Esomeprazol 40-MV USP medicine for gastroesophageal reflux treatment, esophagus, gastrointestinal ulcer (3 blisters x 10 tablets)

pharmacokinetics

absorption:

Esomeprazol is absorbed quickly after drinking, the peak concentration of plasma is achieved after 1-2 hours. Esomeprazol's bioavailability increases according to the dose and when used to repeat, reaching about 68% when taking the dose of 20 mg and 89% when taking the dose of 40 mg. Food slows down and reduces the absorption, the area under the curve (AUC) after taking a single dose of 40 mg at meals compared to hunger decreases from 33 - 53%. So drink Esomeprazol 1 hour before meals.

Distribution:

About 97% Esomeprazol binds to plasma proteins.

Metabolism:

Esomeprazol is widely metabolized in the liver by the cytochrom P450 ISOENZYM CYP2C19 system into non -activated hydroxy and demethyl derivatives. The rest is converted through isenzyme CYP3A4 to Esomeprazol Sulfon. When used repeated, the initial metabolism through the liver and the clearance of the drug may be due to the inhibited ISOENZYM CYP2C19. However, there is no accumulated phenomenon when used once a day. In some Asians (15-20%) because of the lack of genetic ISOENZYMYMYMYM, slowing down the metabolism of Esomeprazol, resulting in an increase in AUC 2 times compared to people with enough enzymes.

Era:

Esomeprazol's waste sale time is about 1 - 1.5 hours, about 80% of oral doses are eliminated in the form of non -active metabolites in the urine, the rest is excreted through 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 they must reduce the dose for these objects and should not use more than 20 mg daily.

Pharmacokinetics in people under 18 years of age have not been studied.

Be cautious when used

Before taking proton pump inhibitors, it is necessary to eliminate the possibility of 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 nursing.The long -lasting

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

may increase the risk of diarrhea due to Clostridium difficile when using proton pump inhibitors.

When using proton pump inhibitors, especially when taking high and prolonged doses (over 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 at risk of osteoporosis should use enough calcium and vitamin D, assess bone condition and follow the instructions of health experts.

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).

Esomeprazol may reduce the absorption of vitamin B12 (cyanocobalamin) due to a decrease in stomach acid secretion. This should be carefully considered in patients with reduced vitamin B12 reserves or risk factors for reducing vitamin B12 absorption when long -term treatment.

Affects laboratory tests: Increasing Chromographin A (CGA) level may affect the test of endocrine nerve tumors. To avoid this influence, Esomeprazol should be stopped for at least five days before CGA. If the CGA and Gastrin concentrations do not return to the reference level after the initial measurement, the measurement must be repeated 14 days after stopping the treatment of Proton pump inhibitors.

Due to the micro-seed component containing sucrose, patients with rare genetic diseases in galactose tolerance, or malposive glucose-galactose should not be taken.

Be cautious when used for patients with diabetes.

The effect of drugs on driving and operating machinery

Some cases of dizziness, headache, dizziness when using Esomeprazol, therefore, use care of the drug while driving or operating machinery.

Using drugs for women during pregnancy and lactation

Using drugs for pregnant women

The drug does not affect the development of fetuses in humans and animals, but should only be used for pregnant women when necessary.

Using medicine for breastfeeding women

Because there is not enough data on the excretion of breast milk and the effects of the drug on the baby, it is not advisable to use esomeprazol in case of breastfeeding. In case of medication, it is necessary to stop breastfeeding.

Drug interaction

Esomeprazole inhibits acid secretion, increases gastric pH, so the drug can affect the bioavailability of some pH -dependent absorption drugs such as ketoconazole, digoxin, iron salt.

Simultaneous use of ecomeprazol, clarithromycin and amoxicillin increases the concentration of ecomeprazol and 14-hydroxyclarithromycin in the blood.

Esomeprazol interact with dynamic pharmacokinetics with metabolic drugs by the cytochrom P450 enzyme system P450 isoenzyme CYP2C19 in the liver. Simultaneously use 30mg of Esomeprazol and Diazepam, reducing Diazepam's 45% of clearance.

Esomeprazol may increase the blood concentration of Saquinavir and reduce the concentration of Nelfinavir and Atazanavir through an unclear mechanism. Therefore, it is advisable to consider reducing the dose of Saquinavir when used with Esomeprazol to avoid unwanted effects of Saquinavir.

Esomeprazol reduces the activity of clopidogrel metabolic enzymes into an active form, thus reducing the activity of clopidogrel, so it is recommended to use only the combination of these two drugs when it is really necessary.

Esomeprazol increases the concentration of cilostazol and its metabolites. The dose of cilostazol should be reduced from 100 mg twice a day to 50 mg twice daily when used with Esomeprazol.

methotrexate: When used with PPI, methotrexate levels have been reported in some patients. It is necessary to consider using high -dose methotrexate with esomeprazol.

tacrolimus: simultaneously used with Esomeprazol will increase the concentration of Tacrolimus. Strict monitoring of tacrolimus concentration as well as renal function (creatinine clearance) and adjust the dose of tacrolimus if necessary.

warfarin: Simultaneously use 40 mg of Esomeprazol for patients treated with warfarin in a clinical trial showing that blood clotting time is within the scope of acceptance. However, in some cases, the high -rise Inr clinical index has been reported during simultaneous treatment. It is recommended to closely monitor at the beginning and finish the simultaneous treatment of ecomeprazol with warfarin or other cooumarin derivatives.

Phenytoin: Simultaneously use 40 mg of Esomeprazol, resulting in a 13% increase in phenytoin plasma concentrations in epilepsy patients. It is recommended to closely monitor phenytoin concentrations in plasma when treated with esomeprazol.

CYP2C19 and/or CYP3A4 inhibitors: Esomeprazol is metabolized by CYP2C19 and CYP3A4. Concomitant use of Esomeprazol and a CYP3A4 inhibitor (such as Clarithromycin) led to double the AUC index of Esomeprazol. Concomitant use of Esomeprazol and a synthetic inhibitor of CYP2C19 and CYP3A4 can lead to more than double the concentration of Esomeprazol.

CYP2C19 and/or CYP3A4 induction drugs: CYP2C19 or CYP3A4 induction drugs or both (such as rifampicin) can lead to reduced concentration in Esomeprazol serum by increasing Esomeprazol metabolism.