Prokinetika jsou skupinou léčiv, které díky schopnosti stimulace hladké svaloviny zvyšují motilitu trávicího traktu, a to především v jeho proximální části. V současnosti se prokinetika využívají primárně pro léčbu funkční dyspepsie, ale uplatnění mohou nalézt i u jiných indikací. Pozitivního účinku na motilitu dosahují prostřednictvím mechanismů, které jsou v rámci skupiny prokinetik do značné míry heterogenní. Článek poskytuje čtenářům základní přehled informací vztahujícím se k jednotlivým prokinetikům aktuálně registrovaných na trhu v České republice, blíže popisuje jejich farmakologické účinky a diskutuje užití prokinetik v léčbě funkční dyspepsie a refluxní nemoci jícnu, což jsou nejčastější indikace k užití prokinetik v klinické praxi.
Prokinetics are a group of drugs that, due to their ability to stimulate smooth muscle contraction, enhance the motility of the digestive tract, particularly in its proximal part. Currently, prokinetics are primarily used to treat functional dyspepsia, though they may also be prescribed for other indications. They exert their positive effects on motility through mechanisms that vary within this drug class. This article provides readers with a basic overview of the prokinetic agents currently registered on the market in the Czech Republic, describes their pharmacological effects in more detail, and discusses the use of prokinetics in the treatment of functional dyspepsia and gastroesophageal reflux disease, which are the most common indications for the use of prokinetics in clinical practice.
- Keywords
- prokinetika, cinitaprid, itoprid,
- MeSH
- Benzamides administration & dosage pharmacology MeSH
- Dyspepsia drug therapy MeSH
- Gastroesophageal Reflux drug therapy MeSH
- Gastrointestinal Agents * administration & dosage classification MeSH
- Gastrointestinal Motility * drug effects MeSH
- Gastrointestinal Diseases drug therapy MeSH
- Humans MeSH
- Metoclopramide pharmacology therapeutic use MeSH
- Check Tag
- Humans MeSH
- Publication type
- Review MeSH
Gynekomastie je benigní zvětšení prsní žlázy u mužů, které může mít významný psychologický dopad, zejména u dětí a adolescentů. Tento článek se zabývá farmakologicky indukovanou gynekomastií a nejčastějšími léky, které mohou přispět k jejímu vzniku. V rámci naší analýzy jsme identifikovali a přezkoumali relevantní studie a kazuistiky publikované v databázi PubMed, které se zabývají různými aspekty gynekomastie u dětských pacientů. Důležitým krokem v prevenci gynekomastie je informovanost zdravotnického personálu, rodičů a pacientů o potenciálních rizicích spojených s užíváním určitých léků. Je nevyhnutelné, aby při předepisovaní léčby byly zohledněny veškeré možné vedlejší účinky, a aby se provedlo důkladné zhodnocení poměru přínosů a rizik. Mimo jiné se doporučuje provádět pravidelné kontroly a hodnocení pacientů, kteří užívají rizikové léky, aby bylo možné včas identifikovat a řešit případné příznaky gynekomastie. Tento článek zdůrazňuje potřebu zvýšené pozornosti k vybraným lékům, které jsou nejčastěji uváděny v odborné literatuře, a multidisciplinární přístup k léčbě. Informovanost o farmakologických rizicích a podpora ze strany zdravotnických odborníků jsou klíčové pro prevenci a zvládnutí tohoto stavu, ale také pro psychologickou pohodu dětských pacientů trpících touto diagnózou.
Gynecomastia is a benign enlargement of breast tissue in males that can have significant psychological impacts, especially in children and adolescents. This article focuses on pharmacologically induced gynecomastia and the most common medications that may contribute to its development. In our analysis, we identified and examined relevant studies and case reports published in the PubMed database that discuss various aspects of gynecomastia in pediatric patients. An important step in the prevention of gynecomastia is the awareness of healthcare professionals, parents, and patients regarding the potential risks associated with the use of certain medications. It is essential that all possible side effects are considered when prescribing treatment and that a thorough assessment of the benefits and risks is conducted. Additionally, it is recommended to carry out regular check-ups and evaluations of patients who are taking high-risk medications to identify and address any symptoms of gynecomastia in a timely manner. This article emphasizes the need for increased attention to selected medications commonly cited in the scientific literature and a multidisciplinary approach to treatment. Awareness of pharmacological risks and support from healthcare professionals are crucial for the prevention and management of this condition, as well as for the psychological well-being of pediatric patients suffering from this diagnosis.
