Esozot Globe Treatment Treatment of esophageal ulcer due to reflux (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Esomeprazol

Ingredient

Composition information	Content
Esomeprazol	20mg

Uses

indications

Esozot drug indicated in the following cases:

Adults

Treatment of esophageal ulcer due to reflux; Prolonged control for patients with healed esophagitis to prevent recurrence; Treatment of gastroesophageal reflux symptoms.

Combined with some other drugs in the appropriate antibacterial regimen to kill H.pylori and duodenal ulcer caused by H. Pylori, prevent recurrence of peptic ulcer in cases of H.pylori ulcer.

For patients being treated with NSAID: Preventive and treatment of duodenum ulcers caused by NSAID; After that, continue the prolonged treatment to prevent bleeding after the treatment of peptic bleeding with intravenous sugar.

Treatment of Zollinger - Ellison syndrome.

Adolescents (12 years old)

Treatment of esophageal ulcer caused by reflux.

Prolonged control for patients with healed esophagitis to prevent recurrence.

Treatment of symptoms of gastroesophageal reflux.

Pharmacology

Pharmacological group: Proton pump inhibitors

ATC code: A02BC05

Esomeprazol is the S-Omeprazole isomer, which reduces gastric acid secretion through a specialized mechanism. Private inhibitors of proton pumps in the gastric border cells. Omeprazol's isomorphic isomers have similar pharmacological activity.

Mechanism of action

Esomeprazol is a weak base that is concentrated and moved to an active form in a highly acidic environment in the sub -control tubes of the border cell secretion, where this drug inhibits the H '/K*/ATPase - Proton pump and inhibits normal discharge or stimulating fluid.

Pharmacokology

After orally of 20 mg and 40 mg of Esomeprazol, the effect of the drug starts to appear within 1 hour. After repeating with the dose of Esomeprazol 20 mg and 40 mg once a day for 5 days, the pH in the stomach> 4 is maintained for an average period of about 13 hours and 17 hours, and about 24 hours in patients with gastroesophageal reflux. The proportion of patients taking the drug maintains the gastric pH level above 4 for at least 6, 12 and 16 hours when taking 20 mg dose of 76%, 54%and 4%respectively; For 40 mg, equivalent is 97%, 92%and 56%.

In many studies, the area under the AUC curve is considered a parameter representing the concentration of drugs in plasma, proving the link between acid secret inhibition and agriculture and drug use time.

A gastroesophageal reflux syndrome is healed over 78% of patients after 4 weeks and about 93% after 8 weeks when taking Esomeprazol 40 mg.

Combined treatment of Esomeprazol 20 mg with an appropriate antibiotic for 1 week shows that H.pylori is completely destroyed in 90% of patients.

After 1 week of H. Pylori's treatment, it is not necessary to add more anti -secretions to treat ulcers effectively and overcome symptoms of uncomplicated duodenal ulcers.

There have been reports that gastric gland cysts appear relatively more often when long -term treatment with Esomepazol. This change is the physiological result of the inhibition of gastric acid secretion, benign and recovered.

Reducing stomach acid for any cause, including proton pump inhibitors, increases the number of gastrointestinal bacteria in the stomach. Treatment with proton pump inhibitors may increase the risk of gastrointestinal tract infections caused by Salmonella, Campylobacter, may have Clostridium difficile with boarding patients.

In two comparative pharmaceutical studies, Ranitidin, Esomeprazol shows the effect of healing stomach ulcers better in patients taking NSAID, including selective inhibitors on COX-2.

Clinical effectiveness

In two control studies with placebo, Esomeprazol shows a better effect in preventing stomach and duodenal ulcers in patients taking NSAIDs (for patients under 60 years old and/or having previously ulcered), including NSAID selected on COX-2.

Children

In a study conducted on children with gastroesophageal reflux (

Pharmacokinetics

Absorb

Esomeprazol is not durable in acidic environments and is used by oral in the form of antacids or soluble in the intestine. In the body, the hill of Esomeprazol into isomers R- is negligible.

