Losek

Losek – antiulcerous medicine.

Form of release and structure

Dosage form of drug – lyophilisate for preparation of solution for infusions (on 40 mg in 1 bottle, in a cardboard pack of 5 bottles).

Contain in 1 bottle:

• Active ingredient: омепразол sodium – 42,6 mg (corresponds to the maintenance of an omeprazol – 40 mg);
• Auxiliary components: sodium ethylene diamine tetraacetate, sodium hydroxide (for correction рН).

Indications to use

Drug is shown for intravenous administration as replacement of peroral dosage forms of an omeprazol at therapy of the following diseases:

• Gastrinoma (Zollingera-Ellison's syndrome);
• Peptic ulcer of a stomach;
• Peptic ulcer of a duodenum;
• Reflux esophagitis.

Contraindications

• Combined use with nelfinaviry and atazanaviry;
• Children's age (experience of use is limited);
• Hypersensitivity to benzimidazole derivatives, an omeprazol or to other components of lyophilisate.

As a result of a number of researches lack of side effects of an omeprazol on pregnancy therefore drug is allowed for use during this period is revealed.

At a lactation for the period of therapy breastfeeding needs to be stopped as омепразол gets into breast milk, and its influence on children is not studied.

Route of administration and dosage

Lyophilisate solution right after preparation should be entered intravenously, in the form of infusion, for 20-30 minutes.

Doses are selected the attending physician individually. If a required daily dose more than 60 mg, then it is necessary to divide it into two introductions.

It is recommended (if oral administration of an omeprazol is impossible) at a peptic ulcer of a stomach and duodenum or a reflux esophagitis infusional introduction of Losek in a dose of 40 mg of 1 times a day. At Zollingera-Ellison's syndrome the initial dose makes 60 mg of 1 times a day.

Patients with abnormal liver functions can reduce a daily dose to 10-20 mg, it has to be enough as they increased _T1/2 – an elimination half-life of an omeprazol.

At renal failures and the patient of advanced age dose adjustment is not required.

For cultivation of 1 bottle of lyophilisate Losek 5% infusion solution of a dextrose or infusional 0,9% chloride sodium solution of 100 ml are used.

Solutions prepare without special precautions at room lighting as follows:

1. In the prepared syringe to gain 5 ml of infusion solution from an infusional bag or a bottle;
2. To enter infusion solution into a bottle with lyophilisate Losek, to stir up a bottle before full dissolution of powder;
3. To gather the dissolved lyophilisate in the syringe;
4. To transfer solution of an omeprazol to an infusional bag or to a bottle;
5. To repeat actions with 1 on 4 to transfer all drug from a bottle.

Other way of preparation of infusion solution using a soft container:

1. To use a bilateral needle adapter, having punctured with one of its end a membrane of an infusional bag, having connected other end to a lyophilisate bottle;
2. Pumping over infusion solution from a bag in a bottle and to back dissolve the lyophilized powder;
3. After full dissolution of powder to disconnect an empty bottle and to take out a needle from an infusional bag.

Side effects

The side effects noted during clinical trials and at post-marketing studying of use of lyophilisate Losek, which are not depending on the mode of its dosing:

• Gepatobiliarny system: infrequently – increase in activity of liver enzymes; seldom – hepatic encephalopathy at patients with liver diseases, hepatitis with jaundice or without it;
• Digestive Tract (DT): often – nausea, vomiting, diarrhea, a meteorism, a lock, abdominal pain; seldom – gastrointestinal candidiasis, dryness in a mouth, stomatitis;
• Immune system: seldom – hypersensitivity reactions, such as an angioedema, fever, an anaphylaxis;
• Skin and hypodermic cellulose: infrequently – urticaria, dermatitis, skin rash, a skin itch; seldom – photosensitivity reactions, an alopecia, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a multiformny erythema;
• Hemopoietic system: seldom – a leukopenia, an agranulocytosis, thrombocytopenia, a pancytopenia;
• Urinary system: seldom – intersticial nephrite;
• Nervous system (central and peripheral): often – a headache; infrequently – paresthesias, dizziness, drowsiness, sleeplessness; seldom – aggression, hypererethism, a depression, hallucinations, consciousness disturbance, taste disturbance;
• Musculoskeletal system: seldom – a mialgiya, an arthralgia, muscular weakness;
• Respiratory organs: seldom – a bronchospasm;
• Reproductive organs: seldom – a gynecomastia;
• Another: infrequently – a febricula, вертиго; seldom – a sight illegibility, a hyponatremia, peripheral hypostases, the increased sweating; very seldom – a hypomagnesiemia.

