Neksium

Neksium – the drug reducing secretion of hydrochloric acid in a stomach.

Form of release and structure

Neksium release in three dosage forms:

• Tablets, coated: biconvex, oblong, on a break – white with yellow impregnations; on 20 mg – light pink, with an engraving of "20 mG" on one of the parties, on another – "And / EN" in the form of fraction; on 40 mg – pink, with an engraving of "40 mG" on one of the parties, on another – "And / EI" in the form of fraction (in blisters on 7 pieces, on 1, 2 or 4 blisters in a cardboard pack);
• The granules and pellets covered with a kishechnorastvorimy cover for preparation of suspension for oral administration: various size, pale yellow, brownish granules can meet (in the triple laminated packages on 3042,7 mg, on 28 packages in a cardboard pack);
• Lyophilisate for preparation of solution for intravenous administration: the pressed mass of almost white or white color (on 5 ml in glass bottles, on 10 bottles in paper supports, on 1 support in a cardboard pack with control of the first opening).

Is a part of 1 tablet:

• Active agent: esomeprazole – 20 or 40 mg (in the form of magnesium esomeprazole trihydrate – 22,3 or 44,5 mg);
• Auxiliary components (20/40 mg respectively): glyceryl 40-55 monostearate – 1,7/2,3 mg, a hypro rod – 8,1/11 mg, a gipromelloza – 17/26 mg, dye iron oxide red (E172) – 0,06/0,45 mg, dye iron oxide yellow (E172) – 0,02/0 mg, microcrystallic cellulose – 273/389 mg, magnesium stearate – 1,2/1,7 mg, copolymer of etakrilovy and methacrylic acids (1:1) – 35/46 mg, paraffin – 0,2/0,3 mg, polysorbate 80 – 0,62/1,1 mg, a macrogoal – 3/4,3 mg, кросповидон – 5,7/8,1 mg, the stearylfumarating sodium – 0,57/0,81 mg, sucrose spherical granules (sugar, spherical granules of 0,25-0,355 mm in size) – 28/30 mg, titanium dioxide (E171) – 2,9/3,8 mg, talc – 14/20 mg, triethyl citrate – 10/14 mg.

Enters into structure of 1 package of granules and pellets:

• Active agent: esomeprazole – 10 mg (in the form of magnesium esomeprazole trihydrate – 11,1 mg);
• Auxiliary components: talc – 8,4 mg, a hypro rod – 32,2 mg, copolymer of ethyl acrylate and methacrylic acid (1:1) – 9,5 mg, sugar, spherical granules (sucrose, spherical granules of 0,250-0,355 mm in size) – 7,4 mg, a dextrose – 2813 mg, magnesium stearate – 0,65 mg, a gipromelloza – 1,7 mg, triethyl citrate – 0,95 mg, monostearate of a glitserol 40-55 – 0,48 mg, anhydrous citric acid – 4,9 mg, кросповидон – 75 mg, polysorbate of 80 - 0,27 mg, xanthane gum – 75 mg, dye iron oxide yellow – 1,8 mg.

For preparation of injection solution is a part of 1 bottle of lyophilisate:

• Active agent: esomeprazole – 40 mg (in the form of sodium esomeprazole – 42,5 mg);
• Auxiliary components: a dihydrate of an edetat of dinatrium – 1,5 mg, sodium hydroxide – 0,2-1 mg.

Indications to use

Granules and pellets for preparation of suspension for intake, a tablet

• Treatment erosive reflux esophagitis;
• The long supporting treatment at patients after healing erosive a reflux esophagitis (for the purpose of prevention of a recurrence);
• Symptomatic treatment of a gastroesophageal reflux disease;
• Therapy of an ulcer of the duodenum associated with Helikobakter of a pilora (Helicobacter pylori);
• Prevention of a recurrence of the pilora of a round ulcer associated with Helikobakter;
• Long kislotopodavlyayushchy treatment after the postponed bleedings from a round ulcer (after intravenous use of the drugs reducing secretion of glands of a stomach for prevention of a recurrence);
• Healing of the stomach ulcer connected with reception of non-steroidal anti-inflammatory drugs;
• Prevention of the stomach ulcer and duodenum tied with reception of non-steroidal anti-inflammatory drugs at the patients belonging to risk group;
• Zollingera-Ellison's syndrome or other states which are characterized by pathological hypersecretion (including idiopathic hypersecretion).

