Nexium

Nexium is a drug for the prevention and treatment of diseases of the digestive tract, caused by increased secretion of gastric juice and digestive enzymes. He refers to the inhibitors of so-called. proton pump

Nexium is available in three dosage forms: tablets, a lyophilisate for preparing a solution for intravenous administration, and enteric coated pellets for preparing an oral suspension.

The dose and frequency of use is determined by the attending physician depending on the disease, its severity and the individual characteristics of the patient.

Clinico-pharmacological group

Inhibitor H + -K + -ATP-ase.

Pharmacy sales terms

It is released on prescription.

Prices

How much does Nexium in pharmacies? The average price is at the level of 1 600 rubles.

Release form and composition

Nexium is available in the following dosage forms:

  • Tablets, coated: oblong, biconvex, on a break - white color with yellow impregnations; on 20 mg - light pink color, on one of the parties an engraving in the form of A / EH fraction, on another - "20 mG"; 40 mg each - pink, on one of the sides there is an engraving in the form of an A / EI fraction, on the other - 40 mG (7 pieces each in blisters, 1, 2 or 4 blisters in a cardboard box);
  • Pellets coated with an enteric coating and granules for the preparation of a suspension for oral administration: pale yellow, brown granules of various sizes can be found (3042.7 mg in triple laminated bags, 28 bags in a cardboard bundle);
  • Lyophilisate for preparation of the solution for intravenous administration: almost white or white compressed mass (in glass vials of 5 ml, 10 vials in paper tripods, 1 tripod in a cardboard bundle with the control of the first opening).

The composition of 1 tablet includes:

  • Active ingredient: esomeprazole - 20 or 40 mg (in the form of magnesium esomeprazole trihydrate - 22.3 or 44.5 mg);
  • Auxiliary components (tablets of 20/40 mg, respectively): sodium fumarate - 0.57 / 0.81 mg; macrogol - 3 / 4.3 mg; magnesium stearate - 1.2 / 1.7 mg; hyprolosis - 8.1 / 11 mg; glyceryl monostearate 40-55 - 1.7 / 2.3 mg; microcrystalline cellulose - 273/389 mg; hypromellose - 17/26 mg; red dye iron oxide (E172) - 0.06 / 0.45 mg; yellow dye iron oxide (E172) - 0.02 / 0 mg; copolymer (1: 1) of methacrylic and ethacrylic acid - 35/46 mg; paraffin - 0.2 / 0.3 mg; polysorbate 80 - 0.62 / 1.1 mg; triethyl citrate - 10/14 mg; Crospovidone - 5.7 / 8.1 mg; sugar, spherical granules (sucrose, spherical granules from 0.25 to 0.355 mm in size) - 28/30 mg; talc - 14/20 mg; titanium dioxide (E171) - 2.9 / 3.8 mg.

The composition of 1 package of pellets and granules include:

  • Active ingredient: esomeprazole - 10 mg (in the form of magnesium esomeprazole trihydrate - 11.1 mg);
  • Auxiliary components: anhydrous citric acid - 4.9 mg; hyprolosis - 32.2 mg; talc - 8.4 mg; copolymer (1: 1) of ethyl acrylate and methacrylic acid - 9.5 mg; sugar, spherical granules (sucrose, spherical granules of 0.25 to 0.355 mm in size) - 7.4 mg; hypromellose - 1.7 mg; dextrose - 2813 mg; magnesium stearate - 0.65 mg; triethyl citrate - 0.95 mg; glycerol monostearate 40-55 - 0.48 mg; Polysorbate 80 - 0.27 mg; xanthan gum - 75 mg; Crospovidone dye - 75 mg; iron oxide yellow - 1.8 mg.

The composition of 1 bottle of lyophilisate for the preparation of injection solution includes:

  • Active ingredient: esomeprazole - 40 mg (in the form of esomeprazole sodium - 42.5 mg);
  • Auxiliary components: edetate disodium dihydrate - 1.5 mg; sodium hydroxide - 0.2-1 mg.

Pharmacological effect

Nexium is the S-isomer of omeprazole, which reduces the secretion of hydrochloric acid in the stomach by inhibiting the proton pump in the parietal cells of the stomach

Esomeprazole is a weak base that becomes active in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa and inhibits the proton pump, the enzyme H + / K + - ATPase, and inhibition of both basal and stimulated secretion of hydrochloric acid occurs.

