Controls - instructions for use, dose, side effects, contraindications

Excipients: sodium carbonate anhydrous 10.00 mg; mannitol 42.70 mg; crospovidone 50.00 mg; Povidone K90 4.00 mg; calcium stearate 3.20 mg; purified water 9.00 mg;

Shell

hypromelose-2910 19.00 mg; Povidone K25 0.38 mg; titanium dioxide E171 0.34 mg; ferric iron oxide yellow E172 0.03 mg; propylene glycol 4.25 mg; eudragit L 30D-55 * 14.56 mg; triethyl citrate 1.45 mg.

* Eudragit L 30D-55 dispersion composition: eudragit L30D-55 (methacrylic acid and ethyl acrylate copolymer [1: 1]) 14.13 mg; polysorbate 80 0.33 mg; sodium lauryl sulfate 0.10 mg;

Brown Ink Opacode S-1-16530 for labeling on tablets:

shellac 0.036 mg; iron dye red oxide (E172) 0.009 mg; ferric dye oxide black (E172) 0.009 mg; ferric iron oxide yellow (E172) 0.0009 mg; ammonia solution concentrated 25% 0.001 mg;

Description:

Oval biconvex tablets, covered with a film coating of yellow color with a core from white to almost white. On one side of the tablet brown ink is printed: "P40".

Pharmacotherapeutic group:glands of the stomach secretion-lowering agent - proton pump inhibitor

ATX: & nbsp

A.02.B.C Proton pump inhibitors

A.02.B.C.02 Pantoprazole

Pharmacodynamics:

Proton pump inhibitor (H⁺ TO⁺ ATPase). It blocks the final stage of hydrochloric acid secretion, reducing basal and stimulated secretion, regardless of the nature of the stimulus.

Antisecretory activity. After the first oral administration of 20 mg of Controllok®, the decrease in gastric juice secretion by 24% occurs 2.5-3.5 hours and 26% after 24.5-25.5 hours. After oral administration, once a day for 7 days antisecretory activity increases to 56% after 2.5-3.5 h and up to 50% after 24.5-25.5 h. In peptic ulcer disease associated with duodenal ulcer Helicobacter pylori, decrease in gastric secretion increases the sensitivity of microorganisms to antibiotics. Does not affect the motility of the gastrointestinal tract. Secretory activity is normalized 3-4 days after the end of admission.

Compared to other inhibitors of the proton pump, Controllok® has a high chemical stability at neutral pH, and a lower interaction potential with a liver oxidase system dependent on cytochrome P450. Therefore, there was no clinically significant interaction between the Controll ® preparation and many other drugs.

Pharmacokinetics:Pantoprazole is rapidly absorbed after ingestion. The maximum concentration in the blood plasma (C_max) for oral administration is achieved after the first dose of 40 mg. Average, C_max, 1.0 to 1.5 μg / ml is achieved at 2.0 to 3.0 μg / ml after 2.5 hours for a dosage of 40 mg. This indicator remains constant after repeated use of this drug.

The volume of distribution is 0.15 l / kg, the clearance is 0.1 l / h / kg.

Half-life of the drug -1h.

Pharmacokinetics is the same as after a single, and after repeated use of the drug.

The binding of pantoprazole to plasma proteins is 98%. Metabolised in the liver. The main way of excretion - through the kidneys (about 80%) in the form of metabolites of pantoprazole, in a small amount is output through kiwStern. The main metabolite in the blood plasma and in urine is desmethylpentoprazole, conjugating with sulfate.

Absolute bioavailability of pantoprazole tablets is 77%. Simultaneous use of them with food does not affect the area under the curve "concentration-time" (AUC) and C_max.

When pantoprazole is used in patients with limited renal function (including patients on hemodialysis), no dose reduction is required. As in healthy patients, the half-life of pantoprazole is short. Only a very small part of the drug is dialyzed. Does not accumulate.

In patients with cirrhosis of the liver (classes A, B and C according to the Child-Pugh classification), the value of the elimination half-life increases to 7-9 hours when pantoprazole is administered at a dosage of 40 mg. Index AUC increases 5-7 times for a dosage of 40 mg. FROM_maxincreases by 1.5 times for a dosage of 40 mg compared to healthy patients. A slight increase in the indicator AUC and C_max in the elderly is not clinically relevant.

