Amoklav-375

General characteristics. Structure:

Active ingredients: 250 mg or 500 mg of amoxicillin, 125 mg of clavulanic acid.

Excipients: microcrystallic cellulose, magnesium stearate, colloid silicon dioxide, sodium glikolit starch, TabcoatTC-1709 Mvbely, talc, propylene glycol, диметикон.

Semi-synthetic beta лактамный antibiotic of a wide range of antibacterial action.

Pharmacological properties:

Pharmacodynamics. Amoxicillin has a wide range of antibacterial activity against many gram-positive and gram-negative microorganisms. The mechanism of action consists in inhibition of biosynthesis of mukopeptid of a cell wall. Amoxicillin is exposed to destruction by beta lactamelements therefore  the microorganisms producing beta lactamelements do not enter a range of its antibacterial activity. Clavulanic acid - a beta lactam, has ability to inactivate a wide range beta лактамаз, enzymes which usually produce microorganisms, resistant to penicillin and cephalosporins. In particular, it has high activity against clinically significant plasmid beta лактамаз with which medicinal resistance is often connected, but is less effective concerning chromosomal beta лактамаз 1 type. Presence of clavulanic acid at structure Amoklava protects amoxicillin from destruction by beta lactamelements and expands a range of its antibacterial activity with inclusion in it of microorganisms, usually resistant to other penicillin and cephalosporins.

Thus, Amoklav has properties of an antibiotic with a wide range of bactericidal action and inhibitor beta лактамаз. Амоклав it is effective concerning the following microorganisms:

- Gram-positive aerobes: Bacillus anthracis, Corynebacteriumspecies, Enterococcusfaecalis, Enterococcusfaecium, Listeriamonocytogenes, Nocardiaasteroids, Staphylococcusaureus, Coagulasenegativestaphylococci (including Staphylococcusepidermidis), Streptococcusagalactiae, Streptococcuspneumonia, Streptococcuspyogenes, Streptococcusspecies, Streptococcusviridans;

- Anaerobe bacterias: Clostridium species, Peptococcus species, Peptostreptococcus species;

- Gram-otritsatelnyeaeroba: Bordetella pertussis, Brucella species, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Helicobacter pylori, Klebsiella species, Legionella species, Moraxella catarrhalis (Branhamella catarrhalis), Neisseria gonorrhoeae, Neisseria meningitides, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, Salmonella species, Shigella species, Vibrio cholerae, Yersinia enterocolitica;

- Anaerobe bacterias: Bacteroides species vklyuchayabacteroides fragilis), Fusobacterium species;

- Others: Borrelia burgdorferi, Chlamydiae, Leptospira icterohaemorrhagiae, Treponema pallidum

Pharmacokinetics. Both components Amoklava are completely dissolved in water at physiological PH values, quickly and well soaked up at intake. Absorption Amoklava is optimum on condition of his reception at the beginning of food.

Amoxicillin and clavulanic acid have no high ability to contact proteins of plasma. Only about 25% of clavulanic acid and about 18% of amoxicillin of the general content of drugs in plasma are connected with proteins. Clavulanate in trace quantities and amoxicillin are defined in breast milk. However, the children who are on breastfeeding have only a risk of a sensitization without other negative impacts.

Amoxicillin and clavulanic acid get through a placenta. However, there are no data on a negative impact on reproductive function and about harm for a fruit.

Elimination. As well as at all penicillin, at amoxicillin the main way of elimination renal, whereas at clavulanate a renal and extrarenal way of removal. After a single dose in one tablet about 60%-70% of amoxicillin and about 40%-65% of clavulanic acid within the first 6 hours it is allocated with urine in not changed look.

Amoxicillin is partially excreted in urine in the form of inactive penitsillovy acid in the quantity equivalent to 10%-25% of an initial dose.

Clavulanic acid is extensively metabolized in an organism to 2,5-digidro-4-(2 hydroethyl) - 5-oxo-1 N-pirol-3-karboksilovoy acids and 1-amino-4gidroksi-butane-2-one and emitted with urine and excrements, and also in the form of carbonaceous dioxide through expired air.

Indications to use:

Амоклав it is applied to treatment of the bacterial infections caused by sensitive microorganisms including:

- Upper respiratory tract infections (including infections of an ear, throat, nose), for example, recurrent tonsillitis, sinusitis, average otitis. These infections most often are caused by Streptococcus pneumonia, Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes.

- Lower respiratory tract infections, for example, an acute bronchitis and an exacerbation of chronic bronchitis, share pneumonia and bronchial pneumonia which usually are caused by Streptococcus pneumonia, Haemophilus influenzae and Moraxella catarrhalis.

