Ultop, 10 mg 14 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 CYP2C19 enzyme system. T1/2 is 0.5-1 hours. Renal excretion is 70-80% and bile excretion is 20-30%. In 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

short-term therapy of non-ulcer dyspepsia;
long-term maintenance therapy to prevent relapses of gastroesophageal reflux disease (GERD);
long-term maintenance therapy to prevent relapses of duodenal ulcers.

Pharmacological effect

Ultop is a proton pump inhibitor.

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 the level of basal and stimulated secretion, regardless of the nature of the stimulus. After a single dose of the drug orally, the effect of omeprazole occurs within the first hour and continues for 24 hours, the maximum effect is achieved after 2 hours.

After stopping the drug, secretory activity is completely restored within 3–5 days. Basal gastric secretion decreases to 94% after taking 40 mg of omeprazole. The acidity of gastric juice within 24 hours is reduced by 80–97% when taking 20 mg of omeprazole and by 92–94% when taking 40 mg. Inhibition of 50% of maximum secretion lasts 24 hours.

Pharmacokinetics

Omeprazole is rapidly absorbed from the gastrointestinal tract, Cmax in plasma is reached after 0.5–1 hour. Bioavailability is 30–40%. Bioavailability increases slightly in elderly patients and patients with impaired liver function, and to a significant extent in patients with chronic liver failure (can reach 100%). Plasma protein binding is about 90–95%.

Omeprazole is almost completely metabolized in the liver with the formation of 6 pharmacologically inactive metabolites. It is an inhibitor of the CYP2C19 enzyme system. T1/2 – 0.5-1 hour. Excretion by the kidneys – 70-80% and with bile – 20-30%. In case of impaired renal function, the excretion of omeprazole decreases in proportion to the decrease in creatinine clearance. In case of liver dysfunction, T1/2 is 2–3 hours. Total clearance is 500–600 ml/min.

Special instructions

Before starting treatment, it is necessary to exclude the presence of a malignant process in the upper gastrointestinal tract (since treatment can mask symptoms and complicate diagnosis).
In special cases, if you have difficulty swallowing a whole capsule, you can swallow its contents after opening or dissolving the capsule, and you can also mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

Active ingredient

Omeprazole

Composition

1 capsule contains:

Active substance:

omeprazole 10 mg;

Excipients:

granulated sugar (sucrose, starch syrup);

hyprolose;

magnesium hydroxycarbonate;

sucrose;

corn starch;

sodium lauryl sulfate.

Pregnancy

Ultop should not be used during pregnancy. If it is necessary to prescribe the drug during lactation, it is necessary to decide on stopping breastfeeding.

Contraindications

hypersensitivity to omeprazole or other components of the drug;
childhood;
pregnancy;
lactation period;
hereditary fructose intolerance;
glucose-galactose malabsorption syndrome;
sucrase/isomaltase deficiency.

With caution: renal and/or liver failure.

Side Effects

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 previous severe liver disease – hepatitis (including jaundice), impaired liver function.

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

From the cardiovascular system: angina pectoris, tachycardia, bradycardia, palpitations, increased blood pressure, vasculitis, peripheral edema.

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

From the musculoskeletal system: muscle weakness, myalgia, arthralgia, bone pain, muscle cramps.

From the hematopoietic system: pancytopenia, agranulocytosis, anemia, neutropenia, thrombocytopenia, leukocytosis, leukopenia.

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

From the respiratory system: sore throat, cough, profuse nosebleeds.

From the senses: ringing in the ears, mild visual and hearing impairment.

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

Laboratory indicators: hypoglycemia, hyponatremia.

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

Interaction

Long-term use of omeprazole at a dose of 20 mg 1 time / 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 concentrations.
There was no interaction between omeprazole and concomitantly taken antacids.
Omeprazole may reduce the absorption of ampicillin esters, iron salts, itraconazole and ketoconazole (because omeprazole increases gastric pH).
Being an inhibitor of cytochrome P450, omeprazole can increase the concentration and reduce the excretion of diazepam, indirect anticoagulants, phenytoin, which in some cases may require a reduction in the doses of these drugs.
When taken simultaneously, the absorption of omeprazole and clarithromycin is enhanced.

Overdose

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

There is no specific antidote.

Treatment: symptomatic.

Storage conditions

In a dry place, at temperatures below 25 °C

Shelf life

2 years

Manufacturer

KRKA-RUS, Russia