medicalmeds.eu Medicines H+-K inhibitor +-ATF-azy. Antiulcerous drug. Gasek-20

Gasek-20

Producer: LLC Mepha, Switzerland

Code of automatic telephone exchange: A02BC01

Release form: Firm dosage forms. Capsules.

Indications to use: Peptic ulcer of a stomach. Peptic ulcer of 12 perstny guts. Reflux esophagitis. Zollingera-Ellison's syndrome. Erosive gastritis. Eradikation N. pylori.

General characteristics. Structure:

Active ingredient: омепразол 20 mg

Excipients: sugar, gipromelloz (gidroksipropilmetiltsellyuloz), phosphate sodium dihydrate, silicon dioxide colloid, titanium dioxide (E171), copolymer of methacrylic acid (type C), triethyl citrate, talc.

Structure of a cover of the capsule: the case - titanium dioxide (E171), gelatin, indigotin (E132), gland (III) oxide yellow (E172); a lid - gelatin, titanium dioxide (E171), gland (III) oxide red (E172), gland (III) oxide yellow (E172).

Pharmacological properties:

Inhibitor of the protonew pump. Omeprazol is the weak basis, concentrates and converted into an active form in acid medium of tubules of covering cells where inhibits the fermental protonew pump - H+-K +-ATF-azu and blocks thereby a final stage of secretion of hydrochloric acid. This effect is dozozavisimy and provides highly effective inhibition to both basal, and stimulated secretion of acid, irrespective of irritant type.

Pharmakodinamichesky effects of an omeprazol are caused by its inhibiting effect on secretion of hydrochloric acid.

At administration of drug of Gasek™-20 in a single dose of 1 times / there is a bystry and effective inhibition of secretion of hydrochloric acid during the day and at night. The maximum effect is reached within 4 days of treatment.

At the patients suffering from a peptic ulcer of a duodenum decrease in hydrochloric acid on average of 80% it can be reached during 24 h. In 24 h after administration of drug of Gasek™-20 average decrease in peak of products of acid after stimulation by Pentagastrinum makes about 70%. Administration of drug in a dose of 20 mg brings to rn3 into gastric cavities on average in 17-24 h.

As a result of decrease in secretion of Gasek™-20 hydrochloric acid reduces and normalizes time of influence of acid for a gullet in a dozozavisimy form at the patients suffering from a gastroesophageal reflux.

It is known that 70-95% of all patients suffering from a round ulcer including an ulcer of a duodenum and stomach, are infected with Helicobacter pylori.

Eradikation Helicobacter pylori as a result of treatment by the drug Gasek™-20 in a combination with antibiotics leads to bystry disappearance of symptoms, high level of healing of any mucous defeats and to long-term remission of round ulcers. It reduces risk of emergence of complications, such as gastrointestinal bleedings.

Pharmacokinetics. Omeprazol is kislotolabilny therefore it is made in the form of capsules with pellets, steady against a gastric juice.

Absorption

After reception drug inside омепразол is absorbed in a small intestine during 3-6 h. System bioavailability at reception in a single dose makes 35% and increases to 60% after repeated introduction. Bioavailability does not depend on a concomitant use of food.

Distribution

Linkng with proteins of plasma of an omeprazol – about 95%. At healthy people of Vd makes about 0.3 l/kg. Similar sizes were observed at patients with a renal failure.

At patients of advanced age and patients with a chronic liver failure of Vd it is a little reduced.

Metabolism

Omeprazol is metabolized almost completely in a liver under the influence of fermental system of P450 cytochrome. Metabolism is carried out by polymorphic specific isoenzymes of CYP2C19 (S-Mephenytoinum a hydroxylase). They are responsible for formation of inactive metabolites of a gidroksimeprazol, main metabolite in plasma. Omeprazol competitively inhibits CYP2C19, there is a risk of metabolic interaction between omeprazoly and other substances which are metabolized CYP2C19. This risk increases at slow metabolizator ("polymorphism of Mephenytoinum"; 3-5% of the white population).

Removal

After intake of 80% of a dose the rest - with bile and with a stake is removed in the form of metabolites with urine.

T1/2 of an omeprazol makes 0.5-1 h and does not change during prolonged treatment. The general clearance makes 0.3-0.6 l/min.

Pharmacokinetics in special clinical cases

At patients with a chronic renal failure system bioavailability is not changed.

At patients are raised by abnormal liver functions of AUC value. However administration of drug in a single dose of 1 times / does not lead to any accumulation of an omeprazol.

Indications to use:

— treatment and prevention of a recurrence of a peptic ulcer of a stomach and duodenum;

— gastroesophageal reflux disease;

— Zollingera-Ellison's syndrome;

— GIT erosive cankers owing to use of NPVS;

— the stomach diseases associated with Helicobacter pylori (as a part of complex therapy).

Route of administration and doses:

Peptic ulcer of a duodenum

Гасек™-20 appoint 20 mg in a dose 1 time / Relief of symptoms of an aggravation is done quickly, and treatment of an ulcer usually is done in 2 weeks. If therapy within 2 weeks is insufficiently effective, then treatment is in most cases reached during an additional two-week course of therapy.

At inefficiency of other therapy of Gasek™-20 appoint in a dose 40 mg of 1 times / within 4 weeks.

