Nexium, 14 pcs., 40 mg, film-coated tablets

Composition and form of the product

Nexium is produced in the form of tablets, extended-release capsules or lyophilisate in vials. The active substance in it is esomeprazole. Its content in various forms of the drug is:

• In tablets - 20 or 40 mg.
• In capsules - 10 mg.
• In bottles with lyophilisate – 40 mg.

Other auxiliary components that were used in the manufacture of the products are indicated in the manufacturer's instructions.

Action of the medicine

The action of zomeprazole is aimed at inhibiting the production of hydrochloric acid by the glands of the digestive organ. After taking Nexium tablets, the pH level of the stomach is quickly normalized. In this case, the indicators are maintained for 3–17 hours. In the future, a cumulative effect is ensured.

By providing a sustainable decrease in acidity, the medicine creates optimal conditions for the destruction of the bacterium Helicobacter pylori, which provokes the development of gastritis and peptic ulcers. In combination with antibiotics Nexium, the instructions focus on this, it allows you to destroy the pathogenic microorganism in almost a week. Patients with reflux esophagitis can get rid of unpleasant symptoms after a 4-week course of treatment. When using the drug, the risks of relapses and complications are significantly reduced.

Use of the drug Nexium tablets

Nexium tablets should be swallowed whole with plenty of liquid; the tablets should not be crushed or chewed. For patients who cannot swallow the tablet, it is recommended to dissolve it in 100 ml of still water. Other liquids should not be used as they may damage the enteric coating. The resulting liquid should be taken immediately or within 30 minutes. Then take another glass of water, rinse the walls with water and drink. Microgranules should not be chewed or crushed. For patients with difficulty swallowing, the tablet can be administered through a nasogastric tube after placing it in 1/2 glass of still water. It is very important that the syringe and probe are of the appropriate size. Administration of the drug through a nasogastric tube

1. Place the tablet in the appropriate syringe and fill it with approximately 25 ml of water and 5 ml of air. Some probes may require 50 ml of water to prevent the tablet from obstructing the passage of the probe.
2. Shake the syringe for 2 minutes until the tablet dissolves.
3. Holding the syringe vertically (tip up), check the patency of the tip.
4. Attach the syringe to the probe, holding it vertically.
5. Shake the syringe and turn it upside down. Quickly inject 5–10 ml of liquid. Invert the syringe after injection and shake again (the syringe should be held vertically to prevent clogging of the tip).
6. Turn the syringe over and inject another 5–10 ml of liquid into the probe. Repeat the procedure until all the liquid has been administered.
7. To wash off the remaining drug from the walls of the syringe, fill it with 25 ml of water and 5 ml of air, shake, turn over and quickly inject the liquid. Some probes may require 50 ml of water.

Adults and children over 12 years of age Reflux esophagitis with GERD Treatment of erosive reflux esophagitis with GERD: 40 mg 1 time per day for 4 weeks. If symptoms of esophagitis persist, it is recommended to continue treatment for another 4 weeks. Anti-relapse treatment: 20 mg 1 time per day. Symptomatic treatment of GERD: 20 mg 1 time per day daily for 4 weeks in the absence of symptoms of esophagitis. If symptoms persist, re-examination is necessary. After eliminating the symptoms of the disease, further control is achieved by taking the drug at a dose of 20 mg 1 time per day. In adults, you can use the “on demand” regimen: 20 mg 1 time per day. In patients at risk of developing gastric or duodenal ulcers after taking NSAIDs, further symptom control using an on-demand regimen is not recommended. Adults In a complex regimen combined with antibacterial agents for the eradication of Helicobacter pylori Treatment of duodenal ulcers associated with Helicobacter pylori: 20 mg of Nexium with 1 g of amoxicillin and 500 mg of clarithromycin 2 times a day for 7 days. Anti-relapse treatment in patients with peptic ulcers caused by Helicobacter rulori: 20 mg of Nexium with 1 g of amoxicillin and 500 mg of clarithromycin 2 times a day for 7 days. Patients requiring long-term treatment with NSAIDs Treatment of peptic ulcers of the stomach caused by the use of NSAIDs: the recommended dose is 20 mg 1 time per day, duration of treatment is 4-8 weeks. Prevention of the development of peptic ulcers of the stomach and duodenum caused by NSAIDs in patients at risk: the recommended dose is 20 mg 1 time per day. Maintaining hemostasis and preventing the development of recurrent bleeding from a gastric or duodenal ulcer after treatment with Nexium (infusion solution): 40 mg 1 time per day for 4 weeks. The period of prescribing Nexium for oral administration should be preceded by infusion therapy with Nexium in the form of an infusion for 30 minutes, followed by intravenous infusion at a dose of 8 mg/hour for 3 days (72 hours). Treatment of Zollinger-Ellison syndrome: 40 mg 2 times a day. The dose should be selected individually, the duration of treatment is determined according to clinical indications. According to the clinical data obtained, disease control can be achieved in most patients when taking 80 and 160 mg of esomeprazole per day. If the dose exceeds 80 mg/day, it should be divided into 2 doses.

