Kontrolok 1's 40 mg powder for solution for injection

The instruction for medical use




of Controlok Torgovoye medicine a name
Controlok

Mezhdunarodnoye the unlicensed


name Pantoprazol Lekarstvennaya a form
Powder for preparation of solution for injections, 40 mg

Structure
One bottle contains
active agent - a pantoprazol of sodium sexivihydrat of 45.10 mg (it is equivalent to a pantoprazol of 40.0 mg),
excipients: dinatrium edetat, sodium hydroxide.

The description
From white till almost white color dry matter

Pharmacotherapeutic group
Drugs for treatment of the diseases connected with disturbance of acidity. Antiulcerous drugs and drugs for treatment of a gastroezofagalny reflux. Inhibitors of the protonew pump. Pantoprazol.
The ATX A02BC02 code

the Pharmacological

Pharmacokinetics Pharmacokinetics properties does not change after one-time or repeated introduction. In the range of doses from 10 to 80 mg the pharmacokinetics of a pantoprazol remains linear both after oral administration, and after intravenous maintaining.
Linking with proteins of blood plasma - approximately for 98%. Substance is almost completely metabolized in a liver. The main metabolite defined in blood serum and urine – desmetilpantoprazol, being connection with sulfate.
The volume of distribution is about 0.15 l/kg, clearance about 0.1 l/h/kg. Elimination half-life makes about 1.5 hours. Due to the specific activation of a pantoprazol in covering cells the elimination half-life does not correlate with duration of its action (acid secretion oppression). About 80% of drug eliminirutsya by kidneys, other 20% with excrements.
The pharmacodynamics
Pantoprazol is the substituted benzimidazole which is slowing down secretion of hydrochloric acid in a stomach by specific impact on a proton pomp of covering cells.
In acidic environment of covering cells pantoprazol turns into the active form – cyclic sulphenamide where it suppresses enzyme H+, K+-ATFazu.
Blocking the proton pump, Controlok interferes with process of a kislotoobrazovaniye at the level of a final stage of synthesis of hydrochloric acid in a stomach. Inhibiting effect dozozavisimo also influences the level of basal and stimulated secretion of hydrochloric acid (irrespective of a type of an irritant). In a peptic ulcer of a stomach and the duodenum associated with Helicobacter pylori, such decrease in gastric secretion increases sensitivity of a microorganism to antibiotics.
Pantoprazol has big chemical stability at a neutral rn, and the smaller potential of interaction with other medicines.
At intravenous administration of 80 mg of a pantoprazol, the anti-secretory effect reaches a maximum within 1 hour and 24 hours remain.

Indications
- a peptic ulcer of a stomach and duodenum
- a reflux esophagitis
- Zollingera-Ellison's syndrome or other states which are characterized by pathological gastric hypersecretion

the Route of administration and doses
At impossibility of administration of drug inside in the tableted form or insufficient efficiency at such method of administration apply it intravenously. For full elimination of symptoms the administration of drug within 7 days can be required.
For preparation of solution, ready to the use, for injections, 10 ml of normal saline solution of sodium of chloride (0.9%) add to the bottle containing dry matter. This solution can be applied directly (intravenously struyno) or after mixing from 100 ml of 0.9% of solution of sodium of chloride and also from 5% by glucose solution (intravenously by drop infusion).
The prepared solution has to be used within 12 hours after preparation. Intravenous administration should be carried out for 2–15 min.
A peptic ulcer of a stomach and duodenum, complicated by gastrointestinal bleeding, for the purpose of prevention of repeated bleeding, a gastroesophageal reflux disease (GERD)
the Recommended dose of 40 mg a day.
Zollingera-Ellison
Pri's syndrome long-term treatment of a syndrome of Zolingera-Ellison and other morbid hyper secretory conditions the recommended daily dose in an initiation of treatment makes 80 mg of Controlok intravenously. After that the dose can be increased or reduced. In case of use of drug in a daily dose over 80 mg, a dose can be divided and be entered twice a day. Perhaps temporary increase in a daily dose up to 160 mg Controlok. The course of treatment is not limited, and depends on clinical need.
Special groups of patients
At patients with the profound abnormal liver functions the daily dose of drug should not exceed 20 mg
of Dose adjustment it is not required to patients of advanced age and patients with renal failures

Side effects
Below the observed side reactions with a frequency of their occurrence are listed: very often (³ 1/10), it is frequent (from ³ 1/00 to & lt, 1/10), infrequently (from ³ 1/1000 to & lt, 1/100), is rare (from ³ 1/10000 to & lt, 1/1000), is very rare (& lt, 1/10000), it is unknown (it is impossible to estimate on the available data).
Often
– thrombophlebitis in the injection site of an injection
Infrequently
- a headache, dizziness
- dryness in a mouth, nausea, vomiting, an abdominal distension, abdominal pain and discomfort, diarrhea, a constipation
- skin rash, an itching, a dieback
- an asthenia, fatigue and an indisposition
- increase in activity of liver enzymes (transaminases, g-GT)
- the sleep disorder
Is rare
- an agranulocytosis
- hypersensitivity to active and to auxiliary components of drug (including anaphylactic reactions and an acute anaphylaxis)
- a lipidemia, increase in level of triglycerides, cholesterol
- increase in content of bilirubin
- change of weight, disturbance of taste
- a depression (and all accompanying deteriorations)
- disorder of vision / illegibility of sight
- urticaria, a Quincke's disease
- an arthralgia, myalgia
- a gynecomastia
- fervescence, peripheral hypostases
Very seldom
- thrombocytopenia, a leukopenia, a pancytopenia
- a disorientation (and all accompanying deteriorations)
It is unknown
- a hyponatremia, a hypomagnesiemia
- hallucinations, confusion of consciousness (especially at the patients predisposed to these states and also deterioration in these symptoms if they existed prior to treatment)
- hepatocellular damages, jaundice, hepatocellular insufficiency
- Stephens-Johnson's syndrome, a Lyell's disease, an exudative mnogoformny erythema, photosensitivity
- interstitial nephrite

of the Contraindication
- hypersensitivity to drug components, other substituted benzimidazoles
- combined use of a pantoprazol with atazanaviry

