Description
Release form
tablets
Packing
56 pcs
Pharmacological action of
Nolpase inhibits the enzyme H + -K + -ATPase (proton pump) in the parietal cells of the stomach, thereby blocking the final stage of hydrochloric acid synthesis. 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 the drug in a dose of 20 mg, the effect of pantoprazole occurs within the first hour, the maximum effect is achieved after 2 2.5 hours. It does not affect the motility of the gastrointestinal tract. After discontinuation of the drug, secretory activity is fully restored after 3-4 days.
Pharmacokinetics
Pantoprazole is rapidly absorbed from the gastrointestinal tract, Cmax in plasma is 1 1.5 μg / ml and is reached 2 2.5 hours after ingestion, while its value remains constant with repeated administration. 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.
Plasma Protein Binding – About 98%. The volume of distribution is approximately 0.15 l / kg and the clearance is 0.1 l / h / kg. Pantoprazole is almost completely metabolized in the liver. It is an inhibitor of the CYP2C19 enzyme system. The half-life (T1 / 2) is 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, determined in blood serum and in urine, is desmethyl pantoprazole, which is conjugated to sulfate. T1 / 2 of desmethyl pantoprazole – about 1.5 hours, i.e. much more than T1 / 2 of pantoprazole itself. In chronic renal failure (i.e. including those on hemodialysis) no change in dosage is required. T1 / 2 is short, as in healthy individuals. Very small amounts of pantoprazole can be dialyzed.
In patients with cirrhosis (classes A and B according to the Child-Pugh classification) 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.
Indications
gastroesophageal reflux disease (GERD), incl. erosive-ulcerative reflux esophagitis and symptoms associated with GERD: heartburn, acid regurgitation, pain when swallowing
erosive-ulcerative lesions of the stomach and duodenum associated with taking NSAIDs
gastric ulcer and duodenal ulcer disease combination with two antibiotics
Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.
Contraindications
hypersensitivity to pantoprazole or other components of the
drug contains sorbitol, therefore, it is not recommended for persons with rare hereditary fructose intolerance
dyspepsia of the neurotic origin of
children under 18 years of age (efficacy and safety have not been studied).
Precautions: pregnancy, lactation, liver failure, risk factors for deficiency of cyanocobalamin (vitamin B12), especially against the background of hypo- and achlorhydria.
Pregnancy and lactation
Nolpase is contraindicated in pregnancy and lactation
Composition
1 tablet contains:
Active ingredient: pantoprazole sodium 40 mg
Aux powerful substances: mannitol crospovidone sodium carbonate anhydrous calcium sorbitol stearate
Shell: hypromellose povidone titanium dioxide (E171) dye iron oxide yellow (E172) propylene glycol methacrylic acid and ethyl acrylate copolymer (1: 1) 30% dispersion (dispersion of Eudragacrylate and L30D acid and ethacrylate and water, contains sodium lauryl sulfate (0.7%, calculated on the dry matter in the dispersion) and polysorbate 80 (2.3%, calculated on the dry matter in the dispersion), talc, macrogol 6000
Dosage and administration
Inside, the tablet should not be chewed and broken. Swallow the tablet whole with a little liquid before meals, usually before breakfast. With a double dose, it is recommended to take the second dose of the drug before dinner.
GERD, incl. erosive and ulcerative reflux esophagitis and associated symptoms: heartburn, sour regurgitation, pain when swallowing:
– mild: recommended dose – 1 table. Nolpases of 20 mg per day
– moderate and severe: the recommended dose is 1-2 tablets. Nolpases at 40 mg per day (40 80 mg / day). Relief of symptoms usually occurs within 2-4 weeks. The course of therapy is 4-8 weeks. For prophylaxis, as well as supporting long-term therapy, 20 mg / day are taken (1 tab. Nolpases, 20 mg each), if necessary, the dose is increased to 40 80 mg / day. It is possible to take the drug “on demand” in case of symptoms.
Erosive-ulcerative lesions of the stomach and duodenum associated with the use of NSAIDs: the recommended dosage is 1-2 tablets. Nolpase 40 mg (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 each.
Peptic ulcer of the stomach and duodenum (treatment and prevention) – appoint 40 80 mg / day. The course of treatment for exacerbation of peptic ulcerno duodenal ulcer is usually 2 weeks, gastric ulcer – 4-8 weeks. If necessary, the duration of therapy is increased.
Helicobacter pylori eradication (in combination with antibiotics): the recommended dose is 1 tablet. Nolpases (40 mg) 2 times a day in combination with two antibiotics, usually the course of anti-Helicobacter therapy is 7-14 days.
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 (2 tablets of Nolpase 40 mg) per 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 older people and patients with kidney disease, the maximum daily dose of pantoprazole is 40 mg. In elderly people receiving Helicobacter pylori eradication therapy, the duration of therapy usually does not exceed 7 days.
Side effects
From the hemopoietic organs: very rarely – leukopenia, thrombocytopenia.
From the digestive system: often – abdominal pain, diarrhea, constipation, flatulence infrequently – nausea, vomiting rarely – dry mouth is very rare – increased activity of hepatic transaminases and gamma-glutamintransferase (GGT), severe liver damage leading to jaundice with liver failure or without.
On the part of the immune system: very rarely – anaphylactic reactions, including anaphylactic shock.
From the musculoskeletal system: rarely – arthralgia very rarely – myalgia.
From the central and peripheral nervous system: often – headache infrequently – dizziness, blurred vision (blurred vision).
Mental disorders: very rarely – depression.
From the genitourinary system: very rarely – interstitial nephritis.
Allergic reactions: infrequently – itching and rash are very rare – urticaria, angioedema, Stevens-Johnson syndrome, polymorphic erythema or Lyell syndrome, photosensitivity.
General disorders: very rarely – peripheral edema, hyperthermia, weakness, painful tension of the mammary glands, increased triglycerides.
Drug Interaction
Nolpase reduces the absorption of drugs whose bioavailability depends on the pH of the stomach and is absorbed at acidic pH values (eg ketoconazole). pantoprazole is metabolised in the liver by the cytochrome P450 enzyme system. Interactions of pantoprazole with drugs that are metabolized by the same system cannot be excluded. However, no significant interaction with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine, piroxicam, theophylline, and peroraminalin was found in clinical studies.
Although no significant interaction was found in clinical pharmacokinetic studies when co-administered with warfarin, several separate reports of MHO change were noted. Patients receiving coumarin anticoagulants concomitantly with pantoprazole are advised to regularly monitor PV or MHO.
No drug interactions have been reported with pantoprazole co-administered with antacids.
Storage Conditions
At a temperature not exceeding 30 ° C.
Shelf life
3 years
Deystvuyushtee substance
Pantoprazole
Terms and conditions
prescription
dosage form
tablets
Possible product names
Nolpaza tablets 40 mg 56 pcs.
