Beta клатинол

General characteristics. Structure:

Active ingredient: 40 mg of a pantoprazol.

Excipients: lactose, starch corn, povidone, methylparaben, propylparaben, magnesium stearate, talc, sodium krokhmalglikolit, titanium dioxide, ferrous oxide yellow, cellulose ацетилфталат.

Active ingredient: 500 mg of a klaritromitsin.

Excipients: cellulose microcrystallic, povidone (PVPK-30), sodium of a kroskarmeloz, magnesium stearate, silicon dioxide colloid anhydrous, gipromelloza, titanium dioxide, quinolinic yellow, macrogoal (PEG-6000).

Active ingredient: 1 g of amoxicillin.

Excipients: cellulose microcrystallic, povidone (PVPK-30), magnesium stearate, dioxide colloid is more waterless than silicon, опадрай white, a macrogoal (PEG-6000), talc.

The combined drug for H.Pylory eradikation.

Pharmacological properties:

Pharmacodynamics. Pharmacological action of a pantoprazol - antiulcerous. It collects in tubules of covering cells of a stomach and is transformed to an active form - cyclic sulphenamide, selectively interacts (forms a covalent bond) with H+-K - Atfaza. Inhibits H+-K - to ATFAZ of covering cells, breaks transfer of ions of hydrogen from covering cell in a gleam of a stomach and blocks a final stage of hydrophilic secretion of hydrochloric acid. Dozozavisimo proceeded suppresses basal and stimulated (regardless of a type of an incentive - acetylcholine, a histamine, gastrin) secretion of hydrochloric acid. Value of an average effective dose at the researches in vivo is varied within 0,2 - 2,4 mg/kg. The maximum effect is shown only in silnokisly (рН 3) Wednesday (at higher values рН remains almost inactive).

It has antibacterial effect vidnosno Helicobacter pylori and promotes manifestation antikhelikobakterny effect of other drugs. The Minimum Inhibiting Concentration (MIC) makes 128 g/l. The therapeutic effect after a single dose occurs quickly and remains during 24 h. Provides bystry reduction of symptomatology and healing of an ulcer of a duodenum. At reception in a dose of 40 mg of value рН> 3 more than 19 h are stored.

Klaritromitsin is a makrolidny antibiotic which has antibacterial activity against many aerobic and anaerobic gram-positive and gram-negative microorganisms, including H. pylori. Klaritromitsin carries out the antibacterial action by oppression of synthesis of protein, communicating with 50S in subunit of a membrane of ribosomes of a microbic cell. The minimum inhibiting concentration (MIK90) of a klaritromitsin and its active metabolite of a 14-gidroksiklaritromitsin concerning H. pylori makes 0,06 mkg/ml.

Pharmacological effect of amoxicillin - antibacterial (bactericidal). It inhibits transpeptidases, breaks synthesis of a peptidoglikan (basic protein of a cell wall) during division and growth, causes a lysis of microorganisms.

Pharmacokinetics. Tablets of a pantoprazol having entero the form, thus, absorption of a pantoprazol begins after the tablet leaves a stomach. It is soaked up quickly and completely. Absolute bioavailability makes 70-80% (average 77%). The maximum concentration in plasma (Cmax) is reached in 2-4 h (on average in 2,7 h). Linkng with proteins of plasma makes 98%. The period poluvyvedeniya1/2) makes 0,9-1,9 h, distribution volume - 0,15 l/kg, clearance (Cl) - 0,1 l/h/kg. Very poorly gets through a blood-brain barrier, cosecretes in breast milk. Reception of antacids or food does not influence area size under a curve "concentration - time" (AUC), Cmax and bioavailability. Pharmacokinetics linear in the range of doses from 10 to 80 mg (in proportion to increase in a dose AUC and Cmax increases). T1/2 and Cl values - dozonezalezhn. It is metabolized in a liver (oxidation, dealkylations, conjugation). Has low affinity concerning system of P450 cytochrome, in metabolism isoenzymes of CYP3A4 and CYP2S19 are attracted preferential. The main metabolites - деметилпантопразол (T1/2 - 1,5 of the h) and 2 sulphated conjugates. It is removed preferential with urine (82%) in the form of metabolites, in a small amount is in Calais. Does not kumulirut. T1/2 at patients with cirrhosis increases up to 9 h, at a renal failure increases slightly, but T1/2 of the main metabolite reaches 3 h AUC and Cmax slightly above in the senior age group.

