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Pantoprazole in the treatment of acid-dependent diseases

E.P. Yakovenko, A.V. Yakovenko, Yu.V. Illarionova, N.A. Agafonova, S.A. Lavrentiev, A.N. Ivanov,
A.S. Pryanishnikova, L.P. Krasnolobova
Department of Gastroenterology, Faculty of Postgraduate Medical Education, State Budget Educational Institution of Higher Professional Education
"Russian National Research Medical University named after N.I. Pirogov"
Ministry of Health and Social Development of Russia, Moscow

The proton pump inhibitor (PPI) pantoprazole blocks basal and stimulated secretion of hydrochloric acid in the stomach by inhibiting the enzyme H+/K+-ATPase. According to the literature and the results of our own studies, the antisecretory effect of pantoprazole is comparable to that of other PPIs. The main distinguishing properties of pantoprazole is the lack of interaction with concomitantly taken medicines, the drug does not accumulate in the body, when it is taken, dose adjustment is not required for elderly patients with renal and hepatic insufficiency, its effect does not depend on the genetically determined metabolic rate in the liver. Modern schemes of therapy using pantoprazole for gastroesophageal reflux disease, infections are presented. Helicobacter pylori, gastropathy associated with the use of non-steroidal anti-inflammatory drugs, for the prevention and treatment of stress ulcers and gastroduodenal bleeding.

Keywords: acid-dependent diseases, proton pump inhibitors, pantoprazole, drug interactions

Pantoprazole, proton pump inhibitor (PPI), blocks basal and stimulated secretion of hydrochloric acid in the stomach by inhibiting the H+/K+-ATPase. According to the literature data and own research results, the antisecretory effect of pantoprazole is comparable with that of other PPIs. The main distinguishing features of pantoprazole are the lack of interaction with simultaneously taken drugs, the drug does not accumulate in the body, dose adjustment for elderly patients with the presence of renal and hepatic failure is not required, and its effect does not depend on the genetically determined metabolic rate in the liver. Modern medical regimens with pantoprazole for the treatment of gastroesophageal reflux disease, Helicobacter pylori infection, NSAID-associated gastropathy, and for the prevention and treatment of stress ulcers and gastroduodenal bleeding are presented.

key words: acid-related diseases, proton pump inhibitors, pantoprazole, drug-drug interactions

Acid-dependent diseases (ADD), in the pathogenesis of which hydrochloric acid plays a significant role, are the most common in the practice of a gastroenterologist and occur in more than 30% of the Russian population. The main ones are gastroesophageal reflux disease (GERD), peptic ulcers of the stomach and duodenum, gastropathy caused by the use of non-steroidal anti-inflammatory drugs (NSAID-dependent gastropathy), non-ulcer dyspepsia, chronic gastritis, pancreatitis. Currently, it is difficult to imagine CCZ therapy without the use of proton pump inhibitors (PPIs), which include omeprazole, esomeprazole, pantoprazole, lansoprazole, and rabeprazole.

All PPIs are benzimidazole derivatives and differ in the radicals in the pyridine and benzimidazole rings, as well as in some pharmacokinetic and pharmacodynamic properties. At the same time, all PPIs have a similar mechanism of action - the ability to inhibit basal and stimulated secretion of hydrochloric acid in the stomach by inhibiting the enzyme H + / K + -ATPase (or proton pump), localized on the surface of the parietal cell facing the lumen of the gastric glands. H+/K+-ATPase is a key enzyme in the transport system involved in the transfer of hydrogen ions from the cytoplasm of the parietal cell to the lumen of the secretory tubules and their exchange for potassium ions from the extracellular space. Subsequently, C1 ions along the concentration gradient also enter the lumen of the secretory tubules, where hydrochloric acid is formed. PPIs, which are weak bases, accumulate in the acidic environment of the secretory tubules near the proton pump. Subsequently, the pyridine ring atom of the PPI molecule is protonated and converted into the active substance, sulfenamide, which covalently binds to one or more cysteine ​​residues on the catalytic (a) subunit of the proton pump, which leads to its irreversible inhibition and cessation of hydrochloric acid synthesis. As a result, PPIs cause a pronounced inhibition of hydrochloric acid secretion, which lasts for a longer period than the time of their circulation in the blood plasma, and the synthesis of new proton pumps is required to restore acid production. PPIs differ in the location and number of bonds with cysteine ​​on the catalytic α-subunit of the proton pump. In this case, only pantoprazole specifically binds to the site, including the fifth and sixth transmembrane segments of the α-subunit of the proton pump, as well as to cysteine ​​822, which is located deep in the transport domain of the proton pump, which makes it inaccessible to glutathione and dithiothreitol, which can eliminate the inhibition of the proton pump. pumps. In this regard, pantoprazole has a longer duration of action than other PPIs.

Pantoprazole is characterized by high and stable bioavailability (77%), which contributes to the achievement of the maximum acid-suppressive effect starting from the first dose of the drug, as well as a constant linear predictable pharmacokinetics, which allows maintaining the maximum level of depression of acid production throughout the entire time of taking the drug. At the same time, more optimal inhibition of hydrochloric acid secretion is achieved when taking 40 mg of the drug in the morning than when taking the same dose in the evening. According to the results of daily monitoring of the intragastric pH level, the acid-suppressive effect of pantoprazole at a dose of 40 mg was more pronounced than that of omeprazole at a dose of 20 mg, similar to that when taking lansoprazole 30 mg / day and slightly lower than when taking a double dose (40 mg) of esomeprazole. At the same time, the antisecretory effect of pantoprazole did not differ significantly when administered enterally or intravenously at a dose of 40 mg.

We conducted a comparative study of the acid-suppressive effect of equivalent doses of the original drugs esomeprazole (Nexium, Astra Zeneca) - 20 mg, rabeprazole (Pariet, Janssen-Cilag) - 20 mg and pantoprazole (Controloc, Nycomed) - 40 mg when taken enterally at 8 am patients with duodenal ulcer. The results of the study are presented in the table.

Table. Comparative evaluation of the acid-suppressive effect of esomeprazole, rabeprazole and pantoprazole

Thus, the acid-suppressive effect of pantoprazole (Controloc) did not differ significantly from other original PPIs - esomeprazole and rabeprazole.

