Kontrolok

Kontrolok – the drug promoting decrease in secretion of gastric glands.

Form of release and structure

Kontrolok release in the following dosage forms:

• The tablets covered with a kishechnorastvorimy cover: biconvex, oval, covered with a yellow film cover, with a kernel from almost white till white color; on one of the parties – marking by brown ink (tablets on 20/40 mg) "P20" or "P40" (on 5 pieces in blisters, on 3 blisters in a cardboard pack; on 7 pieces in blisters, on 1, 4 blisters in a cardboard pack; on 14 pieces in blisters, on 1, 2 blisters in a cardboard pack);
• Powder for preparation of solution for intravenous administration: almost white or white dry substance (in bottles, on 1 bottle in a cardboard pack).

Is a part of 1 tablet:

• Active agent: пантопразол – 20 or 40 mg (in the form of a pantoprazol of sodium of sexivihydrat – 22,57 or 45,1 mg);
• Auxiliary components: anhydrous sodium carbonate – 5/10 mg, кросповидон – 25/50 mg, Mannitolum – 21,33/42,7 mg, K90 povidone – 2/4 mg, calcium stearate – 1,6/3,2 mg, the purified water – 4,5/9 mg.

Structure of a cover (a tablet on 20/40 mg respectively): the gipromelloza of 2910 - 11,88/19 mg, K25 povidone – 0,24/0,38 mg, titanium dioxide (E171) – 0,21/0,34 mg, dye ferrous oxide yellow (E172) – 0,02/0,03 mg, propylene glycol – 2,66/4,25 mg, eudragit L30D-55 – 8,18/14,56 mg (ethyl acrylate and methacrylic acid copolymer [1:1] – 7,94/14,13 mg, polysorbate 80 – 0,18/0,33 mg, sodium lauryl sulfate – 0,06/0,1 mg), triethyl citrate – 0,82/1,45 mg.

Composition of Opacode S-1-16530 ink of brown color for drawing on marking tablets: shellac (shellac) – 0,036 mg, strong solution of ammonia of 25% – 0,001 mg, dyes (ferrous oxide red (E172) – 0,009 mg, ferrous oxide black (E172) – 0,009 mg, ferrous oxide yellow (E172) – 0,0009 mg).

For preparation of solution for injections is a part of 1 bottle:

• Active agent: пантопразол – 40 mg (in the form of a pantoprazol of sodium of sexivihydrat – 45,1 mg);
• Auxiliary components: эдетат dinatrium – 1 mg, sodium hydroxide – 0,24 mg.

Indications to use

• Gastroesophageal reflux disease of easy degree of manifestation at adults, including heartburn, nausea, an acid eructation (symptomatic treatment);
• Peptic ulcer of a stomach and duodenum (at an aggravation), erosive gastritis (including connected using non-steroidal anti-inflammatory drugs);
• Zollingera-Ellison's syndrome;
• Eradikation Helicobacter pylori (along with antibacterial drugs).

Contraindications

• Dyspepsia of neurotic genesis;
• Simultaneous use with atazanaviry;
• Age up to 18 years;
• Pregnancy and period of a lactation;
• Hypersensitivity to drug components, and also to soy.

Route of administration and dosage

Kontrolok in the form of tablets accept inside to food, washing down with enough liquid. Tablets should not be chewed and crushed.

The mode of dosing is defined by indications.

At treatment of the symptoms of a gastroesophageal reflux disease (such as nausea, heartburn, an acid eructation) proceeding with easy degree of manifestation, the adult appoint 20 mg of Kontrolok inside. As a rule, positive dynamics is reached within 2-3 days of administration of drug, however for full elimination of symptoms therapy is usually continued for 7 days. If in the first 3 days of treatment the state worsens, and also in cases of lack of improvement at continuous reception of Kontrolok for 14 days, it is necessary to consult with the doctor.

At a peptic ulcer of a stomach and duodenum and erosive gastritis (including connected using non-steroidal anti-inflammatory drugs), Kontrolok appoint 40-80 mg in a daily dose. At an aggravation of a peptic ulcer of a duodenum the course of therapy makes 14 days, a stomach – 4-8 weeks. For prevention of development of a recurrence of a peptic ulcer of a stomach and a duodenum drug is accepted on 20 mg a day.

Kontrolok in a single dose of 20-40 mg is recommended to apply to Helicobacter pylori eradikation at the same time with the following drugs (single dose):

• Amoxicillin – 1000 mg, кларитромицин – 500 mg;
• Metronidazole – 500 mg, кларитромицин – 500 mg;
• Amoxicillin – 1000 mg, metronidazole – 500 mg.

Frequency rate of use of all drugs – 2 times a day. Duration of a therapeutic course – 1-2 weeks.

At a syndrome Zollingera-Ellisona Kontrolok appoint 40-80 mg in a daily dose.

At patients with the expressed functional disturbances of a liver the dose is reduced to 40 mg of 1 times in 2 days, at the same time it is necessary to carry out control of biochemical indicators of blood. At increase in level of liver enzymes Kontrolok's use should be interrupted.

Dose adjustment is not required to elderly patients, and also patients with functional disturbances of kidneys, however the daily dose should not be more than 40 mg (except performing the combined antibacterial therapy concerning Helicobacter pylori when drug is accepted on 40-80 mg in 2 receptions).

Kontrolok it is not necessary to accept in the preventive purposes.

Intravenously Kontrolok's solution is entered in cases when administration of drug is inside impossible. The recommended daily dose – 40 mg.

