Amoxiclav (amoxicillin) powder solution for injections 500 mg/100 mg. N5 vial

Amoxiclav (amoxicillin) powder solution for injections 500 mg/100 mg. N5 vial

$46.30

Manufacturer: Austria

Treatment of bacterial infections caused by microorganisms sensitive to the drug, such as:

  • severe throat, nose, and ear infections (such as mastoiditis, peritonsillar infections, epiglottitis, and sinusitis with associated severe systemic signs and symptoms);
  • exacerbation of chronic bronchitis (after confirming the diagnosis);
  • nosocomial pneumonia;
  • cystitis
  • pyelonephritis;
  • skin and soft tissue infections, including bacterial cellulitis, animal bites, severe dentoalveolar abscesses with widespread cellulitis;
  • bone and joint infections, including osteomyelitis;
  • intra-abdominal infections;
  • genital infections in women.

Prevention of bacterial infections during major surgical interventions in the following areas:

  • gastrointestinal tract;
  • pelvic organs;
  • head and neck;
  • bile ducts

When prescribing antibacterial drugs, one should be guided by the rules of their proper use.

Category:

Description

Ingredients

active substances : amoxicillin, clavulanic acid;

1 vial contains 500 mg of amoxicillin in the form of a sodium salt and 100 mg of clavulanic acid in the form of a potassium salt.

Medicinal form

Powder for solution for injection.

Main physical and chemical properties: white to light yellow powder.

Pharmacotherapeutic group

Antibacterial agents for systemic use. Beta-lactam antibiotics, penicillins.

Combinations of penicillins with beta-lactamase inhibitors. ATX code J01C R02.

Pharmacodynamics

Mechanism of action. Amoxicillin is a semi-synthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes, often called penicillin-binding proteins (PBPs), in the process of biosynthetic metabolism of bacterial peptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to weakening of the cell wall, resulting in cell lysis and death.

Amoxicillin is sensitive to cleavage by beta-lactamases produced by resistant bacteria, therefore, the spectrum of activity of amoxicillin as monotherapy does not include organisms that produce these enzymes.

Clavulanic acid is a beta-lactam structurally related to penicillins. It deactivates some beta-lactamase enzymes, thereby preventing the inactivation of amoxicillin. Clavulanic acid in the form of monotherapy does not have a clinically useful antibacterial effect.

FK/FD ratio. The time exceeding the minimum inhibitory concentration (T>MIC) is considered the main factor that determines the effectiveness of amoxicillin.

Mechanisms of resistance

There are two mechanisms of resistance to amoxicillin/clavulanic acid:

  • inactivation by bacterial beta-lactamases that are not themselves inhibited by clavulanic acid, including class B, C and D;
  • conversion of PZB, which reduces the affinity of the antibacterial drug to the target.

Bacterial impermeability or the efflux pump mechanism can cause or contribute to bacterial resistance, particularly in Gram-negative bacteria.

Limit values

MIC breakpoints for amoxicillin/clavulanic acid established by the European Committee on Antimicrobial Susceptibility Testing (EUCAST)

Microorganisms Limit values ​​of sensitivity (μg/ml)
sensitive Moderately sensitive Resistant
Haemophilus influenzae1 ≤1 – > 1
Moraxella catarrhalis1 ≤1 – > 1
Staphylococcus aureus 2 ≤2 – >2
Coagulase-negative staphylococci 2 ≤ 0.25 > 0.25
Enterococcus1 ≤4 8 > 8
Streptococcus A, B, C, G 5 ≤ 0.25 – > 0.25
Streptococcus pneumoniae3 ≤ 0.5 1–2 >2
Enterobacteria 1, 4 – – > 8
Gram-negative anaerobic bacteria 1 ≤4 8 > 8
Gram-positive anaerobic bacteria 1 ≤4 8 > 8
Limit values ​​that do not apply to individual species 1 ≤2 4–8 > 8
1 – Reported values ​​for amoxicillin concentrations. For the purpose of sensitivity testing, the concentration of clavulanic acid is set at 2 mg/l.

2 – Reported values ​​for oxacillin concentrations.

3 – The limit values ​​given in the table are calculated from the limit values ​​for ampicillin.

4 – The limit value of resistance R>8 mg/l means that all strains with resistance mechanisms are declared resistant.

5 – The limit values ​​given in the table are calculated from the limit values ​​for benzylpenicillin.

