Losek

General characteristics. Structure:

Active ingredient: омепразол sodium of 42.6 mg, 40 mg of an omeprazol are equivalent.
Auxiliary ingredients: disodium salt of ethylene diamine tetraacetic acid (EDTA) of 1.5 mg, sodium hydroxide of 0.1-1.2 mg for finishing рН, nitrogen, water for injections to 2.0 ml
Description
Lyophilisate of color, white or white with a shade, in the form of the pressed weight or powder in bottles on 10 ml.

Pharmacological properties:

Pharmacodynamics. Omeprazol is racemic mix of two enantiomer, reduces secretion of acid at the expense of specific inhibition of an acid pomp of covering cells. At single appointment drug quickly works and renders reversible oppression of secretion of acid.
Action mechanism
Omeprazol is the weak basis, concentrates and converted into an active form in acid medium of tubules of cells of a pristenochny layer of a mucous membrane of a stomach where it is activated and inhibits H+,K+ - Atfazy-kislotnoy a pomp. Drug has dozozavisimy effect on the last stage of synthesis of acid, oppresses both basal, and stimulated secretion irrespective of the stimulating factor.
Influence on gastric secretion
Intravenous administration of an omeprazol renders dozozavisimy oppression of secretion of hydrochloric acid at people. To reach bystry decrease in intragastric acidity, intravenous administration of 40 mg of an omeprazol after which there is a bystry decrease in intragastric secretion which is supported within 24 hours is recommended.
Extent of oppression of secretion of acid is proportional to the area under a curve (concentration time of AUC) of an omeprazol and is not proportional to the valid concentration of drug in blood of time at present.
During treatment omeprazoly the tachyphylaxis was not noted.
Decrease in secretion of acid in a stomach under the influence of inhibitors of the proton pump or other kisloto-inhibiting agents leads to increase in growth of normal intestinal microflora that in turn can lead to small increase in risk of development of the intestinal infections caused by such bacteria as Salmonella and Campylobacter.

Pharmacokinetics. Distribution
Distribution volume at healthy subjects makes 0.3 l/kg, the similar indicator decides at patients on a renal failure. At patients of advanced age and at patients with a liver failure the volume of distribution is a little reduced. The indicator of a svyazyvayemost of an omeprazol with proteins of plasma makes about 95%.
Metabolism and excretion
After intravenous administration the average value of semi-removal in a terminal phase makes 40 minutes; the general clearance makes from 0.3 to 0.6 l/min. During treatment change of duration of an elimination half-life is not noted.
Omeprazol is completely metabolized by P450 (CYP) cytochrome in a liver. Drug metabolism generally depends on a specific isoenzyme of CYP2C19 (S-mefiniton a hydroxylase) which is responsible for formation of the main metabolite of a gidroksiomeprazol.
Metabolites do not exert impact on gastric secretion of acid. About 80% of intravenously entered dose are removed in the form of metabolites with urine, and other part - with excrements.
At patients with the lowered function of kidneys excretion of an omeprazol does not undergo any changes. Increase in an elimination half-life at patients with the broken function of a liver is noted, however, accumulation of an omeprazol does not happen.

Indications to use:

Duodenum ulcer, stomach ulcer, reflux esophagitis, treatment of a syndrome
Zollingera-Ellisona.

Route of administration and doses:

At impossibility of performing peroral therapy to patients with stomach ulcer and a duodenum or a reflux esophagitis Losek in a dose of 40 mg is recommended to appoint drug infusion once a day. To patients with Zollingera-Ellison's syndrome
initial intravenous administration of Losek in a dose of 60 mg a day is recommended. Doses are selected individually, introduction of higher dose sometimes is required. If the size of a daily dose exceeds 60 mg, then the dose has to be divided into two receptions. Infusional Losek is entered intravenously within 20-30 minutes.
It is recommended to enter solution for infusions at once after its preparation.
Patients with an impaired renal function
Patients with an impaired renal function have no need to carry out dose adjustment.
Patients with the broken function of a liver
For patients with the broken function of a liver the daily dose of 10-20 mg a day can be sufficient as at these patients the elimination half-life of an omeprazol is increased.
Patients of advanced age
There is no need to carry out correction of a dose at patients of advanced age.
Children
There is a limited experience of use of Losek for children.
Instruction for preparation of infusion solution
Infusion solution prepares by dissolution of the lyophilized powder of an omeprazol in 100 ml of 5% of infusion solution of a dextrose or in 100 ml of infusion normal saline solution.
Infusion solution for 5% to a dextrose has to be used within 6 hours. Infusion solution on normal saline solution has to be used within 12 hours.
Preparation
1. To gain the syringe 5 ml of infusion solution from a bottle or an infusional bag.
2. To enter infusion solution into a bottle with the lyophilized powder of an omeprazol, to stir up a bottle before full dissolution of drug.
3. To gather solution of an omeprazol in the syringe.
4. To transfer solution of an omeprazol to a bottle or an infusional bag.
5. To repeat operations 1-4 to transfer all drug from a bottle.
Alternative preparation of infusion solution in a soft container
1. For preparation of solution to use a bilateral needle (-an adapter). To puncture with one end of a needle a membrane of an infusional bag, to connect other end of a needle to a bottle of the lyophilized omeprazol.
2. To dissolve powder of an omeprazol, pumping over infusion solution from a bag in a bottle and back.
3. To be convinced that powder was completely dissolved then to disconnect an empty bottle and to remove a needle from an infusional bag.

