Нольпаза®

General characteristics. Structure:

Active agent: a pantoprazola of sodium sexivihydrat of 22,55 mg 45,10 mg (corresponds to a pantoprazol — 20 and 40 mg)  
excipients: Mannitolum; кросповидон; sodium carbonate anhydrous; sorbitol; calcium stearate  
cover: gipromelloza; povidone; titanium dioxide (E171); dye ferrous oxide yellow (E172); propylene glycol; methacrylic acid and ethyl acrylate copolymer (1:1); 30% dispersion (dispersion of Eudragit of L30D, in addition to methacrylic acid and ethyl acrylate of copolymer and water, contains lauryl sulfate in quality of emulsifiers of sodium (0,7%, are calculated on dry matter in dispersion) and polysorbate 80 (2,3%, are calculated on dry matter in dispersion), talc, a macrogoal 6000  

Description of a dosage form

Oval, slightly biconvex tablets, film coated light yellowish-brown color.

Look on a break: weight from white till light-yellowish-brown color with a rough surface with a layer of a cover of light yellowish-brown color.

Pharmacological properties:

Pharmacodynamics. Inhibits H+-K+-Atfazu enzyme (the proton pump) in covering cells of a stomach, thereby blocking a final stage of synthesis of hydrochloric acid. It leads to decrease in level of basal and stimulated secretion of hydrochloric acid, irrespective of the irritant nature. After a single dose of drug inside in a dose of 20 mg action of a pantoprazol comes within the first hour, the maximum of effect is reached in 2–2,5 h. Does not influence motility of a GIT. After the termination of administration of drug secretory activity is completely recovered in 3–4 days.

Pharmacokinetics. Pantoprazol is quickly absorbed from a GIT, Cmax in plasma makes 1–1,5 mkg/ml and is reached in 2–2,5 h after intake, at the same time its value remains to constants at multiple dose. Bioavailability of drug makes 77%. The concomitant use of food does not influence an indicator of AUC, Cmax and bioavailability; only change of the beginning of effect of drug is observed.

Linkng with proteins of plasma — about 98%. The volume of distribution makes about 0,15 l/kg, and clearance — 0,1 l/h/kg. Pantoprazol is almost completely metabolized in a liver. Is inhibitor of the fermental CYP2C19 system. An elimination half-life (T1/2) — 1 h. Because of specific linkng of a pantoprazol with a proton pomp of T1/2 covering cells does not correlate with a duration of therapeutic effect.

Removal of metabolites (80%) — is preferential through kidneys; the rest is removed with bile. The main metabolite defined in blood serum and in urine — десметилпантопразол which is conjugated with sulfate. T1/2 of a desmetilpantoprazol is about 1,5 h, i.e. it is much more, than T1/2 of the pantoprazol. At a chronic renal failure (including at being on a hemodialysis) change of doses of drug is not required. T1/2 — short, as at healthy faces. Very small quantities of a pantoprazol can be dialyzed.

At patients with cirrhosis (classes A and B on Child-Pugh classification) at reception of a pantoprazol in a dose of 20 mg/days of T1/2 increases to 3–6 h, AUC increases by 3–5 times, and Cmax — by 1,3 times in comparison with healthy faces.

Small increase in AUC and increase in Cmax at patients of advanced age in comparison with the relevant data at patients of younger age are not clinically significant.

Indications to use:

gastroesophageal reflux disease (GERB), including erosive and ulcer reflux esophagitis and symptoms associated with GERB: heartburn, regurgitation acid, pain when swallowing;

the erosive cankers of a stomach and duodenum connected with reception of NPVS;

peptic ulcer of a stomach and duodenum (treatment and prevention);

Helicobacter pylori eradikation in a combination with two antibiotics;

Zollingera-Ellison's syndrome and other morbid conditions connected with the increased gastric secretion.

Route of administration and doses:

Inside, the tablet should not be chewed and broken. To swallow a tablet entirely, washing down with a small amount of liquid, before food, usually before a breakfast. At double reception the second dose of drug is recommended to be accepted before a dinner.

GERB, including erosive and ulcer reflux esophagitis and the associated symptoms: heartburn, regurgitation acid, pain when swallowing:

- easy degree: the recommended dose — 1 tab. of Nolpaza on 20 mg a day;

- average and heavy degree: the recommended dose — 1–2 tab. of Nolpaza on 40 mg a day (40–80 mg/days). Relief of symptoms comes usually during 2–4 weeks. The course of therapy makes 4–8 weeks. For prevention, and also as the supporting long therapy accept 20 mg/days (1 tab. of Nolpaza on 20 mg), if necessary raise a dose to 40–80 mg/days. Administration of drug is possible "on demand" at emergence of symptoms.

The erosive cankers of a stomach and duodenum connected with reception of NPVS: the recommended dosage — 1–2 tab. of Nolpaza of 40 mg (40–80 mg/days). A therapy course — 4–8 weeks. For prevention of erosive defeats against the background of prolonged use of NPVS — on 20 mg.

Peptic ulcer of a stomach and duodenum (treatment and prevention) — appoint 40–80 mg/days. The course of treatment at an aggravation of a peptic ulcer of a duodenum usually makes 2 weeks, a peptic ulcer of a stomach — 4–8 weeks. If necessary duration of therapy increases.

