Efficacy of esomeprazole in patients with acid-peptic disorders.

Esomeprazole (Nexium) is a new proton pump inhibitor that provides more effective acid control compared with other proton pump inhibitors. In patients with gastroesophageal reflux disease, standard doses of esomeprazole maintain intragastric pH above 4 for significantly longer periods compared with standard doses of other proton pump inhibitors after 5 days of treatment. Esomeprazole is approved for the treatment of symptomatic gastroesophageal reflux disease, the healing of erosive esophagitis, and maintenance of healing. In clinical trials, esomeprazole 40 mg once daily for up to 8 weeks provided higher rates of healing of erosive esophagitis and a greater proportion of patients with sustained resolution of heartburn, than either omeprazole 20 mg or lansoprazole 30 mg once daily. For the maintenance of healing, esomeprazole 20 mg once daily provided significantly higher rates of maintained healing of erosive esophagitis after 6 months of treatment compared with lansoprazole 15 mg once daily. Esomeprazole is also approved for use as part of a triple-drug therapy regimen in combination with amoxicillin and clarithromycin for the eradication of Helicobacter pylori in patients with duodenal ulcer disease. The side effect profile of esomeprazole is similar to that of omeprazole. Many patients with acid-related disorders may benefit from the more rapid symptom relief, higher rates of healing of erosive esophagitis, and improved maintenance of healing that can be achieved with esomeprazole.     

Esomeprazole, a new proton pump inhibitor: pharmacological characteristics and clinical efficacy

Esomeprazole, the S-isomer of omeprazole, is the first proton pump inhibitor synthesised as an optical isomer to become available for clinical use. Esomeprazole is optically stable in humans with negligible inversion to the R-isomer. Esomeprazole has significantly higher oral bioavailability than omeprazole, resulting in greater acid suppression. In clinical studies, 4 weeks' treatment with 40 mg esomeprazole demonstrated greater healing of all grades of erosive oesophagitis, compared with 20 mg omeprazole (76-82% versus 69-71%) and higher rates of symptom resolution (65-68% versus 58-61%) Furthermore, esomeprazole maintained healing rates of up to 90% over 6 months in erosive oesophagitis. Comparisons with other proton pump inhibitors in oesophagitis are, as yet, unavailable. In patients with endoscopy-negative gastro-oesophageal reflux disease (GERD), on-demand therapy with esomeprazole 20 mg has been shown to be very efficacious compared with placebo, and is well tolerated; however, comparisons with other proton pump inhibitors have not been performed. Long-term use of esomeprazole for up to 12 months in patients with GERD have not raised any significant safety concerns with respect to the development of atrophic gastritis or clinically relevant changes in enterochromaffin-like cells.     

A review of the clinical and economic impact of using esomeprazole or lansoprazole for the treatment of erosive esophagitis

BACKGROUND: The use of proton pump inhibitors (PPIs) for the treatment of erosive esophagitis has had a major impact on the prescribing budgets of primary care organizations in the United Kingdom. Assessments of the clinical and economic effectiveness of PPIs would provide useful tools for decision-making. OBJECTIVE: The goal of this study was to review the available preclinical and clinical studies comparing esomeprazole with lansoprazole in the healing and maintenance of erosive esophagitis, and to compare the budgeting impact of the 2 strategies. Comparative tolerability was also reviewed. METHODS: MEDLINE (1966-September 2002) and EMBASE (1980-September 2002) were searched for abstracts and articles reporting comparative studies of esomeprazole and lansoprazole. The search terms used were gastroesophageal reflux disease, reflux esophagitis, and proton pump inhibitor; all comparisons of esomeprazole and lansoprazole at any dose were considered. The database search was supplemented based on the authors' familiarity with the literature. RESULTS: The comparative studies that were identified fell into 4 categories: (1) intragastric acid suppression studies; (2) randomized controlled trials in the healing of erosive esophagitis; (3) randomized controlled trials in the maintenance of erosive esophagitis; and (4) health economic analyses. Based on these studies, when healing doses (esomeprazole 40 mg once daily, lansoprazole 30 mg once daily) and low doses (20 and 15 mg once daily, respectively) were compared, esomeprazole was more efficacious than lansoprazole in suppressing acid in the intragastric compartment (both comparisons, P < 0.05). More patients with erosive esophagitis experienced healing at 4 and 8 weeks with esomeprazole 40 mg once daily than with lansoprazole 30 mg once daily (P < 0.001 at 4 and 8 weeks). At 6 months, remission was maintained in more patients receiving esomeprazole 20 mg once daily than in those receiving lansoprazole 15 mg once daily (P < 0.001). No significant differences in tolerability were noted in clinical trials that directly compared the 2 PPIs. When the cost-effectiveness of esomeprazole treatment was compared with that of lansoprazole treatment in the healing and maintenance of erosive esophagitis, the greater efficacy of esomeprazole translated into potential cost savings and better outcomes. CONCLUSION: The currently available comparative data for esomeprazole and lansoprazole indicate clinical and cost-effectiveness advantages for esomeprazole in the healing and maintenance of erosive esophagitis compared with lansoprazole.     