Indications:

- peptic ulcer of the stomach and duodenum (in the phase of exacerbation), erosive gastritis (including associated with the use of non-steroidal anti-inflammatory drugs NSAIDs);

- Zollinger-Ellison syndrome;

- eradication Helicobacter pylori in combination with antibacterial agents;

Contraindications:

- hypersensitivity to any of the components of the drug, as well as to soy.

- dyspepsia of a neurotic genesis.

- combined use with atazanavir.

- age to 18 years.

- pregnancy, lactation.

Dosing and Administration:

Controllok® is taken orally, before meals, without chewing or grinding, with a sufficient amount of liquid.

Peptic ulcer of the stomach and duodenum, erosive gastritis (including, associated with the use of non-steroidal anti-inflammatory drugs NSAIDs).

For 40-80 mg per day.

The course of treatment - 2 weeks with exacerbation of duodenal ulcer and 4-8 weeks with peptic ulcer exacerbation.

Anti-relapse treatment of peptic ulcer of the stomach and duodenum - 20 mg per day.

Eradication Helicobacter pylori.

The following combinations are recommended:

1. Controlul® on 20-40 mg twice a day + amoxicillin 1000 mg twice a day + clarithromycin 500 mg twice a day

2. Controlul® on 20-40 mg twice a day + metronidazole 500 mg twice a day + clarithromycin 500 mg twice a day

3. Controlul® on 20-40 mg twice a day + amoxicillin 1000 mg twice a day + metronidazole 500 mg twice a day.

The course of treatment is 7-14 days.

Zollinger-Ellison syndrome.

For 40-80 mg per day.

In patients with severe impairment of liver function, the dose should be reduced to 40 mg once every 2 days. In this case it is necessary to control the biochemical parameters of the blood. When the activity of liver enzymes increases, the drug should be discontinued.

Dose adjustments in elderly patients, as well as in patients with impaired renal and hepatic function, are not required, but the daily dose of 40 mg can not be exceeded. An exception is the use of combined antimicrobial therapy in relation to Helicobacter pylori, when elderly patients should also use Controlul® 40 mg twice daily.

Do not take Controller® for prophylaxis.

Side effects:

When taking Controlulok® in accordance with the indications and in recommended doses, side effects occur extremely rarely. The most frequent undesirable

adverse reactions are diarrhea and headache - are observed in about 1% of patients.

The following are the data on undesirable side reactions, depending on the frequency of their occurrence:

Often ≥ 1/10

Often ≥ 1/100 and <1/10

Infrequently ≥ 1/1000 and <1/100

Rarely ≥ 1/10000 and <1/1000

Very rarely <1/10000, including individual cases

The frequency is unknown (can not be estimated from the available data).

Violations from the blood and lymphatic system:

Rarely:

agranulocytosis

Rarely:

thrombocytopenia, leukopenia, pancytopenia.

Impaired nervous system:

Infrequently:

headache, dizziness.

Rarely:

dysgeusia

Disorders from the organs of vision:

Rarely:

visual impairment (fogging).

Disorders from the gastrointestinal tract:

Infrequently:

diarrhea, nausea / vomiting, bloating and flatulence, constipation, dry mouth, abdominal pain. Disorders from the kidneys and urinary tract:

Frequency unknown:

Interstitial nephritis.

Disturbances from the skin and subcutaneous tissues:

Infrequently:

Exanthema / rash, itching.

Rarely:

Hives, angioedema.

Frequency unknown:

malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, toxic epidermal necrolysis, photosensitivity.

Disturbances from the musculoskeletal and connective tissue:

Rarely:

Arthralgia, myalgia.

Disorders from the metabolism:

Rarely:

Hyperlipidemia and increased concentration of lipids (triglycerides, cholesterols), change in body weight.

Frequency unknown:

Hyponatremia, hypomagnesemia.

General disorders:

Infrequently:

Weakness, fatigue and malaise.

Rarely:

Increase temperatures body, peripheral edema.

Immune system disorders:

Rarely:

Hypersensitivity (including anaphylactic reactions and anaphylactic shock).

