Expiration date: 04/2025

Augmentin EC. Description of the active substance (instructions for use)

Pharm group: antibiotic-penicillin, semi-synthetic+betalactamase inhibitor.

Formdata: a Combination drug of amoxicillin and clavulanic acid - inhibitor of beta-lactamase. Acts bactericidal, inhibits the synthesis of bacterial walls.

Active against aerobic gram-positive bacteria (including strains producing beta-lactamases): Staphylococcus aureus, 

aerobic gram-negative bacteria: Enterobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp., Moraxella catarrhalis.

The following agents are only sensitive in vitro: Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus anthracis, Streptococcus pneumoniae, Streptococcus viridans group, Enterococcus faecalis, Corynebacterium spp., Listeria monocytogenes, anaerobic Clostridium spp., Peptococcus spp., Peptostreptococcus spp., 

aerobic gram-negative bacteria (including strains producing beta-lactamases): Proteus mirabilis, Proteus vulgaris, Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus ducreyi, Yersinia multocida (formerly Pasteurella), Campylobacter jejuni, 

anaerobic gram-negative bacteria (including strains producing beta-lactamases): Bacteroides spp., including Bacteroides fragilis.

Clavulanic acid suppresses II, III, IV and V types of beta-lactamases, is inactive against type I beta-lactamases, produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp. Clavulanic acid has a high tropism to penicillinases, thereby forming a stable complex with the enzyme, which prevents the enzymatic degradation of amoxicillin under the influence of beta-lactamases.

Pharmacokinetics: after oral administration, both components are rapidly absorbed into the digestive tract. Simultaneous eating does not affect absorption. TCmax-45 min. after oral administration at a dose of 250/125 mg every 8 h Cmax amoxicillin-2.18-4.5 mg / ml, clavulanic acid-0.8-2.2 mg/ ml, at a dose of 500/125 mg every 12 h Cmax amoxicillin - 5.09-7.91 mg/ ml, clavulanic acid-1.19-2.41 mg/ ml, at a dose of 500/125 mg every 8 h Cmax amoxicillin-4.9 9.46 µg / ml, clavulanic acid-1.57-3.23 µg / ml, at a dose of 875/125 mg Cmax amoxicillin-8.82-14.38 mg/ ml, clavulanic acid-1.21-3.19 mg / ml. After the on/in the introduction in doses of 1000/200 500/100 mg and a Cmax of amoxicillin - 105.4 and 32.2 µg/ml, respectively, and clavulanic acid - 28.5 and 10.5 µg/ml the maximum inhibitory concentration of 1 mcg/ml for amoxicillin similar when applied within 12 h and 8 h in both adults and children.

Plasma protein binding: amoxicillin-17-20%, clavulanic acid - 22-30%.

Both components are metabolized in the liver: amoxicillin-10% of the dose administered, clavulanic acid - 50%.

T1 / 2 after administration at a dose of 375 and 625 mg - 1 and 1.3 h for amoxicillin, 1.2 and 0.8 h - for clavulanic acid, respectively. T1/2 after the on / in the dose of 1200 and 600 mg - 0.9 and 1.07 h - for amoxicillin, 0.9 and 1.12 h - for clavulanic acid, respectively. It is excreted mainly by the kidneys (glomerular filtration and tubular secretion): 50-78 and 25-40% of the administered dose of amoxicillin and clavulanic acid is excreted, respectively, unchanged during the first 6 h after administration.

Indications: Bacterial infections caused by sensitive pathogens: 

lower respiratory tract infections (bronchitis, pneumonia, empyema of pleura, lung abscess),  

infections of ENT organs (sinusitis, tonsillitis, otitis media),  

infections of the genitourinary system and pelvic organs (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, cervicitis, salpingitis, salpingo-oophoritis, tuboovarian abscess, endometritis, bacterial vaginitis, septic abortion, postpartum sepsis, pelviperitonitis, mild shankr, gonorrhea),  

skin and soft tissue infections (erysipelas, impetigo, secondary infected dermatoses, abscess, phlegmon, wound infection),  

osteomyelitis,  

postoperative infection,  

prevention of infections in surgery.

Contraindications: Hypersensitivity (including to cephalosporins and other beta-lactam antibiotics), infectious mononucleosis (including the appearance of a korepodobnoy rash), phenylketonuria, episodes of jaundice or liver dysfunction due to the use of amoxicillin/clavulanic acid in the anamnesis, CC less than 30 ml/min (for tablets 875 mg/125 mg).

With caution. Pregnancy, lactation, severe hepatic insufficiency, gastrointestinal disorders (including history of colitis associated with the use of penicillins), CPN.

Dosing: Inside, in/out.

Doses are given in terms of amoxicillin. Dosing regimen is set individually depending on the severity of the course and the location of the infection, the sensitivity of the pathogen.

