• Augmentin SR (Amoxicillin + Clavulanic acid) 1000mg + 62.5mg 28 tablets

Expiration date: 04/2024

Description of dosage form

Tablets: coated with a film coating of white, capsule-shaped, on one side is engraved "AC 1000/62.5", on the other — dividing groove.

Pharmacological action

Pharmacological action-broad-spectrum antibacterial (bactericidal).

Pharmacodynamics

Amoxicillin is a broad-spectrum semi-synthetic antibiotic with activity against many gram-positive and gram-negative microorganisms. At the same time, amoxicillin is susceptible to destruction by beta-lactamases, and therefore the spectrum of activity of amoxicillin does not extend to microorganisms that produce this enzyme.

Clavulanic acid-inhibitor of beta-lactamase, structurally related to penicillin, has the ability to inactivate a wide range of beta-lactamases found in microorganisms resistant to penicillin and cephalosporins. Clavulanic acid has sufficient effectiveness against plasmid beta-lactamases, which most often cause resistance of bacteria, and is less effective against chromosomal beta-lactamases of the 1st type, which are not inhibited by clavulanic acid.

The presence of clavulanic acid in the drug Augmentin ® protects amoxicillin from destruction by enzymes-beta-lactamases, which allows to expand the antibacterial spectrum of amoxicillin.

The delayed release of amoxicillin in the drug Augmentin® CP allows you to maintain the sensitivity of those strains S. pneumoniae, in which resistance to amoxicillin due to penicillin binding proteins (penicillin-resistant S. pneumoniae, or PRSP).

Below is the activity of a combination of amoxicillin with clavulanic acid in vitro.

Bacteria usually sensitive to the combination of amoxicillin with clavulanic acid

Gram-positive airbags: Bacillus anthracis, Enterococcus faecalis, Listeria monocytogenes, Nocardia asteroides,Streptococcus pneumoniae1, 2,Streptococcus pyogenes1, 2,Streptococcus agalactiae1, 2, Streptococcus groups Viridans2, Streptococcus spp. (other beta-hemolytic streptococci)1,2, Staphylococcus aureus (sensitive to methicillin) 1, Staphylococcus saprophyticus (sensitive to methicillin), coagulase-negative staphylococci (sensitive to methicillin).

Gram-negative airbags: Bordetella pertussis, Haemophilus influenzae1, Helicobacter pylori, Moraxella catarrhalis1, Neisseria gonorrhoeae, Pasteurella multocida, Vibrio cholerae.

Other: Borrelia burgdorferi, Leptospira icterohaemorrhagiae, Treponema pallidum.

Gram-positive anaerobes: Clostridium spp., Peptostreptococcus spp., including Peptococcus niger, Peptostreptococcus magnus, Peptostreptococcus micros.

Gram negative anaerobes: Bacteroides spp., including Bacteroides fragilis, Capnocytophaga spp., Eikenella corrodens, Fusobacterium spp., including Fusobacterium nucleatum, Porphyromonas spp., Prevotella spp.

Bacteria that are likely to have acquired resistance to a combination of amoxicillin with clavulanic acid

Gram-negative aerobes: Escherichia coli1, Klebsiella spp., including Klebsiella oxytoca, Klebsiella pneumoniae1, Proteus spp., including Proteus mirabilis, Proteus vulgaris, Salmonella spp., Shigella spp.

Gram-positive aerobes: Corynebacterium spp., Enterococcus faecium.

Bacteria with natural resistance to the combination of amoxicillin with clavulanic acid

Gram-negative aerobes: Acinetobacter spp., Citrobacter freundii, Enterobacter spp., Hafnia alvei, Legionella pneumophila, Morganella morganii, Providencia spp., Pseudomonas spp., Serratia spp., Stenotrophomonas maltophilia, Yersinia enterocolitica.

Other: Chlamydia spp., including Chlamydia pneumoniae, Chlamydia psittaci, Coxiella burnetii, Mycoplasma spp.

1 clinical efficacy of amoxicillin and clavulanic acid combination was demonstrated in clinical studies for these types of microorganisms.

2 Strains of these bacteria do not produce beta-lactamases. Sensitivity in monotherapy with amoxicillin suggests a similar sensitivity to the combination of amoxicillin with clavulanic acid.

Resistance

Cross-resistance. Amoxicillin directly demonstrates cross-resistance with other beta-lactam antibiotics, as well as a combination of beta-lactam antibiotics with beta-lactamase inhibitors and cephalosporins.

The mechanisms of resistance. Clavulanic acid protects amoxicillin from the damaging effects of beta-lactamase. Delayed release of active ingredients of the drug Augmentin® CP increases the efficiency of amoxicillin against microorganisms, resistance of which is due to the modification of penicillin-binding proteins.

