Ceska a Slovenska Farmacie最新文献

Alleviating the symptoms of irritable bowel syndrome (IBS) through the addition of probiotics to the treatment of IBS patients appears to be promising. The present randomized clinical trial seeks to assess the efficacy of a multi-strain probiotic product combining two Lactobacillus (L.) strains: L. acidophilus and L. plantarum, in diarrhea-predominant IBS (IBS-D) patients. A randomized, single-blinded clinical trial design was adopted to randomly assign 100 patients into two groups. Patients in group A received standard IBS treatment, whereas Group B patients were treated with probiotics besides the standard treatment. Both groups were treated for up to 12 weeks. The patients were assessed clinically by using IBS - Symptom Severity Scale (IBS-SSS) before starting the treatment and then at the end of the treatment period to evaluate the actual effect of probiotic intervention in treating IBS-D. Both treatments resulted in significant reductions in the total IBS-SSS score, but the reduction in Group B was significantly higher than in Group A. The reduction was significant in the number of days with pain, the severity of abdominal distension, satisfaction with bowel symptoms, and the effect of IBS on patients' life. The standard treatment showed a reduction of 241 points in the overall IBS-SSS score, while adding the probiotic resulted in 307 points reduction. Before treatment, all patients had severe IBS symptoms, but after treatment, 100% of patients in group B either achieved complete remission or had mild symptoms, while 14.3% of patients in group A still had moderate IBS. The patients on probiotics exhibited higher reductions in IBS-SSS overall scores as well as scores of individual sections. The probiotics also improved the severity of the disease and its symptoms when added to standard treatment. The results of this trial could support the addition of probiotics to the guidelines for managing IBS.

Current trends in drug design notably consider so-called privileged scaffolds as the core structural fragments with decisive impact on affinity to properly chosen biological targets, potency, selectivity and toxicological characteristics of drugs and prospective drug candidates. Fruquintinib (1) is a novel synthetic selective inhibitor of vascular endothelial growth factor receptor (VEGFR) isoforms, i.e., VEGFR-1, VEGFR-2 and VEGFR-3. The therapeutic agent (1) consists of a flat bicyclic heteroaromatic ring, in which two nitrogens are suitablyincorporated, a core bicyclic heteroaromatic ring - privileged (substituted) benzofuran scaffold, and a pair of hydrogen bond (H-bond) donor and acceptor group, i.e., amide functional moiety. Fruquintinib (1) was first approved in China for the treatment of metastatic colorectal cancer, a severe malignant disease with a high mortality rate. The review article offered a brief insight into the topic of privileged structures, their drug- -like ranges of several parameters, pharmacodynamic characteristics of fruquintinib (1) and various in silico descriptors characterizing drug's structural and physicochemical properties (molecular weight, number of heavy atoms, number of aromatic heavy atoms, fraction of sp3 C-atoms, number of H-bond acceptors, number of H-bond donors, total polar surface area, molar refractivity, molecular volume as well as parameters of lipophilicity and solubility). Some of these descriptors were related to pharmacokinetics and distribution of fruquintinib (1), and, in addition, might help predict its ability to cross passively the blood-brain barrier (BBB). Moreover, a possible connection between the induction potential on cytochrome P450 isoenzymes (CYP1A2 and CYP3A4) and passive transport of a given drug into the central nervous system via BBB was investigated. Current clinical experience and future directions regarding of fruquintinib (1) were also briefly outlined.

Dose-response relationships are not fully understood for antipsychotics. Especially in the case of multimodal antipsychotics, these relationships cannot be simplified to the level of dopaminergic receptor occupancy alone. In general, for most antipsychotics, there is no linear dose-response relationship. Reasons for this include, among others, pharmacokinetic factors affecting plasma levels. Based on meta-analyses, the doseresponse curve appears to be bell-shaped. However, in the case of some antipsychotics, it appears that even increasing the dose beyond the recommended range could yield further increases in efficacy. It should be stressed that this is an off-label procedure and cannot generally be recommended and there is not enough valid information for general conclusions for these antipsychotics either. Mini-invasive sampling and alternative matrices such as saliva or dry blood spots could open the way to more frequent monitoring of antipsychotics and a better understanding of doseresponse relationships.

