What are proton pump inhibitors and how can they help?

Updated: 02/24/2021 17:56:39

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Proton pump inhibitors (PPIs) are a group of medications that reduce the synthesis of hydrochloric acid in the stomach. Doctors recommend these remedies for both therapeutic and preventive purposes.

When are proton pump inhibitors prescribed?

1. The main indication for drugs from this group is diseases caused by increased 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 ulcers - a bacterium called Helicobacter Pilory.
2. To destroy this bacterium, proton pump inhibitors can be prescribed even if the acidity of the gastric contents is normal. Helicobacter has adapted well to living in an acidic environment, and when the pH increases above 4, it becomes more sensitive to antibiotics. Therefore, to eradicate it, a complex of PPIs and 2–3 antibacterial agents are prescribed.
3. Another acid-dependent disease for which proton pump inhibitors are prescribed is complicated gastroesophageal reflux disease. It disrupts the normal functioning of the lower esophageal sphincter, a circular muscle that blocks the flow of stomach contents into the esophagus. Constantly exposed to unprotected mucous membranes, acid causes inflammation, ulcers, and disrupts the normal structure of cells, which over time can lead to malignant neoplasms. To protect the esophageal mucosa from the effects of acid, PPIs are recommended.
4. Another situation when 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 insufficient amounts of enzymes for normal digestion. In such cases, enzyme preparations are usually prescribed. But for them to work, they need an alkaline environment. The alkali for neutralizing the acidic food bolus coming from the stomach is synthesized by the same pancreas, and if it is insufficient, 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 bolus of food that comes out of it.
5. For preventive purposes, proton pump inhibitors are recommended for people who are forced to regularly take medications from the group of non-steroidal anti-inflammatory drugs: diclofenac, ibuprofen, paracetamol, aspirin, etc. These medications slow down the regeneration of the gastric mucosa and often cause “silent”, asymptomatic ulcers. To prevent this, PPIs are prescribed.

Participation of hydrochloric acid and enzymes in gastric digestion

Hydrochloric acid is produced by the parietal cells in the body and fundus of the stomach, creating an acidic environment that is optimal for the action of gastric juice enzymes. Under the influence of hydrochloric acid, inactive pepsinogen in gastric juice is converted into active pepsin.

Gastric digestion

Protein foods are mainly digested in the stomach - this is the first stage of gastric digestion of protein: swelling, coagulation (denaturation) of protein occurs, dilution of food by the multicomponent contents of the stomach and enzymatic breakdown (hydrolysis, digestion) of plant and animal proteins of food.

Gastric digestion converts proteins into polypeptides and oligopeptides, smaller protein particles that are prepared for final digestion in the intestines by pancreatic enzymes. When a significant amount of undigested protein enters the intestine, the proteolytic action of enzymes secreted by the pancreas (trypsin, chymotrypsin, etc.) and the intestinal wall (polyamino- and dipeptidases) may be insufficient. On the surface of the villi of the small intestine, parietal hydrolysis of the protein occurs, the formation of amino acids and their immediate absorption into the blood to participate in the synthesis of protein structures in the human body, reducing body weight.

Along with the lack of digestion in the stomach and absorption of protein products in the upper intestinal tract, their transfer into thick porridge, where they are used by bacteria, increases. The process of bacterial breakdown of protein and amino acids (rotting) is accompanied by the formation of substances (proteinogenic amines - histamine, cadaverine, etc.) and aromatic compounds (indole, skatole, etc.). The neutralization of these compounds occurs in the liver. With excessive formation of protein decay products in the colon, bloating (flatulence) occurs, and general intoxication of the body with these substances may occur. A complex violation of the first stage of protein digestion in clinical practice is observed after gastric surgery (gastric resection), when 2/3 of the stomach or the entire stomach is removed, thus eliminating or sharply limiting the secretory function of the stomach and the partial flow of protein into the intestine. Gastric juice has a bactericidal effect on the microflora of the stomach and intestines.

The stomach contents of 10% of healthy people are sterile due to the bacteriostatic and bactericidal effects of hydrochloric acid and lysozyme. When gastric secretion is preserved, it does not exceed 103 microorganisms in 1 ml of gastric juice; anaerobic microorganisms predominate. When aggressive and protective factors of the stomach are violated, the use of drugs (antisecretory and antacids) disrupts the microecology of the stomach and gastric dysbiosis occurs when the opportunistic flora becomes pathogenic, so according to data published in Gastroenterol & hepatol (2000 Mar), taking antacids leads to increased increase in the number of H. pylori, Enterobacter, Staphylococcus and Propionobacterium.

The use of antisecretory drugs that reduce the acidity of gastric juice (PPIs, histamine H2 blockers) promotes the penetration of infection entering the stomach with food, changes in the composition and quality of microorganisms in the stomach and excessive growth of microflora in the intestinal lumen due to the lack of the bactericidal effect of active gastric juice.

About the Castle factor

The antianemic Castle factor is produced in the stomach, and food iron is converted from trivalent to divalent, which is more easily absorbed in the intestines. Without Castle factor, vitamin B12 is not absorbed in the intestines and does not enter the bloodstream, but is excreted in the feces. Disorders of the microflora lead to a decrease in the formation of B12-like substances, and some representatives of the microflora fight for vitamin B12, which enters the body with food.

A decrease in the formation of Castle factor in the stomach leads to the development of B12 deficiency anemia. The source of B12 in the human body is only animal food (see article B12-deficiency anemia).

The administration of antisecretory drugs (usually proton pump inhibitors - PPIs) reduces the acidity of gastric juice and thereby complicates the transition of 3-valent iron contained in food into 2-valent iron, which is absorbed many times faster in the small intestine. Iron deficiency anemia develops. When iron is deficient, there is a lack of absorption of iron in the intestines, appetite decreases, the frequency of meals decreases, weakness and fatigue develop, and body weight decreases.

Hydrochloric acid regulates the production of gastric juice, so when the pH in the antrum of the stomach is equal to 3.0, secretion begins to inhibit.

Hydrochloric acid has a regulating effect on gastric motility and the process of evacuation of gastric contents into the duodenum.

Rating of the best proton pump inhibitors

Best Over-the-Counter 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 or may not be prescription drugs. For example, Omez, which we will talk about in this section of the rating of the best proton pump inhibitors, is available from pharmacies without a prescription. And its domestic analogue, Gastrozol, is a prescription drug. An even stranger situation has developed with the drug Ultop, which contains a similar active ingredient: 10 mg capsules are available without a prescription, and 20 and 40 mg capsules are prescription. Therefore, no matter how much we would like to use only active ingredients in the rating, allowing readers to choose from the proposed analogues taking into account financial capabilities, in this section of the rating of the best proton pump inhibitors we are forced to use the trade names of the drugs.