Disorders from the liver and bile ducts:

Infrequently:

Increase in activity of hepatic enzymes (aspartate aminotransphase, gamma - glutamintransferase).

Rarely:

Increased bilirubin level.

Frequency unknown:

Hepatocellular injuries, jaundice.

Violations of the genitals and mammary glands:

Rarely:

Gynecomastia

Disorders from the psyche:

Infrequently:

Sleep disturbance.

Rarely:

Depression (including exacerbations of existing disorders).

Rarely:

Disorientation (including exacerbations of existing disorders).

Frequency unknown:

Hallucinations, confusion (especially in patients predisposed to this), as well as possible exacerbation of symptoms when they exist before the start of therapy.

Overdose:

To date, there have been no overdose events as a result of the use of Controllok®. Doses up to 240 mg were administered intravenously for 2 minutes and were tolerated well.

However, in case of an overdose and only in the presence of clinical manifestations, symptomatic and supportive therapy is performed. Pantoprazole is not excreted by hemodialysis.

Interaction:

It is not recommended simultaneous use of other inhibitors of the proton pump or H2-histamine receptor blockers without consulting a doctor.

Simultaneous use of Controllok® can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (for example, iron salts, ketoconazole).

Controller® can be prescribed without the risk of drug interaction:

- patients with cardiovascular diseases receiving cardiac glycosides (digoxin), blockers of slow calcium channels (nifedipine), beta-blockers (metoprolol);

- patients with diseases of the gastrointestinal tract, taking antacids, antibiotics (amoxicillin, clarithromycin);

- patients taking oral contraceptives containing levonorgestrel and ethinyl estradiol;

- patients taking non-steroidal anti-inflammatory drugs (diclofenac, phenazone, naproxen, piroxicam);

patients with diseases of the endocrine system who receive glibenclamide, levothyroxine;

- patients with anxiety and sleep disorders receiving diazepam;

- patients with epilepsy receiving carbamazepine and phenytoin;

- patients taking indirect anticoagulants, such as warfarin and fenprokumone, under the control of prothrombin time and INR at the beginning and at the end of treatment, as well as during the irregular intake of pantoprazole;

- patients who have undergone transplantation, receive ciclosporin, tacrolimus.

There was also a lack of clinically significant drug interaction with caffeine, ethanol, theophylline.

Special instructions:

Before beginning treatment with the drug Controllok®, the possibility of malignant neoplasm should be excluded, since the drug can mask symptoms and delay the correct diagnosis.

Patients should consult a physician if they are to carry out endoscopy or a urea breath test.

Patients should consult a doctor if the following cases occur: unintended weight loss, anemia, gastrointestinal bleeding, swallowing disorder, persistent vomiting or vomiting with blood. In these cases, taking the drug can partially alleviate the symptoms and delay the correct diagnosis;

- previously suffered surgical intervention on the gastrointestinal tract or stomach ulcer;

- continuous symptomatic treatment of dyspepsia and heartburn for 4 weeks or more;

- liver disease, including jaundice and liver failure;

- other serious diseases that worsen overall health;

Patients over the age of 55 years, with new or newly changed symptoms, should consult a physician.

When you receive drugs that reduce gastric acidity, slightly increase the risk of gastro-intestinal infections, pathogens that are bacteria of the genus Salmonella spp., Campylobacter spp. or C. difficile.

Effect on the ability to drive transp. cf. and fur:It should refrain from driving and other mechanisms that require increased attention, due to the likelihood of dizziness and visual impairment.

Form release / dosage:

Tablets coated with enteric coating 40 mg.

Packaging:

For 14 tablets per blister Aluminum PVC / Aluminum PVC. 1 or 2 blisters together with instructions for use in a cardboard pack.

5 tablets in a blister enclosed in a folding cardboard cover. On 3 cardboard covers together with the instruction on application place in a pack a cardboard. 7 tablets in a blister enclosed in a folding cardboard cover. For 1 or 4 cardboard covers, along with instructions for use, put in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N011341 / 01

Date of registration:28.04.2008

The owner of the registration certificate:Takeda GmbHTakeda GmbH Germany

Manufacturer: & nbsp

TAKEDA, GmbH Germany

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp08.09.2015

Illustrated instructions

Instructions

Controller® (Controloc®)