Lantserol

General characteristics. Structure:

Acting veshchestvo:lansoprazole;

1 capsule contains a lansoprazol, as a part of pellets, in terms of 100% substance of 30 mg;

excipients (as a part of pellets): sakharnyesfer (sucrose, corn starch, the water purified) (0,85-1 mm), sodium lauryl sulfate, Megluminum, a mannitol (Е 421), a gipromelloz (gidroksipropilmetiltsellyuloz), a macrogoal 6000, talc, polysorbate 80, titanium dioxide (Е 171), methacrylate copolymer (type A);

structure of a cover капсулы:желатин.

Pharmacological properties:

Pharmacodynamics. Lansoprazol oppresses activity of H+/K +-ATF-azy a proton pomp in covering cells of a mucous membrane of a stomach. Thus, Lantserol® oppresses a final mode of formation of acid of a gastric juice, reduces quantity and acidity of a gastric juice owing to what the adverse effect of a gastric juice on a mucous membrane decreases.

Extent of oppression is defined by a dose and duration of treatment. Even the single dose of 30 mg of a lansoprazol oppresses secretion of acid of a gastric juice for 70-90%. The beginning of action is observed within 1-2 hours and proceeds within a day.

Pharmacokinetics. Lansoprazol is absorbed in intestines. At healthy volunteers at reception of 30 mg of a lansoprazol the maximum concentration in a blood plasma makes 0,75-1,15 mg/l and is reached within 1,5-2 hours. The maximum concentration in a blood plasma and bioavailability depend on specific features of the patient and do not change depending on the frequency of administration of drug.

Linkng of drug with proteins of a blood plasma makes 98%.

Lansoprazol is brought from an organism with bile and urine (only in the form of metabolites – лансопразолсульфон and гидроксилансопразол), at the same time per day with urine 21% of a dose of drug are removed. The elimination half-life makes 1,5 hours.

The elimination half-life is extended at patients with the expressed abnormal liver functions and at patients aged from 69 years. At patients with renal failures absorption of a lansoprazol practically does not change.

Main physical and chemical svoystva:tverdy gelatin capsules No. 1, case and cover colourless, transparent. Contents of capsules – pellets of white or almost white color.

Indications to use:

– The Dobrokachestvennayapeptichesky yazvazheludka and a duodenum including connected using non-steroidal anti-inflammatory drugs;

– gastroesophageal reflux disease;

– Zollingera-Ellison's syndrome;

– for Helicobacter pylori eradikation (in a combination with antibiotics).

Route of administration and doses:

Primenyatvzrosly inside. Usually the dose makes 30 mg of 1 times a day in 30-40 minutes prior to food, to the prinimatena chewing capsules, washing down 150-200 ml of water. If it is impossible, the capsule it is possible to open and dissolve its contents in a small amount of apple juice (about 1 tablespoon) and to swallow immediately without chewing. The same procedure should be carried out if drug вводитьчерез the nazogastralny probe.

The question of a dosage and term of treatment is solved by the doctor individually, depending on a clinical situation and character of a course of a disease.

The maximum daily dose makes 60 mg, for patients with abnormal liver functions – 30 mg. For patients with Zollingera-Ellison's syndrome of a dose can be increased.

If it is necessary to accept 2 daily doses, the patient has to accept one before a breakfast, and another – before a dinner.

If the patient did not accept drug in due time, it has to accept it as soon as possible. However, if there was a little time before reception of the following dose, to the patient to nelzyaprinimat the passed dose.

Duodenum ulcer

The drug dose for treatment of an active ulcer makes 30 mg of 1 times a day within               2-4 weeks. The dose for treatment of the ulcers caused by reception of non-steroidal anti-inflammatory drugs makes 30 mg of 1 times a day. Treatment lasts                4-8 weeks.

High-quality round ulcer of a stomach

The drug dose for treatment of an active ulcer makes 30 mg of 1 times a day within 8 weeks.

The dose for treatment of the ulcers caused by reception of non-steroidal anti-inflammatory drugs makes 30 mg of 1 times a day within 4-8 weeks.

Gastroesophageal reflux disease

At average and heavy forms the recommended dose – 30 mg of 1 times a day within 4 weeks. If the erosive esophagitis does not recover within 4 weeks, duration of treatment can be twice longer. The dose for long prevention of a recurrence of an erosive esophagitis makes 30 mg of 1 times a day. Safety and efficiency of a maintenance therapy lansoprazoly is confirmed for 12-month reception.

Eradikation Helicobacter pylori

The dose makes 30 mg 2 times a day (before a breakfast and before a dinner). To the patient to neobkhodimoprinimat drug together with antibiotics according to the approved schemes within 1-2 weeks.

Zollingera-Ellison's syndrome

The dose is selected individually so that basal secretion of acid did not exceed             10 mmol/hour. The recommended initial dose makes 60 mg of 1 times a day before a breakfast. If the patient accepts doses more than 120 mg, he should accept the first half of a daily dose before a breakfast, and the second half – before a dinner. Treatment continues before disappearance of clinical indications.

