Proton pump inhibitors are a list of the latest generation of drugs. Ipp in the treatment of diseases of the gastrointestinal tract. Why are PPIs prescribed?

PPIs, or proton pump inhibitors, belong to a group of pharmacological drugs used in the treatment of gastric pathologies. Medicines quickly eliminate the symptoms provoked by excessive production of hydrochloric acid. Modern representatives of PPIs are most effective: Rabeprazole, Omeprazole, Lansoprazole, Pantoprazole and. They are used as part of the complex treatment of various types of gastritis and ulcerative lesions. Before prescribing proton pump inhibitors, the gastroenterologist examines the results of laboratory and instrumental studies. When prescribing dosages and determining the duration of treatment, the doctor takes into account the general health of the patient and the presence of a history of diseases.

Omeprazole is the best known member of the proton pump inhibitor group.

Features of pharmacological preparations

Antacids have long been used to raise the pH of gastric juice. When it enters the human body, the active ingredients of the drugs enter into a chemical reaction with hydrochloric acid. The resulting neutral products are excreted from the digestive tract with each bowel movement. But antacids have serious disadvantages:

• lack of long-term therapeutic action;
• inability to act on the underlying cause of the disease.

Therefore, the synthesis of the first representative of proton pump inhibitors () made a breakthrough in the treatment of ulcers and gastritis. If antacids help to reduce the level of already produced hydrochloric acid, then PPI prevents its production. This avoids the development of dyspeptic disorders in a person - excessive gas formation, nausea, vomiting, heartburn and acid belching. The undoubted advantage of proton pump inhibitors is the ability to maintain the maximum therapeutic concentration in the systemic circulation for a long time. Only after 15-20 hours, the parietal cells of the stomach begin to produce hydrochloric acid again.

It takes a different time to activate PPI representatives in the digestive tract:

• Rabeprazole has the fastest therapeutic effect;
• Pantoprazole has the slowest action.

There are proton pump inhibitors and general properties. For example, after penetration into the gastrointestinal tract, all PPIs inhibit the production of caustic acid by more than 85%.

Warning: “When choosing a drug for the treatment of gastritis or ulcerative lesions, physicians take into account the individual sensitivity of patients to the active substance of a particular proton form inhibitor. It manifests itself in a rather peculiar way - even with a recent intake of tablets, the pH of the gastric juice drops sharply. This concentration of acid is determined within about an hour, and then there is a sharp improvement in the well-being of a person.

The action of drugs in the human body

PPIs are drug precursors. The therapeutic effect begins only after the addition of a hydrogen proton to them in the gastrointestinal tract. The active form of the drugs acts directly on the enzymes responsible for the production of hydrochloric acid. Proton pump inhibitors do not immediately begin to show their medicinal properties, but only as the accumulation of basic compounds in the tissues and their conversion into sulfenamides. The rate of decline in hydrochloric acid production may vary depending on the type of drug.

But such a difference is possible only in the first days of using PPIs. In the course of clinical studies, it has been proven that after a week of using any proton pump inhibitors, their therapeutic efficacy levels off. This is possible due to the similar chemical composition of drugs. All PPIs are substituted benzimidazole derivatives and are formed by the reaction of a weak acid. After activation in the small intestine, the drugs begin to act on the glandular cells of the gastric mucosa. It happens like this:

• PPIs penetrate into the tubules of parietal cells, turning into tetracyclic sulphenamides;
• the proton pump contains cysteine ​​receptors, with which sulfenamides bind via disulfide bridges;
• the action of (H +, K +) -ATPases located on the apical membranes of glandular cells begins to be suppressed;
• slows down, and then completely stops the transfer of hydrogen protons into the stomach cavity.

After inhibition of (H +, K +) -ATPase, the production of hydrochloric acid by the cells of the gastric mucosa becomes impossible. Carrying out antisecretory therapy is indicated for patients with any form of gastritis, even with low acidity. This is necessary for the rapid regeneration of damaged tissues - the main cause of pain in the epigastric region.

Tip: “Don't skip PPIs or stop treatment. A prerequisite for rapid tissue regeneration is the constant presence of drugs in the human body. Healing and scarring of ulceration occurs several weeks after the start of proton pump inhibitors.