Over-the-counter PPIs can be taken on your 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.

Omez

Rating: 4.9

Active ingredient: Omeprazole.

A time-tested product that combines proven effectiveness and an affordable price. Available in capsules of 10, 20 and 40 mg. Capsules are taken once a 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 10 mg is often sufficient (or, conversely, a higher dose is necessary).

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 approved in pediatrics from 2 years of age, but there are separate forms for patients of this age), in case of individual intolerance.

Can be used during pregnancy.

Possible over-the-counter analogues: Ultop.

Advantages

• efficiency,
• can be taken by pregnant women.

Flaws

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

Control

Rating: 4.7

Active ingredient: pantoprazole.

A combination of German quality and relatively affordable price. Available in tablets of 20 and 40 mg, available without a prescription only in minimal dosages.

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

It is effective from the first days of use, 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%), so the disappearance of symptoms can be judged no earlier than after 5 - 7 days reception. Acidity is restored 3 to 4 days after use.

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

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

It can be combined with almost any medicine (with the exception of azatanovir, during therapy with which Controloc is contraindicated).

Not recommended for children under 18 years of age, pregnant or breastfeeding women due to lack of information about safety in these groups of people.

Possible over-the-counter analogues: Panum, Paltaz.

Advantages

• relatively affordable price,
• Compatible with most medications.

Flaws

• There are 14 tablets per package, which is inconvenient for constant use.

Pariet

Rating: 4.5

Active ingredient: rabeprazole

Formally, the license to produce 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 produced in Japan. So the quality of this proton pump inhibitor is beyond doubt, but the price is quite high.

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

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

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

It can be combined with most medications, but simultaneous 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 over-the-counter analogues: Beretta, Norflux, Ulcernil, Rabelok.

Advantages

• effectiveness does not depend on food intake,
• Compatible with most medications.

Flaws

• high price.

Doctor of Medical Sciences Professor E.B. Shustov, Candidate of Medical Sciences A.A. Ihalainen PROTON PUMP INHIBITORS AND THEIR EFFECTIVE USE
The study of the molecular mechanisms of the formation of hydrochloric acid in gastric juice made it possible to identify its key link - the active secretion of protons, coupled with K+ transport, realized a special membrane complex - a proton pump. While the formation of protons during various intracellular reactions is controlled by various regulatory factors (acetylcholine, histamine, gastrin, prostaglandins, gastrointestinal tissue factors, etc.), the operation of this mechanism is practically unrelated to physiological regulatory mechanisms. Therefore, the development of drugs that can reduce the activity of proton pump ATPase is an important task in pharmacology. The first proton pump inhibitor was omeprazole (on the market in Sweden since 1987), followed by lansoprazole (since 1992, France). Pantoprazole was introduced in Germany in 1994. Recently, the drugs rabeprazole (UK) and esomeprazole (Sweden) have appeared.

Pharmacological characteristics

Proton pump inhibitors belong to the chemical class of substituted benzimidazole derivatives and have an antisecretory effect due to inhibition of H+, K+-ATPase (proton pump) of parietal cells of the gastric mucosa. In the tubules of the gastric glands, proton pump inhibitors, being weak bases, interact with a hydrogen ion and are transformed into sulfenamide derivatives, which form covalent bonds with the SH groups of cysteine ​​H+, K+-ATPase on the surface of the apical membrane of parietal cells facing the lumen of the gastric glands , and block the final stage of hydrochloric acid formation. This connection is irreversible, therefore the duration of action of the proton pump inhibitor depends on the rate of synthesis of new proton pump molecules, as well as on the duration of circulation of the drug in the blood. All compounds of this group are quickly activated in a strongly acidic environment (pH less than 3.0). In a less acidic environment (pH ~ 3.5-7.4), pantoprazole is chemically more stable than omeprazole or lansoprazole; it is less transformed into the active form. Therefore, its inhibitory ability in reactions from neutral to moderately acidic is approximately 3 times less than omeprazole. The drugs reduce basal and stimulated gastric secretion, regardless of the nature of the stimulus. Their clinical effectiveness is the highest among antiulcer drugs. These drugs ensure the maintenance of intragastric pH at a level of 3.0 and above for 18 hours a day, which promotes scarring of ulcerative defects in a short time. Duodenal ulcers scar in 2 weeks in 60% of patients, in 4 weeks in 96% of patients, scarring of stomach and duodenal ulcers was noted in ranitidine-resistant ulcers in 94.4% of cases. Proton pump inhibitors are used in anti-Helicobacter (eradication) therapy. Although their bactericidal effect is controversial, especially since they are all used in granules that have a special shell, which dissolves in the small intestine at alkaline pH values, and are enclosed in a gelatin capsule.

Indications for use:

• non-ulcer dyspepsia;
• peptic ulcer of the stomach and duodenum;UL>
• peptic ulcer;
• stress ulcers;
• erosive and ulcerative esophagitis;
• reflux esophagitis;
• Zollinger-Ellison syndrome;
• polyendocrine adenomatosis;
• systemic mastoidosis;
• Helicobacter pylori infection.

Contraindications:

• hypersensitivity;
• malignant neoplasms in the gastrointestinal tract;
• pregnancy (especially the first trimester);
• breast-feeding.

Side effects:
From the gastrointestinal tract
: dyspepsia, nausea, diarrhea, constipation, abdominal pain, flatulence, dry mouth, lack of appetite;
From the nervous system
: headache, dizziness, weakness (including muscle), sleep disturbance, drowsiness, depression, anxiety, restlessness, agitation, hallucinations;
From other organs and systems:
allergic reactions (bronchospasm, pharyngitis, rhinitis, skin rashes, itching), myalgia, arthralgia.
With short (up to 3 months) courses of therapy with proton pump inhibitors, side effects rarely develop. With long-term (especially for several years) continuous use of these drugs, patients develop hypergastrinemia, the symptoms of atrophic gastritis progress, and nodular hyperplasia of endocrine cells (ECL cells) of the gastric mucosa, which produce histamine, may develop. Hypergastrinemia is most pronounced with the use of rabeprazole. 2-3 weeks after cessation of treatment, serum gastrin levels return to baseline. If prolonged or continuous maintenance treatment is required to reduce the severity of hypergastrinemia, proton pump inhibitors are recommended to be taken together with synthetic prostaglandin analogues (misoprostol) or pirenzepine, which significantly reduce gastrin levels. The use of proton pump inhibitors also leads to an increase in serum pepsinogen I levels. Hypergastrinemia and increased pepsinogen I levels during treatment with these drugs are significantly more pronounced in patients with Helicobacter pylori infection than in patients in whom it has been eradicated. Taking omeprazole at a dose of 40 mg daily led to a decrease in the motor-evacuation function of the stomach. After a 10-day course of treatment, differences were observed in serum concentrations of motilin, gastrin and cholecystokinin in the omeprazole and placebo groups. A decrease in the motor-evacuation function of the stomach due to hypomotilinemia during treatment with proton pump inhibitors may be one of the reasons for the occurrence of gastroesophageal reflux disease after eradication therapy. Interactions with other pharmacological drugs: Pharmacokinetic
It is possible to change the pH-dependent absorption of drugs belonging to the groups of weak acids (deceleration) and bases (acceleration).

