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Sample records for omeprazole

  1. Therapeutic evaluation of omeprazole.

    Science.gov (United States)

    Adams, M H; Ostrosky, J D; Kirkwood, C F

    1988-10-01

    The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of omeprazole are reviewed. Omeprazole, a substituted benzimidazole, has a unique site and mechanism of action because it inhibits the proton pump--i.e., hydrogen, potassium adenosine triphosphatase (H+,K+-ATPase)--and consequently blocks the final common step in the gastric acid secretory pathway. Omeprazole inhibits basal and histamine-, gastrin- and pentagastrin-stimulated gastric hydrochloric acid secretion. It produces a dose-dependent reduction in gastric acidity, gastric acid output, and gastric juice volume and has variable effects on pepsin secretion. Omeprazole has no documented effect on esophageal motility or lower esophageal sphincter pressure. Omeprazole is variably absorbed from the gastrointestinal tract, and food appears to decrease the rate, but not the extent, of drug absorption. The drug is approximately 95% bound to plasma proteins and is metabolized to inactive components that are enterohepatically or renally eliminated. Omeprazole is more effective (in most studies) than H2-receptor antagonists in treating duodenal ulcer, at least as effective in treating benign gastric ulcer, and more effective in treating reflux esophagitis. Omeprazole has been used successfully in patients with Zollinger-Ellison syndrome refractory to treatment with H2-receptor antagonists. Gastrointestinal complaints (nausea and diarrhea) are the most commonly reported adverse effects associated with omeprazole therapy. The most frequently reported laboratory abnormality occurring with omeprazole use is elevation of serum aspartate aminotransferase and alanine aminotransferase concentrations. Omeprazole will serve a valuable role in the management of gastrointestinal tract ulcers and hypersecretory conditions.

  2. Compound list: omeprazole [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available omeprazole OPZ 00012 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in_vitro/omeprazole....Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitro/omeprazole....Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Single/omeprazole...ive/open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/omeprazole.Rat.in_vivo.Liver.Repeat.zip ftp://ftp.bioscienc...edbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Kidney/Single/omeprazole.Rat.in_vivo.Kidney.Single.zip ftp:/

  3. Reversible renal failure after treatment with omeprazole.

    Science.gov (United States)

    Post, A T; Voorhorst, G; Zanen, A L

    2000-08-01

    Omeprazole is a proton pump inhibitor widely used in the treatment of gastro-esophageal reflux disease and peptic ulcer disease. In a 73-year-old man we describe renal failure due to acute interstitial nephritis after use of omeprazol during 4 months. Unexpected renal failure without signs of hydronephrosis should always provoke awareness of drug reaction, omeprazole being one of the possible drugs.

  4. Pharmacokinetics of intrarectal omeprazole in alpacas.

    Science.gov (United States)

    Marmulak, T; Stanley, S; Kass, P H; Wiebe, V; McKemie, D; Pusterla, N

    2010-08-01

    The purpose of this study was to evaluate the pharmacokinetics of omeprazole in three different vehicles when administered rectally to six alpacas. Alpacas were given single doses of omeprazole (4 mg/kg) in a double-blinded, randomized cross-over design with a 1 week washout period. Omeprazole formulations consisted of (1) Treatment A: omeprazole paste mixed in surgical lubricant (2) Treatment B: omeprazole capsule contents in 8.4% sodium bicarbonate and (3) Treatment C: omeprazole capsule contents in surgical lubricant and 8.4% sodium bicarbonate solution. Plasma samples were drawn at 0, 5, 10, 15, 30, 45, 60, 90, 120, 180, 300 and 480 min. Omeprazole plasma concentrations were determined by high-pressure liquid chromatography-mass spectrometry. Pharmacokinetic results demonstrated median peak plasma concentrations (C(max)) of 7.35 (3.2-15.2), 7.30 (1.7-10.9) and 8.65 (1.8-19.3) ng/mL and median area under the concentration curve (AUC((0-180))) of 747 (237-1681) min x ng/mL, 552.9 (39-1063) min x ng/mL, and 972 (107-1841) min x ng/mL for treatments A, B and C, respectively. The median half-lives were similar between groups: 38, 50, and 53 min. As a result of the low measured omeprazole plasma concentrations, it is assumed that rectal absorption of omeprazole is poor in alpacas and not an effective route of administration.

  5. Omeprazole

    Science.gov (United States)

    ... sores in the lining of the stomach or intestine) and it is also used with other medications ... voriconazole (Vfend) and other prescription antifungal or anti-yeast medications. Your doctor may need to change the ...

  6. Zegerid--immediate-release omeprazole.

    Science.gov (United States)

    2005-04-11

    The FDA has approved marketing of Zegerid powder for oral suspension (Santarus), an immediate-release formulation of the proton-pump inhibitor (PPI) omeprazole (Prilosec, and others). All other oral PPIs are delayed-release, enteric-coated formulations designed to prevent degradation of the drug by gastric acid. Each 20- or 40-mg packet of Zegerid contains 1680 mg sodium bicarbonate, which protects the drug from gastric acid degradation. A dose of Zegerid contains 460 mg of sodium, which may be excessive for some patients. Zegerid is the first oral PPI to be approved by the FDA for reduction of risk of upper GI bleeding in critically ill patients. The drug may be useful for patients who are unable to swallow and have nasogastric (NG) tubes in place. Zegerid cost $70.00 for 14 days' treatment, compared to less than $10 for 14 tablets of Prilosec OTC.

  7. Omeprazole inhibits proliferation and modulates autophagy in pancreatic cancer cells.

    Directory of Open Access Journals (Sweden)

    Andrej Udelnow

    Full Text Available BACKGROUND: Omeprazole has recently been described as a modulator of tumour chemoresistance, although its underlying molecular mechanisms remain controversial. Since pancreatic tumours are highly chemoresistant, a logical step would be to investigate the pharmacodynamic, morphological and biochemical effects of omeprazole on pancreatic cancer cell lines. METHODOLOGY/PRINCIPAL FINDINGS: Dose-effect curves of omeprazole, pantoprazole, gemcitabine, 5-fluorouracil and the combinations of omeprazole and 5-fluorouracil or gemcitabine were generated for the pancreatic cancer cell lines MiaPaCa-2, ASPC-1, Colo357, PancTu-1, Panc1 and Panc89. They revealed that omeprazole inhibited proliferation at probably non-toxic concentrations and reversed the hormesis phenomena of 5-fluorouracil. Electron microscopy showed that omeprazole led to accumulation of phagophores and early autophagosomes in ASPC-1 and MiaPaCa-2 cells. Signal changes indicating inhibited proliferation and programmed cell death were found by proton NMR spectroscopy of both cell lines when treated with omeprazole which was identified intracellularly. Omeprazole modulates the lysosomal transport pathway as shown by Western blot analysis of the expression of LAMP-1, Cathepsin-D and β-COP in lysosome- and Golgi complex containing cell fractions. Acridine orange staining revealed that the pump function of the vATPase was not specifically inhibited by omeprazole. Gene expression of the autophagy-related LC3 gene as well as of Bad, Mdr-1, Atg12 and the vATPase was analysed after treatment of cells with 5-fluorouracil and omeprazole and confirmed the above mentioned results. CONCLUSIONS: We hypothesise that omeprazole interacts with the regulatory functions of the vATPase without inhibiting its pump function. A modulation of the lysosomal transport pathway and autophagy is caused in pancreatic cancer cells leading to programmed cell death. This may circumvent common resistance mechanisms of

  8. Omeprazole/Antacid-powder suspension-Santarus: omeprazole/sodium bicarbonate powder-Santarus, SAN 05.

    Science.gov (United States)

    2004-01-01

    Santarus Inc. is developing an immediate-release formulation of omeprazole in combination with an antacid (sodium bicarbonate) as a powder for suspension, known as Acitreltrade mark [SAN 05] and also as Rapinex powder for oral suspension. This omeprazole powder suspension will be used to treat gastrointestinal haemorrhage, gastro-oesophageal reflux disease, heartburn and peptic ulcers. Acitreltrade mark is based on technology licensed from the University of Missouri. Santarus have also licensed technology from Tulane and North Carolina Universities relating to potential treatments for gastrointestinal (GI) diseases. Santarus has licensed exclusive, worldwide rights to patent applications covering specific combination formulations of proton pump inhibitors (PPIs) and antacids for treating various upper GI diseases and disorders. Santarus plans to license the development, distribution and marketing rights of omeprazole powder for oral suspension 20 mg outside the US, to one or more well established pharmaceutical companies. The US FDA has requested that Santarus pursue a name other than Rapinex for the product. Santarus is currently discussing potential alternative names for the product with the FDA. Santarus announced positive results in August 2003 from a phase III trial comparing oral Acitrel (Rapinex 40 mg) with intravenous cimetidine in preventing upper GI bleeding in 359 critically ill adult patients. Santarus has also completed an open-label clinical trial in 243 patients, including 97 patients with gastric ulcers, evaluating the safety of this omeprazole 40 mg powder suspension for an 8-week period. In connection with the NDA for omeprazole powder suspension 40 mg, Santarus provided notice to the NDA holder for Prilosec delayed-release capsules and related patent owners that omeprazole powder suspension 40 mg does not infringe currently listed patents for Prilosec or that those patents are invalid.

  9. Omeprazole promotes proximal duodenal mucosal bicarbonate secretion in humans

    DEFF Research Database (Denmark)

    Mertz-Nielsen, A; Hillingsø, Jens; Bukhave, K

    1996-01-01

    with high dose omeprazole (n = 17) and ranitidine (n = 9), respectively, by use of a technique permitting simultaneous measurements. Concentrations of bicarbonate were measured in the respective effluents by the method of back titration. Both omeprazole and ranitidine completely inhibited gastric acid...

  10. Omeprazole promotes proximal duodenal mucosal bicarbonate secretion in humans

    DEFF Research Database (Denmark)

    Mertz-Nielsen, Anette; Hillingsø, J; Bukhave, Klaus

    1996-01-01

    dose omeprazole (n=17) and ranitidine (n=9), respectively, by use of a technique permitting simultaneous measurements. Concentrations of bicarbonate were measured in the respective effluents by the method of back titration. Both omeprazole and ranitidine completely inhibited gastric acid secretion (p...

  11. [OMEPRAZOL VS RANITIDINE IN UPPER DIGESTIVE BLEEDING

    Science.gov (United States)

    Regis R, Regina; Bisso A, Aland; Rebaza, Segundo

    1999-01-01

    Pectic ulcer is the most frequent cause of gastrointestinal bleeding. The homeostatic mechanism of bleeding, and coagulation, does not happen with values of pH less than 5,0. Therefore neutralization of gastric acidity (pH more than 5,0) is a recourse of control, improve the evolution and healing of peptic ulcer and to avoid a new bleeding. The aim of this study was to compare the results of treatment with omeprazole and ranitidine, in 57 patients admitted at emergency room of the Hospital Central de la Polic a Nacional del Per with endoscopic diagnosis of peptic ulcer, using Forrest classification. Patients received omeprazole 40 mg in bolus IV, followed by continuos infusion of 8 mg/hour for 72 hours (group A) or ranitidine 50 mg IV each 8 hours for 72 hours (group B). A new endoscopy was made 72 hours after admission demostrated a succesful therapy in both group. Bleeding stopped in 26/27 patients in group A (96,2%) and in 23/30 patients in group B (76,6%) (pomeprazole IV is more effective than ranitidine IV in the control of UGB because of peptic ulcer and provides a faster healing.

  12. Omeprazole promotes proximal duodenal mucosal bicarbonate secretion in humans.

    Science.gov (United States)

    Mertz-Nielsen, A; Hillingsø, J; Bukhave, K; Rask-Madsen, J

    1996-01-01

    The proton pump inhibitor, omeprazole, surprisingly resulted in higher rates of proximal duodenal mucosal bicarbonate secretion than previously reported using an H2 receptor antagonist for gastric acid inhibition. Gastroduodenal perfusions were performed in healthy volunteers to evaluate whether this incidental finding is explained by more potent gastric acid inhibition by omeprazole or might be caused by the different mode of drug action. Basal and stimulated gastric and duodenal bicarbonate secretion rates were measured in the same subjects in control experiments (n = 17) and after pretreatment with high dose omeprazole (n = 17) and ranitidine (n = 9), respectively, by use of a technique permitting simultaneous measurements. Concentrations of bicarbonate were measured in the respective effluents by the method of back titration. Both omeprazole and ranitidine completely inhibited gastric acid secretion (pH 6.9 v 6.8; p > 0.05). Omeprazole caused higher rates of basal (mean (SEM)) (597 (48) v 351 (39) mumol/h; p 0.05) duodenal bicarbonate secretion compared with control experiments. Also the combination of omeprazole and ranitidine increased (p = 0.05) duodenal bicarbonate secretion, while ranitidine alone caused no change in either basal or stimulated secretion. In the stomach basal as well as vagally stimulated bicarbonate secretion was independent of the means of acid inhibition. These results show that the proton pump inhibitor, omeprazole, promotes proximal duodenal mucosal bicarbonate secretion apparently independent of its gastric acid inhibitory effect. The mechanism of action remains speculative.

  13. Omeprazole for Refractory Gastroesophageal Reflux Disease during Pregnancy and Lactation

    Directory of Open Access Journals (Sweden)

    John K Marshall

    1998-01-01

    Full Text Available Symptomatic gastroesophageal reflux is a common complication of pregnancy and lactation. However, the safety of many effective medical therapies, including oral proton pump inhibitors, has not been well defined. The administration of oral omeprazole to a 41-year-old female during the third trimester of pregnancy, after ranitidine and cisapride failed to control her refractory gastroesophageal reflux, is reported. No adverse fetal effects were apparent, and the patient elected to continue omeprazole therapy (20 mg/day while breastfeeding. Peak omeprazole concentrations in breast milk (58 nM, 3 h after ingestion were less than 7% of the peak serum concentration (950 nM at 4 h, indicating minimal secretion. Although omeprazole is a potentially useful therapy for refractory gastroesophageal reflux during pregnancy and lactation, further data are needed to define better its safety and efficacy.

  14. Omeprazole promotes proximal duodenal mucosal bicarbonate secretion in humans.

    OpenAIRE

    Mertz-Nielsen, A; Hillingsø, J; Bukhave, K; Rask-Madsen, J

    1996-01-01

    The proton pump inhibitor, omeprazole, surprisingly resulted in higher rates of proximal duodenal mucosal bicarbonate secretion than previously reported using an H2 receptor antagonist for gastric acid inhibition. Gastroduodenal perfusions were performed in healthy volunteers to evaluate whether this incidental finding is explained by more potent gastric acid inhibition by omeprazole or might be caused by the different mode of drug action. Basal and stimulated gastric and duodenal bicarbonate...

  15. Omeprazole decreases magnesium transport across Caco-2 monolayers

    Institute of Scientific and Technical Information of China (English)

    Narongrit Thongon; Nateetip Krishnamra

    2011-01-01

    AIM: To elucidate the effect and underlying mechanisms of omeprazole action on Mg2+ transport across the intestinal epithelium. METHODS: Caco-2 monolayers were cultured in various dose omeprazole-containing media for 14 or 21 d before being inserted into a modified Ussing chamber apparatus to investigate the bi-directional Mg2+ transport and electrical parameters. Paracellular permeability of the monolayer was also observed by the dilution potential technique and a cation permeability study. An Arrhenius plot was performed to elucidate the activation energy of passive Mg2+ transport across the Caco-2 monolayers. RESULTS: Both apical to basolateral and basolateral to apical passive Mg2+ fluxes of omeprazole-treated epithelium were decreased in a dose- and time-dependent manner. Omeprazole also decreased the paracellular cation selectivity and changed the paracellular selective permeability profile of Caco-2 epithelium to Li+, Na+, K+, Rb+, and Cs+ from series Ⅶ to series Ⅵ of the Eisenman sequence. The Arrhenius plot revealed the higher activation energy for passive Mg2+ transport in omeprazoletreated epithelium than that of control epithelium, indicating that omeprazole affected the paracellular channel of Caco-2 epithelium in such a way that Mg2+ movement was impeded. CONCLUSION: Omeprazole decreased paracellular cation permeability and increased the activation energy for passive Mg2+ transport of Caco-2 monolayers that led to the suppression of passive Mg2+ absorption.

  16. Esomeprazole tablet vs omeprazole capsule in treating erosive esophagitis

    Institute of Scientific and Technical Information of China (English)

    Chih-Yen Chen; Ching-Liang Lu; Jiing-Chyuan Luo; Full-Young Chang; Shou-Dong Lee; Yung-Ling Lai

    2005-01-01

    AIM: Esomeprazole, an oral S-form of omeprazole, has been a greater acid inhibitor over omeprazole in treating acid-related diseases. Only less published data is available to confirm its efficacy for Asian people. Therefore, a perspective, double-blind, randomizedcomparison of esomeprazole tablets 40 mg (Nexium (R)) vs omeprazole capsules 20 mg (Losec(R)) in treating Chinese subjects with erosive/ulcerative reflux esophagitis (EE) was conducted.METHODS: A total of 48 EE patients were enrolled and randomized into two treatment groups under 8-wk therapy: 25 receiving esomeprazole, while another 23 receiving omeprazole treatment. Finally, 44 completed the whole 8-wk therapy. RESULTS: The difference in healing EE between two groups was 22.7% (72.7% vs 50.0%), not reaching significant value (P = 0.204). The median of the first time needed in relieving heartburn sensation was 1 d for both groups and the remission rates for heartburn on the 1st d after treatment were 77.3% and 65%,respectively (NS). The scores of various reflux relieving symptoms evaluated either by patients or by investigators were not different. Regarding drug safety, 28% of esomeprazole group and 26.1% of omeprazole groupreported at least one episode of adverse effects, while constipation and skin dryness were the common side effects in both groups (NS). CONCLUSION: Esomeprazole 40 mg is an effective and safe drug at least comparable to omeprazole in treating Chinese EE patients.

  17. Stability of omeprazole in an extemporaneously prepared oral liquid.

    Science.gov (United States)

    Quercia, R A; Fan, C; Liu, X; Chow, M S

    1997-08-15

    The stability of omeprazole 2 mg/mL. in an extemporaneously prepared oral liquid was studied. The contents of five 20-mg omeprazole capsules were mixed with 50 mL of 8.4% sodium bicarbonate solution in a Luer-Lok syringe. Three vials of this liquid were prepared for storage at 24, 5, and -20 degrees C. A 3-mL. sample of each was taken initially and on days 1, 2, 3, 4, 6, 8, 10, 12, 14, 18, 22, 26, and 30 and assayed by high-performance liquid chromatography. The liquids stored at 5 degrees C and at -20 degrees C did not change color during the study period, but the color of the liquid stored at 24 degrees C changed from white to brown. There were no significant changes in the omeprazole concentrations of the liquids stored at 5 and -20 degrees C during the study period, but the omeprazole concentration of the liquid stored at 24 degrees C was Omeprazole 2 mg/mL in an oral liquid compounded extemporaneously from capsules and sodium bicarbonate injection was stable for up to 14 days at 24 degrees C and for up to 30 days at 5 and -20 degrees C.

  18. Transport through liquid membranes containing omeprazole and lansoprazole.

    Science.gov (United States)

    Nagappa, A N; Pandi, P V; Mishra, P K; Girish, Rahul K; Shanmukh, I

    2002-12-01

    Omeprazole and lansoprazole, the therapeutically important drugs belonging to proton pump inhibitor category are extensively used in the treatment of gastric ulcers. Transport through liquid membranes generated by these drugs in lecithin-cholesterol mixture in series with a supporting membrane has been studied. The data obtained show the formation of liquid membrane in series with the supporting membrane. Transport of cations, chloride and bicarbonate ions in the presence liquid membranes generated by omeprazole and lanzoprazole indicate the modification in the permeability of various permeants.

  19. Desenvolvimento de minicomprimidos gastro-resistentes contendo Omeprazol

    OpenAIRE

    Tondo Filho, Volnei José

    2011-01-01

    Resumo: O presente trabalho teve como objetivo desenvolver e avaliar um sistema multiparticulado de liberação modificada, composto por minicomprimidos revestidos com polímero de liberação pH-dependente, tendo como fármaco modelo o omeprazol. O omeprazol é o fármaco mais utilizado no tratamento de desordens ácido-pépticas e quando administrado por via oral deve ser liberado rapidamente nas porções iniciais do intestino. Com esta finalidade tem se desenvolvido sistemas multiparticulados, na for...

  20. Pharmacokinetics of omeprazole and its metabolites in three phases of menstrual cycle.

    Science.gov (United States)

    Nazir, Shabnam; Iqbal, Zafar; Ahmad, Lateef; Shah, Yasar; Nasir, Fazli

    2015-03-01

    Omeprazole (OMP) is effective in the treatment of gastric hyperacidity and is metabolized by CYP2C19 and CYP3A4. These enzymes are modulated by estrogen and progesterone which regulate the menstrual cycle. The variations in the pharmacokinetics (PK) of many drugs like amphetamine, benzodiazepines and caffeine have been reported during menstrual cycle. In present study, the PK of the omeprazole and its metabolites was investigated during various phases of the menstrual cycle. A single oral dose, open-label, non-controlled, pharmacokinetic study of omeprazole was conducted in healthy young/premenopausal females (n = 16). The PK of omeprazole, 5-hydroxy-omeprazole and omeprazole sulphone was evaluated in three phases of menstrual cycle. The blood samples were analyzed using reversed-phase HPLC coupled with UV detector and the PK data were evaluated. The activities of CYP2C19 and CYP3A4 were determined as AUC(OH-OMP)/AUC(OMP) and AUC(OMP-SUL)/AUC(OMP), respectively. Omeprazole showed significantly (p menstrual phases, respectively. The [Formula: see text] of 5-hydroxy omeprazole was also significantly (p < 0.05) higher in follicular phase. The metabolic ratios (MR) of 5-hydroxy omeprazole and omeprazole sulphone were lower in follicular phase compared with the luteal phase. The present study suggests that high estrogen levels of follicular phase may result in increased absorption of omeprazole. The lower MR for 5-hydroxy omeprazole and omeprazole sulphone in follicular phase as compared to luteal phase suggests that metabolism of omeprazole is low in follicular phase as compared to luteal phase, which is progesterone-dominant phase. However, the clinical significance for these findings needs to be determined.

  1. Stability of omeprazole in SyrSpend SF Alka (reconstituted).

    Science.gov (United States)

    Whaley, Paul A; Voudrie, Mark A; Sorenson, Bridget

    2012-01-01

    Omeprazole is used in the treatment of dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger-Ellison syndrome. Omeprazole is marketed by AstraZeneca under a number of names, most notably Prilosec and Losec, as well as being available from a number of generic manufacturers. Omeprazole is available in both tablet and capsule form, with varying strengths of each. The need for other administration options for those patients who cannot take tablets or capsules has led compounding pharmacies to seek other alternatives. One possible alternative is the use of a suspending agent to create an oral solution or suspension. In the past, this has been accomplished using a sodium bicarbonate solution as the vehicle. However, sodium bicarbonate/omeprazole combination imparts a bitter and unpleasant taste. SyrSpend SF Alka (reconstituted) is a vehicle for making a suspension which has a pleasant taste, thus increasing palpability and compliance. The objective of this study was to determine the stability of omeprazole in SyrSpend SF Alka (for reconstitution). The studied sample was compounded into a 2-mg/mL suspension and stored in a low-actinic plastic prescription bottle at temperatures between 2 degrees C and 8 degrees C. Six samples were assayed at each time point out to 92 days by a stability-indicating high-performance liquid chromatography method. The method was validated for its specificity through forced degradation studies. The shelf life of this product is at least 92 days, based on data collected when refrigerated and protected from light.

  2. Effects of pirenzepine on omeprazole-induced hypergastrinemia and acid suppression in peptic ulcer patients.

    Science.gov (United States)

    Tari, A; Hamada, M; Kamiyasu, T; Fukino, Y; Sumii, M; Haruma, K; Sumii, K; Inoue, M; Kajiyama, G

    1996-04-01

    Omeprazole effectively suppresses acid secretion, resulting in the long-term elevation of intragastric pH and serum gastrin level. Pirenzepine has been reported to inhibit gastrin secretion. This study was carried out to examine the effects of additional pirenzepine treatment on the hypergastrinemia and gastric acid suppression induced by omeprazole. Concentrations of serum gastrin and plasma somatostatin were measured in 28 peptic ulcer patients before treatment, after omeprazole treatment (20 mg/day) for 2 weeks, and after omeprazole and pirenzepine (100 mg/day) treatment for 2 weeks. The acid inhibitory effect of pirenzepine treatment in addition to omeprazole was evaluated by 24-h intragastric pH measurement in six healthy volunteers. Serum gastrin level was increased significantly, to 2.4-fold the pretreatment level, by omeprazole treatment. Additional treatment with pirenzepine suppressed serum gastrin level to 0.6-fold the omeprazole-treatment level. The serum somatostatin level was not altered significantly either by omeprazole treatment or by omeprazole and pirenzepine treatment. In healthy volunteers whose pH 3 holding time on 24-h intragastric pH monitoring was 70% by omeprazole treatment, omeprazole and pirenzepine treatment markedly increased the pH 3 holding time, to 89%. These findings suggest that pirenzepine is useful in reducing the undesirable effects of omeprazole-induced hypergastrinemia, i.e., the excessive trophic effect of omeprazole on the acid-secreting part of the stomach and the overstimulation of acid secretion. The additional pirenzepine treatment is also effective in suppressing acid secretion.

  3. FORMULATION AND IN VITRO EVALUATION OF OMEPRAZOLE FAST DISSOLVING TABLETS

    Directory of Open Access Journals (Sweden)

    Soumya Missula

    2013-08-01

    Full Text Available Omeprazole is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD, Gastroesophageal reflux disease (GERD, laryngopharyngeal reflux disease (LPR and Zollinger-Ellison syndrome. The present study deals with the formulation of omeprazole fast dissolving tablets utilising cross linked alginic acid and calcium silicate as super disintegrates and a total of 8 formulation batches were prepared. All the pre compression and post compression parameters are studied and the results comply with in the limits. In vitro dissolution studies explained that the optimised F7 formulation with super disintegrants Cross linked alginic acid at low ratio and Calcium silicate at high ratio showed a cumulative release of 99.6 % of drug at the end of 12 minutes and also exhibited first order kinetics with Higuchi mechanism of drug release.

  4. Solid solution hardening of molecular crystals: tautomeric polymorphs of omeprazole.

    Science.gov (United States)

    Mishra, Manish Kumar; Ramamurty, Upadrasta; Desiraju, Gautam R

    2015-02-11

    In the context of processing of molecular solids, especially pharmaceuticals, hardness is an important property that often determines the manufacturing steps employed. Through nanoindentation studies on a series of omeprazole polymorphs, in which the proportions of the 5- and 6-methoxy tautomers vary systematically, we demonstrate that solid-solution strengthening can be effectively employed to engineer the hardness of organic solids. High hardness can be attained by increasing lattice resistance to shear sliding of molecular layers during plastic deformation.

  5. Effects of omeprazole and pirenzepine on enterochromaffin-like cells and parietal cells in rat stomach.

    Science.gov (United States)

    Tari, A; Kuruhara, Y; Yonei, Y; Yamauchi, R; Okahara, S; Sumii, K; Kajiyama, G

    2001-06-01

    The purpose of this study was to investigate the mechanism of the regulation of histamine synthesis in enterochromaffin-like cells, chemically and structurally, by treatment with omeprazole and pirenzepine. The ultrastructures of enterochromaffin-like cells and parietal cells were examined in rats treated with oral omeprazole (20 mg/kg) or intraperitoneal pirenzepine (1 mg/kg) administration. Serum gastrin concentrations, mRNA levels of H+-K+-ATPase and histidine decarboxylase, and the fundic concentrations of somatostatin and histamine were determined. Pirenzepine treatment suppressed omeprazole-induced increases in serum gastrin levels and mRNA levels of H+-K+-ATPase and histidine decarboxylase. Pirenzepine also decreased omeprazole-induced increases of histamine concentration in fundic mucosa. Pirenzepine elevated somatostatin mRNA level, previously decreased by omeprazole treatment, in fundic mucosa. In the cytoplasm of enterochromaffin-like cells, omeprazole markedly reduced the numbers of vesicles and granules, but significantly increased their diameters, whereas pirenzepine treatment changed neither of these features. The densities and diameters of both vesicles and granules produced by treatment with omeprazole and pirenzepine were between those produced by treatment with omeprazole alone and pirenzepine alone. Omeprazole-induced hypergastrinemia and pirenzepine-induced somatostatin synthesis play important roles not only in histamine synthesis but also in ultrastructural changes in enterochromaffin-like cells.

  6. Sensitive quantification of omeprazole and its metabolites in human plasma by liquid chromatography-mass spectrometry.

    Science.gov (United States)

    Hofmann, Ute; Schwab, Matthias; Treiber, Gerd; Klotz, Ulrich

    2006-02-02

    A sensitive method was developed for the simultaneous determination of omeprazole and its major metabolites 5-hydroxyomeprazole and omeprazole sulfone in human plasma by HPLC-electrospray mass spectrometry. Following liquid-liquid extraction HPLC separation was achieved on a ProntoSil AQ, C18 column using a gradient with 10 mM ammonium acetate in water (pH 7.25) and acetonitrile. The mass spectrometer was operated in the selected ion monitoring mode using the respective MH(+) ions, m/z 346 for omeprazole, m/z 362 for 5-hydroxy-omeprazole and omeprazol-sulfone and m/z 300 for the internal standard (2-{[(3,5-dimethylpyridine-2-yl)methyl]thio}-1H-benzimidazole-5-yl)methanol. The limit of quantification (LOQ) achieved with this method was 5 ng/ml for 5-hydroxyomeprazole and 10 ng/ml for omeprazole and omeprazole-sulfone using 0.25 ml of plasma. Intra- and inter-assay variability was below 11% over the whole concentration range from 5 to 250 ng/ml for 5-hydroxyomeprazol and from 10 to 750 ng/ml for omeprazole and omeprazole-sulfone. The method was successfully applied to the determination of pharmacokinetic parameters of esomeprazole and the two major metabolites after a single dose and under steady state conditions.

  7. Effects of Omeprazole on Iron Absorption: Preliminary Study

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    Mahmut Yaşar Çeliker

    2013-09-01

    Full Text Available Objective: Increasing numbers of pediatric and adult patients are being treated with proton pump inhibitors (PPIs. PPIs are known to inhibit gastric acid secretion. Nonheme iron requires gastric acid for conversion to the ferrous form for absorption. Ninety percent of dietary and 100% of oral iron therapy is in the nonheme form. To the best of our knowledge, the effect of PPIs on iron absorption has not been studied in humans. Our study assessed the relationship between omeprazole therapy and iron absorption in healthy subjects. Materials and Methods: We recruited 9 healthy volunteers between June 2010 and March 2011. Subjects with chronic illness, anemia, or use of PPI therapy were excluded. Serum iron concentrations were measured 1, 2, and 3 h after the ingestion of iron (control group. The measurements were repeated on a subsequent visit after 4 daily oral administrations of omeprazole at a dose of 40 mg (treatment group. Results: One female and 8 male volunteers were enrolled in the study with a mean age of 33 years. There was no statistical difference detected between baseline, 1-h, 2-h, and 3-h iron levels between control and treatment groups. Conclusion: Administration of omeprazole for a short duration does not affect absorption of orally administered iron in healthy individuals.

  8. Determination of omeprazole and its metabolites in human plasma by liquid chromatography-mass spectrometry.

    Science.gov (United States)

    Kanazawa, Hideko; Okada, Akiko; Matsushima, Yoshikazu; Yokota, Hiromitsu; Okubo, Shigeo; Mashige, Fumiko; Nakahara, Kazuhiko

    2002-03-08

    Omeprazole is a benzimidazole compound that acts as a proton-pump inhibitor. Because the metabolism of omeprazole is mainly catalyzed by cytochrome P-450 (CYP) 3A4 and CYP2C19. the genetic polymorphism of CYP2C19 could be of clinical concern in the treatment of acid-related diseases with omeprazole. Therefore, a reliable method for omeprazole phenotyping is desirable in clinical situations. This study has demonstrated the determination of omeprazole and its metabolites in human plasma by liquid chromatography-three-dimensional quadrupole mass spectrometry with a sonic spray ionization interface. The analytical column was YMC-Pack Pro C18(50x2.0 mm I.D.) using acetonitrile-50 mM ammonium acetate (pH 7.25) (1:4) at a flow-rate of 0.2 ml/min. The drift voltage was 30 V. The sampling aperture was heated at 110 degrees C and Shield temperature was 230 degrees C. In the mass spectrum, the molecular ions of omeprazole, hydroxyomeprazole and omeprazole sulfone were clearly observed as base peaks. This method is sufficiently sensitive and accurate for pharmacokinetic studies of omeprazol.

  9. Giardial triosephosphate isomerase as possible target of the cytotoxic effect of omeprazole in Giardia lamblia.

    Science.gov (United States)

    Reyes-Vivas, Horacio; de la Mora-de la Mora, Ignacio; Castillo-Villanueva, Adriana; Yépez-Mulia, Lilian; Hernández-Alcántara, Gloria; Figueroa-Salazar, Rosalia; García-Torres, Itzhel; Gómez-Manzo, Saúl; Méndez, Sara T; Vanoye-Carlo, América; Marcial-Quino, Jaime; Torres-Arroyo, Angélica; Oria-Hernández, Jesús; Gutiérrez-Castrellón, Pedro; Enríquez-Flores, Sergio; López-Velázquez, Gabriel

    2014-12-01

    Giardiasis is highly prevalent in the developing world, and treatment failures with the standard drugs are common. This work deals with the proposal of omeprazole as a novel antigiardial drug, focusing on a giardial glycolytic enzyme used to follow the cytotoxic effect at the molecular level. We used recombinant technology and enzyme inactivation to demonstrate the capacity of omeprazole to inactivate giardial triosephosphate isomerase, with no adverse effects on its human counterpart. To establish the specific target in the enzyme, we used single mutants of every cysteine residue in triosephosphate isomerase. The effect on cellular triosephosphate isomerase was evaluated by following the remnant enzyme activity on trophozoites treated with omeprazole. The interaction of omeprazole with giardial proteins was analyzed by fluorescence spectroscopy. The susceptibility to omeprazole of drug-susceptible and drug-resistant strains of Giardia lamblia was evaluated to demonstrate its potential as a novel antigiardial drug. Our results demonstrate that omeprazole inhibits giardial triosephosphate isomerase in a species-specific manner through interaction with cysteine at position 222. Omeprazole enters the cytoplasmic compartment of the trophozoites and inhibits cellular triosephosphate isomerase activity in a dose-dependent manner. Such inhibition takes place concomitantly with the cytotoxic effect caused by omeprazole on trophozoites. G. lamblia triosephosphate isomerase (GlTIM) is a cytoplasmic protein which can help analyses of how omeprazole works against the proteins of this parasite and in the effort to understand its mechanism of cytotoxicity. Our results demonstrate the mechanism of giardial triosephosphate isomerase inhibition by omeprazole and show that this drug is effective in vitro against drug-resistant and drug-susceptible strains of G. lamblia.

  10. Rhabdomyolysis secondary to drug interaction between atorvastatin, omeprazole, and dexamethasone

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    Elazzazy S

    2012-09-01

    Full Text Available Shereen Elazzazy,1 Saad S Eziada,2 Manal Zaidan11Pharmacy Department, 2Oncology Hematology Department, National Center for Cancer Care and Research, Hamad Medical Corporation, Doha, QatarAbstract: Concomitant administration of atorvastatin, omeprazole, and dexamethasone has been shown to increase the serum concentration of serum hydroxymethylglutaryl coenzyme A which can be associated with elevation of creatine kinase and an increased risk of severe myopathy and rhabdomyolysis. In this paper, we report a case of a 60-year-old female patient with stage IV colon cancer and compromised hepatic function receiving palliative care who developed rhabdomyolysis while taking atorvastatin, omeprazole, and dexamethasone. Atorvastatin was stopped, and the dexamethasone dose was decreased. Her case was complicated by urosepsis cultures revealing an extended spectrum β-lactamase-producing strain of Escherichia coli, and she died on the second day after admission. Physicians should evaluate the risk/benefit ratio of continuing statins in palliative care patients, and pay special attention to the monitoring of patients on statins and P-glycoprotein inhibitors regardless of hepatic function.Keywords: statins, rhabdomyolysis, drug–drug interaction, P-glycoprotein inhibitors

  11. Formulation and evaluation of omeprazole tablets for duodenal ulcer

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    Choudhury A

    2010-01-01

    Full Text Available Omeprazole pellets containing mucoadhesive tablets were developed by direct punch method. Three mucoadhesive polymers namely hydroxypropylemethylcellulose K4M, sodium carboxy methylcellulose, carbopol-934P and ethyl cellulose were used for preparation of tablets which intended for prolong action may be due to the attachment with intestinal mucosa for relief from active duodenal ulcer. Mucoadhesive tablets were coated with respective polymer and coated with Eudragit L100 to fabricate enteric coated tablets. The prepared tablets were evaluated for different physical parameters and dissolution study were performed in three dissolution mediums like 0.1N hydrochloric acid for 2h, pH 6.5 and pH 7.8 phosphate buffer solution for 12hr. Sodium carboxymethylcellulose showed above 95% release within 10 h where as carbopol-934P showed slow release about 88% to 92% over a period of 12 h. having excellent mucoadhesive strength but ethyl cellulose containing tablets showed less than 65% release. The release mechanism of all formulation was diffusion controlled confirmed from Higuchi′s plot. Thus, the present study concluded that, carbopol-934P containing mucoadhesive tablets of omeprazole pellets can be used for local action in the ulcer disease as well as for oral controlled release drug delivery.

  12. Omeprazole use at University Hospital in Porto Alegre-RS (Brazil / Uso de omeprazol en el hospital universitario de Porto Alegre-RS (Brasil / Uso de omeprazol em hospital universitário de Porto Alegre-RS (Brasil

    Directory of Open Access Journals (Sweden)

    Morrone FB

    2004-12-01

    Full Text Available Intestinal bleeding are important cause of hospital admissions and death, being relevant in critically weak patients and those with arthritis and osteoarthritis using NSAIDs. Omepazole is the first choice drug for prophylaxis of stress ulcer and NSAID complications prevention, because it prevent not only duodenal but also gastric ulcer and eradication of H pylori used with antibiotics. The aim of this study was to determine frequency of use, indications and characteristics of population using omeprazole. A qualitative and quantitative drug utilization study was done. In-hospital adults at a University Hospital constituted study population. From 91 patients studied, the majority suffered from cancer (24.2%. Average length of stay and omeprazole use time was 20 and 12 days, respectively. Abdominal surgery team was the higher omeprazole prescriber, and main indication was post-surgery. Although most of omeprazole uses was acceptable, those could be better evaluated. T could be useful implementing a pharmaceutical care program and creating a omeprazole use guideline with the objective of prescribing it in a more rationale and adequate way for each patient.

  13. Omeprazole maintenance therapy prevents recurrent ulcer bleeding after surgery for duodenal ulcer

    Institute of Scientific and Technical Information of China (English)

    Konstantinos Demertzis; Dimitrios Polymeros; Theodoros Emmanuel; Konstantinos Triantafyllou; Pericles Tassios; Spiros D Ladas

    2006-01-01

    AIM: To evaluate the omeprazole maintenance therapy in patients with recurrent ulcer bleeding after surgery for duodenal ulcer.METHODS: We studied 15 consecutive patients with recurrent ulcer bleeding after surgery for duodenal ulcer.Omeprazole (20 mg/d) maintenance therapy was given after ulcer healing. In addition to clinical follow-up, ambulatory 24-h gastric pH assay was performed before and during omeprazole therapy in those patients and controls with previous duodenal ulcer surgery but no ulcer recurrence.RESULTS: All the 15 ulcers were healed after being treated with omeprazole (40 mg/d) for 2 mo. Eleven patients with two (1-9) episodes of recurrent ulcer bleeding completed the follow-up (43, 12-72 mo). None of them had a bleeding episode while on omeprazole. One patient discontinued the therapy and had recurrent bleeding. The median 24-h fraction time of gastric pH <4 in patients was 80, 46-95% , and was reduced to 32, 13-70% by omeprazole (P = 0.002).CONCLUSION: Long-term maintenance therapy with omeprazole (20 mg/day) is effective in preventing recurrent ulcer bleeding.

  14. Efficacy of omeprazole paste in the treatment and prevention of gastric ulcers in horses.

    Science.gov (United States)

    Andrews, F M; Sifferman, R L; Bernard, W; Hughes, F E; Holste, J E; Daurio, C P; Alva, R; Cox, J L

    1999-04-01

    Equine gastric ulcer syndrome (EGUS) is very common among performance horses, with a reported prevalence of approximately 90% in racehorses, and also > 50% in foals. Omeprazole, an acid pump inhibitor 5 times more potent than ranitidine, has been used with great success to treat EGUS. This multicentre study of Thoroughbred racehorses with endoscopically verified gastric ulcers was designed to demonstrate the efficacy of an equine oral paste formulation of omeprazole in the treatment and prevention of recurrence of EGUS. Of the 100 horses entered into the study, 25 were sham-dosed for the full 58 days of the study. The remaining 75 horses all received omeprazole paste, 4 mg/kg bwt/day once daily for 28 days. At Day 28, 25 of treated horses continued on this dosing regimen while 25 received a half dose (2 mg/kg bwt once daily) and 25 horses were sham-dosed. By Day 28, gastric ulcers were completely healed in 77% of omeprazole-treated horses, while 92% were significantly (P < 0.01) improved. In contrast, 96% of the sham-dosed horses still had gastric ulcers at Day 28. The improvement was maintained in horses that continued on either a full dose or half dose of omeprazole paste until Day 58. However, in those horses that were removed from omeprazole treatment at Day 28, the incidence and severity of the gastric ulcers at the end of the study were similar to those horses that did not receive the omeprazole paste. This study demonstrates that omeprazole paste, 4 mg/kg bwt per os, once daily, is highly effective in healing gastric ulcers in Thoroughbred racehorses and that either a full dose or half dose of omeprazole paste effectively prevents the recurrence of EGUS. The study also indicates that gastric ulcers in untreated horses did not demonstrate a significant rate of spontaneous healing.

  15. Pharmacokinetic Comparison of Omeprazole Granule and Suspension Forms in Children: A Randomized, Parallel Pilot Trial.

    Science.gov (United States)

    Karami, S; Dehghanzadeh, G; Haghighat, M; Mirzaei, R; Rahimi, H R

    2016-03-01

    Although, omeprazole is widely used for treatment of gastric acid-mediated disorders. However, its pharmacokinetic and chemical instability does not allow simple aqueous dosage form formulation synthesis for therapy of, especially child, these patients. The aim of this study was at first preparation of suspension dosage form omeprazole and second to compare the blood levels of 2 oral formulations/dosage forms of suspension & granule by high performance liquid chromatography (HPLC). The omeprazole suspension was prepared; in this regard omeprazole powder was added to 8.4% sodium bicarbonate to make final concentration 2 mg/ml omeprazole. After that a randomized, parallel pilot trial study was performed in 34 pediatric patients with acid peptic disorder who considered usage omeprazole. Selected patients were received suspension and granule, respectively. After oral administration, blood samples were collected and analyzed for omeprazole levels using validated HPLC method. The mean omeprazole blood concentration before usage the next dose, (trough level) were 0.12±0.08 µg/ml and 0.18±0.15 µg/ml for granule and suspension groups, respectively and mean blood level after dosing (C2 peak level) were 0.68±0.61 µg/ml and 0.86±0.76 µg/ml for granule and suspension groups, respectively. No significant changes were observed in comparison 2 dosage forms 2 h before (P=0.52) and after (P=0.56) the last dose. These results demonstrate that omeprazole suspension is a suitable substitute for granule in pediatrics.

  16. Animal pharmacodynamics of omeprazole. A survey of its pharmacological properties in vivo.

    Science.gov (United States)

    Larsson, H; Mattson, H; Sundell, G; Carlsson, E

    1985-01-01

    In the present paper, a collection of experimental data is presented describing the pharmacological profile of omeprazole mainly in dogs and rats. Omeprazole potently inhibited gastric acid secretion in different experimental models. In the dog, for instance, omeprazole was 2-7 times more potent than cimetidine, depending on the route of administration, and in the rat the difference was even greater. Omeprazole was equally potent against different types of stimulation, whereas cimetidine was not, indicating differences in their mechanisms of action. In the dog, the duration of the antisecretory effect was long and lasted for 3-4 days after a single maximal dose of omeprazole. The inhibitory effect after repeated, daily administration of submaximal doses therefore gradually increased and attained a steady-state level after five doses. Treatment up to one year with very high oral doses did not affect the duration of effect. During long-term treatment with high doses of omeprazole a 10-fold increase in meal-stimulated plasma gastrin levels was recorded. This was probably due to a nearly complete inhibition of acid secretion over 24 hours during the study. The gastrin values returned to control levels within eight days after the end of the treatment. Omeprazole was rapidly absorbed (peak plasma levels were reached within one hour) and the elimination half-life was approximately one hour. In the dog, the gastric antisecretory effect was related to the total dose and the area under the plasma concentration curve, whereas the peak level or the shape of the curve was of minor importance. Omeprazole, given orally to rats, dose-dependently prevented experimentally induced gastric lesions. Neither inhibition of acid secretion, stimulation of gastric bicarbonate secretion nor interference with the synthesis of endogenous prostaglandins seems to be of any great importance for the gastric protective effect of omeprazole. Omeprazole seems to be very specific in its gastric acid

  17. Effects of omeprazole on iron absorption: preliminary study.

    Science.gov (United States)

    Tempel, Mila; Chawla, Anupama; Messina, Catherine; Celiker, Mahmut Yaşar

    2013-09-01

    Amaç: Giderek artan sayıda pediatrik ve yetişkin hastalar proton pompa inhibitörleri (PPI) ile tedavi edilmektedir. PPI’ların mide asidini inhibe ettikleri bilinmektedir. Heme’e bağlı olmayan demir ferroz şekline geçerek absorb edilebilmesi için mide asidi gerektirir. Diyetteki demirin yüzde doksanı ve tedavide kullanılan demirin yüzde yüzü heme’e bağlı olmayan durumdadır. Bilgimize göre PPI’ların demir absobsiyonunda nasıl etki ettiği insanlarda araştırılmamıstır. Araştırmamız omeprazol tedavisi ile demir absorbsiyonu arasındaki ilişkiyi sağlıklı kişilerde incelemiştir.Gereç ve Yöntemler: Haziran 2010 ile Mart 2011 arasında 9 sağlıklı gönüllüyü çalışmamiz için davet ettik. Kronik hastalığı veya anemisi olan kişilerle PPI tedavisinde olan kişileri dışladık. Serum demir konsantrasyonunu demir alımından 1, 2, ve 3 saat sonra ölçtük (kontrol grubu). Bu ölçümleri bir sonraki ziyarette 4 günlük oral 40 mg dozunda omeprazol tedavisinden sonra tekrarladık (tedavi grubu).Bulgular: Ortalama yaşları 33 yıl olan 8 erkek ve 1 kadın gönüllü çalışmamıza katıldı. Kontrol grubu ile tedavi grubu arasında bazal, 1 saat, 2 saat, ve 3 saat sonraki demir konsantrasyonları arasında istatistiksel anlamlı bir fark görülmedi. Sonuç: Sağlıklı kişilerde kısa bir zaman sürecince verilen omeprazol oral olarak alınan demirin absorbsiyonunu etkilemez.

  18. [Behavior of acid secretion under the long-term daily administration of omeprazol].

    Science.gov (United States)

    Dammann, H G; Müller, P; Seitz, H K; Simon, B

    1983-06-18

    The effect of the substituted benzimidazole omeprazole on acid secretion after repeated administration to healthy volunteers has been studied. During repeated dosage of 30 mg once daily inhibition of basal and pentagastrin-stimulated acid output was increased from 30% after the first dose to about 60% after dose 4. The extent of inhibition did not further increase between day 5 and day 10. In four volunteers acid secretion returned to predose levels within 5 days after drug withdrawal. The 24-hour gastric acidity was reduced by about 72% and 82% after 9-day pretreatment with 30 mg and 60 mg omeprazole respectively. The antisecretory effect of omeprazole was independent of peak plasma concentrations. Omeprazole given once daily therefore possesses a long-lasting effect on gastric acid secretion, i.e. for more than 24 hours. This effect appears to be fully reversible since control levels of acid output are reached within 5 days.

  19. Pharmacokinetic drug interaction profile of omeprazole with adverse consequences and clinical risk management

    Directory of Open Access Journals (Sweden)

    Li W

    2013-05-01

    Full Text Available Wei Li,1 Su Zeng,2 Lu-Shan Yu,2 Quan Zhou31Division of Medical Affairs, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, People’s Republic of China; 2Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People’s Republic of China; 3Department of Pharmacy, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, People’s Republic of ChinaBackground: Omeprazole, a proton pump inhibitor (PPI, is widely used for the treatment of dyspepsia, peptic ulcer, gastroesophageal reflux disease, and functional dyspepsia. Polypharmacy is common in patients receiving omeprazole. Drug toxicity and treatment failure resulting from inappropriate combination therapy with omeprazole have been reported sporadically. Systematic review has not been available to address the pharmacokinetic drug-drug interaction (DDI profile of omeprazole with adverse consequences, the factors determining the degree of DDI between omeprazole and comedication, and the corresponding clinical risk management.Methods: Literature was identified by performing a PubMed search covering the period from January 1988 to March 2013. The full text of each article was critically reviewed, and data interpretation was performed.Results: Omeprazole has actual adverse influences on the pharmacokinetics of medications such as diazepam, carbamazepine, clozapine, indinavir, nelfinavir, atazanavir, rilpivirine, methotrexate, tacrolimus, mycophenolate mofetil, clopidogrel, digoxin, itraconazole, posaconazole, and oral iron supplementation. Meanwhile, low efficacy of omeprazole treatment would be anticipated, as omeprazole elimination could be significantly induced by comedicated efavirenz and herb medicines such as St John's wort, Ginkgo biloba, and yin zhi huang. The mechanism for DDI involves induction or inhibition of cytochrome P450, inhibition of P-glycoprotein or breast

  20. [Omeprazole: a new treatment for paranasal sinus polyps in Widal syndrome. Preliminary study].

    Science.gov (United States)

    Serra, J; Piñas, J; Arnaiz, J A; Quesada, P; Naches, S; Lorente, J; Carne, X

    1998-05-01

    A preliminary report is made of the potential therapeutic effect of omeprazol in reducing nasosinusal polyps. This study is based on the empirical observation of nasal airflow improvement in patients suffering from nasosinusal polyposis after administering omeprazol. Different phases of the study suggested that patients with Widal's syndrome benefited the most. Based on the results of this study, we have undertaken a randomized, parallel, double-blind, placebo-controlled clinical trial.

  1. Omeprazole pharmacodynamics and gastric acid suppression in critically ill pediatric transplant patients.

    Science.gov (United States)

    Olsen, K M; Bergman, K L; Kaufman, S S; Rebuck, J A; Collier, D S

    2001-07-01

    OBJECTIVE: To characterize the pharmacodynamics and pharmacokinetics of omeprazole suspension in critically ill pediatric liver/intestinal transplant patients. DESIGN: Open-label pharmacodynamic and pharmacokinetic study. SETTING: Pediatric intensive care unit of an academic medical center. PATIENTS: Eleven pediatric liver and/or intestinal transplant patients. INTERVENTIONS: Extemporaneously prepared 0.5 mg/kg omeprazole suspension every 12 hrs via nasogastric tube before sequential measurements of omeprazole serum concentration and gastric pH monitoring. Gastric pH was monitored continuously for 48 hrs and plasma omeprazole concentrations were determined upon first and multiple dosing. MEASUREMENTS AND MAIN RESULTS: Mean onset of action of omeprazole in a sodium bicarbonate vehicle was 62 +/- 82 mins (range, 2-226 mins). Subjects omeprazole action (range, 3-226 mins) when compared with older subjects (onset of action, 2-40 min). Omeprazole maximum concentration and area under the concentration-time curve for the dosage interval were significantly greater upon multiple dosing when compared with the first dose. Mean baseline gastric pH in this study population was 1.0 +/- 0.8. Gastric pH remained >4.0 for 78.8% +/- 18.9% of the first dosage interval and 97.8% +/- 5.4% of multiple dosage intervals regardless of age when administered twice daily as a suspension. CONCLUSION: These results support the use of omeprazole administered twice daily as a suspension to maintain gastric pH of >4.0 and to achieve maximal pharmacodynamic effect in pediatric liver and/or intestinal transplant patients.

  2. Effects of pirenzepine on omeprazole-induced gastrin gene expression in rat antral tissues.

    Science.gov (United States)

    Tari, A; Hamada, M; Kamiyasu, T; Fukino, Y; Sumii, M; Sumii, K; Kajiyama, G

    1996-06-01

    Pirenzepine has inhibitory effects on gastrin secretion both in vivo and in vitro. The aim of this study was to determine the mechanism responsible for the suppression of omeprazole-induced hypergastrinemia that occurs with pirenzepine treatment. The effects were measured in rats treated with oral omeprazole plus intraperitoneal pirenzepine or saline once daily for seven days in the antrum. The serum gastrin level increased significantly by more than sixfold with omeprazole treatment; additional treatment with pirenzepine suppressed this increase by 48%. Pirenzepine treatment did not change the level of gastrin mRNA but significantly increased the level of somatostatin mRNA. Combination treatment with omeprazole plus pirenzepine significantly decreased the gastrin mRNA level to half and significantly increased the somatostatin mRNA level up to 1.4-fold of the levels achieved with omeprazole treatment alone. These results suggest that the stimulatory effect of omeprazole on gastrin synthesis is partially blocked by pirenzepine via mediation of somatostatin synthesis in the antrum.

  3. A double-blind placebo-controlled trial of omeprazole on urinary pH in healthy subjects

    DEFF Research Database (Denmark)

    Osther, P J; Rasmussen, L; Pedersen, S A

    1992-01-01

    Urinary pH is related to urinary calculus formation as well as urinary infection. Omeprazole is an effective inhibitor of gastric acid secretion through inhibition of the parietal cell H+K+ATPase. In this study we have evaluated a possible effect of omeprazole on urine acidification. Ten healthy...... male subjects took placebo and omeprazole, 40 mg o.m., for 10 days in a double-blind placebo-controlled trial. Morning fasting urinary pH was measured on day 10 of each treatment course using a pH meter. No effect of omeprazole on urinary pH could be demonstrated. It is thus unlikely...... that it is necessary to take omeprazole treatment into consideration in stone screening. As omeprazole did not affect urinary pH, no urological side effects related to changes in urinary pH can be expected....

  4. The effect of intravenous omeprazole on the gastric and duodenal potential difference and pH in healthy subjects

    DEFF Research Database (Denmark)

    Rubinstein, E; Højgaard, L

    1993-01-01

    The effect of intravenous omeprazole (40 and 80 mg) on the gastric and duodenal potential difference (PD) and pH was investigated in 9 healthy volunteers. Gastric PD and pH increased significantly (p omeprazole, and the increases were equal following the two doses. No changes were...... found in duodenal PD or pH. It has been claimed that gastric PD changes following acid secretion inhibition with cimetidine and glucagon might be due to changes in the parietal cell surface area. Omeprazole causes no changes in the parietal cell structure, and the changes in gastric PD following...... omeprazole might therefore be ascribed to changes in mucosal electrophysiologic transport or resistance....

  5. Effect of L-lactic acid on calcium absorption in rats fed omeprazole.

    Science.gov (United States)

    Chonan, O; Takahashi, R; Yasui, H; Watanuki, M

    1998-06-01

    We examined the effect of L-lactic acid on calcium absorption in male Wistar rats made achlorhydric by dietary omeprazole, a proton pump inhibitor. The dietary omeprazole intake (0.03 g/100 g of diet) increased the gastric pH and decreased the apparent calcium absorption ratio. Dietary famotidine (0.03 g/100 g of diet), an H2-receptor antagonist, and lower doses of omeprazole (0.005 or 0.01 g/100 g of diet) did not affect the gastric pH or the calcium absorption. In a second experiment, dietary lactic acid (0.5, 1.0, or 2.5 g/100 g of diet) increased the intestinal calcium absorption dose dependently in rats fed omeprazole (0.03 g/100 g of diet). The gastric pH was significantly decreased only in the rats fed higher doses of lactic acid (1.0, or 2.5 g/100 g of diet). In a third experiment, a dietary sour milk beverage containing lactic acid (0.5 g/100 g of diet) increased the intestinal calcium absorption, but did not affect the gastric pH in rats fed omeprazole (0.03 g/100 g of diet). Although the significance of gastric acid in terms of overall calcium absorption is not known, under the present experimental conditions, the inhibition of gastric acid secretion by dietary omeprazole decreased the apparent calcium absorption, and the dietary lactic acid prevented the calcium absorption in rats fed omeprazole.

  6. A comparison of oral omeprazole and intravenous cimetidine in reducing complications of duodenal peptic ulcer

    Directory of Open Access Journals (Sweden)

    Khaleghian Farzaneh

    2006-01-01

    Full Text Available Abstract Background Gastrointestinal bleeding is a common problem and its most common etiology is peptic ulcer disease. Ulcer rebleeding is considered a perilous complication for patients. To reduce the rate of rebleeding and to fasten the improvement of patients' general conditions, most emergency departments in Iran use H2-blockers before endoscopic procedures (i.e. intravenous omeprazole is not available in Iran. The aim of this study was to compare therapeutic effects of oral omeprazole and intravenous cimetidine on reducing rebleeding rates, duration of hospitalization, and the need for blood transfusion in duodenal ulcer patients. Methods In this clinical trial, 80 patients with upper gastrointestinal bleeding due to duodenal peptic ulcer and endoscopic evidence of rebleeding referring to emergency departments of Imam and Sina hospitals in Tabriz, Iran were randomly assigned to two equal groups; one was treated with intravenous cimetidine 800 mg per day and the other, with 40 mg oral omeprazole per day. Results No statistically significant difference was found between cimetidine and omeprazole groups in regards to sex, age, alcohol consumption, cigarette smoking, NSAID consumption, endoscopic evidence of rebleeding, mean hemoglobin and mean BUN levels on admission, duration of hospitalization and the mean time of rebleeding. However, the need for blood transfusion was much lower in omeprazole than in cimetidine group (mean: 1.68 versus 3.58 units, respectively; p Conclusion This study demonstrated that oral omeprazole significantly excels intravenous cimetidine in reducing the need for blood transfusion and lowering rebleeding rates in patients with upper gastrointestinal bleeding. Though not statistically significant (p = 0.074, shorter periods of hospitalization were found for omeprazole group which merits consideration for cost minimization.

  7. Acid Inhibitory Effect of a Combination of Omeprazole and Sodium Bicarbonate (CDFR0209) Compared With Delayed-Release Omeprazole 40 mg Alone in Healthy Adult Male Subjects.

    Science.gov (United States)

    Kim, Kyu-Nam; Yang, Sung-Won; Kim, Hyunil; Kwak, Seong Shin; Kim, Young-Sang; Cho, Doo-Yeoun

    2017-01-23

    CDFR0209, a combination of an immediate-release formulation of omeprazole 40 mg and sodium bicarbonate 1100 mg, has been developed to treat acid-related disorders. We compared the acid inhibitory effects of CDFR0209 and delayed-release omeprazole (omeprazole-DR, Losec 40 mg) after repeated dosing in Helicobacter pylori-negative healthy adult male subjects. In this 2-period crossover study, 30 subjects were randomized to CDFR0209 or omeprazole-DR daily for 7 days. An ambulatory continuous 24-hour intragastric pH recording was performed at baseline and on days 1 and 7 of each administration period. Integrated gastric acidity was calculated from time-weighted average hydrogen ion concentrations at each hour of the 24-hour record. An analysis of variance model was used to test the pharmacodynamic equivalence of CDFR0209 and omeprazole-DR, using the natural logarithmic transformation of the percent decrease from baseline in integrated gastric acidity for the 24-hour interval after the seventh dose of each omeprazole formulation. The geometric least-squares mean ratios (CDFR0209/omeprazole-DR) of the percent decrease from baseline in integrated gastric acidity was 0.98 (90%CI, 0.93-1.07). Both CDFR0209 and omeprazole-DR are equally effective in decreasing integrated gastric acidity at steady state.

  8. Chemical stability of extemporaneously compounded omeprazole formulations: a comparison of two methods of compounding.

    Science.gov (United States)

    Garg, Sanjay; Svirskis, Darren; Al-Kabban, Majid; Farhan, Samer; Komeshi, Mohammed; Lee, Jacky; Liu, Quincy; Naidoo, Sacha; Kairuz, Therese

    2009-01-01

    Liquid preparations of omeprazole are compounded extemporaneously for patients who cannot tolerate or have difficulty with tablets or capsules, such as those with a nasogastric tube or jejunal or feeding tube, those with a swallowing disorder, and young children and the elderly. Recommendations for preparation of a liquid from the enteric-coated pellets of omeprazole capsules are available in the literature. The pellets are dissolved in a sodium bicarbonate solution; shaking is recommended to aid dissolution. Apparently some pharmacists crush the pellets to speed up the compounding process. The aim of this study was to investigate the chemical stability of omeprazole in extemporaneously compounded liquids prepared by the grinding and shaking methods. A high-performance liquid chromatographic method was developed for evaluation of chemical stability. Samples were stored at 2 deg C (refrigerated conditions) or 25 deg C/60% relative humidity and assayed for drug concentration at 0, 1, 2, 4, and 8 weeks. The method of preparation affected the chemical stability of omeprazole when stored at 25 deg C/60% relative humidity; it was stable for 4 weeks if prepared by the shaking method, but for only 1 week if prepared by the grinding method. For both methods, the suspension was stable for 8 weks if stored under refrigerated conditions. It is recommended that the shaking method be employed for extemporaneously compounded omeprazole suspensions, and that the prepared suspension be stored in the refrigerator.

  9. Avaliação do uso profilático de omeprazol em pacientes internados no hospital estadual Américo Brasiliense

    OpenAIRE

    Abjaude, Samir Antonio Rodrigues [UNESP

    2015-01-01

    Introduction. Omeprazole is a widely used drug; in most cases, it is effective and safe. However, studies have found omeprazole to be the drug most frequently related to hospital admissions due to adverse drug reactions (ADRs). The ADRs could have occurred as a result of abuse or irrational prescribing of omeprazole. Despite that possibility, the risks and benefits of prophylactic omeprazole considering the approved and off-label uses and the potential consequences for patient safety have not...

  10. Effect of omeprazole and cimetidine on healing of chronic gastric ulcers and gastric acid secretion in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier

    1988-01-01

    The effect of omeprazole and cimetidine on healing of chronic gastric ulcers and gastric acid secretion was investigated in rats. The effect of three doses of omeprazole given orally once daily for 25 days was investigated. In controls median ulcer healing was 19.6% after 25 days. Omeprazole...... increased median ulcer healing from 36% at 145 mumole/kg/day to 80% at 580 mumole/kg/day. Basal and pentagastrin stimulated gastric acid secretion decreased dose-dependently by nearly 90% at a dose of 580 mumole/kg/day 22-24 hr after the last dose of omeprazole. Cimetidine given twice daily, in a dose...... that initially inhibits gastric acid secretion by 95%, reduced acid secretion by only 50% 11 hr after the last dose. Median ulcer healing after treatment with cimetidine for 25 days was 41%. This study demonstrates that omeprazole has a more long-acting inhibitory effect on gastric acid secretion compared...

  11. Esophagectomy with gastroplasty in advanced megaesophagus: late results of omeprazole use

    Directory of Open Access Journals (Sweden)

    Celso de Castro Pochini

    Full Text Available Objective: To analyze the late results of advanced Chagasic megaesophagus treatment by esophagectomy associated with the use of proton pump inhibitor (omeprazole as for the incidence of esophagitis and Barrett's esophagus in the remaining stump. Methods : We studied patients with advanced megaesophagus undergoing esophagectomy and transmediastinal esophagogastroplasty. Patients were divided into three groups: A (20 with esophageal replacement by full stomach, without the use of omeprazole; B (20 with esophageal replacement by full stomach, with omeprazole 40 mg/day introduced after the first postoperative endoscopy and maintained for six years; and C (30 with esophageal replacement by gastric tube with use of omeprazole. Dysphagia, weight loss and BMI were clinical parameters we analyzed. Upper gastrointestinal endoscopy was performed in all patients, and determined the height of the anastomosis, the aspect of the mucosa, with special attention to possible injuries arising from gastroesophageal reflux, and the patency of the esophagogastric anastomosis. Results : We studied 50 patients, 28 males (56% and 22 (44% females. All underwent endoscopy every year. In the first endoscopy, erosive esophagitis was present in nine patients (18% and Barrett's esophagus, in four (8%; in the last endoscopy, erosive esophagitis was present in five patients (8% and Barrett's esophagus in one (2%. When comparing groups B and C, there was no evidence that the manufacturing of a gastric tube reduced esophagitis and Barrett's esophagus. However, when comparing groups A and C, omeprazole use was correlated with reduction of reflux complications such as esophagitis and Barrett's esophagus (p <0.005. Conclusion : The use of omeprazole (40 mg/day reduced the onset of erosive esophagitis and Barrett's esophagus during the late postoperative period.

  12. The effects of dose and diet on the pharmacodynamics of omeprazole in the horse.

    Science.gov (United States)

    Sykes, B W; Underwood, C; Greer, R; McGowan, C M; Mills, P C

    2017-07-01

    Conflicting data are presented in the current literature regarding the efficacy of omeprazole for suppressing gastric acidity in the horse. The objective of this study was to investigate the duration of intraday acid suppression achieved with two doses of omeprazole under two different dietary conditions. A four-way crossover design. Six adult Thoroughbred horses instrumented with percutaneous gastrotomy tubes were used. Intragastric pH was measured for continuous 23 h periods (08.00-07.00 h) for six consecutive days (Days 0-5). Baseline data was recorded on Day 0 and omeprazole administered on Days 1-5. Two doses (1 mg/kg and 4 mg/kg bwt per os once a day) and two diets (a high grain/low fibre [HG/LF] and ad libitum hay [HAY)] diet) were studied. Data for the percent (%) time pH was above 4 (%tpH>4) and median intraday pH was reported for two measurement locations and analysed using generalised estimating equations. An effect of both diet and dose was evident with mean %tpH>4 and the mean of the median intraday pHs typically higher at the higher (4 mg/kg bwt) dose and in HG/LF diet. The overall efficacy of omeprazole in raising intragastric pH was good under the HG/LF conditions but relatively poor in the HAY diet. A cumulative effect of dosing, not previously reported in the horse, was observed. The overall efficacy of omeprazole in raising ventral gastric pH was less than previously reported. Both dose and diet may play a role in the efficacy of omeprazole in the horse. Therefore, the use of singular dosing recommendations that encompass all horse types and management conditions may not be appropriate and dosing recommendations that take into account the diet of the horse may be advantageous. © 2016 EVJ Ltd.

  13. Omeprazole Inhibits Pancreatic Cancer Cell Invasion through a Nongenomic Aryl Hydrocarbon Receptor Pathway.

    Science.gov (United States)

    Jin, Un-Ho; Kim, Sang-Bae; Safe, Stephen

    2015-05-18

    Omeprazole and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) are aryl hydrocarbon receptor (AhR) agonists that inhibit the invasion of breast cancer cells through inhibition of CXCR4 transcription. Treatment of highly invasive Panc1 pancreatic cancer cells with TCDD, omeprazole, and seven other AhR-active pharmaceuticals showed that only omeprazole and tranilast, but not TCDD, inhibited invasion in a Boyden chamber assay. Similar results were observed in MiaPaCa2 cells, another quasimensenchymal pancreatic ductal adenocarcinoma (QM-PDA) pancreatic cancer cell line, whereas invasion was not observed with BxPC3 or L3.6pL cells, which are classified as classical (less invasive) pancreatic cancer cells. It was also observed in QM-PDA cells that TCDD, omeprazole, and tranilast did not induce CYP1A1 or CXCR4 and that treatment with these compounds did not result in nuclear uptake of AhR. In contrast, treatment of BxPC3 and L3.6pL cells with these AhR ligands resulted in induction of CYP1A1 (by TCDD) and nuclear uptake of AhR, which was similar to that observed for Ah-responsive MDA-MB-468 breast and HepG2 liver cancer cell lines. Results of AhR and AhR nuclear translocator (Arnt) knockdown experiments in Panc1 and MiaPaCa2 cells demonstrated that omeprazole- and tranilast-mediated inhibition of invasion was AhR-dependent but Arnt-independent. These results demonstrate that in the most highly invasive subtype of pancreatic cancer cells (QM-PDA) the selective AhR modulators omeprazole and tranilast inhibit invasion through a nongenomic AhR pathway.

  14. Comparison of outcomes twelve years after antireflux surgery or omeprazole maintenance therapy for reflux esophagitis

    DEFF Research Database (Denmark)

    Lundell, Lars; Miettinen, Pekka; Myrvold, Helge E

    2009-01-01

    . Heartburn and regurgitation were significantly more common in patients given omeprazole, whereas dysphagia, rectal flatulence, and the inability to belch or vomit were significantly more common in surgical patients. The therapies were otherwise well-tolerated. CONCLUSIONS: As long-term therapeutic...

  15. Perbandingan Efektivitas antara Omeprazol dan Lansoprazol terhadap Perbaikan Kualitas Hidup Penderita Rinosinusitis Kronik Akibat Refluks Laringofaring

    Directory of Open Access Journals (Sweden)

    Tantri Kurniawati

    2012-09-01

    Full Text Available Laryngopharyngeal reflux (LPR is the reflux of gastric acid through the esophagus that reaches laringopharyngeal area. The prevalence of LPR in the range 15–20%, and caused chronic rhinosinusitis (CRS. The incidence of LPR in patients with CRS has ranged between 37–72%. The prevalence of CRS 16,3% in adults and affecting quality of life. Omeprazole and lansoprazole are proton pump inhibitors (PPIs for LPR’s therapy and also a therapy for CRS with LPR as the etiology. This research method was randomized clinical trial with open trial observation, conducted in June to December 2009. Twenty subjects with consecutive sampling method, divided into two groups (with simple randomization, the first group received omeprazole and the other lansoprazole. The subjects conducted complete physical otolaryngology examination, sino-nasal outcome test 20, reflux symptom index and reflux finding score with fiber optic rhinolaryngoscopy. These data was obtained before therapy, after 2 weeks and two months therapy, analyzed with Wilcoxon’s and Mann-Whitney’s test. There was no effectivity difference between omperazole and lansoprazole in reducing the level of severity of LPR (p>0.05, but quality of life improvement was better in lansoprazole than omeprazole group (p<0.05. In conclusion, lansoprazole is more effective than omeprazole in improvement of quality of life in patients with chronic rhinosinusitis caused by LPR

  16. Pharmacokinetics and tolerability of a new formulation of omeprazole in the horse.

    Science.gov (United States)

    Di Salvo, A; Busechian, S; Zappulla, F; Marchesi, M C; Pieramati, C; Orvieto, S; Boveri, M; Predieri, P G; Rueca, F; Della Rocca, G

    2017-08-01

    A new formulation of omeprazole in gastro-resistant granules was tested with regard to its pharmacokinetics and tolerability. Twenty-four horses were randomly divided into three groups (8 horses/group) and treated, according a parallel study design, as follows: Group A untreated (control group), Group B received 4 mg/kg of omeprazole, and Group C received 12 mg/kg of omeprazole, both of which were treated orally once a day for 90 days. Blood samples, taken from Group B subjects during the 1st and the 29th day of treatment at pre-established time points, were used to determine the concentration-time curves of omeprazole. The treatments were found to be safe and well tolerated by the horses. The serum hematological and biochemical values were within reference ranges for the entire observational time. No accumulation of the drug was found after 29 days of treatment. Lower Cmax and AUCs were obtained at the 29th day of treatment. © 2016 John Wiley & Sons Ltd.

  17. Pharmacokinetics and bioequivalence testing of five commercial formulations of omeprazole in the horse.

    Science.gov (United States)

    Sykes, B W; Underwood, C; Greer, R; McGowan, C M; Mills, P C

    2016-02-01

    Omeprazole is widely used in the treatment of equine gastric ulcer syndrome. To date, little is known about the relative pharmacokinetics of the different formulations making comparisons between products difficult. The objectives of the study were to investigate the relative pharmacokinetics of five commercially available formulations of omeprazole in the horse and to test for bioequivalence of four of the formulations using one of the formulations as a reference standard. Twelve mature Thoroughbred horses were fasted for 16 h then administered 2 g of each formulation in a cross-over design. Serial blood samples were collected and plasma omeprazole concentration was determined by ultra high-performance liquid chromatography-mass spectrometry (UHPLC-MS). No significant differences were present between three of the formulations and the reference formulation, while the fourth formulation had a lower Cmax and longer Tmax than the reference formulation. Bioequivalence against the reference formulation could not be demonstrated for any of the formulations tested. The findings of the study suggested that the method of protection utilised by different formulations of omeprazole (enteric-coated granules vs. buffering) does not significantly alter the pharmacokinetics of the drug. Further work to establish bioequivalence is needed before direct comparisons can be drawn between different formulations.

  18. Prediction of Relative In Vivo Metabolite Exposure from In Vitro Data Using Two Model Drugs: Dextromethorphan and Omeprazole

    Science.gov (United States)

    Lutz, Justin D.

    2012-01-01

    Metabolites can have pharmacological or toxicological effects, inhibit metabolic enzymes, and be used as probes of drug-drug interactions or specific cytochrome P450 (P450) phenotypes. Thus, better understanding and prediction methods are needed to characterize metabolite exposures in vivo. This study aimed to test whether in vitro data could be used to predict and rationalize in vivo metabolite exposures using two model drugs and P450 probes: dextromethorphan and omeprazole with their primary metabolites dextrorphan, 5-hydroxyomeprazole (5OH-omeprazole), and omeprazole sulfone. Relative metabolite exposures were predicted using metabolite formation and elimination clearances. For dextrorphan, the formation clearances of dextrorphan glucuronide and 3-hydroxymorphinan from dextrorphan in human liver microsomes were used to predict metabolite (dextrorphan) clearance. For 5OH-omeprazole and omeprazole sulfone, the depletion rates of the metabolites in human hepatocytes were used to predict metabolite clearance. Dextrorphan/dextromethorphan in vivo metabolite/parent area under the plasma concentration versus time curve ratio (AUCm/AUCp) was overpredicted by 2.1-fold, whereas 5OH-omeprazole/omeprazole and omeprazole sulfone/omeprazole were predicted within 0.75- and 1.1-fold, respectively. The effect of inhibition or induction of the metabolite's formation and elimination on the AUCm/AUCp ratio was simulated. The simulations showed that unless metabolite clearance pathways are characterized, interpretation of the metabolic ratios is exceedingly difficult. This study shows that relative in vivo metabolite exposure can be predicted from in vitro data and characterization of secondary metabolism of probe metabolites is critical for interpretation of phenotypic data. PMID:22010218

  19. EFEITO DA RANITIDINA E DO OMEPRAZOL SOBRE O pH GÁSTRICO EM CÃES

    Directory of Open Access Journals (Sweden)

    Silvio Abrahão

    1999-01-01

    Full Text Available O objetivo deste trabalho foi investigar o efeito da ranitidina e omeprazol sobre o pH gástrico em 24 cães adultos, machos, sem raça definida, distribuídos em 3 grupos: grupo A - controle, grupo B - ranitidina e grupo C - omeprazol. O pH gástrico foi medido, após coleta do suco gástrico, com seringa, em cães submetidos a gastrotomia. Esta medida foi feita no grupo controle nos tempos zero, 30, 60, 90 e 120 minutos, no grupo ranitidina a medida foi feita no tempo zero, seguida de aplicação de 0,85 mg/kg de ranitidina por via endovenosa, sendo realizada nova medida nos tempos 30, 60, 90 e 120 minutos e, no grupo omeprazol a medida foi feita no tempo zero, seguida de aplicação de 0,68 mg/kg de omeprazol por via endovenosa, sendo realizada nova medida nos tempos 30,60, 90 e 120 minutos. A comparação entre os grupos mostrou um aumento significante do pH gástrico após o uso de ranitidina e omeprazol. Entretanto, os efeitos comparados da ranitidina e omeprazol não apresentaram diferenças significantes na variação do pH.The aim of this work was the ranitidine and omeprazole gastric pH effect investigation. 24 adults, male, mongrel dogs were distributed in 3 groups: group A - control, group B - ranitidine and group C - omeprazole. Gastric pH was measured after gastric juice syringe collection in dogs submitted to gastrotomy. Control group measurements were done at times zero, 30, 60, 90 and 120 minutes. Ranitidine group measurements were done at time zero, followed by 0,85 mg/kg endovenous ranitidine, and also at times 30, 60, 90 and 120 minutes. Omeprazole group measurements were done at time zero, followed by 0,68 mg/kg endovenous omeprazole and also at times 30, 60, 90 and 120 minutes. A significant increase in gastric pH, was observed, comparing groups, after ranitidine and omeprazole use. However, ranitidine and omeprazole compared effects presented no significant differences in pH variation.

  20. Omeprazole Blocks STAT6 Binding to the Eotaxin-3 Promoter in Eosinophilic Esophagitis Cells

    Science.gov (United States)

    Zhang, Xi; Cheng, Edaire; Huo, Xiaofang; Yu, Chunhua; Zhang, Qiuyang; Pham, Thai H.; Wang, David H.; Spechler, Stuart J.; Souza, Rhonda F.

    2012-01-01

    Background Patients who have esophageal eosinophilia without gastroesophageal reflux disease (GERD) nevertheless can respond to proton pump inhibitors (PPIs), which can have anti-inflammatory actions independent of effects on gastric acid secretion. In esophageal cell cultures, omeprazole has been reported to inhibit Th2 cytokine-stimulated expression of eotaxin-3, an eosinophil chemoattractant contributing to esophageal eosinophilia in eosinophilic esophagitis (EoE). The objective of this study was to elucidate molecular mechanisms underlying PPI inhibition of IL-4-stimulated eotaxin-3 production by esophageal cells. Methods/Findings Telomerase-immortalized and primary cultures of esophageal squamous cells from EoE patients were treated with IL-4 in the presence or absence of acid-activated omeprazole or lansoprazole. We measured eotaxin-3 protein secretion by ELISA, mRNA expression by PCR, STAT6 phosphorylation and nuclear translocation by Western blotting, eotaxin-3 promoter activation by an exogenous reporter construct, and STAT6, RNA polymerase II, and trimethylated H3K4 binding to the endogenous eotaxin-3 promoter by ChIP assay. Omeprazole in concentrations ≥5 µM significantly decreased IL-4-stimulated eotaxin-3 protein secretion and mRNA expression. Lansoprazole also blocked eotaxin-3 protein secretion. Omeprazole had no effect on eotaxin-3 mRNA stability or on STAT6 phosphorylation and STAT6 nuclear translocation. Rather, omeprazole blocked binding of IL-4-stimulated STAT6, RNA polymerase II, and trimethylated H3K4 to the eotaxin-3 promoter. Conclusions/Significance PPIs, in concentrations achieved in blood with conventional dosing, significantly inhibit IL-4-stimulated eotaxin-3 expression in EoE esophageal cells and block STAT6 binding to the promoter. These findings elucidate molecular mechanisms whereby patients with Th2 cytokine-driven esophageal eosinophilia can respond to PPIs, independent of effects on gastric acid secretion. PMID:23185525

  1. Effects of ischemia and omeprazole preconditioning on functional recovery of isolated rat heart

    Directory of Open Access Journals (Sweden)

    Nevena Jeremic

    2015-04-01

    Full Text Available AbstractObjective:The aim of this study was to compare protective effects of ischemic and potential protective effects of pharmacological preconditioning with omeprazole on isolated rat heart subjected to ischemia/reperfusion.Methods:The hearts of male Wistar albino rats were excised and perfused on a Langendorff apparatus. In control group (CG after stabilization period, hearts were subjected to global ischemia (perfusion was totally stopped for 20 minutes and 30 minutes of reperfusion. Hearts of group II (IPC were submitted to ischemic preconditioning lasting 5 minutes before 20 minutes of ischemia and 30 minutes of reperfusion. In third group (OPC hearts first underwent preconditioning lasting 5 minutes with 100μM omeprazole, and then submitted 20 minutes of ischemia and 30 minutes of reperfusion.Results:Administration of omeprazole before ischemia induction had protective effect on myocardium function recovery especially regarding to values of systolic left ventricular pressure and dp/dt max. Also our findings are that values of coronary flow did not change between OPC and IPC groups in last point of reperfusion.Conclusion:Based on our results it seems that ischemic preconditioning could be used as first window of protection after ischemic injury especially because all investigated parameters showed continuous trend of recovery of myocardial function. On the other hand, preconditioning with omeprazole induced sudden trend of recovery with positive myocardium protection, although less effective than results obtained with ischemic preconditioning not withstand, we must consider that omeprazole may be used in many clinical circumstances where direct coronary clamping for ischemic preconditioning is not possible.

  2. Early effects of oral administration of omeprazole and roxatidine on intragastric pH

    Institute of Scientific and Technical Information of China (English)

    Hiroshi IIDA; Masato YONEDA; Tomoko KOIDE; Hirokazu TAKAHASHI; Chikako TOKORO; Ayumu GOTO; Yasunobu ABE; Noritoshi KOBAYASHI; Kensuke KUBOTA; Eiji GOTOH; Shin MAEDA; Shingo KATO; Atsushi NAKAJIMA; Masahiko INAMORI; Yusuke SEKINO; Eiji SAKAI; Takashi UCHIYAMA; Hiroki ENDO; Kunihiro HOSONO; Yasunari SAKAMOTO; Koji FUJITA

    2012-01-01

    Objective:The ideal medication for the treatment of acid-related diseases,e.g.,peptic ulcers,stressrelated gastric bleeding,functional dyspepsia,and gastroesophageal reflux disease,should have a rapid onset of action to promote hemostasis and relieve the symptoms.The aim of our study was to investigate the inhibitory effects on gastric acid secretion of a single oral administration of a proton pump inhibitor,omeprazole 20 mg,and an H2-receptor antagonist,roxatidine 75 mg.Methods:Ten Helicobacterpylori-negative male subjects participated in this randomized,two-way crossover study.Intragastric pH was monitored continuously for 6 h after single oral administration of omeprazole 20 mg and roxatidine 75 mg.Each administration was separated by a 7-d washout period.Results:During the 6-h study period,the average pH after administration of roxatidine was higher than that after administration of omeprazole (median:4.45 vs.2.65; P=0.0367).Also during the 6-h study period,a longer duration of maintenance at pH above 2,5,and 6 was observed after administration of roxatidine 75 mg than after administration of omeprazole 20 mg (median:90.6% vs.55.2%,P=0.0284; 43.7% vs.10.6%,P=0.0125; 40.3% vs.3.3%,P=0.0125;respectively).Conclusions:In Helicobacter pylori-negative healthy male subjects,oral administration of roxatidine 75 mg increased the intragastric pH more rapidly than that of omeprazole 20 mg.

  3. [Omeprazol and ezomeprazol pharmacokinetics, duration of antisecretory effect, and reasons for their probable changes in duodenal ulcer].

    Science.gov (United States)

    Serebrova, S Iu; Starodubtsev, A K; Pisarev, V V; Kondratenko, S N; Vasilenko, G F; Dobrovol'skiĭ, O V

    2009-01-01

    There were authentic distinctions between the groups of healthy volunteers and patients with a peptic ulcer disease in Cmax, Tmax, AUC(0-t), AUC(0-infinity), CIt, Vd of omeprazole and Cmax of esomeprazole (Nexium, AstraZeneca). When the pharmacokinetics of omeprazole and ezomeprazole were compared in both groups, there were authentic distinctions in Cmax, AU(0-t), AUC(0-infinity), CIt, T1/2. The patients who had taken omeprazole the time of hypoacide condition was much shorter than in other groups. Disintegration test modeling pHmax for pH oscillation with large amplitude, that is typical for ulcer disease, demonstrated a possibility of early partial release of omeprazole, its acid-depended degradation and reduction of its bioavailability.

  4. Histopathology of the gastric oxyntic mucosa in two different patient groups during long-term treatment with omeprazole

    DEFF Research Database (Denmark)

    Hage, Esther; Hendel, Lene; Gustafsen, Jens

    2003-01-01

    OBJECTIVES: Hypochlorhydria, hypergastrinaemia, inflammation and Helicobacter pylori infection, dose and duration of omeprazole treatment may separately, or in combination, influence the proliferation of enterochromaffin-like (ECL) cells and parietal cell changes in gastric mucosa. To assess the ...... of gastric mucosal inflammation, omeprazole dose, duration of treatment and acid inhibition. The level of gastrin secretion and high plasma gastrin appear to accelerate ECL cell proliferation and parietal cell changes possibly influenced by chronic gastritis and H. pylori infection....

