Amiodarone, a multi-channel blocker, enhances anticonvulsive effect of carbamazepine in the mouse maximal electroshock model

2018 ◽  
Vol 140 ◽  
pp. 105-110 ◽  
Author(s):  
Monika Banach ◽  
Monika Popławska ◽  
Kinga K. Borowicz-Reutt
Keyword(s):  
Channel Blocker ◽  
Maximal Electroshock ◽  
Anticonvulsive Effect

scholarly journals Screening Study for Anticonvulsive Activity of Lipophilic Fractions from Empetrum nigrum L.

2020 ◽  
Vol 6 (3) ◽  
pp. 67-74
Author(s):  
Ekaterina A. Bezverkhniaia ◽  
Tatyana N. Povet’eva ◽  
Tatyana V. Kadyrova ◽  
Nikolai I. Suslov ◽  
Yuliya V. Nesterova ◽  
...  
Keyword(s):  
Survival Rate ◽  
Chloroform Extract ◽  
Positive Control ◽  
Control Group ◽  
Maximal Electroshock ◽  
Anticonvulsive Activity ◽  
Neuroprotective Effects ◽  
Empetrum Nigrum ◽  
Mes Test ◽  
Anticonvulsive Effect

Introduction: The plants of genus Empetrum, which are used in the traditional medicine to cure seizures and neurodegenerative diseases, can be considered as potent antiepileptic drugs. This paper focuses on a comparative analysis of an anticonvulsive activity of lipophilic fractions from Empetrum nigrum L. Materials and methods: The experiments were conducted using mature outbred CD-1 male mice. The lipophilic fractions from aerial parts of Empetrum nigrum L. were administered through a catheter into the stomach at a dose of 150 mg/kg for 5 days. The anticonvulsive effects were studied using the acute seizure tests: strychnine-, pentylenetetrazole – and maximal electroshock (MES) induced tests. Carbamazepine was used as a positive control drug at a dose of 100 mg/kg. Results and discussion: The acetone-soluble fraction (ASF) of the chloroform extract from Empetrum nigrum L. showed a pronounced anticonvulsive effect on seizures induced by strychnine (1.5 mg/kg) and pentylenetetrazole (150 mg/kg). In comparison to the control group, the time from seizures to death increased by 1.5 for the strychnine-induced seizures, and 1.9 times in case of pentylenetetrazole model. The survival rate of the animals was 22.2% and 20%, correspondingly. The survival rate in the MES test was 77.8%. Overall, ASF demonstrates a remarkable anticonvulsive activity in all the tests, especially in the MES test. Conclusion: Our study for the first time shows a potent antiepileptic effect of ASF from Empetrum nigrum L., containing triterpene compounds and chalcones. The future studies will be focused on investigating the exact mechanisms of anticonvulsive and neuroprotective effects of ASF.

scholarly journals Amiodarone Enhances Anticonvulsive Effect of Oxcarbazepine and Pregabalin in the Mouse Maximal Electroshock Model

2021 ◽  
Vol 22 (3) ◽  
pp. 1041
Author(s):  
Monika Banach ◽  
Monika Rudkowska ◽  
Agata Sumara ◽  
Kinga Borowicz-Reutt
Keyword(s):  
Antiepileptic Drugs ◽  
Antiarrhythmic Drug ◽  
Molecular Mechanisms ◽  
Experimental Studies ◽  
Avoidance Task ◽  
Maximal Electroshock ◽  
Main Metabolite ◽  
Brain Concentration ◽  
Anticonvulsive Effect ◽  
The Brain

Accumulating experimental studies show that antiarrhythmic and antiepileptic drugs share some molecular mechanisms of action and can interact with each other. In this study, the influence of amiodarone (a class III antiarrhythmic drug) on the antiseizure action of four second-generation antiepileptic drugs was evaluated in the maximal electroshock model in mice. Amiodarone, although ineffective in the electroconvulsive threshold test, significantly potentiated the antielectroshock activity of oxcarbazepine and pregabalin. Amiodarone, given alone or in combination with oxcarbazepine, lamotrigine, or topiramate, significantly disturbed long-term memory in the passive-avoidance task in mice. Brain concentrations of antiepileptic drugs were not affected by amiodarone. However, the brain concentration of amiodarone was significantly elevated by oxcarbazepine, topiramate, and pregabalin. Additionally, oxcarbazepine and pregabalin elevated the brain concentration of desethylamiodarone, the main metabolite of amiodarone. In conclusion, potentially beneficial action of amiodarone in epilepsy patients seems to be limited by neurotoxic effects of amiodarone. Although results of this study should still be confirmed in chronic protocols of treatment, special precautions are recommended in clinical conditions. Coadministration of amiodarone, even at low therapeutic doses, with antiepileptic drugs should be carefully monitored to exclude undesired effects related to accumulation of the antiarrhythmic drug and its main metabolite, desethylamiodarone.