In clinical terms, in addition to the acid-suppressive effect, extremely significant properties that are taken into account when choosing PPIs are the low level of interaction with other drugs, the absence of a cumulative effect with long-term use, and the presence of a dosage form of the drug for parenteral administration. The latter is necessary for the prevention and treatment of stress erosive and ulcerative lesions and bleeding from the upper gastrointestinal tract, the prevention of acid aspiration syndrome during anesthesia, as well as for the treatment of patients for whom the enteral route of administration of the drug is unacceptable (nausea, vomiting, diarrhea, esophageal stenosis). , pylorus, swallowing disorders, etc.).

It is known that PPIs, like most other drugs, are metabolized in the liver with the participation of enzymes of the cytochrome P450 system, in particular the isoenzymes CYP2C19 and CYP3A4, and therefore they can interact, changing the pharmacodynamic and pharmacokinetic effects of drugs taken simultaneously. It should be noted that pantoprazole, compared with other PPIs, has a lower affinity for these isoenzymes, therefore, it has the narrowest spectrum of drug interactions. A number of pharmacological and clinical studies have shown that pantoprazole (Controloc) does not interact with antacids, antipyrine, caffeine, clopidogrel, oral contraceptives, ethanol, glibeclamide, levothyroxine, metoprolol, piroxicam, theophylline, amoxicillin, clarithromycin, diclofenac, naproxen, diazepam, carbame , digoxin, nifedepine, warfarin, cyclosporine, tacrolimus, etc., which allows it to be used in the treatment and prevention of erosive and ulcerative lesions of the stomach and duodenum in patients receiving several drugs simultaneously. Data on drug interactions have proved to be extremely important in the management of cardiac patients receiving long-term antiplatelet agents, anticoagulants and other drugs in combination with PPIs. In particular, it has been shown that among patients who have had myocardial infarction, the simultaneous use of clopidogrel and any PPI, except pantoprazole, significantly increases the incidence of recurrent myocardial infarction in the early stages of observation.

Pantoprazole (Controloc), unlike omeprazole and esomeprazole, does not accumulate in the body after repeated doses. So, after intravenous administration of pantoprazole at a dose of 30 mg / day for 5 days, the pharmacokinetics were comparable to those obtained after intravenous administration of the first dose. In pharmacokinetic studies of pantoprazole when administered orally at doses of 10 to 80 mg and when administered intravenously at a dose of 240 mg, its content in the blood serum was linear. These properties of pantoprazole differ significantly from those found with intravenous administration of omeprazole, with increasing doses of which in the same range, the area under the concentration-time curve (AUC) changes disproportionately, and the half-life increases after a single intravenous injection. In addition, it turned out that the differences in the pharmacokinetics of pantoprazole in individuals with slow and accelerated metabolism, which is assessed by the genetically determined activity of the 5-mephenytoin-4 "-hydroxylase isoenzyme, do not have any clinical significance. An important property of pantoprazole (Controloc), which makes in certain situations, it is the drug of choice in the therapy of SCZ, the absence of the need for dose adjustment for elderly patients, as well as with renal and hepatic insufficiency.

At present, a large clinical experience has been accumulated in the use of pantoprazole in the treatment of SCZ. There are enough publications on the evaluation of the effectiveness of classical triple anti-Helicobacter therapy, which included pantoprazole at a dose of 40 mg 2 times a day in combination with two drugs from the following twice a day: amoxicillin 1 g, clarithromycin 500 mg, metronidazole 400 or 500 mg within 7-14 days. The frequency of Helicobacter pylori (HP) eradication using triple therapy, which included pantoprazole, ranged from 71-93.8% in the ITT (intention-to-treat) analysis (calculated on all patients included in therapy according to the study protocol) and 86 -100% for PP (reg-rotocol) analysis (based on patients who completed treatment according to the study protocol). At the same time, a group of authors showed that when using triple therapy, which included pantoprazole, the frequency of eradication was more effective than the therapy regimen, which included omeprazole. At the same time, it should be noted that the frequency of H. pylori eradication is affected not so much by the choice of PPI, but by the resistance of the pathogen to the antibacterial component of the triple therapy regimen used. In addition, it should be borne in mind that the effectiveness of anti-Helicobacter therapy varies with different clinical manifestations RR infection and strains of H. pylori. The results of a number of studies indicate that H. pylori strains positive for the cytokine-associated gene (CagA), more often detected in patients with duodenal ulcer, are easier to eradicate than CagA-negative, which are more often found in patients with non-ulcer dyspepsia.

The results of numerous studies have confirmed the effectiveness of pantoprazole in the treatment and maintenance of remission of erosive and non-erosive GERD. So, in the course of randomized double-blind or open studies, it was found that in the treatment of erosive GERD (grades II and III according to Savary-Miller), the effectiveness of pantoprazole at a dose of 40 mg / day was comparable to that of omeprazole at doses of 20 and 40 mg / day, lansoprazole 30 mg/day and esomeprazole 40 mg/day was significantly superior to ranitidine 300 mg/day or famotidine 40 mg/day. Similar results were obtained with the use of pantoprazole in the prevention of GERD relapses. Thus, it was shown that pantoprazole at a dose of 20 or 40 mg / day for 12-24 months prevented the development of relapses of reflux esophagitis in the majority of patients in whom healing of ulcers and erosions of the mucosa of the esophagus was achieved against the background of previous therapy. At the same time, the effectiveness of 20 and 40 mg of pantoprazole in prophylactic therapy did not differ significantly.

Pantoprazole has found wide application in the treatment and prevention of NSAID-associated gastropathy. So, in a randomized comparative study D. Olteanu et al. it was found that after 4 weeks of therapy, scarring of NSAID-associated ulcers was observed among 87% of patients taking pantoprazole at a dose of 40 mg / day and among 75% of those taking omeprazole at a dose of 20 mg / day. After 8 weeks, the ulcers healed in all patients treated with the above PPIs. The high efficacy of pantoprazole at a dose of 40 mg / day in the prevention of NSAID-associated gastropathy was confirmed by patients who had achieved scarring of pre-existing ulcers and at the time of the start of prophylactic therapy, endoscopic examination revealed a normal or hyperemic mucosa with the presence of less than 5 focal petechiae in the upper sections of the gastrointestinal tract. In addition, there was at least one risk factor for the development of erosive and ulcerative lesions, which included a history of gastritis or peptic ulcer disease, the use of one or more NSAIDs, the use of corticosteroids or anticoagulants, elderly age and etc. .

