Амоксил® DT

General characteristics. Structure:

Active ingredient: amoxicillin;

1 tablet contains trihydrate amoxicillin, in terms of amoxicillin, 500 mg; auxiliary a veshchestva:tsellyuloza microcrystallic, the cellulose dispersed кросповидон, vanillin, fragrance tangerine, fragrance a lemon, saccharin, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Амоксил® DT - an antibiotic of a broad spectrum of activity of group of semi-synthetic penicillin. Works bakteritsidno.

The following table illustrates data on sensitivity of in vitro of some clinically significant microorganisms to amoxicillin.
Activity                        the Average minimum inhibiting concentration (M_S)
 
in vitro                          of 0,01-0,1                                      mkg/ml 0,1-1 mkg/ml 1-10 mkg/ml

Gram-positive                               Streptococci S.                          aureus S. faecalis
            microorganisms (B) of Streptococci    (отрицательныйпо b-laktamaze)
                                    S. pneumonie,
                                                     C.welchii B. anthracis
                                                     C. tetani L.subtilis
                                                                   L. monocytogenes 
Gram-negative                                                      N. gonorrhoeae H. influenzae E. coli 
                                                                                N. meningitidis B.pertussis P. mirabilis
microorganisms                                                                                                 of S. typhi
                                                                                                                          S. sonnei
                                                                                                                       V.cholerae.
  

Amoxicillin is inactive concerning the microorganisms producing b-lactamazu, for example such kakPseudomonas and Enterobacter strains. Level of resistance of microorganisms, sensitive to amoxicillin, can be variable in different territories.

Pharmacokinetics. Absorption. After oral administration of drug amoxicillin is soaked up quickly and almost completely (85-90%), drug acid resisting. Meal practically does not influence drug absorption. The maximum concentration of active agent in a blood plasma is reached in 1-2 hours. After intake of 375 mg of amoxicillin the maximum concentration of active agent in a blood plasma makes 6 mkg/l. When doubling (or decrease twice) the maximum concentration in a blood plasma also varies drug doses (increases or decreases) twice.

Distribution. About 20% of amoxicillin contact proteins of a blood plasma. Amoxicillin gets into mucous membranes, a bone tissue, intraocular liquid, a phlegm in therapeutic effective concentration. Concentration of amoxicillin in bile exceeds its concentration in blood by 2-4 times. In amniotic liquid and funic vessels concentration of amoxicillin makes 25-30% of its level in a blood plasma of the pregnant woman. Amoxicillin badly diffuses in cerebrospinal fluid, however at an inflammation of a meninx (for example at meningitis) concentration in cerebrospinal fluid makes about 20% of concentration in a blood plasma.

Metabolism. Amoxicillin is partially metabolized, the majority of its metabolites are inactive concerning microorganisms.

Removal. Amoxicillin eliminirutsya preferential by kidneys, about 80% - by canalicular excretion, 20% - by glomerular extraction. About 90% of amoxicillin eliminirut in 8 hours, 60-70% are removed in not changed look by kidneys. In the absence of renal failures the elimination half-life of amoxicillin makes 1-1,5 hours. At premature, newborn children and babies aged up to 6 months the elimination half-life of amoxicillin makes 3-4 hours.

At a renal failure (the clearance of creatinine is equal or less than 15 ml/min.) the elimination half-life of amoxicillin increases and reaches at an anury 8,5 hours.

The elimination half-life of amoxicillin does not change at an abnormal liver function.

Indications to use:

The infections caused by microorganisms, sensitive to medicine:

−органов breath;

−органов urinogenital system;

−органов digestive tract;

−кожи and soft tissues.

Use during pregnancy or feeding by a breast.

Limited data concerning use of amoxicillin during pregnancy confirm lack of undesirable impact on the fruit/newborn. Drug during pregnancy it is possible to appoint advantage/risk after careful assessment of a ratio.

Amoxicillin gets in insignificant quantity into breast milk therefore the giperchuvstvitelnosti of the child who is nursed cannot exclude risk of development. For treatment it is necessary to stop feeding by a breast.

Children.

Drug is used to children of 1 year (in this dosage form).

Route of administration and doses:

Drug is accepted irrespective of meal. The tablet can be swallowed entirely or to chew, having washed down with a glass of water; it is also possible to part in water (in 20 ml - ½ glasses), the sweetish suspension having lemon and tangerine taste is formed.

Dosing. In case of infectious and inflammatory diseases easy and moderate severity it is recommended to accept:

- to adults and children 10 years are more senior: 500-750 mg 2 times a day or 500 mg 3 times a day;
- children are 3-10 years old - in a dose of 250 mg 3 times a day;

- to children of 1-3 years of-250 mg 2 times a day or 125 mg 3 times in сутки*.

Usually daily dose of drug for children makes 30 mg/kg/days, distributed on 2-3 receptions.

For receiving a dosage of 250 mg it is necessary to halve a tablet.

* In case of need receiving a smaller dosage it is necessary to apply amoxicillin in other dosage form.

At treatment of chronic diseases, a recurrence, infections of a heavy current administration of drug is recommended: the adult appoint 750-1000 mg 3 times a day, to children - to 60 mg/kg/days (divided into 3 receptions).

