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

Active substance: pantoprazole sodium sesquihydrate 45.1 mg corresponds to: pantoprazole sodium (anhydride) 42.3 mg and pantoprazole (free acid) 40.0 mg

Excipients: disodium edetate 1.0 mg; sodium hydroxide 0.24 mg;

Description:

White or almost white dry substance.

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.

Compared with other proton pump inhibitors pantoprazole has a high chemical stability at neutral pH and a lower interaction potential with a liver oxidase system dependent on cytochrome P450. Therefore, it was not observed clinically significant interaction between the Controll ® preparation and many other drugs.

Pharmacokinetics:

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

Half-life of the drug -1h.

Several cases of delayed elimination were noted.

Pharmacokinetics is the same as after a single, and after repeated use of the drug. In the dose range of 10 mg to 80 mg, the kinetic direct concentration of pantoprazole in blood plasma has a linear relationship both after oral and after intravenous administration.

The binding of pantoprazole to plasma proteins is 98%. Metabolised in the liver. The main way of excretion is through the kidneys (about 80%) in the form of metabolites of pantoprazole, in a small amount is excreted through the intestine. The main metabolite in the blood plasma and in urine is desmethylpentoprazole, conjugating with sulfate. The half-life of the metabolite is about 1.5 h.

When pantoprazole is used in patients with impaired renal function (including patients on hemodialysis), no dose reduction is required. As in patients with normal renal function, 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 and B according to the Child-Pugh classification), the value of the elimination half-life increases to 7-9 hours. AUC increases 5 to 7 times. FROMmah increases by 1.5 times compared with patients with normal liver function.

A slight increase in the indicator AUC and Cmah in the elderly is not clinically significant.

Indications:

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

- gastroesophageal reflux disease (GERD): erosive reflux-esophagitis (treatment), symptomatic treatment of GERD (ie NERB - non-erosive reflux disease);

- Zollinger-Ellison syndrome;

- eradication Helicobacter pylori in combination with antibacterial agents;

- treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration).

Contraindications:

- hypersensitivity to any of the components of the drug.

- combined use with atazanavir.

- age to 18 years.

- pregnancy, lactation.

Dosing and Administration:

Intravenous administration of the drug should be carried out by medical personnel. Intravenous use of the preparation Controllok® is recommended in cases when oral administration of the drug is not possible and for a period not exceeding 7 days. If the patient has the possibility of oral administration, intravenous administration should be replaced with the ingestion of Controlul® tablet coated with an enteric coating. Stomach ulcer and duodenal ulcer (in the phase of exacerbation), erosive gastritis (including those associated with taking nonsteroidal anti-inflammatory drugs NSAIDs), gastroesophageal reflux disease (GERD).

The recommended daily dose is 40 mg (1 vial) per day.

Zollinger-Ellison syndrome.

With long-term treatment of Zolinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose at the beginning of treatment is 80 mg of Controllok® intravenously. After this, the dose may be increased or decreased. If the drug is used in a daily dose of more than 80 mg, the dose should be divided and administered twice a day. It is possible to temporarily increase the daily dose to 160 mg, but not longer than necessary for adequate acidity control.

If an emergency acidity control is required, the initial dose of twice 80 mg is sufficient to reduce the acid release in the range of less than 10 mEq / h for 1 hour in most patients.

Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration).

The recommended daily dose is 80 mg per day. If the drug is used in a daily dose of more than 80 mg, the dose should be divided and administered twice a day. Perhaps a temporary increase in the daily dose to 160 mg.

To prepare a ready-to-use solution for injection, 10 ml of a 0.9% sodium chloride solution is added to a vial containing a dry substance.The ready-made solution can be administered in an amount of 10 ml, it is also permissible to dilute it in 100 ml of a 0.9% solution of sodium chloride or in a 5% solution of glucose.

Do not use any other solvents!

The drug should be administered within 2-15 minutes.

The prepared solution is stable for 12 hours after preparation. However, it is recommended to use the solution immediately after preparation in order to avoid microbial contamination.

In patients with severe impairment of liver function, the daily dose should not exceed 20 mg of pantoprazole (half a vial).

Dose adjustments in elderly patients and patients with impaired renal function are not required, but do not exceed recommended daily dose of pantoprazole 40 mg.

Side effects:

When taking Controlulok® in accordance with the indications and in recommended doses, side effects occur extremely rarely. The most common undesirable side effect is thrombophlebitis at the injection site. Diarrhea and headache is 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, discomfort and 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:

Often:

Thrombophlebitis at the injection site.

Infrequently:

Weakness, fatigue and malaise.

Rarely:

Increased body temperature, peripheral edema.

Immune system disorders:

Rarely:

Hypersensitivity (including anaphylactic reactions and anaphylactic shock).

Disorders from the liver and bile ducts:

Infrequently:

Increased activity of hepatic enzymes (aspartate aminotransferase, gamma-glutamintransferase).

Rarely:

Increased bilirubin level.

Frequency unknown:

Hepatocellular injuries, jaundice.

Violations of the genitals and breast:

Rarely:

Dinecomastia.

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 they were well tolerated.

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:

Simultaneous use of the drug Controllok® can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (for example, ketoconazole, intraconazole, posaconazole and such as erlotinib). The drug Controllok® can be prescribed without the risk of negative drug interactions:

- Patients with diseases of the cardiovascular system who take cardiac glycosides (digoxin), blockers of slow calcium channels (nifedipine), beta-blockers (metoprolol);

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

- patients taking oral contraceptives containing levonorgestrel and ethinyl estradiol;

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

patients with diseases of the endocrine system who receive glibenclamide;

- patients with anxiety and sleep disorders receiving diazepam;

- patients with epilepsy receiving carbamazepine and phenytoin; patients receiving 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;

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

Special instructions:

The use of pantoprazole is not indicated for the treatment of mild gastrointestinal complaints, such as dyspepsia of a neurogenic genesis.

Patients should consult a physician if the following symptoms occur:

- Significant unintended weight loss,

- periodic vomiting,

- swallowing disorder,

- gastrointestinal bleeding,

- anemia or melena.

If you suspect or have a stomach ulcer before starting treatment with pantoprazole, you should rule out the possibility of a malignant neoplasm,because the drug can mask the symptoms and delay the correct diagnosis.

If the symptoms persist despite adequate treatment, further examination should be carried out.

In patients with severe impairment of liver function, biochemical blood counts must be monitored. When the activity of liver enzymes increases, the drug should be discontinued.

When taking drugs that reduce the acidity of gastric juice, slightly increases the risk of gastrointestinal infections, the causative agents of which are bacteria of the genus Salmonella spp., Campylobacter spp.

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:

Powder for the preparation of a solution for intravenous administration of 40 mg.

Packaging:

For 40 mg of pantoprazole in bottles of clear glass, sealed with a rubber stopper and crimped with an aluminum cap with a disk of gray polypropylene.

1 bottle is placed in a cardboard box with instructions for use.

Storage conditions:

In the dark place.

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-004368/08

Date of registration:07.06.2008

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®)