Controlock, powder 40mg vial 1pc

Composition

1 bottle contains:

Active ingredient:

pantoprazole sodium sesquihydrate-45.1 mg (corresponds to pantoprazole sodium (anhydride) 42.3 mg and pantoprazole (free acid) 40 mg);

Auxiliary substances:

disodium edetate — 1 mg;

sodium hydroxide-0.24 mg

Pharmacological action

Kontrolok is a proton pump inhibitor.

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

Antisecretory activity. After oral use of 20 mg of Controlok®, the antisecretory effect occurs in 1 hour and reaches a maximum in 2-4 hours. With intravenous use of 80 mg, the antisecretory effect reaches a maximum within 1 hour and persists for 24 hours. In Helicobacter pylori-associated duodenal ulcer, a decrease in gastric secretion increases the sensitivity of microorganisms to antibiotics. It does not affect the motility of the gastrointestinal tract. Secretory activity normalizes in 3-4 days after the end of treatment.

Compared to other proton pump inhibitors, Controlok ® has a higher chemical stability at neutral pH, and a lower potential for interaction with the cytochrome P450-dependent liver oxidase system. Therefore, Kontrolok does not interact with many other common medications.

Indications

• Peptic ulcer of the stomach and duodenum (in the acute phase), erosive gastritis (including those associated with taking NSAIDs).
• Gastroesophageal reflux disease( GERD): treatment of erosive reflux esophagitis, symptomatic treatment of non-erosive reflux disease (NERD).
• Zollinger-Ellison syndrome.
• Eradication of Helicobacter pylori in combination with antibacterial agents.
• Treatment and prevention of stress ulcers, as well as their complications in the form of bleeding, perforation, and penetration (for intravenous solution).

Use during pregnancy and lactation

Kontrolok should be used with caution during pregnancy and lactation.

Contraindications

Hypersensitivity; dyspepsia of neurotic origin (tablets).

With caution:  pregnancy, lactation, liver failure.

Side effects

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

Atypical ones:  nausea/vomiting, dizziness, blurred vision; allergic reactions such as pruritus and skin rash.

Rare ones:  dry mouth, arthralgia, depression, hallucinations, disorientation and confusion, especially in patients predisposed to this, as well as an increase in these symptoms if patients have previously experienced them.

Very rare ones:  leukopenia, thrombocytopenia; thrombophlebitis at the injection site (powder for preparing a solution for intravenous use); peripheral edema; severe hepatocellular damage leading to jaundice with or without liver failure; anaphylactic reactions, including anaphylactic shock; increased liver enzymes (transaminases, glutamyltranspeptidases); increased triglycerides; increased body temperature; myalgia, interstitial nephritis; urticaria, angioedema; severe skin reactions such as Stevens-Johnson syndrome, erythema multiforme, photosensitivity, Lyell’s syndrome.

Interaction

Concomitant use of Kontrolok may reduce the absorption of drugs whose bioavailability depends on the pH of the gastric environment (for example, iron salts, ketoconazole).

Kontrolok®, unlike other proton pump inhibitors, can be prescribed without the risk of drug interaction:

• patients with diseases of the cardiovascular system, the receiving cardiac glycosides (digoxin), CCB(nifedipine), β-blockers (metoprolol);
• patients with diseases of the gastrointestinal tract taking antacids, antibiotics (amoxicillin, clarithromycin);
• patients receiving oral contraceptives;
• patients receiving NSAIDs (diclofenac, phenazone, naproxen, piroxicam);
• patients with diseases of the endocrine system, the receiving glibenclamide, levothyroxine;
• patients with anxiety and sleep disorders, receiving diazepam;
• patients with epilepsy taking carbamazepine and phenytoin;
• patients receiving indirect anticoagulants, such as warfarin and phenprocoumon;
• patients undergoing transplantation receiving cyclosporine, tacrolimus.

There was also no drug interaction with theophylline, caffeine, and ethanol.

Interaction with atazanavir and ritonavir (tablets) is possible.

How to take, course of use and dosage

of intravenous use of Kontrolok® is recommended in cases where oral use of the drug is not possible. The recommended dose is 40 mg/day.

For 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 Controlok ® iv. After that, the dose can 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 of Controlok®.

In the treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration):  the drug Controlok ® is prescribed at 80 mg / 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. It is possible to temporarily increase the daily dose to 160 mg of Controlok®.

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

The solution for intravenous use 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 cooking.

Overdose

To date, no overdose events have been observed as a result of the use of Controlok.

Doses up to 240 mg were administered intravenously for 2 minutes and were well tolerated.

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

Pantoprazole is not eliminated by hemodialysis.

Special instructions

Intravenous use is recommended only if oral use is not possible.

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

In the presence of any of the disturbing symptoms (e. g. significant unintended weight loss, recurrent vomiting, dysphagia, anemia, or melena) and in the case of suspected or present stomach ulcers, the possibility of malignancy should be excluded, as treatment with pantoprazole may reduce symptoms and delay the correct diagnosis.

If symptoms persist despite adequate treatment, then a further examination should be performed.

Do not increase the daily dose of pantoprazole 40 mg in elderly patients and people with impaired renal function.

In patients with severe hepatic insufficiency, the daily dose should be reduced to 20 mg of pantoprazole. In addition, liver enzymes should be monitored during therapy with Controlok® in these patients. If their level increases, treatment should be interrupted.

Before and after treatment, endoscopic monitoring is recommended to exclude malignancy, as treatment may mask the symptoms and delay the correct diagnosis.

Form of production

Powder for solution preparation

Storage conditions

At a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Pantoprazole

Conditions of release from pharmacies

By prescription

Dosage form

infusion solution