  5. Comparison of 24-hour intragastric pH using four liquid formulations of lansoprazole and omeprazole.

    Science.gov (United States)

    Sharma, V K

    1999-12-01

    The results of previous studies evaluating the effect of four liquid formulations of proton-pump inhibitors on 24-hour intragastric pH are described. Patients with a gastrostomy who were resident in a Veterans Affairs medical center or its affiliated nursing home were eligible for enrollment in one of four open-label studies in which each patient served as his own control. Patients underwent 24-hour intragastric pH studies before and after receiving seven consecutive days of one of the following liquid formulations of a proton-pump inhibitor administered once daily: omeprazole granules 20 mg in orange juice, lansoprazole granules 30 mg in orange juice, simplified omeprazole suspension 20 mg, and simplified lansoprazole suspension 30 mg. The suspensions were prepared with 10 mL of 8.4% sodium bicarbonate solution. Mean intragastric pH was measured, as was the time pH stayed above 3.0 and 4.0 during the 24-hour period. Six to 14 patients participated in each study. The mean posttreatment pH was 4.9+/-0.8, 4.7+/-0.6, 4.1+/-1.5, and 5.1+/-1.1 for omeprazole granules in orange juice, lansoprazole granules in orange juice, simplified omeprazole suspension, and simplified lansoprazole suspension, respectively. Both drugs in orange juice maintained pH above 4.0 longer than 14 hours and above 3.0 for close to 20 hours, which are the levels deemed optimal for healing erosive esophagitis and duodenal ulcers, respectively. Simplified lansoprazole suspension maintained pH above those thresholds for the optimal times, but simplified omeprazole suspension did not (20 and 15 hr above 3.0, 17 and 12 hr above 4.0 for lansoprazole and omeprazole, respectively). Further development of liquid formulations of proton-pump inhibitors may have important implications for the treatment of acid-related diseases in patients, including children, who are unable to swallow capsules.

  6. Effects of omeprazole and cisapride treatment in Japanese asthmatics with reflux esophagitis

    Directory of Open Access Journals (Sweden)

    Katsuya Fujimori

    1997-01-01

    Full Text Available In the United States and Europe, gastroesophageal reflux (GER is receiving attention as a potential cause of bronchial asthma. Few Japanese case reports have described this relationship. Therefore, we investigated the effect of omeprazole and cisapride on pulmonary function tests, blood gases and home peak expiratory flow rates (PEFR in six Japanese outpatients with asthma and proven GER. After 8 weeks of treatment, reflux esophagitis had improved in all patients. However, the parameters of pulmonary function showed no change other than a significant post- treatment increase in home PEFR (4.4-27.7% in three patients. These results suggest that anti-reflux (omeprazole and cisapride treatment will produce small improvements in the PEFR in some Japanese asthmatics with GER.

  7. The effect of immobilization stress on the pharmacokinetics of omeprazole in rats.

    Directory of Open Access Journals (Sweden)

    Watanabe K

    2002-02-01

    Full Text Available The effects of immobilization stress on the pharmacokinetics of omeprazole were studied in rats. The immobilization stress for 30 or 60 min immediately after oral administration of the drug caused an increase in the time to reach the maximum concentration. However, such stress did not alter the area under the plasma concentration-time curve (AUC. When administered intravenously, the half-life during the elimination phase was significantly prolonged by 30 min of immobilization stress, but the AUC value remained unchanged. The intestinal propulsive activity was significantly decreased by immobilization stress. These findings suggest that immobilization stress reduces gastrointestinal motility. A resulting delay during the absorption phase of omeprazole occurs, although the degree of influence on overall pharmacokinetics is relatively insignificant.

  8. Review of immediate-release omeprazole for the treatment of gastric acid-related disorders.

    Science.gov (United States)

    Castell, Donald

    2005-11-01

    Immediate-release omeprazole (Zegerid, Santarus) is the first immediate-release oral proton pump inhibitor to reach the market. As a powder formulation for oral suspension, it is indicated for the treatment of gastroesophageal reflux disease, erosive oesophagitis, duodenal ulcer and gastric ulcer, and is the only proton pump inhibitor approved for the reduction of risk of upper gastrointestinal bleeding in critically ill patients. Administration of immediate-release omeprazole at bedtime results in a rapid and sustained elevation of gastric pH, and seems to provide better night time control of gastric acidity than that observed with conventional morning dosing of delayed-release proton pump inhibitors. The immediate-release formulation may provide a good treatment option for patients who require flexible dosing, quick onset of action and nocturnal gastric acid control.

  9. Comparison of omeprazole with cimetidine for prophylaxis of acid aspiration in elective surgery.

    Science.gov (United States)

    Bouly, A; Nathan, N; Feiss, P

    1993-05-01

    Gastric pH and volume were measured in four groups of 15 patients scheduled for elective surgery. The patients were randomly allocated to receive either no antacid, oral omeprazole 40 mg the evening before surgery, oral omeprazole 40 mg 2 h before surgery, or effervescent cimetidine 800 mg, 2 h before surgery. Anaesthesia was induced with thiopentone (4-6 mg kg-1), fentanyl (0.03 mg kg-1) and vecuronium (0.1 mg kg-1) and maintained with nitrous oxide in oxygen (50/50) and isoflurane. After induction of anaesthesia and on completion of surgery, gastric pH (mean +/- SEM) and volume were measured using a glass electrode and a phenol red dilution technique. Gastric pH were significantly higher in the three treated groups than in control (P 25 ml).

  10. Omeprazole and lansoprazole enantiomers induce CYP3A4 in human hepatocytes and cell lines via glucocorticoid receptor and pregnane X receptor axis.

    Science.gov (United States)

    Novotna, Aneta; Dvorak, Zdenek

    2014-01-01

    Benzimidazole drugs lansoprazole and omeprazole are used for treatment of various gastrointestinal pathologies. Both compounds cause drug-drug interactions because they activate aryl hydrocarbon receptor and induce CYP1A genes. In the current paper, we examined the effects of lansoprazole and omeprazole enantiomers on the expression of key drug-metabolizing enzyme CYP3A4 in human hepatocytes and human cancer cell lines. Lansoprazole enantiomers, but not omeprazole, were equipotent inducers of CYP3A4 mRNA in HepG2 cells. All forms (S-, R-, rac-) of lansoprazole and omeprazole induced CYP3A4 mRNA and protein in human hepatocytes. The quantitative profiles of CYP3A4 induction by individual forms of lansoprazole and omeprazole exerted enantiospecific patterns. Lansoprazole dose-dependently activated pregnane X receptor PXR in gene reporter assays, and slightly modulated rifampicin-inducible PXR activity, with similar potency for each enantiomer. Omeprazole dose-dependently activated PXR and inhibited rifampicin-inducible PXR activity. The effects of S-omeprazole were much stronger as compared to those of R-omeprazole. All forms of lansoprazole, but not omeprazole, slightly activated glucocorticoid receptor and augmented dexamethasone-induced GR transcriptional activity. Omeprazole and lansoprazole influenced basal and ligand inducible expression of tyrosine aminotransferase, a GR-target gene, in HepG2 cells and human hepatocytes. Overall, we demonstrate here that omeprazole and lansoprazole enantiomers induce CYP3A4 in HepG2 cells and human hepatocytes. The induction comprises differential interactions of omeprazole and lansoprazole with transcriptional regulators PXR and GR, and some of the effects were enantiospecific. The data presented here might be of toxicological and clinical importance, since the effects occurred in therapeutically relevant concentrations.

  11. The effects of omeprazole on interdigestive motility and early postprandial levels of gastrin and secretin

    DEFF Research Database (Denmark)

    Rasmussen, L; Oster-Jørgensen, E; Qvist, N

    1992-01-01

    Ten healthy men participated in a crossover study, and the experiments took place after 10 days of treatment (40 mg omeprazole every morning). Blood samples were drawn at fixed intervals during a complete migrating motor complex (MMC) cycle. The manometric pressure tube was removed after passage ...... plasma gastrin, ii) a decrease in secretin in phases I and III, iii) an augmented meal-stimulated gastrin response, and iv) a secretin response characterized by a significantly lower mean in the immediate postprandial period....

  12. Early effects of oral administration of omeprazole and roxatidine on intragastric pH

    OpenAIRE

    2012-01-01

    Objective: The ideal medication for the treatment of acid-related diseases, e.g., peptic ulcers, stress-related gastric bleeding, functional dyspepsia, and gastroesophageal reflux disease, should have a rapid onset of action to promote hemostasis and relieve the symptoms. The aim of our study was to investigate the inhibitory effects on gastric acid secretion of a single oral administration of a proton pump inhibitor, omeprazole 20 mg, and an H2-receptor antagonist, roxatidine 75 mg. Methods:...

  13. Buspirone, fexofenadine, and omeprazole: quantification of probe drugs and their metabolites in human plasma.

    Science.gov (United States)

    Gor, Parul; Alnouti, Yazen; Reed, Gregory A

    2011-07-15

    Probe drugs are critical tools for the measurement of drug metabolism and transport activities in human subjects. Often several probe drugs are administered simultaneously in a "cocktail". This cocktail approach requires efficient analytical methods for the simultaneous quantitation of multiple analytes. We have developed and validated a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of three probe drugs and their metabolites in human plasma. The analytes include omeprazole and its metabolites omeprazole sulfone and 5'-hydroxyomeprazole; buspirone and its metabolite 1-[2-pyrimidyl]-piperazine (1PP); and fexofenadine. These analytes and the internal standard lansoprazole were extracted from plasma using protein precipitation with acetonitrile. Gradient reverse-phase chromatography was performed with 7.5mM ammonium bicarbonate and acetonitrile, and the analytes were quantified in positive ion electrospray mode with multiple reaction monitoring. The method was validated to quantify the concentration ranges of 1.0-1000ng/ml for omeprazole, omeprazole sulfone, 5'-hydroxyomeprazole, and fexofenadine; 0.1-100ng/ml for buspirone, and 1.0-100ng/ml for 1PP. These linear ranges span the plasma concentrations for all of the analytes from probe drug studies. The intra-day precision was between 2.1 and 16.1%, and the accuracy ranged from 86 to 115% for all analytes. Inter-day precision and accuracy ranged from 0.3 to 14% and from 90 to 110%, respectively. The lower limits of quantification were 0.1ng/ml for buspirone and 1ng/ml for all other analytes. This method provides a fast, sensitive, and selective analytical tool for quantification of the six analytes in plasma necessary to support the use of this probe drug cocktail in clinical studies.

  14. Effect of omeprazole on symptoms and ultrastructural esophageal damage in acid bile reflux

    Institute of Scientific and Technical Information of China (English)

    Carlo Calabrese; Anna Fabbri; Mauro Bortolotti; Giovanna Cenacchi; Scialpi Carlo; Desiree Zahlane; Mario Miglioli; Giulio Di Febo

    2005-01-01

    AIM: To value whether omeprazole could induce the healing of DIS and regression of symptoms in patients with DGER.METHODS: We enrolled 15 symptomatic patients with a pathological esophageal 24-h pH-metry and bilimetry.Patients underwent endoscopy and biopsies were taken from the distal esophagus. Specimens were analyzed at histology and transmission electron microscopy (TEM).Patients were treated with omeprazole 40 mg/d for 3 mo and then endoscopy with biopsies was repeated. Patients with persistent heartburn and/or with an incomplete recovery of DIS were treated for 3 more months and endoscopy with biopsies was performed.RESULTS: Nine patients had a non-erosive reflux disease at endoscopy (NERD) while 6 had erosive esophagitis (ERD). At histology, of the 6 patients with erosive esophagus,5 had mild esophagitis and 1 moderate esophagitis. No patients with NERD showed histological signs of esophagitis.After 3 mo of therapy, 13/15 patients (86.7%, P<0.01)showed a complete recovery of DIS and disappearance of heartburn. Of the 2 patients treated for 3 more months,complete recovery of DIS and heartburn were achieved in one.CONCLUSION: Three or 6 mo of omeprazole therapy led to a complete regression of the ultrastructural esophageal damage in 86.7% and in 93% of patients with DGER, NERD and ERD respectively. The ultrastructural recovery of the epithelium was accompanied by regression of heartburn in all cases.

  15. Ultra-fast gradient LC method for omeprazole analysis using a monolithic column: assay development, validation, and application to the quality control of omeprazole enteric-coated pellets.

    Science.gov (United States)

    Borges, Keyller Bastos; Sánchez, Antonio José Macías; Pupo, Mônica Tallarico; Bonato, Pierina Sueli; Collado, Isidro González

    2010-01-01

    A method was optimized for the analysis of omeprazole (OMZ) by ultra-high speed LC with diode array detection using a monolithic Chromolith Fast Gradient RP 18 endcapped column (50 x 2.0 mm id). The analyses were performed at 30 degrees C using a mobile phase consisting of 0.15% (v/v) trifluoroacetic acid (TFA) in water (solvent A) and 0.15% (v/v) TFA in acetonitrile (solvent B) under a linear gradient of 5 to 90% B in 1 min at a flow rate of 1.0 mL/min and detection at 220 nm. Under these conditions, OMZ retention time was approximately 0.74 min. Validation parameters, such as selectivity, linearity, precision, accuracy, and robustness, showed results within the acceptable criteria. The method developed was successfully applied to OMZ enteric-coated pellets, showing that this assay can be used in the pharmaceutical industry for routine QC analysis. Moreover, the analytical conditions established allow for the simultaneous analysis of OMZ metabolites, 5-hydroxyomeprazole and omeprazole sulfone, in the same run, showing that this method can be extended to other matrixes with adequate procedures for sample preparation.

  16. Inhibition of gastric perception of mild distention by omeprazole in volunteers

    Institute of Scientific and Technical Information of China (English)

    Akihito Iida; Hiroshi Kaneko; Toshihiro Konagaya; Yasushi Funaki; Kentaro Tokudome; Shinya Izawa; Yasuhiro Tamura

    2012-01-01

    To evaluate the effects of omeprazole on gastric mechanosensitivity in humans.METHODS:A double lumen polyvinyl tube with a plastic bag was introduced into the stomach of healthy volunteers under fluorography and connected to a barostat device.Subjects were then positioned so they were sitting comfortably,and the minimal distending pressure (MDP) was determined after a 30-min adaptation period.Isobaric distensions were performed in stepwise increments of 2 mmHg (2 min each) starting from the MDP.Subjects were instructed to score feelings at the end of every step using a graphic rating scale:0,no perception; 1,weak/vague; 2,weak but significant; 3,moderate/vague; 4,moderate but significant; 5,severe discomfort; and 6,unbearable pain.After this first test,subjects received omeprazole (20 mg,after dinner) once daily for 1 wk.A second test was performed on the last day of treatment.RESULTS:No adverse effects were observed.Mean MDP before and after treatment was 6.3 ± 0.3 mmHg and 6.2 ± 0.5 mmHg,respectively.One subject before and 2 after treatment did not reach a score of 6 at the maximum bag volume of 750 mL.After omeprazole,there was a significant increase in the distension pressure required to reach scores of 1 (P =0.019) and 2(P =0.017) as compared to baseline.There were no changes in pressure required to reach the other scores after treatment.Two subjects before and one after omeprazole rated their abdominal feeling < 1 at MDP,and mean (± SE) abdominal discomfort scores at MDP were 0.13 ±± 0.09 and 0.04 ±± 0.04,respectively.Mean scores induced by each MDP + 2,4,6,8,10,12,14,16,18 and 20 (mmHg) were 1.1 ± 0.3,2.0 ± 0.4,2.9± 0.5,3.3 ± 0.4,4.6 ± 0.3,5.2 ± 0.3,5.5 ± 0.2,5.5± 0.3,5.7 ± 0.3,and 5.4,respectively.After omeprazole,abdominal feeling scores for the same incremental pressures over MDP were 0.3 ± 0.1,0.8 ± 0.1,2.0±-0.4,2.8-0.4,3.8 ±± 0.4,4.6 ±± 0.4,4.9 ± 0.3,5.4± 0.4,5.2 ±± 0.6,and 5.0 ±± 1.0,respectively.A significant decrease in

  17. Comparison of Omeprazole with Ranitidine for Treatment of Symptoms Associated with Gastroesophageal Reflux Disease and Uncomplicated Duodenal Ulcer

    Directory of Open Access Journals (Sweden)

    Andre P Archambault

    1996-01-01

    Full Text Available This randomized, single-blind, parallel group study was conducted to compare omeprazole with ranitidine for the treatment of symptoms associated with gastroesophageal reflux disease (GERD, uncomplicated duodenal ulcer (DU or both. After baseline assessments, patients were randomized to receive daily treatment with either 20 mg omeprazole or 300 mg ranitidine for four weeks. In total, 1481 patients (1001 omeprazole, 480 ranitidine with a diagnosis of GERD (n=904 and/or DU (n=577, confirmed by endoscopy or barium meal and reporting moderate to severe symptoms, were included in the analyses. The seventy of overall daytime symptoms reported by the omeprazole group at clinic visits was lower than that reported by the ranitidine group at week 2 for the entire patient group (P=0.0002 and at both weeks 2 and 4 for the subgroup of patients with GERD (P=0.0001 and P=0.001, respectively. The severity of overall night-time symptoms reported by the omeprazole group was lower than that reported by the ranitidine group at week 4 for all patients as a whole (P=0.042 and at both weeks 2 and 4 for the subgroup of patients with GERD (P=0.035 and P=0.010, respectively. There were no significant differences in reports of adverse events. In the omeprazole group, 19% of patients at week 2 and 15% of patients at week 4 reported adverse events, while the corresponding results from the ranitidine group were 21% and 11%. In conclusion, patients with GERD, DU or both treated with omeprazole 20 mg daily for four weeks showed statistically significant reductions in symptoms compared with patients treated with ranitidine 300 mg daily for the same period of time. The percentage of patients with any remaining daytime symptoms was 12% lower in the omeprazole group compared with the ranitidine group at week 2, and 7% lower at week 4. Five per cent fewer patients in the omeprazole group experienced night-time symptoms at either week 2 or week 4.

  18. Omeprazole affects clopidogrel efficacy but not ischemic events in patients with acute coronary syndrome undergoing elective percutaneous coronary intervention

    Institute of Scientific and Technical Information of China (English)

    REN Yi-hong; GUO Yu-song; XIE Yong-jin; WANG Chun-ya; ZHAO Ming; CHEN Yun-dai; CHEN Lian; LIU Hong-bin; WANG Yu; SUN Zhi-jun; CHEN Jin-song; HUANG Ting-ting

    2011-01-01

    Background Omeprazole, usually used in the antiplatelet therapy during percutaneous coronary intervention (PCI) in acute coronary syndrome (ACS), has been reported to increase ischemic events in retrospective studies. However, other clinical trials gave paradoxical results. The aim of this study was to assess the effects of omeprazole on clopidogrel efficacy and clinical events.Methods All patients (n=172) received aspirin (loading dose 300 mg and maintenance dose 100 mg/d) and clopidogrel (loading dose 600 mg and maintenance dose 75 mg/d) during the therapy. They were randomized to receive omeprazole (20 mg/d) or placebo for 30 days. Residual platelet activities in the adenosine 5'-diphosphate (ADP) pathway were detected on the fifth day after PCI with thrombelastography (TEG)-mapping. The clinical events were recorded after one month.Results According to the five levels of platelet activities, the frequency distributions of the inhibition rates were significantly different (P=0.0062). However, no significant change was seen in the distribution among the highest or the lowest inhibiting levels (>95% and <30% inhibition rate). And there were no significant differences (P >0.05) in events incidence, while gastra-intesternal bleeding decreased in co-administration of omeprazole.Conclusions Omeprazole significantly blunts clopidogreal efficacy while not exacerbates ischimic events in ACS undergoing PCI. Omeprazaole even can decrease gastra-intestinal bleeding in those patients.

  19. Using omeprazole to link the components of the post-prandial alkaline tide in the spiny dogfish, Squalus acanthias.

    Science.gov (United States)

    Wood, Chris M; Schultz, Aaron G; Munger, R Stephen; Walsh, Patrick J

    2009-03-01

    After a meal, dogfish exhibit a metabolic alkalosis in the bloodstream and a marked excretion of basic equivalents across the gills to the external seawater. We used the H(+), K(+)-ATPase pump inhibitor omeprazole to determine whether these post-prandial alkaline tide events were linked to secretion of H(+) (accompanied by Cl(-)) in the stomach. Sharks were fitted with indwelling stomach tubes for pretreatment with omeprazole (five doses of 5 mg omeprazole per kilogram over 48 h) or comparable volumes of vehicle (saline containing 2% DMSO) and for sampling of gastric chyme. Fish were then fed an involuntary meal by means of the stomach tube consisting of minced flatfish muscle (2% of body mass) suspended in saline (4% of body mass total volume). Omeprazole pre-treatment delayed the post-prandial acidification of the gastric chyme, slowed the rise in Cl(-) concentration of the chyme and altered the patterns of other ions, indicating inhibition of H(+) and accompanying Cl(-) secretion. Omeprazole also greatly attenuated the rise in arterial pH and bicarbonate concentrations and reduced the net excretion of basic equivalents to the water by 56% over 48 h. Arterial blood CO(2) pressure (Pa(CO(2))) and plasma ions were not substantially altered. These results indicate that elevated gastric H(+) secretion (as HCl) in the digestive process is the major cause of the systemic metabolic alkalosis and the accompanying rise in base excretion across the gills that constitute the alkaline tide in the dogfish.

  20. Prescripción, dispensación y sustitución de recetas de omeprazol Prescription, dispensation and sustitution of prescription forms of omeprazole

    Directory of Open Access Journals (Sweden)

    M. B. Vaquero

    2003-07-01

    Full Text Available Objetivo: Comprobar y cuantificar, para un principio activo concreto (omeprazol 20 mg, y para unos médicos de atención primaria y oficinas de farmacia seleccionados, si las especialidades farmacéuticas prescritas en recetas oficiales de la Seguridad Social coinciden o no con las especialidades farmacéuticas dispensadas, o bien la dispensación se ha efectuado a criterio del farmacéutico al ir la receta prescrita en denominación oficial española (DOE, calculando el coste de las recetas en cada supuesto, expresado en DDD. Método: Revisión de 592 recetas oficiales de la Seguridad Social de un principio activo seleccionado (omeprazol 20 mg, prescritas por 56 médicos de atención primaria con alta prescripción de este principio activo, y dispensadas en 16 oficinas de farmacia. Resultados: Las recetas en que se respetó la prescripción del médico (50% de los casos resultaron ser más baratas que las prescritas en DOE y dispensadas EFG por el farmacéutico a su criterio (36% de los casos. En el supuesto de recetas en las que se produjeron sustituciones de la especialidad prescrita (14% de los casos, se dispensó en todos los casos una EFG y en el 76% fue de especialidades más caras. Conclusiones: Los resultados demuestran que el médico prescriptor valora el coste de la especialidad farmacéutica a la hora de prescribir y se decanta por especialidades más baratas aunque no sean EFG. El farmacéutico, cuando dispensa a su criterio o sustituye la especialidad prescrita, lo hace siempre por una EFG que en la mayoría de los casos resultó ser más cara.Objective: To verify and quantify, for a given active principle (omeprazole 20 mg and for selected primary care physicians and pharmacies, the extent to which the drug prescribed on official national health system prescription forms coincides with the drug dispensed or whether the drug was dispensed following the pharmacist's criteria because the prescription was drafted in terms of the

  1. Gastric bicarbonate secretion, acid secretion, and mucosal blood flow during influence of pentagastrin and omeprazole in the cat.

    Science.gov (United States)

    Guttu, K; Røsok, B; Gislason, H; Fändriks, L; Svanes, K; Grønbech, J E

    1991-04-01

    In this study secretion of bicarbonate and acid and mucosal blood flow were determined simultaneously in cats. The gastric lumen of anesthetized cats was continuously perfused with isotonic saline. Secretion of HCO-3 and H+ was calculated from continuous measurements of pH and PCO2 in the perfusate. Mucosal blood was measured by means of radiolabeled microspheres. Under resting acid secretory conditions, bicarbonate secretion into the gastric lumen averaged 1.0 mumol/min. Somewhat surprising, both omeprazole (4 mg/kg as bolus) and pentagastrin (16 micrograms/kg.h intravenously) significantly reduced the HCO-3 secretion. Omeprazole did not influence mucosal blood flow, whereas corpus mucosal blood flow increased during pentagastrin stimulation. Under resting acid secretory conditions and during omeprazole treatment there was a close linear relationship between acid and bicarbonate secretion. No such relationship was found during pentagastrin stimulation of the mucosa. No consistent relationship was obtained between blood flow and bicarbonate secretion in normal gastric mucosa.

  2. Residual solvent determination by head space gas chromatography with flame ionization detector in omeprazole API

    Directory of Open Access Journals (Sweden)

    Saurabh Pandey

    2011-06-01

    Full Text Available Residual solvents in pharmaceutical samples are monitored using gas chromatography with head space. Based on good manufacturing practices, measuring residual solvents is mandatory for the release testing of all active pharmaceutical ingredients (API. The analysis of residual organic solvents (methanol, acetone, cyclohexane, dichloromethane, toluene in Omeprazole, an active pharmaceutical ingredient was investigated. Omeprazole is a potent reversible inhibitor of the gastric proton pump H+/K+-ATPase. The Head space gas chromatography (HSGC method described in this investigation utilized a SPB TM-624, Supelco, 30 m long x 0.25 mm internal diameter, 1.4µm-thick column. Since Omeprazole is a thermally labile compound, the selection of the proper injector temperature is critical to the success of the analysis. The injector temperature was set at 170ºC to prevent degradation. The initial oven temperature was set at 40ºC for 12 min and programmed at a rate of 10ºC min-1 to a final temperature of 220ºC for 5 min. Nitrogen was used as a carrier gas. The sample solvent selected was N,N-dimethylacetamide. The method was validated to be specific, linear, precise, sensitive, rugged and showed excellent recovery.Solventes residuais em amostras farmacêuticas são monitoradas utilizando-se cromatografia a gás "headspace". Com base nas boas práticas de fabricação, a medida de solventes residuais é obrigatória para o teste de liberação de todos os ingredientes farmacêuticos (API. Efetuou-se a análise de solventes orgânicos residuais (metanol, acetona, cicloexano, diclorometano, tolueno em omeprazol, ingrediente farmacêutico ativo. O omeprazol é potente inibidor reversível da bomba de prótons H+/K+-ATPase. A cromatografia a gás "headspace" (HSGC descrita nessa pesquisa utilizou um SPB TM-624, Supelco, de 30 m de comprimento x 0,25 mm de diâmetro interno, e coluna de 1,4 µm de espessura. Considerando-se que o omeprazol é termicamente l

  3. A double-blind placebo-controlled study on the effects of omeprazole on gut hormone secretion and gastric emptying rate

    DEFF Research Database (Denmark)

    Rasmussen, L; Qvist, N; Oster-Jørgensen, E;

    1997-01-01

    BACKGROUND: The present study was designed to investigate whether an effect of omeprazole on gastric emptying is related to changes in the secretion of selected gut hormones. METHODS: The studies were performed in healthy men after 10 days' treatment with 40 mg omeprazole daily/placebo. Food...... ingestion took place in a duodenal phase, I and the meal consisted of an omelette labelled with technetium Tc 99m, followed by 150 ml water labelled with indium In 111. Plasma concentrations of gastrin, cholecystokinin (CCK), and motilin were measured. RESULTS: Pretreatment with omeprazole reduced gastric...... emptying rates. This applied to all variables and was most pronounced with regard to amounts of solid (median (95% confidence interval)) emptied at 180 min (71% (48 - 86) for omeprazole versus 96% (87 - 100) for placebo; P omeprazole...

  4. Suboptimal response to ferrous sulfate in iron-deficient patients taking omeprazole.

    Science.gov (United States)

    Ajmera, Akash V; Shastri, Ghanshyam S; Gajera, Mithil J; Judge, Thomas A

    2012-05-01

    Iron deficiency anemia is commonly encountered in outpatient practice. Gastric acid is one of the important factors for optimum absorption of iron. Proton pump inhibitors are very commonly prescribed medications. One of the debated effects of proton pump inhibitors is on oral iron absorption. Their effect on absorption of oral iron supplementation in iron-deficient patients has not been studied. At the Cooper Hematology Outpatient office, we reviewed charts of iron-deficient anemic patients who were on omeprazole for the last 4 years. Fifty patients having no apparent ongoing blood loss, having other causes of anemia especially that of chronic diseases ruled out, and on omeprazole while starting ferrous sulfate therapy for iron deficiency were selected for chart review. The iron-study results at the start of oral ferrous sulfate therapy and at 3 months follow-up were compared to evaluate the response of ferrous sulfate. The mean hemoglobin change was 0.8 ± 1.2 g/L. The mean change in ferrtin values was 10.2 ± 7.8 μg/L. Only 16% of the patients had a normal response to hemoglobin levels (rise of >2 g/dL), and only 40% had a normal response to ferritin levels (rise of >20 μg/dL). The average age of patients having a suboptimal response to both hemoglobin and ferritin was significantly higher compared with that of the patients with an optimal response. Omeprazole and possibly all proton pump inhibitors decrease the absorption of oral iron supplementation. Iron-deficient patients taking proton pump inhibitors may have to be treated with high dose iron therapy for a longer duration or with intravenous iron therapy.

  5. Differential effects of omeprazole and lansoprazole enantiomers on aryl hydrocarbon receptor in human hepatocytes and cell lines.

    Science.gov (United States)

    Novotna, Aneta; Srovnalova, Alzbeta; Svecarova, Michaela; Korhonova, Martina; Bartonkova, Iveta; Dvorak, Zdenek

    2014-01-01

    Proton pump inhibitors omeprazole and lansoprazole contain chiral sulfur atom and they are administered as a racemate, i.e. equimolar mixture of S- and R-enantiomers. The enantiopure drugs esomeprazole and dexlansoprazole have been developed and introduced to clinical practice due to their improved clinical and therapeutic properties. Since omeprazole and lansoprazole are activators of aryl hydrocarbon receptor (AhR) and inducers of CYP1A genes, we examined their enantiospecific effects on AhR-CYP1A pathway in human cancer cells and primary human hepatocytes. We performed gene reporter assays for transcriptional activity of AhR, RT-PCR analyses for CYP1A1/2 mRNAs, western blots for CYP1A1/2 proteins and EROD assay for CYP1A1/2 catalytic activity. Lansoprazole and omeprazole enantiomers displayed differential effects on AhR-CYP1A1/2 pathway. In general, S-enantiomers were stronger activators of AhR and inducers of CYP1A genes as compared to R-enantiomers in lower concentrations, i.e. 1-10 µM for lansoprazole and 10-100 µM for omeprazole. In contrast, R-enantiomers were stronger AhR activators and CYP1A inducers than S-enantiomers in higher concentrations, i.e. 100 µM for lansoprazole and 250 µM for omeprazole. In conclusion, we provide the first evidence of enantiospecific effects of omeprazole and lansoprazole on AhR signaling pathway.

  6. Influence of omeprazole on pharmacokinetics of domperidone given as free base and maleate salt in healthy Chinese patients

    Institute of Scientific and Technical Information of China (English)

    Yi-fan ZHANG; Xiao-yan CHEN; Xiao-jian DAI; Yi-ni ZHANG; Qi-zhi LIU; Hua-ling YU; Da-fang ZHONG

    2007-01-01

    Aim: To investigate the influence of omeprazole on the pharmacokinetics of domperidone given as free base and maleate salt. Methods: An open, randomized, 2-period crossover study with a washout period of 7 d was conducted in 10 healthy Chinese, male patients. In each study period, the patients were adminis-tered a single oral dose of l0 mg domperidone as free base or maleate salt on d 1,20 mg omeprazole twice daily on d 2 and 3, and once on d 4. A single dose of 10 mg domperidone as free base or maleate salt was taken at 4 h after administration of omeprazole on d 4. Plasma samples were collected on d 1 and 4 after the adminis- tration of domperidone, and the plasma concentrations of domperidone were de- termined by a sensitive liquid chromatography-tandem mass spectrometry method.Results: For free-base domperidone, pretreatment with omeprazole resulted in a 16% decrease in maximum concentration (Cmax), compared with administration alone (P<0.05). However, for maleate salt, with the exception of an increase in t1/2,no pharmacokinetic parameters were significantly changed. When the free base and maleate salt were administered alone, no differences were found in any param-eters between the 2 formulations. In contrast, when they were administered in the presence of omeprazole, the Cmax of domperidone given as free base was lower (25.9%) than that given as maleate salt (P<0.05). Conclusion: Pretreatment of omeprazole does not affect the absorption of domperidone maleate, but leads to a moderately decreased rate of absorption of the free base.

  7. Incompatibility of omeprazole sodium for injection%注射用奥美拉唑钠的配伍禁忌

    Institute of Scientific and Technical Information of China (English)

    王诗鸿; 王秀中; 解放军第

    2012-01-01

    aObjective To investigate the incompatibility of omeprazole sodium for injection. Methods Domestic literatures of omeprazole sodium for injection in recent years were summarized and analyzed. Results Omeprazole sodium for injection was incompatible with many drugs. Adding other drugs into omeprazole sodium for injection could result in the change of the external appearance of solution. The pH value, temperature and light could affect the stability of omeprazole sodium for injection. Conclusion Omeprazole sodium for injection is incompatible with many drugs. It should be added into 0. 9% NS in clinical infusion,and the infusion should be finished within 4 h.%目的 了解注射用奥美拉唑钠的配伍禁忌.方法 收集国内公开发表的注射用奥美拉唑钠的相关文献,并进行归纳分析.结果 注射用奥美拉唑钠与多种药物配伍后,会出现溶液变色、混浊、沉淀等现象.溶液的pH值、温度、光线等会对奥美拉唑钠溶液的稳定性产生影响.结论 奥美拉唑钠与多种药物存在配伍禁忌,应避免联合使用.临床应用时建议首选0.9%氯化钠注射液稀释,并在4 h内滴注完毕.

  8. Neutron activation analysis of chemical impurities in manipulated samples of omeprazole

    Energy Technology Data Exchange (ETDEWEB)

    Sepe, Fernanda Peixoto; Leal, Alexandre Soares; Gomes, Tatiana Cristina Bomfim; Menezes, Maria Angela de Barros Correia; Silva, Maria Aparecida, E-mail: asleal@cdtn.br [Nuclear Technology Development Centre/Brazilian Commission for Nuclear Energy (CDTN/CNEN-MG), Belo Horizonte, MG (Brazil)

    2011-07-01

    In this work, samples of Omeprazole (C{sub 17}H{sub 19}N{sub 3}O{sub 3}S), a largely used drug in the treatment of dyspepsia and peptic ulcer, were acquired from five different pharmacies of manipulation - or retail pharmacies which prepare personalized drugs under medical recommendation - in Belo Horizonte/Brazil and investigated using the k{sub 0} - Neutron Activation Analysis (NAA). The preliminary results showed the presence of elements not foreseen in the original formula. It confirms the potential risk offered by medicines without suitable inspection. (author)

  9. Triple therapy with clarithromycin, amoxicillin and omeprazole for Helicobacter pylori eradication in children and adolescents

    Directory of Open Access Journals (Sweden)

    KAWAKAMI Elisabete

    2001-01-01

    Full Text Available Background - Helicobacter pylori infection presents high prevalence in developing countries, but there are few pediatric assays evaluating antimicrobial treatment. Objective - The aim of this study was to investigate Helicobacter pylori eradication rate using a short regimen (7 and 10 days of triple therapy with clarithromycin, amoxicillin and omeprazole. Patients and methods - Twenty-five Hp positive patients who presented severe epigastralgia, were submitted to antimicrobial treatment with amoxicillin (50 mg/kg/day - maximum dose 1g bid, clarithromycin (30 mg/kg/day - maximum dose 500 mg bid and omeprazole (0.6 mg/kg/day - maximum dose 20 mg bid during 7 or 10 days. After 2 months, clinical symptoms were evaluated and gastric biopsies were taken to test Hp eradication. Results - Overall eradication rate was achieved in 16/25 patients (64% - IC(95% = 45-83%, in 11/15 (73% - IC(95% = 51-95% patients who used 10 days therapy course and in 5/10 (50% - IC(95% = 19-81% who used 7 days therapy course. Eradication drugs were well accepted and adverse effects were reported in two patients (8%. Conclusions - This triple therapy regimen had moderate efficacy (64%. The data suggests that 10 days therapy course achieves better eradication rate (73% than 7 days course (50% to treat Hp infection in our population.

  10. FIRST-ROW TRANSITION METAL COMPLEXES OF OMEPRAZOLE AS ANTI-ULCERATIVE DRUGS

    Directory of Open Access Journals (Sweden)

    Suman Malik

    2010-12-01

    Full Text Available Omeprazole (OME is a proton pump inhibitor (PPI. PPIs have enabled to improve the treatment of various acid-peptic disorders. OME is a weak base and it can form several complexes with transition and non-transition metal ions. In the present paper, we are describing series of transition metal complexes of omeprazole i.e., 5-methoxy-2[(4methoxy-3, 5dimethyl-2-pyridinyl methylsulfinyl]-1H-benzimidazole with CuII, MnII, CoII, NiII, FeII, ZnII and HgII. These complexes were characterized by elemental analysis, molar conductivity, IR, NMR, magnetic susceptibility, UV-visible spectral studies, ESR, SEM and X-ray diffraction. Based on the above studies, the ligand behaves as bidentate O, N donor and forms coordinate bonds through C=N and S=O groups. The complexes were found to non-electrolytic in nature on the basis of low values of molar conductivity. Analytical data and stoichiometry analysis suggest ligand to metal ratio of 2:1 for all the complexes. Electronic spectra and magnetic susceptibility measurements reveal octahedral geometry for Mn(II,Co(II, Ni(II,Fe(II and Cu(II complexes and tetrahedral for Hg(II and Zn(II complexes. Ligands and their metal complexes have been screened for their antibacterial and antifungal activities against bacteria Pseudomonas, Staphylococcus aureus and fungi Aspergillus niger and A. flavous.

  11. Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity.

    Science.gov (United States)

    El-Nezhawy, Ahmed O H; Biuomy, Ayman R; Hassan, Fatma S; Ismaiel, Ayman K; Omar, Hany A

    2013-04-01

    A new series of novel benzimidazole derivatives containing substituted pyrid-2-yl moiety and polyhydroxy sugar conjugated to the N-benzimidazole moiety has been synthesized and evaluated as orally bioavailable anti-inflammatory agents with anti-ulcerogenic activity. The anti-inflammatory and anti-ulcerogenic activities of these compounds were compared to diclofenac and omeprazole, respectively. In carrageenan-induced paw oedema assay, 2-methyl-N-((3,4-dimethoxypyridin-2-yl)methyl)-1H-benzimidazol-5-amine (12d) and 1-(1,2,3,5-tetrahydroxy-α-D-mannofuranose)-5-(((3,4-dimethoxypyridin-2yl)methyl)amino)-2-methyl-1H-benzimidazole (15d) displayed dose-dependent anti-inflammatory activities by decreasing the inflammation by 62% and 72%, respectively which is comparable to that of diclofenac (73%). In contrast to diclofenac, the anti-inflammatory activity of these compounds was not only free from any side effects on the gastric mucosa but also showed significant anti-ulcerogenic activity in rat pyloric ligation and ethanol-induced gastric ulcer models similar to that of omeprazole. Together, these findings suggest that 12d and 15d are potent anti-inflammatory agents with concurrent anti-ulcerogenic activity and support its clinical promise as a component of therapeutic strategies for inflammation, for which the gastric side effects are always a major limitation.

  12. Formulation and In-Vitro Evaluation of Chitosan Based Omeprazole Mucoadhesive Buccal Tablets

    Directory of Open Access Journals (Sweden)

    Amit E. Birari

    2014-10-01

    Full Text Available The present study is concerned with formulation and evaluation of mucoadhesive buccal tablets containing proton pump inhibitors drug, Omeprazole to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. The tablets were prepared by direct compression method. Nine formulations were prepared with Chitosan as primary polymer and Carbopol 934, Hydroxy Propyl Methyl Cellulose (HPMC K4M and Xanthan gum as a secondary polymer. All formulations were evaluated for weight variation, hardness, surface pH, drug Content uniformity, swelling index, and bioadhesive strength and in-vitro drug dissolution study. Physical compatibility studies showed no evidence on interactions between drug, polymers, and excipients. The in vitro release of Omeprazole was performed under sink conditions (Phosphate buffer PH 6.8, 37±0.5ºC, rpm 50 using USP dissolution apparatus type II. The best in-vitro drug release profile was achieved with the formulation F8 which contains the Chitosan combine with Xanthan gum. The surface pH and swelling index of formulation F8 was found to be 6.8, and 60 %, respectively.

  13. Enantioseparation of omeprazole--effect of different packing particle size on productivity.

    Science.gov (United States)

    Enmark, Martin; Samuelsson, Jörgen; Forssén, Patrik; Fornstedt, Torgny

    2012-06-01

    Enantiomeric separation of omeprazole has been extensively studied regarding both product analysis and preparation using several different chiral stationary phases. In this study, the preparative chiral separation of omeprazole is optimized for productivity using three different columns packed with amylose tris (3,5-dimethyl phenyl carbamate) coated macroporous silica (5, 10 and 25 μm) with a maximum allowed pressure drop ranging from 50 to 400 bar. This pressure range both covers low pressure process systems (50-100 bar) and investigates the potential for allowing higher pressure limits in preparative applications in a future. The process optimization clearly show that the larger 25 μm packing material show higher productivity at low pressure drops whereas with increasing pressure drops the smaller packing materials have substantially higher productivity. Interestingly, at all pressure drops, the smaller packing material result in lower solvent consumption (L solvent/kg product); the higher the accepted pressure drop, the larger the gain in reduced solvent consumption. The experimental adsorption isotherms were not identical for the different packing material sizes; therefore all calculations were recalculated and reevaluated assuming identical adsorption isotherms (with the 10 μm isotherm as reference) which confirmed the trends regarding productivity and solvent consumption.

  14. HCO3- secretion in rat duodenum after treatment with omeprazole and ranitidine.

    Science.gov (United States)

    Knutson, L; Flemström, G; Gustavsson, S; Jedstedt, G; Lönnerholm, G

    1987-01-01

    The bicarbonate secretion by the duodenal mucosa, which is stimulated by luminal acid, is very probably important in mucosal protection against the acid. It was of interest to investigate whether long-term deprivation of the mucosa of this acid stimulus affected the alkali secretion. Sprague-Dawley rats were treated for 4-6 weeks with either omeprazole, 14 mg/kg body weight twice daily, or ranitidine, 300 mg/kg twice daily, by means of gastric intubation. The rate of bicarbonate secretion by the duodenal mucosa was determined in situ by continuous titration. Neither the basal secretion nor the increase in secretion in response to stimulation by prostaglandin E2 or luminal acid (pH 2.0 for 5 or 60 min) differed in treated animals from that in controls that had received placebo (p greater than 0.05). Thus, 4-6 weeks of treatment with omeprazole or ranitidine did not reduce duodenal mucosal bicarbonate secretion in the rat, nor did these drugs diminish the ability of this mucosa to respond to prolonged luminal acidification or luminally administered prostaglandin E2.

  15. Protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats

    Institute of Scientific and Technical Information of China (English)

    Wei Gao; Hai-Ying Li; Li-Xin Wang; Li-Jun Hao; Jian-Li Gao; Rong-Juan Zheng; Chun-Jiang Cai; Yan-Ling Si

    2014-01-01

    Objective:To observe the protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.Methods:All rats were randomly divided into normal control group, cirrhosis and treatment group.Thioacetamide was used to establish rat model of cirrhotic portal hypertension.The necrotic tissue of gastric mucosa ulcer focus, degree of neutrophils infiltration at the ulcer margin, portal pressure, portal venous flow, abdominal aortic pressure, abdominal aortic blood flow at front end, gastric mucosal blood flow(GMBF), glycoprotein(GP) of gastric mucosa,basal acid secretion,H+ back -diffusion, gastric mucosal damage index,NO, prostaglandinE2(PGE2) and tumor necrosis factor-α(TNF-α) were determined respectively, and the pathological changes of gastric mucosa were also observed by microscope.Results:Compared with cirrhosis group and the control group, the ulcer bottom necrotic material, gastric neutrophil infiltration andUI of the treatment group were all decreased significantly(P<0.01), GMBF value,GP values, serumNO,PGE2,TNF-α were all significantly increased.Conclusions:Omeprazole has an important protective effect on gastric mucosal and it can increase gastric mucosal blood flow and related to many factors.

  16. The comparasion of combined effects of vitamin D3 and Omeprazole on prevention of menopausal

    Directory of Open Access Journals (Sweden)

    ahmad Tamjidipur

    2010-02-01

    Full Text Available Menopause and decrease of estrogenic hormones lead to osteoporosis. Treatment of osteoporosis by estrogenic hormones like estrogen in women has resulted in secondary complications such as cancers of breast and genital system. Activity of osteoclasts for removing bone is necessary to secretion of H+ ions on bone matrix. Today, using proton pump inhibitors to inhibit the activity of osteoclasts is under study. In other hand, recent researches show that these inhibitors by decrease absorbing of calcium intestine, can increase the risk of fracture. According to physiology of osteoclasts and the vitamin D mechanism on absorbing calcium from intestine, the combined effect of vitamin D3 and omeprazole were studied. Materials and Methods: 64 female Sprague dawlley rats (160 to 180 gr were selected and divided into 8 groups ( 8 in each : 1- Sham group, without ovariectomy, 2- ovariectomized group without treatment, 3- ovariectomized group, treated with vitamin D3 100 µg ∕ kg, 4- ovariectomized group, , treated with vitamin D3 400 µg ∕ kg, 5- ovariectomized group, treated with omeprazole 20 mg/ kg and vitamin D3 100 µg/kg, 6- ovariectomized group, treated with omeprazole 20 mg/ kg and vitamin D3 400 µg/kg, 7- ovariectomized group, treated with omeprazole 20 mg/ kg, 8- ovariectomized group, treated with DMSO as a solvent. A week after ovariectomy, treatment of 3th to 8th groups began and continued for 12 weeks. During the sampling, under general anesthesia, blood were sampled and serum was prepared, and then lumbar vertebrae, femur bones and the right tibia separated and were put in the fixative solution. Serum alkaline phosphatase and Ca were measured. Resistance of femur bones were measured against fracture. Histological section prepared from L3 vertebrae and the end of tibia bones. The volume density of trabeculae of the L3 vertebrae body of samples was measured by stereologic rules. The number of osteoclasts in tibias sections was measured

  17. Omeprazole versus ranitidine in the medical treatment of acute upper gastrointestinal bleeding: assessment by early repeat endoscopy.

    Science.gov (United States)

    Fasseas, P; Leybishkis, B; Rocca, G

    2001-12-01

    The purpose of this study was to assess the effects of acid suppression in patients with upper gastrointestinal bleeding using early repeat endoscopy. Ninety-two patients with the diagnosis of acute upper gastrointestinal bleeding (endoscopically verified), entered a single-blind, randomised study comparing two treatment groups: omeprazole (40 mg orally daily) to ranitidine (50 mg intravenously four times daily). The lesions considered were gastric ulcers, duodenal ulcers and erosive gastritis. All patients were candidates for medical treatment. The parameters assessed included: 1) stabilisation of the lesion by repeat endoscopy at 7.0 +/- 3.0 days, 2) bleeding recurrence, 3) duration of stay in the intermediate medical care unit. For erosive gastritis only parameters 2 and 3 were considered. The study was limited to the hospitalisation period. Endoscopic stabilisation rate at 7.0 +/- 3.0 days for duodenal lesions was higher in the omeprazole group (71% vs 37%, p=0.03), but there was no significant difference for gastric lesions (50% vs 54%, NS). The overall bleeding recurrence rate (0% vs 17%, p=0.013) and the duration of stay (3.9 vs 6.4 days, p<0.01) were significantly lower in the omeprazole group. Our study suggests that omeprazole is more effective than ranitidine in the pharmacological treatment of acute upper gastrointestinal bleeding.

  18. Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.

    Science.gov (United States)

    Dmochowski, Roger; Chen, Andrew; Sathyan, Gayatri; MacDiarmid, Scott; Gidwani, Shalini; Gupta, Suneel

    2005-08-01

    This study assessed the effect of the proton pump inhibitor omeprazole on the bioavailability of the extended-release formulations of oxybutynin and tolterodine. Forty-four healthy volunteers received each of 4 treatments in a 4-period crossover design. The treatments consisted of osmotically controlled extended-release oxybutynin chloride tablets at 10 mg/d or extended-release tolterodine tartrate capsules at 4 mg/d, with and without preceding treatment with 20 mg omeprazole daily for 4 days. Blood samples collected predose and at scheduled time points for 36 hours postdose were analyzed for oxybutynin and its active metabolite, N-desethyloxybutynin, or tolterodine and its active 5-hydroxymethyl metabolite, as appropriate. The AUCinfinity ratios for oxybutynin and its metabolite with and without prior omeprazole fell within the 80% to 125% range (accepted as the criterion for bioequivalence), as did those for tolterodine and its active moiety. The peak concentration ratios for oxybutynin and metabolite also conformed to this range; those for tolterodine did not. Increasing gastric pH with omeprazole does not substantially alter the pharmacokinetic properties of extended-release oxybutynin but may alter those of extended-release tolterodine.

  19. Gestão das inovações incrementais, o caso Omeprazola Management of incremental innovations, the case Omeprazole

    Directory of Open Access Journals (Sweden)

    Alexandre Lopes Lourenço

    2010-01-01

    Full Text Available Our report shows the strategies adopted by pharmaceutical industry in the development of incremental innovations, through the development carried out after the launch of omeprazole. Some improvements are really necessary and others are used only as a market strategy and evergreening.

  20. Bismuth-Based Quadruple Therapy with Bismuth Subcitrate, Metronidazole, Tetracycline and Omeprazole in the Eradication of Helicobacter pylori

    Directory of Open Access Journals (Sweden)

    Raymond Lahaie

    2001-01-01

    Full Text Available BACKGROUND: A previous study showed that 14 days of qid bismuth-based triple therapy with tetracycline 500 mg, metronidazole 250 mg and colloidal bismuth subcitrate 120 mg resulted in excellent Helicobacter pylori eradication rates (89.5%. The present study looked at a shorter treatment period by adding omeprazole and by reducing the dose of tetracycline.

  1. Gaviscon® vs. omeprazole in symptomatic treatment of moderate gastroesophageal reflux. a direct comparative randomised trial

    Directory of Open Access Journals (Sweden)

    Pouchain Denis

    2012-02-01

    Full Text Available Abstract Background Medical management of GERD mainly uses proton pump inhibitors. Alginates also have proven efficacy. The aim of this trial was to compare short-term efficacy of an alginate (Gaviscon®, 4 × 10 mL/day and omeprazole (20 mg/day on GERD symptoms in general practice. Methods A 14-day multicentre randomised double-blind double-dummy non-inferiority trial compared Gaviscon® (4 × 10 mL/day and omeprazole (20 mg/day in patients with 2-6 day heartburn episodes weekly without alarm signals. The primary outcome was the mean time to onset of the first 24-h heartburn-free period after initial dosing. Secondary outcomes were the proportion of patients without heartburn by D7, pain relief by D7, and reduction in pain intensity by D7 and D14. Results 278 patients were recruited; 120 were included in the Gaviscon® group and 121 in the omeprazole group for the per protocol non-inferiority analysis. The mean time to onset of the first 24-h heartburn-free period after initial dosing was 2.0 (± 2.2 days for Gaviscon® and 2.0 (± 2.3 days for omeprazole (p = 0.93; mean intergroup difference was 0.01 ± 1.55 days (95% CI = -0.41 to 0.43: i.e., less than the lower limit of the 95% CI of -0.5 days predetermined to demonstrate non-inferiority. The mean number of heartburn-free days by D7 was significantly greater in the omeprazole group: 3.7 ± 2.3 days vs. 3.1 ± 2.1 (p = 0.02. On D7, overall quality of pain relief was slightly in favour of omeprazole (p = 0.049. There was no significant difference in the reduction in pain intensity between groups by D7 (p = 0.11 or D14 (p = 0.08. Tolerance and safety were good and comparable in both groups. Conclusion Gaviscon® was non-inferior to omeprazole in achieving a 24-h heartburn-free period in moderate episodic heartburn, and is a relevant effective alternative treatment in moderate GERD in primary care. Trial registration ISRCTN62203233.

  2. Herbal medicine Yin Zhi Huang induces CYP3A4-mediated sulfoxidation and CYP2C19-dependent hydroxylation of omeprazole

    Institute of Scientific and Technical Information of China (English)

    Lan FAN; Hong-hao ZHOU; Guo WANG; Lian-sheng WANG; Yao CHEN; Wei ZHANG; Yuan-fei HUANG; Rui-xue HUANG; Dong-li HU; Dan WANG

    2007-01-01

    Aim: To explore the potential interactions between Yin Zhi Huang (YZH) and omeprazole, a substrate of CYP3A4 and CYP2C19. Methods: Eighteen healthy volunteers, including 6 CYP2C19* 1/*1, 6 CYP2C19*1/*2 or *3 and 6 CYP2C19*2/ *2 were enrolled in a 2-phase, randomized, crossover clinical trial. In each phase,the volunteers received either placebo or 10 mL YZH oral liquid, 3 times daily for 14 d. Then all the patients took a 20 mg omeprazole capsule orally. Blood samples were collected up to 12 h after omeprazole administration. Plasma concentrations of omeprazole and its metabolites were quantified by HPLC with UV detection.Results: After 14 d of treatment of YZH, plasma omeprazole significantly decreased and those of omeprazole sulfone and 5-hydroxyomeprazole signifi-cantly increased. The ratios of the area under the plasma concentration-time curves from time 0 to infinity (AUC(0-∞) of omeprazole to 5-hydroxyomprazole and those of omeprazole to omeprazole sulfone decreased by 64.80%±12.51% (P=0.001 ) and 63.31%±18.45 % (P=0.004) in CYP2C 19* 1/* 1,57.98%±14. 80% (P=0.002)and 54.87%±18.42% (P=0.003) in CYP2C19*1/*2 or *3, and 37.74%±16.07% (P=0.004) and 45.16%± 15.54% (P=0.003) in CYP2C19*2/*2, respectively. The decrease of the AUC(0-∞) ratio of omeprazole to 5-hydroxyomprazole in CYP2C19*1/*1 and CYP2C19*1/*2 or *3 was greater than those in CYP2C19*2/*2 (P=0.047 and P=0.009). Conclusion: YZH induces both CYP3A4-catalyzed sulfoxidation and CYP2C19-dependent hydroxylation of omeprazole leading to decreases in plasma omeprazole concentrations.

  3. The effect of changes in gastric pH induced by omeprazole on the absorption and respiratory depression of methadone.

    Science.gov (United States)

    de Castro, J; Aguirre, C; Rodríguez-Sasiaín, J M; Gómez, E; Garrido, M J; Calvo, R

    1996-10-01

    The effect of omeprazole (2 mg kg-1 i.v.) on respiratory depression induced in rats by acute oral methadone administration (5 mg kg-1) was examined and compared with control animals that only received methadone. Quantitative assessments of arterial Pco2,Po2, pH, and respiratory rate were employed as criteria for evaluation. Intragastric pH was measured in each rat immediately before and 2 h after methadone. Plasma concentration of methadone was measured for 3 h. The relationship between drug effect and the systemic bioavailability of methadone, measured as the area under the plasma concentration-time curve (AUC0-180), was also evaluated. The intensity of the methadone-induced respiratory depression was significantly greater in the omeprazole group than in control rats. A significant variation (p Omeprazole caused a significant increase in methadone levels (Cmax = 156 +/- 6.5 ng mL-1 against 51 +/- 5.8 ng mL-1 in control; p omeprazole treatment (18.6 +/- 1.4 micrograms mL-1 min) than in control (6.8 +/- 0.6 microgram mL-1 min). Two hours after treatment with omeprazole, intragastric pH values were significantly elevated (4.7 +/- 0.1 against 2.2 +/- 0.04) and continued increasing, being 6.4 +/- 0.1 at the end of the experiment. Correlation was observed between intragastric pH and the area under the effect- (respiratory depression-) time curve (r = 0.74; p bicarbonate whereas opposite results were obtained with acidic pH2 solution.

  4. Development of a multiparticulate system containing enteric-release mini-tablets of omeprazole

    Directory of Open Access Journals (Sweden)

    Volnei Jose Tondo Filho

    2014-09-01

    Full Text Available The main aim of this study was to develop a multiparticulate system containing mini-tablets of omeprazole formulated with an enteric polymer with pH-dependent solubility. Pre-formulation studies showed good flow and compaction capacity, leading to the production ofhigh quality mini-tablets. The mini-tablets were coated in a fluidized bed with hydroxypropylmethylcellulose /Eudragit(r L30D55 and packed into hard gelatin capsules. The dissolution profile showed gastro-resistance and zero-order kinetics. The dissolution profile for the formulation containing lactose as the diluent and coated with 12% (tablet weight gain of polymer was similar to that ofthe reference drug.

  5. Nizatidine and omeprazole enhance the effect of metronidazole on Helicobacter pylori in vitro

    DEFF Research Database (Denmark)

    Chen, Ming; Jensen, Bente; Zhai, Lin

    2002-01-01

    Treatment failures are common in patients infected with metronidazole-resistant Helicobacter pylori in the gastric mucosa when triple therapy including metronidazole is used. In patients with treatment failure and metronidazole-resistant H. pylori, a higher eradication rate for H. pylori was found...... after secondary treatment with bismuth/ranitidine in combination with antibiotics including metronidazole, compared with the same antibiotics combined with a standard dose of omeprazole. This agrees with our previous finding that bismuth was able to reduce the susceptibility of H. pylori...... to metronidazole. In this study, we have found that nizatidine, an H(2)-receptor antagonist, is also able to reduce the susceptibility of H. pylori to metronidazole in vitro, despite having no direct inhibitory effect on the growth of H. pylori. This agrees with earlier findings that compounds having the ability...

  6. Hydroxylation index of omeprazole in relation to CYP2C19 polymorphism and sex in a healthy Iranian population.

    Science.gov (United States)

    Payan, Maryam; Rouini, Mohammad Reza; Tajik, Nader; Ghahremani, Mohammad Hossein; Tahvilian, Reza

    2014-12-11

    Polymorphism of CYP2C19 gene is one of the important factors in pharmacokinetics of CYP2C19 substrates. Omeprazole is a proton pump inhibitor which is mainly metabolized by cytochrome P450 2C19 (CYP2C19). The aim of present study was to assess omeprazole hydroxylation index as a measure of CYP2C19 activity considering new variant allele (CYP2C19*17) in Iranian population and also to see if this activity is sex dependent. One hundred and eighty healthy unrelated Iranian individuals attended in this study. Blood samples for genotyping and phenotyping were collected 3 hours after administration of 20 mg omeprazole orally. Genotyping of 2C19 variant alleles *2, *3 and *17 was performed by using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) and semi-nested PCR methods. Plasma concentrations of omeprazole and hydroxyomeprazole were determined by high performance liquid chromatography (HPLC) technique and hydxroxylation index (HI) (omeprazole/ hydroxyomeprazole) was calculated. The CYP2C19*17 was the most common variant allele in the studied population (21.6%). Genotype frequencies of CYP2C19*17*17, *1*17, and *2*17 were 5.5%, 28.8% and 3.3% respectively. The lowest and the highest median omeprazole HI was observed in *17*17 and *2*2 genotypes respectively (0.36 vs. 13.09). The median HI of omeprazole in subjects homozygous for CYP2C19*1 was 2.16-fold higher than individuals homozygous for CYP2C19*17 (P < 0.001) and the median HI of CYP2C19*1*17 genotype was 1.98-fold higher than CYP2C19 *17*17 subjects (P < 0.001). However, subjects with CYP2C19*2*17 (median HI: 1.74) and CYP2C19*1*2 (median HI: 1.98) genotypes and also CYP2C19*1*17 (median HI: 0.71) and CYP2C19*1*1 (mean HI: 0.78) did not show any significantly different enzyme activity. In addition, no statistically significant difference was found between women and men in distribution of CYP2C19 genotypes. Furthermore, the hydroxylation index of Omeprazole was not different

  7. Involvement of cytochrome P450 3A4 and P-glycoprotein in first-pass intestinal extraction of omeprazole in rabbits

    Institute of Scientific and Technical Information of China (English)

    Hai-ming FANG; Jian-ming XU; Qiao MEI; Lei DIAO; Mo-li CHEN; Juan JIN; Xin-hua XU

    2009-01-01

    Aim: To quantitatively evaluate in vivo first-pass intestinal extraction of omeprazole and to investigate the possible involvement of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) in this process in rabbits.Methods: Pharmacokinetic parameters were examined after intraduodenal (id), intraportal venous (ipv), and intravenous (iv) administration of omeprazole at various doses to intestinal and vascular access-ported rabbits. Extraction ratios in the liver and intestinal tract were determined from the area under the plasma concentration-time curve (AUC). In addition, omeprazole was administered by id or iv to rabbits alone or 30 min after the id administration of CYP3A4 or P-gp inhibitors (ketoconazole or verapamil, respectively). Results: Pharmacokinetic parameters of omeprazole were dose-dependent after id, ipv, and iv administration at various doses. After id administration of 3 mg/kg omeprazole, the hepatic and intestinal extraction ratio was 57.18%±2.73% and 54.94%±1.85%, while the value was 59.29%±3.14% and 54.20%±1.53% after given 6 mg/kg, respectively. Compared with the control group, the presence of ketoconazole (60 mg/kg) or verapamil (9 mg/kg) significantly increased the area under the plasma concentration time curve (AUC) and the peak concentration (C_(max)) of id-administered omeprazole, while it had no significant effect on omeprazole administered by iv. Conclusion: Oral omeprazole undergoes marked extraction in the small intestine, and increased bioavailability of the drug after id administration of ketoconazole and verapamil suggests that this increase results from inhibition of CYP3A4 and P-gp function in the intestine rather than the liver.

  8. Pharmacokinetic and pharmacodynamic effects of two omeprazole formulations on stomach pH and gastric ulcer scores.

    Science.gov (United States)

    Raidal, S L; Andrews, F M; Nielsen, S G; Trope, G

    2017-04-22

    Limited data are available on the relative pharmacokinetics and pharmacodynamics of different omeprazole formulations. To compare pharmacokinetic and pharmacodynamic effects of a novel omeprazole formulation against a currently registered product. Masked 2 period, 2 treatment crossover. Twelve clinically healthy horses were studied over two 6-day treatment periods. Horses were randomly assigned to receive a novel omeprazole paste (Ulcershield: ULS) or a currently registered reference omeprazole product (OMO). Gastric pH was measured continuously for 10 h on the day prior to commencing treatment (Day -1) and after 6 days of oral treatment (Day 5) using in situ antimony pH probes within an indwelling nasogastric tube. Plasma pharmacokinetics were determined on Days 0 and 6. Treatment significantly (Pgastric pH on Day 5, compared to results obtained prior to treatment (Day -1) and there was no significant difference between products (P = 0.773). Similarly, comparison of median hourly gastric pH (P = 0.593), mean gastric pH (P = 0.154), percentage time pHgastric pH response curve (P = 0.734) did not discriminate between products. Both treatments resulted in significantly lower gastric ulcer severity scores (both P = 0.004), with no difference between treatments (P = 0.688). Comparison of mean log area under time-plasma concentration curves demonstrated that, although the lower limit of the 90% confidence interval was within the -20% limit for bioequivalence, the upper limit was exceeded, suggesting that the test product could have greater bioavailability than the reference product. The small sample size, large interhorse plasma omeprazole concentrations, and low bioavailability of omeprazole impacted the sensitivity of the bioequivalence analysis. ULS matched or slightly exceeded OMO plasma concentrations. Both products resulted in equivalent increases in gastric pH, gastric pH profiles and decrease in gastric ulcer scores. Thus, ULS was pharmacodynamically equivalent

  9. Anti-carcinogenic properties of omeprazole against human colon cancer cells and azoxymethane-induced colonic aberrant crypt foci formation in rats.

    Science.gov (United States)

    Patlolla, Jagan M R; Zhang, Yuting; Li, Qian; Steele, Vernon E; Rao, Chinthalapally V

    2012-01-01

    Omeprazole is a proton pump inhibitor, a widely used drug to treat ulcers and gastroesophageal refluxdisease. We have evaluated colon cancer chemopreventive properties of omeprazole using azoxymethane (AOM)-induced colonic aberrant crypt foci (ACF) in male F344 rats and analyzed cell growth inhibition and apoptosis induction in human colon cancer cells. Five-week-old male F344 rats were fed a control or experimental diet containing two doses of omeprazole (200 and 400 ppm). After one week, all animals were s.c. injected with AOM (15 mg/kg body weight, once weekly for two weeks). Rats continued on experimental diets for seven more weeks before being sacrificed. Colons were histopathologically evaluated for ACF. Human colon cancer HCT-116 and HCA-7 cells treated with omeprazole were evaluated for different markers associated with proliferation and apoptotic markers using Western blot technique. Rats fed with 200 and 400 ppm of omeprazole significantly suppressed total colonic ACF formation (~30%, Pcancer cell lines HCT-116 and HCA-7 cells resulted in induction of p21waf1/cip1 and decreased the expression of anti-apoptotic proteins Bcl-2, Bcl-XL and survivin in a dose-dependent manner. Anticancer properties observed in colon cancer cell lines suggest that omeprazole may induce key signaling molecules of antiproliferation and inhibition of anti-apoptotic proteins.

  10. Treatment with omeprazole, metronidazole, and amoxicillin in captive South African cheetahs (Acinonyx jubatus) with spiral bacteria infection and gastritis.

    Science.gov (United States)

    Lane, Emily; Lobetti, Remo; Burroughs, Richard

    2004-03-01

    Six captive cheetahs (Acinonyx jubatus) with severe gastritis diagnosed by gastric endoscopy and mucosal histopathology were treated with omeprazole, metronidazole, and amoxicillin for 3 wk. Endoscopic biopsies were performed before therapy, immediately after treatment, and 3, 7, and 19 mo after treatment. Macroscopic appearance of the stomach, histologic scoring of gastric inflammation, and the presence or absence of spiral bacteria were recorded. Spiral bacteria were absent histologically immediately after treatment but reappeared in endoscopic biopsies by 3 mo after treatment. Gastritis scores fluctuated widely during the trial but improved in five of six cheetahs by 3 mo after treatment. By 19 mo after treatment, scores were close to the pretreatment scores. Therapy with omeprazole, amoxicillin, and metronidazole was associated with temporary improvement in the degree and distribution of gastritis in some cheetahs with gastritis, suggesting that treatment may be warranted once severe gastric inflammation has been diagnosed.

  11. Enantioselective endocrine disrupting effects of omeprazole studied in the H295R cell assay and by molecular modeling.

    Science.gov (United States)

    Sørensen, Amalie Møller; Hansen, Cecilie Hurup; Bonomo, Silvia; Olsen, Lars; Jørgensen, Flemming Steen; Weisser, Johan Juhl; Kretschmann, Andreas Christopher; Styrishave, Bjarne

    2016-08-01

    Enantiomers possess different pharmacokinetic and pharmacodynamic properties and this may not only influence the therapeutic effect of a drug but also its toxicological effects. In the present work we investigated the potential enantioselective endocrine disrupting effects of omeprazole (OME) and its two enantiomers on the human steroidogenesis using the H295R cell line. Differences in production of 16 steroid hormones were analyzed using LC-MS/MS. Additionally, to evaluate the differences in binding modes of these enantiomers, docking and molecular dynamics (MD) simulations of S-omeprazole (S-OME) and R-omeprazole (R-OME) in CYP17A1, CYP19A1 and CYP21A2 were carried out. Exposing H295R cells to OME and its enantiomers resulted in an increase of progesterone (PRO) and 17α-hydroxy-progesterone (OH-PRO) levels. At the same time, a decrease in the corticosteroid and androgen synthesis was observed, indicating inhibition of CYP21A2 and CYP17A1. In both cases, the effect of R-OME was smaller compared to that of the S-OME and a certain degree of enantioselectivity of CYP17A1 and CYP21A2 was suggested. Docking indicated that the N-containing rings of OME possibly could interact with the iron atom of the heme for S-OME in CYP17A1 and S- and R-OME in CYP21A2. However, density functional theory calculations suggest that the direct N-Fe interaction is weak. The study demonstrates enantioselective differences in the endocrine disrupting potential of chiral drugs such as omeprazole. These findings may have potential implications for drug safety and drug design.

  12. Efficacy of adding sodium alginate to omeprazole in patients with nonerosive reflux disease: a randomized clinical trial.

    Science.gov (United States)

    Manabe, N; Haruma, K; Ito, M; Takahashi, N; Takasugi, H; Wada, Y; Nakata, H; Katoh, T; Miyamoto, M; Tanaka, S

    2012-07-01

    Nonerosive reflux disease (NERD) is the most common form of gastroesophageal reflux disease. Patients with NERD have a lower response rate to proton pump inhibitors (PPIs) than patients with erosive esophagitis when gauged from relief of heartburn. Sodium alginate decreases the acidity of refluxate and protects the esophageal mucosa. However, whether the addition of sodium alginate to PPI therapy can improve NERD symptoms remains unknown. Accordingly, the aim of this study was to evaluate the efficacy of adding sodium alginate to basal PPI therapy for NERD. Patients who had experienced heartburn on at least 2 days per week during the 1-month period before entering the study and had no endoscopic mucosal breaks (grade M or N according to Hoshihara's modification of the Los Angeles classification) were randomized to one of two treatments for 4 weeks: omeprazole (20 mg once daily) plus sodium alginate (30 mL four times a day) (group A) or omeprazole (20 mg once daily) alone (group B). Eighty-seven patients were enrolled, and 76 patients were randomly assigned to group A (n = 36) or group B (n = 40). Complete resolution of heartburn for at least 7 consecutive days by the end of treatment was significantly more common in group A (56.7%) than in group B (25.7%). One patient from group A had mild drug-related diarrhea that was not clinically serious. In conclusion, omeprazole combined with sodium alginate was better than omeprazole alone in Japanese patients with NERD. © 2011 Copyright the Authors. Journal compilation © 2011, Wiley Periodicals, Inc. and the International Society for Diseases of the Esophagus.

  13. Enantioselective endocrine disrupting effects of omeprazole studied in the H295R cell assay and by molecular modeling

    DEFF Research Database (Denmark)

    Sørensen, Amalie Møller; Hansen, Cecilie Hurup; Bonomo, Silvia

    2016-01-01

    ) and its two enantiomers on the human steroidogenesis using the H295R cell line. Differences in production of 16 steroid hormones were analyzed using LC-MS/MS. Additionally, to evaluate the differences in binding modes of these enantiomers, docking and molecular dynamics (MD) simulations of S-omeprazole (S......-OME) and R-omeprazole (R-OME) in CYP17A1, CYP19A1 and CYP21A2 were carried out. Exposing H295R cells to OME and its enantiomers resulted in an increase of progesterone (PRO) and 17α-hydroxy-progesterone (OH-PRO) levels. At the same time, a decrease in the corticosteroid and androgen synthesis was observed...... of the heme for S-OME in CYP17A1 and S- and R-OME in CYP21A2. However, density functional theory calculations suggest that the direct N-Fe interaction is weak. The study demonstrates enantioselective differences in the endocrine disrupting potential of chiral drugs such as omeprazole. These findings may have...

  14. Effects of omeprazole and eradication of Helicobacter pylori on gastric and duodenal mucosal enzyme activities and DNA in duodenal ulcer patients.

    Science.gov (United States)

    Vetvik, K; Schrumpf, E; Mowinckel, P; Aase, S; Andersen, K J

    1994-11-01

    Duodenal and gastric content of mucosal enzymes in duodenal ulcer (DU) patients differs from that of controls. The purpose of this study has been to examine the effect of omeprazole and eradication of Helicobacter pylori on mucosal enzymes in DU patients. The enzyme activities of seven gastric and duodenal mucosal marker enzymes from the brush border, lysosomes, and mitochondria have been studied. In study I the measurements were made in 29 patients with an active DU before and after 14 days of omeprazole treatment. In study II 22 duodenal ulcer patients were given bismuth subnitrate, oxytetracycline, and metronidazole (triple therapy) for 2 weeks to eradicate H. pylori. Biopsy specimens were taken from the duodenum and the stomach for enzyme measurements and histologic assessment. In study II additional specimens were obtained from the prepyloric region for urease tests and culture of H. pylori. The ulcer healing rates were more than 90% after both omeprazole and triple therapy. H. pylori was eradicated in 86% after triple therapy. The activities of the brush-border enzymes lactase, neutral-alpha-glucosidase, alkaline phosphatase, leucyl-beta-naphthylamidase, and gamma-glutamyltransferase (gamma-GT) increased significantly in the duodenal bulb and the descending duodenum during treatment with omeprazole. No changes in duodenal enzyme activity were detected after triple therapy, whereas a significant fall in gamma-GT and acid phosphatase activities was seen in the stomach. The mucosal DNA in the gastric antrum decreased both after treatment with omeprazole and after triple therapy. A similar decrease in mucosal DNA of the gastric antrum was demonstrated after both omeprazole and triple therapy with bismuth subnitrate, oxytetracycline, and metronidazole. Omeprazole also affects the content of duodenal mucosal enzymes, whereas triple therapy particularly affects the gastric mucosal enzyme activity.

  15. Efficacy of omeprazole and amoxicillin with either clarithromycin or metronidazole on eradication of Helicobacter pylori in Chinese peptic ulcer patients

    Institute of Scientific and Technical Information of China (English)

    Wei-Hao Sun; Han Su; Xi-Long Ou; Da-Zhong Cao; Qian Yu; Ting Yu; Jin-Ming Hu; Feng Zhu; Yun-Liang Sun; Xi-Ling Fu

    2005-01-01

    AIM: One-week triple therapy with proton pump inhibitors, clarithromycin and amoxicillin has recently been proposed as the first-line treatment for Helicobacter pylori(H pylori) infection; however, data regarding the effects of this regimen in China are scarce. The aim of this prospective and randomized study was to compare the efficacy of clarithromycin and metronidazole when they were combined with omeprazole and amoxicillin on eradication of H pylori and ulcer healing in Chinese peptic ulcer patients.METHODS: A total of 103 subjects with H pylori-positive peptic ulcer were randomly divided into two groups, and accepted triple therapy with omeprazole 20 mg, amoxicillin 1 000 mg and either clarithromycin 500 mg (OAC group,n = 58) or metronidazole 400 mg (OAM group, n = 45).All drugs were given twice daily for 7 d. Patients with active peptic ulcer were treated with omeprazole 20 mg daily for 2-4 wk after anti-H pylori therapy. Six to eight weeks after omeprazole therapy, all patients underwent endoscopies and four biopsies (two from the antrum and two others from the corpus of stomach) were taken for rapid urease test and histological analysis (with modified Giemsa staining) to examine H pylori. Successful eradication was defined as negative results from both examination methods.RESULTS: One hundred patients completed the entire course of therapy and returned for follow-up. The eradication rate of H pylori for the per-protocol analysis was 89.3% (50/56) in OAC group and 84.1% (37/44) in OAM group. Based on the intention-to-treat analysis, the eradication rate of H pylori was 86.2% (50/58) in OAC group and 82.2% (37/45) in OAM group. There were no significant differences in eradication rates between the two groups on either analysis. The active ulcer-healing rate was 96.7% (29/30) in OAC group and 100% (21/21)in OAM group (per-protocol analysis, P>0.05). Six patients in OAC group (10.3%) and five in OAM group (11.1%)reported adverse events (P>0.05).CONCLUSION

  16. The bioavailability of bromazepam, omeprazole and paracetamol given by nasogastric feeding tube.

    Science.gov (United States)

    Podilsky, Gregory; Berger-Gryllaki, Markoulina; Testa, Bernard; Buclin, Thierry; Roulet, Michel; Pannatier, Andre

    2009-05-01

    To characterize and compare the pharmacokinetic profiles of bromazepam, omeprazole and paracetamol when administered by the oral and nasogastric routes to the same healthy cohort of volunteers. In a prospective, monocentric, randomized crossover study, eight healthy volunteers received the three drugs by the oral (OR) and nasogastric routes (NT). Sequential plasma samples were analyzed by high-performance liquid chromatography-UV, pharmacokinetic parameters (Cmax, AUC(0-infinity), t(1/2), k(e), tmax) were compared statistically, and Cmax, AUC(0-infinity) and t(max) were analyzed for bioequivalence. A statistically significant difference was seen in the AUC(0-infinity) of bromazepam, with nasogastric administration decreasing availability by about 25%: AUC(OR) = 2501 ng mL(-1) h; AUC(NT) = 1855 ng mL(-1) h (p 0.05); ratio (geometric mean) = 1.01 (90% CI 0.64-1.61). An extended study with a larger number of subjects may possibly provide clearer answers. The narrow 90% confidence limits of paracetamol indicate bioequivalence: AUC(OR) = 37 microg mL(-1) h; AUC(NT) = 41 microg mL(-1) h(p > 0.05); ratio (geometric mean) = 1.12 (90% CI 0.98-1.28). The results of this study show that the nasogastric route of administration does not appear to cause marked, clinically unsuitable alterations in the bioavailability of the tested drugs.

  17. Effects of cisapride on ulcer formation and gastric secretion in rats: comparison with ranitidine and omeprazol.

    Science.gov (United States)

    Alarcón de la Lastra, C; Martin, M J; La Casa, M; López, A; Motilva, V

    1996-12-01

    1. The antiulcerogenic effects of cisapride, a potent benzamide-stimulating gastrointestinal motility agent, were studied on cold-resistant and pylorus-ligated gastric ulcers. Acidity, composition of gastric secretion, and quantitative and qualitative changes on mucus glycoprotein content were also determined. These effects were compared with those of ranitidine (50 mg/kg) and omeprazol (10 mg/kg). 2. Oral cisapride (10-100 mg/kg) dose-relatedly and significantly (P < 0.01, P < 0.05) decreased the severity of the lesions induced by cold-resistant stress. In stressed rats, cisapride increased the amount of mucus secretion and markedly enhanced the glycoprotein content. Morphometric evaluation of mucus secretion revealed a significant increase in both the PAS area (neutral glycoproteins) and Alcian blue area (sulfated glycoproteins). 3. In 4 h pyloric-ligated animals, cisapride (10-100 mg/kg) showed a significant reduction in the number and severity of ulcers (P < 0.01) and histamine concentration (P < 0.01, P < 0.001). In addition, at the highest doses (50-100 mg/kg), cisapride produced a significant decreases in acidity; however, it did not alter the gastric volume secretion or pepsin concentrations. 4. These results suggest that cisapride shows antiulcerogenic effects which could possibly be explained through antisecretory and cytoprotective mechanisms involving an enhancement of cuality and production of gastric mucus.

  18. Potentiation of the action of calcium hydroxide on Enterococcus faecalis by proton pump inhibitor omeprazole = Potencialização da ação do hidróxido de cálcio sobre o Enterococcus faecalis pelo inibidor da bomba de prótons omeprazol

    Directory of Open Access Journals (Sweden)

    Cogo, Deborah Meirelles

    2015-01-01

    Full Text Available Objetivo: O hidróxido de cálcio não representa uma estratégia totalmente eficaz contra Enterococcus faecalis (E. faecalis, uma bactéria anaeróbia facultativa resistente aos processos de desinfecção mais convencionais. O objetivo deste estudo in vitro foi avaliar o efeito do hidróxido de cálcio, do omeprazol e das associações destas substâncias contra Enterococcus faecalis, assim como avaliar se a catalização ácida do omeprazol pode ter influência sobre os resultados. Métodos: A Concentração Inibitória Mínima (CIM destes medicamentos contra E. faecalis (ATCC 29212 foi determinada pelo teste de macrodiluição adaptado do CLSI (Clinical Laboratory Standards Institute. Soluções com diferentes concentrações de hidróxido de cálcio, associadas ou não ao omeprazol, foram testadas. Os dados foram analisados estatisticamente pelo teste ANOVA com post-hoc de Tukey, com um nível de significância de 5%. Resultados: A CIM para o hidróxido de cálcio foi de 32 mg mL-1 e, quando associada com omeprazol, foi reduzida para 16 mg mL-1. O omeprazol e o omeprazol acidificado tiveram atividade semelhante. Conclusões: O omeprazol foi capaz de potencializar o efeito do hidróxido de cálcio, uma vez que a associação dessas drogas reduziu a CIM para o E. faecalis. A acidificação do omeprazol, quando associado com o hidróxido de cálcio, em concentrações diferentes, não influenciou o seu efeito

  19. A randomized controlled study comparing omeprazole and cimetidine for the prophylaxis of stress-related upper gastrointestinal bleeding in patients with intracerebral hemorrhage.

    Science.gov (United States)

    Liu, Bo-lin; Li, Bing; Zhang, Xiang; Fei, Zhou; Hu, Shi-jie; Lin, Wei; Gao, Da-kuan; Zhang, Li

    2013-01-01

    Patients with intracerebral hemorrhage (ICH) are at high risk for severe stress-related upper gastrointestinal (UGI) bleeding, which is predictive of higher mortality. The aim of this study was to evaluate the effectiveness of omeprazole and cimetidine compared with a placebo in the prevention and management of stress-related UGI bleeding in patients with ICH. In a single-center, randomized, placebo-controlled study, 184 surgically treated patients with CT-proven ICH within 72 hours of ictus and negative results for gastric occult blood testing were included. Of these patients, 165 who were qualified upon further evaluation were randomized into 3 groups: 58 patients received 40 mg intravenous omeprazole every 12 hours, 54 patients received 300 mg intravenous cimetidine every 6 hours, and 53 patients received a placebo. Patients whose gastric occult blood tests were positive at admission (n = 70) and during/after the prophylaxis procedure (n = 48) were treated with high-dose omeprazole at 80 mg bolus plus 8 mg/hr infusion for 3 days, followed by 40 mg intravenous omeprazole every 12 hours for 7 days. Of the 165 assessable patients, stress-related UGI bleeding occurred in 9 (15.5%) in the omeprazole group compared with 15 patients (27.8%) in the cimetidine group and 24 patients (45.3%) in the placebo group (p = 0.003). The occurrence of UGI bleeding was significantly related to death (p = 0.022). Nosocomial pneumonia occurred in 14 patients (24.1%) receiving omeprazole, 12 (22.2%) receiving cimetidine, and 8 (15.1%) receiving placebo (p > 0.05). In patients with UGI bleeding in which high-dose omeprazole was initiated, UGI bleeding arrested within the first 3 days in 103 patients (87.3%). Omeprazole significantly reduced the morbidity of stress-related UGI bleeding in patients with ICH due to its effective prophylactic effect without increasing the risk of nosocomial pneumonia, but it did not reduce the 1-month mortality or ICU stay. Further evaluation of high

  20. A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358, in healthy adults

    Directory of Open Access Journals (Sweden)

    Pierce D

    2015-02-01

    Full Text Available David Pierce,1 Mary Corcoran,2 Maria Velinova,3 Stuart Hossack,4 Mieke Hoppenbrouwers,5 Patrick Martin,21Shire, Basingstoke, UK; 2Shire, Wayne, PA, USA; 3PRA International, Zuidlaren, the Netherlands; 4Covance, Leeds, UK; 5Shire-Movetis NV, Turnhout, BelgiumBackground: About 30% of patients with gastroesophageal reflux disease continue to experience symptoms despite treatment with proton pump inhibitors. The 5-hydroxytryptamine 4 receptor agonist revexepride (SSP-002358 is a novel prokinetic that stimulates gastrointestinal motility, which has been suggested as a continued cause of symptoms in these patients. The aim of this study was to assess whether revexepride pharmacokinetics were affected by co-administration of omeprazole, in preparation for a proof-of-concept evaluation of revexepride added to proton pump inhibitor treatment.Methods: In this phase 1, open-label, randomized, two-period crossover study, healthy adults aged 18–55 years were given a single dose of revexepride 1 mg or revexepride 1 mg + omeprazole 40 mg. Pharmacokinetic parameters were assessed for up to 48 hours after administration of the investigational product. Adverse events, clinical chemistry and hematology parameters, electrocardiograms, and vital signs were monitored.Results: In total, 42 participants were enrolled and 40 completed the study. The median age was 24 years (18–54 years, 55% were women and 93% were white. The pharmacokinetic parameters of revexepride were similar without or with omeprazole co-administration. The mean area under the plasma concentration–time curve from time 0 to infinity (AUC0–∞ was 23.3 ng · h/mL (standard deviation [SD]: 6.33 ng · h/mL versus 24.6 ng · h/mL (SD: 6.31 ng · h/mL, and maximum plasma concentrations (Cmax were 3.89 ng/mL (SD: 1.30 ng/mL and 4.12 ng/mL (SD: 1.29 ng/mL in participants without and with omeprazole, respectively. For AUC0–∞ and Cmax, the 90% confidence intervals for the ratios of geometric least

  1. Effects of Shuanghuanglian Injection on Omeprazole Metabolism%双黄连注射液对奥美拉唑代谢的影响

    Institute of Scientific and Technical Information of China (English)

    于伟凡

    2011-01-01

    Objective:To investigate the effects of omeprazole metabolism by Shuanghuanglian injection.Methods:Determined the consistency of omeprazole in incubation reaction system by HPLC. Calculated metabolic conversion of omeprazole.Results:Metabolic conversion of omeprazole decreased with increasing concentration of Shuanghuanglian Injection. IC50 was 1 .09μ1·100μ1-1 .Conclusion: Shuanghuanglian inj ection can inhibit the metabolism of omeprazole.%目的:研究双黄连注射液对奥美拉唑代谢的影响.方法:采用高效液相色谱法测定大鼠肝微粒体温孵系统中奥美拉唑的浓度,计算奥美拉唑代谢转化率.结果:奥美拉唑代谢转化率随双黄连注射液的浓度的升高而降低.IC50为1.09μl·100μl-1.结论:双黄连注射液可抑制奥美拉唑的代谢.

