National Repository of Grey Literature 151 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
Monitoring of basic pharmacokinetic parameters of acetylcholinesterase inhibitors used in the treatment of Alzheimer's disease
Krejčiová, Markéta ; Doležal, Martin (advisor) ; Vopršalová, Marie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Control of Pharmaceuticals Student: Markéta Krejčiová Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Supervisor specialist: Mjr. PharmDr. Jana Žďárová Karasová, Ph.D. Title of diploma thesis: Monitoring of basic pharmacokinetic parameters of acetylcholinesterase inhibitors used in the treatment of Alzheimer's disease Alzheimer's disease is a progressive irreversible neurodegenerative disorder that is globally associated with the most frequent cause of dementia. The pathophysiology of this illness is not fully understood yet. The commonly used treatment is still symptomatic, based on IAChE and memantine. Great attention is paid particularly to IAChEs and their derivatives, which arise from the basic structure of tacrine and 7-MEOTA. These two molecules were used as a reference for comparison with newly synthetized IAChE derivatives KB-36 and KB-38. Changes in plasma and brain tissue concentration levels were studied. The in vivo study was performed on rats (male, tribe Wistar). Equimolar doses were administered intramuscularly. Samples of plasma and brain tissue were evaluated by using HPLC techniques. The main aim was to determine the real concentration levels of all IAChE in both...
In vitro Methods for the Prediction of Blood Brain Barrier Penetration
Zálešáková, Helena ; Vopršalová, Marie (advisor) ; Čečková, Martina (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Helena Zálešáková Supervisor: PharmDr. Marie Vopršálová, CSc. Title of diploma thesis: In vitro Methods for the Prediction of Blood Brain Barrier Penetration This thesis deals with the correlation between two in vitro models simulating the blood- brain barrier (HEB, hematoencephalic barrier) and their comparison in terms of practical use. These are the PAMPA (Parallel Artificial Membrane Permeability Assay) method and the MDCK (Madin-Darby Canine Kidney) cell line, which are models for potential central nervous system (CNS) penetration screening. Within this work, a set of sixteen standard drugs were measured. The procedure was similar in both methods in order to obtain information on the amount of test substances passing through the membrane from the donor portion of the plate to the acceptor. The concentration in the donor portion was measured by UV-VIS spectrophotometry. The main difference between these methods is the membrane through which the substances penetrate. In the case of PAMPA, a lipid solution that has been isolated from pig brain (PBL, polar brain lipid) is used. This lipid simulates the phospholipid membrane of the brain capillary endothelium. In the MDCK model, the membrane...
Role of selected ABC and SLC transporters in transmembrane permeability of maraviroc: effect on transport in placenta
Matiašková, Zuzana ; Čečková, Martina (advisor) ; Vopršalová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and toxikology Student: Zuzana Matiašková Supervisor: doc. PharmDr. Martina Čečková, Ph.D. Title of diploma thesis: Role of selected ABC and SLC transporters in transmembrane permeability of maraviroc: effect on transport in placenta Antiretroviral drug maraviroc is an inhibitor of CCR5-trophic HIV virus and belongs to the group of entry inhibitors. Nowadays, maraviroc is administered as part of combination antiretroviral therapy (cART) primarily in adults, children over the age of two and pregnant women to reduce the risk of transmission of HIV to the fetus. The knowledge of interactions of maraviroc with drug transporters in placenta is crucial for optimizing the therapy during pregnancy, both in terms of efficacy and potential adverse effects. Maraviroc is known substrate of ABCB1 transporter, which plays a protective role to the fetus by its efflux activity in the apical membrane of trophoblast. However, the results of recent study employing dually perfused human placenta suggest involvement of other transport mechanisms in the maraviroc transplacental pharmaocokinetics, especially those operating in the opposite direction to ABCB1. The aim of this study was to evaluate in vitro studies whether, besides ABCB1,...