Proton pump inhibitors with pantoprazole increase the effect of antibiotics

All types of proton pump inhibitors

Gastroenterologists use for the treatment of gastrointestinal pathologies five representatives of proton pump inhibitors, which differ from each other in active ingredients. If one PPI fails, the doctor replaces it with another drug. On the shelves of pharmacies, each type of antisecretory agent is represented by many structural analogues of Russian and foreign production. They can have serious price differences, despite the same dosage and number of capsules.

When choosing between analogues of one of the PPI representatives, a gastroenterologist often recommends a more expensive drug to the patient. You should not accuse the doctor of any self-interest - such a preference is justified in most cases. For example, the Russian drug Omeprazole has analogues:

• Indian Omez;
• Ultop made in Slovenia.

Many patients will not feel the difference when taking these drugs, as they show approximately the same therapeutic effect. But for some people, recovery will come after a course of treatment with Ultop. This is due not only to the quality of the active substance, but also to the various auxiliary ingredients used to form capsules and tablets. Proton pump blockers are drugs that require an individual approach when prescribing dosages and duration of course treatment.

Omeprazole is the most common and widely used proton pump inhibitor in the treatment of gastrointestinal pathologies. It stops inflammatory processes on the mucous membranes, promotes rapid regeneration of damage. Its effectiveness has been proven in the treatment of patients diagnosed with a malignant neoplasm in the stomach, which provokes increased production of hydrochloric acid. Omeprazole significantly enhances the bactericidal effect of antibiotics when they are administered simultaneously. An hour after taking the drug in the blood, its maximum concentration is detected, which persists for 2.5-4 hours.

Lansoprazole

The bioavailability of this member of the PPI group approaches 90%. The mechanism of action of Lansoprazole differs from other drugs in the design of radicals that provide an antisecretory effect. The drug contributes to the formation of the formation of specific immunoglobulins to Helicobacter pylori. As a result, the growth of the Gram-negative bacterium is successfully suppressed. This proton pump inhibitor has no effect on gastrointestinal motility. Structural analogues of Lansoprazole include: Lancid, Epicurus, Lanzap.

Pantoprazole

Unlike other PPIs, Pantoprazole can be used for a long time in the treatment of gastritis and ulcerative lesions. This method does not provoke the development of side effects. Pantoprazole is used regardless of the pH of the gastric juice, as this does not affect its therapeutic efficacy. The undoubted advantage of a proton pump inhibitor is the absence of diagnosed exacerbations of the disease after its course administration. Pantoprazole is available from manufacturers in the form of capsules for oral administration and injection solutions. The most famous structural analogues of the drug are Krosacid, Controloc, Nolpaza.

Rabeprazole

This anti-ulcer agent differs from omeprazole in the structure of the pyridine and imidazole rings, which allows Rabeprazole to more effectively bind protons and potassium ions. The proton pump inhibitor comes in the form of enteric-coated capsules. After the use of Rabeprazole, ulcerative lesions are completely cured one month after the start of the drug. Gastroenterologists include the drug in the therapeutic scheme of gastritis provoked by Helicobacter pylori. Structural analogues of Rabeprazole include: Zolispan, Hairabezol, Beret.

Esomeprazole

Due to the presence of only one S-isomer, esomeprazole is not as rapidly metabolized by hepatocytes as other proton pump inhibitors. The drug is in the systemic circulation for a long time at the maximum therapeutic concentration. The therapeutic effect of esomeprazole lasts about 15 hours, which is the highest among all PPIs. The most famous analogues of this drug are Emanera, Nexium.

Benefits of Proton Pump Inhibitors

Manufacturers produce proton pump inhibitors in the form of capsules, tablets, solutions for parenteral use. Injectable drugs are used for exacerbation of gastric pathologies, when it is necessary to quickly reduce the production of hydrochloric acid. The active substances of solid dosage forms are coated with a strong shell. It is necessary to protect proton pump inhibitors from the effects of aggressive gastric juice. Without the shell, the main compound of the drugs would quickly collapse, without having time to have any therapeutic effect.

The presence of such protection ensures that the PPI enters the small intestine and the active substance is released in an alkaline environment. This route of penetration allows drugs to exhibit maximum therapeutic properties. The undoubted advantages of drugs include:

• fast and effective elimination of heartburn and epigastric pain in patients with increased production of gastric juice and digestive enzymes;
• longer and more intense reduction in hydrochloric acid production compared to antacids and H2 receptor antagonists;
• the highest efficiency in the treatment of patients with gastroduodenitis, gastric ulcer and duodenal ulcer;
• the presence of a short half-life and a slight renal clearance;
• rapid absorption in the small intestine;
• high level of activation even at low pH values.