Esomeprazol is quickly absorbed and achieved plasma peak concentrations after about 1-2 hours of taking the drug. The bioavailability of the drug is 64% after the first 40 mg dose and increased to 89% after repeated use; For 20 mg dose, these values are 50% and 68% respectively. Food slows down and reduces the absorption of ecomeprazol, although the effect of the drug on gastric acid secretion is not significantly affected.

Distribution

The apparent distribution integral in a healthy state is about 0.22 l/kg of body weight.

Esomeprazol binds to plasma proteins at 97%.

Metabolism

Esomeprazol is completely metabolized through the Cytochrom P450 (CYP) system. Most of the metabolism of Esomeprazol depends on the morphological CYP2C19, forming metabolites in the form of hydroxy and desmethyl of Esomeprazol. The rest of the metabolic process depends on a different enzyme CYP3A4, forming Esomeprazol Sulphon - the main metabolitus of the Esomeprazol in plasma.

Elimination

The following parameters mainly reflect pharmacokinetic processes in patients where metabolic enzymes are CYP2C19, with strong metabolic groups.

The total plasma clearance is about 17 l/hour after the single dose and about 9 l/hour after the dose is repeated.

Sell waste time in plasma is about 1.3 hours after the dose is repeated once a day. Esomeprazol's pharmacokinetics have been studied with a dose of up to 40mg, 2 times/day.

Esomeprazol is completely excreted from the plasma between the drug use without the trend of accumulation when taking the drug once a day.

The main metabolites of Esomeprazol does not affect the process of gastric acid secretion. About 80% of esomeprazol oral dose is excreted in the urine in the form of metabolites, the rest is excreted through stool. Less than 1% of the drug is found in urine in the form of an original drug.

linear/non -linear

Esomeprazol's

pharmacokinetics has been studied at a dose of up to 40 mg. The area under the AUC curve represents the plasma concentration over time increased after repeated use of Esomeprazol. This increase depends on the dose and leads to an increase in AUC when the dose is repeated. This dependence on time and dose is caused by a decrease in the liver and reducing the body clearance may be caused by the inhibition of the enzyme CYP2C19 of ecomeprazol and/or sulphon metabolites.

Special target groups

Weak metabolic group

about 2.9 ± 1.5% of the population is deficient in CYP2C19 function enzymes and is called a group of weak metabolic people. In these patients, the metabolism of Esomeprazol is catalyzed mainly by CYP3A4 enzyme. After the dose repeated Esomeprazol 40mg, 1 time/day, the average AUC value in the group of people metabolic is about 100% higher than patients with CYP2C19 function enzymes (strong metabolic people). The average peak concentration in the plasma of the drug increased by about 60%. These findings do not affect the dose of Esomeprazol.

Gender

After taking the single dose of Esomeprazol 40mg, the average AUC in women is about 30%higher than that of men. It is not noticed that the difference in AUC between the sexes after the dose is repeated once a day. These records do not affect the dose of Esomeprazol.

Hepatic failure

Esomeprazol's metabolism may be reduced in patients with mild to medium liver failure. The rate of drug metabolism decreases in patients with severe liver failure, resulting in double the AUC of Esomeprazol. Therefore, no overdose of a maximum of 20 mg in patients with severe liver failure. Esomeprazol or its main metabolites do not tend to accumulate when used once a day.

kidney failure

No studies have been conducted in patients with renal function impairment. Because the kidney is the agency responsible for the excretion of the metabolites of ecomeprazol but is not responsible for excreting drugs in the form of constant, it is thought that the metabolism of esomeprazol is unchanged in patients with impaired kidney function.

Elderly

Esomeprazol metabolism has not changed significantly in elderly patients (71 - 80 years old).

Children

Adolescents (12-18 years old): When using the drug repeated at the dose of 20 mg and 40 mg, AUC and the time to achieve the peak concentration of the drug in plasma in children from 12 to 18 years old is not different from adults with both dose levels.

Before taking Esozot Globe Treatment Treatment of esophageal ulcer due to reflux (3 blisters x 10 tablets)

How to use

Esozot drug used by oral.

