Amikacin, 500 mg

A semisynthetic broad-spectrum antibiotic from the group of aminoglycosides, acts bactericidally. Binding to 30S ribosome subunit, it prevents formation of transport and matrix RNA complex, blocks protein synthesis and destroys cytoplasmic membranes of bacteria.

Highly active against aerobic gram-negative microorganisms: Pseudomonas aeruginosa, Escherichia coli, Klebsiella spp, Serratia spp, Providencia spp, Enterobacter spp, Salmonella spp., Shigella spp.; some gram-positive microorganisms: Staphylococcus spp. (including those resistant to penicillin, some cephalosporins).

It is moderately active against Streptococcus spp.

In concomitant administration with benzylpenicillin it shows synergistic action against strains of Enterococcus faecalis.

The drug is resistant to anaerobic microorganisms.

Amicacin does not lose activity under the action of enzymes that inactivate other aminoglycosides and may remain active against strains of Pseudomonas aeruginosa resistant to tobramycin, gentamicin and netilmicin.

Indications

Infectious and inflammatory diseases caused by gram-negative microorganisms (resistant to gentamicin, sizomycin and kanamycin) or associations of gram-positive and gram-negative microorganisms:

respiratory tract infections (bronchitis, pneumonia, pleural empyema, lung abscess);
sepsis;
septic endocarditis;
central nervous system infections (including meningitis);
abdominal infections (including peritonitis);
genitourinary tract infections (pyelonephritis, cystitis, urethritis);
purulent infections of the skin and soft tissues (including infected burns, infected ulcers and bedsores of various origins);
biliary tract infections;
infections of bones and joints (including osteomyelitis);
wound infection;
postoperative infections.

Pharmacological effect

A semi-synthetic broad-spectrum antibiotic from the group of aminoglycosides, has a bactericidal effect. By binding to the 30S subunit of ribosomes, it prevents the formation of a transport and messenger RNA complex, blocks protein synthesis, and also destroys the cytoplasmic membranes of bacteria.

Highly active against aerobic gram-negative microorganisms: Pseudomonas aeruginosa, Escherichia coli, Klebsiella spp., Serratia spp., Providencia spp., Enterobacter spp., Salmonella spp., Shigella spp.; some gram-positive microorganisms: Staphylococcus spp. (including those resistant to penicillin and some cephalosporins).

Moderately active against Streptococcus spp.

When administered simultaneously with benzylpenicillin, it exhibits synergistic action against strains of Enterococcus faecalis.

Anaerobic microorganisms are resistant to the drug.

Amikacin does not lose activity under the influence of enzymes that inactivate other aminoglycosides, and may remain active against strains of Pseudomonas aeruginosa resistant to tobramycin, gentamicin and netilmicin.

Special instructions

Before use, the sensitivity of the isolated pathogens is determined using disks containing 30 μg of amikacin. With a diameter of the growth-free zone of 17 mm or more, the microorganism is considered sensitive, from 15 to 16 mm – moderately sensitive, less than 14 mm – resistant.

The concentration of amikacin in plasma should not exceed 25 mcg/ml (a concentration of 15-25 mcg/ml is therapeutic).

During the treatment period, it is necessary to monitor the function of the kidneys, auditory nerve and vestibular apparatus at least once a week.

The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as when prescribing high doses or for a long time (in these patients, daily monitoring of renal function may be required).

If audiometric tests are unsatisfactory, the dose of the drug is reduced or treatment is stopped.

Patients with infectious and inflammatory diseases of the urinary tract are recommended to take increased amounts of fluid with adequate diuresis.

In the absence of positive clinical dynamics, one should remember the possibility of the development of resistant microorganisms. In such cases, it is necessary to discontinue treatment and begin appropriate therapy.

The sodium disulfite contained in the drug can cause the development of allergic complications in patients (including anaphylactic reactions), especially in patients with an allergic history.

Active ingredient

Amikacin

Composition

1 bottle contains amikacin (in the form of sulfate) 500 mg.

Excipients:

sodium disulfite (sodium metabisulfite),

sodium citrate d/i ​​(sodium citrate pentasesquihydrate),

diluted sulfuric acid,

water d/i.

Contraindications

acoustic neuritis;
severe chronic renal failure with azotemia and uremia;
pregnancy;
hypersensitivity to the components of the drug;
history of hypersensitivity to other aminoglycosides.

