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

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, penetration (for solution for intravenous administration).

Pharmacological effect

Controloc 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 administration of 20 mg of the drug Controloc®, the antisecretory effect occurs within 1 hour and reaches a maximum after 2–4 hours. With intravenous administration of 80 mg, the antisecretory effect reaches a maximum within 1 hour and lasts 24 hours. In case of duodenal ulcer associated with Helicobacter pylori, a decrease in gastric secretion increases the sensitivity of microorganisms to antibiotics. Does not affect gastrointestinal motility. Secretory activity returns to normal 3–4 days after the end of administration.

Compared to other proton pump inhibitors, Controloc® has greater chemical stability at neutral pH, and a lower potential for interaction with the liver oxidase system, which is dependent on cytochrome P450. Therefore, Controloc does not interact with many other common drugs.

Special instructions

IV use is recommended only if oral administration is not possible.

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

In the presence of any of the warning signs (eg significant unintentional weight loss, recurrent vomiting, dysphagia, anemia or melena) and if a gastric ulcer is suspected or present, the possibility of malignancy should be excluded, because Treatment with pantoprazole 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 or those with impaired renal function.

In persons with severe hepatic impairment, the daily dose should be reduced to 20 mg pantoprazole. In addition, liver enzymes should be monitored in such patients during therapy with Controloc®. If their level increases, treatment should be interrupted.

Before and after treatment, endoscopic monitoring is recommended to exclude malignant neoplasms, because treatment may mask symptoms and delay correct diagnosis.

Active ingredient

Pantoprazole

Composition

1 bottle contains:

Active substance:

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

Excipients:

disodium edetate – 1 mg;

sodium hydroxide – 0.24 mg.

Pregnancy

Controloc 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: pain in the upper abdomen, diarrhea, constipation, flatulence; headache.

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

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

Very rare: leukopenia, thrombocytopenia; thrombophlebitis at the injection site (powder for preparing a solution for intravenous 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’s syndrome.

Interaction

The simultaneous use of Controloc® may reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (for example, iron salts, ketoconazole).

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

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

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

Possible interaction with atazanavir and ritonavir (tablets).

Overdose

To date, no overdose phenomena have been observed as a result of using the drug Controloc.

Doses up to 240 mg were administered intravenously over 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.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf life

3 years.

Manufacturer

Takeda GmbH, Germany