Ультоп®

General characteristics. Structure:

Active ingredient: 10 mg or 40 mg of an omeprazol.

Excipients: sugar        krupka (sucrose, starch syrup), hypro rod, magnesium hydroxycarbonate (magnesium carbonate, heavy), sucrose, starch corn, sodium lauryl sulfate, methacrylic acid of an etakrilat % copolymer (1:1) 30 dispersion, talc, macrogoal 6000, titanium dioxide; structure of the capsule: titanium dioxide (E171), dye ferrous oxide red (E172), gelatin.

The drug used at digestive tract diseases.

Pharmacological properties:

Pharmacodynamics. Inhibits      H+ K enzyme +  ATP-ase  ("the proton  pump")  in covering cells of a stomach and blocks thereby a final stage of synthesis of hydrochloric  acid.  It leads to decrease in level of basal and stimulated secretion, irrespective of the irritant nature. Omeprazol is pro-medicine and is activated in acid medium of secretory tubules of covering cells. After a single dose of drug inside action of an omeprazol comes within the first hour and continues within 24 hours, the maximum of effect is reached in 2 hours. After the termination of administration of drug secretory activity is completely recovered in 3-5 days. Basal gastric secretion decreases to 94% after reception of 40 mg of an omeprazol. Acidity of a gastric juice within 24 hours снижаетя for 80-97% at reception of 20 mg of an omeprazol and for 92-94% at reception of 40 mg. The inhibition of 50% of the maximum secretion proceeds 24 h. At patients with a peptic ulcer of a duodenum reception of 20 mg of an omeprazol supports intragastric рН - 3 within 17 hours.

Pharmacokinetics. Omeprazol is quickly absorbed from digestive tract, the maximum concentration in plasma is reached in 0,5-1 hour. Bioavailability makes 30-40%. Bioavailability increases at elderly patients and patients with an abnormal liver function a little, and substantially – at пациентовс a chronic liver failure (can reach – 100%). Communication with proteins of plasma - about 90-95%. Omeprazol is almost completely metabolized in a liver with education 6 pharmacological of inactive metabolites (гидроксиомепразол, sulphidic and sulfonic derivatives, etc.). Is inhibitor of the fermental CYP2C19 system. An elimination half-life - 0,5-1 hour. Removal by kidneys (70-80%) and with bile (20-30%). At renal failures removal of an omeprazol decreases in proportion to decrease in clearance of creatinine. At abnormal liver functions of T1/2 makes 2-3ch. The general clearance – 500-600 ml/min.

Indications to use:

Capsules kishechnorastvorimy 40 mg
- A peptic  ulcer  of a stomach  and    duodenum  (in  a phase of an aggravation  and antirecurrent treatment),  including  associated with  Helicobacter pylori ( as a part of a combination therapy);
- Gastroesophageal reflux disease (GERB), including reflux esophagitis and not erosive forms of a reflux disease (NERB);
- The erosive cankers of a stomach and   duodenum  connected with reception of non-steroidal anti-inflammatory drugs (NPVP), stressful ulcers;
- Zollingera-Ellison's syndrome and other morbid conditions connected with the increased gastric secretion.
Capsules kishechnorastvorimy 10 mg
- Short-term therapy of not ulcer dyspepsia which is shown by a stomach ache, nausea, heartburn, an eructation;
- A long maintenance therapy for the purpose of prevention of a recurrence of a gastroesophageal reflux disease (GERB) (prevention of a recurrence of heartburn)
- A long maintenance therapy for the purpose of prevention of a recurrence of an ulcer of a duodenum.

Route of administration and doses:

Inside, to food (since meal slows down drug absorption), washing down with a small amount of water (contents of the capsule cannot be chewed).

Peptic ulcer of a duodenum in an aggravation phase - on 20 mg a day within 2-4 weeks (in resistant cases to 40 mg a day).

Peptic ulcer of a stomach in a phase of an aggravation and an erosive and ulcer esophagitis - on 20-40 mg a day within 4-8 weeks.

