2010/06/16

Nexium

Name: Nexium

Mode of action:
Neksium (esomeprasol) - a specific inhibitor of proton pump of parietal cells of the mucous layer of the stomach. Is the S-isomer form of omeprazole. Cumulating and transformed into an active state in the secretory tubules, which inhibits the proton pump (enzyme H + K +-ATPase), thereby developing the inhibition of secretion of hydrochloric acid.

The drug takes effect within 60 minutes after taking 20-40 mg esomeprasol. Repeated application of 20 mg esomeprasol 24 hours 1 time per day accompanied by a decrease in gastric secretion caused by the action of pentagastrin on the 90% approximately 5 day admission.

At a dose of 40 mg is effective for the treatment of reflux esophagitis. It is used to treat ulcers gastric and duodenal ulcers, in combination with a suitable antibiotic can achieve a better effect of Helicobacter pylori (90%). Typically, when the complex treatment of peptic ulcer after taking antibiotics does not arise a need to continue antisecretory monotherapy.

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, is due to increase in concentration of gastrin in the blood. In some cases, an increase in the incidence of granular cysts of the gastric mucosa during long-term use of antisecretory drugs. This phenomenon is regarded as a physiological response to inhibition of production of hydrochloric acid. Cysts are always benign and transient (after treatment disappear).

Omeprazole is effective for prevention of peptic ulcers with concomitant therapy with nonsteroidal anti-inflammatory drugs (even inhibitors of COX - 2 selective group).

Neksium - of acid drug, use it in the form of granules, coated, inside. Esomeprasol rapidly absorbed, C max is achieved in plasma after about 60-120 minutes after internal use. Bioavailability after the adoption of a single dose of 40 mg - 64%, increasing to 90% in case of re-admission. At a dose of 20 mg absolute bioavailability of respectively 50%, 68%.
Blood plasma proteins bind 97% of the active substance. At the same time.The esomeprasol and food does not change antisecretory effect, but the absorption may be impaired.

Biometabolizm most esomeprasol occurs with the participation of the enzyme CYP 2S19, the rest of the - isomer of the enzyme: CYP 3A4, all reactions occur with the participation of cytochrome P450. The half-life of approximately 70 minutes after the second dose esomeprasol 24 hours. Eliminated by the kidneys completely in the interval between administration of the drug does not accumulate in the body when taking a once in 24 hours. A small portion is excreted in the feces esomeprasol. The metabolites of the drug have no effect on the secretion of hydrochloric acid. Less than 1% esomeprasol eliminated unchanged by the kidneys. Metabolism esomeprasol not changed in the case of elderly patients (71-80 years). Women have a higher value of AUC, than men (30%), the choice of doses for patients, male and female are not affected. Special patient groups are weak metabolizatory - people whose metabolism is due only to the influence of CYP 3A4.U weak metabolizatorov figures AUC (average per day) to 100% higher than in those who have expressed and active isomer (metabolizatory extensive) - enzyme CYP 2C19. The choice of dosage for that and other groups are not affected. Metabolic disorders esomeprasol studied in patients with liver failure is not revealed. Biotransformation rate decreased only when expressed violations, which leads to an increase in AUC of 2 times. Due to this, use the recommended dose for such patients esomeprasol equal to 20 mg per day.

No study to identify characteristics esomeprasol metabolism in patients with renal insufficiency. Because the kidneys are not eliminated in the active substance and metabolites, a biotransformation of violations should not be expected. The studies in adolescence - the effect of options and the maximum concentration of omeprazole in blood plasma from 12 years are the same as in patients of adult age.


Indications:
• therapy of Zollinger-Ellison syndrome;
• reflux esophagitis (both symptomatic therapy as well and anti-treatment, and etiologic treatment of peptic forms reflux gastritis);
• eradication of Helicobacter pylori - in complex treatment with antibacterial drugs for stomach ulcers and duodenal ulcers;
• Preventive treatment of peptic ulcers in NSAID use, treatment of ulcers caused by nonsteroidal antiinflammatory drugs.


Instructions:
Neksium used only for internal use, tablets should be swallowed without chewing, drink a little water. If any of swallowing function can put a tablet in water (100 ml, still) and have a drink after the dissolution of tablets immediately (or within 30 minutes). Other solutions (tea, milk) to use, you should not - it can damage the special coating of tablets. Once the liquid is drained, you must take an additional 1 cup of water and use the same glass. In an extreme case, disturbancies swallowing function should enter neksium through a tube (nasogastric). Before the introduction of the tablet is dissolved in water by the method already described. Dissolved in water neksium gain by 5-10 ml syringe suitable to probe the size and enter into the probe.

Treatment of reflux esophagitis
At 40 mg / day for 4 weeks, if symptoms persist, therapy can be extended for a further 4 weeks. As a preventive treatment using a dose of 20 mg / day. For relief of symptoms with reflux esophagitis used 20 mg / day for 4 weeks, while maintaining the signs of the disease need to clarify the diagnosis. For further control, you can use 20 mg / day, or "on demand". Do not use neksiuma "on demand" as a preventive therapy to persons using NSAIDs with an increased risk of peptic ulcers.

In the complex treatment of gastric ulcer and duodenal ulcer associated with Helicobacter pylori infection, or as a preventive treatment.
20 mg esomeprasol combined and amoxicillin (1000 mg) and clarithromycin (500 mg) 2 p / day for 1 week.
Patients administered non-steroidal anti-inflammatory drugs for a long time: 20 mg / 1 p / day. In the treatment of peptic ulcers caused by NSAIDs, the duration of therapy is 4-8 weeks.