Use duration. In case of infections easy and moderate severity drug is accepted within 5-7 days. However in case of the infections caused by a streptococcus, duration of treatment has to make not less than 10 days.

At treatment of chronic diseases and local infectious defeats of a dose of drug have to be defined by a clinical picture of a disease.

Administration of drug needs to be continued within 48 hours after disappearance of symptoms of a disease.

Patients with renal failures. To patients with renal failures at clearance of creatinine lower than 10 ml/min. reduce a dose of drug by 15-50%.

Patients with abnormal liver functions. The abnormal liver function does not influence a drug elimination half-life.

Features of use:

Serious and sometimes lethal cases of hypersensitivity (anaphylactic reactions) are observed at the patients who are on penicillinic therapy (such reactions are frequent at patients who had hypersensitivity cases). Treatment by the drug Amoksil® DT in this case needs to be stopped and replaced with other corresponding treatment. Treatment of symptoms of anaphylactic reaction, for example, immediate administration of adrenaline, steroids (intravenously) and emergency treatment of respiratory insufficiency can be required.

At patients with the known heavy allergic reactions emergence of undesirable reactions is probable.

There can be a cross hypersensitivity and cross resistance between penicillin and cephalosporins.

As well as in a case with other antibiotics of a broad spectrum of activity, there can be superinfections.

Developing of the heavy diarrhea characteristic of pseudomembranous colitis is recommended to be considered the basis for acceptance of the appropriate measures. It is necessary to be careful using drug when developing hemorrhagic colitis or reaction of hypersensitivity.

At use of high doses of drug it is necessary to use enough liquid for prevention of a crystalluria which can be caused by amoxicillin.

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

Data on influence on speed of response at control of motor transport or work with other mechanisms are not established, however it is necessary to consider a possibility of development of undesirable effects from a nervous system.

Interaction with other medicines and other types of interactions.

Probenetsid, phenylbutazone, оксифенбутазон, to a lesser extent - acetylsalicylic acid and Sulfinpyrazonum, suppress canalicular secretion of drugs of a penicillinic row that leads to increase in an elimination half-life and concentration of amoxicillin in a blood plasma.

Simultaneous use of amoxicillin and oral contraceptives is connected with cases of bleeding and decrease in efficiency of contraceptives.

Simultaneous use with Allopyrinolum does not increase the frequency of skin reactions unlike Allopyrinolum combination to ampicillin.

Preparatybakteriostatichesky action: antibiotics of a tetracycline row, macroleads, chloramphenicol can neutralize bactericidal effect of amoxicillin.

Perhaps parallel use of amoxicillin and aminoglycosides (synergy effect).

Side effects:

Often (³1%, <10%):

From a digestive trakta:diareya, nausea.

From outside kozhi:kozhny rash, an itch in the field of an anus.

Infrequently (³0,1%, <1%):

From a digestive trakta:rvot.

From kozhi:krapivniyets and itch.

From kidneys and urinary sistemy:interstitsialny nephrite.

Seldom (³0,01%, <0, 1%):

From a digestive tract: pseudomembranous colitis, hemorrhagic colitis.

From system krovi:gemolitichesky anemia, thrombocytopenia.

Very seldom (≤ 0,01%):

Sostorona of a digestive tract: intestines candidiasis, antibiotikoassotsiirovanny colitis (including pseudomembranous colitis and hemorrhagic colitis) and superficial decolouration of teeth.

From outside kozhi:multiformny erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis, violent or exfoliative dermatitis and acute generalized exanthematous пустулез.

From system of a krovi:leykopeniye (including a heavy neutropenia and an agranulocytosis), and also lengthening of bleeding and a prothrombin time. These manifestations are reversible on condition of the treatment termination.

From kidneys and urinary sistemy:interstitsialny nephrite, crystalluria.

From an immune sistemy:kak for all antibiotics - heavy allergic reactions, including a Quincke's disease, an anaphylaxis, a serum disease and an allergic vasculitis.

From gepatobiliarny sistemy:gepatit, cholestatic jaundice, moderate increase in concentration of liver enzymes (nuclear heating plant, ALT).

From nervous a sistemy:giperaktivnost, dizziness and spasms (in cases of an impaired renal function or in overdose cases).

Infections and инвазии:кандидоз skin and mucous membranes.

Contraindications:

Hypersensitivity to amoxicillin and another beta лактамным to antibiotics, medicines of a penicillinic and tsefalosporinovy row, and also to drug excipients; infectious mononucleosis and leukemoid tests of lymphatic type.

 

Overdose:

Simptomy:narusheny functions of a digestive tract - nausea, vomiting, diarrhea; disturbance of water and electrolytic balance can be a consequence of vomiting and diarrhea.

The crystalluria chances sometimes leading to a renal failure. Lecheniye:sleduyet to cause vomiting or to carry out a gastric lavage then to accept absorbent carbon and an osmotic purgative. It is necessary to support water and electrolytic balance.

Amoxicillin is not removed by means of a hemodialysis. The specific antidote is unknown.

Storage conditions:

Period of validity. 1 year. To store in original packaging at a temperature not over 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 2 blisters in a pack.