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Ipp drugs. Pitfalls of long-term acid suppression with proton pump inhibitors. What you need to know before starting treatment

Ipp drugs. Pitfalls of long-term acid suppression with proton pump inhibitors. What you need to know before starting treatment

26.02.2022

Particularly common:

Gastritis is observed in 80 percent of the population, gastric dyspepsia covers a percentage. It is quite clear that with such disappointing statistics, the problem of curing gastrointestinal pathologies is especially topical.

What is a proton pump?

Proton pump inhibitors inhibit the production of acid in the stomach

Pump - a technical term meaning one of the varieties of the pump. And it is a bit strange to see this name in the anatomy of the human body. However, the term proton pump, applied to hydrogen-potassium adenosine triphosphatase, is able to explain the function of this enzyme protein, which transports positive electrons through the intercellular septum.

A proton pump is also called a proton pump. This is a complex polypeptide chain, consisting of amino acid residues, and containing positive hydrogen and potassium ions in its structure. H+/K+-ATPase was isolated forty years ago as an enzymatic hydrolase protein, and at the same time it was called the proton pump. It 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 found in parental cells of the gastric mucosa. They also produce hydrochloric acid. It carries positively charged hydrogen protons (H+) from the cytoplasm of the parental (parietal) cell to the stomach cavity through the superior intercellular septum. In this case, the potassium ion (K+) moves into the cell. At the same time, chloride anions (CL-) are transported to the stomach area.

H+ protons are released as a result of the decomposition of carbonic acid (H2CO3) by the action of the enzyme carbonic anhydrase. The remaining cations (HCO3-) are transferred into the blood instead of chlorine cations, which, having moved to the stomach, and combined with hydrogen there, 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 Clv€’ ions, and K+ ions move back through the membrane.

What are proton pump inhibitors and what are they for?

Inhibition means restraint. In this case, the inhibition of the synthesis of HCl. 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 out of the cell. Inhibition proved to be effective in the treatment of acid-dependent diseases of the gastrointestinal tract, such as

Proton pump inhibitors block the production of hydrochloric acid to varying degrees. These drugs do not develop addiction, there are no side effects. Therefore, this category of drugs was adopted by the World Congress of Gastroenterologists 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 effectiveness is influenced by certain factors, the first place of which is occupied by the individual susceptibility of the organism.

PPI mechanism of action

Proton pump drugs are taken by mouth as tablets or capsules. From the stomach, the drug enters the small intestine, where 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 leave the secretory tubules, binds to the ionic residues of the pump and blocks it. Thus, H+/K+-ATPase is excluded from the formation of hydrochloric acid. In order for this process to resume, the production of a new H + / K + -ATPase enzyme is needed, which occurs after 1.5-2 days. This time determines the duration of the therapeutic effect of proton pump inhibitors.

At the first or one-time use of the drug, its effectiveness is not so significant, since not all proton pumps are currently embedded in the secretory membrane, some of them are inside the cell. These microparticles, together with newly synthesized hydrogen-potassium adenosine triphosphatases, appear on the membrane, they interact with subsequent doses of the drug, and its antisecretory effect is fully performed.

Antisecretory therapy allows you to stop diseases that are dependent on the concentration of hydrochloric acid. Thus, a duodenal ulcer heals at 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 bacterium Helicobacter pylori is destroyed in a slightly 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 pH scale, which determines the acid-base nature of liquid substances and solutions, can be compared with a mathematical straight line on which positive and negative numbers are located.

The pH value is 14 units. The chemically neutral substance water (comparable to zero on a mathematical scale) is pH7. Substances with a pH less than 7 are acidic. Those above the number 7 are alkaline. Accordingly, the lower the pH number, 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 increases.

Characterization of proton pump inhibitors

PPIs are recognized as particularly effective drugs in the treatment of peptic ulcers associated with high acidity, and occupy a leading position among antiulcer medications. The antisecretory result in this case is achieved by directly influencing the formation of hydrochloric acid.

This category of drugs surpasses all other antisecretory drugs in terms of 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 widely used and widely used drugs. Its effectiveness is confirmed by the results of studies in which over-patients with various pathologies of the gastrointestinal tract participated. In comparison of omeprazole with H2-blockers, there is an advantage of the proton pump inhibitor in the effectiveness of the relief of inflammatory processes, and at the same time, the ulcerative mucosal abscess was clearly delayed.

Even in patients with gastrinoma (a malignant tumor that produces the hormone gastrin, which stimulates the production of HCl), a positive trend was observed. In addition, omeprazole increased the anti-helicobacter effect of the antibiotics taken. Bioavailability, that is, the amount of the drug reaching the area of its effect in the body, ranges from 50%, 95 percent of which binds to plasma proteins.

The highest content of this medication in the blood is concentrated one 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 of 80-90% in the group of drugs that inhibit the production of hydrochloric acid. Lansoprazole differs from its predecessor in the design of radicals that provide an antisecretory effect.

Studies have shown that on the 5th day of use, Lansoprazole provides a pH in the stomach above 4, for 11.5 hours (for comparison, pantoprazole maintained the same acidity for 10 hours). Lansoprazole is recommended to take 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 in that it allows long-term use in order to consolidate the therapeutic effect in the treatment of peptic ulcer. Despite the variability of the result (the acid-base level ranged from 2.3 to 4.3), the methods of administration of the drug do not have a significant effect on its pharmacokinetics.

In other words, Pantoprazole is used both intravenously and orally. A ten-year observation of patients treated with pantoprazole showed that there were no relapses after the use of this drug.

Rabeprazole

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

Esomeprazole

In the structural formula of Esomeprazole, there is only one S-isomer, and therefore the drug is not as susceptible to hydroxylation by the liver as its predecessors, which have R-isomers, and are not so quickly excreted from the body. These factors increase the amount of inhibitors reaching the proton pumps in the parietal cells. Esomeprazole, taken at 40 mg per day, keeps a pH greater than 4 for 14 hours. This is the highest therapeutic effect that has been achieved to date.

Helicobacter pylori and PPIs

There are 5 generations of proton pump inhibitors in total.

Speaking about acid-dependent diseases and the causes that give rise to them, one cannot help but recall the gram-negative spiral 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. Work on the API continues

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

A new IPN is currently being developed and tested in Japan. This is tenatoprazole. It is a derivative of imidazopyridine. True, some experts believe that this drug generally 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 Russia there is no permission for its use. Now Japan is trying to promote this drug to the Western market.

