Ulcozol^® (Capsules) Instructions for Use

Marketing Authorization Holder

Laboratorios Bagó, S.A. (Argentina)

Contact Information

B-C FARMA B.V. (Netherlands)

ATC Code

A02BC01 (Omeprazole)

Active Substance

Omeprazole (Rec.INN registered by WHO)

Dosage Form

Ulcozol®

Capsules 20 mg: 7, 14, or 28 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 2, with a white body and a gray cap; the capsule contents are pellets from white to yellowish in color.

Excipients: sugar spheres, sodium lauryl sulfate, sodium phosphate dibasic, lactose monohydrate, hypromellose, hyprolose, hypromellose phthalate, diethyl phthalate, gelatin, titanium dioxide, iron oxide black.

7 pcs. – blisters (1) – carton packs.
7 pcs. – blisters (2) – carton packs.
7 pcs. – blisters (4) – carton packs.

Lyophilisate for preparation of solution for intravenous administration (included with solvent) white or almost white in color; the supplied solvent is a transparent colorless liquid; the prepared solution is slightly yellowish in color, transparent.

Solvent: macrogol 400, citric acid, water for injections – 10 ml.

Dark glass vials (1) in a set with solvent (amp. 1 pc.) – carton packs.

Clinical-Pharmacological Group

H⁺-K⁺-ATPase inhibitor. Antiulcer drug

Pharmacotherapeutic Group

Proton pump inhibitor

Pharmacological Action

Omeprazole inhibits the enzyme H⁺, K⁺-ATPase (“proton pump”) in the parietal cells of the stomach and thereby blocks the final stage of hydrochloric acid synthesis. This leads to a decrease in the level of basal and stimulated secretion, regardless of the nature of the stimulus. After a single oral dose, the effect of omeprazole occurs within the first hour and lasts for 24 hours, with the maximum effect achieved after 2 hours. In patients with duodenal ulcer disease, taking 20 mg of omeprazole maintains intragastric pH ≥ 3.0 for 17 hours. After discontinuation of the drug, secretory activity is fully restored within 3-5 days.

Pharmacokinetics

When taken orally, Omeprazole is rapidly absorbed from the gastrointestinal tract, C_max in plasma is reached within 0.5-1 h. Bioavailability is 30-40%. Protein binding is about 90%. Omeprazole is almost completely metabolized in the liver. The half-life is 0.5 -1 h. It is excreted by the kidneys (70-80%) and with bile (20-30%). In chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases, bioavailability increases. In hepatic insufficiency, bioavailability is 100%, T_1/2 increases to 3 h.

Indications

• Gastric and duodenal ulcer;
• Reflux esophagitis;
• Erosive-ulcerative lesions of the stomach and duodenum associated with NSAID use, stress ulcers;
• Erosive-ulcerative lesions of the stomach and duodenum associated with Helicobacter pylori (as part of combination therapy);
• Zollinger-Ellison syndrome;
• Prevention of aspiration of acidic gastric contents into the respiratory tract during general anesthesia (Mendelson’s syndrome).

ICD codes

Dosage Regimen

Capsules.

Orally. The capsules should be taken without chewing, with a small amount of liquid, regardless of meals (it is usually recommended to take in the morning before meals or during meals). If a twice-daily dose is necessary, the evening dose should be taken before dinner.

Duodenal ulcer in the acute phase – 20 mg/day for 2-4 weeks (in resistant cases up to 40 mg/day).

Gastric ulcer in the acute phase and erosive-ulcerative esophagitis – 20-40 mg/day for 4-8 weeks.

Erosive-ulcerative lesions of the gastrointestinal tract caused by NSAID use – 20 mg/day for 4-8 weeks.

Eradication of Helicobacter pylori – 20 mg 2 times/day for 7 days in combination with antibacterial agents.

Maintenance therapy for gastric and duodenal ulcer – 20 mg/day.

