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RESUMEN Los inhibidores de la bomba de protones (IBP) son los medicamentos más potentes para inhibir la secreción gástrica ácida, y se utilizan en el tratamiento de la mayor parte de las afecciones inflamatorias de la mucosa gástrica. Forman parte de los fármacos más recetados y sobreprescritos en todo el mundo; por ejemplo, en los Estados Unidos, según la Encuesta nacional de salud y nutrición, casi duplicaron su uso en los adultos de 40 años de un 4,9 % hasta un 8,3 %, entre los años 1999 a 2012. Aunque, en general, se consideran bien tolerados, algunos estudios epidemiológicos ―que extraen información a partir de grandes bases de datos― han reportado una serie de efectos adversos asociados con su uso prolongado, entre los cuales están el deterioro cognitivo, la enfermedad renal crónica, el infarto de miocardio, el accidente cerebrovascular, las fracturas óseas e incluso la muerte, entre otros. El objetivo fue realizar una revisión narrativa de la literatura acerca de los efectos del uso crónico de los IBP sobre el deterioro cognitivo en los adultos mayores. Se revisaron artículos a partir de una búsqueda en las bases de datos Pudmed, Scopus y Scielo con las palabras clave y términos Mesh/DeCS relacionados tanto en inglés como en español. Los efectos secundarios a nivel neurológico inducidos por el uso crónico de los IBP pueden estar relacionados indirectamente con la presencia de alteraciones sistémicas secundarias (deficiencia de magnesio y vitamina B12) o con efectos directos sobre el funcionamiento neuronal después de pasar a través de la barrera hematoencefálica. Si bien se han descrito varios mecanismos neurobiológicos por medio de los cuales los IBP podrían favorecer el desarrollo de la demencia ―que comprenden el funcionamiento de la proteína tau, la acumulación de beta amiloide (βA) y la deficiencia de cobalamina, entre otros―, la mayor parte de la evidencia clínica disponible no ha encontrado una asociación significativa entre el uso de los IBP y el riesgo de demencia o el deterioro cognitivo. Para establecer de una manera más clara los efectos clínicos adversos del uso crónico de los IBP, en especial, en el funcionamiento cerebral, se necesitan estudios de cohorte bien diseñados, con tamaños de muestra grandes y periodos de seguimiento prolongados, con un método confiable para ajustar los factores de confusión estandarizados y, además, realizar análisis por subgrupos.
ABSTRACT Proton pump inhibitors (PPIs) are the most potent drugs to inhibit gastric acid secretion, being used in the treatment of most inflammatory conditions of the gastric mucosa. They are among the most prescribed and overprescribed medications worldwide; for example, in the United States, according to the National Health and Nutrition Examination Survey, they almost doubled their use in adults aged 40 years and older from 4.9 % to 8.3 % between 1999 and 2012. Although they are generally considered well tolerated, some epidemiological studies extracting information from large databases have reported a number of adverse effects associated with their prolonged use, including cognitive impairment, chronic kidney disease, myocardial infarction, stroke, bone fractures and even death, among others. The objective was to conduct a narrative review of the literature on the effects of chronic use of PPIs on cognitive impairment in older adults. Articles were reviewed based on a search in the PubMed, Scopus and SciELO databases using both English and Spanish keywords and related MeSH/DeCS terms. Neurological side effects induced by chronic PPI use may be indirectly related to secondary systemic disorders (magnesium and vitamin B12 deficiency) or to direct effects on neuronal functioning after passing through the blood-brain barrier. Although several neurobiological mechanisms by which PPIs could favor the development of dementia-which involve Tau protein function, beta-amyloid [βA] accumulation and cobalamin deficiency, among others-have been described, most of the available clinical evidence has not shown a significant association between PPI use and the risk of dementia or cognitive impairment. To establish the adverse clinical effects of chronic PPI use more clearly, especially on brain functioning, well-designed cohort studies with large sample sizes and long follow-up periods, with a reliable method to adjust for standardized confounders, as well as subgroup analyses are needed.
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Background: Esomeprazole, an S-isomer of omeprazole, is a much more potent acid inhibitor than most other currently available PPIs and gives excellent results. Therefore, it is a first-line drug for acid-related diseases like NonErosive Reflux Disease (NERD). Yet, patients demand faster onset and response. Aim : To establish the role of esomeprazole and the importance of anti-reflux agents like a combination of two antacids (calcium carbonate and sodium bicarbonate) and alginate in treating NERD. Conclusion: Esomeprazole therapy shows potential efficacy in the continuous maintenance treatment of the NERD. However, it is suggested that to improve the efficiency of esomeprazole for the treatment of NERD; we can supplement the drug with antacids (sodium bicarbonate and calcium carbonate) and alginates.