埃索拉唑治疗胃食管反流病的效果观察

目的:探讨埃索拉唑治疗胃食管反流病的效果.方法:将经胃镜检查证实的96例胃食管反流病,采用随机、双盲法分成埃索拉唑组、奥美拉唑组、法莫替丁组,每组各32例.3组均予西沙比利10 mg,每日3次口服;在此基础上三组分别予埃索拉唑20 mg,每日2次口服;奥美拉唑20 mg,每日2次口服;法莫替丁20 mg,每日2次口服.于治疗8周后观察症状的缓解情况,同时复查胃镜观察食管炎治愈效果.结果:埃索拉唑组、奥美拉唑组、法莫替丁组治疗8周后症状改善总有效率分别为96.88%、93.75%、62.50%,埃索拉唑组和奥美拉唑组与法莫替丁组比较差异有非常显著的统计学意义(P＜0.01),埃索拉唑组与奥美拉唑组比较差异无统计学意义(P＞0.05);治疗8周后三组食管炎总有效率分别为87.5%、81.25%、28.14%,埃索拉唑组和奥美拉唑组与法莫替丁组比较差异具有非常显著性统计学意义(P＜0.01).结论:埃索拉唑是治疗胃食管反流病的有效药物.     

埃索美拉唑联合莫沙比利治疗反流性食管炎临床观察

目的探讨埃索美拉唑联合莫沙比利治疗反流性食管炎（RE）的临床疗效。方法选取2008年至2010年新野卫生职业中专附属医院治疗的86例RE患者,将其随机分成两组：治疗组和对照组各43例,治疗组用埃索美拉唑＋莫沙比利治疗,对照组采用奥美拉唑＋多潘立酮治疗,4周后观察两组的临床症状改善率,并评价内镜下有效率。结果 4周后,治疗组临床总有效率为为93.02%,内镜下总有效率90.70%;对照组临床总有效率为72.09%,内镜下总有效率为69.77%;两组比较差异有统计学意义（P〈0.05）。结论埃索美拉唑联合莫沙比利治疗RE效果良好,值得推广。     

Antimicrobial activity of esomeprazole versus omeprazole against Helicobacter pylori

OBJECTIVE: Esomeprazole is an enantiomorph of omeprazole, which inhibits gastric acid secretion more effectively than omeprazole. As proton pump inhibitors also exert an antibacterial activity, we aimed to compare esomeprazole and omeprazole for their antimicrobial activity against Helicobacter pylori in vitro. METHODS: We studied 52 H. pylori isolates obtained from gastric biopsies and inoculated onto agar plates containing the acid-converted drugs at different concentrations. The minimal concentrations that inhibited the growth of 50% and 90% of isolates were defined as MIC(50) and MIC(90). RESULTS: The MIC(50) and MIC(90) of esomeprazole were 16 and 32 mg/L; and those of omeprazole were 32 and 64 mg/L. Overall, 63.5% of isolates showed the same susceptibility to both drugs; 17 isolates were two- to 64-fold more susceptible to esomeprazole and two isolates were two-fold more susceptible to omeprazole. CONCLUSIONS: The increased antimicrobial activity in vitro of esomeprazole against H. pylori could contribute to improving the outcome of the eradication treatment of such an infection.     