What does the drug treat?

Nexium tablets and other medications are used to treat various pathologies of the digestive system. In particular, the drug is considered effective for stomach ulcers caused by the bacterium Helicobacter pylori. Gastroesophageal reflux disease can also be successfully treated with this medicine. Thanks to him, you can quickly:

• Stabilize the condition.
• Prevent relapses.
• Remove negative symptoms.

As a prophylactic agent, Nexium, the instructions indicate this, is effective against the background of long-term treatment with non-steroidal anti-inflammatory drugs.

It also improves the condition of patients when diagnosing Zollinger-Ellison syndrome or other pathologies characterized by hypersecretion of the glands of the digestive organ.

A contraindication to taking the drug is intolerance to the active substance or other components that are included in the composition. The medicine is not prescribed for children under 12 years of age. They are prescribed treatment with caution for problems with kidney function. Also, when prescribing, be sure to take into account interactions with other medications.

Nexium

Nexium ®

(lat.
Nexium ®
) is an antiulcer drug, proton pump inhibitor (PPI).

Composition of Nexium

Nexium is available as extended-release capsules (enteric-coated pellets), 10 mg, film-coated tablets of 20 mg and 40 mg, and as a lyophilisate for solution for IV administration. The active substance of Nexium is esomeprazole. One capsule of Nexium extended-release contains:

• esomeprazole magnesium trihydrate 11.1 mg (equivalent to 10 mg esomeprazole)
• excipients: copolymer of methacrylic acid and ethyl acrylate, talc, sucrose in the form of spherical granules ranging in size from 0.25 to 0.355 mm, hyprolose, hypromellose, triethyl citrate, magnesium stearate, glycerol monostearate, polysorbate, dextrose, crospovidone, xanthan gum, citric acid, dye iron oxide yellow

One Nexium tablet contains:

• active substances: 22.3 mg or 44.5 mg of esomeprazole magnesium trihydrate, corresponding to 20 mg and 40 mg of esomeprazole
• excipients: glyceryl monostearate 40-55, hyprolose, hypromellose, red iron oxide, yellow iron oxide (for a dosage of 20 mg), magnesium stearate, methacrylic and ethacrylic acid copolymer (1:1), microcrystalline cellulose, synthetic paraffin, macrogol, polysorbate 80, crospovidone, sodium stearyl fumarate, spherical sucrose granules, titanium dioxide, talc, triethyl citrate.

One bottle of Nexium lyophilisate contains 42.5 mg of esomeprazole sodium, which corresponds to the content of 40 mg of esomeprazole.

Indications for use of Nexium

Gastroesophageal reflux disease (GERD):

• treatment of erosive reflux esophagitis
• long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse
• symptomatic treatment of GERD

Peptic ulcer of the stomach and duodenum: As part of combination therapy (monotherapy with Nexium is not used for HP eradication):

• treatment of duodenal ulcer associated with Helicobacter pylori (Hp)
• prevention of relapses of peptic ulcer disease associated with Hp

With long-term use of non-steroidal anti-inflammatory drugs (NSAIDs):

• healing of stomach ulcers associated with taking NSAIDs
• prevention of gastric and duodenal ulcers associated with taking NSAIDs in patients at risk

Zollinger-Ellison syndrome
or other conditions characterized by pathological hypersecretion, including idiopathic hypersecretion.

