After intramuscular injection (in / m) of the injection is absorbed quickly and completely. The maximum concentration (Cmah) with an IM injection of 7.5 mg / kg - 21 mcg / ml, after 30 min IV infusion 7.5 mg / kg - 38 mcg / ml. Time to reach the maximum concentration (Tcmah) - about 1.5 hours after the / m introduction. Connection with plasma proteins - 4-11%.
It is well distributed in the extracellular fluid (the contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal fluid); in high concentrations is found in urine; at low - at bile, breast milk, watery eye moisture, bronchial secretion, sputum and cerebrospinal fluid (CSF). It penetrates well into all tissues of the body, where it accumulates intracellularly; high concentrations are noted in organs with good blood supply: lungs, liver, myocardium, spleen, and especially in the kidneys where it accumulates in the cortex, lower concentrations - in muscles, adipose tissue and bones.
At appointment in sredneverapepticheskih doses (in norm or rate) to adults amikacin does not penetrate the hemato-encephalic barrier (BBB), with inflammation of the meninges, the permeability slightly increases. In newborns, higher concentrations are achieved in CSF than in adults; passes through the placenta - is found in the fetal blood and amniotic fluid. The volume of distribution in adults is 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 grams - up to 0.58 l / kg, in cystic fibrosis patients - 0.3-0.39 l / kg. The average therapeutic concentration with IV or IM injection is maintained for 10-12 hours.
It is not metabolized. The half-life period (T1 / 2) in adults is 2-4 hours, in newborns 5-8 hours, in older children 2.5-4 hours. The final value of T1 / 2 is more than 100 hours (release from intracellular depots).
It is excreted by the kidneys by glomerular filtration (65-94%), mainly unchanged. Kidney clearance - 79-100 ml / min.
T1 / 2 in adults with renal dysfunction varies depending on the degree of impairment - up to 100 h, in patients with cystic fibrosis - 1 -2 h, in patients with burns and hyperthermia T1 / 2 may be shorter in comparison with the average values due to elevated clearance .
It is excreted during hemodialysis (50% for 4-6 hours), peritoneal dialysis is less effective (25% for 48-72 hours).