Золопент

General characteristics. Structure:

Active ingredient: pantoprazole; 1 tablet contains a pantoprazol of sodium of sexivihydrat, is equivalent to a pantoprazol of 40 mg.

Auxiliary the veshchestva:natriya a carbonate anhydrous, attracts (Е 421), кросповидон, hydroxypropyl cellulose, calcium stearate, oydragit L30D55, triethyl citrate, sodium lauryl sulfate, titanium dioxide (Е 171), ferrous oxide yellow (Е 172), talc, Opadry 03F58750 covering white.

Pharmacological properties:

Pharmacodynamics. Pantoprazol is a blocker of gastric secretion, it oppresses activity of H+/K+-Atfazu in covering cells of a stomach and thus blocks a final phase of secretion of hydrochloric acid. It leads to reduction of level of basal secretion irrespective of the irritation nature. Shows antibacterial activity concerning Helicobacter pylori and promotes manifestation of antikhelikobakterny effect of other drugs. The therapeutic effect after a single dose occurs quickly and remains for 24 hours.

Pharmacokinetics. It is quickly and completely absorbed after intake. Absolute bioavailability makes 77%. The maximum concentration is reached in 2–4 hours. Linkng with proteins of plasma makes 98%. An elimination half-life – about 1 hour. Very poorly gets through a blood-brain barrier. It is metabolized in a liver. It is removed preferential with urine (82%) in the form of metabolites, in a small amount it is observed in Calais. Does not kumulirut. The elimination half-life at patients with cirrhosis increases till 7-9 o'clock, with a liver failure – increases slightly, but the elimination half-life of the main metabolite reaches 2–3 hours.

Indications to use:

- Reflux esophagitis of average and heavy degree. Eradikation Helicobacter pylori at patients with the round ulcers caused by this microorganism in a combination with the corresponding antibiotics.
- Duodenum ulcer.
- Stomach ulcer.
- At Zollingera-Ellison's syndrome and other morbid hyper secretory conditions.

Route of administration and doses:

Treatment reflux esophagitis of average and heavy degree.
The recommended dose for children over 12 years and adults makes 1 tablet of Zolopent of 40 mg once a day. In some cases the dose can be doubled (2 tablets of Zolopent of 40 mg a day), especially in the absence of effect of use of other drugs.
At adult patients with stomach ulcer and a duodenum and with a positive take on Helicobacter pylori the microorganism eradikation needs to reach by means of a combination therapy. Depending on sensitivity of microorganisms for the purpose of an eradikation of H. pylori at adults such therapeutic combinations can be applied:
a) 1 tablet of Zolopent of 40 mg 2 times a day
+ 1000 mg of amoxicillin 2 times a day
+ 500 mg of a klaritromitsin 2 times a day;
b) 1 tablet of Zolopent of 40 mg 2 times a day
+ 500 mg of metronidazole 2 times a day
+ 500 mg of a klaritromitsin 2 times a day
c) 1 tablet of Zolopent of 40 mg 2 times a day
+ 1000 mg of amoxicillin 2 times a day
+ 500 mg of metronidazole 2 times a day
If the combination therapy is not shown, for example, at patients with a negative take on Helicobacter pylori, for monotherapy of stomach ulcer and a duodenum drug of Zolopent the recommended dose makes 1 tablet of Zolopent 40 mg of 1 times in days. In some cases the dose can be doubled (2 tablets of Zolopent of 40 mg in days), especially in the absence of effect of use of other drugs.
For prolonged treatment of a syndrome of Zollingera-Ellison and other morbid hyper secretory conditions the initial daily dose makes 80 mg (2 tablets of Zolopent on 40 mg). If necessary the dose is titrated further, raising or reducing it, depending on indicators of gastric secretion. The dose which exceeds 80 mg in days needs to be distributed on two receptions. Perhaps temporary increase in a dose over 160 mg of a pantoprazol, but only for time necessary for adequate control of secretion of acid.
Duration of treatment of a syndrome of Zollingera-Ellison and other morbid hyper secretory conditions depends only on clinical need.
At patients with heavy abnormal liver functions the dose can be lowered to 1 tablet of Zolopent of 40 mg of 1 times in 2 days. Besides, at such patients it is necessary to control the level of liver enzymes. In case of its increase, treatment by drug of Zolopent needs to be stopped.
Patients of advanced age and patients with renal failures are not recommended to exceed a daily dose of 40 mg of a pantoprazol. An exception – a combination therapy, which purpose – an eradikation of H. рylori when patients of advanced age have to receive a usual daily dose of a pantoprazol (1 tablet of Zolopent of 40 mg 2 times in days) during 1 week.

General instructions.
Золопент tablets, resistant to a gastric juice, take for 1 h till a breakfast whole, without chewing and without crushing, washing down with water. At a combination therapy which purpose there is an eradikation of H. рylori the second pill of Zolopent is taken before a dinner. The combination therapy is carried out, as a rule, for 7 days, but it can be prolonged up to 2 weeks. If for therapy further treatment pantoprazoly is shown, it is necessary to consider recommendations concerning dosing at stomach ulcer and a duodenum.
Duodenal ulcers, as a rule, cure within 2 weeks. If two weeks are not enough, treatment can be expected within the next 2 weeks.
Treatment of stomach ulcers and a reflux esophagitis, as a rule, requires 4 weeks. If it is not enough, treatment can be expected within the next 4 weeks.

