Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Martin Huličiak Supervisor: PharmDr. Lukáš Červený, Ph.D Title of diploma thesis: Study of interactions of antiviral drugs with intestinal drug efflux ABC transporters P-gp, MRP2 and BCRP are efflux transporters, members of the family of ATP binding cassette (ABC) transporters. These transporters are located on the apical membrane of the intestinal epithelium, where they may limit absorption of orally administered drugs. Study of drug interactions with/on intestinal efflux transporters is necessary to provide safe and effective treatment. The Caco-2 cell line is FDA recommended in vitro model of intestinal barrier and it is used for bidirectional testing of substrates and inhibitors of ABC transporters in preclinical research. However, this methodology has several shortcomings, so the need of introduction of new experimental models is increasing and the ex vivo method based on human or rat intestine is a promising option. Precision-cut intestinal slices (PCIS) represent a mini-model of the organ and contain all types of cells of the tissue. We used both in vitro model using Caco-2 cell monolayers for drug transport study and in our lab established ex vivo method of PCIS for accumulation study...

HORMONAL CONTRACEPTION - USERS̕ KNOWLEDGE Student: Křiklánová, J. Tutor: Marešová, H. Department of Social and Clinical Pharmacy, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic Introduction: Hormonal contraception is a broadly used and very reliable birth control method. Nonetheless, it is not entirely risk-free. This thesis deals with the awareness of those risks in women who are currently using hormonal contraception or have ever used it before. Aim of the thesis: The main aim was to determine the extent of the users' awareness of hormonal contraception and its risks, undesirable side effects and contraindications, as well as their source of information. Furthermore, the awareness of the environmental impact, the reasons for using hormonal contraception and user satisfaction were examined. Methodology: The research was carried out by means of online questionnaires, which were spread among current or former users of hormonal contraception regardless of age, educational background or place of residence. 148 completed questionnaires were gathered and the data which were obtained were statistically evaluated. Results: It was discovered that women feel informed (25 %) or rather informed (44,6 %) more often than uninformed; the most frequent source of information is patient...

Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, Ph.D. Student: Michal Bárta Title of Thesis: Preparation of pharmaceutical nanoparticles: optimalization process Pharmaceutical, polymer nanoparticles besides others work as well as a drug carriers. Their uniqueness is not only because of their subcelular size, but as well because of the biodegradability and biocompatibility they hold. The benefit of these nanoparticiples is the possibility of creation of selective naoparticiples which are able to controle long-term release. The formulation of polymer nanoparticles can be reached within methods using preformed polymer or with polymerization of monomers. The main goal of my thesis was to optimize the production process of polymer nanoparticles and the observation of the solvent influences. The methods used for this reaserch were evaporation method and nanoprecipitation. Granulometric and electrical characteristics of particles were measured with Zetasizer ZS 90. Measurements have prooved, that it is preferable to use the nanoparticle method for the prepartion of the the small nanoparticles with low polydispersity and sufficient stability. From the results of the granulometric analysis of nanoparticles made by the...

1 ABSTRACT Background The annual drug overdose rates have been increasing exponentially since the 90's worldwide. Toxicological information centre (TIC) represents a valuable source of information for evaluating the trends in the drug poisonings in Czech Republic. Aim of the study The purpose was to analyze the number and trends in the calls concerning poisonings due to central nervous system (CNS) affecting drugs, identify the reasons of medication errors caused by laymen, frequency and consequences of these errors across all age groups and also to analyze the numbers, causes, symptoms and severity of the paracetamol intoxications. Methods During the reference period the data from the enquiries were extracted from the TIC electronic database, discharge reports from the hospital were studied or phone call follow-ups with the patients were carried out to be able to evaluate the outcome of the poisonings. Results In the years 1997-2002 the number of calls caused by poisoning with tricyclic antidepressants and barbiturates decreased (by 366.7 % and 340,0 %, respectively) whereas the calls due to selective serotonin reuptake inhibitors and benzodiazepines overdose increased (by 1347.4 % and 359.8 %). The 0-5 years old children are at the highest risk of experiencing medication errors or accidental poisonings...

