Peak concentrations aminoglycosides varies between different patients, because they depend on the volume of distribution. The volume of distribution, in turn, depends on body weight, fluid volume and adipose tissue of the patient. For example, patients with extensive burns, ascites volume of distribution of aminoglycosides is increased. On the contrary, dehydration, or muscular dystrophy, it decreases. Aminoglycosides are distributed in the extracellular fluids, including blood serum, exudate abscesses, ascitic, pericardial, pleural, synovial, peritoneal and lymphatic fluid.
Capable of creating high concentrations in organs with a good blood supply: Liver, lungs, kidneys (where they accumulate in the cortex). Low concentrations are found in sputum, bronchial secretions, bile, breast milk. Aminoglycosides are poorly through the BBB. When inflammation of the meninges, the permeability of several increases. Babies in the CSF reached a higher concentration than in adults.
Aminoglycosides are not metabolized, the kidneys by glomerular filtration as unchanged, creating a high concentration in urine. Excretion rate depends on age, renal function and patient comorbidities. In patients with fever, it may increase with decreasing kidney function slows down considerably. People elderly because of reduced glomerular filtration rate may also slow excretion. The half-life of aminoglycosides in adults with normal renal function is 2-4 hours, in the newborn – 5-8 hours in children – 2.5-4 h. In renal failure the half-life can increase up to 70 hours or more. Indications Empiric therapy (in most cases is prescribed in combination with -lactams, glycopeptides or antianaerobnymi drugs, Depending on the alleged agents): Sepsis of unknown etiology. Infective endocarditis. Post-traumatic and postoperative meningitis. Fever in neutropenic patients. Nosocomial pneumonia (including ventilation). Pyelonephritis. Intra-abdominal infections. Pelvic infection. Diabetic foot. Postoperative or post-traumatic osteomyelitis. Septic arthritis. Local therapy: eye infection – bacterial conjunctivitis and keratitis. Specific therapy: Plague (streptomycin). Tularemia (streptomycin, gentamicin). Brucellosis (streptomycin). Tuberculosis (streptomycin, kanamycin). Antibiotic prophylaxis: Decontamination bowel before elective surgery on the colon (neomycin or kanamycin in combination with erythromycin). Aminoglycosides can be used to treat community-acquired pneumonia in both outpatient and in-patient conditions. This is due to the lack of activity of this group of antibiotics for the primary causative agent – the pneumococcus. In the treatment of nosocomial pneumonia aminoglycosides administered parenterally. Intratracheal instillation aminoglycosides because of the unpredictable pharmacokinetics does not improve clinical efficacy. It is wrong for the appointment of aminoglycoside therapy, shigellosis and salmonellosis (both inside and parenterally) because they are clinically ineffective against pathogens, which are localized intracellularly. Aminoglycosides are not recommended for monotherapy staph infections, since there Other effective but less toxic drugs antistafilokokkovye. Aminoglycosides should not be used for the treatment of uncomplicated infections IMP, except in cases where the pathogen is resistant to other, less toxic antibiotics. Aminoglycosides also should not be used for local application in the treatment of skin infections due to the rapid development of resistance in microorganisms. You should avoid the use of aminoglycosides for flow-through drainage and irrigation of the abdominal cavity due to their severe toxicity. From market analysis of substances of antibiotics can be found in the report of the Academy of IKAR industrial markets "Market substances antibiotics in Russia. "