  2. Efeito do omeprazol e do pantoprazol sobre a regeneração hepática após hepatectomia parcial em ratos Effect of omeprazole and pantoprazole on liver regeneration after partial hepatectomy in rats

    Directory of Open Access Journals (Sweden)

    Gustavo Barreto de Melo

    2003-12-01

    Full Text Available OBJETIVO: Avaliar os efeitos do omeprazol e do pantoprazol sobre a regeneração hepática após hepatectomia parcial. MÉTODOS: Cinqüenta e oito ratos Wistar machos foram divididos em 4 grupos: Grupo SHAM, Grupo HP, Grupo PANTO e Grupo OMEP. Eles foram submetidos a hepatectomia parcial de 67% (Grupos HP, PANTO e OMEP ou laparotomia (Grupo SHAM. Os fígados foram removidos 32 e 56 horas após a operação. Depois, os animais foram sacrificados. Em todos os grupos, as substâncias (solução salina, omeprazol e pantoprazol foram aplicadas diariamente a partir do momento em que foram operados até o sacrifício. RESULTADOS: O índice de mitose no Grupo SHAM não foi significativo. Trinta e duas horas após a hepatectomia, a contagem de mitoses foi de 1,2 ± 1,09 para o Grupo HP, 1,2 ± 1,6 para o Grupo OMEP e 2,6 ± 3,2 para o Grupo PANTO. Na análise após 56 horas, os valores foram 1,6 ± 0,89 para o HP, 2 ± 1,8 para o OMEP e 2,6 ± 0,54 para o PANTO. Esses resultados não foram estatisticamente significativos. CONCLUSÃO: O omeprazol e o pantoprazol, agentes inibidores da bomba de prótons (H+, K+-ATPase, não interferem na regeneração hepática 32 e 56 horas após hepatectomia parcial a 67% em ratos.PURPOSE: To assess the effects of omeprazole and pantoprazole on liver regeneration after partial hepatectomy. METHODS: Fifty eight male Wistar rats were divided into 4 groups: SHAM, HP, PANTO and OMEP Groups. They were submitted to 67% partial hepatectomy (HP, PANTO and OMEP Groups or laparotomy (SHAM Group. Their livers were removed 32 and 56 hours after the operation. Then, the animals were sacrificed. In all groups, the substances (saline solution, omeprazole and pantoprazole were injected once daily from the moment they were operated on until the time of sacrifice. RESULTS: In SHAM Group the mitotic index was not significant. Thirty two hours after hepatectomy, the mitosis index was 1.2 ± 1.09 in HP Group, 1.2 ± 1.6 in OMEP Group and 2

  3. A Case-Control Study of Esomeprazole Plus Rebamipide vs. Omeprazole Plus Rebamipide on Post-ESD Gastric Ulcers.

    Science.gov (United States)

    Bunno, Maki; Gouda, Kyosuke; Yamahara, Kunihiro; Kawaguchi, Masanori

    2013-01-01

    Endoscopic submucosal dissection (ESD) is useful for treating gastric tumors. Several trials have shown the efficacy of 4 or 8 weeks of proton pump inhibitor (PPI) administration for post-ESD ulcers. However, if the size of the post-ESD ulcer is larger than predicted, PPI administration alone might not be sufficient for the ulcer to heal within 4 weeks. There is no report about the efficacy of post-ESD gastric ulcers by esomeprazole. We examined retrospectively the efficacy of a combination therapy of esomeprazole plus rebamipide, a mucosal-protective antiulcer drug, on the acceleration of post-ESD ulcer healing comparing with omeprazole plus rebamipide. We reviewed the medical records of patients who underwent ESD for gastric neoplasia. We conducted a case-control study to compare the healing rates within 4 weeks effected by esomeprazole plus rebamipide (group E) and omeprazole plus rebamipide (group O). The sizes of the artificial ulcers were divided into normal-sized or large-sized. The baseline characteristics did not differ significantly between the two groups except age and sex. Stage S1 disease was observed in 27.6% and 38.7% of patients after 4 weeks of treatment in the group E and O, respectively. In large-sized artificial ulcers, the healing rate of stage S1 in group E is significantly higher than that in group O in 4 weeks.(25% VS 0%:P = 0.02). The safety and efficacy profiles of esomeprazole plus rebamipide and omeprazole and rebamipide are similar for the treatment of ESD-induced ulcers. In large-sized ulcers, esomeprazole plus rebamipide promotes ulcer healing.

  4. Comparative study of omeprazole, lansoprazole,pantoprazole and esomeprazole for symptom relief in patients with reflux esophagitis

    Institute of Scientific and Technical Information of China (English)

    Ri-Nan Zheng

    2009-01-01

    AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs).METHODS: Two hundred and seventy-four patients with erosive reflux esophagitis were randomized to receive 8 wk of 20 mg omeprazole ( n = 68), 30 mg of lansoprazole ( n = 69), 40 mg of pantoprazole ( n= 69), 40 mg of esomeprazole ( n = 68) once a day in the morning. Daily changes in heartburn and acid reflux symptoms in the first 7 d of administration were assessed using a six-point scale (0: none; 1: mild; 2:mild-moderate; 3: moderate; 4: moderate-severe; 5:severe).RESULTS: The mean heartburn score in patients treated with esomeprazole more rapidly decreased than those receiving other PPI. Complete resolution of heartburn was also more rapid in patients treated with esomeprazole for 5 d compared with omeprazole ( P = 0.0018, P = 0.0098, P = 0.0027, P = 0.0137, P = 0.0069,respectively), lansoprazole ( P = 0.0020, P = 0.0046, P= 0.0037, P = 0.0016, P = 0.0076, respectively), and pantoprazole ( P = 0.0006, P = 0.0005, P = 0.0009, P =0.0031, P = 0.0119, respectively). There were no significant differences between the four groups in the rate of endoscopic healing of reflux esophagitis at week 8.CONCLUSION: Esomeprazole may be more effective than omeprazole, lansoprazole, and pantoprazole for the rapid relief of heartburn symptoms and acid reflux symptoms in patients with reflux esophagitis.

  5. Effects of long-term administration of omeprazole on bone mineral density and the mechanical properties of the bone☆

    Science.gov (United States)

    Yanagihara, Gabriela Rezende; de Paiva, Aline Goulart; Neto, Maurílio Pacheco; Torres, Larissa Helena; Shimano, Antônio Carlos; Louzada, Mário Jefferson Quirino; Annoni, Raquel; de Oliveira Penoni, Álvaro César

    2015-01-01

    Objectives Epidemiological studies have shown a relationship between long-term use of proton pump inhibitors and bone metabolism. However, this relationship has not yet become established. The aim of the present study was to analyze the mechanical properties and bone mineral density (BMD) of rats that were subjected to long-term omeprazole use. Methods Fifty Wistar rats weighing between 200 and 240 g were divided equally into five groups: OMP300 (omeprazole intake at a dose of 300 μmoL/kg/day); OMP200 (200 μmoL/kg/day); OMP40 (40 μmoL/kg/day); OMP10 (10 μmoL/kg/day); and Cont (control group; intake of dilution vehicle). The solutions were administered for 90 consecutive days. After the rats had been sacrificed, their BMD, the mechanical properties of the dissected femurs and their serum Ca++ levels were analyzed. Results The BMD of the OMP300 group was lower than that of the controls (p = 0.006). There was no difference on comparing the OMP200, OMP40 and OMP10 groups with the controls. The maximum strength and rigidity of the femur did not differ in the experimental groups in comparison with the controls. The OMP300 group had a statistically lower serum Ca++ concentration than that of the controls (p = 0.049), but the other groups did not show any difference in relation to the controls. Conclusion Daily intake of 300 μmoL/kg/day of omeprazole decreased the BMD of the femur, but without changes to the rigidity and strength of the femur in adult rats. PMID:26229922

  6. Effects of long-term administration of omeprazole on bone mineral density and the mechanical properties of the bone

    Directory of Open Access Journals (Sweden)

    Gabriela Rezende Yanagihara

    2015-04-01

    Full Text Available OBJECTIVES: Epidemiological studies have shown a relationship between long-term use of proton pump inhibitors and bone metabolism. However, this relationship has not yet become established. The aim of the present study was to analyze the mechanical properties and bone mineral density (BMD of rats that were subjected to long-term omeprazole use.METHODS: Fifty Wistar rats weighing between 200 and 240 g were divided equally into five groups: OMP300 (omeprazole intake at a dose of 300 µmoL/kg/day; OMP200 (200 µmoL/kg/day; OMP40 (40 µmoL/kg/day; OMP10 (10 µmoL/kg/day; and Cont (control group; intake of dilution vehicle. The solutions were administered for 90 consecutive days. After the rats had been sacrificed, their BMD, the mechanical properties of the dissected femurs and their serum Ca++ levels were analyzed.RESULTS: The BMD of the OMP300 group was lower than that of the controls (p = 0.006. There was no difference on comparing the OMP200, OMP40 and OMP10 groups with the controls. The maximum strength and rigidity of the femur did not differ in the experimental groups in comparison with the controls. The OMP300 group had a statistically lower serum Ca++ concentration than that of the controls (p = 0.049, but the other groups did not show any difference in relation to the controls.CONCLUSION: Daily intake of 300 µmoL/kg/day of omeprazole decreased the BMD of the femur, but without changes to the rigidity and strength of the femur in adult rats.

  7. A Solid-Contact Indium(III) Sensor based on a Thiosulfinate Ionophore Derived from Omeprazole

    Energy Technology Data Exchange (ETDEWEB)

    Abbas, Mohammad Nooredeen; Hend Samy Amer [National Research Centre, Cairo (Egypt)

    2013-04-15

    A novel solid-contact indium(III)-selective sensor based on bis-(1H-benzimidazole-5-methoxy-2-[(4-methoxy-3, 5-dimethyl-1-pyridinyl) 2-methyl]) thiosulfinate, known as an omeprazole dimer (OD) and a neutral ionophore, was constructed, and its performance characteristics were evaluated. The sensor was prepared by applying a membrane cocktail containing the ionophore to a graphite rod pre-coated with polyethylene dioxythiophene (PEDOT) conducting polymer as the ion-to-electron transducer. The membrane contained 3.6% OD, 2.3% oleic acid (OA) and 62% dioctyl phthalate (DOP) as the solvent mediator in PVC and produced a good potentiometric response to indium(III) ions with a Nernstian slope of 19.09 mV/decade. The constructed sensor possessed a linear concentration range from 3 Χ 10{sup -7} to 1 Χ 10{sup -2} M and a lower detection limit (LDL) of 1 Χ 10{sup -7} M indium(III) over a pH range of 4.0-7.0. It also displayed a fast response time and good selectivity for indium(III) over several other ions. The sensor can be used for longer than three months without any considerable divergence in potential. The sensor was utilized for direct and flow injection potentiometric (FIP) determination of indium(III) in alloys. The parameters that control the flow injection method were optimized. Indium(III) was quantitatively recovered, and the results agreed with those obtained using atomic absorption spectrophotometry, as confirmed by the f and t values. The sensor was also utilized as an indicator electrode for the potentiometric titration of fluoride in the presence of chloride, bromide, iodide and thiocyanate ions using indium(III) nitrate as the titrant.

  8. [Omeprazole/amoxicillin: improved eradication of Helicobacter pylori in smokers because of N-acetylcysteine].

    Science.gov (United States)

    Zala, G; Flury, R; Wüst, J; Meyenberger, C; Ammann, R; Wirth, H P

    1994-08-09

    Colonization of Helicobacter pylori (HP) beneath the protective film of gastric mucus enables the organism to survive in the hostile environment of the gastric mucosa. N-acetylcysteine (NAC), a sulfhydryl compound with potent mucolytic activity, induces a reduction of gastric barrier mucus thickness of about 75% and reduces mucus viscoelasticity. We therefore tested the hypothesis whether better eradication results could be achieved by addition of NAC to omeprazole/amoxicillin (OME/AMOX). 34 HP positive outpatients with endoscopically documented recurrent duodenal ulcer were included in an ongoing, prospective, randomized trial. Exclusion criteria were: alcoholism, previous gastric surgery, or intake of antibiotics, OME, bismuth salts, corticosteroids or NSAIDs within 4 weeks before study entry. Patients currently smoking > 10 cigarettes/day were classified as smokers. HP infection was confirmed by histology (3 biopsy specimens from gastric antrum and 2 from gastric body; H&E, Giemsa) and at least positive rapid urease test or culture. All 34 patients underwent ulcer therapy with OME (20 mg per day) for 20 days (d 1-20). Group A: in 17 patients (5 females, 12 males, mean age 46 [29-74] years; 8 smokers, 9 nonsmokers) the subsequent eradication therapy, consisting of oral OME (40 mg bid) and AMOX solute (750 mg tid) for 10 days, was combined with NAC solute (2 x 600 mg bid (d 21-30). Group B: 17 patients (2 females, 15 males, mean age 39 [19-70] years; 11 smokers, 6 nonsmokers) underwent eradication therapy without NAC (d 21-30). Control endoscopy was done after a minimal interval of 30 days from the end of treatment.(ABSTRACT TRUNCATED AT 250 WORDS)

  9. Synergy of Omeprazole and Praziquantel In Vitro Treatment against Schistosoma mansoni Adult Worms

    Science.gov (United States)

    Anderson, Leticia; Venancio, Thiago M.; Nakaya, Helder I.; Miyasato, Patrícia A.; Rofatto, Henrique K.; Zerlotini, Adhemar; Nakano, Eliana; Oliveira, Guilherme; Verjovski-Almeida, Sergio

    2015-01-01

    Background Treatment and morbidity control of schistosomiasis relies on a single drug, praziquantel (PZQ), and the selection of resistant worms under repeated treatment is a concern. Therefore, there is a pressing need to understand the molecular effects of PZQ on schistosomes and to investigate alternative or synergistic drugs against schistosomiasis. Methodology We used a custom-designed Schistosoma mansoni expression microarray to explore the effects of sublethal doses of PZQ on large-scale gene expression of adult paired males and females and unpaired mature females. We also assessed the efficacy of PZQ, omeprazole (OMP) or their combination against S. mansoni adult worms with a survival in vitro assay. Principal Findings We identified sets of genes that were affected by PZQ in paired and unpaired mature females, however with opposite gene expression patterns (up-regulated in paired and down-regulated in unpaired mature females), indicating that PZQ effects are heavily influenced by the mating status. We also identified genes that were similarly affected by PZQ in males and females. Functional analyses of gene interaction networks were performed with parasite genes that were differentially expressed upon PZQ treatment, searching for proteins encoded by these genes whose human homologs are targets of different drugs used for other diseases. Based on these results, OMP, a widely prescribed proton pump inhibitor known to target the ATP1A2 gene product, was chosen and tested. Sublethal doses of PZQ combined with OMP significantly increased worm mortality in vitro when compared with PZQ or OMP alone, thus evidencing a synergistic effect. Conclusions Functional analysis of gene interaction networks is an important approach that can point to possible novel synergistic drug candidates. We demonstrated the potential of this strategy by showing that PZQ in combination with OMP displayed increased efficiency against S. mansoni adult worms in vitro when compared with

  10. Omeprazole/antacid-powder suspension--Santarus: Acitrel, Rapinex Powder for oral suspension, SAN 05.

    Science.gov (United States)

    2004-01-01

    Santarus Inc., is developing an immediate-release formulation of omeprazole in combination with an antacid (sodium bicarbonate) as a powder for suspension, known as Acitrel [SAN 05], and also as Rapinex powder for oral suspension. Acitrel is based on technology licensed from the University of Missouri. Santarus have also licensed technology from Tulane and North Carolina Universities relating to potential treatments for GI diseases. Santarus have licensed exclusive, worldwide rights to patent applications covering specific combination-formulations of proton pump inhibitors and antacids for treating various upper GI diseases and disorders. Santarus plans to license development, distribution and marketing rights of Rapinex Powder for oral suspension 20mg outside the US, to one or more well established pharmaceutical companies. The US FDA has requested that Santarus pursue a name other than Rapinex for the product. Santarus is currently discussing potential alternative names for the product with the FDA. Santarus announced positive results, in August 2003, from a phase III trial comparing oral Acitrel (Rapinex 40mg) to intravenous cimetidine in preventing upper GI bleeding in 359 critically ill adult patients. Santarus has also completed an open-label clinical trial in 243 patients, including 97 patients with gastric ulcers, evaluating the safety of Rapinex 40mg for an 8-week period. In connection with the NDA for Rapinex 40mg, Santarus provided notice to the NDA holder for Prilosec delayed-release capsules and related patent owners that Rapinex 40mg does not infringe currently listed patents for Prilosec or that those patents are invalid.

  11. Effect of omeprazole and domperidone on adult asthmatics with gastroesophageal reflux

    Institute of Scientific and Technical Information of China (English)

    Bhavneesh Sharma; Manisha Sharma; Mradul Kumar Daga; Gopal Krishan Sachdev; Elliott Bondi

    2007-01-01

    AIM: To study the effect of combined omeprazole(Ome) and domperidone(Dom) therapy on asthma symptoms and pulmonary function in asthmatics with gastroesoph ageal reflux.METHODS: We selected 198 asthmatics with gastro esophageal reflux diagnosed by 24-h esophageal pH moni toring to receive Ome 20 mg twice daily and Dom 10 mg three times daily or placebo for 16 wk (1:1 double-blind randomization). Spirometry was done at baseline and af ter 16 wk of treatment. The primary outcome measures were: mean daily daytime and nighttime asthma symp tom scores. Mean daily reflux symptom scores, albuterol use as rescue medication (number of puffs), daytime and nighttime peak expiratory flow rate (PEFR), postbroncho dilator forced expiratory volume in 1 second (FEV1) and postbronchodilator forced vital capacity (FVC) were sec ondary outcome measures.RESULTS: Comparison of mean change from baseline between antireflux therapy and placebo groups revealed significant reduction in daytime asthma symptom score (17.4% vs 8.9 %), nighttime asthma symptom score (19.6% vs 5.4%), reflux symptom score (8.7% vs 1.6%) and rescue medication use (23.2% vs 3.1%) after antire flux therapy compared to mean change in placebo group (P < 0.001). There was significant improvement in morn ing PEFR (7.9% vs 0.2%), evening PEFR (9.8% vs 0.5%), FEV1 (11.1% vs 3.78%) and FVC (9.3% vs 1.52%) in the antireflux therapy group compared to placebo on comparing the mean change from baseline after 16 wk (P < 0.01).CONCLUSION: Combined therapy with Ome and Dom in adult asthmatics with gastroesophageal reflux may be beneficial by reducing asthma symptoms, rescuing medi cation use, and improving pulmonary function.

  12. Therapeutic usage of omeprazole and corticoid in a dog with hydrocephalus unresponsive to conventional therapyUso terapêutico da associação do omeprazol com corticóide em um cão com hidrocefalia não-responsiva ao tratamento convencional

    Directory of Open Access Journals (Sweden)

    Alexandre Mendes Amude

    2013-05-01

    Full Text Available Medical therapy for hydrocephalus includes the administration of medications to limit the production of the cerebrospinal fluid (CSF resulting in reduced intracranial pressure (ICP. This report describes the clinical findings in one dog with congenital hydrocephalus that was unresponsive to conventional medical treatment with steroids, but demonstrated good response to omeprazole when this drug was added to the steroid. Omeprazole might decrease the CSF production by about 26% according to experimental studies with healthy dogs, but the usage of the omeprazole in clinical trials with affected dogs such as hydrocephalic animals is lacking. The results of this report might suggest that omeprazole can be used added to steroids to ameliorate the neurological status in dogs with increased ICP by hydrocephalus.O tratamento médico para a hidrocefalia inclui a administração de medicamentos para limitar a produção do fluido cerebroespinhal (FCE, resultando em redução da pressão intracraniana (PIC. Este trabalho descreve os achados clínicos em um cão com hidrocefalia congênita não responsiva ao tratamento médico convencional com esteróides mas que apresentou boa resposta à associação omeprazolesteróides. O omeprazol pode diminuir a produção de FCE em cerca de 26% de acordo com estudos experimentais realizados com cães saudáveis. Porém, o uso do omeprazol em ensaios clínicos com cães enfermos, como os animais hidrocefálicos, não é descrito. Os resultados deste trabalho sugerem que o omeprazol pode ser empregado em associação ao corticóide para melhorar o estado neurológico em cães com aumento da PIC devido à hidrocefalia.

  13. Simultaneous pharmacokinetics evaluation of human cytochrome P450 probes, caffeine, warfarin, omeprazole, metoprolol and midazolam, in common marmosets (Callithrix jacchus).

    Science.gov (United States)

    Uehara, Shotaro; Inoue, Takashi; Utoh, Masahiro; Toda, Akiko; Shimizu, Makiko; Uno, Yasuhiro; Sasaki, Erika; Yamazaki, Hiroshi

    2016-01-01

    1. Pharmacokinetics of human cytochrome P450 probes (caffeine, racemic warfarin, omeprazole, metoprolol and midazolam) composite, after single intravenous and oral administrations at doses of 0.20 and 1.0 mg kg(-1), respectively, to four male common marmosets were investigated. 2. The plasma concentrations of caffeine and warfarin decreased slowly in a monophasic manner but those of omeprazole, metoprolol and midazolam decreased extensively after intravenous and oral administrations, in a manner that approximated those as reported for pharmacokinetics in humans. 3. Bioavailabilities were ∼100% for caffeine and warfarin, but midazolam was 4% in marmosets, presumably because of contribution of marmoset P450 3A4 expressed in small intestine and liver, with a high catalytic efficiency for midazolam 1'-hydroxylation as evident in the recombinant system. 4. These results suggest that common marmosets, despite their rapid clearance of some human P450 probe substrates, could be an experimental model for humans and that marmoset P450s have functional characteristics that differ from those of human and/or cynomolgus monkey P450s in some aspects, indicating their importance in modeling in P450-dependent drug metabolism studies in marmosets and of further studies.

  14. A Single Gradient Stability-Indicating Reversed-Phase LC Method for the Estimation of Impurities in Omeprazole and Domperidone Capsules.

    Science.gov (United States)

    Seshadri, Raja Kumar; Raghavaraju, Thummala Veera; Chakravarthy, Ivon Elisha

    2013-01-01

    A gradient reversed-phase liquid chromatographic (RP-LC) method was developed for the quantitative estimation of impurities in the pharmaceutical dosage form of Omeprazole and Domperidone capsules. The developed method is a stability-indicating test method for the estimation of impurities generated during the formulation and storage of Omeprazole and Domperidone capsules. The chromatographic separation was achieved on a column packed with octadecyl silane, having a column length of 250 mm and diameter of 4.6 mm with a particle size of 5 μm, and by following a gradient program using a combination of a monobasic potassium phosphate buffer (0.05M) and acetonitrile. Since the spectral properties were similar, both compounds' individual impurities were estimated at 285 nm. Forced degradation studies were performed on Omeprazole pellets (enteric coated) and Domperidone pellets (SR coated) encapsulated in size '1' hard gelatin capsules. Omeprazole and Domperidone were degraded using acid hydrolysis (0.1 N hydrochloric acid), base (0.1 N sodium hydroxide), oxidation (50% hydrogen peroxide), heat (105 °C), and UV light (254 nm). The established method was validated and found to be linear, accurate, precise, specific, robust, and rugged.

  15. [Various mechanisms of cytoprotective effect of omeprazole and low intensity laser radiation on the gastroduodenal mucosa in the treatment of patients with duodenal ulcer].

    Science.gov (United States)

    Akhmadkhodzhaev, A M

    2002-01-01

    Clinical studies were made in 130 patients with duodenal ulcer in the phase of exacerbation of the disease. There were 98 men and 32 women who ranged from 17 to 50 years old. Results of examination of 7 essentially healthy subjects were regarded as control. The patients were divided into three groups. Group I patients (n = 48) received a conventional therapy; in group II patients, the adopted therapy was supplemented by omeprazol, 20 mg twice daily, group III patients (n = 43) were (in addition to the above therapeutic regimen) exposed to a session of endoscopic low-intensity laser irradiation (LILI) for 5 min (overall 6 to 8 LILI procedures). It has been ascertained that omeprazol exerts a cytoprotective effect on the mucozal barrier of the gastroduodenal zone brought about by increase in the synthesis of glucoproteins in the mucous membrane, improvement of the water-and-elastic properties, and enhancement of resistance of the mucosal barrier to the action of the aggressive factors. Administration of endoscopic LILI treatments in DU patients has also been found out to have a cytoprotective effect but superior to omeprazol. A protective action of LILI is believed to be caused by stimulation of synthesis of the most important components of glycoproteins. A cytoprotective effect of omeprazol and endoscopic LILI is ccompanied by a significant shortening of time for the clinical symptoms to get dispelled, the ulcer cicatrization frequency increased.

  16. Influence of Food on the Bioavailability of an Enteric-Coated Tablet Formulation of Omeprazole 20 mg Under Repeated Dose Conditions

    Directory of Open Access Journals (Sweden)

    ABR Thomson

    1997-01-01

    Full Text Available The objective of this study was to investigate the influence of food on the bioavailability of omeprazole (20 mg given as an enteric-coated tablet under repeated dose conditions. This open randomized crossover study consisted of three seven-day treatment periods, each separated by a drug-free period. During each treatment period an enteric-coated tablet of omeprazole was taken once daily either under fasting conditions, or immediately before or after a standardized breakfast. On the last day of each treatment period, blood samples for the determination of plasma omeprazole concentrations were collected at baseline and at predetermined intervals over the 24 h period following drug administration. Fifty-seven male and female subjects, aged 18 to 52 years, completed the study according to the protocol. No statistically significant differences were found when comparing either the before breakfast or after breakfast treatment regimens with the fasting regimen for the estimated mean area under the plasma concentration-time curve (AUC. The maximum plasma concentration was not found to differ significantly among any of the treatment regimens. However, the lower limit of the CI for the comparison of fasting/before breakfast was not contained within the limits of bioequivalence. The time to reach maximum plasma concentration was significantly different when fasting and after breakfast regimens were compared. Thus, under repeated dose conditions, food has no influence on the bioavailability (expressed as AUC of omeprazole given as the enteric-coated tablet formulation.

  17. Randomised clinical trial: sodium alginate oral suspension is non-inferior to omeprazole in the treatment of patients with non-erosive gastroesophageal disease.

    Science.gov (United States)

    Chiu, C-T; Hsu, C-M; Wang, C-C; Chang, J-J; Sung, C-M; Lin, C-J; Chen, L-W; Su, M-Y; Chen, T-H

    2013-11-01

    The burden of gastroesophageal reflux disease (GERD) is increasing in the Asia area and the majority of GERD patients have non-erosive reflux disease (NERD). To evaluate the efficacy and safety of sodium alginate suspension compared to omeprazole in adult subjects with NERD. In this 4-week, double-blind, parallel study, 195 NERD subjects were randomised to one of two treatment groups: sodium alginate suspension 20 mL three times a day and omeprazole 20 mg once daily. The primary efficacy endpoint was the percentage of patients achieving adequate heartburn or regurgitation relief at day 28 assessed by patient diary. The secondary efficacy endpoints included percentage of patients achieving adequate heartburn or regurgitation relief, change from baseline of the Reflux Disease Questionnaire total score at day 14 and 28 from baseline, and patients' overall satisfaction. In this study, 183 subjects were included in the intent-to-treat population, and 172 subjects were included in the per-protocol population. Non-inferiority of sodium alginate to omeprazole was demonstrated in the intent-to-treat population [difference, 2.7% (53.3% vs. 50.5%, P = 0.175), 95% lower confidence interval -11.9%, above the preset margin of -19%]. All of the secondary efficacy endpoints were comparable between two groups. The incidence of adverse event was relatively low and there was no difference between the two groups (5.4% vs. 5.5% for sodium alginate vs. omeprazole). No severe adverse event was noted in this study. The study showed that sodium alginate was as effective as omeprazole for symptomatic relief in patients with non-erosive reflux disease (Clinicaltrials.gov NCT01338077). © 2013 John Wiley & Sons Ltd.

  18. The comparison of extemporaneous preparations of omeprazole, pantoprazole oral suspension and intravenous pantoprazole on the gastric pH of critically ill-patients

    Directory of Open Access Journals (Sweden)

    Yasamin Dabiri

    2015-01-01

    Full Text Available Background: Stress-related mucosal disease occurs in many critically ill-patients within 24 h of admission. Proton pump inhibitor therapy has been documented to produce more potent inhibition of gastric acid secretion than histamine 2 receptor antagonists. This study aimed to compare extemporaneous preparations of omeprazole, pantoprazole oral suspension and intravenous (IV pantoprazole on the gastric pH in intensive care unit patients. Materials and Methods: This was a randomized single-blind-study. Patients of ≥ 16 years of age with a nasogastric tube, who required mechanical ventilation for ≥ 48 h, were eligible for inclusion. The excluded patients were those with active gastrointestinal bleeding, known allergy to omeprazole and pantoprazole and those intolerant to the nasogastric tube. Fifty-six patients were randomized to treatment with omeprazole suspension 2 mg/ml (40 mg every day, pantoprazole suspension 2 mg/ml (40 mg every day and IV pantoprazole (40 mg every day for up to 14 days. Gastric aspirates were sampled before and 1-2.5 h after the drug administration for the pH measurement using an external pH meter. Data were analyzed using SPSS (version 21.0. Results: In this study, 56 critically ill-patients (39 male, 17 female, mean age: 61.5 ± 15.65 years were followed for the control of the gastric pH. On each of the 14 trial days the mean of the gastric pH alteration was significantly higher in omeprazole and pantoprazole suspension-treated patients than in IV pantoprazole-treated patients (P < 0.001. Conclusion: Omeprazole and pantoprazole oral suspension are more effective than IV pantoprazole in increasing the gastric pH.

  19. A head to head comparison of oral vs intravenous omeprazole for patients with bleeding peptic ulcers with a clean base, flat spots and adherent clots

    Institute of Scientific and Technical Information of China (English)

    (S)erif Y(i)lmaz; Kadim Bayan; Yekta Tüzün; Mehmet Dursun; Fikri Canoru(c)

    2006-01-01

    AIM: To compare the effect of intravenous and oral omeprazole in patients with bleeding peptic ulcers without high-risk stigmata.METHODS: This randomized study included 211 patients [112 receiving iv omeprazole protocol (Group 1),99 receiving po omeprazole 40 mg every 12 h (Group 2)] with a mean age of 52.7. In 144 patients the ulcers showed a clean base, and in 46 the ulcers showed fiat spots and in 21 old adherent clots. The endpoints were re-bleeding, surgery, hospital stay, blood transfusion and death. After discharge, re-bleeding and death were reevaluated within 30 d.RESULTS: The study groups were similar with respect to baseline characteristics. Re-bleeding was recorded in 5 patients of Group 1 and in 4 patients of Group 2 (P = 0.879). Three patients in Group 1 and 2 in Group 2 underwent surgery (P = 0.773). The mean length of hospital stay was 4.6 ± 1.6 d in Group 1 vs 4.5 ± 2.6 d in Group 2 (P = 0.710); the mean amounts of blood transfusion were 1.9 ± 1.1 units in Group 1 vs 2.1 ± 1.7 units in Group 2 (P = 0.350). Four patients, two in each group died (P = 0.981). After discharge, a new bleeding occurred in 2 patients of Group 1 and in 1 patient of Group 2, and one patient from Group 1 died.CONCLUSION: We demonstrate that the effect of oral omeprazole is as effective as intravenous therapy in terms of re-bleeding, surgery, transfusion requirements,hospitalization and mortality in patients with bleeding ulcers with low risk stigmata. These patients can be treated effectively with oral omeprazole.

  20. DEVELOPMENT AND VALIDATION OF A RP- HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF OMEPRAZOLE AND CINITAPRIDE IN BULK AND CAPSULE DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    G. Nagarajan

    2013-02-01

    Full Text Available A simple reversed-phase high-performance liquid chromatographic (RP-HPLC method has been developed and validated for simultaneous determination of Omeprazole and Cinitapride in bulk and Capsule dosage form. Chromatographic analysis was performed on a Symmetry C8 column (150x 4.5 mm, 5μm column ambient temperature with a mixture of mixed phosphate buffer and Acetonitrile in the ratio 50:50 (mixed phosphate buffer preparation; 1.625 gm of potassium Dihydrogen phosphate and 0.3 gm of Di potassium hydrogen phosphate in 550 mL HPLC grade water, pH= 6.0 adjust with phosphoric acid as mobile phase, at a flow rate of 1.0 mL min-1. UV detection was performed at 287 nm. The method was validated for accuracy, precision, specificity, linearity and sensitivity. The retention times of Omeprazole and Cinitapride were 2.49 and 3.650 min, respectively. Calibration plots were linear over the concentration ranges 5–30 μg mL-1 and 0.75-4.5 μg mL-1 for Omeprazole and Cinitapride, respectively. The Limit of detection was 1.43570 and 0.086 µg mL-1 and the quantification limit was 4.35 µg mL-1 and 0.26 µg mL-1 for Omeprazole and Cinitapride, respectively. The accuracy of the proposed method was determined by recovery studies and found to be 98.62% to 100.37%. Commercial capsule formulation was successfully analyzed using the developed method and the proposed method is applicable to routine analysis of determination of Omeprazole and Cinitapride in bulk and capsule dosage form.

  1. Inhibition of gastric secretion by omeprazole and efficiency of calcium carbonate on the control of hyperphosphatemia in patients on chronic hemodialysis.

    Science.gov (United States)

    Hardy, P; Sechet, A; Hottelart, C; Oprisiu, R; Abighanem, O; Said, S; Rasombololona, M; Brazier, M; Moriniere, P; Achard, J M; Pruna, A; Fournier, A

    1998-07-01

    Contradictions exist in the literature regarding the effect of gastric secretion inhibition on phosphate absorption. In healthy controls, omeprazole would decrease the hyperphosphatemia or the hyperphosphaturia induced by an acute phosphate load, suggesting an inhibition of phosphate absorption. In chronic hemodialysis patients, gastric hypersecretion is associated with hyperphosphatemia, but inhibition of gastric hypersecretion by ranitidine in those receiving calcium carbonate (CaCO3) as a phosphate binder would paradoxically exacerbate their hyperphosphatemia. Because of these conflicting observations, we performed an open crossover study on 16 chronic stable hemodialyzed patients with a daily mean intake of 9.4+/-4 g of CaCO3, and we compared the plasmatic predialysis levels of phosphate, calcium, protides, bicarbonates, intact parathyroid hormone (PTH), urea, and creatininemia during 2 successive periods of 2 months, the first one without omeprazole and the second one with 20 mg omeprazole intake in the morning. Phosphatemia increased with omeprazole but not significantly from 1.80+/-0.38 to 1.89+/-0.42 mM whereas corrected calcemia decreased significantly (p = 0.04) from 2.41+/-0.18 to 2.36+/-0.16 mM as did bicarbonatemia from 26.7+/-3.5 to 25.7+/-3.1 mM (p omeprazole increases the plasmatic phosphate predialytic level but in a nonsignificant way. This increase may be explained by a slight but significant concomitant decrease of calcemia and bicarbonatemia. These results do not support the phosphate binding efficiency of CaCO3 being decreased by the inhibition of gastric acid secretion.

  2. Dilated intercellular spaces in gastroesophageal reflux disease patients and the changes of intercellular spaces after omeprazole treatment

    Institute of Scientific and Technical Information of China (English)

    XUE Yan; ZHOU Li-ya; LIN San-ren

    2008-01-01

    Background Gastroesophageal reflux disease (GERD) is a common disorder. Dilation of intercellular spaces of esophageal epithelium has been revealed at transmission electron microscopy both in the rabbit acid-perfused esophagus and in esophageal biopsies from GERD patients. This study aimed to observe the changes of the intercellular spaces of squamous epithelium of lower esophagus in patients with GERD and the changes of intercellular spaces of patients with erosive esophagitis (EE) before and after omeprazole treatment.Methods Outpatients having GERD symptoms for more than 3 months and volunteers were collected. All of them underwent gastroendoscopy and 24-hour ambulatory pH monitoring. Biopsies were taken from the lower esophagus (2 cm above Z-line) for electron microscope examination. Five healthy volunteers, six non-erosive reflux disease (NERD) patients, and five EE patients were enrolled. Intercellular spaces of GERD patients and controls were calculated. Then we selected 20 patients with EE diagnosed by gastroendoscopy. All of them were treated with omeprazole (Losec, 20 mg bid) for 4 weeks then underwent gastroendoscopy again. Biopsies were taken from 2 cm above Z-line for electron microscope examination. All the patients completed the questionnaire about reflux symptoms before and after treatment.Results Intercellular spaces of esophageal epithelial cell in volunteers, NERD patients and EE patients were (0.37±0.07) μm, (1.31±0.08) μm, and (1.33±0.14) μm, respectively, with significant differences between the control group and the NERD group (P=0.000). In the 20 EE patients, the mean intercellular space before treatment was (1.14±0.15) μm. After treatment the intercellular space was (0.51±0.18) μm, a significant difference compared with pre-treatment measurements (P=0.000).Conclusions Dilated intercellular spaces (DIS) were seen in both NERD and EE cases. The dilated intercellularspaces of esophageal epithelium in EE patients could be recovered

  3. Omeprazole, Furazolidone, and Tetracycline: an eradication treatment for resistant H. pylori in Brazilian patients with peptic ulcer disease Omeprazol, Tetraciclina e Furazolidona, um tratamento para erradicação do H. pylori resistente em pacientes ulcerosos do Brasil

    Directory of Open Access Journals (Sweden)

    Fernando Marcuz Silva

    2002-09-01

    Full Text Available OBJECTIVES: To determine the efficacy of a simple, short-term and low-cost eradication treatment for Helicobacter pylori (H. pylori using omeprazole, tetracycline, and furazolidone in a Brazilian peptic ulcer population, divided into 2 subgroups: untreated and previously treated for the infection. PATIENTS AND METHODS: Patients with peptic ulcer disease diagnosed by endoscopic examination and infected by H. pylori diagnosed by the rapid urease test (RUT and histological examination, untreated and previously unsuccessfully treated by macrolides and nitroimidazole, were medicated with omeprazole 20 mg daily dose and tetracycline 500 mg and furazolidone 200 mg given 3 times a day for 7 days. Another endoscopy or a breath test was performed 12 weeks after the end of treatment. Patients were considered cured of the infection if a RUT and histologic examination proved negative or a breath test was negative for the bacterium. RESULTS: Sixty-four patients were included in the study. The women were the predominant sex (58%; the mean age was 46 years. Thirty-three percent of the patients were tobacco users, and duodenal ulcer was identified in 80% of patients. For the 59 patients that underwent follow-up examinations, eradication was verified in 44 (75%. The eradication rate for the intention-to-treat group was 69%. The incidence of severe adverse effects was 15%. CONCLUSION: The treatment provides good efficacy for H. pylori eradication in patients who were previously treated without success, but it causes severe adverse effects that prevented adequate use of the medications in 15% of the patients.OBJETIVO: Testar a eficácia de um esquema simplificado e de baixo custo para erradicação do H. pylori utilizando omeprazol, tetraciclina e furazolidona, em uma população de ulcerosos do Brasil, já tratados e não tratados previamente para a infecção. PACIENTES E MÉTODOS: Pacientes portadores de úlcera péptica, documentada por exame endoscópico e

  4. Furazolidona, tetraciclina e omeprazol: uma alternativa de baixo custo para erradicação de Helicobacter pylori em crianças Furazolidone, tetracycline and omeprazole: a low-cost alternative for Helicobacter pylori eradication in children

    Directory of Open Access Journals (Sweden)

    Rodrigo Strehl Machado

    2008-04-01

    Full Text Available OBJETIVOS: Avaliar furazolidona, tetraciclina e omeprazol como tratamento de primeira linha para Helicobacter pylori em crianças com sintomas digestivos. MÉTODOS: Ensaio clínico aberto, prospectivo e consecutivo. O estudo incluiu pacientes acima de 8 anos com dispepsia funcional, dor abdominal funcional, anormalidades histológicas graves (metaplasia intestinal, atrofia gástrica ou linfoma do tecido linfóide associado às mucosas ou úlcera péptica. A presença de H. pylori foi definida com base em exame histológico e teste da urease. O regime medicamentoso consistiu de um tratamento de 7 dias com omeprazol, tetraciclina (ou doxiciclina e furazolidona duas vezes por dia. A erradicação foi avaliada através de endoscopia digestiva alta 2 meses após o tratamento (exame histológico e teste da urease. Avaliações clínicas posteriores foram realizadas 7 dias e 2 meses após o tratamento. RESULTADOS: Foram incluídos 36 pacientes (21 meninas/15 meninos. A idade variou de 8 a 19 anos (média de 12,94+2,89 anos. Na análise por intenção de tratar (n = 36, a taxa de erradicação foi de 83,3% (IC95% 77,1-89,5, ao passo que na análise por protocolo (n = 29, foi de 89,7% (IC95% 84,6-94,7. A adesão foi melhor quando se utilizou doxiciclina, mas as taxas de sucesso foram semelhantes para as duas tetraciclinas. Não houve nenhuma variável associada à falha no tratamento. Foram relatados efeitos colaterais em 17 pacientes (47,2%, principalmente dor abdominal (11/30,5%, náusea (sete/19,4% e vômitos (cinco/13,9%. CONCLUSÃO: A terapia tripla com furazolidona e tetraciclina é uma alternativa de baixo custo para o tratamento da infecção pelo H. pylori.OBJECTIVE: To evaluate furazolidone, tetracycline and omeprazole as first line therapy for Helicobacter pylori in children with digestive symptoms. METHODS: Prospective and consecutive open trial. The study included patients older than 8 years old with functional dyspepsia, functional

  5. Effect of various salts on the stability of lansoprazole, omeprazole, and pantoprazole as determined by high-performance liquid chromatography.

    Science.gov (United States)

    Ekpe, A; Jacobsen, T

    1999-09-01

    A fast and reproducible reverse-phase high-performance liquid chromatography (HPLC) assay method has been developed for the simultaneous quantitation of omeprazole, lansoprazole, and pantoprazole. The three compounds were monitored at 280 nm using Zorbax Eclipse XDB C8 (5 microns, 150 cm x 4.6 mm i.d.) and a mobile phase consisting of 700:300 phosphate buffer:acetonitrile with the pH adjusted to 7.0 with phosphoric acid. The method was used to study the effect of pH and various salts on the stability of the three compounds. The pH rate profile curve showed that pantoprazole was the most stable compound and lansoprazole the least stable. The stabilities of the compounds in salt solutions were found to be in the following order: phosphate buffer bicarbonate < sodium chloride < water. The rate of degradation had a direct relationship with the H+ and salt concentration.

  6. Prescripción, dispensación y sustitución de recetas de omeprazol

    Directory of Open Access Journals (Sweden)

    Vaquero M. B.

    2003-01-01

    Full Text Available Objetivo: Comprobar y cuantificar, para un principio activo concreto (omeprazol 20 mg, y para unos médicos de atención primaria y oficinas de farmacia seleccionados, si las especialidades farmacéuticas prescritas en recetas oficiales de la Seguridad Social coinciden o no con las especialidades farmacéuticas dispensadas, o bien la dispensación se ha efectuado a criterio del farmacéutico al ir la receta prescrita en denominación oficial española (DOE, calculando el coste de las recetas en cada supuesto, expresado en DDD. Método: Revisión de 592 recetas oficiales de la Seguridad Social de un principio activo seleccionado (omeprazol 20 mg, prescritas por 56 médicos de atención primaria con alta prescripción de este principio activo, y dispensadas en 16 oficinas de farmacia. Resultados: Las recetas en que se respetó la prescripción del médico (50% de los casos resultaron ser más baratas que las prescritas en DOE y dispensadas EFG por el farmacéutico a su criterio (36% de los casos. En el supuesto de recetas en las que se produjeron sustituciones de la especialidad prescrita (14% de los casos, se dispensó en todos los casos una EFG y en el 76% fue de especialidades más caras. Conclusiones: Los resultados demuestran que el médico prescriptor valora el coste de la especialidad farmacéutica a la hora de prescribir y se decanta por especialidades más baratas aunque no sean EFG. El farmacéutico, cuando dispensa a su criterio o sustituye la especialidad prescrita, lo hace siempre por una EFG que en la mayoría de los casos resultó ser más cara.

  7. Acute Coronary Syndromes, Gastrointestinal Protection, and Recommendations Regarding Concomitant Administration of Proton-Pump Inhibitors (Omeprazol/Esomeprazole) and Clopidogrel.

    Science.gov (United States)

    Lozano, Iñigo; Sanchez-Insa, Esther; de Leiras, Sergio Rodríguez; Carrillo, Pilar; Ruiz-Quevedo, Valeriano; Pinar, Eduardo; Gopar-Gopar, Silvia; Bayon, Jeremías; Mañas, Pilar; Lasa, Garikoitz; CruzGonzalez, Ignacio; Hernandez, Felipe; Fernandez-Portales, Javier; Fernandez-Fernandez, Javier; Pérez-Serradilla, Ana; de la Torre Hernandez, José M; Gomez-Jaume, Alfredo

    2016-02-01

    The Food and Drug Administration and the European Medicines Agency sent a warning in 2010 discouraging the concomitant use of clopidogrel with omeprazole or esomeprazole. The purpose is to know the gastroprotective approach in patients with acute coronary syndrome (ACS) and the level of follow-up of the alert. In 17 hospitals with catheterization laboratory in Spain, 1 per region, we studied 25 consecutive patients per hospital whose diagnosis of discharge since October 1, 2013, had been any type of ACS. We analyzed their baseline clinical profile, the gatroprotective agents at admission and discharge and the antiplatelet therapy at discharge. The number of patients included was 425: age 67.2 ± 12.5 years, women 29.8%, diabetes 36.5%. The patients presented unstable angina in 21.6%, non-ST-elevation myocardial infarction in 35.3% and ST-elevation myocardial infarction in 43.1%. Conservative approach was chosen in 17.9%, bare-metal stents 32.2%, ≥ 1 drug-eluting stent 48.5%, and surgery 1.4%. Aspirin was indicated in 1.9%, aspirin + clopidogrel 73.6%, aspirin + prasugrel 17.6%, and aspririn + ticagrelor 6.8%. Gastroprotective agents were present in 40.2% patients at admission and this percentage increased to 93.7% at discharge. Of the 313 (73.6%) on clopidogrel in 96 (30.6%) was combined with omeprazole and 3 (0.95%) with esomeprazole, whereas the most commonly used was pantoprazole with 190 patients (44.7%). In conclusion, almost the totality of the patients with an ACS receive gastroprotective agents at the moment of discharge, most of them with proton-pump inhibitors. In one every 3 cases of the patients who are on clopidogrel, the recommendation of the Food and Drug Administration and the European Medicines Agency is not followed.

  8. Eradication of Helicobacter pylori in Children by Triple Therapy Regimens of Amoxicillin, Omeprazole, and Clarithromycin or Azithromycin

    Directory of Open Access Journals (Sweden)

    Mohammad Reza Esmaeili-Dooki

    2015-12-01

    Full Text Available Background and Objectives: The present study aimed to evaluate the effect of classical and azithromycin-containing triple therapy eradication regimen against H. Pylori in children, and to determine the level of patients’ tolerance. Patients and Methods: This single clinical trial was performed in 2014 on 2 to 15 years old children. All children, in whom H. Pylori infection was confirmed through multiple biopsies of the stomach and required treatment, were enrolled in the study. H. Pylori-positive patients were treated alternately with two different drug regimens; Group OCA received clarithromycin 7.5 mg/kg/day every 12 hours for 10 days, amoxicillin 50 mg/kg/day every 12 hours for 10 days, and omeprazole 1 mg/kg/day every 12 hours for two weeks, and Group OAA received azithromycin 10 mg/kg/day once a day (before meal for 6 days along with amoxicillin and omeprazole. Four to six weeks after completion of treatment, patients’ stool was tested for H. Pylori through the monoclonal method using the Helicobacter antigen quick kit. Results: There were no significant differences between the two groups regarding gender and age of patients. Based on ITT analysis, the therapeutic response in the OAA and OCA groups were 56.2% and 62.5%, respectively (P = 0.40. Drug adverse effects were 15.6% in the OCA and 3.1% in the OAA group (P = 0.19. Conclusions: The therapeutic response was seen in more than half of the patients treated with triple therapy of H. Pylori eradication regimen including azithromycin or clarithromycin, and there was no significant difference between the two treatment groups.

  9. 奥美拉唑知识产权保护策略分析%Analysis of omeprazole intellectual property protection strategy

    Institute of Scientific and Technical Information of China (English)

    沙宇慧; 李玉丹; 杨悦

    2013-01-01

    The inntellectual property strategies maximize the economic return of the proton pump inhibitor omeprazole. This paper gives pharmaceutical companies some references through analyzing the intellectual property strategies implemented by AstraZeneca to protect omeprazole in U. S.%阿斯利康公司的知识产权保护策略实现了质子泵抑制剂奥美拉唑的收益最大化,值得制药企业借鉴.文中分析了阿斯利康公司在美国对奥美拉唑采取的知识产权保护策略,以期为制药企业提供参考.

  10. A terapêutica com o omeprazol: avaliação da potencial relação com a suscetibilidade ao cancro

    OpenAIRE

    Inácio, Ana Filipa Ferreira da Costa Palma

    2012-01-01

    Dissertação de mest., Ciências Farmacêuticas, Faculdade de Ciências e Tecnologia, Univ. do Algarve, 2012 O omeprazol, principal benzimidazol substituído utilizado na inibição da secreção gástrica, através do bloqueio da ATPase da célula parietal, é um dos 10 fármacos mais prescritos do mundo. Farmacodinamicamente aliciante, dada a sua extraordinária seletividade química, o omeprazol foi um sucesso imediato, desde o seu lançamento, em 1988. Para além da sua eficácia altamente satisfatória, ...

  11. Severe bradycardia caused by omeprazole: 4 case reports%奥美拉唑致严重心动过缓4例

    Institute of Scientific and Technical Information of China (English)

    钟建玲; 陈仕珠; 谢波

    2011-01-01

    Four male patients (aged 20,40,22, and 28 years) with chronic superficial gastritis or duodenal ulcer or gastric ulcer received omeprazole 20 mg twice daily. Three of them were given oral omeprazole alone. One of them received combined treatment with omeprazole, azithromycin, and colloidal bismmth pectin. Two days later, they developed dizziness, fatigue, chest distress, and short of breath. Their heart rate decreased to 44 beats/min, 46 beats /min, 46 beats /min, and 44 beats /min, respectively. After discontinuation of omeprazole and administration of IM atropine 0.5 mg 3 times a day, four patients' heart rate returned to baseline.%4例男性患者(年龄分别为20、40、22和28岁)分别因慢性浅表性胃炎、十二指肠球部溃疡或胃溃疡服用奥美拉唑20 mg,2次/d,其中3例单独口服奥美拉唑,1例合并应用奥美拉唑、阿奇霉素和胶体果胶铋.2d后均出现头晕、乏力、胸闷、气短等症状,心率分别下降为44、46、46和44 次/min.停用奥美拉唑并肌内注射阿托品0.5 mg,3次/d后,4例患者心率均恢复至用药前水平.

  12. 奥美拉唑不良反应文献分析%Literature Analysis of Omeprazole-induced Adverse Drug Reactions

    Institute of Scientific and Technical Information of China (English)

    陈颖; 封宇飞

    2011-01-01

    目的:探讨奥美拉唑不良反应发生的规律及特点,为临床合理用药提供参考.方法:通过中国知网(CNKI)的中国医院知识仓库(CHKD)期刊全文数据库及万方数据库检索到2000~2010年有关奥美拉唑致不良反应的有效文献,并按患者性别、年龄、原患疾病与过敏史、给药途径、累及器官或系统及临床表现等方面进行统计、分析.结果:收集奥美拉唑所致不良反应50例,其中,不良反应以过敏性反应和血液系统反应最多.结论:奥美拉唑引起的不良反应临床表现复杂多样,其发生与多种因素有关,值得临床医师关注.%Objective: To explore the regularity and characteristics of ADRs induced by omeprazole. Method; Based on the CHKD and Wanfang database,literatures about omeprazole- induced ADRs from 2000 to 2010 were collected and statistically analyzed in respect of patients'gender,age,case history,administration route,clinical manifestation. Re-Sult-.The most ADRs were anaphylactic reactions and hematological system damage. Conclusion; ADRs induced by omeprazole presented complicated and various symptoms owing to different reasons. Clinical doctors should pay more attention to the omeprazole-induced ADRs.

  13. 35例奥美拉唑不良反应分析%Analyse 35 Cases of Adverse Reactions in Omeprazole

    Institute of Scientific and Technical Information of China (English)

    郭晶

    2015-01-01

    目的:探讨奥美拉唑不良反应(ADR)的发生规律和特点,为临床合理用药提供参考。方法对2013年4月~2014年10月我院发生的35例奥美拉唑所致不良反应进行分类与分析。结果奥美拉唑不良反应的临床表现包括白细胞减少、变态反应、过敏性休克、乳腺增生,及血液系统、内分泌系统、消化系统、皮肤等。结论应加强对奥美拉唑用药后的监测,应重视其不良反应,以保障患者的用药安全。%Objective To investigate the regular pattern and characteristic caused by the adverse drug reactions(ADR)in omeprazole,in order to provide reference for rational clinical drug use. Methods Analyzed the 35 patients’cases caused by the adverse drug reactions(ADR)in omeprazole which were chosen from April 2013 to Oct. 2014. Results The adverse reactions of omeprazole included leukopenia,al ergy,anaphylactic shock,hyperplasia of mammary glands,and the blood system,endocrine system,digestive system,skin,etc. Conclusion To strengthen the monitoring of the drug omeprazole,more attention should be paid on its adverse reactions in order to ensure the patients' medication safety.

  14. Omeprazole-based triple therapy with low-versus high-dose of clarithromycin plus amoxicillin for H pylori eradication in Iranian population

    Institute of Scientific and Technical Information of China (English)

    Ali Asghar Keshavarz; Homayoon Bashiri; Mahtab Rahbar

    2007-01-01

    AIM: To investigate the efficacy and tolerability of Hpylori eradication in an omeprazole-based triple therapy with high- and low-dose of clarithromycin and amoxicillin.METHODS: One hundred and sixty H pylori positive patients were randomly assigned to two groups based on the following 2 wk investigation; (1) group A or low-dose regimen received omeprazole 20 mg b.i.d, clarithromycin 250 mg b.i.d and amoxicillin 500 mg b.i.d; and (2) group B or high-dose regimen received omeprazole 20 mg b.i.d, clarithromycin 500 mg b.i.d and amoxicillin 1000 mg b.i.d. During the study H pylori status was assessed by histology and rapid urease test prior and by 13C-urea breath test 6 wk after the therapy. Standard questionnaires were administered to determine the compliance to treatment and possible adverse events of therapy. Data were subject to % to compare the eradication rates in the two groups. The significant level of 95% (P≤0.05) was considered statistically different.RESULTS: We found that the per-protocol eradication rate was 88% (68/77) in group A, and 89% (67/75) in group B. The intension-to-treat eradication rate was 85% (68/80) in group A and 83.75% (67/80) in group B. Overall adverse events were 26% in group A and 31% in group B. The adverse events were generally mild in nature and tolerated well in both groups with a compliance of 98% in group A vs 96% in group B.CONCLUSION: The omeprazole-based low dose regimen of clarithromycin and amoxicillin for two weeks in H pylori eradication is as effective as high dose regimen in Iranian population.

  15. Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole on nanocrystalline titania films in alkaline media: Effect of applied electrical bias on degradation and transformation products

    Energy Technology Data Exchange (ETDEWEB)

    Tantis, Iosif [Department of Chemical Engineering, University of Patras, Caratheodory 1, University Campus, GR-26504 Patras (Greece); Bousiakou, Leda [Department of Physics and Astronomy, King Saud University, Riyadh (Saudi Arabia); Department of Automation Engineering, Technological Educational Institute of Pireaus, GR-12244 Athens (Greece); Frontistis, Zacharias; Mantzavinos, Dionissios [Department of Chemical Engineering, University of Patras, Caratheodory 1, University Campus, GR-26504 Patras (Greece); Konstantinou, Ioannis; Antonopoulou, Maria [Department of Environmental and Natural Resources Management, University of Patras, GR-30100 Agrinio (Greece); Karikas, George-Albert [Department of Medical Laboratories Technology, Technological Educational Institute of Athens, 12210 Athens (Greece); Lianos, Panagiotis, E-mail: lianos@upatras.gr [Department of Chemical Engineering, University of Patras, Caratheodory 1, University Campus, GR-26504 Patras (Greece); FORTH/ICE-HT, P.O. Box 1414, GR-26504 Patras (Greece)

    2015-08-30

    Highlights: • Photocatalytic and photoelectrocatalytic degradation of the proton pump omeprazole. • Improvement of photocatalysis rate by applying a moderate forward bias. • Highlighting of the advantages of photoelectrocatalysis in a straightforward manner. • HPLC and HR-LC–MS analysis of transformation products. - Abstract: Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole has been studied in the presence of nanocrystalline titania films supported on glass slides or transparent FTO electrodes in alkaline environment. Its photocatalytic degradation rate was assessed by its UV absorbance and by HPLC, while its transformation products were analyzed by HR-LC–MS. Based on UV absorbance, omeprazole can be photocatalytically degraded at an average rate of 6.7 × 10{sup −4} min{sup −1} under low intensity UVA irradiation of 1.5 mW cm{sup −2} in the presence of a nanoparticulate titania film. This corresponds to degradation of 1.4 mg of omeprazole per gram of the photocatalyst per liter of solution per hour. The photodegradation rate can be accelerated in a photoelectrochemical cell by applying a forward bias. In this case, the maximum rate reached under the present conditions was 11.6 × 10{sup −4} min{sup −1} by applying a forward bias of +0.6 V vs. Ag/AgCl. Four major transformation products were successfully identified and their profiles were followed by HR-LC–MS. The major degradation path includes the scission of the sulfoxide bridge into the corresponding pyridine and benzimidazole ring derivates and this is accompanied by the release of sulfate anions in the reaction mixture.

  16. Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole on nanocrystalline titania films in alkaline media: Effect of applied electrical bias on degradation and transformation products.

    Science.gov (United States)

    Tantis, Iosif; Bousiakou, Leda; Frontistis, Zacharias; Mantzavinos, Dionissios; Konstantinou, Ioannis; Antonopoulou, Maria; Karikas, George-Albert; Lianos, Panagiotis

    2015-08-30

    Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole has been studied in the presence of nanocrystalline titania films supported on glass slides or transparent FTO electrodes in alkaline environment. Its photocatalytic degradation rate was assessed by its UV absorbance and by HPLC, while its transformation products were analyzed by HR-LC-MS. Based on UV absorbance, omeprazole can be photocatalytically degraded at an average rate of 6.7×10(-4)min(-1) under low intensity UVA irradiation of 1.5mWcm(-2) in the presence of a nanoparticulate titania film. This corresponds to degradation of 1.4mg of omeprazole per gram of the photocatalyst per liter of solution per hour. The photodegradation rate can be accelerated in a photoelectrochemical cell by applying a forward bias. In this case, the maximum rate reached under the present conditions was 11.6×10(-4)min(-1) by applying a forward bias of +0.6V vs. Ag/AgCl. Four major transformation products were successfully identified and their profiles were followed by HR-LC-MS. The major degradation path includes the scission of the sulfoxide bridge into the corresponding pyridine and benzimidazole ring derivates and this is accompanied by the release of sulfate anions in the reaction mixture.

  17. Delayed-release oral suspension of omeprazole for the treatment of erosive esophagitis and gastroesophageal reflux disease in pediatric patients: a review

    Directory of Open Access Journals (Sweden)

    Alice Monzani

    2010-03-01

    Full Text Available Alice Monzani, Giuseppina Oderda1Department of Pediatrics, Università del Piemonte Orientale, Novara, ItalyAbstract: Omeprazole is a proton-pump inhibitor indicated for gastroesophageal reflux disease and erosive esophagitis treatment in children. The aim of this review was to evaluate the efficacy of delayed-release oral suspension of omeprazole in childhood esophagitis, in terms of symptom relief, reduction in reflux index and/or intragastric acidity, and endoscopic and/or histological healing. We systematically searched PubMed, Cochrane and EMBASE (1990 to 2009 and identified 59 potentially relevant articles, but only 12 articles were suitable to be included in our analysis. All the studies evaluated symptom relief and reported a median relief rate of 80.4% (range 35%–100%. Five studies reported a significant reduction of the esophageal reflux index within normal limits (<7% in all children, and 4 studies a significant reduction of intra-gastric acidity. The endoscopic healing rate, reported by 9 studies, was 84% after 8-week treatment and 95% after 12-week treatment, the latter being significantly higher than the histological healing rate (49%. In conclusion, omeprazole given at a dose ranging from 0.3 to 3.5 mg/kg once daily (median 1 mg/kg once daily for at least 12 weeks is highly effective in childhood esophagitis.Keywords: proton pump inhibitors, children, ranitidine, H2-blockers

  18. Multicenter evaluation of dual-therapy (omeprazol and amoxycillin) for Helicobacter pylori-associated duodenal and gastric ulcer (two years of the observation).

    Science.gov (United States)

    Gabryelewicz, A; Laszewicz, W; Dzieniszewski, J; Ciok, J; Marlicz, K; Bielecki, D; Popiela, T; Legutko, J; Knapik, Z; Poniewierka, E

    1997-09-01

    Treatment with the proton pump inhibitor (omeprazole) and single antibiotic (amoxycillin), two synergistic compounds, can cure Helicobacter pylori (H. pylori) infection, but this therapy is not as effective as had been expected. However, some studies show promising results. The aim of our study was to evaluate the effect of two weeks dual-therapy with omeprazole (O) and amoxycillin (A) on gastric (GU) and duodenal ulcer (DU) patients: ulcer healing, eradication of the H. pylori and recurrence rate of the ulcer. We studied 216 patients (aged 18-70) endoscopically proven GU (58 patients) and DU (158 patients). Rapid urease test from the two antrum biopses and two antral and two corporeal biopses using Giemsa stain method for confirmation of the H. pylori infection were used. The patients were treated with omeprazole 20 mg BID and amoxycillin 1.0 g BID for 2 weeks and investigated every 4 months during 2 years. Clearance effect of Hp infection was achieved in 65.1% GU and 66.4% DU patients. Eradication ("check point" after 4 months) in 43% DU and 56.6% GU patients was confirmed. Reinfection rate was found in 16% during 2 years. We conclude--dual-therapy (O and A) is not sufficiently effective to be recommended as an anti-H. pylori treatment. H. pylori eradication prevents recurrence of peptic ulcer and is an important issue in attempts to achieve permanent ulcer healing.

  19. Development and validation of new analytical methods for simultaneous estimation of Drotaverine hydrochloride in combination with Omeprazole in a pharmaceutical dosage form

    Directory of Open Access Journals (Sweden)

    Smita Sharma

    2017-02-01

    Full Text Available A rapid and precise method (in accordance with ICH guidelines is developed for the quantitative simultaneous determination of Drotaverine hydrochloride and Omeprazole in a combined pharmaceutical dosage form. Three methods are described for the simultaneous determination of Drotaverine hydrochloride and Omeprazole in a binary mixture. The first method was based on UV-Spectrophotometric determination of two drugs, using Vierordt!s simultaneous equation method. It involves absorbance measurement at 226.8 nm (λmax of Drotaverine hydrochloride and 269.4 nm (λmax of Omeprazole in methanol; linearity was obtained in the range of 5–30 μg ml−1 for both the drugs. The second method was based on HPLC separation of the two drugs using potassium dihydrogen phosphate buffer pH 5.0: Acetonitrile: Triethylamine (60:40:0.5, v/v as a mobile phase. Areas were recorded at 260 nm for both the drugs and retention time was found to be 2.71 min. and 3.87 min for Drotaverine hydrochloride and Omeprazole, respectively at 1.0 mL/min flow rate. The selected chromatographic conditions were found to determine Drotaverine hydrochloride and Omeprazole quantitatively in a combined dosage form without any physical separation. The method has been validated for linearity, accuracy and precision. Linearity was found over the range of 5–30 μg mL−1 for both drugs. The third method was based on HPTLC method for simultaneous quantification of these compounds in pharmaceutical dosage forms. Precoated silica gel 60 F254 plate was used as stationary phase. The separation was carried out using Glacial acetic acid:Cyclohexane:Methanol:(80:15:5 v/v/v as mobile phase. The proposed method was found to be fast, accurate, precise, reproducible and rugged and can be used for a simultaneous analysis of these drugs in combined formulations.

  20. Stability-indicating high-performance thin-layer chromatographic method for quantitative determination of omeprazole in capsule dosage form.

    Science.gov (United States)

    Jha, Preeta; Parveen, Rabea; Khan, Suroor A; Alam, Ozair; Ahmad, Sayeed

    2010-01-01

    A novel HPTLC method has been developed and validated for quantitative determination of omeprazole (OPZ) in capsule dosage form. The method was validated according to the International Conference on Harmonization guidelines for accuracy, precision, linearity, specificity, and robustness. HPTLC aluminum sheets precoated with silica gel 60F24 were used as the stationary phase and chloroform-methanol (9 + 1) as the mobile phase. The mobile phase was found to give compact bands for OPZ (Rf value of 0.39 +/- 0.12) in densitometric analysis in the absorbance mode at 302 nm. The linear regression analysis data for the calibration plots showed good linearity (r2 = 0.997) with respect to peak area in the concentration range 50-3000 ng/band. The mean values of the slope and intercept were 9.896 +/- 0.0753 and 1870.761 +/- 16.866, respectively. The method was also applied for stability testing of OPZ in different stress conditions and found to be accurate, linear, precise, robust, specific, and stability indicating. The method proposed can be used for QC and stability testing of different dosage forms such as tablets and capsules, as well as for bulk drug analysis of OPZ.

  1. A Validated High-Throughput Fluorometric Method for Determination of Omeprazole in Quality Control Laboratory via Charge Transfer Sensitized Fluorescence.

    Science.gov (United States)

    Mahmoud, Ashraf M; Ahmed, Sameh A

    2016-03-01

    A high-throughput 96-microwell plate fluorometric method was developed and validated to determine omeprazole (OMZ) in its dosage forms. The method was based on the charge-transfer (CT) sensitized fluorescence reaction of OMZ with 2, 3-dichloro-5, 6-dicyano-1, 4-benzoquinone (DDQ). This fluorescence reaction provided a new approach for simple, sensitive and selective determinations of OMZ in pharmaceutical preparations. In the present method, the fluorescence reaction was carried out in 96-microwell plates as reaction vessels in order to increase the automation of the methodology and the efficiency of its use in quality control laboratories. All factors affecting the fluorescence reaction were carefully studied and the conditions were optimized. The stoichiometry of the fluorescence reaction between OMZ and DDQ was determined and the reaction mechanism was suggested. Under the optimum conditions, the linear range was 100-6000 ng/ml with the lowest LOD of 33 ng/ml. Analytical performance of the proposed assay, in terms of accuracy and precision, was statistically validated and the results were satisfactory; RSD was <2.6 % and the accuracy was 98.6-101.6 %. The method was successfully applied to the analysis of OMZ in its dosage forms; the recovery values were 98.26-99.60 ± 0.95-2.22 %. The developed methodology may provide a safer, automated and economic tool for the analysis of OMZ in quality control laboratories.

  2. Analysis of the literature and in 32 cases of adverse reaction induced by omeprazole%奥美拉唑致不良反应32例文献分析及进展

    Institute of Scientific and Technical Information of China (English)

    覃光灵

    2013-01-01

      目的概述并分析奥美拉唑引起不良反应的情况,为临床用药提供参考。方法检索1998至2010年国内外有关奥美拉唑不良反应(ADR)报道的文献,进行总结分析。结果奥美拉唑致ADR临床表现比较复杂,能够影响人体大部分系统。结论临床医师在对患者应用奥美拉唑治疗时,要严格掌握其适应症,注意不良反应的发生,规避奥美拉唑用药风险,达到合理用药的目的。%Objective Overview and analysis of omeprazole induced adverse reaction conditions, to provide reference for clinical medication. Methods The retrieval of 1998-2010 at home and abroad on the adverse reaction of omeprazole (ADR) reported in the literature, summarized analysis. Results Omeprazole induced ADR clinical manifestation is complicated, can affect the human body most system. Conclusion Clinicians in the application of omeprazole treatment, should strictly control the indications, pay attention to the occurrence of adverse reactions, to avoid omeprazole risks, achieve reasonable use.

  3. Avaliação do efeito antiparasitário do omeprazol na prevenção do desenvolvimento de lesões cutâneas em hamsters infectados por Leishmania brasiliensis Evaluation of omeprazole's antiparasitary effect preventing the development of cutaneous lesions due to Leishmania brasiliensis in hamsters

    Directory of Open Access Journals (Sweden)

    Hélio Amante Miot

    2005-12-01

    Full Text Available FUNDAMENTOS: A leishmaniose tegumentar americana permanece doença endêmica em diversas regiões brasileiras. A sobrevivência do parasita no interior dos macrófagos se deve, em parte, pela atividade de uma K+/H+-ATPase de membrana que pode ser inibida pelo omeprazol. OBJETIVOS: Avaliar a eficácia do omeprazol na prevenção do desenvolvimento de lesões de leishmaniose em hamsters. MÉTODOS: Empregaram-se 18 hamsters, divididos em três grupos: o grupo L recebeu apenas a inoculação de L. brasiliensis na pata anterior direita, o grupo O recebeu apenas doses diárias de 0,4mg de omeprazol subcutâneo, e o grupo L+O recebeu o inóculo de leishmanias e o tratamento com omeprazol desde o dia da inoculação. O estudo foi conduzido por 42 dias, realizaram-se medidas dos diâmetros das patas semanalmente, e, ao final do estudo, foram realizados esfregaços das lesões para verificação dos parasitas. RESULTADOS: Os hamsters dos grupos L e L+O desenvolveram lesões de leishmaniose tegumentar havendo ulceração em duas patas do grupo L e uma do grupo L+O. Ao final do estudo, a mobilidade e vitalidade no grupo L foram menores que em L+O, e estas menores que no grupo O. Os diâmetros das patas inoculadas nos grupos L e L+O foram significativamente maiores que no início do estudo (pBACKGROUND: Cutaneous leishmaniasis remains an endemic disease in several brazilian regions. The parasite’ survival in macrophages is due to a membrane K+/H+-ATPase that can be inhibited by omeprazole. OBJECTIVES: Evaluate omeprazole’s efficacy preventing the development of cutaneous leishmaniasis in hamsters. METHODS: Eighteen hamsters were divided in 3 groups: the L group received an inoculation of L. brasiliensis on right paw, the O group received daily 0,4mg omeprazole subcutaneously, and L+O group received both omeprazole and the inocule. The study was performed in 42 days, and the measurements of the diameter of paws were done weekly. At the end of the study

  4. Pharmacokinetic drug-drug interaction assessment of LCZ696 (an angiotensin receptor neprilysin inhibitor) with omeprazole, metformin or levonorgestrel-ethinyl estradiol in healthy subjects.

    Science.gov (United States)

    Gan, Lu; Jiang, Xuemin; Mendonza, Anisha; Swan, Therese; Reynolds, Christine; Nguyen, Joanne; Pal, Parasar; Neelakantham, Srikanth; Dahlke, Marion; Langenickel, Thomas; Rajman, Iris; Akahori, Mizuki; Zhou, Wei; Rebello, Sam; Sunkara, Gangadhar

    2016-01-01

    LCZ696 is a novel angiotensin receptor neprilysin inhibitor in development for the treatment of cardiovascular diseases. Here, we assessed the potential for pharmacokinetic drug-drug interaction of LCZ696 (400 mg, single dose or once daily [q.d.]) when co-administered with omeprazole 40 mg q.d. (n = 28) or metformin 1000 mg q.d. (n = 27) or levonorgestrel-ethinyl estradiol 150/30 μg single dose (n = 24) in three separate open-label, single-sequence studies in healthy subjects. Pharmacokinetic parameters of LCZ696 analytes (sacubitril, LBQ657, and valsartan), metformin, and levonorgestrel-ethinyl estradiol were assessed. Omeprazole did not alter the AUCinf of sacubitril and pharmacokinetics of LBQ657; however, 7% decrease in the Cmax of sacubitril, and 11% and 13% decreases in AUCinf and Cmax of valsartan were observed. Co-administration of LCZ696 with metformin had no significant effect on the pharmacokinetics of LBQ657 and valsartan; however, AUCtau,ss and Cmax,ss of metformin were decreased by 23%. Co-administration of LCZ696 with levonorgestrel-ethinyl estradiol had no effect on the pharmacokinetics of ethinyl estradiol and LBQ657 or AUCinf of levonorgestrel. The Cmax of levonorgestrel decreased by 15%, and AUCtau,ss and Cmax,ss of valsartan decreased by 14% and 16%, respectively. Co-administration of LCZ696 with omeprazole, metformin, or levonorgestrel-ethinyl estradiol was not associated with any clinically relevant pharmacokinetic drug interactions.

  5. Efficacy of omeprazole on cough, pulmonary function and quality of life of patients with sulfur mustard lung injury: A placebo-control, cross-over clinical trial study

    Directory of Open Access Journals (Sweden)

    Mohammad Hossein Emami

    2014-01-01

    Full Text Available Background: Gastro-esophageal reflux disease (GERD is prevalent and related to more severe disease in patients with respiratory problems. We evaluated the effects of antireflux therapy in warfare victims of exposure to Mustard gas with chronic cough. Materials and Methods: This randomized, double-blind, placebo-controlled, cross-over study was conducted on 45 cases of sulfur mustard injury with chronic cough (≥8 weeks and GERD. Patients were randomized into two groups, receiving either 20 mg twice daily omeprazole-placebo (OP or matching placebo (placebo-omeprazole [PO] for 4 months, followed by a 1-month washout period and the alternative treatment for 4 months. Assessments included GERD and cough, quality of life, and pulmonary function using spirometry. Leicester Cough Questionnaire and SF-36 were used for measuring quality of life. Results: Patients in the OP group experienced a more decrease than those in the PO group in severity of Leicester cough scores during the first 4-month of trial. After crossing the groups, the OP group experienced an increase (P = 0.036 and the PO group experienced a nonsignificant decrease (P = 0.104 in the severity of scores. The OP group also experienced improvement in GERD symptoms and quality of life at the end of the trial, but changes in the PO group was not significant. There was no significant change in respiratory function indices in any groups. Conclusion: Long-term treatment with high-dose omeprazole improved GERD as well as cough, and quality of life, but not changed respiratory function indices in sulfur mustard injured cases with respiratory symptoms.

  6. Evaluation of antiulcer activity of indole-3-carbinol and/or omeprazole on aspirin-induced gastric ulcer in rats.

    Science.gov (United States)

    El-Shinnawy, Nashwa A; Abd-Elmageid, Samira A; Alshailabi, Eda M A

    2014-05-01

    The present work is an attempt to elucidate the antiulcer activity of indole-3-carbinol (I3C), which is one of the anticarcinogenic phytochemicals found in the vegetables of Cruciferae family such as broccoli and cauliflower, alone or in combination with omeprazole (OMP), a proton pump inhibitor, to diminish the effects of induced acute gastric ulcer by aspirin (ASA) in male albino rats. A total of 48 adult male albino rats were used in the present study. Animals were divided into eight experimental groups (six animals each group). They were given different experimental inductions of ASA at a dose of 500 mg/kg/body weight, OMP at a dose of 20 mg/kg/body weight and I3C at a dose of 20 mg/kg/body weight either alone or in combination with each other orally for a duration of 7 days. Inner stomach features, ulcer index, pH activity, body weight, stomach weight, hematological investigations, serum total protein albumin and reduced glutathione activity were investigated in addition to the histological, histochemical and immunohistochemical stain of cyclooxygenase-2 to the stomach tissue of normal control, ulcerated and treated ulcerated rats. The results of this study revealed that oral administration of ASA to rats produced the expected characteristic mucosal lesions. OMP accelerated ulcer healing but the administration of I3C either alone or in combination with OMP to ASA-ulcerated rats produced a profound protection to the gastric mucosa from injury induced by ASA. Our results suggested that administration of antiulcer natural substances such as I3C in combination with the perused treatment such as OMP is a very important initiative in the development of new strategies in ulcer healing.

  7. Omeprazole increases the efficacy of a soluble epoxide hydrolase inhibitor in a PGE2 induced pain model

    Science.gov (United States)

    Goswami, Sumanta Kumar; Inceoglu, Bora; Yang, Jun; Wan, Debin; Kodani, Sean D.; da Silva, Carlos Antonio Trindade; Morisseau, Christophe; Hammock, Bruce D.

    2015-01-01

    Epoxyeicosatrienoic acids (EETs) are potent endogenous analgesic metabolites produced from arachidonic acid by cytochrome P450s (P450s). Metabolism of EETs by soluble epoxide hydrolase (sEH) reduces their activity, while their stabilization by sEH inhibition decreases both inflammatory and neuropathic pain. Here, we tested the complementary hypothesis that increasing the level of EETs through induction of P450s by omeprazole (OME), can influence pain related signaling by itself, and potentiate the anti-hyperalgesic effect of sEH inhibitor. Rats were treated with OME (100 mg/kg/day, p.o., 7 days), sEH inhibitor TPPU (3 mg/kg/day, p.o.) and OME (100 mg/kg/day, p.o., 7 days) + TPPU (3 mg/kg/day, p.o., last 3 days of OME dose) dissolved in vehicle PEG400, and their effect on hyperalgesia (increased sensitivity to pain) induced by PGE2 was monitored. While OME treatment by itself exhibited variable effects on PGE2 induced hyperalgesia, it strongly potentiated the effect of TPPU in the same assay. The significant decrease in pain with OME + TPPU treatment correlated with the increased levels of EETs in plasma and increased activities of P450 1A1 and P450 1A2 in liver microsomes. The results show that reducing catabolism of EETs with a sEH inhibitor yielded a stronger analgesic effect than increasing generation of EETs by OME, and combination of both yielded the strongest pain reducing effect under the condition of this study. PMID:26522832

  8. Omeprazole Attenuates Pulmonary Aryl Hydrocarbon Receptor Activation and Potentiates Hyperoxia-Induced Developmental Lung Injury in Newborn Mice

    Science.gov (United States)

    Shivanna, Binoy; Zhang, Shaojie; Patel, Ananddeep; Jiang, Weiwu; Wang, Lihua; Welty, Stephen E.; Moorthy, Bhagavatula

    2015-01-01

    Hyperoxia contributes to the development of bronchopulmonary dysplasia (BPD) in human preterm infants and a similar lung phenotype characterized by alveolar simplification in newborn mice. Omeprazole (OM) is a proton pump inhibitor that is used to treat humans with gastric acid related disorders. OM-mediated aryl hydrocarbon receptor (AhR) activation attenuates acute hyperoxic lung injury (HLI) in adult mice. Whether OM activates pulmonary AhR and protects C57BL/6J newborn mice against hyperoxia-induced developmental lung (alveolar and pulmonary vascular simplification, inflammation, and oxidative stress) injury (HDLI) is unknown. Therefore, we tested the hypothesis that OM will activate pulmonary AhR and mitigate HDLI in newborn mice. Newborn mice were treated daily with i.p. injections of OM at doses of 10 (OM10) or 25 (OM25) mg/kg while being exposed to air or hyperoxia (FiO2 of 85%) for 14 days, following which their lungs were harvested to determine alveolarization, pulmonary vascularization, inflammation, oxidative stress, vascular injury, and AhR activation. To our surprise, hyperoxia-induced alveolar and pulmonary vascular simplification, inflammation, oxidative stress, and vascular injury were augmented in OM25-treated animals. These findings were associated with attenuated pulmonary vascular endothelial growth factor receptor 2 expression and decreased pulmonary AhR activation in the OM25 group. We conclude that contrary to our hypothesis, OM decreases functional activation of pulmonary AhR and potentiates HDLI in newborn mice. These observations are consistent with our previous findings, which suggest that AhR activation plays a protective role in HDLI in newborn mice. PMID:26272953

  9. High-performance liquid chromatographic separation of rolipram, bupivacaine and omeprazole using a tartardiamide-based stationary phase influence of flow rate and temperature on the enantioseparation.

    Science.gov (United States)

    da Silva Junior, Ivanildo José; Sartor, João Paulo; Rosa, Paulo César Pires; de Veredas, Vinícius; Barreto Júnior, Amaro Gomes; Santana, Cesar Costapinto

    2007-08-24

    Chromatographic separation of the chiral drugs rolipram, bupivacaine and omeprazole on a tartardiamide-based stationary phase commercially named Kromasil CHI-TBB is shown in this work. The effect of temperature on the chromatographic separation of the chiral drugs using the Kromasil CHI-TBB stationary phase was determined quantitatively so as to contribute toward the design for the racemic mixtures of the named compound by using chiral columns. A decrease in the retention and selectivity factors was observed, when the column temperature increased. Van't Hoff plots provided the thermodynamic data. The variation of the thermodynamic parameters enthalpy and entropy are clearly negative meaning that the separation is enthalpy controlled.

  10. A randomized, crossover pharmacodynamic study of immediate‐release omeprazole/sodium bicarbonate and delayed‐release lansoprazole in healthy adult volunteers

    OpenAIRE

    Pratha, Vijayalakshmi S.; McGraw, Thomas; Tobin, William

    2016-01-01

    Abstract Proton pump inhibitors (PPIs) effectively block gastric acid secretion and are the treatment of choice for heartburn. PPIs differ, however, in onset of action and bioavailability. In this single‐center, open‐label, three‐way crossover study, onset of action of immediate‐release omeprazole 20 mg/sodium bicarbonate 1100 mg (IR‐OME) and delayed‐release (DR) lansoprazole 15 mg was evaluated in 63 healthy fasting adults. Subjects were randomized to once daily IR‐OME, or DR‐lansoprazole, o...

  11. Avaliação do efeito antiparasitário do omeprazol na prevenção do desenvolvimento de lesões cutâneas em hamsters infectados por Leishmania brasiliensis

    OpenAIRE

    Miot, Hélio Amante; Miot,Luciane Donida Bartoli; Costa,Ana Laura Bastos da; Matsuo, Cristiane Yuri [UNESP; O’Dwyer,Lúcia Helena

    2005-01-01

    FUNDAMENTOS: A leishmaniose tegumentar americana permanece doença endêmica em diversas regiões brasileiras. A sobrevivência do parasita no interior dos macrófagos se deve, em parte, pela atividade de uma K+/H+-ATPase de membrana que pode ser inibida pelo omeprazol. OBJETIVOS: Avaliar a eficácia do omeprazol na prevenção do desenvolvimento de lesões de leishmaniose em hamsters. MÉTODOS: Empregaram-se 18 hamsters, divididos em três grupos: o grupo L recebeu apenas a inoculação de L. brasiliensi...

  12. Myrtus communis L. Freeze-Dried Aqueous Extract Versus Omeprazol in Gastrointestinal Reflux Disease: A Double-Blind Randomized Controlled Clinical Trial.

    Science.gov (United States)

    Zohalinezhad, Mohammad E; Hosseini-Asl, Mohammad Kazem; Akrami, Rahimeh; Nimrouzi, Majid; Salehi, Alireza; Zarshenas, Mohammad M

    2016-01-01

    The current work assessed a pharmaceutical dosage form of Myrtus communis L. (myrtle) in reflux disease compared with omeprazol via a 6-week double-blind randomized controlled clinical trial. Forty-five participants were assigned randomly to 3 groups as A (myrtle berries freeze-dried aqueous extract, 1000 mg/d), B (omeprazol capsules, 20 mg/d), and C (A and B). The assessment at the beginning and the end of the study was done by using a standardized questionnaire of frequency scale for the symptoms of gastroesophageal reflux disease (FSSG). In all groups, both reflux and dyspeptic scores significantly decreased in comparison with the respective baselines. Concerning each group, significant changes were found in FSSG, dysmotility-like symptoms and acid reflux related scores. No significant differences were observed between all groups in final FSSG total scores (FSSG2). Further studies with more precise design and larger sample size may lead to a better outcome to suggest the preparation as an alternative intervention.

  13. A double-blind placebo-controlled randomized trial on probiotics in small bowel bacterial overgrowth in children treated with omeprazole.

    Science.gov (United States)

    Hegar, Badriul; Hutapea, Esther I; Advani, Najid; Vandenplas, Yvan

    2013-01-01

    To evaluate the incidence of small bowel bacterial overgrowth (SBBO) in children treated with omeprazole, and to test whether probiotics influence the incidence. A double-blinded, placebo-controlled trial was performed in 70 children treated orally during four weeks with 20mg omeprazole per day. Lactobacillus rhamnosus R0011 (1.9×10(9) cfu) and Lactobacillus acidophilus R0052 (0.1×10(9) cfu) were simultaneously given daily to 36 subjects (probiotic group), while 34 subjects received placebo (placebo group). The diagnosis of SBBO was based on the development of suggestive symptoms, in combination with a positive glucose breath test. After one month of proton pump inhibitor (PPI) treatment, 30% (21/70) had a positive breath test suggesting SBBO; of these 62% were symptomatic. Five children developed SBBO-like symptoms, but had a negative breath test; and 44 (63%) were symptom free and had a negative breath test. There was no difference in the incidence of positive breath tests in the probiotic versus the placebo group (33% vs 26.5%; p=0.13). Since symptoms suggesting SBBO developed in 26% of PPI-treated children, and since the glucose breath test was abnormal in 72% of these, this side-effect should be more frequently considered. The probiotic tested did not decrease the risk to develop SBBO. Copyright © 2013 Sociedade Brasileira de Pediatria. Published by Elsevier Editora Ltda. All rights reserved.

