Controlock, 40 mg 14 pcs

Controlok 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 administration of 20 mg of Controlock^® antisecretory effect occurs after 1 hour and reaches a maximum after 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.

Pharmacokinetics

Pantoprazole is rapidly absorbed after oral administration. C_max in plasma with oral administration is reached after the first dose of 20 or 40 mg. On average, C_max equal to 1-1.5 mcg/ml is reached after 2-2.5 h for 20 mg doses and 2.0-3.0 mcg/ml after 2.5 h for 40 mg doses. This value remains constant after multiple uses of this drug.

V_d is 0.15 L/kg, clearance is 0.1 L/h/kg.

T_1/2 is 1 hour.

The pharmacokinetics are the same after both single and multiple applications of the drug.

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

The absolute bioavailability of pantoprazole tablets is 77%. Their concomitant use with food has no effect on the AUC and C_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 does not cumulate.

In patients with cirrhosis (Child-Pugh grades A and B), the T_1/2 is increased to 3-6 h when pantoprazole is used at 20 mg and to 7-9 h when pantoprazole is used at 40 mg. AUC increases 3-5-fold (for 20 mg dosage) and 5-7-fold (for 40 mg dosage). C_max is increased 1.3-fold (for 20 mg dosage) and 1.5-fold (for 40 mg dosage) compared to healthy patients. Slight increases in AUC and C_max in the elderly are not clinically significant.

Indications

Active ingredient

Composition

1 tablet contains:

Active ingredients:

Pantoprazole sodium sesquihydrate22.57 mg (corresponding to 20 mg of pantoprazole);

pantoprazole sodium sesquihydrate45.1 mg (corresponding to 40 mg of pantoprazole);

Excipients:

Sodium carbonate anhydrous;

Mannitol;

Crospovidone;

povidone K90;

calcium stearate;

purified water;

Shell:

Hypromellose 2910; povidone K25; titanium dioxide (E171); iron oxide yellow (E172); propylene glycol; eudragit L 30D-55 (methacrylic acid and ethyl acrylate copolymer, polysorbate 80, sodium lauryl sulfate); triethylcitrate.

How to take, the dosage

Orally with liquid and swallowed whole (tablets should not be crushed or dissolved).

Gastric and duodenal ulcer, erosive gastritis (including those associated with taking NSAIDs): 40-80 mg/day. The course of treatment is 2 weeks in case of duodenal ulcer exacerbation and 4-8 weeks – in case of gastric ulcer exacerbation. Antiretroviral treatment of gastric and duodenal ulcer – 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. Antiretroviral treatment – 20 mg/day.

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

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

In indications requiring once daily administration, Controlock® should be taken in the morning. Neither time of day nor food intake has been found to affect the activity of the drug, but the recommended time of taking Contrololok®® tablets promotes better patient adherence.

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

Before starting treatment with Controlock®, the presence of a malignancy should be excluded because the drug can mask symptoms and delay a 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, no overdose has been observed with 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 increase in side effects) symptomatic and supportive treatment is given.

Pantoprazole is not excreted by hemodialysis.

Similarities