Ultop, 20 mg 28 pcs.

Ultop is a proton pump inhibitor.

Pharmacodynamics

Inhibits the enzyme H+-K+-ATPase (proton pump) in the parietal cells of the stomach and thus blocks the final stage of hydrochloric acid synthesis. This leads to a decrease in basal and stimulated secretion, regardless of the nature of the stimulus. After single oral administration, the action of omeprazole occurs within the first hour and lasts for 24 h, the maximum effect is reached after 2 h.

After discontinuation of the drug secretory activity is fully restored after 3-5 days. Basal gastric secretion decreases to 94% after 40 mg of omeprazole. Gastric acidity within 24 hours is reduced by 80-97% with 20 mg omeprazole and by 92-94% with 40 mg. Inhibition of 50% of maximum secretion lasts for 24 h.

Pharmacokinetics

Omeprazole is rapidly absorbed from the GI tract, Cmax in plasma is reached after 0.5-1 h. Bioavailability is 30-40%. Bioavailability is slightly increased in elderly patients and patients with hepatic impairment, and to a large extent in patients with chronic hepatic failure (can reach 100%). Binding to plasma proteins is about 90-95%. Omeprazole is almost completely metabolized in the liver to form 6 pharmacologically inactive metabolites.

It is an inhibitor of the enzyme system CYP2C19. T1/2 is 0.5-1 hours. Renal excretion is 70-80% and with the bile 20-30%. With impaired renal function, excretion of omeprazole decreases in proportion to the decrease in creatinine clearance. In liver dysfunction T1/2 is 2-3 h. Total clearance is 500-600 ml/min.

Indications

Active ingredient

Composition

1 capsule:

– omeprazole 10 mg, 20 mg or 40 mg

Supplementary substances:

Sugar granules,

sucrose,

corn starch,

hydroxypropylcellulose (hyprolose),

magnesium carbonate heavy,

sodium lauryl sulfate,

Methacrylic and ethylacrylic acid copolymer,

Talc,

Macrogol 6000,

Titanium dioxide,

Sodium hydroxide.

Capsule shell composition:

Titanium dioxide (E171), iron oxide (E172), gelatin.

How to take, the dosage

Overly, before meals, with a small amount of water (the contents of the capsule should not be chewed).

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

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

Gastroesophageal reflux disease (GERD): patients with moderate inflammation – 1 capsule (20 mg) once daily in the morning, before breakfast, for 4-8 weeks. To ensure the dosing regimen below, it is possible to take the drug in another registered dosage (Ultop® 40 mg capsules). Patients with severe GERD resistant to conventional therapy – 40 mg once daily, before breakfast. Duration of basic course is usually 4-8 weeks. After healing of erosive esophagitis maintenance treatment for 26-52 weeks is indicated, in severe esophagitis – for life.

Errotic ulcerative lesions of the gastrointestinal tract caused by taking NSAIDs – 20 mg/day for 4-8 weeks.

Eradication of Helicobacter pylori – 20 mg 2 times per day for 7 or 14 days (depending on the applied regimen) in combination with antibacterial agents.

Antiretroviral treatment of peptic ulcer of the stomach and duodenum – 10-20 mg/day.

Antiretroviral treatment of reflux esophagitis – 20 mg/day for a long time. On-demand administration is possible.

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

Non-ulcer dyspepsia – the usual dose is 10 mg to 20 mg once daily for 2 to 4 weeks. If the condition does not improve after 4 weeks of taking the drug, or if symptoms of dyspepsia reappear shortly after discontinuation, the diagnosis should be reconsidered.

Renal dysfunction. No dose adjustment is required for patients with impaired renal function.

Hepatic impairment. The bioavailability and clearance of omeprazole are increased in patients with hepatic impairment. Due to this reason, the therapeutic dose should not exceed 10-20 mg per day.

Elderly age. For elderly patients correction of the treatment regimen is not required.

Interaction

The long-term use of omeprazole at a dose of 20 mg once daily in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol has not resulted in changes in their plasma concentrations.

No interaction of omeprazole with concomitantly taken antacids was noted.

Omeprazole may decrease absorption of ampicillin esters, iron salts, itraconazole and ketoconazole (because omeprazole increases gastric pH).

As a cytochrome P450 inhibitor, omeprazole may increase concentrations and decrease excretion of diazepam, indirect anticoagulants, phenytoin, which in some cases may require reduction of doses of these drugs.

The absorption of omeprazole and clarithromycin is increased with concomitant administration.

Special Instructions

Before starting treatment it is necessary to rule out the presence of a malignant process in the upper gastrointestinal tract (since treatment may mask symptoms and complicate diagnosis).

In special cases, if there is difficulty in swallowing the whole capsule, its contents may be swallowed after opening or disgorging the capsule, or the contents of the capsule may be mixed with a slightly acidic liquid (juice, yogurt) and the resulting suspension may be used within 30 minutes.

Contraindications

With caution: renal and/or hepatic impairment.

Side effects

Digestive system disorders: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disorders, stomatitis, transient increase in plasma liver enzyme activity; in patients with previous severe liver disease – hepatitis (including jaundice), liver function abnormality.

Nervous system disorders: headache, dizziness, agitation, drowsiness, insomnia, paresthesia, depression, hallucinations; in patients with severe concomitant somatic diseases, patients with previous severe liver disease – encephalopathy.

Systemic diseases: angina, tachycardia, bradycardia, palpitations, increased BP, vasculitis, peripheral edema.

Urogenital system disorders: interstitial nephritis, urinary tract infections, microscopic pyuria, proteinuria, hematuria, glucosuria, increased serum creatinine concentration, gynecomastia, testicular pain.

Musculoskeletal system: muscle weakness, myalgia, arthralgia, bone pain, muscle cramps.

Hematopoietic system disorders: pancytopenia, agranulocytosis, anemia, neutropenia, thrombocytopenia, leukocytosis, leukopenia.

Skin disorders: petechiae, skin itching, skin rash; in some cases – photosensitization, erythema multiforme exudative, hair loss, alopecia, dry skin, epidermal toxic necrolysis, Stevens-Johnson syndrome.

Respiratory system disorders: sore throat, cough, profuse nasal bleeding.

Sensory organs: ringing in the ears, mild visual and hearing impairment.

Allergic reactions: urticaria, angioneurotic edema, bronchospasm, interstitial nephritis, anaphylactic shock, fever.

Laboratory parameters: hypoglycemia, hyponatremia.

Others: back pain, increased sweating; rarely – formation of gastric glandular cysts during long-term treatment (consequence of inhibition of hydrochloric acid secretion, is benign and reversible), general fatigue, general weakness, weight gain, fever.

Overdose

Symptoms: abdominal pain, drowsiness, headache, dizziness, dry mouth, tachycardia, arrhythmia, blurred vision, agitation, confusion, increased sweating, nausea; in rare cases – seizures, shortness of breath, hypothermia.

There is no specific antidote.

Treatment: symptomatic.

Pregnancy use

Ultop should not be used during pregnancy.

If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be addressed.

Similarities