Proton pump inhibitors are drugs that gastroenterologists always include in the therapeutic regimen if Helicobacter pylori was detected in patients during laboratory tests. These gram-negative bacteria often cause ulcers and gastritis. Pathogenic microorganisms are equipped with flagella, with which they.

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Today, about 21 million people in the United States take prescription drugs for heartburn, pain, and stomach discomfort.

We are talking about drugs from the group of proton pump inhibitors (PPIs) and H2-histamine blockers.

But what do you have to pay for taking these highly effective drugs?

A recent study found that proton pump inhibitors are associated with an increased risk of myocardial infarction. And this is not all that patients taking PPIs may encounter.

PPIs include esomeprazole (Nexium), lansoprazole (Prevacid), rabeprazole (Pariet), omeprazole (Omez), and others.

Many drugs in this group are available without a doctor's prescription. They block the so-called proton pump in the cells of the gastric mucosa, thereby reducing the production of hydrochloric acid. Excess hydrochloric acid is the main cause of heartburn and stomach discomfort. PPIs are used in the complex treatment of stomach ulcers, gastritis and to prevent damage to the esophagus in acid reflux.

Due to the emergence of new data on the safety of PPIs and H2-histamine blockers, the medical publication WebMD decided to ask two well-known American experts what they think about these drugs.

What exactly did the researchers find?

The authors of the latest study analyzed the medical records of almost 3 million patients, many of whom were taking proton pump inhibitors and H2-histamine blockers. None of the patients had coronary heart disease.

H2-histamine blockers include the somewhat outdated drug cimetidine (Tagamet), as well as the more modern famotidine (Quamatel), ranitidine (Zantac), and nizatidine (Axid).

H2-histamine blockers, or H2-histamine receptor blockers, are classified as antisecretory drugs that reduce the production of hydrochloric acid. Unlike PPIs, these drugs block the H2-histamine receptors of the parietal cells of the stomach. They are used for chronic gastritis, peptic ulcer, Barrett's esophagus and other acid-dependent diseases.

The analysis showed that those patients who take PPIs have an increased risk of myocardial infarction. This does not apply to H2-histamine blockers. However, the design of this work does not allow to prove a causal relationship between PPI use and heart attack.

Scientists are at a loss to answer what could be the reason for such a connection, although previous studies have shown that proton pump inhibitors can damage the endothelium of blood vessels. This may explain why PPI use is associated with an increased risk of myocardial infarction.

“Based on the results of this study, we can say that with regular use of proton pump inhibitors, the risk of myocardial infarction increases by an average of 16%. On the one hand, this is a big number. But if you take into account how many heart attacks do occur, then it turns out that taking PPIs leads to 1 additional heart attack per 4,000 people taking these drugs. When you consider the huge benefits of these drugs, it's not so clear, - says Dr. Brian Lacy (Brian Lacy).

Dr. Lacey is the head of the department of gastroenterology and hepatology at the Dartmouth-Hitchcock Medical Center (Lebanon, New Hampshire, USA). He was not directly involved in the latest study.

Does the risk of heart attack depend on the duration of PPI use?

“Based on the results of this study, we cannot answer this question. We do not know if this risk depends on the duration of proton pump inhibitor use, dose, or other factors. Further work is needed for this,” says Dr Lacey.

If PPIs do damage the vascular endothelium over time, as scientists have previously argued, then it can be assumed that the risk of heart attack will increase with prolonged use of these drugs.

Can I take PPIs for a long time?

FDA experts say that proton pump inhibitors, prescribed by a doctor, are usually taken for six months. Without prescription, these drugs are allowed to be used no more than 14 days in a row and no more than 3 times a year. But American doctors say they sometimes take much longer.

According to Dr. Lacey, there is no set maximum duration of treatment for prescription PPIs - it is determined by the doctor depending on the situation. Some patients take them for years. But he stipulates that the lower the dose and the shorter the duration of treatment, the better.

“It is true that I have patients who have been taking proton pump inhibitors day after day for more than 10 years and they have no significant side effects,” Lacey said.

Why are proton pump inhibitors dangerous?

In 2012, the FDA warned that prescription PPIs can significantly lower blood magnesium levels, leading to muscle spasms and irregular heartbeats. The same year, the agency stated that PPIs increase the risk of Clostridium difficile infection with severe diarrhea.