  14. Mercapto-ordered carbohydrate-derived porous carbon electrode as a novel electrochemical sensor for simple and sensitive ultra-trace detection of omeprazole in biological samples

    Energy Technology Data Exchange (ETDEWEB)

    Kalate Bojdi, Majid [Department of Chemistry, Faculty of Science, Shahid Beheshti University, Tehran 1983963113 (Iran, Islamic Republic of); Faculty of Chemistry, Kharazmi (Tarbiat Moallem) University, Tehran (Iran, Islamic Republic of); Behbahani, Mohammad [Department of Chemistry, Faculty of Science, Shahid Beheshti University, Tehran 1983963113 (Iran, Islamic Republic of); Mashhadizadeh, Mohammad Hosein [Faculty of Chemistry, Kharazmi (Tarbiat Moallem) University, Tehran (Iran, Islamic Republic of); Bagheri, Akbar [Department of Chemistry, Faculty of Science, Shahid Beheshti University, Tehran 1983963113 (Iran, Islamic Republic of); Hosseiny Davarani, Saied Saeed, E-mail: ss-hosseiny@sbu.ac.ir [Department of Chemistry, Faculty of Science, Shahid Beheshti University, Tehran 1983963113 (Iran, Islamic Republic of); Farahani, Ali [Department of Chemistry, Faculty of Science, Shahid Beheshti University, Tehran 1983963113 (Iran, Islamic Republic of)

    2015-03-01

    We are introducing mercapto-mesoporous carbon modified carbon paste electrode (mercapto-MP-C-CPE) as a new sensor for trace determination of omeprazole (OM) in biological samples. The synthesized modifier was characterized by thermogravimetry analysis (TGA), differential thermal analysis (DTA), transmission electron microscopy (TEM), Fourier transform infrared spectrometry (FT-IR), X-ray diffraction (XRD), elemental analysis (CHN) and N{sub 2} adsorption surface area measurement (BET). The electrochemical response characteristic of the modified-CPE toward OM was investigated by cyclic and differential pulse voltammetry (CV and DPV). The proposed sensor displayed a good electrooxidation response to the OM, its linear range is 0.25 nM to 25 μM with a detection limit of 0.04 nM under the optimized conditions. The prepared modified electrode shows several advantages such as high sensitivity, long-time stability, wide linear range, ease of preparation and regeneration of the electrode surface by simple polishing and excellent reproducibility. - Highlights: • A modified nanoporous carbon as a novel sensor • High stability and good repeatability and reproducibility by the prepared sensor • Trace determination of omeprazole • Biological and pharmaceutical samples.

  15. Efecto de la interacción clopidogrel-omeprazol en el reingreso hospitalario de pacientes por recidiva de síndrome coronario agudo: estudio de casos y controles

    Directory of Open Access Journals (Sweden)

    Pedro Amariles

    2014-10-01

    Conclusiones: En este pequeño grupo de pacientes con SCA previo, la utilización simultánea de clopidogrel con omeprazol no aumenta el riesgo de un reingreso hospitalario por recurrencia de este tipo de evento coronario.

  16. 奥美拉唑钠在木糖醇注射液中的稳定性考察%Study on Compatible Stability of omeprazole in Xylitol Injection

    Institute of Scientific and Technical Information of China (English)

    李文兵; 李智勇; 李清

    2011-01-01

    目的 考察注射用奥美拉唑钠与木糖醇注射液配伍后的德定性.方法 用高效液相色谱法考察配伍前后奥美拉唑钠的含量变化,并观察配伍液的外观及pH变化.结果注射用奥美拉唑钠与木糖醇注射液配伍后4h内含量、pH及溶液外观均无明显变化.结论注射用奥美拉唑钠与木糖醇注射液配伍后4h内稳定.%Objective To investigate the compatible stability of Omeprazole Sodium for Injection in Xylitol Injection. Methods The variance of omeprazole sodium content in Xylitol Injection was determined by HPLC within 4 h. Meanwhile, the appearance and pH value change of compatible solution were observed. Results The appearance, pH value and content of Omeprazole Sodium for Injection in Xylitol Injection within 4 h were not found obvious variations. Conclusion Omeprazole Sodium for Injection can be used in compatibility with Xylitol Injection for 4 hours.

  17. 3种不同制剂的奥美拉唑治疗胃十二指肠溃疡的疗效研究%Efficacy Study of Three Different Formulations of Omeprazole Treatment of Gastroduodenal Ulcers

    Institute of Scientific and Technical Information of China (English)

    彭锡其; 黎永华

    2013-01-01

    Objective To explore three different formulations of omeprazole in the treatment of gastric ulcer efficacy. Methods Firstly, we choose 120 Gastroduodenal Ulcers patients who conform to the research diagnosis standard.Then the patients were divided into three groups. Group A were cured by the omeprazole enteric-coated capsules, 20mg/day time.B group were cured by the omeprazole enteric-coated tablets, 20mg/day time. Group C were cured by the Omeprazole Sodium injection 80mg what intravenous infusion, once a day. Three groups of treatment time was 4 weeks. Results No significant difference between the three different formulations of omeprazole in the treatment of gastroduodenal ulcers the gastroscope efficacy and clinical efficacy. And three different formulations of omeprazole were no serious adverse reactions during treatment.Conclusion lllustrating three different formulations of omeprazole were no difference in the clinical use, instead of using other.%  目的探索3种不同制剂的奥美拉唑治疗胃十二指肠溃疡的疗效研究.方法将120例符合胃十二指肠溃疡诊断的患者随机分为3组, A组用奥美拉唑肠溶胶囊口服,20mg/次,日一次.B组用奥美拉唑肠溶片口服,20mg/次,日一次.C组用注射用奥美拉唑钠80mg加入,0.9%氯化钠溶液100mL中静脉滴注,日一次.三组治疗时间均为4周.结果三种不同制剂的奥美拉唑在治疗胃十二指肠溃疡的胃镜疗效和临床疗效上没有显著性差异.而且三种不同制剂的奥美拉唑在治疗过程中均未出现严重不良反应.结论说明三种不同制剂的奥美拉唑在临床使用上没有差异,可以互相代替使用.

  18. Evaluate the effect to omeprazole in preventing treatment of hypertensive cerebral hemorrhage with stress ulcer bleeding%奥美拉唑对脑出血应激性溃疡的预防效果

    Institute of Scientific and Technical Information of China (English)

    丁凤英; 罗伟良

    2008-01-01

    Objective To evaluate the effect of omeprazole in preventing treatment of hypertensive cerebral hemorrhage with stress ulcer bleeding. Methods A total of 100 patients with hypertensive cerebral hemorrhage were treated with conventional therapy including dehydration, antihypertensive and supporting treatment. The patients were randomly divided into omeprazole group(n=50) and control group( n = 50). The control group received conventional therapyonly, while the omeprazole group received additional omeprazole 40mg, iv, qd, for 14d. Results Omeprazole group stress ulcer 6 eaess(12.0% ) was significantly lower than the control group 12 cases(24.0% );two groups stress ulcer incidence of severity are increasing with the increase of the disease; the mortalities of cerbral hemorrhage were 6.0 % in the omeprazole group and 16.0 % in the control group and the difference had significant meaning(P>0.05). Conclusion Omeprazole has significant beneficial effect in preventing upper gastrointestinal hemorrhage after hypertensive cerebral hemorrhage.%目的 观察奥美拉唑治疗高血压性脑出血并发应激性溃疡出血的疗效.方法 将100例高血压性脑出血患者分为奥美拉唑组(50例)和对照组(50例),均予常规脱水、降颅压及对症支持治疗,奥美拉唑组加用奥美拉唑40 mg,静脉注射,1次/d,共14 d.结果 奥美拉唑组应激性溃疡6例(12.0%),明显低于对照组12例(24.0%);两组应激性溃疡发生率均随病情程度加重而增加;奥美拉唑组死亡3例(6.0%),明显低于对照组8例(16.0%)(P<0.05).结论 奥美拉唑静脉注射预防高血压性脑出血并发应激性溃疡出血疗效确切,且未见不良反应发生.

  19. 奥美拉唑和泮托拉唑在反流性食管炎中的成本效果观察%The Effect Observation of Omeprazole and Pantoprazole in Reflux Esophagitis

    Institute of Scientific and Technical Information of China (English)

    佘子岳; 刘学功

    2014-01-01

    Objective To compare the analysis of omeprazole and pantoprazole in reflux esophagitis affect difference. Methods A retrospective analysis of our hospital between January 2012 and January 2014, 85 cases of reflux esophagitis patients clinical data, according to different therapeutic methods, divided the patients into two groups, omeprazole group and pantoprazole groups, two groups of patients after the treatment effect of comparative cost differences. Results Omeprazole group of 42 patients, treatment the total effective rate was 90.48%, pantoprazole groups of 43 patients, treatment the total effective rate was 93.02%, slightly higher than that of omeprazole group, by comparison, P>0.05, no significant difference. Omeprazole group C/E value is 4.99, much smaller than pantoprazole groups, suggests that the treatment of patients with omeprazole group cost effect is well. Conclusion The domestic omeprazole enteric-coated tablets in treatment of reflux esophagitis have relative cost effect advantage, is the ideal treatment.%目的:比较分析奥美拉唑和泮托拉唑在反流性食管炎中的成本效果差异性。方法回顾性分析我院2012年1月至2014年1月收治的85例反流性食管炎患者的临床资料,根据治疗方法不同,将患者分为2组,奥美拉唑组和泮托拉唑组,两组患者疗程结束后比较成本效果差异。结果奥美拉唑组42例患者,治疗总有效率为90.48%,泮托拉唑组43例患者,治疗总有效率为93.02%,略高于奥美拉唑组,经比较,P>0.05,无显著性差异。奥美拉唑组的 C/E 值为4.99,明显小于泮托拉唑组,说明奥美拉唑组患者的治疗成本效果较好。结论采用国产奥美拉唑肠溶片治疗反流性食管炎具有相对的成本效果优势,是较为理想的治疗方案。

  20. 奥美拉唑对利培酮和9-羟利培酮血药浓度影响的研究%Influence study of omeprazole on blood drug concentration of risperidone and 9-hydroxy risperidone

    Institute of Scientific and Technical Information of China (English)

    巫艳芬; 王玉梅; 陈宝燕

    2014-01-01

    目的:观察奥美拉唑对利培酮和9-羟利培酮血药浓度的影响。方法20例精神分裂症合并胃溃疡患者,给予利培酮联合奥美拉唑治疗1周。检测奥美拉唑治疗后利培酮以及9-羟利培酮血药浓度。结果未使用奥美拉唑前,利培酮与9-羟利培酮血药浓度为(29.25±7.82)μg/L;使用奥美拉唑后,利培酮与9-羟利培酮血药浓度为(37.15±11.68)μg/L,差异有统计学意义(P<0.05)。结论奥美拉唑能够提高利培酮与9-羟利培酮血药浓度,因此,临床上治疗精神分裂症合并胃溃疡患者,给予奥美拉唑联合利培酮治疗时,应该监测患者利培酮与9-羟利培酮血药浓度,及时对药物剂量进行调整。%Objective To observe the influence of omeprazole on blood drug concentration of risperidone and 9-hydroxy risperidone. Methods A total of 20 schizophrenia with gastric ulcer cases were treated by risperidone combined with omeprazole for 1 week. Detections of blood drug concentration of risperidone and 9-hydroxy risperidone were made after the omeprazole treatment. Results Before application of omeprazole, blood drug concentration of risperidone and 9-hydroxy risperidone was (29.25±7.82)μg/L. After using omeprazole, blood drug concentration of risperidone and 9-hydroxy risperidone was (37.15±11.68) μg/L. The difference had statistical significance (P<0.05). Conclusion Omeprazole can increase the blood drug concentration of risperidone and 9-hydroxy risperidone, which should be monitored in the risperidone combined with omeprazole treatment of schizophrenia with gastric ulcer, and timely adjustment of drug dose is necessary.

  1. Jinsangliyan pills combined with omeprazole in the treatment of gastroesophageal reflux pharyngitis%金嗓利咽丸联合奥美拉唑治疗胃食管反流性咽炎

    Institute of Scientific and Technical Information of China (English)

    李成光; 王广科

    2013-01-01

    Objective To observe the clinical effect of jinsangliyan pills combined with omeprazole on gastroesophageal reflux pharyngitis.Methods Ninety-seven patients with gastroesophageal reflux pharyngitis were randomly divided into treatment group and control group,patients in treatment group were given jinsangliyan pills combined with omeprazole,the patients in control group were only given omeprazole.Results The total effective rate was 89.8% in the treatment group and 72.92% in the control group,there were significant differences between the two groups (P < 0.05).Conclusions The effect of jinsangliyan pills combined with omeprazole on gastroesophageal reflux pharyngitis was better than simple application of omeprazole.%目的 观察金嗓利咽丸联合奥美拉唑治疗胃食管反流性咽炎的临床疗效.方法 将确诊为胃食管反流性咽炎的97例患者随机分为治疗组和对照组,治疗组给予金嗓利咽丸联合奥美拉唑治疗,对照组仅给予奥美拉唑治疗.结果 治疗组总有效率为89.8%,对照组为72.92%,两组总有效率比较差异有统计学意义(P< 0.05).结论 临床应用金嗓利咽丸联合奥美拉唑治疗胃食管反流性咽炎明显优于单纯应用奥美拉唑治疗.

  2. 奥美拉唑镁肠溶片含量测定方法的改进%Improve method for the content determination of Omeprazole Magnesium Enteric-coared Tablets

    Institute of Scientific and Technical Information of China (English)

    孙蕊; 刘世超

    2011-01-01

    目的:建立高效液相法测定奥美拉唑镁肠溶片含量的方法.方法:采用Diamonsil-C18(4.6 mm×150 mm,5μm)色谱柱;流动相:甲醇-水-磷酸-三乙胺(65∶35∶0.12∶0.3);检测波长:302 nm;流速:1.0 ml/min.结果:奥美拉唑镁在13.3182~31.0758μg范围内与峰而积呈良好的线性关系(r=0.999 0),平均回收率为101.14%,RSD=1.64%.结论:本法简便、准确、重现性好,可用于奥美拉唑镁肠溶片的质量控制.%Objective: To establish a method for the content determination of Omeprazole Magnesium in Omeprazole Mag nesium Enteric-coated Tablets by HPLC. Methods: The Diamonsil-C18 (4.6 mm×150 mm, 5 μm) column was used. The mo bile phases consisted of methanol, water, phosphoric acid and triethylamine (65:35:0.12:0.3), the flow rate was 1.0 ml/min and the detection wavelength was at 302 nm. Results: The linear ranges of Omeprazole was at 13.318 2-31.075 8 μg (r=0.999 0),the average recovery was 101.14% with a RSD of 1.64%. Conclusion: The method is fast, reliable, accurate and can be used in the quality control of Omeprazole Magnesium in Omeprazole Magnesium Enteric-coared Tablets.

  3. Utilização do óleo de alho e da amoxilina, metronidazol e omeprazol no controle de Helicobacter spp. em cães Use of garlic oil and amoxicillin, metronidazole, and omeprazol in the control of Helicobacter spp. in dogs

    Directory of Open Access Journals (Sweden)

    M.C. Costa

    2009-04-01

    Full Text Available Avaliaram-se a eficácia do óleo de alho e da terapia tripla (amoxicilina, metronidazol e omeprazol no tratamento de 21 cães infectados por Helicobacter spp., que apresentavam alterações histológicas nas biopsias endoscópicas da mucosa gástrica e reação positiva ao teste de urease. Os animais foram distribuídos, aleatoriamente, em três grupos de sete cães, os quais receberam os seguintes tratamentos: grupo 1 - cápsulas vazias; grupo 2 - 500mg de óleo de alho em cápsulas, diariamente, por um período de 30 dias; grupo 3 - amoxicilina, metronidazol e omeprazol, respectivamente, nas doses de 20mg/kg a cada 12 horas, 25mg/kg e 20mg/kg a cada 24 horas, durante 15 dias. Ao final dos tratamentos, os cães foram submetidos à endoscopia com realização de biopsias da mucosa gástrica. O tratamento com amoxicilina, metronidazol e omeprazol resultou em erradicação de Helicobacter spp. tanto na região fúndica quanto na pilórica. No grupo 2, houve redução da degeneração glandular na região fúndica em dois animais e em outros dois na pilórica. O tratamento com óleo de alho não foi eficaz em erradicar Helicobacter spp., apenas reduziu a sua colonização em quatro dos animais tratados.The efficacy of garlic oil and triple therapy (amoxicillin, metronidazole, and omeprazol were evaluated in the treatment of 21 dogs infected by Helicobacter spp., which presented histological alterations of the gastric mucosa according to endoscopic biopsies and positive reaction to urease test. The animals were randomly distributed into three groups of seven dogs each, and received the following treatment, group 1 - empty capsules; group 2 - 500mg of garlic oil capsules daily for a period of 30 days; and group 3 - amoxicillin, metronidazole, and omeprazol, in doses of 20mg/kg every 12 hours, 25mg/kg and 20mg/kg every 24 hours, respectively, for 15 days. By the end of the treatment, the dogs were subjected to new endoscopic procedure with gastric

  4. Omeprazole treatment of gastrointestinal bleeding on clinical observation and analysis%奥美拉唑治疗上消化道出血的临床疗效

    Institute of Scientific and Technical Information of China (English)

    张振宇

    2014-01-01

    目的:观察分析奥美拉唑治疗上消化道出血临床疗效。方法:选取本院2009年5月-2012年9月上消化道出血患者80例,分为对照组和观察组各40例。观察组在常规治疗的基础上采用奥美拉唑进行治疗,对照组只用常规方法治疗。观察两组止血和不良反应情况。结果:观察组止血率与再出血率均优于对照组。在治疗过程中,组均未发现不良反应。结论:奥美拉唑治疗上消化道出血效果显著,止血起效时间短,不良反应轻微。%Objective:To observe the clinical efficacy of gastrointestinal bleeding Analysis of omeprazole treatment. Methods: A hospital in May 2009 September 2012 80 patients with upper gastrointestinal bleeding, divided into control group and observation group, 40 cases, with no difference among the two groups of basic physical condition, age, gender will not affect the results, observation group omeprazole treatment on the basis of conventional treatment, the control group only conventional therapy. Results: gastrointestinal bleeding continues on the observation group were four cases, bleeding rate of 90%;the control group, 8 patients with gastrointestinal bleeding continued bleeding rate of 80%. In the course of treatment, observation and treatment groups were found adverse reactions. Conclusions: In the treatment of gastrointestinal bleeding during omeprazole treatment significantly shorter onset time to stop bleeding, help stop bleeding and prevention of rebleeding after the effect of adverse reactions were mild, less bleeding continues, and reduce the amount of bleeding, is one of the best drug for the treatment of gastrointestinal bleeding.

  5. Cysteamine-colon and cysteamine-duodenum lesions in rats. Attenuation by gastric pentadecapeptide BPC 157, cimetidine, ranitidine, atropine, omeprazole, sulphasalazine and methylprednisolone.

    Science.gov (United States)

    Sikiric, P; Seiwerth, S; Grabarevic, Z; Balen, I; Aralica, G; Gjurasin, M; Komericki, L; Perovic, D; Ziger, T; Anic, T; Prkacin, I; Separovic, J; Stancic-Rokotov, D; Lovric-Bencic, M; Mikus, D; Staresinic, M; Aralica, J; DiBiaggio, N; Simec, Z; Turkovic, B; Rotkvic, I; Mise, S; Rucman, R; Petek, M; Sebecic, B; Ivasovic, Z; Boban-Blagaic, A; Sjekavica, I

    2001-01-01

    Recently, we showed cysteamine-duodenal lesions without gastric acid, since they were induced also in gastrectomized rats, as in naive rats, and they were inhibited by the novel stomach pentadecapeptide BPC 157 as well as standard antiulcer drugs (i.e. cimetidine, ranitidine, omeprazole, bromocriptine, atropine). Therefore, as an advantage of considering cysteamine as a directly acting cytotoxic agent and mentioned agents as direct cytoprotective agents, the present focus was on the ulcerogenic effect of cysteamine and protective effect of gastroduodenal antiulcer agents outside upper gastrointestinal tract (i.e. in colon). Intrarectal administration of the cysteamine (200 or 400 mg/kg b.w) produced severe colon lesions (i.e. transmural inflammation with serosal involvement) in rats (30 min-72 h-experimental period), apparently distinctive from smaller lesions after non-specific irritant enema [diluted HCl solution, pH 3.8 (adjusted to pH of cysteamine solution (pH 3.8)]. All of the tested antiulcer agents were applied simultaneously with cysteamine enema (8 cm from the anus, in a volume of the 1.0 ml/rat) intraperitoneally (i.p.), intragastrically (i.g.) or intrarectally (i.r.). Pentadecapeptide BPC 157 (10 microg or 10 ng/kg b.w.), given in either regimen, previously shown to have, besides others, a particular beneficial activity just in the intestinal mucosa, inhibited these cysteamine colon lesions (assessed after 30 min, 60 min, 180 min, 24 h, 48 h, 72 h following cysteamine in a dose of either 200 or 400 mg/kg i.r.). Cysteamine-colon lesions were also attenuated by standard antiulcer agents (mg/kg b.w.), given i.p., i.g., or i.r., such as ranitidine (10), cimetidine (50), omeprazole (10), atropine (10), together with methylprednisolone (1), and sulphasalazine (50, i.r.), assessed 30 min following application of 200 mg of cysteamine. Finally, standard cysteamine duodenal lesions (assessed 24 h after a subcutaneous application of 400 mg/kg of cysteamine) were

  6. Alginate beads as a carrier for omeprazole/SBA-15 inclusion compound: A step towards the development of personalized paediatric dosage forms.

    Science.gov (United States)

    Del Gaudio, Pasquale; De Cicco, Felicetta; Sansone, Francesca; Aquino, Rita Patrizia; Adami, Renata; Ricci, Maurizio; Giovagnoli, Stefano

    2015-11-20

    The treatment of gastro-esophageal reflux disease (GERD) shows several issues among paediatric patients. This work aims to the formulation of enteric alginate beads loaded with omeprazole (OME) allowing age- and weight-related personalized dosages in children. OME was entrapped in SBA-15 mesoporous compound, characterized and loaded into alginate beads by prilling at different OME and alginate concentrations. The beads resulted of homogeneous size, spherical morphology and very consistent in drug loading and distribution. Formulations demonstrated limited swelling and release (about 10%) in simulated gastric fluid (SGF) after 2h and a prolonged release in simulated intestinal fluid (SIF), till 6h, due to a mixed diffusion-case II transport mechanism. The beads were superior to the market product, which showed lower release in SGF but immediate dissolution in SIF. The high alginate beads uniformity and release properties make them a potential novel tool for a personalized treatment of GERD in children.

  7. 雷贝拉唑与奥美拉唑在消化性溃疡治疗中的应用%Rabeprazole and Omeprazole in Peptic ulcer Treatment

    Institute of Scientific and Technical Information of China (English)

    向四国; 胡忠金; 潘润洪

    2013-01-01

      目的研究和比较雷贝拉唑与奥美拉唑在消化性溃疡治疗中的临床疗效。方法选取2011年2月至2012年3月本院收治的消化性溃疡患者38例,随机分为雷贝拉唑组和奥美拉唑组各19例。雷贝拉唑组采用口服雷贝拉唑组进行治疗,奥美拉唑组则采用口服奥美拉唑进行治疗,比较两组患者的治疗效果。结果雷贝拉唑组的有效率为89.5%远高于奥美拉唑组的57.9%,说明雷贝拉唑的疗效明显优于奥美拉唑,差异有统计学意义(P<0.05);在雷贝拉唑组中,仅有5例患者发生了各种类型的药物不良反应,占26.32%。而奥美拉唑组中,有11例患者发生药物不良反应,占57.89%,雷贝拉唑组不良反应发生率明显低于奥美拉唑组,差异具有统计学意义(P<0.05)。结论采用雷贝拉唑治疗消化性溃疡,起效迅速,作用持久,安全可靠。其疗效和不良反应发生率均明显优于奥美拉唑,值得临床推广和应用。%Objective To study and compare rabeprazole and omeprazole in the treatment of peptic ulcer clinical efficacy. Methods Our hospital from February 2011 to March 2012, 38 cases of peptic ulcer patients were randomly divided into 19 cases of rabeprazole group and omeprazole group. Rabeprazole group therapy with rabeprazole group, omeprazole, omeprazole treatment, the therapeutic effect of the two groups were compared. Results 89.5%of the rabeprazole group was much higher than 57.9%of the omeprazole group, said Mingleibeila azole significantly better than omeprazole, the difference was statistically significant (P<0.05);rabeprazole group occurred only five patients, the types of adverse drug reactions, accounting for 26.32%. Omeprazole 11 patients, adverse drug reactions, accounting for 57.89%, the rabeprazole group incidence of adverse events was significantly lower than the omeprazole group, the difference was statistically significant (P<0.05). Conclusion

  8. Observation Curative and Untoward Effect on Omeprazole Combined With Antibiotics in Treatment of Gastric Ulcer%奥美拉唑联合抗生素治疗胃溃疡的疗效及不良反应观察

    Institute of Scientific and Technical Information of China (English)

    程艳艳

    2016-01-01

    目的:观察奥美拉唑联合抗生素治疗胃溃疡的疗效及不良反应。方法将我院收治的52例胃溃疡患者作为研究对象,随机分组,各26例。西咪替丁组予以甲硝唑片、阿莫西林及西咪替丁片治疗,奥美拉唑组予以甲硝唑片、阿莫西林及奥美拉唑肠溶片治疗。对比两组患者临床效果、不良反应发生率。结果西咪替丁组临床总有效率69.2%,低于奥美拉唑组96.2%,差异有统计学意义(P<0.05);西咪替丁组不良反应发生率46.2%,高于奥美拉唑组15.4%,差异有统计学意义(P<0.05)。结论应用抗生素与奥美拉唑联合治疗胃溃疡可提高其临床效果,有效降低不良反应发生率。%Objective To observe the curative effect and adverse reaction of omeprazole combined with antibiotics in the treatment of gastric ulcer.Methods 52 cases of gastric ulcer patients treated in our hospital were studied, random divided into difference groups, each of 26 cases. The cimetidine group were given metronidazole tablets, amoxicillin and cimetidine tablets treatment, The omeprazole group received metronidazole tablets, amoxicillin and omeprazole enteric-coated tablets treatment. The clinical effect and incidence of adverse reactions in the two groups were analyzed.Results The clinical total effective rate of cimetidine group was 69.2%, lower than the omeprazole group 96.2%, and the difference was signiifcant (P<0.05), The incidence of adverse reactions in cimetidine group was 46.2%, higher than that in omeprazole group 15.4%, the difference was signiifcant (P<0.05).Conclusion The combination of antibiotics and omeprazole in the treatment of gastric ulcer can signiifcantly improve the clinical effect, reduce the incidence of adverse reactions.

  9. 兰索拉唑与奥美拉唑治疗酒精型消化性溃疡的临床疗效比较%Efficacy comparison of lansoprazole and omeprazole in treatment for alcoholic peptic ulcer

    Institute of Scientific and Technical Information of China (English)

    吴江涛

    2012-01-01

    目的 对比分析兰索拉唑与奥美拉唑治疗酒精型消化性溃疡的临床疗效.方法 将126例酒精型消化性溃疡患者随机分入兰索拉唑组与奥美拉唑组,兰索拉唑组给予兰索拉唑+阿莫西林+克拉霉素治疗,奥美拉唑组给予奥美拉唑+阿莫西林+克拉霉素治疗,两组疗程均为4周.比较两组的临床疗效、幽门螺杆菌(Hp)清除率及不良反应发生率.结果 兰索拉唑组与奥美拉唑组临床治疗总有效率分别为95.5%和95.0%,两组比较差异无统计学意义(P>0.05);两组患者治疗前后临床症状比较差异无统计学意义(P>0.05);兰索拉唑组Hp清除率显著高于奥美拉唑组(90.9% vs.78.3%,P0.05).结论 兰索拉唑治疗酒精型消化性溃疡Hp清除率高,不良反应少.%Objective To compare the clinical efficacy of lansoprazole and omeprazole in treatment for alcoholic peptic ulcer. Methods 126 cases with alcoholic peptic ulcer were randomly divided into lansoprazole group and omeprazole group. Lansoprazole group received lansoprazole, amoxicillin and clarithromycin treatment. Omeprazole group was given omeprazole, amoxicillin and clarithromycin treatment. Clinical effect, Hp eradication rate and adverse reaction rate were compared between the two groups. Results The effective rates in lansoprazole group and omeprazole group were 95. 5% and 95. 0% respectively ( P >0. 05 ); There was no significant difference in clinical symptoms before and after treatment between the two groups ( P > 0. 05 ); Hp eradication rate in lansoprazole group was much higher than that in omeprazole group( 90. 9% vs 78. 3% ,P 0. 05 ). Conclusion Lansoprazole treatment for alcoholic peptic ulcer has high eradication rate and low adverse reaction rate.

  10. Proteção da recuperação funcional do miocárdio pelo omeprazol após isquemia-reperfusão em corações isolados de ratos Myocardium functional recovery protection by omeprazole after ischemia-reperfusion in isolated rat hearts

    Directory of Open Access Journals (Sweden)

    Otoni Moreira Gomes

    2010-09-01

    Full Text Available OBJETIVO: Analisar efeitos do omeprazol na proteção da recuperação funcional de corações isolados de ratos submetidos à lesão de isquemia-reperfusão. MÉTODOS: Foram estudados 12 ratos Wistar, peso corpóreo médio de 280g. Após anestesia com injeção intra-abdominal de 10mg de cetamina e 2mg de xilazina, os corações foram removidos e mantidos em perfusão com solução Krebs-Henseleit (95%O2 e 5% CO2, 37ºC, 110-120mmHg de pressão de perfusão e pressão diastólica de 8 mmHg em sistema Langendorff, modificado, descartável, modelo FCSFA-ServCor (Comex Ltda.. Os seis corações do Grupo I (GI e os seis do Grupo II (GII foram submetidos a 20 minutos de isquemia e 30 minutos de reperfusão. Nos corações do Grupo II, imediatamente antes da isquemia, foram administrados via perfusão coronária 200mcg de omeprazol. Foram controlados frequência cardíaca (FC, fluxo coronário (FCo, pressão sistólica (PS, +dP/dt e -dP/dt, após estabilização (t0 e no final da reperfusão (t30. Empregou-se método não paramétrico de Kruskal-Wallis (P0,05 entre os valores de FCo e FC nos dois grupos. No final do período de reperfusão (t30, foram significantes (POBJECTIVE: To evaluate the myocardium contractility alterations of isolated hearts of rats, submitted to ischemia and reperfusion with and without administration of the omeprazole. METHODS: Twelve Wistar breed rats with 270g mean body weight was studied. After anesthesia by intraperitoneal injection of ketamine 10mg and xylazine 2mg, their hearts were removed and perfused with Krebs-Henseleit solution (95% of O2 and 5% of CO2, 37ºC, 110-120 mmHg perfusion pressure, 8 mmHg ventricular diastolic pressure in the São Francisco de Assis disposable Langendorff system model Comex Ltda, MG. The six hearts of Group I (GI and of the Group II (GII were submitted to 20 min ischemia and 30 min reperfusion. In GII hearts, intracoronary injection of omeprazole 200 mcg was done immediately before the

  11. 埃索美拉唑与奥美拉唑治疗胃溃疡的临床疗效对比%Comparison of Clinical Efficacy of Esomeprazole and Omeprazole in Treatment of Gastric Ulcer

    Institute of Scientific and Technical Information of China (English)

    杨薇

    2015-01-01

    目的对比分析埃索美拉唑与奥美拉唑治疗胃溃疡的临床疗效。方法收集我院2010年2月~2015年1月诊治的158例胃溃疡患者作为研究对象,根据患者的治疗药物将其分为埃索美拉唑组(79例)与奥美拉唑组(79例),奥美拉唑组采用奥美拉唑+克拉霉素缓释片+阿莫西林克拉维酸钾治疗,埃索美拉唑组采用埃索美拉唑+克拉霉素缓释片+阿莫西林克拉维酸钾治疗,观察两组患者的总体治疗效果、幽门螺杆菌根除率及复发率。结果埃索美拉唑组患者的总体治疗效果和幽门螺杆菌根除率均明显高于奥美拉唑组(<0.05)。在为期一年的随访中,埃索美拉唑组仅有4例患者复发,复发率为5.06%,奥美拉唑组有15名患者复发,复发率为18.99%,埃索美拉唑组的复发率明显低于奥美拉唑组(<0.05)。结论埃索美拉唑治疗胃溃疡的临床疗效优于奥美拉唑。%Objective To compare and analyze the clinical ef ects of esomeprazole and omeprazole triple therapies on gastric ulcer. Methods 158 patients who suf ered from the gastric ulcer and who accepted treatments in our hospital from February, 2010 to January, 2015 were taken as the research objects, and these patients were according the the drug randomly divided into esomeprazole group (79 cases) and omeprazole group (79 cases). In the omeprazole group , they were treated with the omeprazole, clarithromycin sustained release tablets and amoxicil in clavulanic acid potassium while in the esomeprazole group, they were treated with the esomeprazole , clarithromycin sustained release tablets and amoxicil in and clavulanate potassium. Then, the overal treatment ef ect, helicobacter pylori eradication rate and recur ence rate of these two groups of patients were observed. Results The overal treatment ef ect and Helicobacter pylori eradication rate in esomeprazole group were significantly higher than those in omeprazole group ( <0.05). During the one

  12. Clinical Study on Pantoprazole and Omeprazole in the Treatment of Patients With Peptic Ulcer%洋托拉唑和奥美拉唑治疗消化性溃疡的临床研究

    Institute of Scientific and Technical Information of China (English)

    高虹

    2016-01-01

    目的:对比研究泮托拉唑和奥美拉唑治疗消化性溃疡的临床疗效和毒副作用。方法选取2013年10月~2015年10月我院收治消化性溃疡94例患者。随机将患者分为泮托拉唑组(47例)和奥美拉唑组(47例)。泮托拉唑组和奥美拉唑组均依据有无幽门螺杆菌感染,给予阿莫西林、甲硝唑治疗。泮托拉唑组以泮托拉唑治疗;奥美拉唑组以奥美拉唑治疗。观察治疗效果以及不良反应。结果泮托拉唑组总有效率高于奥美拉唑组,差异具有统计学意义(P<0.05)。泮托拉唑组和奥美拉唑组的不良反应率分别为6.4%和12.8%,两组对比,差异具有统计学意义(P<0.05)。结论泮托拉唑和奥美拉唑治疗消化性溃疡均能达到较好的临床疗效,而泮托拉唑效果更好,不良反应更少。%Objective To comparative study of pantoprazole and omeprazole in treating peptic ulcer clinical curative effect and side effect.Methods 94 cases of peptic ulcer in our hospital from October 2013 to October 2015 were selected. The patients were randomly divided into pantoprazole group (47 cases) and omeprazole group (47 cases). Pantoprazole group and omeprazole group were of no Helicobacter pylori infection, amoxicillin and metronidazole treatment. Pantoprazole in the treatment group; Omeprazole group was treated with omeprazole. Therapeutic effects and adverse reactions were observed.ResultsThe total effciency of pantoprazole group is higher than that of omeprazole group, the difference was statistically significant (P<0.05). The adverse reaction of pantoprazole group and omeprazole group were 6.4% and 12.8%, the difference was statistically signiifcant between the two groups (P<0.05).Conclusion Pantoprazole and omeprazole in treating peptic ulcer can achieve better clinical effcacy, the better effect of pantoprazole, less adverse reactions.

  13. Clinical curative effect evaluation of hydrotalcite combined with omeprazole in gastric ulcer%铝碳酸镁联合奥美拉唑用于胃溃疡的临床疗效评价

    Institute of Scientific and Technical Information of China (English)

    向良宏; 胡文江; 沈小平

    2016-01-01

    Objective:To explore the clinical effect of hydrotalcite combined with omeprazole in the treatment of gastric ulcer. Methods:72 patients with gastric ulcer were selected.They were randomly divided into the observation group and the control group with 36 cases in each.The control group was given omeprazole treatment.The observation group was given hydrotalcite combined with omeprazole treatment.The clinical curative effects were compared between the two groups.Results:The average time of ulcer healing in the observation group was significantly shorter than that of the control group(P<0.05).The treatment total effective rate of the observation group was significantly higher than that of the control group(P<0.05).Conclusion:The clinical curative effect of hydrotalcite combined with omeprazole in the treatment of gastric ulcer is significant.%目的:探讨铝碳酸镁联合奥美拉唑治疗胃溃疡的临床效果。方法:收治胃溃疡患者72例,随机分成观察组与对照组各36例,对照组给予奥美拉唑治疗,观察组给予铝碳酸镁联合奥美拉唑治疗,比较两组临床疗效。结果:观察组溃疡愈合平均时间明显短于对照组(P<0.05);观察组治疗总有效率明显高于对照组(P<0.05)。结论:铝碳酸镁联合奥美拉唑治疗胃溃疡的临床疗效明显。

  14. Comparison Observation of Lansoprazole and Omeprazole Treatment of Gerd%兰索拉唑与奥美拉唑治疗胃食管反流病的比较观察

    Institute of Scientific and Technical Information of China (English)

    吴琳琳; 黄婷

    2012-01-01

      目的比较兰索拉唑与奥美拉唑治疗胃食管反流病的疗效.方法 将我院2010年1月至2011年6月确诊为胃食管反流病的98名患者随机分为兰索拉唑组和奥美拉唑组,分别服用兰索拉唑30mg/日 ,奥美拉唑20mg/日,疗程4周,疗程结束后比较症状与胃镜检查结果.结果 兰索拉唑组的有效率为95.92%,奥美拉唑组的有效率为79.59%,通过χ2检验,两组有显著性差异,P<0.01.结论 兰索拉唑对胃食管反流病的疗效优于奥美拉唑.%  Objective Lansoprazole is compared with omeprazole treatment of gastroesophageal reflux disease. Methods 98 patients who diagnosed with gastroesophageal reflux in our hospital from January 2010-June 2011 were randomized into lansoprazole group and omeprazole group, respectively take 30 mg/day lansoprazole and omeprazole 20 mg/day, four weeks of treatment, symptoms after treatment compared with gastroscope inspection results. Results Lansoprazole was the effective rate of 95.92%, omeprazole group of effective rate of 79.59%, through the chi-square test, a significant difference between the two groups, P<0.01. Conclusion Lansoprazole was gastroesophageal reflux disease better therapeutic omeprazole.

  15. Comparative Study on the Different Chromatographic Conditions of Determining Omeprazole Content%不同色谱条件下测定奥美拉唑含量方法的比较研究

    Institute of Scientific and Technical Information of China (English)

    李亚东

    2015-01-01

    Objective To compare the content of omeprazole under differences chromatographic conditions for HPLC between two different methods. Methods The C18-methanol system and C8-acetonitrile system were established,and then used the systems to determinate the contents of omeprazole from 3 different manufacturers. Results The content determination of omeprazole from three different manufacturers were determined by C18-methanol methanol and C8-acetonitrile system. There were no significant differences between them(P>0.05). Conclusion The two kinds of different chromatographic conditions for determining omeprazole have no significant difference.%目的:比较2种不同色谱条件下用高效液相色谱法检测奥美拉唑含量的差异。方法建立C18-甲醇体系与C8-乙腈体系,并分别测定3个不同厂家奥美拉唑的含量,对含量测定结果进行统计学分析。结果C18-甲醇体系与C8-乙腈体系测定三家不同厂家奥美拉唑的含量,差异均无统计学意义(P>0.05)。结论2种不同色谱条件下对奥美拉唑进行含量测定,其测定方法无统计学差异。

  16. 阿托品联合奥美拉唑在急性胃炎治疗中的应用效果观察%Observation on the Results of Atropine Plus Omeprazole in the Treatment of Acute Gastritis

    Institute of Scientific and Technical Information of China (English)

    刘冬曼

    2016-01-01

    Objective To investigate the effect of the application of atropine combined with omeprazole in treating acute gastritis.Methods72 cases of acute gastritis were divided into two groups,the treatment group used atropine therapy plus omeprazole,control group used omeprazole alone,compared efficacy and drug safety.Results Treatment group’total effective rate was 94.4%,significantly higher than 77.8% in control group(P<0.05). The incidence of adverse reactions in the treatment group and the control group were statistically significant. Conclusion Omeprazole and atropine in the treatment of acute gastritis have significant,and can reduce adverse reactions in patients after treatment.%目的:探讨阿托品联合奥美拉唑在急性胃炎治疗中的应用效果。方法将72例急性胃炎患者分为两组,治疗组应用阿托品联合奥美拉唑治疗,对照组单纯应用奥美拉唑治疗,对比2组疗效以及用药安全性。结果治疗组治疗总有效率是94.4%,高于对照组的77.8%(P<0.05);治疗组、对照组的不良反应发生率组间对比差异有统计学意义(P<0.05)。结论阿托品联合奥美拉唑在急性胃炎治疗中的应用效果满意,且可减少患者用药后不良反应。

  17. Incompatibility investigation between cefamandole nafate for injection and omeprazole sodium for injection%注射用头孢孟多酯钠与注射用奥美拉唑钠的配伍禁忌探讨

    Institute of Scientific and Technical Information of China (English)

    黎敏如

    2015-01-01

    Objective To investigate the incompatibility between cefamandole nafate for injection and omeprazole sodium for injection.Methods High performance liquid chromatography (HPLC) was applied to detect changes of external appearance, relative amount and pH of cefamandole nafate and omeprazole sodium in different time points during 6 h under 4, 25, and 30℃.Results After 6 h under indoor temperature (25 and 30℃), the solutions had obvious changes in external appearance, clarity, and pH. Contents of cefamandole nafate and omeprazole sodium were remarkably decreased.Conclusion Cefamandole nafate for injection is incompatible with omeprazole sodium for injection, and they should be applied separately.%目的:探讨注射用头孢孟多酯钠与注射用奥美拉唑钠的配伍禁忌。方法高效液相色谱法(HPLC)法测定头孢孟多酯钠、奥美拉唑钠配伍液在4、25、30℃环境下放置6 h内不同时间点外观、相对含量及pH值的变化。结果在室温(25、30℃)条件6 h下,配伍液外观、澄明度及pH值发生明显变化,且头孢孟多酯钠、奥美拉唑钠含量明显降低。结论注射用头孢孟多酯钠与注射用奥美拉唑钠存在配伍禁忌,应间隔使用。

  18. Oscillopolarographic Determination of Omeprazole and Its Electrochemical Behavior%奥美拉唑的示波极谱法测定及其电化学行为

    Institute of Scientific and Technical Information of China (English)

    曹尔新; 曾泳淮

    2001-01-01

    在0.1 mol/L NH3-NH4Cl(pH 8.90)底液中,奥美拉唑在汞电极上有一灵敏的导数还原峰,峰电位Ep=-1.105 V(vs.SCE),峰高与奥美拉唑的浓度在5.0×10-7~1.0×10-5范围内呈线性关系(r=0.9989),检出限为2.0×10-7mol/L。该法应用于胶囊中奥美拉唑含量的测定,结果满意。对奥美拉唑在汞电极上的电化学行为进行了探讨。%In a supporting electrolyte of NH3-NH4Cl(pH 8.90), a sensitive derivative reduction peak of Omeprazole was found by single-sweep oscillopolarography. The potential peak is -1.105 V (vs. SCE). The relationship between peak height and the concentration of Omeprazole is linear from 5.0×10-7 to 1.0×10-5 mol/L. The detection limit is 2.0×10-7 mol/L. The method was applied to the determination of Omeprazole in capsule with satisfactory results. The electrochemical behavior of Omeprazole at Hg electrode was also explored.

  19. Preparation of omeprazole enteric-coated pellets with homemade polyacrylic acid resin II%采用国产聚丙烯酸树脂Ⅱ制备奥美拉唑肠溶微丸的研究

    Institute of Scientific and Technical Information of China (English)

    刘羽; 刘燕; 孙备; 王贺

    2009-01-01

    目的 考察采用国产的聚丙烯酸树脂Ⅱ作为肠溶包衣材料制备奥美拉唑肠溶丸的可行性.方法 分别的采用国产聚丙烯酸树脂Ⅱ与Eudragit L30D作为肠溶包衣材料制备奥美拉唑肠溶丸.并对包衣质量加以比较.结果 未碱化聚丙烯酸树脂Ⅱ 60%与95%的乙醇溶液均可包出合格的奥美拉唑小丸,质量与用L30D所制小丸相近.结论 采用国产聚丙烯酸树脂Ⅱ可以用于制备奥美拉唑肠溶微丸.%Aim To study the feasibility of using polyacrylic acid resin II as the omeprazole enteric-coated pellets′coating material.Methods The omeprazole enteric-coated pellets were prepared by using polyacrylic acid resin II.They were compared with the same pellets prepared by using Eudragit L30D.Results Unbasified polyacrylic acid resin II 60% and 95% of the ethanol solution can be used to produce qualified Omeprazole pellets.There were no significant differences.Conclusion The domestic polyacrylic acid resin II can be used as the omeprazole enteric-coated pellets′coating material.

  20. Influência da monofenilbutazona associada ou não ao omeprazol sobre o sistema digestório e renal de pôneis hígidos Influence of mofebutazone associated or not to omeprazole on the digestive and renal tracts of healthy ponies

    Directory of Open Access Journals (Sweden)

    José de Oliveira Pinto

    2009-02-01

    Full Text Available Os objetivos deste trabalho foram averiguar se a monofenilbutazona causa efeitos colaterais no trato digestório e lesões renais em pôneis hígidos e verificar a capacidade do omeprazol em inibir a gênese de úlceras gástricas. O experimento foi executado em duas etapas. Na primeira foram utilizados seis pôneis, sendo três deles tratados diariamente por via intravenosa (IV com as doses de 3, 4,5 ou 6mg kg-1 de monofenilbutazona durante 12 dias. Os demais, além de antiinflamatório, também receberam 3mg kg-1 de omeprazol. Já na segunda etapa foram incluídos quatro pôneis hígidos, sendo dois tratados com doses diárias de 4,5mg kg-1 de monofenilbutazona durante 12 dias e os demais com 5mL de NaCl a 0,9%, por via IV. Todos os pôneis foram submetidos à gastroscopia antes e após cada etapa experimental. Adicionalmente, na primeira etapa, foram realizadas urinálise e determinação dos valores de variáveis hematológicas (hematócrito e proteína plasmática total e bioquímicas (creatinina, albumina, Ca+2 e P+3. Na primeira etapa, apenas os dois pôneis tratados com 6mg kg-1 de monofenilbutazona apresentaram úlceras na região aglandular, ao longo da margo plicatus. Na segunda etapa, dois animais também apresentaram úlceras gástricas, sendo que um deles havia recebido apenas NaCl a 0,9%. A ocorrência das úlceras não foi influenciada (P>0,05 pela administração e pela dose da monofenilbutazona, nem pela presença do omeprazol. O efeito da monofenilbutazona sobre as variáveis hematológicas e bioquímicas foi inexpressivo (P+3 ou ausente (hematócrito, proteína plasmática total, creatinina, albumina, Ca+2 (P>0,05. Os resultados obtidos permitem concluir que: a ocorrência de úlceras na região aglandular de pôneis hígidos não sofre a influência da aplicação e da dose de monofenilbutazona, quando administrada durante 12 dias; úlceras em grau 4 na região aglandular de pôneis não necessariamente estão acompanhadas

  1. Clinical Observation of Omeprazole Combined With Thrombin for Upper Gastrointestinal Bleeding%奥美拉唑联合血凝酶治疗上消化道出血的临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    杨卫东

    2016-01-01

    目的:探讨奥美拉唑联合血凝酶治疗上消化道出血的效果。方法随机将82例上消化道出血患者平均分为两组。对照组行奥美拉唑治疗;观察组在对照组的基础上行血凝酶治疗。结果观察组总有效率、止血时间等均优于对照组(P<0.05)。结论奥美拉唑联合血凝酶治疗上消化道出血效果理想。%ObjectiveTo investigate the omeprazole combined with thrombin for upper gastrointestinal bleeding.MethodsWe divided 82 patients into two groups,control group received omeprazole treatment,and observation group used thrombin on the basis of control group. ResultsThe total efficiency,the bleeding time of observation group were significantly better than control group(P<0.05).ConclusionThe effect of omeprazole combined with thrombin for upper gastrointestinal bleeding is ideal.

  2. Treating 85 cases of peptic ulcer by the Xianfang Huoming decoction combined with omeprazole%仙方活命饮联合奥美拉唑治疗消化性溃疡85例

    Institute of Scientific and Technical Information of China (English)

    曾铭文

    2013-01-01

      目的:仙方活命饮联合奥美拉唑治疗消化性溃疡疗效观察。方法:将170例患者平均分为两组,治疗组口服奥美拉唑结合仙方活命饮加减治疗,对照组只用奥美拉唑治疗。结果:治疗组疗效明显高于对照组,两组总有效率比较差异有显著性意义(P<0.05)。结论:中西医结合治疗消化性溃疡疗效满意,值得临床推广使用。%Objective:To observe the clinical effect of the Xianfang Huoming decoction combined with omeprazole on treating peptic ulcer. Methods: 170 cases divided into two groups, the treated group was given omeprazole combined with Xianfang Huoming decoction, and the control group was given omeprazole. Results:The effect of treated group was higher than that of the control group, the total efficiency difference was significant (P<0.05). Conclusion:The integrative medicine on treating peptic ulcer has a good curative effect, worthy of a wide clinical research and application.

  3. 高效液相色谱法测定复方奥美拉唑干混悬剂中的有关物质及奥美拉唑磺酰化物的含量%HPLC determination of relevant substances and omeprazole sulphone in compound omeprazole powder for oral suspension

    Institute of Scientific and Technical Information of China (English)

    朱迎军; 李昌亮; 黄莉

    2011-01-01

    Objective To establish an HPLC method to determine the relevant substances and omeprazole sulphone in compound omeprazole powder for oral suspension. Methods Agilent-C8 column (4. 6 mm×200 mm, 5 μm) was used at 280 nm. The mobile phase consisted of 0.01 mol · L-1 dibasic sodium phosphate (adjusted to pH 7. 6 with phosphate acid) -acetonitrile (75 : 25), the flow rate was 1. 0 mL · min-1, the column temperature was 40℃, and the injection volume was 20 μL. Results There was good linearity for omeprazole sulphone at 0. 2-1.0 μg · mL-1 (r=1. 0, n= 5). The average recovery was 99.6% (n=6), RSD=0. 2%. Conclusion The method is simple, efficient and accurate.%目的 建立复方奥美拉唑干混悬剂中有关物质及奥美拉唑磺酰化物的测定方法.方法 色谱柱:Agilent-C8(4.6 mm×200 mm,5 μm);流动相:0.01 mol·L-1磷酸氢二钠(用磷酸调节pH值至7.6)-乙腈(75:25);检测波长:280 nm;流速:1.0 mL·min-1;柱温:40℃;进样量:20μL.结果 奥美拉唑磺酰化物在0.2~1.0μg·ML-1与峰面积呈良好的线性关系(r=1.0,n=5).平均回收率99.6%,RSD= 0.2% (n=6).结论 本方法 简便、迅速、准确.

  4. Effect of Pantoprazole and Omeprazole in the treatment of olderly peptic ulcer bleeding%泮托拉唑与奥美拉唑治疗老年消化性溃疡出血疗效对比

    Institute of Scientific and Technical Information of China (English)

    万晓林

    2016-01-01

    Objective To investigate the clinical effect of pantoprazole and omeprazole on elderly peptic ulcer bleeding. Methods 52 cases of elderly patients with peptic ulcer hemorrhage were divided into pantoprazole group(28 cases, give pantoprazole)and omeprazole group (24 cases, give omeprazole), bleeding stop time, pH of gastric juice, the clinical efficacy of two groups was observed, and the cost-effectiveness was calculated. Results In pantoprazole group, bleeding stop time was shorter than that of omeprazole, and gastric juice pH value was higher than that of omeprazole group,the differences between groups were statistically significant (P<0.05).The total efficiency of pantoprazole group was 96.4% (27/28), and was91.7% in omeprazole group (22/24), cost of omeprazole group was significantly higher than that of pantoprazole group, C/E was 13.046, and △C/△E was 117.723. Conclusion Using pantoprazole in elderly patients with peptic ulcer bleeding has good curative effect with less adverse reaction and low cost of medical , it is worth of farther explore and promote to use.%目的:对比泮托拉唑和奥美拉唑对老年消化溃疡出血的临床疗效。方法将52例老年消化溃疡出血患者分为泮托拉唑组(28例,给予泮托拉唑)和奥美拉唑组(24例,给予奥美拉唑),观察2组出血停止时间、胃液 pH、临床疗效,并进行成本-效果分析。结果泮托拉唑组患者出血停止时间短于奥美拉唑组,胃液pH 值高于奥美拉唑组,组间比较差异均有统计学意义(P<0.05)。泮托拉唑组总有效率96.4%(27/28),奥美拉唑组91.7%(22/24),奥美拉唑组成本明显高于泮托拉唑组,C/E 为13.046,△C/△E 为117.723。结论泮托拉唑用于老年患者消化溃疡出血疗效较好,不良反应少,医疗费用低,值得临床进一步研究推广。

  5. Omeprazole and misoprostol for preventing gastric mucosa effects caused by indomethacin and celecoxib in rats Omeprazol e misoprostol na prevenção de lesões de mucosa gástrica causadas por indometacina e celecoxib em ratos

    Directory of Open Access Journals (Sweden)

    Míriam Elias Cavallini

    2006-06-01

    Full Text Available PURPOSE: To evaluate and to compare macro and microscopically the intense injuries of the gastric mucosa of rats which were caused by NSAIDS celecoxib and indomethacin and the gastric cytoprotection with omeprazole and misoprostol. METHODS: The sample is formed by one hundred and fifty Wistar rats with average weight 200 g, distributed in four groups, such as: Group A, subdivided in groups A1 and A2 - pre-treatment with omeprazole (20 mg/rat during seven days and on the 8th day - use of NSAIDS, concerning A1 (20 rats were given celecoxib (1mg/rat and A2 (20 rats were given indomethacin. The Group B, subdivided in group B1 and B2 - pre-treatment with misoprostol (20mg/rat during seven days and on the 8th day use of NSAIDS, concerning B1 (20 rats were given celecoxib (1 mg/ rat and B2 (20 rats were given indomethacin (12.5 mg/rat. The Group C: were not given cytoprotection during seven days, from the 7th to the 8th day - fast of food and water ad libitum, on the 8th day of NSAIDS use, concerning C1 (20 rats were given celecoxib, C2 (20 rats were given indomethacin (12.5 mg/ rat, C3 (20 rats were given celecoxib (200mg/rato, and Group D - control group, concerning 10 rats were observed during seven days ingesting food and water ad libitum. On the 9th day, the stomachs were taken out and were macro and microscopically evaluated for the identification of the gastric injuries. RESULTS: On the macroscopic studies, the groups A2, B2 and C2 presented a remarkable high number of injuries for cm² /animal, respectively 18.55 injuries for cm² /animal, 16.25 injuries for cm² /animal and 13.55 injuries for cm²/animal. On the microscopic studies, the percentage of the injured mucosa, presented expressive difference among the groups A1, B1, C1 when compared to the groups A2, B2, C2 (pOBJETIVO: Avaliar e comparar macro e microscopicamente as lesões agudas da mucosa gástrica de ratos provocadas pelos AINEs celecoxib e indometacina e a citoproteção g

  6. Erradicación de Helicobacter pylori mediante triple terapia (amoxicilina, claritromicina y omeprazole, en pacientes del Hospital Rafael Ángel Calderón Guardia

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    Rigoberto Salas-Aguilar

    2003-06-01

    Full Text Available Justificación y objetivo: H. pylori es un factor importante en el desarrollo de diversos tipos de patologías gástricas como: gastritis crónica, úlcera péptica, adenocarcinoma tipo intestinal y linfoma. Erradicar la infección es una importante posibilidad en la terapia de los pacientes con esas patologías. En el estudio se analizó la utilidad de la triple terapia para erradicar de la infección por H. pylori en pacientes con gastritis crónica y úlcera péptica. Métodos: Se incluyeron 267 pacientes que atendieron el Servicio de Gastroenterología del HCG, entre enero y mayo de 2000. La presencia de H. pylori fue determinada por ureasa rápida, cultivo y antígenos fecales específicos. Se determinó la CIM de algunos aislamientos mediante la prueba de E-test. Los pacientes recibieron triple terapia con amoxicilina (1000 mg bid vo, claritromicina (500 mg bid vo - Claritrobac‚ y omeprazole (20 mg bid vo - Proton‚, por 10 días. La erradicación de la infección se definió como presencia de H. pylori al principio del tratamiento y un resultado negativo en la prueba de antígenos fecales específicos, entre 30 y 45 días después de finalizado el tratamiento. Resultados: De los 267 pacientes que recibieron la triple terapia, 189 (70,8% la completaron. La erradicación de la bacteria se confirmó en 127 (84,7% de los pacientes que completaron el tratamiento. Treinta y siete (94,9% de los 39 pacientes con diagnóstico endoscópico de úlcera péptica erradicaron la bacteria. La erradicación fue exitosa incluso en pacientes portadores de cepas que mostraron resistencia in vitro a amoxicilina o a claritromicina, aunque en este estudio la presencia de cepas sensibles no predice el éxito del tratamiento en todos los casos. Conclusión: La triple terapia basada en amoxicilina (1000 mg bid vo, claritromicina (500 mg bid vo - Claritro-bac‚ y omeprazole (20 mg bid vo - Proton‚, por 10 días, erradicó la infección por H. pylori en el 84

  7. Interferon titer and the 2',5'-oligoadenylate-synthetase activity in rat thymus lymphocytes in conditions of Omeprazol-caused hypergastrinemia

    Directory of Open Access Journals (Sweden)

    Kompanets I. V.

    2013-01-01

    Full Text Available The aim of this work was the determination of rat thymocytes response to hypergastrinemia evoked by hypoacidity and multiprobiotic «Symbiter® acidophilic concentrated» (symbiter treatment via the estimation of the interferon (IFN titer and 2', 5'-oligoadenylate (OA-synthetase activity in lymphocytes. 2', 5'-OA-synthetase is the IFN-induced enzyme. Methods. The micromethod of IFN titer determination by antiviral activity, spectrophotometrical method of 2', 5'-OA-synthetase activity determination. Results. It was shown that the IFN production by cultivated thymocytes is amplified while the 2', 5'-OA-synthetase activity decreases in these cells in conditions of hypoacidity caused by the 28-days omeprazol treatment. The treatment of animals by symbiter against a background of hypoacidity causes the augmentation of IFN production by thymocytes, but does not stimulate the 2', 5'-OA-synthetase activity. The IFN production by thymocytes in response to IFN inducers (PHA and cycloferone in vitro is intensified comparatively to the control at hypoacidity and symbiter treatment. Conclusions. The multiprobiotic symbiter exhibits interferonogenic properties. The IFN synthesis in response to induction in vitro is intensified in comparison with healthy animals at both hypoacidity and symbiter treatment while the 2', 5'-OA-synthetase acivity in thymocytes decreases.

  8. Gastrin-releasing peptide receptor antagonist or N-acetylcysteine combined with omeprazol protect against mitochondrial complex II inhibition in a rat model of gastritis.

    Science.gov (United States)

    Rezin, Gislaine T; Petronilho, Fabricia C; Araújo, João H; Gonçalves, Cinara L; Daufenbach, Juliana F; Cardoso, Mariane R; Roesler, Rafael; Schwartsmann, Gilberto; Dal-Pizzol, Felipe; Streck, Emilio L

    2011-03-01

    The pathophysiology of gastritis involves an imbalance between gastric acid attack and mucosal defence. In addition, the gastric mucosal injury results in adenosine triphosphate (ATP) depletion leading to mitochondrial dysfunction. Several studies have shown the association of mitochondrial disorders with gastrointestinal dysfunction. In the present study, we investigated the activity of mitochondrial respiratory chain complexes activity in the stomach of rats with gastritis induced by indomethacin (IDM) and treated with omeprazole (OM), N-acetylcysteine (NAC) and the gastrin-releasing peptide receptor (GRPR) antagonist RC-3095. Adult male Wistar rats were pre-treated for 7 days with OM, NAC, RC-3095, combination of OM plus RC-3095, OM plus NAC and water (control). The animals were then submitted to fasting for 24 hr; IDM was administered. The rats were killed 6 hr later, and the stomachs were used for evaluation of macroscopic damage and respiratory chain activity. Our results showed that complex I and IV activities were not affected by administration of IDM. On the other hand, complex II and III activities were inhibited. In addition, OM plus RC-3095 and OM plus NAC did not reverse complex II activity inhibition. However, the complex III activity inhibition was reversed only with the combined use of OM plus RC-3095 and OM plus NAC. Our results are in agreement with previous studies indicating mitochondrial dysfunction in the pathophysiology of gastrointestinal tract disease and we suggest that GRPR antagonism might be a novel therapeutic strategy in gastritis.

  9. Effects of acute administration of omeprazole or ranitidine on basal and vagally stimulated gastric acid secretion and alkalinization of the duodenum in anaesthetized cats.

    Science.gov (United States)

    Fändriks, L; Jönson, C

    1990-02-01

    Experiments were performed on acutely vagotomized cats during chloralose anaesthesia. In order to avoid sympathoadrenergic influences, the adrenal glands were ligated and the splanchnic nerves were cut bilaterally in all animals. The gastric lumen was perfused with saline and the H+ secretion was calculated from pH measurements in the perfusate. HCO3- secretion by the duodenal mucosa was titrated in situ. Omeprazole (4 mg kg-1 i.v., dissolved in PEG400, 40% w/v) did not influence basal or vagally induced HCO3- secretions, but inhibited by about 80% the H+ secretory response induced by electric vagal stimulation. Acute administration of ranitidine (5 mg kg-1 i.v.) transiently lowered arterial pressure, an effect which was followed by a sustained compensatory tachycardia. Ranitidine raised basal duodenal HCO3- secretion by 50% and inhibited vagally induced gastric H+ secretion by about 70%, whereas vagally induced HCO3- secretion was not influenced. The results suggest that vagal nerve stimulation raises the duodenal bicarbonate secretion via a mechanism independent of the level of gastric H+ secretion.

  10. ADSORPTIVE VOLTAMMETRIC BEHAVIOR OF OMEPRAZOLE AND ITS APPLICATION%奥美拉唑的吸附伏安特性及其应用

    Institute of Scientific and Technical Information of China (English)

    曹尔新; 曾泳淮

    2001-01-01

    目的研究奥美拉唑(omeprazole,OPZ)的电化学行为,拟定测定OPZ的吸附溶出伏安法。方法用单扫示波极谱法、循环伏安法等技术进行研究。结果在0.1 mol*L-1 NH3-NH4Cl (pH 8.90)底液中,OPZ在汞电极上有一线性扫描还原峰,其峰电位Ep=-1.04 V (vs Ag/AgCl),该峰有明显的吸附性。吸附粒子为OPZ中性分子,测得OPZ在汞电极上的饱和吸附量Γs=9.55×10-11 mol*cm-2,每个OPZ分子所占电极面积为1.74 nm2,OPZ在汞电极上的吸附符合Frumkin吸附等温式。测得吸附系数β=1.32×106,25℃时的吸附自由能ΔGθ=-34.93 kJ*mol-1,电极反应电子数n=4,不可逆体系动力学参数αnα=0.78,表面电极反应速率常数ks=0.18 s-1,OPZ在溶液中的扩散系数D=1.03×10-5 cm2*s-1。建立了吸附溶出伏安法测定OPZ的最佳条件,检出限为2.0×10-9 mol*L-1。结论证实该体系为具有吸附性的不可逆过程。%AIM To study the electrochemical behavior of omeprazole (OPZ) and a new method for the determination of the compound was established by adsorptive stripping voltammetry. METHODS Linear-sweep polarography and cyclic voltammetry were used. RESULTS In a supporting electrolyte containing 0.1 mol*L-1 NH3-NH4Cl, a reduction peak of OPZ was observed by linear-sweep voltammetry at Hg electrode. The peak showed a potential of -1.04 V (vs Ag/AgCl at 100 mV*s-1) and adsorptive characteristics. The adsorbed species is most probably the neutral molecular of OPZ. The saturated adsorption of OPZ at Hg electrode is 9.55×10-11 mol*cm-2 and every OPZ molecule occupies an area of 1.74 nm2. On the surface of the hanging mercury drop electrode, the adsorption of OPZ obeys Frumkin adsorption isotherm. The adsorption coefficient β is 1.32×106, the Gibbs energy of adsorption ΔGθ is -34.93 kJ*mol-1, the number of electrons transferred n is 4, the kinetics parameter αnα is 0.78, the rate constant of the surface electrode reaction ks is 0.18 s-1, the diffusion coefficient

  11. Erradicación de Helicobacter pylori mediante triple terapia (amoxicilina, claritromicina y omeprazole, en pacientes del Hospital Rafael Ángel Calderón Guardia

    Directory of Open Access Journals (Sweden)

    Rigoberto Salas-Aguilar

    2003-06-01

    Full Text Available Justificación y objetivo: H. pylori es un factor importante en el desarrollo de diversos tipos de patologías gástricas como: gastritis crónica, úlcera péptica, adenocarcinoma tipo intestinal y linfoma. Erradicar la infección es una importante posibilidad en la terapia de los pacientes con esas patologías. En el estudio se analizó la utilidad de la triple terapia para erradicar de la infección por H. pylori en pacientes con gastritis crónica y úlcera péptica. Métodos: Se incluyeron 267 pacientes que atendieron el Servicio de Gastroenterología del HCG, entre enero y mayo de 2000. La presencia de H. pylori fue determinada por ureasa rápida, cultivo y antígenos fecales específicos. Se determinó la CIM de algunos aislamientos mediante la prueba de E-test. Los pacientes recibieron triple terapia con amoxicilina (1000 mg bid vo, claritromicina (500 mg bid vo - Claritrobac‚ y omeprazole (20 mg bid vo - Proton‚, por 10 días. La erradicación de la infección se definió como presencia de H. pylori al principio del tratamiento y un resultado negativo en la prueba de antígenos fecales específicos, entre 30 y 45 días después de finalizado el tratamiento. Resultados: De los 267 pacientes que recibieron la triple terapia, 189 (70,8% la completaron. La erradicación de la bacteria se confirmó en 127 (84,7% de los pacientes que completaron el tratamiento. Treinta y siete (94,9% de los 39 pacientes con diagnóstico endoscópico de úlcera péptica erradicaron la bacteria. La erradicación fue exitosa incluso en pacientes portadores de cepas que mostraron resistencia in vitro a amoxicilina o a claritromicina, aunque en este estudio la presencia de cepas sensibles no predice el éxito del tratamiento en todos los casos. Conclusión: La triple terapia basada en amoxicilina (1000 mg bid vo, claritromicina (500 mg bid vo - Claritro-bac‚ y omeprazole (20 mg bid vo - Proton‚, por 10 días, erradicó la infección por H. pylori en el 84

  12. Separation of omeprazole enantiomers by pre-column derivatization high performance liquid chromatography%柱前衍生化高效液相色谱法分离分析奥美拉唑对映体

    Institute of Scientific and Technical Information of China (English)

    周长民; 关瑾; 任丽艳; 王思林

    2012-01-01

    Objective To establish a pre-column derivatization high performance liquid chromatography for the separation of omeprazole enantiomers. Methods (S)-( + )- camphorsulfonyl chloride was used as the pre-column derivation agent, and the separation was performed on a Diamonsil Cijcolumn with 10 mmol · L-1 ammonium acetate (pH 7. 5) -isopropyl alcohol (75 : 25, v/v) as the mobile phase at 0. 5 mL · Min-1. Results The derivatives were separated at the resolution of 1. 72. Conclusion Omeprazole has been separated with pre-column derivatization high performance liquid chromatography using common Cu column. The method provides reference substances for chiral separation of omeprazole.%目的 建立柱前衍生化高效液相色谱法分离奥美拉唑对映体.方法 以(S)-(+)-樟脑磺酰氯为柱前手性衍生化试剂,衍生物在Diamonsil C18色谱柱上,以10 mmol·L-1醋酸铵(pH 7.5)-异丙醇(75:25,v/v)为流动相分离,流速为0.5 mL· min-1.结果 奥美拉唑衍生物可达到基线分离,分离度为1.72.结论 采用柱前衍生化高效液相色谱法,在普通C18色谱柱上分离奥分析美拉唑衍生物,为此类手性药物的分离分析提供一个新方法.

  13. To Observe the Effect of Omeprazole on Reflux Disease Curative Effect of Stomach%奥美拉唑治疗小儿胃食管反流病的疗效观察

    Institute of Scientific and Technical Information of China (English)

    王敏华

    2014-01-01

    Objective Explore the omeprazole for treatment of children with gastroesophageal reflux disease.Methods To 50 cases esophageal reflux sex disease were randomly divided into observation group and control group(25 cases)and observation group treated with omeprazole,ranitidine group applied treatment,compare the curative ef ect of two groups of patients.Results The total ef ective rate was 96%of observation group was obviously higher than that of control group,the dif erences were statistical y significant ( <0.05).Conclusion Omeprazole treatment of children with gastroesophageal reflux disease curative ef ect,high ef iciency,no obvious adverse reactions,worthy of clinical popularization and application.%目的探讨奥美拉唑治疗小儿胃食管反流病的临床效果。方法将50例反流性食管病患儿随机分为观察组和对照组(各25例),观察组应用奥美拉唑进行治疗,对照组应用雷尼替丁治疗,比较两组患者的疗效。结果观察组的总有效率为96%,明显高于对照组,差异均具有统计学意义(<0.05)。结论奥美拉唑治疗小儿胃食管反流病疗效确切,有效率高,无明显不良反应,值得临床推广应用。

  14. Clinical Observation of Omeprazole and Thrombin in Treatment of Hemorrhage of Upper Digestive Tract%奥美拉唑联合凝血酶治疗上消化道出血临床观察

    Institute of Scientific and Technical Information of China (English)

    肖义琼

    2014-01-01

    Objective To investigate the thrombin and omeprazole in treatment of upper gastrointestinal hemor hage induced. Methods In our hospital for diagnosis and treatment of gastrointestinal bleeding were randomly divided into two groups of 56 cases of upper digestive, 28 patients in control group received comprehensive treatment, the treatment group of 28 cases in the control group based on the use of thrombin, omeprazole. Results The total ef ective rate of the treatment group (96.4%) was higher than that of the control group (75%), adverse reactions of two groups were 17.9%, 14.3%( >0.05). Conclusion Thrombin joint omeprazole treatment, and the security is good, worthy of clinical application.%目的探讨凝血酶联合奥美拉唑治疗上消化道出血。方法56例住院患者随机分为两组,对照组28例采用综合治疗,治疗组28例使用凝血酶联合奥美拉唑治疗。结果治疗组总有效率(96.4%)明显高于对照组(75%),两组不良反应分别为17.9%,14.3%(跃0.05)。结论凝血酶联合奥美拉唑治疗,且安全性好,值得临床推广应用。

  15. Synthesis, physicochemical characterization, DFT calculation and biological activities of Fe(III) and Co(II)-omeprazole complexes. Potential application in the Helicobacter pylori eradication

    Science.gov (United States)

    Russo, Marcos G.; Vega Hissi, Esteban G.; Rizzi, Alberto C.; Brondino, Carlos D.; Salinas Ibañez, Ángel G.; Vega, Alba E.; Silva, Humberto J.; Mercader, Roberto; Narda, Griselda E.

    2014-03-01

    The reaction between the antiulcer agent omeprazole (OMZ) with Fe(III) and Co(II) ions was studied, observing a high ability to form metal complexes. The isolated microcrystalline solid complexes were characterized by elemental analysis, X-ray powder diffraction (XRPD), Scanning Electron Microscopy (SEM), magnetic measurements, thermal study, FTIR, UV-Visible, Mössbauer, electronic paramagnetic resonance (EPR), and DFT calculations. The metal-ligand ratio for both complexes was 1:2 determined by elemental and thermal analysis. FTIR spectroscopy showed that OMZ acts as a neutral bidentate ligand through the pyridinic nitrogen of the benzimidazole ring and the oxygen atom of the sulfoxide group, forming a five-membered ring chelate. Electronic, Mössbauer, and EPR spectra together with magnetic measurements indicate a distorted octahedral geometry around the metal ions, where the coordination sphere is completed by two water molecules. SEM and XRPD were used to characterize the morphology and the crystal nature of the complexes. The most favorable conformation for the Fe(III)-OMZ and Co(II)-OMZ complexes was obtained by DFT calculations by using B3LYP/6-31G(d)&LanL2DZ//B3LYP/3-21G(d)&LanL2DZ basis set. Studies of solubility along with the antibacterial activity against Helicobacter pylori for OMZ and its Co(II) and Fe(III) complexes are also reported. Free OMZ and both metal complexes showed antibacterial activity against H. pylori. Co(II)-OMZ presented a minimal inhibitory concentration ˜32 times lower than that of OMZ and ˜65 lower than Fe(III)-OMZ, revealing its promising potential use for the treatment of gastric pathologies associated with the Gram negative bacteria. The morphological changes observed in the cell membrane of the bacteria after the incubation with the metal-complexes were also analyzed by SEM microscopy. The antimicrobial activity of the complexes was proved by the viability test.

  16. A randomized, crossover pharmacodynamic study of immediate-release omeprazole/sodium bicarbonate and delayed-release lansoprazole in healthy adult volunteers.

    Science.gov (United States)

    Pratha, Vijayalakshmi S; McGraw, Thomas; Tobin, William

    2016-06-01

    Proton pump inhibitors (PPIs) effectively block gastric acid secretion and are the treatment of choice for heartburn. PPIs differ, however, in onset of action and bioavailability. In this single-center, open-label, three-way crossover study, onset of action of immediate-release omeprazole 20 mg/sodium bicarbonate 1100 mg (IR-OME) and delayed-release (DR) lansoprazole 15 mg was evaluated in 63 healthy fasting adults. Subjects were randomized to once daily IR-OME, or DR-lansoprazole, or no treatment for 7 days. The primary efficacy endpoint was the earliest time where a statistically significant difference was observed between IR-OME and DR-lansoprazole in median intragastric pH scores for three consecutive 5-min intervals on day 7. Secondary endpoints compared effects of active treatments on days 1 and 7 (e.g., time to sustained inhibition, percentage of time with pH >4). A significant difference in median intragastric pH favoring IR-OME was observed on day 7 starting at the 10- to 15-min interval postdosing (P = 0.024) and sustaining through the 115- to 120-min interval (P = 0.017). On day 1, IR-OME achieved sustained inhibition of intragastric acidity significantly faster than DR-lansoprazole. IR-OME maintained pH >4 significantly longer than DR-lansoprazole over a 24-h period (P = 0.007) on day 7. Overall, results of this study demonstrate IR-OME is safe and well tolerated and that treatment with IR-OME results in significantly faster onset of action and better gastric acid suppression at steady state than DR-lansoprazole.

  17. Normal and polar-organic-phase high-performance liquid chromatographic enantioresolution of omeprazole, rabeprazole, lansoprazole and pantoprazole using monochloro-methylated cellulose-based chiral stationary phase and determination of dexrabeprazole.

    Science.gov (United States)

    Dixit, Shuchi; Dubey, Rituraj; Bhushan, Ravi

    2014-01-01

    Enantioresolution of four anti-ulcer drugs (chiral sulfoxides), namely, omeprazole, rabeprazole, lansoprazole and pantoprazole, was carried out by high-performance liquid chromatography using a polysaccharide-based chiral stationary phase consisting of monochloromethylated cellulose (Lux cellulose-2) under normal and polar-organic-phase conditions with ultraviolet detection at 285 nm. The method was validated for linearity, accuracy, precision, robustness and limit of detection. The optimized enantioresolution method was compared for both the elution modes. The optimized method was further utilized to check the enantiomeric purity of dexrabeprazole.

  18. Influência da monofenilbutazona associada ou não ao omeprazol sobre o sistema digestório e renal de pôneis hígidos

    OpenAIRE

    Pinto,José de Oliveira; de Souza, Maria Verônica; Costa,Paulo Renato dos Santos; RIBEIRO JÚNIOR,JOSÉ IVO; Maia, Leandro [UNESP; Monteiro, Gabriel Augusto [UNESP

    2009-01-01

    Os objetivos deste trabalho foram averiguar se a monofenilbutazona causa efeitos colaterais no trato digestório e lesões renais em pôneis hígidos e verificar a capacidade do omeprazol em inibir a gênese de úlceras gástricas. O experimento foi executado em duas etapas. Na primeira foram utilizados seis pôneis, sendo três deles tratados diariamente por via intravenosa (IV) com as doses de 3, 4,5 ou 6mg kg-1 de monofenilbutazona durante 12 dias. Os demais, além de antiinflamatório, também recebe...

  19. 埃索美拉唑与奥美拉唑治疗胃溃疡的临床效果分析%Clinical Effect Analysis of esomeprazole and omeprazole in treatment of gastric ulcer

    Institute of Scientific and Technical Information of China (English)

    徐晓萌

    2016-01-01

    目的:观察并分析埃索美拉唑联合奥美拉唑治疗胃溃疡的具体效果。方法选择2014年8月至2015年9月于我院收治的胃溃疡患者80例,随机分为对照组(奥美拉唑治疗)和观察组(埃索美拉唑治疗)各40例,对比两组疗效。结果观察组的治疗有效率为95.00%,显著高于对照组,且夜间酸突破发生率仅为7.50%,较对照组下降明显,组间对比差异显著(χ2=6.49,7.60;P<0.05)。结论与奥美拉唑治疗对比,胃溃疡患者予以埃索美拉唑治疗的效果更为确切,有利于病情康复,具备推广应用。%Objective To observe and analyze esomeprazole plus omeprazole treatment of gastric ulcers specific effects. Methods According to a completely random number table method, August 2014-September 2015 I was admitted to hospital, 80 patients with gastric ulcer were randomly divided into control grouP(omeprazole) and observation grouP(esomeprazole joint omeprazole) 40 cases, compared to the two groups. Results The effective rate of the observation grouPwas 95.00%, significantly higher, and nocturnal acid breakthrough incidence rate was 7.50%, compared with the control grouPdecreased significantly between groups comparison significant difference (χ2=6.49,7.60;P<0.05 ). C o n c l u s i o n The patients with gastric ulcer Esomeprazole be combined with the effect of omeprazole exactly conducive to rehabilitation of the disease, with the application.

  20. 多潘立酮片联合奥美拉唑治疗浅表性胃炎的临床观察%CLINICALEFFECTOFTHECOMBINEDAPPLICATION OFDOMPERIDONE TABLETS AND OMEPRAZOLE ON SUPERFICIAL GASTRITIS

    Institute of Scientific and Technical Information of China (English)

    徐春雨

    2016-01-01

    Objective To explore the clinical effect of the combined application of domperidone tablets and omeprazole on superficial gastritis .Methods 40 cases of superficial gastritis treated in this hospital from January ,2015 to March ,2016 were randomly divided into a control group and an observation group ,with 20 cases in each group .The control group was treated with omeprazole ,while the observation group was treated with omeprazole and domperidone tablets .The curative effects were compared between the two groups .Results The total therapeutic effect rates in the observation group and the control group were 95%and 60% respectively ,and there existed significant difference between the two groups( P<0 .05) .Conclu‐sion n The combined use of domperidone tablets and omeprazole can produce good curative effect on super‐ficial gastritis .%目的:探讨多潘立酮片联合奥美拉唑治疗浅表性胃炎的临床效果。方法以2015年1月至2016年3月收治的40例浅表性胃炎患者为研究对象,随机分为对照组和观察组,每组20例,对照组使用奥美拉唑进行治疗,观察组在此基础上联合多潘立酮片治疗。对比两组的临床疗效。结果观察组临床治疗的总有效率为95%,对照组治疗总有效率为60%,两组治疗效果差异有统计学意义( P <0.05)。结论利用多潘立酮片联合奥美拉唑治疗浅表性胃炎,有很好的治疗效果,值得在临床上推广使用。

  1. Observation on the Curative Effect of the Combined Therapy of Omeprazole and Rabeprazole on Peptic Ulcer%奥美拉唑联合雷贝拉唑治疗消化性溃疡疗效观察

    Institute of Scientific and Technical Information of China (English)

    饶媛

    2015-01-01

    目的:观察奥美拉唑联合雷贝拉唑治疗消化性溃疡疗效。方法:回顾性分析我院2013年6月-2015年6月收治的90例消化性溃疡患者的临床资料,根据不同治疗方案分为两组(各45例),对照组予以奥美拉唑治疗,研究组联合雷贝拉唑治疗,观察并比较两组临床疗效及不良反应情况。结果:研究组总有效率比对照组明显升高(95.55% vs 73.33%,P<0.05);研究组不良反应总发生率比对照组略低(6.67% vs 11.11%,P>0.05)。结论:奥美拉唑联合雷贝拉唑治疗消化性溃疡疗效显著,且安全性高,值得临床推广及应用。%Objective: To observe the curative effect of the combined therapy of omeprazole and rabeprazole on peptic ulcer. Methods: A retrospective analysis was performed on the clinical data from 90 peptic ulcer patients treated by our hospital during June 2013 and June 2015 , and they were divided into two groups according to the different treatment options (each 45 cases). The control group was treated by omeprazole, and the research group was treated by combined therapy of omeprazole and rabeprazole. The clinical efficacy and adverse reactions of these two groups were observed and compared. Results: The total effective rate of the research group was higher than that of the control group ((95.55% vs 73.33%, P0.05). Conclusion: the combined therapy of omeprazole and rabeprazole has a significant curative effect on peptic ulcer, and meanwhile, this therapy is of high safety.Therefore, it is worthwhile to be popularized and widely applied.

  2. Study on Omeprazole Medication Effect in Treatment of Upper Digestive Tract Hemorrhage Caused by Gastritis%奥美拉唑治疗胃炎致上消化道出血的效果研究

    Institute of Scientific and Technical Information of China (English)

    佟春艳

    2015-01-01

    目的:研究胃炎致上消化道出血应用奥美拉唑治疗的临床效果。方法选取我院2013年12月~2014年12月间收治的胃炎致上消化道出血患者47例,对照组应用常规剂量的奥美拉唑静滴治疗,研究组应用大剂量的奥美拉唑静滴治疗,对比两组临床效果。结果研究组总有效率(92.31%)与对照组(76.19%)比较相对较高,输血量少,两组治疗效果差异有统计学意义(P<0.05)。结论胃炎致上消化道出血应用大剂量的奥美拉唑治疗疗效确切,安全可靠,切实可行。%Objective Clinical efficacy of omeprazole medication in treatment of upper digestive tract hemorrhage caused by gastritis is to be studied. Methods Selected 47 patients of upper digestive tract hemorrhage caused by gastritis that were treated in hospital from December 2013 to December 2014,patients in control group were given omeprazole intravenous injection treatment with routine dosage,while patients in study group were given omeprazole intravenous injection treatment with excessive dosage,and then compared clinical treatment effects between two groups. Results Treatment efficacy in study group(92.31%)was much higher than that in control group(76.19%),and patients’blood transfusion amount in study group was less,there was a differential between two groups and such a differential had statistic valu(P<0.05). Conclusion Omeprazole medication is of efficacy and safety in treatment of upper digestive tract hemorrhage caused by gastritis.

  3. 奥美拉唑治疗新生儿应激性溃疡的效果观察%The Efficacy Observation of Omeprazole in Treatment of Neonatal Stress Ulcer

    Institute of Scientific and Technical Information of China (English)

    杨丹凤

    2015-01-01

    目的:观察新生儿应激性溃疡应用奥美拉唑注射治疗的临床效果。方法选取2013年10月~2014年10月间我院收治的应激性溃疡患儿45例,对照组应用常规药物治疗,观察组加用奥美拉唑注射治疗,对比两组治疗效果。结果经过治疗,观察组总有效率(91.30%)与对照组(81.82%)比较明显较高,两组临床疗效差异有统计学意义(P<0.05)。结论新生儿应激性溃疡应用奥美拉唑注射治疗能够控制溃疡发展,促进患儿病情恢复,起效迅速。%Objective The clinical efficacy of Omeprazole injection in treatment of neonatal stress ulcer is to be observed. Methods Chose 45 neonatal patients with stress ulcer who were treated in hospital from October 2013 to October 2014 and separated them into control group and study group at random. Patients in control group were given conventional medicine treatment, while patients in study group were given Omeprazole injection treatment, and then observe and compare the treatment efficacy of the two groups. Results The treatment efficiency in study group was up to 91.30% and the treatment efficiency in control group was up to 81.82%,there was a treatment differential between the two groups, and such a differential had statistic value(P<0.05).Conclusion Omeprazole injection treatment is effective and rapid to control neonatal stress ulcer degeneration and improve patients’ recovery. Thus, Omeprazole injection treatment is quite worthwhile to be promoted and applied.