Use as directed by the treating doctor. Drugs used by oral, no chewing or crushing drugs when used, the form of preparation is not suitable for patients who cannot swallow.

Dosage

Treatment of gastroesophageal reflux in adults and children over 12 years:

Treatment of esophageal ulcer due to reflux: 40 mg x 1 time/day for 4 weeks. It is recommended that treating 4 more weeks for patients whose esophagus has not been completely healed or people with persistent symptoms.

Prolonged treatment to prevent recurrence for patients with healed esophagitis: 20 mg x 1 time/day.

Symptomatic treatment of gastroesophageal reflux: 20 mg x 1 time/day for patients without esophagitis. If symptoms are not controlled after 4 weeks, patients need to continue treatment. Once the symptoms are healed, controlled after treatment by indicating the dose of 20 mg x 1 time/day.

Adults

Coordinate in H.pylori's elimination regimen: 20 mg Esomeprazol and 500 mg Clarithromycin, 2 times/day for 7 days.

Prophot and treatment of peptic ulcer due to NSAID use: 20 mg x 1 time/day for 4 - 8 weeks.

Prolonged treatment of reinforcement after bleeding after the treatment of peptic bleeding by vein: 40 mg x 1 day/time for 4 weeks.

Treatment of Zollinger Ellison syndrome: The initial dose is recommended to be 40 mg x 2 times/day. The following dose should be adjusted to suit the response of each patient and continue treatment when clinically indicated. The clinical data shows that most patients are controlled at the dose of 80 - 160 mg Esomeprazol/day. With a dose of over 80mg/day, it should be divided into 2 times/day.

Children over 12 years:

Treatment of duodenal ulcerative ulcerative ulcer: Select the appropriate treatment sketch according to the specific instructions of each country, the region about the local drug resistance and the treatment time (usually 7 days, but sometimes it can last up to 14 days), and select the appropriate antibacterial drugs. This treatment process should be supervised by a professional.

The recommended treatment regimen is as follows:

Weight 30 - 40 kg: Combined with 2 antibiotics: Esomeprazol 20 mg, Amoxicillin 750 mg and Clarithromycin 7.5mg/kg Weight x 2 times/day for 1 week.

Weight> 40 kg: Combined with 2 antibiotics: Esomeprazol 20 mg, Amoxicillin 1 G and Clarithromycin 500 mg x 2 times/day for 1 week.

Children under 12 years of age: No research data is available in patients under 12 years old, so they do not use drugs for children under 12 years old.

Dosage for patients with renal impairment: There is no need to adjust the dose for patients with renal impairment. Due to limited data on patients with severe renal failure, caution should be careful when indicated in this object.

Dosage for patients with liver failure: There is no need to adjust in patients with mild to medium liver failure. For patients with severe liver failure, it is recommended that the dose does not exceed 20 mg/day.

Elderly: No need to adjust the dose.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What do

do when using overdose? The described symptoms related to the use of 280mg dose are symptoms on the gastrointestinal tract and fatigue. Esomeprazol 80mg single doses are still safe to use. There is no specific detox. Esomeprazol is strongly connected to plasma proteins and therefore not easy to separate. In case of overdose, symptomatic treatment should be treated and used for common support measures.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

The most unwanted effects include: headache, abdominal pain, diarrhea and nausea (including after -sales studies). Safety characteristics are similar to each other between drugs, indications, age groups and patient populations. There is no relationship between unwanted effects and dosage.

The following adverse reactions have been recorded or suspected in Esomeprazol's clinical research programs and monitored after the drug to the market. There is no reaction related to the dose.

These reactions are arranged according to the frequency: very common> 1/10; Usually ≥ 1/100 to

Blood disorders and lymphatic systems

Rare: leukopenia, thrombocytopenia.

Rare: Hypersensitivity reactions such as fever, angioedema, anaphylaxis/anaphylaxis.

Uncommon: peripheral edema. Hypergathed blood magnesium may be associated with hypocalcemia. Hematoma reduction can also lead to hypokalemia.

Mental disorders

Less: Insomnia

Common: headache

Rare: blurred vision.

