Controloc powder for solution preparation bottle 40mg №1

Proton pump inhibitor (H + -K + -ATP-ase).
Blocks the final stage of secretion of hydrochloric acid, reducing basal and stimulated secretion, regardless of the nature of the stimulus.
After ingestion of 20 mg of the drug, Controloc, the antisecretory effect occurs after 1 hour and reaches a maximum after 2-4 hours. With an 80 mg injection, the antisecretory effect of pantoprazole reaches a maximum for 1 hour and lasts 24 hours.
In duodenal ulcer associated with Helicobacter pylori, a decrease in gastric secretion increases the sensitivity of microorganisms to antibiotics. Does not affect the motility of the digestive tract. Secretory activity is normalized 3-4 days after the end of the application.
Compared to other proton pump inhibitors, Controloc has greater chemical stability at neutral pH, and less potential for interaction with the liver oxidase system, dependent on cytochrome P450. Therefore, Controloc does not interact with many other common drugs.

Pharmacokinetics

The pharmacokinetics are the same after single, and after repeated use of the drug.
Suction
After oral administration, pantoprazole is rapidly absorbed from the gastrointestinal tract. Cmax in oral blood plasma is achieved already after the first dose of 20 mg or 40 mg. On average, Cmax = 1.0-1.5 mcg / ml is achieved in 2-2.5 hours for a dose of 20 mg and 2.0-3.0 mcg / ml - in 2.5 hours for a dose of 40 mg. This indicator remains constant after repeated use of this drug. Absolute bioavailability of pantoprazole pills - 77%. The simultaneous use of pantoprazole pills with food does not affect the AUC and Cmax.
In the dose range from 10 to 80 mg, the kinetic direct concentration of pantoprazole in the blood plasma has a linear relationship both after oral administration and after intravenous administration.
Distribution
The binding of pantoprazole to plasma proteins is 98%. Vd is 0.15 l / kg, clearance is 0.1 l / h / kg.
Metabolism
Metabolized in the liver. The main metabolite in the blood plasma and urine is desmethylpanthoprazole, conjugated with sulfate.
Removal
The main route of excretion is with the urine (about 80%) in the form of pantoprazole metabolites, in a small amount is excreted in the feces. T1 / 2 preparation -1 h, T1 / 2 metabolite - about 1.5 h. Several cases of delayed elimination were observed (when using the solution for intravenous administration).
Pharmacokinetics in special clinical situations
When using pantoprazole in patients with limited kidney function (including patients on hemodialysis), no dose reduction is required. As in healthy patients, T1 / 2 pantoprazole is short. Only a very small portion of the drug is dialyzed. Although the T1 / 2 of the main metabolite slows down (2-3 hours), excretion proceeds rather quickly and does not cumulate.
In patients with cirrhosis of the liver (classes A, B according to Child-Pugh classification), the T1 / 2 value increases to 7-9 hours with the use of the solution for intravenous administration, up to 3-6 hours (for a dose of 20 mg) and up to 7 9 hours (for a dose of 40 mg) with the use of Controloc tablets. When applying the solution for intravenous administration, the AUC index increases by 5–7 times, and when pills are used, Controloc increases by 3-5 times (for a dose of 20 mg) and by 5-7 times (for a dose of 40 mg). Compared to healthy patients, when applying the solution for intravenous administration, Cmax increases 1.5 times, and when using Kontrol tablets, it increases 1.3 times (for a dose of 20 mg) and 1.5 times (for a dose of 40 mg).
A slight increase in AUC and Cmax in the elderly is not clinically significant.

Indications and usage

- gastric ulcer and duodenal ulcer (in acute phase), erosive gastritis (including those associated with the intake of 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).