Method of administration of Nexium and dose

The Nexium tablet is swallowed whole with liquid.
The tablets are not chewed or crushed. If you have problems swallowing, dissolve the tablet until the tablet disintegrates into microgranules in 100 ml of still water, after which all microgranules are drunk immediately or within half an hour, then add another 100 ml of still water, stir the remainder and drink. If oral therapy is not possible, a Nexium solution prepared from lyophilisate is administered intravenously based on a dose of 20-40 mg of esomeprazole once a day.

GERD (children over 12 years old and adults)

• one or two courses (the second - if the first is not enough to heal or get rid of the symptoms of esophagitis), each for 40 days, 40 mg of Nexium once a day
• maintenance therapy after healing of esophagitis - 20 mg Neximum once a day for a long period
• symptomatic treatment of GERD without esophagitis - 20 mg Nexium once a day; symptoms should disappear within 4 weeks

Stomach and duodenal ulcers (adults only)

• treatment of DU or prevention of PU associated with HP - Nexium 20 mg, amoxicillin 1 g and clarithromycin 500 mg twice a day for a week; it is possible to use Nexium as part of other eradication regimens ( see “Standards for diagnosis and treatment of acid-dependent and Helicobacter pylori-associated diseases (4th Moscow agreement)”)
  .
• treatment of ulcer associated with NSAID use - a maximum of 20 mg or 40 mg once a day for 4-8 weeks
• prevention of peptic ulcer associated with NSAID use - Nexium 20 mg or 40 mg once a day

Conditions associated with pathological hypersecretion (adults only)
, including Zollinger-Ellison syndrome and idiopathic hypersecretion. The starting dose is 40 mg Nexium twice daily. Next, the dose is selected individually, the duration of treatment depends on the development of the disease.

Comparison of Nexium with other acid-blocking drugs

It is generally accepted that proton pump inhibitors (PPIs) are the most effective class of drugs among antisecretory drugs that block the secretion of hydrochloric acid in the stomach. Nexium is the most modern PPI drug. The patent protection period for esomeprazole has not expired and there are no generics or other drugs with the active substance esomeprazole on the pharmaceutical market. However, among gastroenterologists there are different opinions regarding the exclusivity of Nexium among other drugs used to treat acid-related diseases. Recognizing its advantages in some of the parameters, especially over omeprazole, lansoprazole and pantoprazole and H2-blockers, a number of gastroenterologists (not all) believe that Nexium is inferior to Pariet (rabeprazole). This issue is discussed in more detail in the section Comparison of esomeprazole with other proton pump inhibitors
of the article
Esomeprazole
. It is important to note that the cost of Nexium and Pariet significantly exceeds the cost of other PPIs, and the effectiveness, even according to its “apologists,” is not very significant. In addition, the reaction of an individual organism to any antisecretory agent is strictly individual and the “best” medicine does not always cure a particular person. To select a medication and an individual dose, intragastric pH-metry is used, which is used to determine the patient’s response to the drug (see S.I. Rapoport et al. Selection of individual drug therapy for various diseases).

Preparation of Nexium solutions for injections and infusions from lyophilisate and their use

When preparing a Nexium solution for intravenous injection, 5 ml of a 0.9% sodium chloride solution for intravenous administration is added to the vial with Nexium lyophysate.
When preparing an infusion solution of Nexium, the contents of one bottle of Nexium lyophilisate are dissolved in 100 ml of 0.9% sodium chloride solution for intravenous administration. Nexium solution is a clear, pale yellow liquid. The degradation of the solution depends mainly on its acidity, so only 0.9% sodium chloride solution for intravenous administration should be used. Nexium solution should not be mixed or administered with other medications. The solution should not contain visible mechanical impurities or discoloration. The solution must be transparent. When prescribing 20 mg of Nexium per day, half of the prepared solution is administered, the rest is destroyed.

Nexium solution for injection is administered immediately after preparation intravenously for at least 3 minutes. Nexium solution for infusion is administered over 10–30 minutes.

Pharmacological properties of Nexium

The pharmacokinetics and pharmacodynamics of Nexium are determined by the active substance and are described in the article esomeprazole in the sections pharmacokinetics of esomeprazole
and
pharmacodynamics of esomeprazole
.

