Description
Release form
Tablets.
Packing
56 pcs.
Pharmacological action
Pharmaceutical group:
Anti-gastric secretion drug – proton pump inhibitor
Pharmaceutical effect:
Nolpaza – pr anti-ulcer drug. It inhibits the enzyme H + -K + -ATPase (proton pump) in the parietal cells of the stomach and thereby blocks the final stage of the synthesis of hydrochloric acid. This leads to a decrease in the level of basal and stimulated secretion of hydrochloric acid, regardless of the nature of the stimulus.
After a single oral administration of a drug in a dose of 20 mg, the action of pantoprazole develops within the first hour, the maximum effect is achieved after 2-2.5 hours. Does not affect the motility of the gastrointestinal tract. After stopping the drug, secretory activity is fully restored after 3-4 days.
Pharmacokinetics:
Absorption
Pantoprazole is rapidly absorbed from the gastrointestinal tract, Cmax is achieved 2-2.5 hours after ingestion and is 1-1.5 μg / ml, while the Cmax value remains constant when taken repeatedly.
The bioavailability of the drug is 77%. Simultaneous eating does not affect the AUC, Cmax and bioavailability, there is only a change in the onset of the drug.
Distribution of
Plasma Protein Binding – About 98%. Vd is approximately 0.15 l / kg and clearance is 0.1 l / h / kg.
Metabolism
Pantoprazole is almost completely metabolized in the liver. It is an inhibitor of the isoenzyme CYP2C19.
Elimination of
T1 / 2 – 1 hour. Due to the specific binding of pantoprazole to the proton pump of parietal cells, T1 / 2 does not correlate with the duration of the therapeutic effect. Excretion of metabolites (80%) – mainly through the kidneys, the remaining part is excreted in the bile.
The main metabolite found in blood serum and urine is desmethyl pantoprazole, which is conjugated to sulfate. T1 / 2 of desmethyl pantoprazole (approximately 1.5 hours) is much larger than T1 / 2 of pantoprazole itself.
Pharmacokinetics in special clinical cases
In chronic renal failure (including patients undergoing hemodialysis), dose changes are not required. T1 / 2 – short, as in healthy individuals. Pantoprazole in very small quantities can be excreted during dialysis.
In patients with cirrhosis of the liver (classes A and B on the Child-Pugh scale) when taking pantoprazole at a dose of 20 mg / day. T1 / 2 increases to 3-6 hours, AUC increases by 3-5 times, and Cmax – by 1.3 times compared with healthy individuals.
A slight increase in AUC and an increase in Cmax in elderly patients compared with the corresponding data in young patients are not clinically significant.
Contraindications
Dyspepsia of the neurotic genesis of
Children under 18 years of age (efficacy and safety not studied)
Hypersensitivity to pantoprazole or other components of the drug.
Nolpase contains sorbitol, so the drug is not recommended for patients with rare hereditary fructose intolerance.
Caution is advised to prescribe the drug during pregnancy, lactation, liver failure, risk factors for cyanocobalamin deficiency (especially against hypo- and achlorhydria).
Special instructions
Before starting therapy, it is necessary to exclude the presence of a malignant neoplasm (endoscopic control, if necessary with a biopsy – especially with gastric ulcer), because treatment, masking symptoms, may delay the correct diagnosis.
If after 4 weeks of pantoprazole therapy the patient does not have the desired therapeutic effect, he should undergo a second examination.
Like other proton pump inhibitors, pantoprazole can reduce the absorption of cyanocobalamin (vitamin B12) against the background of hypo- and achlorhydria. This should be especially taken into account with prolonged treatment and in patients with risk factors for vitamin B12 deficiency.
Conducting long-term therapy, especially lasting more than 1 year, requires regular monitoring of the patient.
Influence on the ability to drive vehicles and control mechanisms
The drug Nolpaza does not affect the ability to drive a car or other technical means.
Composition
d 1 tablet 22.55 mg, which corresponds to the content of pantoprazole 20 mg
Pantoprazole sodium sesquihydrate 45.1 mg, which corresponds to the content of pantoprazole 40 mg
Excipients:
Mannitol
Crospovidone
Sodium carbonate anhydrous
sporbitol becoming a shell: hypromellose, povidone, titanium dioxide (E171), dye iron oxide yellow (E172), propylene glycol, dispersion Eudragit L30D (copolymer of methacrylic acid and ethyl acrylate (1: 1) dispersion 30%, water, sodium lauryl sulfate, polysorbate-80), talc, macrogol 6000.
