Composition, form of production and packaging
? The tablets covered with an enteric coating , oval, biconvex, covered with a film coat of yellow color, with a core from white to almost white; on one side of the tablet brown ink is printed "P20".
1 tab.
pantoprazole sodium sesquihydrate 22.57 mg,
which corresponds to the content of pantoprazole 20 mg
Excipients: sodium carbonate anhydrous - 5 mg, mannitol - 21.33 mg, crospovidone - 25 mg, povidone K90 - 2 mg, calcium stearate - 1.6 mg, purified water - 4.5 mg.
The composition of the coating: hypromellose 2910 - 11.88 mg, povidone K25 - 0.24 mg, titanium dioxide (E171) 0.21 mg, iron dye oxide yellow (E172) 0.02 mg, propylene glycol 2.66 mg, eudragit L 30 D 55 * 8.18 mg, triethyl citrate - 0.82 mg.
* The composition of the dispersion Eudragit L 30D-55: eudragit L 30D-55 (methacrylic acid and ethyl acrylate copolymer [1: 1]) - 7.94 mg, polysorbate 80 - 0.18 mg, sodium lauryl sulfate - 0.06 mg.
The composition of brown Opacode ink S-1-16530 for labeling on tablets: shellac (0.036 mg, iron oxide red oxide (E172) 0.009 mg, ferric iron oxide black (E172) 0.009 mg, iron oxide pigment yellow E172) - 0.0009 mg, ammonia solution concentrated 25% - 0.001 mg.
7 pcs. - blisters (1) - cardboard folding covers (1) - cardboard packs.
14 pcs. - blisters (1) - packs of cardboard.
The tablets covered with an enteric coating , oval, biconvex, covered with a film coat of yellow color, with a core from white to almost white; on one side of the tablet brown ink is printed "P40".
1 tab.
pantoprazole sodium sesquihydrate 45.1 mg,
which corresponds to the content of pantoprazole 40 mg
Excipients: sodium carbonate anhydrous - 10 mg, mannitol - 42.7 mg, crospovidone - 50 mg, povidone K90 - 4 mg, calcium stearate - 3.2 mg, purified water - 9 mg.
The composition of the membrane: hypromellose 2910-19 mg, povidone K25 0.38 mg, titanium dioxide (E171) 0.34 mg, iron dye oxide yellow (E172) 0.03 mg, propylene glycol 4.25 mg, eudragit L 30 D 55 * 14.56 mg, triethyl citrate - 1.45 mg.
* Eudragit L 30D-55 dispersion composition: eudragit L 30D-55 (methacrylic acid and ethyl acrylate copolymer [1: 1]) - 14.13 mg, polysorbate 80 - 0.33 mg, sodium lauryl sulfate 0.1 mg.
The composition of brown Opacode ink S-1-16530 for labeling on tablets: shellac (0.036 mg, iron oxide red oxide (E172) 0.009 mg, ferric iron oxide black (E172) 0.009 mg, iron oxide pigment yellow E172) - 0.0009 mg, ammonia solution concentrated 25% - 0.001 mg.
7 pcs. - blisters (1) - cardboard folding covers (1) - cardboard packs.
7 pcs. - blisters (1) - covers cardboard folding (4) - packs cardboard.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
PHARMACHOLOGIC EFFECT
Proton pump inhibitor (H + -K + -ATPase). It blocks the final stage of hydrochloric acid secretion, reducing basal and stimulated secretion, regardless of the nature of the stimulus.
Antisecretory activity. After ingestion of the drug Controlul В® in a dose of 20 mg, the decrease in gastric juice secretion by 24% occurs 2.5-3.5 hours and 26% after 24.5-25.5 hours. After taking 1 time / day for 7 days, antisecretory activity rises to 56% through 2.5-3.5 h and up to 50% after 24.5-25.5 h.
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 gastrointestinal tract. Secretory activity is normalized 3-4 days after the end of the application.
Compared to other inhibitors of the proton pump Controll В® has a great chemical stability at neutral pH and a lower interaction potential with the liver oxidase system dependent on cytochrome P450. Therefore, there was no clinically significant interaction between the Controll В® preparation and many other drugs.
PHARMACOKINETICS
Pharmacokinetics is the same as after a single, and after repeated use of the drug.
Suction
Pantoprazole is rapidly absorbed after ingestion. C max in blood plasma for oral administration is achieved after the first dose of 20 mg or 40 mg. On average, Cmax is 1.0-1.5 Ојg / ml and is achieved after 2-2.5 hours at a dose of 20 mg and 2.0-3.0 Ојg / ml in 2.5 hours at a dose of 40 mg. This indicator remains constant after repeated use of this drug. Absolute bioavailability of pantoprazole tablets is 77%. The simultaneous use of pantoprazole tablets with food does not affect AUC and C max .