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

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List of drugs - proton pump inhibitors - with a description

Proton pump inhibitors (PPIs) in the modern pharmaceutical market are isolated in the form of capsules or tablets. These medicines can only be used as directed by your doctor. You will learn more about medications from our article.

Pathologies of the gastric mucosa, which have arisen due to violations of the acidity of gastric juice, are treated with proton pump inhibitors. The 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 to eradicate the Helicobacter Pylori bacterium, as well as in the case of systematic use of drugs that adversely affect the functioning of the stomach and intestines.

How the drugs work

The drug is taken orally with a sufficient amount of water. The active substance of the drug enters the intestine, after which absorption into the blood occurs. 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. This is primarily due to the fact that these tablets have a cumulative effect, that is, they begin to work at full strength 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

A gastroenterologist prescribes proton inhibitors if the pathology of the stomach is caused by a change in the level of acidity of 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, this drug is recommended to be used 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 a child.
You can not treat the stomach with these drugs for children who have not reached 12 years of age.
Also in the list of contraindications there is a line that refers to the individual intolerance of the active substance. In this case, the doctor changes the tablets to similar ones.

Possible side effects

Each group of blockers is characterized by 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;
allergic reaction in the form of a rash on the skin.

Effective PPIs

Proton pump inhibitors can be roughly divided into five groups. Their difference is the active substance and its quantity. Depending on the active ingredient, the regimen, course of treatment or dosage of the drug may change. 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 of this group is high absorbability. These funds include: Lanzap, Helicol, Lansoprol, Lanzoptol, Lanpro, Lanset, Lansodin and others.

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

Acrylans. The drug is available in the form of capsules. 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 drink once a day. Depending on the severity of the disease, the regimen and course of treatment can be adjusted by the attending physician.
Lancid. Means 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 analogues.

Medications 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 a stomach ulcer. Many studies have proven the effectiveness of this drug. Medicines with this active substance have the advantage of low cost.

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

Consider some of the names of these proton pump inhibitors:

Omez. 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 inhibit the production of acid during the day and at night. The course of treatment is determined by the attending physician.
Bioprazol. One capsule contains 20 mg. active substance. The proton pump inhibitor effectively reduces acid production. You only need to drink one capsule per day.
Omezol. The proton pump inhibitor helps 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 a certain peculiarity - they gently affect the gastric mucosa. For this reason, the course of treatment may 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:

Controloc. The inhibitor is available in tablet form. One capsule may contain 20 or 40 mg. active component. Depending on the diagnosis, the method of administration and dosage may differ.
Nolpaza. Released in a dosage of 20 and 40 mg. The peculiarity of this drug is that its use is prohibited until the age of 18. Use it once a day, preferably in the morning.
Ulter. The proton pump inhibitor is an analogue of Nolpaza. Dosage and method of administration are identical.

Preparations based on rabeprazole

The funds of this group effectively cope with the task.

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

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

Beret. The proton pump inhibitor contains 20 or 40 mg. active component. The drug is prescribed once or twice a day, depending on the purpose of therapy.
Zulbeks. Available in the form of tablets, the composition 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 peptic ulcer of the stomach or duodenum. 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-based 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 1500 rubles.
Emanera. Assign twice a day. Contains 20 mg. active substance. Based on consumer feedback, we can conclude that the product has good efficiency, but a rather high cost.

To date, physicians and patients prefer preparations based on lansoprazole and pantoprazole. This group very rarely causes side effects and is suitable for almost every person. 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 the attending physician after a diagnostic examination.

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

Treatment of problems with the gastrointestinal tract occupies a fundamental place in therapy. More than half of the population suffers from diseases associated with a violation of the acid-forming function of the stomach. They affect performance, bring discomfort, but there are medications that alleviate conditions that help manage symptoms and improve quality of life. One such group of drugs are proton pump blockers.

A proton pump, hydrogen pump or hydrogen-potassium adenosine triphosphatase (H / K-ATPase) is an enzyme that secretes hydrochloric acid in the stomach, consisting 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. For the exchange, energy is required, the source of which is the hydrolyzed ATP molecule. With the help of a concentration gradient, chloride 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 necessary for the digestion of food and the destruction of microbes. With hyperfunction of parietal cells, increased acid formation occurs, this condition is called hyperchlorhydria. It causes stomach irritation and discomfort.

An inhibitor is the name of a substance that should inhibit enzymatic processes. These drugs include hydrogen pump blockers, intended for the treatment of diseases of the gastrointestinal tract, accompanied by increased acid formation.

Their mechanism of action is based on the 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 secretion decreases, the symptoms of heartburn, discomfort in the epigastric region, and bitterness in the mouth decrease.

Indications for taking proton pump inhibitors (PPIs):

stomach ulcer and 12 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 a gastrinoma that causes increased secretion of hydrochloric acid);
ulcers formed during severe stress;
reflux esophagitis (GERD, a disease in which the contents of the stomach are thrown into the esophagus, thereby corroding the mucous membrane);
erosions and ulcers associated with the bacterium helicobacter pylori (treatment in combination with other drugs).

high sensitivity to the drug;
children's age up to 13 years (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 (no studies have been conducted, 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 irritation of receptors located on the basal membrane layer of secretory cells. Drugs that block the activity of this protein inhibit secretory function and are used for combined therapy of conditions whose symptoms and manifestations 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 lining 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 inhibiting the activity of H+/K+-ATPase was experimentally obtained 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. Mass blockers of the proton pump began to be used since 1988, and studies conducted over the next five years made it possible to abandon surgical therapy as the main method of treating peptic ulcer.

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 prescribing. 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 submucosal layer in the process. Gastritis occurs in about every fourth inhabitant of large settlements, so 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 bacterium Helicobacter pylori, the main causative agent of infectious inflammation in the stomach, resistant to acid 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 certain scheme.

The insidious bacterium Helicobacter pylori

Other indications for the appointment of PPI 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 a tumor formation in the pancreas (ulcerogenic pancreatic adenoma);
ulceration of the mucous membrane of the stomach or the initial sections of the small intestine;
gastroesophageal reflux disease (a recurrent pathology that occurs against the background of a weakening of the muscles of the esophageal sphincter and is manifested by regular reflux of gastric contents into the esophagus);
chronic pancreatitis;
dyspeptic disorders (as a symptomatic treatment).

PPIs can be used to treat conditions of the esophageal tube that are accompanied by the formation of cylindrical epithelial patches. Such pathologies, such as Barrett's esophagus, are precancerous conditions and may require long-term use of proton pump blockers.

