Intravenous Esomeprazole 40mg is Effective for the Control of Intragastric Acid Levels Whether Given as a 3-Minute Injection or a 30-Minute Infusion.

BACKGROUND: An intravenous (IV) formulation of esomeprazole has been developed as an alternative to oral administration. To meet the needs of different clinical situations it would be preferable if an IV dose could be administered as either an injection or an infusion, while producing similar effects. AIM: To compare the effects of IV esomeprazole 40mg given as a 3-minute injection or a 30-minute infusion on intragastric pH during single and repeated once-daily dosing in healthy subjects. METHODS: In this single-centre, double-blind, double-dummy, randomised, two- way crossover study, subjects were randomised to receive either a 3-minute IV injection or a 30-minute IV infusion of esomeprazole 40mg. Both regimens were given once daily for 10 days. After a washout period of at least 13 days, subjects were crossed over to the other treatment. Intragastric pH monitoring was performed on days 1 and 10. Blood samples were also taken throughout days 1 and 10. RESULTS: Data were available from 41 subjects. Time with intragastric pH >4 was 3.1h/24h at baseline, increasing to almost 8h in association with IV esomeprazole injection or infusion on day 1, and to >13h on day 10. Geometric mean time with pH >4/24h ratios (injection/infusion) were 0.99 on day 1 and 1.03 on day 10. Mean esomeprazole AUC values were approximately 15% higher with the injection than the infusion, but 90% CI limits for geometric mean AUC ratios ranged from 1.07 to 1.23, indicating bioequivalence. CONCLUSIONS: IV esomeprazole 40mg provides similarly potent acid control whether administered by injection or infusion.

Acid control with esomeprazole and lansoprazole: a comparative dose-response study.

OBJECTIVE: To determine the level of acid control and the dose-response relationships achieved with esomeprazole and lansoprazole. These data are relevant in helping clinicians to decide on whether to increase a proton-pump inhibitor dose, or whether to switch to an alterative drug for increased acid control. MATERIAL AND METHODS: In an open-label, single-centre, randomized, six-way crossover study, 40 healthy subjects received esomeprazole 20, 40 and 80 mg, and lansoprazole 15, 30 and 60 mg once daily for 5 days. The mean time with intragastric pH >4 and mean 24-h median intragastric pH on day 5 were analyzed using a mixed-model ANOVA. Post-hoc analyses were completed for 0-12-h (daytime) and 12-24-h (night-time) post-dose intervals. RESULTS: Increasing the dose of esomeprazole from 20 mg to 40 mg resulted in significantly improved acid control over 0-12, 12-24 and 0-24 h post-dose (p<0.001), but no significant improvement in acid control for either period was seen when further increasing the dose to 80 mg. Increasing the dose of lansoprazole from 15 mg to 30 mg or from 30 mg to 60 mg significantly improved acid control over 0-12 and 0-24 h (p<0.01) but not over 12-24 h. With the exception of the esomeprazole 20 mg versus lansoprazole 30 mg comparisons, and the esomeprazole 20 mg versus lansoprazole 15 mg during 12-24 h post-dose comparison, esomeprazole provided significantly greater acid control than lansoprazole at each dose level over 0-12, 12-24 and 0-24 h (p<0.05). Mean 24-h median intragastric pH was higher following esomeprazole dosing compared with lansoprazole at each dose level. CONCLUSIONS: For low-, standard- and double-dose comparisons, esomeprazole achieved greater elevation of gastric pH and better acid control in more subjects than lansoprazole. Use of esomeprazole may therefore reduce the need for dose adaptations or drug switching.

Esomeprazole 40 mg provides improved intragastric acid control as compared with lansoprazole 30 mg and rabeprazole 20 mg in healthy volunteers.

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 > or =12 h and > or =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.