Dosage regimen
: Orally:
in the morning, before meals.
Without chewing. Take a small amount of water. Intravenously
: once a day. The use of proton pump inhibitors in elderly patients does not require dose adjustment. Since proton pump inhibitors have a slow onset of action (no earlier than 1 hour), they are not suitable for on-demand therapy (at the time of pain or heartburn). For such therapy, it is more advisable to use modern antacid drugs or soluble tablets of H-2 blockers (the effect manifests itself within 1-6 minutes).

Release form

The drugs are available in a dosage form that has an acid-resistant coating that dissolves in the intestines.

Precautionary measures

Use with caution in children and elderly patients. Treatment of patients with reduced liver function should begin with half doses, gradually increasing them to the recommended ones. The activity of liver enzymes should be regularly checked; if they increase, the drug should be discontinued. Before starting and after finishing therapy, endoscopic monitoring is required to exclude malignant neoplasms, since lansoprazole can mask symptoms and delay the establishment of an accurate diagnosis. It is necessary to stop breastfeeding for the period of treatment.

Comparative characteristics of drugs

Omeprazole, pantoprazole and lansoprazole differ in chemical structure, bioavailability, half-life, etc., but the results of their clinical use are almost identical. The minimum inhibitory concentration for omeprazole is 25-50 mg/l, lansoprazole - 0.78-6.25 mg/l, pantoprazole - 128 mg/l. Treatment regimens with lansoprazole provide earlier onset of clinical remission compared to omeprazole. The recurrence rate of peptic ulcers after treatment with lansoprazole is 55-62%, pantoprazole - 55%, omeprazole - 41%. Currently, only omeprazole and lansoprazole are approved for long-term maintenance therapy. Long-term use (more than 5.5 years) of omeprazole in patients does not lead to the development of neoplastic changes. In patients with peptic ulcer disease who received maintenance therapy with pantoprazole at a dose of 40-80 mg daily for more than 3 years, there was a slight and statistically insignificant increase in the number of ECL cells. Unlike omeprazole and lansoprazole, pantoprazole interacts significantly less with the cytochrome P-450 system. Taking antacids, like food, does not affect the pharmacokinetics of pantoprazole. Sucralfate and food intake may alter the absorption of lansoprazole. The pharmacokinetics of omeprazole can be altered by food intake, but is not affected by liquid antacids. Therefore, lansoprazole and omeprazole are taken 30 minutes before meals, and pantoprazole - regardless of meals.

Treatment costs:
Omeprazole
The price of a 21-day oral course of omeprazole (20 mg per day) ranges from 60 (Omizak, Torrent) to 1470 (Losec, Astra) rubles. The lower price range (60-100 rubles for a 21-day course) includes the following drugs: Omizak (Torrent), Zolser (Aurobindo Pharma), Zerotsid (Sun Pharm.), Romesec (Ranbaxy Labs.), Omez (Dr.Reddy's Labs. ), Omeprazole (Olainskiy HFZ), Omeprazole (Akrikhin), Vero-Omeprazole (Styrene). More expensive (from 110 to 250 rubles) are the courses of drugs Gastrozol (ICN October), Omeprazole (KRKA), Omeprol (Zdravle). And by far the leader is Losek from Astra (course price 1250-1470 rubles).

Lanzoprazole

Lanzoprazole is represented on the market by Lanzap drugs from Dr. Reddy's Labs. (price of a 21-day course is 80-200 rubles) and Lansofed (Moskhimfarmpreparaty, course price is about 240 rubles).

Omeprazole
Omeprazole
5-Methoxy-2-[[(4-methoxy-3, 5-dimethyl-2-pyridinyl) methyl]sulfinyl] 1H-benzimidazole Table 1. Omeprazole preparations for oral use (not shown in the online version)

Table 2. Omeprazole preparations for parenteral use (not shown in the online version)

The reference representative of the group is the drug Losek from ASTRA (Sweden). The substance used by the company is the standard of purity, and the microgranules in capsules used for oral administration are the standard of stability. The Losec production technology developed by the company ensures very high stability of the solubility, absorption and bioavailability of omeprazole, which significantly affects the clinical effectiveness of its use.

Pharmacological characteristics

Has an antiulcer effect. It is highly lipophilic and easily penetrates into the parietal cells of the gastric mucosa, where it accumulates and is activated at an acidic pH value. Inhibits the H+ K+-ATPase of the secretory membrane of parietal cells, stopping the release of hydrogen ions into the gastric cavity. Bactericidal for Helicobacter pylori. It is quickly and fairly completely absorbed from the gastrointestinal tract, but bioavailability is no more than 50-55% (first-pass effect through the liver). Maximum plasma concentration is achieved after 0.5-3.5 hours. Protein binding 95%. The half-life is 0.5-1 hour (with normal liver function) or 3 hours (with chronic liver diseases). Subject to biotransformation in the liver. Metabolites are not active. Excreted by the kidneys in the form of metabolites (72-80%) and through the intestines (18-23%). After a single dose of 20 mg, inhibition of gastric secretion occurs within the first hour, reaches a maximum after 2 hours and lasts about 24 hours. The severity of the effect depends on the dose. The ability of parietal cells to produce hydrochloric acid is restored within 3-5 days after the end of therapy. A feature of omeprazole is that after repeated use, absorption of the drug increases, while its antisecretory effect increases. The injection form of the drug (the only representative on the Russian pharmaceutical market is Losek from the Swedish company Astra) is used for rapid relief (in the first 1-2 days) of clinical symptoms of exacerbations of acid-related diseases of the upper digestive tract, especially those with a complicated course. Particularly important is the intravenous use of Losek for gastroduodenal bleeding that occurs as a complication of peptic ulcer disease, portal hypertension, as well as for stress, steroid, indomethacin (or when using other ulcerogenic drugs) and other acute ulcers. Numerous clinical studies have shown the possibility of conservatively stopping such bleeding without surgical intervention. The intravenous form of Losek is also convenient if it is impossible to take the drug orally.