Features of use:

At suspicion of stomach ulcer at early stages it is necessary to undergo x-ray or endoscopic inspection for installation of the correct diagnosis and purpose of adequate treatment.
In the presence of any alarming symptoms (for example, such as considerable spontaneous loss of body weight, frequent vomiting, a dysphagy, vomiting with blood or a melena), and also in the presence of stomach ulcer (or at suspicion of stomach ulcer) it is necessary to exclude a possibility of a malignant new growth as treatment by Losek can lead to smoothing of symptomatology and delay diagnosis.
Incompatibility
It is not noted if to follow the instruction in the section "Route of Administration and Doses".

Side effects:

Drug Losek in general is well transferred. It was reported about the following side effects, however, in most cases the valid communication between effects and treatment was not established.
Integuments
Skin rashes and/or skin itch.
In some cases photosensitivity reaction, multiformny erythema, alopecia.
Musculoskeletal system
In rare instances arthralgia, muscular weakness, mialgiya.
Central and peripheral nervous system
Headache, hyponatremia.
Dizziness, paresthesia, drowsiness, sleeplessness. In rare instances at patients with serious associated diseases the depression, excitement, aggression and hallucinations can be noted.
Gastrointestinal system
Diarrhea, lock, abdominal pains, nausea/vomiting, meteorism. In some cases dryness in a mouth, stomatitis, gastrointestinal candidiasis.
System of a liver
In rare instances increase in activity of liver enzymes. In extremely exceptional cases at patients with a serious illness of a liver (hepatitis with/without jaundice, a liver failure) encephalopathy can develop.
Endocrine system
In extremely exceptional cases gynecomastia
Circulatory system
In rare instances leukopenia, thrombocytopenia, agranulocytosis and pancytopenia.
Others
Febricula.
Reaction of hypersensitivity in the form of a small tortoiseshell (seldom), in some cases a Quincke's disease, fever, a bronchospasm, intersticial nephrite, an acute anaphylaxis.
In some cases the increased sweating, peripheral hypostasis, a vision disorder, changes of flavoring feelings can be noted.
There were messages on Stephens-Johnson's syndrome and a toxic epidermal necrolysis, connection with administration of drug is not established.
Patients had messages on irreversible dysfunction of sight with serious associated diseases against the background of intravenous injections of an omeprazol in high doses. However, the causal relationship between deterioration in function of sight and treatment omeprazoly was not established.

Interaction with other medicines:

It is necessary to avoid combined use of Losek of lyophilisate for preparation of solution for intravenous infusions with ketokonazoly and itrakonazoly.
Absorption of some drugs can change in connection with impact of an omeprazol on acidity of the gastric environment.
So, dissolution of tablets of a ketokonazol decreases at increase gastric рН
owing to use of the drugs inhibiting acid secretion (antiacid agents, сукральфат) that in turn leads to decrease in concentration of a ketokonozol in plasma. At combined use of an omeprazol and itrakonazol concentration in plasma and the area under a curve "concentration time" of an itrakonazol decreases approximately to 65% probably owing to lower absorption which depends from рН.
Omeprazol inhibits CYP2C19 in this connection combined use of an omeprazol with drugs in which metabolism CYP2C19, such as diazepam, warfarin, Phenytoinum takes part can lead to increase in concentration of these drugs in plasma and demand a dose decline.
At joint reception of a klaritromitsin or erythromycin and an omeprazol concentration of an omeprazol in plasma increases. Joint reception with amoxicillin or metronidazole does not influence concentration of an omeprazol in plasma.
Influence of medicines on pharmacokinetics of an omeprazol
The drugs inhibiting CYP2C19 or CYP3A enzymes (protease HIV inhibitors, кетоконазол, итраконазол), can increase concentration of an omeprazol in plasma.
Influence of an omeprazol on the following drugs is not revealed: antacids, theophylline, caffeine, quinidine, lidocaine, propranolol or ethanol.

Contraindications:

Hypersensitivity to an omeprazol.
Pregnancy and lactation
Pregnancy
Results of epidemiological researches showed lack of side effect
omeprozola on pregnancy course, on a fruit or on the newborn.
Losek can be applied during pregnancy.
Lactation
Omeprazol is allocated with breast milk. Influence on children if that is available, is not known.

Overdose:

In clinical trials intravenous administration of drug within one day to 270 mg and to 650 mg during the three-day period without any effects for the patient was carried out.
Influence on ability to manage transport and work with mechanisms
Losek does not influence ability to manage transport and work with mechanisms.

Storage conditions:

In the place protected from light at a temperature below 25 °C. To store bottles in packaging.
Bottle (a bottle without cardboard box): to store in the place protected from light, at room lighting to store no more than 24 hours.
The prepared solution: infusion has to be carried out within 12 hours if normal saline solution and within 6 hours was used if solution of 5% of a dextrose was used.
Special precautions at storage
Powder for infusion has to be dissolved in 100 ml of infusion normal saline solution or in 100 ml of 5% of infusion solution of a dextrose. Infusion has to be carried out within 12 hours if normal saline solution was used, within 6 hours if solution of 5% of a dextrose was used.
Solutions prepare at room lighting without special precautions.
Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 40 mg of active agent of an omeprazol in a glass bottle. A glass bottle with a rubber bung and an aluminum blooming ring and a plastic lid. 5 bottles in a plastic planimetric cell are placed in a cardboard box with the application instruction.