  4. The Efficacy Analysis of Gastric Ulcer with Omeprazole and Chinese Medicine%奥美拉唑联合中药制剂在胃溃疡的疗效分析

    Institute of Scientific and Technical Information of China (English)

    吴金芝

    2015-01-01

    目的:探究奥美拉唑联合中药制剂在胃溃疡的疗效分析。方法随机选取2013年2月-2014年2月间在该院进行治疗的胃溃疡患者100例,随机分为两组,每组50例,对照组患者采用奥美拉唑联合阿莫西林进行治疗,观察组在对照组的基础上加服中药制剂,观察两组患者的疗效。结果观察组患者治疗有效率为98%,对照组治疗有效率为74%,治疗总有效率比较(χ2=5.738,P=0.023),差异具有统计学意义,P<0.05。结论奥美拉唑联合中药制剂治疗胃溃疡的疗效优于单纯的西药联合治疗。%Objective To explore the efficacy of stomach ulcers with Omeprazole and Chinese medicine. Methods Selected 100 ulcer patients from February 2013 to February 2014 in our hospital for treatment,randomly divided into two groups of 50 people,in the control group patients were treated with omeprazole amoxicillin treatment, observation group on the basis of the control group plus service Chinese medicine, the efficacy of the two groups were observed. Results Effective treatment of patients in the obser-vation group was 98% in the control group was 74% effective treatment, the total effective rate of treatment (χ² = 5.738, P =0.023), a statistically significant (P<0.05). Conclusion The efficacy of Chinese medicine treatment of gastric ulcer Omeprazole is better than pure medicine combination therapy (such as omeprazole and amoxicillin).

  5. Long-term omeprazole and esomeprazole treatment does not significantly increase gastric epithelial cell proliferation and epithelial growth factor receptor expression and has no effect on apoptosis and p53 expression

    Institute of Scientific and Technical Information of China (English)

    Istvan Hritz; Laszlo Herszenyi; Bela Molnar; Zsolt Tulassay; Laszlo Pronai

    2005-01-01

    AIM: To study the effect of proton pump inhibitor (PPI)treatment on patients with reflux esophagitis and its in vivo effect on apoptosis, p53- and epidermal growth factor receptor (EGFR) expression.METHODS: After informed consent was obtained, gastric biopsies of the antrum were taken from patients with reflux oesophagitis prior to and after 6 mo of 20 mg omeprazole (n = 14) or 40 mg esomeprazole (n = 12) therapy.Patients did not take any other medications known to affect the gastric mucosa. All patients were Helicobacter pylori negative as confirmed by rapid urease test and histology,respectively. Cell proliferation, apoptosis, EGFR, and p53expression were measured by immunohistochemical techniques. At least 600 glandular epithelial cells were encountered and results were expressed as percentage of total cells counted. Was considered statistically significant.RESULTS: Although there was a trend towards increase of cell proliferation and EGFR expression both in omeprazole and esomeprazole treated group, the difference was not statistically significant. Neither apoptosis nor p53 expression was affected.CONCLUSION: Long-term PPI treatment does not significantly increase gastric epithelial cell proliferation and EGFR expression and has no effect on apoptosis and p53 expression.

  6. 奥美拉唑联合山莨菪碱治疗急性胰腺炎的临床研究%Omeprazole combined mountain scopolamine clinical research for the treatment of acute pancreatitis

    Institute of Scientific and Technical Information of China (English)

    朱健

    2014-01-01

    目的:探讨奥美拉唑联合山莨菪碱治疗急性胰腺炎的治疗效果。方法选取2010年1月~2013年12月在我院消化科治疗的急性胰腺炎病例160例,从中选出符合研究标准的样本病例50例进行回顾性分析。将50例病例按照单双数分成治疗组和对照组,每组病例各25例。两组病例采用不同的治疗方法,治疗组使用奥美拉唑联合山莨菪碱,并且附带常规治疗。奥美拉唑(常州四药制药有限公司)40mg,静脉输液2次/d,山莨菪碱20mg融入250ml生理盐水,静脉输液2次/d,治疗时间7d为一个疗程。对照组单独使用奥美拉唑(常州四药制药有限公司)40mg,静脉输液2次/d,7d为一个疗程。两组病例的常规治疗内容包括,禁食、禁水、胃肠减压、镇静、止痛、吸氧、保证电解质平衡、营养支持、适当的抗生素防止感染。结果治疗组在使用奥美拉唑联合山莨菪碱治疗后效果明显,治疗组总有效率为92%。对照组单独使用奥美拉唑进行治疗,总有效率为60%。从7d的治疗结果来看治疗组的效果明显要优于对照组。治疗组的各项病症消失较快,治疗组的治疗时长明显短于对照组。两组病例治疗前后,胆固醇(T C)、三酰甘油(T G)、低密度脂蛋白胆固醇(L D L-C)、高密度脂蛋白胆固醇CHDL-C)均存在明显改变。结论在急性胰腺炎的临床治疗中,奥美拉唑联合山莨菪碱的疗效优于单独使用奥美拉唑。%Objective to explore the omeprazole combined mountain scopolamine treatment effect for the treatment of acute pancreatitis.Methods from January 2010 to December 2010 in our hospital cases, 160 cases of digestive department treatment of acute pancreatitis, choose the standard sample cases of 50 cases were retrospectively analyzed. The 50 cases according to the number of single and double were divided into treatment group and control group, each group of 25

  7. Study on the Dissolution of Omeprazole Sodium Bicarbonate Magnesium Hydroxyl Tablets by HPLC%HPLC法测定奥美拉唑碳酸氢钠氢氧化镁片溶出度

    Institute of Scientific and Technical Information of China (English)

    彭东明; 王福东; 卢茂芳; 刘艳飞

    2012-01-01

    目的:建立奥美拉唑碳酸氢钠氢氧化镁片溶出度测定方法.方法:以水为溶出介质,采用高效液相色谱法测定奥美拉唑碳酸氢钠氢氧化镁片的溶出度.结果:奥美拉唑线性方程为A =5.45×105C -7.58×104 (r =0.999 9)线性范围:4.0~40.0μg·ml-1.平均回收率为99.86%;RSD为0.42%.结论:本法可用于奥美拉唑碳酸氢钠氢氧化镁片溶出度测定.%Objective; To establish a dissolution determination method for omeprazole sodium bicarbonate magnesium hydroxyl tablets. Method; The dissolution was determined by HPLC using water as the dissolution medium. Result; A good linear relationship was within the range of 4.0 ~40.0 jig Ml'' (r = 0.999 1, r = 0.999 8). The average recovery was 99. 86% ( RSD = 0.42% ). Conclusion; The method can be used in the dissolution determination of omeprazole sodium bicarbonate magnesium hydroxyl tablets.

  8. 以奥美拉唑为主的三联疗法治疗小儿消化性溃疡%Omeprazole-based Triple Therapy for Treatment of Children with Peptic Ulcer

    Institute of Scientific and Technical Information of China (English)

    詹璐

    2015-01-01

    目的:讨论研究应用以奥美拉唑为主的三联疗法治疗小儿消化性溃疡的临床疗效与意义。方法随机选取该院儿科消化性溃疡患者60例。随机分为A、B两组。 A组患者使用奥美拉唑、克拉霉素片及阿莫西林进行治疗;B组患者使用西咪替丁、克拉霉素片、阿莫西林治疗。比较两组患者治疗后总有效率以及幽门螺杆菌根除率等指标。结果A组以奥美拉唑为主使用三联疗法治疗后其幽门螺杆菌清除率86.7%显著优于其他药物组73.3%(P<0.05);A组以奥美拉唑为主三联疗法治疗后总有效率100%显著优于常规治疗B组93.3%(P<0.01)。结论应用以奥美拉唑为主的三联疗法治疗小儿消化性溃疡可有效提高幽门螺杆菌根除率。可缩短疾,病治疗时间并促进恢复,更能够显著降低疾病复发率,快速改善胃黏膜糜烂并抑制细菌闭合成。%Objective To discuss the clinical effect and significance of omeprazole-based triple therapy in children with peptic ulcer. Methods 60 children with peptic ulcer in our hospital. were randomly divided into A, B two groups. Patients in the group A was given triple therapy of omeprazole, clarithromycin tablets and amoxicillin; while those in the group B received treatment of cimetidine, clarithromycin tablets and amoxicillin. Indexes including the total efficiency and Helicobacter pylori eradication rate of the two group was compared. Results Clearance rate of 86% is significantly better than other drugs group 72% the Helicobacter pylori A group with omeprazole based triple therapy using after treatment (P<0.05);A group with omeprazole-based triple therapy after treatment, the total efficiency of 100%was significantly higher than that of conventional treatment and 96%in B group (P<0.05). Conclusion The application of omeprazole-based triple therapy for treatment of children with peptic ulcer can effectively improve the eradication of helicobacter pylori and

  9. 不同剂量奥美拉唑治疗溃疡性上消化道出血的疗效比较%Different Doses of Omeprazole in the Treatment of Ulcer of Upper Gastrointestinal Hemorrhage

    Institute of Scientific and Technical Information of China (English)

    段誉

    2014-01-01

    目的比较大剂量奥美拉唑和常规剂量奥美拉唑治疗溃疡性上消化道出血的治疗效果。方法选取156例患者随机分为治疗组和对照组各78例。治疗组院先给予奥美拉唑80mg加入生理盐水20ml缓慢静脉推注,约5~10min推完,然后再将奥美拉唑80mg加入生理盐水共50ml加入微量泵,以8mg/h的速度持续泵入,持续泵入72h;对照组院予奥美拉唑40mg加入生理盐水100ml,以q12h频率静脉滴注,用药72h。观察比较两组患者止血有效率、再出血情况、输红细胞悬液量、不良反应等。结果总有效率(<0.05)院治疗组94.8%,对照组总有效率为80.7%。72h再出血率(<0.05)院治疗组1.28%,对照组6.41%;平均每例输红细胞悬液输入量(<0.05)院治疗组(2.0±1.0)U,对照组(4.0±1.1)U;两组患者均无明显不良反应。结论大剂量奥美拉唑组对急性溃疡性上消化道出血止血效果明显优于常规剂量奥美拉唑组,无明显不良反应,且能缩短住院时间、节约患者住院费用,值得基层医院进一步推广应用。%Objective To compare high-dose omeprazole and routine dose of omeprazole in the treatment of ulcerative upper digestive tract hemorrhage treatment ef ect. Methods 156 patients were randomly divided into treatment group and control group with 78 cases in each. Treatment group:first given omeprazole 80mg join saline 20ml slow intravenous injection, about 5~10 minutes to finish, and then omeprazole 80mg join saline 50ml adding trace pump continuous infusion, with the speed of 8mg/h, continuous infusion of 72 hours; the control group: Omeprazole 40mg join saline 100ml, at a frequency of q12h intravenous drug use, 72 hours. The two groups were observed and compared hemostatic efficiency, rebleeding rate, transmission and suspension of red blood cells, adverse reaction. Results The total ef ective rate ( <0.05):treatment group 94.8%, control group total ef ectiveness is 80.7%;. 72

  10. 单纯手术修补结合奥美拉唑治疗胃溃疡穿孔33例%Simple Operative Repair Combined with Omeprazole in Treating 33 Cases of Gastric Ulcer Perforation

    Institute of Scientific and Technical Information of China (English)

    肖虹; 高少琳

    2013-01-01

    Objective To investigate the effect and the clinical value of simple operative repair combined with omeprazole in treating gastric ulcer perforation.Methods The clinical data of 63 patients with gastric ulcer perforation treated in this hospital from June 2007 and June 2012 were retrospectively analyzed.Among them,the control group(30 cases) was treated by repair alone while the treatment group(33 cases) was given omeprazole on the basis of simple operative repair.Then the effects were compared between the two groups.Results The two groups were successful in performing operation.But the effect in the treatment group was superior to that in the control group(P < 0.05).The incidence rates of the postoperative complications had no statistical difference between the two groups (P > 0.05).Conclusion The combination of simple operative repair combined with omeprazole has better effect for treating gastric ulcer perforation and deserves to be popularized in clinic.%目的 观察单纯手术修补结合奥美拉唑治疗胃溃疡穿孔的疗效,探讨其临床价值.方法 回顾性分析2007年6月至2012年6月胃溃疡穿孔患者63例的临床资料,其中对照组30例仅行单纯手术修补治疗,治疗组33例在单纯手术修补治疗基础上给予奥美拉唑治疗,比较两组疗效.结果 两组均顺利完成手术,治疗组疗效优于对照组(P<0.05);两组术后并发症发生率差异无统计学意义(P>0.05).结论 单纯手术修补结合奥美拉唑治疗胃溃疡穿孔效果良好,值得临床推广.

  11. Clinical study of omeprazole in the treatment of gastroesophageal reflux disease%奥美拉唑治疗胃食管反流病的临床研究

    Institute of Scientific and Technical Information of China (English)

    杜红霞

    2015-01-01

    Objective:To investigate the clinical curative effect of omeprazole in the treatment of gastroesophageal reflux disease(GERD).Methods:60 patients with GERD were selected from September 2013 to June 2014.They were randomly divided into the control group and the observation group with 30 cases in each.The observation group were given omeprazole enteric-coated tablets 20 mg/time,2 times/d;the control group were given ranitidine 150 mg/time,2 times/d.After 8 weeks of the treatment,we observed the changes of clinical symptoms score and endoscopic classification of two groups.Results:The changes of clinical symptoms score and endoscopic grading of the observation group were improved significantly better than those of the control group after the treatment.The total efficiency was 93.33%.Conclusion:The clinical curative effect of omeprazole for GERD is significantly.The curative effect is better than the H2 receptor antagonist ranitidine.%目的:探讨奥美拉唑治疗胃食管反流病(GERD)的临床疗效。方法:2013年9月-2014年6月收治GERD患者60例,随机分成对照组和观察组,各30例,观察组服用奥美拉唑肠溶片20 mg/次,2次/d;对照组服用雷尼替丁150 mg/次,2次/d。治疗8周后,观察两组的临床症状积分和内镜分级。结果:观察组治疗后的临床症状积分和内镜分级改善明显优于对照组,总有效率93.33%。结论:奥美拉唑治疗GERD疗效显著,且疗效优于H2受体阻滞剂雷尼替丁。

  12. Clinical Analysis on the Treatment of Peptic Ulcer by Ranitidine Hydrochloride Tablets Combine Omeprazole Sodium for Injection%雷尼替丁联合奥美拉唑治疗消化性溃疡的临床研究

    Institute of Scientific and Technical Information of China (English)

    孙晓春

    2015-01-01

    目的:探究消化性溃疡患者采用雷尼替丁联合奥美拉唑综合治疗的效果。方法选取2013年2月~2014年3月收治的40例消化性溃疡患者进行治疗,随机分组,实验组23例患者采用雷尼替丁和奥美拉唑的综合治疗,对照组17例患者选择雷尼替丁的治疗,对比疗效。结果实验组患者治疗有效率为91.30%,复发率为8.7%,对照组治疗有效率为76.47%,复发率为29.4%。两组患者的治疗效果和复发率差异有统计学意义(P<0.05)。结论消化性溃疡患者采用雷尼替丁和奥美拉唑的综合治疗,能够缓解恶心等胃肠道反应,复发率低,效果显著。%Objective To explore the effect on the treatment of peptic ulcer by ranitidine hydrochloride tablets combine omeprazole sodium for injection. Methods We divided the 40 patients into control group(17 cases)and experimental group(23 cases). Al the cases were chosen from February 2013 to March 2014. The patients in the experimental group adopted the ranitidine hydrochloride tablets combine omeprazole sodium for injection treatment and the control group adopted the ranitidine hydrochloride tablets treatment. We compared the difference beteen the two groups. Results The effective rate in the experimental group was 91.30%,and the recurrence rate was 8.7%. The effective rate in the control group was 76.47%,and the recurrence rate was 29.4%. It was in a high treatment efficiency and obvious difference between the two groups and the statistical y significant(P<0.05). Conclusion The patients with peptic ulcer adopt the ranitidine hydrochloride tablets combine omeprazole sodium for injection treatment wil obviously al eviate gastrointestinal reactions such as nausea. The recurrence rate was lower than others.

  13. 奥美拉唑治疗胃食管返流相关性肺炎的疗效观察%Observation of the Effect of Omeprazole on Infants with Pneumonia Related with Gastro Esophageal Reflux

    Institute of Scientific and Technical Information of China (English)

    杨海花

    2014-01-01

    Objective:to Observe the effect of Omeprazole in treatment of infants with pneumonia related with gastro esophageal reflux.Method:60 infants with pneumonia related with gastro esophageal reflux were divided into two groups randomly.The control group were treated with anti-infective,respiratory managemant,diet and body position,the treatment group were treated with Omeprazole(0.7mg/Kg.d)for one week in addition to those of control group.Results:the clinical symptoms and signs of the infants in the treatment group disappeared earlier than those in the control group.The total effective rate was 93.3% in the treatment group and 43.3% in the control group(χ2=5.76,P<0.05).Conclusion:Omeprazole is effective in treatment of infants with pneumonia related with gastro esophageal reflux.%目的:观察奥美拉唑治疗婴儿胃食管返流相关性肺炎的效果。方法:2011年6月至2014年5月郑州市儿童医院60例2-9月确诊为胃食管反流相关性肺炎的婴儿,随机分为治疗组30例和对照组30例,对照组予以改变体位和少量多次进食等方法,治疗组在对照组的基础上加用奥美拉唑静点0.7m g/K g . d,疗程1周。结果:治疗组显效、有效分别为15例和13例,总有效率93.3%,对照组显效、有效分别为7例和6例,总有效率为43.3%,两组比较差异有统计学意义(χ2=5.76,P<0.05)。结论:奥美拉唑治疗胃食管返流相关性肺炎安全有效。

  14. Effect Comparison of Omeprazole and Norepinephrine in Treating Ulcer Hemorrhage in the Newborn%奥美拉唑治疗新生儿应激性溃疡临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    姜小华; 吕艳; 宋晓松

    2012-01-01

    目的:探讨奥美拉唑治疗新生儿应激性溃疡的临床疗效.方法:将56例患应激性溃疡的新生儿随机分为治疗组30例和对照组26例,在综合治疗基础上,治疗组静脉注射奥美拉唑0.5 ~0.8 mg/(kg·d),1次/d,对照组给予去甲肾上腺素0.4 mg+NS 10 mL胃管内注入,每6 h一次,比较两种方法治疗新生儿应激性溃疡的疗效.结果:治疗组总有效率80.0%,对照组总有效率42.3%,两组比较差异有统计学意义(P<0.01).治疗组循环不良消失、胃肠功能紊乱消失、意识恢复、神经反射恢复及肌张力恢复时间均短于对照组,差异均有统计学意义(P<0.05).结论:奥美拉唑治疗新生儿应激性溃疡疗效显著,未见明显不良反应发生.%Objective: To observe the efficacy of omeprazole in treating stress ulcer hemorrhage in the newborn. Methods: Together 56 patients were divided into two groups randomly: treatment group ( n = 30 ) and control group ( n = 26 ). Besides the combined treatment, treatment group were given omeprazole injection, 0.5 ~0.8 mg/(kg ? D), while control group received norepinephrine 0.4 mg + NS 10 Ml injected into the stomach, once every 6 hours. The efficacy of two groups in treating stress ulcer hemorrhage of newborn was compared. Results; The total effective rate was 80. 0% in treatment group and 42. 3% in control group. There was significant difference between them (P<0.01). The disappearance time of poor circulation and gastrointestinal disorders, and the recovery time of consciousness, nerve reflex and muscle tension of the treatment group were shorter than those of the control group, the differences were statistically significant ( P<0.05 ). Conclusions; The efficacy of omeprazole is obvious for treating stress ulcer hemorrhage in newborn. . There is no obvious adverse reaction.

  15. Omeprazole combined thrombin treatment of neonatal upper gastrointestinal hemorrhage curative effect observation%奥美拉唑联合凝血酶治疗新生儿上消化道出血疗效观察

    Institute of Scientific and Technical Information of China (English)

    刘寒梅

    2013-01-01

    Objective:To observe the omeprazole,thrombin treatment effect for the treatment of neonatal upper gastrointestinal hemorrhage.Methods:In our hospital in March 2009-June 201 3.83 case of neonatal upper gastrointestinal hemorrhage were randomly divided into treatment group 42cases and control group 41 cases were performed in two groups of children actively treading the primary disease.Fast,and through the mouth or nasal insert gastric tube,with 1 .4%sodium bicarbonate solution gastric lavage,until eluate turned clear,intravenous drip etamsylate,etc.The treatment group in the treatment at the same time,using the stomach tube injection of thrombin,at the same time the use of omeprazole intravenous drip.The control group using omeprazole intravenous drip.Results:The total effective rate was 95.2% in treatment group and 68.3,% in observation group.There was significant difference between them(P<0.01 ).Conclusions:Omeprazole ,thrombin combination treatment of neonatal upper gastrointestinal hemorrhage curative effect is distinct,and less adverse reactions,is worthy of popu-larization and application.%目的:观察奥美拉唑、凝血酶治疗新生儿上消化道出血的治疗效果。方法:对我院2009年3月~2013年6月收治的83例新生儿上消化道出血的患儿,随机分为治疗组42例和对照组41例,两组患儿均给予积极治疗原发病,禁食,经口或经鼻插入胃管,用1.4%碳酸氢钠液洗胃,至洗出液转清亮为止,静脉滴注酚磺乙胺等,治疗组在上述治疗同时,采用胃管注入凝血酶,同时使用奥美拉唑静脉滴注;对照组使用奥美拉唑静脉滴注。结果:治疗组总有效率为95.2%,观察组总有效率为68.3%,两组比较,差异有统计学意义,P<0.01。结论:奥美拉唑、凝血酶联用治疗新生儿上消化道出血疗效显著,且不良反应少,值得推广应用。

  16. Deanxit combined with omeprazole and mosapride for gastroesophageal reflux disease in 129 senile patients%黛力新辅助奥美拉唑、莫沙必利治疗老年患者胃食管反流病的临床研究(129例)

    Institute of Scientific and Technical Information of China (English)

    冯永航; 高川

    2013-01-01

    Objective: To explore the efficacy of deanxit combined with omeprazole and mosapride in treatment of elderly patients with gastroesophageal reflux disease. Methods:A total of 129 elderly patients with gastroesophageal reflux disease in our hospital,were randomly assigned to omeprazole,mosapride combined with deanxit(n=70) or omeprazole plus mosapride(n=59). the clinical efficacy and reflux, heartburn symptom score of the two groups were evaluated. Results: The total effective rate was higner in omeprazole,mosapride combined with deanxit (94.28%) than in omeprazole plus mosapride (61.02%). Reflux and heartburn and other symptoms in two groups were improved, and reflux symptoms score was significantly lower in omeprazole,mosapride combined with deanxit than in omeprazole plus mosapride(P< 0.05); Conclusion: improvement effect on reflux, heartburn and other symptoms is better in omeprazole,mosapride combined with deanxit than in omeprazole plus mosapride in senile patients with gastroesophageal reflux disease, and worthy of clinical application.%  目的:观察黛力新辅助奥美拉唑、莫沙必利治疗老年人胃食管反流病的临床疗效。方法:选取我院收治的129例老年胃食管反流病患者,随机分为观察组70例和对照组59例,对照组采用奥美拉唑联合莫沙必利治疗,观察组在对照组基础上加用黛力新。观察治疗后两组患者临床疗效以及反酸、烧心症状评分。结果:治疗后观察组总有效率为94.28%,对照组为61.02%,观察组总有效率明显高于对照组(P <0.05);两组患者治疗后反酸和烧心等症状均有所改善,其中观察组4周后反酸症状评分明显低于对照组(P <0.05);2周末烧心症状评分观察组优于对照组(P <0.05)。结论:黛力新辅助奥美拉唑、莫沙必利治疗老年人胃食管反流病临床疗效明显,对反酸、烧心等症状有明显改善作用,值得临床推广应用。

  17. Um ensaio randomizado duplo-cego e controlado por placebo com probióticos em casos de supercrescimento bacteriano no intestino delgado em crianças tratadas com omeprazol

    Directory of Open Access Journals (Sweden)

    Badriul Hegar

    2013-08-01

    Full Text Available OBJETIVO: Avaliar a incidência de SBID em crianças tratadas com omeprazol e testar se os probióticos influenciam essa incidência. MÉTODOS: Um ensaio duplo-cego controlado por placebo foi realizado em 70 crianças tratadas oralmente, durante 4 semanas, com 20 mg de omeprazol por dia. Desses, 36 indivíduos receberam diária e simultaneamente Lactobacillus rhamnosus R0011 (1,9 x 10(9 cfu e Lactobacillus acidophillus R0052 (0,1 x 10(9 cfu (grupo probiótico, enquanto 34 receberam placebo (grupo placebo. O diagnóstico de SBID teve como base o desenvolvimento de sintomas sugestivos em combinação com um teste respiratório com glicose positivo. RESULTADOS: Após um mês de tratamento com IBP, 30% (21/70 apresentaram um teste respiratório positivo sugerindo SBID; desses, 62% foram sintomáticos. Cinco crianças desenvolveram sintomas parecidos com os de SBID, mas apresentaram um teste respiratório negativo; 44 (63% não apresentavam sintomas e tiveram teste respiratório negativo. Não houve diferença na incidência de testes respiratórios positivos no grupo probiótico em comparação ao grupo placebo (33% em comparação a 26,5%; p: 0,13. CONCLUSÕES: Como houve sintomas sugestivos de SBID em 26% das crianças tratadas com IBP e o teste respiratório com glicose deu resultados anormais em 72% delas, esse efeito colateral deve ser levado em consideração com mais frequência. O probiótico testado não reduziu o risco de desenvolver SBID.

  18. Low efficacy of an ultra-short term, once-daily dose triple therapy with omeprazole, azithromycin, and secnidazole for Helicobacter pylori eradication in peptic ulcer Baixa eficácia de um tratamento tríplice de curta duração, em dose única diária, para erradicação do Helicobacter pylori em pacientes ulcerosos com Omeprazol, Azitromicina e Secnidazol

    Directory of Open Access Journals (Sweden)

    Fernando Marcuz Silva

    2002-02-01

    Full Text Available PURPOSE: To determine the eradication rate of an ultra-short treatment schedule for Helicobacter pylori infection in a population with peptic ulcers, using omeprazole, secnidazole, and azithromycin in a once-daily dose for 3 days. METHODS: Thirty patients with peptic ulcer diagnosed by upper endoscopy and for Helicobacter pylori infection by rapid urease test and histologic examination received omeprazole 40 mg, secnidazole 1000 mg, and azithromycin 500 mg, administered once daily for 3 days. A follow-up exam was performed 12 weeks after the end of the treatment. Patients who were negative for Helicobacter pylori infection by rapid urease test and histologic examination were considered cured. RESULTS: Patients were predominantly female, and the mean age was 50 years. Duodenal peptic ulcer was found in 73% of the patients. Eradication was achieved in 9 of the 28 (32% patients as determined from the follow-up endoscopic exam. The eradication rate by intention to treat was 30%. Side effects were present in 3% of the patients, and compliance to treatment was total. CONCLUSIONS: In spite of the low rate of side effects and good compliance, the eradication index was low. A possible drawback of this therapy is that it reduces the efficacy of macrolide and nitroimidazole compounds in subsequent treatments.OBJETIVO: Testar a eficácia de um esquema ultra-curto de erradicação do H. pylori em uma população de ulcerosos, usando Omeprazol, Secnidazol e Azitromicina em dose única diária por três dias. PACIENTES E MÉTODOS: Trinta doentes portadores de úlcera péptica, documentada por exame endoscópico e com infecção pelo H. pylori confirmada pelo teste da urease e exame histológico, foram tratados com Omeprazol 40mg, Secnidazol 1000 mg e Azitromicina 500mg dados em dose única diária por três dias. Em controle endoscópico realizado 12 semanas após o término do tratamento, foram considerados curados da infecção os pacientes que apresentaram

  19. 奥美拉唑联合奥曲肽治疗肝硬化上消化道出血临床分析%Clinical analysis of omeprazole combined with octreotide in the treatment of upper gastrointestinal bleeding in liver cirrhosis

    Institute of Scientific and Technical Information of China (English)

    毛蓓

    2016-01-01

    目的:探讨奥美拉唑联合奥曲肽治疗肝硬化上消化道出血的效果。方法:收治肝硬化上消化道出血患者60例,随机分成单一组和联合组,单一组应用奥美拉唑治疗,联合组应用奥美拉唑联合奥曲肽治疗,比较两组的治疗效果。结果:在联合组,治疗效果明显优于单一组,止血时间明显短于单一组,输血量明显少于单一组(P<0.05)。结论:奥美拉唑联合奥曲肽治疗肝硬化上消化道出血的效果显著。%Objective:To explore the clinical effect of omeprazole combined with octreotide in the treatment of upper gastrointestinal bleeding in liver cirrhosis.Methods:60 patients with upper gastrointestinal bleeding in liver cirrhosis were selected. They were randomly divided into the single group and the combined group.Patients in the single group were treated with omeprazole,while patients in the combined group was treated with omeprazole combined with octreotide.We compared the treatment effect of two groups.Results:In the combined group,the treatment effect was better than the single group;the bleeding time was significantly shorter than the single group;the volume of blood transfusion was significantly less than the single group(P<0.05).Conclusion:The clinical effect of omeprazole combined with octreotide in the treatment of upper gastrointestinal bleeding in liver cirrhosis was significant.

  20. Clinical Observation of Omeprazole Treatment of Peptic Ulcer (with 142 Cases Analysis)%奥美拉唑治疗消化性溃疡的临床观察(附142例分析)

    Institute of Scientific and Technical Information of China (English)

    邓晓锋; 白慧荣

    2014-01-01

    目的:探讨临床上医护人员对消化性溃疡患者采用奥美拉唑的治疗效果。方法对我院接受检查和治疗的142例消化性溃疡患者入院资料进行分析,随机分为两组,每组有71例患者。对照组采用阿莫西林、果胶铋片和雷尼替丁治疗,实验组采用阿莫西林、果胶铋片、奥美拉唑治疗,比较两组患者临床治疗效果等指标。结果实验组患者临床治疗总有效率为97.18%,与对照组患者相比优势较大(总有效率为88.73%);实验组患者对我院治疗满意度达到96.34%,明显优于对照组患者。结论临床上,医护人员对消化性溃疡患者采用奥美拉唑治疗效果比较好,患者治疗后并发症较少,患者治疗后消化性溃疡痊愈率较高,且患者Hp转阴率高,值得推广使用。%Objective: To investigate the clinical staf on the treatment of peptic ulcer patients with omeprazole. Methods: hospital for examination and treatment of 142 cases of peptic ulcer patients admit ed to hospital were analyzed, were randomly divided into two groups of 71 patients. The control group, amoxicil in, tablets and ranitidine bismuth pectin treatment, experimental group amoxicil in, bismuth pectin films, omeprazole treatment, clinical outcomes were compared in patients with other indicators. Results: The clinical treatment of patients in the experimental group total ef ective rate was 97.18%, compared with the control group of patients the advantages of a large (total ef ective rate of 88.73%); experimental group patients in our hospital satisfaction reached 96.34%, significantly bet er than the control group patients. Conclusion: In clinical, medical treatment for peptic ulcer patients with omeprazole results were bet er, fewer complications in patients after treatment, the cure rate was higher in patients with peptic ulcer treatment, and the patient Hp negative rate, it is worth widely used.

  1. 奥美拉唑对肝癌HepG2细胞增殖与凋亡的影响%Effects of Omeprazole on the Proliferation and Apoptosis of Hepatoma Cell Line HepG2

    Institute of Scientific and Technical Information of China (English)

    魏艳; 梁宁林; 朱永军; 吴文超; 刘小菁; 杨丽

    2012-01-01

    Objective To investigate the effects of omeprazole (OME), a proton pump inhibitor, on the proliferation and apoptosis of human hepatoma cell line HepG2. Methods HepG2 cells were cultured to the logarithmic phase, and then treated with OME of different concentrations (10, 20, 40, 80, 160 mg/L) for 24 h or 48 h. Cell proliferation was evaluated by MTT assay, DNA synthesis was measured with 5 ethynyl-2'-deoxyuridine (Edu) fluorescent assay and the apoptosis of cells was measured by the Hoechst33342 assay. Results MTT assay showed that OME (40, 80 and 160 mg/L concentrations) could inhibit the proliferation of HepG2 cells for 24 h or 48 h treatment (P<0. 05) and 80 mg/L group has strongest effect. Compared with that of 24 h treatment, the same concentration of OME could inhibit HepG2 more significantly with 48 h treatment. After different concentrations of OME treatment for 24 h and then incubation with Edu for 2 h, compared with the control group, the proportion of Cells in S phase in 20, 40, 80, 160 mg/L groups decreased. Hoechst33342 staining demonstrated that treatment with OME (40,80,160 mg/L) for 24 h could significantly promote the cell apoptosis. Conclusion Omeprazole could inhibit human hepatoma cell line HepG2 cell proliferation and promote apoptosis.%目的 探讨质子泵抑制剂奥美拉唑(omeprazole,OME)对肝癌HepG2细胞增殖和细胞凋亡的影响.方法 不同浓度(0、10、20、40、80、160 mg/L)的OME作用于HepG2细胞后,分别于不同时间(24 h、48 h),采用甲基四唑蓝(MTT)法测定OME对HepG2细胞增殖的影响;5-乙炔基-2’-脱氧尿嘧啶核苷(Edu)荧光检测法测定DNA合成期(S期)细胞所占比例;Hoechst33342染色法检测细胞凋亡.结果 MTT结果示,10、20 mg/L OME对HepG2细胞增殖无明显抑制,而40、80、160 mg/L OME可产生明显抑制作用,其中80 mg/L OME作用最强;且相同浓度OME作用下,48 h较24 h对HepG2的抑制率增加.Edu荧光检测法表明,不同浓度OME处理细胞24h

  2. 不同厂家奥美拉唑肠溶胶囊释放曲线评价%Evaluation of release curve for omeprazole enteric-coated capsules made by different manufacturers

    Institute of Scientific and Technical Information of China (English)

    王震红; 杨永刚; 薛娇; 王新意

    2013-01-01

    Objective To evaluate the quality of omeprazole enteric-coated capsules overall by analyzing release curve. Methods Release curve of omeprazole enteric-coated capsules in 52 manufactures was determined to stud-y single batch consistency, consistency between batches and similarity of release curve. Results Single batch consistency of 32 manufactures was lack in 52 manufactures. Consistency between batches of 2 manufactures was bad in 5 manufactures. The similarity of release curve of 11 manufactures was poor in 20 manufactures of good RSD comparing with first investigative manufacture. Conclusion The release curve should be evaluated by centralized operating to promote standard work and to ensure the equivalence with first investigative manufacture.%目的 通过分析奥美拉唑肠溶胶囊释放曲线,全面评价国产奥美拉唑肠溶胶囊的质量.方法 测定52家生产企业的奥美拉唑肠溶胶囊的释放曲线,进行批内均一性、批间均一性及释放曲线相似性比较.结果 52家生产企业中32家批内均一性较差;5家生产企业中2家生产企业批间均一性较差;20家RSD符合要求的生产企业中,11家企业的产品与原研制剂释放曲线相似度较差.结论 上市后的产品可采用集中抽验方式进行释放曲线评价,促进生产企业严格规范的生产,保证国内产品与原研产品质量的一致性和等效性.

  3. Determination of residual organic solvent acetic acid in Omeprazole Magnesium by HPLC%HPLC 法测定奥美拉唑镁原料药中醋酸的残留量

    Institute of Scientific and Technical Information of China (English)

    李菊平; 刘效平; 金永亮

    2015-01-01

    目的:建立高效液相色谱法测定奥美拉唑镁原料药中有机溶剂醋酸含量。方法以色谱柱:以 X -Bridge TM C18(4.6 mm ×250 mm,5μm)为分离柱,采用等度洗脱,检测波长:210 nm。结果线性关系良好,方法精密度,重复性均符合要求。冰醋酸检测浓度线性范围为0.01~0.06 mg·mL -1(r =0.999994),低、中、高浓度平均回收率(n =9)分别为100.60%、100.38%、100.23%,RSD 分别为2.20%、2.21%、1.60%,最低检测限为0.0050 mg·mL -1。结论该方法可用于奥美拉唑镁原料药中残留溶剂醋酸含量的测定,限度为不得过0.05%(500 ppm)。%Objective To establish a method for the determination of residual acetic acid in Omeprazole Magnesium by HPLC Methods The X - Bridge TM C18(4. 6 mm × 250 mm,5 μm)column was adopted,temperature programming and FID detector was used. Results The solvent had good linear relationship and the precision and reproducibility of the meth-od were in accord with the requests. The linear range of acetic acid was 0. 01 ~ 0. 06 mg·mL - 1(r = 0. 999 994);The aver-age recovery rates of low,middle,high concentration(n = 9)were 100. 60% ,100. 38% ,100. 23% ,respectively and the RSDs were 2. 20% ,2. 21% ,1. 60% ,respectively;LOD was 0. 005 0 mg·mL - 1 . Conclusion This method could be used to determine residual acetic acid in Omeprazole Magnesium. The limit was not more than 0. 05%(500 ppm).

  4. 奥美拉唑、阿莫西林、甲硝唑治疗消化性溃疡的疗效观察%Curative Effect Observation of Omeprazole, Amoxicillin, Metronidazole for the Treatment of Peptic Ulcer

    Institute of Scientific and Technical Information of China (English)

    高红光

    2012-01-01

      Objective To summarize, amoxicillin, tinidazole omeprazole triple therapy on peptic ulcer. Methods 180cases of duodenal ulcer patients were randomly divided into treatment group and control group,90 cases in the treatment group, omeprazole, amoxicillin, metronidazole is composed of triple therapy;90 cases in the control group, with ranitidine, furazolidone, metronidazole is composed of triple therapy. Results By omeprazole metronidazole, amoxicillin, consisting of triple therapy for the treatment of duodenal ulcer with ranitidine, efficiency is significantly higher than that of the furazolidone, metronidazole is composed of triple therapy. Conclusion The triple drug omeprazole, amoxicillin, metronidazole for the treatment of peptic ulcer, fewer adverse reactions, good curative effect, for clinical application%  目的总结阿莫西林、替硝唑奥美拉唑、三联疗法对消化性溃疡的疗效。方法 180例十二指肠溃疡患者随机分为治疗组和对照组,治疗组90例,采用奥美拉唑、阿莫西林、甲硝唑组成的三联疗法治疗;对照组90例,采用雷尼替丁、呋喃唑酮、甲硝唑组成的三联疗法治疗。结果 由奥美拉唑、阿莫西林、甲硝唑组成的三联疗法治疗十二指肠溃疡有效率显著高于由雷尼替丁、呋喃唑酮、甲硝唑组成的三联疗法。结论 三联药物奥美拉唑、阿莫西林、甲硝唑治疗消化性溃疡,不良反应少,疗效好,适合临床推广

  5. 离子色谱法测定奥美拉唑镁原料药中硫酸盐的含量%Determination of sulfate omeprazole magnesium in raw medicine by Ion Chromatography

    Institute of Scientific and Technical Information of China (English)

    赵昌军; 高新贞

    2016-01-01

    Objective: to determine the content of sulfate omeprazole magnesium in raw medicine established by ion chromatography. Methods:thermo IonPac AS19 (50mm×4mm)anion exchange column and IonPac AG19 (50mm×4mm)anion protective column, eluent:3.6mmol/L sodium carbonate and 6 mmol / L sodium bicarbonate solution and velocity: 1.0mL/min, the column temperature: 30℃, the conductance pool temperature: 35℃, anion suppressor current 40mA, sample volume: 25μL. Results: The linear range of Sulfate was 0.1~40.0μg/mL (r=0.9996), the recovery rate was 100.3%. Conclusion: the method is accurate and reliable, and can be used for determination of omeprazole magnesium sulphate impurity in raw medicine.%目的:建立离子色谱法测定奥美拉唑镁原料药中硫酸盐的含量。方法:用Thermo IonPac AS19(250mm×4mm)阴离子交换柱和IonPac AG19(50mm×4mm)阴离子保护柱,淋洗液:3.6mmol/L碳酸钠和6mmol/L碳酸氢钠溶液,流速:1.0mL/min,柱温:30℃,电导池温度:35℃,阴离子抑制器电流40mA,进样量:25μL。结果:硫酸根酸根离子在0.1~40.0μg/mL范围内线性关系良好(r为0.9996),回收率为100.3%。结论:该方法准确可靠,可用于奥美拉唑镁原料药中硫酸盐杂质的测定。

  6. 自制胃炎II号片联合奥美拉唑胶囊治疗萎缩性胃炎临床初探%Clinical Study on the Treatment of Atrophic Gastritis With Gastritis II Number Plate Combined With Omeprazole Capsule

    Institute of Scientific and Technical Information of China (English)

    许邹华; 陆喜荣; 徐进康

    2016-01-01

    Objective To investigate the clinical effect of treating chronic atrophic gastritis with gastritis II tablet combined with omeprazole capsule. Methods100 patients with atrophic gastritis were randomly divided into A group (35 cases), group B (35 cases) and group C (30 cases). Group A was treated with gastritis II number plate combined with omeprazole capsule, B group was treated with the combination of the stomach and the spring and the omeprazole capsule, C group was treated with omeprazole capsule. The therapeutic effect of the three groups were compared.Results The clinical symptoms of the patients in the A group score in the treatment of 6 weeks and 12 weeks was higher than that of B group and C group (P<0.05). Conclusion Gastritis II number combined with omeprazole in treating atrophic gastritis has obvious curative effect, effectively improve the patient's clinical symptoms, improve the quality of life of patients.%目的:探讨研究胃炎II号片联合奥美拉唑胶囊治疗慢性萎缩性胃炎的临床效果。方法选择符合标准的100例患有萎缩性胃炎患者,随机分成A组(35例)、B组(35例)和C组(30例)。A组采用胃炎II号片联合奥美拉唑胶囊进行治疗;B组采用胃复春联合奥美拉唑胶囊进行治疗;C组采用奥美拉唑胶囊进行治疗。比较三组患者的治疗效果。结果 A组患者的临床症状评分在治疗6周与12周后均高于B组与C组(P<0.05)。结论胃炎II号片联合奥美拉唑治疗萎缩性胃炎具有明显的疗效,有效改善患者的临床症状,提高患者的生活质量。

  7. To Investigate the Efficacy of Octreotide Combined with Omeprazole in Treating Gastrointestinal Bleeding%奥曲肽联合奥美拉唑对上消化道出血的疗效分析

    Institute of Scientific and Technical Information of China (English)

    杨睿

    2014-01-01

    上消化道出血作为消化内科上的一种常见急症,主要是指涵盖屈氏韧带及以上消化道病变诱发的出血,其中胃、食管、十二指肠、胰胆、空肠病出血尤为突出,临床多表现为黑便、呕血,严重情况下易出现急性周围循环衰竭。本文主要立足于上消化道出血角度,深入探究奥美拉唑联合奥曲肽治疗方案对其的应用价值。%The upper gastrointestinal bleeding as a common emergency in the history of digestive diseases,is mainly refers to cover closely ligament and above the digestive tract lesions induced bleeding,including stomach,esophagus,duodenum,pancreas bile,especial y jejunum bleeding disease, clinical manifestations of the black,hematemesis,more around the most case of severe acute circulatory failure. In this paper,based on the Angle of upper gastrointestinal bleeding,delve into omeprazole combined the octreotide therapy for its application value.

  8. Development and Validation of a Novel Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Related Substances of Ketoprofen and Omeprazole in Combined Capsule Dosage Form.

    Science.gov (United States)

    Koppala, Srinivasarao; Reddy, V Ranga; Anireddy, Jaya Shree

    2016-01-01

    A novel, simple, sensitive, selective and reproducible stability-indicating high performance liquid chromatographic method was developed for the quantitative determination of degradation products and process-related impurities of ketoprofen (KET) and omeprazole (OMZ) in combined oral solid dosage form. Chromatographic separation was achieved on a Phenomenex Luna C18 (2) column (150 × 4.6 mm, 5 μm) under gradient elution by using a binary mixture of potassium dihydrogen phosphate buffer and acetonitrile at a flow rate of 0.8 mL/min. Chromatogram was monitored at 233 nm for KET impurities and at 305 nm for OMZ impurities using a dual wavelength UV detector. Resolution for KET and OMZ and 14 impurities was found to be >1.5 for any pair of components. Typical retention behaviors of impurities at various pH values were depicted graphically. To prove the stability-indicating power of the method, the drug product was subjected to hydrolytic, oxidative, photolytic, humidity and thermal stress conditions as per ICH. The developed method was validated according to the current ICH guidelines for specificity, limit of detection, limit of quantification, linearity, accuracy, precision, ruggedness and robustness.

  9. 国产奥美拉唑治疗急性非静脉曲张性上消化道出血的Meta分析%Effectiveness and Safety of China-Made Omeprazole in Treating Acute Non-Variceal Upper Gastrointestinal Bleeding: A Meta-Analysis

    Institute of Scientific and Technical Information of China (English)

    刘文平; 黄彩云

    2013-01-01

    目的 系统评价国产奥美拉唑治疗急性非静脉曲张性上消化道出血的疗效和安全性.方法 计算机检索PubMed、MEDLINE、Springer、The Cochrane Library、CNKI、VIP、CBM、WanFang Data等数据库,收集国产奥美拉唑治疗急性非静脉曲张性上消化道出血的随机对照试验(RCT),检索时限均为建库至2012年12月,并追溯纳入研究的参考文献.由两位研究者按照纳入与排除标准独立筛选文献、提取资料和评价质量后,采用RevMan 5.1软件进行Meta分析.结果 纳入11个RCT,共1 075例患者(试验组544例,对照组531例).Meta分析结果显示,国产奥美拉唑与进口奥美拉唑相比,在急性非静脉曲张性上消化道出血的总有效率[OR=0.68,95%CI (0.35,1.33),P=0.26]和不良反应发生率[RR=1.33,95%CI (0.45,3.91),P=0.60]方面,两组差异无统计学意义.结论 国产奥美拉唑治疗急性非静脉曲张性上消化道出血疗效与进口奥美拉相当,安全有效.%Objective To systematically evaluate the effectiveness and safety of China-made omeprazole in treating acute non-variceal upper gastrointestinal bleeding.Methods Such databases as PubMed,MEDLINE,Springer,The Cochrane Library,CNKI,VIP,CBM and WanFang data were searched to collect the randomized controlled trials (RCTs)about China-made omeprazole in treating acute non-variceal upper gastrointestinal bleeding,and the references of included studies were also retrieved.The retrieval time was from inception to December 2012.Two reviewers independently screened the literature according to the inclusion and exclusion criteria,extracted the data,and assessed the quality,and then the meta-analysis was conducted by using RevMan 5.1 software.Results A total of 11 RCTs were included.Among all 1 075 patients,544 were in the treatment group,while the other 531 were in the control group.The results of metaanalysis showed that,there were no significant differences in the total effective rate (OR=0.68,95

  10. Omeprazole Induces NAD(P)H Quinone Oxidoreductase 1 via Aryl Hydrocarbon Receptor-Independent Mechanisms: Role of the Transcription Factor Nuclear Factor Erythroid 2–Related Factor 2

    Science.gov (United States)

    Zhang, Shaojie; Patel, Ananddeep; Moorthy, Bhagavatula; Shivanna, Binoy

    2015-01-01

    Activation of the aryl hydrocarbon receptor (AhR) transcriptionally induces phase I (cytochrome P450 (CYP) 1A1) and phase II (NAD(P)H quinone oxidoreductase 1 (NQO1) detoxifying enzymes. The effects of the classical and nonclassical AhR ligands on phase I and II enzymes are well studied in human hepatocytes. Additionally, we observed that the proton pump inhibitor, omeprazole (OM), transcriptionally induces CYP1A1 in the human adenocarcinoma cell line, H441 cells via AhR. Whether OM activates AhR and induces the phase II enzyme, NAD(P)H quinone oxidoreductase 1 (NQO1), in fetal primary human pulmonary microvascular endothelial cells (HPMEC) is unknown. Therefore, we tested the hypothesis that OM will induce NQO1 in HPMEC via the AhR. The concentrations of OM used in our experiments did not result in cytotoxicity. OM activated AhR as evident by increased CYP1A1 mRNA expression. However, contrary to our hypothesis, OM increased NQO1 mRNA and protein via an AhR-independent mechanism as AhR knockdown failed to abrogate OM-mediated increase in NQO1 expression. Interestingly, OM activated Nrf2 as evident by increased phosphoNrf2 (S40) expression in OM-treated compared to vehicle-treated cells. Furthermore, Nrf2 knockdown abrogated OM-mediated increase in NQO1 expression. In conclusion, we provide evidence that OM induces NQO1 via AhR-independent, but Nrf2-dependent mechanisms. PMID:26441083

  11. Development of RP UPLC-TOF/MS, stability indicating method for omeprazole and its related substances by applying two level factorial design; and identification and synthesis of non-pharmacopoeial impurities.

    Science.gov (United States)

    Jadhav, Sushant Bhimrao; Kumar, C Kiran; Bandichhor, Rakeshwar; Bhosale, P N

    2016-01-25

    A new UPLC-TOF/MS compatible, reverse phase-stability indicating method was developed for determination of Omeprazole (OMP) and its related substances in pharmaceutical dosage forms by implementing Design of Experiment (DoE) i.e. two level full factorial Design (2(3)+3 center points=11 experiments) to understand the Critical Method Parameters (CMP) and its relation with Critical Method Attribute (CMA); to ensure robustness of the method. The separation of eleven specified impurities including conversion product of OMP related compound F (13) and G (14) i.e. Impurity-I (1), OMP related compound-I (11) and OMP 4-chloro analog (12) was achieved in a single method on Acquity BEH shield RP18 100 × 2.1 mm, 1.7 μm column, with inlet filter (0.2 μm) using gradient elution and detector wavelength at 305 nm and validated in accordance with ICH guidelines and found to be accurate, precise, reproducible, robust and specific. The drug was found to degrade extensively in heat, humidity and acidic conditions and forms unknown degradation products during stability studies. The same method was used for LC-MS analysis to identify m/z and fragmentation of maximum unknown impurities (Non-Pharmacopoeial) i.e. Impurity-I (1), Impurity-III (3), Impurity-V (5) and Impurity-VIII (9) formed during stability studies. Based on the results, degradation pathway for the drug has been proposed and synthesis of identified impurities i.e. impurities (Impurity-I (1), Impurity-III (3), Impurity-V (5) and Impurity-VIII (9)) are discussed in detail to ensure in-depth understanding of OMP and its related impurities and optimum performance during lifetime of the product.

  12. Observation Clinical Effect of Omeprazole Combine With Octreotide in Treatment of 65 Cases With Upper Gastrointestinal Hemorrhage%65例奥美拉唑联合奥曲肽治疗上消化道出血的临床观察

    Institute of Scientific and Technical Information of China (English)

    牛月华

    2015-01-01

    Objective Survey the effect of omeprazole combined with octreotide in the treatment of upper gastrointestinal hemorrhage. Methods Selected 65 patients with upper digestive tract hemorrhage form January 2014 to March 2015 in our hospital as the research object, randomly divided into the observation group (33 cases, octreotide combined omeprazole) and control group ( 32 cases, treated with omeprazole ), the clinical efifcacy and adverse reactions were compared. ResultsThe total effective rate of observation group was higher than the control group. The incidence of adverse reactions in observation group was lower than the control group,P<0.05, had difference statistically signiifcance. Conclusion The effect of omeprazole combined with octreotide in the treatment of upper gastrointestinal hemorrhage is good, and acting fast, effectively reduce the incidence of adverse reactions.%目的:观察分析奥美拉唑联合奥曲肽治疗上消化道出血的临床效果。方法选取2014年1月~2015年3月来本院就诊的上消化道出血患者65例作为研究对象,随机分为观察组33例(奥曲肽联合奥美拉唑治疗)与对照组32例(奥美拉唑进行治疗),比较两组患者的临床疗效、不良反应发生情况。结果观察组治疗总有效率为93.94%,高于对照组的75%,观察组不良反应发生率为15.15%,低于对照组的34.38%,P<0.05,差异具有统计学意义。结论奥美拉唑联合奥曲肽治疗上消化道出血效果理想,见效快,能效降低不良反应发生率。

  13. The compatibility between compound amino acid injection (18AA-VII) and Omeprazole Sodium for injection%复方氨基酸注射液(18AA-VII)与注射用奥美拉唑钠存在配伍禁忌

    Institute of Scientific and Technical Information of China (English)

    程菲

    2015-01-01

    Objective:To study the compatibility of compound amino acid injection (18AA-VII) and Omeprazole Sodium for injection. Methods a retrospective analysis was performed on 1 patients with simultaneous injection of compound amino acid injection (18AA-VII) and omeprazole sodium. Results:injection of compound amino acid injection for patients with injection of omeprazole sodium, found that the scalp needle in the liquid into a white turbid liquid. Conclusion:There is a compatibility between compound amino acid injection (18AA-VII) and Omeprazole Sodium for injection. If you need a combination of drugs, in the middle of the use of the two, physiological salineshould be used to flush the catheter.After using,the nurse should observe the patient’s condition changes for ten minutes,in order to avoid adverse reactions.%目的:研究复方氨基酸注射液(18AA-VII)与注射用奥美拉唑钠是否存在配伍禁忌。方法采用回顾性分析法对1例患者同时注射复方氨基酸注射液(18AA-VII)与奥美拉唑钠的情况进行分析。结果在注射复方氨基酸注射液的同时为患者注射奥美拉唑钠,发现头皮针内液体变成白色浑浊液体。结论复方氨基酸注射液(18AA-VII)与注射用奥美拉唑钠存在配伍禁忌。临床上如果需要联合用药时,两者间应用生理盐水冲管,用完后,护士应在病床前观察10 min,以免发生不良反应。

  14. Clinical Observation of Pingwei Powder Combined with Omeprazole in the Treatment of Helicobacter Pylori Associated Peptic Ulcer%平胃散联合奥美拉唑治疗幽门螺杆菌相关性消化性溃疡的临床观察

    Institute of Scientific and Technical Information of China (English)

    申仲能

    2014-01-01

    Objective To observe the clinical ef ect of Pingwei Powder Combined with omeprazole on Helicobacter pylori associated peptic ulcer. Methods 140 cases of peptic ulcer patients as the research object, randomly divided into observation group and control group with 70 cases in each. The control group used omeprazole, clarithromycin and amoxicil in treatment, the observation group with Pingwei Powder Combined with omeprazole treatment, to observe the ef ect of therapy ef ect of two group and Hp. Results In the observation group, the treatment ef iciency (94.29%), group of eradication rate of Helicobacter pylori (88.57%) was significantly higher than the control group ( <0.05). Conclusion Pingwei Powder Combined with omeprazole in the treatment of Helicobacter pylori associated peptic ulcers, gastrointestinal symptoms, Hp eradication rate is high, clinical curative ef ect.%目的观察分析平胃散联合奥美拉唑治疗幽门螺杆菌相关性消化性溃疡的临床疗效。方法选取140例消化性溃疡患者作为研究对象,采用数字表法随机平分成观察组和对照组各70例。对照组采用奥美拉唑+克拉霉素+阿莫西林治疗,观察组采用平胃散联合奥美拉唑治疗,观察两组治疗效果及Hp的根除情况。结果观察组治疗有效率(94.29%)、组幽门螺杆菌根除率(88.57%)明显高于对照组(<0.05)。结论平胃散联合奥美拉唑治疗幽门螺杆菌相关性消化性溃疡,消化道症状缓解快,Hp根除率高,临床疗效确切。

  15. Observation of the clinical efficacy of omeprazole,tinidazole combined with clarithromycin in the treatment of helicobacter pylori infection%奥美拉唑、替硝唑联用克拉霉素三联疗法治疗幽门螺杆菌感染的临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    王东升

    2014-01-01

    To explore the clinical efficacy of omeprazole,tinidazole combined with clarithromycin in the treatment of helicobacter pylori infection.Methods:220 cases with helicobacter pylori infection were selected from March 2009 to March 2010. They were randomLy divided into the treatment group and the control group with 110 cases in each.The treatment group were treated with omeprazole,tinidazole and clarithromycin,and the control group were treated with omeprazole,metronidazole, amoxicillin.We observed the therapeutic effect of the two groups.Results:In the remission rate,hp eradication rate,adverse reactions and the ulcer healing rate,two groups had no significant difference(P>0.05).Conclusion:The clinical efficacy of omeprazole,tinidazole combined with clarithromycin in the treatment of helicobacter pylori infection is good.%目的:探讨奥美拉唑、替硝唑联用克拉霉素三联疗法治疗幽门螺杆菌(Hp)感染的临床疗效。方法:2009年3月-2010年3月收治Hp感染患者220例,随机分为治疗组和对照组各110例。治疗组采用奥美拉唑、替硝唑、克拉霉素治疗,对照组采用奥美拉唑、甲硝唑、阿莫西林治疗,观察两组的治疗效果。结果:在症状缓解率、Hp根除率、不良反应和溃疡治愈率方面,两组差异无统计学意义(P>0.05)。结论:奥美拉唑、替硝唑联用克拉霉素三联疗法治疗Hp感染的临床疗效是良好的。

  16. Analysis of Curative Effect of Propranolol Combined With Omeprazole on Gastric Ulcer Patients With Liver Cirrhosis%普萘洛尔联合奥美拉唑对肝硬化并胃溃疡的疗效影响分析

    Institute of Scientific and Technical Information of China (English)

    赵学娟

    2016-01-01

    Objective To explore the therapeutic effect of propranolol combined with omeprazole on gastric ulcer in patients with liver cirrhosis.Methods The data of 152 patients with liver cirrhosis and gastric ulcer in our hospital from June 2014 to December 2015 were analyzed retrospectively. According to the different drug treatment,the patients were divided into two groups,omeprazole treatment was given to the control group, the observation group given propranolol combined with omeprazole in the treatment,and the two treatment curative effect and adverse reaction were observed.ResultsThe effective rate of the observation group was 90.91%,higher than the control group,and the incidence of adverse reactions and the control group was not significantly different.Conclusion Propranolol plus omeprazole in treatment of liver cirrhosis and gastric ulcer patients have good results.%目的:探究普萘洛尔联合奥美拉唑对肝硬化并胃溃疡的治疗效果。方法回顾性分析我院2014年6月~2015年12月收治的152例肝硬化并胃溃疡患者资料,依照不同的药物治疗分为两组,对照组给予奥美拉唑治疗,观察组给予普萘洛尔联合奥美拉唑治疗,观察两组治疗效果及不良反应情况。结果观察组的治疗有效率为90.91%,高于对照组,不良反应发生率与对照组差异无统计学意义。结论运用普萘洛尔联合奥美拉唑对肝硬化并胃溃疡患者的治疗效果较好。

  17. Comparative study of the effects of omeprazole and rabeprazole on intestinal P-glycoprotein in rats%奥美拉唑与雷贝拉唑对大鼠肠道P-糖蛋白作用比较

    Institute of Scientific and Technical Information of China (English)

    方海明; 王佳佳; 章礼久; 许建明; 梅俏; 陆春霞

    2013-01-01

    OBJECTIVE To investigate the effects of consecutive administration of omeprazole or rabeprazole on the intestinal P-gp activity and protein expression in rats. METHODS 30 rats were divided into five groups randomly as omeprazlc, rabeprazole, verapamil, dexamethasone and control group, respectively. Drugs were given to rats by intragastnc administration once per day for 7 days. The control group was given the same dose of saline. On d8, rats were sacrificed, everted sac of jeju-num, ileum and colon were prepared quickly concentration of rhodamine 123 at AP side were analyzed by fluorescence spectro-photometer assays. Transport rates of rhodamine-123 were also caculated. Expressions of P-gp in jejunum, ileum and colon of rat were analyzed by immunohistochemistry assays. RESULTS After 90 min, the accumulated concentration of rhodamine-123 at AP side of the everted jejunum, ileum and colon segments in the omeprazole group was (2. 7 ± 0. 5) , (1. 95 ± 0. 21) ng·mL-1 and (0. 78 ± 0. 24) ng·mL-1 respectively. Transport rate of rhodamine-123 from BL to AP was (0. 05 ± 0. 01), (0. 04 ± 0. ()2)ng ·ml/-1·min-1 and (0. 01 ± 0. 01 )ng·mL -1·min -1 , respectively. Mean P-gp protein expression level on jejunum, ileum and colon was (0. 35 ± 0. 02), (0. 45 ± 0. 05) and (0. 43 ± 0. 07), respectively. Compared with the control group, the accumulated concentration and P-gp protein expression levels had significantly differences respectively (P<(). 05), while there were no differences between the transport rate. In rabeprazole group,, the accumulated concentration of rhodamine-123 at AP side the everted jejunum, ileum and colon segments was (4. 6 ± 1. 2), (2. 91± 0. 2)ng·mL-1 and (1. 4 ± 0. 4) ng·mL-1 , respectively. Transport rate was (0.11 ± 0. 05) , (0. 06 ± 0. 02) ng·mL-1 ·min-1 and (0. 02 ± 0. 01 )ng·mL-1 · min-1 , respectively. Mean P-gp protein expression level was (0. 42 ± 0. 05), (0. 47 ± 0. 06) and (0. 52 ± 0. 07), respectively. CONCLUSION

  18. Clinical observation on hematological adverse reactions of oral omeprazole in aged patients%老年反流性食管炎患者口服奥美拉唑的血液系统不良反应

    Institute of Scientific and Technical Information of China (English)

    王薇; 许乐

    2012-01-01

    Objective To discuss the hematological adverse reactions of oral omeprazole administration with convention dosage and treatment course in aged patients.Methods Four hundred and nine cases of reflux esophagitis by endoscopic diagnosis from Beijing Hospital during January 2000 to December 2010 were divided into three groups according to their ages: group A ( 168 cases) aged from 60 to 69 years,group B ( 152 cases) aged from 70 to 79 years and group C (89 cases) aged equal to or above 80 years.Each group of patients was randomly divided into three subgroups,A 1 ( 56 cases),B 1 ( 51 cases) and C 1 ( 30 cases ) were administered with oral omeprazole,20 mg,bid; A2 ( 56 cases ),B2 ( 51 cases ) and C2 ( 30 cases ) were administered with oral famotidine,20 mg,bid; A3 ( 56 cases),B3 ( 50 cases),C3 ( 29 cases ) and all above subgroups were administered with oral sucralfate,10 ml,tid.The treatment course lasted for one month.The clinical efficacy,WBC count,RBC count,the Hemoglobin level,platelet count,as well as the prothrombin time,thrombin time,activated partial thromboplastin time,fibrinogen,Plasma fibronectin and serum D-Dimer were tested and compared after 10-days and 30-days treatment.Results After the treatment,all the patients had alleviated symptoms,to varied extend,especially in subgroups treated with oral omeprazole and sucralfate.After 30 days' treatment,blood WBC counting in B1 subgroup declined to lower than normal values in two cases; PLT counting drops in 1 case; blood WBC dropped in 6 cases and PLT dropped in4 cases of the C1 subgroup;blood WBC counting dropped in 1 case and PLT dropped in 2 cases of the C2 subgroup.Hemoglutination did not show significant change in all groups (P > 0.05 ).Conclusion The hematological adverse reactions of oral omeprasole in aged patients,under convention dosage and treatment course,occured with age increase,especially for blood WBC and platelet counting.%目的 探讨口服常规剂量和疗程的奥美拉唑对老年反流

  19. 奥美拉唑与雷尼替丁治疗急性上消化道出血的荟萃分析%Meta analysis of efficacy and safety of omeprazole versus ranitidine in the treatment of upper gastrointestinal bleeding

    Institute of Scientific and Technical Information of China (English)

    曲连悦; 姜明燕

    2014-01-01

    目的:系统评价奥美拉唑与雷尼替丁治疗上消化道出血的疗效和安全性。方法电子检索PubMed、MEDLINE、The Cochrane Library、CNKI、VIP、CBM等数据库,收集奥美拉唑治疗上消化道出血的随机对照试验( RCT),检索时限均至2013年6月。采用RevMan软件进行Meta分析。结果纳入25项研究,共2497例患者(试验组1230例,对照组1267例)。根据干预措施的不同,将研究分为注射剂型、口服剂型及序贯治疗3个亚组分别进行Meta分析,结果显示:与雷尼替丁相比,奥美拉唑治疗上消化道出血的止血率分别为OR=5.39,95%CI=(4.18,6.96),P <0.05;OR =6.27,95%CI =(3.65,10.77),P <0.05;OR =3.69,95%CI =(2.65,5.15),P<0.05。二者不良反应发生率的Meta结果为OR=0.49,95%CI=(0.24,1.01),P=0.05。未见严重不良反应。结论与雷尼替丁相比,奥美拉唑治疗上消化道出血具有止血迅速、不良反应少等优点,是治疗上消化道出血安全、有效的药物。%Objective To estimate the efficacy and safety of omeprazole and ranitidine in the treatment of up-per gastrointestinal bleeding. Methods The studies which were about the omeprazole in the treatment of upper gastro-intestinal bleeding were collected by electronic retrieval PubMed,MEDLINE and The Cochrane Library,CNKI,VIP, CBM until June 2013. Revman 5. 0 software and publication bias were analyzed by funnel plots. Results 25 studies were selected,of which a total of 2 497 patients ( treatment group was 1 230 cases and control group was 1 267 cases) . According to different interventions, the research was divided into injection dosage forms, oral dosage forms and se-quential treatment forms. Meta analysis indicated that compared with ranitidine,the bleeding rate of omeprazole in the treatment of upper gastrointestinal bleeding OR =5. 39,95% CI = (4. 18,6. 96),P <0. 05;OR =6. 27,95% CI =(3. 65,10. 77),P<0. 05;OR=3. 69,95%CI=(2. 65,5. 15),P<0. 05 respectively

  20. TO COMPARE THE SAFETY AND EFFICACY OF THREE DIFFERENT, PROTON PUMP INHIBITORS OMEPRAZOLE, ESO M EPRAZOLE AND RABEPRAZOLE IN A TRIPLE DRUG REGIMEN IN PATIENTS WITH PEPTIC ULCER DISEASE IN THE ERADICATION OF H. PYLORI INFECTION

    Directory of Open Access Journals (Sweden)

    Margaret Viola

    2015-03-01

    Full Text Available Peptic ulcer disease continues to be issue especially due to its high prevalence in the developing world. Helicobacter pylori ( H. pylori infection associated duodenal ulcers should undergo eradication therapy. There are many regimens offered for H. pylori eradication which include triple , quadruple , or sequential therapy regimens. In our study we planned to see whether these differences in pharmacokinetic properties show any difference in t he efficacy and safety parameters between treatment with omeprazole rabeprazole and esomeprazole in the triple drug regimen for eradication of H.pylori infection in peptic ulcer patients in our hospital Osmania General Hospital / Osmania Medical College , Hyderabad. MATERIALS AND METHODS: A total number of 45 patients were enrolled in the study. Patients with either sex suffering from peptic ulcer defined as ulcer crater of >2.5mm in size by endoscopy. Study Design : It was a randomized double blind , paralle l and comparative study. CONCLUSION: Two weeks after triple drug treatment , H.pylori was negative in 66.7% , 73% and 80% and Rapid urease test was negative in 53% , 60% and 66% in group A , B and C respectively. Endoscopy findings showed significant reduction in size and healing of ulcers in group A , B and C. There was improvement in signs and symptoms by 53 to 80% , after 2 weeks. Hence after therapy with triple drug regimen H.pylori eradication was 66 - 80% and healing of ulcers was 83 – 100% which was higher in Rabeprazole group. At 6 weeks , there was complete relief of signs and symptoms. At the follow up of 10 weeks there was no ulcer recurrence. No adverse effects were noted in all the groups. In conclusion , Triple drug regimen had shown to eradicate H.pylori infection in the treatment of Peptic ulcer. There was healing of ulcers in all the groups which was highly significant. There was no recurrence of peptic ulcer with these regimens in all the groups. However Rabeprazole group patients

  1. 奥美拉唑对小鼠胸腺、脾脏免疫功能的影响%Effects of omeprazole on thymus and spleen immunity in mice

    Institute of Scientific and Technical Information of China (English)

    齐东江; 徐阿曼

    2015-01-01

    Objective To investigate if long-term use omeprazole( OME) will inhibit lysosomal in vivo in mice and its effect on the im-mune organs of mice.Methods Mice were divided into 3 group:control group,low dose OME group,high dose OME group,10 mice in each group.After 24 wk mice were sacrificed to collect samples and calculate the spleen index,ELISA was employed to assay the serum concentration of acid phosphatase(ACP)and N-acetyl -β-D-glucosaminidase(NAG).Results OME group compare with the control group,spleen weight index,thymus index decreased significantly,serum lysosomal enzyme levels also decreased significantly,the differences was satatically significant(P<0.05).Conclusion OME can inhibit the lysosomal hydrolase activity in mice,resulting in systemic immune function is impaired,thereby reducing immune function in mice.%目的:研究长期使用奥美拉唑( omeprazole,OME)是否会抑制小鼠体内溶酶体及其对小鼠免疫器官的影响。方法实验分为单纯对照组、OME低剂量组(6 mg· kg-1)、OME高剂量组(30 mg· kg-1),每组10只小鼠。饲养24周后处死小鼠, ELISA法检测小鼠血清及脾脏中酸性磷酸酶( acid phosphatase,ACP)、N-乙酰-β-D-氨基葡萄糖苷酶( N-acetyL-β-D-glucosamini-dase,NAG)含量,采集小鼠胸腺、脾脏并称重计算小鼠脾脏、胸腺重量指数。结果 OME组与对照组相比血清中溶酶体酶活性下降,两者差异具有统计学意义(P<0.05),同时小鼠脾脏及胸腺重量指数明显下降。结论 OME可以抑制小鼠体内溶酶体及其水解酶的活性,导致系统性免疫功能受损,从而降低小鼠免疫功能。

  2. Problems and countermeasures in domestic human bioequivalence studies for the oral preparations containing omeprazole or its salt%国内奥美拉唑(盐)口服制剂人体生物等效性试验的问题和对策

    Institute of Scientific and Technical Information of China (English)

    王晓琳; 刘会臣

    2011-01-01

    Omeprazole is a representative drug of the proton pump inhibitors (PPIs), and has been applied widely in clinical therapy. Here, we summarized 26 domestic references of human bioequivalence researches for the oral preparations containing omeprazole or its salt. The problems and countermeasures referred to experiment contents, reference preparations, subjects, collection and analysis of biological samples, pharmacokinetic parameters, and post-marketing bioequivalence re-evaluation or monitoring were described and discussed. The goal is to provide useful reference information for human bioequivalence research and clinical application of omeprazole or its salt. Based on the current research situation, it is advisable to carry out food-effect bioequivalence studies, exclude poor metabolizers from subjects in bioequivalence studies, choose corresponding original drugs as reference preparations, standardize bioanalytical method validation, and perform post-marketing bioequivalence re-evaluation or monitoring.%奥美拉唑是质子泵抑制剂类代表药物,临床上应用广泛.文中通过对国内26篇奥美拉唑(盐)12服制剂人体生物等效性试验文献进行分析,探讨了试验内容、参比制剂、受试者、生物样品采集及分析、药动学参数、上市后生物等效性再评价或监测等方面的问题和对策,以期为奥美拉唑(盐)口服制剂人体生物等效性研究和临床应用提供参考信息,并基于现有研究状况提出以下建议:开展食物影响研究、在受试者筛选时排除弱代谢者、参比制剂选择相同剂型的原创药、规范分析测定方法的确证并开展和加强奥美拉唑(盐)口服制剂的上市后生物等效性再评价或监测.

  3. COST-EFFECTIVENESS ANALYSIS OF APPLICATION OF TWO DIFFERENT TREATMENTS FOR UPPER GASTROINTESTINAL BLEEDING WITH OMEPRAZOLE%应用奥美拉唑的2种不同方案治疗上消化道出血的成本-效果分析

    Institute of Scientific and Technical Information of China (English)

    焦付哲

    2011-01-01

    [Objective] To investigate the cost-effectiveness of 2 kind of different treatments for the upper gastrointestinal hemorrhage with omeprazole. [Methods] Chose 82 patients with upper gastrointestinal hemorrhage from March 2008 to the March 2010, and divided them into two groups, the observation group and the control group. The patients in observation group were given l50mg ranitidine hydrochloride capsules orally, twice a day; intravenous injection with 40mg omeprazole, once a day; intravenous drip with 2.0g etamsylate in 500ml physiological saline, once a day. The patients in control group were given oral administration with 20mg omeprazole enteric-coated tablets, twice a day; 1.5g Almagate Suspension orally, twice a day; 2.0g etamsylate in 500ml physiological saline intravenously, once a day. All were given 7-day treatment course. Determined the costs and analyzed the cost effectiveness. [ Results] The total effective rates in two groups were not different (P > 0.05); after 1 unit of effect, the cost in the observation group was smaller than that in the control group. [Conclusion] The clinical effect of ranitidine hydrochloride capsules, omeprazole and etamsylate is remarkable, and the cost is small.%[目的]探讨应用奥美拉唑的2种不同方案治疗上消化道出血的成本一效果差异.[方法]选择2008年3月~2010年3月消化性溃疡所致上消化道出血患者82例,将以上患者随机分为两组,观察组和对照组.观察组患者给予盐酸雷尼替丁胶囊150mg口服,每天2次;奥美拉唑40mg静脉注射液,每天1次;酚磺乙胺2.Og加入生理盐水500ml中静脉滴注,每天1次.对照组患者给予奥美拉唑肠溶片20mg口服,每天2次;给予铝镁加混悬液1.5g口服,每天2次;给予酚磺乙胺2.0g加入生理盐水500ml中静脉滴注,每天1次.两组患者均治疗7d.确定两组患者成本.分析两组患者成本效果.[结果]两组患者总有效率比较,差异无统计学意义(P>O.05);获得1个单位

  4. The comparative study of efficacy on domperidone poly I:C and omeprazol in treatment of Helicobacter pylori negative chronic superficial gastritis%多潘立酮聚肌胞与奥美拉唑治疗Hp(-)慢性浅表性胃炎疗效的比较研究

    Institute of Scientific and Technical Information of China (English)

    冯盛才; 夏敏; 晏明君; 吴攀

    2011-01-01

    目的 比较多潘立酮聚肌胞与奥美拉唑治疗幽门螺杆菌(HP)阴性慢性浅表性胃炎的疗效.方法 选择确诊为慢性浅袁性胃炎且Hp(-)的患者89例,随机分为治疗组45例,对照组44例,治疗组采用多潘立酮聚肌胞治疗;对照组采用奥美拉唑治疗;3周后进行疗效观察;统计学处理.结果 治疗组总有效41例,显效28例,对照组总有效30例,显效13例,治疗组总有效率及显效率均明显高于对照组;统计学处理,差异有统计学意义.结论 治疗组的治疗效果优于对照组治疗效果.%Objective Compare domperidone polyI:C and omeprazol treatment Helicobacter pylori negative chronic superficial gastritis curative effect. Methods Selecting helicobacter pylori negative chronic superficial gastritis 89 cases diagnosed were randomly divided into the treatment group 45 cases and control group 44 cases, the treatment group using domperidone polyI:C treatment,the control group using omeprazol treatment, treated for 3 weeks, observation clinical manifestations. Results The total effective of treatment group got 41 cases, powerfully 28 cases and The total effective of control group got 29 cases, powerfully 11 cases. Conclusion Curative effects of treatment group are better than that of control group, Statistical processing, Significant differences.

  5. 定量5-羟奥美拉唑和奥美拉唑砜以探测中国人肝微粒体中CYP2C19和CYP3A4的活性%Probing CYP2C19 and CYP3A4 activities in Chinese liver microsomes by quantification of 5-hydroxyomeprazole and omeprazole suiphone

    Institute of Scientific and Technical Information of China (English)

    舒焱; 王连生; 肖卫民; 王伟; 黄松林; 周宏灏

    2000-01-01

    AIM: To develop an analytical method for simultaneous quantification of 5-hydroxyomeprazole (5-OH-OP) and omeprazole suffone (OPS), and explore whether omeprazole (OP) is an appropriate phenotypic probe for CYP2C19 and CYP3A4 in Chinese liver microsomes.METHODS: OP metabolism in vitro was conducted in Chinese liver microsomes, and the major metabolites 5-OH-OP and OPS were determined using high pressure liquid chromatography (HPLC). Monoclonal antibodies anti-CYP2C8/9/19 and anti-CYP3A4 were employed to conduct inhibition experiments. The protein contents of CYP2C19 and CYP3A4 were quantified using Western blot analysis and densitometric scanning. RESULTS:5-OH-OP and OPS gave a baseline resolution in the HPLC analysis. The detection limits for both compounds were 0.01 nmol and the recovery (98 % -102 %) had good precision with relative standard deviation of 87 % ). At a substrate concentration of 2 μmol/L OP, good correlations were found between OP 5-hydroxylation and S-mephenytoin 4'-hydroxylation activities ( r = 0.72, P 87%);在底物浓度为2 μmol/L OP时,中国人肝微粒体中OP的5-羟化与美芬妥英的4'-羟化活性之间(r=0.72,P<0.01)、OP的5-羟化活性与CYP2C19含量之间(r=0.82,P<0.01)以及OP的硫代氧化活性与CYP3A4含量之间(r=0.78,P<0.01)均有很好的相关性.结论:中国人肝微粒体中OP的代谢主要由CYP2C19和CYP3A4介导;采用本研究建立的HPLC方法,在适当的底物浓度下,OP能用于体外探测中国人肝微粒体中CYP2C19及CYP3A4的活性.

  6. 奥美拉唑联合血凝酶对老年胃溃疡伴出血的临床疗效及作用机制探讨%Study on efficacy and mechanism of omeprazole combined with hemocoagulase for gastric ulcer with bleeding in the elderly

    Institute of Scientific and Technical Information of China (English)

    胡渊文; 苏法; 王庆华

    2016-01-01

    Objective To observe the effect of omeprazole combined with hemocoagulase on serum levels of tumor necrosis factor ( TNF)⁃α, superoxide dismutase ( SOD) , vascular endothelial growth factor ( VEGF) and epidermal growth factor (EGF) in the elderly patients with gastric ulcer complicated with gastrorrhagia. Methods Ninety⁃eight elderly patients suffering from gastric ulcer complicated with gastrorrhagia from April 2013 to October 2014 were randomly divided into the observation group(n=48)and the control group(n=50). On basis of conventional therapy,the control group received omeprazole, while the observation group received omeprazole and hemocoagulase. The course of treatment was 2 months in two groups. The bleeding time, the effect of ulcer healing and the adverse reactions were recorded. The levels of TNF⁃α, SOD, VEGF and EGF between two groups were compared before and after the treatment. Results After treatment, the level of TNF⁃α was more significantly decreased ( P<0�05) ,and the levels of SOD, VEGF and EGF were more significantly increased( P<0�05) in the observation group than those in the control group. The hemostatic effect and the ulcer healing in the observation group was better than that in the control group ( P<0�05 ) . There was no significiant difference between the two groups in the incidence rate of adverse reactions. Conclusions Combining application of omeprazole and hemocoagulase to treat gastric ulcer complicated with gastrorrhagia show remarkable curative effect, which is worthy of extension in clinic.%目的:探讨奥美拉唑联合血凝酶治疗老年胃溃疡合并出血的治疗效果及其对肿瘤坏死因子( TNF⁃α)、超氧化物歧化酶( SOD)、血管内皮生长因子( VEGF)及表皮生长因子( EGF)的影响。方法选取2013年4月至2014年10月来我院就诊的老年胃溃疡伴出血患者98例,随机分为对照组和观察组,对照组50例,观察组48例。在常规综合治疗

  7. 奥美拉唑快速纠正先天性肥厚性幽门狭窄代谢性碱中毒的临床研究%The clinical study of omeprazole in rapid correction of metabolic alkalosis in congenital hypertrophic pyloric stenosis

    Institute of Scientific and Technical Information of China (English)

    孙邡; 刘斌; 张宏伟; 禚保彪; 刘丰丽; 方允

    2014-01-01

    Objetive To explore the function of omeprazole in rapid correction of metabolic alkalosis in congenital hypertrophic pyloric stenosis(CHPS). Methods 80 infants with CHPS were randomly divided into two groups,treatment group 40 cases,control group 40 cases.According to the pH on admission ,those patients were divided into pH>7.5 group (treatment group 21 cases,control group 22 cases),pH≤7.5 group (treat-ment group19 cases,control group18 cases ).The control group was given conventional normal saline,equilibri-um liquid to correct electrolyte and acid-base balance disorders,the treatment group in addition to routine thera-py was given omeprazole 0.7 mg/(kg.d)qd intravenous injection.The arterial blood gas analysis were detec-ted in every 12 h after admission,The SPSS13.0 software of statistics analyzed the primary data. Results pH>7.5 group:12 h after admission treatment group with 8 cases (8/21,38.1%)pH returned to normal,while control group only with 2 cases (2/22,9.1%),(P0.05).Conclusion Intravenous omeprazole administration can rapidly normalize severe meta-bolic alkalosis in CHPS patients,particularly for moderately severe metabolic alkalosis.As a result,pyloromyoto-my can be performed sooner reducing both hospital stay and costs.%目的:探讨奥美拉唑在快速纠正先天性肥厚性幽门狭窄代谢性碱中毒中的作用。方法将本院80例诊断为先天性肥厚性幽门狭窄的患儿随机分成两组,治疗组40例,对照组40例。根据入院时pH值又分为pH>7.5组(治疗组21例,对照组22),pH≤7.5组(治疗组19例,对照组18例)。对照组采用补充生理盐水、平衡液等纠正电解质紊乱及酸碱失衡,治疗组除采用上述治疗外加用奥美拉唑0.7 mg·kg-1·d-1静脉滴注,每日1次。入院后每12 h行动脉血气分析,数据通过SPSS13.0软件包进行统计学处理。结果 pH>7.5组:入院后12h治疗组有8例(8/21,38.1%)pH

  8. 奥美拉唑四联疗法合理饮食治疗十二指肠球部溃疡临床疗效观察%Clinical observation of omeprazole quadruple therapy + proper diet treatment of duodenal ulcer

    Institute of Scientific and Technical Information of China (English)

    王柏; 陈南燕

    2012-01-01

      目的探讨奥美拉唑四联疗法+合理饮食治疗十二指肠球部溃疡疾病的临床疗效. 方法 选取笔者所在医院收治的98例患者,采用奥美拉唑、克拉霉素、枸橼酸铋钾胶囊、阿莫西林四联疗法并辅以合理饮食进行治疗并观察疗效. 结果 奥美拉唑四联疗法+合理饮食治疗十二指肠溃疡总有效率达97.96%,幽门螺旋杆菌的根除率为96.93%,治疗十二指肠溃疡伴有明显腹痛腹胀嗳气返酸有效率为98.98%. 结论 奥美拉唑四联疗法治疗十二指肠球部溃疡效果显著,后期再配以合理饮食能使大多数消化道溃疡彻底根治.%  Objective To investigate the intractable duodenal ulcer disease, cure HP can significantly reduce the recurrence rate of ulcers. Plus the daily life of a reasonable diet and regular sports make the majority of peptic ulcer and complete cure. Methods 98 patients of the hospital, the adoption of quadruple therapy with omeprazole, clarithromycin, bismuth potassium citrate capsules, amoxicillin treatment effects were observed. Results Omeprazole quadruple therapy + proper diet treatment of duodenal ulcer total effective rate 97.96% 96.93% of the eradication rate of Helicobacter pylori, the treatment of duodenal ulcer associated with significant abdominal pain, abdominal distension and belching back to acid efficiency of 98.98%. Conclusion The omeprazole quadruple therapy for the treatment of duodenal ulcer effect was significant, post-matched to the proper diet is possible to cure peptic ulcer.

  9. L-谷氨酰胺呱仑酸钠颗粒联合奥美拉唑治疗儿童消化性溃疡病的临床研究及安全性观察%Study on Marzulene combined with Omeprazole for treating peptic ulcer disease and the safety of Marzulene in children

    Institute of Scientific and Technical Information of China (English)

    陈凤; 刘文莉; 耿岚岚; 谢晓莉; 郭艳芳; 朱朝敏

    2014-01-01

    ),Hp清除率为72.7%(24/33例).试验组与对照组相比,萎缩、出血缓解率差异有统计学意义(x2=66.67、15.05,P均<0.05).试验组和对照组临床有效率分别为98.7%(74/75例)、98.4%(62/63例),试验组和对照组胃镜有效率分别为98.5%(67/68例)、96.8%(61/63例).试验组患儿服用麦滋林8周内及停药后4周随访无不良反应.结论 麦滋林对于减轻儿童消化性溃疡病的临床表现及改善胃镜表现有一定疗效,对辅助治疗儿童消化性溃疡病有重要作用,且在儿童中使用具有较好的安全性.%Objective To assess the effect of Marzulene as an adjuvant therapy for peptic ulcer disease in children and the safety of Marzulene.Methods From Dec.2011 to Feb.2013,138 cases of peptic ulcer disease in children from Chongqing,Guiyang,Guangzhou,Chengdu and Xinjiang were randomly divided into trial group (n =75) and control group (n =63).The treatment protocls of the trial group was Marzulene combined with Omeprazole,and the control group gave Omeprazole only,all the cases with Helicobacter pylori (Hp) infection were treated by antibiotics,then clinical manifestations,gastroscopy and laboratory examinations were followed up after 8 weeks.Results The remission rates of clinical manifestations in the trial group were abdominal pain 91.8% (56/61 cases),vomiting 90.2%(37/41 cases),melena 92.9% (26/28 cases),nausea 93.1% (27/29 cases),hematemesis 89.5% (17/19 cases),abdominal discomfort 100.0% (19/19 cases),abdominal distension 100.0% (11/11 cases),sour regurgitation 100.0% (9/9 cases),ozostomia 90.0% (9/10 cases),eructaion 88.9 % (8/9 cases),bloody stools 100.0% (4/4 cases),poor appetite 50.0% (1/2 case),and abdominal tenderness 89.3 % (50/56 cases) ;the remission rates of clinical manifestations in the control group were abdominal pain 90.4% (47/52 cases),vomiting 89.7% (26/29 cases),melena 96.4%(27/28 cases),nausea 87.5 % (21/24 cases),hematemesis 92.9 % (13/14 cases

  10. Omeprazole and Ranitidine in the Prevention of Relapse in Patients with Duodenal Ulcer Disease

    Directory of Open Access Journals (Sweden)

    K Lauritsen

    1999-01-01

    Full Text Available BACKGROUND: Although the eradication of Helicobacter pylori is of primary importance when initiating treatment, it is also important to have a strategy for patients who are H pylori-negative, fail to demonstrate eradication or have a tendency to become re-infected or relapse.

