Which of the hippies does not give weight gain. Proton pump inhibitors: new safety data. Class-specific side effects: infectious complications

(they are also proton pump inhibitors, proton pump blockers, hydrogen pump blockers, blockers H + /K+ -ATPases, most often reduction of PPI, sometimes - PPI) are drugs that regulate and suppress the secretion of hydrochloric acid. Designed for the treatment of gastritis, and other diseases associated with high acidity.

There are several generations of PPIs, which differ from each other by additional radicals in the molecule, due to which the duration of the therapeutic effect of the drug and the speed of its onset change, the side effects of the previous drugs are eliminated, and the interaction with other drugs is regulated. There are 6 types of inhibitors registered in Russia.

By generations

1st generation

2nd generation

3rd generation

There is also Dexrabeprazole, an optical isomer of rabeprazole, but it does not yet have state registration in Russia.

By active ingredients

Preparations based on omeprazole

Lansoprazole based preparations

Rabeprazole based drugs

Pantoprazole based preparations

Esomeprazole preparations

Dexlansoprazole based preparations

Dexilant. It is used to treat ulcers in the esophagus and to relieve heartburn. Practically not popular with doctors as a drug for the treatment of gastric ulcer. The capsule contains 2 types of granules, which dissolve at different times, depending on the pH level. USA.

When prescribing a certain group of "prazoles", the question always arises: "Which drug is better to choose - the original or its generic?" For the most part, original means are considered more effective, since they have been studied for many years in the molecular stage, then preclinical and clinical trials, interactions with other substances, etc. have been carried out. The quality of raw materials, as a rule, is better. Manufacturing technologies are more modern. All this directly affects the speed of the onset of the effect, the therapeutic effect itself, the presence of side effects, etc.

If you choose analogs, it is better to give preference to drugs made in Slovenia and Germany. They are sensitive to each stage of drug production.

Indications for admission

All proton pump blockers are used to treat gastrointestinal diseases:

Features of the use of PPIs for various pathologies

These drugs are used only in conditions where the acidity of the gastric juice is increased, since they change into their active form only at a certain pH level. This should be understood in order not to diagnose ourselves and not to prescribe treatment without a doctor.

Low acid gastritis

PPIs are not helpful for this condition if the pH of the gastric juice is above 4-6. At such values, the drugs do not pass into the active form and are simply excreted from the body, without bringing any relief to the condition.

Stomach ulcer

For its treatment, it is extremely important to follow the rules for taking PPIs. If the regimen is systematically violated, then therapy can be delayed for a long time and the likelihood of side effects increases. The most important thing is to take the medicine 20 minutes before meals so that the correct pH is in the stomach. Some generations of PPIs do not work well in the presence of food. It is better to drink the drug at the same time in the morning in order to develop a habit of taking it.

Myocardial infarction

It would seem, what does he have to do with it? Quite often, after a heart attack, patients are prescribed an antiplatelet agent - clopidogrel. Almost all proton pump inhibitors reduce the effectiveness of this important substance by 40-50%. This is because PPIs block an enzyme that is responsible for converting clopidogrel to its active form. These drugs are often given together because the antiplatelet agent can cause stomach bleeding, so doctors try to protect the stomach from side effects.

The only proton pump blocker that is safest when combined with clopidogrel is pantoprazole.

Systemic fungal diseases

Sometimes the fungus is treated with oral itraconazole. In this case, the drug acts not in one specific place, but on the entire body as a whole. The antifungal agent is covered with a special membrane that dissolves in an acidic environment; with a decrease in pH values, the drug is less absorbed. With their joint appointment, the drugs are taken at different times of the day, while itraconazole is best taken with cola or other drinks that increase acidity.

Contraindications

Although the list is not very long, it is important to read this point of the instructions carefully. And be sure to warn the doctor about any diseases and other medications taken.

Side effects

Usually, the unwanted effects are minimal if the course of treatment is short. But the occurrence of the following phenomena is always possible, which disappear with the withdrawal of the drug or after the course of treatment completed:

abdominal pain, stool disturbance, bloating, nausea, vomiting, dry mouth;
headache, dizziness, general malaise, insomnia;
allergic reactions: itching, rash, drowsiness, swelling.

Alternative PPI drugs

There is another group of antisecretory drugs, which is also used for peptic ulcer disease and other syndromes - H2-histamine receptor blockers. Unlike PPIs, drugs block certain receptors in the stomach, while proton pump inhibitors inhibit the activity of enzymes that help produce hydrochloric acid. The exposure to H2 blockers is shorter and less effective.

The main representatives are famotidine and ranitidine. The duration of action is about 10-12 hours with a single application. They cross the placenta and pass into breast milk. They have the effect of tachyphylaxis - the body's reaction to repeated use of the drug consists in a noticeable decrease in the therapeutic effect, sometimes even 2 times. Usually observed after 1-2 days after the start of admission. In most cases, they are used when there is an acute question about the price of treatment.

It can also be attributed to alternative remedies. They reduce the acidity of the stomach, but they do it for a very short time and are used only as an emergency aid for stomach pain, heartburn, and nausea. They have an unpleasant effect - rebound syndrome. It lies in the fact that the pH rises sharply after the end of the action of the drug, the acidity rises even more, the symptoms can be exacerbated with double strength. This effect is more commonly seen after taking calcium-containing antacids. The acidic ricochet is neutralized by the ingestion of food.

Comments:

What substances belong to the family
How drugs in this group work
When are medications prescribed
To whom medications are contraindicated

Proton pump inhibitors, drugs designed to block the production of hydrochloric acid in the stomach, are often used in gastroenterology. These agents suppress the work of the proton pump in the cell membrane that produces hydrochloric acid for digestion. A new type of drug could change the situation in the treatment of gastrointestinal diseases.

Suppression of biochemical processes by active substances occurs at the level of secretory cells.

The first drug with the property of significantly reducing the production of hydrochloric acid by interfering with the work of cell membranes was Omeprazole.

It is now the most common drug for home treatment, but it has side effects that prevent it from being used for long-term therapy. Then other active substances were found that have a similar effect. In the pharmacy, you can buy new drugs with better effect and fewer side effects. For the treatment of gastritis complicated by infection, combined preparations are used, which include not only inhibitors, but also antibacterial agents.

What substances belong to the family

After Omeprazole passed all the tests and was released on the market, many people were able to get rid of stomach diseases, which were aggravated at the moment of activation of the cells responsible for the high concentration of hydrochloric acid. The effect obtained surpassed all the results that were observed with the use of other antisecretory agents. Due to the fact that in patients who have been using Omeprazole for a long time, cell resistance to this active substance began to be revealed, there was a need for drugs of a similar action, but with no side effects. In the laboratories of many of the largest pharmaceutical companies, work has begun on the creation of substances with a similar effect.

Modern pharmaceuticals offer patients 5 active substances that significantly improve the condition of a person suffering from acid-dependent diseases of the digestive system:

omeprazole;
lansoprazole;
pantoprazole;
rabeprazole;
esomeprazole.

The use of these substances does not relieve patients of the seasonal exacerbation of peptic ulcer disease if it was caused by the bacterium Helicobacter pylori, which irritates the stomach wall. Each course of treatment gives only long-term remission. For a complete recovery from ulcerative gastritis, complex treatment should be carried out, which must include a proton pump inhibitor.

All active substances belonging to one group have a long-term effect on cells, but the later they were discovered, the better their effect on the body became. The most effective is pantoprazole, which is used for hospital treatment.

Back to the table of contents

How drugs in this group work

Proton pump inhibitors are actively prescribed by gastroenterologists for the treatment of acid-dependent conditions. In 95% they help to achieve stable remission with the formation of duodenal ulcers and reflux, in which there is a reflux of the eaten food from the stomach into the esophagus.

All active substances are absorbed in the small intestine and accumulate as much as possible in the plasma within 3.5 hours after taking the capsule. They enter the tubules of parietal cells, where they begin their work to block their activity.

The bioavailability of known proton pump inhibitors is variable, but stable. Neither food intake nor antacids can change it. Omeprazole after the second dose of a single dose decreases it, esomeprazole increases it, and the other three active substances do not change this indicator from the first to the last dose. The breakdown of active substances occurs in the liver. The resulting metabolites are non-toxic and are excreted in the urine. This allows the use of drugs for a long time, if required by the state of the body.

