Kontrolok

General characteristics. Structure:

Active agent: пантопразол sodium sexivihydrat of 45,1 mg corresponds to a sodium pantoprazol (anhydride) of 42,3 mg and a pantoprazola (free acid) of 40 mg.

Excipients: dinatrium эдетат 1 mg; sodium hydroxide of 0,24 mg.

Description: white or almost white dry substance.

Pharmacological properties:

Inhibitor of the proton pump (N + ATP-ase K+). Blocks a final stage of secretion of hydrochloric acid, reducing bazapny and stimulated secretion, irrespective of the irritant nature. At in introduction of 80 mg the anti-secretory effect reaches a maximum during 1 h and 24 h remain. At a peptic ulcer of the duodenum associated with Helicobacter pylori, decrease in gastric secretion increases sensitivity of microorganisms to antibiotics. Does not influence motility of the digestive tract (DT). Secretory activity is normalized in 3-4 days after the end of use,

In comparison with other inhibitors of the proton pump, Kontroyaok has big chemical stability at a neutral rn, and the smaller potential of interaction with oksidazny system of the liver depending on P450 cytochrome. Therefore Kontrolok does not interact with many other widespread drugs.

Pharmacokinetics. The volume of distribution makes 0,15 l/kg, clearance - 0,1 l/h/kg,
Elimination half-life of drug of 1 h.
Several cases of the slowed-down elimination were noted.
The pharmacokinetics is identical both after single, and after repeated use of drug.

In the range of doses from 10 to 80 mg the kinetic straight line of concentration of a pantoprazol in a blood plasma has linear dependence both after oral, and after intravenous use.

Linkng of a pantoprazol with proteins of a blood plasma makes 98%. It is metabolized in a liver. The main way of removal - through kidneys (about 80%) in the form of metabolites of a pantoprazol, in a small amount is removed with a stake. The main metabolite in a blood plasma and in urine is десметилпантопразол, conjugating with sulfate. A metabolite elimination half-life - about 1,5 h.

At use of a pantoprazol for patients with limited functioning of kidneys (including the patients who are on a hemodialysis) the dose decline is not required. As well as at healthy patients, the elimination half-life of a pantoprazol is short. Dialysis irutsya only very small part of drug. Though the elimination half-life of the main metabolite is slowed down (2 - 3 hours), excretion goes still quickly enough and thus accumulation does not happen.

At patients with cirrhosis (classes A and B on Child classification) value of an elimination half-life increases to 7 - 9 h and the indicator of AUC increases by 5 - 7 times, With max increases by 1,5 times in comparison with healthy patients.

Small increase in an indicator of AUC and S max at elderly people is not clinically significant.

Indications to use:

• a peptic ulcer of a stomach and a 12-perstny gut (in an aggravation phase), erosive gastritis (including connected with reception of non-steroidal anti-inflammatory drugs (NPVP);
• gastroesophageal reflux disease (GERB): an erosive reflux esophagitis (treatment), a symptomatic treatment of GERB (i.e. NERB - not erosive reflux disease);
• Zollingera-Ellison's syndrome;
• Helicobacter pylori eradikation in a combination with antibacterial agents.
• treatment and prevention of stressful ulcers, and also their complications (bleeding, perforation, penetration).

Route of administration and doses:

Intravenous use of drug Kontrolok is recommended in cases when oral administration of drug is impossible. The recommended dose are 40 mg a day.

At prolonged treatment of a syndrome of Zolingera-Ellison and other morbid hyper secretory conditions the recommended daily dose in an initiation of treatment makes 80 mg of Kontrolok in / century. After that the dose can be increased or reduced. In case of use of drug in a daily dose over 80 mg, a dose it has to be divided and be entered twice a day. Perhaps temporary increase in a daily dose up to 160 mg of Kontrolok.

At treatment and prevention of stressful ulcers, and also their complications (bleeding, perforation, a penetration). Kontrolok appoint 80 mg a day. In case of use of drug in a daily dose over 80 mg, a dose it has to be divided and be entered twice a day. Perhaps temporary increase in a daily dose up to 160 mg of Kontrolok.

For preparation of solution, ready to the use, for injections of 10 ml of normal saline solution of sodium of chloride add to the bubble containing dry matter. This solution can be applied after mixing from 100 ml of normal saline solution of sodium of chloride, and also from 5% by glucose solution.

Solution for in/in introductions has to have рН 9. Administration of drug should be made within 2-15 minutes. The prepared solution has to be used within 3 hours after preparation.

