Комплексные лабораторные исследования при профессиональных заболеваниях органов дыхания

Results of complex laboratory examination of 103 patients with dust related bronchitis caused by exposure of various industrial dusts, 22 patients with pneumoconiosis and 12 subjects not having respiratory pathology and not exposed to quartz dust or any other occupational hazards are presented in this article. Laboratory examination included morphological investigations of sputum and bronchial brush biopsy specimens, cytochemical characterization of bronchial ciliated epithelium and blood cells, and bacteriological and serological investigations of bronchial mucus. Our results demonstrated that morphological lesions of bronchial epithelium cells leading to their death followed cell dysfunction, disorders of enzyme activity, hypoxemia, predominance of Haemophilus influenzae in microflora, and significant inflammatory and allergic response in blood. These changes were found in different clinical stages of dust related bronchitis and pneumoconiosis. The findings obtained are of great importance for understanding pathogenic mechanisms of dust related lung diseases as well as from clinical point of view such as diagnosis and development of individual treatment strategies.В статье представлены результаты комплексного лабораторного обследования 103 больных с пылевым бронхитом, вызванным различными видами производственной пыли, 22 пациентов с пневмокониозом различной степени выраженности и 12 человек, не имевших в анамнезе заболеваний органов дыхания и не подвергавшихся воздействию кварцсодержащей пыли и других профессиональных вредностей. Комплекс лабораторного обследования включал морфологическое изучение мокроты, соскоб слизистой бронхов, цитохимическую характеристику функционального состояния мерцательного эпителия, а также клеток крови в сочетании с бактериологической и серологической оценкой отделяемого бронхов. Исследования показали, что изменения морфологической структуры клеток бронхиального эпителия, приводящие к их гибели, связаны с нарушением функционального состояния, ферментативной активности клеток, гипоксемией, изменением микробной флоры с преобладанием Haemophilus influenzae, выраженной воспалительной и аллергической реакцией крови и характерны для различной степени выраженности клинических проявлений пылевого бронхита и пневмокониоза. Полученные данные имеют значение как с позиции уточнения патогенетических механизмов развития пылевых заболеваний легких, так и с практической точки зрения – в диагностике и при формировании индивидуальных лечебных комплексов при этой патологии

European Registry on Helicobacter pylori management (Hp-EuReg): Patterns and trends in first-line empirical eradication prescription and outcomes of 5 years and 21 533 patients

Objective The best approach for Helicobacter pylori management remains unclear. An audit process is essential to ensure clinical practice is aligned with best standards of care. Design International multicentre prospective non-interventional registry starting in 2013 aimed to evaluate the decisions and outcomes in H. pylori management by European gastroenterologists. Patients were registered in an e-CRF by AEG-REDCap. Variables included demographics, previous eradication attempts, prescribed treatment, adverse events and outcomes. Data monitoring was performed to ensure data quality. Time-trend and geographical analyses were performed. Results 30 394 patients from 27 European countries were evaluated and 21 533 (78%) first-line empirical H. pylori treatments were included for analysis. Pretreatment resistance rates were 23% to clarithromycin, 32% to metronidazole and 13% to both. Triple therapy with amoxicillin and clarithromycin was most commonly prescribed (39%), achieving 81.5% modified intention-to-treat eradication rate. Over 90% eradication was obtained only with 10-day bismuth quadruple or 14-day concomitant treatments. Longer treatment duration, higher acid inhibition and compliance were associated with higher eradication rates. Time-trend analysis showed a region-dependent shift in prescriptions including abandoning triple therapies, using higher acid-inhibition and longer treatments, which was associated with an overall effectiveness increase (84%-90%). Conclusion Management of H. pylori infection by European gastroenterologists is heterogeneous, suboptimal and discrepant with current recommendations. Only quadruple therapies lasting at least 10 days are able to achieve over 90% eradication rates. European recommendations are being slowly and heterogeneously incorporated into routine clinical practice, which was associated with a corresponding increase in effectiveness