Omeprazole acts in the body for no more than 14 hours. And this makes you take 2 capsules a day when the symptoms of increased acidity in the stomach return. With prolonged use of this active substance, the body's immunity, or resistance, is developed.

Esomeprazole is an isomer of omeprazole with great metabolic stability. It can control the production of hydrochloric acid for 24 days without causing addiction or other side effects. Having bought a drug with this active substance in a pharmacy, the patient must take 1 capsule per day, which is very convenient.

Pantoprazole, which has a pH of 5.0, is the most stable and weakest. Its high bioavailability makes it possible to use preparations with this active substance for injections in hospitalized patients during the treatment of severe gastric lesions. Pantoprazole reacts with antibacterial drugs in combination therapy, and this enhances its therapeutic effect. This active substance has shown good results in the treatment of bronchial asthma.

Back to the table of contents

When are medications prescribed

The gastroenterologist recommends proton pump inhibitors for any acid-related digestive system disease. Conditions where drugs that suppress the processes of excess production of hydrochloric acid are especially useful include:

hyperacid gastritis, in which the walls of the stomach become inflamed;
the use of hormone-containing drugs;
treatment with non-steroidal anti-inflammatory drugs;
defeat of the lower esophageal sphincter;
regular reflux of food from the stomach into the esophagus.

Proton pump blockers are used in the complex treatment of pancreatitis, gallstone disease and other diseases of the digestive system, which entail an increase in acid levels.

The drugs of this group, in combination with antibacterial active agents, accelerate the treatment of diseases of the digestive tract caused by Helicobacter pylori. Pharmacists offer complex combinations of inhibitors with metronidazole, tinidazole, amoxicillin, and clarithromycin.

Such complex formulations can be taken only after the recommendation of a doctor, which he does after a diagnosis.

The selection of the active substance is carried out after measuring the acidity in the upper parts of the patient's stomach. Treatment is adjusted if the response to the drug is ineffective. This is due to the individual characteristics of the organism and the resistance of cells to the selected active substance. The resistance of cells to a proton pump inhibitor can be caused by genetic characteristics of the organism or formed during the course of the disease. At the beginning of treatment, the doctor determines the individual intake rhythm and specifies the doses of drugs using the analysis of intragastric pH. The gastroenterologist may prescribe original preparations of lansoprazole, pantoprazole or other similar drugs, because generic inhibitors may contain less active substance, and this reduces the expected effectiveness of treatment.

(also called: proton pump inhibitors, proton pump inhibitors, proton pump blockers, H + / K + -ATPase blockers, hydrogen pump blockers, etc.) - antisecretory drugs intended for the treatment of acid-dependent diseases of the stomach, duodenum and esophagus blocking the proton pump (H + / K + -ATPase) of the parietal (parietal) cells of the gastric mucosa and thus reducing the secretion of hydrochloric acid. The most commonly used abbreviation is PPI, less often - PPI.

Proton pump inhibitors are the most effective and modern drugs in the treatment of ulcerative lesions of the stomach, duodenum (including those associated with infection with Helicobacter pylori) and esophagus, providing a decrease in acidity and, as a consequence, the aggressiveness of gastric juice.

All proton pump inhibitors are benzimidazole derivatives and have a similar chemical structure. IPP differ only in the structure of the radicals on the pyridine and benzimidazole rings. The mechanism of action of various proton pump inhibitors is the same, they differ mainly in their pharmacokinetics and pharmacodynamics.

Mechanism of action of a proton pump inhibitor

Proton pump inhibitors, after passing through the stomach, enter the small intestine, where they dissolve, after which they enter the liver through the bloodstream, and then penetrate through the membrane into the parietal cells of the gastric mucosa, where they are concentrated in the secretory tubules. Here, at acidic pH, proton pump inhibitors are activated and converted into tetracyclic

Mechanism of action of inhibitors
proton pump
(Maev I.V. and others)

sulfenamide, which is charged and therefore unable to penetrate membranes and does not leave the acidic compartment inside the secretory tubules of the parietal cell. In this form, proton pump inhibitors form strong covalent bonds with mercapto groups of cysteine residues of H + / K + -ATPase, which blocks conformational transitions of the proton pump, and it becomes irreversibly excluded from the secretion of hydrochloric acid. For acid production to resume, the synthesis of new H + / K + -ATPases is necessary. Half of human H + / K + -ATPases are renewed in 30-48 hours, and this process determines the duration of the therapeutic effect of PPIs. With the first or a single dose of PPI, its effect is not maximal, since not all proton pumps by this time are built into the secretory membrane, some of them are in the cytosol. When these molecules, as well as newly synthesized H + / K + -ATPases, appear on the membrane, they interact with subsequent doses of PPIs, and its antisecretory effect is fully realized (Lapina T.L., Vasiliev Yu.V.).

Types of proton pump inhibitors

The Anatomical Therapeutic Chemical Classification (ATC) in section A02B Antiulcer and gastroesophageal reflux drugs contains two groups with proton pump inhibitors. The group A02BC "Proton pump inhibitors" lists the international non-proprietary names (INN) of seven PPIs (the first six types of them are approved for use in the United States and the Russian Federation, the seventh, dexrabeprazole, has no approval for use):

Esomeprazole, dexlansoprazole and dexarabeprazole are optical isomers of omeprazole, lansoprazole and rabeprazole, respectively, with greater biological activity. Also included in this group are combinations:

A02BC53 Lansoprazole in combination with other drugs
A02BC54 Rabeprazole in combination with other drugs

In group A02BD "Combinations of drugs for eradication Helicobacter pylori»Lists proton pump inhibitors in combination with various antibiotics for treatment Helicobacter pylori-associated diseases of the digestive tract:

A02BD01 Omeprazole, amoxicillin and metronidazole
A02BD02 Lansoprazole, tetracycline and metronidazole
A02BD03 Lansoprazole, amoxicillin and metronidazole
A02BD04 Pantoprazole in combination with amoxicillin and clarithromycin
A02BD05 Omeprazole, amoxicillin and clarithromycin
A02BD06 Esomeprazole, amoxicillin and clarithromycin
A02BD07 Lansoprazole, amoxicillin and clarithromycin
A02BD09 Lansoprazole, clarithromycin and tinidazole
A02BD10 Lansoprazole, amoxicillin and levofloxacin

There are a number of new proton pump inhibitors in various stages of development and clinical trials. The best known of these and close to completion of trials is tenatoprazole. However, some clinicians believe that it does not have clear pharmacodynamic advantages over its predecessors and that the differences relate only to the pharmacokinetics of the active substance (Zakharova N.V.). Among the advantages of ilaprazole is that it is less dependent on the polymorphism of the CYP2C19 gene and that its half-life (T 1/2) is 3.6 hours (Mayev I.V. et al.)

In January 2009, the US Food and Drug Administration (FDA) approved the sixth proton pump inhibitor dexlansoprazole, which is an optical isomer of lansoprazole, for the treatment of GERD; in May 2014, it received permission in Russia.

In the Pharmacological Index in the section Gastrointestinal drugs there is a group "Proton pump inhibitors".

By order of the Government of the Russian Federation of December 30, 2009 No. 2135-r, one of the proton pump inhibitors - omeprazole (capsules; lyophilisate for preparing a solution for intravenous administration; lyophilisate for preparing a solution for infusion; coated tablets) is included in the List of vital and essential medicines.

Currently, 5 standard doses of proton pump inhibitors are licensed in Europe for the treatment of GERD (esomeprazole 40 mg, lansoprazole 30 mg, omeprazole 20 mg, rabeprazole 20 mg,
pantoprazole 40 mg) and one double (omeprazole 40 mg). Standard doses of proton pump inhibitors are licensed for the treatment of erosive esophagitis for 4-8 weeks, and the double dose is for the treatment of refractory patients who have previously been treated with standard doses prescribed for up to 8 weeks. Standard doses are prescribed once a day, a double dose - twice a day (V.D. Pasechnikov and others).

Over-the-counter proton pump inhibitors

In the first decades after their appearance, antisecretory drugs in general and proton pump inhibitors in the United States, Russia, and many other countries were prescription drugs. In 1995, the FDA authorized the Over-the-Coutne (R) sale of the H2 blocker Zantac 75, and in 2003, the first non-prescription PPI Prilosec OTC (omeprazole magnesium). Later, OTC PPIs were registered in the US: Omeprazole (omeprazole), Prevacid 24HR (lansoprazole),

Nexium 24HR (esomeprazole magnesium), Zegerid OTC (omeprazole + sodium bicarbonate). All OTC forms are characterized by a reduced content of active ingredient and are intended "for the treatment of frequent heartburn."

