Пилобакт AM

General characteristics. Structure:

Active agent: кларитромицин - 500 mg
Excipients: cellulose microcrystallic, povidone, magnesium stearate, sterinovy acid, the talc purified silicon dioxide colloid, croscarmellose sodium.
Material of a film cover: a gipromelloza, a hypro rod, propylene glycol, sorbitan monooleate, titanium dioxide, dye quinolinic yellow, the vanillin, talc purified.
Ink for a text: black Opacode S-1-27794 ink (metilirovanny IMS 74 OP alcohol, 47.5% shellac solution in metilirovanny IMS 74 OP alcohol, dye ferrous oxide black, N - butyl alcohol, propylene glycol, the water purified).
Active agent: amoxicillin the trihydrate of-592.856 mg equivalent to amoxicillin -
500 mg
 Excipients: sodium lauryl sulfate, silicon dioxide colloid, kroskarmelloza, cellulose microcrystallic, magnesium stearate.
Capsule cover:
Lid: dye diamond blue, dye azoruby, dye quinolinic yellow, titanium dioxide, methylparahydroxybenzoate, пропилпарагидроксибензоат, sodium lauryl sulfate, gelatin.
Case: dye sunset yellow, dye quinolinic yellow, titanium dioxide, methylparahydroxybenzoate, пропилпарагидроксибензоат, sodium lauryl sulfate, gelatin.
Ink for a text: dehydrated alcohol, butyl alcohol, shellac, dye ferrous oxide black, strong solution of ammonia, propylene glycol.
Active agent: омепразол 20 mg
 Excipients: Non Pareil Seeds (the granule from sucrose and corn starch covered with a kishechnorastvorimy cover), lactose, starch corn, Mannitolum, povidone, talc purified sodium lauryl sulfate, sodium hydrophosphate (anhydrous).
Material of a kishechnorastvorimy cover: gipromeloza phthalate, dichloromethane, isopropanol, diethyl phthalate, titanium dioxide, a cover of an empty solid gelatin capsule of No. in size 2 with a dark blue lid and the transparent pink case. 
 Capsule cover:
Lid: diamond blue, кармоизин (azoruby), gelatin, methylparahydroxybenzoate, пропилпаргидроксибензоат.
Case: кармоизин (azoruby), gelatin, methylparahydroxybenzoate, пропилпаргидроксибензоат.
Description
Klaritromitsin, tablets coated: light yellow color, an oval form, biconvex, film coated, with the text of "CXT 500" printed with black ink on one party.
Amoxicillin, capsules: solid gelatin capsules, the 0 el size (diameter of a cover of the capsule 7,57 – 7,71mm, diameter of the case of the capsule 7,27 – 7,41 mm, capsule 11,22 cover length – 12,30mm, capsule 19,70 case length – 20,70mm), the case of yellow color, a lid of brown color with the text printed with black ink "500" on a lid and the case. Capsule contents white to almost white granulated powders/pellets.

Omeprazol of the capsule: solid gelatin capsules with "lock" No. in size 2 with a lid of dark blue color and the transparent pink case, the containing white or almost white spherical granules covered with a kishechnorastvorimy cover.

Pharmacological properties:

The triple therapy including омепразол кларитромицин and amoxicillin allows to reach high percent of an eradikation of Helicobacter pylori (85-94%).
Omeprazol oppresses secretion of gastric acid at the expense of specific inhibition of H+ K +-Atfazy - the enzyme which is in membranes of covering cells of a mucous membrane of a stomach. Reduces basal and stimulated secretion irrespective of the irritant nature. After a single dose of drug inside action of an omeprazol comes within the first hour and continues within 24 hours, the maximum of effect is reached in 2 hours. After the termination of administration of drug secretory activity is completely recovered in 3 – 5 days.
Klaritromitsin - an antibiotic from group of macroleads, semi-synthetic derivative erythromycin A. Has antimicrobic effect which is connected with suppression of synthesis of protein by interaction with 50S a ribosome subunit of a microbic cell. Pylori is effective concerning a large number of gram-positive, gram-negative aerobic and anaerobic microorganisms, including N. The metabolite which is formed in an organism 14-gidroksiklaritromitsin also has the expressed antimicrobic activity.
Amoxicillin – semi-synthetic penicillin, possesses bactericidal action, has a broad spectrum of activity. Antimicrobic action is connected with inhibition of synthesis of a peptidoglikan (basic polymer of a cell wall) during division and growth. Pylori has the expressed activity in relation to N. N.'s resistance of Pylori to amoxicillin is shown seldom.
The combination of amoxicillin and klaritromitsin has the potentiated antimicrobic effect in relation to N. Pylori.