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Objective:To investigate the inhibitory effect of esomeprazole on proliferation and chemosensitizing effect of breast cancer cells.Methods:Human MBA-MD-231, MCF-7 breast cancer cell line and human Huh7 liver cancer cell line were cultured by conventional methods; cells were treated with different concentrations of esomeprazole, and CCK8 kit was used to detect the proliferation of different tumor cells after stimulation. Cells were treated with different concentrations of esomeprazole, and the effects of esomeprazole on cell cycle of different cells were analyzed by flow cytometry. Cells were treated with different concentrations of paclitaxel and epirubicin combined with esomeprazole, and CCK8 kit was used to detect the proliferation of different tumor cells after stimulation. Measurement data were expressed as mean ± standard deviation ( ± s), and analysis of variance was used for comparison among multiple groups. Results:CCK8 results showed that esomeprazole could inhibit the proliferation of MBA-MD-231 cells, MCF-7 cells and Huh7 cells in a dose-dependent manner. Flow cytometry results showed that cells in G 0/G 1 phase were significantly increased by esomeprazole treatment. Esomeprazole can enhance the inhibitory effect of paclitaxel and epirubicin on the proliferation of MBA-MD-231 cells and MCF-7 cells, and improve the chemosensitivity. Conclusion:Esomeprazole blocks breast cancer cell MBA-MD-231, MCF-7 and liver cancer cell Huh7 in G 0/G 1 phase, thereby inhibiting cell proliferation. Esomeprazole can enhance the inhibitory effect of chemotherapeutic drugs on the proliferation of MBA-MD-231 and MCF-7 cells.
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Changes in structure of oral solid dosage forms (OSDF) elementally determine the drug release and its therapeutic effects. In this research, synchrotron radiation X-ray micro-computed tomography was utilized to visualize the 3D structure of enteric coated pellets recovered from the gastrointestinal tract of rats. The structures of pellets in solid state and in vitro compendium media were measured. Pellets in vivo underwent morphological and structural changes which differed significantly from those in vitro compendium media. Thus, optimizations of the dissolution media were performed to mimic the appropriate in vivo conditions by introducing pepsin and glass microspheres in media. The sphericity, pellet volume, pore volume and porosity of the in vivo esomeprazole magnesium pellets in stomach for 2 h were recorded 0.47, 1.55 × 108 μm3, 0.44 × 108 μm3 and 27.6%, respectively. After adding pepsin and glass microspheres, the above parameters in vitro reached to 0.44, 1.64 × 108 μm3, 0.38 × 108 μm3 and 23.0%, respectively. Omeprazole magnesium pellets behaved similarly. The structural features of pellets between in vitro media and in vivo condition were bridged successfully in terms of 3D structures to ensure better design, characterization and quality control of advanced OSDF.
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OBJECTIVE：To develop a metho d for determining the plasma concentration of sulfasalazine （SSZ）metabolite sulfapyridine（SP）in rats ，and to investigate the effects of esomeprazole （ESOM）on the pharmacokinetic behavior of SSZ in rats. METHODS：Male SD rats were randomly divided into SSZ group and SSZ+ESOM group ，with 6 rats in each group. SSZ+ESOM group were given Esomeprazole enteric-coated tablets [ 90 mg/（kg·d）] intragastrically for 14 days. On the 15th day ，the rats in 2 groups were given Sulfasalazine enteric coated tablets （90 mg/kg）intragastrically，and blood sample was collected from the inner canthus at 0.5，1，1.5，2，3，4，6，8，10，12，24，36，48，72 h after administration. After protein precipitation with methanol ， using diazepam as internal standard ，Agilent XDR-C 18 column was adopted with methanol- 0.1％ formic acid solution （gradient elution）as mobile phase. The concentration of SSZ metabolite SP in plasma was determined by LC-MS/MS. The pharmacokinetic parameters were calculated by using DAS 3.0.1 software and compared between 2 groups. RESULTS ：The linear range of SP were 2-1 000 ng/mL. The methodology met the requirements of Chinese Pharmacopeia . There was no statistical significance in pharmacokinetic parameters of SP between 2 groups，such as AUC 0－t，tmax，t1/2z，cmax，MRT0－t（P＞0.05）. CONCLUSIONS ：The established method is simple ，rapid and sensitive ；it can be used for the concentration determination of SSZ metabolite SP in plasma. ESOM has no significant effect on the pharmacokinetic behavior of SSZ in rats.