Side effects

General for the group, as well as:

• fever,
• photosensitivity,
• paresthesia,
• interstitial nephritis,
• alopecia,
• gynecomastia,
• impotence,
• taste disturbances,
• stomatitis,
• candidiasis,

From the hematopoietic organs: thrombocytopenia, leukopenia, agranulocytosis, pancytopenia.

Interaction

General for the group, as well as:

• Enhances the effect of coumarins and diphenine.
• Slows down the elimination of drugs metabolized in the liver by microsomal oxidation (warfarin, diazepam, phenytoin).
• Increases (mutually) the blood concentration of clarithromycin.

Doses and use
Orally:
For gastric ulcers, duodenal ulcers and reflux esophagitis - 20 mg once a day (if necessary - 40 mg).
For duodenal ulcers, the course of treatment is 2-4 weeks, for stomach ulcers and reflux esophagitis - 4-8 weeks. For the prevention of peptic ulcers - 20 mg 1 time per day. For Zollinger-Ellison syndrome: initial dose - 20-60 mg per day, if necessary up to 120 mg / day (daily dose above 80 mg should be divided into two doses) for 2-8 weeks. The level of secretion in the stomach should be up to 10 mmol HCl/h in unresected patients, and up to 5 mmol HCl/h in resected patients. For peptic ulcers caused by Helicobacter pylori, in combinations: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg or omeprazole 20 mg, metronidazole 400 mg, clarithromycin 250 mg 2 times a day for 7 days. Intravenous:
1 time per day. The substance (40 mg) is dissolved in 100 ml of saline or 5% dextrose solution and administered within 20-30 minutes after dilution. The infusion should be completed within 12 hours if the vehicle is saline and within 6 hours if diluted in dextrose. Usually, infusions for 2-5 days are sufficient, after which the patient can be transferred to oral administration of the drug.

Overdose
Symptoms:
blurred vision, confusion, headache, increased sweating, drowsiness, dry mouth, nausea, flushing, tachycardia, arrhythmia.
Treatment:
symptomatic. Given the high level of binding to plasma proteins, dialysis is not effective.

Precautionary measures

In patients with severe liver failure, the dose should not exceed 20 mg per day.

Lansoprazole
Lansoprazole
2-[[[3-Methyl-4-(2, 2, 2-trifluoroethoxy)-2 pyridyl]-methyl] sulfinyl] benzimidazole Table 3. Lansoprazole preparations for oral use (not shown in the online version)

Lansoprazole substance is also produced by CHEMO IBERICA SA (Spain).

Pharmacological characteristics

Has an antiulcer effect. Reduces acid production in the stomach, regardless of the type of stimulating factor, by specifically blocking H+ K+-ATPase (proton pump) of parietal cells. The rate and degree of inhibition of basal and stimulated secretion of hydrochloric acid depend on the dose: pH begins to rise 1-2 and 2-3 hours after taking 15 and 30 mg, respectively, and secretion decreases to 80-97%. Restoration of H+ K+-ATPase activity occurs with a half-life of 30-48 hours. Inhibits the production of pepsin and has a gastroprotective effect. Suppresses the growth of Helicobacter pylori. The drug is used in the form of granules with a special coating. Thanks to the acid-resistant coating, lansoprazole is not destroyed in the stomach and, being absorbed quite completely in the small intestine, enters the systemic circulation. The maximum concentration in plasma is achieved after 1.5-2.2 hours, bioavailability is at least 80% of the dose. After eating, bioavailability decreases by 50%, but this does not affect the inhibition of acid production. In the dose range from 15 to 60 mg, the pharmacokinetics are linear - the measured concentrations are proportional to the dose, the parameters are constant and no accumulation occurs. Plasma protein binding is 97-99%. The half-life is 1.0 hour in healthy subjects and 2-3 hours in patients with chronic liver diseases. Metabolized in the liver, 2/3 of the metabolites are excreted in bile, the rest in urine (renal failure does not significantly affect the rate and amount of excretion).

Interaction
Pharmacokinetic
Reduces the clearance of theophylline by 10%. Inhibits the metabolism of diazepam and phenytoin. Sucralfate reduces bioavailability by 30%; an interval between taking these drugs is required for 30-40 minutes. Antacids containing aluminum and magnesium hydroxides should be taken no earlier than 2 hours after taking lansoprazole.

Doses and administration
Orally:
Non-ulcer dyspepsia: 15-30 mg per day for 2-4 weeks. Stomach ulcer: 30-60 mg per day for 4-8 weeks. Erosive-ulcerative esophagitis: 30-60 mg per day for 4-8 weeks. Reflux esophagitis: 30 mg per day for 4 weeks. Zollinger-Ellison syndrome: the dose is individually selected to ensure basal acid production below 10 mmol/h. Helicobacter pylori infection: 30 mg 2 times a day in various combinations with metronidazole, tetracycline, bismuth oxide, clarithromycin or amoxicillin for 7 days.

Side effects

General for the group, as well as:

• paresthesia,
• interstitial nephritis,
• changes in the blood (eosinophilia, leukopenia, pancytopenia, thrombocytopenia),
• petechiae,
• peripheral edema.

Precautions
For Helicobacter pylori infection, the drug should not be used as monotherapy before starting a course of combination eradication therapy.

Pantoprazole Panthoprazole

Table 4. Oral pantoprazole preparations (not shown in the online version)

Pharmacological characteristics

After a single dose of the drug, the therapeutic effect lasts for 24 hours.

Side effects

General for the group, as well as:

• swelling;
• increase in body temperature.

Doses and use Orally:
40-80 mg per day. Course of treatment: 2 weeks (up to 4-8 weeks).