Peptic ulcer of a stomach, gastroesophageal disease

Гасек™-20 appoint 20 mg in a dose 1 time / Relief of symptoms of an aggravation is done quickly, and at most of patients the ulcer recovers within 4 weeks. If within 4 weeks treatment is inefficient, then it is necessary to continue drug use 4 more weeks.

At inefficiency of other forms of therapy it is recommended to appoint Gasek™-20 in a dose of 40 mg of 1 times / within 8 weeks.

For prevention of a recurrence at patients with a peptic ulcer of a stomach and duodenum

The recommended drug dose - 20 mg of 1 times / If necessary a dose can be increased to 40 mg of 1 times /

The stomach diseases associated with Helicobacter pylori (as a part of complex therapy)

For Helicobacter pylori eradikation at the round ulcer revealed at clinical inspection carry out short-term therapy:

Гасек™-20 in a dose of 20 mg in a combination with amoxicillin of 1 g and klaritromitsiny 500 mg 2, treatment duration - 1 week;

Гасек™-20 in a dose of 20 mg in a combination from klaritromitsiny 250 mg and metronidazole of 500 mg (or Tinidazolum of 500 mg) 2, treatment duration - 1 week;

Гасек™-20 in a dose of 40 mg of 1 times / in a combination with amoxicillin (on 500 mg 3) and metronidazole (on 500 mg 3), treatment duration - 1 week. Treatment can be continued if the patient has a positive take of a research on existence of Helicobacter pylori after short-term therapy within 1 week.

GIT erosive cankers owing to use of NPVS

To the patients who are receiving or not receiving now NPVS, the recommended dose of the drug Gasek™-20 makes 20 mg 1 times / Symptoms of a disease pass quickly and treatment is usually limited for 4 weeks. At insufficient efficiency of therapy within 4 weeks the dose can be increased to 40 mg /

For prevention of a recurrence in case of the round ulcer, gastroduodenal erosion or dispeptic symptoms connected with reception of NPVS the dose of 20 mg of 1 times / is recommended

Gastroesophageal reflux disease

The recommended drug Gasek™-20 dose - 20mg/Symptoms of a disease disappear quickly. At insufficient efficiency of therapy within 4 weeks it is necessary to conduct clinical examination.

Zollingera-Ellison's syndrome

Doses should be selected individually. The recommended initial dose makes 60 mg/Duration of treatment is defined by clinical need. More than at 90% of the patients suffering from a severe form of a disease at whom treatment by other drugs was inefficient successful stabilization of a state at use of drug in doses of doses between 20 mg and 120 mg of an omeprazol was reached in If the dose more than 80 mg / is required, then it should be divided into 2 receptions.

Features of use:

Before purpose of drug it is necessary to exclude a malignancy in case of existence of the following symptoms: considerable inexplicable loss of weight, long vomiting, a dysphagy, a hematemesis or a bloody chair, is suspicion of stomach ulcer. Without preliminary exception of a malignancy treatment can disguise symptoms and will detain diagnosis.

Influence on ability to driving of motor transport and to control of mechanisms

Considering possible side effects, administration of drug of Gasek™-20 can negatively affect ability to control of motor transport and to others potentially dangerous types of activity.

Side effects:

From the alimentary system: dryness in a mouth, an abdominal pain, nausea, vomiting, a meteorism, diarrhea, a lock, stomatitis, gastrointestinal candidiasis, increase in activity of liver enzymes, hepatitis, a liver failure.

From TsNS: headache, dizziness, disturbance of space orientation.

From system of a hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis and pancytopenia.

From a musculoskeletal system: muscle and joints pain and/or myasthenia.

Allergic reactions: skin rash, small tortoiseshell, itch, Quincke's edema.

Others: fervescence.

Interaction with other medicines:

At combined use with other blockers of secretion of hydrochloric acid and antacids bioavailability of a ketokonazol and itrakonazol decreases.

Гасек™-20 it is capable to slow down removal of diazepam and drugs which are metabolized by oxidation in a liver (with the participation of CYP2C19 isoenzyme). Though at use of the drug Gasek™-20 in a dose of 20 mg of 1 times/, Css of Phenytoinum was invariable, it is recommended to carry out monitoring of maintenance of Phenytoinum, and also peroral anticoagulants and to reduce their doses if it is required.

At simultaneous use of concentration of an omeprazol and klaritromitsin in plasma raise.

It is reported that in case of joint purpose of an omeprazol with atazanaviry, concentration of an atazanavir in plasma was reduced.

At joint purpose of the drug Gasek™-20 and a takrolimus increase in concentration of a takrolimus in serum is possible.

Contraindications:

— children's and teenage age up to 18 years;

— hypersensitivity to drug components.

Use of the drug GASEK™-20 at pregnancy and feeding by a breast

Adequate and strictly controlled clinical trials on safety and efficiency of the drug Gasek™-20 at pregnancy it was not carried out. Therefore at appointment pregnant women need care.

Omeprazol is allocated in small amounts with breast milk and deactivated by acid in the newborn's stomach. Therefore it is improbable that administration of drug of Gasek™-20 during breastfeeding will be accorded by any effect on the child.

Overdose:

Symptoms: nausea, vomiting, disturbance of space orientation, abdominal pain, diarrhea, headache. These symptoms also pass passing character independently.

Treatment: if necessary – performing symptomatic therapy.