The stereoselective pharmacokinetics of lansoprazole enantiomers is likely due to its stereoselective protein binding and/or metabolism.
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The stool assay was an accurate tool for diagnosis of H. pylori infection and eradication control.
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Triple therapy with metronidazole and clarithromycin, but not amoxicillin, can be used for H. pylori eradication in patients with chronic renal insufficiency, because it is more effective, well tolerated and less likely to cause deterioration of renal function.
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To test the impact of intravenous omeprazole on Helicobacter pylori eradication for bleeding peptic ulcers.
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The study enrolled healthy adult men and consisted of 2 periods. In the first period, all subjects received a single 40-mg dose of omeprazole. This was followed by an 8-day period during which fluoxetine monotherapy (60 mg/d) was administered as a single oral daily dose. At the end of those 8 days, the subjects were administered a 40-mg dose of omeprazole with a 60-mg dose of fluoxetine. Plasma concentrations of omeprazole were determined at 0.5, 1, 1.33, 1.66, 2, 2.5, 3, 4, 5, 6, 7, 8, 10, and 12 hour(s) after study drug administration. Omeprazole plasma concentrations were determined by a validated HPLC method. Pharmacokinetic parameters of omep-razole were calculated using noncompartmental analysis. Adverse events were assessed throughout the study duration.
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Administration of RPZ not only inhibited gastric H. pylori colonization, but also reduced gastric mucosal inflammation in gerbils, possibly through its antibacterial action as well as pharmacological recruitment of the reduced form of GSH.
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Median body weight significantly increased by 29 kg (range, 10 to 50 kg). Mean +/- SE gastric fluid pH significantly decreased from 4.9 +/- 0.4 to 3.1 +/- 0.3 over 5 weeks, and total volatile fatty acid concentration significantly decreased over time. Mean +/- SE severity of nonglandular ulcers significantly increased from 0.4 +/- 0.1 to 1.2 +/- 0.2 over 5 weeks. Nonglandular ulcers significantly increased in number (mean +/- SE, 1.3 +/- 0.2 to 3.0 +/- 0.2) and severity (mean +/- SE, 1.2 +/- 0.2 to 2.6 +/- 0.2) during the 7-day alternating feed deprivation period. No effects of treatment were detected.
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TNF-alpha has numerous biological activities, including the induction of chemokine expression, and is involved in many gastric injuries. C-C chemokines [monocyte chemotactic protein (MCP)-1 and macrophage inflammatory protein (MIP)-1alpha] and C-X-C chemokines [MIP-2 and cytokine-induced neutrophil chemoattractant (CINC)-2alpha] mediate chemotaxis of monocytes and neutrophils, respectively. We examined the roles of TNF-alpha and dynamics of chemokine expression in gastric ulceration including ulcer recurrence and indomethacin-induced injury. Rats with healed chronic gastric ulcers received intraperitoneal TNF-alpha to induce ulcer recurrence. Some rats were given neutralizing antibodies against neutrophils or MCP-1 together with TNF-alpha. In a separate experiment, rats were orally administered 20 mg/kg indomethacin with or without pretreatment with pentoxifylline (an inhibitor of TNF-alpha synthesis) or anti-MCP-1 antibody. TNF-alpha (1 microg/kg) induced gastric ulcer recurrence after 48 h, which was completely prevented by anti-neutrophil antibody. TNF-alpha increased the number of macrophages and MCP-1 mRNA expression in scarred mucosa from 4 h, whereas it increased MPO activities (marker of neutrophil infiltration) and mRNA expression of MIP-2 and CINC-2alpha from 24 h. Anti-MCP-1 antibody inhibited leukocyte infiltration with reduction of the levels of C-X-C chemokines and prevented ulcer recurrence. Indomethacin treatment increased TNF-alpha/chemokine mRNA expression from 30 min and induced macroscopic erosions after 4 h. Pentoxifylline inhibited the indomethacin-induced gastric injury with reduction of neutrophil infiltration and expression of chemokine (MCP-1, MIP-2, and CINC-2alpha). Anti-MCP-1 antibody also inhibited the injury and these inflammatory responses but did not affect TNF-alpha mRNA expression. In conclusion, increased MCP-1 triggered by TNF-alpha may play a key role in gastric ulceration by regulating leukocyte recruitment and chemokine expression.
