SWISS PHARMA SWISS PHARMA medicine treats gastroesophageal reflux, esophagus, gastric 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.

Dynamic pharmacokinetics

Esomeprazol absorbed quickly after drinking, reaching the highest concentration in plasma after 1 to 2
now. 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 under the curve (AUC) after taking a single dose of Esomeprazol 40 mg at meals compared to when hunger drops 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 medication is mainly metabolic in the liver thanks to isenzyme CYP2C19, the cytochrom P450 enzyme system, into hydroxyl and desmethyl metabolites that are no longer active.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.

Instructions on how to handle ADR

Must stop the drug when there is an unwanted effect.

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 Esomeprazol can cause gastritis or an increase in the risk of bacterial infections (such as inflammation
caught 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.

Esomeprazol interact with dynamic pharmacokinetics with specialized drugs by the cytochrom P450 enzyme system, isenzyme CYP2C19 in the liver (see the drug interaction).

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 reduction in unanimidated calcium absorption due to gastric pH increase.

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, reduction of steaming
Glucose-Galactose or Sucrase-Isomaltase deficiency should not be taken.

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 05 days before CGA.

Lupus erythematosus: Lupus erythematosus has been reported in patients using
proton pumps 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

can be used when driving and operating machinery but it should be noted because the drug can cause dizziness, headache.

Use drugs for women during pregnancy and nursing mothers

There is no adequate study when using Esomeprazol in pregnant people. On animals, white rats Esomeprazol dose 280 mg/ kg/ day (57 times the dose on humans calculated by body surface area) and rabbit oral dose of 86 mg/ kg/ day (35 times the dose on humans calculated by the body surface area) did not see evidence of reproductive or toxic fetus by fetal by Esomeprazol.

However, only use Esomeprazol when really necessary during pregnancy.

It is not known whether esomeprazol will excrete in human milk. However, Omeprazol's
concentration has been measured in women's milk after taking 20mg of omeprazol. Esomeprazol has the ability to cause serious unwanted effects in breastfeeding, 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,
isoenzyme CYP2C19 in the liver.

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

Simultaneous use of Esomeprazol with voriconazole may increase exposure to Esomeprazol more than 2 times more
, consider in patients with high doses of Esomeprazol (240 mg/day) like Zollinger - Ellison syndrome.

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 proton pump inhibitors that reduce the plasma concentration of the active metabolites of clopidogrel, reducing platelet resistance.

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 inhibits absorption and reduces 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 proton pump inhibitors, 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.

Protease inhibitor: Esomeprazol has been reported interacting with some protease inhibitors.

Hangered gastric pH in Esomeprazol treatment may change the absorption of protease inhibitors. Other possible interactive mechanisms occur due to CYP 2C19 inhibition. For Atazanavir and Nelfinavir, the decreased serum concentration has been reported when used in combination with ecomeprazol. Hence recommendations not to be used in combination.

For Saquinavir (combined with Ritonavir), there has been a report on the increase in serum levels (80-100%) during the treatment period along with Esomeprazol (40 mg/day).

Methotrexate: When used with PPI, methotrexate levels have been recorded in some patients. In high doses of methotrexate treatment, temporarily stop using Esomeprazol.

Phenytoin: Concomitance of 40 mg Esomeprazol increases the level of phenytoin in plasma
to 13% in epilepsy patients. Need to monitor phenytoin concentration in plasma when treated with
esomeprazol.

Cisaprid: simultaneously use Esomeprazol 40 mg increases 32% of the area under the curve (AUC) and
extending the sale time but does not significantly increase the concentration of Cisaprid's plasma peak. The distance of QTC lasts a little if using Cisapride separately, does not last longer when using Cisaprid in combination with Esomeprazol.