Amikacin powder d / prig. solution for injection 1000mg, No. 1

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

• respiratory tract infections (bronchitis, pneumonia, pleural empyema, lung abscess);

• sepsis;

• septic endocarditis;

• CNS infections (including meningitis);

• infections of the abdominal cavity (including peritonitis);

• urinary 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.

The drug is administered intramuscularly, intravenously (jet, within 2 minutes or drip) to adults and children over 6 years old - 5 mg / kg every 8 hours or 7.5 mg / kg every 12 hours.

For bacterial urinary tract infections (uncomplicated) - 250 mg every 12 hours; after a hemodialysis session, an additional dose of 3-5 mg / kg may be prescribed. The maximum dose for adults is 15 mg / kg / day, but not more than 1.5 g / day for 10 days. The duration of treatment with intravenous administration is 3-7 days, with intramuscular injection - 7-10 days.

For premature newborns, the initial single dose is 10 mg / kg, then 7.5 mg / kg every 18-24 hours; for newborns and children under 6 years of age, the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.

For infected burns, a dose of 5-7.5 mg / kg every 4-6 hours may be required due to the shorter T1 / 2 (1-1.5 hours) in this category of patients.

Intravenous amikacin is injected drip for 30-60 minutes, if necessary - jet. For intravenous administration (drip), the drug is pre-diluted with 200 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution. The concentration of amikacin in a solution for intravenous administration should not exceed 5 mg / ml.

In case of impaired renal excretory function, a dose reduction or an increase in the intervals between injections is necessary. In the case of an increase in the interval between injections (if the CC value is unknown, and the patient's condition is stable), the interval between the administration of the drug is set according to the following formula: interval (h) = serum creatinine concentration? 9. If the concentration of serum creatinine is 2 mg / dl, then the recommended single dose (7.5 mg / kg) should be administered every 18 hours. If the interval is increased, the single dose is not changed. In the case of a single dose reduction with an unchanged dosage regimen, the first dose for patients with renal insufficiency is 7.5 mg / kg. Subsequent doses are calculated using the following formula: Subsequent dose (mg) administered every 12 hours = CC (ml / min) in the patient? initial dose (mg) / CC is normal (ml / min).

Powder for preparation of solution for intravenous and intramuscular administration of white or almost white color, hygroscopic.

1 fl. amikacin (in the form of sulfate) 1 g

• Acoustic neuritis;

• severe chronic renal failure with azotemia and uremia;

• pregnancy;

• hypersensitivity to drug components;

• a history of hypersensitivity to other aminoglycosides.

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

pharmachologic effect

Semisynthetic broad-spectrum antibiotic from the group of aminoglycosides, has a bactericidal effect. By binding to the 30S ribosome subunit, it prevents the formation of a complex of transport and messenger RNA, 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, 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 action of enzymes that inactivate other aminoglycosides, and may remain active against Pseudomonas aeruginosa strains resistant to tobramycin, gentamicin and netilmicin.

Pharmacokinetics

Suction

After i / m administration, it is absorbed quickly and completely. Cmax in blood plasma with intramuscular injection at a dose of 7.5 mg / kg - 21 ?g / ml, after 30 minutes of intravenous infusion at a dose of 7.5 mg / kg - 38 ?g / ml. After intramuscular administration, Tmax is about 1.5 hours. The average therapeutic concentration with intravenous or intramuscular administration is maintained 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: at the age of less than 1 week and weighing less than 1500 g - up to 0.68 l / kg, at the age of less than 1 week and weighing more than 1500 g - up to 0.58 l / kg, in patients with cystic fibrosis - 0.3-0.39 l / kg. It is well distributed in the extracellular fluid (contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal fluid); found in high concentrations in urine; in low - in bile, breast milk, aqueous humor of the eye, bronchial secretions, sputum and cerebrospinal fluid. It 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 it accumulates in the cortical substance, lower concentrations - in muscles, adipose tissue and bones. When administered in medium therapeutic doses (normally) for adults, amikacin does not penetrate the BBB; with inflammation of the meninges, the permeability increases slightly. Newborns achieve higher cerebrospinal fluid concentrations than adults. Penetrates the placental barrier: is found in fetal blood and amniotic fluid. Metabolism Not metabolized. Excretion of 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.adipose tissue and bones. When administered in medium therapeutic doses (normally) for adults, amikacin does not penetrate the BBB; with inflammation of the meninges, the permeability increases slightly. Newborns achieve higher cerebrospinal fluid concentrations than adults. Penetrates the placental barrier: is found in fetal blood and amniotic fluid. Metabolism Not metabolized. Excretion of 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.adipose tissue and bones. When administered in medium therapeutic doses (normally) for adults, amikacin does not penetrate the BBB; with inflammation of the meninges, the permeability increases slightly. Newborns achieve higher cerebrospinal fluid concentrations than adults. Penetrates the placental barrier: is found in fetal blood and amniotic fluid. Metabolism Not metabolized. Excretion of 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.with inflammation of the meninges, the permeability increases slightly. Newborns achieve higher cerebrospinal fluid concentrations than adults. Penetrates the placental barrier: is found in fetal blood and amniotic fluid. Metabolism Not metabolized. Excretion of 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.with inflammation of the meninges, the permeability increases slightly. In newborns, higher concentrations in the cerebrospinal fluid are achieved than in adults. Penetrates the placental barrier: is found in fetal blood and amniotic fluid. Metabolism Not metabolized. Excretion of 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.Excretion of 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.Excretion of 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 cases 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 averages due to increased clearance. It is excreted during hemodialysis (50% in 4-6 hours), peritoneal dialysis is less effective (25% in 48-72 hours).