Contraindications for taking Nexium

• hypersensitivity to esomeprazole, substituted benzimidazoles or other ingredients included in the drug
• hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency
• age up to 12 years (for GERD) and any child age according to indications other than GERD
• Nexium should not be taken with atazanavir
• with caution in severe renal failure

Use of Nexium during pregnancy and breastfeeding

During pregnancy, Nexium therapy is possible only for health reasons. While taking Nexium, you must stop breastfeeding.

Side effects of Nexium

Headache, abdominal pain, diarrhea, flatulence, nausea, vomiting, constipation, dermatitis, itching, urticaria, rash, dizziness, dry mouth, insomnia, paresthesia, drowsiness, increased activity of liver enzymes, peripheral edema.
Long-term or high-dose use of Nexium increases the risk of hip, wrist, and spine fractures (“FDA Warns”).

Nexium overdose

To date, extremely rare cases of intentional overdose of Nexium have been described. Taking Nexium at a dose of 280 mg was accompanied by general weakness and gastrointestinal symptoms. A single dose of 80 mg of Nexium does not cause any negative effects. Specific antidotes are unknown. Esomeprazole binds to plasma proteins, making dialysis ineffective. In case of overdose, symptomatic and general supportive treatment is provided.

Special instructions for Nexium therapy

If any alarming symptoms are present (eg, significant spontaneous weight loss, repeated vomiting, dysphagia, hematemesis, or melena), or if a gastric ulcer is present or suspected, the presence of a malignant neoplasm must be excluded, since treatment with Nexium may lead to flattening symptoms and delay diagnosis.
Those taking Nexium for a long period (especially more than a year) should be under regular medical supervision. Those taking Nexium "as needed" should be instructed to contact their doctor if their symptoms change. Since there are fluctuations in the concentration of esomeprazole in plasma when prescribing therapy “as needed”, it is necessary to take into account the interaction of the drug with other drugs. Clarithromycin is a potent inhibitor of CYP3A4, therefore, when prescribing eradication therapy to patients receiving other drugs metabolized by CYP3A4 (for example, cisapride), possible contraindications and interactions of clarithromycin with these drugs must be taken into account. Nexium contains sucrose and is therefore contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase deficiency.

Interaction of Nexium with other drugs

The interaction of Nexium with other drugs is determined by its active substance and is described in the article esomeprazole, in the section interaction of esomeprazole with other drugs
.

Instructions for medical use of Nexium

Official instructions for medical use of the drug Nexium from the manufacturer, pdf:

• Nexium, film-coated tablets containing 20 or 40 mg esomeprazole
• Nexium, enteric-coated pellets and granules for oral suspension
• Nexium, lyophilisate for the preparation of solution for intravenous administration
• Instructions (medical guide) for US patients “Nexium - capsules and extended-release suspension” (in English): “Medication Guide Nexium (esomeprazole magnesium) Delayed-Release Capsules, Nexium (esomeprazole magnesium) for Delayed-Release Oral Suspension.”

Nexium does not affect the ability to drive a car
or operate machinery.

According to the pharmacological index, Nexium belongs to the group “Proton pump inhibitors”«

. According to ATC, it belongs to the group “Proton pump inhibitors” and has the code A02BC05.

Medicines containing the active ingredient esomeprazole

Manufacturer of Nexium: AstraZeneca AB (AstraZeneca), Sweden.
In addition to Nexium, the following drugs with the active substance esomeprazole are registered in Russia: Neo-Zext, Esomeprazole-Vial, Esomeprazole Zentiva, Esomeprazole Canon, Esomeprazole-native, Emanera, Emezol.

In some other countries, brands are registered and produced: Nexium and Nexium IV (USA), Esopral (Italy, the Netherlands), Axagon (Italy), Nexiam (Belgium, Luxembourg, South Africa), as well as generics of esomeprazole: Ezocar (Belarus, Palestine), Sompraz (India, Myanmar), Neksium and Neksium Inj (India), Nexpro (India), etc.

