Gentamycin

General characteristics. Structure:

Active ingredient: 40 mg of Gentamycini sulfas in 1 ml of solution.

Pharmacological properties:

Pharmacodynamics. Gentamycini sulfas is characterized by a wide range of antimicrobic action. It is active concerning the majority of gram-negative and gram-positive microorganisms: Pseudomonas aeruginosa, Escherichia coli, Proteus spp., Klebsiella spp., Serratia spp., Salmonella spp., Shigella spp., Staphylococcus spp., including in the relation it is multiple resistant strains. Is less active concerning streptococci of different types and gram-negative cocci. Drug does not affect anaerobic bacteria, mushrooms, viruses.

Gentamycini sulfas has bactericidal effect. Actively getting through a cellular membrane of bacteria, communicates with 30S in subunit of bacterial ribosomes and activator protein synthesis oppresses.

Pharmacokinetics. The maximum concentration of gentamycin in blood serum is reached in 1 hour after intramuscular introduction. At intravenous drop administration within the first two hours concentration of an antibiotic in blood exceeds observed at intramuscular introduction. At both ways of introduction therapeutic concentration of drug remain within 8 hours. At endolymphatic introduction of concentration of gentamycin in blood serum in the first 6 hours are close to those at intramuscular introduction; therapeutic activity remains within 12 — 24 hours. At patients with disturbance of secretory function of kidneys concentration of drug in blood increases. Normal at parenteral administration badly gets through a blood-brain barrier; at meningitis its concentration in cerebrospinal fluid increases. The antibiotic is found in therapeutic concentration in kidneys, lungs, in exudates of pleural and peritoneal cavities. Gets through a placenta. It is not metabolized. It is removed by kidneys (70 — 95%), partially allocated with bile.

Indications to use:

Medicine is appointed at sepsis, meningitis, peritonitis, a septic endocarditis; infectious and inflammatory diseases of a respiratory organs (pneumonia, pleura empyema, lung abscess), infections of kidneys and urinary tract; the infected burns and other diseases caused by preferential gram-negative microorganisms steady against antibiotics.

Gentamycin is shown at is purulent - the septic diseases arising at patients with leukoses and malignant new growths against the background of the carried-out cytostatic, radiation therapy and at use of immunodepressants. The endolymphatic way of introduction is used at patients with a severe disease when other methods of treatment are inefficient.

Route of administration and doses:

Gentamycini sulfas is applied intramusculary, intravenously (kapelno), by endolimfatichesk. The maximum daily dose at adults and children at intramuscular and intravenous administration makes 5 mg/kg, at endolymphatic — 2 mg/kg. The single dose for adults and children is more senior than 14 years at infections of urinary tract makes 0,4 mg/kg, daily — 0,8 — 1,2 mg/kg. At the heavy course of an infection the daily dose can be increased to 3 mg/kg. At sepsis and other heavy infections (peritonitis, destructive pneumonia, abscess of lungs, etc.) depending on weight of process the single dose for adults and children is more senior than 14 years makes 0,8 — 1 mg/kg, daily — 2,4 — 3,2 mg/kg. Children of younger age, especially have the first weeks lives, gentamycin is recommended to be applied only according to vital indications at heavy infections (sepsis, a septic endocarditis, meningitis, peritonitis). The daily dose of Gentamycini sulfas at newborns and babies makes 2 — 5 mg/kg; children of 1 — 5 years have 1,5 — 3 mg/kg; 6 — 14 years — 3 mg/kg. The daily dose of drug is entered into 2 — 3 receptions.

At intravenous administration the single dose of drug for adults is parted in 200 ml (for children — in 50 — 100 ml) 5% of solution of glucose or isotonic solution of sodium chloride. The drug is administered by 2 times a day with a speed of 60 thaws a minute. Concentration of drug in solution should not exceed 1 mg/ml.

At a renal failure the scheme of introduction is adjusted by reduction of doses or lengthening of intervals between introductions. When carrying out a hemodialysis the single dose of an antibiotic is in addition entered.

Treatment duration at intramuscular introduction makes 7 — 10 days, at intravenous — 2 — 3 days with the subsequent transition on intramuscular.

Endolimfaticheski the drug is administered in peripheral absorbent vessels on foot or in the lower third of a shin slowly (with a speed of 0,5 — 1 ml of 1 min.) 1 — 2 time a day with an interval by not less than 12 hours. The course of treatment consists of 3 — 8 introductions within 5 — 10 days.

Features of use:

With care apply gentamycin at parkinsonism, a myasthenia, renal failures.

Side effects:

At use of drug a hearing disorder and balances, damages of kidneys, a headache, nausea, vomiting, spasms, muscular weakness, changes of cellular composition of blood (anemia, a leukopenia, thrombocytopenia, a granulocytopenia), increase in activity of hepatic transaminases, a hyperbilirubinemia, allergic reactions (a skin itch, a small tortoiseshell) is possible.

At endolymphatic administration of gentamycin the first minutes there can be a feeling of "pricking" on the course of absorbent vessel which usually quickly disappears.

Interaction with other medicines:

At simultaneous use with aminoglycosides, Vancomycinum, cephalosporins, Acidum etacrynicum strengthening from - and nephrotoxic action is possible. Strengthens (mutually) effect of a karbenitsillin, benzylpenicillin and cephalosporins.

At simultaneous use with indometacin, loopback diuretics (including furosemide), concentration of gentamycin increases in a blood plasma, the risk of side effect increases.

Muscle relaxants increase probability of paralysis of breath.

At simultaneous use with means for an inhalation anesthesia, opioid analgetics the risk of development of neuromuscular blockade up to development of an apnoea increases.

Contraindications:

Use of gentamycin is contraindicated at an allergy to drug. Gentamycin should not be applied at heavy renal failures, uraemia, at diseases of the acoustical and vestibular devices connected with neuritis of the 8th couple of cranial nerves, myasthenias, during breastfeeding (it is necessary to stop for treatment), at pregnancy if it is not caused by vital indications.

It is impossible to appoint drug at the same time or consistently with others from - and nephrotoxic drugs, and also with loopback diuretics. Endolimfaticheski Gentamycini sulfas should not be entered at the diseases which are followed by disturbance of outflow of a lymph (a limfodema, a lymphostasis, лимфосклероз the inborn or acquired character), existence of ulcers, a wound or inflammatory surface in the field of introduction to absorbent vessel.

Storage conditions:

To store at a temperature not above 25 °C. Period of validity of 5 years.

Issue conditions:

According to the recipe

Packaging:

Solution for injections 40mg/ml in ampoules of 2 ml in packaging No. 10.