Important! PPIs can in some cases be used to treat gastroesophageal reflux disease, which is a complication of gastric ischemia. Pathology develops against the background of circulatory disorders in the vessels of the gastric walls and can lead to complete tissue necrosis.

Gastroesophageal reflux disease (GERD)

List of drugs and brief instructions

Below is an overview of the main drug groups related to proton pump blockers, as well as brief instructions 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 peptic ulcer of the stomach and intestines. 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 patients with low body weight.

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. Pantoprazole should be carefully prescribed to elderly and senile people, since with prolonged use in this category of patients, the risk of severe kidney disease increases, up to their complete dysfunction. It is forbidden to take the listed 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 drug is used to treat peptic ulcers of the intestine and stomach and can be used to correct unspecified disorders in the digestive system, accompanied by pain in the stomach, heartburn, sour belching and other symptoms of increased secretion of hydrochloric acid. The drug is produced 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, 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 medicine is used 1 capsule per day.

Analogues of "Omeprazole" are:

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

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

The effectiveness of rabeprazole and its substitutes

Rabeprazole is a substance in the form of a sodium salt from the group of proton pump blockers, which has an antiulcer effect. 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 with fat cells;
easily penetrates into the parietal cells of the stomach and increases the secretion of bicarbonate.

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

Table. Rabeprazole analogues and their cost.

PPI tolerance

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

Drowsiness is one of the possible side effects.

Typical side effects characteristic of this group of drugs are:

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

In some, against the background of a decrease in local immunity of the mucous membranes, stomatitis develops, requiring additional symptomatic treatment.

In persons with reduced immunity and pathologies of the respiratory organs, rare complications of taking PPIs are respiratory diseases (pharyngitis, rhinitis, inflammation of the paranasal sinuses, damage to the bronchi and bronchioles). Approximately 2-3% of patients had isolated cases of convulsive syndrome, myalgia and disorders of blood coagulation.

Can PPIs be given 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 in this category of patients. Experts in the field of gastroenterology believe that the appointment of PPIs for children older than 6 years is quite justified in some cases, which is confirmed by many years of 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 strong indication, starting at the age of three.

proton pump inhibitors

What do you need to know before starting treatment?

If a patient is prescribed PPIs, possible malignant lesions of the intestines and stomach, which may have the same symptoms as chronic pathologies of the mucous membranes of the gastrointestinal tract, should be completely excluded. In addition, long-term use of this group of drugs in itself can increase the risk of malignant tumor growth, so the task of specialists is to conduct a full range of secondary diagnostics aimed at identifying concomitant diseases and disorders. Patients with liver disease should 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 positions that require increased concentration should be careful during the treatment period. If the patient notices that he has drowsiness, he should consult a doctor to adjust the treatment regimen or issue a temporary disability sheet. Performing work with severe side effects during treatment is unacceptable.

Care must be taken when treating

PPIs are 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, a correction of the dosing regimen is required, so self-medication with drugs of this group is unacceptable.

Top 5 Effective Heartburn Drugs (Hydrogen Pump Blockers)

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

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

The so-called acid-dependent diseases include a whole complex of pathological processes that occur against the background, under the influence or in violation of acid formation in the stomach. Unfortunately, the prevalence of these diseases has only increased in recent years.

Acid-related diseases can manifest themselves at any age. Such severe conditions as gastroesophageal reflux disease (GERD), reflux esophagitis with erosions of the esophageal mucosa occur not only in adults and elderly patients, but even in children of the first year of life. The erroneous opinion that very little hydrochloric acid is produced in the stomach in young children was refuted back in the mid-1980s. A. V. Mazurin, showing that even a newborn child produces a sufficient amount of concentrated acid. Of course, the volume and concentration of acid at different ages must be assessed in relation to the volume of the stomach and the quality of food eaten by a person at different periods of life (table).

An excess of hydrochloric acid and aggressive gastric enzymes is a powerful damaging factor in the mucous membrane of the esophagus, stomach and duodenum, which confirms the postulate put forward by K. Schwartz back in 1910: "No acid - no ulcer." Other factors of aggression include various drugs, Helicobacter pylori, impaired motility of the gastrointestinal tract.

Currently, acid-dependent diseases are understood as chronic multifactorial pathological processes that require long-term therapy and increase the likelihood of concomitant treatment. To neutralize excess acid and treat acid-dependent diseases themselves, agents are used that prevent the formation of acid in the stomach or help neutralize already formed acid in the lumen of the stomach.

Currently, there are three main groups of drugs used to treat acid-related conditions.

The first one is antacids. However, the use of antacids cannot radically solve the problem. Antacids quickly neutralize the acid in the stomach lumen. However, this group of drugs has several disadvantages. First of all - a short duration of action. Even the longest-acting drugs "work" for no more than 1.5 hours. For this reason, antacid treatment requires frequent administration of large doses of drugs to achieve the desired effect. Prolonged use of antacids can lead to the development of side and unwanted effects. Side effects of the use of antacids can be manifested by a banal stool disorder with the appearance of constipation or, conversely, diarrhea, depending on the composition of the antacid preparations the patient took - aluminum- or magnesium-containing. In addition, prolonged use of antacids can lead to an imbalance in the mineral balance in the body with the development of alkalosis. Antacid therapy does not control hydrochloric acid production and cannot be used as a primary treatment for acid-dependent conditions.

Another group of drugs used to treat acid-dependent diseases include histamine H 2 receptor blockers. Inhibition of histamine H 2 receptors on the surface of the parietal cell reduces acid secretion. However, this group of drugs also has its drawbacks. Therapeutic efficacy is provided by a high level of the drug in the blood, which sometimes requires multiple doses. When using blockers of H 2 -histamine receptors of parietal cells of the gastric mucosa, suppression of gastric secretion is achieved by acting on one type of receptor, while hypersecretion of hydrochloric acid may be due to stimulation of other receptors also present on the cell surface - gastrin or acetylcholine. Finally, when using these drugs, tolerance to them can develop and a “rebound” syndrome may appear. Tolerance can develop as early as two days after the start of treatment, therefore, at present, H 2 -histamine receptor blockers are practically not used for treatment.

