Composition, form of production and packaging
Powder for the preparation of a solution for intravenous administration as a dry substance white or almost white.
pantoprazole sodium sesquihydrate 45.1 mg,
which corresponds to the content of pantoprazole sodium (anhydride) 42.3 mg,
which corresponds to the content of pantoprazole (free acid) 40 mg
Excipients: disodium edetate - 1 mg, sodium hydroxide - 0.24 mg.
Vials of colorless glass (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
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.
Compared to other proton pump inhibitors, Controll В® has a great chemical stability at neutral pH, and a lower interaction potential with liver oxidase system dependent on cytochrome P450. Therefore Controller В® does not interact with many other drugs.
Pharmacokinetics is the same as after a single, and after repeated use of the drug.
In the dose range of 10 to 80 mg, the kinetic direct concentration of pantoprazole in blood plasma has a linear relationship both after ingestion and after intravenous administration.
The binding of pantoprazole to plasma proteins is 98%.
V d is 0.15 l / kg, clearance is 0.1 l / h / kg.
Metabolised in the liver. The main metabolite in the blood plasma and in urine is desmethylpentoprazole, conjugating with sulfate.
The main way of excretion is by kidneys (about 80%) in the form of metabolites of pantoprazole, in a small amount is excreted through the intestine. T 1/2 of the drug - 1 hour, T 1/2 metabolite - about 1.5 hours. There were several cases of delayed elimination.
Pharmacokinetics in special clinical cases
When pantoprazole is used in patients with impaired renal function (including patients on hemodialysis), no dose reduction is required. As in healthy patients, T 1/2 ofpantoprazole is short. Only a very small part of the drug is dialyzed. Do not cumulate.
In patients with cirrhosis of the liver (classes A, B on the Child-Pugh scale) the value of T 1/2 increases to 7-9 h and the AUC increases 5-7 times, C max in blood plasma increases by 1.5 times in comparison with patients with normal liver function.
A slight increase in AUC and C max in elderly patients is not clinically significant.
- peptic ulcer of the stomach and duodenum (in the phase of exacerbation), erosive gastritis (including associated with the intake of NSAIDs);
- gastroesophageal reflux disease (GERD): treatment of erosive reflux esophagitis, symptomatic treatment of non-erosive reflux disease (NERD);
- Zollinger-Ellison syndrome;
- eradication of Helicobacter pylori in combination with antibacterial agents;
- treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration).
Controls В® should be administered iv only in those cases when it is impossible to take the drug inside. Duration of application - no more than 7 days. If there is a possibility of oral administration, intravenous infusion should be replaced by ingestion of Controlol В® tablets coated with an enteric-coated membrane.
Peptic ulcer of the stomach and duodenum (in the phase of exacerbation), erosive gastritis (including those associated with taking NSAIDs), GERD: therecommended dose is 40 mg (1 bottle) per day.
Zollinger-Ellison syndrome: with the long-term treatment of Zolinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose for IV administration at the beginning of treatment is 80 mg. After this, the dose may be increased or decreased. If the drug is used in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. It is possible to temporarily increase the daily dose to 160 mg, but not longer than necessary for adequate acidity control. If an emergency acidity control is required, the initial dose of 80 mg 2 times / day is sufficient to reduce the acid release in the range of less than 10 mEq / h for 1 h in most patients.
Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration): the recommended dose is 80 mg / day. If the drug is used in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. Perhaps a temporary increase in the daily dose to 160 mg.
In patients with severe impairment of liver function, the daily dose should not exceed 20 mg of pantoprazole (half a vial).
In elderly patients and patients with impaired renal function, dose adjustment is not required, but the recommended daily dose of pantoprazole 40 mg should not be exceeded.
Rules for the preparation and injection of injection solutions
To prepare a ready-to-use solution for injection, 10 ml of 0.9% sodium chloride solution is added to a vial containing a dry substance. The ready-made solution can be administered in an amount of 10 ml, it is also permissible to dilute it in 100 ml of a 0.9% solution of sodium chloride or in a 5% solution of glucose.
