- [Analysis of proton pump inhibitors anti-ulcer drugs use in the Araba district primary care area]. [Journal Article]
- RERev Esp Salud Publica 2018 Aug 16; 92
- CONCLUSIONS: There is an overall increase in the prescription of PPIs, although the expenses have decreased due to price drop. Likewise there is a decrease in the relative consumption of omeprazole, although the indications approved had not changed. PPIs prescription should be done with caution since their unjustified high use in the prevention of gastropathy increases the risk of inappropriate prescriptions. The most recommended PPI continues to be omeprazole.
- Influence of organic modifier and separation modes for lipophilicity assessment of drugs using thin layer chromatography indices. [Journal Article]
- JCJ Chromatogr A 2018 Aug 04
- Lipophilicity constitutes one of the most important physicochemical properties in the design and development of drug molecules. In the present work thin layer chromatography (TLC) has been utilized t...
Lipophilicity constitutes one of the most important physicochemical properties in the design and development of drug molecules. In the present work thin layer chromatography (TLC) has been utilized to evaluate lipophilicity of 11 representative drugs, which included six proton pump inhibitors (omeprazole, pantoprazole, rabeprazole, lansoprazole, ilaprazole, and tenatoprazole), an anti-vertigo drug, betahistine, nonsteroidal anti-inflammatory drug, ibuprofen, anti-malarial drug, atovaquone, an anti-HIV agent, atazanavir and a hormonal drug, calcitriol. Normal as well as reversed-phase separation modes were evaluated to study the effect of different organic modifiers for the estimation of lipophilicity. The quantitative descriptor of lipophilicity, the partition coefficient (logP) was estimated by suitably optimizing the solvent systems for both the modes. The best mobile phase pairs for NPTLC and RPTLC were toluene-acetonitrile and water-methanol respectively. Principal component analysis, hierarchical cluster analysis, as well as non-parametric methods like sum of ranking differences and generalized pair wise correlation revealed the dominant pattern in the data. The results obtained from both the separation modes were comparable and were in good agreement with the computational data for all the drugs.
- Efficacy and Safety Profile of Z-215 (Azeloprazole Sodium), a Proton Pump Inhibitor, Compared with Rabeprazole Sodium in Patients with Reflux Esophagitis: A Phase II, Multicenter, Randomized, Double-Blind, Comparative Study. [Journal Article]
- CTCurr Ther Res Clin Exp 2018; 88:26-34
- CONCLUSIONS: Z-215 was as effective and well tolerated as 10 mg RPZ in the treatment of RE in this selected population. CYP2C19 genotype status may not influence the efficacy and safety of Z-215. There were no clear dose-response effects between Z-215 doses in the endoscopic healing of RE. These findings suggest that Z-215 may be 1 option for the initial treatment of RE. ClinicalTrials.gov identifier: NCT 02463643.
- Second-line triple therapy in failures with vonoprazan-based triple therapy for eradication of Helicobacter pylori. [Journal Article]
- BRBiomed Rep 2018; 9(2):169-174
- Gastric acid inhibition during treatment is important for the eradication of Helicobacter pylori (H. pylori) infection. A novel potassium-competitive acid blocker, vonoprazan (VPZ), has been demonstr...
Gastric acid inhibition during treatment is important for the eradication of Helicobacter pylori (H. pylori) infection. A novel potassium-competitive acid blocker, vonoprazan (VPZ), has been demonstrated to achieve high eradication rates; however, the efficacy of second-line treatment in failures of VPZ-based triple therapy has not been well studied. The aim of the current study was to determine the efficacy of VPZ in a first-line regimen for H. pylori eradication, and the efficacy of a second-line regimen using metronidazole (MTZ) in failures with the first-line regimen. Of 580 subjects enrolled in the study, 524 patients completed first-line treatment (275 patients who received VPZ and 249 patients who received LPZ). First-line regimens consisted of a combination of clarithromycin (CAM) 200 or 400 mg twice a day, amoxicillin (AMPC) 750 mg twice a day, and either LPZ 30 mg or VPZ 20 mg twice a day, administered orally for 7 days. CAM and VPZ/LPZ were replaced with metronidazole (MTZ) 250 mg and rabeprazole 10 mg in the second-line regimens. The eradication of H. pylori was assessed by the H. pylori stool antigen test. The overall first-line eradication rate with VPZ was significantly higher than that with LPZ [91.0% (250/275) vs. 84.7% (211/249), respectively, P=0.030]. The dose of CAM (400 vs. 800 mg) did not affect the eradication rate in either the VPZ or LPZ regimens. The overall eradication rates of the second-line regimens with MTZ did not differ significantly between the VPZ-failure and LPZ-failure groups [87.0% (20/23) vs. 87.9% (29/33), respectively, P=0.700]. Therefore, VPZ was significantly more effective than LPZ for first-line treatment. In patients with failure of first-line eradication therapy, successful results of second-line eradication therapy did not differ between the VPZ- and LPZ-failure groups. In conclusion, VPZ-based triple therapy should be recommended for eradication of H. pylori.
