Otitis

Pantoprazole or omeprazole, which is better, reviews from doctors. Comparison of the effects of esomeprazole, rabeprazole, lansoprazole and pantoprazole in patients with gerb - “rapid metabolizers”

In this article you can read the instructions for use of the drug Pantoprazole. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Pantoprazole in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Pantoprazole in the presence of existing structural analogues. Use for the treatment of ulcers, gastritis, esophagitis of the stomach and duodenum in adults, children, as well as during pregnancy and lactation. Composition of the drug.

Pantoprazole- H-K-ATPase inhibitor. Blocks the final stage of hydrochloric acid secretion, reduces the level of basal and stimulated (regardless of the type of stimulus) secretion of hydrochloric acid in the stomach. In case of duodenal ulcer associated with Helicobacter pylori (Helicobacter), this decrease in gastric secretion increases the sensitivity of the microorganism to antibiotics. Pantoprazole has its own antimicrobial activity against Helicobacter pylori.

Compound

Pantoprazole sodium + excipients.

Pharmacokinetics

Quickly and completely absorbed after oral administration. Absolute bioavailability 70-80% (average 77%). Plasma protein binding is 98%. Very weakly penetrates the blood-brain barrier (BBB) and is secreted into breast milk. Taking antacids or food does not affect AUC, Cmax or bioavailability. Pharmacokinetics are linear in the dose range of 10-80 mg (AUC and Cmax increase in proportion to increasing doses). Metabolized in the liver (oxidation, dealkylation, conjugation). It has low affinity for the cytochrome P450 system; the metabolism involves mainly the CYP3A4 and CYP2C19 isoenzymes. The main metabolites are demethylpantoprazole and 2 sulfated conjugates. It is excreted mainly in the urine (82%) in the form of metabolites, and is found in small amounts in feces. Does not accumulate.

Indications

peptic ulcer of the stomach or duodenum in the acute phase;
Zollinger-Ellison syndrome;
eradication of Helicobacter pylori (in combination with antibacterial therapy);
dyspepsia (nausea, vomiting, flatulence and other symptoms);
reflux esophagitis.

Release forms

Film-coated tablets 20 mg and 40 mg (sometimes mistakenly called capsules).

Instructions for use and dosage regimen

Inside. The tablet should be swallowed whole, without chewing or breaking, with a small amount of liquid, before meals, usually before breakfast. When taken twice, the second dose of the drug is recommended to be taken before dinner.

Peptic ulcer of the stomach and duodenum, erosive gastritis (including those associated with taking NSAIDs)

Anti-relapse treatment of gastric and duodenal ulcers - 20 mg per day.

Helicobacter pylori eradication

The following combinations are used as triple therapy:

Pantoprazole 20-40 mg 2 times a day + amoxicillin 1000 mg 2 times a day + clarithromycin 500 mg 2 times a day. The course of treatment is 7-14 days.
Pantoprazole 20-40 mg 2 times a day + metronidazole 500 mg 2 times a day + clarithromycin 500 mg 2 times a day. The course of treatment is 7-14 days.
Pantoprazole 20-40 mg 2 times a day + amoxicillin 1000 mg 2 times a day + metronidazole 500 mg 2 times a day. The course of treatment is 7-14 days.

After the end of combination therapy, taking Pantoprazole can be continued for the purpose of healing the ulcer. For duodenal ulcers, taking Pantoprazole can be extended from 1 to 3 weeks.

Patients with severe renal impairment (creatinine clearance less than 20 ml/min) or those on hemodialysis are not prescribed Helicobacter pylori eradication therapy.

Treatment of mild GERD symptoms (such as heartburn, nausea, sour belching)

The recommended dose of the drug is 20 mg per day. To achieve positive dynamics in eliminating symptoms, it may be necessary to take the drug for 2-3 days, but to completely eliminate symptoms, it may be necessary to take the drug for 7 days. If the condition worsens during the first 3 days of treatment, consultation with a specialist is recommended. The drug should be stopped immediately after symptoms disappear.

Zollinger-Ellison syndrome

The recommended dose is 40-80 mg per day. In patients with severe liver dysfunction, the dose should be reduced to 40 mg once every 2 days. In this case, it is necessary to monitor biochemical blood parameters. If the activity of liver enzymes increases, the use of the drug should be discontinued.

Side effect

diarrhea;
nausea;
pain in the upper abdomen;
flatulence;
headache;
weakness;
dizziness;
initial manifestations of depressive states;
visual impairment;
rash;
weakness;
dizziness;
swelling;
increase in body temperature.

Contraindications

dyspepsia of neurotic origin;
malignant diseases of the gastrointestinal tract;
children under 6 years of age (no experience of use);
hypersensitivity to pantoprazole.

Use during pregnancy and breastfeeding

If it is necessary to use Pantoprazole during pregnancy, it is necessary to evaluate the expected benefit to the mother and the potential risk to the fetus.

If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.

Experimental studies have found that Pantoprazole is excreted in breast milk.

Use in children

Contraindicated in children under 6 years of age (there are no clinical data on the use of the drug in this age group).

