Nexium

Nexium contains the element esomeprazole. It specifically slows down the action of the proton pump of the parietal cells of the gastric mucosa, and in addition, it acts as an S-isomeric variety of the component omeprazole.

The substance accumulates and takes on an active form inside the excretory tubules, where it inhibits the effect of the proton pump (the enzyme H ⁺ K ⁺ -ATPase), resulting in a slowdown in the process of hydrochloric acid excretion.

Indications Nexium

It is used to treat the following disorders:

• gastrinoma;
• reflux esophagitis (as a symptomatic substance or to prevent relapse, and also as an etiological treatment for ulcerative reflux gastritis);
• destruction of the H.pylori microbe (in combination with antibacterial drugs) in ulcers affecting the gastrointestinal tract;
• preventive treatment of peptic ulcers in case of NSAID use, as well as for the treatment of ulcers that appeared as a result of NSAID use.

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Release form

The therapeutic element is released in tablets with a volume of 20 or 40 mg. There are 7 tablets in a blister pack. There are 1, 2 or 4 packages in a box.

Pharmacodynamics

The medicinal effect develops after 1 hour from the moment of administration of 20-40 mg of esomeprazole. With repeated administration of 20 mg of the drug after 24 hours (1 time per day), approximately by the 5th day of use, a 90% decrease in the volume of gastric secretion associated with the effect of pentagastrin occurs.

Taking a 40 mg dose is effective in reflux esophagitis. It is prescribed as a treatment for ulcerative lesions of the gastrointestinal mucosa; when combined with a properly selected antibiotic, it increases the effectiveness of destroying Helicobacter pylori (in 90% of cases). Usually, with combined ulcer therapy, after the end of antibiotic use, there is no need to prolong antisecretory monotherapy.

Clinical tests have shown that the use of the drug leads to an increase in blood gastrin levels (as a response to a decrease in the production of hydrochloric acid). An increase in the number of endocrine cells producing histamine occurs with an increase in the blood level of gastrin.

An increased incidence of granular cysts in the gastric mucosa has occasionally been observed in cases of prolonged administration of antisecretory drugs. This phenomenon is considered a physiological response to the suppression of hydrochloric acid production. Such cysts are always temporary and benign, disappearing upon completion of the treatment cycle.

Omeprazole is highly effective in preventing the formation of peptic ulcers when administered together with NSAIDs (including selective COX-2 inhibitors).

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Pharmacokinetics

Esomeprazole is rapidly absorbed, reaching plasma Cmax values approximately 1-2 hours after oral administration.

The bioavailability level when administered as a single dose of 40 mg is 64%, and increases to 90% when administered repeatedly. At a dosage of 20 mg, the absolute bioavailability index is 50% and 68%, respectively.

The values of intraplasmic protein synthesis are 97%. Administration with food does not change the intensity of the antisecretory effect, but slows down the rate of absorption.

The metabolic processes of the main part of esomeprazole are realized with the help of the enzyme CYP 2C19, and the remainder - with the participation of the isomer of the enzyme CYP 3A4. All these reactions occur with the help of hemoprotein P450. The half-life is approximately 70 minutes - after the introduction of a repeated portion after 24 hours.

Elimination occurs through the kidneys, completely, in the interval between drug administrations; with a single administration, it does not accumulate in the body over 24 hours. A smaller portion of the drug is excreted with feces. Metabolic elements of the drug do not affect the excretion of hydrochloric acid. Less than 1% of the drug is eliminated unchanged through the kidneys.

Dosing and administration

Nexium can only be used orally - the tablets are swallowed without chewing, washed down with plain water.

In case of problems with swallowing function, add 1 tablet of LS to plain still water (0.1 l), wait for it to dissolve and drink the resulting liquid (you can drink the medicine within a maximum of half an hour from the moment the tablet dissolves). Any other solvents (milk or tea) cannot be used, because they can damage the tablet shell. Then pour more water into the glass from which you drank the medicine and drink it again.

In case of very serious problems with swallowing, the drug is administered using a nasogastric tube. Before administration, the tablet is dissolved according to the above scheme. Then the medicine is drawn into a syringe (5-10 ml), and then injected into the tube.

Therapy for reflux esophagitis.

During the first month, 40 mg of the drug should be taken per day. If after this period the signs of the disease persist, the treatment is extended for another month. To prevent a relapse of the pathology, 20 mg of the drug is administered per day.

To eliminate the symptoms of the disease during reflux esophagitis, 20 mg is administered per day during the first month; if symptoms persist, the diagnosis should be reviewed. Then, if necessary, 20 mg is administered per day to control the situation. Nexium should not be used "as needed" as a preventive treatment in people using NSAIDs and who have an increased tendency to develop peptic ulcers.

