Drug

Proton pump inhibitor (PPI)

Synonyms in a broader sense

Proton pump inhibitors
PPI
Gastric acid blockers
Nexium® MUPS
Agopton®
Lansogamma®
Lansoprazole ratiopharm
Antra® MUPS
Omegamma®
Omep®
Omeprazole STADA
Ulcozol®
Pariet®
Pantozol®
Pantoprazole®
Rifun®

definition

Proton pump inhibitors (short: PPI; = proton pump inhibitors) are very effective drugs for the treatment of gastric acid-related symptoms such as heartburn, esophagitis or gastric ulcers. Proton pump inhibitors (PPIs) block the function of stomach acid-producing cells. Symptoms are alleviated and inflammation can heal better. In addition, PPIs can counteract the gastric damaging effects of non-steroidal anti-inflammatory drugs (NSAIDs).

What are proton pumps?

Proton pumps, also called proton potassium ATPases, are gastric acid-producing units in the stomach wall (see anatomy stomach). You can find them in the so-called Parietal cells. As the name suggests, proton pumps transport protons into the stomach. The higher the number of protons, the stronger the stomach acid. The number of protons is a measure of the acid strength and is determined by the so-called PH value expressed (Scale 1-14). The lower the pH, the higher the proton concentration and the acid strength. There is usually one in the stomach pH of 1.5, so a very acidic environment.

Gastric acid-related diseases

Stomach acid is necessary for the digestion of protein from food. In addition, digestive enzymes like pepsin can only work effectively in an acidic environment. In addition, the stomach acid disinfects the food from germs.
The stomach wall is lined with an acid-insensitive protective film so that the stomach does not digest itself. Certain drugs, such as non-steroidal anti-inflammatory drugs (NSAIDs), can attack this protective film. This can lead to inflammation of the stomach wall (gastritis, ulcus ventriculi).
The esophagus is separated from the stomach by a "valve", the esophageal sphincter, so that the acidic chyme does not flow back. If this does happen, the irritation of the acid-sensitive esophagus manifests itself as heartburn (see also reflux disease / reflux). If a patient suffers from heartburn more often, the permanent irritation of the esophageal lining can lead to inflammation (reflux esophagitis).

Illustration heartburn

Esophagus (esophagus)
stomach

The detail shows the leaky gastric entrance, which allows acidic porridge to flow back through the esophagus.

Use of proton pump inhibitors

Heartburn is an unpleasant symptom that can take various forms. Mild forms can usually be resolved by changing lifestyle and taking Antacids (Gastric acid binding drugs). However, if acid-related stomach problems and heartburn occur relatively often, you should have the cause clarified by a doctor. You may have an underlying disease that requires treatment, for which antacids are not an effective treatment. Proton pump inhibitors are mostly used here. Unlike antacids, these cannot be sold over the counter in pharmacies because they require a medical diagnosis! Proton pump inhibitors (PPIs) inhibit stomach acid production. Due to the low acidity of the stomach, heartburn and stomach pain quickly, because the mucous membranes are less irritated. The healing process of esophagitis or inflammation of the gastric wall healing process is thus effectively supported by PPIs. Patients in whom the Reflux has anatomical causes, such as the Diaphragmatic hernia (Hiatal hernia) have a higher risk of developing esophagitis. Therefore it makes sense to continue to administer proton pump inhibitors (PPIs) prophylactically even after the inflammation has been successfully treated.

In patients with a diaphragmatic hernia, PPIs are a therapeutic alternative to surgery.

Active substances that belong to the non-steroidal anti-inflammatory drugs (NSAIDs), such as Acetylsalicylic acid, Diclofenac or Ibuprofen, can attack the protective layer of the stomach. Patients who are treated with NSAIDs as part of long-term therapy should therefore also take a proton pump inhibitor.

Read more on this topic at: Heartburn medication

How do proton pump inhibitors work?

Proton pump inhibitors (PPIs) are mainly available in tablet form, but also as capsules. However, their active ingredients are acid-unstable. The acidic gastric juice would break down the active ingredient before it reaches its destination. In order to transport the active ingredient undamaged to its destination, the proton pumps in the stomach wall, one takes a detour.

The dosage form is covered with a protective layer so that it passes through the stomach undamaged and reaches the small intestine. Only then can it dissolve because the pH value is higher. The active ingredient is released, absorbed into the blood through the mucous membrane of the small intestine and transported to the proton pumps.

