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Nexium

Nexium
Nexium reduces the amount of acid produced in the stomach and thereby reduces the symptoms. It also cures the damage caused by reflux disease.

Brand: Esomeprazole

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: March 2024
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Nexium 40 mg
360 pills - 40 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$195.55 $0.54 $162.41 Add to cart
270 pills - 40 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$151.93 $0.56 $116.54 Add to cart
180 pills - 40 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$108.97 $0.61 $70.01 Add to cart
120 pills - 40 mg $79.91 $0.67 $39.41 Add to cart
90 pills - 40 mg $65.95 $0.73 $23.54 Add to cart
60 pills - 40 mg $51.93 $0.87 $7.73 Add to cart
30 pills - 40 mg $29.83 $0.99 No Add to cart
Nexium 20 mg
360 pills - 20 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$161.91 $0.45 $149.49 Add to cart
270 pills - 20 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$129.97 $0.48 $103.58 Add to cart
180 pills - 20 mg $91.99 $0.51 $63.71 Add to cart
120 pills - 20 mg $66.93 $0.56 $36.87 Add to cart
90 pills - 20 mg $54.91 $0.61 $22.94 Add to cart
60 pills - 20 mg $39.90 $0.67 $12.00 Add to cart
30 pills - 20 mg $25.95 $0.87 No Add to cart

Product description

Name

Nexium (Esomeprazole)

Pharmacological action

H+-K+-ATPase inhibitor. Esomeprazole is the S-isomer of omeprazole and reduces gastric hydrochloric acid secretion by specific proton pump inhibition in parietal cells. The S- and R-isomer of omeprazole have similar pharmacodynamic activity.


Mechanism of action


Esomeprazole is a weak base which converts to its active form in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it inhibits the proton pump enzyme H+-K+-ATPase. This inhibits both basal and stimulated secretion of hydrochloric acid.


Effect on acid secretion in the stomach


After oral administration of esomeprazole at a dose of 20 mg or 40 mg for 5 days in patients with symptomatic gastroesophageal reflux disease (GERD), a decrease in gastric hydrochloric acid secretion for most of the day was noted. The effect was the same when administered intravenously and when taken orally.


Analysis of the pharmacokinetic data revealed the relationship between inhibition of acid secretion and the plasma concentration of the drug after oral administration (to estimate the concentration, the AUC parameter was used).


After intravenous injection of 80 mg of esomeprazole into healthy volunteers for 30 minutes, followed by prolonged intravenous infusion of 8 mg/h for 23.5 hours, the gastric pH was above 4 for an average of 21 hours, and above 6 for 11-13 hours.


The therapeutic effect achieved by inhibiting acid secretion


Healing of reflux esophagitis when using esomeprazole in dose of 40 mg occurs in approximately 78% of patients after 4 weeks of therapy and in 93% of patients after 8 weeks of therapy (when taken orally).


The efficacy of Nexium® for peptic ulcer bleeding has been demonstrated in a study of patients with endoscopically confirmed peptic ulcer bleeding.


Other effects related to inhibition of acid secretion


During treatment with drugs that reduce gastric gland secretion, plasma gastrin concentrations are increased as a result of decreased hydrochloric acid secretion. The decrease in hydrochloric acid secretion increases chromogranin A (CgA) concentrations. Increased concentration of CgA may affect the results of examinations for detection of neuroendocrine tumors. To prevent this effect, esomeprazole should be temporarily stopped 5 days before the CgA concentration study. If CgA concentrations have not returned to normal during this time, the study should be repeated.


In children and adult patients treated with oral esomeprazole for a long period of time, an increase in enterochromaffin-like cells was observed, which is probably related to an increase in plasma gastrin. This phenomenon has no clinical significance.


Formation of glandular cysts in the stomach was more frequently observed in patients who had taken orally for a long period of time the drugs decreasing gastric gland secretion. These phenomena are due to physiological changes resulting from inhibition of hydrochloric acid secretion. The cysts are benign and undergo reverse development.