Eradikation Helicobacter pylori (in a combination with antibiotics): the recommended dose — 1 tab. of Nolpaza (40 mg) 2 times a day in a combination with two antibiotics, usually a course of antikhelikobakterny therapy makes 7–14 days.

Zollingera-Ellison's syndrome and other morbid conditions connected with the increased gastric secretion: the recommended starting dose of long therapy pantoprazoly — 80 mg (2 tab. of Nolpaza on 40 mg) in days, divided into 2 receptions. Further the daily dose can be titrated depending on the initial level of gastric secretion. Perhaps temporary increase in a daily dose of a pantoprazol up to 160 mg for the purpose of adequate control of gastric secretion. Duration of therapy is selected individually.

At patients with heavy abnormal liver functions the dose of a pantoprazol should not exceed 40 mg/days and it is regularly recommended to control activity of "hepatic" enzymes, especially at prolonged treatment pantoprazoly. At increase in activity of "hepatic" enzymes it is recommended to cancel drug.

Elderly persons and patients with diseases of kidneys have the maximum daily dose of a pantoprazol — 40 mg. At the elderly persons receiving eradikatsionny therapy of Helicobacter pylori, therapy duration usually does not exceed 7 days.

Features of use:

Before therapy it is necessary to exclude existence of a malignant new growth (endoscopic control, if necessary with a biopsy — especially at stomach ulcer) since treatment, masking symptomatology, can delay statement of the correct diagnosis. If in 4 weeks of therapy pantoprazoly the patient has no desirable medical effect, it has to undergo repeated inspection. As well as other inhibitors of a proton pomp, пантопразол absorption of cyanocobalamine (B12 vitamin) against the background of hypo - and achlorhydrias can reduce. Especially it should be considered at prolonged treatment and at patients with risk factors of deficit of B12 vitamin.

Performing long therapy, especially lasting more than 1 year, demands regular observation of the patient.

Influence on ability to drive the car or to perform the works demanding the increased speed of physical and mental reactions. Drug does not influence ability to drive the car or other technical means.

Side effects:

Side effects according to the WHO classification are given:

From bodies of a hemopoiesis: very seldom — a leukopenia, thrombocytopenia.

From the alimentary system: often — an abdominal pain, diarrhea, locks, a meteorism; infrequently — nausea, vomiting; seldom — dryness in a mouth; very seldom — increase in activity of hepatic transaminases and gamma glutaminetransferase (GGT), the severe damages of a liver leading to jaundice with a liver failure or without.

From immune system: very seldom — anaphylactic reactions, including an acute anaphylaxis.

From a musculoskeletal system: seldom — an arthralgia; very seldom — a mialgiya.

From the central and peripheral nervous system: often — a headache; infrequently — dizziness, a vision disorder (indistinct sight).

Mental disorders: very seldom — a depression.

From urinogenital system: very seldom — intersticial nephrite.

Allergic reactions: infrequently — an itch and rash; very seldom — a small tortoiseshell, a Quincke's disease, Stephens-Johnson's syndrome, a polymorphic erythema or a Lyell's disease, a photosensitization.

General frustration: very seldom — peripheral hypostases, a hyperthermia, weakness, painful tension of mammary glands, increase in level of triglycerides.

At development of heavy undesirable effects treatment by drug should be stopped.

Interaction with other medicines:

Nolpaza reduces absorption of drugs which bioavailability depends from рН environments of a stomach and soaking up at acid values рН (for example кетоконазол).

Pantoprazol is metabolized in a liver by means of fermental system of P450 cytochrome. It is impossible to exclude interactions of a pantoprazol with medicines which are metabolized by the same system. Nevertheless, in clinical trials significant interaction with digoxin, diazepam, diclofenac, ethanol, Phenytoinum, glibenclamide, carbamazepine, caffeine, metoprololy, Naproxenum, nifedipine, piroxicam, theophylline and oral contraceptives was not revealed.

Though at simultaneous use with warfarin in clinical pharmacokinetic trials significant interaction was not revealed, several separate messages on MHO change are noted. At the patients receiving coumarinic anticoagulants along with pantoprazoly it is recommended to control PV or MHO regularly.

At a concomitant use of a pantoprazol with antacids of any medicinal interaction it is not registered.

Contraindications:

Hypersensitivity to a pantoprazol or other components of drug;

drug contains sorbitol therefore it is not recommended to persons with rare hereditary intolerance of fructose;

dyspepsia of neurotic genesis;

children's age up to 18 years (efficiency and safety are not studied).

With care: pregnancy, the lactation period, a liver failure, risk factors of deficit of cyanocobalamine (B12 vitamin), especially against the background of hypo - and achlorhydrias.

Use at pregnancy and feeding by a breast

Experience of use of a pantoprazol for pregnant women is limited. At pregnancy and during feeding by a breast it is possible to use only if the positive effect for mother justifies possible risk for a fruit and the child.

There are no data on allocation of a pantoprazol with breast milk.

Overdose:

Overdose symptoms at the person are unknown.

Treatment: symptomatic, the specific antidote does not exist. In case of the overdose of drug which is followed by usual symptoms of intoxication apply disintoxication actions.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children. Period of validity of drug of Nolpaz 3 years.

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover, 20 mg and 40 mg. On 14 pieces in the blister; in a cardboard pack 1 or 2 blisters.