- Infections of an urogenital path, for example, cystitis (especially recurrent and complicated), an urethritis, pyelonephritis, gynecologic infections which usually are caused by Enterobacteriaceae (mainly, Escherichia coli) Staphylococcus saprophyticus, Enterococcus species, and gonorrhea which is caused by Neisseria gonorrhoeae.

- Infections of skin and soft tissues which usually are caused by Staphylococcus aureus, Streptococcus pyogenes and Bacteroides species.

- Infections of bones and joints, such as osteomyelitis which usually is caused by Staphylococcus aureus and demands longer therapy.

Other infectious diseases, for example, septic abortion, puerperal sepsis, intra belly sepsis.

- The infections caused by microorganisms, sensitive to amoxicillin, will respond to treatment by Amoklav as amoxicillin is its part. Амоклав it is effective also at the multi-infections caused by the microorganisms sensitive to amoxicillin and the microorganisms producing beta lactamelements which are insensitive to amoxicillin.

Route of administration and doses:

Body weights, functions of kidneys of patients and from weight of an infection depend on age.

Adults and children are more senior than 12 years: slight and average infections: the tablets "Amoklav-375" 3 times a day or the tablets "Amoklav-625" 2 or 3 of time a day.

Heavy infections (including persistent and recurrent infections of urinary tract and a lower respiratory tract infection): 2 tablets "Amoklav-375" 3 times a day or 1-2 tablets "Amoklav-625" 3 times a day.

To children up to 12 years with the body weight of 40 kg drug doses, as at adults are also more appointed.

Low doses are recommended for treatment of infections of skin and soft tissues, recurrent tonsillitis.

High doses are recommended at average otitis, sinusitis, infections of upper and lower respiratory tracts.

Elderly: correction of a dose is not required, the same doses, as at adults are applied.

At a renal failure of a dose are selected, as well as at adults. The technique of selection of a dose is based on the greatest possible level of amoxicillin at a certain extent of decrease in clearance of creatinine.

The recommended doses for adults. Adults - 1 tablet "Amoklav-625" each 24 hours.

Hemodialysis. The technique of selection of a dose is based on the greatest possible level of amoxicillin at a certain degree of depression of function of kidneys. In combination with 1 dose during a hemodialysis and 1 dose after a hemodialysis as concentration of amoxicillin and clavulanic acid decreases

The clearance of creatinine> 30 ml/min. of Correction of a dose is not required.

Clearance of creatinine of 10-30 ml/min. 1 tablet "Amoklav-625" 2 times a day.

Clearance of creatinine <10 ml/min. 1 tablet "Amoklav-625" of 1 times a day.

Abnormal liver function. It is necessary to dose with care and to watch regularly function of a liver.

The doses given for the recommendation are not enough. Two doses of "Amoklav-375" cannot be replaced with one dose of "Amoklav-625" as they are nonequivalent.

Intake. Амоклав it is appointed at the beginning of meal to reduce by-effects from digestive tract.

Absorption Amoklava optimum on condition of reception at the beginning of food.

It is impossible to carry out treatment by Amoklav more than 14 days without assessment of expediency of his continuation. Therapy can be begun with parenteral administration Amoklava, and then to continue administration of drug inside.

Features of use:

Before purpose of therapy by Amoklav it is necessary to collect carefully the anamnesis at patients for clarification of hypersensitivity cases in it on penicillin, cephalosporins or other allergens.

Serious, often fatal reactions (anaphylactic) were noted at penicillin use, especially at patients with hypersensitivity on penicillin. If such reactions develop, Amoklav should cancel and appoint the corresponding therapy. Heavy anaphylactic reactions demand emergency treatment using adrenaline, and also oxygen, intravenous administration of corticosteroids and an intubation can be required.

In general Amoklav is well transferred and possesses a hypotoxicity of antibiotics of group of penicillin. It is recommended to watch in the course of therapy function of a liver, kidneys and hematologic indicators.

At use Amoklava changes of functional tests of a liver can be observed. Though the clinical importance of these changes is not clear, Amoklav should be applied with care at an abnormal liver function.

It is sometimes reported about development of cholestatic jaundice which can be expressed on weight, but reversible.

At the children receiving amoxicillin erythematic rash with ferruterous fever is registered.

Prolonged use of drug can cause the overgrowth of microorganisms, insensitive to it.

Амоклав it is not necessary to appoint at suspicion to an infectious mononucleosis as mononukleozopodobny rash can develop at amoxicillin use.

