Nexium - a drug that helps reduce the secretion of hydrochloric acid in the stomach.
Release form and composition
Nexium is available in the following dosage forms:
- 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);
- 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 side there is an engraving in the form of “A / EI” fraction, on the other side - “40 mG” (7 pieces in blisters, 1, 2 or 4 blisters in a carton box);
- Lyophilisate for preparation of the solution for intravenous administration: almost white or white compressed mass (in 5 ml glass vials, 10 vials each in paper tripods, 1 tripod per carton with the control of the first opening).
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 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 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: dihydrate edetate disodium - 1.5 mg; sodium hydroxide - 0.2-1 mg.
Indications for use
Tablets, suspension for oral administration.
- Erosive reflux esophagitis (treatment);
- Peptic ulcer associated with Helicobacter pylori (relapse prevention);
- Condition after healing of erosive reflux esophagitis (long-term supportive treatment with prophylactic purposes);
- Duodenal ulcer associated with Helicobacter pylori (treatment);
- State after suffering bleeding from peptic ulcers: after intravenous administration of drugs that lower the secretion of the gastric glands (long-term acid suppression therapy to prevent relapse);
- Gastroesophageal reflux disease (symptomatic treatment);
- A gastric ulcer associated with taking nonsteroidal anti-inflammatory drugs (healing treatment);
- Gastric and duodenal ulcer associated with nonsteroidal anti-inflammatory drugs (prevention in at-risk patients);
- Zollinger-Ellison syndrome or other conditions that are accompanied by pathological hypersecretion, including idiopathic hypersecretion (treatment).
Nexium in the form of an injection solution is used as an alternative when it is impossible to take the drug inside.
The solution is prescribed for adults with the following indications:
- Gastroesophageal reflux disease with esophagitis and / or severe signs of reflux disease (treatment);
- Peptic ulcers associated with taking nonsteroidal anti-inflammatory drugs (prevention in at-risk patients);
- Peptic ulcers associated with the use of nonsteroidal anti-inflammatory drugs (treatment for the purpose of healing);
- Bleeding from peptic ulcers after endoscopic hemostasis (prevention of relapse).
Children 1-18 years old Nexium is prescribed for gastroesophageal reflux disease on the background of erosive reflux esophagitis and / or severe symptoms of reflux disease.
- Glucose-galactose malabsorption, sucrase-isomaltase deficiency, hereditary fructose intolerance (tablets, oral suspension);
- Combined use with nelfinavir and atazanavir;
- Hypersensitivity to the components of the drug, as well as to substituted benzimidazoles.
Nexium should be used with caution in case of severe renal failure.
Children, depending on the dosage form, the drug is prescribed:
- Suspension for oral administration: from 1 year old (with a body weight of not less than 10 kg) in the treatment of erosive esophagitis and symptomatic therapy of gastroesophageal reflux disease; from the age of 12 in the treatment of gastroesophageal reflux disease;
- Tablets: from 12 years in the treatment of gastroesophageal reflux disease;
- Injection solution: from 1 year in the treatment of gastroesophageal reflux disease.
In pregnancy, Nexium can be prescribed only after the doctor has assessed the ratio of the health benefits of the mother to the risk to the fetus. If necessary, the use of the drug during lactation, breastfeeding should be interrupted.
Dosing and Administration
Tablets, suspension for oral administration.
Nexium tablets are swallowed whole (without crushing and not chewing), with a liquid. When swallowing is difficult, a single dose of the drug can be dissolved in 1/2 cup of non-carbonated water. The resulting suspension of microgranules should be drunk for 30 minutes, then the glass should be refilled with 100 ml of water and drink the suspension with the remnants of the dissolved tablet.
Granules and pellets for the preparation of suspensions for oral administration Nexium is prescribed, as a rule, for children and patients who have problems with swallowing. To get 10 mg, the contents of 1 package must be dissolved in 15 ml of water. Before taking you need to wait a few minutes before the formation of a suspension. The resulting suspension should be taken within 30 minutes, then the glass should be refilled with the same volume of water and drink a suspension with the remnants of the dissolved granules. It is not necessary to use soda water to obtain a suspension, as well as to chew or crush the microgranules.
When swallowing is difficult, diluted tablets or suspensions are administered through a nasogastric tube.
