Controls for solution preparation lyophilisate 40mg, No. 1
Russian Pharmacy name:
Контролок для приготовления раствора лиофилизат 40мг, №1
peptic ulcer of the stomach and duodenum (in the acute phase), erosive gastritis (including those associated with the use 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).
ControlokЃ should be administered intravenously only in cases where it is impossible to take the drug inside. Duration of use - no more than 7 days. If the possibility of oral administration arises, intravenous administration should be replaced by ingestion of ControlokЃ enteric-coated tablets.
Peptic ulcer and duodenal ulcer (in the acute phase), erosive gastritis (including those associated with taking NSAIDs), GERD: the recommended dose is 40 mg (1 bottle) per day.
Zollinger-Ellison syndrome: for long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose for intravenous administration at the beginning of treatment is 80 mg. Thereafter, the dose can be increased or decreased. In the case of using the drug in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. A temporary increase in the daily dose to 160 mg is possible, but no longer than is necessary for adequate control of acidity. If emergency control of acidity is necessary, an initial dose of 80 mg 2 times / day is sufficient to reduce acid release in the range of less than 10 mEq / h for 1 hour in most patients.
Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration): the recommended dose is 80 mg / day. In the case of using the drug in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. A temporary increase in the daily dose to 160 mg is possible.
In patients with severe liver dysfunction, the daily dose should not exceed 20 mg of pantoprazole (half a bottle).
In elderly patients and in patients with impaired renal function, dose adjustment is not required, however, the recommended daily dose of pantoprazole 40 mg should not be exceeded.
Rules for the preparation and administration of solution for injection
To prepare a ready-to-use solution for injection, 10 ml of 0.9% sodium chloride solution is added to a vial containing dry matter. The finished solution can be injected in an amount of 10 ml, it is also permissible to dilute it in 100 ml of 0.9% sodium chloride solution or in 5% glucose solution.
Do not use other solvents!
The drug 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 to avoid microbial contamination.
Lyophilisate for the preparation of a solution for intravenous administration in the form of a white or almost white powder or a compacted mass of white or almost white color.
1 fl. pantoprazole sodium sesquihydrate 45.1 mg,
which corresponds to the content of sodium pantoprazole (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.
Bottles of colorless glass (1) - cardboard packs.
concomitant use with atazanavir;
pregnancy;
lactation period (breastfeeding);
children and adolescents up to 18 years old;
hypersensitivity to the components of the drug.
Pharmaco-therapeutic group: Proton pump inhibitor
pharmachologic effect
Proton pump inhibitor (H + -K + -ATP-ase).
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, ControlocЃ has a greater chemical stability at neutral pH, and a lower potential for interaction with the liver oxidase system, which depends on cytochrome P450. Therefore, ControlocЃ does not interact with many other drugs.
Pharmacokinetics
The pharmacokinetics are the same after both single and multiple use of the drug.
Suction
In the dose range from 10 to 80 mg, the kinetic direct concentration of pantoprazole in blood plasma has a linear relationship both after oral administration and after intravenous administration.
Distribution
The binding of pantoprazole to blood plasma proteins is 98%.
Vd is 0.15 l / kg, ground clearance is 0.1 l / h / kg.
Metabolism
It is metabolized in the liver. The main metabolite in blood plasma and urine is desmethylpantoprazole, conjugated with sulfate.
Withdrawal
The main route of excretion is by the kidneys (about 80%) in the form of pantoprazole metabolites, in a small amount it is excreted through the intestines. T1 / 2 of the drug is 1 hour, T1 / 2 of the metabolite is about 1.5 hours. Several cases of delayed elimination have been observed.
Pharmacokinetics in special clinical situations
When using pantoprazole in patients with impaired renal function (including patients on hemodialysis), dose reduction is not required. As in healthy patients, the T1 / 2 of pantoprazole is short. Only a very small part of the drug is dialyzed. Does not cumulate.