Pharmacokinetics

Suction

Both active ingredients of the drug Augmentin® CP, amoxicillin and clavulanic acid, dissolve well in aqueous solutions with a physiological pH value, quickly and completely absorbed from the gastrointestinal tract after oral administration. Absorption of active ingredients is optimal in the case of taking the drug at the beginning of a meal.

Below are the pharmacokinetic parameters amoxicillin and clavulanic acid after taking 2 tablets. drug Augmentin® CP healthy volunteers at the beginning of the meal.

The drug Augmentin CP has a unique pharmacological profile, the indicator T>IPC, characteristic of this drug, is not achieved when taking tablets with immediate release of active ingredients containing a combination of amoxicillin and clavulanic acid.

Distribution

As with the / in the combination of amoxicillin and clavulanic acid, therapeutic concentrations of amoxicillin and clavulanic acid are created in various tissues and interstitial fluid (gall bladder, abdominal tissue, skin, fat and muscle tissue, synovial and peritoneal fluid, bile, purulent discharge).

Amoxicillin and clavulanic acid have a low degree of binding to plasma proteins. Studies have shown that plasma proteins bind about 25% of total clavulanic acid and 18% of amoxicillin in the blood plasma.

In animal studies has not been detected cumulation of the drug components Augmentin CP in any organ.

Amoxicillin, like most penicillins, can be detected in breast milk. Trace amounts of clavulanic acid were also found in breast milk. With the exception of the possibility of diarrhea and candidiasis of the mucous membranes of the oral cavity, no other negative effects of amoxicillin and clavulanic acid on the health of children who are fed breast milk are known.

Studies of reproductive function in animals when taking the drug Augmentin CP showed that amoxicillin and clavulanic acid penetrate the placental barrier. However, there was no negative impact on the fetus.

Metabolism

10-25% of the initial dose of amoxicillin is excreted by the kidneys in the form of an inactive metabolite (penicillic acid). Clavulanic acid is subjected to intense metabolism to 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrol-3-carboxylic acid and 1-amino-4-hydroxy-butane-2-it is excreted by the kidneys, through the digestive tract, as well as exhaled air in the form of carbon dioxide.

Breeding

Like other penicillins, amoxicillin is excreted mainly by the kidneys, whereas clavulanic acid is excreted by both renal and extrarenal mechanisms.

Studies have shown that, on average, approximately 60-70% amoxicillin and about 40-65% of the clavulanic acid are excreted by the kidneys in unchanged form.

Simultaneous reception of probenecid slows the excretion of amoxicillin, but does not slow the excretion of clavulanic acid (see. "Interaction").

Indications of the drug Augmentin CP

The drug Augmentin SR is indicated for the treatment of bacterial infections of the following localizations caused by microorganisms sensitive to the combination of amoxicillin with clavulanic acid:

respiratory tract infections such as community-acquired pneumonia, exacerbation of chronic bronchitis, acute bacterial sinusitis usually caused by Streptococcus pneumoniae (including penicillin-resistant strains), Haemophilus influenzae1, Moraxella catarrhalis1 and Streptococcus pyogenes;

prevention of local infections after surgery in dentistry.

1 some strains of these bacteria produce beta-lactamases, which makes them insensitive to monotherapy with amoxicillin.

Infections caused by microorganisms sensitive to amoxicillin can be treated with the drug Augmentin CP, as amoxicillin is one of its active ingredients. The drug Augmentin CP is also indicated for the treatment of mixed infections caused by microorganisms sensitive to amoxicillin, as well as microorganisms producing beta-lactamase sensitive to a combination of amoxicillin with clavulanic acid.

The drug Augmentin CP demonstrated efficacy against strains of S. pneumoniae resistant to penicillin (strains with IPC ?2 mg/l).

Preparations containing a combination of amoxicillin with clavulanic acid should be used according to the Russian guidelines for antibiotic therapy and regional data on the sensitivity of pathogens to a combination of amoxicillin with clavulanic acid.

The sensitivity of bacteria to the combination of amoxicillin with clavulanic acid varies by region and over time. Where possible, local sensitivity data should be taken into account. If necessary, microbiological samples should be collected and analyzed for bacteriological sensitivity.

Contraindications

hypersensitivity to amoxicillin, clavulanic acid, other components of the drug, beta-lactam antibiotics (e.g. penicillins, cephalosporins) in history;

previous episodes of jaundice or liver dysfunction when using a combination of amoxicillin with clavulanic acid in the anamnesis.

Caution: impaired liver function.

Application for pregnancy and breastfeeding

In studies of reproductive function in animals oral and parenteral administration of the drug Augmentin® CP did not cause teratogenic effects.

