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1.
Ultrason Sonochem ; 77: 105702, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34375945

RESUMO

2-picoline is a very important pyridine derivative with significant applications though it is also poisonous and harmful having considerable adverse influence on aquatic life, environment and organisms. The need for developing effective treatment methodologies for 2-Picoline directed the current work focusing on degradation of 2-Picoline using the combination of ultrasound and advanced oxidants such as hydrogen peroxide (H2O2), potassium persulphate (KPS), Fenton's reagent, and Peroxymonosulphate (PMS) along with the use of Titanium oxide (TiO2) as catalyst. Ultrasonic bath having 8 L capacity and operating frequency of 40 ± 2 kHz has been used. The effect of parameters like power, initial pH, temperature, time and initial concentration of 2-Picoline were studied to establish best operating conditions which were further used in the combination treatment approaches of ultrasound with oxidising agents. The chemical oxygen demand (COD) reduction for the optimized approaches of ultrasound in combination with oxidizing agents was also determined. Degradation experiments were performed using oxidising agents also in absence of ultrasound to investigate the individual treatment capacity of the oxidants and also the synergetic index for the combination. Kinetic study demonstrated that second order model suited for all the treatment approaches except US/Fenton where first order model fitted better. Ultrasound in combination with Fenton reagent demonstrated a substantial synergy for the degradation of 2-Picoline compared to other treatment approaches showing highest degradation of 97.6 %, synergetic index as 5.71, cavitational yield of 1.82 × 10-5 mg/J and COD removal of 82.4 %.


Assuntos
Oxidantes/química , Picolinas/química , Ondas Ultrassônicas , Concentração de Íons de Hidrogênio , Cinética , Temperatura
2.
J Environ Manage ; 295: 113080, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34186312

RESUMO

Unprecedented increases in agricultural nitrous oxide (N2O) emissions in recent years have caused substantial environmental pollution that leads to ozone depletion and global warming. Application of biochar and/or nitrification inhibitors (NIs) has the potential to reduce N2O emissions; however, it is not clear how biochar application may affect the efficacy of NI in reducing nitrification rates, soil enzyme activities, and N2O emissions under different soil moisture regimes. We conducted a 60-day laboratory incubation experiment to study the effects of manure biochar and nitrapyrin (as a NI) on N2O emissions from a urea fertilized soil with either 60 (low) or 80% (high) water-filled pore space (WFPS). Nitrification rates were significantly affected by biochar × NI × WFPS and biochar × WFPS interactions. Biochar initially increased and then decreased the rates, resulting in 45.2 and 26.6% (P < 0.001 for both) overall reductions in low and high WFPS, respectively while NI reduced the rates only in the first 10 days at 60% WFPS. Biochar decreased (P < 0.001) and NI increased (P = 0.007) ß-1,4-N-acetyl glucosaminidase activities while urease activities were increased (P < 0.001) by biochar across WFPS. Biochar had significant interaction with NI in cumulative N2O emissions with the efficacy of NI being reduced when co-applied with biochar. Cumulative N2O emissions were greater at high than at low WFPS; the emissions were decreased by biochar at 60% WFPS and NI at both 60 and 80% WFPS. We conclude that biochar reduces efficacy of nitrapyrin in mitigating N2O emissions and their effects on net nitrification rates, enzyme activities and N2O emissions are dependent on soil moisture level.


Assuntos
Nitrificação , Óxido Nitroso , Agricultura , Carvão Vegetal , Fertilizantes/análise , Óxido Nitroso/análise , Picolinas , Solo
3.
Artigo em Russo | MEDLINE | ID: mdl-33834719

RESUMO

OBJECTIVE: To study the efficacy and safety of complex treatment with 2-ethyl-3-hydroxy-6-methylpyridine (mexidol forte 250) and venotonic drugs L-lysine aescinat and diosmin/hesperidin in patients with chronic cerebral venous insufficiency (CCVI). MATERIAL AND METHODS: One hundred and twenty CCVI patients with clinical and ultrasonic signs of cerebral venous discirculation were studied. Patients were stratified into group 1 (n=40) treated perorally with mexidol forte 250 and diosmin/hesperidin during 74 days in combination with two courses of L-lysine aescinat intravenously on the 1st and 30th days from baseline, group 2 (n=40) treated with mexidol forte 250 and diosmin/hesperidin during 74 days, group 3 (n=40) treated perorally with diosmin/hesperidin during 74 days. RESULTS AND CONCLUSION: The efficacy and safety of the complex treatment of CCVI patients with venotonic drugs with the inclusion of mexidol forte 250 at a dose of 750 mg/day for 74 days is shown. The study demonstrates a significant positive effect of mexidol forte 250 on the dynamics of complaints and indicators of the neurological and psychoemotional status of patients. Monotherapy with the venotonic drug diosmin/hesperidin shows its insufficient efficacy.


