Expiration date: 07/2025

Composition:

1 tablet is intestinal-soluble, film-coated, 20 mg contains:

active substance: pantoprazole sodium sesquihydrate 22, 57 mg, in terms of pantoprazole 20 mg;

excipients: heavy magnesium hydroxycarbonate 7, 53 mg, macrogol (polyethylene glycol) 1, 2 mg, mannitol 63 mg, calcium stearate 1, 2 mg, silicon colloidal dioxide 1 mg, crosspovidone 20 mg, povidone K-30 3, 5 mg;

the film composition of the shell: transparent Opadry 2, 4 mg (including: hypromellose (hydroxypropyl methylcellulose) 1, 920 mg, macrogol (polyethylene glycol) 0, 48 mg), Acrylic-green 8, 6 mg (including methacrylic acid and ethylacrylate copolymer [1:1] 5, 676 mg, silicon dioxide colloidal 0, 086 mg of sodium bicarbonate of 0 086 mg, sodium lauryl 0, 043 mg, iron oxide yellow 0, 06 mg, the dye Indigo Carmine 0, 069 mg, the dye brilliant blue 0, 026 mg, talc 1, 419 mg, titanium dioxide 1, 135 mg). Triethyl nitrate 1 mg.

1 tablet is intestinal-soluble, film-coated, 40 mg contains:

active substance: pantoprazole sodium sesquihydrate 45, 14 mg, equivalent to pantoprazole 40 mg;

excipients: heavy magnesium hydroxycarbonate 15, 06 mg, macrogol (polyethylene glycol) 2, 4 mg, mannitol 126 mg, calcium stearate 2, 4 mg, silicon colloidal dioxide 2 mg, crosspovidone 40 mg, povidone K-30 7 mg;

the film composition of the shell: transparent Opadry 4, 8 mg (including: hypromellose (hydroxypropyl methylcellulose) 3, 84 mg, macrogol (polyethylene glycol) 0, 96 mg), Acrylic-green 17, 2 mg (including methacrylic acid and ethylacrylate copolymer [1:1] 11, 352 mg, silicon dioxide colloidal 0, 172 mg of sodium bicarbonate 0, 172 mg sodium lauryl 0, 086 mg, iron oxide yellow 0, 12 mg dye Indigo Carmine 0, 138 mg, the dye brilliant blue 0, 052 mg, talc 2, 838 mg, titanium dioxide 2, 27 mg). Triethyl nitrate 2 mg.

Description: 

Round, biconvex tablets, film-coated light green or green with a bluish tinge of color. On the cross section-almost white.

Pharmacotherapeutic group: 

Means of lowering the secretion of the glands of the stomach – a proton pump inhibitor.

ATC code: A02BC02

Pharmacological action

Pharmacodynamics

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

Anti-secretory activity

After oral administration of the drug Pantoprazole Canon antisecretory effect occurs after 1 h and reaches a maximum of 2-4 h. when duodenal ulcer associated with Helicobacter pylori, decreased gastric secretion increases the sensitivity of microorganisms to antibiotics. Does not affect the motility of the gastrointestinal tract. Secretory activity is normalized after 3-4 days after the end of the reception.

Compared with other proton pump inhibitors, pantoprazole has greater chemical stability at neutral pH and less potential for interaction with the liver oxidase system dependent on cytochrome P450. Therefore, pantoprazole does not interact with many other common drugs.

Pharmacokinetics

Suction

Pantoprazole is rapidly absorbed after oral administration. The maximum concentration (Cmax) in plasma during oral administration is achieved after the first dose of 20 mg or 40 mg.on average, Cmax, equal to 1, 0 – 1, 5 mg/ml, is achieved after 2-2. 5 h for a dosage of 20 mg, and equal to 2, 0 – 3, 0 mg/ml – after 2, 5 h for a dosage of 40 mg. This figure remains constant after repeated use of the drug. Absolute bioavailability is 77 %. Simultaneous use of pantoprazole with food does not affect the area under the pharmacokinetic curve "concentration-time" (AUC) and Cmax.

Distribution

Plasma protein binding is 98 %. The volume of distribution is 0, 15 l / kg, clearance-0, 1 l / h / kg. 

Metabolism

Metabolized in the liver. The main metabolite in plasma and urine is desmethyldonepezil, conjugii sulfate.

Breeding

The elimination half-life (T1/2) of pantoprazole is 1 h metabolite – 1, 5 h. the Main route of excretion is via the kidneys (approximately 80 %) in the form of metabolites.omeprazole, in a small amount is excreted through the intestines.

Pharmacokinetics in different groups of patients

Age: a Small increase in the AUC and Smack of the elderly is not clinically significant.

Renal failure: when using pantoprazole in patients with impaired renal function (including patients on hemodialysis) dose reduction is not required. As in healthy patients, the excretion of the drug occurs quickly and cumulation is not happening.