“We know that PPI use is associated with an increased risk of bone fractures and intestinal infections. Patients are afraid to take these drugs for many reasons, but I think they are generally safe,” says Dr. Paul Buckley III, Chief Surgeon at the Heartburn and Acid Reflux Center at Baylor Scott & White Healthcare (Round Rock, Texas, USA).

What should I look for if I am already taking proton pump inhibitors?

According to Dr. Lacey, your doctor should ideally ask about unusual events at every visit.

“It’s hard to say what you need to pay attention to in the first place. One side effect, severe diarrhea, may indicate a Clostridium difficile infection, so you should definitely consult a doctor in this case. Some people who have just started taking PPIs (the first three weeks) may develop watery stools. If it does not go away after 5-7 days, you should contact your doctor. Sometimes switching to another drug helps,” Lacey says.

How to change lifestyle during treatment with proton pump inhibitors?

Dr. Lacey believes that lifestyle changes in this case are really necessary:

1. The most important thing is to follow the diet recommended by your doctor.
2. Do not eat at night and reduce the fat content in dinner. Do not eat fried and fast food.
3. Try to normalize body weight: your BMI should be no higher than 27-30.

“I tell my patients that they should eat no later than 4 hours before going to bed. This gives them time to digest properly. Fast food "on the go" can disrupt digestion and trigger heartburn. You should also avoid certain foods that cause heartburn (wine, tomatoes, mint),” adds Dr. Buckley.

Are there new drugs that are safer and more effective than PPIs?

Yes, such drugs are being actively developed today. They act on the production of hydrochloric acid in the stomach in a different way, but these drugs are currently in the early stages of testing, and they may not appear on the pharmaceutical market soon.

Comments:

• What substances belong to the family
• How do these drugs work?
• When medications are prescribed
• To whom are drugs contraindicated?

Proton pump inhibitors, drugs designed to block the formation of hydrochloric acid in the stomach, are often used in gastroenterology. These drugs inhibit the work of the proton pump in the cell membrane that produces hydrochloric acid for digestion. A new type of medicine 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 ability to significantly reduce the production of hydrochloric acid by interfering with the functioning of cell membranes was Omeprazole.

It is now the most commonly used home treatment, but has side effects that prevent it from being used for long-term therapy. Then other active substances with a similar effect were found. 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 to the market, many people got the opportunity to get rid of stomach diseases that worsened at the time 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 used Omeprazole for a long time, cell resistance to this active substance began to be detected, there was a need for drugs of similar action, but with no side effects. In the laboratories of many major pharmaceutical companies, work has begun on the creation of substances of 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 from seasonal exacerbation of peptic ulcer if it was caused by the bacterium Helicobacter pylori, which irritates the stomach wall. Each course of treatment gives only a long-term remission. For a complete recovery from ulcerative gastritis, complex treatment should be carried out, which must necessarily include a proton pump inhibitor.

All active substances belonging to the same group have a lasting 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 treatment in a hospital.

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How do these drugs work?

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

All active substances are absorbed in the small intestine and maximally accumulate in plasma 3.5 hours after taking the capsule. They enter the tubules of the parietal cells, where they begin their work of blocking their activity.

The bioavailability of known proton pump inhibitors varies, but is stable. Neither food intake nor antacids can change it. Omeprazole after the second dose of a single dose reduces 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, excreted from the body with urine. This allows you to use drugs for a long time, if the condition of the body requires it.

Omeprazole acts in the body for no more than 14 hours. And this makes it necessary to take 2 capsules per 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 greater 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, having a pH of 5.0, is the most stable and least activated. Its high bioavailability allows the use of preparations with this active substance for injection to patients in a hospital during the treatment of severe gastric lesions. Pantoprazole reacts with antibacterial drugs in complex therapy, and this enhances its therapeutic effect. This active substance has shown good results in the treatment of bronchial asthma.

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When medications are prescribed

A gastroenterologist recommends proton pump inhibitors if any acid-related disease of the digestive system is detected. Conditions where agents that suppress excess hydrochloric acid production are particularly 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, cholelithiasis and other diseases of the digestive system, which entail an increase in acid levels.