The third group of drugs are proton pump inhibitors (PPIs). PPIs are most effective for the treatment of acid-related diseases. They are significantly superior to histamine H2-receptor blockers, prokinetics, cytoprotectors, and placebo in their clinical efficacy and ability to control acid suppression processes. All modern PPIs (omeprazole, lansoprazole, pantoprazole, rabeprazole, esomeprazole) are substituted benzimidazoles that differ in radicals in the pyridine and benzimidazole rings. These are weak bases that accumulate in the secretory tubules of parietal cells, where, at low pH values, they are transformed into a chemically active form (tetracyclic sulfenamide) and irreversibly bind to H + /K + -ATPase (proton pump), blocking the active transfer of hydrogen ions from the intercellular space into the excretory ducts of the gland. Its restoration occurs after the incorporation of new proton pumps into the membrane of the secretory tubules, free from binding to the active metabolite of PPI, so the duration of the antisecretory effect is determined by the rate of renewal of proton pumps, that is, the rate of renewal of gastric epithelial cells.

PPI, acting on the parietal cell, controls daytime, food-stimulated and nocturnal secretions, inhibits the production of hydrochloric acid, regardless of the stimulus acting on the receptors of parietal cells, does not cause the development of "rebound" syndrome and tolerance, quickly suppresses acid secretion. That is why PPIs allow 24-hour control of gastric secretion and are the main tool for the treatment of acid-related diseases.

The high pharmacological safety of PPIs is ensured by the selectivity of their accumulation in the body and the specificity of their interaction with H + /K + -dependent ATPase, the proton pump of the parietal cell of the gastric glands. The higher the selectivity of the action of the drug, the better it is tolerated by the patient and the fewer adverse reactions it causes. After taking PPIs and their absorption in the small intestine, their active part, a benzimidazole derivative, selectively accumulates by diffusion in the acidic environment of the secretory tubules of the parietal cell. There, the protonation of the nitrogen atom of the pyridine ring of the PPI molecule occurs and the transition to the active form - sulfenamide, due to which it becomes possible to bind to the thiol groups of cysteine as part of the proton pump and block this enzyme. Charged (protonated) forms of substituted benzimidazoles are concentrated where the pH is below pK, and their protonation occurs. In a living cell, there are compartments with an acidic environment - lysosomes, neurosecretory granules and endosomes, where the pH level is 4.5-5.0. With full stimulation of the parietal cell, the pH of the secretory tubule reaches 0.8. Thus, for selective accumulation in the secretory tubule, the pK of the IPP must be below 4.5. The concentration of these drugs in the secretory tubules of the parietal cell is 1000 times higher than their concentration in the blood.

With an increase in the level of intragastric pH against the background of taking (especially long-term and in high doses) PPIs, hypergastrinemia develops due to the reaction of G-cells. Acid production is regulated by a negative feedback mechanism: when the pH shifts to the alkaline side, gastrin-producing cells are activated and gastrin is secreted, which affects both parietal cells directly and enterochromaffin-like (ECL) cells. Gastrin and histamine, produced by ECL cells, serve as activating stimuli for parietal cells - acid production resumes. When prescribing PPIs, intragastric pH is under drug control, and reciprocal hypergastrinemia is an expected effect.

Is long-term hypergastrinemia dangerous during the use of PPIs, especially in terms of the development of oncological processes? This question was answered by the results of experiments conducted on rats with long-term administration of PPIs. Thus, a significant increase in the level of gastrin and the possibility of the occurrence of carcinoid tumors emanating from ECL cells were shown, and hyperplasia of ECL cells depends on the dose of PPI and on the sex of the animal. Subsequently, significant differences were identified between the likelihood of developing tumors from ECL cells in an experiment on rats and when using PPIs in humans: different susceptibility to damage to the gastric mucosa of hypergastrinemia (in the experiment, hypergastrinemia develops only with lifelong intake of PPIs) and the specific genetic predisposition of ECL cells rats to hyperplasia.

In general, given the many years of experience in the use of PPIs in clinical practice, based on many meta-analyses, not a single case of the occurrence of not only carcinoid, but even pre-stage carcinoid has been recorded. Therapy with lansoprazole for up to 4 years, omeprazole for up to 7 years was not associated with any neoplastic or dysplastic process in the endocrine or non-endocrine cells of the stomach.

Metabolism of almost all existing proton pump inhibitors occurs mainly in the liver by cytochrome P450. As a result of the competitive interaction of PPIs and other drugs, the metabolism of which also takes place with the participation of this cytochrome, the intake of PPIs can affect the hepatic metabolism of some drugs, changing their activity. PPIs can potentially alter the solubility of other substances or interfere with their release from dosage forms with pH-dependent solubility. The more drugs the patient takes, the higher the likelihood of interactions between them. In clinical practice, drug interactions involving substituted benzimidazoles are rarely significant, but careful monitoring of patients taking omeprazole and phenytoin or warfarin concomitantly is recommended. It is possible that lansoprazole affects the metabolism of theophylline via CYP1A2.

Data from epidemiological studies and, in particular, the MEGRE study conducted in Russia, initiated by the Central Research Institute, indicate that the prevalence of GERD increases with the age of the population. If in respondents under 44 years of age quantitative signs of GERD are detected in 10.8%, then after 60 years - in 18.8%, while in older women the prevalence of GERD reaches 24%. In elderly patients, as a rule, several chronic diseases are observed. So, according to A. A. Masharova (2008), 59.3% of elderly patients with GERD have arterial hypertension, 41.1% have coronary heart disease (CHD). And a multicenter study conducted in the UK showed that of 5453 patients with GERD observed in 360 medical institutions, 20.1% had concomitant arterial hypertension, 16.8% of patients suffered from arthritis, 13.6% had coronary artery disease, 10% chronic obstructive pulmonary disease was determined, in 8.8% - mental disorders.