Parenteral administration of PPIs is an essential component of therapy aimed at preventing rebleeding from gastric and duodenal ulcers after endoscopic hemostasis. Numerous studies have found that intravenous administration pantoprazole significantly reduced rebleeding rates at 48 and 72 hours, transfusion episodes at 72 hours, and mortality at 14 days.

An analysis of the literature data and the results of our own studies allow us to present the optimal regimens for the treatment of major CVDs using pantoprazole.

Non-erosive GERD. Pantoprazole is prescribed 20 mg 1 time per day (30 minutes before breakfast) for 4-8 weeks, followed by on-demand administration.

Erosive GERD. Pantoprazole is taken 40 mg 1 time per day (30 minutes before breakfast) for 4-8 weeks with a transition to maintenance therapy, which involves taking the drug daily at a dose of 20 mg / day for 6-12 months and then taking it "on demand" at a dose of 20 mg / day.

Current H. pylori eradication regimens include PPI +2 antibiotics, in most cases in combination with a bismuth preparation. Pantoprazole 40 mg twice daily can be used as a PPI. Below are several schemes, in the appointment of which the eradication of H. pylori exceeds 80%.

The currently proposed first-line regimens are usually four-component.

Empiric Therapy: pantoprazole (Controloc) 40 mg + amoxicillin 1000 mg + clarithromycin 500 mg + tinidazole 500 mg or metronidazole 500 mg. All drugs are taken twice a day for 10-14 days.

Sequential Therapy: pantoprazole (Controloc) 40 mg + amoxicillin 1000 mg twice a day for 5-7 days, then pantoprazole (Controloc) 40 mg + clarithromycin 500 mg + tinidazole 500 mg or metronidazole 500 mg twice a day for 5-7 days . The total duration of therapy is 10-14 days.

Bismuth Quad Therapy: pantoprazole 40 mg 2 times a day + bismuth subcitrate 240 mg + tetracycline hydrochloride 500 mg (both 4 times a day) + metronidazole 500 mg or tinidazole 500 mg 3 times a day for 10, but preferably 14 days. Another regimen: pantoprazole (Controloc) 40 mg + amoxicillin 1000 mg + clarithromycin 500 mg + bismuth subcitrate 240 mg. All drugs are taken twice a day for 10-14 days.

If the above methods of eradication therapy are ineffective, reserve regimens are offered: PPI + levofloxacin 500 mg 1 time per day + amoxicillin 1000 mg 2 times a day for 14 days or PPI + rifabutin 150 mg + amoxicillin 1000 mg 2 times a day for 14 days.

At peptic ulcer associated with H. pylori, the duration of taking pantoprazole 40 mg / day is 2-4 weeks for duodenal ulcers, and 4-8 weeks for gastric ulcers.

To prevent the development of stress ulcers, pantoprazole (Controloc) is prescribed intravenously at a dose of 40 mg every 12 hours until the patient's condition stabilizes and is transferred to enteral nutrition. Due to the fact that acid-associated lesions of the gastric mucosa occur within 24 hours from the onset of a stressful situation, parenteral administration of Controloc should begin immediately after the patient enters the intensive care unit, and during planned operations for the prevention of acid-aspiration syndrome - before or during anesthesia.

As the condition stabilizes, the parenteral administration of the drug is stopped and the patient is transferred to the enteral administration of pantoprazole according to the "last injection + first tablet of the drug" scheme. Due to the different pharmacokinetic and pharmacodynamic properties of PPIs (for example, the maximum acid-suppressive effect is achieved when using pantoprazole from the first dose, and omeprazole - on the 7th day), it is necessary to use pantoprazole in oral therapy.

On average, scarring of stressful erosive and ulcerative lesions requires a four-week course of PPI therapy.

Thus, pantoprazole (Controloc) is currently one of the effective PPIs used in the treatment of CVD. Due to the fact that differences between PPIs in terms of how they clinical effectiveness in equivalent doses, and side effects, apparently small an important factor that influences the choice of drug is its individual ability to enter into drug interactions. This is of particular importance for elderly people who take many medications at the same time, as well as for patients using drugs with a narrow therapeutic range. In such cases, preference should be given to pantoprazole, for which the likelihood of developing drug interactions is the minimum. In addition, the presence of this drug dosage forms for both enteral and intravenous use allows you to expand the indications for its use and ensures a safe transition from parenteral to oral administration.

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I want to quickly take an effective medicine.

But Omeprazole, how to take it to restore the function of the gastrointestinal tract and intestines, who is indicated and contraindicated, what side effects does it have and can it be replaced with other analogues? It is worth considering in more detail.

Release form composition and packaging

Omeprazole is a fairly well-known drug.

Produced by many Russian companies under the brands:

• akrikhin;
• teva;
• avva rus;
• astrafarm;
• sandoz;
• richter;
• promed;
• staff.

The drug acts on the enzyme in the stomach as part of hydrochloric acid, inhibits secretion, accelerates the exchange of hydrogen ions in the mucus of the epithelium, thereby blocking the production of hydrochloric acid production.

As a result, the level, secretion of digestive juice decreases.

Taking into account the intake of doses, the effectiveness of the drug is observed for one 1-1.5 days.

Release form of the drug- hard capsules (10, 20, 40 mg). Packing - cell, contour. Pack - cardboard or polymer cans (10, 20 mg).

Composed of:

• active ingredient - omeprazole;
• auxiliary elements: sodium lauryl sulfate, purified water, dye e129, glycerin, gelatin, nipagin, mannitol, sugar, titanium dioxide, talc, methacrylic acid.

Pharmacological action, pharmacokinetics

Omeprazole has an inhibitory and antiulcer effect, inhibits the activity of the enzyme adenosine triphosphate H + K.