Indications for use

Coated tablets; enteric coated pellets and granules for the preparation of oral suspension

  1. Zollinger-Ellison syndrome or other conditions characterized by pathological hypersecretion of the gastric glands, including idiopathic hypersecretion.
  2. Gastroesophageal Reflux Disease (GERD): therapy of erosive reflux esophagitis; long-term maintenance therapy after healing of erosive reflux esophagitis (to prevent relapse); symptomatic GERD therapy;
  3. Peptic ulcer and duodenal ulcer;
  4. Duodenal ulcer associated with Helicobacter pylori (therapy in combination with other drugs);
  5. Peptic ulcer associated with Helicobacter pylori (prevention of relapse in combination with other drugs);
  6. The state after bleeding from peptic ulcers associated with the intravenous administration of drugs that lower the secretion of the gastric glands (prolonged acid suppression therapy and prevention of relapse);
  7. Gastric ulcer associated with long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) (therapy and prevention in patients at risk).

Nexium in the form of a lyophilisate is used as an alternative to oral therapy when it is not possible:

  1. Children and adolescents from 1 to 18 years: GERD with erosive reflux esophagitis and / or severe symptoms of reflux disease.
  2. Adults: GERD with esophagitis and / or severe symptoms of reflux disease; peptic ulcers associated with taking NSAIDs (treatment and prevention in patients at risk); bleeding from peptic ulcers after endoscopic hemostasis (prevention of relapse).

Contraindications

Before starting therapy, patients should carefully read the enclosed instructions. Tablets are contraindicated in the following cases:

  1. The age of children under 12 years of age due to the lack of clinical experience of use;
  2. Individual intolerance of the components included in the preparation;
  3. Hereditary intolerance to fructose;
  4. Renal failure severe forms of flow.

Use during pregnancy and lactation

An experimental study of the drug in animals did not reveal any negative effects on the fetus, but such tests were not carried out for understandable ethical reasons in pregnant women. That is why Nexium is not recommended for use during pregnancy. However, if there is a need to use the drug, then it can be taken by pregnant women only if the intended benefit exceeds all possible risks.

Since it is not known whether Nexium penetrates into breast milk, the drug should not be used during the entire breastfeeding period.

Dosage and method of use

The instructions for use indicate that Nexium in the form of tablets must be swallowed whole (without chewing or crushing), with a liquid. If swallowing is difficult, the tablet can be dissolved in 1/2 cup of non-carbonated water. To drink the resulting suspension of microgranules should be for 30 minutes, after which you need to refill the glass with 100 ml of water, stir the remainder of the preparation and drink.

Nexium in the form of granules and pellets for the preparation of suspensions for oral administration, as a rule, are prescribed to children and patients with difficulty swallowing. To obtain 10 mg of the drug, the contents of 1 package should be dissolved in 15 ml of water. The resulting solution must be stirred and wait a few minutes (until a suspension forms). The resulting suspension should be taken for 30 minutes, after which you need to refill the glass with the same volume of water, stir the residue and take it inside.

It is not necessary to use carbonated water to dissolve the preparation, as well as to crush or chew the microgranules.

Patients who cannot swallow, tablets dissolved in still water or obtained from the granules and pellet suspension are administered through a nasogastric tube.

It is recommended to use the following dosing regimen:

  1. Peptic ulcer and duodenal ulcer (simultaneously with other drugs) for eradication of Helicobacter pylori, as well as treatment of duodenal ulcer associated with Helicobacter pylori, and prevention of recurrence of peptic ulcers associated with this bacterium in patients with peptic ulcer (adults): 2 times day 20 mg Nexium, 500 mg clarithromycin and 1000 mg amoxicillin. Therapy is carried out for 7 days;
  2. Treatment of erosive reflux esophagitis (children 1-11 years old with a body weight of 10 kg, Nexium in the form of granules and pellets): a single dose for children weighing 10-20 kg is 10 mg, more than 20 kg - 10-20 mg. Reception frequency - once a day, duration of therapy - 8 weeks;
  3. Symptomatic treatment of gastroesophageal reflux disease (children 1-11 years old with a body weight of 10 kg, Nexium in the form of granules and pellets): 1 time per day, 10 mg for up to 8 weeks;
  4. Treatment of erosive reflux esophagitis (adults and children from 12 years): 1 time per day, 40 mg per month. An additional four-week course of treatment is recommended if the symptoms of the disease persist or if the esophagitis does not cure after the first course;
  5. Long-term maintenance therapy to prevent relapse (adults and children from 12 years of age): 20 mg 1 time per day;
  6. Symptomatic therapy of gastroesophageal reflux disease without esophagitis (adults and children from 12 years): 20 mg 1 time per day. If after a month of therapy the symptoms do not go away, it is necessary to conduct an additional examination. After improvement, it is possible to switch to the Nexium reception mode “as needed”, i.e. The drug is taken when symptoms occur before they are withdrawn in a daily dose of 20 mg in 1 dose. For patients taking nonsteroidal anti-inflammatory drugs, and patients who are at risk of developing gastric or duodenal ulcers, "on-demand" therapy is not recommended;
  7. Prolonged acid suppression therapy in patients who have undergone bleeding from peptic ulcers after intravenous use of antisecretory drugs for preventing relapse (adults): once a day, 40 mg for 30 days (after termination of intravenous therapy with antisecretory drugs);
  8. The healing of gastric ulcers associated with prolonged use of nonsteroidal anti-inflammatory drugs (adults): 1 time per day, 20 or 40 mg, the duration of the course is 1-2 months;
  9. Prevention of gastric and duodenal ulcers associated with taking nonsteroidal anti-inflammatory drugs: 1 time a day, 20 or 40 mg;
  10. Conditions characterized by pathological hypersecretion, including Zollinger-Ellison syndrome and idiopathic hypersecretion: the initial dose is 2 times a day, 40 mg. In the future, the dose is selected individually, the duration of the course is determined by the clinical picture of the disease.