scholarly journals Semicarbazone – a versatile therapeutic pharmacophore for fragment based anticonvulsant drug design

2012 ◽  
Vol 62 (3) ◽  
pp. 263-286 ◽  
Author(s):  
Surendra Nath Pandeya
Keyword(s):  
Hydrogen Bonding ◽  
Antiepileptic Drug ◽  
Channel Blocker ◽  
Anticonvulsant Drug ◽  
Maximal Electroshock ◽  
Sodium Channel Blocker ◽  
Gaba Transaminase ◽  
Protective Index ◽  
Structure Activity ◽  
Oral Screen

During the last fifteen years, semicarbazones have been extensively investigated for their anticonvulsant properties. 4-(4-Flurophenoxy) benzaldehyde semicarbazone (C0102862, V102862) was discovered as a lead molecule and is being developed as a potent antiepileptic drug, with maximal electroshock (MES) ED50 of i.p. 12.9 mg kg-1. In MES (oral screen), this compound has a protective index (PI = TD50/ED50 > 315) higher than carbamazepine (PI 101), phenytoin (PI > 21.6) and valproate (PI 2.17). The compound is a potent sodium channel blocker. Other semicarbazones have demonstrated activity in various chemoshock screens, like subcutaneous pentylenetetrazole, subcutaneous strychnine, subcutaneous picrotoxin and subcutaneous bicculine. Semicarbazones are also GABA-transaminase inhibitors. Extensive structure- -activity relationship has demonstrated that F, Cl, Br and NO2 substituents in the arylhydrophobic pocket and a hydrogen bonding domain (HBD) are generally found in active anticonvulsant agents.

Ivabradine (a hyperpolarization activated cyclic nucleotide-gated channel blocker) elevates the threshold for maximal electroshock-induced tonic seizures in mice

2013 ◽  
Vol 65 (5) ◽  
pp. 1407-1414 ◽  
Author(s):  
Jarogniew J. Łuszczki ◽  
Andrzej Prystupa ◽  
Marta Andres-Mach ◽  
Ewa Marzęda ◽  
Magdalena Florek-Łuszczki
Keyword(s):  
Cyclic Nucleotide ◽  
Channel Blocker ◽  
Maximal Electroshock ◽  
Gated Channel

Chronic treatment by the calcium channel blocker ± PN 200-110 in the rat counteracts the stimulations of pituitary weight, prolactin release and pituitary C-kinase activity induced by a chronic estradiol treatment, in vivo

1990 ◽  
Vol 122 (3) ◽  
pp. 403-408
Author(s):  
Ph. Touraine ◽  
P. Birman ◽  
F. Bai-Grenier ◽  
C. Dubray ◽  
F. Peillon ◽  
...  
Keyword(s):  
Protein Kinase C ◽  
Protein Kinase ◽  
Calcium Channel ◽  
Calcium Channel Blocker ◽  
Channel Blocker ◽  
Plasma Prolactin ◽  
Estradiol Treatment ◽  
Kinase C ◽  
Protein Kinase C Activity

Abstract In order to investigate whether a calcium channel blocker could modulate the protein kinase C activity in normal and estradiol pretreated rat pituitary, female Wistar rats were treated or not (controls) with ± PN 200-110 (3 mg · kg−1 · day−1, sc) for 8 days or with estradiol cervical implants for 8 or 15 days, alone or in combination with PN 200-110 the last 8 days. Estradiol treatment induced a significant increase in plasma prolactin levels and pituitary weight. PN 200-110 administered to normal rats did not modify these parameters, whereas it reduced the effects of the 15 days estradiol treatment on prolactin levels (53.1 ± 4.9 vs 95.0 ±9.1 μg/l, p<0.0001) and pituitary weight (19.9 ± 0.4 vs 23.0 ± 0.6 mg, p <0.001), to values statistically comparable to those measured after 8 days of estradiol treatment. PN 200-110 alone did not induce any change in protein kinase C activity as compared with controls. In contrast, PN 200-110 treatment significantly counteracted the large increase in soluble activity and the decrease in the particulate one induced by estradiol between day 8 and day 15. We conclude that PN 200-110 opposed the stimulatory effects of chronic in vivo estradiol treatment on plasma prolactin levels and pituitary weight and that this regulation was related to a concomitant modulation of the protein kinase C activity.