  11. Potentiation of the action of metronidazole on Helicobacter pylori by omeprazole and bismuth subcitrate

    DEFF Research Database (Denmark)

    Andersen, L P; Colding, H; Kristiansen, J E

    2000-01-01

    Treatment failures using triple therapy that include metronidazole, are common in patients infected with metronidazole-resistant Helicobacter pylori in the gastric mucosa. Higher eradication rates in such patients have been described when treatment regimens include bismuth salts compared...

  12. Pharmacokinetic drug interaction profile of omeprazole with adverse consequences and clinical risk management

    OpenAIRE

    2013-01-01

    Wei Li,1 Su Zeng,2 Lu-Shan Yu,2 Quan Zhou31Division of Medical Affairs, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, People’s Republic of China; 2Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People’s Republic of China; 3Department of Pharmacy, Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, People’s Republic of ChinaBac...

  13. Buspirone, fexofenadine, and omeprazole: Quantification of probe drugs and their metabolites in human plasma

    OpenAIRE

    Gor, Parul; Alnouti, Yazen; Reed, Gregory A.

    2011-01-01

    Probe drugs are critical tools for the measurement of drug metabolism and transport activities in human subjects. Often several probe drugs are administered simultaneously in a —cocktail . This cocktail approach requires efficient analytical methods for the simultaneous quantitation of multiple analytes. We have developed and validated a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of three probe drugs and their metabolites in human plasma. The anal...

  14. Aspirin and omeprazole for secondary prevention of cardiovascular disease in patients at risk for aspirin-associated gastric ulcers.

    Science.gov (United States)

    García-Rayado, Guillermo; Sostres, Carlos; Lanas, Angel

    2017-08-01

    Cardiovascular disease is the most important cause of morbidity and mortality in the world and low-dose aspirin is considered the cornerstone of the cardiovascular disease prevention. However, low-dose aspirin use is associated with gastrointestinal adverse effects in the whole gastrointestinal tract. In this setting, co-therapy with a proton pump inhibitor is the most accepted strategy to reduce aspirin related upper gastrointestinal damage. In addition, some adverse effects have been described with proton pump inhibitors long term use. Areas covered: Low-dose aspirin related beneficial and adverse effects in cardiovascular system and gastrointestinal tract are reviewed. In addition, this manuscript summarizes current data on upper gastrointestinal damage prevention and adverse events with proton pump inhibition. Finally, we discuss the benefit/risk ratio of proton pump inhibitor use in patients at risk of gastrointestinal damage taking low-dose aspirin. Expert commentary: Nowadays, with the current available evidence, the combination of low-dose aspirin with proton pump inhibitor is the most effective therapy for cardiovascular prevention in patients at high gastrointestinal risk. However, further studies are needed to discover new effective strategies with less related adverse events.

  15. Differential effects of omeprazole and lansoprazole enantiomers on aryl hydrocarbon receptor in human hepatocytes and cell lines

    National Research Council Canada - National Science Library

    Novotna, Aneta; Srovnalova, Alzbeta; Svecarova, Michaela; Korhonova, Martina; Bartonkova, Iveta; Dvorak, Zdenek

    2014-01-01

    .... equimolar mixture of S- and R-enantiomers. The enantiopure drugs esomeprazole and dexlansoprazole have been developed and introduced to clinical practice due to their improved clinical and therapeutic properties...

  16. Omeprazol ¿Un nuevo tratamiento de la poliposis nasal? Del empirismo al saber científico

    OpenAIRE

    Serra Carreras, Jordi

    2001-01-01

    Descripció del recurs: 28 febrer 2002 Títol obtingut de la portada digitalitzada El tratamiento de la poliposis nasal en la actualidad no está resuelto. El tratamiento quirúrgico o el tratamiento médico (corticoterapia) están condenados a elevados índices de recurrencias, especialmente entre los enfermos con poliposis que asocian además intolerancia al Ácido Acetilsalicílico y asma. El desconocimiento de la etiología de la poliposis y de los mecanismos fisiopatológicos más íntimos, no p...

  17. Drug: D10246 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10246 Mixture, Drug Omeprazole - clarithromycin - amoxicillin mixt; Omeclamox-pak ...cter pylori A02BD05 Omeprazole, amoxicillin and clarithromycin D10246 Omeprazole - clarithromycin - amoxicillin mixt PubChem: 163312277 ...

  18. Comparison of reversed-phase enantioselective HPLC methods for determining the enantiomeric purity of (S-omeprazole in the presence of its related substances

    Directory of Open Access Journals (Sweden)

    Bruno Gallinella

    2016-04-01

    Full Text Available A simple analytical high-performance liquid chromatography (HPLC method was applied for the enantiomeric excess determination of esomeprazole ((S-OME, the enantiopure active ingredient contained in drug products, in the presence of its potential organic impurities A-E. The enantioselective separation was accomplished on the immobilized-type Chiralpak ID-3 chiral stationary phase (CSP under reversed-phase conditions. The results were evaluated and compared with those obtained by the official enantioselective method of European Pharmacopoeia used as the reference for checking the enantiomeric excess of (S-OME. It has been established that the use of the Chiralpak ID-3 CSP allows the determination of the enantiomeric purity of (S-OME without any interference coming from its chiral and achiral related substances. The analytical procedure of the drug regulatory agencies based on the AGP CSP suffered instead from poor specificity due to overlap of the peaks pertinent to the achiral impurity A and the chiral impurity (R-OME (impurity F.

  19. Comparison of reversed-phase enantioselective HPLC methods for determining the enantiomeric purity of (S)-omeprazole in the presence of its related substances$

    Institute of Scientific and Technical Information of China (English)

    Bruno Gallinella; Rosella Ferretti; Leo Zanitti; Isabella Sestili; Antonina Mosca; Roberto Cirilli n

    2016-01-01

    A simple analytical high-performance liquid chromatography (HPLC) method was applied for the en-antiomeric excess determination of esomeprazole ((S)-OME), the enantiopure active ingredient con-tained in drug products, in the presence of its potential organic impurities A-E. The enantioselective separation was accomplished on the immobilized-type Chiralpak ID-3 chiral stationary phase (CSP) under reversed-phase conditions. The results were evaluated and compared with those obtained by the official enantioselective method of European Pharmacopoeia used as the reference for checking the enantiomeric excess of (S)-OME. It has been established that the use of the Chiralpak ID-3 CSP allows the determination of the enantiomeric purity of (S)-OME without any interference coming from its chiral and achiral related substances. The analytical procedure of the drug regulatory agencies based on the AGP CSP suffered instead from poor specificity due to overlap of the peaks pertinent to the achiral impurity A and the chiral impurity (R)-OME (impurity F).

  20. Symptomatic response to blocked and unblocked pentagastrin stimulation in functional dyspepsia - Comparison of responders and non-responders to omeprazole identified in a single-subject trial model

    DEFF Research Database (Denmark)

    Madsen, L.G.; Bytzer, P.

    2008-01-01

    -over design. Epigastric pain was assessed every 15 for 90 min after stimulation using a 5-graded Likert scale and a VAS scale. A positive acid provocation test was defined as an increase of the Likert score of epigastric pain by at least one grade after pentagastrin stimulation during placebo treatment...

  1. Cure of Helicobacter pylori infection in patients with reflux oesophagitis treated with long term omeprazole reverses gastritis without exacerbation of reflux disease: results of a randomised controlled trial

    NARCIS (Netherlands)

    E.J. Kuipers (Ernst); N. Havu; A. Walan; M. Lamm; G.F. Nelis; E.C. Klinkenberg-Knol; P. Snel; D. Goldfain; J.J. Kolkman (Jeroen); H.P. Festen; J. Dent; P. Zeitoun

    2004-01-01

    textabstractBACKGROUND: Helicobacter pylori gastritis may progress to glandular atrophy and intestinal metaplasia, conditions that predispose to gastric cancer. Profound suppression of gastric acid is associated with increased severity of H pylori gastritis. This prospective random

  2. Cure of Helicobacter pylori infection in patients with reflux oesophagitis treated with long term omeprazole reverses gastritis without exacerbation of reflux disease: results of a randomised controlled trial

    NARCIS (Netherlands)

    E.J. Kuipers (Ernst); N. Havu; A. Walan; M. Lamm; G.F. Nelis; E.C. Klinkenberg-Knol; P. Snel; D. Goldfain; J.J. Kolkman (Jeroen); H.P. Festen; J. Dent; P. Zeitoun

    2004-01-01

    textabstractBACKGROUND: Helicobacter pylori gastritis may progress to glandular atrophy and intestinal metaplasia, conditions that predispose to gastric cancer. Profound suppression of gastric acid is associated with increased severity of H pylori gastritis. This prospective

  3. The Effect of Roux-en-Y Gastric Bypass Surgery in Morbidly Obese Patients on Pharmacokinetics of (Acetyl)Salicylic Acid and Omeprazole: the ERY-PAO Study

    NARCIS (Netherlands)

    Mitrov-Winkelmolen, Lieke; van Buul-Gast, Marie Christine W; Swank, Dingeman J.; Overdiek, Hans W P M; van Schaik, Ron H N; Touw, Daan J.

    2016-01-01

    Background Data on the absorption of orally administered drugs following Roux-en-Y gastric bypass (RYGB) surgery in obese patients are limited and inconclusive. As it is difficult to predict changes in absorption, studies on frequently used drugs in this population are necessary. Acetylsalicylic aci

  4. The Effect of Roux-en-Y Gastric Bypass Surgery in Morbidly Obese Patients on Pharmacokinetics of (Acetyl)Salicylic Acid and Omeprazole : the ERY-PAO Study

    NARCIS (Netherlands)

    Mitrov-Winkelmolen, Lieke; van Buul-Gast, Marie-Christine W.; Swank, Dingeman J.; Overdiek, Hans W. P. M.; van Schaik, Ron H. N.; Touw, Daan J.

    2016-01-01

    Data on the absorption of orally administered drugs following Roux-en-Y gastric bypass (RYGB) surgery in obese patients are limited and inconclusive. As it is difficult to predict changes in absorption, studies on frequently used drugs in this population are necessary. Acetylsalicylic acid (ASA) and

  5. An Analysis of the Effectiveness of the Retail Pharmacy Utilization Intervention at General Leonard Wood Army Community Hospital

    Science.gov (United States)

    2009-04-23

    limited to those beneficiaries who filled prescriptions for esomeprazole, clopidogrel, zolpidem, omeprazole , atorvastatin, monteluckast, fexofenadine...formulary. Nexium (esomeprazole) Plavix (clopidogrel) Ambien (zolpidem) Prilosec ( omeprazole ) Lipitor (atorvastatin) Singulair (montelukast...Prilosec ( omeprazole ) • Topimax (topiramate) • Detrol (tolterodine) Lipitor (atorvastatin) We would like to remind you that these medications and many

  6. Drug: D01207 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D01207 Drug Omeprazole sodium (USAN); Losec sodium (TN) C17H18N3O3S. Na 367.0967 367.3979 D0120...itors A02BC01 Omeprazole D01207 Omeprazole sodium (USAN) USP drug classification ...[BR:br08302] Gastrointestinal Agents Proton Pump Inhibitors Omeprazole D01207 Omeprazole sodium (USAN) Targe...[KO:K01542 K01543] Omeprazol [ATC:A02BC01] D01207 Omeprazole sodium (USAN) CAS: 95510-70-6 PubChem: 7848270 ...DrugBank: DB00338 LigandBox: D01207 ATOM 25 1 C8x C 22.6800 -19.3200 2 C8y C 22.6

  7. 奥美拉唑在大鼠肝微粒体中的酶促反应动力学研究%Enzyme Kinetics of Omeprazole Metabolism in Rat Liver Microsomes

    Institute of Scientific and Technical Information of China (English)

    王国利; 刘金华; 薛书霞; 李景武

    2006-01-01

    目的:研究奥美拉唑在大鼠肝微粒体中的酶促反应动力学.方法:采用高效液相色谱法测定奥美拉唑在体外代谢系统中的产物5'-羟基奥美拉唑,并用Eadie-Hofstee作图法分析数据,计算酶促反应动力学参数最大反应速率(Vmax)、米氏常数(Km).结果:在体外代谢系统中,奥美拉唑生成5'-羟基奥美拉唑的Vmax为2 010nmol/(min·mg protein)、Km为50.3μmol/L.结论:本分析方法符合方法学验证的要求,体外代谢常数准确,可满足奥美拉唑体外代谢的研究.

  8. El Mecanismo de la Oxidación de Omeprazol Sobre el Electrodo de Carbono Vitroso, Modificado por Polializarina, y Su Descripción Matemática

    Directory of Open Access Journals (Sweden)

    Volodymyr Valentynovych Tkach

    2015-04-01

    Full Text Available For the electroanalytical work of glassy carbon electrode, modified by polyalizarine, a mechanism, confirmed by experimental observations, has been proposed. This mechanism is also mathematically studied by means of linear stability theory and bifurcation analysis. The stable steady-state conditions, like also the causes for the oscillatory and monotonic instabilities, have been obtained on the base of the analysis of the model.DOI: http://dx.doi.org/10.17807/orbital.v7i1.599

  9. 奥美拉唑肠溶胶囊在健康人体药动学及生物等效性研究%OMEPRAZOLE ENTERIC-COATED CAPSULES IN HEAL THY VOLUNTEERS PHARMACOKINETICS AND BIOEQUIVALENCE STUDIES

    Institute of Scientific and Technical Information of China (English)

    周鲲; 王国志; 伊红琳

    2010-01-01

    目的 研究两个不同厂家生产的奥美拉唑肠溶胶囊在健康人体的生物等效性.方法 20 名健康志愿者采用双周期交叉试验.高效液相色谱法测定血清中奥美拉唑浓度.血药浓度-时间数据采用DAS2.0统计软件处理,计算主要药代动力学参数,并进行两种制剂的生物等效性评价.结果 受试制剂及参比制剂的主要药代动力学参数t1/2、cmax、Tmzx和AUCO-12 h分别为(1.79±0.86)h和(1.49±0.50)h、(0.51±0.25)trg·mL-1和(0.49±0.19)μg·mL-1、(2.05±0.64)h和(2.04±0.63)h、(1.64±1.41)μg·h-1·mL-1和(1.57±0.99)μg·h-1·mL-1.受试制剂的相对生物利用度为(101.48±33.82)%.结论 两种奥美拉唑肠溶胶囊具有生物等效性.

  10. Pharmacy Use and Costs in Employer-Provided Health Plans. Insights for TRICARE Benefit Design from the Private Sector

    Science.gov (United States)

    2005-01-01

    Effect of Moving Prilosec ( Omeprazole ) from Second to Third T ier ................................................................ 3 7 4.3. Effect of...not shown) were virtually the same. The inconsistent relationship between tier changes and market share ob- served for omeprazole , simvastatin, and...1 2 3 4 5 6 7 8 9 10 11 1213 1415 1617 1819 2021 2223 24 Month RAND MG15444.2 Figure 4.2--Effect of Moving Prilosec ( Omeprazole ) from Second to Third

  11. [Changes in the ultrastructure of the stomach mucous membrane parietal cells caused by inhibitors of hydrochloric acid secretion].

    Science.gov (United States)

    Dondukova, G V; Morozov, I A

    2002-01-01

    The study of the action of phamotidine and omeprazol on the stomach parietal cells in patients with duodenal ulcer has shown that phamotidin results in changes of secretory membrane of the parietal cells increasing its secretory potential while omeprazol reduces energetic metabolism of the lining cell by the impact on its mitochondrial apparatus. Both in children and adults with duodenal ulcer more developed mitochondrial cell activity was found after omeprazol treatment.

  12. Safety of the long-term use of proton pump inhibitors

    Institute of Scientific and Technical Information of China (English)

    Alan; BR; Thomson; Michel; D; Sauve; Narmin; Kassam; Holly; Kamitakahara

    2010-01-01

    The proton pump inhibitors (PPIs) as a class are remarkably safe and effective for persons with peptic ulcer disorders. Serious adverse events are extremely rare for PPIs, with case reports of interstitial nephritis with omeprazole, hepatitis with omeprazole and lansoprazole, and disputed visual disturbances with pantoprazole and omeprazole. PPI use is associated with the development of fundic gland polyps (FGP); stopping PPIs is associated with regression of FGP. In the absence of Helicobacter pylori infec...

  13. Review article: immediate-release proton-pump inhibitor therapy--potential advantages.

    Science.gov (United States)

    Howden, C W

    2005-12-01

    The absorption of most oral proton-pump inhibitors is delayed by the enteric coating required to protect the acid-labile proton-pump inhibitor from degradation in the stomach and, as a result, antisecretory effect is also delayed. This article provides an overview of the pharmacokinetics and pharmacodynamics of a new immediate-release omeprazole [(IR-OME) Zegerid power for oral suspension; Santarus Inc., San Diego, CA, USA] and its potential advantages over delayed-release proton-pump inhibitors. Immediate-release omeprazole has a higher mean peak plasma omeprazole concentration (C(max)) and a significantly shorter mean time to reach C(max) (t(max)) than delayed-release omeprazole. Immediate-release omeprazole 40 mg has a prolonged antisecretory effect with median intragastric pH above 4.0 for 18.6 h/day at steady-state, after 7 days of once daily dosing. The sodium bicarbonate in immediate-release omeprazole protects the uncoated omeprazole from degradation by gastric acid. The accelerated antisecretory action of immediate-release omeprazole compared with delayed-release omeprazole may be due to the activation of proton pumps by the rapid neutralization of intragastric acid by the sodium bicarbonate. The faster onset of action seen with immediate-release omeprazole is not achieved by using an antacid with a delayed-release proton-pump inhibitor, because administering antacids with conventional delayed-release proton-pump inhibitors does not significantly enhance absorption of the proton-pump inhibitor. In conclusion, immediate-release omeprazole is associated with rapid absorption of omeprazole and rapid onset of antisecretory effect, without compromising the duration of acid suppression.

  14. Short report

    DEFF Research Database (Denmark)

    Rasmussen, L; Oster-Jørgensen, E; Qvist, N;

    1991-01-01

    The aim of the study was to investigate a possible effect of omeprazole on the characteristics of the gastric emptying of liquid and solid in healthy subjects. The study was performed as a double-blind crossover study and the gastric emptying studies were performed after 10 days of treatment...... with placebo or omeprazole 40 mg o.m. Omeprazole was without effect on the characteristics of liquid emptying or the lag phase of solid. It does, however, decrease the emptying rate of solid as the omeprazole group had a median half-time duration of the linear emptying period which had twice the duration...

  15. 77 FR 3777 - Draft and Revised Draft Guidances for Industry Describing Product-Specific Bioequivalence...

    Science.gov (United States)

    2012-01-25

    ... RLDs) Mifepristone Milnacipran HCl Minocycline HCl Minoxidil (multiple RLDs) Mirtazapine Misoprostol... RLDs) Minoxidil Morphine N Nebivolol Niacin Nilutamide Nitroglycerin O Omeprazole Orlistat (multiple...

  16. Delavirdine

    Science.gov (United States)

    ... and propafenone (Rythmol); medications for indigestion, heartburn, or ulcers such as cimetidine (Tagamet), famotidine (Pepcid), lansoprazole (Prevacid), nizatidine (Axid), omeprazole (Prilosec), and ranitidine (Zantac); ...

  17. Gefitinib

    Science.gov (United States)

    ... proton pump inhibitor medication for indigestion, heartburn, or ulcers such as esomeprazole (Nexium), lansoprazole (Prevacid), omeprazole (Prilosec), pantoprazole (Protonix), or rabeprazole (AcipHex), ...

  18. Cobicistat

    Science.gov (United States)

    ... also taking a medication for indigestion, heartburn, or ulcers (proton pump inhibitors) such as esomeprazole (Nexium, in Vimovo), lansoprazole (Prevacid), omeprazole (Prilosec, in Zegerid), pantoprazole (Protonix), or ...

  19. Drug-induced diarrhea

    Science.gov (United States)

    ... cancer Drugs used to treat heartburn and stomach ulcers, such as omeprazole (Prilosec), esomeprazole (Nexium), lansoprazole (Prevacid), rabeprazole (AcipHex), pantoprazole (Protonix), cimetidine (Tagamet), ranitidine ( ...

  20. Ceritinib

    Science.gov (United States)

    ... your blood pressure; medications for indigestion, heartburn, or ulcers such as cimetidine (Tagamet, in Duexis), esomeprazole (Nexium), famotidine (Pepcid), lansoprazole (Prevacid), nizatidine (Axid), omeprazole (Prilosec), pantoprazole (Protonix), rabeprazole ( ...

  1. ГАСТРОЭЗОФАГЕАЛЬНАЯ РЕФЛЮКСНАЯ БОЛЕЗНЬ: ОСОБЕННОСТИ БАЗИСНОЙ ТЕРАПИИ

    Directory of Open Access Journals (Sweden)

    Н. Л. Аванян

    2012-01-01

    Full Text Available The authors present their own clinical experience in treating elderly patients with gastroesophageal reflux disease using different therapy regimens: monotherapy with proton pump inhibitors (Omeprazole Sandoz and H2-histamine blockers using a combination of a prokinetic in different modes of observation. It is shown that use of Omeprazole Sandoz is preferable in terms of efficacy, safety and cost of treatment.

  2. [THE EFFECTIVENESS OF ERADICATION IN PATIENTS WITH PEPTIC ULCER DISEASE ASSOCIATED WITH HELICOBACTER PYLORI, DEPENDING ON THE GENOTYPE OF THE DRUGMETABOLISM OF PROTON PUMP INHIBITORS].

    Science.gov (United States)

    Elokhina, E V; Kostenko, M B; Livzan, M A; Scalskiy, S V

    2015-01-01

    One of the most likely causes of the lack of effectiveness of eradication therapy of peptic ulcer associated with Helicobacter pylori, is a feature of omeprazole metabolism by cytochrome CYP2C19. The paper work presents evidence that the rate of reduction of the clinical picture and the likelihood of scarring ulcers and eradication rates higher in patients slow metabolizers of omeprazole.

  3. Reappraisal of bicarbonate secretion by the human oesophagus

    DEFF Research Database (Denmark)

    Mertz-Nielsen, A; Hillingsø, J; Bukhave, Klaus

    1997-01-01

    BACKGROUND AND AIMS: Administration of omeprazole to healthy volunteers was recently reported to increase proximal duodenal mucosalbicarbonate secretion. As human oesophagus also secretes bicarbonate, the hypothesis was tested that omeprazole may stimulate oesophagealbicarbonate secretion and thus....../day omeprazole for three days and 80 mg intravenous omeprazole before perfusionor 600 mg/day ranitidine for three days and 50 mg/h intravenously during the perfusion. Saliva and samples of aspirate from the perfusedoesophagus and stomach were collected and bicarbonate concentrations were measured. RESULTS......: The median rates (95% confidence intervals)of intrinsic oesophageal bicarbonate secretion, corrected for contaminating salivary and gastric bicarbonate, were 89 (33-150) and 121 (63-203)mumol/h/10 cm (p > 0.5) in omeprazole and ranitidine treated subjects respectively. Salivary and gastric bicarbonate...

  4. Simultaneous determination of midazolam, dextromethorphan and omeprazole in rat plasma by LC-MS%LC-MS法同时测定大鼠血浆中咪达唑仑、右美沙芬及奥美拉唑的浓度

    Institute of Scientific and Technical Information of China (English)

    许潇; 谢林; 梁艳; 陈卫东; 刘晓东; 王广基

    2006-01-01

    目的:LC-MS法同时测定大鼠血浆中咪达唑仑、右美沙芬及奥美拉唑浓度,并用于药代动力学高通量筛选中"鸡尾酒法"的研究中.方法:色谱柱为Shim-pack ODS(250 mm×2.0 mm ID,5.0μm);流动相为0.01%醋酸铵-甲醇(30:70).检测仪为岛津LC-MS-2010四极杆质谱检测器,电喷雾离子化(ESI),内标为地西泮.检测离子:咪达唑仑为[M+H]+m/z:326.0,右美沙芬为[M+H]+m/z:272.1,奥美拉唑为[M+H]+m/z:346.0,地西泮为[M+H]+m/z:284.9.血浆样品处理方法为碱化后用乙醚提取.结果:咪达唑仑、右美沙芬和奥美拉唑的线性范围为2~2 000 ng/mL,方法的回收率均大于85%,日内和日间的精密度均小于10%,且没有基质效应.结论:该方法符合血浆样品的测定要求,可用于药代动力学高通量筛选中的"鸡尾酒法"研究.

  5. A STUDY ON OMEPRAZOLE COMBIND AMOXILLIN IN THE TREATMENT OF DUODENAL ULCER WITH HELICOBACTER PYLORI POSITIVE IN CHILDREN%奥美拉唑与阿莫西林联合治疗儿童幽门螺杆菌阳性十二指肠溃疡效果观察

    Institute of Scientific and Technical Information of China (English)

    曹敬梅; 高金亭; 李春枝

    2001-01-01

    ①目的观察奥美拉唑合用阿莫西林治疗儿童幽门螺杆菌(Hp)阳性十二指肠溃疡的效果.②方法84例Hp阳性十二指肠溃疡病儿随机分为两组,分别给予奥美拉唑(Ome)加阿莫西林(Amx)和单用Ome治疗28d,定期复查胃镜和Hp感染情况.③结果联合组溃疡近期愈合率与Ome组差异无显著意义(x2=0.070,P>0.05),但Hp清除率联合组显著高于Ome组(x2=49.909,P<0.001).联合组0.5,1.0年时溃疡累积复发率和Hp感染复发率显著低于Ome组(x2=6.215~35.484,P<0.05,0.01).④结论奥美拉唑合用阿莫西林可提高Hp阳性十二指肠溃疡病儿Hp清除率,降低溃疡的近期复发率.

  6. Curative Effect of Therapeutic Alliance of Omeprazole and Hemocoagulase Combined with Norepinephrine for Hemorrhagic Disease of Newborn%奥美拉唑血凝酶去甲肾上腺素联合治疗新生儿出血症的疗效分析

    Institute of Scientific and Technical Information of China (English)

    赖银诊

    2014-01-01

    目的:探讨奥美拉唑、血凝酶、去甲肾上腺素联合治疗新生儿出血症的疗效.方法:对照组应用常规禁食、输血、留置胃管等治疗方法,治疗组在对照组的基础上加用奥美拉唑、血凝酶和去甲肾上腺素进行联合治疗.结果:治疗组总有效率明显比对照组高,两组有显著性差异(P<0.05),具有统计学意义.结论:奥美拉唑、血凝酶、去甲肾上腺素联合治疗新生儿出血症过程中,联合用药具有协同作用,值得临床推广应用.

  7. Clinical efficacy of omeprazole enteric-coated tablets plus sodium bicarbonate spray on the treatment of iaryngopharygeal reflux%奥美拉唑加碳酸氢钠喷雾治疗反流性咽喉炎的疗效观察

    Institute of Scientific and Technical Information of China (English)

    蒋星; 仇翼; 薛建荣

    2009-01-01

    目的:探讨奥美拉唑加碳酸氢钠喷雾治疗反流性咽喉炎的疗效.方法:对50例反流性咽喉炎患者应用奥美拉唑加碳酸氢钠喷雾治疗.结果:50例患者治疗后,有46例咽喉部症状明显改善,LPR反流症状指数降低>4;镜下咽喉部病变好转,LPR体征量表降低>2.有效率92%(46例).结论:奥美拉唑加碳酸氢钠喷雾可缓解或改善反流性咽喉炎的症状和病理.

  8. Determination of Omepraxole in Omeprazole Sodium bicarbonate Magnesium hydrate Chewable Tablets by HPLC%HPLC法测定复方奥美拉唑碳酸氢钠氢氧化镁咀嚼片中奥美拉唑的含量

    Institute of Scientific and Technical Information of China (English)

    黄懿

    2012-01-01

    目的:建立复方奥美拉唑碳酸氢钠氢氧化镁咀嚼片含量测定方法.方法:采用HPLC法测定复方奥美拉唑碳酸氢钠氢氧化镁咀嚼片中奥美拉唑的含量.结果:奥美拉唑在4.6 ~ 46μg·mL-1浓度范围内与峰面积呈良好的线性关系;平均回收率为99.93%,RSD为0.67%(n=9).结论:本法专属性强,灵敏度高,重复性好,可用于复方奥美拉唑碳酸氢纳氢氧化镁咀嚼片的质量控制.

  9. 奥美拉唑碳酸氢钠干混悬剂和肠溶制剂在健康人体的药动学对比研究%Pharmacokinetic comparison of omeprazole sodium bicarbonate for suspension and enteric-coated preparations in healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    梅亚君; 勾忠平; 秦永平; 冯萍; 李燕; 南峰; 向瑾; 王颖; 苗佳

    2016-01-01

    目的:研究奥美拉唑碳酸氢钠干混悬剂(试验制剂)和肠溶制剂(参比制剂)在健康人体内的药动学差异.方法:采用单中心、开放、随机、自身交叉对照试验,12例志愿受试者(男女各半)于不同试验周期分别餐后单次、空腹单次和多次口服20 mg试验制剂和参比制剂.用HPLC-MS/MS法测定血浆中奥美拉唑浓度,用PhoenixTM WinNonlin 6.1药动学软件计算主要药动学参数.结果:试验制剂空腹单、多次给药的AUC与参比制剂一致,Tmax较参比制剂快,空腹单次给药试验制剂Cmax较参比制剂高,多次给药差异不明显;t1/2和参比制剂比较无统计学差异,高脂高热餐后给药,试验制剂的AUC小于参比制剂.结论:试验制剂与参比制剂相比:达峰时间较快,空腹单次和多次给药AUC无明显差异,饮食会抑制试验制剂的吸收;多次给药2种制剂的AUC均明显增大;建议奥美拉唑碳酸氢钠干混悬剂空腹服用.

  10. A Domain Independent Framework for Extracting Linked Semantic Data from Tables

    Science.gov (United States)

    2012-01-01

    Gasbarrini, G., Roda, E., Bazzoli, F.: Comparison of 1 and 2 weeks of omeprazole , amoxicillin and clarithromycin treat- ment for helicobacter pylori eradication: the hyper study. Gut 56(4), 475 (2007)

  11. Download this PDF file

    African Journals Online (AJOL)

    Dr Olaleye

    omeprazole and magnesium showed scanty inflammation with no signs of edema and hemorrhage. ... magnesium supplementation can prevent cardiovascular disease and has been ... in their drinking water for a period of 14 days prior to.

  12. Efavirenz

    Science.gov (United States)

    ... HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex ... and tolbutamide (Orinase); proton pump inhibitors such as lansoprazole (Prevacid), omeprazole (Prilosec), and pantoprazole (Protonix); quinidine (Quinidex); ...

  13. Treatment Option Overview (Pancreatic Neuroendocrine Tumors / Islet Cell Tumors)

    Science.gov (United States)

    ... NETs may include treatment for the following: Stomach ulcers may be treated with drug therapy such as: Proton pump inhibitor drugs such as omeprazole , lansoprazole , or pantoprazole. Histamine blocking drugs such as cimetidine , ...

  14. Voriconazole

    Science.gov (United States)

    ... pump inhibitors such as esomeprazole (Nexium, in Vimovo), lansoprazole (Prevacid), omeprazole (Prilosec, in Prevpac), pantoprazole (Protonix), and ... have ever been treated with chemotherapy medications for cancer, and if you have or have ever had ...

  15. Emtricitabine, Rilpivirine, and Tenofovir

    Science.gov (United States)

    ... HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex ... Tegretol, others), dexamethasone, dexlansoprazole (Dexilant), esomeprazole (Nexium, Vimovo), lansoprazole (Prevacid, in Prevpac), omeprazole (Prilosec, in Zegerid), oxcarbazepine ( ...

  16. General Information about Pancreatic Neuroendocrine Tumors (Islet Cell Tumors)

    Science.gov (United States)

    ... NETs may include treatment for the following: Stomach ulcers may be treated with drug therapy such as: Proton pump inhibitor drugs such as omeprazole , lansoprazole , or pantoprazole. Histamine blocking drugs such as cimetidine , ...

  17. Atazanavir

    Science.gov (United States)

    ... are taking a medication for indigestion, heartburn, or ulcers such as cimetidine, esomeprazole (Nexium, in Vimovo), famotidine (Pepcid, in Duexis), lansoprazole (Prevacid, in Prevpac), nizatidine (Axid), omeprazole (Prilosec, in ...

  18. Zollinger-Ellison syndrome

    Science.gov (United States)

    ... test Treatment Drugs called proton pump inhibitors (omeprazole, lansoprazole, and others) used for treating this problem. These drugs reduce acid production by the stomach. This helps the ulcers in the stomach and small intestine heal. These ...

  19. Rilpivirine

    Science.gov (United States)

    ... HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex ... Phenytek); proton pump inhibitors including esomeprazole (Nexium, Vimovo), lansoprazole (Prevacid), omeprazole (Prilosec), pantoprazole (Protonix), or rabeprazole (Aciphex); ...

  20. Treatment Options for Pancreatic Neuroendocrine Tumors

    Science.gov (United States)

    ... NETs may include treatment for the following: Stomach ulcers may be treated with drug therapy such as: Proton pump inhibitor drugs such as omeprazole , lansoprazole , or pantoprazole. Histamine blocking drugs such as cimetidine , ...

  1. Comparison of four proton pump inhibitors for the short-term treatment of esophagitis in elderly patients

    Institute of Scientific and Technical Information of China (English)

    Alberto Pilotto; Francesco Di Mario; Marilisa Franceschi; Gioacchino Leandro; Carlo Scarcelli; Luigi Piero D'Ambrosio; Francesco Paris; Vito Annese; Davide Seripa; Angelo Andriulli

    2007-01-01

    AIM: To compare efficacy and tolerability of four proton pump inhibitors (PPIs) commonly used in the short-term therapy of esophagitis in elderly patients.METHODS: A total of 320 patients over 65 years with endoscopically diagnosed esophagitis were randomly assigned to one of the following treatments for 8 wk:(1) omeprazole 20 mg/d; (2) lansoprazole 30 mg/d;(3) pantoprazole 40 mg/d, or (4) rabeprazole 20 mg/d.Major symptoms, compliance, and adverse events were recorded. After 8 wk, endoscopy and clinical evaluation were repeated.RESULTS: Per protocol and intention to treat healing rates of esophagitis were: omeprazole = 81.0% and 75.0%, lansoprazole = 90.7% (P = 0.143 vs omeprazole) and 85.0%, pantoprazole=93.5% (P = 0.04vs omeprazole) and 90.0% (P = 0.02 vs omeprazole),rabeprazole = 94.6% (P = 0.02 vs omeprazole) and 88.8% (P = 0.04 vs omeprazole). Dividing patients according to the grades of esophagitis, omeprazole was significantly less effective than the three other PPIs in healing grade 1 esophagitis (healing rates:81.8% vs 100%, 100% and 100%, respectively, P =0.012). Pantoprazole and rabeprazole (100%) were more effective vs omeprazole (89.6%, P = 0.0001)and lansoprazole (82.4%, P = 0.0001) in decreasing heartburn. Pantoprazole and rabeprazole (92.2% and 90.1%, respectively) were also more effective vs lansoprazole (75.0%, P < 0.05) in decreasing acid regurgitation. Finally, pantoprazole and rabeprazole (95.2% and 100%) were also more effective vs lansoprazole (82.6%, P < 0.05) in decreasing epigastric pain.CONCLUSION: In elderly patients, pantoprazole and rabeprazole were significantly more effective than omeprazole in healing esophagitis and than omeprazole or lansoprazole in improving symptoms.H pylori infection did not influence the healing rates of esophagitis after a short-term treatment with PPI.

  2. Reappraisal of bicarbonate secretion by the human oesophagus.

    OpenAIRE

    Mertz-Nielsen, A; Hillingsø, J; Bukhave, K; Rask-Madsen, J

    1997-01-01

    BACKGROUND AND AIMS: Administration of omeprazole to healthy volunteers was recently reported to increase proximal duodenal mucosal bicarbonate secretion. As human oesophagus also secretes bicarbonate, the hypothesis was tested that omeprazole may stimulate oesophageal bicarbonate secretion and thus contribute to the therapeutic efficacy of the drug in gastro-oesophageal reflux disease. SUBJECTS AND METHODS: In nine healthy volunteers, oesophageal "steady state" perfusion of a 10 cm open segm...

  3. Sesgos de confusión por indicación y gravedad en estudios observacionales Confounding bias due to indication and severity in observational studies

    Directory of Open Access Journals (Sweden)

    Javier Nuevo

    2011-04-01

    Full Text Available Los estudios observacionales están sujetos a sesgos que pueden conducir a una interpretación errónea de los resultados. El presente estudio tuvo como objetivo determinar la influencia del tratamiento con omeprazol sobre la duración de la baja laboral en pacientes con esguince de tobillo que tomaban antiinflamatorios no esteroideos. Se utilizaron los registros de la base de datos de la mutua Ibermutuamur. En contra de lo esperado, se observó que los pacientes que recibieron omeprazol presentaron una baja más prolongada que los que no recibieron omeprazol. Es probable que estos hallazgos se deban a la influencia de un sesgo de confusión por gravedad, pues los pacientes que recibieron omeprazol presentaban un esguince más grave, aunque no se puede descartar un sesgo de confusión por indicación. Para evitar la influencia de estos errores sistemáticos se deben controlar los sesgos a lo largo de todo el estudio, desde el diseño hasta el análisis de los datos.Observational studies are subject to biases that may lead to misinterpretation of the results. This study aimed to determine the influence of omeprazole treatment on the duration of sick leave in patients with ankle sprains treated with non-steroidal anti-inflammatory drugs. We used the Ibermutuamur database. Contrary to our expectations, sick leave was longer in patients who received omeprazole than in those who did not. These findings were probably due to the influence of a bias due to confounding by severity, given that patients who received omeprazole had a worse kind of ankle sprain; however, a bias due to confounding by indication cannot be excluded. To avoid the influence of these systematic errors, biases should be monitored from the design stage to the data analysis stage.

  4. A randomized comparison of triple therapy Helicobacter pylori eradication regimens in children with peptic ulcers.

    Science.gov (United States)

    Shcherbakov, P L; Filin, V A; Volkov, I A; Tatarinov, P A; Belousov, Y B

    2001-01-01

    An open, randomized trial was performed to compare the efficacy of three Helicobacter pylori eradication regimens in children with peptic ulcer disease. A total of 106 children (5 - 15 years) were treated for 1 week with metronidazole, 30 - 40 mg/kg per day depending on age, amoxycillin, 750 mg/day, and one of three anti-secretory agents: proprietary omeprazole, 20 - 40 mg/day depending on age; generic omeprazole, 20 - 40 mg/day; or ranitidine, 150 mg twice daily. The H. pylori eradication rate was significantly higher in patients receiving proprietary omeprazole (88.9%) than in those receiving generic omeprazole (80.0%) or ranitidine (74.3%), and this was associated with a trend towards faster ulcer healing. It is concluded that triple therapy consisting of an anti-secretory agent and two antimicrobials produces effective eradication of H. pylori and ulcer healing in children with peptic ulcer disease, and that proprietary omeprazole is more effective than both ranitidine and the generic formulation used in this study.

  5. [Do proton pump inhibitors after endoscopic control of acute ulcer hemorrhage have an advantage over H2 receptor antagonists?].

    Science.gov (United States)

    Prassler, R; Hendrich, H; Barnert, J; Richter, G; Fleischmann, R; Wienbeck, M

    1995-08-01

    During a two year period (1992-1993) we investigated whether or not, after endoscopic therapy of bleeding ulcers, the suppression of gastric acid secretion with an administration of a proton pump blocker (Omeprazol) is more effective than the administration of H2-receptor antagonist (Ranitidin) with respect to prevention of recurrent bleeding episodes, frequency of surgical intervention and mortality. 106 patients (64 men, 42 women) were treated with the proton pump blocker and 126 patients (82 men, 44 women) received the H2-receptor antagonist. Patients were treated either with an initial dose of 80 mg Omeprazol followed by 3 x 40 mg Omeprazol i.v. or with a daily dose of 3 mg/kg body weight Ranitidin i.v. No significant differences could be detected between the two treatment regimes with respect to the parameters mentioned above. Rebleeding which could be controlled by endoscopic hemostasis occurred in 19.8% vs. 17.5% (Omeprazol/Ranitidin) of patients. Surgical intervention because of rebleeding was necessary on 8.5% vs. 8.7% of the patients. Mortality due to hemorrhage was 5.7% vs. 4.0%. From these results we conclude that, following endoscopic hemostasis of bleeding ulcers, Omeprazol has no advantage over Ranitidin using our dosage regimes.

  6. Gastrin release: Antrum microdialysis reveals a complex neural control

    DEFF Research Database (Denmark)

    Ericsson, P; Håkanson, R; Rehfeld, Jens F.;

    2010-01-01

    in serum regardless of the prandial state. The rats were conscious during microdialysis except when subjected to electrical vagal stimulation. Acid blockade (omeprazole treatment of freely fed rats for 4 days), or bilateral sectioning of the abdominal vagal trunks (fasted, 3 days post-op.), raised...... the gastrin concentration in blood as well as microdialysate. The high gastrin concentration following omeprazole treatment was not affected by vagotomy. Vagal excitation stimulated the G cells: electrical vagal stimulation and pylorus ligation (fasted rats) raised the gastrin concentration transiently...... microdialysate gastrin concentration in omeprazole-treated rats by 65%. We conclude that activated gastrin release, unlike basal gastrin release, is highly dependent on a neural input: 1) Vagal excitation has a transient stimulating effect on the G cells. The transient nature of the response suggests...

  7. 奥美拉唑与法莫替丁治疗反流性食管炎的临床疗效对比

    Institute of Scientific and Technical Information of China (English)

    任伟旺

    2016-01-01

    目的:分析奥美拉唑与法莫替丁治疗反流性食管炎的临床疗效。方法收集我院2011年1月至2014年7月期间诊治的96例反流性食管炎患者作为研究对象,根据患者的治疗方式将其分为奥美拉唑联合组(48例)与奥美拉唑组(48例),奥美拉唑组患者单纯采用奥美拉唑治疗,奥美拉唑联合组采用奥美拉唑与法莫替丁治疗,观察患者的治疗效果及治疗前后的症状评分改善情况。结果奥美拉唑联合组的总体疗效明显优于奥美拉唑组(P<0.05),且奥美拉唑联合组治疗前后的症状评分改善水平明显优于奥美拉唑组(P<0.05)。结论奥美拉唑与法莫替丁治疗反流性食管炎具有良好的临床疗效,值得临床进一步推广使用。%Objective To analyze the clinical effects of reflux esophagitis cured by omeprazole and famotidine.Methods 96 patients who suffered from the reflux esophagitis and who accepted treatments in our hospital from January , 2011 to July, 2014 were taken as the research objects , and according to the patient's treatment methods these patients were randomly divided into the omeprazole combination group ( 48 cases ) and omeprazole group (48 cases).In the omeprazole group , they were treated with the simple omeprazole while in the omeprazole combination group , they were treated with the omeprazole and famotidine .Then, the curing effects and before and after treatment , the symptom score improvement of these two groups of patients were observed . Results The comparison results of the overall effect of the two groups found that the omeprazole combination group was significantly better than that of omeprazole group (P<0.05), in addition, before and after treatment,the symptom score improvement in the omeprazole group was evidently better than that of omeprazole group (P <0.05).Conclusions The clinical effects of reflux esophagitis cured by omeprazole and famotidine has goodclinical

  8. The potential therapeutic effect of melatonin in gastro-esophageal reflux disease

    Directory of Open Access Journals (Sweden)

    El-Gendy Ahmed A

    2010-01-01

    Full Text Available Abstract Background Gastro-Esophageal Reflux Disease (GERD defined as a condition that develops when the reflux of stomach contents causes troublesome symptoms and/or complications. Many drugs are used for the treatment of GERD such as omeprazole (a proton pump inhibitor which is a widely used antiulcer drug demonstrated to protect against esophageal mucosal injury. Melatonin has been found to protect the gastrointestinal mucosa from oxidative damage caused by reactive oxygen species in different experimental ulcer models. The aim of this study is to evaluate the role of exogenous melatonin in the treatment of reflux disease in humans either alone or in combination with omeprazole therapy. Methods 36 persons were divided into 4 groups (control subjects, patients with reflux disease treated with melatonin alone, omeprazole alone and a combination of melatonin and omeprazole for 4 and 8 weeks Each group consisted of 9 persons. Persons were subjected to thorough history taking, clinical examination, and investigations including laboratory, endoscopic, record of esophageal motility, pH-metry, basal acid output and serum gastrin. Results Melatonin has a role in the improvement of Gastro-esophageal reflux disease when used alone or in combination with omeprazole. Meanwhile, omeprazole alone is better used in the treatment of GERD than melatonin alone. Conclusion The present study showed that oral melatonin is a promising therapeutic agent for the treatment of GERD. It is an effective line of treatment in relieving epigastric pain and heartburn. However, further studies are required to confirm the efficacy and long-term safety of melatonin before being recommended for routine clinical use. Trial Registration QA13NCT00915616

  9. The effect of N-acetyl cysteine on laryngopharyngeal reflux.

    Directory of Open Access Journals (Sweden)

    Payman Dabirmoghaddam

    2013-11-01

    Full Text Available Laryngopharyngeal reflux (LPR is a variant of gastroesophageal reflux disease (GERD in which the stomach contents go up into the pharynx and then down into the larynx. LPR causes a wide spectrum of manifestations mainly related to the upper and the lower respiratory system such as laryngitis, asthma, chronic obstructive pulmonary disease, cough, hoarseness, postnasal drip disease, sinusitis, otitis media, recurrent pneumonia, laryngeal cancer and etc. The object of this study was to examine the effect of N-acetyl Cysteine (NAC with and without Omeprazole on laryngitis and LPR. Ninety patients with laryngitis or its symptoms were referred and randomly assigned into three groups. The first group was treated by Omeprazole and NAC. The second group was treated by Omeprazole and placebo and the last group was treated by NAC and placebo. Duration of treatment was 3 months and all patients were evaluated at the beginning of study, one month and three month after treatment of sign and symptoms, based on reflux symptom index (RSI and reflex finding score (RFS. Based on the results of this study, despite therapeutic efficacy of all treatment protocols, the RSI before and after 3 months treatment had significant difference in (NAS+ Omeprazole and (Omeprazole+ placebo group (P<0.001 in the first group, P<0.001 in the second group and P=0.35 in the third group. Whereas RFS before and after 3 month treatment had significant difference in all groups. (P<0.001 in each group in comparison with itself but this results had not significant difference after 1 month treatment. Our results showed that the combination therapy with Omeprazole and NAC treatment had the most effect on both subjective and objective questionnaire at least after 3 months treatment. Based on the results of the present study, it seems that the use objective tools are more accurate than subjective tools in evaluation of therapeutic effects in patients with GERD-related laryngitis.

  10. The OAC and OMC options.

    Science.gov (United States)

    Unge, P

    1999-08-01

    In three studies, the two most successful regimens in the MACH1 study (omeprazole-amoxycillin-clarithromycin (OAC) and omeprazole-metronidazole-clarithromycin (OMC)) were investigated further. Double-blind, randomized, international, multi-centre studies with parallel groups. The studies were performed at centres in France, Germany, Ireland, Norway, Sweden and the UK (MACH2), Canada (DU-MACH) and Germany, Hungary and Poland (GU-MACH). In MACH2, the influence of omeprazole on eradication was investigated in patients with duodenal ulcers in remission, using OAC, AC, OMC and MC. In DU-MACH and GU-MACH, eradication and relapse rates were investigated in patients with active peptic ulcers, using: OAC, OMC and omeprazole alone. Eradication of Helicobacter pylori. In patients with active peptic ulcer, ulcer healing was also assessed. In MACH2 (n = 514, intention-to-treat (ITT) analysis), the addition of omeprazole to AC increased the eradication rate from 26 to 94%. The corresponding increase for MC/ OMC was from 69 to 87%. The efficacy of the AC and OAC regimens was unaffected by primary metronidazole resistance, while that of MC was halved and that of OMC reduced by 15%. Clarithromycin resistance was uncommon. In DU-MACH and GU-MACH (n = 146 and 145, ITT analysis), eradication rates were high with both regimens. Ulcer healing rates were also high in all treatment groups; ulcer relapse was significantly less frequent in the OAC and OMC groups. All regimens were well tolerated. Omeprazole triple therapy is highly effective in patients with active or healed peptic ulcer disease, and is well tolerated.

  11. The influence of changes in hospital drug formulary on the prescription of proton pump inhibitors

    Directory of Open Access Journals (Sweden)

    Raquel Vázquez-Mourelle

    2017-01-01

    Full Text Available Objective: To analyze the impact of introducing omeprazole in the drug formulary of the Hospital de Barbanza on prescriptions made in hospital and out-of-hospital (Outpatient Units and Primary Care for all Proton Pump Inhibitors (PPIs. Material and methods: A 36-month retrospective descriptive study in a level I hospital. The basic units of work are Dose-Population- Day in the outpatient setting, and the Defined Daily Dose/stays-day for hospitalized patients; the proportion of DDDs for omeprazole vs. the rest of PPIs is used as measure of efficiency. For statistical analysis, we built a segmented regression model. Results: In the outpatient units, there are statistically significant changes for pantoprazole and rabeprazole. The first drug, which was stable before the intervention, suffered an immediate decrease; rabeprazole, which was increasing before the intervention, presented a subsequent downward trend. In Primary Care, a statistically significant change was confirmed for pantoprazole, with a long-term decreasing trend. In hospitalization, statistically significant changes were observed for pantoprazole and omeprazole; the first one with an immediate decrease and a long-term tendency to decrease, while omeprazole experienced an immediate increase and long-term growth. The evolution of the omeprazole percentage vs. all PPIs showed increases in all three scenarios. Conclusions: A shift to a more efficient prescription of PPIs was observed in all healthcare settings following the introduction of omeprazole in the hospital drug formulary. The inclusion of efficient drugs, or the removal of those inefficient, can be a potentially useful tool in order to improve prescription profiles.

  12. Antagonism of Fluconazole and a Proton Pump Inhibitor against Candida albicans.

    Science.gov (United States)

    Liu, Ning-Ning; Köhler, Julia R

    2016-02-01

    Hospitalized ill patients, at risk for invasive candidiasis, often receive multiple medications, including proton pump inhibitors (PPIs). The antifungal fluconazole perturbs the vacuolar proton ATPase. The PPI omeprazole antagonized Candida albicans growth inhibition by fluconazole. A C. albicans codon-adapted pHluorin, Ca.pHluorin, was generated to measure cytosolic pH. The fungal cytosol was acidified by omeprazole and realkalinized by coexposure to fluconazole. Vacuolar pH was alkalinized by fluconazole. Off-target effects of any medication on fungal pathogens may occur.

  13. Sesgos de confusión por indicación y gravedad en estudios observacionales Confounding bias due to indication and severity in observational studies

    OpenAIRE

    2011-01-01

    Los estudios observacionales están sujetos a sesgos que pueden conducir a una interpretación errónea de los resultados. El presente estudio tuvo como objetivo determinar la influencia del tratamiento con omeprazol sobre la duración de la baja laboral en pacientes con esguince de tobillo que tomaban antiinflamatorios no esteroideos. Se utilizaron los registros de la base de datos de la mutua Ibermutuamur. En contra de lo esperado, se observó que los pacientes que recibieron omeprazol presentar...

  14. Revealing the Mechanistic Pathway of Acid Activation of Proton Pump Inhibitors To Inhibit the Gastric Proton Pump: A DFT Study.

    Science.gov (United States)

    Jana, Kalyanashis; Bandyopadhyay, Tusar; Ganguly, Bishwajit

    2016-12-29

    Acid-related gastric diseases are associated with disorder of digestive tract acidification due to the acid secretion by gastric proton pump, H(+),K(+)-ATPase. Omeprazole is one of the persuasive irreversible inhibitor of the proton pump H(+),K(+)-ATPase. However, the reports on the mechanistic pathway of irreversible proton pump inhibitors (PPIs) on the acid activation and formation of disulfide complex are scarce in the literature. We have examined the acid activation PPIs, i.e., timoprazole, S-omeprazole and R-omeprazole using M062X/6-31++G(d,p) in aqueous phase with SMD solvation model. The proton pump inhibitor is a prodrug and activated in the acidic canaliculi of the gastric pump H(+),K(+)-ATPase to sulfenic acid which can either form another acid activate intermediate sulfenamide or a disulfide complex with cysteine amino acid of H(+),K(+)-ATPase. The quantum chemical calculations suggest that the transition state (TS5) for the disulfide complex formation is the rate-determining step of the multistep acid inhibition process by PPIs. The free energy barrier of TS5 is 5.5 kcal/mol higher for timoprazole compared to the S-omeprazole. The stability of the transition state for the formation of disulfide bond between S-omeprazole and cysteine amino acid of H(+),K(+)-ATPase is governed by inter- and intramolecular hydrogen bonding. The disulfide complex for S-omeprazole is thermodynamically more stable by 4.5 kcal/mol in aqueous phase compared to disulfide complex of timoprazole, which corroborates the less efficacy of timoprazole as irreversible PPI for acid inhibition process. It has been speculated that sulfenic acid can either form sulfenamide or a stable disulfide complex with cysteine amino acid residue of H(+),K(+)-ATPase. The M062X/6-31++G(d,p) level of theory calculated results reveal that the formation of tetra cyclic sulfenamide is unfavored by ∼17 kcal/mol for S-omeprazole and 11.5 kcal/mol for timoprazole compared to the disulfide complex formation

  15. Are proton pump inhibitors the first choice for acute treatment of gastric ulcers? A meta analysis of randomized clinical trials

    Directory of Open Access Journals (Sweden)

    Ward Alexandra

    2002-07-01

    Full Text Available Abstract Background Gastric ulcers are a frequent problem in the United States. Proton pump inhibitors have been shown to increase healing rates and improve clinical symptoms. The objective of this study is to compare gastric ulcer healing rates for patients treated with a proton pump inhibitor (PPI (omeprazole, rabeprazole, pantoprazole, or lansoprazole, an histamine 2- receptor antagonist (ranitidine or placebo. Methods A literature search was conducted to identify randomized, controlled clinical trials that included a PPI in at least one treatment arm and assessed the gastric ulcer healing rates endoscopically. The healing rates were estimated for each treatment at specific time points, and Rate Ratios (RR and 95% confidence intervals (CI were estimated for each trial. Results Sixteen trials met the inclusion criteria: four compared a PPI versus placebo, nine compared a PPI versus ranitidine (no trials of rabeprazole versus ranitidine met the inclusion criteria, and three compared a newer PPI (lansoprazole, pantoprazole or rabeprazole versus omeprazole. In relation to ranitidine, the pooled RR of PPIs (lansoprazole, omeprazole and pantoprazole was 1.33 (95% CI 1.24 to 1.42 at four weeks. In each trial, greater improvement in the studied clinical symptoms was found with the newer PPIs (rabeprazole, pantoprazole and lansoprazole when compared to omeprazole. Conclusion In this study treatment with PPIs resulted in higher healing rates than ranitidine or placebo. This evidence suggests that the first choice for gastric ulcer treatment for the greater relief of symptoms is one of the newer PPIs.

  16. An optimized methodology for combined phenotyping and genotyping on CYP2D6 and CYP2C19

    NARCIS (Netherlands)

    Tamminga, C.A; Wemer, J; Oosterhuis, B; Brakenhoff, J.P G; Gerrits, M.G F; de Zeeuw, R.A; de Leij, Lou; Jonkman, J.H.G.

    2001-01-01

    A method for simultaneous phenotyping and genotyping for CYP2D6 and CYP2C19 was tested. Six healthy volunteers were selected (three extensive and three poor metabolisers for CYP2D6). CYP2D6 was probed with dextromethorphan and metoprolol and CYP2C19 was probed with omeprazole. Blood samples were col

  17. Effects of acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir and ritonavir-boosted atazanavir.

    Science.gov (United States)

    Klein, Cheri E; Chiu, Yi-Lin; Cai, Yan; Beck, Katrin; King, Kathryn R; Causemaker, Sonja J; Doan, Thao; Esslinger, Hans-Ulrich; Podsadecki, Thomas J; Hanna, George J

    2008-05-01

    A total of 71 HIV-negative healthy adults were randomized to 1 of 6 regimens to receive lopinavir/ritonavir tablets 400/100 mg twice daily (bid) or 800/200 mg once daily (qd) or atazanavir 300 mg + ritonavir 100 mg qd from study days 1 to 15 with a moderate-fat meal. One hour before breakfast, either omeprazole 40 mg qd was administered on study days 11 through 15, or a single dose of ranitidine 150 mg was administered on study day 11. Lopinavir, atazanavir, and ritonavir pharmacokinetics were determined on study days 10, 11, and 15 and compared using point estimates and 90% confidence intervals (CIs). The point estimates for lopinavir Cmax and AUCtau were in the range of 0.92 to 1.08, with 90% CI contained within the range of 0.80 to 1.25 after coadministration of omeprazole or ranitidine. The point estimates for atazanavir Cmax and AUCtau were decreased by 48% to 62% with the upper bound of the 90% CI ranitidine. The results indicated that lopinavir bioavailability was not affected by the coadministration of omeprazole or ranitidine. In contrast, atazanavir bioavailability was decreased by 48% to 62% when coadministered with ritonavir and either omeprazole or ranitidine.

  18. Comparative study of proton pump inhibitors on dexamethasone plus pylorus ligation induced ulcer model in rats

    Directory of Open Access Journals (Sweden)

    Thippeswamy A. H. M.

    2010-01-01

    Full Text Available The present study was designed to compare ulcer protective effect of proton pump inhibitors viz. omeprazole, rabeprazole and lansoprazole against dexamethasone plus pylorus ligation induced ulcer model. Dexamethasone (5 mg/kg was used as an ulcerogen. Dexamethasone suspended in 1% CMC in water was given orally to all the rats 15 min after the pylorus ligation. Omeprazole (20 mg/kg, rabeprazole (20 mg/kg, and lansoprazole (20 mg/kg were administered by oral route 30 min prior to ligation was used for ulcer protective studies, gastric secretion and mucosal studies. Effects of proton pump inhibitors were determined by the evaluation of various biochemical parameters such as ulcer index, free and total acidity, gastric pH, mucin, pepsin and total proteins. Oral administration of proton pump inhibitors showed significant reduction in gastric acid secretion and ulcer protective activity against dexamethasone plus pylorus ligation induced ulcer model. The % protection of omeprazole, rabeprazole and lansoprazole was 84.04, 89.36 and 79.78, respectively. Rabeprazole significantly inhibited the acid-pepsin secretion and increased the gastric mucin secretion. The observations made in the present study suggest that rabeprazole is the most effective gastric antisecretory and ulcer healing agent as compared to omeprazole and lansoprazole.

  19. Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.

    NARCIS (Netherlands)

    Witte, W.E.; Wong, Y.C.; Nederpelt, I.; Heitman, L.H.; Danhof, M.; Graaf, van der P.H.; Gilissen, R.A.; de, Lange E.C.

    2016-01-01

    INTRODUCTION Drug-target binding kinetics are major determinants of the time course of drug action for several drugs, as clearly described for the irreversible binders omeprazole and aspirin. This supports the increasing interest to incorporate newly developed high-throughput assays for drug-target

  20. 奥美拉唑联合血凝酶治疗上消化道出血的临床疗效分析

    Institute of Scientific and Technical Information of China (English)

    周燕

    2013-01-01

      为探讨奥美拉唑联合血凝酶治疗上消化道出血的临床疗效,抽取上消化道出血患者60例,分为两组进行不同的治疗,对对照组进行单纯奥美拉唑治疗,对实验组采取奥美拉唑联合血凝酶治疗。可知奥美拉唑联合血凝酶治疗上消化道出血的临床效果更好,有一定的积极临床治疗意义。%in order to investigate the effect of omeprazole combined with hemocoagulase treatment of upper gastrointestinal hemorrhage, extraction of upper gastrointestinal bleeding in patients with 60 cases, divided into two groups for different treatment, the control group were only treated with omeprazole, taking omeprazole combined with hemocoagulase therapy on experimental group. The effect of omeprazole combined with hemocoagulase treatment of upper digestive tract hemorrhage better clinical effect, have positive clinical significance.

  1. Pharmacoeconomic analysis of proton pump inhibitor therapy and interventions to control Helicobacter pylori infection

    NARCIS (Netherlands)

    Klok, Rogier Martijn

    2006-01-01

    In dit proefschrift worden de farmacoeconomische aspecten van problemen in het bovenste deel van het gastrointestinale tract besproken. De uitwisselbaarheid van proton pomp remmers (PPRs) wordt besproken net als switch patronen na het aflopen van het patent van omeprazol, de eerste PPR op de Nederla

  2.   A Cost-Effectiveness Analysis of Two Management Strategies for Dyspepsia

    DEFF Research Database (Denmark)

    Kjeldsen, Hans Chr; Bech, Mickael; Christensen, Bo

    2007-01-01

    June 2000 to August 2002, Aarhus County, Denmark. We randomly assigned 368 dyspeptic patients from 32 general practices to treatment with omeprazol 40 mg for two weeks (n: 184) or endoscopy (n: 184). The study adopted a societal perspective, and the year of costing was 2006. Outcome measures: days free...

  3. Experiments to optimize enzyme substitution therapy in pancreatic duct-ligated pigs.

    Science.gov (United States)

    Kammlott, E; Karthoff, J; Stemme, K; Gregory, P; Kamphues, J

    2005-01-01

    Ligation of the pancreatic duct in pigs leads to severe maldigestion and malabsorption of crude nutrients. Supplementation with 24 capsules of Creon (Solvay Pharmaceuticals GmbH, Hannover, Germany) per meal led to an increased digestibility of crude nutrients. With regard to optimization of the treatment of EPI no essential improvements can be achieved by adding omeprazol or lecithin to the diet. In pancreatic duct-ligated pigs the isolated addition of omeprazol led to an increase of the pre-caecal digestibility of crude fat and organic matter. With additional enzyme substitution, the application of omeprazol did not result in an improved fat digestibility. Isolated addition of lecithin to the diet resulted in a reduced total digestibility of crude fat. Offering the diet twice a day and using a higher frequency of enzyme applications (four or six instead of only two applications) had no effects on the digestibilty of crude fat or organic matter. According to the observations in pancreatic duct-ligated pigs, the addition of missing enzymes to the diet led to the best treatment results in EPI. Administration of omeprazol or a higher feeding frequency as well as the application of enzymes in small proportion of the whole meal or dosages given consecutively over the day showed no advantages. Furthermore, the present study suggests that the addition of lecithin cannot be recommended in EPI, when given diets with butter as the predominant fat source as in human dietetics.

  4. Leucopenia grave em paciente com artrite reumatoide tratada com combinação de metotrexato e leflunomida

    Directory of Open Access Journals (Sweden)

    Paola Toth

    2014-04-01

    Full Text Available Apresentamos o caso de uma paciente com artrite reumatoide tratada por dois anos com associação de metotrexato e leflunomida. A paciente foi internada com leucopenia grave quatro semanas após acrescentar ao esquema medicamentoso as drogas clopidogrel, isosorbida, sinvastatina, AAS e omeprazol.

  5. [Switching to a generic drugA blessing or a curse?

    NARCIS (Netherlands)

    Ebbelaar, C.F.; Lammers, H.A.; Schobben, A.F.

    2016-01-01

    A patient suffering from Zollinger-Ellison was treated with Nexium, but after patent expiry only the costs of generic omeprazol were reimbursed. Generic tablets and capsules, pantoprazol and rabeprazol, were tried without success and finally the pharmacist dispensed Nexium at his own expense. Regist

  6. Aplicación de la farmacoeconomía a los resultados de la medicación para la curación de las úlceras pépticas

    Directory of Open Access Journals (Sweden)

    Manuel M Collazo Herrera

    2000-12-01

    Full Text Available Se realizó una evaluación económica comparativa de los costos de los tratamientos quimioterapéuticos de 3 esquemas antiulcerosos (ranitidina, omeprazol y cimetidina; así como el análisis costo-efectividad para determinar la combinación de medicamentos que sería la más factible desde el punto de vista técnico-económico para la cicatrización de las úlceras pépticas y la erradicación del agente causante, el Helicobacter pylori. Como resultado se obtiene un esquema quimioterapéutico combinado para diferentes ciclos de tiempos en los tratamientos antiulcerosos (ranitidina-omeprazol, que incrementa la efectividad y disminuye los costos de los medicamentos para el sistema nacional de salud.A comparative economic evaluation of the costs of chemotherapeutic treatments of 3 anti-ulcer schemes (ranitidine, omeprazol and cimetidine, as well as the cost-effectiveness analysis were made to determine the most convenient drug combination for the cicatrization of peptic ulcer and for the erradication of its causal agent, Helicobacter pylori, from the economic and technical point of view. As a result, it was obtained a combined chemotherapeutic scheme for different cycles of time in the anti-ulcer treatments (ranitidine-omeprazol that increases the effectiveness and reduces the costs of drugs for the national health system.

  7. MOLECULARLY IMPRINTED POLYMER TECHNOLOGY: A ...

    African Journals Online (AJOL)

    dell

    Salbutamol (2-(hydroxymethyl)-4-[1-hydroxy-2-(tert-butylamino)ethyl]phenol) ... dimethylamino-3-methyl-1,2-diphenyl-butan-2-yl]propanoate) is an anti-cough agent. ... Efficacy of (S)-omeprazole over the racemic mixture is claimed. .... simultaneous exclusion of sulphur dioxide. ... thermal stability, which affords sterilization.

  8. Pharmacoeconomic analysis of proton pump inhibitor therapy and interventions to control Helicobacter pylori infection

    NARCIS (Netherlands)

    Klok, Rogier Martijn

    2006-01-01

    In dit proefschrift worden de farmacoeconomische aspecten van problemen in het bovenste deel van het gastrointestinale tract besproken. De uitwisselbaarheid van proton pomp remmers (PPRs) wordt besproken net als switch patronen na het aflopen van het patent van omeprazol, de eerste PPR op de

  9. The Weber-curve pitfall : effects of a forced introduction on reporting rates and reported adverse reaction profiles

    NARCIS (Netherlands)

    de Graaf, Linda; Fabius, Mariette A; Diemont, Willem L; van Puijenbroek, Eugène P

    2003-01-01

    BACKGROUND: In May 1999 Losec MUPS (MUPS) were granted a marketing authorization in the Netherlands, followed by the withdrawal of the Losec capsules (capsules) in September 1999. Both formulations contain omeprazole as active substance. This forced switch resulted in a large number of spontaneous r

  10. The Clopidogrel-PPI Interaction

    DEFF Research Database (Denmark)

    Juel, Jacob; Pareek, Manan; Jensen, Svend Eggert

    2014-01-01

    the potential for PPIs, especially omeprazole, to decrease the efficacy of clopidogrel, and both the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) have issued warnings regarding the concomitant use of these medications. A review of the literature revealed that the pharmacodynamic...

  11. [THE EFFECTIVENESS OF A 10-DAY DRUG THERAPY IN CHILDREN WITH CHRONIC GASTRODUODENAL PATHOLOGY ASSOCIATED WITH CAGA-POSITIVE STRAINS OF HELICOBACTER PYLORI].

    Science.gov (United States)

    Dudnyk, V M; Rudenko, G M

    2015-01-01

    The results of triple Helicobacter-therapy (omeprazole, amoxicillin, nifuratel) in the treatment of chronic gastroduodenal pathology in children depending on the duration of it's use. The effectiveness of drug therapy was evaluated in terms of eradication of Helicobacter pylori and dynamics of pain, dyspeptic syndrome and astenovegetative syndrome.

  12. A randomized controlled comparison of three quadruple therapy regimens in a population with low Helicobacter pylori eradication rates

    NARCIS (Netherlands)

    Sotudehmanesh, Rasool; Malekzadeh, Reza; Fazel, Ali; Massarrat, Sadegh; Ziad-Alizadeh, Behrooz; Eshraghian, Mohammed Reza

    2001-01-01

    Background and Aim: We sought to compare the efficacy and tolerability of an omeprazole/clarithromycin/bismuth/tetracycline-based quadruple therapy to that of a ranitidine/metronidazole/bismuth/tetracycline-based quadruple therapy of 2 or 3 weeks duration in a population with a high prevalence of me

  13. Leucopenia grave em paciente com artrite reumatoide tratada com combinação de metotrexato e leflunomida

    OpenAIRE

    Paola Toth; Roberto Bernd

    2014-01-01

    Apresentamos o caso de uma paciente com artrite reumatoide tratada por dois anos com associação de metotrexato e leflunomida. A paciente foi internada com leucopenia grave quatro semanas após acrescentar ao esquema medicamentoso as drogas clopidogrel, isosorbida, sinvastatina, AAS e omeprazol.

  14. Morbidity and Mortality in Preterm Infants following Antacid Use: A Retrospective Audit

    Directory of Open Access Journals (Sweden)

    Natasha Singh

    2016-01-01

    Full Text Available Background and Objectives. Antacids are often prescribed to preterm infants due to misdiagnosis of gastro-oesophageal reflux. This suppresses gastric acidity, a major defence mechanism against infection. This study aims to determine if ranitidine and omeprazole use in very low birth weight (VLBW neonates, <1500 grams, is associated with increased risk of late onset sepsis, necrotising enterocolitis (NEC, and mortality. Methods. Retrospective analysis was conducted on neonates, <1500 grams, born and admitted into the Neonatal Intensive Care Unit at The Canberra Hospital during the period from January 2008 to December 2012. Information regarding late onset sepsis, NEC, mortality, ranitidine/omeprazole use, and other neonatal/hospital factors was collected for each neonate. Results. 360 neonates were evaluated, 64 received ranitidine and/or omeprazole, and 296 had not. There were no statistically significant differences in incidence of late onset sepsis (OR = 0.52, CI = 0.24–1.1, and p = 0.117, NEC Stage 2 and above (OR = 0.4, CI = 0.05–3.2, and p = 0.7, or mortality (OR = 0.35, CI = 0.08–1.5, and p = 0.19 between the two groups. After adjusting significant differences in neonatal and hospital factors, risk of late onset sepsis was significantly lower in those that received ranitidine/omeprazole (OR = 0.28, CI = 0.13–0.65, and p = 0.003. Conclusions. Ranitidine and omeprazole use in VLBW preterm infants may not be associated with an increased risk of infection, NEC, and mortality.

  15. Relationship between the acid-suppression efficacy of proton pump inhibitors and CYP2C19 genetic polymorphism in patients with peptic ulcer

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Obiective To investigate acid-suppression efficacy of proton pump inhibitors(PPls) in relation to CYP2C19 genetic polymorphism on patients with peptic ulcer. Methods By an open, randomized and control trial, fifty nine patients with active peptic ulcer were randomly assigned to receive one of three PPIs on a single dose (20 mg of each drug): omeprazole group (n=19), rabeprazole group (n=20) and esomeprazole group (n=20). lntragastric pH was recorded 1 hour before and 24 hours after administration. CYP2C19 genotype was tested in all patients. Resuits The EMs/PMs ratio of each group was 16/3,17/3 and 17/3, respectively. The total time that intragastric pH>4, time percent pH>4 and median pH in PMs patients were significantly higher than those in EMs patients of omeprazole group (P<0.05). But all these differences were not found in rabeprazole group and esomeprazole group. The pH of nocturnal acid breakthrough (NAB) in both rabeprazole group and esomeprazole group was higher than that of omeprazole group, while there was no significant difference between rabeprazole group and esomeprazole group. Gonclusion The acid-suppression efficacy of omeprazole is highly dependent on CYP2C19 genetic polymorphism, while CYP2C19 genetic polymorphism may have a little influence on the acid-suppression efficacy of rabeprazole and esomeprazole. The acid-suppression action of rabeprazole and esomeprazole is superior to omeprazole, especially on night acid secretion.

  16. Azithromycin in a triple therapy for H. pylori eradication in active duodenal ulcer

    Institute of Scientific and Technical Information of China (English)

    Vladimir T. Ivashkin; Tatiana L. Lapina; Oksana Yu. Bondarenko; Olga A. Sklanskaya; Petr Ya. Grigoriev; Yuri V. Vasiliev; Emilia P. Yakovenko; Pavel V. Gulyaev; Valeri I. Fedchenko

    2002-01-01

    AIM: To assess and compare the efficacy and safety of twotriple regimes: A) metronidazole, amoxicillin and omeprazole,which is still widely used in Russia, and B) azithromycin,amoxicillin and omeprazole in healing active duodenal ulcerand H.pylori eradication. METHODS: 100 patients with active duodenal ulcer wereincluded in the open, multicentre, randomized study withcomparative groups. Patients were randomly assigned toone of the following one-week triple regimes: A)metronidazole 500 mg bid, amoxicillin 1 g bid and omeprazole20 mg bid (OAM, n=50) and B) azithromycin 1 g od for thefirst 3 days (total dose 3 g), amoxicillin 1 g bid andomeprazole 20 mg bid (OAA, n=50). Omeprazole 20 mg odwas given after the eradication course as a monotherapyfor three weeks. The control endoscopy was performed 8weeks after the entry. H. pylori infection was determined inthe entry of the study and four weeks after the cessation oftreatment by means of histology and CLO-test.RESULTS: 97 patients completed the study according tothe protocol (1 patient of the OAM group did not come tothe control endoscopy, 2 patients of the OAA group stoppedthe treatment because of mild allergic urticaria). Duodenalulcers were healed in 48 patients of the OAM group (96 %;CI 90.5-100 %) and in 46 patients of the OAA group (92 %;CI 89.5-94.5 %) (p=ns). H. pylori infection was eradicatedin 15 out of 50 patients with OAM (30 %; CI 17-43 %) andin 36 out of 50 patients treated with OAA (72 %; CI 59-85 %)(P<0.001)-ITT analysis.CONCLUSION: The triple therapy with omeprazole,amoxicillin and metronidazole failed to eradicate H. pylori inthe majority of patients, which is an essential argument towithdraw this regimen out of the national recommendations.Macrolide with amoxicillin are preferable to achieve highereradication rates. Azithromycin (1 g od for the first 3 days)can be considered as a successful component of the triplePPI-based regimen.

  17. Evaluation of Clinical Curative Effect on 142 Patients With Gastric Ulcer%142例胃溃疡病例的临床疗效评价

    Institute of Scientific and Technical Information of China (English)

    王颖

    2015-01-01

    目的:对比分析不同治疗方案治疗胃溃疡的临床疗效。方法选择胃溃疡病例142例,随机分入奥美拉唑联合阿莫西林克拉维酸钾组和奥美拉唑组,每组各72例,选择总有效率为观察指标。结果奥美拉唑联合阿莫西林克拉维酸钾组总有效率95.13%和奥美拉唑组总有效率73.41%,P<0.05,差异具有统计学意义。结论对于胃溃疡的治疗,奥美拉唑联合阿莫西林克拉维酸钾具有更好的临床疗效。%Objective Compare with the curative effect on different treatment protocols of gastric ulcer. Methods Selected 142 patients with gastric ulcer were randomized to the omeprazole combined with amoxicillin group and the omeprazole group, each group had 72 cases. Observation index of total efifciency rate. Results The total efifciency rate was 95.13%in the omeprazole combined with amoxicillin group and 73.41% in the omeprazole group, P<0.05, had difference statistically significance. Conclusion Omeprazole combine with amoxicillin has better clinical curative effect on gastric ulcers.

  18. Characteristics of the K+-competitive H+,K+-ATPase inhibitor AZD0865 in isolated rat gastric glands.

    Science.gov (United States)

    Kirchhoff, P; Andersson, K; Socrates, T; Sidani, S; Kosiek, O; Geibel, J P

    2006-11-01

    The gastric H+,K+-ATPase of the parietal cell is responsible for acid secretion in the stomach and is the main target in the pharmacological treatment of acid-related diseases. Omeprazole and other benzimidazole drugs, although having delayed efficacy if taken orally, have high success rates in the treatment of peptic ulcer disease. Potassium competitive acid blockers (P-CAB) compete with K+ for binding to the H+,K+-ATPase and thereby they inhibit acid secretion. In this study, the in vitro properties of AZD0865, a reversible H+,K+-ATPase inhibitor of gastric acid secretion, are described. We used a digital-imaging system and the pH sensitive dye BCECF to observe proton efflux from hand-dissected rat gastric glands. Glands were stimulated with histamine (100 microM) and exposed to a bicarbonate- and Na+-free perfusate to induce an acid load. H+,K+-ATPase inhibition was determined by calculating pHi recovery (dpH/dT) in the presence of omeprazole (10-200 microM) or AZD0865 (0.01-100 microM). The efficacies of both drugs were compared. Our data show that acid secretion is inhibited by both the proton pump inhibitor omeprazole and the P-CAB AZD0865. Complete inhibition of acid secretion by AZD0865 had a rapid onset of activation, was reversible, and occurred at a 100-fold lower dose than omeprazole (1 microM AZD0865 vs. 100 microM omeprazole). This study demonstrates that AZD0865 is a potent, fast-acting inhibitor of gastric acid secretion, effective at lower concentrations than drugs of the benzimidazole class. Therefore, these data strongly suggest that AZD0865 has great potential as a fast-acting, low-dose inhibitor of acid secretion.

  19. Importance of Helicobacter pylori eradcation for maintenance of remission of drug associated peptic ulcer disease

    Directory of Open Access Journals (Sweden)

    Dajani A

    2006-01-01

    Full Text Available Background: The role of Helicobacter pylori (H. pylori eradication in non-steroidal anti inflammatory drug (NSAID users with peptic ulcer disease is controversial especially in countries with a high prevalence of the infection. Furthermore the value of low dose omeprazole for maintenance of remission is not yet known. Patients and methods: 138 symptomatic out-patients receiving continuous COX 1 NSAID therapy, were treated with omeprazole 40mg/day upon endoscopic confirmation of gastro-duodenal ulceration or erosions while those infected with H. pylori received in addition clarithromycin 500 mg and amoxycillin 1000 mg twice daily during the first week of treatment. After endoscopic confirmation of healing at the end of week 5, the patients were randomized to receive omeprazole 10 mg (n=50 or 20 mg once daily (n=66 and endoscopy repeated after 20 weeks. Results: The overall healing rate (per protocol at five weeks (116/128 was 90.6% while in 85.5% (65/76 eradication was successful. The healing rate for the H. pylori eradicated patients (58/65 was 89.2%. For those who failed eradication (8/11 it was 72.7% (NS, while for patients not infected with H. pylori at entry to the study (50/52 it was 96.2% (NS. An intention to treat analysis showed that after 20 weeks of omeprazole prophylaxis with the 10mg dose 86% (43/50 had maintained healing while for the 20mg dose a similar figure was observed (87.9; 58/66. Only three patients in the two groups (pp had persistent H. pylori infection, all of whom relapsed. No patients discontinued treatment because of adverse effects of the drugs. Conclusion: H. pylori eradication was not associated with impaired ulcer healing in a Middle Eastern population with symptomatic NSAID induced gastro/duodenal lesions, when a high healing dose of omeprazole (40 mg was used. After eradication, omeprazole 10 or 20 mg per day were highly and equally effective for maintenance of gastroduodenal mucosal integrity during continued

  20. Comparison of the protective effects of various antiulcer agents alone or in combination on indomethacin-induced gastric ulcers in rats.

    Science.gov (United States)

    Izzettin, Fikret Vehbi; Sancar, Mesut; Okuyan, Betul; Apikoglu-Rabus, Sule; Cevikbas, Ugur

    2012-05-01

    The aim of this study which was structured with the objective of determination of the optimum protective therapy against the long term NSAID therapy-induced ulcers was to compare the gastro-protective effects of various antiulcer drugs (ranitidine, omeprazole, bismuth and misoprostol) alone or in combination with each other in different doses on indomethacin-induced gastric ulcers in rats. In this experimental study the protective effect of misoprostol (100 μg/kg/day and 10 μg/kg/day i.g.), omeprazole (5 mg/kg/day and 1.5 mg/kg/day i.p.), ranitidine (40 mg/kg/day and 10 mg/kg/day i.p.), bismuth (70 mg/kg/day and 15 mg/kg/day i.g.), combinations of misoprostol (10 μg/kg/day i.g.) plus omeprazole (1.5mg/kg/day i.p.) and misoprostol (10 μg/kg/day i.g.) plus ranitidine (10 mg/kg/day i.p.) are investigated on indomethacin (50 mg/kg/day s.c.) induced gastric ulcers. Half an hour before indomethacin administration, each group received the above treatment regimens for 5 days. After 5-day treatment, the rats were sacrificed and histopathological and hematological examinations were performed. The following regimens were found to be effective in the prevention of indomethacin-induced gastric lesions: 100 μg/kg misoprostol, 10 μg/kg misoprostol, 5mg/kg omeprazole, combination of 10 μg/kg misoprostol plus 1.5 mg/kg omeprazole and 10 μg/kg misoprostol plus 10 mg/kg ranitidine. The prevention rates achieved by these treatments were 71.4%, 50%, 47.6%, 52.4% and 50%, respectively. As a result of this study, misoprostol and omeprazol were found to be effective in protection against NSAID-induced gastric problems; while, ranitidine and bismuth were not. Also, the combinations of these agents were not found to have additive or synergistic effects.

  1. Gastrin release: Antrum microdialysis reveals a complex neural control

    DEFF Research Database (Denmark)

    Ericsson, P; Håkanson, R; Rehfeld, Jens F.

    2010-01-01

    in serum regardless of the prandial state. The rats were conscious during microdialysis except when subjected to electrical vagal stimulation. Acid blockade (omeprazole treatment of freely fed rats for 4 days), or bilateral sectioning of the abdominal vagal trunks (fasted, 3 days post-op.), raised...... the gastrin concentration in blood as well as microdialysate. The high gastrin concentration following omeprazole treatment was not affected by vagotomy. Vagal excitation stimulated the G cells: electrical vagal stimulation and pylorus ligation (fasted rats) raised the gastrin concentration transiently...... that vagotomy suppresses an inhibitory as well as a stimulating effect on the G cells. While local infusion of atropine was without effect, infusion of the neuronal blocker tetrodotoxin (TTX) (which had no effect on basal gastrin) virtually abolished the food-evoked gastrin response and lowered the high...

  2. Impact of Age, Gender, and Addition of Probiotics on Treatment Success for Helicobacter pylori in Children

    Directory of Open Access Journals (Sweden)

    Noam Weiner MD

    2015-10-01

    Full Text Available The primary objective of this study was to evaluate the effect of age, gender, and the use of probiotics with standard treatment regimen on Helicobacter pylori eradication. Based on endoscopic findings and clinical presentation, selected patients were treated with standard triple therapy (omeprazole, clarithromycin, and amoxicillin. Those who failed were offered a repeat treatment with omeprazole, metronidazole, and amoxicillin. After the publications of the possible advantages of probiotic treatment on H pylori eradication, the probiotic agent “Probiotica Forte” was routinely added to the treatment. Eradication was noted for 94/130 patients (72% and for 128/197 patients (65% with or without probiotic agent, respectively (P = .23. For second-line treatment eradication was noted in 33/46 (72% and in 9/20 (45% with or without probiotic agent, respectively (P = .053. The addition of probiotics may improve eradication success especially in addition to second-line treatment.

  3. Effect of antisecretory agents and vagotomy on healing of "chronic" cysteamine-induced duodenal ulcers in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier

    1986-01-01

    Penetrated cysteamine-induced duodenal ulcers in rats have a very prolonged course of healing. In this study, it was investigated how much the healing of these ulcers is accelerated by some treatments. The treatments included omeprazole, cimetidine, and truncal vagotomy. In addition, the effect...... of omeprazole and cimetidine on gastric acid secretion was investigated in chronic gastric fistula rats. After 25 days of treatment, significantly more rats in the treated groups had healed ulcers than in the control group. There was little further improvement up to 100 days of treatment, and the difference...... between treated and untreated groups decreased. The morphology of healing ulcers in treated and untreated rats was also compared. In controls, there was a simultaneous regeneration of mucosa and the submucosal Brunner's glands from the edges of the ulcer, the slow proliferation rate of the latter probably...

