Esomeprazole 40 mg Provides Improved Intragastric Acid Control as Compared with Lansoprazole 30 mg and Rabeprazole 20 mg in Healthy Volunteers

Abstract

Aim: To compare the effects of standard-dose esomeprazole with those of standard doses of lansoprazole and rabeprazole on intragastric pH during repeated daily oral dosing in healthy volunteers. Methods: In two standardized, randomized crossover studies, Helicobacter pylori negative healthy volunteers (study A: 19 males, 5 females; study B: 13 males, 10 females) received esomeprazole 40 mg and either lansoprazole 30 mg (study A) or rabeprazole 20 mg (study B) orally once daily in the morning for 5 days. Continuous 24-hour intragastric pH recording was performed on day 5. Results: The intragastric pH was maintained >4 for 65% (95% CI 59.5–71.3) of the 24-hour period with esomeprazole and for 53% of the time (95% CI 47.0–58.9) with lansoprazole in study A (p < 0.001). In study B, the proportion of time with pH >4 was 61% (95% CI 53.6–68.3) with esomeprazole versus 45% (95% CI 37.7–52.5) with rabeprazole (p = 0.005). The 24-hour median pH and the proportion of volunteers with intragastric pH >4 for ≧12 h and ≧16 h were significantly higher with esomeprazole than with either lansoprazole or rabeprazole. Conclusion: Esomeprazole 40 mg provides significantly more effective and more sustained gastric acid control than lansoprazole 30 mg or rabeprazole 20 mg in healthy volunteers.

Efficacy of esomeprazole in treating acid-related diseases in Japanese populations

“…However, rabeprazole at 20 mg increased intragastric pH compared with esomeprazole at 20 mg on Day 1 and showed a higher AUC and intragastric pH on Day 118 while also producing greater acid suppression on Day 1 than esomeprazole at 40 mg, particularly at night 19. Findings from these studies suggest that rabeprazole has a faster onset of acid inhibitory action than esomeprazole at either 20 or 40 mg from Day 1,19 although esomeprazole remains the most effective PPI from Day 5 20. Physicians should therefore consider the time and onset of treatment when selecting a PPI.…”

Proton pump inhibitors: from CYP2C19 pharmacogenetics to precision medicine

“…While some studies have documented genotype dependent differences in acid suppression and outcomes, others showed no relation between genotype and degree of acid suppression or outcomes for rabeprazole and esomeprazole [40,48,53,71,73,108]. This may be attributed in part to their lesser dependence on CYP2C19 metabolism, the higher potency of these PPIs [53,109,110], compared to other PPIs, lack of *17 testing [71], or combination of these factors, leading to diminished differences between the different CYP2C19 metabolizer phenotypes. Although the CYP2C19 genotype dependent increase of AUC in patients with PM phenotype may be less for PPIs that are minimally metabolized by CYP2C19, such as rabeprazole, the elevation in drug concentrations may still pose a risk of adverse events given its high potency.…”

A comparison of esomeprazole and lansoprazole for control of intragastric pH in patients with symptoms of gastro‐oesophageal reflux disease

“…Previous studies have demonstrated that intragastric acid is more effectively controlled with esomeprazole than rabeprazole, omeprazole, lansoprazole and pantoprazole, as measured by the percentage of time pH > 4.0 and mean 24-hour pH. [14][15][16][17] In a five-way crossover study, standard-dose esomeprazole also was shown to provide a greater mean number of hours in a 24-hour period with pH above prespecified thresholds (between 2.0 and 6.0) than standard doses of rabeprazole, omeprazole, lansoprazole and pantoprazole. 17 These results are consistent with those of previous studies comparing standard and escalated doses of esomeprazole, either alone or in comparison with other PPIs.…”

“…[11][12][13] Intragastric acid is more effectively controlled with the standard dose of esomeprazole (40 mg once daily) than standard doses of all other PPIs, as measured by the percentage of time pH > 4.0 and mean 24-hour pH. [14][15][16][17] Furthermore, esomeprazole provides complete heartburn relief in the majority of patients with GERD.…”