. Most patients starting barnidipine had a previous CCB exposure (69%; 57.9% of these were withdrawn for AEs). During follow-up, RCS decreased significantly (6.6 ± 1.8 vs 4.4 ± 1.8, p < 0.001), while the MBP did not change significantly (86.4 ± 8.4 vs 85 ± 7.3 mmHg; p = 0.36). Nine patients (31%) discontinued barnidipine during the follow-up (AEs 6/9, inefficacy 3/9). Previous CCB failure did not predict barnidipine withdrawal (OR = 0.188 95%CI [0.02-1.8]; p = 0.147). No predictors of barnidipine withdrawal were found, and no clinical or demographic differences were found between patients withdrawing and continuing barnidipine. The 6-month retention rates of barnidipine and MR-nifedipine did not differ significantly (69 vs 80%; log-rank p = 0.23), and the two groups had a similar incidence of AEs leading to discontinuation (20.1 vs 17%; p = 0.48).CONCLUSIONSBarnidipine could be an effective and well-tolerated therapeutic option to treat SSc-RP, even in patients previously failing other CCBs. Key Points • Calcium channel blockers (CCBs) currently represent the first-line treatment for Raynaud's phenomenon secondary to Systemic Sclerosis (SSc-RP). However, little data exists about using novel CCBs, such as barnidipine, in this condition. • This study retrospectively evaluated patients with SSc-RP treated with barnidipine to assess its short-term efficacy. To serve as a control group for tolerability, we retrospectively compared these patients with others starting modified release-nifedipine (MR-nifedipine). • In patients treated with barnidipine, we observed a significant decrease in Raynaud's condition score at the 6-month follow-up without substantial changes in mean blood pressure. • The proportion of adverse events and drug withdrawal rate between patients starting barnidipine and MR-nifedipine did not differ significantly, even in patients starting barnidipine after previously failing other CCBs.

01 Apr 2024·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Ginseng root extract-mediated synthesis of monodisperse silver nanoparticles as a fluorescent probe for the spectrofluorometric determination of nilvadipine; Evaluation of remarkable anti-bacterial, anti-fungal and in-vitro cytotoxic activities

Article

Author: Rabie Shehab El-Din, Eman M ; El-Emam, Ali A ; El-Semary, Mariam S ; El-Masry, Amal A ; Belal, F

Nanoparticles are a boon for humanity because of their improved functionality and unlimited potential applications. Considering this significance, the proposed study introduced a simple, fast and eco-friendly method for synthesis of fluorescent silver nanoparticles (Ag-NPs) using Panax Ginseng root extract as a reducing and capping agent. Synthesis of Ag-NPs was performed in one step within three minutes utilizing microwave irradiation. The resulting Ag-NPs were characterized using various microscopic and spectroscopic techniques such as, Transmission Electron Microscope (TEM), UV/Visible spectroscopy, Fourier Transform Infrared Spectroscopy(FTIR) and Energy Dispersive X-ray analysis (EDX). The prepared Ag-NPs, which act as a fluorescent nano-probe with an emission band at 416 nm after excitation at 331 nm, were used to assay nilvadipine (NLV) spectrofluorimetrically in its pharmaceutical dosage form with good sensitivity and reproducibility. The proposed study is based on the ability of NLV to quantitatively quench the native Ag-NPs fluorescence, forming a ground state complex as a result of static quenching and an inner filter mechanism. The suggested approach displayed a satisfactory linear relationship throughout a concentration range of 5.0 μM - 100.0 μM, with LOD and LOQ values of 1.18 μM and 3.57 μM, respectively. Validation of the suggested approach was examined in accordance with ICH recommendations. In addition, the anti-bacterial and anti-fungal activities of the prepared nanoparticles were investigated, and they demonstrated effective anti-microbial activities and opened a future prospective to combat future antibiotic resistance. Finally, in-vitro cytotoxicity assay of Ag-NPs against normal and cancerous human cell lines was studied using MTT assay. The results proved the potential use of the produced Ag-NPs as an adjunct to anticancer treatment or for drug delivery without significantly harming healthy human cells.

100 Deals associated with Barnidipine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D01104	Barnidipine Hydrochloride	C08CA12	DB09227

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Essential Hypertension	Netherlands	ADOH B.V	11 Jul 2000
Hypertension, Renovascular	Japan	LTL Pharma Co., Ltd.	07 Sep 1994
Parenchymal renal hypertension	Japan	LTL Pharma Co., Ltd.	03 Jul 1992
Hypertension	Japan	Japan Established Medicine Corp	01 Jan 1992

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


EULAR2024	Not Applicable	Scleroderma, Systemic	-	Barnidipine 10mg/day	mjutkjwgpi(iqzlttncyk) = The two groups had a similar incidence of AEs leading to discontinuation (20.1 vs 17%), the most commonly reported being headache (38.5%), hypotension (30.8%), palpitations, flushing, and edema (7.7% each). No serious AE was reported in any group. cxdkjzzgux (fhclzeetmb )	-	05 Jun 2024
				MR-nifedipine 20mg/day
[PP.35.33] (ESH2015)	Not Applicable	Diabetes Mellitus, Type 2 \| Hypertension fasting plasma glucose \| glycated hemoglobin \| high-sensitivity C-reactive protein ... View more	151	Barnidipine 20 mg/day + Losartan 100 mg/day	(zcbhrkcbzw) = whpllhplfa yjxpjuzfkl (imjvfnpcwm ) View more	Positive	01 Jun 2015
				Lercanidipine 20 mg/day + Losartan 100 mg/day	(zcbhrkcbzw) = vkcaphyrmx yjxpjuzfkl (imjvfnpcwm ) View more
ASN2014	Not Applicable	Hypertension aldosterone \| renin \| cortisol ... View more	-	Spironolactone 50mg	(gupmpuzbsc) = dhonktavxu qkpbbdascw (woyobofbdd, 10.8)	Positive	11 Nov 2014
				Barnidipine 15mg	(gupmpuzbsc) = lubgkcnnkq qkpbbdascw (woyobofbdd, 13.8)