Ulcers in the gastrointestinal tract associated with Helicobacter pylori, or anti-relapse treatment.

Combination therapy includes the use of 20 mg esomeprazole and 1 g amoxicillin, as well as 0.5 g clarithromycin 2 times a day for 7 days.

People who use NSAIDs for a long time should take 20 mg once a day. In the case of a peptic ulcer that developed due to taking NSAIDs, the course duration is 1-2 months.

In case of gastrinoma, 40 mg of Nexium is used twice a day. The duration of the cycle is selected individually, taking into account the clinical picture. With such a disease, you can use within 0.08-0.16 g of the drug per day.

People with liver failure may be given no more than 20 mg of esomeprazole per day.

Use Nexium during pregnancy

There is very little information regarding the introduction of esomeprazole during pregnancy, which is why it is prescribed with great caution. In clinical tests, the teratogenic and embryotoxic effect of the drug was not detected, as well as the effect on gestation and delivery, as well as the rate of postnatal development.

There is no data on the excretion of Nexium in breast milk, so it is not prescribed during breastfeeding.

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Contraindications

Among the contraindications:

• symptoms of intolerance to the drug (also to benzimidazoles);
• co-administration with atazanavir.

Side effects Nexium

Main signs of traffic jams:

• lesions associated with the activity of the central nervous system and the peripheral nervous system: depression, insomnia, dizziness, drowsiness and aggressiveness, as well as paresthesia, increased excitability and hallucinations (especially in individuals with severe stages of the disease);
• gastrointestinal dysfunction: stomatitis or candidiasis;
• problems with hematopoietic processes: leukopenia, thrombocyto- or pancytopenia, as well as agranulocytosis;
• liver dysfunction: liver failure, hepatitis (with or without jaundice), and encephalopathy (with a history of severe liver pathologies);
• musculoskeletal disorders: pain in the joint area and muscle weakness;
• signs associated with the epidermis: rashes, alopecia, photosensitivity and TEN;
• others: symptoms of intolerance (increased temperature, hyperhidrosis, bronchial spasm and nephritis), hyponatremia, edema and taste disturbances.

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Overdose

There is very little information regarding cases of intoxication with esomeprazole. When the drug was administered in doses up to 80 mg, no strong toxic effects developed. After using a dose of 0.28 g, symptoms of gastrointestinal disorders and systemic weakness were noted.

Esomeprazole has no antidote. Hemodialysis procedures will be ineffective because most of the drug is synthesized with plasma protein. If signs of poisoning appear, symptomatic and supportive measures are taken.

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Interactions with other drugs

For drugs whose absorption depends on the level of gastric pH, esomeprazole can enhance or weaken the ability to absorb. In the case of using drugs, a weakening of the absorption of ketoconazole with itraconazole is noted.

Inhibition of the production of the CYP 2C19 element causes an increase in the plasma values of those drugs whose metabolic processes are carried out with the help of this enzyme (among them diazepam with phenytoin, citalopram and imipramine with clomipramine). Often in such cases it is necessary to reduce the dose of such drugs.

When Nexium is administered with warfarin, coagulation parameters must be monitored.

Combination of the drug with cisapride causes an increase in AUC values by 32%, as well as a prolongation of the half-life of cisapride by 31%. However, this does not lead to a significant change in blood levels of cisapride.

Combination with ritonavir or atazanavir causes a weakening of the effect of antiviral drugs, even if their doses are increased.

Because the active ingredient of the drug undergoes exchange processes involving CYP 3A4 enzymes with CYP 2C19, its administration together with clarithromycin (slows down the activity of CYP 3A4 enzymes) increases the AUC level of Nexium. But such changes do not require correction of the esomeprazole dose.

The use of the drug together with voriconazole increases the exposure rates of the former more than twofold (but this does not require a change in the dose of the drug).

Storage conditions

Nexium should be stored in a place closed to small children. Temperature level – maximum 30°C.

Shelf life

Nexium can be used for a period of 3 years from the date of manufacture of the pharmaceutical product.

Application for children

It should not be used by persons under 12 years of age, as clinical testing has not been performed in this age group.

Analogues

The analogs of the drug are Emanera, Losek Maps, Omep and Lansoprazole with Ultop, and also Omeprazole, Gasec and Pariet with Sanpraz and Lansoprol.

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Reviews

Nexium gets good reviews from patients - it works very effectively and helps eliminate the disorders described in the drug's indications. The only downside is the high cost of the medication.