Ultop, 20 mg 14 pcs

Pharmacodynamics
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 basal and stimulated secretion, regardless of the nature of the stimulus. The drug is prodrug and is activated in the acid environment of the secretory tubules of the parietal cells. After a single oral dose, the action of omeprazole occurs within the first hour and continues for 24 hours, the maximum effect being reached after 2 hours.

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 to 97% with 20 mg omeprazole and by 92 to 94% with 40 mg. Inhibition of 50% of maximum secretion lasts for 24 hours.

Pharmacokinetics
Omeprazole is rapidly absorbed from the gastrointestinal tract, reaching maximum plasma concentration in 0.5-1 hours. Bioavailability is 30-40%. Bioavailability is slightly increased in elderly and patients with impaired liver function, and to a large extent in patients with chronic hepatic failure (can reach 100%). Binding to plasma proteins is about 90% to 95%. Omeprazole is almost completely metabolized in the liver with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.), pharmacologically inactive. It is an inhibitor of the CYP2C19 enzyme system. The elimination half-life is 0.5-1 hour. Excretion 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. In patients with hepatic insufficiency half-life is 2 – 3 hours.
Total clearance is 500 – 600 ml/min.

Indications

Active ingredient

Composition

1 capsule contains:

Active substance:

Omeprazole 20 mg.

Associates:

Sugarcane (sucrose, starch treacle);

Hyprolose;

Magnesium hydroxycarbonate;

Sucrose;

Corn starch;

Sodium lauryl sulfate.

How to take, the dosage

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

Duodenal ulcer in 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/d 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. A different registered dosage (Ultop® capsules 40 mg) is available to provide the dosing regimen below. 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 is indicated for 26-52 weeks, in severe esophagitis – for life.

Erosive-ulcerative gastrointestinal lesions caused by taking NSAIDs, – 20 mg/day for 4-8 weeks.

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

Antiretreatment of gastric and duodenal ulcer – 10-20 mg/day.

Antiretreatment of reflux esophagitis – 20 mg/d for a long time. On-demand administration is possible.

Sollinger-Ellison syndrome – the dose is adjusted individually depending on the baseline level of gastric secretion, usually starting at 60 mg/d. 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 2-4 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. Dose adjustment is not necessary for patients with impaired renal function.

Hepatic dysfunction. In patients with impaired liver function the bioavailability and clearance of omeprazole are increased. Because of this therapeutic dose should not exceed 10-20 mg per day.

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

Interaction

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 altered 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 (as omeprazole increases gastric pH).
As a cytochrome P450 inhibitor, omeprazole may increase the concentration and decrease excretion of diazepam, indirect anticoagulants, phenytoin, which in some cases may require reduction of doses of these drugs.
Simultaneous administration increases absorption of omeprazole and clarithromycina.

Special Instructions

Before initiating therapy, the presence of a malignant process (especially with gastric ulcer) should be excluded, since treatment, by masking symptoms, may delay the correct diagnosis.
No adjustment of the drug dose is required for elderly patients. The bioavailability of omeprazole is increased in patients with cirrhosis, but no increase in toxicity has been noted. The daily dose should not exceed 20 mg.
No dose adjustment is required for patients with renal disease. Dialysis in patients with chronic kidney disease has no effect on pharmacokinetic properties of omeprazole.
Effect on driving and other mechanisms
In usual dosages the drug does not affect the speed of psychomotor reactions and concentration of attention.

Contraindications

With caution:

Hepatic and/or renal insufficiency;

Hereditary intolerance of fructose;

Glucose and/or galactose malabsorption syndrome or sucrose/isomaltose deficiency.

Side effects

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

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

CCS:stenocardia, 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 disorders: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.

In the respiratory system:throat pain, cough, profuse nasal bleeding.

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

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

Laboratory findings:hypoglycemia, hyponatremia.

Others:back pain, increased sweating; rarely – formation of gastric gladular cysts during long-term treatment (consequence of inhibition of hydrochloric acid secretion, is benign, reversible), general fatigue, general weakness, increased body weight, 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.
treatment symptomatic. There is no specific antidote. Hemodialysis is ineffective.

Pregnancy use

Safety of use during pregnancy and lactation has not been studied. Therefore, it is not recommended to prescribe the drug during pregnancy. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Similarities