Syndrome Zollinger - Ellison - 40 mg, 2 p / day. The duration of treatment and dose are selected individually depending on the clinical situation. The maximum permissible dose for patients with this deficiency syndrome - 80-160 mg / day.

When liver failure esomeprasol maximum permissible dose is 20 mg / day. No dosage adjustment in patients with renal insufficiency, however, marked disturbances of renal function neksium be used with caution.


Side effects:
Central nervous system and peripheral nervous system: drowsiness, depression, paresthesia, aggression, insomnia, irritability, dizziness, hallucinations (especially in severely ill).
Gastrointestinal tract: candidiasis, stomatitis.
The system of blood and blood: thrombocytopenia, leukopenia, pancytopenia, agranulocytosis.

Liver: hepatitis (with or without jaundice), encephalopathy (in case of severe liver disease in history), liver failure.
Musculoskeletal system: muscle weakness, joint pain.
Skin: photosensitivity, rash, toxic epidermal necrolysis, alopecia.

Other: hypersensitivity reactions (bronchospasm, fever, nephritis, increased sweating), edema, hyponatremia, changes in taste.


Contraindications:
• age 12 years (ostutstvuyut clinical studies in this age group);
• hypersensitivity reactions (including benzimidazole);
• by atazanavir.


Pregnancy:
Very little data on the use esomeprasol pregnant, and the drug prescribed with caution. In clinical experiments revealed no embryotoxicity or teratogenicity neksiuma, impact on family process and nurturing pregnancy, the rate of postnatal period. It is not known about the probability of penetration neksiuma in breast milk - during lactation drug appoint not recommended.


Interaction with other drugs:
If you suck other drugs depends on the acidity of gastric contents, then esomeprasol may increase or decrease the capacity for absorption. In therapy esomeprasol a decrease in suction itrokonazola and ketoconazole. The suppression of elaboration of CYP 2C19 leads to increased concentration in the blood plasma of those drugs, biometabolizm which occurs with the participation of this enzyme: Citalopram, diazepam, clomipramine, phenytoin, imipramine. Usually, this requires a reduction in dosage of the latter.
In applying esomeprasol to monitor indicators of coagulation with the simultaneous use of warfarin and esomeprasol.

With the combination esomeprasol tsizaprida and there is an increase of 32% AUC and an increase in half-life tsizaprida (31%), but significant fluctuations in blood concentrations tsizaprida not observed. In some cases, a marked increase in QT interval, but in combination with esomeprasol progression of increasing the interval were found. The combination of atazanavir, ritonavir observed decrease in the activity of antiviral drugs, even at higher dosages.

Because the active ingredient neksiuma metabolized by enzymes CYP 3A4 and CYP 2C19, the combined reception esomeprasol and clarithromycin, which is an inhibitor of the enzyme activity of CYP 3A4, there is an increase AUC neksiuma. This correction dosage esomeprasol not required.

The combined use of voriconazole and esomeprasol increases exposure of the last more than 2 times (correction dosage neksiuma not required).


Overdose:
Very little data on cases of overdose esomeprasol. It is known that the use neksiuma a dose of 80 mg did not cause any marked toxic effects. After using the drug at a dose of 280 mg there is a general weakness, signs of violation of the gastro-intestinal tract. Specific antidote in esomeprasol no. Hemodialysis is ineffective, as the drug most associated plasma proteins. If symptoms of overdose spend supportive and symptomatic therapy.


Product:
Tablets of 20, 40 mg, and 7 pieces in blister in carton 1, 2 or 4 blisters. Tablets are light-pink, biconvex, oblong, one side engraved "20 mG» (tablet 20 mg) or "40 mG» (for tablets of 40 mg), on the other side is engraved a fraction A / EN ".


Storage:
In a place which is inaccessible to children. Temperature - not above 30 ° C.


Ingredients:
Active ingredient: esomeprasol (as sodium trihydrate).

Other ingredients: iron dioxide, red-brown (£ 172), magnesium stearate, glitserolmonostearat 40-55, iron oxide yellow (E172), polysorbate 80, macrogol 6000, METHACRYLIC-acid ethyl acrylate copolymer 1:1, sugar, gidroksipropiltsellyuloza, sodium stearyl fumarate, triethylamine citrate, microcrystalline cellulose, titanium dioxide (E171), gipromelloza, talc, krospovidon, synthetic paraffin.


Extras:
Receiving neksiuma contributes masking signs of malignant disease of the stomach, therefore should be excluded before prescribing esomeprasol neoplasm (especially in cases of weight loss, dysphagia, bleeding from the gut - or melena gematemezis, nausea). Those patients who take medication more than 1 year should be under the supervision of medical staff. Should inform patients taking neksium "on demand", that in case of any new symptoms of this need to tell your doctor. The drug is not prescribed in case of intolerance (hereditary nature) of fructose or glucose malabsorption (galactose), or in cases of lack izomaltozy-sucrose.
Receiving neksiuma does not affect the ability to drive vehicles or work with complex mechanisms.


Warning
Before using the product Neksium you should consult your doctor. This instruction is given a free transfer and is intended solely for information. For more information, please contact the manufacturer annotations.