Assuntos
Veias Cerebrais , Insuficiência Venosa , Antioxidantes , Humanos , Picolinas , Insuficiência Venosa/tratamento farmacológico
4.
Zh Nevrol Psikhiatr Im S S Korsakova ; 121(3. Vyp. 2): 60-66, 2021.
Artigo em Russo | MEDLINE | ID: mdl-33908234

RESUMO

OBJECTIVE: To study the possibility of improving the efficacy of treatment with mexidol in COVID-19 patients with chronic cerebral ischemia (CCI). MATERIAL AND METHODS: Three hundred and four patients with CCI and COVID-19 were observed, group 1 (n=152) consisted of patients receiving basic therapy and mexidol, group 2 (n=152) received only basic therapy. Mexidol was administered intravenously for 14 days, 500 mg (10 ml) per 400 ml of saline solution, then Mexidol FORTE 250 was administered in a dose of 250 mg 3 times a day for 2 months. The state of cognitive functions (MoCA scale), sleep (Spiegel questionnaire), asthenia (MFI-20 scale), and quality of life (SIP questionnaire) were evaluated. Examinations were performed before treatment, 30 and 75 days after start of treatment. RESULTS: In group 1, there was a more complete and earlier recovery of the state of cognitive functions (an increase in indicators on the MoCA scale, p<0.01), a regression of asthenia (p<0.05), and normalization of sleep (p<0.01). By the end of the study, there were significantly more patients in group 1 with complete or significant recovery of all quality of life indicators. CONCLUSION: Long-term sequential therapy with mexidol provides a more complete recovery of impaired functions in patients with CCI and COVID-19.


Assuntos
Isquemia Encefálica , COVID-19 , Astenia , Isquemia Encefálica/tratamento farmacológico , Humanos , Picolinas/uso terapêutico , Qualidade de Vida , SARS-CoV-2
5.
Am J Gastroenterol ; 116(6): 1156-1181, 2021 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-33767108

RESUMO

INTRODUCTION: Constipation is commonly treated with over-the-counter (OTC) products whose efficacy and safety remain unclear. We performed a systematic review of OTC therapies for chronic constipation and provide evidence-based recommendations. METHODS: We searched PubMed and Embase for randomized controlled trials of ≥4-week duration that evaluated OTC preparations between 2004 and 2020. Studies were scored using the US Preventive Services Task Force criteria (0-5 scale) including randomization, blinding, and withdrawals. The strengths of evidence were adjudicated within each therapeutic category, and recommendations were graded (A, B, C, D, and I) based on the level of evidence (level I, good; II, fair; or III, poor). RESULTS: Of 1,297 studies identified, 41 met the inclusion criteria. There was good evidence (grade A recommendation) for the use of the osmotic laxative polyethylene glycol (PEG) and the stimulant senna; moderate evidence (grade B) for psyllium, SupraFiber, magnesium salts, stimulants (bisacodyl and sodium picosulfate), fruit-based laxatives (kiwi, mango, prunes, and ficus), and yogurt with galacto-oligosaccharide/prunes/linseed oil; and insufficient evidence (grade I) for polydextrose, inulin, and fructo-oligosaccharide. Diarrhea, nausea, bloating, and abdominal pain were common adverse events, but no serious adverse events were reported. DISCUSSION: The spectrum of OTC products has increased and quality of evidence has improved, but methodological issues including variability in study design, primary outcome measures, trial duration, and small sample sizes remain. We found good evidence to recommend polyethylene glycol or senna as first-line laxatives and moderate evidence supporting fiber supplements, fruits, stimulant laxatives, and magnesium-based products. For others, further validation with more rigorously designed studies is warranted.