Administration of cytostatic drugs and extravasation
Rohová, Marie ; Vopršalová, Marie (advisor) ; Pourová, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové, Heyrovského 1203, Hradec Králové Department of pharmacology and toxicology Candidate: Mgr. Marie Rohová Consultant: PharmDr. Marie Vopršalová, CSc. Title of Thesis: Administration of cytostatic drugs and extravasation Key words: extravasation of cytostatics, vesicants, irritants, specific measures This thesis deals with the issue of extravasation in intravenous administration of cytostatics in oncologic patients, as one of the most feared complication of cytostatic therapy, which may has a serious irreversible consequences for patients. Extravasation describes the unintended leakage of drug from vessel into surrounding tissues or the unintended instillation of drug directly into the perivascular tissues. The severity of tissue injuries depends on several factors, including the volume and concentration of the cytotoxic agent, the localization of extravasation, the sensitivity of the tissue and the vesicant potential of the cytotoxic agent. In order to avoid extravasation, the principles of safe drug use must be followed, and if extravasation occurs, the recommendations for the drug should be known and followed. This is the only way to prevent serious damage to the patient, or significantly reduce the consequences. The experimental...
The effects of some flavonoids on isolated rat aortic rings
Fišrová, Martina ; Vopršalová, Marie (advisor) ; Pourová, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Kralove Department of Farmacology & Toxikology Student: Martina Fišrová Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: The effects of some flavonoids on isolated rat aortic rings Flavonoids are secondary plant metabolites that are profusely represented in nature. They are known for their wide range of effects and many of them have beneficial effects on the human body. Above all, they have anti-bacterial and anti-inflammatory properties and effects on cardiovascular system - they cause vasodilation. The aim of this diploma thesis was to investigate vasorelaxation effects of selected flavonoids from the group of flavonolignans - 2,3-dehydrosilybin A (DHS-A), 2,3-dehydrosilybin B (DHS-B) and metabolites, which are components of the silymarin complex found in the plant Silybum marianum (Asteraceae). The vasorelaxation potential of tested substances was verified in ex vivo conditions on isolated rat aortic rings. The effect of increasing doses of individual substances in precontracted aortic rings with intact endothelium was measured. From the measured values, the DRC curves were constructed and EC50 values were determined. The analysis of the results shows, that DHS-A (EC50 = 30,1 mol/l) had the most signifiant activity. Its...
In vitro Methods for the Prediction of Blood Brain Barrier Penetration
Zálešáková, Helena ; Vopršalová, Marie (advisor) ; Čečková, Martina (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Helena Zálešáková Supervisor: PharmDr. Marie Vopršálová, CSc. Title of diploma thesis: In vitro Methods for the Prediction of Blood Brain Barrier Penetration This thesis deals with the correlation between two in vitro models simulating the blood- brain barrier (HEB, hematoencephalic barrier) and their comparison in terms of practical use. These are the PAMPA (Parallel Artificial Membrane Permeability Assay) method and the MDCK (Madin-Darby Canine Kidney) cell line, which are models for potential central nervous system (CNS) penetration screening. Within this work, a set of sixteen standard drugs were measured. The procedure was similar in both methods in order to obtain information on the amount of test substances passing through the membrane from the donor portion of the plate to the acceptor. The concentration in the donor portion was measured by UV-VIS spectrophotometry. The main difference between these methods is the membrane through which the substances penetrate. In the case of PAMPA, a lipid solution that has been isolated from pig brain (PBL, polar brain lipid) is used. This lipid simulates the phospholipid membrane of the brain capillary endothelium. In the MDCK model, the membrane...
Role of selected ABC and SLC transporters in transmembrane permeability of maraviroc: effect on transport in placenta
Matiašková, Zuzana ; Čečková, Martina (advisor) ; Vopršalová, Marie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and toxikology Student: Zuzana Matiašková Supervisor: doc. PharmDr. Martina Čečková, Ph.D. Title of diploma thesis: Role of selected ABC and SLC transporters in transmembrane permeability of maraviroc: effect on transport in placenta Antiretroviral drug maraviroc is an inhibitor of CCR5-trophic HIV virus and belongs to the group of entry inhibitors. Nowadays, maraviroc is administered as part of combination antiretroviral therapy (cART) primarily in adults, children over the age of two and pregnant women to reduce the risk of transmission of HIV to the fetus. The knowledge of interactions of maraviroc with drug transporters in placenta is crucial for optimizing the therapy during pregnancy, both in terms of efficacy and potential adverse effects. Maraviroc is known substrate of ABCB1 transporter, which plays a protective role to the fetus by its efflux activity in the apical membrane of trophoblast. However, the results of recent study employing dually perfused human placenta suggest involvement of other transport mechanisms in the maraviroc transplacental pharmaocokinetics, especially those operating in the opposite direction to ABCB1. The aim of this study was to evaluate in vitro studies whether, besides ABCB1,...