- Drugs and Lactation Database (LactMed) [BOOK]
- BOOKNational Library of Medicine (US): Bethesda (MD)
- Because no information is available on the use of rabeprazole during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Because no information is available on the use of rabeprazole during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
- Changes in proton pump inhibitor prescribing trend over the past decade and pharmacists' effect on prescribing practice at a tertiary hospital. [Journal Article]
- BHBMC Health Serv Res 2018 Jul 11; 18(1):537
- CONCLUSIONS: The utilization of and expenditure on PPIs grew due to the increase of patients and irrational use of PPI. Pharmacist interventions help to reduce PPI utilization and expenditure and enhance rationality for inpatients, but much work should be done to regulate injection and originator formulas, and improve the rationality in the future.
- Ten-day quadruple therapy comprising low-dose rabeprazole, bismuth, amoxicillin and tetracycline is an effective and safe first-line treatment for Helicobacter pylori infection in population with high antibiotic resistance: a prospective, multicenter, randomized, parallel-controlled clinical trial in China. [Journal Article]
- AAAntimicrob Agents Chemother 2018 Jun 18
- CONCLUSIONS: Bismuth-containing quadruple therapy with low-dose rabeprazole, amoxicillin and tetracycline is a good option for first-line treatment of H. pylori infection in population with high antibiotic resistance.
- Efficacies of different proton pump inhibitor-based 14-day bismuth-furazolidone quadruple regimens for the initial eradication of Helicobacter pylori in the southeast coastal region of China: an open-label, randomized clinical trial. [Journal Article]
- CEClin Exp Med 2018 Jun 06
- To evaluate potency and safety of 14-day bismuth-furazolidone quadruple regimens and to compare efficacies of five proton pump inhibitors (PPIs) for the initial eradication of Helicobacter pylori (H....
To evaluate potency and safety of 14-day bismuth-furazolidone quadruple regimens and to compare efficacies of five proton pump inhibitors (PPIs) for the initial eradication of Helicobacter pylori (H. pylori), 175 eligible patients were enrolled and randomly assigned to 14-day quadruple regimens consisting of bismuth (400 mg), amoxicillin (1 g), furazolidone (100 mg), and a PPI, twice a day. PPIs used were Group A (pantoprazole capsules, 40 mg), Group B (pantoprazole tablets, 40 mg), Group C (lansoprazole, 30 mg), Group D (esomeprazole, 20 mg), and Group E (rabeprazole, 10 mg). H. pylori status was reassessed by 13C urea breath test on day 56 as the primary outcome. Gastrointestinal symptoms, parenteral side effects, compliance, and stool type were recorded simultaneously. The total eradication rates were 86.9% (152/175 [95% CI 80.9-91.5%]) and 95.6% (152/159 [91.1-98.2%]) by intention-to-treat (ITT) and per-protocol (PP) analysis. The efficacies of Group A, B, C, D, and E by ITT analysis were 91.4% (32/35 [76.9-98.2%]), 85.7% (30/35 [69.7-95.2%]), 88.6% (31/35 [73.3-96.8%]), 85.7% (30/35 [69.7-95.2%]), and 82.9% (29/35 [66.4-93.4%]) (p > 0.05). In the PP analysis, the efficacies were 97.0% (32/33), 93.8% (30/32), 93.9% (31/33), 100% (30/30), and 93.5% (29/31) (p > 0.05). Gastrointestinal symptoms and stool type were improved significantly (p < 0.05). Total side effects rate and poor compliance rate were 15.7% (25/159) and 5.0% (8/159). Fourteen-day bismuth-furazolidone quadruple regimens are of high potency and safety for the initial eradication of H. pylori. Efficacies of different PPIs and different dosages (9-32 mg omeprazole equivalents) showed no significant difference. The appropriate PPI can thus be chosen by clinicians.
- First characterization of a microsporidial triosephosphate isomerase and the biochemical mechanisms of its inactivation to propose a new druggable target. [Journal Article]
- SRSci Rep 2018 Jun 05; 8(1):8591
- The microsporidia are a large group of intracellular parasites with a broad range of hosts, including humans. Encephalitozoon intestinalis is the second microsporidia species most frequently associat...
The microsporidia are a large group of intracellular parasites with a broad range of hosts, including humans. Encephalitozoon intestinalis is the second microsporidia species most frequently associated with gastrointestinal disease in humans, especially immunocompromised or immunosuppressed individuals, including children and the elderly. The prevalence reported worldwide in these groups ranges from 0 to 60%. Currently, albendazole is most commonly used to treat microsporidiosis caused by Encephalitozoon species. However, the results of treatment are variable, and relapse can occur. Consequently, efforts are being directed toward identifying more effective drugs for treating microsporidiosis, and the study of new molecular targets appears promising. These parasites lack mitochondria, and oxidative phosphorylation therefore does not occur, which suggests the enzymes involved in glycolysis as potential drug targets. Here, we have for the first time characterized the glycolytic enzyme triosephosphate isomerase of E. intestinalis at the functional and structural levels. Our results demonstrate the mechanisms of inactivation of this enzyme by thiol-reactive compounds. The most striking result of this study is the demonstration that established safe drugs such as omeprazole, rabeprazole and sulbutiamine can effectively inactivate this microsporidial enzyme and might be considered as potential drugs for treating this important disease.
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- Safe use of proton pump inhibitors in patients with cirrhosis. [Journal Article]
- BJBr J Clin Pharmacol 2018 Apr 24
- CONCLUSIONS: We suggest using esomeprazole, omeprazole or rabeprazole in patients with CTP A or B cirrhosis and only esomeprazole in patients with CTP C. Pharmacokinetic changes are also important to consider when prescribing PPIs to vulnerable, cirrhotic patients.