Neksium

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

The substance accumulates and acquires an active form inside the excretory tubules, where the influence of the proton pump (enzyme H ⁺ K ⁺ -ATPase) inhibits, as a result of which the release of hydrochloric acid is slowed down.

Indications Neksium

It is used to treat such disorders:

• gastrinoma ;
• reflux esophagitis (in the form of a symptomatic substance or to prevent recurrence, and in addition, as an etiological treatment for reflux gastritis of the ulcer variety);
• destruction of H. Pylori microbe (in conjunction with antibacterial drugs) for ulcers affecting the gastrointestinal tract;
• preventive treatment of peptic ulcers in the case of the use of NSAIDs, as well as for the treatment of ulcers resulting from the use of NSAIDs.

[1]

Release form

The release of the therapeutic element is produced in tablets with a volume of 20 or 40 mg. Inside the blister pack - 7 tablets. In the box - 1, 2 or 4 packs.

Pharmacodynamics

Drug effect develops after 1 hour after the introduction of 20-40 mg of esomeprazole. When you re-take 20 mg of the drug after 24 hours (1 time per day), by about the 5th day of use, there is a decrease by 90% of the amount of gastric secretion associated with the effect of pentagastrin.

Receiving a serving of 40 mg effectively acts with reflux esophagitis. It is prescribed as a therapeutic agent for ulcerative lesions of the gastrointestinal mucosa; when combined with a properly selected antibiotic, it increases the effectiveness of the destruction of Helicobacter pylori (in 90% of cases). Usually, in the combination therapy of an ulcer, after the completion of antibiotic use, there is no need for prolongation of anti-secretory monotherapy.

Clinical tests revealed that the use of drugs leads to an increase in blood values of gastrin (as a reaction to a decrease in the production of hydrochloric acid). The increase in the number of endocrine cells that produce histamine, is carried out with an increase in blood levels of gastrin.

Sometimes there was an increase in the frequency of development of granular cysts in the gastric mucosa in the case of prolonged administration of antisecretory drugs. This phenomenon is considered a physiological response to the suppression of the production of hydrochloric acid. Such cysts always have a temporary and benign character, passing at the end of the treatment cycle.

Omeprazole with high efficiency prevents the formation of peptic ulcer varieties when administered together with NSAIDs (this also includes selective inhibitors of COX-2).

[2]

Pharmacokinetics

Esomeprazole is absorbed at high speed, reaching plasma values of Cmax after approximately 1-2 hours from the moment of oral administration.

The level of bioavailability with the introduction of a single dose of 40 mg equals 64%, and with repeated administration increases to 90%. At a dosage of 20 mg, the absolute bioavailability index, respectively, is 50% and 68%.

The values of intraplasma protein synthesis are 97%. Introduction together with food does not change the intensity of the anti-secretory influence, but it slows down the rate of absorption.

The exchange processes of the main part of esomeprazole are realized with the help of the enzyme CYP 2С19, and the balance with the participation of the isomer of the enzyme CYP 3A4. All these reactions proceed with the help of the hemoprotein P450. The term half-life is approximately 70 minutes after the introduction of a second portion after 24 hours.

Elimination is performed through the kidneys, fully, in the interval between the use of drugs; when administered once in 24 hours, it does not accumulate inside the body. A smaller portion of the drug is excreted in the feces. Metabolic elements of drugs do not affect the release of hydrochloric acid. Less than 1% of the drug is eliminated through the kidneys unchanged.

Dosing and administration

Nexium can be used exclusively orally - pills are swallowed, without chewing, with simple water.

In case of problems with the swallowing function 1-well, a pill of a drug is added to plain non-carbonated water (0.1 l), they wait until it is dissolved, and the resulting liquid is drunk (you can drink the medicine within a maximum of half an hour after the tablet is dissolved). Any other solvents (milk or tea) can not be used, because they can damage the tablet shell. Further, in a glass from which they drank the medicine, they poured more water and again they drink.

For very serious problems with swallowing, the drug is administered with a nasogastric tube. Before the introduction of the tablet is dissolved according to the above scheme. Next, the drug is collected in a syringe (5-10 ml), and then injected into the probe.

Therapy for reflux esophagitis.

In the period of the 1st month you need to take 40 mg of the drug per day. If after this period the symptoms of the disease persist, the treatment is extended for another 1 month. To prevent the recurrence of pathology, 20 mg of drugs are administered per day.

