Nexium (Esomeprazole) is a specific inhibitor of the proton pump of the parietal cells of the mucous layer of the stomach. It is the S-isomer form of omeprazole. Cumulated and transformed into an active state in the secretory canaliculi, Nexium inhibits the proton pump (enzyme H +, K + -ATPase), thereby developing the inhibition of gastric acid secretion.
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Nexium is engaged in the treatment of the following conditions:
Treatment of Zollinger-Ellison syndrome;
Reflux esophagitis (as symptomatic therapy and anti-treatment, as well as the etiological treatment of peptic forms of reflux gastritis);
Eradication of Helicobacter pylori - in the complex treatment with antibacterial drugs for stomach ulcers and duodenal ulcers;
Preventive treatment of peptic ulcers when using NSAIDs, treatment of ulcers caused by non-steroidal anti-inflammatory drugs.
How It Works?
The drug takes effect within 60 minutes after administration of 20-40mg of esomeprazole. Iterative application of esomeprazole 20mg within 24 hours once a day is followed by a reduction of gastric secretions due to the action of pentagastrin by 90% for approximately 5 days after the intake.
Nexium at a dose of esomeprazole 40mg is effective in the treatment of reflux esophagitis. Used for the treatment of ulcers of the gastric mucosa and duodenal ulcers, in combination with an appropriate antibiotic allows to achieve the best effect of eradication of Helicobacter pylori (90%). Typically, after the complex treatment of peptic ulcer disease with antibiotics a need to continue antisecretory monotherapy does not arise.
Clinical studies have shown that while taking the drug content of gastrin in the blood increases in response to a decrease in production of hydrochloric acid. Increasing the number of endocrine cells that produce histamine occurs by increasing the concentration of gastrin in the blood. In some cases, there was an increase in the incidence of granular cysts gastric mucosa with prolonged use of antisecretory drugs. This phenomenon is regarded as a physiological response to depression of the production of hydrochloric acid. The cysts are always benign and transient (and disappear after the treatment).
Nexium is effective in preventing the formation of peptic ulcers during concomitant therapy with non-steroidal anti-inflammatory drugs (even cyclooxygenase-2 selective group).
Nexium is a preparation of acid, it is used in the form of granules, coated tablets, orally. Esomeprazole is rapidly absorbed, the maximal effect is achieved in the blood plasma about 60-120 minutes after the internal application.
Blood plasma proteins bind 97% of the active substance. At the same time taking esomeprazole and food does not change antisecretory effect, but absorption can be slowed.
How It Is Taken?
Nexium is indicated only for internal use, the tablets should be swallowed without chewing; drink some water to wash down the pills. For patients with swallowing function failure the tablet can be put in water (100ml, non-carbonated) and drunk immediately after the dissolution of the tablet (or within 30 minutes).
Do not use other solutions (tea, milk), since they can damage the special coating of tablets. After the liquid is drunk, it is necessary to take another glass of water, using the same glass. In an extreme case, at manifested failure of swallowing function, Nexium should be ingested through a tube (nasogastric). Before administration a tablet is dissolved in water by the method described above.
The choice of dosage for elderly is not affected. Errors of metabolism of esomeprazole in patients with presence of hepatic failure have been identified. Due to this the dose recommended for such patients is esomeprazole 20mg per day.
For the treatment of reflux esophagitis Nexium should be taken at esomeprazole 40mg / day for four weeks, if symptoms persist therapy may extend for four weeks more. When used in the preventive treatment, Nexium is taken at esomeprazole 20mg / day. For relief of symptoms of reflux esophagitis esomeprazole 20mg / day is taken during four weeks, while preserving the signs of the disease indicate a need to clarify the diagnosis. For further control of the condition take esomeprazole 20mg / day, or "on demand". Do not use Nexium "on demand" as a preventive therapy for persons using NSAIDs with an increased risk of peptic ulcers.
Nexium is used in the complex treatment of gastric ulcer and duodenal ulcers associated with Helicobacter pylori infection, or as a preventive treatment. In such patients Nexium is taken in form of esomeprazole 20mg in combination with amoxicillin (1000mg) and clarithromycin (500mg), twice a day during one week.
Patients administered NSAIDs for a long time should take esomeprazole 20mg once a day. In the treatment of peptic ulcers caused by NSAIDs, the duration of treatment is four to eight weeks.
The syndrome Zollinger - Ellison requires esomeprazole 40mg administered twice per day. The duration of treatment and the dose are selected individually depending on the clinical situation. The maximum tolerated dose for patients with this syndrome is 80-160mg per day.
When liver failure the maximum allowable dose of esomeprazole 20mg / day. No dosage adjustment is required in patients with renal insufficiency, however in patients with severe renal impairment Nexium should be used with caution.
Is It For Me?
Nexium should not be used in children under 12 years of age (no key clinical trials in this age group has been taken) and in individuals with hypersensitivity reactions (including the benzimidazoles).
The research data to identify the characteristics of the metabolism of esomeprazole in patients with renal insufficiency is absent. Since the kidneys do not eliminated the active substance, but only metabolites, the biotransformation violations should not be expected.
Any Drug Interactions or Incompatibilities?
Nexium is not compatible with Reyataz, since the latter contains atazanavir. Atazanavir effects are dramatically oppressed by proton pump inhibitors alongside with reduction of gastric acid. The same holds true for ritonavir containing drugs.
If the absorption of other agents depends on the acidity of gastric contents, esomeprazole may then increase or decrease the absorption capacity. When therapy with esomeprazole, absorption of itraconazole and ketoconazole is decreased. Suppression of CYP 2C19 increases the blood plasma content of preparations, biometabolism of which occurs with this enzyme (citalopram, diazepam, clomipramine, phenytoin, imipramine).
Typically, this requires a reduction in dosage of the latter.
During coadministration of esomeprazole and warfarin, coagulation parameters should be monitored.
The combined use of voriconazole and esomeprazole leads to increased exposure to the letter by more than two times (Nexium dosage adjustment is not required).
What Side Effects Should I Brace Myself For?
Nexium can produce side effects on different systems of the body. Below we will break down the most common of them.
Central nervous system and peripheral nervous system: drowsiness, depression, paresthesia, aggression, insomnia, irritability, dizziness, hallucinations (particularly in severely ill).
Gastrointestinal tract: candidiasis, stomatitis.
The system of blood and hemogenesis: thrombocytopenia, leukopenia, pancytopenia, agranulocytosis.
Liver: Hepatitis (with or without jaundice), encephalopathy (in case of severe liver disease in history), hepatic failure.
Musculoskeletal: muscle weakness, pain in the joints.
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Nexium - contraindications, warnings and precautions
With symptoms of overdose a supportive and symptomatic therapy should be administered. Hemodialysis is ineffective, since the drug is more often associated plasma proteins.
Very few data on the use of esomeprazole in pregnant women, so the drug is prescribed with caution. In clinical experiments revealed no embryotoxic and teratogenic effects of Nexium, the impact on pregnancy and child bearing, as well as the rate of post-natal period. There is no data about the probability of penetration of Nexium passing into breast milk - during lactation it is not recommended to prescribe the drug.
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