After intramuscular (IM injection) absorbed quickly and completely. The maximum concentration (CmOh) with an IM injection of 7.5 mg / kg - 21 μg / ml, after 30 minutes of intravenous (IV) infusion 7.5 mg / kg - 38 μg / ml. Time to reach the maximum concentration (TCmOh) - 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 the urine; in low - in 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 blood-brain 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 over body weight 1500 g - up to 0.58 l / kg, in patients with cystic fibrosis - 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. Half-life (T1/2) in adults 2-4 hours, in newborns 5-8 hours, in older children 2.5-4 hours. The final value of T1/2 - more than 100 hours (release from the intracellular depot).
It is excreted by the kidneys by glomerular filtration (65 - 94%) mostly 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 can be shorter compared with the average due to increased clearance.
It is excreted in hemodialysis (50% in 4-6 h), peritoneal dialysis is less effective (25 % for 48 - 72 hours).