Side effect

From the digestive system: nausea, vomiting, liver dysfunction (increased activity of hepatic transaminases, hyperbilirubinemia). From the hematopoietic system: anemia, leukopenia, granulocytopenia, thrombocytopenia. From the side of the central nervous system and peripheral nervous system: headache, drowsiness, neurotoxic effects (muscle twitching, feeling of numbness, tingling, epileptic seizures), impaired neuromuscular transmission (respiratory arrest). From the senses: ototoxicity (hearing loss, vestibular and labyrinthine disorders, irreversible deafness), toxic effects on the vestibular apparatus (discoordination of movements, dizziness, nausea, vomiting). From the urinary system: nephrotoxicity - impaired renal function (oliguria, proteinuria, microhematuria). Allergic reactions: skin rash, itching,hyperemia of the skin, fever, Quincke's edema. Local reactions: pain at the injection site, dermatitis, phlebitis and periphlebitis (with intravenous injection).

Application during pregnancy and lactation

The drug is contraindicated in pregnancy. In the presence of vital indications, the drug can be used in nursing women. It should be borne in mind that aminoglycosides are excreted in breast milk in small quantities. They are poorly absorbed from the gastrointestinal tract, and there are no associated complications in infants.

Application for impaired renal function

Use is contraindicated in severe chronic renal failure with azotemia and uremia. In case of impaired renal excretory function, correction of the dosage regimen is required.

Application in children

For premature newborns, the initial single dose is 10 mg / kg, then 7.5 mg / kg every 18-24 hours; for newborns and children under 6 years of age, the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.

Use in elderly patients

The drug should be used with caution in elderly patients.

special instructions

Before use, the sensitivity of the isolated pathogens is determined using discs containing 30 ?g of amikacin. With a diameter of the free from growth 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 ?g / ml (the therapeutic concentration is 15-25 ?g / ml). During the treatment period, it is necessary to monitor the function of the kidneys, auditory nerve and vestibular apparatus at least 1 time per week. The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as with the appointment of high doses or for a long time (in this category of patients, daily monitoring of renal function may be required). In case of unsatisfactory audiometric tests, the dose of the drug is reduced or treatment is stopped.Patients with infectious and inflammatory diseases of the urinary tract are advised to take an increased amount of fluid with adequate diuresis. In the absence of positive clinical dynamics, one should bear in mind the possibility of the development of resistant microorganisms. In such cases, it is necessary to discontinue treatment and begin appropriate therapy. Disulfite contained in the sodium preparation can cause the development of allergic complications in patients (up to anaphylactic reactions), especially in patients with an allergic history.In such cases, it is necessary to discontinue treatment and begin appropriate therapy. Disulfite contained in the sodium preparation can cause the development of allergic complications in patients (up to anaphylactic reactions), especially in patients with an allergic history.In such cases, it is necessary to discontinue treatment and begin appropriate therapy. Disulfite contained in the sodium preparation can cause the development of allergic complications in patients (up to anaphylactic reactions), especially in patients with an allergic history.

Overdose

Symptoms: toxic reactions - hearing loss, ataxia, dizziness, urination disorders, thirst, loss of appetite, nausea, vomiting, ringing or a feeling of stuffiness in the ears, respiratory failure. Treatment: to remove the blockade of neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis; anticholinesterase drugs, calcium salts, mechanical ventilation, other symptomatic and supportive therapy.

Drug interactions

Shows synergism when interacting with carbenicillin, benzylpenicillin, cephalosporins (in patients with severe chronic renal failure, when combined with beta-lactam antibiotics, the effectiveness of aminoglycosides may decrease). Nalidixic acid, polymyxin B, cisplatin, and vancomycin increase the risk of ototoxicity 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 serum concentration, increasing nephro- and neurotoxicity. Amikacin enhances the muscle relaxant effect of curariform drugs. With simultaneous use with amikacin, methoxyflurane, polymyxins for parenteral administration, capreomycin and other drugs,blocking neuromuscular transmission (halogenated hydrocarbons - means for 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 the toxic effect of aminoglycosides (increased T1 / 2 and decreased clearance). Amikacin reduces the effectiveness of anti-myasthenic drugs. Pharmaceutical interactions Pharmaceutical incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.Transfusing large amounts of blood with citrate preservatives increases the risk of respiratory arrest. Parenteral administration of indomethacin increases the risk of developing the toxic effect of aminoglycosides (increased T1 / 2 and decreased clearance). Amikacin reduces the effectiveness of anti-myasthenic drugs. Pharmaceutical interactions Pharmaceutical incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.Transfusing large amounts of blood with citrate preservatives increases the risk of respiratory arrest. Parenteral administration of indomethacin increases the risk of developing the toxic effect of aminoglycosides (increased T1 / 2 and decreased clearance). Amikacin reduces the effectiveness of anti-myasthenic drugs. Pharmaceutical interactions Pharmaceutical incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.Pharmaceutical interactions Pharmaceutical incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.Pharmaceutical interactions Pharmaceutical incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins B and C, potassium chloride.