Renal and liver failure

Patients with abnormal liver functions and kidneys of easy or moderate degree do not demand dose adjustment.

Patients with heavy abnormal liver functions should accept the smallest effective doses of drug, but no more than 30 mg a day.

Patients of advanced age

At use of drug there is no need to adjust a dose.

Features of use:

Before purpose of the drug Lantserol® it is necessary to exclude a possibility of malignant new growths in a stomach and a gullet as drug can disguise symptoms and, thus, delay the correct diagnosis therefore before the beginning and after the termination of a course of treatment lansoprazoly it is necessary to carry out endoscopic control with a biopsy.

Due to the content of sucrose, drug is not used at patients with hereditary intolerance of fructose, glucose, a galactose, sucrose and isomaltose.

When carrying out a combination therapy with klaritromitsiny and caution amoxicillin concerning use of these medicines it is necessary to look in instructions on a medical use of a klaritromitsin and amoxicillin, and also it is necessary to consider before use of amoxicillin and a klaritromitsin existence in the anamnesis of reactions of hypersensitivity to penicillin, cephalosporins and other allergens.

At use of antibacterial agents developing of pseudomembranous colitis, sometimes vitally dangerous therefore it is important to consider it in the presence at patients of diarrhea is possible.

At patients with a renal failure of linkng with blood proteins decreases by           1-1,5%.

At patients with a chronic liver failure plasma elimination half-life of blood increases from 1,5 to 3,2-7,2 hours depending on degree of an abnormal liver function. Patients with a heavy liver failure should reduce a drug dose. To begin treatment with a half of the specified dose, gradually increasing to the recommended doses, but no more than 30 mg a day.

Under the influence of a lansoprazol acidity of a gastric juice decreases that leads to increase in risk of development of the gastrointestinal infections caused by opportunistic microorganisms, such as Salmonella and Campylobacter.

Because of limitation of data on safety of use of a lansoprazol as a maintenance therapy lasting more than 1 year it is regularly necessary to carry out ratio assessment risk/advantage for this group of patients.

Patients of advanced age.

Treatment of an ulcer at patients of advanced age practically does not differ from treatment at patients of younger age. Side reactions and laboratory changes at patients of advanced age same, as well as at patients of younger age.

 

Ability to influence speed of response at control of motor transport or work with other mechanisms.

During control of motor transport or work with other mechanisms it is necessary to consider possibility of side reactions from a nervous system and organs of sight.

Side effects:

During treatment it is often reported about such side reactions as an abdominal pain, diarrhea, nausea; most often – about diarrhea. Also in more than in 1% of cases it was reported about a headache.

From cardiovascular sistemy:stenokardiya, cerebrovascular changes, arterial hypertension, arterial hypotension, myocardial infarction, heart consciousness, shock (circular insufficiency), vazodilatation.

From digestive a trakta:anoreksiya, a cardiospasm, a cholelithiasis, a lock, vomiting, a hepatotoxic, jaundice, hepatitis, candidiasis of mucous membranes of a digestive tract, dryness in mouth/thirst, dyspepsia, a dysphagy, an eructation, an ezofagealny stenosis, an ezofagealny ulcer, an esophagitis, discoloration a calla, a meteorism, stomach polyps, a gastroenteritis, colitis, gastrointestinal bleedings, vomiting with blood impurity, increase or a loss of appetite, the raised sialosis, a melena, rectal bleedings, stomatitis, flavoring frustration, a glossitis, pancreatitis, tenesmus, ulcer colitis.

From endocrine sistemy:sakharny diabetes, craw, hyperglycemia/hypoglycemia.

From system of blood and lymphatic system: anemia (including aplastic and hemolitic anemia), hemolysis, agranulocytosis, leukopenia, neutropenia, pancytopenia, thrombocytopenia, eosinophilia, trombotichesky and Werlhof's disease.

From a musculoskeletal system and connecting ткани:артрит / arthralgia, musculoskeletal pain, mialgiya.

From nervous sistemy:azhitation, amnesia, hypererethism, apathy, depression, dizziness/syncope, вертиго, hallucinations, hemiplegia, hostility, fear, decrease libido, nervousness, sleeplessness, drowsiness, tremor, paresthesias, disturbances of thinking, confusion of consciousness.

From respiratory sistemy:odyshka, cough, pharyngitis, rhinitis, infections of upper and lower respiratory tracts (bronchitis, pneumonia), asthma, nasal bleeding, pulmonary bleeding, hiccups.

From skin and hypodermic kletchatki:angionevrotichesky hypostasis, multiformny erythema, toxic epidermal necrolysis, Stephens-Johnson's syndrome, polymorphic erythema, acne, hyperemia of the person, allopecia, itch, rash, urticaria, purpura, petechias, hyperhidrosis, photosensitivity.

From bodies sight chuvstv:pomutneniye, eye pain, defects of fields of vision, sonitus, deafness, average otitis, changes of taste, alalia.

From urinogenital sistemy:interstitsialny nephrite that can lead to a renal failure, formation of stones in kidneys, an ischuria, a glucosuria, a hamaturia, an albuminuria, disturbance of periods, increase in milk glands / a gynecomastia, morbidity of mammary glands, impotence.

