Кламосар®

General characteristics. Structure:

Active ingredient: 0,5 g or 1 g of amoxicillin of sodium salt (in terms of active agent), 100 mg or 200 mg of clavulanate of potassium (in terms of active agent).

Antibacterial drug with a wide range of antimicrobic action.

Pharmacological properties:

Pharmacodynamics. Klamosar represents an amoxicillin combination - semi-synthetic penicillin with a wide range of antibacterial activity and clavulanic acid - irreversible inhibitor a beta - лактамаз.

Amoxicillin is the semi-synthetic penicillin relating to group a beta - laktamny antibiotics, possessing a wide range of antibacterial activity against many gram-positive and gram-negative microorganisms. Amoxicillin collapses under action a beta - лактамаз and is not effective concerning microorganisms which produce these enzymes.

Clavulanic acid has ability to inactivate a beta - lactamelements, protects amoxicillin from the destroying action a beta - лактамаз and expands a range of antimicrobic activity of drug. Drug is active concerning aerobic gram-positive bacteria (including the strains producing beta lactamelements): Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus anthracis, Streptococcus pneumoniae, Streptococcus viridans, Enterococcus faecalis, Corynebacterium spp., Listeria monocytogenes; anaerobic gram-positive bacteria: Clostridium spp., Peptococcus spp., Peptostreptococcus spp., aerobic gram-negative bacteria (including the strains producing beta lactamelements): Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrahalis, Haemophilus influenzae, Haemophilus ducreyi, Yersinia multocida (before Pasteurella), Campylobactes jejuni; anaerobic gram-negative bacteria (including the strains producing beta lactamelements): Bacteroires spp., including Bacteroides fragilis.

Clavulanic acid suppresses II, III, IV and V types beta лактамаз, is inactive concerning the beta laktamaz of the I type produced by Enterobacter spp., Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp

Pharmacokinetics. After intravenous administration (in/in) in doses of 1200 mg and 600 mg the maximum concentration (Cmax) of amoxicillin - 105.4 mkg/ml and 32.2 mkg/ml respectively, klavulanovy acid - 28.5 mkg/ml and 10.5 mkg/ml respectively.

Therapeutic concentration of amoxicillin and clavulanic acid are created in abdominal, fatty and muscular fabrics of intersticial liquid, in skin, lungs and pleural liquid, in a gall bladder, and also in synovial and peritoneal liquids, bile and pus. Communication with proteins of plasma: amoxicillin - 17-20%, klavulanovy kilothat - 22-30%. Both components of a liver are metabolized: moksitsillin-for 10% of the entered dose, clavulanic acid - for 50%.

Elimination half-life (Т½) later in/in introductions in a dose of 1200 mg and 600 mg – 0.9 h and 1.07ch for amoxicillin, 0.9ch and 1.12 h - for clavulanic acid respectively. It is removed generally by kidneys (glomerular filtering and canalicular secretion): 50-78% and 25 - 40% of a dose of amoxicillin and clavulanic acid respectively, are removed in an invariable look during the first 6 h after reception. Drug gets into breast milk and through a placental barrier.

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms: upper dyyokhatelny ways (bronchitis, pneumonia, a pleura empyema, lung abscess), an infection of ENT organs (sinusitis, tonyozillit, average otitis), infections of biliary tract (a cholangitis, cholecystitis), intestinal infections (a dizenteyoriya, a salmonellosis, a salmonellezny carriage), infections of urinogenital system and bodies of a small pelvis (pyelonephritis, a pyelitis, cystitis, an urethritis, prostatitis, a cervicitis, a salpingitis, a salpingo-oophoritis, tubo-ovarian abscess, an endometritis, a bacterial vaginitis, septic abortion, puerperal sepsis, a pelviperitonitis, a venereal ulcer, gonorrhea), infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis, абс­цесс, phlegmon, a wound fever), osteomyelitis, an endocarditis, meningitis, sepsis; peritonitis, posleoperatsionyony infections, prevention of infections in surgery.

Route of administration and doses:

The dosage depends on age, body weight and function of kidneys of the patient, and also on weight of an infection. At in introduction by the adult and to teenagers 12 years are more senior 3 times a day, if necessary - 4 times a day enter 1.2 g. The maximum daily dose - 6 g. For children of 3 months - 12 years - 25 mg/kg (30 mg/kg counting on all drug) 3 times a day; in hard cases - 4 times a day; for children up to 3 months: premature and in the perinayotalny period - 30 mg/kg 2 times a day, in the post-perinatal period - 25 mg/kg 3 times a day. Treatment duration - up to 14 days.