Klaritromitsin at intake is quickly and rather fully soaked up. Food slows down absorption, significantly without influencing bioavailability. After a single dose 2 peaks of serumal concentration are registered. The second peak is caused by ability to concentrate in a gall bladder with the subsequent gradual or bystry release. In plasma contacts serum proteins (more than 90%). About 20% of the accepted dose are oxidized in a liver with formation of the main active metabolite of a 14-gidroksiklaritromitsin at once. Biotransformation is catalyzed by enzymes tsitokhromny the P450 complex. Well gets into liquids and body tissues, forming concentration which by 10 times exceed level in a blood plasma. T1/2 at reception of a dose of 500 mg makes 7-9 h. The rest is removed with urine in not changed look to 30%, - in the form of metabolites.

Amoxicillin at intake quickly and almost is completely soaked up, creating Cmax in 1-2 h. It is stable in acid medium, meal does not influence absorption. Linkng with proteins of a blood plasma - about 17%. Easily passes gistogematichesky barriers, except not changed hematoencephalic, and gets into the majority of fabrics and bodies the hydrothorax, lungs, a mucous membrane of intestines, female generative organs, liquid of a middle ear, a gall bladder and bile (collects in therapeutic concentration in peritoneal liquid, urine, contents of skin blisters, at normal function of a liver), fruit fabrics. T1/2sostavlyaet 1-1,5 of h. At a renal failure of T1/2 it is extended to 12,6 h, depending on clearance of creatinine. It is partially metabolized with formation of inactive metabolites. 50 - 70% are removed by kidneys in not changed look by canalicular excretion (80%) and glomerular filtering (20%), 10-20% - to cookies. In a small amount it is allocated with breast milk.

Indications to use:

The stomach ulcer and a duodenum associated with H.Pylori.

Route of administration and doses:

The adult set on 1 tablet of a pantoprazol, a tablet of a klaritromitsin, an amoxicillin tablet 2 times a day (in the morning and in the evening) to food, daily. Treatment duration - 7 days.

Features of use:

Before an initiation of treatment it is necessary to exclude malignant diseases of a gullet and stomach (symptomatic improvement can delay the correct diagnosis and treatment).

Klaritromitsin with care appoint against the background of drugs which are metabolized by a liver (it is recommended to measure their concentration in blood). In case of a combination with warfarin or other indirect anticoagulants it is necessary to control a prothrombin time. At heart diseases in the anamnesis the concomitant use from terfenadiny, tsizapridy, astemizoly is not recommended.

With care appoint at abnormal liver functions.

It is not necessary to appoint drug to patients with organic neurologic frustration.

It is important to provide existence of pseudomembranous colitis at patients who complain of diarrhea after reception of antibacterial drugs.

During treatment it is necessary to control function of kidneys, a liver and a hemogenesis.

Administration of drug does not influence ability to manage vehicles, to work with potentially dangerous mechanisms, and also to be engaged in activity which needs vigilance and coherence of actions.

Side effects:

Tablets of a pantoprazol.

From the alimentary system: diarrhea, it is rare - dryness in a mouth, the increased appetite, an eructation, nausea, vomiting, a meteorism, abdominal pains, a lock, increase in activity of transaminases, a gastrointestinal carcinoma (isolated case).

From a nervous system and sense bodys: a headache, it is rare - an adynamy, dizziness, drowsiness, sleeplessness; in some cases - nervousness, a depression, a tremor, paresthesias, photophobia, vision disorders, a sonitus.

From urinogenital system: in isolated cases - a hamaturia, hypostases, impotence.

From integuments: in isolated cases - an alopecia, an acne, exfoliative dermatitis.

Allergic reactions: seldom - rash, urticaria, an itch, a Quincke's disease.

Others: seldom - a hyperglycemia, a mialgiya in isolated cases - fever, a giperlipoproteinemiya, a hypercholesterolemia.

Tablets of a klaritromitsin.

From the alimentary system: nausea, vomiting, change of flavoring feelings, pains in a stomach, diarrhea, pseudomembranous colitis, stomatitis, a glossitis, increase in activity of enzymes of a liver.

From a nervous system and sense bodys: dizziness, headache, concern, fear, sleeplessness, nightmares.