Vasorelaxant activity of selected metabolites of quercetine on isolated rat aorta
Horáčková, Markéta ; Vopršalová, Marie (advisor) ; Pourová, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradech Králové Department of Pharmacology and Toxicology Candidate: Mgr. Markéta Horáčková Supervisor: PharmDr. Marie Vopršálová, CSc. Title of rigorous thesis: The vasorelaxing effect of selected quercetin metabolites on isolated rat aorta Quercetin with its metabolites belongs into wide group called flavonoids, which are polyphenolic secondary metabolites of plants. This work, that is part extensive research ongoing in Department of Pharmacology and Toxicology of Faculty of Pharmacy in Hradec Králové, is focused on selected metabolites of propionic acid. In theoretical part I included characterisation of flavonoid group and their pharmacological effect. I also described morphology of blood-vessels and mechanisms of regulation of systemic circulation, because this work is about effect on blood-vessels. In experimental part we observed vasorelaxation effect of selected metabolites on isolated thoracic aorta of strain Wistar rat first. We compared effects of tested metabolites with quercetin, which was also included in experiment. As the most efficient metabolite was found 3-(3-hydroxyphenyl)propionic acid (3-HPPA). Its vasorelaxing effect was about one order bigger than quercetin and its other tested metabolites. 3-HPPA was selected for the...
Determination of pharmacological properties of potencial drugs for the treatment of Alzheimer's disease
Schejbalová, Kateřina ; Herink, Josef (advisor) ; Vopršalová, Marie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Candidate: Mgr. Kateřina Schejbalová Supervisor: Doc. MUDr. Josef Herink, Dr.Sc. Consultant: Kpt. PharmDr. Vendula Hepnarová Title of thesis: Determination of pharmacokinetic properties of potential drugs for the treatment of Alzheimer's disease Alzheimer's disease (AD) is an illness caused by neurodegenerative changes in the brain tissue. It belongs to the diseases that lead to the origin of dementia. The occurrence of this illness has been rising over past years. Unfortunately, the causative treatment has not been found yet and the only available treatment is the symptomatic one. Therefore, it is necessary strive towards the discovery new and more efficient drugs. The aim of this thesis is to determinate the inhibiting concentrations and to measure the antioxidative activity of the new synthetic potential anti-Alzheimer drugs. Seven hybrids of 6 - chlorotacrine - tryptophan (6-Cl-THA-Trp), 7 - methoxytacrine - tryptophan (7-MEOTA-Trp) and tacrine - tryptophan (THA-Trp) were tested. The in vitro inhibiting potentials of the tested compounds against human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were evaluated. Spectrophotometer was used for the measurements by...
The effect of quercetin metabolite on the rat isolated arteries.
Rudišarová, Simona ; Vopršalová, Marie (advisor) ; Pourová, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Simona Rudišarová Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: The effect of quercetin metabolite on the rat isolated arteries This study is focused on the research of the effects of flavonol quercetin and its selected metabolites (3-(3-hydroxyphenyl)propionic acid and 3-hydroxybenzoic acid) on blood vessels in vitro. A standardized method of an isolated rat aorta was used. The aim of this study was to find out how substances act on the isolated aorta and if the effect of the effective metabolite is dependent on the presence of the endothelium in the vessel. After precontracting with noradrenaline, individual concentrations of the test substances were added to the aortic ring bath (final concentrations in the bath ranging from 10-7 to 10-3 M). From the measured values EC50 values (quercetin = 3,63 . 10-5 M, 3-(3-hydroxyphenyl)propionic acid = 3,21 . 10-6 M, 3-hydroxybenzoic acid = 4,38 . 10-5 M) were obtained and the corresponding DRC curves were constructed using S.P.E.L. Advanced Kymograph Software. The experiment was performed once again with quercetin and 3-(3-hydroxyphenyl)propionic acid on the endothelium-denuded vessel. According to the results is...

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