АМИКОР

INSTRUCTIONSONMEDICALUSE

AMICOR 100

AMICOR 500

Trade name of the drug:Amicor100, Amikor500

Active ingredients (INN):amikacin sulfate

Dosage form: solution for injection

Composition:

Every 2 ml of solution contains:

for a dose of 100mg/2ml:

active substance:amikacin sulfate (as amikacin sulfate) – 100 mg;

excipients: methylparaben, propylparaben, sodium metabisulfite, sodium citrate dihydrate, water for injection.

for a dose of 500mg/2ml:

active substance:amikacin sulfate (as amikacin sulfate) – 500 mg;

excipients: methylparaben, propylparaben, sodium metabisulfite, sodium citrate dihydrate, water for injection.

Description:.

for a dose of 100 mg/2ml: transparent colorless solution;

for a dose of 500 mg/2ml: a transparent, colorless to slightly yellowish solution.

Pharmacotherapeutic group:antibiotic (aminoglycoside group)

ATC code: J01GB06

Pharmacological properties

Pharmacodynamics

Antibiotic of the aminoglycoside group. A semi-synthetic broad-spectrum antibiotic with 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 bacterial membranes cytoplasmically.

Highly active against aerobic gram-negative microorganisms:Pseudomonasaeruginosa,Escherichia < /em>coli,Klebsiellaspp.,Serratiaspp.,Providenciaspp.,Enterobacterspp., Salmonellaspp.,Shigellaspp em>., some gram-positive microorganisms:Staphylococcusspp. (including including resistant to penicillin and some cephalosporins).

The drug is moderately active against Streptococcusspp. When administered simultaneously with benzylpenicillin, it exhibits synergism against Enterococcusfaecalis strains.

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

Pharmacokinetics

Suction

After intramuscular administration, it is absorbed quickly and completely. C_max in blood plasma with IM administration of the drug at a dose of 7.5 mg/kg – 21 mcg/ml, after IV infusion at a dose of 7.5 mg/kg for 30 min – 38 mcg/ml. The time to reach C_max after IM administration is about 1.5 hours.

Distribution

Plasma protein binding 4-11%.

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 it accumulates in the cortex; lower concentrations are found in muscles, adipose tissue and bones.

In adults, when used in average therapeutic doses (normally), amikacin does not penetrate the BBB; with inflammation of the meninges, permeability increases slightly. Neonates achieve higher concentrations in the CSF than adults.

Amikacin penetrates the placental barrier and is found in fetal blood and amniotic fluid.

V_d 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 1.5 kg – up to 0.68 l/kg, at the age of less than 1 week and body weight over 1.5 kg — up to 0.58 l/kg, in patients with cystic fibrosis — 0.3-0.39 l/kg.

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

Metabolism

Not metabolized.

Removal

T_1/2 in the terminal (β) phase in adults – 2-4 hours, in newborns – 5-8 hours, in older children – 2.5-4 hours. Final value T< sub>1/2 — more than 100 hours (release from intracellular depots).

Excreted by the kidneys by glomerular filtration (65-94%) mainly unchanged