Liver failure: in patients with liver cirrhosis (classes A and b classification child-Pugh) T1/2 value increases to 3-6 h when using pantoprazole in the dosage of 20 mg and up to 7-9 h when using pantoprazole in the dosage of 40 mg.AUC Indicator increases 3-5 times (for the dosage of 20 mg) and 5-7 times (for the dosage of 40 mg). Smowiliams 1, 3 times (for dose 20 mg) and 1, 5 times (for dose 40 mg) compared with healthy patients.

Indications for use

• gastric and duodenal ulcer (in the acute phase), erosive gastritis (including those associated with taking non-steroidal anti-inflammatory drugs (NSAIDs));
  
• treatment of symptoms of gastroesophageal reflux disease of mild severity (such as heartburn, nausea, sour burp);
  
• Zollinger-Ellison syndrome;
  
• Helicobacter pylori eradication in combination with antibacterial agents.
  

Contraindications

• hypersensitivity to the drug components;
  
• dyspepsia of neurotic origin;
  
• children under the age of 18 (safety and efficacy are not established in Pediatrics);
  
• malignant diseases of the gastrointestinal tract;
  
• concomitant use with atazanavir;
  
• Helicobacter pylori eradication in patients with severe renal failure (creatinine clearance <20 ml/min.);
  
• the period of breastfeeding.
  

With caution

• liver failure;
  
• pregnancy;
  
• old age;
  
• in patients with an increased risk of complications from the gastrointestinal tract and long-term receiving nonsteroidal anti-inflammatory drugs as an anti-relapse treatment of gastric ulcer or duodenal ulcer at a dose of 20 mg.
  

Use during pregnancy and breastfeeding.

The drug Pantoprazole Canon can be used during pregnancy only if the benefit to the mother exceeds the possible potential risk to the fetus.

In experimental studies found that pantoprazole is excreted in breast milk, therefore, if necessary, the drug Pantoprazole Canon breastfeeding should be discontinued. 

Dosage and administration

Inside. The tablet should be swallowed whole, without chewing or breaking, with a small amount of liquid, before eating, usually before Breakfast. When twice taking a second dose of the drug is recommended before dinner.

Gastric and duodenal ulcer, erosive gastritis (including those associated with the intake of NSAIDs)

The recommended dose of 40-80 mg per day. The course of treatment 2 weeks during exacerbation of peptic ulcer disease duodenal ulcer for 4-8 weeks and during exacerbation of peptic ulcer of the stomach.

Anti-relapse treatment of gastric ulcer and duodenal ulcer – 20 mg per day.

Eradication Of Helicobacterpylori

As a triple therapy, the following combinations are used:

1.  Pantoprazole, Kanono 20-40 mg 2 times per day + amoxicillin for 1000 mg 2 times per day + clarithromycin on 500 mg 2 times a day. The course of treatment is 7-14 days.

2.  Pantoprazole, Kanono 20-40 mg 2 times daily + metronidazole 500 mg 2 times per day + clarithromycin on 500 mg 2 times a day. The course of treatment is 7-14 days.

3. Pantoprazole, Kanono 20-40 mg 2 times per day + amoxicillin for 1000 mg 2 times daily + metronidazole 500 mg 2 times a day. The course of treatment is 7-14 days.

After the end of combination therapy, the drug Pantoprazole Canon can be continued for the purpose of healing the ulcer. In duodenal ulcer administration of the drug Pantoprazole Canon can be extended from 1 to 3 weeks.

Patients with severe renal impairment (creatinine clearance <20 ml / min), or hemodialysis eradication therapy Helicobacter pylori such patients are not assigned.

Treatment of symptoms of gastroesophageal reflux disease of mild severity (such as heartburn, nausea, sour burp)

The recommended dose is 20 mg per day. To achieve positive dynamics in the elimination of symptoms may require taking the drug for 2-3 days, but to completely eliminate the symptoms may require taking the drug for 7 days. If the condition worsens during the first 3 days of treatment, a specialist consultation is recommended. The drug should be stopped immediately after the symptoms disappear.

Zollinger-Ellison Syndrome

The recommended dose is 40-80 mg per day. In patients with severe hepatic impairment dose should be reduced to 40 mg 1 every 2 days. In this case, it is necessary to control the biochemical parameters of the blood. When increasing the activity of liver enzymes should stop the use of the drug.

Elderly patient

Dose adjustment is not required. However, elderly patients should not exceed the daily dose of 40 mg. the Exception is the use of combination antimicrobial therapy against Helicobacter pylori, when elderly patients should use the drug Pantoprazole Canon 40 mg 2 times a day.

Patients with renal insufficiency

Patients with severe renal dysfunction (creatinine clearance <20 ml/min) or on hemodialysis should not exceed the daily dose of 40 mg. For this reason, eradication therapy of Helicobacter pylori in such patients is not assigned.

Do not take the drug Pantoprazole Canon for prevention.

Side effect

Who classification of incidence of side effects:

very often - ?1/10 appointments (>10%)

often from ?1/100 to < 1/10 appointments (>1% and <10%)

infrequently-from ?1/1000 to <1/100 appointments (>0.1% and <1%)

rarely from ?1/10000 to <1/1000 appointments (>0.01% and <0.1%)

very rare - <1/10000 appointments (<0.01%)

frequency not known - cannot be estimated from available data

Disorders of the blood and lymphatic system:

rarely-agranulocytosis;

very rarely – leukopenia, thrombocytopenia, pancytopenia.