At long therapy of a syndrome of Zollingera-Ellison and other morbid conditions with the increased secretory function in an initiation of treatment the drug is administered on 80 mg a day. Depending on reaction to Kontrolok, the daily dose can be reduced or increased. If the daily dose exceeds 80 mg, the drug should be administered in 2 receptions. If necessary perhaps temporary increase in a dose up to 160 mg a day.

The same mode of dosing is applied at prevention and treatment of stressful ulcers and their complications (perforation, bleeding, a penetration).

For preparation of solution of Kontrolok of 10 ml of normal saline solution of sodium chloride it is necessary to add to the bottle containing dry matter. Solution can be applied after mixing from 100 ml of normal saline solution of sodium chloride, and also from 5% glucose solution.

Kontrolok's solution for intravenous administration has to have рН =9. The drug is administered within 2-15 minutes.

It is possible to store the prepared solution no more than 3 hours.

Side effects

At Kontrolok's use according to indications and with observance of the recommended doses side effects are observed extremely seldom.

Most often (about 1% of cases) there is a headache and diarrhea.

Also during Kontrolok's use the following disturbances (≥1/10 – very often, ≥1/100 and <1/10 – it is frequent, ≥1/1000 and <1/100 – infrequently, ≥ 1/10 000 and <1/1000 – it is rare, <1/10 000 (including separate cases) can develop – it is very rare; at impossibility to estimate emergence frequency on the basis of the available data – with an unknown frequency):

• Alimentary system: infrequently – dryness in a mouth, diarrhea, vomiting/nausea, a meteorism, abdominal distention, a lock, pains in a stomach;
• Musculoskeletal system: seldom – a mialgiya, an arthralgia;
• Endocrine system: seldom – a gynecomastia;
• Immune system: seldom - hypersensitivity (including an acute anaphylaxis and anaphylactic reactions);
• Urinary system: with an unknown frequency – intersticial nephrite;
• Nervous system: infrequently – dizziness, a headache; seldom – a dysgeusia;
• System of a hemopoiesis: seldom – an agranulocytosis; very seldom – a leukopenia, thrombocytopenia, a pancytopenia;
• Liver and biliary tract: infrequently – increase in activity of liver enzymes (aspartate aminotransferase, gamma глутамилтрансферазы); seldom – increase in level of bilirubin; with an unknown frequency – jaundice, hepatocellular damages;
• Organ of sight: seldom – a vision disorder (in the form of misting);
• Skin and hypodermic fabrics: infrequently – a rash/dieback, an itch; with an unknown frequency – an exudative mnogoformny erythema, a malignant exudative erythema (Stephens-Johnson's syndrome), a photosensitization, a toxic epidermal necrolysis;
• Metabolism: seldom – a lipidemia and the increased concentration of lipids (holesterol, triglycerides), change of body weight; with an unknown frequency – a hypomagnesiemia, a hyponatremia;
• Mentality: infrequently – a sleep disorder; seldom – a depression (including an aggravation of the available frustration); very seldom – a disorientation (including an aggravation of the available frustration); with an unknown frequency – confusion of consciousness, a hallucination (in particular at the patients predisposed to it), and also an aggravation of symptoms at their existence prior to treatment;
• Allergic reactions: seldom – a Quincke's disease, a small tortoiseshell;
• General reactions: infrequently – an indisposition, fatigue, weakness; seldom – peripheral hypostases, increase in body temperature.

Special instructions

Before therapy it is necessary to exclude a possibility of existence of malignant new growths as Kontrolok can mask their signs and delay diagnosis.

Before carrying out the ureal respiratory test or endoscopy it is necessary to consult with the doctor who appointed treatment. Also it is necessary to see a doctor at the following diseases / states:

• Anemia, inadvertent loss of weight, gastrointestinal bleedings, dysphagias, vomiting with blood or constant vomiting (Kontrolok's use can partially facilitate symptoms of a disease and delay the correct diagnosis);
• Peptic ulcer of a stomach or the surgical intervention on digestive tract postponed earlier;
• Continuous long (of 4 weeks) symptomatic therapy of heartburn and dyspepsia;
• Liver diseases, including jaundice and a liver failure;
• Other serious diseases worsening the general state of health.

To patients 55 years at emergence of the new or changed recently symptoms are more senior it is necessary to consult with the doctor.

At simultaneous use with the drugs reducing acidity of a gastric juice the risk of development of infections which causative agents are bacteria of a sort of gastrointestinal Campylobacter spp slightly increases., Salmonella spp. or Clostridia difficile.

During therapy it is recommended to abstain from the control of motor transport and other mechanisms demanding bystry reactions and special attention (because of probability of development of vision disorders and dizziness).

Medicinal interaction

Kontrolok can reduce absorption of medicines which bioavailability depends from рН stomach environments (including кетоконазол, iron salts).

Without risk of medicinal interaction Kontrolok it is possible to apply along with such drugs as:

• Beta adrenoblockers (метопролол), blockers of slow calcium channels (nifedipine), cardiac glycosides (digoxin): at diseases of cardiovascular system;
• Antacids, antibiotics (кларитромицин, amoxicillin): at digestive tract diseases;
• Diazepam: at alarming conditions and frustration of a dream;
• Left thyroxine, glibenclamide: at diseases of endocrine system;
• Takrolimus, cyclosporine: after transplantation;
• Oral contraceptives with the content of levonorgestrel and ethinylestradiol;
• Non-steroidal anti-inflammatory drugs (piroxicam, diclofenac, Naproxenum, phenazone);
• Phenytoinum, carbamazepine;
• Indirect anticoagulants (фенпрокумон, warfarin).

Development of clinically significant medicinal interaction with ethanol, caffeine and theophylline is noted.

Terms and storage conditions

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

Period of validity – 3 years.