Features of use:

Before an initiation of treatment and after it it is necessary to exclude malignant diseases of a gullet and stomach as treatment can disguise symptomatology and delay the correct diagnosis. The diagnosis of a reflux disease has to be confirmed endoscopic. It is not recommended to appoint Zolopent the patient with not ulcer dyspepsia. At elderly patients and at patients with renal failures it is not recommended to exceed a dose of 40 mg/days. At a heavy renal failure the mode of dosing needs to be modified – on 1 tablet every other day, under control of level of liver enzymes (at its increase drug needs to be cancelled immediately).
In the presence of alarming symptoms (essential loss of body weight, vomiting, a dysplasia, vomiting with blood, anemia, a melena), existence of stomach ulcer the zlokachestvennost as treatment pantoprazoly can mask symptoms of a malignant ulcer has to be excluded and defer establishment of the diagnosis.
Further researches have to be caused if symptoms remain at adequate treatment.

Ability to influence the speed of reactions at control of motor transport or other mechanisms.
During treatment at some patients emergence of side reactions from a nervous system therefore it is necessary to be careful at control of motor transport or work with difficult mechanisms is possible.

Use during pregnancy or feeding by a breast.
Experience of use of Zolopent during pregnancy and feeding by a breast is absent therefore it is not necessary to appoint it during these periods.
In need of Zolopent's use in the period of a lactation feeding by a breast should be stopped.

Children. Do not apply.

Side effects:

Undesirable effects on the frequency of emergence classify by such categories: often (> 1/100 and <1/10), sometimes (> 1/1000 and <1/100), it is rare (> 1/10000 and <1/1000), is very rare (<1/10000, including isolated cases).
- From blood: leukopenia, thrombocytopenia.
- From a digestive tract: often – pain in epigastric area, diarrhea, lock meteorism; sometimes – nausea, vomiting; seldom – dryness in a mouth.
- General frustration: very seldom – peripheral hypostases.
- From a liver: very seldom – increase in level of liver enzymes (transaminases, &gama;-ГТ), triglycerides, fervescence, intersticial nephrite and heavy gepatokletochny frustration which leads to jaundice or bezpechenochny insufficiency.
- From immune system: very seldom – anaphylactic reactions, including an acute anaphylaxis.
- From skin: sometimes – allergic reactions (an itch, skin rashes); very seldom – a small tortoiseshell, an angioedema, an erythema multiformny, photosensitivity, Lay¾ll's syndrome.
- From a musculoskeletal system: seldom – an arthralgia; very seldom – a mialgiya.
- From a nervous system: often – a headache; sometimes – dizziness, a vision disorder (zatumanennost); very seldom – depressions.
- From an urinary system: very seldom – intersticial nephrite.

Interaction with other medicines:

Drug of Zolopent can reduce absorption of drugs which bioavailability depends from рН a stomach (for example, a ketokonazola).
Pantoprazol is metabolized in a liver by means of system of enzymes of P450 cytochrome. Interaction of a pantoprazol with other drugs which are metabolized by means of the same system is not excluded. Carrying out special researches with the majority of such means did not reveal clinically significant interactions (in particular, with carbamazepine, caffeine, diazepam, diclofenac, ethanol, glibenclamide, metoprololy, Naproxenum, nifedipine, fenprokumony, Phenytoinum, piroxicam, theophylline, warfarin and oral contraceptives).
Interaction with antacids which were appointed at the same time is not revealed.
Researches on studying of interaction of a pantoprazol with at the same time priznachenny certain antibiotics were conducted (klaritromitsiny, metronidazole, amoxicillin). Clinically significant interactions between these drugs are not revealed.
It is proved that use of an atazanavir of 300 mg / a ritonavira of 100 mg with omeprazoly () or an atazanavira of 400 mg with lansoprazoly (60 mg disposable) causes 40 mg of 1 times in days in healthy volunteers essential to reduction of bioavailability of an atazanavir. Absorption of an atazanavir depends from рН. Therefore inhibitors of a proton pomp, including пантопразол, should not be applied along with atazanaviry.

Contraindications:

Hypersensitivity to drug components. Hepatitis and cirrhosis which are followed by a heavy liver failure. Drug of Zolopent should not be used for a combination therapy which purpose is the eradikation of H. рylori, at patients with a renal or liver failure of average or heavy severity. Pantoprazol, as well as other inhibitors of a proton pomp, it is contraindicated to apply with atazanaviry. Period of pregnancy and lactation. Children's age.

Overdose:

Symptoms: hypoactivity, ataxy and tremor. At suspicion on overdose it is recommended to carry out symptomatic therapy. Carrying out dialysis is not shown.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 14 tablets in the blister; on 1 blister in cardboard packaging No. 14. On 10 tablets in the blister; on 3 blisters in cardboard packaging No. 30 (10 x 3).