Amoxiclav (amoxicillin) powder solution for injections 1000 mg/200 mg. N5 vial

Description

Ingredients

active substances: amoxicillin, clavulanic acid;

1 bottle contains:

• 500 mg (or 1000 mg) of amoxicillin in the form of a sodium salt and 100 mg (or 200 mg) of clavulanic acid in the form of a potassium salt.

Medicinal form

Powder for solution for injections.

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.

Pharmacological properties

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)

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.

Method of use and doses of Amoxiclav (amoxicillin) 1000 mg/200 mg.

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, alternative forms of Amoxiclav can be used (for example, with higher doses of amoxicillin and/or a different ratio of amoxicillin and clavulanic acid).

These dosage forms of Amoxiclav 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:

Children with body weight < 40 kg:

Violation of liver function.

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

Features of drug administration.

Amoxiclav (amoxicillin) 1000 mg/200 mg. is administered by intravenous injections (jet) or by periodic infusions (drip). The drug cannot be administered intramuscularly.

Children under 3 months of age are prescribed Amoxiclav only as an intravenous infusion.

Treatment can be started with intravenous administration of Amoxiclavut 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 Amoxiclav (amoxicillin) 1000 mg/200 mg. is dissolved and it is at room temperature, the infusion must be carried out within the time specified below.

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 Amoxiclav (amoxicillin) 1000 mg/200 mg. solutions depends on the concentration. If you prepare a solution of higher concentration, the period of stability of the solution increases proportionally.

Amoxiclav (amoxicillin) 1000 mg/200 mg. 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.

Packaging

5 vials with powder in a cardboard box.