Uncommon: Dizziness.

Rare: Bronchospasm.

Digestive disorders

Common: abdominal pain, constipation, diarrhea, bloating, nausea/vomiting.

Unknown: Micro colitis

Uncommon: increased liver enzymes.

Less: dermatitis, itching, rash, urticaria.

Rare: baldness, light sensitivity.

Uncommon: hip fractures, wrists and spine (see "Warning and caution")

rare: joint pain, muscle pain.

Very rare: interstitial nephritis; In some patients with the accompanying kidney failure,

Reproductive and mammary disorders

Very rare: female mammary glands.

General and local disorders

Rare: Difficult, increased sweating.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

anti -contraindications Esozot in the following cases:

Patients with hypersensitivity to Esomeprazol, Benzimidazol derivatives or any ingredients of the drug.

Be cautious when using

When there is any alarm symptom such as significant weight loss, recurrent vomiting, difficulty swallowing, vomiting blood or defecation of black feces) and when suspected or have stomach ulcers, it is necessary to eliminate malignant abilities because Esomeprazol treatment can cover symptoms and slow diagnostic.

Patients with long -term treatment (especially patients treated for over a year) should be monitored regularly.

Patients are indicated to use the drug when necessary, need to be directed to cases that need to contact the doctor. When prescribing esomeprazol oral, it is necessary to consider the ability to interact with other drugs, as well as change the concentration of esomeprazol in plasma.

When using the H. Pylori elimination regimen combined with Esomeprazol and other drugs, it is necessary to consider the possible interactions in the 3 -drug treatment regimen. Clarithromycin is a powerful CYP3A4 inhibitor, contraindicated to use Clarithromycin simultaneously with drug products transformed through CYP3A4 as Cisaprid.

Proton pump inhibitors may increase the risk of gastrointestinal infections such as Samonella and Campylobacter, which can include C. Difficile in boarding patients.

It is not recommended to simultaneously use Esomeprazol with Atazanavir. If it is required to combine these two drugs, clinical monitoring should be closely monitored when combining Atazanavir at a dose of up to 400 mg and 100 mg of ritonavir, the dose of Esomeprazol is not allowed to exceed 20 mg.

Like other acid secretion inhibitors, Esomeprazol can reduce the absorption of vitamin B12 due to reduced or deficient gastric acid. This should be considered in patients with reduced vitamin B12 reserves or at risk of reducing vitamin B12 absorption when long -term treatment.

Esomeprazol is a CYP2C19 inhibitor. When starting or ending treatment with esomeprazol, it is necessary to consider the ability to interact with metabolic drugs through this enzyme. To prevent, should not use Esomeprazol and Clopidogrel simultaneously.

Proton pump inhibitors, especially high doses and for a long time (> 1 year) can slightly increase the risk of hip, wrist and spine fractures, mainly in the elderly or in people with other risk factors. An observation study found that proton pump inhibitors may increase the risk of 10-40%fractures, which may include other risk factors. Patients at risk of osteoporosis need to be cared for under the current clinical instructions and need to be provided with enough calcium and vitamin D.

Effects of the drug on test results: During the treatment of anti -stomach anti -acid, gastrin levels increased in response to a reduction in gastric acid. Chromographin A (CGA) concentration also increases due to reduced gastric acid. The increase in CGA levels can affect the detection and detection of endocrine nerve tumors.

Therefore, in order to avoid this effect, it is necessary to temporarily stop treatment with Esomeprazol for at least 5 days before quantifying CGA.

Serious reduction of blood magnesia has been reported in patients treated with pump inhibitors like Esomeprazol for at least 3 months, and in most cases in 1 year. The manifestations of severe blood magnesium loss such as fatigue, spastic spasticity, delirium, convulsions, dizziness, ventricular arrhyths can be silently and often ignored.

In the majority of patients, blood magnesium reduces are improved after adding magnesium and stopping the use of proton pump inhibitors. For prolonged patients or users of proton pump inhibitors with digoxin or other drugs that reduce blood magnesia such as diuretics, doctors need to check blood magnesium levels before starting and periodically during treatment.