Features of use:

Intravenous use is recommended only if oral administration is impossible. Use of a pantoprazol is not shown for treatment of easy gastrointestinal complaints, such as dyspepsia of neurogenic genesis. In the presence of any of alarming symptoms (for example, significant inadvertent loss of weight, periodic vomiting, a dysphagy, anemia or a melena) and in case of suspicion or existence of stomach ulcer, it is necessary to exclude a possibility of a malignant new growth as treatment pantoprazoly can reduce symptoms and delay the correct diagnosis. If symptoms remain, despite adequate treatment, then it is necessary to conduct further examination.

It is not necessary to raise a day dose of a pantoprazol of 40 mg at elderly patients and at persons with the broken renal function.

At persons with a heavy liver failure the day dose has to be reduced to 20 mg of a pantoprazol. Besides, at such patients during therapy by drug Kontrolok it is necessary to control liver enzymes. In case of increase in their level treatment has to be interrupted.

Before treatment endoscopic control for an exception of a malignant new growth as treatment can disguise symptomatology is recommended and delay the correct diagnosis.

Side effects:

At Kontrolok's reception according to indications and in the recommended doses by-effects arise extremely seldom.

Purpose of a pantoprazol can be followed by the following side reactions: Typical (> 1/100, <1/10): pains in an upper part of a stomach, diarrhea, a lock, a meteorism; headache.

Not typical (> 1/1 000, <1/100): nausea/vomiting; dizziness, a vision disorder (the obscured sight); allergic reactions, such as itch and skin rash,

Rare (> 1/10 000, <1/1 000): dryness in a mouth, an arthralgia, a depression, hallucinations, a disorientation and confusion of consciousness, especially at the patients predisposed to it, and also strengthening of these symptoms if at patients they were observed earlier.

Very rare (<1/1 0000, including separate cases): leukopenia, thrombocytopenia; thrombophlebitis in an injection site, peripheral hypostases; the hepatocellular insufficiency leading to jaundice with or without liver failure; anaphylactic reactions, including an acute anaphylaxis; increase in enzymes of a liver (transaminase, glyutamiltranspeptidaza); increase in triglycerides; fervescence; mialgiya, intersticial nephrite; small tortoiseshell, Quincke's disease; heavy skin reactions, such as Stephens-Johnson's syndrome, polymorphic erythema, photosensitivity, Layell's cider.

Interaction with other medicines:

Simultaneous use of Kontrolok can reduce absorption of drugs whose bioavailability depends from рН stomach environments (for example, iron salts, кетоконазол, атазанавир and ритонавир).

Kontrolok, unlike other inhibitors of a proton pomp, can be appointed without risk of medicinal interaction:

• to the patients with diseases of cardiovascular system accepting cardiac glycosides (digoxin), blockers of slow calcium channels (nifedipine), beta adrenoblockers (метопролол);
• to the patients with digestive tract diseases accepting antacids, antibiotics (amoxicillin, кларитромицин);
• to the patients accepting oral contraceptives;
• to the patients accepting non-steroidal anti-inflammatory drugs (diclofenac, phenazone, Naproxenum, piroxicam);
• to the patients with diseases of endocrine system accepting glibenclamide, sodium left thyroxine;
• to the patients with alarming conditions and frustration of a dream accepting diazepam;
• to the patients with epilepsy accepting carbamazepine and Phenytoinum;
• to the patients accepting indirect anticoagulants, such as warfarin and фенпрокумон
• to the patients who transferred transplantation, accepting cyclosporine, такролимус.
Also lack of medicinal interaction with theophylline, caffeine and ethanol is noted.

Contraindications:

Hypersensitivity.
There are no data on a clinical use of Kontrolok in pediatric practice.

With care: pregnancy, lactation period, liver failure.

Overdose:

So far the overdose phenomena as a result of Kontrolok's use were not noted. Doses to 240 mg were entered in/in within 2 minutes and transferred well.

Nevertheless, in case of overdose and only in the presence of clinical manifestations (possible strengthening of side effects) the symptomatic and supporting treatment is carried out. Pantoprazol is not brought by means of a hemodialysis.

Storage conditions:

Period of validity 2 years. Not to apply after the expiry date specified on packaging. In the place protected from light. At a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 40 mg of a pantoprazol of powder for preparation of solution for intravenous administration of 40 mg in the bottles of transparent glass corked by a rubber bung and which are pressed out by a cap aluminum with a disk from polypropylene of gray color. On 1 bottle place in a cardboard pack with the application instruction.