The metabolite, when it enters an acidic environment, already after 4-5 minutes, begins to transform into sulfenamide, entering into active interaction with phosphates, blocking the phase.

This drug is a highly selective drug for conversion into an active metabolite in an acidic environment.

In relation to parietal cells, the drug is not absorbed, but quickly suppresses the secretion of hydrochloric acid irritants and the production of pepsin, leading to a decrease in the total volume of contents in the stomach.

Omeprazole in capsules with a thin shell contains microgranules, the release of which already 1 hour after application leads to the achievement of the maximum therapeutic effect. Preservation lasts up to 1 day.

A single dose of omeprazole is sufficient so that the suppression of the secretion of hydrochloric acid was carried out to the maximum for the whole day. Secretory activity will be restored after 5-6 days if you stop taking Omeprazole.

The pharmacokinetics of the drug is as follows:

• bioavailability - 40%, but an increase in people in old age is possible;
• absorption is high;
• lipophilicity - high at the time of entry into contact with albumin and glycoproteins (proteins) in blood plasma;
• the elimination period is 0.5 hours and a little more up to 3 hours for liver diseases.

Metabolism occurs in the liver cells in the form of 6 inactive metabolites. Up to 80% of the drug is excreted by the kidneys, up to 40% - by bile. The rate of elimination of the drug may be reduced in elderly people with chronic renal failure.

Indications for use

The main effect of the drug is the suppression of the synthesis of hydrochloric acid, the elimination of excessive secretion against the background of food intake.

Main indications:

With these diseases, there is an excessive production of gastric juice, which inevitably destroys the mucous membrane, forming erosion and ulcers.

Omeprazole in tablets is prescribed for any pathology of the gastrointestinal tract, which led to an increase in the production of gastric juice, an increase in the concentration of organic acids.

The drug contributes to:

• decrease in acidity in the stomach;
• suppression of Helicobacter pylori bacteria;
• improvement of general well-being;
• elimination of pain, dyspepsia.

The most common appointment is peptic ulcer against the background of increased acidity in the stomach. The use of omeprazole capsules will help with heartburn, although in cases of relapse it should be taken under the supervision of a doctor.

The effect on heartburn after taking the drug is observed after 3-4 days, and the primary relief - after 1 day.

Portability of Omeprazole is excellent. The risks of side effects are minimal.

Intravenous administration of the drug in injections is possible in the treatment of:

• reflux esophagitis;
• peptic ulcer and 12 duodenal ulcer.

Omeprazole eliminates dyspepsia well and can be used for a long time - up to 0.5 years. Doctors recommend taking the drug in case of discomfort after eating, alcohol poisoning to relieve pain, burning, and other discomfort.

Contraindications for use

The use of Omeprazole is excluded when:

• pancreatitis;
• individual intolerance;
• pregnancy, which can adversely affect the formation of the digestive tract in the baby, cause disorders.

It is forbidden to give the drug to children under 5 years of age with a body weight of not more than 20 kg due to difficulty swallowing capsules.

In some cases, it is possible to prescribe together with antibiotics during complex therapy by opening the capsules, mixing with liquid (yogurt, water).

The drug can be given to a child, but it is extremely important to keep the situation under control and it is better to consult a doctor first.

Side effects

Rarely, but omeprazole causes side effects

• insomnia;
• hallucinations;
• dizziness;
• muscle weakness;
• myalgia;
• increased sweating;
• itching on the skin up to anaphylactic shock.

With uncontrolled use, constipation, dry mouth, nausea, and vomiting may occur.

Instructions for use

The use of the drug is aimed at reducing the production of gastric juice secretion, therefore, in some cases, the use may become inappropriate.

Only on the basis of the diagnosis, general well-being and existing symptoms, the dosages prescribed by the attending physician, the course of application (before or after meals) will depend.

It is advisable to first consult with a gastroenterologist about the rules for using the drug.

For example, during an exacerbation, it is treated by taking 20 mg immediately before meals in the morning 1 time per day. The capsule must be swallowed whole with water.

Often a drug is prescribed for the prevention of stomach ulcers. To avoid possible exacerbations, the permissible dosage is 20 mg per day.

The main purpose of the drug is to neutralize unpleasant symptoms., normalize the production of hydrochloric acid. If, after the course of treatment, the problem does not go away, then it is possible to increase the dosage, but with the permission of the doctor.

The drug is often prescribed for heartburn, but it is permissible to use it only in an emergency and at a dose of no more than 10 mg per day, the duration of the treatment course is 2 weeks. It is important to understand that the drug can lead to a cumulative effect.

If taken without the permission of a doctor in order to get rid of heartburn, then the use should not be more than 5 days in a row. In the future, it is advisable to visit a doctor, undergo an examination to correct subsequent therapy.

Overdose

If you neglect the doctor's prescriptions, violate the rules for taking and dosing the drug, then there may be an intolerance to the components of the drug and cases of overdose with side effects:

• muscle weakness;
• myalgia;
• headache;
• rash, redness, itching on the skin;
• failure of liver function;
• depression;
• stress;
• increased sweating;
• deviations in the composition of the blood;
• atrophic gastritis

If you take the drug in acceptable doses with an increased level of acidity, then an overdose is extremely rare.

Only when the dose is exceeded over 60 mg per day, drowsiness, fever throughout the body, confusion, tachycardia, dryness of the mucous membrane in the nose and mouth, difficulty breathing, visual impairment may occur.

Omeprazole is rapidly absorbed into the blood within 1 hour and dialysis is already becoming ineffective. Although, with confusion and poor health, of course, one cannot do without an urgent appeal to specialists.

Interaction with other drugs

Features of co-administration of Omeprazole with other drugs:

Alcohol compatibility

The proton pump inhibitor in the composition of Omeprazole contributes to the rapid suppression of the secretion of gastric juice, if you read the instructions for use, then the possible danger in combination with alcoholic beverages is not indicated.

This means that joint application is possible.

However, if you take an analogue of Nexium, then the manifestation of side effects is possible:

• diarrhea;
• depression;
• allergy;
• overexcitation;
• nausea, vomiting;
• possible development of hepatitis with excessive imbalance of liver function.

