Controlock, pills 40mg, 14pcs

Composition

1 tablet contains:

Active ingredients:

pantoprazole sodium sesquihydrate 22.57 mg (corresponds to 20 mg of pantoprazole);

pantoprazole sodium sesquihydrate 45.1 mg (corresponds to 40 mg of pantoprazole);

Auxiliary substances:

sodium carbonate anhydrous;

mannitol;

crospovidone;

povidone K 90;

calcium stearate;

purified water;

Shell:

hypromellose 2910; povidone K 25; titanium dioxide (E 171); iron oxide yellow (E 172); propylene glycol; eudragite L 30D-55 (methacrylic acid and ethyl acrylate copolymer, polysorbate 80, sodium lauryl sulfate); triethyl citrate.

Pharmacological action

Kontrolok is a proton pump inhibitor.

Pharmacodynamics

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.

Pharmacokinetics

Pantoprazole is rapidly absorbed after oral use. _Cmax in blood plasma with oral use is reached after the first dose of 20 or 40 mg. On average, _cmaxof 1-1.5 mcg / ml is reached after 2-2.5 hours for a dosage of 20 mg and 2.0–3.0 mcg/ml — after 2.5 hours for a dosage of 40 mg. This indicator remains constant after repeated use of this drug.

Vd is 0.15 l / kg, clearance is 0.1 l / h/kg.

T_1/2-1 h

. Pharmacokinetics are the same after both single and repeated use of the drug.

The binding of pantoprazole to plasma proteins is 98%. It is metabolized in the liver. The main route of elimination is through the kidneys (about 80%) in the form of metabolites of pantoprazole, in a small amount it is excreted in the faeces. The main metabolite in blood plasma and urine is desmethylpantoprazole conjugating with sulfate.

The absolute bioavailability of pantoprazole tablets is 77%. Concomitant use with food does not affect the AUC and With_max.

When using pantoprazole in patients with limited renal function (including patients on hemodialysis), no dose reduction is required. As in healthy patients, the T_1/2 of pantoprazole is short. Only a very small portion of the drug is dialyzed. It is not accumulated.

In patients with liver cirrhosis (classes A and b according to the classification of child-Pugh) T_1/2 increased to 3-6 hours when using pantoprazole dosage 20 mg and up to 7-9 hours upon application of pantoprazole at a dosage of 40 mg AUC is increased by 3-5 times (for a dosage of 20 mg) and 5-7 times (for a dosage of 40 mg). _Cmax increases by 1.3 times (for a dosage of 20 mg) and 1.5 times (for a dosage of 40 mg) compared to healthy patients. Slight increase in AUC and _{Cmax in the}elderly is not clinically significant.

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).

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

Inside, wash down with liquid and swallow whole (tablets can not be crushed or dissolved).

Peptic ulcer of the stomach and duodenum, erosive gastritis (including those associated with taking NSAIDs):  40-80 mg/day. The course of treatment is 2 weeks for exacerbation of duodenal ulcer and 4-8 weeks for exacerbation of gastric ulcer. Anti-relapse treatment of gastric and duodenal ulcers-20 mg/day.

Eradication of Helicobacter pylori. The following combinations are recommended:

The course of treatment is 7-14 days.

Reflux esophagitis:  20-40 mg/day. The course of treatment is 4-8 weeks. Anti-relapse treatment — 20 mg/day.

Zollinger-Ellison syndrome:  40-80 mg/day. In patients with severe hepatic impairment, the dose should be reduced to 40 mg once every 2 days. In this case, it is necessary to monitor the biochemical parameters of the blood. If the level of liver enzymes increases, the drug should be discontinued.

Elderly patients, as well as patients with impaired renal function, should not exceed the daily dose of 40 mg. An exception is the use of combined antimicrobial therapy against Helicobacter pylori, when elderly patients should also use the drug Controlok® 40 mg 2 times a day.

For indications that require taking the drug 1 time a day, the drug Controlok® should be taken in the morning. It was found that neither the time of day nor food intake affects the activity of the drug, but the recommended time for taking Controlok®tablets promotes better patient compliance with the treatment regimen.

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

Before starting treatment with Kontrolok®, the presence of a malignant neoplasm should be excluded, since the drug can mask symptoms and delay the correct diagnosis.

Form of production

Coated tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Pantoprazole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets