Composition, form of production and packaging
Liofilizate for the preparation of a solution for intravenous administration of white or almost white; The applied solvent is a clear, colorless solution.
1 f.
pantoprazole sodium sesquihydrate 45.1 mg,
which corresponds to the content of pantoprazole 40 mg
Solvent: r-p sodium chloride 0.9% - 10 ml.
40 mg - bottles of colorless glass with a volume of 10 ml (1) complete with a solvent (amp.) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
H + -K + -ATPase inhibitor. It blocks the final stage of the secretion of hydrochloric acid (hydrochloric acid), reducing the basal and stimulated (irrespective of the nature of the stimulus) secretion. In duodenal ulcer associated with Helicobacter pylori, a decrease in gastric secretion increases the sensitivity of microorganism to antibiotics.
Does not affect the motility of the gastrointestinal tract.
With IV administration, 80 mg antisecretory effect reaches a maximum within 1 h and lasts 24 hours. Secretory activity is normalized 3-4 days after the end of the drug intake.
PHARMACOKINETICS
In the dose range of 10 to 80 mg, the pharmacokinetic parameters of pantoprazole have a linear relationship after intravenous administration. The drug does not cumulate. Values ​​of pharmacokinetic parameters of pantoprazole for multiple and single administrations are comparable.
Distribution
V d is 0.15 l / kg. Basically, the drug is distributed in the extracellular fluid. Binding to plasma proteins is 98%.
Metabolism
Intensively metabolized in the liver, mainly with the participation of the enzyme system CYP2C19. The main metabolite in blood plasma and urine is desmethylpentoprazole, conjugated with sulfate.
Excretion
T 1/2 after intravenous administration is an average of 1 hour. Most of the drug is excreted by the kidneys in the form of inactive metabolites. In small quantities is excreted through the intestine.
Pharmacokinetics in special clinical cases
In patients with renal insufficiency, the pharmacokinetics do not change significantly.
In liver failure, the duration of T 1/2 increases to 7-9 hours. AUC values ​​are 5-7 times higher, and C max is 1.5 times higher in patients with hepatic impairment compared with volunteers.
INDICATIONS
- Stomach ulcer and duodenal ulcer (in the phase of exacerbation), erosive gastritis (including associated with the intake of NSAIDs);
- Gastroesophageal reflux disease (GERD): erosive reflux esophagitis (treatment), symptomatic treatment of GERD (ie NERB - non-erosive reflux disease);
- 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).
DOSING MODE
This dosage form of Sunprase is indicated only for IV administration. The drug is recommended only in cases where oral administration of pantoprazole is not indicated. As soon as oral therapy becomes available, IV administration should be discontinued.
The recommended dose for intravenous administration is the administration of the contents of one vial (40 mg pantoprazole) 1 time / day. Data on intravenous administration can be used within 7-10 days, prolongation of the course of treatment depends on the clinical need.
With prolonged treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose at the beginning of treatment is 80 mg of Sanpras. 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 injected 2 times / day. Perhaps a temporary increase in the daily dose to 160 mg of Sanpras.
With the eradication of Helicobacter pylori in combination with antibacterial agents, the recommended daily dose is 80 mg of Sanprasse for 7-10 days, the dose should be divided and administered 2 times / day.
In severe violations of liver function, the daily dose should be reduced to 20 mg of pantoprazole. In addition, during treatment with the drug, such patients need regular monitoring of the activity of liver enzymes. In the case of increased activity of hepatic enzymes, treatment should be discontinued.
Older patients, as well as patients with impaired renal function (including patients on hemodialysis) do not need to increase the daily dose of pantoprazole 40 mg.
Rules for preparation and administration of the drug
Before the injection, the contents of the vial must be reconstituted with 10 ml of 0.9% sodium chloride solution.
This solution is injected or infused after mixing with 100 ml of 0.9% sodium chloride solution, 5% glucose solution or 10% glucose solution. The pH of the ready-to-use solution should be within 9-10.
The duration of administration should be 2-15 minutes. The prepared solution should be used within 3 hours after preparation.
SIDE EFFECT
When taking Sanpras according to the indications and in recommended doses, side effects occur extremely rarely.
From the side of the central nervous system: sometimes - a headache; rarely - depression, hallucinations (especially in predisposed patients), disorientation and confusion; at single cases - dizziness or visual impairment.