Preparations 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 compositions can be taken only after the doctor's recommendation, which he makes after the 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 does not work. 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 the genetic characteristics of the organism or formed during the course of the disease. At the beginning of treatment, the doctor determines the individual rhythm of taking and clarifies the doses of drugs using an analysis of intragastric pH. The gastroenterologist may prescribe brand-name preparations of lansoprazole, pantoprazole, or other similar drugs because generic inhibitors may contain less active substance, and this reduces the expected effectiveness of the treatment.

Omeprazole is one of the most modern antisecretory drugs used in the treatment of peptic ulcer and erosive and inflammatory diseases of the upper gastrointestinal tract.

Omeprazole inhibits the production of hydrochloric acid in the stomach and reduces its activity. This drug acquires its medicinal properties only after it enters an acidic environment, which is just characteristic of the stomach.

After ingestion, the drug actively penetrates into the special cells of the stomach that are responsible for the secretion of hydrochloric acid. In them, it accumulates and, thus, regulates the production of gastric juice and pepsin (an enzyme that breaks down proteins).

Omeprazole has a bactericidal effect on the main "culprit" of gastritis and peptic ulcer - the microorganism Helicobacter pylori (Helicobacter pylori). That is why Omeprazole is mandatory included in the list of drugs that suppress Helicobacter pylori infection in gastric and duodenal ulcers.

With pathological reflux of gastric contents into the esophagus (reflux ulcerative and erosive esophagitis), the mucous membrane is inevitably damaged, and ulcerative defects are formed on it. Omeprazole, taken orally, is able to reduce the damaging effect of hydrochloric acid, restore the pH of gastric juice and significantly reduce the severity of the main symptoms of the disease.

Nexium is a drug that reduces the production of hydrochloric acid by the glands of the stomach. By inhibiting the secretory activity of the glands, Nexium reduces the acidity of gastric juice and is used in the complex treatment of various conditions associated with excessive secretion of hydrochloric acid (for example, gastroesophageal reflux disease, peptic ulcer of the stomach or duodenum, violation of the structure of the mucous membrane under the influence of drugs from the group of NSAIDs, eradication of Helicobacter pylori, etc.).

Release forms, names and composition of Nexium

Nexium is currently available in the following three dosage forms:

• Coated tablets of 20 mg and 40 mg;
• Granules (pellets) for the preparation of a solution for oral administration of 10 mg;
• Lyophilisate for solution for intravenous administration, 40 mg.

That is, Nexium is available in two dosage forms for oral administration (tablets, pellets and granules) and one for intravenous administration. Most often, the drug is used in the form of tablets, since this is the most convenient and familiar option. Although, in principle, pellets (granules) are the same tablets, only containing a lower dosage of the active substance. To understand how insignificant the difference between these two forms is, you should know that pellets are active and excipients of the drug pressed into small flat particles, that is, in fact, granules. In pellets, these substances are located freely, and in tablets they are tightly compressed.

Pellets are used less often than tablets, since they contain a lower dosage of the active substance, which is rather inconvenient. Oral solution pellets are usually used either for children or for people who, for whatever reason, cannot swallow a tablet.

Finally, Nexium lyophilisate is used to prepare a solution for intravenous administration, which is used when it is impossible to take the medicine by mouth.

Pariet is an antiulcer drug that belongs to the group of proton pump (pump) inhibitors. Pariet is used in the treatment of gastric and duodenal ulcers of various etiologies, reflux esophagitis, stress ulcers and Zollinger-Ellinson syndrome.

Release forms, names and composition of Pariet

Currently, Pariet is produced in a single dosage form - pills coated with enteric coating. However, there are two dosages of tablets - 10 and 20 mg of the active substance, respectively. Due to the different dosages of the active substance in everyday speech, the names "Pariet 10" and "Pariet 20" are often used for their short designation. In these names, the figure reflects exactly the dosage of the tablets.

Each Pariet tablet contains either 10 mg or 20 mg as an active ingredient. rabenprazole. As auxiliary components, 10 mg and 20 mg tablets of rabenprazole contain the same substances, such as:

• Mannitol;
• magnesium oxide;
• Giproloza and giproloza low-substituted;
• magnesium stearate;
• Ethylcellulose;
• Hypromellose phthalate;
• Diacetylated monoglyceride;
• Talc;
• Titanium dioxide;
• Iron oxide red (for tablets 10 mg);
• Iron oxide yellow (for tablets 20 mg);
• Anhydrous ethanol;
• carnauba wax;
• Edible gray ink (for 10 mg tablets);
• Food ink red (for 20 mg tablets);
• Butanol.