Pantoprazole 20 mg is approved for OTC dispensing in the European Union (EU) on 12.6.2009, in Australia - in 2008. Esomeprazole 20 mg - in the EU on 26.8.2013 Lansoprazole - in Sweden since 2004, later allowed in a number other EU countries, Australia and New Zealand. Omeprazole has been in Sweden since 1999, later in Australia and New Zealand, other EU countries, Canada, and a number of Latin American countries. Rabeprazole has been in Australia since 2010, later in the UK (Boardman HF, Heeley G. The role of the pharmacist in the selection and use of over-the-counter proton-pump inhibitors. Int J Clin Pharm (2015) 37: 709-716. DOI 10.1007 / s11096-015-0150-z).

In Russia, over-the-counter sales are allowed, in particular, the following dosage forms of PPIs
:

Gastrozole, Omez, Ortanol, Omeprazole-Teva, Ultop, capsules containing 10 mg of omeprazole
Bereta, Noflux, Pariet, Rabiet, capsules containing 10 mg rabeprazole sodium (or rabeprazole)
Controloc capsules containing 20 mg pantoprazole

The general rule of thumb when taking an over-the-counter PPI is that if there is no effect within the first three days, consult a specialist. The maximum duration of treatment with an OTC PPI without consulting a doctor is 14 days (for Controloc - 4 weeks). The interval between 14-day courses must be at least 4 months.

Proton pump inhibitors in the treatment of gastrointestinal diseases

Proton pump inhibitors are the most effective drugs that suppress hydrochloric acid production, although they have some disadvantages. As such, they have found wide application in the treatment of acid-dependent diseases of the gastrointestinal tract, including, if necessary, the eradication of Helicobacter pylori.

Diseases and conditions in the treatment of which the use of proton pump inhibitors is indicated (Lapina T.L.):

gastroesophageal reflux disease (GERD)
stomach and / or duodenal ulcer
Zollinger-Ellison syndrome
damage to the gastric mucosa caused by taking non-steroidal anti-inflammatory drugs (NSAIDs)
diseases and conditions in which the eradication of Helicobacter pylori is indicated.

Numerous studies have shown a direct relationship between the duration of maintaining gastric acidity with a pH> 4.0 and the speed of healing of ulcers and erosions in the esophagus, gastric and duodenal ulcers, the frequency of Helicobacter pylori eradication, and a decrease in symptoms characteristic of extraesophageal manifestations of gastroesophageal reflux. The lower the acidity of the stomach contents (i.e. the higher the pH value), the sooner the treatment effect is achieved. In general, we can say that for most acid-related diseases, it is important that the pH level in the stomach is more than 4.0 for at least 16 hours a day. More detailed studies have established that each of the acid-dependent diseases has its own critical level of acidity, which must be maintained for at least 16 hours a day (Isakov V.A.):

Acid-related diseases	The level of acidity required to heal, pH, not less
Gastrointestinal bleeding	6
GERD complicated by extraesophageal manifestations	6
Quad or triple therapy with antibiotics	5
Erosive GERD	4
Damage to the gastric mucosa caused by taking non-steroidal anti-inflammatory drugs	4
Functional dyspepsia	3
Maintenance therapy for GERD	3

In the pathogenesis of gastric and / or duodenal ulcers, the decisive link is the imbalance between the factors of aggression and the factors of protection of the mucous membrane. Currently, among the factors of aggression, in addition to the hypersecretion of hydrochloric acid, there are: hyperproduction of pepsin, Helicobacter piylori, impaired gastroduodenal motility, the effect on the mucous membrane of the stomach and duodenum of bile acids and lysolicetin, pancreatic enzymes in the presence of duodenogastric membrane, and reflux smoking, drinking alcoholic beverages, taking certain medications such as nonsteroidal anti-inflammatory drugs.

Protection factors include: secretion of gastric mucus, production of bicarbonates, which help to neutralize intragastric acidity at the surface of the gastric mucosa up to 7 units. pH, the ability of the latter to regenerate, the synthesis of prostaglandins, which have a protective effect and are involved in ensuring adequate blood flow in the mucous membrane of the stomach and duodenum. It is important that many of these factors of aggression and defense are genetically determined, and the balance between them is maintained by the coordinated interaction of the neuroendocrine system, including the cerebral cortex, hypothalamus, peripheral endocrine glands, and gastrointestinal hormones and polypeptides. The most important role of hyperacidity in the genesis of peptic ulcer disease is confirmed by the high clinical efficacy of antisecretory drugs that are widely used in modern therapy of peptic ulcer disease, among which proton pump inhibitors play a leading role (Mayev I.V.).

Proton pump inhibitors in eradication regimens Helicobacter pylori

Eradication Helicobacter pylori does not always reach the goal. The very widespread and inappropriate use of common antibacterial agents has led to increased resistance to them. Helicobacter pylori.

It is recognized that in different countries of the world (different regions), it is advisable to use different schemes. In the vast majority of regimens, one of the proton pump inhibitors is necessarily present in the so-called standard dosage (omeprazole 20 mg, lansoprazole 30 mg, pantoprazole 40 mg, esomeprazole 20 mg, rabeprazole 20 mg 2 times a day). The presence of a proton pump inhibitor in the scheme significantly increases the effectiveness of antibiotics and dramatically increases the percentage of successful eradication. An exception when proton pump inhibitors are not used is atrophy of the gastric mucosa with achlorhydria, confirmed by pH metry. The choice of one or another proton pump inhibitor affects the likelihood of eradication, however, replacing other drugs (antibiotics, cytoprotectors) has a much greater effect than PPIs. Specific recommendations for the eradication of Helicobacter pylori are given in the Standards for the diagnosis and treatment of acid-dependent and Helicobacter pylori-associated diseases adopted by the Scientific Society of Gastroenterologists of Russia in 2010.

Proton pump inhibitors increase the risk of fractures, possibly cause Clostridium difficile-associated diarrhea and may cause hypomagnesemia and dementia in old age, and probably increase the risk of pneumonia in the elderly

The United States Food and Drug Administration (FDA) has issued a number of reports of possible dangers with prolonged or high doses of proton pump inhibitors:

In May 2010, the FDA issued a warning about the increased risk of fractures of the hip, wrist and spine with prolonged use or high doses of proton pump inhibitors ("FDA warns")
In February 2012, the FDA issued a notice warning patients and clinicians that proton pump inhibitor therapy may increase the risk of Clostridium difficile-associated diarrhea (FDA Communication of 8.2.2012).

Based on this and similar information, the FDA believes: When prescribing proton pump inhibitors, physicians should choose the lowest possible dose or shorter course of treatment that is appropriate for the patient's condition.

Several cases of life-threatening hypomagnesemia (lack of magnesium in the blood) associated with the use of proton pump inhibitors have been described (Yang Y.-X., Metz D.C.). Proton pump inhibitors, when taken in conjunction with diuretics in elderly patients, slightly increase the risk of hospitalizations for hypomagnesemia. However, this fact should not affect the reasonable prescription of proton pump inhibitors, and the low risk does not require screening for magnesium levels in the blood (Zipursky J el al. Proton Pump Inhibitors and Hospitalization with Hypomagnesemia: A Population-Based Case-Control Study / PLOS Medicine - Sep 30, 2014).

According to studies conducted in Germany (German Center for Neurodegenerative Diseases, Bonn), long-term use of proton pump inhibitors increases the risk of dementia in old age by 44% (Gomm W. et al. Association of Proton Pump Inhibitors With Risk of Dementia. A Pharmacoepidemiological Claims Data Analysis. JAMA Neurol. Published online February 15, 2016. doi: 10.1001 / jamaneurol.2015.4791).

Scientists from the UK have found that older people who received PPIs within a two-year period have a higher risk of pneumonia. The logic of the authors of the study is as follows: the acid in the stomach creates a barrier for the intestinal microbiota, which is pathogenic for the lungs. Therefore, if acid production decreases due to PPI intake, then due to high refluxes, more pathogens can enter the respiratory tract (J. Zirk-Sadowski, et al. Proton-Pump Inhibitors and Long-Term Risk of Community-Acquired Pneumonia in Older Adults. Journal of the American Geriatrics Society, 2018; DOI: 10.1111 / jgs.15385).

