NEXIUM PILLS 40MG

Packaging

14 pcs.

Mechanism of action

H inhibitor+-TO+-ATP-ase. The active substance of the drug Nexium - esomeprazole, S-isomer of Omeprazole, reduces the secretion of hydrochloric acid in the stomach by specific inhibition of the acid pump in the parietal cells. S- and R-isomer of omeprazole have similar pharmacodynamic activity.
Esomeprazole is a weak base and is activated in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it inhibits the activity of H+-K+-ATP-ase and thereby blocks the final stage of the secretion of hydrochloric acid. Nexium inhibits both basal and stimulated gastric secretion.
The effect of the drug develops within 1 hour after it is taken orally at a dose of 20 mg or 40 mg. When taking the drug daily for 5 days at 20 mg 1 time / day, the average maximum concentration of acid in the gastric contents after stimulation with pentagastrin is reduced by 90% (when measuring the concentration of acid 6-7 hours after taking the dose on the 5th day of therapy).
In patients with symptoms of gastroesophageal reflux disease, after 5 days of daily administration of Nexium orally at a dose of 20 mg or 40 mg of pH in the stomach with daily monitoring was higher than 4 for an average of 13 and 17 h, respectively. Among patients who took 20 mg of the drug per day, the maintenance of acidity at a pH above 4 for 8, 12 and 16 hours was achieved in 76%, 54% and 24%, respectively. For 40 mg of esomeprazole, this ratio was 97%, 92% and 56%, respectively.
Analysis of the pharmacokinetic data revealed a relationship between acid secretion and plasma concentration of the drug (the AUC parameter was used to estimate the concentration).
When receiving 40 mg of the drug per day, cure of reflux esophagitis occurs in 78% of patients after 4 weeks of therapy and in 93% of patients after 8 weeks of therapy.
Treatment with Nexium at a dose of 20 mg 2 times / day in combination with appropriate antibiotics for one week leads to successful eradication of Helicobacter pylori in approximately 90% of patients.
Patients with uncomplicated duodenal ulcer after a week-long course of eradication therapy do not require further treatment with antisecretory drugs for healing the ulcer.
During the use of the drug, the level of gastrin in the plasma increases as a result of reduced intragastric acid secretion.
In patients who have used antisecretory drugs for a long time, the formation of glandular cysts in the stomach is more often observed. This phenomenon is due to physiological changes as a result of inhibition of acid secretion. The cysts are benign and tend to disappear.
Due to the fact that esomeprazole is unstable in an acidic environment, the pills contain granules of the active substance coated with a coating resistant to the action of gastric juice.

Indications and usage

Gastroesophageal Reflux Disease:
- treatment of erosive reflux esophagitis;
- long-term maintenance therapy to prevent recurrence in patients with cured esophagitis;
- symptomatic therapy of gastroesophageal reflux disease.
Eradication of Helicobacter pylori (in combination with antibiotic therapy), as well as:
- treatment of duodenal ulcer associated with Helicobacter pylori;
- prevention of recurrence of peptic ulcers associated with Helicobacter pylori. Gastroesophageal Reflux Disease:
- treatment of erosive reflux esophagitis;
- long-term maintenance therapy to prevent recurrence in patients with cured esophagitis;
- symptomatic therapy of gastroesophageal reflux disease.
Eradication of Helicobacter pylori (in combination with antibiotic therapy), as well as:
- treatment of duodenal ulcer associated with Helicobacter pylori;
- prevention of recurrence of peptic ulcers associated with Helicobacter pylori.

Contraindications

Hypersensitivity to esomeprazole, substituted benzimidazoles or other components of the drug Nexium.

Pregnancy and Breastfeeding

Currently there are no data on the use of Nexium during pregnancy. Drug administration during this period is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
It is currently unknown if esomeprazole is excreted in breast milk, therefore, Nexium should not be administered during breastfeeding.
ATexperimental animal studies no adverse effect of esomeprazole on the development of the embryo or fetus has been identified. The introduction of the racemic drug also did not have any negative impact on the course of pregnancy in animals, childbirth and the period of postnatal development.

Before the prescription of esomeprazole, the possibility of a malignant neoplasm should be excluded, since treatment with Nexium can lead to a smoothing of symptoms and delay the diagnosis.
Patients taking the drug for a long period (especially more than a year) should be under the regular supervision of a physician.
Patients who are on “on-demand therapy” should be instructed to contact their physician when symptoms change.Taking into account fluctuations in the concentration of esomeprazole in plasma in the appointment of the drug in the mode of "therapy on demand," you should consider the interaction of the drug with other drugs.
In appointing Nexium for the eradication of Helicobacter pylori, the possibility of drug interaction for all components of triple therapy should be taken into account. Clarithromycin is a potent inhibitor of CYP3A4, therefore, all contraindications and interactions of clarithromycin should be considered when used in patients taking other drugs that are metabolized with CYP3A4 (for example, cisapride).
Patients with hereditary fructose intolerance, glucose – galactose malabsorption, or sucrose – isomalta deficiency should not take this drug.
Use in pediatrics
The use of the drug in children is not recommended due to lack of data.
Influence on ability to drive motor transport and control mechanisms
No effect of the drug on the ability to drive vehicles and control mechanisms.

Drug Interactions

Effect of esomeprazole on the pharmacokinetics of other drugs
When using Nexium simultaneously with other drugs, the mechanism of absorption of which depends on the acidity of the medium, it is possible to decrease or increase the absorption of other drugs.As with other drugs that suppress the secretion of acid or antacid agents, treatment with esomeprazole may lead to a decrease in the absorption of Ketoconazole or itraconazole.
The combined use of Nexium with drugs that are involved in the metabolism of CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, can lead to an increase in the concentration of these drugs in the plasma and require a reduction in their doses.
With the joint intake of 30 mg of Nexium and diazepam, the clearance of the enzyme-substrate complex (CYP2C19-diazepam) decreases by 45%.
With the simultaneous use of Nexium at a dose of 40 mg, residual concentrations of phenytoin in the blood plasma of patients with epilepsy increase by 13% (it is recommended to control the concentration of phenytoin in the blood plasma when prescribing esomeprazole and when it is canceled).
In healthy volunteers, co-administration of cisapride with 40 mg of Nexium resulted in a 32% increase in the AUC of cisapride and an increase in T1/2 cisapride by 31%, however, plasma cisapride concentrations did not change significantly. The slight lengthening of the QT interval, which was observed with cisapride monotherapy, did not increase with the addition of Nexium.
With the simultaneous use of Nexium does not cause clinically significant changes in the pharmacokinetic parameters of Amoxicillin, quinidine and Warfarin .
The effect of drugs on the pharmacokinetics of esomeprazole.
With the simultaneous use of Nexium with clarithromycin (500 mg 2 times / day), AUC of esomeprazole increases by 2 times (dose adjustment of Nexium is not required).

Currently not described cases of overdose. Single dose of 80 mg of esomeprazole did not cause any negative effects.
Treatment: Symptomatic and supportive therapy is performed if necessary. The specific antidote is unknown. Dialysis is ineffective, because esomeprazole binds to plasma proteins .

Currently not described cases of overdose. Single dose of 80 mg of esomeprazole did not cause any negative effects.
Treatment: Symptomatic and supportive therapy is performed if necessary. The specific antidote is unknown. Dialysis is ineffective, because esomeprazole binds to plasma proteins.