Dosage and administration
The drug is taken orally. The Nolpase tablet should be swallowed whole without chewing or breaking, washed down with a small amount of liquid, before meals, usually before breakfast. With a double dose, it is recommended to take the second dose of Nolpaza before dinner.
With GERD, incl. erosive-ulcerative reflux esophagitis and associated symptoms (heartburn, acidic regurgitation, pain when swallowing) mild, the recommended dose is 20 mg / day, moderate and severe – 40-80 mg / day. Relief of symptoms usually occurs within 2-4 weeks. The course of therapy is 4-8 weeks.
For prevention, as well as supporting long-term therapy, 20 mg / day are prescribed. If necessary, the dose is increased to 40-80 mg / day. It is possible to take the drug on demand if symptoms occur.
For erosive and ulcerative lesions of the stomach and duodenum associated with NSAIDs, the recommended dose of Nolpase is 40-80 mg / day. The course of therapy is 4-8 weeks.
For the prevention of erosive lesions against the background of prolonged use of NSAIDs – 20 mg.
For the treatment and prevention of peptic ulcer of the stomach and duodenum, 40-80 mg / day are prescribed. The course of treatment for exacerbation of peptic ulcer of the duodenum is usually 2 weeks, peptic ulcer of the stomach – 4-8 weeks. If necessary, the duration of therapy is increased.
For eradication of Helicobacter pylori (in combination with antibiotics), the recommended dose of Nolpase is 40 mg 2 times a day in combination with two antibiotics, usually the course of anti-Helicobacter therapy is 7-14 days.
With Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion, the recommended starting dose of long-term therapy with pantoprazole is 80 mg / day, divided into 2 doses. In the future, the daily dose can be titrated depending on the initial level of gastric secretion. A temporary increase in the daily dose of pantoprazole to 160 mg is possible in order to adequately control gastric secretion. The duration of therapy is selected individually.
In patients with severely impaired liver function, the dose of pantoprazole should not exceed 40 mg / day. and it is recommended to regularly monitor the activity of liver enzymes, especially with prolonged treatment with pantoprazole. With an increase in the activity of liver enzymes, it is recommended to cancel the drug.
In elderly patients and patients with kidney disease, the maximum daily dose of pantoprazole is 40 mg.
In elderly patients receiving Helicobacter pylori eradication therapy, the duration of therapy usually does not exceed 7 days.
Side effects of
From the hemopoietic organs:
very rarely – leukopenia, thrombocytopenia.
From the digestive system:
often – abdominal pain, diarrhea, constipation, flatulence
infrequently – nausea, vomiting rarely – dry mouth
very rarely – increased activity of liver transaminases and GGT, severe liver damage leading to jaundice with liver failure or without.
On the part of the immune system:
is very rare – anaphylactic reactions,
From the musculoskeletal system:
rarely – arthralgia is very rare – myalgia.
From the side of the central nervous system and peripheral nervous system:
often – headache
infrequently – dizziness, blurred vision (blurred vision)
very rarely – depression.
From the genitourinary system:
is very rare – interstitial nephritis.
Allergic reactions:
infrequently – itching, rash
very rarely – urticaria, angioedema, Stevens-Johnson syndrome, erythema multiforme or Lyell’s syndrome, photosensitivity.
Other:
is very rare – peripheral edema, hyperthermia, weakness, painful tension of the mammary glands, increased triglycerides.
If severe adverse effects develop, discontinue treatment with the drug.
Drug interactions
Nolpase reduces the absorption of drugs whose bioavailability depends on the pH of the stomach and absorbed at acidic pH values (e.g. ketoconazole).
Pantoprazole is metabolized in the liver via the cytochrome P450 enzyme system. The interactions of pantoprazole with drugs that are metabolized by the same system cannot be ruled out. However, no significant interactions with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine, piroxicam, theophylline, and oral contraceptives were found in clinical studies.
Although there were no significant interactions with warfarin in clinical pharmacokinetic studies, there have been several separate reports of a change in MHO. In patients receiving coumarin anticoagulants, simultaneously with pantoprazole, it is recommended to regularly monitor prothrombin time or MHO.
While taking pantoprazole with antacids, no drug interactions have been reported.
Overdose
Symptoms of overdose in humans are not known.
Treatment: no specific antidote exists. In case of an overdose of the drug, accompanied by the usual signs of intoxication, detoxification measures are used. The treatment is symptomatic.
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Prescription
dosage form
tablets