Correction of doses has to be carried out at adult patients with a renal failure.

Use at pregnancy and feeding by a breast. The researches conducted on animals did not reveal teratogenic effects at Amoklava. Appointment Amoklava it is necessary to avoid at pregnancy, especially in the first trimester if only the doctor does not consider it necessary.

Амоклав it can be appointed in the period of a lactation. Except for risk of a sensitization, any other undesirable symptoms, Amoklav does not cause in the children who are on breastfeeding.

Influence on ability to drive the car and moving mechanisms. Adverse influence on ability to drive the car and moving mechanisms was not observed.

Side effects:

Side effects for Amoklava as a rule, are poorly expressed also tranzitorna.

Gastrointestinal symptoms. There are data on development of diarrhea, digestion disturbance, nausea, vomiting and candidiasis of skin and mucous membranes. The colitis associated with reception of antibiotics (including pseudomembranous and hemorrhagic colitis, meets seldom. Nausea, though is not typical, but arises at intake of high doses Amoklava. Expressiveness of gastrointestinal symptoms decreases at reception Amoklava at the beginning of food.

Liver. Moderate asymptomatic increase in level of nuclear heating plant and/or ALT and alkaline phosphatase is sometimes observed. Hepatitis and cholestatic jaundice meet seldom.

Symptoms from a liver are more characteristic for Amoklava, than of other penicillin, and meet at men more often and 65 years are more senior than patients of advanced age. The risk increases lasting treatment more than 14 days. Very seldom similar complications occur at children.

Symptoms of involvement of a liver usually develop in time of treatment or soon after its termination, but sometimes only in several weeks after drug withdrawal. They are usually reversible though they are much expressed, very seldom come to an end letalno.

Blood. As well as at reception of other penicillin, a tranzitorny leukopenia (including a neutropenia and an agranulocytosis), thrombocytopenia and hemolitic anemia, lengthening of a bleeding time and prothrombin time seldom meet.

Hypersensitivity reactions. Sometimes there are urticaria or erythematic skin rash, a skin itch, a mnogoformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, violent exfoliative dermatitis, acute generalized exanthematous пустулез, a serum disease and a hyper sensitive vasculitis.

Treatment should be stopped at emergence of one of the listed symptoms.

It is reported about a Quincke's disease and an anaphylaxis. Occasionally intersticial nephrite can develop.

TsNS. Symptoms from TsNS develop very seldom. The reversible hyperactivity, dizziness, a headache, spasms concern to them. Spasms can arise at a renal failure or at the patients receiving high doses Amoklava.

Interaction with other medicines:

At the patients receiving Amoklav lengthening of a bleeding time and prothrombin time was noted. Амоклав it is necessary to apply with care at the patients receiving anticoagulants. Амоклав increases efficiency of indirect anticoagulants as, suppressing an indestinal flora, it reduces synthesis of vitamin K and a prothrombin.

It can lower efficiency of oral contraceptives, ethinylestradiol with risk of development of bleedings of" break". Simultaneous use with Allopyrinolum can cause allergic skin reactions.

Diuretics, Allopyrinolum, phenylbutazone, NPVP and other drugs blocking canalicular secretion increase concentration of amoxicillin.

Antacids, glycosamine, purgatives, aminoglycosides slow down and reduce absorption Amoklava, ascorbic acid increases it. Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) have sinergidny effect, bacteriostatic drugs (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) – antagonistic.

Contraindications:

 - hypersensitivity to a beta laktamnym to antibiotics in the anamnesis (for example, to penicillin and cephalosporins).

- a jaundice / abnormal liver function, connected using Amoklava or penicillin, in the anamnesis of patients.

- infectious mononucleosis.

With care to apply at pregnancy, in the period of a lactation, digestive tract diseases (including at colitis, connected using penicillin), at a chronic renal failure.

Overdose:

Emergence of symptoms from digestive tract is possible and disturbance of water and electrolytic balance.

Symptomatic therapy at symptoms of disturbance of water and electrolytic balance is carried out. Амоклав it can be removed from blood by means of a hemodialysis.

During reception of high doses of amoxicillin it is necessary to support adequate consumption of liquid and release of urine at patients to reduce probability of development of an amoksitsillinovy crystalluria.

No more than 250 mg/kg are reported about reception by children of a superdose of amoxicillin that was not followed by development of the expressed clinical symptoms and did not demand a gastric lavage.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above + 25 °C. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 6 tablets in the blister. 2 or 3 blisters together with a leaf insert in secondary packaging.