Comparison of the effects of esomeprazole, rabeprazole, lancoprazole and pantoprazole in patients with GERD – “rapid metabolizers. What is the difference between omeprazole and pantoprazole? Various active substances

The pharmaceutical market is growing by leaps and bounds. Every year, new drugs and analogues of existing ones appear. The number of gastroenterological drugs is also constantly growing, proton pump inhibitors (PPIs) are no exception. Omeprazole, which has long been sold under a variety of trade names, there are many analogues, among which is pantoprazole.

What are the similarities:

• indications (as a rule, these are diseases caused by the aggressive action of acid on the walls of the stomach, intestines and esophagus, the fight against Helicobacter in combination with other drugs.)
• contraindications (primarily pregnancy, lactation and childhood, increased sensitivity)
• side effects and precautions

You can easily find a complete list of indications, side effects and contraindications in online reference books or instructions for drugs.

The drug Omeprazole

What is the difference between Pantoprazole and Omeprazole?

There are not many differences between these drugs. The main difference between Pantoprazole and Omeprazole is its greater bioavailability, but at the same time its antisecretory activity is lower than that of omeprazole. Also, the use of pantoprazole is more appropriate if simultaneous treatment with drugs such as citalopram (antidepressant) and clopidogrel (antiplatelet agent) is necessary. It can be added that omeprazole has been used in medicine for much longer.

Which is more profitable: Pantoprazole or Omeprazole?

And here the difference between Omeprazole and Pantoprazole is already more significant.
The price range of Omeprazole and its analogues sold under other trade names (Omez, Ultop, Helicid, Losek, Gastrozol and others) varies from 30 to 200 rubles. The cost of Pantroazole and preparations based on it (Nolpaza, Controloc) starts from 200 rubles and above.

It is important to remember that this article is purely informative in nature, the decision in choosing in the first place should be within the competence of your attending physician.

Esomeprazole(English) esomeprazole) is an antiulcer drug, a proton pump inhibitor (PPI).

Chemical compound:(S)-5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-3H-benzimidazole. Empirical formula C 17 H 19 N 3 O 3 S.

Esomeprazole is the international non-proprietary name (INN) of the drug. According to the pharmacological index, it belongs to the group "Proton pump inhibitors". According to ATC - to the group "Proton pump inhibitors" and has the code A02BC05.

Indications for the use of esomeprazole

Dosage and procedure for taking esomeprazole

The pharmacokinetics of esomeprazole is less subject to individual fluctuations compared to the pharmacokinetics of omeprazole. This indicates a reduction in inter-individual variability in acid control and, therefore, an increase in clinical predictability and reliability of pharmacotherapy using esomeprazole. Due to the improved pharmacokinetics, the antisecretory effect of esomeprazole is more pronounced, manifests faster and is more stable compared to that of omeprazole. While doing daily pH-metry against the background of oral administration of 40 mg of esomeprazole or omeprazole after 12 hours, the proportion of patients with intragastric pH> 4 was 88 and 75%, respectively, and after 24 hours the proportion of patients with intragastric pH> 4 was 68.4% of all those receiving esomeprazole and 62.0 % of all treated with omeprazole. Comparative analysis pharmacodynamic parameters of oral forms of esomeprazole 40 mg, pantoprazole 40 mg, rabeprazole 20 mg, led to the conclusion that esomeprazole has a fundamentally better efficacy profile. Daily pH-metry against the background of oral administration of drugs found that on the 5th day the proportion of patients with intragastric pH> 4 was 69.8% in the esomeprazole group, 44.8% in the pantoprazole group and 44.5% in the rabeprazole group. % (Golovin R.A. and others).

However, the cost of a comparable dose of esomeprazole is substantially greater than that of omeprazole. At the same time, there are studies showing that the treatment of GERD with esomeprazole is more cost-effective than with rabeprazole (Rudakova A.V.).

Esomeprazole has contraindications, side effects and application features, consultation with a specialist is necessary.

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 capsules 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. Risks side effects- are minimal.

Intravenous administration 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 negatively 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 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 ATPase in the cells of the stomach, blocking the production of hydrochloric acid, and 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. Appointed at chronic gastritis, gastroduodenitis, peptic ulcer 12 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 is an excellent treatment for diseases associated with increased production gastric secretion. 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, because it has maximum amount 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.

It is an antisecretory modern facility, which 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.

Introduction

The mechanism of action of pantoprazole is the same as that of other drugs from the group of proton pump inhibitors.

Pantoprazole is the first of the "proton pump" inhibitors, which is available for both oral and intravenous use.

In the US, the main indication for pantoprazole is the treatment of erosive esophagitis associated with gastroesophageal reflux disease (1,2).

Pharmacology

Like other proton pump inhibitors, pantoprazole inhibits ATPase only during hydrochloric acid secretion. Inhibitors of the "proton pump" bind to H+, K+-ATPase and irreversibly block the transport of hydrogen ions.