Parieta tablets containing 10 mg of rabenprazole are colored pink, have a round, biconvex shape and are marked with ink "∈241" on one side. Tablets containing 20 mg of rabenprazole also have a round, biconvex shape with the marking "∈243" on one side, but they are painted in a light yellow color. Pariet is available in packs of 7, 14 and 28 pieces.

Nolpaza is a drug from the group of proton pump inhibitors, which reduces the production of hydrochloric acid by stomach cells, thereby reducing the acidity of gastric juice. Nolpaza is used to treat various diseases of the stomach and esophagus, in which it is necessary to reduce the acidity of gastric juice, such as peptic ulcer of the stomach or duodenum, erosive gastritis, gastric pathology caused by the use of drugs from the NSAID group (Aspirin, Indomethacin, Ibuprofen, etc.). ), stress ulcers, gastroesophageal reflux disease, Zollinger-Ellinson syndrome, as well as in combination therapy for the eradication of Helicobacter pylori.

Composition, names and forms of release

Currently, Nolpaza is available in two dosage forms - tablets for oral administration and lyophilisate for the preparation of a solution for intravenous injection. Lyophilizate for solution for injection in everyday life is often called Nolpaza ampoules. The pills are called Nolpaza 20 or Nolpaza 40, where the figure displays the dosage of the active substance.

The composition of both dosage forms of Nolpaza as an active substance includes pantoprazole in various dosages. So, tablets are available in two dosages - 20 mg and 40 mg of the active substance. The lyophilisate for the preparation of the solution contains 40 mg of the active substance per vial. That is, a ready-made solution for injection prepared from a lyophilisate will also contain 40 mg of pantoprazole.

The lyophilizate contains the following substances as auxiliary components:

• Mannitol;
• Sodium citrate dihydrate;
• Sodium hydroxide solution 1N.

Tablets of both dosages of Nolpaza contain the following substances as auxiliary components:

• Water;
• Hypromellose;
• Titanium dioxide;
• Macrogol 6000;
• Mannitol;
• Sodium carbonate anhydrous;
• Crospovidone;
• Sodium lauryl sulfate;
• Iron oxide yellow;
• Polysorbate-80;
• propylene glycol;
• Copolymer of methacrylic acid and ethyl acrylate;
• calcium stearate;
• Talc.

Tablets of both dosages are coated, colored in light yellow-brown color, and have an oval biconvex shape. On the fault, a rough mass is visible, colored in colors from white to light yellow-brown. Tablets are available in packs of 14, 28 and 56 pieces.

The lyophilisate for solution for injection is a white or white-yellowish powder that can be sintered into a single dense mass. The lyophilisate is available in sealed bottles of 1, 5, 10 or 20 pieces per box.

Why is Nolpaza prescribed (therapeutic effect)

According to the anatomical-therapeutic-chemical classification, Nolpaza belongs to antiulcer drugs, that is, its main scope is the treatment of peptic ulcer and stress ulcers of the stomach or duodenum. However, in practice, in addition to the treatment of ulcers, Nolpaza is also used in the treatment of other conditions, for the successful treatment of which it is necessary to reduce the acidity of gastric juice, for example, with gastritis, gastroesophageal reflux, etc.

Nolpaza inhibits the production of hydrochloric acid in the stomach, thereby reducing the acidity of gastric juice. Suppression of hydrochloric acid secretion is achieved by stopping the work of the proton pump, which supplies hydrogen ions to cells that produce HCl.

A decrease in the acidity of gastric juice makes it less aggressive, due to which the defects present on the mucous membranes begin to heal and heal. Thus, after some time, the ulcer heals, and the unpleasant symptoms disappear due to the presence of this defect on the gastric mucosa.

Also, a decrease in the acidity of gastric juice enhances the effect of antibiotics that destroy Helicobacter pylori, thereby increasing the effectiveness of eradication therapy. It is due to this effect that Nolpaza or other drugs that reduce the acidity of gastric juice are used in combined eradication therapy against Helicobacter pylori, in combination with antibiotics. In addition, it is now believed that the use of antibiotics in combination with proton pump inhibitors increases the effectiveness of therapy, and therefore provides complete elimination of Helicobacter pylori in a greater number of cases compared with the use of antibiotics alone.

In addition, a decrease in acidity reduces the severity of damage to the esophagus during reflux of gastric contents. It is due to this mechanism that Nolpaza is effective in the treatment of gastroesophageal reflux and GERD (gastroesophageal reflux disease).