Verapamil enhances the anticonvulsant effect of oxcarbazepine in the maximal electroshock-induced seizure model in mice

2009 ◽  
Vol 22 (2) ◽  
pp. 115-124
Author(s):  
Anna Zadrożniak ◽  
MichaŁ K. Trojnar ◽  
Marcin P. Trojnar ◽  
Żaneta Kimber-Trojnar ◽  
Monika Dudra-Jastrzębska ◽  
...  
Keyword(s):  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Seizure Model

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

2019 ◽  
Author(s):  
Jacob Porter ◽  
Oscar Vivas-Rodriguez ◽  
C. David Weaver ◽  
Eamonn Dickson ◽  
Abdulmohsen Alsafran ◽  
...  
Keyword(s):  
Patch Clamp ◽  
Neurodegenerative Disorders ◽  
Channel Blocker ◽  
Optimal Combination ◽  
Channel Blockers ◽  
Enolate Alkylation ◽  
Cyp Inhibition ◽  
Alkylation Reactions ◽  
Metabolic Instability

A set of novel Kv7.2/7.3 (KCNQ2/3) channel blockers was synthesized to address several liabilities of the known compounds XE991 (metabolic instability and CYP inhibition) and the clinical compound DMP 543 (acid instability, insolubility, and lipophilicity). Using the anthrone scaffold of the prior channel blockers, alternative heteroarylmethyl substituents were installed via enolate alkylation reactions. Incorporation of a pyridazine and a fluorinated pyridine gave an analog (JDP-107) with an optimal combination of potency (IC<sub>50</sub>= 0.16 𝜇M in a Kv7.2 thallium flux assay), efficacy in a Kv7.2/7.3 patch clamp assay, and drug-like properties.

Pengaruh Penggunaan Obat Antihipertensi Terhadap Sindroma Mata Kering di Surabaya

2020 ◽  
Vol 17 (2) ◽  
pp. 159
Author(s):  
WISNU TRI PAMUNGKAS ◽  
INDIRA RA ◽  
IRMA ANDRIANI PASARIBU
Keyword(s):  
Public Health ◽  
Health Center ◽  
Dry Eye ◽  
Channel Blocker ◽  
Antihypertensive Drugs ◽  
Descriptive Analysis ◽  
Dry Eye Syndrome ◽  
Chi Square ◽  
Cross Sectional ◽  
Public Health Center