The use of drugs that inhibit hydrochloric acid secretion, including proton pump inhibitors, is accompanied by an increase in the content of microbial flora normally present in the stomach. Proton pump inhibitors use may lead to a slight increase in the risk of gastrointestinal infections caused by Salmonella spp., Campylobacter spp. and probably Clostridium difficile in hospitalized patients.


In children less than 1 month of age and 1-11 months of age, a decrease in the mean percentage of time with an intragastric pH value less than 4 was observed with oral esomeprazole doses of 0.5 mg/kg and 1 mg/kg, respectively. The safety profile of esomeprazole in children is similar to that of adults.

Pharmacokinetics

Absorption and distribution


The apparent Vd at equilibrium in healthy volunteers is approximately 0.22 l/kg body weight. Binding to plasma proteins is 97%.


Metabolism and excretion


Esomeprazole is completely metabolized by cytochrome P450 isoenzymes. The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP2C19, with the formation of hydroxylated and desmethylated metabolites of esomeprazole. The remainder is metabolized by the CYP3A4 isoenzyme, producing esomeprazole sulfo-derivative, the main plasma-detectable metabolite.


The parameters below mainly reflect the pharmacokinetics in patients with increased CYP2C19 isoenzyme activity.


Total plasma clearance is approximately 17 l/h after single drug administration and 9 l/h after multiple administration. T1/2 is 1.3 h after repeated doses of the drug once daily. AUC increases with repeated administration. This increase is dose- and time-dependent, which is a consequence of decreased metabolism during "first passage" through the liver and decreased systemic clearance, probably caused by the fact that esomeprazole and/or its sulfo metabolite inhibit the CYP2C19 isoenzyme.


When administered once daily, esomeprazole is completely eliminated from the plasma between doses. No tendency to cumulation has been observed.


When repeated intravenous administration of esomeprazole at a dose of 40 mg, the average plasma Cmax is approximately 13.6 µmol/L. When administered orally at similar doses, the average plasma Cmax is 4.6 µmol/L. Total exposure is slightly lower (approximately 30%) when esomeprazole is administered by injection compared to oral administration.


When esomeprazole was administered by IV at doses of 40 mg, 80 mg and 120 mg for 30 min followed by IV administration at a dose of 4 mg/h or 8 mg/h for 23.5 h, a linear dependence of AUC on the administered dose was shown.


The major metabolites of esomeprazole have no effect on gastric hydrochloric acid secretion. When administered orally, up to 80% of the dose is excreted as metabolites in the urine, the remainder in the feces. Less than 1% of unchanged esomeprazole is detected in the urine.


Pharmacokinetics in special clinical cases


About 2.9±1.5% of the population have reduced CYP2C19 isoenzyme activity (patients with slow metabolism). In these patients metabolism of esomeprazole is mainly due to CYP3A4 and in repeated oral administration of 40 mg of esomeprazole once daily the average AUC is 100% higher than in patients with active CYP2C19 enzyme (fast metabolism patients). Mean plasma Cmax values are approximately 60% higher in patients with slow metabolism. Similar differences have been found in the intravenous administration of esomeprazole. The noted features do not affect the dose and route of administration of esomeprazole.


The metabolism of esomeprazole is not significantly altered in elderly patients (71-80 years).


Metabolism of esomeprazole may be impaired in patients with moderate to moderate hepatic impairment. In patients with severe hepatic impairment the metabolic rate is reduced, resulting in a doubling of the AUC for esomeprazole. There is no tendency for cumulation of esomeprazole and its major metabolites when administered once daily.


No pharmacokinetic studies have been performed in patients with impaired renal function. Since it is not the esomeprazole itself but its metabolites that are excreted through the kidneys, it may be assumed that the metabolism of esomeprazole in patients with impaired renal function is not altered.


