Esotrax 40 Mepro medicine for gastroesophageal reflux, esophagus, healing duodenal ulcer (3 blisters x 10 tablets)

Position and impact mechanism

Esomeprazol is a weak, concentrated and transformed basic into a highly acidic environment in the sub-control tube of the cell's secretion, where H+K+--Aatpase inhibitors (acid pump) and inhibit both basic fluid and stimulating fluid.

Acting on gastric acid secretion

After taking the oral dosage of Esomeprazol 20 mg and 40 mg, the drug has an impact within 1 hour.

After repeating the dose of Esomeprazol 20 mg, 1 time/day for 5 days, the maximum maximum acid secretion after stimulation with Pentangastrin decreases 90% when measured at 6-7 hours after taking the drug on the 5th day.

After 5 days of taking the oral dose of Esomeprazol 20 mg and 40 mg of pH in the stomach> 4 has been maintained within the average time, respectively, 13 and 17 hours within 24 hours in patients with symptoms of gastroesophageal reflux.

The percentage of patients maintaining the pH in the stomach at a minimum of 8. 12 and 16 hours corresponding to 76%, 54% and 24% for esomeprazol 20 mg and 97%. 92% and 56% for Esomeprazol 40 mg.

When using AUC as a parameter representing the concentration of plasma drugs, people have proven to have a relationship between acid secret inhibition and concentration and contact time.

The therapeutic effect of acid inhibition

When using Esomeprazole 40 mg, about 78% of patients with esophagitis due to reflux are healed after 4 weeks and about 93% are healed after 8 weeks.

Esomeprazol treatment 20 mg, 2 times/day and appropriate antibiotics during the week have eradicated Helicobacter pylori successfully in about 90% of patients.

After 1 week of eradication treatment, no additional anti -acid drugs to heal ulcers and reduce symptoms in patients with uncomplicated duodenal ulcer.

Other effects related to acid inhibition

During the treatment with anti -acid antimicrobial drugs, the serum galastine concentration responds to a reduction of gastric acid.

After a long period of treatment with gastric acid -secreting drugs, there has been a relatively increased frequency of gastric follicles. These changes are due to the intense but benign and recovery inhibitors.

pharmacokinetics

absorption and distribution

Esomeprazol is easily canceled in an acidic environment and is taken in the form of a grain soluble in the intestine.

In animals (in vivo), the transition to isomer r is negligible.

Esomeprazol is quickly absorbed with peak plasma concentrations reaching about 1-2 hours after drinking.

Absolute bioavailability is 64% after taking a single dose of 40mg and increased to 89% after the dose is repeated once a day. For the dose of Esomeprazol 20mg, these values ​​correspond to 50% and 68%.

Expected distribution integral in a healthy state is about 0.22 l/kg of body weight. Esomeprazol binds 97% to plasma protein.

Food slows down and reduces the absorption of Esomeprazol, although this does not significantly affect the effects of Esomeprazol on gastric acid secretion.

metabolism and excretion

Esomeprazol is completely metabolized through the Cytochrom P450 (CYP) system. The main part of Esomeprazol metabolism depends on the morphological CYP2C19 enzyme, forming the metabolites of hydroxy and desmethyl of Esomeprazol.

The rest of the metabolic process depends on another specific homogeneous substance, CYP3A4, forming Esomeprazol Sulfon, the main metabolite in plasma.

The following parameters mainly reflect pharmacokinetics in individuals with CYP2C19 function yeast, a group of strong metabolic people.

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

The area under the curve shows the plasma concentration over time (AUC) increases after repeated use of esomeprazol. This increase depends on the dose and the increase in AUC rise than the dose ratio after the dose is repeated.

This time and dosage dependence is due to the decrease in the first stage of the liver and reducing the body clearance is probably due to the inhibition of Esomeprazol's CYP2C19 enzyme and/or sulfon metabolites. Esomeprazol completely eliminated from plasma between doses without a tendency to accumulate when used 1 time/day.

The main metabolites of Esomeprazol does not affect stomach acid secretion. About 80% of Esomeprazol oral dose is excreted in the urine in the form of metabolites, the rest through feces. Less than 1% of constant drugs found in urine.

Instructions on how to handle ADR:

With minor adverse reactions, usually just stop the drug. In case of severe sensitivity or allergic reactions, supportive treatment (airy keeping and using epinephrin, oxygen breathing, antihistamine, corticoid ...).

Caution when using

when there is any alert symptom (such as significant weight loss, recurrent vomiting, difficulty swallowing, vomiting blood or black defecation) and when suspected or stomach ulcer, should eliminate malignant diseases. Because Esomeprazol treatment can reduce symptoms and delay in diagnosis.

Patients with long -term treatment (especially those who have been treated for more than 1 year) should be monitored regularly.

Patients with demand should be contacted with a doctor if there are symptoms that change in characteristics. When prescribing Esomeprazol for demand treatment, it is advisable to consider interaction associated with other drugs due to the change in the plasma Esomeprazol level (see drug interactions).

When prescribing Esomeprazol to eliminate Helicobacter pylori, drug interactions should be considered in the 3 -drug treatment regimen. Clarithromycin is a strong CYP3A4 inhibitor and therefore should consider contraindicated and interact with clarithromycin when taking 3 drugs for patients who are taking other drugs metabolized through CYP3A4 as Cisapride.

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

Drug interaction

The reduction of stomach acid when treated with ecomeprazol may increase or reduce the absorption of other drugs if the absorption mechanism of these drugs is affected by stomach acid. Like other gastric acid secretions or antacids, the absorption of ketoconazole and iTraconazole may decrease during treatment with ecomeprazol.

Esomeprazol inhibits CYP2C19, Esomeprazol metabolism.

Therefore, when Esomeprazol is used with metabolic drugs with CYP2C19, such as Diazepam, Citalopram, Imipramine, Clomipramine, Phenytoin ... The concentration of these drugs in plasma can increase and need to decrease the dose. This should be paid special attention when prescribing Esomeprazol for treatment according to demand.

Concentrated with Esomeprazol 30 mg reduces 45% of Diazepam clearance is the substrate of CYP2C19. When used simultaneously with Esomeprazol 40 mg increases 13% of the bottom concentration of phenytoin in plasma in epilepsy patients. Should monitor phenytoin concentration in plasma when starting or stopping treatment with Esomeprazol.

In healthy volunteers, when used with 40 mg of Esomeprazol, the area under the curve shows Cisapride concentration in plasma over time (AUC) increases to 32% and the half -life of Cisapride exhaust is 31% but the cisapride peak concentration in plasma increases is not significant.

The qtc distance is slightly lasting, after using Cisapride separately, it is not longer lasting when used simultaneously Cisapride with Esomeprazol.

Esomeprazol has been shown to have no significant clinical impact on pharmacokinetics of amoxicilline, quinidine or warfarin.

The effect of the other drugs on Esomeprazol

Esomeprazol is metabolized by CYP2C19 and CYP3A4. When using Esomeprazol simultaneously with a CYP3A4 inhibitor, Clarithromycin (500 mg, 2 times/day) double the area under the curve (AUC) of Esomeprazol. No need to adjust the dose of Esomeprazol.