<p><strong>Abstrak</strong></p><p><strong>Latar Belakang : </strong>Prevalensi Hipertensi di Indonesia semakin meningkat mencapai 25,8% pada penduduk berusia 18 tahun keatas.  Amlodipin merupakan salah satu pilihan obat untuk terapi Hipertensi yang termasuk golongan Calsium Channel Blocker (CCB). Penggunaan obat antihipertensi sendiri merupakan salah satu faktor risiko yang menyebabkan sindroma mata kering.</p><p><strong>Tujuan : </strong>Penelitian ini bertujuan untuk mengetahui pengaruh penggunaan obat antihipertensi terhadap sindroma mata kering pada penderita Hipertensi di wilayah kerja Puskesmas Jagir kota Surabaya.</p><p><strong>Metode penelitian : </strong>Penelitian ini adalah penelitian observasional analitik dengan metode cross-sectional. Subyek pada penelitian ini adalah 48 responden yang didapatkan dibagi kedalam 2 kelompok yakni, kelompok minum obat antihipertensi &gt;6 bulan dan tidak minum obat. Dilakukan pengisian kuesioner DEQ-5 dan pemeriksaan schirmer I.</p><p><strong>Hasil penelitian : </strong>Analisa deskriptif dari tes schirmer I frekuensi sindroma mata kering lebih tinggi pada responden yang mengkonsumsi obat antihipertensi dari pada responden yang tidak minum obat antihipertensi. Hasil analisa statistik menggunakan uji chi-square signifikansinya yaitu sebesar &lt;0,001 atau dapat dikatakan bahwa p&lt;α (0,05), menunjukkan ada pengaruh pemberian obat antihipertensi terhadap sindroma mata kering yang berdasarkan tes Schirmer pada pasien Hipertensi di wilayah kerja puskesmas Jagir  kota Surabaya.</p><p><strong>Simpulan : </strong>Penggunaan obat antihipertensi berpengaruh terhadap sindroma mata kering pada penderita hipertensi di wilayah kerja Puskesmas Jagir kota Surabaya</p><p><strong>Kata Kunci : </strong>Sindroma mata kering, obat antihipertensi, hipertensi</p><p><strong> </strong></p><p><strong>Abstract</strong></p><p><strong>Background: </strong>Hypertension prevalence in Indonesia is increasing to reach 25.8% in the population aged 18 years and over. Amlodipine is one of the drugs for hypertension therapy which is included in the Calcium Channel Blocker (CCB) class. The use of antihypertensive medication itself is one of the risk factors that cause dry eye syndrome.</p><p><strong>Purpose</strong>: This study aims to determine the effect of the use of antihypertensive drugs on dry eye syndrome in patients with hypertension at Jagir Public Health Center in Surabaya working area.</p><p><strong>Methods:</strong> This study was an observational analytic study with a cross-sectional method. The subjects in this study were 48 respondents found divided into 2 groups namely, the group taking antihypertensive drugs&gt; 6 months and not taking medication. The DEQ-5 questionnaire was completed and Schirmer I was examined.</p><p><strong>Results:</strong> Descriptive analysis of the Schirmer I test for the frequency of dry eye syndrome was higher in respondents who took antihypertensive drugs than those who did not take antihypertensive drugs. The results of statistical analysis using the chi-square test of significance that is equal to &lt;0.001 or it can be said that p &lt;α (0.05), indicates there is an effect of antihypertensive drug administration on dry eye syndrome based on the Schirmer test in hypertension patients at Jagir Public Health Center in Surabaya..</p><p><strong>Conclusion:</strong> The use of antihypertensive drugs has an effect on dry eye syndrome in patients with hypertension at the Jagir Public Health Center in Surabaya</p><strong>Keywords:</strong> Dry eye syndrome, antihypertensive drugs, hypertension

THE USE OF MEDICINES IN TREATING HYPERTENSION IN HUE UNIVERSITY HOSPITAL

2016 ◽  
pp. 76-84
Author(s):  
Khoa Bao Chau Thai ◽  
Thi Hong Phuong Vo
Keyword(s):  
Blood Pressure ◽  
Channel Blocker ◽  
Enzyme Inhibitor ◽  
Antihypertensive Drugs ◽  
Good Prognosis ◽  
Target Blood Pressure ◽  
University Hospital ◽  
Key Words Hypertension ◽  
Cross Sectional ◽  
Positive Effects

Background: Hypertension is a common condition in the world as well as in Viet Nam. If hypertension isn’t treated well, it can cause many serious complications. Controlling target blood pressure will bring positive effects on reducing mortality rate and also disabilities caused by diseases related to hypertension. Objectives: (1) Analyzing the use of medicines in treating hypertension. (2) Evaluating the effects of medicine usage in treating hypertension at the hospital of Hue University of Medicine and Pharmacy. Materials and methods: 388 patients were diagnosed as having hypertension with inpatient care at the Cardiovascular Department of Hue University of Medicine and Pharmacy’s hospital, using cross-sectional descriptive study methods. Results: All antihypertensive drugs in the research were contained in the antihypertensive list recommended by Vietnamese Society of Cardiology. Angiotensin converting enzyme inhibitor and calcium channel blocker were the two most popular drug groups (96.6% and 71.4%, respectively). The rate of using multi-therapy regimens was higher than the rate of using uni-therapy regimens in both initial therapies (64.7%>35.3%) and final therapies (61.9%>38.1%). The rate of patients having interactions between antihypertensive drugs and the other kinds of drugs was 7.5%. The rate of patients having reasonable prescriptions was 84.3%. Evaluating the effects of medicine usage in treatments showed that the rate of patients reaching target blood pressure before leaving the hospital was 67.3%. Most patients were evaluated as having good prognosis after treatment, up to 81.7%. Conclusions: All antihypertensive drugs in the research were contained in the antihypertensive list recommended by Vietnamese Society of Cardiology. The rate of using multi-therapy regimens was higher than the rate of using uni-therapy regimens. The rate of drug interactions was quite low; most patients were evaluated as having good prognosis after treatment. Key words: hypertension, antihypertensive drugs.

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