The prevalence of resistance may vary geographically and over time for individual species, so local susceptibility information is desirable, especially when treating severe infections. Expert opinion may be required if the local prevalence of resistance is such that the benefit of the drug, at least in some types of infection, is questionable.

Usually sensitive species

Gram-positive aerobes : Enterococcus faecalis, Gardnerella vaginalis, Staphylococcus aureus (sensitive to methicillin), Coagulase-negative staphylococci (sensitive to methicillin), Streptococcus agalactiae, Streptococcus pneumoniae1, Streptococcus pyogenes and other beta-hemolytic streptococci, Streptococcus viridans group.

Gram-negative aerobes: Actinobacillus actinomycetemcomitans, Capnocytophaga spp., Eikenella corrodens, Haemophilus influenzae2, Moraxella catarrhalis, Neisseria gonorrhoeae§, Pasteurella multocida.

Anaerobes: Bacteroides fragilis, Fusobacterium nucleatum, Prevotella spp.

Species for which the acquisition of resistance may be a problem

Gram-positive aerobes: Enterococcus faecium$.

Gram-negative aerobes: Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris.

Naturally resistant microorganisms

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

Other microorganisms:

Chlamydophila pneumoniae, Chlamydophila psittaci, Coxiella burnetti, Mycoplasma pneumoniae.

– Natural moderate sensitivity in the absence of an acquired resistance mechanism.

– All staphylococci resistant to methicillin are resistant to amoxicillin/clavulanic acid.

– All amoxicillin-resistant strains that are not mediated by beta-lactamases are resistant to amoxicillin/clavulanic acid.

– This dosage form of amoxicillin/clavulanic acid may not be suitable for the treatment of Streptococcus pneumoniae, which is resistant to penicillin.

– Strains with reduced sensitivity have been registered in some EU countries with a frequency higher than 10%.

Indications

Treatment of bacterial infections caused by microorganisms sensitive to Amoxiclav (amoxicillin), such as:

  • severe throat, nose, and ear infections (such as mastoiditis, peritonsillar infections, epiglottitis, and sinusitis with associated severe systemic signs and symptoms);
  • exacerbation of chronic bronchitis (after confirming the diagnosis);
  • nosocomial pneumonia;
  • cystitis
  • pyelonephritis;
  • skin and soft tissue infections, including bacterial cellulitis, animal bites, severe dentoalveolar abscesses with widespread cellulitis;
  • bone and joint infections, including osteomyelitis;
  • intra-abdominal infections;
  • genital infections in women.

Prevention of bacterial infections during major surgical interventions in the following areas:

  • gastrointestinal tract;
  • pelvic organs;
  • head and neck;
  • bile ducts

When prescribing antibacterial drugs, one should be guided by the rules of their proper use.

Contraindications

  • Increased sensitivity to active substances, penicillin and other components of the drug.
  • History of a severe immediate-type allergic reaction (eg, anaphylaxis) to another beta-lactam antibiotic (eg, a cephalosporin, carbapenem, or monobactam).
  • Jaundice/history of liver dysfunction caused by amoxicillin/clavulanic acid.

Dosage and Administration

Doses are given as amoxicillin/clavulanic acid content unless a dose of an individual component is specified.

When choosing a dose of a drug for the treatment of a certain infection, it is necessary to take into account:

  • expected pathogens and their expected sensitivity to antibacterial substances;
  • severity and localization of infection;
  • the patient’s age, body weight, and renal function status, as described below.

If necessary, you can use alternative forms of Amoxiclav (amoxicillin) powder (for example, with higher doses of amoxicillin and/or a different ratio of amoxicillin and clavulanic acid).

These dosage forms of Amoxiclav (amoxicillin) powder can be used in a daily dose of up to 3000 mg of amoxicillin and 600 mg of clavulanic acid. If it is necessary to use a higher dose of amoxicillin, a drug with a different amoxicillin/clavulanic acid ratio should be prescribed to avoid excessively high daily doses of clavulanic acid.

The duration of treatment is determined by the doctor individually. Some infections (for example, osteomyelitis) require longer treatment. The duration of treatment should not exceed 14 days without evaluating the results of use and the clinical picture.

Dosage for adults and children whose body weight is ≥ 40 kg.

Standard dose: 1000 mg/200 mg every 8 hours.

Prevention of complications during surgical interventions.

For operations lasting less than 1 hour, the recommended dose is from 1000 mg/200 mg to 2000 mg/200 mg when administered under anesthesia (a dose of 2000 mg/200 mg can be achieved when using the appropriate intravenous form of the drug).

