Description
Latin name
Nolpaza
enteric-coated release form
enteric-coated
packaging 14 pcs
Pharmacological action
Nolpaza – proton pump inhibitor.
Pharmacodynamics
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 food intake does not affect the AUC, Cmax and bioavailability, only a change in the onset of the drug is observed.
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. a lot more, than T1 / 2 of pantoprazole itself. In chronic renal failure (including those on hemodialysis), dose changes are not required. T1 / 2 – 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 and ulcerative lesions of the stomach and duodenum associated with taking NSAIDs
peptic ulcer of the stomach and duodenum (treatment and prevention)
eradication Helicobacter pylori in combination with two antibiotics
l Zol syndrome and other
syndrome Zol increased gastric secretion.
Contraindications
hypersensitivity to pantoprazole or other components of nolpase
the drug contains sorbitol, therefore it is not recommended for persons with rare hereditary fructose intolerance
dyspepsia of neurotic
genesis of children under 18 years of age (efficacy and safety.
Precautions: pregnancy, lactation, liver failure, risk factors for deficiency of cyanocobalamin (vitamin B12), especially against the background of hypo- and achlorhydria.
Use during pregnancy and lactation
Experience with pantoprazole in pregnant women is limited. During pregnancy and during lactation, it can be used only if the positive effect for the mother justifies the possible risk to the fetus and baby.
There is no data on the release of pantoprazole with breast milk.
Composition
1 tablet and it contains: Active substance
: pantoprazole sodium sesquihydrate 45.10 mg (corresponding to pantoprazole – 40 mg)
Excipients: mannitol, crospovidone, sodium carbonate, sorbitol, anhydrous calcium stearate
Sheath: hypromellose povidone titanium dioxide (E171) dye iron oxide yellow (E172) propylene glycol methacrylic acid and ethyl acrylate copolymer (1: 1) 30% dispersion (dispersion Eudragit L30D, in addition to methacrylic acid and ethyl acrylate copolymer and water, contains lauryl sulfate as sodium emulsifiers , 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, acid regurgitation, pain when swallowing: mild: recommended dose – 1 tablet Nolpazy 20 mg per day
moderate and severe degree: recommended dose – 1-2 tablets Nolpazy 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 prevention, as well as supporting long-term therapy, 20 mg / day are taken (1 Nolpase tablet, 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 NSAIDs: the recommended dosage is 1-2 tablets of 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 duodenal ulcer is usually 2 weeks, gastric ulcer – 4-8 weeks. If necessary, the duration of therapy is increased.
Eradication of Helicobacter pylori (in combination with antibiotics): the recommended dose is 1 tablet of Nolpase (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 Nolpase tablets of 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 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 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 decreases 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 interactions with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine, piroxicam, theophylline, and peromyramine were found in clinical studies.
Although no significant interactions were detected with warfarin in clinical pharmacokinetic studies, several separate reports of MHO change were noted. Patients receiving coumarin anticoagulants concomitantly with pantoprazole should be monitored regularly for prothrombin time or MHO.
No drug interactions have been reported with pantoprazole co-administered with antacids.
overdose
Symptoms: overdoses are unknown in humans.
Treatment: No specific antidote exists. In case of overdose of the drug accompanied by the usual signs of intoxication, detoxification measures are used. Treatment is symptomatic.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C.
Expiration
5 Chron
Deystvuyuschee substances
Pantoprazole
pharmacy terms and conditions for prescription
dosage form
dosage form
tablets
KRKA-RUS LLC, Slovenia
