Delving into the Latest Updates on Cinnarizine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine, 1-Benzhydryl-4-cinnamylpiperazin, 1-Cinnamyl-4-(diphenylmethyl)piperazine

+ [11]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOtorhinolaryngologic Diseases

Active Indication

Cerebrovascular DisordersVertigo

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC26H28N2

InChIKeyDERZBLKQOCDDDZ-UHFFFAOYSA-N

CAS Registry298-57-7

The goal of this pilot, open-label prospective study is to evaluate if the effect of calcium channel blockade on plasma aldosterone levels in people with primary aldosteronism (PA) is due primarily to Cav1.3 blockade.
This will be tested by treating participants who have PA with both cinnarizine (Cav1.3 blocker) and nifedipine (Cav1.2 blocker) and evaluating effect on aldosterone levels and blood pressure over a two week course of treatment.

Start Date24 Apr 2023

Sponsor / Collaborator

Queen Mary University of London

IRCT20221108056444N1 / RecruitingPhase 3IIT

Comparison of the effectiveness of Cinnarizine V/S Topiramate in migraine prophylaxis of children referred to pediatric neurology clinic

Start Date23 Sep 2022

Sponsor / Collaborator-

IRCT20110628006907N16 / SuspendedPhase 3IIT

Interventional comparison of the effect of cinnarizine with placebo on mood swings and self-harm and stereotyped behaviors of autistic patients

Start Date20 Jan 2022

Sponsor / Collaborator

Tehran University of Medical Sciences

100 Clinical Results associated with Cinnarizine

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100 Translational Medicine associated with Cinnarizine

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100 Patents (Medical) associated with Cinnarizine

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1,071

Literatures (Medical) associated with Cinnarizine

01 Nov 2024·International Journal of Pharmaceutics

The Langmuir-Blodgett trough (Langmuir film balance) can be used to understand the stabilizer concentrations in aqueous nano- and microsuspensions

Article

Author: Holm, René ; Zulbeari, Nadina ; Lund, Frederik Wendelboe ; Mustafova, Sibel Selyatinova ; Simonsen, Adam Cohen

Aqueous suspensions of poorly soluble, crystalline drug particles in the sub-micron range hold the ability to regulate the drug release for a defined period of time after e.g., intramuscular, or subcutaneous administration, working as an eminent formulation strategy for the preparation of long-acting injectables. Aqueous suspensions are typically prepared by top-down approaches, e.g., wet bead media milling or high-pressure homogenization, containing the active pharmaceutical compound and surfactants and/or polymers for stabilization purposes. Currently, the screening of proper stabilizers and adequate stabilizer concentration during formulation investigations is based on a trial-and-error approach with variations in combinations, concentrations, and/or ratios. To obtain a more efficient methodology during formulation screening, the present study investigated the correlation between the surface activity of two different surfactants, i.e., poloxamer 188 and polysorbate 20, by drop profile tensiometry and Langmuir trough monolayer, and the obtained sizes of cinnarizine particles as a tool to predict the optimal surfactant concentration to prepare physical stable nano- and microsuspensions. The obtained results demonstrated that the molecular area determined as the area per surfactant molecule measured in the Langmuir trough combined with the specific surface area of the prepared suspensions could be used to predict the suitable concentration of the surfactant based upon short-term stress stability data. The results further showed that higher concentrations of poloxamer 188 were necessary to stabilize the suspensions when compared to the needed concentration of polysorbate 20. In addition, it was observed that there was a need for a slightly higher surfactant concentration when the suspensions were milled with the smallest bead size of 0.5 mm instead of larger sizes of bead (0.8 and 1.0 mm), which could not be accounted for by differences in specific surface area.

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

ChlorTox scale assessment, greenness, and whiteness evaluation of selective spectrophotometric analysis of dimenhydrinate and cinnarizine

Article

Author: Morgan, Eman M ; Fayez, Yasmin M ; Obaydo, Reem H ; Boltia, Shereen A ; Lotfy, Hayam M ; Abdelkawy, M

Nausea and vomiting are considered common series side effects induced by chemotherapy treatment in cancer patients. This annoying side effect can impair the patient's compliance to cancer treatment and affect their quality of life. Dimenhydrinate and cinnarizine in combined pharmaceutical dosage form is used to control chemotherapy induced nausea and vomiting in cancer patients. For safety, selective spectrophotometric methods based on novel dual resolution strategies were introduced to estimate dimenhydrinate and cinnarizine in presence of their harmful impurities namely benzophenone and 1- (diphenylmethyl)piperazine, respectively. These methods namely, dual ratio difference (DRD), dual ratio extraction (DRE) and dual absorbance extraction coupled with dual ratio extraction (DAE-DRE) were successfully performed to simultaneously analyze the drug of interests dimenhydrinate and cinnarizine in their pure form, synthetic mixtures and in market dosage form. Linearity ranges were 6.0-60.0 μg/mL and 3.0-30.0 μg/mL for dimenhydrinate and cinnarizine, respectively with good recovery% of Mean ± SD for all the proposed methods 99.82 ± 0.48, 99.79 ± 0.40, 100.14 ± 0.82, 100.03 ± 0.69, respectively. ICH guidelines were adhered in accordance with confirming validation of the proposed methods where fulfilling results were accomplished. Various unified greenness and whiteness assessment tools, such as the chlorTox scale, greenness index via spider chart, AGREE (The Analytical Greenness Metric), green certificate, and the RGB12 algorithm were employed in this research to assess the greenness and sustainability of the introduced UV-spectrophotometric methods in comparison to the reported HPLC method. As a result, these methods hold significant potential for utilization in the quality control department of pharmaceutical companies, contributing to enhanced pharmaceutical product analysis and overall sustainability practices.

16 Jul 2024·ACS Omega

Antihistamines H₁ as Potential Anthelmintic Agents against the Zoonotic Parasite Angiostrongylus cantonensis

Article

Author: Roquini, Daniel B. ; Fernandes, João Paulo S. ; Lopes, Flavia B. ; Kreutz, Amanda L. B. ; Amaro, Monique C. ; de Moraes, Josué ; Spoladore, Sophia C. ; Lemes, Bruna L.

Infections caused by parasitic helminths pose significant health concerns for both humans and animals. The limited efficacy of existing drugs underscores the urgent need for novel anthelmintic agents. Given the reported potential of antihistamines against various parasites, including worms, this study conducted a screening of clinically available antihistamines against Angiostrongylus cantonensis-a nematode with widespread implications for vertebrate hosts, including humans. Twenty-one anti-H₁ antihistamines were screened against first-stage larvae (L₁) of A. cantonensis obtained from the feces of infected rats. Standard anthelmintic drugs ivermectin and albendazole were employed for comparative analysis. The findings revealed four active compounds (promethazine, cinnarizine, desloratadine, and rupatadine), with promethazine demonstrating the highest potency (EC₅₀ = 31.6 μM). Additionally, morphological analysis showed that antihistamines induced significant changes in larvae. To understand the mechanism of action, antimuscarinic activities were reported based on average pK _i values for human muscarinic receptor (mAChR) subtypes of the evaluated compounds. Furthermore, an analysis of the physicochemical and pharmacodynamic properties of antihistamines revealed that their anthelmintic activity does not correlate with their activity at H1 receptors. This study marks the first documentation of antihistamines' activity against A. cantonensis, offering a valuable contribution to the quest for novel agents effective against zoonotic helminths.

100 Deals associated with Cinnarizine

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