Materials for healthcare professionals regarding the treatment of gastrointestinal diseases with Nexium

Articles

• Ivashkin V.T., Nemytin Yu.V., Makarov Yu.S. et al. Comparative assessment of the antisecretory activity of Losec MAPS, Pariet and Nexium in patients with peptic ulcer. TsVKG im. A.A. Vishnevsky, MMA named after. THEM. Sechenov.
• Zvyagin A.A., Shcherbakov P.L., Pochivalov A.V., Kashnikov V.V. Esomeprazole (Nexium) in the treatment of functional dyspepsia in children according to 24-hour pH monitoring // Bulletin of Siberian Medicine. — Appendix 2. — 2005.
• Demyanenko D. Nexium (esomeprazole) is a new word in the treatment of acid-related diseases of the gastrointestinal tract // Medical newspaper “Health of Ukraine”. – 2008. – No. 6/1. - With. 36–37.
• Grinevich V.B., Uspensky Yu.P. Secretolytic therapy of acid-dependent diseases of the digestive system from the position of a clinician: 2003 // Experimental and clinical gastroenterology. – 2003. – No. 6.
• Rudakova A.V. Pharmacoeconomic aspects of the use of rabeprazole and esomeprazole in patients with gastroesophageal reflux disease // Consilium-Medicum. – 2006. – Volume 8. – No. 2.
• Dobrovolsky O.V., Serebrova S.Yu. Endoscopic pH-metry as a method for assessing the effect of Nexium on the acid-producing function of the stomach in hyperacid gastritis // Evidence-based medicine - the basis of modern healthcare: abstracts of the VI International Congress. - Khabarovsk. – 2007. – P. 107-109.
• Bordin D.S., Berezina O.I., Yanova O.B., Kim V.A. The effectiveness of esomeprazole in the treatment of gastroesophageal reflux disease // Gastroenterology. 2015. No. 2. pp. 20–25.
• Sarsenbaeva A.S., Petukhova T.P. et al. Efficacy of standard first-line triple eradication therapy based on esomeprazole and other PPIs in patients with H. pylori-associated gastritis // Breast Cancer. Gastroenterology. – 2022. – No. 17. P. 1215-1219.

On the website GastroScan.ru in the “Literature” section there is a subsection “Esomeprazole”, containing articles for doctors regarding the treatment of diseases of the gastrointestinal tract with Nexium.

Video

Still from video: Popova E.N. Gastroesophageal reflux disease

Still from video Osadchuk A.M. Gastroesophageal reflux disease: current issues of diagnosis and treatment

Still from video Bordin D.S. A simple and effective algorithm for the treatment of acid-related diseases

Still from a video for pediatricians Mukhametova E.M.
Ipatova M.G. Symptoms of gastroesophageal reflux in a child: when is additional examination needed? On the website in the “Video” section there is a subsection for patients “Popular Gastroenterology” and a subsection “For Doctors”, containing video recordings of reports, lectures, webinars in various areas of gastroenterology for healthcare professionals.
Nexium has contraindications, side effects and application features; consultation with a specialist is necessary. Back to section

Negative effects and overdose

The active substance is well tolerated. Therefore, negative reactions of the body rarely occur when using the drug for the prevention and treatment of various diseases. The following symptoms indicate drug intolerance:

• Dry mouth.
• Increased body temperature.
• Bronchial spasm.
• Swelling.
• Hyperhidrosis.

Sometimes Nexium can provoke disturbances in the functioning of the central nervous system: depression, drowsiness, dizziness. In severe cases, increased excitability and hallucinations may occur.

There are certain risks of disruptions in the gastrointestinal tract, disorders of the liver and problems with hematopoietic processes.

In case of an overdose, which can be caused by an amount of active substance exceeding 280 mg, severe weakness and negative effects on the digestive system occur. There is no specific antidote. Therefore, all that is needed is to refuse treatment with the drug and carry out symptomatic treatment. Dialysis is ineffective.

