Delving into the Latest Updates on Pizotifen with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pizotifen malate, Pizotyline

+ [4]

Target

5-HT receptor

Mechanism

5-HT receptor antagonists(Serotonin (5-HT) receptor antagonists)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesCardiovascular Diseases+ [2]

Active Indication

AngioedemaAtrial Premature ComplexesChronic Urticaria+ [3]

Inactive Indication-

Originator Organization

Phoenix Labs

Active Organization

Jinan Yongning Pharmaceutical Co. Ltd.

Paladin Labs, Inc.

Phoenix Labs

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

GB (15 Mar 1974),

Vascular Headaches

Regulation-

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Structure

Molecular FormulaC23H27NO5S

InChIKeyIWAWCPZVTXCFKD-UHFFFAOYSA-N

CAS Registry5189-11-7

View All Structures (2)

The goal of this clinical trial is to compare efficacy and observe common adverse effects of a combination of amitriptyline-propranolol and pizotifen as prophylactic treatments for migraine. The main question it aims to answer is:
• Does pizotifen more effective than the combination of amitriptyline-propranolol in migraine prophylaxis?
Participants will be asked to :
Maintain the provided headache diary accordingly
Take supplied drugs as described during clinical visits
Contact principle investigator if there is any issues regarding drug use and/or their adverse effects

Start Date19 Mar 2023

Sponsor / Collaborator

Bangabandhu Sheikh Mujib Medical University

ISRCTN97360154 / CompletedNot ApplicableIIT

A double-blind parallel-group randomised placebo-controlled trial of propranolol and pizotifen in preventing migraine in children

Start Date01 Jun 2009

Sponsor / Collaborator-

100 Clinical Results associated with Pizotifen

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100 Translational Medicine associated with Pizotifen

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100 Patents (Medical) associated with Pizotifen

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397

Literatures (Medical) associated with Pizotifen

01 Mar 2024·Chemistry & Biodiversity

Molecular Docking and GC/MS‐Based Approach for Identification of Anxiolytic Alkaloids from Griffinia (Amaryllidaceae) Species in a Zebrafish Model

Article

Author: Florêncio Martins, Natália ; Kueirislene Amâncio Ferreira, Maria ; de Cássia Alves Pereira, Rita ; Sheila de Queiroz Souza, Ana ; Marques Canuto, Kirley ; Silva Alencar de Menezes, Jane Eire ; Leite, Elder Luis Lima ; Riceli Vasconcelos Ribeiro, Paulo ; Deusdênia Loiola Pessoa, Otília ; Silva Dos Santos, Hélcio

AbstractGriffinia gardneriana Ravenna, Griffinia liboniana Morren and Griffinia nocturna Ravenna (Amarillydaceae) are bulbous plants found in tropical regions of Brazil. Our work aimed to determine the alkaloid profiles of Griffinia spp. and evaluate their anxiolytic potential through in vivo and in silico assays. The plants grown in greenhouses were dried and their ground bulbs were subjected to liquid‐liquid partitions, resulting in alkaloid fractions that were analyzed by gas chromatography coupled to mass spectrometry (GC‐MS). Anxiolytic activity was evaluated in zebrafish (Danio rerio) through intraperitoneal injection at doses of 40, 100 and 200 mg/kg in light‐dark box test. GC‐MS analyses revealed 23 alkaloids belonging to different skeleton types: lycorine, homolychorine, galanthamine, crinine, haemanthamine, montanine and narcisclasine. The chemical profiles were relatively similar, presenting 8 alkaloids common to the three species. The major component for G. gardneriana and G. liboniana was lycorine, while G. nocturna consisted mainly of anhydrolycorine. All three alkaloid fractions demonstrated anxiolytic effect. Furthermore, pre‐treatment with diazepam and pizotifen drugs was able to reverse the anxiolytic action, indicating involving the GABAergic and serotonergic receptors. Molecular docking showed that the compounds vittatine, lycorine and 11,12‐dehydro‐2‐methoxyassoanine had high affinity with both receptors, suggesting them to be responsible for the anxiolytic effect.