Rabeprazole

Produced by ESAI Ltd for Jansen Pharmaceuticals (UK) under the name Pariet. Release form: enteric-coated tablets of 10 and 20 mg. In animal experiments, inhibition of the proton pump by rabeprazole is partially reversible. In vitro, rabeprazole has 2-10 times greater antisecretory activity than omeprazole. Rabeprazole, compared to omeprazole, has a shorter duration of action. Its complex with H+-K+-ATPase is prone to dissociation. In comparative clinical studies, rabeprazole was significantly more active than placebo, famotidine or ranitidine and was as effective as omeprazole in the treatment of patients with erosive or ulcerative reflux esophagitis and gastric and duodenal ulcers. The presence of Helicobacter pylori did not affect the healing process. The antisecretory effect after oral administration of 20 mg occurs within 1 hour and reaches a maximum after 2-4 hours. Inhibition of basal and food-stimulated acid secretion 23 hours after taking the first dose is 62 and 82%, respectively, duration of action is 48 hours After finishing the dose, secretory activity returns to normal within 2-3 days. In the first 2-8 weeks of therapy, serum gastrin concentrations increase and return to baseline levels within 1-2 weeks after discontinuation. An important feature of the drug is the absence of side effects from the central nervous system, cardiovascular and respiratory systems. Eradication of Helicobacter pylori at the end of a 7-day course of therapy was observed when treated with combinations of rabeprazole with:

• clarithromycin + metronidazole in 100% of cases;
• clarithromycin + amoxicillin in 95%;
• amoxicillin + metronidazole in 90%;
• clarithromycin in 63%.

Dosage regimen: Orally
: 20 mg 1 time per day, in the morning. Course of treatment for gastric and duodenal ulcers: 4-6 weeks, if necessary - up to 12 weeks; for reflux esophagitis: 4-8 weeks. The tablets are swallowed whole, without chewing or crushing. Tolerability of rabeprazole 20 mg once daily in comparative studies was the same as famotidine 20 mg twice daily, ranitidine 150 mg four times daily, or omeprazole 20 mg once daily. Side effects of a single dose of rabeprazole 20 mg were observed in 0.7-2.2% of patients and included moderate dizziness, nausea, headache, diarrhea, general malaise, and itching. In case of an overdose of the drug, the following may occur: nausea, diarrhea, constipation, abdominal pain, flatulence, headache, dizziness, drowsiness, weakness, skin rash, increased activity of liver transaminases, thrombocytopenia, leukopenia; pharyngitis, rhinitis, asthenia, back pain, flu-like syndrome, myalgia, dry mouth, calf muscle cramps, arthralgia, fever. Rarely - anorexia, weight gain, depression, visual or taste disturbances, stomatitis, increased sweating.

Interaction:

Slows down the elimination of certain drugs metabolized in the liver by microsomal oxidation (diazepam, phenytoin, indirect anticoagulants). Reduces the concentration of ketoconazole by 33%, digoxin by 22%.

Esomeprazole

It is produced by Astra under the name Nexium. The first approval for the use of this drug was received in March 2000 in Sweden, where its promotion was planned to begin in August 2000. This approval also gives the right to use the drug in Norway and Iceland. In July 2000, Nexium (esomeprazole) underwent registration and approval in all countries of the European Union. Promotion of the drug in the UK began last fall. It is expected to be approved in the United States (registration documents were submitted to the FDA in December 1999), Canada, Australia, New Zealand and Switzerland. Currently, the drug is registered in Russia. Nexium at a dose of 40 mg provides more effective, pronounced, rapid and long-lasting control of hydrochloric acid secretion compared to omeprazole at standard therapeutic doses of both 20 and 40 mg, other drugs of this class at standard doses, such as pantoprazole at a dose of 40 mg and lansoprazole at a dose of 30 mg. Nexium is the first drug to demonstrate significant clinical benefits over omeprazole. A new regimen for using the drug Nexium has been proposed - as needed, which allows doctors to prescribe the drug to patients who need a single dose of the drug to relieve symptoms of the disease only when needed. Clinical trial results showed that after six months of treatment, up to 90% of patients were able to effectively control the symptoms of their disease by taking Nexium only as needed. This approach to long-term control of symptoms of gastroesophageal reflux disease is effective, convenient for patients, and appears to be attractive in terms of cost-effectiveness. Another regimen for using Nexium is triple therapy for one week in the treatment of duodenal ulcer associated with Helicobacter pylori. This regimen is as effective as triple therapy containing omeprazole for one week followed by omeprazole monotherapy for a further three weeks. Nexium has a similar safety profile to omeprazole, and the most common adverse effects are headache, abdominal pain, and diarrhea. Nexium will replace the drug Losec (omeprazole) from the same company.

Literature Belousov Yu. B., Asetskaya I. L. Pharmacotherapy of peptic ulcer. Clinical pharmacology and therapy, 1993, v2. P. 54-57 Komarov F.I., Grebenev A.L., Sheptulin A.A. et al. Guide to gastroenterology: In three volumes. T. 1. Diseases of the esophagus and stomach. - M.: Medicine, 1995. - 672 p. On standards (protocols) for diagnosis and treatment of patients with diseases of the digestive system / Order of the Ministry of Health of the Russian Federation dated April 17, 1998 No. 125 // Healthcare, No. 7, 1998. - P. 103-139. Register of Medicines of Russia - encyclopedia of medicines. Seventh edition, revised and expanded / Ch. editor Yu.F. Krylov. - M.: RLS-2000, 2000. - 1520 p. Secrets of gastroenterology / Transl. from English - M. - St. Petersburg: ZAO Publishing House BINOM, Nevsky Dialect, 1999. - 1023 p. Vidal Directory. Medicines in Russia: Directory. - Moscow, 2000. Federal guide for doctors on the use of medicines (formulary system): Issue I. - M.: GEOTAR Medicine, 2000. - 975 p.

Table 5. Proton pump inhibitors on the market (not shown in the online version)

Best Prescription Proton Pump Inhibitors

In this section we have collected drugs that should only be sold with a doctor's prescription.

Nexium

Rating: 4.8

Active ingredient: esomeprazole.

Available in the form of tablets for oral administration of 20 and 40 mg, as well as in the form of 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 effect 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 use is 1 time per day, but if the medicine is prescribed in combination with antibiotics to destroy Helicobacter, 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 due to lack of safety data.

Possible analogues: Esomeprazole, Emanera, Pemosar, Rediomez

Lancid

Rating: 4.6

Active ingredient: lansoprazole.

Available in capsules of 15 and 30 mg.

The effect increases during the first 4 days of administration, at a maximum a decrease in the synthesis of hydrochloric acid is achieved by 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, it should be taken 2 times a day. If antacids are prescribed at the same time, it is better to take them separately with Lancid, as they prevent 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;

Flaws

• prohibited during pregnancy.

Dexilant

Rating: 4.4

The active ingredient is dexlansoprazole.

