Anticolvulsant activity of new amine-alkyl derivatives of pyrrolidine-2,5-dione

Przedmiotem niniejszej pracy była ocena potencjalnej aktywności przeciwdrgawkowej nowych aminoalkilowych pochodnych pirolidyno-2,5-dionu (zsyntetyzowanych w Zakładzie Chemii Leków Katedry Chemii Farmaceutycznej UJ CM) w różnych modelach napadów padaczkowych u myszy. Badane związki poddano następującym testom: maksymalnego wstrząsu elektrycznego (MES), drgawek wywołanych podskórnym podaniem pentetrazolu (s.c.PTZ) oraz drgawek psychomotorycznych indukowanych prądem o częstotliwości 6 pulsów na minutę (6 Hz). Wpływ badanych związków na koordynację ruchową oceniono w teście pręta obrotowego (rotarod). Uzyskane wyniki wykazują, że prawie każda nowa aminoalkilowa pochodna pirolidyno-2,5-dionu wykazuje aktywność przeciwdrgawkową. Największą aktywność w teście MES wykazały związki RS 110, RS 113, RS 114, RS 117, RS 119, RS 121 dla których wyznaczone wartości ED50 mieszczą się w granicach 78 - 101 mg/kg. W teście s.c.PTZ największą aktywność wykazały związki RS 110, RS 111, RS 112, RS 121, RS 146, RS 147, RS 149, dla których wartości ED50 mieszczą się w granicach 60 - 90 mg/ kg, natomiast w teście 6 Hz najbardziej aktywny okazał się związek RS 117.The aim of the study was to evaluate anticolvulsant activity of new amine - alkyl derivatives of pyrrolidine-2,5-dione which were synthesized in the Department of Medicinal Chemistry Chair of Pharmaceutical Chemistry, Jagiellonian University in various models of seizures in mice. The compounds were tested in the following test: maximal electroshock (MES), the subcutaneous pentylenetetrazol (s.c.PTZ) and the 6- Hz psychomotor seizure tests. The impact of examineted compounds on motor coordination was evaluated in the rotarod test. The results obtained show that almost every new amine-alkyl derivatives of pyrrolidine-2,5-dione exhibits anticonvulsant activity. The greatest activity in the MES test showed RS 110, RS 113, RS 114, RS 117, RS 119, RS 121 compounds for which ED50 values are in the range 78 - 101 mg/kg. The greatest activity in the s.c.PTZ test showed RS 110, RS 111, RS 112, RS 121, RS 146, RS 147, RS 149 compounds for which ED50 values are in the range 60 - 90 mg/kg, whereas in 6 Hz test the most active was compound RS 117

The role of Pharmacist in optimizing antibiotic therapy. Impact of pharmaceutical consultations on antibiotic and antimicrobial drugs consumption

Introduction According to the data provided by the National Antibiotic Protection Program, approximately 50% of antibiotic prescriptions are inappropriate and every tenth hospitalized patient receives antibiotics for unjustified reasons. Overuse of this group of drugs has led to antibiotic resistance, which- according to the European Center for Disease Prevention and Control (ECDC) is a significant clinical problem in Poland. Extended hospitalization time due to infection and costs associated with antibiotic therapy are becoming an important financial problem. The report of the Supreme Audit Office (NIK) estimated them in 2019 at 800 million PLN during one year. Aim The aim of the study was to assess the impact of the introduced pharmaceutical consultations and other elements of antibiotic stewardship on the use of antimicrobial drugs in the Ludwik Rydygier Memorial Specialized Hospital in Krakow. Methods Prescribed second – and thitrd – line drugs vere verified by a pharmacist from The Antibiotics Team during dispensing drugs from The Hospital Pharmacy. After verifying the of antibiotic therapy, the pharmacist approved the dispense of the drug or performed consultations. Results The effect of the efforts carried out by the antibiotic stewardship team is a 35% decrease in the frequency of 2nd and 3rd line anti-microbial drugs dispensed within 2 years. The decrease in the use of carbapenems was 51% and the use of intravenous fluoroquinolones was reduced by 79%. Conclusions The prospective pharmacist control at The Ludwik Rydygier Memorial Specialized Hospital in Krakow, antibiotic therapy was associated with changes in the structure and quantity of antimicrobial drugs dispensed. It is not clear what type of pharmacist activity (empiric ntibiotics therapy consultations, de-escalation, drug concentration-monitored therapy consultations) contributed the most to reducing the number of drugs dispensed. This issue requires further research and is particularly important in connection with the implementation of clinical pharmacy services in Poland, their evaluation and standardization