Omeprazole can adversely affect the liver. And if combined together with strong drinks, then there may be an excessive burden on the body, stress with regular long-term use of alcohol.

And, in particular, with the use of Omeprazole, fatty hepatosis is ensured and even doctors say this, and the patient may be completely unaware of the disease and only random examinations can confirm the diagnosis.

Use during pregnancy and lactation

Following the instructions for use, omeprazole is contraindicated in women during pregnancy, regardless of the trimester.

The main component of the drug quickly crosses the placenta, has a negative effect on the development and condition of the fetus, also during breastfeeding.

Despite the lack of studies, it is not recommended to take the drug.

Exclusively in case of acute vital necessity and only with the permission of the attending physician

Application in childhood

According to the instructions, the use of Omeprazole in children under 5 years of age is prohibited. Only if a tumor is detected in the pancreas is it possible to prescribe the drug, but taking into account the weight of the child and under the supervision of a specialist.

Application is possible only with a mass of more than 10 kg.

Indications:

• heartburn;
• reflux esophagitis;
• Zollinger-Ellison syndrome.

The use of omeprazole in children is indicated from the age of 4 for a comprehensive treatment course in the detection of peptic ulcer. Permissible doses - 5 mg per day with a weight of up to 10 kg, 10 mg - with a weight of up to 20 kg, 20 mg with a weight of over 20 kg.

The use of the drug is possible only in cases where the intended benefit is much higher than the possible risks from the therapy.

Use for liver and kidney dysfunction

If you take Omeprazole for diseases of the kidneys (liver), then the results of a blood test may be distorted, a decrease in the concentration of gastrin in the blood plasma.

Failure of the liver should be the reason for reducing the dose - 20 mg.

Application for the elderly

If in elderly patients there is a failure of liver function, then dose adjustment of omeprazole is not carried out. Pharmacokinetics will not change as dialysis is carried out in chronic kidney disease.

If there is a violation of liver function, then the dose should not be more than 20 mg per day.

special instructions

The reaction of the body may be inadequate to any substance, in particular the components of Omeprazole.

The drug should be used with caution in case of:

Possible side effects: bloating, upset stool, nausea, vomiting.

Vacation from pharmacies

The medicine is dispensed strictly according to the prescriptions of doctors.

Storage conditions and shelf life

Price

The approximate cost of Omeprazole in Russia starts from 28 rub. for package number 10 and from 50 rub. for packing No. 230. Lyophilisate price - from 235 rub.

Analogues

A number of analogues contain the same active substance and all of them are proton pump inhibitors. They may well replace Omeprazole, suppress the level of gastric secretion and the release of pepsin. These are inexpensive drugs, but give quick results.

Analogues from Russian manufacturers or close substitutes are distinguished by high popularity among patients:

1. Ultop with the active substance - Omeprazole as an antiulcer agent for inhibiting the activity of ATP-ase in the cells of the stomach, blocking the production of hydrochloric acid, the concentration of basal secretion. Indicated for use in gastric ulcer, Zollinger-Ellison syndrome, non-ulcer dyspepsia, gastroesophageal reflux. Price 148-337 rubles.
2. , as a means to eliminate disorders of the gastrointestinal tract, the active ingredient, a derivative of benzimidazole. The main purpose is the treatment of reflux disease, the elimination of unpleasant signs of heartburn, acid reflux, pain when swallowing. Price - 110-170 rubles for 30 capsules with a pack of 10.20 mg.
3. Ortanol with active omeprazole, an antiulcer inhibitor for the treatment of gastric ulcers, systemic mastocytosis, polyendocrine adenomatosis, uninfected duodenal ulcer. Price - 107-112 rub.(10 mg, 20 mg).
4. Omepradex, to suppress gastric secretion and block hydrochloric acid. It is indicated for gastroesophageal disease, hypersecretory condition, peptic ulcer of the stomach, non-ulcer dyspepsia. Price - 120-135 rub.
5. Gastrosol- anti-ulcer proton pump inhibitor with the active ingredient - omeprazole to reduce the level of basal, stimulated secretion regardless of the stimulus, blocking the production of hydrochloric acid. Price for 14 capsules - 80 rub., 28 capsules - 130 rub.
6. , antiulcer for the treatment of stomach ulcers, 12 duodenal ulcers. Perhaps the appointment in combination with antibiotics. Average price in Moscow - 110-180 rub.
7. Gasek from Switzerland to suppress the secretion of hydrochloric acid. Available in capsules, vials. Reduces acid production, is considered highly effective, versatile and affordable. Cost in Ukraine - 180 hryvnia.
8. omephez with the appointment of reflux esophagitis, polyendocrine adenomatosis, mastocytosis, systemic NSAID gastropathy, hypersecretory conditions. Active substitutes Omeprazole Shtpda, Omeprazole Akri. Price - 20-57 rub.
9. with active omeprazole. An antiulcer drug with a release form - a lyophilisate for the preparation of infusion solutions. Suppresses the secretion of hydrochloric acid, inhibits the proton pump of parietal cells in the stomach, reduces the production of secretion. Significant cost, within 1800 rub.
10. Omitox, proton pump to block the synthesis of hydrochloric acid. It treats peptic ulcer of the stomach and duodenum, restores secretory activity completely after 3-5 days. Price 87-92 rub.
11. Promez- active substance (omeprazole). Rapid absorption from the gastrointestinal tract is observed after 1 hour. Bioavailability - up to 40%, plasma protein binding - 90%. Indicated for use in reflux esophagitis, ulcers with Helicobacter pylori, erosive lesions of the duodenum. Price - 20-57 rub.
12. Crosacid- ATPase inhibitor to block the secretion of hydrochloric acid. Treats peptic ulcer caused by Helicobacter pylori, increases the sensitivity of bacteria to antibiotics. This is an antimicrobial agent with an appointment for stomach ulcers, Zollinger-Ellison syndrome, reflux esophagitis. Price - 98 rub.
13. to reduce the secretion of the gastric glands with the active substance - Rabeprazole, to suppress the secretion of basal secretion juice, regardless of the stimulus that caused it. Price - 330 rub .
14. - a hypoacid medication with the active ingredient - Pantoprazole (a derivative of benzimidazole) to block the hydrophilic secretion of hydrogen chloride in the stomach, to suppress the stimulated basal production of hydrochloric acid. Shown orally. Price - 120 rub.(20 mg), per pack of 14 180 rub.
15. Rabeprazole- antiulcer agent with complete absorption after 3 hours. They are prescribed for stomach ulcers, gastritis, relapses of peptic ulcers caused by Helicobacter pylori, gastroesophageal disease. Price in Moscow - 200 rub. for 20 mg.
16. De-nol- antiulcer, gastroprotective, antibacterial composition. Refers to the adsorbent. Promotes the formation of a protective film on the gastric mucosa, the formation of special compounds to cover damaged areas. It becomes a barrier to the mucosa, stimulates acid synthesis, reduces the activity of gastric pepsin, and has an antimicrobial effect. It is prescribed for chronic gastritis, gastroduodenitis, duodenal ulcer. Price - 570 rub. for 56 pieces, 250 rub. for 112 pcs.

