Proton pump inhibitors: better acid suppression when taken before a meal than without a meal

Abstract

Background: Proton pump inhibitors including omeprazole and lansoprazole inhibit gastric acid secretion by selectively and non‐competitively inactivating the H+, K+ ATPase molecules of the parietal cell, but possibly only those that are actively secreting acid. This might imply that stimulation of acid secretion by a meal is necessary for optimal inhibition of gastric secretion. Aim: To quantify and compare the effect on daytime gastric acidity of omeprazole 20 mg or lansoprazole 30 mg daily taken 15 min before breakfast, with that of the same drug taken without a meal. Methods: Twenty‐one healthy volunteers were randomized to receive either omeprazole or lansoprazole. They were given the drug for two separate periods of 7 days in randomized order and at least 7 days apart. During one period the study medication was taken before breakfast; during the other it was taken at the same hour, but with no meal until 12:00 hours. Lunch was standardized. On day 7, intragastric pH‐metry was performed, starting at 08:00 hours. Tracings were analysed for the 8‐h period from 08:00 hours until 16:00 hours with regard to percentage time for which gastric pH was below 4.0 and 3.0, and median gastric pH. Tracings were also analysed after removing the 1 h breakfast period, to exclude the buffering effect of the meal. Results: When taking the drug with breakfast, the median percentage time for which gastric pH < 4.0 was 17.2 (interquartile range 4.6–45.5), compared with 42.0 (interquartile range 31.4–48.8) when taken without food (P=0.01). Fifteen subjects had better control of gastric acidity when the medication was taken with breakfast. A pH threshold of 3 and median pH showed similar differences. When the breakfast period was removed, the differences were no longer statistically significant. Conclusions: When therapy with omeprazole or lansoprazole is indicated, medication should be taken before a meal for optimal control of daytime gastric acidity.

Proton pump inhibitors: from CYP2C19 pharmacogenetics to precision medicine

“…The optimal activity of PPIs is achieved when they are administered on an empty stomach, preferably 30–60 min before meals. Taking PPIs on an empty stomach not only improves their absorption, but also ensures that their peak plasma levels match the presence of a large pool of pumps that get activated by presence of food [5,17]. Patients are therefore advised to take their PPIs in a fasting state to ensure maximum absorption and activation of PPIs.…”

Comparison of the effects of immediate‐release omeprazole powder for oral suspension and pantoprazole delayed‐release tablets on nocturnal acid breakthrough in patients with symptomatic gastro‐oesophageal reflux disease

“…However, the explanation may lie in the requirement for gastric proton pumps to be in an active state in order to be maximally inhibited by a PPI. Delayed-release PPIs are often administered in conjunction with a meal to take advantage of the active pump status achieved by the meal itself, 8,9 and they may be less effective after bedtime dosing when that stimulus is not present. It may be that the rapid neutralization of the gastric acid contents by the sodium bicarbonate in the IR-OME formulation is sufficient to activate the proton pumps, rendering them more susceptible to the substantial plasma concentrations of omeprazole achieved within minutes of acid neutralization by the sodium bicarbonate.…”

Treatment Strategy for Standard-Dose Proton Pump Inhibitor-Resistant Reflux Esophagitis

“…To maximize the effect of a PPI, it is necessary to set its peak circulating concentration after a meal. Since the blood concentration of PPI reaches a peak 2 3 hours after oral administration, it is considered effective to administer PPI 1 hour before a meal 22 . In addition, it is effective to administer PPI before dinner 23 , because the largest number of proton pumps appear on the membranes of secretory canaliculi after dinner, which is generally the most substantial meal of the day.…”