On the one hand, this product is based on a relatively new active ingredient with high biological activity. On the other hand, until the patent expires and generics appear, the original manufacturer remains a monopolist, and the price of the 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 form of release. The seemingly ordinary capsules contain several types of granules that dissolve in the intestines depending on the pH of the environment. That is, after administration, not all of the active substance is released at once. and different granules dissolve at different times as the bolus moves. Due to this, the effect occurs 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: 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 for prolonged effect.

Flaws

• high price.

Efficacy and safety of proton pump inhibitors: searching for a middle ground

The annual international congress of the Scientific Society of Gastroenterologists of Russia celebrated its tenth anniversary in March 2010. It took place from March 2 to 5 at the Central House of Scientists. The congress was attended by academicians of the Russian Academy of Medical Sciences, corresponding members of the Russian Academy of Medical Sciences, doctors and candidates of medical sciences, students, and representatives of foreign scientific organizations. As part of the congress, on March 4, 2010, a symposium was held on the effectiveness and safety of the use of proton pump inhibitors, in particular, the use of the drug Zypantol® was discussed. Presentations were made by I.V. Mayev, professor, head. Department of Propaedeutics of Internal Diseases and Gastroenterology of Moscow State Medical University; Associate Professor Yu.A. Curly, Ph.D.; A.A. Masharova, Doctor of Medical Sciences

Presidium of the symposium: Director of the Central Research Institute of Gastroenterology, President of the National Research Institute of Gastroenterology, prof. L.B. Lazebnik; prof. G.Ya. Schwartz

I.V. Mayev, professor, head. Department of Propaedeutics of Internal Diseases and Gastroenterology MGMSU

Figure 1. Duration of acid-lowering effect after a single dose of the drug

Table 1. PPI drug-drug interactions

Yu.A. Kucheryavyi, Associate Professor, Department of Propaedeutics of Internal Diseases and Gastroenterology, Moscow State Medical University, Ph.D.

Figure 2. Efficiency of eradication therapy

A.A. Masharova, senior researcher at the Central Research Institute of Gastroenterology, MD.

When might proton pump inhibitors be ineffective?

Currently, the problem of the clinical use of PPIs as the most powerful antisecretory drugs in the treatment of acid-related diseases is widely discussed. Usually they dwell on issues of their effectiveness and features of clinical use. The issues of low effectiveness of proton pump inhibitors - how often it occurs and what reasons it can be caused by - are not so often covered at various events. Clinical effectiveness or ineffectiveness or low effectiveness can be considered depending on how quickly and well the symptoms of acid-related diseases are corrected. You can approach this issue from the point of view of clinical assessment (persistence of symptoms), you can - from the point of view of endoscopic assessment (lack of healing of ulcers and erosions in the esophagus, stomach, duodenum), you can from the point of view of pH-metry analysis (lack of increase in pH in in the stomach above 3, in the esophagus - above 4 on the 4-5th day of administration in patients with initial hyper- or normacidity).

It would be more correct to comprehensively evaluate all these components in order to talk about low, high, average effectiveness of certain inhibitors. There are studies that indicate that if we take as the main criterion of effectiveness the dynamics of relief of symptoms of acid-related diseases, in particular, heartburn as the most commonly used criterion, then approximately one third of patients with gastroesophageal reflux disease against the background of standard courses of treatment with a proton pump inhibitor demonstrates the low effectiveness of these drugs.

Studies have also been conducted that show: despite the fact that the effectiveness of treatment of the classical model of acid-dependent disease with proton pump inhibitors is relatively better than with the use of H2 histamine receptor blockers (H2-H2), however, about 42% of patients showed no significant improvement symptoms.

Patients receiving treatment with proton pump inhibitors are often forced, due to low effectiveness, to turn to the use of other medications in order to additionally relieve symptoms. In 11% of cases, H2-HB is additionally used. In 37% of cases, according to a study by Crawley (Crawley et al., 2000, PUNS), patients are forced to take antacids in order to relieve heartburn. Of course, all this indicates a bleak prospect for monotherapy with proton pump inhibitors in all cases of acid-related diseases.

What is the reason for this inefficiency? Of course, this important question does not have a clear answer today. Recent studies that were presented at international gastroenterological symposiums cite several reasons: it may be due to the wrong choice of drug, the wrong dosage, or a violation of the dosage regimen. But, apparently, this is not the only reason for all cases of low efficiency.

In recent years, the factors influencing the effectiveness of the antisecretory action of proton pump inhibitors have been studied quite well. They can be divided into absolute and relative. Absolute ones include genetically determined (CYP2C19 polymorphism); clinically determined (concurrent use of aspirin, nonsteroidal anti-inflammatory drugs; bile reflux; extraesophageal manifestations of gastroesophageal reflux disease (GERD): Zollinger-Ellison syndrome, error in diagnosis - GERD vs

eosinophilic esophagitis; functional heartburn). Relative factors are a violation of the strategy of determining one or another proton pump inhibitor as the most indicated for a particular clinical situation; compliance; choice of daily dosage and duration of treatment; age characteristics of patients (old age).

Compliance is of course important. The effectiveness of PPIs depends significantly on the sleep and work schedule the patient follows. It is necessary to limit the consumption of fatty foods; stopping drinking alcohol, smoking, drinking coffee and foods that stimulate the synthesis of hydrochloric acid; fractional meals; weight loss.

Yet the majority of patients are patients who need to be prescribed proton pump inhibitors. Which proton pump inhibitors are more reliably effective for GERD?

All currently existing inhibitors can be divided into four groups. These are the omeprazole group, the lansoprazole group, the rabeprazole group, and the pantoprazole group. Pantoprazole has the longest effect: inhibition of hydrochloric acid secretion for up to 46 hours (Figure 1).

Benefits of pantoprazole (Zypantol®):

• long-lasting effect, allowing you to take the drug once a day;
• dosage form: tablet;
• low affinity for the cytochrome P450 system provides the lowest level of drug interactions among PPIs;
• high level of efficiency and safety.

In addition, pantoprazole has the highest pH selectivity among PPIs, resulting in better tolerability. A widely known fact is the high safety profile of pantoprazole. Unlike other PPIs, pantoprazole has virtually no effect on the pharmacokinetics of other drugs metabolized in the liver by the cytochrome P450 system. Numerous studies have shown that pantoprazole does not affect the metabolism of clopidogrel, glibenclamide, nifedipine, diazem, diclofenac, carbamazepine, warfarin, theophylline and other widely used drugs (Table 1).