To eliminate the signs of the disease during reflux esophagitis, 20 mg is administered per day for the first month; If symptoms persist, the diagnosis must be reviewed. Then, as necessary, 20 mg is administered per day to control the situation. It is impossible to use Nexium “as needed” as a preventive treatment in people using NSAIDs and having an increased tendency to the appearance of peptic ulcers.

Gastrointestinal ulcers associated with Helicobacter pylori or anti-relapse treatment.

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

Persons who use NSAIDs for a long time need to consume 20 mg 1 time a day for 24 hours. In the case of peptic ulcers that developed due to the use of NSAIDs, the duration of the course is 1-2 months.

In the case of gastrinomas, they are used 2 times daily for 40 mg of Nexium. The cycle duration is selected individually, taking into account the clinical picture. With such a disease can be consumed in the range of 0.08-0.16 g of the drug per day.

People with liver failure can enter no more than 20 mg of esomeprazole per day.

Use Neksium during pregnancy

There is very little information about the introduction of esomeprazole during pregnancy, because of what it is prescribed very carefully. In clinical tests, the teratogenic and embryotoxic effect of the drug was not detected, as was the effect on vaginal and childbirth, as well as the rate of postnatal development.

There is no data on the removal of Nexium with breast milk, so when breastfeeding it is not prescribed.

[3]

Contraindications

Among the contraindications:

• symptoms of intolerance towards the drug (also regarding benzimidazoles);
• administration with atazanavir.

Side effects Neksium

The main cork signs:

• lesions associated with the activity of the central nervous system and PNS: depression, insomnia, dizziness, drowsiness and aggressiveness, as well as paresthesias, increased excitability and hallucinations (especially in individuals with severe stages of the disease);
• violations of the gastrointestinal tract: stomatitis or candidiasis;
• problems with hematopoietic processes: leuko-, thrombocyto- or pancytopenia, and also agranulocytosis;
• disorders of the liver: liver failure, hepatitis (accompanied by jaundice or not), as well as encephalopathy (with a history of severe hepatic abnormalities);
• ODA lesions: pain in the joints and muscle weakness;
• signs associated with the epidermis: rash, alopecia, photosensitivity and PET;
• others: intolerance symptoms (fever, hyperhidrosis, bronchial spasm and nephritis), hyponatremia, puffiness and taste disturbances.

[4]

Overdose

Very little information is available regarding cases of esomeprazole intoxication. With the introduction of drugs in portions up to 80 mg, there was no development of a strong toxic effect. After applying a portion of 0.28 g, symptoms of a gastrointestinal tract disorder and systemic weakness were noted.

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

[5], [6], [7]

Interactions with other drugs

In drugs whose absorption depends on the level of gastric pH, esomeprazole is able to enhance or weaken the ability to absorb. In the case of the use of drugs, a decrease in ketoconazole absorption with itraconazole is noted.

The inhibition of the production of the element CYP 2C19 causes an increase in the plasma values of those agents whose metabolic processes are performed using this enzyme (among them, diazepam with phenytoin, citalopram and imipramine with clomipramine). Often, in such cases, a reduction in the portion of such drugs is required.

In the case of the introduction of Nexium with warfarin, it is necessary to monitor coagulation parameters.

The combination of the drug with cisapride causes an increase in the AUC values by 32%, as well as an extension by 31% of the term half-life of cisapride. But this does not lead to a significant change in blood parameters of cisapride.

Combination with ritonavir or atazanavir causes a weakening of the severity of the action of antiviral drugs, even in the case of increasing their portions.

Because the active ingredient of the drug undergoes metabolic processes with the participation of CYP 3A4 enzymes with CYP 2C19, its introduction along with clarithromycin (slows down the activity of CYP 3A4 enzymes) increases the level of Nexium AUC. But such changes do not require correction of a portion of esomeprazole.

The use of drugs with voriconazole increases the exposure of the first more than doubled (but this does not require changing the dose of the drug).

Storage conditions

Nexium must be kept in a closed place for small children. The temperature level is maximum 30 ° С.

Shelf life

Nexium can be used for a 3-year term from the time the pharmaceutical is manufactured.

Application for children

It is impossible to use for persons under the age of 12, because clinical tests have not been performed for the specified age subgroup.

Analogs

Analogues of the drug are substances Emanera, Losek Maps, Omep and Lansoprazole with Ultop, and in addition Omeprazole, Hasek and Pariet with Sanpraz and Lansoprol.

[8], [9]

Reviews

Nexium receives good reviews from patients - it acts very effectively and helps to eliminate the violations described in the medication. Of the minuses noted only the high cost of the drug.