Taking proton pump inhibitors during pregnancy

Different proton pump inhibitors have different FDA risk categories for the fetus:

Taking proton pump inhibitors for gastroesophageal reflux disease during the first trimester of pregnancy more than doubles the risk of having a baby with heart defects (GI & Hepatology News, August 2010).

There are also studies proving that taking proton pump inhibitors during pregnancy increases the risk of asthma in an unborn child by 1.34 times (taking H2 blockers by 1.45 times). Source: Lai T., et al. Acid-Suppressive Drug Use During Pregnancy and the Risk of Childhood Asthma: A Meta-analysis. Pediatrics. Jan 2018.

Selection of proton pump inhibitors

The acid-suppressing effect of proton pump inhibitors is strictly individual for each patient. A number of patients have such phenomena as "resistance to proton pump inhibitors", "nocturnal acid breakthrough", etc. This is due to both genetic factors and the state of the body. Therefore, in the treatment of acid-dependent diseases, the appointment of proton pump inhibitors should be individually and timely adjusted taking into account the response to the treatment. It is advisable to determine the individual intake rhythm and doses of drugs for each patient under the control of intragastric pH-metry (Bredikhina N.A., Kovanova L.A.; Belmer S.V.).

Daily pH-gram of the stomach after taking PPIs

Comparison of proton pump inhibitors

It is generally accepted that proton pump inhibitors are the most effective treatments for acid-related diseases. The class of antisecretory drugs that appeared before PPIs - H2-blockers of histamine receptors are gradually being ousted from clinical practice and PPIs compete only with each other. There are different points of view among gastroenterologists regarding the comparative effectiveness of specific types of proton pump inhibitors. Some of them argue that, despite some differences that exist between PPIs, to date there are no convincing data that allow us to talk about the greater effectiveness of any PPI compared to others (Vasiliev Yu.V. et al.) Or that during eradication Нр type of PPI included in the composition of triple (quadruple therapy) does not matter (Nikonov E.K., Alekseenko S.A.). Others write that, for example, esomeprazole is fundamentally different from the other four PPIs: omeprazole, pantoprazole, lansoprazole and rabeprazole (Lapina T.L., Demyanenko D. and others). Still others believe that rabeprazole is the most effective (Ivashkin V.T. and others, Maev I.V. and others).

A group of scientists from Germany (Kirchheiner J. et al.) Performed a dose-response meta-analysis for the mean 24-hour intragastric pH and the percentage of time with a pH> 4 in 24 hours for various PPIs. They obtained the following values of the effectiveness of various PPIs to achieve an average value of intragastric pH = 4:
The cost of generics of omeprazole, pantoprazole and lansoprazole is much lower than the original preparations of esomeprazole and rabeprazole, which is of no small importance for the patient and often determines the choice of a drug based on financial capabilities, especially for long-term use (Alekseenko S.A.).

Trade names of drugs - proton pump inhibitors

A wide range of various drugs from the group of proton pump inhibitors is presented on the domestic pharmaceutical market:

active substance omeprazole: Bioprazole, Vero-omeprazole, Gastrozole, Demeprazole, Zhelkizol, Zerocid, Zolser, Crismel, Lomak, Losec, Losec MAPS, Omegast, Omez, Omezol, Omecaps, Omeparme, Omeprazole, Omeprazole, Omeprazole-AKO Omeprazol acri, Omeprazole-EK, Omeprazole-OBL, Omeprazole-Teva, Omeprazole-Richter, Omeprazole-FPO, Omeprazole Sandoz, Omeprazole Stada, Omeprol, Omeprus, Omefez, Pmizak, Omipixol, Omitiksid, Ormisak -20, Promez, Risek, Romesek, Sopral, Ulzol, Ultop, Helicide, Helol, Tsisagast
the active substance is omeprazole, in addition to which the medicine contains a noticeable amount of sodium bicarbonate: Omez insta
active substance omeprazole + domperidone: Omez-d
active ingredient pantoprazole: Zipantol, Controloc, Krosacid, Nolpaza, Panum, Peptazol, Pizhenum-Sanovel, Pulloref, Sanpraz, Ultera
active substance lansoprazole: Acrylanz, Helikol, Lanzabel, Lanzap, Lanzoptol, Lansoprazole, Lansoprazole pellets, Lansoprazole Stada, Lansofed, Lancid, Loenzar-Sanovel, Epicur
active substance rabeprazole: Bereta, Zolispan, Zulbex, Noflux (formerly called Zolispan), Ontaym, Noflux, Pariet, Rabelok, Rabeprazole-OBL, Rabeprazol-SZ, Rabiet, Razo, Khairabezol
active substance

Especially common:

Gastritis occurs in 80 percent of the population, and gastric dyspepsia covers a percentage. It is quite understandable that with such disappointing statistics, the problem of curing gastrointestinal pathologies is especially pressing.

What is a proton pump?

Proton pump inhibitors inhibit stomach acid production

Pump is a technical term for a type of pump. And it's a little strange to see this name in the anatomy of the human body. Nevertheless, the term proton pump, applied to hydrogen-potassium adenosine triphosphatase, can explain the function of this enzyme protein, which carries out the movement of positive electrons through the intercellular septum.

A proton pump is also called a proton pump. It is a complex polypeptide chain consisting of amino acid residues and containing positive ions of hydrogen and potassium in its structure. H + / K + -ATPase was isolated forty years ago as an enzymatic protein hydrolase, and at the same time it was named the proton pump. She takes part in the production of hydrochloric acid and an enzyme that converts vitamin B12 from a passive form to an active one.

Hydrogen-potassium adenosine triphosphatase is contained in the parietal cells of the gastric mucosa. They also form hydrochloric acid. It transfers positively charged hydrogen protons (H +) from the cytoplasm of the parietal (parietal) cell into the gastric cavity through the superior intercellular septum. In this case, the potassium ion (K +) moves into the cell. At the same time, chlorine anions (CL-) are transported to the stomach area.

The H + protons are released as a result of the decomposition of carbonic acid (H2CO3) under the action of the enzyme carbonic anhydrase. The remaining cations (НСО3-) are transferred into the blood instead of chlorine cations, which, having moved to the stomach, and combining there with hydrogen, form hydrochloric acid molecules. Thus, hydrochloric acid is released into the lumen of the stomach with the participation of H + / K + -ATPase in the form of H + and Clв € 'ions, and K + ions move through the membrane in a return manner.

What are proton pump inhibitors and what are they for?

Inhibition means containment. In this case, the containment of HCl synthesis. The task of proton pump inhibitors is to suppress the production of hydrochloric acid in the stomach, which is achieved by blocking the transport of potassium and hydrogen ions from the cell. Inhibition was found to be effective in the treatment of acid-dependent gastrointestinal diseases such as

Proton pump inhibitors block the production of hydrochloric acid to varying degrees. Addictiveness to these drugs does not develop, side effects are not noted. Therefore, this category of drugs was adopted by the World Congress of Gastroenterology in 1988 in Rome, as the main group of acid-regulating drugs.

Each subsequent development of PPI differs from its previous one in higher activity and duration of action. But the actual efficiency is influenced by certain factors, the first of which is the individual susceptibility of the organism.

PPI mechanism of action

Proton pump drugs are taken orally, in the form of tablets or capsules. From the stomach, the drug enters the small intestine, here it dissolves and is absorbed into the blood, which first transfers the inhibitor molecules to the liver, and only then they enter the parietal cells of the gastric mucosa, where they accumulate in the secretory tubules.

PPIs are converted to tetracyclic sulfenamide, which does not go beyond the secretory tubules, bind by ionic residues of the pump and block it. Thus, the H + / K + -ATPase is excluded from the formation of hydrochloric acid. For this process to resume, the production of a new enzyme H + / K + -ATPase is needed, which occurs in 1.5-2 days. This time determines the duration of the therapeutic effect of the proton pump inhibitors.

With the first or one-time use of the drug, its efficacy is not so significant, since not all proton pumps have been introduced into the secretory membrane at this point, some of them are inside the cell. These microparticles, together with the newly synthesized hydrogen-potassium adenosine triphosphatases, appear on the membrane, they interact with subsequent doses of the drug, and its antisecretory effect is completely fulfilled.

Antisecretory therapy allows you to stop diseases dependent on the concentration of hydrochloric acid. Thus, the duodenal ulcer heals with a maintained pH above 3 for 18–20 hours a day; for the treatment of GERD, a pH of more than 4 is required, the Helicobacter pylori bacterium is destroyed in a weakly acidic environment at a pH of more than 5.

What is pH?

Proton pump inhibitors

Here, let me make a small digression, in which you will find an explanation of the pH value (pe-ash). It is needed to further explain the acidic state of the gastrointestinal tract and how PPI drugs work.

The scale of the hydrogen number pH, which determines the acid-base nature of liquid substances and solutions, can be compared with the mathematical line on which positive and negative numbers are located.

The pH is 14 units. Chemically neutral substance water (comparable to zero on a mathematical scale) is equal to pH7. Substances with a pH of less than 7 are acidic. Those above the number 7 are alkaline. Accordingly, the lower the pH, the higher the acidity of the substance or solution, and vice versa, the higher the pH, the lower the acidity, but the level of the alkaline medium rises.

Characterization of proton pump inhibitors

PPIs are recognized as particularly effective drugs in the treatment of peptic ulcer diseases associated with high acidity, and occupy a leading place among medicinal antiulcer drugs. In this case, the anti-secretory result is achieved by directly influencing the formation of hydrochloric acid.

This category of drugs is superior to all other antisecretory drugs in terms of the effectiveness and harmlessness of exposure. The PPI includes 5 generations of drugs, the first of which, omeprazole, was developed in 1989.

Omeprazole

Today it is one of the most widespread and used drugs. Its effectiveness is confirmed by the results of studies in which patients with various gastrointestinal tract pathologies participated. In comparison of omeprazole with H2-blockers, there is an advantage of a proton pump inhibitor in the effectiveness of suppressing inflammatory processes, and at the same time, the ulcerative abscess of the mucous membrane was clearly delayed.

Even in patients with gastrinoma (a malignant tumor that produces the hormone gastrin, which stimulates the production of HCl), positive dynamics were observed. In addition, Omeprazole enhanced the anti-Helicobacter effect of the antibiotics taken. Bioavailability, that is, the amount of a drug reaching the zone of its effect in the body, fluctuates within 50%, 95 percent of which binds to plasma proteins.

The highest content of this medication in the blood is concentrated an hour after ingestion and lasts up to 3 hours. The standard therapeutic regimen involves taking the drug 2 times a day, 20 mg per dose. Within a month, ulcerative wounds of the duodenum are healed by 97%, and stomach ulcers by 80%.

Lansoprazole

This drug has the highest bioavailability in the group of drugs that inhibit the production of hydrochloric acid, amounting to 80-90%. Lansoprazole differs from its predecessor in the construction of radicals that provide an anti-secretory effect.

Studies have shown that on the 5th day of consumption, Lansoprazole provides a pH in the stomach above 4, for 11.5 hours (for comparison, pantoprazole kept the same acidity for 10 hours). Lansoprazole is recommended to be taken at 15, 30 and 60 mg per day (depending on the severity of the pathology). In 95% of cases, the ulcer heals within 4 weeks.

Pantoprazole

Pantoprazole is attractive because it allows long-term use in order to consolidate the therapeutic effect in the treatment of peptic ulcer disease. Despite the variability of the result (the acid-base level ranged from 2.3 to 4.3), the methods of administration of the agent do not significantly affect its pharmacokinetics.

In other words, Pantoprazole is administered both intravenously and orally. A ten-year observation of patients taking pantoprazole treatment showed that relapses did not occur after using this drug.

Rabeprazole

Rabeprazole also has distinctive features on the pyridine and imidazole rings from omeprazole, which provide a more efficient binding of potassium and hydrogen protons of adenosine triphosphate MЃse. Rabeprazole is absorbed by the body and a therapeutic effect of 51.8% is achieved, it binds to blood proteins by 96.3%. With the daily use of this drug at 40 mg per day for a month, the ulcer heals by 91%.

Esomeprazole

There is only one S-isomer in the structural formula of Esomeprazole, and therefore the drug is not as susceptible to hydroxylation by the liver as its precursors with R-isomers, and is not eliminated so quickly from the body. These factors increase the number of inhibitors reaching proton pumps in parietal cells. Esomeprazole, taken at 40 mg per day, maintains a pH value of more than 4 for 14 hours. This is the highest therapeutic effect that has been achieved to date.

Helicobacter pylori and PPI

There are 5 generations of proton pump inhibitors in total

Speaking about acid-related diseases and the causes that give rise to them, one cannot but recall the gram-negative helix-like bacterium Helicobacter pylori, since scientists have come to the conclusion that this bacterium is a kind of catalyst, a trigger for the occurrence of these diseases.

And it is this bacterium that settles in the stomach that provokes inflammatory relapses of the gastrointestinal tract. Therefore, the therapy of acid-dependent pathologies is carried out in combination with antibiotics of the tetracycline group, and in particular, with Metronidazole.

Conclusion. API work continues

Five generations of proton pump inhibitors have been widely approved and used successfully. Six years ago, a new drug, Dexlansoprazole, was released on the market, approved for use in the treatment of GERD.

A new PPI is currently being developed and tested in Japan. This is Tenatoprazole. It is a derivative of imidazopyridine. True, some experts believe that this drug as a whole repeats previous generations.

A little earlier, Ilaprazole was developed in Korea, which is 2-3 times more effective than Omeprazole. But in the USA, EU countries and in Russia there is no permission for its use. Now Japan is trying to promote this drug to the Western market.

On the safety of proton pump inhibitors - in a video lecture:

Tell your friends! Share this article with your friends on your favorite social network using the social buttons. Thanks!

List of drugs - proton pump inhibitors - with a description

Proton pump inhibitors (PPIs) are available in the modern pharmaceutical market as capsules or tablets. These medications should only be used as directed by your healthcare professional. You will learn more about medicines from our article.

Pathologies of the gastric mucosa, which have arisen due to disturbances in the acidity of gastric juice, are treated with proton pump inhibitors. Drugs of this group are prescribed for various diseases of the stomach (ulcer, gastritis, gastroduodenitis, reflux esophagitis, erosion of the esophagus, etc.), their action is aimed at reducing the production of gastric juice.

In addition, proton pump inhibitors are necessarily used in complex therapy with antibacterial drugs for the eradication of the Helicobacter Pylori bacteria, as well as in the case of systematic administration of drugs that negatively affect the functioning of the stomach and intestines.

How drugs work

The drug is taken orally with plenty of water. The active substance of the drug enters the intestines, after which it is absorbed into the blood. Further, the active substance of the drug penetrates into the gastric mucosa.

It should be noted that in the first days after the start of taking proton pump inhibitors, the patient does not notice any positive changes. First of all, this is due to the fact that these tablets have a cumulative effect, that is, they begin to work in full force after a sufficient amount of active substance has accumulated in the secretion of gastric juice.

These medications are used in complex treatment with probiotics, enzyme and antacid preparations, sometimes with antibiotics.

Indications for use

The gastroenterologist prescribes proton inhibitors in the event that the pathology of the stomach is caused by a change in the level of acidity of the gastric juice. This feature is usually found in the following diseases of the gastrointestinal tract:

chronic heartburn;
gastritis of various etiologies;
gastroduodenitis;
the presence of a stomach or duodenal ulcer.

Despite the fact that proton pump inhibitors very rarely cause side effects, have a minimal list of contraindications, it is recommended to use this drug only as directed by a doctor.

Contraindications for admission

Proton pump inhibitors have a standard list of contraindications:

The official annotation to the PPI states that the use of funds is categorically not recommended for women who are carrying a child, as well as when breastfeeding.
You cannot treat the stomach with these drugs for children under 12 years of age.
Also in the list of contraindications there is a line that says about the individual intolerance of the active substance. In this case, the doctor changes the pills to similar ones.

Possible side effects

Each group of blockers has individual side effects. It should be noted that they are quite rare. Let's consider the main ones:

nausea;
loss of appetite;
headache;
constipation or diarrhea;
vomit;
pain in the stomach;
an allergic reaction in the form of a skin rash.