Lyophilisate for preparation of injection solution

Neksium in this dosage form appoint at impossibility of performing peroral therapy (as an alternative).

Adults should use drug in the presence of the following indications:

• Treatment of a gastroesophageal reflux disease at patients with an esophagitis and/or the expressed symptoms of a reflux disease;
• Healing of the round ulcers connected with reception of non-steroidal anti-inflammatory drugs;
• Prevention of the round ulcers connected with reception of non-steroidal anti-inflammatory drugs at the patients belonging to risk group;
• Prevention of a recurrence of bleeding from a round ulcer after carrying out an endoscopic hemostasis.

To children of 1-18 years Neksium appoint at a gastroesophageal reflux disease against the background of erosive a reflux esophagitis and/or the expressed symptoms of a reflux disease.

Contraindications

• Glyukozo-galaktozny malabsorption, hereditary intolerance of fructose, sakharazo-izomaltazny insufficiency (tablets, granules and pellets);
• Simultaneous use with atazanaviry and nelfinaviry;
• Hypersensitivity to drug components, and also to the replaced benzimidazoles.

Neksium patients should apply with care with heavy degree of a renal failure.

Depending on a dosage form, Neksium is contraindicated to children in the following cases:

• Tablets: age up to 12 years – all indications; age of 12-18 years – all indications, except a gastroesophageal reflux disease;
• Granules and pellets: age till 1 year or body weight less than 10 kg – all indications; age of 1-11 years – all indications, except an erosive esophagitis and a symptomatic treatment of a gastroesophageal reflux disease; age of 12-18 years – all indications, except a gastroesophageal reflux disease;
• Lyophilisate for preparation of injection solution: age till 1 year – all indications; age of 1-18 years – all indications, except a gastroesophageal reflux disease.

Pregnant women can appoint Neksium only after ratio assessment advantage/risk for health of mother and a fruit. During a lactation for therapy breastfeeding is recommended to be interrupted.

Route of administration and dosage

Granules and pellets for preparation of suspension for intake, a tablet

Neksium in the form of tablets it is necessary to swallow entirely (without chewing and without splitting up), washing down with liquid. At swallowing difficulty the tablet can be dissolved in 1/2 glasses of still water. It is necessary to drink the received suspension of microgranules for 30 minutes then it is necessary to fill once again a glass of 100 ml of water, to stir the remains of drug and to drink.

Neksium in the form of granules and pellets for preparation of suspension for oral administration, as a rule, appoint to children and patients with swallowing difficulty. For receiving 10 mg of drug contents of 1 package should be dissolved in 15 ml of water. The received solution needs to be stirred and waited several minutes (before formation of suspension). The received suspension should be accepted for 30 minutes then it is necessary to fill once again a glass with the same volume of water, to stir the remains and to accept inside.

To use sparkling water for drug dissolution, and also to split up or chew microgranules does not follow.

To patients who cannot swallow the tablets divorced in still water or the suspension received from granules and pellets are entered via the nazogastralny probe.

It is recommended to apply the following mode of dosing:

• Treatment erosive a reflux esophagitis (children of 1-11 years with body weight from 10 kg, Neksium in the form of granules and pellets): the single dose for children weighing 10-20 kg makes 10 mg, more than 20 kg – 10-20 mg. Frequency rate of reception – once a day, therapy duration – 8 weeks;
• Symptomatic treatment of a gastroesophageal reflux disease (children of 1-11 years with body weight from 10 kg, Neksium in the form of granules and pellets): once a day on 10 mg lasting up to 8 weeks;
• Treatment erosive a reflux esophagitis (adults and children of 12 years): once a day on 40 mg within a month. The additional four-week course of treatment is recommended to conduct at preservation of symptoms of a disease or if after the first course treatment of an esophagitis did not come;
• Long maintenance therapy for the purpose of prevention of a recurrence (adults and children of 12 years): on 20 mg once a day;
• Symptomatic therapy of a gastroesophageal reflux disease without esophagitis (adults and children of 12 years): on 20 mg once a day. If in a month of therapy symptoms do not pass, it is necessary to conduct additional examination. After improvement transition to the mode of reception of Neksium "as necessary" is possible, i.e. drug accept at emergence of symptoms before their removal in a daily dose 20 mg in 1 reception. For the patients accepting non-steroidal anti-inflammatory drugs and the patients belonging to risk group of development of stomach ulcer or a duodenum, therapy in the mode "as necessary" is not recommended;
• Peptic ulcer of a stomach and duodenum (along with other drugs) for an eradikation Helikobakter of a pilora, and also treatment of an ulcer of the duodenum associated with Helikobakter of a pilora and prevention of a recurrence of the round ulcers associated with this bacterium at patients with a peptic ulcer (adults): 2 times a day on 20 mg of Neksium, 500 mg of a klaritromitsin and 1000 mg of amoxicillin. Therapy is carried out for 7 days;
• Long kislotopodavlyayushchy therapy at the patients who had bleeding from a round ulcer after intravenous use of anti-secretory medicines for prevention of a recurrence (adults): once a day on 40 mg for 30 days (after the end of intravenous therapy by anti-secretory medicines);
• Healing of the stomach ulcers connected with long use of non-steroidal anti-inflammatory drugs (adults): once a day on 20 or 40 mg, course duration – 1-2 months;
• Prevention of the stomach ulcer and duodenum tied with reception of non-steroidal anti-inflammatory drugs: once a day on 20 or 40 mg;
• The states which are characterized by pathological hypersecretion including Zollingera-Ellison's syndrome and idiopathic hypersecretion: an initial dose – 2 times a day on 40 mg. Further the dose is selected individually, duration of a course is defined by a clinical picture of a disease.

Lyophilisate for preparation of injection solution

For dissolution of drug it is necessary to use only 0,9% chloride sodium solution.

Injection solution of Neksium should not be mixed or entered along with other drugs.

The drug is recommended to be administered right after its preparation. In need of it it is possible to store for 12 hours at a temperature up to 30 °C.

Intravenously Neksium appoint at impossibility of administration of drug inside, frequency rate of use – once a day.

The mode of dosing is defined by indications (daily dose):

• Treatment of an esophagitis at a gastroesophageal reflux disease: children of 1-11 years with body weight to 20 kg – 10 mg; children of 1-11 years with body weight from 20 kg – 10 or 20 mg; adults and children of 12 years – 40 mg;
• Symptomatic treatment of a gastroesophageal reflux disease: children of 1-11 years of-10 mg; adults and children of 12 years – 20 mg;
• Healing of the round ulcers connected with reception of non-steroidal anti-inflammatory drugs at the patients belonging to risk group: adult – 20 mg;
• Prevention of the round ulcers connected with reception of non-steroidal anti-inflammatory drugs: adult – 20 mg.

The period of parenteral use of Neksium is, as a rule, short, the patient is recommended to be transferred to administration of drug inside as soon as possible.

For prevention of a recurrence of bleeding from a round ulcer after carrying out an endoscopic hemostasis usually appoint 80 mg of Neksium in the form of intravenous infusion for 30 minutes with the subsequent prolonged intravenous infusion in a dose of 8 mg an hour for 72 hours. For suppression of secretion of acid after the end of parenteral use performing anti-secretory therapy is recommended (for example, esomeprazole on 40 mg for 1 month once a day).

Duration of introduction of Neksium makes:

• Intravenous injections: 10, 20 and 40 mg – of 3 minutes;
• Intravenous infusions: 10, 20 and 40 mg – 10-30 minutes; 80 mg – 30 minutes; 8 mg/h – 71,5 h (in the form of the prolonged infusion).

At bleeding from a round ulcer at patients with heavy functional disturbances of a liver Neksium appoint on 80 mg in the form of intravenous infusion within 30 minutes with the subsequent prolonged intravenous infusion in the maximum dose 4 mg an hour for 71,5 h.

At Neksium's appointment in all dosage forms dose adjustment is not required to patients with renal failures. With care use drug at patients with a renal failure.

Because of limited clinical experience by the patient with heavy degree of a renal failure Neksium it is necessary to appoint with care. The maximum daily dose at heavy degree of a liver failure adults and children of 12 years have to have no more than 20 mg, children have 1-11 years – no more than 10 mg.

Elderly patients should not adjust the dosing mode.