Side effects of the drug Nexium tablets

Classified depending on the frequency of development: common (1/100, but ≤1/10), uncommon (1/1000, but ≤1/100), rare (1/10,000, but ≤1/1000) and very rare ( ≤1/10,000). From the hematopoietic system: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis and pancytopenia. From the immune system: rarely - hypersensitivity reactions in the form of angioedema and anaphylactic shock, fever. From the side of metabolism: infrequently - peripheral edema; rarely - hyponatremia. From the mental side: infrequently - insomnia; rarely - agitation, depression, confusion; very rarely - aggression, hallucinations. From the side of the central nervous system: often - headache; infrequently - weakness, paresthesia, drowsiness; rarely - taste disturbance. From the organ of vision: rarely - blurred vision. On the part of the hearing organ: infrequently - dizziness. From the respiratory system: rarely - bronchospasm. From the gastrointestinal tract: often - abdominal pain, constipation, diarrhea, bloating, nausea, vomiting; uncommon - dry mouth; rarely - stomatitis, candidiasis of the digestive tract. From the hepatobiliary system: infrequently - increased activity of liver enzymes; rarely - hepatitis with and without jaundice; very rarely - liver failure, encephalopathy in patients with liver disease. From the skin: infrequently - dermatitis, itching, rash; rarely - alopecia, photosensitivity; very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: rarely - arthralgia, myalgia; very rarely - muscle weakness. From the kidneys and urinary system: very rarely - interstitial nephritis. From the endocrine system: very rarely - gynecomastia. Others: rarely - weakness, increased sweating.

Rules of application

Nexium 20 mg tablets, the instructions focus on this, you need to swallow. Be sure to drink them with enough water. If you have problems swallowing, you can dissolve the tablet in 100 g of still water to obtain microgranules. You need to drink the solution, and after half an hour you should fill the glass halfway with water, stir the rest and drink. Alternatively, the medicinal solution can be administered using a probe.

If it is impossible to take the medicine orally, use lyophilisate. A solution is prepared from it for intravenous administration. The recommended dose is 20-40 mg, frequency of administration is once a day.

Always during treatment, the dosage and duration of treatment are determined by the doctor based on the severity of the disease and the patient’s condition. At the same time, it is necessary to monitor the results obtained during the treatment process.