Allergic reactions: small tortoiseshell, Stephens-Johnson's syndrome, anaphylactoid reactions.

Amoxicillin tablets.

From the alimentary system: stomatitis, a glossitis, oral cavity candidiasis, nausea, vomiting, diarrhea, dysbacteriosis, pains in the field of an anus; pseudomembranous or hemorrhagic colitis.

From a nervous system and sense bodys: excitement, concern, sleeplessness, confusion of consciousness, change of behavior, headache, dizziness.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): tachycardia, moderate increase in level of transaminases in blood, tranzitorny anemia, a Werlhof's disease, an eosinophilia, a leukopenia, a neutropenia and an agranulocytosis.

From respiratory system: the complicated breath.

From urinogenital system: intersticial nephrite, vagina candidiasis.

From a musculoskeletal system: convulsive reactions, joint pains.

From integuments: exfoliative dermatitis, multiformny exudative erythema, Stephens-Johnson's syndrome, makulopapulezny rash.

Allergic reactions: acute anaphylaxis, small tortoiseshell, Quincke's edema.

Interaction with other medicines:

Pantoprazol can reduce rn-dependent absorption of a ketokonazol and other medicines. Compatible to drugs which are metabolized with the participation of fermental system of P450 cytochrome (Phenazepamum, diazepam, digoxin, theophylline, carboazepine, diclofenac, Naproxenum, piroxicam, Phenytoinum, warfarin, nifedipine, метопролол, ethanol). Does not influence efficiency of hormonal contraceptives.

Simultaneous use of a klaritromitsin and theophylline can lead to increase in concentration of the last in plasma. Simultaneous use of a klaritromitsin and terfenadin increases concentration of the last in plasma which can lead to prolongation of an interval of QT and cause disturbance of a heart rhythm. Simultaneous use of a klaritromitsin and peroral anticoagulants, such as warfarin, can exponentiate activity of the last. Simultaneous use of a klaritromitsin and carboazepine, cyclosporine, Phenytoinum, Disopyramidum, lovastatin, Valproatum, tsizaprid, Pimozidum, astemizol, digoxin can lead to increase in concentration of the listed drugs in plasma.

Klaritromitsin increases concentration in blood of drugs what are metabolized in a liver with the participation of enzymes of the tsitokhromny P450 complex: warfarin and other indirect coagulants, carbamazepine, theophylline, an astemizol, a tsizaprid, a triazolam, midazolam, cyclosporine, digoxin, alkaloids of horns, etc., reduces absorption of a zidovudine.

Amoxicillin reduces effect of peroral contraceptive drugs which contain estrogen, reduces clearance and increases toxicity of a methotrexate. Strengthens digoxin absorption. Excretion is slowed down probenetsidy, Sulfinpyrazonum, acetylsalicylic acid, indometacin, oksifenbutazony, by phenylbutazone and others preparatm which suppress a tubulyarna secretion. Antibacterial activity decreases bacteriostatic chemotherapeutic means and antacids, increases - aminoglycosides and metronidazole.

Contraindications:

Hypersensitivity to a pantoprazol, a klaritromitsina, amoxicillin, a serious illness of a liver, a digestive tract disease in the anamnesis (especially the colitis connected using antibiotics), a renal failure, a porphyria, allergic diathesis, bronchial asthma, a pollinosis, an infectious mononucleosis, a lymphoid leukosis, pregnancy, a lactation, age up to 18 years.

Overdose:

Overdose of a pantoprazol. Symptoms: are not described.

Treatment: at suspicion on overdose performing the supporting and symptomatic therapy is recommended. Dialysis is not effective.

Overdose of a klaritromitsin. Symptoms: reactions from digestive tract (nausea, vomiting, diarrhea) are possible. The immediate gastric lavage and a symptomatic treatment is necessary. The hemodialysis and dialysis do not lead to considerable change of level of a klaritromitsin in blood.

Amoxicillin overdoses. Symptoms: nausea, vomiting, diarrhea, disturbance of water and electrolytic balance.

Storage conditions:

To store in unavailable to children, the dry place at a temperature not above 30 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

On 2 tablets of a pantoprazol, 2 tablets of a klaritromitsin and 2 tablets of amoxicillin in a tape from aluminum foil. On 7 tapes in a cardboard pack.