Special instructions

Before starting therapy, the possibility of a malignant neoplasm in the stomach and esophagus should be excluded, since the use of Pantoprazole reduces the severity of symptoms and may delay the establishment of the correct diagnosis. The diagnosis of reflux esophagitis requires mandatory endoscopic confirmation.

When used in patients with impaired liver function, the activity of liver enzymes in the blood plasma should be regularly monitored and pantoprazole should be discontinued if it increases.

Drug interactions

With simultaneous use, Pantoprazole may alter the absorption of drugs whose absorption depends on the pH of the gastric contents (ketoconazole).

Due to the fact that pantoprazole is metabolized in the liver by the cytochrome P450 enzyme system, the possibility of drug interactions with drugs metabolized by the same enzyme system cannot be excluded.

Analogues of the drug Pantoprazole

Structural analogues of the active substance:

Zipanthol;
Control;
Crosacid;
Nolpaza;
Pantaz;
Pantoprazole Canon;
Panum;
Peptazol;
Pigenum;
Puloref;
Sanpraz;
Ulthera.

Analogs by pharmacological group (proton pump inhibitors):

Akrilanz;
Vimovo;
Gastrozol;
Dexilant;
Demeprazole;
Zerocide;
Zolser;
Zulbex;
Control;
Crosacid;
Lanzabel;
Lanzap;
Lansoprazole;
Lancid;
Losek;
Loenzar;
Nexium;
Nolpaza;
Noflux;
Omez;
Omez Insta;
Omeprazole;
Omeprus;
Omephesis;
Omizak;
Omitox;
Ontime;
Orthanol;
Ocid;
Pantaz;
Pantoprazole Canon;
Panum;
Pariet;
Peptazol;
Pepticum;
Pilobact;
Pleom;
Rabelok;
Rabeprazole;
Romesek;
Sanpraz;
Ulzol;
Ulkozol;
Ulthera;
Ultop;
Khairabesol;
Helitrix;
Helicide;
Cisagast;
Esomeprazole;
Emanera;
Epicurus.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

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 nonproprietary name (INN) of the drug. According to the pharmacological index, it belongs to the group “Proton pump inhibitors”. According to ATC, it belongs to the group “Proton pump inhibitors” and has the code A02BC05.

Indications for use of esomeprazole

Gastroesophageal reflux disease (GERD): erosive reflux esophagitis (treatment), prevention of relapses in patients with cured esophagitis, symptomatic treatment of GERD. As part of combination therapy: eradication of Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori, prevention of relapse of ulcers in patients with gastric and duodenal ulcer associated with Helicobacter pylori.

Doses and order of taking esomeprazole

The esomeprazole tablet should be swallowed whole with liquid. Tablets must not be chewed or broken. For patients who have problems swallowing, esomeprazole tablets are dissolved in still water and the solution is administered through a nasogastric tube.

The pharmacokinetics of esomeprazole are less subject to individual fluctuations compared to the pharmacokinetics of omeprazole. This indicates a reduction in interindividual variability in acid control and, therefore, an increase in clinical predictability and reliability of pharmacotherapy using esomeprazole. Due to improved pharmacokinetics, the antisecretory effect of esomeprazole is more pronounced, faster to manifest and more stable compared to that of omeprazole. When executing 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 those receiving omeprazole. A comparative analysis of the pharmacodynamic parameters of oral forms of esomeprazole 40 mg, pantoprazole 40 mg, rabeprazole 20 mg allowed us to conclude that esomeprazole has a fundamentally better efficacy profile. Daily pH-metry against the background of oral administration of drugs established 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. et al.).

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

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

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 for 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 from the PPI group, that is, proton pump inhibitors, are used to treat hyperacid conditions. The most common medications in this group are Omeprazene (omeprazole) and Pantoprazolo (pantoprazole). The mechanism of action of the drugs is the same - they inhibit the enzyme H + /K + -ATPase (or “proton pump”), which ensures the flow of hydrogen into the stomach cavity. When the amount of hydrogen decreases, 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 are the differences between Omeprazen and Pantoprosolo?

Comparative characteristics of drugs – 1st and 2nd generation PPIs.

	Omeprazene (omeprazole)	Pantoprazolo (pantoprazole)
Generation of drugs – proton pump inhibitors	1st generation	2nd generation
When was received	in 1979 in Sweden	in the early 90s in Germany
Bioavailability*
Antisecretory activity**
Half-life***		80-90 minutes
Time required to block 50% of all H + /K + -ATPases	400 seconds (equals 6 minutes 40 seconds)	1100 seconds (equals 18 minutes 20 seconds)
Route of elimination from the body	Through the kidneys with urine
Contraindications for use	Hypersensitivity to the active substance, severe liver or kidney failure. Strictly under medical supervision in the following cases: childhood, pregnancy and breastfeeding
Antimicrobial activity	Not noted	Antimicrobial activity against Helicobacter pylori is noted. Strengthens the effect of drugs aimed at destroying H. pylori
Drug compatibility
Joint use only after consultation with a doctor	Ketoconazole, Itraconazole, Posaconazole, Voriconazole, Digoxin, St. John's wort (Hypericum perforatum) based preparations, Cilostazol Phenytoin, Diazepam, Warfarin, Clapidogrel, Rifampicin, Atazanavir, Saquinavir, Cyclosporine, Erlotinib, Methotrexate	Ketoconazole, Itraconazole, Posaconazole, Erlotinib, Methotrexate, Warfarin, Phenprocoumon, Liquamar, Marcumar, Atazanavir
Joint use only after consultation with a doctor		Approved for use together with Citaloram (antidepressant) and Clopidogrel (antiplatelet agent)

