Nexium 20mg #14 tablet

Nexium 20mg #14 tablet

Nexium  annotation
(nexium)

International non-proprietary name: esomeprazole

Pharmaceutical form: coated tablets

Composition
Each tablet contains:
Active substances: 22.3 mg or 44.5 mg of esomeprazole magnesium trihydrate, which corresponds to 20 mg and 40 mg of esomeprazole.
Excipients: glycerol monostearite 40-55, oxypropyl cellulose, cypromellose, iron oxide, red-brown color (E172), magnesium stearate, co-polymer of methacrylic acid with ethyl acrylate (1:1) 30% dispersion, microcrystalline cellulose, synthetic paraffin, nicrogol, polysorbate 80, cropovidone , sodium stearyl fumarate, safari spherical granules (starch and corn starch), talc, titanium dioxide (E 171) 77 triethyl citrate.

Description: 20 mg tablets: pale pink, oblong biconvex tablets, film-coated, engraved with “20 mg” on one side and A on the other side.
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40 mg tablets: pink oblong biconvex tablets, coated with garcite, engraved with “40 mg” on one side and A on the other side
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Pharmacotherapeutic group: proton pump inhibitor
Code: ATX: A02BC05

Pharmacological properties
Pharmacodynamics.
Esomeprazole is the S-isomer of omeprazole; Reduces gastric acid secretion by specific inhibition of the proton pump in parietal cells. The S- and R-isomers of omeprazole have similar pharmacodynamic activity.
mechanism of action.
Esomeprazole is a weak base, and in the acidic environment of the secretory channels of the parietal cells of the gastric mucosa, it is converted into an active form.
Effect on gastric acid secretion.
The effect of esomeprazole develops within 1 hour after oral administration of 20 mg or 40 mg. During daily intake of the drug for 5 days at a dose of 20 mg once a day, the average maximum concentration of acid after stimulation with pentagastrin decreases by 90% (measurement of acid concentration 6-7 hours after taking the dose on the 5th day of therapy). After 5 days of oral daily administration of esomeprazole at a dose of 20 mg or 40 mg, pH in the stomach was greater than 4 for an average of 13 and 17 hours out of 24 hours during daily monitoring, respectively, in patients with symptomatic gastro-esophageal reflux disease. Among patients who receive 20 mg of esomeprazole per day, the registration of acidity at the level of PH more than 4 for 8, 12 and 16 hours is achieved in 76%, 54% and 24, respectively. For 40 mg esomeprazole, this ratio is 97%, 92% and 56%, respectively. A correlation between acid secretion and the concentration of the drug in the plasma has been revealed (the AUC parameter was used to estimate the concentration). Therapeutic effect achieved as a result of inhibition of acid secretion. Treatment of reflux esophagitis with Nexum 40 mg dose is approximately 78% after 4 weeks of therapy and 93% after 8 weeks of therapy. Treatment with Nexum at a dose of 20 mg 2 times a day in combination with appropriate antibiotics for a week gives a successful result in the form of Helicobacter pylori eradication in about 90% of patients.
Patients without duodenal ulcer complications after a one-week eradication course do not require further monotherapy with antisecretory drugs for ulcer healing and symptom relief. Other effects related to inhibition of acid secretion. During treatment with anti-secretory drugs, gastrin level in plasma increases as a result of decreased acid secretion. In patients who have been taking antisecretory drugs for a long time, the formation of a glandular cyst in the stomach is often observed, which occurs independently on the background of continued therapy. These events are due to physiological changes as a result of inhibition of acid secretion. Nexium with ranitidine in two comparative studies in patients receiving non-steroidal anti-inflammatory therapy including Tsog-2 selective non-steroidal anti-inflammatory drugs (NSAIDs) showed better efficacy in healing peptic ulcers. In two studies, Nexium showed better efficacy in preventing peptic ulcers in patients receiving anti-inflammatory NSAIDs (age group 60 years and above and/or with a history of peptic ulcer), including the use of group-2 selective NSAIDs (NSAIDs). .
Pharmacokinetics.