Omez and Omeprazole - which is better?

The active substance of the drugs is the same. Omez is much more expensive, but according to user reviews, it is more effective, well eliminates the symptoms of acid-dependent diseases, perfectly penetrates the gastrointestinal mucosa, and is absorbed into the blood.

After 1 hour, the elimination of unpleasant symptoms in the stomach is observed.

Pantoprazole and Omeprazole - which is better?

Omeprazole perfectly treats diseases associated with increased production of gastric secretions. Pantoprazole, as an analogue, is more affordable. Although antisecretory activity, the therapeutic effect is more reduced, in particular in the treatment of peptic ulcers of the stomach, esophagitis.

If you choose between 2 drugs, then you should give preference to Omeprazole, since it can be used in combination with drugs: Clopidogrel, Citalopram.

Which is better - Nolpaza or Omeprazole?

The composition of the active substance is Rabeprazole, but the effectiveness when compared with Omeprazole is the same. According to patient reviews, Nolpaza is a safer drug, since it has the maximum number of side effects.

The use of omeprazole is effective in excess gastric juice in order to eliminate gastritis, heartburn to relieve unpleasant symptoms.

But with low acidity, it is unreasonable to use the drug, which can only lead to an aggravation of the course of the disease due to excessive suppression of the production of gastric juice.

Omeprazole is considered a gastroprotective drug, well eliminates the symptoms of heartburn. In other cases, it is unreasonable to apply. It may be worth giving preference to other effective and popular generic analogues.

The drug eliminates problems with the stomach, prevents the development of complications, the re-emergence of unpleasant symptoms.

This is a modern antisecretory remedy that allows you to quickly cope with the inflammatory course in the upper gastrointestinal tract, suppress hydrochloric acid or reduce its activation.

Omeprazole is an excellent level of the impact of Helicobacter pylori microorganisms on the gastrointestinal tract, leading to gastritis, peptic ulcer. The medicine perfectly improves well-being and reduces the likelihood of side effects later.

Only a specialist can adjust the therapy taking into account the severity of the pathology, the patient's condition. It is possible to increase the dosage, for example, when Zollinger-Ellison syndrome is detected, up to 60-120 mg 2 times a day. But with liver diseases, it is not recommended to exceed the dosage of more than 20 mg per day.

This drug has generics with identical chemical compounds, although prices vary significantly.

Given the reviews, Omeprazole's tolerability is good. Patients claim that it is advisable to use it for various disorders in the digestive tract. Moreover, omeprazole capsules well eliminate heartburn immediately after the first application, treat gastritis and ulcers.

However, side effects are possible. It is necessary to use the drug strictly according to the instructions, do not neglect therapeutic doses, and it is best to first consult a doctor before use.

Proton pump inhibitors are indispensable in modern gastroenterology for the treatment of acid-dependent indigestion. For about 20 years, pharmaceuticals of this group have been used with a high therapeutic effect. Recently, two more similar remedies, Pariet and Nolpaza, have appeared in our pharmacies.

In order not to think about the alternative in front of the pharmacy showcase - Nolpaza or Pariet: which is better to buy? Let's do a little comparative analysis of these drugs.

Preparations Pariet and Nolpaza

The acidic environment in the stomach is formed due to its lining (parietal) cells. In the wall of the secretory tubules of these cells there is a special carrier H+/K+ ATPase, the so-called proton pump, which transports hydrogen ions from the cell into the lumen of the tubule in exchange for potassium ions. Paired with it, another pump works, an anion pump, which ensures the delivery of chlorine ions to the same place. As a result, hydrochloric acid is formed. Normally, cells are reliably protected from its damaging effect by a layer of mucus that covers the walls of the stomach. If the integrity of the protective layer is violated, the cells are damaged, ulcers are formed. If you do not reduce the production of acid, then the process will progress.

Pariet and Nolpaza: similarities and differences

The chemical nature of the active ingredients of both drugs, as well as their clinical efficacy, are similar. Rabeprazole (Pariet) and pantoprazole (Nolpaza) are benzimidazole derivatives. Acting at the cellular level, they bind hydrogen ions and attach themselves to the carrier molecule, thereby disrupting its operation.

Nolpaza or Pariet with the same frequency are found in the list of prescriptions for patients suffering from gastric and duodenal ulcers. They are also used for complex therapy, the purpose of which is to eliminate Helicobacter pylori from the stomach. These drugs are also indicated for gastroesophageal reflux (GERD).

Nolpaza is produced in the form of tablets of 20 and 40 mg. In addition, it is the only proton pump inhibitor available in an injectable form. The difference between Pariet and Nolpaza is that it contains a smaller dose of the active substance (10 or 20 mg).

The dosage of Pariet, like Nolpaza, depends on the type and severity of the course of the disease. For ulcers and GERD, the doctor may prescribe Pariet 10 or 20 mg once a day. Together with antibiotics for the eradication of Helicobacter pylori, it is usually prescribed 20 mg 2 times a day.