Clinical effect of proton pump inhibitors on reflux esophagitis]

The clinical efficacy of proton pump inhibitors (PPI, omeprazole 20 mg or lansoprazole 30 mg), once daily, after breakfast, was studied in patients with erosive/ulcerative reflux esophagitis. The following results were obtained. 1) Twenty-four hour esophageal pH monitoring was performed before treatment and on 7th day of PPI medications. Omeprazole reduced the percent time pH less than 4 from 29.1 to 1.2 and lansoprazole from 68.0 to 2.4. 2) The cumulative disappearance rate of overall symptom was 52% after 1 week and 62% after 2 weeks with omeprazole these were 66% and 91%, and with lansoprazole respectively 3) The endoscopic healing rate was 63% was after 2 weeks and 76% after 4 weeks with omeprazole medication, and 76% and 97% respectively with lansoprazole. These results indicate that PPI medication inhibits the acid reflux almost completely and is a more useful therapeutic agent for GERD than H2-antagonists.     

Healing and relapse rates in gastroesophageal reflux disease treated with the newer proton-pump inhibitors lansoprazole, rabeprazole, and pantoprazole compared with omeprazole, ranitidine, and placebo: evidence from randomized clinical trials

BACKGROUND: The older proton pump inhibitor (PPI) omeprazole and the newer PPIs lansoprazole, rabeprazole, and pantoprazole are approved for the acute and maintenance treatment of gastroesophageal reflux disease (GERD). OBJECTIVE: On the basis of the results of randomized clinical trials, this study sought to estimate healing and relapse rates in acute and maintenance treatment of GERD with the newer PPIs compared with omeprazole, the histamine2-receptor antagonist ranitidine (the most frequent non-PPI comparator in studies of PPIs), and placebo. METHODS: A search of MEDLINE was conducted to identify randomized, controlled clinical trials that included a PPI in > or =1 treatment arm and assessed the healing of erosive esophagitis endoscopically. The primary outcome for studies of acute therapy was healing rate, and the primary outcome for studies of maintenance therapy was relapse rate. RESULTS: Fifty-three studies were identified, of which 38 involved acute therapy (12 excluded) and 15 maintenance therapy. None of the studies of pantoprazole met the inclusion criteria for maintenance therapy. The 8-week overall healing rate ratios in the comparison of newer PPIs with omeprazole 20 mg/d were as follows: lansoprazole 30 mg/d, 1.02 (95% CI, 0.98-1.06): rabeprazole 20 mg/d, 0.93 (95% CI, 0.87-1.00); and pantoprazole 40 mg/d, 0.98 (95% CI, 0.90-1.07). In the comparison of any PPI with ranitidine 300 mg/d, the ratios were as follows: lansoprazole, 1.62 (95% CI, 1.46-1.76); rabeprazole, 1.36 (95% CI, 1.20-1.54); pantoprazole, 1.60 (95% CI, 1.33-1.96); and omeprazole, 1.58 (95% CI, 1.41-1.78). Relapse rates over 1 year of treatment were similar between lansoprazole and rabeprazole. Compared with ranitidine, there were statistically significant differences in the rates of resolution of heartburn symptoms (P < 0.002), ulcer healing (P < 0.05), and relapse (P < 0.01). Similar results were seen in the comparison of PPIs with placebo in terms of rates of resolution of heartburn symptoms (P < 0.01), ulcer healing (P < 0.001), and relapse (P < 0.006). CONCLUSIONS: In this study, the newer PPIs were of similar efficacy to omeprazole in terms of heartburn control, healing rates, and relapse rates. All the PPIs were superior to ranitidine and placebo in healing erosive esophagitis and decreasing relapse rates.     

An overview of proton pump inhibitors.

