Ortanol

Ortanol – ^{H+-K inhibitor +-ATF-azy}, antiulcerous means.

Form of release and structure

• Capsules size No. 3: firm, with the case and kryshechny light pinkish-brown color on which there is a text "OHM 10" black color; contents – granules of light yellow color (on 7 pieces in blisters, 1, 2 or 4 blisters in packaging);
• Capsules size No. 2: firm, with the case and a lid of white color on which there is a text of "OME 20" of black color; contents – granules of light yellow color (on 7 pieces in blisters, 1, 2 or 4 blisters in packaging);
• Capsules size No. 1: firm, with the case of light pinkish-brown color and a white lid on which there is a text of "OME 40" of black color; contents – granules of light yellow color (on 7 pieces in blisters, 1, 2 or 4 blisters in packaging);
• Lyophilisate for preparation of solution for infusions: powder or mass of almost white or white color (on 40 mg in transparent glass bottles, in a pack of cardboard 1, 5 or 10 bottles).

Active agent – омепразол:

• 1 capsule – 10 mg (size No. 3), 20 mg (size No. 2) or 40 mg (size No. 1);
• 1 bottle of lyophilisate – 40 mg.

Auxiliary components of capsules: lactose anhydrous, cellulose microcrystallic, the croscarmellose sodium, a hypro rod low-replaced povidone, gipromelloza phthalate, polysorbate 80, talc, дибутилсебакат.

Structure of a capsular cover:

• Capsules of 10 mg: gipromelloza, каррагинан, potassium chloride, titanium dioxide, water, gland (III) oxide yellow and oxide red; ink for drawing a text – shellac, propylene glycol, isopropanol anhydrous, ethanol anhydrous, ammonium hydroxide, potassium hydroxide, the water purified gland (III) oxide black (E172);
• Capsules of 20 mg: titanium dioxide, каррагинан, gipromelloza, water, potassium chloride; ink for drawing a text – ammonium hydroxide, ethanol anhydrous, butanol, isopropanol anhydrous, shellac, potassium hydroxide, propylene glycol, the water purified gland (III) oxide black (E172);
• Capsules of 40 mg: potassium chloride, каррагинан, titanium dioxide, gipromelloza, water, gland (III) oxide red and oxide yellow; ink for drawing a text – ammonium hydroxide, butanol, potassium hydroxide, ethanol anhydrous, propylene glycol, shellac, isopropanol anhydrous, the water purified gland (III) oxide black (E172).

Auxiliary components of lyophilisate: dinatrium of an edetat dihydrate, sodium hydroxide.

Indications to use

• Peptic ulcer of a stomach and 12-perstny gut (including prevention of a recurrence);
• Hyper secretory states (stressful ulcers of digestive tract, Zollingera-Ellison's syndrome, system mastocytosis, polyendocrine adenomatosis);
• Reflux esophagitis;
• Gastroesophageal reflux (symptomatic treatment);
• Eradikation Helicobacter pylori at the infected patients with a peptic ulcer of a stomach and a 12-tiperstny gut (as one of components of a combination therapy);
• Treatment and the prevention of injuries of a mucous membrane of a stomach and 12-perstny gut (dyspepsia, a round ulcer, an erosion of a mucous membrane) owing to reception of non-steroidal anti-inflammatory drugs (NPVS).

Contraindications

Absolute:

• Age up to 18 years;
• Feeding by a breast;
• Simultaneous use of an atazanavir, erlotinib, nelfinavir, pozakonazol;
• Hypersensitivity to any component which is a part of drug or the replaced benzimidazoles.

With care:

• Renal/liver failure;
• Osteoporosis;
• Existence of "alarming symptoms": the repeating vomiting, vomiting blood, discoloration a calla (melena), swallowing disturbances, considerable decrease in body weight, deficit _{of B12 vitamin};
• Pregnancy period;
• Simultaneous use of drugs of the St. John's Wort which is made a hole, rifampicin, a vorikonazol, a klaritromitsin, diazepam, warfarin, a klopidogrel, a sakvinavir, a tsilostazol, an itrakonazol, a takrolimus, Phenytoinum.

Route of administration and dosage

Capsules
Drug is accepted inside before food, at single use – it is desirable before a breakfast: swallow of capsules entirely and wash down with enough water.

Patients who experience difficulties with a proglatyvaniye can dissolve capsules in a small amount of fruit juice (for example, orange or apple) or waters.

The recommended dosing modes depending on indications:

• Peptic ulcer of a 12-perstny gut: on 20 mg of 1 times a day a course 2 weeks. If full scarring after the end of therapy is not noted, conduct one more 2 weeks course;
• Peptic ulcer of a 12-perstny gut, resistant to therapy: on 40 mg of 1 times a day within 2-4 weeks;
• Peptic ulcer of a stomach: on 20 mg of 1 times a day for 4 weeks. If full scarring after the end of therapy is not noted, conduct one more 4 weeks course;
• Peptic ulcer of a stomach, resistant to therapy: on 40 mg of 1 times a day within 4-8 weeks;
• Hyper secretory states: the dose is selected individually, the recommended initial dose – 60 mg of 1 times a day, maximum daily – 120 mg. If the dose exceeds 80 mg a day, it should be divided into several receptions;
• Eradikation Helicobacter pylori (in a combination with antibacterial agents): on 20 mg 2 times a day within 2 weeks;
• Reflux esophagitis: on 20 mg of 1 times a day a 4 weeks course. If full treatment after the end of therapy does not come, conduct a repeated 4 weeks course. At severe forms of a disease duration of treatment can be prolonged up to 8 weeks;
• Injuries of a mucous membrane of digestive tract owing to reception of NPVS: prevention – on 20 mg of 1 times a day during all course of use of NPVS, treatment – on 20 mg of 1 times a day within 4-8 weeks.