Analgesis and anti-inflammatory activity of new analogs of HC-030031 : a TRPA1 channel antagonist

One of our study direction is research in the group of compounds affecting the TRPA1 ion channel (Transient receptor potential cation channel, subfamily A, member 1) which can perform an important function in pain (including neuropathic pain) and inflammation for example in asthma and other chronic respiratory diseases. The aim of this study was to evaluate the analgesic and anti-inflammatory activity of two analogs of HC- 030031 analogs belonging to nitrogen derivatives of the heterocyclic system: xanthine (compound 1) and benzimidazole (compound 2) with hydrazide and amide moieties respectively. In this paper, for two derivatives (compound 1 and compound 2) potential analgesic and anti-inflammatory/anti-edematous activities were evaluated in animal models of pain in mice (writhing response test, formalin test) and inflammation in rats (carrageenan- induced paw edema test). Both the tested compounds 1 and 2 showed significant analgesic and antiinflammatory activities

Clinical pharmacy - at what stage are we in Poland?

The functioning of health care centers is highly dependent on the quality of cooperation between medical staff - doctors, nurses, but also pharmacists. Pharmaceutical knowledge about medicines, combined with daily practice and supervision of the pharmacotherapy used, can bring a number of benefits, primarily increasing effectiveness and safety of treatment, as well as reducing the cost of treatment. Despite numerous difficulties, in some hospitals in Poland pharmacists undertake various types of clinical activities by directly joining the work of a hospital ward or remote monitoring of patient's pharmacotherapy using electronic systems. It should be emphasized that these are often tasks carried out outside the basic dimension of working time. The initiative taken in 2017 by the Director of the Provincial Specialist Hospital in Wroclaw, Research and Development Center, deserves a mention. Pharmacist (during the specialization in clinical pharmacy) was fully engaged in the work of hospital wards focusing first in the Department of Vascular Surgery, and then also General Surgery. Her daily duties include participation in medical celebrations, conducting medical history with newly admitted patients, optimization of pharmacotherapy, consultation with the medical and nursing team, control of orders and results of laboratory tests, giving advice to staff and educating patients in correct use of medicines. This kind of multidisciplinary cooperation has become a standard of care, which has been approved by the accreditation committee of the Center for Quality Monitoring in Health Care. In Poland, clinical pharmacy is constantly developing and gaining importance every year, but as of today, there are still no clear law regulations. Will the draft Act On The Pharmacy Profession adopted by the Council of Ministers introduce regulations and clearly define the place of a clinical pharmacist in the healthcare system? Undoubtedly, it would be a basic step to the further development of clinical pharmacy services.Funkcjonowanie placówek ochrony zdrowia w dużym stopniu zależne jest od jakości współpracy między personelem medycznym – lekarzami, pielęgniarkami, ale także farmaceutami. Wiedza farmaceutyczna na temat leków, połączona z codzienną praktyką i sprawowowanie nadzoru nad stosowaną farmakoterapią, może przynieść szereg korzyści, przede wszystkim zwiększenie skuteczności i bezpieczeństwa leczenia, a także obniżenie jego kosztów. W Polsce obserwuje się rozwój farmacji klinicznej, jednak jego tempo jest wolne, gdyż stale brak jest jednoznacznych umocowań prawnych do zatrudniania farmaceutów klinicznych. Czy przyjęty przez Radę Ministrów, projekt Ustawy o zawodzie farmaceuty wprowadzi takie możliwości i wyraźnie określi miejsce farmaceuty klinicznego w systemie opieki zdrowotnej? Bez wątpienia byłby to podstawowy krok do dalszego rozwoju usług farmacji klinicznej