It is recommended to adhere to the following dosing regimen:
- Erosive reflux esophagitis (treatment; prescribed for children 1-11 years old with a body weight of 10 kg in oral dosage form): single dose for children with a body weight of 10-20 kg - 10 mg, more than 20 kg - 10-20 mg, the multiplicity of use - 1 time per day, the duration of the course - 8 weeks;
- Erosive reflux esophagitis (treatment; prescribed for adults and children from 12 years old): single dose - 40 mg, frequency of use - 1 time per day, course duration - 4 weeks. An additional course of the same duration is possible if the symptoms of the disease persist or if the cure of esophagitis does not occur after one course;
- Erosive reflux esophagitis (prolonged supportive therapy after healing to prevent relapse; prescribed for adults and children from 12 years of age): single dose - 20 mg, frequency of use - 1 time per day;
- Gastroesophageal reflux disease (symptomatic treatment; prescribed for children 1-11 years old with a body weight of 10 kg in oral dosage form): single dose - 10 mg, frequency of application - 1 time per day, course duration - up to 8 weeks;
- Gastroesophageal reflux disease without esophagitis (symptomatic therapy; prescribed for adults and children over 12 years old): single dose - 20 mg, frequency of application - 1 time per day. If after a month from the start of treatment the symptoms persist, an additional examination is recommended. After improving the state, it is possible to switch to the Nexium use mode “as needed”, which involves taking the drug if symptoms of the disease occur before their removal in a single dose of 20 mg with a dose rate once a day. For patients taking nonsteroidal anti-inflammatory drugs and patients who are at risk of developing stomach ulcers or duodenal ulcers, the “on-demand” therapy is not recommended;
- Peptic ulcer and duodenal ulcer for eradication of Helicobacter pylori, as well as duodenal ulcer associated with Helicobacter pylori (combination therapy, as well as prevention of peptic ulcers associated with this bacterium in patients with peptic ulcer disease; they are prescribed for adults): Nexium - Necium - 21% clarithromycin - 500 mg, amoxicillin - 100 mg, the frequency of each medication - 2 times a day, the course duration - 7 days;
- Conditions after bleeding from peptic ulcers after intravenous use of antisecretory drugs (long-term acid suppression therapy and prevention of relapse; prescribed for adults): single dose - 40 mg, frequency of use - 1 time per day, course duration - 30 days;
- Gastric ulcer associated with prolonged use of nonsteroidal anti-inflammatory drugs (treatment for the purpose of healing; prescribed for adults): single dose - 20 or 40 mg, the frequency of application - 1 time per day, the course duration - 1-2 months;
- Gastric and duodenal ulcer associated with nonsteroidal anti-inflammatory drugs (prevention; prescribed for adults): single dose - 20 or 40 mg, the frequency of application - 1 time per day;
- Conditions characterized by pathological hypersecretion, including idiopathic hypersecretion and Zollinger-Ellison syndrome: the initial single dose is 40 mg (the dose is selected individually), the frequency of use is 2 times a day, the duration of the course is determined by the clinical picture of the disease.
Intravenous administration of the drug is indicated when it is impossible to ingest Parenteral administration of Nexium, as a rule, is short-lived, and it is recommended that the patient be transferred as soon as possible to receive the drug in the form of a suspension or tablets.
To dissolve the lyophilisate, you can use only 0.9% sodium chloride solution. It is recommended to introduce the drug immediately after its preparation. If necessary, it can be stored at temperatures up to 30 ° C for 12 hours.
Mixing or injecting Nexium injecting solution along with other drugs should not be.
The dosage regimen is determined by the indications (daily dose with a frequency of use 1 time per day):
- Esophagitis with gastroesophageal reflux disease (treatment): children of 1-11 years old weighing up to 20 kg - 10 mg, children of 1-11 years old weighing 20 kg - 10 or 20 mg, children of 12 years old and adults - 40 mg;
- Gastroesophageal reflux disease (symptomatic treatment): children 1-11 years old –10 mg, children over 12 years old and adults 20 mg;
- Peptic ulcers associated with taking nonsteroidal anti-inflammatory drugs (treatment for the purpose of healing): adults - 20 mg;
- Peptic ulcers associated with taking nonsteroidal anti-inflammatory drugs (prevention): adults - 20 mg.
In order to prevent recurrence of bleeding from peptic ulcers after endoscopic hemostasis, as a rule, 80 mg of Nexium is used as an intravenous infusion for 30 minutes, followed by a prolonged intravenous infusion at a dose of 8 mg per hour for 72 hours. To suppress the secretion of acid after the end of parenteral administration of the drug, it is recommended to conduct antisecretory therapy (for example, for 1 month, esomeprazole 40 mg once a day).