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HepaRG cells possess the unique property to differentiate in vitro and to express various functions of mature hepatocytes, including the major cytochromes P450 (P450s). In the present study, we carefully analyzed mRNA expression and activity of the major P450s and their responsiveness to three prototypical inducers, phenobarbital, rifampicin, and omeprazole, in differentiated HepaRG cell cultures over a 4-week period after low and high seeding. Only minor differences were observed in P450 activities when measured by two cocktails of probe substrates, probably related to the choice and/or concentration of substrates. Similar results were obtained from the two cell seeding conditions. Expression and activities of several P450s were dimethyl sulfoxide-dependent. However, basal P450 expression and activities as well as their responsiveness to the prototypical inducers were well maintained over the 4-week period, and a good correlation was observed between transcript levels and corresponding activities. Thus, CYP1A2, CYP2B6, and CYP3A4 were found to accurately respond to their respective prototypical inducers, i.e., omeprazole, phenobarbital, and rifampicin. Likewise, basal expression of several phase II enzymes, transporters, and nuclear receptors, and response to inducers were also well preserved. More genes were found to be induced in HepaRG cells than in primary human hepatocytes, and no marked variation was noticed between the different passages. Taken together, these data support the conclusion that HepaRG cells represent a promising surrogate to primary human hepatocytes for xenobiotic metabolism and toxicity studies.
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The present study indicates that there are significant drug interactions between lansoprazole and clarithromycin in all CYP2C19 genotype groups probably through CYP3A inhibition. The bioavailability of lansoprazole might, to some extent, be increased through inhibition of P-glycoprotein during clarithromycin treatment.
This study was designed to evaluate the absolute bioavailability (F value) of 2-chlorodeoxyadenosine (cladribine; 2-CdA) after multiple oral administrations, and the intersubject variability after oral and 2-hour intravenous (IV) administration schedules in patients with malignancy.
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Analysis of oesophageal motility showed no improvement in peristaltic activity after healing of oesophagitis, suggesting that the abnormal motility is either a primary disorder or an irreversible consequence of mucosal damage.
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Clarithromycin inhibits the metabolism of omeprazole. Drug interaction between clarithromycin and omeprazole may underlie high eradication rates achieved by triple therapy with omeprazole, amoxicillin, and clarithromycin.
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The objective of this work was to investigate the antiulcerogenic and anti-inflammatory activities of the essential oil from Pterodon emarginatus seeds.
The therapeutic regimen containing ciprofloxacin is preferable, although all drug regimens were less effective in Iran than in other parts of the world.
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Bedtime ranitidine is more effective than bedtime omeprazole on residual nocturnal acid secretion in patients receiving omeprazole twice daily. This finding suggests that fasting breakthrough nocturnal acid secretion in patients receiving omeprazole twice daily is most likely histamine related.
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All articles reporting original data on drug and food interactions with warfarin.
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In an open study 66 consecutive infected patients with ulcer disease or non-ulcer dyspepsia were treated with 4-day quadruple therapy after 3 days of lansoprazole pretreatment. H. pylori status was determined before and at least 6 weeks after therapy by endoscopy with antral and corpus biopsies for rapid urease test, histology and culture.
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To evaluate the effectiveness of triple therapy containing either omeprazole or ranitidine bismuth citrate (RBC) to treat H. pylori infection in Vietnamese duodenal ulcer patients.
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The study was designed to research whether providing doctors with customized reports on prescription indicators,plus a presentation of the project to clinical departments and hospital boards, would improve prescription quality in specialized care.
Percentage times intragastric pH < 4 on omeprazole, 20 mg, in the morning of the day after receiving famotidine, 10 mg, at bedtime (58.6 +/- 4.8); at 05.30 h (54.1 +/- 5.1); or at bedtime and at 05.30 h (54.3 +/- 5.0) did not differ significantly (P=0.65) from percentage times intragastric pH on day 7 of omeprazole, 20 mg, in the morning (49.5 +/- 5.1).
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The dose of lansoprazole appears to be more important than the duration of therapy. Dual therapy with lansoprazole and clarithromycin should be investigated further as a possible treatment regimen for H. pylori infection.