Distribution
The binding of pantoprazole to plasma proteins is 98%. V d is 0.15 l / kg.
Metabolism
Metabolised in the liver. The main metabolite in the blood plasma and in urine is desmethylpentoprazole, conjugating with sulfate.
Excretion
T 1/2 of the drug - 1 hour. Clearance - 0.1 l / h / kg. 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 in special clinical cases
When pantoprazole is used in patients with limited renal function (including patients on hemodialysis), dose reduction is not required. As in healthy patients, T 1/2 ofpantoprazole is short. Only a very small part of the drug is dialyzed. Cumulation does not occur.
In patients with cirrhosis of the liver (classes A, B and C according to the Child-Pugh classification) the value of T 1/2 increases to 3-6 hours at a dose of 20 mg and up to 7-9 hours at a dose of 40 mg. The AUC is increased 3-5 times (for a dose of 20 mg) and 5-7 times (for a dose of 40 mg).
Cmax increases 1.3 times (for a dose of 20 mg) and 1.5 times (for a dose of 40 mg) compared to healthy patients.
A slight increase in AUC and C max in elderly people is not clinically significant.
INDICATIONS
For tablets of 20 mg
- Treatment of symptoms of gastroesophageal reflux disease of mild severity (such as heartburn, nausea, acidic eructation) in adults.
For tablets 40 mg
- peptic ulcer of the stomach and duodenum (in the phase of exacerbation), erosive gastritis (including associated with the intake of NSAIDs);
- Zollinger-Ellison syndrome;
- eradication of Helicobacter pylori in combination with antibacterial agents.
DOSING MODE
Controllers В® are taken orally before meals, without chewing or grinding, with plenty of liquid.
Tablets 20 mg
For the treatment of symptoms of gastroesophageal reflux disease of mild severity (such as heartburn, nausea, acidic eructation) in adults prescribe Controller В® at 20 mg / day. To achieve positive dynamics in the removal 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. If there is no positive dynamics during 2 weeks of continuous intake of the drug, the patient should consult a physician.
Tablets 40 mg
When treating peptic ulcer of stomach and duodenum, erosive gastritis (including those associated with the use of NSAIDs), the drug is prescribed in a dose of 40-80 mg / day.
The course of treatment is 2 weeks with exacerbation of duodenal ulcer and 4-8 weeks with peptic ulcer exacerbation. Anti-relapse treatment of peptic ulcer of the stomach and duodenum - 20 mg / day.
For the eradication of Helicobacter pylori the following combinations are recommended:
1. Controls В® 20-40 mg 2 times / day + amoxicillin 1000 mg 2 times / day + clarithromycin 500 mg 2 times / day;
2. Controls В® 20-40 mg 2 times / day + metronidazole 500 mg 2 times / day + clarithromycin 500 mg 2 times / day;
3. Controls В® 20-40 mg 2 times / day + amoxicillin 1000 mg 2 times / day + metronidazole 500 mg 2 times / day.
The course of treatment is 7-14 days.
With Zollinger-Ellison syndrome Controlot В® is prescribed in a dose of 40-80 mg / 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. With an increase in the level of liver enzymes should stop using the drug.
Older patients, as well as patients with impaired renal function, do not need to adjust the dose, but do not exceed the dose of 40 mg / day. An exception is the use of combined antibacterial therapy against Helicobacter pylori, when elderly patients should also use Controlul В® in a dose of 40 mg 2 times / day.
Do not take Controller В® for prophylaxis.
SIDE EFFECT
When using Controlulok В® in accordance with the indications and in the recommended doses, adverse reactions are extremely rare. Most often (about 1%) there is diarrhea and headache.
Determination of the frequency of adverse reactions: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10 000 and <1 / 1000), very rarely (<1/10 000, including individual cases), the frequency is unknown (it is impossible to estimate based on available data).
From the hemopoietic system: rarely - agranulocytosis; very rarely - thrombocytopenia, leukopenia, pancytopenia.
From the nervous system: infrequently - headache, dizziness; rarely - dysgeusia.
From the side of the organ of vision: rarely - visual impairment (fogging).
From the digestive tract: infrequently - diarrhea, nausea / vomiting, bloating and flatulence, constipation, dry mouth, abdominal pain.
From the liver and bile ducts: infrequently - increased activity of liver enzymes (AST, GGT); rarely - increased bilirubin levels; frequency unknown - hepatocellular injury, jaundice.
From the side of the urinary system: the frequency is unknown - interstitial nephritis.
From the skin and subcutaneous tissues: infrequently - exanthema / rash, itching; rarely - hives, angioedema; frequency unknown - malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, toxic epidermal necrolysis, photosensitivity.