Gastroesophageal reflux disease (GERB): patients with a moderate inflammation on 1 capsule on 20 mg once a day in the morning, before a breakfast within 4-8 weeks. For providing the below-mentioned mode of dosing, administration of drug in other registered dosage is possible (Ultop®, capsules kishechnorastvorimy 10 mg and 40 mg). Duration of a basic course of treatment makes 4-8 weeks. After healing of an erosive esophagitis the supporting treatment for 26-52 weeks is shown, at a heavy esophagitis – for life. In case of a recurrence of heavy GERB or resistant GERB of a disease treatment can be prolonged up to 4-8 weeks.

 Zollingera-Ellison's syndrome and other morbid conditions connected with the increased gastric secretion: the dose is selected individually  depending on the initial  level  of gastric secretion,  usually    since  60  mg a day.  If necessary the dose is increased to 80 - 120 mg a day, in this case it is divided into 2-3 receptions.

At patients with a heavy liver failure the daily dose should not exceed 20 mg.

Eradikation Helicobacterpylori-on 20 mg 2 times a day within 7 or 14 days (  depending on  the applied  scheme  of treatment) in combination with antibacterial agents.

Not ulcer dyspepsia: the dose is usual makes from 10 mg to 20 mg within 2-4 weeks once a day. If in 4 weeks of administration of drug the state does not improve, or dyspepsia symptoms appear again soon after the reception termination, it is necessary to revise the diagnosis.

Prevention of a recurrence of a peptic ulcer of a stomach and 12-perstny gut: on 10-20 mg a day.

Prevention of a recurrence of GERB: on 20 mg a day for a long time. Safety and efficiency of a 12-month maintenance therapy are proved. Use on demand is possible.

Renal failure. For patients with a renal failure dose adjustment is not required.

Abnormal liver function. At patients with an abnormal liver function bioavailability and clearance of an omeprazol increases. In this regard the therapeutic dose should not exceed 10-20 mg a day.

Advanced age. For patients of advanced age correction of the scheme of treatment is not required.

Features of use:

Before therapy it is necessary to exclude existence of malignant process (especially at stomach ulcer) since treatment, masking symptomatology, can delay statement of the correct diagnosis.

Meal slows down absorption of an omeprazol therefore the drug Ultop® is rkomendutsya to be accepted before food.

In special cases, at emergence of difficulties with a proglatyvaniye of the whole capsule, it is possible to swallow its contents after opening or a rassasyvaniye of the capsule, and also it is possible to mix capsule contents with slightly acidified liquid (juice, yogurt) and to use the received suspension within 30 min.

In usual dosages drug does not exert impact on the speed of psychomotor reactions and concentration of attention.

Safety of use of the drug Ultop® during pregnancy and during feeding by a breast is not studied therefore its use during pregnancy is not recommended; in need of use of the drug Ultop® in the period of a lactation, breastfeeding should be stopped.

In usual dosages drug does not exert impact on the speed of psychomotor reactions and concentration of attention.

Side effects:

In rare instances there can be following, usually reversible, side reactions:

From digestive organs: diarrhea or a lock, nausea, vomiting, a meteorism, an abdominal pain, a syndrome of the angry intestines, heartburn, dryness in a mouth, taste disturbances, stomatitis, pancreatitis (including fulminantny is possible), appetite loss, discoloration of fecal masses, gullet candidiasis, a language mucosal atrophy, tranzitorny increase in activity of "hepatic" enzymes and bilirubin in plasma; patients with the previous serious illness of a liver have a hepatitis (including with jaundice), an abnormal liver function and hepatic encephalopathy.

From a nervous system: headache, dizziness, aggression, apathy, nervousness, excitement, drowsiness, sleeplessness, tremor, вертиго, paresthesias, depression, hallucinations, confusion of consciousness; at patients with the serious accompanying somatopathies, patients with the previous serious illness of a liver - encephalopathy.

From cardiovascular system: stenocardia, tachycardia, bradycardia, feeling of heartbeat, increase in arterial pressure, vasculites, peripheral hypostases.