The duration of the introduction of Nexium is:
- Intravenous injections: at a dose of 10, 20 and 40 mg - from 3 minutes;
- Intravenous infusions: at a dose of 10, 20 and 40 mg - 10-30 minutes; 80 mg - 30 minutes; 8 mg / h - 71.5 hours (prolonged infusion).
When bleeding from peptic ulcers in patients with functional disorders of the liver in severe form, Nexium is prescribed 80 mg as an intravenous infusion for 30 minutes, followed by a prolonged intravenous infusion at a maximum dose of 4 mg per hour for 71.5 hours.
Adjust the dosing regimen in elderly patients should not be.
In case of impaired renal function during the use of Nexium in any dosage form, the dose should not be adjusted. Patients with renal insufficiency, the drug is prescribed with caution.
Due to limited clinical experience, Nexium patients with severe degrees of liver failure must be prescribed with caution. The maximum daily dose in adults and children from 12 years should not be more than 20 mg, in children 1-11 years old - 10 mg.
- Musculoskeletal system: rarely - myalgia, arthralgia; very rarely, muscle weakness;
- Nervous system: often - headache; infrequently - drowsiness, paresthesia, dizziness; rarely - a violation of taste;
- Urinary system: very rarely - interstitial nephritis;
- Blood system: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia;
- Gastrointestinal system: often - vomiting and / or nausea, constipation, abdominal pain, flatulence, diarrhea; infrequently - dry mouth; rarely - stomatitis, gastrointestinal candidiasis; very rarely - microscopic colitis confirmed by histological studies;
- Respiratory system: rarely - bronchospasm;
- The reproductive system and mammary glands: very rarely - gynecomastia;
- Skin and subcutaneous tissues: often - reactions at the injection site (for intravenous administration); infrequently - itching, dermatitis, rash, urticaria; rarely - photosensitivity, alopecia; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme;
- Organ of vision: rarely - blurred vision;
- Liver and biliary tract: infrequently - increased activity of liver enzymes; rarely, hepatitis (with or without jaundice); very rarely - liver failure, encephalopathy in patients with liver disease;
- Mental disorders: infrequently - insomnia; rarely - depression, agitation, confusion; very rarely - hallucinations, aggressive behavior;
- Allergic reactions: rarely - hypersensitivity reactions (in the form of fever, angioedema, anaphylactic shock and / or anaphylactic reactions);
- Metabolism: rarely - hyponatremia; very rarely - hypomagnesaemia, hypocalcemia associated with severe hypomagnesemia, hypokalemia associated with hypomagnesemia;
- Other: infrequent - peripheral edema; rarely - indisposition, sweating.
In critically ill patients, intravenous administration of Nexium, especially when using high doses, may develop irreversible visual impairment (a causal link with therapy has not been established).
When conducting long-term therapy (especially longer than 12 months), patients need to undergo regular medical examination.
With the development of any warning signs (vomiting with blood, repeated vomiting, dysphagia, significant sudden weight loss), as well as with a stomach ulcer (or in case of suspicion of it), the presence of malignant neoplasms should be excluded, since the treatment with Nexium due to the smoothing of symptoms may lead to a delay in diagnosis.
When conducting a combined treatment with Helicobacter pylori, it is necessary to take into account the possibility of drug interactions of all the drugs used.
If there is a high risk of osteoporosis or fractures, the condition of the patients requires careful monitoring.
When using Nexium, care must be taken when driving vehicles, as during therapy dizziness, blurred vision and drowsiness may develop.
With the joint appointment of Nexium with some drugs may develop the following effects:
- Digoxin: increase its absorption;
- Rifampicin, drugs Hypericum perforatum: a decrease in the concentration of esomeprazole in the blood plasma;
- Itraconazole, ketoconazole, erlotinib: a decrease in their absorption;
- Saquinavir, methotrexate, tacrolimus: an increase in their concentration in serum;
- Antiretroviral drugs (nelfinavir, atazanavir): a decrease in their concentration in serum (simultaneous use is not recommended);
- Clomipramine, citalopram, diazepam, phenytoin, imipramine, and other drugs whose metabolism involves the CYP2C19 isoenzyme: an increase in their plasma concentration;
- Phenytoin: an increase in its residual concentration in patients with epilepsy.
Terms and conditions of storage
Keep out of the reach of children.
- Granules and pellets for suspension for oral administration: 3 years at storage temperatures up to 25 ° C;
- Tablets: 3 years at storage temperatures up to 30 ° C;
- Lyophilisate for preparing injection solution: 2 years at a storage temperature of up to 30 ° C in a dark place. A bottle with the drug in room lighting without cardboard packaging can be stored for up to 24 hours.