The pharmacokinetics of esomeprazole in children and adolescents aged 0 to 18 years were studied after a 3-minute IV injection once daily for 4 days. The maximum equilibrium plasma concentration of the drug (Css,max) was assessed 5 min after administration of the dose in children in all age groups, and in adult patients - 7 min after administration of the drug at a dose of 40 mg and at the end of the drug infusion at a dose of 20 mg.

Contraindications to use

  • Childhood under 1 year of age;

Children and adolescents under 18 years of age for other indications except gastroesophageal reflux disease;

concomitant use with atazanavir and nelfinavir;

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

Caution should be exercised when prescribing the drug in patients with severe renal insufficiency.

Use in pregnancy and lactation

Data on the use of esomeprazole in pregnancy are currently limited. The drug should be administered during pregnancy only if the expected benefits to the mother exceed the possible risk to the fetus.


No direct or indirect adverse effects of Nexium on embryo or fetal development have been observed in experimental animal studies. Administration of racemic mixture of the drug also did not have any adverse effects on animals during pregnancy, delivery, and postnatal development.


There are no data on the use of the drug in women during lactation. It is unknown whether esomeprazole is excreted with breast milk, therefore Nexium® should not be prescribed during breast-feeding. If therapy with Nexium® during lactation is necessary, discontinuation of breast-feeding should be considered.


Administration in liver dysfunction

No dose adjustment is required in GERD in patients with liver dysfunction of mild to moderate degree of severity. In patients with severe liver dysfunction the maximum daily dose is 20 mg.


In patients with peptic ulcer bleeding a dose adjustment of Nexium® in patients with mild to moderate liver dysfunction is not required. In patients with severe hepatic impairment the following mode of Nexium® administration is recommended: 80 mg by intravenous infusion for 30 min followed by prolonged intravenous infusion at a maximum dose of 4 mg/hour for 71.5 hours.


Administration in renal dysfunction

No dose adjustment of Nexium is required in patients with impaired renal function. Due to limited experience of Nexium® use in patients with severe renal failure, caution should be exercised when treating such patients.

Administration in children

Administration in children under 1 year of age and in children and adolescents under 18 years of age for other indications, except for gastroesophageal reflux disease is contraindicated.

Use in elderly patients

In elderly patients no adjustment of the drug dose is required.

Indications for Nexium

Adults


As an alternative to oral therapy when it is not possible:


  • For gastroesophageal reflux disease in patients with esophagitis and/or severe reflux disease symptoms;
  • for healing of peptic ulcers associated with taking NSAIDs;
  • for prevention of peptic ulcers associated with taking NSAIDs in patients at risk.
For prevention of recurrence of bleeding from peptic ulcer after endoscopic hemostasis.

Children and adolescents (ages 1 to 18 years).

  • For gastroesophageal reflux disease in patients with erosive reflux esophagitis and/or marked symptoms of reflux disease.


Dosing regimen

Adults


As an alternative to oral therapy, IV administration of esomeprazole at a dose of 20-40 mg once daily may be recommended if this is not possible.


In GERD patients with esophagitis, the recommended dose of Nexium® is 40 mg once daily.


For treatment of GERD symptoms, the drug is prescribed in a dose of 20 mg once daily.


For healing of peptic ulcers associated with taking NSAIDs in patients at risk, esomeprazole in a dose of 20 mg once daily is recommended.


For prevention of peptic ulcers associated with taking NSAIDs, the recommended dose of Nexium® is 20 mg once daily.


As a rule, the period of parenteral use of Nexium® is short, the patient should be transferred to oral administration as soon as possible.


In order to prevent recurrence of peptic ulcer bleeding after endoscopic hemostasis, esomeprazole at a dose of 80 mg as an IV infusion for 30 min followed by an extended IV infusion of esomeprazole at a dose of 8 mg/h for 3 days (72 h) is recommended. After parenteral therapy to inhibit acid secretion, antisecretory therapy (e.g., esomeprazole 40 mg once daily for 4 weeks) is recommended.


Duration of injections and infusions


IV injections


40 mg dose: a prepared solution of esomeprazole (5 ml, 8 mg/ml) is injected intravenously for at least 3 minutes.