For operations lasting more than 1 hour, the recommended dose is from 1000 mg/200 mg to 2000 mg/200 mg under anesthesia, a dose of 1000 mg/200 mg can be administered 3 times within 24 hours.

If there are clinical signs of infection during surgery, a course of treatment with intravenous or oral administration of the drug should be prescribed in the postoperative period.

Dosage for children with body weight < 40 kg.

Children aged 3 months and older: 25 mg/5 mg/kg of body weight every 8 hours.

Children under 3 months of age or weighing less than 4 kg: 25 mg/5 mg/kg of body weight every 12 hours.

Elderly patients. Dose correction is not required.

Impaired kidney function.

Dosage adjustments are based on the maximum recommended doses of amoxicillin.

No dose adjustment is required for creatinine clearance > 30 ml/min.

Adults and children with body weight ≥ 40 kg:

Creatinine clearance 10–30 ml/min The first dose is 1000 mg/200 mg, then 500 mg/100 mg 2 times a day
Creatinine clearance < 10 ml/min The first dose is 1000 mg/200 mg, then 500 mg/100 mg every 24 hours
Hemodialysis The first dose is 1000 mg/200 mg, then 500 mg/100 mg every 24 hours + 500 mg/100 mg after dialysis

 

Children with body weight < 40 kg:

Creatinine clearance 10–30 ml/min 25 mg/5 mg/kg every 12 hours
Creatinine clearance < 10 ml/min 25 mg/5 mg/kg every 24 hours
Hemodialysis 25 mg/5 mg/kg every 24 hours + 12.5/2.5 mg after dialysis

 

Violation of liver function

Care must be taken when dosing, constant monitoring of liver function at regular intervals.

Features of drug administration

Amoxiclav (amoxicillin) powder solution is administered by intravenous injection (jet) or by periodic infusions (drip). The drug cannot be administered intramuscularly.

Children under 3 months of age are prescribed Amoxiclav (amoxicillin) powder solution only as an intravenous infusion.

Treatment can be started with intravenous administration of Amoxiclav (amoxicillin)  powder solution and continued with forms for oral administration.

Preparation of solution for intravenous injections.

500 mg/100 mg: dissolve the contents of the vial in 10 ml of water for injections (final volume – 10.5 ml);

1000 mg/200 mg: dissolve the contents of the vial in 20 ml of water for injections (final volume – 20.9 ml).

The reconstituted solutions have a yellowish (pale straw) color. Use only clear solutions. The solution should be used within 20 minutes after recovery, inject the drug slowly for 3-4 minutes directly into a vein or through a catheter, drip.

Preparation of solution for intravenous infusion

Reconstituted as above, the 500 mg/100 mg solution is then added without delay to 50 ml of infusion liquid or the 1000 mg/200 mg solution to 100 ml of infusion liquid (it is better to use a mini-container or burette). The infusion should be carried out for 30–40 minutes.

The solution for infusions is chemically and physically stable for 2-3 hours at a temperature of 25 °C or 8 hours at a temperature of 5 °C. From a microbiological point of view, it is better to introduce the prepared solution immediately.

Various solvents can be used for intravenous infusions. A satisfactory concentration of the antibiotic is maintained at 5 ºС and at room temperature (25 ºС) in the recommended volumes of the infusion solutions indicated below.

When the drug is dissolved and it is at room temperature, the infusion must be carried out within the time indicated below.

Solution for intravenous (IV) administration Stability period at 25 °C, hours
Water for injections 3
0.9% sodium chloride solution 3
Combined solution of sodium chloride

(Ringer’s solution)

 2
Combined sodium lactate solution

(Hartmann’s solution)

 2
0.3% solution of potassium chloride and 0.9% solution of sodium chloride 2

 

In the case of storage at a temperature of 5 °C, reconstituted solutions of 1000 mg/200 mg and 500 mg/100 mg can be added to a pre-cooled solution for infusions (water for injections or 0.9% sodium chloride solution), the resulting drug can be stored at the specified temperature for up to 8 hours.

After the solution reaches room temperature, it should be used immediately.

The stability of drug solutions depends on the concentration. If you prepare a solution of higher concentration, the period of stability of the solution increases proportionally.

Amoxiclav (amoxicillin) powder solution is less stable in solutions of glucose, dextran, and bicarbonate, so solutions based on this should be used within 3–4 minutes after dissolution.

Any unused solution should be disposed of in accordance with applicable requirements.

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