11 Feb 2024·Journal of Biomolecular Structure and Dynamics

Synthesis and anxiolytic effect of europium metallic complex containing lapachol [Eu(DBM) ₃ . LAP] in adult zebrafish through serotonergic neurotransmission: in vivo and in silico approach

Article

Author: Ferreira, Maria Kueirislene Amâncio ; de Menezes, Jorge Fernando Silva ; Sá Pires Silva, Andrei Marcelino ; dos Santos, Hélcio Silva ; Marinho, Gabrielle Silva ; Morais Bomfim De Lima, Julia ; Marinho, Emmanuel Silva ; Aparecida Faria de Almeida, Edna ; de Menezes, Jane Eire Silva Alencar ; da Silva, Antonio Wlisses ; da Silva, Ananias Freire ; Marques da Fonseca, Aluísio

Anxiety-related mental health problems are estimated at 3.6% globally, benzodiazepines (BZDs) are the class of drugs indicated for the treatment of anxiety, including lorazepam and diazepam. However, concerns have been raised about the short- and long-term risks associated with BZDs. Therefore, despite anxiolytic and antidepressant drugs, there is a need to develop more effective pharmacotherapies with fewer side effects than existing drugs. The present work reported the synthesis, anxiolytic activity, mechanism of action in Adult Zebrafish (Danio rerio) and in silico study of a europium metallic complex with Lapachol, [Eu(DBM)₃. LAP]. Each animal (n = 6/group) was treated intraperitoneally (i.p.; 20 µL) with the synthesized complex (4, 20 and 40 mg/Kg) and with the vehicle (DMSO 3%; 20 µL), being submitted to the tests of locomotor activity and 96h acute toxicity. The light/dark test was also performed, and the serotonergic mechanism (5-HT) was evaluated through the antagonists of the 5-HTR₁, 5-HTR_2A/2C and 5-HTR_3A/3B receptors. The complex was characterized using spectrometric techniques, and the anxiolytic effect of complex may be involved the neuromodulation of receptors 5-HT3A/3B, since the pre-treatment with pizotifen and cyproheptadine did not block the anxiolytic effect of [Eu(DBM)₃. LAP], unlike fluoxetine had its anxiolytic effect reversed. In addition, molecular docking showed interaction between the [Eu(DBM)₃. LAP] and 5HT_3A receptor with binding energy -7.8 kcal/mol and the ADMET study showed that complex has low toxic risk. It is expected that the beginning of this study will allow the application of the new anxiolytic drugs, given the pharmacological potential of the lapachol complex.Communicated by Ramaswamy H. Sarma.

01 Feb 2024·Science of The Total Environment

Pharmaceutical residues in stranded dolphins in the Bay of Biscay

Article

Author: Orive, Gorka ; Domingo-Echaburu, Saioa ; Brodin, Tomas ; Cerveny, Daniel ; Ruiz-Sancho, Leire ; Alzola-Andres, Maitane ; Lertxundi, Unax ; Lekube, Xabier

There is a growing concern about the presence of pharmaceuticals on the aquatic environment, while the marine environment has been much less investigated than in freshwater. Marine mammals are suitable sentinel species of the marine environment because they often feed at high trophic levels, have unique fat stores and long lifespan. Some small delphinids in particular serve as excellent sentinel species for contamination in the marine environment worldwide. To the best of our knowledge, no pharmaceuticals have been detected or reported in dolphins so far. In the present study, muscle, liver and blubber samples from three common dolphins (Delphinus delphis) and seven striped dolphins (Stenella coeruleoalba) stranded along the Basque Coast (northern Spain) were collected. A total of 95 pharmaceuticals based on detectability and predicted ability to bioaccumulate in fish were included in the liquid chromatography tandem mass spectrometry (LC-MS/MS) analysis. At least one pharmaceutical was found in 70 % of the individuals. Only three of the 95 monitored pharmaceuticals were detected in dolphin's tissues. Very low concentrations (<1 ng/g) of orphenadrine and pizotifen were found in liver and promethazine in blubber. Herein, the gap in the knowledge regarding the study organisms and marine environments with respect to pharmaceutical pollution, which demands further research to understand if pharmaceuticals are a threat for these apex predators, is highlighted and discussed.

100 Deals associated with Pizotifen

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External Link

KEGG	Wiki	ATC	Drug Bank
D08397	Pizotifen	N02CX01	DB06153

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Angioedema	CN	Jinan Yongning Pharmaceutical Co. Ltd.	01 Jan 1995
Atrial Premature Complexes	CN	Jinan Yongning Pharmaceutical Co. Ltd.	01 Jan 1995
Chronic Urticaria	CN	Jinan Yongning Pharmaceutical Co. Ltd.	01 Jan 1995
Ventricular Premature Complexes	CN	Jinan Yongning Pharmaceutical Co. Ltd.	01 Jan 1995
Migraine Disorders	CA	Paladin Labs, Inc.	01 Jan 1975
Vascular Headaches	GB	Phoenix Labs	15 Mar 1974