Many single and multicenter studies have been conducted by various researchers, showing that people over 65 years of age, as a rule, suffer from a number of chronic diseases and are forced to take 3 to 8 different medications daily. Recently, drug interactions between PPIs and the antiplatelet agent clopidogrel, widely used in the treatment of patients with coronary artery disease, have been discovered and are being investigated. Compared with acetylsalicylic acid monotherapy, its combination with clopidogrel significantly reduces the incidence of recurrence of acute myocardial infarction (AMI). To reduce the risk of gastrointestinal complications, patients receiving such therapy are prescribed PPIs. Since clopidogrel is a prodrug whose bioactivation is mediated by cytochrome P450 isoenzymes, mainly CYP2C19, taking PPIs metabolized by this cytochrome may reduce the activation and antiplatelet effect of clopidogrel. In May 2009, at the 32nd Annual Conference of the Society for Cardiovascular Angiography and Interventions (SCAI), data were presented showing that the concomitant use of clopidogrel and PPI significantly increases the risk of major adverse cardiovascular events. which include myocardial infarction, stroke, unstable angina, the need for repeated coronary interventions, and coronary death. This conclusion was made based on the results of a large-scale study conducted in the United States in the analysis of the Medco database, which assessed the risk of complications while taking PPIs and clopidogrel in patients undergoing stenting. It turned out that the risk of adverse cardiovascular events in patients who took PPIs together with clopidogrel (number of patients (n) = 9862) was 25%, while in those who did not take PPIs (n = 6828) the risk was lower - 17 ,nine% . In connection with the above, SCAI has issued an official statement, which states that further study of this issue is necessary. The Food and Drugs Administration of the United States (FDA) has published a message about a possible decrease in the effect of clopidogrel when taking PPI (omeprazole) and about the undesirability of using this combination. At the same time, a population-based case-control cohort study was published in March 2009 among Ontario residents aged 66 years and older who started clopidogrel after being discharged from hospital after treatment for AMI (n = 13636). The main group consisted of 734 patients who died or were rehospitalized with AMI within 90 days after discharge from the hospital. The control group included 2057 patients who were correlated with the main age and the predicted probability of early death (within 0.05), determined using the cardiac risk prediction model. PPI intake during clopidogrel therapy was taken into account. Primary analysis found a significant association of readmission for AMI with current PPI use (adjusted odds ratio (OR) 1.27, 95% confidence interval (CI) 1.03-1.57). A stratified analysis did not reveal an association between pantoprazole and recurrent MI in patients receiving clopidogrel (OR 1.02, 95% CI 0.70-1.47). In contrast, other PPIs were associated with a 40% increased risk of recurrent MI within 90 days of discharge (OR 1.40, 95% CI 1.10-1.77). Thus, in patients taking clopidogrel after acute myocardial infarction, concomitant use of PPIs that inhibit cytochrome P450 2C19 (omeprazole, lansoprazole or rabeprazole) is associated with an increased risk of recurrent MI. This effect, not observed with pantoprazole therapy, seems to reflect a disturbance in the metabolic bioactivation of clopidogrel. Until further data are available on the clinical significance of drug interactions with clopidogrel, concomitant therapy with clopidogrel and PPIs other than pantoprazole should be limited whenever possible. Of all PPIs, pantoprazole has minimal affinity for CYP2C19 and CYP3A4. Phase II of biotransformation consists in conjugation with sulfate and proceeds in the cytosol. The potential for pantoprazole to be involved in drug interactions is limited compared to other PPIs. A July 2009 review of the literature on PPI-clopidegrel interactions (PubMed 1980-January 2009, Proceedings of the American Heart Association (AHA) 2008 convention and the 2009 SCAI scientific session) noted, that there is sufficient data to indicate that omeprazole has a significant drug interaction with clopidogrel. Further studies are required regarding the interaction of other PPIs with it. If it is necessary to use PPIs in patients taking clopidogrel, it is recommended to give preference to pantoprazole. In studies conducted at the Central Research Institute for IHD in patients with coronary artery disease, it was noted that among patients suffering from GERD, while taking clopidogrel or warfarin for 1 year of observation, repeated heart attacks were observed only in those who were treated with various omeprazole derivatives, and none one on background therapy for GERD with pantoprazole. However, it should be noted that these data are still being processed and it will be possible to speak about them with full confidence only after a complete analysis of the data obtained.

Thus, PPIs are a proven, safe and quite powerful tool in the way of acid-related diseases. Elderly patients with GERD who need to take multiple drugs while taking PPIs, taking into account the profile of drug interactions, preference should be given to pantoprazole, for example, Controloc.

Literature

Mazurin A.V. Diseases of the digestive system in children. Moscow: Medicine, 1984. 685 p.
Humphries T. J., Merritt G. J. Drug interactions with agents used to treat acid-related diseases // Aliment Pharmacol Ther. 1999; 13 Suppl. 3:18-26.
Onasanwo S. A., Singh N., Olaleye S. B., Palit G. Anti-ulcerogenic and proton pump (H + , K + ATPase) inhibitory activity of Kolaviron from Garcinia kola Heckel in rodents // Indian J Exp Biol. Jun 2011 49(6):461-468.
Wilder-Smith C. H., Halter F., Hackiv W., Merki H. S. pH-feedback controlled infusions of ranitidine are no more effective than fixed-dose infusions in reducing gastric acidity and variability in antisecretory responses // Br. J. clin. Pharmac. 1992, 33, 487-493.
Hogan W. J., Dodds W. J. Gastroesophageal reflux disease (reflux esophagitis). Gastrointestinal disease: Pathophysiology, diagnosis, management, 4 th ed (Sleisenger M. N., Fordtran J. S. eds) W. B. Saunders, Philadelphia, 1989, pp. 594-619.
Modlin I. M., Sachs G. Acid related diseases. biology and treatment. Schnetztor-Verlag GmbH, Konstanz. 1998. P. 126-42.
Lapina T. L. Safety of proton pump inhibitors // Clinical perspectives of gastroenterology, hepatology. 2009, no. 4, p. 22-28.
Ekman L., Hansson E., Havu N. et al. Toxicological studies on omeprazole // Scand. J. Gastroenterol. 1985 Vol. 20 (Suppl. 108). P. 53-69.
Haveu N. Enterochromaffin-like cell car-cinoids of gastric mucosa in rats after life-long inhibition of gastric secretion // Digestion. 1986 Vol. 35 (Suppl. 1). P. 42-55.
Freston J. W., Borch K., Brand S. J. et al. Effects of hypochlorhydria and hypergastrine-mia on structure and function of gastrointestinal cells: a review and analysis // Dig. Dis. sci. 1995 Vol. 40 (Suppl). 50S-62S.
Johnson A. G., Seidemann P., Day R. O. NSAID-related adverse drug interactions with clinical relevance: an update // Int J Clin Pharmacol Ther. 1994; 32:509-532.
Belousov Yu. B., Leonova M. V. Fundamentals of clinical pharmacology and rational pharmacotherapy. M.: JSC Publishing house "Bionika". 2002. S. 254-258.
Grass U. Drug interactions with proton pump inhibitors // Der Kassenarzt. 2000, 43, p. 32-39.
Johnson et al. // Int J Clin Pharmacol Ther 1994; 32:509-32. Steward, Cooper. Drugs & Aging 1994; 4:449-461.
Ho P. M., Maddox T. M., Wang L. et al. // JAMA. 2009 Vol. 301, No. 9. P. 937-44.
Simon W.A. Pantoprazole: which cytochrome P450 isoenzymes are involved in its biotransformation? //Gut. 1995; 37: A1177.
Radhofer-Welte S. Pharmacokinetics and metabolism of the proton pump inhibitor pantoprazole in man // Drugs Today. 1999; 35:765-772.