This allows us to consider pantoprazole (Zypantol®) the safest PPI.

How to increase the effectiveness of antisecretory therapy? Important:

• correct diagnosis;
• the correct choice of PPI – the maximum predicted effect in all patients, regardless of the type of metabolism;
• compliance (including ease of taking the drug, absence of drug-drug interactions);
• taking into account the possibility of duodenogastroesophageal reflux - expanding therapy in cases resistant to PPI monotherapy (ursodeoxycholic acid drugs, prokinetics, antacids and adsorbents).

Comparative effectiveness of triple first-line anti-Helicobacter therapy using Pantoprazole and Omeprazole

One of the most important problems at present remains the treatment of peptic ulcer with first-line therapy and the continuing decline in its effectiveness, which is partly determined, of course, by the growing resistance of
H. pylori
to standard drugs - antibiotic eradication regimens: clarithromycin and metronidazole. But in a fairly large number of studies, which is increasing from year to year, another potential possibility of reducing effectiveness is noted - this is the insufficient acid-suppressive effect of basic anti-Helicobacter drugs. And that is why there is a general trend that can be seen both in the global pharmacological market and in our country - the prescription of more modern proton pump inhibitors and the study of new drugs in large studies.

New studies show a trend towards increasing the daily dose of proton pump inhibitors. And to some extent, the effectiveness of therapy may depend on the choice of a more convenient and safe proton pump inhibitor. Of course, compliance is very important, because some patients, unfortunately, sometimes forget to take medications, and these omissions can have a certain significance and affect the unconditional effectiveness of therapy.

As is known, all proton pump inhibitors are substituted benzimidazoles, differing in the radicals in the pyridine and benzimidazole rings. All of them accumulate in the acidic environment of the secretory tubules of the parietal cell near the target - the proton pump. They undergo a number of changes: protonation, transformation into an active substance - a sulfonamide, which irreversibly blocks the covalent bond with cysteines of the H+/K+-ATphase. PPIs provide active, powerful and long-lasting suppression of acid production, regardless of the nature of the stimulating factor. The specific effect of all proton pump inhibitors is fairly high safety.

What is the reason for selecting pantoprazole (Zypantol®) as the test agent? This is a more modern drug, synthesized after omeprazole and lansoprazole. Synthesized in 1994 in Germany. Recently it has proven itself well in clinical studies. It is, like all inhibitors available on the Russian market, an irreversible inhibitor and is perfectly soluble in water. It has some advantages: rapid absorption from the gastrointestinal tract, which is fundamentally important; absorption does not depend on food intake, that is, the drug can be taken before meals, during or even after if the patient has forgotten to do so, and the effectiveness of the drug does not suffer - this is the most important advantage of pantoprazole (Zipantol®).

Pharmacokinetics of pantoprazole:

• quickly absorbed from the gastrointestinal tract;
• bioavailability is about 77%, not related to food intake;
• the maximum plasma concentration of 2–3 mcg/ml is achieved after 2.5 hours and does not change with repeated doses;
• the metabolism of pantoprazole (Zypantol®) occurs mainly in the liver;
• excreted primarily by the kidneys (about 80%) in the form of metabolites;
• The half-life is about an hour.

Work was carried out on the use of pantoprazole (Zipantol®) in triple regimens of first-line eradication therapy. A study based on a 7-day regimen, dated 1999-2000, shows 84-90%, or even more, eradication efficiency in standard first-line therapy. The use (2009) of 14-day regimens gives more than 80% eradication.

The purpose of the work was a comparative assessment of the effectiveness of eradication therapy for H. pylori

in patients with duodenal ulcer (PU) when using pantoprazole (Zipantol®) or generic omeprazole in a triple eradication regimen.
The study included 105 patients with duodenal ulcer aged 18 to 60 years. Criteria for inclusion in the study: the presence of one or more duodenal ulcers (regardless of size) according to endoscopy; confirmed presence of H. pylori
; signed informed consent to participate in the study. Exclusion criteria from the study: complications of peptic ulcer; concomitant gastroesophageal reflux disease (GERD); previously performed first-line eradication therapy; taking any antibiotics within 1 month before the start of the current study; taking macrolides for 1 year before the start of the study; surgical interventions on the esophagus, stomach or duodenum; severe diseases of various organs and systems (heart, kidney, liver, respiratory failure); known hypersensitivity to drugs of the groups used; concomitant use of aspirin or non-steroidal anti-inflammatory drugs (NSAIDs); pregnancy or lactation; mental disorders, alcohol abuse.

The patients were divided into two groups.

• Group I (PAC): 35 patients who were prescribed pantoprazole (Zipantol®) - 40 mg 2 times a day; amoxicillin – 1000 mg 2 times a day; Clarithromycin (Clarexide) – 500 mg 2 times a day, course – 7 days.
• Group II (OAC): 70 patients who were prescribed omeprazole - 20 mg 2 times a day; amoxicillin – 1000 mg 2 times a day; Clarithromycin (Clarexide) – 500 mg 2 times a day, course – 7 days.

After completing the one-week course of therapy, it was allowed to take antacids if pain and/or dyspeptic syndromes persisted.

The effectiveness analysis was carried out by two methods: histobacterioscopic with Giemsa staining and a rapid urease test. Eradication was considered achieved if the results of both methods used were negative. Compliance was 95.2% (100 people out of 105). 4 patients from group II and 1 patient from group I dropped out of the study. During treatment, side effects of the drugs (diarrhea) were noted, requiring discontinuation of the drug.

In the group of patients taking pantoprazole (Zypantol®) as a basic drug, 29 out of 35 patients (82.9%) achieved eradication of H .
pylori
(Figure 2). Thus, the level of effectiveness of anti-Helicobacter therapy in 80% of cases, recommended by the III Maastricht Agreement and the American College of Gastroenterologists as the minimum level, is exceeded. In the group of patients taking another PPI - omeprazole, the eradication rate was significantly and significantly lower than when using pantoprazole (Zipantol®) (eradication was achieved in 47 patients out of 70, which is 67.1%).

conclusions

• The effectiveness of eradication therapy for H. pylori in patients with duodenal ulcer when using pantoprazole (Zypantol®) is significantly higher (82.9% versus 67.1%) than when using generic omeprazole in the first- line triple eradication therapy regimen, and fully complies with modern requirements.
• When carrying out eradication therapy for H. pylori in patients with ulcer disease, the use of pantoprazole (Zipantol®) can be recommended as a basic PPI due to its greater effectiveness and safety compared to generic omeprazole.

