Proton pump inhibitors

Proton pump inhibitors belong to a drug group that is one of the strongest sales drivers worldwide. The drugs inhibit the proton potassium pump, an enzyme that acts as a proton pump in the parietal cells of the stomach for the production and release of gastric acid. The drugs are therefore mainly used against ailments and diseases that can be associated with increased gastric acid production.

What are proton pump inhibitors?

Proton pump inhibitors, also called Proton pump inhibitors (PPI) or simply as Acid blockers called, inhibit the proton potassium pump in the parietal cells of the gastric mucosa. It is the enzyme H + / K + -ATPase, which is responsible for the release of protons (H +) and the introduction of K + ions in the parietal cells of the stomach.

The protons combine with negative chloride ions to form hydrochloric acid (HCl). The energy required is obtained from the conversion of ATP (adenosine triphosphate) into ADP (adenosine diphosphate). By inhibiting or blocking the process, most of the hydrochloric acid production in the stomach is prevented.

The so-called parietal cells or parietal cells are located in certain areas of the gastric mucosa. In addition to hydrochloric acid, they also release the important intrinsic factor, which binds the acid-sensitive vitamin B12 in the stomach and carries the vitamin to the end of the small intestine, where it is released again and then absorbed.

Pharmacological effect on the body and organs

Proton pump inhibitors block the H + / K + -ATPases in the parietal cells of the gastric mucosa. The specific ATPases are transmembrane proteins that channel positively charged hydrogen ions (protons) out of the cytoplasm against an electrochemical gradient and channel positive K + ions into the cytoplasm. The “transmembrane sluice enzyme” draws the necessary energy through hydrolytic cleavage of a phosphate residue from the ATP, which becomes ADP with only two phosphate residues.

Since all previously known proton pump inhibitors are acid-sensitive, they are offered in an enteric form. The medicinal substances are only released and absorbed in the small intestine. The active substance of the PPIs reaches the parietal cells via the bloodstream and blocks the H + / K + -ATPases directly in the secretory ducts of the parietal cells.

Because of the long distance that the active pharmaceutical ingredient has to travel via the stomach, small intestine and bloodstream before it can take effect in the parietal cells, it takes about one and a half hours after taking the preparation before it takes effect. The irreversible blockade of the enzyme ensures a strong reduction in hydrochloric acid production in the stomach, which can even come to a complete standstill.

The pH value of the digestive juices in the stomach rises sharply and becomes less aggressive. On the one hand, this is intentional in order to achieve certain effects, on the other hand, the higher pH value influences digestion. For example, the breakdown of long-chain proteins and the absorption of certain minerals such as calcium and magnesium are made more difficult.

Another effect of the acid blockers results in the parietal cells themselves. In addition to acid production, they are also responsible for the secretion of the intrinsic factor. It is a special glycoprotein that binds the acid-sensitive vitamin B12 (cobalamin) from the food pulp and carries it to the lower part of the small intestine, where it is released and absorbed again.

The PPIs also - unintentionally - reduce the release of the intrinsic factor, so that long-term use can lead to problems due to an insufficient supply of vitamin B12.

Medical application & use for treatment & prevention

Proton pump inhibitors are primarily used to treat esophageal reflux and problems with the lining of the stomach. Frequent reflux of acidic stomach contents into the esophagus often causes inflammation there, in some cases even in the throat. Curbing acid production can provide relief.

People who react particularly strongly to stressful situations tend to produce a pathologically increased amount of gastric acid due to an increased concentration of stress hormones. This is why PPIs are often used to prevent backflow into the esophagus (gullet).

In the case of gastritis or gastric ulcers, a less acidic environment in the gastric juices supports healing. PPIs are also used to support the treatment of a duodenal ulcer (ulcus duodeni).

Another area of ​​application is so-called stomach protection when taking nonsteroidal anti-inflammatory drugs (NSAIDs) over the long term. NSAIDs contain anti-inflammatory agents, the main action of which is to block cyclooxygenases (COX), which play an important role in the sensation of pain. Inhibiting the tissue hormone COX therefore has a pain-relieving effect, among other things. However, NSAIDs also have an inhibiting effect on the gastric mucous membrane formation, so that the protective effect of the gastric mucus is reduced. The additional intake of PPIs therefore serves to protect the gastric mucosa by increasing the pH value.

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Risks & side effects

A short-term use of PPIs is associated with few risks. In rare cases, there are unspecific symptoms such as abdominal pain, diarrhea or dizziness and headaches, which subside after a period of getting used to.

The real risks mainly arise with long-term therapies. A general problem arises from the higher pH in the stomach. This makes it more difficult to break down large-molecule proteins and remove minerals and trace elements from the food pulp.

Another problem area is the reduction of the intrinsic factor by taking PPIs. It is a special glycoprotein that binds the acid-sensitive vitamin B12 (cobalamin) from the food pulp in the stomach and can thus protect against hydrochloric acid. In the long term, this can lead to a deficiency in vitamin B12 with the development of corresponding deficiency symptoms such as mild to severe neurological problems or arteriosclerosis.