Immune system disorders:

very rarely-anaphylactic reactions, including anaphylactic shock.

Mental disorders:

infrequent-sleep disorders;

rarely-depression, hallucinations, disorientation, confusion, especially in patients predisposed to this, as well as the strengthening of these symptoms if the patients they were previously observed.

Disorders of the nervous system:

often - headache;

infrequently-dizziness;

rarely dysgeusia.

Violation by the organ of vision:

rarely – visual disturbances (blurred vision).

Disorders of the gastrointestinal tract:

often-upper abdominal pain, diarrhea, constipation, flatulence;

infrequently-nausea/vomiting;

rarely-dry mouth.

Disorders of the liver and biliary tract:

very rarely-severe damage to the liver parenchyma, leading to jaundice with or without liver failure.

Skin and subcutaneous tissue disorders:

infrequently-itching and skin rash;

very rarely-urticaria, angioedema, malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, Lyell's syndrome, photosensitization.

Disorders of the musculoskeletal and connective tissue:

rarely-arthralgia;

very rarely – myalgia.

Metabolic disorders:

rarely-hyperlipidemia, changes in body weight;

the frequency is unknown-hyponatremia, hypomagnesemia.

Disorders of the urinary system:

very rarely – interstitial nephritis.

Violations of the genital organs and breast:

rarely-gynecomastia.

Common disorders:

infrequently-weakness, fatigue and malaise;

very rarely – peripheral edema, fever.

Laboratory and instrumental data:

rarely-increasing the content of bilirubin;

very rarely-increased activity of "hepatic" enzymes (aspartate aminotransaminase, gamma-glutamyltransferase), increased triglycerides.

Overdose

Until now, the phenomena of overdose as a result of the use of pantoprazol have not been marked. Doses greater than 240 mg intravenous were administered over 2 minutes and were well tolerated.

However, in the case of overdose and only in the presence of clinical manifestations, symptomatic and supportive treatment is carried out. Hemodialysis is ineffective.

Interaction with other drugs

Concomitant use of pantoprazole may reduce the absorption of drugs, the bioavailability of which depends on the pH of the stomach (eg, iron salts, ketoconazole, atazanavir).

It is known that the absorption of ritonavir also depends on the pH. Therefore, the use of pantoprazole in conjunction with ritonavir should be cautious, because of the possible reduction of the bioavailability of ritonavir.

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

• patients with diseases of the cardiovascular system, taking cardiac glycosides( digoxin), "slow" calcium channel blockers (nifedipine), beta-blockers (metoprolol);
  
• patients with diseases of the gastrointestinal tract, taking antibiotics (amoxicillin, clarithromycin);
  
• patients taking oral contraceptives;
  
• patients taking non-steroidal anti-inflammatory drugs (diclofenac, phenazone, naproxen, piroxicam);
  
• patients with diseases of the endocrine system, taking glibenclamide, levothyroxine sodium;
  
• patients with anxiety and sleep disorders taking diazepam;
  
• patients with epilepsy taking carbamazepine and phenytoin;
  
• patients undergoing transplantation, taking cyclosporine, tacrolimus.
  

There are no data on the simultaneous interaction of pantoprazole with antacids.With simultaneous use of warfarin can increase the international normalized ratio (INR), it is necessary to monitor this indicator.The absence of drug interaction with theophylline, caffeine and ethanol was also noted.

Special instruction

It is necessary to regularly monitor the activity of liver enzymes in blood plasma when using Pantoprazole Canon in patients with severe liver failure, especially with long-term use. With increased activity of transaminases in blood plasma treatment should be discontinued.

In patients with an increased risk of complications from the gastrointestinal tract and receiving long-term nonsteroidal anti-inflammatory drugs, the drug Pantoprazole Canon in a dose of 20 mg for the prevention of gastric ulcer and duodenal ulcer should be used with caution.

It is necessary to use with caution the drug Pantoprazole Canon in elderly patients (over 65 years), with a history of gastric ulcer or duodenal ulcer, as well as bleeding from the upper gastrointestinal tract.

Before and after treatment, endoscopic control is required to exclude the possibility of malignant diseases of the stomach and esophagus, since treatment with Pantoprazole Canon can mask symptoms and complicate the correct diagnosis.

Lowering the acidity of gastric juice increases the number of bacteria in the stomach, leading to the development of infectious diseases of the gastrointestinal tract caused by Salmonella spp., and Campylobacter spp.

Pantoprazole reduces the absorption of vitamin B12 due to Hypo - and achlorhydria. This should be taken into account in long-term therapy in patients with low body weight or with an increased risk of decreased absorption of vitamin B12.

Patients who have not been treated for 4 weeks need to be examined.

With long-term use of the drug Pantoprazole Canon, patients need regular medical supervision.

Impact on the ability to drive and engage in other potentially hazardous activities

It should be noted that during treatment may develop dizziness, and therefore need to be careful when driving and doing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.