Ultop capsules 40 mg № 28

PHARMACEUTICAL FORM

Capsules 10 mg: two-color capsules - light pink capsule body and cap
white color.
Capsules 40 mg: two-color capsules - brown-pink capsule body and cap
light pink color.
Capsules 10mg and 40mg contain white to white pellets with a slightly yellowish
shade or pinkish tint color.

CLINICAL DATA

Therapeutic indications

 40 mg Enteric Capsules
- Peptic ulcer of the stomach and duodenum (in the acute phase and anti-relapse treatment), including 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 taking nonsteroidal anti-inflammatory drugs (NSAIDs), stressful ulcers;
- Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.
10 mg Enteric Capsules
- Short-term treatment of non-ulcer dyspepsia, which is manifested by pain in the stomach, nausea, heartburn, belching;
- Long-term maintenance therapy to prevent the recurrence of gastroesophageal reflux disease (GERD) (prevention of heartburn recurrence)
- Long-term maintenance therapy to prevent recurrence of duodenal ulcer.

Dosage and administration

Inside, before eating (becausefood intake slows down the absorption of the drug), drinking a small amount of water (the contents of the capsule can not be chewed).
Duodenal ulcer in acute phase - on 20 mg a day in
for 2-4 weeks (in resistant cases up to 40 mg per day).
Peptic ulcer in the acute phase and erosive-ulcerative esophagitis - 20-40 mg in
day for 4-8 weeks.
Gastroesophageal Reflux Disease (GERD): patients with moderate inflammation in 1 capsule 20 mg once a day in the morning, before breakfast for 4-8 weeks. To ensure the following dosing regimen, it is possible to take the drug in another registered dosage (Ultop®, enteric 10 mg and 40 mg capsules). The duration of the main course of treatment is 4-8 weeks. After healing of erosive esophagitis, supportive treatment is indicated for 26-52 weeks, with severe esophagitis - for life. In the case of relapsed severe GERD or resistant GERD, treatment can be extended to 4–8 weeks.
Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion: The dose is adjusted individually depending on the initial level of gastric secretion, usually starting at 60 mg per day. If necessary, increase the dose to 80 -120 mg per day, in this case, it is divided into 2-3 doses.
In patients with severe hepatic impairment, the daily dose should not exceed
20 mg.
Eradication of Helicobacterpylori- 20 mg 2 times a day for 7 or 14 days (depending on the treatment regimen used) in combination with antibacterial agents.
Nonulcer dyspepsia: The usual dose is from 10 mg to 20 mg once a day for 2-4 weeks. If after 4 weeks of taking the drug, the condition does not improve, or the symptoms of dyspepsia reappear soon after stopping, you should reconsider the diagnosis.
Prevention of recurrence of gastric ulcer and 12 duodenal ulcer: on 10-20 mg in
day.
Prevention of relapsed GERD: 20 mg per day for a long time. Proven safety and efficacy of 12-month maintenance therapy. Possible use on demand.
Renal dysfunction
For patients with impaired renal function dose adjustment is not required
Liver dysfunction
In patients with impaired liver function, bioavailability and clearance of Omeprazole increases. In this regard, the therapeutic dose should not exceed 10-20 mg per day.
Elderly age
For elderly patients, correction of the treatment regimen is not required.

Contraindications

Hypersensitivity to omeprazole or other components of the drug, childhood, pregnancy, lactation, hereditary fructose intolerance, glucose-galactose malabsorption syndrome, sucrose / isomaltase deficiency
With care - renal and / or liver failure.

Special instructions and precautionary measures

 Before starting therapy, it is necessary to exclude the presence of a malignant process (especially in case of a stomach ulcer), since treatment, masking the symptoms, may delay the correct diagnosis.
Eating slows down the absorption of omeprazole, so the drug Ultop® is recommended to be taken before meals.
In special cases, if you have difficulty in swallowing a whole capsule, you can swallow its contents after opening or resorbing the capsule, and you can mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.
In normal dosages, the drug does not affect the speed of psychomotor reactions and concentration.

Interaction with other drugs

Prolonged use of omeprazole in a dose of 20 mg 1 time per 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 interactions with concomitant antacids were observed.
May reduce the absorption of ampicillin esters, iron salts, itraconazole and Ketoconazole (omeprazole increases the pH of the stomach). As 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 doses of these drugs.
The effectiveness of prednisone and cyclosporine can be reduced, which in some cases may require a dose adjustment of cyclosporine.
With the simultaneous reception increases the absorption of omeprazole and Clarithromycin, which leads to an increase in their concentration in the blood plasma.