To patients with renal failures to adjust a dose there is no need. Patients with a serious illness of a liver and to elderly people should not exceed a dose of 20 mg a day.

Lyophilisate for preparation of solution for infusions
The drug is administered intravenously kapelno within 20-30 minutes.

In this dosage form Ortanol appoint at impossibility of performing peroral therapy.

To patients about a reflux esophagitis, a peptic ulcer of a stomach and a 12-perstny gut appoint 40 mg of 1 times a day.

For patients with Zollingera-Ellison's syndrome the recommended dose makes 60 mg of 1 times a day. In need of it increase up to 80-120 mg a day, but in this case divide into 2 introductions.

At an abnormal liver function the maximum daily dose makes 20 mg.

Rules of preparation of solution for injections (1 bottle with lyophilisate requires 100 ml of solution of glucose of 5% or sodium of chloride of 0,9%):

• From a bottle with solvent or an infusional bag to gain 5 ml of solution in the syringe;
• To enter solvent into a bottle with lyophilisate Ortanol and to mix carefully before full dissolution of powder;
• To gather solution of an omeprazol in the syringe and to transfer it to an infusional bag or a bottle with solvent;
• To repeat the first three actions until all is transferred омепразол.

Alternative way of preparation of solutions for infusions in soft containers with use of a bilateral needle adapter:

• To enter one end of a needle into a bottle with lyophilisate, and to attach the second to an infusional bag with solution for infusions;
• To dissolve lyophilisate, pumping over infusion solution between a bag and a bottle;
• To be convinced that powder was completely dissolved then to disconnect an empty bottle and to remove a needle from a bag.

The received solution cannot be reused. Its physical and chemical stability remains within 4 hours at storage in the dark place at a temperature up to 25 ºС.

From the microbiological point of view divorced solution should be used immediately.

Side effects

• From system of a hemopoiesis: in individual cases – thrombocytopenia, an agranulocytosis, a pancytopenia, a leukopenia;

• From a nervous system: in the presence of the accompanying heavy somatopathies – a headache; seldom – вертиго, sleeplessness, drowsiness, disturbance of flavoring feelings, paresthesias; very seldom – reversible confusion of consciousness, excitement, a depression; patients with a serious illness of a liver have an encephalopathy;
• From the alimentary system: seldom – a meteorism, a diarrhea/lock, an abdominal pain, nausea and/or vomiting; very seldom – increase in activity of hepatic transaminases and an alkaline phosphatase, stomatitis, dryness in a mouth; after the postponed serious illness of a liver – an abnormal liver function, hepatitis; at prolonged treatment – formation of reversible benign gastric glandulyarny cysts;
• From a musculoskeletal system: arthralgia, mialgiya; in individual cases – muscular weakness;
• From integuments: sweating strengthening, photosensitization, alopecia, mnogoformny exudative erythema;
• Allergic reactions: seldom – a skin itch, a small tortoiseshell; very seldom – fever, intersticial nephrite, an eosinophilia, anaphylactoid reactions, a bronchospasm, a Quincke's disease;
• Others: vision disorder, peripheral hypostases, gynecomastia.

The side effects arising owing to Ortanol's reception are usually expressed poorly and have passing character.

Special instructions

Before purpose of drug the patient has to undergo inspection to exclude existence of malignant process as омепразол can mask symptoms and by that to delay timely diagnosis.

At prolonged treatment patients have to be under constant observation of the doctor.

Omeprazol can reduce absorption _{of B12 vitamin} owing to hypo - or achlorhydrias that should be considered at treatment of patients with deficit of cyanocobalamine or risk of its development.

During treatment by Ortanol concentration of chromogranin A in a blood plasma because of what obtaining false positive results when carrying out diagnosis at patients with suspicion of neuroendocrinal tumors is possible can increase. For this reason in 5-14 days prior to the appointed research it is necessary to suspend therapy omeprazoly.

To the patients subject to risk of development of osteoporosis, additional purpose of drugs of calcium and vitamin D as prolonged use of inhibitors of the proton pump can lead to moderate increase of risk of developing of a fracture of bodies of vertebrae, hips and wrists, especially at people of advanced age and at patients with existence of other known risk factors is recommended.

During treatment it is recommended to be careful at the driving of the car and performance of work requiring special attention and high speed of reactions.

Medicinal interaction

Omeprazol can increase an elimination half-life and increase concentration of Phenytoinum, diazepam, warfarin and other drugs which are metabolized in a liver with the participation of CYP2C19 isoenzyme in this connection it is necessary to control their content in blood and if necessary to reduce a dose.

At simultaneous use омепразол increases bioavailability of digoxin for 10%.

In case of the combined appointment disturbance of absorption of medicines which bioavailability is defined preferential by acidity of a gastric juice, for example, of cyanocobalamine, salts of iron, ethers of ampicillin, an itrakonazol, ketokonazol is possible.

Ortanol can strengthen an inhibiting effect on system of a hemostasis of other medicines.

It is not established clinically significant interaction with lidocaine, caffeine, ethanol, propranolol, theophylline, metoprololy, quinidine, antiacid means.

Terms and storage conditions

To store in the place protected from light unavailable to children, at a temperature up to 25 °C.

Period of validity – 2 years.

It is possible to store the solution prepared from lyophilisate no more than 4 hours at a temperature up to 25 ºС.