Pantoprazole Canon enteric-Soluble tablets 40mg, 28pcs

Composition

1 tablet enteric-soluble, film-coated,40 mg contains:

Active ingredient:

pantoprazole sodium sesquihydrate 45.14 mg, based on pantoprazole 40 mg;

excipients:

heavy magnesium hydroxycarbonate 15.06 mg,

macrogol (polyethylene glycol) 2.4 mg,

mannitol 126 mg,

calcium stearate 2.4 mg,

colloidal silicon dioxide 2 mg,

crospovidone 40 mg,

povidone K-30 7 mg;

film shell composition: Opadray transparent 4.8 mg (including: hypromellose (hydroxypropylmethylcellulose) 3.84 mg, macrogol (polyethylene glycol) 0.96 mg), Acrylic-Is green 17.2 mg (including: methacrylic acid and ethyl acrylate copolymer [1: 1] 11.352 mg, colloidal silicon dioxide 0.172 mg, sodium bicarbonate 0.172 mg, sodium lauryl sulfate 0.086 mg, iron yellow oxide 0.12 mg, indigo carmine dye 0.138 mg, diamond blue dye 0.052 mg, talcum powder 2.838 mg, titanium dioxide 2.27 mg). Triethyl citrate 2 mg

Pharmacological action

Pharmacotherapy group:

Means that reduces the secretion of gastric glands-proton pump inhibitor.

ATX code:  A02BC02

Pharmacological properties

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 Pantoprazole Canon, the antisecretory effect occurs in 1 hour and reaches a maximum in 2-4 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, pantoprazole has a higher chemical stability at neutral pH and a lower potential for interaction with the cytochrome P450-dependent liver oxidase system. Therefore, pantoprazole does not interact with many other common medications.

Pharmacokinetics

Suction

Pantoprazole is rapidly absorbed after oral use. The maximum concentration (Cmax) in blood plasma with oral use is reached after the first dose of 20 mg or 40 mg. On average, Cmax of 1.0-1.5 mcg / ml is reached after 2-2.5 hours for a dosage of 20 mg, and equal to 2.0 -3.0 mcg / ml – after 2.5 hours for a dosage of 40 mg. This indicator remains constant after repeated use of the drug. Absolute bioavailability is 77%. Concomitant use of pantoprazole with food does not affect the area under the pharmacokinetic curve “concentration-time” (AUC) and Cmax.

Distribution

Binding to plasma proteins is 98%. The volume of distribution is 0.15 l / kg, the clearance is 0.1 l / h/kg.

Metabolism

It is metabolized in the liver. The main metabolite in blood plasma and urine is desmethylpantoprazole conjugating with sulfate.

Deduction

The half-life (half-life) of pantoprazole is 1 hour, the metabolite-1.5 hours. 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 through the intestine.

Pharmacokinetics in different groups of patients

Age: A small increase in AUC and Cmax in the elderly is not clinically significant.

Renal insufficiency: When using pantoprazole in patients with impaired renal function (including patients on hemodialysis), no dose reduction is required. As in healthy patients, the drug is excreted fairly quickly and there is no accumulation.

Hepatic insufficiency: In patients with cirrhosis of the liver (Child-Pugh class A and B), the half-life increases to 3-6 hours when using pantoprazole at a dosage of 20 mg and to 7-9 hours when using pantoprazole at a dosage of 40 mg. The AUC value increases 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 with healthy patients.

Indications

• peptic ulcer of stomach and duodenum (in the acute phase), erosive gastritis (including those associated with nonsteroidal anti-inflammatory drugs (NSAIDs));
• the treatment of symptoms of gastroesophageal reflux disease mild symptoms (such as heartburn, nausea, acid regurgitation);
• syndrome zollingerellison;
• Helicobacter pylori eradication in combination with antibacterial agents.

Use during pregnancy and lactation

The drug Pantoprazole Canon can be used during pregnancy only if the benefit to the mother exceeds the possible potential risk to the fetus. Experimental studies have established that pantoprazole is excreted in breast milk, so if it is necessary to use the drug Pantoprazole Canon, breastfeeding should be discontinued.

Contraindications

• hypersensitivity to any component of the drug;
• dyspepsia neurotic origins;
• children up to age 18 years (safety and effectiveness in pediatric patients have not been established);
• malignant diseases of the gastrointestinal tract;
• concurrent use of atazanavir;
• eradication of Helicobacter pylori in patients with severe renal failure (creatinine clearance <20 ml/min);
• the period of breastfeeding.

With caution

• hepatic insufficiency;
• pregnancy;
• elderly age;
• in patients who have an increased risk of developing gastrointestinal complications and are receiving long-term nonsteroidal anti-inflammatory drugs as an anti-relapse treatment for gastric or duodenal ulcer at a dose of 20 mg.

Side effects

WHO classification of frequency of side effects:

• very often – >1/10 appointments (>>10%)
• often – from >1/100 to ><1/10 appointments (>1% and <1/10 appointments (>
• rare – from >1/1000 to <1/100 appointments (>0.1% and <1%)
• rare – from >1/10000 to <1/1000 appointments (>0.01% and <0.1%)
• very rarely <1/10000 appointments (<0.01%)
• frequency unknown – cannot be estimated from available data.