Side effects

In patients not exceeding the prescribed dosages, side effects are rarely observed. With individual hypersensitivity, there is a likelihood of allergic reactions - pruritus and rash, angioedema, and bronchospasm.

Sometimes during the treatment of Nexium are noted:

  • intestinal candidiasis;
  • blurred vision;
  • hair loss;
  • increased skin sensitivity to solar ultraviolet;
  • erythema multiforme;
  • change in taste perception;
  • paresthesia;
  • high emotional lability:
  • depression;
  • headaches;
  • dyspeptic disorders;
  • intestinal dysfunctions (diarrhea or constipation);
  • general malaise and muscle weakness;
  • daytime sleepiness;
  • hyperhidrosis (excessive sweating);
  • dry mouth;
  • stomatitis;
  • painful swelling of the mammary glands;
  • hepatitis.

When liver failure is not excluded the development of encephalopathy.

Overdose

Very little data on cases of esomeprazole overdose. It is known that the use of Nexium at a dose of 80 mg does not cause any pronounced toxic effects. After using the drug at a dose of 280 mg, there is a general weakness, signs of disorders of the gastrointestinal tract.

Esomeprazole has no specific antidote. Hemodialysis is ineffective, since the drug is mostly bound to plasma proteins. In case of overdose symptoms, supportive and symptomatic therapy is carried out.

Special instructions

In rare cases, atrophic gastritis was detected by histological examination of biopsy specimens of the gastric mucosa in patients who had taken omeprazole for a long time.

If there are any alarming symptoms (for example, such as significant spontaneous weight loss, repeated vomiting, dysphagia, vomiting with blood or melena), as well as in the presence of a stomach ulcer (or if a stomach ulcer is suspected), the presence of a malignant neoplasm should be excluded, since Nexium treatment can smooth symptoms and delay diagnosis.

Nexium tablets contain sucrose, so they are contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency.

According to the research results, pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and esomeprazole (40 mg / day inside) is observed, which leads to a decrease in the active metabolite of clopidogrel by an average of 40% and a decrease in the maximum inhibition of ADP-induced platelet aggregation by an average of 14%. Therefore, the simultaneous use of esomeprazole and clopidogrel should be avoided (see the section "Interaction with other drugs and other types of drug interactions").

Separate observational studies indicate that proton pump inhibitor therapy may slightly increase the risk of osteoporosis-related fractures, but in other similar studies there has been no increase in risk.

In randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open-label studies of long-term therapy (more than 12 years), the connection of fractures against osteoporosis with the use of proton pump inhibitors was not confirmed.

Although the causal relationship between the use of omeprazole / esomeprazole and fractures against osteoporosis has not been established, patients at risk of developing osteoporosis or fractures against its background should be under appropriate clinical supervision.

Patients taking the drug for a long period (especially more than a year) should be under regular medical supervision. Patients taking Nexium “as needed” should be instructed to contact their physician when symptoms change. Taking into account fluctuations in the concentration of esomeprazole in plasma in the appointment of therapy "as needed", you should consider the interaction of the drug with other drugs (see the section "Interaction with other drugs and other types of drug interactions"). When prescribing Nexium for the eradication of Helicobacter pylori, the possibility of drug interactions for all components of triple therapy should be taken into account.Clarithromycin is a potent inhibitor of CYP3A4, so when prescribing eradication therapy to patients receiving other drugs metabolized with CYP3A4 (for example, cisapride), it is necessary to take into account possible contraindications and interactions of clarithromycin with these drugs.

