Overview
Blocks the 30S subunit of ribosomes and inhibits protein synthesis. At higher concentrations, it disrupts the function of the cytoplasmic membranes, Bramitob cell death. Suppresses the growth and development of gram-negative and gram-positive microorganisms. Most active against Staphylococcus spp., including Staphylococcus aureus and Staphylococcus epidermidis (coagulase-negative and coagulase-positive), including penicillin resistant strains, Citrobacter spp., Streptococcus spp., including some groups are beta-hemolytic species of group A, some non-hemolytic species and Streptococcus pneumoniae; Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Morganella morganii, Proteus mirabilis, most strains Proteus vulgaris, Haemophilus influenzae, Haemophilus aegyptius, Moraxella lacunata, Acinetobacter calcoaceticus, some species Neisseria. Tests for bacterial sensitivity show that in some cases gentamicin-resistant Bramitob remain sensitive to tobramycin.
It is poorly absorbed from the gastrointestinal tract, rapidly absorbed by intramuscular administration. Cmax reached in 30–90 minutes. A single i / m injection at a dose of 1 μg / kg provides a concentration in the serum of 4 μg / ml for 8 hours. With an intravenous infusion for 1 hour, the concentration in the serum is similar to that for i / m administration. Therapeutic serum concentration is typically 4–6 μg / ml. It practically does not bind to plasma proteins. In patients with normal renal function, except for newborns, tobramycin sulfate, administered every 8 hours, does not cumulate in serum. In patients with other renal function and newborns, serum antibiotic concentrations are usually higher and can be determined over a longer period of time. It penetrates sputum, peritoneal and synovial fluids, the contents of the abscess. Almost does not penetrate the intact BBB. Passes through the placenta. It is excreted by the kidneys unchanged by glomerular Bramitob, in patients with normal renal function, 84% of the dose is excreted within 8 hours, 93% in 24 hours. The maximum concentration in the urine, determined after a / m injection of a single dose of 1 mg / kg, 75–100 mcg / ml. Follow case of impaired renal function, Chlormic excretion of tobramycin sulfate slows down and the cumulation of the substance can create a toxic level in serum. T1/2 2 hours from serum. 25–70% is removed by dialysis (depending on the duration and type of dialysis).
When applied topically in ophthalmology, systemic absorption is negligible.
Indications.
For systemic use: infectious diseases caused by sensitive microflora - infections of the biliary tract, bones and joints (including osteomyelitis), central nervous system (including meningitis), infections of the abdominal cavity (including peritonitis), respiratory organs (including including pneumonia, pleural empyema, lung abscess), skin and soft tissue infections (including infected burns), urinary tract infections (including pyelonephritis, pyelitis, cystitis), sepsis, postoperative infections.
In ophthalmology: bacterial infections of the eye and its appendages caused by sensitive microflora, including blepharitis, conjunctivitis, keratoconjunctivitis, blepharoconjunctivitis, keratitis, iridocyclitis.
Contraindications.
Hypersensitivity, including to other aminoglycosides; severe chronic renal failure, dysfunction of Bramitob VIII pair of cranial nerves, auditory nerve neuritis.
Application restrictions.
Renal failure, botulism, myasthenia gravis, parkinsonism, dehydration, advanced age.
Side effects.
For systemic use
From the digestive tract: nausea, vomiting, diarrhea, impaired liver function (increased activity of hepatic transaminases, LDH, bilirubin level).
From the cardiovascular system and blood (hematopoiesis, hemostasis): anemia, leukopenia, leukocytosis, granulocytopenia, thrombocytopenia.
From the nervous system and sensory organs: ototoxicity - irreversible damage to the vestibular and auditory branches of the VIII pair of cranial nerves with partial or complete bilateral deafness, dizziness, vertigo, tinnitus; headache, disorientation, drowsiness, paresthesia, muscle fasciculations, cramps.
From the genitourinary system: nephrotoxicity (oliguria, cylindruria, proteinuria, tubular disorders, increased levels of creatinine and urea nitrogen, a significant increase or decrease in the frequency of urination, polyuria, thirst).
Allergic reactions: pruritus, skin hyperemia, rash, fever, angioedema, eosinophilia.
Other: hypocalcemia, hyponatremia, hypomagnesemia.