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Objective:To explore the efficacy and safety of intermittent infusion of ilaprazole sodium and high-dose continuous infusion of esomeprazole sodium in preventing rebleeding in patients with peptic ulcer bleeding after successful endoscopic hemostasis.Methods:This is a multi-center, interval randomized, double-blind, double-dummy, parallel controlled study. From March 3rd to June 15th, 2021, 151 patients with high risk of peptic ulcer bleeding and successfully underwent endoscopic hemostasis from 33 hospitals including the First Affiliated Hospital of Zhejiang University School of Medicine were enrolled. Patients were interval randomly divided into the trial group (74 cases) and the control group (77 cases). Patients in the trial group received intermittent intravenous infusion of ilaprazole sodium once daily (20 mg administered as a 60 min intravenous infusion on day 1, and 10 mg administered as a 30 min intravenous infusion on day 2 and 3); patients in the control group received continuous intravenous infusion of esomeprazole sodium for 72 h (esomeprazole sodium 80 mg at first dose in half an hour, and 8 mg per hour continuous intravenous infusion for 71.5 h). After intravenous infusion treatment, patients of both groups were given oral ilaprazole enteric-coated tablets, 10 mg each time, once a day for 4 d. The rebleeding rate after 72 h and within 7 d after treatment and the proportion of patients who received endoscopic retreatment or surgery due to rebleeding within 72 h after treatment were analysised based on the full analysis set (72 cases in the trial group and 75 cases in the control group); and the incidence rate of adverse reactions was observed in the two groups based on the safety analysis set (74 cases in the trial group and 76 cases in the control group). Chi-square test or Fisher exact probability test was used for statistical analysis.Results:There was no rebleeding case in the trial group within 72 h and 1 case of rebleeding within 7 d (1.39%, 1/72). In the control group, there was 1 case of rebleeding (1.33%, 1/75) within 72 h and 4 cases of rebleeding (5.33%, 4/75) within 7 d. There was no significant difference in rebleeding rate either after 72 h or within 7 d after treatment between the two groups (both P>0.05). Within 72 h of treatment, no patients in both groups needed endoscopic or surgical retreatment due to rebleeding. Adverse reactions occurred in 5 cases (6.8%, 5/74) and 6 cases (7.9%, 6/76) in the trial group and control group, respectively, which recovered spontaneously without treatment. No serious adverse reactions occurred in both groups. Conclusion:In patients with high-risk peptic ulcer bleeding with successful endoscopic hemostasis, intermittent intravenous infusion of ilaprazole sodium has similar efficacy and safety as continuous high-dose intravenous infusion of esomeprazole sodium, but the dosage of intermitten regimen is less, the administration is more convenient, and it is worthy of clinical promotion.
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Objective:To evaluate the clinical efficacy of Wanfu-Qutong Decoction combined with esomeprazole in the treatment of chronic atrophic gastritis (CAG). Methods:A total of 106 CAG patients who met the inclusion criteria from June 2017 to June 2019 were randomly divided into two groups with 53 in each group. The control group took esomeprazole magnesium enteric coated tablets, and the observation group took Wanfu-Qutong Decoction on the basis of the control group. Both groups were treated continuously for 3 months. TCM syndrome score was performed before and after treatment, and the new Sydney system intuitive simulation score method was used to score the histopathology of gastric mucosa. The levels of gastrin 17 (G-17), pepsinogen (PGⅠ , PGⅡ) and the PG Ⅰ/Ⅱ were measured by ELISA. Results:The total effective rate was 96.2% (51/53) in the observation group and 79.2% (42/53) in the control group. There was significant difference between the two groups ( χ2=7.414, P<0.01). After treatment, the scores of epigastric pain, fullness, liking temperature and pressing, vomiting clear water, eating less and staying foolish, and limb burnout in the observation group were significantly lower than those in the control group ( t values were 2.788, 3.632, 3.816, 1.590, 2.183, 2.103, respectively, all Ps<0.05), and the scores of chronic inflammatory reaction, inflammatory activity, atrophy degree, dysplasia and intestinal metaplasia in the mucosa were significantly lower than those in the control group ( t values were 2.983, 2.106, 2.106, 3.773, 1.922, 3.095, respectively, all Ps<0.05). After treatment, the serum G-17 [(14.47 ± 3.06) pmol/L vs. (10.67 ± 2.47) pmol/L, t=10.510] and PG Ⅰ [(130.31 ± 14.79) μg/L vs. (102.36 ± 12.63) μg/L, t=8.178] and PG Ⅰ/Ⅱ [(10.45 ± 0.48) vs. (9.17 ± 0.72), t=2.104] in the observation group were significantly higher than those in the control group ( P<0.01 or P<0.05). Conclusion:Wanfu-Qutong Decoction combined with esomeprazole tablets can effectively improve the clinical symptoms of CAG patients, regulate the levels of G-17, PG Ⅰ , PG Ⅱ and PGⅠ/Ⅱ, and promote the repair of gastric mucosa.