Pharmacokinetics

Pantoprazole unstable to acid, so it is available in enteric-coated tablets. Pantoprazole is characterized by rapid absorption and its maximum concentration is reached approximately 2.5 hours after a single or repeated dose per os. Pantoprazole undergoes little first-pass metabolism. Its absolute bioavailability is about 77%. The drug can be taken regardless of food intake or antacids. The volume of distribution is approximately 11.0-23.6 liters, and the percentage of protein binding is about 98%. In the liver, pantoprazole undergoes extensive metabolism with the participation of the cytochrome P-450 system. Pantoprazole does not accumulate in the body and repeated doses of the drug during the day do not affect its pharmacokinetics. There is no need for special dose selection of pantoprazole in elderly patients or in patients with kidney failure, as well as with moderately severe liver failure. The half-life of pantoprazole in patients with severe liver cirrhosis is increased to 7-9 hours (6). Data on the pharmacokinetics of pantoprazole in persons under 18 years of age have not yet been published (1).

Indications

Intravenous administration of pantoprazole is indicated for the short-term (7-10 days) treatment of GERD in patients who cannot take tablet forms of the drug.

Additional studies are currently underway to evaluate the effectiveness of intravenous forms of pantoprazole in the treatment of Zollinger-Ellison syndrome, in the prevention of stress ulcers (in patients in intensive care units), as well as in the prevention of aspiration pneumonia in patients undergoing elective surgical interventions.

Clinical Efficiency

Erosive esophagitis in GERD

Comparative studies have been carried out clinical efficacy pantoprazole, histamine H2 receptor antagonists, and omeprazole in patients with grade II or III reflux esophagitis (according to the Savary-Miller scale) (Table 1). As a result of these studies, pantoprazole was found to be more effective than H2 receptor antagonists in terms of ulcer healing and symptom control (10,11).

Tab. 1. Placebo-controlled studies of the efficacy of pantoprazole in erosive esophagitis associated with GERD

GERD - gastroesophageal reflex disease;

PANT - pantoprazole;

P - randomized;

OMP - omeprazole;

MC - multicenter.

In another comparative clinical study, emphasis was placed on studying the pharmacodynamic features of pantoprazole and omeprazole in healthy volunteers. Pantoprazole 40 mg daily has been shown to provide a faster onset of effect and greater suppression of gastric secretion than omeprazole 20 mg daily (14). However, so far it has not been possible to show that these pharmacodynamic differences are significantly reflected in the results of comparative studies of the effectiveness of these drugs in the treatment of esophagitis.

A clinical study by Van Rensburg et al (15) compared the clinical efficacy and tolerability of pantoprazole at daily doses of 40 mg and 80 mg. It was found that after 4 weeks of treatment, complete healing was recorded in 78% and 72% of patients, respectively, and after 8 weeks - in 95% and 94% of patients (p>0.05). These results correlate with those of a well-designed pharmacodynamic study conducted in healthy volunteers, which showed that a daily dose of pantoprazole of 40 mg was as effective as daily doses of 80 and 120 mg (16).

More than 90% of patients with erosive esophagitis heal with short-term proton pump inhibitor therapy, but maintenance therapy is needed to prevent recurrence (17).

In a specially conducted multicenter clinical study, which lasted for a year, the preventive efficacy and safety of maintenance therapy was studied using pantoprazole 40 mg per day. A study was conducted on those patients who managed to achieve healing of reflux esophagitis with omeprazole or pantoprazole therapy (18). Endoscopy data showed recurrence rates of 2% and 6% at 6 and 12 months, respectively. In 24% of patients, side effects were noted, most often diarrhea, nausea, vomiting and dizziness.

In a prospective, randomized, multicenter study, the results of long-term maintenance therapy with pantoprazole 40 mg or 20 mg once a day for 12 months were studied. The study was conducted on 396 patients who achieved complete healing of grade II and III esophagitis (19). According to endoscopies, relapses after six months of treatment with 40 mg or 20 mg of pantoprazole per day occurred in 7% versus 16%, and after 12 months in 19% versus 29%. The authors conclude that the administration of pantoprazole at a daily dose of 20 mg is effective and safe for maintenance therapy in patients who managed to stop the acute period of reflux esophagitis.

Peptic ulcer of the duodenum

Savarino et al. conducted a prospective, randomized, multicenter study of 64 patients with duodenal ulcer. In this study, a 24-hour assessment of gastric acidity and the degree of scarring of ulcers was carried out. Before the start of a 2-week course of therapy with pantoprazole (20 mg once a day, 40 mg once a day and 40 mg twice a day), and also after its completion, all patients underwent endoscopic examination and monitoring of pH in the stomach cavity. Ulcer healing was achieved in 94%, 88% and 95%, respectively. Daily pH monitoring allowed to reveal a dose-dependent effect, while it turned out that taking 40 mg of pantoprazole twice a day is more effective than taking 40 mg of pantoprazole once a day (p<0.01) и 20 мг один раз в сутки (р<0.001). Вместе с тем, полученные данные нуждаются в уточнении, так как было исследовано относительно небольшое количество больных. Кроме того, практически все обследованные пациенты были носителями Н.pylori.

