Pantoprazole Canon - instructions for use, dose, side effects, contraindications

Excipients: magnesium hydroxycarbonate heavy 7.53 mg, macrogol (polyethylene glycol) 1.2 mg, mannitol 63 mg, calcium stearate 1.2 mg, silicon dioxide colloid 1 mg, crospovidone 20 mg, povidone K-30 3.5 mg;

composition of film shell: Opadry Clear 2.4 mg (including: hypromellose (hydroxypropyl methylcellulose) 1.920 mg macrogol (polyethylene glycol) 0.48 mg) acryl-green 8.6 mg Of (including methacrylic acid-ethyl acrylate copolymer [1: 1 ] 5,676 mg, silicon dioxide colloid 0,086 mg, sodium hydrogen carbonate 0,086 mg, sodium lauryl sulfate 0.043 mg, iron oxide yellow 0.06 mg, dye indigocarmine 0.069 mg, brilliant blue dye 0.026 mg, talc 1.419 mg, titanium dioxide 1.135 mg). Triethyl citrate 1 mg.

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

active substance: pantoprazole sodium sesquihydrate 45.14 mg, calculated as pantoprazole 40 mg;

Excipients: magnesium hydroxycarbonate heavy 15.06 mg macrogol (polyethylene glycol) 2.4 mg, mainitol 126 mg, 2.4 mg calcium stearate, colloidal silicon dioxide 2 mg crospovidone 40 mg, povndon K-30 7 mg;

composition of film shell: Opadry Clear 4.8 mg (including: hypromellose (hydroxypropyl methylcellulose) 3.84 mg macrogol (polyethylene glycol) 0.96 mg) acryl-Green From 17.2 mg (including methacrylic acid-ethyl acrylate copolymer [1: 1 ] 11.352 mg, silicon dioxide colloid 0.172 mg, sodium hydrogen carbonate 0.172 mg, sodium lauryl sulfate 0.086 mg, iron oxide yellow 0.12 mg,indigo carmine dye 0.138 mg, brilliant blue dye 0.052 mg, talc 2.838 mg, titanium dioxide 2.27 mg). Triethyl citrate 2 mg.

Description:

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

Pharmacotherapeutic group:An agent that reduces the secretion of the glands of the stomach is a proton pump inhibitor.

ATX: & nbsp

A.02.B.C Proton pump inhibitors

A.02.B.C.02 Pantoprazole

Pharmacodynamics:

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

Antisecretory activity

After oral administration of the preparation Paitoprazole Canon antisecretory effect occurs after 1 hour and reaches a maximum after 2-4 hours. With 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 gastrointestinal tract. Secretory activity is normalized 3-4 days after the end of admission.

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

Pharmacokinetics:

Suction

Pantoprazole is rapidly absorbed after ingestion. The maximum concentration (C_max) in blood plasma for oral administration is achieved after the first dose of 20 mg or 40 mg. On the average, C_max, equal to 1,0 - 1.5 mcg / ml, achieved after 2-2.5 h for a dosage of 20 mg, and equal to 2.0 - 3,0 μg / 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 %. Simultaneous application of the panToprazole with food does not affect the area under the pharmacokinetic curve "concentration-time" (AUC) and C_max.

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

Metabolised in the liver. The main metabolite in the blood plasma and urine is desmethylpentoprazole, conjugating with sulfate.

Excretion

The half-life (T1/2) of pantoprazole is 1 hour, the metabolite is 1.5 hours.The main way of excretion is through the kidneys (about 80%) in the form of metabolites of pantoprazole, in a small amount is excreted through the intestine

Pharmacokinetics the different patient groups

Age: A slight increase in the indicator AUC and C_1ШХin the elderly is not clinically relevant.

Renal insufficiency: When pantoprazole is used in patients with impaired renal function (including patients on hemodialysis), a dose reduction is not required. As in healthy patients, the excretion of the drug occurs rather quickly and cumulation does not occur.