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ABSTRACT BACKGROUND: Psoriasis is an inflammatory skin disease that affects 1%-3% of Caucasian populations and may be persistent, disfiguring and stigmatising. Proton pump inhibitors (PPI) are potent blockers of gastric acid secretion. They are widely regarded as the agents of choice for the treatment of acid-peptic disorders. In addition to anti-secretory effects PPI have been found to have anti-oxidant properties and direct effects on neutrophils, monocytes, endothelial, and epithelial cells that might prevent inflammation. OBJECTIVE: This study evaluated the treatment of psoriasis with esomeprazole. METHODS: Ten patients were selected and psoriasis was evaluated according to Psoriasis Area and Severity Index (PASI). Exclusion criteria included concomitant use of any treatment for Psoriasis, organic diseases, use of other PPI than esomeprazole. Patients were medicated with esomeprazole 40 mg B.I.D. for 90 days. At the 90th day the patients were evaluated according PASI score. RESULTS: Statistically significant results were seen when compared PASI before and at 90th day of treatment (P=0.0002). CONCLUSION: The use of esomeprazole for psoriasis resulted in excellent clinical results with a significant reduction of PASI score.
RESUMO CONTEXTO: A psoríase é uma doença inflamatória da pele que afeta 1%-3% das populações caucasianas e pode ser persistente, desfigurante e estigmatizante. Inibidores da bomba de prótons (IBP) são potentes bloqueadores da secreção de ácido no estômago. Eles são considerados como os agentes de escolha para o tratamento de doenças ácido-pépticas. No entanto, além dos efeitos anti-secretores, IBP apresentam propriedades anti-oxidantes e efeitos diretos sobre os neutrófilos, monócitos, células epiteliais e endoteliais que podem impedir a inflamação. OBJETIVO: Avaliar o tratamento da psoríase com esomeprazol. MÉTODOS: Foram selecionados pacientes adultos (18 anos ou mais) com psoríase. Os critérios de exclusão foram o uso concomitante de qualquer tratamento para a psoríase, doenças orgânicas e uso de outro IBP. Foram selecionados 10 pacientes e a psoríase foi avaliada pelo índice de gravidade e área da psoríase (Psoriasis Area and Severity Index - PASI). Os pacientes foram medicados com esomeprazol 40 mg BID por 90 dias. No nonagésimo dia os pacientes foram novamente avaliados por meio do PASI. RESULTADOS: Dados estatisticamente significativos foram vistos quando comparado PASI antes do tratamento e no nonagésimo dia de tratamento, P=0,0002. CONCLUSÃO: O uso do esomeprazol para psoríase apresentou excelentes resultados clínicos com redução importante do PASI. Este estudo piloto é a primeira publicação na literatura inglesa sobre o tratamento da psoríase com esomeprazol.
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Humanos , Masculino , Feminino , Adulto , Idoso , Psoríase/tratamento farmacológico , Inibidores da Bomba de Prótons/uso terapêutico , Esomeprazol/uso terapêutico , Projetos Piloto , Pessoa de Meia-IdadeRESUMO
Resumen Introducción: el presente estudio tuvo como fin investigar la efectividad clínica de dos presentaciones de esomeprazol en pacientes con dispepsia de causa no estudiada. Métodos: se realizó un ensayo clínico piloto de dos presentaciones de esomeprazol de 40 mg recibidos diariamente por 28 días. Se eligieron pacientes con diagnóstico de dispepsia no estudiada que asistieron a consulta de gastroenterología en un hospital de referencia. Se evaluaron a los pacientes inicialmente con endoscopia y biopsia, el seguimiento a 2 y 4 semanas con escalas clínicas de síntomas y calidad de vida con cuestionarios validados en español (SODA y QoL-PEI) y eventos adversos. Además, se midieron los niveles de pH gástrico con pH-metrías en 24 horas al día 14 de tratamiento. Se tomaron niveles séricos del medicamento al momento de la evaluación de la pH-metría. Para las escalas clínicas se aplicó un análisis de varianza (ANOVA) de dos factores con medidas repetidas y al encontrar diferencias significativas en los tiempos se realizó una corrección de Bonferroni. Resultados: se aleatorizó un total de 33 pacientes, 16 y 17 pacientes en cada grupo. No hubo diferencias en el porcentaje de inhibición del pH gástrico al día 14 de tratamiento (p = 0,9795). No hubo diferencias en concentraciones de niveles séricos el día 14 (p = 0,2199). No se encontraron diferencias significativas en las escalas de gravedad y calidad de vida en las dos primeras semanas de tratamiento, pero sí en las últimas dos semanas, en las cuales el producto de prueba demostró mayor disminución del dolor (p = 0,0048) y superioridad en conformidad (p = 0,01) en la subescala SODA. No se presentaron eventos adversos serios y no hubo diferencias estadísticas entre la presentación eventos adversos no serios. Conclusiones: los productos de prueba y el de referencia mostraron efectos similares en variables clínicamente relevantes.