Nolpaza completely eliminates the symptoms of diseases of the stomach and esophagus, caused by increased acidity of gastric juice, within about 2 weeks of regular use. However, for a complete cure or to achieve a stable remission, it is necessary to take the drug for at least 4 weeks.

Nolpaza, reducing the acidity of gastric juice, increases the level of gastrin. However, this increase is reversible, and enzyme levels usually return to normal after discontinuation of the drug.

The action of Nolpaza when taken in the form of tablets or when administered intravenously is exactly the same.

When ingested tablets with a dosage of 20 mg, the effect of the drug develops within an hour, and the maximum is observed after 2-2.5 hours. After the complete cessation of taking Nolpaza, the acidity of gastric juice is restored to normal parameters within 3-4 days.

Nolpaza does not change the motility of the digestive tract, and therefore does not affect the speed of the food bolus and the usual rhythm of bowel movement.

Indications for use

Nolpaza tablets and intravenous injections are indicated for the treatment of the following conditions or diseases:

• Treatment of gastroesophageal reflux disease (GERD) in various forms, including erosive and ulcerative reflux esophagitis;
• Relief of symptoms caused by GERD, such as heartburn, pain when swallowing, belching with sour, etc.;
• Treatment of erosions and ulcers of the mucous membrane of the stomach and intestines caused by taking drugs from the NSAID group (for example, Aspirin, Indomethacin, Ibuprofen, Nimesulide, Nise, Ketanov, Ketorol, etc.);
• Treatment and prevention of exacerbations of peptic ulcer of the stomach and duodenum;
• Use in combination with two antibiotics for the eradication of Helicobacter pylori;
• Zollinger-Ellison syndrome.

Instructions for use

Consider the rules for the use of tablets and lyophilisate for the preparation of a solution for injection separately in order to avoid confusion.

Nolpaza tablets (Nolpaza 20, Nolpaza 40) - instructions

Tablets of both dosages should be taken orally, swallowed whole, without biting, chewing or crushing in other ways, but with a small amount of liquid (still water, compote, etc.). The drug should be taken before meals, preferably before breakfast. If the tablets need to be taken twice a day, then it is best to do this before breakfast and dinner.

Dosages and duration of Nolpaz use are determined by the rate of recovery and the type of disease for which the drug is taken.

For the treatment of GERD, reflux esophagitis, as well as for the relief of symptoms caused by these diseases (heartburn, belching sour, pain when swallowing), it is necessary to take Nolpaza in the following dosages, depending on the severity of the pathology:

A stomach ulcer is a very, very common disease today. We eat, as a rule, unhealthy food and do not follow any regimen. And besides, we are nervous for any reason. The ecological situation is becoming more and more tense. Therefore, the increase in patients with ulcers and other digestive disorders no longer surprises anyone. Probably, two hundred years ago, an ulcer was an almost incurable disease. But you and I are very lucky. We live in an age of rapid development of medicine and pharmacology. A huge number of drugs and dietary supplements have been created to normalize digestion and restore the mucous membrane of the gastrointestinal tract. One of the most common drugs for the treatment of such diseases will be described in this article.

The group of antisecretory drugs includes proton pump inhibitors. The purpose of the therapeutic effect of these drugs is the treatment of acid-dependent pathological conditions of the stomach. The main action is to reduce the production of hydrochloric acid, which provokes irritation and inflammation of the gastrointestinal mucosa. This is achieved by blocking the proton pump type H + / K + -ATPase, localized in the parietal cells of the gastric mucosa. The modern pharmacological market offers a wide range of drugs in this group.

Purpose

Proton pump inhibitors or PPIs are designed to suppress synthesis. This is possible by inhibiting the transport of potassium ions and hydrogen from the parietal cells of the stomach. Blockers are effective in the treatment of acid-dependent gastrointestinal pathologies. We are talking about such pathological conditions:

• gastroesophageal reflux;
• esophageal dyspepsia;
• gastritis;
• peptic ulcer of the stomach or duodenum;
• duodenitis.

To PPI does not develop addiction, side effects do not appear. There are 5 generations of inhibitors, each of which increases the activity of the active ingredient and increases the duration of exposure. But in fact, the main criterion that determines the effectiveness of the blocker is the individual susceptibility of an individual organism.

The principle of operation of the proton pump in the stomach

How proton pump inhibitors work.