Pharmacological properties of the drug Nexium tablets

Esomeprazole is the S-isomer of omeprazole. Inhibits the secretion of gastric juice due to specific inhibition of the proton pump of parietal cells of the gastric mucosa. The R- and S-isomers of omeprazole have the same pharmacodynamic properties. Esomeprazole is a weak base, accumulates and becomes active in the acidic environment of the secretory tubules of parietal cells, where it inhibits the enzyme H+K+-ATPase (proton pump), blocking the secretion of hydrochloric acid. After oral administration of the drug at a dose of 20–40 mg, the effect develops within 1 hour. When repeated administration of esomeprazole at a dose of 20 mg once a day for 5 days, the maximum value of gastric secretion stimulated by pentagastrin decreases by an average of 90% after 6–7 hours after taking it on the 5th day. 5 days after taking esomeprazole at a dose of 20 or 40 mg, the gastric pH value in patients with reflux esophagitis remained at level 4 for an average of 13 and 17 hours, respectively, and more than 24 hours in patients with symptomatic reflux esophagitis. The number of patients whose gastric pH remained at 4 for 8, 12 and 16 hours after taking esomeprazole at a dose of 20 mg was 76, 54 and 24%, respectively, and when taking a dose of 40 mg - 97, 92 and 56 %. A pronounced clinical effect of esomeprazole at a dose of 40 mg in the treatment of reflux esophagitis after 4 weeks of treatment is observed in 70% of patients, and after 8 weeks of treatment - in 93%. The use of esomeprazole at a dose of 20 mg 2 times a day for 1 week in combination with appropriate antibiotics ensures successful eradication of Helicobacter pylori in approximately 90% of cases. After a week's use of the drug in a complex eradication regimen, there was no need for further antisecretory monotherapy for complete scarring of an uncomplicated duodenal ulcer and elimination of its symptoms. In a randomized, double-blind, placebo-controlled clinical trial, 764 patients with endoscopically confirmed peptic ulcer bleeding were randomized to receive Nexium infusion (n=375) or placebo (n=389). After endoscopic hemostasis, patients received either 80 mg esomeprazole as an IV infusion over 30 minutes followed by a continuous infusion at a dose of 8 mg/hour, or placebo for 72 hours. After an initial period of 72 hours, all patients received Nexium 40 mg orally - 27 days to suppress the acid-producing function of the stomach. The rate of rebleeding within 3 days was 5.9% in the IV Nexium group compared with 10.3% in the placebo group (p=0.0256). On the 7th and 30th days after treatment, the incidence of rebleeding in the group receiving Nexium, compared with the group receiving placebo, was 7.2 versus 12.9% (p = 0.0096) and 7.7 versus 13.6%, respectively (p=0.0092). During the period of antisecretory therapy, the concentration of gastrin in the blood plasma increases in response to a decrease in acid secretion. The increase in the number of endocrine histamine-producing cells, which was noted in some patients with long-term use of esomeprazole, may be due to an increase in the level of gastrin in the blood plasma. Several cases of increased incidence of gastric granular cysts have been reported with long-term use of antisecretory drugs. These phenomena are a physiological consequence of prolonged inhibition of the secretion of hydrochloric acid of a benign and reversible nature. Nexium, compared to ranitidine, is more effective in the treatment of gastric ulcers caused by the use of NSAIDs, including selective COX-2 inhibitors. The drug is also effective for the prevention of peptic ulcers of the stomach and duodenum in patients receiving NSAIDs (over 60 years of age and/or with a history of peptic ulcers). Esomeprazole is acid-labile and is administered orally in the form of enteric-coated granules. Conversion to the R-isomer in vivo is negligible. Esomeprazole is rapidly absorbed from the intestine, with maximum plasma concentrations achieved approximately 1–2 hours after oral administration. Absolute bioavailability after a single oral dose of 40 mg is 64% and increases to 89% with repeated doses; when used at a dose of 20 mg, it is 50 and 68%, respectively. The volume of distribution in healthy volunteers at steady state is 0.22 l/kg. About 97% of esomeprazole is bound to plasma proteins. Concomitant food intake slows down and reduces the absorption of esomeprazole, but this does not reduce the antisecretory effect of the drug. Esomeprazole is completely metabolized with the participation of the cytochrome P450 system. The main part of esomeprazole is metabolized with the participation of the polymorphic enzyme CYP 2C19, responsible for the formation of hydroxy- and desmethyl metabolites of esomeprazole, the rest is metabolized with the participation of the second isoform of the enzyme CYP 3A4, responsible for the formation of esomeprazole sulfone, the main metabolite of esomeprazole detected in blood plasma. The parameters given below primarily reflect the pharmacokinetics in individuals who extensively metabolize esomeprazole via the CYP 2C19 enzyme. The total clearance is about 17 l/h after a single dose and about 9 l/h after repeated use. The half-life is about 1.3 hours after repeated dosing of the drug once a day. The pharmacokinetics of esomeprazole were studied in doses up to 40 mg 2 times a day. The AUC value increases nonlinearly in a dose-dependent manner with repeated administration of esomeprazole. This time-dependent dose dependence is explained by a decrease in first-pass metabolism and systemic clearance due to inhibition of the CYP2C19 enzyme by esomeprazole or its sulfometabolite. Esomeprazole is completely eliminated from the blood plasma during the interdose period without a tendency to accumulate in the body when taking the drug once a day. The main metabolites of esomeprazole do not affect gastric secretion. About 80% of esomeprazole is excreted in the form of metabolites in the urine, the rest in the feces. Less than 1% is excreted unchanged in urine. Special groups of patients. Approximately 1–2% of patients have low CYP2C19 enzyme activity (so-called poor metabolizers). In these individuals, esomeprazole is metabolized primarily by CYP 3A4. When repeated dosing of esomeprazole 40 mg once daily, the mean AUC value in poor metabolizers is approximately 100% greater than in individuals with high CYP2C19 enzyme activity (extensive metabolizers); the maximum concentration in blood plasma increases by approximately 60%. This fact does not require changing the dose of the drug. The metabolism of esomeprazole does not change significantly in elderly patients (from 71 to 80 years). After a single dose of 40 mg esomeprazole, the average AUC in women is 30% greater than in men. No gender-related differences were noted during repeated appointments. This fact does not require dose adjustment of esomeprazole. The metabolism of esomeprazole in patients with mild to moderate hepatic impairment may not be affected. The metabolic rate is reduced in patients with severe liver dysfunction, which leads to a 2-fold increase in AUC, so the maximum dose of the drug for such patients should not exceed 20 mg/day. There was no tendency for accumulation of esomeprazole and its metabolites when taking the drug once a day. Studies have not been conducted in patients with impaired renal function. Since metabolites of esomeprazole, rather than the parent compound, are excreted by the kidneys, changes in the metabolism of the drug should not be expected in patients with impaired renal function. Adolescent patients After repeated administration of 20 and 40 mg esomeprazole, the overall effect and time to maximum plasma concentrations in adolescents aged 12–18 years were the same as in adults.