Abstract Introduction: This pilot studied the clinical effectiveness of two presentations of esomeprazole in patients with dyspepsia with undiagnosed causes. Methods: We conducted a pilot clinical trial of two 40 mg Esomeprazole presentations. Patients with dyspepsia of unknown cause at a gastroenterology clinic in a referral hospital were included. They received one or the other presentation daily for 28 days. Patients were initially evaluated with endoscopy and biopsy and received follow-up examinations at two and four weeks. Adverse events were recorded, and clinical symptom scales and quality of life questionnaires validated in Spanish (SODA and QoL-PEI) were used. In addition, gastric pH levels were measured continuously for 24 hours on day 14 of treatment. Serum levels of the medication administered were also measured on day 14 of treatment. A two-way repeated measures ANOVA was used to compare mean differences between the two groups. When significant differences in times were found, a Bonferroni correction was made. Results: A total of 33 patients were randomized into two groups: 16 patients in one group and 17 in the other. There were no differences in the percentages of gastric pH inhibition at day 14 of treatment (p = 0.9795). There were no differences in serum level concentrations on day 14 (p = 0.2199). No significant differences were found in severity and quality of life scales in the first two weeks of treatment. However, in the last two weeks of treatment the test product showed a larger decrease in pain (p = 0.0048) and superiority in compliance (p = 0.01) on the SODA subscale. There were no serious adverse events, and there were no statistical differences between the presentations of non-serious adverse events. Conclusions: The Test product and the Reference product showed similar effects on clinically relevant variables.
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Humanos , Masculino , Feminino , Esomeprazol , Pilotos , Pacientes , Terapêutica , Preparações Farmacêuticas , Similar , DispepsiaRESUMO
Background: Proton pump inhibitors (PPIs) largely used a drug to treat gastroesophageal disease such as gastric ulcers. Moreover, in recent years, several studies suggest that PPIs have an important anti-cancer effect in monotherapy and or combination with chemotherapy. The aim of this study was to investigate whether esomeprazole and pantoprazole exhibit anti-cancer effect alone or could enhance chemosensitivity on the human neuroblastoma cell line SH-SY5Y to cisplatin.Methods: The human neuroblastoma SH-SY5Y cells were cultured and treated with different concentrations of esomeprazole, pantoprazole, and cisplatin alone. Also, these cells exposed to cisplatin+ esomeprazole and cisplatin + pantoprazole combinations, respectively and incubated 24 h. The antiproliferative activities of the (PPIs) alone or in a combination of cisplatin was evaluated using the XTT colorimetric assay.Results: According to experimental data, neither PPIs showed no cytotoxicity on the human neuroblastoma cell line SH-SY5Y at all concentrations. However, when combined with cisplatin separately, they were found to have significant antiproliferative effects on the human neuroblastoma SH-SY5Y cell lines when compared to cell lines treated with cisplatin alone (p<0.05).Conclusions: Taken together, the inhibition of V-ATPase via esomeprazole and pantoprazole might enhance the chemosensitivity of cisplatin on the human neuroblastoma cell line SH-SY5Y. However, further studies are needed to be able to utilize PPIs in human neuroblastoma cells.
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OBJECTIVE： To establish a method for simultaneous determination of impurity E， impurity Ⅰ and impurity Ⅳ in crude drug and preparation of esomeprazole sodium. METHODS： LC-MS/MS method was adopted. The separation was performed on Agela VenusiL MP C18 column with mobile phase consisted of acetonitrile-water （gradient elution） at the flow rate of 0.2 mL/min. The column temperature was 35 ℃， and the sample size was 1 μL； analytes were analyzed by electro-spray ionization （ESI） in the multiple reaction monitoring mode， negative ion. The precursors of production transitions m/z 360.1→194.0 （impurity E）， m/z 375.8→210.7 （impurity Ⅰ）， m/z 330.2→312.1 （impurity Ⅳ） were used to measure impurity. RESULTS： The linear range of impurity E， impurity Ⅰ and impurity Ⅳ were 0.001 26-0.044 80 μg/mL （r＝0.994 7）， 0.001 34-0.045 2 μg/mL （r＝0.992 8） and 0.018 9-1.260 00 μg/mL （r＝0.991 4）. The limit of quantitation were 0.001 26， 0.001 34， 0.018 9 μg/mL； the detection limits were 0.000 41， 0.000 44， 0.006 3 μg/mL. RSDs of precision and reproducibility tests were all lower than 4％； RSDs of stability tests of impurity E and impurity Ⅰ were all lower than 10％（n＝5）， and that of impurity Ⅳ was higher than 15％ （n＝7）. The average recoveries were 87.69％-100.72％ （RSD＝4.29％， n＝9）， 90.04％-100.63％（RSD＝3.67％，n＝9）and 93.58％-101.86％（RSD＝2.66％，n＝9）. CONCLUSIONS： The method is accurate， rapid， sensitive， selective and suitable for the content determination of 3 impurities in crude drug and preparation of esomeprazole sodium.