  4. Refractory ulcer of reconstructed gastric tube after esophagectomy: a case report.

    Science.gov (United States)

    Okamura, Yuki; Takeno, Shinsuke; Takahashi, Yoshiaki; Moroga, Toshihiko; Yamashita, Shin-ichi; Kawahara, Katsunobu

    2013-01-01

    We report a case in which rabeprazole cured gastric tube ulcer after esophagectomy for esophageal squamous cell carcinoma (ESCC). A 47-year-old Japanese man was referred to our hospital with refractory ulcer of the reconstructed gastric tube one year after esophagectomy for ESCC. The ulcer proved refractory to healing by the administration of omeprazole or lansoprazole, or eradication of Helicobacter pylori after examinations concerning ischemia, acid over-secretion and H. pylori infection. Finally, metabolizer type was examined for proton pump inhibitors (PPIs), revealing the patient as a hetero-extensive metabolizer for the CYP2C19 genotype. This suggested sensitivity to rabeprazole, but resistance to omeprazole and lansoprazole. The refractory ulcer was subsequently cured after changing the PPI to rabeprazole. Examination of PPI metabolizer type might thus be important, along with an investigation of ischemia, acid secretion and H. pylori infection in the treatment of refractory gastric tube ulcer after esophagectomy.

  5. Acute gastroduodenal injury after ingestion of diluted herbicide pendimethalin.

    Science.gov (United States)

    Tsukada, K; Azuhata, H; Katoh, H; Kuwano, H

    2009-03-01

    The herbicide, pendimethalin, is used worldwide, but its acute toxicity is not yet widely known. There have been some reported acute pendimethalin poisoning cases in humans and most of them intentionally ingested the concentrated formulation. We describe a 73-year-old man who developed corrosive gastroduodenal injury after accidental ingestion of the diluted (300 times with water) pendimethalin formulation. He had a history of reflux oesophagitis and had been taking omeprazol (10 mg/day) for a year. He consumed alcohol two hours after the accidental ingestion and then had nausea and epigastric pain. Endoscopy performed three days post-exposure revealed gastroduodenal injury. As he had consumed alcohol every day for years and had no history of gastroduodenal ulcer, the accidental ingestion may be associated with this injury. He was successfully treated by increasing his dosage of omeprazol (20 mg/day) for two weeks. This case indicates that ingestion of a small quantity of pendimethalin can provoke gastroduodenal injury.

  6. Extraction of the volatile oil from Carum carvi of Tunisia and Lithuania by supercritical carbon dioxide: chemical composition and antiulcerogenic activity.

    Science.gov (United States)

    Baananou, Sameh; Bagdonaite, Edita; Marongiu, Bruno; Piras, Alessandra; Porcedda, Silvia; Falconieri, Danilo; Boughattas, Naceur

    2013-01-01

    This study investigates whether the essential oil prepared from Carum carvi seeds exhibits antiulcerogenic activity. Its volatile oil was obtained by supercritical fluid extraction (SFE) and by hydrodistillation. The essential oils were analysed by GC-MS to monitor their composition. The chemical analysis revealed that the essential oils extracted under SFE conditions had high carvone and limonene contents. The antiulcerogenic activity was evaluated by the HCl/ethanol method, which causes injury to the gastric mucosa. Three treated groups received the essential oil (100-300 mg/kg). The reference group received omeprazole (30 mg/kg) and the control group received NaCl. After 30 min, all groups were treated with HCl/EtOH for gastric ulcer induction. The results show C. carvi essential oil enhanced a significant inhibition of 47%, 81% and 88%, respectively, for three doses of essential oil used, which was similar to that induced by omeprazole (95%) (p < 0.005).

  7. How a Drug Shortage Contributed to a Medication Error Leading to Baclofen Toxicity in an Infant.

    Science.gov (United States)

    Lau, Bonnie; Khazanie, Uma; Rowe, Emily; Fauman, Karen

    2016-01-01

    We report the case of a 4-month-old girl who developed encephalopathy, seizures, and respiratory compromise as a result of baclofen toxicity. After some investigation, the accidental ingestion of baclofen was caused by an error in compounding the patient's prescribed omeprazole with baclofen rather than sodium bicarbonate at a retail pharmacy. This error occurred because these two drugs, which were available as powders, were located side by side on the pharmacy shelf. The pharmacist further reported that their normal practice was to use injectable sodium bicarbonate rather than powder to compound an omeprazole suspension; however, the injectable form was not available due to a national shortage. This report demonstrates how a drug shortage contributed to severe clinical consequences and intensive care hospitalization of a patient. It also highlights the need for system improvement to minimize drug shortages.

  8. Renal Aspects of Peptic Ulcer Pharmacology

    Directory of Open Access Journals (Sweden)

    Daniel Muruve

    1992-01-01

    Full Text Available Medications to treat peptic ulcer disease are used widely and may have adverse effects on renal function. Similarly, renal dysfunction may alter the pharmacokinetics of this diverse group of medications resulting in dosage adjustments. The older agents, antacids and sucralfate, allow absorption of cations (calcium, magnesium and aluminum which may result in toxicity. Newer medications (H2 blockers and omeprazole appear to have fewer side effects and be better tolerated with appropriate dosage adjustments.

  9. Diagnosis of Zollinger-Ellison syndrome: Increasingly difficult

    Institute of Scientific and Technical Information of China (English)

    Tetsuhide Ito; Guillaume Cadiot; Robert T Jensen

    2012-01-01

    In the present paper the increasing difficulty of diagnosis of Zollinger-Ellison syndrome (ZES) due to issues raised in two recent papers is discussed.These issues involve the difficulty and need to withdraw patients suspected of ZES from treatment with Proton Pump Inhibitors (omeprazole,esomeprazole,lansoprazole,rabeprazole,pantoprazole) and the unreliability of many gastrin radioimmunoassays.The clinical context of each of these important issues is reviewed and the conclusions in these articles commented from the perspective of clinical management.

  10. Synthesis and antiulcer activity of 2-[5-substituted-1--benzo(d) imidazol-2-yl sulfinyl]methyl-3-substituted quinazoline-4-(3) ones

    Indian Academy of Sciences (India)

    Avinash Patil; Swastika Ganguly; Sanjay Surana

    2010-05-01

    2-[5-substituted-1--benzo(d)imidazol-2-yl sulfinyl]methyl-3-substituted quinazoline-4-(3)-one derivatives were synthesized and tested for antiulcer activity against pylorus ligation-induced, aspirin induced and ethanol induced ulcer in rat model. All the synthesized compounds were characterized by using IR, MS and 1H NMR spectral and elemental analysis. The compounds were scramed for their antiulcer activity: compounds 5k and 5n showed higher activity than omeprazole used as standard.

  11. Proton pump inhibitors are not the key for therapying non-steroidal anti-inflammatory drugs-induced small intestinal injury.

    Science.gov (United States)

    Zhang, Shuo; Chao, Guan-qun; Lu, Bin

    2013-10-01

    The ability of non-steroidal anti-inflammatory drugs (NSAIDs) to injure the small intestine has been well established in humans and animals. Proton pump inhibitors (PPIs) are frequently prescribed to reduce gastric and duodenal injury caused in high-risk patients taking NSAIDs. However, scarce information is available concerning the effects of PPIs on intestinal damage induced by NSAIDs, and the suppression of gastric acid secretion by PPIs is hard to provide any protection against the damage caused by NSAIDs in the small intestine. The present study was designed to examine the effects of intragastric treatment of two PPIs widely used in clinical practice, namely omeprazole and pantoprazole, on the intestinal damage induced by administration of diclofenac in rat. Male SD rats were treated with omeprazole or pantoprazole for 9 days, with concomitant treatment with anti-inflammatory doses of diclofenac on the final 5 days. The anatomical lesion, villous height, the thickness, and the section area of small intestine were quantitatively analyzed. The change of ultrastructural organization was observed. Endotoxin level in blood was measured by photometry. Epidermal growth factor was observed by immunohistochemistry. Omeprazole and pantoprazole didn't decrease the macroscopic and histologic damage induced by diclofenac in the rat's small intestine. In the two PPI groups, villous height was (89.6 ± 11.8 and 92.6 ± 19.3 μm) lower than which of the control group (P thickness became thinning, and the section area became small. LPS levels in the portal blood of omeprazole and pantoprazole were (4.36 ± 1.26 and 4.25 ± 1.17 EU/ml), significantly higher than in controls (P small intestine from the damage induced by diclofenac in the conscious rat. PPIs cannot repair NSAID-induced intestinal damage at least in part because of significant lesion in mechanical barrier function and reduction in epidermal growth factor.

  12. Effects of an acidic beverage (Coca-Cola) on absorption of ketoconazole.

    Science.gov (United States)

    Chin, T W; Loeb, M; Fong, I W

    1995-08-01

    Absorption of ketoconazole is impaired in patients with achlorhydria. The purpose of this study was to determine the effectiveness of a palatable acidic beverage (Coca-Cola Classic, pH 2.5) in improving the absorption of ketoconazole in the presence of drug-induced achlorhydria. A prospective, randomized, three-way crossover design with a 1-week wash-out period between each treatment was employed. Nine healthy nonsmoking, nonobese volunteers between 22 and 41 years old were studied. Each subject was randomized to receive three treatments: (A) ketoconazole 200-mg tablet with water (control), (B) omeprazole (60 mg) followed by ketoconazole (200 mg) taken with water, and (C) omeprazole (60 mg) followed by ketoconazole (200 mg) taken with 240 ml of Coca-Cola Classic. The pH values of gastric aspirates were checked after omeprazole was administered to confirm attainment of a pH of > 6. Multiple serum samples were obtained for measurements of ketoconazole concentrations by high-pressure liquid chromatography. The mean area under the ketoconazole concentration-time curve from zero to infinity for the control treatment (17.9 +/- 13.1 mg.h/liter) was significantly greater than that for treatment B (3.5 +/- 5.1 mg.h/liter; 16.6% +/- 15.0% of control). The mean peak concentration was highest for the control treatment (4.1 +/- 1.9 micrograms/ml), for which the mean peak concentration showed a significant increase over that for treatment B. The absorption of ketoconazole was reduced in the presence of omeprazole-induced achlorhydria. However, drug absorption was significantly increased, to approximately 65% of the mean for the control treatment, when the drug was taken with an acidic beverage, such as Coca-Cola.

  13. Do proton pump inhibitors decrease calcium absorption?

    Science.gov (United States)

    Hansen, Karen E; Jones, Andrea N; Lindstrom, Mary J; Davis, Lisa A; Ziegler, Toni E; Penniston, Kristina L; Alvig, Amy L; Shafer, Martin M

    2010-12-01

    Proton pump inhibitors (PPIs) increase osteoporotic fracture risk presumably via hypochlorhydria and consequent reduced fractional calcium absorption (FCA). Existing studies provide conflicting information regarding the direct effects of PPIs on FCA. We evaluated the effect of PPI therapy on FCA. We recruited women at least 5 years past menopause who were not taking acid suppressants. Participants underwent three 24-hour inpatient FCA studies using the dual stable isotope method. Two FCA studies were performed 1 month apart to establish baseline calcium absorption. The third study occurred after taking omeprazole (40 mg/day) for 30 days. Each participant consumed the same foods during all FCA studies; study meals replicated subjects' dietary habits based on 7-day diet diaries. Twenty-one postmenopausal women ages 58 ± 7 years (mean ± SD) completed all study visits. Seventeen women were white, and 2 each were black and Hispanic. FCA (mean ± SD) was 20% ± 10% at visit 1, 18% ± 10% at visit 2, and 23% ± 10% following 30 ± 3 days of daily omeprazole (p = .07, ANOVA). Multiple linear regression revealed that age, gastric pH, serum omeprazole levels, adherence to omeprazole, and 25-hydroxyvitamin D levels were unrelated to changes in FCA between study visits 2 and 3. The 1,25-dihydroxyvitamin D(3) level at visit 2 was the only variable (p = .049) associated with the change in FCA between visits 2 and 3. PPI-associated hypochlorhydria does not decrease FCA following 30 days of continuous use. Future studies should focus on identifying mechanisms by which PPIs increase the risk of osteoporotic fracture.

  14. [Feeding disorders, ALTE syndrome, Sandifer syndrome and gastroesophageal reflux disease in the course of food hypersensitivity in 8-month old infant].

    Science.gov (United States)

    Iwańczak, Barbara; Mowszet, Krystyna; Iwańczak, Franciszek

    2010-07-01

    This paper describes the occurrence of feeding disorders, atopic dermatitis, life-threatening symptoms, Sandifer syndrome, and gastroesophageal reflux disease in 8-month old infant in the course of food hypersensitivity. Used in the treatment of cow's milk protein hydrolysates with a considerable degree of hydrolysis, omeprazole, Cisapride. It was not until the introduction of elemental diet based on free amino acids resulted in the withdrawal of life-threatening child's symptoms.

  15. Conflicting results between randomized trials and observational studies on the impact of proton pump inhibitors on cardiovascular events when coadministered with dual antiplatelet therapy: systematic review.

    Science.gov (United States)

    Melloni, Chiara; Washam, Jeffrey B; Jones, W Schuyler; Halim, Sharif A; Hasselblad, Victor; Mayer, Stephanie B; Heidenfelder, Brooke L; Dolor, Rowena J

    2015-01-01

    Discordant results have been reported on the effects of concomitant use of proton pump inhibitors (PPIs) and dual antiplatelet therapy (DAPT) for cardiovascular outcomes. We conducted a systematic review comparing the effectiveness and safety of concomitant use of PPIs and DAPT in the postdischarge treatment of unstable angina/non-ST-segment-elevation myocardial infarction patients. We searched for clinical studies in MEDLINE, EMBASE, and the Cochrane Database of Systematic Reviews, from 1995 to 2012. Reviewers screened and extracted data, assessed applicability and quality, and graded the strength of evidence. We performed meta-analyses of direct comparisons when outcomes and follow-up periods were comparable. Thirty-five studies were eligible. Five (4 randomized controlled trials and 1 observational) assessed the effect of omeprazole when added to DAPT; the other 30 (observational) assessed the effect of PPIs as a class when compared with no PPIs. Random-effects meta-analyses of the studies assessing PPIs as a class consistently reported higher event rates in patients receiving PPIs for various clinical outcomes at 1 year (composite ischemic end points, all-cause mortality, nonfatal MI, stroke, revascularization, and stent thrombosis). However, the results from randomized controlled trials evaluating omeprazole compared with placebo showed no difference in ischemic outcomes, despite a reduction in upper gastrointestinal bleeding with omeprazole. Large, well-conducted observational studies of PPIs and randomized controlled trials of omeprazole seem to provide conflicting results for the effect of PPIs on cardiovascular outcomes when coadministered with DAPT. Prospective trials that directly compare pharmacodynamic parameters and clinical events among specific PPI agents in patients with unstable angina/non-ST-segment-elevation myocardial infarction treated with DAPT are warranted. © 2015 American Heart Association, Inc.

  16. 奥美拉唑的临床应用

    Institute of Scientific and Technical Information of China (English)

    赵延斌

    2000-01-01

    @@ 奥美拉唑(omeprazole,OPZ)系苯并咪唑类质子泵抑制剂(PPI).因其对基础胃酸和由组胺、五肽胃泌素、二丁基环腺酸、胆碱及食物引起的胃酸形成与分泌有强力持久的抑制作用,而被临床广泛应用.

  17. 奥美拉唑的临床应用和不良反应

    Institute of Scientific and Technical Information of China (English)

    张鲜利; 佟灵

    2007-01-01

    奥美拉唑(omeprazole,以下简称为OME)系第一代苯并咪唑类质子泵抑制剂,具有强烈抑制胃酸分泌及胃黏膜修复的作用。为治疗消化性溃疡的首选药。本文介绍其临床应用和不良反应。

  18. ЭФФЕКТИВНОСТЬ ИНГИБИТОРОВ ПРОТОННОЙ ПОМПЫ В ТЕРАПИИ ГАСТРОЭЗОФАГЕАЛЬНОЙ РЕФЛЮКСНОЙ БОЛЕЗНИ

    Directory of Open Access Journals (Sweden)

    А. А. Яковлев

    2013-01-01

    Full Text Available Authors provide results of their own clinical experience of treatment patients with gastro-esophageal reflux disease. Authors use two types of treatment (both for 12 weeks with inhibitors of proton pomp: in standard and high doses of omeprazole and pantoprazole. Design of trail was prospective, 76-weeks of follow up. End points: frequency of relapses as an integral indication of effectiveness of basic treatment.

  19. Clinical relevance of clopidogrel-proton pump inhibitors interaction

    Institute of Scientific and Technical Information of China (English)

    Stella; D; Bouziana; Konstantinos; Tziomalos

    2015-01-01

    Clopidogrel is a widely used antiplatelet agent for the secondary prevention of cardiovascular events in patients with stable coronary heart disease, acute coronary syndromes and ischemic stroke. Even though clopidogrel is safer than aspirin in terms of risk for gastrointestinal(GI) bleeding, the elderly, and patients with a history of prior GI bleeding, with Helicobacter pylori infection or those who are also treated with aspirin, anticoagulants, corticosteroids or nonsteroidal antiinflammatory drugs are at high risk for GI complications when treated with clopidogrel. Accordingly, proton pump inhibitors are frequently administered in combination with clopidogrel to reduce the risk for GI bleeding. Nevertheless, pharmacodynamic studies suggest that omeprazole might attenuate the antiplatelet effect of clopidogrel. However, in observational studies, this interaction does not appear to translate into increased cardiovascular risk in patients treated with this combination. Moreover, in the only randomized, double-blind study that assessed the cardiovascular implications of combining clopidogrel and omeprazole, patients treated with clopidogrel/omeprazole combination had reduced risk for GI events and similar risk for cardiovascular events than patients treated with clopidogrel and placebo. However, the premature interruption of the study and the lack of power analysis in terms of the cardiovascular endpoint do not allow definite conclusions regarding the cardiovascular safety of clopidogrel/omeprazole combination. Other proton pump inhibitors do not appear to interact with clopidogrel. Nevertheless, given the limitations of existing observational and interventional studies, the decision to administer proton pump inhibitors to patients treated with clopidogrel should be individualized based on the patient’s bleeding and cardiovascular risk.

  20. Nebivolol prevents indomethacin-induced gastric ulcer in rats.

    Science.gov (United States)

    El-Ashmawy, Nahla E; Khedr, Eman G; El-Bahrawy, Hoda A; Selim, Hend M

    2016-07-01

    Gastric ulcer is a very common gastrointestinal disease that may lead to dangerous complications and even death. This study was conducted to evaluate the prophylactic effect of nebivolol against indomethacin [INDO]-induced gastric ulcer. Male Wistar rats were divided into four groups: normal control, ulcer control (INDO only), omeprazole before INDO and nebivolol before INDO. Each rat to receive nebivolol and omeprazole was given the agent orally (by gavage) daily for 10 days prior to induction of ulcer by oral dosing with INDO. Four hours after INDO treatment, all rats were euthanized and their stomachs obtained for measures of gastric acidity, oxidative stress and inflammatory markers, as well as cytoprotective mediators. The results showed that a single oral dose of INDO (100 mg/kg) induced gastric acidity, an ulcer index of 2900 and significantly increased levels of gastric tumor necrosis factor (TNF)-α and malondialdehyde (MDA) and significantly decreased levels of gastric prostaglandin E2 (PGE2), glutathione (GSH) and nitric oxide (NO), compared to in normal control counterpart stomachs. Giving nebivolol before INDO corrected the gastric acidity and resulted in a significant increase in GSH, PGE2 and NO and a significant decrease in TNFα and MDA gastric levels, compared to ulcer control values. Results obtained with nebivolol were comparable to those with omeprazole; the preventive index in the nebivolol group was 90.7% compared to 94.5% in rats in the omeprazole group. These studies showed that nebivolol provided a valuable role in preventing gastric ulcers induced by INDO and provided a promise for potentially protecting hypertensive patients from experiencing gastric ulcer. Thus, it is possible that, pending further studies, nebivolol could be used for pre-exposure prophylaxis from gastric ulcer in these patients.

  1. Gastroprotective effect of garlic in indomethacin induced gastric ulcer in rats.

    Science.gov (United States)

    El-Ashmawy, Nahla E; Khedr, Eman G; El-Bahrawy, Hoda A; Selim, Hend M

    2016-01-01

    Garlic, in its natural plant state, has a great history in ancient medicine as a remedy for many diseases. In our study, the gastroprotective effect of aged garlic extract (AGE) and the possible underlying mechanisms were investigated in an experimental model of indomethacin-induced gastric ulcer. Male Wistar rats were divided into four groups: (normal control, n = 20), ulcer control (indomethacin group, n = 20), (omeprazole group, n = 30) and (garlic group, n = 20). Each dose of garlic and omeprazole was given to rats orally daily for 10 consecutive days before induction of ulcer by indomethacin. Indomethacin was given as a single oral dose (100 mg/kg). Four hours later after indomethacin treatment, the rats were sacrificed and gastric tissue was obtained for histopathological examination, calculation of ulcer index and measurement of oxidative stress markers as well as gastroprotective mediators. The results showed that indomethacin induced gastric ulcer (ulcer index = 2900), was associated with a significant increase of tumor necrosis factor-alpha and malondialdehyde, and significant decrease of the gastroprotective mediators prostaglandin E2, glutathione (GSH) and nitric oxide (NO) compared with normal control. Pretreatment with AGE produced comparable results with those obtained in the omeprazole group; the preventive index in the AGE group was 83.4% compared with 94.5% in the omeprazole group. The prophylactic role of AGE in indomethacin-induced ulcer was, in part, mediated by decreasing oxidative stress and increasing gastric level of PGE2, GSH, and NO. AGE corrected the histopathological abnormalities in gastric tissue and proved a promising gastroprotective role in gastric ulcer. Copyright © 2016 Elsevier Inc. All rights reserved.

  2. How a Drug Shortage Contributed to a Medication Error Leading to Baclofen Toxicity in an Infant

    OpenAIRE

    Lau, Bonnie; Khazanie, Uma; Rowe, Emily; Fauman, Karen

    2016-01-01

    We report the case of a 4-month-old girl who developed encephalopathy, seizures, and respiratory compromise as a result of baclofen toxicity. After some investigation, the accidental ingestion of baclofen was caused by an error in compounding the patient's prescribed omeprazole with baclofen rather than sodium bicarbonate at a retail pharmacy. This error occurred because these two drugs, which were available as powders, were located side by side on the pharmacy shelf. The pharmacist further r...

  3. [ROLES OF CONSTITUTIVE SYNTHASES OF NITRIC OXIDE IN THE REGULATION OF GASTRIC BICARBONATE SECRETION INDUCED BY MILD IRRITATION OF THE MUCOSA].

    Science.gov (United States)

    Zolotarev, V A; Andreeva, Yu V; Vershinina, E A; Kropycheva, R P

    2015-04-01

    Roles of isoforms of constitutive synthase of nitric oxide, neuronal or endothelial (nNOS or eNOS), in control of gastric bicarbonate secretion induced by mild irritation of the gastric mucosa was assessed at the normoacid state or after blockade of gastric acid secretion with omeprazole. In anesthetized rats, the concentration of HCO3- in luminal perfusate was calculated basing on measurements of pH/PCO2. Mucosal irritation during 20 min with acidic hypertonic solution (1 M NaCl, pH 2.0) caused marked and omeprazole-independent increase of HCO-secretion. Selective blocker ofnNOS in vivo 7-nitroindazole (7-NI), and the nonselective blocker ofnNOS and eNOS, N(G)-nitro-L-arginine (L-NNA), were applied either intravenously (10 mg/kg), or locally via retrograde injection into the splenic artery (1 mg/kg). At the normo-acid state, the irritation-induced secretion of was suppressed by 7-NI, but was not affected by L-NNA. After administration of omeprazole, both 7-NI and L-NNA equally inhibited HCO3- output. The effect of 7-NI (but not L-NNA) was abolished by cyclooxygenase (COX) inhibitor, indomethacin, which by itself suppressed irritation-induced secretion of HCO3-. Additionally, bicarbonate output was substantially reduced by the blocker of soluble guanylate cyclase (GC), methylene blue. We conclude that irritation-induced secretion of HCO3- is largely mediated by intramural nNOS and depends on GC-COX interaction. As it was theoretically estimated, eNOS activity caused a reduction of HCO3- output in the normo-acid stomach. Omeprazole abolished the effect of eNOS.

  4. The inhibition of monoamine oxidase by esomeprazole

    OpenAIRE

    2013-01-01

    Virtual screening of a library of drugs has suggested that esomeprazole, the S-enantiomer of omeprazole, may possess binding affinities for the active sites of the monoamine oxidase (MAO) A and B enzymes. Based on this finding, the current study examines the MAO inhibitory properties of esomeprazole. Using recombinant human MAO-A and MAO-B, IC50 values for the inhibition of these enzymes by esomeprazole were experimentally determined. To examine the reversibility of MAO inhibition by esomepra...

  5. Management of Nonsteroidal Anti-Inflammatory Drug-Induced Gastroduodenal Disease by Acid Suppression

    Directory of Open Access Journals (Sweden)

    R Lad

    1999-01-01

    Full Text Available One major cause of peptic ulceration is the use of nonsteroidal anti-inflammatory drugs (NSAIDs. The precise mechanisms through which NSAIDs cause peptic ulceration are unknown, but the discovery that they reduce the production of ‘cytoprotective’ prostaglandins led to the hypothesis that coadministration of exogenous prostaglandins heals and prevents NSAID-induced gastroduodenal ulcers and other mucosal lesions. Studies using high doses of misoprostol have shown that it does have a protective effect; however, gastrointestinal intolerance of this prostaglandin E2 analogue is common. Early indications that acid suppression was effective in the management of NSAID-related peptic ulcers came from studies showing that gastric ulcers could be healed by omeprazole in patients who continued to take NSAIDs. Other studies suggested that acid suppression reduces the incidence of mucosal lesions but that standard dose ranitidine protects only against duodenal lesions. Subsequent studies reported that higher dose H2 receptor antagonist therapy can protect against both gastric and duodenal ulcers during continued NSAID therapy. An ideal therapeutic strategy would heal NSAID-related ulcers and prevent the development of new NSAID-related lesions and complications in patients who are unable to discontinue NSAID therapy. A number of recent studies indicate that effective acid-suppressive treatment with the proton pump inhibitor omeprazole can achieve these aims. Overall, data from recent studies show that acid suppression with the proton pump inhibitor omeprazole at a dose of 20 mg daily is the most effective means of healing NSAID-associated gastroduodenal lesions and that it is the most effective prophylactic therapy. In the long run, the role of omeprazole will have to be evaluated with respect to its cost effectiveness compared with other strategies and with respect to the development of less damaging NSAIDs.

  6. [Economic evaluation of the use of diclofenac/misoprostol in the treatment of osteoarticular diseases].

    Science.gov (United States)

    Soto Alvarez, J

    2000-09-01

    To carry out a economic evaluation of diclofenac/misoprostol in the treatment of rheumatoid arthritis and osteoartritis when comparing with diclofenac alone, diclofenac + omeprazol, and diclofenac + ranitidine. Cost effectiveness analysis using a decision analytic model, where the effectiveness unit was defined as the patient free of gastro-intestinal toxicity. The effectiveness data of the four alternatives under evaluation have been obtaining from published clinical trials. In this analysis only direct medical costs have been included without incorporating indirect costs or intangible costs. The perspective chosen has been a primary care area and the time horizon 6 months. All costs are expressed in monetary units of 1998. The cost/effectiveness ratio obtained with diclofenac/misoprostol has been a 37% lower compared with diclofenac alone (42,238 vs 67,214 ptas), a 39% compared with diclofenac + omeprazol (42,238 vs 69,058 ptas) and a 50% compared with diclofenac + ranitidine (42,238 vs 85,198 ptas). The sensitivity analysis performed has shown that diclofenac/misoprostol is the therapeutic alternative more efficient even when most influential variables are modified. Diclofenac/misoprostol has demonstrated to be an alternative with a better cost/effectiveness ratio, and therefore more efficient than diclofenac alone or the concomitant use of diclofenac either with omeprazol or ranitidine. The routinary use of this association will save important resources to the National Health Service.

  7. Clinical and pharmacoeconomic profile of esomeprazole in acid-related diseases

    Directory of Open Access Journals (Sweden)

    Orietta Zaniolo

    2006-09-01

    Full Text Available Protonic pump inhibitors (PPIs are the most prescribed drugs for acute and maintenance therapy of gastroesophageal reflux disease, H. pylori-eradication (in association with antibacterial therapy, for ulcers prevention and cure and, recently, for prevention of NSAIDs-induced gastropathy. The high prevalence of these acid-related disorders induces a large consumption of PPIs; actually, they are the first drug class in terms of National Health Service pharmaceutical expenditure. This widespread and gradually increasing use enforces the need of a rational assessment of their impact on health care resources. This paper provides an updated profile of esomeprazole, the first PPI developed as a pure isomer, which property involves an advantageous metabolism, resulting in enhanced delivery to the proton pump compared with racemic omeprazole. Several studies showed that the success rate for healing reflux esophagitis is greater for esomeprazole than for omeprazole and some other PPIs. According to an Italian pharmacoeconomic model, esomeprazole therapy for erosive esophagitis is associated with higher benefits and lower costs as compared to omeprazole and pantoprazole. For long-term management of non-erosive gastroesophageal reflux disease, on-demand approach with esomeprazole shows clinical outcomes similar to daily treatment regimens, with substantial cost-saving. Furthermore, esomeprazole is the only PPI approved for 1-week triple therapy for both the eradication and the healing of H. pylori-associated duodenal ulcer, while the other PPIs registered the indication for H. pylori-eradication and, separately, a dosing scheme for ulcer healing (independently from etiology.

  8. Proton pump inhibitor-amoxicillin-clarithromycin versus proton pump inhibitor-amoxicillin-metronidazole as first-line Helicobacter pylori eradication therapy.

    Science.gov (United States)

    Nishizawa, Toshihiro; Suzuki, Hidekazu; Suzuki, Masayuki; Takahashi, Masahiko; Hibi, Toshifumi

    2012-09-01

    The aim of this study was to compare the efficacy and tolerability of the first-line Helicobacter pylori (H. pylori) eradication regimen composed of proton pump inhibitor, clarithromycin, and amoxicillin, with those of a regimen composed of proton pump inhibitor, metronidazole, and amoxicillin. Data of patients, who were administered the first-line H. pylori eradication regimen at Tokyo Medical Center between 2008 and 2011, were reviewed. All patients had H. pylori gastritis without peptic ulcer disease. The 7-day triple regimen composed of lansoprazole, clarithromycin, and amoxicillin was administered to 55 patients, and that composed of omeprazole, metronidazole, and amoxicillin was administered to 55 patients. Intention-to-treat and per-protocol eradication rates were 74.5 and 80.4%, respectively, for the regimen of lansoprazole, clarithromycin, and amoxicillin, whereas the corresponding rates were 96.4 and 100%, respectively, for the regimen of omeprazole, metronidazole, and amoxicillin. In conclusion, first-line H. pylori eradication therapy composed of omeprazole, metronidazole, and amoxicillin was significantly more effective than that composed of lansoprazole, clarithromycin, and amoxicillin, without differences in tolerability.

  9. Comparison of Ciprofloxacin-Based Triple Therapy with Conventional Triple Regimen for Helicobacter pylori Eradication in Children.

    Science.gov (United States)

    Farahmand, Fatemeh; Mohammadi, Tayebeh; Najafi, Mehri; Fallahi, Gholamhosein; Khodadad, Ahmad; Motamed, Farzaneh; Mahdi Marashi, Sayed; Shoaran, Maryam; Nabavizadeh Rafsanjani, Raheleh

    2016-06-01

    Helicobacter pylori infection is a prevalent disease among Iranian children. The purpose of this study was to compare the effect of ciprofloxacin and furazolidone on eradicating helicobacter pylori in Iranian children in combination with amoxicillin and omeprazole. In this cohort study, helicobacter pylori infection was confirmed by gastroscopy, rapid urease test or pathologic assessments. A total of 66 children were randomly enrolled; based on the random number table, and were divided into two groups; first, a combination regimen consisting of ciprofloxacin, amoxicillin, and omeprazole; second, a three-medication regimen consisting of amoxicillin, furazolidone, and omeprazole. The effect of both medical regimens on the successful eradication of helicobacter pylori infection was assessed and compared. Chi-square test was used for evaluating the association between quantitative variables. All comparisons were made at the significance of Phelicobacter pylori infection was reported 87.9% (29/33) in the first group (CAO) and 60.6% (20.33) in the second group (FAO) (P=0.011). It appears that a major advantage of our proposed regimen over others is a lack of wide use of fluoroquinolones for treating children's diseases. Given FDA's recommendation about the possibility of prescribing ciprofloxacin for infected patients with multidrug resistance, we can use the regimen proposed in this study in patients with resistance to standard treatments.

  10. Effect of long-term proton pump inhibitor therapy and healing effect of irsogladine on nonsteroidal anti-inflammatory drug-induced small-intestinal lesions in healthy volunteers.

    Science.gov (United States)

    Kojima, Yuichi; Takeuchi, Toshihisa; Ota, Kazuhiro; Harada, Satoshi; Edogawa, Shoko; Narabayashi, Ken; Nouda, Sadaharu; Okada, Toshihiko; Kakimoto, Kazuki; Kuramoto, Takanori; Inoue, Takuya; Higuchi, Kazuhide

    2015-07-01

    This study assessed time-course changes of the small intestinal lesions during long-term treatment with diclofenac sodium plus omeprazole and the effects of irsogladine on such lesions. Thirty two healthy volunteers were treated with diclofenac sodium (75 mg/day) plus omeprazole (10 mg/day) for 6 weeks, with irsogladine (4 mg/day) added from weeks 6 to 10 (Group A) or with diclofenac sodium plus irsogladine for 6 weeks (Group B). Five volunteers received diclofenac sodium plus omeprazole for 10 weeks (Group C). Subjects underwent capsule endoscopy at each time. In Group A, the number of lesions remarkably increased at week 2, but the worse was not found at week 6 compared with week 2, whereas no exacerbation of lesions was observed in Group B. Additional treatment with irsogladine from weeks 6 to 10 in Group A significantly decreased the number of lesions at weeks 10 compared with Group C. In Group C, no significant change in lesions was observed since weeks 2. In conclusions, a PPI did not prevent the occurrence of small intestinal damage. However such lesions were not aggravated since weeks 2. These suggested mucosal adaptation may occur in the small intestine. Irsogladine was effective in both preventing and healing such lesions.

  11. Review article: pharmacokinetic concerns in the selection of anti-ulcer therapy.

    Science.gov (United States)

    Lew, E A

    1999-10-01

    Rabeprazole is a new, highly potent proton pump inhibitor (PPI) being introduced for the treatment of disorders of gastric acid hypersecretion. Rabeprazole joins other drugs in this class, such as omeprazole, pantoprazole, and lansoprazole, which share a common mechanism of action. Each of these drugs is a substituted benzimidazole, which inhibits activity of the H+, K+ -ATPase located on the apical surface of parietal cells, thereby preventing the secretion of gastric acid. As a result of structural and functional similarities, the PPIs share many pharmacokinetic features. They have comparable rates of absorption, maximum plasma concentrations, and total drug absorptions resulting in similar bioavailability after single-dose administration. With multiple dosing, rabeprazole differs from omeprazole in that its pharmacokinetic profile does not change significantly over the course of therapy. All the PPIs are metabolized rapidly, resulting in short half-lives. However, their duration of activity is much longer, due to the way in which they bind to H+, K+ -ATPase. All are metabolized by hepatic cytochrome P450 enzymes, although only omeprazole has demonstrated significant interactions with other drugs metabolized by this pathway. Rabeprazole, which has a low potential for interacting with drugs metabolized by cytochrome P450, does interfere with the absorption of digoxin and ketoconazole because of its antisecretory effects. The pharmacokinetics of rabeprazole are altered slightly in elderly subjects and in patients with renal and moderate hepatic disease. However, the pharmacokinetic findings suggest that no dosage adjustment is required in these special populations.

  12. Clinical evaluation of four one-week triple therapy regimens in eradicating Helicobacter pyloriinfection

    Institute of Scientific and Technical Information of China (English)

    Chuan-Yong Guo; Yun-Bin Wu; Heng-Lu Liu; Jian-Ye Wu; Min-Zhang Zhong

    2004-01-01

    AIM: TO evaluate clinical efficacy of four one-week triple therapies in eradicating Helicobacter pylori infection.METHODS: In this clinical trial, 132 patients with duodenal ulcer and chronic gastritis were randomly divided into four 20 mg+ amoxicillin 1 000 mg + clarithromycin 250 mg), OFC (omeprazole 20 mg + furazolidone 100 mg + clarithromycin 250 mg), OFA (omeprazole 20 mg + furazolidone 100 mg + amoxicillin 1000 mg) and OMC (omeprazole 20 mg +metronidazole 200 mg + cladthromycin 250 mg), respectively.Each drug was taken twice daily for one week. The 13C urea breath test was carried out 4-8 weeks after treatment to determine the success of H pylori eradication.RESULTS: A total of 127 patients completed the treatment.The eradication rate for H pylori infection was 90.3%,90.9%, 70.9% and 65.6%, respectively in OAC, OFC OMC and OFA groups.CONCLUSION: A high eradication rate can be achieved with one-week OAC or OFC triple therapy. Thus, oneweek triple therapies with OAC and OFC are recommended for Chinese patients with duodenal ulcers and chronic gastritis.

  13. Effect of proton pump inhibitors on the secretion of bicarbonates and pepsinogen induced by chemical stimulation of the gastric mucosa.

    Science.gov (United States)

    Zolotarev, V A; Khropycheva, R P

    2013-02-01

    Proton pump inhibitors were shown to affect the sensitivity of the gastric mucosa to chemical agents. This effect is associated with inhibition of proton back-diffusion and increase in the permeability of the gastric epithelium. We studied the effect of omeprazole on gastric secretion of bicarbonates and pepsinogen induced by irritation of the gastric mucosa in narcotized rats with a hypertonic solution of high acidity (500 mM NaCl, pH 2.0). Irritation of the gastric mucosa increased the basal secretion of bicarbonates and potentiated the secretion of HCO3(-)and pepsinogen induced by electrostimulation of the vagus nerve. Omeprazole stimulated the prostaglandin-induced increase in the basal secretion of HCO3(-)and pepsinogen. By contrast, bicarbonate production in response to vagal stimulation was suppressed in the presence of omeprazole. Our results indicate that proton pump blockade has a modulatory effect on gastric secretion of bicarbonates and pepsinogen induced by chemical stimulation of the gastric mucosa.

  14. The caspase-1 inhibitor AC-YVAD-CMK attenuates acute gastric injury in mice: involvement of silencing NLRP3 inflammasome activities.

    Science.gov (United States)

    Zhang, Fang; Wang, Liang; Wang, Jun-jie; Luo, Peng-fei; Wang, Xing-tong; Xia, Zhao-fan

    2016-04-07

    This study evaluated the protective effects of inhibiting caspase-1 activity or gastric acid secretion on acute gastric injury in mice. AC-YVAD-CMK, omeprazole, or vehicle were administered to mice before cold-restraint stress- or ethanol-induced gastric injury. Survival rates and histological evidence of gastric injury of mice pretreated with AC-YVAD-CMK or omeprazole, and exposed to cold-restraint stress, improved significantly relative to the vehicle group. The increased levels of tumour necrosis factor-α, interleukin (IL)-1β, IL-6, and IL-18 following cold-stress injury were decreased by AC-YVAD-CMK, but not omeprazole, pretreatment. The increased expression of CD68 in gastric tissues was inhibited significantly by AC-YVAD-CMK pretreatment. Inhibiting caspase-1 activity in the NLRP3 inflammasome decreased gastric cell apoptosis, and the expression of Bax and cleaved caspase-3. AC-YVAD-CMK pretreatment significantly inhibited cold-restraint stress-induced increases in the expression of phosphorylated IκB-alpha and P38. General anatomy and histological results showed the protective effect of AC-YVAD-CMK on ethanol-induced acute gastric injury. Overall, our results showed that the caspase-1 inhibitor AC-YVAD-CMK protected against acute gastric injury in mice by affecting the NLRP3 inflammasome and attenuating inflammatory processes and apoptosis. This was similar to the mechanism associated with NF-κB and P38 mitogen-activated protein kinase signalling pathways.

  15. Pylera for the eradication of Helicobacter pylori infection.

    LENUS (Irish Health Repository)

    Saleem, Aamir

    2012-02-01

    An ideal antibiotic regimen for Helicobacter pylori should achieve eradication rates of approximately 90%. Current 7-day triple therapy is successful in about two-thirds of patients. A novel treatment is required to achieve higher eradication with minimal induction of bacterial resistance. The aim of this article is to evaluate the safety and efficacy of a single triple capsule (Pylera) containing bismuth, metronidazole and tetracycline, given with omeprazole for the eradication of H. pylori infection. Extensive literature searches were conducted using PubMed data from 1982 to 2007. This search included headings of H. pylori, bismuth and eradication therapy. The triple capsule Pylera, when given with omeprazole, achieved eradication rates ranging between 84 and 97%. Eradication rates were similar for clarithromycin- and metronidazole-resistant strains. Eradication rates with an omeprazole, bismuth, metronidazole and tetracycline regimen appeared comparable for metronidazole-resistant and -sensitive strains. This effect is not seen with the use of triple therapy in cases of clarithromycin resistance. Clinical trials did not report any serious side effects from bismuth-based regimens and compliance was similar to standard triple therapy. Bismuth-based triple therapy using Pylera is a simplified, effective and well-tolerated regimen achieving cure rates of above 90%.

  16. Evolutions in both co-payment and generic market share for common medication in the Belgian reference pricing system.

    Science.gov (United States)

    Fraeyman, Jessica; Verbelen, Moira; Hens, Niel; Van Hal, Guido; De Loof, Hans; Beutels, Philippe

    2013-10-01

    In Belgium, a co-insurance system is applied in which patients pay a portion of the cost for medicines, called co-payment. Co-payment is intended to make pharmaceutical consumers more responsible, increase solidarity, and avoid or reduce moral hazards. Our objective was to study the possible influence of co-payment on sales volume and generic market share in two commonly used medicine groups: cholesterol-lowering medication [statins (HMG-CoA reductase inhibitors) and fibrates] and acid-blocking agents (proton pump inhibitors and histamine H2 receptor antagonists). The data were extracted from the Pharmanet database, which covers pharmaceutical consumption in all Belgian ambulatory pharmacies. First, the proportion of sales volume and costs of generic products were modelled over time for the two medicine groups. Second, we investigated the relation between co-payment and contribution by the national insurance agency using change-point linear mixed models. The change-point analysis suggested several influential events. First, the generic market share in total sales volume was negatively influenced by the abolishment of the distinction in the maximum co-payment level for name brands and generics in 2001. Second, relaxation of the reimbursement conditions for generic omeprazole stimulated generic sales volume in 2004. Finally, an increase in co-payment for generic omeprazole was associated with a significant decrease in omeprazole sales volume in 2005. The observational analysis demonstrated several changes over time. First, the co-payment amounts for name-brand and generic drugs converged in the observed time period for both medicine groups under study. Second, the proportion of co-payment for the total cost of simvastatin and omeprazole increased over time for small packages, and more so for generic than for name-brand products. For omeprazole, both the proportion and the amount of co-payment increased over time. Third, over time the prescription of small packages

  17. Study on the Pharmacokinetics of Combined Medication in Treatment of Rats with Functional Dyspepsia%联合用药治疗大鼠功能性消化不良的药动学研究

    Institute of Scientific and Technical Information of China (English)

    单国冰; 田媛; 黄俊; 黄寅; 张尊建

    2012-01-01

    Objective To investigate the pharmacokinetic interactions after oral administration of mosapride citrate,omeprazole and hydrochloride fluoxetine in treatment of rats with functional dyspesia. Methods Four groups of male SD rats( Ⅰ , Ⅱ , Ⅲ, Ⅳ , n =6 per group) were set in parallel design,the rats were given mosapride citrate, omeprazole, fluoxetine and combination of the three single doses,by intragastric administration. The determination of plasma samples were performed by a HPLC-MS/MS and the pharmacokinetic parameters were estimated(DAS 2.0). Results The Cmax and AUC of mosapride citrate,as well as omeprazole , were significantly increased; the AUC of hydrochlorid fluoxetine were increased, and CL/F of mosapride citrate, omeprazole and hydrochloride fluoxetine was decreased. Conclusion The results of preliminary study showed that there were obvious pharmacokinetic interactions among mosapride citrate,omeprazole and hydrochloride fluoxetine. The dosage of the three drugs was suggested to be reduced appropriately in their combination therapy.%目的 研究枸橼酸莫沙必利、奥美拉唑和盐酸氟西汀联合给药治疗大鼠功能性消化不良的药动学行为变化.方法 4组SD雄性大鼠分别为单药组枸橼酸莫沙必利(Ⅰ)、奥美拉唑(Ⅱ)、盐酸氟西汀(Ⅲ)和联合用药组(Ⅳ).采用HPLC-MS/MS法同时测定大鼠给药后不同时间点的血药浓度(DAS 2.0程序拟合),估算药动学参数.结果 枸橼酸莫沙必利、奥美拉唑与盐酸氟西汀均符合二室模型特征.三药合用时枸橼酸莫沙必利的Cmax和AUC显著增大,CL/F和V/F减小;奥美拉唑的Cmax和AUC显著增大,CL/F减小;盐酸氟西汀AUC增大,CL/F减小.结论 枸橼酸莫沙必利、奥美拉唑和盐酸氟西汀联合应用时存在明显的药代动力学叠加作用,建议临床联合用药时适当减量.

  18. The influence of changes in hospital drug formulary on the prescription of proton pump inhibitors.

    Science.gov (United States)

    Vázquez-Mourelle, Raquel; Carracedo-Martínez, Eduardo

    2017-01-01

    Objetivo: Analizar el impacto de introducir el omeprazol en el formulario del Hospital de Barbanza sobre las prescripciones intrahospitalarias y extrahospitalarias (consultas externas y atención primaria) de todos los Inhibidores de la Bomba de Protones (IBP). Material y métodos: Estudio descriptivo retrospectivo de 36 meses en un hospital de nivel I. Las unidades básicas de trabajo son las dosis-habitantes-día en el ámbito extrahospitalario y las dosis diarias definidas/estancias-día para hospitalización; como medida de eficiencia se utiliza el porcentaje de DDD de omeprazol sobre el resto de IBP. Para el análisis estadístico construimos un modelo de regresión segmentada. Resultados: En consultas externas sufren cambios estadísticamente significativos el pantoprazol y el rabeprazol; el primero, estacionado antes de la intervención, sufre una disminución inmediata; el rabeprazol, en crecimiento antes de la intervención, presenta una posterior tendencia decreciente. En atención primaria se constata un cambio estadísticamente significativo en el pantoprazol, con tendencia decreciente a largo plazo. En hospitalización se observan cambios estadísticamente significativos para el pantoprazol y el omeprazol; el primero con disminución inmediata y tendencia al decrecimiento a largo plazo; el segundo experimenta un aumento inmediato y crecimiento a largo plazo. La evolución del % de omeprazol respecto al total de IBP mostró aumentos en los tres escenarios. Conclusiones: Se observa un cambio hacia una prescripción de IBP más eficiente en todos los ámbitos asistenciales tras la introducción del omeprazol en la guía farmacoterapéutica del hospital. La inclusión de medicamentos eficientes, o la retirada de ineficientes, puede ser una herramienta potencialmente útil para mejorar los perfiles de prescripción.

  19. Eficiencia en la prescripción de medicamentos: impacto de un programa de intercambio terapéutico The efficiency of drug prescription: impact of a therapeutic exchange program

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    Isabel Rosich

    2012-02-01

    Full Text Available Objetivo: Evaluar el impacto de un programa de intercambio terapéutico a omeprazol de los inhibidores de la bomba de protones (IBP. Método: Ensayo comunitario que compara el impacto de un programa de intercambio terapéutico en los equipos de atención primaria de una comarca respecto a la no aplicación en una comarca control. Se incluyó a los pacientes con prescripción de un IBP entre mayo de 2008 y junio de 2009. La intervención consistió en sesiones educativas y facilitar a cada médico (n=68 los pacientes con un IBP que pudiera cambiarse a omeprazol. Se obtuvo información de la historia clínica (IBP prescrito, equipo de atención primaria y de la aplicación de farmacia (coste de la dosis diaria definida de los IBP. A partir del riesgo relativo (RR se comparó el porcentaje de intercambio terapéutico en cada comarca antes y después de la intervención. También se calculó el porcentaje de omeprazol al final de cada periodo de estudio y los cambios en los costes en IBP. Resultados: Hubo más intercambios terapéuticos en el grupo de intervención (RR: 4,2; intervalo de confianza del 95% [IC95%]:3,1-5,8 respecto al control (RR: 1,8; IC95%:1,2-2,6. En el grupo de intervención, el porcentaje de pacientes con omeprazol pasó del 86,2% al 89,3%, y en el control del 84,3% al 84,7%. El coste del grupo IBP disminuyó un 7,6% en el grupo de intervención y aumentó un 2,0% en el control. Conclusiones: El programa de intercambio terapéutico se ha mostrado efectivo. Se trata de una intervención sencilla, capaz de modificar las prescripciones y reducir sus costes.Objective: To assess the impact of substituting proton pump inhibitors (PPI for omeprazole. Method: We performed a community trial of the impact of a therapeutic exchange program in the primary care teams of a region compared with non-implementation in a control region. The study included patients prescribed a PPI between May 2008 and June 2009. The intervention consisted of

  20. Relation between CYP2C19 phenotype and genotype in a group of Brazilian volunteers

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    Rafael Linden

    2009-09-01

    Full Text Available The CYP2C19 gene presents polymorphism affecting the pharmacokinetics of several drugs of clinical importance. The purpose of this study was to investigate the correlation between CYP2C19 genotype and metabolic phenotype in a group of 38 Brazilian volunteers, evaluating the phenotype prediction capacity of the genotyping procedure. For CYP2C19 phenotyping, omeprazole was used as the probe drug, using the hydroxylation metabolic ratio as the phenotypic indicator. Venous blood samples were drawn before and three hours after an oral administration of 20 mg omeprazole. The plasma concentrations of omeprazole and hydroxy-omeprazole were determined by high performance liquid chromatography. The genotyping assay was carried out using a Real-Time-PCR-based assay, identifying the alleles *1 (completely functional, *2, *3 and *4 (null. The phenotyping procedure estimated the presence of 4 poor, 34 extensive and 1 ultra-extensive metabolizer. The genotyping identified 4 poor, 23 extensive and 11 intensive metabolizers. The groups of volunteers classified according to the number of active alleles of CYP2C19 had significant differences in the metabolic ratios of omeprazole hydroxylation. However, volunteers exhibiting the same number of active alleles presented different phenotypes. Therefore, the phenotyping of CYP2C19 is a more promising alternative to dose individualization of CYP2C19 substrate drugs.O gene CYP2C19 apresenta polimorfismo genético, com impacto importante na farmacocinética de diversos fármacos de importância clínica. O objetivo deste estudo foi avaliar a correlação entre genótipo e fenótipo de CYP2C19 em um grupo de 38 voluntários brasileiros, avaliando a capacidade de predição do fenótipo a partir de testes de genotipagem. Para a fenotipagem, utilizou-se omeprazol (OME como fármaco-sonda para CYP2C19, empregando sua razão metabólica de hidroxilação como indicador fenotípico. Amostras de sangue foram coletadas antes e tr

  1. Interaction profile of armodafinil with medications metabolized by cytochrome P450 enzymes 1A2, 3A4 and 2C19 in healthy subjects.

    Science.gov (United States)

    Darwish, Mona; Kirby, Mary; Robertson, Philmore; Hellriegel, Edward T

    2008-01-01

    Armodafinil, a wakefulness-promoting agent, is the pure R-enantiomer of racemic modafinil. The objective of this article is to summarize the results of three clinical drug-interaction studies assessing the potential for drug interactions of armodafinil with agents metabolized by cytochrome P450 (CYP) enzymes 1A2, 3A4 and 2C19. Study 1 evaluated the potential for armodafinil to induce the activity of CYP1A2 using oral caffeine as the probe substrate. Study 2 evaluated the potential for armodafinil to induce gastrointestinal and hepatic CYP3A4 activity using intravenous and oral midazolam as the probe substrate. Study 3 evaluated the potential for armodafinil to inhibit the activity of CYP2C19 using oral omeprazole as the probe substrate. Healthy men and nonpregnant women aged 18-45 years with a body mass index of omeprazole (oral 40 mg) was administered alone or with oral administration of armodafinil 400 mg 2 hours before the omeprazole dose. Pharmacokinetic samples were obtained for caffeine, midazolam and omeprazole for up to 48 hours postdose. The primary pharmacokinetic parameters included the area under the plasma concentration-time curve from time zero to infinity (AUC(infinity)) and the maximum observed drug plasma concentration (C(max)). Safety and tolerability were also assessed. A total of 77 healthy subjects participated in the three studies (study 1, n = 29; study 2, n = 24; study 3, n = 24). Prolonged armodafinil administration had no effect on the C(max) or the AUC of oral caffeine compared with administration of caffeine

  2. Alterações no teste ultra-rápido da urease e no exame anatomopatológico para Helicobacter pylori induzidas por drogas anti-secretoras Changes in ultrarapid urease test and histopathological examination for Helicobacter pylori by antisecretory drugs

    Directory of Open Access Journals (Sweden)

    Lincoln Eduardo Villela Vieira de Castro FERREIRA

    2001-01-01

    Full Text Available Racional - Um dos problemas na avaliação de pacientes dispépticos em instituições públicas é o intervalo de tempo prolongado entre a consulta inicial e a endoscopia digestiva alta, levando à introdução de terapêutica anti-secretora nesse período. Desta forma, os resultados do exame podem não traduzir a condição inicialmente suspeitada. Objetivos - Analisar as alterações no teste ultra-rápido da urease e no exame anatomopatológico para Helicobacter pylori após o uso de drogas anti-secretoras. Casuística e Método - Foram avaliados, de forma prospectiva e duplo-cega, 50 pacientes com queixas dispépticas e diagnóstico endoscópico de úlcera péptica, gastrite, esofagite ou duodenite erosivas e com teste da urease positivo. Os pacientes foram divididos, de forma randomizada, em dois grupos: 25 usaram ranitidina 300 mg/dia e 25, omeprazol 20 mg/dia, durante 7 dias. Antes e após o tratamento, dois fragmentos de biopsia foram obtidos do antro e corpo gástricos, realizando-se o teste ultra-rápido da urease e o exame anatomopatológico para Helicobacter pylori. Resultados - No grupo que usou ranitidina, não se observaram alterações significativas na positividade do teste ultra-rápido da urease e do exame anatomopatológico no antro e corpo gástricos, após 7 dias de medicação. Nos pacientes que utilizaram omeprazol, após tal período, observou-se redução da positividade do teste ultra-rápido da urease e do exame anatomopatológico no antro gástrico, sendo que o mesmo não ocorreu na região do corpo. Conclusão - O omeprazol, utilizado por um período de 7 dias, é capaz de levar a uma negativação do teste ultra-rápido da urease e do exame anatomopatológico para Helicobacter pylori no antro gástrico, devendo ser desaconselhado para pacientes aguardando realização de endoscopia digestiva,Background - One of the major problems when evaluating dyspeptic patients at public hospitals is the large interval between

  3. Dor pós-operatória: combinações analgésicas e eventos adversos Dolor postoperatorio: combinaciones analgésicas y eventos adversos Post operative pain: analgesic combinations and adverse effects

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    Silvia Regina Secoli

    2009-12-01

    Full Text Available O controle da dor e seus eventos adversos são focos de profissionais e gestores das instituições de saúde para obtenção de desfechos assistenciais. O estudo teve como objetivos analisar a prevalência de combinações e interações medicamentosas da terapia analgésica e verificar a associação dessa com os eventos adversos conferidos. Trata-se de estudo descritivo, exploratório e retrospectivo. A amostra foi composta por 260 prontuários de pacientes submetidos a hemorroidectomia, com idade de até 60 anos hígidos. Os resultados mostraram que as associações medicamentosas mais utilizadas foram a dipirona+omeprazol (33,7%, dipirona+cetoprofeno (23,6% e cetoprofeno+lactulose (22,8%. Observou-se que cetoprofeno+ omeprazol (p=0,001 e cetoprofeno+ lactulose (p=0,03 estiveram significativamente relacionados com sangramento. Concluiu-se que, com exceção do cetoprofeno, as outras associações medicamentosas identificadas no estudo se mostraram seguras para serem utilizadas no período pós operatório.El control del dolor y sus eventos adversos se constituyen en el foco de los profesionales y gestores de las instituciones de salud para la obtención de resultados asistenciales. El estudio tuvo como objetivos analizar la prevalencia de combinaciones y interacciones medicamentosas de la terapia analgésica y verificar la asociación de esta con los eventos adversos conferidos. Estudio descriptivo, exploratorio y retrospectivo. La muestra fue compuesta por 260 historias clinicas de pacientes sometidos a hemorroidectomia hasta los 60 años de edad, sanos. Los resultados mostraron que las asociaciones medicamentosas más utilizadas fueron la dipirona y omeprazol (33,7%, dipirona y cetoprofeno (23,6% y cetoprofeno y lactulosa (22,8%. Se observó que el cetoprofeno+omeprazol (p=0,001, cetoprofeno+ lactulosa (p=0,03 estuvieron significativamente relacionados con el sangramiento. Se concluyó que, con excepción del cetoprofeno, las otras

  4. Short-term triple therapy with azithromycin for Helicobacter pylori eradication: Low cost, high compliance, but low efficacy

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    Mattar Rejane

    2008-05-01

    Full Text Available Abstract Background The Brazilian consensus recommends a short-term treatment course with clarithromycin, amoxicillin and proton-pump inhibitor for the eradication of Helicobacter pylori (H. pylori. This treatment course has good efficacy, but cannot be afforded by a large part of the population. Azithromycin, amoxicillin and omeprazole are subsidized, for several aims, by the Brazilian federal government. Therefore, a short-term treatment course that uses these drugs is a low-cost one, but its efficacy regarding the bacterium eradication is yet to be demonstrated. The study's purpose was to verify the efficacy of H. pylori eradication in infected patients who presented peptic ulcer disease, using the association of azithromycin, amoxicillin and omeprazole. Methods Sixty patients with peptic ulcer diagnosed by upper digestive endoscopy and H. pylori infection documented by rapid urease test, histological analysis and urea breath test were treated for six days with a combination of azithromycin 500 mg and omeprazole 20 mg, in a single daily dose, associated with amoxicillin 500 mg 3 times a day. The eradication control was carried out 12 weeks after the treatment by means of the same diagnostic tests. The eradication rates were calculated with 95% confidence interval. Results The eradication rate was 38% per intention to treat and 41% per protocol. Few adverse effects were observed and treatment compliance was high. Conclusion Despite its low cost and high compliance, the low eradication rate does not allow the recommendation of the triple therapy with azithromycin as an adequate treatment for H. pylori infection.

  5. Helicobacter pylori related dyspepsia: prevalence and treatment outcomes at University Kebangsaan Malaysia-Primary Care Centre

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    Abdul Aziz Aznida

    2009-05-01

    Full Text Available Abstract Background Optimum management of dyspepsia in primary care is a debatable subject. Testing for Helicobacter pylori (HP has been recommended in primary care as this strategy will cure most underlying peptic ulcer disease and prevent future gastro duodenal disease. Methods A total of 98 patients completed Modified Glasgow Dyspepsia Severity Score Questionnaire (MGDSSQ at initial presentation before undergoing the 13Carbon Urea Breath Test (UBT for HP. Those with positive UBT received Eradication Therapy with oral Omeprazole 20 mg twice daily, Clarithromycin 500 mg daily and Amoxycillin 500 mg twice daily for one week followed by Omeprazole to be completed for another 4 to 6 weeks. Those with negative UBT received empirical treatment with oral Omeprazole 20 mg twice daily for 4 to 6 weeks. Patients were assessed again using the MGDSSQ at the completion of treatment and one month after stopping treatment. Results The prevalence of dyspepsia at Universiti Kebangsaan Malaysia-Primary Care Centre was 1.12% (124/11037, out of which 23.5% (23/98 was due to HP. Post treatment assessment in both HP (95.7%, 22/23 and non HP-related dyspepsia (86.7%, 65/75 groups showed complete or almost complete resolution of dyspepsia. Only about 4.3% (1/23 in the HP related dyspepsia and 13.3% (10/75 in the non HP group required endoscopy. Conclusion The prevalence of dyspepsia due to HP in this primary care centre was 23.5%. Detection of HP related dyspepsia yielded good treatment outcomes (95.7%.

  6. Management of gastroesophageal reflux disease and erosive esophagitis in pediatric patients: Focus on delayed-release esomeprazole

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    Elizabet V Guimarães

    2010-10-01

    Full Text Available Elizabet V Guimarães, Paula VP Guerra, Francisco J PennaDepartment of Pediatrics, Medical School, Universidade Federal de Minas Gerais, Belo Horizonte, BrazilObjective: To review the literature on the treatment of gastroesophageal reflux disease (GERD with emphasis on proton pump inhibitors (PPIs, particularly on delayed-release esomeprazole, and to identify properties and adverse effects of PPIs observed in the treatment of GERD in children and adolescents.Sources: Electronic search of PubMed/Medline and Cochrane Collaboration databases, and of abstracts on DDW, NASPGHAN, and ESPGHAN. We focused on controlled and randomized studies published since 2000 and identified reviews that presented a consensual position, and directives published within the last 10 years.Main results: PPIs are considered better antisecretory agents than H2-receptor antagonists. Although all PPIs are similar, they are not identical in their pharmacologic properties. For example, the acid-suppressive effect of esomeprazole, the S-isomer of omeprazole, persists for more than 16 hours after administration of the morning dose. Therefore, it can control acidity after night meals better than a single dose of omeprazole. Moreover, the onset of the suppressive effect of esomeprazole is faster. It achieves acid inhibition faster than other PPIs.Conclusion: Currently, the mainstream treatment for GERD in children is a PPI. Although PPIs are safe drugs, effective in healing erosive esophagitis, and in relieving symptoms, studies with esomeprazole have shown that this drug has as powerful an ability to inhibit acid secretion as omeprazole. It also seems that some pharmacologic properties of esomeprazole are actually better for the treatment of GERD.Keywords: gastroesophageal reflux, therapy, child, adolescent.

  7. Gastroprotective activity of Annona muricata leaves against ethanol-induced gastric injury in rats via Hsp70/Bax involvement.

    Science.gov (United States)

    Moghadamtousi, Soheil Zorofchian; Rouhollahi, Elham; Karimian, Hamed; Fadaeinasab, Mehran; Abdulla, Mahmood Ameen; Kadir, Habsah Abdul

    2014-01-01

    The popular fruit tree of Annona muricata L. (Annonaceae), known as soursop and graviola, is a widely distributed plant in Central and South America and tropical countries. Leaves of A. muricata have been reported to possess antioxidant and anti-inflammatory activities. In this study, the gastroprotective effects of ethyl acetate extract of A. muricata leaves (EEAM) were investigated against ethanol-induced gastric injury models in rats. The acute toxicity test of EEAM in rats, carried out in two doses of 1 g/kg and 2 g/kg, showed the safety of this plant, even at the highest dose of 2 g/kg. The antiulcer study in rats (five groups, n=6) was performed with two doses of EEAM (200 mg/kg and 400 mg/kg) and with omeprazole (20 mg/kg), as a standard antiulcer drug. Gross and histological features showed the antiulcerogenic characterizations of EEAM. There was significant suppression on the ulcer lesion index of rats pretreated with EEAM, which was comparable to the omeprazole effect in the omeprazole control group. Oral administration of EEAM to rats caused a significant increase in the level of nitric oxide and antioxidant activities, including catalase, glutathione, and superoxide dismutase associated with attenuation in gastric acidity, and compensatory effect on the loss of gastric wall mucus. In addition, pretreatment of rats with EEAM caused significant reduction in the level of malondialdehyde, as a marker for oxidative stress, associated with an increase in prostaglandin E2 activity. Immunohistochemical staining also demonstrated that EEAM induced the downregulation of Bax and upregulation of Hsp70 proteins after pretreatment. Collectively, the present results suggest that EEAM has a promising antiulcer potential, which could be attributed to its suppressive effect against oxidative damage and preservative effect toward gastric wall mucus.

  8. Prophylactic effects of Clausena excavata Burum. f. leaf extract in ethanol-induced gastric ulcers

    Science.gov (United States)

    Albaayit, Shaymaa Fadhel Abbas; Abba, Yusuf; Abdullah, Rasedee; Abdullah, Noorlidah

    2016-01-01

    Clausena excavata is a natural herb with both antioxidant and anti-inflammatory properties. It has been used for decades in folkloric practice for the amelioration of various ailments. In this study, the gastroprotective activity of methanolic extract of C. excavata leaves (MECE) was determined in the Sprague Dawley rat ethanol-induced gastric ulcer model. Rats were pretreated with a single dose of vehicle (5% Tween 20), 20 mg/mL omeprazole, 400 and 200 mg/mL of MECE dissolved in 5% Tween 20. Ulcer was induced with 5 mL/kg of ethanol and stomach tissue was obtained after 1 hour. Histological examination was done on hematoxylin and eosin, periodic acid-Schiff, and immunochemically stained gastric mucosal tissues. Prostaglandin E2, superoxide dismutase, catalase, glutathione peroxidase, and lipid peroxidation levels of the gastric tissue homogenates were also determined. Significantly (Pulcer areas, less intense edema, and fewer leukocytes’ infiltration were observed in MECE- and omeprazole-treated than in untreated gastric mucosa with ulcer. The gastric pH, mucus production, superoxide dismutase, catalase, and glutathione peroxidase contents increased, while the lipid peroxidation content decreased as a result of MECE treatment. Bcl-2-associated X protein was underexpressed, while heat shock protein 70 and transforming growth factor-beta protein were overexpressed in the ulcerated gastric mucosa tissues treated with omeprazole and MECE. Similarly, there was a reduction in the levels of tumor necrotic factor-alpha and interleukin-6, while the level of interleukin-10 was increased. This study showed that the gastroprotective effect of MECE is achieved through inhibition of gastric juice secretion and ulcer lesion development, stimulation of mucus secretion, elevation of gastric pH, reduction of reactive oxygen species production, inhibition of apoptosis in the gastric mucosa, and modulation of inflammatory cytokines. PMID:27366052

  9. 奥美拉唑胶囊的制备及质量控制

    Institute of Scientific and Technical Information of China (English)

    刘程前

    2014-01-01

    Objective:Preparation of omeprazole capsules analysis and quality control methods. Meth-ods:antacid sodium bicarbonate was added,its content using high performance liquid chromatography to detect. Results:The concentration of omeprazole in the(4-16)ug / mL,the good linear relationship between peak area;RSD were 100 . 35% and 0 . 56%;content of three batches of samples were 99 . 8%, 99. 4%,and 99. 8%. Conclusion:The preparation method is simple,accurate determination of the re-covery precise,contribute to the quality control of omeprazole,worthy of promotion.%目的:分析奥美拉唑胶囊的制备方法及其质量控制方法。方法:制备中加入抗酸剂碳酸氢钠,采用高效液相色谱对其含量进行检测。结果:奥美拉唑的质量浓度在(4-16)ug/mL之内,与峰面积线性关系良好;RSD分别为100.35%和0.56%;3批样品的含量分别为99.8%、99.4%和99.8%。结论:该制备法操作简单、测定精准、回收率精确,有助于对奥美拉唑的质量控制,值得在临床推广。

  10. [Changes of rat gastric mucosal barrier under stress conditions].

    Science.gov (United States)

    Zhan, Xianbao; Li, Zhaoshen; Cui, Zhongmin; Duan, Yimin; Nie, Shinan; Liu, Jing; Xu, Guoming

    2002-06-01

    OBJECTIVE To explore the changes of rat gastric mucosal barrier under conditions of water immersion restraint stress. METHODS Eighty rats were randomly divided into Group A (20 rats), B (40 rats) and C (20 rats) after being fasted for 24 hours. And then Group A was divided into two subgroups with ten rats in each. The two subgroups in Group A were given normal saline or omeprazole respectively while under the stress condition. The changes of gastric acid or bicarbonate secretion were determined. Group B (40 rats) were randomly divided into four subgroups,which were subgroup control, 1h, 2h and 4h after beginning of the stress. The quantity of glandular mucosal adherent mucus, the thickness of mucus gel layer and ulcer index were measured after stress in Group B. The glandular mucosal samples were labeled by Lanthanum and observed by transmission electromicroscopy. Group C was randomly divided into two subgroups in the same way with Group A. And each subgroup received normal saline or omeprazole respectively H(+) loss in gastric lumen was calculated by determining the difference of acidity between lavage and drainage fluid H(+) concentration. RESULTS It was found that gastric alkaline secretion decreased progressively (P omeprazole subgroup, the amount of H(+) loss (micromol) was 7.46 +/- 1.22, 4.56 +/- 0.35, 3.11 +/- 0.81, 2.32 +/- 1.42 and 2.13 +/- 1.60, which decreased progressively, however still higher than those in normal saline subgroup (P "bicarbonate secretion is inhibited; gastric barrier is damaged; and hydrogen permeability through gastric mucosal barrier increases under stress conditions.

  11. Comparison of levofloxacin versus clarithromycin efficacy in the eradication of Helicobacter pylori infection

    Science.gov (United States)

    Haji-Aghamohammadi, Ali Akbar; Bastani, Ali; Miroliaee, Arash; Oveisi, Sonia; Safarnezhad, Saeed

    2016-01-01

    Background: Helicobacter pylori (H.pylori) infection causes multiple upper gastrointestinal diseases but optimal therapeutic regimen which can eradicate infection in all the cases has not yet been defined. This study was designed to evaluate the efficacy of triple levofloxacin-based versus clarithromycin-based therapy. Methods: In this open-label randomized clinical trial study 120 patients who had esophagogastroduodenoscopy (EGD) with positive rapid urease test (RUT) were enrolled and divided into 2 groups. Case group was treated with levofloxacin (500 mg daily) plus amoxicillin (1 gr twice a day) plus omeprazole (20 mg daily) for 2 weeks. Control group was treated with clarithromycin (500 mg twice a day) plus omeprazole (20 mg daily) for 2 weeks. After the main course of treatment, they received maintenance treatment with omeprazole for 4 weeks. Stool antigen test was performed on them after two weeks of not having any medicine. Results: H.pylori eradication (intention to treat analysis) was successful in 75% of case group and 51.7% of control group showing a significant difference (P=0.008). H.p infection eradication (per-protocol analysis) was successful in 80.4% in case group and 57.4%% in control group showing significant difference (P=0.009). Drugs adverse effects causing discontinuation treatment were seen in 5% of case group and 3.3% of control group which have not shown a significant difference between the two groups (P=0.648). Conclusion: Triple therapy with levofloxacin-based regimen has better efficacy than clarithromycin-based regimen and as safe as it is. PMID:27999644

  12. Prevention by lansoprazole, a proton pump inhibitor, of indomethacin -induced small intestinal ulceration in rats through induction of heme oxygenase-1.

    Science.gov (United States)

    Yoda, Y; Amagase, K; Kato, S; Tokioka, S; Murano, M; Kakimoto, K; Nishio, H; Umegaki, E; Takeuchi, K; Higuchi, K

    2010-06-01

    The effect of lansoprazole, a proton pump inhibitor (PPI), on indomethacin-induced small intestinal ulceration was examined in rats, particularly in relation to heme oxygenase (HO)-1. The animals were administered indomethacin (10 mg/kg, p.o.) and killed 24 h later. Lansoprazole (30-100 mg/kg, p.o.) and omeprazole (30-100 mg/kg, p.o.) were given 30 min before the administration of indomethacin, while tin-protoporphyrin IX (SnPP: 30 mg/kg, i.v.), an inhibitor of HO-1, was injected 10 min before indomethacin or lansoprazole. Indomethacin produced hemorrhagic lesions in the small intestine, accompanied with an increase of mucosal invasion of enterobacteria, inducible nitric oxide synthase (iNOS) expression, and myeloperoxidase (MPO) activity in the mucosa. Pretreatment with lansoprazole dose- dependently reduced the severity of the indomethacin-induced intestinal lesions, with suppression of the increased MPO activity, while omeprazole had no effect. Pretreatment with SnPP significantly exacerbated these intestinal lesions and almost totally abolished the protective effect of lansoprazole. The up-regulation of iNOS mRNA expression following indomethacin was suppressed by lansoprazole in a SnPP-inhibitable manner, although the enhanced enterobacterial invasion remained unaffected. The amount of HO-1 protein in the intestinal mucosa was significantly increased by lansoprazole but not by omeprazole. Prior administration of carbon monoxide (CO)-releasing molecule-2 (CORM-2; 10 mg/kg, i.p.) significantly reduced the severity of these lesions and the enhancement of mucosal iNOS mRNA expression induced in the small intestine by indomethacin. These results suggest that lansoprazole prevents indomethacin-induced small intestinal ulceration, and this effect is associated with inhibition of iNOS expression, through up-regulation of HO-1/CO production in the mucosa.

  13. Proton pump inhibitors exert anti-allergic effects by reducing TCTP secretion.

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    Sunghee Choi

    Full Text Available BACKGROUND: Extracellular translationally controlled tumor protein (TCTP is known to play a role in human allergic responses. TCTP has been identified outside of macrophages, in activated mononuclear cells, and in biological fluids from allergic patients. Even TCTP devoid of signal sequences, is secreted to extracellular environment by an yet undefined mechanism. This study is aimed at understanding the mechanism of TCTP release and its regulation. A secondary goal is to see if inhibitors of TCTP release can serve as potential anti-allergic asthmatic drugs. METHODOLOGY/PRINCIPAL FINDINGS: Using Western blotting assay in HEK293 and U937 cells, we found that TCTP secretion is reduced by omeprazole and pantoprazole, both of which are proton pump inhibitors. We then transfected HEK293 cells with proton pump expression vectors to search for the effects of exogeneously overexpressed H(+/K(+-ATPase on the TCTP secretion. Based on these in vitro data we checked the in vivo effects of pantoprazole in a murine model of ovalbumin-induced allergy. Omeprazole and pantoprazole reduced TCTP secretion from HEK293 and U937 cells in a concentration-dependent fashion and the secretion of TCTP from HEK293 cells increased when they over-expressed H(+/K(+-ATPase. In a murine model of ovalbumin-induced allergy, pretreatment with pantoprazole reduced infiltration of inflammatory cells, increased goblet cells, and increased TCTP secretion induced by OVA challenge. CONCLUSION: Since Omeprazole and pantoprazole decrease the secretion of TCTP which is associated with the development of allergic reaction, they may have the potential to serve as anti-allergic (asthmatic drugs.

  14. Efficacy of rifabutin-based triple therapy as second-line treatment to eradicate helicobacter pylori infection

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    Méndez Isabel

    2007-07-01

    Full Text Available Abstract Background Rifabutin has been found to be effective in multi-resistant patients after various treatment cycles for Helicobacter pylori (HP infection, but it has not been analysed as a second-line treatment. Therefore, we seek to compare the effectiveness of a treatment regimen including rifabutin versus conventional quadruple therapy (QT. Methods Open clinical trial, randomised and multi-centre, of two treatment protocols: A Conventional regime -QT- (omeprazole 20 mg bid, bismuth citrate 120 mg qid, tetracycline 500 mg qid and metronidazole 500 mg tid; B Experimental one -OAR- (omeprazole 20 mg bid, amoxicillin 1 gr bid, and rifabutin 150 mg bid, both taken orally for 7 days, in patients with HP infection for whom first-line treatment had failed. Eradication was determined by Urea Breath Test (UBT. Safety was determined by the adverse events. Results 99 patients were randomised, QT, n = 54; OAR, n = 45. The two groups were homogeneous. In 8 cases, treatment was suspended (6 in QT and 2 in OAR. The eradication achieved, analysed by ITT, was for QT, 38 cases (70.4%, and for OAR, 20 cases (44.4%; p = 0.009, OR = 1.58. Of the cases analysed PP, QT were 77.1%; OAR, 46.5%; p = 0.002. Adverse effects were described in 64% of the QT patients and in 44% of the OAR patients (p = 0.04. Conclusion A 7-day rifabutin-based triple therapy associated to amoxicillin and omeprazole at standard dose was not found to be effective as a second-line rescue therapy. The problem with quadruple therapy lies in the adverse side effects it provokes. We believe the search should continue for alternatives that are more comfortably administered and that are at least as effective, but with fewer adverse side effects. Trial Registration Current Controlled Trials ISRCTN81058036

  15. Fade and tachyphylaxis of gastric acid secretory response to pentagastrin in rat isolated gastric mucosa.

    Science.gov (United States)

    Hirst, B H; Holland, J; Parsons, M E; Price, C A

    1988-12-01

    1. Gastric acid secretory responses to pentagastrin were characterized in the rat isolated gastric mucosa. In particular, the mechanisms underlying fade, declining response upon continued stimulation, and tachyphylaxis, progressively reduced responses upon repeated stimulation, were investigated. 2. Pentagastrin, 10(-9)-10(-7) M, resulted in concentration-related increases in acid secretion, with a mean maximum of 2.65 mumol cm-2 h-1 in response to pentagastrin, 10(-7) M. Higher concentrations of pentagastrin produced sub-maximal secretory rates; we define this as auto-inhibition. The responses to all concentrations of pentagastrin demonstrated fade. The rate of fade was correlated with the maximum acid secretory rate, declining at about 36% of the peak over the first 16 min. 3. The PO2, PCO2, [HCO3-], pH, [glucose], [lactate], [Na+] and [K+] did not decline during the fade of the acid secretory response to pentagastrin, 10(-7) M. Addition of a second aliquot of pentagastrin was not able to reverse fade, but these tissues were responsive to histamine. Replacement of the serosal solution, before addition of a second aliquot of pentagastrin, increased the acid response from 3% to 24% of the first response. 4. Serosal solution from donor tissues, allowed to respond to pentagastrin and then the acid secretion to fade, was able to stimulate secretion in fresh recipient tissues, although at lower rates. 5. Acid secretory responses to a second dose of pentagastrin were not significantly different, whether the tissues were previously unstimulated, or stimulated with pentagastrin washed out after attaining its peak secretory response (after 10-20 min). The second response was significantly reduced if the first response was allowed to fade with the pentagastrin in contact for 100 min; i.e. fade significantly influenced the extent of tachyphylaxis. 6. Proglumide, 10(-2) M, a gastrin receptor antagonist, and omeprazole, 10(-5) M, an inhibitor of the gastric (H+ + K

  16. Evaluación económica del tratamiento con ácido acetilsalicílico más esomeprazol comparado con clopidogrel en la prevención de la hemorragia gastrointestinal Economic evaluation of the treatment of aspirin plus esomeprazole compared to clopidogrel in gastrointestinal bleeding prevention

    Directory of Open Access Journals (Sweden)

    Carme Piñol

    2006-02-01

    Full Text Available Objetivo: Evaluar la eficiencia del ácido acetilsalicílico (AAS más esomeprazol frente a clopidogrel en la prevención de la hemorragia gastrointestinal. Métodos: Análisis coste-efectividad (árbol de decisión de 2 ramas: AAS más esomeprazol y clopidogrel respecto a la evitación de casos de hemorragia gastrointestinal en 2 años, y análisis de sensibilidad. Resultados: El coste total del tratamiento con AAS más esomeprazol (2.865 S por paciente libre de hemorragia fue inferior al clopidogrel (2.965 S. El tratamiento con AAS resultó dominante. En todos los análisis de sensibilidad la combinación siguió siendo dominante. Al sustituir esomeprazol 40 mg por omeprazol 40 mg, el coste del tratamiento combinado descendió hasta 1.934S/por episodio evitado. Conclusiones: La asociación de esomeprazol y AAS es más coste-efectiva que clopidogrel en la prevención de la hemorragia gastrointestinal. La combinación con omeprazol resulta aún más coste-efectiva.Objective: To evaluate the use of aspirin plus esomeprazole vs. clopidogrel in the prevention of gastrointestinal bleeding. Methods: We performed a cost-effectiveness analysis (two-branch decision tree: aspirin plus esomeprazole or clopidogrel of prevention of gastrointestinal bleeding over a 2-year period, as well as sensitivity analyses. Results: The total cost of aspirin plus esomeprazole treatment (2,865S/patient free of hemorrhage was lower than that of clopidogrel (2,965S. Aspirin treatment was dominant. The combination continued to be dominant in all sensitivity analyses. When esomeprazole 40 mg was substituted by omeprazole 40 mg, the cost of combination therapy decreased to 1,934 S/prevented hemorrhage. Conclusions: The association of esomeprazole and aspirin is more cost-effective than clopidogrel in preventing gastrointestinal bleeding. Aspirin plus omeprazole was even more cost-effective.

  17. Triple therapy with ilaprazole,levofloxacin and clarithromycin for the eradication of Helicobacter pylori

    Institute of Scientific and Technical Information of China (English)

    黄伟平

    2014-01-01

    Objective To evaluate the efficacy of triple therapy with ilaprazole,levofloxacin and clarithromycin and standard triple therapy for Helicobacter pylori(Hp)eradication.Methods One hundred and twenty Hp(+)patients were randomized to two groups:the treatment group:60 patients received ilaprazole 5 mg,bid,levofloxacin 0.5 g,qd,and clarithromycin 500 mg,bid,for7 days;60 patients received omeprazole 20 mg,bid,amoxicillin 1 g,and clarithromycin 500 mg,bid,for 7days.Follow-up Hp test was performed at four weeks after the treatment.Results Intention-treatment analysis

  18. Therapeutic effect of Streptococcus thermophilus CRL 1190-fermented milk on chronic gastritis

    Institute of Scientific and Technical Information of China (English)

    Cecilia; Rodríguez; Marta; Medici; Fernanda; Mozzi; Graciela; Font; de; Valdez

    2010-01-01

    AIM: To investigate the potential therapeutic effect of exopolysaccharide (EPS)-producing Streptococcus thermophilus (S. thermophilus) CRL 1190 fermented milk on chronic gastritis in Balb/c mice. METHODS: Balb/c mice were fed with the fermented milk for 7 d after inducing gastritis with acetyl-salicylic acid (ASA, 400 mg/kg body weight per day for 10 d). Omeprazole was included in this study as a positive therapeutic control. The gastric in? ammatory activity was evaluated from gastric histology and in? amm...

  19. Synthesis and antiulcer activity studies of 2-(1′-iminothioimido substituted-1′-substituted phenylbenzoic acids

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    Subudhi B

    2008-01-01

    Full Text Available Certain 2-(1′-iminothioimido substituted-1′-substituted phenybenzoic acids (P 1-9 were synthesized by reaction of phthalic anhydride with benzotriazole, 2-mercapto benzothiazole and 2-p-amino phenyl benzimidazole, respectively (A 1-3 followed by imine formation with Schiff bases of thiourea with salicylaldehyde, furfuraldehyde and 1-phenyl-3-methyl-5-pyrazolone. Antiulcer activity was evaluated using reduction in total acidity, free acidity and ulcer index as parameters. Compounds P 3 , P 6 , P 7 and P 9 (100 mg/kg showed significant (P< 0.001 antiulcer action compared to control and omeprazole (40 mg/kg.

  20. Problems experienced by older people when opening medicine packaging.

    Science.gov (United States)

    Philbert, Daphne; Notenboom, Kim; Bouvy, Marcel L; van Geffen, Erica C G

    2014-06-01

    Medicine packages can cause problems in daily practice, especially among older people. This study aimed to investigate the prevalence of problems experienced by older people when opening medicine packaging and to investigate how patients manage these problems. A convenience sample of 30 community pharmacies participated in this study. They selected a systematic sample of 30 patients over 65 years old with a recent omeprazole prescription, and a questionnaire was administered by telephone for at least 10 patients per pharmacy. A total of 317 patients completed the questionnaire. They received their omeprazole in a bottle (n = 179, 56.5%), push-through blister pack (n = 102, 32.2%) or peel-off blister pack (n = 36, 11.4%). Some 28.4% of all patients experienced one or more problems with opening their omeprazole packaging; most problems occurred with peel-off blisters (n = 24, 66.7% of all respondents using peel-off blisters), followed by push-through blisters (n = 34, 33.3%) and finally bottles (n = 32, 17.9%). The risk of experiencing problems with peel-off blisters and push-through blisters was higher [relative risk 3.7 (95% confidence interval 2.5-5.5) and 1.9 (1.2-2.8), respectively] than the risk of experiencing problems with opening bottles. Two-thirds of respondents reported management strategies for their problems. Most were found for problems opening bottles (n = 24, 75%), followed by push-through blisters (n = 24, 70.6%) and peel-off blisters (n = 14, 58.3%). One in four patients over 65 experienced difficulties opening their omeprazole packaging and not all of them reported a management strategy for their problems. Manufacturers are advised to pay more attention to the user-friendliness of product packaging. In addition, it is important that pharmacy staff clearly instruct patients on how to open their medicine packaging, or assist them in choosing the most appropriate packaging. © 2013 Royal Pharmaceutical Society.

  1. [Antisecretory therapy as a component of hemostasis in acute gastroduodenal ulcer bleedings].

    Science.gov (United States)

    Gostishchev, V K; Evseev, M A

    2005-01-01

    Results of antisecretory therapy (pyrenzepin, H(2)-blockers, inhibitors of proton pump, octreotid) in 962 patients with acute gastroduodenal ulcer bleedings (AGDUB) were analyzed over 14-years period. Antisecretory treatment in AGDUB has principally different goals and potential depending on risk of bleeding's recurrence and morphological changes in tissue of gastroduodenal ulcer. Antisecretory therapy is the main treatment in high risk of AGDUB recurrence or before urgent surgery. Intravenous infusion of omeprazol has demonstrated the highest clinical efficacy due to maximal inhibition of gastric secretion and absence of negative influences on oxygen regimen in tissue of ulcer.