Treatment during pregnancy and lactation

No studies have been conducted on the effect of the drug on the fetus during pregnancy. Therefore, it is allowed to prescribe the drug for the treatment of various pathologies during pregnancy in cases where there are guarantees that the benefits to the woman’s body are significantly higher than the possible risks to the fetus.

There is no data on the passage of the active substance into breast milk, therefore, to minimize the risks to the newborn baby during the treatment period, it is recommended to stop breastfeeding.

Drug interactions Nexium tablets

Effect of esomeprazole on the pharmacokinetics of other drugs Reduced gastric acidity during treatment with esomeprazole can lead to increased or decreased absorption of other drugs, the mechanism of absorption of which depends on the acidity of the medium. With simultaneous use of esomeprazole (and other proton pump inhibitors or antacids), the absorption of ketoconazole and itraconazole is reduced. Esomeprazole is metabolized by CYP 2C19 and CYP 3A4 enzymes. The combined use of esomeprazole with other drugs in which CYP 2C19 is involved in the metabolism (diazepam, cytolopram, imipramine, clomipramine, phenytoin) may lead to an increase in the concentration of these drugs in the blood plasma and require a reduction in their dose. This must be taken into account, especially when prescribing esomeprazole according to indications. Concomitant use of 30 mg esomeprazole results in a 45% decrease in clearance of diazepam substrate. The combined use of 40 mg esomeprazole leads to an increase in plasma phenytoin levels by 13% in patients with epilepsy. It is recommended to monitor the concentration of phenytoin in the blood plasma when prescribing or discontinuing esomeprazole. When using Nexium and warfarin simultaneously, blood coagulation parameters should be monitored due to an increase in coagulation time. In healthy volunteers, co-administration of 40 mg esomeprazole with cisapride resulted in a 32% increase in AUC and a 31% increase in half-life, but no significant increase in the maximum plasma concentration of cisapride. A moderately prolonged QT on the ECG was observed after isolated administration of cisapride; subsequently, when cisapride was prescribed in combination with esomeprazole, the interval did not increase. When simultaneous administration of omeprazole (40 mg 1 time per day) with atazanavir (300 mg)/ritonavir (100 mg) in healthy volunteers, the concentration of atazanavir in the blood plasma significantly decreased (about 75% decrease in AUC, Cmax , Cmin ) . Increasing the atazanavir dose to 400 mg did not compensate for the effect of omeprazole on atazanavir concentrations. Proton pump inhibitors (including esomeprazole) should not be used in combination with atazanavir. Esomeprazole does not have a significant effect on the pharmacokinetics of amoxicillin or quinidine. With simultaneous short-term use of esomeprazole and naproxen or rofecoxib, no clinically significant interaction was detected. Effect of other drugs on the pharmacokinetics of esomeprazole When using esomeprazole and the CYP3A4 inhibitor clarithromycin (500 mg 2 times a day) simultaneously, an increase in the AUC of esomeprazole by 2 times was noted. The combined use of esomeprazole and voriconazole (a combined inhibitor of CYP 2C19 and CYP 3A4) may increase the exposure of esomeprazole by more than 2 times. In these cases, no dose adjustment of esomeprazole is required.

special instructions

Side effects when taking Nexium may mask symptoms of the development of cancer pathologies. Therefore, if vomiting and weight loss occur, you should definitely undergo additional examination.

With long-term use, it is necessary to ensure control over the patient's condition. If there are any negative reactions of the body, treatment is stopped. The doctor may prescribe a medicine with a different composition and similar effects.

The drug Nexium does not affect psychomotor reactions, therefore it has no restrictions when driving a car. Drinking alcohol significantly reduces the effectiveness of the drug.