On an empty stomach or not?

[Triton]

Esomeprazole and other PPI should be taken at least an hour before breakfast, am I right? Why the hell in the leaflet is: can be taken with food?!

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[legaia]

Well, it can be taken w/ food.

 

[Triton]

My understanding has always been that proton pumps are mainly activated by food, therefore PPI should be taken before meals.

It strikes me I will have to revise my opinion of the issue.

however as far as I know Lansoprazole might be an exception to the rule.

 

[BMBiology]

Food decreases absorption. Therefore, it should be taken before meals. Is it an absolute requirement? No but it works better that way.

 

[acetyl]

PPI's are pro-drugs of sort in the sense that they become activated by acidic environments. The parent molecule doesn't do the dirty work. Most are enteric coated or buffered anyway so the acid produced from food shouldn't bother them that much. This is why it says either food or empty stomach. However, if the drug does release into the stomach, the acid activates it and it won't be functional.

After dissolution in the duodenum, absorbtion occurs, and eventually drug reaches the parietal cells. Upon entering the lumen, the acid production inside the lumen of the parietal cells activates the pro-drug type compound allowing it to covalent modify the acid pump. So the idea is that acid production is thought to be generally highest in the morning, so taking the drug 30 minutes prior to eating will allow systemic absorption, and better modification of acid pumps because more pumps are activated and thus in an acidic environment necessary to activate the drug.

 

[BMBiology]

Acid production being the highest in the morning may be correct as well. This is from Lexi-Comp on nexium:

Ethanol/Nutrition/Herb Interactions Food: Absorption is decreased by 43% to 53% when taken with food.

 

[Quiksilver]

PPI's are pro-drugs of sort in the sense that they become activated by acidic environments. The parent molecule doesn't do the dirty work. Most are enteric coated or buffered anyway so the acid produced from food shouldn't bother them that much. This is why it says either food or empty stomach. However, if the drug does release into the stomach, the acid activates it and it won't be functional.

After dissolution in the duodenum, absorbtion occurs, and eventually drug reaches the parietal cells. Upon entering the lumen, the acid production inside the lumen of the parietal cells activates the pro-drug type compound allowing it to covalent modify the acid pump. So the idea is that acid production is thought to be generally highest in the morning, so taking the drug 30 minutes prior to eating will allow systemic absorption, and better modification of acid pumps because more pumps are activated and thus in an acidic environment necessary to activate the drug.

i guess only to add to your explanation:

the drug may be buffered but the problem with taking it with food or around meal times is that food slows down gastric emptying and thus as a result of that you see the dissolution of the enteric coating much too soon since it is spending way too long in the acidic stomach. So it should not say "take with food". This exposure to the acidic environment is why bioavailability goes in the crapper.

You also want to make a point of telling pts this "take 1/2 hour AC" because of the interpatient differences with these PPIs. You don't necessarily want a false positive thinking that its one of those patients that the medication does not work on, when in reality the patient just took it with meals.

however this also depends on the formulation, protonix tablets according to clinical pharm do not show a difference in absorption kinetics when taken with or without food. My guess is that it applies more to Nexium, Prilosec and Prevacid (capsules and OTC formulation). Food for thought