Assuntos
Constipação Intestinal/tratamento farmacológico , Defecação/efeitos dos fármacos , Fármacos Gastrointestinais/uso terapêutico , Medicamentos sem Prescrição/uso terapêutico , Bisacodil , Catárticos/uso terapêutico , Doença Crônica , Citratos , Frutas , Glucanos , Humanos , Inulina , Laxantes/uso terapêutico , Magnésio , Oligossacarídeos , Compostos Organometálicos , Picolinas , Polietilenoglicóis , Psyllium , Extrato de Senna , Iogurte
6.
Sensors (Basel) ; 21(5)2021 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-33670860

RESUMO

Gadolinium is extensively used in pharmaceuticals and is very toxic, so its sensitive detection is mandatory. This work presents the elaboration of a gadolinium chemical sensor based on 2-methylpyridine-substituted cyclam thin films, deposited on gold electrodes, using electrochemical impedance spectroscopy (EIS). The 2-methylpyridine-substituted cyclam (bis-N-MPyC) was synthesized in three steps, including the protection of cyclam by the formation of its CH2-bridged aminal derivative; the product was characterized by liquid 1H and 13C NMR spectroscopy. Spin-coated thin films of bis-N-MPyC on gold wafers were characterized by means of infrared spectroscopy in ATR (Attenuated Total Reflectance) mode, contact angle measurements and atomic force microscopy. The impedimetric chemical sensor was studied in the presence of increasing concentrations of lanthanides (Gd3+, Eu3+, Tb3+, Dy3+). Nyquist plots were fitted with an equivalent electrical circuit including two RC circuits in series corresponding to the bis-N-MPyC film and its interface with the electrolyte. The main parameter that varies with gadolinium concentration is the resistance of the film/electrolyte interface (Rp), correlated to the rate of exchange between the proton and the lanthanide ion. Based on this parameter, the detection limit obtained is 35 pM. The bis-N-MPyC modified gold electrode was tested for the detection of gadolinium in spiked diluted negative urine control samples.


Assuntos
Técnicas Biossensoriais , Ouro , Espectroscopia Dielétrica , Eletrodos , Gadolínio , Compostos Heterocíclicos , Limite de Detecção , Picolinas
7.
Environ Sci Technol ; 55(3): 1345-1353, 2021 02 02.
Artigo em Inglês | MEDLINE | ID: mdl-33433195

RESUMO

Agricultural production and associated applications of nitrogen (N) fertilizers have increased dramatically in the last century, and current projections to 2050 show that demands will continue to increase as the human population grows. Applied in both organic and inorganic fertilizer forms, N is an essential nutrient in crop productivity. Increased fertilizer applications, however, create the potential for more N loss before plant uptake. One strategy for minimizing N loss is the use of enhanced efficiency fertilizers, fortified with a nitrification inhibitor, such as nitrapyrin. In soils and water, nitrapyrin inhibits the activity of ammonia monooxygenase, a microbial enzyme that catalyzes the first step of nitrification from ammonium to nitrite. Potential benefits of using nitrification inhibitors range from reduced nitrate leaching and nitrous oxide emissions to increased crop yield. The extent of these benefits, however, depends on environmental conditions and management practices. Thus, such benefits are not always realized. Additionally, nitrapyrin has been shown to transport off-field, and it is unknown what effects environmental nitrapyrin could have on nontarget organisms and the ecological nitrogen cycle. Here, we review the agronomic and environmental benefits and costs of nitrapyrin use and present a series of research questions and considerations to be addressed with future nitrification inhibitor research.


Assuntos
Ecossistema , Nitrificação , Agricultura , Análise Custo-Benefício , Saúde Ambiental , Fertilizantes/análise , Humanos , Nitrogênio/análise , Óxido Nitroso/análise , Picolinas , Solo
8.
J Med Chem ; 64(2): 909-924, 2021 01 28.
Artigo em Inglês | MEDLINE | ID: mdl-33470111

RESUMO

Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of advanced prostate cancer. One resistance mechanism is point mutations in the ligand binding domain of AR that can transform antagonists into agonists. The AR F877L mutation, identified in patients treated with enzalutamide or apalutamide, confers resistance to both enzalutamide and apalutamide. Compound 4 (JNJ-pan-AR) was identified as a pan-AR antagonist with potent activity against wild-type and clinically relevant AR mutations including F877L. Metabolite identification studies revealed a latent bioactivation pathway associated with 4. Subsequent lead optimization of 4 led to amelioration of this pathway and nomination of 5 (JNJ-63576253) as a clinical stage, next-generation AR antagonist for the treatment of castration-resistant prostate cancer (CRPC).