Drug interactions

When using the drug, you must consider the interaction with other drugs:

  1. With care to combine the drug with warfarin and cisapride.
  2. The combination of esomeprazole with drugs such as ketoconazole and intraconazole may interfere with the absorption of drugs from the gastrointestinal tract.
  3. For people with epilepsy, should be treated with caution. Epilepsy medications (phenytoin) do not work well with Nexium.
  4. Simultaneous reception with the means in the assimilation of which is involved CYP2C19, will increase their impact. Such drugs include imipramine, diazepam, clomipramine, citalopram, phenytoin.
  5. Atazanavir, nelfinavir, omeprazole, when combined with Nexium, become less effective. However, when combined with saquinavir, its concentration in the serum increases.

Reviews

We picked up some reviews of people using the drug Nexium:

  1. Julia. She took “Nexium”, perfectly healed a duodenal ulcer. Side effects are not noticed. I was ready to pay any money, if only the medicine would help. Because living with constant nausea was difficult. I took 20 mg in the morning 30 minutes before a meal, and in the evening I just took 20 mg before bedtime. The drug goes well with antibiotics. And, as the doctor said, it is very important to take the medicine at the same time as the correctly chosen antibiotics, for example, with “Amoxicillin” and “Klabuksom”. Nausea and abdominal pain began to subside almost 2-3 days after taking the drug.
  2. Dmitriy. I have a standard set of stomach problems (gastritis, duonitis, etc.) - Nexium did not help me at all! Saw a full course (with add. Drugs - strictly on prescription) - the result is zero! My sincere advice to you all - before buying any expensive medicine from the Nexium / Pariet / Nolpaz series, etc. for the whole course, buy one package and see the reaction of your body, since different people have different reactions to different medicines (sorry for the banality), despite the similarity of the action of these medicines. And doctors, unfortunately, when they write out a particular brand, are often guided solely by their own monetary or other benefits derived from the manufacturers of these drugs.
  3. Marina. She was treated for a long time in the clinic for gastric ulcer and decided to go to a gastroenterologist in a private clinic. I was well investigated there and appointed Nexium. The first impression is expensive! The second impression helps in the same way as more simple (and cheap, respectively) medicines. I didn’t notice the special advantages of Nexium over previously taken drugs for ulcer disease ...

Analogs

In the pharmaceutical market there are drugs analogues and synonyms of Nexium. By synonyms include drugs containing the same active substance as Nexium. Analogs include drugs that have similar therapeutic effects, but contain a substance other than Nexium as an active ingredient.

The following drugs are synonymous with Nexium:

  • Neo-Zext;
  • Esomeprazole tablets;
  • Emanera capsules.

Analogs of Nexium are the following drugs:

  • Acrylans;
  • Vero Omeprazole;
  • Gastrosol;
  • Demeprazole;
  • Zhelkisol;
  • Zerocide;
  • Zipantola;
  • Zolispan;
  • Zolser;
  • Zulbex;
  • Kontrolok;
  • Crismel;
  • Crocicide;
  • Lanzabel;
  • Lanzap;
  • Lanzoptol;
  • Lansoprazole;
  • Lansofed;
  • Lantsid;
  • Losek;
  • Loenzar Sanovel;
  • Nolpaz;
  • Omez;
  • Omez Insta;
  • Omezol;
  • Omecaps;
  • Omeprazole;
  • Omeprus;
  • Omefez;
  • Omipix;
  • Ontime;
  • Orthanol;
  • Ozid;
  • Pantas;
  • Panum;
  • Pariet;
  • Peptazol;
  • Pepticum;
  • Promez;
  • Puloref;
  • Rabelok;
  • Rabeprazole;
  • Romesek;
  • Sanpraz;
  • Ulzol;
  • Ulcosol;
  • Ultra;
  • Ultop;
  • Hairabesol;
  • Helicide;
  • Helol;
  • Tsisagast;
  • Epicurus

Before using analogues consult your doctor.

Storage conditions and shelf life

Tablets and lyophilisate should be stored at a temperature not exceeding 30 ° C, pallets and granules - not more than 25 ° C. Keep out of the reach of children.

Shelf life of tablets, granules and pallets - 3 years, freeze-dried - 2 years. A bottle of powder without a cardboard bundle can be stored in room lighting for up to 24 hours.

Watch the video: Nexium overuse. Consumer Reports (January 2020).

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