For prevention of postoperative infections at operations, lasting less than 1 h, during introduction anesthesia enter in a dose 1.2 g, in / century. At longer operations - on 1.2 g each 6 hours within a day. At high risk of infection introduction can be continued within several days.

At HPN reduce frequency rate of introduction depending on the clearance of creatinine (CC). At KK more than 30 ml/min. of reduction of a dose are not required; at KK of 10-30 ml/min. treatment is begun with in/in introductions of 1.2 g, then on 600 mg in/in or on 250-500 mg in 2 times a day; at KK it is less than 10 ml/min. - 1.2 g, then on 600 mg/days in/in or 250-500 mg/days inside in one step. For children of a dose it is necessary to reduce in the same way.

The hemodialysis reduces concentration in blood serum in this connection and at the end of dialysis dopolniyotelno enter 500 mg into time in / century.

Features of use:

At course treatment it is necessary to carry out control of a condition of function of bodies of a hemopoiesis, a liver and kidneys.

Development of superinfection due to growth of microflora, insensitive to drug, is possible that trebuyot corresponding change of antibacterial therapy. At appointment as the patient with sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

At the patients having hypersensitivity to penicillin cross alleryogichesky reactions with tsefalosporinovy antibiotics are possible.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, an abnormal liver function, povyyosheny activities of "hepatic" transaminases, in isolated cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.

Allergic reactions: urticaria, erythematic rashes, it is rare - a multiformny exudative eriyotema, an acute anaphylaxis, a Quincke's disease, is extremely rare - exfoliative dermatitis, a zlokachestvenyony exudative erythema (Stephens-Johnson's syndrome).

From kidneys and urinary tract: very seldom - a crystalluria.

From the hemopoietic system: seldom causes a reversible leukopenia (including a neutropenia or an agranulocytosis), reversible thrombocytopenia and hemolitic anemia. Increase in time of a krovoyotecheniye and prothrombin time is sometimes observed.

From the central nervous system (CNS): very rare side effects from TsNS include a reversible hyperactivity, dizziness, a headache and spasms. Spasms can arise at patients with abnormal liver functions and at the patients receiving high doses of drug.

Local reactions: in some cases - phlebitis in the place in/in introductions.

Others: candidiasis, development of superinfection. There are rare messages on cases of intersticial nephrite.

Interaction with other medicines:

Klamosar it is not necessary to mix with blood products, other proteinaceous liquids, with solutions of a glyuyokoza, dextran or bicarbonate.

At simultaneous use with aminoglycosides antibiotics should not be mixed in one syringe and in a bottle for intravenous liquids as in such conditions aminoglycosides lose activity. Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) have sinergidny effect; the bacteriostatic medicines (M) (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonistic.

It is not recommended to apply along with probenitsidy.

Probenitsid reduces canalicular secretion of amoxicillin and therefore simultaneous use of drugs can lead to a concentration povyyosheniye in amoxicillin blood, but not clavulanic acid.

Diuretics, Allopyrinolum, phenylbutazone, the non-steroidal anti-inflammatory drugs and other HP blocking kanaltseyovy secretion increase concentration of amoxicillin (clavulanic acid is removed generally by glomerular filtering).

Simultaneous use of Allopyrinolum and amoxicillin can increase risk of a vozniknoyoveniye of allergic reactions.

Reduces efficiency of oral contraceptives, HP in the course of which metabolism paraaminobenzoic acid, ethinylestradiol - risk of development of bleedings of "break" obrazuyotsya.

Increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio). At a concomitant use of anticoagulants it is necessary to watch indicators of coagulability of blood.

Contraindications:

Hypersensitivity (including to cephalosporins, etc. beta лактамным to antibiotics), an infectious mononucleosis (including at emergence of a korepodobnoa of rash).

With care. Pregnancy, the lactation period, a heavy liver failure, diseases gastroкишеч­ного a path (including the colitis in the anamnesis connected using penicillin), the chronic renal nedoyostatochnost (CRN).

Overdose:

Symptoms: dysfunction of a GIT and water and electrolytic balance.

Treatment: symptomatic. The hemodialysis is effective.

Storage conditions:

Period of validity 2 years. Not to use later expiry date, specified on packaging. List B. In the dry, protected from light place at a temperature not above 15 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 500 mg + 100 mg or 1000 mg + 200 mg of active agents in bottles. On 5 bottles with drug in a pack from a cardboard together with the instruction.