The product contains lactose, therefore, the drug should not be used for patients with rare genetic problems that are galactose intolerance, lactase enzyme deficiency or glucose-galactose.

Use drugs for women during pregnancy and lactation

Pregnant women

There is no enough clinical data on the use of drugs on pregnant patients. With the form of Racemic Omeprazol mixture, data from epidemiological studies on large numbers of pregnant women show that the drug does not cause defects or toxicity on the fetus. Esomeprazol studies on animals also do not show any direct or indirect drugs on the development of embryos/fetal embryos. Animal studies with Racemic mixture also do not show direct or indirect effects on pregnancy, childbirth or development of babies after birth. However, it is necessary to be cautious when using drugs for pregnant women

breastfeeding women

It is unknown whether esomeprazol is excreted through breast milk or not, no research has been done in breastfeeding women. Therefore, do not use the drug for this object.

The effect of the drug on the ability to drive and operate machinery

Esomeprazol can cause unwanted effects such as headache, dizziness, so be careful when driving and operating machinery.

Drug interaction

Esomeprazol's effects on pharmacokinetics of drugs

The absorption drug depends on the stomach pH

Reducing gastric acid during ecomeprazol treatment and other proton pump inhibitors may reduce or increase the absorption of drugs when its absorption depends on the pH of the stomach. Using Esomeprazole can reduce the absorption of drugs such as Ketoconazole, Itraconazole and Erlotinib, and increase Digoxin absorption. Simultaneous use of Omeprazol 20 mg/day and Digoxin in healthy people, Digoxin's bioavailability increases 10%, very few reports on Digoxin poisoning. However, it is necessary to be cautious when indicating high doses of Esomeprazol in elderly patients, and closely monitoring Digoxin treatment.

Protease inhibitors

There is a report that omeprazole interacts with some protease enzyme inhibitors. It is unclear clinical importance and the mechanism of impact of the recorded interactions. Increasing stomach pH during treatment with omeprazol can lead to changes in the absorption of protease inhibitors. Another possible interactive mechanism is through the inhibition of CYP2C19 enzyme.

For Atazanavir and Nelfinavir, the serum concentration has been recorded when used with omeprazol, so it is not recommended to simultaneously use these drugs.

Short -term studies evaluate the use of Esomeprazol simultaneously with Naproxen or Rofecoxib, which has not identified any clinical pharmacokinetic interactions.

Results from studies on healthy subjects have shown that the pharmacokinetic/pharmacological interaction between clopidogrel (daily -dose of daily maintenance dose 75mg) and esomeprazol (40mg oral 1 time/day) leads to reduction of concentration and exposure time with active metabolites of clopidogrel average 40% and maximum inhibition of platelets (caused by ADP)

The inconsistent data on clinical manifestations of pharmacokinetic/pharmaceutical interactions of Esomeprazol on the main cardiovascular events have been reported from clinical observation and research studies. For careful purposes, the dynamic use of clopidogrel is not recommended.

The unknown mechanism

When used simultaneously with proton pump inhibitors, there has been a report on increasing methotrexate levels in some patients.

During high doses of methotrexate treatment, temporarily stop using Esomeprazol.

The effect of other drugs on Esomeprazol pharmacokinetics

Esomeprazol is metabolized through CYP2C19 and CYP3A4. Simultaneous use of Esomeprazol and a CYP3A4 inhibitor such as Clarithromycin double the area under the AUC curve of Esomeprazol. Simultaneous use of Esomeprazol and a synthetic inhibitor CYP2C19 and CYP3A4 can lead to an increase of esomeprazol more AUC times. CYP3A4, CYP2C19 and Voriconazole inhibitors increase 280% AUC of Omeprazol. Normally, no adjustment of the Esomeprazol dose in these two cases, however, it is necessary to consider adjusting the dose with patients with severe hepatic impairment or patients are indicated for treatment for a long time.

CYP2C19 or CYP3A4 induction drugs or both (such as rifampicin and St. John Wort) can reduce Esomeprazol levels in the blood by increasing the metabolism of Esomeprazol.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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