Assuntos
Antagonistas de Receptores de Andrógenos/farmacologia , Nitrilas/farmacologia , Picolinas/farmacologia , Piperidinas/farmacologia , Neoplasias de Próstata Resistentes à Castração/tratamento farmacológico , Neoplasias da Próstata/tratamento farmacológico , Piridinas/farmacologia , Compostos de Espiro/farmacologia , Antagonistas de Receptores de Andrógenos/farmacocinética , Antagonistas de Receptores de Andrógenos/uso terapêutico , Animais , Biotransformação , Linhagem Celular Tumoral , Cães , Descoberta de Drogas , Resistencia a Medicamentos Antineoplásicos/genética , Hepatócitos/metabolismo , Humanos , Masculino , Modelos Moleculares , Mutação , Nitrilas/farmacocinética , Nitrilas/uso terapêutico , Picolinas/farmacocinética , Picolinas/uso terapêutico , Piperidinas/farmacocinética , Piperidinas/uso terapêutico , Neoplasias da Próstata/genética , Neoplasias de Próstata Resistentes à Castração/genética , Piridinas/farmacocinética , Piridinas/uso terapêutico , Ratos , Compostos de Espiro/farmacocinética , Compostos de Espiro/uso terapêutico , Relação Estrutura-Atividade
9.
J Sci Food Agric ; 101(5): 1772-1781, 2021 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-32892367

RESUMO

BACKGROUND: Nitrification inhibitors (NIs) and urease inhibitors (UIs) can decrease the risk of nitrogen (N) loss and extend N uptake by plants. However, there are few case studies about reduced N application combined with double inhibitors (DIs, NI plus UI), especially under drip irrigation systems. A 2-year field experiment was therefore conducted to explore the effect of 80% N application rate combined with NI or DIs on soil N transformation, wheat productivity and N use efficiency (NUE) in a drip-irrigated field. The four treatments included a no-fertilizer control, 100% urea, 80% urea + NI (nitrapyrin) and 80% urea + DIs (nitrapyrin and N-(n-butyl) thiophosphorictriamide (NBPT)). RESULTS: Our results showed that the 80% urea + DIs treatment significantly increased the ratio of NH4 + to NO3 - and N content (urea-N, NH4 + -N and NO3 - -N) in soil at 0-20 cm depth (P < 0.05) at the heading stage and the filling stage of wheat in both 2013 and 2014, relative to the 100% urea treatment. A total of 80% urea + NI treatment decreased wheat N uptake and wheat productivity (plant biomass and yield) compared to 100% urea treatments (P < 0.05). However, application of 80% urea combined with DIs achieved equivalent wheat productivity with 100% urea treatment. Moreover, the greatest NUE (43.6%) was recorded with the application of DIs. CONCLUSIONS: Cutting the N application rate by 20% combined with NBPT and nitrapyrin could provide a sustainable fertilization strategy for wheat production under drip irrigation. © 2020 Society of Chemical Industry.


Assuntos
Produção Agrícola/métodos , Nitrogênio/análise , Compostos Organofosforados/farmacologia , Picolinas/farmacologia , Triticum/efeitos dos fármacos , Triticum/crescimento & desenvolvimento , Irrigação Agrícola , Fertilizantes/análise , Nitrificação , Nitrogênio/metabolismo , Solo/química , Triticum/metabolismo , Ureia/análise , Ureia/metabolismo
10.
Rev Esp Enferm Dig ; 113(9): 635-642, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33371690

RESUMO

BACKGROUND: There are contradictory results about the effect of magnesium citrate plus sodium picosulfate bowel cleansing agents on the fluid and electrolyte balance. Therefore, this study aimed to determine the efficacy, tolerability and safety of this medication in colonoscopy preparation. METHODS: 233 patients were enrolled in this phase IV prospective observational study. The effectiveness of bowel cleansing was assessed using the Boston Bowel Preparation Scale (BBPS). Adequate cleansing was defined as BBPS ≥ 6 and excellent cleansing as BBPS > 7. Tolerability was examined using a standardized questionnaire. In the safety analysis, the change of serum electrolytes levels and renal function during bowel cleansing was assessed. RESULTS: Adequate and excellent bowel cleansing were achieved 94.85% and 72.96% of cases, respectively. None or very mild symptoms were reported in 47.21% of cases. Statistically significant changes occurred in serum potassium (4.38±0.43 vs. 4.25±0.43 mmol/L, p<0.0001), urea (4.86±1.37 vs. 3.84±1.43 mmol/L, p<0.0001) and creatinine (male: 81.07±16.02 vs. 84.54±15.11 µmol/L; female: 69.32±12.22 vs. 72.96±12.11 µmol/L, p<0.0001) levels during the colonoscopy preparation. However, the number of patients with values outside of the normal range increased significantly only in the case of serum urea (3.95% vs. 26.97%, p<0.0001). CONCLUSION: Magnesium citrate with sodium picosulfate is outstandingly effective, well tolerated and a safe agent in colonoscopy preparation. It caused significant, but non-clinically relevant changes in serum electrolytes levels and renal function.