From the musculoskeletal system: rarely - arthralgia, myalgia.
From the side of metabolism: rarely - hyperlipidemia and increased concentration of lipids (triglycerides, cholesterols), change in body weight; frequency is unknown - hyponatremia, hypomagnesemia.
From the side of the immune system: rarely - hypersensitivity (including anaphylactic reactions and anaphylactic shock).
From the side of the psyche: infrequently - a violation of sleep; rarely - depression (including exacerbations of existing disorders); very rarely - disorientation (including exacerbations of existing disorders); the frequency is unknown - hallucinations, confusion (especially in patients who are predisposed to it), as well as the possible exacerbation of symptoms when they exist before the start of therapy.
From the genitals and the breast: rarely - gynecomastia.
General disorders: infrequent - weakness, fatigue and malaise; rarely - fever, peripheral edema.
CONTRAINDICATIONS
- dyspepsia of neurotic genesis;
- joint application with atazanavir;
- Pregnancy;
- lactation period;
- age up to 18 years;
- Hypersensitivity to the components of the drug, as well as to soy.
PREGNANCY AND LACTATION
Controls В® are contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Do not increase the daily dose of pantoprazole 40 mg in patients with impaired renal function, as well as elderly patients.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution , use the drug for liver failure.
In individuals with severe hepatic insufficiency, the daily dose should be reduced to 20 mg of pantoprazole. In addition, in these patients during therapy with the drug Controll В® it is necessary to control liver enzymes. If their level is raised, treatment should be interrupted.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
Older patients, dose adjustment is not required, but can not be exceeded by a dose of 40 mg / day. An exception is the use of combined antibacterial therapy for Helicobacter pylori, when elderly patients should also use Controll В® in a dose of 20-40 mg 2 times / day.
SPECIAL INSTRUCTIONS
Before starting treatment with Controlul В® , the possibility of malignant growth should be excluded, since the drug can mask symptoms and delay the correct diagnosis.
Patients should consult a physician if they are to carry out endoscopy or a urea breath test.
Patients should consult a physician in the following cases:
- unintended weight loss, anemia, gastrointestinal bleeding, swallowing disorder, persistent vomiting or vomiting with blood. In these cases, taking the drug can partially alleviate the symptoms and delay the correct diagnosis;
- Previous surgical intervention on the gastrointestinal tract or stomach ulcer;
- Continuous symptomatic treatment of dyspepsia and heartburn for 4 weeks or more;
- liver disease, incl. jaundice and liver failure;
- other serious diseases that worsen overall health.
Patients over the age of 55 years, with new or newly changed symptoms, should consult a physician.
When taking drugs that reduce the acidity of gastric juice, the risk of infections caused by bacteria of the genus of gastrointestinal Salmonella spp., Campylobacter spp., Increases slightly. or Clostridia difficile.
Impact on the ability to drive vehicles and manage mechanisms
Patients should refrain from managing vehicles and other mechanisms requiring increased attention, due to the likelihood of dizziness and visual impairment.
OVERDOSE
To date, no overdosage has occurred as a result of the use of Controlul В® . Doses up to 240 mg were given intravenously for 2 min and were well tolerated.
Treatment: in case of an overdose and only if there are clinical manifestations, symptomatic and supportive therapy is performed. Pantoprazole is not excreted by hemodialysis.
DRUG INTERACTION
Simultaneous use of Controlul В® can reduce the absorption of drugs, the bioavailability of which depends on the pH of the stomach (including iron salts, ketoconazole).
Controllers В® can be prescribed without the risk of drug interaction:
- Patients with cardiovascular diseases receiving cardiac glycosides (digoxin), slow calcium channel blockers (nifedipine), beta-adrenoblockers (metoprolol);
- patients with gastrointestinal diseases who take antacids, antibiotics (amoxicillin, clarithromycin);
- patients taking oral contraceptives containing levonorgestrel and ethinylestradiol;
- patients taking NSAIDs (diclofenac, phenazone, naproxen, piroxicam);
- patients with endocrine system diseases, taking glibenclamide, levothyroxine;
- Patients with anxiety and sleep disorders receiving diazepam;
- patients with epilepsy taking carbamazepine and phenytoin;
- patients taking indirect anticoagulants, such as warfarin and fenprokumone (under the control of prothrombin time and INR at the beginning and after treatment, and also during the irregular intake of pantoprazole);
- patients who underwent transplantation, taking cyclosporin, tacrolimus.
The absence of clinically significant drug interaction with caffeine, ethanol, theophylline was noted.
TERMS OF RELEASE FROM PHARMACY
Controller В® in the form of 20 mg tablets is approved for use as an OTC product.
ControlulВ® in the form of 40 mg tablets is dispensed by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years. Do not use after the expiry date printed on the package.
