Sopezid 40 kwality treatment for gastroesophageal reflux disease, peptic ulcer (3 blisters x 10 tablets)

Prevention and treatment of stomach - duodenal ulcer due to nonsteroidal anti -inflammatory drugs.

Zollinger - Ellison syndrome.

Pharmacokology

Esomeprazol is the isomorphic form of omeprazol, used similar to omeprazol in the treatment of gastric ulcer - duodenum and gastroesophageal reflux disease.

Esomeprazol is associated with H+/ K+ - ATPSE (also known as proton pump) in the stomach wall cell, inhibiting this enzyme system, preventing the final step of acidic secretion into the stomach. So Esomeprazol has the effect of inhibiting the basic acid secretion and even when stimulated by any agent.

Esomeprazol is not an active form, converted into an active form thanks to the acidic environment in the border of the stomach.

Dynamic pharmacokinetics

Esomeprazole absorbed quickly after drinking, reaching the highest concentration in plasma after 1 to 2 hours. Esomeprazol's bioavailability increases according to the dose and when reminded, reaching about 68% after the dose of 20 mg and 89% when taking the dose of 40 mg. Food slows down and reduces the absorption of Esomeprazol, the area below the curved (AUC) after taking a single dose of Esomeprazol 40 mg at a meal compared to the time of hunger decreases from 33% to 53%. Therefore, taking Esomeprazol for at least 1 hour before meals.

About 97% Esomeprazol attaches to plasma proteins. The volume of distribution when the drug concentration is stable in healthy volunteers of 16 liters. The metabolic drug is mainly in the liver thanks to the isenzyme CYP2C19, the cytochrom P45O enzyme system, into hydroxyl and desmethyl metabolites that are no longer active. The rest is converted through ISOENZYM CYP3A4 to Esomeprazol Sulfon. When used repeated, initially metabolized through the liver and the clearance of the drug reduced, possibly due to the inhibited isoenzyme CYP2C19.

However, there is no phenomenon of accumulation of drugs when used once a day. In some people because of the lack of CYP2C19 due to genetics (15-20% of Asians), they should slow down the metabolism of Esomeprazol, resulting in an increase in AUC value about 2 times compared to people with enough enzymes. Half life eliminated in plasma 1 - 1.5 hours. About 80% of oral doses are eliminated in the form of non -active metabolites in the urine, the rest is eliminated in the feces. Under 1% of the mother is eliminated in the urine. In people with severe liver failure, AUC value is 2-3 times higher than that of people with normal liver function, so Esomeprazol is reduced in patients, the dose does not exceed 20 mg a day.

Be cautious when used

Before taking proton pump inhibitors, it is necessary to eliminate stomach cancer because the drug can cover symptoms, slow down the diagnosis of cancer. Be cautious when used in people with liver disease, pregnant or lactating women.

using ecomeprazol can cause gastric atrophy or an increased risk of infection (such as pneumonia in the community).

Gastrointestinal infections: Proton pump inhibitors can increase the risk of gastrointestinal infections such as Salmonella and Campylobacter, increasing the risk of diarrhea caused by Clostridium difficile.

Reducing vitamin B12 absorption: Esomeprazol can reduce the absorption of vitamin B12 (cyanocobalamin) due to reduced gastric acid secretion. Need to consider on long -term patients with Esomeprazol.

When using proton pump inhibitors, especially when taking high and prolonged doses (1 year), it may increase the risk of pelvic fractures, wrist or spine due to osteoporosis. The mechanism of this phenomenon has not been explained, but it may be due to reducing unanimidated calcium absorption due to gastric pH hypoglycemia. The lowest dosage recommendation works in the shortest possible time, suitable for clinical status.

Patients with risk of bone fractures due to osteoporosis should use enough calcium and vitamin D, assess bone condition and manage as instructed.

Hypotension (with or asymptomatic) rarely encountered in patients using prolonged proton pump inhibitors (at least 3 months or in most cases that last for more than 1 year).