Assuntos
Catárticos , Compostos Organometálicos , Catárticos/efeitos adversos , Citratos/efeitos adversos , Ácido Cítrico , Colonoscopia , Feminino , Humanos , Masculino , Compostos Organometálicos/efeitos adversos , Picolinas/efeitos adversos , Polietilenoglicóis
11.
Nat Commun ; 11(1): 6226, 2020 12 04.
Artigo em Inglês | MEDLINE | ID: mdl-33277485

RESUMO

Protein N-phosphorylation plays a critical role in central metabolism and two/multicomponent signaling of prokaryotes. However, the current enrichment methods for O-phosphopeptides are not preferred for N-phosphopeptides due to the intrinsic lability of P-N bond under acidic conditions. Therefore, the effective N-phosphoproteome analysis remains challenging. Herein, bis(zinc(II)-dipicolylamine)-functionalized sub-2 µm core-shell silica microspheres (SiO2@DpaZn) are tailored for rapid and effective N-phosphopeptides enrichment. Due to the coordination of phosphate groups to Zn(II), N-phosphopeptides can be effectively captured under neutral conditions. Moreover, the method is successfully applied to an E.coli and HeLa N-phosphoproteome study. These results further broaden the range of methods for the discovery of N-phosphoproteins with significant biological functions.


Assuntos
Microesferas , Compostos Organometálicos/química , Fosfoproteínas/metabolismo , Picolinas/química , Proteoma/análise , Proteômica/métodos , Dióxido de Silício/química , Proteínas de Escherichia coli/análise , Células HeLa , Células Hep G2 , Humanos , Proteínas de Neoplasias/análise , Tamanho da Partícula , Fosfopeptídeos/análise , Reprodutibilidade dos Testes , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz/métodos
12.
Artigo em Russo | MEDLINE | ID: mdl-33340299

RESUMO

OBJECTIVE: To study of efficacy and safety of mexidol used as intravenous infusion for 14 days, followed by per os treatment with mexidol FORTE 250 for 60 days in patients with chronic brain ischemia (CHM) complicated with arterial hypertension and atherosclerosis. MATERIAL AND METHODS: The mexidol group included 27 patients (24 women and 3 men) with CHM I-II gr and the combination of arterial hypertension and atherosclerosis who received intravenous infusions of mexidol (500 mg once daily) within 14 days, with the subsequent per os treatment with mexidol FORTE 250 in a daily dose of 750 mg (1 tablet 3 times a day) for 60 days. The comparison group consisted of 30 patients (22 women and 8 men) with CHM I-II gr, comparable in age, nature of risk factors and expression of neurological manifestations. Patients in both groups received basic medications to treat their risk factors. Motor activity (Tinetti test), cognitive functions (MoCa test), anxiety and depression (Hamilton anxiety and depression scale), clinical condition (General Clinical Impression scale) were assessed. RESULTS AND CONCLUSION: Inclusion of mexidol (500 mg iv infusion once a day within 14 days with the subsequent oral administration of 750 mg (1 tablet 3 times a day) for 60 days) in standard therapy of arterial hypertension with atherosclerosis and chronic brain ischemia is expedient. The results show greater clinical efficacy and sufficient safety of such combination therapy. By the end of therapy (day 74), patients in the mexidol group have a reliable improvement in motor activity, cognitive function and psychoemotional sphere, as well as a decrease in fatigue and neurological manifestations compared with the comparison group.