Gastroesophageal reflux disease in the elderly: features of the use of proton pump inhibitors

Gastroesophageal reflux disease (GERD) in older people has features in its course and treatment. I would like to present the results of my doctoral work.

In the elderly, two main types of course or variants of gastroesophageal reflux disease can be distinguished, determined by the duration of GERD symptoms. The first type can be called “young”: the disease is detected at a young age, develops evolutionarily and proceeds more favorably (endoscopically negative form and/or non-erosive reflux esophagitis is more common). The second type - the disease occurs in old age, is characterized by a higher frequency of erosive and ulcerative reflux esophagitis, which is observed more often against the background of a hiatal hernia, with less expression of acidic and more alkaline gastroesophageal resources. Next, we analyzed the relationship between the number of comorbidities in the elderly and the stage of GERD. It turned out that in patients of older age groups, with the increase in concomitant diseases, the severity of reflux esophagitis also increases. We examined in great detail whether this depended on the concomitant pathology itself or drug interactions, and we took all this into account in our analysis.

The structure of concomitant diseases in our inpatients: if in young people the combination of GERD diseases with diseases of the cholecystopancreatoduodenal region: cholecystitis, pancreatitis predominates, then in elderly patients it is a predominant combination of diseases of the cardiovascular system: coronary artery disease, arterial hypertension.

After conducting a series of very serious statistical studies, we came to the conclusion that in elderly patients with GERD, the factors influencing the severity of reflux esophagitis are the following: being male (reflux esophagitis is more severe in men), a short history of the disease, the presence of a hernia esophageal segment of the diaphragm, taking anti-inflammatory drugs, drinking alcohol, smoking, the presence of coronary heart disease, as well as multimorbidity.

We analyzed the effectiveness of 3 years of therapy. All patients were taking proton pump inhibitors. After 8 weeks of observation, it was found that the frequency of endoscopic remissions in young patients was higher. And when we changed the timing of therapy, after 12 weeks we saw that in fact there were no differences in the onset of the clinical and endoscopic picture. If in patients under 60 years of age clinical-endoscopic remission is actually at the same level, then in elderly patients there was a tendency to increase, that is, lengthening the duration of therapy with proton pump inhibitors increases and increases the number of occurrences of clinical-endoscopic remission in elderly patients. We concluded that in young patients we can use the usual dose of proton pump inhibitors, and in those who do not experience an increase in effectiveness, it needs to be increased, whereas in older patients, proton pump inhibitors can be left at the usual doses, but the duration of therapy needs to be increase. It is quite obvious that the reactivity of the mucous membrane in the elderly is reduced, so we came to this conclusion.

We did not observe any health problems in elderly patients, although the connection between PPI therapy and an increase in intestinal infections, papillomas, osteoporosis, etc. is now widely discussed. There were no catastrophic changes in our patients: everything was stable. And if any problems were observed (food poisoning), then there was always a connection: let’s say a person ate a pie on the street in the summer. This was not associated with proton pump inhibitor use.

As for the use of the drug Zipantol®, we found that by the seventh day of drug therapy (40 mg/day), its effectiveness increases. This is a very good indicator.

When treating elderly patients, the safety spectrum of the drug is very important. Pantoprazole (Zypantol®) has no effect on the metabolism of digoxin.

Elderly patients with heart failure often suffer from gastroesophageal peptic ulcer disease; these diseases aggravate each other, and it is very important that pantoprazole (Zipantol®) does not affect this cardiac glycoside. Pantoprazole (Zypantol®) also does not affect the metabolism of nifedipine.

We know that in elderly patients hypertension is very often treated with nifedipine drugs, and the absence of drug interactions with nifedipine makes pantoprazole (Zipantol®) truly the drug of choice in the treatment of elderly patients.

Experts from the American Society of Cardiology, the American Society of Gastroenterology, and the American Heart Association have developed a consensus on optimizing long-term antiplatelet therapy in light of the increased risk of gastrointestinal complications with these drugs. At the same time, the authors emphasize that a large number of these complications are caused not so much by the influence of antiplatelet agents, but by the summation of adverse side effects if antiplatelet drugs are taken together with non-steroidal anti-inflammatory drugs, which is the lot of many elderly patients.

Pantoprazole (Zypantol®) has a less pronounced effect on the pharmacokinetic activity of clopidogrel than omeprazole. Dual antiplatelet therapy with clopidogrel and aspirin increases the risk of gastrointestinal bleeding, so it is logical to combine it with proton pump inhibitors (PPIs) to protect the gastric and intestinal mucosa. However, the most commonly used PPI, omeprazole, has been shown to reduce the antiplatelet activity of clopidogrel.

The results obtained are also due to the fact that pantoprazole (Zypantol®) inhibits the CYP2C19 enzyme, which plays a key role in the metabolism of clopidogrel, to a lesser extent.

Thus, pantoprazole (Zipantol®) can be used as the drug of choice in the treatment of GERD, being an effective and safest drug when long-term antisecretory therapy is necessary in elderly patients.

The best combination drugs

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

Pilobact

Rating: 4.3

Strictly speaking. This is not one 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 packaged in strips labeled “morning” or “evening.” The contents of the corresponding strip should be taken during or immediately after a meal, as is clear from the description - in the morning and in the evening. Tablets or capsules cannot be divided, chewed or otherwise crushed.

Contraindicated for:

1. intolerance to components,
2. alcoholism (cannot be combined with ethyl alcohol),
3. liver or kidney failure,
4. impaired bone marrow hematopoiesis,
5. children, pregnant and lactating women.

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

Advantages

• a full range of drugs to eliminate Helicobacter.

Flaws

• many contraindications and side effects.
• high price.

Omez DSR

Rating: 4.2

A combination of 20 mg of omeprazole and 30 mg of domperidone, a regulator of gastrointestinal motility. Minimizes the possible reflux of bile, restoring normal peristalsis of the esophagus and stomach, reduces the acidity of gastric juice. thus reducing damage to the esophagus and promoting its healing. In addition, the drug can be used to reduce nausea and vomiting caused by exacerbation of gastritis and gastric ulcer.

Take 1 time per day half an hour before meals.

Contraindicated for:

1. 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);
2. gastrointestinal bleeding, perforation, intestinal obstruction;
3. moderate to severe liver failure,
4. pregnant and lactating women,
5. children under 18 years of age.

Advantages

• normalizes motility of the esophagus, stomach, intestines,

Flaws

• a wide range of contraindications,
• Possible adverse events.