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

– Peptic ulcer of the stomach and duodenum (in the acute phase and anti-relapse treatment), incl. associated with Helicobacter pylori (as part of combination therapy);

– Gastroesophageal reflux disease (GERD), including reflux esophagitis and non-erosive forms of reflux disease (NERD);

– Erosive and ulcerative lesions of the stomach and duodenum associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs), stress ulcers;

– Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.

Pharmacological effect

Pharmacotherapeutic group:

a drug that reduces the secretion of gastric glands – a proton pump inhibitor. ATX :
A.02.B.C.01

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. The drug is a prodrug and is activated in the acidic environment of the secretory tubules of parietal cells. 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 after 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, the maximum concentration in plasma is reached after 0.5-1 hour. Bioavailability is 30-40%. Bioavailability increases slightly in the elderly and patients with impaired liver function, and to a significant extent in patients with chronic liver failure (can reach 100%). Connection with plasma proteins – about 90% – 95%.
Omeprazole is almost completely metabolized in the liver with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.), which are pharmacologically inactive. It is an inhibitor of the CYP2C19 enzyme system. The half-life is 0.5-1 hour. Excretion by the kidneys (70-80%) and bile (20-30%). In chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases. In liver failure, half-life

– 2 – 3 hours.

Total clearance – 500 – 600 ml/min.

Special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process (especially with a stomach ulcer), since treatment, masking symptoms, can delay the correct diagnosis.

Eating slows down the absorption of omeprazole, so it is recommended to take the drug before meals.

In special cases, if you have difficulty swallowing a whole capsule, you can swallow its contents after opening or dissolving the capsule, or you can mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

Ultop should be taken with caution in patients with liver cirrhosis; the daily dose should not exceed 20 mg.

Ultop should also be taken with caution in patients with renal failure. In patients on dialysis, the pharmacokinetic parameters of omeprazole do not change.

Ultop contains sucrose, so the drug is not recommended for use in patients with glucose and/or galactose malabsorption syndrome, or sucrose/isomaltose deficiency. The hydrosorbent capsule sealed into the cap of the bottle should not be swallowed!

Effect on ability to drive:
in normal dosages, the drug does not affect the speed of psychomotor reactions and concentration.

Active ingredient

Omeprazole

Composition

1 capsule contains enteric granules (sucrose, corn starch), hyprolose, magnesium carbonate, heavy, sucrose, corn starch, sodium lauryl sulfate.

Pellet shell: methacrylic acid and pellets:
Pellet core:

Active substance: omeprazole 20.00 mg Excipients: sugar

granules (sucrose, corn starch) 80.00 mg, hyprolose 4.80 mg, magnesium carbonate, heavy 20.00 mg, sucrose 32.20 mg, corn starch 26.50 mg, sodium lauryl sulfate 2.50 mg.

Pellet shell. methacrylic acid and ethyl acrylate copolymer (1:1), 30% dispersion1 31.00 mg, talc 6.00 mg, macrogol 6000 3.10 mg, titanium dioxide 1.90, sodium hydroxide 0.21 mg.

1 presented as dry weight of polymer Capsule shell composition:

Capsule BODY: iron dye red oxide E172 0.0875%, titanium dioxide E171 3%, gelatin up to 100%. Capsule COVER: red iron oxide dye E172 0.6153%, titanium dioxide E171 2%, gelatin up to 100%.

Pregnancy

The safety of use during pregnancy and lactation and breastfeeding 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.

Contraindications

– Hypersensitivity to omeprazole or other components of the drug;

– Children’s age (efficacy and safety in children has not been proven);

– Pregnancy;

– Lactation period.

With caution:
renal and/or liver failure, hereditary fructose intolerance, glucose and/or galactose malabsorption syndrome, or sucrose/isomaltose deficiency.

Side Effects

In rare cases, the following, usually reversible, adverse reactions may occur:

From the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, heartburn, dry mouth, taste disturbances, stomatitis, pancreatitis (including fulminant pancreatitis), loss of appetite, discoloration of stool, esophageal candidiasis, atrophy of the mucous membrane of the tongue, transient increase in the activity of “liver” enzymes and bilirubin in the plasma; in patients with pre-existing severe liver disease – hepatitis (including jaundice), impaired liver function or hepatic encephalopathy.

From the central or peripheral nervous system: headache,

dizziness, aggressiveness, apathy, nervousness, agitation, drowsiness, insomnia, tremor, vertigo, 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, arterial hypertension, vasculitis, peripheral edema.

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

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

From the hematopoietic system: pancytopenia, agranulocytosis, anemia (including hemolytic anemia), neutropenia, thrombocytopenia, leukocytosis, leukopenia.

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

From the respiratory system: cough, nosebleed.

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

Allergic reactions: urticaria, angioedema, bronchospasm,

interstitial nephritis, anaphylactic shock, fever.

Laboratory indicators: hypoglycemia, hyponatremia.

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

Interaction

Long-term use of omeprazole at a dose of 20 mg 1 time per day in combination with caffeine, theophylline, digoxin, amoxicillin, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, lidocaine, quinidine and estradiol did not lead to changes in their plasma concentrations.

There was no interaction with concomitantly taken antacids.

May reduce the absorption of ampicillin esters, iron salts, itraconazole and ketoconazole (
Omeprazole increases gastric pH). Being an inhibitor of cytochrome P450, it can increase the concentration and reduce the excretion of diazepam, indirect anticoagulants, phenytoin, nifedipine, warfarin and disulfiram, which in some cases may require a reduction in the doses of these drugs.

The effectiveness of prednisone and cyclosporine may be reduced, which in some cases may require a dose adjustment of cyclosporine.

When taken simultaneously, the absorption of omeprazole and clarithromycin is enhanced, which leads to an increase in their concentration in plasma.

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.

Treatment is symptomatic. There is no specific antidote. Hemodialysis is ineffective.

Storage conditions

In a dry place, at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after expiration date.

Manufacturer

KRKA-RUS, Russia