Liver failure: In patients with cirrhosis of the liver (classes A and B according to the Child-Pugh classification), the value of T1 / 2 increases to 3-6 hours with pantoprazole at a dosage of 20 mg and up to 7-9 hours with pantoprazole at a dosage of 40 mg. Index AUC increases 3-5 times (for a dosage of 20 mg) and 5-7 times (for a dosage of 40 mg). FROM_mOh Increases in 1,3 times (for a dosage of 20 mg) and in 1,5 times (for a dosage of 40 mg) in comparison with healthy patients.

Indications:

- Stomach ulcer and duodenal ulcer (in the phase of exacerbation), erosive gastritis (including associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs));

- treatment of gastroesophageal reflux symptomsdisease mild degree of severity (such as heartburn, nausea, acidic eructation);

- Zollinger-Ellison syndrome;

- eradication Helicobacter pylori in combination with antibacterial agents.

Contraindications:

- hypersensitivity to the components of the drug;

- dyspepsia of neurotic genesis;

- children under 18 years of age (safety and efficacy in pediatrics not established);

- malignant diseases of the gastrointestinal tract;

- simultaneous use with atazanavir;

- eradication Helicobacter pylori in patients with severe renal failure (creatinine clearance <20 mL / min);

- the period of breastfeeding.

Carefully:

- liver failure;

- bVariability

- elderly age;

- in patients who have an increased risk of complications from the gastrointestinal tract and long-term non-steroidal anti-inflammatory drugs as an anti-relapse treatment of peptic ulcer of the stomach or duodenum at a dose of 20 mg.

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.

In experimental studies it was established that pantoprazole excreted in breast milk, so if necessary, use Paitoprazole Canon breastfeeding should be discontinued.

Dosing and Administration:

Inside. The tablet should be swallowed whole, not chewing and not breaking, squeezed with a small amount of liquid, before meals, usually before breakfast. When taking twice a second dose of the drug is recommended before dinner.

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

The recommended dose is 40-80 mg per day. The course of treatment 2 weeks with exacerbation of duodenal ulcer and 4-8 weeks with exacerbation of gastric ulcer.

Anti-relapse treatment of peptic ulcer of the stomach and duodenum - 20 mg per day.

Eradikiaia Helicobacter pylori

As a triple therapy, the following combinations are used:

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

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

3. Pantoprazole The canon of 20-40 mg twice a day + amoxicillin 1000 mg twice a day + metronidazole 500 mg twice a day. The course of treatment is 7-14 days.

After the end of combination therapym drug Pantoprazole The canon can be continued to heal ulcers. With a duodenal ulcer, the drug Pantoprazole Canon can be extended from 1 to 3 weeks.

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

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

The recommended dose of the drug is 20 mg per day. For achievement 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 discontinued immediately after the symptoms disappear.

Zollinger-Ellison Syndrome

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

Elderly patients

Correction of the dose is not required. However, elderly patients should not exceed a daily dose of 40 mg. An exception is the use of combined antimicrobial therapy in relation to Helicobacter pylori, when elderly patients should use the drug Pantoprazole Canon 40 mg twice a day.

Patients with renal insufficiency

Patients with severe renal impairment (creatinine clearance <20 mL / min), or who are on hemodialysis should not exceed a daily dose of 40 mg. For this reason, eradication therapy Helicobacter pylori such patients are not assigned.

Do not take Pantoprazole Canon for prevention.

Side effects:

Classification of WHO frequency of development of side effects:

very often - ≥ 1/10 of appointments (> 10%)

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

infrequently - from ≥ 1/1000 to <1/100 of prescriptions (> 0.1% and <1%)

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

very rarely - <1/10000 prescriptions (<0.01%)

frequency is not known - can not be estimated based on available data

Violations from the blood and lymphatic system:

rarely - agranulocytosis;

rarely - leukopenia, thrombocytopenia, pancytopenia.

Immune system disorders:

rarely - anaphylactic reactions, including anaphylactic shock.

Disorders of the psyche:

infrequently - sleep disorders;

rarely - depression, hallucinations, disorientation, confusion, especially in patients who are predisposed to it, and the increase in these symptoms if they have previously been observed in patients.

Impaired nervous system:

often - headache;

infrequently - dizziness;

rarely- dysgeusia.

Impaired vision:

infrequently - visual impairment (blurred vision).

Disorders from the gastrointestinal tract:

often - pain in the upper abdomen, diarrhea, constipation, flatulence;

infrequently - nausea, vomiting;

rarely - dry mouth.