Adverse reactions

When using Controloc in accordance with the indications and in the recommended doses, side effects are extremely rare.
Typical (> 1/100, <1/10): pain in the upper abdomen, diarrhea, constipation, flatulence; headache.
Not typical (> 1/1000, <1/100): nausea, vomiting; dizziness, blurred vision (blurred vision); allergic reactions (including itching, skin rash).
Rare (> 1/10000, 1000): dry mouth, arthralgia, depression, hallucinations, disorientation and confusion, (especially in patients predisposed to this), as well as an increase in these symptoms if they were previously observed in patients.
Very rare (<1/10000, including individual cases): leukopenia, thrombocytopenia, thrombophlebitis at the injection site (for solution for intravenous administration), peripheral edema, hepatocellular failure, leading to jaundice with / without liver failure; Anaphylactic reactions (including anaphylactic shock), elevated liver enzymes (transaminases, glutamyltranspeptidases), increased triglycerides, increased body temperature, myalgia, interstitial nephritis, urticaria, angioedema, Stevens-Johnson syndrome, erythema polymorphism, angioedema, erythema, erythema, erythema, erythema, erection.

Contraindications

- dyspepsia neurotic Genesis (for tablets, enteric-coated);
- hypersensitivity to the drug.
With caution should use the drug for liver failure, pregnancy, during lactation.
There is no data on the clinical use of the drug Controloc in pediatric practice.

Use during pregnancy and lactation

Controloc should be used with caution during pregnancy and lactation.

Application for violations of the liver

With caution should use the drug for liver failure.
In patients with severe hepatic impairment, the daily dose should be reduced to 20 mg pantoprazole. In addition, in such patients during the treatment with Kondrolok, it is necessary to control liver enzymes. In the case of increasing their level of treatment should be interrupted.

Application for violations of kidney function

You should not increase the daily dose of pantoprazole 40 mg in patients with impaired renal function, as well as elderly patients.

Special notes

I / V is recommended only if oral administration is not possible.
The use of pantoprazole is not indicated for the treatment of pulmonary gastrointestinal complaints, such as dyspepsia of neurogenic origin (for solution for iv administration).
Before and after treatment, in the presence of any of the alarming symptoms (includingsignificant unintended weight loss, intermittent vomiting, dysphagia, anemia, melena) and in case of suspicion or the presence of a stomach ulcer, endoscopic control is recommended to rule out malignant neoplasms, since treatment can mask the symptoms and delay the correct diagnosis.
If symptoms persist despite adequate treatment, further examination should be carried out.
You should not increase the daily dose of pantoprazole 40 mg in patients with impaired renal function, as well as in elderly patients (for solution for intravenous administration).
In patients with severe hepatic impairment, the daily dose should be reduced to 20 mg pantoprazole. In addition, in such patients during the treatment with Kondrolok, it is necessary to control liver enzymes. In the case of an increase in their level, treatment should be interrupted (for the solution for intravenous administration).

Overdosage

To date, the effects of overdose as a result of the use of the drug Controloc have been noted. Doses up to 240 mg were administered iv for 2 min and were well tolerated. However, in the case of an overdose and only in the presence of clinical manifestations (possible increased side effects) symptomatic and supportive treatment is carried out. Pantoprazole is not excreted by hemodialysis.

Drug interaction

The simultaneous use of Controloc can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (including iron salts, Ketoconazole, atazanavir, ritonavir).
Controloc can be assigned without risk of drug interactions to patients with diseases of the cardiovascular system, receiving cardiac glycosides (digoxin), blockers of "slow" Calcium channels (nifedipine), beta-blockers (metoprolol); patients with gastrointestinal diseases taking antacids, antibiotics (amoxicillin, clarithromycin); patients taking oral contraceptives; patients taking NSAIDs (diclofenac, phenazone, Naproxen, piroxicam); patients with endocrine diseases taking glibenclamide, levothyroxine; patients with anxiety and sleep disorders taking diazepam; epilepsy patients taking Carbamazepine and phenytoin; patients taking indirect anticoagulants,such as Warfarin and fenprokumon, patients undergoing transplantation, taking cyclosporine, tacrolimus.
The absence of drug interactions with theophylline, caffeine and ethanol was also noted.

Pharmacy sales terms

The drug is available on prescription.

Powder for preparing a solution for intravenous injection should be stored in a dark place at a temperature not exceeding 25 ° C. Shelf life - 2 years.