P. L. Shcherbakov, doctor of medical sciences, professor

GBUZ TsNIIG DZM, Moscow

L. Lundell, Sweden

The problem of comparability of various proton pump inhibitors in terms of their metabolism, pharmacokinetics, ability to suppress acid production by parietal cells, and clinical efficacy in the short and long term is discussed. There are currently two generations of PPIs. The first generation drugs (omeprazole, pantoprazole, lansoprazole and rabeprazole) have approximately the same ability to suppress gastric acid production. The therapeutic efficacy of the drug largely depends on the time during which the pH value in the stomach is maintained above 4. When using first-generation PPIs in therapeutic dosages, pH< 4 в желудке поддерживается более 12 часов приблизительно у 40% больных.

Rice. one.
The mechanism of action of H + ,K + -ATPase inhibitors

The next step in the creation of new PPIs was the synthesis of esomeprazole, which is based on the separation of the racemic mixture of omeprazole into right- (R-) and left-hand (S-) isomers. This method is a fundamental achievement, its developers were awarded the Nobel Prize in Chemistry in 2001. The R-form of omeprazole is significantly less effective than the S-form (esomeprazole) due to their differences in biochemical availability. Most of the R-form is metabolized in the liver and does not reach the parietal cell. These benefits of esomeprazole metabolism are realized in a larger area under the concentration-time curve (AUC) compared to that of omeprazole. The use of esomeprazole allows more effective suppression of gastric acid production in healthy volunteers and patients with GERD, when assessed on the first or fifth day of treatment. pH retention time< 4 в желудке при использовании эзомепразола была на 10-15% выше, чем при использовании ИПП первого поколения. Кривая зависимости эффективности подавления выработки кислоты от дозы препарата выходит на плато при дозе эзомепразола 40 мг/сут-ки. Способность эзомепразола быстро и эффективно подавлять выработку кислоты может быть использована при проведении диагностического теста с ИПП при подозрении на ГЭРБ. По данным большинства исследований, чувствительность теста с эзоме-празолом составляет 80-90% при однократном назначении 40 мг препарата в течение 5 дней. По результатам мета-анализа, эффективность эзомепразола в лечении ГЭРБ на 10% превышала эффективность других ИПП в краткосрочной и долгосрочной (6 месяцев) перспективе. Следует подчеркнуть, что поскольку основным предиктором клинической эффективности ИПП является способность этих препаратов длительно контролировать выработку кислоты, а у эзомепразола эта способность максимальная, экономически не оправдано проводить исследования по сравнению эффективности эзомепразола и рабепразола.

Rice. 2.
Nexium has metabolic advantages, resulting in more drug being delivered to the site of action and inhibiting proton pumps

Rice. 3.
The area under the concentration-time curve is higher for Nexium than for omeprazole for each mg of the substance, and the ACC increases more significantly with respect to the dose.

Rice. 4.
Effect of Esomeprazole and Other PPIs on Intragastric pH in GERD Patients

Rice. 5.
Healing rate of esophagitis at 8 weeks, PPI/PPI isomer vs omeprazole

Rice. 6.
Nexium test for verification of GERD

Another area of use for PPIs is in the treatment of bleeding peptic ulcers. Coagulation and aggregation of platelets do not occur in an acidic environment, in which the blood clot quickly disintegrates, and pepsin is inactivated at pH values.< 5. Показано, что эзомепразол, вводимый внутривенно или внутрь, поддерживает рН в желудке < 4 в течение более длительно, чем пантопразол вводимый внутривенно.

Not all PPIs are equally effective. There are significant differences in the pharmacokinetics and metabolism of esomeprazole and first-generation PPIs, which is reflected in the control of gastric acid production and clinical manifestations of acid-dependent diseases.

Not all APIs are the same:

metabolic pathway
Pharmacokinetics
Ability to suppress acid production
Clinical Efficiency!

How the drugs work

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

Basically, proton pump inhibitors are aimed at reducing hydrochloric acid, which is necessary in the treatment of ulcers. The fact is that with increased acidity of gastric juice, a stomach or duodenal ulcer progresses. Reducing acidity is necessary in order to speed up the healing process of ulcers in the stomach. In addition, these funds are prescribed for chronic diseases of the gastrointestinal tract as a prevention of exacerbations twice a year.

Indications for use

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, this drug is recommended to be used only as directed by a doctor.

If your diagnosis is not confirmed by a specialist, this kind of self-treatment can lead to irreversible consequences.

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 a child.
You can not treat the stomach with these drugs for children who have not reached 12 years of age.
Also in the list of contraindications there is a line that refers to the individual intolerance of the active substance. In this case, the doctor changes the tablets to similar ones.

Despite the manufacturer's recommendations, in some cases, the doctor may prescribe pills during pregnancy and lactation. This usually happens in extreme cases, when there is no other way out for a woman "in position".

Possible side effects

Each group of blockers is characterized by 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;
allergic reaction in the form of a rash on the skin.

Effective PPIs

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

The active substance and its dosage are prescribed by the attending physician, depending on the type of disease, its severity, symptoms and contraindications in the patient.

Lansoprazole-based preparations

The difference of this group is high absorbability. These funds include: Lanzap, Helicol, Lansoprol, Lanzoptol, Lanpro, Lanset, Lansodin and others.

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

Acrylans. The drug is available in the form of capsules. The package contains 30 mg of active ingredient. 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 drink once a day. Depending on the severity of the disease, the regimen and course of treatment can be adjusted by the attending physician.
Lancid. Means for the treatment of acid-dependent diseases of the gastrointestinal tract, produced in capsules. One capsule contains 15 mg of the active ingredient. 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 of the active ingredient. One package contains 10 capsules. The method of administration and dose is no different from the above-mentioned analogues.

Medications based on omeprazole

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

Consider some of the names of these proton pump inhibitors:

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

It should be noted that omeprazole-based proton pump inhibitors are outdated and are rarely used today as a treatment for diseases of the gastrointestinal tract.