Pregnancy and breastfeeding

The safety of the drug Ultop® during pregnancy and lactation has not been studied, so its use during pregnancy is not recommended; if necessary, the use of the drug Ultop® during lactation, breastfeeding should be discontinued.

Influence on ability to drive a car and other mechanisms

 In normal dosages, the drug does not affect the speed of psychomotor reactions and concentration.

Side effects

In rare cases, the following, usually reversible, side reactions may occur:
On the part of the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, irritable bowel syndrome, heartburn, dry mouth, taste disorders, stomatitis, pancreatitis (including fulminant), loss of appetite, discoloration of feces, 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 previous severe liver disease, hepatitis (including jaundice), impaired liver function, and hepatic encephalopathy.
Nervous system disorders: headache, dizziness, aggressiveness, apathy, nervousness, agitation, drowsiness, insomnia, tremor, vertigo, paresthesia, depression, hallucinations, confusion; in patients with severe concomitant somatic diseases, patients with previous severe liver disease
- encephalopathy.
Since the cardiovascular system: angina, tachycardia, bradycardia, sensation of heartbeat, increased blood pressure, vasculitis, peripheral edema.
On the part of the urogenital system: interstitial nephritis, urinary tract infections, microscopic pyuria, proteinuria, hematuria, increased serum creatinine concentration, gynecomastia, pain in the testicles
On the part of the musculoskeletal system: muscle weakness, myalgia, arthralgia, ossalgia (pain in the bones), muscle cramps.
On the part of the hematopoietic system: pancytopenia, agranulocytosis, anemia (including hemolytic anemia), neutropenia, thrombocytopenia, leukocytosis, leukopenia.
On the part of the skin: petechiae, pruritus, skin rash; in some cases - photosensitization, erythema multiforme exudative, hair loss, alopecia, dry skin, epidermal toxic necrolysis, Stevens-Johnson syndrome.
On the part of the respiratory system: sore throat, cough, profuse nasal bleeding.
On the part of the senses: tinnitus, unexpressed vision 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 prolonged treatment
(a consequence of the inhibition of the secretion of hydrochloric acid, is benign, reversible), general weakness, increased body weight.

Overdose

Patients tolerate daily doses up to 360 mg.
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. Symptomatic treatment. Hemodialysis is not effective enough.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics

Pharmacotherapeutic group: antiulcer agent - proton pump inhibitor.

Pharmacological properties.

Inhibits the enzyme H + K + ATP-azu ("proton pump") in the parietal cells of the stomach and thereby blocks the final stage of the synthesis of hydrochloric acid. This leads to a decrease in basal and stimulated secretion, regardless of the nature of the stimulus. Omeprazole is a prodrug and is activated in the acidic environment of the secretory tubules of the parietal cells.After a single dose of the drug inside omeprazole occurs within the first hour and lasts for 24 hours, the maximum effect is achieved after 2 hours. After stopping the drug, secretory activity is fully restored in 3-5 days. Basal gastric secretion is reduced to 94% after taking 40 mg of omeprazole. The acidity of gastric juice within 24 hours reduces by 80-97% when taking 20 mg of omeprazole and 92-94% when taking 40 mg. Inhibition of 50% of the maximum secretion lasts 24 hours. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains intragastric pH - 3 for 17 hours.

Pharmacokinetics

Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration in plasma is reached in 0.5-1 hour. Bioavailability is 30-40%. Bioavailability is slightly increased in elderly patients and patients with impaired liver function, and to a significant degree in patients with chronic liver failure (can reach - 100%). Communication with plasma proteins is about 90-95%. Omeprazole is almost completely metabolized in the liver to form 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.). It is an inhibitor of the CYP2C19 enzyme system. The half-life is 0.5-1 hours. Excretion by the kidneys (70-80%) and with bile (20-30%). With impaired renal function, the elimination of omeprazole decreases in proportion to the decrease in creatinine clearance. When abnormal liver function T1 / 2 is 2-3h. Total clearance - 500-600 ml / min.

List of excipients

Excipients: sugar pellets (sucrose, starch syrup), hyprolose, Magnesium hydroxycarbonate (magnesium carbonate, heavy), sucrose, corn starch, sodium lauryl sulfate, methacrylic acid ethacrylate copolymer (1: 1) 30% dispersion, talc, macrogol 6000, titanium dioxide; the composition of the capsule: titanium dioxide (E171), iron dye red oxide (E172), gelatin.

Special storage conditions

In the place protected from moisture, at a temperature not above 25ºС, in original packaging. Keep out of the reach of children