absorption and distribution. Esomeprazole acid is unstable in the environment, therefore tablets are used for oral use, which contain granules covered with a coating of the drug resistant to the action of gastric juice. Under in vivo conditions, only a minor part of esomeprazole is converted into R-isomers. The drug is quickly absorbed: the maximum concentrations in the plasma will be reached after 1-2 hours. The absolute bioavailability of esomeprazole after a single dose of 40 mg is 64% and increases to 9% after daily administration once a day. For a dose of 20 mg of esomeprazole, these figures are 50% and 68%, respectively. From this, the volume of distribution in healthy people with equilibrium concentration is approximately 0.22 L/kg of body weight. Esomeprazole is 97% bound to plasma proteins. Food intake slows down and accelerates the absorption of esomeprazole in the stomach.
Metabolism and excretion
Esomeprazole undergoes metabolism with the participation of the cytochrome P450 (CYP) system, with the formation of hydroxy and demethylated metabolites of esomeprazole. The remainder is metabolized by another specific isoform, CYP3A4; At the same time, sulfonated derivatives of esomeprazole are formed, which are the main metabolite and which are determined in plasma. The following parameters reflect the nature of pharmacokinetics mainly in patients with active CYP2C19 activity (patients with active metabolism). The general clearance after single administration of the drug is about 17 l/h and 9 l/h after multiple administration. The half-life is 1.3 hours, with systematic intake once a day. The area under the “concentration-time” curve (AUC) increases in a dose-dependent manner during regular administration and is expressed in a non-linear relationship between dose and AUC. Such time and dose dependence is the result of decreased metabolism during the “first pass” in the liver, as well as decreased systemic clearance, which is probably caused by esomeprazole and/or its sulfonated metabolite inhibiting the CYP2C19 enzyme.
During a single daily administration, esomeprazole is completely removed from the blood plasma during the break between administrations and does not accumulate. None of the major metabolites of esomeprazole affect gastric acid secretion. During oral administration, up to 80% of the dose is excreted in the form of metabolites with urine, and the remaining amount with feces. Less than 1% of unchanged esomeprazole is found in urine. Features of pharmacokinetics In some groups of patients, approximately 1-2% of the population, the CYP2C19 enzyme is slightly active (patients with inactive metabolism), in such patients, the metabolism of esomeprazole is mainly carried out as a result of the action of CYP3A4. During the systematic administration of 40 mg of esomeprazole once a day, the average AUC exceeds the value of this parameter by 100% in patients with an active CYP2C19 enzyme (patients with rapid metabolism). The average value of maximum concentrations in plasma of patients with slow metabolism is increased by about 60%. In elderly patients (71-81 years), the metabolism of esomeprazole does not undergo significant changes. After a single dose of 40 mg of esomeprazole in women, the average AUC exceeds the same figure in men by 30%. Subsequently, during systematic daily administration of the drug once a day in patients of both sexes, there is no difference in pharmacokinetics (the specified difference does not affect the dosage regimen of the drug). Esomeprazole metabolism may be disturbed in patients with moderate or moderate severity of liver failure. In patients with a severe form of liver failure, the rate of metabolism is reduced, which increases the AUC of esomeprazole by 2 times. The study of pharmacokinetics in patients with renal failure was not carried out, because it is not esomeprazole itself that is excreted through the kidneys, but its metabolites, which is why it can be considered that the metabolism of esomeprazole in patients with renal failure does not change.

testimonials
Gastro-esophageal reflex
– treatment of erosive reflux – esophagitis;
– Long-term adjuvant treatment to prevent relapses of patients with erosive reflux –
were suffering from esophagitis;
– Symptomatic treatment of gastroesophageal reflux. As part of the combined therapy of gastric and duodenal ulcer disease:
– Treatment of duodenal ulcer associated with Helicobacter pylori
– Prevention and treatment of peptic ulcers in patients with ulcer diseases. Patients who have been taking long-term non-steroidal anti-inflammatory drugs (NSAIDs):
– Healing of peptic ulcers associated with taking ASAP.
– Prevention of ulcer healing associated with taking ASAP.

Contraindications
Hypersensitivity to esomeprazole, when benzimidazole or other ingredients of the medicinal form of the drug were used instead of esomeprazole. Patients with hereditary fructose intolerance, glucogalactose malabsorption or sucrose-isomaltase deficiency.
Children’s age – due to the lack of data on the effectiveness and safety of taking the drug in a given group of patients.
With caution – severe renal failure (use is limited)