Patients have data on an irreversible vision disorder with the heavy accompanying pathologies against the background of injections of an omeprazol in high doses, but to a reliable causal relationship between therapy omeprazoly and deterioration in sight was not established.

By results of clinical trials it was established that intravenous infusional administration of drug in a daily dose to 270 mg, and also to 650 mg within three days for the patient took place without any significant effects.

Can be symptoms of overdose: block, confusion of consciousness, dizziness, headache, tachycardia, dilatation of vessels, nausea, vomiting, diarrhea, meteorism. It is in that case recommended to carry out symptomatic therapy, considering insufficient efficiency of a hemodialysis.

Special instructions

In the presence of suspicions of stomach ulcer it is necessary to undergo endoscopic or x-ray inspection at early stages for establishment of the right diagnosis and purpose of adequate therapy.

It is required to exclude a possibility of malignant new growths at any alarming symptoms (a dysphagy, frequent vomiting, a melena or vomiting with blood, essential spontaneous loss of weight), and also at stomach ulcer or in case of suspicion of stomach ulcer as therapy omeprazoly can lead to weakening of symptomatology and postpone diagnosis.

It is important to consider that inhibitors of the proton pump can increase risk of development of one of the most frequent nozokomialny infections caused by Clostridium difficile microorganism at hospital patients.

Omeprazol does not influence concentration of attention and speed of psychomotor reactions, but during therapy drowsiness and dizziness therefore it is recommended to be careful at control of motor transport or work with other difficult mechanisms can be observed.

Medicinal interaction

Influence of an omeprazol on at the same time applied medicinal substances / drugs:

• Klopidogrel – can decrease his protivotrombotichesky action (the interaction mechanism is completely not studied for today therefore it is recommended to be careful at combined use);
• Ketokonazol or итраконазол – decrease in their absorption is possible;
• Digoxin – increase in its absorption; at combined use of an omeprazol in a daily dose of 20 mg and digoxin bioavailability of the last increases by 10% (at 20% of patients – to 30%);
• Nelfinavir and атазанавир – is marked out decrease in their concentration in serum (combined use with omeprazoly is not recommended);
• Sakvinavir – raises its concentration in serum;
• Diazepam, warfarin, Phenytoinum, other antagonists of vitamin K and цилостазол – decrease in their metabolism is possible (Phenytoinum – is necessary control of its concentration in plasma; warfarin, other antagonists of vitamin K – is required monitoring of an index of the international normalized relation (MHO));
• Lidocaine, quinidine, cyclosporine, erythromycin, oestradiol and будесонид – омепразол does not influence their metabolism;
• Theophylline, caffeine, quinidine, diclofenac, piroxicam, Naproxenum, propranolol, метопролол, ethanol – influence of an omeprazol is not revealed;
• Takrolimus – raises its concentration in blood serum.

Influence of substances/drugs on pharmacokinetics of an omeprazol:

• Vorikonazol and кларитромицин – because of decrease in metabolism of an omeprazol increase in its concentration in a blood plasma (taking into account good tolerance of high doses of an omeprazol of their correction it is not required in case of short combined use) is possible;
• Drugs of the St. John's Wort which is made a hole rifampicin – due to acceleration of metabolism of an omeprazol can reduce its concentration in a blood plasma.

Terms and storage conditions

To store in original packaging, in the protected from light, dry place, at a temperature not above 25 °C. To protect from children.

Period of validity:

• For 5% to a dextrose – to use infusion solution within 6 hours;
• For 0,9% chloride sodium solution – to use infusion solution within 12 hours;
• Bottle unpacked (at room lighting, in the place protected from light) – no more than 24 hours;
• Bottle in original packaging – 2 years.