Sucrose: Patients with rare genetic problems such as fructose intolerance, reducing glucose-galactose absorption or deficiency of sucrase-isomaltase should not be used.

Effects for test results: Increasing chromogranin A (CGA) can hinder the detection of nerve tumors. To avoid this intervention, Esomeprazol should be stopped at least 5 days before CGA.

Lupus erythematosus skin: Lupus erythematosus has been reported in patients using proton pump inhibitors including Esomeprazol. The onset usually occurs within a few days after starting treatment in both patients from children to the elderly. The common symptoms are rash, but joint pain and blood cell reduction have also been reported.

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

Caution when taking the drug when driving and operating machinery because the drug can cause dizziness, headache.

Use drugs for women during pregnancy and lactation

pregnancy: On animals, white rats oral Esomeprazol dose 280 mg/ kg/ day (57 times the dose on humans calculated by the body surface area) and the oral rabbit dose of 86 mg/ kg/ day (35 times the dosage on humans calculated by the surface area of ​​the body) did not see them in terms of reproduction or toxicity for the fetus due to the fetus due to Esomeprazol. However, only use Esomeprazol when really necessary during pregnancy.

Breastfeeding period: It is unknown whether esomeprazol is excreted into human milk or not. However, the concentration of omeprazol in women's milk after taking 20mg of omeprazol.

Esomeprazol is likely to cause serious unwanted effects in breastfed babies, so it is necessary to decide to stop breastfeeding or stopping the drug, depending on the importance of the medication for the mother.

Drug interaction

Due to the inhibition of acid excretion, Esomeprazole increases the gastric pH, affecting the bioavailability of the drugs dependent on pH: ketoconazole, iron salt, digoxin.

Esomeprazol interact with dynamic pharmacokinetics with specialized drugs by the cytochrom P450 enzyme system, isenzyme CYP2C19 in the liver.

Simultaneous use of Esomeprazol with cilostazol increases the concentration of Cilostazol and metabolites with its activity
, considering reducing the dose of Cilostazol.

Simultaneous use of Esomeprazol with voriconazole may increase exposure to Esomeprazol more than 2 times more
, review in patients with high doses of Esomeprazol (240 mg/day) like when treating the Zollinger-Elison.

Use Esomeprazol with CYP2C19 and CYP3 A4 induction drugs such as rifampin reduces Esomeprazol levels, avoiding simultaneous use.

may increase the risk of hypoglycemia when taking ecomeprazol and drugs that also causes hypoglycemia such as thiazid diuretics or diuretic. Check the Magnesi concentration before starting to use proton pump inhibitors and then periodically.

Atazanavir: can change the absorption when taking Atazanavir, reducing this concentration of drugs in plasma, which can reduce antiviral effects. Do not simultaneously inhibit the Proton and Atazanavir inhibitors.

Clopidogrel: Use the same medication inhibitors of the activity of clopidogrel, reducing protons to reduce the concentration of plasma of plasma effects.

Digoxin: Lowering blood magnesia due to prolonged use of proton pump inhibitors that cause heart muscle to increase sensitivity to digoxin, which can increase the risk of toxicity to Digoxin's heart. In patients who are using digoxin, check the magnesium concentration before starting to use proton pump inhibitors and periodically later.

Sucralfate: Inhibition of absorption and reducing the bioavailability of proton pump inhibitors. Use proton pump inhibitors at least 30 minutes before using sucralfat.

tacrolimus: Increased serum concentration of tacrolimus.

warfarin: Inrang and prothrombin time when using warfarin simultaneously with pump inhibitors
proton, can cause abnormal bleeding and death. Track Inr and prothrombin time when using simultaneously Esomeprazol and Warfarin.

Simultaneously use Esomeprazol and Clarithromycin, increasing the concentration of ecomeprazol and 14-hydroxyclarithromycin in the blood.

Simultaneous use of Esomeprazol and Diazepam reduces diazepam metabolism and increases the plasma diazepam concentration.