There are two main forms of PPIs - tablets and capsules for oral administration. Dragees are covered with an enteric coating. This means that when passing through the gastrointestinal tract, the tablet dissolves in the small intestine, is absorbed into the bloodstream, enters the liver, and then into the parietal cells, through which it acts on the stomach and its mucosa. As it accumulates in the secretory tubules, the inhibitor is converted into sulfenamide with four cycles, by which the substance adheres to the ions of the pump without leaving the boundaries of the glandular ducts.

As a result, the proton pump H + / K + -ATPase is blocked and does not take part in the production of hydrochloric acid. To resume the acid-forming process, a new H + / K + -ATPase enzyme is required, and it is produced only after 1.5-2 days. Therefore, this time interval determines the duration of the therapeutic effect of PPIs.

The first or one-time intake of an inhibitor is ineffective, since by the time the drug is taken, the proton pumps have already entered the secretory membrane, that is, the main part of the enzymes is included in the cell. As the pills are used, the microparticles are blocked gradually, as they appear on the membrane. Thus, the antisecretory action of blockers is fully performed.

The advantage of inhibitors is the possibility of stopping the disease, regardless of the level of hydrochloric acid in the gastric juice. Efficiency examples:

• a duodenal ulcer overgrows while maintaining a pH of more than 3 for 18–20 hours;
• GERD maintains a pH above 4;
• in case of Helicobacter pylori infection, treatment is based on maintaining a pH above 5.

Popular APIs

There are 5 generations of modern blockers. The first of them appeared "Omeprazole" (1989). Each generation surpasses the previous one in anti-ulcer and antisecretory therapy in terms of efficiency and safety. Below are the most popular APIs.

"Omeprazole"

The drug is one of the most common. Efficiency is expressed by:

• in the relief of inflammation;
• in the tightening of an ulcerative abscess;
• in positive dynamics in the treatment of patients with malignant gastrinoma (a tumor that provokes excessive production of gastrin);
• in enhancing the anti-helicobacter effect while taking it with antibiotics.

The bioavailability of "Omeprazole" reaches 50%. This is achieved due to 95% binding of the main component to the proteins of the liquid part of the blood. The maximum concentration of the drug is fixed 60 minutes after ingestion. This figure is stored for 3 hours.

Treatment regimen:

• 2 times a day;
• single dose - 20 mg;
• course is long.

Efficiency - scarring of the ulcer in the duodenum - by 97%, and in the stomach - by 80% (with regular intake of PPIs for a month).

"Pantoprazole"

The peculiarity of the drug is the possibility of long-term treatment in order to consolidate the effect achieved by specific antiulcer therapy. There are several forms of the drug that involve oral and intravenous administration. The PPI is able to maintain acid levels in the range of 2.3-4.3 when held for 10 hours. The advantage of treatment is the absence of relapses after the use of Pantoprazole.

It has the highest bioavailability, varying in the range of 85-90%. Another feature is a different structure of the radicals, which are responsible for the antisecretory effect. Already on the 5th day of administration, a pH greater than 4 is established in the stomach. This environment persists for 11.5 hours. The recommended doses of Lansoprazole are 15, 30, 60 mg per day. For a month of taking the medicine in 95% of patients, the ulcer is completely scarred.

"Rabeprazole"

The preparation contains substances with pyridine and imidazole cycles. Due to their reactivity, the H+/K+-ATPase proton pump binds more efficiently. Absorption of "Rabeprazole" - 51.8% when bound to blood enzymes by 96.3%. Within a month of taking the drug daily, the ulcer heals by 91%.

"Esomeprazole"

The structurally active formula of the blocker includes the S-isomer, which is not hydroxylated in the liver, unlike previous drugs with R-isomers. Consequently, "Esomeprazole" is not excreted from the body for a long time, providing more binding to proton pumps in parietal cells. Therefore, smaller dosages are required - 40 mg per day. This concentration of the main substance is enough to keep the pH no higher than 4 for 14 hours.

"Dexlansoprazole"

The Japanese antisecretor with the most favorable tolerability profile contains R-isomers. Differs in ability to keep pH of gastric juice above 4 within 16-24 hours. Features a unique oral capsule structure with dual release of the active ingredient. Due to this effect:

• molecules have 2 times longer half-life in the bloodstream;
• the required level of acid is maintained by the time the second peak of the drug concentration in the blood appears.