Rabeprazole

A multicenter randomized trial comparing rabeprazole and itopride in patients with functional dyspepsia in Japan: the NAGOYA study.[Pubmed:28366993]

J Clin Biochem Nutr. 2017 Mar;60(2):130-135.

The aims of this study were to compare the therapeutic effects of a proton pump inhibitor (PPI), Rabeprazole (RPZ), and a prokinetic agent, itopride (ITO), and to investigate the role of PPI in the treatment strategy for Japanese functional dyspepsia (FD) patients. We randomly assigned 134 patients diagnosed by Rome III criteria to 4 weeks treatment with RPZ 10 mg/day (n = 69) or ITO 150 mg/day (n = 65). Dyspeptic symptoms were evaluated using FD scores at baseline and after 1, 2 and 4 weeks of treatment. We also divided subjects into predominantly epigastric pain syndrome (EPS) or postprandial distress syndrome (PDS), and evaluated the efficacy of RPZ and ITO respectively. RPZ showed a significant decrease in the Rate of Change (RC) in FD score within 1 week, which was maintained until after 4 weeks, with RPZ a significant effect compared with ITO at all evaluation points. In addition, RPZ showed a significant decrease in FD score in subjects with both EPS and PDS, whereas a significant decrease in the RC with ITO was only shown in those with predominant PDS. Acid-suppressive therapy with RPZ is useful for PDS as well EPS in Japanese FD patients (UMIN Clinical Trials Registry number: UMIN 000013962).

Stereoselective and nonstereoselective pharmacokinetics of rabeprazole - an overview.[Pubmed:28294690]

Xenobiotica. 2018 Apr;48(4):422-432.

1. Proton pump inhibitors have been extensively used for the treatment of ailments due to increased gastric acid secretion such as peptic ulcers, gastroesophageal reflux disease, etc. 2. There are several approved drugs in the proton pump inhibitor class with the latest entries representing single enantiomer drugs of the previously approved racemic drugs. 3. Despite having a high degree of structural resemblance, Rabeprazole, was shown to possess some unique differentiation from other drugs in the class. One of the key distinguishing features of Rabeprazole was related to the lesser involvement of polymorphic metabolism in its pharmacokinetic disposition. 4. The review was aimed to provide pharmacokinetic data of Rabeprazole from several clinical studies including drug-drug interaction studies where Rabeprazole was either a perpetrator drug or victim drug. 5. Additional perspectives on therapy considerations due to the unique metabolic disposition of Rabeprazole including the possible issues related to chirality were provided.

Determination of rabeprazole enantiomers in commercial tablets using immobilized cellulose-based stationary phase.[Pubmed:28229392]

Arch Pharm Res. 2017 Mar;40(3):373-381.

Rabeprazole is one of the latest proton-pump inhibitors used for treatment of several gastrointestinal disorders. For therapeutic applications, Rabeprazole has been administered as a mixture of R-(+) and S-(-) enantiomers. Owing to pharmacological and toxicological differences between stereoisomers, chiral recognition has now become an integral part of drug research and development. A simple and rapid liquid chromatographic method for enantioselective separation and determination of R-(+) and S-(-) enantiomers of Rabeprazole in bulk drug and pharmaceutical formulations was developed. Chiralpak IC (150 x 4.6 mm, 5 mum) column and mumobile phase containing hexane:ethanol:ethylenediamine (30:70:0.05 v/v) in an isocratic mode yielded baseline separation with resolution greater than 6.0 at 35 degrees C. Effects of additives and n-hexane were evaluated. Optimized condition was validated as per ICH guidelines. The method has good linearity, high sensitivity with LOD was 0.01 mug/mL and LOQ was 0.03 mug/mL for both enantiomers. Intra-day precision varied between 0.44 and 1.79% for S-(-) enantiomer, 0.65 and 1.97% for R-(+) enantiomer. Relative standard deviations of inter-day precision were less than 1.81% for both enantiomers. The percentage recovery for both enantiomers of Rabeprazole ranged between 99.81 and 101.95%, 98.82 and 101.36% in material and tablets, respectively. The method was successfully applied to determine content of each enantiomer in commercial tablets.

A Multicenter, Randomized, Open-Label Trial: Efficacy of Once-Daily Versus Twice-Daily Double-Dose Rabeprazole on Refractory Gastroesophageal Reflux Disease-Related Symptoms and Quality of Life.[Pubmed:28066515]

Curr Ther Res Clin Exp. 2016 Nov 25;79:1-7.

BACKGROUND: Approximately 20% to 40% of patients with gastroesophageal reflux disease (GERD) are refractory to standard-dose proton-pump inhibitor (PPI) treatment. OBJECTIVE: We compared the efficacy and quality-of-life effects of 20 mg once daily (QD) versus 10 mg twice daily (BID) Rabeprazole (RPZ) in patients with refractory GERD-related symptoms and sleep disturbances. METHODS: This multicenter, prospective, randomized, open-label study included patients in whom PPI treatment >4 weeks was ineffective. According to the Global Overall Symptom (GOS) scale, PPI-refractory GERD was defined as >/=1 category with >3 points among 10 specific upper gastrointestinal symptoms. Seventy-eight patients were randomly assigned to 20 mg QD and 10 mg BID RPZ groups for 8 weeks. Efficacy was evaluated using self-reported questionnaires, including the GOS scale and Pittsburg Sleep Quality Index (PSQI), whereas quality of life was assessed using the Short-Form 8 Health Survey (SF-8), at 4 and 8 weeks. Patients showing improvement at 8 weeks received follow-up every 4 to 8 weeks. RESULTS: GOS scale scores were significantly improved at 8 weeks in both groups, with no significant intergroup differences. Although SF-8 scores showed an increasing trend over 8 weeks in both groups, the physical component summaries in the 10 mg BID group significantly improved. The mental component summaries clearly improved in the 10 mg BID group. Of the 74 cases (4 missing), 51 (68.9%) had PSQI scores >/=5.5. PSQI scores remained unchanged during follow-up in both groups. The recurrence rate was not significantly different (46.1% vs 47.1% in the 20 mg QD and 10 mg BID groups, respectively) during the follow-up period at median (interquartile range) 24.0 (30.5) months. CONCLUSIONS: In patients with refractory GERD, there was no significant difference in GOS scale score, PSQI, or recurrence rate between the groups. With regard to subscores of the SF-8, the 10 mg BID group might be potentially effective.