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Background: Detailed histopathological and histomorphometric analysis of gastric mucosa after long term treatment or ingestion of esomeprazole specifically is lacking in literature. Methods: 24 male and female rats, 12 each were divided into control and experimental groups (6 each for both sexes). Rats of experimental group got 15 mg/kg body weight of esomeprazole by oral intubation for 130 days. After perfusion fixation by Karnovsky’s solution, two pieces of gastric wall were procured from anterior aspect, 1 each from distal part of body and pyloric region respectively. Sections of 8 μm thickness, obtained by using wax embedding technique, were stained with haematoxylin and eosin. Results: In both the regions of stomach in two sexes of control rats, the mucosa showed 1/5th superficial layer of absorptive epithelial cells,3/5th parietal and deepest 1/5th layer of pepsin secreting glands. Parietal and pepsin gland layers were involved in body of male and pyloric region of female. Marked oedema, hypertrophy and hyperplasia were uniformly observed in experimental animals. Conclusion: Atrophic gastritis observed in female pyloric region is an alarming observation because it is the precursor of gastric carcinoma.
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Objective To evaluate the effect and safety of Qizhi Weitong Granule plus Wubei Powder in treatment of army men with helicobacter pylori negative duodenal ulcer disease.Methods A randomized,single-blind,controlled study was conducted in 84 army men with helicobacter pylori negative duodenal ulcer disease.They were randomly divided into trial group (n =40,Qizhi Weitong Granule plus Wubei Powder were administered daily for 4 weeks) and control group(n =44,they took imported esomeprazole daily for 4 weeks).Symptoms and adverse reactions were recorded.Gastroscopy was performed by the end of the fourth week.Results After treatment,the cure rate and total effective healing rate of ulcer were 87.5％ and 95.0％ in trial group,and those in control group were 86.4％ and 97.7 ％ respectively.The difference was not statistically significant(Z =0.074.P ＞ 0.05).The relief rates of symptoms were 95.0％ in trial group and 88.6％ in control group,the difference was not of statistical significance (Z =0.793,P ＞ 0.05).There was no statistically significant difference in the relief of gastric abscess,flatulence,belching and acid regurgitation between the two groups (P ＞ 0.05).But the symptoms of irritability and bad temper,chest distress and deep sighing,bitter taste in the mouth and poor appetite in trial group were improved more significantly than those in control group.The difference was statistically significant(P ＜ 0.05).The incidences of adverse reaction were 15％ in trial group and 13.6％ in control group,the difference was not statistically significant (x2 =0.01,P ＞ 0.05).Conclusion Qizhi Weitong Granule plus Wubei Powder is as effective,safe and well tolerated as imported esomeprazole in army men with helicobacter pylori negative duodenal ulcer disease.But Qizhi Weitong Granule plus Wubei Power can improve mental symptoms and appetite of patients with duodenal ulcer disease significantly.
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Los inhibidores de bomba de protones son usados en el tratamiento de la gastropatía ácido-péptica. Objetivo: comparar la eficacia de dos marcas de esomeprazol en el tratamiento de gastropatía ácido-péptica, la evolución de síntomas y su tolerancia. Materiales y Métodos: Se incluyeron pacientes de ambos sexos, con edades entre 18-60 años, con o sin Helicobacter pylori, que en la gastroscopia presentaron una o más erosiones o úlceras ≥ 5 mm y < 25 mm en su diámetro mayor. Se distribuyeron aleatoriamente a recibir una de las marcas, 40 mg/día, oral, durante 4 semanas. Al final fueron evaluados con endoscopia, interrogatorio de efectos adversos y laboratorio, comparando tasa de curación y evolución de la endoscopia. Se evaluó la tasa de respondedores por disminución del score de síntomas y la tolerancia mediante interrogatorio de efectos adversos y pruebas de laboratorio. Resultados: Ingresaron 34 pacientes, analizando los resultados de 30. En ambos grupos observamos mejoría en la endoscopia (curación y/o mejoría). El score de síntomas mejoró en ambos grupos, con significancia intragrupo pero no intergrupal. Los efectos adversos no fueron significativos. Conclusiones: Observamos mejoría en los criterios de endoscopia, y en el score de síntomas, en ambos grupos.
Introduction: Proton pump inhibitors are used in the treatment of acid-peptic gastropathy. Objective: to compare the efficacy of two brands of esomeprazole in the treatment of acid-peptic gastropathy, the evolution of symptoms and their tolerance. Materials and methods: Patients of both sexes, aged 18-60 years, with or without Helicobacter pylori, who had one or more erosions or ulcers ≥ 5 mm and <25 mm in their largest diameter, in gastroscopy, were included. They were randomized to receive one of the brands, 40 mg / day, orally, for 4 weeks. At the end, they were evaluated with endoscopy, adverse event questioning and laboratory tests, comparing cure rate and evolution of endoscopy. We evaluated the rate of responders according to decreased symptom score, and tolerance through questioning of adverse effects and laboratory tests. Results: Thirty-four patients were enrolled, analyzing the results of 30 patients. In both groups we observed improvement in endoscopy (healing and / or improvement). The score of symptoms improved in both groups, with intragroup but not intergroup significance. Adverse events were not significant. Conclusions: Thirty-four patients were enrolled, analyzing the results of 30 patients. In both groups we observed improvement in endoscopy (healing and / or improvement). The score of symptoms improved in both groups, with intragroup but not intergroup significance. Adverse events were not significant.