4 ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Dimitrios Vagiannis Supervisor: RNDr. Jakub Hofman, Ph.D. Title of diploma thesis: Evaluation of antiproliferative effect of selected tyrosine kinase inhibitors in MDCKII cell lines Tyrosine kinases are important enzymes regulating crucial cellular processes including differentiation, proliferation, apoptosis, transcription, metabolism, and intercellular communication. Deregulation of these enzymes is the cause of various types of cancers. The blockade of their function by tyrosine kinase inhibitors (TKis) is considered a promising approach especially in antitumor pharmacotherapy. ATP-binding cassette (ABC) drug efflux transporters are a family of transmembrane proteins that pump a variety of structurally unrelated compounds out of the cell in an energy-dependent manner. They play an important role in pharmacokinetics (affect absorption, distribution, elimination) and, at the same time, can negatively influence efficacy of chemotherapy (participate in multidrug resistance phenomenon). In our research, we evaluated antiproliferative properties of four selected TKis, namely alectinib, brivanib, osimertinib and selumetinib, in MDCKII cell lines (parent one and those transduced with human...

IN ENGLISH LANGUAGE Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacology and Toxicology Candidate: Mgr. Alžbeta Štefela Supervisor: Prof. PharmDr. Petr Pávek, PhD. Title of the doctoral thesis: Novel bile acid derivatives as promising therapeutic approach Bile acids (BAs) are amphipathic steroidal molecules that are traditionally known to facilitate intestinal digestion and absorption of lipids and fat-soluble substances. On top, the recent findings have revealed that they represent important signaling agents involved in the orchestration of lipid, glucose and energy metabolism and immune response. BAs exhibit these roles by activating intracellular nuclear receptors such as farnesoid X (FXR), pregnane X (PXR) vitamin D receptors. Furthermore, BAs act as endocrine signaling molecules and activate numerous biological cascades via a membrane G-protein-coupled receptor, termed TGR5. Therefore, the extensive modulation of BA scaffold underwent to identify compounds with specific targeting of above-mentioned receptors as a promising therapeutic approach for the treatment of various liver and metabolic disorders including cholestasis, biliary cirrhosis, nonalcoholic steatohepatitis or diabetes. The principal aim of this doctoral thesis was to investigate the structure...

Univerzita Karlova 1. lékařská fakulta Studijní program: Biomedicína Studijní obor: Preventivní medicína MUDr. Karolína Hronová Polymorfismus genů účastnících se v metabolismu léčiv jako potenciální cíl prevence závažných komplikací léčby u novorozenců a dětí Polymorphism of drug metabolizing enzymes as a potential target of prevention of serious treatment complications in neonates and infants Disertační práce- ABSTRAKT V ANGLICKÉM JAZYCE Školitel: prof. MUDr. Ondřej Slanař, Ph.D. Konzultant: MUDr. Pavla Pokorná, PhD. Praha, 2018 Abstract Background and aims: The safety of analgosedative drugs includes drug interactions, adverse effects, withdrawal syndrome and drug dependence are factors that significantly affect morbidity and mortality. Its prevention is critical for quality improvement of care in paediatric patients. The aim of the thesis was to evaluate the prediction of efficacy and safety of analgosedative drugs sufentanil, midazolam, tramadol and valproic acid in neonates and children based on the occurrence of selected pharmacogenetic biomarkers. The incidence of drug interactions of phenobarbital with other analgosedative drugs has also been evaluated. Methodology: The thesis is based on two studies conducted on Intensive and Resuscitation Care Unit of the Clinic of Paediatric and Adolescent...

ANALYSIS OF DRUG-RELATED PROBLEMS IN A HEALTHCARE FACILITY V. Author: Thu Thao Truongová Supervisor of the diploma thesis: PharmDr. Martin Doseděl, Ph.D. Consultant: PharmDr. Veronika Měrková Charles University, Faculty of Pharmacy in Hradec Králové, Department of Social and Clinical Pharmacy INTRODUCTION Medication errors are one of the most frequent medicinal errors. They affect patient's safety from the long-term point of view.1 The great part of medication errors occurs on the level of drug administration.2 In healthcare facilities mostly nurses are responsible for medication administration.3 AIM To obtain and evaluate medication errors during drug administration by nurses in a healthcare facility. METHODICS A prospective observational study was conducted in the facility Hamzova léčebna for children and adults focusing on medical rehabilitation. Data collection was performed in May 2019 three consecutive days on each ward, where drugs were administrated by nurse. Direct observation was done in morning, noon and evening drug administrations. Obtained data were recorded into prepared form and were compared with physician's medication order on the patient's record. Afterwards, the forms were transcripted into online database, data were transfered to MS Excel software programme and evaluated by...

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