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Inhibion potential of acetylcholinesterase reactivators in vitro testing
Šepsová, Vendula ; Vopršalová, Marie (advisor) ; Herink, Josef (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of farmacology and toxicology Candidate: Vendula Šepsová Supervisor: PharmDr. Marie Vopršalová, Csc. Title of diploma thesis: Inhibiotin potencial of acetylcholinesterase reactivators - in vitro testing. Nerve agents belong to the group of OFI that irreversibly binds to acetylcholinesterase (AChE). Neurotransmitter acetylcholine (ACh) is not degraded and its increased concentration causes excessive aggravation of cholinergic receptors, known as acute cholinergic crisis [Patočka, 2004]. The main aim of this study was to compare the relationship between structure and inhibitory effect of AChE reactivators. This knowledge can be used in designing structures of new peripherally acting AChE inhibitors with a reversible effect. The mechanism of peripheral inhibition of AChE is already used for prophylaxis of nerve agent poisoning. The mechanism of action is that reversible inhibitor binds to AChE, it prevents binding of nerve agent on this enzyme. Reversible AChE inhibitors are also used in the treatment of myasthenia gravis and in anesthetic practice, to reverse the action of muscle relaxants administered [Brufani, 1997], where the increased concentration of ACh at the neuromuscular synapses is desirable to restore the...
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Effect of Selected Substances on the Respiratory System of Rat in Vivo and in Vitro
Kottová, Martina ; Pourová, Jana (advisor) ; Herink, Josef (referee) ; Nosálová, Gabriela (referee)
BACKGROUND: Asthma is a chronic inflammatory disorder of the airways in which a number of cells and cellular elements play a role. It is a lifetime disease which is not completely curable. Many factors contribute to the pathogenesis of asthma, oxidative stress being an important one. In healthy humans, the toxicity of free radicals is inhibited by enzymatic and non-enzymatic systems. In asthmatics, the function of these endogenous systems is impaired. Despite treatment, asthma morbidity and mortality steadily increases. The search for new drugs can be based on the knowledge of the pathological changes associated with the disease, and can also be inspired by folk medicine. As regards the latter approach, new, more potent substances could be obtained by isolation and chemical modification of natural products. The aim of this doctoral thesis was to elucidate the effects of selected substances on the respiratory system of rats by in vivo and in vitro methods. We investigated the effects of orally administered α-tocopherol on the lung response in an in vivo rat model of allergic asthma. The second part of this thesis deals with natural quinazoline alkaloids (Justicia adhatoda standardized extract, vasicine, vasicinone) and their synthetic analogues, and their relaxant effects on an isolated rat trachea. The...
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A comparison of central and peripheral effect of galantamine.
Galusová, Petra ; Vopršalová, Marie (referee) ; Herink, Josef (advisor)
Galantamine is a reversible inhibitor of acety1cholinesterase (AchE). It is recommended for the treatment of rnild to moderate Alzheimer's dementia, vascular dementia and dementia with Lewy bodies. Galantamine is characterized as cognitive enhancer with dual mechanism ofaction (it has also shown activity in modulating the nicotinic cholinergic receptor). The aim of this work is to determine the effective inhibitory dose of galantamine on the selected route of administration and comparing its central and peripheral effects of galantamine. Determination to proceed on the basis of the fmdings of AchE activity in the central nervous system (in the frontal cortex, hippocampus, septum, basal ganglia and pituitary gland) and on the contrary peripheral nervous system activity of butyry1cholinesterase has been detected (specifically in the liver and plasma). The results obtained by the Ellman's method showed that galantamine is generally a weak inhibitor and statistically significant effect is found only at the highest dose used. At the highest dose used can be expected adverse effects of peripheral type.
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The effect of MDOC on testicular tissue II. Intratesticular application of a medicament with MDOC
Havlová, Martina ; Semecký, Vladimír (advisor) ; Herink, Josef (referee)
1 Abstract The aim of my rigorose work was to inspect and assess the effects of time and application of calcium/sodium salt of microdispersed oxidised cellulose (MDOC) to the structural components of testes, especially in the time after an operational localization of one testis into the intraabdominal cavity. We used a model of an experimental unilateral cryptorchidism in the adult male Wistar rats. The surgery was performed under standard conditions using a method introduced in the Department of Biological and Medical Sciences of the Faculty of Pharmacy Charles University. The rats were killed by overdosage of aether aenesthesia and the bilateral testes were removed. The tissues were immediately histologically processed. After the histological modifications we tained the sections with hematoxylin - eosin, green trichrome, Periodic acid Schiff and toluidin blue histological stainings. The evaluation was histological with optical microscope. We compared our results with studies, which are described in the theoretical introduction of my work. In the preparations from the time interval of 7 days after surgery with injection application of 1% solution of calcium/sodium salt of MDOC under the tunica albuginea we randomly measured the diameter of the seminiferous tubules. The diameter of the tubules that...
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The effect of MDOCTM on testicular tissue II. Histopathological study of experimentally damaged testicle
Komrska, Josef ; Semecký, Vladimír (advisor) ; Herink, Josef (referee)
Abstract. We had studied changes of Wistar rat germinal epithelium after aplication MDOCTM in the form of gel applied to experimentaly injured testicular peak. Our experiment had lasted for twelve days. Operated testicles was not reduced in size significantly compared with controls. There were apoptotic and multinuclear cells in seminiferous tubules. We recorded numerous populations of testicular macrophages and their phagocytic character. There were also Langhans giant cells. We observed significant infiltration of immune system cells in the apical part of operated testicles in focal way. Infiltration showed character of chronical inflammation. MDOCTM probably caused these changes by its chemotactic effects.
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Study of antileptic drug dispensation in pharmacy with enlarged sphere of activity in years 2005 - 2006
Sedláček, Vladimír ; Vopršalová, Marie (advisor) ; Herink, Josef (referee)
This thesis aims to compare consumption of particular antiepileptics (N03A) in two following years 2005 and 2006 in pharmacy with extended sphere of action to confirm the presumption of continuing increase of new antiepileptics consumption. Using the pharmacy system Paenium the consumption of particular antiepileptics was recorded as a number of drugs actually demanded by patients based on medical prescription. ATC/DDD system valid in year 2006 has been used to express the consumption. Consumption of particular antiepileptics groups was expressed as a sum of expended DDD of all active substances from each particular group of antiepileptics in years 2005 and 2006. Percentage share of particular antiepileptics groups has been calculated from the total consumption in both years. Consumptions of particular antiepileptics groups in years 2005 and 2006 have been compared. Furthermore, consumption of particular active antiepileptic substances was calculated for the years 2005 and 2006 as a sum of DDD of all medicinal product packages with content of each individual active antiepileptic substance. Since a new anti-epileptic drug pregabalin entered the Czech market in 2005, significant increase of it's consumption in first months was assumed. It was interesting to observe the influence of the new marketed drug on...
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