Effective PPIs

Proton pump inhibitors can be roughly divided into five groups. Their difference is the active substance and its amount. Depending on the active ingredient, the dosage regimen, course of treatment or dosage of the drug may vary. All existing types of inhibitors are aimed at reducing the production of gastric juice. Consider a list of the most effective drugs.

Lansoprazole based preparations

The difference between this group is high absorption. Such funds include: Lanzap, Gelikol, Lansoprol, Lanzoptol, Lanpro, Lancet, Lansodin and others.

Let us dwell in more detail on the most popular medicines based on lansoprazole:

Akrilans. The drug is available in capsule form. The package contains 30 mg. active substance. One blister contains 10 tablets. The manufacturer produces the drug in packs of 10, 20 or 30 capsules. According to the official annotation, the drug is recommended to be drunk once a day. Depending on the severity of the disease, the regimen and course of treatment can be adjusted by the attending physician.
Lancid. An agent for the treatment of acid-dependent diseases of the gastrointestinal tract, produced in capsules. One capsule contains 15 mg. active component. The dosage of the drug is designed for a single dose. For serious illnesses, the doctor may increase the dosage.
Epicurus. Each capsule of this proton pump inhibitor contains 30 mg. active substance. One package contains 10 capsules. The method of administration and dose is no different from the above-mentioned analogs.

Medicines based on omeprazole

To date, the most popular remedy that is prescribed for increased secretion of gastric juice, as well as in the presence of stomach ulcers. Many studies have proven the effectiveness of this medication. Medicines with this active ingredient have the advantage of low cost.

There are such tablets with the active ingredient "omeprazole": Gastrozole, Demeprazole, Ultop, Ortanol, Helicide, etc.

Let's take a look at some of the names for these proton pump inhibitors:

Omez. The new generation capsules contain slightly more active ingredient than lansoprazole-based preparations. One capsule contains 40 mg. active component. Apply once a day. This dosage is quite enough to suppress acid production during the day and night. The course of treatment is determined by the attending physician.
Bioprazole. One capsule contains 20 mg. active substance. A proton pump inhibitor effectively reduces acid production. You only need to drink one capsule per day.
Omezol. A proton pump inhibitor helps to inhibit the production of hydrochloric acid. One tablet contains 40 mg. active component. Take one capsule daily. In some cases, the doctor recommends taking the drug twice.
Losek. One capsule contains 30 mg. active substance.

Medicines based on pantoprazole

The proton group has some peculiarity - they gently affect the gastric mucosa. For this reason, the course of treatment can be long in order to avoid possible relapses.

This group includes: Aspan, Proxium, Sanpraz, Panum, Puloref, Ultera, Pantaz, etc.

Let us dwell in more detail on some medicines based on pantoprazole:

Controlok. The inhibitor is available in tablet form. One capsule may contain 20 or 40 mg. active component. The method of administration and dosage may differ depending on the diagnosis.
Nolpaza. Available in dosages of 20 and 40 mg. The peculiarity of this drug is that its use is prohibited until the age of 18. It is consumed once a day, preferably in the morning.
Ulter. The proton pump inhibitor is analogous to Nolpaza. The dosage and route of administration are identical.

Rabeprazole based drugs

The funds of this group effectively cope with the task.

Among the medicines based on rabeprazole, there are: Zolispan, Ontime, Pariet, etc.

Let's describe in detail the action of some drugs based on rabeprazole:

Beret. A proton pump inhibitor contains 20 or 40 mg. active component. The medicine is prescribed once or twice a day, depending on the purpose of therapy.
Zulbex. It is produced in the form of tablets, it contains 20 mg. active substance. The drug is often prescribed to treat ulcers. For effective treatment, a single dose of the drug is sufficient, preferably in the morning.
Rabelok. Often prescribed as a prophylaxis for the development of gastric ulcer or duodenal ulcer. Contains only 15 mg. active component.

Esomeprazole medicines

A feature of this group is that the active components of the funds remain in the human body for a long time. For this reason, doctors usually prescribe the minimum dosage once a day.

The funds of this group include: Neo-Zext, Esomeprazole Canon, etc.

The most popular esomeprazole medicines are as follows:

Nexium. The main indication for treatment is gastroesophageal reflux disease. Available in a dosage of 20 mg. The disadvantage of this tool is the rather high price. One package costs about 1,500 rubles.
Emaner. Prescribed twice a day. Contains 20 mg. active substance. Based on consumer reviews, we can conclude that the tool has good effectiveness, but rather high cost.

Today, doctors and patients give preference to drugs based on lansoprazole and pantoprazole. This group very rarely causes side effects and is suitable for almost everyone. In addition, the course of treatment with capsules based on these active ingredients is much shorter. Remember that any proton pump inhibitor should only be prescribed by your healthcare professional after a diagnostic test.

New generation drugs from the group of proton pump inhibitors (blockers)

Treating gastrointestinal problems is fundamental to therapy. More than half of the population suffers from diseases associated with a violation of the acid-forming function of the stomach. They interfere with performance and cause discomfort, but there are medications to relieve conditions that can help manage symptoms and improve quality of life. One of these groups of drugs are proton pump blockers.

A proton pump, a hydrogen pump or hydrogen-potassium adenosine triphosphatase (H / K-ATPase) is an enzyme that secretes hydrochloric acid in the stomach, which consists of a complex polypeptide chain, which includes amino acid residues. It is present in large quantities in the parietal cells of the mucous membrane of the organ.

Thanks to the proton pump, the hydrogen ion (H +), released in the decomposition reaction of carbonic acid, is transported from the cytoplasm to the stomach cavity, and instead of it, the potassium ion (K +) enters the cell. The exchange requires the expenditure of energy, the source of which is the hydrolyzed ATP molecule. With the help of a concentration gradient, chlorine ions (Cl-) leave the parietal cell, binding in the lumen of the gastric tubules with hydrogen ions, resulting in the formation of hydrochloric acid (HCL). It is essential for the digestion of food and the destruction of germs. With hyperfunction of parietal cells, increased acid production occurs, this condition is called hyperchlorhydria. It causes stomach irritation and discomfort.

An inhibitor is the name of a substance that is supposed to inhibit enzymatic processes. These drugs include hydrogen pump blockers, designed to treat diseases of the gastrointestinal tract, accompanied by increased acid production.

Their mechanism of action is based on inhibition of the enzyme H + -K + -ATPase ("proton pump"). The drug is taken orally in the form of tablets or capsules, absorbed through the mucous membrane of the small intestine, passes through the liver with blood flow and accumulates in the secretory tubules of the stomach, where it blocks the final stage of hydrochloric acid production. Thus, the level of stimulated and basal secretions decreases, the symptoms of heartburn, discomfort in the epigastric region, and bitterness in the mouth decrease.

Indications for taking proton pump inhibitors (PPIs):

stomach and duodenal ulcer;
erosive gastritis;
NSAID gastropathy (the appearance of ulcers due to prolonged use of non-steroidal anti-inflammatory drugs - Ketorol, Diclofenac);
Zollinger-Ellison syndrome (a malignant tumor called gastrinoma that causes an increased secretion of hydrochloric acid);
ulcers caused by severe stress;
reflux esophagitis (GERD, a disease in which the contents of the stomach are thrown into the esophagus, thereby eroding the mucous membrane);
erosion and ulcers associated with the helicobacter pylori bacterium (treatment in combination with other drugs).

high sensitivity to the drug;
children up to 13 years old (during this period, the growth and formation of body systems occurs, taking medications can provoke a malfunction);
current pregnancy (1st trimester, then - with the consent of the attending physician), lactation period (studies have not been carried out, therefore there is no evidence base).

A proton pump (proton pump) is a protein that has an enzymatic structure and exchanges positively charged hydrogen ions for positive potassium ions, regardless of the activity and stimulation of receptors located on the basement membrane layer of secretory cells. Medicines that block the activity of this protein inhibit the secretory function and are used for combination therapy of conditions, the symptoms and manifestations of which depend on the acidity of the gastric environment. They reduce the secretion of hydrochloric acid in the lumen of the gastrointestinal tract by inhibiting the proton pump in the cells of the epithelial membrane of the stomach.