- MeSH
- Anticonvulsants pharmacology adverse effects MeSH
- Antipsychotic Agents pharmacology adverse effects MeSH
- Child MeSH
- Gynecomastia * etiology MeSH
- Isoniazid pharmacology adverse effects MeSH
- Humans MeSH
- Metoclopramide pharmacology adverse effects MeSH
- Drug-Related Side Effects and Adverse Reactions * drug therapy MeSH
- Omeprazole pharmacology adverse effects MeSH
- Check Tag
- Child MeSH
- Humans MeSH
Článek popisuje případ neúmyslného intravenózního podání prokain-penicilinu (P-PNC) místo ordinovaného krystalického penicilinu (G-PNC), přičemž tento výjimečný incident je analyzován z pohledu lidského faktoru a řízení kvality pomocí metody kořenové analýzy (Root Cause Analysis, RCA). Případ zdůrazňuje zásadní roli infuzního setu s filtrem, který zamezil průchodu větších částic suspenze do krevního oběhu pacienta a tím předešel vážnějším následkům. Incident je současně významným příkladem pro ošetřovatelskou praxi, který podtrhuje důležitost důsledného dodržování bezpečnostních a standardních operačních postupů (SOP) v rámci kompetencí sester a nutnost zapojení klinického farmaceuta při práci s LASA léčivy.
The article describes a case of unintended intravenous administration of procaine penicillin (P-PNC) instead of the prescribed crystalline penicillin (G-PNC). This unique incident is analyzed from the perspectives of human factors and quality management, using the Root Cause Analysis (RCA) method. A key element was the protective role of the infusion set with a filter, which prevented larger suspension particles from entering the patient's bloodstream, thereby averting more serious consequences. This case also serves as an important example for nursing practice, emphasizing the necessity of adhering to safety and Standard Operating Procedures (SOP) within the scope of nursing competencies, as well as the crucial role of clinical pharmacists in managing LASA (Look-Alike, Sound-Alike) medications.
- Keywords
- kořenová analýza, Hoigné syndrom,
- MeSH
- Administration, Intravenous MeSH
- Humans MeSH
- Medication Errors * MeSH
- Professional Competence MeSH
- Penicillin G Procaine administration & dosage adverse effects MeSH
- Quality Control MeSH
- Check Tag
- Humans MeSH
- Male MeSH
- Publication type
- Case Reports MeSH
Apart from the SARS-CoV-2 virus, tuberculosis remains the leading cause of death from a single infectious agent according to the World Health Organization. As part of our long-term research, we prepared a series of hybrid compounds combining pyrazinamide, a first-line antitubercular agent, and 4-aminosalicylic acid (PAS), a second-line agent. Compound 11 was found to be the most potent, with a broad spectrum of antimycobacterial activity and selectivity toward mycobacterial strains over other pathogens. It also retained its in vitro activity against multiple-drug-resistant mycobacterial strains. Several structural modifications were attempted to improve the in vitro antimycobacterial activity. The δ-lactone form of compound 11 (11') had more potent in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Compound 11 was advanced for in vivo studies, where it was proved to be nontoxic in Galleria mellonella and zebrafish models, and it reduced the number of colony-forming units in spleens in the murine model of tuberculosis. Biochemical studies showed that compound 11 targets mycobacterial dihydrofolate reductases (DHFR). An in silico docking study combined with molecular dynamics identified a viable binding mode of compound 11 in mycobacterial DHFR. The lactone 11' opens in human plasma to its parent compound 11 (t1/2 = 21.4 min). Compound 11 was metabolized by human liver fraction by slow hydrolysis of the amidic bond (t1/2 = 187 min) to yield PAS and its starting 6-chloropyrazinoic acid. The long t1/2 of compound 11 overcomes the main drawback of PAS (short t1/2 necessitating frequent administration of high doses of PAS).
- MeSH
- Antitubercular Agents chemistry MeSH
- COVID-19 * MeSH
- Zebrafish MeSH
- Aminosalicylic Acid * pharmacology MeSH
- Lactones MeSH
- Humans MeSH
- Mycobacterium tuberculosis * MeSH
- Mice MeSH
- Pyrazinamide pharmacology MeSH
- SARS-CoV-2 MeSH
- Tuberculosis * drug therapy MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Keywords
- Višněvského blokáda,
- MeSH
- Back Pain etiology MeSH
- Lower Extremity pathology MeSH
- Fractures, Bone surgery diagnostic imaging pathology MeSH
- Complex Regional Pain Syndromes * diagnosis etiology drug therapy pathology MeSH
- Pharmaceutical Solutions administration & dosage MeSH
- Middle Aged MeSH
- Humans MeSH
- Heel surgery diagnostic imaging pathology MeSH
- Spine diagnostic imaging pathology MeSH
- Procaine * administration & dosage pharmacology MeSH
- Check Tag
- Middle Aged MeSH
- Humans MeSH
- Male MeSH
- Publication type
- Case Reports MeSH
Správně indikovaná antiemetická profylaxe zásadním způsobem zvyšuje compliance pacientů s protinádorovou léčbou a současně zvyšuje jejich kvalitu života. Současná doporučení vycházejí ze stratifikace chemoterapeutik (chemoterapeutických režimů) do čtyř skupin podle emetogenního potenciálu. Obvyklým doporučením pro vysoce emetogenní režimy je v současnosti čtyřkombinace setronu, inhibitoru receptoru NK1, kortikosteroidu a olanzapinu. V případě středně emetogenních chemoterapeutik je obvykle setron s kortikosteroidem dostatečný a u nízce emetogenních režimů doporučujeme setron nebo metoclopramid jako jednorázovou profylaxi. V žádném případě bychom neměli zapomínat ani na antiemetickou profylaxi v průběhu radioterapie.