A variety of Nolpaza dosage forms provides a wider range of options for complex or intensive therapy. For example, to quickly control acidity, the drug can be administered intravenously. The recommended dose of Nolpaza is 20 mg per day. With exacerbation, 40 mg of the drug is prescribed.

Of course, the dilemma "Pariet or Nolpaza: which is more effective for your disease?" it is better for a specialist to decide, as well as in what dosage to use them.

Possible side effects after taking both drugs are:

• change in appetite
• dry mouth
• stomach ache,
• vomit,
• constipation or diarrhea
• dizziness, drowsiness, headache,
• pain in bones and muscles,
• leuko- and thrombocytopenia,
• allergic reactions.

Contraindications for both drugs are similar. They are not recommended for intolerance to their components and children under 12 years of age. Choice Pariet or Nolpaza in patients with sorbitol intolerance it is better to do in favor of Pariet, since Nolpaza contains sorbitol as an excipient.

Pregnancy and lactation are contraindications for taking Pariet, while the instructions for the use of Nolpaza indicate its possible careful use in these cases.

Nolpaza is produced in Slovenia by KRKA. The price of 14 tablets of 20 mg is on average 160 rubles. Pariet is manufactured by Johnson & Johnson Corporation at the Japanese pharmaceutical company EISAI, which may be why it costs much more. The cost of the same quantity and dosage of Pariet is about 1,844 rubles.

20.01.2017

Gastroesophageal reflux disease (GERD) is the most common acid-dependent disease, and the frequency of its detection continues to grow worldwide (G. R. Lockeet al., 1997; S. Bor et al., 2005). The key goal of managing GERD is to maintain an intragastric pH >4. The most effective in the treatment of reflux esophagitis are proton pump inhibitors (PPIs) (J. Dent et al., 1999; P. O. Katzet al., 2013).

One of the most widely used and sensitive methods for assessing acid-suppressive action is 24-hour monitoring of intragastric pH (S. Shi, U. Klotz, 2008). At the same time, the main parameters characterizing the effectiveness of PPIs are considered to be the average pH value over 24 hours, the average time (in percentage terms) pH > 4, and the rate of onset of an adequate acid-suppressive effect after taking the first dose (N. J. Bellet al., 1992 ).

Cytochrome P450 2C19 (CYP2C19) genotypes and Helicobacter pylori (H. pylori) infection can have a significant impact on the ability of PPIs to reduce stomach acid. In patients with low activity of CYP2C19, the so-called slow metabolizers, the acid-lowering effect of PPIs is more pronounced than in patients with high activity of this enzyme, that is, "fast metabolizers" (E. J. Dickson, R. C. Stuart, 2003) . The frequency of the CYP2C19 genotype with high CYP2C19 activity in different populations can reach 20% (Z. Desta et al., 2002; A. Celebi et al., 2009).
Given the significance of the problem, in recent years a number of studies have been conducted on the comparative assessment of the effect of various PPIs on intragastric pH; however, most of these studies compared only two drugs.
The aim of this study was to evaluate the effects of esomeprazole 40 mg, rabeprazole 20 mg, lansoprazole 30 mg, and pantoprazole 40 mg on intragastric pH >4 and 24-hour pH in patients with GERD who are "rapid metabolizers" according to the CYP2C19 genotype and negative for H. pylori.

Materials and methods
The study included H. pylori-negative patients aged ≥18 years with GERD accompanied by heartburn and/or regurgitation occurring at least once a week for the last 6 months. Exclusion criteria: gastric sphincter obstruction, hiatal hernia >2 cm, active peptic ulcer, cancer of the upper gastrointestinal tract, history of gastrointestinal surgery, motility disorders (systemic sclerosis, achalasia, etc.), atrophic gastritis, so-called alarm symptoms in regarding malignant neoplasms (hematemesis, dysphagia, odynophagia, melena), pregnancy or lactation.
Before treatment, all patients underwent a complete physical examination, esophagogastroduodenoscopy, a urea breath test to rule out H. pylori infection, and determination of the CYP2C19 mutation status. The study included patients with wild (non-mutated) CYP2C19 genotype; patients with homo- or heterozygous CYP2C19 mutations were excluded from participation.
PPIs, histamine H2 receptor antagonists, prokinetics, and antispasmodics were not allowed 2 weeks before the start of the study. Patients could use antacids to control symptoms until the day before starting therapy.
Patients were randomized into 4 groups to receive esomeprazole 40 mg (enteric-coated tablet), rabeprazole 20 mg (enteric-coated tablet), lansoprazole 30 mg (micropellet capsule), or pantoprazole 40 mg (enteric-coated tablet) qd/day. 30 min before standard breakfast.
A 24-hour pH measurement of the esophagus and stomach was performed using an Orion pH meter and two electrodes placed intranasally 5 cm above and 10 cm below the lower esophageal sphincter.
During the 6 days of the study, all meals were standardized; breakfast, lunch and dinner were served at 9:30, 13:00 and 19:00 respectively. Patients were not allowed to consume alcohol, acidic or alkaline drinks.