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PURPOSE: This study was conducted to investigate whether a proton pump inhibitor (PPI) could enhance chemosensitivity via the inhibition of vacuolar-type H⁺ ATPase (V-ATPase) in cervical cancer. MATERIALS AND METHODS: The expression of V-ATPase was evaluated in 351 formalin-fixed, paraffin-embedded human cervical cancer tissues using immunohistochemistry and compared with clinicopathologic risk factors for disease prognosis. The influence of cell proliferation and apoptosis following V-ATPase siRNA transfection or esomeprazole pretreatment was assessed in cervical cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and enzyme-linked immunosorbent assay, respectively. RESULTS: Immunohistochemical analysis revealed that V-ATPase was expressed in about 60% of cervical cancer tissue samples (211/351), and the expression was predominantly found in adenocarcinoma histology (p=0.016). Among patients with initially bulky cervical cancer (n=89), those with V-ATPase expression had shorter disease-free survival (p=0.005) and overall survival (p=0.023). Co-treatment with V-ATPase siRNA or esomeprazole with paclitaxel significantly decreased the cell proliferation of cervical cancer cell lines, including HeLa and INT407, compared to cell lines treated with paclitaxel alone (p < 0.01). Moreover, V-ATPase siRNA or esomeprazole followed by paclitaxel significantly increased the expression of active caspase-3 in these cells compared to cells treated with paclitaxel alone (both, p < 0.05). CONCLUSION: V-ATPase was predominantly expressed in cervical adenocarcinoma, and the expression of V-ATPases was associated with poor prognosis. The inhibition of V-ATPase via siRNA or PPI (esomeprazole) might enhance the chemosensitivity of paclitaxel in cervical cancer cells.
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Humanos , Adenocarcinoma , Adenosina Trifosfatases , Antineoplásicos , Apoptose , Caspase 3 , Linhagem Celular , Proliferação de Células , Intervalo Livre de Doença , Ensaio de Imunoadsorção Enzimática , Esomeprazol , Imuno-Histoquímica , Paclitaxel , Prognóstico , Inibidores da Bomba de Prótons , Bombas de Próton , Prótons , Fatores de Risco , RNA Interferente Pequeno , Transfecção , Neoplasias do Colo do Útero , ATPases Vacuolares Próton-TranslocadorasRESUMO
Objective To observe and investigate the effect of esomeprazol in the elderly patients with gastric ulcers and influence for the pepsinogen,cAMP and cGMP.Methods 86 elderly patients with gastric ulcers in our hospital from June 2015 to August 2016 were selected as the research object,and they were randomly divided into control group 43 cases and observation group 43 cases, the control group were treated with omeprazole,the observation group were treated with esomeprazol,the total effective rates,symptom score and pepsinogen, cAMP, cGMP levels before and after the treatment of two groups were compared.Results The total effective rates of observation group at different time after the treatment were higher than those of control group,the symptom scores after the treatment were all lower than those of control group ,the serum pepsinogen were all lower than those of control group,the plasma cAMP and cAMP /cGMP were lower than those of control group,the plasma cGMP were higher than those of control group, (P<0.05), the differences were all significant.Conclusion The clinical effect of esomeprazol in the elderly patients with gastric ulcers is better,and it can significantly improve the expression situation of pepsinogen, cAMP and cGMP of patients, so its application value in the elderly patients with gastric ulcers is higher.
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Objective To investigate clinical effect of esomeprazole, mosapride, magnesium plus aluminum in patients with reflux esophagitis. Methods 98 patients with reflux esophagitis who were treated in our hospital from October 2014 to October 2016 were selected and randomly divided into control group and observation group, with 49 cases in each group.In the control group, patients were treated with esomeprazole and mosapride.In the observation group, patients were given esomeprazole, mosapride and magnesium plus aluminum.The levels of serum gastrin, serum motilin and 24-hour pH in the esophagus were compared before and after treatment .Results After treatment,The levels of serum gastrin and serum motilin in the observation group were significantly higher than those in the control group, the difference was statistically significant (P<0.05), while the total time percentage of pH<4 at standing position, total time percentage of pH <4 at supine position, total reflux time percentage of pH <4, and the duration of continuous reflux≥five mins in the observation group were significantly lower than those in the control group, the difference was statistically significant (P<0.05). Conclusion Esomeprazole, mosapride and magnesium plus aluminum have significant clinical effect in patients with reflux esophagitis, and can effectively reduce 24-hour pH in the esophagus, decrease the number of reflux, increase serum gastrin and serum motilin levels.