Assuntos
Isquemia Encefálica , Picolinas , Isquemia Encefálica/complicações , Isquemia Encefálica/tratamento farmacológico , Feminino , Humanos , Isquemia , Masculino , Picolinas/efeitos adversos , Resultado do Tratamento
13.
Artigo em Russo | MEDLINE | ID: mdl-33340300

RESUMO

OBJECTIVE: In order to develop methods and means of maintaining normal human functioning under conditions of desynchronizes, the effect of mexidol on the level of corticosterone in the blood serum and the state of the cells of the beam zone of the adrenal cortex of rats after light or dark deprivation and physical activity to a state of fatigue. MATERIALS AND METHODS: The experiments were performed on 7 groups of rats (10 animals each) in the spring. The model of physical activity is the method of forced swimming of rats until exhaustion in its own modification. For the induction of experimental desynchronizes, the animals of the experimental groups were kept around the clock for 10 days with artificial bright light of 150 LX or a complete darkening of 2-3 LX. Mexidol was administered intramuscularly at a dose of 10 mg/kg animal 30 minutes before the swimming test. Control animals under similar conditions were administered 0.9% sodium chloride solution. The level of corticosterone in the serum was determined using enzyme immunoassay. The measurements were carried out on a programmable photometer for STAR FAX 303 PLUS microsamples (USA). Histological analysis of the adrenal glands was carried out according to standard methods. Microscopy of preparations, imaging and measurements were carried out using an Axio Lab A1 microscope, an AxioCamERc 5s camera and ZEN 2012 software («Carl Zeiss Microscopy¼, Germany). Statistical processing of the results was carried out using standard parametric and non-parametric methods, depending on the nature of the distributions. RESULTS AND CONCLUSION: Mexidol under combined successive stress loads - desynchronizes and physical activity - demonstrated anti-stress properties not only at the level of corticosterone in the blood serum of rats, but also at the level of adrenal glands. The severity of this effect of the drug depended on the number of stress loads (isolated physical or shown in conditions of desynchronizes), the phase of stress and the nature of deprivation. Under natural lighting conditions and after light deprivation, when animals were in the anxiety phase of varying severity, the drug worked more reliably than after dark deprivation in conditions of developing depletion. Nevertheless, even in the latter case, he showed himself as a means of preventing exhaustion in animals and the breakdown of adaptation.


Assuntos
Picolinas , Soro , Animais , Corticosterona , Alemanha , Masculino , Ratos
14.
World J Gastroenterol ; 26(40): 6260-6269, 2020 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-33177798

RESUMO

BACKGROUND: Bowel preparation in children can be challenging. AIM: To describe the efficacy, safety, and tolerability of sodium picosulfate, magnesium oxide, and citric acid (SPMC) bowel preparation in children. METHODS: Phase 3, randomized, assessor-blinded, multicenter study of low-volume, divided dose SPMC enrolled children 9-16 years undergoing elective colonoscopy. Participants 9-12 years were randomized 1:1:1 to SPMC ½ dose × 2, SPMC 1 dose × 2, or polyethylene glycol (PEG). Participants 13-16 years were randomized 1:1 to SPMC 1 dose × 2 or PEG. PEG-based bowel preparations were administered per local protocol. Primary efficacy endpoint for quality of bowel preparation was responders (rating of 'excellent' or 'good') by modified Aronchick Scale. Secondary efficacy endpoint was participant's tolerability and satisfaction from a 7-item questionnaire. Safety assessments included adverse events (AEs) and laboratory evaluations. RESULTS: 78 participants were randomized, 48 were 9-12 years, 30 were 13-16 years. For the primary efficacy endpoint in 9-12 years, 50.0%, 87.5%, and 81.3% were responders for SPMC ½ dose × 2, SPMC 1 dose × 2, and PEG groups, respectively. Responder rates for 13-16 years were 81.3% for SPMC 1 dose × 2 and 85.7% for PEG. Overall, 43.8% of participants receiving SPMC 1 dose × 2 reported it was 'very easy' or 'easy' to drink, compared with 20.0% receiving PEG. Treatment-emergent AEs were reported by 45.5% of participants receiving SPMC 1 dose × 2 and 63.0% receiving PEG. CONCLUSION: SPMC was an efficacious and safe for bowel preparation in children 9-16 years, with comparable efficacy to PEG. Tolerability for SPMC was higher compared to PEG.