Medicines based on pantoprazole

The proton group has a certain peculiarity - they gently affect the gastric mucosa. For this reason, the course of treatment may 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:

Controloc. The inhibitor is available in tablet form. One capsule may contain 20 or 40 mg of the active ingredient. Depending on the diagnosis, the method of administration and dosage may differ.
Nolpaza. Released in a dosage of 20 and 40 mg. The peculiarity of this drug is that its use is prohibited until the age of 18. Use it once a day, preferably in the morning.
Ultera. The proton pump inhibitor is an analogue of Nolpaza. Dosage and method of administration are identical.

After the final recovery, medications can be prescribed as a prophylaxis.

Preparations based on rabeprazole

The funds of this group effectively cope with the task.

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

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

Beret. The proton pump inhibitor contains 20 or 40 mg of the active ingredient. The drug is prescribed once or twice a day, depending on the purpose of therapy.
Zulbeks. Produced in the form of tablets, the composition contains 20 mg of the 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 peptic ulcer of the stomach or duodenum. Contains only 15 mg of the active ingredient.

Most often, tablets or capsules based on rabeprazole are prescribed in the presence of a stomach ulcer.

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-based 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 1500 rubles.
Emanera. Assign twice a day. Contains 20 mg of active ingredient. Based on consumer feedback, we can conclude that the product has good efficiency, but a rather high cost.

Depending on the severity of the disease, the dosage may vary.

Updated: 07/23/2019 18:29:34

Judge: Natalia Shneider

*Overview of the best in the opinion of the editors of the site. About selection criteria. This material is subjective, is not an advertisement and does not serve as a guide to the purchase. Before buying, you need to consult with a specialist.

Proton pump inhibitors (PPIs) are a group of drugs that reduce the production of hydrochloric acid in the stomach. Doctors recommend these funds for both therapeutic and prophylactic purposes.

When are proton pump inhibitors prescribed?

The main indication for drugs from this group is diseases caused by high acidity of gastric juice: peptic ulcer of the stomach or duodenum. As they wrote in old textbooks: "no acid - no ulcer." This position remains true even after the discovery of the true cause of peptic ulcer - a bacterium called Helicobacter Pilory (Helicobacter pylori).
To destroy this bacterium, proton pump inhibitors can also be prescribed in normal stomach acidity. Helicobacteria has adapted well to existence in an acidic environment, and with an increase in pH above 4, it becomes more sensitive to antibiotics. Therefore, for its eradication, a complex of PPIs is prescribed, and 2-3 antibacterial agents.
Another acid-dependent disease in which proton pump inhibitors are prescribed is complicated gastroesophageal reflux disease. When it disrupts the normal operation of the lower esophageal sphincter - a circular muscle that blocks the flow of stomach contents into the esophagus. Constantly getting on the unprotected mucous acid causes inflammation, ulcers, disrupts the normal structure of cells, which over time can lead to a malignant neoplasm. PPIs are recommended to protect the esophageal mucosa from the action of acid.
Another situation where drugs from this group are recommended for people with normal stomach acidity is chronic pancreatitis with excretory pancreatic insufficiency. Simply put, when the gland, depleted by constant inflammation, produces an insufficient amount of enzymes for normal digestion. In such cases, enzyme preparations are usually prescribed. But for them to work, you need an alkaline environment. Alkaline to neutralize the acidic food bolus that came from the stomach is synthesized by the same pancreas, and if it is insufficient, the tablets with enzymes taken may also be ineffective. To prevent this from happening, proton pump inhibitors are prescribed, reducing the acidity in the stomach, and, therefore, in the food bolus that comes out of it.
For preventive purposes, proton pump inhibitors are recommended for people who are forced to regularly take drugs from the group of non-steroidal anti-inflammatory drugs: diclofenac, ibuprofen, paracetamol, aspirin, etc. These drugs slow down the regeneration of the gastric mucosa and often cause silent, asymptomatic ulcers. To prevent this, PPIs are prescribed.

Rating of the best proton pump inhibitors

Nomination	place	Name of product	price
Best OTC Proton Pump Inhibitors	1		73 ₽
	2		162 ₽
	3		1 698 ₽
Best Prescription Proton Pump Inhibitors	1		132 ₽
	2		350 ₽
	3		898 ₽
The best combined drugs	1		1 030 ₽
	2		425 ₽

Best OTC Proton Pump Inhibitors

Speaking about drugs dispensed from pharmacies without a doctor's prescription, it should be noted that drugs with the same active ingredient may turn out to be both prescription and not. For example, Omez, which we will talk about in this section of the ranking of the best proton pump inhibitors, is available from pharmacies without a prescription. And its domestic counterpart Gastrozol is prescription. An even stranger situation has developed with Ultop, which contains a similar active ingredient: 10 mg capsules are available without a prescription, and 20 and 40 mg are prescription. Therefore, no matter how much we want to use only active substances in the rating, leaving readers to choose from the proposed analogues, taking into account financial possibilities, in this section of the ranking of the best proton pump inhibitors, we are forced to use the trade names of the drugs.

OTC PPIs can be taken on their own for 2 weeks, but if they don't provide relief in the first 3 days, it's best to see a doctor right away.

Active ingredient: Omeprazole.

A time-tested product that combines proven effectiveness and affordable price. Available in capsules of 10, 20 and 40 mg. Capsules are taken 1 time per day half an hour before meals with water. If necessary, the capsule can be opened and the contents mixed with water or food.

The dosage is selected individually, most often the therapeutic effect appears when taking 20 mg, but often 10 mg is enough (or, conversely, a higher dose is needed).

The most common side effects are headache, insomnia, dizziness, diarrhea or constipation, nausea, bloating, and abdominal pain.

The drug is contraindicated for use in children under 18 years of age (omeprazole is allowed in pediatrics from the age of 2, but there are separate forms for patients of this age), with individual intolerance.

Can be used during pregnancy.

Possible non-prescription analogues: Ultop.

Advantages

economy,
can be taken by pregnant women.

disadvantages

does not combine with some antiviral and antifungal drugs (for more details, see the instructions)

Active ingredient: pantoprazole.

The combination of German quality and relatively affordable price. Available in tablets of 20 and 40 mg, without a prescription it is released only in the minimum dosage.

Take 20 mg once daily before meals with plenty of fluids (some patients may require a higher dose).