Method of use and doses
taking medicine The tablet should be taken whole, followed by liquid. Do not chew or crush the tablet. For patients who have difficulty swallowing, the tablet can be diluted with still water up to half a glass (no other liquid can be used, because the protective coating of the microgranules can be opened), stir until the tablet dissolves, after which the microgranules tube should be drunk immediately or within 30 minutes, then refill the glass Halfway through, stir in the leftovers and drink. Microgranules cannot be chewed or crushed. For patients who cannot swallow, the tablets should be diluted in still water and administered through a nasogastric tube. It is very important that the selected syringe and probe be carefully tested. Instructions for preparation of the drug and administration by nasogastric tube. see In the section “Drug administration by nasogastric tube”.
Gastroesophageal reflux
Treatment of erosive reflux – esophagitis: 40 mg once daily for 4 weeks. A 4-week course of additional treatment is recommended in cases where esophagitis does not improve or symptoms do not disappear after the first course.
Erosive reflux – long-term supportive treatment of patients with left oesophagitis to prevent relapse: 20 mg once daily.
Symptomatic treatment of gastro-esophageal reflux: 20 mg once daily for patients without esophagitis. If the symptoms do not disappear after 4 weeks of treatment, additional examination of the patient should be carried out. After the symptoms disappear, you can switch to the medication regimen, the so-called “In times of need”, i.e. When symptoms develop, 20 mg of Nexium is taken once a day until they disappear.
Stomach and duodenal ulcer disease
For the eradication of Helicobacter pylori as part of combined therapy, and also:
– Treatment of duodenal ulcer associated with Helicobacter pylori: Nexium 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All drugs are used twice a day for 1 week.
Patients who used ASAP for a long time:
– Healing of peptic ulcer associated with taking ASAP: Nexium 20 mg once a day. Duration of treatment is 4-8 weeks.
– Prophylaxis of peptic ulcers, healing of peptic ulcers associated with taking ASAP: Nexium 20 mg once
per day.

Renal failure: No dose adjustment is required, but the use of Nexium in severe renal failure patients is limited; In this regard, caution should be observed when prescribing the drug for such patients (see section
Liver failure: in mild or moderate liver failure, the dose of the drug does not need to be adjusted. Patients with severe liver failure should not exceed the maximum dose of 20 mg per day.
Elderly patients: the dose of the drug does not need to be adjusted.

Side effects.
Below are side effects that do not depend on the dose of the drug.
Common (>1/100, <1/10) __ headache, abdominal pain, diarrhea, flatulence, nausea, vomiting, constipation, dermatitis, itching, urticaria, dizziness, dry mouth, allergic reactions;
less frequent (>1/1000, <1/100) __ angioedema, anaphylactic reaction, increased activity of “liver” enzymes,
Rare (>1/10000, <1/1000) __ Blurred vision, Stevens-Johnson syndrome, exfoliative erythema multiforme, myalgia
The following side effects have been observed with the use of the racemic drug (omeprazole) and can also be expected with the use of esomeprazole.
Central and peripheral nervous system
Paresthesia, drowsiness, insomnia, dizziness, clouding of consciousness, anxiety, agitation, depression, hallucinations (mainly in weakened patients).
Endocrine system: gynecomastia
Gastrointestinal tract: stomatitis and gastrointestinal candidiasis
Hematology
Leukopenia, thrombocytopenia, agranulocytosis and pancytopenia.
liver
“Increased activity of liver enzymes, encephalopathy in patients with long-term severe liver diseases; Hepatitis with (or without) jaundice, liver failure.
Musculoskeletal joint pain, muscle weakness
the skin
Rash, photosensitisation, toxic epidermal necrolysis, alopecia Toxic epidermal necrolysis, alopecia
other
General weakness, increased sweating, peripheral edema, altered taste and hyponatremia.
Allergic reactions
Fever, bronchospasm, interstitial nephritis and anaphylactic shock.

overdose.
Currently, very rare cases of intentional overdose have been described. In the symptoms described when taking esomeprazole at a dose of 280 mg, there was general weakness and dysfunction of the gastrointestinal tract. A single dose of 80 mg Nixium did not cause any adverse effects. No specific antidotes are known. Esomeprazole forms complexes with plasma proteins, so dialysis is less effective, in case of overdose it is necessary to carry out symptomatic and general supportive treatment.