Proton pump blockers: drugs

Medicines of this group began to be used in gastroenterological practice not so long ago. For the first time, a drug capable of suppressing the activity of H + / K + -ATPase was obtained experimentally in 1974. A year later, the drug was released into industrial circulation and began to be used in practice, and experts recognized PPIs as the main group of acid-controlling drugs. Massive proton pump blockers began to be used since 1988, and research carried out over the next five years made it possible to abandon surgical therapy as the main method of treating peptic ulcer disease.

Omeprazole - historically the first proton pump inhibitor

Indications for use

All drugs belonging to the group of proton (proton) pump inhibitors have the same indications for administration. In most cases, these drugs are included in combined regimens for the treatment of gastritis - an infectious or traumatic inflammation of the gastric mucosa with possible involvement of the submucosa in the process. Gastritis occurs in about every fourth inhabitant of large settlements, therefore, the use of PPIs in gastroenterology can be considered massive in this category of patients.

PPI mechanism of action

Some proton pump blockers can be used to eradicate the bacteria Helicobacter pylori, the main causative agent of infectious inflammation in the stomach, resistant to acidic environments and most antibacterial drugs. The protocol for the treatment of infectious gastritis includes three lines, in each of which proton pump inhibitors are used in combination with other drugs (bismuth drugs, antibiotics) strictly according to a specific scheme.

Insidious bacteria Helicobacter pylori

Other indications for PPI prescription are:

duodenitis (a type of enteritis characterized by damage to the duodenum);
increased secretion of gastrin, which develops against the background of the growth of tumor formation in the pancreas (ulcerogenic adenoma of the pancreas);
ulceration of the gastric mucosa or the initial sections of the small intestine;
gastroesophageal reflux disease (recurrent pathology that occurs against the background of weakening of the muscles of the esophageal sphincter and manifests itself by the regular reflux of gastric contents into the esophagus);
chronic pancreatitis;
dyspeptic disorders (as symptomatic treatment).

PPIs can be used to treat conditions of the esophageal tube, accompanied by the formation of columnar epithelial areas. Such pathologies, for example, Barrett's esophagus, are precancerous conditions and may require long-term use of proton pump blockers.

Important! PPIs can sometimes be used to treat gastroesophageal reflux disease, a complication of gastric ischemia. Pathology develops against the background of impaired blood circulation in the vessels of the gastric walls and can lead to complete tissue necrosis.

Gastroesophageal reflux disease (GERD)

List of drugs and short instructions

Below is an overview of the main drug groups related to proton pump blockers, as well as a brief instruction for use.

Medicines based on pantoprazole

Pantoprazole is one of the most popular proton pump inhibitors, which is widely used in patients with chronic gastritis, pancreatitis, and gastric ulcer and intestinal ulcers. If pantoprazole preparations are prescribed for a long time, it is important to consider that they reduce the absorption of vitamin B 12 and can cause anorexia in low body weight patients.

Table. Pantoprazole preparations and their dosage.

Note! Preparations containing pantoprazole should not be used during pregnancy and lactation, as well as in children and adolescents under 18 years of age. Care should be taken to prescribe "Pantoprazole" to elderly and senile people, since long-term use in this category of patients increases the risk of severe kidney disease up to their complete dysfunction. It is forbidden to take these drugs with some antiviral drugs used to treat HIV infection, for example, "Atazanavir".

"Omeprazole" and its analogues

Omeprazole is considered the most popular drug for the treatment of acid-related diseases of the gastrointestinal tract. The agent is used to treat peptic ulcers of the intestines and stomach and can be used to correct unspecified disorders in the digestive system, accompanied by pain in the stomach, heartburn, acid belching and other symptoms of increased secretion of hydrochloric acid. The drug is available in the form of capsules containing 20 mg of omeprazole, and has a very low cost (about 24 rubles), which in most cases makes it the drug of choice for the treatment of various social categories of patients.

The daily dosage of omeprazole preparations is mg (1-2 capsules). The duration of treatment depends on the underlying disease and associated complications. Short courses (up to 7-10 days) are prescribed during an exacerbation of peptic ulcer disease, as well as for the eradication of Helicobacter pylori (in combination with antibiotics). Long-term use (up to six months) is indicated for recurrent forms of reflux esophagitis - in this case, the drug is used 1 capsule per day.

Analogues of "Omeprazole" are:

Ortanol (342 rubles);
Omez (73 rubles);
"Ultop" (116 rubles);
Omitox (118 rubles);
Ulkozol (269 rubles);
"Losek" lyophilisate (1662 rubles).

Important! Long-term use of "Omeprazole" and its analogs negatively affects the musculoskeletal system and increases the risk of injury and bone fracture (especially of the hip joints).

The effectiveness of rabeprazole and its substitutes

Rabeprazole is a sodium salt from the group of proton pump blockers with antiulcer effects. Preparations based on it are not so widely used for the treatment of pathologies of the gastrointestinal tract, since its bioavailability is 10-15% lower compared to omeprazole and pantoprazole. However, the drug has many advantages, for example:

does not have a stimulating and depressing effect on the central nervous system and respiratory function;
blocks the final stage of hydrochloric acid production;
has a high chemical similarity to fat cells;
easily penetrates into the parietal cells of the stomach and increases the secretion of bicarbonate.

The action of "Rabeprazole" begins one minute after taking it. The maximum concentration in blood plasma is reached within 2-4 hours from the moment of oral or parenteral administration. The dosage of "Rabeprazole" and its analogs is mg per day. The course of therapy depends on the main diagnosis, its stage, the degree of damage to the stomach and intestines, and the acidity of the gastrointestinal environment. Experts consider the optimal duration of taking "Rabeprazole" to be from 4 weeks to 2 months.

Table. Analogues of "Rabeprazole" and their cost.

PPI portability

In most cases, proton pump blockers are well tolerated by patients, although the incidence of side effects in different age groups can range from 13 to 31%. Most often, negative reactions during treatment are recorded in elderly patients (over 50 years old). They can be associated with the functioning of the immune (allergic reactions) or nervous system. Elderly people often complain of headaches, sleep disturbances, dizziness, drowsiness, and irritability after taking the drug. With prolonged use (more than 1 month), some patients have been diagnosed with mild to moderate depressive disorders, therefore, persons with a predisposition to psychoemotional instability should not be prescribed PPIs for more than 4 weeks.

Drowsiness is one of the possible side effects

Typical side effects for this group of drugs are:

abdominal pain;
upset stool;
nausea;
cramps in the upper abdomen;
vomiting (rare);
constipation;
flatulence with flatus syndrome.

Some, against the background of a decrease in local immunity of the mucous membranes, develop stomatitis, which requires additional symptomatic treatment.

In individuals with reduced immunity and respiratory pathologies, rare complications of PPI use are respiratory diseases (pharyngitis, rhinitis, inflammation of the paranasal sinuses, damage to the bronchi and bronchioles). In about 2-3% of patients, isolated cases of convulsive syndrome, myalgia and disorders of blood coagulation function were observed.

Can PPIs be prescribed to children?

Despite the fact that in Europe drugs of this group are actively used in pediatric practice, in Russia the use of proton pump blockers in children and adolescents is prohibited due to insufficient research data on the safety of treatment of this category of patients. Experts in the field of gastroenterology believe that prescribing PPIs for children over 6 years old is quite justified in some cases, which is confirmed by the long-term positive practice of gastroenterologists in France, Germany, Great Britain and Denmark. In these countries, it is allowed to prescribe proton pump inhibitors to children if there is a compelling indication, starting from the age of three.

Proton pump inhibitors

What do you need to know before starting treatment?

If the patient is prescribed PPIs, it is necessary to completely exclude possible malignant lesions of the intestine and stomach, which may have the same symptoms as chronic pathologies of the mucous membranes of the gastrointestinal tract. In addition, long-term use of drugs of this group in itself can increase the risk of the growth of malignant tumors, therefore, the task of specialists is to carry out a full complex of secondary diagnostics aimed at identifying concomitant diseases and disorders. Patients with liver disease need to be under the supervision of a specialist during the first three days of treatment in order to assess the frequency and intensity of side effects and adjust the treatment regimen if necessary. The same applies to individuals with partial kidney dysfunction.

Important! Some proton pump blockers, such as rabeprazole-based products, can cause headaches and increased drowsiness, so people working in high-concentration jobs should be careful during treatment. If the patient has noticed that he is drowsy, he should consult a doctor in order to adjust the treatment regimen or issue a temporary disability certificate. Performing work with severe side effects during treatment is unacceptable.