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Objective:To establish a method for the content determination of magnesium in esomeprazole magnesium. Methods:The content of magnesium in esomeprazole magnesium was determined by inductive coupled plasma atomic emission spectrometry. Re-sults:The linear range was 10.0-80.0 μg·ml-1(r=0.999 8). The average recovery was 99.55% with RSD of 1.35% (n=9). The detection limit was 0. 000 75 μg·ml-1 and the quantitative limit was 0. 002 5 μg·ml-1 . Conclusion:The method is accurate, sensitive and reproducible, which can be used for the content determination of magnesium in esomeprazole magnesium.
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Objective To explore the mucosal healing quality of hydrotalcite combined with esomeprazole in gastric ulcer.Methods Forty-two patients visiting from June 2014 to December 2015 and diagnosed with gastric ulcer were selected and divided into combination therapy group and single therapy group with 21 patients in each group.The patients of combination therapy group received esomeprazole combined with hydrotalcite,and the patients of single therapy group received esomeprazole alone.The total therapeutic course was eight weeks.At the same period,21 health check-up participants were enrolled as normal control group.The healing of gastric ulcer was observed under white light endoscopy.The morphological changes of gastric pits and microvessel of mucosal at peripheral mucosa around ulcer and normal gastric mucosal were observed under narrow band imaging magnifying endoscopy.The gastric mucosa tissues of the two groups before and after treatment,and normal gastric mucosa of healthy control group were taken.The amount of deposition and composition of collagen fibers,the expression level of factor Ⅷ,the level of transforming growth factor (TGF)-beta1 and the content of hydroxyproline were analyzed by Masson,immunofluorescent and immunohistochemistry staining as well as enzyme linked immunosorbent assay.Chi square test,one-way analysis of variance (ANOVA),least significant difference (LSD) method,Dunnett's T3 and Kruskal-Wallis test and other method were used for comparison.Results After treatment,18 patients of combination therapy group (21 patients) had regular microvessel nets (85.7％),which was significantly more than those of single therapy group (12 cases,57.1％) and healthy control group (10 cases,47.6 ％),and the differences were statistically significant (x2 =4.200,P=0.040).In the comparison of maturity of regenerative mucosa between combination therapy group and single therapy group after treatment,the ration between collagen type Ⅰ and Ⅱ,deposition of collagen fibers,the number of factor Ⅷ positive cells,the level of TGF-beta1 and the content of hydroxyproline were 36.05 and 23.14;269 375.63.± 171 608.63 and 137 693.14±98 330.93;34.91±8.40 and 28.24±6.93;104 498.71±40 487.96 and 70 757.11±19 323.95;(1 897.80±879.35) and (1 230.57±536.05) μg/L,respectively;while in healthy control group,the above parameters were 36.81,245 696.90 ± 224 687.00,23.10 ± 8.40,94 048.04 ±41 306.55 and 1 681.20 ± 423.61 μg/L,and the differences were statitically significant among these three groups (H=7.375,F=3.465,11.680,5.190,5.160;all P＜0.05).Those parameters of combination therapy group were significantly higher than those of single therapy group (H=2.416,LSD method;all P＜0.05).Conclusion Hydrotalcite combined with esomeprazole in the treatment of gastric ulcer could significantly improve microvessel morphology,maturity degree of regenerative mucosal structure and function,and the mucosal healing quality was also superior to single esomeprazole group.
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Objective To compare the efficacy of esomeprazole and omeprazole in the treatment of gastric ulcer, and to provide a reference for the clinical treatment of gastric ulcer.Methods80 cases of gastric ulcer patients in our hospital from February to April 2014 were randomly divided into observation group and control group, with 40 cases in each group.The patients in the control group were treated with omeprazole,the patients in the observation group were treated with Esomeprazole, patients received three courses of treatment,the changes of body after treatment in two groups were observed, the degree of stomach pain and the changes of the condition were analyzed, the healing degree of gastric ulcer was observed, the clinical therapeutic effect of two groups was analyzed.ResultsAfter treatment, the recovery rate of the observation group was 100%, significantly higher than the control group 90%, the difference was statistically significant (P<0.05).The scores of pain in the observation group and the drug use score were significantly lower than those in the control group (P<0.05).The adverse reaction rate of the observation group was significantly lower than that of the control group, the difference was statistically significant (P<0.05).ConclusionThe efficiency of Esomeprazole in the treatment of gastric ulcer is better than omeprazole, patients with high satisfaction, can effectively shorten the wound healing time, reduce patient treatment time, reduce medical costs, and adverse reactions light.