Gastroprotective Agents (gastroprotective + agent)

Distribution by Scientific Domains


Selected Abstracts


Gastroprotective activity of ferruginol in mice and rats: effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2008
Carlos Areche
The gastroprotective mechanism of the natural diterpene ferruginol was assessed in mice and rats. The involvement of gastric prostaglandins (PGE2), reduced glutathione, nitric oxide or capsaicin receptors was evaluated in mice either treated or untreated with indometacin, N-ethylmaleimide (NEM), N-nitro-L-arginine methyl ester (L-NAME) or ruthenium red, respectively, and then orally treated with ferruginol or vehicle. Gastric lesions were induced by oral administration of ethanol. The effects of ferruginol on the parameters of gastric secretion were assessed in pylorus-ligated rats. Gastric PGE2 content was determined in rats treated with ferruginol and/or indometacin. The reduction of gastric glutathione (GSH) content was determined in rats treated with ethanol after oral administration of ferruginol, lansoprazole or vehicle. Finally, the acute oral toxicity was assessed in mice. Indometacin reversed the gastroprotective effect of ferruginol (25 mg kg,1) but not NEM, ruthenium red or L-NAME. The diterpene (25 mg kg,1) increased the gastric juice volume and its pH value, and reduced the titrable acidity but was devoid of effect on the gastric mucus content. Ferruginol (25, 50 mg kg,1) increased gastric PGE2 content in a dose-dependent manner and prevented the reduction in GSH observed due to ethanol-induced gastric lesions in rats. Single oral doses up to 3 g kg,1 ferruginol did not elicit mortality or acute toxic effects in mice. Our results showed that ferruginol acted as a gastroprotective agent stimulating the gastric PGE2 synthesis, reducing the gastric acid output and improving the antioxidant capacity of the gastric mucosa by maintaining the GSH levels. [source]


Economic analysis of strategies in the prevention of non-steroidal anti-inflammatory drug-induced complications in the gastrointestinal tract

ALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 3 2004
A. Lanas
Summary Background :,It is unclear what the best therapeutic approach is in patients who require non-steroidal anti-inflammatory drugs. In clinical practice, choice of prescriptions are often based on drug costs. Aim :,To evaluate costs per upper gastrointestinal bleeding avoided with different prevention strategies. Methods :,Two major strategies have been considered (coxibs vs. non-steroidal anti-inflammatory drugs plus generic/brand gastroprotective agent). The number of patients needed to treat to prevent a bleeding event, the cost of the drug and duration of treatment were used to estimate costs. Results :,Based on hospitalization costs of a bleeding event, no therapeutic strategy is cost-effective in patients without risk factors. All strategies (including omeprazole + coxib) are cost-effective in patients with bleeding ulcer history. With other risk factors, all strategies are cost-effective but prevention of events is twice as expensive in patients <75 years of age. No strategy shows superiority unless the cheapest generics are prescribed or a 50% reduction in the incidence of lower gastrointestinal complications with coxibs is confirmed. Conclusions :,Current prevention strategies to reduce serious non-steroidal anti-inflammatory drug-associated gastrointestinal events are only cost-effective in patients with risk factors. No strategy shows superiority, but coxib strategy would be more cost-effective if it were associated with a reduction of events of the lower gastrointestinal tract. [source]


Coxibs: evolution of prescription's behaviour in France

FUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 3 2007
Julie Biga
Abstract The aim of the present study was, first to characterize profiles of coxibs' prescribers [general practitioners (GPs) and rheumatologists] in 2002 in France and, secondly, to identify factors associated with modification of this profile 1 year later. All GPs and rheumatologists from Midi-Pyrenees, Aquitaine, Languedoc-Roussillon and Pays de Loire areas (South of France: 11 050 000 inhabitants) were included in the study. For each practitioner, we used data concerning all non-steroidal anti-inflammatory drugs (NSAIDs) including coxibs reimbursed during period 1 (P1; January,March 2002) and period 2 (P2; January,March 2003). The ratio between the number of coxibs' prescriptions and the total number of NSAIDs' prescriptions (including coxibs) was used to define the two profiles of prescribers, one with a low level of coxibs' prescriptions and another one with a high level of coxibs' prescriptions. Characteristics of practitioners and characteristics of their practices were compared according to this profile. In the second step, we investigated the characteristics (of practitioners and practices) associated with an increase in the level of coxibs' prescriptions in P2 for practitioners with a low level of coxibs' prescriptions in P1. Results are expressed as odds ratio with their 95% confidence intervals. A positive statistical link was found between a high level of coxibs' prescriptions, the speciality of rheumatologist or extra costs for consultation. In contrast, a negative association was observed with female gender or age below 44 years. No relationship was found with the status of referent. Concerning practices' characteristics of practitioners, there was a positive statistical link between a high ratio of coxibs' prescriptions and high co-prescriptions of gastroprotective agents and a negative association with a high number of acts, a high proportion of patients with chronic disabling diseases (CDD) or a high number of patients between 15 and 64 years. There was no statistical link with proportion of patients covered by Universal Medical Coverage (UMC) or aged more than 65 years. Among the factors involved in the increase in the ratio (between P1 and P2), no relationship was found with practitioners' characteristics. In contrast, some factors related to practices (level of gastroprotective co-prescriptions, number of acts, number of CDD patients) were related to a change in coxibs' prescriptions between P1 and P2. This study allowed to discuss some relationships between coxibs' prescription and practitioners' (age, gender, medical speciality or extra costs for consultation) or practices' (level of medical practice, patients' age, number of CDD patients or level of gastroprotective prescriptions) characteristics. In contrast, some other factors like the referent status or the number of patients with UMC are not related. Physicians, initially low prescribers of coxibs and increasing their coxibs' prescriptions during the period of our study, were those with a high level of gastroprotective prescriptions, a low number of acts or a small proportion of CDD patients. [source]