Assuntos
Óxido de Magnésio , Compostos Organometálicos , Catárticos/efeitos adversos , Criança , Citratos/efeitos adversos , Ácido Cítrico/efeitos adversos , Colonoscopia , Humanos , Óxido de Magnésio/efeitos adversos , Compostos Organometálicos/efeitos adversos , Picolinas , Polietilenoglicóis/efeitos adversos
15.
West Afr J Med ; 37(6): 656-661, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33185262

RESUMO

BACKGROUND: The cost and availability are among factors that determine bowel preparation regimen for colonoscopy. AIMS: To assess the efficacy of an alternative bowel preparation regimen of Castor oil/Bisacodyl (CaO/B) for colonoscopy in a limited resource setting. MATERIALS AND METHODS: A retrospective cohort study of patients undergoing colonoscopy in an endoscopy referral centre in Port Harcourt Rivers State Nigeria from June 2014 to September 2019. Patients who had bowel preparation prior to colonoscopy with CaO/B were grouped and compared with a control group of patients that received sodium picosulphate magnesium citrate (SPMC). The variables collated were sociodemographics, primary indication, comorbidities, quality of bowel preparation (Aronchick scale), polyp detection and caecal intubation. Statistical analysis was performed using IBM SPSS version 21. RESULTS: A total of 258 patients undergoing colonoscopy met the inclusion criteria with 118 prepared with CaO/B and 140 patients with SPMC. The mean age of patients in the groups were 53.9 ± 11.2 years and 54.7 ± 12.8 years respectively; a total of 192 males and 66 females with a near even distribution in both groups. Bowel preparation was Excellent/Good in 51 patients using CaO/B and 108 for SPMC (p = <0.0001). No statistical difference was noted in the caecal intubation and polyp detection rates between the 2 groups- p values 0.395 and 0.990 respectively. CONCLUSION: Castor oil/ Bisacodyl regimen is cheap but not consistently associated with adequate bowel preparation for colonoscopy. Expertise of endoscopists and copious lavage are crucial when CaO/B regimen is used for bowel cleansing.


Assuntos
Bisacodil , Óleo de Rícino , Adulto , Idoso , Catárticos , Citratos , Ácido Cítrico , Colonoscopia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Nigéria , Compostos Organometálicos , Picolinas , Polietilenoglicóis , Estudos Retrospectivos
16.
Artigo em Russo | MEDLINE | ID: mdl-33244953

RESUMO

OBJECTIVE: To evaluate the efficacy and safety of sequential therapy with mexidol (solution for intravenous and intramuscular injections) and mexidol forte 250 (coated tablets) in acute and early recovery stages of hemispheric ischemic stroke. MATERIAL AND METHODS: The changes in scores on the modified Rankin Scale (mRs) (primary endpoint), the National Institute of Health Stroke Scale (NIHSS), the Bartel Index (BI), the Montreal Cognitive Assessment (MoCa), the Beck Depression Inventory (BDI), the EuroQol Quality of Lifes Scale ( EQ-5D) were assessed in the end of treatment (secondary endpoint). RESULTS AND CONCLUSION: Prolonged and sequential therapy with mexidol at the dose 500 mg daily during 14 days (saturation phase) and mexidol forte 250 at the dose of 250 mg three times a day during 60 days (maximum therapeutic effect) provides additional opportunities for a more complete recovery in acute and early recovery stages of hemispheric ischemic stroke (increases quality of life, improves movement and cognitive functions).


Assuntos
Isquemia Encefálica , Acidente Vascular Cerebral , Isquemia Encefálica/tratamento farmacológico , Humanos , Picolinas , Qualidade de Vida , Acidente Vascular Cerebral/tratamento farmacológico , Resultado do Tratamento
17.
Zh Nevrol Psikhiatr Im S S Korsakova ; 120(8. Vyp. 2): 49-57, 2020.
Artigo em Russo | MEDLINE | ID: mdl-33016677

