The effects of dose and timing of esomeprazole administration on 24‐h, daytime and night‐time acid inhibition in healthy volunteers

BACKGROUND: Symptoms of gastro-oesophageal reflux disease (GERD) may persist despite daily treatment with a proton pump inhibitor (PPI). AIM: To compare the pharmacodynamic effect of various esomeprazole dosage and timing regimens in healthy volunteers. METHODS: The effect of different esomeprazole dosage regimens [20 mg once daily (od) before breakfast or dinner; 20 mg twice daily (b.d.); 40 mg od before breakfast, dinner or at bedtime; and 40 mg b.d.] on 24-h, daytime and night-time acid inhibition was evaluated in a randomized, seven-way crossover study in healthy volunteers. Each regimen was taken for 5 days. RESULTS: Over the 24-h period (day 5), esomeprazole 20 mg b.d. was associated with superior acid inhibition vs. all 20 mg and 40 mg od regimens (P < 0.05), but was less effective than esomeprazole 40 mg b.d. (P < 0.05). Dosing with esomeprazole 20 mg or 40 mg od before breakfast gave improved 24-h and daytime acid inhibition vs. the corresponding administration before dinner or at bedtime (all P < 0.05). Night-time acid inhibition was improved when esomeprazole 40 mg od was administered before dinner or at bedtime vs. before-breakfast dosing (P < 0.05). CONCLUSION: Varying the dose and timing of esomeprazole administration may provide acid inhibition appropriate for the symptom pattern of individual patients with GERD.