Time-trends in gastroprotection with nonsteroidal anti-inflammatory drugs (NSAIDs)

ALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 11 2010
V. E. VALKHOFF
Aliment Pharmacol Ther,31, 1218,1228 Summary Background, Preventive strategies are advocated in patients at risk of upper-gastrointestinal complications associated with nonsteroidal anti-inflammatory drugs (NSAIDs). Aim, To examine time-trends in preventive strategies. Methods, In a study population comprising 50 126 NSAID users ,50 years from the Integrated Primary Care Information database, we considered two preventive strategies: co-prescription of gastroprotective agents and prescription of a cyclooxygenase-2-selective inhibitor. In patients with ,1 risk factor (history of upper-gastrointestinal bleeding/ulceration, age >65 years, use of anticoagulants, aspirin, or corticosteroids), correct prescription was defined as the presence of a preventive strategy and under-prescription as the absence of one. In patients with no risk factors, correct prescription was defined as the lack of a preventive strategy, and over-prescription as the presence of one. Results, Correct prescription rose from 6.9% in 1996 to 39.4% in 2006 (P < 0.01) in high-risk NSAID users. Under-prescription fell from 93.1% to 59.9% (P < 0.01). In the complete cohort, over-prescription rose from 2.9% to 12.3% (P < 0.01). Conclusions, Under-prescription of preventive strategies has steadily decreased between 1996 and 2006; however, 60% of NSAID users at increased risk of NSAID complications still do not receive adequate protection. [source]


Uncomplicated peptic ulcer in the UK: trends from 1997 to 2005

ALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 10 2009
S. CAI
Summary Background, Few studies have examined the incidence of uncomplicated peptic ulcer or the trends in factors affecting its incidence. Aim, To estimate the incidence rate of uncomplicated peptic ulcer in the UK from 1997 to 2005 and report temporal changes in the main known preventive and risk factors. Methods, Population-based cohort study of 1 049 689 patients enrolled in The Health Improvement Network in the UK. We estimated the incidence rate of uncomplicated peptic ulcer and evaluated temporal trends in demographic characteristics and prescription patterns for various anti-inflammatory and gastroprotective agents. Results, Overall uncomplicated peptic ulcer incidence was 0.75 cases per 1000 persons-years, declining from 1.1 to 0.52 cases per 1000 person-years between 1997 and 2005. Distributions of age, gender and alcohol habits were similar in 1997 and 2005. The proportion of documented Helicobacter pylori -negative cases increased from 5% to 12%. Monthly prevalence of subjects with prescriptions for traditional non-aspirin NSAIDs changed from 7.7% to 6.8%, Coxibs from 0% to 0.7%, and proton pump inhibitors (PPIs) from 2.4% to 7.4%. The proportion of subjects on prescription NSAIDs on PPIs increased continuously over time. Conclusion, A reduction in H. pylori -related peptic ulcers, changing patterns in NSAID use and increasing PPI use may have contributed to a decline in uncomplicated peptic ulcer incidence in the UK. [source]


COX-2 inhibitors: complex association with lower risk of hospitalization for gastrointestinal events compared to traditional NSAIDs plus proton pump inhibitors,

PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 10 2009
Michiel W. van der Linden MDPhD
Abstract Purpose To compare hospitalization rates for serious upper and lower gastrointestinal (GI) events between chronic and acute users of a traditional non-steroidal anti-inflammatory drugs (tNSAID),+,proton pump inhibitor (PPI) and users of a COX-2 selective inhibitor (Coxib). Methods The PHARMO Record Linkage System, including linked drug-dispensing and hospital records of approximately 3 million individuals in the Netherlands was used. We selected new Coxib or tNSAID users (01/01/2000,31/12/2004) with ,1,year history before the first NSAID dispensing and ,1,year follow-up ending at the first hospitalization for GI event (the outcome), last dispensing, or end of the study period. Chronic users were patients who used any NSAIDs for ,60,days during the first year (n,=,58,770); others were acute users (n,=,538,420). Multivariate analysis was performed by Poisson regression adjusted for gender, age, and duration of follow-up, tNSAID and Coxib dose, NSAID/PPI adherence, use of other gastroprotective agents, anticoagulants, acetaminophen, corticosteroids, and cardiovascular disease. Results The cohort included 23,999 new tNSAIDs,+,PPI users and 25,977 new Coxib users, with main characteristics: mean,±,SD age 58.1,±,15.5 vs. 56.7,±,17.5; female 55.3% vs. 62.2%; duration of treatment (days): 137,±,217 vs. 138,±,179, respectively. Among acute users, adjusted hazard ratios (95% Confidence Interval) were 0.21 (0.14,0.32) for upper and 0.26 (0.16,0.42) for lower GI events, for Coxib versus tNSAIDs,+,PPI users. Among chronic users, these were 0.35 (0.22,0.55) for upper GI and 0.43 (0.25,0.75) for lower GI events. Conclusions Coxib users had significantly lower rates of GI events. Further research should elucidate the possible impact of selection bias. Copyright © 2009 John Wiley & Sons, Ltd. [source]