20 mg dose: half of the prepared esomeprazole solution (2.5 ml, 8 mg/ml) is administered v/v for at least 3 min; unused solution residues should be disposed of.


IV infusions.


40 mg dose: the prepared esomeprazole solution is administered as an IV infusion for 10-30 min.


20 mg dose: half of the prepared esomeprazole solution is administered as an IV infusion for 10-30 min. Unused residual solution should be disposed of.


80 mg dose: prepared esomeprazole solution is administered as an IV infusion for 30 min.


Dose 8 mg/h: the prepared esomeprazole solution is administered as an extended intravenous infusion for 71.5 h (8 mg/h).


Children and adolescents (ages 1 to 18 years)


As an alternative to oral therapy when this is not possible in patients with gastroesophageal reflux disease with erosive reflux esophagitis and/or severe symptoms of reflux disease, esomeprazole is given parenterally once daily as part of GERD therapy (see table for dosing recommendations).


As a rule, during parenteral administration of Nexium® the patient should be switched to oral administration as soon as possible.

V injections


40 mg dose: prepared esomeprazole solution (5 ml, 8 mg/ml) is injected intravenously for at least 3 min.


20 mg dose: half of the prepared esomeprazole solution (2.5 ml, 8 mg/ml) is administered intravenously for at least 3 min. Unused residues of the solution should be disposed of.


10 mg dose: 1.25 ml of prepared esomeprazole solution (8 mg/ml) is administered intravenously for at least 3 min. Unused residues of the solution should be disposed of.


Intravenous infusions


Dose 40 mg: the prepared esomeprazole solution is administered as an IV infusion for 10-30 minutes.


20 mg dose: half of the prepared esomeprazole solution is administered as an IV infusion for 10-30 min. Unused residual solution should be disposed of.


10 mg dose: a quarter of the prepared esomeprazole solution is administered as an IV infusion for 10-30 min. Unused residual solution should be disposed of.


Special patient groups


No dose adjustment of Nexium® is required in patients with impaired renal function. Due to limited experience of Nexium® use in patients with severe renal failure, caution should be exercised when treating such patients.


In GERD, no dose adjustment is required in patients with mild to moderate hepatic dysfunction. In patients with severe hepatic impairment, the maximum daily dose is 20 mg.


In patients with peptic ulcer bleeding a dose adjustment of Nexium® in patients with mild to moderate liver dysfunction is not required. In patients with severe hepatic impairment the following regimen of Nexium® administration is recommended: 80 mg as an IV infusion for 30 minutes followed by prolonged IV infusion at a maximum dose of 4 mg/h for 71.5 hours.


No dose adjustment is required in elderly patients.


Rules of preparation and use of solutions for IV administration


Degradation of prepared solution mainly depends on pH value, therefore only 0.9% sodium chloride solution for IV administration should be used for dissolving the drug.


Prepared solution should not be mixed or administered together with other drugs.


Before use the solution should be evaluated visually for the absence of visible mechanical impurities and color changes. Only a clear solution can be used.


It is recommended to administer the prepared solution immediately after preparation (from the microbiological point of view).


The prepared solution should be used within 12 h. Store at a temperature not exceeding 30°C.


Unused remains of the solution should be disposed in accordance with the local requirements.


Solution for intravenous injection (8 mg/ml) is prepared by adding 5 ml of 0.9% sodium chloride solution for intravenous injection to the vial with 40 mg of esomeprazole. Diluted esomeprazole solution is a clear liquid of colorless to pale yellow color.


Solution for intravenous infusion 40 mg is prepared by dissolving the contents of one vial with 40 mg of esomeprazole in 100 ml of 0.9% sodium chloride solution for intravenous injection.


Solution for intravenous infusion 80 mg is prepared by dissolving the contents of 2 vials with esomeprazole 40 mg in 100 ml of 0.9% sodium chloride solution for intravenous injection.


Diluted esomeprazole solution for infusion is a clear colorless to pale yellow liquid.