<i>N</i>-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide

Imatinib is one of the most used therapeutic agents to treat leukemia, which specifically inhibits the activity of tyrosine kinases. This polytopic molecule has been structurally characterized only in the form of its piperazin-1-ium salt (mesylate, picrate, citrate, fumarate or malonate). Herein we present the crystal structure of the freebase Imatinib which precipitated from a 1:10 mixture with arginine. The molecule realizes an extended conformation and forms infinite H-bonded chains through its amide, amine and pyrimidine groups

Novel Polymorph of Favipiravir—An Antiviral Medication

Various solid forms of pharmaceutically important compounds exhibit different physical properties and bioactivity; thus, knowledge of the structural landscape and prediction of spontaneous polymorph transformations for an active pharmaceutical ingredient is of practical value for the pharmaceutical industry. By recrystallization from ethyl acetate, a novel polymorph of 6-fluoro-3-hydroxypyrazine-2-carboxamide (trademark favipiravir, RNA polymerase inhibitor) was obtained and characterized using differential scanning calorimetry (DSC), infra-red spectroscopy and powder X-ray diffraction (XRD) analysis. The favipiravir molecule in two polymorphs realizes similar H-bonding motifs, but the overall H-bonded networks differ. Based on periodic density functional theory calculations, the novel tetragonal polymorph with two interpenetrated H-bonded networks is slightly less stable than the orthorhombic one with the zst topology of the underlying H-bonded net that is in accord with experimentally observed powder XRD patterns of slow conversion of the tetragonal phase to the orthorhombic one. However, topological analysis of net relations revealed that no transformations can be applied to convert H-bonded networks in the experimental unit cells, and DSC data indicate no solid-state reactions at heating

Novel Polymorph of Favipiravir—An Antiviral Medication

Various solid forms of pharmaceutically important compounds exhibit different physical properties and bioactivity; thus, knowledge of the structural landscape and prediction of spontaneous polymorph transformations for an active pharmaceutical ingredient is of practical value for the pharmaceutical industry. By recrystallization from ethyl acetate, a novel polymorph of 6-fluoro-3-hydroxypyrazine-2-carboxamide (trademark favipiravir, RNA polymerase inhibitor) was obtained and characterized using differential scanning calorimetry (DSC), infra-red spectroscopy and powder X-ray diffraction (XRD) analysis. The favipiravir molecule in two polymorphs realizes similar H-bonding motifs, but the overall H-bonded networks differ. Based on periodic density functional theory calculations, the novel tetragonal polymorph with two interpenetrated H-bonded networks is slightly less stable than the orthorhombic one with the zst topology of the underlying H-bonded net that is in accord with experimentally observed powder XRD patterns of slow conversion of the tetragonal phase to the orthorhombic one. However, topological analysis of net relations revealed that no transformations can be applied to convert H-bonded networks in the experimental unit cells, and DSC data indicate no solid-state reactions at heating

Dihydrogen Bonds in Salts of Boron Cluster Anions [BnHn]2− with Protonated Heterocyclic Organic Bases

Dihydrogen bonds attract much attention as unconventional hydrogen bonds between strong donors of H-bonding and polyhedral (car)borane cages with delocalized charge density. Salts of closo-borate anions [B10H10]2&minus; and [B12H12]2&minus; with protonated organic ligands 2,2&rsquo;-dipyridylamine (BPA), 1,10-phenanthroline (Phen), and rhodamine 6G (Rh6G) were selectively synthesized to investigate N&minus;H...H&minus;B intermolecular bonding. It was found that the salts contain monoprotonated and/or diprotonated N-containing cations at different ratios. Protonation of the ligands can be implemented in an acidic medium or in water because of hydrolysis of metal cations resulting in the release of H3O+ cations into the reaction solution. Six novel compounds were characterized by X-ray diffraction and FT-IR spectroscopy. It was found that strong dihydrogen bonds manifest themselves in FT-IR spectra that allows one to use this technique even in the absence of crystallographic data