Disorders from the liver and bile ducts:

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

Disturbances from the skin and subcutaneous tissues:

infrequently - itching and skin rash;

rarely - urticaria, angioedema, malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, Lyell syndrome, photosensitivity.

Disturbances from the musculoskeletal and connective tissue:

rarely - arthralgia;

rarely - myalgia.

Disruption from the metabolism:

rarely - hyperlipidemia, changes in body weight;

frequency unknown - hyponatremia, hypomagnesemia.

Disorders from the urinary system:

rarely - interstitial nephritis.

Violations of the genitals and breast:

rarely - gynecomastia.

General disorders:

infrequently - weakness, fatigue and malaise;

rarely - peripheral edema, fever.

Laboratory and instrumental data:

rarely - Increased bilirubin content;

rarely - an increase in the activity of "hepatic" enzymes (aspartate aminotransaminase, gamma-glutamyl transferase), an increase in the content of triglycerides.

Overdose:

To date, no overdose has been observed as a result of the use of pantoprazole. Doses in excess of 240 mg intravenously were given within 2 minutes and were tolerated well.

However, in case of an overdose and only if there are clinical manifestations, symptomatic and supportive treatment is performed. Hemodialysis is ineffective.

Interaction:

The simultaneous use of pantoprazole can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (for example, iron salts, ketoconazole, atazanavir).

It is known that the absorption of ritonavir also depends on pH. Therefore, apply pantoprazole together with ritonavir should be taken with caution, 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 who take antibiotics (amoxicillin, clarithromycin);

- patients taking oral contraceptives;

- patients taking non-steroidal anti-inflammatory drugs drugs (diclofenac, phenazone, naproxen, piroxicam);

- patients with diseases of the endocrine system who receive glibenclamide, levothyroxine sodium;

- patients with anxiety and sleep disorders receiving diazepam;

- patients with epilepsy receiving carbamazepine and phenytoin;

- patients who have undergone transplantation ciclosporin, tacrolimus.

There are no data on the simultaneous interaction of pantoprazole with antacid agents.

With simultaneous application with warfarin, an international normalized relationship (INR) may increase, and monitoring of this indicator is necessary.

There was also a lack of drug interaction with theophylline, caffeine and ethanol.

Special instructions:

It is necessary to regularly monitor the activity of liver enzymes in the blood plasma when using the drug Pantoprazole Canon for patients with severe hepatic insufficiency, especially with prolonged use. When the activity of transaminases in the blood plasma increases, the drug should be discontinued.

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

It is necessary to use with caution the drug Pantoprazole Canon in elderly patients (over 65 years) who have a history of peptic ulcer diseasestomach or duodenal ulcers, and taiyu bleeding from the upper departments of the gastrointestinal tract.

Before and after treatment, endoscopic control is mandatory to exclude the possibility of malignant diseases of the stomach and esophagus, as treatment with Pantoprazole Canon can mask the symptoms and make it difficult to diagnose correctly.

The decrease in the acidity of gastric juice increases the number of bacteria in the stomach, leading to the development of gastrointestinal tract infections caused by Salmonella spp., and Campylobacter spp. Pantoprazole reduces the absorption of vitamin B12 due to hypo- and achlorhydria. This should be considered with prolonged therapy in patients with low body weight or with an increased risk of reductionabsorption of vitamin B12. Patients in whom treatment did not result in an effect within 4 weeks need to be examined.

With prolonged use of the drug Pantoprazole Canon patients need regular medical supervision.

Effect on the ability to drive transp. cf. and fur:

It should pay attention to the fact that during treatment, dizziness may develop, so you need to be careful when driving and taking other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:The tablets are film-soluble, film-coated 20 mg and 40 mg.

Packaging:

By 7, 10, 14 or 28 tablets into a contoured cell pack of a PVC film or a PVC / PVDC film or a PVC / PCTFE film and aluminum foil printed lacquered.

According to 1, 2, 4 contour cell packs of 7, 10 or 14 tablets or 1.2 contour packs of 28 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003024

Date of registration:04.06.2015

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pantoprazole Canon (Pantoprazole Canon)