In a single study in women with premature rupture of membranes, it was found that preventive therapy with the drug may be associated with an increased risk of necrotizing enterocolitis in newborns. As with all drugs, Augmentin ® CP is not recommended during pregnancy, except in cases where the expected benefit to the mother exceeds the potential risk to the fetus.

The drug Augmentin® CP can be used during breastfeeding. With the exception of the possibility of developing diarrhea or candidiasis of the oral mucous membranes associated with the penetration into breast milk trace amounts of the active substances of this drug, no other adverse effects were observed in infants who are breastfed. In case of adverse effects in infants who are breastfed, breastfeeding should be discontinued.

Side effect

Adverse events, presented below, are listed in accordance with the defeat of organs and organ systems and frequency. Frequency of occurrence is determined as follows: very often — ?1/10; often — ?1/100 and <1/10; infrequently — ?1/1000 and <1/100; rarely — ?1/10000 and <1/1000; very rarely — <1/10000, including individual cases. Frequency categories were formed on the basis of clinical trials of the drug and post-registration monitoring.

Infectious and parasitic diseases: often-genital moniliasis, skin and mucous candidiasis.

From the blood and lymphatic system: rarely-reversible leukopenia (including neutropenia) and thrombocytopenia; very rarely — reversible agranulocytosis and hemolytic anemia, increased bleeding time and PV.

From the immune system: very rarely-angioedema, anaphylactic reaction, syndrome similar to serum disease, allergic vasculitis.

From the nervous system: infrequently — dizziness, headache; very rarely — reversible hyperactivity, convulsions.

From the digestive tract: very often — diarrhea; often — nausea, abdominal pain; infrequently — vomiting, digestive disorders; very rarely — colitis induced by antibiotics (including pseudomembranous colitis and hemorrhagic colitis), black "hairy" tongue.

From the liver and biliary tract: infrequently — moderate increase in activity ACT and/or ALT. This phenomenon is observed in patients receiving therapy with beta-lactam antibiotics, but its clinical significance is unknown; very rarely — hepatitis and cholestatic jaundice. This phenomenon has been observed in patients receiving therapy with the antibiotic penicillin and cephalosporins.

Undesirable phenomena from the liver are observed mainly in men and elderly patients and may be associated with prolonged therapy.

These signs and symptoms usually occur during or immediately after therapy, but in some cases may not appear for several weeks after the completion of therapy. Adverse events are typically reversible. Undesirable phenomena on the part of the liver can be severe, in extremely rare cases, there have been reports of fatal outcomes. In almost all cases, these were patients with serious comorbidities or patients receiving potentially hepatotoxic drugs at the same time.

From the skin and subcutaneous tissues: infrequently-rash, itching, urticaria; rarely - multiform erythema; very rarely — Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous exfoliative dermatitis, acute generalized exanthematous pustules. In case of any allergic reactions treatment drug Augmentin® CP should stop.

From the kidneys and urinary tract: very rare — interstitial nephritis, crystalluria.

Interaction

Simultaneous use of the drug Augmentin® CP and probenecid is not recommended. Probenecid reduces the tubular secretion of amoxicillin, and therefore the simultaneous use of the drug Augmentin® CP and probenecid may lead to an increase in blood and consistency in the concentration of amoxicillin, but not clavulanic acid.

Simultaneous use of allopurinol and amoxicillin can increase the risk of skin allergic reactions. Currently in the literature there is no data on the simultaneous use of a combination of amoxicillin with clavulanic acid and allopurinol.

Penicillins are able to slow the excretion of methotrexate by inhibiting its tubular secretion, so the simultaneous use of the drug Augmentin® CP and methotrexate can increase the toxicity of methotrexate.

Like other antibacterial drugs, the drug Augmentin® CP can have an impact on the intestinal microflora, leading to a decrease in the absorption of estrogens from the gastrointestinal tract and reduce the effectiveness of combined oral contraceptives.

The literature describes rare cases of mho increase in patients with the combined use of acenocumarol or warfarin and amoxicillin. If necessary, the simultaneous appointment or withdrawal of the drug Augmentin® CP with anticoagulants PV or MHO should be carefully monitored, may require dose adjustment anticoagulants for oral administration.

Method of application and doses

Inside.

To optimize the absorption of the drug should be taken at the beginning of meals.

Treatment should not last more than 14 days without review of the clinical situation.

Tablets drug Augmentin® CP have a dividing groove, which allows to split them in half for ease of swallowing, but not for dose reduction: both halves must be taken at the same time. The recommended dose of the drug is 2 tables. 2 times a day.