The Role of Adenosine A2a Receptors in Antidepressant Activity in An Experimental Animal Model of Depression

Intensive studies on the role of adenosine A2A receptors in Parkinson’s disease have been carried out for many years,. These studies have indicated that the antagonists of these receptors not only alleviate motor deficits but also exhibit neuroprotective effects in various animal models. Little is known about the role of these receptors in ailments accompanying Parkinson’s disease, such as depression and anxiety. This paper provides a summary of existing research on the role of A2A receptors in comorbid depression in Parkinson’s disease

Pharmacy shop – why we do not want pharmaceutical care?

A pharmacist is an educated specialist working to provide patients’ with the highest level of care for who business goals should be a secondary aim. Due to an ethical attitude which is in line with the pharmacist code of ethics, a set of most important guidelines, regulating the pharmacist's profession, are them main stream of pharmaceutical care regulation implemented in daily practice. Pharmaceutical care by deploying variety of different pharmacy services, is an important element of the process of optimizing the use of medicines. To start providing pharmaceutical care by implementing a wide catalog of pharmaceutical services, a Polish pharmacist must change their attitude from the typical role of the “seller” or “shop assistant” to the role of a professional adviser to the patient who is using skills and references to provide the best possible advice. The term: "pharmaceutical care" used to refer to the understanding of the responsible action of a pharmacist, whose professional goal is to ensure the safety of pharmacotherapy and improve the patient's quality of life. The process of implementing this type of care is very difficult and this is due to the fact that most Polish pharmacies since the 90s of the twentith century operate mainly as business entities (discounts, loyalty programs, marketing campaigns). Due to the fact that the pharmacy market in Poland is constantly evolving, it seems reasonable to reflect on how to make contemporary Polish pharmacies unique medical facility, in which the patient will receive not only the prescription, but above all - substantive support from pharmacists, being specialist consultancy in the field of health and safety in taking medicines. The pharmacist, which is specialist advice on health and safety in admission drugs could start to build an authority and respect by step by step transferring the pharmacy from price only focused pharmacy to advance advice focused center of patient well being . It is a very simple process which can be start even from tomorrow. It only a matter of will, and eagerness to make a chance.Farmaceuta to wykształcony specjalista pracujący nad zapewnieniem swojemu pacjentowi opieki na najwyższym poziomie, dla którego cele biznesowe powinny być wtórne. Dzięki etycznej postawie zgodnym z kodeksem etyki zawody aptekarza, realizowane są założenia opieki farmaceutycznej, będący ważnym elementem procesu optymalizacji użycia leków. Polski farmaceuta, aby rozpocząć sprawowanie opieki farmaceutycznej poprzez realizowanie szerokiego katalogu usług, musi zmienić swoje nastawienie z typowej roli sprzedawcy do roli profesjonalnego doradcy dla pacjenta. Pojęcie: “opieka farmaceutyczna” zwykło się odnosić do rozumienia odpowiedzialnego działania farmaceuty, którego zawodowym celem jest zapewnienie bezpieczeństwa farmakoterapii i podniesienie jakości życia pacjenta. Proces wdrażania tego rodzaju opieki jest bardzo trudny i to z uwagi na to, że większość polskich aptek od lat 90-tych XX w funkcjonuje głównie jako podmioty biznesowe (zniżki, programy lojalnościowe, akcje marketingowe). Ze względu na to, że rynek apteczny w Polsce stale się rozwija zasadne wydaje się poczynienie refleksji na temat tego, w jaki sposób współczesne polskie apteki uczynić wyjątkowymi placówkami medycznymi, w których pacjent otrzyma nie tylko realizację recepty, ale nade wszystko - merytoryczne wsparcie ze strony farmaceuty, będące specjalistycznym doradztwem w sprawach zdrowia i bezpieczeństwa w przyjmowaniu leków