The drug should be used with caution in myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause disruption of neuromuscular transmission, which leads to further weakening of skeletal muscles), dehydration, renal failure, in the neonatal period, in premature infants, in elderly patients, during lactation.

Side Effects

From the digestive system: nausea, vomiting, liver dysfunction (increased activity of liver transaminases, hyperbilirubinemia).

Interaction

Shows synergism when interacting with carbenicillin, benzylpenicillin, cephalosporins (in patients with severe chronic renal failure, when used together with beta-lactam antibiotics, the effectiveness of aminoglycosides may be reduced).

Nalidixic acid, polymyxin B, cisplatin and vancomycin increase the risk of developing oto- and nephrotoxicity.

Diuretics (especially furosemide), cephalosporins, penicillins, sulfonamides and NSAIDs, competing for active secretion in the nephron tubules, block the elimination of aminoglycosides, increase their concentration in the blood serum, increasing nephro- and neurotoxicity.

Amikacin enhances the muscle relaxant effect of curare-like drugs.

When used simultaneously with amikacin, methoxyflurane, polymyxins for parenteral administration, capreomycin and other drugs that block neuromuscular transmission (halogenated hydrocarbons – inhalation anesthesia, opioid analgesics), transfusion of large amounts of blood with citrate preservatives increase the risk of respiratory arrest.

Parenteral administration of indomethacin increases the risk of developing toxic effects of aminoglycosides (increased T1/2 and decreased clearance).

Amikacin reduces the effectiveness of antimyasthenic drugs.

Pharmaceutical interactions

Pharmaceutically incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.

Overdose

Symptoms: toxic reactions – hearing loss, ataxia, dizziness, urination disorders, thirst, loss of appetite, nausea, vomiting, ringing or a feeling of congestion in the ears, breathing problems.

Treatment: to relieve the blockade of neuromuscular transmission and its consequences – hemodialysis or peritoneal dialysis; anticholinesterase drugs, calcium salts, mechanical ventilation, other symptomatic and supportive therapy.

Functional features

Suction

After intramuscular administration, it is absorbed quickly and completely. Cmax in blood plasma with intramuscular administration at a dose of 7.5 mg/kg is 21 mcg/ml, after 30 minutes of intravenous infusion at a dose of 7.5 mg/kg is 38 mcg/ml. After IM administration, Tmax is about 1.5 hours.

The average therapeutic concentration with intravenous or intramuscular administration lasts for 10-12 hours.

Distribution

Plasma protein binding is 4-11%. Vd in adults – 0.26 l/kg, in children – 0.2-0.4 l/kg, in newborns: less than 1 week old and weighing less than 1500 g – up to 0.68 l/kg, less than 1 week old and weighing more than 1500 g – up to 0.58 l/kg, in patients with cystic fibrosis – 0.3-0.39 l/kg.

Well distributed in extracellular fluid (abscess contents, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal fluid); found in high concentrations in urine; in low levels – in bile, breast milk, aqueous humor of the eye, bronchial secretions, sputum and cerebrospinal fluid. Penetrates well into all tissues of the body, where it accumulates intracellularly; high concentrations are observed in organs with good blood supply: lungs, liver, myocardium, spleen, and especially in the kidneys, where they accumulate in the cortex; lower concentrations are found in muscles, adipose tissue and bones.

When administered in moderate therapeutic doses (normally) to adults, amikacin does not penetrate the BBB; with inflammation of the meninges, permeability increases slightly. Neonates achieve higher concentrations in the cerebrospinal fluid than adults. Penetrates the placental barrier: found in fetal blood and amniotic fluid.

Metabolism

Not metabolized.

Removal

T1/2 in adults – 2-4 hours, in newborns – 5-8 hours, in older children – 2.5-4 hours. Final T1/2 – more than 100 hours (release from intracellular depots).

It is excreted by the kidneys by glomerular filtration (65-94%), mainly unchanged. Renal clearance – 79-100 ml/min.

Pharmacokinetics in special clinical situations

T1/2 in adults with impaired renal function varies depending on the degree of impairment – up to 100 hours, in patients with cystic fibrosis – 1-2 hours, in patients with burns and hyperthermia T1/2 may be shorter than the average due to increased clearance.

It is eliminated by hemodialysis (50% in 4-6 hours), peritoneal dialysis is less effective (25% in 48-72 hours).

Storage conditions

List B. The drug should be stored out of the reach of children, in a dry place, protected from light at a temperature of 5° to 25°C.

Shelf life

2 years

Manufacturer

Sintez, Russia