  2. Esofagitis candidiásica en una paciente inmunocompetente: a propósito de un caso

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    D. Palacios Martínez

    2013-12-01

    Full Text Available La esofagitis candidiásica (EC es una de las formas invasivas de candidiasis. Su prevalencia diagnosticada mediante endoscopia digestiva alta oscila entre 0,77-2,4%. Su principal causa es la Candida albicans (CA. La EC afecta con mayor frecuencia a sujetos inmunodeprimidos, aunque también puede aparecer en sujetos sanos. Precisa tratamiento antifúngico sistémico. Presentamos el caso de una EC en una paciente sana con buena respuesta al tratamiento pautado, potencialmente relacionado con la toma de omeprazol por parte de la paciente.

  3. [Posterior gastric wall ulceration as a complication of percutaneous endoscopic gastrostomy. A report of 2 cases].

    Science.gov (United States)

    Szarszewski, Adam; Szlagatys-Sidorkiewicz, Agnieszka; Borkowska, Anna; Landowski, Piotr; Radys, Wojciech

    2009-01-01

    Two cases of posterior gastric wall ulceration are presented as a rare complication of percutaneous endoscopic gastrostomy (PEG). Percutaneous endoscopic gastrostomy (Flocare, Nutricia) was performed in two boys (aged 2 and 19 months), who were unable to take necessary nutrients by mouth due to neurological disorders concerning swallowing and deficiency of body mass. This status does not allow to cover liquid and caloric requirement. In one case bleeding occurred 12 days after PEG insertion, in the second--6 weeks after PEG insertion. Both patients were treated with parenteral nutrition and omeprazol intravenously, with good result. The described complications are rare, however, the proton pomp inhibitors application in prevention should be considered.

  4. [Diagnosis and therapy of laryngitis gastrica].

    Science.gov (United States)

    Pahn, J; Schlottmann, A; Witt, G; Wilke, W

    2000-07-01

    We treated 64 patients with the diagnosis of laryngitis gastrica with Antra (Omeprazol) in doses of 10, 20, and 40 mg. To determine the success of the therapy, pH monitoring of the esophagus and hypopharynx, the voice status and measurement of vocal penetrating capacity were used. The results prove that a 20-mg dose of Antra is suitable for the therapy of laryngitis gastrica with a high rate of success. Problems which arose during the investigation, consequent changes of the original concept of the project as well as new aspects and questions which resulted from this are discussed with respect to further investigation.

  5. Relationship between the acid-suppression efficacy of proton pump inhibitors and CYP2C19 genetic polymorphism in patients with peptic ulcer

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Objective To investigate acid-suppression efficacy of proton pump inhibitors(PPIs) in relation to CYP2C19 genetic polymorphism on patients with peptic ulcer. Methods By an open, randomized and control trial, fifty nine patients with active peptic ulcer were randomly assigned to receive one of three PPIs on a single dose (20 mg of each drug): omeprazole group (n=19), rabeprazole group (n=20) and esomeprazole group (n=20). Intragastric pH was recorded 1 hour before and 24 hours after administration. CYP2C19 g...

  6. Maastricht Ⅱ treatment scheme and efficacy of different proton pump inhibitors in eradicating Helicobacter pylori

    Institute of Scientific and Technical Information of China (English)

    Engin Altintas; Orhan Sezgin; Oguz Ulu; Ozlem Aydin; Handan Camdeviren

    2004-01-01

    AIM: The Maastricht Ⅱ criteria suggest the use of amoxicillin and clarithromycin in addition to a proton pump inhibitor over 7-10 d as a first line therapy in the eradication of Helicobacter pylori(H pylori). For each proton pump inhibitor, various rates of eradication have been reported. The present study was to compare the efficacy of different proton pump inhibitors like omeprazole, lansoprazole and pantoprazole in combination with amoxicillin and clarithromycin in the first line eradication of H pylori and to investigate the success of H pylori eradication in our district.METHODS: A total of 139 patients were included having a Helicobacter pylori(+) gastroduodenal disorders diagnosed by means of histology and urease test. Besides amoxicillin (1 000 mg twice a day) and clarithromycin (500 mg twice a day), they were randomized to take omeprazole (20 mg twice a day), or lansoprazole (30 mg twice a day), or pantoprozole (40 mg twice a day) for 14 d. Four weeks after the therapy, the eradication was assessed by means of histology and urease test. It was evaluated as eradicated if the H pylori was found negative in both. The complaints (pain in epigastrium, nocturnal pain, pyrosis and bloating)were graded in accordance with the Licert scale. The compliance of the patients was recorded.RESULTS: The eradication was found to be 40.8% in the omeprazole group, 43.5% in the lansoprazole group and 47.4% in the pantoprazole group. Sixty-three out of 139patients (45%) had eradication. No statistically significant difference was observed between the groups. Significant improvements were seen in terms of the impact on the symptom scores in each group.CONCLUSION: There was no difference between omeprazole, lansoprazole and pantoprazole in H pylori eradication, and the rate of eradication was as low as 45%.Symptoms were improved independent of the eradication in each treatment group. The iow eradication rates suggest that the antibiotic resistance or the genetic differences of

  7. Clinical and cost impact of intravenous proton pump inhibitor use in non-ICU patients

    Institute of Scientific and Technical Information of China (English)

    Soumana; C; Nasser; Jeanette; G; Nassif; Hani; I; Dimassi

    2010-01-01

    AIM:To assess the appropriateness of the indication and route of administration of proton-pump-inhibitors (PPIs) and their associated cost impact. METHODS:Data collection was performed prospec-tively during a 6-mo period on 340 patients who re-ceived omeprazole intravenously during their hospital stay in non-intensive care floors. Updated guidelines were used to assess the appropriateness of the indication and route of administration. RESULTS:Complete data collection was available for 286 patients which wer...

  8. pH monitoring in patients with benign voice disorders

    DEFF Research Database (Denmark)

    Grøntved, A M; West, F

    2000-01-01

    wall granulation and increased muscle tension. The patients in the reflux group were given medical treatment using omeprazole, and 76% logopedic voice training program. More than 50% of the laryngeal reflux patients were treated for more than 4 months before their voice problems had resolved......The aim of this study was to compare oesophageal pH-metry with laryngeal signs and symptoms in patients suspected of laryngeal reflux disease. A total of 60 patients with voice disorders, who were suspected of laryngeal reflux, were tested by single probe oesophageal pH monitoring. Thirty...

  9. 不同质子泵抑制剂的药理特点与临床疗效对比%Pharmacological characteristics and clinical effect comparison of different proton pump inhibitors

    Institute of Scientific and Technical Information of China (English)

    李莉

    2014-01-01

    Objective To investigate the clinical effect and adverse reactions of the gastric ulcer treated with omeprazole,pantoprazole,lansoprazol,and provide the basis for the rational use of drugs.Methods The clinical data of 180 patients with gastric ulcer from May 2010 to May 2013 in traditional Chinese medicine hospital of Yanzhou were retrospectively analyzed,all patients were treated with antibacterial,acid suppression and gastric mucosa protection,the amoxicillin capsules and colloidal bismuth pectin capsules were chose as antibacterial and gastric mucosa protectant.They were divided into omeprazole group,pantoprazole group,lansoprazole group according to the different acid suppression agent with 60 cases in each group.The clinical curative effect and adverse reactions of the three groups were observed and compared.Results The clinical cure rate of omeprazole group,pantoprazole group and lansoprazole group was 73.33%,71.67%,70.00% respectively,and the clinical effective rate was 86.67%,85.00%,85.00%,respectively,there was no significant difference among the three groups (P > 0.05) ; There was no significant difference in the symptom remission rate of the three groups,but the abdominal distension remission rate in pantoprazole group was obviously better than that in omeprazole group and lansoprazole group,the differences were significant (x2 =4.276,P < 0.05 ; x2 =4.633,P <0.05),the belching anti acid remission rate in the omeprazole group was better than that in the pantoprazole group and lansoprazole group group,the differences were significant (x2 =4.201,P < 0.05 ;x2 =4.317,P <0.05).The incidence of adverse reactions in omeprazole group was significantly lower than that in the pantoprazole group (x2 =4.552,P < 0.05),and the rate in pantoprazole group was significantly lower than that in lansoprazole group (x2 =4.633,P < 0.05).Conclusions All of the three acid-blocking drugs have achieved good clinical curative effect,omeprazole and

  10. Evaluation of Curative Effect of Triple Regimen in The Treatment of Hp Positive Peptic Ulcer%三联方案治疗Hp阳性消化性溃疡的疗效评价

    Institute of Scientific and Technical Information of China (English)

    周欣

    2015-01-01

    Objective To explore the clinical effect of metronidazole, amoxicillin and clavulanate potassium and omeprazole for Helicobacter pylori (Hp) infection positive type peptic ulcer, to guide the clinical rational drug use. Methods 190 cases with Hp positive peptic ulcer were selected randomly in Benxi Central Hospital, control group (95 cases) received only omeprazole, and observation group(95 cases) were treated with metronidazole, amoxicillin and clavulanate potassium and omeprazole, and the clinical effect and adverse reaction were compared between two groups. Results The total effective rate of observation group (96.84%) was signiifcantly higher than that of the control group (84.21%), P<0.05, the difference had statistical significance. Conclusion Metronidazole, amoxicillin and clavulanate potassium and omeprazole triple therapy had remarkable effective in the treatment of Hp positive peptic ulcer. It was worthy of clinical promotion and application.%目的:探究甲硝唑、阿莫西林克拉维酸钾和奥美拉唑三联方案治疗幽门螺杆菌(Helicobacter pylori,Hp)感染阳性型消化性溃疡的效果,指导临床合理用药。方法随机选我院收治的Hp阳性消化性溃疡患者共190例,其中单用奥美拉唑治疗的95例患者作对照组,同时联用甲硝唑和阿莫西林克拉维酸钾的95例患者作观察组,对比两组患者疗效及不良反应。结果观察组总有效率(96.84%)显著高于对照组(84.21%),P<0.05,存在显著性差异。结论甲硝唑、阿莫西林克拉维酸钾和奥美拉唑三联方案能够有效治疗Hp阳性消化性溃疡,建议临床普及应用。

  11. Reappraisal of bicarbonate secretion by the human oesophagus

    DEFF Research Database (Denmark)

    Mertz-Nielsen, A; Hillingsø, Jens; Bukhave, K

    1997-01-01

    measured. RESULTS: The median rates (95% confidence intervals) of intrinsic oesophageal bicarbonate secretion, corrected for contaminating salivary and gastric bicarbonate, were 89 (33-150) and 121 (63-203) mumol/h/10 cm (p > 0.5) in omeprazole and ranitidine treated subjects respectively. Salivary...... and gastric bicarbonate contaminating the oesophagus accounted for 14% and 3%, respectively, of total oesophageal bicarbonate output. CONCLUSIONS: Bicarbonate secretory capacity of the human oesophagus is less than previously assumed, and the clinical relevance of intrinsic oesophageal bicarbonate for mucosal...

  12. Therapeutics for Equine Gastric Ulcer Syndrome.

    Science.gov (United States)

    Zavoshti, Fereydon Rezazadeh; Andrews, Frank M

    2017-04-01

    Equine gastric ulcer syndrome (EGUS) is an umbrella term used to describe ulcers in the nonglandular squamous and glandular mucosa, terminal esophagus, and proximal duodenum. Gastric ulcers in the squamous and glandular regions occur more often than esophageal or duodenal ulcers and likely have a different pathogenesis. At present, omeprazole is accepted globally as the best pharmacologic therapy for both regions of the stomach; however, the addition of coating agents and synthetic prostaglandins could add to its effectiveness in treatment of EGUS. Dietary and environmental management are necessary for prevention of recurrence. Copyright © 2016 Elsevier Inc. All rights reserved.

  13. Clinically significant CYP2C inhibition by noscapine but not by glucosamine.

    Science.gov (United States)

    Rosenborg, S; Stenberg, M; Otto, S; Ostervall, J; Masquelier, M; Yue, Q-Y; Bertilsson, L; Eliasson, E

    2010-09-01

    Noscapine and glucosamine reportedly interact with warfarin. We investigated the effects of these drugs on various cytochrome P450 (CYP) activity markers. Twelve healthy subjects were phenotyped at baseline and during separate treatments with noscapine and glucosamine. Whereas glucosamine had no significant effect on CYP activity, noscapine caused marked inhibition of CYP2C9 (4.9-fold increase in urinary losartan/E3174 ratio) and CYP2C19 (3.6-fold increase in the plasma omeprazole/5-hydroxyomeprazole ratio). Noscapine-dependent inhibition of CYP2C9 may explain the interaction with warfarin.

  14. Efecto citoprotector y antisecretor del aceite de Copaifera officinalis en lesiones gástricas inducidas en ratas

    Directory of Open Access Journals (Sweden)

    Jorge Arroyo

    2009-06-01

    Full Text Available Objetivos: Demostrar el efecto gastroprotector del aceite de Copaifera officinalis usando indometacina y ligadura de píloro en ratas. Diseño: Estudio preclínico. Lugar: Facultades de Medicina, de Farmacia y Bioquímica. Universidad Nacional Mayor de San Marcos, Lima, Perú. Material biológico: Ratas y aceite de copaiba. Intervenciones: Se colectó el aceite de copaiba en Ucayali, Pucallpa. La citoproteccción fue evaluada con indometacina, considerando un grupo control normal, indometacina, grupos de aceite de copaiba y omeprazol. Las lesiones de la mucosa gástrica fueron calificadas como las compatibles con necrosis local (tejido no viable, hiperemia, enrojecimiento presente y hemorragia, empleando la escala de puntaje observacional; y la úlcera, según la escala de Macallister modificado. El ensayo de antisecreción fue realizado por el modelo de ligadura del píloro, en el que 24 ratas albinas fueron divididas al azar en 3 grupos; un control, otro de aceite de copaiba 40mg/kg y un tercero de omeprazol 10 mg/kg. Después de 4 horas de ligazón, fueron sacrificados, extrayéndose los estómagos; con mucho cuidado se midió el volumen y se determinó el pH de la secreción gástrica, por potenciometría. Se realizó evaluación histopatológica según Devi. Principales medidas de resultados: Lesiones ulcerosas. Resultados: Los resultados indicaron 100% de efecto citoprotector con el aceite de copaiba y de 97,8% para el omeprazol (p<0,0001, ratificado con los hallazgos histopatológicos; la disminución del volumen de secreción fue 79,4% para omeprazol y 42,8% para el aceite de copaiba (p<0,001, con incremento del pH. Conclusiones: En condiciones experimentales, el aceite de copaiba fue efectivo como agente gastroprotector en ratas con inducción de úlcera gástrica.

  15. Effects of NorA Inhibitors on In Vitro Antibacterial Activities and Postantibiotic Effects of Levofloxacin, Ciprofloxacin, and Norfloxacin in Genetically Related Strains of Staphylococcus aureus

    Science.gov (United States)

    Aeschlimann, Jeffrey R.; Dresser, Linda D.; Kaatz, Glenn W.; Rybak, Michael J.

    1999-01-01

    NorA is a membrane-associated multidrug efflux protein that can decrease susceptibility to fluoroquinolones in Staphylococcus aureus. To determine the effect of NorA inhibition on the pharmacodynamics of fluoroquinolones, we evaluated the activities of levofloxacin, ciprofloxacin, and norfloxacin with and without various NorA inhibitors against three genetically related strains of S. aureus (SA 1199, the wild-type; SA 1199B, a NorA hyperproducer with a grlA mutation; and SA 1199-3, a strain that inducibly hyperproduces NorA) using susceptibility testing, time-kill curves, and postantibiotic effect (PAE) methods. Levofloxacin had the most potent activity against all three strains and was minimally affected by addition of NorA inhibitors. In contrast, reserpine, omeprazole, and lansoprazole produced 4-fold decreases in ciprofloxacin and norfloxacin MICs and MBCs for SA 1199 and 4- to 16-fold decreases for both SA 1199B and SA 1199-3. In time-kill experiments reserpine, omeprazole, or lansoprazole increased levofloxacin activity against SA 1199-3 alone by 2 log10 CFU/ml and increased norfloxacin and ciprofloxacin activities against all three strains by 0.5 to 4 log10 CFU/ml. Reserpine and omeprazole increased norfloxacin PAEs on SA 1199, SA 1199B, and SA 1199-3 from 0.9, 0.6, and 0.2 h to 2.5 to 4.5, 1.1 to 1.3, and 0.4 to 1.1 h, respectively; similar effects were observed with ciprofloxacin. Reserpine and omeprazole increased the levofloxacin PAE only on SA 1199B (from 1.6 to 5.0 and 3.1 h, respectively). In conclusion, the NorA inhibitors dramatically improved the activities of the more hydrophilic fluoroquinolones (norfloxacin and ciprofloxacin). These compounds may restore the activities of these fluoroquinolones against resistant strains of S. aureus or may potentially enhance their activities against sensitive strains. PMID:9925528

  16. Anti-helicobacter pylori effect of total alkaloids of sophora alopecuroides in vivo

    Institute of Scientific and Technical Information of China (English)

    Tian Aiping; Xu Ting; Liu Kaiyun; Zou Quanming; Yan Xiang

    2014-01-01

    Background Helicobacterpylori (H.pylori) infection could lead to most gastroduodenal diseases and is even identified as a carcinogen of gastric cancer.Total alkaloids of sophora alopecuroides (TASA) is widely used in herbal remedies to treat various infectious diseases,including stomach-associated diseases.This study is aimed at evaluating the antimicrobial activity of TASA on H.pylori-infected BALB/c mice mouse gastritis.Methods Totally 120 BALB/c mice were orally inoculated with H.pylori Bacterial liquid to construct BALB/c mice H.pylori infection gastritis animal model,after the model was successfully created.We randomly assigned 100 infected mice into 10 treatment groups,the first group (normal saline); the second group (bismuth pectin); the third group (omeprazole); the fourth group (TASA 2 mg/d); the fifth group (TASA 4 mg/d); the sixth group (TASA 5 mg/d); the seventh group (TASA + bismuth pectin); the eighth group (TASA + omeprazole); the ninth group (bismuth pectin + clarithromycin + metronidazole);the tenth group (omeprazole + clarithromycin + metronidazole),5 other non-infected mice as negative control.Mice were orally inoculated twice a day and 7 days continuously.Then the mice were killed 4 weeks after treatment,we used realtime PCR to detect 16sDNA of H.pylori to test both the colonization and the clearance mice of bacteria of each treatment.We applied hematoxylin and eosin (HE) staining and immunostaining of mice gastric mucosa to observe the general inflammation and related factors interleukin 8 (IL-8),cyclooxygenase 2 (COX-2),and nuclear factor-kappa B (NF-KB) expression change after treatments.Results Firstly,we ensured that after 6-week intragastric administration,the bacteria colonization reached an exceed peak which is far higher than positive threshold (P <0.001); secondly,after treatments,it is revealed that TASA combined with omeprazole or bismuth pectin showed promising antimicrobial activity against H.pylori as well as conventional

  17. High performance liquid chromatography with photo diode array for separation and analysis of naproxen and esomeprazole in presence of their chiral impurities: Enantiomeric purity determination in tablets.

    Science.gov (United States)

    Ragab, Marwa A A; El-Kimary, Eman I

    2017-05-12

    A stereoselective high performance liquid chromatographic method with diode array detection (HPLC-DAD) was introduced for S-naproxen and esomeprazole determination in tablets. The separation was achieved on a Kromasil Cellucoat chiral column using a mobile phase consisting of hexane: isopropanol: trifluoroacetic acid (TFA) (90:9.9:0.1 v/v/v). The proposed system was found to be suitable for the enantioseparation of naproxen and omeprazole biologically active isomers. After optimization of the chromatographic conditions, resolution values of 3.84 and 2.17 could be obtained for naproxen and omeprazole isomers, respectively. The method was fully validated for the determination of S-isomers of each drug in their dosage form. Also, the enentiomeric purity was determined in commercial tablet containing S-naproxen and esomeprazole. The enantiomeric purity was calculated for each drug and the chiral impurities (R-isomers) could be determined at 1% level. The method was validated and good results with respect to linearity, precision, accuracy, selectivity and robustness were obtained. The limits of detection (LOD) and quantification (LOQ) were 2.00, 6.50 and 0.10, 0.35μgmL(-1) for S-naproxen and esomeprazole, respectively. Copyright © 2017 Elsevier B.V. All rights reserved.

  18. Antiulcer properties of Glycyrrhiza glabra L. extract on experimental models of gastric ulcer in mice.

    Science.gov (United States)

    Jalilzadeh-Amin, Ghader; Najarnezhad, Vahid; Anassori, Ehsan; Mostafavi, Mostafa; Keshipour, Hadi

    2015-01-01

    Glycyrrhiza glabra L. is used in folk medicine for treatment of stomach disorders including peptic ulcers. The hydroalcoholic extract of Glycyrrhiza glabra L. (HEGG) was evaluated for antiulcerogenic activity and acute toxicity profile in mice. Various doses of HEGG (50-200 mg/kg) were administered orally to animals of different groups. Omeprazole and cimetidine at doses of 30 and 100 mg/kg were used as positive controls, respectively. Stomach was opened along the greater curvature then ulceration index was determined examining the inner lining of stomach. Oral administration of the extract at 1600 mg/kg did not produce toxic symptoms and mortality in mice. 2950 mg/kg was determined as the oral LD50. The HEGG (50-200 mg/kg) showed a significant reduction in ulcer index in HCl/Ethanol-induced ulcer. G. glabra extract (50-150 mg/kg) showed antiulcer activity against indomethacin-induced gastric lesions dose dependently. The extract effectively inhibited formation of gastric lesions induced by ethanol. The extract (200 mg/kg) was more potent than omeprazole (30 mg/kg). HEGG reduced the ulcer index in hypothermic stress induced gastric ulcers in mice and the antiulcer effect was comparable to that of cimetidine. The results indicated that G. glabra hydroalcoholic extract exerted an antiulcergenic effect that could be associated with increase in gastric mucosal defensive factors.

  19. Quality of Life in Arthritis Patients Using Nonsteroidal Anti-Inflammatory Drugs

    Directory of Open Access Journals (Sweden)

    Ingela Wiklund

    1999-01-01

    Full Text Available Arthritis is a painful and disabling condition. To suppress the pain and the inflammatory process, patients are often chronic nonsteroidal anti-inflammatory drug (NSAID users. Chronic use of NSAIDs may induce peptic ulcer, dyspeptic problems and heartburn. Therefore, these patients are often provided with treatment to relieve and/or protect against gastrointestinal problems. Rheumatic disorders also affect a range of health-related quality of life domains. In one study, patients with NSAID-associated gastroduodenal lesions complained about lack of energy, sleep disturbances, emotional distress and social isolation in addition to pain and mobility limitations. The degree of distress and dysfunction differed markedly from scores in an unselected population. Clinical trial data suggest that acid-suppressing therapy with omeprazole is superior to therapy with misoprostol and ranitidine in healing gastroduodenal lesions and preventing abdominal pain, heartburn and indigestion symptoms during continued NSAID treatment. Because arthritic patients are severely incapacitated by their condition regarding most aspects of health-related quality of life, it is important to offer a treatment that is effective in healing and preventing NSAID-induced ulcers and gastrointestinal symptoms during continued NSAID treatment without further compromising the patients’ quality of life. Treatment with omeprazole once daily has been shown to be superior to that with ranitidine and misoprostol in this respect.

  20. Gastroprotective effect of Benincasa hispida fruit extract

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    Rachchh Manish

    2008-01-01

    Full Text Available Objectives: The antiulcer activity of Benincasa hispida (Thunb. Cogn. fruit was evaluated in rats against ethanol-induced gastric mucosal damage, pylorus ligated (PL gastric ulcers, and cold restraint-stress (CRS-induced gastric ulcer models. Methods: Petroleum ether and methanol extracts were administrated orally at the dose of 300 mg/kg, and omeprazole (reference standard at the dose of 20 mg/kg. Ulcer index was common parameter studied in all the models. Further, vascular permeability was evaluated in ethanol model, and effect on lipid peroxidation, viz. melondialdehyde (MDA content, superoxide dismutase (SOD, and catalase (CAT levels were studied in CRS model. Results: Both the extracts produced significant reduction in ulcer index (P < 0.05 in all the models and the results were comparable with that of omeprazole-treated group. Further, significant reduction in vascular permeability (P < 0.05 was observed. In CRS model, MDA content was significantly reduced along with increase in CAT levels as compared to control group. Conclusions: Petroleum ether and methanol extracts of B. hispida possess significant antiulcer as well as antioxidant property.

  1. Improved dissolution and pharmacokinetic behavior of dipyridamole formulation with microenvironmental pH-modifier under hypochlorhydria.

    Science.gov (United States)

    Onoue, Satomi; Inoue, Ryo; Taniguchi, Chika; Kawabata, Yohei; Yamashita, Kazuhiro; Wada, Koichi; Yamauchi, Yukinori; Yamada, Shizuo

    2012-04-15

    The present study aimed to develop and characterize new formulations of dipyridamole (DP), a pH-dependent poorly soluble drug, employing an acidic pH-modifier for improving dissolution and absorption under hypochlorhydric condition. Granule formulations of DP (DPG) with and without fumaric acid (FA) were prepared with wet granulation, physicochemical properties of which were characterized focusing on morphology, dissolution and stability. Pharmacokinetic profiling of orally dosed DPG or DPG with 60% loading of FA (DPG/FA60) was carried out in omeprazole-treated rats as a hypochlorhydric model. Although pH-dependent dissolution behavior was observed in DPG, DPG/FA exhibited high rate and extent of dissolution in both acidic and neutral media. Complete supersaturation was achieved with a 2 h testing period in pH6.8 medium, and co-existing fumaric acid had no impact on the chemical/photochemical stability of DP in solid-state. After oral administration of DPG or DPG/FA60 (10 mg-DP/kg), there was ca. 40% reduction of AUC(0-3) for DPG in omeprazole-treated rats as compared to that in normal rats; however, AUC(0-3) for DPG/FA60 under hypochlorhydria was almost identical to that of DPG in normal rats. Given the improved systemic exposure early after oral administration in hypochlorhydric rats, the DPG/FA might provide better clinical outcomes in hypochlorhydric patients.

  2. The effects of acute hydrogen sulfide poisoning on cytochrome P450 isoforms activity in rats.

    Science.gov (United States)

    Wang, Xianqin; Chen, Mengchun; Chen, Xinxin; Ma, Jianshe; Wen, Congcong; Pan, Jianchun; Hu, Lufeng; Lin, Guanyang

    2014-01-01

    Hydrogen sulfide (H2S) is the second leading cause of toxin related death (after carbon monoxide) in the workplace. H2S is absorbed by the upper respiratory tract mucosa, and it causes histotoxic hypoxemia and respiratory depression. Cocktail method was used to evaluate the influences of acute H2S poisoning on the activities of cytochrome P450 isoforms CYP2B6, CYP2D6, CYP3A4, CYP1A2, CYP2C19, and CYP2C9, which were reflected by the changes of pharmacokinetic parameters of six specific probe drugs, bupropion, metoprolol, midazolam, phenacetin, omeprazole, and tolbutamide, respectively. The experimental rats were randomly divided into two groups, control group and acute H2S poisoning group (inhaling 300 ppm for 2 h). The mixture of six probes was given to rats by oral administration and the blood samples were obtained at a series of time points through the caudal vein. The concentrations of probe drugs in rat plasma were measured by LC-MS. The results for acute H2S poisoning and control groups were as follows: there was a statistically significant difference in the AUC and C max for bupropion, metoprolol, phenacetin, and tolbutamide, while there was no statistical pharmacokinetic difference for midazolam and omeprazole. Acute H2S poisoning could inhibit the activity of CYP2B6, CYP2D6, CYP1A2, and CYP2C9 in rats.

  3. Proton pump inhibitors induce a caspase-independent antitumor effect against human multiple myeloma.

    Science.gov (United States)

    Canitano, Andrea; Iessi, Elisabetta; Spugnini, Enrico Pierluigi; Federici, Cristina; Fais, Stefano

    2016-07-01

    Multiple Myeloma (MM) is the second most common hematological malignancy and is responsive to a limited number of drugs. Unfortunately, to date, despite the introduction of novel drugs, no relevant increase in survival rates has been obtained. Proton pump inhibitors (PPIs) have been shown to have significant antitumor action as single agents as well as in combination with chemotherapy. This study investigates the potential anti-tumor effectiveness of two PPIs, Lansoprazole and Omeprazole, against human MM cells. We found that Lansoprazole exerts straightforward efficacy against myeloma cells, even at suboptimal concentrations (50 µM), while Omeprazole has limited cytotoxic action. The Lansoprazole anti-MM effect was mostly mediated by a caspase-independent apoptotic-like cytotoxicity, with only a secondary anti-proliferative action. This study provides clear evidence supporting the use of Lansoprazole in the strive against MM with an efficacy proven much higher than current therapeutical approaches and without reported side effects. It is however conceivable that, consistent with the results obtained in other human tumors, Lansoprazole may well be combined with existing anti-myeloma therapies with the aim to improve the low level of efficacy of the current strategies.

  4. Helicobacter pylori: From Infection to Cure

    Directory of Open Access Journals (Sweden)

    ABR Thomson

    1996-01-01

    Full Text Available Over 380 abstracts, presentations and posters of recent advances were highlighted at the European and International Helicobacter pylori meeting held July 7 to 9, 1995 in Edinburgh, Scotland. New advances abound, with major interest focusing on the simple, safe, inexpensive new `gold standard’ for H pylori eradication therapy: a single week of tid omeprazole 20 mg, metronidazole 400 mg and clarithromycin 250 mg, or omeprazole 20 mg, amoxicillin 1000 mg and clarithromycin 500 mg. To avoid false negative results, two biopsies must be taken from the antrum and two from the gastric body at least four weeks after completion of eradication therapy, and ideally should be supplemented with at least one further H pylori test such as a biopsy for urease activity or culture, or a urea breath test. While most patients with a gastric or duodenal ulcer (DU who do not consume nonsteroidal anti-inflammatory drugs are infected with H pylori, the association is much less apparent in those with a DU who present with an upper gastrointestinal hemorrhage. H pylori eradication for nonulcer dyspepsia is not widely recommended, and the patient with a DU given effective H pylori eradication who presents with dyspepsia likely has erosive esophagitis rather than recurrent DU or H pylori. Gastroenterologists are at increased risk of H pylori infection, particularly older gastroenterologists who are very busy endoscopists.

  5. Mechanisms of Gastroprotective Effects of Ethanolic Leaf Extract of Jasminum sambac against HCl/Ethanol-Induced Gastric Mucosal Injury in Rats

    Directory of Open Access Journals (Sweden)

    Ahmed S. AlRashdi

    2012-01-01

    Full Text Available Jasminum sambac is used in folk medicine as the treatment of many diseases. The aim of the present investigation is to evaluate the gastroprotective effects of ethanolic extracts of J. sambac leaves against acidified ethanol-induced gastric ulcers in rats. Seven groups of rats were orally pre-treated with carboxymethylcellulose (CMC as normal group, CMC as ulcer group, 20 mg/kg of omeprazole as positive group, 62.5, 125, 250, and 500 mg/kg of extract as the experimental groups, respectively. An hour later, CMC was given orally to normal group and acidified ethanol solution was given orally to the ulcer control, positive control, and the experimental groups. The rats were sacrificed after an hour later. Acidity of gastric content, the gastric wall mucus, ulcer areas, and histology and immunohistochemistry of the gastric wall were assessed. Gastric homogenates were determined for prostaglandin E2 (PGE2, superoxide dismutase (SOD, andmalondialdehyde (MDA content. Ulcer group exhibited significantly severe mucosal injury as compared with omeprazole or extract which shows significant protection towards gastric mucosal injury the plant promotes ulcer protection as it shows significant reduction of ulcer area grossly, and histology showed marked reduction of edema and leucocytes infiltration of submucosal layer compared with ulcer group. Immunohistochemistry showed overexpression of Hsp70 protein and downexpression of Bax protein in rats pretreated with extract. Significant increased in the pH, mucus of gastric content and high levels of PGE2, SOD and reduced amount of MDA was observed.

  6. Mechanisms of Gastroprotective Effects of Ethanolic Leaf Extract of Jasminum sambac against HCl/Ethanol-Induced Gastric Mucosal Injury in Rats.

    Science.gov (United States)

    Alrashdi, Ahmed S; Salama, Suzy M; Alkiyumi, Salim S; Abdulla, Mahmood A; Hadi, A Hamid A; Abdelwahab, Siddig I; Taha, Manal M; Hussiani, Jamal; Asykin, Nur

    2012-01-01

    Jasminum sambac is used in folk medicine as the treatment of many diseases. The aim of the present investigation is to evaluate the gastroprotective effects of ethanolic extracts of J. sambac leaves against acidified ethanol-induced gastric ulcers in rats. Seven groups of rats were orally pre-treated with carboxymethylcellulose (CMC) as normal group, CMC as ulcer group, 20 mg/kg of omeprazole as positive group, 62.5, 125, 250, and 500 mg/kg of extract as the experimental groups, respectively. An hour later, CMC was given orally to normal group and acidified ethanol solution was given orally to the ulcer control, positive control, and the experimental groups. The rats were sacrificed after an hour later. Acidity of gastric content, the gastric wall mucus, ulcer areas, and histology and immunohistochemistry of the gastric wall were assessed. Gastric homogenates were determined for prostaglandin E(2) (PGE(2)), superoxide dismutase (SOD), andmalondialdehyde (MDA) content. Ulcer group exhibited significantly severe mucosal injury as compared with omeprazole or extract which shows significant protection towards gastric mucosal injury the plant promotes ulcer protection as it shows significant reduction of ulcer area grossly, and histology showed marked reduction of edema and leucocytes infiltration of submucosal layer compared with ulcer group. Immunohistochemistry showed overexpression of Hsp70 protein and downexpression of Bax protein in rats pretreated with extract. Significant increased in the pH, mucus of gastric content and high levels of PGE(2), SOD and reduced amount of MDA was observed.

  7. Disappearance of Helicobacter without Antibiotics in 12 Patients with Gastritis

    Directory of Open Access Journals (Sweden)

    Hugh James Freeman

    1997-01-01

    Full Text Available Detection of Helicobacter pylori in endoscopic gastric biopsies has been associated with a variety of diseases, including ulcers and gastritis. Although the natural history of H pylori in the gastric mucosa is unknown, antibiotic regimens have been used for eradication. Gastric biopsies from 6050 endoscopic procedures done by a single gastroenterologist from 1981 to 1994 were evaluated. Of these, 2860 from April 1, 1991 to September 30, 1994 had silver-stained biopsies to facilitate H pylori detection, and at least two upper endoscopic procedures were done with gastric biopsies in 188 patients. Twelve of the 188 patients with an initially positive H pylori gastric biopsy became H pylori-negative without antibiotic treatment for H pylori or other infection; 10 received omeprazole and two received no drug treatment. In two of the 12 patients recurrent H pylori in the gastric mucosa was also documented. These findings indicate that H pylori may disappear and reappear in the gastric mucosa with no specific antibiotic eradication regimen, although omeprazole may eradicate H pylori in vivo in some patients. The natural history of H pylori in gastric biopsies is poorly understood. Improved understanding, especially regarding the pathogenesis of upper gastrointestinal ulcerative and inflammatory disease processes, is essential before recommendations for specific antibiotic eradication regimens can be made.

  8. Use of bicarbonate buffer systems for dissolution characterization of enteric-coated proton pump inhibitor tablets.

    Science.gov (United States)

    Shibata, Hiroko; Yoshida, Hiroyuki; Izutsu, Ken-Ichi; Goda, Yukihiro

    2016-04-01

    The aim of this study was to assess the effects of buffer systems (bicarbonate or phosphate at different concentrations) on the in vitro dissolution profiles of commercially available enteric-coated tablets. In vitro dissolution tests were conducted using an USP apparatus II on 12 enteric-coated omeprazole and rabeprazole tablets, including innovator and generic formulations in phosphate buffers, bicarbonate buffers and a media modified Hanks (mHanks) buffer. Both omeprazole and rabeprazole tablets showed similar dissolution profiles among products in the compendial phosphate buffer system. However, there were large differences between products in dissolution lag time in mHanks buffer and bicarbonate buffers. All formulations showed longer dissolution lag times at lower concentrations of bicarbonate or phosphate buffers. The dissolution rank order of each formulation differed between mHanks buffer and bicarbonate buffers. A rabeprazole formulation coated with a methacrylic acid copolymer showed the shortest lag time in the high concentration bicarbonate buffer, suggesting varied responses depending on the coating layer and buffer components. Use of multiple dissolution media during in vitro testing, including high concentration bicarbonate buffer, would contribute to the efficient design of enteric-coated drug formulations. © 2016 Royal Pharmaceutical Society, Journal of Pharmacy and Pharmacology.

  9. Gastroesophageal reflux disease management according to contemporary international guidelines: a translational study.

    Science.gov (United States)

    Pace, Fabio; Riegler, Gabriele; de Leone, Annalisa; Dominici, Patrizia; Grossi, Enzo

    2011-03-07

    To test the Genval recommendations and the usefulness of a short trial of proton pump inhibitor (PPI) in the initial management and maintenance treatment of gastroesophageal reflux disease (GERD) patients. Five hundred and seventy seven patients with heartburn were recruited. After completing a psychometric tool to assess quality of life (PGWBI) and a previously validated GERD symptom questionnaire (QUID), patients were grouped into those with esophagitis (EE, n = 306) or without mucosal damage (NERD, n = 271) according to endoscopy results. The study started with a 2-wk period of high dose omeprazole (omeprazole test); patients responding to this PPI test entered an acute phase (3 mo) of treatment with any PPI at the standard dose. Finally, those patients with a favorable response to the standard PPI dose were maintained on a half PPI dose for a further 3-mo period. The test was positive in 519 (89.9%) patients, with a greater response in EE patients (96.4%) compared with NERD patients (82.6%) (P = 0.011). Both the percentage of completely asymptomatic patients, at 3 and 6 mo, and the reduction in heartburn intensity were significantly higher in the EE compared with NERD patients (P management of GERD patients. In addition, we observed that the overall response to PPI therapy is lower in NERD compared to EE patients.

  10. Efficacy of rebamipide for low-dose aspirin-related gastrointestinal symptoms.

    Science.gov (United States)

    Mizukami, Kazuhiro; Murakami, Kazunari; Hirashita, Yuka; Hisamatsu, Akari; Ogawa, Ryo; Uchida, Masahiro; Nakagawa, Yoshifumi; Okimoto, Tadayoshi; Kodama, Masaaki; Fujioka, Toshio

    2012-11-01

    Gastrointestinal symptoms are a problematic issue for patients who take low-dose aspirin for long time. We conducted a pilot study to investigate the efficacy of combination therapy with proton pump inhibitor and rebamipide. This was a prospective, randomized, double-blind, placebo-controlled cross-over study. All the subjects received aspirin 100 mg and omeprazole 20 mg. The subjects were divided into two groups and received either rebamipide 300 mg or placebo, which was prescribed for 4 weeks. The subjects were instructed to record their gastrointestinal symptom rating scale before the study and 1 and 4 weeks after beginning the protocol. These scores of the groups were compared before and after the treatment to evaluate the severity of their symptoms and the number of symptom items present in each group. For the subjects receiving rebamipide, the total prevalence of lower gastrointestinal symptoms was significantly different from the placebo group (p=0.0093) at week 4. No troublesome symptoms were observed in the rebamipide group. Inconclusion, the administration of rebamipide prevented the occurrence of troublesome symptoms, especially lower gastrointestinal symptoms, in patients taking aspirin and omeprazole. Rebamipide is a candidate drug for combination therapy with proton pump inhibitors to prevent low-dose aspirin-induced gastrointestinal symptoms.

  11. Positive clinical response to clopidogrel is independent of paraoxonase 1 Q192R and CYP2C19 genetic variants.

    Science.gov (United States)

    Martínez-Quintana, Efrén; Medina-Gil, José M; Rodríguez-González, Fayna; Garay-Sánchez, Paloma; Limiñana, José M; Saavedra, Pedro; Tugores, Antonio

    2014-08-01

    There is increasing controversy about the influence of serum paraoxonase type 1 and cytochrome CYP2C19 in the conversion of clopidogrel to its pharmaceutically active metabolite. The effect of concomitant medication with the proton pump inhibitor omeprazole has been also subject of intense scrutiny. We present a cohort of 263 patients receiving anti-platelet aggregation treatment with clopidogrel and aspirin for 1 year. The paraoxonase 1 gene Q192R variant along with the presence of CYP2C19*2 and *3 loss of function alleles, concomitant medication with proton pump inhibitors and known cardiovascular risk factors were examined to determine their influence in disease relapse due to an ischaemic event during the 12 month treatment period. The low number of patients suffering a relapse (20 out of 263), indicates that double anti-aggregation therapy with aspirin and clopidogrel was very effective in our patients. Among the relapsers, evidence of coronary heart disease was the most influencial factor affecting response to therapy, while the presence of the paraoxonase 1 Q192R variant, loss of function of CYP2C19, and concomitant medication with omeprazole were non-significant.

  12. Expression comparison of azithromycin and clarithromycin in triple-therapy regimens for eradication of Helicobacter pylori in hemodialysis patients

    Directory of Open Access Journals (Sweden)

    Jamshid Vafaeimanesh

    2014-01-01

    Full Text Available To compare a triple-therapy regimen based on change of antibiotic (azithromycin and clarithromycin for the eradication of Helicobacter pylori in hemodialysis (HD patients, we studied in a prospective, randomized, double-blinded clinical trial 39 patients who had dyspepsia and showed two positive results from the diagnostic tests of H. pylori infection including anti-H. pylori serology and stool antigen (HpSAg and urease breath test (UBT. The patients were divided into two groups: Group-A received omeprazol 20 mg, amoxycilin 500 mg and clarithromycin 500 mg twice a day and Group-B received omeprazol 20 mg, amoxicillin 500 mg and azithromycin 250 mg twice a day. The adverse events and compliance with triple therapy were reviewed at one visit per week. Both groups were prescribed their medications for 14 days. Of the 39 patients, only 37 patients completed the treatment schedule (20 men and 19 women, with the mean being 59 years. Two patients died due to myocardial infarction before the start of treatment and were out of the study. The eradication rate of H. pylori, evaluated by negative results of UBT, was 82.4% in Group-A and 80% in Group-B (P-value = 1.0. The results of our study showed no significant difference of azitromycin versus claritromycin in the eradication of H. pylori infection in HD patients.

  13. A new gastric ulcer model induced by ischemia-reperfusion in the rat: role of leukocytes on ulceration in rat stomach.

    Science.gov (United States)

    Wada, K; Kamisaki, Y; Kitano, M; Kishimoto, Y; Nakamoto, K; Itoh, T

    1996-01-01

    A new model of gastric ulcer involving damage to the muscularis mucosae was developed by clamping the celiac artery in rat to induce ischemia-reperfusion (I-R) injury. Although erosions with falling off of the gastric mucosa were observed immediately, 24 and 36 hours after the I-R, gastric ulcers involving the injury of muscularis mucosae were observed in the area of gastric glands at 48 and 72 hours after initiation of injury. Administration of omeprazol, a proton pump inhibitor, or pentoxifylline, an anti-leukocyte drug, just after the initiation of injury significantly decreased the total area of ulcers at 72 hours. A combination of omeprazol and pentoxifylline was more effective than either drug alone. An anti-leukocyte adhesion molecule (anti-CD18 antibody) also showed significant inhibitory effect on the development of ulcers at 72 hours and the infiltration of leukocytes into both submucosa and mucosa. These results indicate that in our model, gastric acid together with leukocytes contribute to the development of ulcers following erosions. This model may be used to investigate the mechanisms of the development of gastric ulcer and evaluate antiulcer drugs in a preclinical setting.

  14. 质子泵抑制剂的研究和临床应用进展

    Institute of Scientific and Technical Information of China (English)

    马丽群

    2012-01-01

    @@ 质子泵抑制剂(proton pump inhibitors,PPI)即H+/K+-ATP酶抑制剂, PPI为苯并咪唑类衍生物,20世纪80年代,第1个PPI奥美拉唑(omeprazole)出现以来,PPI己成为胃酸相关性疾病治疗的主要药物[1].目前PPI药物主要有奥美拉唑(omeprazole)、兰索拉唑(1ansoprazole)、泮托拉唑(pantoprazole)、雷贝拉唑(rabeprazole)、埃索美拉唑(esomeprazole)、瑞伐拉赞(revaprazan)、艾普拉唑(ilaprazole)、右兰索拉唑(dex1ansoprazole).此外,有的化合物正处于临床或临床前研究中,如艾沙拉唑(Esaprazole),二硫拉唑(Disuprazole).本文就PPI的研究及其临床应用作一简要综述.

  15. Expression comparison of azithromycin and clarithromycin in triple-therapy regimens for eradication of Helicobacter pylori in hemodialysis patients.

    Science.gov (United States)

    Vafaeimanesh, Jamshid; Jalalzadeh, Mojgan; Nazarian, Morteza

    2014-01-01

    To compare a triple-therapy regimen based on change of antibiotic (azithromycin and clarithromycin) for the eradication of Helicobacter pylori in hemodialysis (HD) patients, we studied in a prospective, randomized, double-blinded clinical trial 39 patients who had dyspepsia and showed two positive results from the diagnostic tests of H. pylori infection including anti-H. pylori serology and stool antigen (HpSAg) and urease breath test (UBT). The patients were divided into two groups: Group-A received omeprazol 20 mg, amoxycilin 500 mg and clarithromycin 500 mg twice a day and Group-B received omeprazol 20 mg, amoxicillin 500 mg and azithromycin 250 mg twice a day. The adverse events and compliance with triple therapy were reviewed at one visit per week. Both groups were prescribed their medications for 14 days. Of the 39 patients, only 37 patients completed the treatment schedule (20 men and 19 women, with the mean being 59 years). Two patients died due to myocardial infarction before the start of treatment and were out of the study. The eradication rate of H. pylori, evaluated by negative results of UBT, was 82.4% in Group-A and 80% in Group-B (P-value = 1.0). The results of our study showed no significant difference of azitromycin versus claritromycin in the eradication of H. pylori infection in HD patients.

  16. 三联疗法治疗幽门螺杆菌相关性胃炎的临床分析%Clinical Analysis of Triple Therapy in the Treatment of Helicobacter Pylori-related Gastritis

    Institute of Scientific and Technical Information of China (English)

    邹庆伟

    2015-01-01

    Objective:To observe the curative effect of Omeprazole and Esomeprazole triple therapy for Helicobacter pylori(Hp) associated gastritis. Method:280 Hp positive patients with chronic gastritis in our hospital from June 2013 to May 2014 were selected,they were divided into the Omeprazole group and the Esomeprazole group according to the random number table method,140 cases in each group.The Omeprazole group was taken with Omeprazole, Amoxicillin and Levofloxacin for treatment.The Esomeprazole group was taken with Esomeprazole,Amoxicillin and Levofloxacin for treatment.The Hp cure rates and differences in clinical symptoms and histological improvement between the two groups were observed and compared.Result:Hp eradication rate of the Esomeprazole group was 81.43%(114/140),which was significantly higher than 69.29%(97/140) of the Omeprazole group,the clinical control rate and total effective rate of clinical symptoms improvement in the Esomeprazole group were 22.86%and 92.14%,which were significantly higher than 14.29%and 76.43%in the Omeprazole group,the clinical control rate and total effective rate of histological improvement in the Esomeprazole group were 29.29%and 65.00%,which were significantly higher than 17.86%and 50.71%in the Omeprazole group,the differences were statistically significant(P<0.05).Conclusion:The Esomeprazole triple therapy in the treatment of Helicobacter pylori-associated gastritis can effectively improve the Hp eradication rate,promote the improvement of clinical symptoms and pathological histology,and its curative effect is better than that of omeprazole triple therapy,is worthy of clinical promotion.%目的:观察奥美拉唑和埃索美拉唑三联疗法治疗幽门螺杆菌(Hp)相关性胃炎的疗效。方法:选取笔者所在医院2013年6月-2014年5月收治的280例Hp阳性的慢性胃炎患者,按照随机数字表法将其分为奥美拉唑组和埃索美拉唑组,各140例。奥美拉唑组采用奥美拉唑、左氧氟

  17. Ten-day bismuth-containing quadruple therapy is effective as first-line therapy for Helicobacter pylori-related chronic gastritis: a prospective randomized study in China.

    Science.gov (United States)

    Wang, L; Lin, Z; Chen, S; Li, J; Chen, C; Huang, Z; Ye, B; Ding, J; Li, W; Wu, L; Jiang, Y; Meng, L; Du, Q; Si, J

    2017-06-01

    To investigate the effectiveness of 10-day bismuth-containing quadruple (B-quadruple) treatment as first-line therapy in patients with Helicobacter pylori-related chronic gastritis. A randomized controlled trial was conducted from October 2011 to December 2013 in Zhejiang, China, including patients with H. pylori-related chronic gastritis who were randomly provided either 10-day omeprazole-based triple therapy (OM-triple; omeprazole 20 mg twice daily, clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily) or 10-day B-quadruple therapy (OM-triple + bismuth subcitrate 120 mg four times daily). H. pylori status, pathologic findings and dyspeptic symptoms were assessed at baseline and after 3 months. The primary outcome was H. pylori eradication rates by intention-to-treat (ITT) and per-protocol (PP) analyses. The secondary outcomes were the histologic and symptomatic benefits from H. pylori eradication. A total of 351 patients with H. pylori-related chronic gastritis were recruited. The eradication rates of the OM-triple and B-quadruple groups were 58.4% (108/185) and 86.1% (143/166) respectively according to ITT analysis (p pylori eradication were 63.2% (108/171) and 92.3% (143/155) respectively (p pylori-induced chronic gastritis in China. Copyright © 2017 The Authors. Published by Elsevier Ltd.. All rights reserved.

  18. Mechanisms behind changes in gastric acid and bicarbonate outputs during the human interdigestive motility cycle.

    Science.gov (United States)

    Dalenbäck, J; Fändriks, L; Olbe, L; Sjövall, H

    1996-01-01

    Human gastric interdigestive acid and bicarbonate outputs vary cyclically in association with the migrating motor complex (MMC). These phenomena were studied in 26 healthy volunteers by constant-flow gastric perfusion, with continuous recording of pH and Pco2 in mixed gastric effluent and concomitant open-tip manometry of gastroduodenal motility. Stable acid and bicarbonate outputs were registered during less than 50% of the MMC cycle. Acid secretion started to increase 71 +/- 3% into the cycle, with maximum output during antral phase III. Bicarbonate output increased biphasically 1) 40 +/- 5% into the cycle, coinciding with reflux of bile, and 2) at the end of duodenal phase III when the aspirate was devoid of bile. The bicarbonate peak associated with phase III was abolished by atropine (0.01 mg/kg iv, n = 8) and by pyloric occlusion (n = 9) but remained unchanged after omeprazole (n = 10). The acid peak was abolished by both atropine and omeprazole. It is concluded that the MMC-related changes in acid and alkaline outputs represent two different and independent phenomena. Acid secretion cyclicity is due to periodical variations in cholinergic stimulation of the parietal cells. In contrast, the phase III-associated increase in bicarbonate output is due to duodenogastric reflux.

  19. [Effect of mild irritants on gastric outputs of bicarbonates and pepsinogen depends on the rate of acid secretion].

    Science.gov (United States)

    Zolotarev, V A; Andreeva, Iu V; Khropycheva, R P

    2012-06-01

    The aggressive luminal content in the stomach activates gastroprotective processes affecting exocrine and endocrine secretion of gastric glands and permeability of the pre-epithelial mucus layer. The aim of the study was to investigate effects of chemical irritants similar to physiological characteristics of digestion (pH 2.0 and/or 500 mM NaCl) on outputs of bicarbonates and pepsinogen as well as assess the role of endogenous acid production in control ofnon-parietal secretion during irritation of the gastric mucosa. In experiments on conscious rats with chronic gastric fistula as well as on anesthetized animals it was demonstrated that luminal infusion of acidic hyperosmotic solution of NaCl enhances basal secretions of bicarbonates and pepsinogen that was fully blocked by indomethacin. Suppression of gastric acid secretion by omeprazole potentiates the stimulative effect of mild irritants likely due to the reduction of pH gradient on the surface of gastric mucosa which causes the growth of sensitivity of the epithelium to chemical stimuli and the increase of synthesis ofprostaglandins. Additionally, mild irritation enhances secretion of HCO3(-) and pepsinogen induced by stimulation of the vagus nerve; and this response does not depend on the action ofprostaglandins. The enhancing effect of irritation on the vagally induced bicarbonate output was eliminated after the treatment with omeprazole.

  20. Intrahypothalamic corticotropin-releasing factor elevates gastric bicarbonate and inhibits stress ulcers in rats.

    Science.gov (United States)

    Gunion, M W; Kauffman, G L; Taché, Y

    1990-01-01

    The effects of intrahyopthalamic microinfusions of corticotropin-releasing factor (CRF) on gastric bicarbonate, acid, and pepsin content and on cold restraint-induced gastric lesion formation were tested in three experiments. Bilateral microinfusions of CRF into the hypothalamic ventromedial nucleus (0.86 nmol/rat) significantly increased both gastric bicarbonate concentration and total bicarbonate output. These effects were observed irrespective of whether rats were pretreated with the acid antisecretory drug omeprazole. In nonomeprazole-pretreated rats, CRF microinfusions also significantly reduced acid secretion and raised pH. The increase in bicarbonate content accounted for half of the observed decrease in acid output, suggesting that CRF microinfusions activated separable bicarbonate-stimulating and acid-inhibiting hypothalamic systems. In non-omeprazole-pretreated rats, CRF microinfusions significantly increased serum gastrin, whereas pepsin output was unchanged. Gastric mucosal damage produced by 4 h of cold restraint was significantly diminished by CRF microinfusion into the ventromedial hypothalamus. These data demonstrate that ventromedial hypothalamic microinfusions of CRF increase bicarbonate content, decrease gastric acid content, and confer protection against cold restraint-induced gastric mucosal damage. Hypothalamic CRF neuronal terminals and receptors may be involved in the central regulation of gastric bicarbonate secretion as well as acid secretion.

  1. Review article: similarities and differences among delayed-release proton-pump inhibitor formulations.

    Science.gov (United States)

    Horn, J R; Howden, C W

    2005-12-01

    Proton-pump inhibitors are acid-labile, and require an enteric coating to protect them from degradation in the stomach when given orally. However, this leads to delayed absorption and onset of action of the proton-pump inhibitor. This article aims to review the similarities and differences between the various formulations of delayed release proton-pump inhibitors. Delayed-release omeprazole and delayed-release lansoprazole have been suspended in sodium bicarbonate for tube administration; however, for omeprazole, absorption is further impaired and antisecretory effects are disappointing. Although such formulations may be more convenient for clinical use in certain patient groups, absorption of the proton-pump inhibitor is still influenced by residual enteric coating. There are few differences among the currently available delayed-release proton-pump inhibitors with respect to their pharmacodynamic effects during chronic administration. There are minor formulation-based pharmacokinetic differences among these agents, primarily reflected in their bioavailability following the first few doses. Differences in bioavailability may explain slight differences in the rate of onset of maximal antisecretory effect. However, minor pharmacodynamic and pharmacokinetic differences are not associated with meaningful differences in clinical outcomes.

  2. Review article: prevention of stress-related mucosal bleeding with proton-pump inhibitors.

    Science.gov (United States)

    Maton, P N

    2005-12-01

    Stress-related gastric mucosal bleeding occurs in a substantial number of critically ill patients, with clinically important gastrointestinal bleeding prolonging intensive care stay and increasing mortality. This paper reviews the role of proton-pump inhibitors in the prevention of stress-related mucosal bleeding. Bleeding prophylaxis appears to be warranted in patients in intensive care units on mechanical ventilation or those who have coagulopathy. Intravenous histamine H2 receptor antagonists, particularly cimetidine, have demonstrated efficacy for the prevention of bleeding in critically ill patients. Standard delayed-release proton-pump inhibitors have not been extensively studied in this patient group, but there are some data to support their efficacy in increasing intragastric pH, and in the case of intravenous pantoprazole in preventing gastrointestinal bleeding. In a large, randomized controlled trial, immediate-release omeprazole [(IR-OME) Zegerid powder for oral suspension; Santarus Inc., San Diego, CA, USA] administered via gastric tube, was as effective as intravenous cimetidine in the prevention of clinically significant bleeding, and more effective in increasing gastric pH. Effective antisecretory therapy does not appear to increase the risk of nosocomial pneumonia. In conclusion, immediate-release omeprazole provides a safe and effective alternative to intravenous cimetidine for the prevention of stress-related mucosal bleeding in critically ill patients.

  3. Quadruple therapy with furazolidone for retreatment in patients with peptic ulcer disease

    Institute of Scientific and Technical Information of China (English)

    Guilherme Eduardo Goncalves Felga; Fernando Marcuz Silva; Ricardo Correa Barbuti; Tomás Navarro-Rodriguez; Schlioma Zaterka; Jaime Natan Eisig

    2008-01-01

    AIM: To establish the efficacy and safety of a 7-d therapeutic regimen using omeprazole, bismuth subcitrate, furazolidone and amoxicillin in patients with peptic ulcer disease who had been previously treated with other therapeutic regimens without success.METHODS: Open cohort study which included patients with peptic ulcer who had previously been treated unsuccessfully with one or more eradication regimens. The therapeutic regimen consisted of 20 mg omeprazole, 240 mg colloidal bismuth subcitrate, 1000 mg amoxicillin, and 200 mg furazolidone, taken twice a day for 7 d. Patients were considered as eradicated when samples taken from the gastric antrum and corpus 12 wk after the end of treatment were negative for Helicobacter pylori (H pylori) (rapidurease test and histology). Safety was determined by the presence of adverse effects. RESULTS: Fifty-one patients were enrolled. The eradication rate was 68.8% (31145). Adverse effects were reported by 31.4% of the patients, and these were usually considered to be slight or moderate in the majority of the cases. Three patients had to withdraw from the treatment due to the presence of severe adverse effects. CONCLUSION: The association of bismuth, furazolidone, amoxicillin and a proton-pump inhibitor is a valuable alternative for patients who failed to respond to other eradication regimens. It is an effective, cheap and safe option for salvage therapy of positive patients.

  4. Thymoquinone: Novel gastroprotective mechanisms.

    Science.gov (United States)

    Magdy, Mahmoud-Awny; Hanan, El-Abhar; Nabila, El-Maraghy

    2012-12-15

    Ample of evidence proved the gastroprotective effect of thymoquinone (TQ), the main constituent of Nigella sativa oil; however, the full mechanistic cassette on the gastric ulcer etiopathogenesis is not fully elucidated. The aim of the present work is to unveil some of the possible mechanisms. Animals were injected with vehicle, TQ (10 & 20mg/kg), omeprazole (10 & 20mg/kg) or their combination (10mg/kg). Thirty minutes later, pyloric ligation was carried out and followed consequently with ischemia for another 30min, abided by reperfusion for 120min. The ischemia/reperfusion insult increased the gastric acid secretion, acid output, and pepsin, as well as the gastric mucosal content/activity of lipid peroxide, proton pump and myeloperoxidase, along with ulcer index. However, content/activity of gastric mucin, reduced glutathione, total nitric oxide, and superoxide dismutase were decreased. TQ, especially the high dose level, corrected the altered parameters in a comparable manner to that of the reference drug used, omeprazole. In addition, when the low doses were combined they add to each other to reach the effect of the high dose of either drug. These results showed that apart from its known antioxidant properties, TQ has novel gastroprotective mechanisms via inhibiting proton pump, acid secretion and neutrophil infiltration, while enhancing mucin secretion, and nitric oxide production.

  5. Inhibitory effects of kale ingestion on metabolism by cytochrome P450 enzymes in rats.

    Science.gov (United States)

    Yamasaki, Izumi; Yamada, Masayoshi; Uotsu, Nobuo; Teramoto, Sachiyuki; Takayanagi, Risa; Yamada, Yasuhiko

    2012-01-01

    Kale (Brassica oleracea L. var acephala DC) is a leafy green vegetable belonging to the cabbage family (Brassicaceae) that contains a large amount of health-promoting phytochemicals. There are any reports about the effects of kale ingestion on the chemoprevention function and mechanism, but the interactions between kale and drugs have not been researched. We investigated the effects of kale intake on cytochrome P450 (CYP) metabolism by using cocktail probe drugs, including midazolam (for CYP3A4), caffeine (for CYP1A2), dextromethorphan (for CYP2D6), tolbutamide (for CYP2C9), omeprazole (for CYP2C19), and chlorzoxazone (for CYP2E1). Cocktail drugs were administered into rats treated with kale and cabbage (2000 mg/kg) for a week. The results showed that kale intake induced a significant increase in plasma levels and the AUC of midazolam, caffeine, and dextromethorphan. In addition, the plasma concentration and AUC of omeprazole tended to increase. Additionally, no almost differences in the mRNA expression levels of CYP enzymes in the liver were observed. In conclusion, kale ingestion was considered to have an inhibitory effect on the activities of CYP3A4, 1A2, 2D6, and 2C19 for a reason competitive inhibition than inhibitory changes in the mRNA expressions.

  6. Melatonin and steroid hormones activate intermembrane Cu,Zn-superoxide dismutase by means of mitochondrial cytochrome P450.

    Science.gov (United States)

    Iñarrea, Pedro; Casanova, Alvaro; Alava, Maria Angeles; Iturralde, María; Cadenas, Enrique

    2011-06-01

    Melatonin and steroid hormones are cytochrome P450 (CYP or P450; EC 1.14.14.1) substrates that have antioxidant properties and mitochondrial protective activities. The mitochondrial intermembrane space (IMS) Cu,Zn-superoxide dismutase (SOD1) is activated after oxidative modification of its critical thiol moieties by superoxide anion (O₂(•-)). This study was aimed at investigating the potential association between the hormonal protective antioxidant actions in mitochondria and the regulation of IMS SOD1 activity. Melatonin, testosterone, dihydrotestosterone, estradiol, and vitamin D induced a sustained activation over time of SOD1 in intact mitochondria, showing a bell-shaped enzyme activation dose response with a threshold at 50nM and a maximum effect at 1μM concentration. Enzyme activation was not affected by furafylline, but it was inhibited by omeprazole, ketoconazole, and tiron, thereby supporting the occurrence of a mitochondrial P450 activity and O₂(•-) requirements. Mitochondrial P450-dependent activation of IMS SOD1 prevented O₂(•-)-induced loss of aconitase activity in intact mitochondria respiring in State 3. Optimal protection of aconitase activity was observed at 0.1μM P450 substrate concentration, evidencing a likely oxidative effect on the mitochondrial matrix by higher substrate concentrations. Likewise, enzyme activation mediated by mitochondrial P450 activity delayed CaCl₂-induced loss of transmembrane potential and decreased cytochrome c release. Omeprazole and ketoconazole abrogated both protecting mitochondrial functions promoted by melatonin and steroid hormones.

  7. Pharmacotherapy of Peptic Ulcer Disease

    Directory of Open Access Journals (Sweden)

    F Molina

    1991-01-01

    Full Text Available The etiology of peptic ulcer is multifactorial; except for omeprazole, all drugs used for the treatment of peptic ulcer result in healing with no statistical difference at four weeks. The healing rare increases with time for active medication and placebo, and is lower among smokers than nonsmokers for all drugs but misoprostol. Mucosal protectives (or ‘cytoprotectives’ as a group seem to have a lower relapse rate than the H2 receptor antagonists at one year. Combination therapy has not yet proved to be better than single drug therapy; however, the number of studies is still small, and more clinical trials are necessary. Resistant ulcers have demonstrated that acid is one of several etiological factors and that more research is needed to elucidate the reason(s for refractoriness. The choice of therapeutic agent is generally made according to patient compliance, medication cost, side effects, effectiveness, relapse rate and physician experience with the drug. Long term maintenance therapy is effective in the prevention of ulcer relapse and is especially recommended for selected patient groups, including patients with recurrent or bleeding ulcer, patients with concomitant nonsteroidal anti-inflammatory drug use, and elderly women. Omeprazole is the treatment of choice for moderate to severe esophagitis and should be reserved for large and resistant ulcers.

  8. Which is the best choice for gastroesophageal disorders:Melatonin or proton pump inhibitors?

    Institute of Scientific and Technical Information of China (English)

    Joanna; Dulce; Favacho; de; Oliveira; Torres; Ricardo; de; Souza; Pereira

    2010-01-01

    Melatonin is used in many countries to improve sleep disorders.Melatonin is a hormone produced by the pineal gland and enterochromaff in cells which control sleep and gastrointestinal motility.Low levels of melatonin lead to gastroesophageal reflux disease(GERD).Most of patients with GERD have a sleep disorder.So,low melatonin levels is the main cause of insomnia.Beyond this,it has an inhibitory action on gastric acid secretion and seems to control the lower esophageal sphincter.Proton pump inhibitors(PPIs) are a group of drugs whose main action is a pronounced and long-lasting reduction of gastric acid production.They are the most potent inhibitors of acid secretion available today.Omeprazole(one of the PPIs) and melatonin have similarities in their chemical structures.Therefore,we could consider omeprazole as a rough copy of melatonin.In this paper,we compare the advantages and disadvantages of the clinical use of melatonin and PPIs.

  9. Antiulcer activity of aqueous extract of leaves ofMadhuca indica J. F. Gmel against naproxen induced gastric mucosal injury in rats

    Institute of Scientific and Technical Information of China (English)

    Smeeta M Mohod; Subhash L Bodhankar

    2013-01-01

    Objective:To evaluate antiulcer potential of aqueous extract ofMadhuca indica(M. indica)J. F.Gmel leaves in rats.Methods:Aqueous extract of M. indicaJ.F.Gmel leaves was tested at the dose of100,200 and400 mg/kg, p.o. against naproxen(30 mg/kg, p.o) induced gastric ulcer. Omeprazole(30 mg kg, p.o.) was used as a positive standard.Ulcerated area was measured by ImageJ software.Various antioxidant parameter likeSOD,GSH,MDA,MPO,NO and histamine were also determined.Results:After4 week treatment period, desired aim was achieved using aqueous extract of plant ofM. indica at the dose of200 and400 mg/kg, p.o.(P<0.01, P<0.001) showed significant reduction in ulcerated area and ulcer index as compared to control group. Omeprazole(30 mg/kg, p.o.) was more effective in reducing ulcerated area after30 days treatment period.In addition,SOD,GSH,NO significantly increased;MDA,MPO content significantly lowered when compared with control group.Histamine content didn’t show any significant change at all the three doses.Conclusions:Our finding suggests that aqueous extract ofM. indicaJ.F. Gmel leaves is effective in gastric ulcer protection.

  10. The Effects of Acute Hydrogen Sulfide Poisoning on Cytochrome P450 Isoforms Activity in Rats

    Directory of Open Access Journals (Sweden)

    Xianqin Wang

    2014-01-01

    Full Text Available Hydrogen sulfide (H2S is the second leading cause of toxin related death (after carbon monoxide in the workplace. H2S is absorbed by the upper respiratory tract mucosa, and it causes histotoxic hypoxemia and respiratory depression. Cocktail method was used to evaluate the influences of acute H2S poisoning on the activities of cytochrome P450 isoforms CYP2B6, CYP2D6, CYP3A4, CYP1A2, CYP2C19, and CYP2C9, which were reflected by the changes of pharmacokinetic parameters of six specific probe drugs, bupropion, metoprolol, midazolam, phenacetin, omeprazole, and tolbutamide, respectively. The experimental rats were randomly divided into two groups, control group and acute H2S poisoning group (inhaling 300 ppm for 2 h. The mixture of six probes was given to rats by oral administration and the blood samples were obtained at a series of time points through the caudal vein. The concentrations of probe drugs in rat plasma were measured by LC-MS. The results for acute H2S poisoning and control groups were as follows: there was a statistically significant difference in the AUC and Cmax for bupropion, metoprolol, phenacetin, and tolbutamide, while there was no statistical pharmacokinetic difference for midazolam and omeprazole. Acute H2S poisoning could inhibit the activity of CYP2B6, CYP2D6, CYP1A2, and CYP2C9 in rats.

  11. Experimental model in the qualitative and quantitative assessment of non-Helicobacter gastric microflora under proton pump inhibitors action Modelo experimental na avaliação qualitativa e quantitativa da microflora gástrica não-Helicobacter sob ação de inibidores de bomba de próton

    Directory of Open Access Journals (Sweden)

    Augusto Diogo Filho

    2006-10-01

    Full Text Available PURPOSE: To evaluate models of gastric material collection from Wistar rats with and without using proton pump inhibitors(PPIs. METHODS: Twenty-four rats underwent intraperitoneal omeprazol treatment, and other 12 received similar treatment with 0.9% saline. All animals underwent collection of gastric material samples, after stomach removal, by either biopsies, or aspirates, or swabs. Samples were bacteriologically processed in order to identify species and strains. Values are described as natural logarithm of colony former units per mL [Ln(CFU/mL]. Kruskal-Wallis and Mann-Whitney non-parametric tests were used, and pOBJETIVO: Avaliar modelos de coleta de material gástrico de ratos da linhagem Wistar, com e sem o uso de inibidores de bomba de próton (IBPs. MÉTODOS: 24 ratos foram submetidos a tratamento com omeprazol intraperitoneal e 12 outros ratos receberam tratamento semelhante com solução salina a 0,9%. Os animais foram submetidos a coleta de amostras de material gástrico, após retirada do estômago, utilizando-se de biópsias, aspirados ou swabs. Os materiais obtidos foram processados bacteriologicamente para identificação de espécimes quanto ao gênero. Os valores são descritos em logaritmo natural das unidades formadoras de colônias por mL [Ln(UFC/mL]. Utilizou-se os testes não-paramétricos de Kruskal-Wallis e Mann-Whitney, considerando-se p<0,05 como estatisticamente significativo. RESULTADOS: Não se observou diferença significativa da quantidade de Ln(UFC/mL entre os três métodos de coleta, independente do uso de omeprazol. Também não se observou diferença significativa de Ln(UFC/mL ao comparar-se os métodos individualmente entre si nas condições de uso de omeprazol ou placebo. Houve aumento significativo da variedade de gêneros de bactérias com o uso de IBP, nos 3 métodos de coleta, sendo isto mais perceptível na biópsia e swab. CONCLUSÃO: Não houve diferença entre os três métodos de coleta de

  12. Prophylactic effects of Clausena excavata Burum. f. leaf extract in ethanol-induced gastric ulcers

    Directory of Open Access Journals (Sweden)

    Albaayit SFA

    2016-06-01

    Full Text Available Shaymaa Fadhel Abbas Albaayit,1,2 Yusuf Abba,3 Rasedee Abdullah,4 Noorlidah Abdullah1 1Faculty of Science, Institute of Biological Sciences, University of Malaya, Kuala Lumpur, Malaysia; 2Department of Biology, College of Science, University of Baghdad, Baghdad, Iraq; 3Department of Veterinary Pathology and Microbiology, 4Department of Veterinary Laboratory Diagnosis, Faculty of Veterinary Medicine, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Abstract: Clausena excavata is a natural herb with both antioxidant and anti-inflammatory properties. It has been used for decades in folkloric practice for the amelioration of various ailments. In this study, the gastroprotective activity of methanolic extract of C. excavata leaves (MECE was determined in the Sprague Dawley rat ethanol-induced gastric ulcer model. Rats were pretreated with a single dose of vehicle (5% Tween 20, 20 mg/mL omeprazole, 400 and 200 mg/mL of MECE dissolved in 5% Tween 20. Ulcer was induced with 5 mL/kg of ethanol and stomach tissue was obtained after 1 hour. Histological examination was done on hematoxylin and eosin, periodic acid-Schiff, and immunochemically stained gastric mucosal tissues. Prostaglandin E2, superoxide dismutase, catalase, glutathione peroxidase, and lipid peroxidation levels of the gastric tissue homogenates were also determined. Significantly (P<0.05 smaller ulcer areas, less intense edema, and fewer leukocytes’ infiltration were observed in MECE- and omeprazole-treated than in untreated gastric mucosa with ulcer. The gastric pH, mucus production, superoxide dismutase, catalase, and glutathione peroxidase contents increased, while the lipid peroxidation content decreased as a result of MECE treatment. Bcl-2-associated X protein was underexpressed, while heat shock protein 70 and transforming growth factor-beta protein were overexpressed in the ulcerated gastric mucosa tissues treated with omeprazole and MECE. Similarly, there was a reduction in

  13. Comparison of clinical effect of different triple therapy for helicobacter pylori infection gastric ulcer%不同三联疗法根除幽门螺杆菌感染胃溃疡的临床效果比较

    Institute of Scientific and Technical Information of China (English)

    王惠德

    2015-01-01

    目的:探讨不同的三联疗法根除幽门螺杆菌感染胃溃疡的临床疗效。方法:收治幽门螺杆菌感染胃溃疡患者126例,分作观察组和对照组各63例,观察组给予奥美拉唑、克拉霉素、阿莫西林治疗,对照组给予奥美拉唑、甲硝唑、阿莫西林治疗,比较两组临床疗效。结果:观察组治愈总有效率95.23%,明显高于对照组的71.42%(P<0.05);观察组幽门螺杆菌根除率93.65%,高于对照组的76.19%(P<0.05)。结论:奥美拉唑、克拉霉素、阿莫西林根除幽门螺杆菌感染胃溃疡效果显著。%Objective:To explore the clinical effect of different triple therapy for helicobacter pylori infection gastric ulcer. Methods:126 patients with helicobacter pylori infection gastric ulcer were selected.They were divided into the observation group and the control group with 63 cases in each.The observation group were given omeprazole,clarithromycin and amoxicillin,and the control group were given omeprazole,metronidazole,amoxicillin,then we compared two groups of clinical curative effect.Results:In the observation group,the total effective rate of 95.23% was significantly higher than 71.42% in the control group(P>0.05),and the eradication rate of helicobacter pylori of 93.65% was higher than 76.19% in the control group(P<0.05).Conclusion:The clinical effect of omeprazole,clarithromycin and amoxicillin for helicobacter pylori infection gastric ulcer was significant.

  14. Highly sensitive LC-MS/MS methods for the determination of seven human CYP450 activities using small oral doses of probe-drugs in human.

    Science.gov (United States)

    Grangeon, Alexia; Gravel, Sophie; Gaudette, Fleur; Turgeon, Jacques; Michaud, Veronique

    2017-01-01

    Cocktails composed of several Cytochrome P450 (CYP450)-selective probe drugs have been shown of value to characterize in vivo drug-metabolism activities. Our objective was to develop and validate highly sensitive and selective LC-MS/MS assays allowing the determination of seven major human CYP450 isoenzyme activities following administration of low oral doses of a modified CYP450 probe-drug cocktail in patients. The seven-drug cocktail was composed of caffeine, bupropion, tolbutamide, omeprazole, dextromethorphan, midazolam (all administered concomitantly) and chlorzoxazone (administered separately) to phenotype for CYP1A2, 2B6, 2C9, 2C19, 2D6, 3A4/5 and 2E1, respectively. Serial plasma and urine samples were collected over an 8h period. The probe-drugs and their respective metabolites were measured in both human plasma and urine, except for omeprazole (plasma only) and chlorzoxazone (urine only). Samples were analyzed by high performance liquid chromatography with heated electrospray ionization tandem mass spectrometry (HPLC-HESI-MS/MS) using a Phenomenex Luna PFP (2) analytical column (3μm PFP(2) 150×3mm) for chromatographic separation. Optimal detection was achieved based on 3 different analytical methods; (1) isocratic elution with a mobile phase consisting of acetonitrile and water both fortified with 0.01% formic acid for the analysis of bupropion, tolbutamide, chlorzoxazone and their respective metabolites; (2) isocratic elution with a mobile phase composed of acetonitrile and ammonium formate (pH 3; 10mM) for omeprazole, dextromethorphan, midazolam and their metabolites; (3) for caffeine and paraxanthine, gradient elution using acetonitrile and 0.01% formic acid in water was used. All calibration functions were linear for all probe drugs and metabolites in both matrices over wide analytical ranges. The main advantages of our methods are the use of specific probe drugs available in most countries, the administration of small doses of probe drugs, small

  15. Efecto cicatrizante del aceite de Copaifera officinalis (copaiba, en pacientes con úlcera péptica

    Directory of Open Access Journals (Sweden)

    Jorge Arroyo-Acevedo

    2011-04-01

    Full Text Available Objetivos: Determinar la eficacia cicatrizante del aceite de copaiba obtenido de la corteza de Copaifera officinalis, comparado con omeprazol 20 mg, en pacientes con diagnóstico definitivo de úlcera péptica. Diseño: Estudio experimental, clínico comparativo, de fase II, aleatorio, doble ciego, grupo paralelo. Institución: Instituto de Investigaciones Clínicas, Facultad de Medicina, Universidad Nacional Mayor de San Marcos, Lima, Perú. Participantes: Pacientes con diagnóstico definitivo de úlcera péptica. Intervenciones: El diagnóstico fue tanto por exploración física como complementaria, siendo la endoscopia la técnica de elección, con evaluación pre y postratamiento con aceite de copaiba, formulada en cápsulas de 80 mg y 120 mg. El ensayo clínico incluyó 60 pacientes que voluntariamente ingresaron al programa de estudio, previa firma del consentimiento informado aprobado por el Comité institucional de Ética en Investigación. Los pacientes fueron distribuidos aleatoriamente en tres grupos, de 20 casos cada uno, según orden de llegada; los dos primeros grupos recibieron cápsulas de aceite de copaiba, en dosis de 80 y 120 mg, respectivamente; y un tercer grupo recibió omeprazol 20 mg. Los tratamientos fueron administrados en ayunas, una vez por la mañana, 30 minutos antes de la ingesta del primer alimento. Los datos fueron evaluados mediante técnicas multivariadas, considerando estadísticamente significativo p<0,05. Se tuvo en cuenta el consentimiento informado aprobado por el Comité de Bioética en Investigación del Centro Asistencial. Principales medidas de resultados: Porcentaje de cicatrización. Resultados: Se logró 65% y 75% de cicatrización de la úlcera péptica con aceite de copaiba, respectivamente, contra 100% en el grupo de omeprazol, sin efectos adversos significativos; dos presentaron náuseas y tres epigastralgia. Conclusiones: Los pacientes con úlcera péptica y con tratamiento de las c

  16. Observation of the Curative Effect of the Triad Therapy in Addition to Helicobacter Pylori%三联疗法根除幽门螺杆菌的疗效观察

    Institute of Scientific and Technical Information of China (English)

    廖肇发

    2009-01-01

    目的:评估左氧氟沙星为基础的三联治疗方案治疗幽门螺杆菌(helicobacter pylori,HP)感染的疗效及安全性.方法:对264例经胃镜检查和病理诊断慢性胃炎、胃溃疡的患者,随机分为治疗组和对照组各132例,治疗组给予左氧氟沙星、奥美拉唑、阿莫西林治疗;对照组给予奥美拉唑、克拉霉素、阿莫西林治疗,疗程均为10 d.结果:治疗组HP根除率为91.67%,对照组HP根除率为83.33%,两组治愈率差异均无统计学意义(P>0.05).结论:左氧氟沙星联合奥美拉唑、阿莫西林是一种安全、疗效高、耐受性好,也是当前根除幽门螺杆菌首选的一线治疗方案.%Objective:Be based on Levofloxacin,to evaluate the curative effect and security of treating helicobacter pylori with the treatment of trigeminy.Methods:Check-up 264 patients with gastroscopy and pathological diagnosis of chronic gastritis,gastric ulcer patients were randomly divided into treatment and control groups with 132 cases respectively,the treatment of levofloxacin group,omeprazole,amoxicillin treatment.In the control group given omeprazole,clarithromycin and amoxicillin treatment,treatment of 10d.Results:Hp eradication rate was 91.67% in the treatment group,83.33% in the control group,the rate difference between the two groups were not significant (P>0.05).Conclusions:the Joint omeprazole and amoxicillin are safe,high effective,with good tolerance,and the eradication of Helicobacter pylori is the current preferred first-line treatment.

  17. Gastroprotective activity of Annona muricata leaves against ethanol-induced gastric injury in rats via Hsp70/Bax involvement

    Directory of Open Access Journals (Sweden)

    Moghadamtousi SZ

    2014-10-01

    Full Text Available Soheil Zorofchian Moghadamtousi,1 Elham Rouhollahi,2 Hamed Karimian,2 Mehran Fadaeinasab,3 Mahmood Ameen Abdulla,2 Habsah Abdul Kadir1 1Biomolecular Research Group, Biochemistry Program, Institute of Biological Sciences, Faculty of Science, 2Department of Biomedical Science, Faculty of Medicine, 3Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur, Malaysia Abstract: The popular fruit tree of Annona muricata L. (Annonaceae, known as soursop and graviola, is a widely distributed plant in Central and South America and tropical countries. Leaves of A. muricata have been reported to possess antioxidant and anti-inflammatory activities. In this study, the gastroprotective effects of ethyl acetate extract of A. muricata leaves (EEAM were investigated against ethanol-induced gastric injury models in rats. The acute toxicity test of EEAM in rats, carried out in two doses of 1 g/kg and 2 g/kg, showed the safety of this plant, even at the highest dose of 2 g/kg. The antiulcer study in rats (five groups, n=6 was performed with two doses of EEAM (200 mg/kg and 400 mg/kg and with omeprazole (20 mg/kg, as a standard antiulcer drug. Gross and histological features showed the antiulcerogenic characterizations of EEAM. There was significant suppression on the ulcer lesion index of rats pretreated with EEAM, which was comparable to the omeprazole effect in the omeprazole control group. Oral administration of EEAM to rats caused a significant increase in the level of nitric oxide and antioxidant activities, including catalase, glutathione, and superoxide dismutase associated with attenuation in gastric acidity, and compensatory effect on the loss of gastric wall mucus. In addition, pretreatment of rats with EEAM caused significant reduction in the level of malondialdehyde, as a marker for oxidative stress, associated with an increase in prostaglandin E2 activity. Immunohistochemical staining also demonstrated that EEAM induced the

  18. 10-(6'-Plastoquinonyl)decyltriphenylphosphonium (SkQ1) Does Not Increase the Level of Cytochromes P450 in Rat Liver and Human Hepatocyte Cell Culture.

    Science.gov (United States)

    Myasoedova, K N; Silachev, D N; Petrov, A D

    2016-12-01

    Mitochondria-targeted antioxidant SkQ1 did not increase the content of cytochromes P450 in livers of rats that were given SkQ1 in drinking water for 5 days in a dose (2.5 µmol per kg body weight) that exceeded 10 times the SkQ1 therapeutic dose. SkQ1 did not affect the levels of cytochrome P450 forms CYP1A2, CYP2B6, and CYP3A4 in monolayer cultures of freshly isolated human hepatocytes, while specific inducers of these forms (omeprazole, phenobarbital, and rifampicin, respectively) significantly increased expression of the cytochromes P450 under the same conditions. We conclude that therapeutic doses of SkQ1 do not induce cytochromes P450 in liver, and the absence of the inducing effect cannot be explained by poor availability of hepatocytes to SkQ1 in vivo.

  19.   A Cost-Effectiveness Analysis of Two Management Strategies for Dyspepsia

    DEFF Research Database (Denmark)

    Kjeldsen, Hans Chr; Bech, Mickael; Christensen, Bo

    2007-01-01

    Objectives: To compare the cost-effectiveness of endoscopy and empirical proton pump inhibition (PPI) therapy for management of dyspepsia in primary care. Methods: A randomized controlled trial (RCT) including prospective collection of economic resource data was conducted in general practice from...... June 2000 to August 2002, Aarhus County, Denmark. We randomly assigned 368 dyspeptic patients from 32 general practices to treatment with omeprazol 40 mg for two weeks (n: 184) or endoscopy (n: 184). The study adopted a societal perspective, and the year of costing was 2006. Outcome measures: days free...... of dyspeptic symptoms and proportion of patients with dyspepsia after one year based on patients' and general practitioners' (GPs') assessment. Costs were estimated from patient and GP questionnaires and from medical records. Results: The incremental cost-effectiveness (CE) ratio for one day free of dyspeptic...

  20. Equine gastric ulcer syndrome (egus: diagnosis and therapy

    Directory of Open Access Journals (Sweden)

    Mot, T.,

    2008-06-01

    Full Text Available Equine gastric ulcer syndrome is especially reported in racing horses, with a prevalence of 60-90% in adults and 25-50% in foals. The ethiology of equine gastric ulcer is polifactorial, represented by nutritional factors, stress generated by training and captivity, drugs (corticosteroids-prednisolone, dexametasone, nesteroidicanti-inflammatory drugs: flumixin-meglumine, fenilbutazone, duodenal refluence. The diagnosis is established on clinical signs and therapeutic response and it is confirmed by endoscopic exam. Therapeutically it is recommended to administer: antiacide (aluminiu hydroxide, magnesium hydroxide, inhibitors of H2 receptors(cimetidine, ranitidine, famotidine, inhibitors of protons pump (Omeprazol, Sucralphate. Diagnosis and therapeutic aspects in equine gastric ulcer syndrome are presented in this study.