Pharmacokinetics. All three drugs which are Pilobakt's part of AM possess good absorption at oral administration.
Omeprazol is quickly soaked up after intake, and its bioavailability makes 30-40%. Meal does not exert impact on bioavailability of an omeprazol. The maximum concentration of drug in plasma (Cmax) is reached in 0,5 - 1 hour. Communication with proteins of plasma makes 90%. It is almost completely metabolized in a liver. The main way of removal - with urine (80%).
Klaritromitsin is quickly absorbed from digestive tract. Absolute bioavailability of 250 mg of a klaritromitsin makes about 50%. Meal slightly slows down the beginning of absorption of a klaritromitsin and formation of a 14-gidroksiklaritromitsin, but does not influence bioavailability. At reception on an empty stomach peak serumal concentration are reached within 2 hours after oral administration and make 0,6 and 0,7 mkg/ml for a klaritromitsin and its main metabolite. The elimination half-life of a klaritromitsin makes 3-4 hours. Klaritromitsin is widely distributed in an organism. Concentration of a klaritromitsin in fabrics exceeds that in serum. Communication with proteins makes from 42% to 70%. It is allocated with kidneys and with a fecal masses (20-30% in not changed form, the rest in the form of metabolites). Co-administration of a klaritromitsin and omeprazol improves pharmacokinetic properties of a klaritromitsin: average Cmax value increases by 10%, the minimum concentration - for 15% in comparison with the same indicators at monotherapy klaritromitsiny. Concentration of a klaritromitsin in mucous a stomach at its co-administration with omeprazoly is also increased.
Amoxicillin is quickly absorbed from digestive tract. Meal does not influence amoxicillin absorption. Bioavailability of amoxicillin makes 75 - 90%. Drug is quickly distributed in body tissues. The elimination half-life makes 1-1,5 hours. Communication with proteins of 20%. About 60% of the accepted dose are removed with urine in not changed look, the insignificant quantity is removed with kalom/

Indications to use:

Eradikatsionny therapy of N. of Pylori at a peptic ulcer of a 12-tiperstny gut.

Route of administration and doses:

Each strip containing tablets and capsules of the Pilobakt®AM set is expected one day of treatment and consists of two parts: red with a text "morning" and blue with a text "evening".
In morning reception before food it is necessary to accept part contents "morning" completely (one capsule of an omeprazol, one tablet of a klaritromitsin and two capsules of amoxicillin). In evening reception before food it is necessary to accept part contents "evening" completely (one capsule of an omeprazol, one tablet of a klaritromitsin and two capsules of amoxicillin).
Tablets and capsule cannot be broken and chewed, they should be swallowed entirely. Duration of treatment makes 7 days.

Features of use:

Before therapy it is necessary to exclude existence of malignant process (especially at stomach ulcer) since treatment, masking symptomatology, can delay statement of the correct diagnosis.
With care appoint against the background of reception of the medicines which are metabolized a liver. In case of joint appointment with warfarin or other indirect anticoagulants it is necessary to control a prothrombin time.
At heart diseases in the anamnesis the concomitant use with terfenadiny, tsizapridy, astemizoly is not recommended.

Side effects:

From digestive organs: dysbacteriosis, diarrhea or a lock, nausea, vomiting, a meteorism, an abdominal pain, dryness in a mouth, taste disturbances, stomatitis, tranzitorny increase in activity of "hepatic" enzymes in plasma, the abnormal liver function, is rare – a pseudomembranous coloenteritis.
From a nervous system: headache, dizziness, excitement, drowsiness, sleeplessness, ataxy, paresthesias, depression, confusion of consciousness, hallucination, epileptic reactions, peripheral neuropathy.
From a musculoskeletal system: muscular weakness, mialgiya, arthralgia.
From system of a hemopoiesis: leukopenia, neutropenia, thrombocytopenia, Werlhof's disease, anemia.
From integuments: itch; seldom – skin rash, in some cases – a photosensitization, a multiformny exudative erythema, an alopecia.
Allergic reactions: small tortoiseshell, Quincke's disease, bronchospasm and acute anaphylaxis.
Others: tachycardia, intersticial nephrite, vision disorder, peripheral hypostases, sweating strengthening, fever, gynecomastia.

Interaction with other medicines:

Co-administration of theophylline and klaritromitsin is followed by increase in concentration of theophylline.
Co-administration of a klaritromitsin with terfinadiny increases concentration of the last and can lead to lengthening of an interval of QT.
Co-administration of a klaritromitsin with indirect anticoagulants can exponentiate action of the last.
At co-administration with klaritromitsiny levels of carbamazepine, cyclosporine, Phenytoinum, Disopyramidum, lovastatin, Valproatum, tsizaprid, Pimozidum, astemizol, digoxin can be increased.
Omeprazol can slow down elimination of Phenytoinum, diazepam, warfarin, and also to influence absorption of a ketokonazol, ampicillin and salts of iron at the expense of inhibition of secretion of acid in a stomach.
At simultaneous purpose of amoxicillin with oral contraceptives is possible decrease in effect of the last.

Contraindications:

• Hypersensitivity to an omeprazol, a klaritromitsin or amoxicillin, and also antibiotics of group of macroleads;
• The combined use with tsizapridy, Pimozidum, astemizoly and terfenadiny is forbidden (see the section "Interaction with Other Medicines");
• Pregnancy;
• Lactation period;
• Porphyria;
• Children's age;
• Renal and/or liver failure.

Storage conditions:

To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets and capsules set (кларитромицин - tablets film coated 500 mg, amoxicillin – capsules of 500 mg, омепразол – capsules kishechnorastorimy 20 mg): on 2 tablets of a klaritromitsin, 4 capsules of amoxicillin, 2 capsules of an omeprazol in one planimetric bezjyacheykovy packaging from aluminum foil (strip). Seven strips in a cardboard pack with the application instruction.