SUMMARY: Proton pump inhibitors are the standard of treatment for acid-related disorders. These disorders include gastroesophageal reflux disease and its complications (i.e., erosive esophagitis and Barrett's esophagus), peptic ulcer disease, Zollinger-Ellison syndrome, and idiopathic hypersecretion. Proton pump inhibitors are also successfully used for the treatment of Helicobacter pylori infection and upper gastrointestinal bleeding.There are currently five proton pump inhibitors approved by the Food and Drug Administration and available in the United States. These are omeprazole (Prilosec), lansoprazole (Prevacid), rabeprazole (Aciphex), pantoprazole (Protonix), and esomeprazole (Nexium). This review discusses the history of proton pump inhibitors and compares and evaluates the pharmacology including mechanism of action, pharmacokinetics, pharmacodynamics, administration, dosage, and drug interactions. Information regarding therapeutic indications, clinical efficacy, short- and long-term side effects, and cost is also presented. A case presentation offers an analysis of the use of proton pump inhibitors in individualized patient care.     

Esomeprazole in treating duodenal ulcer in various modes of anti-Helicobacter therapy

AIM: To assess efficiency of esomeprazole in the treatment of duodenal ulcer (DU) associated with H. pylori in various eradication regimens. MATERIAL AND METHODS: 80 patients with duodenal ulcer at least 0.5 cm in diameter were randomized into three groups. 23 patients of group 1, 28 patients of group 2 received esomeprazole for 7 days in a dose 20 mg twice a day, in a single morning dose 40 mg, respectively. 29 patients of group 3 received omeprazole 20 mg twice a day for 7 days and further 3 weeks 20 mg twice a day. All the patients were also given amoxicillin 1000 mg twice a day and clarithromycin 500 mg twice a day for a week. RESULTS: An antisecretory effect of esomeprazole as shown by 24-h monitoring of gastric secretion was longer and more stable than that of omeprazole: a latent period averaged 1.5 +/- 0.6 h in a pharmacological test with 20 mg esomeprazole, 1.2 +/- 0.4 h in intake of 40 mg esomeprazole and 2.1 +/- 0.3 h in intake of 20 mg omeprazole. Overall duration of the antisecretory effect averaged 16.8 +/- 1.9, 20.3 +/- 1.7 and 12.5 +/- 1.9 h, respectively. The time of intragastric pH > 4 was 13.1 +/- 1.6, 17.2 +/- 1.6 and 9.8 +/- 1.5 hours, respectively. Eradication of H. pylori in group 1, 2 and 3 was 91.3, 89.3 and 89.6%, respectively. Complete epithelization of ulcer occurred in 95.6, 92.8 and 93.1% cases, respectively. In 77 patients who finished the treatment according to the protocol the treatment resulted in eradication in 95.6, 92.5 and 92.8%, respectively; in epithelization--in 100, 96.3 and 96.4% patients of groups 1, 2 and 3, respectively. Side effects were mild or moderate but not causing changes of the regimen or treatment discontinuation. CONCLUSION: Esomeprazole in three-component treatment was highly effective in eradication of H. pylori and epithelisation of duodenal ulcer defects in various regimens of administration. Esomeprazole in combination with amoxicillin and clarithromycin reduces the time of treatment of DU associated with H. pylori to 1 week without further monotherapy with antisecretory drugs.     

Combination drug therapy for gastroesophageal reflux disease

OBJECTIVE: To evaluate the role of combination therapy with proton-pump inhibitors (PPIs) and histamine(2) receptor antagonists in gastroesophageal reflux disease (GERD). DATA SOURCES: Clinical literature identified through MEDLINE (January 1966-August 2001). Key search terms included gastroesophageal reflux, benzimidazoles; omeprazole; lansoprazole; pantoprazole; rabeprazole; receptor antagonists, histamine(2); therapy, combination drug; therapy, combined modality; and combinations, drug. DATA SYNTHESIS: Approximately 80-90% of patients show healing of reflux esophagitis after 8 weeks of once-daily PPI therapy. Patients taking PPI therapy twice daily still have nocturnal acid breakthrough (periods of gastric pH <4 lasting for > or =60 min during the night) as much as 70% of the time. The clinical application of this finding has not been shown. One trial has shown that omeprazole in the morning plus ranitidine at bedtime is not as effective as omeprazole twice daily given before the morning and evening meals at controlling nocturnal acid breakthrough. Further, 1 small trial in healthy subjects without GERD showed that the addition of a 1-time dose of ranitidine at bedtime to a twice-daily regimen of omeprazole may decrease the occurrence of nocturnal acid breakthrough. However, the clinical significance of this finding is not clear. CONCLUSIONS: No studies in patients with GERD demonstrate that the addition of histamine(2) receptor antagonists to twice-daily PPI therapy provides any further benefit above that derived from PPIs alone. The parameter used to measure the efficacy of combination regimens for GERD thus far--nocturnal acid breakthrough--has not been proven to correlate with improvement of GERD symptoms in any controlled or prospective clinical trials. Further investigation is needed to determine optimal therapy in patients refractory to standard doses of PPIs.     