Stomach ulcer

Helicobacter pylori infection

Randomized clinical trials have been conducted comparing the clinical efficacy of omeprazole and pantoprazole when used as one of the components in the combination therapy of H. pylori infection (29). Antibacterial therapy was the same in all cases and consisted of amoxicillin 1 g twice daily and clarithromycin 500 mg twice daily for ten days. The dose of omeprazole was 20 mg twice daily; the dose of pantoprazole is 40 mg once a day or 40 mg twice a day. At the end of the 10-day course of treatment, patients did not receive any therapy except for antacids, if they were needed. The effectiveness of treatment was assessed by the degree of eradication of H. pylori and the degree of healing of ulcers after 4 weeks and 6 months after completion of the course of therapy (Table 4).

Tab. 4. Comparative evaluation of the effectiveness of pantoprazole and omeprazole when they are used in a three-component protocol

OMP 40 = omeprazole 20 mg twice daily;

PANT 40 = pantoprazole 40 mg once daily;

PANT 80 = pantoprazole 40 mg twice a day.

In another study, it was shown that combination therapy, including a high dose of pantoprazole, lasting 7 days allows for the eradication of H. pylori in 93% (30).

In a slightly smaller, prospective, randomized study conducted in 50 patients with peptic ulcer or non-ulcer dyspepsia who were diagnosed with H. pylori, it was found that the clinical efficacy of 40 mg of pantoprazole when taken once a day was equivalent to 40 mg of omeprazole at taking once a day. However, both drugs were given for a week in combination with clarithromycin 50 mg twice daily and metronidazole 500 mg twice daily (31). Eradication of H. pylori was achieved in 100% of patients who received pantoprazole and in 88% of patients who received omeprazole (p = 0.235).

Other treatment options using pantoprazole have also been explored. In particular, the combination of pantoprazole (40 mg daily), clarithromycin (500 mg twice daily) and metronidazole (500 mg three times daily) was found to be more effective than the combination of pantoprazole (40 mg daily) and cparithromycin (500 mg three times a day) (32). At the same time, patients continued to receive treatment with pantoprazole 40 mg per day for two weeks after completing the course of antibiotic therapy. The effectiveness of a course of triple therapy in terms of H. pylori eradication was 95%, while the effectiveness of a course of two-component therapy was 60% (p<0.001).

In addition, a comparative evaluation of the effectiveness of pantoprazole and ranitidine was carried out when used as part of combination therapy for the eradication of H. pylori. It was found that the percentage of H. pylori eradication was higher in those patients who received pantoprazole. The percentage of ervdication and the percentage of healing of ulcers were 82.5% and 100% (when taking 40 mg of pantoprazole once a day in a combination of 500 mg of clarithromycin twice a day); 94.8% and 100% (when taking pantoprazole 40 mg once a day in combination with clarithromycin 500 mg twice a day and amoxicillin 1 g twice a day); 67.6% and 96% (when taking 120 bismuth sucitrate three times a day in combination with 150 mg of roxithromycin twice a day and 250 mg of metronidazole twice a day and 300 mg of ranitidine at bedtime (37). Thus, it was found that the three-component protocol, which included the use of pantoprazole, was significantly more effective in terms of eradication of the infection than the other two protocols studied.

Zollinger-Ellison Syndrome

Acute gastrointestinal bleeding

Side effects and drug toxicity

As pantoprazole became more widespread, side effects such as anaphylaxis, angioedema, pancreatitis, and dermatological reactions were reported.

drug interaction

Dosing regimen

Dose adjustment is not required in elderly patients, as well as in patients with renal insufficiency or with moderate hepatic insufficiency. In addition, there is no need to adjust the dose of pantoprazole in patients on hemodialysis (43).

Pantoprazole extended-release tablets should be swallowed whole, with or without food or antacids. In most clinical studies, pantoprazole was administered before meals.

Tablet forms of pantonrazole

Intravenous forms of nantonrazop

Special remarks

Tab. 2. Placebo-controlled clinical trials of the efficacy of pantoprazole in duodenal ulcer

PANT - pantoprazole;

OMP - omeprazole;

RAS - ranitidine;

P - randomized;

MC - multicenter.

Table 3. Placebo-controlled trial of pantoprazole in acute gastric ulcers

PANT - pantoprazole;

RAS - ranitidine;

P - randomized;

MC - multicenter;

OMP - omeprazole.

Tab. 5. Most common side effects of pantoprazole

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Antiulcer drug pantoprazole: pharmacodynamics, pharmacokinetics and clinical results
Medical News SUN Pharmaceutical Industries Ltd. Information bulletin for doctors. June 2006

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

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

Features of pharmacological preparations

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

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

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

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

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

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

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

The action of drugs in the human body

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

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

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

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

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

Proton pump inhibitors with pantoprazole increase the effect of antibiotics

All types of proton pump inhibitors

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

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

• Indian Omez;
• Ultop made in Slovenia.

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

Lansoprazole

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

Pantoprazole

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

Rabeprazole

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

Esomeprazole

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

Benefits of Proton Pump Inhibitors

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

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

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

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