Nolpaza (Pantoprazole)

Active substance :

pantoprazole sodium sesquihydrate; 

Excipients:

 mannitol;

crospovidone;

sodium carbonate anhydrous;

sorbitol;

calcium stearate; 

Shell:

hypromellose; povidone; titanium dioxide (E171); yellow iron oxide dye (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 sodium lauryl sulfate as emulsifiers (0.7%, calculated on the dry matter in the dispersion) and polysorbate 80 (2.3%, calculated on the dry matter in dispersion), talc, macrogol 6000;

Nolpase inhibits the H ⁺ -K ⁺ -ATPase enzyme (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, C _max  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%. Concomitant food intake does not affect AUC, C _max  and bioavailability; there is only a change in the onset of the drug.

Plasma protein binding is 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 (T _1/2 ) is 1 hour. Due to the specific binding of pantoprazole to the proton pump of parietal cells, T _1/2  does not correlate with the duration of the therapeutic effect.

Excretion of metabolites (80%) - mainly through the kidneys; the remainder is excreted in the bile. The main metabolite, determined in blood serum and in urine, is desmethyl pantoprazole, which is conjugated to sulfate. T _1/2  desmethyl pantoprazole - about 1.5 hours, i.e. much more than T _1/2  of pantoprazole itself. In chronic renal failure (including those on hemodialysis), dose changes are not required. T _1/2  is short, as in healthy individuals. Very small amounts of pantoprazole can be dialyzed.

In patients with cirrhosis of the liver (classes A and B according to the Child-Pugh classification) when taking pantoprazole at a dose of 20 mg / day, T _1/2  increases to 3-6 hours, AUC increases by 3-5 times, and C _max  - by 1 3 times compared with healthy individuals.

A slight increase in AUC and an increase in C _max  in elderly patients compared with the corresponding data in young patients are not clinically significant.

• gastroesophageal reflux disease (GERD), including 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 the intake of NSAIDs;
• peptic ulcer of the stomach and duodenum (treatment and prevention);
• Helicobacter pylori eradication in combination with two antibiotics;
• Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.

• hypersensitivity to pantoprazole or other components of the drug;
• the drug contains sorbitol, therefore, it is not recommended for persons with rare hereditary fructose intolerance;
• dyspepsia of neurotic origin;
• children under 18 years of age (efficacy and safety have not been studied).

With caution: pregnancy, lactation, liver failure, risk factors for deficiency of cyanocobalamin (vitamin B ₁₂ ), especially against the background of hypo- and achlorhydria.

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 hepatic transaminases and gamma-glutamintransferase (GGT), severe liver damage leading to jaundice with or without liver failure.

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, impaired vision (blurred vision).

Mental disorders: very rarely - depression.

From the genitourinary system: very rarely - interstitial nephritis.

Allergic reactions: infrequently - itching and rash; very rarely - urticaria, angioedema, Stevens-Johnson syndrome, polymorphic erythema or Lyell's syndrome, photosensitivity.

General disorders: very rarely - peripheral edema, hyperthermia, weakness, painful tension of the mammary glands, increased triglycerides.

Nolpase reduces the absorption of drugs whose bioavailability depends on the pH of the stomach and absorbed at acidic pH values ​​(for example, ketoconazole).

Pantoprazole is metabolized in the liver through 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 interaction with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine, piroxicam, theophylline, and oral contraceptives was found in clinical studies.

Although there was no significant interaction 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 PV or MHO.

With the simultaneous administration of pantoprazole with antacids, no drug interaction has been recorded.

Inside, the tablet should not be chewed and broken. Swallow the tablet whole with a little liquid before meals, usually before breakfast. When taking twice a second dose of the drug is recommended to be taken before dinner.

GERD, including erosive-ulcerative reflux esophagitis and associated symptoms: heartburn, acid regurgitation, pain when swallowing:

- mild: the recommended dose is 1 tablet. 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 ulcer of the duodenum is usually 2 weeks, peptic ulcer of the stomach - 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 elderly 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.

Before starting therapy, it is necessary to exclude the presence of a malignant neoplasm (endoscopic control, if necessary with a biopsy - especially with a stomach 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 B ₁₂ ) against the background of hypo- and achlorhydria. This should be especially taken into account with long-term treatment and in patients with risk factors for vitamin B ₁₂ deficiency .

Conducting long-term therapy, especially lasting more than 1 year, requires regular monitoring of the patient.

Influence on the ability to drive a car or perform work that requires an increased speed of physical and mental reactions. The drug does not affect the ability to drive a car or other technical means.

tablets