Do not use any other solvents!
The preparation should be administered within 2-15 minutes.
The prepared solution is stable for 12 hours after preparation. However, it is recommended to use the solution immediately after preparation in order to avoid microbial contamination.
When using Controlulok В® in accordance with the indications and in the recommended doses, adverse reactions are extremely rare. The most commonthrombophlebitis at the injection site; about 1% of cases - 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).
On the part of the digestive system: infrequently - diarrhea, nausea / vomiting, bloating and flatulence, constipation, dry mouth, discomfort and 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 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 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 side of the urinary system: the frequency is unknown - interstitial nephritis.
From the skin and subcutaneous tissues: infrequently - exanthema / rash, itching; 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.
Allergic reactions: rarely - hives, angioedema.
From the side of the immune system: rarely - hypersensitivity (including anaphylactic reactions and anaphylactic shock).
From the endocrine system: rarely - gynecomastia.
General reactions: infrequent - weakness, fatigue and malaise; rarely - fever, peripheral edema.
Local reactions: often - thrombophlebitis at the injection site.
- joint application with atazanavir;
- the period of lactation (breastfeeding);
- children and adolescence under 18;
- Hypersensitivity to the components of the drug.
PREGNANCY AND LACTATION
Contraindicated the use of Controller В® during pregnancy and lactation (breastfeeding).
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 such patients during therapy with the drug Controls, it is necessary to monitor 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
In elderly patients, dose adjustment is not required, but the recommended daily dose of pantoprazole 40 mg should not be exceeded.
The use of pantoprazole is not indicated for the treatment of mild gastrointestinal complaints, such as dyspepsia of a neurogenic genesis.
Patients should consult a physician if the following symptoms occur:
significant unintended weight loss;
- periodic vomiting;
- Swallowing disorder;
If you suspect or have a stomach ulcer before starting treatment with pantoprazole, you should rule out the possibility of a malignant neoplasm. treatment with the drug can mask symptoms and delay proper diagnosis.
In patients with severe impairment of liver function, biochemical blood counts must be monitored. When the activity of liver enzymes increases, the drug should be discontinued.
When taking drugs that reduce the acidity of the gastric juice, the risk of gastrointestinal infections, which are caused by the bacteria of the genus Salmonella spp., Campylobacter spp., Is slightly increased.
Impact on the ability to drive vehicles and manage mechanisms
During treatment, patients should refrain from driving and other mechanisms requiring increased attention, due to the likelihood of dizziness and visual impairment.
To date, no overdosage has occurred as a result of the use of Controlul В® . Doses up to 240 mg with IV for 2 min 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.
Simultaneous use of Controller В® can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach environment (eg, ketoconazole, itraconazole, posaconazole and such as erlotinib).
Controller В® can be administered without the risk of undesirable drug interactions to patients with cardiovascular diseases taking cardiac glycosides (digoxin), slow calcium channel blockers (nifedipine), beta-blockers (metoprolol); patients with gastrointestinal diseases who take antacids, antibiotics (amoxicillin, clarithromycin), metronidazole; patients taking oral contraceptives containing levonorgestrel and ethinylestradiol; patients taking NSAIDs (diclofenac, naproxen, piroxicam); patients with diseases of the endocrine system, taking glibenclamide, levothyroxine sodium; patients with anxiety and sleep disorders receiving diazepam; patients with epilepsy taking carbamazepine and phenytoin; patients taking indirect anticoagulants, such as warfarin and fenprocumone (under the control of prothrombin time and INR at the beginning and at the end of treatment, as well as during an irregular intake of pantoprazole, patients undergoing transplantation taking cyclosporin, tacrolimus.
There was also a lack of drug interaction with theophylline, caffeine and ethanol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life - 2 years.