In patients with liver cirrhosis (classes A, B on the Child-Pugh scale), the T1 / 2 value increases to 7-9 hours and AUC increases 5-7 times, Cmax in blood plasma increases 1.5 times compared with patients with normal function liver.
A slight increase in AUC and Cmax in elderly patients is not clinically significant.
Indications of the drug ControlokЃ
peptic ulcer of the stomach and duodenum (in the acute phase), erosive gastritis (including those associated with the use 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).
Dosage regimen
ControlokЃ should be administered intravenously only in cases where it is impossible to take the drug inside. Duration of use - no more than 7 days. If the possibility of oral administration arises, intravenous administration should be replaced by ingestion of ControlokЃ enteric-coated tablets.
Peptic ulcer and duodenal ulcer (in the acute phase), erosive gastritis (including those associated with taking NSAIDs), GERD: the recommended dose is 40 mg (1 bottle) per day.
Zollinger-Ellison syndrome: for long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose for intravenous administration at the beginning of treatment is 80 mg. Thereafter, the dose can be increased or decreased. In the case of using the drug in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. A temporary increase in the daily dose to 160 mg is possible, but no longer than is necessary for adequate control of acidity. If emergency control of acidity is necessary, an initial dose of 80 mg 2 times / day is sufficient to reduce acid release in the range of less than 10 mEq / h for 1 hour in most patients.
Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration): the recommended dose is 80 mg / day. In the case of using the drug in a daily dose of more than 80 mg, the dose should be divided and administered 2 times / day. A temporary increase in the daily dose to 160 mg is possible.
In patients with severe liver dysfunction, the daily dose should not exceed 20 mg of pantoprazole (half a bottle).
In elderly patients and in patients with impaired renal function, dose adjustment is not required, however, the recommended daily dose of pantoprazole 40 mg should not be exceeded.
Rules for the preparation and administration of solution for injection
To prepare a ready-to-use solution for injection, 10 ml of 0.9% sodium chloride solution is added to a vial containing dry matter. The finished solution can be injected in an amount of 10 ml, it is also permissible to dilute it in 100 ml of 0.9% sodium chloride solution or in 5% glucose solution.
Do not use other solvents!
The drug 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 to avoid microbial contamination.
Side effect
When using the drug ControlokЃ in accordance with the indications and in the recommended doses, side reactions are extremely rare. Thrombophlebitis is most often observed at the injection site; in 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 rare (<1/10 000, including isolated cases), the frequency is unknown (cannot be estimated from the available data).
From the digestive system: infrequently - diarrhea, nausea / vomiting, bloating and flatulence, constipation, dry mouth, discomfort and abdominal pain.
From the liver and biliary tract: infrequently - increased activity of hepatic enzymes (AST, GGT); rarely - an increase in the level of bilirubin; frequency unknown - hepatocellular damage, jaundice.
From the hematopoietic 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 - sleep disturbance; rarely - depression (including exacerbation of existing disorders); very rarely - disorientation (including exacerbation of existing disorders); the frequency is unknown - hallucinations, confusion (especially in patients predisposed to this), as well as a possible exacerbation of symptoms if they exist before starting therapy.
From the urinary system: the frequency is unknown - interstitial nephritis.
On the part of the skin and subcutaneous tissues: infrequently - exanthema / rash, itching; frequency unknown - malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, toxic epidermal necrolysis, photosensitization.
From the musculoskeletal system: rarely - arthralgia, myalgia.
From the side of metabolism: rarely - hyperlipidemia and increased concentration of lipids (triglycerides, cholesterols), changes in body weight; frequency unknown - hyponatremia, hypomagnesemia.
Allergic reactions: rarely - urticaria, angioedema.
From the immune system: rarely - hypersensitivity (including anaphylactic reactions and anaphylactic shock).
From the endocrine system: rarely - gynecomastia.
General reactions: infrequently - weakness, fatigue and malaise; rarely - an increase in body temperature, peripheral edema.
Local reactions: often - thrombophlebitis at the injection site.