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

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

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

Resume

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

Pantoprazole is a “softer” drug. It begins to act later and inhibits the secretion of hydrochloric acid to a lesser extent. But at the same time, pantoprazole retains its therapeutic concentration in the blood longer. It has antimicrobial activity that omeprazole does not have. Pantoprazole has 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, Omeprazene 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 carried out expertly by an experienced gastroenterologist. If it is not possible to consult with a specialist, you can independently select the drug based on the above information.

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, and proton pump inhibitors (PPIs) are no exception. Omeprazole, which has long been sold under a variety of trade names, has many analogues, including pantoprazole.

What are the similarities:

indications (these are usually 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, hypersensitivity)
side effects and precautions

You can easily find a complete list of indications, side effects and contraindications in online reference books or instructions for the 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 advisable if simultaneous treatment with drugs such as citalopram (an antidepressant) and clopidogrel (an 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?

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

It is important to remember that this article is of a purely informative nature; the decision to choose should primarily be within the competence of your attending physician.

20.01.2017

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

One of the most widely used and sensitive methods for assessing acid suppressive effects 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 may have a significant impact on the ability of PPIs to reduce gastric acidity. In patients with low activity of CYP2C19, the so-called slow metabolizers, the acid-lowering effect of PPIs is more pronounced compared with that in patients with high activity of this enzyme, that is, “rapid 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 “extensive 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 observed at least once a week in 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 starting treatment, all patients underwent a complete physical examination, esophagogastroduodenoscopy, a urea breath test to exclude H. pylori infection, and determination of the CYP2C19 mutation status. The study included patients with the “wild” (non-mutated) genotype of CYP2C19; patients with homo- or heterozygous CYP2C19 mutations were excluded from participation.
2 weeks before the start of the study, it was not allowed to take PPIs, histamine H2 receptor antagonists, prokinetics and antispasmodics. To control symptoms, patients could use antacids 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) once daily. 30 minutes before standard breakfast.
24-hour pH measurements of the esophagus and stomach were 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 drink alcohol or acidic or alkaline drinks.

Results
The study included 56 patients - 14 patients in each group. Seven subjects were excluded due to protocol deviation, leaving a total of 49 patients in the final analysis.
The groups did not differ statistically in baseline clinical and demographic characteristics (Table). Before treatment, the time of 24-hour intragastric pH >4 for esomeprazole, rabeprazole, lansoprazole and pantoprazole averaged 2.4% (95% confidence interval 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 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). Regarding the time indicator of intragastric pH >4, esomeprazole, rabeprazole and lansoprazole on day 1 were statistically significantly superior to pantoprazole, but on day 5 the difference between the groups was leveled out.
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. For this indicator, esomeprazole, rabeprazole and lansoprazole were significantly better than pantoprazole on day 1.
The time required to achieve 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 administration, 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 at 3 hours (p<0,05), а также пантопразол через 4 и 6 ч после приема (р<0,05).
Regarding the time required to reach pH >4 after the first dose, esomeprazole showed the fastest effect, followed in order of increasing time by lansoprazole, rabeprazole and pantoprazole. The hourly pH values achieved in the 4 treatment groups are presented in the figure.

Discussion
The results of the study showed that in patients with GERD, not infected with H. pylori and belonging to the type of so-called rapid metabolizers, in terms of intragastric pH >4 on the 1st day of treatment, esomeprazole, rabeprazole and lansoprazole are significantly superior to pantoprazole, while esomeprazole turned out to be better than all other PPIs in terms of the rate of onset of adequate acid suppression. These data are generally consistent with observations obtained in other studies.
Thus, scientists from Sweden compared esomeprazole 40 mg with lansoprazole 30 mg, omeprazole 20 mg, pantoprazole 40 mg and rabeprazole 20 mg. Esomeprazole was superior to all other PPIs in terms of mean time of intragastric pH >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 for 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 provides better efficacy and a faster acid suppressive effect compared to rabeprazole 20 mg.
Based on in vitro studies, the slower onset of action of pantoprazole compared to that of other PPIs may be due to two factors: the lower pKa1 and pKa2 values of pantoprazole and its preferential metabolism by CYP2C19.

Conclusions
The present study demonstrated that in non-H. pylori-infected patients with GERD who are “rapid metabolizers,” pantoprazole is a less potent PPI than esomeprazole, lansoprazole, and rabeprazole on day 1 of treatment. On the 5th day of therapy, this difference disappears. In terms of 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 have practical significance when choosing PPIs prescribed on an “on demand” basis for the treatment of patients with GERD.

The article is published in abbreviation.
The list of references is in the editorial office.

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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