results
The study included 56 patients - 14 patients in each group. Due to protocol deviation, 7 people were excluded, so 49 patients were included in the final analysis.
According to the initial clinical and demographic characteristics, the groups did not differ statistically (Table). Prior to treatment, the time to 24-hour intragastric pH >4 for esomeprazole, rabeprazole, lansoprazole, and pantoprazole averaged 2.4% (95% CI 0.3-14.3), 7.4% (0.9-11 .3), 2.8% (0.4-15.5) and 6.4% (0.7-14.9), respectively, without significant differences between the groups (p>0.05). On the 1st day of treatment, the corresponding figures were 56% (21-87), 58% (31-83), 57% (33-91) and 27% (5-77), on the 5th day - 68% ( 36-90), 63% (22-82), 65% (35-99) and 61% (35-98). In terms of intragastric pH time >4, esomeprazole, rabeprazole and lansoprazole were statistically significantly superior to pantoprazole on day 1, but the difference between the groups leveled off on day 5.
Mean 24-hour intragastric pH for esomeprazole, rabeprazole, lansoprazole and pantoprazole on day 1 was 4.2 (1.4-5.9), 4.4 (2.0-5.1), 4.1 ( 2.7-5.2) and 2.1 (1.0-6.0), on the 5th day - 4.5 (2.5-6.2), 4.6 (2.2-5 .5), 4.4 (2.8-6.0) and 4.4 (2.3-5.6), respectively. According to this indicator, esomeprazole, rabeprazole and lansoprazole were significantly better than pantoprazole on the 1st day.
The time required to reach an intragastric pH >4 after the first dose was 3, 4, and 6 hours for esomeprazole, lansoprazole, and rabeprazole, respectively. In the pantoprazole group, the pH reached 3 2 hours after ingestion, but then did not change until the 6th hour.
The mean intragastric pH for esomeprazole, rabeprazole, lansoprazole and pantoprazole 3 hours after the first dose was 4±0.5; 2.6±0.6; 3±0.5 and 2.9±0.7; after 4 hours - 4.1±0.6; 3.2±0.5; 4±0.5 and 2.9±0.6; after 6 hours - 4.8±0.6; 4±0.5; 4.3±0.7 and 3.2±0.7, respectively. Esomeprazole was statistically significantly superior to rabeprazole, lansoprazole, and pantoprazole after 3 hours (p<0,05), а также пантопразол через 4 и 6 ч после приема (р<0,05).
Regarding the time needed to reach a pH >4 after the first dose, esomeprazole showed the fastest effect, followed by lansoprazole, rabeprazole and pantoprazole in increasing order of time. The hourly pH values ​​achieved in the 4 treatment groups are shown in the figure.

Discussion
The results of the study showed that in patients with GERD who are not infected with H. pylori and belong to the type of so-called fast metabolizers, esomeprazole, rabeprazole and lansoprazole are significantly superior to pantoprazole in terms of intragastric pH > 4 on the 1st day of treatment, while esomeprazole proved to be better than all other PPIs in terms of the rate of onset of adequate acid suppression. These data are broadly consistent with those observed in other studies.
So, scientists from Sweden compared esomeprazole 40 mg with lansoprazole 30 mg, omeprazole 20 mg, pantoprazole 40 mg and rabeprazole 20 mg. Esomeprazole outperformed all other PPIs in mean intragastric pH time >4 on days 1 and 5 of treatment (K. Rohss et al., 2004)
In a study by K.Miner et al. (2003) in H. pylori-negative patients with GERD, esomeprazole 40 mg/day on the 5th day of therapy in terms of intragastric pH was statistically significantly better than lansoprazole 30 mg/day, pantoprazole 40 mg/day, rabeprazole 20 mg/day and omeprazole 20 mg/day
N. G.Hunfeld et al. (2012) found that esomeprazole 40 mg provided better efficacy and faster acid suppression than rabeprazole 20 mg.
According to in vitro studies, the slower onset of action of pantoprazole compared to that of other PPIs may be due to two factors: pantoprazole's lower pKa1 and pKa2 values ​​and its preferential metabolism by CYP2C19.

conclusions
The present study demonstrated that in non-H. pylori-infected "rapid metabolisers" GERD patients, pantoprazole was a less potent PPI than esomeprazole, lansoprazole, and rabeprazole on day 1 of treatment. On the 5th day of therapy, this difference disappears. With regard to the time required to increase intragastric pH >4 after the first dose, esomeprazole has the fastest effect, followed by lansoprazole and rabeprazole.
The results obtained may be of practical importance in the choice of PPI prescribed on an “on demand” basis for the treatment of patients with GERD.

The article is printed in abbreviated form.
The bibliography is under revision.

Celebi A., Aydin D., Kocaman O. et al. Comparison of the effects
of esomeprazole 40 mg, rabeprazole 20 mg, lansoprazole 30 mg,
and pantoprazole 40 mg on intragastric pH in extensive metabolizer patients with gastroesophageal reflux disease. Turk J Gastroenterol 2016; 27:408-414.

Translated from English. Alexey Tereshchenko

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Added: 23.04.2017

One of the most common gastroenterological pathological conditions is an increased content of hydrochloric acid in gastric juice (or hyperacidity). This condition is the basis of inflammation of the stomach or duodenum, as well as the formation of ulcerative lesions in them. Increased acidity can occur both due to non-infectious causes - systematic and / or severe stress and poor nutrition, and due to colonization of the gastric mucosa by the bacterium Helicobacter pylori (infectious cause).

In both the first and second cases, drugs of the PPI group, that is, proton pump inhibitors, are used to treat hyperacid conditions. The most common drugs in this group are omeprazole (omeprazole) and pantoprozolo (pantoprazole). The mechanism of action of the drugs is the same - they inhibit the enzyme H + / K + -ATPase (or the “proton pump”), which ensures the flow of hydrogen into the stomach cavity. With a decrease in the amount of hydrogen, the concentration of hydrochloric acid in the stomach decreases and the acidity of gastric juice normalizes. As a result, permanent damage to the mucous membrane is eliminated and it can fully recover.

So what is the difference between Omeprazene and Pantoprosolo?

Comparative characteristics of drugs - PPI 1 and 2 generations.

* That is, the amount of the active substance that reaches the site of its action (in a particular case, to the parietal cells of the stomach).

** That is, how much the drug can reduce the pathologically increased acidity of gastric juice.

*** That is, the time during which the active substance will lose half of its therapeutic concentration.

Summary

Omeprazole has a more pronounced antisecretory effect (4 times stronger than pantoprazole). Omeprazole begins to act faster, but the therapeutic concentration active substance decreases more quickly.

Pantoprazole is a "softer" drug. Begins to act later and less pronounced inhibits the secretion of hydrochloric acid. But at the same time, pantoprazole retains a therapeutic concentration in the blood longer. It has antimicrobial activity that omeprazole does not have. Pantoprazole has a wider drug compatibility.

Of the two drugs, it is impossible to single out a leader, since each of them has its own advantages and disadvantages. In one clinical case, Omeprazen will be preferable for the patient, in another - Pantaprozolo. The exact selection of the drug depends on the individual characteristics of the disease and can only be qualified by an experienced gastroenterologist. In the absence of the opportunity to consult with a specialist, an independent selection of the drug is possible based on the above information.