Interaction with other medicinal products and other interactions
Effects of esomeprazole on the pharmacokinetics of other drugs. A decrease in the acidity of gastric juice during treatment with esomeprazole can be combined with a change in the absorption of the drug, the absorption of which depends on the acidity of the environment. Esomeprazole inhibits cYP2C19 – the main enzyme involved in its metabolism. Therefore, the joint use of esomeprazole with other drugs, in the metabolism of which CYP2C19 participates, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., can lead to an increase in the concentration of these drugs in plasma, which, in turn, leads to the need to reduce the dose. This phenomenon is especially pronounced when using Nexium in the “as needed” mode. When taking 30 mg of esomeprazole and diazepam together, the clearance of the enzyme-substrate complex (CYP2C19-diazepam) decreases by 45%. The minimum concentrations of phenytoin in the plasma of patients with epilepsy increased by 13% when it was combined with 40 mg of esomeprazole. In this regard, it is recommended to control the concentration of phenytoin in the plasma at the beginning of treatment with esomeprazole and during its discontinuation. Concomitant administration of warfarin 40 mg with esomeprazole did not change the coagulation time in patients receiving long-term warfarin, but there were several cases of clinically significant increases in the MHO SNU index (international normalized ratio) during the co-administration of warfarin and esomeprazole. In this regard, it is recommended to monitor patients at the beginning and end of the combined use of this drug. Cisapride concentrations did not change significantly at this time. The slight prolongation of the QT interval observed with cisapride monotherapy was not increased by the addition of Nexium (see the section “Special indications”). Nesxium does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine. Studies evaluating the co-administration of esomeprazole with naproxen or rofecoxib have not revealed clinically significant pharmacokinetic interactions. Effect of medicinal products on the pharmacokinetics of esomeprazole. CYP2C9 and CYP3A4 are involved in the metabolism of esomeprazole. Co-administration of esomeprazole with clarithromycin (500 mg twice a day), which inhibits CYP3A4, increases the AUC exposure of esomeprazole by 2 times. In this case, the dose of esomeprazole does not require correction.

Special instructions.
Before starting treatment with esomeprazole, the possibility of a malignant neoplasm should be excluded, because the treatment may lead to a reduction of symptoms and a delay in the diagnosis. Patients who take the drug for a long time (especially for more than a year) should be under the regular supervision of a doctor. Patients on “as needed” therapy should be instructed to contact their physician if symptoms change. Attention is paid to the variability of the concentration of esomeprazole in plasma when prescribing therapy “as needed”, the interaction of the drug with other drugs should be taken into account (see the chapter “Interaction with other drugs and other types of interaction”).
When prescribing Nexium for the eradication of Helicobacter pylori, the possibility of therapeutic interaction for all components of triple therapy should be taken into account.

Use during pregnancy and lactation
So far, we have not found enough data on the use of Nexium during pregnancy. The results of epidemiological studies conducted on omeprazole (which is a racemic mixture) revealed the absence of phototoxic action or disturbance of fetal development. No direct or indirect adverse effects on embryo or fetal development were observed when esomeprazole was administered to animals. Administration of the drug also did not have negative effects on animals during pregnancy, parturition and postnatal development. The drug should be prescribed to pregnant women only if the expected benefit to the mother exceeds the possible risk to the fetus. It is not known whether esomeprazole is excreted in breast milk, so Nexium is not prescribed during breastfeeding.

Influence on the ability to drive a car and other mechanisms.
The drug does not affect the ability to drive a car or use mechanisms.

release form.
7 tablets in a blister. One, two or four blisters with instructions for use in a cardboard pack.

Storage conditions.
At a temperature no higher than 30°C, in the original packaging, out of the reach of children. Shelf life. Do not use within 3 years of the expiration date, which is indicated on the package.

Dispensing conditions from the pharmacy.
dispensing by prescription.

Company – manufacturer. Astrazenek AB, SE-151 85 Södertälä, Sweden.
Additional information will be provided at the address, 11 9021 Moscow,
Temur Frunze st. S. 11, you. 205.

Administration of the drug through a nasogastric probe
When prescribing the drug with a nasogastric tube.
1. Place the tablet in the syringe and fill the syringe with 25 ml of water and about 5 ml of air. For some probes it can
It is necessary to dilute the drug in 50 ml of drinking water in order not to clog the probe with tablet granules.
2. Immediately shake the syringe for about two minutes to dissolve the tablet.
3. Hold the syringe with the cap and make sure that the cap is not jammed.
4. Insert the tip of the syringe into the probe and hold it upright.
5. Shake the syringe and turn it upside down. Immediately inject 5-10 ml of the dissolved drug into the probe. After injection, return the probe to its previous position and shake it (the syringe should be held with the cap up, to avoid jamming the cap
to prevent).
6. Turn the syringe upside down and inject another 5-10 ml of the drug into the tube. Repeat this operation until the syringe is empty.
7. If part of the drug remains in the syringe in the form of sediment, fill the syringe with 25 ml of water and 5 ml of air and repeat the operation described in point 5. For some probes we may need 50 ml of drinking water for this purpose
GI.000-019-264.4.0
Nexium trademark is owned by AstraZeneca
AstraZeneca