From the digestive system: sometimes - pain in the upper abdomen, diarrhea, constipation, flatulence; rarely - nausea, vomiting, dry mouth; very rarely - hepatocellular insufficiency, leading to jaundice with or without hepatic insufficiency, an increase in the activity of liver enzymes (transaminase, glutamyltranspeptidase).
From the musculoskeletal system: rarely - arthralgia; in isolated cases - myalgia.
From the hemopoietic system: very rarely - leukopenia, thrombocytopenia.
Allergic reactions: very rarely - anaphylactic reactions, including anaphylactic shock, urticaria, angioedema.
Dermatological reactions: very rarely - itching, skin rash, severe skin reactions (Stevens-Johnson syndrome, erythema multiforme, photosensitivity, Lyell's syndrome);
Local reactions: very rarely - phlebitis, thrombophlebitis.
Other: very rarely - peripheral edema, increased triglycerides, interstitial nephritis; in isolated cases - an increase in body temperature.
CONTRAINDICATIONS
- dyspepsia of neurotic genesis,
- lactation period;
- children's age till 18 years;
- Hypersensitivity to the drug.
With caution: use the drug in pregnancy and liver failure.
PREGNANCY AND LACTATION
Experience with the drug during pregnancy and lactation is limited. The drug can be used during pregnancy only if the benefit to the mother exceeds the possible risk to the fetus.
There is no data on the isolation of pantoprazole with breast milk. You should stop breastfeeding while taking the drug.
In experimental studies of reproductive function, slight embryotoxicity was noted in doses exceeding 5 mg / kg.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function (including patients on hemodialysis) there is no need to increase the daily dose of pantoprazole 40 mg.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In severe violations of liver function, the daily dose should be reduced to 20 mg of pantoprazole. In addition, during treatment with the drug, such patients need regular monitoring of the activity of liver enzymes. In the case of increased activity of hepatic enzymes, treatment should be discontinued.
APPLICATION FOR CHILDREN
Contraindication: children under 18 years.
APPLICATION IN ELDERLY PATIENTS
Elderly patients do not need to increase the daily dose of pantoprazole 40 mg.
SPECIAL INSTRUCTIONS
The use of pantoprazole for dyspepsia of neurogenic genesis is not effective.
In the presence of any of the anxiety symptoms (for example, significant unintentional weight loss, recurrent vomiting, dysphagia, anemia or melena) and in case of suspected or having a stomach ulcer, the possibility of malignant growth should be excluded, since. treatment with pantoprazole can reduce symptoms and delay the correct diagnosis. If the symptoms persist despite adequate treatment, further examination should be carried out.
Before and after treatment, endoscopic control is necessary to exclude the possibility of having malignant diseases of the stomach or esophagus, because the treatment can mask the symptoms and delay the correct diagnosis.
Use in Pediatrics
There is insufficient data on the use of the drug in children under 18 years of age .
Impact on the ability to drive vehicles and manage mechanisms
The use of the drug does not affect the patient's ability to perform work requiring increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms of an overdose in humans are not known. Doses up to 240 mg with iv introduction were well tolerated.
Treatment: in case of an overdose with signs of intoxication, general detoxification measures, symptomatic therapy, hemodialysis are used.
DRUG INTERACTION
Simultaneous application of Sanpraz can reduce the absorption of drugs, the bioavailability of which depends on the pH of the stomach (including ketoconazole, iron salts, ritonavir).
With the joint application of Sanpraz with atazanavir, plasma concentrations of atazanavir decrease and its therapeutic effect decreases.
In carrying out specific tests of Sanpras with such drugs as digoxin, nifedipine, metoprolol, amoxicillin, clarithromycin, oral contraceptives (levonorgestrel / ethinyl estradiol), diclofenac, phenazone, naproxen, piroxicam, glibenclamide, levothyroxine sodium, diazepam, carbamazepine, phenytoin, cyclosporin, tacrolimus, cisapride, midazolam, metronidazole, theophylline, caffeine, ethanol, clinically significant interaction was not detected.
According to post-marketing data, when taking a drug with warfarin, prothrombin time increases, which can lead to bleeding, up to a lethal outcome. It is recommended to determine prothrombin time.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light and out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years, solvent - 3 years.