Side effects

• Nervous system: often – a headache; infrequently – paresthesias, dizziness, drowsiness; seldom – taste disturbance;
• Musculoskeletal system: seldom – a mialgiya, an arthralgia; very seldom – muscular weakness;
• Hemopoietic system: seldom – a leukopenia, thrombocytopenia; very seldom – a pancytopenia, an agranulocytosis;
• Urinary system: very seldom – intersticial nephrite;
• Respiratory system: seldom – a bronchospasm;
• Digestive tract: often – a lock, an abdominal pain, diarrhea, a meteorism, vomiting/nausea; infrequently – dryness in a mouth; seldom – digestive tract candidiasis, stomatitis; very seldom – the microscopic colitis confirmed with histologic researches;
• Skin and hypodermic fabrics: often – reactions in a drug injection site (at intravenous administration); infrequently – dermatitis, rash, an itch, urticaria; seldom – a photosensitization, an alopecia; very seldom – a toxic epidermal necrolysis, Stephens-Johnson's syndrome, a mnogoformny erythema;
• Mammary glands and reproductive system: very seldom – a gynecomastia;
• Liver and biliary tract: infrequently – increase in activity of liver enzymes; seldom – the hepatitis (which is followed by jaundice or without it); very seldom – a liver failure, encephalopathy at patients with liver diseases;
• Organ of sight: seldom – a sight illegibility;
• Mental disturbances: infrequently – sleeplessness; seldom – excitement, a depression, confusion; very seldom – an agressive behavior, hallucinations;
• Metabolism: seldom – a hyponatremia; very seldom – the hypomagnesiemia, a hypocalcemia (connected with a heavy hypomagnesiemia), the hypopotassemia (caused by a hypomagnesiemia);
• Allergic reactions: seldom – hypersensitivity reactions (in the form of fever, a Quincke's disease, anaphylactic reactions / an acute anaphylaxis);
• Others: infrequently – peripheral hypostases; seldom – perspiration, an indisposition.

At intravenous administration of Neksium by the patient in a critical state, in particular at introduction of high doses, development of an irreversible vision disorder is possible (relationship of cause and effect is not established with performing therapy).

Special instructions

At emergence of any alarming signs (in the form of considerable sudden loss of body weight, repeated vomiting, a dysphagy, vomiting with blood impurity), and also in the presence of stomach ulcer (or at suspicion of it) it is necessary to exclude existence of malignant new growths as Neksium's use can lead to smoothing of symptoms that will delay diagnosis.

When performing long-term treatment (in particular longer than year) patients have to undergo regular medical observation.

In cases of use of the drug "as necessary" it is necessary to inform the doctor on emergence of atypical symptoms.

During performing therapy for an eradikation Helikobakter pilor it is necessary to consider a possibility of medicinal interaction of all used drugs.

With high risk of development of changes or osteoporosis patients have to be under the corresponding clinical observation.

During therapy it is necessary to be careful at control of motor transport that it is connected with probability of development of such side effects as dizziness, drowsiness and an illegibility of sight.

Medicinal interaction

At simultaneous use of Neksium with some medicines there can be following effects:

• Ketokonazol, итраконазол, эрлотиниб: decrease in their absorption;
• Digoxin: increase in its absorption;
• Anti-retrovirus drugs (атазанавир, нелфинавир): decrease in their concentration in serum (the combination is not recommended);
• Sakvinavir: increase in its concentration in serum;
• Tsitalopram, diazepam, Imipraminum, Phenytoinum, кломипрамин and other drugs in which metabolism CYP2C19 isoenzyme takes part: increase in their concentration in plasma;
• Phenytoinum: increase in its residual concentration at patients with epilepsy;
• Takrolimus, methotrexate: increase in its concentration in blood serum;
• Drugs of the St. John's Wort which is made a hole rifampicin: decrease in concentration of esomeprazole in a blood plasma.

Terms and storage conditions

To store in the place, unavailable to children.

Period of validity:

• Tablets: 3 years at storage at a temperature up to 30 °C;
• Granules and pellets for preparation of suspension for oral administration: 3 years at storage at a temperature up to 25 °C;
• Lyophilisate for preparation of injection solution: 2 years at storage at a temperature up to 30 °C in the place protected from light. Without cardboard pack the bottle at room lighting can be stored till 24 o'clock.