Disorders of the blood and lymphatic system: rarely-agranulocytosis; very rarely-leukopenia, thrombocytopenia, pancytopenia. Immune system disorders: very rare-anaphylactic reactions, including anaphylactic shock. Mental disorders: infrequently-sleep disorders; rarely-depression, hallucinations, disorientation, confusion, especially in patients predisposed to this, as well as an increase in these symptoms if patients have previously been observed. Nervous system disorders: often-headache; infrequently-dizziness; rarely-dysgeusia. Visual impairment: infrequently-visual impairment (blurred vision). Gastrointestinal disorders: often-upper abdominal pain, diarrhea, constipation, flatulence; infrequently-nausea/vomiting; rarely-dry mouth. Liver and biliary tract disorders: very rare-severe damage to the liver parenchyma, leading to jaundice with or without hepatic insufficiency. Skin and subcutaneous tissue disorders: infrequently-pruritus and skin rash; very rarely-urticaria, angioedema, malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, Lyell’s syndrome, photosensitization. Musculoskeletal and connective tissue disorders: rarely-arthralgia; very rarely-myalgia. Metabolic disorders: rarely-hyperlipidemia, changes in body weight; frequency unknown-hyponatremia, hypomagnesemia. Disorders of the urinary system: very rarely – interstitial nephritis. Genital and breast disorders: rarely-gynecomastia. General disorders: infrequently-weakness, fatigue and malaise; very rarely-peripheral edema, fever. Laboratory and instrumental data: rarely-increased bilirubin content; very rarely-increased activity of “liver” enzymes (aspartate aminotransaminase, gamma-glutamyltransferase), increased triglycerides.

Interaction

Concomitant use of pantoprazole may reduce the absorption of drugs whose bioavailability depends on the pH of the stomach environment (for example, iron salts, ketoconazole, atazanavir).

The absorption of ritonavir is also known to depend on pH. Therefore, pantoprazole should be used with caution in combination with ritonavir, because of the possible decrease in the bioavailability of ritonavir.

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

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

There are no data on the simultaneous interaction of pantoprazole with antacids. When used concomitantly with warfarin, the international normalized ratio (INR) may increase, and monitoring of this indicator is necessary. There was also no drug interaction with theophylline, caffeine, and ethanol.

How to take, course of use and dosage

Inside. The tablet should be swallowed whole, without chewing or breaking, washed down with a small amount of liquid, before meals, usually before breakfast. With a double dose, the second dose of the drug is recommended to be taken before dinner.

Peptic ulcer of the stomach and duodenum, erosive gastritis (including those associated with taking NSAIDs)

The recommended dose is 40-80 mg per 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

As a triple therapy, the following combinations are used::

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

2. Pantoprazole Canon 20-40 mg 2 times a day + metronidazole 500 mg 2 times a day + clarithromycin 500 mg 2 times a day. The course of treatment is 7-14 days.

3. Pantoprazole Canon 20-40 mg 2 times a day + amoxicillin 1000 mg 2 times a day + 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 in order to heal the ulcer. With a duodenal ulcer, Pantoprazole Canon can be extended from 1 to 3 weeks.

Patients with severe renal impairment (creatinine clearance

Treatment of mild GERD symptoms (such as heartburn, nausea, and acid belching)

The recommended dose of the drug is 20 mg / day. To achieve a positive trend in the elimination of symptoms, it may be necessary to take the drug for 2-3 days, but to completely eliminate the symptoms, it may be necessary to take the drug for 7 days. If the condition worsens during the first 3 days of treatment, it is recommended to consult a specialist. The drug should be discontinued immediately after symptoms disappear.

Zollinger-Ellison syndrome

The recommended dose is 40-80 mg per 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 activity of liver enzymes increases, the drug should be discontinued.

Elderly patients

No dose adjustment is required. However, elderly patients 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 Pantoprazole Canon 40 mg 2 times a day.

Patients with renal insufficiency

Patients with severe renal impairment (creatinine clearance For this reason, eradication therapy of Helicobacter pylori is not prescribed to such patients.

Do not take the drug Pantoprazole Canon for prevention purposes.

Overdose

To date, no overdose events have been observed as a result of the use of pantoprazole. Doses exceeding 240 mg intravenously were administered within 2 minutes and were well tolerated. However, in case of overdose and only in the presence of clinical manifestations, symptomatic and supportive treatment is provided. Hemodialysis is ineffective.

Special instructions

Liver enzyme activity in blood plasma should be regularly monitored when Pantoprazole Canon is used in patients with severe hepatic insufficiency, especially with prolonged use. If the activity of transaminases in blood plasma increases, treatment with the drug should be discontinued.

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

Pantoprazole Canon should be used with caution in elderly patients (over 65 years of age) with a history of gastric or duodenal ulcer, as well as bleeding from the upper gastrointestinal tract.

Before and after treatment, endoscopic monitoring is required to exclude the possibility of malignant diseases of the stomach and esophagus, since treatment with the drug.

Pantoprazole Canon can mask the symptoms and make it difficult to correctly diagnose.

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 during 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 effectively for 4 weeks should be evaluated.

When taking Pantoprazole Canon for a long time, patients need regular medical supervision.

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

You should pay attention to the fact that dizziness may develop during treatment, and therefore caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C.

Keep out of reach of children.

Shelf life

2 years

Active ingredient

Pantoprazole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Gastrointestinal infections caused by Helicobacter Pylori, Gastric and Duodenal Ulcers, Reflux Esophagitis, Heartburn, Gastritis