Controlock, lyophilizate 40 mg

Controlok is a proton pump inhibitor.

Proton pump inhibitor (H⁺-K⁺-ATPase). Blocks the final stage of hydrochloric acid secretion by reducing basal and stimulated secretion, regardless of the nature of the stimulus.

Antisecretory activity. After oral administration of 20 mg of Controlock^® antisecretory effect occurs in 1 hour and reaches a maximum in 2-4 hours. With intravenous administration of 80 mg the antisecretory effect reaches its maximum within 1 hour and lasts for 24 hours. In duodenal ulcer associated with Helicobacter pylori, decreased gastric secretion increases the sensitivity of microorganisms to antibiotics. It does not affect gastrointestinal motility. The secretory activity is normalized in 3-4 days after the end of administration.

Compared with other proton pump inhibitors, Controlock^® has greater chemical stability at neutral pH, and less potential for interaction with cytochrome P450-dependent liver oxidase system. Therefore, Controlok does not interact with many other common drugs.

Indications

Active ingredient

Composition

1 vial contains:

The active ingredient:

Pantoprazole sodium sesquihydrate – 45.1 mg (corresponding to pantoprazole sodium (anhydride) 42.3 mg and pantoprazole (free acid) 40 mg);

Associates:

Dinatrium edetate, 1 mg;

Sodium hydroxide, 0.24 mg.

How to take, the dosage

Intravenous administration of Controlox® is recommended in cases where oral administration is not possible. The recommended dose is 40 mg/day.

In the long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose at the beginning of treatment is 80 mg of Contrololok® w/v. After that the dose may be increased or decreased. If a daily dose above 80 mg is used, the dose should be divided and administered twice daily. It is possible to temporarily increase the daily dose up to 160 mg of Controlox®.

In the treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration): the drug Controlock® is prescribed at 80 mg/day. In case of using the drug in a daily dose above 80 mg, the dose should be divided and administered twice a day. It is possible to temporarily increase the daily dose to 160 mg of Controlox®.

To prepare a ready-to-use solution for injection, 10 ml of physiological sodium chloride solution is added to the vial containing the dry substance. This solution can be used after mixing with 100 ml of physiological sodium chloride solution as well as with 5% glucose solution.

The solution for IV administration should have a pH of 9. The drug should be administered within 2-15 minutes.

The prepared solution should be used within 3 hours after preparation.

Interaction

The concomitant use of Controlock®® may reduce absorption of drugs whose bioavailability depends on the pH of the stomach (e.g., iron salts, ketoconazole).

Controlok®, unlike other proton pump inhibitors, can be prescribed without risk of drug interactions:

Special Instructions

Injection is recommended only if oral administration is not possible.

Pantoprazole is not indicated for the treatment of mild gastrointestinal complaints, such as dyspepsia of neurogenic origin.

In the presence of any of the alarming symptoms (e.g., significant unintentional weight loss, recurrent vomiting, dysphagia, anemia, or melena) and if gastric ulcer is suspected or present, the possibility of malignancy should be excluded, as pantoprazole treatment may reduce symptoms and delay correct diagnosis.

If symptoms persist despite adequate treatment, further evaluation should be performed.

The daily dose of pantoprazole 40 mg should not be increased in elderly patients and persons with impaired renal function.

In persons with severe hepatic impairment the daily dose should be reduced to 20 mg pantoprazole. In addition, in these patients liver enzymes should be monitored during therapy with Contrololok®. If their levels are elevated, treatment should be interrupted.

Before and after treatment, endoscopic control is recommended to rule out malignancy, as treatment may mask symptoms and delay correct diagnosis.

Contraindications

Hypersensitivity; dyspepsia of neurotic genesis (tablets).

With caution: pregnancy, lactation, liver failure.

Side effects

Typical: upper abdominal pain, diarrhea, constipation, flatulence; headache.

Atypical: nausea/vomiting, dizziness, visual disturbances (blurred vision); allergic reactions such as itching and skin rash.

Rare: dry mouth, arthralgia, depression, hallucinations, disorientation and confusion, especially in patients who are predisposed to it, and also an increase in these symptoms if patients have previously had them.

Very rare: Leukopenia, thrombocytopenia; thrombophlebitis at the injection site (powder for preparation of solution for IV administration); peripheral edema; severe hepatocellular damage leading to jaundice with or without liver failure; anaphylactic reactions, including anaphylactic shock; increased liver enzymes (transaminases, glutamyl transpeptidase); increased triglycerides; increased body temperature; myalgia, interstitial nephritis; urticaria, angioedema; severe skin reactions such as Stevens-Johnson syndrome, erythema multiforme, photosensitivity, Lyell syndrome.

Overdose

To date, there have been no overdoses as a result of Controlock.

Doses up to 240 mg have been administered by IV within 2 minutes and have been well tolerated.

However, in case of overdose and only in the presence of clinical manifestations (possible worsening of side effects), symptomatic and supportive treatment is given.

Pantoprazole is not excreted by hemodialysis.

Pregnancy use

Controlok should be used with caution during pregnancy and lactation.

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