The combination therapy with amoxicillin and klaritromitsinom:pr carrying out a combination therapy of a lansoprazol with amoxicillin and klaritromitsiny is not present side reactions, specific, characteristic of a combination therapy. Side reactions which can arise at a combination therapy, characteristic for lansoprazolu, amoxicillin and a klaritromitsin.

The most frequent side reactions at the patients receiving triple therapy (ланcопразол/кларитромицин/амоксициллин) within 14 days is diarrhea, a headache, taste changes. The most frequent side reactions when performing double therapy of a lansoprazol with amoxicillin are diarrhea and a headache. Side reactions are short and do not demand the treatment termination.

Laboratory izmeneniya:povysheniye of level of nuclear heating plant, ALT, alkaline phosphatase, creatinine, globulins, gamaglutamiltranspeptidaza, ratio distortion of albumine and globulins. Also increase/decrease in level of leukocytes, changes of quantity of erythrocytes, a bilirubinemia, an eosinophilia, a lipidemia, increase/decrease in level of electrolytes, increase/decrease in cholesterol, decrease in hemoglobin, increase in level of potassium, urea, increase in level of glucocorticoids, increase in level of lipoproteids of low density, increase/decrease in thrombocytes, increase in level of gastrin, positive test for the occult blood is noted. In urine – an albuminuria, a glucosuria, a hamaturia, emergence of salts.

Patients of norm more than 3 times higher than the upper bound have data on increase in level of enzymes of a liver at the end of treatment lansoprazoly, however jaundice was not noted.

Prochiye:anafilaktoidny reactions, acute anaphylaxis, adynamy, increased fatigue, candidiasis, stethalgia (not always specific), hypostases, fever, a grippopodobny syndrome, an unpleasant smell from a mouth, infections (not always specific), weakness.

Interaction with other medicines:

Lansoprazol, as well as other inhibitors of a proton pomp, reduces concentration of an atazanavir (HIV protease inhibitor) which absorption depends on gastric acidity therefore can influence therapeutic action of an atazanavir and development of resistance to HIV infection. Contraindicated simultaneous use of an atazanavir and lansoprazol.

Lansoprazol can increase in a blood plasma concentration of the drugs which are metabolized CYP3A4 (warfarin, antipyrine, indometacin, an ibuprofen, Phenytoinum, propranolol, Prednisolonum, diazepam, кларитромицин or терфенадин).

The medicines suppressing CYP2C19 (флувоксамин) lead to substantial increase (by 4 times) concentration of a lansoprazol in a blood plasma. At simultaneous use dose adjustment of a lansoprazol is necessary.

The inductors CYP2C19 and CYP3A4 (rifampicin, St. John's Wort grass) can reduce considerably concentration of a lansoprazol in a blood plasma. At simultaneous use dose adjustment of a lansoprazol is necessary.

Lansoprazol causes long oppression of gastric secretion therefore influence of a lansoprazol on bioavailability of drugs for which at absorption value рН is important is theoretically possible (кетоконазол, итраконазол, ethers of ampicillin, iron salt, digoxin).

Clinical manifestations of interaction of a lansoprazol with amoxicillin were not observed.

Sukralfat and antiacid drugs can reduce bioavailability of a lansoprazol because of what лансопразол it is necessary to accept a minimum in 1 hour after use of these drugs.

Clinically significant interaction between lansoprazoly and nonsteroid antiinflammatory medicines is not revealed.

At simultaneous use of a lansoprazol with theophylline (CYP1A2, CYP3A) moderate increase (to 10%) clearance of theophylline is noted, but clinical value of their interactions is improbable. However dose adjustment of theophylline at the beginning or after the treatment termination lansoprazoly is necessary for maintenance of clinically effective concentration of theophylline by the certain patient.

Lansoprazol does not influence pharmacokinetics of warfarin and a prothrombin time.

Increase in MNO and prothrombin time can lead to bleedings and even by a lethal outcome.

At simultaneous use of digoxin and a lansoprazol increase in level of digoxin in a blood plasma is observed.

At simultaneous use of a lansoprazol and takrolimus concentration of a takrolimus in a blood plasma, especially at patients to whom carried out transplantation can increase.

Contraindications:

– Hypersensitivity to a lansoprazol or to any other component of drug;

– simultaneous use with atazanaviry;

– malignant new growths of a digestive tract.

Use during pregnancy or feeding by a breast.

During pregnancy and feeding by a breast drug cannot be used.

In need of drug use feeding by a breast should be stopped.

Children.

Lansoprazol children cannot apply.

Overdose:

There are no messages on overdose cases lansoprazoly.

There are data that the single dose of drug in a dose of 600 mg is not followed by clinical manifestations of overdose, however at overdose strengthening of manifestations of side reactions is possible.

Treatment. The specific antidote does not exist. The hemodialysis is inefficient. For reduction of absorption of drug it is necessary to accept absorbent carbon. In case of reception of an excess dose carry out the symptomatic and supporting treatment.

Storage conditions:

Period of validity 2 years. To store in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in the blister, 1 blister in a pack.