Children under 12 years-in the form of suspension, syrup or drops for oral administration. Single dose is set depending on age: children up to 3 months - 30 mg/kg/day in 2 admission, 3 months and older - mild infections - 25 mg/kg/day in 2 admission or 20 mg/kg/day in 3 admission, severe infections - 45 mg/kg/day in 2 admission or 40 mg/kg/day in 3 admission.

Adults and children over 12 years of age or weighing 40 kg or more: 500 mg 2 times/day or 250 mg 3 times/day. In severe infections and respiratory infections-875 mg 2 times/day or 500 mg 3 times / day.

The maximum daily dose of amoxicillin for adults and children over 12 years - 6 g, for children under 12 years - 45 mg/kg body weight.

The maximum daily dose of clavulanic acid for adults and children over 12 years - 600 mg, for children under 12 years - 10 mg/kg body weight.

In case of difficulty swallowing in adults, the use of a suspension is recommended.

When preparing the suspension, syrup and drops as a solvent, water should be used.

At/in the introduction adults and adolescents over 12 years is introduced 1 g (amoxicillin) 3 times a day, if necessary - 4 times a day. The maximum daily dose is 6 g. for children 3 months-12 years-25 mg/kg 3 times a day, in severe cases - 4 times a day, for children up to 3 months: premature and in the perinatal period - 25 mg/kg 2 times a day, in the postperinatal period - 25 mg / kg 3 times a day.

Duration of treatment - up to 14 days, acute otitis media - up to 10 days.

For the prevention of postoperative infections in operations lasting less than 1 h, during the introductory anesthesia is administered at a dose of 1 g/in. With longer operations-1 g every 6 h during the day. With a high risk of infection, administration can be continued for several days.

When CPN is carried out dose correction and multiplicity of administration depending on the CC: CC more than 30 ml/min dose adjustment is not required when CC 10-30 ml/min: inside - 250-500 mg/day every 12 h, in/in - 1 g, then 500 mg/in, with CC less than 10 ml/min - 1 g, then 500 mg/day/in or 250-500 mg / St inside one reception. For children, doses should be reduced in the same way.

Patients on hemodialysis-250 mg or 500 mg orally in a single dose or 500 mg/in, an additional 1 dose during dialysis and another 1 dose at the end of a dialysis session.

Side effect: from the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, increased activity of "hepatic" transaminases, in isolated cases - cholestatic jaundice, hepatitis, hepatic insufficiency (more often in the elderly, men, with long-term therapy), pseudomembranous and hemorrhagic colitis (can also develop after therapy), enterocolitis, black "hairy" tongue, sweating tooth enamel.

From the hematopoietic organs: reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolytic anemia.

From the nervous system: dizziness, headache, hyperactivity, anxiety, behavior changes, seizures.

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

Allergic reactions: urticaria, erythematous rashes, rarely-multiform exudative erythema, anaphylactic shock, angioedema, extremely rare-exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), allergic vasculitis, syndrome similar to serum disease, acute generalized exanthematous pustules.

Other: candidiasis, development of superinfection, interstitial nephritis, crystalluria, hematuria.

Overdose: Symptoms: impaired function of the gastrointestinal tract and water-electrolyte balance.

Treatment: symptomatic. Hemodialysis is effective.

Interaction: Antacids, glucosamine, laxatives, aminoglycosides slow down and reduce absorption, ascorbic acid increases absorption.

Bacteriostatic LS (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) have an antagonistic effect.

Increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). The simultaneous administration of anticoagulants is necessary to monitor the indicators of blood coagulation.

Reduces the effectiveness of oral contraceptives, LS, during the metabolism of which is formed PABK, ethinyl estradiol-the risk of bleeding "breakthrough".

Diuretics, allopurinol, phenylbutazone, NSAIDs, etc.LS, blocking tubular secretion, increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

Allopurinol increases the risk of skin rashes.

Special instructions: during the course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver and kidneys.

In order to reduce the risk of side effects from the gastrointestinal tract should take the drug during meals.

Perhaps the development of superinfection due to the growth of insensitive to it microflora, which requires appropriate changes in antibacterial therapy.

Can give false positive results in the determination of glucose in the urine. In this case, it is recommended to use the glucoside method for determining the concentration of glucose in the urine.

After dilution, the suspension should be stored for no more than 7 days in the refrigerator, but do not freeze.

In patients with hypersensitivity to penicillins, cross allergic reactions with cephalosporin antibiotics are possible.

Cases of necrotizing colitis development in newborns, pregnant women with premature rupture of membranes were revealed.

Since the tablets contain the same amount of clavulanic acid (125 mg), it should be borne in mind that 2 tablets of 250 mg (amoxicillin) is not equivalent to 1 tablet of 500 mg (amoxicillin).