Radiopharmaceutical 68Ga-PSMA-11 is one of the newest positron radiopharmaceuticals available for nuclear medicine departments in the Czech Republic. The radiopharmaceutical preparation can be carried out manually or instrumentally using modules for synthesis. Despite the greater technological difficulty of preparation, the success of synthesis of this radiopharmaceutical by both methods is very high, and the evaluated quality parameters of the radiopharmaceutical are comparable by both manual and instrumental preparation methods. Also, regarding professional exposure, the preparation of 68Ga-PSMA-11 does not significantly affect the whole-body and finger dosimetry results.

Pain is a serious subjective experience, which, although it has a protective nature, it physically and mentally exhausts the patient. The pharmacological field of development and research in the treatment and relief of pain has been dynamic and interesting ever since the isolation of salicylic acid. After discovering the molecular nature of cyclooxygenase and its inhibition, research focused on selective COX-2 inhibitors, but they were a big disappointment. Today, the possibility of contributing to safe and effective analgesic-antiphlogistic treatment for the patient with a combination of drugs is emerging again.

The problem of unavailability of drugs and shortages have been a common problem in recent years. Shortages may threaten some treatment regimens for oncological patients. This article presents a systematic review of studies evaluating the efficacy and safety of chemotherapy regimens combining fluorouracil and standard or low-dose leucovorin in treating colorectal cancer. A total of 13 prospective and retrospective studies were included in the review. Meta-analyses and review papers were excluded. It is apparent from the systematic review that a lower dose of leucovorin does not fundamentally affect the efficacy of regimens combining 5-fluorouracil with leucovorin in treating patients with colorectal cancer. Similarly, even in the case of safety, reducing the dose of leucovorin did not influence the frequency and severity of observed adverse effects. Surprisingly, in three studies, some of the adverse effects occurred more often with the higher dose of leucovorin. Furthermore, the article presents the results of a questionnaire survey of the management of leucovorin shortages at the departments of preparation of cytostatics (N = 46) within the Czech Republic. In total, 35 workplaces provided feedback. In 17 cases, the departments for the preparation of cytostatics in the Czech Republic had to accept restrictions on administering the full dose of leucovorin. These restrictions consisted of reducing the dose of the injectable form of leucovorin, changing the chemotherapy regimen, administering the oral form of calcium folinate, forcing a therapeutic break, or a combination of these approaches.

Given the role of the microbial factor in the development of infectious-inflammatory processes in the oral mucosa, the research aim was to study the antimicrobial action of a new combined dental gel containing Rotocan® (10%) and triclosan (0.4%) in vitro and in the traumatic stomatitis in albino rats. Rotrin- Denta® exhibited strong antimicrobial activity against etalon strains of gram-positive (S. aureus ATTC 6538, S. pyogenes DICK 1, B. subtilis ATCC 6633) and gramnegative (E. coli ATCC 25922) bacteria, which exceeded the action of the reference drug Camident-Zdorovia® and weak effects on pseudomonads (P. aeruginosa ATCC 27853) and fungi (C. albicans CCV 885-653), which is less to the reference preparation. Rotrin- Denta® reduced microbial insemination and eliminated oral dysbiosis in albino rats with traumatic stomatitis, exceeding the effect of Kamident-Zdorov'ya®. The results open up the prospect of its clinical testing and further implementation in the dentistry practice.

In continuation of our published review on general inhalational anesthetics, the current article presents a survey of intravenous agents for general anaesthesia. From chemical point of view these compounds belong to structurally diverse categories, such as barbiturates - thiopental (Sodium pentothal®, Trapanal®, Pentothal®), methohexital (Brevital®), and hexobarbital (Evipan®, Hexenal®, Citopan®, Tobinal®); non-barbiturate derivatives - ketamine (Ketalar® Ketaset®), esketamine (Ketanest®), and etomidate (Amidate®, Hypnomidate®), phenolic derivatives - propofol (Diprivan®); steroid derivatives - mixture of alfadolone and alfaxalone (Althesin® in human and Saffan® in veterinary anesthesia); and derivatives of phenylacetic acid - propanidid (Epontol®, Sombrevin®). Most of these compounds are chiral, with the exception of propofol and propanidid. Apart from etomidate and esketamine, they are used in the form of their racemates. Besides their characteristics and mechanism of action, attention is centred also on their chiral properties.