Maintenance therapy for reflux esophagitis – 20 mg/day for a long period (up to 6 months).

Zollinger-Ellison syndrome – the dose is selected individually depending on the initial level of gastric secretion, usually starting from 60 mg/day. If necessary, the dose can be increased to 80-120 mg/day, in which case it is divided into 2 doses.

Lyophilisate for preparation of solution for intravenous administration.

The drug is administered intravenously once a day in cases where oral administration is difficult.

The lyophilisate is dissolved in 10 ml of the supplied solvent (1 ampoule). Do not use other solvents!

The prepared solution should be used within 4 hours.

The solution is administered intravenously slowly over a period of at least 2.5 minutes at a rate not exceeding 4 ml/min.

If infusion administration of omeprazole is necessary, the lyophilisate is dissolved in the supplied solvent and then added to 100 ml of saline or 5% dextrose and the infusion is performed (intravenously drip over 20-30 minutes). The prepared solution can be stored at room temperature for no more than 12 hours.

For the prevention of Mendelson’s syndrome, 40 mg of the drug is administered 1 hour before surgery. If the operation lasts more than 2 hours, the dose of the drug should be repeated.

Adverse Reactions

From the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disturbances, stomatitis, transient increase in the activity of “liver” enzymes in plasma; in patients with pre-existing severe liver disease – hepatitis (including with jaundice), impaired liver function.

From the nervous system: headache, dizziness, agitation, drowsiness, insomnia, paresthesia, depression, hallucinations (in patients with severe concomitant somatic diseases), in patients with pre-existing severe liver disease – encephalopathy.

From the musculoskeletal system: muscle weakness, myalgia, arthralgia.

From the hematopoietic system leukopenia, thrombocytopenia; in some cases – agranulocytosis, pancytopenia.

Dermatological reactions: itching; rarely – skin rash; in some cases – photosensitivity, erythema multiforme, alopecia.

Allergic reactions: urticaria, angioedema, bronchospasm, interstitial nephritis and anaphylactic shock.

Other: visual disturbances, peripheral edema, increased sweating, fever, gynecomastia; rarely – formation of gastric glandular cysts during long-term treatment (a consequence of inhibition of hydrochloric acid secretion, is benign and reversible).

Contraindications

• Childhood;
• Pregnancy and breastfeeding period;
• Hypersensitivity to the drug.

Use with caution in patients with renal and/or hepatic impairment.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

The drug should be prescribed with caution to patients with hepatic impairment. In patients with severe hepatic impairment, the daily dose of the drug should not exceed 20 mg.

Use in Renal Impairment

The drug should be prescribed with caution to patients with renal impairment.

Pediatric Use

The drug is contraindicated for use in children.

Special Precautions

Before starting therapy, it is necessary to exclude the presence of a malignant process (especially in gastric ulcer), because treatment, by masking the symptoms, may delay the correct diagnosis.

Concomitant administration with food does not affect the effectiveness of omeprazole.

In patients with severe hepatic impairment, the daily dose of the drug should not exceed 20 mg.

Overdose

Symptoms: visual disturbances, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia.

There is no specific antidote.

Treatment: symptomatic therapy is performed. Hemodialysis is not sufficiently effective.

Drug Interactions

Long-term use of omeprazole at a dose of 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to a change in their plasma concentration.

No interaction with concomitantly taken antacids was noted.

May reduce the absorption of penicillin esters, iron salts, itraconazole and ketoconazole (Omeprazole increases gastric pH). Being an inhibitor of cytochrome P450, it may increase the concentration and reduce the excretion of diazepam, indirect anticoagulants, phenytoin (drugs that are metabolized in the liver via cytochrome CYP2C19), which in some cases may require a reduction in the doses of these drugs. Enhances the inhibitory effect on the hematopoietic system of other drugs.

Storage Conditions

Storage conditions

List B. Store in a dry, light-protected place, out of reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life

2 years. Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.