Adults (16 years and older). Respiratory infections: 2 table. 2 times a day for 7-10 days, including the following diseases:

  • community acquired pneumonia — 2 table. 2 times a day for 7-10 days;
  • exacerbation of chronic bronchitis-table 2. 2 times a day for 7 days;
  • acute sinusitis of bacterial etiology-table 2. 2 times a day for 10 days.

Prevention of local infections after dental surgery: table 2. 2 times a day for 5 days starting 3 hours after the intervention.

Special groups of patients

Children up to 16 years. Not applicable.

Patients of advanced age. Do not require correction dosing regimen.

Patients with impaired renal function. Is not required correction mode when Cl creatinine ?30 ml/min Not recommended in prescribing the drug to patients with Cl creatinine <30 ml/min.

The patients on hemodialysis. Not recommend.

Impaired liver function. The treatment is carried out with caution; regular monitoring of liver function. Insufficient data to recommend dosing regimen for this group of patients.

Overdose

Symptoms: there may be symptoms from the gastrointestinal tract and violations of water-electrolyte balance. Amoxicillin crystalluria is described, which in some cases led to the development of renal failure (see "Special instructions").

Treatment: symptoms from the gastrointestinal tract-symptomatic therapy, paying special attention to the normalization of water-electrolyte balance. Amoxicillin and clavulanic acid can be removed from the bloodstream by hemodialysis.

Special instruction

Before starting treatment with Augmentin® CP, it is necessary to collect a detailed anamnesis concerning previous hypersensitivity reactions to penicillins, cephalosporins.

Serious and sometimes lethal hypersensitivity reactions (anaphylactic reactions) to penicillins are described. The risk of such reactions is highest in patients with a history of hypersensitivity reactions to penicillins. In case of an allergic reaction, it is necessary to stop treatment with Augmentin® CP and start appropriate alternative therapy.

In case of serious anaphylactic reactions, epinephrine should be administered immediately to the patient. May also require oxygen therapy, in/in the introduction of GCS and provision of airway management, including intubation.

In the case of suspected infectious mononucleosis drug Augmentin® SR should not be used because patients with this disease, amoxicillin may cause a morbilliform rash, which makes diagnosis of the disease.

Prolonged treatment with the drug Augmentin® CP sometimes leads to excessive reproduction of insensitive microorganisms.

In order to reduce the risk of side effects from the gastrointestinal tract should take the drug at the beginning of a meal.

In patients receiving a combination of amoxicillin with clavulanic acid in conjunction with indirect (oral) anticoagulants, in rare cases, an increase in PV (MHO increase) was reported. In the joint appointment of indirect (oral) anticoagulants with a combination of amoxicillin with clavulanic acid, monitoring of relevant indicators is necessary. To maintain the necessary effect of oral anticoagulants may require correction of their dose.

Is not required correction doses of the drug Augmentin® SR in patients with Cl creatinine ?30 ml/min Not recommended in prescribing the drug to patients with Cl creatinine <30 ml/min in patients with reduced diuresis in very rare cases, it was reported on crystalluria development, mainly at parenteral application of the drug. When taking high doses of amoxicillin, it is recommended to take sufficient amount of liquid and maintain adequate diuresis to reduce the probability of amoxicillin crystals formation (see "Overdose").

Ingestion of Augmentin® CP leads to a high content of amoxicillin in the urine, which can lead to false positive results in the determination of glucose in the urine (eg Benedict test, feling test). In this case, it is recommended to use the glucoside method for determining the concentration of glucose in the urine.

Abuse and drug addiction. There was no drug dependence, addiction and euphoria reactions associated with the use of the drug Augmentin® CP.

Influence on the ability to drive vehicles and operate machinery. Since the drug can cause dizziness, it is necessary to warn patients about precautions when driving or working with moving machinery.

Form release

Tablets with modified release, film-coated, 1000 mg+62,5 mg In a blister of PVC or PE/aluminum foil 2 PCs 2 blisters in a combined package with a dividing line between them. 4, 7 or 10 of the combined packs in a cardboard pack.

Manufacturer

"Glaxo Vellkom Production". 53100, Terra II, Z. I. de La peyrin, Mayenne, France.

Name and address of the legal entity in whose name the registration certificate is issued: CJSC "GlaxoSmithKline trading". 119180, Moscow, Yakimanskaya nab., 2.

For more information, please contact: CJSC "GlaxoSmithKline trading". 121614, Moscow, Krylatskaya str., 17, korp. 3, FL. 5. Krylatsky hills business Park.

Storage conditions of the drug Augmentin® CP

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf life of the drug Augmentin® CP

2 years.

Do not use after expiration date indicated on the package.

Augmentin
SR
(Amoxicillin
+
Clavulanic
acid)
1000mg
+
62.5mg
28
tablets