Ezolong

One of the most common drugs for the treatment of peptic ulcer disease and gastroesophageal reflux is Ezolong, an antiulcer drug, the so-called proton pump inhibitor, the main substance of which is esomeprazole.

Indications Ezolong

Ezolong is prescribed as a primary or auxiliary drug in the following situations:

• with erosive reflux esophagitis;
• to prevent recurrence of esophagitis;
• to relieve the condition of reflux disease;
• for duodenal ulcers caused by Helicobacter pylori;
• for the prevention of recurrence of peptic ulcer disease in patients infected with Helicobacter pylori;
• for ulcers caused by taking non-steroidal anti-inflammatory drugs;
• to prevent the formation of ulcers when taking non-steroidal anti-inflammatory drugs;
• in Zollinger-Ellison syndrome.

Release form

Ezolong is produced as film-coated tablets. One tablet may contain 20 or 40 mg of the active ingredient esomeprazole.

Tablet appearance: oval, convex on both sides, slightly pinkish (40 mg) or yellowish (20 mg), with a transverse dosing notch on one side.

An aluminum blister plate contains 7 tablets. One cardboard package contains one or two blister plates, as well as instructions for this drug.

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Pharmacodynamics

Ezolong is represented by the active ingredient esomeprazole, the s-isomer of omeprazole, which is known as a gastric secretion suppressant. Esomeprazole is a specific proton pump inhibitor with targeted pharmacodynamic activity.

The active ingredient of the drug Ezolong belongs to weak bases - the substance accumulates and is activated in the acidic environment of the excretory channels of the parietal cellular structures, where inhibition of the enzyme H+K+ATPase - the acid pump, as well as inhibition of acid production occurs.

Pharmacokinetics

The drug is absorbed quickly, reaching high concentrations within half an hour after taking the dose. Complete bioavailability can be 90%. Plasma protein binding is 95%.

Simultaneous consumption of food reduces absorption and slows down the assimilation of Ezolong.

The drug is metabolized by the cytochrome P450 system. A large percentage of metabolism is dependent on CYP3A4, which is responsible for the formation of esomeprazole sulfone, the main plasma metabolite.

The half-life is 60-90 minutes. The plasma concentration-time ratio increases with repeated administration of the drug. This increase depends on the dosage of Ezolong and provokes a non-linear dependence of the “dose – AUC” type with repeated administration.

This time dependence is due to a decrease in first-pass metabolism, as well as systemic clearance rates due to inhibition of the CYP2C19 enzyme.

The active substance is completely eliminated from the bloodstream in the period between doses, without accumulation, with daily intake of Ezolong once a day.

The presence of the main metabolic products does not show any effect on the production of gastric juice. Approximately 80% of the taken amount of the drug leaves the body with urine, and the rest - with feces.

Dosing and administration

Ezolong is taken one hour before meals with water. The tablets are not crushed or chewed.

For the erosive form of reflux esophagitis, 40 mg of the drug is prescribed daily for a month.

To relieve symptoms of gastroesophageal reflux disease, 20 mg is prescribed daily, provided that there is no esophagitis.

For long-term prevention of recurrent esophagitis, 20 mg of the drug is prescribed daily.

In case of diagnosed Helicobacter pylori and duodenal ulcer, 20 mg of Ezolong with Amoxicillin and Clarithromycin are prescribed twice a day for a week.

To prevent relapses of Helicobacter pylori and peptic ulcer disease, 20 mg of Ezolong with Amoxicillin and Clarithromycin are prescribed twice a day for a week.

To treat ulcers caused by taking non-steroidal anti-inflammatory drugs, 20 mg of the drug is prescribed daily for 1-2 months.

For the treatment of Zollinger-Ellison syndrome, 40 mg of the drug is taken twice a day. However, the dose may be changed depending on clinical indications. It is permissible to take 80 to 160 mg of the drug per day (divided into 2 doses).

In case of impaired renal or hepatic function, as well as for elderly patients, it is not necessary to adjust the amount of the drug taken.

Use Ezolong during pregnancy

There is no clear and reliable information about the use of the drug Ezolong during pregnancy, which does not allow us to recommend this drug for use by pregnant patients.

There is also no information regarding the possibility of treatment with the drug during lactation.

Contraindications

Ezolong is contraindicated:

• in case of hypersensitivity to the drug;
• children under 12 years of age;
• in combination with the drugs Atazanavir and Nelfinavir.

Side effects Ezolong

Treatment with the drug Ezolong may be accompanied by some undesirable effects:

• a decrease in the number of leukocytes or platelets in the blood;
• allergy, anaphylaxis;
• swelling of the extremities associated with metabolic disorders;
• sleep disorders;
• states of overexcitement, depression;
• headaches, fatigue;
• visual and hearing impairment;
• dizziness;
• bronchospasm phenomena;
• dyspepsia, abdominal pain;
• thirst;
• jaundice, hepatitis;
• dermatitis, skin rashes, zonular alopecia;
• pain in joints and muscles;
• increased sweating.

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Overdose

Little information is available on Ezolong overdose. Signs of digestive system damage and a feeling of weakness occur after oral administration of 280 mg of the drug.

No specific antidote has been established.

Hemodialysis is considered ineffective, therefore, in case of overdose, symptomatic treatment and supportive therapeutic measures are limited.

Interactions with other drugs

The presence of reduced stomach acidity when taking Ezolong may affect the absorption of medications if their absorption processes depend on the degree of acidity. It has been noted that taking other drugs that inhibit acid production, as well as antacids, provokes a decrease in the absorption of Ketoconazole or Itraconazole during Ezolong therapy.

Ezolong in combination with drugs that metabolize CYP2C19 (Diazepam, Phenytoin, Imipramine) can provoke an increase in the concentration of the listed drugs. Given this, it is necessary to reduce their dosage.

Concomitant administration of 30 mg Ezolong will result in a 45% reduction in clearance of the substrate Diazepam.

Concomitant use of Ezolong will increase the concentration of Phenytoin in the blood serum of people with epilepsy. The amount of the drug in the bloodstream should be monitored at the time of administration or cancellation of Ezolong.

Taking Ezolong in combination with the drug Warfarin requires monitoring the quality of blood clotting.

Combination with Voriconazole and other CYP2C19 and CYP3A4 inhibitors may result in a more than two-fold increase in the exposure of the active component of Ezolong, which, however, does not require dosage adjustment of the drug.

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Storage conditions

Ezolong is stored in the original packaging at a temperature of up to +25°C, out of reach of children.

Shelf life

Ezolong can be stored for up to 2 years under proper storage conditions.