Appropriate prevention of chemotherapy-induced nausea and vomiting significantly improves compliance of the treated patients and at the same time improves patient quality of life. Current guidelines are based on the chemotherapy stratification into four categories according to the risk of emesis. The generally recommended prophylaxis for the highly emetic chemotherapy regimens is the combination of 5-hydroxytryptamine 3 (5-HT3) receptor antagonists, inhibitor of NK1 receptor, corticosteroid and olanzapine. In the case of moderately emetogenic chemotherapy the combination of 5-HT3 receptor antagonists and corticoid is sufficient and in the case of chemotherapy regimens with low emetogenicity single dose of 5-HT3 receptor antagonists is recommended. We should not forget the antiemetic prophylaxis also in the case of patients undergoing radiotherapy.
- MeSH
- Neurokinin-1 Receptor Antagonists pharmacology classification therapeutic use MeSH
- Serotonin 5-HT3 Receptor Antagonists pharmacology classification therapeutic use MeSH
- Antiemetics * pharmacology classification therapeutic use MeSH
- Adrenal Cortex Hormones pharmacology classification therapeutic use MeSH
- Quality of Life MeSH
- Humans MeSH
- Medication Therapy Management * MeSH
- Metoclopramide pharmacology therapeutic use MeSH
- Drug-Related Side Effects and Adverse Reactions classification MeSH
- Olanzapine pharmacology therapeutic use MeSH
- Check Tag
- Humans MeSH
- Publication type
- Review MeSH
Tuberculosis is the number one killer of infectious diseases caused by a single microbe, namely Mycobacterium tuberculosis (Mtb). The success rate of curing this infection is decreasing due to emerging antimicrobial resistance. Therefore, novel treatments are urgently needed. As an attempt to develop new antituberculars effective against both drugs-sensitive and drug-resistant Mtb, we report the synthesis of a novel series inspired by combining fragments from the first-line agents isoniazid and pyrazinamide (series I) and isoniazid with the second-line agent 4-aminosalicylic acid (series II). We identified compound 10c from series II with selective, potent in vitro antimycobacterial activity against both drug-sensitive and drug-resistant Mtb H37Rv strains with no in vitro or in vivo cytotoxicity. In the murine model of tuberculosis, compound 10c caused a statistically significant decrease in colony-forming units (CFU) in spleen. Despite having a 4-aminosalicylic acid fragment in its structure, biochemical studies showed that compound 10c does not directly affect the folate pathway but rather methionine metabolism. In silico simulations indicated the possibility of binding to mycobacterial methionine-tRNA synthetase. Metabolic study in human liver microsomes revealed that compound 10c does not have any known toxic metabolites and has a half-life of 630 min, overcoming the main drawbacks of isoniazid (toxic metabolites) and 4-aminosalicylic acid (short half-life).
- MeSH
- Antitubercular Agents chemistry MeSH
- Isoniazid pharmacology MeSH
- Aminosalicylic Acid * pharmacology MeSH
- Humans MeSH
- Methionine MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium tuberculosis * MeSH
- Mice MeSH
- Tuberculosis * drug therapy microbiology MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- MeSH
- Adult MeSH
- Comorbidity MeSH
- Humans MeSH
- Breast Neoplasms complications MeSH
- Orbital Cellulitis * diagnosis etiology classification microbiology MeSH
- Penicillin G Procaine administration & dosage therapeutic use MeSH
- Staphylococcus aureus pathogenicity MeSH
- Streptococcus pyogenes pathogenicity MeSH
- Check Tag
- Adult MeSH
- Humans MeSH
- Female MeSH
- Publication type
- Case Reports MeSH
Syphilis je systémová infekce s mnohočetnými projevy, které mohou napodobovat široké spektrum kožních i jiných nemocí. Důležitá je včasná diagnostika i vhodně zvolená antibiotická léčba.
Syphilis is a systemic infection with multiple manifestations that can mimic a wide range of skin and other diseases. Early diagnosis and appropriate antibiotic treatment are important.
- MeSH
- Penicillin G Benzathine administration & dosage therapeutic use MeSH
- Doxycycline administration & dosage therapeutic use MeSH
- Homosexuality, Male MeSH
- Middle Aged MeSH
- Humans MeSH
- Polymerase Chain Reaction MeSH
- Penicillin G Procaine administration & dosage therapeutic use MeSH
- Unsafe Sex MeSH
- Syphilis Serodiagnosis MeSH
- Sexually Transmitted Diseases diagnosis drug therapy MeSH
- Syphilis * diagnosis drug therapy MeSH
- Check Tag
- Middle Aged MeSH
- Humans MeSH
- Male MeSH
- Publication type
- Case Reports MeSH