Primary care for GEDR

Current approach for the treatment of gastroesopageal reflux disease (GERD) was reviewed. The most effective treatment of erosive esophagitis or symptomatic GERD is to reduce gastric acid secretion with either an H2 receptor antagonists (H2RA) or a proton pump inhibitor (PPI). The PPI lead to more rapid healing and symptom relief than H2RA. Despite treatment with PPI, some patients with GERD continue to have symptoms or endoscopic evidence of esophagitis. Nocturnal acid breakthrough may be one of the mechanisms responsible for the refractory GERD. There are two approaches to the initial medical treatment of gastroesophageal reflux disease ('step down' therapy or 'step up' approach). Although there are arguments in favour of both approaches, the former is considered to be preferable these days.     

埃索美拉唑在消化性溃疡中的应用现状

埃索美拉唑是新一代质子泵抑制剂成员,有较强的抑制胃酸分泌效应。本文就埃索美拉唑在消化性溃疡的应用进展进行综述。     

HP根除影响胃食管反流病患者预后的临床及病理分析

目的:探讨根除幽门螺杆菌(Helicobacter pylori, HP)对胃食管反流病(gastro esophageal reflux disease, GERD)疗效及预后的影响。方法:98例GERD患者,均为HP阳性,试验前均行胃镜检查评估食管炎程度及胃粘膜组织病理学改变,然后所有患者随机分为2组:HP根除组49例,接受HP清除三联疗法;对照组49例,仅服用奥美拉唑(20 mg,每日2次)。1周后所有患者开始连续8周的奥美拉唑(20 mg/d)初始治疗阶段,8周后症状缓解及糜烂性食管炎愈合患者开始奥美拉唑10 mgd的维持治疗阶段,直至试验第12个月。初始治疗后症状未完全缓解或内镜下食管炎未完全愈合、维持阶段症状或内镜下食管炎复发为失效病例。试验结束时所有患者均行胃镜复查及14 C呼气试验。结果:试验前共有33 例患者(33.7%)内镜检查发现糜烂性食管炎;试验结束后HP根除组47例患者HP转阴(95.9%),HP阳性组3 例转阴(6.1%),两组HP根除率差异显著(P<0.01);HP根除组16例失效,HP阳性组有7例失效,两者相比差异显著(P<0.05);然而,HP阳性组患者胃体萎缩及胃体肠化较HP根除组明显增多。结论:HP根除可降低质子泵抑制剂(PPI)治疗GERD的疗效,同时HP根除对患者胃体萎缩及胃体肠化有预防作用。     

The proton-pump inhibitors: similarities and differences

OBJECTIVE: This paper examines the clinical pharmacology of the proton-pump inhibitors (PPIs) and briefly reviews some comparative studies of these agents. BACKGROUND: PPIs have emerged as the treatment of choice for acid-related diseases, including gastroesophageal reflux disease (GERD) and peptic ulcer disease. Although these drugs-omeprazole, lansoprazole, pantoprazole, and rabeprazole-share a common structure (all are substituted benzimidazoles) and mode of action (inhibition of H+,K+-adenosine triphosphatase [ATPase]), each differs somewhat in its clinical pharmacology. RESULTS: In comparative clinical trials found in MEDLINE, PPIs administered once daily produced endoscopic evidence of healing in >90% of patients with duodenal ulcer after 4 weeks of treatment, in >90% of those with gastric ulcer after 6 weeks of treatment, and in >90% of those with ulcerative or erosive GERD after 8 weeks of treatment. Maintenance therapy with daily doses of a PPI has been shown to be an effective means of preventing GERD relapse. PPIs also inhibit the growth of Helicobacter pylori, now recognized as an important factor in peptic ulcer disease, and, when administered in combination with antibiotics, provide the best treatment for eradication of the bacterium. Rabeprazole has a more rapid onset of H+,K+-ATPase inhibition than the other PPIs and, compared with omeprazole, a greater effect on intragastric pH after the first dose. Omeprazole and lansoprazole have a greater potential for drug-drug interactions than do pantoprazole and rabeprazole. CONCLUSION: Although the individual PPIs have similar efficacy in many cases, differences between them should be considered when choosing a treatment regimen.     