RESUMO

AIM: To evaluate the efficacy and safety of prolonged sequential therapy with mexidol in the acute and early recovery stages of hemispheric ischemic stroke (IS) across age groups according to the World Health Organization classification. MATERIAL AND METHODS: The study is an additional analysis across age groups among patients participated in the randomized double blind multicenter placebo-controlled, in parallel groups trial EPICA. All subjects (62 men and 88 women) were subdivided into age groups: younger than 60 years, 60-65 years, 76-90 years. Additionally, all participants were divided into 2 populations: ITT (Intent to treat population, patients who received at least one treatment/placebo dose) and PP (Per protocol population, patients who received treatment per study protocol). Results of Modified Rankin scale (mRs) at the end of treatment period, Barthel index, Beck depression inventory, European Quality of Life Questionnaire were assessed. RESULTS: The efficacy of mexidol assessed with all the scales did not differ depending on the age group. By the end of treatment, the mean mRS score was lower in the 76-90 years subgroup (in both populations), compared to placebo (p<0.001). The decrease in mean mRS score (Visit 1-5) was more prominent in patients aged 60-65 years (p=0.025), including patients with diabetes mellitus (DM). Patients aged 76-90 years and patients with DM, compared to placebo, had a decrease of the severity of cognitive-affective depression symptoms (p=0.049 and p=0.02) and an increase in patients without problems with everyday activities (p=0.007 and p=0.02). Patients with DM, compared to placebo, also had the higher levels of everyday activity (p=0.023) and quality of life (p=0.045). There were no statistically significant differences in the frequency of side-effects in patients of all groups. CONCLUSION: It is recommended to include mexidol in therapy of patients with IS in the acute and early rehabilitation stages in all age groups, including patients with DM.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Acidente Vascular Cerebral/tratamento farmacológico , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Picolinas/efeitos adversos , Picolinas/uso terapêutico , Qualidade de Vida
18.
J Toxicol Sci ; 45(8): 503-513, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32741900

RESUMO

Creatine kinase (CK) and lactate dehydrogenase (LDH) serve as biomarkers for skeletal muscle injury in preclinical toxicity studies, but have a limitation regarding tissue specificity. Circulating miR-206 was recently reported to be a useful biomarker for skeletal muscle disorders in humans. Here, we sought to determine whether serum miR-206 can be used as a biomarker in preclinical toxicity studies to detect drug-induced skeletal muscle injury with higher sensitivity and specificity than the biomarkers CK, LDH, skeletal troponin I (sTnI), and myosin light chain 3 (Myl3). We established rat models of skeletal muscle injury through treatment with the muscle toxicant 2,3,5,6-tetramethyl-p-phenylenediamine (TMPD) as well as four in-house compounds. We found that serum miR-206 levels significantly increased after treatment with TMPD, and tended to be higher in rats treated with in-house compounds than in control rats. ROC analysis revealed that the specificity of serum miR-206 for detection of skeletal muscle injury was higher compared with those of other markers. Further, serum miR-206 levels were unchanged in rats with isoproterenol-induced cardiotoxicity. These findings demonstrate that serum miR-206 may serve as a highly specific biomarker for preclinical analysis of rats with drug-induced skeletal muscle injuries.


Assuntos
MicroRNAs/sangue , Músculo Esquelético , Doenças Musculares/induzido quimicamente , Doenças Musculares/diagnóstico , Picolinas/toxicidade , Animais , Biomarcadores/sangue , Modelos Animais de Doenças , Masculino , Especificidade de Órgãos , Curva ROC , Ratos Endogâmicos F344 , Ratos Sprague-Dawley , Sensibilidade e Especificidade
19.
Artigo em Russo | MEDLINE | ID: mdl-32678558

RESUMO

Chronic cerebral ischemia (CCI) is a common cerebrovascular syndrome, the development of which is associated with a high risk of increasing cognitive, behavioral, and motor disorders, and the formation of a patient's dependence on others. Timely start of treatment can slow down the course of the disease, make it more favorable. The review considers the possibility of using the domestic neuroprotector mexidol in patients with CCI. The results of a series of clinical studies on the use of ethylmethylhydroxypyridine succinate (mexidol) in patients with CCI are analyzed. The effectiveness of the drug in relieving cognitive, affective and motor disorders is noted. Information about the good tolerance of mexidol is presented.


Assuntos
Isquemia Encefálica , Antioxidantes , Doença Crônica , Humanos , Picolinas , Piridinas
20.
Artigo em Russo | MEDLINE | ID: mdl-32621483

RESUMO

A review of the current literature on the possible use of mexidol (ethylmethylhydroxypyridine succinate) in the treatment of mental (including addictive) disorders is conducted. The possibility of its use to reduce negative psychopathological symptoms, neurocognitive deficit, manifestations of the antipsychotic syndrome (including its extrapyramidal disorders) in antipsychotic treatment of patients with schizophrenia spectrum disorders and insomnia disorders in the complex therapy of borderline mental disorders has been shown. The potential of mexidol in the treatment of addictive pathology, as well as the effects of intoxication caused by alcohol and other psychoactive (including narcotic) substances, deserves special attention.


Assuntos
Esquizofrenia , Antipsicóticos , Humanos , Picolinas
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