It is effective from the first days of admission, but the maximum effect is achieved only after a week of regular use (if in the first days it reduces gastric secretion by 26%, then after a week - up to 50%), therefore, it is possible to judge the disappearance of symptoms not earlier than after 5-7 days reception. Acidity is restored in 3 - 4 days after the end of the application.

Unlike the rest of the proton pump inhibitors in this section of the best remedies, Controloc can be taken without consulting a doctor for up to 4 weeks.

The most common side effects are indigestion (nausea, bloating, pain, constipation or diarrhea); headache, dizziness.

It is combined with almost any drug (with the exception of azatanovir, in which therapy it is contraindicated to take Controloc).

Possible non-prescription analogues: Panum, Paltaz.

Advantages

relatively affordable price,

disadvantages

14 tablets per package, which is inconvenient for regular use.

Active ingredient: rabeprazole

Formally, the license for the production of this medicine belongs to the Russian branch of Johnson and Johnson, but the substance (active ingredient) is produced in Switzerland, and the tablets themselves are in Japan. So the quality of this proton pump inhibitor is undeniable, but the price is quite high.

Available in dosages of 10 and 20 mg, the first is released without a prescription.

Take 1 tablet per day, without crushing or chewing the tablet. Neither the time of day nor food intake affect the effectiveness of the drug.

The effect begins to appear within an hour after ingestion, and after a day, gastric secretion decreases by 69%.

It is combined with most drugs, but concomitant use with azatonavir is not recommended.

Contraindicated in case of individual intolerance, pregnancy, lactation and children under 18 years of age due to the lack of safety studies in these groups.

Possible non-prescription analogues: Beret, Norflux, Ulcernil, Rabelok.

Advantages

effectiveness does not depend on food intake,
combined with most drugs.

disadvantages

high price.

Best Prescription Proton Pump Inhibitors

In this section, we have collected drugs that should only be sold by prescription.

Active ingredient: esomeprazole.

It is produced in the form of tablets for oral administration of 20 and 40 mg, as well as in the form of a powder for the preparation of suspensions in a dosage of 10 mg.

This is one of the few original modern medicines with an affordable price (except for the powder form, which has no analogues on the Russian market)

At the first dose, the action begins within an hour, the effect “reaches its maximum” by the 5th day of use, reducing the concentration of hydrochloric acid in gastric juice by 90%.

The usual method of application is 1 time per day, but if the medicine was prescribed in combination with antibiotics to destroy Helicobacter pylori - 2 times a day along with antibiotics.

Esomeprazole powder can be used to treat children, but indications are limited to GERD and reflux esophagitis.

Side effects - headache, dyspepsia.

Contraindicated in case of individual intolerance, children under one year old, pregnant women and lactating women due to lack of safety data.

Possible analogues: Esomeprazole, Emaner, Pemozar, Rediomez

Active ingredient: lansoprazole.

Available in capsules of 15 and 30 mg.

The effect increases during the first 4 days of administration, at the maximum, a decrease in the synthesis of hydrochloric acid is achieved up to 97%. Restoration of functions occurs 3-4 days after cessation of use. Eating slows down absorption but does not affect effectiveness.

Use once a day, preferably in the morning. If the medicine is prescribed to destroy Helicobacter pylori, it should be taken 2 times a day. If antacids are prescribed in parallel, it is better to take them separately from Lancid, as they prevent the complete absorption of the drug.

Possible adverse events are typical for the entire group of proton pump inhibitors - abdominal discomfort, stool disorders, bloating, headache.

Contraindicated in case of individual intolerance, in the 1st trimester of pregnancy (but there are no safety studies in other periods), during lactation.

Possible analogues: Lanzabel, Lanzaptol, Epicurus.

Advantages

affordable price;

disadvantages

prohibited during pregnancy.

The active substance is dexlansoprazole.

On the one hand, this remedy is based on a relatively new active substance with high biological activity. On the other hand, until the patent has expired and generics have not appeared, the original manufacturer remains a monopolist, and the price of a medicine is quite high.

Available in capsules of 30 and 60 mg.

The peculiarity of this drug is not only in the active substance, but also in the release form. In ordinary, at first glance, capsules, several types of granules are packed, which dissolve in the intestine, depending on the pH of the medium. That is, after taking, not all the active substance is released at once. and different granules dissolve at different times as the food bolus advances. Due to this, the effect comes on more smoothly and lasts longer. If necessary, the capsule can be opened and the contents diluted in a small amount of water or food that does not require chewing.

Possible side effects are flatulence, dyspepsia.

Contraindicated in case of individual intolerance, patients taking HIV protease inhibitors, children under 18 years of age, pregnant and lactating women.

Advantages

original drug,
modified release, prolonging the effect.

disadvantages

high price.

The best combined drugs

As already mentioned, proton pump inhibitors are often prescribed in combination with antibiotics to destroy Helicobacter pylori, eliminating the cause of an ulcer or gastritis. To save the patient from having to remember when and which pills to take, they began to produce drugs that combine these groups of drugs in one remedy. Another possible combination is proton pump inhibitors and agents. normalizing the motility of the gastrointestinal tract. They are prescribed for the treatment of reflux esophagitis.

Strictly speaking. this is not a single drug, but a set of tablets and capsules containing the proton pump inhibitor omeprazole, the antibiotic clarithromycin, and the antibacterial and antiprotozoal agent tinidazole. All this is packed in strips with the inscription "morning" or "evening". It is necessary to take the contents of the corresponding strip during or immediately after a meal, as is clear from the description - in the morning and in the evening. It is impossible to divide, chew or otherwise crush tablets or capsules.

Contraindicated in:

component intolerance,
alcoholism (cannot be combined with ethyl alcohol),
liver or kidney failure,
impaired bone marrow hematopoiesis,
children, pregnant, lactating.

The course of treatment is from 7 to 14 days, specific recommendations are given by the attending physician. The packaging of the drug is designed for 7 days, so you may need two.

Contraindicated in:

the simultaneous use of some antiviral, antifungal and antibacterial agents (for more detailed information, we refer readers to the instructions, since the list is not limited to 1 - 2 items);
gastrointestinal bleeding, perforation, intestinal obstruction;
insufficiency of liver function of moderate and severe degree,
pregnant and lactating,
children under 18 years of age.

Advantages

normalizes the motility of the esophagus, stomach, intestines,

disadvantages

a wide range of contraindications,
possible side effects.

Attention! This rating is subjective, is not an advertisement and does not serve as a purchase guide. Before buying, you need to consult with a specialist.