Is ranitidine therapy sufficient for healing peptic ulcers associated with non‐steroidal anti‐inflammatory drug use?

Long-term use of non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of serious gastroduodenal events. To minimise these risks, patients often require concomitant acid-suppressive therapy. We conducted a literature review of clinical trials examining use of ranitidine 150 mg twice daily to heal gastroduodenal ulcers (GU) in NSAID recipients. Seven studies were identified. After 8 weeks' treatment with ranitidine, GU healing rates ranged from 50% to 74% and rates of duodenal ulcer (DU) healing ranged from 81% to 84%. Ranitidine was more effective when NSAIDs were discontinued (healing rates reaching 95% and 100%, respectively). The ulcer healing rate with sucralfate was similar to that of ranitidine. However, proton pump inhibitor (PPI) therapy was associated with significantly greater rates of both GU and DU healing than ranitidine; 8-week GU rates were 92% and 88% with esomeprazole 40 mg and 20 mg, respectively (vs. 74% with ranitidine, p < 0.01). For omeprazole, 8-week healing rates were 87% with omeprazole 40 mg and 84% with omeprazole 20 mg (vs. 64% for ranitidine, p < 0.001), and for lansoprazole the corresponding values were 73-74% and 66-69% for the 30 mg and 15 mg doses, respectively (vs. 50-53% for ranitidine, p < 0.05). In the PPI study reporting DU healing the values were 92% for omeprazole 20 mg (vs. 81% for ranitidine, p < 0.05) and 88% for omeprazole 40 mg (p = 0.17 vs. ranitidine). NSAID-associated GU are more likely to heal when patients receive concomitant treatment with a PPI rather than ranitidine.     

埃索美拉唑预防机械通气患者应激性溃疡的疗效观察

目的：对比埃索美拉唑和奥美拉唑预防机械通气患者应激性溃疡的效果。方法：按照随机数字表随机将214例患者分为埃索美拉唑组（108例）、奥美拉唑组（106例）。观察治疗后一周内2组应激性溃疡的发生率。结果：埃索美拉唑组和奥美拉唑组的SU发生率分别为4.63%、12.26%,2组差异有统计学意义（P〈0.05）。结论：埃索美拉唑较奥美拉唑能更有效预防机械通气患者应激性溃疡的发生。     

埃索美拉唑、克拉霉素与甲硝唑联合治疗消化性溃疡65例

目的研究埃索美拉唑、克拉霉素、甲硝唑三联治疗消化性渍疡的疗效。方法将126例经内镜诊断并检测证实幽门螺杆菌（Hp）阳性的消化性溃疡患者随机分为两组。治疗组65例，给予埃索美拉唑20mg＋克拉霉素500mg＋甲硝唑400mg，每日2次，共7d；对照组61倒，给予奥美拉唑20mg＋克拉霉素500mg＋甲硝唑400mg，每日2次，共7d。疗程结束4周后复查胃镜并检测Hp，观察腹痛缓解率、溃疡愈合率，Hp根除率及用药后的不良反应等。结果治疗组组第1d和第2d腹痛缓解率分别为33．8％和53．8％，高于对照组的16．4％和39．3％，有显著性差异（P〈0．05）。治疗组和对照组溃疡治愈率分别为90．8％和86．9％，治疗组和对照组Hp根除率分别为90．8％和86．9％，差异无显著性（P〉0．05）。两组用药后不良反应少，有较好的安全性。结论埃索美拉唑、克拉霉素、甲硝唑三联疗法治疗Hp阳性的消化性溃疡安全有效，腹痛缓解速度优于奥美拉唑三联疗法。     

Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

OBJECTIVE: To review the pharmacology, pharmacokinetics, safety, and efficacy of sitagliptin, a dipeptidyl peptidase IV (DPP-IV) inhibitor in the management of type 2 diabetes mellitus. DATA SOURCES: A MEDLINE search (1966-February 2006) was conducted for English-language articles using the terms dipeptidyl peptidase IV inhibitor, incretin, MK-0431, and sitagliptin. Abstracts from the American Diabetes Association annual meetings in 2004 and 2005 were included as sources of data. STUDY SELECTION AND DATA EXTRACTION: Articles pertaining to the pharmacology of sitagliptin, its pharmacokinetics, safety and efficacy were reviewed. DATA SYNTHESIS: Sitagliptin is a potent, competitive, reversible inhibitor of the DPP-IV enzyme. It is eliminated renally, with a terminal half-life of 11.8-14.4 hours. In Phase II clinical trials, sitagliptin was found to be superior to placebo for the treatment of type 2 diabetes mellitus. Results of a small trial comparing sitagliptin with glipizide indicate that both treatments are comparable. The efficacy of sitagliptin has also been demonstrated when used as adjunctive therapy with metformin. Few adverse effects have been reported. Weight gain and hypoglycemia have not been seen with sitagliptin therapy. CONCLUSIONS: Based on its unique mechanism of action, sitagliptin will provide practitioners with an additional tool in the treatment of diabetes. Review of the literature to date implies sitagliptin may be effective as monotherapy in type 2 diabetes. In addition, existing evidence supports the use of sitagliptin as adjunct therapy to sulfonylureas and metformin. Another advantage of sitagliptin use is that it appears to be free from the adverse effects of weight gain and hypoglycemia that are associated with currently available treatments.     

A review of omeprazole use in the treatment of acid-related disorders in children

BACKGROUND: Acid peptic disease is a common problem, with a similar prevalence of gastroesophageal reflux disease (GERD) in adults and children. The presentation of GERD in infants and children varies from crying, irritability, or sleep disturbance to feeding difficulties, vomiting, or rumination. Helicobacter pylori (HP)-related diseases and gastric and duodenal ulcers are much more common in adults than in children, who are more likely to have gastritis or duodenitis. However, because HP infection is most likely acquired in childhood, treatment of children with endoscopically documented active HP disease may minimize the potential risk for peptic ulcer or gastric cancer in adulthood, although this is yet to be proved. OBJECTIVE: Omeprazole has been shown to be effective in the treatment of acid-related diseases. This paper reviews the literature on the use and administration of omeprazole for the treatment of GERD, peptic ulcer disease, HP infection, and other acid-related conditions in children. METHODS: Studies were identified through searches of MEDLINE and Science Citation Index for the period 1986 to November 2000, and from the reference lists of identified articles. The search terms used included omeprazole, proton pump inhibitor (PPI), children, pediatrics, routes of administration, GERD, HP infection, esophagitis, and administration. In addition, the manufacturer of omeprazole was asked for relevant unpublished information. RESULTS: Marketed and extemporaneous formulations of omeprazole have been administered to children aged 2 months to 18 years for the treatment of erosive esophagitis, gastric ulcer, duodenal ulcer, HP infection, and related conditions at dosages of 5 to 80 mg/d (0.2-3.5 mg/kg/d) for periods ranging from 14 days to 36 months with a low incidence of adverse effects. The initial dose most consistently reported to heal esophagitis and provide relief of symptoms of GERD appears to be 1 mg/kg per day. CONCLUSIONS: In uncontrolled clinical trials and case reports to date, omeprazole has been effective and well tolerated for the acute and chronic treatment of esophageal and peptic ulcer disease in children, particularly those who had failed to respond to previous treatment with histamine2-receptor antagonists. Should future long-term, controlled clinical trials in children demonstrate safety and efficacy, this PPI is likely to find a place in the armamentarium of pediatric pharmacotherapy.