From urinogenital system: intersticial nephrite, infections of urinary tract, a microscopic pyuria, a proteinuria, a hamaturia, increase in concentration of creatinine in serum, a gynecomastia, pain in testicles.

From a musculoskeletal system: muscular weakness, mialgiya, arthralgia, ossalgiya (ostealgia), muscular spasms.

From system of a hemopoiesis: pancytopenia, agranulocytosis, anemia (including hemolitic anemia), neutropenia, thrombocytopenia, leukocytosis, leukopenia.

   From      integuments: petechias, skin itch, skin   rash;         in some cases - a photosensitization, a multiformny exudative erythema, a hair loss, an alopecia, a xeroderma, an epidermal toxic necrolysis, Stephens-Johnson's syndrome.

From a respiratory organs: pharyngalgia, cough, plentiful nasal bleeding.

From sense bodys: a ring in ears, not expressed vision disorder and hearing.

Allergic    reactions:    small tortoiseshell,    Quincke's    disease, bronchospasm, intersticial nephrite, acute anaphylaxis, fever.
Laboratory indicators: hypoglycemia, hyponatremia.

Others: a dorsodynia, sweating strengthening, it is rare - formation of gastric glandulyarny cysts during prolonged treatment (a consequence  of inhibition  of secretion  of hydrochloric  acid,  has high-quality, reversible character), the general weakness, increase in body weight.

Interaction with other medicines:

Prolonged use of an omeprazol in a dose of 20 mg of 1 times a day in a combination with caffeine, theophylline, piroxicam, diclofenac, Naproxenum, metoprololy, propranolol, ethanol,  cyclosporine,  lidocaine,  quinidine  and  oestradiol    did not lead  to change of their concentration in plasma.

Interaction with at the same time accepted antacids is noted.

Can  reduce  absorption  of ethers  of ampicillin,  salts  of iron,  an itrakonazol  and ketokonazol (омепразол raises рН a stomach). Being P450 cytochrome inhibitor, can  increase  concentration  and  reduce  removal  of diazepam,  anticoagulants of indirect action, Phenytoinum, nifedipine, warfarin and Disulfiramum that in certain cases can demand reduction of doses of these medicines.

Efficiency of Prednisonum and cyclosporine can be reduced that in certain cases can demand cyclosporine dose adjustment.

At a concomitant use absorption of an omeprazol and klaritromitsin amplifies that leads to increase in their concentration in a blood plasma.

Contraindications:

  Hypersensitivity  to  an omeprazol or other components of drug,  children's  age,  pregnancy,  the lactation period, hereditary intolerance of fructose, a syndrome of glyukozo-galaktozny malabsorption, deficit of sucrose/isomaltase.

With care - a renal and/or liver failure.

Overdose:

Patients well transfer daily doses to 360 mg.

Symptoms: an abdominal pain, drowsiness, a headache, dizziness, dryness in a mouth, tachycardia, arrhythmia, a sight illegibility, excitement, confusion of consciousness, increase in sweating, nausea; in rare instances: spasms, short wind. Hypothermia.

The specific antidote does not exist. Symptomatic treatment. The hemodialysis is insufficiently effective.

Storage conditions:

In the place protected from moisture, at a temperature not above 25ºС, in original packaging. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Capsules kishechnorastvorimy 10 mg and 40 mg.
By production on KRK, of, the place, Slovenia Is new:
On 7 capsules in the blister from the combined material PVH/PE/PVDH/PE/PVH and aluminum foil;

On 14 or 28 capsules place in a polyethylene case with the polypropylene screwing-up cover with control of the first opening and the capsule of a hydrosorbent. With 28 capsules on 40 mg place the additional capsule of a hydrosorbent in a polyethylene case.

On 2 or 4 blisters place in a cardboard pack together with the instruction on
to use.

1 case is placed in a pack cardboard together with the application instruction.

By production on LLC KRKA-RUS: On 7 capsules in a blister strip packaging (blister) from the combined material PVH/PE/PVDH/PE/PVH and aluminum foil.

2 or 4 blister strip packagings (blister) together with the application instruction place in a pack from a cardboard.