Info: How the proton pump inhibitors work

Proton pump inhibitors irreversibly block the proton pumps so that they become inoperable and die. As a result, the gastric juice becomes less acidic. The pH value in the stomach rises to values between 3-4. Approx. One third of the proton pumps are formed every day, so that acid production can only be reduced for approx. 24 hours. After that, you need to take another tablet or capsule.

Note: taking proton pump inhibitors (PPIs)

It is very important that the tablets must not be broken up, chewed or pounded beforehand! They should be swallowed whole so that the acid-resistant coating remains functional. Otherwise the tablet will be ineffective. PPIs in the form of capsules can be opened, but neither should the contents be chewed or pounded.

The standard dose, independent of the active ingredient, is 20 mg / day, unless your doctor prescribes otherwise. Patients who have been prescribed proton pump inhibitors (PPIs) to treat heartburn are usually symptom-free after 5 days. Thereafter, it can be used as required, unless otherwise prescribed!

If after 14 days of regular use there is still no noticeable relief, consult your doctor to clarify further causes. If PPIs are prescribed to treat gastric ulcer or esophagitis, they should be taken regularly over a period of 4-6 weeks. Even if the symptoms disappear after a few days, the healing process takes longer.

Read a lot more information on this topic at: Effect of proton pump inhibitors

Sneak out

Unlike many other drugs, proton pump inhibitors do not necessarily have to be tapered off when they are stopped. Like any other medication, however, these should only be discontinued on the order of a doctor. Under certain circumstances, it can still make sense to reduce the dosage only gradually, for example to prevent the recurrence of symptoms.

Side effects

Proton pump inhibitors (PPIs) are usually well tolerated and have few side effects.

There may be temporary upper abdominal complaints such as:

stomach pain
nausea
Vomit
diarrhea
constipation
or
Flatulence.

Occasionally, you experience tiredness, difficulty sleeping, dizziness and headache. Accidental overdoses usually do not cause any complaints.

A complete inhibition of the acid production is not to be feared, since proton pumps are constantly being formed anew. A third of all proton pumps are renewed every day. In the context of long-term therapy, the question arises whether the lower acid content of the gastric juice no longer kills pathogens sufficiently. However, serious illnesses have not yet been observed.

Side effects on the bone

Among the possible side effects that can occur from taking proton pump inhibitors, fractures of the hip, wrist, or vertebrae are listed as uncommon. This means that such a side effect is to be feared in about one to ten in 1000 users.

However, there is only a connection to the fact that the drug can slightly increase the risk of a bone fracture if there is already an existing risk. Patients who suffer from osteoporosis (bone loss) or who are being treated with cortisone preparations at the same time are at such a risk and should therefore not be treated with proton pump inhibitors over the long term.

Interactions

The release of active ingredients in some drugs depends on the acidity of the gastric juice. If the acid content is reduced, these can no longer work properly. Like many drugs, proton pump inhibitors are broken down in the liver. If you are dependent on taking other medication, the breakdown can be mutually delayed. For these reasons, please inform your doctor if you are taking other medication at the same time. Interactions were i.a. observed between taking proton pump inhibitors and atazanavir, antibiotics (clarithromycin, erythromycin, roxithromycin), diazepam, digitoxin and St. John's wort.

Medication overview

Esomeprazole: Nexium® MUPS
Lansoprazole: Agopton®, Lansogamma®, Lansoprazol-ratiopharm
Omeprazole: Antra® MUPS, Omegamma®, Omep®, Omeprazol STADA, Ulcozol®
Rabeprazole: Pariet®
Pantoprazole: Pantozol®, Pantoprazol®, Rifun®

What are the alternatives?

In addition to the most commonly prescribed proton pump inhibitors, there are other drugs that use other mechanisms of action to inhibit acid formation in the stomach. The so-called histamine H2 receptor blocker is a frequently prescribed alternative Ranitidine represent.

In addition to conventional medical products, herbal or alternative medicine alternatives are also promising for many diseases. A healthy and balanced diet and avoidance of irritating stimulants such as coffee or alcohol can in many cases alleviate the symptoms better than by taking a proton pump inhibitor.

In the case of a serious illness, such as pronounced inflammation of the esophagus, a proton pump inhibitor should usually be taken, as alternative measures alone are not sufficient.