Contraindications for use
concomitant use with atazanavir;
pregnancy;
lactation period (breastfeeding);
children and adolescents up to 18 years old;
hypersensitivity to the components of the drug.
Application during pregnancy and lactation
The use of the drug ControlokЃ during pregnancy and lactation (breastfeeding) is contraindicated.
Application for violations of liver function
The drug should be used with caution in liver failure.
In persons with severe hepatic impairment, the daily dose should be reduced to 20 mg of pantoprazole. In addition, in such patients, during therapy with Controloc, it is necessary to control liver enzymes. In the event of an increase in their level, treatment should be interrupted.
Application for impaired renal function
Do not increase the daily dose of pantoprazole 40 mg in patients with impaired renal function, as well as in elderly patients.
Application in children
Contraindicated in children and adolescents under 18 years of age.
Use in elderly patients
In elderly patients, dose adjustment is not required, but the recommended daily dose of pantoprazole 40 mg should not be exceeded.
special instructions
Pantoprazole is not indicated for the treatment of mild gastrointestinal complaints such as neurogenic dyspepsia.
Patients should consult a physician if any of the following symptoms occur:
significant unintentional weight loss;
periodic vomiting;
swallowing disorder;
anemia, melena.
If you suspect or have a stomach ulcer before starting treatment with pantoprazole, you should exclude the possibility of a malignant neoplasm, because drug treatment can mask symptoms and delay correct diagnosis.
In patients with severely impaired liver function, it is necessary to monitor blood biochemical parameters. With an increase in the activity of liver enzymes, the drug should be discontinued.
When taking drugs that reduce the acidity of gastric juice, the risk of gastrointestinal infections slightly increases, the causative agents of which are bacteria of the genus Salmonella spp., Campylobacter spp.
Influence on the ability to drive vehicles and mechanisms
During the period of treatment, patients should refrain from driving vehicles and other mechanisms that require increased attention, due to the likelihood of dizziness and visual impairment.
Overdose
Until now, overdose phenomena as a result of the use of the drug ControlokЃ have not been noted. Doses up to 240 mg IV for 2 min were well tolerated.
Treatment: in case of overdose and only in the presence of clinical manifestations, symptomatic and supportive therapy is carried out. Pantoprazole is not excreted by hemodialysis.
Drug interactions
Concomitant use of the drug ControlocЃ can reduce the absorption of drugs, the bioavailability of which depends on the pH of the stomach environment (for example, ketoconazole, itraconazole, posaconazole, and such as erlotinib).
онтролокЃ может быть назначен без риска нежелательного лекарственного взаимодействи¤ пациентам с заболевани¤ми сердечно-сосудистой системы, принимающим сердечные гликозиды (дигоксин), блокаторы медленных кальциевых каналов (нифедипин), бета-адреноблокаторы (метопролол); пациентам с заболевани¤ми ? “, принимающим антациды, антибиотики (амоксициллин, кларитромицин), метронидазол; пациентам, принимающим пероральные контрацептивы, содержащие левоноргестрел и этинилэстрадиол; пациентам, принимающим Ќѕ¬— (диклофенак, напроксен, пироксикам); пациентам с заболевани¤ми эндокринной системы, принимающим глибенкламид, левотироксин натри¤; пациентам с тревожными состо¤ни¤ми и расстройствами сна, принимающим диазепам; пациентам с эпилепсией, принимающим карбамазепин и фенитоин; пациентам, принимающим непр¤мые антикоагул¤нты, такие как варфарин и фенпрокумон (под контролем протромбинового времени и ћЌќ в начале и по окончании лечени¤, а также во врем¤ нерегул¤рного приема пантопразола; пациентам, перенесшим трансплантацию, принимающим циклоспорин, такролимус.
The absence of drug interactions with theophylline, caffeine and ethanol was also noted.
Storage conditions of the drug ControlokЃ
The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25 ? C.
Shelf life of the drug ControlocЃ
Shelf life is 2 years.
Terms of sale
The drug is available with a prescription.