Medicinal interactions
It is necessary to pay attention to a concomitant use with drugs which absorption is rn-dependent, for example ketokonazol, itrakonazol, pozakonazol, erlotinib, including with the drugs appointed shortly before a course of treatment Controlok in view of change of absorption of these drugs.
The concomitant use of Controlok and an atazanavir considerably reduces efficiency of the last.
Pri combined use of a fenprokumon or warfarin, celebrated several isolated cases of change of the International normalizing relation (MNO or INR). Therefore for the patients undergoing treatment by coumarinic anticoagulants (for example, fenprokumony or warfarin), it is recommended to watch a prothrombin time / MNO after the beginning, the termination or during irregular use of Controlok.
Controlok has the low potential of interaction with the system of P450 cytochrome. Therefore the risk of the side reactions caused by Controlok's interaction with other drugs which is metabolized a system P450 cytochrome can be considered as minimum. Special researches did not reveal clinically significant interaction of the drug Controlok with caffeine, carbamazepine, diazepam, ethanol, diclofenac, glibenclamide, Naproxenum, metoprololy, nifedipine, Phenytoinum, piroxicam, theophylline, the oral contraceptives containing levonorgestrel and ethinylestradiol.
At a concomitant use with antibiotics, such as klaritromitsin, amoxicillin, with metronidazole, interactions it is not revealed.


At patients with heavy abnormal liver functions at Controlok's introduction, especially during the long period, regular control of level of enzymes of a liver is recommended to carry out special instructions. At increase in level of liver enzymes it is necessary to stop drug use.
At combination therapy it is necessary to consider in general all characteristics of the used drugs.
At treatment by Controlok the expressiveness of symptoms of malignant diseases can decrease that can delay establishment of the correct diagnosis, in communication with what before an initiation of treatment it is necessary to exclude a possibility of a malignant new growth.
Patients have to consult with the doctor in the following cases:
- if symptoms did not pass within 2 weeks
- involuntary weight reduction of a body, anemia, gastrointestinal bleeding, a dysphagy, persistent vomiting or vomiting with blood, in these cases, it is necessary to exclude existence of malignant process
- earlier there was stomach ulcer, or the undergone surgery on a stomach
- disturbances of digestion or heartburn within 4 or more weeks
- jaundice, dysfunctions or diseases of a liver
- any other serious disease influencing overall health
- patients is more senior than 55 years in the presence of the new or recently changed symptoms.
Patients at whom long-term recurrent symptoms of disturbance of digestion or heartburn are observed have to see a doctor.
At patients with Zollingera-Ellison's syndrome and other morbid hyper secretory conditions which treatment demands long reception of Controlok as the drug blocking secretion of acid in a stomach reduction of absorption of B12 vitamin (cyanocobalamine) owing to hypo - or achlorhydrias is possible. It should be considered in the presence of the corresponding clinical symptoms.
Lowering of acidity of a stomach increases quantity of gastric bacteria which usually are present at digestive tract. Treatment by the drugs lowering acidity leads to increase in risk of developing the gastrointestinal infections caused by such microorganisms as Salmonella, Campylobacter.
Use in pediatrics
of Data on drug Controlok use, powder for preparation of solution for injections, up to 18 years is not available for children and teenagers.
Pregnancy and a lactation
of Adequate data on use of a pantoprazol at pregnancy are not present. Researches on animals demonstrate reproductive toxicity of drug. The potential risk for the person is unknown. Controlok should not be applied during pregnancy if in it there is no obvious need.
The lactation for drug treatment is stopped.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms.
It is necessary to refrain from control of the vehicles and other mechanisms requiring special attention because of the probability of dizzinesses and a disorder of vision

Overdose
Symptoms: are unknown
Treatment: at suspicion on overdose performing the supporting and symptomatic therapy is recommended. Drug is not removed by means of a hemodialysis

the Form of release and packing
On 40 mg of active agent place in the glass colourless bottles corked by rubber bungs and which are pressed out by aluminum caps with disks from polypropylene.
1 bottle together the instruction for medical use in the state and Russian languages is put in a cardboard box
by
Storage conditions
to Store at a temperature not above 25 °C.
To store out of children's reach!


2 years
not to use a period of storage after an expiration date.

Prescription status
According to the prescription


of Proizvoditel Takeda Gmbh, Zingen, Germany

the Name and the country of the owner of the registration certificate
of Takeda GmbH, Germany

the Name and the country
of the organization packer Takeda Gmbh, Zingen, Germany
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) of "Takeda Ostevropa Marketing Service GmbH" Almaty, Begalin St. 136 an anomer of phone number (727) 2444004, Fax number (727) 2444005 E-mail address:
To Develop DSO-KZ@takeda.com