You need to be careful when treating

PPI - a group of drugs that are mandatory for the treatment of pathologies of the digestive tract, accompanied by a violation of acidity. Despite the relative safety, only a doctor should prescribe them, since improper use can cause unwanted side effects and complications. Very often, during treatment, correction of the dosage regimen is required, therefore, self-medication with drugs of this group is unacceptable.

Top 5 effective heartburn medications (hydrogen pump blockers)

In gastroenterology, hydrogen pump blockers, drugs that effectively relieve heartburn, are often used to stop the formation of hydrochloric acid in the stomach.

Quick navigation through the article:
Proton pump inhibitors - what are they?
Top 5 effective drugs
How to choose the right inhibitor
Contraindications
Consequences after taking proton pump inhibitors

Show all

What is a proton pump

Application area

Indications for taking proton pump inhibitors (PPIs):

stomach and duodenal ulcer;
erosive gastritis;
NSAID gastropathy (the appearance of ulcers due to prolonged use of non-steroidal anti-inflammatory drugs - Ketorol, Diclofenac);
Zollinger-Ellison syndrome (a malignant tumor called gastrinoma that causes an increased secretion of hydrochloric acid);
ulcers caused by severe stress;
reflux esophagitis (GERD, a disease in which the contents of the stomach are thrown into the esophagus, thereby eroding the mucous membrane);
erosion and ulcers associated with the helicobacter pylori bacterium (treatment in combination with other drugs).

Contraindications:

high sensitivity to the drug;
children up to 13 years old (during this period, the growth and formation of body systems occurs, taking medications can provoke a malfunction);
current pregnancy (1st trimester, then - with the consent of the attending physician), lactation period (studies have not been carried out, therefore there is no evidence base).

List of drugs

Diseases with a high production of hydrochloric acid have different pH values. For example, scarring of a duodenal ulcer occurs at a pH of more than 3.2 during the day, and to destroy the helicobacter pylori bacteria, a weakly acidic environment is needed, the pH is equal to or greater than 5.

Based on the pathology and pH, the doctor selects an adequate treatment regimen, prescribes the dosage and duration of taking proton pump blockers.

These drugs are superior to all other antisecretory drugs in terms of effectiveness and harmlessness. Currently, there are two generations of PPIs and combinations with other drugs. List of pill names:

Omeprazole

Manufactured and put into use in 1989. The most common drug in therapeutic practice for the treatment of the stomach. Its effectiveness has been proven over the years of use and many studies on groups of people with various diseases.

Bioavailability (this is the amount of a substance that has reached the site of action after being absorbed and transformed in the liver) is 35-45%. The maximum plasma concentration occurs in 30-60 minutes. The half-life is 1 hour. The drug is removed by the kidneys. After a single oral dose, the effect of Omeprazole occurs within the first hour and lasts 24 hours, the maximum effect is achieved after 2 hours. After stopping the use of the drug, secretory activity is fully restored after 3-5 days.

It is taken orally, washed down with water (capsules cannot be chewed). It is prescribed in 1-2 pieces (20-40 mg) for 2-4 weeks. The course of treatment depends on the form of the disease and is established by the doctor depending on the standards of medical care.

Pantoprazole

The versatility of this drug is that it can be used in long courses of therapy without fear of a carcinogenic effect on the stomach. The route of administration does not affect the pharmacokinetics, i.e. it can be taken both orally and intravenously. It is most effective in a strongly acidic environment (pH 3), practically inactive at high pH values. It has anti-Helicobacter properties and enhances the effect of other drugs against helicobacker pylori.

The effect appears quickly after a single dose and lasts about 24 hours. Reduces symptoms and increases the healing of duodenal ulcers. Admission at a dose of 40 mg maintains pH values> 3 for more than 20 hours. After a 2-week course of treatment (40 mg once a day), scarring of the duodenal ulcer is observed in 89% of patients. The recurrence rate is 55%. With 4-week therapy at a dose of 40 mg per day, complete remission is detected in 83% of patients with gastroesophageal reflux disease of the 2-3rd stage, after 8 weeks - in 93%.

Bioavailability is 72-82%. The maximum plasma concentration occurs in 2-4 hours. The half-life is 1-2 hours. Excreted in urine and feces. Insignificantly passes through the blood-brain barrier, is secreted into breast milk. Pharmacokinetics is not affected by food intake and antacids.

Lansoprazole

It is the drug with the highest ability to reduce the production of hydrochloric acid. It differs from Omeprazole in the structure of the formation of radicals, which provide an anti-secretory effect. The study revealed that on the fifth day of the use of Lansoprazole in the stomach, a pH of more than 4 is established for 12 hours (Pantoprazole's acidity was kept for 10 hours). The drug is recommended to be taken at 15, 30 and 60 mg per day (depending on the severity of the pathology). In 95% of cases, the ulcer heals within 4 weeks.

In patients with Zollinger-Ellison syndrome, it has a more positive effect. It is a gastroprotective agent: it increases mucosal oxygenation, enhances the production of bicarbonates. Reduces the growth of helicobacter pylori, forming specific immunoglobulins, increases the anti-Helicobacter activity of other drugs. Provides rapid healing and relief of symptoms of ulcers. The recurrence rate after therapy is 55–62%. With GERD, recovery by the 9th week of admission (30 mg / day) in 89.5%.

Bioavailability is over 85%. The maximum plasma concentration is after 4 hours. Excreted in urine and bile. Acid-labile, therefore it is used in the form of granules to overcome destruction in the stomach. Depending on the disease, Lansoprazole is prescribed at a dose of 15, 30 and 60 mg per day. During treatment, breastfeeding should be discontinued.

Esomeprazole

Nexium (active substance esomeprazole) is one of the newest proton pump inhibitors. It is called revolutionary in the treatment of acid-related diseases. The clearance of Nexium is lower than that of Omeprazole, and the bioavailability is much higher. As a result, a better control of acid production is obtained, which leads to a good clinical result. Its effectiveness has been proven by many scientific studies in closed randomized groups.

It is prescribed 20 or 40 mg once a day, washed down with water or dissolved in it. Under no circumstances should the tablet be chewed or broken.

Interaction with other drugs

PPIs compete with other drugs for enzymatic substances. Effects may increase (synergism) or decrease (antagonism). Careful monitoring is necessary when combining several drugs. Rabeprazole, unlike other blockers, practically does not interact with other substances, since they have a different metabolic pathway. Drug interactions:

A drug	the effect	Note
Ketocanazole	Decreased absorption of antifungal drugs	Avoid using
Phenytoin	Increased effects from the use of Omeprazole	Monitoring side effects
Anticoagulants	Enhancing Effects	Monitor prothrombin time
Diazepam	Decreased metabolism of Diazepam	Monitoring side effects
Digoxin	Increasing the concentration of Digoxin	Avoid using with Rabeprazole
Oral contraceptives, Theophylline	Increased metabolism of Theophylline and COCs (combined oral contraceptives)	Adjust doses
Antibacterial agents	Strengthening the action of antibiotics	Monitoring side effects

Side effects

The side effect is rare and reversible and mild. PPI treatment is not associated with an increased risk of atrophic gastritis, intestinal metaplasia, or adenocarcinoma.

Rare side effects:

drowsiness (take with caution to drivers);
headache;
asthenia (dizziness, weakness, nausea);
dyspepsia (diarrhea, constipation);
pain in the legs, joints;
allergies (urticaria, itching);
decrease in hematopoiesis (decrease in the formation of blood cells - leukocytes, platelets).

If you suspect and identify these symptoms, you should contact your doctor. There are usually no side effects during therapy with new-generation drugs.

Treatment with proton pump inhibitors can hide the symptoms of oncological pathology, therefore, before taking it, it is necessary to consult a doctor and undergo an examination to exclude cancer. Persons who vomit during therapy, especially with blood impurities, changes in color, consistency and odor of stools, and sudden weight loss should immediately seek help. It is necessary to choose the drug that is suitable for the treatment of a specific disease

Absorption slows down in elderly patients, in patients with impaired detoxification and metabolizing functions of the liver. Inadequate volume of distribution in kidney disease.

Not all pathologies are suitable for proton pump blockers, so do not self-medicate. It is necessary to consult a doctor for the selection of the most effective and efficient drug therapy.